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MX2020012261A - Inhibidores de kras g12c que comprenden un anillo de piperazina y uso de estos en el tratamiento del cancer. - Google Patents

Inhibidores de kras g12c que comprenden un anillo de piperazina y uso de estos en el tratamiento del cancer.

Info

Publication number
MX2020012261A
MX2020012261A MX2020012261A MX2020012261A MX2020012261A MX 2020012261 A MX2020012261 A MX 2020012261A MX 2020012261 A MX2020012261 A MX 2020012261A MX 2020012261 A MX2020012261 A MX 2020012261A MX 2020012261 A MX2020012261 A MX 2020012261A
Authority
MX
Mexico
Prior art keywords
kras
cancer
treatment
inhibitors
piperazine ring
Prior art date
Application number
MX2020012261A
Other languages
English (en)
Inventor
Victor J Cee
Brian Alan Lanman
Anthony B Reed
Thomas T Nguyen
Vu Van Ma
Albert Amegadzie
Ning Chen
Alexander J Pickrell
Jian Chen
Jonathan D Low
Patricia Lopez
Nuria A Tamayo
Qiufen Xue
Youngsook Shin
John Gordon Allen
Aaron C Siegmund
Longbin Liu
Ana Elena Minatti
Nobuko Nishimura
Kevin C Yang
Shon Booker
Jennifer Rebecca Allen
Clifford Goodman
Ryan Paul Wurz
Mary Walton
Hui-Ling Wang
Margaret Chu-Moyer
Original Assignee
Amgen 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 Amgen Inc filed Critical Amgen Inc
Publication of MX2020012261A publication Critical patent/MX2020012261A/es

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    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K39/395Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/39558Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against tumor tissues, cells, antigens
    • 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
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D243/00Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/141,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • 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
    • 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
    • C07D471/12Heterocyclic 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 three hetero rings
    • C07D471/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

En la presente, se proporcionan inhibidores de KRAS G12C, tales como (VER FORMULA) composiciones de estos y métodos de utilización de estos. Estos inhibidores son útiles para tratar múltiples trastornos, incluidos cáncer pancreático, colorrectal y de pulmón.
MX2020012261A 2018-06-12 2019-06-11 Inhibidores de kras g12c que comprenden un anillo de piperazina y uso de estos en el tratamiento del cancer. MX2020012261A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862684117P 2018-06-12 2018-06-12
PCT/US2019/036626 WO2020050890A2 (en) 2018-06-12 2019-06-11 Kras g12c inhibitors and methods of using the same

Publications (1)

Publication Number Publication Date
MX2020012261A true MX2020012261A (es) 2021-03-31

Family

ID=68765635

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2020012261A MX2020012261A (es) 2018-06-12 2019-06-11 Inhibidores de kras g12c que comprenden un anillo de piperazina y uso de estos en el tratamiento del cancer.

Country Status (8)

Country Link
US (2) US11285156B2 (es)
EP (1) EP3807276A2 (es)
JP (1) JP7369719B2 (es)
AU (1) AU2019336588B2 (es)
CA (1) CA3100390A1 (es)
MA (1) MA51848A (es)
MX (1) MX2020012261A (es)
WO (1) WO2020050890A2 (es)

Families Citing this family (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS62456B1 (sr) 2016-12-22 2021-11-30 Amgen Inc Derivati benzizotiazola, izotiazolo[3,4-b]piridina, hinazolina, ftalazina, pirido[2,3-d]piridazina i pirido[2,3-d]pirimidina kao kras g12c inhibitori za tretman raka pluća, pankreasa ili debelog creva
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
EP4403175A3 (en) 2017-09-08 2024-10-02 Amgen Inc. Inhibitors of kras g12c and methods of using the same
MA52501A (fr) 2018-05-04 2021-03-10 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
MA52496A (fr) 2018-05-04 2021-03-10 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
CA3099045A1 (en) 2018-05-10 2019-11-14 Amgen Inc. Kras g12c inhibitors for the treatment of cancer
WO2019232419A1 (en) 2018-06-01 2019-12-05 Amgen Inc. Kras g12c inhibitors and methods of using the same
MX2020012261A (es) 2018-06-12 2021-03-31 Amgen Inc Inhibidores de kras g12c que comprenden un anillo de piperazina y uso de estos en el tratamiento del cancer.
JP7451419B2 (ja) 2018-10-26 2024-03-18 大鵬薬品工業株式会社 新規なインダゾール化合物又はその塩
JP7516029B2 (ja) 2018-11-16 2024-07-16 アムジエン・インコーポレーテツド Kras g12c阻害剤化合物の重要な中間体の改良合成法
EP3883565A1 (en) 2018-11-19 2021-09-29 Amgen Inc. Kras g12c inhibitors and methods of using the same
JP7377679B2 (ja) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのkrasg12c阻害剤及び1種以上の薬学的に活性な追加の薬剤を含む併用療法
WO2020123395A1 (en) 2018-12-10 2020-06-18 Ideaya Biosciences, Inc. 2-oxoquinazoline derivatives as methionine adenosyltransferase 2a inhibitors
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
CN114144414A (zh) 2019-05-21 2022-03-04 美国安进公司 固态形式
EP3972967A4 (en) 2019-05-21 2023-07-12 InventisBio Co., Ltd. HETEROCYCLIC COMPOUNDS, PROCESSES FOR THEIR PREPARATION AND THEIR USES
WO2020239123A1 (zh) * 2019-05-31 2020-12-03 上海翰森生物医药科技有限公司 芳香杂环类衍生物调节剂、其制备方法和应用
CN112047937B (zh) * 2019-06-06 2023-04-07 劲方医药科技(上海)有限公司 四氢吡啶并[3,4-d]嘧啶-2(1H)-酮类化合物,其制法与医药上的用途
AU2020308353B9 (en) * 2019-06-24 2024-01-25 Guangdong Newopp Biopharmaceuticals Co., Ltd. Heterocyclic compounds as inhibitors of KRAS G12C
CN110256421A (zh) * 2019-06-26 2019-09-20 微境生物医药科技(上海)有限公司 Kras-g12c抑制剂
US12122787B2 (en) 2019-09-20 2024-10-22 Shanghai Jemincare Pharmaceuticals Co., Ltd Fused pyridone compound, and preparation method therefor and use thereof
CA3158793A1 (en) * 2019-10-28 2021-05-06 Merck Sharp & Dohme Corp. Small molecule inhibitors of kras g12c mutant
US11739074B2 (en) 2019-11-04 2023-08-29 Revolution Medicines, Inc. Ras inhibitors
CA3159561A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
WO2021088458A1 (en) * 2019-11-04 2021-05-14 Jacobio Pharmaceuticals Co., Ltd. Kras mutant protein inhibitor
MX2022005360A (es) 2019-11-04 2022-06-02 Revolution Medicines Inc Inhibidores de ras.
WO2021108683A1 (en) 2019-11-27 2021-06-03 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
WO2021113595A1 (en) * 2019-12-06 2021-06-10 Beta Pharma, Inc. Phosphorus derivatives as kras inhibitors
WO2021120045A1 (en) * 2019-12-18 2021-06-24 InventisBio Co., Ltd. Heterocyclic compounds, preparation methods and uses thereof
TW202128691A (zh) * 2019-12-19 2021-08-01 大陸商北京加科思新藥研發有限公司 Kras 突變蛋白抑制劑
CN113105448A (zh) * 2020-01-13 2021-07-13 苏州泽璟生物制药股份有限公司 芳基或杂芳基并吡啶酮或嘧啶酮类衍生物及其制备方法和应用
US20230118795A1 (en) * 2020-01-13 2023-04-20 Suzhou Zelgen Biopharmaceuticals Co., Ltd. Aryl or heteroaryl pyridone or pyrimidine derivative, preparation method and use thereof
CN111205286B (zh) * 2020-01-13 2022-12-13 中科苏州药物研究院 作为kras g12c突变蛋白抑制剂的腈甲基哌嗪类衍生物及其应用
CN114671866A (zh) * 2020-12-25 2022-06-28 苏州泽璟生物制药股份有限公司 芳基或杂芳基并吡啶酮或嘧啶酮类衍生物及其制备方法和应用
CN113801113A (zh) * 2020-06-12 2021-12-17 苏州泽璟生物制药股份有限公司 芳基或杂芳基并吡啶酮或嘧啶酮类衍生物及其制备方法和应用
WO2021147965A1 (zh) * 2020-01-21 2021-07-29 南京明德新药研发有限公司 作为kras抑制剂的大环类化合物
CN112159405B (zh) * 2020-02-04 2021-09-14 广州必贝特医药技术有限公司 吡啶并嘧啶酮类化合物及其应用
CN113248521B (zh) * 2020-02-11 2023-07-18 上海和誉生物医药科技有限公司 一种k-ras g12c抑制剂及其制备方法和应用
EP4112606A4 (en) * 2020-02-24 2024-04-10 Shanghai Zheye Biotechnology Co., Ltd. AROMATIC COMPOUND AND ITS USE IN THE PREPARATION OF ANTINEOPLASIC DRUGS
CN114901663B (zh) * 2020-03-02 2024-07-02 上海喆邺生物科技有限公司 一类芳香杂环类化合物及其在药物中的应用
WO2021185233A1 (en) * 2020-03-17 2021-09-23 Jacobio Pharmaceuticals Co., Ltd. Kras mutant protein inhibitors
CN114585624A (zh) * 2020-06-02 2022-06-03 上海喆邺生物科技有限公司 一种手性中间体及其制备方法
WO2021252339A1 (en) * 2020-06-08 2021-12-16 Accutar Biotechnology, Inc. Substituted purine-2,6-dione compounds as kras inhibitors
WO2021249563A1 (zh) * 2020-06-12 2021-12-16 苏州泽璟生物制药股份有限公司 芳基或杂芳基并吡啶酮或嘧啶酮类衍生物及其制备方法和应用
JP2023530351A (ja) 2020-06-18 2023-07-14 レヴォリューション・メディスンズ,インコーポレイテッド Ras阻害剤への獲得耐性を遅延させる、防止する、及び、治療する方法
EP4194452A4 (en) * 2020-08-02 2024-08-21 Shanghai Zheye Biotechnology Co Ltd AROMATIC COMPOUND AND ITS USE IN ANTITUMOUS MEDICINES
CN114075195A (zh) * 2020-08-21 2022-02-22 广东东阳光药业有限公司 嘧啶酮衍生物及其在药物中的应用
EP4204412A4 (en) * 2020-08-26 2024-10-09 Inventisbio Co Ltd HETEROARYL COMPOUNDS, PROCESSES OF THEIR PREPARATION AND THEIR USES
CA3187757A1 (en) 2020-09-03 2022-03-24 Ethan AHLER Use of sos1 inhibitors to treat malignancies with shp2 mutations
MX2023003060A (es) 2020-09-15 2023-04-05 Revolution Medicines Inc Derivados indolicos como inhibidores de ras en el tratamiento del cancer.
TW202229278A (zh) * 2020-11-26 2022-08-01 大陸商上海翰森生物醫藥科技有限公司 含氮雜環類衍生物的鹽、晶型及其製備方法和應用
WO2022127915A1 (zh) * 2020-12-18 2022-06-23 正大天晴药业集团股份有限公司 吡啶并嘧啶酮类化合物
CN116249703A (zh) * 2020-12-21 2023-06-09 上海和誉生物医药科技有限公司 一种大环k-ras g12c抑制剂,其制备方法和用途
WO2022221528A2 (en) * 2021-04-16 2022-10-20 Mirati Therapeutics, Inc. Kras g12c inhibitors
AU2022270116A1 (en) 2021-05-05 2023-12-21 Revolution Medicines, Inc. Ras inhibitors
WO2022235870A1 (en) 2021-05-05 2022-11-10 Revolution Medicines, Inc. Ras inhibitors for the treatment of cancer
WO2022237815A1 (en) * 2021-05-12 2022-11-17 Jacobio Pharmaceuticals Co., Ltd. Novel forms of Compound I and use thereof
CN115433183B (zh) * 2021-06-04 2024-01-02 润佳(苏州)医药科技有限公司 Kras抑制剂及其用途
WO2022266206A1 (en) 2021-06-16 2022-12-22 Erasca, Inc. Kras inhibitor conjugates
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
WO2023114954A1 (en) 2021-12-17 2023-06-22 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
WO2023172940A1 (en) 2022-03-08 2023-09-14 Revolution Medicines, Inc. Methods for treating immune refractory lung cancer
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2024102421A2 (en) 2022-11-09 2024-05-16 Revolution Medicines, Inc. Compounds, complexes, and methods for their preparation and of their use
WO2024206858A1 (en) 2023-03-30 2024-10-03 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
WO2024211663A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
WO2024211712A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
US20240352036A1 (en) 2023-04-14 2024-10-24 Revolution Medicines, Inc. Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof
US20240352038A1 (en) 2023-04-14 2024-10-24 Revolution Medicines, Inc. Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof

Family Cites Families (235)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4232027A (en) 1979-01-29 1980-11-04 E. R. Squibb & Sons, Inc. 1,2-Dihydro-2-oxo-4-phenyl-3-quinolinecarbonitrile derivatives
GB2116183B (en) 1982-03-03 1985-06-05 Genentech Inc Human antithrombin iii dna sequences therefore expression vehicles and cloning vectors containing such sequences and cell cultures transformed thereby a process for expressing human antithrombin iii and pharmaceutical compositions comprising it
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
JP2762522B2 (ja) 1989-03-06 1998-06-04 藤沢薬品工業株式会社 血管新生阻害剤
GB8912336D0 (en) 1989-05-30 1989-07-12 Smithkline Beckman Intercredit Compounds
US5112946A (en) 1989-07-06 1992-05-12 Repligen Corporation Modified pf4 compositions and methods of use
PT98990A (pt) 1990-09-19 1992-08-31 American Home Prod Processo para a preparacao de esteres de acidos carboxilicos de rapamicina
US5892112A (en) 1990-11-21 1999-04-06 Glycomed Incorporated Process for preparing synthetic matrix metalloprotease inhibitors
US5120842A (en) 1991-04-01 1992-06-09 American Home Products Corporation Silyl ethers of rapamycin
US5100883A (en) 1991-04-08 1992-03-31 American Home Products Corporation Fluorinated esters of rapamycin
US5118678A (en) 1991-04-17 1992-06-02 American Home Products Corporation Carbamates of rapamycin
CA2066898A1 (en) 1991-04-29 1992-10-30 Chuan Shih Pharmaceutical compounds
ATE159009T1 (de) 1991-05-10 1997-10-15 Rhone Poulenc Rorer Int Bis mono- und bicyclische aryl- und heteroarylderivate mit inhibierender wirkung auf die egf und/oder pdgf-rezeptor tyrosinkinase
US5118677A (en) 1991-05-20 1992-06-02 American Home Products Corporation Amide esters of rapamycin
NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
US5151413A (en) 1991-11-06 1992-09-29 American Home Products Corporation Rapamycin acetals as immunosuppressant and antifungal agents
GB9125660D0 (en) 1991-12-03 1992-01-29 Smithkline Beecham Plc Novel compound
GB9300059D0 (en) 1992-01-20 1993-03-03 Zeneca Ltd Quinazoline derivatives
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
ZA935111B (en) 1992-07-17 1994-02-04 Smithkline Beecham Corp Rapamycin derivatives
ZA935112B (en) 1992-07-17 1994-02-08 Smithkline Beecham Corp Rapamycin derivatives
US5256790A (en) 1992-08-13 1993-10-26 American Home Products Corporation 27-hydroxyrapamycin and derivatives thereof
GB9221220D0 (en) 1992-10-09 1992-11-25 Sandoz Ag Organic componds
US5258389A (en) 1992-11-09 1993-11-02 Merck & Co., Inc. O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives
CA2148484A1 (en) 1992-11-13 1994-05-26 Stewart Lyman Novel cytokine designated elk ligand
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
US5629327A (en) 1993-03-01 1997-05-13 Childrens Hospital Medical Center Corp. Methods and compositions for inhibition of angiogenesis
US5516658A (en) 1993-08-20 1996-05-14 Immunex Corporation DNA encoding cytokines that bind the cell surface receptor hek
US5612340A (en) 1993-10-01 1997-03-18 Ciba-Geigy Corporation Pyrimidineamine derivatives and processes for the preparation thereof
US5656643A (en) 1993-11-08 1997-08-12 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono-and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
EP0729471A1 (en) 1993-11-19 1996-09-04 Abbott Laboratories Semisynthetic analogs of rapamycin (macrolides) being immunomodulators
WO1995016691A1 (en) 1993-12-17 1995-06-22 Sandoz Ltd. Rapamycin derivatives useful as immunosuppressants
US5700823A (en) 1994-01-07 1997-12-23 Sugen, Inc. Treatment of platelet derived growth factor related disorders such as cancers
IL112248A0 (en) 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
WO1995024190A2 (en) 1994-03-07 1995-09-14 Sugen, Inc. Receptor tyrosine kinase inhibitors for inhibiting cell proliferative disorders and compositions thereof
CA2189028A1 (en) 1994-04-15 1995-10-26 Gary M. Fox Hek5, hek7, hek8, hek11, new eph-like receptor protein tyrosine kinases
DK0682027T3 (da) 1994-05-03 1998-05-04 Ciba Geigy Ag Pyrrolopyrimidinderivater med antiproliferativ virkning
US6303769B1 (en) 1994-07-08 2001-10-16 Immunex Corporation Lerk-5 dna
US5919905A (en) 1994-10-05 1999-07-06 Immunex Corporation Cytokine designated LERK-6
US6057124A (en) 1995-01-27 2000-05-02 Amgen Inc. Nucleic acids encoding ligands for HEK4 receptors
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
EP2295415A1 (en) 1995-03-30 2011-03-16 OSI Pharmaceuticals, Inc. Quinazoline derivatives
DE69609602T2 (de) 1995-04-03 2001-04-12 Novartis Ag, Basel Pyrazolderivate und verfahren zu deren herstellung
US5861510A (en) 1995-04-20 1999-01-19 Pfizer Inc Arylsulfonyl hydroxamic acid derivatives as MMP and TNF inhibitors
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
US5650415A (en) 1995-06-07 1997-07-22 Sugen, Inc. Quinoline compounds
ATE228135T1 (de) 1995-06-09 2002-12-15 Novartis Erfind Verwalt Gmbh Rapamycinderivate
PL188959B1 (pl) 1995-07-06 2005-05-31 Novartis Ag Pirolopirymidyny i sposoby ich wytwarzania
DE19534177A1 (de) 1995-09-15 1997-03-20 Merck Patent Gmbh Cyclische Adhäsionsinhibitoren
AR004010A1 (es) 1995-10-11 1998-09-30 Glaxo Group Ltd Compuestos heterociclicos
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
EP0780386B1 (en) 1995-12-20 2002-10-02 F. Hoffmann-La Roche Ag Matrix metalloprotease inhibitors
ATE217873T1 (de) 1996-01-23 2002-06-15 Novartis Erfind Verwalt Gmbh Pyrrolopyrimidinen und verfahren zu deren herstellung
JP3406763B2 (ja) 1996-01-30 2003-05-12 東レ・ダウコーニング・シリコーン株式会社 シリコーンゴム組成物
GB9603097D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline compounds
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
DE19608588A1 (de) 1996-03-06 1997-09-11 Thomae Gmbh Dr K Pyrimido [5,4-d]pyrimidine, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
DE19629652A1 (de) 1996-03-06 1998-01-29 Thomae Gmbh Dr K 4-Amino-pyrimidin-Derivate, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
DE59710417D1 (de) 1996-03-15 2003-08-14 Novartis Ag N-7 HETEROCYCLYL-PYRROLO[ 2,3-d]PYRIMIDINE UND IHRE VERWENDUNG
NZ332119A (en) 1996-04-12 2001-08-31 Warner Lambert Co Quinazoline compounds which are irreversible inhibitors of tyrosine kinases
GB9607729D0 (en) 1996-04-13 1996-06-19 Zeneca Ltd Quinazoline derivatives
WO1997049688A1 (en) 1996-06-24 1997-12-31 Pfizer Inc. Phenylamino-substituted tricyclic derivatives for treatment of hyperproliferative diseases
AU735648B2 (en) 1996-07-12 2001-07-12 Ariad Pharmaceuticals, Inc. Materials and method for treating or preventing pathogenic fungal infection
EP0818442A3 (en) 1996-07-12 1998-12-30 Pfizer Inc. Cyclic sulphone derivatives as inhibitors of metalloproteinases and of the production of tumour necrosis factor
CZ8799A3 (cs) 1996-07-13 1999-06-16 Glaxo Group Limited Bicyklické heteroaromatické sloučeniny, způsob jejich výroby a farmaceutický prostředek
AR007857A1 (es) 1996-07-13 1999-11-24 Glaxo Group Ltd Compuestos heterociclicos fusionados como inhibidores de proteina tirosina quinasa, sus metodos de preparacion, intermediarios uso en medicina ycomposiciones farmaceuticas que los contienen.
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
AU712973B2 (en) 1996-07-18 1999-11-18 Pfizer Inc. Phosphinate based inhibitors of matrix metalloproteases
DK0920505T3 (da) 1996-08-16 2008-09-08 Schering Corp Pattedyrcelleoverfladeantigener og tilhörende reagenser
US6111090A (en) 1996-08-16 2000-08-29 Schering Corporation Mammalian cell surface antigens; related reagents
EA199900139A1 (ru) 1996-08-23 1999-08-26 Пфайзер, Инк. Производные арилсульфониламиногидроксамовой кислоты
PT938486E (pt) 1996-08-23 2008-03-27 Novartis Ag Pirrolopirimidinas substituídas e processos para a sua preparação
WO1998014449A1 (en) 1996-10-02 1998-04-09 Novartis Ag Fused pyrazole derivatives and processes for their preparation
CA2266519C (en) 1996-10-02 2007-01-23 Novartis Ag Pyrimidine derivatives and processes for the preparation thereof
ID18494A (id) 1996-10-02 1998-04-16 Novartis Ag Turunan pirazola leburan dan proses pembuatannya
EP0837063A1 (en) 1996-10-17 1998-04-22 Pfizer Inc. 4-Aminoquinazoline derivatives
GB9621757D0 (en) 1996-10-18 1996-12-11 Ciba Geigy Ag Phenyl-substituted bicyclic heterocyclyl derivatives and their use
BR9714266A (pt) 1997-01-06 2000-04-18 Pfizer Derivados de sulfona cìclicos.
DK0977733T3 (da) 1997-02-03 2003-11-24 Pfizer Prod Inc Arylsulfonylaminohydroxamsyrederivater
JP2001509805A (ja) 1997-02-05 2001-07-24 ワーナー−ランバート・コンパニー 細胞増殖阻害剤としてのピリド〔2,3−d〕ピリミジンおよび4−アミノピリミジン
EP0966438A1 (en) 1997-02-07 1999-12-29 Pfizer Inc. N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases
HUP0000657A3 (en) 1997-02-11 2000-10-30 Pfizer N-arylsulfonyl-piperidine, -morpholine hydroxamic acid derivatives and pharmaceutical compositions containing them
CO4950519A1 (es) 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
US6150395A (en) 1997-05-30 2000-11-21 The Regents Of The University Of California Indole-3-carbinol (I3C) derivatives and methods
AU8689298A (en) 1997-08-05 1999-03-01 Sugen, Inc. Tricyclic quinoxaline derivatives as protein tyrosine kinase inhibitors
YU1900A (sh) 1997-08-08 2002-08-12 Pfizer Products Inc. Derivati ariloksiarilsulfonilamino hidroksaminske kiseline
WO1999020758A1 (en) 1997-10-21 1999-04-29 Human Genome Sciences, Inc. Human tumor necrosis factor receptor-like proteins tr11, tr11sv1, and tr11sv2
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
GB9800575D0 (en) 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
RS49779B (sr) 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
GB9801690D0 (en) 1998-01-27 1998-03-25 Pfizer Ltd Therapeutic agents
JP2002502607A (ja) 1998-02-09 2002-01-29 ジェネンテク・インコーポレイテッド 新規な腫瘍壊死因子レセプター相同体及びそれをコードする核酸
ES2324846T3 (es) 1998-03-04 2009-08-17 Bristol-Myers Squibb Company Inhibidores de la proteina tirosina quinasa de imidazopirazina heterociclo-sustituida.
PA8469501A1 (es) 1998-04-10 2000-09-29 Pfizer Prod Inc Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico
PA8469401A1 (es) 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
TR200003514T2 (tr) 1998-05-29 2002-05-21 Sugen Inc. Pirol ikame edilmiş 2-indolinon protein kinaz inhibitörleri
UA60365C2 (uk) 1998-06-04 2003-10-15 Пфайзер Продактс Інк. Похідні ізотіазолу, спосіб їх одержання, фармацевтична композиція та спосіб лікування гіперпроліферативного захворювання у ссавця
EP1097147A4 (en) 1998-07-10 2001-11-21 Merck & Co Inc NEW ANGIOGENESIS INHIBITORS
JP2002523459A (ja) 1998-08-31 2002-07-30 メルク エンド カムパニー インコーポレーテッド 新規血管形成阻害剤
ATE260255T1 (de) 1998-11-05 2004-03-15 Pfizer Prod Inc 5-oxo-pyrrolidine-2-carbonsäure- hydroxamidderivate
ES2377847T3 (es) 1999-01-13 2012-04-02 Bayer Healthcare Llc Difenil ureas sustituidas con omega-carboxi arilo como agentes inhibidores de la cinasa p38
EP1165085B1 (en) 1999-03-30 2006-06-14 Novartis AG Phthalazine derivatives for treating inflammatory diseases
GB9912961D0 (en) 1999-06-03 1999-08-04 Pfizer Ltd Metalloprotease inhibitors
US6521424B2 (en) 1999-06-07 2003-02-18 Immunex Corporation Recombinant expression of Tek antagonists
PT1187918E (pt) 1999-06-07 2006-08-31 Immunex Corp Antagonistas de tek
AU6085700A (en) 1999-07-12 2001-01-30 Genentech Inc. Promotion or inhibition of angiogenesis and cardiovascularization by tumor necrosis factor ligand/receptor homologs
CA2383451A1 (en) 1999-08-24 2001-03-01 Ariad Gene Therapeutics, Inc. 28-epirapalogs
JP3522727B2 (ja) 1999-11-05 2004-04-26 アストラゼネカ アクチボラグ Vegf阻害剤としてのキナゾリン誘導体
JP5336686B2 (ja) 1999-11-24 2013-11-06 スージェン, インク. 遊離酸または遊離塩基としてイオン化可能な医薬品のための処方
US6515004B1 (en) 1999-12-15 2003-02-04 Bristol-Myers Squibb Company N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases
US6727225B2 (en) 1999-12-20 2004-04-27 Immunex Corporation TWEAK receptor
CA2400040A1 (en) 2000-02-25 2001-08-30 Immunex Corporation Integrin antagonists
KR100773621B1 (ko) 2000-07-19 2007-11-05 워너-램버트 캄파니 엘엘씨 4-요오도 페닐아미노 벤즈히드록삼산의 산소화 에스테르
US6630500B2 (en) 2000-08-25 2003-10-07 Cephalon, Inc. Selected fused pyrrolocarbazoles
CN1307173C (zh) 2000-12-21 2007-03-28 葛兰素集团有限公司 作为血管生成调节剂的嘧啶胺
US7105682B2 (en) 2001-01-12 2006-09-12 Amgen Inc. Substituted amine derivatives and methods of use
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
US7102009B2 (en) 2001-01-12 2006-09-05 Amgen Inc. Substituted amine derivatives and methods of use
US20020147198A1 (en) 2001-01-12 2002-10-10 Guoqing Chen Substituted arylamine derivatives and methods of use
US6878714B2 (en) 2001-01-12 2005-04-12 Amgen Inc. Substituted alkylamine derivatives and methods of use
US7307088B2 (en) 2002-07-09 2007-12-11 Amgen Inc. Substituted anthranilic amide derivatives and methods of use
TWI329112B (en) 2002-07-19 2010-08-21 Bristol Myers Squibb Co Novel inhibitors of kinases
WO2004063195A1 (en) 2003-01-03 2004-07-29 Sloan-Kettering Institute For Cancer Research Pyridopyrimidine kinase inhibitors
RU2369636C2 (ru) 2003-05-23 2009-10-10 Уайт Лиганд gitr и связанные с лигандом gitr молекулы и антитела и варианты их применения
ES2316995T3 (es) 2003-07-08 2009-04-16 Novartis Ag Uso de rapamicina y derivados de rapamicida para el tratamiento de la perdida osea.
WO2005016252A2 (en) 2003-07-11 2005-02-24 Ariad Gene Therapeutics, Inc. Phosphorus-containing macrocycles
EP1660126A1 (en) 2003-07-11 2006-05-31 Schering Corporation Agonists or antagonists of the clucocorticoid-induced tumour necrosis factor receptor (gitr) or its ligand for the treatment of immune disorders, infections and cancer
TW200523262A (en) 2003-07-29 2005-07-16 Smithkline Beecham Corp Inhibitors of AKT activity
CN1839133A (zh) 2003-08-22 2006-09-27 阿文尼尔药品公司 作为巨噬细胞移动抑制因子的抑制剂的取代的二氮杂萘衍生物及其在治疗人类疾病中的应用
JP2007518399A (ja) 2003-12-02 2007-07-12 ジェンザイム コーポレイション 肺癌を診断および治療する組成物並びに方法
GB0409799D0 (en) 2004-04-30 2004-06-09 Isis Innovation Method of generating improved immune response
WO2006083289A2 (en) 2004-06-04 2006-08-10 Duke University Methods and compositions for enhancement of immunity by in vivo depletion of immunosuppressive cell activity
SI1786785T1 (sl) 2004-08-26 2010-07-30 Pfizer Enantiomerno ÄŤiste aminoheteroarilne spojine kot inhibitorji protein-kinaze
GT200500287A (es) 2004-10-13 2006-04-17 Analogos de 17-hidroxiwortmanina como inhibidores de pi3k
BRPI0516609A (pt) 2004-10-18 2008-04-29 Amgen Inc composto ou sal, hidrato, ou estereoisÈmero farmaceuticamente aceitáveis do mesmo, composição farmacêutica, e, uso de um composto
PT2343320T (pt) 2005-03-25 2018-01-23 Gitr Inc Anticorpos anti-gitr e as suas utilizações
WO2006121168A1 (en) 2005-05-09 2006-11-16 Ono Pharmaceutical Co., Ltd. Human monoclonal antibodies to programmed death 1(pd-1) and methods for treating cancer using anti-pd-1 antibodies alone or in combination with other immunotherapeutics
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
CN101267824A (zh) 2005-09-20 2008-09-17 辉瑞产品公司 使用酪氨酸激酶抑制剂的治疗剂型和方法
MY149143A (en) 2006-01-18 2013-07-15 Amgen Inc Thiazole compounds as protien kinase b (pkb) inhibitors
WO2007133822A1 (en) 2006-01-19 2007-11-22 Genzyme Corporation Gitr antibodies for the treatment of cancer
KR101460816B1 (ko) 2006-12-07 2014-11-12 에프. 호프만-라 로슈 아게 포스포이노시타이드 3-키나제 억제제 화합물 및 그의 사용 방법
WO2008118468A1 (en) 2007-03-23 2008-10-02 Amgen Inc. Heterocyclic compounds and their uses
CA2680783C (en) 2007-03-23 2012-04-24 Amgen Inc. Heterocyclic compounds and their uses
CA2680853C (en) 2007-03-23 2012-07-17 Amgen Inc. 3- substituted quinoline or quinoxaline derivatives and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors
CA2689092C (en) 2007-06-07 2013-01-15 Amgen Inc. Raf kinase modulators and methods of use
DK2175884T3 (en) 2007-07-12 2016-09-26 Gitr Inc Combination USING GITR BINDING MOLECULES
WO2009011871A2 (en) 2007-07-17 2009-01-22 Amgen Inc. Thiadiazole modulators of pkb
US7897619B2 (en) 2007-07-17 2011-03-01 Amgen Inc. Heterocyclic modulators of PKB
CA2694136C (en) 2007-08-02 2013-09-17 Amgen Inc. Pi3 kinase modulators and methods of use
MX338504B (es) 2007-09-12 2016-04-20 Genentech Inc Combinaciones de compuestos inhibidores de fosfoinosituro 3-cinasa y agentes quimioterapeuticos, y metodos de uso.
CN101909631B (zh) 2007-10-25 2012-09-12 健泰科生物技术公司 制备噻吩并嘧啶化合物的方法
US8841312B2 (en) 2007-12-19 2014-09-23 Amgen Inc. Fused pyridine, pyrimidine and triazine compounds as cell cycle inhibitors
AU2008343813B2 (en) 2007-12-19 2012-04-12 Amgen Inc. Inhibitors of PI3 kinase
ATE531372T1 (de) 2008-04-07 2011-11-15 Amgen Inc Gem-disubstituierte und spirocyclische aminopyridine/pyrimidine als zellcyclus- inhibitoren
EP2307400B1 (en) 2008-05-30 2014-04-23 Amgen, Inc Inhibitors of pi3 kinase
NZ590667A (en) 2008-07-02 2013-01-25 Emergent Product Dev Seattle Tgf-b antagonist multi-target binding proteins
JPWO2010030002A1 (ja) 2008-09-12 2012-02-02 国立大学法人三重大学 外来性gitrリガンド発現細胞
EP2387570A1 (en) 2009-01-15 2011-11-23 Amgen, Inc Fluoroisoquinoline substituted thiazole compounds and methods of use
CA2752527C (en) 2009-02-18 2014-09-23 Amgen Inc. Indole/benzimidazole compounds as mtor kinase inhibitors
WO2010108074A2 (en) 2009-03-20 2010-09-23 Amgen Inc. Inhibitors of pi3 kinase
UY32582A (es) 2009-04-28 2010-11-30 Amgen Inc Inhibidores de fosfoinositida 3 cinasa y/u objetivo mamífero
AU2010249040B2 (en) 2009-05-13 2013-08-22 Amgen Inc. Heteroaryl compounds as PIKK inhibitors
CA2765817A1 (en) 2009-06-25 2010-12-29 Amgen Inc. 4h-pyrido[1,2-a]pyrimidin-4-one derivatives as pi3k inhibitors
TW201111376A (en) 2009-06-25 2011-04-01 Amgen Inc Heterocyclic compounds and their uses
US8765940B2 (en) 2009-06-25 2014-07-01 Amgen Inc. Heterocyclic compounds and their uses
UY32743A (es) 2009-06-25 2010-12-31 Amgen Inc Compuestos heterocíclicos y sus usos
EP2266984A1 (en) 2009-06-26 2010-12-29 Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts Pyrido[2,3-d]pyrimidines as Wnt antagonists for treatment of cancer and arthritis
RU2595409C2 (ru) 2009-09-03 2016-08-27 Мерк Шарп И Доум Корп., Анти-gitr-антитела
JP5851403B2 (ja) 2009-09-11 2016-02-03 アムジエン・インコーポレーテツド 有糸分裂阻害剤耐性癌の治療における使用のためのn−4(−((3−(2−アミノ−4ピリミジニル)−2−ピリジニル)オキシ)フェニル)−4−(4−メチル−2−チエニル)−1−フタラジンアミン
GB0919054D0 (en) 2009-10-30 2009-12-16 Isis Innovation Treatment of obesity
KR20120125611A (ko) 2009-12-29 2012-11-16 이머전트 프로덕트 디벨롭먼트 시애틀, 엘엘씨 이종이량체 결합 단백질 및 이의 용도
US9133164B2 (en) 2011-04-13 2015-09-15 Innov88 Llc MIF inhibitors and their uses
US20130108641A1 (en) 2011-09-14 2013-05-02 Sanofi Anti-gitr antibodies
CN104379563B (zh) 2012-04-10 2018-12-21 加利福尼亚大学董事会 用于治疗癌症的组合物和方法
CN104507942B (zh) 2012-08-07 2017-03-22 默克专利股份公司 作为蛋白质激酶抑制剂的吡啶并嘧啶衍生物
UY35464A (es) 2013-03-15 2014-10-31 Araxes Pharma Llc Inhibidores covalentes de kras g12c.
WO2014143659A1 (en) 2013-03-15 2014-09-18 Araxes Pharma Llc Irreversible covalent inhibitors of the gtpase k-ras g12c
EP3401314B1 (en) 2013-03-15 2023-11-08 Araxes Pharma LLC Covalent inhibitors of kras g12c
GB201312059D0 (en) 2013-07-05 2013-08-21 Univ Leuven Kath Novel GAK modulators
MX2016004360A (es) * 2013-10-10 2016-08-19 Araxes Pharma Llc Inhibidores de kras g12c.
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Kras g12c之抑制劑
GB201320729D0 (en) 2013-11-25 2014-01-08 Cancer Rec Tech Ltd Therapeutic compounds and their use
EP3097092B1 (en) 2014-01-20 2020-08-26 Cleave Biosciences, Inc. Fused pyrimidines as inhibitors of p97 complex
WO2016035008A1 (en) 2014-09-04 2016-03-10 Lupin Limited Pyridopyrimidine derivatives as mek inhibitors
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
WO2016049565A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Compositions and methods for inhibition of ras
US9862701B2 (en) 2014-09-25 2018-01-09 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2016049568A1 (en) 2014-09-25 2016-03-31 Araxes Pharma Llc Methods and compositions for inhibition of ras
US10246424B2 (en) 2015-04-10 2019-04-02 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
EP3283462B1 (en) 2015-04-15 2020-12-02 Araxes Pharma LLC Fused-tricyclic inhibitors of kras and methods of use thereof
MX2018000777A (es) 2015-07-22 2018-03-23 Araxes Pharma Llc Compuestos de quinazolina sustituido y su uso como inhibidores de proteinas kras, hras y/o nras mutantes g12c.
US10689356B2 (en) 2015-09-28 2020-06-23 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058728A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
WO2017058915A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10875842B2 (en) 2015-09-28 2020-12-29 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10882847B2 (en) 2015-09-28 2021-01-05 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
EP3356354A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3356351A1 (en) 2015-09-28 2018-08-08 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
KR20240113606A (ko) 2015-11-16 2024-07-22 아락세스 파마 엘엘씨 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법
WO2017100546A1 (en) 2015-12-09 2017-06-15 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
WO2017172979A1 (en) 2016-03-30 2017-10-05 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
EP3458445B1 (en) * 2016-05-18 2021-02-17 Mirati Therapeutics, Inc. Kras g12c inhibitors
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
JP2019529484A (ja) 2016-09-29 2019-10-17 アラクセス ファーマ エルエルシー Kras g12c変異体タンパク質の阻害剤
US10377743B2 (en) 2016-10-07 2019-08-13 Araxes Pharma Llc Inhibitors of RAS and methods of use thereof
RS62456B1 (sr) 2016-12-22 2021-11-30 Amgen Inc Derivati benzizotiazola, izotiazolo[3,4-b]piridina, hinazolina, ftalazina, pirido[2,3-d]piridazina i pirido[2,3-d]pirimidina kao kras g12c inhibitori za tretman raka pluća, pankreasa ili debelog creva
WO2018140598A1 (en) 2017-01-26 2018-08-02 Araxes Pharma Llc Fused n-heterocyclic compounds and methods of use thereof
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
EP3630747A1 (en) 2017-05-25 2020-04-08 Araxes Pharma LLC Quinazoline derivatives as modulators of mutant kras, hras or nras
EP4403175A3 (en) 2017-09-08 2024-10-02 Amgen Inc. Inhibitors of kras g12c and methods of using the same
MA52496A (fr) 2018-05-04 2021-03-10 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
MA52501A (fr) 2018-05-04 2021-03-10 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
CA3099045A1 (en) 2018-05-10 2019-11-14 Amgen Inc. Kras g12c inhibitors for the treatment of cancer
WO2019232419A1 (en) 2018-06-01 2019-12-05 Amgen Inc. Kras g12c inhibitors and methods of using the same
AU2019284472B2 (en) 2018-06-11 2024-05-30 Amgen Inc. KRAS G12C inhibitors for treating cancer
MX2020012261A (es) 2018-06-12 2021-03-31 Amgen Inc Inhibidores de kras g12c que comprenden un anillo de piperazina y uso de estos en el tratamiento del cancer.
WO2019243533A1 (en) 2018-06-21 2019-12-26 Janssen Pharmaceutica Nv Oga inhibitor compounds
AU2019291101A1 (en) 2018-06-21 2021-01-07 Janssen Pharmaceutica Nv OGA inhibitor compounds
JP7516029B2 (ja) 2018-11-16 2024-07-16 アムジエン・インコーポレーテツド Kras g12c阻害剤化合物の重要な中間体の改良合成法
EP3883565A1 (en) 2018-11-19 2021-09-29 Amgen Inc. Kras g12c inhibitors and methods of using the same
JP7377679B2 (ja) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのkrasg12c阻害剤及び1種以上の薬学的に活性な追加の薬剤を含む併用療法
KR20210121168A (ko) 2019-01-29 2021-10-07 브라이트제네 바이오-메디컬 테크놀로지 코., 엘티디. 복소환식 화합물인 벤조피리돈 및 그 사용
US10890227B2 (en) 2019-03-20 2021-01-12 Goodrich Corporation Wear liner with unidirectional notch
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
CN114144414A (zh) 2019-05-21 2022-03-04 美国安进公司 固态形式
CA3140394A1 (en) 2019-05-21 2020-11-26 Amgen Inc. Solid state forms
EP4048671A1 (en) 2019-10-24 2022-08-31 Amgen Inc. Pyridopyrimidine derivatives useful as kras g12c and kras g12d inhibitors in the treatment of cancer
AU2020381492A1 (en) 2019-11-14 2022-05-26 Amgen Inc. Improved synthesis of KRAS G12C inhibitor compound
AU2020383535A1 (en) 2019-11-14 2022-05-05 Amgen Inc. Improved synthesis of KRAS G12C inhibitor compound
WO2021126816A1 (en) 2019-12-16 2021-06-24 Amgen Inc. Dosing regimen of a kras g12c inhibitor
WO2021236920A1 (en) 2020-05-20 2021-11-25 Teva Pharmaceuticals International Gmbh Solid state forms of amg-510 and process for preparation thereof

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US12083121B2 (en) 2024-09-10
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