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MX2020003579A - Compuestos de piridina, pirazina, y triazina como inhibidores de shp2 alostericos. - Google Patents

Compuestos de piridina, pirazina, y triazina como inhibidores de shp2 alostericos.

Info

Publication number
MX2020003579A
MX2020003579A MX2020003579A MX2020003579A MX2020003579A MX 2020003579 A MX2020003579 A MX 2020003579A MX 2020003579 A MX2020003579 A MX 2020003579A MX 2020003579 A MX2020003579 A MX 2020003579A MX 2020003579 A MX2020003579 A MX 2020003579A
Authority
MX
Mexico
Prior art keywords
pyrazine
pyridine
triazine compounds
shp2 inhibitors
allosteric shp2
Prior art date
Application number
MX2020003579A
Other languages
English (en)
Inventor
Naing Aay
Walter Won
Ashutosh Jogalekar
Elena S Koltun
Kevin Mellem
Christos Tzitzilonis
Jie Jack Li
Adrian Liam Gill
Andreas Buckl
James Joseph Cregg
Original Assignee
Revolution Medicines 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 Revolution Medicines Inc filed Critical Revolution Medicines Inc
Publication of MX2020003579A publication Critical patent/MX2020003579A/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero 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
    • A61K31/435Heterocyclic 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
    • A61K31/495Heterocyclic 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presente descripción está dirigida a los inhibidores de SHP2 y a su uso en el tratamiento de enfermedades. También se describen composiciones farmacéuticas que los comprenden.
MX2020003579A 2017-10-12 2018-10-11 Compuestos de piridina, pirazina, y triazina como inhibidores de shp2 alostericos. MX2020003579A (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201762571760P 2017-10-12 2017-10-12
US201862615353P 2018-01-09 2018-01-09
US201862678889P 2018-05-31 2018-05-31
PCT/US2018/055502 WO2019075265A1 (en) 2017-10-12 2018-10-11 PYRIDINE, PYRAZINE AND TRIAZINE COMPOUNDS AS ALLOSTERIC INHIBITORS OF SHP2

Publications (1)

Publication Number Publication Date
MX2020003579A true MX2020003579A (es) 2020-07-22

Family

ID=64049755

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2020003579A MX2020003579A (es) 2017-10-12 2018-10-11 Compuestos de piridina, pirazina, y triazina como inhibidores de shp2 alostericos.

Country Status (16)

Country Link
US (2) US11702411B2 (es)
EP (1) EP3694848A1 (es)
JP (1) JP2020536881A (es)
KR (1) KR20200070295A (es)
CN (1) CN111212834B (es)
AU (1) AU2018347516A1 (es)
BR (1) BR112020007058A2 (es)
CA (1) CA3078565A1 (es)
CO (1) CO2020003714A2 (es)
IL (1) IL273756A (es)
MX (1) MX2020003579A (es)
PH (1) PH12020550216A1 (es)
RU (1) RU2020115095A (es)
SG (1) SG11202002941WA (es)
TW (1) TW201930292A (es)
WO (1) WO2019075265A1 (es)

Families Citing this family (72)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11466017B2 (en) 2011-03-10 2022-10-11 Board Of Regents, The University Of Texas System Heterocyclic inhibitors of PTPN11
JO3517B1 (ar) 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
JP7044375B2 (ja) 2016-05-31 2022-03-30 ボード オブ リージェンツ,ザ ユニバーシティ オブ テキサス システム Ptpn11の複素環式阻害剤
PT3464272T (pt) 2016-06-07 2022-03-11 Jacobio Pharmaceuticals Co Ltd Novos derivados heterocíclicos úteis como inibidores de shp2
MX383856B (es) 2016-06-14 2025-03-14 Novartis Ag Compuestos y composiciones para inhibir la actividad de shp2.
PH12019500056B1 (en) 2016-07-12 2024-01-31 Revolution Medicines Inc 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors
US11529347B2 (en) 2016-09-22 2022-12-20 Relay Therapeutics, Inc. SHP2 phosphatase inhibitors and methods of use thereof
TW202500565A (zh) 2016-10-24 2025-01-01 美商傳達治療有限公司 Shp2磷酸酶抑制劑及其使用方法
CA3051206A1 (en) 2017-01-23 2018-07-26 Revolution Medicines, Inc. Bicyclic compounds as allosteric shp2 inhibitors
KR20190110588A (ko) 2017-01-23 2019-09-30 레볼루션 메디슨즈, 인크. 알로스테릭 shp2 억제제로서의 피리딘 화합물
WO2018172984A1 (en) 2017-03-23 2018-09-27 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as shp2 inhibitors
EP3630770B1 (en) 2017-05-26 2024-08-28 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
GB2587457B (en) 2017-08-04 2022-06-01 Skyhawk Therapeutics Inc Methods and compositions for modulating splicing
WO2019051084A1 (en) 2017-09-07 2019-03-14 Revolution Medicines, Inc. SHP2 INHIBITOR COMPOSITIONS AND METHODS OF TREATING CANCER
EP3687997A1 (en) 2017-09-29 2020-08-05 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
MX2020003579A (es) 2017-10-12 2020-07-22 Revolution Medicines Inc Compuestos de piridina, pirazina, y triazina como inhibidores de shp2 alostericos.
TW201927791A (zh) 2017-12-15 2019-07-16 美商銳新醫藥公司 作為變構shp2抑制劑的多環化合物
TWI879728B (zh) 2018-03-21 2025-04-11 美商傳達治療有限公司 Shp2磷酸酶抑制劑及其使用方法
JP7265275B2 (ja) 2018-03-21 2023-04-26 スージョウ プーヘー バイオファーマ カンパニー リミテッド Shp2阻害剤およびその使用
WO2019183364A1 (en) 2018-03-21 2019-09-26 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine shp2 phosphatase inhibitors and methods of use thereof
KR102611661B1 (ko) 2018-05-02 2023-12-08 나비레 파르마, 인코퍼레이티드 Ptpn11의 치환된 헤테로사이클릭 억제제
US11104675B2 (en) 2018-08-10 2021-08-31 Navire Pharma, Inc. PTPN11 inhibitors
CA3113233A1 (en) 2018-09-18 2020-03-26 Nikang Therapeutics, Inc. Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors
WO2020063760A1 (en) 2018-09-26 2020-04-02 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as shp2 inhibitors
KR20210068472A (ko) * 2018-09-29 2021-06-09 노파르티스 아게 Shp2 활성의 억제를 위한 화합물 및 조성물의 제조
EP3860717A1 (en) 2018-10-03 2021-08-11 Gilead Sciences, Inc. Imidozopyrimidine derivatives
AU2019359885B2 (en) 2018-10-17 2024-01-18 Array Biopharma Inc. Protein tyrosine phosphatase inhibitors
CN111138412B (zh) 2018-11-06 2023-09-15 上海奕拓医药科技有限责任公司 一种螺芳环化合物及其应用
CN118812532A (zh) 2019-02-05 2024-10-22 斯基霍克疗法公司 用于调节剪接的方法和组合物
CN113677344A (zh) 2019-02-06 2021-11-19 斯基霍克疗法公司 用于调节剪接的方法和组合物
CN111647000B (zh) 2019-03-04 2021-10-12 勤浩医药(苏州)有限公司 吡嗪类衍生物及其在抑制shp2中的应用
KR102698608B1 (ko) 2019-04-02 2024-08-27 어레이 바이오파마 인크. 단백질 티로신 포스파타제 억제제
AR119731A1 (es) 2019-05-17 2022-01-05 Novartis Ag Inhibidores del inflamasoma nlrp3
US11129829B2 (en) 2019-06-17 2021-09-28 Skyhawk Therapeutics, Inc. Methods for modulating splicing
TWI817018B (zh) 2019-06-28 2023-10-01 美商艾瑞生藥股份有限公司 用於治療braf相關的疾病和失調症之化合物
CN112300160A (zh) * 2019-08-01 2021-02-02 上海奕拓医药科技有限责任公司 一种螺芳环化合物、其制备及应用
EP3772513A1 (en) 2019-08-09 2021-02-10 C.N.C.C.S. S.c.a.r.l. Collezione Nazionale Dei Composti Chimici e Centro Screening Shp2 inhibitors
WO2021043077A1 (zh) * 2019-09-06 2021-03-11 四川科伦博泰生物医药股份有限公司 一种取代吡嗪化合物、其制备方法和用途
CN114450287A (zh) 2019-09-24 2022-05-06 传达治疗有限公司 Shp2磷酸酶抑制剂及其制备和使用方法
TW202128650A (zh) * 2019-10-11 2021-08-01 德商拜耳動物保健有限公司 作為殺蟲劑之新穎的雜芳基取代之吡𠯤衍生物
CN112724145A (zh) * 2019-10-14 2021-04-30 杭州雷索药业有限公司 用于抑制shp2活性的吡嗪衍生物
EP4092019A4 (en) 2020-01-16 2024-02-28 Zhejiang Hisun Pharmaceutical Co., Ltd. HETEROARYL DERIVATIVE, PROCESS THEREOF AND USE THEREOF
CN114761394B (zh) * 2020-01-16 2024-03-29 浙江海正药业股份有限公司 吡啶或嘧啶类衍生物及其制备方法和用途
EP4110338A1 (en) 2020-02-28 2023-01-04 Novartis AG A triple pharmaceutical combination comprising dabrafenib, an erk inhibitor and a shp2 inhibitor
CN115667239A (zh) * 2020-06-22 2023-01-31 四川科伦博泰生物医药股份有限公司 取代吡嗪类化合物,包含其的药物组合物及其用途
WO2022007869A1 (zh) * 2020-07-10 2022-01-13 浙江海正药业股份有限公司 吡啶或嘧啶类衍生物及其制备方法和用途
WO2022083569A1 (en) 2020-10-20 2022-04-28 Amgen Inc. Heterocyclic spiro compounds and methods of use
MX2023004802A (es) 2020-10-27 2023-06-22 Amgen Inc Compuestos espiro heterocíclicos y métodos de uso.
CN116568308A (zh) * 2021-01-29 2023-08-08 四川科伦博泰生物医药股份有限公司 一类杂环类shp2抑制剂、其制备方法及用途
EP4039685A1 (en) 2021-02-08 2022-08-10 Irbm S.P.A. Azabicyclic shp2 inhibitors
TWI825637B (zh) 2021-03-31 2023-12-11 美商輝瑞股份有限公司 啶-1,6(2h,7h)-二酮
EP4067358A1 (en) 2021-04-02 2022-10-05 C.N.C.C.S. S.c.a.r.l. Collezione Nazionale Dei Composti Chimici e Centro Screening (s)-1-(5-((pyridin-3-yl)thio)pyrazin-2-yl)-4'h,6'h-spiro[piperidine-4,5'-pyrrolo[1,2-b]pyrazol]-4'-amine derivatives and similar compounds as shp2 inhibitors for the treatment of e.g. cancer
CA3217830A1 (en) 2021-04-29 2022-11-03 Amgen Inc. 2-aminobenzothiazole compounds and methods of use thereof
JP2024516037A (ja) 2021-05-05 2024-04-11 フヤバイオ インターナショナル,エルエルシー Shp2阻害剤とpd-1阻害剤とを含む併用療法
US20240270753A1 (en) * 2021-05-13 2024-08-15 Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences Heterocyclic compound for inhibiting shp2 activity, preparation method therefor and use thereof
TW202313041A (zh) 2021-06-09 2023-04-01 瑞士商諾華公司 包含達拉菲尼、曲美替尼和shp2抑制劑之三重藥物組合
AU2022289684A1 (en) 2021-06-09 2023-10-05 F. Hoffmann-La Roche Ag Combination of a particular braf inhibitor (paradox breaker) and a pd-1 axis binding antagonist for use in the treatment of cancer
EP4351577A1 (en) 2021-06-09 2024-04-17 F. Hoffmann-La Roche AG Combination therapy for cancer treatment
TW202317100A (zh) 2021-06-23 2023-05-01 瑞士商諾華公司 包含kras g12c抑制劑的藥物組合及其用於治療癌症之用途
CA3226206A1 (en) 2021-07-09 2023-01-12 Kanaph Therapeutics Inc. Shp2 inhibitor and use thereof
IL309086A (en) 2021-09-01 2024-02-01 Novartis Ag Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers
CN118201615A (zh) 2021-11-04 2024-06-14 豪夫迈·罗氏有限公司 喹唑啉酮化合物用于治疗癌症的新用途
WO2023122938A1 (en) * 2021-12-28 2023-07-06 Js Innomed Holdings Ltd. Heterocyclic compounds as shp2 inhibitors, compositions comprising the heterocyclic compound, and methods of use thereof
US20250179077A1 (en) 2022-02-16 2025-06-05 Amgen Inc. Quinazoline compounds and uses thereof as inhibitors of mutant kras proteins
JP2025508702A (ja) 2022-02-16 2025-04-10 アムジエン・インコーポレーテツド キナゾリン化合物、及び変異krasタンパク質の阻害剤としてのその使用
WO2023230205A1 (en) 2022-05-25 2023-11-30 Ikena Oncology, Inc. Mek inhibitors and uses thereof
CN119604508A (zh) * 2022-07-26 2025-03-11 首药控股(北京)股份有限公司 具有生物活性的杂环化合物
EP4345101A1 (en) 2022-09-29 2024-04-03 Irbm S.P.A. Azole derivatives as shp2 inhibitors
TW202440550A (zh) 2022-12-15 2024-10-16 瑞士商赫孚孟拉羅股份公司 用於癌症治療之組合療法
KR20240110741A (ko) * 2023-01-05 2024-07-16 주식회사 카나프테라퓨틱스 Shp2 억제제 및 이의 용도
WO2024218632A1 (en) 2023-04-17 2024-10-24 Array Biopharma Inc. Erk protein kinase inhibitors
WO2025081291A1 (en) * 2023-10-16 2025-04-24 Canwell Biotech Limited Benzo [c] [1, 2] oxaborol-1 (3h) -ol derivatives as shp2 inhibitors, compositions and methods thereof

Family Cites Families (129)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2572728A (en) 1949-01-07 1951-10-23 American Cyanamid Co Hydroxybenzenesulfonamidopyra-zines and preparation of same
US2636882A (en) 1950-08-11 1953-04-28 Quaker Oats Co Preparation of 3-pyridols from 2-acylfurans
BE758503A (fr) 1969-11-07 1971-05-05 Shell Int Research Compositions pesticides
GB1459571A (en) 1974-09-12 1976-12-22 Pfizer Ltd Thiophene-2-sulphonamide derivatives and their use as therapeutic agents sheet orienting apparatus
JPS5762269A (en) 1980-10-03 1982-04-15 Ogawa Koryo Kk 2,3,5-trisubstituted pyrazine derivative
US4513135A (en) 1982-03-05 1985-04-23 Eli Lilly And Company Diaryl-pyrazine derivatives affecting GABA binding
DE3242195A1 (de) 1982-11-15 1984-05-17 Basf Ag, 6700 Ludwigshafen Neue 2-aminopyrazine und verfahren zur herstellung von 2-aminopyrazinen und pyrazinen
JPH0249775A (ja) 1988-05-19 1990-02-20 Nippon Soda Co Ltd 6員環又は7員環を有する複素環化合物及びその製造方法
JPH04112877A (ja) 1990-09-04 1992-04-14 Nippon Soda Co Ltd 新規シアノピラジン誘導体及びその製造方法
WO1993009664A1 (fr) 1991-11-12 1993-05-27 Nippon Soda Co., Ltd. Materiau de conversion de la longueur d'onde de la lumiere, a usage dans l'agriculture
US5262564A (en) 1992-10-30 1993-11-16 Octamer, Inc. Sulfinic acid adducts of organo nitroso compounds useful as retroviral inactivating agents anti-retroviral agents and anti-tumor agents
GB9504854D0 (en) 1994-03-31 1995-04-26 Zeneca Ltd Nitrogen derivatives
ES2168237T3 (es) 1996-02-07 2007-04-01 Neurocrine Biosciences, Inc. Pirazolopirimidinas como antagonistas de receptores de crf.
EP1007042A4 (en) 1997-06-13 2001-07-04 Sugen Inc NEW HETEROCYCLIC COMPOUNDS FOR MODULATING THE PROTEIN-TYROSIN-ENZYME-RELATED CELLULAR SIGNAL TRANSDUCTION
IL148243A0 (en) 1999-08-27 2002-09-12 Sugen Inc Trifluoromethyl sulfonyl and trifluoromethyl sulfonamido compounds and pharmaceutical compositions containing the same
EP1255740B1 (en) 2000-02-16 2005-10-19 Neurogen Corporation Substituted arylpyrazines
EP1448587B1 (en) 2001-10-01 2009-09-02 Mount Sinai School of Medicine Noonan syndrome gene
US6921762B2 (en) 2001-11-16 2005-07-26 Amgen Inc. Substituted indolizine-like compounds and methods of use
EP1446387B1 (en) 2001-11-21 2009-11-04 Pharmacia & Upjohn Company LLC Substituted aryl 1,4-pyrazine derivatives
EP1492784A4 (en) 2002-03-28 2006-03-29 Merck & Co Inc SUBSTITUTED 2,3-DIPHENYLPYRIDINES
MXPA05002418A (es) 2002-09-12 2005-05-27 Pharmacia & Upjohn Co Llc Derivados de 1,4-pirazina sustituidos.
EP1576014B1 (en) 2002-12-23 2011-06-29 Wyeth LLC Antibodies against pd-1 and uses thereof
US7157460B2 (en) 2003-02-20 2007-01-02 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
CA2524519A1 (en) 2003-05-09 2004-11-18 Pharmacia & Upjohn Company Llc Compounds as crf1 receptor antagonists
GB0314057D0 (en) 2003-06-18 2003-07-23 Astrazeneca Ab Therapeutic agents
FR2856684B1 (fr) 2003-06-26 2008-04-11 Sanofi Synthelabo Derives de diphenylpyridine, leur preparation et leur application en therapeutique
CA2537916A1 (en) 2003-09-03 2005-03-31 Neurogen Corporation 5-aryl-pyrazolo[4,3-d]pyrimidines, pyridines, and pyrazines and related compounds
JP2007508290A (ja) 2003-10-10 2007-04-05 ファイザー・プロダクツ・インク GSK−3阻害剤としての置換2H−[1,2,4]トリアゾロ[4,3−a]ピラジン
EP1678160A1 (en) 2003-10-27 2006-07-12 Astellas Pharma Inc. Pyrazine derivatives and pharmaceutical use thereof
DE102004015954A1 (de) 2004-04-01 2005-11-10 Ina-Schaeffler Kg Umschlingungstrieb
CN1938296A (zh) 2004-04-01 2007-03-28 安斯泰来制药有限公司 作为腺苷拮抗剂的吡嗪衍生物及其制药用途
WO2006002284A1 (en) 2004-06-22 2006-01-05 Rigel Pharmaceuticals, Inc. Ubiquitin ligase inhibitors
CN101087767A (zh) 2004-12-23 2007-12-12 马林克罗特公司 荧光吡嗪衍生物及其在评估肾功能中的使用方法
CA2598456A1 (en) * 2005-02-16 2006-08-24 Schering Corporation Heterocyclic substituted piperazines with cxcr3 antagonist activity
AR053712A1 (es) 2005-04-18 2007-05-16 Neurogen Corp Heteroarilos sustituidos, antagonistas de cb1 (receptor 1 canabinoide)
KR101125919B1 (ko) 2005-06-22 2012-06-12 플렉시콘, 인코퍼레이티드 단백질 키나제 억제제로서의 피롤로[2,3-b]피리딘 유도체
EP3061834B1 (en) 2005-10-21 2020-01-08 The Regents of the University of California Shp-2 gene mutations in melanoma
CA2616147A1 (en) 2006-02-24 2007-09-20 Mallinckrodt Inc. Process for using optical agents
JP2007277097A (ja) 2006-04-03 2007-10-25 Mie Univ 発光化合物、発光方法、及びその製造方法
WO2007117699A2 (en) 2006-04-07 2007-10-18 University Of South Florida Inhibition of shp2/ptpn11 protein tyrosine phosphatase by nsc-87877, nsc-117199 and their analogs
WO2007127375A2 (en) * 2006-04-28 2007-11-08 Northwestern University Formulations containing pyridazine compounds for treating neuroinflammatory diseases
US7893058B2 (en) 2006-05-15 2011-02-22 Janssen Pharmaceutica Nv Imidazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases
ATE465164T1 (de) 2006-05-31 2010-05-15 Galapagos Nv Triazolopyrazinverbindungen zur behandlung von degenerations- und entzündungskrankheiten
CA2654202A1 (en) 2006-06-06 2007-12-21 Schering Corporation Imidazopyrazines as protein kinase inhibitors
CN101687040A (zh) 2007-03-01 2010-03-31 马林克罗特公司 整合光活性的小分子及其用途
US20120142685A1 (en) 2007-04-06 2012-06-07 Markus Rolf Dobler Organic compounds
WO2008138843A1 (en) 2007-05-10 2008-11-20 Galapagos N.V. Imidazopyridines and triazolopyrimidines useful for the treatment of joint degenerative & inflammatory diseases
WO2008138842A1 (en) 2007-05-10 2008-11-20 Galapagos N.V. Imidazopyrazines and triazolopyrazine for the treatment of joint degenerative and inflammatory diseases
US20100190980A1 (en) 2007-06-21 2010-07-29 Taisho Pharmaceutical Co., Ltd Pyrazinamide compound
CA2695365A1 (en) * 2007-08-03 2009-02-12 Schering Corporation Method of treating cxcr3 mediated diseases using heterocyclic substituted piperazines
CA2695621A1 (en) 2007-08-09 2009-02-12 Merck Sharp & Dohme Corp. Pyridine carboxamide orexin receptor antagonists
WO2009025823A1 (en) * 2007-08-21 2009-02-26 Amgen Inc. Phosphodiesterase 10 inhibitors
WO2010011666A2 (en) 2008-07-21 2010-01-28 University Of South Florida Indoline scaffold shp-2 inhibitors and cancer treatment method
WO2010051238A1 (en) 2008-10-30 2010-05-06 Merck Sharp & Dohme Corp. Pyridazine carboxamide orexin receptor antagonists
SG2014005318A (en) 2009-01-23 2014-03-28 Rigel Pharmaceuticals Inc Compositions and methods for inhibition of the jak pathway
WO2010121212A2 (en) 2009-04-17 2010-10-21 H. Lee Moffit Cancer Center And Research Institute, Inc. Indoline scaffold shp-2 inhibitors and method of treating cancer
EP2438041A4 (en) * 2009-06-01 2012-11-21 Merck Sharp & Dohme PYRAZINE-carboxamide-orexin receptor Antagonist
CA2771190C (en) 2009-08-17 2020-01-21 Memorial Sloan-Kettering Cancer Center Heat shock protein binding compounds, compositions, and methods for making and using same
AU2010291835A1 (en) 2009-09-03 2012-04-19 Vancouver Biotech Ltd. Monoclonal antibodies against gonadotropin-releasing hormone receptor
US8673913B2 (en) 2009-11-13 2014-03-18 Case Western Reserve University SHP-2 phosphatase inhibitor
CN102918061B (zh) 2010-03-05 2016-06-08 霍夫曼-拉罗奇有限公司 针对人csf-1r的抗体及其用途
TW201200518A (en) * 2010-03-10 2012-01-01 Kalypsys Inc Heterocyclic inhibitors of histamine receptors for the treatment of disease
TW201202251A (en) * 2010-05-11 2012-01-16 Sanofi Aventis Substituted N-heteroaryl spirolactam bipyrrolidines, preparation and therapeutic use thereof
US8703768B2 (en) 2010-06-09 2014-04-22 Hoffmann-La Roche Inc. Nitrogen containing heteroaryl compounds
DK2593452T3 (en) 2010-07-14 2017-04-24 Novartis Ag Heterocyclic compounds as IP receptor agonists
GB201106829D0 (en) 2011-04-21 2011-06-01 Proximagen Ltd Heterocyclic compounds
EP2678016B1 (en) 2011-02-23 2016-08-10 Intellikine, LLC Heterocyclic compounds and uses thereof
WO2012149280A2 (en) 2011-04-29 2012-11-01 Abbott Laboratories Novel tricyclic compounds
CN103181918B (zh) 2011-05-04 2014-10-29 厦门大学 脂肪酸类化合物在制备预防和治疗肝癌药物中的应用
WO2013105063A1 (en) 2012-01-13 2013-07-18 Novartis Ag Fused piperidines as ip receptor agonists for the treatment of pulmonary arterial hypertension (pah) and related disorders
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
US20150291625A1 (en) 2012-11-08 2015-10-15 Pfizer Inc. Heteroaromatic Compounds and their Use as Dopamine D1 Ligands
WO2014085490A1 (en) 2012-11-29 2014-06-05 Chemocentryx, Inc. Cxcr7 antagonists
WO2014113584A1 (en) 2013-01-16 2014-07-24 Rhode Island Hospital Compositions and methods for the prevention and treatment of osteolysis and osteoporosis
AU2014214326B2 (en) 2013-02-07 2018-07-05 Prexton Therapeutics Sa Substituted quinoxaline derivatives and their use as positive allosteric modulators of mGluR4
PL2958943T3 (pl) 2013-02-20 2020-04-30 The Trustees Of The University Of Pennsylvania Leczenie nowotworu złośliwego za pomocą humanizowanego chimerycznego receptora antygenowego anty-egfrviii
SG10201707855YA (en) 2013-03-13 2017-10-30 Prothena Biosciences Ltd Tau immunotherapy
CN103554038B (zh) 2013-06-19 2015-10-14 云南大学 多卤代苯腈喹唑啉酮化合物及其制备方法和用途
US9815813B2 (en) * 2014-01-17 2017-11-14 Novartis Ag 1-(triazin-3-yl/pyridazin-3-yl)-piper(-azine)idine derivatives and compositions therefor for inhibiting the activity of SHP2
EP3094627B1 (en) * 2014-01-17 2018-08-22 Novartis AG 1-pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and and compositions thereof for inhibiting the activity of shp2
JO3517B1 (ar) 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
WO2015164862A1 (en) 2014-04-25 2015-10-29 Memorial Sloan-Kettering Cancer Center Treatment of h-ras-driven tumors
TWI687419B (zh) 2014-07-10 2020-03-11 美商英塞特公司 作為lsd1抑制劑之咪唑并吡啶及咪唑并吡嗪
MA40551A (fr) * 2014-08-01 2021-04-07 Nuevolution As Composés actifs envers des bromodomaines
MX381180B (es) 2014-11-18 2025-03-12 Merck Sharp & Dohme Compuestos aminopirazina con propiedades antagonistas a2a.
US20170362305A1 (en) 2014-12-17 2017-12-21 Siemens Healthcare Diagnostics Inc. Sandwich assay design for small molecules
UY36462A (es) 2014-12-23 2016-07-29 Novartis Ag Compuestos de triazolopirimidina y usos de los mismos
EP4289950A3 (en) 2015-01-09 2024-01-24 Revolution Medicines, Inc. Macrocyclic compounds that participate in cooperative binding and medical uses thereof
AU2016213972B2 (en) 2015-02-05 2020-07-09 Tyrnovo Ltd. Combinations of IRS/Stat3 dual modulators and anti-cancer agents for treating cancer
UA122688C2 (uk) 2015-04-03 2020-12-28 Інсайт Корпорейшн Гетероциклічні сполуки як інгібітори lsd1
CN107787323B (zh) 2015-06-19 2020-09-01 诺华股份有限公司 用于抑制shp2活性的化合物和组合物
CN107922388B (zh) * 2015-06-19 2020-12-29 诺华股份有限公司 用于抑制shp2活性的化合物和组合物
ES2741746T3 (es) 2015-06-19 2020-02-12 Novartis Ag Compuestos y composiciones para inhibir la actividad de SHP2
US10426842B2 (en) 2015-07-15 2019-10-01 The Curators Of The University Of Missouri Targeted nanoparticle conjugate and method for co-delivery of siRNA and drug
EP3355930A4 (en) 2015-10-01 2019-03-06 Warp Drive Bio, Inc. METHOD AND REAGENTS FOR THE ANALYSIS OF PROTEIN-PROTEIN INTERFACES
WO2017156397A1 (en) 2016-03-11 2017-09-14 Board Of Regents, The University Of Texas Sysytem Heterocyclic inhibitors of ptpn11
GB201604969D0 (en) * 2016-03-23 2016-05-04 Syngenta Participations Ag Improvements in or relating to organic compounds
GB201604970D0 (en) * 2016-03-23 2016-05-04 Syngenta Participations Ag Improvements in or relating to organic compounds
PT3464272T (pt) 2016-06-07 2022-03-11 Jacobio Pharmaceuticals Co Ltd Novos derivados heterocíclicos úteis como inibidores de shp2
MX383856B (es) * 2016-06-14 2025-03-14 Novartis Ag Compuestos y composiciones para inhibir la actividad de shp2.
PH12019500056B1 (en) 2016-07-12 2024-01-31 Revolution Medicines Inc 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors
US11529347B2 (en) 2016-09-22 2022-12-20 Relay Therapeutics, Inc. SHP2 phosphatase inhibitors and methods of use thereof
TW202500565A (zh) 2016-10-24 2025-01-01 美商傳達治療有限公司 Shp2磷酸酶抑制劑及其使用方法
CN110730678B (zh) * 2017-01-10 2022-07-15 诺华股份有限公司 包含alk抑制剂和shp2抑制剂的药物组合
CA3051206A1 (en) 2017-01-23 2018-07-26 Revolution Medicines, Inc. Bicyclic compounds as allosteric shp2 inhibitors
KR20190110588A (ko) 2017-01-23 2019-09-30 레볼루션 메디슨즈, 인크. 알로스테릭 shp2 억제제로서의 피리딘 화합물
WO2018172984A1 (en) 2017-03-23 2018-09-27 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as shp2 inhibitors
US20210285955A1 (en) 2017-04-05 2021-09-16 Revolution Medicines, Inc. Methods and reagents for analyzing protein-protein interfaces
JP2020513036A (ja) 2017-04-05 2020-04-30 レボリューション メディシンズ インコーポレイテッドRevolution Medicines,Inc. 協同的結合に関与する化合物及びその使用
EP3630770B1 (en) 2017-05-26 2024-08-28 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
WO2019051084A1 (en) 2017-09-07 2019-03-14 Revolution Medicines, Inc. SHP2 INHIBITOR COMPOSITIONS AND METHODS OF TREATING CANCER
MX2020003579A (es) 2017-10-12 2020-07-22 Revolution Medicines Inc Compuestos de piridina, pirazina, y triazina como inhibidores de shp2 alostericos.
TW201927791A (zh) 2017-12-15 2019-07-16 美商銳新醫藥公司 作為變構shp2抑制劑的多環化合物
CN115448923B (zh) 2018-02-13 2024-03-22 上海青煜医药科技有限公司 嘧啶并环化合物及其制备方法和应用
JP7335882B2 (ja) 2018-02-13 2023-08-30 ブルーレイ セラピューティクス (シャンハイ) カンパニー,リミティド ピリミジン縮合環式化合物及びその製造方法、並びに使用
JP7265275B2 (ja) * 2018-03-21 2023-04-26 スージョウ プーヘー バイオファーマ カンパニー リミテッド Shp2阻害剤およびその使用
CA3096535A1 (en) 2018-04-10 2019-10-17 Revolution Medicines, Inc. Shp2 inhibitor compositions, methods for treating cancer and methods for identifying a subject with shp2 mutations
RS64272B1 (sr) 2018-05-01 2023-07-31 Revolution Medicines Inc C40-, c28- i c-32-vezani analozi rapamicina kao inhibitori mtor
CN112368289B (zh) 2018-05-01 2024-02-20 锐新医药公司 作为mtor抑制剂的c26-连接的雷帕霉素类似物
AU2019338207B2 (en) 2018-09-10 2025-01-02 Mirati Therapeutics, Inc. Combination therapies
CA3113233A1 (en) * 2018-09-18 2020-03-26 Nikang Therapeutics, Inc. Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors
EP3860717A1 (en) 2018-10-03 2021-08-11 Gilead Sciences, Inc. Imidozopyrimidine derivatives
JP2022508651A (ja) 2018-10-08 2022-01-19 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 癌を処置するためのshp2阻害剤組成物および方法
KR20210089716A (ko) 2018-11-07 2021-07-16 상하이 린진 바이오파마 씨오., 엘티디. 질소 함유 축합 헤테로고리 shp2억제제 화합물, 제조방법 및 용도
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
US20220073521A1 (en) 2018-11-30 2022-03-10 Tuojie Biotech (Shanghai) Co., Ltd. Pyrimidine and five-membered nitrogen heterocycle derivative, preparation method therefor, and medical uses thereof
KR20210097144A (ko) 2018-11-30 2021-08-06 투오지에 바이오텍 (상하이) 컴퍼니 리미티드 피리미딘 및 5-원 질소 헤테로사이클 유도체, 이의 제조 방법, 및 이의 의학적 용도
BR112021012057A2 (pt) 2018-12-21 2021-10-19 Revolution Medicines, Inc. Compostos que participam de ligação cooperativa e usos dos mesmos
CN114901366A (zh) 2019-11-04 2022-08-12 锐新医药公司 Ras抑制剂

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