公开(公告)号：US20150018339A1

公开(公告)日：2015-01-15

申请号：US14187035

申请日：2014-02-21

申请人： THE UNIVERSITY OF MISSISSIPPI ,  I'UNIVERSITE CATHOLIQUE DE LOUVAIN ,  THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY

发明人： Christopher R. MCCURDY ,  Christophe Mesangeau ,  Bonnie Ann Avery ,  Ahmed Hassan Amin Abdelazeem ,  Frederick T. Chin ,  Jacques Henri Poupaert

IPC分类号： C07D277/68 ,  C07D413/06 ,  C07D417/06 ,  C07D265/36 ,  C07D491/107 ,  C07D401/06 ,  C07D235/26 ,  C07D209/08 ,  C07D263/58 ,  C07D413/12

CPC分类号： C07D277/68 ,  C07D209/08 ,  C07D209/10 ,  C07D209/48 ,  C07D235/26 ,  C07D263/58 ,  C07D265/36 ,  C07D277/70 ,  C07D279/16 ,  C07D295/13 ,  C07D401/06 ,  C07D403/06 ,  C07D405/04 ,  C07D413/06 ,  C07D413/12 ,  C07D417/06 ,  C07D491/107 ,  C07D491/12

摘要： Compounds having the general formula II, III, or IV wherein R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle or a radical of an optionally substituted cyclic or acyclic tertiary amine or isoindoline-1,3-dione: R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate, optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR. R groups can be either H, aryls, alkyls, or cycloalkyls; “n” can be 1 to 5 carbons in length and stereoisomers, functional analogs, and pharmaceutically acceptable salts thereof and wherein the moiety bridging R1 and N can be a substituted alkylene, optionally substituted alkenylene or optionally substituted alkynylene and where the alkylene group can include an inserted C3-C5 cycloalkyl group, aromatic, and hetercocyclic group; wherein X′ is halogen, or C1-C4 haloalyl; wherein the Rx is a C1-C5 straight chain or branched chain alkyl or a C1-C4 straight chain or branched chain haloalkyl.

摘要翻译： 具有通式II，III或IV的化合物，其中R 1可以是任选取代的C-4至C-7N-杂环的基团或任选取代的环状或无环叔胺或异吲哚啉-1,3- 二硫化物：R2,3,4,5,6可以各自独立地是以下部分的任何一种或组合，氰基，硝基，酰基，烷基，酰氨基，叠氮基，异硫氰酸酯，异氰酸酯，任选取代的苯胺基，卤素，醚，磺酰胺 ，硫代酰基，硝基，芳族，杂环，烯属，乙炔，氘或氚; Y可以是CH，CH 2，O，S，OCH 2，N-R，N-Ar，C-R，C-Ar; Z可以是H，O，S，S-R或NR。 R基团可以是H，芳基，烷基或环烷基; “n”可以是长度为1至5个碳原子，立体异构体，功能类似物和其药学上可接受的盐，并且其中桥接R 1和N的部分可以是取代的亚烷基，任选取代的亚烯基或任选取代的亚炔基，并且其中亚烷基可以包括 插入的C 3 -C 5环烷基，芳族和杂环基团; 其中X'是卤素，或C 1 -C 4卤代芳基; 其中Rx是C1-C5直链或支链烷基或C1-C4直链或支链卤代烷基。

公开(公告)号：US09724435B2

公开(公告)日：2017-08-08

申请号：US14196483

申请日：2014-03-04

申请人： The University of Mississippi ,  The Board of Trustees of the Leland Stanford Junior University

发明人： Christopher R. McCurdy ,  Christophe Mesangeau ,  Frederick T. Chin ,  Michelle L. James ,  Bin Shen ,  Sanjiv Gambhir ,  Sandip Biswal ,  Deepak Behera

IPC分类号： A61K31/428 ,  C07D209/48 ,  C07D235/26 ,  C07D263/58 ,  C07D277/68 ,  C07D403/06 ,  C07D405/04 ,  C07D413/06 ,  C07D413/12 ,  C07D417/06 ,  C07D491/107 ,  C07D491/20 ,  A61K51/04 ,  C07D265/36 ,  C07D209/08 ,  C07D209/10 ,  C07D277/70 ,  C07D279/16 ,  C07D295/13 ,  C07D277/74

CPC分类号： A61K51/0468 ,  A61K31/428 ,  A61K51/0453 ,  A61K51/0455 ,  A61K51/0459 ,  C07D209/08 ,  C07D209/10 ,  C07D209/48 ,  C07D235/26 ,  C07D263/58 ,  C07D265/36 ,  C07D277/68 ,  C07D277/70 ,  C07D277/74 ,  C07D279/16 ,  C07D295/13 ,  C07D403/06 ,  C07D405/04 ,  C07D413/06 ,  C07D413/12 ,  C07D417/06 ,  C07D491/107 ,  C07D491/20

摘要： A method for localizing and quantifying S1R role in nociceptive processing; for providing a guide to providing an analgesic therapy; of using an S1R selective ligand as a biomarker for pathphysiological study of memory deficits and cognitive disorders; or of detecting increased S1R density at the site of nerve injury arising from neuropathic pain comprising using as a probe at least one SR1 selective compound or radioligand of the general formula III′, or IV′:

公开(公告)号：US20140315919A1

公开(公告)日：2014-10-23

申请号：US14321100

申请日：2014-07-01

申请人： The University of Mississippi ,  I'Universite Catholique de Louvain

发明人： Christopher McCurdy ,  Christophe Mesangeau ,  Sanju Narayanan ,  Rae Reiko Matsumoto ,  Jacques Henri Poupaert

IPC分类号： C07D277/70 ,  C07D491/107 ,  C07D417/06

CPC分类号： C07D277/70 ,  A61K51/0455 ,  A61K51/0459 ,  A61K51/0468 ,  C07D235/26 ,  C07D263/58 ,  C07D277/68 ,  C07D401/06 ,  C07D413/06 ,  C07D413/12 ,  C07D417/06 ,  C07D491/10 ,  C07D491/107

摘要： A compound useful for treating subjects in need of therapy involving sigma receptors or for alleviation of affects resulting from drug abuse having the general formula I in which R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle such as, for example, radicals of optionally substituted piperidines, optionally substituted piperazines, optionally substituted tetrahydropyridines, optionally substituted azepanes, tertiary amines (cyclic or acyclic), isoindoline-1,3-dione, or optionally substituted tetrahydroisoquinolones (aromatically substituted): R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR. R groups can be either H, aryls, alkyls, or cycloalkyls; “n” can be 1 to 5 carbons in length and stereoisomers, functional analogs, and pharmaceutically acceptable salts thereof and wherein the moiety bridging R1 and N can be optionally substituted alkylene, optionally substituted alkenylene or optionally substituted alkynylene and where the alkylene group can include an inserted C3-C5 cycloalkyl group, aromatic and heterocyclic group.

摘要翻译： 可用于治疗需要治疗涉及σ受体的受试者或用于缓解由具有通式I的药物滥用引起的影响的化合物的化合物，其中R 1可以是任选取代的C-4至C-7N-杂环的基团， 任选取代的四氢吡啶，任选取代的氮杂环庚烷，叔胺（环状或非环状），异二氢吲哚-1,3-二酮或任选取代的四氢异喹诺酮（芳族取代的）：R2， 3,4,5,6可以各自独立地为下列部分中的任何一种或组合：氰基，硝基，酰基，烷基，酰氨基，叠氮基，异硫氰酸酯，异氰酸酯任选取代的苯胺基，卤素，醚，磺酰胺，硫代酰基，硝基，芳族 ，杂环，烯属，乙炔，氘或氚; Y可以是CH，CH 2，O，S，OCH 2，N-R，N-Ar，C-R，C-Ar; Z可以是H，O，S，S-R或NR。 R基团可以是H，芳基，烷基或环烷基; “n”可以是长度为1至5个碳原子，立体异构体，功能类似物和其药学上可接受的盐，其中桥接R 1和N的部分可以是任选取代的亚烷基，任选取代的亚烯基或任选取代的亚炔基，并且其中亚烷基可以包括 插入的C 3 -C 5环烷基，芳族和杂环基。