RU92004409A - Сахарин-производные ингибиторы протеолитических ферментов, их использование и фармацевтическая композиция - Google Patents
Сахарин-производные ингибиторы протеолитических ферментов, их использование и фармацевтическая композицияInfo
- Publication number
- RU92004409A RU92004409A RU92004409/04A RU92004409A RU92004409A RU 92004409 A RU92004409 A RU 92004409A RU 92004409/04 A RU92004409/04 A RU 92004409/04A RU 92004409 A RU92004409 A RU 92004409A RU 92004409 A RU92004409 A RU 92004409A
- Authority
- RU
- Russia
- Prior art keywords
- carbon atoms
- primary
- proteolytic enzymes
- sakharin
- pharmaceutical composition
- Prior art date
Links
- 102000035443 Peptidases Human genes 0.000 title claims 2
- 108091005771 Peptidases Proteins 0.000 title claims 2
- 229940024999 Proteolytic enzymes for treatment of wounds and ulcers Drugs 0.000 title claims 2
- 239000003112 inhibitor Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000004432 carbon atoms Chemical group C* 0.000 claims 4
- 239000002253 acid Substances 0.000 claims 3
- 150000001875 compounds Chemical class 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 2
- 239000011780 sodium chloride Substances 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000001664 diethylamino group Chemical group [H]C([H])([H])C([H])([H])N(*)C([H])([H])C([H])([H])[H] 0.000 claims 1
- 230000002255 enzymatic Effects 0.000 claims 1
- 125000000524 functional group Chemical group 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
Claims (1)
- Предложены соединения, имеющие структурную формулу
в которой L - N, O или SOn, где n - 0, 1 или 2; L - R1 - уходящая группа, H - L - R1 - ее сопряженная кислота и, когда L - N, H - L -R1 имеет величину рКк, меньшую или равную 6, когда L - O, H - L - R1 имеет величину рКк, меньшую или равную 8, и когда L - SOn, H - L - R1 имеет величину рКк, меньшую или равную 5; R2 - первичный или вторичный алкил из 2-4 атомов углерода, первичный алкиламино из 1-3 атомов углерода, первичный алкилметиламино из 2-4 атомов углерода, диэтиламино или первичный алкокси из 1-3 атомов углерода; R3 - 1-3 заместителя на любом или всех из 5-, 6- и 7-положений; или их фармацевтически приемлемая соль кислотного присоединения, если соединение имеет основную функциональную группу, или их фармацевтически приемлемая соль основного присоединения, если соединение имеет кислотную функцииональную группу, которые тормозят ферментную активность протеолитических ферментов.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US79303591A | 1991-11-15 | 1991-11-15 | |
| US793035 | 1991-11-15 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU92004409A true RU92004409A (ru) | 1995-05-20 |
| RU2114835C1 RU2114835C1 (ru) | 1998-07-10 |
Family
ID=25158888
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU92004409A RU2114835C1 (ru) | 1991-11-15 | 1992-11-13 | Производные сахарина или их фармацевтически приемлемая аддитивная соль кислоты или основания, фармацевтическая композиция, проявляющая активность ингибитора эластазы |
Country Status (15)
| Country | Link |
|---|---|
| EP (1) | EP0542371A1 (ru) |
| JP (1) | JPH06122675A (ru) |
| KR (1) | KR930010016A (ru) |
| AU (1) | AU656027B2 (ru) |
| CA (1) | CA2082774A1 (ru) |
| CZ (1) | CZ338892A3 (ru) |
| FI (1) | FI925166A (ru) |
| HU (2) | HUT65694A (ru) |
| IL (1) | IL103747A (ru) |
| MX (1) | MX9206568A (ru) |
| NO (1) | NO302887B1 (ru) |
| NZ (1) | NZ245126A (ru) |
| RU (1) | RU2114835C1 (ru) |
| SG (1) | SG52778A1 (ru) |
| TW (1) | TW282463B (ru) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5294757A (en) * | 1990-07-18 | 1994-03-15 | Otis Elevator Company | Active vibration control system for an elevator, which reduces horizontal and rotational forces acting on the car |
| US5321217A (en) * | 1990-07-18 | 1994-06-14 | Otis Elevator Company | Apparatus and method for controlling an elevator horizontal suspension |
| US5308938A (en) * | 1990-07-18 | 1994-05-03 | Otis Elevator Company | Elevator active suspension system |
| US5322144A (en) * | 1990-07-18 | 1994-06-21 | Otis Elevator Company | Active control of elevator platform |
| US5306818A (en) * | 1990-11-01 | 1994-04-26 | Sterling Winthrop Inc. | Tetrahydro 2-saccharinylmerthyl aryl carboxylates |
| US5378720A (en) * | 1991-12-19 | 1995-01-03 | Sterling Winthrop Inc. | Saccharin derivative proteolytic enzyme inhibitors |
| AU668694B2 (en) * | 1991-12-19 | 1996-05-16 | Sanofi-Synthelabo | Saccharin derivative proteolytic enzyme inhibitors |
| TW226016B (ru) * | 1991-12-30 | 1994-07-01 | Sterling Winthrop Inc | |
| DE19533643A1 (de) * | 1995-09-12 | 1997-03-13 | Nycomed Arzneimittel Gmbh | Neue cyclische Derivate von Benzolsulfonamiden |
| JP2003508480A (ja) * | 1999-09-10 | 2003-03-04 | ザ、プロクター、エンド、ギャンブル、カンパニー | 酵素インヒビター |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5236917A (en) * | 1989-05-04 | 1993-08-17 | Sterling Winthrop Inc. | Saccharin derivatives useful as proteolytic enzyme inhibitors and compositions and method of use thereof |
| WO1990013549A1 (en) * | 1989-05-04 | 1990-11-15 | Sterling Winthrop Inc. | Saccharin derivatives useful as proteolytic enzyme inhibitors and preparation thereof |
| DE3917597A1 (de) * | 1989-05-26 | 1990-11-29 | Schering Ag | Neue leukotrien-b(pfeil abwaerts)4(pfeil abwaerts)-derivate, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel |
| AU642537B2 (en) * | 1990-11-01 | 1993-10-21 | Sanofi | 2-saccharinylmethyl aryl carboxylates useful as proteolytic enzyme inhibitors and compositions and method of use thereof |
-
1992
- 1992-09-30 AU AU26057/92A patent/AU656027B2/en not_active Ceased
- 1992-09-30 TW TW081107772A patent/TW282463B/zh active
- 1992-11-12 EP EP92203468A patent/EP0542371A1/en not_active Withdrawn
- 1992-11-12 SG SG1996009394A patent/SG52778A1/en unknown
- 1992-11-12 CA CA002082774A patent/CA2082774A1/en not_active Abandoned
- 1992-11-13 CZ CS923388A patent/CZ338892A3/cs unknown
- 1992-11-13 RU RU92004409A patent/RU2114835C1/ru active
- 1992-11-13 IL IL103747A patent/IL103747A/en not_active IP Right Cessation
- 1992-11-13 HU HU9203561A patent/HUT65694A/hu unknown
- 1992-11-13 NZ NZ245126A patent/NZ245126A/en unknown
- 1992-11-13 MX MX9206568A patent/MX9206568A/es unknown
- 1992-11-13 NO NO924402A patent/NO302887B1/no unknown
- 1992-11-13 FI FI925166A patent/FI925166A/fi not_active Application Discontinuation
- 1992-11-14 KR KR1019920021438A patent/KR930010016A/ko not_active Application Discontinuation
- 1992-11-16 JP JP4305222A patent/JPH06122675A/ja not_active Withdrawn
-
1995
- 1995-06-30 HU HU95P/P00612P patent/HU211664A9/hu unknown
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