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1.发明申请EFFICIENT PRODUCTION OF HETEROLOGOUS PROTEINS USING MANNOSYL TRANSFERASE INHIBITORS 有权使用芒硝转移酶抑制剂有效生产异位蛋白公开(公告)号：US20130316398A1
公开(公告)日：2013-11-28
申请号：US13588022
申请日：2012-08-17
申请人： RANJIT DESAI , Lihu Yang
发明人： RANJIT DESAI , Lihu Yang
IPC分类号： C12P21/00 , C07D277/36
CPC分类号： C12P21/005 , C07D277/36 , C12P21/02
摘要： Compounds and methods are described for producing protein compositions having reduced amounts of O-linked glycosylation. The method includes producing the protein in cells cultured in the presence of certain benzylidene thiazolidinediones inhibitors of Pmt-mediated O-linked glycosylation.
摘要翻译： 描述了用于生产具有降低量的O-连接糖基化的蛋白质组合物的化合物和方法。 该方法包括在某些亚苄基噻唑烷二酮类Pmt介导的O-连接糖基化抑制剂存在下培养的细胞中产生蛋白质。
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公开(公告)号：US08592371B2
公开(公告)日：2013-11-26
申请号：US13761407
申请日：2013-02-07
发明人： Tesfaye Biftu , Ann E. Weber
IPC分类号： A61K31/4162 , A61K45/06
CPC分类号： C07D309/30 , A61K9/2054 , A61K31/4162 , A61K38/1709 , A61K38/26 , A61K45/06 , C07D487/04
摘要： The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
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公开(公告)号：US10570202B2
公开(公告)日：2020-02-25
申请号：US15115730
申请日：2015-02-03
IPC分类号： C07K16/28 , A61K39/395 , A61K31/4439 , A61K45/06 , C07K16/30
摘要： The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1) and a VEGFR inhibitor, and the use of the combination therapies for the treatment of cancer, and in particular for treating cancers that express PD-L1.
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公开(公告)号：US09145348B2
公开(公告)日：2015-09-29
申请号：US14355105
申请日：2012-10-26
IPC分类号： C07D263/20 , C07C41/18 , C07C41/30 , A01N43/76 , A61K31/421
CPC分类号： C07C41/18 , C07C41/30 , C07D263/20 , C07C43/23 , C07C43/225
摘要： An efficient process is disclosed for producing the compound of formula I, which is the CETP inhibitor anacetrapib, which raises HDL-cholesterol and reduces LDL-cholesterol in human patients and may be effective for treating or reducing the risk of developing atherosclerosis:
摘要翻译： 公开了一种有效的方法，用于生产式I化合物，其为CETP抑制剂anacetrapib，其提高人类患者的HDL-胆固醇并降低LDL-胆固醇，并且可有效治疗或降低发展动脉粥样硬化的风险：
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公开(公告)号：US08957194B2
公开(公告)日：2015-02-17
申请号：US13466433
申请日：2012-05-08
申请人： Jon H. Condra , Rose M. Cubbon , Holly A. Hammond , Timothy McCabe , Shilpa Pandit , Laurence B. Peterson , Joseph C. Santoro , Ayesha Sitlani , Dana D. Wood , Henryk Mach , Heidi Pixley , Sonia M. Gregory , Jeffrey T. Blue , Kevin Wang , Peizhi (Peter) Luo , Denise K. Nawrocki , Pingyu Zhong , Feng Dong , Yan Li
发明人： Jon H. Condra , Rose M. Cubbon , Holly A. Hammond , Timothy McCabe , Shilpa Pandit , Laurence B. Peterson , Joseph C. Santoro , Ayesha Sitlani , Dana D. Wood , Henryk Mach , Heidi Pixley , Sonia M. Gregory , Jeffrey T. Blue , Kevin Wang , Peizhi (Peter) Luo , Denise K. Nawrocki , Pingyu Zhong , Feng Dong , Yan Li
CPC分类号： C07K16/40 , A61K2039/505 , C07K2317/56 , C07K2317/565 , C07K2317/76 , C07K2317/77 , C07K2317/92 , C12N9/6424
摘要： Antagonists of human proprotein convertase subtilisin-kexin type 9 (“PCSK9”) are disclosed. The disclosed antagonists are effective in the inhibition of PCSK9 function and, accordingly, present desirable antagonists for use in the treatment of conditions associated with PCSK9 activity. The present invention also discloses nucleic acid encoding said antagonists, vectors, host cells, and compositions comprising the antagonists. Methods of making PCSK9-specific antagonists as well as methods of using the antagonists for inhibiting or antagonizing PCSK9 function are also disclosed and form important additional aspects of the present disclosure.
摘要翻译： 公开了人前体蛋白转化酶枯草杆菌蛋白酶-Kexin 9型（“PCSK9”）的拮抗剂。 所公开的拮抗剂在抑制PCSK9功能方面是有效的，因此，呈现用于治疗与PCSK9活性相关的病症的所需拮抗剂。 本发明还公开了编码所述拮抗剂，载体，宿主细胞和包含拮抗剂的组合物的核酸。 还公开了制备PCSK9特异性拮抗剂的方法以及使用拮抗剂抑制或拮抗PCSK9功能的方法，并形成了本公开的重要的附加方面。
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公开(公告)号：US20140343053A1
公开(公告)日：2014-11-20
申请号：US14357690
申请日：2012-11-09
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D401/06 , C07D401/14 , C07D403/06 , C07D413/14 , C07D417/14
摘要： The present invention is directed to triazolopyridinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
摘要翻译： 本发明涉及三唑并吡咯酮化合物，其可用作治疗与磷酸二酯酶10（PDE10）相关的中枢神经系统疾病的治疗剂。 本发明还涉及这些化合物用于治疗神经和精神疾病如精神分裂症，精神病或亨廷顿病以及与纹状体功能减退或基底神经节功能障碍相关的疾病的用途。
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公开(公告)号：US20130039916A1
公开(公告)日：2013-02-14
申请号：US13530854
申请日：2012-06-22
IPC分类号： A61K39/395 , C12N15/13 , A61P37/06 , A61P29/00 , A61P19/02 , C12P21/02 , A61P1/00 , A61P25/00 , A61P19/04 , A61P3/10 , A61P35/00 , C07K16/24 , A61P17/06
CPC分类号： A61K45/06 , A61K2039/505 , C07K16/244 , C07K2317/24 , C07K2317/56 , C07K2317/565 , C07K2317/73 , C07K2317/76 , C07K2317/92
摘要： Engineered antibodies to human IL-23p19 are provided, as well as uses thereof, e.g. in treatment of inflammatory, autoimmune, and proliferative disorders.
摘要翻译： 提供了针对人IL-23p19的工程抗体，以及其用途，例如， 治疗炎症，自身免疫和增殖性疾病。
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8.发明申请BENZYLETHER AND BENZYLAMINO BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE 有权用于治疗阿尔茨海默病的苯甲醚和苯甲酰胺抑制剂公开(公告)号：US20100210693A1
公开(公告)日：2010-08-19
申请号：US12772711
申请日：2010-05-03
IPC分类号： A61K31/18 , C07C311/01 , C07D333/24 , C07D405/04 , C07D207/09 , C07D213/72 , A61K31/381 , A61K31/4025 , A61K31/40 , A61K31/44 , A61P25/28
CPC分类号： C07D213/81 , C07C255/57 , C07C311/08 , C07C2601/02 , C07D207/06 , C07D207/08 , C07D213/76 , C07D295/192 , C07D333/20 , C07D405/04
摘要： The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及作为β-分泌酶的抑制剂并且可用于治疗涉及β-分泌酶的疾病如阿尔茨海默氏病的化合物。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。
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公开(公告)号：US09828369B2
公开(公告)日：2017-11-28
申请号：US15508562
申请日：2015-08-31
申请人： Merck Sharp & Dohme Corp. , Jason Imbriglio , Clare London , Zhijian Lu , James Tata , Yusheng Xiong , Ming You , Hye Won Youm
发明人： Jason Imbriglio , Clare London , Zhijian Lu , James Tata , Yusheng Xiong , Ming You , Hyewon Youm
IPC分类号： C07D217/02 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D417/12 , C07D413/12
CPC分类号： C07D417/12 , A61K45/06 , A61P9/10 , C07D217/02 , C07D217/12 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/12
摘要： The present invention relates to a compound represented by formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cardio-renal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.
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公开(公告)号：US20200325228A1
公开(公告)日：2020-10-15
申请号：US16742657
申请日：2020-01-14
IPC分类号： C07K16/28 , A61K39/395 , A61K31/4439 , A61K45/06 , C07K16/30
摘要： The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1) and a VEGFR inhibitor, and the use of the combination therapies for the treatment of cancer, and in particular for treating cancers that express PD-L 1.
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