C07C215/00

IONIZABLE LIPID COMPOUNDS AND LIPID NANOPARTICLE COMPOSITIONS
20230322689 · 2023-10-12 · ·

Novel ionizable lipids, compositions, and methods of using the novel ionizable lipids and compositions are disclosed. Lipid nanoparticle compositions include a novel ionizable lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Lipid nanoparticle compositions further including biologically active agents such as mRNA or DNA are useful in the delivery of biologically active agents to mammalian cells or organs.

Phenylethynylnaphthalene dyes and methods for their use

Compounds useful as fluorescent or colored dyes that enable visual detection of biomolecules and other analytes are disclosed. The compounds comprise a phenylethynylnapthalene moiety represented by the following structure (I): ##STR00001## including salts thereof, wherein R.sup.1a, R.sup.1b, R.sup.1c, R.sup.1d, R.sup.1e, R.sup.1f, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.2d, R.sup.2e, R.sup.2f, R.sup.2g, R.sup.2h, R.sup.2i, R.sup.2j, x and y are as defined herein. Methods associated with preparation and use of such compounds for visually detecting a biomolecule are also provided.

Pharmaceutical formulation for sublingual or buccal delivery of epinephrine or a pro-drug thereof
11021437 · 2021-06-01 · ·

The present invention relates to a pharmaceutical composition for the treatment of anaphylaxis formulated for rapid delivery, in one embodiment, the delivery vehicle is a rapidly dissolving film. The films contain an epinephrine or a novel epinephrine pro-drag for fee rapid treatment of anaphylaxis in a patient. This invention relates to pharmaceutical compositions made by modifying the physicochemical properties of epinephrine in order to enhance its permeability through biological membranes (sublingual and buccal membranes). Several prodrugs of epinephrine are shown by modifying the two hydroxyl (phenolic) groups in positions 3 and 4 on the benzene ring, by chemically reacting the two groups with several acid moieties to form an ester bond with different alkyl chains. The addition of an alkyl group will enhance the lipophilicity of epinephrine (increase log P) and will consequently increase its permeability through the biological membranes (sublingual and buccal tissues in the oral cavity).

Process for preparation of O-Desmethyltramadol and salts thereof

A process of preparation of O-Desmethyl tramadol through potassium hydroxide mediated demethylation of Tramadol under phase transfer conditions.

A PROCESS FOR PREPARATION OF O-DESMETHYLTRAMADOL AND SALTS THEREOF

A process of preparation of O-Desmethyl tramadol through potassium hydroxide mediated demethylation of Tramadol under phase transfer conditions.

PHARMACEUTICAL FORMULATION FOR SUBLINGUAL OR BUCCAL DELIVERY OF EPINEPHRINE OR A PRO-DRUG THEREOF
20190337886 · 2019-11-07 · ·

The present invention relates to a pharmaceutical composition for the treatment of anaphylaxis formulated for rapid delivery, in one embodiment, the delivery vehicle is a rapidly dissolving film. The films contain an epinephrine or a novel epinephrine pro-drag for fee rapid treatment of anaphylaxis in a patient. This invention relates to pharmaceutical compositions made by modifying the physicochemical properties of epinephrine in order to enhance its permeability through biological membranes (sublingual and buccal membranes). Several prodrugs of epinephrine are shown by modifying the two hydroxyl (phenolic) groups in positions 3 and 4 on the benzene ring, by chemically reacting the two groups with several acid moieties to form an ester bond with different alkyl chains. The addition of an alkyl group will enhance the lipophilicity of epinephrine (increase log P) and will consequently increase its permeability through the biological membranes (sublingual and buccal tissues in the oral cavity).

Process for preparation of 1-[2-(dimethyl amino)-1-(4-hydroxyphenyl) ethyl]-cyclohexanol and salts thereof

A high yield process of preparation of [1-[2-(Dimethylamino)-1-(4-hydroxyphenyl)ethy]-cyclohexanol] through potassium salt mediated demethylation of [1-[2-(Dimethyl amino-1-(4-methoxyphenyl) ethyl cyclohexanol] in monoethylene glycol under phase transfer conditions, as well as the preparation of salt of [1-[2-(Dimethylamino)-1-(4-hydroxyphenyl)ethyl]-cyclohexanol].

Process for preparation of 1-[2-(dimethyl amino)-1-(4-hydroxyphenyl) ethyl]-cyclohexanol and salts thereof

A high yield process of preparation of [1-[2-(Dimethylamino)-1-(4-hydroxyphenyl)ethy]-cyclohexanol] through potassium salt mediated demethylation of [1-[2-(Dimethyl amino-1-(4-methoxyphenyl) ethyl cyclohexanol] in monoethylene glycol under phase transfer conditions, as well as the preparation of salt of [1-[2-(Dimethylamino)-1-(4-hydroxyphenyl)ethyl]-cyclohexanol].

A PROCESS FOR PREPARATION OF 1-[2-(DIMETHYL AMINO)-1-(4-HYDROXYPHENYL) ETHYL]-CYCLOHEXANOL AND SALTS THEREOF

A high yield process of preparation of, [1-[2-(Dimethylamino)-1-(4-hydroxyphenyl)ethy]-cyclohexanol] through potassium hydroxide mediated demethylation of [1-[2-(Dimethyl amino-1-(4-methoxyphenyl) ethyl cyclohexanol] in monoethylene glycol under phase transfer conditions, as well as the preparation of salt of [1-[2-(Dimethylamino)-1-(4-hydroxyphenyl)ethyl]-cyclohexanol].