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71. 发明授权

US06335334B1 Sulfur substituted sulfonylaminocarboxylic acid N-arylamides, their preparation, their use and pharmaceutical preparations comprising them 有权
标题翻译：硫取代磺酰氨基羧酸N-芳基酰胺，其制备方法及其应用和包含它们的药物制剂
公开(公告)号：US06335334B1
公开(公告)日：2002-01-01
申请号：US09349933
申请日：1999-07-08
申请人： Ursula Schindler , Karl Schönafinger , Hartmut Strobel
发明人： Ursula Schindler , Karl Schönafinger , Hartmut Strobel
IPC分类号： A61K315375
CPC分类号： C07C311/21 , C07C311/46 , C07C311/51 , C07C311/58 , C07C317/40 , C07C323/42 , C07C323/52 , C07C323/60 , C07C331/12 , C07C2601/02 , C07C2601/14 , C07C2602/04 , C07C2602/08 , C07D207/12 , C07D207/16 , C07D207/20 , C07D207/48 , C07D209/10 , C07D209/14 , C07D211/46 , C07D211/54 , C07D211/62 , C07D211/96 , C07D213/71 , C07D213/78 , C07D213/80 , C07D213/82 , C07D215/36 , C07D221/20 , C07D231/18 , C07D231/38 , C07D231/42 , C07D233/84 , C07D235/18 , C07D239/06 , C07D239/26 , C07D239/42 , C07D243/08 , C07D261/10 , C07D261/16 , C07D265/30 , C07D277/04 , C07D277/36 , C07D277/46 , C07D277/52 , C07D277/54 , C07D277/64 , C07D279/12 , C07D295/26 , C07D333/34 , C07D333/38 , C07D333/40 , C07D401/12 , C07D413/12 , C07D491/10
摘要： The present invention relates to compounds of the formula I wherein A1, A2, R1, R2, R3, X and n are as defined in the claims, which are valuable pharmaceutically active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of the formula I.
摘要翻译：本发明涉及式I化合物，其中A1，A2，R1，R2，R3，X和n如权利要求中所定义，它们是用于治疗和预防疾病的有价值的药物活性化合物，例如心血管疾病如高血压，心绞痛，心功能不全，血栓形成或动脉粥样硬化。式I的化合物能够调节身体的环鸟苷酸（cGMP）的产生，并且通常适用于治疗和预防与扰乱的cGMP平衡相关的疾病。本发明还涉及制备式I化合物的方法，其用于治疗和预防上述疾病和用于制备用于此目的的药物以及包含式I化合物的药物制剂。

72. 发明授权

US5693865A Fluoroalkenyl compounds and their use as pest repellents 失效
标题翻译：氟烯基化合物及其作为驱虫剂的用途
公开(公告)号：US5693865A
公开(公告)日：1997-12-02
申请号：US763802
申请日：1996-12-11
申请人： Peter Gerrard Ruminski
发明人： Peter Gerrard Ruminski
IPC分类号： A01N33/04 , A01N33/06 , A01N33/12 , A01N33/18 , A01N33/26 , A01N35/10 , A01N37/06 , A01N37/12 , A01N37/18 , A01N37/20 , A01N37/22 , A01N37/26 , A01N37/28 , A01N37/30 , A01N37/38 , A01N37/40 , A01N37/44 , A01N37/46 , A01N37/52 , A01N41/06 , A01N41/12 , A01N43/10 , A01N43/28 , A01N43/36 , A01N43/56 , A01N43/90 , A01N47/12 , A01N47/28 , A01N47/34 , A01N47/40 , A01N47/44 , A01P5/00 , A01P7/00 , C07C57/52 , C07C57/76 , C07C69/65 , C07C203/04 , C07C205/03 , C07C205/09 , C07C205/43 , C07C209/62 , C07C209/64 , C07C211/24 , C07C211/45 , C07C211/48 , C07C211/63 , C07C219/08 , C07C229/12 , C07C229/24 , C07C229/56 , C07C229/60 , C07C233/09 , C07C233/12 , C07C233/13 , C07C233/38 , C07C233/49 , C07C233/55 , C07C237/06 , C07C237/20 , C07C237/22 , C07C237/24 , C07C239/10 , C07C243/10 , C07C243/16 , C07C243/30 , C07C243/34 , C07C243/38 , C07C251/12 , C07C251/24 , C07C259/06 , C07C265/06 , C07C271/20 , C07C271/22 , C07C275/20 , C07C275/64 , C07C279/06 , C07C309/66 , C07C309/73 , C07C311/16 , C07C311/58 , C07C323/60 , C07C327/22 , C07C327/30 , C07C327/32 , C07D207/16 , C07D231/20 , C07D295/185 , C07D317/24 , C07D333/38 , C07D487/18 , C07C211/03
CPC分类号： C07D295/185 , A01N33/04 , A01N33/06 , A01N33/18 , A01N33/26 , A01N35/10 , A01N37/06 , A01N37/12 , A01N37/18 , A01N37/20 , A01N37/22 , A01N37/26 , A01N37/28 , A01N37/30 , A01N37/38 , A01N37/40 , A01N37/44 , A01N37/46 , A01N37/52 , A01N41/06 , A01N41/12 , A01N43/10 , A01N43/28 , A01N43/36 , A01N43/56 , A01N43/90 , A01N47/12 , A01N47/28 , A01N47/34 , A01N47/40 , A01N47/44 , C07C203/04 , C07C205/03 , C07C205/09 , C07C205/43 , C07C211/24 , C07C211/48 , C07C211/63 , C07C219/08 , C07C229/12 , C07C229/24 , C07C229/56 , C07C229/60 , C07C233/09 , C07C233/13 , C07C233/38 , C07C233/49 , C07C233/55 , C07C237/06 , C07C237/20 , C07C237/22 , C07C237/24 , C07C239/10 , C07C243/10 , C07C243/16 , C07C243/30 , C07C243/34 , C07C243/38 , C07C251/24 , C07C259/06 , C07C265/06 , C07C271/20 , C07C271/22 , C07C275/20 , C07C275/64 , C07C279/06 , C07C309/66 , C07C309/73 , C07C311/16 , C07C311/58 , C07C323/60 , C07C327/22 , C07C327/30 , C07C327/32 , C07C57/52 , C07C57/76 , C07D207/16 , C07D231/20 , C07D317/24 , C07D333/38 , C07C2101/02
摘要： Fluorinated alkene compounds useful for and methods of controlling nematodes, insects, and acarids that prey on agricultural crops. Polar compounds, for example, 3,4,4-trifluoro-3-butene-1-amine or 3,4,4-trifluoro-3-butenoic acid, are particularly useful for systemic control of pests. Novel method and intermediates for the preparation of 3,4,4-trifluoro-3-butene-1-amine are also provided.
摘要翻译：氟化烯烃化合物可用于控制在农作物上捕获的线虫，昆虫和螨虫的方法。极性化合物，例如3,4,4-三氟-3-丁烯-1-胺或3,4,4-三氟-3-丁烯酸，特别适用于系统性控制害虫。还提供了用于制备3,4,4-三氟-3-丁烯-1-胺的新方法和中间体。

73. 发明授权

US5607976A Substituted benzenesulfonyl-thioureas and pharmaceutical preparations containing them 失效
标题翻译：取代苯磺酰硫脲和含有它们的药物制剂
公开(公告)号：US5607976A
公开(公告)日：1997-03-04
申请号：US598319
申请日：1996-02-08
申请人： Heinrich Englert , Uwe Gerlach , Peter Crause , Dieter Mania , Heinz G ogelein , Joachim Kaiser
发明人： Heinrich Englert , Uwe Gerlach , Peter Crause , Dieter Mania , Heinz G ogelein , Joachim Kaiser
IPC分类号： C07D333/20 , A61K31/18 , A61K31/34 , A61K31/35 , A61K31/38 , A61K31/381 , A61K31/395 , A61K31/40 , A61K31/425 , A61K31/426 , A61K31/64 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/10 , C07C233/00 , C07C303/40 , C07C311/58 , C07C327/40 , C07C335/42 , C07D207/32 , C07D207/335 , C07D213/40 , C07D277/28 , C07D307/52
CPC分类号： C07C335/42 , C07C311/58
摘要： Substituted benzenesulfonylureas and -thioureas, processes for their preparation, their use for the production of pharmaceutical preparations, and pharmaceutical preparations containing them.Substituted benzenesulfonylureas and -thioureas of the formula I ##STR1## exhibit effects on the cardiovascular system.
摘要翻译：取代的苯磺酰脲和硫脲，其制备方法，其用于制备药物制剂的用途，以及含有它们的药物制剂。式I的取代苯磺酰脲和硫脲显示出对心血管系统的作用。

74. 发明授权

US5378729A Amino acid derivative anticonvulsant 失效
标题翻译：氨基酸衍生物抗惊厥药
公开(公告)号：US5378729A
公开(公告)日：1995-01-03
申请号：US710610
申请日：1991-06-04
申请人： Harold L. Kohn , Darrell Watson
发明人： Harold L. Kohn , Darrell Watson
IPC分类号： A61K31/16 , A61K31/165 , A61K31/195 , A61K31/215 , A61K31/34 , A61K31/341 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/4015 , A61K31/403 , A61K31/404 , A61K31/405 , A61K31/41 , A61K31/415 , A61K31/4172 , A61K31/4196 , A61K31/42 , A61K31/421 , A61K31/4245 , A61K31/425 , A61K31/426 , A61K31/4402 , A61K31/4412 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/505 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K31/69 , A61K38/00 , A61K38/04 , A61P25/00 , A61P25/08 , A61P25/20 , C07C229/30 , C07C233/47 , C07C237/00 , C07C237/22 , C07C237/40 , C07C239/16 , C07C239/18 , C07C239/20 , C07C243/22 , C07C243/42 , C07C259/06 , C07C271/22 , C07C271/52 , C07C271/54 , C07C275/14 , C07C275/16 , C07C275/28 , C07C275/40 , C07C281/02 , C07C309/18 , C07C311/55 , C07C311/58 , C07C317/28 , C07C317/48 , C07C317/50 , C07C323/41 , C07C323/59 , C07C323/60 , C07C327/42 , C07C335/06 , C07C335/08 , C07C335/16 , C07C335/20 , C07D207/32 , C07D207/337 , C07D207/34 , C07D207/40 , C07D207/404 , C07D209/20 , C07D209/40 , C07D209/42 , C07D213/56 , C07D213/64 , C07D231/12 , C07D231/38 , C07D233/54 , C07D233/61 , C07D233/64 , C07D233/84 , C07D235/16 , C07D237/08 , C07D239/26 , C07D241/12 , C07D249/08 , C07D257/04 , C07D261/08 , C07D263/32 , C07D265/02 , C07D271/06 , C07D277/20 , C07D277/44 , C07D295/14 , C07D295/15 , C07D303/46 , C07D307/16 , C07D307/54 , C07D307/68 , C07D307/81 , C07D307/85 , C07D333/10 , C07D333/24 , C07D333/36 , C07D333/38 , C07D333/52 , C07D333/60 , C07D333/66 , C07D333/70 , C07D405/12 , C07D521/00 , A61K31/445 , C07D211/72 , C07D261/04
CPC分类号： C07D207/337 , A61K31/165 , A61K31/195 , A61K31/34 , A61K31/38 , A61K31/40 , C07C229/30 , C07C233/47 , C07C237/00 , C07C237/22 , C07C239/18 , C07C239/20 , C07C243/22 , C07C259/06 , C07C271/22 , C07C271/54 , C07C275/16 , C07C275/28 , C07C281/02 , C07C309/18 , C07C311/55 , C07C311/58 , C07C317/50 , C07C323/60 , C07C327/42 , C07C335/16 , C07D207/34 , C07D207/404 , C07D209/20 , C07D209/42 , C07D213/56 , C07D231/12 , C07D233/56 , C07D233/64 , C07D233/84 , C07D235/16 , C07D249/08 , C07D257/04 , C07D271/06 , C07D295/15 , C07D303/46 , C07D307/16 , C07D307/54 , C07D307/68 , C07D307/81 , C07D307/85 , C07D333/24 , C07D333/38 , C07D333/60 , C07D333/70 , C07D405/12
摘要： The present invention relates to compounds exhibiting central nervous system (CNS) activity which are useful in the treatment of epilepsy and other CNS disorders. The compounds of this invention have the following general formula: ##STR1## and pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及可用于治疗癫痫和其它CNS疾病的中枢神经系统（CNS）活性的化合物。本发明的化合物具有以下通式：其中药学上可接受的盐。

75. 发明授权

US5292711A Thermosensitive recording material 失效
标题翻译：热敏记录材料
公开(公告)号：US5292711A
公开(公告)日：1994-03-08
申请号：US878389
申请日：1992-05-05
申请人： Masaki Nishimura , Kunitaka Toyofuku , Yoshiyuki Takahashi
发明人： Masaki Nishimura , Kunitaka Toyofuku , Yoshiyuki Takahashi
IPC分类号： B41M5/333 , B41M5/337 , C07C311/58 , C07C311/60 , B41M5/32
CPC分类号： C07C311/60 , B41M5/3333 , B41M5/3375 , C07C311/58
摘要： A thermosensitive recording material, capable of providing colored images having a high resistance to oily substances and plasticizers and an excellent storage persistency for a long time, comprises a thermosensitive colored image-forming layer formed on a sheet substrate and comprising a colorless dye precursor, a color developing agent, a colored image-stabilizing agent comprising an aziridinyl compound and/or an epoxy compound, and an additional colored image-stabilizing agent comprising a primary or secondary amine compound and/or a carboxylic compound having a carboxyl group or --CO--O--CO-- group; the color developing agent preferably comprising a compound of the formula (I): ##STR1## wherein X is an O or S atom, R.sub.1 is an unsubstituted aromatic group, or a substituted phenyl group having a lower alkyl or a halogen atom, and R.sub.2 and R.sub.3 are respectively a hydrogen atom, or alkyl group, aryl groups, substituted alkyl group with an aryloxy group, or a substituted aromatic group having an alkyl, aryl, aralkyl, alkyloxy, alkyloxycarbonyl, aryloxycarbonyl, aralkyloxycarbonyl or arylsulfonyl group or a halogen atom.
摘要翻译：能够提供对油性物质和增塑剂具有高耐性的彩色图像和长时间优异的储存持久性的热敏记录材料包括形成在片状基材上并包含无色染料前体的热敏着色图像形成层，彩色显影剂，包含吖丙啶基化合物和/或环氧化合物的着色图像稳定剂和另外的着色图像稳定剂，其包含伯或仲胺化合物和/或具有羧基或-CO- O-CO-基团; 显色剂优选包含式（I）化合物：（*化学结构*）其中X为O或S原子，R 1为未取代的芳族基团或具有低级烷基或卤素原子的取代苯基，R2和R3分别为氢原子或烷基，芳基，具有芳氧基的取代烷基或具有烷基，芳基，芳烷基，烷氧基，烷氧基羰基，芳氧基羰基，芳烷氧基羰基或芳基磺酰基的取代芳基，或卤素原子。

76. 发明授权

US5272175A Substituted tyrosyl diamide compounds 失效
标题翻译：取代的酪氨酰二酰胺化合物
公开(公告)号：US5272175A
公开(公告)日：1993-12-21
申请号：US886276
申请日：1992-05-20
申请人： Donald W. Hansen, Jr. , Nizal S. Chandrakumar , Karen B. Peterson , Sofya Tsymbalov , Robert K. Husa
发明人： Donald W. Hansen, Jr. , Nizal S. Chandrakumar , Karen B. Peterson , Sofya Tsymbalov , Robert K. Husa
IPC分类号： C07C233/47 , C07C237/20 , C07C237/22 , C07C271/20 , C07C271/22 , C07C275/16 , C07C311/58 , C07D207/14 , C07D295/185 , A61K31/165 , A61K31/17 , A61K31/325 , C07C237/28
CPC分类号： C07D295/185 , C07C233/47 , C07C237/20 , C07C237/22 , C07C271/20 , C07C271/22 , C07C275/16 , C07C311/58 , C07D207/14
摘要： The present invention provides substituted tyrosyl diamide compounds of general Formula I: ##STR1## and the pharmaceutically-acceptable salts thereof, which are useful for inducing analgesia in animals, pharmaceutical compositions comprising a pharmaceutically-acceptable carrier and a compound of Formula I, and a method for inducing analgesia in an animal in need thereof comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
摘要翻译：本发明提供通式I的取代的酪氨酰二酰胺化合物：式I及其药学上可接受的盐，其可用于诱导动物镇痛，药物组合物包含药学上可接受的载体和式I化合物，以及用于在有需要的动物中诱导镇痛的方法，包括向动物施用治疗有效量的式I化合物。

77. 发明授权

US4365990A Sulfonylurea herbicidal antidotes 失效
标题翻译：磺酰脲除草剂
公开(公告)号：US4365990A
公开(公告)日：1982-12-28
申请号：US163755
申请日：1980-06-27
申请人： Edmund J. Gaughan
发明人： Edmund J. Gaughan
IPC分类号： A01N25/32 , A01N47/34
CPC分类号： A01N25/32 , A01N47/34 , C07C311/55 , C07C311/58 , C07C311/60
摘要： Sulfonylurea compounds have the formula ##STR1## in which R is selected from the group consisting of 1-4 carbon alkyl, phenyl, and methyl substituted phenyl;R.sub.1 is selected from the group consisting of hydrogen and 1-4 carbon alkyl; andR.sub.2 is selected from the group consisting of mono- and polyhalosubstituted phenyl, 3-6 carbon alkynyl, and 2-6 carbon alkoxyalkyl.
摘要翻译：磺酰脲化合物具有式“IMAGE”，其中R选自1-4个碳原子的烷基，苯基和甲基取代的苯基; R1选自氢和1-4个碳原子的烷基; 并且R 2选自单取代和多取代的苯基，3-6碳炔基和2-6碳烷氧基烷基。

78. 发明授权

US4013706A Derivatives of substituted urea, acyl ureas, and sulphonyl ureas, and a process for producing the same 失效
标题翻译：替代尿酸，尿酸和硫磺尿的衍生物及其生产方法
公开(公告)号：US4013706A
公开(公告)日：1977-03-22
申请号：US523550
申请日：1974-11-13
申请人： Jesus Anatol , Jean Berecoechea
发明人： Jesus Anatol , Jean Berecoechea
IPC分类号： C07C275/50 , C07C67/00 , C07C239/00 , C07C273/00 , C07C275/52 , C07C275/54 , C07C275/60 , C07C301/00 , C07C303/36 , C07C311/13 , C07C311/55 , C07C311/58 , C07C313/00 , C07C323/44 , C07C125/06
CPC分类号： C07C311/55 , C07C275/60 , C07C311/13 , C07C311/58
摘要： A process for the production of compounds of the general formula: ##STR1## and compounds of that general formula, in which A represents hydrogen or an R.sub.1 -- X group (in which X represents --CO or --SO.sub.2 and R.sub.1 represents an optionally substituted alkyl, cycloalkyl, aralkyl, alkoxy, aryl, aryloxy, etheroxy, aliphatic or aromatic group), R.sub.2 represents a hydrogen atom or an optionally substituted alkyl, cycloalkyl, aralkyl, or aryl group, and R.sub.3 represents a hydrogen atom or an alkyl group derived from a secondary or tertiary alcohol, particularly a tertio-butyl group, with the restriction that, when R.sub.2 represents hydrogen, R.sub.3 represents the said alkyl group and that, when R.sub.3 represents hydrogen, R.sub.2 represents the said optionally substituted alkyl, cycloalkyl, aralkyl, or aryl group, the said process comprising reacting a cyanamide of the formula: ##STR2## (in which A and R.sub.2 have the meanings given above) with a compound e.g. a tertiary or secondary alcohol adapted to form readily a carbo cation (R.sub.3 .sup.+) in the presence of a catalyst e.g. sulphuric acid or a Lewis acid.

79. 发明授权

US3998968A Benzenesulfonyl ureas and process for their manufacture 失效
标题翻译：苯磺酰脲及其制备方法
公开(公告)号：US3998968A
公开(公告)日：1976-12-21
申请号：US559712
申请日：1975-03-19
申请人： Volker Hitzel , Werner Pfaff , Rudi Weyer , Helmut Weber
发明人： Volker Hitzel , Werner Pfaff , Rudi Weyer , Helmut Weber
IPC分类号： C07C311/58 , A61K20060101 , A61K31/00 , A61K31/17 , A61K31/18 , A61K31/64 , C07C20060101 , C07C67/00 , C07C301/00 , C07C303/36 , C07C303/38 , C07C303/40 , C07C127/00
CPC分类号： C07C311/58 , Y10S514/866
摘要： N-acylaminoalkyl-benzenesulfonyl-N'-methyl ureas, especially those of the general formula ##STR1## in which R is C.sub.1-- C.sub.4 --alkyl or a phenyl radical substituted in 2-position by alkoxy of 1 to 4 carbon atoms, phenoxy or dimethylamino and in 5-position by H, CH.sub.3, Cl or Br, their manufacture and their use as oral antidiabetics.
摘要翻译： N-酰基氨基烷基 - 苯磺酰基-N'-甲基脲，特别是其中R为C 1 -C 4 - 烷基或2-位被1-4个碳原子的烷氧基取代的苯基的通式为“IMAGE”的那些，苯氧基或二甲基氨基，在H，CH3，Cl或Br的5-位，它们的制备及其作为口服抗糖尿病药的用途。

80. 发明授权

US3984416A Substituted quinoline-8-carboxamido ethyl benzene-sulfonyl N-cyclopentylmethyl urea 失效
标题翻译：取代的喹啉-8-甲酰氨基乙基苯磺酰基N-环戊基甲基脲
公开(公告)号：US3984416A
公开(公告)日：1976-10-05
申请号：US581764
申请日：1975-05-29
申请人： Helmut Weber , Walter Aumuller , Rudi Weyer , Karl Muth , Volker Hitzel
发明人： Helmut Weber , Walter Aumuller , Rudi Weyer , Karl Muth , Volker Hitzel
IPC分类号： C07D215/16 , C07D215/18
CPC分类号： C07D215/16 , C07C311/58 , C07C2101/08 , C07C2102/08 , C07C2102/10
摘要： Sulfonyl-ureas of the formula X--CO--NH--A--SO.sub.2 --NH--CO--NH--R.sup.1, in which R.sup.1 represents cyclopentylmethyl, alkyl-cyclopentylmethyl or dialkyl-cyclopentylmethyl, having up to 2 carbon atoms in the alkyl rest, or cyclopentylethyl, X represents a. ##SPC1##In which R.sup.2 represents hydrogen, F, Cl, Br, CF.sub.3, CH.sub.3 or OCH.sub.3,b. ##SPC2##In which R.sup.3 represents hydrogen, Cl or CH.sub.3,c. ##SPC3##In which R.sup.4 represents hydrogen, Cl or Br,A represents one of the groupings ##SPC4##And their physiologically tolerated salts, process for preparing them and pharmaceutical preparations containing them.
摘要翻译：式X-CO-NH-A-SO2-NH-CO-NH-R1的磺酰脲，其中R1表示烷基休止中具有至多2个碳原子的环戊基甲基，烷基 - 环戊基甲基或二烷基 - 环戊基甲基，或环戊基乙基，X表示a。

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