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    • 4. 发明申请
    • BENZOXAZOCINES AND THEIR THERAPEUTIC USE
    • 苯并噻唑及其治疗用途
    • WO2006095187A1
    • 2006-09-14
    • PCT/GB2006/000858
    • 2006-03-10
    • SOSEI R & D LTD.BAXTER, Andrew, Douglas
    • BAXTER, Andrew, Douglas
    • C07D267/22A61K31/395A61P25/04
    • C07D267/22
    • A compound selected from (1 S )-8-cyano-5-methyl-1-(3-methoxy)phenyl-1,3,4,6-tetrahydro-5H-benz[f]-2,5- oxazocine; (1 R )-8-cyano-5-methyl-1-(3-methoxy)phenyl-1,3,4,6-tetrahydro-5H-benz[f]-2,5- oxazocine; (1 S )-8-cyclopropyl-5-methyl-1-(3-methoxy)phenyl-1,3,4,6-tetrahydro-5H-benz[f]- 2,5-oxazocine; (1 S )-8-cyclopropyl-5-methyl-1-(3-methoxy)phenyl-1,3,4,6-tetrahydro-5H-benz[f]-2,5-oxazocine; (1 S )-5-methyl-1-(3-methoxy)phenyl-1 ,3,4,6-tetrahydro-5H-benz[f]-2,5- oxazocine-8-carboxamide; (1 R )-5-methyl-1-(3-methoxy)phenyl-1,3,4,6-tetrahydro-5H-benz[f]-2,5- oxazocine-8-carboxamide; and the salts thereof. These compounds have therapeutic utility.
    • 选自(1S)-8-氰基-5-甲基-1-(3-甲氧基)苯基-1,3,4,6-四氢-5H-苯并[f] -2,5-恶唑辛的化合物; (1R)-8-氰基-5-甲基-1-(3-甲氧基)苯基-1,3,4,6-四氢-5H-苯并[f] -2,5-恶唑辛; (1S)-8-环丙基-5-甲基-1-(3-甲氧基)苯基-1,3,4,6-四氢-5H-苯并[f] -2,5-恶唑辛; (1S)-8-环丙基-5-甲基-1-(3-甲氧基)苯基-1,3,4,6-四氢-5H-苯并[f] -2,5-恶唑辛; (1S)-5-甲基-1-(3-甲氧基)苯基-1,3,4,6-四氢-5H-苯并[f] -2,5-恶唑烷-8-甲酰胺; (1R)-5-甲基-1-(3-甲氧基)苯基-1,3,4,6-四氢-5H-苯并[f] -2,5-恶唑烷-8-甲酰胺; 及其盐。 这些化合物具有治疗作用。
    • 7. 发明申请
    • THE TREATMENT OF INFLAMMATORY DISORDERS AND PAIN
    • 治疗炎症性疾病和疼痛
    • WO2006027579A3
    • 2007-03-08
    • PCT/GB2005003452
    • 2005-09-07
    • SOSEI R & D LTDBAXTER ANDREW DOUGLASBREW JOHN
    • BAXTER ANDREW DOUGLASBREW JOHN
    • A61K31/137A61K31/138A61K31/37A61K31/4458A61K31/4704A61P1/00A61P1/02A61P11/06A61P11/08A61P13/12A61P17/00A61P19/02A61P19/10A61P25/02A61P29/02
    • A61K31/138A61K31/137A61K31/37A61K31/4458A61K31/4704
    • Compounds that may be used for the treatment or prevention of a condition associated with T-cell proliferation or that is mediated by pro-inflammatory cytokines are of formula (I): wherein R 1 is CHR 4 -OR 5 or CHR 4 -SR 5 , or aryl or heteroaryl optionally substituted with one or more groups R 6 ; R 2 is alkyl or is part of a ring with R 3 ; R 3 is H, alkyl or CH 2 (when forming part of a ring with R 2 ); R 4 is H or alkyl or is part of a ring with R 5 ; R 5 is aryl or heteroaryl optionally substituted with R 7 ; each R 6 is independently alkyl, CF 3 , OH, Oalkyl, OCOalkyl, CONH 2 , CN, halogen, NH 2 , NO 2 , NHCHO, NHCONH 2 , NHSO 2 alkyl, CONH 2 , SOMe, SO 2 NH 2 , Salkyl, CH 2 SO 2 alkyl or OCONalkyl 2 ; R 7 is R 8 or (CH 2 ) n OR 8 , R 9 , CF 3 , OH, OR 9 , OCOR 9 , COR 9 , COOR 9 , CONH 2 , CH 2 CONH 2 , CN, halogen, NH 2 , NO 2 , NHCHO, NHCONH 2 , NHCONHR 7 , NHCON(R 9 ) 2 , NHCOR 9 , NHCOaryl, NHSO 2 Me, CONH 2 , SMe, SOMe or SO 2 NH 2 ; R 8 is (CH 2 ) n OR 9 , (CH) n OR 9 , (CH 2 ) n COOR 9 or (CH 2 ) n COaryl; R 9 is alkyl or cycloalkyl; and n is 1 to 4; or a salt thereof, including clenbuterol and atenolol.
    • 可用于治疗或预防与T细胞增殖相关或由促炎细胞因子介导的病症的化合物具有式(I):其中R 1是CHR 1, 或者任选地被一个或多个基团取代的芳基或杂芳基,其中R 1,R 2,R 3,R 5, > 6 ; R 2是烷基或是具有R 3的环的一部分; R 3是H,烷基或CH 2(当形成具有R 2 2的环的一部分时); R 4是H或烷基或是具有R 5的环的一部分; R 5是任选被R 7取代的芳基或杂芳基; 每个R 6独立地为烷基,CF 3,OH,O烷基,OCO烷基,CONH 2,CN,卤素,NH 2, NH 2 SO 2,NHSO 2,NHCONH 2,NHSO 2烷基,CONH 2,SOMe,SO 2,NH 2,S烷基,CH 2 SO 2烷基或OCON烷基2; R 7是R 8或(CH 2)2,R 2或R 8,R 9,3或3,OH,OR 9,OCOR 9,COR 9, ,COOR 9,CONH 2,CH 2 CONH 2,CN,卤素,NH 2, NH 3,NHCONH 2,NHCONHR 7,NHCON(R 9),N SUB NH 2,NHCOOR 2,NHSO 2 Me,CONH 2,SMe,SOMe或SO 2, / SUB> NH 2 ; R 8是(CH 2)n,(CH 3)n, 或(CH 2)2,或(CH 2)2,或(CH 2) 名词 COaryl; R 9是烷基或环烷基; n为1〜4; 或其盐,包括克伦特罗和阿替洛尔。