Patent classifications
C07C59/52
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.n—CH.sub.3 or CH(OH)—(CH.sub.2).sub.n—CH.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.n—CH.sub.3 or CH(OH)—(CH.sub.2).sub.n—CH.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).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.2—C(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.n—CH.sub.3 or CH(OH)—(CH.sub.2).sub.n—CH.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.n—CH.sub.3 or CH(OH)—(CH.sub.2).sub.n—CH.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).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.2—C(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.
Pharmaceutical salts/co-crystals of pentoxifylline, clonidine and linsidomine with caffeic, protocatechuic or alpha-lipoic acid an use thereof for treatment of pain
Disclosed are pharmaceutical salts and co-crystals of pentoxifylline, clonidine and linsidomine with caffeic acid, protocatechuic acid or α-lipoic acid, and method for preparing thereof. Also disclosed are topical compositions comprising said salts or co-crystals and use thereof for treating pain.
Polymeric biomaterials derived from phenolic monomers and their medical uses
The present invention provides new classes of phenol compounds, including those derived from tyrosol and analogues, useful as monomers for preparation of biocompatible polymers, and biocompatible polymers prepared from these monomeric phenol compounds, including novel biodegradable and/or bioresorbable polymers. These biocompatible polymers or polymer compositions with enhanced bioresorbabilty and processibility are useful in a variety of medical applications, such as in medical devices and controlled-release therapeutic formulations. The invention also provides methods for preparing these monomeric phenol compounds and biocompatible polymers.
Polymeric biomaterials derived from phenolic monomers and their medical uses
The present invention provides new classes of phenol compounds, including those derived from tyrosol and analogues, useful as monomers for preparation of biocompatible polymers, and biocompatible polymers prepared from these monomeric phenol compounds, including novel biodegradable and/or bioresorbable polymers. These biocompatible polymers or polymer compositions with enhanced bioresorbabilty and processibility are useful in a variety of medical applications, such as in medical devices and controlled-release therapeutic formulations. The invention also provides methods for preparing these monomeric phenol compounds and biocompatible polymers.
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 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(O)—(CH.sub.2).sub.n—CH.sub.3 or CH(OH)—(CH.sub.2).sub.n—CH.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(O)—(CH.sub.2).sub.n—CH.sub.3 or CH(OH)—(CH.sub.2).sub.n—CH.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(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.2—C(O)OH or 6) C(O)—C(O)OH.
##STR00001##
EXTRACTION OF NATURAL FERULATE AND COUMARATE FROM BIOMASS
A process for a reactive separation of organic molecules from biomass includes a reaction step for the biomass, a simultaneous extraction step using a solvent, and a filtration step to recover products, wherein the products comprise ferulic acid and/or coumaric acid. The products are extracted from the biomass in a pressurized stirred batch reactor using a liquid extraction solvent and a base in which the ferulate and the coumarate remain.
EXTRACTION OF NATURAL FERULATE AND COUMARATE FROM BIOMASS
A process for a reactive separation of organic molecules from biomass includes a reaction step for the biomass, a simultaneous extraction step using a solvent, and a filtration step to recover products, wherein the products comprise ferulic acid and/or coumaric acid. The products are extracted from the biomass in a pressurized stirred batch reactor using a liquid extraction solvent and a base in which the ferulate and the coumarate remain.
DEVICE METHOD OF MAKING ARTEPILLIN C IN PROPOLIS FOR ANTI-CANCER
A method of making artepillin C in propolis includes the following steps: A. Mix propolis with ethanol to obtain a propolis-ethanol extract; B. Provide supercritical carbon dioxide and the propolis-ethanol extract to a chromatographic column to separate wax and artepillin C, and then remove the wax at a bottom of the chromatographic column and collect the artepillin C containing isolate at a top of the chromatographic column; and C. Test the artepillin C by a cytotoxicity test, a cell morphology analysis, a cell cycle and apoptosis test, and a cell motility metastasis test to find an anti-cancer effect of the artepillin C containing isolate.
DEVICE METHOD OF MAKING ARTEPILLIN C IN PROPOLIS FOR ANTI-CANCER
A method of making artepillin C in propolis includes the following steps: A. Mix propolis with ethanol to obtain a propolis-ethanol extract; B. Provide supercritical carbon dioxide and the propolis-ethanol extract to a chromatographic column to separate wax and artepillin C, and then remove the wax at a bottom of the chromatographic column and collect the artepillin C containing isolate at a top of the chromatographic column; and C. Test the artepillin C by a cytotoxicity test, a cell morphology analysis, a cell cycle and apoptosis test, and a cell motility metastasis test to find an anti-cancer effect of the artepillin C containing isolate.