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公开(公告)号：US08604053B2
公开(公告)日：2013-12-10
申请号：US12579821
申请日：2009-10-15
Applicant: Arthur R. Gomtsyan , Eric A. Voight , Erol K. Bayburt , Jun Chen , Jerome F. Daanen , Stanley DiDomenico , Michael E. Kort , Philip R. Kym , Heath A. McDonald , Richard J. Perner , Robert G. Schmidt
Inventor： Arthur R. Gomtsyan , Eric A. Voight , Erol K. Bayburt , Jun Chen , Jerome F. Daanen , Stanley DiDomenico , Michael E. Kort , Philip R. Kym , Heath A. McDonald , Richard J. Perner , Robert G. Schmidt
IPC: C07D405/12 , A61K31/4709
CPC classification number: C07D311/74 , C07D405/12
Abstract: Disclosed herein are compounds of formula (I) or pharmaceutically acceptable salts, solvates, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and m are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
Abstract translation: 本文公开了式（I）的化合物或其药学上可接受的盐，溶剂合物，前药，前药的盐或其组合，其中R1，R2，R3，R4和m在说明书中定义。 还公开了包含这些化合物的组合物和使用这些化合物和组合物治疗病症和病症的方法。
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2.发明申请FUSED COMPOUNDS THAT INHIBIT VANILLOID RECEPTOR SUBTYPE 1 (VR1) RECEPTOR 有权抑制VANILLOID受体亚型1（VR1）受体的融合化合物公开(公告)号：US20120190845A1
公开(公告)日：2012-07-26
申请号：US13292281
申请日：2011-11-09
Applicant: Arthur R. Gomtsyan , Erol K. Bayburt , Chih-Hung Lee , John R. Koenig , Robert G. Schmidt , Kirill A. Lukin , Gilles Chamboumier , Margaret Chi-Ping Hsu , Robert M. Leanna , Russell D. Cink
Inventor： Arthur R. Gomtsyan , Erol K. Bayburt , Chih-Hung Lee , John R. Koenig , Robert G. Schmidt , Kirill A. Lukin , Gilles Chamboumier , Margaret Chi-Ping Hsu , Robert M. Leanna , Russell D. Cink
IPC: C07D413/12 , C07D401/12 , C07D417/12 , C07D401/14 , C07D451/02 , C07D231/56 , C07D403/12
CPC classification number: C07D231/56 , C07D217/02 , C07D401/12 , C07D403/12
Abstract: The present invention discloses novel compounds of general formula (I) or a pharmaceutically acceptable salt or prodrug thereof (in which X1-X5, R5-R8b, Z1-Z2 and Ar1 are defined herein), a method for inhibiting the VR1 receptor in mammals using these compounds, a method for controlling pain in mammals, and pharmaceutical compositions including those compounds and a process for making those compounds.
Abstract translation: 本发明公开了通式（I）的新化合物或其药学上可接受的盐或前药（其中X1-X5，R5-R8b，Z1-Z2和Ar1如本文所定义），哺乳动物中抑制VR1受体的方法 使用这些化合物，控制哺乳动物疼痛的方法，以及包含那些化合物的药物组合物和制备这些化合物的方法。
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![Trisubstituted-N-[(1S)-1,2,3,4-Tetrahydro-1-naphthalenyl]benzamides which inhibit P2X3 and P2X2/3 containing receptors](/abs-image/US/2004/12/14/US06831193B2/abs.jpg.150x150.jpg)
3.发明授权Trisubstituted-N-[(1S)-1,2,3,4-Tetrahydro-1-naphthalenyl]benzamides which inhibit P2X3 and P2X2/3 containing receptors 有权抑制P2X3和P2X2 / 3含有受体的三取代-N - [（1S）-1,2,3,4-四氢-1-萘基]苯甲酰胺公开(公告)号：US06831193B2
公开(公告)日：2004-12-14
申请号：US10141989
申请日：2002-05-10
Applicant: Chih-Hung Lee , Richard J. Perner , Daniel P. Larson , John R. Koenig , Arthur R. Gomtsyan , Guo Zhu Zheng , Stanley DiDomenico , Andrew O. Stewart , Erol K. Bayburt
Inventor： Chih-Hung Lee , Richard J. Perner , Daniel P. Larson , John R. Koenig , Arthur R. Gomtsyan , Guo Zhu Zheng , Stanley DiDomenico , Andrew O. Stewart , Erol K. Bayburt
IPC: C07C22900
CPC classification number: C07D213/40 , C07D213/68 , C07D213/71 , C07D239/34 , C07D309/12 , C07D317/72 , C07D333/20 , C07D333/34 , C07D333/72
Abstract: Compounds of formula (I) are novel P2X3 and P2X2/P2X3 antagonists which are useful in treating pain, urinary incontinence and bladder overactivity.
Abstract translation: 式（I）化合物是可用于治疗疼痛，尿失禁和膀胱过度活动的新型P2X3和P2X2 / P2X3拮抗剂。
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公开(公告)号：US08350083B2
公开(公告)日：2013-01-08
申请号：US13249010
申请日：2011-09-29
Applicant: Arthur R. Gomtsyan , Robert G. Schmidt , Jerome F. Daanen , Erol K. Bayburt , Chih-hung Lee , Steven P. Latshaw
Inventor： Arthur R. Gomtsyan , Robert G. Schmidt , Jerome F. Daanen , Erol K. Bayburt , Chih-hung Lee , Steven P. Latshaw
IPC: C07C275/00 , C07D215/44
CPC classification number: C07C275/32 , C07D215/12 , C07D215/42 , C07D215/54 , C07D311/58 , C07D311/74
Abstract: The present application is directed to compounds that are TRPV1 antagonists and have formula (I) wherein variables Ar1, L1, R1, R2, R3, R4, R5, Y1, Y2, and Y3, are as defined in the description, which are useful for treating disorders caused by or exacerbated by vanilloid receptor activity.
Abstract translation: 本申请涉及作为TRPV1拮抗剂并且具有式（I）的化合物，其中变量Ar1，L1，R1，R2，R3，R4，R5，Y1，Y2和Y3如说明书中所定义，它们是有用的 用于治疗由香草素受体活性引起或加剧的病症。
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公开(公告)号：US08232309B2
公开(公告)日：2012-07-31
申请号：US11588713
申请日：2006-10-27
Applicant: Arthur R. Gomtsyan , Erol K. Bayburt , John R. Koenig , Kennan C. Marsh , Robert G. Schmidt, Jr. , Chih-Hung Lee , Weili Wang , Jerome F. Daanen , Brian S. Brown
Inventor： Arthur R. Gomtsyan , Erol K. Bayburt , John R. Koenig , Kennan C. Marsh , Robert G. Schmidt, Jr. , Chih-Hung Lee , Weili Wang , Jerome F. Daanen , Brian S. Brown
IPC: A61K31/416 , C07D231/56
CPC classification number: C07D405/12 , C07D231/56 , C07D403/12 , C07F9/65038
Abstract: Compounds of formula (I) wherein A, R1, R2, and R3 are defined in the specification, and which are useful as therapeutic compounds particularly for treating disorders or conditions associated with inflammation, pain, bladder overactivity, urinary incontinence, and other disorders caused by or exacerbated by TRPV1.
Abstract translation: 其中A，R 1，R 2和R 3在本说明书中定义并且可用作特别用于治疗与炎症，疼痛，膀胱过度活动，尿失禁和其他疾病相关的疾病或病症的治疗化合物的式（I）化合物 由TRPV1引起或加剧。
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Patent Agency Ranking
公开(公告)号：US20120108642A1
公开(公告)日：2012-05-03
申请号：US13337550
申请日：2011-12-27
Applicant: Arthur R. Gomtsyan , Robert G. Schmidt , Erol K. Bayburt , Jerome F. Daanen , Michael E. Kort
Inventor： Arthur R. Gomtsyan , Robert G. Schmidt , Erol K. Bayburt , Jerome F. Daanen , Michael E. Kort
IPC: A61K31/4418 , A61P29/00 , A61K31/426
CPC classification number: C07D213/62 , C07D213/06 , C07D277/22
Abstract: The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4, R5, m, and n are defined in the specification are TRPV1 antagonists. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
Abstract translation: 本发明涉及式（I）化合物，其中X，R 1，R 2，R 3，R 4，R 5，m和n在说明书中定义为TRPV1拮抗剂。 还公开了包含这些化合物的组合物和使用这些化合物和组合物治疗病症和病症的方法。
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公开(公告)号：US20100137360A1
公开(公告)日：2010-06-03
申请号：US12579821
申请日：2009-10-15
Applicant: Arthur R. Gomtsyan , Eric A. Voight , Erol K. Bayburt , Jun Chen , Jerome F. Daanen , Stanley DiDomenico , Michael E. Kort , Philip R. Kym , Heath A. McDonald , Richard J. Perner , Robert G. Schmidt
Inventor： Arthur R. Gomtsyan , Eric A. Voight , Erol K. Bayburt , Jun Chen , Jerome F. Daanen , Stanley DiDomenico , Michael E. Kort , Philip R. Kym , Heath A. McDonald , Richard J. Perner , Robert G. Schmidt
IPC: A61K31/4709 , A61P35/00 , A61P1/16 , A61P3/04 , A61P9/10 , A61P11/06 , C07D405/12 , C07D311/02 , A61K31/352 , A61K31/416
CPC classification number: C07D311/74 , C07D405/12
Abstract: Disclosed herein are compounds of formula (I) or pharmaceutically acceptable salts, solvates, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and m are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
Abstract translation: 本文公开了式（I）的化合物或其药学上可接受的盐，溶剂合物，前药，前药的盐或其组合，其中R1，R2，R3，R4和m在说明书中定义。 还公开了包含这些化合物的组合物和使用这些化合物和组合物治疗病症和病症的方法。
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公开(公告)号：US20090124671A1
公开(公告)日：2009-05-14
申请号：US12256924
申请日：2008-10-23
Applicant: Arthur R. Gomtsyan , Robert G. Schmidt , Erol K. Bayburt , Jerome F. Daanen , Michael E. Kort
Inventor： Arthur R. Gomtsyan , Robert G. Schmidt , Erol K. Bayburt , Jerome F. Daanen , Michael E. Kort
IPC: A61K31/44 , C07D213/56 , A61K31/426 , A61P11/00 , A61P3/04 , A61P1/00 , A61P29/00 , C07D277/30
CPC classification number: C07D213/62 , C07D213/06 , C07D277/22
Abstract: The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4, R5, m, and n are defined in the specification are TRPV1 antagonists. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
Abstract translation: 本发明涉及式（I）化合物，其中X，R 1，R 2，R 3，R 4，R 5，m和n在说明书中定义为TRPV1拮抗剂。 还公开了包含这些化合物的组合物和使用这些化合物和组合物治疗病症和病症的方法。
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9.发明申请FUSED AZABICYCLIC COMPOUNDS THAT INHIBIT VANILLOID RECEPTOR SUBTYPE 1 (VR1) RECEPTOR 有权抑制VANILLOID受体亚型1（VR1）受体的融合的偶氮化合物公开(公告)号：US20080214524A1
公开(公告)日：2008-09-04
申请号：US12033233
申请日：2008-02-19
Applicant: CHIH-HUNG LEE , EROL K. BAYBURT , STANLEY DIDOMENICO , IRENE DRIZIN , ARTHUR R. GOMTSYAN , JOHN R. KOENIG , RICHARD J. PERNER , ROBERT G. SCHMIDT , SEAN C. TURNER , TAMMIE K. WHITE , GUO ZHU ZHENG
Inventor： CHIH-HUNG LEE , EROL K. BAYBURT , STANLEY DIDOMENICO , IRENE DRIZIN , ARTHUR R. GOMTSYAN , JOHN R. KOENIG , RICHARD J. PERNER , ROBERT G. SCHMIDT , SEAN C. TURNER , TAMMIE K. WHITE , GUO ZHU ZHENG
IPC: A61K31/4725 , C07D217/02 , A61K31/5377 , C07D413/02 , A61K31/55 , C07D237/26 , A61K31/496 , C07D209/04 , A61K31/416 , A61P13/10 , C07D231/54 , A61K31/404 , A61K31/502 , A61P13/00 , C07D401/02 , C07D417/02 , A61K31/541
CPC classification number: C07D249/08 , C07D209/08 , C07D217/02 , C07D217/22 , C07D217/24 , C07D217/26 , C07D231/12 , C07D231/56 , C07D233/56 , C07D237/28 , C07D401/12 , C07D405/12
Abstract: Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.
Abstract translation: 式（I）化合物是可用于治疗疼痛，炎性热痛觉过敏，尿失禁和膀胱过度活动的新型VR1拮抗剂。
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公开(公告)号：US20080153871A1
公开(公告)日：2008-06-26
申请号：US11954875
申请日：2007-12-12
Applicant: Erol K. Bayburt , Jerome F. Daanen , Arthur R. Gomtsyan , Steven P. Latshaw , Chih-hung Lee , Robert G. Schmidt
Inventor： Erol K. Bayburt , Jerome F. Daanen , Arthur R. Gomtsyan , Steven P. Latshaw , Chih-hung Lee , Robert G. Schmidt
IPC: A61K31/47 , C07D311/04 , C07D215/00 , A61K31/17 , A61P13/02 , A61P43/00 , C07C275/00 , A61K31/352
CPC classification number: C07C275/32 , C07D215/12 , C07D215/42 , C07D215/54 , C07D311/58 , C07D311/74
Abstract: The present application is directed to compounds that are TRPV1 antagonists and have formula (I) wherein variables Ar1, L1, R1, R2, R3, R4, R5, Y1, Y2, and Y3, are as defined in the description, which are useful for treating disorders caused by or exacerbated by vanilloid receptor activity.
Abstract translation: 本申请涉及作为TRPV1拮抗剂并且具有式（I）的化合物，其中变量Ar 1，L 1，R 1，R 1， R 3，R 3，R 4，R 5，Y 1，Y 3， 描述中定义的那些，其可用于治疗由香草素受体活性引起或加剧的病症。
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