Abstract: The present invention relates to novel substituted imidazo[1,2-b]pyridazine compounds of Formula (I): pharmaceutical compositions thereof, and the use such compounds as corticotropin releasing factor 1 (CRF1) receptor antagonists in the treatment of psychiatric disorders and neurological diseases.

Abstract: The present invention is directed to compounds represented by the following structural Formula (I), (a) R1 is selected from the group consisting of hydrogen, substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-4-alkyl, heteroaryl-C0-4-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl, and —CH2—C(O)—R17-R18, wherein R17 is O or NH and R18 is optionally substituted benzyl; (b) R2 is selected from the group consisting of C1-C6 alkyl, C1-C6 alkenyl, aryl-C0-4-alkyl, heteroaryl-C0-4-alkyl, C1-C4 alkyl sulfonamide, C1-C4 alkyl amide, OR10 and C3-C6 cycloalkyl; (c) W is O or S; (d) X is an optionally substituted C1-C5 alkylene linker wherein one carbon atom of the linker may optionally be replaced with O, NH, S, and optionally two carbons together may form a double bond; (e) Y is selected from the group consisting of C, O, S, NH and a single bond; and (f) E is selected from the group consisting of C(R3)(R4)A, A, and a substituted or unsubstituted group selected from the group consisting of (CH2)n COOR19.

Abstract: The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-2-alkyl, heteroaryl-C0-2-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl or phenyl. W is O or S. R2 is H or a substituted or unsubstituted group selected from C1-C6 alkyl, C3-C6 cycloalkyl and heteroaryl. X is a C2-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S. Y is C, O, S, NH or a single bond. Furthermore, E is (CH2)nCOOH, wherein n is 0, 1, 2 or 3, or C(R3)(R4)A, wherein A is an acidic functional group such as carboxyl, carboxamide substituted or unsubstituted sulfonamide, or substituted or unsubstituted tetrazole. R3 is H, saturated or unsaturated C1-C5 alkyl, C1-C5 alkoxy.

Abstract: The present invention relates to novel substituted imidazo[1,2-b]pyridazine compounds of Formula (I): pharmaceutical compositions thereof, and the use such compounds as corticotropin releasing factor 1 (CRF1) receptor antagonists in the treatment of psychiatric disorders and neurological diseases.

Abstract: The present invention provides a process for selectively acylating an A82846A, A82846B, A82846C or PA-42867-A glycopeptide at the N1, N2 or N3 positions and the monoacylated compounds prepared therefrom.

Abstract: The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-2-alkyl, heteroaryl-C0-2-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl or phenyl. W is O or S. R2 is H or a substituted or unsubstituted group selected from C1-C6 alkyl, C3-C6 cycloalkyl and heteroaryl. X is a C2-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S. Y is C, O, S, NH or a single bond. Furthermore, E is (CH2)nCOOH, wherein n is 0, 1, 2 or 3, or C(R3)(R4)A, wherein A is an acidic functional group such as carboxyl, carboxamide substituted or unsubstituted sulfonamide, or substituted or unsubstituted tetrazole. R3 is H, saturated or unsaturated C1-C5 alkyl, C1-C5 alkoxy.

Abstract: The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is selected from the group consisting of hydrogen, substituted or unsubstituted group selected from C1–C8 alkyl, aryl-C0-4-alkyl, heteroaryl-C0-4-alkyl, and C3–C6 cycloalkylaryl-C0-2-alkyl; W is O or S; X is an optionally substituted C1–C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S; Y is C, O, S, NH or a single bond; E is C(R3)(R4)A or A

Abstract: The present invention is directed to N1-acylated derivatives of desleucylA82846B. These derivatives are useful as antibacterials.

Abstract: The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is selected from the group consisting of hydrogen, substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-4-alkyl, heteroaryl-C0-4-alkyl, and C3-C6 cycloalkylaryl-C0-2-alkyl; W is O or S; X is an optionally substituted C1-C5 alkylene linker wherein one carbon atom the linker may be replaced with O, NH or S; Y is C, O, S, NH or a single bond; E is C(R3)(R4)A or A.

Abstract: The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-2-alkyl, heteroaryl-C0-2-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl or phenyl. W is O or S. R2 is H or a substituted or unsubstituted group selected from C1-C6 alkyl, C3-C6 cycloalkyl and heteroaryl. X is a C2-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S. Y is C, O, S, NH or a single bond. Furthermore, E is (CH2)nCOOH, wherein n is 0, 1, 2 or 3, or C(R3)(R4)A, wherein A is an acidic functional group such as carboxyl, carboxamide substituted or unsubstituted sulfonamide, or substituted or unsubstituted tetrazole. R3 is H, saturated or unsaturated C1-C5 alkyl, C1-C5 alkoxy.

Abstract: Described herein are N′-acylated derivatives of desleucylA82846B. The compounds are useful as antibacterial agents.

Abstract: The present invention is directed to N.sup.1 -alkylated derivatives of desleucyl A82846B. These derivatives are useful as antibacterials and also as starting materials from which further antibacterial compounds are prepared.

Abstract: The present invention is directed to glycopeptides and more particularly to derivatives of the glycopeptide A82846B. In these derivatives, the leucyl has been removed to create "hexapeptides" of A82846B and its N.sup.DISACC variations. These hexapeptides are useful as antibacterials and also as starting materials from which further antibacterial compounds are prepared.

Abstract: The present invention is directed to N.sup.LEU -carbamoyl and thiocarbamoyl derivatives of A82846B and N.sup.DISACC variations thereof. These derivatives are useful as antibacterials and also as starting materials from which further antibacterial compounds are prepared.