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41. 发明申请

US20080096935A1 Heterocyclic Indanone Potentiators of Metabotropic Glutamate Receptors 审中-公开
标题翻译：代谢型谷氨酸受体的杂环茚酮电解质
公开(公告)号：US20080096935A1
公开(公告)日：2008-04-24
申请号：US11666072
申请日：2005-10-21
申请人： Anthony Pinkerton , Jean-Michel Vernier , Rowena Cube , John Hutchinson
发明人： Anthony Pinkerton , Jean-Michel Vernier , Rowena Cube , John Hutchinson
IPC分类号： A61K31/4412 , A61K31/4196 , A61K31/4152
CPC分类号： C07D213/30 , C07D207/32 , C07D213/65 , C07D213/70 , C07D231/12 , C07D235/18 , C07D249/08
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。

42. 发明申请

US20050065340A1 Metabotropic glutamate receptor-5 modulators 失效
标题翻译：代谢型谷氨酸受体-5调节剂
公开(公告)号：US20050065340A1
公开(公告)日：2005-03-24
申请号：US10497452
申请日：2002-11-26
申请人： Jeannie Arruda , Celine Bonnefous , Brian Campbell , Rowena Cube , Benito Munoz , Brian Stearns , Jean-Michel Vernier , Bowei Wang , Xiumin Zhao
发明人： Jeannie Arruda , Celine Bonnefous , Brian Campbell , Rowena Cube , Benito Munoz , Brian Stearns , Jean-Michel Vernier , Bowei Wang , Xiumin Zhao
IPC分类号： C07D263/56 , A61K31/422 , A61K31/423 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/506 , A61K31/5377 , A61K45/00 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/34 , A61P25/36 , A61P29/00 , A61P43/00 , C07D263/57 , C07D413/10 , C07D498/04 , C07D521/00 , C07D471/02 , C07D413/02 , C07D417/02 , C07D43/02
CPC分类号： C07D263/57 , C07D231/12 , C07D233/56 , C07D249/08 , C07D413/10
摘要： Phenyl compounds substituted at the 1-position with a fused bicyclo moeity formed from a five-membered heterocycle fused to a six-membered carbocycle, to a six-membered aryl, or to a six-membered hetaryl, and further optionally substituted at 2 the 3,4 positions, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, and panic, as well as in the treatment of pain and other diseases.
摘要翻译：苯基化合物在1位上被一个稠合的双环形成，由与六元碳环稠合的五元杂环，六元芳基或六元杂芳基形成，并进一步任选地在2位上被取代 3,4位是用于治疗精神病和情绪障碍（例如精神分裂症，焦虑，抑郁和恐慌）以及治疗疼痛和其他疾病的mGluR5调节剂。

43. 发明授权

US06316490B1 Substituted aryl compounds useful as modulators of acetylcholine receptors 失效
标题翻译：可用作乙酰胆碱受体调节剂的取代芳基化合物
公开(公告)号：US06316490B1
公开(公告)日：2001-11-13
申请号：US08860954
申请日：1997-07-08
申请人： Jean-Michel Vernier , Ian A. McDonald
发明人： Jean-Michel Vernier , Ian A. McDonald
IPC分类号： C07D20708
CPC分类号： B64C23/06 , Y02T50/162
摘要： In accordance with the present invention, a novel class of substituted aryl compounds (containing ether, ester, amide, ketone or thioether substitution) that promote the release of ligands involved in neurotransmission have been discovered. In a particular aspect, compounds of the present invention are capable of modulating acetylcholine receptors. The compounds of the present invention are capable of displacing one or more acetylcholine receptor ligands, e.g., 3H-nicotine, from mammalian neuronal membrane binding sites. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors. Therapeutic indications for compounds with activity as acetylcholine receptors include diseases of the central nervous system such as Alzheimer's disease and other diseases involving memory loss and/or dementia (including AIDS dementia); cognitive dysfunction (including disorders of attention, focus and concentration), disorders of extrapyramidal motor function such as Parkinson's disease, progressive supramuscular palsy, Huntington's disease, Gilles de la Tourette syndrome and tardive dyskinesia; mood and emotional disorders such as depression, anxiety and psychosis; substance abuse including withdrawal symptoms and substitution therapy; neurocrine disorders and dysregulation of food intake, including bulimia and anorexia; disorders of nociception and control of pain; autonomic disorders including dysfimction 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 cardiac arrhythmias, as well as co-medication uses in surgical applications.
摘要翻译：根据本发明，已经发现了促进参与神经传递的配体释放的新一类取代的芳基化合物（含有醚，酯，酰胺，酮或硫醚取代基）。在特定方面，本发明的化合物能调节乙酰胆碱受体。本发明的化合物能够从哺乳动物神经元膜结合位点置换一个或多个乙酰胆碱受体配体，例如3H-烟碱。本发明化合物可以充当乙酰胆碱受体的激动剂，部分激动剂，拮抗剂或变构调节剂。具有作为乙酰胆碱受体活性的化合物的治疗适应症包括中枢神经系统的疾病如阿尔茨海默病和涉及记忆丧失和/或痴呆（包括AIDS痴呆）的其它疾病; 认知功能障碍（包括注意力集中和集中注意力障碍），帕特森氏病，锥体运动功能障碍，进行性肌肉麻痹，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，焦虑和精神病; 药物滥用，包括戒断症状和替代治疗; 神经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; 自主神经障碍包括消化道运动功能障碍和功能如炎症性肠病，肠易激综合征，腹泻，便秘，胃酸分泌和溃疡; 嗜铬细胞瘤，包括高血压和心律失常的心血管功能障碍，以及在外科应用中的共用药用途。

44. 发明授权

US10266493B2 Thioacetate compounds, compositions and methods of use 有权
公开(公告)号：US10266493B2
公开(公告)日：2019-04-23
申请号：US13703890
申请日：2011-06-15
申请人： Samedy Ouk , Esmir Gunic , Jean-Michel Vernier , Chixu Chen
发明人： Samedy Ouk , Esmir Gunic , Jean-Michel Vernier , Chixu Chen
IPC分类号： C07D213/70 , A61K31/497 , C07D403/10 , C07D405/10 , A61K31/426 , A61K31/4418 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/4725 , A61K31/4965 , A61K31/519 , A61K31/502 , A61K31/505 , A61K31/506 , C07D417/10 , A61K45/06 , C07D401/10 , C07D417/04 , C07D405/04 , C07D403/04 , C07D401/04 , C07D241/18 , C07D239/38
摘要： Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of 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.

45. 发明授权

US08513443B2 Preparation of (R)-N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide and (S)-N-3,4-difluoro-2(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide 有权
标题翻译：（R）-N-（3,4-二氟-2-（2-氟-4-碘苯基氨基）-6-甲氧基苯基）-1-（2,3-二羟基丙基）环丙烷-1-磺酰胺和（S） -N-3,4-二氟-2（2-氟-4-碘苯基氨基）-6-甲氧基苯基）-1-（2,3-二羟基丙基）环丙烷-1-磺酰胺
公开(公告)号：US08513443B2
公开(公告)日：2013-08-20
申请号：US13386519
申请日：2010-07-10
申请人： Andreas Maderna , Jean-Michel Vernier
发明人： Andreas Maderna , Jean-Michel Vernier
IPC分类号： C07D317/10
CPC分类号： C07C303/38 , C07C317/18 , C07C2601/02 , C07D317/18 , C07D317/26 , C07C311/28
摘要： The present invention relates to the preparation of (R)—N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide and (S)—N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide.
摘要翻译：本发明涉及制备（R）-N-（3,4-二氟-2-（2-氟-4-碘苯基氨基）-6-甲氧基苯基）-1-（2,3-二羟基丙基）环丙烷-1 - 磺酰胺和（S）-N-（3,4-二氟-2-（2-氟-4-碘苯基氨基）-6-甲氧基苯基）-1-（2,3-二羟丙基）环丙烷-1-磺酰胺。

46. 发明申请

US20130202573A1 THIOACETATE COMPOUNDS, COMPOSITIONS AND METHODS OF USE 审中-公开
标题翻译：硫酸化合物，组合物和使用方法
公开(公告)号：US20130202573A1
公开(公告)日：2013-08-08
申请号：US13703890
申请日：2011-06-15
申请人： Samedy Ouk , Esmir Gunic , Jean-Michel Vernier , Chixu Chen
发明人： Samedy Ouk , Esmir Gunic , Jean-Michel Vernier , Chixu Chen
IPC分类号： C07D213/70 , C07D401/04 , A61K31/4439 , A61K31/4725 , C07D405/10 , A61K31/4433 , A61K31/4709 , A61K31/444 , C07D401/10 , A61K31/502 , C07D417/10 , C07D403/10 , A61K31/497 , C07D241/18 , A61K31/4965 , C07D239/38 , A61K31/505 , A61K31/443 , A61K45/06 , A61K31/519 , A61K31/506 , A61K31/426 , A61K31/4418
CPC分类号： C07D213/70 , A61K31/426 , A61K31/4418 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/4725 , A61K31/4965 , A61K31/497 , A61K31/502 , A61K31/505 , A61K31/506 , A61K31/519 , A61K45/06 , C07D239/38 , C07D241/18 , C07D401/04 , C07D401/10 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/10 , C07D417/04 , C07D417/10
摘要： Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of 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.
摘要翻译：本文描述了可用于调节血液尿酸水平的化合物，含有它们的制剂和使用它们的方法。在一些实施方案中，本文所述的化合物用于治疗或预防与尿酸异常水平相关的病症。

47. 发明申请

US20130040983A1 RAF KINASE INHIBITORS 审中-公开
标题翻译： RAF激酶抑制剂
公开(公告)号：US20130040983A1
公开(公告)日：2013-02-14
申请号：US13520548
申请日：2011-01-07
申请人： Jean-Michel Vernier , Patrick O'Connor , William Ripka , David Matthews , Anthony Pinkerton , Pierre-Yves Bounaud , Stephanie Hopkins
发明人： Jean-Michel Vernier , Patrick O'Connor , William Ripka , David Matthews , Anthony Pinkerton , Pierre-Yves Bounaud , Stephanie Hopkins
IPC分类号： C07D401/04 , C12N9/99 , A61P35/00 , C07D471/04 , A61K31/437 , A61K31/4439 , C07D401/14
CPC分类号： C07D401/04 , C07D471/04
摘要： Described herein are compounds, pharmaceutical compositions and methods for the inhibition of RAF kinae mediated signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human disease and disorders.
摘要翻译：本文描述了用于抑制RAF基因介导的信号传导的化合物，药物组合物和方法。所述化合物，药物组合物和方法可用于治疗人类疾病和病症。

48. 发明申请

US20130012513A1 HEDGEHOG INHIBITORS 有权
标题翻译： HEDGEHOG抑制剂
公开(公告)号：US20130012513A1
公开(公告)日：2013-01-10
申请号：US13520150
申请日：2011-01-06
申请人： Jean-Michel Vernier , John May , Patrick O'Connor , William Ripka , Anthony Pinkerton , Pierre-Yves Bounaud , Stephanie Hopkins
发明人： Jean-Michel Vernier , John May , Patrick O'Connor , William Ripka , Anthony Pinkerton , Pierre-Yves Bounaud , Stephanie Hopkins
IPC分类号： C07D277/30 , C12N5/07 , C07D413/12 , A61P35/00 , C07D263/32 , A61K31/421 , C07D417/12 , A61K31/496 , A61K31/426 , A61K31/5377
CPC分类号： C07D277/28 , C07D263/32 , C07D277/24 , C07D277/30
摘要： Described herein are compounds, pharmaceutical compositions and methods for the inhibition of Hedgehog signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human and veterinary disease and disorders.
摘要翻译：本文描述了用于抑制Hedgehog信号传导的化合物，药物组合物和方法。所述化合物，药物组合物和方法可用于治疗人和兽医疾病和病症。

49. 发明申请

US20120277206A1 REVERSE TRANSCRIPTASE INHIBITORS 失效
标题翻译：反向转录抑制剂
公开(公告)号：US20120277206A1
公开(公告)日：2012-11-01
申请号：US13470122
申请日：2012-05-11
申请人： Alex Shaginian , Samedy Ouk , Jean-Michel Vernier , Anthony B. Pinkerton
发明人： Alex Shaginian , Samedy Ouk , Jean-Michel Vernier , Anthony B. Pinkerton
IPC分类号： A61K31/52 , A61P31/18 , A61K38/19
CPC分类号： C07D487/04 , C07D473/18
摘要： Described herein are novel enzyme inhibitors. In some embodiments, the enzyme inhibitors are reverse transcriptase inhibitors, particularly HIV reverse transcriptase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV reverse transcriptase as a method of treating or preventing HIV, AIDS or related disorders.
摘要翻译：本文描述的是新的酶抑制剂。在一些实施方案中，酶抑制剂是逆转录酶抑制剂，特别是HIV逆转录酶抑制剂。本文还描述了含有它们的组合物和使用它们的方法。因此，本文所述的化合物和组合物可用于体外和体内抑制HIV逆转录酶，作为治疗或预防HIV，AIDS或相关病症的方法。

50. 发明申请

US20080312286A1 Indanone Potentiators of Metabotropic Glutamate Receptors 审中-公开
标题翻译：代谢型谷氨酸受体的茚酮电位器
公开(公告)号：US20080312286A1
公开(公告)日：2008-12-18
申请号：US11658490
申请日：2005-07-26
申请人： Anthony B. Pinkerton , Jean-Michel Vernier , Rowena Cube , John Hutchinson , Celine Bonnefous , Theodore Kamenecka
发明人： Anthony B. Pinkerton , Jean-Michel Vernier , Rowena Cube , John Hutchinson , Celine Bonnefous , Theodore Kamenecka
IPC分类号： C07D257/04 , A61K31/41 , C07C307/02 , A61K31/18 , C07C233/02 , A61K31/454 , C07D401/02 , A61K31/192 , C07C65/00 , C07D213/80 , A61K31/44 , A61K31/343 , C07D307/78 , A61P25/00 , A61P25/18 , A61P25/24 , A61P25/08
CPC分类号： C07C233/91 , C07C59/90 , C07C65/40 , C07C311/51 , C07C2601/08 , C07C2602/08 , C07D257/04 , C07D307/79 , C07D401/04
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。

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