公开(公告)号：US06297256B1

公开(公告)日：2001-10-02

申请号：US09596031

申请日：2000-06-15

Applicant: Guolin Cai ,  Gang Liu ,  Pamela A. Albaugh

Inventor： Guolin Cai ,  Gang Liu ,  Pamela A. Albaugh

IPC: G07D40104

CPC classification number: C07D401/14 ,  C07D495/04

Abstract: Disclosed are aryl and heteroaryl substitated pyridino compounds. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.

Abstract translation: 公开了芳基和杂芳基取代的吡啶基化合物。 这些化合物是GABAA脑受体的高度选择性激动剂，拮抗剂或反向激动剂或GABAA脑受体的激动剂，拮抗剂或反向激动剂的前药，因此可用于诊断和治疗焦虑症，抑郁症，唐氏综合症，睡眠和癫痫发作障碍， 过量与苯二氮卓类药物和增强记忆。 还提供药物组合物，包括包装的药物组合物。 本发明的化合物也可用作组织样品中GABA A受体定位的探针。

公开(公告)号：US06448246B1

公开(公告)日：2002-09-10

申请号：US09578928

申请日：2000-05-25

Applicant: Guolin Cai ,  Gang Liu ,  Pamela A. Albaugh

Inventor： Guolin Cai ,  Gang Liu ,  Pamela A. Albaugh

IPC: C07D27916

CPC classification number: C07D417/12 ,  C07D279/16 ,  G01N33/948

Abstract: Disclosed are 4H-1,4-Benzothiazine-2-carboxamides. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, depression, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.

Abstract translation: 公开了4H-1,4-苯并噻嗪-2-甲酰胺。 这些化合物是GABAa脑受体的高选择性激动剂，拮抗剂或反向激动剂或GABAa脑受体的激动剂，拮抗剂或反向激动剂的前药。 这些化合物可用于诊断和治疗焦虑，抑郁，睡眠，认知和癫痫发作，以及用苯二氮卓类药物过量并提高警觉性。 还提供药物组合物，包括包装的药物组合物。 本发明的化合物也可用作组织样品中GABA A受体定位的探针。

公开(公告)号：US6166203A

公开(公告)日：2000-12-26

申请号：US259146

申请日：1999-02-26

Applicant: Guolin Cai ,  Gang Liu ,  Guoquing Chen ,  Pamela A. Albaugh

Inventor： Guolin Cai ,  Gang Liu ,  Guoquing Chen ,  Pamela A. Albaugh

IPC: C07D471/04 ,  C07D495/04 ,  C07D413/04 ,  C07D241/04 ,  C07D471/02 ,  C07D513/04 ,  C07D515/04

CPC classification number: C07D471/04 ,  C07D495/04

Abstract: Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: n is an integer from 0 to 3;the C ring is aryl or heteroaryl;X is CH, N, or OZ represents an electron pair, hydrogen, or (un)substituted heterocycle, aryl, or amido;W is (un)substituted alkyl, aryl, or heteroaryl;A and B are hydrogen or lower alkyl,which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.

公开(公告)号：US06423711B1

公开(公告)日：2002-07-23

申请号：US09736497

申请日：2000-12-13

Applicant: Guolin Cai ,  Gang Liu ,  Guoquing Chen ,  Pamela A. Albaugh

Inventor： Guolin Cai ,  Gang Liu ,  Guoquing Chen ,  Pamela A. Albaugh

IPC: C07D41304

CPC classification number: C07D471/04 ,  C07D495/04

Abstract: Disclosed are compounds of the formula or the pharmaceutically acceptable non-toxic salts thereof wherein: n is an integer from 0 to 3; the C ring is aryl or heteroaryl; X is CH, N, or O Z represents an electron pair, hydrogen, or (un)substituted heterocycle, aryl, or amido; W is (un)substituted alkyl, aryl, or heteroaryl; A and B are hydrogen or lower alkyl, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.

Abstract translation: 公开了下式的化合物或其药学上可接受的无毒盐，其中：n是0-3的整数; C环是芳基或杂芳基; X是CH，N或OZ表示电子对，氢或（ 取代的杂环，芳基或酰氨基; W是（未）取代的烷基，芳基或杂芳基; A和B是氢或低级烷基，该化合物是GABAa脑受体或前药的高选择性激动剂，拮抗剂或反向激动剂 激动剂，拮抗剂或GA​​BAa脑受体的反向激动剂。 这些化合物可用于诊断和治疗焦虑症，唐氏综合征，睡眠，认知和癫痫发作，以及用苯二氮卓类药物过量并提高警觉性。

公开(公告)号：US06399604B1

公开(公告)日：2002-06-04

申请号：US09634093

申请日：2000-08-08

Applicant: Pamela A. Albaugh ,  Robert W. DeSimone ,  Gang Liu

Inventor： Pamela A. Albaugh ,  Robert W. DeSimone ,  Gang Liu

IPC: A61K31535

CPC classification number: C07D471/04

Abstract: The present invention encompasses structures of the Formula or the pharmaceutically acceptable non-toxic salts thereof wherein: X is hydrogen, halogen, (un)substituted alkyl, (un)substituted alkoxy or amino; and Y is (un)substituted alkyl, aryl, or heteroaryl, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.

Abstract translation: 本发明包括式的药学上可接受的无毒盐的结构，其中：X是氢，卤素，（未）取代的烷基，（未）取代的烷氧基或氨基; 和Y是（未）取代的烷基，芳基或杂芳基，该化合物是GABAa脑受体的高选择性激动剂，拮抗剂或反向激动剂或GABAa脑受体的激动剂，拮抗剂或反向激动剂的前药。 这些化合物可用于诊断和治疗焦虑症，唐氏综合征，睡眠，认知和癫痫发作，以及用苯二氮卓类药物过量并提高警觉性。

公开(公告)号：US6143760A

公开(公告)日：2000-11-07

申请号：US139456

申请日：1998-08-25

Applicant: Pamela A. Albaugh ,  Robert W. DeSimone ,  Gang Liu

Inventor： Pamela A. Albaugh ,  Robert W. DeSimone ,  Gang Liu

IPC: C07D471/04 ,  A61K31/44 ,  C07D471/02

CPC classification number: C07D471/04

Abstract: The present invention encompasses structures of the Formula ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: x is hydrogen, halogen, (un)substituted alkyl, (un)substituted alkoxy or amino; andY is (un)substituted alkyl, aryl, or heteroaryl,which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.

Abstract translation: 本发明包括式或其药学上可接受的无毒盐的结构，其中：x是氢，卤素，（未）取代的烷基，（未）取代的烷氧基或氨基; 并且Y是（未）取代的烷基，芳基或杂芳基，该化合物是GABAa脑受体的高度选择性激动剂，拮抗剂或反向激动剂或GABAa脑受体的激动剂，拮抗剂或反向激动剂的前药。 这些化合物可用于诊断和治疗焦虑症，唐氏综合征，睡眠，认知和癫痫发作，以及用苯二氮卓类药物过量并提高警觉性。

公开(公告)号：US06646124B2

公开(公告)日：2003-11-11

申请号：US10114743

申请日：2002-04-02

Applicant: Pamela A. Albaugh ,  Robert W. DeSimone ,  Gang Liu

Inventor： Pamela A. Albaugh ,  Robert W. DeSimone ,  Gang Liu

IPC: C07D41300

CPC classification number: C07D471/04

Abstract: The present invention encompasses structures of the Formula or the pharmaceutically acceptable non-toxic salts thereof wherein: X is hydrogen, halogen, (un)substituted alkyl, (un)substituted alkoxy or amino; and Y is (un)substituted alkyl, aryl, or heteroaryl, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.

Abstract translation: 本发明包括式的药学上可接受的无毒盐的结构，其中：X是氢，卤素，（未）取代的烷基，（未）取代的烷氧基或氨基; 和Y是（未）取代的烷基，芳基或杂芳基，该化合物是GABAa脑受体的高选择性激动剂，拮抗剂或反向激动剂或GABAa脑受体的激动剂，拮抗剂或反向激动剂的前药。 这些化合物可用于诊断和治疗焦虑症，唐氏综合征，睡眠，认知和癫痫发作，以及用苯二氮卓类药物过量并提高警觉性。

公开(公告)号：US06380209B1

公开(公告)日：2002-04-30

申请号：US09583147

申请日：2000-05-30

Applicant: Guolin Cai ,  Gang Liu

Inventor： Guolin Cai ,  Gang Liu

IPC: A61K314375

CPC classification number: C07D471/04 ,  C07D495/04

Abstract: Disclosed are compounds of the formula or the pharmaceutically acceptable non-toxic salts thereof wherein: R is hydrogen, alkyl, or(un)substituted alkoxy or amino; and W is (un)substituted alkyl, aryl, or heteroaryl, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. The compounds of the invention are useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.

Abstract translation: 公开了下式的化合物或其药学上可接受的无毒盐，其中：R是氢，烷基或（未）取代的烷氧基或氨基; 和W是（未取代的）取代的烷基，芳基或杂芳基，该化合物是GABAa脑受体的高度选择性激动剂，拮抗剂或反向激动剂或GABAa脑受体的激动剂，拮抗剂或反向激动剂的前药。 本发明的化合物可用于诊断和治疗焦虑症，唐氏综合征，睡眠，认知和发作障碍，以及用苯二氮卓类药物过量并提高警觉性。

公开(公告)号：US6103903A

公开(公告)日：2000-08-15

申请号：US259150

申请日：1999-02-26

Applicant: Guolin Cai ,  Gang Liu

Inventor： Guolin Cai ,  Gang Liu

IPC: A61P25/00 ,  C07D471/04 ,  C07D495/04 ,  C07D401/14 ,  C07D409/14

CPC classification number: C07D471/04 ,  C07D495/04

Abstract: Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: R is hydrogen, alkyl, or(un)substituted alkoxy or amino; andW is (un)substituted alkyl, aryl, or heteroaryl,which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. The compounds of the invention are useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.

Abstract translation: 公开了下式的化合物或其药学上可接受的无毒盐，其中：R是氢，烷基或（未）取代的烷氧基或氨基; W是（un）取代的烷基，芳基或杂芳基，该化合物是GABAa脑受体的高选择性激动剂，拮抗剂或反向激动剂或GABAa脑受体的激动剂，拮抗剂或反向激动剂的前药。 本发明的化合物可用于诊断和治疗焦虑症，唐氏综合征，睡眠，认知和发作障碍，以及用苯二氮卓类药物过量并提高警觉性。

公开(公告)号：US10914361B2

公开(公告)日：2021-02-09

申请号：US16201979

申请日：2018-11-27

Applicant: Gang Liu

Inventor： Gang Liu

IPC: F16H1/28 ,  F16H57/04 ,  F16H3/44 ,  F16H57/031 ,  F16H57/038

Abstract: Disclosed is a multi-gear torquer with end covers on both sides of the casing. An input shaft and an output shaft are respectively arranged at the center of the two end covers. A sun gear is fixed on the input shaft and moves along a planet gear engaged in the transmission mechanism. The planet gear meshes with a gear ring and moves around the sun gear, then the planet gear drives the turntable centrally fixed with the output shaft connected to the load end. The multi-gear torquer disclosed herein has the following advantages: large output torque and high mechanical efficiency, and it can be used as power transmission equipment for a car or a train and used as other mechanical transmission equipment.