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    Phenyl derivative useful as inhibitors of IMPDH enzyme
    59.
    发明专利
    Phenyl derivative useful as inhibitors of IMPDH enzyme 未知

    公开(公告)号：NZ514540A

    公开(公告)日：2003-11-28

    申请号：NZ51454000

    申请日：2000-03-17

    Applicant: VERTEX PHARMA

    Inventor： STAMOS DEAN ,  TRUDEAU MARTIN ,  BETHIEL SCOTT ,  BADIA MICHAEL ,  SAUNDERS JEFFREY

    IPC: C07D307/20 ,  A61K31/27 ,  A61K31/275 ,  A61K31/341 ,  A61K31/421 ,  A61K31/422 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/00 ,  A61P1/18 ,  A61P9/10 ,  A61P11/06 ,  A61P19/02 ,  A61P29/00 ,  A61P31/12 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07C275/40 ,  C07C275/42 ,  C07D263/32 ,  C07D413/12 ,  C07D417/12 ,  C07F9/653 ,  C07C275/34

    Abstract: A phenyl derivative has the formula (A) wherein: each of R1 and R2 is independently hydrogen, -CF3, alkyl, alkenyl, alkynyl, alkyl-R7, alkenyl-R7, alkynyl-R7 or -R7, provided at least one of R1 or R2 is alkyl-R7, alkenyl-R7, alkynyl-R7 or -R7; wherein up to 4 hydrogen atoms in any of the alkyl, alkenyl or alkynyl are optionally replaced by R3, or one or both of R1 or R2 are optionally esterified to form a prodrug or R1 and R2 are alternatively taken together to form tetrahydrofuranyl, when R9 is hydrogen, (R)-methyl, (R)- ethyl or (R)-hydroxymethyl, one hydrogen atom in the tetrahydrofuran is replaced by -OR6 or -R7, and when R9 is (S)- methyl, (S)-ethyl or (S)-hydroxymethyl, one hydrogen atom in the tetrahydrofuran is optionally replaced by -OR6 or -R7 or when R9 is hydrogen, (R)-methyl, (R)-ethyl or (R)- hydroxymethyl and each of R1 and R2 are independently hydrogen, unsubstituted alkyl, or unsubstituted alkenyl or alkynyl, then the portion of the compound represented by - CH(R1)R2 is a C5-12 alkyl, alkenyl or alkynyl; each R3 is independently halo, CN, -OR4, or -N(R5)2; R4, R5, R6 and R8 are as defined in the specification, each R7 is a monocyclic or bicyclic ring system wherein each ring system comprises 3 to 7 ring atoms independently selected from C, N, O and S, no more than 4 ring atoms are selected from N, O or S, any CH2 is optionally replaced with C (O) and any S is optionally replaced with S(O) or S(O)2; R9 is hydrogen, (R)-methyl, (S)-methyl, (R)-ethyl, (S)- ethyl, (R)-hydroxymethyl or (S)-hydroxymethyl; R10 is -C=N or 5-oxazolyl, and R11 is halo, -O-alkyl, or -O-alkenyl or -O-alkynyl. The compounds are useful for treating or preventing an inosine-5'-monophosphate dehydrogenase disease or condition.

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