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121. 发明公开

EP2079683A2 DI-FLUORO CONTAINING COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS 有权
标题翻译： DIFLUORHALTIGE化合物作为半胱氨酸蛋白酶抑制剂
公开(公告)号：EP2079683A2
公开(公告)日：2009-07-22
申请号：EP07853752.9
申请日：2007-10-03
申请人： ViroBay, Inc.
发明人： LINK, John O. , MOSSMAN, Craig J. , LIU, Jie , WOO, Soon Hyung
IPC分类号： C07C255/46 , A61K31/275 , A61P19/02 , A61P9/10
CPC分类号： C07C255/46
摘要： The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S, and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.

122. 发明公开

EP1906945A2 HCV INHIBITORS 有权
标题翻译： HCV抑制剂
公开(公告)号：EP1906945A2
公开(公告)日：2008-04-09
申请号：EP06774467.2
申请日：2006-06-29
申请人： Virobay, Inc.
发明人： GRAUPE, Michael , LINK, John O. , VENKATARAMANI, Chandrasekar
IPC分类号： A61K31/00 , A61K31/74 , A61K47/00 , C07K5/08
CPC分类号： A61K38/05 , C07K5/06034
摘要： The present invention is directed to compounds that are antiviral agents. Specifically the compounds of the present invention inhibit replication of HCV and are therefore useful in treating hepatitis C infections. The present invention is also directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
摘要翻译：本发明涉及作为抗病毒剂的化合物。具体而言，本发明的化合物抑制HCV的复制，因此可用于治疗丙型肝炎感染。本发明还涉及包含这些化合物的药物组合物及其制备方法。

123. 发明授权

US08748649B2 Di-fluoro containing compounds as cysteine protease inhibitors 有权
标题翻译：二氟化合物作为半胱氨酸蛋白酶抑制剂
公开(公告)号：US08748649B2
公开(公告)日：2014-06-10
申请号：US13719024
申请日：2012-12-18
申请人： ViroBay, Inc.
发明人： John O. Link , Craig J. Mossman , Jie Liu , Soon Hyung Woo
IPC分类号： C07C255/46 , A61K31/26
CPC分类号： C07C255/46 , A61K31/26 , C07C2601/02
摘要： The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S, and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
摘要翻译：本发明涉及半胱氨酸蛋白酶，特别是组织蛋白酶B，K，L，F和S的抑制剂的化合物，因此可用于治疗由这些蛋白酶介导的疾病。本发明涉及包含这些化合物的药物组合物及其制备方法。

124. 发明申请

US20120282267A1 CATHEPSIN INHIBITORS FOR THE TREATMENT OF BONE CANCER AND BONE CANCER PAIN 失效
标题翻译：用于治疗骨癌和骨癌的卡非汀抑制剂
公开(公告)号：US20120282267A1
公开(公告)日：2012-11-08
申请号：US13462587
申请日：2012-05-02
申请人： Robert Booth
发明人： Robert Booth
IPC分类号： A61K31/165 , A61P35/04 , A61P25/00 , A61K39/395
CPC分类号： A61K31/165 , A61K31/16 , A61K2300/00
摘要： The present invention is directed to methods of using compounds that are inhibitors of cysteine proteases, in particular, of both cathepsins S and K and optionally further cathepsins B and/or L in treating bone cancer. The present invention is directed to pharmaceutical compositions comprising these compounds for treating bone cancer and bone cancer pain, especially the pain associated with metastasis. A single compound can be used to ameliorate the pain, the injury to bone, while also reducing tumor growth, the risk of metastasis and/or invasiveness of the cancer.
摘要翻译：本发明涉及使用半胱氨酸蛋白酶抑制剂，特别是组织蛋白酶S和K以及任选的其它组织蛋白酶B和/或L治疗骨癌的化合物的方法。本发明涉及包含这些用于治疗骨癌和骨癌疼痛的化合物的药物组合物，特别是与转移有关的疼痛。单一化合物可用于改善疼痛，对骨骼的损伤，同时还可降低肿瘤生长，转移的风险和/或侵袭癌症的风险。

125. 发明授权

US08211897B2 Inhibitors of cathepsin B 失效
标题翻译：组织蛋白酶B的抑制剂
公开(公告)号：US08211897B2
公开(公告)日：2012-07-03
申请号：US12366504
申请日：2009-02-05
申请人： Leslie Holsinger
发明人： Leslie Holsinger
IPC分类号： C07D401/02 , A61K31/47
CPC分类号： A61K38/05
摘要： The present invention is directed to a method of using compounds of Formula (I) to inhibit Cathepsin B. Specifically the compounds of the present invention are useful as therapeutic agents for the treatment of tumor invasion, metastasis, Alzheimer's Disease, arthritis, inflammatory diseases such as chronic and acute pancreatitis, inflammatory airway disease, and bone and joint disorders, including osteoporosis, osteoarthritis, rheumatoid arthritis, psoriasis, and other autoimmune disorders, liver fibrosis, including liver fibrosis associated with HCV, all types of steatosis (including non-alcoholic steatohepatitis) and alcohol-associated steatohepatitis, non-alcoholic fatty liver disease, forms of pulmonary fibrosis including idiopathic pulmonary fibrosis, pathological diagnosis of interstitial pneumonia following lung biopsy, renal fibrosis, cardiac fibrosis, retinal angiogenesis and fibrosis/gliosis in the eye, schleroderma, and systemic sclerosis. The compounds of Formula (I) are also useful for treating subjects with both HCV and fibrosis in a mammal, particularly liver fibrosis, and subjects affirmatively diagnosed or at risk for both HCV and liver fibrosis.
摘要翻译：本发明涉及使用式（I）化合物抑制组织蛋白酶B的方法。具体地，本发明的化合物可用作治疗肿瘤侵袭，转移，阿尔茨海默病，关节炎，炎性疾病等的治疗剂作为慢性和急性胰腺炎，炎性气道疾病以及骨关节疾病，包括骨质疏松症，骨关节炎，类风湿性关节炎，牛皮癣和其他自身免疫性疾病，肝纤维化，包括与HCV相关的肝纤维化，所有类型的脂肪变性（包括非酒精性脂肪性肝炎）和酒精性脂肪性肝炎，非酒精性脂肪性肝病，包括特发性肺纤维化的肺纤维化形式，肺活检后间质性肺炎的病理诊断，肾纤维化，心脏纤维化，视网膜血管生成和眼睛纤维化/神经胶质增生，硬皮病和系统性硬化症。式（I）的化合物还可用于治疗哺乳动物，特别是肝纤维化中HCV和纤维化两者的受试者，以及被肯定地诊断或具有HCV和肝纤维化风险的受试者。

126. 发明授权

US08106059B2 Substituted pyrazines that inhibit protease cathepsin S and HCV replication 失效
标题翻译：抑制蛋白酶组织蛋白酶S和HCV复制的取代吡嗪
公开(公告)号：US08106059B2
公开(公告)日：2012-01-31
申请号：US12256370
申请日：2008-10-22
申请人： Leslie Jean Holsinger , Kyle Elrod , John O. Link , Michael Graupe , In Jong Kim
发明人： Leslie Jean Holsinger , Kyle Elrod , John O. Link , Michael Graupe , In Jong Kim
IPC分类号： A61K31/4965
CPC分类号： C07D403/12
摘要： The present invention is directed to compounds of formula I, below, that have the dual property of acting as cathepsin S inhibitors and of inhibiting HCV replication. Such compounds are therefore useful in treating disease states that include hepatitis C, Alzheimer's disease, and autoimmune disorders. The present invention is also directed to pharmaceutical compositions containing these compounds, and processes for preparing the compounds.
摘要翻译：本发明涉及具有作为组织蛋白酶S抑制剂和抑制HCV复制的双重性质的下式I的化合物。因此，这样的化合物可用于治疗包括丙型肝炎，阿尔茨海默氏病和自身免疫性疾病的疾病状态。本发明还涉及含有这些化合物的药物组合物及其制备方法。

127. 发明申请

US20110281879A1 SULFONYL CONTAINING COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS 审中-公开
标题翻译：含有磺基化蛋白酶抑制剂的含硫化合物
公开(公告)号：US20110281879A1
公开(公告)日：2011-11-17
申请号：US13005361
申请日：2011-01-12
申请人： Craig Mossman
发明人： Craig Mossman
IPC分类号： A61K31/4406 , C07C255/46 , C07D237/08 , C07D307/38 , C07D277/30 , C07D239/26 , C07D207/46 , C07D249/08 , C07D235/26 , C07D215/14 , C07D241/38 , C07D209/20 , C07D311/00 , C07D285/12 , C07D211/86 , C07D261/08 , C07D285/14 , C07D277/64 , C07D249/04 , A61K31/4402 , A61K31/277 , A61K31/50 , A61K31/341 , A61K31/426 , A61K31/505 , A61K31/4015 , A61K31/4196 , A61K31/4184 , A61K31/47 , A61K31/502 , A61K31/404 , A61K31/351 , A61K31/433 , A61K31/4412 , A61K31/42 , A61K31/428 , A61K31/4192 , A61P29/00 , A61P25/00 , A61P17/06 , A61P17/00 , A61P5/14 , A61P19/04 , A61P11/06 , A61P9/10 , C07D213/56
CPC分类号： C07C317/46 , C07C2601/02 , C07C2601/04 , C07D213/32 , C07D213/70 , C07D261/08
摘要： The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
摘要翻译：本发明涉及半胱氨酸蛋白酶，特别是组织蛋白酶B，K，L，F和S的抑制剂的化合物，因此可用于治疗由这些蛋白酶介导的疾病。本发明涉及包含这些化合物的药物组合物及其制备方法。

128. 发明授权

US08013183B2 Alpha ketoamide compounds as cysteine protease inhibitors 有权
标题翻译： α-酮酰胺化合物作为半胱氨酸蛋白酶抑制剂
公开(公告)号：US08013183B2
公开(公告)日：2011-09-06
申请号：US12711217
申请日：2010-02-23
申请人： Michael Graupe , John O. Link , Michael G. Roepel
发明人： Michael Graupe , John O. Link , Michael G. Roepel
IPC分类号： C07C317/48 , C07D213/34
CPC分类号： C07C317/48 , C07C2601/02 , C07D213/32
摘要： The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
摘要翻译：本发明涉及半胱氨酸蛋白酶，特别是组织蛋白酶B，K，L，F和S的抑制剂的化合物，因此可用于治疗由这些蛋白酶介导的疾病。本发明涉及包含这些化合物的药物组合物及其制备方法。

129. 发明申请

US20100305331A1 ALPHA KETOAMIDE COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS 有权
标题翻译： ALPHA KETOAMIDE化合物作为CYSTEINE PROTEASE抑制剂
公开(公告)号：US20100305331A1
公开(公告)日：2010-12-02
申请号：US12711217
申请日：2010-02-23
申请人： Michael Graupe , John O. Link , Michael G. Roepel
发明人： Michael Graupe , John O. Link , Michael G. Roepel
IPC分类号： C07C317/48 , C07D213/34
CPC分类号： C07C317/48 , C07C2601/02 , C07D213/32
摘要： The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
摘要翻译：本发明涉及半胱氨酸蛋白酶，特别是组织蛋白酶B，K，L，F和S的抑制剂的化合物，因此可用于治疗由这些蛋白酶介导的疾病。本发明涉及包含这些化合物的药物组合物及其制备方法。

130. 发明申请

US20090312571A1 PROCESS FOR THE PREPARATION OF (3S)-3-AMINO-N-CYCLOPROPYL-2-HYDROXYALKANAMIDE DERIVATIVES 失效
标题翻译：制备（3S）-3-氨基-N-环丙基-2-羟基烷酰胺衍生物的方法
公开(公告)号：US20090312571A1
公开(公告)日：2009-12-17
申请号：US12484078
申请日：2009-06-12
申请人： Jeffrey Dener
发明人： Jeffrey Dener
IPC分类号： C07C229/18 , C07C237/14 , C07C237/20 , C07C209/50 , C07C53/00
CPC分类号： C07C229/18 , C07C237/02 , C07C237/14
摘要： The present invention relates to a process for the preparation of (2S,3S)-3-amino-N-cyclopropyl-2-hydroxyalkanamides as well as novel compounds prepared or used in the process.
摘要翻译：本发明涉及制备（2S，3S）-3-氨基-N-环丙基-2-羟基烷酰胺的方法以及在该方法中制备或使用的新化合物。

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