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    Topical oestroprogestational compositions with a systemic effect
    2.
    发明授权
    Topical oestroprogestational compositions with a systemic effect 失效
    具有全身作用的局部使用雌二醇组合物

    公开(公告)号：US07030104B2

    公开(公告)日：2006-04-18

    申请号：US10129040

    申请日：2001-09-14

    申请人： Georges Gray ,  Bertrand Villet ,  Jacques Paris ,  Jean-Louis Thomas

    发明人： Georges Gray ,  Bertrand Villet ,  Jacques Paris ,  Jean-Louis Thomas

    IPC分类号： A61K31/56 ,  A61K9/14 ,  A61K9/00

    CPC分类号： A61K9/0014 ,  A61K9/06 ,  A61K9/7015 ,  A61K31/57 ,  A61K31/565 ,  A61K2300/00

    摘要： The present invention relates to the field of therapeutic chemistry and more especially to the realization of new galenic forms intended to be applied on the skin.More particularly it relates to a topical hormonal composition with a systemic effect for the hormonal treatment of the perimenopause and of the menopause as well as for the treatment of the ovarian hormonal deficiencies in women with amenorrhea, characterized in that it comprises, as active ingredients, a progestogen derived from 19-nor progesterone and estradiol or one of its derivatives, a vehicle which allows the systemic passage of said active ingredients, chosen from the group constituted by a solubilizing agent, an absorption promoting agent, a film-forming agent, a gelling agent and their mixtures, in combination or in a mixture with suitable excipients for the realization of a gelled and/or film-forming pharmaceutical form.

    摘要翻译： 本发明涉及治疗化学领域，更具体地涉及旨在应用于皮肤的新的盖仑型形式的实现。 更具体地说，本发明涉及一种局部激素组合物，具有用于激素治疗围绝经期和绝经期以及用于治疗闭经妇女的卵巢激素缺乏的全身效应，其特征在于，其包含作为活性成分的， 衍生自19-没有孕酮和雌二醇或其衍生物之一的孕激素，其允许所述活性成分的全身通过，所述载体选自由增溶剂，吸收促进剂，成膜剂， 胶凝剂及其混合物，组合或与合适的赋形剂的混合物，以实现胶凝和/或成膜药物形式。

    Topical hormonal composition with systemic action
    4.
    发明申请
    Topical hormonal composition with systemic action 审中-公开
    具有全身作用的局部荷尔蒙组成

    公开(公告)号：US20080227763A1

    公开(公告)日：2008-09-18

    申请号：US12077665

    申请日：2008-03-20

    申请人： Michel Lanquetin ,  Jacques Paris ,  Jean-Louis Thomas

    发明人： Michel Lanquetin ,  Jacques Paris ,  Jean-Louis Thomas

    IPC分类号： A61K31/57

    CPC分类号： A61K47/10 ,  A61K9/0014 ,  A61K9/7015 ,  A61K31/57 ,  A61K47/14 ,  A61K47/22 ,  A61K47/26 ,  A61K47/32 ,  A61K47/38

    摘要： The present invention relates to the area of chemotherapy and more especially to the development of new galenic forms for application to the skin.It relates more particularly to a topical hormonal composition with systemic action for the correction of progesterone deficiency in premenopausal women and for hormone replacement in menopausal women, characterized in that it contains, as the active principle, a progestogen derived from 19-nor progesterone, a vehicle permitting systemic passage of the said active principle chosen from the group comprising a solubilizing agent, an absorption promoter, a film-forming agent, a gelling agent or their mixtures, combined with or mixed with suitable excipients for production of a pharmaceutical form as a gel and/or a film.

    摘要翻译： 本发明涉及化学疗法的领域，更具体地涉及用于皮肤应用的新的盖仑制剂形式的开发。 更具体地涉及具有系统性作用的局部激素组合物，其用于矫正绝经前妇女中的孕酮缺乏和绝经妇女的激素替代，其特征在于，其包含作为活性成分的源自19-孕酮的孕激素， 允许所述活性成分的全身通过，所述活性成分选自包含增溶剂，吸收促进剂，成膜剂，胶凝剂或它们的混合物的组，与合适的赋形剂组合或与其混合，用于制备药物形式 凝胶和/或膜。

    Conformationally constrained LH-RH analogues, their uses and pharmaceutical compositions containing them
    5.
    发明授权
    Conformationally constrained LH-RH analogues, their uses and pharmaceutical compositions containing them 失效
    构象约束的LH-RH类似物，其用途和含有它们的药物组合物

    公开(公告)号：US6153587A

    公开(公告)日：2000-11-28

    申请号：US317125

    申请日：1999-05-24

    申请人： Remi Delansorne ,  Jacques Paris

    发明人： Remi Delansorne ,  Jacques Paris

    IPC分类号： A61K45/00 ,  A61K38/00 ,  A61K38/09 ,  A61P15/10 ,  A61P35/00 ,  C07K7/23

    CPC分类号： C07K7/23 ,  A61K38/00 ,  Y10S930/13

    摘要： LH-RH analogues with excellent affinity for LH-RH receptors, of the formula A.sub.1 -A.sub.2 -W-A.sub.3 -A.sub.4 -SPL-A.sub.5 -A.sub.6 -Pro-Z(I) in which:-A.sub.1 is pGlu, AcSar or an aromatic D-amino acid;-A.sub.2 is a direct bond, His, DPhe, DpFPhe or DpClPhe;*W is an aromatic L- or D-amino acid;-A.sub.3 is Ala, Thr, Ser, DSer, Ser(OBzl) or MeSer;-A.sub.4 is Tyr, Phe, cPzACAla, L- or D-PicLys, L- or D-NicLys or L- or D-IprLys;*SPL is the spirolactam of formula: ##STR1## -A.sub.5 is an amino acid with a (C.sub.1 -C.sub.8)alkyl or (C.sub.3-C.sub.6)cycloalkyl side chain;-A.sub.6 is L- or D-(Arg, HArg, Lys, HLys, Orn, Cit, HCit or Aph), where L- or D-(Arg and HArg) can be substituted by one or two (C.sub.1 -C.sub.4)alkyl groups and L- or D-(Lys, HLys, Orn and Aph) can be substituted by an isopropyl, nicotinoyl or picolinoyl group; and*Z is GlyNH.sub.2, DAlaNH.sub.2, AzaGlyNH.sub.2 or --NHR.sub.1 where R.sub.1 is a (C.sub.1 -C.sub.4)alkyl optionally substituted by a hydroxy or one or several fluorine atoms, a (C.sub.3 -C.sub.6)cycloalkyl or a heterocyclic radical selected from the group consisting of morpholinyl, pyrrolidinyl and piperidyl;or its pharmaceutically acceptable salts.

    摘要翻译： 式A1-A2-W-A3-A4-SPL-A5-A6-Pro-Z（I）的LH-RH受体具有优异亲和力的LH-RH类似物，其中：-A1是pGlu，AcSar或芳香族 D-氨基酸; -A2是直接键，His，DPhe，DpFPhe或DpClPhe; * W是芳族L-或D-氨基酸; -A3是Ala，Thr，Ser，DSer，Ser（OBzl）或MeSer; -A4是Tyr，Phe，cPzACAla，L或D-PicLys，L或D-NicLys或L或D-IprLys; * SPL是下式的螺内酰胺：-A5是具有（C1-C8）烷基或（C3-C6）环烷基侧链的氨基酸; -A6是L-或D-（Arg，HArg，Lys，HLys，Orn，Cit，HCit或Aph），其中L-或D-（Arg和HArg）可被一个或两个（C 1 -C 4）烷基取代 基团和L-或D-（Lys，HLys，Orn和Aph）可以被异丙基，烟酰基或吡啶酰基取代; 和* Z是GlyNH 2，DAla NH 2，Aza GlyNH 2或-NHR 1，其中R 1是任选被羟基或一个或多个氟原子取代的（C 1 -C 4）烷基，（C 3 -C 6）环烷基或选自以下的杂环基： 吗啉基，吡咯烷基和哌啶基; 或其药学上可接受的盐。

    3-keto-nor-pregnenes substituted in the 6-position and treatment of menopause
    6.
    发明授权
    3-keto-nor-pregnenes substituted in the 6-position and treatment of menopause 失效
    在6-位取代的3-酮 - 去甲孕烯和治疗更年期

    公开(公告)号：US5795884A

    公开(公告)日：1998-08-18

    申请号：US643623

    申请日：1996-05-06

    申请人： Robert Bucourt ,  Alain Piasco ,  Claude Tchernatinsky

    发明人： Robert Bucourt ,  Alain Piasco ,  Claude Tchernatinsky

    IPC分类号： C07J7/00 ,  A61K31/56 ,  C07J5/00

    CPC分类号： C07J7/0045

    摘要： A 3-keto-19-nor-pregnene of the formula ##STR1## wherein R is selected from the group consisting of hydroxy, acyloxy of an organic carboxylic acid, lower alkoxy, halogen and lower alkyl, R' is selected from the group consisting of hydrogen and halogen, or R and R' together form oxygen, R.sub.3 is selected from the group consisting of methyl, --OH and lower acyloxy of an organic carboxylic acid and the dotted line is an optional double bond in the 6,7-position useful for treating the symptoms of menopause in females.

    摘要翻译： 其中R选自羟基，有机羧酸的酰氧基，低级烷氧基，卤素和低级烷基，R'选自下组的3-酮-19-去甲孕烯烯，其中R选自： 的氢和卤素，或R和R'一起形成氧，R 3选自有机羧酸的甲基，-OH和低级酰氧基，虚线是6,7位任选的双键 可用于治疗女性更年期症状。

    NEW HORMONAL COMPOSITION AND ITS USE
    7.
    发明申请
    NEW HORMONAL COMPOSITION AND ITS USE 审中-公开
    新型HORMONAL组合物及其用途

    公开(公告)号：US20130172300A1

    公开(公告)日：2013-07-04

    申请号：US13448953

    申请日：2012-04-17

    申请人： Jacques Paris ,  Jean-Louis Thomas

    发明人： Jacques Paris ,  Jean-Louis Thomas

    IPC分类号： A61K31/57 ,  A61K31/567 ,  A61K31/565

    CPC分类号： A61K31/57 ,  A61K31/565 ,  A61K31/567 ,  A61K45/06 ,  A61K2300/00

    摘要： A method of preventing estrogen deficiencies and osteoporosis in menopausal women by continuously orally administering without interruption to menopausal women in need thereof an amount of 0.3 to 3 mg of 17β-estradiol or esters thereof and 0.3 to 1.25 mg of nomegestrol or esters thereof in an amount sufficient to prevent said problems.

    摘要翻译： 一种通过不间断地口服给予需要的绝经妇女不断口服绝经期女性的雌激素缺乏和骨质疏松症的方法，其量为0.3至3mg，17β-雌二醇或其酯，和0.3至1.25mg的炔雌醇或其酯， 足以防止所述问题。

    Contraceptive method and composition
    9.
    发明申请
    Contraceptive method and composition 审中-公开
    避孕方法和成分

    公开(公告)号：US20040220163A1

    公开(公告)日：2004-11-04

    申请号：US10753073

    申请日：2004-01-08

    申请人： Laboratoire Theramex

    发明人： Jacques Paris ,  Jean-Louis Thomas ,  Michel Lanquetin

    IPC分类号： A61K031/56

    CPC分类号： A61K45/06 ,  A61K31/56 ,  A61K31/565 ,  A61K31/57 ,  Y10S424/811 ,  Y10S514/841 ,  Y10S514/843 ,  A61K2300/00

    摘要： The present invention relates to a method of achieving contraception in a woman, comprising daily administering to said woman, from the first day of her cycle, a pharmaceutical composition comprising (i) estradiol, an ester thereof or an equine conjugated estrogen and (ii) nomegestrol acetate. The invention further relates to a contraceptive product comprising 21 to 28 dosage forms containing (i) estradiol, an ester thereof or an equine conjugated estrogen and (ii) nomegestrol acetate, and 0 to 7 dosage forms containing a placebo.

    摘要翻译： 本发明涉及一种在女性中实现避孕的方法，包括从其周期的第一天起对所述妇女进行日常施用的药物组合物，其包含（i）雌二醇，其酯或马共轭雌激素，和（ii） 醋酸诺美孕酮 本发明还涉及包含21至28个剂型的避孕产品，其包含（i）雌二醇，其酯或马共轭雌激素和（ii）醋酸甲孕酮，以及含有安慰剂的0至7个剂型。