Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R1, R2, R3, R4, R5, R6, R8, R9 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 invention provides novel &bgr;2 adrenergic receptor agonist compounds of formula (I): 1

Abstract: This invention relates to a controlled or sustained release formulation designed to deliver a PDE4 inhibitor for treating an inflammatory disease such as asthma or COPD and the like.

Abstract: This invention relates generally to amino-thio-acrylonitriles of formula Ia or Ib: as MEK inhibitors, pharmaceutical compositions containing the same, and methods of using the same as for treatment and prevention of inflammatory disorders or as an anticancer radiosensitizing agent.

Abstract: A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of formula I: 1

Abstract: The invention relates to substituted 1 and 2 naphthol Mannich bases, a method for the production thereof, medicaments containing said compounds and the use of said compounds in the production of medicaments.

Abstract: Disclosed are novel urea derivatives and their medical uses, especially as adhesion molecule inhibitors useful for therapies of inflammatory diseases.

Abstract: N-terminal substituted dipeptide nitrites as defined are useful as inhibitors of cysteine cathepsins, e.g. cathepsins B, K, L and S, and can be used for the treatment of cysteine cathepsin dependent diseases and conditions, including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis, tumors (especially tumor invasion and tumor metastasis), coronary disease, atherosclerosis (including atherosclerotic plaque rupture and destabilization).

Abstract: A pharmaceutical composition comprising an effective amount of a compound of formula I 1

Abstract: A compound of Formula (IA) or Formula (IB) 1

Abstract: A sustained-release pharmaceutical preparation is disclosed in which a calcium channel blocker, preferably verapamil, core is surrounded by an optional seal coat layer and a water-insoluble coating.

Abstract: The present invention relates to a method of treating depression or anxiety in a mammal, including a human, by administering to the mammal a CNS-penetrant NK-1 receptor antagonist (e.g., a substance P receptor antagonist) in combination with a PDE IV inhibitor. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a CNS-penetrant NK-1 receptor antagonist and a PDE IV inhibitor.

Abstract: Arylsulfonamidobenzyl alcohols, amines and sulfonamides are provided which are useful in treating lipid disorders, metabolic diseases and cell-proliferative diseases.

Abstract: The invention relates to the use of LTB4 antagonists for preparing a pharmaceutical composition for the treatment or prevention of respiratory diseases in companion and domesticated animals.

Abstract: Aminotetralin derivatives and pharmacological analogs thereof which contain an N-propynyl group exhibit differential dopaminergenic receptor activity. The subject compounds are useful in affecting dopamine receptor activity, particularly in exhibiting differing activity among the various dopamine receptor subtypes. The compounds are useful in treating CNS disorders in mammals in general, and humans in particular.

Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any glucagon-mediated conditions and diseases such as hyperglycemia, Type 1 diabetes, Type 2 diabetes and obesity.

Abstract: Disclosed herein is a oral extended release dosage form comprising a plurality of granules of an effective amount of a pharmaceutically active compound, at least one amino acid, and an intragranular polymer in which the granule is dispersed within a hydrophilic extragranular polymer matrix which is more rapidly hydrating than the intragranular polymer. The amino acid is selected for hydropathy characteristics depending on solubility characteristics of the active compound.

Abstract: Compounds of formula (Ia) as potent, &bgr;1-specific beta blockers with a short duration of action in the systemic circulation, wherein R is 3′,4′-dimethoxyphenyl, R1 is hydrogen, and R2 is selected from methyl, ethyl, propyl, isobutyl and isopropyl; or R is 3′,4′-dimethoxyphenyl, R1 is selected from fluorine, chlorine and bromine, and R2 is selected from methyl, ethyl, propyl, isopropyl, isobutyl and cyclopropylmethyl; of R is 4′-methoxyphenoxy, R1 is selected from hydrogen, fluorine, chlorine and bromine, and R2 is selected from methyl, ethyl, propyl, isopropyl, isobutyl and cyclopropylmethyl; or R is 3′,4′-dimethoxyphenyl, R1 is cyano, and R2 is cyclopropylmethyl; or R is 4′-methoxyphenoxy, R1 is cyano, and R2 is isobutyl; and physiologically acceptable hydrolysable derivatives thereof having the hydroxy group in the 2-position of the 3-aminopropoxy side chain in esterified form, in their racemic and optically active forms, and their pharmaceutically acceptab

Abstract: A dosage form is disclosed comprising means for delaying the delivery of drug from the dosage form following the administration of the dosage form to a patient in need of drug therapy.

Abstract: This invention relates to a 24 hour extended release dosage formulation and unit dosage form thereof of venlafaxine hydrochloride, an antidepressant, which provides better control of blood plasma levels than conventional tablet formulations which must be administered two or more times a day and further provides a lower incidence of nausea and vomiting than the conventional tablets. More particularly, the invention comprises an extended release formulation of venlafaxine hydrochloride comprising a therapeutically effective amount of venlafaxine hydrochloride in spheroids comprised of venlafaxine hydrochloride, microcrystalline cellulose and, optionally, hydroxypropylmethylcellulose coated with a mixture of ethyl cellulose and hydroxypropylmethylcellulose.

Abstract: The use of compounds of formula (1) is described, in which compounds R1, R2 and R3 are each independently of the others hydrogen; C1-C20alkyl; C3-C7cycloalkyl; C2-C20alkenyl; C4-C7cycloalkenyl; C2-C20alkynyl, C4-C7cycloalkynyl; or unsubstituted or C1-C5alkyl-, C3-C7cylcoalkyl-, C1-C5alkoxyl-, C3-C7cycloakoxy-, halo-, oxo-, carboxy-, carboxy-C1-C7alkyl ester-, carboxy-C3-C7cylcloalkyl ester-, cyano-, trifluoromethyl-, pentafluoroethyl-, amino-, N,N-mono- or di-C1-C20alkylamino- or nitro-substituted phenyl-C1-C5alkyl, naphthyl-C1-C5alkyl, phenylcarbonyl-C1-C5alkyl, naphthylcarbonyl-C1-C5alkyl, pyrrolylalkyl, furanylalkyl, thiophenylalkyl, pyrazolylalkyl, imidazolylalkyl, oxazolylalkyl, thiazolylalkyl, isoxazolylalkyl, isothiazolylalkyl, 1,2,3-triazolylalkyl, 1,2,4-triazolylalkyl, 1,2,3-oxadiazolylalkyl, 1,3,4-oxadiazolylalkyl, 1,2,3-thiadiazolylalkyl, 1,3,4-thiadiazolylalkyl, indolylalkyl, pyridylalkyl, pyridazinylalkyl, pyrimidinylalkyl, pyridazinylalkyl, quinolinylalkyl, isoquinolinylalkyl, pyrrolyl, furanyl,

Abstract: The present invention provides a low-irritant pesticidal emulsifiable concentrate comprising (a) 1 to 60% by weight of at least one pesticidal active ingredient compound selected from the group consisting of pyriproxyfen and a pyrethroid compound, (b) 2 to 15% by weight of at least one surfactant and (c) 15 to 90% by weight of at least one aromatic ester solvent represented by the formula: Ar—X—COOR  [1] or the formula: RCOO—X—Ar  [2] [wherein R represents non-aromatic group having 1 to 6 carbon atoms; Ar represents an aromatic group; and X represents a single bond or an alkylene group having 1 to 6 carbon atoms]. The pesticidal emulsifiable concentrate of the present invention can be used as an emulsion which is superior in emulsion stability when using after diluting with water, and has low irritation.

Abstract: Compounds of the class of 4-oxo-butenoic acid derivatives are disclosed along with the surprising use property of these compounds as a anti-tumor agents in humans against breast carcinoma, which include: 2-(N′-Fluoren-9-ylidene-hydrazino)-5,5-dimethyl-4-oxo-hex-2-enoic acid methyl ester (0F-06), 1-(2,4-Dimethyl-phenyl)-2,4-dihydroxy-3-(4-methyl-benzoyl)-5-oxo-2,5-dihydro-1H-pyrrole-2-carboxylic acid methyl ester (1F-07), 4-(4-Methoxy-phenyl)-2,4-dioxo-3-(phenyl-hydrazono)-butyric acid (3F-10), 4-(4-Chloro-phenyl)-2,4-dioxo-3-(phenyl-hydrazono)-butyric acid ethyl ester (3F-11), 2-Hydroxy-4-oxo-4-(2,3,5,6-tetrafluoro-4-methoxy-phenyl)-but-2-enoic acid (3F-15), and 4,4-Dihydroxy-5-(4-methyl-benzoyl)-2-phenyl-2,4-dihydro-pyrazol-3-one (3F-16) as well as some novel derivatives of these compounds claimed (see Table 2).

Abstract: The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a hedgehog agonist, such as the compounds depicted in FIGS. 32 and 33. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal ptc pathway or agonizing smoothened or hedgehog activity.

Abstract: Pharmaceutical compositions comprising the active (R,R′),(R,S′) form of amphetaminil substantially free of (S,R′),(S,S′)-amphetaminil are described for the treatment of humans.

Abstract: This invention encompasses anthranilamides with heteroarylsulfonyl side chain, process for their preparation, their use as medicament or diagnostic aid, and pharmaceutical preparations containing them.

Abstract: Novel styrylacrylonitrile compounds which are useful in treating a variety of cell proliferative disorders such as cancer are disclosed.

Abstract: Pharmaceutical compositions comprising the active (S,R′),(S,S′) form of amphetaminil substantially free of (R,R′),(R,S′)-amphetaminil are described for the treatment of humans.

Abstract: Disclosed are novel succinate derivative compounds of the formula (I)/(Ia): 1

Abstract: The invention relates to a transdermal therapeutic system (TTS) containing desoxypeganine (1,2,3,9-Tetrahydropyrrolo[2,1-b]quinazoline) as the active component, wherein the TSS includes a back layer impermeable to desoxypeganine and an adhesive reservoir layer that contains 10-80 weight percent polymeric material, 0.1-30 weight percent desoxypeganine and/or the pharmaceutically acceptable salts thereof and optionally a softening agent in proportions of 0.1-30 weight percent.

Abstract: A compound of the formula I: wherein A and C are independently H, alkyl of 1-6 carbon atoms, hydroxy, or alkoxy of 1-6 carbon atoms; B is hydroxy, alkoxy of 1-6 carbon atoms —CO2Z, —O(CH2)mCO2Z, —SO3Z, —OPO3Z2; and Y is cyano,   —C(NR1R2)═C(CN)2; wherein X═O or S, and R1 and R2 are independently H, benzyl, —CH(CH3)C6H6, —(CH2)n C6H6, phenyl; —CO2R; n=2-4; R is lower alkyl of 1-6 carbon atoms; m=1-4 and Z is H, a cation or lower alkyl of 1-6 cabon atoms; is used for treating inflammation, immunological diseases or diabetes.

Abstract: Disclosed is a method of treating an individual or animal with osteoarthritis. The method comprises administering to the individual or animal a therapeutically effective amount of a protein tyrosine kinase inhibitor.

Abstract: A substituted aminomethyl-phenyl-cyclohexane derivative of formula I or Ia, 1

Abstract: The invention relates to the use of compounds of formula (I), wherein n=0-3; R1, R2=H, alkyl, aryl, heteroaryl, acyl; R3=H, halogen, alkyl, aryl, heteroaryl, arylalkyl, acyl, CN, NO2, R4—X—; R4=H, alkyl, aryl, heteroaryl, aralkyl, acyl; X=NH, O, S, SO2, NHSO2, OSO2, and A, B, C=organic groups. The inventive compounds are used for the prophylaxis and the therapeutic treatment of infectious processes, especially of infectious processes caused by parasites. The invention further relates to medicaments that contain the inventive compounds.

Abstract: The present invention is directed to nitrosated or nitrosylated &agr;-adrenergic receptor antagonists, compositions comprising &agr;-adrenergic receptor antagonists that are optionally substituted with at least one NO or NO2 moiety and compounds that donate, transfer or release nitric oxide or elevate levels of endogenous endothelium-derived relaxing factor, and methods for treating sexual dysfunctions in males and females.

Abstract: Phenylacetic acid derivatives of the formula I where the variables are as disclosed herein, their salts, processes and intermediates for their preparation, and their use for controlling harmful fungi and animal pests.

Abstract: Elevated glutamate levels are associated with glaucoma, and damage to retinal ganglion cells can be controlled by administering to the patient a compound capable of reducing glutamate induced excitotoxicity in a concentration effective to cause reduction of such excitotoxicity.

Abstract: This invention relates to certain benzenesulfonamides and their use as PDE7 inhibitors

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

Abstract: The present invention relates to ion channel modulating agents. More particularly, the present invention relates to a particular class of oxime derivatives represented by general formula (I) that has proven useful as modulators of SKCa, IKCa and BKCa channels. In further aspects, the present invention relates to the use of these SK/IK/BK channel modulating agents for the manufacture of medicaments, and pharmaceutical compositions comprising the SK/IK/BK channel modulating agents. The SK/IK/BK channel modulating agents of the invention are useful for the treatment or alleviation of diseases and conditions associated with the SK/IK/BK channels.

Abstract: The invention relates to a device and method for the treatment of Alzheimer's dementia with desoxypeganine and/or a pharmaceutically acceptable acid addition salt of desoxypeganine.

Abstract: The present invention provides novel indane-like compounds which can be useful for treating psychosis and other conditions associated with the modulation of a muscarinic receptor. The invention provides formulations and methods for using the novel compounds.

Abstract: Compounds useful for countering undesired toxic effects to cells, tissues or organs having formula (I) wherein: Ar is a group of formulae (i) or (ii), n is 0 or, when Ar has formula (i) above, then n may also be 1, R is CN, —GC(S)NH2, —C(O)NHR3 or, when R1 is 4-NO2 add R2 is H or 3-OH, then R may also be a group of formulae (iii), (iv), (v), (vi) where R3 is H, phenyl, phenyl(lower alkyl) or pyridylmethyl; R1 and R2 are each independently H, OH, NO2 or, when R is CN, also CH3, F, or CF3, provided that both R1 and R2 are not simultaneously H.

Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds.

Abstract: Excessive brain neuronal excitability, associated with a seizure disorder, can be correlated with increased mitogen-activated protein kinase (MAPK) activity in neurons. Such excessive excitability can be ameliorated by administering an effective amount of a compound, such as a MAPK phosphorylation or kinase activity inhibitor, that reduces the amount of MAPK activity in neurons of an individual suffering from a seizure disorder. Compounds that inhibit phosphorylation or kinase activity of upstream activators or downstream targets of the MAPK cascade also are useful in this context.

Abstract: Compounds, compositions and methods are disclosed for treating mitochondria-associated diseases, such as cancer, psoriasis, stroke, Alzheimer's Disease and diabetes. The compounds of this invention have structure (I) below, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein Ar and L are as defined herein. The methods of this invention are directed to treating a mitochondria-associated disease by administering to a warm-blooded animal in need thereof an effective amount of a compound of structure (I), typically in the form of a pharmaceutical composition.

Abstract: The invention relates to a pharmaceutical composition containing an inhibitor for diaphragm pumps and a photoaffinity-marked chemotherapeutic agent. Said composition is suitable for eliminating membrane-mediated cell resistance, especially membrane-mediated multi-chemoresistance of tumor cells.

Abstract: Described are substituted cyanoenamines of formula I wherein Z, R1, R2 and R3 are defined in the description, compositions thereof and methods for preparing these compounds. These compounds are useful in the treatment of diseases of the central nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinologic system.

Abstract: Described are substituted cyanoenamines of formula I wherein Z, R1, R2 and R3 are defined in the description, compositions thereof and methods for preparing these compounds. These compounds are useful in the treatment of diseases of the central nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinologic system.

Abstract: The invention is of a novel, noninvasive method for treating hemangiomas involving the topical application of one or more calcium channel blocker agents suspended in one or more carriers with penetration enhancing agent's to effect transdermal delivery of the calcium channel blocker agent(s). Periodic, topical application of the medicaments taught here in will effect, usually within a few months, and involution of treated hemangiomas with minimized residual cosmetic blemishes after involution.