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1. 发明授权

US08232409B2 Heterocyclic benzimidazoles as TRPM8 modulators 有权
标题翻译：杂环苯并咪唑作为TRPM8调节剂
公开(公告)号：US08232409B2
公开(公告)日：2012-07-31
申请号：US12576283
申请日：2009-10-09
申请人： Mark R. Player , Daniel J. Parks , William Parsons , Sanath K. Meegalla , Carl R. Illig , Shelley K. Ballentine
发明人： Mark R. Player , Daniel J. Parks , William Parsons , Sanath K. Meegalla , Carl R. Illig , Shelley K. Ballentine
IPC分类号： A61K31/4188 , A61K31/4184 , A61K31/422 , A61K31/437 , C07D405/00 , C07D413/04 , C07D413/14
CPC分类号： C07D261/20 , C07D263/52 , C07D403/04 , C07D413/04 , C07D413/14 , C07D471/04 , C07D498/10
摘要： Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein W1, W2, W3, R1, R1a, R2, R2a, R3, V, Q, and X are defined herein.
摘要翻译：公开了用于治疗各种疾病，综合征，病症和障碍（包括疼痛）的化合物，组合物和方法。这样的化合物由式I表示如下：其中W1，W2，W3，R1，R1a，R2，R2a，R3，V，Q和X如本文所定义。

2. 发明授权

US07446210B2 Factor Xa compounds 有权
标题翻译：因子Xa化合物
公开(公告)号：US07446210B2
公开(公告)日：2008-11-04
申请号：US11257208
申请日：2005-10-24
申请人： Tianbao Lu , Tho V. Thieu , Yu-Kai Lee , Daniel J. Parks , Thomas P. Markotan , Wenxi Pan , Karen L. Milkiewicz , Mark R. Player
发明人： Tianbao Lu , Tho V. Thieu , Yu-Kai Lee , Daniel J. Parks , Thomas P. Markotan , Wenxi Pan , Karen L. Milkiewicz , Mark R. Player
IPC分类号： C07D207/00 , C07D213/00 , C07D231/00 , C07D231/54 , C07D239/02 , C07D241/04 , C07D265/28 , C07D295/00 , C07D487/00
CPC分类号： C07D413/14 , C07D231/56 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D409/14 , C07D413/04 , C07D417/10
摘要： The present invention is directed to novel compounds of Formula I: and forms and pharmaceutical compositions thereof, and the use thereof as inhibitors of Factor Xa.
摘要翻译：本发明涉及式I的新型化合物及其形式和药物组合物，以及其作为因子Xa抑制剂的用途。

3. 发明授权

US07115598B2 Substituted 1,4-diazepines and uses thereof 有权
标题翻译：取代的1,4-二氮杂及其用途
公开(公告)号：US07115598B2
公开(公告)日：2006-10-03
申请号：US10829040
申请日：2004-04-21
申请人： Tianbao Lu , Karen L. Milkiewicz , Pierre Raboisson , Maxwell David Cummings , Raul R. Calvo , Daniel J. Parks , Louis V. Lafrance, III , Juan Jose Marugan Sanchez , Joan Gushue , Kristi Leonard
发明人： Tianbao Lu , Karen L. Milkiewicz , Pierre Raboisson , Maxwell David Cummings , Raul R. Calvo , Daniel J. Parks , Louis V. Lafrance, III , Juan Jose Marugan Sanchez , Joan Gushue , Kristi Leonard
IPC分类号： C07D243/14 , A61K31/55
CPC分类号： C07D243/14
摘要： The present invention is directed to novel 1,4-diazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions. Compounds have Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein: R1, R2, R9, R10, Ra, Rd and M are defined herein;X is a bivalent radical of: an alkane, a cycloalkane, an optionally-substituted arene, an optionally-substituted heteroarene, an optionally-substituted arylalkane or an optionally-substituted heteroarylalkane; andR3 is —CO2Rd, —CO2M, —OH, —NHRd, —SO2Rd, —NHCONHRd, optionally-substituted amidino or optionally-substituted guanidino;or R3—X— is hydrogen or an electron pair;R4 is oxygen or —NR9R10;R5 is cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, aralkyl, heteroarylalkyl, or a saturated or partially unsaturated heterocycle, each of which is optionally substituted; andR6, R7 and R8 are independently hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, a saturated or partially unsaturated heterocycle, cycloalkylalkyl, aralkyl or heteroarylalkyl, each of which is optionally substituted; or R6 and R7, together with the carbon atom to which they are attached form a 3- to 7-membered carbocyclic ring optionally substituted 1 to 3 times with Ra.
摘要翻译：本发明涉及新的1,4-二氮杂，其药物组合物及其作为HDM2-p53相互作用抑制剂的用途。化合物具有式I：或其溶剂合物，水合物或其药学上可接受的盐; 其中：R 1，R 2，R 9，R 10，R a， >，R d和M在本文中定义; X是二价基团：烷烃，环烷烃，任选取代的芳烃，任选取代的杂芳烃，任选取代的芳基烷烃或任选取代的杂芳基烷烃; 和R 3是-CO 2 R 2，-CO 2 M，-OH，-NHR 0 任选取代的脒基或任选取代的胍基;其中R 1，R 2，R 3，R 4，或R 3 -X-是氢或电子对; R 4是氧或-NR 9 R 10; R 5是环烷基，芳基，杂芳基，环烷基烷基，芳烷基，杂芳基烷基或饱和或部分不饱和的杂环，其各自任选被取代; R 6和R 8独立地是氢，烷基，环烷基，芳基，杂芳基，饱和或部分不饱和的杂环，环烷基烷基，芳烷基或杂芳基烷基，其各自任选被取代; 或R 6和R 7与它们所连接的碳原子一起形成3-至7-元碳环，任选地被R 1取代1至3倍， SUP> a 。

4. 发明申请

US20100093788A1 HETEROCYCLIC BENZIMIDAZOLES AS TRPM8 MODULATORS 有权
标题翻译：作为TRPM8调节剂的杂环苯并咪唑
公开(公告)号：US20100093788A1
公开(公告)日：2010-04-15
申请号：US12576283
申请日：2009-10-09
申请人： Mark R. Player , Daniel J. Parks , William Parsons , Senath K. Meegalla , Carl R. Illig , Shelley K. Ballentine
发明人： Mark R. Player , Daniel J. Parks , William Parsons , Senath K. Meegalla , Carl R. Illig , Shelley K. Ballentine
IPC分类号： A61K31/437 , C07D261/20 , A61K31/42 , C07D498/10 , C07D263/52 , A61K31/421 , C07D471/02 , A61P29/00 , A61P25/24 , A61P9/00
CPC分类号： C07D261/20 , C07D263/52 , C07D403/04 , C07D413/04 , C07D413/14 , C07D471/04 , C07D498/10
摘要： Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein W1, W2, W3, R1, R1a, R2, R2a, R3, V, Q, and X are defined herein.
摘要翻译：公开了用于治疗各种疾病，综合征，病症和障碍（包括疼痛）的化合物，组合物和方法。这样的化合物由式I表示如下：其中W1，W2，W3，R1，R1a，R2，R2a，R3，V，Q和X如本文所定义。

5. 发明授权

US07612211B2 Benzimidazole TRPV1 inhibitors 有权
标题翻译：苯并咪唑TRPV1抑制剂
公开(公告)号：US07612211B2
公开(公告)日：2009-11-03
申请号：US11954647
申请日：2007-12-12
申请人： Wing S. Cheung , Daniel J. Parks , William H. Parsons , Sharmila Patel , Mark R. Player
发明人： Wing S. Cheung , Daniel J. Parks , William H. Parsons , Sharmila Patel , Mark R. Player
IPC分类号： A61K31/4184 , C07D235/12
CPC分类号： C07D235/12 , C07D235/06 , C07D235/14 , C07D235/26 , C07D235/30 , C07D401/12 , C07D405/12
摘要： The invention is directed to compounds of Formula (I): to pharmaceutical compositions containing such compounds and to methods of treatment using them.
摘要翻译：本发明涉及式（I）的化合物：含有这些化合物的药物组合物和使用它们的治疗方法。

6. 发明申请

US20080146637A1 BENZIMIDAZOLE TRPV1 INHIBITORS 有权
标题翻译：苯并咪唑TRPV1抑制剂
公开(公告)号：US20080146637A1
公开(公告)日：2008-06-19
申请号：US11954647
申请日：2007-12-12
申请人： Wing S. Cheung , Daniel J. Parks , William H. Parsons , Sharmila Patel , Mark R. Player
发明人： Wing S. Cheung , Daniel J. Parks , William H. Parsons , Sharmila Patel , Mark R. Player
IPC分类号： A61K31/4184 , A61P29/00 , C07D235/12
CPC分类号： C07D235/12 , C07D235/06 , C07D235/14 , C07D235/26 , C07D235/30 , C07D401/12 , C07D405/12
摘要： The invention is directed to compounds of Formula (I): to pharmaceutical compositions containing such compounds and to methods of treatment using them.
摘要翻译：本发明涉及式（I）的化合物：含有这些化合物的药物组合物和使用它们的治疗方法。

7. 发明授权

US07067512B2 Substituted 1,4-benzodiazepines and uses thereof 失效
标题翻译：取代的1,4-苯并二氮杂及其用途
公开(公告)号：US07067512B2
公开(公告)日：2006-06-27
申请号：US10292876
申请日：2002-11-13
申请人： Tianbao Lu , Louis V Lafrance, III , Daniel J Parks , Karen L Milkiewicz , Raul R Calvo , Maxwell D Cummings , Alexander J Kim , Bruce L Grasberger , Theodore E Carver, Jr.
发明人： Tianbao Lu , Louis V Lafrance, III , Daniel J Parks , Karen L Milkiewicz , Raul R Calvo , Maxwell D Cummings , Alexander J Kim , Bruce L Grasberger , Theodore E Carver, Jr.
IPC分类号： C07D243/12 , C07D243/18 , C07D243/24 , A61K31/55
CPC分类号： C07D401/04 , C07D243/14 , C07D403/10 , C07D405/04 , C07D409/04
摘要： The present invention is directed to novel 1,4-benzodiazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions. Compounds have Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein: X and Y are independently —C(O)—, —CH2— or —C(S)—; R1, R2, R3, R4, R7, R8, Rb, Rc, Rd and M are defined herein; R5 is hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aralkyl, optionally substituted heteroaralkyl, carboxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, aminocarbonyl, aminocarbonylalkyl, alkylaminocarbonyl or alkylaminocarbonylalkyl; R6 is cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, aralkyl, heteroarylalkyl, or a saturated or partially unsaturated heterocycle, each of which is optionally substituted; R9 is cycloalkyl, aryl, heteroaryl, a saturated or partially unsaturated heterocycle, cycloalkyl(alkyl), aralkyl or heteroarylalkyl, each of which is optionally substituted; and R10 is —(CH2)n—CO2Rb, —(CH2)m—CO2M, —(CH2)i—OH or —(CH2)j—CONRcRd n is 0–8, m is 0–8, i is 1–8 and j is 0–8.
摘要翻译：本发明涉及新的1,4-苯二氮卓类药物，其药物组合物及其作为HDM2-p53相互作用抑制剂的用途。化合物具有式I：或其溶剂合物，水合物或其药学上可接受的盐; 其中：X和Y独立地为-C（O） - ， - CH 2 - 或-C（S） - ; R 1，R 2，R 3，R 4，R 7， R 8，R b，R c，R d和M在本文中定义; R 5是氢，烷基，环烷基，任选取代的芳基，任选取代的杂芳基，任选取代的芳烷基，任选取代的杂芳烷基，羧基烷基，烷氧基羰基，烷氧基羰基烷基，氨基羰基，氨基羰基烷基，烷基氨基羰基或烷基氨基羰基烷基; R 6是环烷基，芳基，杂芳基，环烷基烷基，芳烷基，杂芳基烷基或饱和或部分不饱和的杂环，其各自任选被取代; R 9是环烷基，芳基，杂芳基，饱和或部分不饱和的杂环，环烷基（烷基），芳烷基或杂芳基烷基，其各自任选被取代; 和R 10是 - （CH 2）n - - - - - - （CH 2）n - ， - （CH 2）2 - ， - M 2 - ， - （CH 2） -OH或 - （CH 2 CH 2）n -CONR C n R n为0-8 ，m为0-8，i为1-8，j为0-8。

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