C07C229/08

CRYSTAL OF 1,3,5-TRIAZINE DERIVATIVE OR SOLVATE THEREOF AND METHOD FOR PRODUCING SAME

A crystal of a 1,3,5-triazine derivative or a solvate thereof, and a method for producing the same are provided. The present invention relates to a crystal of a compound represented by Formula (I) or a solvate thereof:

##STR00001## and relates to a pharmaceutical composition containing the same. The present invention also relates to a crystal of a compound represented by Formula (I), or a solvate thereof.

Nitrogen-containing Derivative of Substituted Phenol Hydroxy Acid Ester, and Preparation and Use Thereof
20220388947 · 2022-12-08 ·

A nitrogen-containing derivative of substituted phenol hydroxyl acid ester is represented by formula (I). A salt of the compound of formula (I) has good water solubility, and in vivo, can rapidly and completely release substituted phenols having a pharmacological effect, which can improve the water solubility of substituted phenols, rapidly exert the pharmacological effects of substituted phenols in vivo, and has good safety. The method for preparing the above-mentioned compound is provided. This compound can also be used in the preparation of drugs that produce anaesthesia and/or sedative and hypnotic effects on humans and animals.

##STR00001##

Nitrogen-containing Derivative of Substituted Phenol Hydroxy Acid Ester, and Preparation and Use Thereof
20220388947 · 2022-12-08 ·

A nitrogen-containing derivative of substituted phenol hydroxyl acid ester is represented by formula (I). A salt of the compound of formula (I) has good water solubility, and in vivo, can rapidly and completely release substituted phenols having a pharmacological effect, which can improve the water solubility of substituted phenols, rapidly exert the pharmacological effects of substituted phenols in vivo, and has good safety. The method for preparing the above-mentioned compound is provided. This compound can also be used in the preparation of drugs that produce anaesthesia and/or sedative and hypnotic effects on humans and animals.

##STR00001##

Metformin amino acid compounds and methods of using the same

The present invention relates to metformin amino acid compounds (SLNs), pharmaceutical compositions thereof, and methods of using them for the treatment of hyperglycemia, diabetes, and Type 2 diabetes. The compounds can be synthesized using the processes disclosed herein.

Use of stereoselective transaminase in asymmetric synthesis of chiral amine

Use of a stereoselective transaminase in the asymmetric synthesis of a chiral amine. In particular, provided is use of a polypeptide in the production of a chiral amine or a downstream product using a chiral amine as a precursor. Further provided is a method for producing a chiral amine, comprising culturing a strain expressing the polypeptide so as to obtain a chiral amine. Further provided are a chiral amine production strain and a method for constructing the chiral amine production strain. The stereoselective transaminase has a broad substrate spectrum and thus has a broad application potential in the preparation of a chiral amine.

Use of stereoselective transaminase in asymmetric synthesis of chiral amine

Use of a stereoselective transaminase in the asymmetric synthesis of a chiral amine. In particular, provided is use of a polypeptide in the production of a chiral amine or a downstream product using a chiral amine as a precursor. Further provided is a method for producing a chiral amine, comprising culturing a strain expressing the polypeptide so as to obtain a chiral amine. Further provided are a chiral amine production strain and a method for constructing the chiral amine production strain. The stereoselective transaminase has a broad substrate spectrum and thus has a broad application potential in the preparation of a chiral amine.

PICOLINAMIDES AS FUNGICIDES

This disclosure relates to picolinamides of Formula I and their use as fungicides.

##STR00001##

DNP and DNP Prodrug Treatment of Neuromuscular, Neurodegenerative, Autoimmune, Developmental, Traumatic Brain Injury, Concussion, Dry Eye Disease, Hearing Loss and/or Metabolic Diseases

A composition and method of treatment of neuromuscular, neuromuscular degenerative, neurodegenerative, autoimmune, developmental, traumatic, hearing loss related, and/or metabolic diseases, including spinal muscular atrophy (SMA) syndrome (SMA1, SMA2, SMA3, and SMA4, also called Type I, II, III and IV), traumatic brain injury (TBI), concussion, keratoconjunctivitis sicca (Dry Eye Disease), glaucoma, Sjogren's syndrome, rheumatoid arthritis, post-LASIK surgery, anti-depressants use, Wolfram Syndrome, and Wolcott-Rallison syndrome. The composition is selected from the group consisting of 2,3-DNP, 2,4-DNP, 2,5-DNP, 2,6-DNP, 3,4-DNP, or 3,5-DNP, bipartite 2,3-dinitrophenol, 2,4-dinitrophenol, 2,5-dinitrophenol, 2,6-dinitrophenol, 3,4-dinitrophenol, or 3,5-dinitrophenol (2,3-DNP, 2,4-DNP, 2,5-DNP, 2,6-DNP, 3,4-DNP, or 3,5-DNP) prodrugs; Gemini prodrugs, bioprecursor molecules, and combinations thereof. A dose of the composition for treatment of neurodegenerative diseases may be from about 0.01 mg/kg of body weight to about 50 mg/kg of body weight of the patient in need of treatment. A dose of the composition for treatment of metabolic diseases may be from about 1 mg/70 kg of body weight to about 100 mg/70 kg of body weight of the patient in need of treatment, and a maximum dose per day is about 200 mg/70 kg of body weight of the patient in need of treatment.

DNP and DNP Prodrug Treatment of Neuromuscular, Neurodegenerative, Autoimmune, Developmental, Traumatic Brain Injury, Concussion, Dry Eye Disease, Hearing Loss and/or Metabolic Diseases

A composition and method of treatment of neuromuscular, neuromuscular degenerative, neurodegenerative, autoimmune, developmental, traumatic, hearing loss related, and/or metabolic diseases, including spinal muscular atrophy (SMA) syndrome (SMA1, SMA2, SMA3, and SMA4, also called Type I, II, III and IV), traumatic brain injury (TBI), concussion, keratoconjunctivitis sicca (Dry Eye Disease), glaucoma, Sjogren's syndrome, rheumatoid arthritis, post-LASIK surgery, anti-depressants use, Wolfram Syndrome, and Wolcott-Rallison syndrome. The composition is selected from the group consisting of 2,3-DNP, 2,4-DNP, 2,5-DNP, 2,6-DNP, 3,4-DNP, or 3,5-DNP, bipartite 2,3-dinitrophenol, 2,4-dinitrophenol, 2,5-dinitrophenol, 2,6-dinitrophenol, 3,4-dinitrophenol, or 3,5-dinitrophenol (2,3-DNP, 2,4-DNP, 2,5-DNP, 2,6-DNP, 3,4-DNP, or 3,5-DNP) prodrugs; Gemini prodrugs, bioprecursor molecules, and combinations thereof. A dose of the composition for treatment of neurodegenerative diseases may be from about 0.01 mg/kg of body weight to about 50 mg/kg of body weight of the patient in need of treatment. A dose of the composition for treatment of metabolic diseases may be from about 1 mg/70 kg of body weight to about 100 mg/70 kg of body weight of the patient in need of treatment, and a maximum dose per day is about 200 mg/70 kg of body weight of the patient in need of treatment.

Biologically active cannabidiol analogs

Biologically active cannabidiol analogs comprising a compound of the formula ##STR00001##
wherein one of R.sub.1 or R.sub.2 or both is/are the residue of a moiety formed by the reaction of an amino group of the amino acid ester of R.sub.1 or R.sub.2 or both with a dicarboxylic acid or a dicarboxylic acid derivative and the other R.sub.1 or R.sub.2 (in the case of the mono) is the residue of a dicarboxylic acid or dicarboxylic acid derivative or Hydrogen (H), (i.e. underivatized), and salts thereof. These CBD analogs are be useful in pain management in oncology and other clinical settings in which neuropathy is presented. Furthermore, these CBD-analogs are useful in blocking the addictive properties of opiates.