Patent classifications
C07C255/53
COMPOUNDS WITH ANTIMICROBIAL ACTIVITY
This invention relates to compounds of formula 1, 2 or 3
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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.
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.
METHOD OF SYNTHESIZING (1R,2R)-NITROALCOHOL COMPOUND
Disclosed is a method of synthesizing a (1R,2R)-nitroalcohol compound of formula (I), as shown in the following reaction scheme, including: subjecting a compound of formula (II) and a compound of formula (III) to a condensation reaction in an organic solvent in the presence of a copper complex generated in situ from a chiral (1S,2R)-amino alcohol ligand and a cupric salt to produce the (1R,2R)-nitroalcohol compound of formula (I), where R.sup.1 and R.sup.2 are defined in the same manner as that in the specification. The method involves mild reaction conditions, excellent diastereoselectivity and high chemical yield, and thus it is suitable for industrial applications.
##STR00001##
METHOD OF SYNTHESIZING (1R,2R)-NITROALCOHOL COMPOUND
Disclosed is a method of synthesizing a (1R,2R)-nitroalcohol compound of formula (I), as shown in the following reaction scheme, including: subjecting a compound of formula (II) and a compound of formula (III) to a condensation reaction in an organic solvent in the presence of a copper complex generated in situ from a chiral (1S,2R)-amino alcohol ligand and a cupric salt to produce the (1R,2R)-nitroalcohol compound of formula (I), where R.sup.1 and R.sup.2 are defined in the same manner as that in the specification. The method involves mild reaction conditions, excellent diastereoselectivity and high chemical yield, and thus it is suitable for industrial applications.
##STR00001##
COMPOUNDS FOR USE AS INHIBITORS OF ALTERNATIVE OXIDASE OR CYTOCHROME BC1 COMPLEX
The invention provides compounds for use in inhibiting a microbial alternative oxidase (AOX) and/or cytochrome bc.sub.1 complex. The invention extends to the use of such inhibitors in agrochemicals and in pharmaceuticals, for treating microbial infections, including fungal infections.
COMPOUNDS FOR USE AS INHIBITORS OF ALTERNATIVE OXIDASE OR CYTOCHROME BC1 COMPLEX
The invention provides compounds for use in inhibiting a microbial alternative oxidase (AOX) and/or cytochrome bc.sub.1 complex. The invention extends to the use of such inhibitors in agrochemicals and in pharmaceuticals, for treating microbial infections, including fungal infections.
Compounds for use as inhibitors of alternative oxidase or cytochrome BC1 complex
The invention provides compounds for use in inhibiting a microbial alternative oxidase (AOX) and/or cytochrome bc.sub.1 complex. The invention extends to the use of such inhibitors in agrochemicals and in pharmaceuticals, for treating microbial infections, including fungal infections.
Compounds for use as inhibitors of alternative oxidase or cytochrome BC1 complex
The invention provides compounds for use in inhibiting a microbial alternative oxidase (AOX) and/or cytochrome bc.sub.1 complex. The invention extends to the use of such inhibitors in agrochemicals and in pharmaceuticals, for treating microbial infections, including fungal infections.
CATECHOL O-METHYLTRANSFERASE ACTIVITY INHIBITING COMPOUNDS
Compounds of formula (I), wherein R.sub.1 is as defined in the claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors. Methods of treatment and pharmaceutical dosage forms are also disclosed.