专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2008048540A3 2-HYDROXY-2-PHENYL/THIOPHENYL PROPIONAMIDES AS ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：作为雄激素受体调节剂的2-羟基-2-苯基/噻吩基丙酰胺
公开(公告)号：WO2008048540A3
公开(公告)日：2008-08-14
申请号：PCT/US2007021984
申请日：2007-10-15
申请人： MERCK & CO INC , KIM YUNTAE , MEISSNER ROBERT S , MITCHELL HELEN J , PERKINS JAMES J , ROSSI MICHAEL A , WANG JIABING
发明人： KIM YUNTAE , MEISSNER ROBERT S , MITCHELL HELEN J , PERKINS JAMES J , ROSSI MICHAEL A , WANG JIABING
IPC分类号： A01N43/54 , A61K31/497 , A61K31/517
CPC分类号： C07D213/40 , C07D409/12
摘要： Compounds of structural formula (I) are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid- induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HFV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), abdominal adiposity, metabolic syndrome, type II diabetes, cancer cachexia, Alzheimer's disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.
摘要翻译：结构式（I）的化合物以组织选择性方式是雄激素受体（AR）的调节剂。这些化合物可用于增强肌肉张力减弱和由雄激素缺乏引起的病症的治疗，或可通过施用雄激素改善，包括骨质疏松症，骨质减少症，糖皮质激素诱导的骨质疏松症，牙周病，骨折，骨重建后的骨损伤女性绝经后症状，动脉粥样硬化，高胆固醇血症，高脂血症，肥胖症，再生障碍性贫血和其他造血障碍，炎性关节炎和关节修复，HFV消瘦，前列腺癌，良性前列腺增生症（BPH）），腹部肥胖，代谢综合征，II型糖尿病，癌症恶病质，阿尔茨海默氏病，肌营养不良，认知衰退，性功能障碍，睡眠呼吸暂停，抑郁症，卵巢早衰和自身免疫疾病，单独或与其他活性剂组合。

2. 发明申请

WO2005120477A3 N- (2-BENZYL) -2-PHENYLBUTANAMIDES AS ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译： N-（2-苄基）-2-苯基黄烷作为雄激素受体调节剂
公开(公告)号：WO2005120477A3
公开(公告)日：2006-03-02
申请号：PCT/US2005019554
申请日：2005-06-03
申请人： MERCK & CO INC , HANNEY BARBARA , KIM YUNTAE , KROUT MICHAEL R , MEISSNER ROBERT S , MITCHELL HELEN J , MUSSELMAN JEFFREY , PERKINS JAMES J , WANG JIABING
发明人： HANNEY BARBARA , KIM YUNTAE , KROUT MICHAEL R , MEISSNER ROBERT S , MITCHELL HELEN J , MUSSELMAN JEFFREY , PERKINS JAMES J , WANG JIABING
IPC分类号： A61K31/00 , A61K31/165 , A61K31/277 , A61K31/44 , C07C233/13 , C07C235/34 , C07C271/12 , C07D213/61 , C07D295/205 , A61P5/26 , C07C235/06
CPC分类号： C07D295/205 , C07C233/13 , C07C235/34 , C07C255/60 , C07C271/12 , C07C271/22 , C07C2601/02 , C07D213/61 , C07D213/73
摘要： Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), abdominal adiposity, metabolic syndrome, type II diabetes, cancer cachexia, Alzhheiner's disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.
摘要翻译：结构式I的化合物是以组织选择性方式的雄激素受体（AR）的调节剂。这些化合物可用于增强减弱的肌肉紧张度和治疗由雄激素缺乏引起的或由雄激素施用引起的疾病的治疗，包括骨质疏松症，骨质减少，糖皮质激素诱导的骨质疏松症，牙周病骨折，骨重建手术后的骨损伤，肌肉减少，脆弱，老化的皮肤，男性性腺机能减退，女性绝经后症状，动脉粥样硬化，高胆固醇血症，高脂血症，肥胖，再生障碍性贫血和其他造血障碍，炎症性关节炎和关节修复，艾滋病毒消耗，前列腺癌，良性前列腺增生（BPH），腹部肥胖，代谢综合征，II型糖尿病，癌症恶病质，Alzhheiner病，肌营养不良症，认知衰退，性功能障碍，睡眠呼吸暂停，抑郁症，卵巢早衰以及自身免疫性疾病，单独或与其他活性剂组合。

3. 发明申请

WO03059293A3 17-HYDROXY-4-AZA-ANDROSTAN-3-ONES AS ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：作为雄激素受体调节剂的17-羟基-4-安非他酮-3-
公开(公告)号：WO03059293A3
公开(公告)日：2004-07-22
申请号：PCT/US0300874
申请日：2003-01-10
申请人： MERCK & CO INC , DANKULICH WILLIAM P , MEISSNER ROBERT S , MITCHELL HELEN J , PERKINS JAMES J
发明人： DANKULICH WILLIAM P , MEISSNER ROBERT S , MITCHELL HELEN J , PERKINS JAMES J
IPC分类号： A61K31/473 , A61K31/58 , A61K45/06 , A61P1/02 , A61P3/04 , A61P3/06 , A61P5/26 , A61P7/06 , A61P9/10 , A61P15/00 , A61P15/10 , A61P17/16 , A61P19/00 , A61P19/02 , A61P19/10 , A61P21/00 , A61P35/00 , C07J73/00 , A61K31/56
CPC分类号： C07J73/005 , A61K31/473 , A61K31/58 , A61K45/06 , A61K2300/00
摘要： Compounds of structural formula I as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of activating the function of the androgen receptor in a patient, and in particular the method wherein the function of the androgen receptor is blocked in the prostate of a male patient or in the uterus of a female patient and activated in bone and/or muscle tissue. These compounds are useful in the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, female sexual dysfunction, post-menopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal cancer, prostate cancer, arthritis and joint repair, alone or in combination with other active agents.
摘要翻译：公开了本文定义的结构式I化合物，其可用于在需要这种调节的患者中以组织选择性方式调节雄激素受体的方法，以及在一种激活雄激素受体的功能的方法中特别是其中雄性患者的前列腺中或在女性患者的子宫中阻断雄激素受体的功能并在骨和/或肌肉组织中活化的方法。这些化合物可用于治疗由雄激素缺乏引起的疾病或可通过雄激素给药改善的疾病，包括骨质疏松症，牙周病，骨折，骨重建手术后的骨损伤，肌肉减少症，虚弱，衰老皮肤，男性性腺机能减退，女性性功能障碍，妇女绝经后症状，动脉粥样硬化，高胆固醇血症，高脂血症，肥胖症，再生障碍性贫血和其他造血障碍，胰腺癌，肾癌，前列腺癌，关节炎和关节修复，单独或与其他活性剂组合。

4. 发明申请

WO2007038444A3 N-(4-OXO-3,4-DIHYDROQUINAZOLIN-2-YL)BUTANAMIDES AS ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译： N-（4-氧代-3,4-二氢喹唑啉-2-基）丁酸钠作为雄激素受体调节剂
公开(公告)号：WO2007038444A3
公开(公告)日：2007-08-09
申请号：PCT/US2006037273
申请日：2006-09-22
申请人： MERCK & CO INC , HANNEY BARBARA , KIM YUNTAE , MITCHELL HELEN J , MUSSELMAN JEFFREY D , PERKINS JAMES J
发明人： HANNEY BARBARA , KIM YUNTAE , MITCHELL HELEN J , MUSSELMAN JEFFREY D , PERKINS JAMES J
IPC分类号： A61K31/517 , C07D239/90
CPC分类号： C07D403/06 , C07D239/90 , C07D409/12
摘要： The invention relates to substituted N-(4-oxo-3,4-dihydroquinazolin-2-yl)butanamid derivatives which modulate androgen receptors to treat conditions such as: osteoporosis, peridontal disease, bone fracture, frailty, and sarcopenia.
摘要翻译：本发明涉及调节雄激素受体以治疗诸如骨质疏松症，肠周周疾病，骨折，虚弱和肌肉减少症之类的病症的取代的N-（4-氧代-3,4-二氢喹唑啉-2-基）丁酰胺衍生物。

5. 发明申请

WO0072801A3 ALPHA V INTEGRIN RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO0072801A3
公开(公告)日：2007-10-11
申请号：PCT/US0014901
申请日：2000-05-30
申请人： MERCK & CO INC , COLEMAN PAUL J , DUGGAN MARK E , HALCZENKO WASYL , HARTMAN GEORGE D , HUTCHINSON JOHN H , MEISSNER ROBERT S , PATANE MICHAEL A , PERKINS JAMES J , WANG JIABING , BRESLIN MICHAEL J
发明人： COLEMAN PAUL J , DUGGAN MARK E , HALCZENKO WASYL , HARTMAN GEORGE D , HUTCHINSON JOHN H , MEISSNER ROBERT S , PATANE MICHAEL A , PERKINS JAMES J , WANG JIABING , BRESLIN MICHAEL J
IPC分类号： C07D239/48 , A61K31/437 , A61K31/4375 , A61K31/4709 , A61K31/498 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/536 , A61K31/55 , A61P9/00 , A61P9/08 , A61P9/10 , A61P17/00 , A61P19/08 , A61P19/10 , A61P27/02 , A61P29/00 , A61P31/12 , A61P35/00 , A61P35/04 , A61P43/00 , C07D213/02 , C07D221/00 , C07D223/14 , C07D239/24 , C07D241/36 , C07D265/28 , C07D401/06 , C07D471/02 , C07D471/04 , C07D519/00
CPC分类号： C07D239/48 , C07D401/06 , C07D471/04
摘要： The present invention relates to novel nonanoic acid derivatives, their synthesis, and their use as alphaV integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors alphaV beta3 and alphaV beta5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.
摘要翻译：本发明涉及新型的壬酸衍生物，它们的合成及其作为αV整联蛋白受体拮抗剂的用途。更具体地说，本发明的化合物是整联蛋白受体αVβ3和αVβ5的拮抗剂，可用于抑制骨吸收，治疗和预防骨质疏松症，抑制血管再狭窄，糖尿病性视网膜病变，黄斑变性，血管发生，动脉粥样硬化，炎症，炎症性关节炎，病毒性疾病，癌症和转移性肿瘤生长。

6. 发明申请

WO2004100874A3 ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：雄激素受体调节剂及其使用方法
公开(公告)号：WO2004100874A3
公开(公告)日：2006-01-26
申请号：PCT/US2004013787
申请日：2004-05-03
申请人： MERCK & CO INC , MEISSNER ROBERT S , PERKINS JAMES J
发明人： MEISSNER ROBERT S , PERKINS JAMES J
IPC分类号： A61K20060101 , A61K31/00 , A61K31/56
CPC分类号： A61K31/58 , C07J73/005
摘要： Compounds of structural formula (I) as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of agonizing the androgen receptor in a patient, and in particular the method wherein the androgen receptor is antagonized in the prostate of a male patient or in the uterus of a female patient and agonized in bone and/or muscle tissue. These compounds are useful in the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including: osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, post-menopausal symptoms in women, female sexual dysfunction, atherosclerosis, hypercholesterolemia, hyperlipidemia, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal cancer, arthritis and joint repair, alone or in combination with other active agents. In addition, these compounds are useful as pharmaceutical composition ingredients alone and in combination with other active agents.
摘要翻译：公开了本文定义的结构式（I）的化合物可用于在需要这种调节的患者中以组织选择性方式调节雄激素受体的方法，以及在患者中激动雄激素受体的方法，特别是其中雄性受体在男性患者的前列腺或女性患者的子宫中被拮抗并在骨和/或肌肉组织中激动的方法。这些化合物可用于治疗由雄激素缺乏引起的或可由雄激素施用而改善的病症，包括：骨质疏松症，牙周病，骨折，骨重建手术后的骨损伤，肌肉减少症，虚弱，衰老皮肤，男性性腺机能减退妇女的绝经症状，女性性功能障碍，动脉粥样硬化，高胆固醇血症，高脂血症，再生障碍性贫血和其他造血障碍，胰腺癌，肾癌，关节炎和关节修复，单独或与其他活性剂组合。此外，这些化合物可单独用作药物组合物成分并与其它活性剂组合使用。

7. 发明申请

WO2008060391A2 2-[1-PHENYL-5-HYDROXY OR METHOXY-4ALPHA-METHYL-HEXAHYDROCYCLOPENTA [F]INDAZOL-5-YL]ETHYL PHENYL DERIVATIVES AS GLUCOCORTICOID RECEPTOR LIGANDS 审中-公开
标题翻译： 2- [1-苯基-5-羟基或甲氧基-4-甲基 - 甲基 - 六氢环戊二烯并[F]吲哚-5-基]乙酰苯衍生物作为葡萄糖激动剂受体配体
公开(公告)号：WO2008060391A2
公开(公告)日：2008-05-22
申请号：PCT/US2007022449
申请日：2007-10-23
申请人： MERCK & CO INC , BUNGARD CHRISTOPHER J , MANIKOWSKI JESSE J , PERKINS JAMES J , MEISSNER ROBERT
发明人： BUNGARD CHRISTOPHER J , MANIKOWSKI JESSE J , PERKINS JAMES J , MEISSNER ROBERT
CPC分类号： C07D231/54 , C07D401/10 , C07D403/10 , C07D405/10
摘要： The present invention is directed to 2-[l-phenyl-5-hydroxy-4alpha-methyl- hexahydrocyclopenta[f]indazol-5-yl]ethyl phenyl derivatives as glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.
摘要翻译：本发明涉及作为用于治疗各种自身免疫性和炎性疾病或病症的糖皮质激素受体配体的2- [1-苯基-5-羟基-4α-甲基 - 六氢环戊并[f]吲唑-5-基]乙基苯基衍生物。还包括药物组合物和使用方法。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式