RU94015171A - Derivatives of benzimidazole and a mixture of their isomers or individual isomers and their acid-additive salt - Google Patents
Derivatives of benzimidazole and a mixture of their isomers or individual isomers and their acid-additive saltInfo
- Publication number
- RU94015171A RU94015171A RU94015171/04A RU94015171A RU94015171A RU 94015171 A RU94015171 A RU 94015171A RU 94015171/04 A RU94015171/04 A RU 94015171/04A RU 94015171 A RU94015171 A RU 94015171A RU 94015171 A RU94015171 A RU 94015171A
- Authority
- RU
- Russia
- Prior art keywords
- carbon atoms
- alkyl
- unsubstituted
- isomers
- disubstituted
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title claims 2
- 150000003839 salts Chemical class 0.000 title claims 2
- 239000011780 sodium chloride Substances 0.000 title claims 2
- 239000000654 additive Substances 0.000 title 1
- 125000003785 benzimidazolyl group Chemical class N1=C(NC2=C1C=CC=C2)* 0.000 title 1
- 125000004432 carbon atoms Chemical group C* 0.000 claims 18
- 125000000217 alkyl group Chemical group 0.000 claims 7
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- BNBQRQQYDMDJAH-UHFFFAOYSA-N Benzodioxan Chemical compound C1=CC=C2OCCOC2=C1 BNBQRQQYDMDJAH-UHFFFAOYSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000004442 acylamino group Chemical group 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 claims 1
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 1
- -1 aminosulfonylamino group Chemical group 0.000 claims 1
- 230000003042 antagnostic Effects 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 150000008641 benzimidazolones Chemical class 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000004417 unsaturated alkyl group Chemical group 0.000 claims 1
Claims (1)
где R1 и R2 одинаковы или различны и означают атом водорода, атом галогена, трифторметил, алкил с 1 - 6 атомами углерода, алкокси с 1 - 6 атомами углерода, алкилтио с 1 - 6 атомами углерода, ацил с 1 - 6 атомами углерода, карбоксил, алкоксикарбонил с 1 - 6 атомами углерода, гидрокси, нитро-группу или амино-группу, незамещенную или N-моно- или дизамещенную алкилом с 1 - 4 атомами углерода, ациламино с 1 - 6 атомами углерода, алкоксикарбониламино с 1 - 6 атомами углерода, карбамоил, незамещенный или N-моно- или дизамещенный алкилом с 1 - 4 атомами углерода, циано, алкилсульфинил с 1 - 6 атомами углерода, аминосульфонил, незамещенный или N-моно- или дизамещенный алкилом с 1 - 4 атомами углерода, или аминосульфониламино-группу, незамещенную или N-моно- или дизамещенную алкилом с 1 - 4 атомами углерода; R3 - атом водорода, алкил с 1 - 6 атомами углерода, алкенил с 2 - 6 атомами углерода или алкинил с 2 - 6 атомами углерода; А - группа -CO- или -CONH-, или же А отсутствует; В - неразветвленный или разветвленный, насыщенный или ненасыщенный алкил с 2 - 6 атомами углерода; m и n независимо друг от друга означают целое число 1 - 3; R4 - фенил, нафтил или бензодиоксан, незамещенные или замещенные по меньшей мере одним заместителем из группы, включающей атом галогена, трифторметил, циано, алкокси с 1 - 3 атомами углерода и алкил с 1 - 4 атомами углерода, смеси их изомеров или индивидуальные изомеры и их кислотно-аддитивные соли, которые обладают биологической активностью, в частности могут применяться в качестве антагониста рецептора 5-НТ1 А и 5-НТ2.The object of the invention are benzimidazolone derivatives of General formula (I)
where R 1 and R 2 are the same or different and mean a hydrogen atom, a halogen atom, trifluoromethyl, alkyl with 1-6 carbon atoms, alkoxy with 1-6 carbon atoms, alkylthio with 1-6 carbon atoms, acyl with 1-6 carbon atoms , carboxyl, alkoxycarbonyl with 1-6 carbon atoms, hydroxy, nitro group or amino group, unsubstituted or N-mono- or disubstituted with alkyl with 1-4 carbon atoms, acylamino with 1-6 carbon atoms, alkoxycarbonylamino with 1-6 carbon atoms, carbamoyl, unsubstituted or N-mono- or disubstituted by alkyl with 1-4 carbon atoms, cyano, alkyl sulphinyl with 1 to 6 carbon atoms, aminosulfonyl, unsubstituted or N-mono- or disubstituted with alkyl with 1 to 4 carbon atoms, or an aminosulfonylamino group, unsubstituted with or N-mono- or disubstituted with alkyl with 1 to 4 carbon atoms; R 3 is a hydrogen atom, alkyl with 1 to 6 carbon atoms, alkenyl with 2 to 6 carbon atoms or alkynyl with 2 to 6 carbon atoms; A - group -CO- or -CONH-, or A is absent; B - unbranched or branched, saturated or unsaturated alkyl with 2-6 carbon atoms; m and n independently of each other mean an integer of 1 - 3; R 4 is phenyl, naphthyl or benzodioxane, unsubstituted or substituted by at least one substituent from the group including halogen atom, trifluoromethyl, cyano, alkoxy with 1 to 3 carbon atoms and alkyl with 1 to 4 carbon atoms, mixtures of their isomers or individual isomers and their acid addition salts, which have biological activity, in particular, can be used as an antagonist of the 5-HT 1 A and 5-HT 2 receptor.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ITMI91A002118 | 1991-07-30 | ||
| ITM191A002118 | 1991-07-30 | ||
| ITMI912118A IT1251144B (en) | 1991-07-30 | 1991-07-30 | BENZIMIDAZOLONE DERIVATIVES |
| PCT/IT1992/000088 WO1993003016A1 (en) | 1991-07-30 | 1992-07-30 | Benzimidazolone derivatives as 5-ht1a and 5-ht2 antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU94015171A true RU94015171A (en) | 1995-09-10 |
| RU2096411C1 RU2096411C1 (en) | 1997-11-20 |
Family
ID=11360463
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU9294015171A RU2096411C1 (en) | 1991-07-30 | 1992-07-30 | Derivatives of benzimidazolone, mixture of their isomers or their acid additive salts as antagonist of receptor 5htia and 5ht2 |
Country Status (32)
| Country | Link |
|---|---|
| US (1) | US5576318A (en) |
| EP (1) | EP0526434B1 (en) |
| JP (1) | JP2989667B2 (en) |
| KR (1) | KR100263495B1 (en) |
| AT (1) | ATE191910T1 (en) |
| AU (1) | AU665366B2 (en) |
| CA (1) | CA2114542C (en) |
| CZ (1) | CZ281511B6 (en) |
| DE (1) | DE69230926T2 (en) |
| DK (1) | DK0526434T3 (en) |
| EE (1) | EE03070B1 (en) |
| ES (1) | ES2144412T3 (en) |
| FI (1) | FI111460B (en) |
| GR (1) | GR3033947T3 (en) |
| HK (1) | HK1010725A1 (en) |
| HU (2) | HUT70195A (en) |
| IE (1) | IE922464A1 (en) |
| IL (1) | IL102665A (en) |
| IT (1) | IT1251144B (en) |
| MX (1) | MX9204139A (en) |
| NO (1) | NO304070B1 (en) |
| NZ (1) | NZ243777A (en) |
| PH (1) | PH30998A (en) |
| PL (1) | PL171329B1 (en) |
| PT (1) | PT526434E (en) |
| RU (1) | RU2096411C1 (en) |
| SG (1) | SG52407A1 (en) |
| SK (1) | SK279292B6 (en) |
| TW (1) | TW209862B (en) |
| UA (1) | UA42684C2 (en) |
| WO (1) | WO1993003016A1 (en) |
| ZA (1) | ZA925682B (en) |
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| GB8607294D0 (en) * | 1985-04-17 | 1986-04-30 | Ici America Inc | Heterocyclic amide derivatives |
| NL8601494A (en) * | 1985-06-22 | 1987-01-16 | Sandoz Ag | THIAZOLS, THEIR PREPARATIONS AND PHARMACEUTICAL PREPARATIONS CONTAINING THEM. |
| GB8601160D0 (en) * | 1986-01-17 | 1986-02-19 | Fujisawa Pharmaceutical Co | Heterocyclic compounds |
| US5036088A (en) * | 1986-06-09 | 1991-07-30 | Pfizer Inc. | Antiallergy and antiinflammatory agents, compositions and use |
| JPH0784462B2 (en) * | 1986-07-25 | 1995-09-13 | 日清製粉株式会社 | Benzimidazole derivative |
| US4954503A (en) * | 1989-09-11 | 1990-09-04 | Hoechst-Roussel Pharmaceuticals, Inc. | 3-(1-substituted-4-piperazinyl)-1H-indazoles |
| IT1251144B (en) * | 1991-07-30 | 1995-05-04 | Boehringer Ingelheim Italia | BENZIMIDAZOLONE DERIVATIVES |
-
1991
- 1991-07-30 IT ITMI912118A patent/IT1251144B/en active IP Right Grant
-
1992
- 1992-07-15 MX MX9204139A patent/MX9204139A/en unknown
- 1992-07-28 IL IL10266592A patent/IL102665A/en not_active IP Right Cessation
- 1992-07-28 TW TW081105974A patent/TW209862B/zh not_active IP Right Cessation
- 1992-07-29 ZA ZA925682A patent/ZA925682B/en unknown
- 1992-07-29 PH PH44739A patent/PH30998A/en unknown
- 1992-07-29 IE IE246492A patent/IE922464A1/en not_active IP Right Cessation
- 1992-07-30 SK SK101-94A patent/SK279292B6/en unknown
- 1992-07-30 DK DK92830427T patent/DK0526434T3/en active
- 1992-07-30 ES ES92830427T patent/ES2144412T3/en not_active Expired - Lifetime
- 1992-07-30 EP EP92830427A patent/EP0526434B1/en not_active Expired - Lifetime
- 1992-07-30 AT AT92830427T patent/ATE191910T1/en active
- 1992-07-30 AU AU24275/92A patent/AU665366B2/en not_active Expired
- 1992-07-30 DE DE69230926T patent/DE69230926T2/en not_active Expired - Lifetime
- 1992-07-30 PL PL92302163A patent/PL171329B1/en unknown
- 1992-07-30 HU HU9400255A patent/HUT70195A/en unknown
- 1992-07-30 UA UA94005462A patent/UA42684C2/en unknown
- 1992-07-30 RU RU9294015171A patent/RU2096411C1/en active
- 1992-07-30 JP JP50345393A patent/JP2989667B2/en not_active Expired - Lifetime
- 1992-07-30 SG SG1996004034A patent/SG52407A1/en unknown
- 1992-07-30 KR KR1019940700293A patent/KR100263495B1/en not_active IP Right Cessation
- 1992-07-30 WO PCT/IT1992/000088 patent/WO1993003016A1/en active IP Right Grant
- 1992-07-30 PT PT92830427T patent/PT526434E/en unknown
- 1992-07-30 CZ CZ94170A patent/CZ281511B6/en not_active IP Right Cessation
- 1992-07-30 CA CA002114542A patent/CA2114542C/en not_active Expired - Lifetime
- 1992-07-30 NZ NZ243777A patent/NZ243777A/en unknown
-
1994
- 1994-01-28 FI FI940420A patent/FI111460B/en not_active IP Right Cessation
- 1994-01-28 NO NO940306A patent/NO304070B1/en not_active IP Right Cessation
- 1994-03-23 US US08/216,742 patent/US5576318A/en not_active Expired - Lifetime
- 1994-11-23 EE EE9400396A patent/EE03070B1/en unknown
-
1995
- 1995-06-20 HU HU95P/P00292P patent/HU211256A9/en unknown
-
1998
- 1998-10-21 HK HK98111444A patent/HK1010725A1/en not_active IP Right Cessation
-
2000
- 2000-07-12 GR GR20000401632T patent/GR3033947T3/en unknown
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