C07F9/117

CYCLOALKYL-HYDROXYL COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES
20200189999 · 2020-06-18 ·

The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

CYCLOALKYL-HYDROXYL COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES
20200189999 · 2020-06-18 ·

The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

COMPOUNDS AND METHODS FOR DELIVERY OF PROSTACYCLIN ANALOGS
20200181057 · 2020-06-11 · ·

This invention pertains generally to prostacyclin formulations and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing angiogenesis.

COMPOUNDS AND METHODS FOR DELIVERY OF PROSTACYCLIN ANALOGS
20200181057 · 2020-06-11 · ·

This invention pertains generally to prostacyclin formulations and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing angiogenesis.

Phospholipid Analogues

The present invention relates to a compound having a structure according to formula (I) or a salt thereof, wherein: R.sub.1 is a branched or linear alkyl, acyl, alkenyl, hydroxyalkyl, hydroxyalkenyl, or hydroxy-alkinyl residue comprising 6 to 30 carbon atoms, R.sub.2 is selected from the group consisting of: a) an alkyl residue comprising 1 to 10 carbon atoms and comprising a terminal or cyclic quaternary ammonium, b) an alkyl residue comprising 1 to 10 carbon atoms and comprising a terminal amino group and/or 1 to 3 hydroxyl groups, c) an amino acid residue, d) a five or six carbon sugar and e) H, R.sub.3 is a residue selected from the group consisting of an alkyl, alkenyl, prostanyl-dialkyl, furanyl-dialkyl, cyclobutyl-dialkyl, cycloalkyl and aryl group of 2 to 40 carbon atoms length and comprising at least one keto group, epoxy group, aldehyde group, peroxy group, hydroperoxy group, hydroxyl group or a free carboxyl group, L1 is selected from the group consisting of O, NH, S, CH.sub.2, (aa), (bb), (cc), (dd), (ee), (ff), (gg), (hh), (ii), (jj), (kk), (ll), (mm), or (nn), L2 is an amide group or an ether group, X and Z are independently O, S or CH.sub.2, and Y is selected from the group consisting of O and S.

##STR00001##

Phospholipid Analogues

The present invention relates to a compound having a structure according to formula (I) or a salt thereof, wherein: R.sub.1 is a branched or linear alkyl, acyl, alkenyl, hydroxyalkyl, hydroxyalkenyl, or hydroxy-alkinyl residue comprising 6 to 30 carbon atoms, R.sub.2 is selected from the group consisting of: a) an alkyl residue comprising 1 to 10 carbon atoms and comprising a terminal or cyclic quaternary ammonium, b) an alkyl residue comprising 1 to 10 carbon atoms and comprising a terminal amino group and/or 1 to 3 hydroxyl groups, c) an amino acid residue, d) a five or six carbon sugar and e) H, R.sub.3 is a residue selected from the group consisting of an alkyl, alkenyl, prostanyl-dialkyl, furanyl-dialkyl, cyclobutyl-dialkyl, cycloalkyl and aryl group of 2 to 40 carbon atoms length and comprising at least one keto group, epoxy group, aldehyde group, peroxy group, hydroperoxy group, hydroxyl group or a free carboxyl group, L1 is selected from the group consisting of O, NH, S, CH.sub.2, (aa), (bb), (cc), (dd), (ee), (ff), (gg), (hh), (ii), (jj), (kk), (ll), (mm), or (nn), L2 is an amide group or an ether group, X and Z are independently O, S or CH.sub.2, and Y is selected from the group consisting of O and S.

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LIMONENE-BASED, NON-HALOGENATED FLAME RETARDANTS FOR POLYMERIC APPLICATIONS

A limonene-based flame-retardant compound, a method of making a flame-retardant polymer, and an article of manufacture comprising a material that includes a limonene-based flame-retardant compound are provided. In an embodiment, the method includes forming a limonene-based derivative; forming a phosphorus-based flame-retardant molecule; reacting the limonene-based derivative with the phosphorus-based flame-retardant molecule to form a limonene-based flame-retardant compound; and forming a flame-retardant polymer from the limonene-based flame-retardant compound. In some embodiments, the limonene-based flame-retardant compound has variable functionality including vinyl, epoxide, methylene bridges, and thioethers.

LIMONENE-BASED, NON-HALOGENATED FLAME RETARDANTS FOR POLYMERIC APPLICATIONS

A limonene-based flame-retardant compound, a method of making a flame-retardant polymer, and an article of manufacture comprising a material that includes a limonene-based flame-retardant compound are provided. In an embodiment, the method includes forming a limonene-based derivative; forming a phosphorus-based flame-retardant molecule; reacting the limonene-based derivative with the phosphorus-based flame-retardant molecule to form a limonene-based flame-retardant compound; and forming a flame-retardant polymer from the limonene-based flame-retardant compound. In some embodiments, the limonene-based flame-retardant compound has variable functionality including vinyl, epoxide, methylene bridges, and thioethers.

Substituted tricyclic heterocyclic compounds

Disclosed are compounds of Formula (I), Formula (II), Formula (III), and Formula (IV) or salts thereof, wherein R.sub.2 is OH or OP(O)(OH).sub.2; and R.sub.1 is defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease. ##STR00001##

Substituted tricyclic heterocyclic compounds

Disclosed are compounds of Formula (I), Formula (II), Formula (III), and Formula (IV) or salts thereof, wherein R.sub.2 is OH or OP(O)(OH).sub.2; and R.sub.1 is defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease. ##STR00001##