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1. 发明授权

US06800652B2 Diaryl compounds 失效
标题翻译：二芳基化合物
公开(公告)号：US06800652B2
公开(公告)日：2004-10-05
申请号：US10632355
申请日：2003-07-31
申请人： Mark David Andrews , David Hepworth , Donald Stuart Middleton
发明人： Mark David Andrews , David Hepworth , Donald Stuart Middleton
IPC分类号： C07D21302
CPC分类号： C07D213/70 , C07D213/38
摘要： The invention relates to compounds of formula I
摘要翻译：本发明涉及式I化合物

2. 发明授权

US06677339B2 Phenylalanine derivatives 失效
标题翻译：苯丙氨酸衍生物
公开(公告)号：US06677339B2
公开(公告)日：2004-01-13
申请号：US09927874
申请日：2001-08-10
申请人： John Clifford Head , John Robert Porter , Graham John Warrellow , Sarah Catherine Archibald , Brian Woodside Hutchinson
发明人： John Clifford Head , John Robert Porter , Graham John Warrellow , Sarah Catherine Archibald , Brian Woodside Hutchinson
IPC分类号： C07D21302
CPC分类号： C07D213/81 , C07D213/89 , C07D251/30 , C07D251/46 , C07D401/12 , C07D409/12 , C07D413/12
摘要： Phenylalanine derivatives of formula (1) are described: in which: Ar1 is an aromatic or heteroaromatic group; L1 is a linker atom or group; R is a carboxylic acid or a derivative thereof; Ar2 is an optionally substituted aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of &agr;4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.
摘要翻译：描述了式（1）的苯丙氨酸衍生物：其中：Ar 1是芳族或杂芳族基团; L 1是连接原子或基团; R是羧酸或其衍生物; Ar 2是任选取代的芳族或杂芳族基团;以及其盐，溶剂合物，水合物和N-氧化物。化合物能够抑制α4整联蛋白与其配体的结合，并且可用于预防和治疗免疫或炎性疾病。

3. 发明授权

US06610714B2 Non-nucleoside reverse transcriptase inhibitors 失效
标题翻译：非核苷逆转录酶抑制剂
公开(公告)号：US06610714B2
公开(公告)日：2003-08-26
申请号：US10093112
申请日：2002-03-05
申请人： Christer Sahlberg , Dmitry Antonov , Hans Wallberg , Rolf Noréen
发明人： Christer Sahlberg , Dmitry Antonov , Hans Wallberg , Rolf Noréen
IPC分类号： C07D21302
CPC分类号： C07D213/75 , C07D213/85
摘要： Compounds of the formula I: where; R1 is O, S; R2 is an optionally substituted nitrogen-containing heterocycle, wherein the nitrogen is located at the 2 position relative to the (thio)urea bond; R3 is H, C1-C3 alkyl, R4-R7 are independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, haloC1-C6 alkyl, C1-C6 alkanoyl, haloC1-C6 alkanoyl, C1-C6 alkoxy, haloC1-C6 alkoxy, C1-C6 alkyloxy-C1-C6 alkyl, haloC1-C6 alkyloxy-C1-C6 alkyl hydroxy-C1-C6 alkyl, amino-C1-C6 alkyl, carboxy-C1-C6 alkyl, cyano-C1-C6 alkyl, amino, carboxy, carbamoyl, cyano, halo, hydroxy, keto; X is —(CR8R9)n— R8 and R9 are independently H, C1-C3 alkyl, OH or R8 and R9 together are ═O n is 1, 2 or 3 and prodrugs and pharmaceutically acceptable salts thereof, have utility as inhibitors of HIV-1 reverse transcriptase, particularly drug escape mutants.
摘要翻译：式I化合物：其中R 1为O，S; R 2为任选取代的含氮杂环，其中氮位于相对于（硫）脲键的2位; R 3为H，C 1 -C 3烷基，R 4 -R 7独立地选自H，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷基，C 1 -C 6烷酰基，卤代C 1 -C 6烷酰基，C 1 -C 6烷氧基，卤代C 1 -C 6烷氧基， C 1 -C 6烷氧基-C 1 -C 6烷基，卤代C 1 -C 6烷氧基-C 1 -C 6烷基羟基-C 1 -C 6烷基，氨基-C 1 -C 6烷基，羧基-C 1 -C 6烷基，氰基-C 1 -C 6烷基，氨基，羧基，氨基甲酰基，氰基，卤素，羟基，酮基; X是 - （CR8R9）n-R8和R9独立地是H，C1-C3烷基，OH或R8和R9一起= On是1,2或3，前药和药学上可接受的其盐可用作HIV-1逆转录酶的抑制剂，特别是药物逃避突变体。

4. 发明授权

US06489325B1 Substituted imidazole compounds 失效
标题翻译：取代的咪唑化合物
公开(公告)号：US06489325B1
公开(公告)日：2002-12-03
申请号：US09446147
申请日：2000-03-30
申请人： Jerry L. Adams , Ralph F. Hall
发明人： Jerry L. Adams , Ralph F. Hall
IPC分类号： C07D21302
CPC分类号： C07D403/04
摘要： The present invention relates to novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as CSBP/p38 inhibitors.
摘要翻译：本发明涉及用作CSBP / p38抑制剂治疗的新型1,4,5-取代咪唑化合物和组合物。

5. 发明授权

US06472413B2 Heteroarylacryloylaminoalkyl-substituted benzenesulfonamide derivatives, their preparation, their use and pharmaceutical preparations comprising them 有权
标题翻译：杂芳基丙烯酰基氨基烷基取代的苯磺酰胺衍生物，其制备方法，用途和包含它们的药物制剂
公开(公告)号：US06472413B2
公开(公告)日：2002-10-29
申请号：US09985359
申请日：2001-11-02
申请人： Holger Heitsch , Heinrich Christian Englert
发明人： Holger Heitsch , Heinrich Christian Englert
IPC分类号： C07D21302
CPC分类号： C07D409/12 , C07D213/56 , C07D333/24
摘要： One embodiment of the present invention relates to heteroarylacryloylaminoalkyl-substituted benzenesulfonamide derivatives of the formula (I), in which R(1), R(2), R(3), R(4), Het, X, Y and Z have the meanings indicated in the specification, and to pharmaceutically tolerable salts thereof. The compounds of the invention are valuable pharmaceutically active compounds that have, for example, an at inhibitory action on ATP-sensitive potassium channels in the cardiac muscle and/or in the vagal cardiac nerve and are suitable, for example, for the treatment of disorders of the cardiovascular system such as coronary heart disease, arrhythmias, cardiac insufficiency, cardiomyopathies, decreased contractility of the heart, or vagal dysfunction of the heart, or for the prevention of sudden cardiac death. The invention furthermore relates to processes for the preparation of the compounds of the formula (I) and pharmaceutically tolerable salts thereof, their use, and pharmaceutical preparations comprising them.
摘要翻译：本发明的一个实施方案涉及式（I）的杂芳基丙烯酰氨基烷基取代的苯磺酰胺衍生物，其中R（1），R（2），R（3），R（4），Het，X，Y和Z具有说明书中指出的含义及其药学上可耐受的盐。本发明的化合物是有价值的药物活性化合物，其具有例如对心肌和/或迷走神经心脏神经中对ATP敏感的钾通道的抑制作用，并且适合于例如治疗疾病的心血管系统如冠心病，心律不齐，心功能不全，心肌病，心脏收缩力减退或心脏迷走神经功能障碍，或用于预防心源性猝死。本发明还涉及制备式（I）化合物及其药学上可接受的盐，其用途和包含它们的药物制剂的方法。

6. 发明授权

US06281231B1 2,6-dichloro-4-pyridinemethanol derivatives and agricultural chemicals 失效
标题翻译： 2,6-二氯-4-吡啶甲醇衍生物和农药
公开(公告)号：US06281231B1
公开(公告)日：2001-08-28
申请号：US09508261
申请日：2000-03-09
申请人： Toru Asada , Mika Iiyama , Hiroyuki Tsuboi , Takashi Gotou
发明人： Toru Asada , Mika Iiyama , Hiroyuki Tsuboi , Takashi Gotou
IPC分类号： C07D21302
CPC分类号： C07D401/12 , A01N43/40 , A01N47/06 , A01N47/12 , A01N47/20 , A01N53/00 , A01N55/00 , A01N57/16 , C07D213/61 , C07D405/12 , C07D409/12
摘要： The object is to provide a novel compound, with which there is little possibility of phytotoxicity for crop plants, and which is greatly effective in controlling various plant diseases caused by viruses pathogenic to plants, by bacteria, and by molds, and to provide agricultural chemicals, particularly agents for controlling plant diseases, containing this compound, 2,6-dichloro-4-pyridinemethanol, and/or a benzoic acid ester thereof as an active ingredient. As means for achieving the object, 2,6-dichloro-4-pyridinemethanol derivatives, 2,6-dichloro-4-pyridinemethanol, benzoic acid esters thereof, and agricultural chemicals containing these compounds as active ingredients are provided, the 2,6-dichloro-4-pyridinemethanol derivative being expressed by general formula (1): wherein W denotes an optionally substituted C1 to C8 alkyl group, a trifluoromethylpyridyl group, —COR1, —SO2R2, —PO(OR3)2, —CONHR4, —COOR4, —COCOR4, or —SiR5R6R7, in which: R1 denotes an optionally substituted C1 to C18 alkyl group, an optionally substituted C1 to C18 alkenyl group, a phenyl group which has one or more specific substituent groups, or a 5- or 6-membered heterocyclic ring residue which has any one of a nitrogen atom, an oxygen atom, or a sulfur atom as a ring component atom; R2 denotes an alkyl group or a phenyl group; R3 denotes an alkyl group; R4 denotes an alkyl group or a phenyl group; and each of R5 to R7 denotes an alkyl group.
摘要翻译：目的是提供一种新型化合物，对作物植物毒性的可能性很小，对于控制由植物，细菌和霉菌致病的病毒引起的各种植物病害，并且提供农药特别是用于控制植物病害的药剂，含有该化合物，2,6-二氯-4-吡啶甲醇和/或其苯甲酸酯作为活性成分。作为实现目的的手段，提供2,6-二氯-4-吡啶甲醇衍生物，2,6-二氯-4-吡啶甲醇，苯甲酸酯和含有这些化合物作为活性成分的农药，二氯-4-吡啶甲醇衍生物由通式（1）表示：其中W表示任选取代的C1至C8烷基，三氟甲基吡啶基，-COR1，-SO2R2，-PO（OR3）2，-CONHR4，-COOR4， -COCOR 4或-SiR 5 R 6 R 7，其中：R 1表示任选取代的C 1至C 18烷基，任选取代的C 1至C 18烯基，具有一个或多个特定取代基的苯基或5-或6-元具有氮原子，氧原子或硫原子中的任一个作为环成分原子的杂环残基; R2表示烷基或苯基; R3表示烷基; R4表示烷基或苯基; R5〜R7各自表示烷基。

7. 发明授权

US06172091B2 1,2-Disubstituted cyclopropanes 有权
标题翻译： 1,2-二取代环丙烷
公开(公告)号：US06172091B2
公开(公告)日：2001-01-09
申请号：US09417319
申请日：1999-10-13
申请人： Judith Hope Cohen , Donald Ward Combs , Philip James Rybczynski
发明人： Judith Hope Cohen , Donald Ward Combs , Philip James Rybczynski
IPC分类号： C07D21302
CPC分类号： C07C217/58 , C07D213/36
摘要： Compounds of Formula I wherein the substituents are as described in the specification or pharmaceutically acceptable salts or stereochemically isomeric forms thereof, useful for treating diseases related to calcium imbalance and metabolism.
摘要翻译：取代基中的式I化合物如说明书或其药学上可接受的盐或立体化学异构体形式所述，可用于治疗与钙不平衡和代谢有关的疾病。

8. 发明授权

US06794396B2 Substituted pyridines useful for inhibiting cholesteryl ester transfer protein activity 失效
标题翻译：用于抑制胆固醇酯转移蛋白活性的取代的吡啶
公开(公告)号：US06794396B2
公开(公告)日：2004-09-21
申请号：US10403903
申请日：2003-03-31
申请人： Len F. Lee , Kevin C. Glenn , Daniel T. Connolly , David G. Corley , Daniel L. Flynn , Ashton T. Hamme , Shridhar G. Hegde , Michele A. Melton , Roger J. Schilling , James A. Sikorski , Nancy N. Wall , Jeffery A. Zablocki
发明人： Len F. Lee , Kevin C. Glenn , Daniel T. Connolly , David G. Corley , Daniel L. Flynn , Ashton T. Hamme , Shridhar G. Hegde , Michele A. Melton , Roger J. Schilling , James A. Sikorski , Nancy N. Wall , Jeffery A. Zablocki
IPC分类号： C07D21302
CPC分类号： A61K31/44
摘要： A class of substituted pyridines that are useful for inhibiting the activity of cholesteryl ester transfer protein, and have the structural formula (IA), wherein R2, R3, R4, R5, and R6 are defined in the claims.
摘要翻译：一类可用于抑制胆固醇酯转移蛋白活性的取代吡啶，并具有结构式（IA），其中R 2，R 3，R 4，R 5和R 6在权利要求书中定义。

9. 发明授权

US06630495B1 Fungicides 有权
标题翻译：杀菌剂
公开(公告)号：US06630495B1
公开(公告)日：2003-10-07
申请号：US10049981
申请日：2002-07-22
申请人： Tracey Cooke , Tennyson Ekwuru , David Hardy , Peter Millward , Brian Moloney , Andrew Pettinger , Peter Stanley Thomas , Richard Michael Turner
发明人： Tracey Cooke , Tennyson Ekwuru , David Hardy , Peter Millward , Brian Moloney , Andrew Pettinger , Peter Stanley Thomas , Richard Michael Turner
IPC分类号： C07D21302
CPC分类号： A01N43/90 , A01N43/40 , A01N43/42 , A01N43/50 , A01N43/54 , A01N43/56 , A01N43/60 , A01N43/78 , A01N43/80 , A01N43/82 , A01N47/24 , A01N47/38 , A01N47/40 , A01N53/00
摘要： Compounds of formula (I) or (II): or salts therefor are used as phytopathogenic fungicides wherein the various radicals and substitutents are as defined in the description. Pesticidal compositions contain these compounds together with an agriculturally acceptable diluent or carrier. The compounds and compositions are applied in methods for combating pests.
摘要翻译：式（I）或（II）的化合物或其盐用作植物病原性杀真菌剂，其中各种基团和取代基如说明书中所定义。杀虫组合物含有这些化合物以及农业上可接受的稀释剂或载体。化合物和组合物应用于防治害虫的方法中。

10. 发明授权

US06528651B1 Method for production of 1,3-disubtituted 2-nitroguanidines 有权
标题翻译：生产1,3-二取代的2-硝基胍的方法
公开(公告)号：US06528651B1
公开(公告)日：2003-03-04
申请号：US10149891
申请日：2002-06-14
申请人： Kai van Laak , Wolfram Sirges , Detlef Wollweber
发明人： Kai van Laak , Wolfram Sirges , Detlef Wollweber
IPC分类号： C07D21302
CPC分类号： C07D277/32 , C07D213/61 , C07D307/14
摘要： The present invention relates to a process for the preparation of compounds of the formula (I) by reacting compounds of the formula (II) in which Het, R1, R2 and R4 are as defined in the description, with anhydrous hydrogen chloride or compounds which generate hydrogen chloride.
摘要翻译：本发明涉及通过使式（II）化合物（其中Het，R 1，R 2和R 4如说明书中所定义）与无水氯化氢反应制备式（I）化合物的方法或产生氯化氢。

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