C07C237/24

SUBSTITUTED CYCLOHEXYL COMPOUNDS AS NOP INHIBITORS

Substituted cyclohexyl chemical entities of Formula (I):

##STR00001## wherein R.sup.a, G, and R.sup.b have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive therapies; modulating and treating disorders mediated by nociceptin activity or dopamine signaling; treating neurological disorders, neurodegenerative diseases, depression, and schizophrenia; enhancing the efficiency of cognitive and motor training; and treating peripheral disorders, including renal, respiratory, gastrointestinal, liver, genitourinary, metabolic, and inflammatory disorders.

CYCLIC DIONES AS HERBICIDAL COMPOUNDS

The present invention relates to compounds of Formula (I), wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4x, R.sup.4y, m, n and G are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I), to their use for controlling weeds, in particular in crops of useful plants.

##STR00001##

CYCLIC DIONES AS HERBICIDAL COMPOUNDS

The present invention relates to compounds of Formula (I), wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4x, R.sup.4y, m, n and G are as defined herein. The invention further relates to herbicidal compositions which comprise a compound of Formula (I), to their use for controlling weeds, in particular in crops of useful plants.

##STR00001##

Hypocrellin derivative substituted both in a peri-position and in 2-position by amino, preparation method, and application thereof

The present invention discloses a hypocrellin derivative substituted both in a pen-position and in a 2-position by an amino, and a preparation method and use thereof. A general structural formula of the derivative is as represented by formulas I-a to I-d: ##STR00001## The hypocrellin derivative substituted both in a peri-position and in a 2-position by an amino prepared in the present invention has a maximum absorption wavelength of 600-650 nm and a molar extinction coefficient reaching about 20000-40000 M.sup.−1cm.sup.−1. Compared with unmodified hypocrellin or hypocrellin having only a 2-position modified, an absorption spectrum of the derivative is significantly red-shifted and the molar extinction coefficient is greatly improved, and the derivative can efficiently produce reactive oxygen species such as singlet oxygen in a photosensitive condition. In the same condition, the hypocrellin derivative substituted both in a pen-position and in a 2-position by an amino involved in the present invention, when used as a photosensitizer, has a stronger ability to photo-dynamically inactivate tumor cells than the first and second generation commercial photosensitizers.

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.

MODULATORS OF THE INTEGRATED STRESS PATHWAY

Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions.

HYPOCRELLIN DERIVATIVE SUBSTITUTED BOTH IN A PERI-POSITION AND IN 2-POSITION BY AMINO, PREPARATION METHOD, AND APPLICATION THEREOF

The present invention discloses a hypocrellin derivative substituted both in a peri-position and in a 2-position by an amino, and a preparation method and use thereof. A general structural formula of the derivative is as represented by formulas I-a to I-d:

##STR00001##

The hypocrellin derivative substituted both in a peri-position and in a 2-position by an amino prepared in the present invention has a maximum absorption wavelength of 600-650 nm and a molar extinction coefficient reaching about 20000-40000 M.sup.−1cm.sup.−1. Compared with unmodified hypocrellin or hypocrellin having only a 2-position modified, an absorption spectrum of the derivative is significantly red-shifted and the molar extinction coefficient is greatly improved, and the derivative can efficiently produce reactive oxygen species such as singlet oxygen in a photosensitive condition. In the same condition, the hypocrellin derivative substituted both in a peri-position and in a 2-position by an amino involved in the present invention, when used as a photosensitizer, has a stronger ability to photo-dynamically inactivate tumor cells than the first and second generation commercial photosensitizers.

NOVEL SUBSTITUTED CYCLOBUTYLBENZENE COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE (IDO) INHIBITORS

Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: (Formula (I)). Also disclosed herein are uses of a compound disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of a composition in the potential treatment or prevention of an IDO-associated disease or disorder.

##STR00001##

Agonists of protein tyrosine phosphatase SHP-1
10745346 · 2020-08-18 ·

Some novel compounds are provided in this disclosure. These novel compounds have potential SHP-1 agonist activity for being used in treating cancer.