公开(公告)号：US5883257A

公开(公告)日：1999-03-16

申请号：US994588

申请日：1997-12-19

Applicant: Jun Yuan ,  Xi Chen

Inventor： Jun Yuan ,  Xi Chen

IPC: C07D295/12 ,  A61K31/44 ,  A61K31/445 ,  A61K31/451 ,  A61K31/495 ,  A61P25/00 ,  A61P25/18 ,  A61P25/20 ,  A61P25/28 ,  A61P25/30 ,  C07D211/14 ,  C07D211/28 ,  C07D211/70 ,  C07D217/02 ,  C07D295/13 ,  C07D401/12

CPC classification number: C07D295/13 ,  C07D211/14 ,  C07D211/70 ,  C07C2103/24

Abstract: 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, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 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, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.10 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.

Abstract translation: 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，R 5，R 6，R 7，R 8和R 9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'，-COR'，-SO m R'，其中R'是C 1 -C 6烷基， ，1或2; 或R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8和R 9独立地表示-CONR'R“或-NR'R”，其中R'和R“独立地表示氢或C1-C6烷基; R 10是氢或C 1 -C 6烷基; R表示氨基烷基; 哪些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：US5703235A

公开(公告)日：1997-12-30

申请号：US619351

申请日：1996-03-21

Applicant: Jun Yuan ,  Xi Chen

Inventor： Jun Yuan ,  Xi Chen

IPC: C07D295/12 ,  A61K31/44 ,  A61K31/445 ,  A61K31/451 ,  A61K31/495 ,  A61P25/00 ,  A61P25/18 ,  A61P25/20 ,  A61P25/28 ,  A61P25/30 ,  C07D211/14 ,  C07D211/28 ,  C07D211/70 ,  C07D217/02 ,  C07D295/13 ,  C07D401/10 ,  C07D295/15

CPC classification number: C07D295/13 ,  C07D211/14 ,  C07D211/70 ,  C07C2103/24

Abstract: 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, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 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, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.10 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.

Abstract translation: 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，R 5，R 6，R 7，R 8和R 9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'，-COR'，-SO m R'，其中R'是C 1 -C 6烷基， ，1或2; 或R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8和R 9独立地表示-CONR'R“或-NR'R”，其中R'和R“独立地表示氢或C1-C6烷基; R 10是氢或C 1 -C 6烷基; R表示氨基烷基; 哪些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：US06239179B1

公开(公告)日：2001-05-29

申请号：US09497989

申请日：2000-02-04

Applicant: Jun Yuan ,  Xi Chen

Inventor： Jun Yuan ,  Xi Chen

IPC: A61K31166

CPC classification number: C07D295/13 ,  C07C2603/24 ,  C07D211/14 ,  C07D211/70

Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof, wherein: R1, R2, R3, R4, R5, R6, R7, R8 and R9 are the same or different and represent hydrogen, C1-C6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C1-C6 alkoxy, —O2CR′, —NHCOR′, —COR′, —SOmR′, where R′ is C1-C6 alkyl and wherein m is 0, 1 or 2; or R1, R2, R3, R4, R5, R6, R7, R8 and R9 independently represent —CONR′R″, or —NR′R″ where R′ and R″ independently represent hydrogen or C1-C6 alkyl; R10 is hydrogen or C1-C6 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.

Abstract translation: 公开了下式的化合物或其药学上可接受的酸加成盐，其中：R1，R2，R3，R4，R5，R6，R7，R8和R9相同或不同，代表氢，C1-C6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'，-COR'，-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，R 5，R 6，R 7，R 8和R 9独立地表示-CONR'R“或-NR'R”，其中R'和R“独立地表示氢或C1-C6烷基; R10 是氢或C 1 -C 6烷基; R代表氨基烷基;这些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：US6040459A

公开(公告)日：2000-03-21

申请号：US368542

申请日：1999-08-05

Applicant: Jun Yuan ,  Xi Chen

Inventor： Jun Yuan ,  Xi Chen

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

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

Abstract: 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; 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;R.sub.5 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.

Abstract translation: 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'，-COR'，-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：US5929246A

公开(公告)日：1999-07-27

申请号：US088331

申请日：1998-06-01

Applicant: Jun Yuan ,  Xi Chen

Inventor： Jun Yuan ,  Xi Chen

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

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

Abstract: 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：US5763609A

公开(公告)日：1998-06-09

申请号：US619429

申请日：1996-03-21

Applicant: Jun Yuan ,  Xi Chen

Inventor： Jun Yuan ,  Xi Chen

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

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

Abstract: 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.

Abstract translation: 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：US5703083A

公开(公告)日：1997-12-30

申请号：US631152

申请日：1996-04-15

Applicant: Xi Chen ,  Jun Yuan

Inventor： Xi Chen ,  Jun Yuan

IPC: C07D295/14 ,  A61K31/44 ,  A61K31/47 ,  A61K31/472 ,  A61K31/495 ,  A61P25/00 ,  A61P25/14 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07D213/74 ,  C07D215/40 ,  C07D217/04 ,  C07D217/22 ,  C07D239/26 ,  C07D295/12 ,  C07D295/13 ,  C07D333/54

CPC classification number: C07D295/13 ,  C07D217/22

Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addidon salts thereof wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 independently represent hydrogen, halogen, hydroxy, alkyl, alkoxy, amino, aminosulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl, cyano, nitro, trifluoromethyl, or trifluoromethoxy; R.sub.8 is hydrogen or lower alkyl; X represents an optionally substituted alkylene group; and Y represents a mono-, di- or trisubsituted cyclic amino group which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parldnsonism 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.

Abstract translation: 公开了下式的化合物或其药学上可接受的酸加成盐，其中：R1，R2，R3，R4，R5，R6和R7独立地表示氢，卤素，羟基，烷基，烷氧基，氨基，氨基磺酰基 ，烷基氨基磺酰基，二烷基氨基磺酰基，氰基，硝基，三氟甲基或三氟甲氧基; R8是氢或低级烷基; X表示任选取代的亚烷基; 并且Y代表单，二或三取代的环状氨基，该化合物可用于治疗情感障碍如精神分裂症，抑郁症，阿尔茨海默病，运动障碍如帕尔德森氏症和肌张力障碍，以及其他对多巴胺能阻滞作用的其它病症 作为物质滥用和强迫症。 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：US5659033A

公开(公告)日：1997-08-19

申请号：US527790

申请日：1995-09-13

Applicant: Jun Yuan ,  Xi Chen

Inventor： Jun Yuan ,  Xi Chen

IPC: C07D295/12 ,  A61K31/00 ,  A61K31/38 ,  A61K31/381 ,  A61K31/445 ,  A61K31/451 ,  A61K31/495 ,  A61K31/496 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P43/00 ,  C07D211/14 ,  C07D211/18 ,  C07D211/32 ,  C07D211/70 ,  C07D217/02 ,  C07D217/04 ,  C07D295/13 ,  C07D333/20 ,  C07D333/34

CPC classification number: C07D295/13 ,  C07D211/14 ,  C07D211/32 ,  C07D211/70 ,  C07D217/02 ,  C07C2103/18

Abstract: Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein: G represents a group of the formula ##STR2## where R.sub.a and R.sub.b represent hydrogen, or organic or inorganic substituents;A is an optionally substituted alkylene;R.sub.1, R.sub.2, R.sub.3, R.sub.4 represent organic or inorganic substituents;R.sub.5 is hydrogen or lower alkyl;R.sub.6 and R.sub.7 independently represent hydrogen, lower alkyl; or together form a ring of 5-8 members;Z is nitrogen or carbon; andW is optionally substituted aryl or heteroaryl.Compounds of the present invention demonstrate high affinity and selectivity in binding to the D.sub.3 receptor subtype.

Abstract translation: 公开了式IMA的化合物或其药学上可接受的盐，其中：G表示式Ia的基团，其中R a和R b表示氢，或有机或无机取代基; A是任选取代的亚烷基; R1，R2，R3，R4代表有机或无机取代基; R5是氢或低级烷基; R6和R7独立地表示氢，低级烷基; 或一起组成5-8名成员的戒指; Z是氮或碳; W是任选取代的芳基或杂芳基。 本发明化合物在与D3受体亚型结合中表现出高亲和力和选择性。

公开(公告)号：US06221869B1

公开(公告)日：2001-04-24

申请号：US09499066

申请日：2000-02-04

Applicant: Jun Yuan ,  Xi Chen

Inventor： Jun Yuan ,  Xi Chen

IPC: A61K31496

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

Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof, wherein: R1, R2, R3, R4 are the same or different and represent hydrogen, C1-C6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C1-C6 alkoxy, —O2CR′, —NHCOR′, —COR′, —SOmR′, where R′ is C1-C6 alkyl and wherein m is 0, 1 or 2; or R1, R2, R3, R4 independently represent —CONR′R″, or —NR′R″ where R′ and R″ independently represent hydrogen or C1-C6 alkyl; R5 is hydrogen or C1-C6 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.

Abstract translation: 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'，-COR'，-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; R 5是氢或C 1 -C 6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：US6025493A

公开(公告)日：2000-02-15

申请号：US264448

申请日：1999-03-08

Applicant: Jun Yuan ,  Xi Chen

Inventor： Jun Yuan ,  Xi Chen

IPC: C07D295/12 ,  A61K31/44 ,  A61K31/445 ,  A61K31/451 ,  A61K31/495 ,  A61P25/00 ,  A61P25/18 ,  A61P25/20 ,  A61P25/28 ,  A61P25/30 ,  C07D211/14 ,  C07D211/28 ,  C07D211/70 ,  C07D217/02 ,  C07D295/13 ,  C07D295/15

CPC classification number: C07D295/13 ,  C07D211/14 ,  C07D211/70 ,  C07C2103/24

Abstract: Disclosed arm 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, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 allyl, 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, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.10 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.

Abstract translation: 公开的下式化合物或其药学上可接受的酸加成盐，其中：R1，R2，R3，R4，R5，R6，R7，R8和R9相同或不同，代表氢，C1-C6烯丙基，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'，-COR'，-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，R 5，R 6，R 7，R 8和R 9独立地表示-CONR'R“或-NR'R”，其中R'和R“独立地表示氢或C1-C6烷基; R 10是氢或C 1 -C 6烷基; R表示氨基烷基; 哪些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。