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    Non-peptide GnRH antagonists
    2.
    发明申请
    Non-peptide GnRH antagonists 审中-公开

    公开(公告)号：US20080255109A1

    公开(公告)日：2008-10-16

    申请号：US12149150

    申请日：2008-04-28

    申请人： Michael Bryan Roe ,  Andrzej Roman Batt ,  David Michael Evans ,  Gary Robert William Pitt ,  David Philip Rooker

    发明人： Michael Bryan Roe ,  Andrzej Roman Batt ,  David Michael Evans ,  Gary Robert William Pitt ,  David Philip Rooker

    IPC分类号： A61K31/5365 ,  C07D215/14 ,  C07D413/02 ,  C07D413/06 ,  C07D265/36 ,  A61K31/4985 ,  C07D241/36 ,  A61K31/4709 ,  A61K31/5355 ,  A61P15/08 ,  A61P35/00

    CPC分类号： C07D413/14 ,  C07D217/02 ,  C07D241/44 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06

    摘要： Compounds according to general formula 1, wherein A1-A3 are selected from A5 and A6 where A5 is either ═CR13— or ═N— and A6 is —NR14—, —O— or —S—; A4 is either a covalent bond or A5, provided that when A4 is a covalent bond one of A1-A3 must be A6 and the other two must be A5 and when A4 is A5 then all of A1-A3 must be A5; R1 is selected from H, NHY′ and COY2, in which case R2 is H, or R1 and R2 may both be methyl or together represent ═O; R3, R4 and R5 are each independently selected from H and lower alkyl groups; R6, R7, R8, R9, R10, R11 and R12 are each independently selected from H, lower alkyl groups, NH2, halogens (F, Cl and Br) O-alkyl, CH2NM2 and CF3; R13 is selected from H, F, Cl, Br, NO2, NH2, OH, Me, Et, OMe, NMe2 and CF3; R14 is selected from H, methyl and ethyl; W is selected from ═CH— and ═N—; X is selected from CH2, O, S, SO2, NH and N-lower alkyl; Y1 is selected from CO-lower alkyl, CO(CH2)bY3, CO(CH2)bCOY3 and CO(CH2)bNHCOY3, where b is 1-3; Y2 is selected from OR15, NR16R17 and NH(CH2)cCOY3, where c is 1-3; Y3 is selected from OR15 and NR16R17; R15 is selected from H, lower alkyl and (CH2)aR16, where a is 0-4; R16 and R17 are each independently selected from H, lower alkyl and (CH2)aR16 or together are —(CH2)2-Z-(CH2)2—; R18 is OH, a phenyl group or an aromatic heterocycle selected from pyridyl, pyrimidinyl, pyrazinyl, furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, triazolyl, oxadiazolyl and thiadiazolyl, each of which may optionally have a lower alkyl group substituent; and Z is selected from O, CH2, S, SO2, NH and N-lower alkyl, are new. They are useful in the treatment of breast and prostate cancer, endometriosis and benign prostate hyperplasia, in the regulation of fertility, and in in vitro fertilisation.

    Non-peptide GnRH antagonists
    5.
    发明授权
    Non-peptide GnRH antagonists 失效

    公开(公告)号：US07365065B2

    公开(公告)日：2008-04-29

    申请号：US10507595

    申请日：2003-03-12

    申请人： Michael Bryan Roe ,  Andrzej Roman Batt ,  David Michael Evans ,  Gary Robert William Pitt ,  David Philip Rooker

    发明人： Michael Bryan Roe ,  Andrzej Roman Batt ,  David Michael Evans ,  Gary Robert William Pitt ,  David Philip Rooker

    IPC分类号： C07D215/08 ,  C07D413/06 ,  C07D413/14 ,  A61K31/538

    CPC分类号： C07D413/14 ,  C07D217/02 ,  C07D241/44 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06

    摘要： Compounds according to general formula 1, wherein A1-A3 are selected from A5 and A6 where A5 is either ═CR13— or ═N— and A6 is —NR14—, —O— or —S—; A4 is either a covalent bond or A5, provided that when A4 is a covalent bond one of A1-A3 must be A6 and the other two must be A5 and when A4 is A5 then all of A1-A3 must be A5; R1 is selected from H, NHY′ and COY2, in which case R2 is H, or R1 and R2 may both be methyl or together represent ═O; R3, R4 and R5 are each independently selected from H and lower alkyl groups; R6, R7, R8, R9, R10, R11 and R12 are each independently selected from H, lower alkyl groups, NH2, halogens (F, Cl and Br) O-alkyl, CH2NM2 and CF3; R13 is selected from H, F, Cl Br, NO2, NH2, OH, Me, Et, OMe, NMe2 and CF3; R14 is selected from H, methyl and ethyl; W is selected from ═CH— and ═N—; X is selected from CH2, O, S, SO2, NH and N lower alkyl; Y1 is selected from CO-lower alkyl, CO(CH2)bY3, CO(CH2)bCOY3 and CO(CH)NHCOY3, where b is 1-3; Y2 is selected from OR15, NR16R17 and NH(CH2)CCOY3, where c is 1-3; Y3 is selected from OR15 and NR16R17; R15 is selected from H, lower alkyl and (CH2)aR16, where a is 0-4; R16 and R17 are each independently selected from H, lower alkyl and (CH2)aR16 or together are —(CH2)2-Z-(CH2)2—; R18 is OH a phenyl group or an aromatic heterocycle selected from pyridyl, pyrimidinyl, pyrazinyl, furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, triazolyl, oxadiazolyl and thiadiazolyl, each of which may optionally have a lower alkyl group substituent; and Z is selected from O, CH2, S, SO2, NH and N-lower alkyl, are new. They are useful in the treatment of breast and prostate cancer, endometriosis and benign prostate hyperplasia, in the regulation of fertility, and in in vitro fertilisation.