公开(公告)号：EP1377288A1

公开(公告)日：2004-01-07

申请号：EP02723791.6

申请日：2002-04-05

申请人： Bristol-Myers Squibb Company

发明人： SULSKY, Richard, B. ,  ROBL, Jeffrey, A.

IPC分类号： A61K31/415 ,  A61K31/42 ,  C07D231/04 ,  C07D231/06 ,  C07D261/02

CPC分类号： C07D231/06 ,  A61K31/415 ,  A61K31/42 ,  C07D231/04 ,  C07D261/02 ,  A61K2300/00

摘要： Dipeptidyl peptidase IV (DP 4) inhibiting compounds are provided having the formula where n is 0 or 1; X is H or CN; Y is N, NH or O; Z is CH2 when Y is O or N-H, with Y-Z forming a single bond, and Z is CH when Y is N, with Y-Z forming a double bond; 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.

公开(公告)号：EP2021354A2

公开(公告)日：2009-02-11

申请号：EP07797751.0

申请日：2007-05-25

申请人： Bristol-Myers Squibb Company

发明人： EWING, William, R. ,  MAPELLI, Claudio ,  RIEXINGER, Douglas, James ,  LEE, Ving, G. ,  SULSKY, Richard, B. ,  ZHU, Yeheng

IPC分类号： C07K7/06 ,  A61K38/08 ,  A61K38/26

CPC分类号： A61K33/30 ,  A61K33/26 ,  A61K33/32 ,  A61K38/08 ,  A61K38/26 ,  A61K45/06 ,  C07K14/605 ,  A61K2300/00

摘要： The subject matter described herein provides novel human glucagon-like peptide-1 (GLP-1) receptor modulators that have biological activity similar or superior to native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. The described compounds include chemically modified peptides that may stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 receptor modulators exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration. The disclosed and claimed peptides show desirable pharmacokinetic properties and desirable potency in efficacy models of diabetes.

公开(公告)号：EP1644335A1

公开(公告)日：2006-04-12

申请号：EP04778086.1

申请日：2004-07-12

申请人： Bristol-Myers Squibb Company

发明人： SUN, Chong-Qing ,  SITKOFF, Doree ,  EWING, William, R. ,  HUANG, Yanting ,  ELLSWORTH, Bruce, A. ,  SULSKY, Richard, B. ,  GU, Zhengxiang ,  MURUGESAN, Natesan ,  GERRITZ, Samuel ,  PENDRI, Annapurna

IPC分类号： C07D215/38 ,  A61K31/47

CPC分类号： C07D417/06 ,  C07D215/38 ,  C07D215/48 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

摘要： The invention provides for compounds of formula (I); wherein the substitutents are as described herein. Further provided are methods of using such compounds for the treatment of eating disorders, metabolic disorders, obesity, cognitive disorders, neurological disorders, pain disorders, inflammation disorders, in the promotion of smoking cessation and for the treatment of other psychiatric disorders Also provided are pharmaceutical compositions containing such compounds and pharmaceutical combinations of the compounds of the invention with other therapeutic agents.

公开(公告)号：EP0886637B1

公开(公告)日：2004-12-01

申请号：EP96903604.5

申请日：1996-02-01

申请人： BRISTOL-MYERS SQUIBB COMPANY

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

公开(公告)号：EP1181014A1

公开(公告)日：2002-02-27

申请号：EP00918177.7

申请日：2000-03-20

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： ROBL, Jeffrey, A. ,  SULSKY, Richard, B. ,  MAGNIN, David, R.

IPC分类号： A61K31/41

CPC分类号： C07D207/323 ,  A61K45/06 ,  C07D207/452 ,  C07D231/12 ,  C07D233/64 ,  C07D249/12 ,  C07D263/32 ,  C07D307/42 ,  C07D317/22 ,  C07D333/20 ,  C07D403/10 ,  C07D403/12 ,  C07D405/10 ,  C07D413/10

摘要： aP2 inhibiting compounds are provided having formula (I) wherein R?1, R2, R3, R4¿, X-Z and (a) are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing such aP2 inhibitor or a combination of such aP2 inhibitor and another antidiabetic agent such as metformin, glyburide, troglitazone and/or insulin.

公开(公告)号：EP0904262A1

公开(公告)日：1999-03-31

申请号：EP97903805.0

申请日：1997-01-13

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： BILLER, Scott, A. ,  DICKSON, John, K. ,  LAWRENCE, R., Michael ,  MAGNIN, David, R. ,  POSS, Michael, A. ,  ROBL, Jeffrey, A. ,  SLUSARCHYK, William, A. ,  SULSKY, Richard, B. ,  TINO, Joseph, A.

IPC分类号： A61K31 ,  C07C17 ,  C07C33 ,  C07C47 ,  C07C49 ,  C07C69 ,  C07C205 ,  C07C233 ,  C07C235 ,  C07C237 ,  C07C255 ,  C07C259 ,  C07C271 ,  C07C291 ,  C07C311 ,  C07C317 ,  C07C321 ,  C07C323 ,  C07D207 ,  C07D209 ,  C07D211 ,  C07D213 ,  C07D221 ,  C07D231 ,  C07D233 ,  C07D235 ,  C07D239 ,  C07D249 ,  C07D253 ,  C07D263 ,  C07D271 ,  C07D277 ,  C07D285 ,  C07D295 ,  C07D307 ,  C07D311 ,  C07D317 ,  C07D319 ,  C07D327 ,  C07D333 ,  C07D335 ,  C07D401 ,  C07D403 ,  C07D405 ,  C07D407 ,  C07D409 ,  C07D417 ,  C07D471 ,  C07D473 ,  C07D487 ,  C07F7 ,  C07F9

CPC分类号： C07F7/1856 ,  A61K31/191 ,  A61K31/366 ,  A61K31/404 ,  A61K31/4468 ,  C07C17/093 ,  C07C47/453 ,  C07C49/563 ,  C07C49/567 ,  C07C49/573 ,  C07C69/00 ,  C07C205/11 ,  C07C205/43 ,  C07C205/55 ,  C07C233/58 ,  C07C233/59 ,  C07C233/60 ,  C07C233/62 ,  C07C233/63 ,  C07C233/78 ,  C07C235/40 ,  C07C235/56 ,  C07C237/22 ,  C07C237/24 ,  C07C255/41 ,  C07C259/08 ,  C07C271/22 ,  C07C291/04 ,  C07C311/19 ,  C07C311/21 ,  C07C311/37 ,  C07C311/42 ,  C07C311/46 ,  C07C317/12 ,  C07C321/22 ,  C07C323/60 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2603/00 ,  C07C2603/18 ,  C07C2603/32 ,  C07C2603/74 ,  C07D207/335 ,  C07D207/38 ,  C07D209/08 ,  C07D209/16 ,  C07D209/34 ,  C07D209/38 ,  C07D209/46 ,  C07D209/48 ,  C07D211/60 ,  C07D211/62 ,  C07D213/40 ,  C07D213/64 ,  C07D213/74 ,  C07D213/75 ,  C07D213/80 ,  C07D213/89 ,  C07D221/16 ,  C07D231/56 ,  C07D233/24 ,  C07D233/64 ,  C07D233/84 ,  C07D233/88 ,  C07D233/90 ,  C07D235/06 ,  C07D235/08 ,  C07D235/16 ,  C07D235/24 ,  C07D235/26 ,  C07D235/28 ,  C07D235/30 ,  C07D239/38 ,  C07D239/42 ,  C07D239/47 ,  C07D249/12 ,  C07D249/14 ,  C07D249/18 ,  C07D253/07 ,  C07D263/38 ,  C07D263/46 ,  C07D263/58 ,  C07D271/07 ,  C07D277/36 ,  C07D277/56 ,  C07D277/74 ,  C07D285/08 ,  C07D285/125 ,  C07D295/108 ,  C07D295/155 ,  C07D295/185 ,  C07D307/14 ,  C07D311/84 ,  C07D317/30 ,  C07D317/58 ,  C07D319/06 ,  C07D327/06 ,  C07D333/20 ,  C07D335/14 ,  C07D401/12 ,  C07D403/04 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D417/04 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07C25/22

摘要： Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure (I) or (IA) or (IB) including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0,1 or 2; Rx is H, alkyl, aryl or halogen; A is (1) a bond; (2) -O-; or (3) (i); B is: (ii) or (iii) or (iv) or (v) (wherein (a = 2, 3 or 4)) or (vi) or (vii) or (viii); and wherein L?2, L1, R1, R2, R3, R3', R3a, R3b, R4, R4', R5¿, X, (ix), (x) and (xi) are as defined herein.

公开(公告)号：EP1551511B1

公开(公告)日：2018-10-24

申请号：EP03751958.4

申请日：2003-09-02

申请人： Bristol-Myers Squibb Company

发明人： YU, Guixue ,  LI, Jun ,  EWING, William, R. ,  SULSKY, Richard, B. ,  LI, James, J. ,  TINO, Joseph, A.

IPC分类号： C07D471/04 ,  C07D487/04 ,  C07D513/04 ,  A61K31/55 ,  A61K31/54 ,  A61K31/535 ,  A61K31/495 ,  A61K31/50 ,  A61K31/505 ,  A61K31/44 ,  A61K31/445 ,  A61K31/425 ,  A61K31/42 ,  A61P3/00

CPC分类号： C07D487/04 ,  C07D231/56 ,  C07D261/20 ,  C07D471/04 ,  C07D513/04

摘要： Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula I wherein R 1 , R 1 ', R 2 , R 3 , R 4 , Xa, Y, Z and n are as described herein. The compounds provided herein are useful in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.

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

申请人： Bristol-Myers Squibb Company

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.

公开(公告)号：EP1883652A2

公开(公告)日：2008-02-06

申请号：EP06760391.0

申请日：2006-05-26

申请人： Bristol-Myers Squibb Company

发明人： EWING, William R. ,  MAPELLI, Claudio ,  RIEXINGER, Douglas, James ,  LEE, Ving, G. ,  SULSKY, Richard, B. ,  ZHU, Yeheng

IPC分类号： C07K14/605

CPC分类号： C07K14/605 ,  A61K38/00

摘要： The subject matter described herein provides novel human glucagon-like peptide-1 (GLP-1) receptor modulators that have biological activity similar or superior to native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. The described compounds include chemically modified peptides that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 receptor modulators exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration. The disclosed and claimed peptides show desirable pharmacokinetic properties and desirable potency in efficacy models of diabetes.

公开(公告)号：EP1551511A2

公开(公告)日：2005-07-13

申请号：EP03751958.4

申请日：2003-09-02

申请人： Bristol-Myers Squibb Company

发明人： YU, Guixue ,  LI, Jun ,  EWING, William, R. ,  SULSKY, Richard, B. ,  LI, James, J. ,  TINO, Joseph, A.

IPC分类号： A61P3/00 ,  A61K31/55 ,  A61K31/54 ,  A61K31/535 ,  A61K31/495 ,  A61K31/50 ,  A61K31/505 ,  A61K31/44 ,  A61K31/445 ,  A61K31/425 ,  A61K31/42

CPC分类号： C07D487/04 ,  C07D231/56 ,  C07D261/20 ,  C07D471/04 ,  C07D513/04

摘要： Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula (I) wherein R1, R1', R2, R3, R4, Xa, Y, Z, and n are as described herein. The compounds provided herein are useful in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength.