公开(公告)号：WO2011139951A1

公开(公告)日：2011-11-10

申请号：PCT/US2011/034755

申请日：2011-05-02

Applicant: JANSSEN PHARMACEUTICA NV ,  KEITH, John, M. ,  LIU, Jing

Inventor： KEITH, John, M. ,  LIU, Jing

IPC: C07D405/12 ,  A61K31/496 ,  A61P25/16 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P29/00 ,  A61P35/00 ,  A61P37/06 ,  A61P19/10 ,  A61P9/12 ,  A61P15/00 ,  A61P3/00 ,  A61P3/10

CPC classification number: C07D405/12

Abstract: 4-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethyl)-piperazine-1 -carboxylic acid (4-chloro-pyridin-3-yl)-amide is described, which is useful as a FAAH modulator. 4-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethyl)-piperazine-1 -carboxylic acid (4-chloro-pyridin-3-yl)-amide 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). A method of synthesizing 4- (2,2-difluoro-benzo[1,3]dioxol-5-ylmethyl)-piperazine-1 -carboxylic acid (4- chloro-pyridin-3-yl)-amide is also disclosed.

Abstract translation: 描述了4-（2,2-二氟 - 苯并[1,3]二氧杂环戊烯-5-基甲基） - 哌嗪-1-甲酸（4-氯 - 吡啶-3-基） - 酰胺，其可用作FAAH 调制器。 4-（2,2-二氟 - 苯并[1,3]二氧杂环戊烯-5-基甲基） - 哌嗪-1-甲酸（4-氯 - 吡啶-3-基） - 酰胺可用于药物组合物和方法 治疗由脂肪酸酰胺水解酶（FAAH）活性（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））介导的疾病状态，病症和状况。 还公开了合成4-（2,2-二氟 - 苯并[1,3]二氧杂环戊烯-5-基甲基） - 哌嗪-1-甲酸（4-氯 - 吡啶-3-基） - 酰胺的方法。

公开(公告)号：WO2008144305A1

公开(公告)日：2008-11-27

申请号：PCT/US2008/063516

申请日：2008-05-13

Applicant: JANSSEN PHARMACEUTICA N.V. ,  KEITH, John M.

Inventor： KEITH, John M.

IPC: C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  A61K31/4725 ,  A61P15/00 ,  A61P25/00

CPC classification number: C07D217/14 ,  C07D401/12 ,  C07D401/14 ,  C07D417/12

Abstract: Certain diaryl-substituted tetrahydroisoquinoline compounds are histamine H 3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H 3 receptor- and/or serotonin-mediated diseases.

Abstract translation: 某些二芳基取代的四氢异喹啉化合物是可用于治疗组胺H3受体和/或血清素介导的疾病的组胺H3受体和/或血清素转运蛋白调节剂。

公开(公告)号：WO2008002818A1

公开(公告)日：2008-01-03

申请号：PCT/US2007/071739

申请日：2007-06-21

Applicant: JANSSEN PHARMACEUTICA N.V. ,  ALLISON, Brett ,  CARRUTHERS, Nicholas I. ,  CURTIS, Michael P. ,  KEITH, John M. ,  LETAVIC, Michael A. ,  STOCKING, Emily M.

Inventor： ALLISON, Brett ,  CARRUTHERS, Nicholas I. ,  CURTIS, Michael P. ,  KEITH, John M. ,  LETAVIC, Michael A. ,  STOCKING, Emily M.

IPC: C07D213/64 ,  C07D213/65 ,  C07D295/18 ,  A61K31/551 ,  A61P25/24

CPC classification number: C07D243/08 ,  C07D401/12 ,  C07D413/12

Abstract: Certain substituted aminomethyl benzamide compounds are histamine H 3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H 3 receptor- and/or serotonin-mediated diseases.

Abstract translation: 某些取代的氨基甲基苯甲酰胺化合物是可用于治疗组胺H 3受体和/或5-羟色胺介导的疾病的组胺H 3 N 3受体和/或5-羟色胺转运体调节剂。

公开(公告)号：WO2006138714A3

公开(公告)日：2007-03-15

申请号：PCT/US2006023788

申请日：2006-06-16

Applicant: JANSSEN PHARMACEUTICA NV ,  CARRUTHERS NICHOLAS I ,  KEITH JOHN M ,  LETAVIC MICHAEL A ,  SHAH CHANDRAVADAN R

Inventor： CARRUTHERS NICHOLAS I ,  KEITH JOHN M ,  LETAVIC MICHAEL A ,  SHAH CHANDRAVADAN R

IPC: C07D471/04 ,  A61K31/4745 ,  A61K31/4985 ,  A61K31/52 ,  A61P25/00

CPC classification number: C07D471/04

Abstract: Certain naphthyridine compounds are histamine H 3 receptor and serotonin transporter modulators useful in the treatment of histamine H 3 receptor- and serotonin-medicated diseases.

Abstract translation: 某些萘啶化合物是可用于治疗组胺H 3受体和5-羟色胺药物疾病的组胺H 3 N 3受体和5-羟色胺转运体调节剂。

公开(公告)号：WO2010141809A1

公开(公告)日：2010-12-09

申请号：PCT/US2010/037388

申请日：2010-06-04

Applicant: JANSSEN PHARMACEUTICA NV ,  BREITENBUCHER, Guy, J. ,  TICHENOR, Mark, S. ,  MERIT, Jeffrey, E. ,  HAWRYLUK, Natalie, A. ,  CHAMBERS, Alison, L. ,  KEITH, John, M.

Inventor： BREITENBUCHER, Guy, J. ,  TICHENOR, Mark, S. ,  MERIT, Jeffrey, E. ,  HAWRYLUK, Natalie, A. ,  CHAMBERS, Alison, L. ,  KEITH, John, M.

IPC: C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/437 ,  A61K31/4427 ,  A61K31/4439 ,  A61K31/4725 ,  A61K31/5025 ,  A61P25/28 ,  A61P29/00 ,  A61P35/00

CPC classification number: C07D487/04 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D471/04

Abstract: Certain aryl-substituted heterocyclic urea 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).

Abstract translation: 描述了某些芳基取代的杂环脲化合物，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）。

公开(公告)号：WO2010068452A1

公开(公告)日：2010-06-17

申请号：PCT/US2009/065752

申请日：2009-11-24

Applicant: JANSSEN PHARMACEUTICA NV ,  BREITENBUCHER, J., Guy ,  KEITH, John, M. ,  TICHENOR, Mark, S. ,  CHAMBERS, Alison, L. ,  JONES, William, M. ,  HAWRYLUK, Natalie, A. ,  TIMMONS, Amy, K. ,  MERIT, Jeffrey, E. ,  SEIERSTAD, Mark, J.

Inventor： BREITENBUCHER, J., Guy ,  KEITH, John, M. ,  TICHENOR, Mark, S. ,  CHAMBERS, Alison, L. ,  JONES, William, M. ,  HAWRYLUK, Natalie, A. ,  TIMMONS, Amy, K. ,  MERIT, Jeffrey, E. ,  SEIERSTAD, Mark, J.

IPC: C07D401/12 ,  C07D471/04 ,  A61K31/47 ,  A61P29/00

CPC classification number: C07D498/04 ,  A61K31/437 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/5025 ,  A61K31/506 ,  A61K45/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04

Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl urea 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, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).

Abstract translation: 描述了某些杂芳基取代的哌啶基和哌嗪基脲化合物，其可用作FAAH抑制剂。 这些化合物可用于治疗由脂肪酸酰胺水解酶（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，胰岛素抵抗，糖尿病 ，骨质疏松症和运动障碍（例如，多发性硬化症）。

公开(公告)号：WO2009105220A1

公开(公告)日：2009-08-27

申请号：PCT/US2009/001043

申请日：2009-02-18

Applicant: JANSSEN PHARMACEUTICA N.V. ,  APODACA, Richard ,  BREITENBUCHER, J., Guy ,  CHAMBERS, Alison, L. ,  DENG, Xiaohu ,  HAWRYLUK, Natalie, A. ,  KEITH, John, M. ,  MANI, Neelakandha, S. ,  MERIT, Jeffrey, E. ,  PIERCE, Joan, M. ,  SEIERSTAD, Mark ,  XIAO, Wei

Inventor： APODACA, Richard ,  BREITENBUCHER, J., Guy ,  CHAMBERS, Alison, L. ,  DENG, Xiaohu ,  HAWRYLUK, Natalie, A. ,  KEITH, John, M. ,  MANI, Neelakandha, S. ,  MERIT, Jeffrey, E. ,  PIERCE, Joan, M. ,  SEIERSTAD, Mark ,  XIAO, Wei

IPC: A01N43/66 ,  A61K31/53

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：WO2008153752A2

公开(公告)日：2008-12-18

申请号：PCT/US2008006607

申请日：2008-05-23

Applicant: JANSSEN PHARMACEUTICA NV ,  APODACA RICHARD ,  BREITENBUCHER J GUY ,  HAWRYLUK NATALIE A ,  JONES WILLIAM M ,  KEITH JOHN M ,  MERIT JEFFREY E ,  TICHENOR MARK S ,  TIMMONS AMY K

Inventor： APODACA RICHARD ,  BREITENBUCHER J GUY ,  HAWRYLUK NATALIE A ,  JONES WILLIAM M ,  KEITH JOHN M ,  MERIT JEFFREY E ,  TICHENOR MARK S ,  TIMMONS AMY K

IPC: C07D401/00 ,  A61K31/445 ,  A61K31/496 ,  A61K31/501 ,  A61P1/00 ,  C07D403/00 ,  C07D403/14

CPC classification number: C07D231/40 ,  C07D237/20 ,  C07D241/20 ,  C07D257/06 ,  C07D261/14 ,  C07D261/20 ,  C07D271/12 ,  C07D285/14 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04

Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl urea 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, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).

Abstract translation: 描述了某些杂芳基取代的哌啶基和哌嗪基脲化合物，其可用作FAAH抑制剂。 这些化合物可用于治疗由脂肪酸酰胺水解酶（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，胰岛素抵抗，糖尿病 ，骨质疏松症和运动障碍（例如，多发性硬化症）。

公开(公告)号：WO2008064036A1

公开(公告)日：2008-05-29

申请号：PCT/US2007/084657

申请日：2007-11-14

Applicant: JANSSEN PHARMACEUTICA N.V. ,  KEITH, John, M. ,  MILLER, Jennifer, M., B. ,  STOCKING, Emily, M.

Inventor： KEITH, John, M. ,  MILLER, Jennifer, M., B. ,  STOCKING, Emily, M.

IPC: C07D295/12 ,  C07D213/65 ,  A61K31/445

CPC classification number: C07D295/135 ,  C07D213/65

Abstract: Certain substituted phenyl propyl amine compounds are histamine H 3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H 3 receptor- and/or serotonin-mediated diseases.

Abstract translation: 某些取代的苯基丙基胺化合物是可用于治疗组胺H 3受体和/或5-羟色胺介导的疾病的组胺H 3 N 3受体和/或5-羟色胺转运体调节剂。

公开(公告)号：WO2006138714A2

公开(公告)日：2006-12-28

申请号：PCT/US2006/023788

申请日：2006-06-16

Applicant: JANSSEN PHARMACEUTICA N.V. ,  CARRUTHERS, Nicholas, I. ,  KEITH, John, M. ,  LETAVIC, Michael, A. ,  SHAH, Chandravadan, R.

Inventor： CARRUTHERS, Nicholas, I. ,  KEITH, John, M. ,  LETAVIC, Michael, A. ,  SHAH, Chandravadan, R.

CPC classification number: C07D471/04

Abstract: Certain naphthyridine compounds are histamine H 3 receptor and serotonin transporter modulators useful in the treatment of histamine H 3 receptor- and serotonin-medicated diseases.

Abstract translation: 某些萘啶化合物是可用于治疗组胺H 3受体和5-羟色胺药物疾病的组胺H 3 N 3受体和5-羟色胺转运体调节剂。