A61K31/121

Dihydroorotic and acid dehydrogenase inhibitor

The present invention provides a novel dihydroorotic acid dehydrogenase inhibitor which is applicable to various diseases. When used as an active ingredient, a compound represented by formula (I): ##STR00001##
(wherein X represents a halogen atom, R.sup.1 represents a hydrogen atom, R.sup.2 represents an alkyl group containing 1 to 7 carbon atoms, R.sup.3 represents —CHO, and R.sup.4 represents —CH.sub.2—CH═C(CH.sub.3)—R.sup.0 (wherein R.sup.0 represents an alkyl group containing 1 to 12 carbon atoms which may have a substituent on the terminal carbon and/or on a non-terminal carbon, etc.)),
an optical isomer thereof or a pharmaceutically acceptable salt thereof has a high inhibitory effect on dihydroorotic acid dehydrogenase and can be used as an immunosuppressive agent, a therapeutic agent for rheumatism, an anticancer agent, a therapeutic agent for graft rejection, an antiviral agent, an anti-H. pylori agent, a therapeutic agent for diabetes or the like.

SMALL MOLECULE INHIBITORS OF A PROTEIN COMPLEX

Compositions and methods for treating thrombosis, inflammation, and atherosclerosis by administration of a compound that binds to KRIT1 to inhibit binding with HEG1.

SMALL MOLECULE INHIBITORS OF A PROTEIN COMPLEX

Compositions and methods for treating thrombosis, inflammation, and atherosclerosis by administration of a compound that binds to KRIT1 to inhibit binding with HEG1.

Agent for the prevention, improvement or treatment of retinal disease

A prophylactic, ameliorating or therapeutic agent for a retinal disease, the agent comprising geranylgeranylacetone which (a) is a mixture of (5E,9E,13E)-geranylgeranylacetone and (5Z,9E,13E)-geranylgeranylacetone, the (5E,9E,13E)-geranylgeranylacetone content of the mixture being 80% by weight or more, (b) consists of (5E,9E,13E)-geranylgeranylacetone, or (c) consists of (5Z,9E,13E)-geranylgeranylacetone directly suppresses the death of a retinal cell, thereby fundamentally preventing, ameliorating or treating the retinal disease.

Agent for the prevention, improvement or treatment of retinal disease

A prophylactic, ameliorating or therapeutic agent for a retinal disease, the agent comprising geranylgeranylacetone which (a) is a mixture of (5E,9E,13E)-geranylgeranylacetone and (5Z,9E,13E)-geranylgeranylacetone, the (5E,9E,13E)-geranylgeranylacetone content of the mixture being 80% by weight or more, (b) consists of (5E,9E,13E)-geranylgeranylacetone, or (c) consists of (5Z,9E,13E)-geranylgeranylacetone directly suppresses the death of a retinal cell, thereby fundamentally preventing, ameliorating or treating the retinal disease.

ANTIVIRAL THERAPEUTIC DRUG COMBINATIONS

Provided herein are compositions and methods for the treatment or prevention of viral infections via the use of chemical substances administered in a combinatory fashion for the suppression, inhibition, and elimination of viral loads. These compositions and methods use a glycolysis inhibitor (e.g., 2-deoxy-D-glucose (2-DG)) in combination with one or more compounds comprising one or more aromatic rings and at least one alkylamino.sub.(C≤12) group or substituted alkylamino.sub.(C≤12) group.

ANTIVIRAL THERAPEUTIC DRUG COMBINATIONS

Provided herein are compositions and methods for the treatment or prevention of viral infections via the use of chemical substances administered in a combinatory fashion for the suppression, inhibition, and elimination of viral loads. These compositions and methods use a glycolysis inhibitor (e.g., 2-deoxy-D-glucose (2-DG)) in combination with one or more compounds comprising one or more aromatic rings and at least one alkylamino.sub.(C≤12) group or substituted alkylamino.sub.(C≤12) group.

PHOSPHOLIPASE-A2 INHIBITORS FOR THE PREVENTION OF CANCER METASTASIS
20220265576 · 2022-08-25 ·

A compound of formula (I)


R-L-CO—X   (I)

wherein R is a C.sub.10-24 unsaturated hydrocarbon group optionally interrupted by one or more heteroatoms or groups of heteroatoms selected from S, O, N, SO, SO.sub.2, said hydrocarbon group comprising at least 4 non-conjugated double bonds;

L is a linking group forming a bridge of 1 to 5 atoms between the R group and the carbonyl CO wherein L comprises at least one heteroatom in the backbone of the linking group; and

X is an electron withdrawing group; or a salt thereof;

for use in the prevention of metastasis in cancer, especially breast cancer.

PHOSPHOLIPASE-A2 INHIBITORS FOR THE PREVENTION OF CANCER METASTASIS
20220265576 · 2022-08-25 ·

A compound of formula (I)


R-L-CO—X   (I)

wherein R is a C.sub.10-24 unsaturated hydrocarbon group optionally interrupted by one or more heteroatoms or groups of heteroatoms selected from S, O, N, SO, SO.sub.2, said hydrocarbon group comprising at least 4 non-conjugated double bonds;

L is a linking group forming a bridge of 1 to 5 atoms between the R group and the carbonyl CO wherein L comprises at least one heteroatom in the backbone of the linking group; and

X is an electron withdrawing group; or a salt thereof;

for use in the prevention of metastasis in cancer, especially breast cancer.

WOUND HEALING COMPOSITIONS INVOLVING MEDICINAL HONEY, MINERAL IONS AND METHYLGLYOXAL, AND METHODS OF USE
20170216369 · 2017-08-03 ·

The invention provides compositions based on either medicinal honey containing broad spectrum antibacterial activities of peroxide, polyphenols and methylglyoxal, or an effective amount of an active anti-inflammatory ingredient of mineral solids fortified with methylglyoxal antibacterial activity, or a mixture of both for the treatment of wounds; and methods of treating a wound, comprising contacting a wound with any one of the above compositions or a wound dressing containing any one of the above compositions.