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1. 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.

2. 发明申请

WO1984004307A1 5-ETHYNYL-PROSTACYCLYNE, PRODUCTION PROCESS THEREOF AND PHARMACEUTICAL UTILISATION THEREOF 审中-公开
标题翻译： 5-乙酰基 - 鸟苷酸，其生产工艺及其药物利用
公开(公告)号：WO1984004307A1
公开(公告)日：1984-11-08
申请号：PCT/DE1984000094
申请日：1984-04-17
申请人： SCHERING AKTIENGESELLSCHAFT , VORBRÜGGEN, Helmut , RADÜCHEL, Bernd , SKUBALLA, Werner , STÜRZEBECHER, Claus-Steffen , HABEREY, Martin
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07D307/935
CPC分类号： C07D307/937
摘要： Derivatives of 5-ethynyl-prostacyclyne having the formula (I) wherein R1 is hydrogen, alkyl, cycloalkyl, aryl, a heterocyclic rest or a group$(4,)$, R2 is a hydrogen atom in position alpha or beta or a methyl group in alpha or beta, R3 is an alkyl, cycloalkyl or aryl group optionally substituted, or a heterocyclic group, A is -CH2-CH2-, trans-CH=CH- or -C=C-group, B is a straight chain alkylen group comprising from 1 to 5 atoms of carbon, D and E form together a direct bond or D is a straight chain saturated alkylene group comprising from 1 to 5 atoms of carbon, a branched chain saturated alkylene group or an unsaturated straight chain alkylene group comprising from 2 to 5 atoms of carbon which may optionally be substituted by fluorine atoms, I is an oxygen atom, -C=C-group or CR5-group, wherein R4 and R5 are different from each other, may represent a hydrogen atom or an alkyl group comprising from 1 to 3 atoms of carbon and, if R1 is a hydrogen atom, they represent physiologically acceptable salts of said compounds with organic or inorganic bases; production process and pharmaceutical utilisation thereof.

3. 发明申请

WO1983001951A1 NEW PROSTACYCLINS AND PREPARATION METHOD THEREOF 审中-公开
标题翻译：新的前体化合物及其制备方法
公开(公告)号：WO1983001951A1
公开(公告)日：1983-06-09
申请号：PCT/DE1982000222
申请日：1982-11-25
申请人： SCHERING AKTIENGESELLSCHAFT , NICKOLSON, Robert , VORBRÜGGEN, Helmut , CASALS-STENZEL, Jorge , HABEREY, Martin
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07D307/935
CPC分类号： C07D307/935 , C07C51/09 , C07C51/38 , C07C55/32 , C07C57/52 , C07C405/00 , C07C405/0033 , C07D307/937 , C07D407/12 , C07F7/1804 , C07F9/4015
摘要： Prostacyclin derivatives having the general formula I wherein R1 is either the OR3 rest, wherein R3 may be hydrogen or an alkyl group with 1 to 10 atoms of carbon and optionally substituted by halogen, aryl, C1-C4-alkoxy or C1-C4-dialkyl-amino, a cyclo-alkyl group, an aryl group or an heterocyclic group, or the rest NHR4, wherein R4 may be hydrogen, an alkanoyl or alkane-sulfonyl group with 1 to 10 atoms of carbon, A represents either -CH2-CH2- , or -CH=CH- (trans), W represents either wherein the group OH is either esterified with a benzoyl rest or an alkanoyl rest having 1 to 4 atoms of carbon, or is etherified with a tetra-hydro-pyranyl, tetra-hydro-furanyl, alkoxy-alkyl (1 to 4 atoms of carbon) or tri-(C1 to C4-alkyl)-silyl rest, the free or esterified OH group being in the position alpha or beta ; the symbols D and E representing in common a direct bond or the symbol D representing itself an alkyl group in a straight or branched chain with 1 to 5 atoms of carbon and the symbol E representing an oxygen atom or a direct bond, the symbol R2 represents an alkyl group with a straight or branched chain having 1 to 6 atoms of carbon, an alkenyl group with a straight or branched chain having 2 to 6 atoms of carbon, group which may be substituted by phenyl, halogen or alkyl with 1 to 4 atoms of carbon or then, when the symbols D and E designate a direct bond, an alkinyl group with 2 to 6 atoms of carbon, optionally substituted in position 1 by halogen or alkyl with 1 to 4 atoms of carbon, the symbol R5 represents a hydroxy group which may be either esterified by an alkanoyl rest having 1 to 4 atoms of carbon, or etherified by a tetra-hydro-pyranyl, tetra-hydro-furanyl, alkoxy-alkyl or tri-alkyl-silyl rest and, providing that R3 is hydrogen, the salts of such derivatives with physiologically acceptable bases. Said compounds are characterized by a hypotensive activity and an inhibiting activity of thrombocyte aggregation. The invention also relates to preparation processes of such compounds.
摘要翻译：具有通式I的前列环素衍生物，其中R 1为OR 3残基，其中R 3可为氢或具有1至10个碳原子并且任选被卤素，芳基，C 1 -C 4烷氧基或C 1 -C 4烷氧基取代的烷基， C4-二烷基 - 氨基，环烷基，芳基或杂环基，或其余NHR4，其中R4可以是氢，具有1-10个碳原子的烷酰基或烷 - 磺酰基，A代表 - CH 2 -CH 2 - 或-CH = CH-（反式），W表示其中基团OH用苯甲酰基取代基或具有1-4个碳原子的烷酰基取代基进行酯化，或者与四 - 氢 - 吡喃基，四氢呋喃基，烷氧基 - 烷基（1至4个碳原子）或三 - （C1至C4烷基） - 甲硅烷基，游离或酯化的OH基位于α或β位置; 符号D和E表示直接键合的符号D或符号D表示其具有1至5个碳原子的直链或支链中的烷基，符号E表示氧原子或直接键，符号R2表示具有1至6个碳原子的直链或支链的烷基，具有2至6个碳原子的直链或支链的烯基，可被苯基取代的基团，卤素或具有1至4个原子的烷基的碳，或者当符号D和E表示直接键时，具有2至6个碳原子的炔基，任选在1位被卤素取代或具有1至4个碳原子的烷基，符号R5表示羟基基团可以被具有1-4个碳原子的烷酰基基团酯化，或者被四氢吡喃基，四氢呋喃基，烷氧基 - 烷基或三烷基 - 甲硅烷基取代的醚化，并且R 3是氢，这些衍生物的盐与生理学可接受的基础。所述化合物的特征在于血小板聚集的低血压活性和抑制活性。本发明还涉及这些化合物的制备方法。

4. 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。

5. 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。

6. 发明申请

WO1987005900A1 7-OXOPROSTACYCLINE DERIVATIVES AND PROCESS FOR THEIR MANUFACTURE 审中-公开
标题翻译： 7-氧羰基胆碱衍生物及其制备方法
公开(公告)号：WO1987005900A1
公开(公告)日：1987-10-08
申请号：PCT/DE1987000132
申请日：1987-03-25
申请人： MAAS, Sybille (heiress of MASS, Manfred ... , SCHERING AKTIENGESELLSCHAFT , VORBRÜGGEN, Helmut , STÜRZEBECHER, Claus-Steffen
发明人： MAAS, Sybille (heiress of MASS, Manfred ... , SCHERING AKTIENGESELLSCHAFT , MAAS, Manfred (deceased)
IPC分类号： C07D307/935
CPC分类号： C07D307/937
摘要： 7-oxoprostacyline derivatives of Formula (I) wherein R1 is the residue OR3, in which R3 can be hydrogen or possibly alkyl substituted by halogen, phenyl, C1-C4-alkoxy or C1-C4-dialkylamino with 1-10 C atoms, or the residue NHR4 in the form of an alkanoyl or alkane sulphonyl residue each with 1-10 C atoms; W is a hydroxy methylene or a group (II), in which the OH group may be esterified with a benzoyl or alkane acid residue with 1-4 C atoms or etherified with a tetrahydropyranyl, tetrahydrofuranyl, (C1-C4 alkoxy)-C1-C4-alkyl or tri-(C1-C4-alkyl)-sylyl residue, whereby the free OH-group can be in the alpha or beta position; D is a straight-chain or branched alkylene group with 1-5 C atoms; R2 is a straight-chain or branched alkyl group with 1-6 C atoms; R5 is a hydroxygroup, which can be esterified with an alkane acid residue with 1-4 C atoms or etherified with a tetrahydropyranyl, tetrahydrofuranyl, (C1-C4-alkoxy)-C1-C4-alkyl or tri(C1-C4-alkyl) residue; X is an oxygen atom or the -CH2- residue and, if R3 is hydrogen, their salts with physiologically compatible bases, process for their production and their use as medicaments.
摘要翻译：式（I）的7-氧代前列腺素衍生物，其中R 1是残基OR 3，其中R 3可以是氢或可能被卤素，苯基，C 1 -C 4 - 烷氧基或具有1-10个C原子的C 1 -C 4二烷基氨基取代的烷基，或残基NHR4为烷基或烷烃磺酰基残基，每个残基具有1-10个C原子; W是羟基亚甲基或基团（II），其中OH基团可以被具有1-4个C原子的苯甲酰基或烷烃酸残基酯化，或与四氢吡喃基，四氢呋喃基，（C 1 -C 4烷氧基）-C1- C 4 - 烷基或三 - （C 1 -C 4 - 烷基） - 甲苯基残基，其中游离OH基可以是α或β位; D是具有1-5个C原子的直链或支链亚烷基; R2是具有1-6个C原子的直链或支链烷基; R5是一个羟基，可以用1-4 C原子的烷烃酸残基酯化，或用四氢吡喃基，四氢呋喃基，（C 1 -C 4 - 烷氧基）-C 1 -C 4烷基或三（C 1 -C 4 - 烷基）残留物; X是氧原子或-CH 2 - 残基，如果R 3是氢，则其与生理上相容的碱的盐，其生产过程及其用作药物。

7. 发明申请

WO1986000895A1 NEW CARBACYCLINES, PREPARATION THEREOF AND DRUG CONTAINING THEM 审中-公开
标题翻译：新卡铂，其制剂和含有他们的药物
公开(公告)号：WO1986000895A1
公开(公告)日：1986-02-13
申请号：PCT/DE1985000246
申请日：1985-07-18
申请人： SCHERING AKTIENGESELLSCHAFT , VORBRÜGGEN, Helmut , NIEUWEBOER, Bob , STÜRZEBECHER, Claus-Steffen
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C177/00
CPC分类号： C07C405/0083 , C07C59/62
摘要： Carbacycline derivatives of formula (I) are disclosed, wherein: n is 1 or 3, R1 is the rest having the formula (II), the rest having the formula (III), -COCH3, the rest COOR2 wherein R2 is hydrogen or alkyl with 1 to 10 atoms of carbon optionally substituted by halogen, phenyl, C1-C4-alkoxy or C1-C4-dialkyl-amino; cycloalkyl, aryl or heterocyclic rest; or the rest CONHR3 wherein R3 is hydrogen or a rest alkanoyl sulfonyl or alkane sulfonyl with 1 to 10 atoms of carbon. R9 is an alkyl group with 1 to 10 atoms of carbon or the group -C=C- (CH2)m-R6 wherein m is 1 to 16 and R6 is hydrogen, hydroxy, amino or trimethylsilyl, X is an oxygen atom or when R9 is an alkyl group with 5 to 10 atoms of carbon, a methylene group and Y is hydrogen or fluorine. Also disclosed are a preparation process thereof and drugs containing them.

8. 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.

9. 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.

10. 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。

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