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US 7,678,785 B2Granted
Substituted aniline derivatives
AssigneeUCB Pharma S.A.
InventorsAndrew David Carr, Judi Charlotte Neuss, Michael Glen Orchard, David William Porter
Life of this patent
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Abstract
The present invention relates to novel aniline derivatives and their use in therapy, in particular their use in the treatment of fungal infections.
Claims22
A compound having the structure of Formula I:
- wherein,
- n is 0;
- R1 and R2 together with the nitrogen atom to which they are attached form a 4- to 8-membered heterocycloalkyl or heterocycloalkenyl group which is optionally substituted with 1 or 2 independently selected Rx groups;
- Ar is phenyl that is substituted with OCH2-phenyl wherein the OCH2-phenyl is optionally substituted with 1 or 2 independently selected Rx groups;
- R3 is L1-L2-R4, where
- L1 a bond;
- L2 is selected from a bond, (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)heteroalkyl, (C2-C6)heteroalkenyl, (C3-C8)cycloalkyl, (C3-C8)cycloalkenyl, (C2-C8)heterocycloalkyl and (C2-C8)heterocycloalkenyl;
- wherein the (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)heteroalkyl, (C2-C6)heteroalkenyl, (C3-C8)cycloalkyl, (C3-C8)cycloalkenyl, (C2-C8)heterocycloalkyl, and (C2-C8)heterocycloalkenyl is optionally substituted with 1 or 2 independently selected Rx groups;
- R4 is selected from H, cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl, aryl, and heteroaryl, wherein the cycloalkyl, cycloalkenyl, heterocycloalkyl, heterocycloalkenyl, aryl, and heteroaryl is optionally substituted with 1 or 2 independently selected Rx groups;
- Rx is Ls1Ls2Rs, wherein each Ls1 and Ls2 is independently selected from a bond, —O, —C(═O)—, —S—, —S(═O)—, —S(═O)2—, —NH—, —NHC(O)—, —C(O)NH—, S(═O)2NH—, —NHS(═O)2, —OC(O)NH—, —NHC(O)O—, (C1-C6) alkyl, and —(C2-C6) alkenyl;
- and
- Rs is selected from hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, heteroalicyclic, hydroxy, alkoxy, aryloxy, mercapto, alkylthio, arylthio, alkylsulfoxide, arylsulfoxide, alkylsulfone, arylsulfone, cyano, halo, isocyanato, thiocyanato, isothiocyanato, nitro, perhaloalkyl, perfluoroalkyl, silyl, and amino, including mono- and di-substituted amino groups;
- or a pharmaceutically acceptable salt, tautomer, or optical isomer thereof.
10 more elements
A compound having the structure according to the following formula:
- wherein:
- Y is —COZ;
- Z is selected from the group consisting of Ph, —(C1-C3)alkyl-Ph and —CH═CHPh, wherein Ph is substituted with RC and RD which are independently selected from the group comprising hydrogen, halo, C1-C6 alkyl, ORE, NRGRH, NRGCORW, NRGSO2RW, CONRGRH and SO2RW;
- RL is selected from the group consisting of hydrogen, halogen, Ph, OPh and OCH2Ph, wherein Ph is optionally substituted with halogen, C1-C6 alkyl, ORE or CO2RE;
- RA and RB are independently selected from hydrogen, C1-C6 alkyl and CO2RF;
- RE is hydrogen or C1-C6 alkyl;
- RF is C1-C6alkyl;
- RG and RH are independently hydrogen or C1-C6 alkyl, or together form a 5- or 6-membered ring which optionally contains one further heteroatom selected from NRE, S and O;
- and
- RW is C1-C6 alkyl.
7 more elements
A compound having the structure according to the following formula:
- wherein
- Y″ is selected from the group comprising Ph, —(C1-C3)alkyl-Ph and —CH═CHPh, wherein Ph is substituted with RC2 and RD2 which are independently selected from the group comprising hydrogen, halogen, C1-C6 alkyl, ORE2, NRG2RH2, NRG2CORW2, NRG2SO2RW2, CONRG2RH2 and SO2RW2;
- RL2 is selected from the group consisting of hydrogen, halogen, Ph, OPh and OCH2Ph, wherein Ph is optionally substituted with halogen, C1-C6 alkyl, ORE2 or CO2RE2;
- RE2 and RB2 are independently selected from hydrogen, C1-C6 alkyl and CO2RF2;
- RE2 is hydrogen or C1-C6 alkyl;
- RF2 is C1-C6 alkyl;
- RG2 and RH2 are independently hydrogen or C1-C6 alkyl, or together form a 5- or 6-membered ring which optionally contains one further heteroatom selected from NRE2, S and O;
- and
- RW2 is C1-C6 alkyl.
6 more elements
Dependencies are inferred from the claim text.