C07C235/40

Indene derivatives and uses thereof

The present invention relates to compounds of formula (I): including any stereochemically isomeric form thereof, or pharmaceutically acceptable salts thereof, for the treatment of, for example, cancer.

SSAO INHIBITORS AND USES THEREOF

Described herein are compounds that are semicarbazide-sensitive amine oxidase (SSAO) inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in treating or preventing a liver disease or condition.

Process for the preparation of an amino-pyrimidine and intermediates thereof

Provided herein is a novel process for the preparation of an amino-pyrimidine and salts thereof. Also provided herein are novel intermediates used in this process and their preparation.

Process for the preparation of an amino-pyrimidine and intermediates thereof

Provided herein is a novel process for the preparation of an amino-pyrimidine and salts thereof. Also provided herein are novel intermediates used in this process and their preparation.

A PROCESS METHOD FOR PRODUCING PESTICIDE BY USING CARBON DIOXIDE
20210269390 · 2021-09-02 ·

A process method for producing pesticide by using carbon dioxide comprises the following steps: Weighing 1, 3-cyclohexanedione substrate, catalyst and Cs2CO3 in Schleck bottle, degassing, and continuously introducing 1 atm of carbon dioxide. Add solvent and react for 48 h in an oil bath at 50° C. After the reaction was completed, post-treatment was carried out to obtain 2(a-e). The obtained acid is acylated and then added dropwise to dichloromethane solution containing aniline to react for 2 h at normal temperature. After the reaction, column chromatography was performed to obtain 3(a-e). Add 3 (a-e) into 50% concentrated sulfuric acid and reflux at 80° C. for 8 hours. Through separation, 4(a-e) was obtained. The invention has the advantages that the catalyst is simple to prepare, has high catalytic activity, can be recycled, realizes industrial circulation, and achieves the goal of sustainable production. The preparation process of 3(a-e) and 4 (a-e) is simple, with low requirements on equipment, wide sources of raw materials, low cost, low toxicity and easy industrial scale-up production.

A PROCESS METHOD FOR PRODUCING PESTICIDE BY USING CARBON DIOXIDE
20210269390 · 2021-09-02 ·

A process method for producing pesticide by using carbon dioxide comprises the following steps: Weighing 1, 3-cyclohexanedione substrate, catalyst and Cs2CO3 in Schleck bottle, degassing, and continuously introducing 1 atm of carbon dioxide. Add solvent and react for 48 h in an oil bath at 50° C. After the reaction was completed, post-treatment was carried out to obtain 2(a-e). The obtained acid is acylated and then added dropwise to dichloromethane solution containing aniline to react for 2 h at normal temperature. After the reaction, column chromatography was performed to obtain 3(a-e). Add 3 (a-e) into 50% concentrated sulfuric acid and reflux at 80° C. for 8 hours. Through separation, 4(a-e) was obtained. The invention has the advantages that the catalyst is simple to prepare, has high catalytic activity, can be recycled, realizes industrial circulation, and achieves the goal of sustainable production. The preparation process of 3(a-e) and 4 (a-e) is simple, with low requirements on equipment, wide sources of raw materials, low cost, low toxicity and easy industrial scale-up production.

COMPOUNDS USEFUL FOR IN VIVO IMAGING OF PROTEIN OXIDATION AND/OR CANCER TREATMENT
20210299285 · 2021-09-30 ·

Provided herein are compounds of Formula I, Formula II Formula III which are useful in labeling tissues in a subject (e.g., PET imaging of a subject), for treatment of cancer, and/or for preparing a medicament. Also provided are compounds containing a group that is reactive with sulfenylated proteins for treatment of cancer and/or for preparing a medicament. Methods of synthesis of the compounds and precursor compounds are also provided.

COMPOUNDS USEFUL FOR IN VIVO IMAGING OF PROTEIN OXIDATION AND/OR CANCER TREATMENT
20210299285 · 2021-09-30 ·

Provided herein are compounds of Formula I, Formula II Formula III which are useful in labeling tissues in a subject (e.g., PET imaging of a subject), for treatment of cancer, and/or for preparing a medicament. Also provided are compounds containing a group that is reactive with sulfenylated proteins for treatment of cancer and/or for preparing a medicament. Methods of synthesis of the compounds and precursor compounds are also provided.

ANTI-FIBROTIC COMPOUNDS

Provided herein are anti-fibrotic compounds, in particular those of Formula (I), that inhibit the TGF-beta signaling pathway. Also provided are pharmaceutical compositions comprising the anti-fibrotic compounds, and methods of treating diseases or conditions associated with fibrosis, inflammation, and benign or malignant neoplastic diseases in a subject by administering a compound or composition described herein.

ENANTIOMERICALLY PURE ADAMANTANE CARBOXAMIDES FOR THE TREATMENT OF FILOVIRUS INFECTION

The compounds of the invention as shown by general structure I, as shown below, are effective in treating filovirus infections.

##STR00001## X is selected from the group consisting of O and H; R.sup.1 is selected from (C.sub.6 to C.sub.10) aryl and (C.sub.2 to C.sub.9) heteroaryl, and R.sup.2 is selected from (C.sub.1 to C.sub.10) alkyl, (C.sub.1 to C.sub.10) alkenyl, (C.sub.1 to C.sub.10) alkynyl, (C.sub.3 to C.sub.10) cycloalkyl, and (C.sub.5 to C.sub.10) cycloalkenyl, and NR.sup.3aR.sup.3b is defined in the specification.

These compounds are effective in treating filovirii infections including Ebolavirus and Marburg virus.