Patent classifications
C07D295/10
BENZODICYCLOALKANE DERIVATIVE, PREPARATION METHOD AND USE THEREOF
It is provided herein a benzobicycloalkane derivative, and a preparation method and use thereof. In particular, it is provided herein a compound of Formula (I), or a pharmaceutically acceptable salt, stereoisomer or solvate thereof, a preparation method, and a use thereof in preparation of drugs for treating pain.
##STR00001##
NOVEL N-ACYLUREA DERIVATIVE AND COMPOSITION COMPRISING SAME FOR PREVENTION OR TREATMENT OF CARDIOVASCULAR DISEASE
The present invention relates to a novel N-acylurea derivative and the use thereof for the prevention or treatment of cardiovascular disease, and more particularly to a novel N-acylurea derivative, a pharmaceutical composition for prevention or treatment of cardiovascular disease, which contains the N-acylurea derivative as an active ingredient, and a method of preparing the N-acylurea derivative. The N-acylurea derivative according to the present invention can inhibit platelet aggregation by inhibiting the activity of talin in the intracellular matrix, and thus can be useful for the prevention or treatment of cardiovascular disease.
NOVEL N-ACYLUREA DERIVATIVE AND COMPOSITION COMPRISING SAME FOR PREVENTION OR TREATMENT OF CARDIOVASCULAR DISEASE
The present invention relates to a novel N-acylurea derivative and the use thereof for the prevention or treatment of cardiovascular disease, and more particularly to a novel N-acylurea derivative, a pharmaceutical composition for prevention or treatment of cardiovascular disease, which contains the N-acylurea derivative as an active ingredient, and a method of preparing the N-acylurea derivative. The N-acylurea derivative according to the present invention can inhibit platelet aggregation by inhibiting the activity of talin in the intracellular matrix, and thus can be useful for the prevention or treatment of cardiovascular disease.
Benzoylglycine derivatives and methods of making and using same
Disclosed are compounds of formulae: ##STR00001##
and pharmaceutically acceptable salts thereof, wherein the variables, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.11, R.sub.12, R.sub.13, R.sub.14, R.sub.15, R.sub.16, R.sub.17, n, and m are defined herein. These compounds are useful for treating Gram-negative bacteria infections. Also disclosed are methods of making these compounds.
Benzoylglycine derivatives and methods of making and using same
Disclosed are compounds of formulae: ##STR00001##
and pharmaceutically acceptable salts thereof, wherein the variables, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.11, R.sub.12, R.sub.13, R.sub.14, R.sub.15, R.sub.16, R.sub.17, n, and m are defined herein. These compounds are useful for treating Gram-negative bacteria infections. Also disclosed are methods of making these compounds.
6-SUBSTITUTED NAPHTHALENE-1,3-DISULFONIC ACID DERIVATIVES AS MODULATORS OF THE EXTRACELLULAR NICOTINAMIDE PHOSPHORIBOSYL TRANSFERASE (ENAMPT) FOR THE TREATMENT OF E.G. DIABETES
This invention relates to therapeutic 6-substituted naphthalene-1,3-disulfonic acid derivatives of formula (I) (Formula (I)). More specifically, the invention relates to compounds of formula (I) useful as modulators of extracellular nicotinamide phosphoribosyl transferase (eNAMPT) that stabilize the protein in its dimeric form. In addition the invention contemplates pharmaceutical compositions comprising the compounds, processes to prepare the compounds and the compounds for use in methods of medical treatment of e.g. (i) diabetes; (ii) cardiovascular disease; (iii) inflammatory bowel condition; (iv) cancer; (v) liver disease; (vi) inflammatory skin conditions; (vii) lung conditions; (viii) arthritis; (ix) kidney disease (e.g. chronic kidney disease); or (x) sepsis. An exemplary compound is e.g. 6-(2-fluoro-5-((3-(4-(piperidin-1-ylsulfonyl) phenyl) ureido)methyl)phenyl)-4-(trioxidaneylthio) naphthalene-2-sulfonic acid (example 1).
##STR00001##
Substituted pyrrolidines as G-protein coupled receptor 43 agonists
The present invention is directed to a process for the preparation of aryl-pyrrolidine carboxylic acid derivative compounds which are useful in treating metabolic diseases, said process consisting of coupling an aryl-pyrrolidine compound with an aryl carboxylic acid compound followed by alkaline or acidic treatment, hydrogenolysis or treatment with a fluoride of the ester intermediate to afford novel aryl-pyrrolidine carboxylic acid derivative compounds.
SULFONAMIDE DERIVATIVE AND PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALT THEREOF
The present invention aims to provide a novel low-molecular-weight compound exhibiting an orexin receptor agonist activity and expected to be useful as a prophylactic or therapeutic agent for narcolepsy and the like. The present invention provides a compound represented by the formula (I):
##STR00001##
wherein each symbol is as defined in the description, or a pharmaceutically acceptable acid addition salt thereof, which has an orexin receptor agonist activity, and an orexin receptor agonist containing the compound or a pharmaceutically acceptable acid addition salt thereof.
Neprilysin inhibitors
In one aspect, the invention relates to compounds having the formula I: ##STR00001##
where R.sup.1-R.sup.6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
Polymerization initiator and radically polymerizable composition containing same
Provided is an -aminoalkylphenone compound that has good stability and low sublimability, efficiently generates radicals when irradiated with a bright line at 365 nm (I line) or the like, and is useful as a polymerization initiator to be used in a radically polymerizable composition. The -aminoalkylphenone compound is represented by Formula (I) mentioned below. ##STR00001##
In Formula (I) mentioned above, it is preferable that R.sup.11 is a nitro group, an alkoxy group having 1 to 12 carbon atoms, or an alkoxycarbonyl group having 1 to 12 carbon atoms. The -aminoalkylphenone compound can be preferably used in a polymerization initiator.