JP2020503299A5 - - Google Patents
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- Publication number
- JP2020503299A5 JP2020503299A5 JP2019531992A JP2019531992A JP2020503299A5 JP 2020503299 A5 JP2020503299 A5 JP 2020503299A5 JP 2019531992 A JP2019531992 A JP 2019531992A JP 2019531992 A JP2019531992 A JP 2019531992A JP 2020503299 A5 JP2020503299 A5 JP 2020503299A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- imidazol
- ethynyl
- benzo
- trifluoromethyl
- 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
- -1 -NH 2 Chemical group 0.000 claims description 61
- 150000001875 compounds Chemical class 0.000 claims description 55
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims description 42
- 125000000217 alkyl group Chemical group 0.000 claims description 29
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 28
- 229910052739 hydrogen Inorganic materials 0.000 claims description 26
- 239000001257 hydrogen Substances 0.000 claims description 24
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 22
- 150000003839 salts Chemical class 0.000 claims description 19
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 18
- 208000035475 disorder Diseases 0.000 claims description 17
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 17
- 125000005842 heteroatom Chemical group 0.000 claims description 16
- 125000001072 heteroaryl group Chemical group 0.000 claims description 15
- 238000000034 method Methods 0.000 claims description 15
- 229910052760 oxygen Inorganic materials 0.000 claims description 14
- 229910052717 sulfur Inorganic materials 0.000 claims description 14
- 125000001424 substituent group Chemical group 0.000 claims description 12
- 206010028980 Neoplasm Diseases 0.000 claims description 11
- 201000010099 disease Diseases 0.000 claims description 11
- 125000004663 dialkyl amino group Chemical group 0.000 claims description 10
- 125000001188 haloalkyl group Chemical group 0.000 claims description 10
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 9
- 125000003118 aryl group Chemical group 0.000 claims description 9
- 230000001404 mediated effect Effects 0.000 claims description 9
- IIYVNMXPYWIJBL-UHFFFAOYSA-N 4-(trifluoromethyl)pyridine Chemical compound FC(F)(F)C1=CC=NC=C1 IIYVNMXPYWIJBL-UHFFFAOYSA-N 0.000 claims description 8
- 125000003282 alkyl amino group Chemical group 0.000 claims description 8
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 8
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 8
- 102000016971 Proto-Oncogene Proteins c-kit Human genes 0.000 claims description 7
- 108010014608 Proto-Oncogene Proteins c-kit Proteins 0.000 claims description 7
- 125000003545 alkoxy group Chemical group 0.000 claims description 7
- 201000011510 cancer Diseases 0.000 claims description 7
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims description 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 6
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims description 6
- 210000004027 cell Anatomy 0.000 claims description 5
- 229910052736 halogen Inorganic materials 0.000 claims description 5
- 150000002367 halogens Chemical class 0.000 claims description 5
- 150000002431 hydrogen Chemical class 0.000 claims description 5
- 230000002062 proliferating effect Effects 0.000 claims description 5
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 5
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 4
- 206010041067 Small cell lung cancer Diseases 0.000 claims description 4
- 201000008736 Systemic mastocytosis Diseases 0.000 claims description 4
- 208000000587 small cell lung carcinoma Diseases 0.000 claims description 4
- 206010020751 Hypersensitivity Diseases 0.000 claims description 3
- 208000006673 asthma Diseases 0.000 claims description 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 3
- 230000003176 fibrotic effect Effects 0.000 claims description 3
- 208000008585 mastocytosis Diseases 0.000 claims description 3
- 208000030159 metabolic disease Diseases 0.000 claims description 3
- 201000006417 multiple sclerosis Diseases 0.000 claims description 3
- PVOAHINGSUIXLS-UHFFFAOYSA-N 1-Methylpiperazine Chemical compound CN1CCNCC1 PVOAHINGSUIXLS-UHFFFAOYSA-N 0.000 claims description 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 2
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 2
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims description 2
- LKJPYSCBVHEWIU-UHFFFAOYSA-N N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide Chemical group C=1C=C(C#N)C(C(F)(F)F)=CC=1NC(=O)C(O)(C)CS(=O)(=O)C1=CC=C(F)C=C1 LKJPYSCBVHEWIU-UHFFFAOYSA-N 0.000 claims description 2
- 206010029260 Neuroblastoma Diseases 0.000 claims description 2
- 208000009905 Neurofibromatoses Diseases 0.000 claims description 2
- 208000024313 Testicular Neoplasms Diseases 0.000 claims description 2
- 206010057644 Testis cancer Diseases 0.000 claims description 2
- 201000007455 central nervous system cancer Diseases 0.000 claims description 2
- 208000035250 cutaneous malignant susceptibility to 1 melanoma Diseases 0.000 claims description 2
- 208000024558 digestive system cancer Diseases 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 210000005002 female reproductive tract Anatomy 0.000 claims description 2
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 claims description 2
- 201000010231 gastrointestinal system cancer Diseases 0.000 claims description 2
- 125000002883 imidazolyl group Chemical group 0.000 claims description 2
- 230000002757 inflammatory effect Effects 0.000 claims description 2
- 208000032839 leukemia Diseases 0.000 claims description 2
- 201000006512 mast cell neoplasm Diseases 0.000 claims description 2
- 208000006971 mastocytoma Diseases 0.000 claims description 2
- 201000001441 melanoma Diseases 0.000 claims description 2
- 125000004312 morpholin-2-yl group Chemical group [H]N1C([H])([H])C([H])([H])OC([H])(*)C1([H])[H] 0.000 claims description 2
- 125000001064 morpholinomethyl group Chemical group [H]C([H])(*)N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H] 0.000 claims description 2
- 125000002757 morpholinyl group Chemical group 0.000 claims description 2
- 201000004931 neurofibromatosis Diseases 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000003386 piperidinyl group Chemical group 0.000 claims description 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 2
- 201000003774 sarcomatosis Diseases 0.000 claims description 2
- 210000004116 schwann cell Anatomy 0.000 claims description 2
- 201000003120 testicular cancer Diseases 0.000 claims description 2
- 125000001425 triazolyl group Chemical group 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 4
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 239000000651 prodrug Substances 0.000 description 8
- 229940002612 prodrug Drugs 0.000 description 8
- 239000012453 solvate Substances 0.000 description 8
- 125000004076 pyridyl group Chemical group 0.000 description 5
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 description 2
- 125000004193 piperazinyl group Chemical group 0.000 description 2
- 208000030961 allergic reaction Diseases 0.000 description 1
- 206010003246 arthritis Diseases 0.000 description 1
- 230000001363 autoimmune Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 208000037765 diseases and disorders Diseases 0.000 description 1
- 125000000336 imidazol-5-yl group Chemical group [H]N1C([H])=NC([H])=C1[*] 0.000 description 1
- 208000027866 inflammatory disease Diseases 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 230000010534 mechanism of action Effects 0.000 description 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022163367A JP2022185110A (ja) | 2016-12-15 | 2022-10-11 | Ｃ－ｋｉｔ阻害剤としてのベンズイミダゾール化合物 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662434839P | 2016-12-15 | 2016-12-15 | |
| US62/434,839 | 2016-12-15 | ||
| PCT/US2017/066299 WO2018112140A1 (en) | 2016-12-15 | 2017-12-14 | Benzimidazole compounds as c-kit inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022163367A Division JP2022185110A (ja) | 2016-12-15 | 2022-10-11 | Ｃ－ｋｉｔ阻害剤としてのベンズイミダゾール化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020503299A JP2020503299A (ja) | 2020-01-30 |
| JP2020503299A5 true JP2020503299A5 (enExample) | 2021-01-28 |
| JP7158383B2 JP7158383B2 (ja) | 2022-10-21 |
Family
ID=60888754
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019531992A Active JP7158383B2 (ja) | 2016-12-15 | 2017-12-14 | Ｃ－ｋｉｔ阻害剤としてのベンズイミダゾール化合物 |
| JP2022163367A Pending JP2022185110A (ja) | 2016-12-15 | 2022-10-11 | Ｃ－ｋｉｔ阻害剤としてのベンズイミダゾール化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022163367A Pending JP2022185110A (ja) | 2016-12-15 | 2022-10-11 | Ｃ－ｋｉｔ阻害剤としてのベンズイミダゾール化合物 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US11117883B2 (enExample) |
| EP (1) | EP3555066A1 (enExample) |
| JP (2) | JP7158383B2 (enExample) |
| KR (1) | KR20190092538A (enExample) |
| CN (3) | CN110291081B (enExample) |
| AU (3) | AU2017376629B2 (enExample) |
| BR (1) | BR112019012224A2 (enExample) |
| CA (1) | CA3047107A1 (enExample) |
| EA (1) | EA201991197A1 (enExample) |
| IL (3) | IL314209A (enExample) |
| MA (1) | MA53150A (enExample) |
| MX (2) | MX390348B (enExample) |
| WO (1) | WO2018112140A1 (enExample) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110291081B (zh) * | 2016-12-15 | 2023-01-31 | 阿瑞雅德制药公司 | 作为c-kit抑制剂的苯并咪唑化合物 |
| CN109320503B (zh) * | 2018-12-10 | 2022-07-01 | 怀化学院 | 苯并咪唑炔胺类化合物的无金属一锅合成方法 |
| CN114364798A (zh) | 2019-03-21 | 2022-04-15 | 欧恩科斯欧公司 | 用于治疗癌症的Dbait分子与激酶抑制剂的组合 |
| US20220401436A1 (en) | 2019-11-08 | 2022-12-22 | INSERM (Institute National de la Santé et de la Recherche Médicale) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
| US11845723B2 (en) | 2019-12-24 | 2023-12-19 | Gilead Sciences, Inc. | Diacylglycerol kinase modulating compounds |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| CR20220396A (es) | 2020-02-14 | 2022-11-14 | Jounce Therapeutics Inc | Anticuerpos y proteínas de fusión que se unen a ccr8 y usos de estos |
| CN117377671A (zh) | 2021-06-23 | 2024-01-09 | 吉利德科学公司 | 二酰基甘油激酶调节化合物 |
| IL309378A (en) | 2021-06-23 | 2024-02-01 | Gilead Sciences Inc | Diacylglyercol kinase modulating compounds |
| AU2022297367B2 (en) | 2021-06-23 | 2025-04-10 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| CA3222277A1 (en) | 2021-06-23 | 2022-12-29 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| WO2023076983A1 (en) | 2021-10-28 | 2023-05-04 | Gilead Sciences, Inc. | Pyridizin-3(2h)-one derivatives |
| PE20241186A1 (es) | 2021-10-29 | 2024-06-03 | Gilead Sciences Inc | Compuestos de cd73 |
| JP2024545193A (ja) | 2021-12-22 | 2024-12-05 | ギリアード サイエンシーズ， インコーポレイテッド | Ｉｋａｒｏｓジンクフィンガーファミリー分解剤及びその使用 |
| AU2022419982A1 (en) | 2021-12-22 | 2024-06-06 | Gilead Sciences, Inc. | Ikaros zinc finger family degraders and uses thereof |
| TW202340168A (zh) | 2022-01-28 | 2023-10-16 | 美商基利科學股份有限公司 | Ｐａｒｐ７抑制劑 |
| EP4493554A1 (en) | 2022-03-17 | 2025-01-22 | Gilead Sciences, Inc. | Ikaros zinc finger family degraders and uses thereof |
| AU2023256670A1 (en) | 2022-04-21 | 2024-10-17 | Gilead Sciences, Inc. | Kras g12d modulating compounds |
| WO2024006929A1 (en) | 2022-07-01 | 2024-01-04 | Gilead Sciences, Inc. | Cd73 compounds |
| AU2023409398A1 (en) | 2022-12-22 | 2025-06-05 | Gilead Sciences, Inc. | Prmt5 inhibitors and uses thereof |
| WO2024215754A1 (en) | 2023-04-11 | 2024-10-17 | Gilead Sciences, Inc. | Kras modulating compounds |
| AU2024259556A1 (en) | 2023-04-21 | 2025-10-23 | Gilead Sciences, Inc. | Prmt5 inhibitors and uses thereof |
| US20250042922A1 (en) | 2023-06-30 | 2025-02-06 | Gilead Sciences, Inc. | Kras modulating compounds |
| TW202519517A (zh) | 2023-07-26 | 2025-05-16 | 美商基利科學股份有限公司 | Ｐａｒｐ７抑制劑 |
| WO2025024663A1 (en) | 2023-07-26 | 2025-01-30 | Gilead Sciences, Inc. | Parp7 inhibitors |
| US20250109147A1 (en) | 2023-09-08 | 2025-04-03 | Gilead Sciences, Inc. | Kras g12d modulating compounds |
| WO2025054347A1 (en) | 2023-09-08 | 2025-03-13 | Gilead Sciences, Inc. | Kras g12d modulating compounds |
| WO2025096589A1 (en) | 2023-11-03 | 2025-05-08 | Gilead Sciences, Inc. | Prmt5 inhibitors and uses thereof |
| WO2025137640A1 (en) | 2023-12-22 | 2025-06-26 | Gilead Sciences, Inc. | Azaspiro wrn inhibitors |
| US20250376484A1 (en) | 2024-05-21 | 2025-12-11 | Gilead Sciences, Inc. | Prmt5 inhibitors and uses thereof |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5262564A (en) | 1992-10-30 | 1993-11-16 | Octamer, Inc. | Sulfinic acid adducts of organo nitroso compounds useful as retroviral inactivating agents anti-retroviral agents and anti-tumor agents |
| UA82395C2 (en) * | 2003-08-21 | 2008-04-10 | Оси Фармасьютикалз, Инк. | N-substituted benzimidazolyl c-kit inhibitors |
| US7419995B2 (en) * | 2004-12-01 | 2008-09-02 | Osi Pharmaceuticals, Inc. | N-substituted benzimidazoyl c-Kit inhibitors and combinatorial benzimidazole library |
| UA94055C2 (en) * | 2005-08-30 | 2011-04-11 | Новартис Аг | Substituted benzimidazoles and methods of preparation |
| EP2493460A4 (en) * | 2009-10-30 | 2013-04-24 | Ariad Pharma Inc | METHOD AND COMPOSITIONS FOR THE TREATMENT OF CANCER |
| EA024729B1 (ru) * | 2009-11-13 | 2016-10-31 | Джиноско | Киназные ингибиторы |
| EP2694064A1 (en) * | 2011-04-07 | 2014-02-12 | Ariad Pharmaceuticals, Incorporated | Methods and compositions for treating neurodegenerative diseases |
| CN103664787B (zh) * | 2012-09-17 | 2015-09-09 | 南京圣和药业股份有限公司 | 炔杂芳环化合物及其应用 |
| CA3167093A1 (en) * | 2012-12-12 | 2014-06-12 | Ariad Pharmaceuticals, Inc. | Crystalline form c of 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-n-{4-[(4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl}benzamide mono hydrochloride |
| GB2522226A (en) * | 2014-01-17 | 2015-07-22 | Agency Science Tech & Res | Heteroaryl alkyne derivatives and uses thereof |
| CN110291081B (zh) * | 2016-12-15 | 2023-01-31 | 阿瑞雅德制药公司 | 作为c-kit抑制剂的苯并咪唑化合物 |
-
2017
- 2017-12-14 CN CN201780085539.3A patent/CN110291081B/zh not_active Expired - Fee Related
- 2017-12-14 BR BR112019012224-9A patent/BR112019012224A2/pt not_active Application Discontinuation
- 2017-12-14 AU AU2017376629A patent/AU2017376629B2/en not_active Ceased
- 2017-12-14 CN CN202211737801.7A patent/CN116283910A/zh active Pending
- 2017-12-14 EA EA201991197A patent/EA201991197A1/ru unknown
- 2017-12-14 US US16/469,535 patent/US11117883B2/en not_active Expired - Fee Related
- 2017-12-14 KR KR1020197020159A patent/KR20190092538A/ko not_active Abandoned
- 2017-12-14 CA CA3047107A patent/CA3047107A1/en active Pending
- 2017-12-14 IL IL314209A patent/IL314209A/en unknown
- 2017-12-14 CN CN202211731994.5A patent/CN116178343A/zh active Pending
- 2017-12-14 MX MX2019007080A patent/MX390348B/es unknown
- 2017-12-14 EP EP17822994.4A patent/EP3555066A1/en not_active Withdrawn
- 2017-12-14 IL IL287517A patent/IL287517B2/en unknown
- 2017-12-14 WO PCT/US2017/066299 patent/WO2018112140A1/en not_active Ceased
- 2017-12-14 JP JP2019531992A patent/JP7158383B2/ja active Active
- 2017-12-14 MA MA053150A patent/MA53150A/fr unknown
-
2019
- 2019-06-12 IL IL267260A patent/IL267260B2/en unknown
- 2019-06-14 MX MX2022002581A patent/MX2022002581A/es unknown
-
2021
- 2021-08-12 US US17/400,820 patent/US20220064144A1/en not_active Abandoned
-
2022
- 2022-02-18 AU AU2022201082A patent/AU2022201082B2/en not_active Ceased
- 2022-10-11 JP JP2022163367A patent/JP2022185110A/ja active Pending
-
2024
- 2024-02-01 AU AU2024200624A patent/AU2024200624A1/en not_active Abandoned
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