Abstract: This invention relates to a method of treating inflammatory diseases in a mammal comprising administering to the mammal a therapeutically effective amount of a combination of: (i) at least one TACE inhibitor of Formula (I), (II), (III), or (IV) of the present invention or a stereoisomer or pharmaceutically acceptable salt form thereof, (ii) one or more anti-inflammatory agents selected from the group consisting of: selective COX-2 inhibitors, interleukin-1 antagonists, dihydroorotate synthase inhibitors, p38 MAP kinase inhibitors, TNF-&agr; inhibitors, TNF-&agr; sequestration agents, and methotrexate. The invention also relates to compositions and kits containing the same.

Abstract: A process for preparing an anti-microbial composition including mixing a liquid oxygen-generating base with a liquid acetyl radical generator. The generator contains n-acetylcaprolactam of between 40% and 60% inclusive by weight, alcohol of between 1% and 10% inclusive by weight, a surface active agent of between 0.001% and 20% inclusive by weight, a coloring agent of between 0.001% and 0.01% inclusive by weight, an anti-corrosive agent of between 0.001% and 40% inclusive by weight, and a glycolic derivative of between 0.001% and 10% inclusive by weight.

Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

Abstract: 4-Aryl-1-(indanmethyl, dibydrobenzofuramethyl or dihydrobenzotbiophenemethyl) piperidine, -tetrabydropyridine or -piperazine compounds of general formula (I) 1

Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.

Abstract: The present invention relates to compositions and methods to modulate &agr;-secretase and/or to improve cognitive ability. The invention further relates the improved/enhanced cognitive ability in diseased individuals, particularly Alzheimer's Disease patients, and treatment thereof through increased sAPP production. Macrocyclic lactones (i.e. bryostatin class and neristatin class) are compounds preferred for use with the present composition. The present invention also provides methods for increasing the generation of non-amyloidogenic soluble APP comprising the activation of protein kinase C (PKC) by administering an effective amount of PKC activator(s).

Abstract: A NK1 antagonist having the formula (I), with the variables defined herein, which is useful for treating a number of disorders, including emesis, depression, anxiety and cough.

Abstract: The present invention relates to certain substituted caprolactam carbonate and ether compounds, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for making said compounds.

Abstract: The present application describes novel lactams and derivatives thereof of formula I: 1

Abstract: This invention relates to novel lactams having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A&bgr;-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.

Abstract: This invention relates to novel lactams having the Formula (I): 1

Abstract: The present invention provides methods which use 4-amino-azepan-3-one protease inhibitors of cathepsin S in the treatment of diseases in which cathepsin S is implicated, especially treatment or prevention of autoimmune disease; treatment or prevention of a disease state caused by the formation of atherosclerotic lesions and complications arising therefrom; and diseases requiring inhibition, for therapy, of a class II MHC-restricted immune response, inhibition of an asthmatic response, inhibition of an allergic response, inhibition of immune response against a transplanted organ or tissue, or inhibition of elastase activity in atheroma, and novel compounds for use therewith.

Abstract: Mevinolin derivatives wherein the lactone ring is modified have interesting pharmaceutical properties, particularly in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1 interactions.

Abstract: The present invention relates to certain substituted caprolactam compounds, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for making said compounds.

Abstract: The present invention provides a compound represented by Formula: 1

Abstract: TNF-&agr; inhibitors containing a heterocyclic compound having angiotensin II antagonistic activity which are useful as preventives/remedies for inflammatory diseases, etc.

Abstract: The present invention relates to certain substituted caprolactam carbonate and ether compounds, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for making said compounds.

Abstract: The invention relates to a compound having the formula (I): R1SO2—B—X—Z—C(O)—Y, B is a bond, an amino acid of the formula —NR—CH[(CH2)pC(O)OH]—C(O)— or an ester derivative thereof wherein p is 1, 2, or 3, Gly, D-1-Piq, D-3-Piq, D-1-Tiq, D-3-Tiq, D-Atc, Aic, or a L- or D-amino acid having a hydrophobic, basic or neutral side chain; X is an amino acid with a hydrophobic side chain, glutamine, serine, theronine, a cyclic amino acid optionally containing an additional heteroatom selected from N, O or S, and optionally substituted with (1-6C)alkyl, (1-6C)alkoxy, benzyloxy or oxo, or X is 2-amino-isobutyric acid, —NR2—CH2—C(O)— or the fragment (I) or (II), wherein n is 2, 3, or 4, W is CH or N and R3 is H, (1-6C)alkyl or phenyl which groups may optionally be substituted with hydroxy, (1-6C)alkoxy, COOH, COO(1-6C)alkyl, CONH2, or halogen; Z is lysine or 4-aminocyclohexylglycine.

Abstract: Sulfonyl derivatives represented by general formula (I), salts of the same, and solvates of both: and application of them as drugs: [wherein R1 is hydrogen, hydroxyl, nitro or the like; R2 and R3 are each independently hydrogen, halogeno or the like; R4 and R5 are each dependently hydrogen, halogeno or the like; Q1 is an optionally substituted saturated or unsaturated 5- or 6-membered cyclic hydrocarbon group or the like; Q2 is a single bond, oxygen or the like; Q3 is, e.g., a group represented by formula (a): T1 is carbonyl or the like; and X1 and X2 are each independently methylidyne or nitrogen]. These compounds exhibit potent Fxa inhibiting activities and serve as excellent anticoagulants which speedily exert satisfactory and persistent anti-thrombotic effects through oral administration and little cause adverse effects.

Abstract: Compounds, compositions and methods are disclosed useful for enhancing penetration of a pharmacologically active substances across skin or tissue membranes. Compounds for use in such compositions and methods are highly water-soluble N-substituted polyalkylene oxide derivatives of cyclic amides. A compound of the invention has the structural formula: wherein m is an integer from 2 to about 6, n is an integer from 1 to about 8, and R is hydrogen, trimethylsilyl or lower alkyl.

Abstract: The present invention relates to lactam derivatives of the formula 1

Abstract: Compound of the formula are inhibitors of the enzyme Factor Xa. These compounds are useful as anticoagulants in the treatment of cardiovascular diseases associated with thromboses.

Abstract: Hydroxamic acids are provided which are ACE and/or NEP inhibitors and have the structure wherein R*, R and R1 are as defined herein and A is a dipeptide preferably derived from an amino acid, or is a conformationally restricted dipeptide mimic.

Abstract: Compounds of formula (I) are antibacterial agents wherein: R3 and R4, taken together with the carbon atoms to which they are respectively attached, form an optionally substituted saturated carbocyclic or heterocyclic ring of 5 to 16 atoms, which may be benz-fused or fused to a second optionally substituted saturated carbocyclic or heterocyclic ring of 5 to 16 atoms; and R1 and R2 are as defined in the specification.

Abstract: This invention relates to novel lactams having the Formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A&bgr;-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.

Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.

Abstract: The present invention provides compounds that block calcium channels and have the Formula I: The present invention also provides pharmaceutical compositions containing the compounds of Formula I and methods of using them to treat stroke, cerebral ischemia, head trauma, and epilepsy.

Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

Abstract: This invention relates to novel lactams having the Formula (I): 1

Abstract: A condensed thiophene compound of the formula (I) wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof and hydrates thereof. The compound of the formula (I) of the present invention is useful as a novel antipsychotic agent which is effective for both positive symptoms and negative symptoms of schizophrenia, which is associated with less side effects such as extrapyramidal motor disorder and the like and which is less associated with serious side effects such as agranulocytosis and the like. In addition, this compound is also useful as a therapeutic agent of Alzheimer's disease and manic-depressive illness.

Abstract: The present invention relates to an improved process for preparing certain substituted caprolactam compounds which comprises acylating an aminocaprolactam compound with a lactone compound in the presence of a weak base and a polar, organic solvent, and hydrolyzing the resultant diamide compound in a mixture of solvents to obtain the desired caprolactam compound.

Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

Abstract: This invention relates to novel cyclic malonamides having the formula (I): 1

Abstract: The present invention relates to compounds of the formula 1

Abstract: The present invention relates to compounds of the formula 1

Abstract: The present invention relates to compounds of the formula 1

Abstract: The present invention relates to certain substituted caprolactam carbonate and ether compounds, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for making said compounds.

Abstract: The present invention relates to compounds of the formula 1

Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

Abstract: The present application describes novel lactams and derivatives thereof of formula I: 1

Abstract: Lactam inhibitors are provided which have the structure X is wherein Y is O or S and R4 is  R7O— or R8 and R1, R2, R3, R5, R6, R7, and R8, are as defined herein. These compounds are inhibitors of Factor Xa and thus are useful as anticoagulants, and are inhibitors of tryptase and thus are useful in treating asthma. Methods for treating cardiovascular diseases associated with thromboses and for treating asthma and related diseases are also provided.

Abstract: This invention relates to novel lactams having the Formula (I): 1

Abstract: Vasopeptidase inhibitors, especially omapatrilat, are useful in treating isolated systolic hypertension. The vasopeptidase inhibitor may be used in combination with other pharmaceutically active agents.

Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: 1

Abstract: The present invention relates to certain substituted caprolactam compounds, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for making said compounds.

Abstract: Caprolactam inhibitors are provided which have the structure including pharmaceutically acceptable salts thereof and all stereoisomers thereof, and prodrugs thereof, wherein n is 1 to 5; and and Y R1, R2, R3, R5, R5a, R6, R7, R8, R9 and R10 are as defined herein. These compounds are inhibitors of Factor Xa and thus are useful as anticoagulants. A method for treating cardiovascular diseases associated with thromboses is also provided.

Abstract: The invention relates to pharmaceutical compositions for topical application containing at least one physiologically active agent and an effective amount of 1-oleylazacycloheptan-2-one as the human or animal epithelial membrane permeability enhancer, to the application of such pharmaceutical compositions by means of locally contacting the skin or other membrane of the human or animal with the above composition and to the 1-oleylazacycloheptan-2-one compound per se.

Abstract: The present invention is directed to azepan-2-one compounds which inhibit prenyl-protein transferase, particularly farnesyl-protein transferase (Ftase), and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

Abstract: The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, for treating a patient suffering from, or subject to, a physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.