JP2019527728A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2019527728A5 JP2019527728A5 JP2019522611A JP2019522611A JP2019527728A5 JP 2019527728 A5 JP2019527728 A5 JP 2019527728A5 JP 2019522611 A JP2019522611 A JP 2019522611A JP 2019522611 A JP2019522611 A JP 2019522611A JP 2019527728 A5 JP2019527728 A5 JP 2019527728A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- compound
- tautomer
- solvate
- isomer
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 7
- 239000012453 solvate Substances 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000005101 LEOPARD Syndrome Diseases 0.000 claims 1
- 206010062901 Multiple lentigines syndrome Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 208000037538 Myelomonocytic Juvenile Leukemia Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 206010029748 Noonan syndrome Diseases 0.000 claims 1
- 208000010708 Noonan syndrome with multiple lentigines Diseases 0.000 claims 1
- 102100033019 Tyrosine-protein phosphatase non-receptor type 11 Human genes 0.000 claims 1
- 101710116241 Tyrosine-protein phosphatase non-receptor type 11 Proteins 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000005992 juvenile myelomonocytic leukemia Diseases 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 0 C*(C)CC[C@@]1OCC(CC2)(CCN2c(nc2C)c(CO)nc2Sc2cccc(Cl)c2Cl)[C@@]1N Chemical compound C*(C)CC[C@@]1OCC(CC2)(CCN2c(nc2C)c(CO)nc2Sc2cccc(Cl)c2Cl)[C@@]1N 0.000 description 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021116788A JP7416740B2 (ja) | 2016-07-12 | 2021-07-15 | アロステリックｓｈｐ２阻害剤としての２，５－二置換３－メチルピラジンおよび２，５，６－三置換３－メチルピラジン |
| JP2023177195A JP2024009957A (ja) | 2016-07-12 | 2023-10-13 | アロステリックｓｈｐ２阻害剤としての２，５－二置換３－メチルピラジンおよび２，５，６－三置換３－メチルピラジン |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662361249P | 2016-07-12 | 2016-07-12 | |
| US62/361,249 | 2016-07-12 | ||
| US201762449523P | 2017-01-23 | 2017-01-23 | |
| US62/449,523 | 2017-01-23 | ||
| PCT/US2017/041577 WO2018013597A1 (en) | 2016-07-12 | 2017-07-11 | 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021116788A Division JP7416740B2 (ja) | 2016-07-12 | 2021-07-15 | アロステリックｓｈｐ２阻害剤としての２，５－二置換３－メチルピラジンおよび２，５，６－三置換３－メチルピラジン |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019527728A JP2019527728A (ja) | 2019-10-03 |
| JP2019527728A5 true JP2019527728A5 (https=) | 2021-07-26 |
| JP6916279B2 JP6916279B2 (ja) | 2021-08-11 |
Family
ID=59383648
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019522611A Active JP6916279B2 (ja) | 2016-07-12 | 2017-07-11 | アロステリックｓｈｐ２阻害剤としての２，５−二置換３−メチルピラジンおよび２，５，６−三置換３−メチルピラジン |
| JP2021116788A Active JP7416740B2 (ja) | 2016-07-12 | 2021-07-15 | アロステリックｓｈｐ２阻害剤としての２，５－二置換３－メチルピラジンおよび２，５，６－三置換３－メチルピラジン |
| JP2023177195A Pending JP2024009957A (ja) | 2016-07-12 | 2023-10-13 | アロステリックｓｈｐ２阻害剤としての２，５－二置換３－メチルピラジンおよび２，５，６－三置換３－メチルピラジン |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021116788A Active JP7416740B2 (ja) | 2016-07-12 | 2021-07-15 | アロステリックｓｈｐ２阻害剤としての２，５－二置換３－メチルピラジンおよび２，５，６－三置換３－メチルピラジン |
| JP2023177195A Pending JP2024009957A (ja) | 2016-07-12 | 2023-10-13 | アロステリックｓｈｐ２阻害剤としての２，５－二置換３－メチルピラジンおよび２，５，６－三置換３－メチルピラジン |
Country Status (22)
| Country | Link |
|---|---|
| US (3) | US10590090B2 (https=) |
| EP (2) | EP4302834A3 (https=) |
| JP (3) | JP6916279B2 (https=) |
| KR (2) | KR102598895B1 (https=) |
| CN (3) | CN109983001B (https=) |
| AU (3) | AU2017296289A1 (https=) |
| CA (1) | CA3030167A1 (https=) |
| CL (1) | CL2019000090A1 (https=) |
| CO (1) | CO2019000613A2 (https=) |
| CR (1) | CR20190063A (https=) |
| DO (1) | DOP2019000005A (https=) |
| EC (1) | ECSP19010079A (https=) |
| IL (3) | IL321811A (https=) |
| MA (1) | MA45660A (https=) |
| MX (2) | MX395351B (https=) |
| MY (1) | MY199046A (https=) |
| PE (1) | PE20190624A1 (https=) |
| PH (1) | PH12019500056B1 (https=) |
| SG (1) | SG11201900157RA (https=) |
| TN (1) | TN2019000010A1 (https=) |
| TW (2) | TWI912604B (https=) |
| WO (1) | WO2018013597A1 (https=) |
Families Citing this family (149)
| 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 |
| WO2017210134A1 (en) | 2016-05-31 | 2017-12-07 | Board Of Regents, University Of Texas System | Heterocyclic inhibitors of ptpn11 |
| MX388576B (es) | 2016-06-07 | 2025-03-20 | Jacobio Pharmaceuticals Co Ltd | Derivados heterociclicos novedosos utiles como inhibidores de shp2. |
| WO2017216706A1 (en) | 2016-06-14 | 2017-12-21 | Novartis Ag | Compounds and compositions for inhibiting the activity of shp2 |
| EP4302834A3 (en) * | 2016-07-12 | 2024-07-17 | Revolution Medicines, Inc. | 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors |
| WO2018057884A1 (en) | 2016-09-22 | 2018-03-29 | 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 |
| KR20190110588A (ko) | 2017-01-23 | 2019-09-30 | 레볼루션 메디슨즈, 인크. | 알로스테릭 shp2 억제제로서의 피리딘 화합물 |
| JP7240319B2 (ja) | 2017-01-23 | 2023-03-15 | レヴォリューション・メディスンズ，インコーポレイテッド | アロステリックｓｈｐ２阻害剤としての二環式化合物 |
| EA202190196A1 (ru) * | 2017-03-23 | 2021-08-31 | Джакобио Фармасьютикалс Ко., Лтд. | Новые гетероциклические производные, применимые в качестве ингибиторов shp2 |
| BR102018007822A2 (pt) | 2017-04-20 | 2018-11-06 | Gilead Sciences, Inc. | composto, métodos para inibir pd-1, pd-l1 e/ou interação de pd-1/pd-l1 e para tratamento de câncer, composição farmacêutica, e, kit para tratamento de ou prevenção de câncer ou uma doença ou condição |
| EP3630770B1 (en) | 2017-05-26 | 2024-08-28 | 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 |
| 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 |
| TW201930292A (zh) | 2017-10-12 | 2019-08-01 | 美商銳新醫藥公司 | 作為變構ｓｈｐ２抑制劑的吡啶、吡嗪和三嗪化合物 |
| JP7361693B2 (ja) | 2017-12-15 | 2023-10-16 | レヴォリューション・メディスンズ，インコーポレイテッド | アロステリックｓｈｐ２阻害剤としての多環式化合物 |
| 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 |
| CR20200347A (es) | 2018-02-13 | 2020-09-23 | Gilead Sciences Inc | Inhibidores pd-1/pd-l1 |
| CN110655520A (zh) * | 2018-06-29 | 2020-01-07 | 上海青煜医药科技有限公司 | 嘧啶并环化合物及其制备方法和应用 |
| JP7335882B2 (ja) * | 2018-02-13 | 2023-08-30 | ブルーレイ セラピューティクス （シャンハイ） カンパニー，リミティド | ピリミジン縮合環式化合物及びその製造方法、並びに使用 |
| AU2019240299B2 (en) * | 2018-03-21 | 2023-06-22 | D.E. Shaw Research, Llc | 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 |
| US12138263B2 (en) | 2018-03-21 | 2024-11-12 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine SHP2 phosphatase inhibitors and methods of use thereof |
| MX2020010719A (es) * | 2018-04-10 | 2020-11-06 | Revolution Medicines Inc | Composiciones de inhibidores de shp2, metodos para tratar el cancer y metodos para identificar a un sujeto con mutaciones en shp2. |
| MX2020011528A (es) * | 2018-05-02 | 2021-02-09 | Navire Pharma Inc | Inhibidores heterociclicos sustituidos de ptpn11. |
| SG11202012425QA (en) | 2018-07-13 | 2021-01-28 | Gilead Sciences Inc | Pd-1/pd-l1 inhibitors |
| CN112601750B (zh) | 2018-08-10 | 2023-10-31 | 纳维尔制药有限公司 | Ptpn11（shp2）抑制剂 |
| CR20210175A (es) * | 2018-09-18 | 2021-06-01 | Nikang Therapeutics Inc | Derivados de anillo tricíclico condensado como inhibidores de la fosfatasa de homología a src 2 (shp2) |
| US20210393623A1 (en) | 2018-09-26 | 2021-12-23 | Jacobio Pharmaceuticals Co., Ltd. | Novel Heterocyclic Derivatives Useful as SHP2 Inhibitors |
| CN112867718B (zh) * | 2018-09-29 | 2025-03-04 | 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 |
| EP3860717A1 (en) | 2018-10-03 | 2021-08-11 | Gilead Sciences, Inc. | Imidozopyrimidine derivatives |
| JP2022508651A (ja) * | 2018-10-08 | 2022-01-19 | レヴォリューション・メディスンズ，インコーポレイテッド | 癌を処置するためのｓｈｐ２阻害剤組成物および方法 |
| TW202028183A (zh) * | 2018-10-10 | 2020-08-01 | 大陸商江蘇豪森藥業集團有限公司 | 含氮雜芳類衍生物調節劑、其製備方法和應用 |
| BR112021005733A2 (pt) | 2018-10-17 | 2021-07-27 | Array Biopharma Inc. | inibidores de proteína tirosina fosfatase |
| CN109265352B (zh) * | 2018-10-31 | 2021-06-04 | 杭州迈世腾药物科技有限公司 | 芳基环丙基醚及其衍生物的制备方法 |
| EP3889153A4 (en) | 2018-11-30 | 2022-09-07 | Tuojie Biotech (Shanghai) Co., Ltd. | PYRIMIDINE AND FIVE-MEMBERED HETEROCYCLIC NITROGEN DERIVATIVE, METHOD OF MANUFACTURE THEREOF AND MEDICAL USES THEREOF |
| WO2020156242A1 (zh) * | 2019-01-31 | 2020-08-06 | 贝达药业股份有限公司 | Shp2抑制剂及其应用 |
| MX2021010323A (es) | 2019-03-01 | 2021-12-10 | Revolution Medicines Inc | Compuestos bicíclicos de heterociclilo y usos de este. |
| MX2021010319A (es) | 2019-03-01 | 2021-12-10 | Revolution Medicines Inc | Compuestos biciclicos de heteroarilo y usos de estos. |
| 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 |
| US11033547B2 (en) | 2019-03-07 | 2021-06-15 | Merck Patent Gmbh | Carboxamide-pyrimidine derivatives as SHP2 antagonists |
| CU20210080A7 (es) | 2019-04-02 | 2022-05-11 | Array Biopharma Inc | Triazinas sustituidas como inhibidores de proteína tirosina fosfatasa |
| JP7586834B2 (ja) | 2019-04-08 | 2024-11-19 | 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 | Ｓｈｐ２拮抗薬としてのピリミジノン誘導体 |
| CN115141205A (zh) | 2019-06-07 | 2022-10-04 | 锐新医药公司 | Shp2抑制剂的固体形式 |
| KR20220054285A (ko) | 2019-06-28 | 2022-05-02 | 투오지에 바이오텍 (상하이) 컴퍼니 리미티드 | 피리미딘 5 원 질소 헤테로고리형 유도체, 이의 제조 방법 및 이의 약학적 용도 |
| CN111704611B (zh) * | 2019-07-25 | 2022-01-14 | 上海凌达生物医药有限公司 | 一类芳基螺环类shp2抑制剂化合物、制备方法和用途 |
| 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 |
| GB201911928D0 (en) | 2019-08-20 | 2019-10-02 | Otsuka Pharma Co Ltd | Pharmaceutical compounds |
| WO2021043077A1 (zh) * | 2019-09-06 | 2021-03-11 | 四川科伦博泰生物医药股份有限公司 | 一种取代吡嗪化合物、其制备方法和用途 |
| CN114502165A (zh) * | 2019-09-23 | 2022-05-13 | 苏州浦合医药科技有限公司 | Shp2抑制剂及其用途 |
| MX2022003454A (es) | 2019-09-24 | 2022-04-19 | Relay Therapeutics Inc | Inhibidores de fosfatasa shp2 y metodos para su fabricacion y uso. |
| 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 |
| US20240139193A1 (en) | 2019-10-15 | 2024-05-02 | Amgen Inc. | Combination therapy of kras inhibitor and shp2 inhibitor for treatment of cancers |
| IL322454A (en) | 2019-11-04 | 2025-09-01 | Revolution Medicines Inc | ras inhibitors |
| TW202132316A (zh) | 2019-11-04 | 2021-09-01 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| AU2020377925A1 (en) | 2019-11-04 | 2022-05-05 | Revolution Medicines, Inc. | Ras inhibitors |
| CA3156359A1 (en) | 2019-11-08 | 2021-05-14 | Adrian Liam Gill | Bicyclic heteroaryl compounds and uses thereof |
| EP4065231A1 (en) | 2019-11-27 | 2022-10-05 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
| EP4069301A1 (en) | 2019-12-04 | 2022-10-12 | Bayer Aktiengesellschaft | Inhibitors of shp2 |
| WO2021142026A1 (en) | 2020-01-07 | 2021-07-15 | Revolution Medicines, Inc. | Shp2 inhibitor dosing and methods of treating cancer |
| 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 |
| CN113135910A (zh) | 2020-01-19 | 2021-07-20 | 北京诺诚健华医药科技有限公司 | 嘧啶-4(3h)-酮类杂环化合物、其制备方法及其在医药学上的应用 |
| CN114846005B (zh) * | 2020-01-21 | 2024-04-02 | 贝达药业股份有限公司 | Shp2抑制剂及其应用 |
| EP4110338A1 (en) | 2020-02-28 | 2023-01-04 | Novartis AG | A triple pharmaceutical combination comprising dabrafenib, an erk inhibitor and a shp2 inhibitor |
| CN113493440B (zh) * | 2020-04-03 | 2024-08-23 | 上海翰森生物医药科技有限公司 | 含氮杂芳类衍生物的盐及其晶型 |
| TW202144334A (zh) * | 2020-04-03 | 2021-12-01 | 大陸商上海翰森生物醫藥科技有限公司 | 含氮雜芳類衍生物游離鹼的晶型 |
| CN115362149B (zh) * | 2020-04-26 | 2024-05-14 | 贝达药业股份有限公司 | Shp2抑制剂及其组合物和应用 |
| CA3181898A1 (en) * | 2020-06-11 | 2021-12-16 | Bang Fu | Shp2 inhibitors, compositions and uses thereof |
| IL299131A (en) | 2020-06-18 | 2023-02-01 | Revolution Medicines Inc | Methods for delaying, preventing and treating acquired resistance to RAS inhibitors |
| JP2023530838A (ja) | 2020-06-22 | 2023-07-20 | スーチュアン・コールン－バイオテック・バイオファーマシューティカル・カンパニー・リミテッド | 置換されたピラジン化合物、当該化合物を含む医薬組成物、及びその使用 |
| US12441737B2 (en) | 2020-07-08 | 2025-10-14 | Novartis Ag | Manufacture of compounds and compositions for inhibiting the activity of SHP2 |
| WO2022042331A1 (zh) * | 2020-08-25 | 2022-03-03 | 四川科伦博泰生物医药股份有限公司 | 杂环化合物及其制备方法和用途 |
| US20250195521A1 (en) | 2020-09-03 | 2025-06-19 | Revolution Medicines, Inc. | Use of sos1 inhibitors to treat malignancies with shp2 mutations |
| CA3194067A1 (en) | 2020-09-15 | 2022-03-24 | Revolution Medicines, Inc. | Ras inhibitors |
| US20240059703A1 (en) | 2020-10-20 | 2024-02-22 | Amgen Inc. | Heterocyclic spiro compounds and methods of use |
| WO2022093856A1 (en) | 2020-10-27 | 2022-05-05 | Amgen Inc. | Heterocyclic spiro compounds and methods of use |
| CN116848121A (zh) * | 2020-12-18 | 2023-10-03 | 建新公司 | 制备shp2抑制剂的方法 |
| TW202241907A (zh) * | 2020-12-18 | 2022-11-01 | 美商瑞佛路森醫藥公司 | 製備shp2抑制劑之方法 |
| JP7849366B2 (ja) | 2020-12-22 | 2026-04-21 | キル・レガー・セラピューティクス・インコーポレーテッド | Ｓｏｓ１阻害剤およびその使用 |
| 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 |
| WO2022206684A1 (zh) * | 2021-03-31 | 2022-10-06 | 南京明德新药研发有限公司 | 一系列含Se的吡嗪类化合物及其应用 |
| US20240190843A1 (en) * | 2021-04-01 | 2024-06-13 | 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 |
| MX2023012725A (es) | 2021-04-29 | 2024-09-23 | Amgen Inc | Compuestos de 2-aminobenzotiazol y metodos de uso de los mismos. |
| 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 |
| TW202309052A (zh) | 2021-05-05 | 2023-03-01 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| KR20240017811A (ko) | 2021-05-05 | 2024-02-08 | 레볼루션 메디슨즈, 인크. | 암의 치료를 위한 ras 억제제 |
| JP2024516997A (ja) | 2021-05-05 | 2024-04-18 | フヤバイオ インターナショナル，エルエルシー | Ｓｈｐ２阻害剤単独療法およびその使用 |
| CN117177752A (zh) | 2021-05-05 | 2023-12-05 | 诺华股份有限公司 | 用于治疗mpnst的化合物和组合物 |
| IL308222A (en) | 2021-05-05 | 2024-01-01 | Huyabio Int Llc | Combination therapies that include SHP2 inhibitors and PD-1 inhibitors |
| AU2022274936B2 (en) * | 2021-05-13 | 2025-08-21 | Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences | Heterocyclic compound for inhibiting shp2 activity, preparation method therefor and use thereof |
| WO2022242767A1 (zh) | 2021-05-21 | 2022-11-24 | 石药集团中奇制药技术（石家庄）有限公司 | 螺环类化合物及其用途 |
| WO2022259157A1 (en) | 2021-06-09 | 2022-12-15 | Novartis Ag | A triple pharmaceutical combination comprising dabrafenib, trametinib and a shp2 inhibitor |
| 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 |
| CN113636952B (zh) * | 2021-07-19 | 2023-07-21 | 河南农业大学 | 一种制备4-溴苯甲酰胺的方法 |
| EP4385991A4 (en) * | 2021-08-09 | 2025-10-01 | Ubix Therapeutics Inc | COMPOUND HAVING SHP2 PROTEIN DEGRADING ACTIVITY AND ITS MEDICAL USES |
| KR20240055778A (ko) | 2021-09-01 | 2024-04-29 | 노파르티스 아게 | Tead 억제제를 포함하는 제약 조합물 및 암의 치료를 위한 이의 용도 |
| WO2023046198A1 (zh) * | 2021-09-27 | 2023-03-30 | 中国医药研究开发中心有限公司 | 磺胺酮类化合物及其制备方法和医药用途 |
| 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 |
| EP4479398A1 (en) | 2022-02-16 | 2024-12-25 | Amgen Inc. | Quinazoline compounds and use thereof as inhibtors of mutant kras proteins |
| MX2024010045A (es) | 2022-02-16 | 2024-08-26 | Amgen Inc | Compuestos de quinazolina y uso de los mismos como inhibidores de proteinas mutantes kras. |
| EP4486345A1 (en) | 2022-03-04 | 2025-01-08 | Eli Lilly and Company | Method of treatment including kras g12c inhibitors and shp2 inhibitors |
| JP2025510572A (ja) | 2022-03-08 | 2025-04-15 | レボリューション メディシンズ インコーポレイテッド | 免疫不応性肺癌を治療するための方法 |
| WO2023169170A1 (zh) * | 2022-03-10 | 2023-09-14 | 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 |
| EP4496566A1 (en) | 2022-03-21 | 2025-01-29 | Institut National de la Santé et de la Recherche Médicale (INSERM) | Use of shp2 inhibitors for inhibiting senescence |
| CN118871443A (zh) * | 2022-03-28 | 2024-10-29 | 建新公司 | 用于制备shp2抑制剂的方法 |
| US11878958B2 (en) | 2022-05-25 | 2024-01-23 | Ikena Oncology, Inc. | MEK inhibitors and uses thereof |
| WO2023240263A1 (en) | 2022-06-10 | 2023-12-14 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| WO2024015360A1 (en) | 2022-07-11 | 2024-01-18 | Amgen Inc. | Methods of treating cancer |
| EP4573095A1 (en) | 2022-08-17 | 2025-06-25 | Treeline Biosciences, Inc. | Pyridopyrimidine kras inhibitors |
| 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 |
| AU2023382606A1 (en) | 2022-11-14 | 2025-05-08 | Amgen Inc. | Macrocyclic kras inhibitors and methods of use |
| WO2024113194A1 (en) * | 2022-11-30 | 2024-06-06 | Canwell Biotech Limited | Shp2 inhibitors, compositions and methods thereof |
| AU2024241633A1 (en) | 2023-03-30 | 2025-11-06 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| AR132338A1 (es) | 2023-04-07 | 2025-06-18 | Revolution Medicines Inc | Inhibidores de ras |
| CR20250420A (es) | 2023-04-07 | 2025-11-20 | Revolution Medicines Inc | Inhibidores macrocíclicos de ras |
| CN121464140A (zh) | 2023-04-14 | 2026-02-03 | 锐新医药公司 | Ras抑制剂的结晶形式、含有其的组合物及其使用方法 |
| CN121100123A (zh) | 2023-04-14 | 2025-12-09 | 锐新医药公司 | Ras抑制剂的结晶形式 |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| TW202528315A (zh) | 2023-09-21 | 2025-07-16 | 美商樹線生物科學公司 | 螺環二氫哌喃并吡啶ＫＲａｓ抑制劑 |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras 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 |
| TW202542151A (zh) | 2023-12-22 | 2025-11-01 | 美商銳格醫藥有限公司 | Ｓｏｓ１抑制劑及其用途 |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| 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 |
| TW202547461A (zh) | 2024-05-17 | 2025-12-16 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| WO2025245127A1 (en) | 2024-05-21 | 2025-11-27 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026055477A1 (en) | 2024-09-06 | 2026-03-12 | Amgen Inc. | Macrocyclic compounds as modulators of kras and uses thereof |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
| CN119661551B (zh) * | 2024-12-16 | 2025-11-25 | 重庆大学 | 一种(3r,4s)-3-甲基-2-氧杂-8-氮杂螺[4.5]癸烷-4-胺盐酸盐的制备方法 |
Family Cites Families (125)
| 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 |
| 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 |
| EP0579835A4 (en) | 1991-11-12 | 1994-06-01 | Nippon Soda Co | 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 |
| AU713673B2 (en) | 1996-02-07 | 1999-12-09 | Neurocrine Biosciences Inc. | Pyrazolopyrimidines as crf receptor antagonists |
| CA2293400A1 (en) * | 1997-06-13 | 1998-12-17 | Gerald Mcmahon | Novel heteroaryl compounds for the modulation of protein tyrosine enzyme related cellular signal transduction |
| WO2001016097A1 (en) | 1999-08-27 | 2001-03-08 | Sugen, Inc. | Phosphate mimics and methods of treatment using phosphatase inhibitors |
| PL365238A1 (en) | 2000-02-16 | 2004-12-27 | Neurogen Corporation | Substituted arylpyrazines |
| TWI316055B (https=) | 2001-04-26 | 2009-10-21 | Nippon Shinyaku Co Ltd | |
| 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 |
| BR0214309A (pt) | 2001-11-21 | 2004-10-13 | Upjohn Co | Derivados aril-1,4-pirazina substituìdos |
| EP1492784A4 (en) | 2002-03-28 | 2006-03-29 | Merck & Co Inc | SUBSTITUTED 2,3-DIPHENYLPYRIDINES |
| JP2005533014A (ja) | 2002-04-26 | 2005-11-04 | ファルマシア・アンド・アップジョン・カンパニー・エルエルシー | 置換ピラジン誘導体 |
| US20040116444A1 (en) * | 2002-09-12 | 2004-06-17 | Corbett Jeffrey W. | Substituted 1,4-pyrazine derivatives |
| CN101899114A (zh) | 2002-12-23 | 2010-12-01 | 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 |
| JP2006525993A (ja) | 2003-05-09 | 2006-11-16 | ファルマシア・アンド・アップジョン・カンパニー・エルエルシー | Ｃｒｆ１受容体拮抗剤である化合物 |
| 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 |
| US7326706B2 (en) * | 2003-08-15 | 2008-02-05 | Bristol-Myers Squibb Company | Pyrazine modulators of cannabinoid receptors |
| CA2537916A1 (en) | 2003-09-03 | 2005-03-31 | Neurogen Corporation | 5-aryl-pyrazolo[4,3-d]pyrimidines, pyridines, and pyrazines and related compounds |
| BRPI0415185A (pt) | 2003-10-10 | 2006-11-28 | Pfizer Prod Inc | 2h-[1,2,4]triazol[4,3-a]pirazinas substituìdas como inibidores da gsk-3 |
| CA2543644A1 (en) * | 2003-10-27 | 2005-05-06 | Astellas Pharma Inc. | Pyrazine derivatives and pharmaceutical use thereof |
| WO2005095384A1 (en) | 2004-04-01 | 2005-10-13 | Astellas Pharma Inc. | Pyrazine derivatives and pharmaceutical use thereof as adenosine antagonists |
| DE102004015954A1 (de) * | 2004-04-01 | 2005-11-10 | Ina-Schaeffler Kg | Umschlingungstrieb |
| US20050282818A1 (en) | 2004-06-22 | 2005-12-22 | Rigel Pharmaceuticals, Inc. | Ubiquitin ligase inhibitors |
| AU2005322114A1 (en) | 2004-12-23 | 2006-07-06 | Mallinckrodt Llc | Fluorescent pyrazine derivatives and methods of using the same in assessing renal function |
| TW200716594A (en) * | 2005-04-18 | 2007-05-01 | Neurogen Corp | Substituted heteroaryl CB1 antagonists |
| UA95244C2 (ru) | 2005-06-22 | 2011-07-25 | Плексикон, Инк. | Соединения и способ модулирования активности киназ, и показания для их применения |
| EP1948827B1 (en) | 2005-10-21 | 2016-03-23 | The Regents of The University of California | C-kit oncogene mutations in melanoma |
| CA2616147A1 (en) * | 2006-02-24 | 2007-09-20 | Mallinckrodt Inc. | Process for using optical agents |
| 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 |
| PT2029602E (pt) | 2006-05-31 | 2010-07-08 | Galapagos Nv | Compostos de triazolopirazina uteis para o tratamento de doenãas degenerativas e inflamatërias |
| EP2029605A1 (en) | 2006-06-06 | 2009-03-04 | Schering Corporation | Imidazopyrazines as protein kinase inhibitors |
| 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 |
| 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 |
| WO2008138843A1 (en) | 2007-05-10 | 2008-11-20 | Galapagos N.V. | Imidazopyridines and triazolopyrimidines useful for the treatment of joint degenerative & 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 |
| CA2695621A1 (en) | 2007-08-09 | 2009-02-12 | Merck Sharp & Dohme Corp. | Pyridine carboxamide orexin receptor antagonists |
| US20090062277A1 (en) | 2007-08-21 | 2009-03-05 | Essa Hu | Phosphodiesterase 10 inhibitors |
| JP2010031249A (ja) * | 2008-06-23 | 2010-02-12 | Sumitomo Chemical Co Ltd | 組成物及び該組成物を用いてなる発光素子 |
| WO2010011666A2 (en) | 2008-07-21 | 2010-01-28 | 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 |
| CA2743449C (en) * | 2008-11-12 | 2016-10-18 | Ariad Pharmaceuticals, Inc. | Pyrazinopyrazines and derivatives as kinase inhibitors |
| BRPI1006942A2 (pt) | 2009-01-23 | 2016-04-12 | Rigel Pharmaceuticals Inc | composto, composição farmacêutica, kit, métodos para inibir uma atividade de uma jak quinase, para tratar uma doença, para tratar a rejeição de transplante de aloenxerto em um receptor de transplante, para tratar uma reação de hipersensibilidade, e para inibir uma cascata de transdução de sinal, e, uso do composto |
| WO2010121212A2 (en) | 2009-04-17 | 2010-10-21 | H. Lee Moffit Cancer Center And Research Institute, Inc. | Indoline scaffold shp-2 inhibitors and method of treating cancer |
| EP2438041A4 (en) | 2009-06-01 | 2012-11-21 | Merck Sharp & Dohme | PYRAZINE-carboxamide-orexin receptor Antagonist |
| NZ713361A (en) * | 2009-08-17 | 2017-06-30 | Memorial Sloan Kettering Cancer Center | Heat shock protein binding compounds, compositions, and methods for making and using same |
| US8163283B2 (en) | 2009-09-03 | 2012-04-24 | 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 |
| JP5989547B2 (ja) | 2010-03-05 | 2016-09-07 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | ヒトｃｓｆ−１ｒに対する抗体及びその使用 |
| WO2011143148A1 (en) | 2010-05-11 | 2011-11-17 | Sanofi | Substituted n-heteroaryl spirolactam bipyrrolidines, preparation and therapeutic use thereof |
| US8703768B2 (en) | 2010-06-09 | 2014-04-22 | Hoffmann-La Roche Inc. | Nitrogen containing heteroaryl compounds |
| PT2593452T (pt) | 2010-07-14 | 2017-04-24 | Novartis Ag | Compostos heterocíclicos agonistas do receptor ip |
| 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 |
| US20150005311A1 (en) * | 2012-01-13 | 2015-01-01 | Novartis Ag | IP receptor agonist heterocyclic compounds |
| EA026353B1 (ru) | 2012-01-17 | 2017-03-31 | Астеллас Фарма Инк. | Соединение пиразинкарбоксамида |
| JP6374384B2 (ja) | 2012-08-07 | 2018-08-15 | 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 | プロテインキナーゼ阻害剤としてのピリドピリミジン誘導体 |
| CA2890009C (en) | 2012-11-08 | 2017-11-28 | Pfizer Inc. | Heteroaromatic compounds and their use as dopamine d1 ligands |
| MX359651B (es) | 2012-11-29 | 2018-10-05 | Chemocentryx Inc | Antagonistas de cxcr7. |
| WO2014113584A1 (en) | 2013-01-16 | 2014-07-24 | Rhode Island Hospital | Compositions and methods for the prevention and treatment of osteolysis and osteoporosis |
| WO2014121885A1 (en) * | 2013-02-07 | 2014-08-14 | Merck Patent Gmbh | Substituted quinoxaline derivatives and their use as positive allosteric modulators of mglur4 |
| JP6647868B2 (ja) | 2013-02-20 | 2020-02-14 | ノバルティス アーゲー | ヒト化抗ＥＧＦＲｖＩＩＩキメラ抗原受容体を用いたがんの処置 |
| US10501531B2 (en) | 2013-03-13 | 2019-12-10 | 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 |
| JO3517B1 (ar) | 2014-01-17 | 2020-07-05 | Novartis Ag | ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2 |
| ES2699351T3 (es) | 2014-01-17 | 2019-02-08 | Novartis Ag | Derivados de 1-piridazin/triazin-3-il-piper(-azina)/idina/pirolidina y composiciones de las mismas para inhibir la actividad de 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 |
| WO2016007731A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyridines and imidazopyrazines as lsd1 inhibitors |
| JP6759514B2 (ja) | 2014-08-01 | 2020-09-23 | ヌエヴォリューション・アクティーゼルスカブＮｕｅｖｏｌｕｔｉｏｎ Ａ／Ｓ | ブロモドメインに対して活性な化合物 |
| AU2015311805B2 (en) * | 2014-09-05 | 2020-04-02 | Celgene Quanticel Research, Inc. | Inhibitors of lysine specific demethylase-1 |
| US10472347B2 (en) * | 2014-11-18 | 2019-11-12 | 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 |
| UY36462A (es) | 2014-12-23 | 2016-07-29 | Novartis Ag | Compuestos de triazolopirimidina y usos de los mismos |
| EP3247378B8 (en) | 2015-01-09 | 2023-08-23 | Revolution Medicines, Inc. | Macrocyclic compounds that participate in cooperative binding and medical uses thereof |
| TW201706265A (zh) * | 2015-03-09 | 2017-02-16 | 必治妥美雅史谷比公司 | 做為Ｒｈｏ激酶（ＲＯＣＫ）抑制劑之內醯胺 |
| EP3277689B1 (en) | 2015-04-03 | 2019-09-04 | Incyte Corporation | Heterocyclic compounds as lsd1 inhibitors |
| US10287266B2 (en) * | 2015-06-19 | 2019-05-14 | 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 |
| EP3310779B1 (en) | 2015-06-19 | 2019-05-08 | 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 |
| WO2017079723A1 (en) | 2015-11-07 | 2017-05-11 | Board Of Regents, The University Of Texas System | Targeting proteins for degradation |
| WO2017156397A1 (en) | 2016-03-11 | 2017-09-14 | Board Of Regents, The University Of Texas Sysytem | Heterocyclic inhibitors of ptpn11 |
| MX388576B (es) * | 2016-06-07 | 2025-03-20 | Jacobio Pharmaceuticals Co Ltd | Derivados heterociclicos novedosos utiles como inhibidores de shp2. |
| WO2017216706A1 (en) | 2016-06-14 | 2017-12-21 | Novartis Ag | Compounds and compositions for inhibiting the activity of shp2 |
| EP4302834A3 (en) * | 2016-07-12 | 2024-07-17 | Revolution Medicines, Inc. | 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors |
| WO2018057884A1 (en) | 2016-09-22 | 2018-03-29 | 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 |
| CA3048340A1 (en) | 2017-01-10 | 2018-07-19 | Novartis Ag | Pharmaceutical combination comprising an alk inhibitor and a shp2 inhibitor |
| KR20190110588A (ko) | 2017-01-23 | 2019-09-30 | 레볼루션 메디슨즈, 인크. | 알로스테릭 shp2 억제제로서의 피리딘 화합물 |
| JP7240319B2 (ja) | 2017-01-23 | 2023-03-15 | レヴォリューション・メディスンズ，インコーポレイテッド | アロステリックｓｈｐ２阻害剤としての二環式化合物 |
| EA202190196A1 (ru) | 2017-03-23 | 2021-08-31 | Джакобио Фармасьютикалс Ко., Лтд. | Новые гетероциклические производные, применимые в качестве ингибиторов shp2 |
| IL269779B2 (en) | 2017-04-05 | 2026-04-01 | Revolution Medicines Inc | Methods and reagents for the analysis of protein-protein interfaces |
| CA3058953A1 (en) | 2017-04-05 | 2018-10-11 | Revolution Medicines, Inc. | Compounds that participate in cooperative binding and uses thereof |
| EP3630770B1 (en) | 2017-05-26 | 2024-08-28 | 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 |
| TW201930292A (zh) | 2017-10-12 | 2019-08-01 | 美商銳新醫藥公司 | 作為變構ｓｈｐ２抑制劑的吡啶、吡嗪和三嗪化合物 |
| JP7361693B2 (ja) | 2017-12-15 | 2023-10-16 | レヴォリューション・メディスンズ，インコーポレイテッド | アロステリックｓｈｐ２阻害剤としての多環式化合物 |
| 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 |
| 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 |
| RU2020133727A (ru) | 2018-03-21 | 2022-04-21 | Сучжоу Пухе Биофарма Ко., Лтд. | Ингибиторы shp2 и их применение |
| MX2020010719A (es) | 2018-04-10 | 2020-11-06 | Revolution Medicines Inc | Composiciones de inhibidores de shp2, metodos para tratar el cancer y metodos para identificar a un sujeto con mutaciones en shp2. |
| MX2020011565A (es) | 2018-05-01 | 2021-01-29 | Revolution Medicines Inc | Analogos de rapamicina ligados a c40, c28 y c-32 como inhibidores de mtor. |
| IL312291A (en) | 2018-05-01 | 2024-06-01 | Revolution Medicines Inc | C-26-linked rapamycin analogs as MTOR inhibitors |
| EP3849535A4 (en) | 2018-09-10 | 2022-06-29 | Mirati Therapeutics, Inc. | Combination therapies |
| CR20210175A (es) | 2018-09-18 | 2021-06-01 | Nikang Therapeutics Inc | Derivados de anillo tricíclico condensado como inhibidores de la fosfatasa de homología a src 2 (shp2) |
| JP2022508651A (ja) | 2018-10-08 | 2022-01-19 | レヴォリューション・メディスンズ，インコーポレイテッド | 癌を処置するためのｓｈｐ２阻害剤組成物および方法 |
| 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 |
| BR112021012057A2 (pt) | 2018-12-21 | 2021-10-19 | Revolution Medicines, Inc. | Compostos que participam de ligação cooperativa e usos dos mesmos |
| IL322454A (en) | 2019-11-04 | 2025-09-01 | Revolution Medicines Inc | ras inhibitors |
-
2017
- 2017-07-11 EP EP23209237.9A patent/EP4302834A3/en active Pending
- 2017-07-11 WO PCT/US2017/041577 patent/WO2018013597A1/en not_active Ceased
- 2017-07-11 JP JP2019522611A patent/JP6916279B2/ja active Active
- 2017-07-11 MY MYPI2018003070A patent/MY199046A/en unknown
- 2017-07-11 MX MX2019000548A patent/MX395351B/es unknown
- 2017-07-11 MA MA045660A patent/MA45660A/fr unknown
- 2017-07-11 AU AU2017296289A patent/AU2017296289A1/en not_active Abandoned
- 2017-07-11 PE PE2019000035A patent/PE20190624A1/es unknown
- 2017-07-11 CR CR20190063A patent/CR20190063A/es unknown
- 2017-07-11 EP EP17742609.5A patent/EP3484856B1/en active Active
- 2017-07-11 KR KR1020197004088A patent/KR102598895B1/ko active Active
- 2017-07-11 TW TW112121134A patent/TWI912604B/zh active
- 2017-07-11 CN CN201780050842.XA patent/CN109983001B/zh active Active
- 2017-07-11 PH PH1/2019/500056A patent/PH12019500056B1/en unknown
- 2017-07-11 TW TW106123173A patent/TWI806832B/zh active
- 2017-07-11 IL IL321811A patent/IL321811A/en unknown
- 2017-07-11 CN CN202310268752.5A patent/CN116478131A/zh active Pending
- 2017-07-11 CA CA3030167A patent/CA3030167A1/en active Pending
- 2017-07-11 IL IL264186A patent/IL264186B2/en unknown
- 2017-07-11 KR KR1020237037794A patent/KR102921163B1/ko active Active
- 2017-07-11 CN CN202310285469.3A patent/CN116478132A/zh active Pending
- 2017-07-11 IL IL311645A patent/IL311645B2/en unknown
- 2017-07-11 TN TNP/2019/000010A patent/TN2019000010A1/en unknown
- 2017-07-11 SG SG11201900157RA patent/SG11201900157RA/en unknown
-
2018
- 2018-12-20 US US16/228,324 patent/US10590090B2/en active Active
-
2019
- 2019-01-08 DO DO2019000005A patent/DOP2019000005A/es unknown
- 2019-01-11 MX MX2022007607A patent/MX2022007607A/es unknown
- 2019-01-11 CL CL2019000090A patent/CL2019000090A1/es unknown
- 2019-01-22 CO CONC2019/0000613A patent/CO2019000613A2/es unknown
- 2019-02-12 EC ECSENADI201910079A patent/ECSP19010079A/es unknown
-
2020
- 2020-06-18 US US16/905,884 patent/US11661401B2/en active Active
-
2021
- 2021-07-15 JP JP2021116788A patent/JP7416740B2/ja active Active
- 2021-11-30 AU AU2021277664A patent/AU2021277664B2/en active Active
-
2023
- 2023-03-21 US US18/124,352 patent/US12565476B2/en active Active
- 2023-10-13 JP JP2023177195A patent/JP2024009957A/ja active Pending
- 2023-11-16 AU AU2023266357A patent/AU2023266357A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2019527728A5 (https=) | ||
| JP2015508103A5 (https=) | ||
| JP2018531274A5 (ja) | 炎症促進性細胞へのマクロファージ分極を改変して癌を治療するための抗ＳＩＲＰａ化合物 | |
| JP2009535462A5 (https=) | ||
| JP2020511467A5 (https=) | ||
| JP2016518328A5 (https=) | ||
| JP2019524883A5 (https=) | ||
| RU2016141934A (ru) | Ингибиторы циклин-зависимой киназы 7 (cdk7) | |
| JP2017186358A5 (https=) | ||
| JP2014521688A5 (https=) | ||
| JP2017514910A5 (https=) | ||
| JP2013537203A5 (https=) | ||
| JP2016518437A5 (https=) | ||
| WO2016105528A3 (en) | Inhibitors of cyclin-dependent kinase 7 (cdk7) | |
| JP2014511840A5 (https=) | ||
| JP2017524668A5 (https=) | ||
| JP2018534286A5 (https=) | ||
| JP2016505637A5 (https=) | ||
| JP2013502441A5 (https=) | ||
| JP2017524013A5 (https=) | ||
| JP2015508092A5 (https=) | ||
| JP2016531126A5 (https=) | ||
| JP2019516739A5 (https=) | ||
| JP2015502926A5 (https=) | ||
| JP2015520770A5 (https=) |