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    • 101. 发明授权
    • N-piperidinyl- and N-tetrahydropyridinyl-2-anthracenecarboxamides:
dopamine receptor subtype specific ligands
    • N-哌啶基和N-四氢吡啶基-2-蒽甲酰胺:多巴胺受体亚型特异性配体
    • US5883257A
    • 1999-03-16
    • US994588
    • 1997-12-19
    • Jun YuanXi Chen
    • Jun YuanXi Chen
    • C07D295/12A61K31/44A61K31/445A61K31/451A61K31/495A61P25/00A61P25/18A61P25/20A61P25/28A61P25/30C07D211/14C07D211/28C07D211/70C07D217/02C07D295/13C07D401/12
    • C07D295/13C07D211/14C07D211/70C07C2103/24
    • 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.
    • 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。
    • 103. 发明授权
    • N-Aminoalkyl-2-anthracenecarboxamides; new dopamine receptor subtype
specific ligands
    • N-氨基烷基-2-蒽基甲酰胺; 新的多巴胺受体亚型特异性配体
    • US5703235A
    • 1997-12-30
    • US619351
    • 1996-03-21
    • Jun YuanXi Chen
    • Jun YuanXi Chen
    • C07D295/12A61K31/44A61K31/445A61K31/451A61K31/495A61P25/00A61P25/18A61P25/20A61P25/28A61P25/30C07D211/14C07D211/28C07D211/70C07D217/02C07D295/13C07D401/10C07D295/15
    • C07D295/13C07D211/14C07D211/70C07C2103/24
    • 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.
    • 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。
    • 105. 发明授权
    • Certain pyrroloquinolinones: a new class of GABA brain receptor ligands
    • 某些吡咯喹啉酮:一类新的GABA脑受体配体
    • US5243049A
    • 1993-09-07
    • US823845
    • 1992-01-22
    • Kenneth ShawJun Yuan
    • Kenneth ShawJun Yuan
    • C07D471/04
    • C07D471/04
    • This invention encompasses compounds of the formula: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein X and Y are the same or different and represent oxygen or H.sub.2 with the proviso that not both X and Y are H.sub.2 ; W represents phenyl, thienyl, or pyridyl, each of which may be unsubstituted or momo or disubstituted with organic or inorganic substituents; and R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are variables representing organic and inorganic substituents.These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory.
    • 本发明包括下式的化合物及其药学上可接受的无毒盐,其中X和Y相同或不同,代表氧或H 2,条件是X和Y都不是H 2; W表示苯基,噻吩基或吡啶基,其各自可以是未取代的或用有机或无机取代基进行单或二取代; 并且R1,R2,R3和R4是表示有机和无机取代基的变量。 这些化合物是GABAa脑受体或其前药的高度选择性激动剂,拮抗剂或反向激动剂,并且可用于诊断和治疗焦虑,睡眠和癫痫发作,用苯二氮卓类药物过量和记忆增强。