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91. 发明授权

US07105565B2 Pyrrolcarboxamides and pyrrolcarbothioamides and their agrochemical uses 失效
标题翻译：吡咯烷酰胺和吡咯硫代酰胺及其农用化学品
公开(公告)号：US07105565B2
公开(公告)日：2006-09-12
申请号：US10416219
申请日：2001-11-06
申请人： Harald Walter
发明人： Harald Walter
IPC分类号： A61K31/40 , C07D207/00
CPC分类号： C07D207/34 , A01N43/36 , C07C211/45 , C07C215/68 , C07C215/70 , C07C2601/02 , C07C2602/44
摘要： The invention relates to novel pesticidal pyrrolcarboxamide of the formula (I), wherein X is oxygen or sulfur; R1 is CF3, CF2H or CFH2; R2 is C1–C3alkyl, C1–C3haloalkyl, C1–C3alkoxy-C1–C3alkyl or C1–C3haloalkoxy-C1–C3alkyl; R3 is hydrogen, methyl, CF3 or fluoro; Q is (Q1), (Q2), (Q3), (Q4); R4 is C6–C14bicycloalkyl unsubstituted or substituted by methyl, ethyl or CF3; C6–C14bicycloalkenyl unsubstituted or substituted by methyl, ethyl or CF3; C6–C14bicycloalkadienyl unsubstituted or substituted by methyl, ethyl or CF3; a group of the form (a) wherein R7, R8, R9 are independently of each other C1–C3alkyl or C1–C3haloalkyl; or a group (b) wherein R10 and R11 are independently of each other hydrogen or halogen and n=1 or 2; and R5 and R6 are independently of each other hydrogen or halogen. The novel compounds have plant-protecting properties and are suitable for protecting plants against infestation by phytopathogenic microorganisms.
摘要翻译：本发明涉及式（I）的新型杀虫吡咯烷酰胺，其中X是氧或硫; R 1是CF 3，CF 2 H或CFH 2; R 2是C 1 -C 3烷基，C 1 -C 3烷基，C 1 -C 3烷基，C 1 -C 3烷基，C 1 -C 3烷基，卤代烷基，C 1 -C 3烷氧基-C 1 -C 3烷基或C 1 -C 3烷基， C 3 -C 3卤代烷氧基-C 1 -C 3烷基; R 3是氢，甲基，CF 3或氟; Q为（Q1），（Q2），（Q3），（Q4）; R 4是未被取代的或被甲基，乙基或CF 3 N取代的C 6 -C 14 - 二环烷基; 未取代或被甲基，乙基或CF 3取代的C 6 -C 14 - 二环烯基; 未取代或被甲基，乙基或CF 3取代的C 6 -C 14 - 双环烷二烯基; 其中R 7，R 8，R 9的形式（a）的基团彼此独立地为C 1〜 C 1 -C 3烷基或C 1 -C 3卤代烷基; C 1 -C 3烷基或C 1 -C 3 - 或其中R 10和R 11彼此独立地为氢或卤素且n = 1或2的基团（b）; 并且R 5和R 6彼此独立地为氢或卤素。新型化合物具有植物保护性质，适用于保护植物免受植物病原微生物的侵袭。

92. 发明授权

US07038025B2 Metal complexes of heterocyclic aromatic compounds 失效
标题翻译：杂环芳族化合物的金属络合物
公开(公告)号：US07038025B2
公开(公告)日：2006-05-02
申请号：US10468982
申请日：2002-12-18
申请人： Eriko Matsui , Yuriko Kaino , Toshiyuki Kunikiyo , Yoshifumi Mori , Tatsushiro Hirata
发明人： Eriko Matsui , Yuriko Kaino , Toshiyuki Kunikiyo , Yoshifumi Mori , Tatsushiro Hirata
IPC分类号： C09B45/00 , C07D207/00
CPC分类号： C07D207/32 , C07D207/323
摘要： A novel metal complex of a heterocyclic aromatic compound which shows a low activation energy, is stabilized structurally, is capable of modulation of the structure thereof, and capable of preferably functioning as a molecular device in technological fields. The metal complex of a heterocyclic aromatic compound comprises a transition metal (for example, silver ion) as a central atom, and basic ligands comprised of a 5-membered heterocyclic aromatic compound (for example, pyrrole rings), in which the position of the central atom can be changed by an internal factor such as transfer of an electric charge or by an external factor such as application of an electric field, a change in acidity of the surrounding environment, etc., whereby the number of atoms (or the number of electrons) relating to the coordination ability can be modulated, and, upon polymerization, the conformation can be modulated depending on the position of the central atom.
摘要翻译：显示低活化能的杂环芳族化合物的新型金属络合物在结构上是稳定的，能够调节其结构，并且能够优选在技术领域中用作分子装置。杂环芳族化合物的金属络合物包含作为中心原子的过渡金属（例如银离子）和由5元杂环芳族化合物（例如吡咯环）构成的碱性配体，其中，中心原子可以通过诸如电荷的转移或诸如施加电场的外部因素，周围环境的酸度变化等内部因素而改变，由此原子数（或数）的电子）可以调节，并且在聚合时，可以根据中心原子的位置来调节构象。

93. 发明申请

US20060063942A1 Mitotic kinesin inhibitors 失效
公开(公告)号：US20060063942A1
公开(公告)日：2006-03-23
申请号：US10517576
申请日：2003-06-12
申请人： Kenneth Arrington , Mark Fraley
发明人： Kenneth Arrington , Mark Fraley
IPC分类号： C07D403/02 , C07D207/00
CPC分类号： C07D207/27 , C07D207/20
摘要： The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

94. 发明授权

US06992102B2 Bicyclic modulators of androgen receptor function 失效
公开(公告)号：US06992102B2
公开(公告)日：2006-01-31
申请号：US10685020
申请日：2003-10-14
申请人： Lawrence Hamann , David Augeri , Chongqing Sun , Jeffrey A. Robl , Mark E. Salvati , Tammy Wang
发明人： Lawrence Hamann , David Augeri , Chongqing Sun , Jeffrey A. Robl , Mark E. Salvati , Tammy Wang
IPC分类号： A61K31/40 , C07D207/00
CPC分类号： C07D207/16 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The invention provides compounds of the formula I wherein the substitutents are as described herein.Further provided are methods of using such compounds for the treatment of nuclear hormone receptor-associated conditions, such as age related diseases, for example sarcopenia, and also provided are pharmaceutical compositions containing such compounds.

95. 发明授权

US06946480B2 Glutaminyl based DPIV inhibitors 失效
标题翻译：基于谷氨酰胺基的DPIV抑制剂
公开(公告)号：US06946480B2
公开(公告)日：2005-09-20
申请号：US10244347
申请日：2002-09-16
申请人： Hans-Ulrich Demuth , Torsten Hoffmann , Ulrich Heiser
发明人： Hans-Ulrich Demuth , Torsten Hoffmann , Ulrich Heiser
IPC分类号： C07D295/18 , A61K31/40 , A61K31/426 , A61K38/04 , A61K38/06 , A61K38/07 , A61K38/08 , A61P3/04 , A61P3/10 , A61P17/00 , A61P17/02 , A61P19/02 , A61P25/00 , A61P35/00 , A61P37/00 , A61P37/06 , A61P43/00 , C07D207/04 , C07D277/04 , C07D295/185 , C07K5/083 , C07K5/087 , C07K7/06 , A61K31/425 , C07D207/00
CPC分类号： C07D277/04 , A61K38/04 , A61K38/06 , A61K38/07 , A61K38/08 , C07D207/04 , C07D295/185 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K5/0812 , C07K7/06
摘要： The present invention provides compounds of the formula: wherein X═CH2 or S or pharmaceutical acceptable salts thereof useful for treating conditions mediated by DPIV or DPIV-like enzymes, such as arthritis, obesity, immune and autoimmune disorders, allograft transplantation, cancer, neuronal disorders and dermal diseases.
摘要翻译：本发明提供下式的化合物：其中X-CH 2或S或其药学上可接受的盐可用于治疗由DPIV或DPIV样酶如关节炎，肥胖，免疫和自身免疫介导的病症疾病，同种异体移植，癌症，神经元疾病和皮肤疾病。

96. 发明申请

US20050085644A1 Novel 3-aryl-2,5-dihydroxy-1,4-benzoquinone derivatives, their preparation method and pharmaceutical compositions containing same 审中-公开
标题翻译：新型3-芳基-2,5-二羟基-1,4-苯醌衍生物及其制备方法和含有它们的药物组合物
公开(公告)号：US20050085644A1
公开(公告)日：2005-04-21
申请号：US10503527
申请日：2003-02-04
申请人： Alexandra Dassonville , Anne Breteche , Muriel Duflos , Guillaume Le Baut , Bruno Pfeiffer , Pierre Renard , Nigel Levens , Bernadette Husson-Robert
发明人： Alexandra Dassonville , Anne Breteche , Muriel Duflos , Guillaume Le Baut , Bruno Pfeiffer , Pierre Renard , Nigel Levens , Bernadette Husson-Robert
IPC分类号： A61K31/122 , A61K31/222 , A61K31/4402 , A61P3/10 , C07C45/00 , C07C45/28 , C07C46/00 , C07C46/10 , C07C50/28 , C07C50/30 , C07D213/50 , C07C50/38 , C07D207/00 , C07D213/46
CPC分类号： C07D213/50 , C07C45/00 , C07C45/28 , C07C46/00 , C07C50/28 , C07C49/245
摘要： Compound of formula (I): wherein: R1 and R2, which may be identical or different, each represents hydrogen, acyl or alkyl, Ar represents aryl or heteroaryl, A represents a group selected from: R4 represents hydrogen or alkyl, R5 represents hydrogen, alkyl, aryl or heteroaryl, R3 represents aryl, heteroaryl, dicyclopropylmethyl or benzhydryl, or A-R3 represents an optionally substituted naphthyl group, with the exclusion of 2,5-dihydroxy-3-(4-methoxyphenyl)-6-(2-phenylethenyl)-1,4-benzoquinone, 2,5-dihydroxy-3-(4-methoxyphenyl)-6-(2-naphthyl)-1,4-benzoquinone and 2,5-dihydroxy-3-(2-naphthyl)-6-phenyl-1,4-benzoquinone. Medicinal products containing the same which are useful in the treatment of diseases associated with a deregulation of glycaemia.
摘要翻译：式（I）化合物：其中：R 1和R 2可以相同或不同，各自表示氢，酰基或烷基，Ar表示芳基或杂芳基， A表示选自以下的基团：R 4表示氢或烷基，R 5表示氢，烷基，芳基或杂芳基，R 3表示芳基，杂芳基，二环丙基甲基或二苯甲基或AR 3 3表示任选取代的萘基，排除2,5-二羟基-3-（4-甲氧基苯基）-6-（2-苯基乙烯基）-6- 1,4-苯醌，2,5-二羟基-3-（4-甲氧基苯基）-6-（2-萘基）-1,4-苯醌和2,5-二羟基-3-（2-萘基）-6- 苯基-1,4-苯醌。含有该药物的药物可用于治疗与血糖失调相关的疾病。

97. 发明申请

US20040063897A1 Method for the preparation poly(etherimide)s 失效
标题翻译：制备聚（醚酰亚胺）的方法
公开(公告)号：US20040063897A1
公开(公告)日：2004-04-01
申请号：US10065197
申请日：2002-09-25
发明人： Roy Ray Odle , Thomas Link Guggenheim
IPC分类号： C08G073/00 , C08G075/00 , C08G069/08 , C08G073/10 , C07D207/00 , C07D295/00
CPC分类号： C07D209/48 , C07D401/04 , C07D401/14
摘要： A method for the synthesis of poly(etherimide)s comprises the reaction of 4-halotetrahydrophthalic anhydride with an activating primary amine to yield an activated 4-halotetrahydrophthalimide. Activated 4-halotetrahydrophthalimide may then be aromatized and treated with the disodium salt of a bis(phenol) to yield an activated bisimide. The activated bisimide may then be directly treated with a diamine to yield poly(etherimide)s.
摘要翻译：用于合成聚（醚酰亚胺）的方法包括4-卤代四氢邻苯二甲酸酐与活化伯胺的反应，得到活化的4-卤代四氢邻苯二甲酰亚胺。然后将活化的4-卤代四氢邻苯二甲酰亚胺芳构化并用双（苯酚）的二钠盐处理，得到活化的双酰亚胺。然后可以用二胺直接处理活化的双酰亚胺以产生聚（醚酰亚胺）。

98. 发明申请

US20040019100A1 HMG CoA-reductase inhibitors 失效
标题翻译： HMG辅酶A还原酶抑制剂
公开(公告)号：US20040019100A1
公开(公告)日：2004-01-29
申请号：US10429609
申请日：2003-05-05
发明人： Yatendra Kumar , Ram Chander Aryan , Jitendra Sattigeri , Mohammad Salman , Gowri Shankar , Kumar Hari Bhushan , Bhargav R. Pandya , Ramnik Sharma
IPC分类号： A61K031/401 , C07D207/00
CPC分类号： C07D207/34
摘要： The invention relates to particular hydroxyl and protected hydroxyl derivatives of compounds known to be useful as HMG CoA-reductase inhibitors. In particular, herein are provided hydroxyl and protected hydroxyl compounds of Formula I 1 and their corresponding lactones.
摘要翻译：本发明涉及已知可用作HMG CoA还原酶抑制剂的化合物的特定羟基和被保护的羟基衍生物。特别地，本文提供式I的羟基和保护的羟基化合物及其相应的内酯。

99. 发明申请

US20030078247A1 Alpha-amino-acid compounds 失效
标题翻译： α-氨基酸化合物
公开(公告)号：US20030078247A1
公开(公告)日：2003-04-24
申请号：US10146272
申请日：2002-05-15
发明人： Guillaume De Nanteuil , Bernard Portevin , Alain Benoist , Nigel Levens , Olivier Nosjean , Bernadette Husson-Robert , Michelle Boulanger
IPC分类号： A61K031/33 , C07D207/00
CPC分类号： C07D295/185 , C07D207/16 , C07D277/04 , C07D277/06 , Y02P20/55
摘要： Compound selected from those of formula (I): 1 wherein 2 nullrepresents an optionally substituted 5-membered nitrogen-containing heterocycle, Ak represents an alkylene chain, X represents a single bond or phenylene, R1 and R2, which may be identical or different, each represent hydrogen or alkyl, R3 represents alkyl, nitro or cyano, Y represents NR4 or CHNO2, R4 represents hydrogen or alkyl, its tautomers when they exist, its optical isomers, and addition salts thereof with a pharmaceutically acceptable acid, with the exclusion of compounds wherein, simultaneously, 3 represents an unsubstituted 5-membered nitrogen-containing heterocycle, Ak represents null(CH2)3null, X represents a single bond, Y represents NH and R3 represents nitro. Medicinal products containing the same which are useful as dipeptidyl peptidase IV inhibitors.
摘要翻译：选自式（I）的化合物：其中表示任选取代的5元含氮杂环，Ak表示亚烷基链，X表示单键或亚苯基，可以相同或不同的R 1和R 2各自表示氢或烷基，R 3表示烷基，硝基或氰基，Y表示NR 4或CHNO 2，R 4表示氢或烷基，其互变异构体存在时，其光学异构体及其与药学上可接受的酸的加成盐，同时代表未取代的5元含氮杂环，Ak表示 - （CH2）3-，X表示单键，Y表示NH，R3表示硝基。含有它们的药用产品可用作二肽基肽酶IV抑制剂。

100. 发明申请

US20020156293A1 Process for the preparation of zofenopril calcium salt 失效
标题翻译：制备佐芬普利钙盐的方法
公开(公告)号：US20020156293A1
公开(公告)日：2002-10-24
申请号：US10155129
申请日：2002-05-28
申请人： MENARI RICERCHE S.P.A.
发明人： Raffaello Giorgi , Antonio Giachetti , Carlo Mannucci , Anita Falezza , Rosaria Pirari , Alberta Giorgi
IPC分类号： C07D207/00 , A61K031/40
CPC分类号： C07D207/16
摘要： A process for the preparation of polymorph A of zofenopril calcium salt in substantially pure form, which comprises: 1) reaction of S(-)-3-benzoylthio-2-methylpropanoic acid chloride with cis-4-phenylthio-L-proline in water at pH ranging from 9.0 to 9.5 and recovery of zofenopril in the acidic form; b) salification of acid zofenopril with a potassium salt in alcoholic solution, and recovery of the resulting potassium salt; c) conversion of the potassium salt to the calcium salt by addition of zofenopril potassium salt aqueous solution to a CaCl2 aqueous solution at a temperature of 70-90null C. with simultaneous seeding to promote the precipitation of polymorph A.
摘要翻译：一种以基本纯净的形式制备佐芬普利钙盐的多晶型A的方法，其包括：1）S（ - ） - 3-苯甲酰硫基-2-甲基丙酰氯与顺式-4-苯硫基-L-脯氨酸在水中的反应在9.0至9.5的pH范围内，并以酸性形式回收佐芬普利; b）酸性佐芬普利与醇溶液中的钾盐成盐，并回收得到的钾盐; c）通过在70-90℃的温度下将佐芬普利钾盐水溶液加入CaCl 2水溶液中将钾盐转化为钙盐，同时接种以促进多晶型物A的沉淀。

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