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1. 发明申请

WO2010114780A1 INHIBITORS OF AKT ACTIVITY 审中-公开
标题翻译： AKT活动的抑制剂
公开(公告)号：WO2010114780A1
公开(公告)日：2010-10-07
申请号：PCT/US2010/028989
申请日：2010-03-29
申请人： MERCK SHARP & DOHME CORP. , CHEN, Qi , CUI, Mingziang , HU, Bin , HU, Shuangxi , PU, Zhifa , SANDERSON, Philip, E. , SOLL, Richard , TANG, Xue , WANG, Jiabing , YAN, Yongjin , YAO, Jinfeng , ZHANG, Hongjie
发明人： CHEN, Qi , CUI, Mingziang , HU, Bin , HU, Shuangxi , PU, Zhifa , SANDERSON, Philip, E. , SOLL, Richard , TANG, Xue , WANG, Jiabing , YAN, Yongjin , YAO, Jinfeng , ZHANG, Hongjie
IPC分类号： A61K31/44
CPC分类号： A61K31/44 , C07D487/04
摘要： The instant invention provides for substituted fused pyrimidine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
摘要翻译：本发明提供抑制Akt活性的取代的稠合嘧啶化合物。特别地，所公开的化合物选择性地抑制一种或两种Akt同种型。本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制Akt活性的方法。

2. 发明申请

WO2003026568A3 ANDROSTANES AS ANDROGEN RECEPTOR MODULATORS 审中-公开
公开(公告)号：WO2003026568A3
公开(公告)日：2003-04-03
申请号：PCT/US2002/029436
申请日：2002-09-17
申请人： MERCK & CO., INC. , WANG, Jiabing
发明人： WANG, Jiabing
IPC分类号： A61K31/56
摘要： Compounds of structural formula (I) as herein defined are disclosed as useful in a method for modulating a function of 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 osteopenia, osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, female sexual dysfunction, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal cancer, prostate cancer, inflammatory arthritis and joint repair, alone or in combination with other active agents.

3. 发明申请

WO2011130921A1 INHIBITORS OF AKT ACTIVITY 审中-公开
标题翻译： AKT活动的抑制剂
公开(公告)号：WO2011130921A1
公开(公告)日：2011-10-27
申请号：PCT/CN2010/072132
申请日：2010-04-23
申请人： MERCK SHARP & DOHME CORP. , BANYU PHARMACEUTICAL CO., LTD. , LIANG, Peng , MITSUYA, Morihiro , OGINO, Yoshio , QI, Changhe , TAKAHASHI, Hidekazu , TEMPEST, Paul , WANG, Jiabing , WANG, Zhenzhen , ZHANG, Shaohua , ZHOU, Nanyan , ZHU, Jiuxiang
发明人： LIANG, Peng , MITSUYA, Morihiro , OGINO, Yoshio , QI, Changhe , TAKAHASHI, Hidekazu , TEMPEST, Paul , WANG, Jiabing , WANG, Zhenzhen , ZHANG, Shaohua , ZHOU, Nanyan , ZHU, Jiuxiang
IPC分类号： C07D417/04 , C07D277/20 , A61K31/426 , A61K31/427 , A61P35/00
CPC分类号： C07D417/12 , C07D277/28 , C07D277/30 , C07D277/42 , C07D277/52 , C07D277/56 , C07D417/04 , C07D417/14
摘要： The instant invention provides for substituted thiazoles that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
摘要翻译：本发明提供抑制Akt活性的取代的噻唑。特别地，所公开的化合物选择性地抑制一种或两种Akt同种型。本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制Akt活性的方法。

4. 发明申请

WO2009148916A1 INHIBITORS OF AKT ACTIVITY 审中-公开
标题翻译： AKT活动的抑制剂
公开(公告)号：WO2009148916A1
公开(公告)日：2009-12-10
申请号：PCT/US2009/045456
申请日：2009-05-28
申请人： MERCK & CO., INC. , BANYU PHARMACEUTICAL CO., LTD. , FURUYAMA, Hidetomo , GOTO, Yasuhiro , KAWANISHI, Nobuhiko , LAYTON, Mark, E. , MITA, Takashi , NAYA, Akira , OGINO, Yoshio , ONOZAKI, Yu , RODZINAK, Kevin, J. , SAKAMOTO, Toshihiro , SANDERSON, Philip, E. , WANG, Jiabing
发明人： FURUYAMA, Hidetomo , GOTO, Yasuhiro , KAWANISHI, Nobuhiko , LAYTON, Mark, E. , MITA, Takashi , NAYA, Akira , OGINO, Yoshio , ONOZAKI, Yu , RODZINAK, Kevin, J. , SAKAMOTO, Toshihiro , SANDERSON, Philip, E. , WANG, Jiabing
IPC分类号： A61K31/44 , A61K31/52
CPC分类号： C07D471/14
摘要： The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms, preferably Akt1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity especially Akt1 by administering the compound to a patient in need of treatment of cancer.
摘要翻译：本发明提供抑制Akt活性的取代的萘啶化合物。特别地，所公开的化合物选择性地抑制一种或两种Akt同种型，优选Akt1。本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制Akt活性，尤其是Akt1的方法。

5. 发明申请

WO2008048540A2 2-HYDROXY-2-PHENYL/THIOPHENYL PROPIONAMIDES AS ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译： 2-羟基-2-苯基/噻吩并噻唑类作为雄激素受体调节剂
公开(公告)号：WO2008048540A2
公开(公告)日：2008-04-24
申请号：PCT/US2007/021984
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： A61K31/4436
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疾病或可由雄激素给药改善的情况，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，骨重建后的骨损伤手术，肌肉减少症，虚弱，衰老皮肤，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，炎性关节炎和关节修复，HFV消耗，前列腺癌，良性前列腺增生），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，肌营养不良症，认知衰退，性功能障碍，睡眠呼吸暂停，抑郁症，早期卵巢衰竭和自身免疫性疾病，单独或与其它活性剂组合。

6. 发明申请

WO2003029268A1 ANDROSTANE 17-BETA-CARBOXAMIDES AS ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：安哥拉17-β-羧酰胺作为雄激素受体调节剂
公开(公告)号：WO2003029268A1
公开(公告)日：2003-04-10
申请号：PCT/US2002/030864
申请日：2002-09-27
申请人： MERCK & CO., INC. , WANG, Jiabing , DUGGAN, Mark, E. , WHITMAN, David, B.
发明人： WANG, Jiabing , DUGGAN, Mark, E. , WHITMAN, David, B.
IPC分类号： C07J3/00
CPC分类号： A61K31/568 , A61K31/56 , A61K31/663 , C07J3/00 , A61K2300/00
摘要： Compounds of structural formula 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, 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，以及在患者中激活雄激素受体的功能的方法特别是其中雄性患者的前列腺或女性患者的子宫中的雄激素受体的功能被阻断并在骨和/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，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。

7. 发明申请

WO02090325A2 BENZAZEPINONE ALPHA V INTEGRIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：苯唑嗪酮ALPHA V INTEGRIN受体拮抗剂
公开(公告)号：WO02090325A2
公开(公告)日：2002-11-14
申请号：PCT/US0213457
申请日：2002-04-29
申请人： MERCK & CO INC , MEISSNER ROBERT S , COLEMAN PAUL J , DUGGAN MARK E , HARTMAN GEORGE D , HUTCHINSON JOHN H , WANG JIABING
发明人： MEISSNER ROBERT S , COLEMAN PAUL J , DUGGAN MARK E , HARTMAN GEORGE D , HUTCHINSON JOHN H , WANG JIABING
IPC分类号： A61K31/55 , A61K38/27 , A61K38/29 , A61K45/06 , A61P7/00 , A61P9/08 , A61P17/00 , A61P19/02 , A61P19/08 , A61P19/10 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D213/73 , C07D401/12 , C07D471/04 , C07D471/10 , C07D
CPC分类号： C07D213/73 , A61K31/55 , A61K38/27 , A61K38/29 , A61K45/06 , C07D401/12 , C07D471/04 , C07D471/10 , A61K2300/00
摘要： The present invention relates to novel benzazepinone derivatives, their synthesis, and their use as alpha nu integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors alpha nu beta 3 and alpha nu beta 5 and are therefore useful for inhibiting bone resorption, treating and/or preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth.
摘要翻译：本发明涉及新的苯并氮杂酮衍生物，其合成及其作为αnu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αnββ3和αnuβ5的拮抗剂，因此可用于抑制骨吸收，治疗和/或预防骨质疏松症和抑制血管再狭窄，糖尿病性视网膜病变，黄斑变性，血管生成，动脉粥样硬化，炎性关节炎，癌症和转移性肿瘤生长。

8. 发明申请

WO2011106276A1 TASK CHANNEL ANTAGONISTS 审中-公开
标题翻译：任务通道ANTAGONISTS
公开(公告)号：WO2011106276A1
公开(公告)日：2011-09-01
申请号：PCT/US2011/025596
申请日：2011-02-21
申请人： MERCK SHARP & DOHME CORP. , COBURN, Craig , WANG, Jiabing , SANTARELLI, Vince , HU, Shuangxi , CUI, Mingxiang , HU, Bin , DONG, Jingchao , LUO, Yunfu , SOLL, Richard, M.
发明人： COBURN, Craig , WANG, Jiabing , SANTARELLI, Vince , HU, Shuangxi , CUI, Mingxiang , HU, Bin , DONG, Jingchao , LUO, Yunfu , SOLL, Richard, M.
IPC分类号： A01N43/90 , A61K31/519
CPC分类号： C07D471/04 , C07D471/18
摘要： This invention relates to TASK-1 and/or TASK-3 antagonists and/or their pharmaceutically acceptable salts, compositions and methods for treating and preventing disorders which are caused by activation or by an activated TASK-1 and/or TASK-3, and disorders which have TASK-1 and/or TASK-3-related damage as a secondary cause.
摘要翻译：本发明涉及用于治疗和预防由活化或由活化的TASK-1引起的疾病的TASK-1和/或TASK-3拮抗剂和/或其药学上可接受的盐，组合物和方法和/或TASK-3，以及具有TASK-1和/或TASK-3相关损伤作为次要原因的疾病。

9. 发明申请

WO2011103715A1 TASK CHANNEL ANTAGONISTS 审中-公开
标题翻译：任务通道ANTAGONISTS
公开(公告)号：WO2011103715A1
公开(公告)日：2011-09-01
申请号：PCT/CN2010/070751
申请日：2010-02-25
申请人： MERCK SHARP & DOHME CORP. , COBURN, Craig , WANG, Jiabing , SANTARELLI, Vince , HU, Shuangxi , CUI, Mingxiang , HU, Bin , DONG, Jingchao , LUO, Yunfu , SOLL, Richard, M
发明人： COBURN, Craig , WANG, Jiabing , SANTARELLI, Vince , HU, Shuangxi , CUI, Mingxiang , HU, Bin , DONG, Jingchao , LUO, Yunfu , SOLL, Richard, M
IPC分类号： C07D471/04 , C07D471/18 , A61K31/519 , A61K31/529 , A61P11/00 , A61P25/08 , A61P25/20 , A61P25/24
CPC分类号： C07D471/04 , A61K31/519 , A61K31/529 , A61K45/06 , C07D471/18 , A61K2300/00
摘要： This invention relates to TASK-1 and/or TASK-3 antagonists and/or their pharmaceutically acceptable salts, compositions and methods for treating and preventing disorders which are caused by activation or by an activated TASK-1 and/or TASK-3, and disorders which have TASK-1 and/or TASK-3-related damage as a secondary cause.
摘要翻译：本发明涉及TASK-1和/或TASK-3拮抗剂和/或其药学上可接受的盐，组合物和方法，用于治疗和预防由激活或活化的TASK-1和/或TASK-3引起的疾病，和具有TASK-1和/或TASK-3相关损伤的疾病作为次要原因。

10. 发明申请

WO2008070016A2 INHIBITORS OF AKT ACTIVITY 审中-公开
公开(公告)号：WO2008070016A2
公开(公告)日：2008-06-12
申请号：PCT/US2007/024722
申请日：2007-12-03
申请人： MERCK & CO., INC. , BANYU PHARMACEUTICAL CO., LTD. , KELLY, Michael, J. , LAYTON, Mark, E. , LIQUORI, Michael, E. , OGINO, Yoshio , ONOZAKI, Yu , SANDERSON, Philip, E. , WANG, Jiabing
发明人： KELLY, Michael, J. , LAYTON, Mark, E. , LIQUORI, Michael, E. , OGINO, Yoshio , ONOZAKI, Yu , SANDERSON, Philip, E. , WANG, Jiabing
CPC分类号： C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D407/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D471/14
摘要： The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.

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