Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Abstract: Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardivascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardivascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardivascular and/or sedatory activity.

Abstract: The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I The present invention also provides methods for the use thereof to inhibit ?-secretase (BACE) and treat ?-amyloid deposits and neurofibrillary tangles.

Abstract: Certain novel phenyl substituted cyclic urea derivatives have unexpected insecticidal activity. These compounds are represented by formula I: where A, B a, D, b, E, G, c, d, J, X and R through R10, inclusively, are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.

Abstract: A compound of general formula (I) wherein R and R1 are as defined herein, or a tautomer, diastereomer, enantiomer, or salt thereof, particularly the physiologically acceptable salts thereof, which have valuable pharmacological properties, particularly CGRP-antagonistic properties, pharmaceutical compositions containing the compound, their use, and processes for preparing them.

Abstract: The invention encompasses ureido substituted benzoic acid compounds, compositions comprising the compounds and methods for treating or preventing diseases associated with nonsense mutations of mRNA by administering these compounds or compositions.

Abstract: Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardivascular and/or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.

Abstract: A compound is disclosed herein comprising or a pharmaceutically acceptable salt or a prodrug thereof; wherein R is OH or NH2. Methods, compositions, and medicaments related thereto are also disclosed.

Abstract: The present invention provides methods of reducing angiogenesis in an individual. The methods generally involve administering to the individual an effective amount of a nicotinic acetyl choline receptor antagonist. The methods are useful to treat conditions associated with or resulting from angiogenesis, particularly pathological angiogenesis. The invention further provides methods of treating a condition associated with or resulting from angiogenesis.

Abstract: The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache.

Abstract: Compositions are provided for lightening skin and toning down pigment disorders which include, as active substances, at least one of the compounds of the general formula (I) and/or salts thereof in which R1 is H, alkyl, hydroxyalkyl, or a carboxyalkyl radical having 2 to 30 carbon atoms; and R2 is H or a hydrocarbon radical having 1 to 30 carbon atoms which may be branched or unbranched and may or may not contain double bonds.

Abstract: This invention relates generally to pharmaceutical compositions for treating seizures, and, more particularly, to pharmaceutical compositions that are bioadherent to oral and/or nasal mucosa, comprise one or more anti-acute seizure agents, and can be used to treat one or more conditions selected from the group consisting of acute seizure, repetitive seizures, and status epilepticus. This invention also relates generally to methods for preparing such compositions, methods of treatment using such compositions, uses of such compositions to prepare medicaments, and kits comprising such compositions.

Abstract: The present invention is directed to the use of lipoxin A4 analogs as therapeutic agents in the treatment and/or prevention of intestinal fibrosis.

Abstract: A compound of the formula or a pharmaceutically acceptable salt thereof, is disclosed herein. Methods and compositions related thereto are also disclosed.

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 thereof, 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

Abstract: Membrane permeable prodrugs of creatine analogs, pharmaceutical compositions comprising membrane permeable prodrugs of creatine analogs, and methods of treating diseases such as ischemia, heart failure, and neurodegenerative disorders comprising administering prodrugs of creatine analogs or pharmaceutical compositions thereof are disclosed.

Abstract: A 2-iminoimidazole derivative represented by the formula: {wherein R1, R2 and R3 represent hydrogen, optionally substituted C1-6 alkyl, etc.; R6 represents hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, etc.; Y1 represents a single bond, —CH2—, etc.; Y2 represents a single bond, —CO—, etc.; and Ar represents hydrogen, a group represented by the formula: [wherein R10–R14 represent hydrogen, C1-6 alkyl, hydroxyl, C1-6 alkoxy, etc., and R11 and R12 or R12 and R13 may bond together to form a 5- to 8-membered heterocycle], etc.}or salt thereof.

Abstract: The present invention is directed to compounds that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

Abstract: The present invention relates to certain resorcinol derivatives and their use as skin lightening agents.

Abstract: The present invention provides a 10,11-dihydrospiro[dibenzo[a,d][7]annulene-5,4?-imidazol]-5?(1?H)-one compound of formula I Also provided are methods and compositions for the inhibition of ?-secretase (BACE) and the treatment of ?-amyloid deposits and neurofibrillary tangles.

Abstract: This invention discloses and claims diary heterocycles of formula (I) and their pharmaceutically acceptable salts, pharmaceutical compositions thereof, and methods of using said compounds of formula (I) for the treatment or prevention of excessive weight or obesity, and for treatment of Type II diabetes, arteriosclerosis, high blood pressure, depression, anxiety, anxiety neuroses, and schizophrenia. Methods for treatment of excessive weight or obesity and for treatment of Type II diabetes with a mixture of a compound of formula I and antiobesity agents or appetite-regulating active ingredients, or with a mixture of a compound of formula I and antidiabetics or hypoglycemic active ingredients are also disclosed and claimed.

Abstract: Compounds of formula I: where R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkylaryl, alkyloxy, hydroxy, nitro, amino, alkylcarbonylamino, alkylamino or dialkylamino group; R4 signifies hydrogen, alkyl or alkylaryl group; X is CH2, O or S, and n is 1, 2 or 3, with the proviso that if X is CH2, n is not 1, and a method for their preparation. The compounds have potentially valuable pharmaceutical properties for the treatment of cardiovascular disorders such as hypertension and chronic heart failure.

Abstract: The present inventions relates to a novel compound of formula (I) or a pharmaceutically acceptable salt thereof, the use and manufacture of a compound of formula (I) or a pharmaceutical composition comprising a compound of formula (I).

Abstract: The invention relates to novel imidazolamino compounds. Also disclosed are methods of treating cancer by using one of these compounds and pharmaceutical compositions containing one of these compounds.

Abstract: This invention provides methods for treating in mammals arthritic or rheumatic disorders using substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof, and methods for using the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition of pain and inflammation.

Abstract: Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardivascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardivascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardivascular and/or sedatory activity.

Abstract: An N-aminoimidazole or N-aminoimidazolethione derivative, a pharmaceutically acceptable salt, a tautomer, an isomer, an ester or glycosylation product thereof, said derivative being represented by general formula (I): wherein m=zero or 1, n=zero or 1, R1 is selected from hydrogen, methyl or ethyl, R2 is selected from hydrogen, SH or —SR0 wherein R0 is methyl, benzyl or glucose residue; Q is selected from 1-naphtyl, 2-naphtyl, biphenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl, or a substituted or unsubstituted phenyl ring, wherein the substitution is understood as being one or two substituents selected from H, F, Cl, Br, I, methyl, ethyl or isopropyl; L is selected from 1-naphtyl, 2-naphtyl, biphenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidyl, 4-pyrimidyl, 5-pyrimidyl, thienyl, or a substituted or unsubstituted phenyl ring wherein the substitution is understood as being one or two substituents selected from H, F, Cl, Br, I, methyl, ethyl or isopropyl.

Abstract: The present invention provides methods of reducing angiogenesis in an individual. The methods generally involve administering to the individual an effective amount of a nicotinic acetyl choline receptor antagonist. The methods are useful to treat conditions associated with or resulting from angiogenesis, particularly pathological angiogenesis. The invention further provides methods of treating a condition associated with or resulting from angiogenesis.

Abstract: The present invention is directed to novel themisone derivative compounds that have been modified to prevent the formation of the toxic metabolite, 2-phenyl-acrylamide. Compositions comprising such derivative compounds have activity as anesthetics and as neuroprotective agents.

Abstract: The present invention relates to the use of polysiloxanes containing at least one quaternary ammonium group as formulation auxiliaries in formulations of pharmaceutically and veterinary active compounds, and to compositions comprising a) pharmaceutically or veterinary active compound and b) a polysiloxane derivative containing at least one quaternary ammonium group per molecule, if appropriate, further auxiliaries and carriers.

Abstract: This invention is directed to a class of compounds (Formula I) including succinoyl amino pyrazoles, succinoyl amino thiadiazoles, succinoyl amino acid esters, succinoyl amino acid amides, succinoyl amino alcohols, succinoyl amino ketones, succinoyl amino hydantoins, succinoyl anilines, and succinoyl derivatives of privileged structures. The invention is also directed to a pharmaceutical formation comprising such compound in a pharmaceutically acceptable salt form or prodrug thereof. The invention is further directed to a method for inhibiting ?-amyloid peptide release and/or synthesis, a method for inhibiting ?-secretase activity and a method for treating neurological disorders associated with ?-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.

Abstract: The invention is directed to novel benzimidazolone peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis, hypertension, heart failure, arrhythmia, inflammation, angina, stroke, atherosclerosis, ischemic conditions, Angiogenesis related disorders, cancer, and neurodegenerative disorders. Pharmaceutical compositions comprising the substituted benzimidazolone peptidomimetics of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.

Abstract: The present invention relates to novel trifluorobutenyl imidazole thioether derivatives of the following formula (I) wherein R1 represents hydrogen or halogen, R2 represents hydrogen, halogen or alkoxycarbonyl, R3 represents hydrogen, alkyl, alkenyl, cycloalkyl or aralkyl, and n represents 0,1 or 2, with the proviso that R1, R2 and R3 do not all represent hydrogen at the same time, to a process for their preparation and to their use as nematicides.

Abstract: The present invention relates to a method of amelioring oxidative stress and stress-related degenerative processes associated with aging or various disease conditions such as cancer, neurodegenerative diseases or the dysregulation of redox-regulated physiological processes, as indicated by the prooxidative shift in the plasma thil/disulfide redox state and its consequences in conditions of elevated oxidative stress, characterized by administering creatine.

Abstract: The present invention provides a compound and a method of making a compound according to the following formula: where R1 is an alkyl group having 1 to 12 carbons; R2 is a urea group; R3 is an active group, such as fluorescein, a toxin, radiolabel or drug; and R4, R5 and R6 are each independently a halide group.

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 concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, 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; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R6 is hydrogen or phenylmethyl; 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 bivalent radical.

Abstract: A medicament for inhibiting sodium/calcium exchange system which comprises as an active ingredient a substance selected from the group consisting of an aminobenzenesulfonic acid derivative represented by the following general formula (I) and a salt thereof, and a hydrate thereof and a solvate thereof: 1

Abstract: This invention is directed to lipoxin A4 analogs of the following formula (I) and (II): wherein R1, R2, R3, R4 and R5 are described herein. These analogs are useful in treating inflammatory and autoimmune disorders in humans. These analogs are also useful in treating pulmonary or respiratory tract inflammation in humans.

Abstract: This invention provides substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof, and methods for using the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition of pain and inflammation.

Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

Abstract: The present invention relates to the use of creatine compounds including creatine, creatine phosphate or analogs of creatine, such as cyclocreatine, for treating diseases of the nervous system. Creatine compounds can be used as therapeutically effective agents against a variety of diseases of the nervous system such as diabetic and toxic neuropathies, peripheral nervous system diseases, Alzheimer disease, Parkinson's disease, stroke, Huntington's disease, amyotropic lateral sclerosis, motor neuron disease, traumatic nerve injury, multiple sclerosis, dysmyelination and demyelination disorders, and mitochondrial diseases.

Abstract: A method for treating inflammatory and immune cell-mediated diseases by the administration of compounds of the formula I Exemplary are:

Abstract: The present invention relates to novel sulfoxide and bis-sulfoxide compounds, compositions comprising sulfoxide and bis-sulfoxide compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

Abstract: The present invention provides a method for the long-term relief of chronic pain in a subject by activating in the subject an analgesic &agr;-adrenergic receptor in the absence of &agr;-2A receptor activation over a period of at least three days, such that relief of chronic pain is maintained in the absence of continued activation of said receptor. The analgesic &agr;-adrenergic receptor can be, for example, the &agr;-2B receptor.

Abstract: The present invention is directed to a method for reducing the emetogenic effects of PDE inhibitors, and more particularly is directed to compounds having PDE4 inhibition activity with little or no emetogenic side-effects, and chemical methods including benzylation for preparing such compounds. A benzyl group may be attached to either a carbon or nitrogen atom of a PDE4 inhibitor. Suitable benzylation chemistry is to extract a hydrogen from a PDE4 inhibitor, preferably with a base, and then react the resulting nucleophilic PDE4 inhibitor with a benzylating agent, e.g., benzyl bromide or a derivative thereof.

Abstract: A composition for treatment of biological tissue responsive to a an applied magnetic field comprises a plurality of magnetoliposomes, each magnetoliposome of the plurality having a lipid-containing wall defining a vesicle, and a plurality of subdomain superparamagnetic particles, and an inactive prodrug capable of activating into a drug effective for treatment of the biological tissue, the prodrug carried by the plurality of magnetoliposomes for delivery to the biological tissue.

Abstract: A method of inhibiting the formation of oxygen-containing free radicals and derivatives of them during and following exercise is disclosed. It includes administering an amount of a supplement containing one or more compounds selected from the group consisting of pentose carbohydrates and derivatives thereof in conjunction with said exercise. The supplement is administered as a dose at one or more times selected from prior to, during and after exercise.

Abstract: Compounds, compositions and methods for modulating the activity of nuclear receptors are provided. In particular, heterocyclic compounds are provided for modulating the activity of farnesoid X receptor (FXR), liver X receptor (LXR) and/or orphan nuclear receptors. In certain embodiments, the compounds are thiazolidinone derivatives.

Abstract: A skin moisturizing composition comprising water, a skin moisturizer, a water soluble hydroxyalkylcellulose polymer and additives is free of fats and oils. The composition derives substantial water-barrier properties from the water soluble hydroxyalkylcellulose polymer.