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71. 发明授权

US06498273B2 Contrast media for angiography 失效
公开(公告)号：US06498273B2
公开(公告)日：2002-12-24
申请号：US09866243
申请日：2001-05-25
申请人： Don A. Gabriel , Laura J. Melton
发明人： Don A. Gabriel , Laura J. Melton
IPC分类号： C07C23305
CPC分类号： C07D295/185 , A61K49/0433 , C07C237/46 , C07C279/14 , C07C2601/14 , C07D207/12
摘要： The present invention provides basic ionic contrast agents that have anticoagulant activity. The contrast media incorporate a lysine or arginine group or derivative, and have a free amino or guanidino group. Methods of using the contrast media are also disclosed.

72. 发明授权

US06482985B1 2-benzyloxy-5-halo-acylanilide compounds and method of using them 失效
标题翻译： 2-苄氧基-5-卤代酰酰苯胺化合物及其使用方法
公开(公告)号：US06482985B1
公开(公告)日：2002-11-19
申请号：US10011550
申请日：2001-12-03
申请人： Chang-Kyu Kim
发明人： Chang-Kyu Kim
IPC分类号： C07C23305
CPC分类号： C07C233/25
摘要： Disclosed is a compound comprising a 2-benzyloxy-5-haloacylanilide having the structural formula I: wherein R is hydrogen or an alkyl group, RA is a substituent and n is 0-5; and X is a halogen. Also disclosed is a method for preparing a coupler using the compound. The compound and method simplify the preparation of photographic couplers.
摘要翻译：公开了包含具有结构式I的2-苄氧基-5-卤代酰基苯胺的化合物：其中R是氢或烷基，RA是取代基，n是0-5; 并且X是卤素。还公开了使用该化合物制备成色剂的方法。该化合物和方法简化了照相成色剂的制备。

73. 发明授权

US06479701B1 Method of preparing N,N′-disubstituted-3,3′-dithiodipropionamide and method of preparing substituted 3-isothiazolone by using the same 有权
标题翻译：制备N，N'-二取代-3,3'-二硫代二丙酰胺的方法及其制备取代的3-异噻唑酮的方法
公开(公告)号：US06479701B1
公开(公告)日：2002-11-12
申请号：US09937747
申请日：2001-09-28
申请人： Seung-Hwan Kim , Jeong-Ho Park , Jin-Man Kim , Soon-Jong Hahn , Ki-Seung Choi , Myung-Ho Cho
发明人： Seung-Hwan Kim , Jeong-Ho Park , Jin-Man Kim , Soon-Jong Hahn , Ki-Seung Choi , Myung-Ho Cho
IPC分类号： C07C23305
CPC分类号： C07D275/03 , C07C319/20 , C07C319/24 , C07C323/60
摘要： A method of preparing N,N-disubstituted-3,3′-dithiodipropionamide of formula (2) is provided. In the method, 3-mercaptopropionamide of formula (4) reacts with an aqueous solution of amine to prepare N-substituted-3-mercaptopropionamide of formula (3) and N-substituted-3-mercaptopropionamide reacts with an aqueous solution of hydrogen peroxide. In addition, a method of preparing substituted 3-isothiazolone is provided. In the method, the produced N,N-disubstituted-3,3′-dithiodipropionamide reacts with a halogenating agent, wherein X and Z are same or different and each selected from the group consisting of hydrogen or a lower alkyl group; Y is selected from the group consisting of hydrogen, an alkyl group of 1 to 18 carbon atoms, a cycloalkyl group of up to 10 carbon atoms, an aralkyl group of up to 10 carbon atoms, an aryl group of up to 10 carbon atoms, a halogen-, lower alkyl- or lower alkoxy-substituted aryl group, a cyano alkyl group, a carboalkoxyalkyl group, a haloalkyl group, an alkoxyalkyl group, an aryloxyalkyl group of up to 12 carbon atoms, an aralkoxyalkyl group of up to 12 carbon atoms, a dialkylaminoalkyl group, an alkylacyl group of up to 8 carbon atoms, a lower alkylsulfonyl group, an arylsulfonyl group of up to 10 carbon atoms, a cyano group and a carbamoyl group.
摘要翻译：提供制备式（2）的N，N-二取代-3,3'-二硫代二丙酰胺的方法。在该方法中，式（4）的3-巯基丙酰胺与胺水溶液反应制备式（3）的N-取代-3-巯基丙酰胺，N-取代-3-巯基丙酰胺与过氧化氢水溶液反应。此外，提供了制备取代的3-异噻唑酮的方法。在该方法中，所制备的N，N-二取代-3,3'-二硫代二丙酰胺与卤化剂反应，其中X和Z相同或不同，各自选自氢或低级烷基; Y选自氢，1至18个碳原子的烷基，至多10个碳原子的环烷基，至多10个碳原子的芳烷基，至多10个碳原子的芳基，卤素，低级烷基或低级烷氧基取代的芳基，氰基烷基，碳烷氧基烷基，卤代烷基，烷氧基烷基，至多12个碳原子的芳氧基烷基，至多12个碳原子的芳烷氧基烷基原子，二烷基氨基烷基，至多8个碳原子的烷基酰基，低级烷基磺酰基，至多10个碳原子的芳基磺酰基，氰基和氨基甲酰基。

74. 发明授权

US06472562B1 N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them 有权
标题翻译： N-胍基烷基酰胺，它们的制备方法，它们的用途以及包含它们的药物制剂
公开(公告)号：US06472562B1
公开(公告)日：2002-10-29
申请号：US09697188
申请日：2000-10-27
申请人： Otmar Klingler , Gerhard Zoller , Elisabeth Defossa , Fahad A. Al-Obeidi , Armin Walser , James Ostrem
发明人： Otmar Klingler , Gerhard Zoller , Elisabeth Defossa , Fahad A. Al-Obeidi , Armin Walser , James Ostrem
IPC分类号： C07C23305
CPC分类号： C07D213/30 , C07C279/14 , C07D213/40 , C07D215/48 , C07D239/28
摘要： The present invention relates to compounds of the formula I, in which A, L, Y, and k have the meanings indicated in the specification and claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa and/or factor VIIa and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of conditions in which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
摘要翻译：本发明涉及式I化合物，其中A，L，Y和k具有说明书和权利要求书中所示的含义。式I的化合物是有价值的药理活性化合物。它们具有强烈的抗血栓形成作用，并且适用于例如治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。它们是血液凝固酶因子Xa和/或因子VIIa的可逆抑制剂，并且通常可用于存在因子Xa和/或因子VIIa的不需要的活性或用于治愈或预防其中旨在抑制因子Xa和/或因子VIIa。本发明还涉及制备式I化合物，其用途，特别是药物中的活性成分以及包含它们的药物制剂的方法。

75. 发明授权

US06444849B1 Amide derivatives 失效
标题翻译：酰胺衍生物
公开(公告)号：US06444849B1
公开(公告)日：2002-09-03
申请号：US09469354
申请日：1999-12-22
申请人： Ryoichi Ando , Makoto Kawamura , Noriko Chiba , Kazutoshi Watanabe
发明人： Ryoichi Ando , Makoto Kawamura , Noriko Chiba , Kazutoshi Watanabe
IPC分类号： C07C23305
CPC分类号： C07D307/79 , C07C237/42 , C07C2601/08 , C07C2601/14 , C07D209/18 , C07D317/60 , C07D333/60
摘要： A compound represented by the following general formula (1); wherein X represents R1(R2)(R3)C— where R1 represents a C3-C8 cycloalkyl group, an optionally substituted C6-C14 aryl group, an optionally substituted heterocyclic residue, an optionally substituted C6-C14 aryloxy group, or an optionally substituted C7-C15 arylmethyl group; R2 and R3 independently represent hydrogen atom or a C1-C5 alkyl group, or R2 and R3 may combine to represent a C2-C7 alkylene group; or X represents R7—A— wherein R7 represents (i) a C1-C10 alkyl group which may optionally be substituted with an optionally substituted C6-C14 aryl group, an optionally substituted fluorenyl group or an optionally substituted heterocyclic group, (ii) an optionally substituted C6-C14 aryl group or (iii) an optionally substituted heterocyclic group, and A represents an oxygen atom or —N—R8 where R8 represents hydrogen atom or a C1-C5 alkyl group, Y represents an oxygen atom or a sulfur atom, R4 and R5 independently represent hydrogen atom or a C1-C5 alkyl group; and R6 represents hydrogen atom, a C1-C5 alkyl group which may optionally be substituted with a hydroxyl group, a hydroxyl group or a C1-C5 alkoxy group, provided that the compounds wherein R7 is a benzyl group, A and Y are an oxygen atom, R4 and R5 are hydrogen atom, and R6 is a propyl group are excluded, or a salt thereof, or a solvate thereof or a hydrate thereof.
摘要翻译：由以下通式（1）表示的化合物：其中X表示R 1（R 2）（R 3）C-，其中R 1表示C 3 -C 8环烷基，任选取代的C 6 -C 14芳基，任选取代的杂环残基，任选取代的C 6 -C 14芳氧基，或任选取代的C 7 -C 15芳基甲基; R2和R3独立地表示氢原子或C1-C5烷基，或R2和R3可以组合以表示C2-C7亚烷基; 或X表示R7-A，其中R7表示（i）可任选被任选取代的C 6 -C 14芳基取代的C 1 -C 10烷基，任选取代的芴基或任选取代的杂环基，（ii）任选地取代的C 6 -C 14芳基或（iii）任选取代的杂环基，A表示氧原子或-N-R 8，其中R 8表示氢原子或C 1 -C 5烷基，Y表示氧原子或硫原子， R4和R5独立地表示氢原子或C1-C5烷基; 并且R 6表示氢原子，可任选被羟基，羟基或C 1 -C 5烷氧基取代的C 1 -C 5烷基，条件是其中R 7为苄基，A和Y为氧的化合物为氧原子，R 4和R 5为氢原子，并且R 6为丙基，或其盐，或其溶剂合物或其水合物。

76. 发明授权

US06348627B1 Aryl and heteroarylcyclopropyl oxime ethers and their use as fungicides 失效
标题翻译：芳基和杂芳基环丙基肟醚及其作为杀真菌剂的用途
公开(公告)号：US06348627B1
公开(公告)日：2002-02-19
申请号：US09572487
申请日：2000-05-15
申请人： Ronald Ross, Jr. , Duyan Vuong Nguyen , Edward Michael Szapacs , Frisby Davis Smith , Steven Howard Shaber
发明人： Ronald Ross, Jr. , Duyan Vuong Nguyen , Edward Michael Szapacs , Frisby Davis Smith , Steven Howard Shaber
IPC分类号： C07C23305
CPC分类号： C07D213/53 , A01N37/36 , A01N37/50 , A01N43/08 , A01N43/10 , A01N43/36 , A01N43/40 , A01N43/42 , A01N43/50 , A01N43/54 , A01N43/56 , A01N43/58 , A01N43/60 , A01N43/76 , A01N43/78 , A01N43/80 , A01N53/00 , C07C251/60 , C07C2601/02 , C07C2602/02 , C07D213/62 , C07D215/12 , C07D231/12 , C07D233/64 , C07D237/08 , C07D239/26 , C07D239/34 , C07D241/12 , C07D261/08 , C07D263/32 , C07D275/02 , C07D277/28 , C07D307/52 , C07D307/56 , C07D333/22
摘要： Compounds with fungicidal and insecticidal properties having formula wherein X is N or CH; Z is O, S or NR8; A is hydrogen, halo, cyano, (C1-C12)alkyl, or (C1-C12)alkoxy; R1 and R8 are independently hydrogen or (C1-C4)alkyl; R2 is hydrogen, (C1-C12)alkyl, halo(C1-C12)alkyl, (C3-C7)cycloalkyl, halo(C3-C7)cycloalkyl, (C2-C8)alkenyl, halo(C2-C8)alkenyl, (C2-C8)alkynyl, halo(C2-C8)alkynyl, aryl, aralkyl, heterocyclic, heterocyclic(C1-C4)alkyl or C(R10)═N—OR9; R3 is hydrogen, (C1-C12)alkyl, halo(C1-C12)alkyl, (C3-C7)cycloalkyl, halo(C3-C7)cycloalkyl, (C2-C8)alkenyl, halo(C2-C8)alkenyl, (C2-C8)alkynyl, halo(C2-C8)alkynyl, aryl, aralkyl, aryl(C3-C7)cycloalkyl, heterocyclic or heterocyclic(C1-C4)alkyl; R4 and R5 are independently hydrogen, (C1-C12)alkyl, halo(C1-C12)alkyl, (C3-C7)cycloalkyl, halo(C3-C7)cycloalkyl, (C2-C8)alkenyl, halo(C2-C8)alkenyl, (C2-C8)alkynyl, halo(C2-C8)alkynyl, halo, cyano, (C1-C4)alkoxycarbonyl, aryl, aralkyl, aryl(C3-C7)cycloalkyl, heterocyclic or heterocyclic(C1-C4)alkyl; R6 is hydrogen, (C1-C12)alkyl, halo(C1-C12)alkyl, (C3-C7)cycloalkyl, halo(C3-C7)cycloalkyl, (C2-C8)alkenyl, halo(C2-C8)alkenyl, (C2-C8)alkynyl, halo(C2-C8)alkynyl, halo, cyano, (C1-C4)alkoxycarbonyl, aryl, aralkyl, aryl(C3-C7)cycloalkyl, heterocyclic or heterocyclic(C1-C4)alkyl; R7 is aryl, aralkyl, heterocyclic or heterocyclic(C1-C4)alkyl; R9 is hydrogen, (C1-C12)alkyl, halo(C1-C12)alkyl, (C2-C8)alkenyl, halo(C2-C8)alkenyl, (C2-C8)alkynyl, halo(C2-C8)alkynyl, (C1-C4)alkylcarbonyl, (C1-C4)alkoxycarbonyl, aryl, or aralkyl; and R10 is hydrogen, (C1-C12)alkyl, halo(C1-C12)alkyl, (C3-C7)cycloalkyl, halo(C3-C7)cycloalkyl, (C2-C8)alkenyl, halo(C2-C8)alkenyl, (C2-C8)alkynyl, halo(C2-C8)alkynyl, aryl, aralkyl, heterocyclic, or heterocyclic(C1-C4)alkyl.
摘要翻译：具有杀虫和杀虫性质的化合物，其具有式（X）的化合物是N或CH; Z是O，S或NR8; A是氢，卤素，氰基，（C 1 -C 12）烷基或（C 1 -C 12）烷氧基; R1和R8独立地是氢或（C1-C4）烷基; （C 1 -C 12）烷基，（C 3 -C 7）环烷基，卤代（C 3 -C 7）环烷基，（C 2 -C 8）烯基，卤代（C 2 -C 8） C 2 -C 8炔基，卤代（C 2 -C 8）炔基，芳基，芳烷基，杂环，杂环（C 1 -C 4）烷基或C（R 10）= N-OR 9; （C 1 -C 12）烷基，（C 3 -C 7）环烷基，卤代（C 3 -C 7）环烷基，（C 2 -C 8）烯基，卤代（C 2 -C 8） C 2 -C 8）炔基，卤代（C 2 -C 8）炔基，芳基，芳烷基，芳基（C 3 -C 7）环烷基，杂环或杂环（C 1 -C 4）（C 1 -C 12）烷基，（C 3 -C 7）环烷基，卤代（C 3 -C 7）环烷基，（C 2 -C 8）烯基，卤代（C 2 -C 8）烯基，（C 2 -C 8）炔基，卤代（C 2 -C 8）炔基，卤素，氰基，（C 1 -C 6）

77. 发明授权

US06337422B1 Yellow polymorph of 5-amino-2,4,6-triiodo-n,n′-bis(2-3-dihydroxypropy)-isophthalamide 有权
标题翻译： 5-氨基-2,4,6-三碘-n，N'-双（2,3-二羟基脯氨酸） - 间苯二甲酰胺的黄色多晶型物
公开(公告)号：US06337422B1
公开(公告)日：2002-01-08
申请号：US09438385
申请日：1999-11-12
申请人： Dick Malthe-Sorenssen , Audun Aukrust
发明人： Dick Malthe-Sorenssen , Audun Aukrust
IPC分类号： C07C23305
CPC分类号： A61K49/0447 , A61K49/0438 , C07C237/46
摘要： The yellow polymorph of 5-amino-2,4,6-triiodo-N,N′-bis(2,3-dihydroxypropyl)-isophthalamide is described.
摘要翻译：描述了5-氨基-2,4,6-三碘-N，N'-双（2,3-二羟丙基） - 间苯二甲酰胺的黄色多晶型物。

78. 发明授权

US06320078B1 Method of producing benzamide derivatives 有权
标题翻译：苯甲酰胺衍生物的制备方法
公开(公告)号：US06320078B1
公开(公告)日：2001-11-20
申请号：US09359368
申请日：1999-07-23
申请人： Tsuneji Suzuki , Tomoyuki Ando , Katsutoshi Tsuchiya , Hiroki Ishibashi
发明人： Tsuneji Suzuki , Tomoyuki Ando , Katsutoshi Tsuchiya , Hiroki Ishibashi
IPC分类号： C07C23305
CPC分类号： C07D213/30 , C07C231/02 , C07D213/65 , C07D213/75 , C07D231/12 , C07D233/56 , C07D249/08 , C07C233/80
摘要： In the case that a selectively monoacylated phenylenediamine derivative which is useful as any of medicines, agricultural chemicals, animal drugs and the intermediates of chemicals is prepared by reacting a benzoic acid derivative with a phenylenediamine derivative, the benzoic acid derivative is converted into a benzoyl imidazole derivative and this benzoyl imidazole derivative is then reaction with the phenylenediamine derivative, whereby the improvement of a preparation efficiency and the high selectivity of the monoacylation can be achieved, the steps of protection and deprotection being omitted.
摘要翻译：在苯甲酸衍生物与苯二胺衍生物反应制备可用作药物，农药，动物药物和化学药品中间体的选择性单酰化苯二胺衍生物的情况下，将苯甲酸衍生物转化成苯甲酰咪唑衍生物，然后将苯甲酰咪唑衍生物与苯二胺衍生物反应，从而可以实现制备效率的提高和单酰化的高选择性，省略了保护和脱保护的步骤。

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