Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1? converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-?-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-?-mediated diseases and decreasing IGIF and IFN-? production using the compounds and compositions of this invention.

Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1? converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-?-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-?-mediated diseases and decreasing IGIF and IFN-? production using the compounds and compositions of this invention.

Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1? converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-?-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-?-mediated diseases and decreasing IGIF and IFN-? production using the compounds and compositions of this invention.

Abstract: A series of 5,6-dihydro-1,3-benzothiazol-7(4H)-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PD kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.

Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1? converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-?-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-?-mediated diseases and decreasing IGIF and IFN-? production using the compounds and compositions of this invention.

Abstract: A series of 5,6-dihydro-1,3-benzothiazol-7(4H)-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PD kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.

Abstract: Pyrimidines of formula (1) are described 1

Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1&bgr; converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-&ggr;-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-&ggr;-mediated diseases and decreasing IGIF and IFN-&ggr; production using the compounds and compositions of this invention.

Abstract: Fused polycyclic 2-aminopyrimidines of formula (1): wherein Ar is an optionally substituted aromatic or heteroaromatic group; X is a carbon or nitrogen atom; Y is a carbon or nitrogen atom; Z is a linker group; A together with X and Y forms an optionally substituted monocyclic or bicyclic aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof are described. The compounds are potent and selective inhibitors of the protein tyrosine kinases p56lck and p59fyn and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate p56lck and/or p59fyn activity is believed to have a role.

Abstract: Pyrimidines of formula (1) are described wherein Ar is an optionally substituted aromatic or heteroaromatic group; R1 is a hydrogen atom or a straight or branched chain alkyl group; R2 is a —X1—R3 group where X1 is a direct bond or a linker atom or group, and R3 is an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective KDR Kinase and/or FGFr Kinase inhibitors and are of use in the prophylaxis and treatment of disease states assoicated with angiogenesis.

Abstract: Compounds of general formula (1) are described wherein: Ar is an optionally substituted aromatic group; R2 is a hydrogen or halogen atom or a group —X1—R2a where X1 is a direct bond or a linker atom or group, and R2a is an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; R3 is an optionally substituted heterocycloalkyl group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective protein tyrosine kinase inhibitors, particularly the kinases ZAP-70 and syk and are of use in the prophylaxis and treatment of immune or allergic diseases and diseases involving inappropriate platelet activation.

Abstract: Pyrimidines of formula (1) are described 1

Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1&bgr; converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-&ggr;-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-&ggr;-mediated diseases and decreasing IGIF and IFN-&ggr; production using the compounds and compositions of this invention.

Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-IB converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against IL-1-, apoptosis-, IGIF-, and IFN-&ggr;-mediated diseases, inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, degenerative diseases, and necrotic diseases. This invention also relates to methods for inhibiting ICE activity, for treating interleukin-1-, apoptosis-, IGIF- and IFN-&ggr;-mediated diseases and decreasing IGIF and IFN-&ggr; production using the compounds and compositions of this invention.

Abstract: The present invention relates to pyradazino[1,2-a][1,2]diazepine-1-carboxamide compounds of formula: which compounds are inhibitors of interleukin-1beta converting enzyme.

Abstract: Fused polycyclic 2-aminopyrimidines of formula (1) are described: whereinR.sup.1 is a group --L.sup.1 R.sup.2 where L.sup.1 is a covalent bond or a linker atom or group and R.sup.2 is a group --(Alk).sub.m L.sup.2 R.sup.3 where Alk is an optionally substituted aliphatic or heteroaliphatic chain, m is zero or the integer 1, L.sup.2 is a covalent bond or a linker atom or group and R.sup.3 is an optionally substituted cycloaliphatic or heterocycloaliphatic group provided that when m is zeroL.sup.2 is a covalent bond;Ar is an aryl or heteroaryl group;X is a carbon or nitrogen atom;Y is a carbon or nitrogen atom;Z is a linker group;A together with X and Y forms an optionally substituted monocyclic or bicyclic aromatic or heteroaromatic group;and the salts, solvates, hydrates and N-oxides thereof.

Abstract: Compounds of general formula (1) ##STR1## are described wherein: Ar is an optionally substituted aromatic group;R.sup.2 is a hydrogen or halogen atom or a group --X.sup.1 --R.sup.2a where X.sup.1 is a direct bond or a linker atom or group, and R.sup.2a is an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group;R.sup.3 is an optionally substituted heterocycloalkyl group; and the salts, solvates, hydrates and N-oxides thereof.The compounds are selective protein tyrosine kinase inhibitors, particularly the kinases ZAP-70 and syk and are of use in the prophylaxis and treatment of immune or allergic diseases and diseases involving inappropriate platelet activation.

Abstract: Compounds of general formula (1): ##STR1## are described wherein Het is an optionally substituted heteroaromatic group; R.sup.1 is a hydrogen atom or a straight or branched chain alkyl group; R.sup.2 is a hydrogen or halogen atom or a group --X.sup.1 --R.sup.2a where X.sup.1 is a direct bond or a linker atom or group, and R.sup.2a is an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; R.sup.3 is an optionally substituted aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective protein kinase inhibitors, particularly the kinases p56.sup.lck, ZAP-70 and protein kinase C and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to have a role.

Abstract: Fused polycyclic 2-aminopyrimidines of formula (1): ##STR1## wherein Ar is an optionally substituted aromatic or heteroaromatic group;X is a carbon or nitrogen atom;Y is a carbon or nitrogen atom;Z is a linker group;A together with X and Y forms an optionally substituted monocyclic or bicyclic aromatic or heteroaromatic group;and the salts, solvates, hydrates and N-oxides thereof are described. The compounds are potent and selective inhibitors of the protein tyrosine kinases p56.sup.lck and p59.sup.fyn and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate p56.sup.lck and/or p59.sup.fyn activity is believed to have a role.

Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1.beta. converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against an IL-1 mediated disease, an apoptosis mediated disease, AML, CML, melanoma, myeloma, Kaposi's sarcoma, graft vs host disease, rheumatoid arthritis, inflammatory bowel disorder, psoriasis, osteoarthritis, myeloma, apoptosis, sepsis, rheumatoid arthritis, asthma, Alzheimer's disease, Parkinson's disease, and ischemic heart disease diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.