C07C229/38

Lipids and lipid compositions for the delivery of active agents

This invention provides for a compound of formula (I): ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein R.sup.1-R.sup.4, L.sub.1, n and p are defined herein. The compounds of formula (X) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.

LSD1 inhibitor and preparation method and application thereof

A cyclopropylamine compound as a lysine-specific demethylase 1 (LSD1) inhibitor. Particularly, the present invention relates to a compound represented by formula (I) and a pharmaceutically acceptable salt thereof. The present invention also provides an application of the same in preparing a drug for treating an LSD1-related disease. ##STR00001##

QUATERNARY AMINE COMPOUNDS WITH ISOPROPYLMETHYLPHENOL ESTER MOIETIES AS ANTIVIRALS, ANTIBACTERIALS AND ANTIMYCOTICS
20220213024 · 2022-07-07 ·

Disclosed are compounds having the following formula (I):Formula (I) wherein R is an alkylene chain having between 8 and 20 carbon atoms, and A is one or more anions having a total charge of −2, or R is a quaternary amine having the following formula (Ia):Formula (Ia) wherein R.sub.a and R.sub.b are each an alkylene chain having between 8 and 20 carbon atoms, and A is one or more anions having a total charge of −3; R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are each independently selected from C.sub.1-10 alkyl and H; E has the following Formula (Ib), wherein the ester oxygen is bonded to the aromatic ring of each E at the same position, the position being position 2 or 3; and wherein R.sub.E is H or a halide.

##STR00001##

QUATERNARY AMINE COMPOUNDS WITH ISOPROPYLMETHYLPHENOL ESTER MOIETIES AS ANTIVIRALS, ANTIBACTERIALS AND ANTIMYCOTICS
20220213024 · 2022-07-07 ·

Disclosed are compounds having the following formula (I):Formula (I) wherein R is an alkylene chain having between 8 and 20 carbon atoms, and A is one or more anions having a total charge of −2, or R is a quaternary amine having the following formula (Ia):Formula (Ia) wherein R.sub.a and R.sub.b are each an alkylene chain having between 8 and 20 carbon atoms, and A is one or more anions having a total charge of −3; R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are each independently selected from C.sub.1-10 alkyl and H; E has the following Formula (Ib), wherein the ester oxygen is bonded to the aromatic ring of each E at the same position, the position being position 2 or 3; and wherein R.sub.E is H or a halide.

##STR00001##

Stilbene derivative and method for preparing same
11401231 · 2022-08-02 · ·

This invention relates to a stilbene derivative and a method of preparing the same, and more particularly to a novel stilbene derivative for inhibiting the function of cyclophilin, which is effective at the prevention of cyclophilin-related diseases or at the treatment of symptoms of such diseases, and to a method of preparing the same.

Stilbene derivative and method for preparing same
11286228 · 2022-03-29 · ·

A stilbene derivative and a method of preparing the A stilbene derivative are disclosed. The stilbene derivative is provided for inhibiting the function of cyclophilin, which is effective at the prevention of cyclophilin-related diseases or at the treatment of symptoms of such diseases. The method of preparing a stilbene derivative includes reacting a phenylacetonitrile derivative with a benzaldehyde derivative.

Diamine derivatives as inhibitors of leukotriene A4 hydrolase

This invention is directed to compounds of formula (I): ##STR00001##
where r, q, R, R.sup.2, R.sup.3, R.sup.4, R.sup.5a, R.sup.5b, R.sup.5c, R.sup.6a, R.sup.6b, R.sup.6c, R.sup.7, R.sup.8, and R.sup.9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A.sub.4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

Diamine derivatives as inhibitors of leukotriene A4 hydrolase

This invention is directed to compounds of formula (I): ##STR00001##
where r, q, R, R.sup.2, R.sup.3, R.sup.4, R.sup.5a, R.sup.5b, R.sup.5c, R.sup.6a, R.sup.6b, R.sup.6c, R.sup.7, R.sup.8, and R.sup.9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A.sub.4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

Organic amine ester derivative drug of 2-(α-hydroxypentyl)benzoic acid
11149005 · 2021-10-19 · ·

An organic amine ester derivative drug of 2-(α-hydroxypentyl)benzoic acid and a preparation method thereof and an use thereof are disclosed. The present disclosure particularly relates to a compound having the general formula I or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable formulation prepared from the compound or the pharmaceutically acceptable salt thereof. The compound having the general formula I or the pharmaceutically acceptable salt thereof has in vitro a good solubility and a low hygroscopicity, and has in vivo a bioavailability and a brain aggregation concentration that are significantly greater than those of the original medicine butyphthalide and/or an improving drug efficacy. The use of the compound in the preparation of a drug for preventing and/or treating heart and cerebral ischemic diseases, a drug for preventing and/or treating heart and cerebral artery occlusion diseases, an anti-parkinsonian drug and an anti-senile-dementia drug is also disclosed. ##STR00001##

Organic amine ester derivative drug of 2-(α-hydroxypentyl)benzoic acid
11149005 · 2021-10-19 · ·

An organic amine ester derivative drug of 2-(α-hydroxypentyl)benzoic acid and a preparation method thereof and an use thereof are disclosed. The present disclosure particularly relates to a compound having the general formula I or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable formulation prepared from the compound or the pharmaceutically acceptable salt thereof. The compound having the general formula I or the pharmaceutically acceptable salt thereof has in vitro a good solubility and a low hygroscopicity, and has in vivo a bioavailability and a brain aggregation concentration that are significantly greater than those of the original medicine butyphthalide and/or an improving drug efficacy. The use of the compound in the preparation of a drug for preventing and/or treating heart and cerebral ischemic diseases, a drug for preventing and/or treating heart and cerebral artery occlusion diseases, an anti-parkinsonian drug and an anti-senile-dementia drug is also disclosed. ##STR00001##