C07C233/87

ANTI-TUMOR COMPOUND AND THE MEDICAL USE THEREOF
20170273933 · 2017-09-28 ·

The invention disclose a compound of formula (I), wherein, R.sub.1 is selected from —H or C1-C6 hydrocarbon group, —NH.sub.2, —OH, —O(CH.sub.2).sub.nCH.sub.3 (n=0, 1 or 2), —N(CH.sub.3).sub.2, or —CH.sub.2N(CH.sub.3).sub.2, R.sub.2 is selected from an amino acid

##STR00001##

or an hydroxy acid

##STR00002##

or —OH (R.sub.1, R.sub.2 are not —CH.sub.3 and —OH at the same time), wherein X, Y are

##STR00003##

—H, —CH.sub.3, —CH.sub.2OH, —CH(OH)CH.sub.3, —CH.sub.2SH, —CH(CH.sub.3).sub.2, —CH.sub.2CH(CH.sub.3).sub.2, —CH(CH.sub.3)CH.sub.2CH.sub.3, —CH.sub.2CH.sub.2SCH.sub.3, —CH.sub.2COOH, —CH.sub.2CONH.sub.2, —CH.sub.2CH.sub.2COOH, —CH.sub.2CH.sub.2CH.sub.2CH.sub.2NH.sub.2, or —CH.sub.2CH.sub.2CONH.sub.2, R.sub.3-R.sub.5 are H or C1-C6 hydrocarbon group. The compound has a low toxicity, can significantly inhibit the migration and invasion of tumor cells in vitro, and can inhibit tumor metastasis in vivo in mice at low concentration, while showing notable sensitizing effect on cytotoxic anti-tumor drugs such as Paclitaxel etc.

##STR00004##

ANTI-TUMOR COMPOUND AND THE MEDICAL USE THEREOF
20170273933 · 2017-09-28 ·

The invention disclose a compound of formula (I), wherein, R.sub.1 is selected from —H or C1-C6 hydrocarbon group, —NH.sub.2, —OH, —O(CH.sub.2).sub.nCH.sub.3 (n=0, 1 or 2), —N(CH.sub.3).sub.2, or —CH.sub.2N(CH.sub.3).sub.2, R.sub.2 is selected from an amino acid

##STR00001##

or an hydroxy acid

##STR00002##

or —OH (R.sub.1, R.sub.2 are not —CH.sub.3 and —OH at the same time), wherein X, Y are

##STR00003##

—H, —CH.sub.3, —CH.sub.2OH, —CH(OH)CH.sub.3, —CH.sub.2SH, —CH(CH.sub.3).sub.2, —CH.sub.2CH(CH.sub.3).sub.2, —CH(CH.sub.3)CH.sub.2CH.sub.3, —CH.sub.2CH.sub.2SCH.sub.3, —CH.sub.2COOH, —CH.sub.2CONH.sub.2, —CH.sub.2CH.sub.2COOH, —CH.sub.2CH.sub.2CH.sub.2CH.sub.2NH.sub.2, or —CH.sub.2CH.sub.2CONH.sub.2, R.sub.3-R.sub.5 are H or C1-C6 hydrocarbon group. The compound has a low toxicity, can significantly inhibit the migration and invasion of tumor cells in vitro, and can inhibit tumor metastasis in vivo in mice at low concentration, while showing notable sensitizing effect on cytotoxic anti-tumor drugs such as Paclitaxel etc.

##STR00004##

Carboxamide compounds

Compounds of the formula (I), in which the substituents are as defined in claim 1, are suitable for use as nematicides. ##STR00001##

Carboxamide compounds

Compounds of the formula (I), in which the substituents are as defined in claim 1, are suitable for use as nematicides. ##STR00001##

PPAR AGONISTS AND METHODS OF USE THEREOF

Provided herein are deuterated compounds and compositions useful in increasing PPARδ activity. The compounds and compositions provided herein are useful for the treatment of PPARδ related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).

COMPOUNDS FOR INHIBITION OF ALPHA 4 BETA 7 INTEGRIN

The present disclosure provides a compound of Formula (I):

##STR00001##

or a pharmaceutically acceptable salt thereof as described herein. The present disclosure also provides pharmaceutical compositions comprising a compound of Formula (I), processes for preparing compounds of Formula (I), and therapeutic methods for treating inflammatory disease.

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##

COMPOUNDS AND METHODS FOR TREATING INFLUENZA

A compound including a structure of Formula (I) and a preparation method thereof,

##STR00001##

wherein R.sub.1 is —OH, —CH.sub.2OH, or —OCOCH.sub.3; R.sub.2, R.sub.3, and R.sub.4 are independently —H, —CH.sub.3 or —F, and at least one of R.sub.2, R.sub.3, and R.sub.4 is —F. A method for treating a subject suffering from a viral disease includes administering an effective amount of said compound or a solvate thereof to the subject.

COMPOUNDS AND METHODS FOR TREATING INFLUENZA

A compound including a structure of Formula (I) and a preparation method thereof,

##STR00001##

wherein R.sub.1 is —OH, —CH.sub.2OH, or —OCOCH.sub.3; R.sub.2, R.sub.3, and R.sub.4 are independently —H, —CH.sub.3 or —F, and at least one of R.sub.2, R.sub.3, and R.sub.4 is —F. A method for treating a subject suffering from a viral disease includes administering an effective amount of said compound or a solvate thereof to the subject.

KDM4B INHIBITORS FOR THE TREATMENT OF INFLAMMATORY DISEASES AND DISORDERS
20220119344 · 2022-04-21 ·

The invention relates to KDM4B inhibitors, compositions comprising an effective amount of KDM4B inhibitors and methods for treating inflammatory diseases and disorders.