Abstract: A process of manufacturing of (2S,5R)-5-(2-chlorophenyl)-1-(2?-methoxy-[1,1?-biphenyl]-4-carbonyl)pyrrolidine-2-carboxylic acid (1), including the preparation of (2S,5R)-methyl 5-(2-chlorophenyl)pyrrolidine-2-carboxylate hydrochloride (6·HCl) as an intermediate of synthesis: Also, the sodium salt of the (2S,5R)-5-(2-chlorophenyl)-1-(2?-methoxy-[1,1?-biphenyl]-4-carbonyl)pyrrolidine-2-carboxylic acid (1), and its use in a pharmaceutical composition including sodium the (2S,5R)-5-(2-chlorophenyl)-1-(2?-methoxy-[1,1?-biphenyl]-4-carbonyl)pyrrolidine-2-carboxylate and a method for treating and/or preventing inflammation in a patient.
Abstract: A process of manufacturing of (2S,5R)-5-(2-chlorophenyl)-1-(2?-methoxy-[1,1?-biphenyl]-4-carbonyl)pyrrolidine-2-carboxylic acid (1), including the preparation of (2S,5R)-methyl 5-(2-chlorophenyl)pyrrolidine-2-carboxylate hydrochloride (6·HCl) as an intermediate of synthesis: Also, the sodium salt of the (2S,5R)-5-(2-chlorophenyl)-1-(2?-methoxy-[1,1?-biphenyl]-4-carbonyl)pyrrolidine-2-carboxylic acid (1), and its use in a pharmaceutical composition including sodium the (2S,5R)-5-(2-chlorophenyl)-1-(2?-methoxy-[1,1?-biphenyl]-4-carbonyl)pyrrolidine-2-carboxylate and a method for treating and/or preventing inflammation in a patient.
Abstract: Compounds of formula (I), or the pharmaceutically acceptable salts and/or the solvates thereof, wherein m, n, R1, R2, R3, R4, R5, L, Ar1 and Ar2 are as defined as disclosed, which are useful as inhibitors of METTL3 (N6-adenosine-methlytransferase subunit) activity, in particular for the treatment of proliferative diseases such as cancers.
Abstract: Compounds of formula (I), or the pharmaceutically acceptable salts and/or the solvates thereof, wherein m, n, R1, R2, R3, R4, R5, L, Ar1 and Ar2 are as defined as disclosed, which are useful as inhibitors of METTL3 (N6-adenosine-methlytransferase subunit) activity, in particular for the treatment of proliferative diseases such as cancers.
Abstract: Crystalline form I and form II of (2S,5R)-5-(2-chlorophenyl)-1-(2?-methoxy-[1,1?-biphenyl]-4-carbonyl)pyrrolidine-2-carboxylic acid and preparation processes thereof. Also, a method for treating an inflammatory disease in a patient in need thereof, which includes administering to the patient a therapeutically effective amount of the crystalline form I or the crystalline form II of (2S,5R)-5-(2-chlorophenyl)-1-(2?-methoxy-[1,1?-biphenyl]-4-carbonyl) pyrrolidine-2-carboxylic acid.
Abstract: Compounds of formula (I), or the pharmaceutically acceptable salts and/or the solvates thereof, wherein m, n, R1, R2, R3, R4, R5, L, Ar1 and Ar2 are as defined as disclosed, which are useful as inhibitors of METTL3 (N6-adenosine-methlytransferase subunit) activity, in particular for the treatment of proliferative diseases such as cancers.
Abstract: Crystalline form I and form II of (2S,5R)-5-(2-chlorophenyl)-1-(2?-methoxy-[1,1?-biphenyl]-4-carbonyl)pyrrolidine-2-carboxylic acid and preparation processes thereof. Also, a method for treating an inflammatory disease in a patient in need thereof, which includes administering to the patient a therapeutically effective amount of the crystalline form I or the crystalline form II of (2S,5R)-5-(2-chlorophenyl)-1-(2?-methoxy-[1,1?-biphenyl]-4-carbonyl) pyrrolidine-2-carboxylic acid.
Abstract: Crystalline form I and form II of (2S,5R)-5-(2-chlorophenyl)-1-(T-methoxy-[1,1?-biphenyl]-4-carbonyl)pyrrolidine-2-carboxylic acid and preparation processes thereof. Also, a method for treating an inflammatory disease in a patient in need thereof, which includes administering to the patient a therapeutically effective amount of the crystalline form I or the crystalline form II of (2S,5R)-5-(2-chlorophenyl)-1-(2?-methoxy-[1,1?-biphenyl]-4-carbonyl) pyrrolidine-2-carboxylic acid.
Abstract: A process of manufacturing of (2S,5R)-5-(2-chlorophenyl)-1-(2?-methoxy-[1,1?-biphenyl]-4-carbonyl)pyrrolidine-2-carboxylic acid (1), including the preparation of (2S,5R)-methyl 5-(2-chlorophenyl)pyrrolidine-2-carboxylate hydrochloride (6·HCl) as an intermediate of synthesis: Also, the sodium salt of the (2S,5R)-5-(2-chlorophenyl)-1-(2?-methoxy-[1,1?-biphenyl]-4-carbonyl)pyrrolidine-2-carboxylic acid (1), and its use in a pharmaceutical composition including sodium the (2S,5R)-5-(2-chlorophenyl)-1-(2?-methoxy-[1,1?-biphenyl]-4-carbonyl)pyrrolidine-2-carboxylate and a method for treating and/or preventing inflammation in a patient.
Abstract: The present invention is directed to novel intermediates of the formula E: which are useful in the synthesis of agonists of g-protein coupled receptor 43 for treating and/or preventing metabolic diseases.
Type:
Grant
Filed:
June 18, 2019
Date of Patent:
March 3, 2020
Assignee:
Epics Therapeutics
Inventors:
Hamid R. Hoveyda, Didier Schils, Ludivine Zoute, Julien Parcq
Abstract: The present invention is directed to a process for the preparation of aryl-carbonyl-pyrrolidine carboxylic acid derivative compounds which are useful in treating metabolic diseases, said process consisting of coupling a pyrrolidine ester compound with an aryl carboxylic acid derivative, followed by alkaline or acidic treatment, hydrogenolysis or treatment with a fluoride of the obtained intermediate, to afford novel aryl-carbonyl-pyrrolidine carboxylic acid derivative compounds.
Type:
Grant
Filed:
June 20, 2018
Date of Patent:
July 23, 2019
Assignee:
Epics Therapeutics
Inventors:
Hamid R. Hoveyda, Didier Schils, Ludivine Zoute, Julien Parcq