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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)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (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 (84)

* 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
AU2017274199B2 (en) 2016-05-31 2021-09-23 Board Of Regents, The University Of Texas System Heterocyclic inhibitors of PTPN11
JP6751203B2 (ja) 2016-06-07 2020-09-02 ジャコバイオ ファーマスーティカルズ カンパニー リミテッドJacobio Pharmaceuticals Co., Ltd. Shp2阻害剤として有用な新規複素環式誘導体
RU2021106500A (ru) 2016-06-14 2021-04-16 Новартис Аг Соединения и композиции для подавления активности shp2
TWI806832B (zh) 2016-07-12 2023-07-01 美商銳新醫藥公司 作為異位shp2抑制劑之2,5-雙取代型3-甲基吡嗪及2,5,6-三取代型3-甲基吡嗪
EP3515916B1 (en) 2016-09-22 2023-06-07 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
BR112019014527A2 (pt) 2017-01-23 2020-02-27 Revolution Medicines, Inc. Compostos de piridina como inibidores de shp2 alostéricos
AU2018210770B2 (en) 2017-01-23 2022-03-24 Revolution Medicines, Inc. Bicyclic compounds as allosteric SHP2 inhibitors
SG11201908820VA (en) 2017-03-23 2019-10-30 Jacobio Pharmaceuticals Co Ltd Novel heterocyclic derivatives useful as shp2 inhibitors
WO2018218133A1 (en) 2017-05-26 2018-11-29 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
KR102636383B1 (ko) 2017-08-04 2024-02-14 스카이호크 테라퓨틱스, 인코포레이티드 스플라이싱을 조절하는 방법 및 조성물
SG11202001282UA (en) 2017-09-07 2020-03-30 Revolution Medicines Inc Shp2 inhibitor compositions and methods for treating cancer
EP3687997A1 (en) 2017-09-29 2020-08-05 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
BR112020007058A2 (pt) 2017-10-12 2020-10-06 Revolution Medicines, Inc. compostos de piridina, pirazina, e triazina como inibidores de shp2 alostéricos
WO2019118909A1 (en) 2017-12-15 2019-06-20 Revolution Medicines, Inc. Polycyclic compounds as allosteric shp2 inhibitors
EP3768680A1 (en) 2018-03-21 2021-01-27 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine shp2 phosphatase inhibitors and methods of use thereof
AU2019239658A1 (en) 2018-03-21 2020-11-12 Suzhou Puhe BioPharma Co., Ltd. SHP2 inhibitors and uses thereof
EP3768668B1 (en) 2018-03-21 2024-08-28 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof
CA3099151A1 (en) 2018-05-02 2019-11-07 Navire Pharma, Inc. Substituted heterocyclic inhibitors of ptpn11
MX2021001608A (es) 2018-08-10 2021-07-15 Navire Pharma Inc Inhibidores de ptpn11.
BR112021005082A2 (pt) 2018-09-18 2021-06-08 Nikang Therapeutics, Inc. derivados de anel tricíclico fundido como inibidores de src homologia-2 fosfatase
WO2020063760A1 (en) 2018-09-26 2020-04-02 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as shp2 inhibitors
IL304526B2 (en) * 2018-09-29 2025-05-01 Novartis Ag Production of compounds and preparations for inhibiting the activity of SHP2
WO2020072656A1 (en) 2018-10-03 2020-04-09 Gilead Sciences, Inc. Imidozopyrimidine derivatives
CA3116561C (en) 2018-10-17 2023-09-12 Array Biopharma Inc. Protein tyrosine phosphatase inhibitors
CN117143079A (zh) 2018-11-06 2023-12-01 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
JP7603592B2 (ja) 2019-02-05 2024-12-20 スカイホーク・セラピューティクス・インコーポレーテッド スプライシングを調節するための方法および組成物
CN114126613A (zh) 2019-02-05 2022-03-01 斯基霍克疗法公司 用于调节剪接的方法和组合物
EP3920928A4 (en) 2019-02-06 2022-09-28 Skyhawk Therapeutics, Inc. METHODS AND COMPOSITIONS FOR MODULATION OF SPLICING
CN119638696A (zh) 2019-02-06 2025-03-18 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
CU20210080A7 (es) 2019-04-02 2022-05-11 Array Biopharma Inc Triazinas sustituidas como inhibidores de proteína tirosina fosfatasa
UY38687A (es) 2019-05-17 2023-05-15 Novartis Ag Inhibidores del inflamasoma nlrp3, composiciones, combinaciones de los mismos y métodos para su uso
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
CN114127053B (zh) * 2019-09-06 2023-06-13 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
KR20220066923A (ko) 2019-09-24 2022-05-24 릴레이 테라퓨틱스, 인크. Shp2 포스파테이스 억제제 및 이의 제조 및 사용 방법
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
WO2021143680A1 (zh) 2020-01-16 2021-07-22 浙江海正药业股份有限公司 杂芳基类衍生物及其制备方法和用途
WO2021143823A1 (zh) * 2020-01-16 2021-07-22 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
TW202146021A (zh) 2020-02-28 2021-12-16 瑞士商諾華公司 包含達拉菲尼、erk抑制劑和shp2抑制劑之三重藥物組合
CN115667239B (zh) * 2020-06-22 2025-11-18 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
TW202216723A (zh) 2020-07-08 2022-05-01 瑞士商諾華公司 用於抑制shp2活性的化合物及組成物之製造
CN115916765B (zh) * 2020-07-10 2025-04-18 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
EP4237086A1 (en) 2020-10-27 2023-09-06 Amgen Inc. Heterocyclic spiro compounds and methods of use
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
EP4313307A1 (en) * 2021-04-01 2024-02-07 Array Biopharma Inc. Crystalline form of a shp2 inhibitor
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
JP2024517693A (ja) 2021-04-29 2024-04-23 アムジエン・インコーポレーテツド 2-アミノベンゾチアゾール化合物及びその使用方法
WO2022235822A1 (en) 2021-05-05 2022-11-10 Huabio International, Llc Shp2 inhibitor monotherapy and uses thereof
WO2022235817A1 (en) 2021-05-05 2022-11-10 Huabio International, Llc Combination therapies comprising shp2 inhibitors and pd-1 inhibitors
KR20240007279A (ko) * 2021-05-13 2024-01-16 상하이 인스티튜트 오브 마테리아 메디카 차이니즈 아카데미 오브 싸이언시즈 Shp2활성을 억제하는 헤테로고리 화합물, 이의 제조 방법 및 용도
WO2022259157A1 (en) 2021-06-09 2022-12-15 Novartis Ag A triple pharmaceutical combination comprising dabrafenib, trametinib and a shp2 inhibitor
KR102699226B1 (ko) 2021-06-09 2024-08-27 에프. 호프만-라 로슈 아게 암 치료를 위한 병용요법
MX2023014563A (es) 2021-06-09 2024-02-08 Hoffmann La Roche Combinacion de un inhibidor de braf particular (interruptor de paradoja) y un antagonista de union al eje de pd-1 para su uso en el tratamiento de cancer.
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
TW202319056A (zh) 2021-07-09 2023-05-16 南韓商治納輔醫藥科技有限公司 Shp2抑制劑及其用途
TW202327569A (zh) 2021-09-01 2023-07-16 瑞士商諾華公司 包含tead抑制劑的藥物組合及其用於癌症治療之用途
KR20240105382A (ko) 2021-11-04 2024-07-05 에프. 호프만-라 로슈 아게 암 치료를 위한 퀴나졸리논 화합물의 신규한 용도
CN118401505A (zh) * 2021-12-28 2024-07-26 捷思英达控股有限公司 作为shp2抑制剂的杂环化合物、包括该杂环化合物的组合物及其使用方法
CA3251671A1 (en) 2022-02-16 2023-08-24 Amgen Inc. QUINAZOLINE COMPOUNDS AND THEIR USE AS INHIBITORS OF MUTANT KRAS PROTEINS
AU2023222076A1 (en) 2022-02-16 2024-08-15 Amgen Inc. Quinazoline compounds and use thereof as inhibtors of mutant kras proteins
TW202404581A (zh) 2022-05-25 2024-02-01 美商醫肯納腫瘤學公司 Mek抑制劑及其用途
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
UY40374A (es) 2022-08-03 2024-02-15 Novartis Ag Inhibidores de inflamasoma nlrp3
EP4345101A1 (en) 2022-09-29 2024-04-03 Irbm S.P.A. Azole derivatives as shp2 inhibitors
JP2025541200A (ja) 2022-12-15 2025-12-18 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト がん処置のための併用療法
EP4647433A1 (en) * 2023-01-05 2025-11-12 Kanaph Therapeutics Inc. Shp2 inhibitor and uses thereof
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
WO2025194057A1 (en) 2024-03-14 2025-09-18 Amgen Inc. Macrocyclic compounds as modulators of kras and uses thereof
WO2025194054A1 (en) 2024-03-14 2025-09-18 Amgen Inc. Spirocyclic compounds as modulators of kras and uses thereof
WO2025217247A1 (en) 2024-04-10 2025-10-16 Amgen Inc. Tethered spiro-heterocyclic inhibitors of kras g12c mutant proteins and uses thereof
WO2025230878A1 (en) 2024-04-29 2025-11-06 Amgen Inc. Macrocyclic compounds as modulators of kras and uses thereof
WO2025240582A1 (en) 2024-05-14 2025-11-20 Amgen Inc. Macrocyclic compounds as modulators of kras and uses thereof
WO2025261943A1 (en) 2024-06-18 2025-12-26 F. Hoffmann-La Roche Ag Anti-cancer combinations comprising mosperafenib and folfox or folfiri

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
PT880523E (pt) 1996-02-07 2007-01-31 Neurocrine Biosciences Inc Pirazolopirimidinas com antagonistas dos receptores de crf
WO1998056376A1 (en) 1997-06-13 1998-12-17 Sugen, Inc. Novel heteroaryl compounds for the modulation of protein tyrosine enzyme related cellular signal transduction
DE60023920T2 (de) 1999-08-27 2006-07-20 Sugen, Inc., South San Francisco Phosphatmimetika und Verfahren zur Behandlung mit Phosphataseinhibitoren HIBITOREN
AU783915B2 (en) 2000-02-16 2005-12-22 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
CA2479744A1 (en) 2002-03-28 2003-10-09 Paul E. Finke Substituted 2,3-diphenyl pyridines
WO2004024719A1 (en) 2002-09-12 2004-03-25 Pharmacia & Upjohn Company Llc Substituted 1,4-pyrazine derivatives
JP4511943B2 (ja) 2002-12-23 2010-07-28 ワイス エルエルシー Pd−1に対する抗体およびその使用
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 (fr) 2003-06-26 2008-04-11 Sanofi Synthelabo Derives de diphenylpyridine, leur preparation et leur application en therapeutique
JP2007504243A (ja) 2003-09-03 2007-03-01 ニューロジェン・コーポレーション 5−アリール−ピラゾロ[4,3−d]ピリミジン類、ピリジン類、ピラジン類及び関連化合物
ES2288270T3 (es) 2003-10-10 2008-01-01 Pfizer Products Incorporated 2h-(1,2,4)triazolo(4,3-a)pirazinas sustituidas como inhibidores de gsk-3.
CA2543644A1 (en) 2003-10-27 2005-05-06 Astellas Pharma Inc. Pyrazine derivatives and pharmaceutical use thereof
DE102004015954A1 (de) 2004-04-01 2005-11-10 Ina-Schaeffler Kg Umschlingungstrieb
WO2005095384A1 (en) 2004-04-01 2005-10-13 Astellas Pharma Inc. Pyrazine derivatives and pharmaceutical use thereof as adenosine antagonists
JP2008503591A (ja) 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 ユビキチンリガーゼ阻害剤
DE602005020981D1 (de) 2004-12-23 2010-06-10 Mallinckrodt Inc Fluoreszente pyrazinderivate und verfahren zu deren anwendung bei der bewertung der nierenfunktion
WO2006088837A2 (en) * 2005-02-16 2006-08-24 Schering Corporation Heterocyclic substituted piperazines with cxcr3 antagonist activity
TW200716594A (en) 2005-04-18 2007-05-01 Neurogen Corp Substituted heteroaryl CB1 antagonists
MX2007016463A (es) 2005-06-22 2008-03-04 Plexxikon Inc Derivados de pirrolo [2,3-b] piridina como inhibidores de proteina cinasa.
ES2775049T3 (es) 2005-10-21 2020-07-23 Univ California Mutaciones del gen SHP-2 en melanomas
US9283288B2 (en) 2006-02-24 2016-03-15 Medibeacon, Inc. Methods of 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
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
KR20090026288A (ko) 2006-05-31 2009-03-12 갈라파고스 엔.브이. 퇴행성 및 염증성 질환의 치료에 유용한 트리아졸로피라진 화합물
JP2009539840A (ja) 2006-06-06 2009-11-19 シェーリング コーポレイション プロテインキナーゼ阻害剤としてのイミダゾピラジン
JP2010520238A (ja) 2007-03-01 2010-06-10 マリンクロット インコーポレイテッド 統合された光活性低分子および統合された光活性低分子使用
KR20100016291A (ko) 2007-04-06 2010-02-12 노파르티스 아게 단백질 키나아제 억제제로 유용한 [2,6] 나프티리딘
US8133895B2 (en) 2007-05-10 2012-03-13 Janssen Pharmaceutica N.V. Fused pyrazine compounds useful for the treatment of degenerative and 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
JPWO2008156174A1 (ja) 2007-06-21 2010-08-26 大正製薬株式会社 ピラジンアミド化合物
CA2695365A1 (en) * 2007-08-03 2009-02-12 Schering Corporation Method of treating cxcr3 mediated diseases using heterocyclic substituted piperazines
US8003797B2 (en) 2007-08-09 2011-08-23 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
EP2349267B1 (en) 2008-10-30 2014-06-25 Merck Sharp & Dohme Corp. Pyridazine carboxamide orexin receptor antagonists
PE20110924A1 (es) 2009-01-23 2011-12-24 Rigel Pharmaceuticals Inc Derivados de 2, 4-diamino-pirimidina n2, n4-disustituidos como inhibidores de jak3
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
US20120065205A1 (en) * 2009-06-01 2012-03-15 Mercer Swati P Pyrazine carboxamide orexin receptor antagonists
BR112012003637A2 (pt) * 2009-08-17 2017-04-25 Memorial Sloan Kettering Cancer Center "compostos de ligação de proteína de choque térmico, composições, e métodos para preparar e usar os mesmos"
CA2780713A1 (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
EP2542588A1 (en) 2010-03-05 2013-01-09 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 (ja) * 2010-05-11 2015-12-16 サノフイ 置換n−ヘテロアリールスピロラクタムビピロリジン類、その製造及び治療的使用
US8703768B2 (en) 2010-06-09 2014-04-22 Hoffmann-La Roche Inc. Nitrogen containing heteroaryl compounds
PH12013500084A1 (en) 2010-07-14 2015-09-11 Novartis Ag Ip receptor agonist heterocyclic compounds
GB201106829D0 (en) 2011-04-21 2011-06-01 Proximagen Ltd Heterocyclic compounds
JP5808826B2 (ja) 2011-02-23 2015-11-10 インテリカイン, エルエルシー 複素環化合物およびその使用
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
CA2881279C (en) 2012-08-07 2020-07-07 Merck Patent Gmbh Pyridopyrimidine derivatives as protein kinase inhibitors
KR20150065191A (ko) 2012-11-08 2015-06-12 화이자 인코포레이티드 헤테로방향족 화합물 및 도파민 d1 리간드로서 이의 용도
CA2892042C (en) 2012-11-29 2022-06-14 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
US20150374687A1 (en) 2013-02-07 2015-12-31 Merck Patent Gmbh Substituted quinoxaline derivatives and their use as positive allosteric modulators of mglur4
KR102685501B1 (ko) 2013-02-20 2024-07-17 노파르티스 아게 인간화 항-EGFRvIII 키메라 항원 수용체를 사용한 암의 치료
CU24446B1 (es) 2013-03-13 2019-10-04 Prothena Biosciences Ltd Un anticuerpo monoclonal humanizado que se une a tau
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
JO3517B1 (ar) 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
WO2015107493A1 (en) * 2014-01-17 2015-07-23 Novartis Ag 1 -pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and and compositions thereof for inhibiting the activity of shp2
ES2699354T3 (es) * 2014-01-17 2019-02-08 Novartis Ag Derivados de 1-(triazin-3-il/piridazin-3-il)-piper(-azin)idina y composiciones de las mismas para inhibir la actividad de SHP2
CA2946759A1 (en) 2014-04-25 2015-10-29 Memorial Sloan-Kettering Cancer Center Treatment of h-ras-driven tumors
US9695168B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,5-α]pyridines and imidazo[1,5-α]pyrazines as LSD1 inhibitors
WO2016016316A1 (en) * 2014-08-01 2016-02-04 Nuevolution A/S Compounds active towards bromodomains
MX381180B (es) 2014-11-18 2025-03-12 Merck Sharp & Dohme Compuestos aminopirazina con propiedades antagonistas a2a.
WO2016100116A1 (en) 2014-12-17 2016-06-23 Siemens Healthcare Diagnostics Inc. Sandwich assay design for small molecules
PL3237418T3 (pl) 2014-12-23 2019-07-31 Novartis Ag Związki triazolopirymidyny i ich zastosowania
US10533016B2 (en) 2015-01-09 2020-01-14 Revolution Medicines, Inc. Compounds that participate in cooperative binding and 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
MA51438A (fr) 2015-04-03 2021-04-14 Incyte Corp Composés hétérocycliques utilisés en tant qu'inhibiteurs de lsd1
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
WO2016203404A1 (en) 2015-06-19 2016-12-22 Novartis Ag Compounds and compositions for inhibiting the activity of shp2
WO2016203405A1 (en) 2015-06-19 2016-12-22 Novartis Ag Compounds and compositions for inhibiting the activity of 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
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
JP6751203B2 (ja) 2016-06-07 2020-09-02 ジャコバイオ ファーマスーティカルズ カンパニー リミテッドJacobio Pharmaceuticals Co., Ltd. Shp2阻害剤として有用な新規複素環式誘導体
RU2021106500A (ru) * 2016-06-14 2021-04-16 Новартис Аг Соединения и композиции для подавления активности shp2
TWI806832B (zh) 2016-07-12 2023-07-01 美商銳新醫藥公司 作為異位shp2抑制劑之2,5-雙取代型3-甲基吡嗪及2,5,6-三取代型3-甲基吡嗪
EP3515916B1 (en) 2016-09-22 2023-06-07 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
ES2964956T3 (es) * 2017-01-10 2024-04-10 Novartis Ag Combinación farmacéutica que comprende un inhibidor de ALK y un inhibidor de SHP2
AU2018210770B2 (en) 2017-01-23 2022-03-24 Revolution Medicines, Inc. Bicyclic compounds as allosteric SHP2 inhibitors
BR112019014527A2 (pt) * 2017-01-23 2020-02-27 Revolution Medicines, Inc. Compostos de piridina como inibidores de shp2 alostéricos
SG11201908820VA (en) 2017-03-23 2019-10-30 Jacobio Pharmaceuticals Co Ltd Novel heterocyclic derivatives useful as shp2 inhibitors
US20200199102A1 (en) 2017-04-05 2020-06-25 Revolution Medicines, Inc. Compounds that participate in cooperative binding and uses thereof
JP2020520988A (ja) 2017-04-05 2020-07-16 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. タンパク質−タンパク質界面を分析するための方法及び試薬
WO2018218133A1 (en) 2017-05-26 2018-11-29 Relay Therapeutics, Inc. Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors
SG11202001282UA (en) 2017-09-07 2020-03-30 Revolution Medicines Inc Shp2 inhibitor compositions and methods for treating cancer
BR112020007058A2 (pt) 2017-10-12 2020-10-06 Revolution Medicines, Inc. compostos de piridina, pirazina, e triazina como inibidores de shp2 alostéricos
WO2019118909A1 (en) 2017-12-15 2019-06-20 Revolution Medicines, Inc. Polycyclic compounds as allosteric shp2 inhibitors
AU2019222026B2 (en) 2018-02-13 2022-05-12 Shanghai Blueray Biopharma Co., Ltd. Pyrimidine-fused cyclic compound, preparation method therefor and application thereof
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
AU2019239658A1 (en) * 2018-03-21 2020-11-12 Suzhou Puhe BioPharma Co., Ltd. SHP2 inhibitors and uses thereof
CN112203689A (zh) 2018-04-10 2021-01-08 锐新医药公司 治疗癌症的shp2抑制剂组合物和方法
CN118978535A (zh) 2018-05-01 2024-11-19 锐新医药公司 作为mTOR抑制剂的C40-、C28-及C-32连接的雷帕霉素类似物
MX2020011564A (es) 2018-05-01 2021-01-29 Revolution Medicines Inc Analogos de rapamicina unidos a c26 como inhibidores de mtor.
CA3111980A1 (en) 2018-09-10 2020-03-19 Mirati Therapeutics, Inc. Combination therapies
BR112021005082A2 (pt) * 2018-09-18 2021-06-08 Nikang Therapeutics, Inc. derivados de anel tricíclico fundido como inibidores de src homologia-2 fosfatase
WO2020072656A1 (en) 2018-10-03 2020-04-09 Gilead Sciences, Inc. Imidozopyrimidine derivatives
EP3863636A1 (en) 2018-10-08 2021-08-18 Revolution Medicines, Inc. Shp2 inhibitor compositions for use in treating cancer
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
JP2022509149A (ja) 2018-11-30 2022-01-20 上海拓界生物医薬科技有限公司 ピリミジンと5員窒素ヘテロ環の誘導体、その製造方法、およびそれらの医学的使用
EP3897644A4 (en) 2018-12-21 2022-09-07 Revolution Medicines, Inc. CONNECTIONS INVOLVING IN A COOPERATIVE BINDING AND USES THEREOF
CN114901366A (zh) 2019-11-04 2022-08-12 锐新医药公司 Ras抑制剂

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