Abstract: This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and &agr;,&bgr;-unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.

Abstract: A method for the inhibition of high affinity glycine transporters, compounds that inhibit these transporters; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of disease states in which glycine is involved are disclosed.

Abstract: Novel mono- and dihydroxy phenylethylamine derivatives useful in treating melanoma are provided having the formulae (Ia, Ib or Ic). In the above formulae, Ra is hydrogen or —COORb, Rb is hydrogen or C1-6 alkyl; Re and Re independently represent hydrogen and hydroxy, Rf is hydrogen, C1-4? alkyl or halogen, X is —CHOH—, —CH2-oxygen or sulphur, m is zero or 1, W is oxygen or sulphur, and —ODrug, —NHDrug and —N(Drug)2 each represent a residue of a therapeutically active agent. The above compounds are prodrugs which are inactive until metabolised by enzymes expressed by host melanoma cells. The invention allows a greater amount of active agent to be used while reducing systemic side effects.

Abstract: Provided are a propenohydroxamic acid derivative represented by the following formula (1): 1

Abstract: The present invention provides hydroxamate compounds which are deacetylase inhibitors. The compounds are suitable for pharmaceutical compositions having anti-proliferative properties.

Abstract: N-Substituted-N′-substituted urea derivatives represented by the following formula, analogs thereof or pharmaceutically acceptable salts thereof are herein provided. These compounds show a TNF-&agr; production inhibitory activity.

Abstract: This invention is directed to aromatic sulfone hydroxamates (also known as “aromatic sulfone hydroxamic acids”) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.

Abstract: A compound of formula (I) wherein: R isopropyl; n is 0; R1 is naphthylmethyl; R2 is t-butyl; and R3 is methyl; is useful in the treatment of disorders mediated by s-CD23.

Abstract: The present invention provides the compound having the formula: 1

Abstract: Compounds having therapeutic utility are of formula (I)

Abstract: Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof.

Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes.

Abstract: The present invention relates to methods for the preparation of chemically aminoacylated tRNAs for the purpose of introduction of markers into nascent proteins. The present invention also relates to methods for the non-radioactive labeling, detection, quantitation and isolation of nascent proteins translated in a cellular or cell-free translation system utilizing chemically aminoacylated tRNAs. tRNA molecules are misaminoacylated with non-radioactive markers which may be non-native amino acids, amino acid analogs or derivatives. Markers may comprise cleavable moieties, detectable labels, reporter properties wherein markers incorporated into protein can be distinguished from unincorporated markers, or coupling agents which facilitate the detection and isolation of nascent protein from other components of the translation system.

Abstract: This invention relates to certain sulfonamide derivatives that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.

Abstract: The present application describes novel &bgr;-sulfone derivatives of formula I: 1

Abstract: Formula (I) compounds are described, where the groups are defined in the description, as well as processes for their preparation and their use as medicaments, particularly as selective phosphodiesterase IV inhibitors.

Abstract: The present invention provides a compound of formula (1), or pharmaceutical acceptable salts thereof wherein R1 is C4-12 alkyl, C4-12 alkenyl, C4-12 alkynyl, —(CH2)h-C3-8 cycloalkyl, substituted and unsubstituted —(CH2)h-aryl, substituted and unsubstituted-(CH2)h-het, R2 is substituted and unsubstituted C1-12 alkyl, substituted and unsubstituted C2-12 alkenyl, substituted and unsubstituted C2-12 alkynyl, substituted and unsubstituted-(CH2)h-C3-8 cycloakyl, substituted and unsubstituted —(CH2)h-C3-8 unsubstituted-(CH2)h-C3-8 cycloakyl, substituted and unsubstituted —(CH2)h-C3-8 cycloalkenyl, substituted and unsubstituted-(CH2)h-aryl, substituted and unsubstituted-(CH2)h-heterocyclic ring, substituted and unsubstituted —(CH2)i-X—R4 (X is —O—, —S(═O)j-, —NR7-, —S(═O)2NR8-, or —C(═O)—), and —(CH2)iCHR5R6.

Abstract: Phenylalanine derivatives of the following formula and analogues thereof have an antagonistic activity to &agr;4&bgr;7 integrin and a selectivity toward &agr;4&bgr;1 integrin. They are used as therapeutic agents for various diseases to which &agr;4&bgr;7 integrin relates.

Abstract: Novel cyclo azaphospha hydrocarbons according to formula I are provided. The compounds are useful as metalloprotease inhibitors.

Abstract: The present invention relates to certain tri-substituted phenyl derivatives and analogues of formula (I), to a process for preparing such compounds, having the utility in clinical conditions associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: Compounds of formula (I) wherein R is hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl or heterocyclyl; R1 is bicyclyl or heterobicyclyl; R2 is aryl, heteroaryl, heterocyclyl, alkoxy, alkyl, hydroxy or optionally substituted amino and n is from 0 to 3; with the provisos than when n is 0 R2 is alkyl or when n is from 1 to 3 R2 is not alkyl, are useful in the treatment and prophylaxis of conditions mediated by CD23 or TNF.

Abstract: A treatment and/or prevention agent for osteoarthritis comprising N-hydroxy-5-ethoxymethyloxy-2(S)-methyl-4(S)-(4-phenoxybenzoyl)amino pentanamide having an inhibitory activity of matrix metalloproteinases, or a non-toxic salt thereof as active ingredient.

Abstract: Hydroxamic and carboxylic acid derivatives having MMP and TNF inhibitory activity.

Abstract: Compounds having a zinc-binding moiety, such as, for example, a hydroxamic acid group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Inhibition of histone deacetylase can lead to the histone deacetylase-mediated transcriptional repression of tumor suppressor genes. For example, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, such as hematopoiesis, and genetic related metabolic disorders, such as, cystic fibrosis and adrenoleukodystrophy.

Abstract: A compound of the formula (I): R1—CO—N(OH)—CR2R3—CR4R5—CONH—CR6R7—CONR8R9  (I) wherein: R1 is C1-6alkyl, aryl or arylC1-6alkyl; R2 is hydrogen, C1-6alkyl, C3-8cycloalkyl, aryl or arylC1-6alkyl; R3 is hydrogen, C1-6alkyl or arylC1-6alkyl; or R2 and R3, together with the carbon atom to which they are joined, form a C3-8cycloalkyl ring; R4 is benzyl, phenethyl, phenylpropyl, phenylbutyl or flurophenylbutyl; R5 is hydrogen, C1-6alkyl or arylC1-6alkyl; R6 is hydrogen, C1-6alkyl, C2-6alkenyl, C3-8cycloalkylC1-6alkyl, arylC1-6alkyl, heteroarylC1-6alkyl or the side-chain of a naturally occurring amino acid; R7 is hydrogen or C1-6alkyl; R8 is hydrogen, C1-6alkyl, C3-8cycloalkyl, C3-8cycloalkenyl, arylC1-6alkyl, heteroarylC1-6alkyl or heterocyclylC1-6alkyl; R9 is hydrogen or C1-6alkyl; or R8 and R9, together with the nitrogen atom to which they are joined, form a heterocyclic ring; wherein any group or ring in R1-R9 is optionally substituted; or a pharma

Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.

Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.

Abstract: Compounds of formula I wherein R1, R2, A, X, Y and Z have the meanings provided in the specification, and their enantiomers, diastereoisomers, racemates, pharmaceutically acceptable salts and mixtures thereof. These compounds have HDAC inhibitory activity for inhibiting cell proliferation. Also provided is a process of manufacturing these compounds.

Abstract: Compounds of the formula B—X—(CH2)m—CR1R2—(CH2)n—CO—Y  (I) have therapeutic utility as inhibitors of metalloproteinases etc.

Abstract: The present invention relates to a novel class of organic molecules capable of inhibiting C-proteinase, and to their use to regulate, modulate and/or inhibit abnormal collagen formation as a therapeutic approach towards the treatment of fibrotic disorders.

Abstract: Novel hydroxamic acid compounds, e.g., of formula I, wherein R1, R2, R3 and R4 are as defined, are found to be useful as pharmaceuticals, e.g., for the suppression of TNF release and the treatment of autoimmune and inflammatory diseases, e.g., multiple sclerosis and rheumatoid arthritis. Methods of making the compounds, novel intermediates, and pharmaceutical compositions comprising the compounds are provided.

Abstract: Compounds having a zinc-binding moiety, such as, for example, a hydroxamic acid group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Inhibition of histone deacetylase can lead to the histone deacetylase-mediated transcriptional repression of tumor suppressor genes. For example, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, such as hematopoiesis, and genetic related metabolic disorders, such as, cystic fibrosis and adrenoleukodystrophy.

Abstract: The present invention relates to a silver halide color photographic light-sensitive material wherein at least one of light-sensitive silver halide emulsion layers includes a silver halide emulsion having a silver chloride content of at least 95 mol % and a silver iodide content of 0.05 mol % to 0.75 mol % and/or a silver bromide content of 0.05 mol % to 4.

Abstract: An aromatic sulfonyl alpha-hydroxy hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

Abstract: Compounds of formula (I) are antibacterials: 1

Abstract: An N-hydroxy sulfonyl butanamide compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated N-hydroxy sulfonyl butanamide compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

Abstract: Compounds having therapeutic utility are of formula (I) wherein B1, B2, R1 and R2 are each various sub-stituents, or R1 and R2 together form a ring.

Abstract: Compounds having a zinc-binding moiety, such as, for example, a hydroxamic acid group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Inhibition of histone deacetylase can lead to the histone deacetylase-mediated transcriptional repression of tumor suppressor genes. For example, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, such as hematopoiesis, and genetic related metabolic disorders, such as, cystic fibrosis and adrenoleukodystrophy.

Abstract: This invention provides processes for the preparation of a compound of Formula I:

Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states. The present invention provides low molecular weight, non-peptide inhibitors of matrix metalloproteinases (MMPs) and TNF-&agr; converting enzyme (TACE) for the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.

Abstract: A silver halide photographic material is described, which contains the compound represented by the following formula (I): wherein R1 represents a substituted or unsubstituted alkylene group having from 1 to 5 carbon atoms; X represents a water-soluble group; and R represents a substituted or unsubstituted alkyl group having the sum total of from 14 to 40 carbon atoms, an alkenyl group, an aryl group, an alkoxyl group, —NR3R4 (R3 and R4 each independently represents an alkyl group having from I to 40 carbon atoms, a hydrogen atom, or an aryl group), a bicycloalkyl group, a bicycloalkenyl group, a cycloalkyl group, a cycloalkenyl group or a heterocyclic group, provided that when X represents a quaternary ammonium salt structure, R2 does not represent an alkyl group having from 14 to 17 carbon atoms.

Abstract: A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

Abstract: Compounds of the formula: 1

Abstract: Monohydroxamate vanadium complexes of the formula (1): R—CO—NHOH.X, wherein R is a residue selected from: (i) H2N—CH(COY)—(CH2)n—, wherein n is 1, 2 or 3, and Y is OH or NH2; (ii) H2N—CH2—S—CH2—; and (iii) pyridyl, piperidyl or tetrahydroisoquinolinyl; and X is a vanadium compound selected from a vanadyl (VO2+), metavanadate (VO3−)or vanadate (VO43−)) salt, are useful for inducing normoglycemia and/or reducing blood glucose levels in diabetic patients.

Abstract: This invention relates to novel processes for preparing the pharmaceutically active compound 5-(3-[(2S)-exo-bicyclo[2.2.1]hept-2-yloxy]-4-methoxyphenyl)-3,4,5,6-tetrahydropyrimidin-2(1H)-one and its corresponding 2R enantiomer and for preparing certain intermediates used in the synthesis of these compounds. It also relates to novel intermediates used in the synthesis of such pharmaceutically active compounds and to other novel compounds that are related to such intermediates.

Abstract: The present invention provides compounds of formula I 1

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, AA and Y are as defined herein, inhibit phosphodiesterase type IV or inhibit the production of tumor necrosis factor, and therefore are useful in the treatment of certain conditions and diseases including asthma, arthritis, and sepsis.

Abstract: This invention provides processes for the preparation of a compound of Formula I:

Abstract: An aromatic sulfonyl alpha-hydroxy hydroxamic acid compound that, inter alia, inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.