公开(公告)号：US20070249616A1

公开(公告)日：2007-10-25

申请号：US11763926

申请日：2007-06-15

Applicant: Alan Hutchison ,  Bertrand Chenard ,  James Tarrant ,  Guiying Li ,  Manuka Ghosh ,  George Luke ,  John Peterson ,  Wallace Pringle ,  Mary-Margaret O'Donnell ,  Kyungae Lee ,  Linda Gustavson ,  Dario Doller

Inventor： Alan Hutchison ,  Bertrand Chenard ,  James Tarrant ,  Guiying Li ,  Manuka Ghosh ,  George Luke ,  John Peterson ,  Wallace Pringle ,  Mary-Margaret O'Donnell ,  Kyungae Lee ,  Linda Gustavson ,  Dario Doller

IPC: A61K31/496 ,  A61K31/498 ,  A61P3/04

CPC classification number: C07D213/74 ,  C07D213/82 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08

Abstract: Compounds of Formula I are provided, in which variables are as described herein: Such compounds may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).

Abstract translation: 提供了式I化合物，其中变量如本文所述：这样的化合物可用于在体内或体外调节MCH与MCH受体的结合，并且特别可用于治疗各种代谢，进食和性障碍 在人类，驯养的伴侣动物和家畜中。 还提供了用于治疗这种病症的药物组合物和方法，以及使用这些配体检测MCH受体的方法（例如受体定位研究）。

公开(公告)号：US06656941B2

公开(公告)日：2003-12-02

申请号：US09947702

申请日：2001-09-06

Applicant: George Maynard ,  Pamela Albaugh ,  Stanislaw Rachwal ,  Linda Gustavson

Inventor： George Maynard ,  Pamela Albaugh ,  Stanislaw Rachwal ,  Linda Gustavson

IPC: A61K3150

CPC classification number: C07D231/56 ,  C07D401/12 ,  G01N2333/70571

Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein the variables R1, R2, R3, n, and Ar are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.

Abstract translation: 公开了下式的化合物及其药学上可接受的盐，其中变量R1，R2，R3，n和Ar如本文所定义。 这些化合物是GABAA脑受体的高度选择性激动剂，拮抗剂或反向激动剂或GABAA脑受体的激动剂，拮抗剂或反向激动剂的前药，因此可用于诊断和治疗焦虑症，抑郁症，唐氏综合症，睡眠和癫痫发作障碍， 过量与苯二氮卓类药物和增强记忆。

公开(公告)号：US20070053980A1

公开(公告)日：2007-03-08

申请号：US11592694

申请日：2006-11-03

Applicant: Francisco Alvarez ,  Kathleen Apfelbaum ,  David Brown ,  Linda Gustavson ,  Russell Slade

Inventor： Francisco Alvarez ,  Kathleen Apfelbaum ,  David Brown ,  Linda Gustavson ,  Russell Slade

IPC: A61K9/22

CPC classification number: A61K9/1617 ,  A61K9/2031 ,  A61K9/2054 ,  A61K31/4535

Abstract: Extended release tiagabine formulations that demonstrate fewer side-effects when administered to a patient.

Abstract translation: 延长释放的噻加滨制剂，在给予患者时表现出较少的副作用。

公开(公告)号：US20060280790A1

公开(公告)日：2006-12-14

申请号：US11399964

申请日：2006-04-07

Applicant: Tzuchi Ju ,  Claudia Davila ,  Yi Gao ,  Linda Gustavson ,  David LeBlond ,  Tong Zhu

Inventor： Tzuchi Ju ,  Claudia Davila ,  Yi Gao ,  Linda Gustavson ,  David LeBlond ,  Tong Zhu

IPC: A61K31/192 ,  A61K9/20

CPC classification number: A61K9/5026 ,  A61K9/0004 ,  A61K9/1623 ,  A61K9/1635 ,  A61K9/1652 ,  A61K9/2054 ,  A61K9/2077 ,  A61K9/2846 ,  A61K9/2866 ,  A61K9/4808 ,  A61K31/192

Abstract: The present invention relates to oral formulations comprising an active agent comprising at least one of 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid, salts of 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid or buffered 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid.

公开(公告)号：US20060142301A1

公开(公告)日：2006-06-29

申请号：US11100355

申请日：2005-04-06

Applicant: Alan Hutchison ,  Bertrand Chenard ,  James Tarrant ,  Guiying Li ,  Manuka Ghosh ,  George Luke ,  John Peterson ,  Wallace Pringle ,  Mary-Margaret O'Donnell ,  Kyungae Lee ,  Linda Gustavson ,  Dario Doller

Inventor： Alan Hutchison ,  Bertrand Chenard ,  James Tarrant ,  Guiying Li ,  Manuka Ghosh ,  George Luke ,  John Peterson ,  Wallace Pringle ,  Mary-Margaret O'Donnell ,  Kyungae Lee ,  Linda Gustavson ,  Dario Doller

IPC: A61K31/496 ,  A61K31/497 ,  C07D403/02

CPC classification number: C07D213/74 ,  C07D213/82 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08

Abstract: Compounds of Formula I are provided, in which variables are as described herein: Such compounds may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).

Abstract translation: 提供了式I化合物，其中变量如本文所述：这样的化合物可用于在体内或体外调节MCH与MCH受体的结合，并且特别可用于治疗各种代谢，进食和性障碍 在人类，驯养的伴侣动物和家畜中。 还提供了用于治疗这种病症的药物组合物和方法，以及使用这些配体检测MCH受体的方法（例如受体定位研究）。

公开(公告)号：US06906075B2

公开(公告)日：2005-06-14

申请号：US10339111

申请日：2003-01-09

Applicant: Robert W. DeSimone ,  Cheryl Steenstra ,  Linda Gustavson ,  Rajagopal Bakthavatchalam ,  Alan Hutchison

Inventor： Robert W. DeSimone ,  Cheryl Steenstra ,  Linda Gustavson ,  Rajagopal Bakthavatchalam ,  Alan Hutchison

IPC: A61K31/4184 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/55 ,  A61P1/14 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P15/00 ,  A61P43/00 ,  C07D235/10 ,  C07D235/14 ,  C07D401/04 ,  C07D403/04 ,  C07D403/10 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D471/04 ,  C07D513/04 ,  C07D521/00 ,  C07D401/10 ,  A61K31/445 ,  A61K31/495

CPC classification number: C07D231/12 ,  C07D233/56 ,  C07D235/14 ,  C07D249/08 ,  C07D401/04 ,  C07D403/04 ,  C07D403/10 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D513/04

Abstract: Melanin concentrating hormone receptor ligands (especially substituted benzoimidazole analogues), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).

Abstract translation: 提供能够调节MCH受体活性的黑色素浓缩激素受体配体（特别是取代的苯并咪唑类似物）。 这样的配体可用于在体内或体外调节MCH与MCH受体的结合，并且特别可用于治疗人，驯养的伴侣动物和家畜中的各种代谢，喂养和性障碍。 还提供了用于治疗这种病症的药物组合物和方法，以及使用这些配体检测MCH受体的方法（例如受体定位研究）。

公开(公告)号：US20050065162A1

公开(公告)日：2005-03-24

申请号：US10152189

申请日：2002-05-21

Applicant: Alan Hutchison ,  Linda Gustavson ,  John Peterson ,  Dario Doller ,  Timothy Caldwell ,  Taeyoung Yoon ,  Wallace Pringle ,  Yiping Shen ,  Cheryl Steenstra ,  Helen Yin ,  Xiao-shu He

Inventor： Alan Hutchison ,  Linda Gustavson ,  John Peterson ,  Dario Doller ,  Timothy Caldwell ,  Taeyoung Yoon ,  Wallace Pringle ,  Yiping Shen ,  Cheryl Steenstra ,  Helen Yin ,  Xiao-shu He

IPC: G01N33/53 ,  A61K31/352 ,  A61K31/451 ,  A61K31/495 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/551 ,  A61P3/04 ,  A61P3/10 ,  A61P9/00 ,  A61P15/00 ,  A61P25/00 ,  A61P43/00 ,  C07D209/86 ,  C07D211/44 ,  C07D211/52 ,  C07D213/64 ,  C07D213/74 ,  C07D215/12 ,  C07D215/20 ,  C07D223/04 ,  C07D239/47 ,  C07D243/08 ,  C07D295/08 ,  C07D295/096 ,  C07D295/108 ,  C07D295/18 ,  C07D311/18 ,  C07D311/58 ,  C07D317/58 ,  C07D401/12 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08 ,  C07D513/04 ,  G01N33/566 ,  C07D43/14

CPC classification number: C07D513/04 ,  C07D209/86 ,  C07D211/52 ,  C07D213/64 ,  C07D213/74 ,  C07D215/12 ,  C07D215/20 ,  C07D243/08 ,  C07D295/096 ,  C07D295/108 ,  C07D311/18 ,  C07D317/58 ,  C07D401/12 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08

Abstract: Melanin concentrating hormone receptor ligands (especially 1-benzyl-4-aryl-piperazines, 1-benzyl-4-aryl-piperidines and related compounds), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).

Abstract translation: 提供能够调节MCH受体活性的黑色素浓缩激素受体配体（特别是1-苄基-4-芳基哌嗪，1-苄基-4-芳基哌啶和相关化合物）。 这样的配体可用于在体内或体外调节MCH与MCH受体的结合，并且特别可用于治疗人，驯养的伴侣动物和家畜中的各种代谢，喂养和性障碍。 还提供了用于治疗这种病症的药物组合物和方法，以及使用这些配体检测MCH受体的方法（例如受体定位研究）。

公开(公告)号：US20070185199A1

公开(公告)日：2007-08-09

申请号：US11548960

申请日：2006-10-12

Applicant: Tzuchi Ju ,  Claudia Davila ,  Yi Gao ,  Linda Gustavson ,  David LeBlond ,  Tong Zhu

Inventor： Tzuchi Ju ,  Claudia Davila ,  Yi Gao ,  Linda Gustavson ,  David LeBlond ,  Tong Zhu

IPC: A61K31/222

CPC classification number: A61K9/2077 ,  A61K9/1635 ,  A61K9/1652 ,  A61K9/2846 ,  A61K9/2866 ,  A61K31/192

Abstract: The present invention relates to oral formulations comprising an active agent comprising at least one of 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid, salts of 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid or buffered 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid.

Abstract translation: 本发明涉及包含含有2- [4-（4-氯苯甲酰基）苯氧基] -2-甲基 - 丙酸中的至少一种的活性剂，2- [4-（4-氯苯甲酰基）苯氧基] -2-甲基 - 丙酸或缓冲的2- [4-（4-氯苯甲酰基）苯氧基] -2-甲基 - 丙酸。

公开(公告)号：US20070148234A1

公开(公告)日：2007-06-28

申请号：US11548982

申请日：2006-10-12

Applicant: Tzuchi Ju ,  Claudia Davila ,  Kevin Engh ,  Yi Gao ,  Linda Gustavson ,  Shyamala Jayaraman ,  David LeBlond ,  Dennis Lee ,  Tong Zhu

Inventor： Tzuchi Ju ,  Claudia Davila ,  Kevin Engh ,  Yi Gao ,  Linda Gustavson ,  Shyamala Jayaraman ,  David LeBlond ,  Dennis Lee ,  Tong Zhu

IPC: A61K9/20 ,  A61K31/192

CPC classification number: A61K9/2866 ,  A61K9/1623 ,  A61K9/1635 ,  A61K9/1652 ,  A61K9/2077 ,  A61K9/2846 ,  A61K31/192

Abstract: The present invention relates to oral formulations comprising an active agent comprising at least one of 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid, salts of 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid or buffered 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid.

公开(公告)号：US20060229298A1

公开(公告)日：2006-10-12

申请号：US11436099

申请日：2006-05-17

Applicant: Alan Hutchison ,  Linda Gustavson ,  John Peterson ,  Dario Dollar ,  Timothy Caldwell ,  Taeyoung Yoon ,  Wallace Pringle ,  Rajagopal Bakthavatchalam ,  Yiping Shen ,  Cheryl Steenstra ,  Helen Yin ,  Robert DeSimone ,  Xiao-shu He

Inventor： Alan Hutchison ,  Linda Gustavson ,  John Peterson ,  Dario Dollar ,  Timothy Caldwell ,  Taeyoung Yoon ,  Wallace Pringle ,  Rajagopal Bakthavatchalam ,  Yiping Shen ,  Cheryl Steenstra ,  Helen Yin ,  Robert DeSimone ,  Xiao-shu He

IPC: A61K31/496 ,  A61K31/551 ,  A61K31/495 ,  C07D403/02

CPC classification number: C07D513/04 ,  C07D209/86 ,  C07D211/52 ,  C07D213/64 ,  C07D213/74 ,  C07D215/12 ,  C07D215/20 ,  C07D243/08 ,  C07D295/096 ,  C07D295/108 ,  C07D311/18 ,  C07D317/58 ,  C07D401/12 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08

Abstract: Melanin concentrating hormone receptor ligands (especially 1-benzyl-4-aryl-piperazines, 1-benzyl-4-aryl-piperidines and related compounds), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).