公开(公告)号：EP2405913A1

公开(公告)日：2012-01-18

申请号：EP10707791.9

申请日：2010-03-09

申请人： Bristol-Myers Squibb Company

发明人： AHMAD, Saleem ,  WASHBURN, William, N. ,  HERNANDEZ, Andres, S. ,  ROBL, Jeffrey, A. ,  NGU, Khehyong ,  WANG, Zhenghua

IPC分类号： A61K31/4412 ,  A61P3/04 ,  C07D213/38 ,  C07D213/74 ,  C07D213/30 ,  C07D213/32 ,  C07D213/26 ,  C07D213/68 ,  C07D401/04 ,  A61K31/4409 ,  A61K31/4427

CPC分类号： C07D213/38 ,  A61K31/4412 ,  A61K31/4427 ,  C07D213/26 ,  C07D213/30 ,  C07D213/32 ,  C07D213/68 ,  C07D401/04

摘要： MCHR1 antagonists are provided having the following Formula I: wherein A
1 and A
2 are independently C or N; E is C or N; D
1 is a bond, -CR
8 R
9 X-, -XCR
8 R
9 -, -CHR
8 CHR
9 -, -CR
10 =CR
10' -, -C≡C-, or 1,2-cyclopropyl; X is O, S or -NR
11 ; R
1 , R
2 , and R
3 are independently selected from the group consisting of hydrogen, halogen, lower alkyl, lower cycloalkyl, lower cycloalkoxy, -CF
3 , -OCF
3 , -OR
12 and -SR
12 ; G is O or S; D
2 is lower alkyl, lower cycloalkyl, lower alkylcycloalkyl, lower cycloalkylalkyl, lower cycloalkoxyalkyl or lower alkycycloalkoxy; Z
1 and Z
2 are independently hydrogen, halogen, lower alkyl, lower cycloalkyl, lower alkoxy, lower cycloalkoxy, halo, -CF
3 , -OCONR
14 R
14' , -CN, -CONR
14 R
14' , -SOR
12 , -SO
2 R
12 , -NR
14 COR
14' , -NR
14 CO
2 R
14' , -CO
2 R
12 , NR
14 SO
2 R
12 or -COR
12 provided that if Z
1 is -CH
3 and one of R
1 , R
2 , or R
3 is F, then Z
2 cannot be H;; R
5 , R
6 , and R
7 are independently selected from the group consisting of hydrogen, halogen, lower alkyl, lower cycloalkyl, -CF
3 , -SR
12 , lower alkoxy, lower cycloalkoxy, -OCH
2 OMe, -CN, -CONR
14 R
14' , SOR
12 , SO
2 R
12 , NR
14 COR
14' , NR
14 CO
2 R
12 , CO
2 R
12 , NR
14 SO
2 R
12 and -COR
12 ; R
8 , R
9 , R
10 , R
10' , R
11 are independently hydrogen or lower alkyl; R
12 is lower alkyl or lower cycloalkyl; and R
14 and R
14' are independently H, lower alkyl, lower cycloalkyl or R
14 and R
14' together with the N to which they are attached form a ring having 4 to 7 atoms. Such compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, IBD, depression, and anxiety.

公开(公告)号：EP2925749B1

公开(公告)日：2016-10-26

申请号：EP13795973.0

申请日：2013-11-15

申请人： Bristol-Myers Squibb Company

发明人： ELLSWORTH, Bruce, A. ,  SHI, Jun ,  EWING, William, R. ,  JURICA, Elizabeth, A. ,  HERNANDEZ, Andres, S. ,  WU, Ximao ,  GU, Zhengxiang ,  HONG, Zhenqiu ,  O'CONNOR, Stephen, P.

IPC分类号： C07D405/14 ,  C07D401/12 ,  C07D405/12 ,  C07D417/14 ,  C07D451/06 ,  C07D403/12 ,  C07D401/10 ,  C07D487/08 ,  C07D211/16 ,  C07D211/18 ,  C07D413/14 ,  A61K31/4155 ,  A61P3/10 ,  C07D401/14

CPC分类号： C07D401/12 ,  A61K31/4155 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/46 ,  A61K31/497 ,  A61K31/506 ,  A61K31/55 ,  A61K45/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D451/06 ,  C07D471/08 ,  C07D487/08

公开(公告)号：EP1175213A2

公开(公告)日：2002-01-30

申请号：EP00913733.2

申请日：2000-03-02

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： ROBL, Jeffrey ,  TINO, Joseph, A. ,  HERNANDEZ, Andres, S. ,  LI, James, J. ,  LI, Jun ,  SWARTZ, Stephen, G.

IPC分类号： A61K31/41 ,  A61K31/4178 ,  A61K31/4439 ,  A61K31/5377 ,  A61P3/04 ,  A61P5/08 ,  A61P5/48 ,  A61P19/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14

CPC分类号： C07D233/54 ,  C07D235/14 ,  C07D249/08 ,  C07D249/12 ,  C07D257/04 ,  C07D263/32 ,  C07D271/06 ,  C07D277/28 ,  C07D277/64 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/06 ,  C07D417/06 ,  C07D417/12

摘要： Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength. The heterocyclic aromatic compounds have structure (I) including pharmaceutically acceptable salts thereof and all stereoisomers thereof, wherein Xa is heteroaryl, preferably (a), (b) or (c) and R1, R1a, R6, Y, Xb, A, B, Z, R3, R4, R4a, R5 and R5a are as defined herein.

公开(公告)号：EP2925749A1

公开(公告)日：2015-10-07

申请号：EP13795973.0

申请日：2013-11-15

申请人： Bristol-Myers Squibb Company

发明人： ELLSWORTH, Bruce, A. ,  SHI, Jun ,  EWING, William, R. ,  JURICA, Elizabeth, A. ,  HERNANDEZ, Andres, S. ,  WU, Ximao ,  GU, Zhengxiang ,  HONG, Zhenqiu ,  O'CONNOR, Stephen, P.

IPC分类号： C07D405/14 ,  C07D401/12 ,  C07D405/12 ,  C07D417/14 ,  C07D451/06 ,  C07D403/12 ,  C07D401/10 ,  C07D487/08 ,  C07D211/16 ,  C07D211/18 ,  C07D413/14 ,  A61K31/4155 ,  A61P3/10 ,  C07D401/14

CPC分类号： C07D401/12 ,  A61K31/4155 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/46 ,  A61K31/497 ,  A61K31/506 ,  A61K31/55 ,  A61K45/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D451/06 ,  C07D471/08 ,  C07D487/08

摘要： The present invention provides compounds of Formula (I): (Formula (I), or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.

公开(公告)号：EP1799208A2

公开(公告)日：2007-06-27

申请号：EP05812742.4

申请日：2005-10-12

申请人： Bristol-Myers Squibb Company

发明人： EWING, William, R. ,  LI, Jun ,  SULSKY, Richard, B. ,  HERNANDEZ, Andres, S.

IPC分类号： A61K31/415 ,  C07D231/12

CPC分类号： C07D231/12 ,  C07D231/20 ,  C07D249/08 ,  C07D261/04 ,  C07D261/08 ,  C07D271/10 ,  C07D271/107 ,  C07D403/12 ,  C07D413/12

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, Rla, R6, Xa, Xb and Y 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.