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141. 发明申请

US20140221478A1 DI-FLUORO CONTAINING COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS 审中-公开
标题翻译：含氟化合物作为CYSTEINE PROTEASE抑制剂
公开(公告)号：US20140221478A1
公开(公告)日：2014-08-07
申请号：US14247117
申请日：2014-04-07
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
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。

142. 发明授权

US08367732B2 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：US08367732B2
公开(公告)日：2013-02-05
申请号：US13004834
申请日：2011-01-11
申请人： John O. Link , Craig J. Mossman , Jie Liu , Soon Hyung Woo
发明人： John O. Link , Craig J. Mossman , Jie Liu , Soon Hyung Woo
IPC分类号： A61K31/165
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。

143. 发明申请

US20120329837A1 CATHEPSIN INHIBITORS FOR TREATING MICROGLIA-MEDIATED NEURON LOSS IN THE CENTRAL NERVOUS SYSTEM 审中-公开
标题翻译：用于治疗中枢神经系统中微小介导的神经元损失的CATHEPSIN抑制剂
公开(公告)号：US20120329837A1
公开(公告)日：2012-12-27
申请号：US13525845
申请日：2012-06-18
申请人： Robert Booth
发明人： Robert Booth
IPC分类号： A61K31/277 , A61P25/00 , A61P25/16 , A61K31/4406 , A61P25/28
CPC分类号： A61K31/277 , A61K9/0019 , A61K9/08 , A61K9/2054 , A61K31/4406 , A61K47/12 , A61K47/26
摘要： The present invention concerns methods of using Cathepsin S inhibitors and compounds of Formula I that are inhibitors of cathepsin S in treating CNS disorders, diseases, and injuries, particularly neurodegenerative conditions. The present invention is directed to pharmaceutical compositions comprising these compounds for treating CNS disorders.
摘要翻译：本发明涉及使用组织蛋白酶S抑制剂的组织蛋白酶S抑制剂和式I化合物在治疗CNS疾病，疾病和损伤，特别是神经变性病症中的方法。本发明涉及包含这些化合物用于治疗CNS障碍的药物组合物。

144. 发明授权

US08324417B2 Process for the preparation of (S)-2-amino-5-cyclopropyl-4,4-difluoropentanoic acid and alkyl esters and acid salts thereof 有权
标题翻译：（S）-2-氨基-5-环丙基-4,4-二氟戊酸及其烷基酯及其酸盐的制备方法
公开(公告)号：US08324417B2
公开(公告)日：2012-12-04
申请号：US12857477
申请日：2010-08-16
申请人： Barry Hart , Jeff Dener , Michael Green , Michael Standen , Oldrich Kocian
发明人： Barry Hart , Jeff Dener , Michael Green , Michael Standen , Oldrich Kocian
IPC分类号： C07C213/02 , C07C303/26 , C07C67/303 , C07C67/307
CPC分类号： C07C53/23 , C07B2200/07 , C07C67/307 , C07C67/347 , C07C69/635 , C07C227/18 , C07C309/65 , C07C2601/02 , C07C229/28
摘要： The present invention relates to a process for the preparation of alkyl esters of (S)-2-amino-5-cyclopropyl-4,4-difluoropentanoic acid, which are intermediates useful in the synthesis of (S)—N-(1-cyanocyclopropyl)-5-cyclopropyl-4,4-difluoro-2-((S)-2,2,2-trifluoro-1-(4-fluorophenyl)ethylamino)pentanamide and related compounds, which are compounds that are cysteine protease inhibitors.
摘要翻译：本发明涉及一种制备（S）-2-氨基-5-环丙基-4,4-二氟戊酸的烷基酯的方法，其是用于合成（S）-N-（1- 氰基环丙基）-5-环丙基-4,4-二氟-2 - （（S）-2,2,2-三氟-1-（4-氟苯基）乙基氨基）戊酰胺及其相关化合物，它们是半胱氨酸蛋白酶抑制剂。

145. 发明申请

US20090270415A1 COMPOUNDS THAT INHIBIT PROTEASE CATHEPSIN S AND HCV REPLICATION 失效
标题翻译：抑制蛋白激酶S和HCV复制的化合物
公开(公告)号：US20090270415A1
公开(公告)日：2009-10-29
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： A61K31/497 , C07D403/12
CPC分类号： C07D403/12
摘要： The present invention is directed to compounds 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。

146. 发明申请

US20090233909A1 Sulfonamide compounds as cysteine protease inhibitors 有权
标题翻译：磺酰胺化合物作为半胱氨酸蛋白酶抑制剂
公开(公告)号：US20090233909A1
公开(公告)日：2009-09-17
申请号：US11792101
申请日：2005-12-01
申请人： Soon H. Woo , Randall W. Vivian , John O. Link
发明人： Soon H. Woo , Randall W. Vivian , John O. Link
IPC分类号： A61K31/55 , C07D265/30 , A61K31/5375 , C07D241/04 , A61K31/495 , C07C311/01 , A61K31/18 , C07D211/08 , A61K31/445 , C07D223/02 , C07D213/57 , A61K31/44 , A61P9/00 , A61P37/00 , A61P17/06 , A61P29/00
CPC分类号： C07D209/08 , C07C311/32 , C07C2601/02 , C07D207/48 , C07D211/96 , C07D213/32 , C07D213/76 , C07D217/08 , C07D295/13 , C07D295/26 , C07D401/04 , C07D487/08
摘要： The present invention is directed to compounds of formula (I) 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. Wherein R3 is -alkylene-SO2NR5R6.
摘要翻译：本发明涉及作为半胱氨酸蛋白酶抑制剂，特别是组织蛋白酶B，K，L，F和S的式（I）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。其中R3是 - 亚烷基-SO2NR5R6。

147. 发明申请

US20090203629A1 INHIBITORS OF CATHEPSIN B 失效
标题翻译： CATHEPSIN B的抑制剂
公开(公告)号：US20090203629A1
公开(公告)日：2009-08-13
申请号：US12366504
申请日：2009-02-05
申请人： Leslie Holsinger
发明人： Leslie Holsinger
IPC分类号： A61K38/06 , A61K38/05
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。

148. 发明授权

US07488848B2 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：US07488848B2
公开(公告)日：2009-02-10
申请号：US11384023
申请日：2006-03-17
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： C07C233/05 , A61K31/65
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。

149. 发明申请

US20090023781A1 Haloalkyl Containing Compounds as Cysteine Protease Inhibitors 有权
标题翻译：含卤素的化合物作为半胱氨酸蛋白酶抑制剂
公开(公告)号：US20090023781A1
公开(公告)日：2009-01-22
申请号：US11791928
申请日：2005-12-01
申请人： Eduardo L. Setti
发明人： Eduardo L. Setti
IPC分类号： A61K31/4436 , A61K31/165 , C07C323/65 , A61P11/06 , A61P9/10 , C07D409/06
CPC分类号： C07C317/48 , C07C323/29 , C07C2601/02 , C07D213/38 , C07D213/65 , C07D333/20 , C07D335/02 , C07D409/06
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。

150. 发明申请

US20070287699A1 ANTIVIRAL AGENTS 审中-公开
标题翻译：抗病毒剂
公开(公告)号：US20070287699A1
公开(公告)日：2007-12-13
申请号：US11742461
申请日：2007-04-30
申请人： Dange Kumar , Roopa Rai , Wendy Young , Huiyong Hu , Jennifer Riggs , Tony Ton , Michael Green , Barry Hart , Kenneth Brameld , Jeffrey Dener
发明人： Dange Kumar , Roopa Rai , Wendy Young , Huiyong Hu , Jennifer Riggs , Tony Ton , Michael Green , Barry Hart , Kenneth Brameld , Jeffrey Dener
IPC分类号： A61K31/4709 , A61K31/496 , A61K31/5355 , A61K31/541 , A61K31/551 , A61P31/14 , C07D215/233 , C07D243/08 , C07D279/12 , C07D401/04 , C07D413/04 , C07D455/02 , C07D471/04
CPC分类号： C07D413/14 , C07D413/04
摘要： Compounds are provided having utility for the treatment of viral infections, particularly HCV.
摘要翻译：提供了可用于治疗病毒感染，特别是HCV的化合物。

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