| 摘要 |
Disclosed are compounds having enhanced potency in the modulation of NMD A receptor activity. Such compounds are contemplated for use in the treatment of diseases and disorders, such as learning, cognitive activities, and analgesia, particularly in alleviating and/or reducing neuropathic pain. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed. |
| 主权项 |
1. A peptidyl compound of the formula:wherein:
R1 and R2 are independently selected from the group consisting of hydrogen; halogen; cyclic or acyclic, substituted or unsubstituted, branched or unbranched aliphatic; cyclic or acyclic, substituted or unsubstituted, branched or unbranched heteroaliphatic; substituted or unsubstituted aryl; substituted or unsubstituted heteroaryl; —ORx; —NO2; —N3; —CN; —SCN; —SRx; —C(O)Rx; —CO2(Rx); —C(O)N(Rx)2; —C(NRx)N(Rx)2; —OC(O)Rx; —OCO2Rx; —OC(O)N(Rx)2; —N(Rx)2; —SORx; —S(O)2Rx; —NRxC(O)Rx; —NRxC(O)N(Rx)2; —NRxC(O)ORx; —NRxC(NRx)N(Rx)2; and —C(Rx)3; wherein each occurrence of Rx is independently selected from the group consisting of hydrogen; halogen; acyl; optionally substituted aliphatic; optionally substituted heteroaliphatic; optionally substituted aryl; and optionally substituted heteroaryl; R5 and R6 are independently selected from the group consisting of -Q-Ar and hydrogen; wherein Q is independently selected from the group consisting of cyclic or acyclic, substituted or unsubstituted, branched or unbranched aliphatic; cyclic or acyclic, substituted or unsubstituted, branched or unbranched heteroaliphatic; and a bond; and wherein Ar is selected from the group consisting substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; or R5 and R6, together with the atoms to which they are attached, form a substituted or unsubstituted 4-6 membered heterocyclic or cycloalkyl ring; R7 and R8 are independently selected from the group consisting of hydrogen; halogen; hydroxyl; substituted or unsubstituted C1-C6 alkyl; substituted or unsubstituted C1-C6 alkoxy; and substituted or unsubstituted aryl; or R7 and R8, together with the atoms to which they are attached, form a substituted or unsubstituted 4-6 membered heterocyclic or cycloalkyl ring; R16 and R17 are independently selected from the group consisting of hydrogen; C1-C6 alkyl, optionally substituted by one or more substituents each independently selected from the group consisting of halogen, oxo, and hydroxyl; C2-6alkenyl, optionally substituted by one or more substituents each independently selected from the group consisting of halogen, oxo, and hydroxyl; C2-6alkynyl, optionally substituted by one or more substituents each independently selected from the group consisting of halogen, oxo, and hydroxyl; C3-6cycloalkyl, optionally substituted by one or more substituents each independently selected from the group consisting of C1-6alkyl, halogen, oxo, and hydroxyl; phenyl, optionally substituted by one or more substituents each independently selected from the group consisting of C1-6alkyl, C1-6alkoxy; halogen, and hydroxyl; —C(O)Rx; —CO2(Rx); —C(O)N(Rx)2; —C(NRx)N(Rx)2; and —C(Rx)3; wherein each occurrence of Rx is independently selected from the group consisting of hydrogen; halogen; C1-6alkyl; C2-6alkenyl; C2-6alkynyl; C3-6cycloalkyl; and phenyl; or R16 and R17, together with N, form a 4-6 membered heterocyclic ring, optionally substituted by one or more substituents each independently selected from the group consisting of C1-6alkyl, halogen, oxo, and hydroxyl; L is selected from the group consisting of cyclic or acyclic, substituted or unsubstituted, branched or unbranched aliphatic; cyclic or acyclic, substituted or unsubstituted, branched or unbranched heteroaliphatic; substituted or unsubstituted aryl; and substituted or unsubstituted heteroaryl; andpharmaceutically acceptable salts, stereoisomers, metabolites, and hydrates thereof. |
