Abstract: The present invention relates to novel thyroid receptor ligands and, more particularly, relates to malonamic acids and derivatives thereof of Formula I, which are useful in the treatment of obesity, overweight condition, hyperlipidemia, glaucoma, cardiac arrhythmias, skin disorders, thyroid disease, hypothyroidism, thyroid cancer and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, congestive heart failure, hypercholesteremia, depression, osteoporosis and hair loss. The present invention also provides methods, pharmaceutical compositions and kits for treating such diseases and disorders.

Abstract: 1

Abstract: A compound having general formula 1

Abstract: This invention relates to a series of difluoromethylene aromatic ethers of the formula wherein ring A and X and Y are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.

Abstract: Use of phenethylacrylamides of the formula I: in which the substituents have the following meanings: X is halogen, alkyl, haloalkyl, alkoxy, haloalkoxy and —O—C(Ra,Rb)—C≡C—R6; Ra,Rb and Rc have the meanings given in the description; m,n independently of one another are 1 to 4, it being possible for the radicals X or Y to be different if m or n is greater than 1; Y is halogen, nitro, cyano, alkyl, CF3, alkoxy and phenyl; R1,R2 independently of one another are hydrogen, halogen, alkyl, alkoxy, haloalkoxy and CF3; R3,R4,R5,R6 independently of one another are hydrogen, halogen, alkyl, alkoxy, or R3 and R4 together form a cyclopropyl ring, it being possible for the C—R5— and C—R6 bonds can be in the E- or Z-position relative to each other; for controlling phytopathogenic fungal pests, novel phenethylacrylamides, their preparation, and compositions comprising them.

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: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.

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

Abstract: Compounds of Formula (I) are disclosed which are useful as fungicides wherein R1 is hydrogen; halogen; C1-C2 alkoxy; C1-C2 haloalkoxy, cyano; or C1-C2 alkyl optionally substituted with halogen, C1-C2 alkoxy or cyano; R2 is hydrogen; halogen; or C1-C4 alkyl optionally substituted with halogen, C1-C2 alkoxy or cyano; R3 is hydrogen; halogen; C1-C4 alkoxy; C1-C4 haloalkoxy; or C1-C4 alkyl optionally substituted with halogen, C1-C2 alkoxy or cyano; or R2 and R3 can be taken together as —CH2CH2—; R4 is C1-C2 alkyl; R5 is R6, CH(R8)OR6, CH(R8)CH(R7)R6 or C(R8)═C(R7)R6; and R6, R7 and R8 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (I) and a method for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound of Formula (I).

Abstract: The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor.

Abstract: The present invention provides an NF-kappa B activation inhibitor, an inflammatory cytokine production inhibitor, a matrix metalloprotease production inhibitor, an inflammatory cell adhesion factor expression inhibitor, and an anti-inflammatory agent, an antirheumatic agent, an immuno-suppressive agent, an antiallergic agent, an antiviral agent, or a therapeutic agent for arteriosclerosis, which comprise, as the active ingredient, a cyclopropanecarboxylic acid amide compound or a pharmaceutically acceptable salt thereof effective for the treatment of inflammatory diseases.

Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: 1

Abstract: The invention compounds and methods for the treatment of motor disorders. In particular, the invention provides eicosanoid analogs which are effective in ameliorating motor disorders such as spasticity caused by multiple sclerosis (MS).

Abstract: Compounds of formula I 1

Abstract: This invention relates to N-acylamino aryl derivatives of the formula 1

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: Compounds of formula (I) may be used as alignment layers in liquid crystal devices wherein X1-5 are idependently selected from H, F, CN, phenylene, C1-10 alkyl, whereby when X1=X2, then X1,2=H and when X3=X4, then X3,4=H, S1-3 are spacer units, PG1-3 are photoisomerisable/dimerisable groups.

Abstract: Compounds of formula I, in which R1, R2, A, and B having the definitions set forth in the claims, are valuable pharmacologically active compounds, which exhibit a strong antithrombotic effect and are suitable, for example, for treating thromboembolic diseases and restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. Also disclosed are processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Abstract: The present invention relates to a urea derivative of the formula (1) 1

Abstract: Cyanophenoxy carboxylic acid compounds and compositions for the delivery of active agents are provided. Methods of administration, treatment of disease and preparation are provided as well.

Abstract: Provided are processes for the preparation of the compound of the formula 1

Abstract: The present invention relates to compounds and their ability to act as potassium channel openers.

Abstract: The invention relates to the use of phenethyl acrylamides of formula I for controlling phytopathogenic fungi, wherein the substituents of said phenethyl acrylamides have the following significations: X signifies halogen, alkyl, halogenalkyl, alkoxy halogenalkoxy and —O—C(Ra, Rb)—C≡C—R6; Ra, Rb and Rc have the signification given in the description; m, n independently signify 1 to 4, the radicals X or Y being potentially different if m or n is higher than 1; Y signifies halogen, nitro, cyano, alkyl, CF3, alkoxy and phenyl; R1, R2 independently signify hydrogen, halogen, alkyl, alkoxy, halogenalkoxy and CF3; R3, R4, R5, and R6 independently signify hydrogen, alkyl and alkoxy, or R3 and R4 together form a cyclopropyl ring, whereby the C—R5 and C—R6 bonds can be in position E or Z in relation to each other. The invention also relates to novel phenethyl acrylamides, a method for the productio thereof, and agents containing the same.

Abstract: Aromatic methylidene compounds of the following general formula wherein R11 and R21 independently in each occurrence represent an unsubstituted or substituted alkyl or alkoxy group, a halogen, a cyano group or a nitro group, n11 and n21 are, respectively, an integer, R31 and R41 independently represent hydrogen, an unsubstituted or substituted alkyl group, an unsubstituted or substituted cycloalkyl group, an unsubstituted or substituted aromatic group, or an unsubstituted or substituted aromatic heterocyclic group and may join to complete a condensed ring, along with other types of aromatic methylidene compounds wherein the moieties attached to the naphthalene ring are attached to different positions of the ring. The preparation of the methylidene compounds is also described along with intermediate compounds and their preparation.

Abstract: Disclosed are compounds of formula I 1

Abstract: Novel biphenyl derivatives of the general formula (I), in which Y, R R1, R2, R3, R4, m, o and p are as defined in claim 1, and their physiologically acceptable salts and solvates are integrin inhibitors and can be employed for combating thrombosis, cardiac infarction, coronary heart disease, arteriosclerosis, inflammation, tumours, osteoporosis, infections aid restenosis after angioplasty or in pathological processes which are maintained or propagated by angiogenesis.

Abstract: Novel compounds of the formula I, in which R, R1 and R2 are as defined in patent claim 1, are inhibitors of coagulation factor Xa and VIIa and can be employed for the treatment of thromboses, myocardial infarction, arteriosclerosis, inflammation, apoplexis, angina pectoris, restenosis after angioplasty, claudicatio intermittens, tumours, tumour diseases and/or tumour metastases.

Abstract: 3-(4-Cyanophenyl)uracils I 1

Abstract: The present invention provides certain amide, carbamate and urea derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.

Abstract: A compound of formula I 1

Abstract: Substituted arylcycloalkanes, compositions containing them and use thereof. The present invention relates especially to substituted arylcycloalkanes with therapeutic activity, which may be used such as in oncology.

Abstract: The invention concerns a method for preparing &agr;-halogenated ketones from secondary &agr;-halogenated alcohols. More particularly, the invention concerns the preparation of &agr;-trihalogenated ketones from secondary &agr;-trihalogenated alcohols. The method for preparing said &agr;-halogenated ketone is characterized in that it consists in oxidizing in liquid phase, a secondary &agr;-halogenated alcohol, using molecular oxygen or a gas containing same, in the presence of a catalyst based on a metal M1 selected among metals of group 1b and 8 of the periodic system of elements and optionally an activating element.

Abstract: Compounds of the formula 1

Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein A, B; R1, R2, R3, R4 and R5 are as defined in the specification. Such compounds are tyrosine phosphatase inhibitors and useful in the treatment or prevention of Type II Diabetes Mellitus. Also encompassed by the invention are formulations comprising the noted compounds, processes for preparing such compounds, a method for treating or preventing Type II Diabetes Mellitus.

Abstract: Protein tyrosine phosphatases (PTPs) are implicated in a number of disease processes, including autoimmune diseases, glucose intolerance, diabetes, obesity and certain types of proliferative diseases such as cancer and psoriasis. The present invention discloses novel &agr;-ketocarboxylic acid inhibitors of PTPs, methods for synthesizing said inhibitors, and methods for using pharmaceutical compositions of the inhibitors to treat PTP-mediated disorders, diseases or dysfunctions. The compositions described herein can also be used as diagnostic and screening tools to elucidate complex signal transduction pathways involving PTPs or to identify PTP-mediated disease states.

Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.

Abstract: Disclosed are compounds of the formula (I): 1

Abstract: The present invention relates to novel bicyclic cyclopentane-1,3-dione derivatives of the formula (I) to a process for their preparation and to their use as pesticides and herbicides.

Abstract: This invention relates to derivatives of acrylic acid useful as fungicides, to processes for preparing them, to fungicidal compositions containing them, and to methods of combating fungi, especially fungal infections in plants, using them.

Abstract: The invention provides dicarboxylic acid-substituted heteroaryl derivatives of the formula

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

Abstract: The subject invention provides compounds which are easily metabolized by the metobolic drug detoxification systems. Particularly, fluvoxamine analogs which have been designed to include esters within the structure of the compounds are taught. Also provided are methods of treating depression and affective disorders, such as obsessive compulsive disorder. Pharmaceutical compositions of the fluvoxamine analogs are also taught.

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

Abstract: Benzyl carboxylates can be prepared by reacting dibenzyl ethers with carboxylic acids and optionally carboxylic anhydrides in the presence of one or more, preferably one, acids applied to a support as catalyst.

Abstract: This invention relates to a series of difluoromethylene aromatic ethers of the formula 1

Abstract: Styryl benzylsulfones of formula I are useful as antiproliferative agents, including, for example, anticancer agents: 1

Abstract: This invention provides a means for preparing a monohydrate of the lithium salt of cis 4-cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]cyclohexanecarboxylate which is a novel composition of matter.

Abstract: This invention relates to the novel use of dianilino squarates in the treatment of disease states mediated by the chemokine, Interteukin-8 (IL-8).

Abstract: The present application relates to novel potent PPAR-alpha-activating compounds for treating, for example, coronary heart disease, and to their preparation.

Abstract: A ferulic acid derivative represented by the general formula: wherein R denotes a polyethylene glycol group, a crown ether group, or a azacrown ether group.