公开(公告)号：US20060094702A1

公开(公告)日：2006-05-04

申请号：US11304110

申请日：2005-12-15

申请人： Francis King ,  Laramie Gaster ,  Keith Mulholland

发明人： Francis King ,  Laramie Gaster ,  Keith Mulholland

IPC分类号： A61K31/554 ,  A61K31/553 ,  A61K31/5415 ,  A61K31/538 ,  A61K31/4745 ,  C07D417/02 ,  C07D413/02 ,  C07D455/02

CPC分类号： C07D401/06

摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof, and the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof: X—CO—CH2-Z wherein X is a monocyclic or polycyclic aromatic group, Z is of sub-formula (h), (j) or (k): wherein n1 is 1, 2, 3 or 4; n2 is 0, 1, 2, 3 or 4; n3is 2, 3, 4 or 5; q is 0, 1, 2 or 3; p is 0, 1 or 2; m is 0, 1 or 2; R5 is hydrogen, C1-2 alkyl, aralkyl or R5 is (CH2)z-R10 wherein z is 2 or 3 and R10 is selected from cyano, hydroxyl, C1-6 alkoxy, phenoxy, C(O)C1-6 alkyl, COC6H5, —CONR11R12, NR11COR12, SO2NR11R12 or NR11SO2R12 wherein R11 and R12 are hydrogen or C1-6 alkyl; or R5 is straight or branched chain alkylene of chain length 1-6 carbon atoms terminally substituted by aryl, 3 to 8 membered cycloalkyl, 3 to 8 membered heterocyclyl, 5 or 6 membered monocyclic heteroaryl or 9 or 10 membered fused bicyclic heteroaryl linked through carbon, C2-7 alkoxycarbonyl, or secondary or tertiary hydroxy substituted C1-6 alkyl; ; and R6, R7 and R8 are independently hydrogen or C1-6 alkyl; and R9 is hydrogen or C1-10alkyl; and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.

公开(公告)号：US20050239797A1

公开(公告)日：2005-10-27

申请号：US11151008

申请日：2005-06-13

申请人： Laramie Gaster ,  Thomas Heightman ,  Jean-Pierre Pilleux

发明人： Laramie Gaster ,  Thomas Heightman ,  Jean-Pierre Pilleux

IPC分类号： A61K31/437 ,  A61K31/47 ,  A61K31/4745 ,  A61K31/496 ,  A61K31/505 ,  A61K31/517 ,  A61K31/538 ,  A61P25/24 ,  A61P43/00 ,  C07D217/22 ,  C07D239/94 ,  C07D401/12 ,  C07D471/04 ,  C07D471/14

CPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/47 ,  A61K31/505 ,  C07D217/22 ,  C07D239/94

摘要： The invention relates to novel isoquinoline and quinazoline derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders.

摘要翻译： 本发明涉及具有药理活性的新型异喹啉和喹唑啉衍生物，其制备方法，含有它们的组合物及其在治疗各种病症中的用途。

公开(公告)号：US20050014938A1

公开(公告)日：2005-01-20

申请号：US10495414

申请日：2002-11-14

申请人： Laramie Gaster ,  John Harling ,  Jag Heer ,  Thomas Heightman ,  Andrew Payne

发明人： Laramie Gaster ,  John Harling ,  Jag Heer ,  Thomas Heightman ,  Andrew Payne

IPC分类号： A61K31/4192 ,  A61K31/4196 ,  A61K31/433 ,  A61K31/538 ,  A61P1/00 ,  A61P1/04 ,  A61P1/16 ,  A61P3/12 ,  A61P9/10 ,  A61P11/00 ,  A61P13/12 ,  A61P19/00 ,  A61P19/02 ,  A61P19/10 ,  A61P25/00 ,  A61P25/28 ,  A61P27/02 ,  A61P43/00 ,  C07D249/06 ,  C07D265/36 ,  C07D285/14 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04 ,  C07D417/02 ,  C07D413/02 ,  C07

CPC分类号： C07D285/14 ,  C07D249/06 ,  C07D265/36 ,  C07D471/04

摘要： Phenyl substituted triazoles of formula (I) wherein R1 is naphthyl or phenyl optionally substituted with one or more substituents selected from halo, —O—C1-6alkyl, —S—C1-6alkyl, C1-6alkyl, C1-6haloalkyl, —O—(CH2)n-Ph, —S—(CH2)n-Ph, cyano, phenyl, and CO2R, wherein R is hydrogen or C1-6alkyl, and n is 0, 1, 2 or 3; or R1 is phenyl or pyridyl fused with an aromatic or non-aromatic cyclic ring of 5-7 members wherein said cyclic ring optionally contains up to three heteroatoms, independently selected from N, O and S, and N may be further optionally substituted by C1-6 alkyl, and wherein the cyclic ring may be optionally substituted by ═O; R2 and R3 are independently selected from H, C1-6alkyl, C1-6alkoxy, phenyl, NH(CH2)n-Ph, NH—C1-6alkyl, halo, alkoxy, CN, NO2, CONHR and SO2NHR; two of X1, X2 and X3 are N and the other is NR4 wherein R4 is hydrogen, C1-6alkyl, C3-7cycloalkyl, —(CH2)p—CN, —(CH2)p—CO2H, —(CH2)p—CONHR5R6, —(CH2)pCOR5, —(CH2)q(CR7)2, —(CH2)pOR5, (CH2)qCH═CH—CN, —(CH2)q—CH═CH—CO2H, —(CH2)p—CH═CH—CONHR5R6, —(CH2)pNHCOR8 or —(CH2)pNR9R10; R5 and R6 are independently hydrogen or C1-6alkyl; R7 is C1-6alkyl; R8 is C1-7alkyl, or optionally substituted aryl, heteroaryl, arylC1-6alkyl or heteroaryl C1-6alkyl; R9 and R10 are independently selected from hydrogen, C1-6alkyl, aryl and arylC1-6alkyl; p is 0-4; and q is 1-4 and salts and solvates thereof, are disclosed, as are methods for their preparation, pharmaceutical compositions containing them and their use in medicine.

摘要翻译： 式（I）的苯基取代的三唑，其中R 1是萘基或任选被一个或多个选自卤素，-OC 1-6烷基，-S-C 1-6烷基，C 1-6烷基，C 1-6卤代烷基，-O- （CH 2）n-Ph，-S-（CH 2）n-Ph，氰基，苯基和CO 2 R，其中R是氢或C 1-6烷基，n是0,1,2或3; 或R 1是与5-7个成员的芳族或非芳族环的稠合的苯基或吡啶基，其中所述环任选地含有至多三个独立地选自N，O和S的杂原子，并且N可以进一步任选地被C1 -6烷基，并且其中所述环状环可以任选地被= O取代; R2和R3独立地选自H，C1-6烷基，C1-6烷氧基，苯基，NH（CH2）n-Ph，NH-C1-6烷基，卤素，烷氧基，CN，NO2，CONHR和SO2NHR; X1，X2和X3中的两个是N，另一个是NR4，其中R4是氢，C1-6烷基，C3-7环烷基， - （CH2）p-CN， - （CH2）p-CO2H， - （CH2）p-CONHR5R6 ， - （CH2）pCOR5， - （CH2）q（CR7）2， - （CH2）pOR5，（CH2）qCH = CH-CN， - （CH2）q-CH = CH-CO2H， - （CH2） CH = CH-CONHR5R6， - （CH2）pNHCOR8或 - （CH2）p