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公开(公告)号：US06255545B1
公开(公告)日：2001-07-03
申请号：US09590853
申请日：2000-06-08
申请人： Raymond Cvetovich , Fuh-Rong Tsay
发明人： Raymond Cvetovich , Fuh-Rong Tsay
IPC分类号： C07C1700
摘要： The present invention is concerned with a novel process for the preparation of 3,5-bis(trifluoromethyl)bromobenzene (CAS 328-70-1). This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
摘要翻译： 本发明涉及制备3,5-双（三氟甲基）溴苯（CAS 328-70-1）的新方法。 该化合物可用作合成具有药理活性的化合物的中间体。
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2.发明授权Process for 4"-epi-acetylamino-4"-deoxy-5-oximinoavermectin B.sub.1 失效4'-表乙酰氨基-4'-脱氧-5-肟基亚氨基维生素B1的方法
公开(公告)号：US5420260A
公开(公告)日：1995-05-30
申请号：US129219
申请日：1993-09-29
申请人： Joseph S. Amato , Raymond Cvetovich
发明人： Joseph S. Amato , Raymond Cvetovich
CPC分类号： C07H19/01
摘要： An improved process for formation of a 5-oxime on avermectin derivatives comprises the treatment of the oxo-compound with hydroxylamine in aqueous isopropanol at pH 1.8-2.1.
摘要翻译： 用于在除虫菌素衍生物上形成5-肟的改进方法包括在pH 1.8-2.1的异丙醇水溶液中用羟胺处理氧代化合物。
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3.发明授权Process for 4"-EPI-acetylamino-4"-deoxy-5-oximinoavermectin-B.sub.1 失效4“ - 乙酰氨基-4” - 脱氧-5-肟基维生素B1的方法
公开(公告)号：US5362862A
公开(公告)日：1994-11-08
申请号：US128935
申请日：1993-09-29
申请人： Joseph S. Amato , Raymond Cvetovich
发明人： Joseph S. Amato , Raymond Cvetovich
CPC分类号： C07H19/01
摘要： An improved process for formation of a 5-oxime on avermectin derivatives comprises the treatment of the oxo compound with O-(trimethylsilyl)hydroxylamine in the presence of a Lewis acid.
摘要翻译： 在阿维菌素衍生物上形成5-肟的改进方法包括在路易斯酸存在下用O-（三甲基甲硅烷基）羟胺处理氧代化合物。
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4.发明授权公开(公告)号：US07145002B2
公开(公告)日：2006-12-05
申请号：US10485319
申请日：2002-09-20
申请人： Karel M. J. Brands , Raymond Cvetovich , Louis S. Crocker , Michael D. Ward , Amar J. Mahajan , Robert M. Wenslow , John M. Williams , Daniel R. Sidler , Charles Orella , Elizabeth S. Fisher , Ronald Jobson
发明人： Karel M. J. Brands , Raymond Cvetovich , Louis S. Crocker , Michael D. Ward , Amar J. Mahajan , Robert M. Wenslow , John M. Williams , Daniel R. Sidler , Charles Orella , Elizabeth S. Fisher , Ronald Jobson
IPC分类号： C07D477/20
CPC分类号： C07D477/20
摘要： A process for preparing a crystalline, carbapenem monosodium salt of formula IIa: characterized by the steps a) adding about 10 to 30% of an organic solvent to an aqueous solution of the carbapenem, b) cooling the resulting solution to less than −5° C., c) adjusting the pH using a solution containing an acid in an organic solvent to give the appropriate pH for crystallization, and d) crystallizing the compound by adding methanol, and a C2-5 alcohol at between −5 and −25° C.
摘要翻译： 制备式IIa的结晶碳青霉烯单钠盐的方法，其特征在于以下步骤：a）向碳青霉烯的水溶液中加入约10至30％的有机溶剂，b）将所得溶液冷却至小于-5℃ c）c）使用在有机溶剂中含有酸的溶液调节pH以得到适当的结晶pH，和d）通过加入甲醇和C 2-5醇来使化合物结晶 在-5和-25℃之间
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5.发明申请Process and intermediates for the preparation of pyrrolidine carboxylic acids 审中-公开用于制备吡咯烷羧酸的方法和中间体公开(公告)号：US20060199958A1
公开(公告)日：2006-09-07
申请号：US10550640
申请日：2004-04-09
申请人： Raymond Cvetovich , John Chung , Joseph Amato , Lisa Dimichele
发明人： Raymond Cvetovich , John Chung , Joseph Amato , Lisa Dimichele
IPC分类号： C07D417/02 , C07D413/02 , C07D403/02
CPC分类号： C07D401/04 , C07D207/16 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04
摘要： A novel process is provided for the preparation of pyrrolidine carboxylic acids, and the useful intermediates obtained therein. These compounds are intermediates for the synthesis of melanocortin-4 receptor (MC-4R), which are useful for the treatment of disorders such as obesity, diabetes, sexual dysfunction, male sexual dysfunction, and female sexual dysfunction.
摘要翻译： 提供了一种制备吡咯烷羧酸的新方法及其中获得的有用的中间体。 这些化合物是合成黑皮质素-4受体（MC-4R）的中间体，其可用于治疗诸如肥胖症，糖尿病，性功能障碍，男性性功能障碍和女性性功能障碍的疾病。
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6.发明授权Process for the synthesis of 1-(3,5-bis(trifluoromethyl)phenyl)ethan-1-one 失效1-（3,5-双（三氟甲基）苯基）乙-1-酮的合成方法公开(公告)号：US06814895B2
公开(公告)日：2004-11-09
申请号：US10451293
申请日：2004-01-28
IPC分类号： C07F300
CPC分类号： C07F3/02 , C07C17/12 , C07C45/004 , C07C49/80 , C07C25/13
摘要： The present invention is concerned with a novel process for the preparation of 1-(3,5-bis(trifluoromethyl)phenyl)ethan-1-one (CAS 30071-93-3). This compound is useful as an intermediate in the synthesis of therapeutic agents.
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7.发明授权Stable salts of 4"-deoxy-4"-epi-methylamino avermectin Bla/Blb 失效4“ - 脱氧-4” - 表 - 甲基氨基除虫菌素B1a / B1b的稳定盐
公开(公告)号：US5288710A
公开(公告)日：1994-02-22
申请号：US862035
申请日：1992-04-02
申请人： Raymond Cvetovich
发明人： Raymond Cvetovich
IPC分类号： A01N43/90 , A61K31/70 , A61K31/7042 , A61K31/7048 , A61P33/00 , C07H17/08 , C07H19/01 , C07H17/04
摘要： Certain salts of 4"-deoxy-4"-epi-methylamino avermectin Bla/Blb such as: the benzoic acid salt, gallic acid salt, citric acid salt, benzenesulfonic acid salt and salicyclic acid salt, phosphoric acid salt, tartaric acid salt or maleic acid salt, exhibit enhanced stability, a property which serves to provide greater shelf life and a product of greater safety for the user and the environment.
摘要翻译： 4“ - 脱氧-4” - 表 - 甲基氨基除虫菌素Bla / Blb的某些盐，例如：苯甲酸盐，没食子酸盐，柠檬酸盐，苯磺酸盐和水杨酸盐，磷酸盐，酒石酸 盐或马来酸盐表现出增强的稳定性，其用于提供更大的保存期限的性质以及用户和环境具有更高安全性的产品。
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8.发明授权Salts and polymorphs of 9-(2,2-dimethylpropyl-aminomethyl) minocycline 有权9-（2,2-二甲基丙基氨基甲基）米诺环素的盐和多晶型物公开(公告)号：US08383610B2
公开(公告)日：2013-02-26
申请号：US12471758
申请日：2009-05-26
申请人： Raymond Cvetovich , Tadeusz Warchol
发明人： Raymond Cvetovich , Tadeusz Warchol
IPC分类号： A61K31/65 , C07C237/26
CPC分类号： A61K31/65 , C07B2200/13 , C07C231/12 , C07C237/26 , C07C303/32 , C07C309/30 , C07C2603/46
摘要： Crystalline forms, including salts and polymorphs, of a compound useful in the treatment of tetracycline compound-responsive states are provided herein. The crystalline compounds are useful for the treatment or prevention of conditions and disorders such as bacterial infections and neoplasms, as well as other known applications for tetracycline compounds in general.
摘要翻译： 本文提供了可用于治疗四环素化合物反应状态的化合物的结晶形式，包括盐和多晶型物。 结晶化合物可用于治疗或预防条件和病症，例如细菌感染和肿瘤，以及其他已知的四环素化合物的应用。
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公开(公告)号：US20100113399A1
公开(公告)日：2010-05-06
申请号：US12471758
申请日：2009-05-26
申请人： Raymond Cvetovich , Tadeusz Warchol
发明人： Raymond Cvetovich , Tadeusz Warchol
IPC分类号： A61K31/65 , C07C233/64
CPC分类号： A61K31/65 , C07B2200/13 , C07C231/12 , C07C237/26 , C07C303/32 , C07C309/30 , C07C2603/46
摘要： Crystalline forms, including salts and polymorphs, of a compound useful in the treatment of tetracycline compound-responsive states are provided herein. The crystalline compounds are useful for the treatment or prevention of conditions and disorders such as bacterial infections and neoplasms, as well as other known applications for tetracycline compounds in general.
摘要翻译： 本文提供了可用于治疗四环素化合物反应状态的化合物的结晶形式，包括盐和多晶型物。 结晶化合物可用于治疗或预防条件和病症，例如细菌感染和肿瘤，以及其他已知的四环素化合物的应用。
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公开(公告)号：US07022841B2
公开(公告)日：2006-04-04
申请号：US10485134
申请日：2002-09-20
申请人： Raymond Cvetovich , Robert Wenslow , John M. Williams , Daniel Sidler , Louis Crocker , Hsien-Hsin Tung , Brian K. Johnson , Joseph Kukura, II , Ulf Dolling
发明人： Raymond Cvetovich , Robert Wenslow , John M. Williams , Daniel Sidler , Louis Crocker , Hsien-Hsin Tung , Brian K. Johnson , Joseph Kukura, II , Ulf Dolling
IPC分类号： C07D477/20
CPC分类号： C07D477/20 , C07D477/02
摘要： The present invention relates to a process for reducing the levels of organic solvents to pharmaceutically acceptable levels in thermally unstable crystalline carbapenem solids represented by formula I: or a salt thereof, wherein R1 and R2, are the same or different, and are selected from H, alkyl, aryl, and heteroaryl, comprising washing a carbapenem solid containing organic solvent with an organic solvent containing water; and using vacuum and/or inert gas (hydrated or dry) at low temperature to produce a compound of formula I containing pharmaceutically acceptable levels of organic solvents, wherein the water content of the crystalline carbapenem solid, correcting for organic solvents, is maintained at about 13% to about 25% during the process.
摘要翻译： 本发明涉及一种将由式I表示的热不稳定结晶碳青霉烯固体中的有机溶剂水平降低到可药用水平的方法：或其盐，其中R 1和R 2 包括相同或不同的选自H，烷基，芳基和杂芳基，包括用含水的有机溶剂洗涤含有有机溶剂的碳青霉烯固体; 并在低温下使用真空和/或惰性气体（水合或干燥）以产生含有药学上可接受水平的有机溶剂的式I化合物，其中将有机溶剂校正的结晶碳青霉烯固体的水含量保持在约 13％至25％。
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