JP2020536881A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2020536881A5 JP2020536881A5 JP2020519790A JP2020519790A JP2020536881A5 JP 2020536881 A5 JP2020536881 A5 JP 2020536881A5 JP 2020519790 A JP2020519790 A JP 2020519790A JP 2020519790 A JP2020519790 A JP 2020519790A JP 2020536881 A5 JP2020536881 A5 JP 2020536881A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- pharmaceutically acceptable
- acceptable salt
- compound according
- solvate
- Prior art date
- Legal status (The legal status 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 status listed.)
- Pending
Links
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762571760P | 2017-10-12 | 2017-10-12 | |
| US62/571,760 | 2017-10-12 | ||
| US201862615353P | 2018-01-09 | 2018-01-09 | |
| US62/615,353 | 2018-01-09 | ||
| US201862678889P | 2018-05-31 | 2018-05-31 | |
| US62/678,889 | 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 (2)
| Publication Number | Publication Date |
|---|---|
| JP2020536881A JP2020536881A (ja) | 2020-12-17 |
| JP2020536881A5 true JP2020536881A5 (https=) | 2021-11-11 |
Family
ID=64049755
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020519790A Pending JP2020536881A (ja) | 2017-10-12 | 2018-10-11 | アロステリックshp2阻害剤としてのピリジン、ピラジンおよびトリアジン化合物 |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US11702411B2 (https=) |
| EP (1) | EP3694848A1 (https=) |
| JP (1) | JP2020536881A (https=) |
| KR (1) | KR20200070295A (https=) |
| CN (1) | CN111212834B (https=) |
| AU (1) | AU2018347516A1 (https=) |
| BR (1) | BR112020007058A2 (https=) |
| CA (1) | CA3078565A1 (https=) |
| CO (1) | CO2020003714A2 (https=) |
| IL (1) | IL273756A (https=) |
| MX (1) | MX2020003579A (https=) |
| PH (1) | PH12020550216A1 (https=) |
| RU (1) | RU2020115095A (https=) |
| SG (1) | SG11202002941WA (https=) |
| TW (1) | TW201930292A (https=) |
| WO (1) | WO2019075265A1 (https=) |
Families Citing this family (87)
| 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 |
| EA202092441A1 (ru) | 2016-06-07 | 2021-05-21 | Джакобио Фармасьютикалс Ко., Лтд. | Новые гетероциклические производные, применимые в качестве ингибиторов shp2 |
| MX383856B (es) | 2016-06-14 | 2025-03-14 | Novartis Ag | Compuestos y composiciones para inhibir la actividad de shp2. |
| KR102598895B1 (ko) | 2016-07-12 | 2023-11-07 | 레볼루션 메디슨즈, 인크. | 다른자리 입체성 shp2 억제제로서의 2,5-이치환 3-메틸 피라진 및 2,5,6-3치환 3-메틸 피라진 |
| 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 |
| MX2019008696A (es) | 2017-01-23 | 2019-09-13 | Revolution Medicines Inc | Compuestos de piridina como inhibidores de shp2 alostericos. |
| MX2019008695A (es) | 2017-01-23 | 2019-09-11 | Revolution Medicines Inc | Compuestos biciclicos como inhibidores alostericos de shp2. |
| KR20240026521A (ko) | 2017-03-23 | 2024-02-28 | 자코바이오 파마슈티칼스 컴퍼니 리미티드 | Shp2 억제제로서 유용한 신규한 헤테로환형 유도체 |
| WO2018218133A1 (en) | 2017-05-26 | 2018-11-29 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors |
| JP7312749B2 (ja) | 2017-08-04 | 2023-07-21 | 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 | スプライシングをモジュレートする方法および組成物 |
| CA3074690A1 (en) | 2017-09-07 | 2019-03-14 | 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 |
| MX2020003579A (es) | 2017-10-12 | 2020-07-22 | Revolution Medicines Inc | Compuestos de piridina, pirazina, y triazina como inhibidores de shp2 alostericos. |
| BR112020009757A2 (pt) | 2017-12-15 | 2020-11-03 | Revolution Medicines, Inc. | compostos policíclicos como inibidores alostéricos de shp2 |
| SG11202009245TA (en) | 2018-03-21 | 2020-10-29 | Relay Therapeutics Inc | Shp2 phosphatase inhibitors and methods of use thereof |
| WO2019183364A1 (en) | 2018-03-21 | 2019-09-26 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine shp2 phosphatase inhibitors and methods of use thereof |
| RU2020133727A (ru) | 2018-03-21 | 2022-04-21 | Сучжоу Пухе Биофарма Ко., Лтд. | Ингибиторы shp2 и их применение |
| KR102611661B1 (ko) | 2018-05-02 | 2023-12-08 | 나비레 파르마, 인코퍼레이티드 | Ptpn11의 치환된 헤테로사이클릭 억제제 |
| LT3833670T (lt) | 2018-08-10 | 2024-06-25 | Navire Pharma, Inc. | 6-(4-amino-3-metil-2-oksa-8-azaspiro[4.5]dekan-8-il)-3-(2,3-dichlorfenil)-2-metilpirimidin-4(3h)-ono dariniai ir susiję junginiai kaip ptpn11 (shp2) inhibitoriai, skirti vėžiui gydyti |
| JP7542538B2 (ja) | 2018-09-18 | 2024-08-30 | ニカング セラピューティクス, インコーポレイテッド | Srcホモロジー-2ホスファターゼ阻害剤としての縮合三環式環誘導体 |
| CN112839935A (zh) | 2018-09-26 | 2021-05-25 | 北京加科思新药研发有限公司 | 可用作shp2抑制剂的新型杂环衍生物 |
| CA3112322A1 (en) | 2018-09-29 | 2020-04-02 | Novartis Ag | Manufacture of compounds and compositions for inhibiting the activity of shp2 |
| WO2020072656A1 (en) | 2018-10-03 | 2020-04-09 | Gilead Sciences, Inc. | Imidozopyrimidine derivatives |
| US12187721B2 (en) | 2018-10-17 | 2025-01-07 | 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 |
| JP7551629B2 (ja) | 2019-02-05 | 2024-09-17 | 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 |
| WO2020163405A1 (en) | 2019-02-05 | 2020-08-13 | Skyhawk Therapeutics, Inc. | Methods and compositions for modulating splicing |
| JP7603594B2 (ja) | 2019-02-06 | 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 |
| JP7603595B2 (ja) | 2019-02-06 | 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 |
| 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 |
| WO2020201991A1 (en) | 2019-04-02 | 2020-10-08 | Array Biopharma Inc. | Protein tyrosine phosphatase inhibitors |
| 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 |
| AU2020354475A1 (en) | 2019-09-24 | 2022-05-05 | Relay Therapeutics, Inc. | SHP2 phosphatase inhibitors and methods of making and using the same |
| 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 |
| CN114867720B (zh) | 2020-01-16 | 2024-10-22 | 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 |
| WO2021171261A1 (en) | 2020-02-28 | 2021-09-02 | Novartis Ag | A triple pharmaceutical combination comprising dabrafenib, an erk inhibitor and a shp2 inhibitor |
| EP4169913A4 (en) * | 2020-06-22 | 2024-10-30 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | SUBSTITUTED PYRAZINE COMPOUND, PHARMACEUTICAL COMPOSITION THEREOF AND USE THEREOF |
| CN115916786B (zh) | 2020-07-08 | 2025-10-17 | 诺华股份有限公司 | 用于抑制shp2活性的化合物和组合物的制造 |
| 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 |
| JP7654071B2 (ja) | 2020-10-20 | 2025-03-31 | アムジエン・インコーポレーテツド | 複素環スピロ化合物及び使用方法 |
| JP2023549055A (ja) | 2020-10-27 | 2023-11-22 | アムジエン・インコーポレーテツド | 複素環式スピロ化合物及びその使用方法 |
| WO2022161222A1 (zh) * | 2021-01-29 | 2022-08-04 | 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 |
| CA3215295A1 (en) * | 2021-04-01 | 2022-10-06 | 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 |
| IL308234A (en) | 2021-05-05 | 2024-01-01 | Huyabio Int Llc | Monotherapy with an SHP2 inhibitor and its uses |
| CA3217084A1 (en) | 2021-05-05 | 2022-11-10 | Farbod Shojaei | Combination therapies comprising shp2 inhibitors and pd-1 inhibitors |
| CN114716448B (zh) * | 2021-05-13 | 2024-01-30 | 中国科学院上海药物研究所 | 抑制shp2活性的杂环化合物、其制备方法及用途 |
| 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 |
| WO2022259157A1 (en) | 2021-06-09 | 2022-12-15 | Novartis Ag | A triple pharmaceutical combination comprising dabrafenib, trametinib and a shp2 inhibitor |
| BR112023025916A2 (pt) | 2021-06-09 | 2024-02-27 | Chugai Pharmaceutical Co Ltd | Combinação de um inibidor de braf e um inibidor de mek, uso de uma combinação, método para o tratamento ou profilaxia de câncer, composições farmacêuticas e invenção |
| 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 |
| CN117916242A (zh) * | 2021-07-09 | 2024-04-19 | 治纳辅医药科技有限公司 | Shp2抑制剂及其用途 |
| CA3226206A1 (en) * | 2021-07-09 | 2023-01-12 | Kanaph Therapeutics Inc. | Shp2 inhibitor and use thereof |
| CA3224341A1 (en) | 2021-09-01 | 2023-03-09 | Novartis Ag | Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers |
| AU2022383040A1 (en) | 2021-11-04 | 2024-03-07 | 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 |
| EP4479398A1 (en) | 2022-02-16 | 2024-12-25 | Amgen Inc. | Quinazoline compounds and use thereof as inhibtors 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 |
| IL316768A (en) | 2022-05-25 | 2025-01-01 | Ikena Oncology Inc | MEK inhibitors and their uses |
| WO2024022244A1 (zh) * | 2022-07-26 | 2024-02-01 | 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 |
| EP4598921A1 (en) | 2022-11-14 | 2025-08-13 | Amgen Inc. | Macrocyclic kras inhibitors and methods of use |
| CN120359214A (zh) | 2022-12-15 | 2025-07-22 | 豪夫迈·罗氏有限公司 | 用于癌症治疗的组合疗法 |
| 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 |
| WO2025194054A1 (en) | 2024-03-14 | 2025-09-18 | Amgen Inc. | Spirocyclic compounds as modulators of kras and uses thereof |
| TW202602882A (zh) | 2024-03-14 | 2026-01-16 | 美商安進公司 | 作為kras調節劑的大環化合物及其用途 |
| 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 |
| WO2026055477A1 (en) | 2024-09-06 | 2026-03-12 | Amgen Inc. | Macrocyclic compounds as modulators of kras and uses thereof |
Family Cites Families (129)
| 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 |
| JP3356291B2 (ja) | 1996-02-07 | 2002-12-16 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | Crfレセプター拮抗薬としてのピラゾロピリミジン類 |
| EP1007042A4 (en) | 1997-06-13 | 2001-07-04 | Sugen Inc | NEW HETEROCYCLIC COMPOUNDS FOR MODULATING THE PROTEIN-TYROSIN-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 |
| CN1231473C (zh) | 2000-02-16 | 2005-12-14 | 神经能质公司 | 取代的芳基吡嗪 |
| WO2003029422A2 (en) | 2001-10-01 | 2003-04-10 | 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 |
| AU2002343557A1 (en) | 2001-11-21 | 2003-06-10 | Pharmacia And Upjohn Company | Substituted aryl 1,4-pyrazine derivatives |
| WO2003082191A2 (en) | 2002-03-28 | 2003-10-09 | Merck & Co., Inc. | Substituted 2,3-diphenyl pyridines |
| US20040116444A1 (en) | 2002-09-12 | 2004-06-17 | Corbett Jeffrey W. | Substituted 1,4-pyrazine derivatives |
| CN1753912B (zh) | 2002-12-23 | 2011-11-02 | 惠氏公司 | 抗pd-1抗体及其用途 |
| 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 |
| WO2005028480A2 (en) | 2003-09-03 | 2005-03-31 | Neurogen Corporation | 5-aryl-pyrazolo[4,3-d]pyrimidines, pyridines, and pyrazines and related compounds |
| CA2541832C (en) | 2003-10-10 | 2009-11-24 | Pfizer Products Inc. | Substituted 2h-[1,2,4]triazolo[4,3-a]pyrazines as gsk-3 inhibitors |
| CA2543644A1 (en) | 2003-10-27 | 2005-05-06 | Astellas Pharma Inc. | Pyrazine derivatives and pharmaceutical use thereof |
| 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 |
| DE102004015954A1 (de) | 2004-04-01 | 2005-11-10 | Ina-Schaeffler Kg | Umschlingungstrieb |
| WO2006002284A1 (en) | 2004-06-22 | 2006-01-05 | Rigel Pharmaceuticals, Inc. | Ubiquitin ligase inhibitors |
| DE602005020981D1 (de) | 2004-12-23 | 2010-06-10 | Mallinckrodt Inc | Fluoreszente pyrazinderivate und verfahren zu deren anwendung bei der bewertung der nierenfunktion |
| CA2598456A1 (en) * | 2005-02-16 | 2006-08-24 | Schering Corporation | Heterocyclic substituted piperazines with cxcr3 antagonist activity |
| CA2606288A1 (en) | 2005-04-18 | 2006-10-26 | Neurogen Corporation | Subtituted heteroaryl cb1 antagonists |
| CN102206216B (zh) | 2005-06-22 | 2014-11-12 | 普莱希科公司 | 作为蛋白质激酶抑制剂的吡咯并[2,3-b]吡啶衍生物 |
| ES2577535T3 (es) | 2005-10-21 | 2016-07-15 | Regents Of The University Of California | Mutaciones del oncogén de C-kit 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 |
| BRPI0710938A2 (pt) * | 2006-04-28 | 2012-06-26 | Univ Northwestern | formulações contendo compostos de piridazina para o tratamento de doenças neuroinflamatórias |
| US7893058B2 (en) | 2006-05-15 | 2011-02-22 | Janssen Pharmaceutica Nv | Imidazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases |
| PT2029602E (pt) | 2006-05-31 | 2010-07-08 | Galapagos Nv | Compostos de triazolopirazina uteis para o tratamento de doenãas degenerativas e inflamatërias |
| AR061229A1 (es) | 2006-06-06 | 2008-08-13 | Schering Corp | Imidazopirazinas como inhibidores de la proteina quinasa |
| WO2008108944A2 (en) | 2007-03-01 | 2008-09-12 | Mallinckrodt Inc. | Integrated photoactive small molecules and uses thereof |
| CN101679418A (zh) | 2007-04-06 | 2010-03-24 | 诺瓦提斯公司 | 用作蛋白质激酶抑制剂的[2,6]萘啶类化合物 |
| US8133895B2 (en) | 2007-05-10 | 2012-03-13 | Janssen Pharmaceutica N.V. | Fused pyrazine compounds useful for the treatment of degenerative and inflammatory diseases |
| US8148369B2 (en) | 2007-05-10 | 2012-04-03 | Janssen Pharmaceutica Nv | Fused pyrazine compounds useful for the treatment of degenerative and inflammatory diseases |
| EP2157090A4 (en) | 2007-06-21 | 2011-09-07 | Taisho Pharmaceutical Co Ltd | PYRAZINAMIDE COMPOUND |
| EP2185154A2 (en) * | 2007-08-03 | 2010-05-19 | 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 |
| US8703770B2 (en) | 2008-10-30 | 2014-04-22 | Merck Sharp & Dohme Corp. | Pyridazine carboxamide orexin receptor antagonists |
| PL2565193T3 (pl) | 2009-01-23 | 2014-07-31 | Rigel Pharmaceuticals Inc | Kompozycje i sposoby hamowania szlaku JAK |
| 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 |
| KR101906146B1 (ko) * | 2009-08-17 | 2018-10-10 | 메모리얼 슬로안-케터링 캔서 센터 | 열 충격 단백질 결합 화합물, 조성물, 및 이의 제조 방법 및 사용 방법 |
| 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 |
| 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 |
| EP2593452B1 (en) | 2010-07-14 | 2017-01-18 | Novartis AG | Ip receptor agonist 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 (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 |
| 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 |
| ES2618004T3 (es) | 2012-08-07 | 2017-06-20 | Merck Patent Gmbh | Derivados de piridopirimidina como inhibidores de proteínas quinasas |
| BR112015010620A2 (pt) | 2012-11-08 | 2017-07-11 | Pfizer | compostos heteroaromáticos e seus usos como ligantes de dopamina d1 |
| JP6272897B2 (ja) | 2012-11-29 | 2018-01-31 | ケモセントリックス,インコーポレイティド | Cxcr7アンタゴニスト |
| WO2014113584A1 (en) | 2013-01-16 | 2014-07-24 | Rhode Island Hospital | Compositions and methods for the prevention and treatment of osteolysis and osteoporosis |
| JP2016507538A (ja) | 2013-02-07 | 2016-03-10 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングMerck Patent Gesellschaft mit beschraenkter Haftung | 置換キノキサリン誘導体およびmGluR4の正のアロステリックモジュレーターとしてのそれらの使用 |
| DK2958943T3 (da) | 2013-02-20 | 2019-12-09 | Univ Pennsylvania | Behandling af cancer ved anvendelse af humaniseret anti-EGFRvIII kimær antigenreceptor |
| CA2902026C (en) | 2013-03-13 | 2023-08-29 | Prothena Biosciences Limited | 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 |
| JP6523303B2 (ja) * | 2014-01-17 | 2019-05-29 | ノバルティス アーゲー | Shp2の活性を阻害するための1−ピリダジン/トリアジン−3−イル−ピペラジン/ピペリジン/ピロリジン誘導体およびその組成物 |
| CN105899493B (zh) * | 2014-01-17 | 2019-03-29 | 诺华股份有限公司 | 用于抑制shp2活性的1-(三嗪-3-基/哒嗪-3-基)-哌(-嗪)啶衍生物及其组合物 |
| JO3517B1 (ar) | 2014-01-17 | 2020-07-05 | Novartis Ag | ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2 |
| US11331312B2 (en) | 2014-04-25 | 2022-05-17 | 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 |
| RU2743074C2 (ru) * | 2014-08-01 | 2021-02-15 | Нуэволюшон А/С | Соединения, активные по отношению к бромодоменам |
| CA2967944C (en) | 2014-11-18 | 2020-11-17 | Merck Sharp & Dohme Corp. | Aminopyrazine compounds with a2a antagonist properties |
| WO2016100116A1 (en) | 2014-12-17 | 2016-06-23 | Siemens Healthcare Diagnostics Inc. | Sandwich assay design for small molecules |
| CA2969090C (en) | 2014-12-23 | 2023-05-02 | Novartis Ag | Triazolopyrimidine compounds and uses thereof |
| US10533016B2 (en) | 2015-01-09 | 2020-01-14 | Revolution Medicines, Inc. | Compounds that participate in cooperative binding and uses thereof |
| CN112353938A (zh) | 2015-02-05 | 2021-02-12 | 特尔诺沃有限公司 | 用于治疗癌症的irs/stat3双重调节剂与抗癌剂的组合 |
| EP3277689B1 (en) | 2015-04-03 | 2019-09-04 | Incyte Corporation | Heterocyclic compounds as lsd1 inhibitors |
| ES2741746T3 (es) | 2015-06-19 | 2020-02-12 | Novartis Ag | Compuestos y composiciones para inhibir la actividad de SHP2 |
| ES2824576T3 (es) | 2015-06-19 | 2021-05-12 | Novartis Ag | Compuestos y composiciones para inhibir la actividad de SHP2 |
| CN112625028B (zh) * | 2015-06-19 | 2024-10-29 | 诺华股份有限公司 | 用于抑制shp2活性的化合物和组合物 |
| 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 |
| WO2017059207A1 (en) | 2015-10-01 | 2017-04-06 | Warp Drive Bio, 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 |
| EA202092441A1 (ru) | 2016-06-07 | 2021-05-21 | Джакобио Фармасьютикалс Ко., Лтд. | Новые гетероциклические производные, применимые в качестве ингибиторов shp2 |
| MX383856B (es) * | 2016-06-14 | 2025-03-14 | Novartis Ag | Compuestos y composiciones para inhibir la actividad de shp2. |
| KR102598895B1 (ko) | 2016-07-12 | 2023-11-07 | 레볼루션 메디슨즈, 인크. | 다른자리 입체성 shp2 억제제로서의 2,5-이치환 3-메틸 피라진 및 2,5,6-3치환 3-메틸 피라진 |
| 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 |
| US20190343836A1 (en) * | 2017-01-10 | 2019-11-14 | Novartis Ag | Pharmaceutical combination comprising an alk inhibitor and a shp2 inhibitor |
| MX2019008695A (es) | 2017-01-23 | 2019-09-11 | Revolution Medicines Inc | Compuestos biciclicos como inhibidores alostericos de shp2. |
| MX2019008696A (es) * | 2017-01-23 | 2019-09-13 | Revolution Medicines Inc | Compuestos de piridina como inhibidores de shp2 alostericos. |
| KR20240026521A (ko) | 2017-03-23 | 2024-02-28 | 자코바이오 파마슈티칼스 컴퍼니 리미티드 | Shp2 억제제로서 유용한 신규한 헤테로환형 유도체 |
| KR20240093922A (ko) | 2017-04-05 | 2024-06-24 | 레볼루션 메디슨즈, 인크. | 단백질-단백질 계면을 분석하기 위한 방법 및 시약 |
| AU2018248417A1 (en) | 2017-04-05 | 2019-11-14 | Revolution Medicines, Inc. | Compounds that participate in cooperative binding and uses thereof |
| WO2018218133A1 (en) | 2017-05-26 | 2018-11-29 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors |
| CA3074690A1 (en) | 2017-09-07 | 2019-03-14 | Revolution Medicines, Inc. | Shp2 inhibitor compositions and methods for treating cancer |
| MX2020003579A (es) | 2017-10-12 | 2020-07-22 | Revolution Medicines Inc | Compuestos de piridina, pirazina, y triazina como inhibidores de shp2 alostericos. |
| BR112020009757A2 (pt) | 2017-12-15 | 2020-11-03 | Revolution Medicines, Inc. | compostos policíclicos como inibidores alostéricos de shp2 |
| CN110156786B (zh) | 2018-02-13 | 2022-06-03 | 青煜医药研发(上海)有限公司 | 嘧啶并环化合物及其制备方法和应用 |
| KR102614939B1 (ko) | 2018-02-13 | 2023-12-19 | 블루레이 테라퓨틱스 (상하이) 컴퍼니 리미티드 | 피리미딘-융합고리 화합물 및 그의 제조방법과 용도 |
| RU2020133727A (ru) * | 2018-03-21 | 2022-04-21 | Сучжоу Пухе Биофарма Ко., Лтд. | Ингибиторы shp2 и их применение |
| SG11202009793TA (en) | 2018-04-10 | 2020-10-29 | Revolution Medicines Inc | Shp2 inhibitor compositions, methods for treating cancer and methods for identifying a subject with shp2 mutations |
| IL300091A (en) | 2018-05-01 | 2023-03-01 | Revolution Medicines Inc | C40-, c28-, and c-32-linked rapamycin analogs as mtor inhibitors |
| 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 |
| WO2020055761A1 (en) | 2018-09-10 | 2020-03-19 | Mirati Therapeutics, Inc. | Combination therapies |
| JP7542538B2 (ja) * | 2018-09-18 | 2024-08-30 | ニカング セラピューティクス, インコーポレイテッド | Srcホモロジー-2ホスファターゼ阻害剤としての縮合三環式環誘導体 |
| WO2020072656A1 (en) | 2018-10-03 | 2020-04-09 | Gilead Sciences, Inc. | Imidozopyrimidine derivatives |
| CN113473990A (zh) | 2018-10-08 | 2021-10-01 | 锐新医药公司 | 用于治疗癌症的shp2抑制剂组合物 |
| JP2022506887A (ja) | 2018-11-07 | 2022-01-17 | シャンハイ リンジーン バイオファーマ カンパニー リミテッド | 窒素含有縮合複素環系shp2阻害剤化合物、製造方法及び使用 |
| 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 |
| CN113272303B (zh) | 2018-11-30 | 2024-09-17 | 上海拓界生物医药科技有限公司 | 嘧啶并五元氮杂环类衍生物、其制备方法及其在医药上的应用 |
| 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 |
| KR20210116479A (ko) | 2018-12-21 | 2021-09-27 | 레볼루션 메디슨즈, 인크. | 공동 결합에 참여하는 화합물 및 그의 용도 |
| CN120699039A (zh) | 2019-11-04 | 2025-09-26 | 锐新医药公司 | Ras抑制剂 |
-
2018
- 2018-10-11 MX MX2020003579A patent/MX2020003579A/es unknown
- 2018-10-11 CA CA3078565A patent/CA3078565A1/en not_active Abandoned
- 2018-10-11 RU RU2020115095A patent/RU2020115095A/ru unknown
- 2018-10-11 EP EP18795913.5A patent/EP3694848A1/en not_active Withdrawn
- 2018-10-11 SG SG11202002941WA patent/SG11202002941WA/en unknown
- 2018-10-11 TW TW107135797A patent/TW201930292A/zh unknown
- 2018-10-11 JP JP2020519790A patent/JP2020536881A/ja active Pending
- 2018-10-11 CN CN201880066291.0A patent/CN111212834B/zh not_active Expired - Fee Related
- 2018-10-11 BR BR112020007058-0A patent/BR112020007058A2/pt not_active Application Discontinuation
- 2018-10-11 KR KR1020207013076A patent/KR20200070295A/ko not_active Ceased
- 2018-10-11 AU AU2018347516A patent/AU2018347516A1/en not_active Abandoned
- 2018-10-11 WO PCT/US2018/055502 patent/WO2019075265A1/en not_active Ceased
-
2020
- 2020-03-27 CO CONC2020/0003714A patent/CO2020003714A2/es unknown
- 2020-03-31 PH PH12020550216A patent/PH12020550216A1/en unknown
- 2020-04-01 IL IL273756A patent/IL273756A/en unknown
- 2020-04-10 US US16/845,539 patent/US11702411B2/en active Active
-
2023
- 2023-04-05 US US18/131,226 patent/US20240067636A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2020536881A5 (https=) | ||
| JP2020506178A5 (https=) | ||
| JP2020505376A5 (https=) | ||
| RU2020115095A (ru) | Пиридиновые, пиразиновые и триазиновые соединения в качестве аллостерических ингибиторов shp2 | |
| WO2018013597A4 (en) | 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors | |
| TW444013B (en) | Quinoline and quinazoline compounds useful in treating benign prostatic hyperplasia | |
| JPWO2021092115A5 (https=) | ||
| IL268030B2 (en) | Bicyclics as allosteric shp2 inhibitors | |
| DE69515702T2 (de) | L-Tertiär-leucin-2-pyridylamid | |
| RU2020123241A (ru) | Полициклические соединения в качестве аллостерических ингибиторов shp2 | |
| JP3397320B2 (ja) | 縮合イミダゾリウム誘導体 | |
| JP2005514398A5 (https=) | ||
| JP2019031560A5 (https=) | ||
| RU2019126455A (ru) | Пиридиновые соединения в качестве аллостерических ингибиторов shp2 | |
| JP2017518959A5 (https=) | ||
| RU2004126671A (ru) | Гетероарилсоединения, полезные в качестве ингибиторов gsk-3 | |
| RU92004336A (ru) | Водорастворимые производные камптотецина, способ их получения, фармацевтическая композиция, способ ингибирования энзима топоизомеразы, промежуточные продукты | |
| JP2020506951A5 (https=) | ||
| JP2016121196A5 (https=) | ||
| JP2021500394A5 (https=) | ||
| KR930000517A (ko) | 이미다조디아제핀 | |
| JP2017519754A5 (https=) | ||
| RU96112103A (ru) | Новые бензоилгуанидины, их получение и применение в лекарственных средствах | |
| JP2009543836A (ja) | インドール化合物 | |
| JP2009534358A5 (https=) |