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51. 发明授权

US5977374A 5-(4-hydroxy-OR 4-acetoxy-benzyl)-3- triphenylmethylthiazolidine-2,4-dione and method for producing same 失效
标题翻译： 5-（4-羟基-OR 4-乙酰氧基 - 苄基）-3-三苯基甲基噻唑烷-2,4-二酮及其制备方法
公开(公告)号：US5977374A
公开(公告)日：1999-11-02
申请号：US282579
申请日：1994-07-29
申请人： Takashi Fujita , Takao Yoshioka , Horoyoshi Horikoshi , Shinji Yoshioka
发明人： Takashi Fujita , Takao Yoshioka , Horoyoshi Horikoshi , Shinji Yoshioka
IPC分类号： C07D277/20 , A61K31/13 , A61K31/135 , A61K31/165 , A61K31/19 , A61K31/215 , A61K31/425 , A61K31/426 , A61P3/04 , A61P3/06 , A61P3/08 , A61P3/10 , A61P19/10 , C07C59/48 , C07C69/732 , C07C69/92 , C07C215/08 , C07C215/30 , C07C215/68 , C07C217/18 , C07C217/22 , C07C217/60 , C07C235/34 , C07C235/46 , C07C235/56 , C07C235/58 , C07C259/06 , C07C259/10 , C07C323/25 , C07C323/62 , C07D277/34
CPC分类号： C07D277/20 , C07C217/18 , C07C235/34 , C07C259/06 , C07C323/25 , C07C323/62 , C07D277/34
摘要： A compound of the formula ##STR1## wherein R.sup.7 is a hydrogen atom or an acetyl group, and process for preparing said compounds.
摘要翻译：下式化合物其中R7是氢原子或乙酰基，以及制备所述化合物的方法。

52. 发明授权

US5780485A Use of .alpha..sub.1c specific compounds to treat benign prostatic hyperplasia 失效
标题翻译：使用α1c特异性化合物治疗良性前列腺增生
公开(公告)号：US5780485A
公开(公告)日：1998-07-14
申请号：US415681
申请日：1995-04-03
申请人： Charles Gluchowski , Carlos C. Forray , George Chiu , Theresa A. Branchek , John M. Wetzel , Paul R. Hartig
发明人： Charles Gluchowski , Carlos C. Forray , George Chiu , Theresa A. Branchek , John M. Wetzel , Paul R. Hartig
IPC分类号： A61K31/00 , A61K31/135 , A61K31/137 , A61K31/44 , A61K31/4409 , A61K31/4427 , A61K31/445 , A61K31/4515 , A61K31/454 , A61K31/4545 , A61K31/505 , A61K31/517 , A61K31/55 , A61K45/00 , A61P13/02 , A61P15/00 , A61P43/00 , C07C211/30 , C07C215/50 , C07C215/52 , C07C217/58 , C07C217/60 , C07D211/58 , C07D401/12 , C07D405/12 , C07D495/06
CPC分类号： C07D401/12 , A61K31/00 , A61K31/135 , A61K31/137 , A61K31/44 , A61K31/4409 , A61K31/445 , A61K31/4515 , A61K31/454 , A61K31/4545 , A61K31/505 , A61K31/517 , A61K31/55 , C07C211/30 , C07C215/50 , C07C215/52 , C07C217/58 , C07C217/60 , C07D211/58 , C07D405/12 , C07D495/06 , C07C2102/08 , C07C2102/10 , C07C2102/12
摘要： A method of treating benign prostatic hyperplasia in a subject which comprises administering to the subject a therapeutically effective amount of a compound which binds to a human .alpha..sub.1C adrenergic receptor with a binding affinity greater than ten-fold higher than the binding affinity with which the compound binds to a human .alpha..sub.1A adrenergic receptor, a human .alpha..sub.1B adrenergic receptor, and a human histamine H.sub.1 receptor, and, binds to a human .alpha..sub.2 adrenergic receptor with a binding affinity which is greater than ten-fold lower than the binding affinity with which the compound binds to such .alpha..sub.1C adrenergic receptor. Compounds meeting these criteria are provided.
摘要翻译：一种治疗受试者的良性前列腺增生的方法，其包括向受试者施用治疗有效量的结合人α1C肾上腺素能受体的化合物，其结合亲和力比结合亲和力高10倍，化合物与人α1B肾上腺素能受体，人α1B肾上腺素能受体和人组胺H1受体结合，并且结合人α2肾上腺素能受体，其结合亲和力比结合亲和力低10倍该化合物与这种α1C肾上腺素能受体结合。提供符合这些标准的化合物。

53. 发明授权

US5635534A Aromatic amino-alcohol derivatives having anti-diabetic and anti-obesity properties, their preparation and their therapeutic uses 失效
标题翻译：具有抗糖尿病和抗肥胖特性的芳香族氨基醇衍生物，其制备及其治疗用途
公开(公告)号：US5635534A
公开(公告)日：1997-06-03
申请号：US478610
申请日：1995-06-07
申请人： Takashi Fujita , Takao Yoshioka , Horoyoshi Horikoshi , Shinji Yoshioka
发明人： Takashi Fujita , Takao Yoshioka , Horoyoshi Horikoshi , Shinji Yoshioka
IPC分类号： C07D277/20 , A61K31/13 , A61K31/135 , A61K31/165 , A61K31/19 , A61K31/215 , A61K31/425 , A61K31/426 , A61P3/04 , A61P3/06 , A61P3/08 , A61P3/10 , A61P19/10 , C07C59/48 , C07C69/732 , C07C69/92 , C07C215/08 , C07C215/30 , C07C215/68 , C07C217/18 , C07C217/22 , C07C217/60 , C07C235/34 , C07C235/46 , C07C235/56 , C07C235/58 , C07C259/06 , C07C259/10 , C07C323/25 , C07C323/62 , C07D277/34 , C07C279/34
CPC分类号： C07D277/20 , C07C217/18 , C07C235/34 , C07C259/06 , C07C323/25 , C07C323/62 , C07D277/34
摘要： Compounds of formula (I): ##STR1## (wherein: R.sup.0 is hydrogen, methyl or hydroxymethyl; R.sup.1 is substituted alkyl; R.sup.2 and R.sup.3 are each hydrogen, halogen, hydroxy, alkoxy, carboxy, alkoxycarbonyl, alkyl, nitro, haloalkyl, or substituted alkyl; X is oxygen or sulfur; and Ar optionally substituted phenyl or naphthyl); and pharmaceutically acceptable salts thereof have a variety of valuable pharmaceutical activities, including anti-diabetic and anti-obesity activities; in addition, they are capable of treating or preventing hyperlipemia and hyperglycemia and, by inhibiting the action of aldose reductase, they can also be effective in the treatment and prevention of complications of diabetes.
摘要翻译：式（I）化合物：其中：R 0是氢，甲基或羟甲基; R 1是取代的烷基; R 2和R 3各自是氢，卤素，羟基，烷氧基，羧基，烷氧基羰基，烷基，硝基，卤代烷基或取代烷基; X为氧或硫; Ar为任选取代的苯基或萘基）; 和其药学上可接受的盐具有多种有价值的药物活性，包括抗糖尿病和抗肥胖活性; 此外，它们能够治疗或预防高脂血症和高血糖，并且通过抑制醛糖还原酶的作用，它们也可有效治疗和预防糖尿病并发症。

54. 发明授权

US5604032A Fluorine-containing carboxylic acid amine salt and a magnetic recording medium with the same thereon 失效
标题翻译：含氟羧酸胺盐及其上的磁记录介质
公开(公告)号：US5604032A
公开(公告)日：1997-02-18
申请号：US322551
申请日：1994-10-13
申请人： Yoshiaki Kai , Yukikazu Ohchi
发明人： Yoshiaki Kai , Yukikazu Ohchi
IPC分类号： C07C69/63 , C07C69/65 , C07C211/15 , C07C211/24 , C07C217/08 , C07C217/60 , C10M105/60 , G11B5/71 , G11B5/725
CPC分类号： C07C211/15 , C07C211/24 , C07C217/08 , C07C217/60 , C07C69/63 , C07C69/65 , C10M105/60 , G11B5/71 , G11B5/725 , Y10S428/90 , Y10T428/265 , Y10T428/273 , Y10T428/3154
摘要： A fluorine-containing carboxylic acid amine salt of Formula A below: ##STR1## wherein R.sup.1 denotes an aliphatic alkyl group or an aliphatic alkenyl group with 6 to 30 carbons; R.sup.2 denotes a group selected from the group consisting of a fluoroalkyl group with 3 to 30 carbons, a fluoroalkenyl group with 3 to 30 carbons, a fluorophenyl group with 6 to 18 carbons, and a fluoroalkylether group with 5 to 50 carbons; R.sup.3 and R.sup.4 each denotes a saturated or unsaturated hydrocarbon chain with 1 to 20 carbons; R.sup.5 denotes either a fluoroalkyl group with 3 to 30 carbons or a fluoroalkenyl group with 3 to 30 carbons; n denotes 0 or 1; X denotes hydrogen or -(R.sup.6) -R.sup.7 ; and Y denotes hydrogen or -(R.sup.8) -R.sup.9, where R.sup.6 and R.sup.8 each denotes a saturated or unsaturated hydrocarbon chain with 1 to 20 carbons, and R.sup.7 and R.sup.9 each denotes a fluoroalkyl group with 3 to 30 carbons or a fluoroalkenyl group with 3 to 30 carbons.
摘要翻译：下式A的含氟羧酸胺盐：其中R 1表示脂肪族烷基或碳原子数6〜30的脂肪族烯基; R2表示选自碳原子数为3〜30的氟烷基，碳原子数3〜30的氟烯基，碳原子数6〜18的氟代苯基，碳原子数为5〜50的氟代烷基的基团。 R3和R4各自表示具有1至20个碳的饱和或不饱和烃链; R5表示碳原子数为3〜30的氟代烷基或碳原子数为3〜30的氟代烯基， n表示0或1; X表示氢或 - （R6）-R7; 并且Y表示氢或 - （R8）-R9，其中R6和R8各自表示具有1至20个碳的饱和或不饱和烃链，并且R 7和R 9各自表示具有3至30个碳的氟烷基或具有3个氟烯基的氟代烷基至30个碳。

55. 发明授权

US5597940A Process for producing .beta.-nitroenamine 失效
公开(公告)号：US5597940A
公开(公告)日：1997-01-28
申请号：US401928
申请日：1995-03-09
申请人： Shinzo Seko
发明人： Shinzo Seko
IPC分类号： C07C209/00 , C07C211/24 , C07C211/29 , C07C215/52 , C07C217/60 , C07C239/20 , C07C209/60 , C07C253/30
CPC分类号： C07C217/60 , C07C209/00 , C07C211/24 , C07C211/29 , C07C215/52 , C07C239/20 , C07C2101/16
摘要： Disclosed is a process for producing .beta.-nitroenamine represented by the formula I: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and independently indicate a hydrogen atom or a C.sub.1 -C.sub.10 alkyl group which may be optionally substituted with at least one group selected from the group consisting of a halogen atom, a lower alkoxy group, an aryloxy group, a hydroxyl group or an aryl group, or an aryl group which may be optionally substituted with a halogen atom, a lower alkyl group, a lower alkoxy group, an aryl group, an aryloxy group, a nitro group, a cyano group, an acylamino group, a di-lower alkylamino group, an arylamino group, a hydroxyl group, an arylsulfonyl group, a mercapto group, a lower alkylthio group or an arylthio group, R.sub.1 and R.sub.2 may bond together to form a cycloalkyl or bicycloalkyl and R.sub.3 is a hydrogen atom, a lower alkyl group, a cycloalkyl group or an aralkyl group; and an intermediate for producing the .beta.-nitroenamine.

56. 发明授权

US5550291A Process for key intermediates for HIV protease inhibitors 失效
标题翻译： HIV蛋白酶抑制剂关键中间体的方法
公开(公告)号：US5550291A
公开(公告)日：1996-08-27
申请号：US434691
申请日：1995-05-04
申请人： Pierre L. Beaulieu , Yvan Guindon , Dominik M. Wernic
发明人： Pierre L. Beaulieu , Yvan Guindon , Dominik M. Wernic
IPC分类号： C07D303/36 , C07B53/00 , C07C213/00 , C07C213/08 , C07C215/28 , C07C217/60 , C07C209/26 , C07C209/54 , C07C209/68 , C07C209/82
CPC分类号： C07C213/08 , Y02P20/55
摘要： Disclosed herein is a stereospecific synthesis amenable to the large scale preparation of a hydrochloric acid addition salt of a chlorohydrin of the formula ##STR1## wherein R.sup.1 and R.sup.2 are amino protective groups and R.sup.3 is an amino acid side chain or a protected amino acid side chain. The synthesis involves reacting an aldehyde of the formula ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined hereinbefore with (chloromethyl)lithium at -20.degree. C. or below and contacting the resulting diastereoisomeric mixture of lithium alcoholates with aqueous hydrochloric acid to obtain a separable mixture of the hydrochloric acid addition salts of the chlorohydrin and its corresponding hydroxy diastereoisomer. The hydrochloric acid addition salt of the chlorohydrin is transformed readily into corresponding optionally amino-protected aminoepoxides; for example, 3(S)-(tert-butyloxycarbonylamino)-l,2(S)-epoxy-4-phenyl-butane.
摘要翻译：本文公开了一种立体特异性合成，其可以大规模制备下式的氯醇的盐酸加成盐：其中R1和R2是氨基保护基，R3是氨基酸侧链或被保护的氨基酸侧链。该合成包括使式（Ia）的醛，其中R 1，R 2和R 3如上文所定义，与（氯甲基）锂在-20℃或更低的温度下反应，并使所得到的醇锂与盐酸水溶液的非对映异构体混合物接触，得到氯代醇的盐酸加成盐及其相应的羟基非对映异构体的可分离的混合物。氯代醇的盐酸加成盐容易地转化成相应的任选氨基保护的氨基环氧化物; 例如，3（S） - （叔丁氧基羰基氨基）-1,2（S） - 环氧-4-苯基 - 丁烷。

57. 发明授权

US5403847A Use of .alpha..sub.1C specific compounds to treat benign prostatic hyperlasia 失效
标题翻译：使用α1C特异性化合物治疗良性前列腺增生
公开(公告)号：US5403847A
公开(公告)日：1995-04-04
申请号：US975867
申请日：1992-11-13
申请人： Charles Gluchowski , Carlos C. Forray , George Chiu , Theresa A. Branchek , John M. Wetzel , Paul R. Hartig
发明人： Charles Gluchowski , Carlos C. Forray , George Chiu , Theresa A. Branchek , John M. Wetzel , Paul R. Hartig
IPC分类号： A61K31/00 , A61K31/135 , A61K31/137 , A61K31/44 , A61K31/4409 , A61K31/4427 , A61K31/445 , A61K31/4515 , A61K31/454 , A61K31/4545 , A61K31/505 , A61K31/517 , A61K31/55 , A61K45/00 , A61P13/02 , A61P15/00 , A61P43/00 , C07C211/30 , C07C215/50 , C07C215/52 , C07C217/58 , C07C217/60 , C07D211/58 , C07D401/12 , C07D405/12 , C07D495/06
CPC分类号： C07D401/12 , A61K31/00 , A61K31/135 , A61K31/137 , A61K31/44 , A61K31/4409 , A61K31/445 , A61K31/4515 , A61K31/454 , A61K31/4545 , A61K31/505 , A61K31/517 , A61K31/55 , C07C211/30 , C07C215/50 , C07C215/52 , C07C217/58 , C07C217/60 , C07D211/58 , C07D405/12 , C07D495/06 , C07C2102/08 , C07C2102/10 , C07C2102/12
摘要： A method of treating benign prostatic hyperplasia in a subject which comprises administering to the subject a therapeutically effective amount of a compound which binds to a human .alpha..sub.1C adrenergic receptor with a binding affinity greater than ten-fold higher than the binding affinity with which the compound binds to a human .alpha..sub.1A adrenergic receptor, a human .alpha..sub.1B adrenergic receptor, and a human histamine H.sub.1 receptor, and, binds to a human .alpha..sub.2 adrenergic receptor with a binding affinity which is greater than ten-fold lower than the binding affinity with which the compound binds to such .alpha..sub.1C adrenergic receptor. Compounds meeting these criteria are provided.
摘要翻译：一种治疗受试者的良性前列腺增生的方法，其包括向受试者施用治疗有效量的结合人α1C肾上腺素能受体的化合物，其结合亲和力比结合亲和力高10倍，化合物与人α1B肾上腺素能受体，人α1B肾上腺素能受体和人组胺H1受体结合，并且结合人α2肾上腺素能受体，其结合亲和力比结合亲和力低10倍该化合物与这种α1C肾上腺素能受体结合。提供符合这些标准的化合物。

58. 发明授权

US5198587A Phenethylamine derivatives 失效
标题翻译：苯乙胺衍生物
公开(公告)号：US5198587A
公开(公告)日：1993-03-30
申请号：US737976
申请日：1991-07-30
申请人： Kazuo Imai , Kunihiro Niigata , Takashi Fujikura , Shinichi Hashimoto , Toichi Takenaka , Kazuo Honda
发明人： Kazuo Imai , Kunihiro Niigata , Takashi Fujikura , Shinichi Hashimoto , Toichi Takenaka , Kazuo Honda
IPC分类号： C07C217/60
CPC分类号： C07C217/60
摘要： Phenethylamine derivatives shown by the general formula ##STR1## wherein Ro represents a lower alkyl group; R.sub.1 represents a lower alkyl group or a lower alkoxy group; R.sub.2 represents hydrogen atom or a hydroxyl group; R.sub.3 and R.sub.4 each represents hydrogen atom or a lower alkyl group; R.sub.5 represents hydrogen atom or a lower alkoxy group; X represents oxygen atom or a methylene group; m is an integer of 1-3; and n is an integer of 0-2 and the acid addition salts thereof.These compounds exhibit a strong .alpha.-adrenergic blocking action and are useful as an antihypertensive agent.
摘要翻译：苯乙胺衍生物，其通式为：其中R a代表低级烷基; R1表示低级烷基或低级烷氧基; R2表示氢原子或羟基; R3和R4各自表示氢原子或低级烷基; R5表示氢原子或低级烷氧基; X表示氧原子或亚甲基; m为1-3的整数; n为0-2的整数，及其酸加成盐。这些化合物表现出强的α-肾上腺素能阻断作用，可用作抗高血压药。

59. 发明授权

US5057624A Process for the synthesis of the N-methyl-3,4-dimethoxyphenylethylamine 失效
标题翻译：合成N-甲基-3,4-二甲氧基苯乙酰胺的方法
公开(公告)号：US5057624A
公开(公告)日：1991-10-15
申请号：US502038
申请日：1990-03-30
申请人： Vincenzo Cannata , Giancarlo Tamerlani , Graziano Zagnoni
发明人： Vincenzo Cannata , Giancarlo Tamerlani , Graziano Zagnoni
IPC分类号： C07C213/04 , C07C213/00 , C07C213/02 , C07C217/60
CPC分类号： C07C213/02 , C07C217/60
摘要： New process for the synthesis of the N-methyl-3,4-dimetoxyphenylethylamine of formula ##STR1## intermediate in the synthesis of the drug internationally known as verapamil. The process starts from the 3,4-dimethoxybenzaldehyde which, by means of a Darzens condensation, gives an epoxyester that, by alkaline hydrolysis and subsequent decarboxylation, gives the 3,4-dimethoxyphenylacetaldehyde. This aldehyde gives the amine of formula I by reaction with monomethylamine followed by reduction with sodium borohydride.

60. 发明授权

US5057623A Organic fluorine compound 失效
标题翻译：有机氟化合物
公开(公告)号：US5057623A
公开(公告)日：1991-10-15
申请号：US420876
申请日：1989-10-13
申请人： Yoshiaki Kai , Takashi Suzuki
发明人： Yoshiaki Kai , Takashi Suzuki
IPC分类号： C07C33/48 , C07C53/21 , C07C57/58 , C07C57/60 , C07C57/76 , C07C59/135 , C07C59/68 , C07C69/63 , C07C211/15 , C07C211/29 , C07C211/48 , C07C211/52 , C07C217/08 , C07C217/58 , C07C217/60 , C07C217/62 , C07C233/05 , C07C233/11 , C07C233/13 , C07C233/22 , C07C233/36 , C07C233/69 , C07C235/34 , C07C235/48 , C07C235/52 , C07C237/06 , C07C237/22 , C07C311/05 , C07C311/06 , G11B5/70 , G11B5/725
CPC分类号： C07C53/21 , C07C211/15 , C07C211/29 , C07C211/48 , C07C211/52 , C07C217/08 , C07C217/58 , C07C217/60 , C07C217/62 , C07C233/05 , C07C233/11 , C07C233/13 , C07C233/22 , C07C233/36 , C07C233/69 , C07C235/34 , C07C235/48 , C07C235/52 , C07C237/06 , C07C237/22 , C07C311/05 , C07C311/06 , C07C33/483 , C07C57/58 , C07C57/60 , C07C57/76 , C07C59/135 , C07C59/68 , C07C69/63 , G11B5/7013 , G11B5/725
摘要： An organic fluorine compound represented by the general formulaR.sub.f -(X).sub.h -R-Mwherein R.sub.f is a group selected from the following (a) and (b); ##STR1## X denotes a linking group selected from --O--, --S--, and --COO--, h denotes 0 or 1, R is a hydrocarbon chain comprising a phenylene group having an alkylene group with a total carbon number of 10 or more, or the derivative thereof, or an aliphatic alkylene group of a carbon number of 10 or more, and M is a group selected from --OH, --COOH, --SH, and --CONH.sub.2.The organic fluorine compound of the present invention greatly improves the dispersibility of magnetic powders in magnetic coating materials, has also an excellent rust prevention effect on metallic magnetic powders, and exhibits a marked dispersing effect even on fluorocarbon resin fine powders, which can be difficultly dispersed with conventional dispersing agents.

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