[go: up one dir, main page]

RU94015842A - Пептидные кетоны, фармацевтическая композиция и способ ингибирования интерлейкин-1 протеазы - Google Patents

Пептидные кетоны, фармацевтическая композиция и способ ингибирования интерлейкин-1 протеазы

Info

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
Application number
RU94015842/04A
Other languages
English (en)
Other versions
RU2133251C1 (ru
Inventor
И.Долли Роланд
Л.Грейбилл Тодд
Дж.Спейр Гэри
П.Проути Кэтерин
Дж.Шмидт Стейнли
Original Assignee
Стерлинг Уинтроп Инк.
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Priority claimed from US08/060,197 external-priority patent/US5462939A/en
Application filed by Стерлинг Уинтроп Инк. filed Critical Стерлинг Уинтроп Инк.
Publication of RU94015842A publication Critical patent/RU94015842A/ru
Application granted granted Critical
Publication of RU2133251C1 publication Critical patent/RU2133251C1/ru

Links

Claims (1)

  1. Раскрываются соединения формулы I и их фармацевтически приемлемые соли
    Figure 00000001

    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.
RU94015842A 1993-05-07 1994-05-06 ПЕПТИДНЫЕ КЕТОНЫ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И СПОСОБ ИНГИБИРОВАНИЯ ИНТЕРЛЕЙКИН-1βПРОТЕАЗЫ RU2133251C1 (ru)

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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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)

* Cited by examiner, † Cited by third party
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

Similar Documents

Publication Publication Date Title
RU94015842A (ru) Пептидные кетоны, фармацевтическая композиция и способ ингибирования интерлейкин-1 протеазы
DK0623606T3 (da) Peptidketoner som interleukin-1beta-omdannende enzyminhibitorer
NZ296479A (en) Amino acid or peptide derivatives which are inhibitors of multicatalytic protease (mcp)
RU95112539A (ru) Новый полипептид и фармацевтическая композиция против вич-инфекции
CA2167087A1 (en) Peptides for neutralizing the toxicity of lipid a
EP0873754A4 (en) AMINO ACID COMPOSITIONS
RU96104348A (ru) Профилактика спида
GR3021570T3 (en) Cyclopeptides and their use as resorption enhancers in mucous use
RU92016593A (ru) Новый полипептид со сродством с липополисахаридами и фармацевтическая композиция для ингибирования вич на его основе
KR970005043B1 (en) Tumor necrosis factor alpha muteins
EP0506628A3 (en) Aminoacyl and oligopeptidyl derivatives of allopurinol exhibiting immunostimulatory activity, and pharmaceutical formulations containing these substances
JPS6136297A (ja) カルボキシアルキルジペプチドを製造する方法
WO2001027136A3 (fr) Peptides ayant une activite de stimulation de la reponse immunitaire et de regeneration tissulaire
DE69327310D1 (de) Amadori-reaktion-verbindungen, und -produkte, verfahren zu deren herstellung und deren verwendung
KR890013061A (ko) 폴리펩티드 유도체
ATE42308T1 (de) Pharmakologisch aktive peptide.
ATE30919T1 (de) Magensekretion hemmende peptidderivate, verfahren zu ihrer herstellung und sie enthaltende arzneimittel.
KR920701180A (ko) 4h-3,1-벤즈옥사진-4-온 화합물 및 그의 엘라스타아제 저해용 약학조성물
Tobe et al. Synthesis and structure-activity relationships of amastatin analogues, inhibitors of aminopeptidase A
CA2549890A1 (en) Mri contrast medium composition for oral administration
EP0934952A3 (en) Peptides containing an N-substituted glycine residue
Ravichandran et al. Occurrence of asparagine in “disallowed” conformations in proteins
EA199900551A1 (ru) Фармацевтическая композиция, содержащая ингибитор иммуноглобулин-рецепторного взаимодействия
KR970701732A (ko) 펩신 방출을 억제하기 위한 펩티드(Peptides Inhibiting the Release of Pepsin)
RU96118282A (ru) Пептиды для ингибирования высвобождения пепсина