专利检索 ap:("Zhaoning Zhu" OR "Brian McKittrick" OR "Zhong-Yue Sun" OR "Yuanzan Ye" OR "Johannes Voigt" OR "Corey Strickland" OR "Elizabeth Smith" OR "Andrew Stamford" OR "William Greenlee" OR "Robert Mazzola" OR "John Caldwell" OR "Jared Cumming" OR "Lingyan Wang" OR "Yusheng Wu" OR "Ulrich Iserloh" OR "Tao Guo" OR "Thuy Le" OR "Kurt Saionz" OR "Suresh Babu" OR "Rachael Hunter" OR "Michelle Morris" OR "Huizhong Gu" OR "Gang Qian" OR "Dawit Tadesse") AND inv:"Rachael Hunter" 第 1 页

1.

发明申请
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.

2.

发明申请
Heterocyclic aspartyl protease inhibitors 有权

公开(公告)号：US20080200445A1

公开(公告)日：2008-08-21

申请号：US11710582

申请日：2007-02-23

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 , Xiaoxiang Liu , Tao Guo , Thuy Le , Kurt Saionz , Suresh Babu , Rachael Hunter , Michelle Morris , Huizhong Gu , Gang Qian , Dawit Tadesse , Ying Huang , Guoqing Li , Jianping Pan , Jeffrey Misiaszek , Gaifa Lai , Jingqi Duo , Chuanxing Qu , Yuefei Shao

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 , Xiaoxiang Liu , Tao Guo , Thuy Le , Kurt Saionz , Suresh Babu , Rachael Hunter , Michelle Morris , Huizhong Gu , Gang Qian , Dawit Tadesse , Ying Huang , Guoqing Li , Jianping Pan , Jeffrey Misiaszek , Gaifa Lai , Jingqi Duo , Chuanxing Qu , Yuefei Shao

IPC分类号： A61K31/506 , A61K31/4178 , A61K31/4245 , A61K31/4439 , A61K31/454 , A61K31/541 , A61P31/00 , C07D233/02 , C07D271/00 , C07D413/14 , C07D409/14 , C07D409/04 , C07D403/06 , C07D401/14 , C07D401/12 , C07D401/10 , C07D401/06 , C07D239/04 , A61P9/00 , A61P25/00 , A61K31/5377 , A61K31/4545 , A61K31/4709 , A61K31/498

CPC分类号： C07D233/88 , A61K31/4168 , A61K31/4178 , C07D239/22 , C07D401/06 , C07D401/10 , C07D403/06 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/10 , C07D417/14 , C07D495/10

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 1. 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.

3.

发明申请
Heterocyclic aspartyl protease inhibitors 有权

公开(公告)号：US20070072852A1

公开(公告)日：2007-03-29

申请号：US11010772

申请日：2004-12-13

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

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

IPC分类号： A61K31/549 , A61K31/5395 , A61K31/513

CPC分类号： C07D233/88 , A61K31/4168 , A61K31/4178 , A61K31/4184 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/5377 , A61K31/655 , A61K45/06 , C07D233/46 , C07D233/70 , C07D235/02 , C07D239/22 , C07D239/70 , C07D271/07 , C07D273/00 , C07D295/15 , C07D401/04 , C07D401/06 , C07D401/08 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/10 , C07D403/12 , C07D405/06 , C07D405/10 , C07D405/14 , C07D407/06 , C07D409/04 , C07D409/06 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/12 , C07D417/06 , Y02A50/411

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 antagonist.

4.

发明申请
2-Substituted benzimidazole piperidines analogs as selective melanin concentrating hormone receptor antagonists for the treatment of obesity and related disorders 失效
标题翻译： 2-取代的苯并咪唑哌啶类似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：US20050054628A1

公开(公告)日：2005-03-10

申请号：US10926557

申请日：2004-08-26

申请人： Duane Burnett , Wen-Lian Wu , Thavalakulamgara Sasikumar , William Greenlee , Mary Caplen , Tao Guo , Rachael Hunter

发明人： Duane Burnett , Wen-Lian Wu , Thavalakulamgara Sasikumar , William Greenlee , Mary Caplen , Tao Guo , Rachael Hunter

IPC分类号： A61P3/04 , A61P3/10 , C07D401/06 , C07D401/12 , A61K31/46

CPC分类号： C04B35/632 , C07D401/06 , C07D401/12

摘要： The present invention discloses compounds of formula I wherein Ar, Y, m, n, R1 and R4 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： 本发明公开了其中Ar，Y，m，n，R 1和R 4在本文中定义的式I化合物，所述化合物是黑色素浓缩激素（MCH）的新型拮抗剂，以及制备方法这样的化合物。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。