公开(公告)号：EP2193119A1

公开(公告)日：2010-06-09

申请号：EP08787483.0

申请日：2008-08-26

Applicant: Abbott GmbH & Co. KG ,  Abbott Laboratories

Inventor： MACK, Helmut ,  TEUSCH, Nicole ,  MÜLLER, Bernhard K. ,  HORNBERGER, Wilfried ,  JARVIS, Michael F. ,  SAUER, Daryl ,  SWANN, Steve Jr ,  HOBSON, Adrian Donald ,  KEDDY, Ryan ,  BONAFOUX, Dominique ,  VASUDEVAN, Anil

IPC: C07D213/56 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  A61K31/44 ,  A61K31/4427 ,  A61P9/00 ,  A61P25/00 ,  A61P35/00 ,  A61P29/00

CPC classification number: C07D401/12 ,  C07D213/56 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

Abstract: The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs). R1 and R2 are, independently of each other, hydrogen, hydroxy, cyano, C1-C8-alkyl, C1- C8-haloalkyl, C1-C8-alkoxy or C1-C8-haloalkoxy; R3, R4, R5 and R6 are, independently of each other, hydrogen, hydroxy, halogen, cyano, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy, C1-C8-haloalkoxy, amino, C1-C8-alkylamino or di-(C1-C8-alkyl)-amino; R7 is hydrogen, C1-C8-alkyl, C1-C8-haloalkyl, aryl or aryl-C1-C8-alkyl; R8 is a group of the formula -X-W, where X is a single bond, C1-C4-alkylene or C1-C4-alkylene-O-, where the alkylene group in the three last-mentioned radicals may be linear or branched and may be partly or fully halogenated and/or may be substituted by a hydroxyl group and/or may be interrupted by an oxygen atom; and W is a cyclic radical selected from phenyl and a 5- or 6-membered saturated, partly unsaturated or aromatic heterocyclic ring which contains as ring members 1, 2 or 3 heteroatoms selected from O, S and N and optionally 1 or 2 carbonyl groups; R9 is a group of the formula -Y-Z, where Z is hydrogen, halogen, OR11, NR12R13, S(O)m-R14, phenyl which may carry 1, 2, 3 or 4 substituents R15 or a 5- or 6-membered saturated, partly unsaturated or aromatic heterocyclic ring; and Y is linear or branched C1C4-alkylene which may be partly or fully halogenated and/or may be substituted by a hydroxyl group and/or a phenyl ring; or, in case Z is phenyl or the 5- or 6-membered heterocyclic ring as defined above, Y can also be a single bond.

公开(公告)号：EP2167491A1

公开(公告)日：2010-03-31

申请号：EP08770094.4

申请日：2008-06-04

Applicant: Abbott Laboratories ,  Abbott GmbH & Co. KG

Inventor： AKRITOPOULOU-ZANZE, Irini ,  WAKEFIELD, Brian D ,  MACK, Helmut ,  TURNER, Sean C ,  GASIECKI, Alan F ,  GRACIAS, Vijaya J ,  SARRIS, Kathy ,  KALVIN, Douglas M ,  MICHMERHUIZEN, Melissa J ,  SHUAI, Qi ,  PATEL, Jyoti R ,  BAKKER, Margaretha ,  TEUSCH, Nicole ,  JOHNSON, Eric F. ,  KOVAR, Peter J ,  DJURIC, Stevan W ,  LONG, Andrew J ,  VASUDEVAN, Anil ,  HOBSON, Adrian ,  ST. JOHN MOORE, Nigel ,  WANG, Lu ,  GEORGE, Dawn ,  LI, Biqin ,  FRANK, Kristine

IPC: C07D403/04 ,  C07D413/04 ,  C07D417/04

CPC classification number: C07D403/04 ,  C07D413/04 ,  C07D417/04

Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R1, R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.

公开(公告)号：EP1534703A2

公开(公告)日：2005-06-01

申请号：EP03760268.7

申请日：2003-06-11

Applicant: ABBOTT LABORATORIES

Inventor： BLACKBURN, Christopher ,  LAI, Su-jen ,  LEE, Jennifer, G. ,  MAGUIRE, Martin ,  PATANE, Michael, A. ,  LAMARCHE, Matthew, J. ,  CULLIS, Courtney, A. ,  BROWN, James ,  VASUDEVAN, Anil ,  FREEMAN, Jennifer, C. ,  MULHERN, Mathew, M. ,  LYNCH, John, K. ,  GAO, Ju ,  WODKA, Dariusz ,  SOUERS, Andrew, J. ,  IYENGAR, Rajesh

IPC: C07D405/00

CPC classification number: C07D405/14 ,  C07D401/14 ,  C07D405/12 ,  C07D409/14 ,  C07D413/14

Abstract: This invention provides compounds that are antagonists of melanin concentrating hormone receptor-1 (MCH-R1). The compounds are represented by formula (I): where m is zero or one, n is zero to two, Y is oxygen or -N (R )-, R , R , R , R , R , R , and Ring A are defined in the specification. Coumarin and quinolone compounds where R and R together form a fused benzo ring are preferred. The invention also provides compounds of formula (VI) where the coumarin moiety is replaced by a quinazolinone ring. The compounds are useful for treating MCH-R1-related disorders, particularly overweight conditions including obesity.

公开(公告)号：EP2323659A1

公开(公告)日：2011-05-25

申请号：EP09805407.5

申请日：2009-08-03

Applicant: Abbott Laboratories

Inventor： VASUDEVAN, Anil ,  BROWN, Brian, S. ,  KEDDY, Ryan, G. ,  HOBSON, Adrian, D.

IPC: A61K31/454 ,  A61P9/00

CPC classification number: A61K31/437 ,  C07D471/04

Abstract: Disclosed herein are compounds of formula (I) or pharmaceutical acceptable salts thereof, wherein A, X
1 , X
2 , R
1 , R
2 , R
3 , m, n, and p are defined in the specification. Compositions including the compounds which can be useful for inhibiting Rho kinase (ROCK) and methods for using the compositions are also described.

公开(公告)号：EP2185538A2

公开(公告)日：2010-05-19

申请号：EP08797444.0

申请日：2008-08-08

Applicant: Abbott Laboratories

Inventor： KYM, Philip R ,  BROWN, Brian S ,  DAANEN, Jerome F ,  GOMTSYAN, Arthur R ,  KEDDY, Ryan G ,  KORT, Michael ,  MATULENKO, Mark A ,  VASUDEVAN, Anil ,  JINKERSON, Tammie, K.

IPC: C07D401/04 ,  A61K31/4545

CPC classification number: C07D401/04

Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, and R3, are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.

Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐，前药，前药的盐或其组合，其中R 1，R 2和R 3在说明书中定义。 还公开了包含此类化合物的组合物以及使用此类化合物和组合物治疗疾病和病症的方法。

公开(公告)号：EP1301480A1

公开(公告)日：2003-04-16

申请号：EP01952653.2

申请日：2001-07-11

Applicant: ABBOTT LABORATORIES

Inventor： BENNANI, Youssef, L. ,  FAGHIH, Ramin ,  DWIGHT, Wesley, J. ,  VASUDEVAN, Anil ,  CONNER, Scott, E.

IPC: C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D403/04 ,  C07D417/14 ,  A61K31/4025 ,  A61P9/10 ,  A61P25/28 ,  A61P29/00

CPC classification number: C07D401/12 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D417/14

Abstract: Compounds of formula (I) are useful in treating diseases or conditions prevented by or ameliorated with histamine-3 receptor ligands. Also disclosed are histamine-3 receptor ligand compositions and methods of antagonizing or agonizing histamine-3 receptors.

公开(公告)号：EP2220059B1

公开(公告)日：2011-08-03

申请号：EP08841479.2

申请日：2008-10-25

Applicant: Abbott Laboratories

Inventor： PERNER, Richard J. ,  KOENIG, John R. ,  DIDOMENICO, Stanley, Jr. ,  BAYBURT, Erol, K. ,  DAANEN, Jerome, F. ,  GOMTSYAN, Arthur, R. ,  KORT, Michael E. ,  KYM, Philip R. ,  VASUDEVAN, Anil ,  SCHMIDT, Robert, G. ,  VOIGHT, Eric

IPC: C07D263/48 ,  C07D413/04 ,  C07D413/12 ,  A61K31/421 ,  A61P29/00

CPC classification number: C07D413/12 ,  C07D263/48 ,  C07D413/04

Abstract: Compounds of formula (I) wherein R1, R2, R4, and W are defined in the description are TRPV1 antagonists with CNS penetration. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.

公开(公告)号：EP2220059A1

公开(公告)日：2010-08-25

申请号：EP08841479.2

申请日：2008-10-25

Applicant: Abbott Laboratories

Inventor： PERNER, Richard J. ,  KOENIG, John R. ,  DIDOMENICO, Stanley, Jr. ,  BAYBURT, Erol, K. ,  DAANEN, Jerome, F. ,  GOMTSYAN, Arthur, R. ,  KORT, Michael E. ,  KYM, Philip R. ,  VASUDEVAN, Anil ,  SCHMIDT, Robert, G. ,  VOIGHT, Eric

IPC: C07D263/48 ,  C07D413/04 ,  C07D413/12 ,  A61K31/421 ,  A61P29/00

CPC classification number: C07D413/12 ,  C07D263/48 ,  C07D413/04

Abstract: Compounds of formula (I) wherein R1, R2, R4, and W are defined in the description are TRPV1 antagonists with CNS penetration. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.

Abstract translation: 其中R 1，R 2，R 4和W在说明书中定义的式（I）化合物是具有CNS穿透的TRPV1拮抗剂。 还公开了包含此类化合物的组合物以及使用此类化合物和组合物治疗疾病和病症的方法。

公开(公告)号：EP1549613A1

公开(公告)日：2005-07-06

申请号：EP03773182.5

申请日：2003-10-06

Applicant: Abbott Laboratories

Inventor： COMESS, Kenneth, M. ,  ERICKSON, Scott, A. ,  HENKIN, Jack ,  KALVIN, Douglas, M. ,  KAWAI, Megumi ,  KIM, Ki, H. ,  BAMAUNG, Nwe, Y. ,  PARK, Chan, Hoon ,  SHEPPARD, George, S. ,  VASUDEVAN, Anil ,  WANG, Jieyi ,  BARNES, David, M. ,  FIDANZE, Steve, D. ,  KOLACZKOWSKI, Lawrence ,  MANTEI, Robert, A. ,  PARK, David, C. ,  SANDERS, William, J. ,  TEDROW, Jason, S. ,  WANG, Gary, T.

IPC: C07C311/08

CPC classification number: C07C323/25 ,  C07C311/08 ,  C07C311/13 ,  C07C311/21 ,  C07C311/29 ,  C07C311/37 ,  C07C311/44 ,  C07C311/46 ,  C07C317/28 ,  C07C323/49 ,  C07C323/63 ,  C07C323/67 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2602/12 ,  C07D209/08 ,  C07D209/42 ,  C07D213/70 ,  C07D213/71 ,  C07D215/36 ,  C07D215/48 ,  C07D231/18 ,  C07D233/54 ,  C07D233/84 ,  C07D261/10 ,  C07D285/06 ,  C07D285/14 ,  C07D333/34 ,  C07D333/38 ,  C07D413/04

Abstract: Compounds having methionine aminopeptidase-2 inhibitory (MetAP2) are described. Also described are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating cancer.

Abstract translation: 描述了具有甲硫氨酸氨基肽酶-2抑制剂（MetAP2）的化合物。 还描述了包含该化合物的药物组合物，使用该化合物的治疗方法，抑制血管发生的方法和治疗癌症的方法。