C07C233/58

Bicyclic-compounds for use as a medicament, in particular for treatment of parkinson's disease

The invention relates to novel small molecule compounds having a basic structure as depicted by formula (A), where in particular exemplary embodiments R.sup.1 is —OH, R.sup.2 is —NO.sub.2 and R.sup.3 is H, R.sup.4 and R.sup.5 are H, one of R.sup.6 and R.sup.7 is selected from H, —CONH.sub.2, and —CONR.sup.9.sub.2, and the other one is selected from —CONR.sup.9.sub.2 and —CONR.sup.11R.sup.9, wherein R.sup.9 and R.sup.11 are (possibly multiply) substituted alkyl and H or alkyl, respectively. The compounds of the invention inhibit the enzyme Catechol-O-methyltransferase (COMT) and exhibit a low off-target profile. The compounds are provided for use as a medicament, in particular for use in prevention or treatment of Parkinson's disease.

Physiological cooling compounds
10981862 · 2021-04-20 · ·

Physiological cooling compounds of the structure: ##STR00001##
where R.sub.1 is p-menthyl or 2,3,4-trimethylpent-3-yl group and R.sub.2-R.sub.8 are hydrogen or alkyl groups. The combination of R.sub.2-R.sub.8 is such that the N-alkyl group is a branched C.sub.5 alkyl or branched or linear C.sub.6-C.sub.8 alkyl group. The new carboxamides are valuable sensory ingredients which provide long-lasting cooling sensation and freshness in personal care, oral care, cosmetic products, pharmaceutical preparations, confectionary, food and beverages.

Physiological cooling compounds
10981862 · 2021-04-20 · ·

Physiological cooling compounds of the structure: ##STR00001##
where R.sub.1 is p-menthyl or 2,3,4-trimethylpent-3-yl group and R.sub.2-R.sub.8 are hydrogen or alkyl groups. The combination of R.sub.2-R.sub.8 is such that the N-alkyl group is a branched C.sub.5 alkyl or branched or linear C.sub.6-C.sub.8 alkyl group. The new carboxamides are valuable sensory ingredients which provide long-lasting cooling sensation and freshness in personal care, oral care, cosmetic products, pharmaceutical preparations, confectionary, food and beverages.

SOLVENT COMPOSITION FOR ELECTRONIC DEVICE PRODUCTION
20210115272 · 2021-04-22 · ·

The present invention provides a solvent composition for use in an ink for producing an electronic device using a printing method, the solvent composition being capable of improving the printing accuracy of the ink, being fired at low temperatures, and suppressing the amount of ash remaining after firing to a very low amount. The solvent composition for electronic device production of the present invention is for use in an ink for producing an electronic device by a printing method, and contains a miscible product of: a solvent and a compound represented by Formula (1) below. In Formula (1), R represents the same or different aliphatic hydrocarbon groups having 1 or more carbon atoms.

##STR00001##

SOLVENT COMPOSITION FOR ELECTRONIC DEVICE PRODUCTION
20210115272 · 2021-04-22 · ·

The present invention provides a solvent composition for use in an ink for producing an electronic device using a printing method, the solvent composition being capable of improving the printing accuracy of the ink, being fired at low temperatures, and suppressing the amount of ash remaining after firing to a very low amount. The solvent composition for electronic device production of the present invention is for use in an ink for producing an electronic device by a printing method, and contains a miscible product of: a solvent and a compound represented by Formula (1) below. In Formula (1), R represents the same or different aliphatic hydrocarbon groups having 1 or more carbon atoms.

##STR00001##

METHOD FOR SYNTHESIS OF DEUTERATED AMIDE AND DEUTERATED SULFONAMIDE
20210115009 · 2021-04-22 ·

A novel method for synthesizing deuterated amides and deuterated sulfonamides includes the following steps: (1) adding a compound M, DMAP, R.sup.3—X to a solvent to obtain a compound N after a reaction is complete; and (2) adding the compound N, R.sup.4—NH—R.sup.5, or a salt and base thereof to a solvent, and purifying after a reaction is complete to obtain a compound I.

##STR00001##

METHOD FOR SYNTHESIS OF DEUTERATED AMIDE AND DEUTERATED SULFONAMIDE
20210115009 · 2021-04-22 ·

A novel method for synthesizing deuterated amides and deuterated sulfonamides includes the following steps: (1) adding a compound M, DMAP, R.sup.3—X to a solvent to obtain a compound N after a reaction is complete; and (2) adding the compound N, R.sup.4—NH—R.sup.5, or a salt and base thereof to a solvent, and purifying after a reaction is complete to obtain a compound I.

##STR00001##

NOVEL COMPOUNDS ADVANTAGEOUS IN THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISEASES AND DISORDERS
20210130285 · 2021-05-06 ·

A series of novel amides showing broad pharmaceutical activity. Compounds described herein are effective as anticonvulsants, chemical countermeasures, and analgesics. Such compounds also show, neuroprotective/neuroreparative effects and activity against spinal muscular atrophy. Such pharmaceutically active compounds show utility in the treatment of central nervous system (CNS) diseases and disorders, such as anxiety, depression, insomnia, migraine headaches, schizophrenia, neurodegenerative diseases (e.g., Parkinson's disease, Alzheimer's, ALS, and Huntington's disease) spasticity, and bipolar disorder. Furthermore, such compounds may additionally find utility as analgesics (e.g., for the treatment of chronic or neuropathic pain) and as neuroprotective agents useful in the treatment of stroke(s), and/or traumatic brain and/or spinal cord injuries.

NOVEL COMPOUNDS ADVANTAGEOUS IN THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISEASES AND DISORDERS
20210130285 · 2021-05-06 ·

A series of novel amides showing broad pharmaceutical activity. Compounds described herein are effective as anticonvulsants, chemical countermeasures, and analgesics. Such compounds also show, neuroprotective/neuroreparative effects and activity against spinal muscular atrophy. Such pharmaceutically active compounds show utility in the treatment of central nervous system (CNS) diseases and disorders, such as anxiety, depression, insomnia, migraine headaches, schizophrenia, neurodegenerative diseases (e.g., Parkinson's disease, Alzheimer's, ALS, and Huntington's disease) spasticity, and bipolar disorder. Furthermore, such compounds may additionally find utility as analgesics (e.g., for the treatment of chronic or neuropathic pain) and as neuroprotective agents useful in the treatment of stroke(s), and/or traumatic brain and/or spinal cord injuries.

Modulators of Liver Receptor Homologue 1 (LRH-1) and Uses

This disclosure relates to modulators of liver receptor homologue 1 (LRH-1) and methods of managing disease and conditions related thereto. In certain embodiments, modulators are derivatives of hexahydropentalene. In certain embodiments, this disclosure relates to methods of treating or preventing cancer, diabetes, or cardiovascular disease by administering an effective amount of a hexahydropentalene derivative disclosed herein.