公开(公告)号：US20150274672A1

公开(公告)日：2015-10-01

申请号：US14434524

申请日：2013-10-11

Applicant: Mariappan CHELLIAH ,  Hong Dong CHU ,  Jason M. COX ,  John S. DEBENHAM ,  Keith EAGEN ,  Ping LAN ,  Clare LONDON ,  Michael A. PLOTKIN ,  Unmesh SHAH ,  Christopher Joseph SINZ ,  Zhongxiang SUN ,  Henry M. VACCARO ,  Skikanth KATRAMAN ,  MERCK SHARP & DOHME CORP.

Inventor： Mariappan Chelliah ,  Hong Dong Chu ,  Jason M. Cox ,  John S. Debenham ,  Keith Eagen ,  Ping Lan ,  Clare London ,  Michael A. Plotkin ,  Unmesh Shah ,  Christopher Joseph Sinz ,  Zhongxiang Sun ,  Henry M. Vaccaro ,  Srikanth Venkatraman

IPC: C07D221/20 ,  C07D401/04 ,  C07D491/107 ,  C07D405/10

CPC classification number: C07D221/20 ,  C07D401/04 ,  C07D401/12 ,  C07D405/10 ,  C07D491/107

Abstract: The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing diabetes, hyperlipidemia, obesity, inflammation related disorders, and related diseases and conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR120. Pharmaceutical compositions and methods of treatment are also included.

Abstract translation: 本发明涉及由式（I）表示的化合物及其药学上可接受的盐，其可用于治疗或预防糖尿病，高脂血症，肥胖，炎症相关疾病及相关疾病和病症。 该化合物可用作G蛋白偶联受体GPR120的激动剂。 还包括药物组合物和治疗方法。

公开(公告)号：US20100216815A1

公开(公告)日：2010-08-26

申请号：US12678357

申请日：2008-09-30

Applicant: Joseph L. Duffy ,  Scott B. Hoyt ,  Clare London

Inventor： Joseph L. Duffy ,  Scott B. Hoyt ,  Clare London

IPC: 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 classification number: C07D403/14 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04

Abstract: 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

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

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

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

CPC classification number: A61K31/405

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20100144715A1

公开(公告)日：2010-06-10

申请号：US12528041

申请日：2008-02-25

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

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

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

CPC classification number: C07D281/10 ,  C07D245/06 ,  C07D267/14

Abstract: 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.

Abstract translation: 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：US20090181946A1

公开(公告)日：2009-07-16

申请号：US12308209

申请日：2007-06-05

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

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

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

CPC classification number: C07D223/16 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12

Abstract: 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.

Abstract translation: 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：US07101892B2

公开(公告)日：2006-09-05

申请号：US10845847

申请日：2004-05-14

Applicant: Sylvie Bourrain ,  Peter Alan Hunt ,  Ian Thomas Huscroft ,  Janusz Jozef Kulagowski ,  Clare London ,  Elizabeth Mary Naylor ,  Piotr Antoni Raubo ,  Eileen Mary Seward

Inventor： Sylvie Bourrain ,  Peter Alan Hunt ,  Ian Thomas Huscroft ,  Janusz Jozef Kulagowski ,  Clare London ,  Elizabeth Mary Naylor ,  Piotr Antoni Raubo ,  Eileen Mary Seward

IPC: A61K31/44

CPC classification number: C07D241/38 ,  C07D207/06 ,  C07D207/16 ,  C07D209/44 ,  C07D209/52 ,  C07D209/60 ,  C07D209/62 ,  C07D211/14 ,  C07D211/18 ,  C07D211/22 ,  C07D211/28 ,  C07D211/32 ,  C07D211/60 ,  C07D211/70 ,  C07D217/04 ,  C07D233/04 ,  C07D295/084 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04 ,  C07D487/08

Abstract: The present invention relates to sulfone derivatives of formula (I): Ar—SO2—CR2R3-L-N(R1)2I wherein Ar, L, R1, R2 and R3 are as defined herein, and pharmaceutically acceptable salts and N-oxides thereof, useful in the treatment of a condition which is susceptible to treatment by modulation of 5-HT7 receptor activity, such as depression or a sleep disorder.

Abstract translation: 本发明涉及式（I）的砜衍生物：<？in-line-formula description =“In-line Formulas”end =“lead”→Ar-SO 2 -CR > 2 3 其中Ar，L，R 1，R 2和R 3如本文所定义，并且药学上可接受的是式 可接受的盐和N-氧化物，其可用于治疗通过调节5-HT 7受体活性（例如抑郁症或睡眠障碍）进行治疗的病症。

公开(公告)号：US09549921B2

公开(公告)日：2017-01-24

申请号：US14897966

申请日：2014-06-19

Applicant: Shuwen He ,  Zhong Lai ,  Xing Dai ,  Dong Xiao ,  Clare London ,  Nicolas Zorn ,  Ravi Nargund ,  Anandan Palani ,  Casey C. McComas ,  Peng Li ,  Xuanjia Peng ,  Richard Soll

Inventor： Shuwen He ,  Zhong Lai ,  Xing Dai ,  Dong Xiao ,  Clare London ,  Nicolas Zorn ,  Ravi Nargund ,  Anandan Palani ,  Casey C. McComas ,  Peng Li ,  Xuanjia Peng ,  Richard Soll

IPC: A61K31/454 ,  C07D487/04 ,  A61K31/498 ,  A61K31/4525 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/55 ,  A61K31/502 ,  A61K31/423 ,  A61K31/404 ,  A61K45/06 ,  C07D413/14 ,  C07D498/04 ,  C07D471/04 ,  C07D405/04 ,  C07D417/14 ,  C07D405/14 ,  C07D513/04 ,  C07D495/04

CPC classification number: A61K31/454 ,  A61K31/404 ,  A61K31/423 ,  A61K31/4525 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/498 ,  A61K31/502 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D405/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  A61K2300/00

Abstract: The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.(I)

Abstract translation: 本发明涉及可用作丙型肝炎病毒（HCV）NS5B聚合酶抑制剂，这种化合物的合成以及这些化合物用于抑制HCV NS5B聚合酶活性用于治疗或预防HCV感染的用途的式I化合物和 抑制基于细胞的系统中的HCV病毒复制和/或病毒生产（I）

公开(公告)号：US09351973B2

公开(公告)日：2016-05-31

申请号：US14346518

申请日：2012-09-17

Applicant: 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

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

CPC classification number: A61K31/519 ,  A61K31/437 ,  A61K31/444 ,  C07D471/04 ,  C07D487/04

Abstract: 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.

Abstract translation: 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：US09265773B2

公开(公告)日：2016-02-23

申请号：US14343450

申请日：2012-08-20

Applicant: Casey C. McComas ,  Nigel J. Liverton ,  Joerg Habermann ,  Uwe Koch ,  Frank Narjes ,  Peng Li ,  Xuanjia Peng ,  Richard Soll ,  Hao Wu ,  Anandan Palani ,  Shuwen He ,  Xing Dai ,  Hong Liu ,  Zhong Lai ,  Clare London ,  Dong Xiao ,  Nicolas Zorn ,  Ravi Nargund

Inventor： Casey C. McComas ,  Nigel J. Liverton ,  Joerg Habermann ,  Uwe Koch ,  Frank Narjes ,  Peng Li ,  Xuanjia Peng ,  Richard Soll ,  Hao Wu ,  Anandan Palani ,  Shuwen He ,  Xing Dai ,  Hong Liu ,  Zhong Lai ,  Clare London ,  Dong Xiao ,  Nicolas Zorn ,  Ravi Nargund

IPC: A61K31/553 ,  C07D491/052 ,  A61K31/519 ,  A61K31/407 ,  C07D498/22 ,  A61K31/437 ,  C07D491/147 ,  C07D498/14 ,  C07D498/04 ,  A61K31/5365 ,  A61K45/06

CPC classification number: A61K31/553 ,  A61K31/407 ,  A61K31/437 ,  A61K31/519 ,  A61K31/5365 ,  A61K45/06 ,  C07D491/052 ,  C07D491/147 ,  C07D498/04 ,  C07D498/14 ,  C07D498/22 ,  Y02A50/387 ,  Y02A50/389 ,  Y02A50/395 ,  A61K2300/00

Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

Abstract translation: 本发明涉及可用作丙型肝炎病毒（HCV）NS5B聚合酶抑制剂，这种化合物的合成以及这些化合物用于抑制HCV NS5B聚合酶活性用于治疗或预防HCV感染的式（I）化合物 并用于在基于细胞的系统中抑制HCV病毒复制和/或病毒生产。

公开(公告)号：US09173873B2

公开(公告)日：2015-11-03

申请号：US14346403

申请日：2012-09-17

Applicant: 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

Inventor： 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: A61K31/437 ,  C07D471/04 ,  C07D487/04

Abstract: 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.