Abstract: This invention provides quinazolines that are useful for treating cell proliferative diseases and disorders, such as cardiovascular diseases, infections, cancers, autoimmune diseases, gout, kidney disease, and neurodegenerative diseases and disorders such as Alzheimer's disease. We have now discovered a group of 2-arylamino-7-(alkyl)oxy-8-alkylquinazolines and 8-alkyl-2-arylamino-quinazoline 2,7-diamines that are potent inhibitors of cyclin-dependent kinases (cdks). The compounds are readily synthesized and can be administered by a variety of routes, including orally, and have sufficient bioavailability. This invention also provides pharmaceutical formulations comprising at least one of the quinazoline compounds together with a pharmaceutically acceptable carrier, diluent, or excipient therefor. The invention further provide useful intermediates generated during the production of the quinazoline compounds.

Abstract: The present invention relates to substituted piperidines of general formula wherein A1, A2, R, R1 and R2 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, particularly CGRP-antagonistic properties, pharmaceutical compositions containing these compounds, their use and processes for preparing them.

Abstract: A compound represented by the formula I: wherein A represents the following heterocycles: and R1-9 are as defined herein, a composition containing this compound and methods for treating disorders of the serotonin-affected neurological systems utilizing such a compound or composition.

Abstract: The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase inhibitor, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one phosphodiesterase inhibitor, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents.

Abstract: Quinoline and quinazoline derivatives can be used in the form of pharmaceutical preparations as Neuropeptide Y antagonists for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.

Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereon wherein —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a

Abstract: A febrifugine represented by Formula (A): and an isofebrifugine represented by Formula (B): which exhibit extremely strong activities against tropical malarial protozoan are provided, together with a total synthesis route which enables efficient large scale synthesis of the same.

Abstract: A pharmaceutical compound of the formula (I) in which R1 and R2 are each hydrogen or C1-6 alkyl, R3 is —SR10, —SOR10, —SO2R10, —COR10, —CH2OH or —CONHR11, where R10 is C1-6 alkyl and R11 is hydrogen or C1-6 alkyl, R4, R5, R6 and R7 are each hydrogen or C1-6alkyl, provided that at least one of R4, R5, R6 and R7 is C1-6alkyl, R8 and R9 are each hydrogen, halo, C1-6 alkyl or cyano, n is 0 or 1 and m is 2 or 3, x is a (a) or (b), and y is (c) or (d), wherein R12 and R13 are each hydrogen, C1- alkyl, cyclopropyl or cyclopropyl-C1-6 alkyl; and salts thereof.

Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

Abstract: The use of ketanserin in combination with L-carnitine, some alkanoyl L-carnitines and the pharmacologically acceptable salts thereof is disclosed for the treatment of CRPS.

Abstract: Compounds represented by Formula (I): (I)or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.

Abstract: The present invention provides a method for the treatment or prevention of thrombocythemia in a patient comprising administering to said patient an effective amount of anagrelide, anagrelide in base form, or a pharmaceutically acceptable salt of anagrelide in a manner whereby first pass liver metabolism is avoided.

Abstract: A compound represented by the formula I: 1

Abstract: Piperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.

Abstract: Piperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.

Abstract: This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R1 is C1-6alkyloxy, C2-6alkenyloxy or C2-26alkynyloxy; R2 is hydrogen or C1-6alkyloxy, or when taken together R1 and R2 may form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl, R3 is hydrogen or halo; L is C3-6cycloalkyl, C5-6cycloalkanone, C2-6alkenyl optionally substituted with aryl, or L is a radical of formula —Alk—R4, —Alk—NR5R6, 1-R6-4-piperidinyl, Alk—X—R7, —Alk—Y—C(═O)—R9, or —Alk—Y—C(═O)—NR11R12 wherein each Alk is C1-12alkanediyl; R4 is hydrogen, C1-6alkylsulfonylamino, C3-6cycloalkyl, C5-6cycloalkanone, Ar—, di(Ar)methyl, Ar-oxy- or Het1; R5 is hydrogen or C1-6alkyl; R6 is Het2; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloa

Abstract: This invention relates to peptidyl compounds of the formulas (I) and (II) active as cathepsin S, a cysteine protease, inhibitors. The compounds are selective, reversible inhibitors of the cathepsin S are therefore useful in the treatment of autoimmune and other diseases. The invention also relates to processes for preparing such compounds and pharmaceutical compositions comprising them.

Abstract: The present invention relates to compositions containing quinazolinones. More particularly, the present invention relates to a composition for the treatment of renal fibrosis. This composition includes, as an active ingredient, a quinazolinone derivative such as halofurginone, which is shown herein to slow or prevent progression of renal fibrosis in vivo thereby mitigating or preventing end-stage renal failure.

Abstract: Novel compounds of the formula 1

Abstract: The present invention provides a pharmaceutical composition which is useful as a phosphatidylinositol 3 kinase (PI3K) inhibitor and an antitumor agent, and it provides a novel bicyclic or tricyclic fused heteroaryl derivative or a salt thereof which possesses an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity.

Abstract: Heterocyclylalkylpiperidine derivatives of general formula (I) 1

Abstract: Compounds, compositions and methods useful for treating cellular proliferative diseases and disorders, for example, by modulating the activity of KSP, are disclosed.

Abstract: Piperidine derivatives of formula (I) and pharmaceutically derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.

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

Abstract: There are provided compounds which can be used in the treatment of diseases mediated by the autophosphorylation of a PDGF receptor, specifically, compounds which can inhibit neointima formation hypertrophy.

Abstract: Combinations of atorvastatin and &agr;1 adrenergic receptor antagonists, the use of such combinations in the treatment of benign prostatic hyperplasia (BPH), methods of treating BPH using such combinations and medicaments containing such combinations are described.

Abstract: Aminopiperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.

Abstract: The use of 4-amino-6,7-dimethoxy-2-(5-methanesulfonamido-1,2,3,4-tetrahydroisoquinol-2-yl)-5-(2-pyridyl)quinazoline, or a pharmaceutically acceptable derivative thereof, for treating LUTS associated with: OAB (with or without concomitant detrusor over activity); pelvic floor dysfunction; or chronic prostatitis, is described.

Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein Z1 and Z2 are each independently nitrogen or CH and Ring A, TmR1, QR2, UnR3, and Sp are as described in the specification. The compounds are especially useful as inhibitors of ERK2 and for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, diabetes, and cardiovascular disease.

Abstract: The invention concerns compounds corresponding to general formula (I), wherein, in particular: W represents hydrogen, COR6, CSR6, SO2R6, CO(CH2)nR6, (CH2)nR7; X represents CH or N; Y represents (CH2)n, CO, CH2CO, CH═CHCO, CH2CH2CO; Z represents a heterocycle. When Z=pyridine, then Y is other than CO. R1 represents hydrogen, C1-C6 alkyl, halogen OCH3, CF3; R2 and R3, identical or different, represent hydrogen, C1-C6 alkyl; R4 represents a) hydrogen, b) C1-C6 alkyl, c) an aryl, d) a heterocycle; R5 represents hydrogen, COR7R8, SO2R7, CO(CH2)nSR7, CO(CH2)nOR7, CONR7R8, CO(CH2)mCOR7; R6 represents a) a phenyl or a naphthyl, b) a C1-C6 alkyl, a cycloalkyl, c) a heterocycle, d) NR7R8; R7 and R8, identical or different, represent a) hydrogen, C1-C15 alkyl, b) a heterocycle, c) an aryl; n represents 0 to 10; m represents 2 to 10; provided that when Z represents a quinozaline or benzimidazole group, then R5 is other than CH2Ph or methyl and n is other than zero.

Abstract: The present invention relates to the method of treating cough with ORL-1 agonists, alone or in combination with additional agents for treating symptoms of cough, allergy or asthma, pharmaceutical compositions comprising the combinations, and to compounds of the formula 1

Abstract: The present invention relates to compounds of Formula (I) 1

Abstract: Aminopiperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.

Abstract: Malaria is the most severe tropical parasitic disease that has caused millions of deaths in many countries. The threat of growing drug-resistant parasites requires development of new antimalarial drugs to overcome the emergence of resistance and to control the disease. Febrifugine is the active principle extracted from the Chinese herb Chang Shan (Dichroa febrifuga Lour) that has been used to treat malaria for more than two thousand years. Studies on the efficacy have been hindered due to the emetic effects of febrifugine. The present invention discloses febrifugine, halofuginone and febrifugine derivatives for use as antimalarial agents without the severe emetic effects observed in direct herbal use.

Abstract: Dihydroquinazoline derivatives of the formula where R3 is —(CH2)p—A where p is from 1 to 4 and A is a 5- or 6-membered N-containing heterocyclic ring attached via the N atom or A is —NA′A″ wherein A′ and A″ are the same or different and are each a C1-C4 alkyl group or their pharmaceutically acceptable salts possessing anti-cancer activity.

Abstract: A composition for treating hepatic fibrosis and a method of using and manufacturing the composition are provided. The composition includes a quinazolinone derivative, preferably Halofuginone.

Abstract: Aminopiperidine derivatives of formula (I) and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.

Abstract: Compounds of formula I 1

Abstract: Compounds of formula (I): 1

Abstract: Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds of the present invention are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease.

Abstract: The present invention provides novel methods of inhibiting pathological conditions related to organ systems which respond to estrogen agonists comprising administering to a mammal in need of such treatment an effective amount of a compound of formula I 1

Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R2, R3, R4, R5, R6, R7, R8, Het and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.

Abstract: The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula I: 1

Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R2, R3, R4, R5, R6, R7, R8, Het and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.

Abstract: The present invention relates to the use of specific EGF-receptor antagonists for preparing a pharmaceutical composition for the prevention and/or treatment of benign prostatic hyperplasia and/or prostatic hypertrophy, a method for the treatment or prevention of benign prostatic hyperplasia/prostatic hypertrophy comprising administering an EGF-receptor antagonist of groups (A), (B) or (C), described herein optionally in combination with known compounds for the treatment of benign prostatic hyperplasia/prostatic hypertrophy, as well as associated pharmaceutical compositions.

Abstract: This invention relates to compounds that are efflux pump inhibitors and therefore are useful as potentiators of anti-fungal agents for the treatment of infections caused by fungi that employ an efflux pump resistance mechanism.

Abstract: Piperidine derivatives of formula (I) or a pharmaceutically acceptable derivative thereof and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.

Abstract: A compound given by general formula (1): [wherein T represents oxygen or sulfur atom, Y represents alkyl, cycloalkyl group, etc., ring W represents benzene ring, etc., R1 and R2 represent independently hydrogen atom, lower alkyl group, etc., and R3 represents hydrogen atom, alkyl group, etc. Z represents a group given by formula: {wherein A1 and A2 represent independently hydrogen atom, alkyl group, etc. and G represents straight chain alkylene having 1-6 of the carbon number, etc.} or a group given by formula: {wherein n represents 0, 1 or 2, ring E represents 4-8 membered saturated heterocyclic ring containing nitrogen atom(s), and A3 represents hydrogen atom, alkyl group, etc.}], its prodrug or pharmaceutically acceptable salt thereof is an antagonist against muscarinic receptor that is useful as anticholinergic medicaments, and therefore it is useful as pollakiuria or urinary incontinence remedy.

Abstract: The invention relates to compounds of formula I D—CO—B—A-Het and pharmaceutically acceptable salts thereof where substituents in description have the specified meanings. The compounds are used as thrombin inhibitors.

Abstract: The present invention relates to methods for modulating the cholesterol biosynthetic pathway. The level of cholesterol in the body is linked to numerous pathological states. The methods of the present invention alter the transcription levels of genes involved in the cholesterol biosynthesis. The methods of the present invention can used for treating diseases mediated by the cholesterol biosynthetic pathway.