Patent classifications
C07C57/58
Multiple-component solid phases containing at least one active pharmaceutical ingredient
The subject invention concerns a method for identifying complementary chemical functionalities to form a desired supramolecular synthon. The subject invention also pertains to binary phase compositions comprising one or more pharmaceutical entities and methods for producing such compositions.
SUBSTITUTED AROMATIC COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS FOR TISSUE SELF-REPAIR AND REGENERATION
Described herein are compounds of Formula I, or pharmaceutically acceptable salts thereof, or combinations thereof, as well as uses thereof. Such uses include promoting tissue self-repair or tissue regeneration of an organ, stimulating the generation of tissue growth, modulating (e.g., increasing) the level of a tissue-repair marker, treating physical injury in an organ, tissue or cell, promoting wound healing, as well as anti-aging applications. Corresponding compositions, methods, kits, and uses are also described. Formula I wherein A is C.sub.5 alkyl, C.sub.6 alkyl, C.sub.5 alkenyl, C.sub.6 alkenyl, C(0)-(CH.sub.2).sub.nCH.sub.3 or CH(OH)(CH.sub.2).sub.nCH.sub.3 wherein n is 3 or 4; R.sub.1 is H, F of OH; R.sub.2 is H, F, OH, C.sub.5 alkyl, C.sub.6 alkyl, C.sub.5 alkenyl, C.sub.6 alkenyl, C(0)-(CH.sub.2).sub.nCH.sub.3 or CH(OH)(CH.sub.2).sub.nCH.sub.3 wherein n is 3 or 4; R.sub.3 is H, F, OH, or CH.sub.2Ph; R.sub.4 is H, F or OH; Q is 1) (CH.sub.2),C(0)OH wherein m is 1 or 2 2) CH(CH.sub.3)C(0)OH, 3) C(CH.sub.3).sub.2C(0)OH, 4) CH(F)C(0)OH, 5) CF.sub.2-C(0)OH or 6) C(0)-C(0)OH.
SUBSTITUTED AROMATIC COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS FOR TISSUE SELF-REPAIR AND REGENERATION
Described herein are compounds of Formula I, or pharmaceutically acceptable salts thereof, or combinations thereof, as well as uses thereof. Such uses include promoting tissue self-repair or tissue regeneration of an organ, stimulating the generation of tissue growth, modulating (e.g., increasing) the level of a tissue-repair marker, treating physical injury in an organ, tissue or cell, promoting wound healing, as well as anti-aging applications. Corresponding compositions, methods, kits, and uses are also described. Formula I wherein A is C.sub.5 alkyl, C.sub.6 alkyl, C.sub.5 alkenyl, C.sub.6 alkenyl, C(0)-(CH.sub.2).sub.nCH.sub.3 or CH(OH)(CH.sub.2).sub.nCH.sub.3 wherein n is 3 or 4; R.sub.1 is H, F of OH; R.sub.2 is H, F, OH, C.sub.5 alkyl, C.sub.6 alkyl, C.sub.5 alkenyl, C.sub.6 alkenyl, C(0)-(CH.sub.2).sub.nCH.sub.3 or CH(OH)(CH.sub.2).sub.nCH.sub.3 wherein n is 3 or 4; R.sub.3 is H, F, OH, or CH.sub.2Ph; R.sub.4 is H, F or OH; Q is 1) (CH.sub.2),C(0)OH wherein m is 1 or 2 2) CH(CH.sub.3)C(0)OH, 3) C(CH.sub.3).sub.2C(0)OH, 4) CH(F)C(0)OH, 5) CF.sub.2-C(0)OH or 6) C(0)-C(0)OH.
Substituted aromatic compounds and related method for the treatment of fibrosis
The present invention relates to compounds of: ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein
A is C.sub.5 alkyl, C.sub.6 alkyl, C.sub.5 alkenyl, C.sub.6 alkenyl, C(O)(CH.sub.2).sub.nCH.sub.3 or CH(OH)(CH.sub.2).sub.nCH.sub.3 wherein n is 3 or 4;
R.sub.1 is H, F or OH;
R.sub.2 is C.sub.5 alkyl, C.sub.6 alkyl, C.sub.5 alkenyl, C.sub.6 alkenyl, C(O)(CH.sub.2).sub.nCH.sub.3 or CH(OH)(CH.sub.2).sub.nCH.sub.3 wherein n is 3 or 4;
R.sub.3 is H, F, OH or CH.sub.2Ph;
R.sub.4 is H, For OH;
Q is 1) (CH.sub.2).sub.mC(O)OH wherein m is 1 or 2, 2) CH(CH.sub.3)C(O)OH, 3) C(CH.sub.3).sub.2C(O)OH, 4) CH(F)C(O)OH, 5) CF.sub.2C(O)OH, or 6) C(O)C(O)OH;
and compositions comprising the same and the method using the same for the prevention or treatment of various fibrotic diseases and conditions in subjects, including pulmonary fibrosis, liver fibrosis, skin fibrosis, renal fibrosis, pancreas fibrosis, systemic sclerosis, cardiac fibrosis or macular degeneration.
Substituted aromatic compounds and related method for the treatment of fibrosis
The present invention relates to compounds of: ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein
A is C.sub.5 alkyl, C.sub.6 alkyl, C.sub.5 alkenyl, C.sub.6 alkenyl, C(O)(CH.sub.2).sub.nCH.sub.3 or CH(OH)(CH.sub.2).sub.nCH.sub.3 wherein n is 3 or 4;
R.sub.1 is H, F or OH;
R.sub.2 is C.sub.5 alkyl, C.sub.6 alkyl, C.sub.5 alkenyl, C.sub.6 alkenyl, C(O)(CH.sub.2).sub.nCH.sub.3 or CH(OH)(CH.sub.2).sub.nCH.sub.3 wherein n is 3 or 4;
R.sub.3 is H, F, OH or CH.sub.2Ph;
R.sub.4 is H, For OH;
Q is 1) (CH.sub.2).sub.mC(O)OH wherein m is 1 or 2, 2) CH(CH.sub.3)C(O)OH, 3) C(CH.sub.3).sub.2C(O)OH, 4) CH(F)C(O)OH, 5) CF.sub.2C(O)OH, or 6) C(O)C(O)OH;
and compositions comprising the same and the method using the same for the prevention or treatment of various fibrotic diseases and conditions in subjects, including pulmonary fibrosis, liver fibrosis, skin fibrosis, renal fibrosis, pancreas fibrosis, systemic sclerosis, cardiac fibrosis or macular degeneration.
SUBSTITUTED AROMATIC COMPOUNDS FOR THE TREATMENT OF PULMONARY FIBROSIS, LIVER FIBROSIS,SKIN FIBROSIS AND CARDIAC FIBROSIS
The present invention relates to substituted aromatic compounds for use in prevention or treatment of various fibrotic diseases and conditions in subjects, including pulmonary fibrosis, liver fibrosis, skin fibrosis and cardiac fibrosis, where the compound has the following formula:
##STR00001##
or a pharmaceutically acceptable salt thereof, wherein A is C.sub.5 alkyl, C.sub.6 alkyl, C.sub.5 alkenyl, C.sub.6 alkenyl, C(O)(CH.sub.2).sub.nCH.sub.3 or CH(OH)(CH.sub.2).sub.nCH.sub.3 wherein n is 3 or 4; R.sub.1 is H, OH or F; R.sub.2 is H, OH, F or CH.sub.2OH; R.sub.3 is H, OH, F or CH.sub.2Ph; R.sub.4 is H, OH or F; Q is 1) (CH.sub.2).sub.mC(O)OH wherein m is 1 or 2, 2) CH(CH.sub.3)C(O)OH, 3) C(CH.sub.3).sub.2C(O)OH, 4) CH(F)C(O)OH, 5) CF.sub.2C(O)OH, or 6) C(O)C(O)OH.
SUBSTITUTED AROMATIC COMPOUNDS FOR THE TREATMENT OF PULMONARY FIBROSIS, LIVER FIBROSIS,SKIN FIBROSIS AND CARDIAC FIBROSIS
The present invention relates to substituted aromatic compounds for use in prevention or treatment of various fibrotic diseases and conditions in subjects, including pulmonary fibrosis, liver fibrosis, skin fibrosis and cardiac fibrosis, where the compound has the following formula:
##STR00001##
or a pharmaceutically acceptable salt thereof, wherein A is C.sub.5 alkyl, C.sub.6 alkyl, C.sub.5 alkenyl, C.sub.6 alkenyl, C(O)(CH.sub.2).sub.nCH.sub.3 or CH(OH)(CH.sub.2).sub.nCH.sub.3 wherein n is 3 or 4; R.sub.1 is H, OH or F; R.sub.2 is H, OH, F or CH.sub.2OH; R.sub.3 is H, OH, F or CH.sub.2Ph; R.sub.4 is H, OH or F; Q is 1) (CH.sub.2).sub.mC(O)OH wherein m is 1 or 2, 2) CH(CH.sub.3)C(O)OH, 3) C(CH.sub.3).sub.2C(O)OH, 4) CH(F)C(O)OH, 5) CF.sub.2C(O)OH, or 6) C(O)C(O)OH.
LUMINESCENT NANOCRYSTAL COMPLEX
Object A problem to be solved by the present invention is to provide a luminescent nanocrystal complex that tends to disperse orderly in a polymer matrix and is superior in dispersibility in structurally mesogenic crosslinkable polymer matrices. Solution The present invention is a luminescent nanocrystal complex that contains luminescent nanocrystals and a surface-modifying compound that modifies the surface of the luminescent nanocrystals. The surface-modifying compound has a mesogenic backbone and a group that binds to the surface of the luminescent nanocrystals.
LUMINESCENT NANOCRYSTAL COMPLEX
Object A problem to be solved by the present invention is to provide a luminescent nanocrystal complex that tends to disperse orderly in a polymer matrix and is superior in dispersibility in structurally mesogenic crosslinkable polymer matrices. Solution The present invention is a luminescent nanocrystal complex that contains luminescent nanocrystals and a surface-modifying compound that modifies the surface of the luminescent nanocrystals. The surface-modifying compound has a mesogenic backbone and a group that binds to the surface of the luminescent nanocrystals.
A NOVEL PROCESS FOR THE SYNTHESIS OF 1-ARYL-1-TRIFLUOROMETHYLCYCLOPROPANES
The present invention relates to a process for the manufacturing of 1-aryl-1-trifluoromethylcyclopropanes, which serve as intermediates for the manufacturing of calcium T channel blockers of the general formula (A)
##STR00001##
which are described in WO 2015/186056.