公开(公告)号：US10017536B2

公开(公告)日：2018-07-10

申请号：US15145901

申请日：2016-05-04

申请人： CARA THERAPEUTICS, INC.

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

IPC分类号： C07K5/10 ,  A61K38/00 ,  C07K5/107 ,  C07K5/103 ,  C07K5/117 ,  C07K7/06

CPC分类号： C07K5/1016 ,  A61K38/00 ,  C07K5/1005 ,  C07K5/1008 ,  C07K5/1024 ,  C07K7/06

摘要： 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: The compounds are useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions.

公开(公告)号：US20160376308A1

公开(公告)日：2016-12-29

申请号：US15145901

申请日：2016-05-04

申请人： CARA THERAPEUTICS, INC.

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

IPC分类号： C07K5/107 ,  C07K7/06

CPC分类号： C07K5/1016 ,  A61K38/00 ,  C07K5/1005 ,  C07K5/1008 ,  C07K5/1024 ,  C07K7/06

摘要： 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: The compounds are useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions.

摘要翻译： 该化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。

公开(公告)号：US20150150935A1

公开(公告)日：2015-06-04

申请号：US14403535

申请日：2013-06-05

申请人： CARA THERAPEUTICS, INC.

发明人： Derek T. Chalmers ,  James B. Jones ,  Robert H. Spencer

IPC分类号： A61K38/07 ,  A61K31/485 ,  A61K9/00 ,  A61K31/40

CPC分类号： A61K38/07 ,  A61K9/0019 ,  A61K9/0048 ,  A61K31/40 ,  A61K31/485

摘要： A method of treating of a mammalian subject suffering from an inflammatory disease or condition by administering a peripherally-restricted kappa opioid receptor agonist for reducing the inflammation is provided. The peripherally-restricted kappa opioid receptor agonist can include a peptide and the peptide can include D-amino acids. Administration of peripherally-restricted kappa opioid receptor agonists results in lowering of serum levels of pro-inflammatory cytokines and elevation of levels of anti-inflammatory cytokines.

摘要翻译： 提供了通过施用用于减少炎症的外周限制性κ阿片受体激动剂来治疗患有炎性疾病或病症的哺乳动物受试者的方法。 外周受限制的κ阿片受体激动剂可以包括肽，肽可以包括D-氨基酸。 外周限制性κ阿片受体激动剂的施用导致促炎细胞因子的血清水平降低和抗炎细胞因子水平的升高。

公开(公告)号：US20110144121A1

公开(公告)日：2011-06-16

申请号：US12816657

申请日：2010-06-16

申请人： Robert Zhiyong Luo

发明人： Robert Zhiyong Luo

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

CPC分类号： C07D471/04 ,  C07D231/56 ,  C07D401/04 ,  C07D413/12 ,  C07D417/04 ,  C07D491/052

摘要： 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.

摘要翻译： 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：US07960376B2

公开(公告)日：2011-06-14

申请号：US12207601

申请日：2008-09-10

申请人： Jason S. Newcom ,  Carla M. Gauss ,  Gary R. Gustafson

发明人： Jason S. Newcom ,  Carla M. Gauss ,  Gary R. Gustafson

IPC分类号： C07D279/16 ,  A61K31/5415

CPC分类号： C07D279/16 ,  C07D265/36 ,  C07D281/10 ,  C07D417/04 ,  C07D417/14

摘要： The present invention provides benzo-fused heterocyclic compounds having the structure of formula I, as well as prodrugs, stereoisomers, racemates, salts, hydrates, solvates, acid salt hydrates and isomorphic crystalline forms thereof. The compounds directly or indirectly modulate the activity of one or more cannabinoid receptors and can be incorporated into pharmaceutical preparations that are useful for the prevention and treatment of a variety of diseases and conditions, including pain, inflammation and pruritis.

摘要翻译： 本发明提供具有式I结构的苯并稠合杂环化合物，以及其前体药物，立体异构体，外消旋物，盐，水合物，溶剂化物，酸盐水合物和同构晶体形式。 化合物直接或间接调节一种或多种大麻素受体的活性，并且可以掺入可用于预防和治疗各种疾病和病症（包括疼痛，炎症和瘙痒）的药物制剂中。

公开(公告)号：US07713937B2

公开(公告)日：2010-05-11

申请号：US12119311

申请日：2008-05-12

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

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

IPC分类号： A61K38/07

CPC分类号： C07K5/1016 ,  C07K7/02

摘要： 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.

摘要翻译： 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

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

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

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

CPC分类号： C07K5/1016 ,  C07K7/02

摘要： 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.

摘要翻译： 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

申请人： 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

发明人： 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分类号： A61K31/4985 ,  C07D487/04 ,  A61K31/5377 ,  A61P25/00 ,  A61K31/551

CPC分类号： C07D487/04

摘要： 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.

摘要翻译： 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

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

发明人： 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分类号： A61K31/519 ,  C07D487/04 ,  A61P25/02

CPC分类号： C07D487/04

摘要： 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.

摘要翻译： 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：US07504538B2

公开(公告)日：2009-03-17

申请号：US10575976

申请日：2004-10-14

申请人： Chia-Ping Chang ,  Jacek Stalewski ,  Piere J-M. Riviere ,  Kazimierz A. Wisniewski ,  Claudio D. Schteingart

发明人： Chia-Ping Chang ,  Jacek Stalewski ,  Piere J-M. Riviere ,  Kazimierz A. Wisniewski ,  Claudio D. Schteingart

IPC分类号： C07C275/00

CPC分类号： C07C275/28 ,  C07C237/22 ,  C07C2601/08 ,  C07C2601/14

摘要： The present invention relates to novel compounds, pharmaceutical compositions comprising the same, use of said compounds for the manufacture of a medicament for treatment of pain and disorders related thereto as well as a method for treatment of pain and disorders related thereto, wherein said compounds are administered. The compounds are represented by the general formula (I), as further defined in the specification.

摘要翻译： 本发明涉及新化合物，包含其的药物组合物，所述化合物在制备用于治疗与其相关的疼痛和病症的药物中的用途以及治疗与之有关的疼痛和病症的方法，其中所述化合物为 管理。 化合物由通式（I）表示，如说明书中进一步定义的。