Abstract: The present invention provides compounds of the general formula: wherein W is O or NH, optionally substituted, as well as methods and pharmaceutical compositions utilizing these compounds for the treatment of disorder which may be remedied or alleviated by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, or temporary delay of urination.

Abstract: This invention provides compounds of formula 1 having the structure ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are each independently, hydrogen, halogen, alkyl, cycloalkyl, alkenyl, alkynyl, phenylalkyl, alkoxy, aryloxy, fluoroalkoxy, trifluoromethyl, alkylthio, alkylsulfony, --SCF.sub.3, nitro, alkylamino, or dialkylamino;R.sup.6 is hydrogen, alkyl, cycloalkyl, or arylalkyl; andR.sup.7 is alkyl, cycloalkyl, or arylalkylor a pharmaceutically acceptable salt thereof which are useful as antiatherosclerotic agents.

Abstract: The present invention provides compounds of the general formula: ##STR1## wherein W is O or NH, optionally substituted, as well as methods and pharmaceutical compositions utilizing these compounds for the treatment of disorder which may be remedied or alleviated by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders, or temporary delay of urination.

Abstract: Antiatherosclerotic agents are provided having the structure: ##STR1## wherein R is a lower alkyl of 1-6 carbon atoms, ##STR2## wherein R.sub.5, R.sub.6, and R.sub.7 are lower alkyl of 1-6 carbon atoms; and R.sub.8, R.sub.9 and R.sub.10 are each, independently, hydrogen or halogen;R.sub.1 and R.sub.2 are each, independently, hydrogen or a lower alkyl of 1-6 carbon atoms; andR.sub.3 and R.sub.4 are each, independently, hydrogen, a lower alkyl of 1-6 carbon atoms or halogen;or a pharmaceutically acceptable salt thereof.

Abstract: This invention provides compounds of formula 1 having the structure ##STR1## wherein: R.sup.1 is hydrogen, halogen, alkyl, alkoxy, fluoroalkoxy, trifluoromethyl, alkylthio, or SCF.sub.3R.sup.2 and R.sup.3 are each independently, hydrogen or alkyl, or R.sup.2 and R.sup.3 may be taken together to form a saturated cycloalkyl ring; andR.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are each independently, hydrogen, alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, halogen, fluoroalkoxy, CF.sub.3, or SCF.sub.3 which are useful in the treatment of arthritic disorders, colorectal cancer, and Alzheimer's disease.

Abstract: This invention provides compounds of formula I having the structure ##STR1## wherein R is (CH.sub.2).sub.n COOR.sup.4 ;R.sup.1 is hydrogen, alkyl, alkenyl, alkynyl, alkylcycloalkyl, and alkoxyalkyl;R.sup.4 is hydrogen or alkyl;R.sup.5, R.sup.6, R.sup.7, and R.sup.8 are each, independently, hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, arylalkoxy, fluoroalkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, cyano, nitro, --SCF.sub.3, --COR.sup.3, alkanoyloxy, hydroxy, trifluoromethyl, amino, alkylamino, dialkylamino, alkylamido, or alkylsulfonamido; wherein at least one of R.sup.5, R.sup.6, R.sup.7, or R.sup.8 is cyano;R.sup.3 is alkyl, hydroxy, alkoxy, amino, alkylamino;X is --O-- or --C--; andn=1-4or a pharmaceutically acceptable salt thereof, which are useful in the treatment of arthritic disorders, colorectal cancer, and Alzheimer's disease.

Abstract: This invention provides compounds of formula I having the structure ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are, each, independently, hydrogen, alkyl, alkenyl, alkynyl, alkoxy, aralkoxy, trifluroalkoxy, alkanoyloxy, hydroxy, halo, trifluoromethyl, cyano, amino, mono- or di-alkylamino, alkanamido, or alkanesulfonamido;R.sub.5 is hydrogen, alkyl, alkenyl, alkoxyalkyl or alkylcycloalkyl;R.sub.6 is hydrogen, alkyl or alkenyl;X is oxygen or carbon;A is oxygen or NZ;Z is hydroxyl, alkoxy, aryloxy, carboxyalkyloxy of 2-7 carbon atoms, arylamino, or alkylsulfonyamino of 1-6 carbon atoms;or a pharmaceutically acceptable salt thereof, which are useful in the treatment of arthritic disorders, colorectal cancer, and Alzheimer's disease.

Abstract: This invention provides compounds of formula I having the structure ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are, each, independently, hydrogen, alkyl, alkenyl, alkynyl, alkoxy, aralkoxy, trifluroalkoxy, alkanoyloxy, hydroxy, halo, trifluoromethyl, cyano, amino, mono- or di-alkylamino, alkanamido, or alkanesulfonamido;R.sub.5 is hydrogen, alkyl, alkenyl, alkoxyalkyl or alkylcycloalkyl;R.sub.6 is hydrogen, alkyl or alkenyl;X is oxygen or carbon;A is oxygen or NZ;Z is hydroxyl, alkoxy, aryloxy, carboxyalkyloxy of 2-7 carbon atoms, arylamino, or alkylsulfonyamino of 1-6 carbon atoms;or a pharmaceutically acceptable salt thereof, which are useful in the treatment of arthritic disorders, colorectal cancer, and Alzheimer's disease.

Abstract: A compound of the structure ##STR1## wherein X--Y is C.dbd.NOR.sup.1 or CHNHOR.sup.2 ; R.sup.1 and R.sup.2 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl, alkyloxy, alkoxyalkyl, cycloalkylaminoalkyl, cyanoalkyl, fluoroalkyl, trifluoromethylalkyl, trifluoromethyl, ArO--, --(CH.sub.2).sub.m Ar, or --COR.sup.3 ;R.sup.3 is alkyl of 1-6 carbon atoms, --NH.sub.2, --NHR.sup.4, --NR.sup.4 R.sup.5, or --OR.sup.4 ;R.sup.4 and R.sup.5 are each, independently, alkyl, Ar or if both are present can be taken together to form a 4-7 membered ring;Ar is an aryl or heteroaryl radical which may be optionally substituted; and m=0-6; or a pharmaceutically acceptable salt thereof, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.

Abstract: A compound of the structure ##STR1## wherein X-Y is C=NOR.sup.1 or CHNHOR.sup.2 ; R.sup.1 and R.sup.2 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl, alkyloxy, alkoxyalkyl, cycloalkylaminoalkyl, cyanoalkyl, fluoroalkyl, trifluoromethylalkyl, trifluoromethyl, ArO--, --(CH.sub.2).sub.m Ar, or --COR.sup.3 ;R.sup.3 is alkyl of 1-6 carbon atoms, --NH.sub.2, --NHR.sup.4, --NR.sup.4 R.sup.5, or -OR.sup.4 ;R.sup.4 and R.sup.5 are each, independently, alkyl, Ar or if both are present can be taken together to form a 4-7 membered ring;Ar is an aryl or heteroaryl radical which may be optionally substituted; and m=0-6; or a pharmaceutically acceptable salt thereof, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.

Abstract: A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, --CONR.sup.3 (CR.sup.4 R.sup.5).sub.m (CR.sup.6 R.sup.7).sub.n (CR.sup.8 R.sup.9).sub.p NR.sup.10 R.sup.11, or ##STR2## or --CONR.sup.3 R.sup.13 ; R.sup.3 is hydrogen, alkyl, or arylalkyl;R.sup.4, R.sup.5, R.sup.8, and R.sup.9 are each, independently, hydrogen, alkyl, --OH, --CF.sub.3, or --F;R.sup.6 is hydrogen or --OR.sup.13 ;R.sup.7 is hydrogen or alkyl;R.sup.10 is hydrogen, alkyl, or arylalkyl;R.sup.11, R.sup.12 and R.sup.13 are each, independently, --(CR.sup.15 R.sup.16).sub.r R.sup.17 ;R.sup.14 is hydrogen, alkyl of 1-6 carbon atoms, tri-(alkyl)silyl, tri-(alkyl)silylethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, or tetrahydropyranyl;R.sup.15 and R.sup.16 are each, independently, hydrogen or alkyl;R.sup.17 is ##STR3## or --C.tbd.C--R.sup.21 ; R.sup.18, R.sup.19, R.sup.20, and R.sup.

Abstract: A compound of the structure ##STR1## wherein the variables are defined in the specification, with the proviso that R.sup.1 and R.sup.2 are both not hydrogen, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.

Abstract: A compound of the structure ##STR1## or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent. The substituents are defined elsewhere in the specification.

Abstract: A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, or --CONH--O--(CR.sup.3 R.sup.4).sub.m Z;R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl, cycloalkyl, --CF.sub.3, or F;Z is hydrogen, alkyl, --OR.sup.5, --SR.sup.5, --NRSR.sup.6, --CN, --CF3, --OAr, --Ar, or R.sup.7 ;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl, or Ar;R.sup.7 ##STR2## or --C.tbd.C--R.sup.11 ; R.sup.8, R.sup.9, R.sup.10, and R.sup.11 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, or phenyl, wherein the phenyl group may be optionally mono-, di-, or tri-substituted;Ar is an aryl radical that may be optionally mono-, di-, or tri-substituted; and m=1-6;with the proviso that R.sup.1 and R.sup.

Abstract: A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, or --CONH--O--(CR.sup.3 R.sup.4).sub.m Z;R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl, cycloalkyl, --CF.sub.3, or F;Z is hydrogen, alkyl, --OR.sup.5, --SR.sup.5, --NR.sup.5 R.sup.6, --CN, --CF.sub.3, --OAr, --Ar, or R.sup.7 ;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl, or Ar;R.sup.7 is ##STR2## or --C.tbd.C--R.sup.11 ; R.sup.8, R.sup.9, R.sup.10, and R.sup.11 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, or phenyl, wherein the phenyl group may be optionally mono-, di-, or tri-substituted;Ar is an aryl radical that may be optionally mono-, di-, or tri-substituted; andm=1-6;with the proviso that R.sup.1 and R.sup.

Abstract: A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, or --CONH--O--(CR.sup.3 R.sup.4).sub.m Z;R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl, cycloalkyl, --CF.sub.3, or F;Z is hydrogen, alkyl, --OR.sup.5, --SR.sup.5, --NR.sup.5 R.sup.6, --CN, --CF.sub.3, --OAr, --Ar, or R.sup.7 ;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, alkoxykyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl, or Ar;R.sup.7 is ##STR2## or --C.tbd.C--R.sup.11 ; R.sup.8, R.sup.9, R.sup.10, and R.sup.11 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, or phenyl, wherein the phenyl group may be optionally mono-, di-, or tri-substituted;Ar is an aryl radio that may be optionally mono-, di-, or tri-substituted; and m=1-6;with the proviso that R.sup.1 and R.sup.

Abstract: A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, --CONR.sup.3 (CR.sup.4 R.sup.5).sub.m (CR.sup.6 R.sup.7).sub.n (CR.sup.8 R.sup.9).sub.p NR.sup.10 R.sup.11, or ##STR2## or --CONR.sup.3 R.sup.13 ; R.sup.3 is hydrogen, alkyl, or arylalkyl;R.sup.4, R.sup.5, R.sup.8, and R.sup.9 are each, independently, hydrogen, alkyl, --OH, --CF.sub.3, or --F;R.sup.6 is hydrogen or --OR.sup.13 ;R.sup.7 is hydrogen or alkyl;R.sup.10 is hydrogen, alkyl, or arylalkyl;R.sup.11, R.sup.12, and R.sup.13 are each, independently, --(CR.sup.15 R.sup.16).sub.r R.sup.17 ;R.sup.14 is hydrogen, alkyl of 1-6 carbon atoms, tri-(alkyl)silyl, tri-(alkyl)silylethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, or tetrahydropyranyl;R.sup.15 and R.sup.16 are each, independently, hydrogen or alkyl;R.sup.17 is ##STR3## or --C.ident.C--R.sup.21 ; R.sup.18, R.sup.19, R.sup.20, and R.sup.

Abstract: A compound of the structure ##STR1## where the substituents are defined in the specification.

Abstract: A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, --CONR.sup.3 (CR.sup.4 R.sup.5).sub.m (CR.sup.6 R.sup.7).sub.n (CR.sup.8 R.sup.9).sub.p NR.sup.10 R.sup.11, or ##STR2## or --CONR.sup.3 R.sup.13 ; R.sup.3 is hydrogen, alkyl, or arylalkyl;R.sup.4, R.sup.5, R.sup.8, and R.sup.9 are each, independently, hydrogen, alkyl, --OH, --CF.sub.3, or --F;R.sup.6 is hydrogen or --OR.sup.13 ;R.sup.7 is hydrogen or alkyl;R.sup.10 is hydrogen, alkyl, or arylalkyl;R.sup.11, R.sup.12, and R.sup.13 are each, independently, --(CR.sup.15 R.sup.16).sub.r R.sup.17 ;R.sup.14 is hydrogen, alkyl of 1-6 carbon atoms, tri-(alkyl)silyl, tri-(alkyl)silylethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, or tetrahydropyranyl;R.sup.15 and R.sup.16 are each, independently, hydrogen or alkyl;R.sup.17 is ##STR3## or --C.tbd.C--R.sup.21 ; R.sup.18, R.sup.19, R.sup.20, and R.sup.

Abstract: A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, or --CONH--O--(CR.sup.3 R.sup.4).sub.m Z;R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl, cycloalkyl, --CF.sub.3, or F;Z is hydrogen, alkyl, --OR.sup.5, --SR.sup.5, --NR.sup.5 R.sup.6, --CN, --CF.sub.3, --OAr, --Ar, or R.sup.7 ;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl, or Ar;R.sup.7 is ##STR2## or --C.tbd.C--R.sup.11 ; R.sup.8, R.sup.9, R.sup.10, and R.sup.11 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, or phenyl, wherein the phenyl group may be optionally mono-, di-, or tri-substituted;Ar is an aryl radical that may be optionally mono-, di-, or tri-substituted; andm=1-6;with the proviso that R.sup.1 and R.sup.