C07C405/00

Process for the preparation of carboprost and its tromethamine salt

The subject of the invention is a novel process for the preparation of Carboprost tromethamine salt where alkylation the enone of the general formula (II) is carried out in the presence of a chiral auxiliary in aprotic solvent with a Grignard reagent. The methyl ester epimers of formula (VII) are separated by gravity silica gel chromatography and the salt formation is carried out by using solid tromethamine base. ##STR00001##

PROCESS FOR THE PREPARATION OF A NITRIC OXIDE DONATING PROSTAGLANDIN ANALOGUE

The present invention relates to a process for preparing hexanoic acid, 6-(nitrooxy)-, (1S,2E)-3-[(1R,2R,3S,5R)-2-[(2Z)-7-(ethylamino)-7-oxo-2-hepten-1-yl]-3,5-dihydroxycyclopentyl]-1-(2-phenylethyl)-2-propen-1-yl ester of formula (I).

##STR00001##

In accordance with the present invention, the compound (I) can be efficiently prepared with high purity by coupling bimatoprost in a boronate protected form with 6-(nitrooxy)hexanoyl chloride and removing the boronate protecting group.

The invention also relates to a process for the preparation of 6-(nitrooxy) hexanoic acid having a HPLC purity equal to or greater than 99% and containing an amount of 6-{[6-(nitrooxy)hexanoyl]oxy}hexanoic acid (compound (IXa) equal to or lower than 0.2%.

Methods and compositions for treating metabolic syndrome
10335418 · 2019-07-02 · ·

Provided are methods, compositions, systems, and kits for treating metabolic syndrome or a disorder associated with metabolic syndrome, e.g., obesity, dyslipidemia, and/or a diabetic condition, comprising administering systemically to a subject one or more compounds of the Formula (I) and/or (II): ##STR00001##
or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, polymorph, tautomer, isotopically enriched derivative, or prodrug thereof, wherein custom character, L, R.sub.1, R.sub.2, Z, X, A and B are defined herein.

Process to prepare treprostinil, the active ingredient in remodulin®

This present invention relates to an improved process to prepare prostacyclin derivatives. One embodiment provides for an improved process to convert benzindene triol to treprostinil via salts of treprostinil and to purify treprostinil.

Prostaglandin F2 alpha derivatives for decreasing intraocular pressure

The invention relates to clinical chemistry, in particular, to new biologically active compoundsamide derivatives of prostaglandin F2?. These compounds have low cytotoxicity and are capable of stimulating formation of endogenous nitrogen oxide in mammal cells. Synthesis of such compounds promotes expansion of nomenclature of biologically active derivatives of prostaglandin F2? capable of reducing intraocular pressure.

NOVEL PROSTAGLANDIN DERIVATIVE

The present invention relates to a novel prostaglandin derivative having an alkynyl group on -chain, particularly, a novel prostaglandin derivative having a double bond at the 2-position and an alkynyl group on the -chain and a medicament containing the compound as an active ingredient.

According to the present invention, a compound represented by the formula (1) or a pharmaceutically acceptable salt thereof;

##STR00001## wherein each symbol is as defined in the present specification, or a cyclodextrin clathrate compound thereof, and a medicament containing the compound as an active ingredient, particularly, a medicament for the prophylaxis or treatment of a blood flow disorder associated with spinal canal stenosis or chronic arterial occlusion, can be provided.

NOVEL PROSTAGLANDIN DERIVATIVE

The present invention relates to a novel prostaglandin derivative having an alkynyl group on -chain, particularly, a novel prostaglandin derivative having a double bond at the 2-position and an alkynyl group on the -chain and a medicament containing the compound as an active ingredient.

According to the present invention, a compound represented by the formula (1) or a pharmaceutically acceptable salt thereof;

##STR00001## wherein each symbol is as defined in the present specification, or a cyclodextrin clathrate compound thereof, and a medicament containing the compound as an active ingredient, particularly, a medicament for the prophylaxis or treatment of a blood flow disorder associated with spinal canal stenosis or chronic arterial occlusion, can be provided.

Nitric oxide donating derivatives of fluprostenol

The present invention relates to 15-nitrooxyderivatives of fluprostenol, their use for the treatment of glaucoma and ocular hypertension and formulation containing 15-nitrooxy derivatives of fluprostenol.

Tromethamine salt of bimatoprost acid in crystalline form 1, methods for preparation, and methods for use thereof

The present invention provides tromethamine salt of (Z)-7-[3,5-Dihydroxy-2-((E)-3-hydroxy-5-phenyl-pent-1-enyl)-cyclopentyl]-hept-5-enoic acid in crystalline Form 1 and amorphous form. This compound is may also be referred to as tromethamine salt of bimatoprost acid. The invention crystalline form is useful for solid ocular implant or topical formulations, utilized in the treatment of various ocular conditions, such as, for example, ocular hypertension.

Tromethamine salt of bimatoprost acid in crystalline form 1, methods for preparation, and methods for use thereof

The present invention provides tromethamine salt of (Z)-7-[3,5-Dihydroxy-2-((E)-3-hydroxy-5-phenyl-pent-1-enyl)-cyclopentyl]-hept-5-enoic acid in crystalline Form 1 and amorphous form. This compound is may also be referred to as tromethamine salt of bimatoprost acid. The invention crystalline form is useful for solid ocular implant or topical formulations, utilized in the treatment of various ocular conditions, such as, for example, ocular hypertension.