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91. 发明授权

US6040422A Synthesis and use of amino acid fluorides as peptide coupling reagent 失效
标题翻译：氨基酸氟化物作为肽偶联剂的合成和使用
公开(公告)号：US6040422A
公开(公告)日：2000-03-21
申请号：US2860
申请日：1998-01-05
申请人： Louis A. Carpino , Ayman Ahmed El-Faham
发明人： Louis A. Carpino , Ayman Ahmed El-Faham
IPC分类号： C07C237/22 , C07C255/14 , C07C271/10 , C07C271/34 , C07C275/40 , C07C275/70 , C07C317/04 , C07C317/10 , C07C317/14 , C07C317/18 , C07C321/14 , C07C321/20 , C07C323/14 , C07D207/16 , C07D209/20 , C07D233/64 , C07D233/68 , C07D295/215 , C07D317/18 , C07K1/06 , C07K1/08 , C07K1/10 , C07K1/113
CPC分类号： C07D295/215 , C07C271/10 , C07C271/34 , C07C275/40 , C07C275/70 , C07C317/04 , C07C317/10 , C07C317/14 , C07C317/18 , C07C321/14 , C07C321/20 , C07C323/14 , C07D207/16 , C07D209/20 , C07D233/68 , C07K1/088 , C07K1/10 , C07C2103/18 , Y02P20/55
摘要： The present invention is directed to a process for forming a peptide bond between a first amino acid having a free amino group and a protected carboxy group and a second amino acid or between a peptide having a free amino group and a blocking carboxy group with a second amino acid which comprises (a) reacting the second amino acid of the formula: ##STR1## with a fluoroformamidinium salt of the formula: ##STR2## and (b) reacting the product of (a) with the first amino acid or peptide.
摘要翻译：本发明涉及在具有游离氨基和被保护的羧基的第一个氨基酸与第二个氨基酸之间或具有游离氨基和阻断羧基的肽之间形成肽键的方法，其中第二个氨基酸，其包含（a）使下式的第二氨基酸与下式的氟代甲脒盐反应：和（b）使（a）的产物与第一氨基酸或肽反应。

92. 发明授权

US6005138A Tricyclic taxanes having a butenyl substituted side-chain and pharmaceutical compositions containing them 失效
标题翻译：具有丁烯基取代侧链的三环紫杉烷和含有它们的药物组合物
公开(公告)号：US6005138A
公开(公告)日：1999-12-21
申请号：US989990
申请日：1997-12-12
申请人： Robert A. Holton , Ki-byung Chai , Hossain Nadizadeh
发明人： Robert A. Holton , Ki-byung Chai , Hossain Nadizadeh
IPC分类号： C07C227/22 , C07C231/12 , C07C233/87 , C07D205/08 , C07D305/14 , C07D407/12 , C07D409/12 , C07F7/00 , C07F7/18 , C07C271/10
CPC分类号： C07D407/12 , C07C227/22 , C07C231/12 , C07C233/87 , C07D205/08 , C07D305/14 , C07D409/12 , C07F7/006 , C07F7/1856 , C07F7/186 , C07C2101/14 , C07C2101/16 , C07C2103/62
摘要： Taxane derivatives having a 3' butenyl substituted C13 side chain.
摘要翻译：具有3'丁烯基取代的C13侧链的紫杉烷衍生物。

93. 发明授权

US5998636A Carbamate herbicides 失效
标题翻译：氨基甲酸酯除草剂
公开(公告)号：US5998636A
公开(公告)日：1999-12-07
申请号：US128651
申请日：1998-08-04
申请人： Hermann Rempfler , Fredrik Cederbaum , Felix Spindler , Willy Urs Lottenbach
发明人： Hermann Rempfler , Fredrik Cederbaum , Felix Spindler , Willy Urs Lottenbach
IPC分类号： A01N47/12 , C07C43/23 , C07C269/02 , C07C271/10 , C07C271/12 , C07C323/12 , C07D213/40 , C07D317/46 , C07D333/20 , C07D333/28 , C07D317/44 , C07C43/00
CPC分类号： C07D213/40 , A01N47/12 , C07C271/12 , C07C43/23 , C07D317/46 , C07D333/20 , C07D333/28 , C07B2200/07
摘要： Substituted N-phenyl- and N-heteroarylalkylcarbamates of the formula I ##STR1## in which Q is a group ##STR2## R is halogen, trifluoromethyl, cyano, nitro or C.sub.1 -C.sub.3 haloalkoxy;Z is hydrogen or halogen; orZ and R together in the 2- and 3-position of the phenyl ring form a group --OCF.sub.2 O--;R.sub.1 is C.sub.1 -C.sub.5 alkyl;R.sub.2, R.sub.3, R.sub.4 and R.sub.5, independently of one another, are hydrogen, methyl or ethyl;X is oxygen, sulfur, --SO-- or --SO.sub.2 --;Y is hydrogen, halogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.3 alkoxy or cyano;n is 0, 1 or 2;n.sub.1 is 0 or 1; andm is 0 or 1,with the proviso that m is 1 if Q is group (1) or (2);and the diastereomers and enantiomers thereof,exhibit pre- and post-emergence herbicidal properties. The preparation of these compounds and their use as herbicidally active ingredients are described.
摘要翻译：其中Q为基团R的式I的取代的N-苯基 - 和N-杂芳基烷基氨基甲酸酯是卤素，三氟甲基，氰基，硝基或C 1 -C 3卤代烷氧基; Z是氢或卤素; 或Z和R在苯环的2-和3-位一起形成-OCF 2 O - 基团; R1是C1-C5烷基; R2，R3，R4和R5彼此独立地是氢，甲基或乙基; X是氧，硫，-SO-或-SO 2 - ; Y是氢，卤素，C 1 -C 3烷基，C 1 -C 3卤代烷基，C 1 -C 3烷氧基或氰基; n为0,1或2; n1为0或1; m为0或1，条件是如果Q为基团（1）或（2），则m为1; 及其非对映异构体和对映异构体，显示出芽前和芽后除草性质。描述了这些化合物的制备及其作为除草活性成分的用途。

94. 发明授权

US5968975A Elevation of HDL cholesterol by 2-[(aminothioxomethyl)-hydrazono]-2-arylethyl carbamates 失效
标题翻译： 2 - [（氨基硫代甲基） - 肼基] -2-芳基乙基氨基甲酸酯升高HDL胆固醇
公开(公告)号：US5968975A
公开(公告)日：1999-10-19
申请号：US96091
申请日：1998-06-11
申请人： Thomas Joseph Commons , Susan Christman
发明人： Thomas Joseph Commons , Susan Christman
IPC分类号： C07C337/08 , C07C255/27 , A61K31/27 , C07C271/10
CPC分类号： C07C337/08
摘要： This invention relates to the treatment of atherosclerosis via raising the level of HDL cholesterol by administration of a compound of the formula ##STR1## wherein: R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.6 alkyl or --(CH.sub.2).sub.0-6 Ph where Ph is phenyl optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH;R.sup.4 and R.sup.5 are independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, or --(CH.sub.2).sub.0-6 Ar.sup.1 where Ar.sup.1 is phenyl, naphthyl, furanyl, pyridinyl or thienyl and Ar.sup.1 can be optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, phenyl, C.sub.1 -C.sub.6 alkoxy, phenoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH; andAr is phenyl, naphthyl, furanyl, pyridinyl or thienyl or Ar is optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, phenyl, C.sub.1 -C.sub.6 alkoxy, phenoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH.
摘要翻译：本发明涉及通过施用下式化合物来提高HDL胆固醇水平来治疗动脉粥样硬化：其中：R1，R2和R3独立地是氢，C1-C6烷基或 - （CH2）0-6Ph，其中Ph是任选被卤素，氰基，硝基，C 1 -C 6烷基，C 1 -C 6烷氧基，三氟甲基，C 1 -C 6烷氧基羰基，-CO 2 H或OH取代的苯基; R 4和R 5独立地是氢，C 1 -C 6烷基，C 3 -C 8环烷基或 - （CH 2）0-6Ar 1，其中Ar 1是苯基，萘基，呋喃基，吡啶基或噻吩基，Ar 1可以任选地被卤素，氰基，硝基， C 1 -C 6烷基，苯基，C 1 -C 6烷氧基，苯氧基，三氟甲基，C 1 -C 6烷氧基羰基，-CO 2 H或OH; 氰基，硝基，C 1 -C 6烷基，C 3 -C 6环烷基，苯基，C 1 -C 6烷氧基，苯氧基，三氟甲基，C 1 -C 6烷氧基羰基，C 1 -C 6烷氧基， -CO 2 H或OH。

95. 发明授权

US5863918A Naphthalene derivatives 失效
标题翻译：萘衍生物
公开(公告)号：US5863918A
公开(公告)日：1999-01-26
申请号：US28861
申请日：1998-02-23
申请人： Kiyoshi Taniguchi , Masanobu Nagano , Kouji Hattori , Kazunori Tsubaki , Osamu Okitsu , Seiichiro Tabuchi
发明人： Kiyoshi Taniguchi , Masanobu Nagano , Kouji Hattori , Kazunori Tsubaki , Osamu Okitsu , Seiichiro Tabuchi
IPC分类号： A61K31/16 , A61K31/335 , A61K31/336 , A61K31/44 , A61K31/4418 , A61K31/4425 , A61K31/50 , A61P7/02 , A61P9/10 , A61P9/12 , A61P43/00 , C07C69/145 , C07C235/40 , C07C271/10 , C07C271/12 , C07C271/24 , C07C271/28 , C07C271/32 , C07C281/02 , C07D213/64 , C07D237/14 , C07D303/12 , C07D303/16 , A01N43/58 , C07D237/00
CPC分类号： C07D213/64 , C07C271/12 , C07C271/28 , C07C281/02 , C07D237/14 , C07D303/16 , C07C2102/10
摘要： A compound or the formula: ##STR1## wherein R.sup.1 is carboxy or protected carboxy, R.sup.2 is hydrogen, hydroxy or protected hydroxy,R.sup.3 is hydrogen, hydroxy, protected hydroxy, etc.,R.sup.4 is hydrogen or halogen,A.sup.1 is lower alkylene,A.sup.2 is bond or lower alkylene,--R.sup.5 is ##STR2## (in which R.sup.6 is mono(or di or tri)aryl(lower)alkyl and Z is N or CH), etc., and ##STR3## etc., and a pharmaceutically acceptable salt thereof which are useful as medicaments.
摘要翻译：化合物或式：其中R 1是羧基或保护的羧基，R 2是氢，羟基或被保护的羟基，R 3是氢，羟基，保护的羟基等，R 4是氢或卤素，A 1是低级亚烷基，A 2 （其中R 6是单（或二或三）芳基（低级）烷基，Z是N或CH）等，和

96. 发明授权

US5753731A Viscosity conditioner and emulsion and emulsion paint compositions 失效
标题翻译：粘度调节剂和乳液和乳液漆组合物
公开(公告)号：US5753731A
公开(公告)日：1998-05-19
申请号：US706347
申请日：1996-08-30
申请人： Toyotaro Yoshioka , Kaoru Komiya
发明人： Toyotaro Yoshioka , Kaoru Komiya
IPC分类号： C08G18/28 , C09D7/00 , C08K5/205 , B01J13/00 , C07C269/02 , C07C271/10
CPC分类号： C09D5/024 , C08G18/283 , C09D7/002 , C08L75/08 , Y10S526/932
摘要： A viscosity conditioner is disclosed which comprises a compound structured to have a group of the following formula (1) ##STR1## where R is a hydrocarbyl group, R' is a branched or secondary hydrocarbyl group, and n ranges from 1 to 500. The specified viscosity conditioner is conducive to reduced temperature dependence and hence constant viscosity in a certain range suited for all environmental conditions and good coatability at all seasons. Also disclosed are an emulsion composition and an emulsion paint composition, each of which include of the viscosity conditioner.
摘要翻译：公开了一种粘度调节剂，其包含具有下式（1）的基团的化合物：其中R是烃基，R'是支链或仲烃基，n的范围从1到特定的粘度调节剂有利于降低温度依赖性，因此有利于在适合所有环境条件的一定范围内的恒定粘度和在所有季节具有良好的涂布性。还公开了乳液组合物和乳液漆组合物，其中每一种都包括粘度调节剂。

97. 发明授权

US5646121A Pseudopeptides with antiviral activity 失效
标题翻译：具有抗病毒活性的假肽
公开(公告)号：US5646121A
公开(公告)日：1997-07-08
申请号：US302064
申请日：1994-09-07
申请人： Dieter Habich , Thomas-J. Schulze , Jurgen Reefschlager , Jutta Hansen , Rainer Neumann , Gert Streissle , Arnold Paessens
发明人： Dieter Habich , Thomas-J. Schulze , Jurgen Reefschlager , Jutta Hansen , Rainer Neumann , Gert Streissle , Arnold Paessens
IPC分类号： C07D249/06 , A61K38/00 , A61P31/12 , C07C237/22 , C07C271/10 , C07C275/28 , C07C279/02 , C07C279/14 , C07C311/64 , C07C317/44 , C07D213/24 , C07D213/81 , C07D215/48 , C07D311/70 , C07D333/70 , C07K1/02 , C07K1/10 , C07K1/113 , C07K1/12 , C07K5/068 , C07K5/072 , C07K5/087 , C07K5/09 , C07K5/093 , C07K5/097 , C07D241/04 , A61K31/16 , A61K31/165 , C07D211/06
CPC分类号： C07K5/0817 , C07C311/64 , C07K5/06095 , A61K38/00
摘要： The present invention relates to novel pseudopeptides with antiviral activity of the general formula (I) ##STR1## in which the substituents have the meaning given in the description, to a process for their preparation, and to their use as antiviral agents, especially against cytomegaloviruses.
摘要翻译：本发明涉及具有通式（I）（I）的抗病毒活性的新型伪肽，其中取代基具有本说明书中给出的含义，其制备方法及其作为抗病毒剂的用途，特别是针对巨细胞病毒。

98. 发明授权

US5559256A Aminediol protease inhibitors 失效
标题翻译：胺二醇蛋白酶抑制剂
公开(公告)号：US5559256A
公开(公告)日：1996-09-24
申请号：US79978
申请日：1993-06-25
申请人： Eric M. Gordon , Joel C. Barrish , Gregory S. Bisacchi , Chong-Qing Sun , Joseph A. Tino , Gregory D. Vite , Robert Zahler
发明人： Eric M. Gordon , Joel C. Barrish , Gregory S. Bisacchi , Chong-Qing Sun , Joseph A. Tino , Gregory D. Vite , Robert Zahler
IPC分类号： A61K31/13 , A61K31/16 , A61K31/18 , A61K31/265 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4166 , A61K31/4184 , A61K31/496 , A61K31/505 , A61P31/12 , A61P31/18 , A61P37/00 , C07C215/28 , C07C233/40 , C07C233/78 , C07C235/40 , C07C237/10 , C07C271/10 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/16 , C07C275/24 , C07C311/03 , C07C311/05 , C07C313/06 , C07C333/04 , C07C333/12 , C07D207/09 , C07D207/16 , C07D207/26 , C07D207/267 , C07D209/12 , C07D209/14 , C07D209/18 , C07D209/44 , C07D209/46 , C07D213/30 , C07D213/36 , C07D213/40 , C07D213/55 , C07D213/56 , C07D213/65 , C07D215/14 , C07D215/48 , C07D217/16 , C07D231/56 , C07D233/30 , C07D233/32 , C07D233/54 , C07D235/12 , C07D235/14 , C07D235/16 , C07D235/24 , C07D239/34 , C07D239/91 , C07D241/42 , C07D243/04 , C07D263/22 , C07D263/24 , C07D263/26 , C07D263/32 , C07D263/56 , C07D265/32 , C07D277/64 , C07D295/092 , C07D295/185 , C07D303/36 , C07D305/08 , C07D307/20 , C07D307/24 , C07D309/10 , C07D333/64 , C07D413/14 , C07D491/04 , C07D521/00 , C07F7/08 , C07F7/18 , C07D401/12
CPC分类号： C07D207/267 , C07C215/28 , C07C233/40 , C07C233/78 , C07C235/40 , C07C237/10 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/16 , C07C275/24 , C07C311/03 , C07C333/04 , C07C333/12 , C07D207/09 , C07D207/16 , C07D209/12 , C07D209/14 , C07D209/18 , C07D209/44 , C07D209/46 , C07D213/30 , C07D213/40 , C07D213/56 , C07D213/65 , C07D215/14 , C07D215/48 , C07D217/16 , C07D231/12 , C07D231/56 , C07D233/32 , C07D233/56 , C07D233/64 , C07D235/12 , C07D235/14 , C07D235/16 , C07D235/24 , C07D239/91 , C07D241/42 , C07D249/08 , C07D263/22 , C07D263/24 , C07D263/26 , C07D263/32 , C07D263/56 , C07D265/32 , C07D277/64 , C07D295/088 , C07D295/185 , C07D305/08 , C07D307/20 , C07D307/24 , C07D309/10 , C07D333/64 , C07D413/14 , C07D491/04 , C07F7/0812 , C07F7/0818 , C07F7/1852 , C07F7/1856 , C07C2101/04 , C07C2101/08 , C07C2101/14 , C07C2103/18
摘要： Novel aminediol compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds in inhibiting retroviral protease, particularly useful in the treatment and/or prevention of HIV infection (AIDS).
摘要翻译：新型二胺化合物，含有这些化合物的药物组合物，以及使用这些化合物抑制逆转录病毒蛋白酶的方法，特别可用于治疗和/或预防HIV感染（AIDS）。

99. 发明授权

US5453536A Polycarbamates, process for preparing polycarbamates, and process for preparing polyisocyanates 失效
标题翻译：聚氨酯，制备聚氨酯的方法和制备多异氰酸酯的方法
公开(公告)号：US5453536A
公开(公告)日：1995-09-26
申请号：US209151
申请日：1994-03-10
申请人： Shenghong A. Dai , Chester R. Norman , Hong-Anh Nguyen
发明人： Shenghong A. Dai , Chester R. Norman , Hong-Anh Nguyen
IPC分类号： C07C265/10 , C07B61/00 , C07C263/04 , C07C265/14 , C07C269/06 , C07C271/10 , C07C271/24 , C07C271/28 , C07C261/00 , C07C263/00
CPC分类号： C07C271/24 , C07C271/10 , C07C271/28
摘要： Polycarbamates of a polyisocyanate and secondary alcohols are disclosed. These carbamates are characterized in being readily pyrolyzed to form the corresponding polyisocyanate and alcohol with low formation of tars and other by-products. Thus, these polycarbamates can be pyrolyzed under relatively mild conditions, and in the absence of solvent and catalyst.
摘要翻译：公开了多异氰酸酯和仲醇的聚氨酯。这些氨基甲酸酯的特征在于易于热解以形成相应的多异氰酸酯和醇，形成焦油和其它副产物。因此，这些多氨基甲酸盐可以在相对温和的条件下和在不存在溶剂和催化剂的条件下热解。

100. 发明授权

US5399578A Acyl compounds 失效
标题翻译：酰基化合物
公开(公告)号：US5399578A
公开(公告)日：1995-03-21
申请号：US998755
申请日：1992-12-29
申请人： Peter Buhlmayer , Franz Ostermayer , Tibur Schmidlin
发明人： Peter Buhlmayer , Franz Ostermayer , Tibur Schmidlin
IPC分类号： A61K31/195 , A61K31/41 , A61K31/44 , A61K31/47 , A61K31/535 , A61K31/675 , A61P9/12 , C07C229/38 , C07C231/00 , C07C233/47 , C07C233/51 , C07C233/54 , C07C235/04 , C07C271/10 , C07C311/48 , C07D233/54 , C07D233/58 , C07D233/64 , C07D257/04 , C07D401/12 , C07D401/14 , C07D403/00 , C07D405/00 , C07D409/00 , C07F9/6524
CPC分类号： C07D233/64 , C07C229/38 , C07C233/54 , C07D257/04 , C07D401/12
摘要： Compounds of the formula ##STR1## in which R.sub.1 is an aliphatic hydrocarbon radical which is unsubstituted or substituted by halogen or hydroxyl, or a cycloaliphatic or araliphatic hydrocarbon radical; X.sub.1 is CO, SO.sub.2, or --O--C(.dbd.O)-- with the carbon atom of the carbonyl group being attached to the nitrogen atom shown in formula I; X.sub.2 is a divalent aliphatic hydrocarbon radical which is unsubstituted or substituted by hydroxyl, carboxyl, amino, guanidino or a cycloaliphatic or aromatic radical, or is a divalent cycloaliphatic hydrocarbon radical, it being possible for a carbon atom of the aliphatic hydrocarbon radical to be additionally bridged by a divalent aliphatic hydrocarbon radical; R.sub.2 is carboxyl which, if desired, is esterified or amidated, substituted or unsubstituted amino, formyl which, if desired, is acetalized, 1H-tetrazol-5-yl, pyridyl, hydroxyl which, if desired, is etherified, S(O).sub.m --R where m is 0, 1 or 2 and R is hydrogen or an aliphatic hydrocarbon radical, alkanoyl, unsubstituted or N-substituted sulfamoyl or PO.sub.n H.sub.2 where n is 2 or 3; X.sub.3 is a divalent aliphatic hydrocarbon; R.sub.3 is carboxyl, 5-tetrazolyl, SO.sub.3 H, PO.sub.2 H.sub.2, PO.sub.3 H.sub.2 or haloalkylsulfamoyl; and the rings A and B independently of one another are substituted or unsubstituted; in free form or in salt form, can be prepared in a manner known per se and can be used, for example, as medicament active ingredients.
摘要翻译：式（I）的化合物，其中R 1是未被取代或被卤素或羟基取代的脂族烃基，或脂环族或芳脂族烃基; X 1是CO，SO 2或-O-C（= O） - ，其中羰基的碳原子连接到式I所示的氮原子上; X2是未取代的或被羟基，羧基，氨基，胍基或脂环族或芳族基团取代的二价脂族烃基，或者是二价脂环族烃基，脂族烃基的碳原子可能另外由二价脂族烃基桥连; R 2是羧基，如果需要，其被酯化或酰胺化，取代或未取代的氨基，如果需要，缩醛化的甲酰基，1H-四唑-5-基，吡啶基，羟基，如果需要，其醚化，S（O） mR，其中m为0,1或2，R为氢或脂族烃基，烷酰基，未取代的或N-取代的氨磺酰基或POnH 2，其中n为2或3; X3是二价脂族烃; R3是羧基，5-四唑基，SO3H，PO2H2，PO3H2或卤代烷基氨磺酰; 环A和B彼此独立地是取代或未取代的; 游离形式或盐形式可以以本身已知的方式制备，并且可以用作例如药物活性成分。

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