C07D239/84

FGFR4 inhibitor, preparation method therefor and pharmaceutical use thereof

Provided are an FGFR4 inhibitor having the structure of formula (I), and a preparation method therefor and the use thereof. The compound has a very strong inhibitory effect on FGFR4 kinase activity and has a very high selectivity, and can be widely used in the preparation of a drug for treating cancers, especially prostate cancer, liver cancer, pancreatic cancer, esophageal carcinomas, gastric cancer, lung cancer, breast cancer, ovarian carcinomas, colon cancer, skin cancer, glioblastomas or rhabdomyosarcomas, and is expected to be developed into a new generation of FGFR4 inhibitor drugs. ##STR00001##

FGFR4 inhibitor, preparation method therefor and pharmaceutical use thereof

Provided are an FGFR4 inhibitor having the structure of formula (I), and a preparation method therefor and the use thereof. The compound has a very strong inhibitory effect on FGFR4 kinase activity and has a very high selectivity, and can be widely used in the preparation of a drug for treating cancers, especially prostate cancer, liver cancer, pancreatic cancer, esophageal carcinomas, gastric cancer, lung cancer, breast cancer, ovarian carcinomas, colon cancer, skin cancer, glioblastomas or rhabdomyosarcomas, and is expected to be developed into a new generation of FGFR4 inhibitor drugs. ##STR00001##

Compositions and Methods for Treating Anxiety and Compulsive Behavior
20180002295 · 2018-01-04 ·

Provided herein is compositions and methods for treating anxiety, obsession and/or pathologically compulsive behavior associated with various neuropsychiatric diseases.

Compositions and Methods for Treating Anxiety and Compulsive Behavior
20180002295 · 2018-01-04 ·

Provided herein is compositions and methods for treating anxiety, obsession and/or pathologically compulsive behavior associated with various neuropsychiatric diseases.

INDENE DERIVATIVES USEFUL IN TREATING PAIN AND INFLAMMATION

Compounds of formula (I) wherein, R.sup.1, R.sup.2, R.sup.3, R.sup.4a, R.sup.4b and R.sup.5 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds are useful in treating inflammation and/or pain. Compositions comprising a compound of the invention are also disclosed, as are methods of using the compounds to treat inflammation and/or pain.

INDENE DERIVATIVES USEFUL IN TREATING PAIN AND INFLAMMATION

Compounds of formula (I) wherein, R.sup.1, R.sup.2, R.sup.3, R.sup.4a, R.sup.4b and R.sup.5 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds are useful in treating inflammation and/or pain. Compositions comprising a compound of the invention are also disclosed, as are methods of using the compounds to treat inflammation and/or pain.

A METHOD OF PRODUCING A CRYSTALLINE FORM OF SODIUM 2-[(4S)-8-FLUORO-2-[4-(3-METHOXYPHENYL)PIPERAZIN-1-YL]-3-[2-METHOXY-5-(TRIFLUOROMETHYL)PHENYL]-4H-QUINAZOLINE-4-YL]ACETATE TRIHYDRATE

The present invention refers to an effective method of preparing a crystalline form of 2-[(4S)-8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-[2-methoxy (trifluoromethyl)phenyl]-4H-quinazolin-4-yl]acetic acid sodium trihydrate.

A METHOD OF PRODUCING A CRYSTALLINE FORM OF SODIUM 2-[(4S)-8-FLUORO-2-[4-(3-METHOXYPHENYL)PIPERAZIN-1-YL]-3-[2-METHOXY-5-(TRIFLUOROMETHYL)PHENYL]-4H-QUINAZOLINE-4-YL]ACETATE TRIHYDRATE

The present invention refers to an effective method of preparing a crystalline form of 2-[(4S)-8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-[2-methoxy (trifluoromethyl)phenyl]-4H-quinazolin-4-yl]acetic acid sodium trihydrate.

Sodium 2-[(4S)-8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-4H-quinazolin-4-yl]acetate monohydrate, its preparation and use

The present invention relates to the novel 3,4-dihydroquinazoline sodium 2-[(4S)-8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-4H-quinazolin-4-yl]acetate monohydrate, methods of its preparation as well as pharmaceutical compositions containing said 3,4-dihydroquinazoline. Said compound is particularly useful for treatment and prevention of diseases associated with cytomegalovirus (CMV), particularly human cytomegalovirus (HCMV).

Sodium 2-[(4S)-8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-4H-quinazolin-4-yl]acetate monohydrate, its preparation and use

The present invention relates to the novel 3,4-dihydroquinazoline sodium 2-[(4S)-8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-4H-quinazolin-4-yl]acetate monohydrate, methods of its preparation as well as pharmaceutical compositions containing said 3,4-dihydroquinazoline. Said compound is particularly useful for treatment and prevention of diseases associated with cytomegalovirus (CMV), particularly human cytomegalovirus (HCMV).