C07C405/0016

TOTAL SYNTHESIS OF PROSTAGLANDIN J NATURAL PRODUCTS BY TEREORETENTIVE METATHESIS

This invention relates generally to the synthesis of Δ.sup.12-Prostaglandin J product using stereoretentive ruthenium olefin metathesis catalysts supported by dithiolate ligands. Δ.sup.12-Prostaglandin J products were generated with excellent selectivity (>99% Z) and in moderate to high/good yields (47% to 80% yield; 58% to 80% yield).

PROSTAGLANDIN ANALOGS AND USES THEREOF

The present invention relates to pharmaceutical composition for the prevention or treatment of a disease, disorder, or condition associated with Nurr1, including, as an active ingredient, a prostaglandin analog or a pharmaceutically acceptable salt thereof, wherein the compound has excellent effects in inducing Nurr1, and thus, can be useful as a pharmaceutical composition for the prevention or treatment of a disease, disorder, or condition associated with Nurr1, in particular, cancer, autoimmune disease such as rheumatoid arthritis, schizophrenia, manic depression and neurodegenerative disease such as Alzheimers disease or Parkinson's disease.

Total synthesis of prostaglandin J natural products by stereoretentive metathesis

This invention relates generally to the synthesis of .sup.12-Prostaglandin J product using stereoretentive ruthenium olefin metathesis catalysts supported by dithiolate ligands. .sup.12-Prostaglandin J products were generated with excellent selectivity (>99% Z) and in moderate to high/good yields (47% to 80% yield; 58% to 80% yield).

Processes and intermediates for the preparations of isomer free prostaglandins

Novel processes for the preparation of a compound of Formula I-2 substantially free of the 5,6-trans isomer: ##STR00001##
wherein ##STR00002##
R.sub.2, R.sub.3 and R.sub.4 are as defined in the specification are provided. Novel intermediates for the preparations of isomer free Prostaglandins and derivatives thereof are also provided.

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.

PROCESSES AND INTERMEDIATES FOR THE PREPARATIONS OF ISOMER FREE PROSTAGLANDINS

Novel processes for the preparation of a compound of Formula I-2 substantially free of the 5,6-trans isomer:

##STR00001##

wherein

##STR00002##

R.sub.2, R.sub.3 and R.sub.4 are as defined in the specification are provided. Novel intermediates for the preparations of isomer free Prostaglandins and derivatives thereof are also provided.

Processes and intermediates for the preparations of isomer free prostaglandins

Novel processes for the preparation of a compound of Formula I-2 substantially free of the 5,6-trans isomer: ##STR00001##
wherein ##STR00002##
R.sub.2, R.sub.3 and R.sub.4 are as defined in the specification are provided. Novel intermediates for the preparations of isomer free Prostaglandins and derivatives thereof are also 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.