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1.发明申请PIPERAZINYL DERIVATIVES USEFUL AS MODULATORS OF THE NEUROPEPTIDE Y2 RECEPTOR 审中-公开作为神经元Y2受体的调节剂有用的哌嗪衍生物
公开(公告)号：WO2009079593A1
公开(公告)日：2009-06-25
申请号：PCT/US2008/087250
申请日：2008-12-17
申请人： Janssen Pharmaceutica N.V. , CHAI, Wenying , DVORAK, Curt, A. , JABLONOWSKI, Jill, A. , RUDOLPH, Dale, A. , SHAH, Chandravadan, R. , WONG, Victoria
发明人： CHAI, Wenying , DVORAK, Curt, A. , JABLONOWSKI, Jill, A. , RUDOLPH, Dale, A. , SHAH, Chandravadan, R. , WONG, Victoria
IPC分类号： C07D213/38 , C07D231/12 , C07D231/20 , C07D249/08 , C07D263/16 , C07D263/32 , C07D263/34 , C07D271/06 , C07D271/10 , C07D275/02 , C07D285/08 , C07D295/15 , C07D271/07 , C07D207/335 , A61K31/496
CPC分类号： C07D271/06 , C07D207/335 , C07D213/38 , C07D231/12 , C07D231/20 , C07D249/08 , C07D263/16 , C07D263/32 , C07D263/34 , C07D271/07 , C07D271/10 , C07D275/02 , C07D285/08 , C07D295/15
摘要： The present invention is directed to piperidinyl and piperazinyl derivatives of formula (I) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds for the treatment and / or prevention of disorders, diseases and conditions mediated by the NPY Y2 receptor.
摘要翻译： 本发明涉及可用作NPY Y2受体的抑制剂的式（I）的哌啶基和哌嗪衍生物，包含所述化合物的药物组合物，所述化合物的制备方法和所述化合物用于治疗和/或预防的用途 由NPY Y2受体介导的疾病，疾病和病症。
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2.发明申请(1H-BENZOIMIDAZOL-2-YL)-(PIPERAZINYL)-METHANONE DERIVATIVES AND RELATED COMPOUNDS AS HISTAMINE H4-RECEPTOR ANTAGONISTS FOR THE TREATMENT OF INFLAMMATORY AND ALLERGIC DISORDERS 审中-公开（1H-BENZOIMIDAZOL-2-YL） - （PIPERAZINYL）-METHANONE衍生物及相关化合物作为治疗炎症和过敏性疾病的HISTAMINE H4受体拮抗剂
公开(公告)号：WO2004022060A3
公开(公告)日：2004-07-08
申请号：PCT/US0327461
申请日：2003-09-04
申请人： JANSSEN PHARMACEUTICA NV , CARRUTHERS NICHOLAS I , DVORAK CURT A , EDWARDS JAMES P , GRICE CHERYL A , JABLONOWSKI JILL A , LY KIEV S , PIO BARBARA A , SHAH CHANDRAVADAN R , VENABLE JENNIFER D
发明人： CARRUTHERS NICHOLAS I , DVORAK CURT A , EDWARDS JAMES P , GRICE CHERYL A , JABLONOWSKI JILL A , LY KIEV S , PIO BARBARA A , SHAH CHANDRAVADAN R , VENABLE JENNIFER D
IPC分类号： C07D235/16 , A61K31/4184 , A61K31/439 , A61K31/496 , A61K31/551 , C07D235/24 , C07D263/58 , C07D277/68 , C07D403/06 , C07D413/06 , C07D417/06 , C07D451/04 , C07D471/04
CPC分类号： C07D235/24 , C07D263/58 , C07D277/68 , C07D403/06 , C07D451/04 , C07D471/04
摘要： (1H-Benzoimidazol-2-YL)-(Piperazinyl)-Methanone derivatives of formula (I) and related compounds as histamine H4-receptor antagonists for the treatment of inflammatory and allergic disorders (I) wherein B and B are C or up to one of B and B may be N; Y is O, S or NR , where R is H or C1-4alkyl; Z is O or S; R is H and R is (a), where R Is H or C1-4alkyl, or R and R are taken together with their N of attachment to form (b); n is 1 or 2; m is 1 or 2; n + m is 2 or 3; other substituents as defined in claim 1.
摘要翻译： （1H-苯并咪唑-2-基） - （哌嗪基） - 式（I）的甲酮衍生物和相关化合物作为用于治疗炎性和过敏性疾病的组胺H 4受体拮抗剂（I），其中B和B 1是C 或者至多一个B和B <1>可以是N; Y是O，S或NR 2，其中R 2是H或C 1-4烷基; Z是O或S; R 8是H且R 9是（a），其中R 10是H或C 1-4烷基，或R 8和R 9与其连接的N一起形成（b ）; n为1或2; m为1或2; n + m为2或3; 权利要求1中定义的其它取代基。
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公开(公告)号：WO2004037801A1
公开(公告)日：2004-05-06
申请号：PCT/US2003/033343
申请日：2003-10-21
申请人： JANSSEN PHARMACEUTICA, N.V. , APODACA, Richard, L. , JABLONOWSKI, Jill, A. , LY, Kiev, S. , SHAH, Chandravadan, R. , SWANSON, Devin, M. , XIAO, Wei
发明人： APODACA, Richard, L. , JABLONOWSKI, Jill, A. , LY, Kiev, S. , SHAH, Chandravadan, R. , SWANSON, Devin, M. , XIAO, Wei
IPC分类号： C07D295/18
CPC分类号： C07D295/192 , A61K49/0004 , A61K51/0459 , A61K51/0463 , A61K51/0465 , A61K51/0468 , A61K51/047
摘要： Substituted piperazinyl and diazepanyl benzamides and benzthioamides of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.
摘要翻译： 式（I）的取代的哌嗪基和二氮杂环庚烷基苯甲酰胺和苯并硫代酰胺，含有它们的组合物，以及制备和使用它们来治疗组胺介导的病症的方法。
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公开(公告)号：WO2022256075A1
公开(公告)日：2022-12-08
申请号：PCT/US2022/022933
申请日：2022-03-31
申请人： EPIGEN BIOSCIENCES, INC. , BEATON, Graham , RAVULA, Satheesh, B. , TUCCI, Fabio , LEE, Suk, Joong , SHAH, Chandravadan, R.
发明人： BEATON, Graham , RAVULA, Satheesh, B. , TUCCI, Fabio , LEE, Suk, Joong , SHAH, Chandravadan, R.
IPC分类号： A61K31/4155 , A61K31/435 , A61K31/506 , C07D213/04 , C07D231/12 , C07D239/42
摘要： Pyrimidine and Pyridine amine containing compounds are described herein that are enzyme p70S6K inhibitors useful in the treatment of S6K-dependent or S6K-mediated diseases and conditions, including but not limited to cancer, fibrotic metabolic and certain neurological disorders.
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5.发明申请SUBSTITUTED PIPERAZINES AND PIPERIDINES AS MODULATORS OF THE NEUROPEPTIDE Y2 RECEPTOR 审中-公开作为神经元Y2受体的调节剂的替代哌嗪和哌啶
公开(公告)号：WO2007053436A1
公开(公告)日：2007-05-10
申请号：PCT/US2006/041940
申请日：2006-10-27
申请人： JANSSEN PHARMACEUTICA N.V. , BONAVENTURE, Pascal , CARRUTHERS, Nicholas, I. , CHAI, Wenying , DVORAK, Curt, A. , JABLONOWSKI, Jill, A. , RUDOLPH, Dale, A. , SEIERSTAD, Mark , SHAH, Chandravadan, R. , SWANSON, Devin, M. , WONG, Victoria, D.
发明人： BONAVENTURE, Pascal , CARRUTHERS, Nicholas, I. , CHAI, Wenying , DVORAK, Curt, A. , JABLONOWSKI, Jill, A. , RUDOLPH, Dale, A. , SEIERSTAD, Mark , SHAH, Chandravadan, R. , SWANSON, Devin, M. , WONG, Victoria, D.
IPC分类号： C07D295/14 , C07D413/12 , C07D211/34 , C07D307/24 , C07D261/14 , C07D261/08 , C07D211/58 , C07D213/56 , C07D207/08 , C07D205/04 , C07D213/82 , C07D307/68 , C07D333/38 , C07D207/34 , C07D213/81
CPC分类号： 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
摘要： The invention provides novel non-peptidic NPY Y2 receptor inhibitors (1) 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.
摘要翻译： 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（1） 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; 骨丢失物质相关疾病; 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未排卵和不育症。
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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
申请人： JANSSEN PHARMACEUTICA NV , CARRUTHERS NICHOLAS I , KEITH JOHN M , LETAVIC MICHAEL A , SHAH CHANDRAVADAN R
IPC分类号： C07D471/04 , A61K31/4745 , A61K31/4985 , A61K31/52 , A61P25/00
CPC分类号： C07D471/04
摘要： 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.
摘要翻译： 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。
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7.发明申请
公开(公告)号：WO2005097751A3
公开(公告)日：2006-03-09
申请号：PCT/US2005010570
申请日：2005-03-31
IPC分类号： C07D213/82 , A61K31/422 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/5377 , A61P25/00 , A61P37/08 , C07D213/38 , C07D213/64 , C07D213/65 , C07D213/66 , C07D213/81 , C07D213/83 , C07D241/24 , C07D261/08 , C07D261/12 , C07D413/14
CPC分类号： C07D261/12 , C07D213/38 , C07D213/64 , C07D213/65 , C07D213/66 , C07D213/81 , C07D213/82 , C07D213/83 , C07D241/24 , C07D261/08
摘要： Certain non-imidazole heterocyclic compounds of formula (I) are histamine H
摘要翻译： 某些式（I）的咪唑杂环化合物是组胺H
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公开(公告)号：WO2011050202A1
公开(公告)日：2011-04-28
申请号：PCT/US2010/053611
申请日：2010-10-21
申请人： JANSSEN PHARMACEUTICA NV , BRANSTETTER, Bryan, James , LETAVIC, Michael, A. , LY, Kiev, S. , RUDOLPH, Dale, A. , SAVALL, Brad, M. , SHAH, Chandravadan, R. , SHIREMAN, Brock, T.
发明人： BRANSTETTER, Bryan, James , LETAVIC, Michael, A. , LY, Kiev, S. , RUDOLPH, Dale, A. , SAVALL, Brad, M. , SHAH, Chandravadan, R. , SHIREMAN, Brock, T.
IPC分类号： C07D471/04 , C07D487/04 , A61K31/4353 , A61P25/00
CPC分类号： C07D471/04 , C07D487/04
摘要： Certain disubstituted 3,8-diaza-bicyclo[4.2.0]octane and 3,6-diazabicyclo [3.2.0]heptane are described, which are useful as orexin inhibitors. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.
摘要翻译： 描述了某些二取代的3,8-二氮杂 - 双环[4.2.0]辛烷和3,6-二氮杂双环[3.2.0]庚烷，其可用作食欲素抑制剂。 这样的化合物可用于治疗由食欲素活性（例如失眠）介导的疾病状态，病症和病症的药物组合物和方法。
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公开(公告)号：WO2011050200A1
公开(公告)日：2011-04-28
申请号：PCT/US2010/053609
申请日：2010-10-21
申请人： JANSSEN PHARMACEUTICA NV , BRANSTETTER, Bryan, James , LETAVIC, Michael, A. , LY, Kiev, S. , RUDOLPH, Dale, A. , SAVALL, Brad, M. , SHAH, Chandravadan, R. , SHIREMAN, Brock, T.
发明人： BRANSTETTER, Bryan, James , LETAVIC, Michael, A. , LY, Kiev, S. , RUDOLPH, Dale, A. , SAVALL, Brad, M. , SHAH, Chandravadan, R. , SHIREMAN, Brock, T.
IPC分类号： C07D471/08 , A61K31/439 , A61P25/00
CPC分类号： C07D471/08
摘要： Disubstituted 3,8-diaza-bicyclo[4.2.0]octane and 3,6-diazabicyclo [3.2.0]heptane compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.
摘要翻译： 描述了二取代的3,8-二氮杂双环[4.2.0]辛烷和3,6-二氮杂双环[3.2.0]庚烷化合物，其可用作食欲素受体调节剂。 这样的化合物可用于治疗由食欲素活性（例如失眠）介导的疾病状态，病症和病症的药物组合物和方法。
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10.发明申请NON-IMIDAZOLE HETEROCYCLIC COMPOUNDS AS HISTAMINE H3 RECEPTOR MODULATORS 审中-公开作为组胺H3受体调节剂的非咪唑类杂环化合物
公开(公告)号：WO2005096734A3
公开(公告)日：2006-04-20
申请号：PCT/US2005010632
申请日：2005-03-31
IPC分类号： A61K31/496 , A61K31/506 , A61K31/551 , C07D207/34 , C07D263/34 , C07D277/56 , C07D307/68 , C07D333/38 , A61K31/381 , A61P25/00
CPC分类号： C07D263/34 , C07D207/34 , C07D277/56 , C07D307/68 , C07D333/38
摘要： Certain non-imidazole heterocyclic compounds are histamine H 3 modulators useful in the treatment of histamine H 3 receptor mediated diseases.
摘要翻译： 某些非咪唑杂环化合物是可用于治疗组胺H 3受体介导的疾病的组胺H 3 N调节剂。
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