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32. 发明申请

WO0149278A3 COMPOUNDS AND COMPOSITIONS FOR USE IN INHIBITING ENDOPARASITIC FATTY ACID BIOSYNTHESIS 审中-公开
标题翻译：用于抑制内毒素脂肪酸生物合成的化合物和组合物
公开(公告)号：WO0149278A3
公开(公告)日：2002-04-11
申请号：PCT/GB0100082
申请日：2001-01-08
申请人： UNIV CARDIFF , BERRY COLIN , HARWOOD JOHN L
发明人： BERRY COLIN , HARWOOD JOHN L
IPC分类号： C07D333/32 , A61K31/381 , A61K45/00 , A61P33/00 , A61P33/02 , A61P33/06 , A61P43/00 , C07D409/06 , A61K31/38
CPC分类号： A61K31/381
摘要： Use of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, as an inhibitor of at least one beta -ketoacyl acyl carrier protein synthase operable in the fatty acid biosynthesis of endoparasites, which compound is of the general formula (I) where R1 is selected from the group consisting of hydrogen, alkyl, (cyano)alkylene, alkenyl, alkynyl, (alkoxy)alkylene, (alkoxy)alkenylene, (alkoxy)alkynylene, cycloalkyl, (cycloalkyl)alkylene, (cycloalkyl)alkenylene, (cycloalkyl)alkynylene, (heterocycle)alkylene, (heterocycle)alkenylene, (heterocycle)alkynylene, aryl, (aryl)alkylene, (aryl)alkenylene, (aryl)alkynylene, (arylcarbonylarylene)alkylene, (arylcarbonylarylene)alkenylene and (arylcarbonylarylene)alkynylene; R2 is alkyl or cycloalkyl; R3 is alkyl or cycloalkyl; and R4 is hydrogen or alkyl; including racemic mixtures and enantiomers of said compound when the latter is chiral, but excluding the racemic mixture of a chiral compound of formula (I) in which R1 is CH2=CH-C(CH3)=CH-, R2 is methyl, R3 is methyl and R4 is hydrogen.
摘要翻译：至少一种化合物或其药学上可接受的盐或前药作为至少一种可在内寄生虫的脂肪酸生物合成中操作的β-酮酰酰基载体蛋白合成酶的抑制剂的用途，该化合物具有通式（I），其中R 1 （烷氧基）亚烷基，（烷氧基）亚烯基，（烷氧基）亚炔基，环烷基，（环烷基）亚烷基，（环烷基）亚烯基，（环烷基）亚芳基，（亚芳基）亚烷基，（芳基）亚烯基，（芳基羰基亚芳基）亚烷基，（芳基羰基亚芳基）亚烯基和（芳基羰基亚芳基）亚炔基） R2是烷基或环烷基; R3是烷基或环烷基; 和R4是氢或烷基; 包括当后者为手性时所述化合物的外消旋混合物和对映异构体，但不包括其中R 1为CH 2 = CH-C（CH 3）= CH-的式（I）的手性化合物的外消旋混合物，R 2为甲基，R 3为甲基，R4为氢。

33. 发明申请

WO02026694A1 O-SUBSTITUTED 6-METHYL-TRAMADOL DERIVATIVES 审中-公开
标题翻译： O-取代的6-甲基曲马朵衍生物
公开(公告)号：WO02026694A1
公开(公告)日：2002-04-04
申请号：PCT/EP2001/011276
申请日：2001-09-28
IPC分类号： C07D333/20 , A61K31/135 , A61K31/35 , A61K31/381 , A61P1/06 , A61P15/12 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P29/00 , A61P41/00 , C07C213/00 , C07C215/42 , C07C215/64 , C07C217/74 , C07D333/32
CPC分类号： C07C217/74 , C07C215/42 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D333/32
摘要： The invention relates to O-substituted 6-methyl-tramadol derivatives, to methods for producing them, to medicaments containing these compounds and to the use of O-substituted 6-methyl-tramadol derivatives for producing medicaments for treating pain.
摘要翻译：本发明涉及O-取代-6-甲基反胺苯环醇衍生物，它们的制备方法，包含这些化合物和用于制备药物用于治疗疼痛的药物中的用途O-取代-6-甲基反胺苯环醇衍生物的药物组合物。

34. 发明申请

WO01098292A1 NOVEL ELECTRO-OPTIC CHROMOPHORE BRIDGE COMPOUNDS AND DONOR-BRIDGE COMPOUNDS FOR POLYMERIC THIN FILM WAVEGUIDES 审中-公开
标题翻译：用于聚合物薄膜波形的新型电光色谱桥接化合物和多核化合物
公开(公告)号：WO01098292A1
公开(公告)日：2001-12-27
申请号：PCT/US2001/015818
申请日：2001-05-16
IPC分类号： C07D307/52 , C07D307/58 , C07D333/20 , C07D333/32 , C07F9/655 , C07F9/6553 , C07D335/04 , C07C47/00 , C07C47/52 , C07C49/105 , C07C205/00 , C07D307/00 , C07D307/02 , C07D311/04 , C07D333/02 , C07D333/08 , C07F9/02
CPC分类号： C07D307/58 , C07D307/52 , C07D333/20 , C07D333/32 , C07F9/65515 , C07F9/65522 , C07F9/655345
摘要： The present invention is directed to electro-optico chromophore bridge compounds and donor-bridge compounds which can be used in the preparation of polymeric thin films for waveguide media.
摘要翻译：本发明涉及可用于制备用于波导介质的聚合物薄膜的电光发色团桥接化合物和供体 - 桥接化合物。

35. 发明申请

WO01085664A2 COMPOUNDS AND METHODS FOR REGULATING BACTERIAL GROWTH AND PATHOGENESIS 审中-公开
标题翻译：化合物和调节细菌生长和致病的方法
公开(公告)号：WO01085664A2
公开(公告)日：2001-11-15
申请号：PCT/US2001/015221
申请日：2001-05-10
IPC分类号： G01N33/50 , A61K31/00 , A61K31/12 , A61K31/121 , A61K31/122 , A61K31/201 , A61K31/215 , A61K31/34 , A61K31/341 , A61K31/351 , A61K31/357 , A61K31/365 , A61K31/38 , A61K31/381 , A61K31/385 , A61K31/40 , A61K31/42 , A61K31/43 , A61K31/496 , A61K38/00 , A61K39/00 , A61K45/00 , A61K45/06 , A61P31/04 , A61P43/00 , C07C49/395 , C07C49/597 , C07C49/647 , C07C69/145 , C07D215/56 , C07D261/16 , C07D307/12 , C07D307/20 , C07D307/32 , C07D307/33 , C07D307/58 , C07D307/60 , C07D309/10 , C07D317/20 , C07D317/34 , C07D333/32 , C07D499/68 , C07K14/28 , C12N1/20 , C12P7/26 , C12Q1/02 , C12Q1/18 , C12R1/63 , G01N33/15 , C07C49/00
CPC分类号： C12Q1/18 , A61K31/00 , A61K31/34 , A61K31/365 , A61K31/38 , A61K31/385 , A61K31/40 , A61K39/00 , A61K45/06 , C07K14/28 , Y02A50/401 , Y02A50/47 , Y02A50/472 , A61K2300/00
摘要： The invention provides autoinducer-2 analogs that regulate the activity of autoinducer-2 and methods of using such analogs for regulating bacterial growth and pathogenesis.
摘要翻译：本发明提供了调节自体诱导剂-2的活性的自动诱导剂-2类似物和使用这种类似物调节细菌生长和发病机理的方法。

36. 发明申请

WO01049674A2 GLYCOSIDASE INHIBITORS AND METHODS OF SYNTHESIZING SAME 审中-公开
标题翻译：糖苷酶抑制剂及其合成方法
公开(公告)号：WO01049674A2
公开(公告)日：2001-07-12
申请号：PCT/CA2001/000010
申请日：2001-01-05
IPC分类号： C07D333/32 , A61K31/33 , A61K31/381 , A61K31/40 , A61P3/08 , A61P3/10 , A61P25/28 , A61P35/00 , A61P35/04 , A61P43/00 , C07B61/00 , C07D207/12 , C07D333/46 , C07D345/00 , C07D405/06 , C07D409/06 , C07D421/06 , C07D497/04 , C07D333/00
CPC分类号： C07D333/46 , C07D207/12 , C07D345/00
摘要： A method for synthesizing Salacinol, its stereoisomers, and non-naturally occurring selenium and nitrogen analogues thereof having formula (I). The compounds are potentially useful as glycosidase inhibitors. The synthetic schemes comprise reacting a cyclic sulfate with a 5-membered ring sugar containing a heteroatom (X). The heteroatom preferably comprises sulfur, selenium, or nitrogen. The cyclic sulfate and ring sugar reagents may be readily prepared from carbohydrate precursors, such as D-glucose, L-glucose, D-xylose and L-xylose. The target compounds are prepared by opening of the cyclic sulfates by nucleophilic attack of the heteroatoms on the 5-membered ring sugars. The resulting heterocyclic compounds have a stable, inner salt structure comprising a heteroatom cation and a sulfate anion. The synthetic schemes yield various stereoisomers of the target compounds in moderate to good yields with limited side-reactions. In an alternative embodiment of the invention, the cyclic sulfate may be similarly reacted with a 6-membered ring sugar containing a heteroatom (X) to yield a compound having formula (XII).
摘要翻译：一种用于合成具有式（I）的Salacinol，其立体异构体和非天然存在的硒和氮类似物的方法。这些化合物可能用作糖苷酶抑制剂。合成方案包括使环硫酸盐与含有杂原子（X）的5元环糖反应。杂原子优选包含硫，硒或氮。环状硫酸盐和环糖试剂可以容易地从碳水化合物前体如D-葡萄糖，L-葡萄糖，D-木糖和L-木糖制备。通过在5元环糖上的杂原子的亲核攻击来打开环状硫酸盐来制备目标化合物。所得的杂环化合物具有包含杂原子阳离子和硫酸根阴离子的稳定的内盐结构。合成方案以有限的副反应以中等到良好的产率产生目标化合物的各种立体异构体。在本发明的一个替代实施方案中，环状硫酸盐可以类似地与含有杂原子（X）的6元环糖反应，得到具有式（XII）的化合物。

37. 发明申请

WO01010825A1 CARBAMATE DERIVATIVES AND AGRICULTURAL/HORTICULTURAL BACTERICIDES 审中-公开
标题翻译：碳酸盐衍生物和农业/农业细菌
公开(公告)号：WO01010825A1
公开(公告)日：2001-02-15
申请号：PCT/JP2000/005225
申请日：2000-08-03
IPC分类号： C07C217/20 , A01N47/12 , A01N47/28 , A01P3/00 , C07C271/20 , C07C271/22 , C07C275/24 , C07C317/18 , C07C323/12 , C07C327/58 , C07C327/60 , C07C333/04 , C07D213/30 , C07D213/64 , C07D213/70 , C07D213/74 , C07D213/79 , C07D213/84 , C07D215/14 , C07D237/14 , C07D239/26 , C07D239/34 , C07D277/24 , C07D277/64 , C07D295/08 , C07D303/20 , C07D333/32 , C07D213/65 , C07D213/81 , C07D215/22 , C07D239/56 , C07D239/60 , C07D307/12 , C07D317/22
CPC分类号： C07D213/30 , A01N47/12 , A01N47/28 , C07C271/20 , C07C271/22 , C07C275/24 , C07C317/18 , C07C323/12 , C07C327/58 , C07C327/60 , C07C333/04 , C07D213/64 , C07D213/70 , C07D213/74 , C07D213/79 , C07D213/84 , C07D215/14 , C07D239/26 , C07D239/34 , C07D277/64 , C07D333/32
摘要： Novel bactericides having an excellent controlling effect on plant disease injury (in particular, wheat powdery mildew and cucumber gray mold) without exerting any undesirable effect on crops. Carbamate derivatives represented by general formula [I] and agricultural/horticultural bactericides containing the same as the active ingredient wherein X represents halogeno, C1-6 alkyl, etc.; n is 0 or an integer of from 1 to 4; R represents C1-6 alkyl; R represents hydrogen, C1-6 alkyl, etc.; R represents hydrogen or C1-6 alkyl; G represents oxygen, sulfur, etc.; Y represents C1-10 alkyl; C2-10 alkenyl, etc.; and Q represents hydrogen, C1-6 haloalkyl, phenyl, etc.
摘要翻译：对植物病害损害（特别是小麦白粉病和黄瓜灰霉菌）具有优异防治作用的新型杀菌剂，对作物不产生不良影响。由通式[I]表示的氨基甲酸酯衍生物和含有与活性成分相同的农业/园艺杀菌剂，其中X表示卤代C 1-6烷基等; n为0或1〜4的整数; R 1表示C 1-6烷基; R 2表示氢，C 1-6烷基等; R 3表示氢或C 1-6烷基; G代表氧，硫等; Y表示C1-10烷基; C2-10烯基等; Q表示氢，C 1-6卤代烷基，苯基等。

38. 发明申请

WO00053613A1 CHEMICAL VAPOR DEPOSITION PRECURSORS AND THERMOCHROMIC MATERIALS THEREOF 审中-公开
标题翻译：化学气相沉积前驱体及其热变性材料
公开(公告)号：WO00053613A1
公开(公告)日：2000-09-14
申请号：PCT/US2000/004955
申请日：2000-02-28
IPC分类号： B41M5/28 , C07D233/96 , C07D243/04 , C07D333/32 , C07F9/70 , C07F9/90 , C07F9/94 , C07F9/00 , C07F9/02
CPC分类号： B41M5/284 , C07D233/96 , C07D243/04 , C07D333/32 , C07F9/703 , C07F9/908 , C07F9/94 , Y02P20/582
摘要： Novel compounds that may be used as chemical vapor deposition precursors, thermochromic materials, conductive polymers, light-emitting diode precursors, and molecular charge-transfer salt precursors are provided. In addition, a novel compound that can be used to make the aforementioned compounds is provided. Still further, another aspect of the present invention is to provide methods for making and using the novel compounds provided.
摘要翻译：提供了可用作化学气相沉积前体，热变色材料，导电聚合物，发光二极管前体和分子电荷转移盐前体的新型化合物。此外，提供了可用于制备上述化合物的新型化合物。此外，本发明的另一方面是提供制备和使用所提供的新化合物的方法。

39. 发明申请

WO99062897A1 HIV INTEGRASE INHIBITORS 审中-公开
标题翻译：艾滋病毒整合抑制剂
公开(公告)号：WO99062897A1
公开(公告)日：1999-12-09
申请号：PCT/US1999/012094
申请日：1999-06-01
IPC分类号： A61K31/381 , A61K31/426 , A61K31/4433 , A61K31/4436 , A61K31/4535 , A61P31/18 , A61P37/04 , A61P43/00 , C07D277/20 , C07D277/34 , C07D277/36 , C07D277/38 , C07D277/42 , C07D333/24 , C07D333/28 , C07D333/32 , C07D333/34 , C07D333/36 , C07D333/56 , C07D333/60 , C07D333/74 , C07D409/12 , A61K31/38 , A61K31/425 , C07D277/04 , C07D277/18 , C07D333/22
CPC分类号： C07D409/12 , C07D277/42 , C07D333/24 , C07D333/32 , C07D333/34 , C07D333/36 , C07D333/60 , C07D333/74
摘要： Sulfur-containing heteroaryl dioxo-butyric acid derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
摘要翻译：含硫杂芳基二氧代丁酸衍生物被描述为HIV整合酶的抑制剂和HIV复制抑制剂。这些化合物可用于预防或治疗HIV的感染和治疗AIDS，无论是化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒药，免疫调节剂，抗生素或疫苗结合使用。还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。

40. 发明申请

WO99019321A1 SYNTHESIS OF 3-CARBOMETHOXY-4,5-DIMETHYLTHIOPHENE 审中-公开
标题翻译： 3-CARBOMETHOXY-4,5-二甲基苯乙烯的合成
公开(公告)号：WO99019321A1
公开(公告)日：1999-04-22
申请号：PCT/US1998/021526
申请日：1998-10-13
IPC分类号： C07D333/32 , C07D333/38 , C07D333/40 , C07D333/60
CPC分类号： C07D333/38 , C07D333/32 , C07D333/40
摘要： Fungicides having thiophene rings may be made from the intermediate compound 3-carbomethoxy-4,5-dimethylthiophene. That compound, and related compounds, may be produced by reacting an alpha mercaptoketone, e.g., 3-mercapto-2-butanone, with an acrylate, e.g., methyl-3-methoxy acrylate, in the presence of an alkoxide base, e.g., NaOMe, to form the substituted tetrahydrothiophene, followed by conversion to the aromatic thiophene with an acid treatment. The substituted tetrahydrothiophene is a novel compound.
摘要翻译：具有噻吩环的杀真菌剂可以由中间体化合物3-甲酯基-4,5-二甲基噻吩制备。该化合物和相关化合物可以通过使α-巯基酮（例如3-巯基-2-丁酮）与丙烯酸酯例如甲基-3-甲氧基丙烯酸酯在醇盐碱例如NaOMe ，形成取代的四氢噻吩，然后用酸处理转化成芳香族噻吩。取代的四氢噻吩是一种新型化合物。

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