Patent classifications
C07C69/708
RUTHENIUM COMPLEXES AND THEIR USES AS CATALYSTS IN PROCESSES FOR FORMATION AND/OR HYDROGENATION OF ESTERS, AMIDES AND RELATED REACTIONS
The present invention relates to novel Ruthenium complexes of formulae A1-A4 and their use, inter alia, for (1) dehydrogenative coupling of alcohols to esters; (2) hydrogenation of esters to alcohols (including hydrogenation of cyclic esters (lactones) or cyclic di-esters (di-lactones), or polyesters); (3) preparing amides from alcohols and amines—(including the preparation of polyamides (e.g., polypeptides) by reacting dialcohols and diamines and/or polymerization of amino alcohols and/or forming cyclic dipeptides from p-aminoalcohols; (4) hydrogenation of amides (including cyclic dipeptides, polypeptides and polyamides) to alcohols and amines; (5) hydrogenation of organic carbonates (including polycarbonates) to alcohols or hydrogenation of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (6) dehydrogenation of secondary alcohols to ketones; (7) amidation of esters (i.e., synthesis of amides from esters and amines); (8) acylation of alcohols using esters; (9) coupling of alcohols with water and a base to form carboxylic acids; and (10) preparation of amino acids or their salts by coupling of amino alcohols with water and a base. The present, invention further relates to the use of certain known Ruthenium complexes for the preparation of amino acids or their salts from amino alcohols.
PEG LIPIDS AND USES THEREOF
The present disclosure in part provides compounds (i.e., PEG lipids) which are useful in pharmaceutical compositions, cosmetic compositions, and drug delivery systems, e.g, for use in lipid nanoparticle (LNP) formulations. The present disclosure also provides LNP formulations comprising PEG lipids described herein, and methods of using the same. For example, the LNPs provided herein are useful for the delivery of an agent (e.g, therapeutic agent) to a subject. The PEG lipids and LNPs provided herein, in certain embodiments, exhibit increased PEG shedding compared to existing PEG lipids and LNP formulations.
PEG LIPIDS AND USES THEREOF
The present disclosure in part provides compounds (i.e., PEG lipids) which are useful in pharmaceutical compositions, cosmetic compositions, and drug delivery systems, e.g, for use in lipid nanoparticle (LNP) formulations. The present disclosure also provides LNP formulations comprising PEG lipids described herein, and methods of using the same. For example, the LNPs provided herein are useful for the delivery of an agent (e.g, therapeutic agent) to a subject. The PEG lipids and LNPs provided herein, in certain embodiments, exhibit increased PEG shedding compared to existing PEG lipids and LNP formulations.
Glycosidic derivatives of treprostinil
The present invention relates to the field of pharmaceutical products, specifically the glycosidic derivatives of treprostinil. The glycosidic treprostinil derivatives can be used to treat any conditions responsive to treatment with treprostinil, including pulmonary hypertension, such as pulmonary arterial hypertension.
Glycosidic derivatives of treprostinil
The present invention relates to the field of pharmaceutical products, specifically the glycosidic derivatives of treprostinil. The glycosidic treprostinil derivatives can be used to treat any conditions responsive to treatment with treprostinil, including pulmonary hypertension, such as pulmonary arterial hypertension.
METHODS
A method for preparing a partially fluorinated ester comprising acyl and alkoxy groups wherein the acyl group comprises a branched or linear fluorine containing C.sub.3-C.sub.8 group with one of the structures: (Formulae (I), (II)) wherein X and Y are independently selected from: —H, —CH.sub.3, —F, —Cl, —CH.sub.2F, —CF.sub.3—OCF.sub.3, —OCH.sub.2CF.sub.3, OCH.sub.2CF.sub.2CHF.sub.2 and —CH.sub.2CF.sub.3 (wherein both X and Y cannot be H) comprising reacting an unsaturated halocarbon: (Formula (III)) wherein A and B are independently selected from the group comprising —H, —CH.sub.3, —F, —Cl, —CH.sub.2F, —CF.sub.3, —OCF.sub.3, —OCH.sub.2CF.sub.3, OCH.sub.2CF.sub.2CHF.sub.2 and —CH.sub.2CF.sub.3 (wherein both A and B cannot be H) with carbon monoxide and an alcohol, in the presence of a catalyst methods.
##STR00001##
METHODS
A method for preparing a partially fluorinated ester comprising acyl and alkoxy groups wherein the acyl group comprises a branched or linear fluorine containing C.sub.3-C.sub.8 group with one of the structures: (Formulae (I), (II)) wherein X and Y are independently selected from: —H, —CH.sub.3, —F, —Cl, —CH.sub.2F, —CF.sub.3—OCF.sub.3, —OCH.sub.2CF.sub.3, OCH.sub.2CF.sub.2CHF.sub.2 and —CH.sub.2CF.sub.3 (wherein both X and Y cannot be H) comprising reacting an unsaturated halocarbon: (Formula (III)) wherein A and B are independently selected from the group comprising —H, —CH.sub.3, —F, —Cl, —CH.sub.2F, —CF.sub.3, —OCF.sub.3, —OCH.sub.2CF.sub.3, OCH.sub.2CF.sub.2CHF.sub.2 and —CH.sub.2CF.sub.3 (wherein both A and B cannot be H) with carbon monoxide and an alcohol, in the presence of a catalyst methods.
##STR00001##
METHODS
A method for preparing a partially fluorinated ester comprising acyl and alkoxy groups wherein the acyl group comprises a branched or linear fluorine containing C.sub.3-C.sub.8 group with one of the structures: (Formulae (I), (II)) wherein X and Y are independently selected from: —H, —CH.sub.3, —F, —Cl, —CH.sub.2F, —CF.sub.3—OCF.sub.3, —OCH.sub.2CF.sub.3, OCH.sub.2CF.sub.2CHF.sub.2 and —CH.sub.2CF.sub.3 (wherein both X and Y cannot be H) comprising reacting an unsaturated halocarbon: (Formula (III)) wherein A and B are independently selected from the group comprising —H, —CH.sub.3, —F, —Cl, —CH.sub.2F, —CF.sub.3, —OCF.sub.3, —OCH.sub.2CF.sub.3, OCH.sub.2CF.sub.2CHF.sub.2 and —CH.sub.2CF.sub.3 (wherein both A and B cannot be H) with carbon monoxide and an alcohol, in the presence of a catalyst methods.
##STR00001##
Substituted butanol derivatives and their use as fragrance and flavor materials
The present invention is related to substituted butanol derivatives of the formula: ##STR00001##
wherein R is an unsubstituted or substituted C.sub.1-6 straight chain alkyl, an unsubstituted or substituted C.sub.3-6 branched chain alkyl, an unsubstituted or substituted C.sub.3-6 straight chain alkenyl, an unsubstituted or substituted C.sub.3-6 branched chain alkenyl, an unsubstituted or substituted C.sub.3-6 cycloalkyl, an unsubstituted or substituted C.sub.1-6 alkoxy, nitrile, halo, amino, an unsubstituted or substituted C.sub.1-6 alkylamino, an unsubstituted or substituted C.sub.1-6 dialkylamino, carboxy-C.sub.1-6 alkylamino, carboxy-C.sub.1-6 dialkylamino, an unsubstituted or substituted acetoxy, carboxy, an unsubstituted or substituted carboxyethyl, an unsubstituted or substituted C.sub.1-6 alkylcarbonyl, an unsubstituted or substituted C.sub.1-6 alkylcarboxy, an unsubstituted or substituted C.sub.1-6 alkylthio, an unsubstituted or substituted C.sub.1-6 alkyloxy, carboxamido, an unsubstituted or substituted C.sub.1-6 alkylcarboxamido or an unsubstituted or substituted C.sub.1-6 dialkylcarboxamido. Such compounds are useful in flavor or flavor compositions.
Substituted butanol derivatives and their use as fragrance and flavor materials
The present invention is related to substituted butanol derivatives of the formula: ##STR00001##
wherein R is an unsubstituted or substituted C.sub.1-6 straight chain alkyl, an unsubstituted or substituted C.sub.3-6 branched chain alkyl, an unsubstituted or substituted C.sub.3-6 straight chain alkenyl, an unsubstituted or substituted C.sub.3-6 branched chain alkenyl, an unsubstituted or substituted C.sub.3-6 cycloalkyl, an unsubstituted or substituted C.sub.1-6 alkoxy, nitrile, halo, amino, an unsubstituted or substituted C.sub.1-6 alkylamino, an unsubstituted or substituted C.sub.1-6 dialkylamino, carboxy-C.sub.1-6 alkylamino, carboxy-C.sub.1-6 dialkylamino, an unsubstituted or substituted acetoxy, carboxy, an unsubstituted or substituted carboxyethyl, an unsubstituted or substituted C.sub.1-6 alkylcarbonyl, an unsubstituted or substituted C.sub.1-6 alkylcarboxy, an unsubstituted or substituted C.sub.1-6 alkylthio, an unsubstituted or substituted C.sub.1-6 alkyloxy, carboxamido, an unsubstituted or substituted C.sub.1-6 alkylcarboxamido or an unsubstituted or substituted C.sub.1-6 dialkylcarboxamido. Such compounds are useful in flavor or flavor compositions.