BR0009610A - Inibidores de caspase e uso dos mesmos - Google Patents

Inibidores de caspase e uso dos mesmos

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Publication number
BR0009610A
BR0009610A BR0009610-5A BR0009610A BR0009610A BR 0009610 A BR0009610 A BR 0009610A BR 0009610 A BR0009610 A BR 0009610A BR 0009610 A BR0009610 A BR 0009610A
Authority
BR
Brazil
Prior art keywords
cell death
present
inhibitors
caspase inhibitors
formula
Prior art date
Application number
BR0009610-5A
Other languages
English (en)
Inventor
Sui Xiong Cai
Eckard Weber
Yan Wang
Gordon B Mills
Douglas R Green
Original Assignee
Cytovia Inc
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
Application filed by Cytovia Inc filed Critical Cytovia Inc
Publication of BR0009610A publication Critical patent/BR0009610A/pt

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    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/20—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
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Abstract

"INIBIDORES DE CASPASE E USO DOS MESMOS". A presente invenção é dirigida a novo dipeptídeo dos mesmos, representado por fórmula geral: (I) onde R1-R3, X e Y são definidos aqui. A presente invenção também se refere à descoberta que compostos tendo fórmula (I) são inibidores potentes de caspases e morte de células apoptóticas. Assim, os inibidores desta invenção podem retardar ou bloquear a morte de células em várias condições clinicas em que a perda de células, tecidos ou órgãos completos ocorre.
BR0009610-5A 1999-04-09 2000-04-07 Inibidores de caspase e uso dos mesmos BR0009610A (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US12854599P 1999-04-09 1999-04-09
US15837099P 1999-10-12 1999-10-12
PCT/US2000/009319 WO2000061542A1 (en) 1999-04-09 2000-04-07 Caspase inhibitors and the use thereof

Publications (1)

Publication Number Publication Date
BR0009610A true BR0009610A (pt) 2002-02-13

Family

ID=26826691

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0009610-5A BR0009610A (pt) 1999-04-09 2000-04-07 Inibidores de caspase e uso dos mesmos

Country Status (12)

Country Link
US (3) US6355618B1 (pt)
EP (1) EP1177168B1 (pt)
JP (1) JP2002541237A (pt)
KR (1) KR20020005665A (pt)
CN (1) CN1176941C (pt)
AT (1) ATE363465T1 (pt)
AU (1) AU4213500A (pt)
BR (1) BR0009610A (pt)
CA (1) CA2369619A1 (pt)
DE (1) DE60035037T2 (pt)
MX (1) MXPA01010127A (pt)
WO (1) WO2000061542A1 (pt)

Families Citing this family (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0476916A1 (en) * 1990-09-13 1992-03-25 Westinghouse Electric Corporation Aluminum-silver oxide battery system
US6184210B1 (en) * 1997-10-10 2001-02-06 Cytovia, Inc. Dipeptide apoptosis inhibitors and the use thereof
EP1100520B1 (en) * 1998-07-21 2004-09-22 Cytovia, Inc. Novel fluorescence dyes and their applications for whole cell fluorescence screening assays for caspases, peptidases, proteases and other enzymes and the use thereof
DE60030097T2 (de) * 1999-03-16 2007-03-08 Cytovia, Inc., San Diego Substituierte 2-aminobenzamin caspase inhibitoren und ihre verwendung
BR0009610A (pt) 1999-04-09 2002-02-13 Cytovia Inc Inibidores de caspase e uso dos mesmos
EP1212295B1 (en) 1999-08-27 2008-10-01 Cytovia, Inc. Substituted alpha-hydroxy acid caspase inhibitors and the use thereof
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
AR027993A1 (es) 2000-03-29 2003-04-23 Vertex Pharma Inhibidores de carbonato de caspasa y usos del mismo
PE20011350A1 (es) 2000-05-19 2002-01-15 Vertex Pharma PROFARMACO DE UN INHIBIDOR DE ENZIMA CONVERTIDORA DE INTERLEUCINA-1ß (ICE)
CA2418720A1 (en) * 2000-09-13 2002-03-21 Vertex Pharmaceuticals Incorporated Caspase inhibitors and uses thereof
FR2815541B1 (fr) * 2000-10-24 2008-02-29 Lipha Utilisation d'inhibiteurs de l'apoptose des pericytes pour le traitement et/ou la prevention de la retinopathie diabetique
UA80676C2 (en) * 2001-01-29 2007-10-25 Applied Research Systems Use of il-18 inhibitors for the treatment and/or prevention of cardiomyopathy
ATE409482T1 (de) * 2001-03-02 2008-10-15 Merck Frosst Canada Ltd Cathepsincystein-proteasehemmer
EP1381602A1 (en) 2001-04-19 2004-01-21 Vertex Pharmaceuticals Incorporated Heterocyclyldicarbamides as caspase inhibitors
KR100446961B1 (ko) * 2001-10-09 2004-09-01 주식회사 엘지생명과학 캐스파제 저해제를 이용하여 조혈모세포를 체외에서다량으로 증식시키는 세포배양 방법 및 배지 조성물
AU2003248360A1 (en) * 2002-02-08 2003-09-09 Idun Pharmaceuticals, Inc. (substituted)acyl dipeptidyl inhibitors of the ice/ced-3 family of cysteine proteases
US7410956B2 (en) 2002-02-11 2008-08-12 Vertex Pharmaceuticals Incorporated Caspase inhibitor prodrugs
EP1494700A2 (en) * 2002-04-05 2005-01-12 Cytovia, Inc. Caspase inhibitors for the treatment of diseases and conditions caused by exposure to radionuclides, biological agents, or chemical agents
GB0208579D0 (en) * 2002-04-13 2002-05-22 British Biotech Pharm Antibacterial agents
WO2003088917A2 (en) * 2002-04-19 2003-10-30 Vertex Pharmaceuticals Incorporated Regulation of tnf-alpha
JP2005536462A (ja) * 2002-04-30 2005-12-02 ユン ジン ファーマスーチカル インダストリーズ カンパニー リミテッド カスパーゼ−３阻害剤としてのキノリン誘導体、この製造方法及びこれを含む薬剤学的組成物
US7195884B2 (en) * 2002-07-19 2007-03-27 Promega Corp. Methods and kits for transferases
JP2006502415A (ja) * 2002-10-10 2006-01-19 ベクトン・ディキンソン・アンド・カンパニー カスパーゼ阻害剤を有するサンプル収集システム
EP1628674A2 (en) * 2003-05-06 2006-03-01 Cytovia, Inc. Protease inhibitors for coronaviruses and sars-cov and the use thereof
PE20050159A1 (es) * 2003-05-27 2005-04-19 Vertex Pharma Derivados de acido 3-[2-(3-amino-2-oxo-2h-piridin-1-il)-acetilamino]-4-oxo-pentanoico como inhibidores de caspasa
US20090232866A1 (en) * 2003-10-07 2009-09-17 Mariann Pavone-Gyongyosi Oligopeptides as coating material for medical products
US7297714B2 (en) 2003-10-21 2007-11-20 Irm Llc Inhibitors of cathepsin S
EP1715866A2 (en) * 2004-02-05 2006-11-02 The General Hospital Corporation Protease inhibitors for treatment of wrinkles
EP2399916B1 (en) * 2004-03-12 2014-12-10 Vertex Pharmaceuticals Incorporated Process and intermediates for the preparation of aspartic acetal caspase ihnhibitors
AU2005247409B2 (en) 2004-05-15 2011-11-10 Vertex Pharmaceuticals Incorporated Treating seizures using ICE inhibitors
EP1778221A2 (en) 2004-05-27 2007-05-02 Vertex Pharmaceuticals Incorporated Ice inhibitors for the treatment of autoinflammatory diseases
WO2006030439A2 (en) * 2004-09-17 2006-03-23 Biomas Ltd. Compositions and methods for inducing hair growth
EP1833794B1 (en) 2004-11-24 2012-02-01 Vertex Pharmceuticals Incorporated 3-[2-(3-acylamino-2-oxo-2h-pyridin-1-yl)-acetylamino]-4-oxo-pentanoic acid derivatives and their use as caspase inhibitors
US20090018094A1 (en) * 2006-12-01 2009-01-15 Loma Linda University Medical Center Inhibition of brain enzymes involved in cerebral amyloid angiopathy and macular degeneration
CN101544688B (zh) * 2009-05-06 2012-09-19 河北科技大学 环五肽细胞凋亡酶抑制剂及其制备方法
US20110165143A1 (en) * 2010-01-06 2011-07-07 The Regents Of The University Of Colorado, A Body Corporate Modulation of caspases and therapeutical applications
EP2635906A4 (en) 2010-11-05 2014-04-02 Univ Brandeis ICE INHIBITING COMPOUNDS AND USES THEREOF
US9956260B1 (en) 2011-07-22 2018-05-01 The J. David Gladstone Institutes Treatment of HIV-1 infection and AIDS
US10981961B2 (en) * 2013-03-11 2021-04-20 University Of Florida Research Foundation, Incorporated Delivery of card protein as therapy for occular inflammation
US11053291B2 (en) 2014-02-19 2021-07-06 University Of Florida Research Foundation, Incorporated Delivery of Nrf2 as therapy for protection against reactive oxygen species
EP3116898B1 (en) 2014-03-11 2022-01-26 University of Florida Research Foundation, Inc. Aav-expressed m013 protein as an anti-inflammatroy therapeutic for use in a method of treating inflammatory ocular disease
JP6836996B2 (ja) * 2015-02-25 2021-03-03 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 新しいトリフルオロメチルプロパンアミド誘導体
CN106317161B (zh) * 2015-06-29 2020-05-15 深圳翰宇药业股份有限公司 一种氟甲基酮肽系列化合物的制备方法
CN108699105A (zh) 2016-03-04 2018-10-23 豪夫迈·罗氏有限公司 作为htra1抑制剂的新型二氟酮酰胺衍生物
EP3423469A1 (en) * 2016-03-04 2019-01-09 H. Hoffnabb-La Roche Ag New trifluoromethylpropanamide derivatives as htra1 inhibitors
WO2017172476A1 (en) * 2016-03-28 2017-10-05 The University Of Toledo Potent inhibitors of aspartate n-acetyl-transferase for the treatment of canavan disease
CN109415330A (zh) * 2016-07-18 2019-03-01 豪夫迈·罗氏有限公司 作为htra1抑制剂的新型二氟酮酰胺衍生物
JP2019526563A (ja) 2016-08-23 2019-09-19 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｈｔｒａ１阻害剤としての新規ジフルオロケタミド誘導体
JP2019526564A (ja) 2016-08-23 2019-09-19 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｈｔｒａ１阻害剤としての新規なトリフルオロメチルプロパンアミド誘導体
CN114569702B (zh) * 2022-03-07 2022-10-18 上海揽微赛尔生物科技有限公司 含有抗衰老活性肽与干细胞的药物组合物

Family Cites Families (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2381023A1 (fr) 1977-02-18 1978-09-15 Delalande Sa Nouveaux oligopeptides trifluoromethyles derives de la l-alanine, leur procede de preparation et leur application en therapeutique
US4518528A (en) 1983-05-19 1985-05-21 Rasnick David W α Amino fluoro ketones
US5416013A (en) 1990-04-04 1995-05-16 Sterling Winthrop Inc. Interleukin 1β protease and interleukin 1β protease inhibitors
US5252463A (en) 1990-06-22 1993-10-12 The Du Pont Merck Pharmaceutical Company Clipsin, a chymotrypsin-like protease and method of using same
US5824297A (en) 1990-06-25 1998-10-20 Oncogene Science, Inc. Tissue-derived tumor growth inhibitors, methods of preparation and uses thereof
DE69226820T2 (de) 1991-06-21 1999-05-12 Merck & Co., Inc., Rahway, N.J. Peptidylderivate als Inhibitoren von Interleukin-1B-konvertierenden Enzymen
CA2111100C (en) 1991-08-30 2004-11-02 Roy A. Black Interleukin-1 beta protease and interleukin-1 beta protease inhibitors
GB9123326D0 (en) * 1991-11-04 1991-12-18 Sandoz Ltd Improvements in or relating to organic compounds
AU3666893A (en) 1992-02-21 1993-09-13 Merck & Co., Inc. Peptidyl derivatives as inhibitors of interleukin-1beta converting enzyme
EP0618223A3 (en) 1993-03-08 1996-06-12 Sandoz Ltd Peptides, the release of Interleukin 1-Bêta, useful as anti-inflammatory agents.
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
US6087160A (en) 1993-06-24 2000-07-11 The General Hospital Corporation Programmed cell death genes and proteins
WO1995005192A1 (en) 1993-08-13 1995-02-23 Merck & Co., Inc. SUBSTITUTED KETONE DERIVATIVES AS INHIBITORS OF INTERLEUKIN-1β CONVERTING ENZYME
US5759548A (en) 1993-11-30 1998-06-02 Lxr Biotechnology Inc. Compositions which inhibit apoptosis, methods of purifying the compositions and uses thereof
US5565430A (en) 1994-08-02 1996-10-15 Sterling Winthrop Inc. Azaaspartic acid analogs as interleukin-1β converting enzyme inhibitors
US5798442A (en) 1995-04-21 1998-08-25 Merck Frosst Canada, Inc. Peptidyl derivatives as inhibitors of pro-apoptotic cysteine proteinases
US5744451A (en) 1995-09-12 1998-04-28 Warner-Lambert Company N-substituted glutamic acid derivatives with interleukin-1 β converting enzyme inhibitory activity
US5843904A (en) 1995-12-20 1998-12-01 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1βconverting enzyme
JP3830976B2 (ja) 1996-09-12 2006-10-11 アイドゥン ファーマシューティカルズ，インコーポレイテッド インターロイキン―１β―転換酵素（ＩＣＥ）／ＣＥＤ―３ファミリーインヒビターを用いたアポトーシスの阻害
ATE215953T1 (de) 1996-09-12 2002-04-15 Idun Pharmaceuticals Inc Neue tricyclische verbindungen mit ice/ced-3 protease familie-hemmenden eigenschaften
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
US6200969B1 (en) 1996-09-12 2001-03-13 Idun Pharmaceuticals, Inc. Inhibition of apoptosis using interleukin-1β-converting enzyme (ICE)/CED-3 family inhibitors
AU738341B2 (en) * 1996-10-11 2001-09-13 Abbott Gmbh & Co. Kg Asparate ester inhibitors of interleukin-1beta converting enzyme
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
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
EP0998300A1 (en) 1997-03-18 2000-05-10 Basf Aktiengesellschaft Methods and compositions for modulating responsiveness to corticosteroids
JPH111491A (ja) 1997-04-18 1999-01-06 Takeda Chem Ind Ltd ペプチド類及びその剤
JP4439111B2 (ja) * 1997-10-10 2010-03-24 サイトビア インコーポレイテッド ジペプチドのアポトーシスインヒビターおよびそれらの使用
US6184210B1 (en) * 1997-10-10 2001-02-06 Cytovia, Inc. Dipeptide apoptosis inhibitors and the use thereof
JPH11180891A (ja) 1997-12-25 1999-07-06 Dai Ichi Seiyaku Co Ltd 抗細胞死剤
ATE295177T1 (de) 1998-03-16 2005-05-15 Cytovia Inc Dipeptid kaspase inhibitoren und deren verwendung
TR200003252T2 (tr) 1998-05-05 2001-04-20 Warner-Lambert Company Interleukın-1ß dönüştürme enzimi succınamıde inhibitörleri.
US6197750B1 (en) 1998-07-02 2001-03-06 Idun Pharmaceuticals, Inc. C-terminal modified oxamyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases
US6201118B1 (en) 1998-08-19 2001-03-13 Vertex Pharmaceuticals Inc. Process for forming an N-acylated, N,N-containing bicyclic ring from piperazic acid or an ester thereof especially useful as an intermediate in the manufacture of a caspase inhibitor
US6242422B1 (en) 1998-10-22 2001-06-05 Idun Pharmacueticals, Inc. (Substituted)Acyl dipeptidyl inhibitors of the ice/ced-3 family of cysteine proteases
AU764860B2 (en) 1998-12-02 2003-09-04 Merck Frosst Canada & Co. Gamma-ketoacid tetrapeptides as inhibitors of caspase-3
AU765462B2 (en) * 1999-03-16 2003-09-18 Merck Frosst Canada & Co. Gamma-ketoacid dipeptides as inhibitors of caspase-3
DE60030097T2 (de) * 1999-03-16 2007-03-08 Cytovia, Inc., San Diego Substituierte 2-aminobenzamin caspase inhibitoren und ihre verwendung
BR0009610A (pt) 1999-04-09 2002-02-13 Cytovia Inc Inibidores de caspase e uso dos mesmos
JP2003506389A (ja) 1999-08-06 2003-02-18 バーテックス ファーマシューティカルズ インコーポレイテッド カスパーゼ阻害剤およびその使用
EP1212295B1 (en) 1999-08-27 2008-10-01 Cytovia, Inc. Substituted alpha-hydroxy acid caspase inhibitors and the use thereof
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
AR026748A1 (es) 1999-12-08 2003-02-26 Vertex Pharma Un compuesto inhibidor de caspasas, una composicion farmaceutica que lo comprende, un metodo para la sintesis del mismo y un compuesto intermediario paradicha sintesis
AR027993A1 (es) 2000-03-29 2003-04-23 Vertex Pharma Inhibidores de carbonato de caspasa y usos del mismo
CA2380935A1 (en) 2000-05-23 2001-11-29 Vertex Pharmaceuticals Incorporated Caspase inhibitors and uses thereof
JP2003535865A (ja) 2000-06-07 2003-12-02 バーテックス ファーマシューティカルズ インコーポレイテッド カスパーゼインヒビターおよびその使用

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