Back to results
US 6,028,223 AGranted
Meta-guanidine, urea, thiourea or azacyclic amino benzoic acid compounds and derivatives thereof
AssigneeG. D. Searle & Co.
InventorsPeter Gerrard Ruminski, Michael Clare, Paul Waddell Collins, Bipinchandra Nanubhai Desai, Richard John Lindmark, Joseph Gerace Rico, Thomas Edward Rogers, Mark Andrew Russell
Life of this patent
Estimating the term…
Abstract
The present invention relates to a class of compounds represented by the Formula I ##STR1## or a pharmaceutically acceptable salt thereof, wherein A is ##STR2## pharmaceutical compositions thereof and methods of using such compounds and compositions as .alpha..sub.v .beta..sub.3 antagonists.
Claims36
A compound of the formula ##STR799## or a pharmaceutically acceptable salt thereof, wherein A is ##STR800## wherein Y.sup.1 is selected from the group consisting of N--R.sup.2, O, and S;
- R.sup.2 is selected from the group consisting of H;
- alkyl;
- aryl;
- hydroxy;
- alkoxy;
- cyano;
- nitro;
- amino;
- alkenyl;
- alkynyl;
- amido;
- alkylcarbonyl;
- arylcarbonyl;
- alkoxycarbonyl;
- aryloxycarbonyl;
- haloalkylcarbonyl;
- haloalkoxycarbonyl;
- alkylthiocarbonyl;
- arylthiocarbonyl;
- acyloxymethoxycarbonyl;
- alkyl optionally substituted with one or more substituent selected from lower alkyl, halogen, hydroxyl, haloalkyl, cyano, nitro, carboxyl, amino, alkoxy, aryl or aryl optionally substituted with one or more halogen, haloalkyl, lower alkyl, alkoxy, cyano, alkylsulfonyl, alkylthio, nitro, carboxyl, amino, hydroxyl, sulfonic acid, sulfonamide, aryl, or fused aryl;
- and aryl optionally substituted with one or more substituent selected from halogen, haloalkyl, hydroxy, lower alkyl, alkoxy, methylenedioxy, ethylenedioxy, cyano, nitro, alkylthio, alkylsulfonyl, sulfonic acid, sulfonamide, carboxyl derivatives, amino, aryl, or fused aryl,
- R.sup.7 and R.sup.8 are independently selected from the group consisting of H;
- alkyl;
- alkenyl;
- alkynyl;
- aralkyl;
- amino;
- alkylamino;
- hydroxy;
- alkoxy;
- arylamino;
- amido, alkylcarbonyl, arylcarbonyl;
- alkoxycarbonyl;
- aryloxycarbonyl;
- haloalkylcarbonyl;
- aryloxy;
- haloalkoxycarbonyl;
- alkylthiocarbonyl;
- arylthiocarbonyl;
- acyloxymethoxycarbonyl;
- cycloalkyl;
- bicycloalkyl;
- aryl;
- acyl;
- benzoyl;
- alkyl optionally substituted with one or more substituent selected from lower alkyl, halogen, hydroxy, haloalkyl, cyano, nitro, carboxyl derivatives, amino, alkoxy, thio, alkylthio, sulfonyl, aryl, aralkyl, aryl optionally substituted with one or more substituent selected from halogen, haloalkyl, lower alkyl, alkoxy, methylenedioxy, ethylenedioxy, alkylthio, haloalkylthio, thio, hydroxy, cyano, nitro, carboxyl derivatives, aryloxy, amido, acylamino, amino, alkylamino, dialkylamino, trifluoroalkoxy, trifluoromethyl, sulfonyl, alkylsulfonyl, haloalkylsulfonyl, sulfonic acid, sulfonamide, aryl, or fused aryl;
- aryl optionally substituted with one or more substituent selected from halogen, haloalkyl, lower alkyl, alkoxy, methylenedioxy, ethylenedioxy, alkylthio, haloalkylthio, thio, hydroxy, cyano, nitro, carboxyl derivatives, aryloxy, amido, acylamino, amino, alkylamino, dialkylamino, trifluoroalkoxy, trifluoromethylsulfonyl, alkylsulfonyl, sulfonic acid, sulfonamide, aryl, or fused aryl;
- --SO.sub.2 R.sup.10 wherein R.sup.10 is selected from the group consisting of alkyl, and aryl both optionally substituted with one or more substituent selected from the group consisting of halogen, haloalkyl, alkyl, alkoxy, cyano, nitro, amino, acylamino, trifluoroalkyl, amido, alkylaminosulfonyl, alkylsulfonyl, alkylsulfonylamino, alkylamino, dialkylamino, trifluoromethylthio, trifluoroalkoxy, trifluoromethylsulfonyl, aryl, aryloxy, thio, and alkylthio;
- and ##STR801## wherein R.sup.10 is defined above;
- R.sup.5 is selected from the group consisting of H, alkyl, alkenyl, alkynyl, benzyl, and phenethyl;
- or
- A is ##STR802## wherein Y.sup.2 is selected from the group consisting of alkyl;
- cycloalkyl;
- bicycloalkyl;
- aryl;
- alkyl optionally substituted with aryl which can also be optionally substituted with one or more substituent selected from halo, haloalkyl, alkyl, nitro, hydroxy, alkoxy, aryloxy, aryl, or fused aryl;
- aryl optionally substituted with one or more substituent selected from halo, haloalkyl, hydroxy, alkoxy, aryloxy, aryl, fused aryl, nitro, methylenedioxy, ethylenedioxy, or alkyl;
- alkynyl;
- alkenyl;
- --S--R.sup.9 and --O--R.sup.9 wherein R.sup.9 is selected from the group consisting of H;
- alkyl;
- aralkyl;
- aryl;
- alkenyl;
- and alkynyl;
- and
- R.sup.5 and R.sup.7 are as defined above;
- Z.sup.1 is one or more substituent selected from the group consisting of H;
- alkyl;
- hydroxy;
- alkoxy;
- aryloxy;
- halogen;
- haloalkyl;
- haloalkoxy;
- nitro;
- amino;
- alkylamino;
- acylamino;
- dialkylamino;
- cyano;
- alkylthio;
- alkylsulfonyl;
- carboxyl derivatives;
- trihaloacetamide;
- acetamide;
- aryl;
- fused aryl;
- cycloalkyl;
- thio;
- and A, wherein A is defined above;
- V is selected from the group consisting of --N--(R.sup.6)-- wherein R.sup.6 is selected from the group consisting of H;
- lower alkyl;
- cycloalkyl;
- aralkyl;
- and aryl;
- Y, Y.sup.3, Z and Z.sup.3 are independently selected from the group consisting of hydrogen;
- alkyl;
- aryl;
- and cycloalkyl;
- or Y and Z taken together form a cycloalkyl;
- or Y.sup.3 and Z.sup.3 taken together form a cycloalkyl;
- n is an integer 1, 2, or 3;
- t is an integer 0, 1, or 2;
- p is an integer 0, 1, 2, or 3;
- R is X--R.sup.3 wherein X is selected from the group consisting of O, S and NR.sup.4, wherein R.sup.3 and R.sup.4 are independently selected from the group consisting of hydrogen;
- alkyl;
- alkenyl;
- alkynyl;
- haloalkyl;
- aryl;
- arylalkyl;
- polyalkylethers;
- alkylamido;
- alkyl N,N-dialkylamido;
- pivaloyloxymethyl;
- and in the case of the free acid, all pharmaceutically acceptable salts thereof;
- R.sup.1 is selected from the group consisting of hydrogen;
- alkyl;
- alkenyl;
- alkynyl;
- aryl;
- carboxyl derivatives;
- haloalkyl;
- alkyl optionally substituted with one or more of halo, haloalkyl, hydroxy, alkoxy, aryloxy, thio, alkylthio, alkynyl, alkenyl, alkyl, arylthio, alkylsulfoxide, alkylsulfonyl, arylsulfoxide, arylsulfonyl, cyano, nitro, amino, alkylamino, dialkylamino, alkylsulfonamide, arylsulfonamide, acylamide, carboxyl derivatives, sulfonamide, sulfonic acid, phosphonic acid derivatives, phosphinic acid derivatives, aryl, arylthio, arylsulfoxide, or arylsulfone all optionally substituted on the aryl ring with halo, alkyl, haloalkyl, cyano, nitro, hydroxy, carboxyl derivatives, alkoxy, aryloxy, amino, alkylamino, dialkylamino, amido, aryl, or fused aryl,
- alkylcarbonyl, haloalkylcarbonyl, and arylcarbonyl;
- aryl optionally substituted in one or more positions with halo, haloalkyl, alkyl, alkoxy, aryloxy, methylenedioxy, ethylenedioxy, alkylthio, haloalkylthio, thio, hydroxy, cyano, nitro, acyloxy, carboxyl derivatives, carboxyalkoxy, amido, acylamino, amino, alkylamino, dialkylamino, trifluoroalkoxy, trifluoromethylsulfonyl, alkylsulfonyl, sulfonic acid, sulfonamide, aryl, and fused aryl, and ##STR803## wherein R.sup.7 and R.sup.8 are as defined above and provided that taken together with the nitrogen, R.sup.7 and R.sup.8 comprise an amino acid;
- and
- R.sup.11 is selected from the group consisting of H, alkyl, aralkyl, alkenyl, alkynyl, haloalkyl or haloalkynyl or.
127 more elements
A pharmaceutical composition comprising a therapeutically effective amount of a compound of the formula ##STR806## or a pharmaceutically acceptable salt thereof, wherein A is ##STR807## wherein Y.sup.1 is selected from the group consisting of N--R.sup.2, O, and S;
- R.sup.2 is selected from the group consisting of H;
- alkyl;
- aryl;
- hydroxy;
- alkoxy;
- cyano;
- nitro;
- amino;
- alkenyl;
- alkynyl;
- amido;
- alkylcarbonyl;
- arylcarbonyl;
- alkoxycarbonyl;
- aryloxycarbonyl;
- haloalkylcarbonyl;
- haloalkoxycarbonyl;
- alkylthiocarbonyl;
- arylthiocarbonyl;
- acyloxymethoxycarbonyl;
- alkyl optionally substituted with one or more substituent selected from lower alkyl, halogen, hydroxyl, haloalkyl, cyano, nitro, carboxyl, amino, alkoxy, aryl or aryl optionally substituted with one or more halogen, haloalkyl, lower alkyl, alkoxy, cyano, alkylsulfonyl, alkylthio, nitro, carboxyl, amino, hydroxyl, sulfonic acid, sulfonamide, aryl, or fused aryl;
- and aryl optionally substituted with one or more substituent selected from halogen, haloalkyl, hydroxy, lower alkyl, alkoxy, methylenedioxy, ethylenedioxy, cyano, nitro, alkylthio, alkylsulfonyl, sulfonic acid, sulfonamide, carboxyl derivatives, amino, aryl, or fused aryl;
- R.sup.7 and R.sup.8 are independently selected from the group consisting of H;
- alkyl;
- alkenyl;
- alkynyl;
- aralkyl;
- amino;
- alkylamino;
- hydroxy;
- alkoxy;
- arylamino;
- amido, alkylcarbonyl, arylcarbonyl;
- alkoxycarbonyl;
- aryloxycarbonyl;
- haloalkylcarbonyl;
- aryloxy;
- haloalkoxycarbonyl;
- alkylthiocarbonyl;
- arylthiocarbonyl;
- acyloxymethoxycarbonyl;
- cycloalkyl;
- bicycloalkyl;
- aryl;
- acyl;
- benzoyl;
- alkyl optionally substituted with one or more substituent selected from lower alkyl, halogen, hydroxy, haloalkyl, cyano, nitro, carboxyl derivatives, amino, alkoxy, thio, alkylthio, sulfonyl, aryl, aralkyl, aryl optionally substituted with one or more substituent selected from halogen, haloalkyl, lower alkyl, alkoxy, methylenedioxy, ethylenedioxy, alkylthio, haloalkylthio, thio, hydroxy, cyano, nitro, carboxyl derivatives, aryloxy, amido, acylamino, amino, alkylamino, dialkylamino, trifluoroalkoxy, trifluoromethyl, sulfonyl, alkylsulfonyl, haloalkylsulfonyl, sulfonic acid, sulfonamide, aryl, or fused aryl;
- aryl optionally substituted with one or more substituent selected from halogen, haloalkyl, lower alkyl, alkoxy, methylenedioxy, ethylenedioxy, alkylthio, haloalkylthio, thio, hydroxy, cyano, nitro, carboxyl derivatives, aryloxy, amido, acylamino, amino, alkylamino, dialkylamino, trifluoroalkoxy, trifluoromethylsulfonyl, alkylsulfonyl, sulfonic acid, sulfonamide, aryl, or fused aryl;
- --SO.sub.2 R.sup.10 wherein R.sup.10 is selected from the group consisting of alkyl, and aryl, both optionally substituted with one or more substituent selected from the group consisting of halogen, haloalkyl, alkyl, alkoxy, cyano, nitro, amino, acylamino, trifluoroalkyl, amido, alkylaminosulfonyl, alkylsulfonyl, alkylsulfonylamino, alkylamino, dialkylamino, trifluoromethylthio, trifluoroalkoxy, trifluoromethylsulfonyl, aryl, aryloxy, thio, and alkylthio;
- and ##STR808## wherein R.sup.10 is defined above;
- R.sup.5 is selected from the group consisting of H, alkyl, alkenyl, alkynyl, benzyl, and phenethyl;
- or
- A is ##STR809## wherein Y.sup.2 is selected from the group consisting of alkyl;
- cycloalkyl;
- bicycloalkyl;
- aryl;
- alkyl optionally substituted with aryl which can also be optionally substituted with one or more substituent selected from halo, haloalkyl, alkyl, nitro, hydroxy, alkoxy, aryloxy, aryl, or fused aryl;
- aryl optionally substituted with one or more substituent selected from halo, haloalkyl, hydroxy, alkoxy, aryloxy, aryl, fused aryl, nitro, methylenedioxy, ethylenedioxy, or alkyl;
- alkynyl;
- alkenyl;
- --S--R.sup.9 and --O--R.sup.9 wherein R.sup.9 is selected from the group consisting of H;
- alkyl;
- aralkyl;
- aryl;
- alkenyl;
- and alkynyl;
- and
- R.sup.5 and R.sup.7 are as defined above;
- Z.sup.1 is one or more substituent selected from the group consisting of H;
- alkyl;
- hydroxy;
- alkoxy;
- aryloxy;
- halogen;
- haloalkyl;
- haloalkoxy;
- nitro;
- amino;
- alkylamino;
- acylamino;
- dialkylamino;
- cyano;
- alkylthio;
- alkylsulfonyl;
- carboxyl derivatives;
- trihaloacetamide;
- acetamide;
- aryl;
- fused aryl;
- cycloalkyl;
- thio;
- and A, wherein A is defined above;
- V is selected from the group consisting of --N--(R.sup.6)-- wherein R.sup.6 is selected from the group consisting of H;
- lower alkyl;
- cycloalkyl;
- aralkyl;
- and aryl;
- Y, Y.sup.3, Z and Z.sup.3 are independently selected from the group consisting of hydrogen;
- alkyl;
- aryl;
- and cycloalkyl;
- or Y and Z taken together form a cycloalkyl;
- or Y.sup.3 and Z.sup.3 taken together form a cycloalkyl;
- n is an integer 1, 2, or 3;
- t is an integer 0, 1, or 2;
- p is an integer 0, 1, 2, or 3;
- R is X--R.sup.3 wherein X is selected from the group consisting of O, S and NR.sup.4, wherein R.sup.3 and R.sup.4 are independently selected from the group consisting of hydrogen;
- alkyl;
- alkenyl;
- alkynyl;
- haloalkyl;
- aryl;
- arylalkyl;
- polyalkylethers;
- alkylamido;
- alkyl N,N-dialkylamido;
- pivaloyloxymethyl;
- and in the case of the free acid, all pharmaceutically acceptable salts thereof;
- R.sup.1 is selected from the group consisting of hydrogen;
- alkyl;
- alkenyl;
- alkynyl;
- aryl;
- carboxyl derivatives;
- haloalkyl;
- alkyl optionally substituted with one or more of halo, haloalkyl, hydroxy, alkoxy, aryloxy, thio, alkylthio, alkynyl, alkenyl, alkyl, arylthio, alkylsulfoxide, alkylsulfonyl, arylsulfoxide, arylsulfonyl, cyano, nitro, amino, alkylamino, dialkylamino, alkylsulfonamide, arylsulfonamide, acylamide, carboxyl derivatives, sulfonamide, sulfonic acid, phosphonic acid derivatives, phosphinic acid derivatives, aryl, arylthio, arylsulfoxide, or arylsulfone all optionally substituted on the aryl ring with halo, alkyl, haloalkyl, cyano, nitro, hydroxy, carboxyl derivatives, alkoxy, aryloxy, amino, alkylamino, dialkylamino, amido, aryl, or fused aryl, alkylcarbonyl, haloalkylcarbonyl, and arylcarbonyl;
- aryl optionally substituted in one or more positions with halo, haloalkyl, alkyl, alkoxy, aryloxy, methylenedioxy, ethylenedioxy, alkylthio, haloalkylthio, thio, hydroxy, cyano, nitro, acyloxy, carboxyl derivatives, carboxyalkoxy, amido, acylamino, amino, alkylamino, dialkylamino, trifluoroalkoxy, trifluoromethylsulfonyl, alkylsulfonyl, sulfonic acid, sulfonamide, aryl, and fused aryl, and ##STR810## wherein R.sup.7 and R.sup.8 are as defined above and provided that taken together with the nitrogen, R.sup.7 and R.sup.8 comprise an amino acid;
- and
- R.sup.11 is selected from the group consisting of H, alkyl, aralkyl, alkenyl, alkynyl, haloalkyl or haloalkynyl;
- and
- a pharmaceutically acceptable carrier.
128 more elements
A method for treating conditions mediated by the .alpha..sub.V .beta..sub.3 integrin in a mammal in need of such treatment comprising administering an effective .alpha..sub.V .beta..sub.3 inbhibiting amount of a compound of the formuls ##STR813## or a pharmeceutically acceptable salt thereof, wherein A is ##STR814## wherein Y.sup.1 is selected from the group consisting of N--R.sup.2, O and S;
- R.sup.2 is selected from the group consisting of H;
- alkyl;
- aryl;
- hydroxy;
- alkoxy;
- cyano;
- nitro;
- amino;
- alkenyl;
- alkynyl;
- amido;
- alkylcarbonyl;
- arylcarbonyl;
- alkoxycarbonyl;
- aryloxycarbonyl;
- haloalkylcarbonyl;
- haloalkoxycarbonyl;
- alkylthiocarbonyl;
- arylthiocarbonyl;
- acyloxymethoxycarbonyl;
- alkyl optionally substituted with one or more substituent selected from lower alkyl, halogen, hydroxyl, haloalkyl, cyano, nitro, carboxyl, amino, alkoxy, aryl or aryl optionally substituted with one or more halogen, haloalkyl, lower alkyl, alkoxy, cyano, alkylsulfonyl, alkylthio, nitro, carboxyl, amino, hydroxyl, sulfonic acid, sulfonamide, aryl, or fused aryl;
- aryl optionally substituted with one or more substituent selected from halogen, haloalkyl, hydroxy, lower alkyl, alkoxy, methylenedioxy, ethylenedioxy, cyano, nitro, alkylthio, alkylsulfonyl, sulfonic acid, sulfonamide, carboxyl derivatives, amino, aryl, or fused aryl;
- R.sup.7 and R.sup.8 are independently selected from the group consisting of H;
- alkyl;
- alkenyl;
- alkynyl;
- aralkyl;
- amino;
- alkylamino;
- hydroxy;
- alkoxy;
- arylamino;
- amido, alkylcarbonyl, arylcarbonyl;
- alkoxycarbonyl;
- aryloxycarbonyl;
- haloalkylcarbonyl;
- aryloxy;
- haloalkoxycarbonyl;
- alkylthiocarbonyl;
- arylthiocarbonyl;
- acyloxymethoxycarbonyl;
- cycloalkyl;
- bicycloalkyl;
- aryl;
- acyl;
- benzoyl;
- alkyl optionally substituted with one or more substituent selected from lower alkyl, halogen, hydroxy, haloalkyl, cyano, nitro, carboxyl derivatives, amino, alkoxy, thio, alkylthio, sulfonyl, aryl, aralkyl, aryl optionally substituted with one or more substituent selected from halogen, haloalkyl, lower alkyl, alkoxy, methylenedioxy, ethylenedioxy, alkylthio, haloalkylthio, thio, hydroxy, cyano, nitro, carboxyl derivatives, aryloxy, amido, acylamino, amino, alkylamino, dialkylamino, trifluoroalkoxy, trifluoromethyl, sulfonyl, alkylsulfonyl, haloalkylsulfonyl, sulfonic acid, sulfonamide, aryl, or fused aryl;
- aryl optionally substituted with one or more substituent selected from halogen, haloalkyl, lower alkyl, alkoxy, methylenedioxy, ethylenedioxy, alkylthio, haloalkylthio, thio, hydroxy, cyano, nitro, carboxyl derivatives, aryloxy, amido, acylamino, amino, alkylamino, dialkylamino, trifluoroalkoxy, trifluoromethylsulfonyl, alkylsulfonyl, sulfonic acid, sulfonamide, aryl, or fused aryl;
- --SO.sub.2 R.sup.10 wherein R.sup.10 is selected from the group consisting of alkyl, and aryl both optionally substituted with one or more substituent selected from the group consisting of halogen, haloalkyl, alkyl, alkoxy, cyano, nitro, amino, acylamino, trifluoroalkyl, amido, alkylaminosulfonyl, alkylsulfonyl, alkylsulfonylamino, alkylamino, dialkylamino, trifluoromethylthio, trifluoroalkoxy, trifluoromethylsulfonyl, aryl, aryloxy, thio, and alkylthio;
- and ##STR815## wherein R.sup.10 is defined above;
- R.sup.5 is selected from the group consisting of H, alkyl, alkenyl, alkynyl, benzyl, and phenethyl;
- or A is ##STR816## wherein Y.sup.2 is selected from the group consisting of alkyl;
- cycloalkyl;
- bicycloalkyl;
- aryl;
- alkyl optionally substituted with aryl which can also be optionally substituted with one or more substituent selected from halo, haloalkyl, alkyl, nitro, hydroxy, alkoxy, aryloxy, aryl, or fused aryl;
- aryl optionally substituted with one or more substituent selected from halo, haloalkyl, hydroxy, alkoxy, aryloxy, aryl, fused aryl, nitro, methylenedioxy, ethylenedioxy, or alkyl;
- alkynyl;
- alkenyl;
- --S--R.sup.9 and --O--R.sup.9 wherein R.sup.9 is selected from the group consisting of H;
- alkyl;
- aralkyl;
- aryl;
- alkenyl;
- and alkynyl;
- and
- R.sup.5 and R.sup.7 are as defined above;
- Z.sup.1 is one or more substituent selected from the group consisting of H;
- alkyl;
- hydroxy;
- alkoxy;
- aryloxy;
- halogen;
- haloalkyl;
- haloalkoxy;
- nitro;
- amino;
- alkylamino;
- acylamino;
- dialkylamino;
- cyano;
- alkylthio;
- alkylsulfonyl;
- carboxyl derivatives;
- trihaloacetamide;
- acetamide;
- aryl;
- fused aryl;
- cycloalkyl;
- thio;
- and A, wherein A is defined above;
- V is selected from the group consisting of --N--(R.sup.6)-- wherein R.sup.6 is selected from the group consisting of H;
- lower alkyl;
- cycloalkyl;
- aralkyl;
- and aryl;
- Y, Y.sup.3, Z and Z.sup.3 are independently selected from the group consisting of hydrogen;
- alkyl;
- aryl;
- and cycloalkyl;
- or Y and Z taken together form a cycloalkyl;
- or Y.sup.3 and Z.sup.3 taken together form a cycloalkyl;
- n is an integer 1, 2, or 3;
- t is an integer 0, 1, or 2;
- p is an integer 0, 1, 2, or 3;
- R is X--R.sup.3 wherein X is selected from the group consisting of O, S and NR.sup.4, wherein R.sup.3 and R.sup.4 are independently selected from the group consisting of hydrogen;
- alkyl;
- alkenyl;
- alkynyl;
- haloalkyl;
- aryl;
- arylalkyl;
- polyalkylethers;
- alkylamido;
- alkyl N,N-dialkylamido;
- pivaloyloxymethyl;
- and in the case of the free acid, all pharmaceutically acceptable salts thereof;
- R.sup.1 is selected from the group consisting of hydrogen;
- alkyl;
- alkenyl;
- alkynyl;
- aryl;
- carboxyl derivatives;
- haloalkyl;
- alkyl optionally substituted with one or more of halo, haloalkyl, hydroxy, alkoxy, aryloxy, thio, alkylthio, alkynyl, alkenyl, alkyl, arylthio, alkylsulfoxide, alkylsulfonyl, arylsulfoxide, arylsulfonyl, cyano, nitro, amino, alkylamino, dialkylamino, alkylsulfonamide, arylsulfonamide, acylamide, carboxyl derivatives, sulfonamide, sulfonic acid, phosphonic acid derivatives, phosphinic acid derivatives, aryl, arylthio, arylsulfoxide, or arylsulfone all optionally substituted on the aryl ring with halo, alkyl, haloalkyl, cyano, nitro, hydroxy, carboxyl derivatives, alkoxy, aryloxy, amino, alkylamino, dialkylamino, amido, aryl, or fused aryl, alkylcarbonyl, haloalkylcarbonyl, and arylcarbonyl;
- aryl optionally substituted in one or more positions with halo, haloalkyl, alkyl, alkoxy, aryloxy, methylenedioxy, ethylenedioxy, alkylthio, haloalkylthio, thio, hydroxy, cyano, nitro, acyloxy, carboxyl derivatives, carboxyalkoxy, amido, acylamino, amino, alkylamino, dialkylamino, trifluoroalkoxy, trifluoromethylsulfonyl, alkylsulfonyl, sulfonic acid, sulfonamide, aryl, and fused aryl, and ##STR817## wherein R.sup.7 and R.sup.8 are as defined above and provided that taken together with the nitrogen, R.sup.7 and R.sup.8 comprise an amino acid;
- and
- R.sup.11 is selected from the group consisting of H, alkyl, aralkyl, alkenyl, alkynyl, haloalkyl or haloalkynyl.
125 more elements
Dependencies are inferred from the claim text.