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SG11202002941WA - Pyridine, pyrazine, and triazine compounds as allosteric shp2 inhibitors - Google Patents

Pyridine, pyrazine, and triazine compounds as allosteric shp2 inhibitors

Info

Publication number
SG11202002941WA
SG11202002941WA SG11202002941WA SG11202002941WA SG11202002941WA SG 11202002941W A SG11202002941W A SG 11202002941WA SG 11202002941W A SG11202002941W A SG 11202002941WA SG 11202002941W A SG11202002941W A SG 11202002941WA SG 11202002941W A SG11202002941W A SG 11202002941WA
Authority
SG
Singapore
Prior art keywords
pyrazine
pyridine
triazine compounds
shp2 inhibitors
allosteric shp2
Prior art date
Application number
SG11202002941WA
Inventor
Jie Jack Li
Elena S Koltun
Adrian Liam Gill
Andreas Buckl
Walter Won
Naing Aay
Kevin Mellem
Christos Tzitzilonis
Ashutosh Jogalekar
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 SG11202002941WA publication Critical patent/SG11202002941WA/en

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
    • C07D401/02Heterocyclic 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
    • 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
    • C07D401/14Heterocyclic 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
    • 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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (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)
SG11202002941WA 2017-10-12 2018-10-11 Pyridine, pyrazine, and triazine compounds as allosteric shp2 inhibitors SG11202002941WA (en)

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 shp2 inhibitors

Publications (1)

Publication Number Publication Date
SG11202002941WA true SG11202002941WA (en) 2020-04-29

Family

ID=64049755

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11202002941WA SG11202002941WA (en) 2017-10-12 2018-10-11 Pyridine, pyrazine, and triazine compounds as allosteric shp2 inhibitors

Country Status (16)

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

Families Citing this family (66)

* 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 (en) 2014-01-17 2020-07-05 Novartis Ag N-azaspirocycloalkane substituted n-heteroaryl compounds and compositions for inhibiting the activity of shp2
CN109475531B (en) 2016-05-31 2021-08-17 得克萨斯州立大学董事会 Heterocyclic inhibitors of PTPN11
EA202092442A3 (en) 2016-06-07 2021-08-31 Джакобио Фармасьютикалс Ко., Лтд. NEW HETEROCYCLIC DERIVATIVES USED AS SHP2 INHIBITORS
KR102457146B1 (en) 2016-06-14 2022-10-19 노파르티스 아게 Compounds and compositions for inhibiting the activity of SHP2
CR20190063A (en) 2016-07-12 2019-05-27 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
TWI848901B (en) 2016-10-24 2024-07-21 美商傳達治療有限公司 Shp2 phosphatase inhibitors and methods of use thereof
TWI820013B (en) 2017-01-23 2023-11-01 美商銳新醫藥公司 Bicyclic compounds as allosteric shp2 inhibitors
CA3051054A1 (en) 2017-01-23 2018-07-26 Revolution Medicines, Inc. Pyridine compounds as allosteric shp2 inhibitors
MA49013A (en) 2017-03-23 2021-05-05 Jacobio Pharmaceuticals Co Ltd NEW 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
MX2020001425A (en) 2017-08-04 2020-08-06 Skyhawk Therapeutics Inc Methods and compositions for modulating splicing.
BR112020004246A2 (en) 2017-09-07 2020-09-01 Revolution Medicines, Inc. shp2 inhibitory compositions and methods for the treatment of cancer
US11701354B2 (en) 2017-09-29 2023-07-18 D. E. Shaw Research, Llc Pyrazolo[3,4-b]pyrazine derivatives as SHP2 phosphatase inhibitors
TW201930292A (en) 2017-10-12 2019-08-01 美商銳新醫藥公司 Pyridine, pyrazine, and triazine compounds as allosteric SHP2 inhibitors
MX2020006273A (en) 2017-12-15 2020-09-14 Revolution Medicines Inc Polycyclic compounds as allosteric shp2 inhibitors.
CN112368272B (en) 2018-03-21 2023-04-21 苏州浦合医药科技有限公司 SHP2 inhibitors and uses thereof
CN112166110B (en) 2018-03-21 2023-08-11 传达治疗有限公司 SHP2 phosphatase inhibitors and methods of use thereof
EP3787627A4 (en) 2018-05-02 2021-12-01 Navire Pharma, Inc. Substituted heterocyclic inhibitors of ptpn11
SG11202100199UA (en) 2018-08-10 2021-02-25 Navire Pharma Inc 6-(4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl)-3-(2,3-dichlorophenyl)-2-methylpyrimidin-4(3h)-one derivatives and related compounds as ptpn11 (shp2) inhibitors for treating cancer
CA3113234A1 (en) 2018-09-18 2020-03-26 Nikang Therapeutics, Inc. Tri-substituted heteroaryl derivatives as src homology-2 phosphatase inhibitors
MX2021003460A (en) 2018-09-29 2021-06-18 Novartis Ag Manufacture of compounds and compositions for inhibiting the activity of shp2.
EP3860717A1 (en) 2018-10-03 2021-08-11 Gilead Sciences, Inc. Imidozopyrimidine derivatives
CN111138412B (en) 2018-11-06 2023-09-15 上海奕拓医药科技有限责任公司 Spiro aromatic ring compound and application thereof
KR20210135241A (en) 2019-02-05 2021-11-12 스카이호크 테라퓨틱스, 인코포레이티드 Methods and compositions for controlling splicing
KR20210135507A (en) 2019-02-06 2021-11-15 스카이호크 테라퓨틱스, 인코포레이티드 Methods and compositions for controlling splicing
CN111647000B (en) 2019-03-04 2021-10-12 勤浩医药(苏州)有限公司 Pyrazine derivative and application thereof in inhibition of SHP2
KR102698608B1 (en) 2019-04-02 2024-08-27 어레이 바이오파마 인크. protein tyrosine phosphatase inhibitor
AR119731A1 (en) 2019-05-17 2022-01-05 Novartis Ag NLRP3 INFLAMASOME INHIBITORS
US11129829B2 (en) 2019-06-17 2021-09-28 Skyhawk Therapeutics, Inc. Methods for modulating splicing
TWI817018B (en) 2019-06-28 2023-10-01 美商艾瑞生藥股份有限公司 Compounds for the treatment of braf-associated diseases and disorders
CN112300160A (en) * 2019-08-01 2021-02-02 上海奕拓医药科技有限责任公司 Spiro aromatic ring compound, preparation and application thereof
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
CN114127053B (en) * 2019-09-06 2023-06-13 四川科伦博泰生物医药股份有限公司 Substituted pyrazine compound, preparation method and application thereof
EP4034539A1 (en) 2019-09-24 2022-08-03 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of making and using the same
CN112724145A (en) * 2019-10-14 2021-04-30 杭州雷索药业有限公司 Pyrazine derivatives for inhibiting SHP2 activity
WO2021143680A1 (en) 2020-01-16 2021-07-22 浙江海正药业股份有限公司 Heteroaryl derivative, preparation method therefor, and use thereof
CN114761394B (en) * 2020-01-16 2024-03-29 浙江海正药业股份有限公司 Pyridine or pyrimidine derivative and preparation method and application thereof
KR20220148847A (en) 2020-02-28 2022-11-07 노파르티스 아게 Triple Pharmaceutical Combination Comprising Dabrafenib, ERK Inhibitor, and SHP2 Inhibitor
US20230212180A1 (en) * 2020-06-22 2023-07-06 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. Substituted pyrazine compound, pharmaceutical composition comprising same, and use thereof
CN115916765A (en) * 2020-07-10 2023-04-04 浙江海正药业股份有限公司 Pyridine or pyrimidine derivative and preparation method and application thereof
MX2023004802A (en) 2020-10-27 2023-06-22 Amgen Inc Heterocyclic spiro compounds and methods of use.
CN116568308A (en) * 2021-01-29 2023-08-08 四川科伦博泰生物医药股份有限公司 Heterocyclic SHP2 inhibitor, preparation method and application thereof
EP4039685A1 (en) 2021-02-08 2022-08-10 Irbm S.P.A. Azabicyclic shp2 inhibitors
TWI825637B (en) 2021-03-31 2023-12-11 美商輝瑞股份有限公司 3,4-dihydro-2,7-naphthyridine-1,6(2h,7h)-diones as mek inhibitors
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
CN117651700A (en) 2021-04-29 2024-03-05 安进公司 2-aminobenzothiazole compounds and methods of use
JP2024516037A (en) 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 Combination therapy comprising an SHP2 inhibitor and a PD-1 inhibitor
KR20240007279A (en) * 2021-05-13 2024-01-16 상하이 인스티튜트 오브 마테리아 메디카 차이니즈 아카데미 오브 싸이언시즈 Heterocyclic compounds that inhibit SHP2 activity, methods for producing and uses thereof
TW202313041A (en) 2021-06-09 2023-04-01 瑞士商諾華公司 A triple pharmaceutical combination comprising dabrafenib, trametinib and a shp2 inhibitor.
BR112023025916A2 (en) 2021-06-09 2024-02-27 Chugai Pharmaceutical Co Ltd COMBINATION OF A BRAF INHIBITOR AND A MEK INHIBITOR, USE OF A COMBINATION, METHOD FOR THE TREATMENT OR PROPHYLAXIS OF CANCER, PHARMACEUTICAL COMPOSITIONS AND INVENTION
BR112023025738A2 (en) 2021-06-09 2024-02-27 Hoffmann La Roche COMBINATION OF A BRAF INHIBITOR AND A PD-1 AXIS BINDING ANTAGONIST, USE OF A COMBINATION OF A BRAF INHIBITOR AND A PD-1 AXIS BINDING ANTAGONIST, METHOD FOR THE TREATMENT OR PROPHYLAXIS OF CANCER, PHARMACEUTICAL COMPOSITION AND INVENTION
TW202317100A (en) 2021-06-23 2023-05-01 瑞士商諾華公司 Pharmaceutical combinations comprising a kras g12c inhibitor and uses thereof for the treatment of cancers
MX2024000271A (en) 2021-07-09 2024-01-31 Kanaph Therapeutics Inc Shp2 inhibitor and use thereof.
JP2024532374A (en) 2021-09-01 2024-09-05 ノバルティス アーゲー Pharmaceutical combinations containing TEAD inhibitors and their use for the treatment of cancer - Patents.com
EP4426305A1 (en) 2021-11-04 2024-09-11 F. Hoffmann-La Roche AG Novel use of quinazolinone compound for the treatment of cancer
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
CN118715215A (en) 2022-02-16 2024-09-27 美国安进公司 Quinazoline compounds as inhibitors of mutant KRAS proteins and uses thereof
MX2024010045A (en) 2022-02-16 2024-08-26 Amgen Inc Quinazoline compounds and use thereof as inhibtors of mutant kras proteins.
US11878958B2 (en) 2022-05-25 2024-01-23 Ikena Oncology, Inc. MEK inhibitors and uses thereof
WO2024022244A1 (en) * 2022-07-26 2024-02-01 首药控股(北京)股份有限公司 Heterocyclic compound having biological activity
EP4345101A1 (en) 2022-09-29 2024-04-03 Irbm S.P.A. Azole derivatives as shp2 inhibitors
WO2024126660A1 (en) 2022-12-15 2024-06-20 F. Hoffmann-La Roche Ag Combination therapy for cancer treatment
KR20240110741A (en) * 2023-01-05 2024-07-16 주식회사 카나프테라퓨틱스 Shp2 inhibitors and use thereof
WO2024218632A1 (en) 2023-04-17 2024-10-24 Array Biopharma Inc. Erk protein kinase inhibitors

Family Cites Families (127)

* 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 (en) 1969-11-07 1971-05-05 Shell Int Research PESTICIDE COMPOSITIONS
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 (en) 1982-11-15 1984-05-17 Basf Ag, 6700 Ludwigshafen NEW 2-AMINOPYRAZINE AND METHOD FOR PRODUCING 2-AMINOPYRAZINE AND PYRAZINE
JPH0249775A (en) 1988-05-19 1990-02-20 Nippon Soda Co Ltd Heterocyclic compound having 6-membered or 7-membered ring and production thereof
JPH04112877A (en) 1990-09-04 1992-04-14 Nippon Soda Co Ltd New cyanopyrazine derivative and production thereof
WO1993009664A1 (en) 1991-11-12 1993-05-27 Nippon Soda Co., Ltd. Wavelength conversion material for 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
EE04282B1 (en) 1996-02-07 2004-04-15 Janssen Pharmaceutica N.V. Pyrazole Pyrimidines, Their Preparation and Use as a Pharmaceutical, and Composition Containing Them
JP2002512628A (en) 1997-06-13 2002-04-23 スージェン・インコーポレーテッド Novel heteroaryl compounds for regulating protein tyrosine enzyme-related cell signaling
AU775625B2 (en) 1999-08-27 2004-08-05 Sugen, Inc. Phosphate mimics and methods of treatment using phosphatase inhibitors
CZ20022739A3 (en) 2000-02-16 2003-02-12 Neurogen Corporation Substituted arylpyrazines
CA2495529C (en) 2001-10-01 2009-05-19 Mount Sinai School Of Medicine Of New York University Noonan syndrome gene
US6921762B2 (en) 2001-11-16 2005-07-26 Amgen Inc. Substituted indolizine-like compounds and methods of use
AU2002343557A1 (en) 2001-11-21 2003-06-10 Pharmacia And Upjohn Company Substituted aryl 1,4-pyrazine derivatives
EP1492784A4 (en) 2002-03-28 2006-03-29 Merck & Co Inc Substituted 2,3-diphenyl pyridines
US20040116444A1 (en) 2002-09-12 2004-06-17 Corbett Jeffrey W. Substituted 1,4-pyrazine derivatives
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
WO2004099201A1 (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 (en) 2003-06-26 2008-04-11 Sanofi Synthelabo DIPHENYLPYRIDINE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
US20050070542A1 (en) 2003-09-03 2005-03-31 Hodgetts Kevin J. 5-Aryl-pyrazolo[4,3-d]pyrimidines, pyridines, and pyrazines and related compounds
ES2288270T3 (en) 2003-10-10 2008-01-01 Pfizer Products Incorporated 2H- (1,2,4) TRIAZOLO (4,3-A) REPLACED PIRAZINS AS INHIBITORS OF GSK-3.
RU2006118325A (en) 2003-10-27 2007-12-10 Астеллас Фарма Инк. (Jp) Pyrazine Derivatives and Their Pharmaceutical Use
DE102004015954A1 (en) 2004-04-01 2005-11-10 Ina-Schaeffler Kg belt drive
CA2562126A1 (en) 2004-04-01 2005-10-13 Astellas Pharma Inc. Pyrazine derivatives and pharmaceutical use thereof
JP2008503591A (en) 2004-06-22 2008-02-07 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 Ubiquitin ligase inhibitor
WO2006071759A2 (en) 2004-12-23 2006-07-06 Mallinckrodt Inc. Fluorescent pyrazine derivatives and methods of using the same in assessing renal function
EP1871762A2 (en) 2005-04-18 2008-01-02 Neurogen Corporation Subtituted heteroaryl cb1 antagonists
AU2006261993B2 (en) 2005-06-22 2011-11-17 Plexxikon, Inc. Pyrrolo (2, 3-B) pyridine derivatives as protein kinase inhibitors
JP5671206B2 (en) 2005-10-21 2015-02-18 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア Mutation of c-KIT oncogene in melanoma
CA2616147A1 (en) 2006-02-24 2007-09-20 Mallinckrodt Inc. Process for using optical agents
JP2007277097A (en) 2006-04-03 2007-10-25 Mie Univ Luminous compound, method for emitting light, and method for producing luminous compound
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
AU2007243280A1 (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
DE602007006010D1 (en) 2006-05-31 2010-06-02 Galapagos Nv TRIAZOLOPYRAZIN COMPOUNDS FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES
JP2009539840A (en) 2006-06-06 2009-11-19 シェーリング コーポレイション Imidazopyrazine as a protein kinase inhibitor
US8313729B2 (en) 2007-03-01 2012-11-20 Medibeacon, LLC Integrated photoactive small molecules and uses thereof
EP2144909B1 (en) 2007-04-06 2011-03-23 Novartis AG [2,6]naphthyridines useful as protein kinase inhibitors
US8148369B2 (en) 2007-05-10 2012-04-03 Janssen Pharmaceutica Nv Fused pyrazine compounds useful for the treatment of degenerative and inflammatory diseases
WO2008138843A1 (en) 2007-05-10 2008-11-20 Galapagos N.V. Imidazopyridines and triazolopyrimidines useful for the treatment of joint degenerative & inflammatory diseases
JPWO2008156174A1 (en) 2007-06-21 2010-08-26 大正製薬株式会社 Pyrazineamide compound
WO2009020642A1 (en) 2007-08-09 2009-02-12 Merck & Co., Inc. Pyridine carboxamide orexin receptor antagonists
WO2009025823A1 (en) * 2007-08-21 2009-02-26 Amgen Inc. Phosphodiesterase 10 inhibitors
US9174969B2 (en) 2008-07-21 2015-11-03 University Of South Florida Indoline scaffold SHP-2 inhibitors and cancer treatment method
AU2009308982A1 (en) 2008-10-30 2010-05-06 Merck Sharp & Dohme Corp. Pyridazine carboxamide orexin receptor antagonists
US8324200B2 (en) 2009-01-23 2012-12-04 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
WO2010141275A1 (en) * 2009-06-01 2010-12-09 Merck Sharp & Dohme Corp. Pyrazine carboxamide orexin receptor antagonists
JP2013502424A (en) 2009-08-17 2013-01-24 メモリアル スローン−ケタリング キャンサー センター Heat shock protein binding compounds, compositions, and methods for making them
WO2011026242A1 (en) 2009-09-03 2011-03-10 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
WO2011131407A1 (en) 2010-03-05 2011-10-27 F. Hoffmann-La Roche Ag Antibodies against human csf-1r and uses thereof
TW201200518A (en) 2010-03-10 2012-01-01 Kalypsys Inc Heterocyclic inhibitors of histamine receptors for the treatment of disease
JP5833105B2 (en) * 2010-05-11 2015-12-16 サノフイ Substituted N-heteroaryl spirolactam bipyrrolidines, their preparation and therapeutic use
US8703768B2 (en) 2010-06-09 2014-04-22 Hoffmann-La Roche Inc. Nitrogen containing heteroaryl compounds
CA2804744C (en) 2010-07-14 2019-05-28 Novartis Ag Ip receptor agonist 1,8-naphthyridinyl and 7,8-dihydropyrido[3,2-b]pyrazinyl heterocyclic compounds
GB201106829D0 (en) 2011-04-21 2011-06-01 Proximagen Ltd Heterocyclic compounds
WO2012116237A2 (en) 2011-02-23 2012-08-30 Intellikine, Llc Heterocyclic compounds and uses thereof
WO2012149280A2 (en) 2011-04-29 2012-11-01 Abbott Laboratories Novel tricyclic compounds
CN103181918B (en) 2011-05-04 2014-10-29 厦门大学 Application of fatty acid compound in preparation of medicines for preventing and treating liver cancer
EP2802583A1 (en) 2012-01-13 2014-11-19 Novartis AG Fused piperidines as ip receptor agonists for the treatment of pulmonary arterial hypertension (pah) and related disorders
WO2014023385A1 (en) 2012-08-07 2014-02-13 Merck Patent Gmbh Pyridopyrimidine derivatives as protein kinase inhibitors
MX2015005812A (en) 2012-11-08 2015-09-23 Pfizer Heteroaromatic compounds and their use as dopamine d1 ligands.
SG11201504212WA (en) 2012-11-29 2015-06-29 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
CA2900303A1 (en) 2013-02-07 2014-08-14 Merck Patent Gmbh Substituted quinoxaline derivatives and their use as positive allosteric modulators of mglur4
HUE046961T2 (en) 2013-02-20 2020-04-28 Univ Pennsylvania Treatment of cancer using humanized anti-egfrviii chimeric antigen receptor
EP2970453B1 (en) 2013-03-13 2019-12-04 Prothena Biosciences Limited Tau immunotherapy
CN103554038B (en) 2013-06-19 2015-10-14 云南大学 Phenyl polyhalide nitrile quinazolinones and its production and use
JO3517B1 (en) * 2014-01-17 2020-07-05 Novartis Ag N-azaspirocycloalkane substituted n-heteroaryl compounds and compositions for inhibiting the activity of shp2
WO2015107494A1 (en) * 2014-01-17 2015-07-23 Novartis Ag 1 -(triazin-3-yi_/pyridazin-3-yl)-piper(-azine)idine derivatives and compositions thereof for inhibiting the activity of shp2
US10093646B2 (en) * 2014-01-17 2018-10-09 Novartis Ag 1-pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and compositions thereof for inhibiting the activity of SHP2
WO2015164862A1 (en) 2014-04-25 2015-10-29 Memorial Sloan-Kettering Cancer Center Treatment of h-ras-driven tumors
TWI687419B (en) 2014-07-10 2020-03-11 美商英塞特公司 Imidazopyridines and imidazopyrazines as LSD1 inhibitors
KR20170038877A (en) * 2014-08-01 2017-04-07 누에볼루션 에이/에스 Compounds active towards bromodomains
US10472347B2 (en) 2014-11-18 2019-11-12 Merck Sharp & Dohme Corp. Aminopyrazine compounds with A2A antagonist properties
ES2881305T3 (en) 2014-12-17 2021-11-29 Siemens Healthcare Diagnostics Inc Sandwich Assay Design for Small Molecules
CN107108637B (en) 2014-12-23 2019-10-29 诺华股份有限公司 Triazolopyrimidine compound and application thereof
WO2016112295A1 (en) 2015-01-09 2016-07-14 Warp Drive Bio, Inc. Compounds that participate in cooperative binding and uses thereof
ES2808781T3 (en) 2015-02-05 2021-03-01 Tyrnovo Ltd Combinations of dual IRS / STAT3 modulators and anticancer agents for the treatment of cancer
EP3277689B1 (en) 2015-04-03 2019-09-04 Incyte Corporation Heterocyclic compounds as lsd1 inhibitors
CN107787323B (en) 2015-06-19 2020-09-01 诺华股份有限公司 Compounds and compositions for inhibiting SHP2 activity
CN112625028B (en) * 2015-06-19 2024-10-29 诺华股份有限公司 Compounds and compositions for inhibiting SHP2 activity
WO2016203404A1 (en) 2015-06-19 2016-12-22 Novartis Ag Compounds and compositions for inhibiting the activity of shp2
WO2017011618A1 (en) 2015-07-15 2017-01-19 The Curators Of The University Of Missouri Targeted nanoparticle conjugate and method for co-delivery of sirna and drug
EP4242304A3 (en) 2015-10-01 2024-02-07 Revolution Medicines, Inc. Methods and reagents for analyzing protein-protein interfaces
WO2017156397A1 (en) 2016-03-11 2017-09-14 Board Of Regents, The University Of Texas Sysytem Heterocyclic inhibitors of ptpn11
GB201604970D0 (en) * 2016-03-23 2016-05-04 Syngenta Participations Ag Improvements in or relating to organic compounds
GB201604969D0 (en) * 2016-03-23 2016-05-04 Syngenta Participations Ag Improvements in or relating to organic compounds
EA202092442A3 (en) 2016-06-07 2021-08-31 Джакобио Фармасьютикалс Ко., Лтд. NEW HETEROCYCLIC DERIVATIVES USED AS SHP2 INHIBITORS
KR102457146B1 (en) * 2016-06-14 2022-10-19 노파르티스 아게 Compounds and compositions for inhibiting the activity of SHP2
CR20190063A (en) 2016-07-12 2019-05-27 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
TWI848901B (en) 2016-10-24 2024-07-21 美商傳達治療有限公司 Shp2 phosphatase inhibitors and methods of use thereof
ES2964956T3 (en) * 2017-01-10 2024-04-10 Novartis Ag Pharmaceutical combination comprising an ALK inhibitor and a SHP2 inhibitor
TWI820013B (en) 2017-01-23 2023-11-01 美商銳新醫藥公司 Bicyclic compounds as allosteric shp2 inhibitors
CA3051054A1 (en) 2017-01-23 2018-07-26 Revolution Medicines, Inc. Pyridine compounds as allosteric shp2 inhibitors
MA49013A (en) 2017-03-23 2021-05-05 Jacobio Pharmaceuticals Co Ltd NEW HETEROCYCLIC DERIVATIVES USEFUL AS SHP2 INHIBITORS
EP3606492A4 (en) 2017-04-05 2020-11-11 Revolution Medicines, Inc. Compounds that participate in cooperative binding and uses thereof
EP3607326A4 (en) 2017-04-05 2020-11-18 Revolution Medicines, Inc. Methods and reagents for analyzing protein-protein interfaces
EP3630770B1 (en) 2017-05-26 2024-08-28 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
BR112020004246A2 (en) 2017-09-07 2020-09-01 Revolution Medicines, Inc. shp2 inhibitory compositions and methods for the treatment of cancer
TW201930292A (en) 2017-10-12 2019-08-01 美商銳新醫藥公司 Pyridine, pyrazine, and triazine compounds as allosteric SHP2 inhibitors
MX2020006273A (en) 2017-12-15 2020-09-14 Revolution Medicines Inc Polycyclic compounds as allosteric shp2 inhibitors.
CN110156786B (en) 2018-02-13 2022-06-03 青煜医药研发(上海)有限公司 Pyrimido-cyclic compounds, process for their preparation and their use
KR102614939B1 (en) 2018-02-13 2023-12-19 블루레이 테라퓨틱스 (상하이) 컴퍼니 리미티드 Pyrimidine-fused ring compounds and their production methods and uses
CN112368272B (en) * 2018-03-21 2023-04-21 苏州浦合医药科技有限公司 SHP2 inhibitors and uses thereof
WO2019199792A1 (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
US20190336609A1 (en) 2018-05-01 2019-11-07 Revolution Medicines, Inc. C40-, C28-, and C-32-Linked Rapamycin Analogs as mTOR Inhibitors
AU2019262979B2 (en) 2018-05-01 2023-07-06 Revolution Medicines, Inc. C26-linked rapamycin analogs as mTOR inhibitors
AU2019338207A1 (en) 2018-09-10 2021-04-29 Mirati Therapeutics, Inc. Combination therapies
CA3113234A1 (en) * 2018-09-18 2020-03-26 Nikang Therapeutics, Inc. Tri-substituted heteroaryl derivatives as src homology-2 phosphatase inhibitors
EP3860717A1 (en) 2018-10-03 2021-08-11 Gilead Sciences, Inc. Imidozopyrimidine derivatives
EP3863636A1 (en) 2018-10-08 2021-08-18 Revolution Medicines, Inc. Shp2 inhibitor compositions for use in treating cancer
EP3878853A4 (en) 2018-11-07 2022-12-14 Shanghai Ringene BioPharma Co., Ltd. Nitrogen-containing fused heterocyclic shp2 inhibitor compound, preparation method, and use
JP7377679B2 (en) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド Combination therapy comprising a KRASG12C inhibitor and one or more additional pharmaceutically active agents for the treatment of cancer
MX2021006026A (en) 2018-11-30 2021-07-06 Tuojie Biotech Shanghai Co Ltd Pyrimidine and five-membered nitrogen heterocycle derivative, preparation method therefor, and medical uses thereof.
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
US20200197391A1 (en) 2018-12-21 2020-06-25 Revolution Medicines, Inc. Compounds that participate in cooperative binding and uses thereof
TW202132315A (en) 2019-11-04 2021-09-01 美商銳新醫藥公司 Ras inhibitors

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