Patent classifications
C07D311/22
POLYMERIZABLE ABSORBERS OF UV AND HIGH ENERGY VISIBLE LIGHT
Described are polymerizable high energy light absorbing compounds of formula I:
##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, and X are as described herein. The compounds absorb various wavelengths of ultraviolet and/or high energy visible light and are suitable for incorporation in various products, such as biomedical devices and ophthalmic devices.
POLYMERIZABLE ABSORBERS OF UV AND HIGH ENERGY VISIBLE LIGHT
Described are polymerizable high energy light absorbing compounds of formula I:
##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, and X are as described herein. The compounds absorb various wavelengths of ultraviolet and/or high energy visible light and are suitable for incorporation in various products, such as biomedical devices and ophthalmic devices.
A 5-METHYLCHROMONE AND THE PREPARATION METHOD AND APPLICATION THEREOF
Disclosed is a 5-methylchromone and the preparation method and application thereof, the 5-methylchromone has the following structure:
##STR00001##
wherein R1 and R2 are alkyl groups. The substituted chromone has the biological activity of inhibiting tyrosinase. The preparation method uses 3,5-dihydroxytoluene as a raw material, and synthesis of chromones substituted with different groups at 2-C through acylation, esterification, rearrangement and cyclization reactions, etc. The 5-methylchromone is a completely new compound in condition that R1 is —CH.sub.2CH.sub.2CH.sub.3, and R2 is —CH.sub.2CH.sub.3, or that R1 is —C(CH.sub.3).sub.3, and R2 is H. All the compounds have obvious inhibitory activity against tyrosinase, and can be used to prepare tyrosinase inhibitors or whitening agents.
A 5-METHYLCHROMONE AND THE PREPARATION METHOD AND APPLICATION THEREOF
Disclosed is a 5-methylchromone and the preparation method and application thereof, the 5-methylchromone has the following structure:
##STR00001##
wherein R1 and R2 are alkyl groups. The substituted chromone has the biological activity of inhibiting tyrosinase. The preparation method uses 3,5-dihydroxytoluene as a raw material, and synthesis of chromones substituted with different groups at 2-C through acylation, esterification, rearrangement and cyclization reactions, etc. The 5-methylchromone is a completely new compound in condition that R1 is —CH.sub.2CH.sub.2CH.sub.3, and R2 is —CH.sub.2CH.sub.3, or that R1 is —C(CH.sub.3).sub.3, and R2 is H. All the compounds have obvious inhibitory activity against tyrosinase, and can be used to prepare tyrosinase inhibitors or whitening agents.
ALLOSTERIC CHROMENONE INHIBITORS OF PHOSPHOINOSITIDE 3-KINASE (PI3K) FOR THE TREATMENT OF DISEASE
The disclosure relates to compounds of Formula (I) as allosteric chromenone inhibitors of phosphoinositide 3-kinase (PI3K) useful in the treatment of diseases or disorders associated with PI3K modulation, Formula (I):
##STR00001##
or pharmaceutically acceptable salts thereof wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, and R.sub.8, are as defined herein. The disclosure also relates to methods of making and using compounds of Formula (I) or pharmaceutically acceptable salts thereof.
METHODS, PROCESSES AND INTERMEDIATES FOR PREPARING CHROMAN COMPOUNDS
This disclosure describes an economical and scalable method and process to synthesize the Calcium sensing receptor (CaSR) modulating agent 2-methyl-5-((2R,4S)-2-((((R)-1-(naphthalen-1-yl)ethyl)amino)methyl)chroman-4-yl)benzoic acid, its intermediates and pharmaceutically acceptable salts therefor. Uses of said intermediates for synthesis of compounds which may be intermediates to the synthesis of 2-methyl-5-((2R,4S)-2-((((R)-1-(naphthalen-1-yl)ethyl)amino)methyl)chroman-4-yl)benzoic acid are also described herein.
BIHETEROCYCLIC COMPOUND
The present invention provides a compound of formula (1) and a pharmaceutical composition comprising the compound useful as a nerve regeneration promoter
##STR00001##
wherein R.sup.1-L- is R.sup.1—OC(O)—, or the like, R.sup.1 is hydrogen atom, optionally-substituted C.sub.1-6 alkyl group, optionally-substituted 3- to 8-membered cycloalkyl group, or the like, R.sup.2 is hydrogen atom or the like, Ring A is formula (2) or formula (3) wherein R.sup.3 is hydrogen atom, optionally-substituted C.sub.1-6 alkyl group, or the like, the part of X, Y, and Z is X=Y-Z, X-Y=Z, or X-Y-Z, X is nitrogen atom, NR.sup.4 (R.sup.4 is hydrogen atom, optionally-substituted C.sub.1-6 alkyl group, or the like), or the like, Y is carbon atom or the like, and Z is carbon atom, nitrogen atom or the like.
BIHETEROCYCLIC COMPOUND
The present invention provides a compound of formula (1) and a pharmaceutical composition comprising the compound useful as a nerve regeneration promoter
##STR00001##
wherein R.sup.1-L- is R.sup.1—OC(O)—, or the like, R.sup.1 is hydrogen atom, optionally-substituted C.sub.1-6 alkyl group, optionally-substituted 3- to 8-membered cycloalkyl group, or the like, R.sup.2 is hydrogen atom or the like, Ring A is formula (2) or formula (3) wherein R.sup.3 is hydrogen atom, optionally-substituted C.sub.1-6 alkyl group, or the like, the part of X, Y, and Z is X=Y-Z, X-Y=Z, or X-Y-Z, X is nitrogen atom, NR.sup.4 (R.sup.4 is hydrogen atom, optionally-substituted C.sub.1-6 alkyl group, or the like), or the like, Y is carbon atom or the like, and Z is carbon atom, nitrogen atom or the like.
Macrophages/microglia in neuro-inflammation associated with neurodegenerative diseases
Described herein are methods of treating neuron inflammation conditions, for example, Alzheimer's disease, Parkinson's disease, Huntington's disease, ischemic stroke, and prion disease, comprising administering a therapeutically effective amount of cromolyn or a cromolyn derivative compound.
Macrophages/microglia in neuro-inflammation associated with neurodegenerative diseases
Described herein are methods of treating neuron inflammation conditions, for example, Alzheimer's disease, Parkinson's disease, Huntington's disease, ischemic stroke, and prion disease, comprising administering a therapeutically effective amount of cromolyn or a cromolyn derivative compound.