C07C217/46

NOVEL CATIONIC LIPIDS AND METHODS OF USE THEREOF

The present invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel cationic lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of a specific target protein at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.

SSAO INHIBITORS AND USES THEREOF

Described herein are compounds that are semicarbazide-sensitive amine oxidase (SSAO) inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in treating or preventing a liver disease or condition.

Fluoroallylamine Derivative And Use Thereof

The present invention relates to a fluoroallylamine derivative and use thereof. In particular, the present invention relates to a compound as shown in Formula I, a prodrug, an isomer, an isotope-labeled compound, a solvate or a pharmaceutically acceptable salt thereof, which has VAP-1/SSAO inhibitory activity, and can be used for treating a disease associated with VAP-1/SSAO overactivity.

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Amine Derivatives of The Beta-Farnesene

The invention provides a process for preparing farnesylamines by reacting -farnesene with one or more amines in the presence of a transition metal catalyst from transition group 10 at a temperature in the range from 60 to 150 C.

##STR00001##

Compositions for treating neurodegenerative diseases

The present disclosure relates to novel compounds of Formula I ##STR00001##
wherein each of R.sup.a, R.sup.b, R.sup.d and R.sup.e is independently H; R.sup.c is selected from the group consisting of H, hydroxyl, halo, alkyl, alkoxy, CF.sub.3, SO.sub.2CH.sub.3, and morpholino, R.sup.1 is selected from the group consisting of hydrogen, alkyl, phenyl, or CH?C(CH.sub.3).sub.2; and R.sup.2 is specific substituted cyclic amino groups. The invention also discloses pharmaceutical compositions containing the compounds and methods of using the compounds and pharmaceutical compositions for treating neurogenerative diseases, including Alzheimer's disease and cognitive decline.

METHODS FOR TOTAL SYNTHESIS OF RESOLVIN E1
20180297925 · 2018-10-18 ·

Methods for total chemical synthesis of Resolvin E1 (RvE1) include Wittig reaction of two compounds having hydroxyl protecting group in the presence of a strong base, removal of the hydroxyl-protecting groups with a deprotecting reagent to produce a compound having an ester group, and hydrolysis of the ester group to obtain RvE1

METHODS FOR TOTAL SYNTHESIS OF RESOLVIN E1
20180297925 · 2018-10-18 ·

Methods for total chemical synthesis of Resolvin E1 (RvE1) include Wittig reaction of two compounds having hydroxyl protecting group in the presence of a strong base, removal of the hydroxyl-protecting groups with a deprotecting reagent to produce a compound having an ester group, and hydrolysis of the ester group to obtain RvE1

Etheramines based on 1,2-dialcohols

The invention relates to etheramines of formula (I) or formula (II) or a mixture of etheramines of formula (I) and formula (II) based on 1,2-dialcohols, wherein R.sub.1 is a linear or branched alkyl group with 2 to 16 carbon atoms, R.sub.2 is a hydrogen or an alkyl group with 1 to 16 carbon atoms, x1 and y1 and the sum of x+y is between 2 and 10, and A.sub.1, A.sub.2, A.sub.3 and A.sub.4 are independently selected from the group consisting of linear and/or branched alkylenes having 2 to 18 carbon atoms and wherein Z.sub.1-Z.sub.4 are independently selected from OH, NH.sub.2, NHR or NRR, wherein at least one of Z.sub.1-Z.sub.2 and at least one of Z.sub.3-Z.sub.4 is NH.sub.2, NHR or NRR, wherein R and R are independently selected from alkylenes having 2 to 6 carbon atoms. ##STR00001## The invention further relates to etheramines obtainable by the alkoxylation and amination of 1,2-dialcohols.

Etheramines based on 1,2-dialcohols

The invention relates to etheramines of formula (I) or formula (II) or a mixture of etheramines of formula (I) and formula (II) based on 1,2-dialcohols, wherein R.sub.1 is a linear or branched alkyl group with 2 to 16 carbon atoms, R.sub.2 is a hydrogen or an alkyl group with 1 to 16 carbon atoms, x1 and y1 and the sum of x+y is between 2 and 10, and A.sub.1, A.sub.2, A.sub.3 and A.sub.4 are independently selected from the group consisting of linear and/or branched alkylenes having 2 to 18 carbon atoms and wherein Z.sub.1-Z.sub.4 are independently selected from OH, NH.sub.2, NHR or NRR, wherein at least one of Z.sub.1-Z.sub.2 and at least one of Z.sub.3-Z.sub.4 is NH.sub.2, NHR or NRR, wherein R and R are independently selected from alkylenes having 2 to 6 carbon atoms. ##STR00001## The invention further relates to etheramines obtainable by the alkoxylation and amination of 1,2-dialcohols.

COMPOSITIONS FOR TREATING NEURODEGENERATIVE DISEASES

The present disclosure relates to novel compounds, pharmaceutical compositions containing the compounds and methods of using the compounds and pharmaceutical compositions for treating neurodegerative diseases, including Alzheimer's disease and cognitive decline. Methods for inhibiting synapse number decline or membrane trafficking abnormalities associated with exposure of a neuronal cell to Abeta species are also disclosed.