公开(公告)号：US06281359B1

公开(公告)日：2001-08-28

申请号：US08457409

申请日：1995-06-01

申请人： Jun Yuan ,  Andrew Thurkauf

发明人： Jun Yuan ,  Andrew Thurkauf

IPC分类号： C07D40106

CPC分类号： C07D239/42 ,  C07C211/27 ,  C07D211/14 ,  C07D211/70 ,  C07D295/096 ,  C07D401/06

摘要： Disclosed are compounds of the formula: where S and V are various organic or inorganic substituents; G and K are the same or different and represent N or CR′ where R′ is an organic or inorganic substituent; R is hydrogen or an alkyl group; R1, X, Y, Z and T are organic or inorganic substituents; and R2 and R3 represent hydrogen or organic substituents; or NR2R3 together represents a heterocyclic ring system; and the pharmaceutically acceptable salts thereof; which are highly selective partial agonists or antagonists at brain dopamine receptor subtypes and, thus, 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S和V是各种有机或无机取代基; G和K相同或不同，表示N或CR'，其中R'是有机或无机取代基; R是氢或烷基; R 1 X，Y，Z和T​​是有机或无机取代基; 且R 2和R 3表示氢或有机取代基; 或NRR2R3一起表示杂环系统;及其药学上可接受的盐; 其是脑多巴胺受体亚型的高度选择性部分激动剂或拮抗剂，因此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：US06239179B1

公开(公告)日：2001-05-29

申请号：US09497989

申请日：2000-02-04

申请人： Jun Yuan ,  Xi Chen

发明人： Jun Yuan ,  Xi Chen

IPC分类号： A61K31166

CPC分类号： C07D295/13 ,  C07C2603/24 ,  C07D211/14 ,  C07D211/70

摘要： 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.

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：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：US6068693A

公开(公告)日：2000-05-30

申请号：US876523

申请日：1997-06-16

申请人： William L. Garforth ,  Robert J. Pruett ,  Dona L. Archer ,  Jun Yuan ,  Michael J. Garska ,  H. Vince Brown

发明人： William L. Garforth ,  Robert J. Pruett ,  Dona L. Archer ,  Jun Yuan ,  Michael J. Garska ,  H. Vince Brown

IPC分类号： B03B1/04 ,  B03B9/00 ,  B03D3/06 ,  C04B33/10 ,  C04B33/04 ,  C09C1/42

CPC分类号： B03B1/04 ,  B03B9/00 ,  B03D3/06 ,  C04B33/10

摘要： A method of enhancing the brightness and increasing the yield of a kaolin clay by optimizing the removal of the titania and mica impurities in the clay and the amount of clay remaining in the slurry is disclosed. The method is a selective flocculation process wherein the clay is blunged, dispersed, and conditioned before flocculation. In the flocculation step, a high molecular weight anionic polymer and a low molecular weight anionic polymer, such as sodium polyacrylate, are added to the slurry after the conditioning process, whereby the titania-mica enriched flocs are separated from the suspension which is enriched with kaolin. This final kaolin product has titania levels ranging from 0.1% to 0.5%, a reduced mica level, a high usable product yield, and a brightness greater than 89.5 and at least 91.5.

摘要翻译： 公开了通过优化粘土中二氧化钛和云母杂质的去除以及浆料中剩余的粘土的量来提高高岭土的亮度和提高产量的方法。 该方法是选择性絮凝过程，其中粘土在絮凝之前被白化，分散和调节。 在絮凝步骤中，在调节过程之后，将高分子量阴离子聚合物和低分子量阴离子聚合物（例如聚丙烯酸钠）加入到浆料中，由此将富含二氧化钛 - 云母的絮凝物与富集的悬浮液分离 高岭土 该最终的高岭土产品具有0.1％至0.5％的二氧化钛含量，降低的云母水平，高可用产物收率以及大于89.5和至少91.5的亮度。

公开(公告)号：US6040459A

公开(公告)日：2000-03-21

申请号：US368542

申请日：1999-08-05

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

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; 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.

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'，-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：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。