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公开(公告)号：US20070287707A1
公开(公告)日：2007-12-13
申请号：US11712264
申请日：2007-02-27
Applicant: Mark Arrington , Allen Hopper , Richard Conticello , Hans-Jurgen Hess , Stephen Hitchcock
Inventor： Mark Arrington , Allen Hopper , Richard Conticello , Hans-Jurgen Hess , Stephen Hitchcock
IPC: A61K31/498 , A61K31/5377 , A61P25/18 , C07D237/28 , C07D413/02
CPC classification number: C07D237/28 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/10 , C07D405/04 , C07D413/04 , C07D413/10 , C07D417/04 , C07D471/04
Abstract: The present invention if directed to certain cinnoline compounds that are PDE10 inhibitors, pharmaceutical compounds containing the same and processes for preparing the same. The invention is also directed to methods of treating diseases mediated by PDE10 enzyme such as obesity, non-insulin dependent diabetes, schizophrenia or bipolar disorder, obsessive-compulsive disorder, and the like.
Abstract translation: 本发明如果针对某些作为PDE10抑制剂的噌啉化合物，含有它们的药物化合物及其制备方法。 本发明还涉及治疗由PDE10酶介导的疾病如肥胖症，非胰岛素依赖性糖尿病，精神分裂症或双相情感障碍，强迫症等的疾病的方法。
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公开(公告)号：US20100016297A1
公开(公告)日：2010-01-21
申请号：US12488908
申请日：2009-06-22
Applicant: Richard Conticello , Ruiping Liu , Ashok Tehim , Wenge Xie
Inventor： Richard Conticello , Ruiping Liu , Ashok Tehim , Wenge Xie
IPC: A61K31/536 , C07D401/14 , A61K31/496 , C07D498/00 , A61P25/00 , A61P25/30 , A61P25/28 , A61P25/16 , A61P1/00 , A61P25/22 , A61P25/06 , A61P25/24 , A61P3/04 , A61P9/00 , A61P31/18 , A61P25/18 , A61P3/10
CPC classification number: C07D471/04
Abstract: The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein R1, R2, Ar, m and n are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
Abstract translation: 本公开内容提供对式（I）的5-HT 6受体具有亲和性的化合物：其中R 1，R 2，Ar，m和n如本文所定义。 本公开还涉及制备这种化合物的方法，含有这些化合物的组合物及其使用方法。
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公开(公告)号：US07495017B2
公开(公告)日：2009-02-24
申请号：US11797151
申请日：2007-05-01
Applicant: Allen Hopper , Erik Kuester , Robert Dunn , Richard Conticello
Inventor： Allen Hopper , Erik Kuester , Robert Dunn , Richard Conticello
IPC: A61K31/415 , A61K31/4439 , C07D231/12 , C07D401/04
CPC classification number: C07D403/04 , C07D231/12 , C07D231/56 , C07D307/20 , C07D405/04 , C07D405/12 , C07D409/12
Abstract: Selective PDE4 inhibition is achieved by aryl and heteroaryl pyrazole compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds such as rolipram and show selectivity with regard to inhibition of other classes of PDEs.
Abstract translation: 通过芳基和杂芳基吡唑化合物实现选择性PDE4抑制。 与化合物如咯利普兰相比，化合物表现出改善的PDE4抑制，并且在抑制其他类型的PDE时显示出选择性。
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公开(公告)号：US20070203197A1
公开(公告)日：2007-08-30
申请号：US11797151
申请日：2007-05-01
Applicant: Allen Hopper , Erik Kuester , Robert Dunn , Richard Conticello
Inventor： Allen Hopper , Erik Kuester , Robert Dunn , Richard Conticello
IPC: A61K31/4439 , A61K31/416 , A61K31/415 , C07D405/02 , C07D403/02
CPC classification number: C07D403/04 , C07D231/12 , C07D231/56 , C07D307/20 , C07D405/04 , C07D405/12 , C07D409/12
Abstract: Selective PDE4 inhibition is achieved by aryl and heteroaryl pyrazole compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds such as rolipram and show selectivity with regard to inhibition of other classes of PDEs.
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公开(公告)号：US07226930B2
公开(公告)日：2007-06-05
申请号：US10825611
申请日：2004-04-16
Applicant: Allen Hopper , Erik Kuester , Robert Dunn , Richard Conticello
Inventor： Allen Hopper , Erik Kuester , Robert Dunn , Richard Conticello
IPC: A61K31/437 , A61K31/4155 , C07D231/54 , C07D471/06
CPC classification number: C07D403/04 , C07D231/12 , C07D231/56 , C07D307/20 , C07D405/04 , C07D405/12 , C07D409/12
Abstract: Selective PDE4 inhibition is achieved by aryl and heteroaryl pyrazole compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds such as rolipram and show selectivity with regard to inhibition of other classes of PDEs.
Abstract translation: 通过芳基和杂芳基吡唑化合物实现选择性PDE4抑制。 与化合物如咯利普兰相比，化合物表现出改善的PDE4抑制，并且在抑制其他类型的PDE时显示出选择性。
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Patent Agency Ranking
公开(公告)号：US20060154960A1
公开(公告)日：2006-07-13
申请号：US11249769
申请日：2005-10-14
Applicant: Allen Hopper , Robert Dunn , Erik Kuester , Richard Conticello
Inventor： Allen Hopper , Robert Dunn , Erik Kuester , Richard Conticello
IPC: A61K31/4745 , A61K31/4439 , C07D471/02 , C07D403/02
CPC classification number: C07D405/12 , C07D231/12 , C07D231/56 , C07D403/04 , C07D403/14 , C07D405/04
Abstract: Selective PDE4 inhibition is achieved by aryl and heteroaryl pyrazole compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds such as rolipram and show selectivity with regard to inhibition of other classes of PDEs.
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公开(公告)号：US20070254913A1
公开(公告)日：2007-11-01
申请号：US11785741
申请日：2007-04-19
Applicant: Robert Dunn , Eric Kuester , Richard Conticello , Allen Hopper
Inventor： Robert Dunn , Eric Kuester , Richard Conticello , Allen Hopper
IPC: A61K31/4745 , A61K31/4439 , A61K31/416 , A61K31/4152 , C07D403/02 , C07D405/02 , C07D471/02
CPC classification number: C07D403/04 , C07D231/56 , C07D403/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D407/12 , C07D407/14 , C07D471/04
Abstract: Selective PDE4 inhibition is achieved by aryl and heteroaryl pyrazole compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds such as rolipram and show selectivity with regard to inhibition of other classes of PDEs.
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公开(公告)号：US20060160814A1
公开(公告)日：2006-07-20
申请号：US11217664
申请日：2005-09-02
Applicant: Mark Arrington , Ruiping Liu , Richard Conticello , Carla Gauss , Allen Hopper , Truc Nguyen , Ashok Tehim
Inventor： Mark Arrington , Ruiping Liu , Richard Conticello , Carla Gauss , Allen Hopper , Truc Nguyen , Ashok Tehim
IPC: A61K31/502 , C07D403/02
CPC classification number: C07D495/04 , C07D237/28 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14
Abstract: The present disclosure relates generally to the field of phosphodiesterase 10 (PDE10) enzyme inhibition by cinnoline compounds of Formulas I and II: wherein R1—R3 and R15—R18 are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
Abstract translation: 本公开一般涉及由式I和II的噌啉化合物抑制磷酸二酯酶10（PDE10）的领域：其中R 1〜R 3和R 3' 15R-18是如本文所定义的。 本公开还涉及制备这种化合物的方法，含有这些化合物的组合物及其使用方法。
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公开(公告)号：US07727558B2
公开(公告)日：2010-06-01
申请号：US11669649
申请日：2007-01-31
Applicant: Sam J. Milstein , Eugene N. Barantsevitch , Nai Fang Wang , Jun Liao , John Smart , Richard Conticello , Raphael Ottenbrite
Inventor： Sam J. Milstein , Eugene N. Barantsevitch , Nai Fang Wang , Jun Liao , John Smart , Richard Conticello , Raphael Ottenbrite
IPC: A61K9/50
CPC classification number: C08G65/33396 , A61K9/0019 , A61K38/27 , A61K38/29 , A61K47/10 , A61K47/32 , A61K47/56 , A61K47/60 , C08F8/30 , C08G65/329 , C08L2203/02
Abstract: Polymeric delivery agents, delivery agent compounds and compositions comprising them which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.
Abstract translation: 提供了可用于递送活性剂的聚合物递送剂，递送剂化合物和包含它们的组合物。 也提供给药和制备方法。
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公开(公告)号：US20090221661A1
公开(公告)日：2009-09-03
申请号：US12389873
申请日：2009-02-20
Applicant: Allen Hopper , Erik Kuester , Robert Dunn , Richard Conticello
Inventor： Allen Hopper , Erik Kuester , Robert Dunn , Richard Conticello
IPC: A61K31/4155 , C07D405/10 , A61P25/18
CPC classification number: C07D403/04 , C07D231/12 , C07D231/56 , C07D307/20 , C07D405/04 , C07D405/12 , C07D409/12
Abstract: Selective PDE4 inhibition is achieved by aryl and heteroaryl pyrazole compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds such as rolipram and show selectivity with regard to inhibition of other classes of PDEs.
Abstract translation: 通过芳基和杂芳基吡唑化合物来实现选择性PDE4抑制。 与化合物如咯利普兰相比，化合物表现出改善的PDE4抑制，并且在抑制其他类型的PDE时显示出选择性。
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