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：EP1023068A1

公开(公告)日：2000-08-02

申请号：EP98930307.8

申请日：1998-06-17

申请人： MERCK & CO., INC. ,  SYNAPTIC PHARMACEUTICAL CORPORATION

发明人： PATANE, Michael, A. ,  BOCK, Mark, G. ,  NEWTON, Randall, C. ,  LAGU, Bharat

IPC分类号： A61K31/445 ,  A61K31/505 ,  C07D211/18 ,  C07D239/34 ,  C07D491/08 ,  C07D487/04 ,  C07D401/12 ,  C07D411/12 ,  C07D413/12

CPC分类号： C07D401/12 ,  C07D211/58 ,  C07D265/32 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D491/04 ,  C07D491/10

摘要： This invention relates to certain novel compounds and derivates thereof, their synthesis, and their use as alpha 1a adrenergic receptor antogonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.

公开(公告)号：EP1169042A1

公开(公告)日：2002-01-09

申请号：EP00911811.8

申请日：2000-02-14

申请人： Merck & Co., Inc.

发明人： PATANE, Michael, A. ,  NEWTON, Randall, C.

IPC分类号： A61K31/551 ,  A61K31/553 ,  A61K31/554 ,  A61P9/10 ,  A61P19/08 ,  C07D223/18 ,  C07D243/10 ,  C07D243/38 ,  C07D267/12 ,  C07D273/06 ,  C07D281/02 ,  C07D285/36 ,  C07D291/08 ,  C07D471/02 ,  C07D471/12 ,  C07D487/02 ,  C07D487/12 ,  C07D498/02 ,  C07D498/12 ,  C07D513/02 ,  C07D513/12

CPC分类号： C07D267/20

摘要： The present invention relates to dibenzo-azepine derivatives and their use as alphaV integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors alphaVbeta3, alphaVbeta5, and/or alphaVbeta6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.

摘要翻译： 本发明涉及二苯并吖庚因衍生物及其作为αV整联蛋白受体拮抗剂的用途。 更具体地说，本发明化合物是整联蛋白受体αVβ3，αVβ5和/或αVβ6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 ，炎症，伤口愈合，病毒性疾病，肿瘤生长和转移。

公开(公告)号：EP1040111A1

公开(公告)日：2000-10-04

申请号：EP98963915.8

申请日：1998-12-14

申请人： MERCK & CO., INC.

发明人： DUGGAN, Mark, E. ,  MEISSNER, Robert, S. ,  HUTCHINSON, John, H. ,  HALCZENKO, Wasyl ,  ASKEW, Ben, C. ,  COLEMAN, Paul, J. ,  PATANE, Michael, A. ,  WANG, Jiabing

IPC分类号： C07D471/04 ,  C07D401/06 ,  C07D401/14 ,  C07D519/00 ,  A61K31/415 ,  A61K31/44

CPC分类号： C07D471/04 ,  A61K31/415 ,  A61K31/44 ,  A61K31/66 ,  A61K45/06 ,  C07D401/14 ,  A61K2300/00

摘要： The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors αvβ3, αvβ5 and/or αvβ6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, and tumor growth and metastasis.

摘要翻译： 本发明涉及化合物及其衍生物，它们的合成及其作为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，αvβ5和/或αvβ6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，血管生成，动脉粥样硬化， 炎症，伤口愈合，病毒性疾病以及肿瘤生长和转移。

公开(公告)号：EP0866708A1

公开(公告)日：1998-09-30

申请号：EP96941406.0

申请日：1996-11-15

申请人： SYNAPTIC PHARMACEUTICAL CORPORATION ,  MERCK & CO., INC.

发明人： NAGARATHNAM, Dhanapalan ,  WONG, Wai, C. ,  MIAO, Shou, Wu ,  PATANE, Michael, A. ,  GLUCHOWSKI, Charles

IPC分类号： A61K31 ,  A61P3 ,  A61P9 ,  A61P15 ,  A61P27 ,  C07D239 ,  C07D401 ,  C07D491

CPC分类号： C07D239/22 ,  C07D401/12 ,  C07D491/04

摘要： This invention is directed to dihydropyrimidine compounds which are selective antagonists for human α1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of begnin prostatic hyperplasia, impotency, cardiac arrythmia and for the treatment of any disease where the antagonism of the α1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

公开(公告)号：EP1040111B1

公开(公告)日：2005-06-22

申请号：EP98963915.8

申请日：1998-12-14

申请人： MERCK & CO., INC.

发明人： DUGGAN, Mark, E. ,  MEISSNER, Robert, S. ,  HUTCHINSON, John, H. ,  HALCZENKO, Wasyl ,  ASKEW, Ben, C. ,  COLEMAN, Paul, J. ,  PATANE, Michael, A. ,  WANG, Jiabing ,  PERKINS, James J.

IPC分类号： C07D471/04 ,  C07D401/06 ,  C07D401/14 ,  C07D519/00 ,  A61K31/415 ,  A61K31/44

CPC分类号： C07D471/04 ,  A61K31/415 ,  A61K31/44 ,  A61K31/66 ,  A61K45/06 ,  C07D401/14 ,  A61K2300/00

摘要： The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors αvβ3, αvβ5 and/or αvβ6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, and tumor growth and metastasis.

公开(公告)号：EP1252162A1

公开(公告)日：2002-10-30

申请号：EP01942625.3

申请日：2001-01-16

申请人： Merck & Co., Inc.

发明人： DUGGAN, Mark, E. ,  HALCZENKO, Wasyl ,  HUTCHINSON, John, H. ,  LI, Aiwen ,  MEISSNER, Robert, S. ,  PERKINS, James, J. ,  STEELE, Thomas, G. ,  WANG, Jiabing ,  PATANE, Michael, A.

IPC分类号： C07D471/04 ,  C07D401/06 ,  A61K31/4375 ,  A61K31/444

CPC分类号： C07D213/73 ,  A61K45/06 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04 ,  C07D471/10

摘要： The present invention relates to novel imidazolidinone derivatives thereof, their synthesis, and their use as αν integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors αvβ3 and/or αvβ5 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.

公开(公告)号：EP0853479A1

公开(公告)日：1998-07-22

申请号：EP96933093.0

申请日：1996-09-24

申请人： MERCK & CO., INC.

发明人： BOCK, Mark, G. ,  LUMMA, William, C. ,  PATANE, Michael, A.

IPC分类号： A61K31 ,  A61P9 ,  A61P13 ,  A61P43 ,  C07D403 ,  C07D405

CPC分类号： C07D403/04 ,  C07D405/14

摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha 1b adrenergic receptor antagonists. These compounds display submicromolar affinity for the human alpha 1b adrenergic receptor subtype while displaying at least five-fold lower affinity for the human alpha 1d and alpha 1a adrenergic receptor subtypes, and many other G-protein coupled human receptors. One application of these compounds is in the treatment of hypertension. More specifically, these compounds display selectivity for lowering blood pressure without, for example, substantially affecting urethral pressure.

公开(公告)号：EP1187592B1

公开(公告)日：2007-08-01

申请号：EP00942652.9

申请日：2000-05-30

申请人： Merck & Co., Inc.

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： A61K31/506 ,  C07D239/48 ,  C07D401/06 ,  C07D471/04 ,  A61K31/4375 ,  A61K31/55 ,  C07D519/00 ,  A61P19/10

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.