发明名称 Subunit selective NMDA receptor potentiators for the treatment of neurological conditions
摘要 Provided are compounds, pharmaceutical compositions and methods of treating or preventing disorders associated with NMDA receptor activity, including schizophrenia, Parkinson's disease, cognitive disorders, depression, neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds of the general Formulas A-J, and pharmaceutically acceptable salts, esters, prodrugs or derivatives thereof are disclosed.
申请公布号 US8822462(B2) 申请公布日期 2014.09.02
申请号 US201013146201 申请日期 2010.01.28
申请人 Emory University 发明人 Traynelis Stephen F.;Liotta Dennis C.;Santangelo Rose M.;Garnier Ethel C.
分类号 A61K31/535 主分类号 A61K31/535
代理机构 Emory Patent Group 代理人 Emory Patent Group ;Mason James C.
主权项 1. A compound having the following formula: wherein X is, independently, N or C bonded to H or a substituent, J, with the proviso that no more than one of X are N; Y is O; R1 and R2 are independently selected from H, alkyl, substituted alkyl, alkenyl, substituted alkenyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, and hydroxy, R1 and R2 can optionally join to form a C3-10 heterocyclic moiety, which heterocyclic moiety can optionally include a second heteroatom selected from O, S, and N, z is an integer from 0 to 3, and J is a non-hydrogen substituent selected from the group consisting of halo (—F, —Cl, —Br, —I), amino (NR1R2), OR1, SR1, —R1, —CF3, —CN, —C2R1, —SO2CH3, —C(═O)NR1R2—NR′C(═O)R1, —C(═O)R1, —C(═O)OR1, —(CH2)qOR1, —OC(═O)R1, —OC(═O)NR1R2, —NR1(C═Y)—NR1R2, —NR1(C═Y)—OH, —NR1(C═Y)—SH, sulfonyl, sulfinyl, phosphoryl, and azo, wherein a substituted alkyl, substituted alkenyl, substituted aryl, or substituted heteroaryl is alkyl, alkenyl, aryl, or heteroaryl substituted with one or more substituent, wherein a substituent is fluoro, chloro, bromo, iodo, hydroxy, heterocyclic, heteroaryl, carboxy, alkoxy, NH2, N(alkyl)2, NH(alkyl), alkoxycarbonyl, —N(H or alkyl)C(O)(H or alkyl), —N(H or alkyl)C(O)N(H or alkyl)2, —N(H or alkyl)C(O)O(H or alkyl), —OC(O)N(H or alkyl)2, —S(O)n—(H or alkyl), —C(O)—N(H or alkyl)2, cyano, alkenyl, cycloalkyl, acyl, hydroxyalkyl, heterocyclic, heteroaryl, aryl, aminoalkyl, oxo, carboxyalkyl, —C(O)—NH2, —C(O)—N(H)O(H or alkyl), —S(O)2—NH2, —S(O)n—N(H or alkyl)2 and/or —S(O)2—N(H or alkyl)2 wherein the dashed line is an optional double bond, and pharmaceutically acceptable salts, or esters thereof.
地址 Atlanta GA US