C07C279/08

THERAPEUTIC COMPOUNDS
20180230105 · 2018-08-16 ·

The invention provides compounds of formula Ia, Ib, Ic, and Id:

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and pharmaceutically acceptable salts thereof, wherein the variables A, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.x, L, X, Y, and Z have the meaning as described herein. The compounds are useful for reducing endoplasmic reticulum stress and for producing analgesia in an animal.

Salty taste-enhancing agent and manufacturing method therefor, and salty taste-enhancing method

An object of the present invention is to provide a novel salty taste-enhancing agent and production method therefor, and salty taste-enhancing method for a food and beverage. As means for achieving such object, provided is a salty taste-enhancing agent.

Salty taste-enhancing agent and manufacturing method therefor, and salty taste-enhancing method

An object of the present invention is to provide a novel salty taste-enhancing agent and production method therefor, and salty taste-enhancing method for a food and beverage. As means for achieving such object, provided is a salty taste-enhancing agent.

Ligands for imaging cardiac innervation

Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release (thereby reducing side effects), improved quantitative data, and/or high affinity for VMAT over prior radiotracers. Methods of using the compounds to image cardiac innervation are also provided. In some instances the compounds are developed by derivatizing certain compounds with 18F in a variety of positions: aryl, alkyl, a keto, benzylic, beta-alkylethers, gamma-propylalkylethers and beta-proplylalkylethers. Alternatively or additionally, a methyl group a is added to the amine, and/or the catechol functionality is either eliminated or masked as a way of making these compounds more stable.

Ligands for imaging cardiac innervation

Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release (thereby reducing side effects), improved quantitative data, and/or high affinity for VMAT over prior radiotracers. Methods of using the compounds to image cardiac innervation are also provided. In some instances the compounds are developed by derivatizing certain compounds with 18F in a variety of positions: aryl, alkyl, a keto, benzylic, beta-alkylethers, gamma-propylalkylethers and beta-proplylalkylethers. Alternatively or additionally, a methyl group a is added to the amine, and/or the catechol functionality is either eliminated or masked as a way of making these compounds more stable.

ALKOXY COMPOUNDS FOR DISEASE TREATMENT

The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

ALKOXY COMPOUNDS FOR DISEASE TREATMENT

The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

Biguanide derivative, a preparation method thereof, and a pharmaceutical composition containing the biguanide derivative as an active ingredient

A biguanide derivative compound with N1-N5 substitution, which is represented by Formula 1, or a pharmaceutically acceptable salt thereof a method of preparing the same, and a pharmaceutical composition containing the same as an active ingredient are provided. The biguanide derivative may exhibit excellent effect on activation of AMPK and inhibition of cancer cell proliferation in a low dose, compared to conventional drugs, and thus, may be useful to treat diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovarian syndrome, metabolic syndrome, cancer, etc.

Biguanide derivative, a preparation method thereof, and a pharmaceutical composition containing the biguanide derivative as an active ingredient

A biguanide derivative compound with N1-N5 substitution, which is represented by Formula 1, or a pharmaceutically acceptable salt thereof a method of preparing the same, and a pharmaceutical composition containing the same as an active ingredient are provided. The biguanide derivative may exhibit excellent effect on activation of AMPK and inhibition of cancer cell proliferation in a low dose, compared to conventional drugs, and thus, may be useful to treat diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovarian syndrome, metabolic syndrome, cancer, etc.

GUANICIDE COMPOUND AND FUNGICIDE

A novel guanidine compound having excellent fungicidal activity is represented by formula [I]. (In the formula, Y represents a divalent group represented by formula [II] (wherein each of R.sup.7-R.sup.9 independently represents a hydrogen atom or the like) or the like; each of X and Z independently represents an unsubstituted or substituted alkylene group or the like; each of Q.sup.1 and Q.sup.2 independently represents a single bond or the like; each of A.sup.1 and A.sup.2 independently represents an unsubstituted or substituted divalent heterocyclic compound residue or the like; and each of R.sup.1-R.sup.6 independently represents a hydrogen atom or the like.)

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