公开(公告)号：US20070155675A1

公开(公告)日：2007-07-05

申请号：US11705978

申请日：2007-02-13

Applicant: Duane Burnett ,  John Clader ,  Wayne Vaccaro

Inventor： Duane Burnett ,  John Clader ,  Wayne Vaccaro

IPC: A61K31/7052 ,  A61K31/506 ,  A61K31/4025 ,  A61K31/397

CPC classification number: C07D403/12 ,  C07D205/08 ,  Y10S930/28

Abstract: The present invention provides substituted azetidinone compounds, formulations and processes for preparing the same which can be useful for treating vascular conditions such as atherosclerosis or hypercholesterolemia, diabetes, obesity, stroke, demyelination and lowering plasma levels of sterols and/or stanols in a subject.

Abstract translation: 本发明提供取代的氮杂环丁酮化合物，其制备方法及其制备方法，其可用于治疗受试者血管病变如动脉粥样硬化或高胆固醇血症，糖尿病，肥胖症，中风，脱髓鞘和降低血浆中甾醇和/或甾烷醇的水平。

公开(公告)号：US20070155676A1

公开(公告)日：2007-07-05

申请号：US11708449

申请日：2007-02-20

Applicant: Duane Burnett ,  John Clader

Inventor： Duane Burnett ,  John Clader

IPC: A61K31/7052 ,  A61K31/506 ,  A61K31/4709 ,  A61K31/4025 ,  A61K31/4439 ,  A61K31/397 ,  C07D405/14 ,  C07D405/02

CPC classification number: C07D405/12 ,  C07D405/14 ,  Y10S930/28

Abstract: The present invention provides substituted azetidinone compounds, formulations and processes for preparing the same which can be useful for treating vascular conditions such as atherosclerosis or hypercholesterolemia, diabetes, obesity, stroke, demyelination and lowering plasma levels of sterols and/or stanols in a subject.

Abstract translation: 本发明提供取代的氮杂环丁酮化合物，其制备方法及其制备方法，其可用于治疗受试者的血管病症如动脉粥样硬化或高胆固醇血症，糖尿病，肥胖症，中风，脱髓鞘和降低血浆中甾醇和/或甾醇的水平。

公开(公告)号：US20070197581A1

公开(公告)日：2007-08-23

申请号：US11654821

申请日：2007-01-18

Applicant: Theodros Asberom ,  Thomas Bara ,  Chad Bennett ,  Duane Burnett ,  Mary Ann Caplen ,  John Clader ,  David Cole ,  Martin Domalski ,  Hubert Josien ,  Chad Knutson ,  Hongmei Li ,  Mark McBriar ,  Dmitri Pissarnitski ,  Li Qiang ,  Murali Rajagopalan ,  Thavalakulamgara Sasikumar ,  Jing Su ,  Haiqun Tang ,  Wen-Lian Wu ,  Ruo Xu ,  Zhiqiang Zhao

Inventor： Theodros Asberom ,  Thomas Bara ,  Chad Bennett ,  Duane Burnett ,  Mary Ann Caplen ,  John Clader ,  David Cole ,  Martin Domalski ,  Hubert Josien ,  Chad Knutson ,  Hongmei Li ,  Mark McBriar ,  Dmitri Pissarnitski ,  Li Qiang ,  Murali Rajagopalan ,  Thavalakulamgara Sasikumar ,  Jing Su ,  Haiqun Tang ,  Wen-Lian Wu ,  Ruo Xu ,  Zhiqiang Zhao

IPC: A61K31/4741 ,  A61K31/473 ,  A61K31/353 ,  A61K31/19

CPC classification number: C07D311/22 ,  C07C317/14 ,  C07C317/20 ,  C07C317/44 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2602/12 ,  C07D311/80 ,  C07D311/92 ,  C07D311/94 ,  C07D313/08 ,  C07D335/06 ,  C07D405/12 ,  C07D409/12 ,  C07D491/04 ,  C07D493/04

Abstract: This invention discloses novel gamma secretase inhibitors of the formula: R2 and R3, or R2 and R4, or R3 and R4, together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substitutents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.

Abstract translation: 本发明公开了下式的新型γ分泌酶抑制剂：R 2和R 3，或R 2和R 4 O / >或R 3和R 4与它们所连接的原子一起可以形成稠合的环烷基或稠合的杂环烷基环。 环烷基环或杂环烷基环可任选被一个或多个取代基取代。 一种或多种式（I）化合物或包含这些化合物的制剂可以是有用的，例如， 治疗阿尔茨海默病。

公开(公告)号：US08450343B2

公开(公告)日：2013-05-28

申请号：US12746041

申请日：2008-12-04

Applicant: Xianhai Huang ,  Anandan Palani ,  Jun Qin ,  Robert G. Aslanian ,  Zhaoning Zhu ,  William Greenlee ,  Hubert Josien ,  Wei Zhou ,  Xiaohong Zhu ,  Chad E. Bennett ,  Dmitri Pissarnitski ,  Mihirbaran Mandal ,  Pawan Dhondi ,  Troy McCracken ,  Thomas Bara ,  Zhiqiang Zhao ,  Duane Burnett ,  John Clader

Inventor： Xianhai Huang ,  Anandan Palani ,  Jun Qin ,  Robert G. Aslanian ,  Zhaoning Zhu ,  William Greenlee ,  Hubert Josien ,  Wei Zhou ,  Xiaohong Zhu ,  Chad E. Bennett ,  Dmitri Pissarnitski ,  Mihirbaran Mandal ,  Pawan Dhondi ,  Troy McCracken ,  Thomas Bara ,  Zhiqiang Zhao ,  Duane Burnett ,  John Clader

IPC: A01N43/42 ,  A61K31/44 ,  C07D471/02 ,  C07D491/02 ,  C07D498/02 ,  C07D513/02 ,  C07D515/02

CPC classification number: C07D471/04 ,  C07D403/10 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I) wherein R2 is a fused bicyclic ring of the formula (II). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I).

Abstract translation: 本发明提供了作为γ分泌酶调节剂的新型化合物。 所述化合物具有式（I），其中R 2是式（II）的稠合双环。 还公开了使用式（I）的化合物调节γ-分泌酶活性和治疗阿尔茨海默病的方法的方法。

公开(公告)号：US20110015190A1

公开(公告)日：2011-01-20

申请号：US12746041

申请日：2008-12-04

Applicant: Xianhai Huang ,  Anandan Palani ,  Jun Qin ,  Robert Aslanian ,  Zhaoning Zhu ,  William Greenlee ,  Hubert Josien ,  Wei Zhou ,  Xiaohong Zhou ,  Chad E. Bennett ,  Dmitri Pissarnitski ,  Mihirbaran Mandal ,  Pawan Dhondi ,  Troy McCracken ,  Thomas Bara ,  Zhiqiang Zhao ,  Duane Burnett ,  John Clader

Inventor： Xianhai Huang ,  Anandan Palani ,  Jun Qin ,  Robert Aslanian ,  Zhaoning Zhu ,  William Greenlee ,  Hubert Josien ,  Wei Zhou ,  Xiaohong Zhou ,  Chad E. Bennett ,  Dmitri Pissarnitski ,  Mihirbaran Mandal ,  Pawan Dhondi ,  Troy McCracken ,  Thomas Bara ,  Zhiqiang Zhao ,  Duane Burnett ,  John Clader

IPC: A61K31/5383 ,  C07D471/04 ,  A61K31/437 ,  C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  C07D498/04 ,  C07D403/02 ,  A61K31/4178 ,  A61P25/28

CPC classification number: C07D471/04 ,  C07D403/10 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (I) wherein R2 is a fused bicyclic ring of the formula (II). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's disease using the compounds of formula (I).

Abstract translation: 本发明提供了作为γ分泌酶调节剂的新型化合物。 所述化合物具有式（I），其中R 2是式（II）的稠合双环。 还公开了使用式（I）的化合物调节γ-分泌酶活性和治疗阿尔茨海默病的方法的方法。

公开(公告)号：US20070155674A1

公开(公告)日：2007-07-05

申请号：US11705977

申请日：2007-02-13

Applicant: Duane Burnett ,  John Clader

Inventor： Duane Burnett ,  John Clader

IPC: A61K31/7052 ,  A61K31/397 ,  A61K31/695 ,  C07H17/02 ,  C07D205/02

CPC classification number: C07D403/12 ,  C07D205/08 ,  Y10S930/28

Abstract: The present invention provides substituted azetidinone compounds, formulations and processes for preparing the same which can be useful for treating vascular conditions such as atherosclerosis or hypercholesterolemia, diabetes, obesity, stroke, demyelination and lowering plasma levels of sterols and/or stanols in a subject.

公开(公告)号：US20080076751A1

公开(公告)日：2008-03-27

申请号：US11854754

申请日：2007-09-13

Applicant: Robert Aslanian ,  Chad Bennett ,  Duane Burnett ,  Tin-Yau Chan ,  Eugenia Kiselgof ,  Chad Knutson ,  Joel Harris ,  Brian McKittrick ,  Anandan Palani ,  Elizabeth Smith ,  Henry Vaccaro ,  Dong Xiao ,  Hyunjin Kim

Inventor： Robert Aslanian ,  Chad Bennett ,  Duane Burnett ,  Tin-Yau Chan ,  Eugenia Kiselgof ,  Chad Knutson ,  Joel Harris ,  Brian McKittrick ,  Anandan Palani ,  Elizabeth Smith ,  Henry Vaccaro ,  Dong Xiao ,  Hyunjin Kim

IPC: A61K31/397 ,  A61P25/04 ,  A61P3/00 ,  C07D471/10

CPC classification number: C07D471/10

Abstract: The present invention relates to Azetidinone Derivatives, compositions comprising an Azetidinone Derivative and methods for treating or preventing a disorder of lipid metabolism, pain, diabetes, a vascular condition, demyelination or nonalcoholic fatty liver disease, comprising administering to a patient an effective amount of an Azetidinone Derivative.

Abstract translation: 本发明涉及氮杂环丁酮衍生物，包含氮杂环丁酮衍生物的组合物和用于治疗或预防脂质代谢紊乱，疼痛，糖尿病，血管病症，脱髓鞘或非酒精性脂肪性肝病的方法，包括向患者施用有效量的 氮杂环丁酮衍生物。

公开(公告)号：US20050049269A1

公开(公告)日：2005-03-03

申请号：US10924070

申请日：2004-08-23

Applicant: Wen-Lian Wu ,  Duane Burnett ,  Mary Ann Caplen

Inventor： Wen-Lian Wu ,  Duane Burnett ,  Mary Ann Caplen

IPC: A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  C07D401/06 ,  C07D401/14 ,  C07D417/14 ,  A61K31/4747 ,  A61K31/454 ,  C07D43/02

CPC classification number: C07D401/06 ,  C07D401/14 ,  C07D417/14

Abstract: The present invention discloses compounds of formula I wherein Ar, X, R1 and R11 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.

Abstract translation: 本发明公开了其中Ar，X，R 1和R 11在本文中定义的式I化合物，所述化合物是用于黑色素浓缩激素（MCH）的新型拮抗剂，以及制备此类化合物的方法。 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。

公开(公告)号：US20070072864A1

公开(公告)日：2007-03-29

申请号：US11505140

申请日：2006-08-16

Applicant: Chad Bennett ,  William Greenlee ,  Chad Knutson ,  Duane Burnett

Inventor： Chad Bennett ,  William Greenlee ,  Chad Knutson ,  Duane Burnett

IPC: C07D487/22 ,  A61K31/503

CPC classification number: C07D487/22 ,  C07D495/14

Abstract: In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J3, X, Z, and R1, R3, and R4 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.

Abstract translation: 在其许多实施方案中，本发明提供了式I的三环化合物（其中J 1，X 3，X 3，Z和R 1） ，R 3和R 4如本文所定义），其用作代谢型谷氨酸受体（mGluR）拮抗剂，特别是作为选择性代谢型谷氨酸受体1拮抗剂，含有化合物的药物组合物 以及使用化合物和组合物治疗与代谢型谷氨酸受体（例如，mGluR1）相关的疾病例如疼痛，偏头痛，焦虑症，尿失禁和神经变性疾病如阿尔茨海默病的治疗方法。

公开(公告)号：US20060167029A1

公开(公告)日：2006-07-27

申请号：US11301672

申请日：2005-12-13

Applicant: Julius Matasi ,  Deen Tulshian ,  Duane Burnett ,  Wen-Lian Wu ,  Peter Korakas ,  Lisa Silverman ,  Thavalakulamgara Sasikumar ,  Li Qiang ,  Martin Domalski

Inventor： Julius Matasi ,  Deen Tulshian ,  Duane Burnett ,  Wen-Lian Wu ,  Peter Korakas ,  Lisa Silverman ,  Thavalakulamgara Sasikumar ,  Li Qiang ,  Martin Domalski

IPC: A61K31/519 ,  C07D498/22

CPC classification number: C07D495/14

Abstract: In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1-R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.

Abstract translation: 在其许多实施方案中，本发明提供式I的三环化合物（其中J 1，X 4和X 1，R 2，R 2， 可用作代谢型谷氨酸受体（mGluR）拮抗剂，特别是作为选择性代谢型谷氨酸受体1拮抗剂的药物组合物，以及使用该化合物和组合物治疗疾病的治疗方法 与代谢型谷氨酸受体（例如，mGluR1）相关，例如疼痛，偏头痛，焦虑症，尿失禁和神经变性疾病如阿尔茨海默氏病。