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61. 发明授权

US08367684B2 Derivatives of 4-(N-azacycloalkyl) anilides as potassium channel modulators 有权
标题翻译： 4-（N-氮杂环烷基）苯胺的衍生物作为钾通道调节剂
公开(公告)号：US08367684B2
公开(公告)日：2013-02-05
申请号：US12138251
申请日：2008-06-12
申请人： Jean-Michel Vernier , Samedy Ouk , Martha A. De La Rosa
发明人： Jean-Michel Vernier , Samedy Ouk , Martha A. De La Rosa
IPC分类号： A01N43/54 , A61K31/505
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D471/04
摘要： This invention provides potassium channel modulators which are compounds of formula I where at least one of W and Z is N; where the moiety is one of Groups A or B below A where Ar is a 1,2-fused, six membered ring aromatic group, bearing substituents R1 and R2 as defined below, and containing zero or one ring nitrogen atom; and where other substituents are defined herein. The invention also provides a composition comprising a pharmaceutically acceptable carrier and at least one of the following: i) a pharmaceutically effective amount of a compound of formula I and ii) a pharmaceutically acceptable salt, ester, or prodrug thereof. The invention also provides a method of preventing or treating a disease or disorder which is affected by activities of potassium channels, comprising administering to a patient in need thereof a therapeutically effective amount of a compound of formula I or a salt, ester, or prodrug thereof.
摘要翻译：本发明提供钾通道调节剂，其为W和Z中至少一个为N的式I化合物; 其中该部分是A之下的A或B族之一，其中Ar是1,2-稠合的六元环芳族基团，带有如下定义的取代基R 1和R 2，并且含有一个或多个环氮原子; 并且其中其它取代基在本文中定义。本发明还提供包含药学上可接受的载体和至少一种以下的组合物：i）药学有效量的式I化合物和ii）其药学上可接受的盐，酯或前药。本发明还提供了预防或治疗受钾通道活性影响的疾病或病症的方法，包括向有需要的患者施用治疗有效量的式I化合物或其盐，酯或前药。

62. 发明申请

US20120107307A1 DIHYDROPYRIDIN SULFONAMIDES AND DIHYDROPYRIDIN SULFAMIDES AS MEK INHIBITORS 有权
标题翻译：二氢吡啶磺酸盐和二羟基吡啶磺酸盐作为MEK抑制剂
公开(公告)号：US20120107307A1
公开(公告)日：2012-05-03
申请号：US13259239
申请日：2010-03-23
申请人： Jean-Michel Vernier , Hong Woo Kim , Marion Hitchcock , Shunqi Yan
发明人： Jean-Michel Vernier , Hong Woo Kim , Marion Hitchcock , Shunqi Yan
IPC分类号： A61K31/4412 , A61P35/00 , A61K31/573 , A61K31/565 , A61K31/475 , A61K31/704 , A61K38/14 , A61K31/7048 , A61K31/664 , A61K31/513 , A61K31/7068 , A61K31/7076 , A61K31/522 , A61K33/24 , A61K39/395 , A61K31/519 , A61K31/69 , C07D213/76
CPC分类号： C07D213/76
摘要： This invention concerns N-(ortho phenylamino dihydropyridyl)sulfonamides and N-(ortho phenylamino dihydropyridyl), N′-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.
摘要翻译：本发明涉及作为MEK抑制剂的N-（邻苯基氨基二氢吡啶基）磺酰胺和N-（邻苯基氨基二氢吡啶基），N'-烷基磺酰胺，可用于治疗癌症和其它过度增生性疾病。

63. 发明授权

US08101799B2 Derivatives of N-(arylamino) sulfonamides as inhibitors of MEK 有权
标题翻译： N-（芳基氨基）磺酰胺的衍生物作为MEK的抑制剂
公开(公告)号：US08101799B2
公开(公告)日：2012-01-24
申请号：US11830733
申请日：2007-07-30
申请人： Andreas Maderna , Jean-Michel Vernier , Dinesh Barawkar , Varaprasad Chamakura , Hassan El Abdellaoui , Zhi Hong
发明人： Andreas Maderna , Jean-Michel Vernier , Dinesh Barawkar , Varaprasad Chamakura , Hassan El Abdellaoui , Zhi Hong
IPC分类号： C07C307/00 , A61K31/18
CPC分类号： C07D417/04 , A61K31/18 , A61K31/34 , A61K31/381 , A61K31/40 , A61K31/415 , A61K31/4164 , A61K31/42 , A61K31/426 , A61K31/433 , A61K31/4406 , A61K31/4409 , A61K31/495 , A61K31/496 , A61K45/06 , C07B2200/07 , C07C311/08 , C07C311/09 , C07C311/10 , C07C311/14 , C07C311/21 , C07C311/28 , C07C311/29 , C07C311/32 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D207/36 , C07D211/54 , C07D213/38 , C07D213/42 , C07D231/12 , C07D231/18 , C07D233/84 , C07D261/10 , C07D277/36 , C07D277/54 , C07D285/04 , C07D295/088 , C07D295/13 , C07D307/64 , C07D333/34
摘要： This invention concerns N—(2-arylamino) aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.
摘要翻译：本发明涉及作为MEK抑制剂的N-（2-芳基氨基）芳基磺酰胺，可用于治疗癌症和其它过度增生性疾病。

64. 发明授权

US07842836B2 N-aryl-N'alkyl sulfamides as MEK inhibitors 有权
标题翻译： N-芳基-N'-烷基磺酰胺作为MEK抑制剂
公开(公告)号：US07842836B2
公开(公告)日：2010-11-30
申请号：US11734234
申请日：2007-04-11
申请人： Shunqi Yan , Jean-Michel Vernier , Zhi Hong
发明人： Shunqi Yan , Jean-Michel Vernier , Zhi Hong
IPC分类号： C07C331/00 , A61K31/10
CPC分类号： C07C307/10 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D317/28
摘要： This invention concerns N-(ortho phenylaminoaryl), N′-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.
摘要翻译：本发明涉及作为MEK抑制剂的N-（邻苯基氨基芳基），N'-烷基磺酰胺，可用于治疗癌症和其它过度增生性疾病。

65. 发明授权

US07759518B2 Derivatives of N-(arylamino) sulfonamides as inhibitors of MEK 有权
标题翻译： N-（芳基氨基）磺酰胺的衍生物作为MEK的抑制剂
公开(公告)号：US07759518B2
公开(公告)日：2010-07-20
申请号：US12323279
申请日：2008-11-25
申请人： Andreas Maderna , Jean-Michel Vernier , Dinesh Barawkar , Varaprasad Chamakura , Hassan el Abdellaoui , Zhi Hong
发明人： Andreas Maderna , Jean-Michel Vernier , Dinesh Barawkar , Varaprasad Chamakura , Hassan el Abdellaoui , Zhi Hong
IPC分类号： C07C307/06 , A61K31/63
CPC分类号： C07D417/04 , A61K31/18 , A61K31/34 , A61K31/381 , A61K31/40 , A61K31/415 , A61K31/4164 , A61K31/42 , A61K31/426 , A61K31/433 , A61K31/4406 , A61K31/4409 , A61K31/495 , A61K31/496 , A61K45/06 , C07B2200/07 , C07C311/08 , C07C311/09 , C07C311/10 , C07C311/14 , C07C311/21 , C07C311/28 , C07C311/29 , C07C311/32 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D207/36 , C07D211/54 , C07D213/38 , C07D213/42 , C07D231/12 , C07D231/18 , C07D233/84 , C07D261/10 , C07D277/36 , C07D277/54 , C07D285/04 , C07D295/088 , C07D295/13 , C07D307/64 , C07D333/34
摘要： This invention concerns N-(2-arylamino)aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.
摘要翻译：本发明涉及作为MEK抑制剂的N-（2-芳基氨基）芳基磺酰胺，可用于治疗癌症和其它过度增生性疾病。

66. 发明申请

US20100056465A1 COMPOUNDS, COMPOSITIONS AND METHODS OF USING SAME FOR MODULATING URIC ACID LEVELS 有权
公开(公告)号：US20100056465A1
公开(公告)日：2010-03-04
申请号：US12554719
申请日：2009-09-04
申请人： Esmir Gunic , Jean-Luc Girardet , Jean-Michel Vernier , Martina E. Tedder , David A. Paisner
发明人： Esmir Gunic , Jean-Luc Girardet , Jean-Michel Vernier , Martina E. Tedder , David A. Paisner
IPC分类号： A61K31/7076 , C07D249/12 , A61K31/4196 , C07H19/167 , A61P19/06
CPC分类号： C07D249/12 , C07D249/14 , C07D401/04 , C07D405/12 , C07H19/06 , C07H19/10 , C07H19/16
摘要： Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.

67. 发明申请

US20090326059A1 BENZYLOXY ANILIDE DERIVATIVES USEFUL AS POTASSIUM CHANNEL MODULATORS 有权
标题翻译：可用作钾离子通道调节剂的苯并二恶嗪衍生物
公开(公告)号：US20090326059A1
公开(公告)日：2009-12-31
申请号：US12491055
申请日：2009-06-24
申请人： Jim Zhen Wu , Jean-Michel Vernier , Huanming Chen , Jianlan Song
发明人： Jim Zhen Wu , Jean-Michel Vernier , Huanming Chen , Jianlan Song
IPC分类号： A61K31/27 , C07C271/28 , C07C237/02 , A61K31/165 , A61P25/08
CPC分类号： C07C233/25 , C07C233/26 , C07C271/28
摘要： The present invention relates to benzyloxyanilide derivatives having the following structural formula: The compounds of the present invention are useful for the treatment and prevention of diseases and disorders which are affected by activation or modulation of potassium ion channels. One such condition is seizure disorders.
摘要翻译：本发明涉及具有以下结构式的苄氧基苯胺衍生物：本发明化合物可用于治疗和预防受钾离子通道活化或调节影响的疾病和病症。一种这样的病症是癫痫发作。

68. 发明申请

US20090137635A1 DERIVATIVES OF 5-AMINO-4,6-DISUBSTITUTED INDOLE AND 5-AMINO-4,6-DISUBSTITUTED INDOLINE AS POTASSIUM CHANNEL MODULATORS 有权
标题翻译： 5-氨基-4,6-取代的吲哚和5-氨基-4,6-取代的吲哚的衍生物作为钾通道调节剂
公开(公告)号：US20090137635A1
公开(公告)日：2009-05-28
申请号：US12189709
申请日：2008-08-11
申请人： Jean-Michel Vernier , Huanming Chen , Jianlan Song
发明人： Jean-Michel Vernier , Huanming Chen , Jianlan Song
IPC分类号： A61K31/4439 , C07D209/20 , A61K31/404 , C07D401/06
CPC分类号： C07D209/08 , C07D401/06
摘要： This invention provides compounds of formula I where the dashed line represents an optional double bond; where R1 is phenyl, naphthyl, pyridyl, pyrimidyl, pyrrolyl, imidazolyl, pyrazyl, furyl, thienyl, oxazolyl, isoxazolyl, thiazolyl, or isothiazolyl, optionally substituted, and other substituents are defined herein. Such compounds are potassium channel modulators.
摘要翻译：本发明提供式I化合物，其中虚线表示任选的双键; 其中R 1是苯基，萘基，吡啶基，嘧啶基，吡咯基，咪唑基，吡唑基，呋喃基，噻吩基，恶唑基，异恶唑基，噻唑基或异噻唑基，任选取代的，以及其它取代基。这些化合物是钾通道调节剂。

69. 发明申请

US20070287716A1 Pyrimidine and Quinoline Potentiators of Metabotropic Glutamate Receptors 审中-公开
标题翻译：代谢型谷氨酸受体的嘧啶和喹啉电位
公开(公告)号：US20070287716A1
公开(公告)日：2007-12-13
申请号：US11665422
申请日：2005-10-24
申请人： Essa Hu , Jean-Michel Vernier , Peter Chua , John Hutchinson , Nicholas Cosford
发明人： Essa Hu , Jean-Michel Vernier , Peter Chua , John Hutchinson , Nicholas Cosford
IPC分类号： A61K31/47 , A61P25/00 , C07D215/12 , C07D239/28
CPC分类号： C07D239/26 , C07D215/06
摘要： The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
摘要翻译：本发明涉及作为代谢型谷氨酸受体的增强剂（包括mGluR2受体）的化合物，其可用于治疗或预防与谷氨酸能力障碍相关的神经和精神病学障碍以及其中涉及代谢型谷氨酸受体的疾病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。

70. 发明授权

US06194581B1 Substituted pyridines useful as modulators of acetylcholine receptors 失效
标题翻译：取代的吡啶可用作乙酰胆碱受体的调节剂
公开(公告)号：US06194581B1
公开(公告)日：2001-02-27
申请号：US09218214
申请日：1998-12-22
申请人： Nicholas D. Cosford , Jean-Michel Vernier
发明人： Nicholas D. Cosford , Jean-Michel Vernier
IPC分类号： A61K314427
CPC分类号： C07D213/82 , C07D213/38 , C07D213/48 , C07D401/06 , C07F7/0814
摘要： In accordance with the present invention, there is provided a class of pyridine compounds which are modulators of acetylcholine receptors. The compounds of the invention displace acetylcholine receptor ligands from their binding sites. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors, and are useful for a variety of therapeutic applications, such as the treatment of Alzheimer's disease and other disorders involving memory loss and/or dementia (including AIDS dementia); disorders of attention and focus (such as attention deficit disorder); disorders of extrapyramidal motor function such as Parkinson's disease, Huntington's disease, Gilles de la Tourette syndrome and tardive dyskinesia; mood and emotional disorders such as depression, panic, anxiety and psychosis; substance abuse including withdrawal syndromes and substitution therapy; neuroendocrine disorders and dysregulation of food intake, including bulimia and anorexia; disorders of nociception and control of pain; autonomic disorders including dysfunction of gastrointestinal motility and function such as inflammatory bowel disease, irritable bowel syndrome, diarrhea, constipation, gastric acid secretion and ulcers; pheochromocytoma; cardiovascular dysfunction including hypertension and cardia arrhythmias, comedication in surgical procedures, and the like.
摘要翻译：根据本发明，提供了一类作为乙酰胆碱受体调节剂的吡啶化合物。本发明的化合物从其结合位点取代乙酰胆碱受体配体。本发明化合物可用作乙酰胆碱受体的激动剂，部分激动剂，拮抗剂或变构调节剂，并且可用于各种治疗应用，例如治疗阿尔茨海默氏病和涉及记忆丧失和/或痴呆的其它病症（包括AIDS痴呆） ; 注意力集中障碍（如注意力缺陷障碍）; 锥体外系运动功能紊乱，如帕金森病，亨廷顿疾病，吉列斯·杜列特综合征和迟发性运动障碍; 情绪和情绪障碍如抑郁，恐慌，焦虑和精神病; 药物滥用，包括戒断综合征和替代治疗; 神经内分泌障碍和食物摄入异常，包括贪食症和厌食症; 伤害感受障碍和疼痛控制; 自主神经障碍包括胃肠蠕动功能障碍和功能障碍，如炎性肠病，肠易激综合征，腹泻，便秘，胃酸分泌和溃疡; 嗜铬细胞瘤心血管功能障碍，包括高血压和贲门节律不正，外科手术中的喜剧等。

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