公开(公告)号：US5550254A

公开(公告)日：1996-08-27

申请号：US483700

申请日：1995-06-07

申请人： R. Richard L. Hamer ,  Grover C. Helsley ,  Edward J. Glamkowski ,  Yulin Chiang

发明人： R. Richard L. Hamer ,  Grover C. Helsley ,  Edward J. Glamkowski ,  Yulin Chiang

IPC分类号： A61K31/40 ,  A61K31/44 ,  A61K31/495 ,  A61K31/535 ,  A61P25/04 ,  A61P25/28 ,  C07D487/04

CPC分类号： C07D487/04

摘要： There are described compounds of the formula ##STR1## where (a) X is O or S;(b) R is H, loweralkyl, ##STR2## where Y is O or S; R.sub.2 is alkyl, cycloalkyl, bicycloalkyl, cycloalkenyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl, R.sub.3 is H or alkyl, or the group --NR.sub.2 R.sub.3 taken as a whole is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-thiomorpholinyl, 1-piperazinyl, 4-methyl-1-piperazinyl or 2-(2,6-dichlorophenylimino)-1-imidazolidinyl) and R.sub.4 is hydrogen, loweralkyl, arylloweralkyl, diarylloweralkyl, aryl or heteroaryl,(c) m is 1 or 2;(d) each Z is independently H, loweralkyl, halogen, nitro, --NH.sub.2, loweralkylcarbonylamino, arylcarbonylamino, loweralkoxycarbonylamino or loweralkylamino, and(e) R.sub.1 is H, loweralkyl, arylloweralkyl, heteroarylloweralkyl, cycloalkylmethyl or loweralkenylmethyl,with the proviso that when X is O, m is 1, Z is H and R.sub.1 is methyl, R is not --CONHCH.sub.3, --CONHC.sub.6 H.sub.5, hydrogen, methyl or ethyl, and that when X is O, m is 1 and Z and R.sub.1 are both hydrogen, R is not hydrogen or methyl, and pharmaceutically acceptable acid addition salts thereof which are useful as memory-enhancing and analgesic agents.

摘要翻译： 描述了式（IMAGE）的化合物，其中（a）X是O或S; （b）R是H，低级烷基，其中Y是O或S; R2是烷基，环烷基，二环烷基，环烯基，芳基，芳基低级烷基，杂芳基或杂芳基低级烷基，R3是H或烷基，或作为整体的基团-NR2R3是1-吡咯烷基，1-哌啶基，4-吗啉基，4-硫代吗啉基， 1-哌嗪基，4-甲基-1-哌嗪基或2-（2,6-二氯苯基亚氨基）-1-咪唑烷基），R4是氢，低级烷基，芳基低级烷基，二芳基低级烷基，芳基或杂芳基，（c）m是1或2; （d）每个Z独立地是H，低级烷基，卤素，硝基，-NH 2，低级烷基羰基氨基，芳基羰基氨基，低级烷氧基羰基氨基或低级烷基氨基，和（e）R 1是H，低级烷基，芳基低级烷基，杂芳基低级烷基，环烷基甲基或低级烯基甲基，条件是当X 是O，m是1，Z是H，R1是甲基，R不是-CONHCH3，-CONHC6H5，氢，甲基或乙基，当X是O时，m是1，Z和R1都是氢，R是 不是氢或甲基，以及其药学上可接受的酸加成盐，其可用作记忆增强剂和止痛剂。

公开(公告)号：US4791107A

公开(公告)日：1988-12-13

申请号：US49894

申请日：1987-05-15

申请人： R. Richard L. Hamer ,  Grover C. Helsley ,  Edward J. Glamkowski ,  Yulin Chiang

发明人： R. Richard L. Hamer ,  Grover C. Helsley ,  Edward J. Glamkowski ,  Yulin Chiang

IPC分类号： A61K31/40 ,  A61K31/44 ,  A61K31/495 ,  A61K31/535 ,  A61P25/04 ,  A61P25/28 ,  C07D487/04

CPC分类号： C07D487/04

摘要： There are described compounds of the formula ##STR1## where (a) X is O or S;(b) R is H, loweralkyl, ##STR2## where Y is O or S; R.sub.2 is alkyl, cycloalkyl, bicycloalkyl, cycloalkenyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl, R.sub.3 is H or alkyl, or the group --NR.sub.2 R.sub.3 taken as a whole is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-thiomorpholinyl, 1-piperazinyl, 4-methyl-1-piperazinyl or 2-(2,6-dichlorophenylimino)-1-imidazolidinyl) and R.sub.4 is hydrogen, loweralkyl, arylloweralkyl, diarylloweralkyl, aryl or heteroaryl,(c) m is 1 or 2;(d) each Z is independently H, loweralkyl, halogen, nitro, --NH.sub.2, loweralkylcarbonylamino, arylcarbonylamino, loweralkoxycarbonylamino or loweralkylamino, and(e) R.sub.1 is H, loweralkyl, arylloweralkyl, heteroarylloweralkyl, cycloalkylmethyl or loweralkenylmethyl, with the proviso that when X is O, m is 1, Z is H and R.sub.1 is methyl, R is not --CONHCH.sub.3, --CONHC.sub.6 H.sub.5, hydrogen, methyl or ethyl, and that when X is O, m is 1 and Z and R.sub.1 are both hydrogen, R is not hydrogen or methyl, and pharmaceutically acceptable acid addition salts thereof which are useful as memory-enhancing and analgesic agents.

摘要翻译： 描述了式（IMAGE）的化合物，其中（a）X是O或S; （b）R是H，低级烷基，其中Y是O或S; R2是烷基，环烷基，二环烷基，环烯基，芳基，芳基低级烷基，杂芳基或杂芳基低级烷基，R3是H或烷基，或作为整体的基团-NR2R3是1-吡咯烷基，1-哌啶基，4-吗啉基，4-硫代吗啉基， 1-哌嗪基，4-甲基-1-哌嗪基或2-（2,6-二氯苯基亚氨基）-1-咪唑烷基），R4是氢，低级烷基，芳基低级烷基，二芳基低级烷基，芳基或杂芳基，（c）m是1或2; （d）每个Z独立地是H，低级烷基，卤素，硝基，-NH 2，低级烷基羰基氨基，芳基羰基氨基，低级烷氧基羰基氨基或低级烷基氨基，和（e）R 1是H，低级烷基，芳基低级烷基，杂芳基低级烷基，环烷基甲基或低级烯基甲基，条件是当X 是O，m是1，Z是H，R1是甲基，R不是-CONHCH3，-CONHC6H5，氢，甲基或乙基，当X是O时，m是1，Z和R1都是氢，R是 不是氢或甲基，以及其药学上可接受的酸加成盐，其可用作记忆增强剂和止痛剂。

公开(公告)号：US5621114A

公开(公告)日：1997-04-15

申请号：US479197

申请日：1995-06-07

申请人： Richard L. Hamer ,  Grover C. Helsley ,  Edward J. Glamkowski ,  Yulin Chiang

发明人： Richard L. Hamer ,  Grover C. Helsley ,  Edward J. Glamkowski ,  Yulin Chiang

IPC分类号： A61K31/40 ,  A61K31/44 ,  A61K31/495 ,  A61K31/535 ,  A61P25/04 ,  A61P25/28 ,  C07D487/04

CPC分类号： C07D487/04

摘要： There are described compounds of the formula ##STR1## where (a) X is O or S;(b) R is H, loweralkyl, ##STR2## where Y is O or S; R.sub.2 is alkyl, cycloalkyl, bicycloalkyl, cycloalkenyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl, R.sub.3 is H or alkyl, or the group --NR.sub.2 R.sub.3 taken as a whole is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-thiomorpholinyl, 1-piperazinyl, 4-methyl-1-piperazinyl or 2-(2,6-dichlorophenylimino)-1-imidazolidinyl) and R.sub.4 is hydrogen, loweralkyl, arylloweralkyl, diarylloweralkyl, aryl or heteroaryl,(c) m is 1 or 2;(d) each Z is independently H, loweralkyl, halogen, nitro, --NH.sub.2, loweralkylcarbonylamino, arylcarbonylamino, loweralkoxycarbonylamino or loweralkylamino, and(e) R.sub.1 is H, loweralkyl, arylloweralkyl, heteroarylloweralkyl, cycloalkylmethyl or loweralkenylmethyl, with the proviso that when X is O, m is 1, Z is H and R.sub.1 is methyl, R is not --CONHCH.sub.3, --CONHC.sub.6 H.sub.5, hydrogen, methyl or ethyl, and that when X is O, m is 1 and Z and R.sub.1 are both hydrogen, R is not hydrogen or methyl, and pharmaceutically acceptable acid addition salts thereof which are useful as memory-enhancing and analgesic agents.

摘要翻译： 描述了式（IMAGE）的化合物，其中（a）X是O或S; （b）R是H，低级烷基，其中Y是O或S; R2是烷基，环烷基，二环烷基，环烯基，芳基，芳基低级烷基，杂芳基或杂芳基低级烷基，R3是H或烷基，或作为整体的基团-NR2R3是1-吡咯烷基，1-哌啶基，4-吗啉基，4-硫代吗啉基， 1-哌嗪基，4-甲基-1-哌嗪基或2-（2,6-二氯苯基亚氨基）-1-咪唑烷基），R4是氢，低级烷基，芳基低级烷基，二芳基低级烷基，芳基或杂芳基，（c）m是1或2; （d）每个Z独立地是H，低级烷基，卤素，硝基，-NH 2，低级烷基羰基氨基，芳基羰基氨基，低级烷氧基羰基氨基或低级烷基氨基，和（e）R 1是H，低级烷基，芳基低级烷基，杂芳基低级烷基，环烷基甲基或低级烯基甲基，条件是当X 是O，m是1，Z是H，R1是甲基，R不是-CONHCH3，-CONHC6H5，氢，甲基或乙基，当X是O时，m是1，Z和R1都是氢，R是 不是氢或甲基，以及其药学上可接受的酸加成盐，其可用作记忆增强剂和止痛剂。

公开(公告)号：US5547977A

公开(公告)日：1996-08-20

申请号：US962079

申请日：1992-10-16

申请人： Richard L. Hamer ,  Grover C. Helsley ,  Edward J. Glamkowski ,  Yulin Chiang

发明人： Richard L. Hamer ,  Grover C. Helsley ,  Edward J. Glamkowski ,  Yulin Chiang

IPC分类号： A61K31/40 ,  A61K31/44 ,  A61K31/495 ,  A61K31/535 ,  A61P25/04 ,  A61P25/28 ,  C07D487/04

CPC分类号： C07D487/04

摘要： There are described compounds of the formula ##STR1## where (a) X is O or S;(b) R is H, loweralkyl, ##STR2## where Y is O or S; R.sub.2 is alkyl, cycloalkyl, bicycloalkyl, cycloalkenyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl, R.sub.3 is H or alkyl, or the group --NR.sub.2 R.sub.3 taken as a whole is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-thiomorpholinyl, 1-piperazinyl, 4-methyl-1-piperazinyl or 2-(2,6-dichlorophenylimino)-1-imidazolidinyl) and R.sub.4 is hydrogen, loweralkyl, arylloweralkyl, diarylloweralkyl, aryl or heteroaryl,(c) m is 1 or 2;(d) each Z is independently H, loweralkyl, halogen, nitro, --NH.sub.2, loweralkylcarbonylamino, arylcarbonylamino, loweralkoxycarbonylamino or loweralkylamino, and(e) R.sub.1 is H, loweralkyl, arylloweralkyl, heteroarylloweralkyl, cycloalkylmethyl or loweralkenylmethyl, with the proviso that when X is O, m is 1, Z is H and R.sub.1 is methyl, R is not --CONHCH.sub.3, --CONHC.sub.6 H.sub.5, hydrogen, methyl or ethyl, and that when X is O, m is 1 and Z and R.sub.1 are both hydrogen, R is not hydrogen or methyl, and pharmaceutically acceptable acid addition salts thereof which are useful as memory-enhancing and analgesic agents.

摘要翻译： 描述了式（IMAGE）的化合物，其中（a）X是O或S; （b）R是H，低级烷基，其中Y是O或S; R2是烷基，环烷基，二环烷基，环烯基，芳基，芳基低级烷基，杂芳基或杂芳基低级烷基，R3是H或烷基，或作为整体的基团-NR2R3是1-吡咯烷基，1-哌啶基，4-吗啉基，4-硫代吗啉基， 1-哌嗪基，4-甲基-1-哌嗪基或2-（2,6-二氯苯基亚氨基）-1-咪唑烷基），R4是氢，低级烷基，芳基低级烷基，二芳基低级烷基，芳基或杂芳基，（c）m是1或2; （d）每个Z独立地是H，低级烷基，卤素，硝基，-NH 2，低级烷基羰基氨基，芳基羰基氨基，低级烷氧基羰基氨基或低级烷基氨基，和（e）R 1是H，低级烷基，芳基低级烷基，杂芳基低级烷基，环烷基甲基或低级烯基甲基，条件是当X 是O，m是1，Z是H，R1是甲基，R不是-CONHCH3，-CONHC6H5，氢，甲基或乙基，当X是O时，m是1，Z和R1都是氢，R是 不是氢或甲基，以及其药学上可接受的酸加成盐，其可用作记忆增强剂和止痛剂。

公开(公告)号：US5663190A

公开(公告)日：1997-09-02

申请号：US962080

申请日：1992-10-16

申请人： Richard L. Hamer ,  Grover C. Helsley ,  Edward J. Glamkowski ,  Yulin Chiang

发明人： Richard L. Hamer ,  Grover C. Helsley ,  Edward J. Glamkowski ,  Yulin Chiang

IPC分类号： A61K31/40 ,  A61K31/44 ,  A61K31/495 ,  A61K31/535 ,  A61P25/04 ,  A61P25/28 ,  C07D487/04 ,  A61K31/405 ,  C07D487/12

CPC分类号： C07D487/04

摘要： There are described compounds of the formula ##STR1## where (a) X is O or S;(b) R is H, loweralkyl, ##STR2## where Y is O or S; R.sub.2 is alkyl, cycloalkyl, bicycloalkyl, cycloalkenyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl, R.sub.3 is H or alkyl, or the group --NR.sub.2 R.sub.3 taken as a whole is 1-pyrrolidinyl, 1-piperldinyl, 4-morpholinyl, 4-thiomorpholinyl, 1-piperazinyl, 4-methyl-1-piperazinyl or 2-(2,6-dichlorophenylimino)-1-imidazolidinyl) and R.sub.4 is hydrogen, loweralkyl, arylloweralkyl, diarylloweralkyl, aryl or heteroaryl,(c) m is 1 or 2;(d) each Z is independently H, loweralkyl, halogen, nitro, --NH.sub.2, loweralkylcarbonylamino, arylcarbonylamino, loweralkoxycarbonylamino or loweralkylamino, and(e) R.sub.1 is H, loweralkyl, arylloweralkyl, heteroarylloweralkyl, cycloalkylmethyl or loweralkenylmethyl,with the proviso that when X is O, m is 1, Z is H and R.sub.1 is methyl, R is not --CONHCH.sub.3, --CONHC.sub.6 H.sub.5, hydrogen, methyl or ethyl and that when X is O, m is 1 and Z and R.sub.1 are both hydrogen, R is not hydrogen or methyl, and pharmaceutically acceptable acid addition salts thereof which are useful as memory-enhancing and analgesic agents.

摘要翻译： 描述了式（IMAGE）的化合物，其中（a）X是O或S; （b）R是H，低级烷基，其中Y是O或S; R2是烷基，环烷基，二环烷基，环烯基，芳基，芳基低级烷基，杂芳基或杂芳基低级烷基，R3是H或烷基，或者作为整体的基团-NR2R3是1-吡咯烷基，1-哌嗪基，4-吗啉基，4-硫代吗啉基， 1-哌嗪基，4-甲基-1-哌嗪基或2-（2,6-二氯苯基亚氨基）-1-咪唑烷基），R4是氢，低级烷基，芳基低级烷基，二芳基低级烷基，芳基或杂芳基，（c）m是1或2; （d）每个Z独立地是H，低级烷基，卤素，硝基，-NH 2，低级烷基羰基氨基，芳基羰基氨基，低级烷氧基羰基氨基或低级烷基氨基，和（e）R 1是H，低级烷基，芳基低级烷基，杂芳基低级烷基，环烷基甲基或低级链烯基甲基，条件是当X 是O，m是1，Z是H，R1是甲基，R不是-CONHCH3，-CONHC6H5，氢，甲基或乙基，当X是O时，m是1，Z和R1都是氢，R不是 氢或甲基及其药学上可接受的酸加成盐，其可用作记忆增强剂和止痛剂。

公开(公告)号：US5639892A

公开(公告)日：1997-06-17

申请号：US466013

申请日：1995-06-06

申请人： R. Richard L. Hamer ,  Grover C. Helsley ,  Edward J. Glamkowski ,  Yulin Chiang

发明人： R. Richard L. Hamer ,  Grover C. Helsley ,  Edward J. Glamkowski ,  Yulin Chiang

IPC分类号： A61K31/40 ,  A61K31/44 ,  A61K31/495 ,  A61K31/535 ,  A61P25/04 ,  A61P25/28 ,  C07D487/04

CPC分类号： C07D487/04

摘要： There are described compounds of the formula ##STR1## where X is O or S;(b) R is H, loweralkyl, ##STR2## where Y is O or S; R.sub.2 is alkyl, cycloalkyl, bicyclcalkyl, cycloalkenyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl, R.sub.3 is H or alkyl, or the group --NR.sub.2.sub.R.sub.3 taken as a whole is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-thiomorpholinyl, 1-piperazinyl, 4-methyl-1-piperazinyl or 2-(2,6-dichlorophenylimino)-1-imidazolidinyl) and R.sub.4 is hydrogen, loweralkyl, arylloweralkyl, diarylloweralkyl, aryl or heteroaryl,(c) m is 1 or 2;(d) each Z is independently H, loweralkyl, halogen, nitro, --NH.sub.2, loweralkylcarbonylamino, arylcarbonylamino, loweralkoxycarbonylamino or loweralkylamino, and(e) R.sub.1 is H, loweralkyl, arylloweralkyl, heheroarylloweralkyl, cycloalkylmethyl or loweralkenylmethyl, with the proviso that when X is O, m is l, Z is H and R.sub.1 is methyl, R is not --CONHCH.sub.3, --CONHC.sub.6 H.sub.5, hydrogen, methyl or ethyl, and that when X is O, m is l and Z and R.sub.1 are both hydrogen, R is not hydrogen or methyl, and, pharmaceutically acceptable acid addition salts thereof which are useful as memory-enhancing and analgesic agents.

摘要翻译： 描述了式（I）的化合物，其中X是O或S; （b）R是H，低级烷基，其中Y是O或S; R2是烷基，环烷基，双环烷基，环烯基，芳基，芳基低级烷基，杂芳基或杂芳基低级烷基，R3是H或烷基，或作为整体的基团-NR2R3是1-吡咯烷基，1-哌啶基，4-吗啉基，4-硫代吗啉基， 1-哌嗪基，4-甲基-1-哌嗪基或2-（2,6-二氯苯基亚氨基）-1-咪唑烷基），R4是氢，低级烷基，芳基低级烷基，二芳基低级烷基，芳基或杂芳基，（c）m是1或2; （d）每个Z独立地是H，低级烷基，卤素，硝基，-NH 2，低级烷基羰基氨基，芳基羰基氨基，低级烷氧基羰基氨基或低级烷基氨基，和（e）R 1是H，低级烷基，芳基低级烷基，杂芳基芳基低级烷基，环烷基甲基或低级烯基甲基，条件是当X 是O，m是1，Z是H，R1是甲基，R不是-CONHCH3，-CONHC6H5，氢，甲基或乙基，当X是O时，m是1，Z和R1都是氢，R是 不是氢或甲基，和其药学上可接受的酸加成盐，其可用作记忆增强剂和止痛剂。

公开(公告)号：US5550253A

公开(公告)日：1996-08-27

申请号：US483696

申请日：1995-06-07

申请人： R. Richard L. Hamer ,  Grover C. Helsley ,  Edward J. Glamkowski ,  Yulin Chiang

发明人： R. Richard L. Hamer ,  Grover C. Helsley ,  Edward J. Glamkowski ,  Yulin Chiang

IPC分类号： A61K31/40 ,  A61K31/44 ,  A61K31/495 ,  A61K31/535 ,  A61P25/04 ,  A61P25/28 ,  C07D487/04

CPC分类号： C07D487/04

摘要： There are described compounds of the formula ##STR1## where (a) X is O or S;(b) R is H, loweralkyl, ##STR2## where Y is O or S; R.sub.2 is alkyl, cycloalkyl, bicycloalkyl, cycloalkenyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl, R.sub.3 is H or alkyl, or the group --NR.sub.2 R.sub.3 taken as a whole is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-thiomorpholinyl, 1-piperazinyl, 4-methyl-1-piperazinyl or 2(2,6-dichlorophenylimino)-1-imidazolidinyl) and R.sub.4 is hydrogen, loweralkyl, arylloweralkyl, diarylloweralkyl, aryl or heteroaryl,(c) m is 1 or 2;(d) each Z is independently H, loweralkyl, halogen, nitro, --NH.sub.2, loweralkylcarbonylamino, arylcarbonylamino, loweralkoxycarbonylamino or loweralkylamino, and(e) R.sub.1 is H, loweralkyl, arylloweralkyl, heteroarylloweralkyl, cycloalkylmethyl or loweralkenylmethyl, with the proviso that when X is O, m is 1, Z is H and R.sub.1 is methyl, R is not --CONHCH.sub.3, --CONHC.sub.6 H.sub.5, hydrogen, methyl or ethyl, and that when X is O, m is 1 and Z and R.sub.1 are both hydrogen, R is not hydrogen or methyl, and pharmaceutically acceptable acid addition salts thereof which are useful as memory-enhancing and analgesic agents.

摘要翻译： 描述了式（IMAGE）的化合物，其中（a）X是O或S; （b）R是H，低级烷基，其中Y是O或S; R2是烷基，环烷基，二环烷基，环烯基，芳基，芳基低级烷基，杂芳基或杂芳基低级烷基，R3是H或烷基，或作为整体的基团-NR2R3是1-吡咯烷基，1-哌啶基，4-吗啉基，4-硫代吗啉基， 芳基或杂芳基，（c）m是1或2;和（c）m是1或2; （d）每个Z独立地是H，低级烷基，卤素，硝基，-NH 2，低级烷基羰基氨基，芳基羰基氨基，低级烷氧基羰基氨基或低级烷基氨基，和（e）R 1是H，低级烷基，芳基低级烷基，杂芳基低级烷基，环烷基甲基或低级烯基甲基，条件是当X 是O，m是1，Z是H，R1是甲基，R不是-CONHCH3，-CONHC6H5，氢，甲基或乙基，当X是O时，m是1，Z和R1都是氢，R是 不是氢或甲基，以及其药学上可接受的酸加成盐，其可用作记忆增强剂和止痛剂。

公开(公告)号：US5541340A

公开(公告)日：1996-07-30

申请号：US486256

申请日：1995-06-07

申请人： Richard L. Hamer ,  Grover C. Helsley ,  Edward J. Glamkowski ,  Yulin Chiang

发明人： Richard L. Hamer ,  Grover C. Helsley ,  Edward J. Glamkowski ,  Yulin Chiang

IPC分类号： A61K31/40 ,  A61K31/44 ,  A61K31/495 ,  A61K31/535 ,  A61P25/04 ,  A61P25/28 ,  C07D487/04

CPC分类号： C07D487/04

摘要： There are described compounds of the formula ##STR1## where (a) X is O or S;(b) R is H, loweralkyl, ##STR2## where Y is O or S; R.sub.2 is alkyl, cycloalkyl, bicycloalkyl, cycloalkenyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl, R.sub.3 is H or alkyl, or the group --NR.sub.2 R.sub.3 taken as a whole is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-thiomorpholinyl, 1-piperazinyl, 4-methyl-1-piperazinyl or 2-(2,6-dichlorophenylimino)-1-imidazolidinyl) and R.sub.4 is hydrogen, loweralkyl, arylloweralkyl, diarylloweralkyl, aryl or heteroaryl,(c) m is 1 or 2;(d) each Z is independently H, loweralkyl, halogen, nitro, --NH.sub.2, loweralkylcarbonylamino, arylcarbonylamino, loweralkoxycarbonylamino or loweralkylamino, and(e) R.sub.1 is H, loweralkyl, arylloweralkyl, heteroarylloweralkyl, cycloalkylmethyl or loweralkenylmethyl,with the proviso that when X is O, m is 1, Z is H and R.sub.1 is methyl, R is not --CONHCH.sub.3, --CONHC.sub.6 H.sub.5, hydrogen, methyl or ethyl, and that when X is O, m is 1 and Z and R.sub.1 are both hydrogen, R is not hydrogen or methyl, and pharmaceutically acceptable acid addition salts thereof which are useful as memory-enhancing and analgesic agents.

摘要翻译： 描述了式（IMAGE）的化合物，其中（a）X是O或S; （b）R是H，低级烷基，其中Y是O或S; R2是烷基，环烷基，二环烷基，环烯基，芳基，芳基低级烷基，杂芳基或杂芳基低级烷基，R3是H或烷基，或作为整体的基团-NR2R3是1-吡咯烷基，1-哌啶基，4-吗啉基，4-硫代吗啉基， 1-哌嗪基，4-甲基-1-哌嗪基或2-（2,6-二氯苯基亚氨基）-1-咪唑烷基），R4是氢，低级烷基，芳基低级烷基，二芳基低级烷基，芳基或杂芳基，（c）m是1或2; （d）每个Z独立地是H，低级烷基，卤素，硝基，-NH 2，低级烷基羰基氨基，芳基羰基氨基，低级烷氧基羰基氨基或低级烷基氨基，和（e）R 1是H，低级烷基，芳基低级烷基，杂芳基低级烷基，环烷基甲基或低级烯基甲基，条件是当X 是O，m是1，Z是H，R1是甲基，R不是-CONHCH3，-CONHC6H5，氢，甲基或乙基，当X是O时，m是1，Z和R1都是氢，R是 不是氢或甲基，以及其药学上可接受的酸加成盐，其可用作记忆增强剂和止痛剂。

公开(公告)号：US5541216A

公开(公告)日：1996-07-30

申请号：US967534

申请日：1992-10-28

申请人： Richard L. Hamer ,  Grover C. Helsley ,  Edward J. Glamkowski ,  Yulin Chiang

发明人： Richard L. Hamer ,  Grover C. Helsley ,  Edward J. Glamkowski ,  Yulin Chiang

IPC分类号： A61K31/40 ,  A61K31/44 ,  A61K31/495 ,  A61K31/535 ,  A61P25/04 ,  A61P25/28 ,  C07D487/04

CPC分类号： C07D487/04

摘要： There are described compounds of the formula ##STR1## where (a) X is O or S;(b) R is H, loweralkyl, ##STR2## where Y is O or S; R.sub.2 is alkyl, cycloalkyl, bicycloalkyl, cycloalkenyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl, R.sub.3 is H or alkyl, or the group --NR.sub.2 R.sub.3 taken as a whole is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-thiomorpholinyl, 1-piperazinyl, 4-methyl-1-piperazinyl or 2-(2,6-dichlorophenylimino)-1-imidazolidinyl) and R.sub.4 is hydrogen, loweralkyl, arylloweralkyl, diarylloweralkyl, aryl or heteroaryl,(c) m is 1 or 2;each Z is independently H, loweralkyl, halogen, nitro, --NH.sub.2, loweralkylcarbonylamino, arylcarbonylamino, loweralkoxycarbonylamino or loweralkylamino, and(e) R.sub.1 is H, loweralkyl, arylloweralkyl, heteroarylloweralkyl, cycloalkylmethyl or loweralkenylmethyl,with the proviso that when X is O, m is 1, Z is H and R.sub.1 is methyl, R is not --CONHCH.sub.3, --CONHC.sub.6 H.sub.5, hydrogen, methyl or ethyl, and that when X is O, m is 1 and Z and R.sub.1 are both hydrogen, R is not hydrogen or methyl, and pharmaceutically acceptable acid addition salts thereof which are useful as memory-enhancing and analgesic agents.

摘要翻译： 描述了式（IMAGE）的化合物，其中（a）X是O或S; （b）R是H，低级烷基，其中Y是O或S; R2是烷基，环烷基，二环烷基，环烯基，芳基，芳基低级烷基，杂芳基或杂芳基低级烷基，R3是H或烷基，或作为整体的基团-NR2R3是1-吡咯烷基，1-哌啶基，4-吗啉基，4-硫代吗啉基， 1-哌嗪基，4-甲基-1-哌嗪基或2-（2,6-二氯苯基亚氨基）-1-咪唑烷基），R4是氢，低级烷基，芳基低级烷基，二芳基低级烷基，芳基或杂芳基，（c）m是1或2; 每个Z独立地是H，低级烷基，卤素，硝基，-NH 2，低级烷基羰基氨基，芳基羰基氨基，低级烷氧基羰基氨基或低级烷基氨基，和（e）R 1是H，低级烷基，芳基低级烷基，杂芳基低级烷基，环烷基甲基或低级烯基甲基，条件是当X是O时， m是1，Z是H，R1是甲基，R不是-CONHCH3，-CONHC6H5，氢，甲基或乙基，当X是O时，m是1，Z和R1都是氢，R不是氢或 甲基和其药学上可接受的酸加成盐，其可用作记忆增强和止痛剂。

公开(公告)号：US5919798A

公开(公告)日：1999-07-06

申请号：US468075

申请日：1995-06-06

申请人： Joseph T. Strupczewski ,  Grover C. Helsley ,  Edward J. Glamkowski ,  Yulin Chiang ,  Kenneth J. Bordeau ,  Peter A. Nemoto ,  John J. Tegeler

发明人： Joseph T. Strupczewski ,  Grover C. Helsley ,  Edward J. Glamkowski ,  Yulin Chiang ,  Kenneth J. Bordeau ,  Peter A. Nemoto ,  John J. Tegeler

IPC分类号： A61K31/415 ,  A61K31/42 ,  A61K31/425 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/4453 ,  A61K31/47 ,  A61K31/495 ,  A61K31/496 ,  A61K31/505 ,  A61K31/55 ,  A61P23/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/18 ,  C07C45/45 ,  C07C45/67 ,  C07C45/71 ,  C07C49/84 ,  C07C233/25 ,  C07C233/33 ,  C07C255/54 ,  C07C323/22 ,  C07D207/08 ,  C07D221/04 ,  C07D231/56 ,  C07D239/02 ,  C07D261/20 ,  C07D275/04 ,  C07D275/06 ,  C07D277/82 ,  C07D401/00 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/00 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/00 ,  C07D417/04 ,  C07D417/14 ,  C07D419/00 ,  C07D471/04 ,  C07F7/18 ,  A61K31/535

CPC分类号： C07D231/56 ,  C07C233/25 ,  C07C233/33 ,  C07C255/54 ,  C07C323/22 ,  C07C45/45 ,  C07C45/673 ,  C07C45/71 ,  C07D207/08 ,  C07D261/20 ,  C07D275/04 ,  C07D275/06 ,  C07D277/82 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04 ,  C07F7/1856

摘要： Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

摘要翻译： 杂芳基哌啶，吡咯烷酮和哌嗪可用作抗精神病药和镇痛药。 通过向哺乳动物施用精神病治疗有效量的一种化合物，该化合物特别可用于治疗精神病。 化合物的储备衍生物可用于提供化合物的长效作用。 通过向哺乳动物施用减轻疼痛的有效量的一种化合物，化合物也可用作镇痛药。