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13 条记录 (耗时 0.042 秒)

    Non-peptide GnRH antagonists
    1.
    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
    2.
    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.

    Inhibitors of dipeptidyl peptidase IV
    3.
    发明授权
    Inhibitors of dipeptidyl peptidase IV 失效
    二肽基肽酶抑制剂

    公开(公告)号：US07189728B2

    公开(公告)日：2007-03-13

    申请号：US10221129

    申请日：2001-04-26

    申请人： David Michael Evans ,  Gary Robert William Pitt

    发明人： David Michael Evans ,  Gary Robert William Pitt

    IPC分类号： A61K31/4905 ,  A61K31/44 ,  A61K31/40 ,  A01N43/40 ,  A01N43/36

    CPC分类号： C07D213/82 ,  C07D207/16 ,  C07D241/24 ,  C07D277/04 ,  C07D295/185 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12

    摘要： Compounds according to general formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is O, S or CH2, X3 is NR5 or a carbonyl or thiocarbonyl group and R4 is R6R7N, R8(CH2)qOC(═O), R8(CH2)qOC(═S), R6R7NC(═O), R6R7NC(═S); R8(CH2)qC(═O), R8(CH2)qC(═S) or R8(CH2)qSO2, m is 1–3 and n is 0–4 are new. The compounds of the invention are inhibitors of dipeptidyl peptidase IV. Pharmaceutical compositions of the compounds of the invention, or pharmaceutically acceptable salts thereof, are useful in the treatment of, inter alia, type 2 diabetes

    摘要翻译： 根据通式（1）的化合物，其中R 1是H或CN，X 1是S，O，SO 2或CH 3， S 2，X 2，O，S或CH 2，X 3是NR 5 O >或羰基或硫代羰基，R 4是R 6 R 7，R 8（CH 3） （-O），R 8（CH 2）2）C（O），R 8（CH 2） OC（-S），R 6，R 7，NC（-O），R 6 R 7 NC（ -S）; （CH 2）2 C（-O），R 8（CH 2） C（-S）或R 8（CH 2 CH 2）q SO 2， 2，m是1-3，n是0-4是新的。 本发明的化合物是二肽基肽酶IV的抑制剂。 本发明化合物或其药学上可接受的盐的药物组合物可用于治疗尤其是2型糖尿病

    Selective dipeptide inhibitors of kallikrein
    8.
    发明授权
    Selective dipeptide inhibitors of kallikrein 有权
    激肽释放酶的选择性二肽抑制剂

    公开(公告)号：US07649000B2

    公开(公告)日：2010-01-19

    申请号：US10506535

    申请日：2003-03-04

    申请人： David Michael Evans

    发明人： David Michael Evans

    IPC分类号： A61K31/4468 ,  C07D211/56

    CPC分类号： C07K5/0606 ,  A61K38/00 ,  C07K5/06034 ,  C07K5/06078

    摘要： Compounds of general formula 1, or a pharmaceutically acceptable salt thereof, wherein R1 is selected from H, lower alkyl, R4—CO, R4—O2CCH2, R5—OCO and R5—SO2; R2 is selected from lower alkyl, cycloalkyl optionally substituted with an alkyl or alkyloxy group, (C5-C12)cycloalkylalkyl optionally substituted with an alkyl or alkyloxy group, aralkyl optionally substituted with up to three groups chosen from F, Cl, Br, I, OH, lower alkyl, O-(lower alkyl), O-benzyl, NH2, NO2, NH-acyl, CN and CF3, and aralkyloxymethyl optionally substituted with up to three groups chosen from F, Cl, Br, OH, lower alkyl and O-(lower alkyl); or R1 and R2 together are an o-xylylene group optionally substituted on the aromatic ring with a group selected from F, Cl, Br, OH, lower alkyl and O-(lower alkyl); R3 is selected from H, OH and O-lower alkyl; R4 is selected from H, lower alkyl and phenyl; and R5 is selected from lower alkyl, phenyl and benzyl. The compounds are useful as pharmaceutical compositions.

    摘要翻译： 通式1的化合物或其药学上可接受的盐，其中R1选自H，低级烷基，R4-CO，R4-O2CCH2，R5-OCO和R5-SO2; R 2选自低级烷基，任选被烷基或烷氧基取代的环烷基，任选被烷基或烷氧基取代的（C 5 -C 12）环烷基烷基，任选被至多三个选自F，Cl，Br，I， OH，低级烷基，O-（低级烷基），O-苄基，NH 2，NO 2，NH-酰基，CN和CF 3，以及任选被至多三个选自F，Cl，Br，OH，低级烷基的基团取代的芳烷氧基甲基， O-（低级烷基）; 或R 1和R 2一起是在芳环上任选被选自F，Cl，Br，OH，低级烷基和O-（低级烷基）的基团取代的邻苯二甲酰基。 R3选自H，OH和O-低级烷基; R4选自H，低级烷基和苯基; 并且R 5选自低级烷基，苯基和苄基。 这些化合物可用作药物组合物。

    Antidiabetic agents
    10.
    发明授权
    Antidiabetic agents 失效

    公开(公告)号：US07169806B2

    公开(公告)日：2007-01-30

    申请号：US11106594

    申请日：2005-04-15

    申请人： David Michael Evans

    发明人： David Michael Evans

    IPC分类号： A61K31/40 ,  C07D207/04

    CPC分类号： C07D401/12 ,  C07D207/16

    摘要： Compounds which are 1-(2′-aminoacyl)-2-cyanopyrrolidine derivatives according to general formula (1) are DP-IV inhibitors for treatment of impaired glucose tolerance or type 2 diabetes; wherein A is selected from groups (2, 3 and 4); X is selected from aminoacyl groups corresponding to the natural amino acids, acyl groups R3CO, groups R4COOC(R5)(R6)OCO, methoxycarbonyl, ethoxycarbonyl and benzyloxycarbonyl; R1 is selected from H, C1–C6alkyl residues, (CH2)aNHW1, (CH2)bCOW2, (CH2)cOW3, CH(Me)OW4, (CH2)d—C6H4—W5 and (CH2)eSW6, where a is 2–5, b is 1–4, c is 1–2, d is 1–2, e is 1–3, W1 is COW6, CO2W6 or SO2W6, W2 is OH, NH2, OW6 or NHW6, W3 is H or W6, W4 is H or W6, W5 is H, OH or OMe, and W6 is C1–C6 alkyl, optionally substituted phenyl, optionally substituted heteroaryl or benzyl and R2 is selected from H and (CH2)n—C5H3N—Y, where n is 2–4 and Y is H, F, Cl, NO2 or CN, or R1 and R2 together are —(CH2)p— where p is 3 or 4; R3 is selected from H, C1–C6 alkyl and phenyl; R4 is selected from H, C1–C6 alkyl, benzyl and optionally substitued phenyl; R5 and R6 are each independently selected from H and C1–C6 alkyl or together are —(CH2)m—, where m is 4–6; R7 is selected from pyridyl and optionally substituted phenyl; R8 is selected from H and C1–C3 alkyl; and R9 is selected from H, C1–C6 alkyl, C1–C6 alkoxy and phenyl.