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41. 发明申请

US20080039639A1 Chromane and chromene derivatives and uses thereof 审中-公开
标题翻译：色原和色烯衍生物及其用途
公开(公告)号：US20080039639A1
公开(公告)日：2008-02-14
申请号：US11787860
申请日：2007-04-18
申请人： Alexander Gontcharov , Antonia Nikitenko , Panolil Raveendranath , Chia-Cheng Shaw , Bogdan Wilk , Dahui Zhou
发明人： Alexander Gontcharov , Antonia Nikitenko , Panolil Raveendranath , Chia-Cheng Shaw , Bogdan Wilk , Dahui Zhou
IPC分类号： C07D311/04
CPC分类号： C07D311/58
摘要： Methods of preparing compounds of formula I or pharmaceutically acceptable salts thereof are provided: wherein each of R1, R2, R3, R4, x, m, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.
摘要翻译：提供制备式I化合物或其药学上可接受的盐的方法：其中R 1，R 2，R 3，R 3， SUP，4，x，m，n和Ar如上所定义，并且在本文的类别和亚类中描述，它们是脑5-羟色胺受体的2C亚型的激动剂或部分激动剂。化合物和含有这些化合物的组合物可用于治疗各种中枢神经系统疾病如精神分裂症。

42. 发明申请

US20070015824A1 Serotonin and norepinephrine reuptake inhibitor and uses thereof 失效
标题翻译： 5-羟色胺和去甲肾上腺素再摄取抑制剂及其应用
公开(公告)号：US20070015824A1
公开(公告)日：2007-01-18
申请号：US11486336
申请日：2006-07-13
申请人： Syed Shah , Mahdi Fawzi , Eric Ehrnsperger , Panolil Raveendranath
发明人： Syed Shah , Mahdi Fawzi , Eric Ehrnsperger , Panolil Raveendranath
IPC分类号： A61K31/35 , C07D309/10 , A61K9/48 , A61K9/20
CPC分类号： C07D309/10 , A61K9/20 , A61K9/48
摘要： Selective dual serotonin and norepinephrine reuptake inhibitors are provided. These compounds have a lower side-effect profile and are useful in compositions and products for use in treatment of a variety of conditions including depression, fibromyalgia, anxiety, panic disorder, agoraphobia, post traumatic stress disorder, premenstrual dysphoric disorder, attention deficit disorder, obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, autism, schizophrenia, obesity, anorexia nervosa, bulimia nervosa, Gilles de la Tourette Syndrome, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction, borderline personality disorder, fibromyalgia syndrome, diabetic neuropathic pain, chronic fatigue syndrome, pain, Shy Drager syndrome, Raynaud's syndrome, Parkinson's Disease, and epilepsy.
摘要翻译：提供选择性双重5-羟色胺和去甲肾上腺素再摄取抑制剂。这些化合物具有较低的副作用特征，并且可用于治疗各种病症的组合物和产品，包括抑郁症，纤维肌痛，焦虑症，惊恐障碍，广场恐怖症，创伤后应激障碍，经前期焦虑障碍，注意力缺陷障碍，强迫症，社会焦虑症，广泛性焦虑症，自闭症，精神分裂症，肥胖症，神经性厌食症，神经性贪食症，杜氏综合征，血管舒缩性潮红，可卡因和酒精成瘾，性功能障碍，边缘性人格障碍，纤维肌痛综合征，糖尿病性神经病变疼痛，慢性疲劳综合征，疼痛，Shie Drager综合征，雷诺综合征，帕金森病和癫痫。

43. 发明申请

US20060247442A1 Process for preparing isatins with control of side-product formation 审中-公开
标题翻译：用于制备具有副产物形成控制的异硬脂酸酯的方法
公开(公告)号：US20060247442A1
公开(公告)日：2006-11-02
申请号：US11413160
申请日：2006-04-27
申请人： Bogdan Wilk , Panolil Raveendranath , Zhixian Ding , Peter Wehrenberg
发明人： Bogdan Wilk , Panolil Raveendranath , Zhixian Ding , Peter Wehrenberg
IPC分类号： C07D209/36 , C07D405/02 , C07D403/02
CPC分类号： C07D209/38 , C07D403/04
摘要： Methods and kits for preventing or minimizing the formation of isatin oximes during formation of an isatin from an isonitrosoacetanilide are provided. Also provided are methods and kits for preventing or minimizing the formation of isatin oxime impurities after formation of an isatin from an isonitrosoacetanilide by using a decoy agent in the quenching and/or extraction steps. The isatins can be prepared using a decoy agent and desirably a strong acid. Further provided are methods for preparing isatin oximes.
摘要翻译：提供了用于防止或最小化来自异硝基乙酰替苯胺的靛红形成期间靛红肟形成的方法和试剂盒。还提供了用于在骤冷和/或萃取步骤中通过使用诱饵剂从异亚氨基乙酰替苯胺形成靛红后，防止或最小化靛红肟杂质形成的方法和试剂盒。异丁锭可以使用诱饵剂和期望的强酸来制备。还提供了制备靛红肟的方法。

44. 发明申请

US20050070723A1 Process for the synthesis of a CPLA2 inhibitor 失效
标题翻译：合成CPLA2抑制剂的方法
公开(公告)号：US20050070723A1
公开(公告)日：2005-03-31
申请号：US10948004
申请日：2004-09-23
申请人： Christoph Dehnhardt , Sreenivasulu Megati , Ronald Michalak , Panolil Raveendranath
发明人： Christoph Dehnhardt , Sreenivasulu Megati , Ronald Michalak , Panolil Raveendranath
IPC分类号： C07D209/18 , C07D209/48 , C07D43/02
CPC分类号： C07D209/48 , C07D209/18
摘要： A process for making a substituted indole compound, including the steps of: reacting the compounds in a non-protic polar solvent in the presence of a catalyst to form the intermediate compound wherein Ph and X are as defined herein; and then, heating this intermediate compound in the solvent in the presence of the catalyst to form the substituted indole compound The invention also includes compounds formed by this process.
摘要翻译：一种制备取代的吲哚化合物的方法，包括以下步骤：使化合物在非质子极性溶剂中在催化剂存在下反应形成中间体化合物，其中Ph和X如本文所定义; 然后在催化剂存在下，在溶剂中加热该中间体化合物，形成取代的吲哚化合物。本发明还包括通过该方法形成的化合物。

45. 发明授权

US06818636B2 B-ring estratrienes 有权
标题翻译： B环雌三烯
公开(公告)号：US06818636B2
公开(公告)日：2004-11-16
申请号：US10348506
申请日：2003-01-21
申请人： Syed M. Shah , Panolil Raveendranath , Michael Z. Kagan
发明人： Syed M. Shah , Panolil Raveendranath , Michael Z. Kagan
IPC分类号： A61K3156
CPC分类号： C07J1/00 , A61K31/56 , Y10S514/824
摘要： This invention provides 3&bgr;-hydroxy-5,7,9-estratriene-17-one and a pharmaceutically acceptable salt of its 3-sulfate ester, which is useful as an estrogen.
摘要翻译：本发明提供了可用作雌激素的3,3-羟基-5,7,9-雌三烯-17-酮及其3-硫酸酯的药学上可接受的盐。

46. 发明授权

US07737303B2 Production of chirally pure amino alcohol intermediates, derivatives thereof, and uses thereof 失效
标题翻译：手性纯氨基醇中间体，其衍生物及其用途的生产
公开(公告)号：US07737303B2
公开(公告)日：2010-06-15
申请号：US12546121
申请日：2009-08-24
申请人： John Sellstedt , Gloria Cheal , Razzak Noureldin , Anita Wai-Yin Chan , Panolil Raveendranath , Thomas Joseph Caggiano
发明人： John Sellstedt , Gloria Cheal , Razzak Noureldin , Anita Wai-Yin Chan , Panolil Raveendranath , Thomas Joseph Caggiano
IPC分类号： C07C209/42 , C07C215/08 , C07D333/28
CPC分类号： C07C213/02 , C07B2200/07 , C07C215/08 , C07D333/34
摘要： A method of selectively preparing a chiral 2S-amino alcohol useful in preparation of an amide sulfonated or acylated with alkyl, substituted aryl or substituted heteroaryl is described. The method involves reacting a di-tert-butyl diazene-1,2-dicarboxylate with a (4S)-4-benzyl-3-[(S)-trifluoromethyl-alkyl substituted alkanoyl]-1,3-oxazolidin-2-one to afford a di-tert-butyl 1-(1S,2S)-([(4S)-4-benzyl-2-oxo-1,3-oxazolidine-3-yl]-carbonyl}-trifluoromethyl-alkyl substituted alkyl)hydrazine-1,2-dicarboxylate. This dicarboxylate is then reduced to yield di-tert-butyl 1-(1S,2S)-[trifluoromethyl-alkyl substituted alkyl]hydrazine-1-(hydroxymethyl)-1,2-dicarboxylate. The resulting product is deblocked with an acid to yield the acid addition salt of (2S,3S)-trifluoro-hydrazino-methyl alkan-1-ol. The acid addition salt of (2S,3S)-trifluoro-2-hydrazino-methyl alkan-1-ol is hydrogenated in the presence of a suitable metal catalyst to yield the amino alcohol (2S,3S)-2-amino-trifluoro-methyl alkan-1-ol HCl.
摘要翻译：描述了选择性制备可用于制备用烷基，取代的芳基或取代的杂芳基磺化或酰化的酰胺的手性2S-氨基醇的方法。该方法包括使二噻唑-1,2-二羧酸二叔丁酯与（4S）-4-苄基-3 - [（S） - 三氟甲基 - 烷基取代的烷酰基] -1,3-恶唑烷-2-酮得到1-（1S，2S） - （[（4S）-4-苄基-2-氧代-1,3-恶唑烷-3-基] - 羰基} - 三氟甲基 - 烷基取代的烷基的二 - 叔丁基）肼-1,2-二羧酸。然后将该二羧酸酯还原，得到1-（1S，2S） - [三氟甲基 - 烷基取代的烷基]肼-1-（羟甲基）-1,2-二羧酸二叔丁酯。所得产物用酸解封，得到（2S，3S） - 三氟 - 肼基 - 甲基烷-1-醇的酸加成盐。（2S，3S） - 三氟-2-肼基 - 甲基烷-1-醇的酸加成盐在合适的金属催化剂存在下氢化，得到氨基醇（2S，3S）-2-氨基 - 三氟 - 甲基链烷-1-醇HCl。

47. 发明授权

US07687520B2 Serotonin and norepinephrine reuptake inhibitors and uses thereof 失效
标题翻译： 5-羟色胺和去甲肾上腺素再摄取抑制剂及其用途
公开(公告)号：US07687520B2
公开(公告)日：2010-03-30
申请号：US11485693
申请日：2006-07-13
申请人： Syed M. Shah , Mahdi B. Fawzi , Panolil Raveendranath , Eric C. Ehrnsperger
发明人： Syed M. Shah , Mahdi B. Fawzi , Panolil Raveendranath , Eric C. Ehrnsperger
IPC分类号： A61K31/445 , C07D211/44
CPC分类号： C07D211/44
摘要： Selective dual serotonin and norepinephrine reuptake inhibitors are provided. These compounds have a lower side-effect profile and are useful in compositions and products for use in treatment of a variety of conditions including depression, fibromyalgia, anxiety, panic disorder, agorophobia, post traumatic stress disorder, premenstrual dysphoric disorder, attention deficit disorder, obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, autism, schizophrenia, obesity, anorexia nervosa, bulimia nervosa, Gilles de la Tourette Syndrome, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction, borderline personality disorder, fibromyalgia syndrome, diabetic neuropathic pain, chronic fatigue syndrome, pain, Shy Drager syndrome, Raynaud's syndrome, Parkinson's Disease, and epilepsy.
摘要翻译：提供选择性双重5-羟色胺和去甲肾上腺素再摄取抑制剂。这些化合物具有较低的副作用特征，并且可用于治疗各种病症的组合物和产品，包括抑郁症，纤维肌痛，焦虑症，惊恐障碍，广泛性恐惧症，创伤后应激障碍，经前焦虑障碍，注意力缺陷障碍，强迫症，社会焦虑症，广泛性焦虑症，自闭症，精神分裂症，肥胖症，神经性厌食症，神经性贪食症，杜氏综合征，血管舒缩性潮红，可卡因和酒精成瘾，性功能障碍，边缘性人格障碍，纤维肌痛综合征，糖尿病性神经病变疼痛，慢性疲劳综合征，疼痛，Shie Drager综合征，雷诺综合征，帕金森病和癫痫。

48. 发明申请

US20080177085A1 Process for the Synthesis of a CPLA2 Inhibitor 审中-公开
标题翻译：合成CPLA2抑制剂的方法
公开(公告)号：US20080177085A1
公开(公告)日：2008-07-24
申请号：US12041988
申请日：2008-03-04
申请人： Christoph M. Dehnhardt , Sreenivasulu Megati , Ronald S. Michalak , Panolil Raveendranath
发明人： Christoph M. Dehnhardt , Sreenivasulu Megati , Ronald S. Michalak , Panolil Raveendranath
IPC分类号： C07D209/20
CPC分类号： C07D209/48 , C07D209/18
摘要： A process for making a substituted indole compound, including the steps of: reacting the compounds in a non-protic polar solvent in the presence of a catalyst to form the intermediate compound wherein Ph and X are as defined herein; and then, heating this intermediate compound in the solvent in the presence of the catalyst to form the substituted indole compound The invention also includes compounds formed by this process.
摘要翻译：一种制备取代的吲哚化合物的方法，包括以下步骤：使化合物在非质子极性溶剂中在催化剂存在下反应形成中间体化合物，其中Ph和X如本文所定义; 然后在催化剂存在下，在溶剂中加热该中间体化合物，形成取代的吲哚化合物。本发明还包括通过该方法形成的化合物。

49. 发明授权

US06693207B2 B-ring estratriene diols 有权
标题翻译： B环雌二醇
公开(公告)号：US06693207B2
公开(公告)日：2004-02-17
申请号：US10164149
申请日：2002-06-05
申请人： Michael Z. Kagan , Panolil Raveendranath , Syed M. Shah , Michael W. Winkley
发明人： Michael Z. Kagan , Panolil Raveendranath , Syed M. Shah , Michael W. Winkley
IPC分类号： C07J100
CPC分类号： A61K31/56 , C07J1/00
摘要： This invention provides estrogenic agents having the formula wherein A and B are each, independently, R is SO3−X+; X+ is alkali metal, alkaline earth metal, ammonium, alkylammonium containing 1-6 carbon atoms, or dialkylammonium containing 1-6 carbon atoms in each alkyl group, or trialkylammonium containing 1-6 carbon atoms in each alkyl group; with the proviso that at least one of A or B is
摘要翻译：本发明提供具有马来酰亚胺A的雌激素剂，B各自独立地是R 3是SO 3 - ，X +; X +是含有1-6个碳原子的碱金属，碱土金属，铵，烷基铵或二烷基铵每个烷基中含有1-6个碳原子，或每个烷基含有1-6个碳原子的三烷基铵;条件是A或B中的至少一个为

50. 发明授权

US06458778B1 Estradienes 失效
标题翻译：埃斯特丹人
公开(公告)号：US06458778B1
公开(公告)日：2002-10-01
申请号：US09049485
申请日：1998-03-27
申请人： Fangming Kong , Leonard A. McDonald , Michael Z. Kagan , Syed M. Shah , Panolil Raveendranath , Mark A. Collins
发明人： Fangming Kong , Leonard A. McDonald , Michael Z. Kagan , Syed M. Shah , Panolil Raveendranath , Mark A. Collins
IPC分类号： A61K3156
CPC分类号： C07J1/00
摘要： This invention provides estra-5(10),7-dien-3&bgr;-ol-17-one or a pharmaceutically acceptable salt of its 3-sulfate ester, estra-5(10),7-dien-3&bgr;-ol-17-one 3-glucuronide or a pharmaceutically acceptable salt thereof, estra-5(10),7-dien-3&agr;-ol-17-one or a pharmaceutically acceptable salt of its 3-sulfate ester, estra-5(10),7-dien-3&bgr;-ol-17-one 3-glucuronide or a pharmaceutically acceptable salt thereof, estra-5(10),7-dien-3&bgr;-ol-17-one 3-alkali metal salt, and estra-5(10),7-dien-3&agr;-ol-17-one 3-alkali metal salt which are useful as estrogenic agents.
摘要翻译：本发明提供雌甾-5（10），7-二烯-3β-醇-17-或其3-硫酸酯，雌-5（10），7-二烯-3β-醇-17-酮的药学上可接受的盐，一种3-葡糖苷酸或其药学上可接受的盐，estra-5（10），7-二烯-3α-醇-17-或其3-硫酸酯的药学上可接受的盐，estra-5（10），7- 二烯-3β-醇-17-酮3-葡糖苷酸或其药学上可接受的盐，雌-5（10），7-二烯-3β-醇-17-酮3-碱金属盐和雌甾-5（10），7-二烯-3α-醇-17-酮3-碱金属盐，其可用作雌激素剂。

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