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121. 发明申请

WO1995017194A1 COMPOSITION FOR A CONTRACEPTIVE COMPRISING AN ESTROGEN AND A GESTAGEN 审中-公开
标题翻译：组成避孕，包括雌激素和孕激素
公开(公告)号：WO1995017194A1
公开(公告)日：1995-06-29
申请号：PCT/EP1994004274
申请日：1994-12-22
申请人： SCHERING AKTIENGESELLSCHAFT
发明人： SCHERING AKTIENGESELLSCHAFT , SPONA, Jürgen , DÜSTERBERG, Bernd , LÜDICKE, Frank , FEICHTINGER, W. , ELSTEIN, Max
IPC分类号： A61K31/57
CPC分类号： A61K31/565 , A61K31/567 , A61K31/57 , A61K31/58 , A61K2300/00
摘要： The invention concerns the use of a composition comprising an estrogen selected from 2.0-6.0 mg 17 beta -estradiol and 0.015-0.020 mg ethinyl estradiol and a gestagen selected from 0.05-0.075 mg gestodene, 0.075-0.125 mg levonorgestrel, 0.06-0.15 mg desogestrel, 0.06-0.15 mg 3-ketodesogestrel, 0.1-0.3 mg drospirenone, 0.1-0.2 mg cyproterone acetate, 0.2-0.3 mg norgestimate and >0.35-0.75 mg norethisterone, used to produce a dosage formulation for contraception for a woman of child-bearing age who has not reached premenopause by administering the dosage formulation during 23 or 24 days, beginning on day one of the menstrual cycle, followed by 5 or 4 pill-free or placebo days, over a complete 28-day cycle of administration, wherein the individual dosage formulations contain a constant amount of estrogen/gestagen throughout the 23 or 24 days. The invention also pertains to a combination oral contraceptive based on this composition.
摘要翻译：本发明涉及使用包含选自2.0至6.0毫克17β-雌二醇和0.015至0.020毫克乙炔雌二醇的雌激素的组合物; 和孕激素选自0.05至0.075毫克孕二烯酮的，左炔诺孕酮0.06 0.075至0.125毫克至0.15mg去氧孕烯的0.06至0.15毫克3-酮去氧孕烯，0.1〜0.3毫克的屈螺酮，0.1至0.2mg醋酸环丙孕酮，0.2至0.3mg诺孕酯和> 0.35至0.75毫克炔诺酮的用于生产剂型的避孕对于女人育龄谁尚未绝经前期已达到，通过施用为23或24天的剂型，自月经周期的第一天，接着用5或4丸免费或空白丸天，总共在施用周期28天，所有的23或24天，单个剂型是恒定的雌激素/ 包含孕激素量，以及用于基于该组合物口服避孕单相组合产品。

122. 发明申请

WO1995013802A1 TREATMENT OF UTERINE CONTRACTILITY DISORDERS WITH A NITRIC OXIDE SYNTHASE SUBSTRATE AND/OR DONOR, OR A NITRIC OXIDE INHIBITOR 审中-公开
标题翻译：用氮氧化物合成酶底物和/或离子或氮氧化物抑制剂治疗子宫内膜异位症的治疗
公开(公告)号：WO1995013802A1
公开(公告)日：1995-05-26
申请号：PCT/EP1994003817
申请日：1994-11-17
申请人： SCHERING AKTIENGESELLSCHAFT , GARFIELD, Robert, E. , YALLAMPALLI, Chandra
发明人： SCHERING AKTIENGESELLSCHAFT , CHWALISZ, Kristof , BUKOWSKI, Radoslaw
IPC分类号： A61K31/195
CPC分类号： A61K31/565 , A61K31/04 , A61K31/195 , A61K31/557 , A61K31/57 , A61K38/11 , A61K31/41 , A61K31/34 , A61K31/295 , A61K31/21 , A61K2300/00
摘要： Dysmenorrhea, disfunctional uterine bleeding, preterm labor and postpartum labor in female mammals are treated by inhibiting uterine contractility by administering thereto a nitric oxide synthase substrate, a nitric oxide donor or both, optionally in combination with one or more of a prostaglandin inhibitor, a prostacyclin-mimetic, a progestin, an oxytocin antagonist or a beta -agonist in an amount effective to ameliorate the symptoms thereof; and inadequate menses treated and induction of abortion or stimulation of labor in a pregnant female is achieved by uterine contractility stimulation by administering thereto a nitric oxide inhibitor, either alone or in a combination of progesterone antagonist, an oxytocin or oxytocin analogue antagonist or prostaglandin.
摘要翻译：通过给予一氧化氮合酶底物，一氧化氮供体或两者，任选地与一种或多种前列腺素抑制剂，前列环素组合，通过抑制子宫收缩力来治疗女性哺乳动物的痛经，功能性子宫出血，早产和产后劳动孕激素，孕激素，催产素拮抗剂或β-拮抗剂，其量有效地改善其症状; 通过对单独的或孕酮拮抗剂，催产素或催产素类似物拮抗剂或前列腺素的组合施用一氧化氮抑制剂，通过子宫收缩力刺激来实现对怀孕女性的月经不足和诱导堕胎或刺激劳动。

123. 发明申请

WO1995013800A1 TREATMENT OF CLIMACTERIC DISORDERS WITH NITRIC OXIDE SYNTHASE SUBSTRATES AND/OR DONORS 审中-公开
标题翻译：用氮氧化物合成酶底物和/或配体处理气候障碍
公开(公告)号：WO1995013800A1
公开(公告)日：1995-05-26
申请号：PCT/EP1994003818
申请日：1994-11-17
申请人： SCHERING AKTIENGESELLSCHAFT , YALLAMPALLI, Chandra , GARFIELD, Robert, E.
发明人： SCHERING AKTIENGESELLSCHAFT , CHWALISZ, Kristof , BUKOWSKI, Radoslaw
IPC分类号： A61K31/04
CPC分类号： A61K31/565 , A61K31/04 , A61K31/195 , A61K31/198 , A61K31/295 , A61K31/341 , A61K31/57 , A61K31/60 , Y10S514/899 , A61K31/41 , A61K31/34 , A61K31/21 , A61K2300/00 , A61K31/557 , A61K31/26
摘要： The symptoms of the climacterium are ameliorated by the administration to an afflicted individual one or both of a nitric oxide substrate and/or nitric acid donor, alone or optionally in combination with a progestin or, in the case of non-pregnant female, either a progestin or an estrogen or both.
摘要翻译：通过向受苦的个体一个或两个一氧化氮底物和/或硝酸供体施用单独或任选地与孕激素组合，或者在非怀孕的雌性的情况下，可以改善天敌的症状，孕激素或雌激素或两者。

124. 发明申请

WO1995010528A1 PROCESS FOR PRODUCING SULFURIC ACID SEMI-ESTERS 审中-公开
标题翻译：用于生产硫酸半星
公开(公告)号：WO1995010528A1
公开(公告)日：1995-04-20
申请号：PCT/EP1994003296
申请日：1994-10-06
申请人： SCHERING AKTIENGESELLSCHAFT , JUNGHANS, Klaus
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07J31/00
CPC分类号： C07J31/006
摘要： The invention relates to a process for producing sulfuric acid semi-esters of general formula (I): RO-SO2-OH, in which R is an organic radical, from hydroxy compounds of general formula (II): R-OH, in which R is the same as in formula (I), characterized in that these compounds are reacted in an inert solvent with a pyrosulphuric acid salt of general formula (III): O(SO2OX)2, in which X represents an alkaline metal atom.
摘要翻译：本发明涉及一种用于通式（I）的硫酸单酯的制备：RO-SO 2 OH，其中R是有机基团，从通式（II）的羟基化合物：R-OH，其中R具有相同的含义如式具有（I），其特征在于Daduchus，这些与Dischwefelsäuresalz通式（III）在惰性溶剂：反应是O（SO2OX）2，其中X象征碱金属原子。

125. 发明申请

WO1995007263A1 1,2-DI(HETERO)ARYLBENZIMIDAZOLE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS PROSTACYCLIN (PGI2) MIMETICS 审中-公开
标题翻译： 1,2-二（HET）芳基 - 苯并咪唑衍生物，它们的制备以及它们作为前列环素的使用（PGI2）模拟物
公开(公告)号：WO1995007263A1
公开(公告)日：1995-03-16
申请号：PCT/EP1994002948
申请日：1994-09-06
申请人： SCHERING AKTIENGESELLSCHAFT , KUHNKE, Joachim , ECKLE, Emil , THIERAUCH, Karl-Heinz , VERHALLEN, Peter
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07D235/18
CPC分类号： C07D235/18
摘要： The invention concerns benzimidazole derivatives of the formula (I) in which: R and R are hetero-aryl or phenyl which may be mono- or di-substituted with halogen, a straight-chain or branched-chain alkyl group with 1-6 C-atoms, perfluoroalkyl with 1-4 C-atoms, alkoxy with 1-6 C-atoms, perfluoroalkoxy with 1-4 C-atoms, carboxyl, straight-chain or branched-chain alkoxycarbonyl with 1-6 C-atoms in the alkoxy chain, the CONHR group, straight-chain or branched-chain alkylcarbonyl with 1-6 C-atoms, nitro, amino, the NHCOR group or the NHSO2R group, R and R are hydrogen, halogen, a straight-chain or branched-chain alkyl group with 1-6 C-atoms, perfluoroalkyl with 1-4 C-atoms, alkoxy with 1-6 C-atoms, perfluoroalkoxy with 1-4 C-atoms, carboxyl, straight-chain or branched-chain alkoxycarbonyl with 1-6 C-atoms in the alkoxy chain, the CONHR group, straight-chain or branched-chain alkylcarbonyl with 1-6 C-atoms, nitro, amino, the NHCOR group or the NHSO2R group, A is a direct link, straight-chain or branched-chain alkylene with 1-8 C-atoms, straight-chain or branched-chain alkenylene with 2-8 C-atoms, straight-chain or branched-chain alkinylene with 2-8 C-atoms or one of the groups (a), (b) or (c) in which n may be 1-4, whereby one of the methylene groups in the alkylene, alkenylene or alkinylene groups or in the alkylaryl groups may be replaced by oxygen or sulphur, or two of the methylene groups may be replaced by oxygen and/or sulphur provided the hetero-atoms are separated by at least two C-atoms, R is carboxyl, SO3H, PO3H2 or tetrazolyl, plus their salts with physiologically tolerated bases, their addition compounds with physiologically tolerated acids or alpha -, beta - or gamma -cyclodextrin clathrates and compounds encapsulated in liposomes. The invention also concerns methods of preparing these compounds and their use as drugs. These compounds are useful aids in the therapy of illnesses provoked by a deficiency of PGI2 in the body and/or an excess of TXA2 or PGH2.
摘要翻译：本发明涉及式（I）其中，R <1>和R <2>杂芳基或苯基，其任选地单或二取代由卤素，直链或支链的烷基，具有1-6个碳原子，1全氟烷基的苯并咪唑衍生物 4个碳原子，烷氧基具有1-6个碳原子的，全氟烷氧基1-4个碳原子，羧基，直链或支链烷氧基羰基具有在直链中含有1-6个C原子或支链烷基部分，基团CONHR <6>，直链的或具有1-6个碳原子，硝基，氨基，自由基NHCOR <6>或基团NHSO 2 <7>可以被取代，R <3>和R <4>支链烷基羰基为氢，卤素，直链或支链烷基具有1-6个碳原子，1-4个碳原子的全氟烷基，烷氧基具有1-6个碳原子的，全氟烷氧基1-4个碳原子，羧基，直链或支链烷氧基羰基的在直链具有1-6个C原子的或支链烷基部分，其余CONHR <6>中，具有1-6个碳原子，硝基，氨基的直链或支链的烷基羰基时，R EST NHCOR <6>或基团NHSO 2 <7>中，A是直接键，具有1-8个C原子的直链或支链亚链烯基具有2-8个碳原子的，直链或支链的亚炔基具有2-8℃的直链或支链亚 -atoms，或基团（A），（b）或（c）中，其中n可以是1-4 =，其中在所述取代的亚烷基，亚烯基或亚炔的亚甲基基团的一个或被氧或硫Alkylarylenresten 可以，或两个亚甲基可以被氧和/或硫，其中杂原子被至少两个碳原子，R <5>羧基，SO 3 H，PO 3 H 2或四唑基，它们与生理上相容的碱形成的盐，它们的加成化合物中分离取代的与生理上可接受的酸，α - ，β - 或伽马-Cyclodextrinclathrate和与脂质体包封的化合物，它们的制备方法和它们作为药物的用途。所述化合物可用于它们是由于缺乏内源性PGI2和/或过量TXA2和PGH2的疾病的治疗有价值的工具，是。

126. 发明申请

WO1995006647A1 ALKOXY-SUBSTITUTED 'beta'-CARBOLINES ACTING ON THE AMPA-RECEPTOR 审中-公开
标题翻译：烷氧基 - 取代的β-咔啉与暴露于AMPA受体
公开(公告)号：WO1995006647A1
公开(公告)日：1995-03-09
申请号：PCT/DE1994001009
申请日：1994-08-29
申请人： SCHERING AKTIENGESELLSCHAFT , SEIDELMANN, Dieter , TURSKI, Lechoslaw
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Compounds having the formula (I) are disclosed, as well as their preparation and use in medicaments acting on the AMPA-receptor.
摘要翻译：有式（I）和它们在作用于AMPA受体药物的制备和用途的描述的化合物。

127. 发明申请

WO1994027978A1 MACROCYCLIC METAL COMPLEXES CONTAINING FLUORINE 审中-公开
标题翻译： FLUOR含大环金属络合物
公开(公告)号：WO1994027978A1
公开(公告)日：1994-12-08
申请号：PCT/EP1994001377
申请日：1994-04-29
申请人： SCHERING AKTIENGESELLSCHAFT , PLATZEK, Johannes , RADÜCHEL, Bernd , NIEDBALLA, Ulrich , WEINMANN, Hanns-Joachim , BAUER, Hans , ROTH, Klaus
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07D257/02
CPC分类号： G01R33/5601 , A61K49/0433 , C07D257/02 , G01R33/4804
摘要： The invention concerns fluorine-containing macrocyclic metal complexes consisting of a complexing agent of formula (I), in which n, m, R , R , R and A are defined differently, plus at least one metal ion with an atomic number of 21 to 29, 42, 44 or 57 to 83. The invention also concerns agents containing such complexes, their use as NMR and X-ray diagnostic agents and methods of preparing these compounds and agents.
摘要翻译：本发明涉及由式（I）的配位剂的新型含氟大环金属络合物和原子序数21-29，42，44或57-83，其中N，M，R <1>，R <2>的元素的至少一种金属离子，R <3>和A unterschliedliche含义，这些化合物含，它们作为NMR和X射线诊断和制备这些化合物和制剂的方法中使用。

128. 发明申请

WO1994025472A1 PYRIDO(1,2,3-DE)QUINOXALINE DERIVATIVES, PROCESS FOR PREPARING THE SAME AND THEIR USE IN MEDICAMENTS 审中-公开
标题翻译：吡啶并[1,2,3-de]喹喔，METHOD FOR它们在新药与
公开(公告)号：WO1994025472A1
公开(公告)日：1994-11-10
申请号：PCT/DE1994000494
申请日：1994-04-28
申请人： SCHERING AKTIENGESELLSCHAFT , KRÜGER, Martin , SEELEN, Werner , TURSKI, Lechoslaw
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07F09/6561
CPC分类号： C07D471/06 , C07F9/6561
摘要： Pyrido[1,2,3-de]quinoxaline derivatives have formula (I), in which R , R and R stand for hydrogen, -POXY, halogen or -COR; R stand for hydrogen or OH; R , R and R are the same or different and stand for hydrogen, halogen, nitro, NR R , cyano, CF3, C1-6-alkyl or C1-4-alkoxy; or R and R or R and R ===

129. 发明申请

WO1994017029A1 DERIVATED DTPA COMPLEXES, PHARMACEUTICALS CONTAINING THESE COMPOUNDS, THEIR USE AS NMR- AND RADIOGRAPHIC CONTRASTING AGENTS AND PROCESS FOR PRODUCING THE SAME 审中-公开
标题翻译：衍生化DTPA络合物，含有它们的制药，其作为核磁共振和X射线造影剂和方法使用其
公开(公告)号：WO1994017029A1
公开(公告)日：1994-08-04
申请号：PCT/EP1994000033
申请日：1994-01-08
申请人： SCHERING AKTIENGESELLSCHAFT , SCHMITT-WILLICH, Heribert , PLATZEK, Johannes , GRIES, Heinz , RADÜCHEL, Bernd , PETROV, Orlin , MÜHLER, Andreas , FRENZEL, Thomas , VOGLER, Hubert , BAUER, Hans , NICKISCH, Klaus , HILSCHER, Jean-Claude
发明人： SCHERING AKTIENGESELLSCHAFT
IPC分类号： C07C229/16
CPC分类号： A61K49/06 , C07C229/16 , C07C229/76 , Y10S514/836 , Y10T436/24
摘要： Complex compounds and their salts consist of at least one metal ion and a complexing agent having general formula (I), in which Z and Z represent independently from each other a hydrogen atom, the residue -(CH2)m-(C6H4)q-(O)k-(CH2)n-(C6H4)l-(O)r-R, or the residue -(CH2)m-(C6H10)q-(O)k-(CH2)n-(C6H10)l-(O)r-R, in which m and n are the numbers 0-5, q, k, l and r are the numbers 0 or 1 and s is the number 1 or 2; R stands for a hydrogen atom, an if required OR - substituted, straight-chain or branched-chain C1-C6-alkyl residue or a CH2-COOR group, in which R stands for a hydrogen atom, a C1-C6-alkyl residue or a benzyl group, with the proviso that one of the substituents Z or Z stands for a hydrogen atom and the other does not, and that a direct oxygen-oxygen bond is not allowed. Also disclosed is their use for producing radiotherapy agents and NMR and radiographic diagnosing agents, in particular for contrasting the hepatobiliary system. A process for producing these compounds and agents is further disclosed.

130. 发明申请

WO1994007853A1 25-CARBOXYLIC ACID DERIVATIVES IN THE VITAMIN D SERIES, METHOD OF PRODUCING THEM, INTERMEDIATE PRODUCTS FOR THIS METHOD, PHARMACEUTICAL PREPARATIONS CONTAINING THESE DERIVATIVES AND THEIR USE IN THE MANUFACTURE OF MEDICINES 审中-公开
标题翻译：中的维生素D系列25羧酸衍生物，产生方法，中间产品对于此方法，这些衍生物药物制剂和它们在药物的生产
公开(公告)号：WO1994007853A1
公开(公告)日：1994-04-14
申请号：PCT/EP1993002814
申请日：1993-10-06
申请人： SCHERING AKTIENGESELLSCHAFT
发明人： SCHERING AKTIENGESELLSCHAFT , STEINMEYER, Andreas , KIRSCH, Gerald , NEEF, Günter , SCHWARZ, Katica , THIEROFF-EKERDT, Ruth , WIESINGER, Herbert , HABEREY, Martin
IPC分类号： C07C401/00
CPC分类号： C07C401/00
摘要： Described are the new 25-carboxylic acid derivatives of general formula (I), R and R each denoting a hydrogen atom or in common an exocyclic methyl group, R and R independently of each other denoting a hydrogen atom, a chlorine or fluorine atom, an alkyl group with 1-4 carbon atoms, in common a methylene group, a 3-7 membered, saturated or unsaturated carbocyclic ring in common with the quaternary 20 carbon atom, Y preferably denoting a derivatized carboxyl residue, with the other substituents as indicated in the description, and a method of producing them. The new compounds possess vitamin D activity as well as anti-proliferative and cell-differentiating action and can be used in the manufacture of medicines.

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