Nuformix Limited

Nuformix Technologies Limited

Ucl Business Plc

Manoira Corporation

Conduit UK Management Ltd

Joanne Holland

Christopher Frampton

Daniel Gooding

Alan Chorlton

Alex Eberlin

Alex Peter Dyson

Cocrystals of a benzamide compound, specifically 3-{[5-(azetidine-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-{[(1S)-1-methyl-2-(methyloxy)ethyl]oxy}-N-(5-methylpyrazin-2-yl)benzamide, therapeutic uses of the benzamide cocrystals and pharmaceutical compositions containing them are disclosed. For purposes of this disclosure and for ease of understanding, 'benzamide' or “benzamide compound” as well as “AZD1656” refer to 3-{[5-(azetidine-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-{[(1S)-1-methyl-2-(methyloxy)ethyl]oxy}-N-(5-methylpyrazin-2-yl)benzamide. The benzamide cocrystals of the invention include a 1:1 benzamide fumaric acid (Cocrystal 1), a 1:1 benzamide maleic acid (Cocrystal 2), a 1:1 benzamide malonic acid (Cocrystal 3), a 1:1 benzamide L-tartaric acid hydrate (Cocrystal 4), and a 1:1 benzamide gentisic acid (Cocrystal 5), which includes a 1:1 benzamide gentisic acid form 1 (Cocrystal 5A), a 1:1 benzamide gentisic acid form 2 (Cocrystal 5B), a 1:1 benzamide gentisic acid form 3 (Cocrystal 5C), and a 1:1 benzamide gentisic acid form 4 (Cocrystal 5D).

Therapeutic cocrystals of 3-{[5-(azetidine-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-{[(1S)-1-methyl-2-(methyloxy)ethyl]oxy)-N-(5-methylpyrazin-2-yl)benzamide

The present invention relates to compositions comprising a cannabidolic acid cocrystal. In particular, the cannabidiolic acid cocrystals include a cannabidiolic acid L-phenylalanine cocrystal, a cannabidiolic acid vanillin cocrystal, a cannabidiolic acid betaine cocrystal, a cannabidiolic acid ethyl maltol cocrystal, a cannabidiolic acid L-proline cocrystal and a cannabidiolic acid D-proline cocrystal. The present invention also relates to compositions, particularly pharmaceutical compositions comprising a cannabidiolic acid cocrystal and a pharmaceutically acceptable carrier. The present invention further relates to methods to treat a disease, disorder or condition in a patient by administering to the patient a therapeutically effective amount of cannabidiolic acid cocrystal or a pharmaceutical composition comprising a therapeutically effective amount of cannabidiolic acid cocrystal.

Cannabidiolic acid cocrystals

The invention relates to crystalline tranilast salts. The crystalline tranilast salts, their preparation and their characterization are described and shown in the figures. The invention relates to pharmaceutical compositions containing a crystalline tranilast salt of the invention and a pharmaceutically acceptable carrier. The invention also relates to methods of treatment and the use of a therapeutically effective amount of a crystalline tranilast salt of the invention for treatment. The invention also relates to a method of preparing a liquid pharmaceutical composition comprising the step of dissolving a crystalline tranilast salt of the invention in a pharmaceutically acceptable solvent and to liquid pharmaceutical compositions prepared according to that method.

Crystalline tranilast salts and their pharmaceutical use

The invention relates to new 1:1 olaparib:hydroxybenzoic acid cocrystals. The invention also relates to new 2:1 olaparib:hydroxybenzoic acid cocrystals which may contain no water (anhydrous) or may optionally be hydrated. The invention also relates to pharmaceutical compositions containing an olaparib hydroxybenzoic acid cocrystal of the invention and a pharmaceutically acceptable carrier. The olaparib hydroxybenzoic acid cocrystals of the invention may be useful for the treatment of diseases that benefit from inhibition of poly (ADP-ribose) polymerase (PARP).

Olaparib hydroxybenzoic acid cocrystals and their pharmaceutical use

The invention relates to new olaparib oxalic acid cocrystals. The olaparib oxalic acid cocrystals vary in ratio from 1:1 to 2:3 olaparib:oxalic acid. In particular, the invention relates to a 2:3 olaparib oxalic acid cocrystal, a 1:1 olaparib oxalic acid cocrystal, and a 2:1 olaparib oxalic acid cocrystal. The invention also relates to pharmaceutical compositions containing an olaparib oxalic acid cocrystal of the invention and a pharmaceutically acceptable carrier. The olaparib oxalic acid cocrystals of the invention Got may be useful for the treatment of diseases that benefit from inhibition of poly (ADP-ribose) polymerase (PARP). These include cancer, fibrosis, inflammatory conditions (e.g. asthma, colitis, arthritis), neurological diseases (e.g. neurodegeneration, neurotrauma, stroke), cardiovascular conditions, ophthalmic degenerative diseases, vascular diseases (e.g. diabetic complications, atherosclerosis), and various forms of critical illness (e.g. septic shock, ALI, acute liver failure).

Olaparib oxalic acid cocrystals and their pharmaceutical use

The invention relates to a crystalline diethylamine tetrathiomolybdate salt (DEA-TTM). The invention also relates to methods for producing the crystalline DEA-TTM salt of the invention. The invention also relates to pharmaceutical compositions comprising the crystalline DEA-TTM salt of the invention. The invention also relates to the use of the crystalline DEA-TTM salt of the invention in the treatment of the human or animal body, in particular its use in treatment of a condition requiring reduced metabolism of an organ or the whole body of a patient, by administering to a patient in need thereof a therapeutically effective amount of the crystalline DEA-TTM salt.

Crystalline diethylamine tetrathiomolybdate and its pharmaceutical uses

New tranilast complexes and new tranilast cocrystals are disclosed. These include a 1:1 tranilast nicotinamide complex, a 1:1 tranilast nicotinamide cocrystal, a 1:1 tranilast saccharin complex, a 1:1 tranilast saccharin cocrystal, a 1:1 tranilast gentisic acid complex, a 1:1 tranilast gentisic acid cocrystal, a 1:1 tranilast salicylic acid complex, a 1:1 tranilast salicylic acid cocrystal, a 1:1 tranilast urea complex, a 1:1 tranilast urea cocrystal, a 1:1 tranilast 4-aminobenzoic acid complex, a 1:1 tranilast 4-aminobenzoic acid cocrystal, a 1:1 tranilast 2,4-dihydroxybenzoic acid complex and a 1:1 tranilast 2,4-dihydroxybenzoic acid cocrystal. Also disclosed are pharmaceutical compositions containing a tranilast complex or cocrystal of the invention and a pharmaceutically acceptable carrier. Methods of treatment using the tranilast complexes and cocrystals as well as the pharmaceutical compositions are disclosed.

Tranilast compositions and cocrystals

Aprepitant L-proline solvate compositions and aprepitant L-proline solvate cocrystals are disclosed as well as pharmaceutical compositions containing them. The compositions and cocrystals of the invention are: 1:1:1 aprepitant L-proline methanol composition; a 1:1:1 aprepitant L-proline methanol cocrystal; a 1:1:1:1 aprepitant L-proline ethanol composition; a 1:1:1 aprepitant L-proline ethanol cocrystal; 1 1:1:1 aprepitant L-proline n-propanol composition; and a 1:1:1 aprepitant L-proline n-propanol cocrystal: The aprepitant L-proline solvate compositions or cocrystals may be used in the same way as aprepitant to treat or prevent disorders relating to emesis, a neuropsychiatric disease, an inflammatory disease, pain, cancer, a skin disease, itch a respiratory disease, or an addiction.

Aprepitant L-proline solvates&#x2014;compositions and cocrystals

Mew tranilast complexes and new tranilast cocrystais are disclosed. These include all tranilast nicotinamide complex, a 1:1 tranilast nicotinamide cocrystal, a 1:1 tranilast saccharin complex, a 1:1 tranilast saccharin cocrystal, a 1:1 tranilast gentisic acid complex, a 1:1 tranilast gentisic acid cocrystal, a 1:1 tranilast salicylic acid complex, a 1:1 tranilast salicylic acid cocrystal, a 1:1 tranilast urea complex, a 1:1 tranilast urea cocrystal, a 1:1 tranilast 4-amtnoben2oic acid complex, a 1:1 tranilast 4-am!nobers2oic acid cocrystal, a 1:1 tranilast 2,4-di'hydroxybenzoic acid complex and a 1:1 tranilast 2,4-dihydroxybenzoic acid cocrystal. Also disclosed are pharmaceutical compositions containing a tranilast complex or cocrystal of the invention and a pharmaceutically acceptable carrier. Methods of treatment using the tranilast complexes and cocrystais as well as the pharmaceutical compositions are disclosed.

New rebamipide complexes and new rebamipide cocrystals are disclosed, specifically a 1:1 rebamipide nicotinamide complex, a 1:1 rebamipide nicotinamide cocrystal, a 1:1 rebamipide 2,4-dihydroxybenzolc acid complex, and a 1:1 rebamipide 2,4-dihydroxybenzoic acid cocrystal. Pharmaceutical compositions containing a rebamipide complex or cocrystal of the invention and a pharmaceutically acceptable carrier and methods of treatment are also disclosed. 

Rebamipide complexes and cocrystals

A 1:1:1 aprepitant L-proline HO composition and a 1:1:1 aprepitant L-proline HO cocrystal are disclosed as well as pharmaceutical compositions containing a 1:1:1 aprepitant L-proline HO composition or cocrystal and a pharmaceutically acceptable carrier. The 1:1:1 aprepitant L-proline HO composition or cocrystal may be used in the same way as aprepitant to treat or prevent disorders relating to emesis, a neuropsychiatric disease, an inflammatory disease, pairs, cancer, a skin disease, itch, a respiratory disease, or an addiction.

Aprepitant L-proline composition and cocrystal

The invention relates to improvements of the physiochemical and/or the pharmaceutical properties of metaxalone. Disclosed herein are several new cocrystals of metaxalone, including: a 1:1 metaxalone adipic acid cocrystal, a 1:0.5 metaxalone fumaric acid cocrystal, a 1:1 metaxalone salicyclic acid cocrystal, a 1:0.5 metaxalone succinic acid cocrystal, and a 1:0.5 metaxalone maleic acid cocrystal. The therapeutic uses of these metaxalone cocrystals are described as well as therapeutic compositions containing them.

Metaxalone cocrystals

The invention relates to improvements of the physiochemical and/or the pharmaceutical properties of cilostazol. Disclosed herein are several new compositions and cocrystals of cilostazol, including: a 1:1 cilostazol gentisic acid cocrystal, a 1:1:1 cilostazol gentisic acid HO cocrystal, a 1:1 cilostazol 4-hydroxybenzoic acid cocrystal, and a 1:1 cilostazol 2,4-dihydroxybenzoic acid cocrystal. The therapeutic methods and uses of these cilostazol cocrystals are described as well as therapeutic compositions containing them.

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Cambridge, United Kingdom

Joanne Holland