JP2016539157A5 - - Google Patents
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- Publication number
- JP2016539157A5 JP2016539157A5 JP2016536607A JP2016536607A JP2016539157A5 JP 2016539157 A5 JP2016539157 A5 JP 2016539157A5 JP 2016536607 A JP2016536607 A JP 2016536607A JP 2016536607 A JP2016536607 A JP 2016536607A JP 2016539157 A5 JP2016539157 A5 JP 2016539157A5
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- benzimidazol
- methanone
- phenyl
- pyrrolidin
- 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
- 150000003839 salts Chemical class 0.000 claims 8
- 150000001875 compounds Chemical class 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 4
- 208000011580 syndromic disease Diseases 0.000 claims 4
- CXFXCNXDHHKIKS-VWLOTQADSA-N [(2S)-2-(6-bromo-4-methyl-1H-benzimidazol-2-yl)-2-methylpyrrolidin-1-yl]-(5-methyl-2-pyrimidin-2-ylphenyl)methanone Chemical compound Cc1ccc(-c2ncccn2)c(c1)C(=O)N1CCC[C@@]1(C)c1nc2cc(Br)cc(C)c2[nH]1 CXFXCNXDHHKIKS-VWLOTQADSA-N 0.000 claims 2
- NBGABHGMJVIVBW-QHCPKHFHSA-N [(2s)-2-(5-chloro-4-methyl-1h-benzimidazol-2-yl)-2-methylpyrrolidin-1-yl]-[5-methoxy-2-(triazol-2-yl)phenyl]methanone Chemical compound N1([C@](CCC1)(C)C=1NC2=CC=C(Cl)C(C)=C2N=1)C(=O)C1=CC(OC)=CC=C1N1N=CC=N1 NBGABHGMJVIVBW-QHCPKHFHSA-N 0.000 claims 2
- 238000011282 treatment Methods 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- XWYOWTGUVQJLBN-VWLOTQADSA-N [(2S)-2-(5,6-dimethoxy-1H-benzimidazol-2-yl)-2-methylpyrrolidin-1-yl]-(5-methyl-2-pyrazol-1-ylphenyl)methanone Chemical compound COc1cc2nc([nH]c2cc1OC)[C@]1(C)CCCN1C(=O)c1cc(C)ccc1-n1cccn1 XWYOWTGUVQJLBN-VWLOTQADSA-N 0.000 claims 1
- JAOXZMJRODOOQL-DEOSSOPVSA-N [(2S)-2-(5,6-dimethoxy-1H-benzimidazol-2-yl)-2-methylpyrrolidin-1-yl]-[5-methoxy-2-(triazol-2-yl)phenyl]methanone Chemical compound COC1=CC2=C(NC(=N2)[C@]2(N(CCC2)C(=O)C2=C(C=CC(=C2)OC)N2N=CC=N2)C)C=C1OC JAOXZMJRODOOQL-DEOSSOPVSA-N 0.000 claims 1
- VCQFUAGWDVFPQB-QFIPXVFZSA-N [(2S)-2-(5-bromo-6-fluoro-1H-benzimidazol-2-yl)-2-methylpyrrolidin-1-yl]-[5-methyl-2-(triazol-2-yl)phenyl]methanone Chemical compound Cc1ccc(c(c1)C(=O)N1CCC[C@@]1(C)c1nc2cc(F)c(Br)cc2[nH]1)-n1nccn1 VCQFUAGWDVFPQB-QFIPXVFZSA-N 0.000 claims 1
- ZXEWKIMFKPFZMU-VWLOTQADSA-N [(2S)-2-(5-chloro-4-methyl-1H-benzimidazol-2-yl)-2-methylpyrrolidin-1-yl]-(5-methyl-2-pyrimidin-2-ylphenyl)methanone Chemical compound Cc1ccc(-c2ncccn2)c(c1)C(=O)N1CCC[C@@]1(C)c1nc2c(C)c(Cl)ccc2[nH]1 ZXEWKIMFKPFZMU-VWLOTQADSA-N 0.000 claims 1
- XSONELHLKWDPKV-QHCPKHFHSA-N [(2S)-2-(6-bromo-4-methyl-1H-benzimidazol-2-yl)-2-methylpyrrolidin-1-yl]-[5-methyl-2-(triazol-2-yl)phenyl]methanone Chemical compound Cc1ccc(c(c1)C(=O)N1CCC[C@@]1(C)c1nc2cc(Br)cc(C)c2[nH]1)-n1nccn1 XSONELHLKWDPKV-QHCPKHFHSA-N 0.000 claims 1
- JVWVAASSQXQBNF-QFIPXVFZSA-N [(2S)-2-[5-chloro-6-(trifluoromethyl)-1H-benzimidazol-2-yl]-2-methylpyrrolidin-1-yl]-[5-methyl-2-(triazol-2-yl)phenyl]methanone Chemical compound ClC=1C(=CC2=C(NC(=N2)[C@]2(N(CCC2)C(=O)C2=C(C=CC(=C2)C)N2N=CC=N2)C)C1)C(F)(F)F JVWVAASSQXQBNF-QFIPXVFZSA-N 0.000 claims 1
- XSNFSFXKMQPCNT-DEOSSOPVSA-N [(2s)-2-(5,6-dimethoxy-1h-benzimidazol-2-yl)-2-methylpyrrolidin-1-yl]-[5-methyl-2-(triazol-2-yl)phenyl]methanone Chemical compound C([C@@]1(C)C2=NC=3C=C(C(=CC=3N2)OC)OC)CCN1C(=O)C1=CC(C)=CC=C1N1N=CC=N1 XSNFSFXKMQPCNT-DEOSSOPVSA-N 0.000 claims 1
- DOWZCWSQZJMWOI-QFIPXVFZSA-N [5-methyl-2-(triazol-2-yl)phenyl]-[(2S)-2-methyl-2-[6-(trifluoromethoxy)-1H-benzimidazol-2-yl]pyrrolidin-1-yl]methanone Chemical compound Cc1ccc(c(c1)C(=O)N1CCC[C@@]1(C)c1nc2cc(OC(F)(F)F)ccc2[nH]1)-n1nccn1 DOWZCWSQZJMWOI-QFIPXVFZSA-N 0.000 claims 1
- VGDLIWVHXXDXQV-QFIPXVFZSA-N [5-methyl-2-(triazol-2-yl)phenyl]-[(2S)-2-methyl-2-[6-(trifluoromethyl)-1H-benzimidazol-2-yl]pyrrolidin-1-yl]methanone Chemical compound CC=1C=CC(=C(C1)C(=O)N1[C@@](CCC1)(C1=NC2=C(N1)C=CC(=C2)C(F)(F)F)C)N2N=CC=N2 VGDLIWVHXXDXQV-QFIPXVFZSA-N 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 238000011321 prophylaxis Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IBPCT/IB2013/060630 | 2013-12-04 | ||
| IB2013060630 | 2013-12-04 | ||
| PCT/IB2014/066548 WO2015083094A1 (en) | 2013-12-04 | 2014-12-03 | Use of benzimidazole-proline derivatives |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016539157A JP2016539157A (ja) | 2016-12-15 |
| JP2016539157A5 true JP2016539157A5 (enExample) | 2018-01-18 |
| JP6421185B2 JP6421185B2 (ja) | 2018-11-07 |
Family
ID=52347368
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016536607A Active JP6421185B2 (ja) | 2013-12-04 | 2014-12-03 | ベンゾイミダゾール−プロリン誘導体の使用 |
Country Status (29)
| Country | Link |
|---|---|
| US (1) | US9914721B2 (enExample) |
| EP (1) | EP3077391B1 (enExample) |
| JP (1) | JP6421185B2 (enExample) |
| KR (1) | KR102330133B1 (enExample) |
| CN (1) | CN105873921B (enExample) |
| AU (1) | AU2014358766B2 (enExample) |
| CA (1) | CA2930053A1 (enExample) |
| CL (1) | CL2016001349A1 (enExample) |
| CY (1) | CY1121089T1 (enExample) |
| DK (1) | DK3077391T3 (enExample) |
| EA (1) | EA029725B1 (enExample) |
| ES (1) | ES2696708T3 (enExample) |
| HK (1) | HK1225734B (enExample) |
| HR (1) | HRP20181710T1 (enExample) |
| HU (1) | HUE040555T2 (enExample) |
| IL (1) | IL245914B (enExample) |
| LT (1) | LT3077391T (enExample) |
| MA (1) | MA39165A1 (enExample) |
| MX (1) | MX366642B (enExample) |
| MY (1) | MY179605A (enExample) |
| PH (1) | PH12016500985B1 (enExample) |
| PL (1) | PL3077391T3 (enExample) |
| PT (1) | PT3077391T (enExample) |
| SA (1) | SA516371253B1 (enExample) |
| SI (1) | SI3077391T1 (enExample) |
| TR (1) | TR201815342T4 (enExample) |
| UA (1) | UA116053C2 (enExample) |
| WO (1) | WO2015083094A1 (enExample) |
| ZA (1) | ZA201604502B (enExample) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101995683B1 (ko) | 2012-06-04 | 2019-07-02 | 이도르시아 파마슈티컬스 리미티드 | 벤즈이미다졸-프롤린 유도체 |
| UA119151C2 (uk) | 2013-12-03 | 2019-05-10 | Ідорсія Фармасьютікалз Лтд | КРИСТАЛІЧНА СОЛЬОВА ФОРМА (S)-(2-(6-ХЛОР-7-МЕТИЛ-1H-БЕНЗО[d]ІМІДАЗОЛ-2-ІЛ)-2-МЕТИЛПІРОЛІДИН-1-ІЛ)(5-МЕТОКСИ-2-(2H-1,2,3-ТРИАЗОЛ-2-ІЛ)ФЕНІЛ)МЕТАНОНУ ЯК АНТАГОНІСТ ОРЕКСИНОВОГО РЕЦЕПТОРА |
| US9914720B2 (en) | 2013-12-03 | 2018-03-13 | Idorsia Pharmaceuticals Ltd | Crystalline form of (S)-(2-(6-chloro-7-methyl-1H-benzo[D]imidazol-2-yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone and its use as orexin receptor antagonists |
| HK1225734B (en) | 2013-12-04 | 2017-09-15 | Idorsia Pharmaceuticals Ltd | Use of benzimidazole-proline derivatives |
| WO2017012502A1 (en) | 2015-07-17 | 2017-01-26 | Sunshine Lake Pharma Co., Ltd. | Substituted quinazoline compounds and preparation and uses thereof |
| US10370380B2 (en) | 2015-11-23 | 2019-08-06 | Sunshine Lake Pharma Co., Ltd. | Octahydropyrrolo[3,4-c]pyrrole derivatives and uses thereof |
| KR102582197B1 (ko) | 2017-05-03 | 2023-09-22 | 이도르시아 파마슈티컬스 리미티드 | 2-([1,2,3]트리아졸-2-일)-벤조산 유도체의 제조 |
| JP2023521492A (ja) * | 2020-04-19 | 2023-05-24 | イドーシア ファーマシューティカルズ リミテッド | ダリドレキサントの医学的用途 |
| CN116783182B (zh) * | 2021-02-02 | 2025-08-29 | 南京明德新药研发有限公司 | 四氢吡咯并环化合物及其应用 |
| WO2023160004A1 (zh) * | 2022-02-25 | 2023-08-31 | 南京知和医药科技有限公司 | 具有镇痛活性的稠环化合物及其制备方法与用途 |
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| KR101995683B1 (ko) | 2012-06-04 | 2019-07-02 | 이도르시아 파마슈티컬스 리미티드 | 벤즈이미다졸-프롤린 유도체 |
| SG11201502493XA (en) | 2012-10-10 | 2015-04-29 | Actelion Pharmaceuticals Ltd | Orexin receptor antagonists which are [ortho bi (hetero )aryl]-[2-(meta bi (hetero )aryl)-pyrrolidin-1-yl]-methanone derivatives |
| EP2970241A1 (en) | 2013-03-12 | 2016-01-20 | Actelion Pharmaceuticals Ltd. | Azetidine amide derivatives as orexin receptor antagonists |
| US9914720B2 (en) | 2013-12-03 | 2018-03-13 | Idorsia Pharmaceuticals Ltd | Crystalline form of (S)-(2-(6-chloro-7-methyl-1H-benzo[D]imidazol-2-yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone and its use as orexin receptor antagonists |
| UA119151C2 (uk) | 2013-12-03 | 2019-05-10 | Ідорсія Фармасьютікалз Лтд | КРИСТАЛІЧНА СОЛЬОВА ФОРМА (S)-(2-(6-ХЛОР-7-МЕТИЛ-1H-БЕНЗО[d]ІМІДАЗОЛ-2-ІЛ)-2-МЕТИЛПІРОЛІДИН-1-ІЛ)(5-МЕТОКСИ-2-(2H-1,2,3-ТРИАЗОЛ-2-ІЛ)ФЕНІЛ)МЕТАНОНУ ЯК АНТАГОНІСТ ОРЕКСИНОВОГО РЕЦЕПТОРА |
| HK1225734B (en) | 2013-12-04 | 2017-09-15 | Idorsia Pharmaceuticals Ltd | Use of benzimidazole-proline derivatives |
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- 2014-12-03 KR KR1020167017709A patent/KR102330133B1/ko active Active
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