公开(公告)号：US20090264373A1

公开(公告)日：2009-10-22

申请号：US11938776

申请日：2007-11-12

Applicant: Claudio D. Schteingart ,  Frederique Menzaghi ,  Guangcheng Jiang ,  Roberta Vezza Alexander ,  Javier Sueiras-Diaz ,  Robert H. Spencer ,  Derek T. Chalmers ,  Zhiyong Luo

Inventor： Claudio D. Schteingart ,  Frederique Menzaghi ,  Guangcheng Jiang ,  Roberta Vezza Alexander ,  Javier Sueiras-Diaz ,  Robert H. Spencer ,  Derek T. Chalmers ,  Zhiyong Luo

IPC: A61K38/07 ,  C07K7/00

CPC classification number: C07K5/1016 ,  A61K38/00 ,  C07K5/1005 ,  C07K5/1008 ,  C07K5/1024 ,  C07K7/06

Abstract: The invention relates to synthetic peptide amide ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P450 CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure: Pharmaceutical compositions containing these compounds are useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions. Such treatable pain includes visceral pain, neuropathic pain and hyperalgesia. Inflammation associated with conditions such as IBD and IBS, ocular and otic inflammation, other disorders and conditions such as pruritis, edema, hyponatremia, hypokalemia, ileus, tussis and glaucoma are treatable or preventable with the pharmaceutical compositions of the invention.

Abstract translation: 本发明涉及κ阿片样物质受体的合成肽酰胺配体，特别是涉及低P450 CYP抑制和低渗透入脑的κ阿片受体激动剂。 本发明的合成肽酰胺符合以下结构：含有这些化合物的药物组合物可用于预防和治疗与各种疾病和病症相关的疼痛和炎症。 这种可治疗的疼痛包括内脏痛，神经性疼痛和痛觉过敏。 与IBD和IBS等条件相关的炎症，眼部和耳部炎症，其他疾病和病症如瘙痒症，水肿，低钠血症，低钾血症，肠梗阻，肠炎和青光眼均可用本发明的药物组合物治疗或预防。

公开(公告)号：US06825043B1

公开(公告)日：2004-11-30

申请号：US09565087

申请日：2000-05-05

Applicant: Dennis P. Curran ,  Roger Read ,  Zhiyong Luo

Inventor： Dennis P. Curran ,  Roger Read ,  Zhiyong Luo

IPC: G01N3700

CPC classification number: C07D213/40 ,  C07C69/96 ,  C07C237/22 ,  C07C237/42 ,  C07C255/62 ,  C07D207/14 ,  C07D207/16 ,  C07D211/62 ,  C07D217/06 ,  C07D401/06 ,  C07D405/06 ,  Y10T436/13 ,  Y10T436/19

Abstract: A method of increasing the fluorous nature of a compound includes the step of reacting the compound with at least one second compound having the formula: wherein Rf is a fluorous group, Rs is a spacer group, d is 1 or 0, m is 1, 2 or 3, Ra is an alkyl group and X is a suitable leaving group. A compound has the formula: wherein Rf is a fluorous group, n is an integer between 0 and 6, m is 1, 2 or 3, Ra is an alkyl group and X is a leaving group.

Abstract translation: 增加化合物的氟性质的方法包括使化合物与至少一种具有下式的第二化合物反应的步骤：其中Rf是氟基，Rs是间隔基，d是1或0，m是1， 2或3，Ra是烷基，X是合适的离去基团。 化合物具有下式：其中Rf是氟基，n是0和6之间的整数，m是1,2或3，Ra是烷基，X是离去基团。

公开(公告)号：US09537390B2

公开(公告)日：2017-01-03

申请号：US14378751

申请日：2012-03-07

Applicant: Jingwen Mao ,  Zhiyong Luo ,  Kaihua Zheng

Inventor： Jingwen Mao ,  Zhiyong Luo ,  Kaihua Zheng

IPC: H02J3/12 ,  G05F1/00 ,  H02M3/04 ,  H02M3/157 ,  H02M1/08 ,  H02M3/158 ,  H02M1/00

CPC classification number: H02M3/04 ,  H02M1/08 ,  H02M3/157 ,  H02M3/1588 ,  H02M2001/0003 ,  Y02B70/1466

Abstract: A control circuit (115), a control method, a DC-DC converter and an electronic device are provided. The control circuit (115) is used to control the DC-DC converter to switch its operation modes. In the control circuit (115), whether mode of the DC-DC converter is to be switched is judged according to parameters of a first duration of an active duration and a second duration of an inactive duration. Comparison of analog values is prevented, and as a result, the use of the analog comparator is reduced, thus the influence of the semiconductor processes on designing a controller can be reduced.

Abstract translation: 提供控制电路（115），控制方法，DC-DC转换器和电子设备。 控制电路（115）用于控制DC-DC转换器切换其工作模式。 在控制电路（115）中，根据活动持续时间的第一持续时间和非活动持续时间的第二持续时间的参数来判断是否要切换DC-DC转换器的模式。 可以防止模拟值的比较，结果减少了模拟比较器的使用，从而可以降低半导体工艺对设计控制器的影响。

公开(公告)号：US20110144121A1

公开(公告)日：2011-06-16

申请号：US12816657

申请日：2010-06-16

Applicant: Robert Zhiyong Luo

Inventor： Robert Zhiyong Luo

IPC: A61K31/497 ,  C07D231/00 ,  C07D401/14 ,  C07D471/04 ,  A61K31/4162 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/437 ,  A61P25/00

CPC classification number: C07D471/04 ,  C07D231/56 ,  C07D401/04 ,  C07D413/12 ,  C07D417/04 ,  C07D491/052

Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.

Abstract translation: 本发明提供了具有式I的通式结构的取代的吡唑并 - 杂环。还提供式I化合物的药学上可接受的盐，酸式盐，水合物，溶剂化物和立体异构体。该化合物可用作大麻素受体的调节剂和预防 以及治疗大麻素受体相关疾病和病症，如疼痛，炎症和瘙痒。

公开(公告)号：US07713937B2

公开(公告)日：2010-05-11

申请号：US12119311

申请日：2008-05-12

Applicant: Claudio D. Schteingart ,  Frédérique Menzaghi ,  Guangcheng Jiang ,  Roberta Vezza Alexander ,  Javier Sueiras-Diaz ,  Robert H. Spencer ,  Derek T. Chalmers ,  Zhiyong Luo

Inventor： Claudio D. Schteingart ,  Frédérique Menzaghi ,  Guangcheng Jiang ,  Roberta Vezza Alexander ,  Javier Sueiras-Diaz ,  Robert H. Spencer ,  Derek T. Chalmers ,  Zhiyong Luo

IPC: A61K38/07

CPC classification number: C07K5/1016 ,  C07K7/02

Abstract: The invention relates to synthetic peptide amides that are ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P450 CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure: wherein Xaa is a D-amino acid and G is selected from the following three groups: The compounds are useful in the prophylaxis and treatment of pain, pruritis and inflammation associated with a variety of diseases and conditions.

Abstract translation: 本发明涉及作为κ阿片受体的配体的合成肽酰胺，特别是涉及低P450 CYP抑制和低渗透入脑的κ阿片样物质受体的激动剂。 本发明的合成肽酰胺符合以下结构：其中Xaa是D-氨基酸，G选自以下三组：所述化合物可用于预防和治疗与各种各样的相关的疼痛，瘙痒和炎症 疾病和病症。

公开(公告)号：US20090156508A1

公开(公告)日：2009-06-18

申请号：US12119311

申请日：2008-05-12

Applicant: Claudio D. Schteingart ,  Frederique Menzaghi ,  Guangcheng Jiang ,  Roberta Vezza Alexander ,  Javier Sueiras-Diaz ,  Robert H. Spencer ,  Derek T. Chalmers ,  Zhiyong Luo

Inventor： Claudio D. Schteingart ,  Frederique Menzaghi ,  Guangcheng Jiang ,  Roberta Vezza Alexander ,  Javier Sueiras-Diaz ,  Robert H. Spencer ,  Derek T. Chalmers ,  Zhiyong Luo

IPC: A61K38/00 ,  C07K7/06 ,  A61K38/07 ,  C07K5/10

CPC classification number: C07K5/1016 ,  C07K7/02

Abstract: The invention relates to synthetic peptide amides that are ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P450 CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure: wherein Xaa is a D-amino acid and G is selected from the following three groups: The compounds are useful in the prophylaxis and treatment of pain, pruritis and inflammation associated with a variety of diseases and conditions.

Abstract translation: 本发明涉及作为κ阿片受体的配体的合成肽酰胺，特别是涉及低P450 CYP抑制和低渗透入脑的κ阿片样物质受体的激动剂。 本发明的合成肽酰胺符合以下结构：其中Xaa是D-氨基酸，G选自以下三组：所述化合物可用于预防和治疗与各种各样的相关的疼痛，瘙痒和炎症 疾病和病症。

公开(公告)号：US20090149450A1

公开(公告)日：2009-06-11

申请号：US12337683

申请日：2008-12-18

Applicant: R. Paul Beckett ,  Richard Foster ,  Christelle Henault ,  Janet L. Ralbovsky ,  Carla M. Gauss ,  Gary R. Gustafson ,  Robert Zhiyong Luo ,  Ann-Marie Campbell ,  Tatiana E. Shelekhin ,  Mary-Margaret E. Zablocki

Inventor： R. Paul Beckett ,  Richard Foster ,  Christelle Henault ,  Janet L. Ralbovsky ,  Carla M. Gauss ,  Gary R. Gustafson ,  Robert Zhiyong Luo ,  Ann-Marie Campbell ,  Tatiana E. Shelekhin ,  Mary-Margaret E. Zablocki

IPC: A61K31/4985 ,  C07D487/04 ,  A61K31/5377 ,  A61P25/00 ,  A61K31/551

CPC classification number: C07D487/04

Abstract: The present invention provides substituted imidazoheterocyclic compounds having the structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.

Abstract translation: 本发明提供了具有式I结构的取代的咪唑并杂环化合物。还提供式I化合物的药学上可接受的盐，酸式盐，水合物，溶剂合物和立体异构体。该化合物可用作大麻素受体的调节剂和预防和治疗 的大麻素受体相关疾病和病症，如疼痛，炎症和瘙痒。

公开(公告)号：US07517874B2

公开(公告)日：2009-04-14

申请号：US12142846

申请日：2008-06-20

Applicant: R. Paul Beckett ,  Richard Foster ,  Christelle Henault ,  Janet L. Ralbovsky ,  Carla M. Gauss ,  Gary G. Gustafson ,  Zhiyong Luo ,  Ann-Marie Campbell ,  Tatiana E. Shelekhin

Inventor： R. Paul Beckett ,  Richard Foster ,  Christelle Henault ,  Janet L. Ralbovsky ,  Carla M. Gauss ,  Gary G. Gustafson ,  Zhiyong Luo ,  Ann-Marie Campbell ,  Tatiana E. Shelekhin

IPC: A61K31/519 ,  C07D487/04 ,  A61P25/02

CPC classification number: C07D487/04

Abstract: The present invention provides substituted imidazoheterocyclic compounds having the structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.

Abstract translation: 本发明提供了具有式I结构的取代的咪唑并杂环化合物。还提供式I化合物的药学上可接受的盐，酸式盐，水合物，溶剂合物和立体异构体。该化合物可用作大麻素受体的调节剂和预防和治疗 的大麻素受体相关疾病和病症，如疼痛，炎症和瘙痒。

公开(公告)号：US20080194589A1

公开(公告)日：2008-08-14

申请号：US11576957

申请日：2005-10-19

Applicant: Marion Lanier ,  Zhiyong Luo ,  Manisha Moorjani ,  John Edward Tellew ,  John P. Williams ,  Xiaohu Zhang

Inventor： Marion Lanier ,  Zhiyong Luo ,  Manisha Moorjani ,  John Edward Tellew ,  John P. Williams ,  Xiaohu Zhang

IPC: A61K31/519 ,  C07D487/04 ,  A61P25/00 ,  A61P1/00

CPC classification number: C07D487/04

Abstract: CRF receptor antagonists are disclosed which may have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in mammals. The CRF receptor antagonists of this invention have the following structure: (I); and pharmaceutically acceptable salts, esters, solvates, stereoisomers and prodrugs thereof, wherein R1, R2a, R2b, Y, Het, n, o, R6, Ar and R7 are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same.

Abstract translation: 公开了CRF受体拮抗剂，其可用于治疗多种疾病，包括治疗在哺乳动物中表现出CRF过度分泌的病症。 本发明的CRF受体拮抗剂具有以下结构：（I）; 和其药学上可接受的盐，酯，溶剂合物，立体异构体和前药，其中R 1，R 2a，R 2b，Y，Het，n ，o，R 6，Ar和R 7如本文所定义。 还公开了含有CRF受体拮抗剂与药学上可接受的载体的组合物，以及其用途的方法。

公开(公告)号：US20070287705A1

公开(公告)日：2007-12-13

申请号：US10596648

申请日：2004-12-20

Applicant: Zhiyong Luo ,  Deborah Slee ,  John Tellew ,  John Willaims ,  Xiaohu Zhang

Inventor： Zhiyong Luo ,  Deborah Slee ,  John Tellew ,  John Willaims ,  Xiaohu Zhang

IPC: A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61P1/00 ,  A61P25/00 ,  A61P25/22 ,  A61P25/24 ,  A61P3/04 ,  C07D487/04

CPC classification number: C07D487/04

Abstract: CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure (I), including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, Y, Ar, and het are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same.

Abstract translation: 公开了CRF受体拮抗剂，其可用于治疗多种疾病，包括治疗在温血动物（例如中风）中表现出CRF分泌过高的病症。 本发明的CRF受体拮抗剂具有以下结构（I），其包括其立体异构体，前药和药学上可接受的盐，其中R1，R2，R3，Y，Ar和het如本文所定义。 还公开了含有CRF受体拮抗剂与药学上可接受的载体的组合物，以及其用途的方法。