ZA200207483B - Carbamate caspase inhibitors and uses thereof. - Google Patents
Carbamate caspase inhibitors and uses thereof. Download PDFInfo
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- ZA200207483B ZA200207483B ZA200207483A ZA200207483A ZA200207483B ZA 200207483 B ZA200207483 B ZA 200207483B ZA 200207483 A ZA200207483 A ZA 200207483A ZA 200207483 A ZA200207483 A ZA 200207483A ZA 200207483 B ZA200207483 B ZA 200207483B
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| US7531570B2 (en) * | 2004-05-27 | 2009-05-12 | Vertex Pharmaceuticals Incorporated | Treatment of diseases using ICE inhibitors |
| KR100619439B1 (ko) | 2004-05-27 | 2006-09-08 | 한기종 | 포밀기 도입된 아민유도체의 제조방법 |
| US8012751B2 (en) * | 2005-03-31 | 2011-09-06 | Wisconsin Alumni Research Foundation | Differentiation of pluripotent embryonic stem cells |
| CN101268084A (zh) | 2005-07-28 | 2008-09-17 | 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前体药物 |
| CN101278598B (zh) * | 2005-10-07 | 2011-05-25 | 松下电器产业株式会社 | 音频信号处理装置以及音频信号处理方法 |
| WO2008051243A2 (en) | 2005-11-30 | 2008-05-02 | Massachusetts Institute Of Technology | Pathogen-detecting cell preservation systems |
| US20100137239A1 (en) * | 2006-04-24 | 2010-06-03 | Gloucester Pharmaceuticals | Gemcitabine combination therapy |
| CA2656487A1 (en) * | 2006-07-07 | 2008-01-17 | The Board Of Trustees Of The Leland Stanford Junior University | Selective caspase inhibitors |
| WO2008021745A2 (en) * | 2006-08-16 | 2008-02-21 | Itherx Pharmaceuticals, Inc. | Hepatitis c virus entry inhibitors |
| CA2666814A1 (en) * | 2006-08-21 | 2008-05-29 | United Therapeutics Corporation | Combination therapy for treatment of viral infections |
| WO2008106167A1 (en) * | 2007-02-28 | 2008-09-04 | Conatus Pharmaceuticals, Inc. | Combination therapy comprising matrix metalloproteinase inhibitors and caspase inhibitors for the treatment of liver diseases |
| US8828950B2 (en) * | 2007-05-01 | 2014-09-09 | Cedars-Sinai Medical Center | Caspase inhibitors in the treatment of infection-associated preterm delivery |
| KR101009588B1 (ko) * | 2008-06-04 | 2011-01-20 | 거진산업주식회사 | 미세여과막을 이용한 부유고형물 처리장치 |
| JP2012051804A (ja) * | 2008-12-26 | 2012-03-15 | Kyoto Univ | Ｅｇ５阻害剤 |
| KR101010350B1 (ko) * | 2009-03-26 | 2011-01-25 | 삼성중공업 주식회사 | 역세척 여과장치 |
| WO2012061785A2 (en) | 2010-11-05 | 2012-05-10 | Brandeis University | Ice inhibiting compounds and uses thereof |
| TW201236239A (en) * | 2010-11-16 | 2012-09-01 | Solvay | Rechargeable metal or metal-ion cell |
| EP2490021A1 (en) | 2011-02-18 | 2012-08-22 | Biotempt B.V. | Modulators of PRR and GPCR signalling |
| US9956260B1 (en) | 2011-07-22 | 2018-05-01 | The J. David Gladstone Institutes | Treatment of HIV-1 infection and AIDS |
| EP3142649B1 (en) | 2014-05-12 | 2019-07-24 | Conatus Pharmaceuticals, Inc. | Treatment of the complications of chronic liver disease with caspase inhibitor emricasan |
| WO2017079566A1 (en) | 2015-11-05 | 2017-05-11 | Conatus Pharmaceuticals, Inc. | Caspase inhibitors for use in the treatment of liver cancer |
| SG11201805480TA (en) | 2015-12-31 | 2018-07-30 | Conatus Pharmaceuticals Inc | Methods of using caspase inhibitors in treatment of liver disease |
| MX2019003889A (es) | 2016-10-05 | 2019-08-12 | Novartis Ag | Composiciones de combinacion que comprenden agonistas de fxr para tratar o prevenir una enfermedad o trastorno fibrotico o cirrotico. |
| PL3630742T3 (pl) * | 2017-05-24 | 2024-04-08 | Ramot At Tel-Aviv University Ltd. | Sondy chemiluminescencyjne do obrazowania/wykrywania proteaz |
| WO2022123062A1 (en) | 2020-12-11 | 2022-06-16 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Blocking caspase and/or fasl for preventing fatal outcome in covid-19 patients |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1991015577A1 (en) | 1990-04-04 | 1991-10-17 | Black, Roy, A. | INTERLEUKIN 1'beta' PROTEASE |
| ATE257517T1 (de) | 1991-08-30 | 2004-01-15 | Vertex Pharma | Interleukin 1-beta protease und ihre inhibitoren |
| EP0618223A3 (en) | 1993-03-08 | 1996-06-12 | Sandoz Ltd | Peptides, the release of Interleukin 1-Bêta, useful as anti-inflammatory agents. |
| WO1996030395A2 (en) | 1995-03-31 | 1996-10-03 | Takeda Chemical Industries, Ltd. | Cysteine protease inhibitor |
| EP0900791A1 (en) | 1995-12-27 | 1999-03-10 | Ono Pharmaceutical Co., Ltd. | Tetrazole derivatives and drugs containing the same as the active ingredient |
| CN1234038A (zh) | 1996-09-12 | 1999-11-03 | 伊邓药品公司 | 作为ICE/ced－3类半胱氨酸蛋白酶抑制剂的C－末端修饰的(N－取代)－2－吲哚基二肽 |
| PL332640A1 (en) * | 1996-10-11 | 1999-09-27 | Warner Lambert Co | Sulphonamide-group substituted derivatives of aspartic acid as inhibitors of an interleukin-1beta transforming enzyme |
| EP0932598A1 (en) | 1996-10-11 | 1999-08-04 | Warner-Lambert Company | ASPARTATE ESTER INHIBITORS OF INTERLEUKIN-1$g(b) CONVERTING ENZYME |
| CA2306692C (en) | 1997-10-10 | 2010-09-21 | Cytovia, Inc. | Dipeptide apoptosis inhibitors and the use thereof |
| US6184210B1 (en) | 1997-10-10 | 2001-02-06 | Cytovia, Inc. | Dipeptide apoptosis inhibitors and the use thereof |
| CA2323439A1 (en) | 1998-03-16 | 1999-09-23 | Cytovia, Inc. | Dipeptide caspase inhibitors and the use thereof |
| US6242422B1 (en) | 1998-10-22 | 2001-06-05 | Idun Pharmacueticals, Inc. | (Substituted)Acyl dipeptidyl inhibitors of the ice/ced-3 family of cysteine proteases |
| JP2002539183A (ja) | 1999-03-16 | 2002-11-19 | サイトビア インコーポレイテッド | 置換２−アミノベンズアミドカスパーゼインヒビターおよびその使用 |
| ATE363465T1 (de) | 1999-04-09 | 2007-06-15 | Cytovia Inc | Caspase inhibitoren und ihre verwendung |
| DE60040397D1 (de) | 1999-08-27 | 2008-11-13 | Cytovia Inc | Substituierte alpha-hydroxy-säuren als caspase-hemmer und ihre verwendung |
| PE20011267A1 (es) * | 2000-03-29 | 2001-12-15 | Vertex Pharma | Carbamato como inhibidores de caspasa |
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