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1. 发明申请

WO1988003568A1 STEREOSPECIFIC KETO-REDUCTION OF BICYCLOOCTANDIONE-CARBOXYLIC ACID ESTERS BY MICROORGANISMS 审中-公开
标题翻译：通过微生物降解双酚A羧酸酯的立体化学方法
公开(公告)号：WO1988003568A1
公开(公告)日：1988-05-19
申请号：PCT/DE1987000517
申请日：1987-11-12
申请人： SCHERING AKTIENGESELLSCHAFT , PETZOLDT, Karl , DAHL, Helmut , VORBRÜGGEN, Helmut
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C12P41/00
CPC分类号： C07D317/72 , C07C405/0083 , C07D319/08 , C12P7/62 , C12P17/02 , C12P41/002 , Y10S435/911 , Y10S435/921 , Y10S435/939
摘要： Process for the production of 3 alpha -hydroxy-prostacyclin intermediates of formula (+)-I, where A is the residue -CH2- or >CH-COOR, B is oxygen or the double-bond residue -O-X-O- with X as a straight or branched-chain alkylene with 1-7 C atoms and R is a straight or branched-chain alkyl group with 1-6 C atoms or benzyl. The process is characterized in that a racemic bicyclooctandione of formula (+/-)-II, where A, B and R have the above notations, is treated with rhizopus-, rhodotorula- or candida strains, and in the case that the strain used reduces the form (-)- from the racemate (+/-)-II, a chemical or microbiological reduction of the unmodified bicyclooctandion of formula (+)-II follows said treatment.
摘要翻译：制备式（+） - I的3α-羟基 - 前列环素中间体的方法，其中A为残基-CH 2 - 或> CH-COOR，B为氧或双键残基-OXO-，X为具有1-7个C原子的直链或支链亚烷基，R是具有1-6个C原子的直链或支链烷基或苄基。该方法的特征在于式（+/-） - II的外消旋二环辛二酮，其中A，B和R具有上述符号，用根霉，rhodotorula或念珠菌菌株进行处理，并且在使用菌株的情况下根据所述处理，式（+） - II的未修饰双环化合物的化学或微生物学降低可以从外消旋体（+/-） - II中减少形式（ - ）。

2. 发明申请

WO1988003570A1 RACEMIC SEPARATION OF 7'alpha'-ACYLOXY-6'beta'-HYDROXYMETHYL-2-OXABICYCLO[3.3.0]OCTANE-3-ONES BY STEREO-SPECIFIC ENZYMATIC ACYLATE HYDROLYSIS 审中-公开
标题翻译： 7种α-乙酰基-6β-羟基甲基-2-氧杂环戊烯[3.3.0]季铵盐的异构分离通过立体特异性乙酸酯水解
公开(公告)号：WO1988003570A1
公开(公告)日：1988-05-19
申请号：PCT/DE1987000520
申请日：1987-11-12
申请人： SCHERING AKTIENGESELLSCHAFT , PETZOLDT, Karl , DAHL, Helmut
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C12P41/00
CPC分类号： C12P17/02 , C12P41/004
摘要： Process for the manufacture of (-)-oxabicyclo[3.3.0]octanolones of formula (-)-I, where R is hydrogen or the residue (a), in which R1 has the notation of a hydrogen, alkyl with 1-7 C atoms, or phenyl. The process is characterized in that a racemic oxabicyclo[3.3.0]-octanolone-acylate of formula (U)-II, where R1 has the above notation, is subjected to a stereo-specific acylate hydrolysis and the (-)-I (R = (a)) is separated from the saponified (+)-I (R = H) or the saponified (-)-I (R = H) is separated from the unsaponified (+)-II.

3. 发明申请

WO1988003567A1 RACEMIC DISSOCIATION OF 3-ACYLOXILIC-BICYCLO[3.3.0]OCTANE-7-ONE-2-CARBOXYLIC ACID ESTERS BY STEREOSPECIFIC ENZYME OR MICROBIOLOG ICAL ACYLATE HYDROLYSIS 审中-公开
标题翻译： 3-ACYLOXILIC-BICYCLO [3.3.0]季铵化合物的7-二-2-羧酸酯的立体解离通过立体酶或微生物酸性水解
公开(公告)号：WO1988003567A1
公开(公告)日：1988-05-19
申请号：PCT/DE1987000513
申请日：1987-11-12
申请人： SCHERING AKTIENGESELLSCHAFT , PETZOLDT, Karl , DAHL, Helmut , SKUBALLA, Werner
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C12P41/00
CPC分类号： C07D317/72 , C07C405/0083 , C07D319/08 , C12P7/26 , C12P7/42 , C12P7/62 , C12P17/02 , C12P41/004
摘要： Process for the production of optically active (+)-bicyclo[3.3.0]octanol derivatives of formula (+)-I, in which R1 and R2 represent jointly an oxygen atom or the double-bond residue -O-X-O-, with X as a straight or branched-chain alkylene with 1-7 C-atoms, or R1 and R2 represent separately the residue OR5, with R5 as a straight or branched-chain alkyl with 1-7 C-atoms, and R3 the residue COOZ with Z as a hydrogen atom, straight or branched chain alkyl with 1-7 C atoms, cycloalkyl with 3-6 C atoms, phenyl or aralkyl with 7-10 C atoms or R3 is the residue -(CH2)n-O-COR4, with n having the meaning 1-4 and R4 as a straight or branched-chain alkyl with 1-7 C atoms, cycloalkyl with 3-6 C atoms, phenyl or aralkyl with 7-10 C atoms. The process is characterized in that racemic 3 alpha -cyloxy-cis-bicyclo[3.3.0]-octane derivatives of formula (+/-)-II, wherein R1, R2, R3 and R4 have the above meanings, are subjected enzymatically or microbiologically to a stereospecific acylate hydrolysis and the (+)-bicyclo[3.3.0]-octanol derivative produced is separated from the unsaponified bicyclo[3.3.0]-octanol acylate of formula (-)-II or the unsaponified enantiomers (+)-II are separated from the saponified bicyclo[3.3.0]octanol derivative (-)-I and then subjected to chemical acylate hydrolysis.
摘要翻译：制备式（+） - I的光学活性（+） - 双环[3.3.0]辛醇衍生物的方法，其中R 1和R 2共同表示氧原子或双键残基-OXO-，其中X为具有1-7个C原子的直链或支链亚烷基，或R1和R2分别表示残基OR5，R5表示具有1-7个C原子的直链或支链烷基，R3表示残基COOZ与Z 作为氢原子，具有1-7个C原子的直链或支链烷基，具有3-6个C原子的环烷基，具有7-10个C原子的苯基或芳烷基或R3是残基 - （CH 2）n O-COR 4，其中n具有含1-4个碳原子的直链或支链烷基，含3-6个碳原子的环烷基，含有7-10个C原子的苯基或芳烷基。该方法的特征在于其中R1，R2，R3和R4具有上述含义的式（+/-） - II的外消旋3α-甲氧基 - 顺式 - 二环[3.3.0] - 辛烷衍生物经酶促或将微生物学上的立体定向酰化物水解，并将所产生的（+） - 双环[3.3.0] - 辛醇衍生物与式（ - ） - II的未皂化的双环[3.3.0] - 辛醇酰化物或未掺杂的对映异构体（+） -II与皂化的双环[3.3.0]辛醇衍生物（ - ） - I分离，然后进行化学酰化物水解。

4. 发明申请

WO1993007118A1 9-SUBSTITUTED BICYCLO[3.3.0]OCTANE DERIVATIVES, FOR USE AS TXA2 ANTAGONISTS 审中-公开
标题翻译： 9-替代双酚A [3.3.0] OCTANE衍生物，用作TXA2拮抗剂
公开(公告)号：WO1993007118A1
公开(公告)日：1993-04-15
申请号：PCT/DE1992000865
申请日：1992-10-09
申请人： SCHERING AKTIENGESELLSCHAFT , KLAR, Ulrich , VORBRÜGGEN, Helmut , REHWINKEL, Hartmut , THIERAUCH, Karl-Heinz , VERHALLEN, Peter
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C405/00
CPC分类号： C07C405/0083
摘要： The invention concerns 9-substituted bicylo[3.3.0]octane derivaties of formula (I) and their physiologically acceptable bases, and also the α-, β- or η-cyclodextrin clathrates, and the compounds of formula (I) encapsulated in liposomes. The invention also concerns methods of preparing such compounds and their use in pharmaceuticals.

5. 发明申请

WO1993005785A1 COMBINATION PHARMACEUTICAL PREPARATIONS CONTAINING A NON-STEROIDAL ANTI-INFLAMMATORY AGENT AND NOCLOPROST 审中-公开
标题翻译：含有非甾体抗炎药物和药物的组合药物制剂
公开(公告)号：WO1993005785A1
公开(公告)日：1993-04-01
申请号：PCT/EP1992001994
申请日：1992-08-28
申请人： SCHERING AKTIENGESELLSCHAFT , VORBRÜGGEN, Helmut , TÄUBER, Ulrich , TACK, Johannes , AMON, Ingrid , WABNITZ, Rudolf
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： A61K31/557
CPC分类号： A61K31/557 , A61K9/209 , A61K9/5084 , A61K31/60 , A61K31/19 , A61K31/195 , A61K31/405 , A61K2300/00
摘要： Pharmaceutical preparation contain as active substance a combination of a non-steroidal anti-inflammatory agent with nocloprost.

6. 发明申请

WO1988007050A1 NEW PROCESS FOR THE ANTIPODAL SEPARATION OF BICYCLO[3.3.0]OCTANE-3,7-DION-2-CARBOXYLIC ACID ESTERS AND THEIR 7-MONOCETALS 审中-公开
标题翻译：双氰胺[3.3.0]月桂-3,7-二酮-2-羧酸酯及其7-二醇的抗体分离新工艺
公开(公告)号：WO1988007050A1
公开(公告)日：1988-09-22
申请号：PCT/DE1988000149
申请日：1988-03-11
申请人： SCHERING AKTIENGESELLSCHAFT , VORBRÜGGEN, Helmut
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07J01/00
CPC分类号： C07J1/0074
摘要： Process for the production of (+)-bicyclo-[3.3.0]octane-3-on-2-carboxylic acid steroid esters having the formula (I), in which X represents oxygen or the -O-(CH2)n-O- or the -O-CH2-C(CH3)2-CH2-O- residue; n represents 2 or 3; R2 represents hydrogen or methyl; Y represents the X or X1 residues; X1 represents the OCH3 or OCOR3 residues; and R3 represents methyl, ethyl, phenyl, benzyl or pivalyl.
摘要翻译：制备具有式（I）的（+） - 双环 - [3.3.0]辛烷-3-对2-羧酸类固醇酯的方法，其中X表示氧或-O-（CH 2）n O- 或-O-CH 2 -C（CH 3）2 -CH 2 -O-残基; n表示2或3; R2代表氢或甲基; Y表示X或X 1残基; X1表示OCH3或OCOR3残基; 并且R 3表示甲基，乙基，苯基，苄基或新戊酰基。

7. 发明申请

WO1983003248A1 CARBACYCLINE, PREPARATION AND UTILIZATION THEREOF 审中-公开
标题翻译：卡巴肼，其制备和利用
公开(公告)号：WO1983003248A1
公开(公告)日：1983-09-29
申请号：PCT/DE1983000045
申请日：1983-03-11
申请人： SCHERING AKTIENGESELLSCHAFT , VORBRÜGGEN, Helmut , RADÜCHEL, Bernd , SKUBALLA, Werner , SCHWARZ, Norbert , CASALS-STENZEL, Jorge , MANNESMANN, Gerda , TOWN, Michael-Harold
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C177/00
CPC分类号： C07D317/72 , C07C45/59 , C07C57/26 , C07C57/60 , C07C405/0083 , C07D263/14 , C07F9/4018 , C07C49/743
摘要： Carbacycline derivatives having the formula I wherein R1 is the residue CH2OH or -C-OR2, R2 representing a hydrogen atom, an alkyl, cycloalkyl, aryl, CH2 -C-aryl residue or a heterocyclic residue, or R1 is the residue -C-NHR3, R3 representing an alkanoyl or alkanesulfonyl residue containing each 1 to 10 atoms of carbon or the residue R2 or R1 is the residue wherein m is 1 or 2. X is an oxygen atom or CH2 group, A is a trans -CH=CH- or -C=C- group, W is a free or modified hydrocymethylene group wherein the OH group may be in the position alpha or beta , n represents the integer 1, 2 or 3, D is a straight chain alkylene group with 1 to 3 atoms of carbon, E represents a -C=C- bond or a -CR6=CR7 group, R6 and R7 being different and representing a hydrogen atom or an alkyl group with 1 to 5 atoms of carbon or a hydrogen atom or an a halogen atom, preferably chlorine, R4 represents an alkyl, cycloalkyl group or an optionally substituted aryl group or a heterocyclic group, R5 represents a free or modified hydroxy group. When R2 represents a hydrogen atom, the salts of compounds with pharmaceutically acceptable bases are also involved. The compounds are used as hypotensive agents.
摘要翻译：具有式I的卡巴环素衍生物，其中R 1是残基CH 2 OH或-CON OR 2，R 2表示氢原子，烷基，环烷基，芳基，CH 2 -C芳基或杂环残基，或R 1 是残基，如表示含有1-10个碳原子的链烷酰基或烷磺酰基残基，R 2或R 1为残基，其中m为1或2.X为氧原子或CH 2基团，A是反式-CH = CH-或-C = C-基团，W是游离或修饰的水合甲基基团，其中OH基团可以在α或β位置，n表示整数1,2或 3，D是具有1至3个碳原子的直链亚烷基，E表示-C = C-键或-CR 6 = CR 7基团，R 6和R 7不同，表示氢原子或具有1个至5原子的碳或氢原子或卤素原子，优选氯，R4表示烷基，环烷基或任选取代的芳基或杂环酰基，R5表示游离或改性的羟基。当R 2表示氢原子时，也涉及具有药学上可接受的碱的化合物的盐。这些化合物用作降压剂。

8. 发明申请

WO1988007037A1 6-OXOPROSTAGLANDIN-E DERIVATIVES, PROCESS FOR THEIR PRODUCTION AND THEIR PHARMACEUTICAL APPLICATION 审中-公开
标题翻译： 6-OXOPROSTAGLANDIN-E衍生物，其生产方法及其药物应用
公开(公告)号：WO1988007037A1
公开(公告)日：1988-09-22
申请号：PCT/DE1988000151
申请日：1988-03-11
申请人： SCHERING AKTIENGESELLSCHAFT , KLAR, Ulrich , SKUBALLA, Werner , VORBRÜGGEN, Helmut , STÜRZEBECHER, Claus-Steffen , THIERAUCH, Karl-Heinz , SCHILLINGER, Ekkehard
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C177/00
CPC分类号： C07C405/00
摘要： 6-Oxoprostaglandin-E, derivatives having the formula (I), in which R signifies the residue COOR where R signifies a hydrogen atom, a C1-10 alkyl, a C5-6 cycloalkyl, a C6-C10 aryl group, a heterocyclic residue or the residue CONHSO2R where R signifies a C1-10 alkyl, C5-6 cycloalkyl or C6-10 aryl; A signifies a CH=CH or a -C=C- group in an E configuration; W signifies a free or functionally modified hydroxymethylene group or a free or functionally modified group having the formula (II), in which the group OH may be either alpha - or beta - permanent; D signifies a straight-chain or branched-chain alkylene group with between 1 and 5 C atoms; E signifies a -C=C- group or a C2-C4 alkenyl group; R signifies a C1-C10 alkyl group, a C3-C10 cycloalkyl group or a C6-C10 aryl -C=C- group which may have been substituted, or a heterocyclic group; R signifies a free or functionally modified hydroxy and R and, where R signifies a hydrogen atom, the salts of said group with physiologically compatible bases; also the alpha -, beta - or gamma - cyclodextrinclothrate of the compounds having the formula (I). Process for their production and their pharmaceutical application.
摘要翻译： 6-氧前列腺素E，具有式（I）的衍生物，其中R 1表示残基COOR 2，其中R 2表示氢原子，C1-10烷基，C5-6环烷基， C 6 -C 10芳基，杂环残基或残基CONHSO 2 R 5，其中R 5表示C1-10烷基，C5-6环烷基或C6-10芳基; A表示E配置中的CH = CH或-C = C-基团; W表示游离或官能改性的羟基亚甲基或具有式（II）的游离或官能改性基团，其中基团OH可以是α-或β-永久的; D表示具有1至5个C原子的直链或支链亚烷基; E表示-C = C-基或C 2 -C 4烯基; R 3表示可以被取代的C1-C10烷基，C3-C10环烷基或C6-C10芳基-C = C-基或杂环基; R 4表示游离或官能改性的羟基和R 4，并且其中R 2表示氢原子，所述基团的盐与生理上相容的碱基相同; 还有具有式（I）的化合物的α，β或γ-环糊精碱。生产过程及其药物应用。

9. 发明申请

WO1985002187A1 20-ALKYL-7-OXOPROSTACYCLINE DERIVATIVES AND PRODUCTION PROCESS THEREOF 审中-公开
标题翻译： 20-烷基-7-氧代环糊精衍生物及其生产方法
公开(公告)号：WO1985002187A1
公开(公告)日：1985-05-23
申请号：PCT/DE1984000238
申请日：1984-11-08
申请人： SCHERING AKTIENGESELLSCHAFT , NICKOLSON, Robert , VORBRÜGGEN, Helmut , STÜRZEBECHER, Claus - Steffen , HABEREY, Martin
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07D307/935
CPC分类号： C07D307/935 , C07C405/00 , C07D307/937
摘要： 20-alkyl-7-oxoprostacycline derivatives having the general formula (I) wherein R1 is either the rest OR3, R3 representing hydrogen or alkyl comprising from 1 to 10 atoms of carbon optionally substituted by halogen, phenyl, alkoxy having from 1 to 4 atoms of carbon or dialkylamino having from 1 to 4 atoms of carbon, cycloalkyl, aryl or a heterocyclic rest, or the rest NHR4, R4 representing hydrogen or an alkanoyl or alkansulphonyl rest having from 1 to 10 atoms of carbon; n is 1 or 2; A is a group-CH2-CH2-, cis -CH=CH- or trans -CH=CH-; W is a groupe (II) or (III) wherein the group OH may be esterified with benzoyl or alkane acid rest having from 1 to 4 atoms of carbon or etherified with a tetrahydropyranol-, tetrahydrofuranyl-, alkoxyalkyl-, or trialkylsilyle rest, the free or esterified OH group being in the alpha or beta position; R2 is a straight or branched chain alkyl comprising from 1 to 6 atoms of carbon; R5 is a hydroxy group esterified with an alkane acid rest having from 1 to 4 atoms of carbon or etherified with tetrahydropyranyl-, tetrahydrofuranyl-, alkoxy alkyl- or trialkylsilyle rest; R6 and R7 are hydrogen or a straight or branched chain alkyl having from 1 to 4 atoms of carbon or R6 and R7 form together a trimethylene radical, R8 and R9 form together a bound, hydrogen or a straight or branched chain alkyl having from 1 to 4 atoms of carbon and if R3 is hydrogen, the salts thereof with physiologically compatible bases; production thereof and utilization thereof as medicine.

10. 发明申请

WO1985000367A1 11-HALOGENE-PROSTANE DERIVATIVES, PROCESS FOR OBTAINING THEM AND UTILIZATION THEREOF AS DRUGS 审中-公开
标题翻译： 11-卤代 - 衍生物衍生物，用于获得它们的方法和作为药物的利用
公开(公告)号：WO1985000367A1
公开(公告)日：1985-01-31
申请号：PCT/DE1984000139
申请日：1984-07-05
申请人： SCHERING AKTIENGESELLSCHAFT , VORBRÜGGEN, Helmut , SCHWARZ, Norbert , LOGE, Olaf , STÜRZEBECHER, Claus-Steffen , ELGER, Walter
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C177/00
CPC分类号： C07C405/0016 , C07C405/00 , C07C405/0041 , C07D317/20
摘要： 11-halogene-prostane derivatives of the general formula (I), wherein X is F, Cl or Br; R1 is CH2OH or (II) wherein R2 is a hydrogen atom, a rest of alkyl, cycloalkyl, aryl, phenacyl or heterocyclic rest; A is a group -CH2-CH2- or cis -CH=CH-; B is a group -CH2-CH2-, or trans -CH=CH- or -C=C-; W is an ethylenedioxymethylene group or a hydroxymethylene group; D and E form together a direct bound or D is C1-10-alkylene group and E an oxygen atom or a sulphur atom, a direct bound, -C=C- bound or -CR6=CR7- group wherein R6 and R7 are a hydrogen atom, a chlorane atom or an alkyl group; R4 is a hydroxy group; R5 represents an hydrogen atom, an alkyl, cycloalkyl, aryle or heterocyclic group and the salts thereof with physiologically acceptable bases, method for the preparation thereof and utilization thereof as inhibitors of the secretion of gastric juice.
摘要翻译：通式（I）的11-卤代 - 前列腺衍生物，其中X为F，Cl或Br; R 1为CH 2 OH或（II）其中R 2为氢原子，其余为烷基，环烷基，芳基，苯甲酰基或杂环基; A是基团-CH 2 -CH 2 - 或顺式-CH = CH-; B是基团-CH 2 -CH 2 - 或反-CH = CH-或-C = C-; W是亚乙基二氧基亚甲基或羟基亚甲基; D和E一起形成直接结合或D为C 1-10 - 亚烷基，E为氧原子或硫原子，直接结合，-C = C-结合或-CR 6 = CR 7 - 基，其中R 6和R 7为氢原子，氯原子或烷基; R4是羟基; R5表示氢原子，烷基，环烷基，芳基或杂环基，其盐与生理上可接受的碱，其制备方法和作为胃液分泌抑制剂的应用。

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