JP2018517752A5 - - Google Patents
Download PDFInfo
- Publication number
- 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.)
- Granted
Links
- 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 (enExample) | 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 (enExample) |
| EP (1) | EP3310774B1 (enExample) |
| JP (1) | JP6718889B2 (enExample) |
| CN (2) | CN107922388B (enExample) |
| ES (1) | ES2805232T3 (enExample) |
| WO (1) | WO2016203406A1 (enExample) |
Families Citing this family (118)
| 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 |
| ES2699354T3 (es) | 2014-01-17 | 2019-02-08 | Novartis Ag | Derivados de 1-(triazin-3-il/piridazin-3-il)-piper(-azin)idina y composiciones de las mismas para inhibir la actividad de SHP2 |
| EP3094627B1 (en) | 2014-01-17 | 2018-08-22 | Novartis AG | 1-pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and and compositions thereof for inhibiting the activity of shp2 |
| WO2016203406A1 (en) * | 2015-06-19 | 2016-12-22 | Novartis Ag | Compounds and compositions for inhibiting the activity of shp2 |
| US10308660B2 (en) * | 2015-06-19 | 2019-06-04 | 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 |
| WO2017210134A1 (en) | 2016-05-31 | 2017-12-07 | Board Of Regents, University Of Texas System | Heterocyclic inhibitors of ptpn11 |
| EA202092441A1 (ru) * | 2016-06-07 | 2021-05-21 | Джакобио Фармасьютикалс Ко., Лтд. | Новые гетероциклические производные, применимые в качестве ингибиторов shp2 |
| JP6994474B2 (ja) | 2016-06-14 | 2022-01-14 | 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 |
| CN116478131A (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 |
| WO2018057884A1 (en) | 2016-09-22 | 2018-03-29 | 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 |
| CA3048340A1 (en) * | 2017-01-10 | 2018-07-19 | Novartis Ag | Pharmaceutical combination comprising an alk inhibitor and a shp2 inhibitor |
| CN110431134A (zh) * | 2017-01-23 | 2019-11-08 | 锐新医药公司 | 作为变构shp2抑制剂的吡啶化合物 |
| AU2018210770B2 (en) | 2017-01-23 | 2022-03-24 | Revolution Medicines, Inc. | Bicyclic compounds as allosteric SHP2 inhibitors |
| TWI664175B (zh) * | 2017-03-23 | 2019-07-01 | 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 |
| WO2018218133A1 (en) | 2017-05-26 | 2018-11-29 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine derivatives as shp2 phosphatase inhibitors |
| 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 |
| TWI851542B (zh) | 2017-09-11 | 2024-08-11 | 美商克魯松藥物公司 | Ｓｈｐ２之八氫環戊烷并[c]吡咯別構抑制劑 |
| WO2019067843A1 (en) | 2017-09-29 | 2019-04-04 | Relay Therapeutics, Inc. | PYRAZOLO [3,4-B] PYRAZINE DERIVATIVES AS INHIBITORS OF PHOSPHATASE SHP2 |
| KR20200070295A (ko) * | 2017-10-12 | 2020-06-17 | 레볼루션 메디슨즈, 인크. | 알로스테릭 shp2 억제제로서의 피리딘, 피라진 및 트리아진 화합물 |
| CN111433205B (zh) | 2017-12-15 | 2024-01-19 | 锐新医药公司 | 作为变构shp2抑制剂的多环化合物 |
| AU2019222026B2 (en) | 2018-02-13 | 2022-05-12 | Shanghai Blueray Biopharma Co., Ltd. | Pyrimidine-fused cyclic compound, preparation method therefor and application thereof |
| CA3092011A1 (en) | 2018-03-02 | 2019-09-06 | Otsuka Pharmaceutical Co., Ltd. | Pharmaceutical compounds |
| WO2019183364A1 (en) | 2018-03-21 | 2019-09-26 | Relay Therapeutics, Inc. | Pyrazolo[3,4-b]pyrazine shp2 phosphatase inhibitors and methods of use thereof |
| US10561655B2 (en) | 2018-03-21 | 2020-02-18 | Synblia Therapeutics, Inc. | SHP2 inhibitors and uses thereof |
| EP3768668B1 (en) | 2018-03-21 | 2024-08-28 | Relay Therapeutics, Inc. | Shp2 phosphatase inhibitors and methods of use thereof |
| EP3773590A1 (en) | 2018-04-10 | 2021-02-17 | Revolution Medicines, Inc. | Shp2 inhibitor compositions, methods for treating cancer and methods for identifying a subject with shp2 mutations |
| CR20240382A (es) | 2018-05-01 | 2025-08-29 | Revolution Medicines Inc | ANÁLOGOS DE RAPAMICINA A C40, C28 Y C32 COMO INHIBIDORES DE MTOR (Divisional 2020-578) |
| KR102611661B1 (ko) | 2018-05-02 | 2023-12-08 | 나비레 파르마, 인코퍼레이티드 | Ptpn11의 치환된 헤테로사이클릭 억제제 |
| CN112174935B (zh) * | 2018-05-09 | 2022-12-06 | 北京加科思新药研发有限公司 | 可用作shp2抑制剂的杂环衍生物 |
| MA53395A (fr) | 2018-07-24 | 2021-06-02 | Otsuka Pharma Co Ltd | Composés hétérobicycliques pour inhiber l'activité de shp2 |
| IL307361B2 (en) | 2018-08-10 | 2024-12-01 | 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 |
| WO2020061103A1 (en) | 2018-09-18 | 2020-03-26 | Nikang Therapeutics, Inc. | Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors |
| WO2020063760A1 (en) | 2018-09-26 | 2020-04-02 | Jacobio Pharmaceuticals Co., Ltd. | Novel heterocyclic derivatives useful as shp2 inhibitors |
| AU2019346118B2 (en) * | 2018-09-29 | 2024-05-16 | Novartis Ag | Manufacture of compounds and compositions for inhibiting the activity of SHP2 |
| JP2022502385A (ja) | 2018-09-29 | 2022-01-11 | 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の製造方法 |
| EP3860717A1 (en) | 2018-10-03 | 2021-08-11 | Gilead Sciences, Inc. | Imidozopyrimidine derivatives |
| EP3863636A1 (en) | 2018-10-08 | 2021-08-18 | Revolution Medicines, Inc. | Shp2 inhibitor compositions for use in treating cancer |
| 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 |
| IL282179B2 (en) | 2018-10-17 | 2024-10-01 | Array Biopharma Inc | Protein tyrosine phosphatase inhibitors |
| CN111138412B (zh) | 2018-11-06 | 2023-09-15 | 上海奕拓医药科技有限责任公司 | 一种螺芳环化合物及其应用 |
| CA3120791A1 (en) | 2018-11-30 | 2020-06-04 | Tuojie Biotech (Shanghai) Co., Ltd. | Pyrimidine and five-membered nitrogen heterocycle derivative, preparation method therefor, and medical uses thereof |
| CN113164418A (zh) | 2018-12-05 | 2021-07-23 | 米拉蒂治疗股份有限公司 | 组合疗法 |
| 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 |
| WO2020165732A1 (en) * | 2019-02-12 | 2020-08-20 | Novartis Ag | Pharmaceutical combination comprising tno155 and a krasg12c inhibitor |
| KR20210146287A (ko) | 2019-03-01 | 2021-12-03 | 레볼루션 메디슨즈, 인크. | 이환식 헤테로아릴 화합물 및 이의 용도 |
| SG11202109422WA (en) | 2019-03-01 | 2021-09-29 | 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 |
| JP7734586B2 (ja) | 2019-03-07 | 2025-09-05 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｓｈｐ２アンタゴニストとしてのカルボキサミド－ピリミジン誘導体 |
| 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 |
| 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 |
| CN114787150A (zh) * | 2019-08-15 | 2022-07-22 | 黑钻治疗公司 | 炔基喹唑啉化合物 |
| 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 |
| AR120082A1 (es) | 2019-09-24 | 2022-02-02 | Relay Therapeutics Inc | Inhibidores de fosfatasa shp-2 y métodos para fabricarlos y usarlos |
| US20240139193A1 (en) | 2019-10-15 | 2024-05-02 | Amgen Inc. | Combination therapy of kras inhibitor and shp2 inhibitor for treatment of cancers |
| WO2021091982A1 (en) | 2019-11-04 | 2021-05-14 | Revolution Medicines, Inc. | Ras inhibitors |
| CN114901366A (zh) | 2019-11-04 | 2022-08-12 | 锐新医药公司 | Ras抑制剂 |
| PH12022550988A1 (en) | 2019-11-04 | 2023-10-09 | Revolution Medicines Inc | Ras inhibitors |
| PE20230249A1 (es) | 2019-11-08 | 2023-02-07 | Revolution Medicines Inc | Compuestos de heteroarilo biciclicos y usos de estos |
| EP4065231A1 (en) | 2019-11-27 | 2022-10-05 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
| WO2021142026A1 (en) | 2020-01-07 | 2021-07-15 | 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 |
| CN113493440B (zh) * | 2020-04-03 | 2024-08-23 | 上海翰森生物医药科技有限公司 | 含氮杂芳类衍生物的盐及其晶型 |
| TW202144334A (zh) * | 2020-04-03 | 2021-12-01 | 大陸商上海翰森生物醫藥科技有限公司 | 含氮雜芳類衍生物游離鹼的晶型 |
| 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 |
| AU2021293228A1 (en) | 2020-06-18 | 2023-02-09 | Revolution Medicines, Inc. | Methods for delaying, preventing, and treating acquired resistance to RAS inhibitors |
| 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 |
| WO2022009098A1 (en) | 2020-07-08 | 2022-01-13 | 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 |
| CN116209438A (zh) | 2020-09-03 | 2023-06-02 | 锐新医药公司 | 使用sos1抑制剂治疗具有shp2突变的恶性疾病 |
| JP2023541916A (ja) | 2020-09-15 | 2023-10-04 | レボリューション メディシンズ インコーポレイテッド | がんの治療における、ｒａｓ阻害剤としてのインドール誘導体 |
| CN116348466B (zh) * | 2020-09-23 | 2025-05-30 | 上海齐鲁制药研究中心有限公司 | 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 |
| MX2023011664A (es) * | 2021-04-01 | 2023-10-11 | Array Biopharma Inc | Forma cristalina de un inhibidor de shp2. |
| CN118852330A (zh) | 2021-05-05 | 2024-10-29 | 锐新医药公司 | 用于治疗癌症的ras抑制剂 |
| EP4334318A4 (en) | 2021-05-05 | 2025-03-05 | Huyabio International, LLC | COMBINATION THERAPIES WITH SHP2 INHIBITORS AND PD-1 INHIBITORS |
| WO2022235866A1 (en) | 2021-05-05 | 2022-11-10 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
| US12390469B2 (en) | 2021-05-05 | 2025-08-19 | Huyabio International, Llc | SHP2 inhibitor monotherapy and uses thereof |
| AU2022270116A1 (en) | 2021-05-05 | 2023-12-21 | Revolution Medicines, Inc. | Ras inhibitors |
| 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 |
| AU2022306911A1 (en) * | 2021-07-07 | 2024-02-22 | Hinova Pharmaceuticals Inc. | Synthesis and application of phosphatase degrader |
| WO2023031781A1 (en) | 2021-09-01 | 2023-03-09 | 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 |
| 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 |
| CN120504682A (zh) | 2022-06-10 | 2025-08-19 | 锐新医药公司 | 大环ras抑制剂 |
| WO2024113194A1 (en) * | 2022-11-30 | 2024-06-06 | Canwell Biotech Limited | Shp2 inhibitors, compositions and methods thereof |
| TW202504611A (zh) | 2023-03-30 | 2025-02-01 | 美商銳新醫藥公司 | 用於誘導ｒａｓ ｇｔｐ水解之組合物及其用途 |
| AU2024253668A1 (en) | 2023-04-07 | 2025-11-13 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| CR20250420A (es) | 2023-04-07 | 2025-11-20 | Revolution Medicines Inc | Inhibidores macrocíclicos de ras |
| WO2024216048A1 (en) | 2023-04-14 | 2024-10-17 | 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 |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| WO2025034702A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Rmc-6291 for use in the treatment of ras protein-related disease or disorder |
| WO2025034919A1 (en) | 2023-08-08 | 2025-02-13 | Quanta Therapeutics, Inc. | Combination therapies with kras modulators |
| 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 |
| 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 |
| US20250375445A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| 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 |
| EP0799617A3 (en) | 1986-02-24 | 1997-11-12 | 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 |
| CN100522967C (zh) | 2002-02-01 | 2009-08-05 | 阿里亚德基因治疗公司 | 含磷化合物及其应用 |
| DK1482924T3 (da) | 2002-03-05 | 2008-09-29 | Merck Frosst Canada Ltd | Cathepsin-cystein-protease-inhibotorer |
| TWI275390B (en) | 2002-04-30 | 2007-03-11 | Wyeth Corp | Process for the preparation of 7-substituted-3- quinolinecarbonitriles |
| CA2517422A1 (en) | 2003-03-07 | 2004-09-16 | Merck Sharp & Dohme Limited | Tetrahydropyran compounds as tachykinin antagonists |
| US7399865B2 (en) | 2003-09-15 | 2008-07-15 | Wyeth | Protein tyrosine kinase enzyme inhibitors |
| CN1938296A (zh) | 2004-04-01 | 2007-03-28 | 安斯泰来制药有限公司 | 作为腺苷拮抗剂的吡嗪衍生物及其制药用途 |
| CA2563699C (en) | 2004-04-23 | 2014-03-25 | Exelixis, Inc. | Kinase modulators and method of use |
| KR20200019263A (ko) | 2004-09-02 | 2020-02-21 | 제넨테크, 인크. | 헤지호그 신호전달에 대한 피리딜 억제제 |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| EP1928862A1 (en) | 2005-09-13 | 2008-06-11 | 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 |
| US20090137549A1 (en) | 2006-11-09 | 2009-05-28 | Paul John Edward | Novel compounds useful for the treatment of degenerative & inflamatory diseases |
| JP2010518083A (ja) | 2007-02-12 | 2010-05-27 | メルク・シャープ・エンド・ドーム・コーポレイション | ピペリジン誘導体 |
| AR065718A1 (es) | 2007-03-15 | 2009-06-24 | Novartis Ag | Compuestos heterociclicos nitrogenados,utiles en el diagnostico y tratamiento de trastornos hiperproliferativos. |
| BRPI0816769A2 (pt) | 2007-09-12 | 2016-11-29 | Hoffmann La Roche | combinações de compostos inibidores de fosfoinositida 3-cinase e agentes quimioterapêuticos, e métodos de uso |
| ES2439705T3 (es) | 2007-10-25 | 2014-01-24 | Genentech, Inc. | Proceso para la preparación de compuestos de tienopirimidina |
| AU2009238590A1 (en) | 2008-04-22 | 2009-10-29 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| EA201100136A1 (ru) | 2008-06-13 | 2011-08-30 | Новартис Аг | 2,4'-бипиридинилы в качестве ингибиторов протеинкиназы d, применимые для лечения сердечной недостаточности и рака |
| US8168784B2 (en) | 2008-06-20 | 2012-05-01 | Abbott Laboratories | Processes to make apoptosis promoters |
| KR20110026481A (ko) | 2008-06-20 | 2011-03-15 | 메타볼렉스, 인코포레이티드 | 아릴 ｇｐｒ１１９ 작동약 및 이의 용도 |
| TWI458721B (zh) | 2008-06-27 | 2014-11-01 | Celgene Avilomics Res Inc | 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 |
| 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 |
| 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 |
| SG186877A1 (en) | 2010-06-30 | 2013-02-28 | Fujifilm Corp | Novel nicotinamide derivatives or salts thereof |
| 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 |
| SG186850A1 (en) | 2010-07-29 | 2013-02-28 | 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 |
| JP5802756B2 (ja) | 2010-10-20 | 2015-11-04 | ファイザー・インク | スムーズンド受容体モジュレーターとしてのピリジン−２−誘導体 |
| HRP20171655T1 (hr) | 2011-09-12 | 2017-12-15 | Merck Patent Gmbh | Derivati aminopirimidina za upotrebu kao modulatori aktivnosti kinaze |
| WO2013096093A1 (en) | 2011-12-21 | 2013-06-27 | Merck Sharp & Dohme Corp. | Compounds as dgat-1 inhibitors |
| BR112014030410A2 (pt) | 2012-06-07 | 2017-06-27 | Hoffmann La Roche | inibidores de pirazolopirimidona e pirazolopiridona de tanquirase |
| EP2903985A1 (en) | 2012-10-03 | 2015-08-12 | 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 |
| EP3094627B1 (en) | 2014-01-17 | 2018-08-22 | 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 |
| ES2699354T3 (es) * | 2014-01-17 | 2019-02-08 | Novartis Ag | Derivados de 1-(triazin-3-il/piridazin-3-il)-piper(-azin)idina y composiciones de las mismas para inhibir la actividad de 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 |
| US10308660B2 (en) | 2015-06-19 | 2019-06-04 | 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 |
| WO2016203406A1 (en) * | 2015-06-19 | 2016-12-22 | Novartis Ag | Compounds and compositions for inhibiting the activity of shp2 |
-
2016
- 2016-06-15 WO PCT/IB2016/053550 patent/WO2016203406A1/en not_active Ceased
- 2016-06-15 CN CN201680035707.3A patent/CN107922388B/zh active Active
- 2016-06-15 JP JP2017565777A patent/JP6718889B2/ja active Active
- 2016-06-15 EP EP16731666.0A patent/EP3310774B1/en active Active
- 2016-06-15 ES ES16731666T patent/ES2805232T3/es active Active
- 2016-06-15 CN CN202011428718.2A patent/CN112625028B/zh active Active
- 2016-06-15 US US15/736,925 patent/US10287266B2/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2018517752A5 (enExample) | ||
| JP2018517746A5 (enExample) | ||
| US20230047816A1 (en) | Pfkfb3 inhibitors and their uses | |
| CN103402519B (zh) | 肿瘤治疗剂 | |
| JP2017524005A5 (enExample) | ||
| JP2014513110A5 (enExample) | ||
| JP2017533968A5 (enExample) | ||
| HRP20171957T1 (hr) | Derivati 2-(2,4,5-supstituiranog-anilino) pirimidina kao modulatori egfr koji su korisni za liječenje raka | |
| JP2015534578A5 (enExample) | ||
| ES2911040T3 (es) | Nuevos derivados de heteroaril amida como inhibidores selectivos de histona deacetilasa 1 y 2 (HDAC1/2) | |
| JP2017502994A5 (enExample) | ||
| JP2020506951A5 (enExample) | ||
| JP2008513515A5 (enExample) | ||
| JP2017503000A5 (enExample) | ||
| JP2012507566A5 (enExample) | ||
| JP2018500342A5 (enExample) | ||
| JP2019517487A5 (enExample) | ||
| JP2017537948A5 (enExample) | ||
| JP2013056930A5 (enExample) | ||
| JP2014518544A5 (enExample) | ||
| JP2010539110A5 (enExample) | ||
| JP2016040288A5 (enExample) | ||
| RU2011108281A (ru) | Трипиридилкарбоксамидные антагонисты орексиновых рецепторов | |
| TWI664166B (zh) | Ｋｃｎｑ２至５通道活化劑 | |
| JP2015534580A5 (enExample) |