C07D339/04

PROBUCOL DERIVATIVE, PREPARATION METHOD THEREFOR AND USE THEREOF
20210040052 · 2021-02-11 ·

The present invention relates to the field of compounds, and in particular to a probucol derivative, a preparation method therefor and use thereof, the probucol derivative having a structure represented by general formula I. The probucol derivative provided in the present invention can be used for the prevention and treatment of vascular diseases including diabetes, cardio-cerebrovascular diseases or complications thereof, and can be effectively used for reducing blood glucose, reducing blood lipid, reducing cholesterol, reducing body weight, reducing triglyceride, anti-inflammatory, and anti-oxidation, etc., having broad prospective applications.

##STR00001##

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 -lipoic acid, and method for preparing thereof. Also disclosed are topical compositions comprising said salts or co-crystals and use thereof for treating pain.

1,2-dithiolane compounds useful in neuroprotection, autoimmune and cancer diseases and conditions

This invention provides compounds of the formula (I): ##STR00001##
wherein Y.sup.1, Y.sup.2, Z, X.sup.1, X.sup.2, and W are defined in the specification. These compounds are useful in the treatment of tyrosine kinases, MAPK signaling pathway kinases and PI3K/AKT/mTor signaling pathway kinases-mediated diseases or conditions, such as neurodegeneration, neuroprotection, cancer, autoimmune as well as other diseases and conditions associated with the modulation of tyrosine kinases selected from FYN, FYN Y531F, FLT3, FLT3-ITD, BRK, ITK, FRK, BTK, BMX, SRC, FGR, YES1, LCK, HCK, RET, CSK, LYN, and ROS1; MAPK pathway kinases selected from ARAF, BRAF, CRAF, ERK1/2, MEK1, MEK2, MEK3, MEK4, MEK5, MEK6, and MEK7; and PI3K/AKT/mTor pathway kinases: selected from mTor, PI3K , PI3K , PI3K , and PI3K .

1,2-dithiolane compounds useful in neuroprotection, autoimmune and cancer diseases and conditions

This invention provides compounds of the formula (I): ##STR00001##
wherein Y.sup.1, Y.sup.2, Z, X.sup.1, X.sup.2, and W are defined in the specification. These compounds are useful in the treatment of tyrosine kinases, MAPK signaling pathway kinases and PI3K/AKT/mTor signaling pathway kinases-mediated diseases or conditions, such as neurodegeneration, neuroprotection, cancer, autoimmune as well as other diseases and conditions associated with the modulation of tyrosine kinases selected from FYN, FYN Y531F, FLT3, FLT3-ITD, BRK, ITK, FRK, BTK, BMX, SRC, FGR, YES1, LCK, HCK, RET, CSK, LYN, and ROS1; MAPK pathway kinases selected from ARAF, BRAF, CRAF, ERK1/2, MEK1, MEK2, MEK3, MEK4, MEK5, MEK6, and MEK7; and PI3K/AKT/mTor pathway kinases: selected from mTor, PI3K , PI3K , PI3K , and PI3K .

Choline Esters
20200352903 · 2020-11-12 ·

Compounds, formulations, and methods are provided containing the choline ester of a reducing agent, especially lipoic acid or derivatives thereof. The compounds may be administered via a topical ocular route to treat or prevent oxidative damage.

Choline Esters
20200352903 · 2020-11-12 ·

Compounds, formulations, and methods are provided containing the choline ester of a reducing agent, especially lipoic acid or derivatives thereof. The compounds may be administered via a topical ocular route to treat or prevent oxidative damage.

S-SUBSTITUTED-2-AMINO-3-MERCAPTOPROPIONATE DERIVATIVE, PREPARATION METHOD AND APPLICATION THEREOF

The present invention relates to a S-substituted-2-amino-3-mercaptopropionate derivative, a preparation method and an application thereof. The S-substituted-2-amino-3-mercaptopropionate derivative in the present invention has a structure of a formula (A). The present invention also includes an application of the S-substituted-2-amino-3-mercaptopropionate derivative serving as a medicine for treating and/or preventing neurodegenerative diseases, particularly Alzheimer's disease.

##STR00001##

S-SUBSTITUTED-2-AMINO-3-MERCAPTOPROPIONATE DERIVATIVE, PREPARATION METHOD AND APPLICATION THEREOF

The present invention relates to a S-substituted-2-amino-3-mercaptopropionate derivative, a preparation method and an application thereof. The S-substituted-2-amino-3-mercaptopropionate derivative in the present invention has a structure of a formula (A). The present invention also includes an application of the S-substituted-2-amino-3-mercaptopropionate derivative serving as a medicine for treating and/or preventing neurodegenerative diseases, particularly Alzheimer's disease.

##STR00001##

COMPOUNDS, COMPOSITIONS AND METHODS FOR TREATMENT OF EYE DISORDERS AND SKIN DISEASES
20200262809 · 2020-08-20 ·

Disclosed is a compound of formula I or a pharmaceutically acceptable hydrate, solvate, crystal, co-crystal, enantiomer, stereoisomer, polymorph or prodrug thereof, which is useful for treatment of eye disorders, skin diseases and/or complications associated therewith. Also disclosed is a pharmaceutical composition comprising as an active ingredient at least one compound of formula I and a pharmaceutically acceptable excipient. Also disclosed is a method of treating an eye disorder, skin disease and/or a complication thereof in a subject in need thereof by administering at least one compound of formula I or a pharmaceutically acceptable hydrate, solvate, crystal, co-crystal, enantiomer, stereoisomer, polymorph or prodrug thereof.

COMPOUNDS, COMPOSITIONS AND METHODS FOR TREATMENT OF EYE DISORDERS AND SKIN DISEASES
20200262809 · 2020-08-20 ·

Disclosed is a compound of formula I or a pharmaceutically acceptable hydrate, solvate, crystal, co-crystal, enantiomer, stereoisomer, polymorph or prodrug thereof, which is useful for treatment of eye disorders, skin diseases and/or complications associated therewith. Also disclosed is a pharmaceutical composition comprising as an active ingredient at least one compound of formula I and a pharmaceutically acceptable excipient. Also disclosed is a method of treating an eye disorder, skin disease and/or a complication thereof in a subject in need thereof by administering at least one compound of formula I or a pharmaceutically acceptable hydrate, solvate, crystal, co-crystal, enantiomer, stereoisomer, polymorph or prodrug thereof.