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11. 发明授权

US06562844B2 Oxazolidinone combinatorial libraries, compositions and methods of preparation 失效
公开(公告)号：US06562844B2
公开(公告)日：2003-05-13
申请号：US10034754
申请日：2001-12-28
申请人： Mikhail F. Gordeev , Gary W. Luehr , Dinesh V. Patel , Zhi-Jie Ni , Eric Gordon
发明人： Mikhail F. Gordeev , Gary W. Luehr , Dinesh V. Patel , Zhi-Jie Ni , Eric Gordon
IPC分类号： C07D41312
CPC分类号： C07D263/20 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12 , C07F9/653 , C40B40/00
摘要： Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.

12. 发明授权

US06465499B1 Sulphonylbenzazolones 失效
标题翻译：磺酰基苯并唑酮
公开(公告)号：US06465499B1
公开(公告)日：2002-10-15
申请号：US09718047
申请日：2000-11-21
申请人： Lutz Assmann , Hans-Ludwig Elbe , Robert Markert , Ralf Tiemann , Klaus Stenzel
发明人： Lutz Assmann , Hans-Ludwig Elbe , Robert Markert , Ralf Tiemann , Klaus Stenzel
IPC分类号： C07D41312
CPC分类号： C07D413/12 , A01N43/80 , C07D417/12
摘要： Sulphonylbenzazolones of the formula in which R1, R2, R3, R4, R5 and Q are each as defined in the description, a process for preparing these compounds and their use as microbicides in crop protection and in the protection of materials.
摘要翻译： R1，R2，R3，R4，R5和Q的磺酰基苯并咪唑酮各自如说明书中所定义，这些化合物的制备方法及其作为杀菌剂在作物保护和材料保护中的用途。

13. 发明授权

US06458814B1 Vitronectin receptor antagonists 失效
标题翻译： Vitronectin受体拮抗剂
公开(公告)号：US06458814B1
公开(公告)日：2002-10-01
申请号：US09762406
申请日：2001-02-07
申请人： Peter J. Manley , William H. Miller
发明人： Peter J. Manley , William H. Miller
IPC分类号： C07D41312
CPC分类号： C07D413/12
摘要： Compounds of the formula (I) are disclosed which are vitronectin receptor antagonists and are useful in the treatment of osteoporosis: or a pharmaceutically acceptable salt thereof.
摘要翻译：公开了式（I）的化合物，其是玻连蛋白受体拮抗剂，可用于治疗骨质疏松症：或其药学上可接受的盐。

14. 发明授权

US06451790B1 Azadioxacycloalkenes and their use for combating harmful fungi and animal pests 失效
标题翻译： Azadioxacycalkalk烯及其用于防治有害真菌和动物害虫的用途
公开(公告)号：US06451790B1
公开(公告)日：2002-09-17
申请号：US09889164
申请日：2001-07-11
申请人： Markus Gewehr , Hubert Sauter , Bernd Müller , Wassilios Grammenos , Andreas Gypser , Arne Ptock , Oliver Cullmann , Jordi Tormo i Blasco , Eberhard Ammermann , Siegfried Strathmann , Gisela Lorenz , Volker Harries , Roland Götz , Thomas Grote
发明人： Markus Gewehr , Hubert Sauter , Bernd Müller , Wassilios Grammenos , Andreas Gypser , Arne Ptock , Oliver Cullmann , Jordi Tormo i Blasco , Eberhard Ammermann , Siegfried Strathmann , Gisela Lorenz , Volker Harries , Roland Götz , Thomas Grote
IPC分类号： C07D41312
CPC分类号： C07D413/12 , A01N43/82 , A01N43/88 , C07D231/20 , C07D249/12 , C07D413/14
摘要： Compounds of formula I wherein W is optionally substituted alkylene; Y is N or CRa; Ra is hydrogen, halogen or alkyl; R1n represents hydrogen or 1 to 4 substituents; R2 is hydrogen, nitro, cyano, halogen, alkyl, haloalkyl, alkoxy, alkylthio or alkoxycarbonyl; R3 is optionally substituted alkyl, cycloalkyl, aryl or hetaryl; A is N—OR4, CH—OR4, CH—SR4 or CHR5; R4 is alkyl or haloalkyl; R5 is halogen, alkyl or haloalkyl; methods and intermediates for their preparation. The compounds and compositions comprising them are useful for combating animal pests and harmful fungi.
摘要翻译：式I的化合物，其中W是任选取代的亚烷基; Y是N或CR a; R a是氢，卤素或烷基; R 11代表氢或1-4个取代基; R 2是氢，硝基，氰基，卤素，烷基，卤代烷基，烷氧基，烷硫基或烷氧基羰基; R3是任选取代的烷基，环烷基，芳基或杂芳基; A是N-OR4，CH-OR4，CH-SR4或CHR5; R4是烷基或卤代烷基; R5是卤素，烷基或卤代烷基;其制备方法和中间体。包含它们的化合物和组合物可用于对抗动物害虫和有害真菌。

15. 发明授权

US06313114B1 3,4-Dihydro-2H-benzo[1,4]oxazinyl-methyl)-[3-(1H-indol-3yl)-alkyl]- amines 失效
标题翻译： 3,4-二氢-2H-苯并[1,4]恶嗪基 - 甲基） - [3-（1H-吲哚基） - 烷基] - 胺
公开(公告)号：US06313114B1
公开(公告)日：2001-11-06
申请号：US09475940
申请日：1999-12-30
申请人： Richard E. Mewshaw , Dahui Zhou , Ping Zhou
发明人： Richard E. Mewshaw , Dahui Zhou , Ping Zhou
IPC分类号： C07D41312
CPC分类号： C07D413/12
摘要： Compounds are provided which have the following formula: wherein: R is hydrogen, alkyl of 1 to 6 carbon atoms, phenyl, or substituted phenyl; X and Y are each, independently, hydrogen, halogen, cyano, or alkoxy of 1 to 6 carbon atoms; and m is 1 to 5; or a pharmaceutically acceptable salt thereof.
摘要翻译：提供具有下式的化合物：其中：R是氢，1至6个碳原子的烷基，苯基或取代的苯基; X和Y各自独立地是氢，卤素，氰基或1-6个碳的烷氧基原子 andm是1到5; 或其药学上可接受的盐。

16. 发明授权

US06211365B1 Fused pyrrolecarboxamides; a new class of GABA brain receptor ligands 失效
标题翻译：熔融吡咯烷酰胺; 一类新的GABA脑受体配体
公开(公告)号：US06211365B1
公开(公告)日：2001-04-03
申请号：US09387313
申请日：1999-08-31
申请人： Pamela Albaugh , Gang Liu , Kenneth Shaw , Alan Hutchison
发明人： Pamela Albaugh , Gang Liu , Kenneth Shaw , Alan Hutchison
IPC分类号： C07D41312
CPC分类号： C07D401/12 , C07D209/42 , C07D209/52 , C07D405/12 , C07D413/12
摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein: G, X, T, n, and R3-R6 are as defined herein, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.
摘要翻译：公开了下式的化合物或其药学上可接受的无毒盐，其中：G，X，T，n和R3-R6如本文所定义，这些化合物是GABAa脑受体的高选择性激动剂，拮抗剂或反向激动剂或GABAa脑受体的激动剂，拮抗剂或反向激动剂的前药。这些化合物可用于诊断和治疗焦虑，睡眠和癫痫发作，用苯二氮卓类药物过量并用于记忆增强。

17. 发明授权

US06177573B1 Process to prepare taxol 失效
标题翻译：紫杉醇的制备方法
公开(公告)号：US06177573B1
公开(公告)日：2001-01-23
申请号：US09304788
申请日：1999-05-04
申请人： Peter G. M. Wuts , Robert C. Kelly
发明人： Peter G. M. Wuts , Robert C. Kelly
IPC分类号： C07D41312
CPC分类号： C07D263/04 , C07B2200/07 , C07C233/83 , C07C233/87 , C07C237/20 , C07C251/44 , C07C255/44 , C07C271/22 , C07C311/19 , C07D263/06 , C07D277/80 , C07D285/125 , C07D305/14 , C07D417/12 , C07F7/1804 , C08L67/07 , C12P7/42 , C12P41/005
摘要： The invention is an oxazolidine ester of silylated baccatin III of formula (VII) which is a useful intermediate to produce pharmaceutically useful anti-cancer compounds.
摘要翻译：本发明是式（VII）的甲硅烷基化浆果赤霉素III的恶唑烷酯，其是产生药学上可用的抗癌化合物的有用中间体。

18. 发明授权

US06743914B2 Kinetic resolutions of chiral 2-and 3-substituted carboxylic acids 有权
标题翻译：手性2-取代和3-取代羧酸的动力学分辨率
公开(公告)号：US06743914B2
公开(公告)日：2004-06-01
申请号：US10300704
申请日：2002-11-20
申请人： Li Deng , Jianfeng Hang , Liang Tang
发明人： Li Deng , Jianfeng Hang , Liang Tang
IPC分类号： C07D41312
CPC分类号： C07D263/20 , C07B53/00 , C07B57/00 , C07B2200/07 , C07C51/00 , C07C51/487 , C07C67/12 , C07C227/34 , C07C269/06 , C07D317/36 , C07D401/14 , C07D453/02 , Y02P20/582 , C07C59/56 , C07C59/48 , C07C59/01 , C07C69/732 , C07C69/675 , C07C271/22
摘要： One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e., a kinetic resolution wherein the yield of the resolved enantiomer or diastereomer, respectively, exceeds the amount present in the original mixture due to the in situ equilibration of the enantiomers or diastereomers under the reaction conditions prior to the resolution step.
摘要翻译：本发明的一个方面涉及手性化合物的外消旋和非对映体混合物的动力学拆分方法。该方法的关键元素是：非外消旋手性叔胺催化剂; 手性底物，例如环状碳酸酯或环状氨基甲酸酯的外消旋或非对映体混合物; 和亲核试剂，例如醇，胺或硫醇。本发明的优选实施方案涉及一种实现α和β-氨基，羟基和硫代羧酸的衍生物的外消旋和非对映体混合物的动力学拆分的方法。在某些实施方案中，本发明的方法实现了底物的外消旋或非对映体混合物的动态动力学拆分，即动力学拆分，其中分辨的对映异构体或非对映体的产率分别超过原始混合物中存在的量涉及在分离步骤之前的反应条件下对映异构体或非对映异构体的原位平衡。

19. 发明授权

US06562967B2 Kinetic resolutions of chiral 2-and-3-substituted carboxylic acids 有权
公开(公告)号：US06562967B2
公开(公告)日：2003-05-13
申请号：US10010752
申请日：2001-11-05
申请人： Li Deng , Jianfeng Hang , Liang Tang
发明人： Li Deng , Jianfeng Hang , Liang Tang
IPC分类号： C07D41312
CPC分类号： C07D263/20 , C07B53/00 , C07B57/00 , C07B2200/07 , C07C51/00 , C07C51/487 , C07C67/12 , C07C227/34 , C07C269/06 , C07D317/36 , C07D401/14 , C07D453/02 , C07C59/48 , C07C59/01 , C07C59/56 , C07C69/732 , C07C69/675 , C07C271/22
摘要： One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e., a kinetic resolution wherein the yield of the resolved enantiomer or diastereomer, respectively, exceeds the amount present in the original mixture due to the in situ equilibration of the enantiomers or diastereomers under the reaction conditions prior to the resolution step.

20. 发明授权

US06515136B1 Methods for the preparation of biphenyl isoxazole sulfonamides 失效
公开(公告)号：US06515136B1
公开(公告)日：2003-02-04
申请号：US09141402
申请日：1998-08-27
申请人： Richard P. Polniaszek , Xuebao Wang , Jeffrey S. DePue , Chennagiri R. Pandit , Kumar G. Gadamasetti , Yadagiri Pendri , Eduardo J. Martinez
发明人： Richard P. Polniaszek , Xuebao Wang , Jeffrey S. DePue , Chennagiri R. Pandit , Kumar G. Gadamasetti , Yadagiri Pendri , Eduardo J. Martinez
IPC分类号： C07D41312
CPC分类号： C07D405/12 , C07D263/32
摘要： Methods for the preparation of biphenyl isoxazole sulfonamides and intermediates thereof. The present invention also relates to the novel intermediates prepared by these methods. The biphenyl isoxazole sulfonamides prepared by the present methods are endothelin antagonists useful, inter alia, for the treatment of hypertension.

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