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1. 发明申请

US20070099954A1 Prodrugs of compounds that inhibit TRPV1 receptor 有权
标题翻译：抑制TRPV1受体的化合物的前药
公开(公告)号：US20070099954A1
公开(公告)日：2007-05-03
申请号：US11588713
申请日：2006-10-27
申请人： Arthur Gomtsyan , Erol Bayburt , John Koenig , Kennan Marsh , Robert Schmidt , Chih-Hung Lee , Weili Wang , Jerome Daanen , Brian Brown
发明人： Arthur Gomtsyan , Erol Bayburt , John Koenig , Kennan Marsh , Robert Schmidt , Chih-Hung Lee , Weili Wang , Jerome Daanen , Brian Brown
IPC分类号： A61K31/4709 , A61K31/416 , C07D405/02 , C07D403/02
CPC分类号： C07D405/12 , C07D231/56 , C07D403/12 , C07F9/65038
摘要： 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.
摘要翻译：其中A，R 1，R 2和R 3的式（I）化合物在说明书中定义，并且其可用作治疗性化合物，特别用于治疗与炎症，疼痛，膀胱过度活动，尿失禁以及由TRPV1引起或加重的其它障碍有关的疾病或病症。

2. 发明申请

US20110152250A1 CHROMANYLUREA COMPOUNDS THAT INHIBIT VANILLOID RECEPTOR SUBTYPE 1 (VR1) RECEPTOR AND USES THEREOF 有权
标题翻译：抑制VANILLOID受体亚型1（VR1）受体的氯霉素化合物及其用途
公开(公告)号：US20110152250A1
公开(公告)日：2011-06-23
申请号：US12875839
申请日：2010-09-03
申请人： Arthur Gomtsyan , Erol K. Bayburt , Robert G. Schmidt, JR. , Chih-Hung Lee , Brian S. Brown , Tammie K. Jinkerson , John R. Koenig , Jerome F. Daanen , Steven P. Latshaw
发明人： Arthur Gomtsyan , Erol K. Bayburt , Robert G. Schmidt, JR. , Chih-Hung Lee , Brian S. Brown , Tammie K. Jinkerson , John R. Koenig , Jerome F. Daanen , Steven P. Latshaw
IPC分类号： A61K31/55 , C07D231/56 , A61K31/416 , C07D215/00 , A61K31/47 , C07D217/00 , C07D401/02 , A61K31/4709 , C07D403/02 , C07D413/02 , A61K31/5377 , A61P29/00 , A61P13/00 , A61P19/02
CPC分类号： C07D405/12 , C07D401/12 , C07D403/12 , C07D413/12
摘要： Compounds that are antagonists of the VR1 receptor, having formula (I) or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein A1, A2, A3, A4, R7, R8, R9, X, Y, Z, L, n, and m, are as defined herein, and are useful in disorders prevented or ameliorated by inhibiting the VR1 receptor.
摘要翻译：作为VR1受体的拮抗剂的化合物，其具有式（I）或其前药的药学上可接受的盐，前药或盐，其中A1，A2，A3，A4，R7，R8，R9，X，Y，Z， L，n和m如本文所定义，并且可用于通过抑制VR1受体而防止或改善的病症。

3. 发明授权

US07902236B2 Antagonists of the vanilloid receptor subtype 1 (VR1) and use thereof 有权
标题翻译：香草素受体亚型1（VR1）的拮抗剂及其用途
公开(公告)号：US07902236B2
公开(公告)日：2011-03-08
申请号：US12365643
申请日：2009-02-04
申请人： Arthur Gomtsyan , Richard J. Perner , John R. Koenig , Margaret Chi-Ping Hsu , Dilinie P. Fernando , Chih-Hung Lee
发明人： Arthur Gomtsyan , Richard J. Perner , John R. Koenig , Margaret Chi-Ping Hsu , Dilinie P. Fernando , Chih-Hung Lee
IPC分类号： A61K31/426 , A61K31/421
CPC分类号： C07D263/48
摘要： The present invention is directed to compounds of formula (I) wherein variables W, X, Y, D, A, n, R1, R2 and R9 are as defined in the description.
摘要翻译：本发明涉及式（I）化合物，其中变量W，X，Y，D，A，n，R 1，R 2和R 9如说明书中所定义。

4. 发明授权

US06693136B1 Fluorenes and anthracenes that inhibit P2X3 and P2X2/3 containing receptors 有权
标题翻译：抑制P2X3和P2X2 / 3受体的芴和蒽
公开(公告)号：US06693136B1
公开(公告)日：2004-02-17
申请号：US10206265
申请日：2002-07-26
申请人： Chih-Hung Lee , Meiqun Jiang , Richard A. Perner , Arthur Gomtsyan , Erol K. Bayburt , Guo Zhu Zheng
发明人： Chih-Hung Lee , Meiqun Jiang , Richard A. Perner , Arthur Gomtsyan , Erol K. Bayburt , Guo Zhu Zheng
IPC分类号： A61K3118
CPC分类号： C07C311/21 , C07C311/29 , C07C2603/18 , C07C2603/24
摘要： Compounds of formula (I) are novel P2X3 and P2X2/P2X3 containing receptor antagonists and are useful in treating pain, urinary incontinence, and bladder overactivity.
摘要翻译：式（I）化合物是新型P2X3和P2X2 / P2X3受体拮抗剂，可用于治疗疼痛，尿失禁和膀胱过度活动。

5. 发明授权

US06242390B1 Cleanup additive 失效
标题翻译：清洁添加剂
公开(公告)号：US06242390B1
公开(公告)日：2001-06-05
申请号：US09127023
申请日：1998-07-31
申请人： Thomas O. Mitchell , Roger J. Card , Arthur Gomtsyan
发明人： Thomas O. Mitchell , Roger J. Card , Arthur Gomtsyan
IPC分类号： C09K300
CPC分类号： C09K8/685 , Y10S507/922
摘要： According to the present invention, a composition and method for hydraulically fracturing a subterranean formation is provided. The composition comprises an aqueous mixture of a hydrated polysaccharide, preferably a galactomannan gum, the hydrated polysaccharide having a plurality of bonding sites; a crosslinking agent for crosslinking the hydrated polysaccharide at the bonding sites at the conditions of the subterranean formation with a polyvalent metal ion to form a polyvalent metal crosslink, thereby increasing the viscosity of the hydrated polysaccharide; and a controlled solubility compound for releasing a chelating agent for controllably breaking the polyvalent metal crosslink and bonding with the polyvalent metal ion released by breaking the crosslink, thereby decreasing the viscosity of the hydrated polysaccharide. The method comprises the steps of injecting the above-described composition into the subterranean formation at fracturing pressures; allowing the controlled solubility compound to begin breaking the polyvalent metal crosslink, thereby reducing the viscosity of the hydrated polysaccharide and yielding a lower viscosity fluid; and removing the lower viscosity fluid from the subterranean formation.
摘要翻译：根据本发明，提供了一种用于水下压裂地层的组合物和方法。该组合物包含水合多糖，优选半乳甘露聚糖胶的水性混合物，所述水合多糖具有多个结合位点; 交联剂，用于在多层金属离子的地下条件下在结合位置处交联水合多糖以形成多价金属交联，从而提高水合多糖的粘度; 以及用于释放螯合剂以控制性地破坏多价金属交联并与通过断裂交联而释放的多价金属离子键合的受控溶解性化合物，从而降低水合多糖的粘度。该方法包括以下步骤：在压裂压力下将上述组合物注入地层; 允许受控溶解度化合物开始破坏多价金属交联，从而降低水合多糖的粘度并产生较低粘度的流体; 以及从地层中去除较低粘度的流体。

6. 发明授权

US08802711B2 TRPV1 antagonists 有权
标题翻译： TRPV1拮抗剂
公开(公告)号：US08802711B2
公开(公告)日：2014-08-12
申请号：US13426732
申请日：2012-03-22
申请人： Arthur Gomtsyan , Jerome F. Daanen , Gregory A. Gfesser , Michael E. Kort , Chih-Hung Lee , Heath A. McDonald , Pamela S. Puttfarcken , Eric A. Voight , Philip R. Kym
发明人： Arthur Gomtsyan , Jerome F. Daanen , Gregory A. Gfesser , Michael E. Kort , Chih-Hung Lee , Heath A. McDonald , Pamela S. Puttfarcken , Eric A. Voight , Philip R. Kym
IPC分类号： C07D265/36 , C07D215/38 , C07D217/02 , C07D231/56 , A61K31/17 , A61K31/538 , A61K31/192 , A61K31/472
CPC分类号： C07C275/32 , C07C2601/08 , C07C2602/08 , C07D209/08 , C07D215/38 , C07D217/02 , C07D231/56 , C07D239/80 , C07D263/48 , C07D265/36 , C07D401/04 , C07D413/12 , C07D417/12
摘要： Disclosed herein are compounds of formula (I) or pharmaceutically acceptable salts, solvates, or combinations thereof, wherein X1, X2, X3, X4, J, K, L, X5, X6, Rb, G2, 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.
摘要翻译：本文公开了式（I）化合物或其药学上可接受的盐，溶剂化物或其组合，其中X1，X2，X3，X4，J，K，L，X5，X6，Rb，G2和m在本说明书中定义。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。

7. 发明授权

US08026256B2 Fused compounds that inhibit vanilloid subtype 1 (VR1) receptor 有权
标题翻译：抑制香草素亚型1（VR1）受体的融合化合物
公开(公告)号：US08026256B2
公开(公告)日：2011-09-27
申请号：US11258980
申请日：2005-10-26
申请人： Arthur Gomtsyan , Erol K. Bayburt , John R. Koenig , Chih-Hung Lee
发明人： Arthur Gomtsyan , Erol K. Bayburt , John R. Koenig , Chih-Hung Lee
IPC分类号： C07D217/00 , A61K31/47
CPC分类号： C07D231/56 , C07D217/02 , C07D401/12 , C07D403/12
摘要： Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence, or bladder overactivity.
摘要翻译：式（I）化合物是可用于治疗疼痛，炎性热痛觉过敏，尿失禁或膀胱过度活动的新型VR1拮抗剂。

8. 发明申请

US20050113576A1 Fused azabicyclic compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor 审中-公开
标题翻译：融合的氮杂双环化合物抑制香草素受体亚型1（VR1）受体
公开(公告)号：US20050113576A1
公开(公告)日：2005-05-26
申请号：US10911019
申请日：2004-08-04
申请人： Chih-Hung Lee , Erol Bayburt , Stanley DiDomenico , Irene Drizin , Arthur Gomtsyan , John Koenig , Richard Perner , Robert Schmidt , Sean Turner , Tammie Jinkerson , Guo Zheng
发明人： Chih-Hung Lee , Erol Bayburt , Stanley DiDomenico , Irene Drizin , Arthur Gomtsyan , John Koenig , Richard Perner , Robert Schmidt , Sean Turner , Tammie Jinkerson , Guo Zheng
IPC分类号： C07D209/08 , C07D217/02 , C07D217/22 , C07D231/56 , C07D265/30 , C07D487/08 , C07D43/02
CPC分类号： C07D217/02 , C07D209/08 , C07D217/22 , C07D231/56 , C07D265/30 , C07D487/08
摘要： Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.
摘要翻译：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。

9. 发明申请

US20050043351A1 Fused compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor 有权
标题翻译：抑制香草素受体亚型1（VR1）受体的融合化合物
公开(公告)号：US20050043351A1
公开(公告)日：2005-02-24
申请号：US10864068
申请日：2004-06-09
申请人： Arthur Gomtsyan , Erol Bayburt , Chih-Hung Lee , John Koenig , Robert Schmidt , Kirill Lukin , Margaret Hsu , Marvin Leanna , Russell Cink , Gilles Chambournier
发明人： Arthur Gomtsyan , Erol Bayburt , Chih-Hung Lee , John Koenig , Robert Schmidt , Kirill Lukin , Margaret Hsu , Marvin Leanna , Russell Cink , Gilles Chambournier
IPC分类号： A61K31/47 , C07D217/12
CPC分类号： C07D217/02 , C07D231/56 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , C07D417/12 , C07D471/08
摘要： 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.
摘要翻译：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。

10. 发明授权

US08440691B2 Tetrahydroquinolinyl compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor and uses thereof 有权
标题翻译：抑制香草素受体亚型1（VR1）受体的四氢喹啉基化合物及其用途
公开(公告)号：US08440691B2
公开(公告)日：2013-05-14
申请号：US12875839
申请日：2010-09-03
申请人： Arthur Gomtsyan , Erol K. Bayburt , Robert G. Schmidt, Jr. , Chih-Hung Lee , Brian S. Brown , Tammie K. Jinkerson , John R. Koenig , Jerome F. Daanen , Steven P. Latshaw
发明人： Arthur Gomtsyan , Erol K. Bayburt , Robert G. Schmidt, Jr. , Chih-Hung Lee , Brian S. Brown , Tammie K. Jinkerson , John R. Koenig , Jerome F. Daanen , Steven P. Latshaw
IPC分类号： A61K31/47 , A61K31/445 , A61K31/415 , C07D217/00 , C07D215/00 , C07D211/00 , C07D231/56
CPC分类号： C07D405/12 , C07D401/12 , C07D403/12 , C07D413/12
摘要： Compounds that are antagonists of the VR1 receptor, having formula (I) or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein A1, A2, A3, A4, R7, R8, R9, X, Y, Z, L, n, and m, are as defined herein, and are useful in disorders prevented or ameliorated by inhibiting the VR1 receptor.
摘要翻译：作为VR1受体的拮抗剂的化合物，其具有式（I）或其前药的药学上可接受的盐，前药或盐，其中A1，A2，A3，A4，R7，R8，R9，X，Y，Z， L，n和m如本文所定义，并且可用于通过抑制VR1受体而防止或改善的病症。

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