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91. 发明申请

US20110071131A1 Substituted Spirocyclic Piperidine Derivatives as Histamine-3 (H3) Receptor Ligands 失效
标题翻译：取代的螺环哌啶衍生物作为组胺-3（H3）受体配体
公开(公告)号：US20110071131A1
公开(公告)日：2011-03-24
申请号：US12846100
申请日：2010-07-29
申请人： Edward R. Bacon , Nadine C. Becknell , Reddeppa reddy Dandu , Lisa Guise-Zawacki , Tao Guo , Chia-yu Huang , Robert L. Hudkins , Babu G. Sundar , Ming Tao , Minglang Wu , Allison L. Zulli
发明人： Edward R. Bacon , Nadine C. Becknell , Reddeppa reddy Dandu , Lisa Guise-Zawacki , Tao Guo , Chia-yu Huang , Robert L. Hudkins , Babu G. Sundar , Ming Tao , Minglang Wu , Allison L. Zulli
IPC分类号： A61K31/397 , C07D471/10 , A61K31/438 , C07D413/14 , A61K31/5377 , C07D401/14 , A61K31/506 , A61P25/00 , A61P1/00 , A61P11/00 , A61P9/00 , A61P29/00
CPC分类号： C07D491/10
摘要： The present invention provides compounds of Formula (I): their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceuticals compositions thereof.
摘要翻译：本发明提供式（I）化合物：其用作H3拮抗剂/反向激动剂，其制备方法及其药物组合物。

92. 发明授权

US07662816B2 Cyclic amine BACE-1 inhibitors having a benzamide substituent 有权
标题翻译：具有苯甲酰胺取代基的环胺BACE-1抑制剂
公开(公告)号：US07662816B2
公开(公告)日：2010-02-16
申请号：US10910987
申请日：2004-08-04
申请人： Jared N. Cumming , Ulrich Iserloh , Andrew Stamford , Corey Strickland , Johannes H. Voigt , Yusheng Wu , Ying Huang , Yan Xia , Samuel Chackalamannil , Tao Guo , Douglas W. Hobbs , Thuy X. H. Le , Jeffrey F. Lowrie , Kurt W. Saionz , Suresh D. Babu
发明人： Jared N. Cumming , Ulrich Iserloh , Andrew Stamford , Corey Strickland , Johannes H. Voigt , Yusheng Wu , Ying Huang , Yan Xia , Samuel Chackalamannil , Tao Guo , Douglas W. Hobbs , Thuy X. H. Le , Jeffrey F. Lowrie , Kurt W. Saionz , Suresh D. Babu
IPC分类号： A61K31/496 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/12 , C07D211/34 , C07D207/16 , C07D207/26 , C07D243/08 , C07D413/12
CPC分类号： C07D243/08 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/26 , C07D209/52 , C07D211/26 , C07D211/46 , C07D217/18 , C07D233/32 , C07D241/04 , C07D241/08 , C07D401/06 , C07D401/10 , C07D401/12 , C07D403/12 , C07D403/14 , C07D409/06 , C07D409/12 , C07D413/06
摘要： Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I.Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease.Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a β-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.
摘要翻译：公开了下式的化合物或其药学上可接受的盐或溶剂化物，其中R1是R是-C（O）-N（R27）（R28），或其余的变量如说明书中所定义。还公开了包含式I化合物的药物组合物。还公开了治疗认知或神经变性疾病如阿尔茨海默病的方法。还公开了治疗认知或神经变性疾病的药物组合物和方法，其包含式I化合物与除式I以外的β-分泌酶抑制剂，HMG-CoA还原酶抑制剂，γ-分泌酶抑制剂，甾族抗炎剂，N-甲基-D-天冬氨酸受体拮抗剂，胆碱酯酶抑制剂或抗淀粉样蛋白抗体。

93. 发明授权

US07598250B2 Cyclic amine BACE-1 inhibitors having a heterocyclic substituent 有权
标题翻译：具有杂环取代基的环胺BACE-1抑制剂
公开(公告)号：US07598250B2
公开(公告)日：2009-10-06
申请号：US10911030
申请日：2004-08-04
申请人： Jared N. Cumming , Ying Huang , Guoqing Li , Ulrich Iserloh , Andrew Stamford , Corey Strickland , Johannes H. Voigt , Yusheng Wu , Jianping Pan , Tao Guo , Douglas W. Hobbs , Thuy X. H. Le , Jeffrey F. Lowrie
发明人： Jared N. Cumming , Ying Huang , Guoqing Li , Ulrich Iserloh , Andrew Stamford , Corey Strickland , Johannes H. Voigt , Yusheng Wu , Jianping Pan , Tao Guo , Douglas W. Hobbs , Thuy X. H. Le , Jeffrey F. Lowrie
IPC分类号： A61K31/506 , A61K31/496 , C07D403/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
CPC分类号： C04B35/632 , C07D207/277 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14
摘要： Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is X is —O—, —C(R14)2— or —N(R)—; Z is —C(R14)2— or —N(R)—; t is 0, 1, 2 or 3; each R and R2 is independently H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, alkenyl or alkynyl; each R14 is H, alkyl, alkenyl, alkynyl, halo, —CN, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, —OR35, —N(R24)(R25) or —SR35; R41 is alkyl, cycloalkyl, —SO2(alkyl), —C(O)-alkyl, —C(O)-cycloalkyl or -alkyl-NH—C(O)CH3; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating cognitive or neurodegenerative diseases with compounds of formula I.Also disclosed are pharmaceutical compositions and methods of treatment comprising compounds of formula I in combination with other agents useful in treating cognitive or neurodegenerative diseases.
摘要翻译：公开了下式的新化合物或其药学上可接受的盐或溶剂合物，其中R 1是X是-O - ， - C（R 14）2 - 或-N（R） - ; Z是-C（R 14）2 - 或-N（R） - ; t为0,1,2或3; 每个R和R 2独立地为H，烷基，环烷基，环烷基烷基，芳基，杂芳基，杂环烷基，芳基烷基，杂芳基烷基，杂环烷基烷基，烯基或炔基; 每个R 14是H，烷基，烯基，炔基，卤素，-CN，卤代烷基，环烷基，环烷基烷基，芳基，杂芳基，杂环烷基，芳基烷基，杂芳基烷基，杂环烷基烷基，-OR 35，-N（R 24）（R 25）或-SR 35; R41是烷基，环烷基，-SO2（烷基），-C（O） - 烷基，-C（O） - 环烷基或 - 烷基-NH-C（O）CH3; 其余变量如本说明书中所定义。还公开了包含式I化合物的药物组合物和用式I化合物治疗认知障碍或神经变性疾病的方法。还公开了药物组合物和治疗方法，其包含式I化合物与用于治疗认知或神经变性的其它药剂疾病

94. 发明授权

US07416840B2 Replication of hepatitis C virus in non-hepatic epithelial and mouse hepatic cells 有权
标题翻译：在非肝上皮和小鼠肝细胞中复制丙型肝炎病毒
公开(公告)号：US07416840B2
公开(公告)日：2008-08-26
申请号：US10536955
申请日：2003-12-12
申请人： Qing Zhu , Ju-Tao Guo , Christoph Seeger
发明人： Qing Zhu , Ju-Tao Guo , Christoph Seeger
IPC分类号： C12Q1/70 , C12N5/10 , C12N15/87
CPC分类号： C12N7/00 , C07K14/005 , C12N2770/24051 , C12N2770/24221 , C12N2770/24222 , G01N2333/18 , G01N2500/10
摘要： Cells and cell lines which replicate HCV of non-hepatic human and non human origin are disclosed. Also provided are methods of using such cells and cell lines to identify anti-HCV agents for the treatment of HCV infection.
摘要翻译：公开了复制非肝人和非人源HCV的细胞和细胞系。还提供了使用这种细胞和细胞系鉴定用于治疗HCV感染的抗HCV药物的方法。

95. 发明申请

US20080176868A1 Preparation and use of compounds as protease inhibitors 有权
标题翻译：化合物作为蛋白酶抑制剂的制备和使用
公开(公告)号：US20080176868A1
公开(公告)日：2008-07-24
申请号：US11451065
申请日：2006-06-12
申请人： Andrew Stamford , Guoqing Li , William Greenlee , Zhaoning Zhu , Brian McKittrick , Robert Mazzola , Ying Huang , Tao Guo , Thuy X.H. Le , Gang Qian , Yuefei Shao
发明人： Andrew Stamford , Guoqing Li , William Greenlee , Zhaoning Zhu , Brian McKittrick , Robert Mazzola , Ying Huang , Tao Guo , Thuy X.H. Le , Gang Qian , Yuefei Shao
IPC分类号： A61K31/519 , C07D209/44 , A61K31/4035 , A61P25/00 , A61P25/28 , A61P31/18 , A61P9/00 , C07D487/04
CPC分类号： C07D471/04 , C07D209/44 , C07D487/04
摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Q is a bond or —N(R5)—; T is a bond, —O—, —C(O)—; S, —N(R5)—, or —C(R6′R7′); U is a bond or —C(R6)(R7)— Y is C or N; Z is C or N; ring A, including variables Y and Z, is a three to nine membered cycloalkyl, cycloalkenyl, heterocylcyl, heterocyclenyl, aryl, and heteroaryl ring having 0 to 4, preferably 0 to 2, heteroatoms independently selected from the group consisting of O, S, N and —N(R)—, wherein ring A is unsubstituted or substituted with 1 to 5 independently selected R1 moieties and/or oxo when ring A is cycloalkyl, cycloalkenyl, heterocyclyl or heterocyclenyl;and R, R1, R2, R3, R4, R5, R6, R6, R7 and R7′ are as defined in the specification; pharmaceutical compositions comprising the compounds of formula I and the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases.
摘要翻译：公开了式I化合物或其立体异构体，互变异构体或其药学上可接受的盐或溶剂化物，其中Q是一个键或-N（R 5） - ; T是键，-O - ， - C（O） - ; S，-N（R 5） - 或-C（R 6'，R 7'）; U是键或-C（R 6）（R 7） - Y是C或N; Z是C或N; 环A包括变量Y和Z是具有0至4个，优选0至2个杂原子的3至9元环烷基，环烯基，杂环基，杂环烯基，芳基和杂芳基环，其独立地选自O，S， N和-N（R） - ，其中当环A是环烷基，环烯基，杂环基或杂环烯基时，环A是未取代的或被1至5个独立选择的R 1 O 1部分和/或氧代取代。 R 1，R 2，R 2，R 3，R 4，R 5， R 4，R 6，R 6，R 7和R 7'如说明书中所定义; 包含式I化合物的药物组合物和抑制天冬氨酰蛋白酶的方法，特别是治疗心血管疾病，认知和神经变性疾病的方法。

96. 发明授权

US07208602B2 Gamma secretase inhibitors 失效
标题翻译： γ分泌酶抑制剂
公开(公告)号：US07208602B2
公开(公告)日：2007-04-24
申请号：US10358898
申请日：2003-02-05
申请人： Dmitri A. Pissarnitski , Hubert B. Josien , Elizabeth M. Smith , John W. Clader , Theodros Asberom , Tao Guo , Douglas W. Hobbs
发明人： Dmitri A. Pissarnitski , Hubert B. Josien , Elizabeth M. Smith , John W. Clader , Theodros Asberom , Tao Guo , Douglas W. Hobbs
IPC分类号： C07D211/08 , C07D207/46 , C07D205/00 , C07D279/00 , A01N43/00
CPC分类号： C07D401/12 , C07D211/96 , C07D401/14 , C07D409/12 , C07D471/10
摘要： This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —X(CO)Y, or alkylene-X(CO)Y wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.
摘要翻译：本发明公开了下式的新型γ分泌酶抑制剂：其中：R 1是取代的芳基或取代的杂芳基; R 2是R 1基团，烷基，-X（CO）Y或亚烷基-X（CO）Y，其中X和Y如本文所定义; 每个R 3和R 3各自独立地为H或烷基; R 11是芳基，杂芳基，烷基，环烷基，芳基烷基，芳基环烷基，杂芳基烷基，杂芳基环烷基，芳基杂环烷基或烷氧基烷基。还公开了使用一种或多种本发明化合物治疗阿尔茨海默病的方法。

97. 发明授权

US07093384B2 Mist iron 有权
标题翻译：薄雾铁
公开(公告)号：US07093384B2
公开(公告)日：2006-08-22
申请号：US10498770
申请日：2002-12-03
申请人： Nyik Siong Wong , Yong Jiang , Tao Guo , Kumar Asok SO Kasevan
发明人： Nyik Siong Wong , Yong Jiang , Tao Guo , Kumar Asok SO Kasevan
IPC分类号： D06F75/22
CPC分类号： D06F75/22 , D06F75/10
摘要： An iron comprising a housing (1), a heatable soleplate (4) and means for generating very fine liquid droplets to be expelled from at least one discharge opening (9) of the iron, said means comprising at least one air passage (8) for pressurized air supply and at least one liquid passage (13) for pressurized liquid supply, said air passage (8) and said liquid passage (13) communicating with each other for mixing air and liquid, said mixture of air and liquid being supplied to the discharge opening (9). To improve the generation of fine liquid droplets (mist) an outlet of the liquid passage (8) ends into the air passage (13) upstream of the discharge opening (9) to introduce liquid into the air passage and an outlet of the air passage is provided with a nozzle (10) having said discharge opening (9). Preferably the pressurized air and liquid supply is obtained by means of electric pumps (6,7). The liquid may be water or a (diluted) additive liquid.
摘要翻译：一种熨斗，包括壳体（1），可加热底板（4）和用于产生要从铁的至少一个排放开口（9）排出的非常细的液滴的装置，所述装置包括至少一个空气通道（8）用于加压空气供应和用于加压液体供应的至少一个液体通道（13），所述空气通道（8）和所述液体通道（13）彼此连通以混合空气和液体，所述空气和液体混合物供应到排出口（9）。为了改善细液滴（雾）的产生，液体通道（8）的出口在排出口（9）的上游端部进入空气通道（13），以将液体引入空气通道和空气通道的出口设置有具有所述排出口（9）的喷嘴（10）。优选地，加压空气和液体供应通过电动泵（6,7）获得。液体可以是水或（稀释的）添加剂液体。

98. 发明申请

US20060128011A1 Replication of hepatitis c virus in non-hepatic epithelial and mouse hepatic cells 有权
标题翻译：在非肝上皮和小鼠肝细胞中复制丙型肝炎病毒
公开(公告)号：US20060128011A1
公开(公告)日：2006-06-15
申请号：US10536955
申请日：2003-12-12
申请人： Qing Zhu , Ju-Tao Guo , Christoph Seeger
发明人： Qing Zhu , Ju-Tao Guo , Christoph Seeger
IPC分类号： C12Q1/68 , C12N7/00 , C12N5/00 , C12N7/01 , C12N5/02
CPC分类号： C12N7/00 , C07K14/005 , C12N2770/24051 , C12N2770/24221 , C12N2770/24222 , G01N2333/18 , G01N2500/10
摘要： Cells and cell lines which replicate HCV of non-hepatic human and non human origin are disclosed. Also provided are methods of using such cells and cell lines to identify anti-HCV agents for the treatment of HCV infection.
摘要翻译：公开了复制非肝人和非人源HCV的细胞和细胞系。还提供了使用这种细胞和细胞系鉴定用于治疗HCV感染的抗HCV药物的方法。

99. 发明申请

US20060111370A1 Heterocyclic aspartyl protease inhibitors 有权
公开(公告)号：US20060111370A1
公开(公告)日：2006-05-25
申请号：US11149027
申请日：2005-06-09
申请人： Zhaoning Zhu , Brian McKittrick , Zhong-Yue Sun , Yuanzan Ye , Johannes Voigt , Corey Strickland , Elizabeth Smith , Andrew Stamford , William Greenlee , Robert Mazzola , John Caldwell , Jared Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Tao Guo , Thuy Le , Kurt Saionz , Suresh Babu , Rachael Hunter , Michelle Morris , Huizhong Gu , Gang Qian , Dawit Tadesse
发明人： Zhaoning Zhu , Brian McKittrick , Zhong-Yue Sun , Yuanzan Ye , Johannes Voigt , Corey Strickland , Elizabeth Smith , Andrew Stamford , William Greenlee , Robert Mazzola , John Caldwell , Jared Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Tao Guo , Thuy Le , Kurt Saionz , Suresh Babu , Rachael Hunter , Michelle Morris , Huizhong Gu , Gang Qian , Dawit Tadesse
IPC分类号： A61K31/519 , A61K31/497 , A61K31/513 , A61K31/4439 , A61K31/454 , A61K31/4245 , C07D413/02 , C07D403/02
CPC分类号： C07D233/46 , C07D233/70 , C07D233/88 , C07D239/22 , C07D239/70 , C07D271/07 , C07D273/00 , C07D401/04 , C07D401/08 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/10 , C07D403/12 , C07D405/10 , C07D409/04 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/12 , C07D417/06
摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(═S)—, —S(O)—, —S(O)2—, —C(═O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(═N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(═O)— or —C(═NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(═NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

100. 发明申请

US20060111360A1 Bicyclic compounds as selective melanin concentrating hormone receptor antagonists for the treatment of obesity and related disorders 失效
标题翻译：双环化合物作为选择性黑色素浓缩激素受体拮抗剂用于治疗肥胖症和相关疾病
公开(公告)号：US20060111360A1
公开(公告)日：2006-05-25
申请号：US11247635
申请日：2005-10-11
申请人： Tao Guo , Huizhong Gu , Douglas Hobbs
发明人： Tao Guo , Huizhong Gu , Douglas Hobbs
IPC分类号： A61K31/496 , A61K31/495 , C07D405/14 , C07D403/14 , C07D241/04
CPC分类号： C07D213/75 , C07D295/13 , C07D311/58
摘要： The present invention discloses compounds of Formula I wherein V, W, Y, Z, R1, R2, R3, R4, d, m, n, p and r are herein defined, said compounds being novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
摘要翻译：本发明公开了式I的化合物，其中V，W，Y，Z，R 1，R 2，R 3，R SUP 本文定义了d，m，n，p和r，所述化合物是黑色素浓缩激素（MCH）的新型拮抗剂，以及制备这些化合物的方法。在另一个实施方案中，本发明公开了包含这样的MCH拮抗剂的药物组合物以及使用它们治疗肥胖，代谢紊乱，进食障碍如食欲过盛和糖尿病的方法。

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