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1. 发明申请

WO1995001960A1 NOVEL STRUCTURAL ANALOGUES OF VITAMIN D 审中-公开
标题翻译：维生素D的新型结构类似物
公开(公告)号：WO1995001960A1
公开(公告)日：1995-01-19
申请号：PCT/EP1994002294
申请日：1994-07-07
申请人： LABORATOIRE THERAMEX S.A. , BOUILLON, Roger , VANDEWALLE, Maurits , DE CLERCQ, Pierre, Jean
发明人： LABORATOIRE THERAMEX S.A.
IPC分类号： C07C401/00
CPC分类号： C07C47/198 , C07C35/22 , C07C35/27 , C07C47/192 , C07C47/36 , C07C47/37 , C07C49/242 , C07C49/517 , C07C49/687 , C07C49/743 , C07C49/755 , C07C57/26 , C07C59/01 , C07C401/00
摘要： The present invention relates to analogues of vitamin D, which lack the combined presence of the trans-fused six-membered C-ring and of five-membered D-ring, but still possess a central part consisting of a subsituted chain of five atoms, atoms which correspond to positions 8, 14, 13, 17 and 20 of vitamin D, and at the ends of which are connected, at position 20 a structural moiety representing part of the side-chain of vitamin D or of an analogue of vitamin D, and at position 8 the DELTA (5,7)-diene moiety connected to the A-ring of the active 1-alpha-hydroxy metabolite or of an established vitamin D analogue, to their preparation process, to preparation intermediates, to pharmaceutical preparations comprising these compounds and to their use in medicine.
摘要翻译：本发明涉及维生素D的类似物，其缺乏反式融合的六元C-环和五元D环的组合存在，但仍具有由五个原子的取代链构成的中心部分，对应于维生素D的位置8,14,13,17和20的原子，并且其末端连接在20位，代表部分维生素D的侧链或维生素D的类似物的结构部分，并且在位置8将与活性1-α-羟基代谢物或已建立的维生素D类似物的A环相连的DELTA（5,7） - 二烯部分，其制备方法制备中间体至药物制剂包括这些化合物及其在药物中的用途。

2. 发明申请

WO1992001706A1 NEW DERIVATIVES OF 3-SUBSTITUTED 6-METHYL 19-NOR PROGESTERONE AND METHOD FOR PRODUCING THEM 审中-公开
标题翻译： 3-取代的6-甲基十九烷基异构体的新衍生物及其生产方法
公开(公告)号：WO1992001706A1
公开(公告)日：1992-02-06
申请号：PCT/FR1991000587
申请日：1991-07-17
申请人： LABORATOIRE THERAMEX S.A. , PIASCO, Alain , BUCOURT, Robert , TCHERNATINSKY, Claude
发明人： LABORATOIRE THERAMEX S.A.
IPC分类号： C07J07/00
CPC分类号： C07J21/006 , C07J7/0045 , C07J41/0016
摘要： The invention relates to the field of organic chemistry and more particularly to therapeutical chemistry. It relates in particular to 6-methyl 19-nor pregna 4,6-diene 20-one having general formula (I) wherein R1 is hydrogen and R2 is a radical OR3 wherein R3 is hydrogen or an acyl residue or R1 and R2 form together a group oximino =N-OR4, or alkylene dioxy optionally substituted, or R1 and R2 are each a lower alkoxy radical or alkylene dioxy optionally substituted and Ac is the acyl residue of an organic carboxylic acid. The compounds of formula (I) are active principles of progesteronic medicaments.

3. 发明申请

WO1989003839A1 DERIVATIVES OF 19-NORPROGESTERONE, THEIR PREPARATION AND THEIR USE 审中-公开
标题翻译： 19-NORPROGESTERONE的衍生物及其制备及其使用
公开(公告)号：WO1989003839A1
公开(公告)日：1989-05-05
申请号：PCT/FR1988000527
申请日：1988-10-27
申请人： LABORATOIRE THERAMEX S.A. , PIASCO, Alain , NASRAOUI, Mohamed, Nejib
发明人： LABORATOIRE THERAMEX S.A.
IPC分类号： C07J09/00
CPC分类号： C07J9/00 , C07J13/007
摘要： The invention relates to the field of chemistry and more particularly to the field of therapeutic chemistry. Its specific subject matter concerns compounds of general formula (I), in which R is a hydrogen atom, a lower alkyl, methoxymethyl, or tetrahydropyranyl radical, or an acyl residue of a carboxylic, aliphatic or aromatic carbonic organic acid containing 1 to 10 carbon atoms, and a process for preparing them. The compounds of general formula (I), are used as the active principle in pharmaceutical compositions with a progesterone-type action.

4. 发明申请

WO1994006437A1 SUBCUTANEOUS IMPLANTS BASED ON NOMEGESTROL DERIVATIVES 审中-公开
标题翻译：基于NOMEGESTROL衍生物的不足植入物
公开(公告)号：WO1994006437A1
公开(公告)日：1994-03-31
申请号：PCT/FR1993000900
申请日：1993-09-17
申请人： LABORATOIRE THERAMEX S.A. , LANQUETIN, Michel , THOMAS, Jean, Louis , PARIS, Jacques , COUTINHO, Elsimar
发明人： LABORATOIRE THERAMEX S.A.
IPC分类号： A61K31/57
CPC分类号： A61K31/57
摘要： The present invention relates to the field of therapeutical chemistry and more particularly to pharmacotechny. Specially, the present invention relates to new compositions adapted to local administration and more precisely to forms intended to be placed in the subcutaneous tissues and commonly called implants. Said implants are of various natures (hydrophobic, hydrophilic, biodegradable) and of various types (reservoir, matrix). Said implants incorporate an efficient dose of a derivative of 3,20-dioxo 6-methyl 17(alpha)-acetoxy 19-nor pregna 4,6-diene optionally substituted in the 3 and/or 17(alpha) position, associated or mixed with a biologically acceptable inert excipient. The implants thus obtained are efficient contraceptive agents having an active duration of a least one year with minimum secondary effects.
摘要翻译：本发明涉及治疗化学领域，更具体地涉及药理学技术领域。特别地，本发明涉及适于局部施用的新组合物，更准确地说涉及旨在放置在皮下组织和通常称为植入物中的形式。所述植入物具有各种性质（疏水性，亲水性，生物降解性）和各种类型（储层，基质）。所述植入物掺入有效剂量的3,20-二氧代6-甲基17（α） - 乙酰氧基19-去甲前na 4,6-二烯衍生物，其在3和/或17（α）位置任选取代，相关联或混合具有生物学上可接受的惰性赋形剂。如此获得的植入物是具有至少一年的活性持续时间并且具有最小次要效果的有效的避孕药。

5. 发明申请

WO1992006977A1 NOVEL p-SUBSTITUTED PHENYL 4-OXYBUTANE AMINE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME 审中-公开
标题翻译：新型对取代苯基4-氧代氨基衍生物，其制备方法和含有其的药物组合物
公开(公告)号：WO1992006977A1
公开(公告)日：1992-04-30
申请号：PCT/FR1991000811
申请日：1991-10-17
申请人： LABORATOIRE THERAMEX S.A. , BONNET, Paule , DELANSORNE, Rémi , FAURE, Maurice , LANQUETIN, Michel , ZUNINO, Serge
发明人： LABORATOIRE THERAMEX S.A.
IPC分类号： C07D473/08
CPC分类号： C07D235/30 , C07D401/12 , C07D409/04 , C07D473/08
摘要： The present invention concerns organic chemistry and more particulary therapeutic chemistry. It has as its subject novel (4-substituted phenyl) 4-oxy 1-aminobutane of the general formula (I) in which X is a nitrogen atom or >CH-NH, and R is a cyclic substituent chosen from the group comprising a) a xanthic substituent, b) a benzimidazolic substituent, as well as salts and optic isomers of the compounds of formula (I). The invention also concerns processes for obtaining the compounds of formula (I) and pharmaceutical compositions containing, as active ingredient, at least one compound of formula (I) or one of its salts with a mineral or organic acid.

6. 发明申请

WO1993002095A1 NOVEL 6-SUBSTITUTED STEROIDS, METHODS FOR PRODUCING SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAID STEROIDS 审中-公开
标题翻译：新6取代的甾体，其生产方法和含有固体甾体的药物组合物
公开(公告)号：WO1993002095A1
公开(公告)日：1993-02-04
申请号：PCT/FR1992000697
申请日：1992-07-17
申请人： LABORATOIRE THERAMEX S.A. , BUCOURT, Robert , PIASCO, Alain , TCHERNATINSKY, Claude
发明人： LABORATOIRE THERAMEX S.A.
IPC分类号： C07J07/00
CPC分类号： C07J7/0045
摘要： In the field of organic chemistry, and therapeutical chemistry in particular, 6-substituted 19-nor pregnanes are provided which are selected from the group consisting of 6-substituted 3-keto-Δ4-19-nor-pregnenes having partial formula (A) and 6-substituted 3-keto-19-nor-Δ4,6-pregnadienes having partial formula (B), wherein substituents R, R', R1 and R'1 are as defined in the description. Methods for preparing these compounds, and pharmaceutical compositions containing them as the active principles, are also provided.

7. 发明申请

WO1992008730A1 NOVEL STEROIDAL ORGANIC SUBSTANCE CRYSTALLIZATION METHOD AND COMPOUNDS THEREBY OBTAINED 审中-公开
标题翻译：新型有机物质结晶方法和化合物
公开(公告)号：WO1992008730A1
公开(公告)日：1992-05-29
申请号：PCT/FR1991000888
申请日：1991-11-12
申请人： LABORATOIRE THERAMEX S.A. , LANQUETIN, Michel
发明人： LABORATOIRE THERAMEX S.A.
IPC分类号： C07J01/00
CPC分类号： C07J7/0045 , C07J1/0025 , C07J1/0074 , C07J1/0077 , C07J5/0053 , C07J11/00
摘要： A novel method is provided for crystallizing organic and particularly steroidal substances. In particular, a crystallization method is provided whereby a predeterminable and homogenous particle size class can be obtained non-mechanically, and wherein a substance is dissolved in a ternary mixture consisting of a lipophilic solvent, a hydrophilic solvent and a surface-active agent at a temperature close to boiling, whereafter the mixture is allowed to cool to a temperature at which crystallization is initiated and the crystals thereby formed are separated. The method can be used for producing pharmaceutical active principles.
摘要翻译：提供了一种用于结晶有机和特别是甾族物质的新方法。特别地，提供了一种结晶方法，其中可以非机械地获得可预定和均匀的粒度等级，并且其中将物质溶解在由亲脂性溶剂，亲水性溶剂和表面活性剂组成的三元混合物中温度接近沸腾，然后使混合物冷却至结晶开始的温度，并且由此形成的晶体分离。该方法可用于制备药物活性成分。

8. 发明申请

WO1990015067A2 NOVEL METHODS FOR OBTAINING 6-METHYL 19-NOR STEROIDS AND CONVERTING THEM INTO 17'alpha'-SUBSTITUTED 19-NOR PREGNADIENES 审中-公开
标题翻译：用于获得6-甲基十九烷基异黄酮的新方法，并将其转化为17α-取代的19-非共生体
公开(公告)号：WO1990015067A2
公开(公告)日：1990-12-13
申请号：PCT/FR1990000363
申请日：1990-05-23
申请人： LABORATOIRE THERAMEX S.A. , TCHERNATINSKY, Claude , NASRAOUI, Nejib, Mohamed , PIASCO, Alain
发明人： LABORATOIRE THERAMEX S.A.
IPC分类号： C07J01/00
CPC分类号： C07J7/002 , C07J1/0055
摘要： The invention relates to the field of organic chemistry and to steroid chemistry in particular. Its particular subject are novel 6-methyl estra 4,6-dienes of general formula (I) in which A is hydrogen or a lower oxoalkyl radical and B is hydrogen, or A is a free or esterified hydroxyl and B is a lower alkyl radical or a lower alcynyl radical, or A and B together form the oxygen of a cetone. The invention also relates to a method of obtaining compounds of general formula (I). These compounds are valuable synthesis agents which make it possible to obtain pharmacologically active 6-methyl 19-nor pregna 4,6-dienes.

9. 发明申请

WO1992022300A1 OCULAR COMPOSITIONS CONTAINING STEROIDS AND THEIR USE IN TREATING GLAUCOMA 审中-公开
标题翻译：含有甾体的组合物及其在治疗葡萄球菌中的应用
公开(公告)号：WO1992022300A1
公开(公告)日：1992-12-23
申请号：PCT/FR1992000549
申请日：1992-06-18
申请人： LABORATOIRE THERAMEX S.A. , SCHWADROHN, Gérard
发明人： LABORATOIRE THERAMEX S.A.
IPC分类号： A61K31/56
CPC分类号： A61K31/57 , A61K31/565 , A61K31/575 , C07J9/00 , C07J71/0005
摘要： The invention relates to chemotherapy and concerns particularly the preparation of pharmaceutical compositions for ocular application, said compositions being characterized in that they contain at least one selected compound of steroidal structure in association or in a mixture with a pharmaceutically acceptable inert excipient or carrier. The compositions of the invention may be used for the treatment of glaucoma.
摘要翻译：本发明涉及化学疗法，并且特别涉及用于眼部施用的药物组合物的制备，所述组合物的特征在于它们包含与药学上可接受的惰性赋形剂或载体相关联或与药学上可接受的惰性赋形剂或载体的混合物中的至少一种选定的甾体结构化合物。本发明的组合物可用于治疗青光眼。

10. 发明申请

WO1990012027A1 ALKYL DERIVATES IN 17/21 OF 19-NOR PROGESTERONE 审中-公开
标题翻译： 19-21岁的非洲前列腺素的阿尔金衍生物
公开(公告)号：WO1990012027A1
公开(公告)日：1990-10-18
申请号：PCT/FR1990000270
申请日：1990-04-13
申请人： LABORATOIRE THERAMEX S.A. , TCHERNATINSKY, Claude , NASRAOUI, Nejib, Mohamed
发明人： LABORATOIRE THERAMEX S.A.
IPC分类号： C07J07/00
CPC分类号： C07J9/00 , C07J7/004
摘要： The invention, which relates to the domain of chemistry and in particular therapeutic chemistry, essentially has as its subject matter b-methyl 19-nor pregna 4,6-dienes 17α, and if necessary, 21-alkylates of general formula (I) in which R'' and R', identical or different represent hydrogen or an alkyl radical having 1 to 3 carbon atoms in linear or branched chain and R1 represents a lower alkyl radical having 1 to 6 carbon atoms, in a linear or branched chain. Said invention is also concerned with a process for production of compounds of general formula (I) and their use as active principles in medication.

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