公开(公告)号：US07888345B2

公开(公告)日：2011-02-15

申请号：US12308209

申请日：2007-06-05

申请人： Scott B. Hoyt ,  Clare London ,  Dong Ok ,  William H. Parsons

发明人： Scott B. Hoyt ,  Clare London ,  Dong Ok ,  William H. Parsons

IPC分类号： C07D223/16 ,  A61K31/55 ,  A61P29/02

CPC分类号： C07D223/16 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12

摘要： Benzazepinone compounds represented by Formula (I), or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, urinary incontinence, pruritis, itchiness, allergic dermatitis, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier.

摘要翻译： 由式（I）表示的苯并氮杂酮化合物或其药学上可接受的盐。 药物组合物包含单独的或与一种或多种其它治疗活性化合物组合的有效量的本发明化合物和药学上可接受的载体。 治疗与钠通道活性相关或由其引起的症状的方法，包括例如急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛，癫痫，肠易激综合征，尿失禁，瘙痒，瘙痒，过敏性皮炎 抑郁，焦虑，多发性硬化和双相性精神障碍，包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物组合施用。 施用局部麻醉的方法包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物和药学上可接受的载体组合施用。

公开(公告)号：US20090181946A1

公开(公告)日：2009-07-16

申请号：US12308209

申请日：2007-06-05

申请人： Scott B. Hoyt ,  Clare London ,  Dong Ok ,  William H. Parsons

发明人： Scott B. Hoyt ,  Clare London ,  Dong Ok ,  William H. Parsons

IPC分类号： C07D223/16 ,  A61K31/55 ,  A61P29/00

CPC分类号： C07D223/16 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12

摘要： Benzazepinone compounds represented by Formula (I), or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, urinary incontinence, pruritis, itchiness, allergic dermatitis, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier.

摘要翻译： 由式（I）表示的苯并氮杂酮化合物或其药学上可接受的盐。 药物组合物包含单独的或与一种或多种其它治疗活性化合物组合的有效量的本发明化合物和药学上可接受的载体。 治疗与钠通道活性相关或由其引起的症状的方法，包括例如急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛，癫痫，肠易激综合征，尿失禁，瘙痒，瘙痒，过敏性皮炎 抑郁，焦虑，多发性硬化和双相性精神障碍，包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物组合施用。 施用局部麻醉的方法包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物和药学上可接受的载体组合施用。

公开(公告)号：US20100144715A1

公开(公告)日：2010-06-10

申请号：US12528041

申请日：2008-02-25

申请人： Scott B. Hoyt ,  Dong Ok ,  Hyun Ok ,  Clare London ,  Joseph I. Duffy

发明人： Scott B. Hoyt ,  Dong Ok ,  Hyun Ok ,  Clare London ,  Joseph I. Duffy

IPC分类号： A61K31/551 ,  C07D243/12 ,  C07D281/08 ,  A61K31/553 ,  A61K31/554 ,  A61P25/08

CPC分类号： C07D281/10 ,  C07D245/06 ,  C07D267/14

摘要： The present invention is directed to substituted benzodiazepinones, benzoxazepinones and benzothiazepinones compounds that are sodium channel blockers useful for the treatment of chronic and neuropathic pain. The compounds of the present invention are also useful for the treatment of other conditions, including disorders of the CNS such as anxiety, depression, epilepsy, manic depression and bipolar disorder. This invention also provides pharmaceutical compositions comprising a compound of the present invention, either alone, or in combination with one or more therapeutically active compounds, and a pharmaceutically acceptable carrier. This invention further comprises methods for the treatment of acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain and disorders of the CNS including, but not limited to, epilepsy, manic depression, depression, anxiety and bipolar disorder comprising administering the compounds and pharmaceutical compositions of the present invention.

摘要翻译： 本发明涉及用作治疗慢性和神经性疼痛的钠通道阻滞剂的取代苯并二氮杂酮，苯并氧氮杂酮和苯并噻唑酮化合物。 本发明的化合物还可用于治疗其他病症，包括CNS的疾病如焦虑症，抑郁症，癫痫症，躁狂抑郁症和双相性精神障碍。 本发明还提供包含单独的或与一种或多种治疗活性化合物组合的本发明化合物和药学上可接受的载体的药物组合物。 本发明还包括用于治疗急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛和中枢神经系统疾病的方法，包括但不限于癫痫症，躁狂抑郁症，抑郁症，焦虑症和双相性躁动症，包括给予化合物 和本发明的药物组合物。

公开(公告)号：US09073929B2

公开(公告)日：2015-07-07

申请号：US14112945

申请日：2012-04-20

申请人： Scott B. Hoyt ,  Whitney Lane Petrilli ,  Clare London ,  Yusheng Xiong ,  Jerry Andrew Taylor ,  Amjad Ali ,  Michael Man-Chu Lo ,  Timothy J. Henderson ,  Qingzhong Hu ,  Rolf Hartmann ,  Lina Yin ,  Ralf Heim ,  Emmanuel Bey ,  Rohit Saxena ,  Swapan Kumar Samanta ,  Bheemashankar A. Kulkarni

发明人： Scott B. Hoyt ,  Whitney Lane Petrilli ,  Clare London ,  Yusheng Xiong ,  Jerry Andrew Taylor ,  Amjad Ali ,  Michael Man-Chu Lo ,  Timothy J. Henderson ,  Qingzhong Hu ,  Rolf Hartmann ,  Lina Yin ,  Ralf Heim ,  Emmanuel Bey ,  Rohit Saxena ,  Swapan Kumar Samanta ,  Bheemashankar A. Kulkarni

IPC分类号： C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  A61K31/41 ,  A61K45/06

CPC分类号： C07D487/04 ,  A61K31/41 ,  A61K45/06 ,  C07D471/04 ,  C07D519/00 ,  A61K2300/00

摘要： This invention relates to tricyclic triazole analogs of the formula I or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthetase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthetase.

摘要翻译： 本发明涉及式I的三环三唑类似物或其药学上可接受的盐，其中该变量在本文中定义。 本发明化合物选择性地抑制醛固酮合成酶。 本发明还提供包含式I化合物或其盐的药物组合物，以及用于治疗，改善或预防可通过抑制醛固酮合成酶治疗的病症的方法。

公开(公告)号：US20140045819A1

公开(公告)日：2014-02-13

申请号：US14112945

申请日：2012-04-20

申请人： Scott B. Hoyt ,  Whitney Lane Petrilli ,  Clare London ,  Yusheng Xiong ,  Jerry Andrew Taylor ,  Amjad Ali ,  Michael Man-Chu Lo ,  Timothy J. Henderson ,  Qingzhong Hu ,  Rolf Hartmann ,  Lina Yin ,  Ralf Heim ,  Emmanuel Bey ,  Rohit Saxena ,  Swapan Kumar Samanta ,  Bheemashankar A. Kulkarni

发明人： Scott B. Hoyt ,  Whitney Lane Petrilli ,  Clare London ,  Yusheng Xiong ,  Jerry Andrew Taylor ,  Amjad Ali ,  Michael Man-Chu Lo ,  Timothy J. Henderson ,  Qingzhong Hu ,  Rolf Hartmann ,  Lina Yin ,  Ralf Heim ,  Emmanuel Bey ,  Rohit Saxena ,  Swapan Kumar Samanta ,  Bheemashankar A. Kulkarni

IPC分类号： C07D487/04 ,  C07D471/04

CPC分类号： C07D487/04 ,  A61K31/41 ,  A61K45/06 ,  C07D471/04 ,  C07D519/00 ,  A61K2300/00

摘要： This invention relates to tricyclic triazole analogues of the formula I or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthetase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthetase.

摘要翻译： 本发明涉及式I的三环三唑类似物或其药学上可接受的盐，其中该变量在本文中定义。 本发明化合物选择性地抑制醛固酮合成酶。 本发明还提供包含式I化合物或其盐的药物组合物，以及用于治疗，改善或预防可通过抑制醛固酮合成酶治疗的病症的方法。

公开(公告)号：US20130317057A1

公开(公告)日：2013-11-28

申请号：US13811059

申请日：2011-07-20

申请人： Scott B. Hoyt ,  Min K. Park ,  Clare London ,  Yusheng Xiong ,  D. Jonathan Bennett ,  Jaiqiang Cai ,  Paul Ratcliffe ,  Andrew Cooke ,  Emma Carswell ,  John MacLean ,  Rohit Saxena ,  Bheemashankar A. Kulkarni ,  Archana Gupta

发明人： Scott B. Hoyt ,  Min K. Park ,  Clare London ,  Yusheng Xiong ,  D. Jonathan Bennett ,  Jaiqiang Cai ,  Paul Ratcliffe ,  Andrew Cooke ,  Emma Carswell ,  John MacLean ,  Rohit Saxena ,  Bheemashankar A. Kulkarni ,  Archana Gupta

IPC分类号： C07D401/04 ,  C07D413/14 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/4439 ,  C07D471/04

CPC分类号： C07D401/04 ,  A61K31/4184 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/4709 ,  C07D413/14 ,  C07D471/04

摘要： The invention involves compounds of structural Formula (I) and the pharmaceutically acceptable salts thereof. The compounds of the invention are effective at selectively inhibiting CYP11B2, and are therefore useful for the treatment or prophylaxis of disorders that are associated with elevated aldosterone levels, including, but not limited to, hypertension and heart failure.

摘要翻译： 本发明涉及结构式（I）的化合物及其药学上可接受的盐。 本发明的化合物对选择性抑制CYP11B2有效，因此可用于治疗或预防与升高的醛固酮水平相关的病症，包括但不限于高血压和心力衰竭。

公开(公告)号：US09351973B2

公开(公告)日：2016-05-31

申请号：US14346518

申请日：2012-09-17

申请人： D. Jonathan Bennett ,  Jaiqiang Cai ,  Emma Carswell ,  Andrew Cooke ,  Scott B. Hoyt ,  Clare London ,  John MacLean ,  Min K. Park ,  Paul Ratcliffe ,  Yusheng Xiong ,  Swapan Kumar Samanta ,  Bheemashankar A. Kulkarni

发明人： D. Jonathan Bennett ,  Jaiqiang Cai ,  Emma Carswell ,  Andrew Cooke ,  Scott B. Hoyt ,  Clare London ,  John MacLean ,  Min K. Park ,  Paul Ratcliffe ,  Yusheng Xiong ,  Swapan Kumar Samanta ,  Bheemashankar A. Kulkarni

IPC分类号： C07D471/04 ,  A61K31/437 ,  C07D487/04 ,  A61K31/519 ,  A61P9/12 ,  A61P13/12 ,  A61P9/00 ,  A61P9/10 ,  A61P1/16

CPC分类号： A61K31/519 ,  A61K31/437 ,  A61K31/444 ,  C07D471/04 ,  C07D487/04

摘要： This invention relates to pyrazolopyridyl compounds of the structural formula: or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.

摘要翻译： 本发明涉及以下结构式的吡唑并吡啶基化合物或其药学上可接受的盐，其中该变量在本文中定义。 本发明化合物选择性地抑制醛固酮合酶。 本发明还提供包含式I化合物或其盐的药物组合物，以及潜在的治疗，改善或预防可通过抑制醛固酮合酶治疗的病症的方法。

公开(公告)号：US09173873B2

公开(公告)日：2015-11-03

申请号：US14346403

申请日：2012-09-17

申请人： Amjad Ali ,  D. Jonathan Bennett ,  Jaiqiang Cai ,  Emma Carswell ,  Andrew Cooke ,  Scott B. Hoyt ,  Michael Lo ,  Clare London ,  John MacLean ,  Min K. Park ,  Paul Ratcliffe ,  Jerry Andrew Taylor ,  Brent Whitehead ,  Yusheng Xiong

发明人： Amjad Ali ,  D. Jonathan Bennett ,  Jaiqiang Cai ,  Emma Carswell ,  Andrew Cooke ,  Scott B. Hoyt ,  Michael Lo ,  Clare London ,  John MacLean ,  Min K. Park ,  Paul Ratcliffe ,  Jerry Andrew Taylor ,  Brent Whitehead ,  Yusheng Xiong

IPC分类号： A61K31/437 ,  C07D471/04 ,  C07D487/04

摘要： This invention relates to imidazopyridyl compounds of the structural formula: I or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.

公开(公告)号：US20100216815A1

公开(公告)日：2010-08-26

申请号：US12678357

申请日：2008-09-30

申请人： Joseph L. Duffy ,  Scott B. Hoyt ,  Clare London

发明人： Joseph L. Duffy ,  Scott B. Hoyt ,  Clare London

IPC分类号： A61K31/497 ,  C07D403/14 ,  A61K31/506 ,  C07D239/42 ,  C07D401/04 ,  A61K31/4439 ,  C07D241/20 ,  C07D403/04 ,  A61K31/4178 ,  C07D249/14 ,  A61K31/427 ,  A61P29/00 ,  A61P25/08

CPC分类号： C07D403/14 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04

摘要： A series of N-substituted oxindole derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.

公开(公告)号：US20100204247A1

公开(公告)日：2010-08-12

申请号：US12678820

申请日：2008-09-30

申请人： Joseph L. Duffy ,  Scott B. Hoyt ,  Clare London ,  Christian P. Stevenson

发明人： Joseph L. Duffy ,  Scott B. Hoyt ,  Clare London ,  Christian P. Stevenson

IPC分类号： A61K31/506 ,  A61K31/4439 ,  A61P25/08 ,  A61K31/4196

CPC分类号： A61K31/405

摘要： A series of N-substituted oxindole derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.

摘要翻译： 一系列由式I表示的N-取代的羟基吲哚衍生物或其药学上可接受的盐。 药物组合物包含单独的或与一种或多种其它治疗活性化合物组合的有效量的本发明化合物和药学上可接受的载体。 治疗与钙通道活性相关或由其引起的疾病的方法，包括例如急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛，尿失禁，瘙痒，过敏性皮炎，癫痫，糖尿病性神经病，肠易激综合征 综合征，抑郁症，焦虑症，多发性硬化症，睡眠障碍，双相性精神障碍和中风，包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物组合施用。