公开(公告)号：EP0811006A1

公开(公告)日：1997-12-10

申请号：EP96902191.0

申请日：1996-02-20

申请人： ENDORECHERCHE INC.

发明人： LABRIE, Fernand ,  MERAND, Yves ,  GAUTHIER, Sylvain

IPC分类号： C07D405 ,  A61K31 ,  A61P35 ,  C07C215 ,  C07C217 ,  C07C235 ,  C07C317 ,  C07D215 ,  C07D217 ,  C07D295 ,  C07D311 ,  C07D335 ,  C07J1 ,  C07J17 ,  C07J21 ,  C07J41 ,  C07J51 ,  C07J53 ,  C07J71

CPC分类号： A61K31/10 ,  A61K31/135 ,  A61K31/138 ,  A61K31/165 ,  A61K31/35 ,  A61K31/352 ,  A61K31/38 ,  A61K31/382 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/445 ,  A61K31/4453 ,  A61K31/453 ,  A61K31/4535 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/472 ,  A61K31/4725 ,  C07C215/64 ,  C07C217/18 ,  C07C235/34 ,  C07C317/18 ,  C07C2602/10 ,  C07D215/14 ,  C07D217/16 ,  C07D295/088 ,  C07D295/096 ,  C07D295/185 ,  C07D311/60 ,  C07D335/06 ,  C07J1/0055 ,  C07J1/0059 ,  C07J1/007 ,  C07J1/0074 ,  C07J1/0085 ,  C07J17/00 ,  C07J21/006 ,  C07J21/008 ,  C07J41/0072 ,  C07J41/0094 ,  C07J51/00 ,  C07J53/008 ,  C07J71/001 ,  C07J71/0021

摘要： Certain benzopyran antiestrogens are disclosed for treating estrogen sensitive diseases such as breast cancer. Prodrug forms provide ease of manufacturing, good shelf life, and bioavailibility, and preferred stereoisomers are shown to be more effective than racemic mixtures.

摘要翻译： 公开了某些苯并吡喃抗雌激素用于治疗雌激素敏感性疾病如乳腺癌。 前药形式提供易于制造，良好的保质期和生物利用度。

公开(公告)号：EP0680327A1

公开(公告)日：1995-11-08

申请号：EP94904546.0

申请日：1994-01-19

申请人： ENDORECHERCHE INC.

发明人： LABRIE, Fernand

IPC分类号： A61K8 ,  A61K31 ,  A61P5 ,  A61P15 ,  A61P17 ,  A61P25 ,  A61Q19 ,  C07J1 ,  C07J43

CPC分类号： C07J43/006 ,  A61K31/565 ,  A61K31/566 ,  A61K31/5685 ,  A61K31/57 ,  A61K31/58 ,  C07J1/0011 ,  C07J43/003 ,  A61K2300/00

摘要： Sex steroid precursors such as dehydroepiandrosterone and dehydroepiandrosterone sulphate, and compounds converted in vivo to either of the foregoing, are utilized for the treatment and/or prevention of vaginal atrophy, hypogonadism, diminished libido, osteoporosis, urinary incontinence, ovarian cancer, uterine cancer, skin atrophy, for contraception, and, in combination with an estrogen and/or progestin, for the treatment of menopause. The precursors may be formulated for percutaneous or transmucosal administration. Gels, solutions, lotions, creams, ointments and transdermal patches for the administration of these presursors are provided, as are certain pharmaceutical compositions and kits which can be used for the prevention and treatment of a wide variety of conditions related to decreased secretion of sex steroid precursors by the adrenals.

公开(公告)号：EP0579607A1

公开(公告)日：1994-01-26

申请号：EP92902434.0

申请日：1992-01-13

申请人： ENDORECHERCHE INC.

发明人： LABRIE, Fernand

IPC分类号： G01N33 ,  C07K14

CPC分类号： G01N33/57438

摘要： Procédé permettant de dépister la présence éventuelle d'un cancer de la prostate, qui consiste à mesurer la concentration en antigène spécifique de prostate dans le sérum (PSA) et à comparer ladite concentration à une certaine valeur seuil, de manière à pouvoir identifier une sous-catégorie de la population masculine présentant un risque élevé de cancer de la prostate, et entamer des procédures de diagnostic plus approfondies pour confirmer ou infirmer le diagnostic de cancer de la prostate.

公开(公告)号：EP1899305B1

公开(公告)日：2018-12-12

申请号：EP06752811.7

申请日：2006-06-16

申请人： ENDORECHERCHE INC.

发明人： LABRIE, Fernand ,  BRETON, Rock ,  SINGH, Shankar, Mohan ,  MALTAIS, Rene

IPC分类号： C07D233/42 ,  A61K31/4178 ,  A61K31/4166 ,  A61K31/5377 ,  C07D403/12 ,  C07D413/12 ,  A61P5/24

CPC分类号： C07D417/12 ,  C07D207/40 ,  C07D211/48 ,  C07D233/74 ,  C07D233/86

摘要： Compounds having the structure (or their salts): are used to treat or reduce the likelihood of acquiring androgen-dependent diseases, such as prostate cancer, benign prostatic hyperplasia, polycystic ovarian syndrome, acne, hirsutism, seborrhea, androgenic alopecia and male baldness. The compounds can be formulated together with pharmaceutically acceptable diluents or carriers or otherwise made into any pharmaceutical dosage form. Combinations with other active pharmaceutical agents are also disclosed.

公开(公告)号：EP3083590A1

公开(公告)日：2016-10-26

申请号：EP14872056.8

申请日：2014-12-16

申请人： Endorecherche, Inc.

发明人： LABRIE, Fernand ,  SINGH, Shankar Mohan ,  LABRECQUE, Richard ,  CIOBANU, Liviu Constantin

IPC分类号： C07D401/12 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/517 ,  A61P35/00 ,  A61P5/26 ,  C07D233/74 ,  C07D401/14 ,  C07D403/12

CPC分类号： C07D403/12 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/506 ,  A61K31/517 ,  A61K31/58 ,  A61K38/09 ,  A61K45/06 ,  C07D401/12 ,  C07D401/14 ,  A61K2300/00

摘要： Compounds having the structure or their salts: are used to treat or reduce le likelihood of acquiring androgen-dependent diseases, such as prostate cancer, benign prostatic hyperplasia, polycystic ovarian syndrome, acne, hirsutism, seborrhea, androgenic alopecia, male baldness, muscle atrophy and weakness, sarcopenia, male hypogonadism, erectile dysfunction, female sexual dysfunction and osteoporosis. They can be formulated together with pharmaceutically acceptable diluent or carrier or otherwise made into any pharmaceutical dosage form. Combinations with other active pharmaceutical agents are also disclosed.

公开(公告)号：EP1802312B1

公开(公告)日：2015-09-16

申请号：EP05797148.3

申请日：2005-10-20

申请人： ENDORECHERCHE INC.

发明人： EL-ALFY, Mohamed ,  LABRIE, Fernand ,  BERGER, Louise

IPC分类号： A61K31/5685 ,  A61K31/566 ,  A61K31/453 ,  A61K31/519 ,  A61P15/02

CPC分类号： A61K31/5685 ,  A61K31/453 ,  A61K31/519 ,  A61K31/566

公开(公告)号：EP2386305B9

公开(公告)日：2014-12-17

申请号：EP11174933.9

申请日：1999-06-10

申请人： ENDORECHERCHE INC.

发明人： Labrie, Fernand

IPC分类号： A61P21/00 ,  A61K31/565 ,  A61K45/06 ,  A61P3/06 ,  A61P9/00 ,  A61P19/10

CPC分类号： A61K31/565 ,  A61K31/57 ,  A61K31/66 ,  A61K45/06 ,  A61K31/445 ,  A61K31/41 ,  A61K31/40 ,  A61K31/38 ,  A61K31/135 ,  A61K2300/00

公开(公告)号：EP2386304A2

公开(公告)日：2011-11-16

申请号：EP11174925.5

申请日：1999-06-10

申请人： ENDORECHERCHE INC.

发明人： Labrie, Fernand

IPC分类号： A61K31/565 ,  A61K45/06 ,  A61P3/06 ,  A61P9/00 ,  A61P19/10

CPC分类号： A61K31/565 ,  A61K31/57 ,  A61K31/66 ,  A61K45/06 ,  A61K31/445 ,  A61K31/41 ,  A61K31/40 ,  A61K31/38 ,  A61K31/135 ,  A61K2300/00

摘要： Novel methods for the medical treatment and/or inhibition of the development of breast cancer, hypercholesterolemia, hyperlipidemia or atherosclerosis in susceptible warm-blooded animals including humans involving administration of selective estrogen receptor modulator and an amount of a sex steroid precursor selected from the group consisting of dehydroepiandrosterone, dehydroepiandrosterone sulfate, androst-5-ene-3ß,17ß-diol, and compounds converted in vivo to one of the foregoing precursors.
Further administration of bisphosphonates in combination with selective estrogen receptor modulators and/or sex steroid precursors is disclosed. Pharmaceutical compositions for delivery of active ingredients and kits useful to the invention are disclosed.

公开(公告)号：EP1731157A3

公开(公告)日：2009-07-15

申请号：EP06018947.9

申请日：1999-06-10

申请人： Endorecherche, Inc.

发明人： Labrie, Fernand

IPC分类号： A61K31/565 ,  A61P15/08 ,  A61P15/12 ,  A61P13/00 ,  A61P17/00

CPC分类号： A61K31/568 ,  A61K31/565 ,  A61K2300/00

摘要： Androst-5-ene3ß,17ß-diol is used to treat or reduce menopausal symptoms, or other diseases affected by estrogen receptor activity, and for conditions which respond well to DHEA treatment, but where a higher ratio of estrogenic to androgenic effects is desired. Combination therapies are included, as are kits and pharmaceutical compositions for providing the active ingredients of claimed methods and combinations.
The indication is selected from the group consisting of hypogonadism, skin atrophy, skin dryness, diminished libido, and urinary incontinence.

公开(公告)号：EP1083905B1

公开(公告)日：2005-11-02

申请号：EP99955419.9

申请日：1999-06-10

申请人： ENDORECHERCHE INC.

发明人： LABRIE, Fernand

IPC分类号： A61K31/565 ,  A61P19/10

CPC分类号： A61K31/565 ,  A61K31/57 ,  A61K31/66 ,  A61K45/06 ,  A61K31/445 ,  A61K31/41 ,  A61K31/40 ,  A61K31/38 ,  A61K31/135 ,  A61K2300/00

摘要： Novel methods for the medical treatment and/or inhibition of the development of breast cancer, hypercholesterolemia, hyperlipidemia or atherosclerosis in susceptible warmblooded animals including humans involving administration of selective estrogen receptor modulator and an amount of a sex steroid precursor selected from the group consisting of dehydroepiandrosterone, dehydroepiandrosterone sulfate, androst-5-ene-3²,17²-diol, and compounds converted in vivo to one of the foregoing precursors. Further administration of bisphosphonates in combination with selective estrogen receptor modulators and/or sex steroid precursors is disclosed. Pharmaceutical compositions for delivery of active ingredients and kits useful to the invention are disclosed.

摘要翻译： 用于治疗和/或抑制涉及施用选择性雌激素受体调节剂的敏感温血动物（包括人）中的乳腺癌，高胆固醇血症，高脂血症或动脉粥样硬化发展的新方法，以及选自脱氢表雄酮 ，脱氢表雄酮硫酸酯，雄甾-5-烯-3,2α-二醇，以及在体内转化成前述前体之一的化合物。 公开了将二膦酸盐与选择性雌激素受体调节剂和/或性类固醇前体组合的进一步给药。 公开了用于递送用于本发明的活性成分和试剂盒的药物组合物。