C07C257/18

NOVEL NAMPT ENZYME AGONIST AND PREPARATION AND USE THEREOF

The present invention provides a class of novel NAMPT enzyme agonist and preparation and use thereof, which has a structural formula as shown in formula I or formula II. The present invention screens the NAMPT agonist NAT from the chemical small molecule library, and the NAT exhibits a good cytoprotective effect and a good anti-neurodegeneration effect in animal models of neurodegeneration. We studied the binding of NAT to enzymes, and then carried out multiple rounds of structure optimization based on the chemical structure characteristics of NAT and its enzyme activity properties, and obtained a relatively defined structure-activity relationship. The present patent not only lays the foundation for developing innovative drugs for anti-aging and neurodegenerative diseases, but also theoretically provides a proof-of-concept that enhancing NAMPT enzyme activity plays an important role in neuroprotection.

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MASP-2 INHIBITORS AND METHODS OF USE

The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds and methods of making and using such compounds.

STROMAL DERIVED FACTOR INHIBITION AND CXCR4 BLOCKADE
20190322633 · 2019-10-24 ·

The invention relates to inhibition of SDF-1 expression in subacromial bursa cells by CXCR-4 inhibitors. Bursal cell migration in response to SDF- stimulation is also decreased in the presence of CXCR4 inhibitors. Accordingly, provided are methods for treating or ameliorating a musculoskeletal disorder.

STROMAL DERIVED FACTOR INHIBITION AND CXCR4 BLOCKADE
20190322633 · 2019-10-24 ·

The invention relates to inhibition of SDF-1 expression in subacromial bursa cells by CXCR-4 inhibitors. Bursal cell migration in response to SDF- stimulation is also decreased in the presence of CXCR4 inhibitors. Accordingly, provided are methods for treating or ameliorating a musculoskeletal disorder.

PHENYLAMIDINES AND THE USE THEREOF AS FUNGICIDES

The present invention relates to compounds of the formula (I), in particular to phenylamidines of the formula (I), to a process for their preparation, to the use of phenylamidines of the formula (I) according to the invention for controlling unwanted microorganisms, in particular phytopathogenic fungi and also to a composition for this purpose, comprising the phenylamidines of the formula (I) according to the invention. Furthermore, the invention relates to a method for controlling unwanted microorganisms, in particular phytopathogenic fungi, characterized in that the compounds of the formula (I) are applied to the microorganisms, in particular to the phytopathogenic fungi and/or in their habitat.

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PHENYLAMIDINES AND THE USE THEREOF AS FUNGICIDES

The present invention relates to compounds of the formula (I), in particular to phenylamidines of the formula (I), to a process for their preparation, to the use of phenylamidines of the formula (I) according to the invention for controlling unwanted microorganisms, in particular phytopathogenic fungi and also to a composition for this purpose, comprising the phenylamidines of the formula (I) according to the invention. Furthermore, the invention relates to a method for controlling unwanted microorganisms, in particular phytopathogenic fungi, characterized in that the compounds of the formula (I) are applied to the microorganisms, in particular to the phytopathogenic fungi and/or in their habitat.

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LINKED DIARYL COMPOUNDS WITH ANTICANCER PROPERTIES AND METHODS OF USING THE SAME
20190209548 · 2019-07-11 ·

Provided are compositions comprising linked diaryl compounds that possess anticancer properties. Methods of use are also disclosed herein. The method comprises administering an effective amount of a compound described herein to an individual in need thereof.

LINKED DIARYL COMPOUNDS WITH ANTICANCER PROPERTIES AND METHODS OF USING THE SAME
20190209548 · 2019-07-11 ·

Provided are compositions comprising linked diaryl compounds that possess anticancer properties. Methods of use are also disclosed herein. The method comprises administering an effective amount of a compound described herein to an individual in need thereof.

Process for the manufacture of 4-aminobenzoamidine dihydrochloride

The present invention relates to a process for the preparation of 4-aminobenzoamidine (4-AMBA) salts of general formula (I) ##STR00001##
preferably the salts thereof with hydrochloric or hydrobromic acid, particularly preferred the dichloride salt.

Process for the manufacture of 4-aminobenzoamidine dihydrochloride

The present invention relates to a process for the preparation of 4-aminobenzoamidine (4-AMBA) salts of general formula (I) ##STR00001##
preferably the salts thereof with hydrochloric or hydrobromic acid, particularly preferred the dichloride salt.