公开(公告)号：EP1631548B1

公开(公告)日：2009-10-28

申请号：EP04750420.4

申请日：2004-04-20

申请人： Merck & Co., Inc.

发明人： DUGGAN, Mark, E. ,  LINDSLEY, Craig, W. ,  WU, Zhicai ,  ZHAO, Zhijian ,  HARTNETT, John, C.

IPC分类号： A61K31/44 ,  C07D213/02

CPC分类号： C07D213/85 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

摘要： The present invention is directed to compounds which contain a substituted pyridine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

公开(公告)号：EP1807076A1

公开(公告)日：2007-07-18

申请号：EP05851360.7

申请日：2005-10-25

申请人： Merck & Co., Inc.

发明人： KIM, Yuntae ,  CLOSE, Joshua ,  DUGGAN, Mark, E. ,  HANNEY, Barbara ,  MEISSNER, Robert, S. ,  MUSSELMAN, Jeffrey ,  PERKINS, James, J. ,  WANG, Jiabing

IPC分类号： A61K31/44 ,  C07D213/02

CPC分类号： C07D213/64 ,  A61K31/44 ,  C07D213/74

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, 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.

公开(公告)号：EP1040098B1

公开(公告)日：2005-04-27

申请号：EP98963136.1

申请日：1998-12-14

申请人： Merck & Co., Inc. (a New Jersey corp.)

发明人： ASKEW, Ben, C. ,  COLEMAN, Paul, J. ,  DUGGAN, Mark, E. ,  HALCZENKO, Wasyl ,  HARTMAN, George, D. ,  HUNT, Cecilia ,  HUTCHINSON, John, H. ,  MEISSNER, Robert, S. ,  PATANE, Michael, A. ,  SMITH, Garry, R. ,  WANG, Jiabing

IPC分类号： C07D213/30 ,  C07D235/12 ,  C07D239/26 ,  C07D257/00 ,  C07D277/00 ,  C07D471/04 ,  C07D471/14 ,  A61K31/155 ,  A61K31/415 ,  A61K31/44 ,  A61K31/505 ,  C07D401/12 ,  C07D491/04 ,  C07D401/06 ,  C07D519/00 ,  C07D213/74

CPC分类号： C07D401/06 ,  C07D401/12 ,  C07D471/04 ,  C07D495/04

公开(公告)号：EP1254116A1

公开(公告)日：2002-11-06

申请号：EP01908643.8

申请日：2001-01-19

申请人： Merck & Co., Inc.

发明人： ASKEW, Ben, C. ,  BRESLIN, Michael, J. ,  DUGGAN, Mark, E. ,  HUTCHINSON, John, H. ,  MEISSNER, Robert, S. ,  PERKINS, James, J. ,  STEELE, Thomas, G. ,  PATANE, Michael, A.

IPC分类号： C07D213/02 ,  C07D233/04 ,  C07D233/14 ,  C07C233/16 ,  C07D239/02 ,  C07D265/36 ,  C07D471/02 ,  C07D487/02 ,  A61K31/40 ,  A61K31/44 ,  A61K31/55 ,  A61K31/415 ,  A61K31/495 ,  A61K31/505 ,  A61K31/535

CPC分类号： C07D213/73 ,  A61K45/06 ,  C07D239/26 ,  C07D239/42 ,  C07D239/48 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D471/04 ,  C07D471/10

摘要： The present invention relates to novel alkanoic acid derivatives thereof, their synthesis, and their use as αv integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors αvβ3 and/or αβ5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth.

摘要翻译： 本发明涉及新的链烷酸衍生物，它们的合成，以及它们作为αv整联蛋白受体拮抗剂的用途。 更具体地说，本发明化合物是整联蛋白受体αvβ3和/或αβ5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，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。

公开(公告)号：EP0946165A1

公开(公告)日：1999-10-06

申请号：EP97947280.0

申请日：1997-10-27

申请人： MERCK & CO., INC.

发明人： DUGGAN, Mark, E. ,  HARTMAN, George, D.

IPC分类号： C07D235 ,  A61K31 ,  A61K45 ,  A61P9 ,  A61P19 ,  A61P35 ,  A61P43 ,  C07D213 ,  C07D401 ,  C07D471

CPC分类号： C07D213/73 ,  A61K45/06 ,  C07D401/12 ,  C07D471/04

摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are αvβ3 antagonists, αvβ5 antagonists or dual αvβ3/αvβ5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.

公开(公告)号：EP0673247A1

公开(公告)日：1995-09-27

申请号：EP94904069.0

申请日：1993-11-29

申请人： MERCK & CO. INC.

发明人： EGBERTSON, Melissa, S. ,  TURCHI, Laura, M. ,  HARTMAN, George, D. ,  HALCZENKO, Wasyl ,  WHITMAN, David, B. ,  PERKINS, James, J. ,  KRAUSE, Amy, E. 570 W. Dekalb Pike ,  IHLE, Nathan ,  CLAREMON, David, Alan ,  HOFFMAN, William ,  DUGGAN, Mark, E.

IPC分类号： C07D295 ,  A61K31 ,  A61P7 ,  A61P43 ,  C07C255 ,  C07C271 ,  C07C309 ,  C07C311 ,  C07D205 ,  C07D207 ,  C07D211 ,  C07D213 ,  C07D233 ,  C07D401 ,  C07D409 ,  C07D521

CPC分类号： C07D213/30 ,  C07C311/19 ,  C07D205/04 ,  C07D211/22 ,  C07D211/26 ,  C07D211/34 ,  C07D211/46 ,  C07D211/70 ,  C07D213/71 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D249/08 ,  C07D295/084 ,  C07D295/088 ,  C07D295/096 ,  C07D295/155 ,  C07D401/12 ,  C07D409/12

摘要： Novel fibrinogen receptor antagonists of the formula: X-Y-Z-Aryl-A-B are provided in which the claimed compounds exhibit fibrinogen receptor antagonist activity, inhibit platelet aggregation and are therefore useful in modulating thrombus formation.

公开(公告)号：EP1631548A2

公开(公告)日：2006-03-08

申请号：EP04750420.4

申请日：2004-04-20

申请人： Merck & Co., Inc.

发明人： DUGGAN, Mark, E. ,  LINDSLEY, Craig, W. ,  WU, Zhicai ,  ZHAO, Zhijian ,  HARTNETT, John, C.

IPC分类号： C07D213/02 ,  A61K31/44

CPC分类号： C07D213/85 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

摘要： The present invention is directed to compounds which contain a substituted pyridine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

摘要翻译： 本发明涉及含有抑制丝氨酸/苏氨酸蛋白激酶Akt活性的取代吡啶部分的化合物。 本发明还涉及含有本发明化合物的化学治疗组合物和用于治疗癌症的方法，其包括施用本发明的化合物。

公开(公告)号：EP1496896A1

公开(公告)日：2005-01-19

申请号：EP03719597.1

申请日：2003-04-04

申请人： Merck & Co., Inc.

发明人： BILODEAU, Mark, T. ,  DUGGAN, Mark, E. ,  HARTNETT, John, C. ,  LINDSLEY, Craig, W. ,  MANLEY, Peter, J. ,  WU, Zhicai ,  ZHAO, Zhijian

IPC分类号： A61K31/4375 ,  A61K31/4709 ,  A61K31/4985 ,  A61K31/52 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D417/14 ,  C07D473/32

CPC分类号： C07D401/10 ,  A61K31/498 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04

摘要： The present invention is directed to compounds comprising a 2,3-diphenylquinoxaline moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

公开(公告)号：EP1434786A1

公开(公告)日：2004-07-07

申请号：EP02768911.6

申请日：2002-09-27

申请人： Merck & Co., Inc.

发明人： WANG, Jiabing ,  DUGGAN, Mark, E. ,  WHITMAN, David, B.

IPC分类号： C07J3/00 ,  A61K31/56

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.

公开(公告)号：EP1387688A2

公开(公告)日：2004-02-11

申请号：EP02725848.2

申请日：2002-04-29

申请人： Merck & Co., Inc.

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 ,  A61P19/10 ,  C07D401/02

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 αξ integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors αξβ3 and αξβ5 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.