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1. 发明专利

JP2006001944A New structural analogue of vitamin d 有权
标题翻译：维生素D的新结构模拟
公开(公告)号：JP2006001944A
公开(公告)日：2006-01-05
申请号：JP2005253297
申请日：2005-09-01
申请人： Lab Theramex Sa , ラボラトワル・セラメックス・ソシエテ・アノニムLaboratoire Theramex S.A.
发明人： BOUILLON ROGER , VANDEWALLE MAURITS , DE CLERCQ PIERRE JEAN
IPC分类号： A61K31/59 , C07C401/00 , A61K31/045 , A61K31/047 , A61K31/075 , A61P3/10 , A61P3/14 , A61P5/00 , A61P5/18 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/02 , A61P17/06 , A61P17/10 , A61P17/14 , A61P19/02 , A61P19/10 , A61P25/00 , A61P29/00 , A61P31/18 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/00 , A61P37/04 , A61P37/06 , A61P43/00 , C07B53/00 , C07C35/22 , C07C35/27 , C07C43/188 , C07C45/28 , C07C47/192 , C07C47/198 , C07C47/347 , C07C47/36 , C07C47/37 , C07C49/242 , C07C49/517 , C07C49/523 , C07C49/687 , C07C49/743 , C07C49/755 , C07C57/26 , C07C59/01 , C07C61/13 , C07C69/18 , C07C69/21 , C07C69/757 , C07C255/47 , C07D301/14 , C07D303/32
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： PROBLEM TO BE SOLVED: To provide new vitamin D analogues, their production method, medicinal preparations comprising these compounds, and use of them for medicines. SOLUTION: The vitamin D analogues 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 substituted chain of five atoms which correspond to positions 8, 14, 13, 17 and 20 of vitamin D, and 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 Δ(5,7)-diene moiety connected to the A-ring of the active 1-α-hydroxy metabolite or of an established vitamin D analogue. COPYRIGHT: (C)2006,JPO&NCIPI
摘要翻译：要解决的问题：提供新的维生素D类似物，其制备方法，包含这些化合物的药物制剂以及它们用于药物。解决方案：维生素D类似物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组成的中心部分，其对应于维生素D的位置8,14,13,17和20，其末端连接，在位置20处代表维生素D的侧链或维生素D的类似物的一部分的结构部分和位置8 连接到活性1-α-羟基代谢物的A环上的Δ（5,7） - 二烯部分或已建立的维生素D类似物。版权所有（C）2006，JPO＆NCIPI

2. 发明公开

US20230390306A1 METHODS OF CONTRACEPTION USING NOMEGESTROL ACETATE AND ESTRADIOL 审中-公开
公开(公告)号：US20230390306A1
公开(公告)日：2023-12-07
申请号：US18031749
申请日：2021-10-12
申请人： THERAMEX HQ UK LIMITED
发明人： Mitra BOOLELL
IPC分类号： A61K31/573 , A61K9/00 , A61K31/565 , A61P15/18 , A61K31/567
CPC分类号： A61K31/573 , A61K9/0053 , A61K31/565 , A61P15/18 , A61K31/567
摘要： Provided are methods of contraception using as a first line combined oral contraceptive (COC), a COC composition comprising nomegestrol acetate (NOMAC) and estradiol or an ester thereof. Said COC compositions are associated with a lower risk of venous thromboembolism (VTE) as compared to other CHCs. The compositions may also be used in methods of treatment in women having conditions linked to menstruation and/or fertility.

3. 发明专利

JP2011190277A 1-n-phenylamino-1h-imidazole derivative and pharmaceutical composition containing the same 有权
标题翻译：含有它的1-N-苯基氨基-1H-咪唑衍生物和药物组合物
公开(公告)号：JP2011190277A
公开(公告)日：2011-09-29
申请号：JP2011137461
申请日：2011-06-21
申请人： Lab Theramex , ラボラトワールテラメックス
发明人： LAFAY JEAN , RONDOT BENOIT , BONNET PAULE , CLERC THIERRY , SHIELDS JACQUELINE , DUC IGOR , DURANTI ERIC , PUCCIO FRANCOIS , BLOT CHRISTIAN , MAILLOS PHILIPPE
IPC分类号： C07D409/12 , A61K31/4178 , A61P5/00 , A61P15/00 , A61P35/00 , A61P43/00 , C07D233/54 , C07D419/12
CPC分类号： C07D233/54 , C07D409/12 , C07D419/12
摘要： PROBLEM TO BE SOLVED: To provide 1-N-phenylamino-1H-imidazole derivatives and pharmaceutical compositions containing them. SOLUTION: The invention relates to the compounds of formula (I), in which R 1 , R 2 , R 3 , R 4 , Q and Z are as defined in the specification. The invention also relates to a pharmaceutical compositions containing these compounds. The invention generally relates to the field of hormone- and non hormone-dependent cancer and endocrine disorders. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：提供1-N-苯基氨基-1H-咪唑衍生物和含有它们的药物组合物。解决方案：本发明涉及式（I）化合物，其中R 1，R 2，R SB 2，R SB 3，R 3，＆lt; SB＆gt; 4＆gt;中，Q和Z如说明书中所定义。本发明还涉及含有这些化合物的药物组合物。本发明一般涉及激素和非激素依赖性癌症和内分泌疾病领域。版权所有（C）2011，JPO＆INPIT

4. 发明专利

JP2011157371A Benzothiophene sulfamic acid salt derivative as steroid sulfatase inhibitor 审中-公开
标题翻译：苯甲酸硫酸盐衍生物作为固体硫酸盐抑制剂
公开(公告)号：JP2011157371A
公开(公告)日：2011-08-18
申请号：JP2011059439
申请日：2011-03-17
申请人： Lab Theramex , ラボラトワールテラメックス
发明人： LAFAY JEAN , RONDOT BENOIT , CARNIATO DENIS , BONNET PAULE , CLERC THIERRY , SHIELDS JACQUELINE , DUC IGOR , DURANTI ERIC
IPC分类号： C07D333/54 , A61K31/381 , A61P13/08 , A61P15/00 , A61P35/00 , A61P43/00
摘要： PROBLEM TO BE SOLVED: To provide a sulfamate benzothiophene derivative as a steroid sulfatase inhibitor. SOLUTION: There is provided the sulfamate benzothiophene derivative producible from a 6-methoxy-benzothiophene (3) wherein R 3 is H, 1C-6C alkoxy or a halogen or corresponding 5-methoxy-benzothiophene by a method comprising several steps. Specifically, the compound is 3-cyclopentyl-benzothiophen-6-yl sulfamate, etc. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：提供作为类固醇硫酸酯酶抑制剂的氨基磺酸盐苯并噻吩衍生物。解决方案：提供由6-甲氧基 - 苯并噻吩（3）制备的氨基磺酸酯苯并噻吩衍生物，其中R 3是H，C 1 -C 6烷氧基或卤素或相应的5-甲氧基 - 苯并噻吩通过包括几个步骤的方法。具体地，该化合物是3-环戊基 - 苯并噻吩-6-基氨基磺酸酯等。版权所有（C）2011，JPO＆INPIT

5. 发明专利

JP2009167188A New 19-nor-pregnene derivative 审中-公开
标题翻译：新的19-NOR-PREGNENE DERIVATIVE
公开(公告)号：JP2009167188A
公开(公告)日：2009-07-30
申请号：JP2009024075
申请日：2009-02-04
申请人： Lab Theramex , ラボラトワール・テラメクス
发明人： PIASCO ALAIN , LAFAY JEAN , DELANSORNE REMI , PARIS JACQUES , PASCAL JEAN-CLAUDE
IPC分类号： A61K31/57 , C07J53/00 , A61K31/00 , A61P5/24 , A61P5/34 , A61P15/00 , A61P15/18 , C07J5/00 , C07J7/00 , C07J21/00 , C07J41/00 , C07J71/00
CPC分类号： C07J7/0045 , C07J21/006 , C07J41/0016 , C07J53/004 , C07J71/001
摘要： PROBLEM TO BE SOLVED: To provide a new compound having a specific strong progesterone-like property and devoid of residual androgenic activity.
SOLUTION: The compound is expressed by formula (I), wherein R
1 , R
2 , R
3 , R
4 , R
5 and R
6 are each a hydrogen atom or a specific substituent, X is an oxygen atom or the like, and n is 1. A pharmaceutical composition is also provided which contains the compound.
COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：要解决的问题：提供具有特异性强孕酮样特性且缺乏残留雄激素活性的新化合物。解决方案：化合物由式（I）表示，其中R 1，R 2，R 2，R 2，R SB 3，R SB， 4 ，R SB 5和R SB 6各自为氢原子或特定取代基，X为氧原子等，n为1. A 还提供含有该化合物的药物组合物。版权所有（C）2009，JPO＆INPIT

6. 发明申请

US20040220163A1 Contraceptive method and composition 审中-公开
标题翻译：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。

7. 发明授权

US3862195A Steroid derivatives and the preparation thereof 失效
标题翻译：甾体衍生物及其制备
公开(公告)号：US3862195A
公开(公告)日：1975-01-21
申请号：US15339971
申请日：1971-06-15
申请人： THERAMEX SA FRANC
发明人： GASTAUD JEAN MARIE
IPC分类号： A61K20060101 , C07C20060101 , C07C169/32
CPC分类号： C07J1/00
摘要： IN WHICH R1 is a primary, secondary or tertiary alkyl group of less than 12 carbon atoms and R2R3, R4, and R5 are the same or different and each is either hydrogen, chlorine or a methyl group. The compounds have anabolic or androgenic activity.

As new compounds 17-beta-alkyl-phenoxyacetates of 19norandrostenolone or 19-nor-testosterone of the formula:
摘要翻译：作为下式的新化合物17-去甲睾酮或19-去甲睾酮的17-β-烷基 - 苯氧基乙酸酯：

8. 发明公开

US20230398127A1 USE OF COMBINED ORAL CONTRACEPTIVES CONTAINING NOMEGESTROL ACETATE AND ESTRADIOL 审中-公开
公开(公告)号：US20230398127A1
公开(公告)日：2023-12-14
申请号：US18031748
申请日：2021-10-12
申请人： THERAMEX HQ UK LIMITED
发明人： Mitra BOOLELL
IPC分类号： A61K31/565 , A61K31/57 , A61K9/00 , A61P7/02
CPC分类号： A61K31/565 , A61K31/57 , A61K9/0053 , A61P7/02
摘要： The present invention relates to the use of compositions comprising nomegestrol acetate (NOMAC) and estradiol or an ester thereof. The compositions are for use in reducing the risk of venous thromboembolism (VTE) associated with the use of combined oral contraceptives (COC). The compositions may be used in methods of contraception and/or methods of treatment in women having conditions linked to menstruation and/or fertility.

9. 发明授权

US3558607A 1,3,5(10)-estratriene diesters 失效
标题翻译： 1,3,5（10）-ESTRATRIENE DIESTERS
公开(公告)号：US3558607A
公开(公告)日：1971-01-26
申请号：US3558607D
申请日：1968-01-18
申请人： THERAMEX
发明人： GUERITEE NICHOLAS
IPC分类号： C07J43/00 , C07C173/10
CPC分类号： C07J43/003
摘要： NEW DIESTERS OF 1,3,5(10)-ESTRATRIENE ARE PROVIDED WHICH ARE CHARACTERIZED BY TROPHIC AND ANABOLIC ACTIVITY WITH LITTLE OR NO HORMONAL ACTIVITY. THE DIESTERS ARE PREPARED FROM THE CORRESPONDING MONO-ESTERIFIED HYDROXY COMPOUNDS. THE ESTER GROUPINGS ARE ONLY IN THE 3,17-POSITIONS. THE ESTER GROUP IN THE 17-POSITION IS NICOTINOYLOXY WHILE THAT IN THE 3-POSITION MAY VARY. THE 3-HYDROXY-17NICOTINOYLOXY COMPOUND IS ALSO A PART OF THE INVENTION.

10. 发明申请

WO1998015279A1 HORMONAL COMPOSITION CONSISTING OF AN OESTROGEN COMPOUND AND OF A PROGESTATIONAL COMPOUND 审中-公开
标题翻译：雌激素化合物和孕激素组合物的组成
公开(公告)号：WO1998015279A1
公开(公告)日：1998-04-16
申请号：PCT/FR1997001792
申请日：1997-10-08
申请人： LABORATOIRE THERAMEX , LANQUETIN, Michel , PARIS, Jacques , THOMAS, Jean-Louis
发明人： LABORATOIRE THERAMEX
IPC分类号： A61K31/57
CPC分类号： A61K45/06 , A61K31/56 , A61K31/565 , A61K31/57 , Y10S424/811 , Y10S514/841 , Y10S514/843 , A61K2300/00
摘要： The invention concerns the field of chemical therapy and more particularly the field of pharmaceutical hormonal technique. More precisely it concerns novel pharmaceutical hormonal compositions characterised in that they are formed by an oestroprogestational combination consisting of an oestrogen compound and a progestational compound, associated or mixed with one or several non-toxic, inert and pharmaceutically acceptable excipients, for oral administration. The invention also concerns the use of the oestroprogestational mixture in which the oestrogenic constituent and the progestational constituent are administered in combination. The combined association can be prescribed continuously or intermittently, for producing a composition for treating oestrogenic deficiencies, preventing osteoporosis and cardiovascular diseases in the menopausal woman, or still for blocking ovulation in a woman during the period of ovarian activity. The invention also concerns a method for preparing these novel pharmaceutical oestroprogestational compositions.
摘要翻译：本发明涉及化学治疗领域，更具体地涉及药物激素技术领域。更确切地说，它涉及新型药物激素组合物，其特征在于它们由与雌激素化合物和促孕化合物组成的产卵组合形成，其与一种或多种无毒，惰性和药学上可接受的赋形剂相关或混合，用于口服给药。本发明还涉及其中雌激素成分和促孕成分组合施用的产卵药混合物的用途。可以连续或间歇地规定组合关联，用于生产用于治疗雌激素缺乏症，预防绝经妇女的骨质疏松症和心血管疾病的组合物，或仍然在卵巢活动期间阻止女性排卵。本发明还涉及制备这些新型药物产卵药组合物的方法。

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