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公开(公告)号：US20180311214A1
公开(公告)日：2018-11-01
申请号：US15973939
申请日：2018-05-08
IPC分类号： A61K31/4164 , A61K9/00 , C07D233/94 , A61K45/06
CPC分类号： A61K31/4164 , A61K9/0014 , A61K45/06 , C07D233/94
摘要： This invention relates to the medical use of an antimicrobial agent, racemic Ornidazole, its (R) and (S) enantiomers, or pharmaceutically acceptable salts or esters thereof, and to methods of treatment which involve treating a subject with Ornidazole. The racemic (rac)-ornidazole, its enantiomers, or pharmaceutically acceptable salts or esters thereof, may be used in combination with other actives. The invention also relates to pharmaceutical formulations and compositions comprising (rac)-ornidazole, (R)-ornidazole, (S)-ornidazole, or pharmaceutically acceptable salts or esters thereof, and/or other actives as well as methods to stereoselectively manufacture the enantiomers.
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公开(公告)号：US09233932B2
公开(公告)日：2016-01-12
申请号：US14477606
申请日：2014-09-04
申请人： NEKTAR THERAPEUTICS
IPC分类号： A61K31/41 , C07D233/94 , A61K47/48
CPC分类号： C07D233/94 , A61K47/48215 , A61K47/60
摘要： The invention provides (among other things) small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer.
摘要翻译： 本发明提供了（尤其是）通过共价连接水溶性低聚物化学改性的小分子药物。
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公开(公告)号：US20130217740A1
公开(公告)日：2013-08-22
申请号：US13806719
申请日：2011-06-29
IPC分类号： C07D233/94
CPC分类号： C07D233/94 , A61K9/0014 , A61K31/4164
摘要： A compound of formula (I): is described, as well as enantiomers, pharmaceutically acceptable salts thereof, and uses thereof.
摘要翻译： 描述了式（I）的化合物，以及对映异构体，其药学上可接受的盐及其用途。
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公开(公告)号：US20130197048A1
公开(公告)日：2013-08-01
申请号：US13807167
申请日：2011-06-29
IPC分类号： C07D233/94
CPC分类号： C07D233/94 , A61K9/0014 , A61K31/4164
摘要： A compound of formula (I): is described, as well as pharmaceutically acceptable salts thereof, and its use as a medicament.
摘要翻译： 描述了式（I）的化合物，以及其药学上可接受的盐及其作为药物的用途。
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公开(公告)号：US20120202756A1
公开(公告)日：2012-08-09
申请号：US13253677
申请日：2011-10-05
IPC分类号： A61K31/7056 , C07H15/14 , C07C229/22 , C07C229/60 , C07D211/46 , C07D211/22 , C07D417/12 , C07D403/12 , A61K31/4164 , A61K31/225 , A61K31/24 , A61K31/445 , A61K31/554 , A61K31/506 , A61P31/04 , A61P9/06 , A61P25/28 , A61P19/02 , A61P25/24 , A61P35/00 , A61P19/10 , A61P31/12 , A61P3/10 , C07D233/94
CPC分类号： C07C279/26 , A61K31/4375 , C07C233/47 , C07C233/54 , C07C2601/14 , C07D211/32 , C07D211/46 , C07D233/94 , C07D285/135 , C07D307/20 , C07D403/12 , C07D405/12 , C07D417/12 , C07D471/04 , C07D501/60 , C07F9/3873 , C07H15/04
摘要： The present invention relates to prodrugs of a wide variety of drugs and pharmaceutical compositions containing such prodrugs. Methods for minimizing locally mediated (from within the gut lumen) adverse gastrointestinal events associated with the underivatised drug and increasing the sustainment of plasma drug levels with the aforementioned prodrugs are also provided. Thus, the present invention relates to the use of prodrugs of a wide diversity of drugs (other than opioids) to transiently inactivate them and so reduce directly, locally mediated adverse gastrointestinal (GI) side-effects normally evident after administration of the parent compound. Additionally, such prodrugs may confer improved pharmacokinetics.
摘要翻译： 本发明涉及各种药物的前药和含有这些前药的药物组合物。 还提供了用于使局部介导的（来自肠内腔）最小化与未发病药物相关的不良胃肠道事件和用上述前药增加血浆药物水平的维持的方法。 因此，本发明涉及广泛多样的药物（阿片样物质除外）的前体药物使用以使其短暂失活，并因此降低在给予母体化合物后通常明显的局部介导的不良胃肠道（GI）副作用。 此外，这样的前药可以赋予改善的药代动力学。
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公开(公告)号：US20090258859A1
公开(公告)日：2009-10-15
申请号：US12096998
申请日：2006-12-08
IPC分类号： A61K31/4164 , A61K31/55
CPC分类号： C07D233/94 , C07D223/28
摘要： Cocrystals of metronidazole are described herein. Such cocrystals are a cocrystal of metronidazole with gentisic acid and a cocrystal of metronidazole with gallic acid. Cocrystals of imipramine hydrochloride are also described. Such cocrystals are a cocrystal of imipramine hydrochloride with (+)-camphoric acid, a cocrystal of imipramine hydrochloride with fumaric acid, and a cocrystal of imipramine hydrochloride with 1-hydroxy-2-naphthoic acid.
摘要翻译： 本文描述了甲硝唑的晶体。 这种共晶体是甲硝唑与龙胆酸的共结晶体和甲硝唑与没食子酸的共结晶体。 也描述了盐酸丙咪嗪的Cystystals。 这种共晶体是盐酸丙咪嗪与（+） - 樟脑酸，盐酸丙咪嗪与富马酸的共结晶和盐酸丙咪嗪与1-羟基-2-萘甲酸的共结晶。
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7.发明申请Antibacterial and/or antiprotozoal nitromidazole derivative compounds with urease inhibitor activity, process for preparing these compounds and use in pharmaceutical compositions and medicines 失效具有脲酶抑制剂活性的抗细菌和/或抗原生动物硝唑唑衍生物化合物，用于制备这些化合物的方法和用于药物组合物和药物公开(公告)号：US20070072929A1
公开(公告)日：2007-03-29
申请号：US10577331
申请日：2004-10-27
申请人： Antônio Silva , Andressa Munhoz , Jean Santos , Rodolfo Camargo , Lucia Castro , Renato Menegon , Wagner Vilegas , Antonio Ferreira , Eliana Varanda , Man Chung
发明人： Antônio Silva , Andressa Munhoz , Jean Santos , Rodolfo Camargo , Lucia Castro , Renato Menegon , Wagner Vilegas , Antonio Ferreira , Eliana Varanda , Man Chung
IPC分类号： A61K31/4178 , C07D403/02
CPC分类号： C07D233/94
摘要： The present application describes nitroimidazolic derivative compounds with antibacterial and/or antiprotozoal activity, which are potent urease inhibitors. It also describes the process for preparing those compounds and their use in pharmaceutical compositions and medicines.
摘要翻译： 本申请描述了具有抗细菌和/或抗原虫活性的硝基咪唑衍生物化合物，其是有效的脲酶抑制剂。 它还描述了制备这些化合物的方法及其在药物组合物和药物中的应用。
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8.发明授权Substituted diaryl heterocycles, process for their preparation and their use as medicaments 有权取代的二芳基杂环，其制备方法及其作为药物的用途公开(公告)号：US07141561B2
公开(公告)日：2006-11-28
申请号：US10626314
申请日：2003-07-24
申请人： Lothar Schwink , Siegfried Stengelin , Matthias Gossel , Thomas Boehme , Gerhard Hessler , Gerard Rosse , Armin Walser
发明人： Lothar Schwink , Siegfried Stengelin , Matthias Gossel , Thomas Boehme , Gerhard Hessler , Gerard Rosse , Armin Walser
IPC分类号： A61K31/397 , A61K31/415 , C07D417/10 , C07D401/10 , C07D233/02
CPC分类号： C07D233/92 , C07D209/02 , C07D233/32 , C07D233/70 , C07D233/74 , C07D233/94 , C07D243/04 , C07D249/12 , C07D401/12 , C07D403/12 , C07D405/10 , C07D405/12 , C07D409/10 , C07D409/12 , C07D417/12 , C07D487/08 , C07D491/10
摘要： This invention discloses and claims diary heterocycles of formula (I) and their pharmaceutically acceptable salts, pharmaceutical compositions thereof, and methods of using said compounds of formula (I) for the treatment or prevention of excessive weight or obesity, and for treatment of Type II diabetes, arteriosclerosis, high blood pressure, depression, anxiety, anxiety neuroses, and schizophrenia. Methods for treatment of excessive weight or obesity and for treatment of Type II diabetes with a mixture of a compound of formula I and antiobesity agents or appetite-regulating active ingredients, or with a mixture of a compound of formula I and antidiabetics or hypoglycemic active ingredients are also disclosed and claimed.
摘要翻译： 本发明公开并要求式（I）的日记杂环及其药学上可接受的盐，其药物组合物，以及使用式（I）化合物治疗或预防过度体重或肥胖以及用于治疗II型 糖尿病，动脉硬化，高血压，抑郁，焦虑，焦虑神经症和精神分裂症。 用于治疗过度体重或肥胖以及用式I化合物与抗肥胖剂或食欲调节活性成分的混合物或与式I化合物与抗糖尿病药或降血糖活性成分的混合物治疗II型糖尿病的方法 也被公开和要求保护。
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9.发明申请公开(公告)号：US20060063820A1
公开(公告)日：2006-03-23
申请号：US10540038
申请日：2003-12-22
申请人： Peter Renold , Werner Zambach , Arthur Steiger , Roger Hall , Olivier Loiseleur , Stephan Trah
发明人： Peter Renold , Werner Zambach , Arthur Steiger , Roger Hall , Olivier Loiseleur , Stephan Trah
CPC分类号： C07C255/54 , A01N31/08 , A01N31/16 , A01N33/20 , A01N37/38 , A01N37/40 , A01N43/28 , A01N43/30 , A01N43/40 , A01N43/42 , A01N43/56 , A01N47/30 , A01N53/00 , C07C43/225 , C07C43/29 , C07C49/84 , C07C69/708 , C07C69/712 , C07C69/743 , C07C69/76 , C07C69/92 , C07C205/34 , C07C205/37 , C07C205/43 , C07C205/49 , C07C205/56 , C07C205/57 , C07C235/16 , C07C255/55 , C07C255/57 , C07C271/16 , C07C271/48 , C07C275/30 , C07C275/34 , C07C2601/02 , C07D213/63 , C07D213/64 , C07D213/643 , C07D213/65 , C07D213/68 , C07D215/20 , C07D215/233 , C07D215/58 , C07D231/20 , C07D231/22 , C07D233/94 , C07D257/04 , C07D277/34 , C07D285/08 , C07D285/14 , C07D307/58 , C07D317/64 , C07D333/32
摘要： Compounds of formula (I), wherein A1 is, for example, a bond or a C1-C6alkylene bridge; A2 is, for example, a bond or C1-C6alkylene; A3 is, for example, C1-C6alkylene; W is, for example, O or S; T is, for example, a bond, O, NH, NR7, S, SO, SO2, —C(═O)—O— or —O—C(═O)—; Q is a bond, O, NR7, S, SO or SO2; Y is O, NR7, S, SO or SO2; X1 and X2 are, each independently of the other, fluorine, chlorine, bromine or iodine; R1 is, for example, halogen, CN, nitro, C1-C6alkyl or C1-C6haloalkyl; R2 and R3 are, for example, H, halogen, CN, nitro or C1-C6alkyl; R7 is, for example, H, C1-C6alkyl or C1-C3haloalkyl; m is 1 or 2; and E is C1-C6alkyl, C1-C6haloalkyl, aryl or heterocyclyl; and, where applicable, possible E/Z isomers, mixtures of E/Z isomers and/or tautomers thereof, in each case in free form or in salt form; a process for the preparation of and the use of those compounds; pesticidal compositions in which the active ingredient has been selected from those compounds, or an agrochemically usable salt thereof; a process for the preparation of and the use of those compositions; plant propagation material treated with those compositions; and a method of controlling pests are described.
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10.发明申请Phenylethynyl and styryl derivatives of imidazole and fused ring heterocycles 失效咪唑和稠环杂环的苯乙炔基和苯乙烯基衍生物公开(公告)号：US20030208082A1
公开(公告)日：2003-11-06
申请号：US10396172
申请日：2003-03-25
发明人： Vincent Mutel , Jens-Uwe Peters , Juergen Wichmann
IPC分类号： C07D233/02 , C07D43/02
CPC分类号： C07D233/56 , A61K31/4164 , C07D209/14 , C07D233/64 , C07D233/90 , C07D233/92 , C07D233/94 , C07D403/06 , C07D413/04 , C07D513/14
摘要： This invention relates to a compound and the use of the compound of the formula 1 wherein R1, R2, R3, R4 and R5 are as defined in the description, A signifies nullCHnullCHnull or nullCnullCnull; and B signifies 2 wherein R6 to R26, X and Y are as defined In the specification or a pharmaceutically acceptable salt thereof, for use in pharmaceutical compositions for the treatment or prevention of mGluR5 receptor mediated disorders.
摘要翻译： 本发明涉及化合物和下式化合物的用途，其中R 1，R 2，R 3，R 4和R 5如描述中所定义，A表示 - CH = CH-或-C = C-; 和B表示其中R 6至R 26，X和Y如说明书或其药学上可接受的盐中所定义，用于治疗或预防mGluR5受体介导的病症的药物组合物中。
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