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AR076550A1 - Inhibidores de la janus tirosina kinasa (jak) - Google Patents

Inhibidores de la janus tirosina kinasa (jak)

Info

Publication number
AR076550A1
AR076550A1 ARP100101558A ARP100101558A AR076550A1 AR 076550 A1 AR076550 A1 AR 076550A1 AR P100101558 A ARP100101558 A AR P100101558A AR P100101558 A ARP100101558 A AR P100101558A AR 076550 A1 AR076550 A1 AR 076550A1
Authority
AR
Argentina
Prior art keywords
alkyl
heterocyclyl
aryl
heteroalkyl
heteroaryl
Prior art date
Application number
ARP100101558A
Other languages
English (en)
Inventor
Jack W Rose
Yonghong Song
Qing Xu
Mukund Mehrotra
Anjali Pandey
Shawn M Bauer
Wolin Huang
Original Assignee
Portola Pharm 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 Portola Pharm Inc filed Critical Portola Pharm Inc
Publication of AR076550A1 publication Critical patent/AR076550A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Compuestos de formula 1 y tautomeros y sales de los mismos farmacéuticamente aceptables que son inhibidores selectivos de JAK. También se refiere a intermediarios que se utilizan para hacer dichos compuestos, a la preparacion de un compuesto con dichas características, a composiciones farmacéuticas que lo contienen, a métodos para inhibir la actividad de la JAK, y a métodos para impedir o tratar varias condiciones mediadas por lo menos en parte por la actividad de la JAK. Reivindicacion 1: Un compuesto caracterizado porque responde a la formula (1) o un tautomero o sales farmacéuticamente aceptables del mismo, donde Y1 es N o CR1c; R1a es (a) cicloalquilo C3-8, opcionalmente sustituido con entre 1 y 3 sustituyentes R1d donde cada R1d se selecciona independientemente entre el grupo que consiste en alquilo C1-8, alquenilo C2-8, alquinilo C2-8, hidroxilo, halogeno, heteroalquilo C1-8, ciano, arilo, heteroarilo, heterociclilo y heterociclilcarbonilo; o si se encuentran en átomos de carbono adyacentes del cicloalquilo C3-8, se pueden combinar con los átomos a los cuales están unidos para formar un grupo arilo; (b) alquilo C1-8, opcionalmente sustituido con entre 1 y 3 sustituyentes seleccionados entre el grupo que consiste en alquenilo C2-8, alquinilo C2-8, amino, hidroxilo, halogeno, heteroalquilo C1-8, ciano, cicloalquilo C3-8, arilo, haloarilo, alquilarilo C1-8, alcoxiarilo C1-8, heteroarilo, heterociclilo C3-8 y heterociclilcarbonilo C3-8; (c) heterociclilo, opcionalmente sustituido con entre 1 y 3 sustituyentes seleccionados entre el grupo que consiste en alquilo C1-8, alquenilo C2-8, alquinilo C2-8, hidroxilo, halogeno, heteroalquilo C1-8, ciano, arilo, heteroarilo, heterociclilo y heterociclilcarbonilo; (c) arilo, opcionalmente sustituido con entre 1 y 3 sustituyentes seleccionados entre el grupo que consiste en aIquilo C1-8, alquenilo C2-8, alquinilo C2-8, hidroxilo, halogeno, heteroalquilo C1-8, ciano, arilo, heteroarilo, heterociclilo y heterociclilcarbonilo, amino y alquilsulfonilo; y (d) heteroarilo, opcionalmente sustituido con entre 1 y 3 sustituyentes seleccionados entre el grupo que consiste en alquilo C1-8, alquenilo C2-8, alquinilo C2-8, hidroxilo, halogeno, heteroalquilo C1-8, ciano, arilo, heteroarilo, heterociclilo y heterociclilcarbonilo; R1b es H o aIquilo C1-8; R1c es H, alquilo C1-8 o halogeno; R2 es H, alquilo C1-8, heteroalquilo C1-8, heterociclil C1-8alcoxi, halogeno o heterociclilo; R3 es H o alquilo C1-8 o cicloalquilo C3-8; R4 se selecciona entre el grupo formado por amino, alquilo C1-8, amino C1-8alquilo, alquenilo C2-8, alquinilo C2-8, heteroalquilo C1-8, cicloalquilo C3-8, arilo, heteroarilo y heterociclilo C3-8; y m es 0, 1, 2 o 3.
ARP100101558A 2009-05-06 2010-05-06 Inhibidores de la janus tirosina kinasa (jak) AR076550A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US17607709P 2009-05-06 2009-05-06
US25623909P 2009-10-29 2009-10-29

Publications (1)

Publication Number Publication Date
AR076550A1 true AR076550A1 (es) 2011-06-22

Family

ID=42558558

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100101558A AR076550A1 (es) 2009-05-06 2010-05-06 Inhibidores de la janus tirosina kinasa (jak)

Country Status (4)

Country Link
US (2) US8367689B2 (es)
AR (1) AR076550A1 (es)
TW (1) TW201040162A (es)
WO (1) WO2010129802A1 (es)

Families Citing this family (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT2323993E (pt) 2008-04-16 2015-10-12 Portola Pharm Inc 2,6-diamino-pirimidina-5-il-carboxamidas como inibidores de quinasses syk ou jak
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
CA2723205C (en) * 2008-04-16 2017-03-14 Portola Pharmaceuticals, Inc. 2,6-diamino-pyrimidin-5-yl-carboxamides as syk or jak kinase inhibitors
TW201040162A (en) 2009-05-06 2010-11-16 Portola Pharm Inc Inhibitors of JAK
EP2571361A4 (en) 2010-05-19 2013-11-13 Univ North Carolina PYRAZOLOPYRIMIDINE COMPOUNDS FOR CANCER TREATMENT
EP2481411A1 (en) * 2011-01-27 2012-08-01 Ratiopharm GmbH Oral dosage forms for modified release comprising the JAK3 inhibitor tasocitinib
CA2829264C (en) 2011-04-22 2020-04-07 Signal Pharmaceuticals, Llc Substituted diaminocarboxamide and diaminocarbonitrile pyrimidines, compositions thereof, and methods of treatment therewith
WO2013054351A1 (en) * 2011-08-08 2013-04-18 Cadila Healthcare Limited Heterocyclic compounds
KR102063098B1 (ko) 2011-10-03 2020-01-08 더 유니버시티 오브 노쓰 캐롤라이나 엣 채플 힐 암 치료를 위한 피롤로피리미딘 화합물
US8987456B2 (en) 2011-10-05 2015-03-24 Merck Sharp & Dohme Corp. 3-pyridyl carboxamide-containing spleen tyrosine kinase (SYK) inhibitors
US9216173B2 (en) 2011-10-05 2015-12-22 Merck Sharp & Dohme Corp. 2-Pyridyl carboxamide-containing spleen tyrosine kinase (SYK) inhibitors
WO2013052391A1 (en) 2011-10-05 2013-04-11 Merck Sharp & Dohme Corp. PHENYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS
SG11201402570QA (en) 2011-11-23 2014-06-27 Portola Pharm Inc Pyrazine kinase inhibitors
KR20140114344A (ko) 2011-12-23 2014-09-26 셀좀 리미티드 키나제 억제제로서의 피리미딘-2,4-디아민 유도체
CN104302627A (zh) * 2012-05-22 2015-01-21 北卡罗来纳大学教堂山分校 用于治疗癌症的嘧啶化合物
US9296725B2 (en) * 2012-05-24 2016-03-29 Cellzome Limited Heterocyclyl pyrimidine analogues as TYK2 inhibitors
US9013997B2 (en) * 2012-06-01 2015-04-21 Broadcom Corporation System for performing distributed data cut-through
US9242984B2 (en) 2012-06-20 2016-01-26 Merck Sharp & Dohme Corp. Pyrazolyl derivatives as Syk inhibitors
WO2013192128A1 (en) 2012-06-20 2013-12-27 Merck Sharp & Dohme Corp. Imidazolyl analogs as syk inhibitors
EP2900665B1 (en) 2012-09-28 2018-01-03 Merck Sharp & Dohme Corp. Triazolyl derivatives as syk inhibitors
EP2909211A4 (en) 2012-10-17 2016-06-22 Univ North Carolina PYRAZOLOPYRIMIDINE COMPOUNDS FOR CANCER TREATMENT
JP6266639B2 (ja) * 2012-11-08 2018-01-24 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ ＩＬ−１２、ＩＬ−２３および／またはＩＦＮαの調節に有用なアルキルアミド置換ピリミジン化合物
EP2925752A4 (en) 2012-11-27 2016-06-01 Univ North Carolina PYRIMIDINE COMPOUNDS FOR CANCER TREATMENT
CN105612154A (zh) 2013-08-07 2016-05-25 卡迪拉保健有限公司 作为詹纳斯激酶的抑制剂的n-氰基甲基酰胺
CN104262328B (zh) * 2013-09-18 2016-09-07 北京韩美药品有限公司 抑制btk和/或jak3激酶活性的化合物
TWI582077B (zh) * 2013-11-07 2017-05-11 必治妥美雅史谷比公司 作爲ＩＬ－１２、ＩＬ－２３及／或ＩＦＮα反應調節劑之經烷基－醯胺取代之吡啶化合物
AU2014360446A1 (en) 2013-12-05 2016-06-09 Pharmacyclics, Llc Inhibitors of Bruton's tyrosine kinase
US9783531B2 (en) 2013-12-20 2017-10-10 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
US9822107B2 (en) 2013-12-20 2017-11-21 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
US9670196B2 (en) 2013-12-20 2017-06-06 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as Spleen Tyrosine Kinase inhibitors
NZ715903A (en) * 2014-01-30 2017-06-30 Signal Pharm Llc Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use
US9775839B2 (en) 2014-03-13 2017-10-03 Merck Sharp & Dohme Corp. 2-pyrazine carboxamides as spleen tyrosine kinase inhibitors
EP3129379A4 (en) 2014-04-11 2017-09-13 The University of North Carolina at Chapel Hill Mertk-specific pyrrolopyrimidine compounds
ES2877642T3 (es) 2014-12-16 2021-11-17 Signal Pharm Llc Formulaciones de 2-(terc-butilamino)-4-((1R,3R,4R)-3-hidroxi-4-metilciclohexilamino)-pirimidin-5-carboxamida
US9513297B2 (en) 2014-12-16 2016-12-06 Signal Pharmaceuticals, Llc Methods for measurement of inhibition of c-Jun N-terminal kinase in skin
US20180022710A1 (en) 2015-01-29 2018-01-25 Signal Pharmaceuticals, Llc Isotopologues of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide
CN104987324B (zh) * 2015-06-04 2018-05-04 湖北生物医药产业技术研究院有限公司 作为alk抑制剂的嘧啶衍生物
MX2018001004A (es) 2015-07-24 2018-06-07 Celgene Corp Metodos de sintesis de clorhidrato de (1r,2r,5r)-5-amino-2-metilci clohexanol e intermedios utiles en este.
SG10201913989QA (en) 2015-10-16 2020-03-30 Abbvie Inc PROCESSES FOR THE PREPARATION OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZO[1,2-a]PYRROLO[2,3-e]-PYRAZIN-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND SOLID STATE FORMS THEREOF
US11365198B2 (en) 2015-10-16 2022-06-21 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US10550126B2 (en) 2015-10-16 2020-02-04 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-A]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11780848B2 (en) 2015-10-16 2023-10-10 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1- carboxamide and solid state forms thereof
US10736895B2 (en) 2015-12-04 2020-08-11 Portola Pharmaceuticals, Inc. Cerdulatinib for treating hematological cancers
US10709708B2 (en) 2016-03-17 2020-07-14 The University Of North Carolina At Chapel Hill Method of treating cancer with a combination of MER tyrosine kinase inhibitor and an epidermal growth factor receptor (EGFR) inhibitor
SG10201913471VA (en) * 2016-04-15 2020-03-30 Epizyme Inc Amine-substituted aryl or heteroaryl compounds as ehmt1 and ehmt2 inhibitors
JP2020504715A (ja) * 2016-12-19 2020-02-13 エピザイム，インコーポレイティド Ｅｈｍｔ２阻害剤としてのアミン置換複素環化合物およびその使用方法
CN118021814A (zh) 2017-04-21 2024-05-14 Epizyme股份有限公司 用ehmt2抑制剂进行的组合疗法
WO2019213606A2 (en) 2018-05-04 2019-11-07 Portola Pharmaceuticals, Inc. Solid forms of cerdulatinib
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
MX2021013317A (es) * 2019-04-30 2022-01-18 Celgene Corp Terapias de combinacion que comprenden inhibidores de apremilast y tyk2.
US20230416237A1 (en) * 2020-11-26 2023-12-28 Artivila (Shenzhen) Innovation Center, Ltd. Amide compound, pharmaceutical composition and use thereof
WO2022166916A1 (zh) * 2021-02-05 2022-08-11 深圳市塔吉瑞生物医药有限公司 取代的杂芳基衍生物及其组合物及用途
EP4401735A1 (en) * 2021-09-16 2024-07-24 Lomond Therapeutics, Inc. Compounds having n-arylpyrimidin-2-amine derivatives as therapeutic agents
TW202329961A (zh) * 2021-11-30 2023-08-01 日商興和股份有限公司 新穎菸鹼醯胺化合物及其用途
WO2023218245A1 (en) * 2022-05-13 2023-11-16 Voronoi Inc. Heteroaryl derivative compounds, and pharmaceutical composition comprising thereof

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6432963B1 (en) 1997-12-15 2002-08-13 Yamanouchi Pharmaceutical Co., Ltd. Pyrimidine-5-carboxamide derivatives
SE0101675D0 (sv) 2001-05-11 2001-05-11 Astrazeneca Ab Novel composition
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
US7449456B2 (en) * 2002-06-28 2008-11-11 Astellas Pharma, Inc. Diaminopyrimidinecarboxamide derivative
US7517886B2 (en) * 2002-07-29 2009-04-14 Rigel Pharmaceuticals, Inc. Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
US7122542B2 (en) 2003-07-30 2006-10-17 Rigel Pharmaceuticals, Inc. Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
AR048454A1 (es) 2004-03-30 2006-04-26 Vertex Pharma Azaindoles utiles como inhibidores de las proteinas quinasas jak u otras proteinas quinasas
US7557207B2 (en) 2004-11-24 2009-07-07 Rigel Pharmaceuticals, Inc. Spiro 2,4-pyrimidinediamine compounds and their uses
JP4801096B2 (ja) 2005-01-19 2011-10-26 ライジェル ファーマシューティカルズ， インコーポレイテッド ２，４−ピリミジンジアミン化合物のプロドラッグおよびそれらの使用
EP1951684B1 (en) * 2005-11-01 2016-07-13 TargeGen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
RU2009105826A (ru) * 2006-07-21 2010-08-27 Новартис АГ (CH) 2,4-ди(ариламино)питимидин-5-карбоксамидные соединения в качестве ингибиторов jak-киназ
EP2152702B1 (en) 2007-05-04 2011-08-24 AstraZeneca AB Amino-thiazolyl- pyrimidine derivatives and their use for the treatment of cancer
US8138339B2 (en) * 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
CA2723205C (en) * 2008-04-16 2017-03-14 Portola Pharmaceuticals, Inc. 2,6-diamino-pyrimidin-5-yl-carboxamides as syk or jak kinase inhibitors
PT2323993E (pt) * 2008-04-16 2015-10-12 Portola Pharm Inc 2,6-diamino-pirimidina-5-il-carboxamidas como inibidores de quinasses syk ou jak
NZ603525A (en) * 2008-06-27 2015-02-27 Celgene Avilomics Res Inc Pyrimidine based compound and uses thereof
US8338439B2 (en) * 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
EA021367B1 (ru) * 2008-11-28 2015-06-30 Кова Компани, Лтд. Производное пиридин-3-карбоксамида
TW201040162A (en) 2009-05-06 2010-11-16 Portola Pharm Inc Inhibitors of JAK

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US20130137673A1 (en) 2013-05-30
US8853230B2 (en) 2014-10-07

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