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    SUBSTITUTED BENZO(1,2-b:5,4-b')DIPYRAN-4-AMINES AS CCR5 MODULATORS
    1.
    发明授权
    SUBSTITUTED BENZO(1,2-b:5,4-b')DIPYRAN-4-AMINES AS CCR5 MODULATORS 有权
    取代的苯并（1,2-B：5,4-B“）dipyran -4-胺作为CCR5调节剂

    公开(公告)号：EP1156801B1

    公开(公告)日：2004-07-07

    申请号：EP00913848.8

    申请日：2000-03-10

    申请人： SMITHKLINE BEECHAM CORPORATION ,  SmithKline Beecham plc

    发明人： BLANEY, Frank, E. ,  BONDINELL, William, E. ,  CHAN, James, A.

    IPC分类号： A61K31/35 ,  C07D493/02 ,  A61K31/352 ,  A61P11/06

    CPC分类号： C07D493/04 ,  A61K31/352 ,  C07D493/14

    摘要： This invention relates to substituted benzo[1,2-b:5,4-b']dipyran-4-amines which are modulators, agonists or antagonists, of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5, including, but not limited to, asthma and atopic disorders (for example, atopic dermatitis and allergies), rheumatoid arthritis, sarcoidosis and other fibrotic diseases, atherosclerosis, psoriasis, autoimmune diseases such as multiple sclerosis, and inflammatory bowel disease, all in mammals, by the use of substituted benzo[1,2-b:5,4-b']dipyran-4-amines which are CCR5 receptor antagonists. Furthermore, since CD8+ T cells have been implicated in COPD, CCR5 may play a role in their recruitment and therefore antagonists to CCR5 could provide potential therapeutic in the treatment of COPD. Also, since CCR5 is a co-receptor for the entry of HIV into cells, selective receptor modulators may be useful in the treatment of HIV infection.

    COMPOUNDS AND METHODS
    2.
    发明公开
    COMPOUNDS AND METHODS 有权
    取代的苯并（1,2-B：5,4-B“）dipyran -4-胺作为CCR5调节剂

    公开(公告)号：EP1156801A1

    公开(公告)日：2001-11-28

    申请号：EP00913848.8

    申请日：2000-03-10

    申请人： SMITHKLINE BEECHAM CORPORATION ,  Smithkline Beecham PLC

    发明人： BLANEY, Frank, E. ,  BONDINELL, William, E. ,  CHAN, James, A.

    IPC分类号： A61K31/35

    CPC分类号： C07D493/04 ,  A61K31/352 ,  C07D493/14

    摘要： This invention relates to substituted benzo[1,2-b:5,4-b']dipyran-4-amines which are modulators, agonists or antagonists, of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5, including, but not limited to, asthma and atopic disorders (for example, atopic dermatitis and allergies), rheumatoid arthritis, sarcoidosis and other fibrotic diseases, atherosclerosis, psoriasis, autoimmune diseases such as multiple sclerosis, and inflammatory bowel disease, all in mammals, by the use of substituted benzo[1,2-b:5,4-b']dipyran-4-amines which are CCR5 receptor antagonists. Furthermore, since CD8+ T cells have been implicated in COPD, CCR5 may play a role in their recruitment and therefore antagonists to CCR5 could provide potential therapeutic in the treatment of COPD. Also, since CCR5 is a co-receptor for the entry of HIV into cells, selective receptor modulators may be useful in the treatment of HIV infection.

    COMPOUNDS AND METHODS
    3.
    发明公开
    COMPOUNDS AND METHODS 审中-公开
    化合物和方法

    公开(公告)号：EP1037635A1

    公开(公告)日：2000-09-27

    申请号：EP98952132.3

    申请日：1998-10-07

    申请人： Smithkline Beecham ,  SMITHKLINE BEECHAM PLC

    发明人： BONDINELL, William, E. ,  CHAN, James ,  PORTER, Roderick, A. ,  VENSLAVSKY, Joseph, W. ,  DABBS, Steven ,  DAVIES, David, T.

    IPC分类号： A61K31/445 ,  A61K31/53 ,  C07D401/04 ,  C07D401/14

    CPC分类号： C07D401/04 ,  A61K31/454 ,  C07D401/14

    摘要： This invention relates to substituted 3-(4-piperidinyl)indoles which are modulators, agonists or antagonists, of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5, including, but not limited to, asthma and atopic disorders (for example, atopic dermatitis and allergies), rheumatoid arthritis, sarcoidosis and other fibrotic diseases, atherosclerosis, psoriasis, autoimmune diseases such as multiple sclerosis, and inflammatory bowel disease, all in mammals, by the use of substituted 3-(4-piperidinyl)indoles which are CCR5 receptor modulators. Furthermore, since CD8+ T cells have been implicated in Chronic Obstructive Pulmonary Disease ('COPD'), CCR5 may play a role in their recruitment and therefore antagonists to CCR5 could provide potential therapeutic in the treatment of COPD. Also, since CCR5 is a co-receptor for the entry of Human Immunodeficiency Virus ('HIV') into cells, receptor modulators may be useful in the treatment of HIV infection.

    摘要翻译： 本发明涉及取代的3-（4-哌啶基）吲哚，其为CCR5受体的调节剂，激动剂或拮抗剂。 此外，本发明涉及治疗和预防由CCR5介导的疾病状态，包括但不限于哮喘和特应性疾病（例如特应性皮炎和变态反应），类风湿性关节炎，结节病和其他纤维化疾病，动脉粥样硬化， 牛皮癣，自身免疫性疾病如多发性硬化症和炎性肠病，所有这些在哺乳动物中都是通过使用取代的3-（4-哌啶基）吲哚（它们是CCR5受体调节剂）来实现的。 此外，由于CD8 + T细胞与慢性阻塞性肺病（'COPD'）有关，CCR5可能在其募集中发挥作用，因此CCR5的拮抗剂可为COPD的治疗提供潜在治疗。 而且，因为CCR5是人免疫缺陷病毒（“HIV”）进入细胞的共同受体，所以受体调节剂可用于治疗HIV感染。

    BETA-LACTAM INHIBITORS OF CoA-IT
    5.
    发明公开
    BETA-LACTAM INHIBITORS OF CoA-IT 失效
    BETA-LACTAM INHIBITOREN DES Co A-IT

    公开(公告)号：EP1011663A1

    公开(公告)日：2000-06-28

    申请号：EP98920353.4

    申请日：1998-05-08

    申请人： SMITHKLINE BEECHAM CORPORATION

    发明人： BONDINELL, William, E. ,  WINKLER, James, David

    IPC分类号： A61K31/395

    CPC分类号： C07D405/12 ,  A61K31/397 ,  A61K31/4436 ,  C07D205/085 ,  C07D205/095 ,  C07D409/14

    摘要： This invention relates to a novel method for treating disease or disorders mediated by the lipid inflammatory mediators, arachidonic acid, its metabolites and/or platelet activating factor (PAF), which method comprising administering to a mammal in need thereof an effective Coenzyme A independent transacylase (CoA-IT) inhibiting amount of a compound of formula (I). This invention also relates to a method of treating or reducing inflammation in a mammal in need thereof, which comprises administering to said mammal an effective amount of a compound or composition of formula (I).

    INTEGRIN RECEPTOR ANTAGONISTS
    6.
    发明公开
    INTEGRIN RECEPTOR ANTAGONISTS 失效
    整合素受体拮抗剂

    公开(公告)号：EP0910563A1

    公开(公告)日：1999-04-28

    申请号：EP96923553.0

    申请日：1996-06-28

    申请人： SMITHKLINE BEECHAM CORPORATION

    发明人： BONDINELL, William, E. ,  MILLER, William, H.

    IPC分类号： C07C ,  C07D ,  C07D235 ,  A61K31 ,  A61P9 ,  A61P19 ,  A61P43 ,  C07C235 ,  C07D211 ,  C07D213 ,  C07D233 ,  C07D403 ,  F01C1 ,  F01C21 ,  F02B53

    CPC分类号： C07D211/26 ,  C07D213/74 ,  C07D235/14 ,  C07D235/16

    摘要： Compounds of formula (I) wherein A1 is C or N; E is a five- or six-membered heteroaromatic or six-membered aromatic ring optionally substituted by R?3 or R4; X1-X2 is CHR1-CH, CR1=CH, NR1¿-CH, S(O)¿u?-CH or O-CH; X?3 is CR5R5', NR5¿, S(O)¿u? or O; R?2¿ is -OR', -NR'R', -NR'SO¿2?R'', -NR'OR', -OCR'2C(O)OR', -OCR'2OC(O)-R', -OCR'2C(O)NR'2, CF3 or -COCR'2R?2'; R3, R4 and R7¿ are independently H, halo, -OR?12, -SR12¿, -CN, -NR'R12, -NO2, -CF3, CF3S(O)r-, -CO2R', -CONR'2, R14-C0-6alkyl-, R14-C1-6oxoalkyl-, R14-C2-6alkenyl-, R14-C2-6alkynyl-, R14-C0-6alkyloxy-, R14-C0-6alkylamino- or R14-C0-6alkyl-S(O)r-; R6 is W-(CR'¿2?)q-Z-(CR'R?10)¿r-U-(CR'2)s-V- or W'-(CR'2)q-U-(CR'2)s- U and V are absent or CO, CR'2, C(=CR152), S(O)n, O, NR?15, CR15'OR15¿, CR'(OR')CR'¿2?, CR'2CR'(OR'), C(O)CR'2, CR?15¿2C(O), CONR?15, NR15¿CO, OC(O), C(O)O, C(S)O, OC(S), C(S)NR?15, NR15¿C(S), SO¿2?NR?15, NR15SO¿2, N=N, NR?15NR15, NR15CR15¿2, NR15CR152, CR152O, OCR152, C$(m)ZC, CR15=CR15, Het, or Ar, provided that U and V are not simultaneously absent; and W and W' are a nitrogen-containing substituent, and integrin receptor antagonists.

    摘要翻译： 其中A1是C或N的式（I）化合物; E是任选被R 13或R 4取代的五元或六元杂芳族或六元芳族环; X 1 -X 2是CHR 1 -CH，CR 1 = CH，NR 1 -CH，S（O）-CH 2或CH 2; X 3是CR 5 R 5'，NR 5，S（O） 或O; （O）OR'， - OR'， - NR'R'， - NR'SO 2 R''， - NR'OR'， - R'， - OCR'2C（O）NR'2，CF3或-COCR'2R'2'; R 3，R 4和R 7独立地为H，卤素，-OR 12，-SR 12，-CN，-NR'R 12，-NO 2，-CF 3，CF 3 S（O）r - ，-CO 2 R'， - CONR'2 ，R14-C0-6烷基 - ，R14-C1-6氧代烷基 - ，R14-C2-6烯基 - ，R14-C2-6炔基 - ，R14-C0-6烷氧基 - ，R14-C0-6烷基氨基 - 或R14-C0-6烷基-S （要么-; R6是W-（CR'2）qZ-（CR'R'10）∪RU-（CR'2）sV-或W' - （CR'2）qU-（CR'2）s-U和 （= CR152），S（O）n，O，NR15，CR15'OR15'，CR'（OR'）CR'2'，CR'2CR'（ （O），C（O）O，C（S）O，OC（S）），C（O）CR'2，CR 15 C（O），CONR 15，NR 15 CO， ，C（S）NR 15，NR 15 C（S），SO 2 NR 15，NR 15 SO 2，N = N，NR 15 NR 15，NR 15 CR 15，NR 15 CR 152，CR 15 2 O，OCR 152， ）ZC，CR15 = CR15，Het或Ar，条件是U和V不同时不存在; W和W'是含氮取代基和整联蛋白受体拮抗剂。

    COMPOUNDS AND METHODS
    7.
    发明授权
    COMPOUNDS AND METHODS 有权
    化合物和方法

    公开(公告)号：EP1140072B1

    公开(公告)日：2004-04-14

    申请号：EP99967619.0

    申请日：1999-12-28

    申请人： SMITHKLINE BEECHAM CORPORATION

    发明人： BONDINELL, William, E. ,  KU, Thomas, W. ,  WANG, Ning

    IPC分类号： A61K31/41 ,  A61K31/36 ,  A61K31/135 ,  A61K31/165

    CPC分类号： A61K31/167

    摘要： This invention relates to substituted benzanilides which are modulators, agonists or antagonists, of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5, including, but not limited to, asthma and atopic disorders (for example, atopic dermatitis and allergies), rheumatoid arthritis, sarcoidosis and other fibrotic diseases, atherosclerosis, psoriasis, autoimmune diseases such as multiple sclerosis, and inflammatory bowel disease, all in mammals, by the use of substituted benzanilides which are CCR5 receptor antagonists. Furthermore, since CD8+ T cells have been implicated in COPD, CCR5 may play a role in their recruitment and therefore antagonists to CCR5 could provide potential therapeutic in the treatment of COPD. Also, since CCR5 is a co-receptor for the entry of HIV into cells, selective receptor modulators may be useful in the treatment of HIV infection.

    摘要翻译： 本发明涉及取代的苯甲酰苯胺类化合物，它们是CCR5受体的调节剂，激动剂或拮抗剂。 此外，本发明涉及治疗和预防由CCR5介导的疾病状态，包括但不限于哮喘和特应性疾病（例如特应性皮炎和变态反应），类风湿性关节炎，结节病和其他纤维化疾病，动脉粥样硬化， 牛皮癣，自身免疫性疾病如多发性硬化症和炎症性肠病，都是在哺乳动物中，通过使用取代的苯甲酰苯胺类（它们是CCR5受体拮抗剂）。 此外，由于CD8 + T细胞与COPD有关，CCR5可能在其募集中发挥作用，因此CCR5的拮抗剂可为COPD的治疗提供潜在治疗。 而且，因为CCR5是HIV进入细胞的辅助受体，所以选择性受体调节剂可用于治疗HIV感染。

    VITRONECTIN RECEPTOR ANTAGONISTS
    9.
    发明公开
    VITRONECTIN RECEPTOR ANTAGONISTS 失效
    连素拮抗剂

    公开(公告)号：EP0906103A1

    公开(公告)日：1999-04-07

    申请号：EP96943818.0

    申请日：1996-12-20

    申请人： SMITHKLINE BEECHAM CORPORATION

    发明人： ALI, Fadia, E. ,  BONDINELL, William, E. ,  KEENAN, Richard, M. ,  KU, Thomas, Wen, Fu ,  MILLER, William, H. ,  SAMANEN, James

    IPC分类号： A61K31 ,  A61P7 ,  A61P9 ,  A61P19 ,  A61P29 ,  A61P35 ,  A61P43 ,  C07D213 ,  C07D401 ,  C07D403 ,  C07D405 ,  C07D413 ,  C07D487

    CPC分类号： C07D213/74 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D487/04

    摘要： Compounds of formula (I) are disclosed, wherein: A is a fibrinogen antagonist template; W is a linking moiety of the form -(CHRg)a-U-(CHRg)b-V-; Q?1, Q2, Q3 and Q4¿ are independently N or C-Ry, provided that no more than one of Q?1, Q2, Q3 and Q4¿ is N; R' is H or C¿1-6?alkyl, C3-7cycloalkyl-C0-6alkyl or Ar-C0-6alkyl; R?g¿ is H or C¿1-6?alkyl, Het-C0-6alkyl, C3-7cycloalkyl-C0-6alkyl or Ar-C0-6alkyl; R?k is Rg¿, -C(O)Rg or -C(O)ORg Ri is H, C¿1-6?alkyl, Het-C0-6alkyl, C3-7cycloalkyl-C0-6alkyl, Ar-C0-6alkyl, Het-C0-6alkyl-U'-C1-6alkyl, C3-7cycloalkyl-C0-6alkyl-U'-C1-6alkyl or Ar-C0-6alkyl-U'-C1-6alkyl; R?y¿ is H, halo, -ORg, -SRg, -CN, -NR?gRk, -NO¿2, -CF3, CF3S(O)r-, -CO2R?g, -CORg¿ or -CONRg2, or C1-6alkyl optionally substituted by halo, -ORg, -SRg, -CN, -NRgR'', -NO¿2?, -CF3, R'S(O)3-, -CO2R?g, -CORg¿ or -CONRg2; U and V are absent or CO, CRg2, C(=CRg2), S(O)c, O, NR?g, CRgORg, CRg(ORk)CRg¿2, CRg2CRg(ORk), C(O)CRg2, CRg2C(O), CONRi, NRiCO, OC(O), C(O)O, C(S)O, OC(S), C(S)NRg, NRgC(S), S(O)¿2?NR?g, NRgS(O)¿2N=N, NR?gNRg, NRgCRg¿2, NRgCRg2, CRg2O, OCRg2, CRg=CRg, C C, Ar or Het; a is 0, 1, 2 or 3; b is 0, 1 or 2; c is 0, 1 or 2; r is 0, 1 or 2; and u is 0 or 1; or pharmaceutically acceptable salts thereof, which are vitronectin receptor antagonists useful in the treatment of osteoporosis.