JP2017502994A5 - - Google Patents
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- JP2017502994A5 JP2017502994A5 JP2016546924A JP2016546924A JP2017502994A5 JP 2017502994 A5 JP2017502994 A5 JP 2017502994A5 JP 2016546924 A JP2016546924 A JP 2016546924A JP 2016546924 A JP2016546924 A JP 2016546924A JP 2017502994 A5 JP2017502994 A5 JP 2017502994A5
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- Prior art keywords
- alkyl
- amino
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- hydrogen
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- Prior art date
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- 125000000217 alkyl group Chemical group 0.000 claims description 62
- 229910052739 hydrogen Inorganic materials 0.000 claims description 47
- 239000001257 hydrogen Substances 0.000 claims description 47
- 125000001475 halogen functional group Chemical group 0.000 claims description 46
- -1 amino, hydroxy Chemical group 0.000 claims description 34
- 150000002431 hydrogen Chemical class 0.000 claims description 34
- 125000003545 alkoxy group Chemical group 0.000 claims description 28
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 26
- 150000001875 compounds Chemical class 0.000 claims description 21
- 150000003839 salts Chemical class 0.000 claims description 21
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 14
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 12
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 10
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims description 10
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims description 10
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 9
- 125000001624 naphthyl group Chemical group 0.000 claims description 9
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 9
- LLAPDLPYIYKTGQ-UHFFFAOYSA-N 1-aminoethyl Chemical group C[CH]N LLAPDLPYIYKTGQ-UHFFFAOYSA-N 0.000 claims description 8
- 125000003282 alkyl amino group Chemical group 0.000 claims description 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 8
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 6
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 6
- 125000004076 pyridyl group Chemical group 0.000 claims description 6
- 125000000335 thiazolyl group Chemical group 0.000 claims description 6
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 5
- 229910052760 oxygen Inorganic materials 0.000 claims description 5
- 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
- 125000003277 amino group Chemical group 0.000 claims description 4
- 125000003118 aryl 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
- 125000001072 heteroaryl group Chemical group 0.000 claims description 4
- 125000005842 heteroatom Chemical group 0.000 claims description 4
- 230000001404 mediated effect Effects 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 229910052717 sulfur Inorganic materials 0.000 claims description 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 2
- 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
- 229910052799 carbon Inorganic materials 0.000 claims description 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 201000004101 esophageal cancer Diseases 0.000 claims description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 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
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 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
- 229910052757 nitrogen Inorganic materials 0.000 claims description 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 2
- 229920006395 saturated elastomer Polymers 0.000 claims description 2
- 201000011549 stomach cancer Diseases 0.000 claims description 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- 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
- 125000006163 5-membered heteroaryl group Chemical group 0.000 description 1
- 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 |
|---|---|---|---|
| US201461928746P | 2014-01-17 | 2014-01-17 | |
| US61/928,746 | 2014-01-17 | ||
| US201461991122P | 2014-05-09 | 2014-05-09 | |
| US61/991,122 | 2014-05-09 | ||
| PCT/IB2015/050344 WO2015107494A1 (en) | 2014-01-17 | 2015-01-16 | 1 -(triazin-3-yi_/pyridazin-3-yl)-piper(-azine)idine derivatives and compositions thereof for inhibiting the activity of shp2 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017502994A JP2017502994A (ja) | 2017-01-26 |
| JP2017502994A5 true JP2017502994A5 (enExample) | 2018-02-22 |
| JP6473457B2 JP6473457B2 (ja) | 2019-02-20 |
Family
ID=52462362
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016546924A Active JP6473457B2 (ja) | 2014-01-17 | 2015-01-16 | 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 |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US9815813B2 (enExample) |
| EP (1) | EP3094629B1 (enExample) |
| JP (1) | JP6473457B2 (enExample) |
| CN (1) | CN105899493B (enExample) |
| ES (1) | ES2699354T3 (enExample) |
| WO (1) | WO2015107494A1 (enExample) |
Families Citing this family (121)
| 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 |
| WO2015107493A1 (en) | 2014-01-17 | 2015-07-23 | Novartis Ag | 1 -pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and and compositions thereof for inhibiting the activity of shp2 |
| GB201416351D0 (en) * | 2014-09-16 | 2014-10-29 | Shire Internat Gmbh | Heterocyclic derivatives |
| EP3310774B1 (en) * | 2015-06-19 | 2020-04-29 | Novartis AG | Compounds and compositions for inhibiting the activity of shp2 |
| WO2016203404A1 (en) | 2015-06-19 | 2016-12-22 | Novartis Ag | Compounds and compositions for inhibiting the activity of shp2 |
| WO2016203405A1 (en) | 2015-06-19 | 2016-12-22 | Novartis Ag | Compounds and compositions for inhibiting the activity of shp2 |
| EP3848035B1 (en) | 2015-12-10 | 2025-02-19 | PTC Therapeutics, Inc. | 1,4-disubstituted pyridazine compounds for treating huntington's disease |
| CA3024706A1 (en) | 2016-05-31 | 2017-12-07 | Board Of Regents, The University Of Texas System | Heterocyclic inhibitors of ptpn11 |
| MA45189A (fr) * | 2016-06-07 | 2019-04-10 | Jacobio Pharmaceuticals Co Ltd | Nouveaux dérivés hétérocycliques utiles en tant qu'inhibiteurs de shp2 |
| CA3023216A1 (en) | 2016-06-14 | 2017-12-21 | Novartis Ag | Compounds and compositions for inhibiting the activity of shp2 |
| CN116478132A (zh) * | 2016-07-12 | 2023-07-25 | 锐新医药公司 | 作为变构shp2抑制剂的2,5-双取代型及2,5,6-三取代型3-甲基吡嗪 |
| 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 |
| RU2769132C2 (ru) | 2017-01-10 | 2022-03-28 | Новартис Аг | Фармацевтическая комбинация, содержащая ингибитор alk и ингибитор shp2 |
| CN110446709B (zh) | 2017-01-23 | 2023-09-12 | 锐新医药公司 | 作为变构shp2抑制剂的二环化合物 |
| AU2018210196B2 (en) | 2017-01-23 | 2022-06-02 | Revolution Medicines, Inc. | Pyridine compounds as allosteric SHP2 inhibitors |
| HRP20241239T1 (hr) * | 2017-03-23 | 2024-12-06 | Jacobio Pharmaceuticals Co., Ltd. | Novi heterociklički derivati korisni kao shp2 inhibitori |
| WO2018218133A1 (en) | 2017-05-26 | 2018-11-29 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors |
| WO2018226622A1 (en) | 2017-06-05 | 2018-12-13 | Ptc Therapeutics, Inc. | Compounds for treating huntington's disease |
| WO2019005993A1 (en) | 2017-06-28 | 2019-01-03 | Ptc Therapeutics, Inc. | METHODS OF TREATING HUNTINGTON'S DISEASE |
| BR112019027717A2 (pt) | 2017-06-28 | 2020-07-28 | Ptc Therapeutics, Inc. | métodos para tratar a doença de huntington |
| WO2019039390A1 (ja) * | 2017-08-25 | 2019-02-28 | 国立大学法人名古屋大学 | 若年性骨髄単球性白血病治療薬 |
| TWI852912B (zh) | 2017-09-07 | 2024-08-21 | 美商銳新醫藥公司 | Shp2抑制劑組合物以及治療癌症的方法 |
| 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 |
| US11701354B2 (en) | 2017-09-29 | 2023-07-18 | D. E. Shaw Research, Llc | Pyrazolo[3,4-b]pyrazine derivatives as SHP2 phosphatase inhibitors |
| CA3078565A1 (en) * | 2017-10-12 | 2019-04-18 | Revolution Medicines, Inc. | Pyridine, pyrazine, and triazine compounds as allosteric shp2 inhibitors |
| 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 |
| BR112020009757A2 (pt) | 2017-12-15 | 2020-11-03 | Revolution Medicines, Inc. | compostos policíclicos como inibidores alostéricos de shp2 |
| EP3753941B1 (en) | 2018-02-13 | 2024-05-01 | Shanghai Blueray Biopharma Co., Ltd. | Pyrimidine-fused cyclic compound, preparation method therefor and application thereof |
| MX2020008754A (es) | 2018-03-02 | 2020-12-07 | Otsuka Pharma Co Ltd | Compuestos farmaceuticos. |
| US12138263B2 (en) | 2018-03-21 | 2024-11-12 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine SHP2 phosphatase inhibitors and methods of use thereof |
| CN112368272B (zh) | 2018-03-21 | 2023-04-21 | 苏州浦合医药科技有限公司 | Shp2抑制剂及其用途 |
| KR20210015758A (ko) | 2018-03-21 | 2021-02-10 | 릴레이 테라퓨틱스, 인크. | Shp2 포스파타제 억제제 및 그의 사용 방법 |
| BR112020019373A2 (pt) | 2018-03-27 | 2020-12-29 | Ptc Therapeutics, Inc. | Compostos para o tratamento da doença de hutington |
| 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 |
| TW202014208A (zh) | 2018-05-01 | 2020-04-16 | 美商銳新醫藥公司 | 作為ｍＴＯＲ抑制劑之Ｃ４０-、Ｃ２８-及Ｃ-３２連接之雷帕黴素類似物 |
| MX2020011528A (es) | 2018-05-02 | 2021-02-09 | Navire Pharma Inc | Inhibidores heterociclicos sustituidos de ptpn11. |
| KR20210038845A (ko) | 2018-06-27 | 2021-04-08 | 피티씨 테라퓨틱스, 인크. | 헌팅턴병 치료를 위한 헤테로아릴 화합물 |
| RS65727B1 (sr) | 2018-06-27 | 2024-08-30 | Ptc Therapeutics Inc | Heterociklična i heteroaril jedinjenja za lečenje hantingtonove bolesti |
| MA53395A (fr) | 2018-07-24 | 2021-06-02 | Otsuka Pharma Co Ltd | Composés hétérobicycliques pour inhiber l'activité de shp2 |
| ES2981592T3 (es) | 2018-08-10 | 2024-10-09 | Navire Pharma Inc | Derivados de 6-(4-amino-3-metil-2-oxa-8-azaespiro[4.5]decan-8-il)-3-(2,3-diclorofenil)-2-metilpirimidin-4(3H)-ona y compuestos relacionados como inhibidores de PTPN11 (SHP2) para tratar el cáncer |
| TWI827677B (zh) | 2018-09-18 | 2024-01-01 | 美商尼坎醫療公司 | 作為src同源-2磷酸酶抑制劑之稠合三環衍生物 |
| US20210393623A1 (en) | 2018-09-26 | 2021-12-23 | Jacobio Pharmaceuticals Co., Ltd. | Novel Heterocyclic Derivatives Useful as SHP2 Inhibitors |
| IL305106B2 (en) * | 2018-09-29 | 2025-08-01 | Novartis Ag | Process of manufacture of a compound for inhibiting the activity of shp2 |
| 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 |
| WO2020072656A1 (en) | 2018-10-03 | 2020-04-09 | Gilead Sciences, Inc. | Imidozopyrimidine derivatives |
| WO2020076723A1 (en) | 2018-10-08 | 2020-04-16 | Revolution Medicines, Inc. | Shp2 inhibitor compositions for use in treating cancer |
| AU2019359885B2 (en) | 2018-10-17 | 2024-01-18 | Array Biopharma Inc. | Protein tyrosine phosphatase inhibitors |
| 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 |
| MX2021002804A (es) | 2018-12-05 | 2021-07-15 | Mirati Therapeutics Inc | Terapias de combinacion. |
| CA3130080A1 (en) | 2019-03-01 | 2020-09-10 | Revolution Medicines, Inc. | Bicyclic heteroaryl compounds and uses thereof |
| AU2020232616A1 (en) | 2019-03-01 | 2021-09-09 | Revolution Medicines, Inc. | Bicyclic heterocyclyl compounds and uses thereof |
| 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 |
| CA3135555C (en) * | 2019-04-02 | 2023-09-19 | Array Biopharma Inc. | Protein tyrosine phosphatase inhibitors |
| CN113646049B (zh) * | 2019-04-08 | 2024-08-13 | 默克专利有限公司 | 作为shp2拮抗剂的嘧啶酮衍生物 |
| 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 |
| 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 |
| AU2020354475A1 (en) * | 2019-09-24 | 2022-05-05 | Relay Therapeutics, Inc. | SHP2 phosphatase inhibitors and methods of making and using the same |
| 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 |
| CA3159559A1 (en) | 2019-11-04 | 2021-05-14 | Revolution Medicines, Inc. | Ras inhibitors |
| CN114867735A (zh) | 2019-11-04 | 2022-08-05 | 锐新医药公司 | Ras抑制剂 |
| KR20250175006A (ko) | 2019-11-04 | 2025-12-15 | 레볼루션 메디슨즈, 인크. | Ras 억제제 |
| TW202128688A (zh) | 2019-11-08 | 2021-08-01 | 美商銳新醫藥公司 | 雙環雜芳基化合物及其用途 |
| CN114980976A (zh) | 2019-11-27 | 2022-08-30 | 锐新医药公司 | 共价ras抑制剂及其用途 |
| AU2021206217A1 (en) | 2020-01-07 | 2022-09-01 | Revolution Medicines, Inc. | SHP2 inhibitor dosing and methods of treating cancer |
| AU2021226205A1 (en) | 2020-02-28 | 2022-10-20 | Novartis Ag | A triple pharmaceutical combination comprising dabrafenib, an Erk inhibitor and a SHP2 inhibitor |
| WO2021247836A1 (en) | 2020-06-03 | 2021-12-09 | Board Of Regents, The University Of Texas System | Methods for targeting shp-2 to overcome resistance |
| MX2022016355A (es) | 2020-06-18 | 2023-04-03 | Revolution Medicines Inc | Metodos para retardar, prevenir, y tratar la resistencia adquirida a inhibidores de ras. |
| 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 |
| WO2022009098A1 (en) | 2020-07-08 | 2022-01-13 | Novartis Ag | Manufacture of compounds and compositions for inhibiting the activity of shp2 |
| KR20230081726A (ko) | 2020-09-03 | 2023-06-07 | 레볼루션 메디슨즈, 인크. | Shp2 돌연변이가 있는 악성 종양을 치료하기 위한 sos1 억제제의 용도 |
| IL301298A (en) | 2020-09-15 | 2023-05-01 | Revolution Medicines Inc | Indole derivatives as RAS inhibitors in cancer therapy |
| CA3203111A1 (en) | 2020-12-22 | 2022-06-30 | Kailiang Wang | Sos1 inhibitors and uses thereof |
| 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 |
| 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 |
| EP4333850A4 (en) | 2021-05-05 | 2025-04-09 | Huyabio International, LLC | SHP2 INHIBITOR MONOTHERAPY AND ITS USES |
| CA3217084A1 (en) | 2021-05-05 | 2022-11-10 | Farbod Shojaei | Combination therapies comprising shp2 inhibitors and pd-1 inhibitors |
| CN117616031A (zh) | 2021-05-05 | 2024-02-27 | 锐新医药公司 | 用于治疗癌症的ras抑制剂 |
| 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 |
| CN115960109B (zh) * | 2021-05-31 | 2024-06-25 | 药雅科技(上海)有限公司 | 稠环类shp2磷酸酶抑制剂的制备及其应用 |
| TW202244049A (zh) * | 2021-05-12 | 2022-11-16 | 大陸商藥雅科技（上海）有限公司 | Shp2磷酸酶抑制劑的製備及其應用 |
| EP4351577A1 (en) | 2021-06-09 | 2024-04-17 | F. Hoffmann-La Roche AG | Combination therapy for cancer treatment |
| TW202313041A (zh) | 2021-06-09 | 2023-04-01 | 瑞士商諾華公司 | 包含達拉菲尼、曲美替尼和shp2抑制劑之三重藥物組合 |
| JP2024521579A (ja) | 2021-06-09 | 2024-06-03 | エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト | がんの治療における使用のための特定のｂｒａｆ阻害剤（パラドックスブレーカー）とｐｄ－１軸結合アンタゴニストとの組み合わせ |
| 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 |
| US20240374571A1 (en) | 2021-09-01 | 2024-11-14 | 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 |
| KR20240105382A (ko) | 2021-11-04 | 2024-07-05 | 에프. 호프만-라 로슈 아게 | 암 치료를 위한 퀴나졸리논 화합물의 신규한 용도 |
| 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 |
| 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 |
| IL317476A (en) | 2022-06-10 | 2025-02-01 | Revolution Medicines Inc | Macrocyclic RAS inhibitors |
| EP4345101A1 (en) | 2022-09-29 | 2024-04-03 | Irbm S.P.A. | Azole derivatives as shp2 inhibitors |
| WO2024126660A1 (en) | 2022-12-15 | 2024-06-20 | F. Hoffmann-La Roche Ag | Combination therapy for cancer treatment |
| CN116332908B (zh) * | 2023-03-21 | 2024-07-02 | 杭州医学院 | 一种shp2变构抑制剂及其制备方法和应用 |
| WO2024206858A1 (en) | 2023-03-30 | 2024-10-03 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| 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 |
| US20240352038A1 (en) | 2023-04-14 | 2024-10-24 | Revolution Medicines, Inc. | Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof |
| WO2024216016A1 (en) | 2023-04-14 | 2024-10-17 | Revolution Medicines, Inc. | Crystalline forms of a ras inhibitor |
| WO2024218632A1 (en) | 2023-04-17 | 2024-10-24 | Array Biopharma Inc. | Erk protein kinase inhibitors |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | 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 |
| WO2025036475A1 (en) * | 2023-08-17 | 2025-02-20 | Jacobio Pharmaceuticals Co., Ltd. | A pharmaceutical combination and use thereof |
| WO2025075693A1 (en) * | 2023-10-02 | 2025-04-10 | Purdue Research Foundation | Shp2 degraders for cancer therapy |
| TW202530228A (zh) | 2023-10-12 | 2025-08-01 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| WO2025106901A1 (en) | 2023-11-17 | 2025-05-22 | Quanta Therapeutics, Inc. | Combination cancer therapies with a kras modulator and an rtk-mapk pathway inhibitor |
| WO2025137507A1 (en) | 2023-12-22 | 2025-06-26 | Regor Pharmaceuticals, Inc. | Sos1 inhibitors and uses thereof |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| 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 |
| WO2025261943A1 (en) | 2024-06-18 | 2025-12-26 | F. Hoffmann-La Roche Ag | Anti-cancer combinations comprising mosperafenib and folfox or folfiri |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| CN119798246B (zh) * | 2024-12-20 | 2025-08-05 | 山东大学齐鲁医院 | 靶向shp2的荧光探针、制备方法及其应用 |
Family Cites Families (69)
| 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 |
| US3426011A (en) | 1967-02-13 | 1969-02-04 | Corn Products Co | Cyclodextrins with anionic properties |
| US3453257A (en) | 1967-02-13 | 1969-07-01 | Corn Products Co | Cyclodextrin with cationic 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 |
| 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 |
| US4959368A (en) | 1986-02-24 | 1990-09-25 | Mitsui Petrochemical Industries Ltd. | Therapeutic agent for neurological diseases |
| 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 |
| 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 |
| 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 |
| 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 |
| EP1438053B1 (de) | 2001-10-17 | 2008-09-10 | Boehringer Ingelheim Pharma GmbH & Co.KG | Pyrimidinderivate, arzneimittel enthaltend diese verbindungen, deren verwendung und verfahren zu ihrer herstellung |
| EP2407473A3 (en) | 2002-02-01 | 2012-03-21 | ARIAD Pharmaceuticals, Inc | Method for producing phosphorus-containing compounds |
| EP1482924B1 (en) | 2002-03-05 | 2008-05-21 | Merck Frosst Canada Ltd. | Cathepsin cysteine protease inhibitors |
| TWI275390B (en) | 2002-04-30 | 2007-03-11 | Wyeth Corp | Process for the preparation of 7-substituted-3- quinolinecarbonitriles |
| US7399865B2 (en) | 2003-09-15 | 2008-07-15 | Wyeth | Protein tyrosine kinase enzyme inhibitors |
| CA2562126A1 (en) | 2004-04-01 | 2005-10-13 | Astellas Pharma Inc. | Pyrazine derivatives and pharmaceutical use thereof |
| WO2005117909A2 (en) * | 2004-04-23 | 2005-12-15 | Exelixis, Inc. | Kinase modulators and methods of use |
| AU2005282722C1 (en) | 2004-09-02 | 2011-08-18 | Curis, Inc. | Pyridyl inhibitors of hedgehog signalling |
| CA2580401C (en) | 2004-09-30 | 2015-06-30 | Lg Electronics Inc. | A method of supporting operation of sleep mode in a wideband radio access system |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| AU2006290715A1 (en) | 2005-09-13 | 2007-03-22 | Palau Pharma, S.A. | 2-aminopyrimidine derivatives as modulators of the histamine H4 receptor activity |
| US7515405B2 (en) | 2006-07-25 | 2009-04-07 | Hewlett-Packard Development Company, L.P. | Anti-rotation mechanism for an electronic device |
| WO2008031556A2 (en) * | 2006-09-12 | 2008-03-20 | Ucb Pharma, S.A. | 2 amino-pyrimidine derivatives as h4 receptor antagonists, processes for preparing them and their use in pharmaceutical compositions |
| US20090137549A1 (en) | 2006-11-09 | 2009-05-28 | Paul John Edward | Novel compounds useful for the treatment of degenerative & inflamatory diseases |
| NZ578744A (en) * | 2007-01-31 | 2012-02-24 | Vertex Pharma | 2-aminopyridine derivatives useful as kinase inhibitors |
| EP2120573A4 (en) | 2007-02-12 | 2011-05-25 | Merck Sharp & Dohme | piperidine |
| KR101473504B1 (ko) * | 2007-03-15 | 2014-12-16 | 노파르티스 아게 | 유기 화합물 및 그의 용도 |
| US8247397B2 (en) | 2007-09-12 | 2012-08-21 | Genentech, Inc. | Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use |
| CN101909631B (zh) | 2007-10-25 | 2012-09-12 | 健泰科生物技术公司 | 制备噻吩并嘧啶化合物的方法 |
| BRPI0910668A2 (pt) | 2008-04-22 | 2019-09-24 | Portola Pharmaceutiacals Inc | inibidores de proteína quinases |
| WO2009150230A1 (en) | 2008-06-13 | 2009-12-17 | 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 |
| MX2010013876A (es) | 2008-06-20 | 2011-03-04 | Metabolex Inc | Agonistas de arilo grpr119 y sus usos . |
| TWI546290B (zh) | 2008-06-27 | 2016-08-21 | 賽基艾維洛米斯研究股份有限公司 | 雜芳基化合物及其用途 |
| WO2010048149A2 (en) | 2008-10-20 | 2010-04-29 | Kalypsys, Inc. | Heterocyclic modulators of gpr119 for treatment of disease |
| CA2743134A1 (en) * | 2008-11-10 | 2010-05-14 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| JP2012511567A (ja) | 2008-12-10 | 2012-05-24 | ドン ファ ファーム カンパニー リミテッド | 新規の２，６−置換−３−ニトロピリジン誘導体、その製造方法及びこれを含む薬学組成物 |
| FR2941696B1 (fr) | 2009-02-05 | 2011-04-15 | Sanofi Aventis | Derives d'azaspiranyl-alkylcarbamates d'heterocycles a 5 chainons, leur preparation et leur application en therapeutique |
| WO2010121212A2 (en) | 2009-04-17 | 2010-10-21 | H. Lee Moffit Cancer Center And Research Institute, Inc. | Indoline scaffold shp-2 inhibitors and method of treating cancer |
| BR112012003637A2 (pt) * | 2009-08-17 | 2017-04-25 | Memorial Sloan Kettering Cancer Center | "compostos de ligação de proteína de choque térmico, composições, e métodos para preparar e usar os mesmos" |
| 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 |
| BR112012033770A2 (pt) | 2010-06-30 | 2016-11-22 | Fujifilm Corp | novo derivado de nicotinamida ou sal do mesmo |
| WO2012009217A1 (en) | 2010-07-13 | 2012-01-19 | Merck Sharp & Dohme Corp. | Spirocyclic compounds |
| CA2806341C (en) | 2010-07-29 | 2020-03-24 | Rigel Pharmaceuticals, Inc. | Ampk-activating heterocyclic compounds and methods for using the same |
| US8609672B2 (en) * | 2010-08-27 | 2013-12-17 | University Of The Pacific | Piperazinylpyrimidine analogues as protein kinase inhibitors |
| US9056865B2 (en) | 2010-10-20 | 2015-06-16 | Pfizer Inc. | Pyridine-2-derivatives as smoothened receptor modulators |
| KR101992505B1 (ko) | 2011-09-12 | 2019-06-24 | 메르크 파텐트 게엠베하 | 키나아제 활성의 조절제로서 용도를 위한 아미노피리미딘 유도체 |
| WO2013096093A1 (en) | 2011-12-21 | 2013-06-27 | Merck Sharp & Dohme Corp. | Compounds as dgat-1 inhibitors |
| MX2014014582A (es) | 2012-06-07 | 2015-05-11 | Hoffmann La Roche | Inhibidores pirazolopirimidona y pirazolopiridona de tanquirasa. |
| WO2014054053A1 (en) | 2012-10-03 | 2014-04-10 | Advinus Therapeutics Limited | Spirocyclic compounds, compositions and medicinal applications thereof |
| US9499522B2 (en) * | 2013-03-15 | 2016-11-22 | Blueprint Medicines Corporation | Compositions useful for treating disorders related to kit |
| WO2015107493A1 (en) | 2014-01-17 | 2015-07-23 | Novartis Ag | 1 -pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and and compositions thereof for inhibiting the activity of shp2 |
| JO3517B1 (ar) | 2014-01-17 | 2020-07-05 | Novartis Ag | ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2 |
| EA036672B8 (ru) | 2014-05-01 | 2021-01-13 | Селджен Квонтисел Рисёрч, Инк. | Ингибиторы лизин-специфической деметилазы-1 |
| US10174032B2 (en) | 2014-05-05 | 2019-01-08 | Signalrx Pharmaceuticals, Inc. | Heterocyclic compound classes for signaling modulation |
| WO2016203404A1 (en) | 2015-06-19 | 2016-12-22 | Novartis Ag | Compounds and compositions for inhibiting the activity of shp2 |
| EP3310774B1 (en) | 2015-06-19 | 2020-04-29 | 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 |
-
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- 2015-01-16 JP JP2016546924A patent/JP6473457B2/ja active Active
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