Abstract: This invention relates to compounds that are agonists of the muscarinic M1 and/or M4 receptor and which are useful in the treatment of diseases mediated by the muscarinic M1 and M4 receptors. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where X1; X2; R1 and R4 are as defined herein.

Abstract: The disclosures herein relate to compounds of Formula (1?): or a salt thereof, wherein A, Q, X, Z, L, R2, R3 and R9 are defined herein, and their use in the treatment of SARS-CoV-2 and related viruses and disorders associated with SARS-CoV-2: Mpro.

Abstract: The invention relates to mutant G-protein coupled receptors with increased conformational stability, and methods of use thereof. In some aspects, polynucleotides encoding the mutant G-protein coupled receptors are provided. In some aspects, host cells comprising the polynucleotides are provided. In some aspects, the invention relates to crystallized forms of the mutant G-protein coupled receptors, and methods of preparing the same.

Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor or M1 and M4 receptors and which are useful in the treatment of muscarinic M1 or M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula wherein Q4, Q5, R5, p, V, Q1, Q2, X1, X2 and W are defined herein.

Abstract: The disclosures herein relate to novel compounds of formula (1): and salts thereof, wherein Q, X, AA1, AA2, AA3, AA4, AA5, AA6, AA7, AA8, AA9, AA10, AA11, AA12, AA13, R1 R2 and n are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with Apelin receptors.

Abstract: The disclosures herein relate to novel compounds of formula (1) and salts thereof, wherein Q, X, AA1, AA2, AA3, AA4, AA5, AA6, AA7, AA8, R1, R2 and n are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with apelin receptors.

Abstract: The disclosures herein relate to novel compounds of Formula (1): or a salt thereof, wherein Q, V, L, W, R1 and R2 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with GPR52 receptors.

Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula I, where n is 1 or 2; p is 0, 1 or 2; q is 0, 1 or 2; and R1-R6 are as defined herein.

Abstract: This invention relates to compounds that are agonists of the muscarinic M1 and/or M4 receptor and which are useful in the treatment of diseases mediated by the muscarinic M1 and M4 receptors. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where Y, R1, R2 and R4 are as defined herein.

Abstract: The disclosures herein relate to novel compounds of formula (1): and salts thereof, wherein Q, W, X, Y, Z, AA1, AA2, AA3, AA4, AA5, AA6, AA7, AA8, AA9, LysR, R 1, R2 and n are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with Glucagon-like peptide (GLP) receptors.

Abstract: The disclosures herein relate to novel internally cyclic peptide compounds of formula (1) and salts thereof, wherein R1, AA1, AA2, LysR, X and Y are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with Glucagon-like peptide-1 (GLP-1) receptors.

Abstract: The disclosures herein relate to novel compounds of formula wherein R1, R2, R3 and R4 and n are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of inflammation, neurological or psychiatric disorders associated with modulating mGlu5 receptor function.

Abstract: The invention relates to mutant G-protein coupled receptors with increased conformational stability, and methods of use thereof. In some aspects, polynucleotides encoding the mutant G-protein coupled receptors are provided. In some aspects, host cells comprising the polynucleotides are provided. In some aspects, the invention relates to crystallized forms of the mutant G-protein coupled receptors, and methods of preparing the same.

Abstract: The disclosure herein relates to azetidinylpyrimidin-2-amine derivatives, their use as Histamine H4 receptor antagonists and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with H4 receptors.

Abstract: The disclosures herein relate to novel compounds of formula wherein R1, R2, R3 and R4 and n are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of inflammation, neurological or psychiatric disorders associated with modulating mGlu5 receptor function.

Abstract: This invention relates to compounds that are agonists of the muscarinic M1 and/or M4 receptor and which are useful in the treatment of diseases mediated by the muscarinic M1 and M4 receptors. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula (1) wherein X1; X2; R1 and R4 are as defined herein.

Abstract: The invention provides a mutant of a parent heterotrimeric G protein alpha (G?) subunit, which mutant (i) lacks at least one helix of the helical domain of the parent G? subunit; (ii) is capable of binding to a GPCR in the absence of a heterotrimeric G protein beta (G?) subunit and a heterotrimeric G protein gamma (G?) subunit; and (iii) has an amino acid sequence that contains one or more mutations compared to the amino acid sequence of the parent heterotrimeric G? subunit, which mutations are selected from a deletion, a substitution and an insertion.

Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1a or a salt thereof, wherein n, p, Q, R1, R2, R3, R9 and R4 are as defined herein.

Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1 or a salt thereof, wherein q, r, s, Q, R1, R2?, R2?, R3 and R4 are as defined herein.

Abstract: The disclosures herein relate to novel compounds of formula (I): and salts thereof, wherein W; X; Y; Z; R1; R2; R3 and R4 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of neurological or psychiatric disorders associated with orexin receptors.