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41. 发明专利

CA2689080C TREATING BENIGN PROSTATE HYPERPLASIA WITH SARMS 未知
公开(公告)号：CA2689080C
公开(公告)日：2011-07-05
申请号：CA2689080
申请日：2003-02-06
申请人： UNIV TENNESSEE RES FOUNDATION
发明人： STEINER MITCHELL S , VEVERKA KAREN A , MILLER DUANE D , DALTON JAMES T , GAO WENQING
IPC分类号： A61K45/00 , C07C255/60 , A61K31/00 , A61K31/167 , A61K31/277 , A61K31/56 , A61P13/08 , A61P43/00
摘要： This invention provides a method of treating, preventing, suppressing, inhibiting or reducing the incidence of benign prostate hyperplasia in a male subject, by administering to the subject a selective androgen receptor modulator (SARM) and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof as described herein. This invention also provides a method of treating a subject suffering from hair loss, comprising the step of administering to the subject a therapeutically effective amount of a 5-a reductase enzyme type 1 and /or type 2 inhibitor, wherein said inhibitor is a selective androgen receptor modulator (SARM) and/or its analog, derivative, isomer, metabolite,pharmaceutically acceptable salt, pharmaceutical product, hydrate, Woxide, or any combination thereof as described herein.; This invention also provides a method of inhibiting a 5-a reductase type 1 and/or type 2 enzyme, comprising contacting the enzyme with an effective 5-a reductase inhibitory amount of a selective androgen receptor modulator (SARM) and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof, as described herein.

42. 发明专利

CA2538095C SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 未知
公开(公告)号：CA2538095C
公开(公告)日：2009-12-22
申请号：CA2538095
申请日：2003-10-14
申请人： UNIV TENNESSEE RES FOUNDATION
发明人： YIN DONGHUA , MILLER DUANE D , STEINER MITCHELL S , HE YALI , DALTON JAMES T , VEVERKA KAREN A
IPC分类号： C07C255/60 , A61K31/165 , A61K31/277 , A61K31/404 , A61K31/4706 , A61K31/661 , A61P5/26 , A61P15/16 , A61P35/00 , C07C235/16 , C07C235/24 , C07C335/18 , C07D209/08 , C07D215/22 , C07D215/227 , C07D271/12
摘要： This invention provides a class of androgen receptor targeting agents (ARTA) . The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. The SARM compounds, either alone or as a composition, are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Femal e (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopeni a, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatmen t and/or prevention of acute and/or chronic muscular wasting conditions; e) preventin g and/or treating dry eye conditions; f) oral androgen replacement therapy; g) decreasing the incidence of, halting or causing a regression of prostate cancer; and/or h) inducing apoptosis in a cancer cell.

43. 发明专利

HK1082724A1 LARGE-SCALE SYNTHESIS OF SELECTIVE ANDROGEN RECEPTOR MODULATORS 未知
公开(公告)号：HK1082724A1
公开(公告)日：2006-06-16
申请号：HK06104418
申请日：2006-04-11
申请人： UNIV TENNESSEE RES FOUNDATION
发明人： STEINER MITCHELL S , CHUNG KIWON , DALTON JAMES , MILLER DUANE D , VEVERKA KAREN A
IPC分类号： C07C20060101 , C07C231/12 , C07C235/24

44. 发明专利

CA2538095A1 SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 未知
公开(公告)号：CA2538095A1
公开(公告)日：2004-04-29
申请号：CA2538095
申请日：2003-10-14
申请人： UNIV TENNESSEE RES FOUNDATION
发明人： MILLER DUANE D , DALTON JAMES T , STEINER MITCHELL S , YIN DONGHUA , HE YALI , VEVERKA KAREN A
IPC分类号： C07C255/60 , A61K31/165 , A61K31/277 , A61K31/404 , A61K31/4706 , A61K31/661 , A61P5/26 , A61P15/16 , A61P35/00 , C07C235/16 , C07C235/24 , C07C335/18 , C07D209/08 , C07D215/22 , C07D215/227 , C07D271/12
摘要： This invention provides a class of androgen receptor targeting agents (ARTA) . The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. The SARM compounds, either alone or as a composition, are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Femal e (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopeni a, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatmen t and/or prevention of acute and/or chronic muscular wasting conditions; e) preventin g and/or treating dry eye conditions; f) oral androgen replacement therapy; g) decreasing the incidence of, halting or causing a regression of prostate cancer; and/or h) inducing apoptosis in a cancer cell.

45. 发明专利

DK1592658T3 Syntese af selektive, androgene receptormodulatorer i stor målestok 未知
公开(公告)号：DK1592658T3
公开(公告)日：2013-07-29
申请号：DK04701496
申请日：2004-01-12
申请人： UNIV TENNESSEE RES FOUNDATION
发明人： STEINER MITCHELL S , CHUNG KIWON , DALTON JAMES , MILLER DUANE D , VEVERKA KAREN A
IPC分类号： C07C231/12 , C07C231/00 , C07C235/24

46. 发明专利

CA2513242C LARGE-SCALE SYNTHESIS OF SELECTIVE ANDROGEN RECEPTOR MODULATORS 未知
公开(公告)号：CA2513242C
公开(公告)日：2013-07-09
申请号：CA2513242
申请日：2004-01-12
申请人： UNIV TENNESSEE RES FOUNDATION
发明人： DALTON JAMES , MILLER DUANE D , VEVERKA KAREN A
IPC分类号： C07C231/12 , A61K31/167 , A61K31/277 , C07C235/24 , C07C253/30 , C07C255/60
摘要： The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM), represented in one aspect by general formula I: (see formula I)

49. 发明专利

EA011744B1 ГАЛОГЕНИРОВАННЫЕ СЕЛЕКТИВНЫЕ МОДУЛЯТОРЫ АНДРОГЕНОВЫХ РЕЦЕПТОРОВ И СПОСОБЫ ИХ ПРИМЕНЕНИЯ 未知
公开(公告)号：EA011744B1
公开(公告)日：2009-06-30
申请号：EA200500648
申请日：2003-10-14
申请人： UNIV TENNESSEE RES FOUNDATION
发明人： DALTON JAMES T , MILLER DUANE D , YIN DONGHUA , HE YALI , STEINER MITCHELL S , VEVERKA KAREN A
IPC分类号： C07C233/05 , A61K31/165 , A61K31/275 , A61K31/404 , A61K31/4706 , A61K31/661 , C07C235/16 , C07C235/24 , C07C255/50 , C07C255/60 , C07C335/18 , C07D209/08 , C07D215/22 , C07D215/227 , C07D271/12
摘要： Настоящееизобретениепредставляетклассвеществформулыгде X означает O, CH, NH, Se, PR, NO или NR; T означает OH, OR, -NHCOCHили NHCOR; Z означает CN, COOH, COR, NHCOR или CONHR; Y означает CF, I, Br, Cl, CN, CRили Sn(R)либо Z и Y вместес бензольнымкольцом, ккоторомуониприкреплены, образуютконденсированнуюбициклическую, карбоциклическуюилигетероциклическую, кольцевуюсистему; Q означает F; R означаеталкил, галоалкил, дигалоалкил, тригалоалкил, CHF, CHF, CF, CFCF, арил, фенил, F, Cl, Br, I, алкенилилиОНи RозначаетСН, CHF, CHF, CF, СНСНили CFCF, направленныхнаандрогеновыерецепторы (ARTA). Этивеществаопределяютновыйподкласссоединений, являющихсяселективнымимодуляторамиандрогеновыхрецепторов (SARM). Некоторыесоединения SARM, какоказалось, обладаютнеожиданнойандрогеннойи анаболическойактивностьюнестероидныхлигандовандрогеновыхрецепторов. Другиесоединения SARM, какоказалось, обладаютнеожиданнойантиандрогеннойактивностьюнестероидныхлигандовандрогеновыхрецепторов. Соединения SARM, самипосебеилив видекомпозиции, применимыдляа) мужскойконтрацепции; b) леченияцелогорядагормонзависимыхрасстройств, напримеррасстройств, связанныхс возрастнымснижениемуровняандрогенову мужчин (ADAM), такихкакусталость, депрессия, пониженноелибидо, половаядисфункция, нарушенияэрекции, гипогонадизм, остеопороз, выпадениеволос, анемия, ожирение, саркопения, остеопения, доброкачественнаягиперплазияпростаты, изменениянастроенияи сознанияи ракпростаты; с) лечениярасстройств, связанныхсоснижениемуровняандрогенову женщин (ADIF), такихкакполоваядисфункция, пониженноесексуальноелибидо, гипогонадизм, саркопения, остеопения, остеопороз, измененияв сознаниии настроении, депрессия, анемия, выпадениеволос, ожирение, эндометриоз, ракмолочной

50. 发明专利

HRP20070457A2 HALOGENATED SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 未知
公开(公告)号：HRP20070457A2
公开(公告)日：2008-05-31
申请号：HRP20070457
申请日：2007-10-01
申请人： UNIV TENNESSEE RES FOUNDATION
发明人： DALTON JAMES T , MILLER DUANE D , YIN DONGHUA , HE YALI , STEINER MITCHELL S , VEVERKA KAREN A
IPC分类号： C07C233/05 , A61K31/165 , A61K31/275 , A61K31/404 , A61K31/4706 , A61K31/661 , C07C235/16 , C07C235/24 , C07C255/50 , C07C255/60 , C07C335/18 , C07D209/08 , C07D215/22 , C07D215/227 , C07D271/12
摘要： Selective androgen receptor modulator (SARM) compounds having the formula Ia: wherein X is O; T is OH, OR, -NHCOCH 3 , or NHCOR; Z is CN; Y is CF 3 , I, Br, Cl, CN, C(R) 3 or Sn(R) 3 ; or Z and Y together with the benzene ring to which they are attached form a fused bicyclic carbocyclic or heterocyclic ring system; Q is F, Cl, Br or I; R is alkyl, haloalkyl, dihaloalkyl, trihaloalkyl, CH 2 F, CHF 2 , CF 3 , CF 2 CF 3 , aryl, phenyl, F, Cl, Br, I, alkenyl or OH; and R 1 is CH 3 , CH 2 F, CHF 2 , CF 3 , CH 2 CH 3 , or CF 2 CF 3 ; can be used in the treatment of osteoporosis, osteopenia, low bone mass, bone fragility, osteomalacia, or any combination thereof, a male subject having an Androgen Decline in Aging Male (ADAM)-associated condition, or a female subject having an Androgen Decline in Female (ADIF)-associated condition, in a subject.

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