The present invention relates to guanidine compounds for inhibiting mitochondrial oxidative phosphorylation (OXPHOS) and use thereof. More specifically, the present invention relates to a pharmaceutical composition for preventing or treating a OXPHOS-related disease, particularly cancer, by inhibiting mitochondrial oxidative phosphorylation and reprogramming cellular metabolism.

Cannabigerol proline cocrystals are disclosed, specifically a 1:2 cannabigerol L-proline cocrystal, a 1:2 cannabigerol D-proline cocrystal and a 1:2 cannabigerol D, L-proline cocrystal and their preparation. Also disclosed are pharmaceutical compositions containing a cannabigerol proline cocrystal and a pharmaceutically acceptable excipient as well as methods and uses of a cannabigerol proline cocrystal or pharmaceutical composition to treat a disease, disorder or condition by administering to a patient in need thereof a therapeutically effective amount of a cannabigerol proline cocrystal or a pharmaceutical composition containing a cannabigerol proline cocrystal. Also disclosed are processes for the preparation of crystalline cannabigerol, Forms I, II and III.

Cannabigerol proline cocrystals are disclosed, specifically a 1:2 cannabigerol L-proline cocrystal, a 1:2 cannabigerol D-proline cocrystal and a 1:2 cannabigerol D, L-proline cocrystal and their preparation. Also disclosed are pharmaceutical compositions containing a cannabigerol proline cocrystal and a pharmaceutically acceptable excipient as well as methods and uses of a cannabigerol proline cocrystal or pharmaceutical composition to treat a disease, disorder or condition by administering to a patient in need thereof a therapeutically effective amount of a cannabigerol proline cocrystal or a pharmaceutical composition containing a cannabigerol proline cocrystal. Also disclosed are processes for the preparation of crystalline cannabigerol, Forms I, II and III.

The present disclosure discloses free form or base and salts of compound of formula (I). Said salts include adipate, benzenesulphonate, hydrobromide, fumarate, benzoate, methanesulfonate, L-malate, d-glyconate, sorbate, phosphate, sulfate, L-tartrate, p-methylbenzenesulphonate, citrate, hydrochloride, ethanesulfonate, 1-hydroxy-2-naphthoate, succinate, acetate, glutarate or L-pyroglutamate. The present disclosure also discloses the crystals of free form and above salts.

The present disclosure discloses free form or base and salts of compound of formula (I). Said salts include adipate, benzenesulphonate, hydrobromide, fumarate, benzoate, methanesulfonate, L-malate, d-glyconate, sorbate, phosphate, sulfate, L-tartrate, p-methylbenzenesulphonate, citrate, hydrochloride, ethanesulfonate, 1-hydroxy-2-naphthoate, succinate, acetate, glutarate or L-pyroglutamate. The present disclosure also discloses the crystals of free form and above salts.

Provided herein are compounds of formula (I′):

##STR00001##

or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, wherein Y.sup.2, Y.sup.3, L.sup.1, L.sup.2, X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5, Q.sup.1, R.sup.1, R.sup.2, R.sup.k, R.sup.m, and R.sup.n are as defined elsewhere herein. Also provided herein are methods of preparing compounds of formula (I′). Also provided herein are methods of inhibiting GYS1 and methods of treating a GYS1-mediated disease, disorder, or condition in an individual in need thereof.

Provided herein are compounds of formula (I′):

##STR00001##

or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, wherein Y.sup.2, Y.sup.3, L.sup.1, L.sup.2, X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5, Q.sup.1, R.sup.1, R.sup.2, R.sup.k, R.sup.m, and R.sup.n are as defined elsewhere herein. Also provided herein are methods of preparing compounds of formula (I′). Also provided herein are methods of inhibiting GYS1 and methods of treating a GYS1-mediated disease, disorder, or condition in an individual in need thereof.

The present inventors found cyclic peptide compounds that interact with Ras, and non-natural amino acids useful for the production of the cyclic peptide compounds. The inventors also found that the cyclic peptide compounds inhibit the binding between Ras and SOS. In addition, the inventors found specific non-natural amino acids contained in the cyclic peptide compounds and methods for production thereof.

The present invention provides novel sulphonamide inhibitors of cystathionin gamma synthase (CGS), their use as selective and non-selective herbicides, agricultural and non-agricultural herbicides, herbicides in integrated pest management, herbicides for gardening, clearing waste ground, clearing industrial or constructions sites, clearing railways and railway embankments, pesticide, fungicide, agricultural plant stimulant or antimicrobial agent. Also provided is a method for the control of undesired vegetation or clearing areas from the undesired vegetation comprising applying to the locus of said undesired vegetation, to the undesired plants or to a habitat thereof, a herbicidally effective amount of the compound of the present invention.

The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds and methods of making and using such compounds.