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1. 发明申请

US20060058360A1 Propanamine derivatives as serotonin and norepinephrine reuptake inhibitors 失效
公开(公告)号：US20060058360A1
公开(公告)日：2006-03-16
申请号：US10532765
申请日：2003-10-24
申请人： Serge Boulet , Sandra Filla , Peter Gallagher , Kevin Hudziak , Anette Johansson , Rushad Karanjawala , John Masters , Brian Mathes , Richard Rathmell , Maria Whatton , Victor Matassa , Chad Wolfe
发明人： Serge Boulet , Sandra Filla , Peter Gallagher , Kevin Hudziak , Anette Johansson , Rushad Karanjawala , John Masters , Brian Mathes , Richard Rathmell , Maria Whatton , Victor Matassa , Chad Wolfe
IPC分类号： A61K31/428 , A61K31/425 , C07D277/62 , C07D275/06
CPC分类号： C07D275/04 , C07D215/20 , C07D217/02 , C07D217/04 , C07D217/24 , C07D277/62 , C07D333/54 , C07D471/04 , C07D495/04
摘要： There is provided a heretoaryloxy/thio 3-substituted propanamine compound of formula (I) wherein A is selected from —)— and —S—; X is selected from phenyl optionally substituted with up to 5 substituents each independently selected from halo, C1-C4 alkyl and C1-C4 alkoxy, thienyl optionally substituted with up to 3 substituents each independently selected from halo and C1-C4 alkyl, and C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl —S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, and thienopyridyl, each of which may be optionally substituted with up to 4 or, where possible, up to 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro acetyl, —CF3, —SCF3 and cyano; Z is selected from H, OR3 or F, wherein R3 is selected from H, C1-C6 alkyl and phenyl C1C6 alkyl; R1 and R2 are each independently H or C1-C4 alkyl; and pharmaceutically acceptable salts thereof.

2. 发明申请

US20060014779A1 3-Aryloxy/thio-3-substituted propanamines and their use in inhibiting serotonin and norephinephrine reuptake 失效
公开(公告)号：US20060014779A1
公开(公告)日：2006-01-19
申请号：US10532657
申请日：2003-10-24
申请人： Serge Boulet , Ann Filla , Peter Gallagher , Kevin Hudziak , Anette Johansson , Rushad Karanjawla , John Masters , Victor Matassa , Brian Mathes , Richard Rathmell , Maria Whatton , Chad Wolfe
发明人： Serge Boulet , Ann Filla , Peter Gallagher , Kevin Hudziak , Anette Johansson , Rushad Karanjawla , John Masters , Victor Matassa , Brian Mathes , Richard Rathmell , Maria Whatton , Chad Wolfe
IPC分类号： A61K31/4745 , A61K31/4743 , A61K31/4704 , A61K31/428 , A61K31/423
CPC分类号： C07C217/20 , C07C217/34 , C07D333/54
摘要： There is provided a compound of formula (I) wherein A is selected from —O— and —S—; X is selected from C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl, 1,3-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to 4 or, where possible, 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro, acetyl, —CF3, —SCF3 and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C1-C4 alkyl; Z is selected from H, OR3 or F, wherein R3 is selected from H, C1-C6 alkyl and phenyl C1-C6 alkyl; R1 and R2 are each independently H or C1-C4 alkyl; with the proviso that, when Z is H, then Y may not be optionally substituted phenyl or optionally substituted naphthyl.

3. 发明申请

US20070093526A1 4-Amino-piperidine derivatives as monoamine uptake inhibitors 失效
标题翻译： 4-氨基 - 哌啶衍生物作为单胺吸收抑制剂
公开(公告)号：US20070093526A1
公开(公告)日：2007-04-26
申请号：US10597795
申请日：2005-02-11
申请人： Serge Boulet , Barry Clark , John Fairhurst , Peter Gallagher , Anette Johansson , Maria Whatton , Virginia Wood
发明人： Serge Boulet , Barry Clark , John Fairhurst , Peter Gallagher , Anette Johansson , Maria Whatton , Virginia Wood
IPC分类号： A61K31/4545 , A61K31/454 , C07D403/02 , C07D401/02
CPC分类号： C07D513/04 , A61K31/454 , A61K31/4545 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The present invention provides compounds of formula (I) where n, R1, R2, R3, R4, R5 and Heteroaryl are defined herein. The compounds are inhibitors of the uptake of one or more monoamines selected from serotonin, norepinephrine and dopamine and, as such, may be useful in the treatment of disorders of the central and/or peripheral nervous system.
摘要翻译：本发明提供式（I）化合物，其中n，R 1，R 2，R 3，R 4，R 5和杂芳基如本文所定义。这些化合物是一种或多种选自5-羟色胺，去甲肾上腺素和多巴胺的单胺摄取的抑制剂，因此可用于治疗中枢和/或周围神经系统疾病。

4. 发明申请

US20070072859A1 Pharmaceutical compounds 审中-公开
公开(公告)号：US20070072859A1
公开(公告)日：2007-03-29
申请号：US10597835
申请日：2005-02-18
申请人： Serge Boulet , Anette Johansson , Sarah Smith
发明人： Serge Boulet , Anette Johansson , Sarah Smith
IPC分类号： A61K31/5375 , A61K31/445 , A61K31/40 , A61K31/137 , C07D211/06
CPC分类号： C07C217/20 , C07D295/125 , C07D295/13
摘要： The present invention relates to inhibitors of serotonin and/or norepinephrine reuptake and specifically provides compounds of formula (I): wherein A is selected from —O— and —S—; X is selected from C1-C8 alkyl, C2-C8 alkenyl, and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from phenyl, pyrrolidinyl, piperidinyl, morpholinyl, halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from (a), (b), (c), (d), (e), (f) where R3, R4 and R5 are independently selected from hydrogen, halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro, acetyl, —CF3, —SCF3 and cyano; R6 and R7 are independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro, acetyl, —CF3, —SCF3 and cyano; R8 is selected from chloro, bromo, iodo, C1-C4alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro, acetyl, —CF3, —SCF3 and cyano; R1 and R2 are each independently hydrogen or C1-C4 alkyl; or pharmaceutically acceptable salts thereof; or compositions thereof and methods of using the same.

5. 发明申请

US20060173035A1 3-Aryloxy/thio-2,3-substituted propanamines and their use in inhibiting serotonin and norepinephrine reuptake 失效
公开(公告)号：US20060173035A1
公开(公告)日：2006-08-03
申请号：US10533328
申请日：2003-10-24
申请人： Serge Boulet
发明人： Serge Boulet
IPC分类号： A61K31/4745 , A61K31/4743 , A61K31/4704 , A61K31/428 , A61K31/404 , A61K31/381 , A61K31/138
CPC分类号： C07D275/04 , C07C217/16 , C07C217/30 , C07C217/48 , C07C323/32 , C07D307/86 , C07D333/54 , C07D333/62 , C07D475/04
摘要： There is provided a compound of formula (I) wherein A is selected from —O— and —S—; X is selected from phenyl optionally substituted with up to 5 substituents each independently selected from halo, C1-C4 alkyl and C1-C4 alkoxy, thienyl optionally substituted with up to 3 substituents each independently selected from halo and C1-C4 alkyl, and C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl, 1,3-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to 4 or, where possible, up to 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro, acetyl, —CF3, —SCF3 and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C1-C4 alkyl; Z is selected from OR3 or F, wherein R3 is selected from H, C1-C6 alkyl and phenyl C1-C6 alkyl; R1 and R2 are each independently H or C1-C4 alkyl; and pharmaceutically acceptable salts thereofwith the proviso that when Y is optionally substituted phenyl or optionally substituted 1,3-benzodioxolyl and Z is OR3 and X is optionally substituted phenyl then A is —S—.

6. 发明申请

US20070197604A1 Oxazole derivatives as histamine h3 receptor agents,preparation and therapeutic uses 有权
标题翻译：恶唑衍生物作为组胺h3受体剂，制备和治疗用途
公开(公告)号：US20070197604A1
公开(公告)日：2007-08-23
申请号：US11572283
申请日：2005-07-14
申请人： Lisa Beavers , Serge Boulet , Terry Finn , Robert Gadski , Willaim Hornback , Cynthia Jesudason , Richard Pickard , Freddie Stevens , Grant Vaught
发明人： Lisa Beavers , Serge Boulet , Terry Finn , Robert Gadski , Willaim Hornback , Cynthia Jesudason , Richard Pickard , Freddie Stevens , Grant Vaught
IPC分类号： A61K31/421 , A61K31/44 , C07D413/10
CPC分类号： C07D413/14 , C07D263/32 , C07D413/06 , C07D417/14
摘要： The present invention discloses novel aryl oxazole compounds of Formula I (I), or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing and using such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using these compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases. Formula I (I) or a pharmaceutically acceptable salt thereof, wherein: m is independenlly at each occurrence 1, 2, or 3, Z independently represents carbon (substituted with hydrogen or the optional substituents indicated herein) or nitrogen, provided that when Z is nitrogen then R6 is not attached to Z; R1 and R2 are independently —(C1—C7) alkyl (optionally substituted with one to three halogens), or R1 and R2 and the nitrogen to which they are attached form an azetidinyl ring, a pyrrolidinyl ring, or a piperidinyl ring, wherein further the azetidinyl, pyrrolidinyl, or piperidinyl ring so formed may be optionally substituted one to three times with R5; R6 is independently at each occurrence —H, -halogen, or —CH3.
摘要翻译：本发明公开了具有组胺H3受体拮抗剂或反向激动剂活性的式I（I）的新型芳基恶唑化合物或其药学上可接受的盐，以及制备和使用这些化合物的方法。在另一个实施方案中，本发明公开了包含式I化合物的药物组合物以及使用这些组合物治疗肥胖症，认知缺陷，发作性睡病和其他组胺H3受体相关疾病的方法。式I（I）或其药学上可接受的盐，其中：m在每次出现时独立地为1,2或3，Z独立地表示碳（被氢或本文所示的任选取代基）或氮，条件是当Z为氮，然后R6不连接到Z; R 1和R 2独立地为 - （C 1 -C 7 -C 7）烷基（任选被一至三个卤素取代），或R 1和R 2以及与它们相连的氮形成氮杂环丁烷基环，吡咯烷基环或哌啶基环，其中如此形成的氮杂环丁烷基，吡咯烷基或哌啶基环可以任选地被R 5取代一至三次; R 6在每次出现时独立地为-H， - 卤素或-CH 3。

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