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117 条记录 (耗时 0.016 秒)

    INDOLE-TYPE DERIVATIVES AS INHIBITORS OF P38 KINASE
    94.
    发明授权
    INDOLE-TYPE DERIVATIVES AS INHIBITORS OF P38 KINASE 有权
    吲哚-TYPE作为p38激酶抑制剂衍生物

    公开(公告)号：EP1178983B1

    公开(公告)日：2007-10-24

    申请号：EP00939322.4

    申请日：2000-05-19

    申请人： SCIOS INC.

    发明人： MAVUNKEL, Babu, J. ,  CHAKRAVARTY, Sarvajit ,  PERUMATTAM, John, J. ,  DUGAR, Sundeep ,  LU, Qing ,  LIANG, Xi

    IPC分类号： C07D401/06 ,  A61K31/404 ,  A61P43/00 ,  C07D209/24 ,  C07D401/14

    CPC分类号： C07D401/06 ,  C07D209/24 ,  C07D401/14

    摘要： The invention is directed to methods to inhibit p38-α kinase using compounds of formula (1), and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wherein (a) represents a single or double bond; one Z2 is CA or CR8A and the other is CR1, CR12, NR6 or N wherein each R?1, R6 and R8¿ is independently hydrogen or noninterfering substituent; A is -W¿i?-COXjY wherein Y is COR?2¿ or an isostere thereof and R2 is hydrogen or a noninterfering substituent, each of W and X is a spacer of 2-6Å, and each of i and j is independently 0 or 1; Z?3 is NR7¿ or O; each R3 is independently a noninterfering substituent; n is 0-3; each of L?1 and L2¿ is a linker; each R4 is independently a noninterfering substituent; m is 0-4; Z?1 is CR5¿ or N wherein R5 is hydrogen or a noninterfering substituent; each of l and k is an integer from 0-2 wherein the sum of l and k is 0-3; Ar is an aryl group substituted with 0-5 noninterfering substituents, wherein two noninterfering substituents can form a fused ring; and the distance between the atom of Ar linked to L2 and the center of the α ring is 4.5-24Å.

    PIPERIDINE/PIPERAZINE-TYPE INHIBITORS OF P38 KINASE
    96.
    发明授权
    PIPERIDINE/PIPERAZINE-TYPE INHIBITORS OF P38 KINASE 有权
    哌啶基/哌嗪型的P38KINASE抑制剂

    公开(公告)号：EP1353905B1

    公开(公告)日：2007-01-10

    申请号：EP01989111.8

    申请日：2001-11-20

    申请人： SCIOS INC.

    发明人： DUGAR, Sundeep ,  PERUMATTAM, John ,  TESTER, Richland ,  LU, Qing ,  MCENROE, Glenn

    IPC分类号： C07D211/18 ,  C07D513/04 ,  C07D471/04 ,  C07D207/40 ,  A61K31/445 ,  A61P29/00

    CPC分类号： C07D207/416 ,  C07D211/18 ,  C07D401/06 ,  C07D471/04 ,  C07D513/04

    摘要： The invention is directed to inhibition of p38-α kinase using compounds of the formula (1) and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wherein: Ar1 is an aryl group substituted with 0-5 non-interfering substituents, wherein two adjacent noninterfering substituents can form a fused aromatic or nonaromatic ring; L?1 and L2¿ are linkers; each R1 is independently a noninterfering substitutent; Z?1 is CR2¿ or N wherein R2 is hydrogen or a noninterfering substituent; m is 0-4; each of n and p is an integer from 0-2 wherein the some of n and p is 0-3; Ar2 is a substantially planar, monocyclic or polycyclic aromatic moiety having one or more optional ring heteroatoms, said moiety being optionally substituted with one or more optional ring heteroatoms, said moiety being optionally substituted with one or more non-interfering substituents, two or more of which may form a fused ring; Z is W¿1?-COXjY wherein Y is COR?3¿ or an isotere thereof; R3 is a noninterfering substituent, each of W and X is a spacer of 2-6 Å, and each of i and j is independently 0 or 1; wherein the smallest number of covalent bonds is the compound separating the atom of Ar1 bonded to L2 to the atom of Ar2 bonded to L1 is at least 6, where each of said bonds has a bond length of 1.2 to 2.0 angstroms; and/or wherein the distance in space between the atom of Ar1 bonded to L2 and the atom of Ar2 bonded to L1 is 4.5-24 angstroms; with the proviso that the protion of the compound represented by Ar2-Z is not formula (2) wherein formula (3) represents a singel or double bond; n is 0-3; one Z2 is CA or CRA and the other is CR, CR¿2?, NR or N; A is Wi-COXjY wherein Y is COR or an isostere thereof, each of W and X is a spacer of 2-6Å, and each of i and j is independently 0 ot 1; Z?3¿ is NR or O; and each R independently hydrogen or a mominterfering substituent.

    AGONISTS AND ANTAGONISTS OF PERIPHERAL-TYPE BENZODIAZEPINE RECEPTORS
    99.
    发明授权
    AGONISTS AND ANTAGONISTS OF PERIPHERAL-TYPE BENZODIAZEPINE RECEPTORS 有权
    激动剂和苯二氮卓周围型的拮抗剂

    公开(公告)号：EP1140107B1

    公开(公告)日：2006-07-19

    申请号：EP99966269.5

    申请日：1999-12-15

    申请人： SCIOS INC.

    发明人： JOLY, Alison ,  SCHREINER, George, F. ,  STANTON, Lawrence, W. ,  WHITE, R., Tyler

    IPC分类号： A61K31/55 ,  A61K31/47 ,  A61K39/395 ,  A61K31/435 ,  A61K31/40 ,  A61K31/41 ,  A61P9/00

    CPC分类号： C12Q1/6883 ,  C12Q2600/158

    摘要： The invention concerns the use of agonists and antagonists of peripheral-type benzodiazepine receptors (PTBR) in the diagnosis and treatment of cardiac hypertrophy and other circulatory conditions. The invention specifically concerns the use of PTBR antagonists in the prevention or treatment of decompensated cardiac hypertrophy and, eventually, heart failure. The invention also concerns the use of PTBR agonists in the management of conditions calling for increased blood flow or cardiac output, including injury or functional compromise of the heart, increased demand for physical exercise, or an acquired or inherited predisposition to cardiac contractile disfunction. Pharmaceutical compositions for the treatment of such conditions and screening methods to identify PTBR agonists and antagonists are also included.

    HETEROCYCLIC COMPOUNDS AND METHODS TO TREAT CARDIAC FAILURE AND OTHER DISORDERS
    100.
    发明授权
    HETEROCYCLIC COMPOUNDS AND METHODS TO TREAT CARDIAC FAILURE AND OTHER DISORDERS 有权
    HETEROZYCLISCHE衍生物对心力衰竭等疾病的治疗

    公开(公告)号：EP1080078B1

    公开(公告)日：2006-02-01

    申请号：EP99924412.2

    申请日：1999-05-21

    申请人： SCIOS INC.

    发明人： MAVUNKEL, Babu, J. ,  LIU, David, Y. ,  SCHREINER, George, F. ,  LEWICKI, John, A. ,  PERUMATTAM, John, J.

    IPC分类号： C07D235/06 ,  C07D401/06 ,  C07D401/14 ,  C07D209/08 ,  C07D403/06 ,  A61K31/445 ,  A61K31/40 ,  A61K31/41

    CPC分类号： C07D209/08 ,  C07D235/06 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06

    摘要： Compounds of formulae α or β, and the pharmaceutically acceptable salts thereof, wherein each of Z?1 and Z2¿ is independently CR4 or N; where each R4 is independently H or is alkyl (1-6C) or aryl, each of said alkyl or aryl optionally including one or more heteroatoms selected from O, S and N and optionally substituted by one or more of halo, OR, SR, NR¿2?, RCO, COOR, CONR2, OOCR, or NROCR where R is H or alkyl (1-6C), or by one or more CN or =O, or by one or more aliphatic or aromatic 5- or 6-membered rings optionally containing 1-2 heteroatoms; R?1¿ is formula (I); wherein X1 is CO or an isostere thereof; m is 0 or 1; Y is optionally substituted alkyl, optionally substituted aryl, or optionally substituted arylalkyl or two Y taken together may form an alkylene (2-3C) bridge; n is 0 or 2; Z3 is CH or N; X2 is CH, CH¿2? or an isostere thereof; and Ar consists of one or two phenyl moieties directly coupled to X?2¿ optionally substituted by halo, nitro, alkyl(1-6C), alkenyl(1-6C), alkynyl(1-6C), CN or CF¿3?, or by RCO, COOR, CONR2, NR2, OR, SR, OOCR or NROCR wherein R is H or alkyl(1-6C) or by phenyl, itself optionally substituted by the foregoing substituents; R?2¿ is H, or is alkyl(1-6C) or aryl, each or said alkyl or aryl optionally including one heteroatome which is O, S or N, and optionally substituted by one or more of halo, OR, SR, NR¿2?, RCO, COOR, CONR2, OOCR, or NROCR where R is H or alkyl(1-6C), alkynyl(1-6C), or by one or more CN or =O, or by one or more aliphatic or aromatic 5- or 6-membered rings optionally containing 1-2 heteroatoms; R?3¿ is H, halo, NO¿2?, alkyl(1-6C), alkenyl(1-6C), alkynyl(1-6C), CN, OR, SR, NR2, RCO, COOR, CONR2, OOCR, or NROCR where R is H or alkyl(1-6C) are disclosed. These compounds are selective inhibitors of p38α kinase.