JP2017502993A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2017502993A5 JP2017502993A5 JP2016546839A JP2016546839A JP2017502993A5 JP 2017502993 A5 JP2017502993 A5 JP 2017502993A5 JP 2016546839 A JP2016546839 A JP 2016546839A JP 2016546839 A JP2016546839 A JP 2016546839A JP 2017502993 A5 JP2017502993 A5 JP 2017502993A5
- Authority
- JP
- Japan
- Prior art keywords
- amino
- alkyl
- substituted
- halo
- pharmaceutically acceptable
- 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
- 125000000217 alkyl group Chemical group 0.000 claims description 64
- 125000001475 halogen functional group Chemical group 0.000 claims description 50
- -1 amino, hydroxy Chemical group 0.000 claims description 44
- 150000003839 salts Chemical class 0.000 claims description 44
- 229920006395 saturated elastomer Polymers 0.000 claims description 42
- 150000001875 compounds Chemical class 0.000 claims description 34
- 229910052739 hydrogen Inorganic materials 0.000 claims description 33
- 239000001257 hydrogen Substances 0.000 claims description 33
- 125000003545 alkoxy group Chemical group 0.000 claims description 30
- 229910052799 carbon Inorganic materials 0.000 claims description 29
- 150000002431 hydrogen Chemical class 0.000 claims description 28
- 125000005842 heteroatom Chemical group 0.000 claims description 26
- 229910052760 oxygen Inorganic materials 0.000 claims description 26
- 229910052717 sulfur Inorganic materials 0.000 claims description 22
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 20
- 125000004432 carbon atom Chemical group C* 0.000 claims description 20
- 125000003282 alkyl amino group Chemical group 0.000 claims description 16
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 13
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 12
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims description 11
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 11
- 125000003118 aryl group Chemical group 0.000 claims description 10
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 9
- 229910052757 nitrogen Inorganic materials 0.000 claims description 9
- 125000003277 amino group Chemical group 0.000 claims description 8
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 8
- 125000001072 heteroaryl group Chemical group 0.000 claims description 6
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims description 6
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 6
- 125000001624 naphthyl group Chemical group 0.000 claims description 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 4
- 206010029260 Neuroblastoma Diseases 0.000 claims description 4
- 102100033019 Tyrosine-protein phosphatase non-receptor type 11 Human genes 0.000 claims description 4
- 101710116241 Tyrosine-protein phosphatase non-receptor type 11 Proteins 0.000 claims description 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 4
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 4
- 201000010099 disease Diseases 0.000 claims description 4
- 208000035475 disorder Diseases 0.000 claims description 4
- 230000000694 effects Effects 0.000 claims description 4
- 230000001404 mediated effect Effects 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 claims description 3
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 2
- 206010073478 Anaplastic large-cell lymphoma Diseases 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims description 2
- 208000005101 LEOPARD Syndrome Diseases 0.000 claims description 2
- 208000032004 Large-Cell Anaplastic Lymphoma Diseases 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- 206010062901 Multiple lentigines syndrome Diseases 0.000 claims description 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims description 2
- 208000037538 Myelomonocytic Juvenile Leukemia Diseases 0.000 claims description 2
- 206010029748 Noonan syndrome Diseases 0.000 claims description 2
- 208000010708 Noonan syndrome with multiple lentigines Diseases 0.000 claims description 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 2
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims description 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 2
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 201000004101 esophageal cancer Diseases 0.000 claims description 2
- 206010017758 gastric cancer Diseases 0.000 claims description 2
- 208000005017 glioblastoma Diseases 0.000 claims description 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 2
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 claims description 2
- 201000005992 juvenile myelomonocytic leukemia Diseases 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 208000020816 lung neoplasm Diseases 0.000 claims description 2
- 201000001441 melanoma Diseases 0.000 claims description 2
- 201000011549 stomach cancer Diseases 0.000 claims description 2
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 238000000034 method Methods 0.000 description 2
- 206010009944 Colon cancer Diseases 0.000 description 1
- 208000029742 colonic neoplasm Diseases 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461928754P | 2014-01-17 | 2014-01-17 | |
| US61/928,754 | 2014-01-17 | ||
| US201461991129P | 2014-05-09 | 2014-05-09 | |
| US61/991,129 | 2014-05-09 | ||
| PCT/IB2015/050345 WO2015107495A1 (en) | 2014-01-17 | 2015-01-16 | N-azaspirocycloalkane substituted n-heteroaryl compounds and compositions for inhibiting the activity of shp2 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017502993A JP2017502993A (ja) | 2017-01-26 |
| JP2017502993A5 true JP2017502993A5 (cg-RX-API-DMAC7.html) | 2018-02-22 |
| JP6534389B2 JP6534389B2 (ja) | 2019-06-26 |
Family
ID=52462974
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016546839A Active JP6534389B2 (ja) | 2014-01-17 | 2015-01-16 | Shp2の活性を阻害するためのn−アザスピロシクロアルカン置換n−ヘテロアリール化合物および組成物 |
Country Status (42)
Families Citing this family (141)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10357184B2 (en) * | 2012-06-21 | 2019-07-23 | Globus Medical, Inc. | Surgical tool systems and method |
| US11466017B2 (en) | 2011-03-10 | 2022-10-11 | Board Of Regents, The University Of Texas System | Heterocyclic inhibitors of PTPN11 |
| ES2935352T3 (es) | 2013-01-29 | 2023-03-06 | Aptinyx Inc | Moduladores de receptores NMDA de espiro-lactama y sus usos |
| CN105899491B (zh) | 2014-01-17 | 2019-04-02 | 诺华股份有限公司 | 用于抑制shp2活性的1-哒嗪-/三嗪-3-基-哌(-嗪)/啶/吡咯烷衍生物及其组合物 |
| JO3517B1 (ar) | 2014-01-17 | 2020-07-05 | Novartis Ag | ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2 |
| JP6473457B2 (ja) | 2014-01-17 | 2019-02-20 | ノバルティス アーゲー | Shp2の活性を阻害するための1−(トリアジン−3−イル/ピリダジン−3−イル)−ピペリジン/ピペラジン誘導体およびその組成物 |
| JP2018509448A (ja) * | 2015-03-25 | 2018-04-05 | ノバルティス アーゲー | 組合せ医薬 |
| EP3310771B1 (en) * | 2015-06-19 | 2020-07-22 | Novartis AG | Compounds and compositions for inhibiting the activity of shp2 |
| JP6718889B2 (ja) * | 2015-06-19 | 2020-07-08 | ノバルティス アーゲー | Shp2の活性を阻害するための化合物および組成物 |
| CN105503725B (zh) * | 2015-12-30 | 2018-03-27 | 天津药明康德新药开发有限公司 | 一种叔丁基1‑羟基‑8‑氮杂螺烷[4,5]葵烷‑8‑羧酸酯的制备方法 |
| 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 |
| KR20230109185A (ko) * | 2016-06-07 | 2023-07-19 | 자코바이오 파마슈티칼스 컴퍼니 리미티드 | Shp2 억제제로서 유용한 신규한 헤테로환형 유도체 |
| CN114057689A (zh) * | 2016-06-14 | 2022-02-18 | 诺华股份有限公司 | 用于抑制shp2活性的化合物和组合物 |
| TN2019000010A1 (en) * | 2016-07-12 | 2020-07-15 | Revolution Medicines Inc | 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors |
| CA3031563C (en) | 2016-08-01 | 2023-12-05 | Aptinyx Inc. | Spiro-lactam nmda modulators and methods of using same |
| KR102503590B1 (ko) | 2016-08-01 | 2023-02-24 | 앱티닉스 인크. | 스피로-락탐 nmda 수용체 조정제 및 그의 용도 |
| EA201990424A1 (ru) | 2016-08-01 | 2019-08-30 | Аптиникс Инк. | Спиролактамовые модуляторы nmda-рецептора и их применение |
| US11529347B2 (en) | 2016-09-22 | 2022-12-20 | Relay Therapeutics, Inc. | SHP2 phosphatase inhibitors and methods of use thereof |
| TWI848901B (zh) | 2016-10-24 | 2024-07-21 | 美商傳達治療有限公司 | Shp2磷酸酶抑制劑及其使用方法 |
| EP3568204B1 (en) | 2017-01-10 | 2023-08-30 | Novartis AG | Pharmaceutical combination comprising an alk inhibitor and an shp2 inhibitor |
| CA3051054A1 (en) * | 2017-01-23 | 2018-07-26 | Revolution Medicines, Inc. | Pyridine compounds as allosteric shp2 inhibitors |
| CA3051206A1 (en) | 2017-01-23 | 2018-07-26 | Revolution Medicines, Inc. | Bicyclic compounds as allosteric shp2 inhibitors |
| PT3601239T (pt) * | 2017-03-23 | 2024-10-24 | Jacobio Pharmaceuticals Co Ltd | Novos derivados heterocíclicos úteis como inibidores de shp2 |
| WO2018218133A1 (en) | 2017-05-26 | 2018-11-29 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors |
| GB2577436B (en) * | 2017-06-20 | 2024-11-27 | Control Components | Multi-stage, multi-path rotary disc valve |
| AU2018328273A1 (en) | 2017-09-07 | 2020-03-12 | Revolution Medicines, Inc. | SHP2 inhibitor compositions and methods for treating cancer |
| CN118684652A (zh) * | 2017-09-11 | 2024-09-24 | 克鲁松制药公司 | SHP2的八氢环戊二烯并[c]吡咯别构抑制剂 |
| EP3687997A1 (en) | 2017-09-29 | 2020-08-05 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors |
| RU2020115095A (ru) | 2017-10-12 | 2021-11-12 | Революшн Медсинз, Инк. | Пиридиновые, пиразиновые и триазиновые соединения в качестве аллостерических ингибиторов shp2 |
| TWI697490B (zh) * | 2017-12-06 | 2020-07-01 | 大陸商北京加科思新藥研發有限公司 | 用於作為shp2抑制劑之新穎雜環衍生物 |
| MX2020006273A (es) | 2017-12-15 | 2020-09-14 | Revolution Medicines Inc | Compuestos policiclicos como inhibidores alostericos de shp2. |
| WO2019152454A1 (en) * | 2018-01-30 | 2019-08-08 | Research Development Foundation | Shp2 inhibitors and methods of use thereof |
| SG11202007256PA (en) | 2018-01-31 | 2020-08-28 | Aptinyx Inc | Spiro-lactam nmda receptor modulators and uses thereof |
| AU2019222026B2 (en) * | 2018-02-13 | 2022-05-12 | Shanghai Blueray Biopharma Co., Ltd. | Pyrimidine-fused cyclic compound, preparation method therefor and application thereof |
| 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 |
| US20200392161A1 (en) | 2018-02-21 | 2020-12-17 | Relay Therapeutics, Inc. | Shp2 phosphatase inhibitors and methods of use thereof |
| MX2020008754A (es) | 2018-03-02 | 2020-12-07 | Otsuka Pharma Co Ltd | Compuestos farmaceuticos. |
| WO2019183364A1 (en) | 2018-03-21 | 2019-09-26 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine shp2 phosphatase inhibitors and methods of use thereof |
| 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 |
| AU2019240299B2 (en) * | 2018-03-21 | 2023-06-22 | D.E. Shaw Research, Llc | SHP2 phosphatase inhibitors and methods of use thereof |
| JP2021521155A (ja) * | 2018-04-10 | 2021-08-26 | 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 | Shp2阻害剤組成物、癌を処置するための方法、およびshp変異を有する対象を特定するための方法 |
| IL300091A (en) | 2018-05-01 | 2023-03-01 | Revolution Medicines Inc | C40-, c28-, and c-32-linked rapamycin analogs as mtor inhibitors |
| KR102611661B1 (ko) * | 2018-05-02 | 2023-12-08 | 나비레 파르마, 인코퍼레이티드 | Ptpn11의 치환된 헤테로사이클릭 억제제 |
| CN116003321A (zh) * | 2018-05-09 | 2023-04-25 | 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 |
| US12037345B2 (en) | 2018-07-24 | 2024-07-16 | Taiho Pharmaceutical Co., Ltd. | Heterobicyclic compounds for inhibiting the activity of SHP2 |
| AU2019319971B2 (en) | 2018-08-10 | 2024-11-28 | Navire Pharma, Inc. | 6-(4-amino-3-methyl-2-oxa-8-azaspiro(4.5)decan-8-yl)-3-(2,3-dichlorophenyl)-2-methylpyrimidin-4(3h)-one derivatives and related compounds as ptpn11 (shp2) inhibitors for treating cancer |
| FI3853234T3 (fi) | 2018-09-18 | 2025-07-28 | Nikang Therapeutics Inc | Fuusioituja trisyklisiä rengasjohdannaisia SRC-homologia-2-fosfataasin estäjinä |
| 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 |
| JP7386855B2 (ja) * | 2018-09-29 | 2023-11-27 | ノバルティス アーゲー | Shp2の活性を阻害するための化合物及び組成物の製造 |
| BR112021005606A2 (pt) | 2018-09-29 | 2021-06-22 | Novartis Ag | processo de produção de um composto para inibir a atividade de shp2 |
| US11179397B2 (en) | 2018-10-03 | 2021-11-23 | Gilead Sciences, Inc. | Imidazopyrimidine derivatives |
| 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 |
| ES2947464T3 (es) | 2018-10-17 | 2023-08-09 | Array Biopharma Inc | Inhibidores de la proteína tirosina fosfatasa |
| CN117143079A (zh) * | 2018-11-06 | 2023-12-01 | 上海奕拓医药科技有限责任公司 | 一种螺芳环化合物及其应用 |
| CN111153899B (zh) * | 2018-11-08 | 2023-12-01 | 四川科伦博泰生物医药股份有限公司 | 一种取代吡啶化合物、其制备方法和用途 |
| 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 |
| CA3112129A1 (en) | 2018-12-05 | 2020-06-11 | Mirati Therapeutics, Inc. | Combination therapies |
| CN113316574B (zh) * | 2019-01-31 | 2024-01-30 | 贝达药业股份有限公司 | Shp2抑制剂及其应用 |
| JP7572958B2 (ja) * | 2019-02-12 | 2024-10-24 | ノバルティス アーゲー | Tno155及びkrasg12c阻害剤を含む医薬組合せ |
| MX2021009563A (es) | 2019-02-12 | 2021-09-08 | Novartis Ag | Combinacion farmaceutica que comprende tno155 y ribociclib. |
| EP3923940B1 (en) * | 2019-02-12 | 2025-12-03 | Novartis AG | Pharmaceutical combination comprising tno155 and a pd-1 inhibitor |
| 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 |
| WO2020181283A1 (en) | 2019-03-07 | 2020-09-10 | Merck Patent Gmbh | Carboxamide-pyrimidine derivatives as shp2 antagonists |
| AU2020251841B2 (en) | 2019-04-02 | 2025-01-30 | Array Biopharma Inc. | Protein tyrosine phosphatase inhibitors |
| AU2020271838A1 (en) * | 2019-04-08 | 2021-08-19 | Merck Patent Gmbh | Pyrimidinone derivatives as SHP2 antagonists |
| EP4306529A3 (en) | 2019-05-13 | 2024-04-10 | Relay Therapeutics, Inc. | Fgfr inhibitors and methods of use thereof |
| EP3980128A1 (en) * | 2019-06-07 | 2022-04-13 | Revolution Medicines, Inc. | Solid forms of {6-[(2-amino-3-chloropyridin-4-yl)sulfanyl]-3-[(3s,4s)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-5-methylpyrazin-2-yl}methanol, an shp2 inhibitor |
| 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 |
| CN113840603B (zh) | 2019-06-28 | 2024-08-13 | 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 |
| 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 |
| US12122787B2 (en) | 2019-09-20 | 2024-10-22 | Shanghai Jemincare Pharmaceuticals Co., Ltd | Fused pyridone compound, and preparation method therefor and use thereof |
| US11890281B2 (en) | 2019-09-24 | 2024-02-06 | Relay Therapeutics, Inc. | SHP2 phosphatase inhibitors and methods of making and using the same |
| MX2022005525A (es) | 2019-11-08 | 2022-06-08 | Revolution Medicines Inc | Compuestos de heteroarilo bicíclicos y usos de estos. |
| CN114761394B (zh) * | 2020-01-16 | 2024-03-29 | 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 |
| 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 |
| US20230090389A1 (en) | 2020-02-28 | 2023-03-23 | Novartis Ag | A triple pharmaceutical combination comprising dabrafenib, an erk inhibitor and a shp2 inhibitor |
| 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 |
| 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 |
| WO2021218755A1 (zh) * | 2020-04-30 | 2021-11-04 | 贝达药业股份有限公司 | Shp2抑制剂及其组合物和应用 |
| AU2021267213B2 (en) | 2020-05-08 | 2023-11-30 | Novartis Ag | Pharmaceutical combination comprising TNO155 and nazartinib |
| WO2021236775A1 (en) * | 2020-05-19 | 2021-11-25 | The Regents Of The University Ofmichigan | Small molecule degraders of shp2 protein |
| WO2021247836A1 (en) | 2020-06-03 | 2021-12-09 | Board Of Regents, The University Of Texas System | Methods for targeting shp-2 to overcome resistance |
| CN115734966B (zh) * | 2020-06-12 | 2025-07-18 | 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 |
| CN115916194A (zh) | 2020-06-18 | 2023-04-04 | 锐新医药公司 | 用于延迟、预防和治疗针对ras抑制剂的获得性抗性的方法 |
| CN115667239B (zh) | 2020-06-22 | 2025-11-18 | 四川科伦博泰生物医药股份有限公司 | 取代吡嗪类化合物,包含其的药物组合物及其用途 |
| WO2022006780A1 (en) * | 2020-07-08 | 2022-01-13 | Novartis Ag | Manufacture of compounds and compositions for inhibiting activity of shp2 |
| ES3040751T3 (en) | 2020-07-08 | 2025-11-04 | Novartis Ag | Manufacture of compounds and compositions for inhibiting the activity of shp2 |
| US20230339882A1 (en) * | 2020-07-24 | 2023-10-26 | Betta Pharmaceuticals Co., Ltd. | Shp2 inhibitor and composition and application thereof |
| US20250195521A1 (en) | 2020-09-03 | 2025-06-19 | Revolution Medicines, Inc. | Use of sos1 inhibitors to treat malignancies with shp2 mutations |
| CN117683049A (zh) | 2020-09-15 | 2024-03-12 | 锐新医药公司 | 作为ras抑制剂以治疗癌症的吲哚衍生物 |
| WO2022063190A1 (zh) * | 2020-09-23 | 2022-03-31 | 南京明德新药研发有限公司 | 吡嗪硫联苯基类化合物及其应用 |
| TW202233625A (zh) | 2020-11-18 | 2022-09-01 | 美商傳達治療有限公司 | Fgfr抑制劑及其製造及使用方法 |
| EP4039685A1 (en) | 2021-02-08 | 2022-08-10 | Irbm S.P.A. | Azabicyclic shp2 inhibitors |
| AU2022244941B2 (en) * | 2021-03-23 | 2024-08-01 | Shanghai Haiyan Pharmaceutical Technology Co., Ltd. | Heterocycle substituted ketone derivative, and composition and medicinal use thereof |
| 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 |
| CN117083285A (zh) * | 2021-03-31 | 2023-11-17 | 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 |
| 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 |
| WO2022235866A1 (en) | 2021-05-05 | 2022-11-10 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
| WO2022235822A1 (en) | 2021-05-05 | 2022-11-10 | Huabio International, Llc | Shp2 inhibitor monotherapy and uses thereof |
| US20230106174A1 (en) | 2021-05-05 | 2023-04-06 | Revolution Medicines, Inc. | Ras inhibitors |
| EP4334325A1 (en) | 2021-05-05 | 2024-03-13 | Revolution Medicines, Inc. | Ras inhibitors for the treatment of cancer |
| EP4334318A4 (en) | 2021-05-05 | 2025-03-05 | Huyabio International, LLC | COMBINATION THERAPIES WITH SHP2 INHIBITORS AND PD-1 INHIBITORS |
| 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 |
| WO2022259157A1 (en) | 2021-06-09 | 2022-12-15 | Novartis Ag | A triple pharmaceutical combination comprising dabrafenib, trametinib and a shp2 inhibitor |
| CN117642166A (zh) | 2021-06-09 | 2024-03-01 | 中外制药株式会社 | 用于癌症治疗的组合疗法 |
| WO2022258600A1 (en) | 2021-06-09 | 2022-12-15 | 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 |
| 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 |
| EP4368614A4 (en) * | 2021-07-07 | 2025-07-09 | Hinova Pharmaceuticals Inc | SYNTHESIS AND USE OF PHOSPHATASE DEGRADING AGENT |
| AU2022336415A1 (en) | 2021-09-01 | 2024-01-04 | Novartis Ag | Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| JP2024539852A (ja) | 2021-11-04 | 2024-10-31 | エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト | がんの治療のためのキナゾリノン化合物の新規使用 |
| TW202342040A (zh) | 2022-02-21 | 2023-11-01 | 瑞士商諾華公司 | 藥物配製物 |
| CN114524772B (zh) * | 2022-02-28 | 2023-07-11 | 中国药科大学 | 一种含杂环串联类化合物及其制备方法与应用 |
| EP4489755A1 (en) | 2022-03-08 | 2025-01-15 | Revolution Medicines, Inc. | Methods for treating immune refractory lung cancer |
| CN116903581A (zh) * | 2022-04-14 | 2023-10-20 | 山东大学 | Shp2/hdac双靶点抑制剂及其制备方法和应用 |
| AU2023285116A1 (en) | 2022-06-10 | 2024-12-19 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| EP4568956A1 (en) | 2022-08-11 | 2025-06-18 | Relay Therapeutics, Inc. | Solid forms of a cdk inhibitor |
| EP4345101A1 (en) | 2022-09-29 | 2024-04-03 | Irbm S.P.A. | Azole derivatives as shp2 inhibitors |
| AU2023380159A1 (en) | 2022-11-18 | 2025-05-15 | Novartis Ag | Pharmaceutical combinations and uses thereof |
| WO2024113194A1 (en) * | 2022-11-30 | 2024-06-06 | Canwell Biotech Limited | Shp2 inhibitors, compositions and methods thereof |
| WO2024126660A1 (en) | 2022-12-15 | 2024-06-20 | F. Hoffmann-La Roche Ag | Combination therapy for cancer treatment |
| KR20250164828A (ko) | 2023-03-30 | 2025-11-25 | 레볼루션 메디슨즈, 인크. | Ras gtp 가수분해 유도를 위한 조성물 및 이의 용도 |
| AU2024243852A1 (en) | 2023-04-07 | 2025-11-06 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| WO2024211663A1 (en) | 2023-04-07 | 2024-10-10 | Revolution Medicines, Inc. | Condensed macrocyclic compounds as ras inhibitors |
| CN121100123A (zh) | 2023-04-14 | 2025-12-09 | 锐新医药公司 | Ras抑制剂的结晶形式 |
| TW202448897A (zh) | 2023-04-14 | 2024-12-16 | 美商銳新醫藥公司 | Ras抑制劑之結晶形式、含有其之組合物及其使用方法 |
| WO2024218632A1 (en) | 2023-04-17 | 2024-10-24 | Array Biopharma Inc. | Erk protein kinase inhibitors |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025034919A1 (en) | 2023-08-08 | 2025-02-13 | Quanta Therapeutics, Inc. | Combination therapies with kras modulators |
| WO2025080946A2 (en) | 2023-10-12 | 2025-04-17 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025106901A1 (en) | 2023-11-17 | 2025-05-22 | Quanta Therapeutics, Inc. | Combination cancer therapies with a kras modulator and an rtk-mapk pathway inhibitor |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025215527A2 (en) | 2024-04-10 | 2025-10-16 | Novartis Ag | Pharmaceutical combinations and uses thereof |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| CN119039223B (zh) * | 2024-10-31 | 2025-02-25 | 江苏豪森药业集团有限公司 | 一种含氮杂芳类衍生物的制备方法及其中间体 |
| 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 (135)
| 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 |
| EP0090505B1 (en) | 1982-03-03 | 1990-08-08 | Genentech, Inc. | Human antithrombin iii, dna sequences therefor, expression vehicles and cloning vectors containing such sequences and cell cultures transformed thereby, a process for expressing human antithrombin iii, and pharmaceutical compositions comprising it |
| 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 |
| DE3752141T2 (de) | 1986-02-24 | 1998-03-26 | Mitsui Petrochemical Ind | Mittel zur behandlung von neuropathie |
| 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 |
| CA2263129C (en) | 1996-08-16 | 2007-01-09 | Schering Corporation | Mammalian cell surface antigens; related reagents |
| US6111090A (en) | 1996-08-16 | 2000-08-29 | Schering Corporation | Mammalian cell surface antigens; related reagents |
| MA26473A1 (fr) | 1997-03-01 | 2004-12-20 | Glaxo Group Ltd | Composes pharmacologiquement actifs. |
| AU1102399A (en) | 1997-10-21 | 1999-05-10 | Human Genome Sciences, Inc. | Human tumor necrosis factor receptor-like proteins tr11, tr11sv1, and tr11sv2 |
| EP1053321A1 (en) | 1998-02-09 | 2000-11-22 | Genentech, Inc. | Novel tumor necrosis factor receptor homolog and nucleic acids encoding the same |
| WO2000059893A1 (en) | 1999-04-06 | 2000-10-12 | 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 |
| ES2295040T3 (es) | 1999-07-12 | 2008-04-16 | Genentech, Inc. | Promocion o inhibicion de la angiogenesis y cardiovascularizacion mediante homologos del ligando / receptor del factor de necrosis del tumor. |
| 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 |
| CA2463989C (en) | 2001-10-17 | 2012-01-31 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Pyrimidine derivatives, pharmaceutical compositions containing these compounds, the use thereof and process for the preparation thereof |
| WO2003064383A2 (en) | 2002-02-01 | 2003-08-07 | Ariad Gene Therapeutics, Inc. | Phosphorus-containing compounds & uses thereof |
| MXPA04007697A (es) | 2002-02-06 | 2004-11-10 | Vertex Pharma | Compuestos de heteroarilo utiles como inhibidores de gsk-3. |
| HRP20040800B1 (en) | 2002-03-05 | 2012-11-30 | Merck Frosst Canada & Co Axys | Cathepsin cysteine protease inhibitors |
| TWI275390B (en) | 2002-04-30 | 2007-03-11 | Wyeth Corp | Process for the preparation of 7-substituted-3- quinolinecarbonitriles |
| ES2367430T3 (es) | 2002-12-23 | 2011-11-03 | Wyeth Llc | Anticuerpos contra pd-1 y sus usos. |
| GB0300783D0 (en) | 2003-01-14 | 2003-02-12 | Btg Int Ltd | Treatment of neurodegenerative conditions |
| EP1603901B1 (en) * | 2003-03-07 | 2008-10-15 | MERCK SHARP & DOHME LTD. | Tetrahydropyran compounds as tachykinin antagonists |
| JP4638876B2 (ja) | 2003-05-23 | 2011-02-23 | ワイス | Gitrリガンド及びgitrリガンド関連分子及び抗体及びその使用 |
| WO2005007190A1 (en) | 2003-07-11 | 2005-01-27 | Schering Corporation | Agonists or antagonists of the clucocorticoid-induced tumour necrosis factor receptor (gitr) or its ligand for the treatment of immune disorders, infections and cancer |
| US7399865B2 (en) | 2003-09-15 | 2008-07-15 | Wyeth | Protein tyrosine kinase enzyme inhibitors |
| JP2007518399A (ja) | 2003-12-02 | 2007-07-12 | ジェンザイム コーポレイション | 肺癌を診断および治療する組成物並びに方法 |
| EP1737841A1 (en) | 2004-04-01 | 2007-01-03 | Astellas Pharma Inc. | Pyrazine derivatives and pharmaceutical use thereof as adenosine antagonists |
| JP5213229B2 (ja) * | 2004-04-23 | 2013-06-19 | エグゼリクシス, インコーポレイテッド | キナーゼ調節因子および使用方法 |
| GB0409799D0 (en) | 2004-04-30 | 2004-06-09 | Isis Innovation | Method of generating improved immune response |
| EP1765402A2 (en) | 2004-06-04 | 2007-03-28 | Duke University | Methods and compositions for enhancement of immunity by in vivo depletion of immunosuppressive cell activity |
| KR20180122750A (ko) | 2004-09-02 | 2018-11-13 | 제넨테크, 인크. | 헤지호그 신호전달에 대한 피리딜 억제제 |
| KR20070095952A (ko) | 2004-12-16 | 2007-10-01 | 버텍스 파마슈티칼스 인코포레이티드 | 염증성 질환, 증식성 질환 및 면역학적으로 매개된 질환치료용 Tec 계열 단백질 키나제의 억제제로서 유용한피리드-2-온 |
| DK1866339T3 (da) | 2005-03-25 | 2013-09-02 | Gitr Inc | GTR-bindende molekyler og anvendelser heraf |
| EP1896582A4 (en) | 2005-05-09 | 2009-04-08 | Ono Pharmaceutical Co | HUMAN MONOCLONAL ANTIBODIES AGAINST PROGRAMMED CELL DEATH 1 (PD-1) AND METHOD FOR CREATING TREATMENT WITH ANTI-PD-1 ANTIBODIES ALONE OR IN COMBINATION WITH OTHER IMMUNOTHERAPEUTICS |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| CN104356236B (zh) | 2005-07-01 | 2020-07-03 | E.R.施贵宝&圣斯有限责任公司 | 抗程序性死亡配体1(pd-l1)的人单克隆抗体 |
| KR20080043840A (ko) | 2005-09-13 | 2008-05-19 | 팔라우 파르마 에스에이 | 히스타민 h4 수용체 활성의 조정자로서 2-아미노피리미딘유도체 |
| AR057579A1 (es) * | 2005-11-23 | 2007-12-05 | Merck & Co Inc | Compuestos espirociclicos como inhibidores de histona de acetilasa (hdac) |
| EP1981969A4 (en) | 2006-01-19 | 2009-06-03 | Genzyme Corp | ANTI-GITRANT ANTIBODIES FOR THE TREATMENT OF CANCER |
| WO2007112368A1 (en) | 2006-03-28 | 2007-10-04 | Takeda Pharmaceutical Company Limited | Preparation of (r)-3-aminopiperidine dihydrochloride |
| DK2041071T3 (da) | 2006-06-29 | 2014-09-01 | Kinex Pharmaceuticals Llc | Biarylsammensætninger og fremgangsmåder til modulering af en kinasekaskade |
| 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 |
| WO2008100412A1 (en) | 2007-02-12 | 2008-08-21 | Merck & Co., Inc. | Piperidine derivatives |
| DK2137162T3 (en) * | 2007-03-15 | 2018-11-26 | Novartis Ag | Organic compounds and their applications |
| WO2008156712A1 (en) | 2007-06-18 | 2008-12-24 | N. V. Organon | Antibodies to human programmed death receptor pd-1 |
| AU2008275589B2 (en) | 2007-07-12 | 2013-11-21 | Gitr, Inc. | Combination therapies employing GITR binding molecules |
| PE20090678A1 (es) | 2007-09-12 | 2009-06-27 | Genentech Inc | Combinaciones de compuestos inhibidores de fosfoinositida 3-quinasa y agentes quimioterapeuticos y los metodos de uso |
| WO2009055730A1 (en) | 2007-10-25 | 2009-04-30 | Genentech, Inc. | Process for making thienopyrimidine compounds |
| BRPI0907718A2 (pt) | 2008-02-11 | 2017-06-13 | Curetech Ltd | método para tratar um tumor, método para melhorar a tolerabilidade a pelo menos um agente quimiterápico, método para aumentar a sobrevida de um indivíduo que tem um tumor, método para reduzir ou prevenir recidiva tumoral, uso de um anticorpo monoclonal humanizado ou seu fragmento e anticorpo monoclonal humanizado ou seu fragmento |
| WO2009114335A2 (en) | 2008-03-12 | 2009-09-17 | Merck & Co., Inc. | Pd-1 binding proteins |
| EP2271631B1 (en) | 2008-04-22 | 2018-07-04 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| EP2310381A1 (en) | 2008-06-13 | 2011-04-20 | Novartis AG | 2,4'-bipyridinyl compounds as protein kinase d inhibitors useful for the treatment of ia heart failure and cancer |
| US8168784B2 (en) | 2008-06-20 | 2012-05-01 | Abbott Laboratories | Processes to make apoptosis promoters |
| CN102203074A (zh) | 2008-06-20 | 2011-09-28 | 麦它波莱克斯股份有限公司 | 芳基gpr119激动剂及其用途 |
| CA2986640C (en) | 2008-06-27 | 2019-03-26 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| GB0812031D0 (en) | 2008-07-01 | 2008-08-06 | 7Tm Pharma As | Thiazole derivatives |
| CA2729810A1 (en) | 2008-07-02 | 2010-01-07 | Emergent Product Development Seattle, Llc | Tgf-.beta. antagonist multi-target binding proteins |
| US9174969B2 (en) | 2008-07-21 | 2015-11-03 | University Of South Florida | Indoline scaffold SHP-2 inhibitors and cancer treatment method |
| AR072999A1 (es) | 2008-08-11 | 2010-10-06 | Medarex Inc | Anticuerpos humanos que se unen al gen 3 de activacion linfocitaria (lag-3) y los usos de estos |
| EP2328919A2 (en) | 2008-08-25 | 2011-06-08 | Amplimmune, Inc. | Pd-i antagonists and methods for treating infectious disease |
| EP2350129B1 (en) | 2008-08-25 | 2015-06-10 | Amplimmune, Inc. | Compositions of pd-1 antagonists and methods of use |
| US8586023B2 (en) | 2008-09-12 | 2013-11-19 | Mie University | Cell capable of expressing exogenous GITR ligand |
| WO2010048149A2 (en) | 2008-10-20 | 2010-04-29 | Kalypsys, Inc. | Heterocyclic modulators of gpr119 for treatment of disease |
| EP2370424A1 (en) * | 2008-11-10 | 2011-10-05 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| TW202442680A (zh) | 2008-12-09 | 2024-11-01 | 美商建南德克公司 | 抗pd-l1抗體及其於增進t細胞功能之用途 |
| 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 |
| WO2010089411A2 (en) | 2009-02-09 | 2010-08-12 | Universite De La Mediterranee | Pd-1 antibodies and pd-l1 antibodies and uses thereof |
| 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 |
| CN108752280A (zh) | 2009-08-17 | 2018-11-06 | 纪念斯隆-凯特琳癌症中心 | 热休克蛋白结合化合物、组合物以及其制备和使用方法 |
| IN2012DN01920A (cg-RX-API-DMAC7.html) | 2009-09-03 | 2015-07-24 | Schering Corp | |
| GB0919054D0 (en) | 2009-10-30 | 2009-12-16 | Isis Innovation | Treatment of obesity |
| US8673913B2 (en) | 2009-11-13 | 2014-03-18 | Case Western Reserve University | SHP-2 phosphatase inhibitor |
| WO2011066342A2 (en) | 2009-11-24 | 2011-06-03 | Amplimmune, Inc. | Simultaneous inhibition of pd-l1/pd-l2 |
| 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 |
| WO2011090762A1 (en) | 2009-12-29 | 2011-07-28 | Emergent Product Development Seattle, Llc | Heterodimer binding proteins and uses thereof |
| WO2012002577A1 (ja) | 2010-06-30 | 2012-01-05 | 富士フイルム株式会社 | 新規なニコチンアミド誘導体またはその塩 |
| JP2013531037A (ja) | 2010-07-13 | 2013-08-01 | メルク・シャープ・エンド・ドーム・コーポレイション | スピロ環式化合物 |
| ES2823350T3 (es) | 2010-07-29 | 2021-05-06 | Rigel Pharmaceuticals Inc | Compuestos heterocíclicos que activan AMPK y métodos de uso de los mismos |
| WO2012027495A1 (en) * | 2010-08-27 | 2012-03-01 | University Of The Pacific | Piperazinylpyrimidine analogues as protein kinase inhibitors |
| EP2630134B9 (en) | 2010-10-20 | 2018-04-18 | Pfizer Inc | Pyridine-2- derivatives as smoothened receptor modulators |
| AU2011344001B2 (en) | 2010-12-13 | 2016-06-30 | Array Biopharma Inc. | Substituted N-(1H-indazol-4-yl)imidazo[1,2-a]pyridine-3-carboxamide compounds as type III receptor tyrosine kinase inhibitors |
| JP5727276B2 (ja) | 2011-03-04 | 2015-06-03 | 協同油脂株式会社 | グリース組成物及びグリース封入転がり軸受 |
| HUE034979T2 (en) | 2011-09-12 | 2018-05-02 | Merck Patent Gmbh | Aminopyrimidine derivatives for use as modulators of kinase activity |
| WO2013039954A1 (en) | 2011-09-14 | 2013-03-21 | Sanofi | Anti-gitr antibodies |
| MX349096B (es) | 2011-11-28 | 2017-07-11 | Merck Patent Gmbh | Anticuerpos anti-pd-l1 y sus usos. |
| WO2013096093A1 (en) | 2011-12-21 | 2013-06-27 | Merck Sharp & Dohme Corp. | Compounds as dgat-1 inhibitors |
| KR20150016406A (ko) | 2012-06-07 | 2015-02-11 | 에프. 호프만-라 로슈 아게 | 탄키라제의 피라졸로피리미돈 및 피라졸로피리돈 억제제 |
| CN104364239B (zh) | 2012-06-13 | 2017-08-25 | 霍夫曼-拉罗奇有限公司 | 二氮杂螺环烷烃和氮杂螺环烷烃 |
| UY34887A (es) | 2012-07-02 | 2013-12-31 | Bristol Myers Squibb Company Una Corporacion Del Estado De Delaware | Optimización de anticuerpos que se fijan al gen de activación de linfocitos 3 (lag-3) y sus usos |
| WO2014054053A1 (en) | 2012-10-03 | 2014-04-10 | Advinus Therapeutics Limited | Spirocyclic compounds, compositions and medicinal applications thereof |
| WO2014160521A1 (en) * | 2013-03-15 | 2014-10-02 | Blueprint Medicines Corporation | Piperazine derivatives and their use as kit modulators |
| US10189859B2 (en) | 2013-12-21 | 2019-01-29 | Nektar Therapeutics | Derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5-amine |
| JO3517B1 (ar) | 2014-01-17 | 2020-07-05 | Novartis Ag | ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2 |
| CN105899491B (zh) | 2014-01-17 | 2019-04-02 | 诺华股份有限公司 | 用于抑制shp2活性的1-哒嗪-/三嗪-3-基-哌(-嗪)/啶/吡咯烷衍生物及其组合物 |
| JP6473457B2 (ja) | 2014-01-17 | 2019-02-20 | ノバルティス アーゲー | Shp2の活性を阻害するための1−(トリアジン−3−イル/ピリダジン−3−イル)−ピペリジン/ピペラジン誘導体およびその組成物 |
| HRP20220096T1 (hr) | 2014-05-01 | 2022-04-15 | Celgene Quanticel Research, Inc. | Inhibitori lizin specifične demetilaze-1 |
| US10174032B2 (en) | 2014-05-05 | 2019-01-08 | Signalrx Pharmaceuticals, Inc. | Heterocyclic compound classes for signaling modulation |
| EP3310771B1 (en) | 2015-06-19 | 2020-07-22 | Novartis AG | Compounds and compositions for inhibiting the activity of shp2 |
| ES2741746T3 (es) | 2015-06-19 | 2020-02-12 | Novartis Ag | Compuestos y composiciones para inhibir la actividad de SHP2 |
| JP6718889B2 (ja) | 2015-06-19 | 2020-07-08 | ノバルティス アーゲー | Shp2の活性を阻害するための化合物および組成物 |
| 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 |
| KR20230109185A (ko) | 2016-06-07 | 2023-07-19 | 자코바이오 파마슈티칼스 컴퍼니 리미티드 | Shp2 억제제로서 유용한 신규한 헤테로환형 유도체 |
| TN2019000010A1 (en) | 2016-07-12 | 2020-07-15 | Revolution Medicines Inc | 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors |
| US11529347B2 (en) | 2016-09-22 | 2022-12-20 | Relay Therapeutics, Inc. | SHP2 phosphatase inhibitors and methods of use thereof |
| TWI848901B (zh) | 2016-10-24 | 2024-07-21 | 美商傳達治療有限公司 | Shp2磷酸酶抑制劑及其使用方法 |
| EP3568204B1 (en) | 2017-01-10 | 2023-08-30 | Novartis AG | Pharmaceutical combination comprising an alk inhibitor and an shp2 inhibitor |
| CA3051054A1 (en) | 2017-01-23 | 2018-07-26 | Revolution Medicines, Inc. | Pyridine compounds as allosteric shp2 inhibitors |
| CA3051206A1 (en) | 2017-01-23 | 2018-07-26 | Revolution Medicines, Inc. | Bicyclic compounds as allosteric shp2 inhibitors |
| PT3601239T (pt) | 2017-03-23 | 2024-10-24 | Jacobio Pharmaceuticals Co Ltd | Novos derivados heterocíclicos úteis como inibidores de shp2 |
| AU2018328273A1 (en) | 2017-09-07 | 2020-03-12 | 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 |
| RU2020115095A (ru) | 2017-10-12 | 2021-11-12 | Революшн Медсинз, Инк. | Пиридиновые, пиразиновые и триазиновые соединения в качестве аллостерических ингибиторов shp2 |
| MX2020006273A (es) | 2017-12-15 | 2020-09-14 | Revolution Medicines Inc | Compuestos policiclicos como inhibidores alostericos de shp2. |
| US20200392161A1 (en) | 2018-02-21 | 2020-12-17 | Relay Therapeutics, Inc. | Shp2 phosphatase inhibitors and methods of use thereof |
| AU2019240299B2 (en) | 2018-03-21 | 2023-06-22 | D.E. Shaw Research, Llc | SHP2 phosphatase inhibitors and methods of use thereof |
| JP2021521155A (ja) | 2018-04-10 | 2021-08-26 | 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 | Shp2阻害剤組成物、癌を処置するための方法、およびshp変異を有する対象を特定するための方法 |
-
2015
- 2015-01-15 JO JOP/2015/0004A patent/JO3517B1/ar active
- 2015-01-16 PE PE2016001228A patent/PE20170011A1/es unknown
- 2015-01-16 KR KR1020167021977A patent/KR102501558B1/ko active Active
- 2015-01-16 EP EP15703321.8A patent/EP3094628B1/en active Active
- 2015-01-16 EA EA201691442A patent/EA031573B1/ru not_active IP Right Cessation
- 2015-01-16 CN CN201580004708.7A patent/CN105916845B/zh active Active
- 2015-01-16 CR CR20200617A patent/CR20200617A/es unknown
- 2015-01-16 UY UY0001035957A patent/UY35957A/es active IP Right Grant
- 2015-01-16 JP JP2016546839A patent/JP6534389B2/ja active Active
- 2015-01-16 CU CU2016000115A patent/CU24424B1/es unknown
- 2015-01-16 CA CA2935695A patent/CA2935695C/en active Active
- 2015-01-16 RS RS20181174A patent/RS57757B1/sr unknown
- 2015-01-16 MX MX2016009223A patent/MX356895B/es active IP Right Grant
- 2015-01-16 ES ES15703321T patent/ES2695242T3/es active Active
- 2015-01-16 LT LTEP15703321.8T patent/LT3094628T/lt unknown
- 2015-01-16 AP AP2016009299A patent/AP2016009299A0/en unknown
- 2015-01-16 MA MA39282A patent/MA39282B1/fr unknown
- 2015-01-16 HR HRP20181832TT patent/HRP20181832T1/hr unknown
- 2015-01-16 SI SI201530432T patent/SI3094628T1/sl unknown
- 2015-01-16 US US15/110,511 patent/US10077276B2/en active Active
- 2015-01-16 TW TW104101593A patent/TWI657083B/zh active
- 2015-01-16 SG SG11201605272SA patent/SG11201605272SA/en unknown
- 2015-01-16 PT PT15703321T patent/PT3094628T/pt unknown
- 2015-01-16 AR ARP150100117A patent/AR100033A1/es active IP Right Grant
- 2015-01-16 TN TN2016000268A patent/TN2016000268A1/en unknown
- 2015-01-16 DK DK15703321.8T patent/DK3094628T3/en active
- 2015-01-16 HU HUE15703321A patent/HUE039869T2/hu unknown
- 2015-01-16 MY MYPI2016702327A patent/MY176357A/en unknown
- 2015-01-16 NZ NZ721598A patent/NZ721598A/en unknown
- 2015-01-16 BR BR112016016432-6A patent/BR112016016432B1/pt active IP Right Grant
- 2015-01-16 CR CR20160328A patent/CR20160328A/es unknown
- 2015-01-16 KR KR1020237005361A patent/KR102688024B1/ko active Active
- 2015-01-16 WO PCT/IB2015/050345 patent/WO2015107495A1/en not_active Ceased
- 2015-01-16 AU AU2015207757A patent/AU2015207757B8/en active Active
- 2015-01-16 PL PL15703321T patent/PL3094628T3/pl unknown
-
2016
- 2016-06-23 IL IL24643616A patent/IL246436B/en active IP Right Grant
- 2016-07-05 PH PH12016501336A patent/PH12016501336B1/en unknown
- 2016-07-13 CL CL2016001790A patent/CL2016001790A1/es unknown
- 2016-07-15 NI NI201600101A patent/NI201600101A/es unknown
- 2016-07-15 DO DO2016000177A patent/DOP2016000177A/es unknown
- 2016-07-15 SV SV2016005245A patent/SV2016005245A/es unknown
- 2016-07-15 GT GT201600147A patent/GT201600147A/es unknown
- 2016-08-16 EC ECIEPI201667692A patent/ECSP16067692A/es unknown
-
2018
- 2018-02-20 US US15/899,821 patent/US10336774B2/en active Active
- 2018-11-08 CY CY20181101177T patent/CY1121155T1/el unknown
-
2019
- 2019-05-21 US US16/418,978 patent/US10968235B2/en active Active
-
2021
- 2021-02-23 US US17/182,756 patent/US11952386B2/en active Active
- 2021-02-23 US US17/182,744 patent/US12209098B2/en active Active
- 2021-11-22 US US17/532,367 patent/US20220073537A1/en not_active Abandoned