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1. 发明申请

WO1988003527A1 IMPROVED KETO-REDUCTION OF CARBACYCLINE INTERMEDIATES 审中-公开
标题翻译：改善卡巴肼中间体的减少
公开(公告)号：WO1988003527A1
公开(公告)日：1988-05-19
申请号：PCT/DE1987000519
申请日：1987-11-12
申请人： SCHERING AKTIENGESELLSCHAFT , DAHL, Helmut , BÜTTNER, Gabriele , PESCHEL, Dieter
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C177/00
CPC分类号： C07D317/72 , C07C405/0083 , C07D319/08
摘要： Process for the production of alpha-hydroxy-bicyclo[3.3.0]octane derivatives of formula (I), where A is the double-bound residue -O-X-O-, X having the notation of a straight or branched-chain alkalin with 1-7 C atoms or the residue =CH-(CH2)3-COOR', =CH-CH2-O-CH2-COOR' or = CH-(CH2)3-O-CH2-CH2-COOR', with R' as C1-C7 alkyl; R is the residue (a), R'' having the notation of a hydrogen or phenyl, or the residue - SiR1, R2, R3, whereby R1, R2 and R3 can be the same or different and a straight or branched-chain alkyl group with 1-7 C atoms or phenyl; B is a trans-CH=C(X), with X as hydrogen or bromine, whereby the trans configuration relates to the C network; and D is an alkyl group with 1-10 C atoms, an alkenyl group with 1-10 C atoms or an alkinyl group with 1-10 C atoms. This process is characterized in that keto-bicyclo[3.3.0]octane derivatives of formula (II) are reduced in the presence of Cer-III salts.

2. 发明申请

WO1988003526A1 NEW PROCESS FOR MANUFACTURING OPTICALLY ACTIVE CARBOCYCLINE INTERMEDIATES 审中-公开
标题翻译：制造光学活性炭中间体的新工艺
公开(公告)号：WO1988003526A1
公开(公告)日：1988-05-19
申请号：PCT/DE1987000515
申请日：1987-11-12
申请人： SCHERING AKTIENGESELLSCHAFT , SKUBALLA, Werner , DAHL, Helmut
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C177/00
CPC分类号： C07D319/08 , C07C405/0083
摘要： Process for manufacturing cis-bicyclo[3.3.0]octane-2-aldehydes of formula (I), in which R1 and R2 jointly represent the double-bound residue -O-X-O-, with X as straight or branched-chain alkylene with 1-7 C-atoms or R1 and R2 accordingly represent the residue OR with R as a straight or branched-chain alkyl with 1-7 C atoms and R3 represents hydrogen, a saturated alkyl residue with 1-7 C atoms, an aralkyl residu with 7-10 C atoms, a tetrahydropyranyl residue, a trialkylsilyl residue with 1-6 C atoms in the alkyl whereby alkyl also can be substituted by phenyl, a dialkylphenylsilyl residue or alkyldiphenylsilyl residue with 1-16 C atoms in the alkyl, characterized by the fact that the diastereomeric amides of formula (II) are separated, whereby in said formula R1, R2 and R3 have the stated meanings, and in that the enantiomerically pure amide of formula (II) is reduced.
摘要翻译：制备式（I）的顺式 - 双环[3.3.0]辛烷-2-醛的方法，其中R 1和R 2共同代表双键残基-OXO-，X为直链或支链亚烷基， 7个C原子或R 1和R 2相应地表示残基OR，其中R为具有1-7个C原子的直链或支链烷基，R 3表示氢，具有1-7个C原子的饱和烷基残基，残基为7 -10 C原子，四氢吡喃基残基，烷基中含有1-6个C原子的三烷基甲硅烷基残基，其中烷基也可以被苯基，二烷基苯基甲硅烷基残基或烷基中具有1-16个碳原子的烷基二苯基甲硅烷基残基取代，其特征在于分离式（II）的非对映体酰胺，其中在所述式R1中，R2和R3具有所述含义，并且由式（II）的对映体纯的酰胺还原。

3. 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（ - ）。

4. 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.

5. 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。

6. 发明申请

WO1999001160A1 SACCHARIDE CONJUGATES, PHARMACEUTICALS CONTAINING THE SAME, PROCESS FOR PREPARING THE SAME AND THEIR USE 审中-公开
标题翻译：糖缀合物，含制药，制造方法相同，它们的用途
公开(公告)号：WO1999001160A1
公开(公告)日：1999-01-14
申请号：PCT/EP1998003142
申请日：1998-05-27
申请人： SCHERING AKTIENGESELLSCHAFT
发明人： SCHERING AKTIENGESELLSCHAFT , MARESKI, Peter , PLATZEK, Johannes , RADÜCHEL, Bernd , BERNDORFF, Dietmar , WEINMANN, Hanns-Joachim
IPC分类号： A61K49/00
CPC分类号： A61K49/124 , A61K49/085 , A61K49/146
摘要： Conjugates consist of an amino-group-containing polymer, signal-generating group(s) which contain metal ion(s), and mono- or oligosaccharides, and optionally of cations of inorganic and/or organic bases, amino acids or amino acid amides. These conjugates are valuable compounds for diagnosis and therapy.
摘要翻译：由含氨基的聚合物的缀合物，含有信令组（一个或多个）和单糖或寡糖，以及无机和/或有机碱，氨基酸或氨基酸酰胺任选阳离子金属离子（S）是用于诊断和治疗价值的化合物。

7. 发明申请

WO1998024803A1 STEROID ESTERS, METHOD FOR THE MANUFACTURE THEREOF AND THEIR PHARMACEUTICAL USE 审中-公开
标题翻译：甾族酯，PROCESS FOR THEIR和制药用
公开(公告)号：WO1998024803A1
公开(公告)日：1998-06-11
申请号：PCT/EP1997006829
申请日：1997-12-08
申请人： SCHERING AKTIENGESELLSCHAFT
发明人： SCHERING AKTIENGESELLSCHAFT , KLAR, Ulrich , CLEVE, Arwed , SCHWEDE, Wolfgang , NEEF, Günter , OTTOW, Eckhard , CHWALISZ, Kristof , SCHNEIDER, Martin
IPC分类号： C07J53/00
CPC分类号： C07J53/002 , Y10S514/843
摘要： Disclosed are novel steroid esters of formula (I), wherein m means 1 or 2, n is 0 or 1, X is F or CN and the line drawn between carbon atoms 15 and 16 symbolizes the possible presence of a dual bond, excluding compound (Z)-6'-(4-cyanphenyl)-9,11 alpha -dihydro-17 beta -hydroxy-17 alpha -[3-(1-oxo-2-methylpropoxy)-1-propenyl]-4'H-naphto[3',2',1';10,9,11] ester-4-en-3-on. Derivatization occurs with a carboxylic acid. The novel compounds are characterized by a significantly enhanced solubility in comparison with the basic hydroxy compounds, and by enhanced biological effectiveness and selectivity. Said novel compounds are suitable for the production of medicaments.
摘要翻译：它描述了式（I）其中m是1或2的新的类固醇酯，n为0或1，X为F或CN和碳原子数为15和16之间的虚线，双键的符号，但不包括化合物（Z）的任选存在 - 6 ' - （4-氰基苯基）-9,11二氢-α17的β - 羟基17α - [3-（1-氧代-2-甲基丙氧基）-1-丙烯基] -4'H - 萘并[3' ，2”，1' ：10,9,11]雌-4-烯-3-酮。衍生化用的羧酸中进行。新化合物由显着改进的溶解度以及通过增加的生物活性和选择性是从基础羟基化合物区别开来。这些新化合物是适用于生产药品。

8. 发明申请

WO1998024801A1 OXYIMINOPREGNANCARBOLACTONE 审中-公开
公开(公告)号：WO1998024801A1
公开(公告)日：1998-06-11
申请号：PCT/EP1997006657
申请日：1997-12-01
申请人： SCHERING AKTIENGESELLSCHAFT , LAURENT, Henry , LIPP, Ralph , ESPERLING, Peter , TACK, Johannes-Wilhelm
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07J41/00
CPC分类号： C07J41/0016
摘要： Disclosed are 3-oxyiminopregnan-21-carbolactone, (E,Z) mixtures and isomerically pure (E) and (Z) compounds, the production and use thereof as medicaments.
摘要翻译： 3- Oxyiminopregnan -21-内酯，（E，Z）-mixtures，和异构体纯的（E） - 和（Z）的化合物，它们的制备和在药物组合物使用进行了描述。

9. 发明申请

WO1998020856A2 MICROPARTICLES CONTAINING ACTIVE SUBSTANCES, AGENTS CONTAINING THE SAME, THEIR USE IN ULTRASOUND-CONTROLLED RELEASING OF ACTIVE SUBSTANCES AS WELL AS THE METHOD FOR THEIR PRODUCTION 审中-公开
标题翻译：有源音响微粒含剂，它们的使用在生产活性物质和方法，超声控释
公开(公告)号：WO1998020856A2
公开(公告)日：1998-05-22
申请号：PCT/EP1997006257
申请日：1997-11-04
申请人： SCHERING AKTIENGESELLSCHAFT , WEITSCHIES, Werner , BERGMANN, Martina , UHLENDORF, Volkmar , HELDMANN, Dieter
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： A61K09/00
CPC分类号： A61K41/0028 , A61K9/0009 , A61K9/5026 , A61K9/5089
摘要： The invention relates to microparticles containing active substances, wherein the active substance has been dissolved, suspended or emulsified in a low boiling fluid phase, the agents containing these particles, their use in ultrasound controlled in vivo releasing of active substances, as well as the method for producing said particles and agents.
摘要翻译：本发明涉及含有药物的微型颗粒，将活性化合物溶解，悬浮或以低siedenen液体相中乳化，含有这些药剂的颗粒，其用于超声体内药物释放，并用于生产颗粒和装置引导过程使用。

10. 发明申请

WO1998007740A1 7'alpha'-('xi'-AMINOALKYL)ESTRATRIENES, PROCESS FOR PREPARING THE SAME, PHARMACEUTICAL PREPARATIONS CONTAINING SAID 7'alpha'-('xi'-AMINOALKYL)ESTRATRIENES AND THEIR USE FOR PREPARING MEDICAMENTS 审中-公开
标题翻译： 7ALPHA-（XI-氨基烷基） - 雌三烯，制造方法药物制剂THAT THIS 7ALPHA-（XI-氨基烷基） - 雌三烯容纳和它们在药物的生产
公开(公告)号：WO1998007740A1
公开(公告)日：1998-02-26
申请号：PCT/EP1997004517
申请日：1997-08-20
申请人： SCHERING AKTIENGESELLSCHAFT
发明人： SCHERING AKTIENGESELLSCHAFT , BOHLMANN, Rolf , BITTLER, Dieter , HEINDI, Josef , HEINRICH, Nikolaus , HOFMEISTER, Helmut , KÜNZER, Hermann , SAUER, Gerhard , HEGELE-HARTUNG, Christa , LICHTNER, Rosemarie , NISHINO, Yukishige , PARCZYK, Karsten , SCHNEIDER, Martin
IPC分类号： C07J53/00
CPC分类号： C07J53/008 , C07J41/0072 , C07J43/006 , C07J53/002
摘要： The present invention describes new substituted 7α-(κ-aminoalkyl)-estratrienes of general formula (I), in which the side chain SK is a radical of partial formula (II), where m equals 4, 5 or 6; n equals 0, 1 or 2; x equals 0, 1 or 2; A is a hydrogen atom or a C1-5-alkyl group; B and D represent each a hydrogen atom, or A and B represent together an alkylene group -(CH2)p- where p = 2, 3, 4 or 5 and D is a hydrogen atom, or A and D form together an alkylene group -(CH2)q- where q = 2, 3 or 4 and B is a hydrogen atom; and E is a non-substituted ethyl radical or an ethyl radical fluorinated one to five times; or the terminal substituent -(CH2)3-E in the side chain is substituted by an optionally substituted aryl or heteroaryl radical bonded to the sulphur atom directly or by a mono-, di- or trimethylene group; R3 is a hydrogen atom, a hydrocarbon radical with up to 8 carbon atoms or a radical of partial formula R3'-C(O)-, where R3' is a hydrogen atom or a hydrocarbon radical with up to 8 carbon atoms or a phenyl radical; R11 is a hydrogen atom, a halogen atom or a nitrooxy group -O-NO¿2?, R?14, R15α, R15β, R16α and R16β¿ represent each a hydrogen atom or R?14 and R15α¿ are an additional bond or a methylene bridge, or R15β is a methyl group and R15α is a hydrogen atom, R?15α and R15β¿ represent each a methyl group, or R?15β and R16β¿ form together a methylene bridge, or R?16α or R16β¿ are a halogen atom or R?16α and R16β¿ form together a methylidene group, and the remaining substitutents R?14, R15α, R15β, R16α and R16β¿ represent each a hydrogen atom, R17' at the α- or β-position is a hydrogen atom, a C¿1-5? alkyl, C2-5 alkenyl or C2-5 alkinyl group or a trifluoromethyl group; and R?17'¿ is a hydrogen atom or a radical of partial formula R17'''-C(O)-, where R17''' is a hydrogen atom or a hydrocarbon radical with up to 8 carbon atoms, or when R17' is at the α-position, R17' forms together with R14 an ethano bridge, provided that when A and B do not stand together for -(CH¿2?)p- or A and D stand together for -(CH2)q-, at least one of the substituents R?11, R14, R15α, R15β, R16α and R16b¿ be not a hydrogen atom. Also disclosed are the physiologically tolerable addition salts of these compounds with organic and inorganic acids. These new compounds have a very strong anti-estrogenic activity. Some of them are pure anti-estrogenes, others are anti-estrogenes with a partial estrogenic effect. Because of their spectrum of activity, these new compounds are most suitable for preparing medicaments for tumor therapy and hormone substitution therapy.

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