C07C251/38

Biodegradable lipids for the delivery of active agents

The present invention relates to a cationic lipid having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid.

Compounds and compositions for intracellular delivery of therapeutic agents

The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.

Methods for preparing dihydroxyammonium 5,5′-bistetrazole-1,1′diolate

The present invention relates to a method for preparing dihydroxyammonium 5,5-bistetrazole-1,1-diolate. The method for preparing dihydroxyammonium 5,5-bistetrazole-1,1-diolate, according to one embodiment of the present invention, comprises the steps of: synthesizing 5,5-bistetrazole-1,1-diol dihydrate (1,1-BTO) from ditetrahydropyranyl diazidoglyoxime (THP-DAG) by using a hydrochloric acid (HCl) solution in a first solvent; and reacting 1,1-BTO with an amine solution so as to neutralize same and, simultaneously, obtaining dihydroxylammonium 5,5-bistetrazole-1,1-diolate (Thomas Klapotke explosive-50, TKX-50).

Methods for preparing dihydroxyammonium 5,5′-bistetrazole-1,1′diolate

The present invention relates to a method for preparing dihydroxyammonium 5,5-bistetrazole-1,1-diolate. The method for preparing dihydroxyammonium 5,5-bistetrazole-1,1-diolate, according to one embodiment of the present invention, comprises the steps of: synthesizing 5,5-bistetrazole-1,1-diol dihydrate (1,1-BTO) from ditetrahydropyranyl diazidoglyoxime (THP-DAG) by using a hydrochloric acid (HCl) solution in a first solvent; and reacting 1,1-BTO with an amine solution so as to neutralize same and, simultaneously, obtaining dihydroxylammonium 5,5-bistetrazole-1,1-diolate (Thomas Klapotke explosive-50, TKX-50).

SUBSTITUTED BICYCLIC COMPOUNDS

Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V):

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and/or a salt thereof, wherein R.sub.1 is OH or OP(O)(OH).sub.2, and X.sub.1, X.sub.2, X.sub.3, R.sub.2, R.sub.2a, R.sub.a, R.sub.b, and R.sub.c are 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.

Methods of producing molindone and its salts

The present invention is directed towards novel methods of synthesis of molindone, synthesis of the intermediates of molindone, and high-purity compositions of molindone. In particular, the invention relates to the methods of synthesis of molindone through the Mannich reaction.

Methods of producing molindone and its salts

The present invention is directed towards novel methods of synthesis of molindone, synthesis of the intermediates of molindone, and high-purity compositions of molindone. In particular, the invention relates to the methods of synthesis of molindone through the Mannich reaction.

PROCESS FOR THE PREPARATION OF EXAMETAZIME

The present invention provides an improved process for the preparation of exametazime, which is used as ligand in preparation of technetium-99m complex.

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PROCESS FOR THE PREPARATION OF EXAMETAZIME

The present invention provides an improved process for the preparation of exametazime, which is used as ligand in preparation of technetium-99m complex.

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