RU94015842A - Пептидные кетоны, фармацевтическая композиция и способ ингибирования интерлейкин-1 протеазы - Google Patents
Пептидные кетоны, фармацевтическая композиция и способ ингибирования интерлейкин-1 протеазыInfo
- Publication number
- RU94015842A RU94015842A RU94015842/04A RU94015842A RU94015842A RU 94015842 A RU94015842 A RU 94015842A RU 94015842/04 A RU94015842/04 A RU 94015842/04A RU 94015842 A RU94015842 A RU 94015842A RU 94015842 A RU94015842 A RU 94015842A
- Authority
- RU
- Russia
- Prior art keywords
- protease
- aryl
- pharmaceutical composition
- heteroaryl
- compounds
- Prior art date
Links
Claims (1)
- Раскрываются соединения формулы I и их фармацевтически приемлемые соли
в которой R1 - (CR5R6)n, (CR6R6)n-арил, (CR5R6)n-гетероарил, X-(CR5R6)n, X-(CR5R6)n-арил или X-(CR5R6)n-гетероарил, при этом арил и гетероарил необязательно могут быть замещены; X - О или NR5; R5 и R6 независимо - Н или низший алкил; R2 - Н, галоген, низший алкил или (CR5R6)n-арил; R3 и R4 независимо - Н или алкил; А - D-или α -изомер аминокислоты, выбираемой из группы, состоящей из аланина, валина, лейцина, изолейцина, пролина, фенилаланина, глицина, тирозина, метионина, аспарагина, глутамина, аспарагиновой кислоты, глутаминовой кислоты, лизина, аргинина, гистидина и b -тиенилаланина; Z - CH2 или О; n = 0 - 4; фармацевтические композиции, содержащие такие соединения, и способ ингибирования активности интерлейкин-1β-протеазы у млекопитающих с использованием упомянутых соединений и композиций.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US08/060,197 US5462939A (en) | 1993-05-07 | 1993-05-07 | Peptidic ketones as interleukin-1β-converting enzyme inhibitors |
US060197 | 1993-05-07 |
Publications (2)
Publication Number | Publication Date |
---|---|
RU94015842A true RU94015842A (ru) | 1996-01-10 |
RU2133251C1 RU2133251C1 (ru) | 1999-07-20 |
Family
ID=22027975
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU94015842A RU2133251C1 (ru) | 1993-05-07 | 1994-05-06 | ПЕПТИДНЫЕ КЕТОНЫ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И СПОСОБ ИНГИБИРОВАНИЯ ИНТЕРЛЕЙКИН-1βПРОТЕАЗЫ |
Country Status (21)
Country | Link |
---|---|
US (2) | US5462939A (ru) |
EP (1) | EP0623606B1 (ru) |
JP (1) | JPH0725839A (ru) |
AT (1) | ATE161849T1 (ru) |
AU (1) | AU668465B2 (ru) |
CA (1) | CA2123055A1 (ru) |
CZ (1) | CZ108394A3 (ru) |
DE (1) | DE69407654T2 (ru) |
DK (1) | DK0623606T3 (ru) |
ES (1) | ES2113606T3 (ru) |
FI (1) | FI942107A7 (ru) |
GR (1) | GR3026556T3 (ru) |
HK (1) | HK1008146A1 (ru) |
HU (1) | HU217070B (ru) |
IL (1) | IL109585A0 (ru) |
NO (1) | NO941675L (ru) |
NZ (1) | NZ260477A (ru) |
PH (1) | PH30362A (ru) |
RU (1) | RU2133251C1 (ru) |
SK (1) | SK282270B6 (ru) |
TW (1) | TW377350B (ru) |
Families Citing this family (43)
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US6008217A (en) * | 1995-12-20 | 1999-12-28 | Vertex Pharmaceuticals Incorporated | Inhibitors of interleukin-1β converting enzyme |
US5874424A (en) * | 1995-12-20 | 1999-02-23 | Vertex Pharmaceuticals Incorporated | Inhibitors of interleukin-1β converting enzyme |
US6204261B1 (en) | 1995-12-20 | 2001-03-20 | Vertex Pharmaceuticals Incorporated | Inhibitors of interleukin-1β Converting enzyme inhibitors |
US5462939A (en) * | 1993-05-07 | 1995-10-31 | Sterling Winthrop Inc. | Peptidic ketones as interleukin-1β-converting enzyme inhibitors |
JPH0789951A (ja) * | 1993-06-03 | 1995-04-04 | Sterling Winthrop Inc | インターロイキン−1β転換酵素阻害剤 |
US5843905A (en) * | 1993-06-04 | 1998-12-01 | Vertex Pharmaceuticals, Incorporated | Peptidic phosphinyloxymethyl ketones as interleukin-1β-converting enzyme inhibitors |
US5714484A (en) * | 1993-12-08 | 1998-02-03 | Prototek, Inc. | α-(1,3-dicarbonylenol ether) methyl ketones as cysteine protease inhibitors |
US5486623A (en) | 1993-12-08 | 1996-01-23 | Prototek, Inc. | Cysteine protease inhibitors containing heterocyclic leaving groups |
US5798247A (en) * | 1994-05-06 | 1998-08-25 | Basf Aktiengesellschaft | Organic-chemical compound with ice-inhibitory action |
US6420522B1 (en) | 1995-06-05 | 2002-07-16 | Vertex Pharmaceuticals Incorporated | Inhibitors of interleukin-1β converting enzyme |
US5716929A (en) * | 1994-06-17 | 1998-02-10 | Vertex Pharmaceuticals, Inc. | Inhibitors of interleukin-1β converting enzyme |
US5756466A (en) * | 1994-06-17 | 1998-05-26 | Vertex Pharmaceuticals, Inc. | Inhibitors of interleukin-1β converting enzyme |
US5847135A (en) * | 1994-06-17 | 1998-12-08 | Vertex Pharmaceuticals, Incorporated | Inhibitors of interleukin-1β converting enzyme |
US5585504A (en) * | 1994-09-16 | 1996-12-17 | Merck & Co., Inc. | Process of making cox-2 inhibitors having a lactone bridge |
WO1996029088A1 (en) * | 1995-03-23 | 1996-09-26 | Affymax Technologies N.V. | Novel piperazine derivatives as type il-1 receptor antagonists |
US6162828A (en) * | 1995-03-31 | 2000-12-19 | Takeda Chemical Industries, Ltd. | Cysteine protease inhibitor |
CN1221514C (zh) * | 1995-05-09 | 2005-10-05 | 拜尔公司 | 制备烷基-二卤代苯基取代的酮烯醇的中间体 |
US5843904A (en) * | 1995-12-20 | 1998-12-01 | Vertex Pharmaceuticals, Inc. | Inhibitors of interleukin-1βconverting enzyme |
US5869519A (en) * | 1996-12-16 | 1999-02-09 | Idun Pharmaceuticals, Inc. | C-terminal modified (n-substituted)-2-indolyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases |
US5968927A (en) * | 1996-09-20 | 1999-10-19 | Idun Pharmaceuticals, Inc. | Tricyclic compounds for the inhibition of the ICE/ced-3 protease family of enzymes |
US5877197A (en) * | 1996-12-16 | 1999-03-02 | Karanewsky; Donald S. | C-terminal modified (N-substituted)-2-indolyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases |
US6184244B1 (en) | 1996-12-16 | 2001-02-06 | Idun Pharmaceuticals, Inc. | C-terminal modified (N-substituted)-2-indolyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases |
US6184210B1 (en) | 1997-10-10 | 2001-02-06 | Cytovia, Inc. | Dipeptide apoptosis inhibitors and the use thereof |
BR9814817A (pt) * | 1997-10-10 | 2002-01-08 | Cytovia Inc | Inibidores de apoptose de dipeptìdio e o uso dos mesmos |
CN1278243A (zh) * | 1997-11-06 | 2000-12-27 | 西巴特殊化学品控股有限公司 | 二酯胺加合物 |
ATE296812T1 (de) | 1998-03-09 | 2005-06-15 | Vertex Pharma | 1,2-diazepanderivate als inhibitoren des interleukin-1beta umwandelnden enzyms |
KR20010041905A (ko) * | 1998-03-16 | 2001-05-25 | 시토비아 인크. | 디펩티드 카스파제 억제제 및 이의 용도 |
HU227920B1 (en) * | 1998-03-19 | 2012-06-28 | Vertex Pharma | Inhibitors of caspases, pharmaceutical compositions comprising thereof and their use |
US6242422B1 (en) | 1998-10-22 | 2001-06-05 | Idun Pharmacueticals, Inc. | (Substituted)Acyl dipeptidyl inhibitors of the ice/ced-3 family of cysteine proteases |
US7157430B2 (en) | 1998-10-22 | 2007-01-02 | Idun Pharmaceuticals, Inc. | (Substituted)acyl dipeptidyl inhibitors of the ICE/CED-3 family of cysteine proteases |
WO2000055114A1 (en) * | 1999-03-16 | 2000-09-21 | Cytovia, Inc. | Substituted 2-aminobenzamide caspase inhibitors and the use thereof |
ATE363465T1 (de) * | 1999-04-09 | 2007-06-15 | Cytovia Inc | Caspase inhibitoren und ihre verwendung |
JP2003508379A (ja) | 1999-08-27 | 2003-03-04 | サイトビア インコーポレイテッド | 置換α−ヒドロキシ酸カスパーゼインヒビターおよびその使用 |
US6566338B1 (en) | 1999-10-12 | 2003-05-20 | Cytovia, Inc. | Caspase inhibitors for the treatment and prevention of chemotherapy and radiation therapy induced cell death |
US6525024B1 (en) | 2000-04-17 | 2003-02-25 | Idun Pharmaceuticals, Inc. | Inhibitors of the ICE/ced-3 family of cysteine proteases |
PE20011350A1 (es) * | 2000-05-19 | 2002-01-15 | Vertex Pharma | PROFARMACO DE UN INHIBIDOR DE ENZIMA CONVERTIDORA DE INTERLEUCINA-1ß (ICE) |
CA2421172A1 (en) | 2000-09-08 | 2002-03-14 | Merck Frosst Canada & Co. | Gamma-ketoacid dipeptides as inhibitors of caspase-3 |
US6699866B2 (en) * | 2001-04-17 | 2004-03-02 | Sepracor Inc. | Thiazole and other heterocyclic ligands for mammalian dopamine, muscarinic and serotonin receptors and transporters, and methods of use thereof |
DE10150203A1 (de) * | 2001-10-12 | 2003-04-17 | Probiodrug Ag | Peptidylketone als Inhibitoren der DPIV |
WO2003068242A1 (en) * | 2002-02-11 | 2003-08-21 | Vertex Pharmaceuticals Incorporated | Phospholipids as caspase inhibitor prodrugs |
US20060128696A1 (en) * | 2004-05-15 | 2006-06-15 | Annamaria Vezzani | Treating seizures using ice inhibitors |
CN1980658A (zh) * | 2004-05-27 | 2007-06-13 | 沃泰克斯药物股份有限公司 | 治疗自身炎性疾病的ice抑制剂 |
US9956260B1 (en) | 2011-07-22 | 2018-05-01 | The J. David Gladstone Institutes | Treatment of HIV-1 infection and AIDS |
Family Cites Families (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4582821A (en) * | 1983-11-16 | 1986-04-15 | E. I. Du Pont De Nemours And Company | Inhibition of cyclic nucleotide independent protein kinases |
US5055451A (en) * | 1986-12-22 | 1991-10-08 | Syntex Inc. | Aryloxy and arylacyloxy methyl ketones as thiol protease inhibitors |
DE3737399A1 (de) * | 1987-11-04 | 1989-05-18 | Schwabe Willmar Gmbh & Co | Aminosaeureester, verfahren zu ihrer herstellung und ihre verwendung |
AU7775991A (en) * | 1990-04-04 | 1991-10-30 | Immunex Corporation | Interleukin 1beta protease |
EP0519748B1 (en) * | 1991-06-21 | 1998-09-02 | Merck & Co. Inc. | Peptidyl derivatives as inhibitors of interleukin-1B converting enzyme |
DK0600880T3 (da) * | 1991-08-30 | 2004-04-13 | Vertex Pharma | Interleukin 1-beta-protease og interleukin 1-beta-proteasehæmmere |
GB9123326D0 (en) * | 1991-11-04 | 1991-12-18 | Sandoz Ltd | Improvements in or relating to organic compounds |
JP3386125B2 (ja) * | 1992-02-21 | 2003-03-17 | メルク エンド カンパニー インコーポレーテッド | インターロイキン−1β変換酵素阻害剤としてのペプチジル誘導体 |
US5462939A (en) * | 1993-05-07 | 1995-10-31 | Sterling Winthrop Inc. | Peptidic ketones as interleukin-1β-converting enzyme inhibitors |
-
1993
- 1993-05-07 US US08/060,197 patent/US5462939A/en not_active Expired - Lifetime
-
1994
- 1994-04-12 TW TW083103254A patent/TW377350B/zh active
- 1994-04-28 JP JP6091021A patent/JPH0725839A/ja active Pending
- 1994-04-29 DK DK94201192T patent/DK0623606T3/da active
- 1994-04-29 AT AT94201192T patent/ATE161849T1/de not_active IP Right Cessation
- 1994-04-29 EP EP94201192A patent/EP0623606B1/en not_active Expired - Lifetime
- 1994-04-29 ES ES94201192T patent/ES2113606T3/es not_active Expired - Lifetime
- 1994-04-29 DE DE69407654T patent/DE69407654T2/de not_active Expired - Lifetime
- 1994-05-02 SK SK509-94A patent/SK282270B6/sk unknown
- 1994-05-03 CZ CZ941083A patent/CZ108394A3/cs unknown
- 1994-05-06 RU RU94015842A patent/RU2133251C1/ru not_active IP Right Cessation
- 1994-05-06 HU HU9401423A patent/HU217070B/hu not_active IP Right Cessation
- 1994-05-06 FI FI942107A patent/FI942107A7/fi unknown
- 1994-05-06 IL IL10958594A patent/IL109585A0/xx unknown
- 1994-05-06 AU AU61906/94A patent/AU668465B2/en not_active Ceased
- 1994-05-06 NZ NZ260477A patent/NZ260477A/en not_active IP Right Cessation
- 1994-05-06 CA CA002123055A patent/CA2123055A1/en not_active Abandoned
- 1994-05-06 NO NO941675A patent/NO941675L/no unknown
- 1994-05-06 PH PH48226A patent/PH30362A/en unknown
-
1995
- 1995-05-12 US US08/440,166 patent/US5585486A/en not_active Expired - Lifetime
-
1998
- 1998-04-06 GR GR980400743T patent/GR3026556T3/el unknown
- 1998-07-07 HK HK98109010A patent/HK1008146A1/en not_active IP Right Cessation
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