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1. 发明申请

US20110136846A1 Buprenorphine Analogs 有权
标题翻译：丁丙诺啡类似物
公开(公告)号：US20110136846A1
公开(公告)日：2011-06-09
申请号：US13055873
申请日：2009-07-30
申请人： Donald J. Kyle , R. Richard Goehring , Marian E. Fundytus
发明人： Donald J. Kyle , R. Richard Goehring , Marian E. Fundytus
IPC分类号： A61K31/485 , C07D489/00 , A61P25/00
CPC分类号： C07D489/12 , C07D489/02
摘要： The present invention is directed to Buprenorphine Analog compounds of the Formula I, Formula II or Formula III shown below, wherein R1, R2, R8, R3, R3a, R3b, X, Z and Y are as defined herein, R1 H3CO (I) OCH3 OCH3 (III) Compounds of the Invention are useful for treating pain and other conditions modulated by activity of opioid and ORL1 receptors.
摘要翻译：本发明涉及如下所示的式I，式II或式III的丁丙诺啡类似物，其中R1，R2，R8，R3，R3a，R3b，X，Z和Y如本文所定义，R1H3CO（I） OCH 3 OCH 3（III）本发明化合物可用于治疗由阿片样物质和ORL1受体活性调节的疼痛和其它状况。

2. 发明授权

US08530494B2 Buprenophine analogs 有权
标题翻译：丁丙宁类似物
公开(公告)号：US08530494B2
公开(公告)日：2013-09-10
申请号：US13055873
申请日：2009-07-30
申请人： Donald J. Kyle , R. Richard Goehring , Marian E. Fundytus
发明人： Donald J. Kyle , R. Richard Goehring , Marian E. Fundytus
IPC分类号： A61K31/485 , C07D489/12
CPC分类号： C07D489/12 , C07D489/02
摘要： The present invention is directed to Buprenorphine Analog compounds of the Formula I, Formula II or Formula III shown below, wherein R1, R2, R8, R3, R3a, R3b, X, Z and Y are as defined herein. Compounds of the Invention are useful for treating pain and other conditions modulated by activity of opioid and ORL1 receptors.
摘要翻译：本发明涉及如下所示的式I，式II或式III的丁丙诺啡类似物，其中R1，R2，R8，R3，R3a，R3b，X，Z和Y如本文所定义。本发明的化合物可用于治疗由阿片样物质和ORL1受体的活性调节的疼痛和其它状况。

3. 发明授权

US07229993B2 Aryl substituted pyrimidines and the use thereof 有权
标题翻译：芳基取代的嘧啶及其用途
公开(公告)号：US07229993B2
公开(公告)日：2007-06-12
申请号：US10386483
申请日：2003-03-13
申请人： R. Richard Goehring , Sam F. Victory , Donald J. Kyle
发明人： R. Richard Goehring , Sam F. Victory , Donald J. Kyle
IPC分类号： C07D237/02 , C07D239/02 , A01N43/58 , A61K31/50
CPC分类号： C07D239/42 , C07D239/47
摘要： This invention relates to a method of treating disorders responsive to the blockade of sodium ion channels using novel aryl-substituted pyrimidine compounds of Formula I: or a pharmaceutically acceptable salt, or solvate thereof, wherein A, R1, R2, R3 and R4 are defined in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
摘要翻译：本发明涉及使用新的式I的芳基取代嘧啶化合物或其药学上可接受的盐或溶剂化物来治疗对钠离子通道阻断有反应的病症的方法，其中A，R 1，在说明书中定义了R 2，R 3和R 4。本发明还涉及式I化合物用于治疗全身和局部缺血后的神经元损伤，用于治疗或预防神经变性疾病如肌萎缩性侧索硬化（ALS）以及治疗，预防或改善的用途作为抗惊厥剂，作为抗惊厥剂，作为抗躁狂抑制剂，作为局部麻醉剂，作为抗心律失常药物和用于治疗或预防糖尿病性神经病变。

4. 发明授权

US09045435B2 Quinazoline compounds as sodium channel blockers 有权
标题翻译：喹唑啉化合物作为钠通道阻断剂
公开(公告)号：US09045435B2
公开(公告)日：2015-06-02
申请号：US13878004
申请日：2011-10-05
申请人： R. Richard Goehring , Laykea Tafesse , Jiangchao Yao
发明人： R. Richard Goehring , Laykea Tafesse , Jiangchao Yao
IPC分类号： C07D239/74 , C07D239/84 , A01N43/54 , A61K31/517 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D471/08
CPC分类号： A61K31/517 , C07D239/74 , C07D239/84 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D471/08
摘要： The invention relates to aryl substituted quinazolines of Formula I, and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein G, A, and R1-R4 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
摘要翻译：本发明涉及式I的芳基取代喹唑啉及其药学上可接受的盐，前药或溶剂化物，其中G，A和R 1 -R 4如说明书所述定义。本发明还涉及式I化合物用于治疗对钠通道阻断有反应的病症。本发明的化合物特别适用于治疗疼痛。

5. 发明授权

US08846929B2 Substituted-quinoxaline-type piperidine compounds and the uses thereof 有权
标题翻译：取代的喹喔啉型哌啶化合物及其用途
公开(公告)号：US08846929B2
公开(公告)日：2014-09-30
申请号：US12712042
申请日：2010-02-24
申请人： Kouki Fuchino , R. Richard Goehring , Bin Shao , Yoshiyuki Taoda , Naoki Tsuno , John William Frank Whitehead , Jiangchao Yao
发明人： Kouki Fuchino , R. Richard Goehring , Bin Shao , Yoshiyuki Taoda , Naoki Tsuno , John William Frank Whitehead , Jiangchao Yao
IPC分类号： C07D295/00
CPC分类号： C07D451/14 , A61K31/498 , C07D401/04 , C07D401/14 , C07D451/04 , C07D471/08 , C07D471/14 , C07D487/04 , C07D498/08 , C07D519/00
摘要： The invention relates to Substituted-Quinoxaline-Type Piperidine Compounds, compositions comprising an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound.
摘要翻译：本发明涉及取代的喹喔啉型哌啶化合物，包含有效量的取代的喹喔啉型哌啶化合物的组合物和治疗或预防诸如疼痛的病症的方法，包括向有需要的动物施用有效量的取代的喹喔啉型哌啶化合物。

6. 发明申请

US20100048626A1 Aryl Substituted Pyridines and the Use Thereof 有权
标题翻译：芳基取代的吡啶类及其用途
公开(公告)号：US20100048626A1
公开(公告)日：2010-02-25
申请号：US12546572
申请日：2009-08-24
申请人： Bin SHAO , R. Richard Goehring , Samuel F. Victory , Qun Sun
发明人： Bin SHAO , R. Richard Goehring , Samuel F. Victory , Qun Sun
IPC分类号： A61K31/4545 , C07D401/12 , C07D213/56 , A61K31/4418 , A61P25/00 , G01N33/00
CPC分类号： C07D213/81 , C07D213/82 , Y10T436/145555
摘要： This invention relates aryl substituted pyridines of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Ar and R1-R4 are set in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
摘要翻译：本发明涉及式I的芳基取代的吡啶：或其药学上可接受的盐，前药或溶剂化物，其中Ar和R 1 -R 4被置于说明书中。本发明还涉及式I化合物用于治疗全身和局部缺血后的神经元损伤，用于治疗或预防神经变性疾病如肌萎缩性侧索硬化（ALS）以及治疗，预防或改善的用途作为抗惊厥剂，作为抗惊厥剂，作为抗躁狂抑制剂，作为局部麻醉剂，作为抗心律失常药物和用于治疗或预防糖尿病性神经病变。

7. 发明授权

US07456198B2 Benzimidazole compounds having nociceptin receptor affinity 有权
标题翻译：具有伤害感受器受体亲和力的苯并咪唑化合物
公开(公告)号：US07456198B2
公开(公告)日：2008-11-25
申请号：US09730934
申请日：2000-12-06
申请人： Donald Kyle , R. Richard Goehring , Bin Shao
发明人： Donald Kyle , R. Richard Goehring , Bin Shao
IPC分类号： A61K31/44 , C07D211/32
CPC分类号： C07D401/04
摘要： Disclosed are compounds of the formula (I) wherein A, R1, R2, R3, R4 and X1 are as disclosed herein. The compounds have affinity for the ORL1 receptor and are useful in the treatment of chronic and acute pain.
摘要翻译：公开了式（I）的化合物，其中A，R 1，R 2，R 3，R 4， >和X 1'如本文所公开的。该化合物对ORL1受体具有亲和力，可用于治疗慢性和急性疼痛。

8. 发明授权

US07105549B2 Aryl substituted pyridines and the use thereof 有权
标题翻译：芳基取代的吡啶及其用途
公开(公告)号：US07105549B2
公开(公告)日：2006-09-12
申请号：US10235673
申请日：2002-09-06
申请人： Bin Shao , R. Richard Goehring , Samuel F Victory , Qun Sun
发明人： Bin Shao , R. Richard Goehring , Samuel F Victory , Qun Sun
IPC分类号： A61K31/443 , A61K31/4439 , A61K31/451 , C07D213/60 , C07D401/04 , C07D405/04 , C07D413/04
CPC分类号： C07D213/81 , C07D213/82 , Y10T436/145555
摘要： This invention relates aryl substituted pyridines of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Ar and R1–R4 are set in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
摘要翻译：本发明涉及式I的芳基取代的吡啶：或其药学上可接受的盐，前药或溶剂化物，其中Ar和R 1 -R 4定义在说明书中。本发明还涉及式I化合物用于治疗全身和局部缺血后的神经元损伤，用于治疗或预防神经变性疾病如肌萎缩性侧索硬化（ALS）以及治疗，预防或改善的用途作为抗惊厥剂，作为抗惊厥剂，作为抗躁狂抑制剂，作为局部麻醉剂，作为抗心律失常药物和用于治疗或预防糖尿病性神经病变。

9. 发明授权

US06541477B2 Inhibitors of p38-a kinase 有权
标题翻译： p38-a激酶抑制剂
公开(公告)号：US06541477B2
公开(公告)日：2003-04-01
申请号：US09796997
申请日：2001-02-28
申请人： R. Richard Goehring , Babu J. Mavunkel , David Y. Liu , George F. Schreiner , Gregory Leudtke , John A. Lewicki
发明人： R. Richard Goehring , Babu J. Mavunkel , David Y. Liu , George F. Schreiner , Gregory Leudtke , John A. Lewicki
IPC分类号： A61K31495
CPC分类号： C07D215/04 , A61K31/00 , A61K31/426 , A61K31/445 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/495 , A61K31/496 , A61K31/522 , A61K31/5377 , A61K45/06 , C07D209/08 , C07D211/14 , C07D211/16 , C07D215/06 , C07D235/06 , C07D277/52 , C07D295/192 , C07D307/68 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/06 , C07D471/04 , C07D471/10 , C07D473/06 , C07D495/04
摘要： The invention is directed to methods for treating conditions mediated by by P38&agr; kinase using compounds of the formula wherein Ar1 and Ph are limited to specific embodiments or wherein the compound of formula (3) is a compound set forth in FIGS. 1A-1T.
摘要翻译：本发明涉及用于治疗由P38α激酶介导的病症的方法，其中使用化学式Ar1和Ph的化合物限于具体实施方案或其中式（3）化合物是图1和图2所示的化合物。 1A-1T。

10. 发明授权

US08637502B2 2,3,4,5-tetrahydro-benzo{B}{1,4}diazepine-comprising compounds of formula(III) for treating pain 有权
标题翻译： 2,3,4,5-四氢 - 苯并{B} {1,4}二氮杂的式（Ⅳ）化合物
公开(公告)号：US08637502B2
公开(公告)日：2014-01-28
申请号：US13349522
申请日：2012-01-12
申请人： Kevin C. Brown , R. Richard Goehring
发明人： Kevin C. Brown , R. Richard Goehring
IPC分类号： A61K31/55
CPC分类号： C07D401/04 , C07D451/14 , C07D471/04 , C07D471/08
摘要： The invention relates to Heterocyclic-Substituted Piperidine Compounds, compositions comprising an effective amount of a Heterocyclic-Substituted Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Heterocyclic-Substituted Piperidine Compound.
摘要翻译：本发明涉及杂环取代的哌啶化合物，包含有效量的杂环取代的哌啶化合物的组合物和治疗或预防诸如疼痛的病症的方法，包括向有需要的动物施用有效量的杂环 - 取代哌啶化合物。

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