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1.发明授权公开(公告)号：US10337014B2
公开(公告)日：2019-07-02
申请号：US15706041
申请日：2017-09-15
IPC分类号： C07D211/40 , C12N15/113 , A61K9/51 , C07D223/08 , C07D207/12
摘要： The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids comprising at least one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.
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公开(公告)号：US10336684B2
公开(公告)日：2019-07-02
申请号：US16033645
申请日：2018-07-12
发明人： Peter T. W. Cheng , David S. Yoon
IPC分类号： C07C229/42 , C07C59/72 , C07D205/04 , C07C62/34 , C07C59/68 , C07C59/64 , C07D213/65 , C07D211/46 , C07D211/42 , C07D211/14 , C07D207/12 , C07D223/08 , A61K31/192 , A61K31/196 , A61K31/397 , A61K31/402 , A61K31/44 , A61K31/451 , A61K31/55
摘要： The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.
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公开(公告)号：US10292987B2
公开(公告)日：2019-05-21
申请号：US15459141
申请日：2017-03-15
发明人： Jae U. Jeong , Deepak Bandyopadhyay , Patrick M. Eidam , Philip Anthony Harris , Jianxing Kang , Bryan Wayne King , Ami Lakdawala Shah , Lara Kathryn Leister , Attiq Rahman , Joshi M. Ramanjulu , Clark A. Sehon , Robert Singhaus, Jr. , Daohua Zhang
IPC分类号： A61K31/553 , C07D267/14 , C07D403/12 , C07D413/14 , C07D403/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D487/04 , C07D498/04 , C07D281/10 , A61K31/55 , C07D223/08
摘要： Disclosed are compounds having the formula: wherein X, Y, Z1, Z2, Z3, Z4, R5, RA, m, A. L, and B are as defined herein, and methods of making and using the same.
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4.发明申请公开(公告)号：US20170015629A1
公开(公告)日：2017-01-19
申请号：US15277421
申请日：2016-09-27
发明人： George D. Hartman , Scott Kuduk
IPC分类号： C07D223/08 , A61K31/55 , C07D221/22 , A61K31/439 , C07D267/10 , A61K31/554 , C07D243/08 , A61K31/551 , C07D295/26 , C07D403/12 , C07D223/32 , C07D283/00 , A61K45/06 , A61K31/553
CPC分类号： C07D223/08 , A61K31/439 , A61K31/55 , A61K31/551 , A61K31/553 , A61K31/554 , A61K38/21 , A61K45/06 , A61K47/60 , C07D221/22 , C07D223/06 , C07D223/32 , C07D243/08 , C07D267/10 , C07D283/00 , C07D295/26 , C07D403/12 , A61K2300/00
摘要： Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
摘要翻译： 本文提供了可用于治疗有需要的受试者的HBV感染的化合物，其药物组合物，以及抑制，抑制或预防受试者中HBV感染的方法。
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公开(公告)号：US09181288B2
公开(公告)日：2015-11-10
申请号：US14597814
申请日：2015-01-15
发明人： George D. Hartman , Scott Kuduk
IPC分类号： A61K31/55 , C07D223/08 , C07D267/10 , C07F9/6527 , C07D223/06 , C07D221/24 , A61K31/439 , A61K31/553 , C07D243/08 , A61K31/5513 , C07D223/32 , C07D281/06 , A61K31/554 , C07F9/553 , A61K31/675 , A61K45/06 , A61K31/551
CPC分类号： A61K31/675 , A61K31/439 , A61K31/55 , A61K31/551 , A61K31/5513 , A61K31/553 , A61K31/554 , A61K38/21 , A61K38/212 , A61K38/215 , A61K38/217 , A61K39/292 , A61K45/06 , C07D221/24 , C07D223/06 , C07D223/08 , C07D223/32 , C07D243/08 , C07D267/10 , C07D281/06 , C07F9/5532 , C07F9/6527 , A61K2300/00
摘要： Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject. In an embodiment of the compounds provided herein, the compounds are of Formula Va:
摘要翻译： 本文提供了可用于治疗有需要的受试者的HBV感染的化合物，其药物组合物，以及抑制，抑制或预防受试者中HBV感染的方法。 在本文提供的化合物的一个实施方案中，化合物为式Va：
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6.发明申请公开(公告)号：US20150197533A1
公开(公告)日：2015-07-16
申请号：US14597814
申请日：2015-01-15
发明人： George D. Hartman , Scott Kuduk
IPC分类号： C07F9/6527 , A61K31/55 , C07D223/06 , C07D221/24 , A61K31/439 , C07D267/10 , A61K31/553 , C07D243/08 , A61K31/5513 , C07D223/32 , C07D281/06 , A61K31/554 , C07F9/553 , A61K31/675 , A61K45/06 , C07D223/08
CPC分类号： A61K31/675 , A61K31/439 , A61K31/55 , A61K31/551 , A61K31/5513 , A61K31/553 , A61K31/554 , A61K38/21 , A61K38/212 , A61K38/215 , A61K38/217 , A61K39/292 , A61K45/06 , C07D221/24 , C07D223/06 , C07D223/08 , C07D223/32 , C07D243/08 , C07D267/10 , C07D281/06 , C07F9/5532 , C07F9/6527 , A61K2300/00
摘要： Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
摘要翻译： 本文提供了可用于治疗有需要的受试者的HBV感染的化合物，其药物组合物，以及抑制，抑制或预防受试者中HBV感染的方法。
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公开(公告)号：US08835682B2
公开(公告)日：2014-09-16
申请号：US13827101
申请日：2013-03-14
IPC分类号： C07C229/00 , C07C233/80 , C07D453/02 , C07D211/46 , C07D333/24 , C07D223/08 , C07D491/08 , C07D451/10 , C07D211/44 , C07D209/02 , C07D207/12 , C07D211/42
CPC分类号： C07D453/02 , C07C233/80 , C07D207/12 , C07D209/02 , C07D211/42 , C07D211/44 , C07D211/46 , C07D223/08 , C07D333/24 , C07D451/10 , C07D491/08
摘要： Alkaloid aminoester compounds which act as muscarinic receptor antagonists are useful for the prevention and/or treatment of a broncho-obstructive or inflammatory diseases.
摘要翻译： 作为毒蕈碱受体拮抗剂的生物碱类氨基酯化合物可用于预防和/或治疗支气管阻塞性或炎性疾病。
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公开(公告)号：US08217063B2
公开(公告)日：2012-07-10
申请号：US12529342
申请日：2008-03-15
申请人： Michael Hahn , Eva-Maria Becker , Andreas Knorr , Dirk Schneider , Johannes-Peter Stasch , Karl-Heinz Schlemmer , Frank Wunder , Dieter Lang
发明人： Michael Hahn , Eva-Maria Becker , Andreas Knorr , Dirk Schneider , Johannes-Peter Stasch , Karl-Heinz Schlemmer , Frank Wunder , Dieter Lang
IPC分类号： C07D207/24 , C07D233/32 , C07D249/12 , C07D255/02 , C07D211/74 , C07D239/10 , C07D241/08 , C07D223/08 , C07D263/18 , C07D271/07 , C07D265/10 , C07D265/32 , C07D273/02 , C07D273/04 , C07D273/06 , A61K31/4015 , A61K31/4166 , A61K31/4196 , A61K31/42 , A61K31/421 , A61K31/4245 , A61K31/4412 , A61K31/45 , A61K31/513 , A61K31/53 , A61K31/535 , A61K31/5375 , A61K31/539 , A61K31/5395
CPC分类号： C07D207/267 , C07D211/76 , C07D239/10 , C07D263/22 , C07D265/32
摘要： The present application relates to novel lactam-substituted dicarboxylic acid derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
摘要翻译： 本申请涉及新型内酰胺取代的二羧酸衍生物，其制备方法，其用于治疗和/或预防疾病的用途及其用于治疗和/或预防疾病，特别是用于治疗的药物的用途 和/或预防心血管疾病。
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9.发明申请SUBSTITUTED AZEPINE- AND DIAZEPINE-SULFONAMIDES USEFUL TO INHIBIT 11BETA-HYDROXYSTEROID DEHYDROGENASE TYPE-1 审中-公开用于抑制11BETA-羟基脱氢酶脱氢酶1型的替代亚硒酸和二氮杂萘磺酰胺公开(公告)号：US20110129542A1
公开(公告)日：2011-06-02
申请号：US12672826
申请日：2008-08-12
IPC分类号： A61K31/55 , C07D223/08 , C07D401/12 , C07D409/04 , C07D243/08 , A61K31/551 , C07D403/04 , A61K35/60 , A61P3/00 , A61P3/04 , A61P9/10 , A61P9/12 , A61P3/10 , C12N9/99
CPC分类号： C07D223/08 , C07D223/04 , C07D223/12 , C07D223/30 , C07D243/08 , C07D401/12 , C07D409/04
摘要： In its many embodiments, the present invention relates to a novel class of substituted azepine- and diazepine-sulfonamide compounds useful to inhibit 11β-hydroxysteroid dehydrogenase type-I, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11β-hydroxysteroid dehydrogenase type-I using such compounds or pharmaceutical compositions.
摘要翻译： 在其许多实施方案中，本发明涉及可用于抑制11β-羟基类固醇脱氢酶I型的新一类替代的吖庚因和二氮杂 - 磺酰胺化合物，含有该化合物的药物组合物，以及治疗，预防，抑制或抑制 使用这些化合物或药物组合物改善与11＆bgr-羟基类固醇脱氢酶I型的表达相关的一种或多种病症。
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公开(公告)号：US20090298781A1
公开(公告)日：2009-12-03
申请号：US12094828
申请日：2006-11-22
申请人： Enrique Perez Payá , Maria Jesús Vicent Docon , Mar Orzaez Calatayud , Laura Mondragon Martinez , Angél Messeguer Paypoch , Alejadra Moure Fernandez , Gloria Sanclimens Perez De Rozas , Gema Malet Engra
发明人： Enrique Perez Payá , Maria Jesús Vicent Docon , Mar Orzaez Calatayud , Laura Mondragon Martinez , Angél Messeguer Paypoch , Alejadra Moure Fernandez , Gloria Sanclimens Perez De Rozas , Gema Malet Engra
CPC分类号： C07K5/0821 , C07K5/1024 , C07K14/001
摘要： The present invention relates to compounds of formula (I) as well as to drug conjugates based on compounds of formula (I) acting as apoptosis inhibitors, as well as to processes for their preparation, to pharmaceutical compositions containing them and their use in medicine.
摘要翻译： 本发明涉及式（I）化合物以及基于作为凋亡抑制剂的式（I）化合物的药物偶联物，以及其制备方法，含有它们的药物组合物及其在药物中的用途。
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