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1. 发明申请

WO1990011290A1 METHOD FOR THE PREPARATION OF 3-DESOXY-4-ENE STEROIDS 审中-公开
标题翻译：制备3-脱氧-4-烯酮甾体的方法
公开(公告)号：WO1990011290A1
公开(公告)日：1990-10-04
申请号：PCT/DE1990000183
申请日：1990-03-08
申请人： SCHERING AKTIENGESELLSCHAFT , WINTERFELDT, Ekkehard , TILSTAMM, Ulf , HOFMEISTER, Helmut , LAURENT, Henry
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07J11/00
CPC分类号： C07J11/00
摘要： The invention concerns a method for the preparation of 3-desoxy-4-ene steroids of the general formula I in which R1, R2 and R3 are a hydrogen atom or a methyl group, R4 is a lower alkyl group, a phenyl group or a free, esterified or etherified hydroxyl group, R5 is a hydrogen atom, a vinyl group or the -C=CR6 grouping, R6 being a hydrogen atom, an alkyl group with at the most 4 carbon atoms or a halogen atom, X is a methylene group, a fluoromethylene group, an ethylidene group or a vinylidene group, Y and U are a methylene group or an ethylidene group, and Z is a methylene group, an ethylidene group, a vinylidene group, a chloromethylene group or a hydroxymethylene group, and in which the bonds are three single bonds, or a double bond and two single bonds, or a conjugated double bond. The 3-oxo-4-ene steroid is reduced using a reaction mixture comprising trifluoroacetic or trichloroacetic acid, optionally additional carboxylic acid, and sodium borohydride.
摘要翻译：本发明涉及制备通式Ⅰ的3-脱氧-4-烯类固醇的方法，其中R1，R2和R3为氢原子或甲基，R4为低级烷基，苯基或游离的，酯化的或醚化的羟基，R5是氢原子，乙烯基或-C = CR6基，R6是氢原子，具有最多4个碳原子的烷基或卤素原子，X是亚甲基亚乙基，亚乙烯基，Y和U是亚甲基或亚乙基，Z是亚甲基，亚乙基，亚乙烯基，氯亚甲基或羟基亚甲基，和其中键是三个单键，或双键和两个单键，或共轭双键。使用包含三氟乙酸或三氯乙酸，任选的另外的羧酸和硼氢化钠的反应混合物还原3-氧代-4-烯类固醇。

2. 发明申请

WO1994029318A1 CEPHALOSTATIN ANALOGUES AND THEIR USE AS ANTI-TUMOUR AGENTS 审中-公开
标题翻译： Cephalostatin类似物及其作为抗肿瘤药
公开(公告)号：WO1994029318A1
公开(公告)日：1994-12-22
申请号：PCT/EP1994001858
申请日：1994-06-03
申请人： SCHERING AKTIENGESELLSCHAFT , WINTERFELDT, Ekkehard , KRAMER, Andreas , ULLMANN, Ulrike , LAURENT, Henry
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07D491/22
CPC分类号： C07D491/22
摘要： Described are synthetic cephalostatin analogues of general formula (I) in which (a) A and A' are each an R-CO-O- alkanoyloxy group, R being a straight-chain or branched-chain C1-C7 alkyl group, and B and D together and B' and D' together are each an additional C-C bond or (b) A' is an R-CO-O- alkanoyloxy group, R being a straight-chain or branched-chain C1-C7 alkyl group, and B' and D' together are an additional C-C bond and A and B together are a keto oxygen atom and D is a hydrogen atom or (c) A is a beta -hydroxy group and B and D are each a hydrogen atom and A' and B' together are keto oxygen atom and D' is a hydrogen atom or (d) A and A' are each a beta -hydroxy group and B, D, B' and D' are each a hydrogen atom. Such cephalostatin analogues correspond largely in their structure and substituents to the naturally occurring but only difficultly obtainable cephalostatin 1 and cephalostatin 7. The synthetic analogues possess, like the naturally occurring products, exceptional cytotoxic power and are therefore suitable for use in the preparation of drugs (anti-tumour agents).
摘要翻译：它可以是通式（I），其中a）A和A“各自代表烷酰氧基时R-CO-O-，其中R为直链或支链C1至C7烷基，B和D和的合成制备cephalostatin类似物 b“和D”各自一起代表一个附加CC键，或b）“其中R代表烷酰氧基时R-CO-O-为直链或支链C1至C7烷基，b”和D“一起是一个额外的 CC键，并且A和B一起代表酮基氧原子，D表示氢原子，或c）是β--ständige羟基和B和D每一个代表氢原子，A“和B”一起代表酮基氧原子和D“为氢原子或d）A和A“各-ständige为β羟基基团和B，D，B”和D“各自代表一个氢原子被描述，其在它们的结构和替代基本上与天然存在的，但只有非常有限的访问cephalostatins 1 和图7相对应。合成类似物具有 - 如Naturstoffe-一个特殊的细胞毒性效力，并因此可用于药物（抗肿瘤剂）的制备有用的是合适的。

3. 发明申请

WO1994004555A1 ANTI-ANDROGENE STEROIDS WITH AN ANNULATED FIVE-MEMBERED RING 审中-公开
标题翻译：抗雄激素类固醇融合五环
公开(公告)号：WO1994004555A1
公开(公告)日：1994-03-03
申请号：PCT/EP1993002194
申请日：1993-08-17
申请人： SCHERING AKTIENGESELLSCHAFT , SAUER, Gerhard , SCHRÖTER, Bernd , HOFMEISTER, Helmut , BRUMBY, Thomas , FRITZEMEIER, Karl-Heinrich , MICHNA, Horst
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07J71/00
CPC分类号： C07J1/0037 , C07J53/002 , C07J71/0005 , C07J71/0047 , C07J71/0078
摘要： New steroids with an annulated five-membered ring have general formula (I), in which Y stands for an oxygene or sulphur atom or for a sulfonyl group or for the groups (a) or (b), in which X stands for a hydrogen atom, a saturated, straight or branched chain or cyclic hydrocarbon residue substituted if required by a cyano group of by a fluorine, chlorine or bromine atom, having 1 to 8 carbon atoms in the case of the branched chain or 3 to 8 carbon atomes in the cyclic case, or an alkanoyl group with 1 to 5 carbon atoms, or a benzoyl residue or a methylsulfonyl group, or X stands for a group Z-NH or Z-O, in which Z stands for the above-mentioned substituents represented by X; R17 stands for a hydrogene atom or a straight or branched chain, saturated or unsaturated hydrocarbon residue with up to 6 carbon atoms substituted if required by a hydroxy group; R17' stands for a hydrogen atom or an alkanoyl group with 1 to 4 carbon atoms, and (c) stands for a C-C simple (5(alpha)-H) or C-C double bond and the dotted circle stands for two double bonds in the annulated five-membered ring. These new compounds have strong anti-androgene activity and are suitable for preparing medicaments.

4. 发明申请

WO1989012064A1 1'beta',15'alpha'-DIHYDROXY-1'alpha'-METHYL-5'alpha'-ANDROSTAN-3,17-DIONE, ITS PREPARATION AND USE 审中-公开
标题翻译： 1β，15α-DIHYDROXY-1α-甲基-5α-萘啶-3,17-二酮，其制备和使用
公开(公告)号：WO1989012064A1
公开(公告)日：1989-12-14
申请号：PCT/DE1989000362
申请日：1989-05-30
申请人： SCHERING AKTIENGESELLSCHAFT , PETZOLDT, Karl , HOFMEISTER, Helmut
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07J01/00
CPC分类号： C07J41/0094 , C07J1/0011 , C07J21/008 , C12P33/00
摘要： 1beta,15alpha-Dihydroxy-1alpha-methyl-5alpha-androstan-3,17-dione of formula (I) and its subsequent processing to pharmacologically active steroids.

5. 发明申请

WO1993013122A1 3-METHYLSULPHONYLHYDRAZONO AND 3-OXYIMINO STEROIDS, A METHOD OF PREPARING THEM, PHARMACEUTICAL PREPARATIONS CONTAINING THEM AND THEIR USE IN THE PREPARATION OF DRUGS 审中-公开
标题翻译： 3-甲基磺酰脲和3-氧亚氨基甾体，其制备方法，包含它们的药物制剂及其在制备药物中的用途
公开(公告)号：WO1993013122A1
公开(公告)日：1993-07-08
申请号：PCT/EP1992002983
申请日：1992-12-22
申请人： SCHERING AKTIENGESELLSCHAFT , BITTLER, Dieter , HOFMEISTER, Helmut , BRUMBY, Thomas , KROLL, Jörg , KÜNZER, Hermann , SAUER, Gerhard , FRITZEMEIER, Karl-Heinrich , MICHNA, Horst
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07J41/00
CPC分类号： C07J41/0016 , C07J41/0005
摘要： Described are 3-methylsulphonylhydrazono and 3-oxyimino steroids of the general formula (I), in which X is an oxygen atom or an NH group; the C4-C5 bond is a single or double C-C bond and the C15-C16 bond is a single or double C-C bond, and R', which depends on the nature of X, and the other substituents are as defined in the description. The new compounds are anti-androgens with peripheral selectivity and with an activity comparable to that of cyproterone acetate, and are suitable for use in the preparation of drugs.
摘要翻译：描述了通式（I）的3-甲基磺酰肼基和3-氧亚氨基类固醇，其中X是氧原子或NH基团; C4-C5键是单或双C-C键，C15-C16键是单或双C-C键，R'取决于X的性质，其他取代基如说明书中所定义。新化合物是具有周围选择性的抗雄激素，具有与醋酸环丙孕酮相当的活性，并且适用于制备药物。

6. 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。

7. 发明申请

WO1994022898A1 NEW GLUCOCORTICOIDS 审中-公开
标题翻译：新糖皮质激素
公开(公告)号：WO1994022898A1
公开(公告)日：1994-10-13
申请号：PCT/EP1994000937
申请日：1994-03-24
申请人： SCHERING AKTIENGESELLSCHAFT , ZENTEL, Hans, Joachim , TÖPERT, Michael , LAURENT, Henry , BRUMBY, Thomas , ESPERLING, Peter
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07J43/00
CPC分类号： C07J41/005 , C07J43/003
摘要： Glucocorticoids have the general formula (I): R-Val-O-GC, in which O-GC stands for the rest of an anti-inflammatory 21-hydroxycorticoid, Val stands for a valine residue located at the 21st position of the corticoid and R stands for a hydrogen atom or for a hydrocarbon residue having up to 32 carbon atoms and if required substituted by hydroxy groups, amino groups, oxo groups and/or halogen atoms and/or interrupted by oxygen atoms, SO2 groups and/or NH groups. Also disclosed are the salts of said corticoids.

8. 发明申请

WO1997040032A1 CHIRAL PHENYLDIHYDROFURANONES AS PDE-IV INHIBITORS 审中-公开
标题翻译：手性PHENYLDIHYDROFURANONE AS PDE IV抑制剂
公开(公告)号：WO1997040032A1
公开(公告)日：1997-10-30
申请号：PCT/DE1997000826
申请日：1997-04-22
申请人： SCHERING AKTIENGESELLSCHAFT , LAURENT, Henry , ESPERLING, Peter , HAMP, Kurt , SCHNEIDER, Herbert , WACHTEL, Helmut
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07D307/58
CPC分类号： C07D307/33 , C07C45/292 , C07C45/71 , C07C49/84
摘要： Described are racemic and enantiomerically pure chiral phenyldihydrofuranones, their preparation and their use in drugs (selective inhibition of the cAMP-specific phosphodiesterase IV).
摘要翻译：外消旋和对映体纯的手性Phenyldihydrofuranone，其制备和用途在药物（cAMP特异性磷酸二酯酶IV的选择性抑制）进行说明。

9. 发明申请

WO1997025312A1 NEW ROLIPRAM DERIVATIVES AS cAMP-PDE IV INHIBITORS 审中-公开
标题翻译：新咯利普兰衍生物AS的cAMP-PDE IV抑制剂
公开(公告)号：WO1997025312A1
公开(公告)日：1997-07-17
申请号：PCT/DE1997000058
申请日：1997-01-10
申请人： SCHERING AKTIENGESELLSCHAFT , SCHMIECHEN, Ralph , LAURENT, Henry , ESPERLING, Peter , HAMP, Kurt , BREITKOPF, Alfred , SKÖTSCH, Carlo , SCHNEIDER, Herbert , WACHTEL, Helmut
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07D207/26
CPC分类号： C07D207/26 , C07D207/38 , C07D211/76 , C07D211/86 , C07D307/58
摘要： Described are compounds of the formula (I), their preparation and their use in drugs.
摘要翻译：有式（I），它们在药物的制备和用途的描述的化合物。

10. 发明申请

WO1986004900A1 1'alpha'.7'alpha'-DITHIO SUBSTITUTED SPIROLACTONE, PREPARATION PROCESS THEREOF AND UTILIZATION THEREOF AS DRUG 审中-公开
标题翻译： 1α7αα-取代的螺旋体，其制备方法及其作为药物的利用
公开(公告)号：WO1986004900A1
公开(公告)日：1986-08-28
申请号：PCT/DE1986000055
申请日：1986-02-13
申请人： SCHERING AKTIENGESELLSCHAFT , NICKISCH, Klaus , LAURENT, Henry , BITTLER, Dieter , WIECHERT, Rudolf , LOSERT, Wolfgang
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07J53/00
CPC分类号： C07J53/008
摘要： New 1 alpha .7 alpha -dithio substituted spirolactones having the general formula (I) wherein R1 is C1-3-alkyl and C1-3-acyl and R2 is hydrogen, C1-3-alkyl and C1-3-acyl, preparation thereof and utilization thereof as drug. The compounds have an antialdosterone activity and present the activity profile of pro-drug.
摘要翻译：具有通式（I）的新的1α.7α-二硫代取代的己内酯，其中R 1是C 1-3 - 烷基和C 1-3 - 酰基且R 2是氢，C 1-3 - 烷基和C 1-3 - 酰基，其制备并将其用作药物。该化合物具有抗醛固酮活性，并呈现前药的活性。

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