SK287070B6 - Profarmakum ICE inhibítora, farmaceutická kompozícia s jeho obsahom, jeho použitie a medziprodukt - Google Patents
Profarmakum ICE inhibítora, farmaceutická kompozícia s jeho obsahom, jeho použitie a medziprodukt Download PDFInfo
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Families Citing this family (33)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CZ302281B6 (cs) * | 1998-03-19 | 2011-01-26 | Vertex Pharmaceuticals Incorporated | Inhibitory kaspázy a farmaceutická kompozice, která je obsahuje |
TWI373343B (en) * | 2000-02-10 | 2012-10-01 | Abbott Gmbh & Co Kg | Antibodies that bind human interleukin-18 and methods of making and using |
PE20011350A1 (es) | 2000-05-19 | 2002-01-15 | Vertex Pharma | PROFARMACO DE UN INHIBIDOR DE ENZIMA CONVERTIDORA DE INTERLEUCINA-1ß (ICE) |
US7410956B2 (en) * | 2002-02-11 | 2008-08-12 | Vertex Pharmaceuticals Incorporated | Caspase inhibitor prodrugs |
WO2003080104A2 (en) | 2002-03-22 | 2003-10-02 | Applied Research Systems Ars Holding N.V. | Use of il-18 inhibitors for the treatment and/or prevention of peripheral vascular diseases |
JP2007510931A (ja) * | 2003-11-10 | 2007-04-26 | 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 | Il−18をモニターするための方法 |
US7968684B2 (en) | 2003-11-12 | 2011-06-28 | Abbott Laboratories | IL-18 binding proteins |
US20050233974A1 (en) * | 2003-12-01 | 2005-10-20 | John Randle | Treating infectious diseases using ice inhibitors |
AR047981A1 (es) * | 2004-02-27 | 2006-03-15 | Vertex Pharma | Inhibidores de caspasa y sus usos correspondientes |
CN1942466B (zh) * | 2004-02-27 | 2011-02-23 | 沃泰克斯药物股份有限公司 | 天冬氨酸特异性半胱氨酸蛋白酶抑制剂及其用途 |
AU2011226946B2 (en) * | 2004-02-27 | 2012-05-03 | Vertex Pharmaceuticals Incoporated | Caspase Inhibitors and Uses Thereof |
EP1725548B1 (en) | 2004-03-12 | 2015-01-14 | Vertex Pharmaceuticals Incorporated | Processes and intermediates for the preparation of aspartic acetal caspase inhibitors |
NZ588448A (en) * | 2004-05-15 | 2012-01-12 | Vertex Pharma | Treating seizures using interleukin-1beta converting enzyme (ICE) inhibitors |
US7531570B2 (en) * | 2004-05-27 | 2009-05-12 | Vertex Pharmaceuticals Incorporated | Treatment of diseases using ICE inhibitors |
CA2610691C (en) | 2005-06-03 | 2015-12-01 | Laboratoires Serono S.A. | Use of il-18bp isoforms for the treatment and/or prevention of neurological inflammatory diseases |
US7879891B2 (en) * | 2005-07-28 | 2011-02-01 | Vertex Pharmaceuticals Incorporated | Caspase inhibitor prodrugs |
EP2037887B1 (en) * | 2006-05-31 | 2010-09-15 | Vertex Pharmaceuticals Incorporated | Oral controlled release formulations of an interleukin-1 beta converting enzyme inhibitor |
WO2008060621A2 (en) * | 2006-11-17 | 2008-05-22 | Abbott Laboratories | Aminopyrrolidines as chemokine receptor antagonists |
CA2695244A1 (en) | 2007-08-03 | 2009-02-12 | Sanofi-Aventis | Caspase imaging probes |
US20100158905A1 (en) | 2008-12-19 | 2010-06-24 | Nuon Therapeutics, Inc. | Combination therapy of arthritis with tranilast |
US9365612B2 (en) | 2010-01-29 | 2016-06-14 | United States Of America As Represented By The Secretary, Department Of Health And Human Services | Caspase inhibitors |
EP2635907A4 (en) * | 2010-11-05 | 2014-04-16 | Univ Brandeis | ALPHA-SYNUCLEINE CLIVED ICE AS A BIOLOGICAL MARKER |
US9944674B2 (en) | 2011-04-15 | 2018-04-17 | Genesis Technologies Limited | Selective cysteine protease inhibitors and uses thereof |
US9956260B1 (en) | 2011-07-22 | 2018-05-01 | The J. David Gladstone Institutes | Treatment of HIV-1 infection and AIDS |
EP2848696A1 (en) | 2013-09-13 | 2015-03-18 | Sanofi-Aventis Deutschland GmbH | Caspase-1 imaging probes |
JP7213555B2 (ja) | 2016-12-23 | 2023-01-27 | シーエーエスピー-エイド インク. | 神経学的状態の予防および治療のためのカスパーゼ1の阻害およびその使用 |
ES2769975B2 (es) * | 2018-12-27 | 2020-12-04 | Univ Murcia | Inhibidores de caspasa 1 para el tratamiento de anemia |
CA3146794A1 (en) * | 2019-07-16 | 2021-01-21 | Rush University Medical Center | Use of a benzoate containing composition to treat neurodegenerative disorders |
BR112022021827A2 (pt) | 2020-05-01 | 2023-01-17 | Medstar Health Inc | Métodos para tratar covid-19 |
EP4225301A1 (en) | 2020-10-07 | 2023-08-16 | Institut National de la Santé et de la Recherche Médicale | Treatments of coronavirus infections, cytokine release syndrome, cytokine storm syndrome, or diseases associated with excessive activation of inflammasomes by the use of inhibitors of inflammatory caspases |
FR3114741A1 (fr) | 2020-10-07 | 2022-04-08 | Etienne Jacotot | Traitements des infections à coronavirus, du syndrome de libération de cytokine, du syndrome de la tempête de cytokines ou des maladies associées à l'activation excessive des inflammasomes par l'utilisation d'inhibiteurs des caspases inflammatoires. |
EP4377295A1 (en) * | 2021-07-28 | 2024-06-05 | F. Hoffmann-La Roche AG | Haloacethydrazides useful as aep inhibitors |
WO2024097731A2 (en) * | 2022-11-02 | 2024-05-10 | Medstar Health, Inc. | Methods for treating covid-19 |
Family Cites Families (124)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
US4465679A (en) * | 1983-01-31 | 1984-08-14 | Usv Pharmaceutical Corporation | 1,2-Diaza-3-one compounds, their use in treating hypertension and pharmaceutical compositions thereof |
IL72523A (en) | 1983-08-12 | 1988-06-30 | Takeda Chemical Industries Ltd | 3-amino-4-oxo-2,3,4,5-tetrahydro-1,5-benzoxazepine derivatives,their production and pharmaceutical compositions containing them |
US5055451A (en) * | 1986-12-22 | 1991-10-08 | Syntex Inc. | Aryloxy and arylacyloxy methyl ketones as thiol protease inhibitors |
US5158936A (en) * | 1986-12-22 | 1992-10-27 | Syntex (U.S.A.) Inc. | Aryloxy and arylacyloxy methyl ketones as thiol protease inhibitors |
US5008245A (en) * | 1988-10-27 | 1991-04-16 | University Of Kentucky Research Foundation | Novel peptidyl carbamate inhibitors of the enzyme elastase |
CA2021660A1 (en) | 1989-07-26 | 1991-01-27 | Philippe Bey | Peptidase inhibitors |
NZ235155A (en) | 1989-09-11 | 1993-04-28 | Merrell Dow Pharma | Peptidase substrates in which the carboxy terminal group has been replaced by a tricarbonyl radical |
AU7775991A (en) | 1990-04-04 | 1991-10-30 | Immunex Corporation | Interleukin 1beta protease |
US5416013A (en) * | 1990-04-04 | 1995-05-16 | Sterling Winthrop Inc. | Interleukin 1β protease and interleukin 1β protease inhibitors |
ES2124710T3 (es) * | 1991-03-15 | 1999-02-16 | Hoechst Ag | Procedimiento para el acoplamiento pinacolinico reductor diastereoselectivo de alfa-aminoaldehidos homoquirales. |
DE69226820T2 (de) | 1991-06-21 | 1999-05-12 | Merck & Co., Inc., Rahway, N.J. | Peptidylderivate als Inhibitoren von Interleukin-1B-konvertierenden Enzymen |
JP3190431B2 (ja) | 1991-07-01 | 2001-07-23 | 三菱化学株式会社 | ケトン誘導体 |
DE69229252T2 (de) | 1991-08-16 | 1999-12-16 | Merck & Co., Inc. | DNS, welche das Interleukin-1B-Vorläufer-Converting-Enzym kodiert |
EP0533226A3 (en) | 1991-08-16 | 1993-08-18 | Merck & Co. Inc. | Novel chromophore containing compounds |
US5278061A (en) | 1991-08-16 | 1994-01-11 | Merck & Co., Inc. | Affinity chromatography matrix useful in purifying interleukin-1β converting enzyme |
US6348570B1 (en) | 1991-08-16 | 2002-02-19 | Merck & Co., Inc. | Chromophore containing compounds and their use in determining interleukin-1β convertase activity |
DE69133354T2 (de) | 1991-08-30 | 2004-11-11 | Vertex Pharmaceuticals Inc., Cambridge | Interleukin 1-beta protease und ihre inhibitoren |
EP0541946B1 (de) * | 1991-10-07 | 1996-07-17 | Hoechst Aktiengesellschaft | Verfahren zur diastereoselektiven reduktiven Pinakol-Kupplung von homochiralen alpha-Aminoaldehyden |
GB9123326D0 (en) | 1991-11-04 | 1991-12-18 | Sandoz Ltd | Improvements in or relating to organic compounds |
AU1339092A (en) | 1991-12-13 | 1993-07-19 | Corvas International, Inc. | Reagents for automated synthesis of peptide analogs |
EP0547699A1 (en) | 1991-12-19 | 1993-06-23 | Merck & Co. Inc. | Peptidyl derivatives as inhibitors of interleukin-1B converting enzyme |
AU3479593A (en) | 1992-01-31 | 1993-09-01 | Merck & Co., Inc. | Peptidyl derivatives as inhibitors of interleukin-1beta converting enzyme |
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 |
JPH08500242A (ja) | 1992-06-24 | 1996-01-16 | 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前駆体の転換酵素をコードするDNA |
WO1994003480A1 (en) | 1992-07-31 | 1994-02-17 | Pfizer Inc. | Peptidyl 4-amino-2,2-difluoro-3-oxo-1,6-hexanedioic acid derivatives as antiinflammatory agents |
CA2109646C (en) * | 1992-11-24 | 2000-03-07 | Gaston O. Daumy | Para-nitroanilide peptides |
EP0618223A3 (en) | 1993-03-08 | 1996-06-12 | Sandoz Ltd | Peptides, the release of Interleukin 1-Bêta, useful as anti-inflammatory agents. |
TW494094B (en) | 1993-04-29 | 2002-07-11 | Vertex Pharma | Peptide analogs as irreversible interleukin-1β protease inhibitors and pharmaceutical compositions comprising the same |
US5462939A (en) * | 1993-05-07 | 1995-10-31 | Sterling Winthrop Inc. | Peptidic ketones as interleukin-1β-converting enzyme inhibitors |
US5411985A (en) * | 1993-05-17 | 1995-05-02 | Merck & Co., Inc. | Gamma-pyrone-3-acetic acid as an inhibitor or interleukin-1 β inventory enzyme |
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 |
DK0644197T3 (da) | 1993-06-04 | 1999-06-07 | Vertex Pharma | Peptidphosphinyloxymethylketoner som inhibitorer af interleukin-1beta-konverterende enzymer |
JPH08511690A (ja) | 1993-06-24 | 1996-12-10 | ザ・ジェネラル・ホスピタル・コーポレーション | プログラムされた細胞死遺伝子及びタンパク質 |
JPH08512006A (ja) | 1993-06-30 | 1996-12-17 | フォード モーター カンパニー | 自動車hvacシステムを制御する方法およびシステム |
AU7714594A (en) | 1993-08-13 | 1995-03-14 | Merck & Co., Inc. | Substituted ketone derivatives as inhibitors of interleukin-1beta converting enzyme |
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 |
DE69532113T2 (de) | 1994-03-31 | 2004-07-29 | Vertex Pharmaceuticals Inc., Cambridge | Pyrimidin-derivate als interleukin inhibitoren |
MX9605196A (es) | 1994-04-29 | 1997-12-31 | Sanofi Winthrop Inc | Halometilamidas como inhibidores de la proteasa il-1b. |
BE1008343A3 (nl) | 1994-05-06 | 1996-04-02 | Dsm Nv | Bidentaat fosfineligand |
US5492824A (en) | 1994-05-12 | 1996-02-20 | Basf Ag | Ice and ice-like compositions and methods of making same |
US5552400A (en) | 1994-06-08 | 1996-09-03 | Sterling Winthrop Inc. | Fused-bicyclic lactams as interleukin-1β converting enzyme inhibitors |
US5856116A (en) | 1994-06-17 | 1999-01-05 | Vertex Pharmaceuticals, Incorporated | Crystal structure and mutants of interleukin-1 beta 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 |
US6420522B1 (en) | 1995-06-05 | 2002-07-16 | Vertex Pharmaceuticals Incorporated | Inhibitors of interleukin-1β converting enzyme |
US5847135A (en) | 1994-06-17 | 1998-12-08 | Vertex Pharmaceuticals, Incorporated | Inhibitors of interleukin-1β converting enzyme |
US5565430A (en) * | 1994-08-02 | 1996-10-15 | Sterling Winthrop Inc. | Azaaspartic acid analogs as interleukin-1β converting enzyme inhibitors |
US5704001A (en) | 1994-08-04 | 1997-12-30 | Qualcomm Incorporated | Sensitivity weighted vector quantization of line spectral pair frequencies |
GB2292149A (en) | 1994-08-09 | 1996-02-14 | Ferring Res Ltd | Peptide inhibitors of pro-interleukin-1beta converting enzyme |
US5498616A (en) * | 1994-11-04 | 1996-03-12 | Cephalon, Inc. | Cysteine protease and serine protease inhibitors |
TW394764B (en) | 1995-02-14 | 2000-06-21 | Mitsubishi Chemcal Corp | Oxygen-containing heterocyclic derivatives |
KR0144921B1 (ko) * | 1995-02-17 | 1998-07-01 | 김광호 | 반도체 메모리소자의 커패시터 구조 및 그 제조방법 |
WO1996030395A2 (en) | 1995-03-31 | 1996-10-03 | Takeda Chemical Industries, Ltd. | Cysteine protease inhibitor |
JPH09165360A (ja) | 1995-03-31 | 1997-06-24 | Takeda Chem Ind Ltd | システインプロテアーゼ阻害剤 |
US5798442A (en) | 1995-04-21 | 1998-08-25 | Merck Frosst Canada, Inc. | Peptidyl derivatives as inhibitors of pro-apoptotic cysteine proteinases |
WO1997008174A1 (en) | 1995-08-31 | 1997-03-06 | Smithkline Beecham Corporation | Interleukin converting enzyme and apoptosis |
WO1997007805A1 (en) | 1995-08-31 | 1997-03-06 | Smithkline Beecham Corporation | Interleukin converting enzyme and apoptosis |
US5744451A (en) | 1995-09-12 | 1998-04-28 | Warner-Lambert Company | N-substituted glutamic acid derivatives with interleukin-1 β converting enzyme inhibitory activity |
EP0761680A3 (en) * | 1995-09-12 | 1999-05-06 | Ono Pharmaceutical Co., Ltd. | Tetrazole compounds having Interleukin-1beta converting enzyme inhibitory activity |
US5843904A (en) | 1995-12-20 | 1998-12-01 | Vertex Pharmaceuticals, Inc. | Inhibitors of interleukin-1βconverting enzyme |
EP0900791A1 (en) * | 1995-12-27 | 1999-03-10 | Ono Pharmaceutical Co., Ltd. | Tetrazole derivatives and drugs containing the same as the active ingredient |
WO1998001133A1 (fr) | 1996-07-08 | 1998-01-15 | Yamanouchi Pharmaceutical Co., Ltd. | Inhibiteurs de la resorption osseuse |
WO1998004539A1 (fr) | 1996-07-29 | 1998-02-05 | Mitsubishi Chemical Corporation | Derives heterocycliques oxygenes |
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 |
EP0874850B1 (en) | 1996-09-12 | 2002-04-10 | Idun Pharmaceuticals, Inc. | Novel tricyclic compounds for the inhibition of the ice/ced-3 protease family of enzymes |
EP0929311B8 (en) | 1996-09-12 | 2006-02-01 | Idun Pharmaceuticals, Inc. | INHIBITION OF APOPTOSIS USING INTERLEUKIN-1 beta-CONVERTING ENZYME (ICE)/CED-3 FAMILY INHIBITORS |
US6200969B1 (en) | 1996-09-12 | 2001-03-13 | Idun Pharmaceuticals, Inc. | Inhibition of apoptosis using interleukin-1β-converting enzyme (ICE)/CED-3 family inhibitors |
AU739321B2 (en) | 1996-09-12 | 2001-10-11 | Idun Pharmaceuticals, Incorporated | 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 |
KR20000049047A (ko) | 1996-10-11 | 2000-07-25 | 로즈 암스트롱, 크리스틴 에이. 트러트웨인 | 술폰아미드 인터루킨-1β 전환 효소 억제제 |
WO1998016502A1 (en) | 1996-10-11 | 1998-04-23 | Warner-Lambert Company | ASPARTATE ESTER INHIBITORS OF INTERLEUKIN-1β CONVERTING ENZYME |
US5919790A (en) | 1996-10-11 | 1999-07-06 | Warner-Lambert Company | Hydroxamate inhibitors of interleukin-1β converting enzyme |
ES2169880T3 (es) | 1996-10-18 | 2002-07-16 | Vertex Pharma | Inhibidores de proteasas de serina, particularmente de la proteasa ns3 del virus de la hepatitis c. |
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 |
US6054487A (en) | 1997-03-18 | 2000-04-25 | Basf Aktiengesellschaft | Methods and compositions for modulating responsiveness to corticosteroids |
HUP9700816A3 (en) | 1997-04-28 | 1999-06-28 | Gyogyszerkutato Intezet | 3(r)-3-amino-4-carboxy-butiraldehyde derivatives inhibiting release of interleukin-1-beta |
FR2766188B1 (fr) | 1997-07-15 | 2000-02-11 | Hoechst Marion Roussel Inc | Nouveau procede de preparation de derives amines d'alkyloxy furanone, composes issus de ce procede et utilisation de ces composes |
US6184210B1 (en) | 1997-10-10 | 2001-02-06 | Cytovia, Inc. | Dipeptide apoptosis inhibitors and the use thereof |
JP4524039B2 (ja) | 1997-12-18 | 2010-08-11 | ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド | Srcファミリーsh2ドメインインヒビターとしてのピリドン |
CA2309546A1 (en) | 1998-01-20 | 1999-07-22 | Warner-Lambert Company | N-[2-(5-benzyloxycarbonyl-amino-6-oxo-2-(4-fluorophenyl)-1,6-dihydro-1-pyrimidinyl)acetoxyl]-l-aspartic acid aldehyde as an in vivo inhibitor of interleukin-1.beta. converting enzyme (ice) |
CZ302281B6 (cs) | 1998-03-19 | 2011-01-26 | Vertex Pharmaceuticals Incorporated | Inhibitory kaspázy a farmaceutická kompozice, která je obsahuje |
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 |
US6323180B1 (en) | 1998-08-10 | 2001-11-27 | Boehringer Ingelheim (Canada) Ltd | Hepatitis C inhibitor tri-peptides |
US6242422B1 (en) | 1998-10-22 | 2001-06-05 | Idun Pharmacueticals, Inc. | (Substituted)Acyl dipeptidyl inhibitors of the ice/ced-3 family of cysteine proteases |
AU765462B2 (en) | 1999-03-16 | 2003-09-18 | Merck Frosst Canada & Co. | Gamma-ketoacid dipeptides as inhibitors of caspase-3 |
KR20010110667A (ko) | 1999-03-16 | 2001-12-13 | 추후보정 | 치환 2-아미노벤즈아미드 카스파제 저해제 및 그것의 용도 |
WO2000061542A1 (en) | 1999-04-09 | 2000-10-19 | Cytovia, Inc. | Caspase inhibitors and the use thereof |
WO2001005772A1 (en) | 1999-07-19 | 2001-01-25 | Merck Frosst Canada & Co. | Pyrazinones, compositions containing such compounds |
AU6894800A (en) | 1999-08-06 | 2001-03-05 | Vertex Pharmaceuticals Incorporated | Caspase inhibitors and uses thereof |
US6442565B1 (en) | 1999-08-13 | 2002-08-27 | Hiddenmind Technology, Inc. | System and method for transmitting data content in a computer network |
EA200200301A1 (ru) | 1999-08-27 | 2002-08-29 | Сайтовиэ, Инк. | ЗАМЕЩЕННЫЕ α-ГИДРОКСИКИСЛОТЫ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СПОСОБ ИНГИБИРОВАНИЯ КЛЕТОЧНОЙ ГИБЕЛИ НА КЛЕТОЧНОМ ИЛИ ТКАНЕВОМ УРОВНЕ, СПОСОБ ЛЕЧЕНИЯ ИЛИ ОБЛЕГЧЕНИЯ СОСТОЯНИЯ ПРИ ГИБЕЛИ КЛЕТОК У ЖИВОТНОГО, СПОСОБ ЛЕЧЕНИЯ ИЛИ ПРОФИЛАКТИКИ РАЗЛИЧНЫХ БОЛЕЗНЕЙ |
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 |
US6689784B2 (en) | 2000-03-29 | 2004-02-10 | Vertex Pharmaceuticals Incorporated | Carbamate caspase inhibitors and uses thereof |
ES2240446T3 (es) | 2000-04-03 | 2005-10-16 | Vertex Pharma | Inhibidores de serina proteasas, particularmente la proteasa ns3 del virus de la hepatitis c. |
ATE472539T1 (de) | 2000-04-24 | 2010-07-15 | Vertex Pharma | Verfahren und zwischenprodukte zur herstellung von substituierten asparaginsäure-acetalen |
TWI291462B (en) | 2000-04-25 | 2007-12-21 | Daiichi Sankyo Co Ltd | Hydrate crystal of neuraminic acid compound |
PE20011350A1 (es) | 2000-05-19 | 2002-01-15 | Vertex Pharma | PROFARMACO DE UN INHIBIDOR DE ENZIMA CONVERTIDORA DE INTERLEUCINA-1ß (ICE) |
AP2002002407A0 (en) | 2000-05-23 | 2002-03-31 | Vertex Pharma | Caspase inhibitors and uses thereof. |
KR20030025235A (ko) | 2000-06-07 | 2003-03-28 | 버텍스 파마슈티칼스 인코포레이티드 | 카스파제 억제제 및 이의 용도 |
BR0112540A (pt) | 2000-07-21 | 2003-06-24 | Schering Corp | Peptìdios como inibidores da ns-3-serina protease do vìrus da hepatite c |
PE20020500A1 (es) | 2000-09-13 | 2002-06-25 | Vertex Pharma | Derivados de piperidina, tetrahidroquinolina, tetrahidroisoquinolina como inhibidores de caspasas |
US6846806B2 (en) | 2000-10-23 | 2005-01-25 | Bristol-Myers Squibb Company | Peptide inhibitors of Hepatitis C virus NS3 protein |
WO2002042278A2 (en) | 2000-11-21 | 2002-05-30 | Vertex Pharmaceuticals Incorporated | Imidazole and benzimidazole caspase inhibitors and uses thereof |
GB0107924D0 (en) | 2001-03-29 | 2001-05-23 | Angeletti P Ist Richerche Bio | Inhibitor of hepatitis C virus NS3 protease |
JP4676676B2 (ja) | 2001-04-19 | 2011-04-27 | 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 | カスパーゼ阻害剤としての複素環ジカルバミド |
JP4428926B2 (ja) | 2001-05-23 | 2010-03-10 | 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れらの使用 |
JP4455056B2 (ja) | 2001-07-11 | 2010-04-21 | 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 | 架橋二環式セリンプロテアーゼ阻害剤 |
AU2002348533A1 (en) | 2001-10-09 | 2003-05-26 | Vertex Pharmaceuticals Incorporated | Process for synthesizing aspartic and glutamic acid derivatives and diazoketone intermediates thereof |
US7410956B2 (en) | 2002-02-11 | 2008-08-12 | Vertex Pharmaceuticals Incorporated | Caspase inhibitor prodrugs |
EP1499898A2 (en) | 2002-04-19 | 2005-01-26 | Vertex Pharmaceuticals Incorporated | Regulation of tnf-alpha |
US7138395B2 (en) | 2002-06-10 | 2006-11-21 | The Procter & Gamble Company | Interleukin-1β converting enzyme inhibitors |
US7001899B2 (en) | 2002-06-10 | 2006-02-21 | The Procter & Gamble Company | Interleukin converting enzyme inhibitors |
US7041696B2 (en) | 2002-06-17 | 2006-05-09 | The Procter & Gamble Company | Interleukin-1β converting enzyme inhibitors |
CA2493646A1 (en) | 2002-06-28 | 2004-01-08 | Vertex Pharmaceuticals Incorporated | Caspase inhibitors and uses thereof |
EP1581501A1 (en) | 2002-12-20 | 2005-10-05 | Vertex Pharmaceuticals Incorporated | 4-oxo-3-(1-oxo-1h-isoquinolin-2-ylacetylamino)-pentanoic acid ester and amide derivatives and their use as caspase inhibitors |
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 |
JP2007510931A (ja) | 2003-11-10 | 2007-04-26 | 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 | Il−18をモニターするための方法 |
AR047981A1 (es) | 2004-02-27 | 2006-03-15 | Vertex Pharma | Inhibidores de caspasa y sus usos correspondientes |
EP1725548B1 (en) | 2004-03-12 | 2015-01-14 | Vertex Pharmaceuticals Incorporated | Processes and intermediates for the preparation of aspartic acetal caspase inhibitors |
US7531570B2 (en) | 2004-05-27 | 2009-05-12 | Vertex Pharmaceuticals Incorporated | Treatment of diseases using ICE inhibitors |
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