公开(公告)号：US07241798B2

公开(公告)日：2007-07-10

申请号：US11147602

申请日：2005-06-07

申请人： Barbara E. Segelstein ,  Travis T. Wager ,  Willard M. Welch

发明人： Barbara E. Segelstein ,  Travis T. Wager ,  Willard M. Welch

IPC分类号： C07D209/52 ,  A61K31/403

CPC分类号： C07D209/52 ,  C07D403/12

摘要： The invention is to compounds exhibiting neurokinin inhibitory properties, pharmaceutical compositions comprising same and methods of treatment for neurokinin-mediated conditions.

摘要翻译： 本发明涉及显示神经激肽抑制性质的化合物，包含其的药物组合物和治疗神经激肽介导的病症的方法。

公开(公告)号：US20120157440A1

公开(公告)日：2012-06-21

申请号：US13323883

申请日：2011-12-13

申请人： TODD W. BUTLER ,  Ramalakshmi Y. Chandrasekaran ,  Scot R. Mente ,  Chakrapani Subramanyam ,  Travis T. Wager

发明人： TODD W. BUTLER ,  Ramalakshmi Y. Chandrasekaran ,  Scot R. Mente ,  Chakrapani Subramanyam ,  Travis T. Wager

IPC分类号： A61K31/4355 ,  C07D471/04 ,  A61K31/437 ,  C07D498/04 ,  A61P25/24 ,  A61K31/506 ,  C07D401/04 ,  A61K31/435 ,  A61P25/18 ,  A61P25/00 ,  C07D491/048 ,  A61K31/553

CPC分类号： C07D401/04 ,  C07D471/04 ,  C07D491/048 ,  C07D498/04

摘要： Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, A, R4, n, and R7 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

摘要翻译： 公开了化合物的化合物和药学上可接受的盐，其中所述化合物具有式I的结构及其药学上可接受的盐，其中X，Y，A，R4，n和R7如说明书中所定义。 还公开了相应的药物组合物，治疗方法，合成方法和中间体。

公开(公告)号：US07115600B2

公开(公告)日：2006-10-03

申请号：US11045968

申请日：2005-01-28

申请人： Travis T. Wager ,  Ramalakshmi Y. Chandrasekaran

发明人： Travis T. Wager ,  Ramalakshmi Y. Chandrasekaran

IPC分类号： A61K31/496 ,  A61K31/541 ,  A61K31/4995 ,  C07D241/50 ,  C07D403/10 ,  C07D417/10

CPC分类号： C07D295/096 ,  C07D207/04 ,  C07D207/06 ,  C07D213/30 ,  C07D215/227 ,  C07D231/12 ,  C07D239/26 ,  C07D239/34 ,  C07D271/06 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D471/10 ,  C07D487/04

摘要： This invention is directed to a compound of the formula I as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by modulating histamine H3 receptors, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of depression, mood disorders, schizophrenia, anxiety disorders, Alzheimer's disease, attention-deficit hyperactivity disorder (ADHD), psychotic disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper and hypo motility and acidic secretion of the gastro-intestinal tract, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above.

摘要翻译： 本发明涉及本文定义的式I化合物或其药学上可接受的盐; 含有式I化合物的药物组合物，治疗可以通过调节组胺H3受体治疗的病症或病症的方法，所述方法包括向需要这种治疗的哺乳动物施用如上所述的式I化合物， 以及治疗选自抑郁症，情绪障碍，精神分裂症，焦虑症，阿尔茨海默氏病，注意力缺陷多动障碍（ADHD），精神障碍，睡眠障碍，肥胖，眩晕，癫痫， 过敏反应，过敏引起的气道反应，过敏性鼻炎，鼻充血，过敏充血，充血，低血压，心血管疾病，胃肠道疾病，胃肠道过度运动和运动不足及酸性分泌， 该方法包括向需要这种治疗的哺乳动物施用如上所述的式I化合物。

公开(公告)号：US08178574B2

公开(公告)日：2012-05-15

申请号：US12745982

申请日：2008-12-04

申请人： Travis T. Wager ,  Todd W. Butler

发明人： Travis T. Wager ,  Todd W. Butler

IPC分类号： A61K31/40 ,  C07D207/08 ,  A61P25/00 ,  A61P11/00 ,  A61P37/08 ,  A61P9/00 ,  A61P1/04

CPC分类号： C07D295/073

摘要： The present invention is directed to the tosylate salt of trans-N-isobutyl-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)-phenyl]-cyclobutanecarboxamide Formula (I): to solvates (e.g., hydrates) thereof, to polymorphs thereof, to pharmaceutical compositions thereof and to a method of treating depression, mood disorders, schizophrenia, anxiety disorders, cognitive disorders, Alzheimer's disease, attention-deficit disorder (ADD), attention-deficit hyperactivity disorder (ADHD), psychotic disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper- and hypo-motility and acidic secretion of the gastro-intestinal tract comprising administering a therapeutically effective amount thereof.

摘要翻译： 本发明涉及反式-N-异丁基-3-氟-3- [3-氟-4-（吡咯烷-1-基甲基） - 苯基] - 环丁烷甲酰胺（I）的甲苯磺酸盐：溶剂化 ，水合物），其多晶型物，其药物组合物和治疗抑郁症，情绪障碍，精神分裂症，焦虑症，认知障碍，阿尔茨海默氏病，注意力缺陷障碍（ADD），注意缺陷多动障碍（ADHD） ），精神障碍，睡眠障碍，肥胖，眩晕，癫痫，运动病，呼吸系统疾病，过敏，过敏引起的气道反应，过敏性鼻炎，鼻充血，过敏充血，充血，低血压，心血管疾病，胃肠道疾病， 包括给予治疗有效量的胃肠道的超和不足和酸分泌。

公开(公告)号：US20080176925A1

公开(公告)日：2008-07-24

申请号：US12016521

申请日：2008-01-18

申请人： Todd W. Butler ,  Travis T. Wager

发明人： Todd W. Butler ,  Travis T. Wager

IPC分类号： A61K31/40 ,  A61P25/28 ,  A61P25/24 ,  C07D207/08

CPC分类号： C07D295/155

摘要： The present invention is directed to the tosylate salt of trans-N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)-phenyl]-cyclobutanecarboxamide (1): to solvates (e.g., hydrates) thereof, to polymorphs thereof, to pharmaceutical compositions thereof and to a method of treating depression, mood disorders, schizophrenia, anxiety disorders, cognitive disorders, Alzheimer's disease, attention-deficit disorder (ADD), attention-deficit hyperactivity disorder (ADHD), psychotic disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper- and hypo-motility and acidic secretion of the gastro-intestinal tract comprising administering a therapeutically effective amount thereof.

摘要翻译： 本发明涉及反式-N-乙基-3-氟-3- [3-氟-4-（吡咯烷-1-基甲基） - 苯基] - 环丁烷甲酰胺（1）的甲苯磺酸盐：溶剂合物（例如， 抑郁症，情绪障碍，精神分裂症，焦虑障碍，认知障碍，阿尔茨海默氏病，注意力缺陷障碍（ADD），注意缺陷多动障碍（ADHD）等）的治疗方法，其特征在于， ，精神障碍，睡眠障碍，肥胖，眩晕，癫痫，运动病，呼吸系统疾病，过敏，过敏引起的气道反应，过敏性鼻炎，鼻塞，过敏充血，充血，低血压，心血管疾病，胃肠道疾病， - 和 - 肠动力不足和酸分泌，包括给予治疗有效量的。

公开(公告)号：US07300944B2

公开(公告)日：2007-11-27

申请号：US10875009

申请日：2004-06-23

申请人： Daniel W. Kung ,  Travis T. Wager

发明人： Daniel W. Kung ,  Travis T. Wager

IPC分类号： C07D471/02 ,  A61K31/4745

CPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/4745 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention provides compounds of formula (I) the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers, and prodrugs, wherein R1, R2 and R3 are as defined herein; pharmaceutical formulations thereof; and use thereof in the treatment of, inter alia, conditions, diseases, and symptoms such as bipolar disorder, diabetes, dementia, Alzheimer's Disease, stroke, schizophrenia, depression, hair loss, and cancer.

摘要翻译： 本发明提供式（I）化合物，其立体异构体和前药，以及化合物，立体异构体和前药的药学上可接受的盐，其中R 1，R 2， R 3和R 3如本文所定义; 药物制剂; 及其用于治疗特别是诸如双相情感障碍，糖尿病，痴呆，阿尔茨海默氏病，中风，精神分裂症，抑郁症，脱发和癌症的病症，疾病和症状。

公开(公告)号：US08536164B2

公开(公告)日：2013-09-17

申请号：US13323883

申请日：2011-12-13

申请人： Todd W. Butler ,  Ramalakshmi Y. Chandrasekaran ,  Scot R. Mente ,  Chakrapani Subramanyam ,  Travis T. Wager

发明人： Todd W. Butler ,  Ramalakshmi Y. Chandrasekaran ,  Scot R. Mente ,  Chakrapani Subramanyam ,  Travis T. Wager

IPC分类号： A61K31/4355 ,  A61K31/437 ,  A61K31/506 ,  A61K31/435 ,  C07D471/04 ,  C07D498/04 ,  C07D401/04 ,  A61P25/24

CPC分类号： C07D401/04 ,  C07D471/04 ,  C07D491/048 ,  C07D498/04

摘要： Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, A, R4, n, and R7 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

摘要翻译： 公开了化合物的化合物和药学上可接受的盐，其中所述化合物具有式I的结构及其药学上可接受的盐，其中X，Y，A，R4，n和R7如说明书中所定义。 还公开了相应的药物组合物，治疗方法，合成方法和中间体。

公开(公告)号：US08518944B2

公开(公告)日：2013-08-27

申请号：US12911030

申请日：2010-10-25

申请人： Chakrapani Subramanyam ,  Travis T. Wager

发明人： Chakrapani Subramanyam ,  Travis T. Wager

IPC分类号： C07D403/14 ,  C07D401/14 ,  C07D413/14 ,  A61K31/506

CPC分类号： C07D403/14 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

摘要： Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

摘要翻译： 公开了化合物的化合物和药学上可接受的盐，其中化合物具有说明书中定义的式I的结构。 还公开了相应的药物组合物，治疗方法，合成方法和中间体。

公开(公告)号：US20120220568A1

公开(公告)日：2012-08-30

申请号：US13415944

申请日：2012-03-09

申请人： Travis T. Wager ,  Ramalakshmi Y. Chandrasekaran ,  Todd William Butler

发明人： Travis T. Wager ,  Ramalakshmi Y. Chandrasekaran ,  Todd William Butler

IPC分类号： A61K31/40 ,  C07D403/12 ,  A61K31/4025 ,  C07D413/12 ,  A61K31/5377 ,  A61K31/553 ,  A61P25/24 ,  A61P25/18 ,  A61P25/22 ,  A61P25/28 ,  A61P25/00 ,  A61P3/04 ,  A61P25/08 ,  A61P11/00 ,  A61P37/08 ,  A61P11/02 ,  A61P9/02 ,  A61P9/00 ,  A61P1/00 ,  A61P11/08 ,  A61P11/06 ,  A61K31/4402 ,  A61K31/435 ,  A61K31/445 ,  C07D295/155

CPC分类号： C07D295/155 ,  C07D295/185

摘要： This invention is directed to a compound of formula I, wherein R1, R2, R4, R5, R6, R7, R8 and n are as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a process of preparation of a compound of formula I, a method of treatment of a disorder or condition such as depression, mood disorders, schizophrenia, anxiety disorders, Alzheimer's disease, attention-deficit hyperactivity disorder (ADHD), psychotic disorders, cognitive disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper and hypo motility and acidic secretion of the gastro-intestinal tract that may be treated by antagonizing histamine H3 receptors, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above.

摘要翻译： 本发明涉及式I化合物或其药学上可接受的盐，其中R 1，R 2，R 4，R 5，R 6，R 7，R 8和n如本文所定义。 包含式I化合物的药物组合物，式I化合物的制备方法，治疗诸如抑郁症，情绪障碍，精神分裂症，焦虑症，阿尔茨海默病，注意缺陷多动障碍的病症或病症的方法 （ADHD），精神障碍，认知障碍，睡眠障碍，肥胖，眩晕，癫痫，运动病，呼吸系统疾病，过敏，过敏引起的气道反应，过敏性鼻炎，鼻塞，过敏性充血，充血，低血压，心血管疾病 的胃肠道，可以通过拮抗组胺H3受体来治疗的胃肠道的超低和低运动性和酸性分泌，所述方法包括向需要这种治疗的哺乳动物施用如上所述的式I化合物。

公开(公告)号：US20100256213A1

公开(公告)日：2010-10-07

申请号：US12745982

申请日：2008-12-04

申请人： Travis T. Wager ,  Todd W. Butler

发明人： Travis T. Wager ,  Todd W. Butler

IPC分类号： A61K31/40 ,  C07D207/08 ,  A61P25/00 ,  A61P11/00 ,  A61P37/08 ,  A61P9/00 ,  A61P1/04

CPC分类号： C07D295/073

摘要： The present invention is directed to the tosylate salt of trans-N-isobutyl-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)-phenyl]-cyclobutanecarboxamide Formula (I): to solvates (e.g., hydrates) thereof, to polymorphs thereof, to pharmaceutical compositions thereof and to a method of treating depression, mood disorders, schizophrenia, anxiety disorders, cognitive disorders, Alzheimer's disease, attention-deficit disorder (ADD), attention-deficit hyperactivity disorder (ADHD), psychotic disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper- and hypo-motility and acidic secretion of the gastro-intestinal tract comprising administering a therapeutically effective amount thereof.

摘要翻译： 本发明涉及反式-N-异丁基-3-氟-3- [3-氟-4-（吡咯烷-1-基甲基） - 苯基] - 环丁烷甲酰胺（I）的甲苯磺酸盐：溶剂化 ，水合物），其多晶型物，其药物组合物和治疗抑郁症，情绪障碍，精神分裂症，焦虑症，认知障碍，阿尔茨海默氏病，注意力缺陷障碍（ADD），注意缺陷多动障碍（ADHD） ），精神障碍，睡眠障碍，肥胖，眩晕，癫痫，运动病，呼吸系统疾病，过敏，过敏引起的气道反应，过敏性鼻炎，鼻充血，过敏充血，充血，低血压，心血管疾病，胃肠道疾病， 包括给予治疗有效量的胃肠道的超和不足和酸分泌。