JP2018517752A5 - - Google Patents
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- JP2018517752A5 JP2018517752A5 JP2017565777A JP2017565777A JP2018517752A5 JP 2018517752 A5 JP2018517752 A5 JP 2018517752A5 JP 2017565777 A JP2017565777 A JP 2017565777A JP 2017565777 A JP2017565777 A JP 2017565777A JP 2018517752 A5 JP2018517752 A5 JP 2018517752A5
- Authority
- JP
- Japan
- Prior art keywords
- hydrogen
- amino
- methyl
- fluoro
- alkyl
- 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.)
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- 229910052739 hydrogen Inorganic materials 0.000 claims description 112
- 239000001257 hydrogen Substances 0.000 claims description 112
- 150000002431 hydrogen Chemical class 0.000 claims description 94
- 125000000217 alkyl group Chemical group 0.000 claims description 78
- 125000005843 halogen group Chemical group 0.000 claims description 70
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 70
- 125000001153 fluoro group Chemical group F* 0.000 claims description 66
- -1 cyclopropyl-carbonyl-amino Chemical group 0.000 claims description 54
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 44
- 150000003839 salts Chemical class 0.000 claims description 40
- 125000003545 alkoxy group Chemical group 0.000 claims description 30
- 150000001875 compounds Chemical class 0.000 claims description 26
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 20
- 229910052757 nitrogen Inorganic materials 0.000 claims description 20
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 20
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 18
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 18
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims description 16
- PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 claims description 14
- LPIQUOYDBNQMRZ-UHFFFAOYSA-N cyclopentene Chemical compound C1CC=CC1 LPIQUOYDBNQMRZ-UHFFFAOYSA-N 0.000 claims description 12
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims description 10
- 229910052799 carbon Inorganic materials 0.000 claims description 10
- 125000004432 carbon atom Chemical group C* 0.000 claims description 10
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 10
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 10
- 125000001064 morpholinomethyl group Chemical group [H]C([H])(*)N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H] 0.000 claims description 10
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 claims description 10
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 8
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 8
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 8
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 claims description 6
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims description 6
- RGSFGYAAUTVSQA-UHFFFAOYSA-N pentamethylene Natural products C1CCCC1 RGSFGYAAUTVSQA-UHFFFAOYSA-N 0.000 claims description 6
- 125000003396 thiol group Chemical group [H]S* 0.000 claims description 6
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims description 6
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 4
- PIGFYZPCRLYGLF-UHFFFAOYSA-N Aluminum nitride Chemical compound [Al]#N PIGFYZPCRLYGLF-UHFFFAOYSA-N 0.000 claims description 4
- MHZGKXUYDGKKIU-UHFFFAOYSA-N Decylamine Chemical compound CCCCCCCCCCN MHZGKXUYDGKKIU-UHFFFAOYSA-N 0.000 claims description 4
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-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
- 201000010099 disease Diseases 0.000 claims description 4
- 208000035475 disorder Diseases 0.000 claims description 4
- 230000000694 effects Effects 0.000 claims description 4
- 229910052731 fluorine Inorganic materials 0.000 claims description 4
- 239000011737 fluorine Substances 0.000 claims description 4
- 125000005842 heteroatom Chemical group 0.000 claims description 4
- 230000001404 mediated effect Effects 0.000 claims description 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 4
- 229910052760 oxygen Inorganic materials 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 229910052717 sulfur Inorganic materials 0.000 claims description 4
- MYTHQSLASJNVRG-MRXNPFEDSA-N (4R)-8-[5-(2-aminophenyl)sulfanylpyrazin-2-yl]-8-azaspiro[4.5]decan-4-amine Chemical compound NC1=C(C=CC=C1)SC=1N=CC(=NC=1)N1CCC2(CCC[C@H]2N)CC1 MYTHQSLASJNVRG-MRXNPFEDSA-N 0.000 claims description 2
- KOUHTVINHNKPPC-LJQANCHMSA-N (4R)-8-[5-(2-tert-butylphenyl)sulfanylpyrazin-2-yl]-8-azaspiro[4.5]decan-4-amine Chemical compound C(C)(C)(C)C1=C(C=CC=C1)SC=1N=CC(=NC=1)N1CCC2(CCC[C@H]2N)CC1 KOUHTVINHNKPPC-LJQANCHMSA-N 0.000 claims description 2
- OBSORTGEYVDFIG-MRXNPFEDSA-N (4R)-8-[5-[2-(trifluoromethyl)phenyl]sulfanylpyrazin-2-yl]-8-azaspiro[4.5]decan-4-amine Chemical compound FC(C1=C(C=CC=C1)SC=1N=CC(=NC=1)N1CCC2(CCC[C@H]2N)CC1)(F)F OBSORTGEYVDFIG-MRXNPFEDSA-N 0.000 claims description 2
- PCDXJTLHNWHOPH-MRXNPFEDSA-N (4R)-8-[5-[3-(trifluoromethoxy)phenyl]sulfanylpyrazin-2-yl]-8-azaspiro[4.5]decan-4-amine Chemical compound FC(OC=1C=C(C=CC=1)SC=1N=CC(=NC=1)N1CCC2(CCC[C@H]2N)CC1)(F)F PCDXJTLHNWHOPH-MRXNPFEDSA-N 0.000 claims description 2
- ABADUMLIAZCWJD-UHFFFAOYSA-N 1,3-dioxole Chemical compound C1OC=CO1 ABADUMLIAZCWJD-UHFFFAOYSA-N 0.000 claims description 2
- JKTCBAGSMQIFNL-UHFFFAOYSA-N 2,3-dihydrofuran Chemical compound C1CC=CO1 JKTCBAGSMQIFNL-UHFFFAOYSA-N 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
- 206010009944 Colon cancer 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
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 claims description 2
- 125000001246 bromo group Chemical group Br* 0.000 claims description 2
- CWJSHJJYOPWUGX-UHFFFAOYSA-N chlorpropham Chemical compound CC(C)OC(=O)NC1=CC=CC(Cl)=C1 CWJSHJJYOPWUGX-UHFFFAOYSA-N 0.000 claims description 2
- 208000029742 colonic neoplasm Diseases 0.000 claims description 2
- 239000003814 drug Substances 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
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([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
- 125000004674 methylcarbonyl group Chemical group CC(=O)* 0.000 claims description 2
- VXPLXMJHHKHSOA-UHFFFAOYSA-N propham Chemical compound CC(C)OC(=O)NC1=CC=CC=C1 VXPLXMJHHKHSOA-UHFFFAOYSA-N 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
- 125000004076 pyridyl group Chemical group 0.000 claims description 2
- 201000011549 stomach cancer Diseases 0.000 claims description 2
- 230000000069 prophylactic effect Effects 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 description 2
- 230000004075 alteration Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562181893P | 2015-06-19 | 2015-06-19 | |
| US62/181,893 | 2015-06-19 | ||
| PCT/IB2016/053550 WO2016203406A1 (en) | 2015-06-19 | 2016-06-15 | Compounds and compositions for inhibiting the activity of shp2 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018517752A JP2018517752A (ja) | 2018-07-05 |
| JP2018517752A5 true JP2018517752A5 (cg-RX-API-DMAC7.html) | 2019-07-18 |
| JP6718889B2 JP6718889B2 (ja) | 2020-07-08 |
Family
ID=56194530
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017565777A Active JP6718889B2 (ja) | 2015-06-19 | 2016-06-15 | Ｓｈｐ２の活性を阻害するための化合物および組成物 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US10287266B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP3310774B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP6718889B2 (cg-RX-API-DMAC7.html) |
| CN (2) | CN112625028B (cg-RX-API-DMAC7.html) |
| ES (1) | ES2805232T3 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2016203406A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (113)
| 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 |
| 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 |
| 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 |
| ES2741746T3 (es) | 2015-06-19 | 2020-02-12 | Novartis Ag | Compuestos y composiciones para inhibir la actividad de SHP2 |
| 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 |
| 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 |
| 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 |
| CA3051206A1 (en) | 2017-01-23 | 2018-07-26 | Revolution Medicines, Inc. | Bicyclic compounds as allosteric shp2 inhibitors |
| CA3051054A1 (en) * | 2017-01-23 | 2018-07-26 | Revolution Medicines, Inc. | Pyridine 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 |
| 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 |
| MX2020006273A (es) | 2017-12-15 | 2020-09-14 | Revolution Medicines Inc | Compuestos policiclicos como inhibidores alostericos de shp2. |
| AU2019222026B2 (en) | 2018-02-13 | 2022-05-12 | 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. |
| AU2019240299B2 (en) * | 2018-03-21 | 2023-06-22 | D.E. Shaw Research, Llc | SHP2 phosphatase inhibitors and methods of use thereof |
| WO2019183364A1 (en) | 2018-03-21 | 2019-09-26 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine shp2 phosphatase inhibitors and methods of use thereof |
| 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 |
| 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 |
| BR112021005606A2 (pt) | 2018-09-29 | 2021-06-22 | Novartis Ag | processo de produção de um composto para inibir a atividade de shp2 |
| 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 |
| US11179397B2 (en) | 2018-10-03 | 2021-11-23 | Gilead Sciences, Inc. | Imidazopyrimidine derivatives |
| CN113473990A (zh) | 2018-10-08 | 2021-10-01 | 锐新医药公司 | 用于治疗癌症的shp2抑制剂组合物 |
| 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 |
| 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 |
| WO2020156243A1 (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 |
| 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 |
| WO2020180768A1 (en) | 2019-03-01 | 2020-09-10 | Revolution Medicines, Inc. | Bicyclic heteroaryl compounds and uses thereof |
| US20230096028A1 (en) | 2019-03-01 | 2023-03-30 | 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 |
| 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 |
| 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 |
| CA3150701A1 (en) * | 2019-08-15 | 2021-02-18 | Black Diamond Therapeutics, Inc. | Alkynyl quinazoline compounds |
| GB201911928D0 (en) | 2019-08-20 | 2019-10-02 | Otsuka Pharma Co Ltd | Pharmaceutical compounds |
| US20230010886A1 (en) * | 2019-09-23 | 2023-01-12 | Suzhou Puhe BioPharma Co., Ltd. | Shp2 inhibitors and uses thereof |
| US11890281B2 (en) | 2019-09-24 | 2024-02-06 | Relay Therapeutics, Inc. | SHP2 phosphatase inhibitors and methods of making and using the same |
| US20240139193A1 (en) | 2019-10-15 | 2024-05-02 | Amgen Inc. | Combination therapy of kras inhibitor and shp2 inhibitor for treatment of cancers |
| TW202132315A (zh) | 2019-11-04 | 2021-09-01 | 美商銳新醫藥公司 | Ras 抑制劑 |
| CN115873067A (zh) | 2019-11-04 | 2023-03-31 | 锐新医药公司 | Ras抑制剂 |
| AU2020379734B2 (en) | 2019-11-04 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| MX2022005525A (es) | 2019-11-08 | 2022-06-08 | Revolution Medicines Inc | Compuestos de heteroarilo bicíclicos y usos de estos. |
| EP4065231A1 (en) | 2019-11-27 | 2022-10-05 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
| CA3163703A1 (en) | 2020-01-07 | 2021-07-15 | Steve Kelsey | Shp2 inhibitor dosing and methods of treating cancer |
| 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 |
| CN113754683A (zh) | 2020-06-05 | 2021-12-07 | 上海奕拓医药科技有限责任公司 | 同位素取代的螺芳环化合物及其应用 |
| 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 |
| ES3040751T3 (en) | 2020-07-08 | 2025-11-04 | Novartis Ag | Manufacture of compounds and compositions for inhibiting the activity of shp2 |
| CN114195799B (zh) * | 2020-09-02 | 2025-01-28 | 勤浩医药（苏州）有限公司 | 吡嗪类衍生物及其在抑制shp2中的应用 |
| 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 |
| CN112062699B (zh) * | 2020-11-13 | 2021-02-26 | 苏州开元民生科技股份有限公司 | 一种邻氨基苯硫酚的制备方法 |
| WO2022140427A1 (en) | 2020-12-22 | 2022-06-30 | Qilu Regor Therapeutics Inc. | Sos1 inhibitors and uses thereof |
| CN113376301B (zh) * | 2020-12-25 | 2022-11-15 | 上海药坦药物研究开发有限公司 | 一种2-氨基-3-氯吡啶-4-硫醇钠的检测方法 |
| CA3215295A1 (en) * | 2021-04-01 | 2022-10-06 | Array Biopharma Inc. | Crystalline form of a shp2 inhibitor |
| EP4334318A4 (en) | 2021-05-05 | 2025-03-05 | Huyabio International, LLC | COMBINATION THERAPIES WITH SHP2 INHIBITORS AND PD-1 INHIBITORS |
| 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 |
| 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 |
| 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 |
| 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 |
| CN118019537A (zh) * | 2021-09-28 | 2024-05-10 | 上海翰森生物医药科技有限公司 | Shp2抑制剂联合egfr-tki治疗和预防肿瘤疾病的医药用途 |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| CN116063307B (zh) * | 2021-10-29 | 2025-08-19 | 中国药科大学 | Shp2与cdk4/6双靶点抑制化合物合成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 |
| AU2023285116A1 (en) | 2022-06-10 | 2024-12-19 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| WO2024113194A1 (en) * | 2022-11-30 | 2024-06-06 | Canwell Biotech Limited | Shp2 inhibitors, compositions and methods thereof |
| 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 |
| 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 |
| CN121100123A (zh) | 2023-04-14 | 2025-12-09 | 锐新医药公司 | Ras抑制剂的结晶形式 |
| 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 |
| 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 |
| WO2025242126A1 (zh) * | 2024-05-22 | 2025-11-27 | 上海正大天晴医药科技开发有限公司 | 一种药物组合及其应用 |
| 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 |
| 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 (66)
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| EP1603901B1 (en) | 2003-03-07 | 2008-10-15 | MERCK SHARP & DOHME LTD. | Tetrahydropyran compounds as tachykinin antagonists |
| US7399865B2 (en) | 2003-09-15 | 2008-07-15 | Wyeth | Protein tyrosine kinase enzyme inhibitors |
| 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 |
| KR20180122750A (ko) | 2004-09-02 | 2018-11-13 | 제넨테크, 인크. | 헤지호그 신호전달에 대한 피리딜 억제제 |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| KR20080043840A (ko) | 2005-09-13 | 2008-05-19 | 팔라우 파르마 에스에이 | 히스타민 ｈ4 수용체 활성의 조정자로서 2-아미노피리미딘유도체 |
| 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 |
| 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 |
| 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 |
| WO2010048149A2 (en) | 2008-10-20 | 2010-04-29 | Kalypsys, Inc. | Heterocyclic modulators of gpr119 for treatment of disease |
| CN102356066A (zh) | 2008-12-10 | 2012-02-15 | 同和药品株式会社 | 新型2，6-取代的-3-硝基吡啶衍生物、其制备方法及包含有其的药物组合物 |
| FR2941696B1 (fr) | 2009-02-05 | 2011-04-15 | Sanofi Aventis | Derives d'azaspiranyl-alkylcarbamates d'heterocycles a 5 chainons, leur preparation et leur application en therapeutique |
| WO2010121212A2 (en) * | 2009-04-17 | 2010-10-21 | H. Lee Moffit Cancer Center And Research Institute, Inc. | Indoline scaffold shp-2 inhibitors and method of treating cancer |
| 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 |
| 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 |
| HUE034979T2 (en) | 2011-09-12 | 2018-05-02 | Merck Patent Gmbh | Aminopyrimidine derivatives for use as modulators of kinase activity |
| 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 |
| 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 |
| 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 |
| JO3517B1 (ar) * | 2014-01-17 | 2020-07-05 | Novartis Ag | ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2 |
| 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 |
| 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 |
| 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 |
-
2016
- 2016-06-15 JP JP2017565777A patent/JP6718889B2/ja active Active
- 2016-06-15 CN CN202011428718.2A patent/CN112625028B/zh active Active
- 2016-06-15 WO PCT/IB2016/053550 patent/WO2016203406A1/en not_active Ceased
- 2016-06-15 US US15/736,925 patent/US10287266B2/en active Active
- 2016-06-15 ES ES16731666T patent/ES2805232T3/es active Active
- 2016-06-15 EP EP16731666.0A patent/EP3310774B1/en active Active
- 2016-06-15 CN CN201680035707.3A patent/CN107922388B/zh active Active