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1.发明授权Process for the preparation of indazolyl ureas that inhibit Vanilloid subtype 1 (VR1) receptors 失效制备抑制香草素亚型1（VR1）受体的吲唑脲的方法公开(公告)号：US08519186B2
公开(公告)日：2013-08-27
申请号：US12914645
申请日：2010-10-28
Applicant: Kirill A. Lukin , Margaret Chi-Ping Hsu , Dilinie P. Fernando , Brian J. Kotecki , Marvin R. Leanna
Inventor： Kirill A. Lukin , Margaret Chi-Ping Hsu , Dilinie P. Fernando , Brian J. Kotecki , Marvin R. Leanna
IPC: C07C275/26
CPC classification number: C07D231/56
Abstract: The present invention relates to a process of preparing indazolyl ureas that are useful as antagonists of the vanilloid receptor subtype 1 (VR1).
Abstract translation: 本发明涉及制备可用作香草素受体亚型1（VR1）的拮抗剂的吲唑基脲的方法。
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2.发明授权Methods for making central nervous system agents that are TRPV1 antagonists 有权制备TRPV1拮抗剂的中枢神经系统药物的方法公开(公告)号：US08232411B2
公开(公告)日：2012-07-31
申请号：US12407857
申请日：2009-03-20
Applicant: Kirill A. Lukin , Brian J. Kotecki , Su Yu , Lei Wang , Anthony R. Haight
Inventor： Kirill A. Lukin , Brian J. Kotecki , Su Yu , Lei Wang , Anthony R. Haight
IPC: C07D231/56 , C07C211/00 , C07C237/00
CPC classification number: C07D231/56
Abstract: The invention discloses compounds of formula II: and methods of making the compounds, which are VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.
Abstract translation: 本发明公开了式II化合物及其制备可用于治疗疼痛，炎性热痛觉过敏，尿失禁和膀胱过度活动的VR1拮抗剂的化合物的方法。
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3.发明授权Process for the synthesis of (2S,3AR,7AS)-octahydro-1H-indole carboxylic acid as an intermediate for trandolapril 失效用于合成（2S，3AR，7AS） - 八氢-1H-吲哚羧酸作为中度剂的方法公开(公告)号：US08288565B2
公开(公告)日：2012-10-16
申请号：US12837686
申请日：2010-07-16
Applicant: Sanjay R. Chemburkar , Rajarathnam E. Reddy , Douglas M. Reamer , John T. Pavlina , Stephen S. Ulrey , Brian J. Kotecki
Inventor： Sanjay R. Chemburkar , Rajarathnam E. Reddy , Douglas M. Reamer , John T. Pavlina , Stephen S. Ulrey , Brian J. Kotecki
IPC: C07D209/04
CPC classification number: C07D209/42
Abstract: A process for the preparation of (2S,3aR,7aS)-octahydro-1H-indole-20carboxylic acid hydrochloride.
Abstract translation: （2S，3aR，7aS） - 八氢-1H-吲哚-20羧酸盐酸盐的制备方法。
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4.发明授权Process for the preparation of indazolyl ureas that inhibit Vanilloid subtype1 (VR1) receptors 有权制备抑制香草素亚型1（VR1）受体的吲唑基脲的方法公开(公告)号：US07847104B2
公开(公告)日：2010-12-07
申请号：US11734900
申请日：2007-04-13
Applicant: Kirill A. Lukin , Margaret Chi-Ping Hsu , Dilinie P. Fernando , Brian J. Kotecki , Marvin R. Leanna
Inventor： Kirill A. Lukin , Margaret Chi-Ping Hsu , Dilinie P. Fernando , Brian J. Kotecki , Marvin R. Leanna
IPC: C07D231/56
CPC classification number: C07D231/56
Abstract: The present invention relates to a process of preparing indazolyl ureas that are useful as antagonists of the vanilloid receptor subtype 1 (VR1).
Abstract translation: 本发明涉及制备可用作香草素受体亚型1（VR1）的拮抗剂的吲唑基脲的方法。
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5.发明申请PROCESS FOR THE SYNTHESIS OF (2S,3AR,7AS)-OCTAHYDRO-1H-INDOLE CARBOXYLIC ACID AS AN INTERMEDIATE FOR TRANDOLAPRIL 失效（2S，3AR，7AS）-OCTAHYDRO-1H-吲哚羧酸合成方法作为中间体用于沙丁胺醇公开(公告)号：US20110065930A1
公开(公告)日：2011-03-17
申请号：US12837686
申请日：2010-07-16
Applicant: Sanjay R. Chemburkar , Rajarathnam E. Reddy , Douglas M. Reamer , John T. Pavlina , Stephen S. Ulrey , Brian J. Kotecki
Inventor： Sanjay R. Chemburkar , Rajarathnam E. Reddy , Douglas M. Reamer , John T. Pavlina , Stephen S. Ulrey , Brian J. Kotecki
IPC: C07D209/42
CPC classification number: C07D209/42
Abstract: A process for the preparation of (2S,3aR,7aS)-octahydro-1H-indole-20carboxylic acid hydrochloride.
Abstract translation: （2S，3aR，7aS） - 八氢-1H-吲哚-20羧酸盐酸盐的制备方法。
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Patent Agency Ranking
![(1S,5S)-3-(5,6-dichloro-3-pyridinyl)-3,6-diazabicyclo[3.2.0]heptane](/abs-image/US/2009/05/26/US07538226B2/abs.jpg.150x150.jpg)
6.发明授权(1S,5S)-3-(5,6-dichloro-3-pyridinyl)-3,6-diazabicyclo[3.2.0]heptane 有权（1S，5S）-3-（5,6-二氯-3-吡啶基）-3,6-二氮杂双环[3.2.0]庚烷公开(公告)号：US07538226B2
公开(公告)日：2009-05-26
申请号：US11838745
申请日：2007-08-14
Applicant: Michael J. Buckley , Jianguo Ji , Geoff G. Z. Zhang , Rodger F. Henry , Weili W. Wang , Gregory S. Wayne , Wenke Li , Timothy B. Towne , Steven J. Wittenberger , Steven M. Hannick , Brian J. Kotecki , Bryan S. Macri , Timothy A. Robbins
Inventor： Michael J. Buckley , Jianguo Ji , Geoff G. Z. Zhang , Rodger F. Henry , Weili W. Wang , Gregory S. Wayne , Wenke Li , Timothy B. Towne , Steven J. Wittenberger , Steven M. Hannick , Brian J. Kotecki , Bryan S. Macri , Timothy A. Robbins
IPC: C07D487/04
CPC classification number: C07D487/04 , A61K31/397
Abstract: The present invention discloses (1S,5S)-3-(5,6-dichloro-3-pyridinyl)-3,6-diazabicyclo[3.2.0]heptane, salts thereof, and its use to treat pain and other disorders associated with the nicotinic acetylcholine receptor.
Abstract translation: 本发明公开了（1S，5S）-3-（5,6-二氯-3-吡啶基）-3,6-二氮杂双环[3.2.0]庚烷及其盐，其用于治疗与 烟碱乙酰胆碱受体。
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7.发明申请PROCESS FOR THE PREPARATION OF INDAZOLYL UREAS THAT INHIBIT VANILLOID SUBTYPE 1 (VR1) RECEPTORS 失效制备VANILLOID SUBTYPE 1（VR1）受体的非佐剂类URAAS的制备方法公开(公告)号：US20110040102A1
公开(公告)日：2011-02-17
申请号：US12914645
申请日：2010-10-28
Applicant: Kirill A. Lukin , Margaret Chi-Ping Hsu , Dilinie P. Fernando , Brian J. Kotecki , Marvin R. Leanna
Inventor： Kirill A. Lukin , Margaret Chi-Ping Hsu , Dilinie P. Fernando , Brian J. Kotecki , Marvin R. Leanna
IPC: C07D231/56 , C07C275/26
CPC classification number: C07D231/56
Abstract: The present invention relates to a process of preparing indazolyl ureas that are useful as antagonists of the vanilloid receptor subtype 1 (VR1).
Abstract translation: 本发明涉及制备可用作香草素受体亚型1（VR1）的拮抗剂的吲唑基脲的方法。
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![(1S,5S)-3-(5,6-DICHLORO-3-PYRIDINYL)-3,6- DIAZABICYCLO[3.2.0]HEPTANE](/abs-image/US/2009/08/13/US20090203664A1/abs.jpg.150x150.jpg)
8.发明申请(1S,5S)-3-(5,6-DICHLORO-3-PYRIDINYL)-3,6- DIAZABICYCLO[3.2.0]HEPTANE 审中-公开（1S，5S）-3-（5,6-二氯-3-吡啶基）-3,6-二氮杂双环[3.2.0]庚烷公开(公告)号：US20090203664A1
公开(公告)日：2009-08-13
申请号：US12426511
申请日：2009-04-20
Applicant: Michael J. Buckley , Jianguo Ji , Geoff G.Z. Zhang , Rodger F. Henry , Weili W. Wang , Gregory S. Wayne , Wenke Li , Timothy B. Towne , Steven J. Wittenberger , Steven M. Hannick , Brian J. Kotecki , Bryan S. Macri , Timothy A. Robbins
Inventor： Michael J. Buckley , Jianguo Ji , Geoff G.Z. Zhang , Rodger F. Henry , Weili W. Wang , Gregory S. Wayne , Wenke Li , Timothy B. Towne , Steven J. Wittenberger , Steven M. Hannick , Brian J. Kotecki , Bryan S. Macri , Timothy A. Robbins
IPC: A61K31/397 , A61P25/00 , A61P25/28 , C07D401/14
CPC classification number: C07D487/04 , A61K31/397
Abstract: The present invention discloses (1S,5S)-3-(5,6-dichloro-3-pyridinyl)-3,6-diazabicyclo[3.2.0]heptane, salts thereof, and its use to treat pain and other disorders associated with the nicotinic acetylcholine receptor.
Abstract translation: 本发明公开了（1S，5S）-3-（5,6-二氯-3-吡啶基）-3,6-二氮杂双环[3.2.0]庚烷及其盐，其用于治疗与 烟碱乙酰胆碱受体。
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![(1S,5S)-3-(5,6-dichloro-3-pyridinyl)-3,6-diazabicyclo[3.2.0]heptane](/abs-image/US/2008/04/08/US07354937B2/abs.jpg.150x150.jpg)
9.发明授权(1S,5S)-3-(5,6-dichloro-3-pyridinyl)-3,6-diazabicyclo[3.2.0]heptane 有权（1S，5S）-3-（5,6-二氯-3-吡啶基）-3,6-二氮杂双环[3.2.0]庚烷公开(公告)号：US07354937B2
公开(公告)日：2008-04-08
申请号：US11176087
申请日：2005-07-07
Applicant: Michael J. Buckley , Jianguo Ji , Geoff G. Z. Zhang , Rodger F. Henry , Weili W. Wang , Gregory S. Wayne , Wenke Li , Timothy B. Towne , Steven J. Wittenberger , Steven M. Hannick , Brian J. Kotecki , Bryan S. Macri , Timothy A. Robbins
Inventor： Michael J. Buckley , Jianguo Ji , Geoff G. Z. Zhang , Rodger F. Henry , Weili W. Wang , Gregory S. Wayne , Wenke Li , Timothy B. Towne , Steven J. Wittenberger , Steven M. Hannick , Brian J. Kotecki , Bryan S. Macri , Timothy A. Robbins
IPC: A61K31/4745 , C07D487/04
CPC classification number: C07D487/04 , A61K31/397
Abstract: The present invention discloses (1S,5S)-3-(5,6-dichloro-3-pyridinyl)-3,6-diazabicyclo[3.2.0]heptane, salts thereof, and its use to treat pain and other disorders associated with the nicotinic acetylcholine receptor.
Abstract translation: 本发明公开了（1S，5S）-3-（5,6-二氯-3-吡啶基）-3,6-二氮杂双环[3.2.0]庚烷及其盐，其用于治疗与 烟碱乙酰胆碱受体。
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10.发明申请METHODS FOR MAKING CENTRAL NERVOUS SYSTEM AGENTS THAT ARE TRPV1 ANTAGONISTS 有权用于制造TRPV1拮抗剂的中央神经系统药物的方法公开(公告)号：US20100016611A1
公开(公告)日：2010-01-21
申请号：US12407857
申请日：2009-03-20
Applicant: Kirill A. Lukin , Brian J. Kotecki , Su Yu , Lei Wang , Anthony R. Haight
Inventor： Kirill A. Lukin , Brian J. Kotecki , Su Yu , Lei Wang , Anthony R. Haight
IPC: C07D231/56 , C07C211/00 , C07C237/00
CPC classification number: C07D231/56
Abstract: The invention discloses compounds of formula II: and methods of making the compounds, which are VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.
Abstract translation: 本发明公开了式II化合物及其制备可用于治疗疼痛，炎性热痛觉过敏，尿失禁和膀胱过度活动的VR1拮抗剂的化合物的方法。
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