公开(公告)号：EP1040098A1

公开(公告)日：2000-10-04

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

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

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 αξβ3, αξβ5, and/or αξβ6 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.

公开(公告)号：EP1229910A1

公开(公告)日：2002-08-14

申请号：EP00967201.5

申请日：2000-09-29

申请人： Merck & Co., Inc.

发明人： ASKEW, Ben, C. ,  SMITH, Garry, R.

IPC分类号： A61K31/437 ,  A61K31/44 ,  C07D401/06 ,  C07D471/04

CPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/44 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention relates to compounds and derivatives thereof, their synthesis, and their use as vitronectin 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, inflammatory arthritis, cancer, and metastatic tumor growth.

公开(公告)号：EP0934305A1

公开(公告)日：1999-08-11

申请号：EP97938568.0

申请日：1997-08-25

申请人： MERCK & CO., INC.

发明人： DUGGAN, Mark, E. ,  HARTMAN, George, D. ,  HOFFMAN, William, F. ,  MEISSNER, Robert, S. ,  PERKINS, James, J. ,  ASKEW, Ben, C. ,  COLEMAN, Paul, J. ,  HUTCHINSON, John, H. ,  NAYLOR-OLSEN, Adel, M.

IPC分类号： A61K31 ,  A61P3 ,  A61P9 ,  A61P19 ,  A61P27 ,  A61P29 ,  A61P35 ,  A61P43 ,  C07D471 ,  C07D519 ,  C07K5 ,  A61K38

CPC分类号： C07D471/04 ,  A61K31/4375 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/506 ,  A61K38/00 ,  C07K5/0202

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：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：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：EP1150965A1

公开(公告)日：2001-11-07

申请号：EP00907089.7

申请日：2000-01-31

申请人： Merck & Co., Inc.

发明人： ASKEW, Ben, C.

IPC分类号： C07D267/02 ,  C07D243/12 ,  C07D491/00 ,  A61K31/55 ,  A61K31/553

CPC分类号： C07D491/04

摘要： The present invention relates to benzazepine derivatives and their use as alpha-V 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.

公开(公告)号：EP0866705A1

公开(公告)日：1998-09-30

申请号：EP96936505.0

申请日：1996-10-15

申请人： MERCK & CO., INC.

发明人： ASKEW, Ben, C. ,  HARTMAN, George, D. ,  DUGGAN, Mark, E. ,  YOUNG, Steven, D. ,  HUTCHINSON, John, H. ,  WAI, John, S. ,  EGBERTSON, Melissa, S. ,  VASSALLO, Laura, M. ,  LIBBY, Laura, A. ,  IHLE, Nathan, C. ,  KRAUSE, Amy, E. ,  HALCZENKO, Wasyl

IPC分类号： A61K31 ,  A61P7 ,  C07D401 ,  C07D405 ,  C07D453 ,  C07D521 ,  C07K5

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D453/04 ,  C07K5/06026

摘要： Fibrinogen receptor antagonists having structure, for example, of (I) or for example (II).

摘要翻译： 具有例如（I）或例如（II）结构的纤维蛋白原受体拮抗剂。

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。