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SI3523302T1 - Substituirane spojine pirazolo(1,5-A)piridina kot inhibitorji ret kinaze - Google Patents

Substituirane spojine pirazolo(1,5-A)piridina kot inhibitorji ret kinaze

Info

Publication number
SI3523302T1
SI3523302T1 SI201731196T SI201731196T SI3523302T1 SI 3523302 T1 SI3523302 T1 SI 3523302T1 SI 201731196 T SI201731196 T SI 201731196T SI 201731196 T SI201731196 T SI 201731196T SI 3523302 T1 SI3523302 T1 SI 3523302T1
Authority
SI
Slovenia
Prior art keywords
kinase inhibitors
pyridine compounds
ret kinase
substituted pyrazolo
pyrazolo
Prior art date
Application number
SI201731196T
Other languages
English (en)
Inventor
Steven W. Andrews
Sean Aronow
James F. Blake
Barbara J. Brandhuber
James Collier
Adam Cook
Julia Haas
Yutong Jiang
Gabrielle R. Kolakowski
Elizabeth A. Mcfaddin
Megan L. Mckenney
Oren T. MCKNULTY
Andrew T. Metcalf
David A. Moreno
Ginelle A. Ramann
Tony P. Tang
Li Ren
Shane M. Walls
Original Assignee
Array Biopharma, Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Array Biopharma, Inc. filed Critical Array Biopharma, Inc.
Publication of SI3523302T1 publication Critical patent/SI3523302T1/sl

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41621,2-Diazoles condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12Antidiarrhoeals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
SI201731196T 2016-10-10 2017-10-10 Substituirane spojine pirazolo(1,5-A)piridina kot inhibitorji ret kinaze SI3523302T1 (sl)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201662406275P 2016-10-10 2016-10-10
US201762447849P 2017-01-18 2017-01-18
US201762491180P 2017-04-27 2017-04-27
US201762531690P 2017-07-12 2017-07-12
US201762566030P 2017-09-29 2017-09-29
EP17787844.4A EP3523302B1 (en) 2016-10-10 2017-10-10 Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
PCT/US2017/055993 WO2018071454A1 (en) 2016-10-10 2017-10-10 Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors

Publications (1)

Publication Number Publication Date
SI3523302T1 true SI3523302T1 (sl) 2022-09-30

Family

ID=60153576

Family Applications (1)

Application Number Title Priority Date Filing Date
SI201731196T SI3523302T1 (sl) 2016-10-10 2017-10-10 Substituirane spojine pirazolo(1,5-A)piridina kot inhibitorji ret kinaze

Country Status (35)

Country Link
US (5) US10144734B2 (sl)
EP (2) EP3523302B1 (sl)
JP (1) JP7075399B2 (sl)
KR (1) KR102287752B1 (sl)
CN (1) CN110177786B (sl)
AU (1) AU2017342027B2 (sl)
BR (1) BR112019007143A2 (sl)
CA (1) CA3039912A1 (sl)
CL (1) CL2019000942A1 (sl)
CO (1) CO2019004649A2 (sl)
CR (1) CR20190224A (sl)
CY (1) CY1125606T1 (sl)
DK (1) DK3523302T3 (sl)
DO (1) DOP2019000091A (sl)
EC (1) ECSP19033052A (sl)
ES (1) ES2926136T3 (sl)
HR (1) HRP20221154T1 (sl)
HU (1) HUE060089T2 (sl)
IL (1) IL265918B (sl)
JO (1) JOP20190077A1 (sl)
LT (1) LT3523302T (sl)
MD (1) MD3523302T2 (sl)
MX (1) MX2019004204A (sl)
PE (1) PE20191613A1 (sl)
PH (1) PH12019500776A1 (sl)
PL (1) PL3523302T3 (sl)
PT (1) PT3523302T (sl)
RS (1) RS63510B1 (sl)
SA (1) SA519401544B1 (sl)
SG (1) SG11201903187WA (sl)
SI (1) SI3523302T1 (sl)
TN (1) TN2019000107A1 (sl)
TW (1) TWI752098B (sl)
UA (1) UA125032C2 (sl)
WO (1) WO2018071454A1 (sl)

Families Citing this family (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2018000577A (es) 2015-07-16 2018-09-05 Array Biopharma Inc Compuestos de pirazolo[1,5-a]piridina sustituidos como inhibidores de la ret quinasa.
HUE064659T2 (hu) 2015-11-02 2024-04-28 Blueprint Medicines Corp RET inhibitorai
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret
WO2018091687A1 (en) * 2016-11-18 2018-05-24 Integrative Research Laboratories Sweden Ab Novel azetidine derivatives useful as modulators of cortical catecholaminergic neurotransmission
ES2948194T3 (es) 2017-01-18 2023-09-01 Array Biopharma Inc Compuestos de pirazolo[1,5-a]pirazina sustituida como inhibidores de la cinasa RET
TWI791053B (zh) * 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
EP3740491A1 (en) 2018-01-18 2020-11-25 Array Biopharma, Inc. Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors
EP3740490A1 (en) 2018-01-18 2020-11-25 Array Biopharma, Inc. Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors
CN111615514B (zh) 2018-01-18 2022-10-11 奥瑞生物药品公司 作为ret激酶抑制剂的取代的吡唑并[4,3-c]吡啶化合物
EP4353317A3 (en) 2018-04-03 2024-05-08 Blueprint Medicines Corporation Ret inhibitor for use in treating cancer having a ret alteration
US11964988B2 (en) 2018-09-10 2024-04-23 Array Biopharma Inc. Fused heterocyclic compounds as RET kinase inhibitors
KR102558308B1 (ko) * 2018-09-27 2023-07-24 주식회사 엘지화학 3-아자바이사이클로[3,1,1]헵탄 유도체 및 이를 포함하는 약제학적 조성물
CN112771047A (zh) * 2018-09-27 2021-05-07 重庆复创医药研究有限公司 作为RET激酶抑制剂的取代的咪唑[1,2-a]吡啶和[1,2,4]三唑[1,5-a]吡啶化合物
US20210379056A1 (en) * 2018-09-30 2021-12-09 Applied Pharmaceutical Science, Inc. Substituted pyrazole fused ring derivative, preparation method therefor, and application thereof
WO2020094084A1 (zh) * 2018-11-07 2020-05-14 南京明德新药研发有限公司 作为ret抑制剂的三并环衍生物
AU2019387370A1 (en) 2018-11-30 2021-06-10 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
CA3117854A1 (en) * 2018-12-07 2020-06-11 Sunshine Lake Pharma Co., Ltd. Ret inhibitors, pharmaceutical compositions and uses thereof
KR20210100155A (ko) * 2018-12-07 2021-08-13 선샤인 레이크 파르마 컴퍼니 리미티드 Ret 억제제, 이의 약학 조성물 및 용도
AU2020242287A1 (en) 2019-03-21 2021-09-02 INSERM (Institut National de la Santé et de la Recherche Médicale) A Dbait molecule in combination with kinase inhibitor for the treatment of cancer
CN111808077B (zh) 2019-04-12 2023-05-02 浙江海正药业股份有限公司 哌嗪酰胺衍生物,其制备方法及其在医药上的用途
CA3137887A1 (en) * 2019-05-14 2020-11-19 Yidong Su Inhibitor containing bicyclic derivative, preparation method therefor and use thereof
WO2020248972A1 (en) * 2019-06-10 2020-12-17 Js Innopharm (Shanghai) Ltd Heterocyclic compounds as kinase inhibitors, compositions comprising the heterocyclic compound, and methods of use thereof
CN112442050B (zh) * 2019-09-04 2024-08-09 广东东阳光药业股份有限公司 一种ret抑制剂、其药物组合物及其用途
CN112574236B (zh) * 2019-09-29 2024-08-09 广东东阳光药业股份有限公司 一种ret抑制剂、其药物组合物及其用途
WO2021057963A1 (zh) * 2019-09-29 2021-04-01 广东东阳光药业有限公司 一种ret抑制剂、其药物组合物及其用途
WO2021088911A1 (zh) * 2019-11-08 2021-05-14 杭州邦顺制药有限公司 作为ret激酶抑制剂的3、6二氮杂双环[3.1.1]庚烷衍生物
WO2021089791A1 (en) 2019-11-08 2021-05-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
US20230095530A1 (en) * 2019-12-27 2023-03-30 TYK Medicines, Inc Compound used as ret kinase inhibitor and application thereof
CN113121524B (zh) * 2019-12-31 2023-04-25 南京创济生物医药有限公司 杂环亚砜亚胺化合物及其中间体、制备方法和应用
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN111410662B (zh) * 2020-03-27 2020-12-29 苏州信诺维医药科技有限公司 一种酪氨酸激酶抑制剂
CN111269229B (zh) * 2020-03-27 2021-02-12 苏州信诺维医药科技有限公司 一种治疗癌症的化合物
CN111285887B (zh) * 2020-03-27 2020-11-17 苏州信诺维医药科技有限公司 一种螺环化合物
CN111233899B (zh) * 2020-03-27 2020-12-29 苏州信诺维医药科技有限公司 一种ret抑制剂
CN113527291A (zh) * 2020-04-13 2021-10-22 广东东阳光药业有限公司 Ret抑制剂、其药物组合物及其用途
CN113527292A (zh) * 2020-04-13 2021-10-22 广东东阳光药业有限公司 一种ret抑制剂、其药物组合物及其用途
CN113527290A (zh) * 2020-04-13 2021-10-22 广东东阳光药业有限公司 一种ret抑制剂、其药物组合物及其用途
CN115605477B (zh) * 2020-04-22 2024-07-05 深圳众格生物科技有限公司 一种吡唑并[1,5-a]吡啶类衍生物及其制备方法,组合物以及用途
CN113620944B (zh) * 2020-05-07 2024-10-15 广东东阳光药业股份有限公司 新型的ret抑制剂、其药物组合物及其用途
CN113683611A (zh) * 2020-05-18 2021-11-23 广东东阳光药业有限公司 新的ret抑制剂、其药物组合物及其用途
CN113683610A (zh) * 2020-05-18 2021-11-23 广东东阳光药业有限公司 一种ret抑制剂、其药物组合物及其用途
EP4155304A4 (en) * 2020-05-20 2024-05-29 TYK Medicines Inc. COMPOUND USED AS RET KINASE INHIBITOR AND ITS APPLICATION
US20230406865A1 (en) * 2020-11-13 2023-12-21 Shanghai Hansoh Biomedical Co., Ltd. Crystal form of free base of inhibitor containing bicyclic ring derivative and preparation method and application of crystal form
CA3234317A1 (en) 2021-10-22 2023-12-14 Wa Xian Methods and compositions for treating chronic inflammatory injury, metaplasia, dysplasia and cancers of epithelial tissues
WO2024006841A2 (en) * 2022-06-29 2024-01-04 Knowledge Pharmaceuticals Inc. Compositions for weight loss and cancer treatment
WO2024027690A1 (zh) * 2022-08-01 2024-02-08 江苏豪森药业集团有限公司 一种二并环类抑制剂的中间体及其制备方法
WO2024030968A1 (en) * 2022-08-03 2024-02-08 Brystol-Myers Squibb Company Compounds for modulating ret protein

Family Cites Families (264)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4783443A (en) 1986-03-03 1988-11-08 The University Of Chicago Amino acyl cephalosporin derivatives
US5844092A (en) 1994-03-18 1998-12-01 Genentech, Inc. Human TRK receptors and neurotrophic factor inhibitors
US5877016A (en) 1994-03-18 1999-03-02 Genentech, Inc. Human trk receptors and neurotrophic factor inhibitors
ATE335003T1 (de) 1996-05-08 2006-08-15 Biogen Idec Inc Ret-ligand 3 (retl3), um neurales und renales wachstum zu stimulieren
US6677135B1 (en) 1996-05-08 2004-01-13 Biogen, Inc. Ret ligand (RetL) for stimulating neutral and renal growth
US6682921B1 (en) 1996-08-21 2004-01-27 New York University Crystals of the tyrosine kinase domain of non-insulin receptor tyrosine kinases
US6531152B1 (en) 1998-09-30 2003-03-11 Dexcel Pharma Technologies Ltd. Immediate release gastrointestinal drug delivery system
AU7103900A (en) 1999-09-01 2001-03-26 Biogen, Inc. Ret ligand 5 (retl5) compositions and uses thereof
FI20000403A0 (fi) 2000-02-22 2000-02-22 Hannu Sariola GDNF perhesukuisten yhdisteiden käyttö kivessyövän hoitoon tarkoitettujen tuotteiden valmistamiseksi
CN100519749C (zh) 2000-06-22 2009-07-29 基因技术股份有限公司 抗trk-c拮抗剂的单克隆抗体
WO2003020698A2 (en) 2001-09-06 2003-03-13 Prochon Biotech Ltd. Protein tyrosine kinase inhibitors
PE20030762A1 (es) 2001-12-18 2003-09-05 Schering Corp Compuestos heterociclicos como antagonistas nk1
US7466344B2 (en) 2002-06-07 2008-12-16 Scimeasure Analytical Systems, Inc. High-speed low noise CCD controller
ITMI20021620A1 (it) 2002-07-23 2004-01-23 Novuspharma Spa Composto ad ativita' antitumorale
US20060116381A1 (en) 2002-07-24 2006-06-01 Fagin James A 4-4(methylpiperazin-1-ylmethyl)-n-[4-methyl-3-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-ben-zamide for treating mutated-ret kinase associated diseases
US7514446B2 (en) 2003-02-20 2009-04-07 Smithkline Beecham Corporation Pyrimidine compounds
US20090143399A1 (en) 2003-10-14 2009-06-04 Arizona Board Of Regents On Behalf Of The University Of Arizona Protein Kinase Inhibitors
US7169918B2 (en) 2003-10-27 2007-01-30 Genelabs Technologies, Inc. Methods for preparing 7-(2′-substituted-β-D-ribofuranosyl)-4-(NR2R3)-5-(substituted ethyn-1-yl)-pyrrolo[2,3-d]pyrimidine derivatives
MY141220A (en) 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
CA2546117A1 (en) 2003-11-21 2005-06-16 Novartis Ag 1h-imidazoquinoline derivatives as protein kinase inhibitors
RU2006122853A (ru) 2003-11-28 2008-01-10 Новартис АГ (CH) Производные диарилмочевины для лечения заболеваний, зависимых от протеинкиназы
PL1696920T3 (pl) 2003-12-19 2015-03-31 Plexxikon Inc Związki i sposoby opracowywania modulatorów Ret
GB0330043D0 (en) 2003-12-24 2004-01-28 Pharmacia Italia Spa Pyrrolo [2,3-b] pyridine derivatives active as kinase inhibitors process for their preparation and pharmaceutical compositions comprising them
GB0330042D0 (en) 2003-12-24 2004-01-28 Pharmacia Italia Spa Pyrrolo [2,3-b] pyridine derivatives active as kinase inhibitors process for their preparation and pharmaceutical compositions them
WO2005068424A1 (en) 2004-01-20 2005-07-28 Cell Therapeutics Europe S.R.L. Indolinone derivatives as receptor tyrosine kinase ihibitors
US20050222171A1 (en) 2004-01-22 2005-10-06 Guido Bold Organic compounds
PE20051089A1 (es) 2004-01-22 2006-01-25 Novartis Ag Derivados de pirazolo [1,5-a] pirimidin-7-il-amina como inhibidores de quinasa de proteina
WO2005099363A2 (en) 2004-03-26 2005-10-27 Whitehead Institute For Biomedical Research Methods of diagnosing, preventing and treating cancer metastasis
GB0512324D0 (en) 2005-06-16 2005-07-27 Novartis Ag Organic compounds
MX2007001399A (es) 2004-08-02 2007-04-18 Osi Pharm Inc Compuestos que inhiben pirrolopirimidina multi-cinasa aril-amino sustituidas.
PE20060664A1 (es) 2004-09-15 2006-08-04 Novartis Ag Amidas biciclicas como inhibidores de cinasa
WO2006050076A1 (en) 2004-10-29 2006-05-11 Janssen Pharmaceutica, N.V. Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders
EP1841465A4 (en) 2004-12-17 2009-04-01 Univ Pennsylvania STYLENE DERIVATIVES AND THEIR USE OF THE BINDING AND IMAGE DISPLAY OF AMYLOID PLAQUE
DE102005003687A1 (de) 2005-01-26 2006-07-27 Sphingo Tec Gmbh Immunoassay zur Bestimmung der Freisetzung von Neurotensin in die Zirkulation
GB0501999D0 (en) 2005-02-01 2005-03-09 Sentinel Oncology Ltd Pharmaceutical compounds
CN101257948A (zh) 2005-02-18 2008-09-03 阿特努奥恩公司 嘧啶并二氮䓬衍生物及吲哚并蝶啶化合物
GB0507575D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
EP1874731A4 (en) 2005-04-15 2009-08-05 Cylene Pharmaceuticals Inc CHINOBENZOXAZINANALOGA AND METHOD FOR THE APPLICATION
AU2006248780B2 (en) 2005-05-16 2010-06-03 Astrazeneca Ab Pyrazolylaminopyrimidine derivatives useful as tyrosine kinase inhibitors
US20100047777A1 (en) 2005-05-26 2010-02-25 The Johns Hopkins University Methods for identifying mutations in coding and non-coding dna
EP1896462A2 (en) 2005-05-31 2008-03-12 The Pfahl Family Trust (Dated 9 July 1996) Substituted biarylheterocycle derivatives as protein kinase inhibitors for the treatment of cancer and other diseases
US7541367B2 (en) 2005-05-31 2009-06-02 Janssen Pharmaceutica, N.V. 3-benzoimidazolyl-pyrazolopyridines useful in treating kinase disorders
ITRM20050290A1 (it) 2005-06-07 2006-12-08 Lay Line Genomics Spa Uso di molecole in grado di inibire il legame tra ngf e il suo recettore trka come analgesici ad effetto prolungato.
US7863288B2 (en) 2005-06-22 2011-01-04 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
GB0515026D0 (en) 2005-07-21 2005-08-31 Novartis Ag Organic compounds
PL1919979T5 (pl) 2005-08-25 2017-10-31 Creabilis Therapeutics Spa Polimerowe koniugaty K-252a i ich pochodne
JP2009519218A (ja) 2005-11-03 2009-05-14 エスジーエックス ファーマシューティカルズ、インコーポレイテッド ピリミジニル−チオフェンキナーゼモジュレータ
EP1785420A1 (en) 2005-11-14 2007-05-16 4Sc Ag Thiazole analogues and uses thereof
US20070149523A1 (en) 2005-11-14 2007-06-28 Jan Ehlert Thiazole Analogues and Uses Thereof
WO2007057397A1 (en) 2005-11-15 2007-05-24 Boehringer Ingelheim International Gmbh Treatment of cancer
WO2007057399A2 (en) 2005-11-15 2007-05-24 Boehringer Ingelheim International Gmbh Treatment of cancer with indole derivatives
GB0524436D0 (en) 2005-11-30 2006-01-11 Novartis Ag Organic compounds
RU2008127263A (ru) 2005-12-08 2010-01-20 Новартис АГ (CH) ПИРАЗОЛ [1,5-a] ПИРИДИН-3-КАРБОНОВЫЕ КИСЛОТЫ В КАЧЕСТВЕ ИНГИБИТОРОВ EphB-И VEGFR2-КИНАЗЫ
EP1968579A1 (en) 2005-12-30 2008-09-17 Astex Therapeutics Limited Pharmaceutical compounds
US20090227598A1 (en) 2006-01-24 2009-09-10 Buser-Doepner Carolyn A Ret Tyrosine Kinase Inhibition
DK1973910T3 (da) 2006-01-27 2013-08-12 Shanghai Hengrui Pharm Co Ltd Pyrrolo[3,2-c]pyridin-4-on-2-indolinon-proteinkinaseinhibitorer
WO2007109045A1 (en) 2006-03-16 2007-09-27 Novartis Ag Heterocyclic organic compounds for the treatment of in particular melanoma
BRPI0708823B1 (pt) 2006-03-17 2022-01-18 Ambit Biosciences Corporation Composto, e, composição
KR20090008286A (ko) 2006-03-27 2009-01-21 네르비아노 메디칼 사이언시스 에스.알.엘. 키나제 억제제로서의 피리딜- 및 피리미디닐-치환된 피롤-,티오펜- 및 푸란- 유도체
KR20080109095A (ko) 2006-05-15 2008-12-16 아이알엠 엘엘씨 Fgf 수용체 키나제 억제제를 위한 조성물 및 방법
ES2556173T3 (es) 2006-05-18 2016-01-13 Eisai R&D Management Co., Ltd. Agente antitumoral para un cáncer de tiroides
US8063225B2 (en) 2006-08-14 2011-11-22 Chembridge Corporation Tricyclic compound derivatives useful in the treatment of neoplastic diseases, inflammatory disorders and immunomodulatory disorders
EP2067039A2 (en) 2006-09-12 2009-06-10 Novartis Forschungsstiftung, Zweigniederlassung Friedrich Miescher Institute for Biomedical Research Non-neuroendocrine cancer therapy
EP2079727B1 (en) 2006-09-15 2016-02-17 Xcovery, INC. Kinase inhibitor compounds
US20120225057A1 (en) 2006-10-11 2012-09-06 Deciphera Pharmaceuticals, Llc Methods and compositions for the treatment of myeloproliferative diseases and other proliferative diseases
EP1918291A1 (en) 2006-10-30 2008-05-07 Novartis AG 3-Aminocarbonyl-substituted fused pyrazolo-derivatives as protein kinase modulators
SI2848610T1 (sl) 2006-11-15 2018-02-28 Ym Biosciences Australia Pty Ltd Inhibitorji aktivnosti kinaze
CL2007003627A1 (es) * 2006-12-15 2008-07-25 Bayer Schering Pharma Ag Compuestos derivados de 3-h-pirazolopiridinas; metodo de preparacion; composicion farmaceutica; y uso para el tratamiento de enfermedades de crecimiento vascular desregulado tal como leucemia mielogena aguda, retinopatia, artritis reumatoide, psorias
CN101641351A (zh) 2006-12-21 2010-02-03 普莱希科公司 用于激酶调节的化合物和方法及其适应症
WO2008079909A1 (en) 2006-12-21 2008-07-03 Plexxikon, Inc. Pyrrolo [2,3-b] pyridines as kinase modulators
PE20121126A1 (es) 2006-12-21 2012-08-24 Plexxikon Inc Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa
US20080199426A1 (en) 2007-01-11 2008-08-21 Sukhatme Vikas P Methods and compositions for the treatment and diagnosis of vascular inflammatory disorders or endothelial cell disorders
EP2114403A2 (en) 2007-01-19 2009-11-11 Bayer Healthcare, LLC Treatment of cancers having resistance to chemotherapeutic agents
US20080234267A1 (en) 2007-03-20 2008-09-25 Karen Elizabeth Lackey Compounds and Methods of Treatment
US20110189167A1 (en) * 2007-04-20 2011-08-04 Flynn Daniel L Methods and Compositions for the Treatment of Myeloproliferative Diseases and other Proliferative Diseases
AU2008247442B2 (en) 2007-05-04 2013-01-10 Irm Llc Compounds and compositions as c-kit and PDGFR kinase inhibitors
WO2008138184A1 (fr) 2007-05-14 2008-11-20 Shanghai Hengrui Pharmaceutical Co.Ltd. Dérivés de pyrrolo-azacycles, leur procédé de fabrication et leur utilisation en tant qu'inhibiteurs de protéine kinases
WO2009003136A1 (en) 2007-06-26 2008-12-31 Rigel Pharmaceuticals, Inc. Substituted pyrimidine-2, 4 -diamines for treating cell proliferative disorders
BRPI0814818A2 (pt) 2007-07-09 2019-09-10 Astrazeneca Ab composto, uso de um composto, métodos para produzir um efeito anti-proliferativo e um efeito inibitório de mtor quinase em uma animal de sangue quente, método para tratar doenças, e, composição farmacêutica
US20100209488A1 (en) 2007-07-16 2010-08-19 The Regents Of The University Of California Protein kinase modulating compounds and methods for making and using them
AU2008276063B2 (en) 2007-07-17 2013-11-28 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
AR067585A1 (es) 2007-07-19 2009-10-14 Schering Corp Compuestos heterociclicos de amidas como inhibidores de la proteincinasa
CN101754956B (zh) 2007-07-20 2014-04-23 内尔维阿诺医学科学有限公司 作为具有激酶抑制剂活性的取代的吲唑衍生物
WO2009017838A2 (en) 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
EP2185698B1 (en) 2007-08-07 2015-04-22 Purdue Research Foundation Kinase inhibitors and uses thereof
EP2025678A1 (en) 2007-08-17 2009-02-18 Oncalis AG Pyrazolo[3,4-d]pyrimidine compounds and their use as modulators of protein kinase
WO2009042646A1 (en) 2007-09-24 2009-04-02 Curis, Inc. Anti-proliferative agents
EA201000603A1 (ru) 2007-10-23 2010-12-30 Новартис Аг ПРИМЕНЕНИЕ АНТИТЕЛ К TrkB ДЛЯ ЛЕЧЕНИЯ РЕСПИРАТОРНЫХ НАРУШЕНИЙ
JP5400791B2 (ja) 2007-12-04 2014-01-29 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ 置換ジヒドロプテリジン−6−オン誘導体、その製造方法及びキナーゼ阻害剤としてのその使用
CN101459004B (zh) 2007-12-14 2011-02-09 深圳富泰宏精密工业有限公司 电子装置的按键面板结构及制造该按键面板结构的方法
EA028621B1 (ru) 2008-01-17 2017-12-29 Новартис Аг АНТИТЕЛО ИЛИ ЕГО АНТИГЕНСВЯЗЫВАЮЩИЙ ФРАГМЕНТ, КОТОРЫЙ СПЕЦИФИЧНО СВЯЗЫВАЕТ РЕЦЕПТОРНУЮ ТИРОЗИНКИНАЗУ (TrkB), ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ ЭТО АНТИТЕЛО ИЛИ ЕГО АНТИГЕНСВЯЗЫВАЮЩИЙ ФРАГМЕНТ, И КОМБИНАЦИЯ, ВКЛЮЧАЮЩАЯ УКАЗАННУЮ КОМПОЗИЦИЮ
JP2009203226A (ja) 2008-01-31 2009-09-10 Eisai R & D Management Co Ltd ピリジン誘導体およびピリミジン誘導体を含有するレセプターチロシンキナーゼ阻害剤
TW200942537A (en) 2008-02-01 2009-10-16 Irm Llc Compounds and compositions as kinase inhibitors
US20090209496A1 (en) 2008-02-15 2009-08-20 David Chaplin Methods and compositions for enhancing the efficacy of rtk inhibitors
AU2009226153B2 (en) 2008-03-19 2014-02-20 Chembridge Corporation Novel tyrosine kinase inhibitors
ES2588193T3 (es) 2008-03-28 2016-10-31 Nerviano Medical Sciences S.R.L. Derivados de 3,4-dihidro-2H-pirazino[1,2-a]indol-1-ona activos como inhibidores de cinasa, proceso para su preparación y composiciones farmacéuticas que los comprenden
PE20091846A1 (es) 2008-05-19 2009-12-16 Plexxikon Inc DERIVADOS DE PIRROLO[2,3-d]-PIRIMIDINA COMO MODULADORES DE CINASAS
WO2009143018A2 (en) 2008-05-19 2009-11-26 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
CN102036963B (zh) 2008-05-23 2013-08-21 诺瓦提斯公司 作为蛋白酪氨酸激酶抑制剂的喹啉类和喹喔啉类衍生物
AU2009257635A1 (en) 2008-06-10 2009-12-17 Plexxikon, Inc. 5H-Pyrrolo [2,3-b] pyrazine derivatives for kinase modulation, and indications therefor
EP2303890A4 (en) 2008-06-19 2012-04-11 Progenics Pharm Inc INHIBITORS OF PHOSPHATIDYLINOSITE-3-KINASE
US8629135B2 (en) 2008-07-14 2014-01-14 Queen's University At Kingston Pharmaceutical compositions comprising RET inhibitors and methods for the treatment of cancer
JO3041B1 (ar) 2008-07-25 2016-09-05 Galapagos Nv مركبات جديدة مفيدة لمعالجة الأمراض التنكسية والالتهابية
EP2323664B1 (en) 2008-07-29 2015-01-07 Nerviano Medical Sciences S.r.l. Use of a cdk inhibitor for the treatment of glioma
RU2476036C2 (ru) 2008-09-01 2013-02-20 Шарп Кабусики Кайся Органическая электролюминесцентная панель, органический электролюминесцентный дисплей, органическое электролюминесцентное осветительное устройство и способы их производства
WO2010028254A2 (en) 2008-09-05 2010-03-11 Auspek Pharmaceuticals, Inc. Substituted quinazoline inhibitors of growth factor receptor tyrosine kinases
EP2161271A1 (en) 2008-09-08 2010-03-10 Università Degli Studi Di Milano - Bicocca Alpha-carboline inhibitors of NMP-ALK, RET, and Bcr-Abl
ES2536730T3 (es) 2008-09-19 2015-05-28 Nerviano Medical Sciences S.R.L. Derivados de 3,4-dihidro-2H-pirrolo[1,2-a]pirazin-1-ona
EP2350075B1 (en) 2008-09-22 2014-03-05 Array Biopharma, Inc. Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors
KR101718386B1 (ko) 2008-09-26 2017-03-21 내셔날 헬스 리서치 인스티튜트 단백질 키나아제 억제제로서의 융합 다환 화합물
KR101652189B1 (ko) 2008-10-22 2016-08-29 어레이 바이오파마 인크. TRK 키나아제 억제제로서 치환된 피라졸로[1,5­a] 피리미딘 화합물
JP5686736B2 (ja) 2008-11-06 2015-03-18 アムビト ビオスシエンセス コルポラチオン プロテインキナーゼモジュレーターとしてのイミダゾロチアゾール化合物
JP2012509859A (ja) 2008-11-24 2012-04-26 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ 中皮腫の治療のためのcdk阻害物質
KR101061599B1 (ko) 2008-12-05 2011-09-02 한국과학기술연구원 비정상 세포 성장 질환의 치료를 위한 단백질 키나아제 저해제인 신규 인다졸 유도체, 이의 약학적으로 허용가능한염 및 이를 유효성분으로 함유하는 약학적 조성물
JO3265B1 (ar) 2008-12-09 2018-09-16 Novartis Ag مثبطات بيريديلوكسى اندولات vegf-r2 واستخدامها لعلاج المرض
MX337352B (es) 2009-03-18 2016-02-29 Resverlogix Corp Nuevos agentes anti-inflamatorios.
WO2010111527A1 (en) 2009-03-26 2010-09-30 Plexxikon, Inc. Pyrazolo [ 3, 4 -b] pyridines as kinase inhibitors and their medical use
TWI410418B (zh) 2009-04-29 2013-10-01 Ind Tech Res Inst 氮雜薁化合物、藥學組合物與抑制一細胞中蛋白質激酶之活性的方法
NO3009428T3 (sl) 2009-05-08 2018-07-21
CN102480966B (zh) 2009-06-12 2015-09-16 达娜-法勃肿瘤研究所公司 融合的杂环化合物及其用途
JP5789602B2 (ja) 2009-06-15 2015-10-07 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ 置換ピリミジニルピロロピリジノン誘導体、これらの製造のための方法およびキナーゼ阻害剤としてのこれらの使用
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
US9085560B2 (en) 2009-08-17 2015-07-21 Intellikine, Inc. Heterocyclic compounds and uses thereof
KR101256018B1 (ko) 2009-08-20 2013-04-18 한국과학기술연구원 단백질 키나아제 저해활성을 갖는 1,3,6-치환된 인돌 화합물
FR2951172B1 (fr) 2009-10-13 2014-09-26 Pf Medicament Derives pyrazolopyridines en tant qu'agent anticancereux
KR101147550B1 (ko) 2009-10-22 2012-05-17 한국과학기술연구원 단백질 키나아제 저해활성을 가지는 2,7-치환된 티에노[3,2-d]피리미딘 화합물
KR101116756B1 (ko) 2009-10-27 2012-03-13 한국과학기술연구원 단백질 키나아제 저해활성을 갖는 신규의 1,6-치환된 인돌 화합물
JP5993742B2 (ja) 2009-10-29 2016-09-14 ジェノスコ キナーゼ阻害剤
WO2011060295A1 (en) 2009-11-13 2011-05-19 Genosco Kinase inhibitors
KR101094446B1 (ko) 2009-11-19 2011-12-15 한국과학기술연구원 단백질 키나아제 저해활성을 가지는 2,4,7-치환된 티에노[3,2-d]피리미딘 화합물
EP2519517B1 (en) 2009-12-29 2015-03-25 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
SG182361A1 (en) 2010-01-29 2012-08-30 Hanmi Science Co Ltd THIENO[3,2-d]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY ON PROTEIN KINASES
ES2524576T3 (es) 2010-01-29 2014-12-10 Nerviano Medical Sciences S.R.L. Derivados de 6,7-dihidroimidazo[1,5-a]pirazin-8(5H)-ona como moduladores de proteína cinasa
KR101483215B1 (ko) 2010-01-29 2015-01-16 한미약품 주식회사 단백질 키나아제 저해활성을 갖는 비시클릭 헤테로아릴 유도체
EP2536414B1 (en) 2010-02-18 2016-07-13 INSERM (Institut National de la Santé et de la Recherche Médicale) Method for preventing cancer metastasis
TWI619713B (zh) 2010-04-21 2018-04-01 普雷辛肯公司 用於激酶調節的化合物和方法及其適應症
US8933084B2 (en) 2010-05-20 2015-01-13 Array Biopharma Inc. Macrocyclic compounds as Trk kinase inhibitors
WO2012034095A1 (en) 2010-09-09 2012-03-15 Irm Llc Compounds and compositions as trk inhibitors
UY33597A (es) 2010-09-09 2012-04-30 Irm Llc Compuestos y composiciones como inhibidores de la trk
WO2012037155A2 (en) 2010-09-13 2012-03-22 Gtx, Inc. Tyrosine kinase inhibitors
WO2012047017A2 (ko) 2010-10-05 2012-04-12 크리스탈지노믹스(주) 2,3-디히드로-이소인돌-1-온 유도체 및 이를 포함하는 조성물
JP2014005206A (ja) 2010-10-22 2014-01-16 Astellas Pharma Inc アリールアミノヘテロ環カルボキサミド化合物
JP5925808B2 (ja) 2011-01-26 2016-05-25 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ 三環式誘導体、これらの調製方法およびこれらのキナーゼ阻害剤としての使用
EP2668190B1 (en) 2011-01-26 2016-08-17 Nerviano Medical Sciences S.r.l. Tricyclic pyrrolo derivatives, process for their preparation and their use as kinase inhibitors
CN102093421B (zh) 2011-01-28 2014-07-02 北京康辰药业有限公司 一种含磷取代基的喹啉类化合物及其制备方法、以及含有该化合物的药物组合物及其应用
EA028821B9 (ru) 2011-02-07 2018-10-31 Плексксикон, Инк. Соединения и способы для модуляции киназ, а также показания к их применению
US9199979B2 (en) 2011-02-24 2015-12-01 Nerviano Medical Sciences S.R.L. Thiazolylphenyl-benzenesulfonamido derivatives as kinase inhibitors
JP5959541B2 (ja) 2011-02-25 2016-08-02 ノバルティス アーゲー Trk阻害剤としてのピラゾロ[1,5−a]ピリジン
WO2012135631A1 (en) 2011-03-30 2012-10-04 Arrien Pharmaeuticals Llc Substituted 5-(pyrazin-2-yl)-1h-pyrazolo [3, 4-b] pyridine and pyrazolo [3, 4-b] pyridine derivatives as protein kinase inhibitors
WO2012135800A1 (en) 2011-04-01 2012-10-04 University Of Utah Research Foundation Substituted n-phenylpyrimidin-2-amine analogs as inhibitors of the axl kinase
WO2012139930A1 (en) 2011-04-11 2012-10-18 Nerviano Medical Sciences S.R.L. Pyrazolyl-pyrimidine derivatives as kinase inhibitors
BR112013026137B1 (pt) 2011-04-19 2020-12-01 Nerviano Medical Sciences S.R.L pirimidinil-pirróis substituídos ativos como inibidores da quinase
AR086042A1 (es) 2011-04-28 2013-11-13 Galapagos Nv Compuesto util para el tratamiento de enfermedades degenerativas e inflamatorias y composicion farmaceutica
EA023579B1 (ru) 2011-05-12 2016-06-30 НЕРВИАНО МЕДИКАЛ САЙЕНСИЗ С.р.л. Замещенные производные индазола, активные в качестве ингибиторов киназы
NZ618795A (en) 2011-05-13 2015-07-31 Array Biopharma Inc Pyrrolidinyl urea, pyrrolidinyl thiourea and pyrrolidinyl guanidine compounds as trka kinase inhibitors
RU2477723C2 (ru) 2011-06-16 2013-03-20 Общество С Ограниченной Ответственностью "Фьюжн Фарма" Ингибиторы протеинкиназ (варианты), их применение для лечения онкологических заболеваний и фармацевтическая композиция на их основе
CN102827073A (zh) * 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
WO2013016720A2 (en) 2011-07-28 2013-01-31 Gerinda Therapeutics, Inc. Novel substituted biarylheterocycle derivatives as protein kinase inhibitors for the treatment of cancer and other diseases
WO2013014039A1 (en) 2011-07-28 2013-01-31 Nerviano Medical Sciences S.R.L. Alkynyl substituted pyrimidinyl-pyrroles active as kinases inhibitors
IN2014DN01605A (sl) 2011-08-04 2015-05-15 Nat Cancer Ct
BR112014004213A2 (pt) 2011-08-23 2017-06-20 Found Medicine Inc novas moléculas de fusão kif5b-ret e usos das mesmas
AU2012341028C1 (en) 2011-09-02 2017-10-19 Mount Sinai School Of Medicine Substituted pyrazolo[3,4-D]pyrimidines and uses thereof
WO2013036232A2 (en) 2011-09-08 2013-03-14 Deciphera Pharmaceuticals, Llc Methods and compositions for the treatment of myeloproliferative diseases and other proliferative diseases
CN102408411B (zh) 2011-09-19 2014-10-22 北京康辰药业股份有限公司 一种含喹啉基的羟肟酸类化合物及其制备方法、以及含有该化合物的药物组合物及其应用
WO2013042137A1 (en) 2011-09-19 2013-03-28 Aurigene Discovery Technologies Limited Bicyclic heterocycles as irak4 inhibitors
WO2013050448A1 (en) 2011-10-07 2013-04-11 Nerviano Medical Sciences S.R.L. 4-ALKYL SUBSTITUTED 3,4-DIHYDROPYRROLO[1,2-a]PYRAZIN-1(2H)-ONE DERIVATIVES AS KINASES INHIBITORS
WO2013050446A1 (en) 2011-10-07 2013-04-11 Nerviano Medical Sciences S.R.L. SUBSTITUTED 3,4-DIHYDROPYRROLO[1,2-a]PYRAZIN-1(2H)-ONE DERIVATIVES AS KINASES INHIBITORS
EP2779833A4 (en) 2011-11-14 2015-03-18 Tesaro Inc MODULATION OF SPECIFIC TYROSINE KINASES
WO2013081188A1 (ja) 2011-11-30 2013-06-06 独立行政法人国立がん研究センター 誘導悪性幹細胞
WO2013100632A1 (en) 2011-12-30 2013-07-04 Hanmi Pharm Co., Ltd. THIENO[3,2-d]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY FOR PROTEIN KINASES
US8377946B1 (en) 2011-12-30 2013-02-19 Pharmacyclics, Inc. Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors
JP2015109806A (ja) 2012-03-22 2015-06-18 アステラス製薬株式会社 新規ret融合体の検出法
TW201350479A (zh) 2012-04-26 2013-12-16 Ono Pharmaceutical Co Trk阻害化合物
CA2871540A1 (en) 2012-05-10 2013-11-14 Synta Pharmaceuticals Corp. Treating cancer with hsp90 inhibitory compounds
CN106167485A (zh) 2012-05-23 2016-11-30 内尔维阿诺医学科学有限公司 苯甲酰胺类,含有苯甲酰胺类的组合物以及苯甲酰胺类的制备方法
TWI585088B (zh) 2012-06-04 2017-06-01 第一三共股份有限公司 作爲激酶抑制劑之咪唑并[1,2-b]嗒衍生物
BR112015000653A2 (pt) 2012-07-11 2019-11-05 Blueprint Medicines Corp compostos inibidores do receptor de fator de crescimento de fibroblasto, sua composição farmacêutica e seus usos
CN109024018B (zh) 2012-07-13 2021-10-08 奥的斯电梯公司 包括纤维的皮带
WO2014017491A1 (ja) 2012-07-26 2014-01-30 独立行政法人国立がん研究センター Cep55遺伝子とret遺伝子との融合遺伝子
WO2014019908A2 (en) 2012-08-02 2014-02-06 Nerviano Medical Sciences S.R.L. Substituted pyrroles active as kinases inhibitors
CN104703600A (zh) 2012-09-07 2015-06-10 埃克塞里艾克西斯公司 用于治疗肺腺癌的met、vegfr和ret的抑制剂
US10668075B2 (en) 2012-09-25 2020-06-02 Chugai Seiyaku Kabushiki Kaisha RET inhibitor
CN104870446B (zh) 2012-11-07 2019-08-13 内尔维阿诺医学科学有限公司 取代的嘧啶基和吡啶基吡咯并吡啶酮类、其制备方法及其作为激酶抑制剂的用途
SG11201503560TA (en) 2012-11-12 2015-06-29 Ignyta Inc Bendamustine derivatives and methods of using same
WO2014078328A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. N-bicyclic aryl,n'-pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
US9969694B2 (en) 2012-11-13 2018-05-15 Array Biopharma Inc. N-(arylalkyl)-N′-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
US9822118B2 (en) 2012-11-13 2017-11-21 Array Biopharma Inc. Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
WO2014078325A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. N-(monocyclic aryl),n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2014078378A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2014078372A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
UA117573C2 (uk) 2012-11-13 2018-08-27 Ерей Біофарма Інк. Біциклічні сполуки сечовини, тіосечовини, гуанідину й ціаногуанідину, придатні для лікування болю
US9809578B2 (en) 2012-11-13 2017-11-07 Array Biopharma Inc. Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trkA kinase inhibitors
ME02990B (me) 2012-11-13 2018-10-20 Array Biopharma Inc Jedinjenja n-pirolidinil, n'-pirazolil- uree, tiouree, guanidina i cijanoguanidina kао inhibitori trka kinaze
US9981959B2 (en) 2012-11-13 2018-05-29 Array Biopharma Inc. Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
AU2013350721A1 (en) 2012-11-29 2015-01-29 Yeda Research And Development Co. Ltd. Methods of preventing tumor metastasis, treating and prognosing cancer and identifying agents which are putative metastasis inhibitors
WO2014086284A1 (zh) 2012-12-04 2014-06-12 上海医药集团股份有限公司 一类氘代3-氰基喹啉类化合物、其药用组合物、制备方法及其用途
FR3000494B1 (fr) 2012-12-28 2015-08-21 Oribase Pharma Nouveaux derives d'azaindoles en tant qu'inhibiteurs de proteines kinases
PL2940014T3 (pl) 2012-12-28 2019-03-29 Crystalgenomics, Inc. Pochodne 2,3-dihydro-isoindole-1-on jako supresant kinazy btk i mieszanka farmaceutyczna
FR3000492B1 (fr) 2012-12-28 2015-09-11 Oribase Pharma Nouveaux derives azaindole en tant qu'inhibiteurs multikinases
FR3000493A1 (fr) 2012-12-28 2014-07-04 Oribase Pharma Nouveaux inhibiteurs de proteines kinases
KR20150118148A (ko) 2013-02-19 2015-10-21 오노 야꾸힝 고교 가부시키가이샤 Trk 저해 화합물
WO2014160524A1 (en) 2013-03-14 2014-10-02 The Trustees Of The University Of Pennsylvania Cardio- metabolic and cascular effects of glp-1 metabolites
BR112015023618A2 (pt) 2013-03-15 2017-07-18 Glaxosmithkline Ip Dev Ltd derivados de piridina como inibidores de quinase reorganizada durante a transfecção (ret)
WO2014160521A1 (en) 2013-03-15 2014-10-02 Blueprint Medicines Corporation Piperazine derivatives and their use as kit modulators
MA38394B1 (fr) 2013-03-15 2018-04-30 Glaxosmithkline Ip Dev Ltd Dérivés pyridine utilisés comme inhibiteurs de la kinase réarrangée au cours de la transfection (ret)
EP2997030B1 (en) 2013-05-14 2017-08-09 Nerviano Medical Sciences S.R.L. Pyrrolo[2,3-d]pyrimidine derivatives, process for their preparation and their use as kinase inhibitors
EP3004060B1 (en) 2013-05-30 2019-11-27 Plexxikon Inc. Compounds for kinase modulation, and indications therefor
US10407509B2 (en) 2013-07-30 2019-09-10 Blueprint Medicines Corporation NTRK2 fusions
WO2015017528A1 (en) 2013-07-30 2015-02-05 Blueprint Medicines Corporation Pik3c2g fusions
EP3037547A1 (en) 2013-08-20 2016-06-29 National Cancer Center New fusion gene detected in lung cancer
CA2922230A1 (en) 2013-08-30 2015-03-05 Ambit Biosciences Corporation Biaryl acetamide compounds and methods of use thereof
WO2015046653A1 (ko) 2013-09-30 2015-04-02 한국화학연구원 신규한 트리아졸로 피라진 유도체 및 그의 용도
SG11201602937UA (en) 2013-10-17 2016-05-30 Blueprint Medicines Corp Compositions useful for treating disorders related to kit
US9334263B2 (en) 2013-10-17 2016-05-10 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
EP3060560A1 (en) 2013-10-25 2016-08-31 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
GB201321146D0 (en) 2013-11-29 2014-01-15 Cancer Rec Tech Ltd Quinazoline compounds
EP3076966A2 (en) 2013-12-02 2016-10-12 BerGenBio AS Use of kinase inhibitors
US9695165B2 (en) 2014-01-15 2017-07-04 Blueprint Medicines Corporation Inhibitors of the fibroblast growth factor receptor
RS59059B1 (sr) 2014-01-24 2019-08-30 Turning Point Therapeutics Inc Diaril makrociklična jedinjenja kao modulatori protein kinaza
JP6756617B2 (ja) 2014-02-14 2020-09-16 エグゼリクシス, インコーポレイテッド N−{4−[(6,7−ジメトキシキノリン−4−イル)オキシ]フェニル}−n’−(4−フルオロフェニル)シクロプロパン−1,1−ジカルボキサミドの結晶性固体形態、製造プロセス、及び使用方法
US10231965B2 (en) 2014-02-20 2019-03-19 Ignyta, Inc. Molecules for administration to ROS1 mutant cancer cells
US20170044622A1 (en) 2014-04-18 2017-02-16 Blueprint Medicines Corporation Pik3ca fusions
US20170044621A1 (en) 2014-04-18 2017-02-16 Blueprint Medicines Corporation Met fusions
RS59286B1 (sr) * 2014-05-15 2019-10-31 Array Biopharma Inc 1-((3s,4r)-4-(3-fluorofenil)-1-(2-metoksietil)pirolidin-3-il)-3-(4-metil-3-(2-metilpirimidin-5-il)-1-fenil-1h-pirazol-5-il)urea kao inhibitor trka kinaze
EP3155118A1 (en) 2014-06-10 2017-04-19 Blueprint Medicines Corporation Pkn1 fusions
EP3155131B1 (en) 2014-06-10 2020-02-12 Blueprint Medicines Corporation Raf1 fusions
WO2016011144A1 (en) 2014-07-17 2016-01-21 Blueprint Medicines Corporation Tert fusions
EP3169809B1 (en) 2014-07-17 2020-04-29 Blueprint Medicines Corporation Prkc fusions
ES2747249T3 (es) 2014-07-17 2020-03-10 Sunshine Lake Pharma Co Ltd Derivados de 1-(5-(terc-butil)isoxazol-3-il)-3-(4-((fenil)etinil)fenil)urea y compuestos relacionados como inhibidores de FLT3 para el tratamiento de cáncer
US10370725B2 (en) 2014-07-17 2019-08-06 Blueprint Medicines Corporation FGR fusions
US9688680B2 (en) 2014-08-04 2017-06-27 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
MX2017002199A (es) 2014-08-18 2017-08-18 Ono Pharmaceutical Co Sal de adicion de acido de compuesto inhibidor de cinasa del receptor de trompomosina (trk).
AU2015313894A1 (en) 2014-09-08 2017-03-23 Glaxosmithkline Intellectual Property Development Limited Crystalline forms of 2-(4-(4-ethoxy-6-oxo-1,6-dihydropyridin-3-yl)-2-fluorophenyl)-n-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)acetamide
PE20170705A1 (es) 2014-09-10 2017-05-21 Glaxosmithkline Ip Dev Ltd Nuevos compuestos como inhibidores de ret (reorganizado durante la transfeccion)
US9879021B2 (en) 2014-09-10 2018-01-30 Glaxosmithkline Intellectual Property Development Limited Compounds as rearranged during transfection (RET) inhibitors
TWI538914B (zh) 2014-10-03 2016-06-21 國立交通大學 蛋白質激酶之選擇性抑制劑、其醫藥組成物及其用途
US10221181B2 (en) 2014-11-14 2019-03-05 Nerviano Medical Sciences S.R.L. 6-amino-7-bicyclo-7-deaza-purine derivatives as protein kinase inhibitors
EP3699181B1 (en) 2014-11-16 2023-03-01 Array Biopharma, Inc. Crystalline form of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate
US20170356052A1 (en) 2014-11-18 2017-12-14 Blueprint Medicines Corporation Prkacb fusions
WO2016096709A1 (en) 2014-12-16 2016-06-23 Eudendron S.R.L. Heterocyclic derivatives modulating activity of certain protein kinases
WO2016127074A1 (en) 2015-02-06 2016-08-11 Blueprint Medicines Corporation 2-(pyridin-3-yl)-pyrimidine derivatives as ret inhibitors
KR101675984B1 (ko) 2015-02-23 2016-11-14 한양대학교 에리카산학협력단 티에노디아제핀 유도체 또는 이의 약학적으로 허용가능한 염, 및 이를 유효성분으로 포함하는 약학적 조성물
US20180045727A1 (en) * 2015-03-03 2018-02-15 Caris Mpi, Inc. Molecular profiling for cancer
US10364247B2 (en) 2015-04-21 2019-07-30 Ruijin Hospital Affiliated To Shanghai Jiao Tong University School Of Medicine Preparation and use of novel protein kinase inhibitors
GB201512365D0 (en) 2015-07-15 2015-08-19 King S College London Novel therapy
MX2018000577A (es) 2015-07-16 2018-09-05 Array Biopharma Inc Compuestos de pirazolo[1,5-a]piridina sustituidos como inhibidores de la ret quinasa.
EP3120851A1 (en) 2015-07-21 2017-01-25 Pangaea Biotech S.L. 4-amino-6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)-pyrido[2,3-d]pyrimidin-7(8h)-one for treatment of solid cancers
KR101766194B1 (ko) 2015-08-07 2017-08-10 한국과학기술연구원 RET 키나아제 저해제인 신규 3-(이속사졸-3-일)-피라졸로[3,4-d]피리미딘-4-아민 화합물
WO2017027883A1 (en) 2015-08-13 2017-02-16 San Diego State University Research Foundation Atropisomerism for increased kinase inhibitor selectivity
MA41559A (fr) 2015-09-08 2017-12-26 Taiho Pharmaceutical Co Ltd Composé de pyrimidine condensé ou un sel de celui-ci
WO2017049462A1 (zh) 2015-09-22 2017-03-30 合肥中科普瑞昇生物医药科技有限公司 一类新型的flt3激酶抑制剂及其用途
CN105255927B (zh) 2015-09-30 2018-07-27 温州医科大学附属第一医院 一种kiaa1217-ret融合基因
HUE064659T2 (hu) 2015-11-02 2024-04-28 Blueprint Medicines Corp RET inhibitorai
WO2017097697A1 (en) 2015-12-08 2017-06-15 Boehringer Ingelheim International Gmbh Method using a ret fusion gene as a biomarker to select non-small cell lung cancer (nsclc) and thyroid cancer patients for a cancer treatment
JP6871869B2 (ja) 2016-01-15 2021-05-19 公益財団法人がん研究会 新規融合体及びその検出法
TWI620748B (zh) 2016-02-05 2018-04-11 National Health Research Institutes 氨基噻唑化合物及其用途
MX2018010176A (es) 2016-02-23 2019-01-21 Taiho Pharmaceutical Co Ltd Compuesto novedoso de pirimidina condensada o sal del mismo.
WO2017145050A1 (en) 2016-02-23 2017-08-31 Glaxosmithkline Intellectual Property Development Limited Pyridylpyridone derivative useful as a ret kinase inhibitor in the treatment of ibs and cancer
WO2017161269A1 (en) 2016-03-17 2017-09-21 Blueprint Medicines Corporation Inhibitors of ret receptor tyrosine kinases
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
US10844067B2 (en) 2016-04-15 2020-11-24 Cancer Research Technology Limited Heterocyclic compounds as RET kinase inhibitors
RU2742115C2 (ru) 2016-04-15 2021-02-02 Кэнсер Рисерч Текнолоджи Лимитед Гетероциклические соединения в качестве ингибиторов киназы RET
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret

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