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EA201990019A1 - Соединения и композиции для подавления активности shp2 - Google Patents

Соединения и композиции для подавления активности shp2

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Publication number
EA201990019A1
EA201990019A1 EA201990019A EA201990019A EA201990019A1 EA 201990019 A1 EA201990019 A1 EA 201990019A1 EA 201990019 A EA201990019 A EA 201990019A EA 201990019 A EA201990019 A EA 201990019A EA 201990019 A1 EA201990019 A1 EA 201990019A1
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EA
Eurasian Patent Office
Prior art keywords
compounds
compositions
suspension
shp2
activity
Prior art date
Application number
EA201990019A
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English (en)
Other versions
EA036446B1 (ru
Inventor
Чжолян Чэнь
Хорхе Гарсия Фортанет
Раджеш Карки
Мэттью Дж. Ламарш
Диути Маджумдар
Лоренс Блас Перес
Мартин Сендцик
Трой Дуглас Смит
Фань Ян
Бин Юй
Original Assignee
Новартис Аг
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Publication date
Application filed by Новартис Аг filed Critical Новартис Аг
Publication of EA201990019A1 publication Critical patent/EA201990019A1/ru
Publication of EA036446B1 publication Critical patent/EA036446B1/ru

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    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • A61K31/4965Non-condensed pyrazines
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    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • C07D207/30Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
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  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Compounds Of Unknown Constitution (AREA)
  • Transition And Organic Metals Composition Catalysts For Addition Polymerization (AREA)

Abstract

Настоящее изобретение относится к соединениям формулы I, в которой Y, Y, R, Rи Rопределены в кратком изложении сущности изобретения; способным ингибировать активность SHP2. В изобретении дополнительно предложен способ получения соединений данного изобретения, фармацевтических препаратов, содержащих такие соединения, и методы использования таких соединений и композиций в лечении заболеваний или расстройств, связанных с отличающейся от нормальной активностью SHP2.
EA201990019A 2016-06-14 2017-06-12 Соединения и композиции для подавления активности shp2 EA036446B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662349697P 2016-06-14 2016-06-14
PCT/IB2017/053469 WO2017216706A1 (en) 2016-06-14 2017-06-12 Compounds and compositions for inhibiting the activity of shp2

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EA201990019A1 true EA201990019A1 (ru) 2019-05-31
EA036446B1 EA036446B1 (ru) 2020-11-11

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US (3) US10934285B2 (ru)
EP (1) EP3468972B1 (ru)
JP (2) JP6994474B2 (ru)
KR (1) KR102457146B1 (ru)
CN (2) CN109415360B (ru)
AU (1) AU2017283769B2 (ru)
CA (1) CA3023216A1 (ru)
EA (1) EA036446B1 (ru)
ES (1) ES2810852T3 (ru)
MX (2) MX383856B (ru)
PL (1) PL3468972T3 (ru)
PT (1) PT3468972T (ru)
RU (2) RU2021106500A (ru)
WO (1) WO2017216706A1 (ru)

Families Citing this family (89)

* 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
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
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
KR20190110588A (ko) 2017-01-23 2019-09-30 레볼루션 메디슨즈, 인크. 알로스테릭 shp2 억제제로서의 피리딘 화합물
CA3051206A1 (en) 2017-01-23 2018-07-26 Revolution Medicines, Inc. Bicyclic compounds as allosteric shp2 inhibitors
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
WO2019051084A1 (en) 2017-09-07 2019-03-14 Revolution Medicines, Inc. SHP2 INHIBITOR COMPOSITIONS AND METHODS OF TREATING CANCER
JP7447002B2 (ja) 2017-09-11 2024-03-11 クルーゾン・ファーマシューティカルズ・インコーポレイテッド SHP2のオクタヒドロシクロペンタ[c]ピロールのアロステリック阻害剤
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
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
EP3759111A1 (en) 2018-03-02 2021-01-06 Otsuka Pharmaceutical Co., Ltd. Pharmaceutical compounds
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
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
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
SG11202100719YA (en) 2018-07-24 2021-02-25 Taiho Pharmaceutical Co Ltd Heterobicyclic compounds for inhibiting the activity of shp2
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
KR102820455B1 (ko) 2018-09-29 2025-06-16 노파르티스 아게 Shp2 활성 억제용 화합물의 제조 방법
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
CN111333663A (zh) * 2018-12-19 2020-06-26 天津医科大学 一类环烷基并噻吩并嘧啶酮化合物及其制法和用途
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
AU2020232026A1 (en) 2019-03-07 2021-09-02 Merck Patent Gmbh Carboxamide-pyrimidine derivatives as shp2 antagonists
KR102698608B1 (ko) 2019-04-02 2024-08-27 어레이 바이오파마 인크. 단백질 티로신 포스파타제 억제제
AU2020271838A1 (en) 2019-04-08 2021-08-19 Merck Patent Gmbh Pyrimidinone derivatives as SHP2 antagonists
TW202112761A (zh) 2019-06-14 2021-04-01 中國商北京盛諾基醫藥科技股份有限公司 Shp2磷酸酶變構抑制劑
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
US20230010886A1 (en) * 2019-09-23 2023-01-12 Suzhou Puhe BioPharma Co., Ltd. Shp2 inhibitors and uses thereof
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
EP4076667A1 (en) 2019-12-20 2022-10-26 Erasca, Inc. Tricyclic pyridones and pyrimidones
EP4092019A4 (en) 2020-01-16 2024-02-28 Zhejiang Hisun Pharmaceutical Co., Ltd. HETEROARYL DERIVATIVE, PROCESS THEREOF AND USE THEREOF
CN113754683A (zh) 2020-06-05 2021-12-07 上海奕拓医药科技有限责任公司 同位素取代的螺芳环化合物及其应用
WO2021249057A1 (zh) * 2020-06-12 2021-12-16 石药集团中奇制药技术(石家庄)有限公司 杂环化合物及其用途
AU2021293228A1 (en) 2020-06-18 2023-02-09 Revolution Medicines, Inc. Methods for delaying, preventing, and treating acquired resistance to RAS inhibitors
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
CN114053270B (zh) * 2020-08-05 2023-06-13 兰州大学第二医院 泛素结合酶e2t的小分子抑制剂
CN111943988B (zh) * 2020-08-17 2023-04-18 奥来德(上海)光电材料科技有限公司 一种铱掺杂电致发光材料及其制备方法和光电器件
CN114195799B (zh) * 2020-09-02 2025-01-28 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
AU2021344830A1 (en) 2020-09-03 2023-04-06 Revolution Medicines, Inc. Use of SOS1 inhibitors to treat malignancies with SHP2 mutations
US11690915B2 (en) 2020-09-15 2023-07-04 Revolution Medicines, Inc. Ras inhibitors
MX2023003338A (es) 2020-09-23 2023-06-14 Erasca Inc Piridonas y pirimidonas tricíclicas.
CN114437116A (zh) * 2020-10-30 2022-05-06 赣江新区博瑞创新医药有限公司 杂环化合物及其制备方法、药物组合物和应用
CN112062699B (zh) * 2020-11-13 2021-02-26 苏州开元民生科技股份有限公司 一种邻氨基苯硫酚的制备方法
US20230107642A1 (en) 2020-12-18 2023-04-06 Erasca, Inc. Tricyclic pyridones and pyrimidones
EP4039685A1 (en) 2021-02-08 2022-08-10 Irbm S.P.A. Azabicyclic shp2 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
JP2024516450A (ja) 2021-05-05 2024-04-15 レボリューション メディシンズ インコーポレイテッド 共有結合性ras阻害剤及びその使用
CA3217920A1 (en) 2021-05-05 2022-11-10 Andreas BUCKL Ras inhibitors for the treatment of cancer
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
US20220370456A1 (en) * 2021-05-05 2022-11-24 Huyabio International, Llc Combination therapies comprising shp2 inhibitors and egfr tyrosine kinase inhibitors
CN118234731A (zh) 2021-05-05 2024-06-21 锐新医药公司 Ras抑制剂
US20220370458A1 (en) * 2021-05-05 2022-11-24 Huyabio International, Llc Shp2 inhibitor monotherapy and uses thereof
CN115340561A (zh) * 2021-05-14 2022-11-15 药雅科技(上海)有限公司 Shp2磷酸酶稠环类抑制剂的制备及其应用
TW202244049A (zh) * 2021-05-12 2022-11-16 大陸商藥雅科技(上海)有限公司 Shp2磷酸酶抑制劑的製備及其應用
CN115340559A (zh) * 2021-05-12 2022-11-15 药雅科技(上海)有限公司 Shp2磷酸酶杂环类抑制剂的制备及其应用
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
US20240299393A1 (en) * 2021-06-17 2024-09-12 Dana-Farber Cancer Institute, Inc. Small molecule disruptors of protein interactions in histone deacetylase complexes
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
US20250230154A1 (en) * 2021-08-09 2025-07-17 Ubix Therapeutics, Inc. Compound having shp2 protein degrading activity, and medical uses 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
CN113717178B (zh) * 2021-09-30 2022-07-22 上海皓鸿生物医药科技有限公司 一种shp2抑制剂的中间体及其制备方法
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
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
WO2023172940A1 (en) 2022-03-08 2023-09-14 Revolution Medicines, Inc. Methods for treating immune refractory lung cancer
WO2023230205A1 (en) 2022-05-25 2023-11-30 Ikena Oncology, Inc. Mek inhibitors and uses thereof
KR20250022133A (ko) 2022-06-10 2025-02-14 레볼루션 메디슨즈, 인크. 거대고리 ras 억제제
EP4345101A1 (en) 2022-09-29 2024-04-03 Irbm S.P.A. Azole derivatives as shp2 inhibitors
KR20250087568A (ko) * 2022-10-19 2025-06-16 주식회사 유빅스테라퓨틱스 Shp2 단백질 분해용 화합물 및 이들의 의약 용도
CN116354960A (zh) * 2023-03-19 2023-06-30 药雅科技(上海)有限公司 Shp2磷酸酶抑制剂
TW202504611A (zh) 2023-03-30 2025-02-01 美商銳新醫藥公司 用於誘導ras gtp水解之組合物及其用途
WO2024211712A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
AR132338A1 (es) 2023-04-07 2025-06-18 Revolution Medicines Inc Inhibidores de ras
WO2024216048A1 (en) 2023-04-14 2024-10-17 Revolution Medicines, Inc. Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof
US20240352036A1 (en) 2023-04-14 2024-10-24 Revolution Medicines, Inc. Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
WO2025011568A1 (zh) * 2023-07-11 2025-01-16 勤浩医药(苏州)有限公司 用作shp2抑制剂的杂环化合物、包含其的药物组合物及其制备方法和用途
WO2025034702A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Rmc-6291 for use in the treatment of ras protein-related disease or disorder
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors

Family Cites Families (96)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH445129A (fr) 1964-04-29 1967-10-15 Nestle Sa Procédé pour la préparation de composés d'inclusion à poids moléculaire élevé
US3459731A (en) 1966-12-16 1969-08-05 Corn Products Co Cyclodextrin polyethers and their production
US3453257A (en) 1967-02-13 1969-07-01 Corn Products Co Cyclodextrin with cationic properties
US3426011A (en) 1967-02-13 1969-02-04 Corn Products Co Cyclodextrins with anionic properties
US3453259A (en) 1967-03-22 1969-07-01 Corn Products Co Cyclodextrin polyol ethers and their oxidation products
JPS6041077B2 (ja) 1976-09-06 1985-09-13 喜徳 喜谷 1,2‐ジアミノシクロヘキサン異性体のシス白金(2)錯体
US4235871A (en) 1978-02-24 1980-11-25 Papahadjopoulos Demetrios P Method of encapsulating biologically active materials in lipid vesicles
US4261989A (en) 1979-02-19 1981-04-14 Kaken Chemical Co. Ltd. Geldanamycin derivatives and antitumor drug
US4512991A (en) 1982-12-27 1985-04-23 Merck & Co., Inc. 3-Acyl-2-amino-5-halo-6-(substituted)pyrazine antimicrobial compounds
FR2567518B1 (fr) 1984-07-11 1987-11-13 Sanofi Sa Nouveaux composes a noyau heterocyclique azote, leur preparation et les medicaments qui en contiennent
US4737323A (en) 1986-02-13 1988-04-12 Liposome Technology, Inc. Liposome extrusion method
EP0257102B1 (en) 1986-02-24 1997-11-19 Mitsui Petrochemical Industries, Ltd. Agents for treating neurophathy
US5266573A (en) 1989-08-07 1993-11-30 Elf Sanofi Trifluoromethylphenyltetrahydropyridines for the treatment and/or prophylaxis of intestinal motility disorders
KR0166088B1 (ko) 1990-01-23 1999-01-15 . 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도
GB9012316D0 (en) 1990-06-01 1990-07-18 Wellcome Found Pharmacologically active cns compounds
DK169008B1 (da) 1990-06-01 1994-07-25 Holec Lk A S Fremgangsmåde og skærm til afskærmning af en strømtransformer samt strømtransformer med en sådan afskærmning
EP0647450A1 (en) 1993-09-09 1995-04-12 BEHRINGWERKE Aktiengesellschaft Improved prodrugs for enzyme mediated activation
IL115849A0 (en) 1994-11-03 1996-01-31 Merz & Co Gmbh & Co Tangential filtration preparation of liposomal drugs and liposome product thereof
MA26473A1 (fr) 1997-03-01 2004-12-20 Glaxo Group Ltd Composes pharmacologiquement actifs.
AU4198400A (en) 1999-04-06 2000-10-23 Krenitsky Pharmaceuticals Inc. Neurotrophic thio substituted pyrimidines
PE20010306A1 (es) 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
GB0018891D0 (en) 2000-08-01 2000-09-20 Novartis Ag Organic compounds
JP4272338B2 (ja) 2000-09-22 2009-06-03 バイエル アクチェンゲゼルシャフト ピリジン誘導体
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
EP2090571B1 (de) 2001-10-17 2012-05-16 Boehringer Ingelheim Pharma GmbH & Co. KG Pyrimidinderivate, Arzneimittel enthaltend diese Verbindungen, deren Verwendung und Verfahren zu ihrer Herstellung
JP4547911B2 (ja) 2002-02-01 2010-09-22 アリアド・ファーマシューティカルズ・インコーポレイテッド リン含有化合物およびその用途
MXPA04007697A (es) 2002-02-06 2004-11-10 Vertex Pharma Compuestos de heteroarilo utiles como inhibidores de gsk-3.
NZ534583A (en) 2002-03-05 2006-11-30 Axys Pharm Inc Leucinamide derivatives suitable as cathepsin cysteine protease inhibitors
TWI275390B (en) 2002-04-30 2007-03-11 Wyeth Corp Process for the preparation of 7-substituted-3- quinolinecarbonitriles
GB0300783D0 (en) 2003-01-14 2003-02-12 Btg Int Ltd Treatment of neurodegenerative conditions
US7399865B2 (en) 2003-09-15 2008-07-15 Wyeth Protein tyrosine kinase enzyme inhibitors
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
CA2563699C (en) 2004-04-23 2014-03-25 Exelixis, Inc. Kinase modulators and method of use
KR101225018B1 (ko) 2004-09-02 2013-01-23 쿠리스 인코퍼레이션 헤지호그 신호전달에 대한 피리딜 억제제
CA2591413A1 (en) 2004-12-16 2006-06-22 Vertex Pharmaceuticals Incorporated Pyrid-2-ones useful as inhibitors of tec family protein kinases for the treatment of inflammatory, proliferative and immunologically-mediated diseases
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
BRPI0615880A2 (pt) 2005-09-13 2011-05-31 Palau Pharma Sa compostos derivados de 2-aminopirimidina como moduladores da atividade de receptor da histamina h4, uso dos mesmos e composição farmacêutica
JP2009531456A (ja) 2006-03-28 2009-09-03 武田薬品工業株式会社 (r)−3−アミノピペリジン二塩酸塩の調製
US7515405B2 (en) 2006-07-25 2009-04-07 Hewlett-Packard Development Company, L.P. Anti-rotation mechanism for an electronic device
US20090137549A1 (en) 2006-11-09 2009-05-28 Paul John Edward Novel compounds useful for the treatment of degenerative & inflamatory diseases
CA2676920A1 (en) 2007-02-12 2008-08-21 Merck & Co., Inc. Piperidine derivatives
MY156814A (en) 2007-03-15 2016-03-31 Novartis Ag Organic compounds and their uses
AU2008298948B2 (en) 2007-09-12 2014-09-04 F. Hoffmann-La Roche Ag Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use
CA2701292C (en) 2007-10-25 2015-03-24 Genentech, Inc. Process for making thienopyrimidine compounds
BRPI0910668A2 (pt) 2008-04-22 2019-09-24 Portola Pharmaceutiacals Inc inibidores de proteína quinases
US20110092505A1 (en) 2008-06-13 2011-04-21 Robin Burgis Organic compounds
US8168784B2 (en) 2008-06-20 2012-05-01 Abbott Laboratories Processes to make apoptosis promoters
KR20110026481A (ko) 2008-06-20 2011-03-15 메타볼렉스, 인코포레이티드 아릴 gpr119 작동약 및 이의 용도
RU2536584C2 (ru) 2008-06-27 2014-12-27 Авила Терапьютикс, Инк. Гетероарильные соединения и их применение
WO2010011666A2 (en) 2008-07-21 2010-01-28 University Of South Florida Indoline scaffold shp-2 inhibitors and cancer treatment method
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
CN102356066A (zh) 2008-12-10 2012-02-15 同和药品株式会社 新型2,6-取代的-3-硝基吡啶衍生物、其制备方法及包含有其的药物组合物
FR2941696B1 (fr) 2009-02-05 2011-04-15 Sanofi Aventis Derives d'azaspiranyl-alkylcarbamates d'heterocycles a 5 chainons, leur preparation et leur application en therapeutique
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
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
US8673913B2 (en) 2009-11-13 2014-03-18 Case Western Reserve University SHP-2 phosphatase inhibitor
WO2011078143A1 (ja) 2009-12-22 2011-06-30 塩野義製薬株式会社 ピリミジン誘導体およびそれらを含有する医薬組成物
PH12012502572A1 (en) 2010-06-30 2022-03-30 Fujifilm Corp Novel nicotinamide derivative or salt thereof
CA2804970A1 (en) 2010-07-13 2012-01-19 Merck Sharp & Dohme Corp. Spirocyclic compounds
JP5889895B2 (ja) 2010-07-29 2016-03-22 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 Ampk活性化複素環化合物およびその使用方法
US8609672B2 (en) 2010-08-27 2013-12-17 University Of The Pacific Piperazinylpyrimidine analogues as protein kinase inhibitors
US9056865B2 (en) 2010-10-20 2015-06-16 Pfizer Inc. Pyridine-2-derivatives as smoothened receptor modulators
BR112013014854B1 (pt) * 2010-12-13 2020-12-08 Array Biopharma compostos de n-(1h-indazol-4-il)imidazo[1,2-a]piridina-3- carboxamida substituídos como inibidores de tirosina quinase de receptor tipo iii, seu processo de produção e composição farmacêutica
DK2755958T3 (en) 2011-09-12 2017-09-25 Merck Patent Gmbh AMINOPYRIMIDINE DERIVATIVES USED AS MODULATORS OF KINASE ACTIVITY
WO2013096093A1 (en) 2011-12-21 2013-06-27 Merck Sharp & Dohme Corp. Compounds as dgat-1 inhibitors
CN104540830A (zh) 2012-06-07 2015-04-22 霍夫曼-拉罗奇有限公司 端锚聚合酶的吡唑并嘧啶酮和吡唑并吡啶酮抑制剂
WO2013186159A1 (en) 2012-06-13 2013-12-19 F. Hoffmann-La Roche Ag New diazaspirocycloalkane and azaspirocycloalkane
EP2903985A1 (en) 2012-10-03 2015-08-12 Advinus Therapeutics Limited Spirocyclic compounds, compositions and medicinal applications thereof
US9499522B2 (en) 2013-03-15 2016-11-22 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
WO2015092819A2 (en) 2013-12-21 2015-06-25 Nektar Therapeutics (India) Pvt. Ltd. Derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5- amine
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
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
HUE057895T2 (hu) 2014-05-01 2022-06-28 Celgene Quanticel Res Inc Lizinspecifikus demetiláz-1 inhibitorai
US10174032B2 (en) 2014-05-05 2019-01-08 Signalrx Pharmaceuticals, Inc. Heterocyclic compound classes for signaling modulation
US10189812B2 (en) 2014-08-15 2019-01-29 The Key Laboratory Of Chemistry For Natural Produc Bi-benzyl isoquinoline derivative, preparation method and use thereof in hepatopathy treatment and prevention
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
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
WO2017156397A1 (en) 2016-03-11 2017-09-14 Board Of Regents, The University Of Texas Sysytem Heterocyclic inhibitors of ptpn11
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
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
KR20190110588A (ko) 2017-01-23 2019-09-30 레볼루션 메디슨즈, 인크. 알로스테릭 shp2 억제제로서의 피리딘 화합물
CA3051206A1 (en) 2017-01-23 2018-07-26 Revolution Medicines, Inc. Bicyclic compounds as allosteric shp2 inhibitors
WO2018172984A1 (en) 2017-03-23 2018-09-27 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as shp2 inhibitors
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
EP3755699A1 (en) 2018-02-21 2020-12-30 Relay Therapeutics, Inc. Shp2 phosphatase inhibitors and methods of use thereof
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
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

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