-
公开(公告)号:US06646152B1
公开(公告)日:2003-11-11
申请号:US10070759
申请日:2002-03-12
申请人: Monika Knopp , Rolf Jansen
发明人: Monika Knopp , Rolf Jansen
IPC分类号: C07C6976
CPC分类号: C07C67/343 , C07C69/675 , C07C69/732
摘要: A process for preparing 2-hydroxycarboxylic esters having a quaternary &bgr;-carbon atom by reaction of glycidyl esters with an organoaluminum reagent is described.
摘要翻译: 描述了通过缩水甘油酯与有机铝试剂的反应来制备具有季铵碳原子的2-羟基羧酸酯的方法。
-
公开(公告)号:US06630493B1
公开(公告)日:2003-10-07
申请号:US09673087
申请日:2000-10-11
IPC分类号: A01N4340
CPC分类号: C07D213/82 , C07D233/90 , C07D239/28 , C07D239/30 , C07D277/56 , C07D401/04
摘要: Amides of the general formula I and their tautomeric and isomeric forms, possible enantiomeric and diastereomeric forms, as well as possible physiologically tolerable salts, in which the variables have the meanings stated in the description, their preparation and use as calpain inhibitors.
摘要翻译: 通式I的酰胺及其互变异构体和异构体形式,可能的对映异构体和非对映体形式,以及可能的生理上可耐受的盐,其中变量具有描述中所述的含义,其制备和用作钙蛋白酶抑制剂。
-
公开(公告)号:US08536373B2
公开(公告)日:2013-09-17
申请号:US12442162
申请日:2007-09-27
申请人: Michael Stanek , Stefan Essl , Monika Knopp , Erwin Kübel
发明人: Michael Stanek , Stefan Essl , Monika Knopp , Erwin Kübel
IPC分类号: C07C61/00
CPC分类号: C07C403/20 , C07B2200/09 , C07C2601/16 , C07F9/5442
摘要: Improved method of production of 9-(Z)-retinoic acid, in which a) a β-formyl-crotonic acid C1-C10 alkyl or phenyl ester is reacted with an isolated 9-(Z)—C15-triarylphosphonium salt by the Wittig reaction in the presence of a base to the corresponding 9-(Z)-retinoic acid ester; which b) is then saponified with a base to the corresponding 9-(Z)-retinoic acid carboxylate and then, following protonation with an acid, the desired 9-(Z)-retinoic acid is obtained, and improved method for the enrichment and isolation of the 9-(Z)—C15-triarylphosphonium salt.
摘要翻译: 改进的9-(Z) - 视黄酸的制备方法,其中a)β-甲酰基 - 巴豆酸C1-C10烷基或苯基酯与Wittig与分离的9-(Z)-C15-三芳基鏻盐反应 在碱存在下与相应的9-(Z) - 视黄酸酯反应; 然后将b)用碱皂化成相应的9-(Z) - 视黄酸羧酸酯,然后在用酸质子化后,得到所需的9-(Z) - 视黄酸,并且改进了富集和 分离9-(Z)-C 15 - 三芳基鏻盐。
-
公开(公告)号:US06639081B1
公开(公告)日:2003-10-28
申请号:US10031703
申请日:2002-04-30
申请人: Monika Knopp , Stefan Koser , Bernd Schaefer
发明人: Monika Knopp , Stefan Koser , Bernd Schaefer
IPC分类号: C07D27704
CPC分类号: C07D277/56
摘要: The invention relates to processes for preparing 2-aminomethyl-4-cyanothiazole and its salts of the formulae Ia and Ib in which n=1 or 2 and for n=1, X is chloride, bromide, triflate and hydrogen sulfate and for n=2, X is sulfate, which comprises the process step where the aminonitrile of the formula II is stirred with a cysteine ester of the formula III, in which R1 is branched or linear C1-10-alkyl or where n=0, 1 or 2 and R2 is branched or linear C1-C10C10-alkyl or C1-C4-alkoxy or C1-C4-dialkylamino in an inert solvent in the presence of a base at from 0° C. to 80° C. until the reaction has essentially proceeded to completion, and to the compounds of the formulae Ia and Ib.
摘要翻译: 本发明涉及制备2-氨基甲基-4-氰基噻唑及其盐,其中n = 1或2,n = 1,X为氯化物,溴化物,三氟甲磺酸酯和硫酸氢盐,n = 2,X为 硫酸盐,其包括其中式II的氨基腈与式III的半胱氨酸酯一起搅拌的方法步骤,其中R 1是支链或直链的C 1-10 - 烷基或其中n = 0,1或2, 2>是在0℃至80℃的碱存在下,在惰性溶剂中的支链或直链C 1 -C 10 C 10 - 烷基或C 1 -C 4 - 烷氧基或C 1 -C 4 - 二烷基氨基,直到反应基本上进行 以及式Ia和Ib的化合物。
-
5.
公开(公告)号:US06482832B1
公开(公告)日:2002-11-19
申请号:US09700453
申请日:2000-11-15
IPC分类号: C07D20914
CPC分类号: C07D401/04 , C07D215/06 , C07D217/14 , C07D403/04
摘要: Amides of the general formula I and their tautomeric and isomeric forms, possible enantiomeric and diastereomeric forms, and also possible physiologically tolerated salts, in which the variables have the meanings indicated in the description.
摘要翻译: 通式I的酰胺及其互变异构体和异构体形式,可能的对映异构体和非对映体形式,以及可能的生理上耐受的盐,其中变量具有说明书中指出的含义。
-
公开(公告)号:US20110275615A1
公开(公告)日:2011-11-10
申请号:US12915680
申请日:2010-10-29
IPC分类号: A61K31/166 , C07D213/80 , C07D295/135 , C07D207/09 , C07D211/32 , C07D213/50 , C07D401/10 , C07D413/10 , C07D209/14 , C07D223/04 , C07D217/20 , A61K31/455 , A61K31/5375 , A61K31/40 , A61K31/495 , A61K31/4453 , A61K31/44 , A61K31/496 , A61K31/4439 , A61K31/444 , A61K31/5377 , A61K31/454 , A61K31/55 , A61K31/4725 , A61K31/472 , A61P25/28 , A61P25/00 , A61P25/14 , A61P25/08 , A61P9/10 , A61P21/00 , A61P35/00 , A61P9/00 , A61P27/12 , A61P35/04 , A61P29/00 , C07C237/32
CPC分类号: C07D213/82 , A61K31/195 , A61K31/5375 , C07C229/38 , C07C237/22 , C07C237/32 , C07C2601/14 , C07D295/155
摘要: An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine, morpholine, piperidine, —NR5R6 and and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m—, —CH═CH—, —C═C—, and R2 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl and NH2, and R3 is —C1-C6-alkyl, branched or unbranched, and which may also carry a phenyl ring, indolyl ring or cyclohexyl ring which is in turn substituted by a maximum of two R8 radicals, where R8 is hydrogen, C1-C4-alkyl, branched or unbranched, —O—C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COO—C1-C4-alkyl, NHCO—C1-C4-alkyl, —NHSO2—C1-C4-alkyl and —SO2—C1-C4-alkyl; and Y is phenyl, pyridine, pyrimidine and pyrazine and R4 is hydrogen, COOR9 and CO—Z in which Z is NR10R11 and R9 is hydrogen, C1-C6-alkyl, linear or branched, and which may [lacuna] substituted by a phenyl ring which may itself also be substituted by one or two R12 radicals, and R10 is hydrogen, C1-C6-alkyl, linear or branched, and which may [lacuna] substituted by a phenyl ring which itself may also be substituted by one or two R12 radicals, and R11 is hydrogen, C1-C6-alkyl, branched or unbranched, which may also be and substituted by a phenyl ring which may also carry an R9 radical, and R12 can be hydrogen, C1-C4-alkyl, branched or unbranched, —O—C1-C4-alkyl, OH, Cl, F, Br, J, CF3, NO2, NH2, CN, COOH, COO—C1-C4-alkyl, —NHCO—C1-C4-alkyl, —NHCO-phenyl, —NHSO2—C1-C4-alkyl, NHSO2-phenyl, —SO2—C1-C4-alkyl and —SO2-phenyl, R13 is hydrogen, C1-C6-alkyl, linear or branched, and which may [lacuna] substituted by a phenyl ring which may itself also be substituted by one or two R12 radicals, and R14 is hydrogen, C1-C6-alkyl, linear or branched, and which may [lacuna] substituted by a phenyl ring which may itself also be substituted by one or two R12 radicals, and n is a number 0, 1 or 2, and m,q are, independently of one another, a number 0, 1, 2, 3 or 4.
-
公开(公告)号:US20080113989A1
公开(公告)日:2008-05-15
申请号:US11897057
申请日:2007-08-29
IPC分类号: A61K31/5375 , A61K31/195 , A61P19/02 , A61P25/28 , A61P35/00 , A61P37/00 , A61P9/10 , C07C233/76 , C07D265/30
CPC分类号: C07D213/82 , A61K31/195 , A61K31/5375 , C07C229/38 , C07C237/22 , C07C237/32 , C07C2601/14 , C07D295/155
摘要: An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts.
摘要翻译: 式I的酰胺及其互变异构形式,可能的对映体和非对映体形式,E和Z形式以及可能的生理上耐受的盐。
-
公开(公告)号:US06448254B1
公开(公告)日:2002-09-10
申请号:US09647677
申请日:2000-10-03
IPC分类号: C07C31121
CPC分类号: C07D213/56 , C07C311/21 , C07D215/36 , C07D239/70 , C07D239/96
摘要: Amides of the general formula I and their tautomeric and isomeric forms, possible enantiomeric and diastereomeric forms, as well as possible physiologically tolerable salts, in which the variables have the following meanings: R1 [sic] can be C1-C6-alkyl, phenyl, naphthyl, quinolyl, pyridyl, pyrimidyl, pyridazyl, quinazolyl and quinoxalyl, where the rings can additionally be substituted by up to 2 radicals R4 [sic], and R2 [sic] is —(CH2)m—R8 [sic], where R8 [sic] can be phenyl, cyclohexyl- or indolyl and m=1 to 6, and X is a bond, —CH2—, —CH2CH2—, —CH═CH—, —C≡C—, —CONH—, —SO2NH— [sic], and and [sic] R1—X [sic] together are also and R3 [sic] is hydrogen and CO—NR6R7 [sic], R4 [sic] is hydrogen, C1-C4-alkyl [sic], which is branched and unbranched, and —O—C1-C4-alkyl [sic]; R5 [sic] is hydrogen, C1-C4-alkyl [sic], which is branched or unbranched, and —O—C1-C4-alkyl [sic]; R6 [sic] is hydrogen, C1-C6-alkyl, which is branched and unbranched, and R7 [sic] is hydrogen, C1-C6-alkyl, which is branched or unbranched, and n is is [sic] a number 0, 1 or 2.
摘要翻译: 通式I的酰胺及其互变异构体和异构体形式,可能的对映异构体和非对映体形式,以及可能的生理上可耐受的盐,其中变量具有以下含义:R 1 [C 1-6]可以是C 1 -C 6 - 烷基,苯基,萘基 ,喹啉基,吡啶基,嘧啶基,哒嗪基,喹唑啉基和喹喔啉基,其中环可以另外被至多2个基团R 4 [sic]取代,并且R 2是 - (CH 2)m -R 8 [sic],其中R 8 [ ]可以是苯基,环己基或吲哚基并且m = 1至6,X是键,-CH 2 - , - CH 2 CH 2 - , - CH = CH - , - C≡C - , - CONH - , - SO 2 NH- ],并且R 1-X [sic]一起也是且R 3 [sic]是氢且CO-NR 6 R 7 [sic],R 4 [sic]是氢,C 1 -C 4 - 烷基[ 非支链和-O-C 1 -C 4 - 烷基[sic]; R 5 [sic]是氢,C 1 -C 4 - 烷基[sic],其是支链或非支链的,和-O-C 1 -C 4 - 烷基[ R 6是氢,C 1 -C 6 - 烷基,其是支链和非支链的,并且R 7 [sic]是氢,C 1 -C 6 - 烷基,其是支链或 不分支,而且是数字0,1或2。
-
公开(公告)号:US06753327B1
公开(公告)日:2004-06-22
申请号:US09673089
申请日:2000-10-11
IPC分类号: A61K3116
CPC分类号: C07D213/82 , A61K31/195 , A61K31/5375 , C07C229/38 , C07C237/22 , C07C237/32 , C07C2601/14 , C07D295/155
摘要: An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine, morpholine, piperidine, —NR5R6 and and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m, —CH═CH—, —C≡C—, and Y is phenyl, pyridine, pyrimidine and pyrazine and n is a number 0, 1 or 2, and m,q are, independently of one another, a number 0, 1, 2, 3 or 4.
摘要翻译: 式I的酰胺及其互变异构形式,可能的对映异构体和非对映体形式,E和Z形式以及可能的生理学耐受盐,其中变量具有以下含义:A - (CH 2)p R 1,其中R 1 可以是吡咯烷,吗啉,哌啶,-NR 5 R 6和R 5,R 6和R 7可以彼此独立地是氢,C 1 -C 4 - 烷基,CH 2 Ph ,Ph,CH2CH2Ph,苯环可被R 6取代,p可以是1和2,B可以是苯基,吡啶基,嘧啶基和哒嗪基,环也可以是 被至多2个R 8基团取代,并且D可以是键, - (CH 2)m,-CH = CH-,-C = C-,Y是苯基,吡啶,嘧啶和吡嗪,n是0, 1或2,且m,q彼此独立地为0,1,2,3或4。
-
公开(公告)号:US06562827B1
公开(公告)日:2003-05-13
申请号:US09647681
申请日:2000-10-03
IPC分类号: A61K3155
CPC分类号: C07D213/80 , C07D213/82 , C07D295/192 , C07D401/04 , C07D401/14 , C07D405/12
摘要: Heterocyclically substituted amides of the general formula I wherein the variables as defined in the specification are useful in pharmaceuticals for the treatment of diseases in which increased interleuken-1 levels occur.
摘要翻译: 在说明书中定义的变量中的通式I的杂环取代的酰胺可用于治疗发生白介素-1水平升高的疾病的药物。
-
-
-
-
-
-
-
-
-