Patent classifications
C07C255/53
PROCESS FOR THE PREPARATION OF 4,5-DIHYDROXY-2-(4-METHYLBENZYL)ISOPHTHALONITRILE
The present disclosure relates to a process for the preparation of 4,5-dihydroxy-2-(4-methylbenzyl)isophthalonitrile, to use of a compound which is 2-methoxy-5-(4-methylbenzyl)phenol, (3-hydroxy-4-methoxyphenyl)(p-tolyl)methanone, 2-methoxy-5-(4-methylbenzoyl)phenyl 2-chloroacetate, 4-methylbenzoyl chloride, 2-methoxyphenyl 2-chloroacetate or 2-methoxyphenol in the preparation of 4,5-dihydroxy-2-(4-methylbenzyl)isophthalonitrile and to a compound which is 4-hydroxy-5-methoxy-2-(4-methylbenzyl)isophthalaldehyde dioxime or 4-hydroxy-5-methoxy-2-(4-methylbenzyl)isophthalaldehyde and use thereof in the preparation of 4,5-dihydroxy-2-(4-methylbenzyl)isophthalonitrile. 4,5-Dihydroxy-2-(4-methylbenzyl)isophthalonitrile is a COMT inhibitor.
PROCESS FOR THE PREPARATION OF 4,5-DIHYDROXY-2-(4-METHYLBENZYL)ISOPHTHALONITRILE
The present disclosure relates to a process for the preparation of 4,5-dihydroxy-2-(4-methylbenzyl)isophthalonitrile, to use of a compound which is 2-methoxy-5-(4-methylbenzyl)phenol, (3-hydroxy-4-methoxyphenyl)(p-tolyl)methanone, 2-methoxy-5-(4-methylbenzoyl)phenyl 2-chloroacetate, 4-methylbenzoyl chloride, 2-methoxyphenyl 2-chloroacetate or 2-methoxyphenol in the preparation of 4,5-dihydroxy-2-(4-methylbenzyl)isophthalonitrile and to a compound which is 4-hydroxy-5-methoxy-2-(4-methylbenzyl)isophthalaldehyde dioxime or 4-hydroxy-5-methoxy-2-(4-methylbenzyl)isophthalaldehyde and use thereof in the preparation of 4,5-dihydroxy-2-(4-methylbenzyl)isophthalonitrile. 4,5-Dihydroxy-2-(4-methylbenzyl)isophthalonitrile is a COMT inhibitor.
Tetralin and tetrahydroquinoline compounds as inhibitors of HIF-2alpha
- Joel Worley BEATTY ,
- Samuel Lawrie DREW ,
- Matthew Epplin ,
- Jeremy Thomas Andre FOURNIER ,
- Balint GAL ,
- Tezcan GUNEY ,
- Karl T. Haelsig ,
- Clayton HARDMAN ,
- Steven Donald JACOB ,
- Jenna Leigh JEFFREY ,
- Jaroslaw KALISIAK ,
- Kenneth Victor LAWSON ,
- Manmohan Reddy LELETI ,
- Erick Allen LINDSEY ,
- Artur Karenovich MAILYAN ,
- Debashis MANDAL ,
- Guillaume MATA ,
- Hyunyoung Moon ,
- Jay Patrick POWERS ,
- Brandon Reid ROSEN ,
- Yongli Su ,
- Anh Thu TRAN ,
- Zhang Wang ,
- Xuelei Yan ,
- Kai YU
Compounds that inhibit HIF-2α, and compositions containing the compound(s) and methods for synthesizing the compounds, are described herein. Also described are the use of such compounds and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by HIF-2α.
Tetralin and tetrahydroquinoline compounds as inhibitors of HIF-2alpha
- Joel Worley BEATTY ,
- Samuel Lawrie DREW ,
- Matthew Epplin ,
- Jeremy Thomas Andre FOURNIER ,
- Balint GAL ,
- Tezcan GUNEY ,
- Karl T. Haelsig ,
- Clayton HARDMAN ,
- Steven Donald JACOB ,
- Jenna Leigh JEFFREY ,
- Jaroslaw KALISIAK ,
- Kenneth Victor LAWSON ,
- Manmohan Reddy LELETI ,
- Erick Allen LINDSEY ,
- Artur Karenovich MAILYAN ,
- Debashis MANDAL ,
- Guillaume MATA ,
- Hyunyoung Moon ,
- Jay Patrick POWERS ,
- Brandon Reid ROSEN ,
- Yongli Su ,
- Anh Thu TRAN ,
- Zhang Wang ,
- Xuelei Yan ,
- Kai YU
Compounds that inhibit HIF-2α, and compositions containing the compound(s) and methods for synthesizing the compounds, are described herein. Also described are the use of such compounds and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by HIF-2α.
TETRALIN AND TETRAHYDROQUINOLINE COMPOUNDS AS INHIBITORS OF HIF-2ALPHA
- Joel Worley BEATTY ,
- Samuel Lawrie DREW ,
- Matthew Epplin ,
- Jeremy Thomas Andre FOURNIER ,
- Balint GAL ,
- Tezcan GUNEY ,
- Karl T. Haelsig ,
- Clayton HARDMAN ,
- Steven Donald JACOB ,
- Jenna Leigh JEFFREY ,
- Jaroslaw KALISIAK ,
- Kenneth Victor LAWSON ,
- Manmohan Reddy LELETI ,
- Erick Allen LINDSEY ,
- Artur Karenovich MAILYAN ,
- Debashis MANDAL ,
- Guillaume MATA ,
- Hyunyoung Moon ,
- Jay Patrick POWERS ,
- Brandon Reid ROSEN ,
- Yongli Su ,
- Anh Thu TRAN ,
- Zhang Wang ,
- Xuelei Yan ,
- Kai YU
Compounds that inhibit HIF-2α, and compositions containing the compound(s) and methods for synthesizing the compounds, are described herein. Also described are the use of such compounds and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by HIF-2α.
TETRALIN AND TETRAHYDROQUINOLINE COMPOUNDS AS INHIBITORS OF HIF-2ALPHA
- Joel Worley BEATTY ,
- Samuel Lawrie DREW ,
- Matthew Epplin ,
- Jeremy Thomas Andre FOURNIER ,
- Balint GAL ,
- Tezcan GUNEY ,
- Karl T. Haelsig ,
- Clayton HARDMAN ,
- Steven Donald JACOB ,
- Jenna Leigh JEFFREY ,
- Jaroslaw KALISIAK ,
- Kenneth Victor LAWSON ,
- Manmohan Reddy LELETI ,
- Erick Allen LINDSEY ,
- Artur Karenovich MAILYAN ,
- Debashis MANDAL ,
- Guillaume MATA ,
- Hyunyoung Moon ,
- Jay Patrick POWERS ,
- Brandon Reid ROSEN ,
- Yongli Su ,
- Anh Thu TRAN ,
- Zhang Wang ,
- Xuelei Yan ,
- Kai YU
Compounds that inhibit HIF-2α, and compositions containing the compound(s) and methods for synthesizing the compounds, are described herein. Also described are the use of such compounds and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by HIF-2α.
FLUORESCENT DYE, PREPARATION METHOD AND USES THEREOF
A fluorescent dye, as well as a preparation method and uses thereof, wherein the fluorescent dye is sensitive and specific to viscosity and has low background fluorescence; it can also be used as a fluorescent activated and lighted probe used for fluorescent labeling, quantification or monitoring of protein, enzymes or nucleic acid.
Tetralin and tetrahydroquinoline compounds as inhibitors of HIF-2α
- Joel Worley BEATTY ,
- Samuel Lawrie DREW ,
- Matthew Epplin ,
- Jeremy Thomas Andre FOURNIER ,
- Balint GAL ,
- Tezcan GUNEY ,
- Karl T. Haelsig ,
- Clayton HARDMAN ,
- Steven Donald JACOB ,
- Jenna Leigh JEFFREY ,
- Jaroslaw KALISIAK ,
- Kenneth Victor LAWSON ,
- Manmohan Reddy LELETI ,
- Erick Allen LINDSEY ,
- Artur Karenovich MAILYAN ,
- Debashis MANDAL ,
- Guillaume MATA ,
- Hyunyoung Moon ,
- Jay Patrick Powers ,
- Brandon Reid ROSEN ,
- Yongli Su ,
- Anh Thu TRAN ,
- Zhang Wang ,
- Xuelei Yan ,
- Kai YU
Compounds that inhibit HIF-2α, and compositions containing the compound(s) and methods for synthesizing the compounds, are described herein. Also described are the use of such compounds and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by HIF-2α.
Tetralin and tetrahydroquinoline compounds as inhibitors of HIF-2α
- Joel Worley BEATTY ,
- Samuel Lawrie DREW ,
- Matthew Epplin ,
- Jeremy Thomas Andre FOURNIER ,
- Balint GAL ,
- Tezcan GUNEY ,
- Karl T. Haelsig ,
- Clayton HARDMAN ,
- Steven Donald JACOB ,
- Jenna Leigh JEFFREY ,
- Jaroslaw KALISIAK ,
- Kenneth Victor LAWSON ,
- Manmohan Reddy LELETI ,
- Erick Allen LINDSEY ,
- Artur Karenovich MAILYAN ,
- Debashis MANDAL ,
- Guillaume MATA ,
- Hyunyoung Moon ,
- Jay Patrick Powers ,
- Brandon Reid ROSEN ,
- Yongli Su ,
- Anh Thu TRAN ,
- Zhang Wang ,
- Xuelei Yan ,
- Kai YU
Compounds that inhibit HIF-2α, and compositions containing the compound(s) and methods for synthesizing the compounds, are described herein. Also described are the use of such compounds and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by HIF-2α.
COMPOUNDS WITH ANTIMICROBIAL ACTIVITY
This invention relates to compounds of formula 1, 2 or 3
##STR00001##
a pharmaceutically acceptable salt, or solvate thereof, wherein X.sub.1, Y, R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are as defined herein. The compounds are antimicrobial agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1, 2 or 3.