JP2022185110A5 - - Google Patents
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- JP2022185110A5 JP2022185110A5 JP2022163367A JP2022163367A JP2022185110A5 JP 2022185110 A5 JP2022185110 A5 JP 2022185110A5 JP 2022163367 A JP2022163367 A JP 2022163367A JP 2022163367 A JP2022163367 A JP 2022163367A JP 2022185110 A5 JP2022185110 A5 JP 2022185110A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- compound according
- alkyl
- composition
- cancer
- 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.)
- Pending
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- 150000001875 compounds Chemical class 0.000 claims 36
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 36
- 239000000203 mixture Substances 0.000 claims 21
- 125000000217 alkyl group Chemical group 0.000 claims 20
- 208000035475 disorder Diseases 0.000 claims 20
- 201000010099 disease Diseases 0.000 claims 16
- 150000003839 salts Chemical class 0.000 claims 15
- 230000001404 mediated effect Effects 0.000 claims 14
- 206010028980 Neoplasm Diseases 0.000 claims 10
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 9
- 125000005842 heteroatom Chemical group 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 239000001257 hydrogen Substances 0.000 claims 9
- 229910052760 oxygen Inorganic materials 0.000 claims 9
- 229910052717 sulfur Inorganic materials 0.000 claims 9
- 102000016971 Proto-Oncogene Proteins c-kit Human genes 0.000 claims 8
- 108010014608 Proto-Oncogene Proteins c-kit Proteins 0.000 claims 8
- 201000011510 cancer Diseases 0.000 claims 8
- 125000004663 dialkyl amino group Chemical group 0.000 claims 7
- 125000001072 heteroaryl group Chemical group 0.000 claims 7
- 125000001188 haloalkyl group Chemical group 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 6
- 125000003282 alkyl amino group Chemical group 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 4
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 4
- 206010041067 Small cell lung cancer Diseases 0.000 claims 4
- 201000008736 Systemic mastocytosis Diseases 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 210000004027 cell Anatomy 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 125000004438 haloalkoxy group Chemical group 0.000 claims 4
- 238000004519 manufacturing process Methods 0.000 claims 4
- 230000002062 proliferating effect Effects 0.000 claims 4
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 2
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims 2
- 206010020751 Hypersensitivity Diseases 0.000 claims 2
- 206010029260 Neuroblastoma Diseases 0.000 claims 2
- 208000009905 Neurofibromatoses Diseases 0.000 claims 2
- 206010039491 Sarcoma Diseases 0.000 claims 2
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 2
- 206010057644 Testis cancer Diseases 0.000 claims 2
- 208000030961 allergic reaction Diseases 0.000 claims 2
- 206010003246 arthritis Diseases 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 201000007455 central nervous system cancer Diseases 0.000 claims 2
- 208000035250 cutaneous malignant susceptibility to 1 melanoma Diseases 0.000 claims 2
- 210000005002 female reproductive tract Anatomy 0.000 claims 2
- 230000003176 fibrotic effect Effects 0.000 claims 2
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 claims 2
- 230000002757 inflammatory effect Effects 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 208000032839 leukemia Diseases 0.000 claims 2
- 201000006512 mast cell neoplasm Diseases 0.000 claims 2
- 208000006971 mastocytoma Diseases 0.000 claims 2
- 208000008585 mastocytosis Diseases 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 208000030159 metabolic disease Diseases 0.000 claims 2
- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 201000004931 neurofibromatosis Diseases 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 210000004116 schwann cell Anatomy 0.000 claims 2
- 201000003120 testicular cancer Diseases 0.000 claims 2
- ZBJYXLSUSCJBGC-UHFFFAOYSA-N 4-methyl-3-[2-(1-methylbenzimidazol-5-yl)ethynyl]-N-[4-(4-methylpiperazin-1-yl)-3-(trifluoromethyl)phenyl]benzamide Chemical compound CC1=C(C=C(C(=O)NC2=CC(=C(C=C2)N2CCN(CC2)C)C(F)(F)F)C=C1)C#CC1=CC2=C(N(C=N2)C)C=C1 ZBJYXLSUSCJBGC-UHFFFAOYSA-N 0.000 claims 1
- CUCKRCGHXDJPGI-UHFFFAOYSA-N 4-methyl-3-[2-(1-methylbenzimidazol-5-yl)ethynyl]-N-[4-(pyrrolidin-1-ylmethyl)-3-(trifluoromethyl)phenyl]benzamide Chemical compound CC1=C(C=C(C(=O)NC2=CC(=C(C=C2)CN2CCCC2)C(F)(F)F)C=C1)C#CC1=CC2=C(N(C=N2)C)C=C1 CUCKRCGHXDJPGI-UHFFFAOYSA-N 0.000 claims 1
- VDPNLHZVSBNNJR-UHFFFAOYSA-N 4-methyl-3-[2-[1-(1-methylpyrazol-4-yl)benzimidazol-5-yl]ethynyl]-N-[4-(pyrrolidin-1-ylmethyl)-3-(trifluoromethyl)phenyl]benzamide Chemical compound CC1=C(C=C(C(=O)NC2=CC(=C(C=C2)CN2CCCC2)C(F)(F)F)C=C1)C#CC1=CC2=C(N(C=N2)C=2C=NN(C=2)C)C=C1 VDPNLHZVSBNNJR-UHFFFAOYSA-N 0.000 claims 1
- LQMCDBWJLBZNOW-UHFFFAOYSA-N N-(3-cyclopropylphenyl)-4-methyl-3-[2-[1-(1-methylpyrazol-4-yl)benzimidazol-5-yl]ethynyl]benzamide Chemical compound Cc1ccc(cc1C#Cc1ccc2n(cnc2c1)-c1cnn(C)c1)C(=O)Nc1cccc(c1)C1CC1 LQMCDBWJLBZNOW-UHFFFAOYSA-N 0.000 claims 1
- YUFYIJYOJIFZJR-UHFFFAOYSA-N N-[4-cyano-3-(trifluoromethyl)phenyl]-4-methyl-3-[2-[1-(1-methylpyrazol-3-yl)benzimidazol-5-yl]ethynyl]benzamide Chemical compound C(#N)C1=C(C=C(C=C1)NC(C1=CC(=C(C=C1)C)C#CC1=CC2=C(N(C=N2)C2=NN(C=C2)C)C=C1)=O)C(F)(F)F YUFYIJYOJIFZJR-UHFFFAOYSA-N 0.000 claims 1
- UOYWOMANQPPHLW-UHFFFAOYSA-N N-[4-methyl-3-[2-(1-methylbenzimidazol-5-yl)ethynyl]phenyl]-4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)benzamide Chemical compound CC1=C(C=C(C=C1)NC(C1=CC(=C(C=C1)CN1CCN(CC1)C)C(F)(F)F)=O)C#CC1=CC2=C(N(C=N2)C)C=C1 UOYWOMANQPPHLW-UHFFFAOYSA-N 0.000 claims 1
- FLLUGTDVYBTZED-UHFFFAOYSA-N N-[4-methyl-3-[2-[1-(1-methylpyrazol-4-yl)benzimidazol-5-yl]ethynyl]phenyl]-4-(morpholin-4-ylmethyl)-3-(trifluoromethyl)benzamide Chemical compound CC1=C(C=C(C=C1)NC(C1=CC(=C(C=C1)CN1CCOCC1)C(F)(F)F)=O)C#CC1=CC2=C(N(C=N2)C=2C=NN(C=2)C)C=C1 FLLUGTDVYBTZED-UHFFFAOYSA-N 0.000 claims 1
- QFHCBCHHBUYSOH-UHFFFAOYSA-N N-[4-methyl-3-[2-[1-(1-methylpyrazol-4-yl)benzimidazol-5-yl]ethynyl]phenyl]-4-(pyrrolidin-1-ylmethyl)-3-(trifluoromethyl)benzamide Chemical compound CC1=C(C=C(C=C1)NC(C1=CC(=C(C=C1)CN1CCCC1)C(F)(F)F)=O)C#CC1=CC2=C(N(C=N2)C=2C=NN(C=2)C)C=C1 QFHCBCHHBUYSOH-UHFFFAOYSA-N 0.000 claims 1
- VCDLXHKPHNTEMR-UHFFFAOYSA-N N-[4-methyl-3-[2-[1-(1-methylpyrazol-4-yl)benzimidazol-5-yl]ethynyl]phenyl]-4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)benzamide Chemical compound CC1=C(C=C(C=C1)NC(C1=CC(=C(C=C1)CN1CCN(CC1)C)C(F)(F)F)=O)C#CC1=CC2=C(N(C=N2)C=2C=NN(C=2)C)C=C1 VCDLXHKPHNTEMR-UHFFFAOYSA-N 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000003226 pyrazolyl group Chemical class 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
Applications Claiming Priority (4)
| 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 |
| JP2019531992A 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 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019531992A Division 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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2022185110A JP2022185110A (ja) | 2022-12-13 |
| JP2022185110A5 true JP2022185110A5 (https=) | 2023-03-22 |
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 Before (1)
| 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 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US11117883B2 (https=) |
| EP (1) | EP3555066A1 (https=) |
| JP (2) | JP7158383B2 (https=) |
| KR (1) | KR20190092538A (https=) |
| CN (3) | CN116283910A (https=) |
| AU (3) | AU2017376629B2 (https=) |
| BR (1) | BR112019012224A2 (https=) |
| CA (1) | CA3047107A1 (https=) |
| EA (1) | EA201991197A1 (https=) |
| IL (3) | IL314209A (https=) |
| MA (1) | MA53150A (https=) |
| MX (2) | MX390348B (https=) |
| WO (1) | WO2018112140A1 (https=) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA201991197A1 (ru) * | 2016-12-15 | 2020-01-13 | Ариад Фармасьютикалз, Инк. | БЕНЗИМИДАЗОЛЬНЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ c-Kit |
| 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 |
| US20220143049A1 (en) | 2019-03-21 | 2022-05-12 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| EP4054579A1 (en) | 2019-11-08 | 2022-09-14 | Institut National de la Santé et de la Recherche Médicale (INSERM) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
| LT4081305T (lt) | 2019-12-24 | 2024-11-25 | Carna Biosciences, Inc. | Diacilglicerolio kinazę moduliuojantys junginiai |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| KR20260017503A (ko) | 2020-02-14 | 2026-02-05 | 길리애드 사이언시즈, 인코포레이티드 | Ccr8에 결합하는 항체 및 융합 단백질, 및 이의 용도 |
| WO2022271677A1 (en) | 2021-06-23 | 2022-12-29 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| WO2022271659A1 (en) | 2021-06-23 | 2022-12-29 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| KR20240005901A (ko) | 2021-06-23 | 2024-01-12 | 길리애드 사이언시즈, 인코포레이티드 | 디아실글리세롤 키나제 조절 화합물 |
| CA3222277A1 (en) | 2021-06-23 | 2022-12-29 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| US20230183216A1 (en) | 2021-10-28 | 2023-06-15 | Gilead Sciences, Inc. | Pyridizin-3(2h)-one derivatives |
| EP4422756A1 (en) | 2021-10-29 | 2024-09-04 | Gilead Sciences, Inc. | Cd73 compounds |
| CN118488946A (zh) | 2021-12-22 | 2024-08-13 | 吉利德科学公司 | Ikaros锌指家族降解剂及其用途 |
| EP4452415B1 (en) | 2021-12-22 | 2026-02-25 | 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 |
| CA3253296A1 (en) | 2022-03-17 | 2023-09-21 | Gilead Sciences, Inc. | Zinc Finger Degradation Agents of the Ikaros Family and Their Uses |
| WO2023205719A1 (en) | 2022-04-21 | 2023-10-26 | Gilead Sciences, Inc. | Kras g12d modulating compounds |
| US20240116928A1 (en) | 2022-07-01 | 2024-04-11 | Gilead Sciences, Inc. | Cd73 compounds |
| EP4638436A1 (en) | 2022-12-22 | 2025-10-29 | Gilead Sciences, Inc. | Prmt5 inhibitors and uses thereof |
| CN120882725A (zh) | 2023-04-11 | 2025-10-31 | 吉利德科学公司 | Kras调节化合物 |
| WO2024220917A1 (en) | 2023-04-21 | 2024-10-24 | Gilead Sciences, Inc. | Prmt5 inhibitors and uses thereof |
| US20250042922A1 (en) | 2023-06-30 | 2025-02-06 | Gilead Sciences, Inc. | Kras modulating compounds |
| AU2024297978A1 (en) | 2023-07-26 | 2026-02-05 | Gilead Sciences, Inc. | Parp7 inhibitors |
| US20250066328A1 (en) | 2023-07-26 | 2025-02-27 | Gilead Sciences, Inc. | Parp7 inhibitors |
| WO2025054347A1 (en) | 2023-09-08 | 2025-03-13 | Gilead Sciences, Inc. | Kras g12d modulating compounds |
| AU2024337913A1 (en) | 2023-09-08 | 2026-03-26 | Gilead Sciences, Inc. | Pyrimidine-containing polycyclic derivatives as kras g12d modulating compounds |
| US20250154172A1 (en) | 2023-11-03 | 2025-05-15 | 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 |
| WO2026039365A1 (en) | 2024-08-12 | 2026-02-19 | Gilead Sciences, Inc. | Kras modulating compounds |
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 |
| AU2004268949A1 (en) * | 2003-08-21 | 2005-03-10 | Osi Pharmaceuticals, Inc. | N-substituted benzimidazolyl C-kit inhibitors |
| EP1831206B1 (en) * | 2004-12-01 | 2011-08-24 | OSI Pharmaceuticals, Inc. | N-substituted benzimidazolyl c-kit inhibitors and combinatorial benzimidazole library |
| CN101253168B (zh) * | 2005-08-30 | 2012-12-12 | 诺瓦提斯公司 | 作为激酶抑制剂的被取代的苯并咪唑类物质 |
| CA2777128A1 (en) * | 2009-10-30 | 2011-05-05 | Ariad Pharmaceuticals, Inc. | Methods and compositions for treating cancer |
| MX2012005332A (es) * | 2009-11-13 | 2012-10-15 | Oscotec Inc | Inhibidores de cinasa. |
| CA2832483A1 (en) * | 2011-04-07 | 2012-10-11 | Ariad Pharmaceuticals, Inc. | 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 |
| CA3022250A1 (en) * | 2012-12-12 | 2014-06-12 | Ariad Pharmaceuticals, Inc. | Crystalline forms 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 |
| EA201991197A1 (ru) * | 2016-12-15 | 2020-01-13 | Ариад Фармасьютикалз, Инк. | БЕНЗИМИДАЗОЛЬНЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ c-Kit |
-
2017
- 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 BR BR112019012224-9A patent/BR112019012224A2/pt not_active Application Discontinuation
- 2017-12-14 CN CN202211737801.7A patent/CN116283910A/zh active Pending
- 2017-12-14 IL IL314209A patent/IL314209A/en unknown
- 2017-12-14 AU AU2017376629A patent/AU2017376629B2/en not_active Ceased
- 2017-12-14 IL IL287517A patent/IL287517B2/en unknown
- 2017-12-14 EP EP17822994.4A patent/EP3555066A1/en not_active Withdrawn
- 2017-12-14 JP JP2019531992A patent/JP7158383B2/ja active Active
- 2017-12-14 MX MX2019007080A patent/MX390348B/es unknown
- 2017-12-14 CN CN201780085539.3A patent/CN110291081B/zh not_active Expired - Fee Related
- 2017-12-14 MA MA053150A patent/MA53150A/fr unknown
- 2017-12-14 WO PCT/US2017/066299 patent/WO2018112140A1/en not_active Ceased
- 2017-12-14 CN CN202211731994.5A patent/CN116178343A/zh active Pending
- 2017-12-14 CA CA3047107A patent/CA3047107A1/en active Pending
-
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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