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1.发明公开Methods and Compounds for Producing Dipeptidyl Peptidase IV Inhibitors and Intermediates thereof 有权的方法和化合物对二肽基肽酶IV抑制剂和其中间体的制备
公开(公告)号：EP2505578A2
公开(公告)日：2012-10-03
申请号：EP12162626.1
申请日：2003-12-04
发明人： VU, Truc, Chi , FOX, Rita , HANSON, Ronald, L. , MAZZULLO, John, A., Jr. , WANG, Jianji , YU, Jurong , MAGNIN, David, R. , HAMANN, Lawrence, G. , BRZOZOWSKI, David, B. , GODFREY, Jollie, Duaine, Jr. , KOLOTUCHIN, Sergei, V. , PATEL, Ramesh, N. , WONG, Kwok , ZHU, Jason , AUGERI, David, J.
IPC分类号： C07C62/06 , C07C229/28 , C07C271/22 , C07D207/22 , C07D209/52 , C07C69/635 , C07C69/675 , C07C69/757
CPC分类号： C07C69/757 , C07C62/06 , C07C69/635 , C07C69/675 , C07C229/28 , C07C271/22 , C07C2603/74 , C07D207/22 , C07D209/52
摘要： Methods and compounds for production of cycloproyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided.
摘要翻译： 提供了用于生产二肽基肽酶IV的cycloproyl稠合的基于吡咯烷的抑制剂的方法和化合物。
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2.发明授权ADAMANTYLGLYCINE- BASED INHIBITORS OF DIPEPTIDYL PEPTIDASE IV FOR THE TREATMENT OF DIABETES 有权二肽基肽酶IV抑制剂对糖尿病ADAMANTYLGLYCINBASIS处理成
公开(公告)号：EP1658066B9
公开(公告)日：2010-02-24
申请号：EP04779352.6
申请日：2004-07-28
发明人： HAMANN, Lawrence, G. , KHANNA, Ashish , KIRBY, Mark, S. , MAGNIN, David, R. , SIMPKINS, Ligaya, M. , SUTTON, James, C. , ROBL, Jeffrey
IPC分类号： A61K31/40
CPC分类号： C07C255/46 , C07C255/47 , C07C2601/08 , C07C2602/18 , C07C2603/74 , C07D207/16 , C07D209/52 , C07D277/04 , C07D295/185
摘要： Compounds are provided having the formula (I) wherein: n is 0, 1 or 2; m is 0, 1 or 2; the sum of n + m less then or equal to 2; the dashed bonds forming a cyclopropyl ring can only be present when Y is CH; X is H or CN; Y is CH, CH2, CHF, CF2, O, S, SO, or SO2; and A is adamantyl. The compounds are inhibitors of dipeptidyl peptidase IV (DPP-IV) and are useful for the treatment of diabetes and related diseases.
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3.发明公开ADAMANTYLGLYCINE- BASED INHIBITORS OF DIPEPTIDYL PEPTIDASE IV FOR THE TREATMENT OF DIABETES 有权二肽基肽酶IV抑制剂对糖尿病ADAMANTYLGLYCINBASIS处理成
公开(公告)号：EP1658066A2
公开(公告)日：2006-05-24
申请号：EP04779352.6
申请日：2004-07-28
发明人： HAMANN, Lawrence, G. , KHANNA, Ashish , KIRBY, Mark, S. , MAGNIN, David, R. , SIMPKINS, Ligaya, M. , SUTTON, James, C. , ROBL, Jeffrey
IPC分类号： A61K31/40
CPC分类号： C07C255/46 , C07C255/47 , C07C2601/08 , C07C2602/18 , C07C2603/74 , C07D207/16 , C07D209/52 , C07D277/04 , C07D295/185
摘要： Compounds are provided having the formula (I) wherein: n is 0, 1 or 2; m is 0, 1 or 2; the sum of n + m less then or equal to 2; the dashed bonds forming a cyclopropyl ring can only be present when Y is CH; X is H or CN; Y is CH, CH2, CHF, CF2, O, S, SO, or SO2; and A is adamantyl. The compounds are inhibitors of dipeptidyl peptidase IV (DPP-IV) and are useful for the treatment of diabetes and related diseases.
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4.发明公开Methods and Compounds for Producing Dipeptidyl Peptidase IV Inhibitors and Intermediates thereof 有权生产二肽基肽酶IV抑制剂及其中间体的方法和化合物
公开(公告)号：EP2505578A3
公开(公告)日：2013-07-31
申请号：EP12162626.1
申请日：2003-12-04
发明人： VU, Truc, Chi , FOX, Rita , HANSON, Ronald, L. , MAZZULLO, John, A., Jr. , WANG, Jianji , YU, Jurong , MAGNIN, David, R. , HAMANN, Lawrence, G. , BRZOZOWSKI, David, B. , GODFREY, Jollie, Duaine, Jr. , KOLOTUCHIN, Sergei, V. , PATEL, Ramesh, N. , WONG, Kwok , ZHU, Jason , AUGERI, David, J.
IPC分类号： C07C62/06 , C07C229/28 , C07C271/22 , C07D207/22 , C07D209/52 , C07C69/635 , C07C69/675 , C07C69/757
CPC分类号： C07C69/757 , C07C62/06 , C07C69/635 , C07C69/675 , C07C229/28 , C07C271/22 , C07C2603/74 , C07D207/22 , C07D209/52
摘要： Methods and compounds for production of cycloproyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided.
摘要翻译： 提供了用于生产二肽基肽酶IV的基于环丙酰基稠合吡咯烷的抑制剂的方法和化合物。
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公开(公告)号：EP1553937B1
公开(公告)日：2010-06-02
申请号：EP03774915.7
申请日：2003-10-21
IPC分类号： A61K31/40 , A61K31/275 , C07C255/03 , C07D209/48 , A61P3/06 , A61P3/10
CPC分类号： C07C255/30 , C07B2200/07 , C07C255/29 , C07C2601/02 , C07C2601/04 , C07C2602/42 , C07C2603/74 , C07D211/28 , C07D211/34
摘要： A compound of the Formula (I) wherein R1, R2, R3 and R4 are as defined herein. Further provided are methods of using such compounds for the treatment of diabetes and related diseases, and to pharmaceutical compositions containing such compounds.
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6.发明公开GLYCINENITRILE-BASED INHIBITORS OF DIPEPTIDYL PEPTIDASE IV AND METHODS 有权AUF GLYCINNITRIL BASIERENDE HEMMER DER DIPEPTIDYLPEPTIDASE IV
公开(公告)号：EP1553937A2
公开(公告)日：2005-07-20
申请号：EP03774915.7
申请日：2003-10-21
IPC分类号： A61K31/40 , A61K31/275 , C07C255/03 , C07D209/48
CPC分类号： C07C255/30 , C07B2200/07 , C07C255/29 , C07C2601/02 , C07C2601/04 , C07C2602/42 , C07C2603/74 , C07D211/28 , C07D211/34
摘要： A compound of the Formula (I) wherein R1, R2, R3 and R4 are as defined herein. Further provided are methods of using such compounds for the treatment of diabetes and related diseases, and to pharmaceutical compositions containing such compounds.
摘要翻译： 式I的化合物：化学式id =“CHEM-US-00001”num =“000
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7.发明授权ADAMANTYLGLYCINE- BASED INHIBITORS OF DIPEPTIDYL PEPTIDASE IV FOR THE TREATMENT OF DIABETES 有权抑制剂DEP DIPEPTIDYPEPTIDASE IV AUF ADAMANTYLGLYCINBASIS ZUR BEHANDLUNG VON DIABETES
公开(公告)号：EP1658066B1
公开(公告)日：2009-09-30
申请号：EP04779352.6
申请日：2004-07-28
发明人： HAMANN, Lawrence, G. , KHANNA, Ashish , KIRBY, Mark, S. , MAGNIN, David, R. , SIMPKINS, Ligaya, M. , SUTTON, James, C. , ROBL, Jeffrey
IPC分类号： A61K31/40
CPC分类号： C07C255/46 , C07C255/47 , C07C2601/08 , C07C2602/18 , C07C2603/74 , C07D207/16 , C07D209/52 , C07D277/04 , C07D295/185
摘要： Compounds are provided having the formula (I) wherein: n is 0, 1 or 2; m is 0, 1 or 2; the sum of n + m less then or equal to 2; the dashed bonds forming a cyclopropyl ring can only be present when Y is CH; X is H or CN; Y is CH, CH2, CHF, CF2, O, S, SO, or SO2; and A is adamantyl. The compounds are inhibitors of dipeptidyl peptidase IV (DPP-IV) and are useful for the treatment of diabetes and related diseases.
摘要翻译： 本发明的化合物是二肽基肽酶IV（DPP-IV）的基于金刚烷基甘氨酸的抑制剂，可用于治疗糖尿病和相关疾病。
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8.发明授权CYCLOPROPYL-FUSED PYRROLIDINE-BASED INHIBITORS OF DIPEPTIDYL PEPTIDASE IV, PROCESSES FOR THEIR PREPARATION, AND THEIR USE 有权基于吡咯烷环丙基稠合的二肽基肽酶IV抑制剂，其制造方法相同，并且它们的用途
公开(公告)号：EP1261586B1
公开(公告)日：2008-05-21
申请号：EP01918383.9
申请日：2001-03-05
发明人： ROBL, Jeffrey, A. , SULSKY, Richard, B. , AUGERI, David, J. , MAGNIN, David, R. , HAMANN, Lawrence, G. , BETEBENNER, David, A.
IPC分类号： C07D209/52 , A61K31/403 , A61P3/04 , A61P3/06 , A61P3/10
CPC分类号： C07C271/22 , C07C2603/74 , C07D209/52 , C07D401/06 , C07D403/06
摘要： Dipeptidyl peptidase IV (DP 4) inhibiting compounds are provided having the formula (I) where x is 0 or 1 and y is 0 or 1 (provided that x = 1 when y = 0 and x = 0 when y = 1); n is 0 or 1; X is H or CN; and wherein R?1, R2, R3 and R4¿ are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, and other diseases as set out herein, employing such DP 4 inhibitor or a combination of such DP 4 inhibitor and one or more of another antidiabetic agent such as metformin, glyburide, troglitazone, pioglitazone, rosiglitazone and/or insulin and/or one or more of a hypolipidemic agent and/or anti-obesity agent and/or other therapeutic agent.
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公开(公告)号：EP0886637B9
公开(公告)日：2005-05-04
申请号：EP96903604.5
申请日：1996-02-01
发明人： WETTERAU, John, R. II , SHARP, Daru, Young , GREGG, Richard, E. , BILLER, Scott, A. , DICKSON, John, A. , LAWRENCE, R., Michael , MAGNIN, David, R. , POSS, Michael, A. , ROBL, Jeffrey, A. , SULSKY, Richard, B. , TINO, Joseph, A. , LAWSON, John, E. , HOLAVA, Henry, M. , PARTYKA, Richard, A.
IPC分类号： C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D211/58 , A61K31/445
CPC分类号： C07D401/04 , C07D211/58 , C07D211/60 , C07D211/94 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D419/12 , G01N2800/044
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10.发明公开DUAL INHIBITORS OF ADIPOCYTE FATTY ACID BINDING PROTEIN AND KERATINOCYTE FATTY ACID BINDING PROTEIN 审中-公开脂肪酸双抑制剂结合蛋白脂肪细胞和角质形成细胞脂肪酸结合蛋白
公开(公告)号：EP1443919A1
公开(公告)日：2004-08-11
申请号：EP02782300.4
申请日：2002-11-15
发明人： MAGNIN, David, R. , SULSKY, Richard, B. , ROBL, Jeffrey, A. , CAULFIELD, Thomas, J. , PARKER, Rex, A.
IPC分类号： A61K31/19 , A61K31/41 , A61K31/195 , C07C65/00 , C07C59/64 , C07C229/00 , C07D257/00 , C07D257/04
CPC分类号： C07C323/56 , A61K31/155 , A61K31/19 , A61K31/195 , A61K31/41 , A61K31/427 , A61K31/64 , A61K38/28 , A61K45/06 , C07C45/41 , C07C45/59 , C07C45/71 , C07C47/575 , C07C51/487 , C07C59/68 , C07C65/24 , C07C205/35 , C07C205/59 , C07C229/36 , C07C233/47 , C07C233/81 , C07C233/87 , C07C235/12 , C07C251/48 , C07C255/54 , C07C311/21 , C07C317/18 , C40B40/00 , A61K2300/00 , C07C47/565
摘要： Compounds that are dual aP2/k-FABP inhibitors are provided having the formula (I), wherein A, B, X, Y, R?1, R2 and R3¿ are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing dual aP2/k-FABP inhibitors alone or in combination with at least one other antidiabetic agent such as metformin, glyburide, troglitazone and/or insulin.
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