Abstract: In general, the present invention relates to small molecule inhibitors of the heat shock protein 90 family of chaperone proteins. The invention also features pharmaceutical compositions and kits that include the compounds and compositions of the invention. The invention further relates to the medical use of these compounds and compositions for the treatment of neurodegenerative diseases.

Abstract: Compounds of formula (I) are inhibitors of p38 MAP kinase, useful as anti-inflammatory agents in the treatment of inter alia, diseases of the respiratory tract wherein; R1 is C1-C6 alkyl, C3-C6 cycloalkyl, phenyl which is optionally substituted, 5- or 6 membered monocyclic heteroaryl which is optionally substituted, or a radical of formula (II) wherein n is 1 or 2, and R3 and R4 are independently H or C1-C6 alkyl, or R3 and R4 taken together with the nitrogen to which they are attached form a 6-membered heterocyclic ring optionally containing a further heteroatom selected from N and O; Y is —O— or —S(O)p— wherein p is 0, 1 or 2; A is an optionally substituted divalent arylene radical, or a mono- or bicyclic heteroarylene radical, or a C3-C6 divalent cycloalkylene radical having 5 or 6 ring atoms, or a piperidinylene radical wherein the ring nitrogen is linked to R2NHC(?O)W—; W is a bond, —NH— or —C(RA)(RB), wherein RA and RB are independently H, methyl, ethyl, amino, hydroxyl or halo; and R2 is a radical as d

Abstract: Compounds of formula (I) are inhibitors of p38 MAP kinase, useful as anti-inflammatory agents in the treatment of inter alia, diseases of the respiratory tract wherein; R1 is C1-C6 alkyl, C3-C6 cycloalkyl, phenyl which is optionally substituted, 5- or 6 membered monocyclic heteroaryl which is optionally substituted, or a radical of formula (II) wherein n is 1 or 2, and R3 and R4 are independently H or C1-C6 alkyl, or R3 and R4 taken together with the nitrogen to which they are attached form a 6-membered heterocyclic ring optionally containing a further heteroatom selected from N and O; Y is —O— or —S(O)p— wherein p is 0, 1 or 2; A is an optionally substituted divalent arylene radical, or a mono- or bicyclic heteroarylene radical, or a C3-C6 divalent cycloalkylene radical having 5 or 6 ring atoms, or a piperidinylene radical wherein the ring nitrogen is linked to R2NHC(?O)W—; W is a bond, —NH— or —C(RA)(RB), wherein RA and RB are independently H, methyl, ethyl, amino, hydroxyl or halo; and R2 is a radical as d

Abstract: The invention relates to azabenzofuranyl compounds of Formula I with anti-cancer and/or anti-inflammatory activity and more specifically to azabenzofuranyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

Abstract: The invention relates to azabenzothiophenyl compounds of Formula I with anti-cancer and/or anti-inflammatory activity and more specifically to azabenzothiophenyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

Abstract: A compound of formula (I) wherein one of X and Y is silicon, and the other is carbon or silicon; Z is oxygen, sulphur or —N(R)—, wherein R is hydrogen or alkyl; R1 is hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy or cycloalkyl; and R2 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, -alkyl-cycloalkyl, -alkyl-heterocycloalkyl, -alkyl-aryl or -alkyl-heteroaryl; or a pharmaceutically acceptable salt thereof. The compounds are used in the manufacture of a medicament for the treatment or prevention of a disease or condition associated with GnRH (gonadotropin-releasing hormone), e.g. for the treatment or prevention of progression of cancer (e.g. leukaemia therapy), of a fertility disorder, of HIV infection or AIDS, of Alzheimer's disease of fibrosis, of endometriosis, of uterine fibroids or of uterine leiomyoma.

Abstract: Compounds of general formula (I): have utility as inhibitors of matrix metalloproteinases and TNF.

Abstract: The compound, according to formula (i) wherein X and Y are independently CH, N or N-oxide, provided that X and Y do not both represent CH; Z is CO or CS; R1 is alkyl, optionally substituted with one or more halogens; and R2, R3, R4 and R5 are each various organic groups. Such compounds have therapeutic utility, via inhibition of phosphodiesterase IV.

Abstract: Tripeptidyl derivatives having a SH or acylS group and which are amides, have therapeutic utility via MMP or TNF inhibition.

Abstract: Compounds of general formula (I): ##STR1## have utility as inhibitors of matrix metalloproteinases and TNF.

Abstract: Dipeptidyl derivatives having a SH of acylS group and which are amides, thioamides or S(O).sub.0-2 -amides, have therapeutic utility via MMP or TNF inhibition.

Abstract: Peptidyl compounds have therapeutic utility via MMP/TNF inhibition.

Abstract: The present invention concerns novel mercaptoalkylpeptidyl compounds of formula (I) which are useful inhibitors of matrix metalloproteinase and/or TNF-mediated diseases including degenerative diseases and certain cancers. The invention also concerns methods of treating patients suffering from disorders or diseases which can be attributed to or are associated with matrix metalloproteinase or TNF activity.

Abstract: Compounds of formula I ##STR1## where n=0-2;R.sup.1 is H, NH.sub.2 or a halogen;R.sup.2 is H or NH.sub.2 ;R.sup.3 is any of the four groups ##STR2## where m=0 or 1; andX is O, NR.sup.5, or S(O).sub.0-2 and, in group (b), the X's may be the same or different.Compounds of the invention have utility as inhibitors of purine nucleoside phosphyorylase (PNP).

Abstract: Peptidyl derivatives having a SH or acylS group and which are amides, primary amides or thioamides, have therapeutic utility via MMP or TNF inhibition.