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    MORPHOLINYLMETHYLUREAS CCR-3 RECEPTOR ANTAGONIST
    5.
    发明申请
    MORPHOLINYLMETHYLUREAS CCR-3 RECEPTOR ANTAGONIST 审中-公开

    公开(公告)号：WO2003099798A1

    公开(公告)日：2003-08-14

    申请号：PCT/EP2003/005597

    申请日：2003-05-26

    Applicant: GLAXO GROUP LIMITED ,  COOK, Caroline, Mary ,  ELDRED, Colin, David ,  HARRISON, Lee, Andrew

    Inventor： COOK, Caroline, Mary ,  ELDRED, Colin, David ,  HARRISON, Lee, Andrew

    IPC: C07D265/30

    Abstract: Compounds of formula (I): wherein:R 1 represents C 3-8 cycloalkyl-Y 1 -, aryl-Y 1 -, heteroaryl-Y 1 -, aryl- G-Y 1 -, heteroaryl-G-Y 1 -, C 1-6 alkyl-G-Y 1 -, J 1 -Y 1 -, R 22 R 23 N-Y 1 -, R 22 R 23 N-CO-Y 1 - or R 24 -CONR 22 -Y 1 -; Q represents -(CR 19 R 20 )(CR 19a R 20a )t-, wherein t represents an integer from 0 to 3;R 2 and R 3 independently represent hydrogen or C 1-6 alkyl;X represents ethylene or a group of formula CR e R f wherein R e and R f independently represent hydrogen or C 1-4 alkyl or R e and R f may together with the carbon atom to which they are attached form a C 3-8 cycloalkyl group; R 4 and R 5 independently represent hydrogen or C 1-4 alkyl; Z represents a bond, CO, SO 2 , CR 10 R 7 (CH 2 ) n , (CH 2 ) n CR 10 R 7 , CR 10 R 7 (CH 2 ) n O, CR 10 R 7 (CH 2 ) n S, CR 10 R 7 (CH 2 ) n CO, COCR 10 R 7 (CH 2 ) n or SO 2 CR 10 R 7 (CH 2 ) n ; R 6 represents aryl, heteroaryl or aryl-C 2-6 alkenyl-; R 7 represents hydrogen, C 1-4 alkyl, CONR 8 R 9 or COOC 1-6 alkyl;a and b represent 1 or 2, such that a+b represents 2 or 3;G represents -S-, -SO 2 -, -SO 2 NR 21 , -NR 21 SO 2 or -NR 21 -; n represents an integer from 0 to 4; J 1 independently represents a moiety of formula (K): wherein X 1 represents oxygen, NR 11 or sulphur, X 2 represents CH 2 , oxygen, NR 12 or sulphur, m 1 represents an integer from 1 to 3, m 2 represents an integer from 1 to 3, provided that m 1 +m 2 is in the range from 3 to 5, also provided that when both X 1 and X 2 represent oxygen, NR 11 , NR 12 or sulphur, m 1 and m 2 must both not equal less than 2, wherein K is optionally substituted by one or more (eg. 1 or 2) -Y 3 -aryl, -Y 3 -heteroaryl, -Y 3 -CO-aryl, -Y 3 -CO-heteroaryl, -C 1-6 alkyl, -Y 3 -COOC 1-6 alkyl, -Y 3 -COC 1-6 alkyl, -Y 3 -W, -Y 3 -CO-W, -Y 3 -NR 15 R 16 , -Y 3 -CONR 15 R 16 , hydroxy, oxo, -Y 3 -SO 2 NR 15 R 16 , -Y 3 -SO 2 C 1-6 alkyl, -Y 3 -SO 2 aryl, -Y 3 -SO 2 heteroaryl, -Y 3 -NR 13 C 1-6 alkyl, -Y 3 -NR 13 SO 2 C 1-6 alkyl, -Y 3 -NR 13 CONR 15 R 16 , -Y 3 -NR 13 COOR 14 or -Y 3 -OCONR 15 R 16 groups, and is optionally fused to a monocyclic aryl or heteroaryl ring;R 8 , R 9 , R 10 , R 11 , R 12 , R 13 and R 14 independently represent hydrogen or C 1-6 alkyl; R 15 and R 16 independently represent hydrogen or C 1-6 alkyl or R 15 and R 16 together with the nitrogen atom to which they are attached may form a morpholine, piperidine or pyrrolidine ring; R 17 , R 18 , R 19 , R 20 , R 19a , R 20a , and R 21 independently represent hydrogen or C 1-4 alkyl; R 22 and R 23 independently represent hydrogen, C 1-6 alkyl, C 3-8 cycloalkyl or C 3-8 cycloalkylC1-6alkyl; R 24 represents C 1-6 alkyl, C 3-8 cycloalkyl, aryl or heteroaryl; W represents a saturatedor unsaturated, non-aromatic 5-7 membered ring containing between 1 and 3 heteroatoms selected from nitrogen, oxygen or sulphur, optionally substituted with one or more C 1-6 alkyl, halogen or hydroxy groups; Y 1 and Y 3 independently represent a bond or a group of formula - (CH 2 ) p CR c R d (CH 2 ) q - wherein R c and R d independently represent hydrogen or C 1-4 alkyl or R c and R d may together with the carbon atom to which they are attached form a C 3-8 cycloalkyl group, and p and q independently represent an integer from 0 to 5 wherein p + q is an integer from 0 to 5; and salts and solvates thereof are CCR3 receptor antagonists and thus are indicated to be useful in therapy.

    MORPHOLINYLMETHYLUREAS CCR-3 RECEPTOR ANTAGONIST
    10.
    发明申请
    MORPHOLINYLMETHYLUREAS CCR-3 RECEPTOR ANTAGONIST 审中-公开
    吗啉酰吗啉CCR-3受体拮抗剂

    公开(公告)号：WO03099798A8

    公开(公告)日：2004-01-15

    申请号：PCT/EP0305597

    申请日：2003-05-26

    Applicant: GLAXO GROUP LTD ,  COOK CAROLINE MARY ,  ELDRED COLIN DAVID ,  HARRISON LEE ANDREW

    Inventor： COOK CAROLINE MARY ,  ELDRED COLIN DAVID ,  HARRISON LEE ANDREW

    IPC: A61P11/06 ,  C07D265/30 ,  C07D413/12 ,  A61K31/5375 ,  A61K31/5377

    CPC classification number: C07D265/30 ,  C07D413/12

    Abstract: Compounds of formula (I): wherein:R represents C3-8 cycloalkyl-Y -, aryl-Y -, heteroaryl-Y -, aryl- G-Y -, heteroaryl-G-Y -, C1-6 alkyl-G-Y -, J -Y -, R R N-Y -, R R N-CO-Y - or R -CONR -Y -; Q represents -(CR R )(CR R )t-, wherein t represents an integer from 0 to 3;R and R independently represent hydrogen or C1-6 alkyl;X represents ethylene or a group of formula CR R wherein R and R independently represent hydrogen or C1-4 alkyl or R and R may together with the carbon atom to which they are attached form a C3-8 cycloalkyl group; R and R independently represent hydrogen or C1-4 alkyl; Z represents a bond, CO, SO2, CR R (CH2)n, (CH2)nCR R , CR R (CH2)nO, CR R (CH2)nS, CR R (CH2)nCO, COCR R (CH2)n or SO2CR R (CH2)n; R represents aryl, heteroaryl or aryl-C2-6 alkenyl-; R represents hydrogen, C1-4 alkyl, CONR R or COOC1-6 alkyl;a and b represent 1 or 2, such that a+b represents 2 or 3;G represents -S-, -SO2-, -SO2NR , -NR SO2 or -NR -; n represents an integer from 0 to 4; J independently represents a moiety of formula (K): wherein X represents oxygen, NR or sulphur, X represents CH2, oxygen, NR or sulphur, m represents an integer from 1 to 3, m represents an integer from 1 to 3, provided that m +m is in the range from 3 to 5, also provided that when both X and X represent oxygen, NR , NR or sulphur, m and m must both not equal less than 2, wherein K is optionally substituted by one or more (eg. 1 or 2) -Y -aryl, -Y -heteroaryl, -Y -CO-aryl, -Y -CO-heteroaryl, -C1-6 alkyl, -Y -COOC1-6 alkyl, -Y -COC1-6 alkyl, -Y -W, -Y -CO-W, -Y -NR R , -Y -CONR R , hydroxy, oxo, -Y -SO2NR R , -Y -SO2C1-6 alkyl, -Y -SO2aryl, -Y -SO2heteroaryl, -Y -NR C1-6 alkyl, -Y -NR SO2C1-6 alkyl, -Y -NR CONR R , -Y -NR COOR or -Y -OCONR R groups, and is optionally fused to a monocyclic aryl or heteroaryl ring;R , R , R , R , R , R and R

    Abstract translation: 式（I）化合物：其中：R 1表示C 3-8环烷基-Y 1 - ，芳基-Y 1 - ，杂芳基-Y 1 - ，芳基-GY 1 - ，杂芳基 -GY 1 - ，C 1-6烷基-GY 1 - ，J 1 -Y 1 - ，R 22 R 23，NY 22 - ，R 22 R 23 > N-CO-Y 1 - 或R 24 -CONR 22 -Y 1 - ; Q表示 - （CR 19 R 20）（CR 19 R 20）t - ，其中t表示0至3的整数; R 2和R 3独立地表示氢或C 1 -6-烷基; X表示亚乙基或式CR e R f的基团，其中R e和R f独立地表示氢或C 1-4烷基或R e和R f可以在一起 与它们所连接的碳原子一起形成C 3-8环烷基; R 4和R 5独立地表示氢或C 1-4烷基; Z表示键，CO，SO 2，CR 10 R 7（CH 2）n，（CH 2）n CR 10 R 7，CR 10 R 7（CH 2）n O，CR 10 （CH 2）n C，CR 10 R 7（CH 2）n CO，COCR 10 R 7（CH 2）n或SO 2 CR 10 R 7（CH 2）n; R 6代表芳基，杂芳基或芳基-C 2-6烯基 - ; R 7表示氢，C 1-4烷基，CONR 8 R 9或COOC 1-6烷基; a和b表示1或2，使得a + b表示2或3; G表示-S-， -SO 2 - ，-SO 2 NR 21，-NR 21 SO 2或-NR 21 - ; n表示0〜4的整数， J 1独立地表示式（K）的部分：其中X 1表示氧，NR 11或硫，X 2表示CH 2，氧，NR 12或硫，m表示 1〜3的整数，m 2表示1〜3的整数，条件是m 1 + m 2在3〜5的范围内，条件是当X 1和X 2表示氧，NR 11，NR 12或硫，m 1和m 2都必须不小于2，其中K任选被一个或多个（例如1或2个）取代 ）-Y 3 - 芳基，-Y 3 - 杂芳基，-Y 3 -CO-芳基，-Y 3 -CO-杂芳基，-C 1-6烷基，-Y 3 -COOC 1 -6烷基，-Y 3 -COC 1-6烷基，-Y 3 -W，-Y 3 -CO-W，-Y 3 -NR 15 R 16，-Y -CONR 15，R 16，羟基，氧代，-Y 3 -SO 2 NR 15，-Y 3 -SO 2 C 1-6烷基，-Y 3 -SO 2芳基 ，-Y 3 -SO 2杂芳基，-Y 3 -NR 13 C 1-6烷基，-Y 3 -NR 13 SO 2 C 1-6烷基，-Y 3 -NR 13 CONR R 15，-Y 3 -NR 13 COOR 14或-Y 3 -CONR 15 R 16基团，并且任选地与单环芳基或杂芳基环稠合 R 8，R 9，R 10，R 11，R 12，R 13和R 10， 14

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