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1. 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

2. 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

3. 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

4. 发明申请

WO2011098439A3 A PROCESS FOR INTRODUCING A DOUBLE BOND INTO POSITION 15,16 OF A STEROID 审中-公开
标题翻译：将双键引入甾体化合物的位置15,16的方法
公开(公告)号：WO2011098439A3
公开(公告)日：2011-10-27
申请号：PCT/EP2011051783
申请日：2011-02-08
申请人： THERAMEX , MOUTOU JEAN-LUC , MOUTON FLORENT , PELLEGRINO GILLES , DILLENSCHNEIDER JEAN-MARC , LAFAY JEAN
发明人： MOUTOU JEAN-LUC , MOUTON FLORENT , PELLEGRINO GILLES , DILLENSCHNEIDER JEAN-MARC , LAFAY JEAN
IPC分类号： C07J1/00
CPC分类号： C07J1/00 , C07J1/0059
摘要： The invention relates to a process for the preparation of a compound of formula (I): wherein R1 and R2 are as defined in the description, by reaction of a compound of formula (II) with a base. Compound (I) is an intermediate useful in the preparation of gestodene.
摘要翻译：本发明涉及通过式（II）化合物与碱反应制备式（I）化合物的方法：其中R 1和R 2如说明书中所定义。化合物（I）是用于制备孕二烯酮的中间体。

5. 发明申请

WO2004054983A3 1-N-PHENYLAMINO-1H-IMIDAZOLE DERIVATIVES AS AROMATASE INHIBITORS 审中-公开
标题翻译：作为芳香化酶抑制剂的1-N-苯基氨基-1H-咪唑衍生物
公开(公告)号：WO2004054983A3
公开(公告)日：2004-08-05
申请号：PCT/EP0315027
申请日：2003-12-15
申请人： THERAMEX , ADJE NATHALIE , BONNET PAULE , CARNIATO DENIS , LAFAY JEAN , DELANSORNE REMI , PASCAL JEAN-CLAUDE
发明人： ADJE NATHALIE , BONNET PAULE , CARNIATO DENIS , LAFAY JEAN , DELANSORNE REMI , PASCAL JEAN-CLAUDE
IPC分类号： A61P43/00 , C07D233/54 , C07D233/88 , C07D521/00 , A61K31/4164
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： The present invention relates to imidazole derivatives of the formula: (I) in which R1, R2, R3, R4, R5, R6 and n are as defined in the specification.The invention also relates to pharmaceutical compositions containing these derivatives, and to the uses thereof.
摘要翻译：本发明涉及式（I）的咪唑衍生物，其中R 1，R 2，R 3，R 4，R 5，R 6和n如说明书中所定义。本发明还涉及含有这些衍生物的药物组合物，用途。

6. 发明公开

EP0886645A1 NEW 19-NOR-PREGNENE DERIVATIVES 失效
标题翻译： NEW 19-NOR - 孕甾烯衍生物
公开(公告)号：EP0886645A1
公开(公告)日：1998-12-30
申请号：EP97902235
申请日：1997-01-17
申请人： THERAMEX
发明人： PIASCO ALAIN , LAFAY JEAN , DELANSORNE REMI , PARIS JACQUES , PASCAL JEAN-CLAUDE
IPC分类号： A61K31/57 , A61K31/00 , A61P5/24 , C07J5/00 , C07J7/00 , C07J21/00 , C07J41/00 , C07J53/00 , C07J71/00
CPC分类号： C07J7/0045 , C07J21/006 , C07J41/0016 , C07J53/004 , C07J71/001
摘要： The invention relates to compounds of formula (I), in which R1, R2, R3, R4, R5, R6, n and X are as defined in the specification, and to pharmaceutical compositions containing them. These compounds are excellent progestogens which are devoid of residual androgenic activity.

7. 发明专利

CA2582180C INDAZOLES, BENZISOXAZOLES AND BENZISOTHIAZOLES, PROCESS FOR PREPARING THEM, PHARMACEUTICAL COMPOSITIONS AND USE AS ESTROGENIC AGENTS 未知
公开(公告)号：CA2582180C
公开(公告)日：2013-04-30
申请号：CA2582180
申请日：2005-10-14
申请人： THERAMEX
发明人： RONDOT BENOIT , LAFAY JEAN , BONNET PAULE , CLERC THIERRY , DUC IGOR , DURANTI ERIC , PUCCIO FRANCOIS , SHIELDS JACQUELINE , BLOT CHRISTIAN , MAILLOS PHILIPPE
IPC分类号： C07D231/56 , A61K31/416 , A61K31/4162 , A61K31/423 , A61K31/428 , A61P5/30 , C07D261/20 , C07D275/04 , C07D275/06 , C07D491/06
摘要： The present invention relates to compounds of formula (I): in which R1, R2, R3, X, Y and A are as defined in the specification. The compounds are modulators of the estrogen receptors.

8. 发明专利

AU2011226950B9 1-N-phenyl-amino-1H-imidazole derivatives and pharmaceutical compositions containing them 未知
公开(公告)号：AU2011226950B9
公开(公告)日：2013-04-11
申请号：AU2011226950
申请日：2011-09-29
申请人： LABORATOIRE THERAMEX
发明人： RONDOT BENOIT , BLOT CHRISTIAN , DURANTI ERIC , PUCCIO FRANCOIS , CLERC THIERRY , SHIELDS JACQUELINE , LAFAY JEAN , BONNET PAULE , MAILLOS PHILIPPE , DUC IGOR
IPC分类号： C07D233/54 , C07D409/12 , C07D419/12
摘要： 1-N-phenyl-amino- 1H-imidazole derivatives and pharmaceutical compositions containing them Abstract 5 The invention relates to the compounds of formula (1), in which RI, R2, R3, R4, Q and Z are as defined in the specification. The invention also relates to the pharmaceutical compositions containing these compounds. The invention generally relates to the field of hormone- and non hormone-dependent cancer and endocrine disorders.

9. 发明专利

ES2368203T3 INDAZOLES, BENCISOXAZOLES Y BENCISOTIAZOLES Y SU USO COMO AGENTES ESTROGENICOS. 未知
公开(公告)号：ES2368203T3
公开(公告)日：2011-11-15
申请号：ES05794749
申请日：2005-10-14
申请人： THERAMEX
发明人： RONDOT BENOIT , LAFAY JEAN , BONNET PAULE , CLERC THIERRY , DUC IGOR , DURANTI ERIC , PUCCIO FRANCOIS , SHIELDS JACQUELINE , BLOT CHRISTIAN , MAILLOS PHILIPPE
IPC分类号： C07D231/56 , A61K31/416 , A61K31/4162 , A61K31/423 , A61K31/428 , A61P5/30 , C07D261/20 , C07D275/04 , C07D275/06 , C07D491/06
摘要： Un compuesto de fórmula (I) o una sal de adición de ácidos o una forma estereoisomérica del mismo, en el que: - R1 es hidrógeno o un alquilo (C1-C6), cicloalquilo (C3-C6), trifluorometilo, -N=CR5R6, - SO2NR7R8, fenilo, fenilalquilo (C1-C3) o alquilo (C1-C3) sustituido por un radical heterocíclico saturado, en el que el fenilo está sin sustituir o sustituido por al menos un sustituyente seleccionado entre el grupo constituido por un hidroxilo, un halógeno, un nitro, un ciano, un alquilo (C1-C3), un alcoxi (C1-C3), y un trifluorometilo; R1 también puede ser una sal; - R2 y R3 son, cada uno independientemente, hidrógeno o un hidroxilo, halógeno, nitro, ciano, alquilo (C1-C6), cicloalquilo (C3-C6), alcoxi (C1-C6), trifluorometilo, un grupo -NR7R8, - CONR7R8, -COR9 o -CO2R9; R2 también puede ser un fenilo o un heterociclo saturado o insaturado, en el que el fenilo está sin sustituir o sustituido por al menos un sustituyente seleccionado entre el grupo constituido por un hidroxilo, un halógeno, un nitro, un ciano, un alquilo (C1-C3), un alcoxi (C1-C3), un trifluormetilo y un radical heterocíclico saturado; - X es O, S, SO, SO2 o NR4; - R4 es hidrógeno o un alquilo (C1-C6), cicloalquilo (C3-C6), fenilo, fenilalquilo (C1-C3), alquilo (C1-C3) sustituido por un radical heterocíclico saturado, un grupo -COR7, -CO2R7 o -SO2NR7R8, en el que el fenilo está sin sustituir o sustituido por al menos un sustituyente seleccionado entre el grupo constituido por un hidroxilo, un halógeno, un nitro, un ciano, un alquilo (C1-C3), un alcoxi (C1-C3), un trifluorometilo, un fenilalquilo (C1- C3) y un fenilalcoxi (C1-C3); - Y es un enlace directo, O, S, SO, SO2, NR4, CO, -(CR10R11)n- o -R10C=CR11-; - R5, R6, R7 y R8 son, cada uno independientemente, hidrógeno o un grupo alquilo (C1-C6) o cicloalquilo (C3- C6); - R9 es hidrógeno, un alquilo (C1-C6), un fenilo o un radical heterocíclico saturado o insaturado, en el que el fenilo está sin sustituir o sustituido por al menos un sustituyente seleccionado entre el grupo constituido por un hidroxilo, un halógeno, un nitro, un ciano, un alquilo (C1-C3), un alcoxi (C1-C3), un trifluormetilo y un radical heterocíclico saturado; - R10 y R11 son, cada uno independientemente, hidrógeno o un ciano, alquilo (C1-C6), -CO-fenilo, -CO (radical heterocíclico insaturado) o un grupo -CONR7R8, en el que el fenilo está sin sustituir o sustituido por al menos un sustituyente seleccionado entre el grupo constituido por un hidroxilo, un halógeno, un nitro, un ciano, un alquilo (C1-C3), un alcoxi (C1-C3), y un trifluorometilo; - n es 1 ó 2; - A es un cicloalquilo (C3-C15), un cicloalqueno (C3-C15), en el que el cicloalquilo o el cicloalqueno está sin sustituir o sustituido por al menos un alquilo (C1-C6); siempre que: 1/ cuando X es NR4 donde R4 es H o alquilo (C1-C6) y R1O es 6-OCH3, entonces Y no es CO; 2/ cuando X es O, R1O es 6-OH o 6-OCH3, Y es un enlace directo y A es ciclopentilo, entonces (R2,R3) o (R3,R2) es diferente de (H, Cl) en Posición 4,5; 3/ el compuesto no es

10. 发明专利

AT512952T 未知
公开(公告)号：AT512952T
公开(公告)日：2011-07-15
申请号：AT05794749
申请日：2005-10-14
申请人： THERAMEX
发明人： RONDOT BENOIT , LAFAY JEAN , BONNET PAULE , CLERC THIERRY , DUC IGOR , DURANTI ERIC , PUCCIO FRANCOIS , SHIELDS JACQUELINE , BLOT CHRISTIAN , MAILLOS PHILIPPE
IPC分类号： C07D231/56 , A61K31/416 , A61K31/4162 , A61K31/423 , C07D261/20 , C07D275/04 , C07D275/06 , C07D491/06
摘要： The present invention relates to compounds of formula (I): in which R 1 , R 2 , R 3 , X, Y and A are as defined in the specification. The compounds are modulators of the estrogen receptors.

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