Abstract: The invention described herein relates to a process for the preparation of (7-(3-carboxyphenyl)-4-chloroisoquinolin-1-yl)guanidine (I), intermediates thereto and new forms and formulations thereof, including the zwitterion monohydrate of (I), suitable for pharmaceutical use.

Abstract: This invention relates to a group of quinolyl, isoquinolyl and pyridyl ureas, their the use in treating raf mediated diseases, and pharmaceutical compositions which contain these ureas for use in such therapy.

Abstract: Compounds having the formula (I), are useful as serine protease inhibitors, more particularly inhibitors of Factors VIIa, IXa, Xa, and/or XIa, wherein ring B is phenyl or pyridyl, W is preferably C(═O)NR4R5, L is a linker group, X2 comprises nitrogen or carbon, Z is an optionally-substituted monocyclic or bicyclic ring system, and R1, R2, R3, R4, R5 and R6 are as defined in the specification.

Abstract: The invention relates to a compound having the formula (I) wherein R1 is cyclopentyl, cyclohexyl or a branched (3-4C)alkyl; R2 is cyclohexyl or phenyl; R3 is H or methyl; and A is an unsubstituted saturated 4, 5 or 6-membered ring; or a pharmaceutically acceptable salt thereof. The compounds of the invention have anticoagulant activity and can be used in treating or preventing thrombin-mediated and thrombin-associated diseases.

Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

Abstract: The invention is related to compounds of formula I 1

Abstract: The invention concerns compounds of general formula (I) wherein: 1

Abstract: The present invention provides methods of treating vascular diseases where nitric oxide insufficiency is a contributing factor by administering a therapeutically effective amount of at least one antioxidant, or a pharmaceutically acceptable salt thereof, and at least one of isosorbide dinitrate and isosorbide mononitrate, and, optionally, at least one nitrosated angiotensin-converting enzyme inhibitor, nitrosated beta-adrenergic blocker, nitrosated calcium channel blocker, nitrosated endothelin antagonist, nitrosated angiotensin II receptor antagonist, nitrosated renin inhibitor, and/or at least one compound used to treat cardiovascular diseases. The antioxidant is preferably a hydralazine compound or a pharmaceutically acceptable salt thereof.

Abstract: A variety of small, guanidino group-containing molecules capable of acting as MC4-R agonists are provided. The compounds have various structures provided herein. The compounds are useful in treating MC4-R mediated diseases and may be formulated into pharmaceutical formulations and compositions.

Abstract: The invention provides compounds which inhibit reverse transcriptase (RT) and which inhibit replication of a retrovirus, such as human immunodeficiency virus-1 (HIV-1). The compound of the invention are phenoxyethyl-thiourea-pyridines. The invention additionally provides a method for inhibiting reverse transcriptase activity of a retrovirus, such as HIV-1, comprising contacting the retrovirus with a compound of the invention. The invention additionally provides a method for inhibiting replication of a retrovirus, such as HIV-1, comprising contacting the retrovirus with a compound of the invention.

Abstract: The invention relates to the use of 2 amino-nicotinamide derivatives of formula I wherein n is from 1 up to and including 6; W is O or S; R1 and R3 represent independently of each other hydrogen, lower alkyl or lower acyl; R2 represents a cycloalkyl group, an aryl group, or a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms and 0, 1 or 2 heteroatoms independently from each other selected from the group consisting of oxygen and sulfur, which groups in each case are unsubstituted or mono- or polysubstituted; R and R′ are independently of each other hydrogen or lower alkyl; X represents an aryl group, or a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms and 0, 1 or 2 heteroatoms independently from each other selected from the group consisting of oxygen and sulfur, which groups in each case are unsubstituted or mono- or polysubstituted; or a N-oxide, a possible tautomer thereof or a pharmaceutically acceptable salt of such a

Abstract: The present invention relates to molecules derived from guggulipid extract which are capable of reducing insulin resistance in humans. The invention further relates food compositions and medicaments comprising such molecules which can be used to treat and/or prevent insulin resistance and the symptoms thereof.

Abstract: This invention describes novel pyrazole compositions comprising a pharmaceutically acceptable carrier and a compound of formula V: wherein Z1 is N, CRa, or CH, and Z2 is N or CH, provided one of Z1 and Z2 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or two ortho substituents independently selected from —R1; Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; Rx and Ry are independently selected from T—R3, or Rx and Ry are taken together with their intervening atoms to form a fused ring; and R1, R2, R2′, R3, and T are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.

Abstract: Enamine derivatives of formula (1) are described: wherein R1 is a group Ar1 L2Ar2Alk- in which Ar1 is an aromatic or heteroaromatic group, L2 is a covalent bond or a linker atom or group, Ar2 is an arylene or heteroarylene group and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; Cy is a cycloaliphatic or heterocycloaliphatic ring in which X is a N atom or a C(Rw) group; Rx is a oxo, thioxo, or imino group; Rw and Rz is each a hydrogen atom or optional substituent; provided that Cy is not a cyclobutenedione group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.

Abstract: Saccharide-free tablets comprising a salt of quinapril or moexipril and an alkaline compound and further comprising an excipient that stabilizes against hydrolysis and is either water-soluble or absorbs water.

Abstract: Compounds of formula (I) are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.

Abstract: Methods for treating erectile dysfunction using tetrahydroisoquinoline aromatic amines that function as melanocortin receptor ligands.

Abstract: The invention relates to compounds of formula I wherein r is from 0 to 2; n is from 0 to 2; m is from 0 to 4; A, B, D and E are each independently of the others N or CH, with the proviso that not more than two of those radicals are N; G is lower alkylene, —CH2—O—, —CH2—S—, —CH2—NH—, oxa (—O—), thia (—S—) or imino (—NH—), or is lower alkylene substituted by acyloxy or by hydroxy; Q is lower alkyl, especially methyl; R is H or lower alkyl; X is imino, oxa or thia; Y is lower alkyl or, especially, aryl, heteroaryl or unsubstituted or substituted cycloalkyl; and Z is amino, mono- or di-substituted amino, halogen, alkyl, substituted alkyl, hydroxy, etherified or esterified hydroxy, nitro, cyano, carboxy, esterified carboxy, alkanoyl, carbamoyl, N-mono- or N,N-di-substituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, phenyl-lower alkylthio, alkylphenylthio, phenylsulfinyl, phenyl-lowe

Abstract: PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs.

Abstract: The present invention provides an oil preparation comprising a high lipophilic medicament such as a compound of the formula (I): 1

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, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.

Abstract: The invention provides compounds of formula: wherein R1 is —NHS(O)mR, wherein R is alkyl, substituted alkyl, alkoxy, substituted alkoxy, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycle, or substituted heterocycle; X is independently selected from the group consisting of halo, alkyl, substituted alkyl, alkoxy, substituted alkoxy, hydroxy, nitro, amino, and substituted amino; R2 is benzyl or benzyl substituted with one or more substituents selected from the group consisting of halo, CF3, hydroxy, nitro, alkoxy, substituted alkoxy, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycle, substituted heterocycle, amino, and substituted amino of formula —NHR' or —NR′R′, wherein each R′ is alkyl, substituted alkyl, —C(O)Y, —C(O)NHY, or —C(O)SY, wherein Y is alkyl or substituted alkyl; R3 is H or alkyl; n

Abstract: Nitric oxide scavengers, such as dithiocarbamate-containing compounds, are used to reduce side effects caused by therapeutic administration of nitric oxide sources by administering the nitric oxide scavenger(s) to the subject after the therapeutic effect of the nitric oxide source has been achieved. For example, the nitric oxide source can be coadministered with the nitric oxide scavenger, with the latter formulated in a time release vehicle selected to delay release of the scavenger for a period of time sufficient to ensure that the therapeutic goal of the nitric oxide source has been achieved before release of the scavenger. Formulations and kits, including a bubble pack with pairwise arrangement of unit doses of a desired nitric oxide source and nitric oxide scavenger, are also provided.

Abstract: A compound of the following formula or a pharmacologically acceptable salt thereof: 1

Abstract: Disclosed are methods of treating certain cytokine mediated diseases or conditions using novel aromatic heterocyclic compounds of the formula(I) wherein Ar1,Ar2,L,Q and X are described herein.

Abstract: The invention is directed to non-hygroscopic oral pharmaceutical compositions of a salt of valproic acid, and processes for preparing the compositions. The non-hygroscopic pharmaceutical compositions are prepared by blending a hygroscopic salt of valproic acid, carbomer, and a non-hygroscopic additive.

Abstract: There is provided an excellent novel analgesic having an analgesic effect which is effective widely against a pain including a chronic pain or an allodynia accompanied with herpes zoster by acting on a nociceptin receptor.

Abstract: The present invention is directed to ophthalmic compositions containing a gelling amount of a combination of galactomannan polysaccharides and borates. The compositions gel or partially gel upon administration to the eye. The present invention also discloses methods of topical ophthalmic administration of the compositions to the eye.

Abstract: Provided herein are compounds of the formula (I): wherein R1-R8 are as described herein, R4 being aryl or heteroaryl Such compounds are particularly useful in the treatment of a disorder which is created by or is dependent upon decreased availability of serotonin, norepinephrine or dopamine.

Abstract: Treatment of psychotic disorders such as schizophrenia, schizophreniform and schizoaffective disorders comprising co-therapy with an anticonvulsant derivative and a typical antipsychotic.

Abstract: Compounds of the formula (I) are disclosed which are vitronectin receptor antagonists and are useful in the treatment of osteoporosis: or a pharmaceutically acceptable salt thereof.

Abstract: Compositions and uses of mGluR5 antagonists for the treatment and prevention of neurological disorders, such as Fragile X, autism, mental retardation, schizophrenia and Down's Syndrome, are disclosed.

Abstract: A method for preventing or treating gastrointestinal or systemic diseases in a mammalian subject, comprising: the step of administering a therapeutically effective amount of a composition comprising adenosine or a prodrug thereof into the peritoneal cavity of said subject at a dose that does not achieve pharmacologically active levels in the aortic arterial plasma of said subject.

Abstract: Sympathetically maintained pain is treated topically by administering to the site where sympathetically maintained pain is present an &agr;-1-adrenergic antagonist, &agr;-2-adrenergic agonist, or other drug that depletes or blocks synthesis of sympathetic norepinephrine, known collectively as sympatholytic agents. Chemical formulas for several sympatholytic agents are given.

Abstract: Disclosed are novel 1,4-disubstituted benzo-fused compounds wherein G, X, L, Q, n and Y are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.

Abstract: Disclosed is a pharmaceutical composition, comprising a combination of a dose of rofecoxib or a pharmaceutically acceptable salt thereof and a dose of oxcodone or a pharmaceutically acceptable salt thereof, said combination in an amount sufficient to provide an analgesic effect in a human patient. Also disclosed is a method of effectively treating pain in humans or other mammals, comprising administering to the patient a combination of a dose of rofecoxib or a pharmaceutically acceptable salt thereof and a dose of oxycodone or a pharmaceutically acceptable salt thereof such that the dosing interval of the rofecoxib overlaps with the dosing interval of the oxycodone, said combination in an amount sufficient to provide an analgesic effect in a human patient.

Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

Abstract: The present invention provides compounds that elevate cellular expression of the ABCA-1 gene, promoting cholesterol efflux from cells and increasing HDL levels in the plasma of a mammal, in particular humans. The compounds are useful for treating coronary artery disease.

Abstract: A mixture comprising: a) virginiamycin; b) a pharmaceutically acceptable and substantially anhydrous wetting agent including sodium lauryl sulfate; c) a sufficient amount of pharmaceutically acceptable buffering agent to provide a pH of from about 3 0 to about 7.0 when said mixture is added to water; and d) from about 0.5 weight percent to about 10 0 weight percent colloidal silicon dioxide, wherein the ratio of the weight percent of (b) to the weight percent of (a) percent by weight is at least about 1.5:1. The mixture is designed to be added to water to produce a stable suspension of the virginiamycin, which can then be applied to, for example, feed grain.

Abstract: The invention involves the identification of a family of compounds which block calcium channels. The compounds can be formulated in pharmaceutical carriers and administered to subjects. The compounds are useful for treating disorders associated with calcium channel activity, such as, cardiovascular diseases, for example hypertension, congestive heart failure, arrhythmia and angina.

Abstract: Disclosed is a method of increasing the market for an existing pharmaceutical including the step of making a reformulated pharmaceutical by combining the existing pharmaceutical with a nondegradable synthetic polymer not substantially absorbed from the human alimentary canal.

Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds of formula (I) below: are useful in vitro or in vivo for preventing or treating coagulation disorders.

Abstract: Amino pyrazole derivatives of the formula: which are ligands for the neuropeptide Y, subtype 5 receptor and pharmaceutical compositions containing an amino pyrazole derivative as the active ingredient are described. The amino pyrazole derivatives are useful in the treatment of disorders and diseases associated with the NPY receptor subtype Y5.

Abstract: This invention provides a novel class of substituted 6(5H)phenanthridinone compounds. The invention also includes pharmaceutical compositions, and methods of making and using the compounds, or a pharmaceutically acceptable salt, hydrate, prodrug, or mixture thereof. Methods of using the compounds and pharmaceutical compositions for treating neurodegenerative disorders, such as multiple sclerosis are also described.

Abstract: Compounds which are useful as potassium channel inhibitors and which because of their slow off-rates are especially useful for the treatment of cardiac arrhythmias are described.

Abstract: A compound of formula I 1

Abstract: A compound of formula I 1

Abstract: A method of microwave assisted chemical reaction includes providing a microwavable reaction vessel which contains at least one material in a sample. The sample is heated by microwave energy to elevate the temperature of the reagent and at least partially volatilize the sample to establish a gas phase within the vessel followed by positive cooling of the gas phase to reduce the temperature and responsively reduce the pressure of the gas phase without effecting substantial cooling of the liquid phase. The method may involve employing cooling exteriorly of and adjacent to the gas phase containing portion of the vessel or cooling by means of a coolant flowing within coils disposed in the interior of the vessel or both. The process is preferably a continuous process. The apparatus may be a vessel transparent to microwave energy for receiving the sample. The vessel has space overlying the liquid phase containing portion for a gas phase.

Abstract: This invention provides low molecular weight, non-peptide inhibitors of matrix metalloproteinases and TNF-&agr; converting enzyme (TACE, tumor necrosis factor-&agr; converting enzyme) of formula (B) as shown herein or a pharmaceutically acceptable salt thereof.

Abstract: This invention is related to a method whereby scar formation in the drainage fistula and subconjunctival bleb created during and after glaucoma surgery using a prostaglandin subtype A or J.