公开(公告)号：US6002005A

公开(公告)日：1999-12-14

申请号：US72469

申请日：1998-05-04

申请人： Jun Yuan ,  Jan W.F. Wasley

发明人： Jun Yuan ,  Jan W.F. Wasley

IPC分类号： C07D233/54 ,  C07D401/06 ,  C07D403/12 ,  C07D498/04 ,  C07D239/02 ,  C07D241/04 ,  C07D295/00

CPC分类号： C07D233/64 ,  C07D401/06 ,  C07D403/12

摘要： Disclosed are compounds of the formula: ##STR1## wherein: A represents arylalkyl, aryl or heteroaryl; X is nitrogen or CH; and R.sub.2, R.sub.3, R4 and R.sub.5 represent organic or inorganic substituents;and the pharmaceutically acceptable salts thereof;useful for treating disorders of the central nervous system.

摘要翻译： 公开了下式的化合物：其中：A表示芳基烷基，芳基或杂芳基; X是氮或CH; R2，R3，R4和R5代表有机或无机取代基; 及其药学上可接受的盐; 可用于治疗中枢神经系统疾病。

公开(公告)号：US5973152A

公开(公告)日：1999-10-26

申请号：US088149

申请日：1998-06-01

申请人： Jun Yuan

发明人： Jun Yuan

IPC分类号： A61P25/04 ,  A61K31/415 ,  A61K31/454 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/5377 ,  A61P25/00 ,  A61P25/22 ,  A61P25/24 ,  C07D231/12 ,  C07D231/14 ,  C07D401/06

CPC分类号： C07D231/12 ,  C07D231/14 ,  C07D401/06

摘要： Disclosed are compounds that are highly selective partial agonists or antagonists at human CRF.sub.1 receptors that are useful in the diagnosis and treatment of treating stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety. The compounds have the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein Ar, R.sub.1, R.sub.2, A, and Z are various organic and inorganic substituents.

摘要翻译： 公开了在人CRF1受体上是高选择性部分激动剂或拮抗剂的化合物，其可用于治疗应激相关疾病如创伤后应激障碍（PTSD）以及抑郁症，头痛和焦虑症的诊断和治疗。 所述化合物具有式或其药学上可接受的盐，其中Ar，R 1，R 2，A和Z是各种有机和无机取代基。

公开(公告)号：US5929246A

公开(公告)日：1999-07-27

申请号：US088331

申请日：1998-06-01

申请人： Jun Yuan ,  Xi Chen

发明人： Jun Yuan ,  Xi Chen

IPC分类号： B32B15/08 ,  C07D333/76 ,  C07D409/12 ,  C08G73/10 ,  H05K1/03 ,  C07D409/14

CPC分类号： C07D409/12 ,  B32B15/08 ,  C07D333/76 ,  C08G73/10 ,  C08G73/1007 ,  C08G73/101 ,  H05K1/0346

摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof, wherein:R.sub.1, R.sub.2, R.sub.3, R.sub.4 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C.sub.1 -C.sub.6 alkoxy, --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; orR.sub.1, R.sub.2, R.sub.3, R.sub.4 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl;R5 is hydrogen or C.sub.1 -C.sub.6 alkyl; andR represents an aminoalkyl group, which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders. Further, compounds of this invention may be useful in treating the extrapyramidal side effects associated with the use of conventional neuroleptic agents.

公开(公告)号：US5892041A

公开(公告)日：1999-04-06

申请号：US695712

申请日：1996-08-12

申请人： Jun Yuan ,  Jan William Francis Wasley

发明人： Jun Yuan ,  Jan William Francis Wasley

IPC分类号： C07D209/88 ,  C07D403/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14

CPC分类号： C07D209/88

摘要： Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof wherein: ##STR2## represents an aromatic or alicyclic ring; R.sub.1 and R.sub.2 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C.sub.1 -C.sub.6 alkoxy, --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; orR.sub.1 and R.sub.2 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.3 is hydrogen, C.sub.1 -C.sub.6 alkyl, or --COR'" where R'" is C.sub.1 -C.sub.6 alkyl;R.sub.4 is hydrogen or C.sub.1 -C.sub.6 alkyl; andR represents an aminoalkyl group,which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders. Further, compounds of this invention are useful in treating the extrapyramidal side effects associated with the use of conventional neuroleptic agents.

摘要翻译： 公开了下式的化合物：其中：＆lt; IMAGE＆gt;或其药学上可接受的酸加成盐，其中：＆lt; IMAGE＆gt;代表芳族或脂环族环; R1和R2相同或不同，表示氢，C1-C6烷基，卤素，羟基，氨基，氰基，硝基，三氟甲基，三氟甲氧基，C1-C6烷氧基，-O2CR'， - NHCOR'，-COR'，-SOmR '，其中R'是C 1 -C 6烷基，其中m是0,1或2; 或R 1和R 2独立地表示-CONR'R“或-NR'R”，其中R'和R“独立地表示氢或C 1 -C 6烷基; R 3是氢，C 1 -C 6烷基或-COR“'，其中R”'是C 1 -C 6烷基; R4是氢或C1-C6烷基; R代表氨基烷基，该化合物可用于治疗情感障碍如精神分裂症，抑郁症，阿尔茨海默氏病，运动障碍如帕金森综合征和肌张力障碍，以及其他对多巴胺能阻滞作用的药物滥用和强迫症 。 此外，本发明的化合物可用于治疗与使用常规精神抑制剂相关的锥体束外副作用。

公开(公告)号：US5773616A

公开(公告)日：1998-06-30

申请号：US463759

申请日：1995-06-05

申请人： Jun Yuan ,  Andrew Thurkauf

发明人： Jun Yuan ,  Andrew Thurkauf

IPC分类号： C07D235/02 ,  C07D403/12 ,  C07D491/04 ,  C07D403/14 ,  C07D401/14

CPC分类号： C07D235/02 ,  C07D403/12 ,  C07D491/04

摘要： Disclosed are compounds encompassed by the following general formula: ##STR1## wherein, A represents ethenylene, or A represents --X--CH.sub.2 --; where X is carbon or oxygen, provided that when X is oxygen, the oxygen is adjacent the 6-membered ring; R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are inorganic or organic substituents; and R.sub.5 and R.sub.6 is are optionally substituted organic substituents; or NR.sub.5 R.sub.6 represents a carbocyclic or heterocyclic six membered ring optionally substituted with various orgainic or inorganic groups, which compounds can be used in the treatment of neuropsychological disorders.

摘要翻译： 公开的是由以下通式包括的化合物：其中A表示亚乙烯基，或A表示-X-CH2-; 其中X是碳或氧，条件是当X是氧时，氧与6元环相邻; R1，R2，R3和R4是无机或有机取代基; 并且R 5和R 6是任选取代的有机取代基; 或NR 5 R 6表示任选被各种有机或无机基团取代的碳环或杂环六元环，该化合物可用于治疗神经心理障碍。

公开(公告)号：US5763609A

公开(公告)日：1998-06-09

申请号：US619429

申请日：1996-03-21

申请人： Jun Yuan ,  Xi Chen

发明人： Jun Yuan ,  Xi Chen

IPC分类号： B32B15/08 ,  C07D333/76 ,  C07D409/12 ,  C08G73/10 ,  H05K1/03 ,  C07D409/14

CPC分类号： C07D409/12 ,  B32B15/08 ,  C07D333/76 ,  C08G73/10 ,  C08G73/1007 ,  C08G73/101 ,  H05K1/0346

摘要： Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C.sub.1 -C.sub.6 alkoxy, --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; or R.sub.1, R.sub.2, R.sub.3, R.sub.4 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl; and R represents an aminoalkyl group, which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders. Further, compounds of this invention may be useful in treating the extrapyramidal side effects associated with the use of conventional neuroleptic agents.

摘要翻译： 公开了下式的化合物或其药学上可接受的酸加成盐，其中：R 1，R 2，R 3，R 4相同或不同，表示氢，C 1 -C 6烷基，卤素，羟基，氨基，氰基， 硝基，三氟甲基，三氟甲氧基，C 1 -C 6烷氧基，-O 2 CR'， - NHCOR'， - CON'，-SO m R'，其中R'是C 1 -C 6烷基，其中m是0,1或2; 或R 1，R 2，R 3，R 4独立地表示-CONR'R“或-NR'R”，其中R'和R“独立地表示氢或C 1 -C 6烷基; R5是氢或C1-C6烷基; R代表氨基烷基，该化合物可用于治疗情感障碍如精神分裂症，抑郁症，阿尔茨海默氏病，运动障碍如帕金森综合征和肌张力障碍，以及其他对多巴胺能阻滞作用的药物滥用和强迫症 。 此外，本发明的化合物可用于治疗与使用常规精神抑制剂相关的锥体束外副作用。

公开(公告)号：US5750700A

公开(公告)日：1998-05-12

申请号：US459093

申请日：1995-06-02

申请人： Jun Yuan ,  Jan W. F. Wasley

发明人： Jun Yuan ,  Jan W. F. Wasley

IPC分类号： C07D233/54 ,  C07D401/06 ,  C07D403/12 ,  C07D498/04

CPC分类号： C07D233/64 ,  C07D401/06 ,  C07D403/12

摘要： Disclosed are compounds of the formula: ##STR1## wherein: A represents arylalkyl, aryl or heteroaryl; X is nitrogen or CH; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent organic or inorganic substituents; and the pharmaceutically acceptable salts thereof; useful for treating disorders of the central nervous system.

公开(公告)号：US5723608A

公开(公告)日：1998-03-03

申请号：US775404

申请日：1996-12-31

申请人： Jun Yuan

发明人： Jun Yuan

IPC分类号： A61P25/04 ,  A61K31/519 ,  A61P25/00 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00 ,  C07D487/04

CPC分类号： C07D487/04

摘要： This invention encompasses compounds of the formula ##STR1## wherein Ar represents a mono-, di- or trisubstituted aryl group where at least one position on Ar ortho to the point of attachment to the pyrazole ring is substituted; and R.sub.1 represents lower alkyl; R.sub.2 is hydrogen or lower alkyl; and R.sub.3 and R.sub.4 independently represent organic and inorganic substituents, which compounds are highly selective partial agonists or antagonists at human CRF.sub.1 receptors and are useful in the diagnosis and treatment of treating stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety.

摘要翻译： 本发明包括下式的化合物：其中Ar表示单取代，二取代或三取代的芳基，其中与吡唑环连接点上Ar邻位的至少一个位置被取代; 并且R 1表示低级烷基; R2是氢或低级烷基; R3和R4独立地表示有机和无机取代基，该化合物是人CRF1受体的高选择性部分激动剂或拮抗剂，可用于诊断和治疗应激相关疾病如创伤后应激障碍（PTSD）以及抑郁症 ，头痛和焦虑。

公开(公告)号：US5712392A

公开(公告)日：1998-01-27

申请号：US464548

申请日：1995-06-05

申请人： Andrew Thurkauf ,  Raymond F. Horvath ,  Jun Yuan ,  John M. Peterson

发明人： Andrew Thurkauf ,  Raymond F. Horvath ,  Jun Yuan ,  John M. Peterson

IPC分类号： C07D233/54 ,  C07D233/64 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/04 ,  A61K31/415 ,  C07D403/06

CPC分类号： C07D233/64 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

摘要： Disclosed are compounds of the formula ##STR1## wherein R.sub.1 represents optionally substituted aryl, heteroaryl, arylalkyl, or cycloalkyl groups; X, Z, and Y are optionally substituted nitrogen or carbon atoms; R.sub.3 and R.sub.4 are organic or inorganic substituents which may together form ring structures; m is zero, one or two; and R.sub.5 and R.sub.6 are are organic or inorganic substituents; and the pharmaceutically acceptable addition salts thereof, which compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.

摘要翻译： 公开了式IMA的化合物，其中R 1表示任选取代的芳基，杂芳基，芳基烷基或环烷基; X，Z和Y是任选取代的氮或碳原子; R3和R4是可以一起形成环结构的有机或无机取代基; m为零，一或二; R5和R6是有机或无机取代基; 和其药学上可接受的加成盐，该化合物是脑多巴胺受体亚型或其前药的高选择性部分激动剂或拮抗剂，并且可用于诊断和治疗情感障碍如精神分裂症和抑郁症以及某些运动障碍如帕金森综合征 。

公开(公告)号：US5656762A

公开(公告)日：1997-08-12

申请号：US461858

申请日：1995-06-05

申请人： Andrew Thurkauf ,  Raymond F. Horvath ,  Jun Yuan ,  John M. Peterson

发明人： Andrew Thurkauf ,  Raymond F. Horvath ,  Jun Yuan ,  John M. Peterson

IPC分类号： C07D233/54 ,  C07D233/64 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/06 ,  C07D403/04

CPC分类号： C07D233/64 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

摘要： Disclosed are compounds of the formula: ##STR1## wherein R.sub.1 represents optionally substituted aryl, heteroaryl, arylalkyl, or cycloalkyl groups; X, Z, and Y optionally substituted nitrogen or carbon atoms; R.sub.3 and R.sub.4 are organic or inorganic substitutents which may together form ring structures; m is zero, one or two; and R.sub.5 and R.sub.6 are are organic or inorganic substituents;and the pharmaceutically acceptable addition salts thereof, which compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.

摘要翻译： 公开了下式的化合物：其中R 1表示任选取代的芳基，杂芳基，芳烷基或环烷基; X，Z和Y任选取代的氮或碳原子; R3和R4是可以一起形成环结构的有机或无机取代基; m为零，一或二; R5和R6是有机或无机取代基; 和其药学上可接受的加成盐，该化合物是脑多巴胺受体亚型或其前药的高选择性部分激动剂或拮抗剂，并且可用于诊断和治疗情感障碍如精神分裂症和抑郁症以及某些运动障碍如帕金森综合征 。