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1. 发明授权

US5359074A Process for the preparation of racemic and optically active 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid and its precursors 失效
公开(公告)号：US5359074A
公开(公告)日：1994-10-25
申请号：US76772
申请日：1993-06-15
申请人： Bernhard Kammermeier , Ulrich Lerch
发明人： Bernhard Kammermeier , Ulrich Lerch
IPC分类号： C07D217/26 , C07D217/20 , A61K31/47 , C07D217/18
CPC分类号： C07D217/26
摘要： A process for the preparation of racemic and optically active 1,2.3,4-tetrahydroisoquinoline-3-carboxylic acid is described, in which dihalo-o-xylylenes are cyclized to dicarboxylic acid esters in basic medium using dialkyl N-acylamidomalonates of the formula (CO.sub.2 R.sup.1).sub.2 CHNHCOR.sup.2, in which R.sup.1 is (C.sub.1 -C.sub.4)-alkyl and R.sup.2 is H, (C.sub.1 -C.sub.4)-alkyl or (C.sub.6 -C.sub.12)-aryl, decarboxylated by basic hydrolysis and subsequent acid work-up and then reacted in acid medium to give (D,L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, or dihalo-o-xylylenes are cyclized in basic medium to give the dicarboxylic acid esters and these are reacted directly without isolation in a one-pot process to give (D,L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, if desired the racemic 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid is reacted with (-)menthol and p-toluenesulfonic acid to give (-)menthyl (D)- or (L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate, then the diastereomers are separated by column chromatography and subjected to basic hydrolysis to give (D)-or (L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, or (D,L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid is esterified by means of benzyl alcohol and p-toluenesulfonic acid, reacted with D(-)mandelic acid to give benzyl (D)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate (D)-mandelate and benzyl (L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate (D)-mandelate or with L(+)mandelic acid to give benzyl (D)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate (L)-mandelate and benzyl (L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate (L)-mandelate and then the compounds obtained are separated into the optical antipodes by fractional crystallization in an inert solvent and the enantiomers (D)- or (L)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid are liberated by basic hydrolysis, the chiral auxiliary reagent being recovered.

2. 发明授权

US4296121A Novel prostaglandin derivatives of the .DELTA.2-PGF.sub.2 and .DELTA.2-PGE.sub.2 series and process for their manufacture 失效
标题翻译： DELTA 2-PGF2和DELTA 2-PGE2系列的新型前列腺素衍生物及其制造方法
公开(公告)号：US4296121A
公开(公告)日：1981-10-20
申请号：US62937
申请日：1979-08-02
申请人： Wilhelm Bartmann , Gerhard Beck , Ulrich Lerch , Elmar Konz
发明人： Wilhelm Bartmann , Gerhard Beck , Ulrich Lerch , Elmar Konz
IPC分类号： A61K31/23 , A61K31/19 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61P43/00 , C07C45/29 , C07C45/60 , C07C47/267 , C07C49/743 , C07C49/757 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/34 , C07D307/58 , C07D307/935 , C07D319/06 , C07D333/16 , C07D333/24 , A61K31/557 , C07C177/00 , C07D307/54
CPC分类号： C07D307/935 , C07C405/00 , C07C45/29 , C07C45/60 , C07C47/267 , C07C49/743 , C07C49/757 , C07D319/06 , Y10S514/822
摘要： What is disclosed are compounds of the formula ##STR1## which are structurally related to natural prostaglandins and a process for their manufacture. The compounds have valuable pharamacological properties and, therefore, they can be used as medicaments.
摘要翻译：公开的是具有结构上与天然前列腺素相关的式（I）＆gt; I的化合物及其制造方法。这些化合物具有宝贵的药理学性质，因此它们可以用作药物。

3. 发明授权

US4198429A Esters of 5-methyl-10,11-dihydroprostaglandin-A.sub.1 失效
标题翻译： 5-甲基-10,11-二氢前列腺素-A1的酯
公开(公告)号：US4198429A
公开(公告)日：1980-04-15
申请号：US809432
申请日：1977-06-23
申请人： Wilhelm Bartmann , Gerhard Beck , Ulrich Lerch , Bernward Scholkens
发明人： Wilhelm Bartmann , Gerhard Beck , Ulrich Lerch , Bernward Scholkens
IPC分类号： A61K31/215 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C07C177/00
CPC分类号： C07C405/00
摘要： Prostaglandin esters of the formula ##STR1## have valuable therapeutical properties.
摘要翻译：式“IMAGE”的前列腺素酯具有有价值的治疗特性。

4. 发明授权

US4078081A Cyclopentane derivatives manufacture 失效
标题翻译：环戊烷衍生物制造
公开(公告)号：US4078081A
公开(公告)日：1978-03-07
申请号：US582927
申请日：1975-06-02
申请人： Ulrich Lerch , Milos Babej , Wilhelm Bartmann , Rudolf Kunstmann
发明人： Ulrich Lerch , Milos Babej , Wilhelm Bartmann , Rudolf Kunstmann
IPC分类号： A61K31/21 , C07C67/00 , C07C401/00 , C07C405/00 , C07C177/00 , A61K31/19 , A61K31/215
CPC分类号： C07C405/00
摘要： The present invention relates to new cyclopentane derivatives having the formula ##STR1## and to a process for their manufacture. The compounds can be used as medicaments due to their antiprostaglandin effect.
摘要翻译：本发明涉及具有式“IMAGE”I的新环戊烷衍生物及其制备方法。这些化合物由于其抗前列腺素的作用可用作药物。

5. 发明授权

US5321139A Process for the enantioselective synthesis of 2(R)-benzylsuccinic acid monoamide derivatives 失效
标题翻译： 2（R） - 苄基琥珀酸单酰胺衍生物的对映选择性合成方法
公开(公告)号：US5321139A
公开(公告)日：1994-06-14
申请号：US22887
申请日：1993-02-16
申请人： Ulrich Lerch , Heiner Jendralla , Bernhard Seuring , Rainer Henning
发明人： Ulrich Lerch , Heiner Jendralla , Bernhard Seuring , Rainer Henning
IPC分类号： B01J31/24 , C07B61/00 , C07C231/02 , C07C231/18 , C07C233/14 , C07C233/22 , C07C233/40 , C07D211/44 , C07D211/58 , C07D241/04 , C07F9/572 , C07F15/00 , C07D211/06
CPC分类号： C07F15/0013 , C07C231/18 , C07D211/58 , C07F15/008 , C07F9/5726
摘要： Two processes are described for the preparation of the optically pure compounds of formula 1: ##STR1## in which R.sup.1 and R.sup.2 are e.g. alkyl, R.sup.3 and R.sup.4 are e.g. hydrogen and R.sup.5 is e.g. hydrogen. Both processes include, as key steps, the enantioselective hydrogenation of a C.dbd.C double bond and the regioselective formation of a dicarboxylic acid monoamide derivative. In one process a phenylitaconic acid derivative is asymmetrically hydrogenated to give an optically active (R)-benzylsuccinic acid which is then converted to a diester, said diester being converted to the monoamide compound of formula 1. In the second process, a phenylitaconic acid derivative is converted to its anhydride, and the anhydride is then converted to a monoamide which is then asymmetrically hydrogenated to give the compound of formula 1.
摘要翻译：描述了制备光学纯的式1化合物的两种方法：其中R 1和R 2是例如：烷基，R 3和R 4是例如。氢和R 5是例如。氢。作为关键步骤，两种方法都包括C = C双键的对映选择性氢化和二羧酸单酰胺衍生物的区域选择性形成。在一个过程中，苯基衣康酸衍生物被不对称氢化，得到光学活性（R） - 苄基琥珀酸，然后将其转化为二酯，所述二酯转化成式1的单酰胺化合物。在第二种方法中，苯基衣康酸衍生物转化成其酐，然后将酸酐转化为单酰胺，然后将其不对称氢化，得到式1的化合物。

6. 发明授权

US4882329A Alkoxyphenylindolinone derivatives, medicaments containing them and their use 失效
标题翻译：烷氧基吲哚啉酮衍生物，含有它们的药物及其用途
公开(公告)号：US4882329A
公开(公告)日：1989-11-21
申请号：US303996
申请日：1989-01-30
申请人： Ulrich Lerch , Rainer Henning , Joachim Kaiser
发明人： Ulrich Lerch , Rainer Henning , Joachim Kaiser
IPC分类号： C07D401/14 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/4427 , A61K31/445 , A61K31/495 , A61P3/00 , A61P3/14 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , C07D209/34 , C07D401/12
CPC分类号： C07D401/12 , C07D209/34
摘要： Calcium antagonists of the formula ##STR1## with R(1), R(2), R(3) and R(4) being, inter alia, H, alkyl, alkoxy, halogen, in some cases phenyl; m being 1-4; n being 0-3; X being CH.sub.2, O, S, CO, CHOH or CR.sub.2, and R(5) being various groups containing nitrogen atoms, are described.They are obtained by reaction of compounds II which are likewise new and which contain in place of R(5) a leaving group Y (Cl, Br, I) with the appropriate (cyclic) amino compound.Another synthesis comprises reaction of the appropriate indolinone derivative IV which has a non-etherified hydroxyl group with a side chain which contains a terminal leaving group Z (Cl, Br, I) in the presence of a base.Furthermore, indolinone derivatives VI with an ether side chain with a terminal epoxide group can be reacted with (cyclic) amines to give compounds I.
摘要翻译：具有R（1），R（2），R（3）和R（4）的式（I）的化合物拮抗剂尤其是H，烷基，烷氧基，卤素，在一些情况下为苯基; m为1-4; n为0-3; X是CH 2，O，S，CO，CHOH或CR 2，R（5）是含有氮原子的各种基团。它们通过同样新的且含有代替R（5）离去基团Y（Cl，Br，I）的化合物II与适当的（环状）氨基化合物反应而获得。另一种合成方法包括在碱存在下，具有非醚化羟基的合适的吲哚啉酮衍生物IV与含有末端离去基团Z（Cl，Br，I）的侧链的反应。此外，具有末端环氧基团的醚侧链的二氢吲哚衍生物VI可以与（环状）胺反应，得到化合物I.

7. 发明授权

US4659838A Method of resolving bicyclic imino-.alpha.-carboxylic acid ester racemates 失效
标题翻译：二环亚氨基-α-羧酸酯外消旋体的拆分方法
公开(公告)号：US4659838A
公开(公告)日：1987-04-21
申请号：US681329
申请日：1984-12-13
申请人： Ulrich Lerch
发明人： Ulrich Lerch
IPC分类号： C07B57/00 , C07B31/00 , C07C67/00 , C07D209/02 , C07D209/42 , C07D209/44 , C07D209/52 , C07D209/12
CPC分类号： C07D209/52
摘要： The invention relates to a process for resolving racemic mixtures of bicyclic imino-.alpha.-carboxylic acid esters into the components of the formula Ia and Ib ##STR1## in which R.sup.1 stands for an aliphatic, cycloaliphatic, aromatic or araliphatic radical,A denotes hydrogen and B and C together form a carbon chain or C denotes hydrogen and A and B together form a carbon chain, by crystallizing diastereoisomeric salts, which comprises preparing the salts of the racemic esters with optically active O,O-diacyltartaric acids in a suitable solvent in which only one of the two diastereoisomeric salts crystallizes in optically pure form, if desired purifying the diastereoisomeric salt by recrystallization, reprecipitation or trituration, and finally adding basec to the salt to cleave it into the pure enantiomer of the formula Ia or Ib.The invention also relates to diastereoisomeric salts of an ester of the formula Ia or Ib and a diacyltartaric acid.
摘要翻译：本发明涉及一种将双环亚氨基-α-羧酸酯的外消旋混合物分解成式Ia和Ib的组分的方法，其中R1代表脂族，脂环族，芳族或芳脂族基团，A表示氢和 B和C一起形成碳链或C表示氢，A和B一起形成碳链，通过结晶非对映异构体盐，其包括在合适的溶剂中制备外消旋酯与光学活性O，O-二酰基酒石酸的盐如果需要，通过重结晶，再沉淀或研磨纯化非对映异构体盐，最后加入碱以将其切割成式Ia或Ib的纯对映体，两种非对映异构体盐中只有一种以光学纯的形式结晶。本发明还涉及式Ia或Ib的酯和二酰基酒石酸的非对映异构体盐。

8. 发明授权

US4595685A Benzothiazine derivatives 失效
标题翻译：苯并噻嗪衍生物
公开(公告)号：US4595685A
公开(公告)日：1986-06-17
申请号：US684711
申请日：1984-12-21
申请人： Rainer Henning , Ulrich Lerch , Joachim Kaiser
发明人： Rainer Henning , Ulrich Lerch , Joachim Kaiser
IPC分类号： A61K31/54 , A61K31/5415 , A61P3/00 , A61P9/00 , C07D279/16 , C07D317/00 , C07D417/04 , C07D417/12 , C07D279/10
CPC分类号： C07D417/04 , C07D279/16 , C07D417/12
摘要： Benzothiazine derivatives of the formula I ##STR1## with (R(1), R(1)', R(1)", R(4) and R(4)' equal to hydrogen, alkyl, alkoxy, halogen, nitro, hydroxyl, acetamido or amino; R(2) equal to hydrogen, alkyl, alkenyl, phenyl; R(3) equal to hydrogen, alkyl, alkenyl, phenyl; R(5) equal to hydrogen or (C.sub.1 -C.sub.3)-alkyl; R(6) equal to one of the following groups, ##STR2## with R(7) and R(8) equal to hydrogen, alkyl, cycloalkyl, phenyl; R(9) equal to hydrogen, alkyl, phenyl, pyridyl, pyrimidinyl or benzoyl; R(10) equal to hydrogen, alkyl, phenyl; R(11) equal to hydrogen, hydroxyl, alkoxy or, together with R(12), a bond; and R(12) equal to hydrogen or, together with R(11), a bond; m equal to 1, 2, 3 or 4; n equal to 0 or 1; p equal to 0, 1, 2, 3 or 4, and X equal to oxygen or two hydrogen atoms, and salts of the compounds of the formula I with physiologically tolerated acids and a process for the preparation of compounds I, likewise a method of treatment of disturbances of the calcium balance of a human body are described.
摘要翻译：式（I）与（R（1），R（1）'，R（1）“，R（4）和R（4）'等于氢，烷基，烷氧基，卤素，硝基，羟基，乙酰氨基或氨基; R（2）等于氢，烷基，烯基，苯基; R（3）等于氢，烷基，链烯基，苯基; R（5）等于氢或（C1-C3 ） - 烷基; R（6）等于以下基团之一，其中R（7）和R（8）等于氢，烷基，环烷基，苯基; R（9）等于氢，烷基，苯基，吡啶基，嘧啶基或苯甲酰基; R（10）等于氢，烷基，苯基; R（11）等于氢，羟基，烷氧基或与R（12）等于氢或与R（11）一起键; m等于1,2,3或4; n等于0或1; p等于0,1,2,3或4，X等于氧或两个氢原子，以及式I化合物与生理学上可耐受的酸的盐以及制备化合物I的方法，同样是治疗钙粘蛋白紊乱的方法描述一个人的身体。

9. 发明授权

US4174458A Novel analogues of prostanoic acids not occurring in nature 失效
标题翻译：自然界中不存在的前列腺酸的新型类似物
公开(公告)号：US4174458A
公开(公告)日：1979-11-13
申请号：US902404
申请日：1978-05-03
申请人： Milos Babej , Wilhelm Bartmann , Gerhard Beck , Ulrich Lerch
发明人： Milos Babej , Wilhelm Bartmann , Gerhard Beck , Ulrich Lerch
IPC分类号： C07C405/00 , C07C177/00
CPC分类号： C07C405/00
摘要： The present invention relates to novel not naturally occurring analogues of prostanoic acids of the formula ##STR1## as well as a process for their preparation. The compounds of the invention have valuable pharmacological properties similar to those of the natural prostaglandins and therefore can be used as medicaments.
摘要翻译：本发明涉及式（I）的前列腺酸的新型非天然存在的类似物以及它们的制备方法。本发明的化合物具有与天然前列腺素类似的有价值的药理学性质，因此可用作药物。

10. 发明授权

US4024181A Analogues of prostanoic acids 失效
标题翻译：前列腺酸的类似物
公开(公告)号：US4024181A
公开(公告)日：1977-05-17
申请号：US525174
申请日：1974-11-19
申请人： Milos Babej , Wilhelm Bartmann , Gerhard Beck , Ulrich Lerch
发明人： Milos Babej , Wilhelm Bartmann , Gerhard Beck , Ulrich Lerch
IPC分类号： C07D319/08 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/935 , C07D339/06 , C07D493/08 , C07C177/00
CPC分类号： C07C405/00 , C07D339/06 , Y10S514/826 , Y10S514/869
摘要： The present invention relates to novel not naturally occuring analogues of prostanoic acids of the formula ##STR1## as well as a process for their preparation. The compounds of the invention have valuable pharmacological properties similar to those of the natural prostaglandins and therefore can be used as medicaments.
摘要翻译：本发明涉及式（I）的前列腺酸的新的非天然存在的类似物以及它们的制备方法。本发明的化合物具有与天然前列腺素类似的有价值的药理学性质，因此可用作药物。

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