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US 11,376,250 B2Granted
Spiro-lactam NMDA receptor modulators and uses thereof
AssigneeAptinyx Inc.
InventorM. Amin Khan
Life of this patent
Estimating the term…
Abstract
Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
Claims20
A compound represented by:
- or a pharmaceutically acceptable salt and/or a stereoisomer thereof, wherein:
- X is O or NR2;
- R1 is selected from the group consisting of H, C1-C6alkyl, phenyl, —C(O)—C1-C6alkyl, and —C(O)—O—C1-C6 alkyl;
- R2 is selected from the group consisting of H, C1-C6alkyl, phenyl, —C(O)—C1-C6alkyl, and —C(O)—O—C1-C6 alkyl;
- p is 2;
- R5 is independently selected for each occurrence from the group consisting of H, C1-C6alkyl, —S(O)w—C1-C3alkyl, —NRaRb, C1-C3alkoxy, cyano and halogen;
- w is 0, 1, or 2;
- R3 is selected from the group consisting of H, C1-C6 alkyl, phenyl, —C(O)R31 and —C(O)OR32;
- R31 and R32 are each independently selected from the group consisting of H, C1-C6alkyl, —C3-C6cycloalkyl, and phenyl;
- and
- R7 is independently selected for each occurrence from the group consisting of H, halogen, and phenyl;
- and
- Ra and Rb are each independently for each occurrence selected from the group consisting of H, C1-C3alkyl, and phenyl, or Ra and Rb taken together with the nitrogen to which they are attached form a 4-6 membered heterocyclic ring;
- wherein any aforementioned C1-C6 alkyl, independently for each occurrence, is optionally substituted by one, two or three substituents each independently selected from —C(O)NRaRb, —NRaRb, hydroxyl, S(O)w—C1-C3alkyl, SH, phenyl and halogen, and any aforementioned phenyl, independently for each occurrence, is optionally substituted by one, two or three substituents each independently selected from hydroxyl, halogen, —C(O)—O—C1-C3alkyl, —C(O)—C1-C3alkyl, methyl, and CF3.
11 more elements
A compound selected from the group consisting of:
- or a pharmaceutically acceptable salt and/or a stereoisomer thereof.
A compound selected from the group consisting of
- or a pharmaceutically acceptable salt and/or a stereoisomer thereof.
Dependencies are inferred from the claim text.