公开(公告)号：US08598202B2

公开(公告)日：2013-12-03

申请号：US12378734

申请日：2009-02-18

Applicant: Richard Apodaca ,  J. Guy Breitenbucher ,  Alison L. Chambers ,  Xiaohu Deng ,  Natalie A. Hawryluk ,  John M. Keith ,  Neelakandha S. Mani ,  Jeffrey E. Merit ,  Joan M. Pierce ,  Mark Seierstad ,  Wei Xiao

Inventor： Richard Apodaca ,  J. Guy Breitenbucher ,  Alison L. Chambers ,  Xiaohu Deng ,  Natalie A. Hawryluk ,  John M. Keith ,  Neelakandha S. Mani ,  Jeffrey E. Merit ,  Joan M. Pierce ,  Mark Seierstad ,  Wei Xiao

IPC: A01N43/54 ,  A61K31/505

CPC classification number: C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D251/22 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/12

Abstract: Certain aryl-hydroxyethylamino-pyrimidine and triazine compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). Methods of synthesizing such compounds are also disclosed.

Abstract translation: 描述了某些芳基 - 羟乙基氨基 - 嘧啶和三嗪化合物，其可用作FAAH抑制剂。 这些化合物可用于治疗由脂肪酰胺水解酶（FAAH）活性介导的疾病状态，病症和病症的药物组合物和方法，例如焦虑症，疼痛，炎症，睡眠障碍，进食障碍，能量代谢紊乱， 和运动障碍（例如多发性硬化）。 还公开了合成这些化合物的方法。

公开(公告)号：US08183239B2

公开(公告)日：2012-05-22

申请号：US11553556

申请日：2006-10-27

Applicant: Pascal Bonaventure ,  Nicholas I. Carruthers ,  Wenying Chai ,  Curt A. Dvorak ,  Jill A. Jablonowski ,  Dale A. Rudolph ,  Mark Seierstad ,  Chandravadan R. Shah ,  Devin M. Swanson ,  Victoria D. Wong

Inventor： Pascal Bonaventure ,  Nicholas I. Carruthers ,  Wenying Chai ,  Curt A. Dvorak ,  Jill A. Jablonowski ,  Dale A. Rudolph ,  Mark Seierstad ,  Chandravadan R. Shah ,  Devin M. Swanson ,  Victoria D. Wong

IPC: A61K31/495 ,  A61K31/496 ,  A61K31/5377 ,  C07D211/34 ,  C07D211/58 ,  C07D213/56 ,  C07D295/15 ,  C07D401/04 ,  A61K31/451 ,  A61K31/454 ,  C07D401/12 ,  C07D417/12

CPC classification number: C07D295/15 ,  C07D205/04 ,  C07D207/06 ,  C07D207/08 ,  C07D207/10 ,  C07D207/27 ,  C07D207/34 ,  C07D211/14 ,  C07D211/16 ,  C07D211/22 ,  C07D211/34 ,  C07D211/38 ,  C07D211/58 ,  C07D211/70 ,  C07D213/55 ,  C07D213/56 ,  C07D213/74 ,  C07D213/81 ,  C07D213/82 ,  C07D231/14 ,  C07D237/20 ,  C07D239/28 ,  C07D239/48 ,  C07D241/04 ,  C07D261/08 ,  C07D261/14 ,  C07D285/01 ,  C07D295/135 ,  C07D295/155 ,  C07D295/185 ,  C07D307/24 ,  C07D307/52 ,  C07D307/68 ,  C07D333/38 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D487/08

Abstract: The invention provides novel non-peptidic NPY Y2 receptor inhibitors useful in treating or preventing: anxiolytic disorders or depression; injured mammalian nerve tissue; conditions responsive to treatment through administration of a neurotrophic factor; neurological disorders; bone loss; substance related disorders; sleep/wake disorders; cardiovascular disease; obesity; or an obesity-related disorder. Compounds of the invention are also useful in modulating endocrine functions, particularly endocrine functions controlled by the pituitary and hypothalamic glands, and are therefore useful in the treatment or prevention of inovulation and infertility. The compounds of the present invention are of the formula where Ring T is a heterocycloalkyl ring selected from the group consisting of:

Abstract translation: 本发明提供了用于治疗或预防：抗焦虑障碍或抑郁症的新型非肽性NPY Y2受体抑制剂; 受伤的哺乳动物神经组织; 通过施用神经营养因子治疗反应的病症; 神经系统疾病; 骨质疏松 物质相关疾病; 睡眠/觉醒障碍 心血管疾病; 肥胖; 或肥胖相关疾病。 本发明的化合物还可用于调节内分泌功能，特别是由垂体和下丘脑腺体控制的内分泌功能，因此可用于治疗或预防排卵和不育症。 本发明的化合物具有下式：其中环T是选自以下的杂环烷基环：

公开(公告)号：US20050070534A1

公开(公告)日：2005-03-31

申请号：US10949055

申请日：2004-09-24

Applicant: Nicholas Carruthers ,  Wenying Chai ,  Scott Dax ,  Jill Jablonowski ,  Xiaobing Li ,  Timothy Lovenberg ,  William Murray ,  Dale Rudolph ,  Mark Seierstad ,  Mark Youngman

Inventor： Nicholas Carruthers ,  Wenying Chai ,  Scott Dax ,  Jill Jablonowski ,  Xiaobing Li ,  Timothy Lovenberg ,  William Murray ,  Dale Rudolph ,  Mark Seierstad ,  Mark Youngman

IPC: A61K31/404 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/497 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/541 ,  A61P3/04 ,  A61P15/08 ,  A61P25/22 ,  A61P25/24 ,  C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D413/02 ,  C07D417/02 ,  C07D473/02 ,  C07D43/02

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D409/14

Abstract: The invention provides novel non-peptidic NPY Y2 receptor inhibitors useful in treating or preventing: anxiolytic disorders or depression; injured mammalian nerve tissue; conditions responsive to treatment through administration of a neurotrophic factor; neurological disorders; bone loss; substance related disorders; obesity; or an obesity-related disorder. Compounds of the invention are also useful in modulating endocrine functions, particularly endocrine functions controlled by the pituitary and hypothalamic glands, and are therefore useful in the treatment or prevention of inovulation and infertility.

Abstract translation: 本发明提供了用于治疗或预防：抗焦虑障碍或抑郁症的新型非肽性NPY Y2受体抑制剂; 受伤的哺乳动物神经组织; 通过施用神经营养因子治疗反应的病症; 神经系统疾病; 骨质疏松 物质相关疾病; 肥胖; 或肥胖相关疾病。 本发明的化合物还可用于调节内分泌功能，特别是由垂体和下丘脑腺体控制的内分泌功能，因此可用于治疗或预防排卵和不育症。

公开(公告)号：US08906914B2

公开(公告)日：2014-12-09

申请号：US13390984

申请日：2010-08-17

Applicant: Natalie A. Hawryluk ,  J. Guy Breitenbucher ,  William M. Jones ,  Alison L. Chambers ,  John M. Keith ,  Mark Seierstad

Inventor： Natalie A. Hawryluk ,  J. Guy Breitenbucher ,  William M. Jones ,  Alison L. Chambers ,  John M. Keith ,  Mark Seierstad

IPC: C07D239/42 ,  C07D403/12 ,  A61K31/506 ,  C07D417/12 ,  C07D413/04 ,  C07D409/12 ,  C07D409/04 ,  C07D401/04 ,  C07D413/12 ,  C07D405/12 ,  C07D405/04

CPC classification number: C07D239/42 ,  C07D401/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12

Abstract: Certain ethylene diamine compounds of Formula (I) are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). Methods of synthesizing such compounds are also disclosed.

Abstract translation: 描述了某些式（I）的乙二胺化合物，其可用作FAAH抑制剂。 这些化合物可用于治疗由脂肪酰胺水解酶（FAAH）活性介导的疾病状态，病症和病症的药物组合物和方法，例如焦虑症，疼痛，炎症，睡眠障碍，进食障碍，能量代谢紊乱， 和运动障碍（例如多发性硬化）。 还公开了合成这些化合物的方法。

公开(公告)号：US07598249B2

公开(公告)日：2009-10-06

申请号：US11321710

申请日：2005-12-29

Applicant: Richard Apodaca ,  J. Guy Breitenbucher ,  Kanaka Pattabiraman ,  Mark Seierstad ,  Wei Xiao

Inventor： Richard Apodaca ,  J. Guy Breitenbucher ,  Kanaka Pattabiraman ,  Mark Seierstad ,  Wei Xiao

IPC: A61K31/497 ,  A61K31/445 ,  A01N43/40 ,  C07D241/04 ,  C07D211/00 ,  C07D295/00

CPC classification number: C07D295/195 ,  C07D207/335 ,  C07D209/08 ,  C07D209/14 ,  C07D209/82 ,  C07D211/16 ,  C07D213/38 ,  C07D213/56 ,  C07D213/61 ,  C07D213/75 ,  C07D215/12 ,  C07D215/18 ,  C07D239/42 ,  C07D241/42 ,  C07D295/20 ,  C07D295/215 ,  C07D307/79 ,  C07D307/81 ,  C07D317/46 ,  C07D317/58 ,  C07D319/16 ,  C07D319/18 ,  C07D333/58 ,  C07D333/60 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12

Abstract: Certain piperazinyl and piperidinyl urea compounds are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).

Abstract translation: 某些哌嗪基和哌啶基脲化合物可用作FAAH抑制剂。 此类化合物可用于治疗由脂肪酰胺水解酶（FAAH）活性介导的疾病状态，病症和病症的药物组合物和方法。 因此，可以施用化合物以治疗例如焦虑，疼痛，炎症，睡眠障碍，进食障碍或运动障碍（例如多发性硬化症）。

公开(公告)号：US08530476B2

公开(公告)日：2013-09-10

申请号：US12557650

申请日：2009-09-11

Applicant: Richard Apodaca ,  J. Guy Breitenbucher ,  Kanaka Pattabiraman ,  Mark Seierstad ,  Wei Xiao

Inventor： Richard Apodaca ,  J. Guy Breitenbucher ,  Kanaka Pattabiraman ,  Mark Seierstad ,  Wei Xiao

IPC: A61K31/497 ,  C07D403/00 ,  C07D405/06 ,  C07D401/06

CPC classification number: C07D295/195 ,  C07D207/335 ,  C07D209/08 ,  C07D209/14 ,  C07D209/82 ,  C07D211/16 ,  C07D213/38 ,  C07D213/56 ,  C07D213/61 ,  C07D213/75 ,  C07D215/12 ,  C07D215/18 ,  C07D239/42 ,  C07D241/42 ,  C07D295/20 ,  C07D295/215 ,  C07D307/79 ,  C07D307/81 ,  C07D317/46 ,  C07D317/58 ,  C07D319/16 ,  C07D319/18 ,  C07D333/58 ,  C07D333/60 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12

Abstract: Certain piperazinyl and piperidinyl urea compounds are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).

公开(公告)号：US20090264429A1

公开(公告)日：2009-10-22

申请号：US12378734

申请日：2009-02-18

Applicant: Richard Apodaca ,  J. Guy Breitenbucher ,  Alison L. Chambers ,  Xiaohu Deng ,  Natalie A. Hawryluk ,  John M. Keith ,  Neelakandha S. Mani ,  Jeffrey E. Merit ,  Joan M. Pierce ,  Mark Seierstad ,  Wei Xiao

Inventor： Richard Apodaca ,  J. Guy Breitenbucher ,  Alison L. Chambers ,  Xiaohu Deng ,  Natalie A. Hawryluk ,  John M. Keith ,  Neelakandha S. Mani ,  Jeffrey E. Merit ,  Joan M. Pierce ,  Mark Seierstad ,  Wei Xiao

IPC: A61K31/5377 ,  A61K31/505 ,  C07D413/14 ,  C07D239/42

CPC classification number: C07D239/42 ,  C07D239/47 ,  C07D239/48 ,  C07D251/22 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/12

Abstract: Certain aryl-hydroxyethylamino-pyrimidine and triazine compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis). Methods of synthesizing such compounds are also disclosed.

Abstract translation: 描述了某些芳基 - 羟乙基氨基 - 嘧啶和三嗪化合物，其可用作FAAH抑制剂。 这些化合物可用于治疗由脂肪酰胺水解酶（FAAH）活性介导的疾病状态，病症和病症的药物组合物和方法，例如焦虑症，疼痛，炎症，睡眠障碍，进食障碍，能量代谢紊乱， 和运动障碍（例如多发性硬化）。 还公开了合成这些化合物的方法。

公开(公告)号：US20080132540A1

公开(公告)日：2008-06-05

申请号：US11942387

申请日：2007-11-19

Applicant: Nicholas I. Carruthers ,  Wenying Chai ,  Scott L. Dax ,  Jill A. Jablonowski ,  Xiaobing Li ,  Timothy W. Lovenberg ,  William V. Murray ,  Dale A. Rudolph ,  Mark Seierstad ,  Mark A. Youngman

Inventor： Nicholas I. Carruthers ,  Wenying Chai ,  Scott L. Dax ,  Jill A. Jablonowski ,  Xiaobing Li ,  Timothy W. Lovenberg ,  William V. Murray ,  Dale A. Rudolph ,  Mark Seierstad ,  Mark A. Youngman

IPC: A61K31/4545 ,  A61K31/404 ,  A61P25/24 ,  A61P3/04 ,  A61P25/00 ,  A61K31/454

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D409/14

Abstract: The invention provides novel non-peptidic NPY Y2 receptor inhibitors useful in treating or preventing: anxiolytic disorders or depression; injured mammalian nerve tissue; conditions responsive to treatment through administration of a neurotrophic factor; neurological disorders; bone loss; substance related disorders; obesity; or an obesity-related disorder. Compounds of the invention are also useful in modulating endocrine functions, particularly endocrine functions controlled by the pituitary and hypothalamic glands, and are therefore useful in the treatment or prevention of inovulation and infertility.

Abstract translation: 本发明提供了用于治疗或预防：抗焦虑障碍或抑郁症的新型非肽性NPY Y2受体抑制剂; 受伤的哺乳动物神经组织; 通过施用神经营养因子治疗反应的病症; 神经系统疾病; 骨质疏松 物质相关疾病; 肥胖; 或肥胖相关疾病。 本发明的化合物还可用于调节内分泌功能，特别是由垂体和下丘脑腺体控制的内分泌功能，因此可用于治疗或预防排卵和不育症。

公开(公告)号：US20100292266A1

公开(公告)日：2010-11-18

申请号：US12227756

申请日：2007-05-25

Applicant: Richard Apodaca ,  James Guy Breitenbucher ,  Alison L. Chambers ,  Mark Seierstad ,  Wei Xiao

Inventor： Richard Apodaca ,  James Guy Breitenbucher ,  Alison L. Chambers ,  Mark Seierstad ,  Wei Xiao

IPC: A61K31/454 ,  C07D413/06 ,  C07D413/14 ,  C07D471/04 ,  A61K31/4545 ,  C07D491/056 ,  A61K31/4709 ,  A61P29/00 ,  A61P25/00 ,  A61P35/00 ,  A61P1/08 ,  A61P1/04

CPC classification number: C07D413/06 ,  C07D413/14 ,  C07D471/04 ,  C07D491/04

Abstract: Certain oxazolyl piperidine compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).

Abstract translation: 描述了某些恶唑基哌啶化合物，其可用作FAAH抑制剂。 此类化合物可用于治疗由脂肪酰胺水解酶（FAAH）活性介导的疾病状态，病症和病症的药物组合物和方法。 因此，可以施用化合物以治疗例如焦虑，疼痛，炎症，睡眠障碍，进食障碍或运动障碍（例如多发性硬化症）。

公开(公告)号：US20090111778A1

公开(公告)日：2009-04-30

申请号：US12094139

申请日：2006-11-17

Applicant: Richard Apodaca ,  J. Guy Breitenbucher ,  Matthew T. Epperson ,  Amy K. Fried ,  Daniel J. Pippel ,  Mark Seierstad

Inventor： Richard Apodaca ,  J. Guy Breitenbucher ,  Matthew T. Epperson ,  Amy K. Fried ,  Daniel J. Pippel ,  Mark Seierstad

IPC: A61K31/60 ,  A61K31/195 ,  A61K31/167 ,  A61K31/192 ,  A61K31/135 ,  C07D413/14 ,  A61K31/4545 ,  C07D413/06 ,  A61K31/454 ,  A61K31/498 ,  A61K31/5377 ,  A61P29/00 ,  A61P25/00 ,  A61P3/00 ,  A61P15/00 ,  A61P27/00 ,  A61P37/00 ,  A61P9/00

CPC classification number: C07D413/04 ,  C07D263/32 ,  C07D263/34 ,  C07D413/12 ,  C07D413/14

Abstract: Certain 2-keto-oxazole compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).

Abstract translation: 描述了某些2-酮 - 恶唑化合物，其可用作FAAH抑制剂。 此类化合物可用于治疗由脂肪酰胺水解酶（FAAH）活性介导的疾病状态，病症和病症的药物组合物和方法。 因此，可以施用化合物以治疗例如焦虑，疼痛，炎症，睡眠障碍，进食障碍或运动障碍（例如多发性硬化症）。