公开(公告)号：US07101887B2

公开(公告)日：2006-09-05

申请号：US11167735

申请日：2005-06-27

申请人： Andrew Thurkauf ,  Xi Chen

发明人： Andrew Thurkauf ,  Xi Chen

IPC分类号： A61K31/495 ,  C07D295/076

CPC分类号： C07D295/073 ,  A61K31/495 ,  C07C2603/08 ,  C07D295/096 ,  C07D295/112 ,  C07D295/135

摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable addition salts thereof wherein: R1 is halogen or C1–C4 alkyl; and R2 and R3 are the same or different and represent hydrogen, halogen, C1–C4 alkyl, C1–C4 alkoxy, alkylthio, hydroxy, amino, mono(C1–C4)alkylamino, di(C1–C4)alkylamino, or R2 and R3 together represent a 4 carbon alkenylene moiety that together with the phenyl ring to which they are attached form a naphthyl moiety, which compounds are useful in the treatment of neuropsycological diseases such as schizophrenia, psychotic depression and mania.

摘要翻译： 公开了下式的化合物或其药学上可接受的加成盐，其中：R 1是卤素或C 1 -C 4烷基; R 2和R 3相同或不同，表示氢，卤素，C 1 -C 4烷基， 烷基，C 1 -C 4烷氧基，烷硫基，羟基，氨基，单（C 1 -C 4 - ）烷基氨基，二（C 1 -C 4 - ）烷基氨基或R 2和R 3一起代表一个 与它们所连接的苯环一起形成萘基部分的4碳亚烯基部分，该化合物可用于治疗神经疾病疾病如精神分裂症，精神病抑郁症和躁狂症。

公开(公告)号：US06288230B1

公开(公告)日：2001-09-11

申请号：US09408035

申请日：1999-09-29

申请人： Xi Chen ,  Xiao-shu He

发明人： Xi Chen ,  Xiao-shu He

IPC分类号： C07D24102

CPC分类号： C07D405/04 ,  C07D405/14

摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof wherein: n is an integer; R1 represents an organic or inorganic group; R2 represents halogen or C1-C6 alkyl; RN is an alkylene carrying a substituted piperazine, piperidine, or tetrahydropyridine; and R4 is hydrogen or C1-C6 alkyl, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of 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：n为整数; R1为有机或无机基团; R2为卤素或C1-C6烷基; RN为带有取代哌嗪的亚烷基，哌啶， 或四氢吡啶; 和R 4是氢或C 1 -C 6烷基，该化合物可用于治疗和/或预防神经心理障碍，包括但不限于精神分裂症，躁狂症，痴呆，抑郁，焦虑，强迫行为，物质滥用，帕金森氏样运动 与使用神经安定药相关的疾病和运动障碍。

公开(公告)号：US06221869B1

公开(公告)日：2001-04-24

申请号：US09499066

申请日：2000-02-04

申请人： Jun Yuan ,  Xi Chen

发明人： Jun Yuan ,  Xi Chen

IPC分类号： A61K31496

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: 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.

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; 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

申请人： Jun Yuan ,  Xi Chen

发明人： Jun Yuan ,  Xi Chen

IPC分类号： 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分类号： C07D295/13 ,  C07D211/14 ,  C07D211/70 ,  C07C2103/24

摘要： 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.

摘要翻译： 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。

公开(公告)号：US6015900A

公开(公告)日：2000-01-18

申请号：US43022

申请日：1998-11-23

申请人： Jun Yuan ,  Xi Chen

发明人： Jun Yuan ,  Xi Chen

IPC分类号： 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 ,  C07D295/15

CPC分类号： C07D295/13 ,  C07D211/14 ,  C07D211/32 ,  C07D211/70 ,  C07D217/02 ,  C07C2103/18

摘要： Disclosed are compounds of formula (I) or the pharmaceutically acceptable salts thereof wherein: ##STR1## G represents a group of the formula (a), (b) or (c) 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; and W is optionally susbtituted aryl or heteroaryl. Compounds of the present invention demonstrate high affinity and selectivity in binding to the D.sub.3 receptor subtype.

摘要翻译： PCT No.PCT / US96 / 14650 Sec。 371日期：1998年11月23日 102（e）1998年11月23日日期PCT 1996年9月12日PCT公布。 出版物WO97 / 10229 日期1997年3月20日公开是式（I）化合物或其药学上可接受的盐，其中：G表示式（a），（b）或（c）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; 并且W是任选的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：US5977367A

公开(公告)日：1999-11-02

申请号：US005285

申请日：1998-01-09

申请人： Jun Yuan ,  Xi Chen

发明人： Jun Yuan ,  Xi Chen

IPC分类号： A61K31/34 ,  A61K31/343 ,  A61K31/443 ,  A61K31/4525 ,  A61K31/496 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P43/00 ,  C07D307/91 ,  C07D405/12

CPC分类号： C07D307/91 ,  A61K31/496 ,  C07D405/12

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'.sub.m, or --NR'.sub.m where m is 0, 1 or 2 and R' is 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'm或-NR'm，其中m为0,1或2，R'为氢或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：US5932734A

公开(公告)日：1999-08-03

申请号：US908361

申请日：1997-08-07

申请人： Jun Yuan ,  Xi Chen

发明人： Jun Yuan ,  Xi Chen

IPC分类号： 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 ,  C07D295/15

CPC分类号： C07D295/13 ,  C07D211/14 ,  C07D211/32 ,  C07D211/70 ,  C07D217/02 ,  C07C2103/18

摘要： 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.

摘要翻译： 公开了下式的化合物或其药学上可接受的盐，其中：G表示下式的基团，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：US5710274A

公开(公告)日：1998-01-20

申请号：US608259

申请日：1996-02-28

申请人： Jun Yuan ,  Xi Chen

发明人： Jun Yuan ,  Xi Chen

IPC分类号： A61K31/34 ,  A61K31/343 ,  A61K31/443 ,  A61K31/4525 ,  A61K31/496 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P43/00 ,  C07D307/91 ,  C07D405/12 ,  C07D209/00 ,  C07D241/02 ,  C07D401/00

CPC分类号： C07D307/91 ,  A61K31/496 ,  C07D405/12

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'.sub.m, or --NR'.sub.m where m is 0, 1 or 2 and R' is 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 blockage 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'm或-NR'm，其中m为0,1或2，R'为氢或C 1 -C 6烷基; R5是氢或C1-C6烷基; 并且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塞作用的疾病，例如药物滥用和强迫症 。 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：US20240311645A1

公开(公告)日：2024-09-19

申请号：US18182744

申请日：2023-03-13

申请人： Guojun Zhang ,  Alex Bie ,  Mahdi Beitollahi ,  Xi Chen

发明人： Guojun Zhang ,  Alex Bie ,  Mahdi Beitollahi ,  Xi Chen

IPC分类号： G06N3/098

CPC分类号： G06N3/098

摘要： Methods and systems for federated learning using feature normalization are disclosed. A client implements a local model including at least: a feature extraction subnetwork to extract a feature vector from input data, a normalization layer to normalize the feature vector, and a final layer to generate a prediction output from the normalized feature vector. The local model is initialized using a set of global parameters received from a central server. The local model is updated using data sampled from a local dataset. Information about a state of the updated local model is transmitted to the central server.

公开(公告)号：US20230079877A1

公开(公告)日：2023-03-16

申请号：US17986210

申请日：2022-11-14

申请人： Nazir Mir ,  Aishwarya Balasubramanian ,  Xi Chen

发明人： Nazir Mir ,  Aishwarya Balasubramanian ,  Xi Chen

IPC分类号： B65D75/58 ,  B65D75/36

摘要： A packaging device incorporating a breathable peel/reseal film and enabling a preservation process for allowing for the distribution, storage and multiple servings of a food product, particularly perishable food product(s), and initiating and controlling the transmission rates, respiration rates or deterioration of the perishable food product(s) and thereby, maintaining good internal and external food quality and normal development of flavor and aroma characteristics. The packaging device includes a plurality of atmospheric control attributes that modulates or controls the atmosphere within the packaging device as the food product(s) respire in order to promote the extended shelf-life of the food product and the maintenance of the quality and desirable marketable characteristics of the food product. The atmospheric control attributes can include perforations that may be positioned in breathable peel/reseal film portion of the package to allow the product respiration for multiple servings without substantially altering the shelf life extension properties of the packaging device.