Abstract: This invention relates to hydroxy-tetrahydro-naphthalenylurea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The hydroxy-tetrahydro-naphthalenylurea derivatives of the present invention have an excellent activity as VR1 antagonist and are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.

Abstract: Compounds of formula (I) wherein R1, R3, R4, R5, R6, R7, and R10 are as defined in the specification, are described. The present invention also relates to pharmaceutical composition comprising said compounds and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of said compounds and to new intermediates useful in the preparation thereof. Beside, the invention relates to salts and polymorphic forms of the new compounds as well as the preparation thereof.

Abstract: The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes.

Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.

Abstract: The invention relates to compounds of formula (I), wherein R, R1, R2, X and n are as defined in the description, and their use for the preparation of pharmaceutical compositions for the treatment of inflammatory states.

Abstract: This invention relates to bicyclic amide, carbamate or urea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The bicyclic amide, carbamate or urea derivative of the present invention has vanilloid receptor (VR1) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urological diseases or disorders, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor oeractivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, and inflammatory disorders such as asthma and chronic obstructive pulmonary (or airways) disease (COPD).

Abstract: The present invention describes compounds comprising new and useful peptides and peptidomimetics that can bind to CD23. They are capable of reducing inflammatory responses associated with auto-immune diseases, chronic inflammatory diseases, allergies and other inflammatory conditions such as those mediated by the mammalian immune system. Compounds of the present invention relate to a CD23-binding peptide wherein said peptide comprises an amino-acid sequence of X1,-X2- X3-X4-X5-X6-X7-X8, wherein: X1 is Phe, or is absent; X2 is His or Ala; X3 is Glu, Ser, Ala, Asn, Lys, or Cys; X4 is Asn, Phe, Gln, Pro, Ser, or Ala; X5 is Trp; X6 is Pro, Arg, Glu, Gly, Cys, or Lys; X7 is Ser, Pro, Leu, Thr Ala, Gly, Asn, or absent; and X8 is Phe, Gly, or is absent.

Abstract: The present application describes modulators of chemokine receptors of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.

Abstract: One aspect of the present invention relates to novel peptidomimetic compounds. A second aspect of the present invention relates to the use of the novel peptidomimetic compounds as ligands—agonists or antagonists—for various cellular receptors, e.g., G-protein-coupled receptors and opioid receptors, and various cellular ion channels, e.g., sodium and calcium. In certain embodiments, compounds of the present invention preferentially or selectively inhibit sodium or calcium ion channels. In certain embodiments, compounds of the present invention preferentially or selectively agonize or antagonize $gm opioid receptors.

Abstract: The present invention relates to a urea derivative of the formula (1) wherein each symbol is as described in the specification, a pharmaceutically acceptable salt thereof and pharmaceutical use thereof. The compound of the present invention has a C5a receptor antagonistic action and is useful as an agent for the prophylaxis or treatment of diseases or syndromes due to inflammation caused by C5a [e.g., autoimmune diseases such as rheumatism, systemic lupus erythematosus and the like, sepsis, adult respiratory distress syndrome, chronic obstructive pulmonary disease, allergic diseases such as asthma and the like, atherosclerosis, cardiac infarction, brain infarction, psoriasis, Alzheimer's disease and serious organ injury (e.g., pneumonia, nephritis, hepatitis, pancreatitis and the like) due to activation of leukocytes caused by ischemia, trauma, burn, surgical invasion and the like].

Abstract: The present invention provides N-aryloxypropanolyl-N?-phenethyl-urea derivatives of formula 3, method for their preparation and use thereof as potent appetite suppressants for treatment of obesity wherein R is selected from the group consisting of H, 2, 3 or 4-trifluoromethyl, 2, 3, or 4-chloro, 2, 3, or 4-bromo, 4-acetyl, 4-propionyl, 4-acetamido, 2,3 or 4 methoxy, 4 nitrile, 2,3 or 4-methyl, and 4 formyl and X is S or O.

Abstract: The present invention relates to methods for elevating high density lipoprotein (HDL) plasma levels, decreasing the absorption of dietary cholesterol in the intestine, decreasing the plasma level of low density lipoprotein (LDL), and increasing the conversion of cholesterol to bile acids, utilizing LXR? selective agonists, usually without elevating the plasma levels of triglycerides. Also provided are methods of using such agonists to treat metabolic diseases alone or in combination with other active agents. Also provided are methods for decreasing hyperglycemia and insulin resistance methods for treating type II diabetes, and methods for treating type II diabetes and reducing the cardiovascular complications of type II diabetes, utilizing an LXR agonist. Further provided are methods for treating obesity and methods for treating the complications of obesity including type II diabetes, cardiovascular disease, hyperlipidemia, and hypertension, administering an LXR?-selective antagonist.

Abstract: Compounds of Formula I and the pharmaceutically acceptable salts and esters thereof, wherein Z is selected from the group consisting of: (a) Formula Ia ?and (b) Formula Ib are novel LXR agonists and are useful in the treatment of dyslipidemic conditions particularly depressed levels of HDL cholesterol.

Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of inflammatory diseases such as asthma and other allergic diseases.

Abstract: Compounds of the formulae 1 2

Abstract: Compounds of general formula I are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.

Abstract: Disclosed are novel processes and novel intermediate compounds for preparing aryl- and heteroaryl-substituted urea compounds of the formula(I) wherein Ar1, Ar2, L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.

Abstract: The invention relates to compounds of formula (I), and also to salts thereof, which have fungicidal activities: in which the various radicals and substituents are as defined in the description, and also to the fungicidal compositions containing them and to methods for combating the phytopathogenic fungi of crops using these compounds and compositions.

Abstract: Phenoxyethylamine derivatives of general formula (I) having high affinity for the 5-HT1A receptor, methods for preparing same, pharmaceutical compositions containing said derivatives, and their use, in particular as gastric acid secretion inhibitors or as antiemetics, are disclosed. In general formula (I), Ar is phenyl substituted by one or more substituents; and R is a C1-10 hydrocarbon radical selected from straight or branched alkyl, alkenyl or alkynyl radicals, saturated or unsaturated mono- or polycyclic cycloalkyl, cycloalkylalkyl or alkylcycloalkyl radicals; a pyridyl or isoquinolyl radical, phenyl optionally substituted by one or more substituents, and salts thereof.

Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of inflammatory diseases such as asthma and other allergic diseases.

Abstract: Disclosed are novel processes and novel intermediate compounds for preparing aryl- and heteroaryl-substituted urea compounds of the formula (I) wherein Ar1, Ar2, L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.

Abstract: Peptoid compounds of Formula I and Formula II are disclosed The compounds are useful in the treatment of matrix metalloproteinase-mediated disorders.

Abstract: Compounds of formula I are useful for treating conditions associated with hyperglycemia, especially Type II diabetes. These compounds are useful in stimulating the kinase activity of the insulin receptor, activating the insulin receptor, and stimulating the uptake of glucose. Pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.

Abstract: Use of at least one aminophenol derivative of formula (I) below: in which: R represents a hydrogen atom or a radical —COR2, wherein R2 represents a saturated or unsaturated, linear, cyclic or branched, optionally hydroxylated, C1 to C30 hydrocarbon or alkoxy radical; R1 is a radical of formula (a), (b) or (c) below: (a) —CO—NR3R4 (b) —CO—O—R5 (c) —SO2—R5 wherein R3 represents a hydrogen atom or a linear or branched, saturated or unsaturated, optionally hydroxylated, C1 to C6 hydrocarbon radical, R4 represents a hydrogen atom or a saturated or unsaturated, linear, cyclic or branched, optionally hydroxylated, C1 to C30 hydrocarbon radical, and R5 represents a saturated or unsaturated, linear, cyclic or branched, optionally hydroxylated, C1 to C30 hydrocarbon radical, in a depigmenting and/or bleaching cosmetic composition for human skin, body hairs or head hair; compositions comprising the derivatives of formula (I) and a process for

Abstract: This invention relates to a process for making certain phenyl urea compounds by using a Lewis acid to effect the ring opening of a benzoxazolinone by an amine.

Abstract: The invention provides compounds, compositions and methods for modulating the effects of LXR in a cell. The compounds and compositions are useful both as diagnostic indicators of LXR function and as pharmacologically active agents. The compounds and compositions find particular use in the treatment of disease states associated with cholesterol metabolism, particularly atherosclerosis and hypercholesterolemia.

Abstract: Peptoid compounds of Formula I and Formula II are disclosed The compounds are useful in the treatment of matrix metalloproteinase-mediated disorders.

Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.

Abstract: This invention relates to the use of phenyl ureas of formulas (I) and (II) in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8). The variables of (I) and (II) are defined herein.

Abstract: The invention relates to new phenylamidine derivatives, processes for preparing them and their use as pharmaceutical compositions.

Abstract: Phenylcarbamates of the formula I ##STR1## where the substituents and the index have the following meanings: R is cyano, nitro, trifluoromethyl, halogen, alkyl or alkoxy;m is 0, 1 or 2;R.sup.1 is alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl, and, in the event that X is NR.sup.a, additionally hydrogen;X is a direct bond, O or NR.sup.a ;R.sup.a is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl;R.sup.2 is hydrogen,substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, alkylcarbonyl or alkoxycarbonyl;R.sup.3 and R.sup.4 independently of one another are hydrogen, cyano, nitro, hydroxyl, amino, halogen, hetaryloxy, hetarylthio, hetarylamino or N-hetaryl-N-alkylamino, andR.sup.5 is one of the groups mentioned under R.sup.3 or a group CR.sup.d .dbd.NOR.sup.e ;processes and intermediates for their preparation, and their use.

Abstract: The present invention is concerned with diaryl compounds of formula (I) and their use in medical therapy, particularly in the prophylaxis or treatment of a clinical condition for which an ACAT inhibitor is indicated, such as hyperlipidaema or atherosclerosis. The invention also relates to pharmaceutical compositions and processes for the preparation of compounds according to the invention.

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

Abstract: Iminooxymethyleneanilides of the formula I ##STR1## where the substituents and the index have the following meanings: R is hydrogen,unsubst. or subst. alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, alkylcarbonyl or alkoxycarbonyl;R.sup.1 is alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl and in the case where X is NR.sup.a, additionally hydrogen;X is a direct bond, O or NR.sup.a ;R.sup.a is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl;R.sup.2 is cyano, nitro, trifluoromethyl, halogen, alkyl or alkoxy;n is 0, 1 or 2;R.sup.3 is hydrogen, hydroxyl, cyano, cyclopropyl, trifluoromethyl, halogen, alkyl, alkoxy or alkylthio;R.sup.4 is hydrogen, hydroxyl, halogen, alkyl, haloalkyl, alkoxy, alkylthio,unsubstituted or substituted cycloalkyl, heterocyclyl, aryl, arylalkyl, hetaryl or hetarylalkyl;R.sup.

Abstract: Compounds of formula I ##STR1## wherein R1.dbd.(cyclo)alk(en)yl, aralkyl, alkyl(oxy)carbonyl, CONH2, etc.; R2.dbd.H, (cyclo)alk(en)yl, aralkyl, etc.; R3-R5.dbd.H, halo, alkyl, alkoxy, etc.; R6,R7.dbd.H, alkyl; R6R7.dbd.atoms to complete a ring; R8,R9.dbd.groups cited for R2, 2-oxoimidazolidinoalkyl, etc.; NR8R9=heterocyclyl; 1 of X,Y=CH2 and the other.dbd.CH2, O, S were prepd. Thus, 1-indancarboxylic acid was converted in 5 steps to 1-(N,N-dipropylaminomethyl)-6-formylaminoindane oxalate which had ED50 of 0.0055.mu.M/kg s.c. in the 8--OH DPAT cue agonism test in rats.

Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.

Abstract: Disclosed herein are substituted vinylurea derivatives represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.3 are independently a phenyl group which may be substituted, R.sup.2 is a phenyl group which may be substituted, or a cycloalkyl group, and wave lines mean that the bonding state may be either E or Z, with the proviso that the cases where R.sup.1, R.sup.2 and R.sup.3 are unsubstituted phenyl groups, and where R.sup.1 and R.sup.2 are unsubstituted phenyl groups and R.sup.3 is a 4-ethoxyphenyl group are excluded, or salt thereof, and medicines comprising such a derivative as an active ingredient as well as a method of preventing and treating arteriosclerosis with such a medicine. The derivatives or salts thereof selectively and strongly inhibit ACAT in macrophages and are hence useful as prophylactic and therapeutic agents for arteriosclerosis.

Abstract: Disclosed are a phenol compound represented by the formula (1): ##STR1## wherein R.sup.0 represents H, alkyl or alkyloxy; R.sup.1 represents alkyl; R.sup.2 represents alkyl or alkyloxy; OR.sup.3 represents OH; R.sup.4 represents H, lower alkyl or acyl, each of the above substituents may be substituted; W represents O, S or NR.sup.7 ; where R.sup.7 represents H, alkyl, aryl, OH or alkyloxy, a group of the formula (2): ##STR2## represents an amino which may be mono- or di-substituted or heterocyclic group containing N atom,or a pharmaceutically acceptable salt thereof, and a process for preparing the same.

Abstract: Carbamates of the formula I ##STR1## where the substituents have the following meanings: Z is methoxy, NH.sub.2, NHCH.sub.3, N(CH.sub.3).sub.2, CH.sub.3, C.sub.2 H.sub.5, CF.sub.3 or CCl.sub.3,X and Y are identical or different and each is hydrogen, F, Cl, Br, CF.sub.3, CN, NO.sub.2, alkoxy, alkenyloxy, alkynyloxy, alkyl, alkenyl or alkynyl or may be condensed together to form a substituted or unsubstituted aromatic or heteroaromatic, alicyclic or heterocyclic, partially or completely hydrogenated ring,R.sup.1 may also be substituted or unsubstituted and is O-alkyl, O-alkenyl, O-alkynyl, O-cycloalkyl, O-cycloalkenyl or O--CO.sub.2 -alkyl,A is --O--, --S--, --CR.sup.2 .dbd.CR.sup.3 --, CHR.sup.2 --O--, --CHR.sup.2 --S--, --CHR.sup.2 --O--N.dbd.C(R.sup.4)--, --CR.sup.2 .dbd.N--O--, --O--N.dbd.C(R.sup.4)--, --C.tbd.C--, --CHR.sup.2 --CHR.sup.3 --, --CHR.sup.2 --O--CO--, --O--CHR.sup.

Abstract: The present invention relates to achiral polyurea oligomers, their uses and formulations as anti-HIV pharmaceuticals and to a process for the preparation of narrow mono- and polydispersed oligomers as an emodiment of the invention. The achiral oligomers are derived from repeating units of the monomer 4,4'-diamino-biphenyl-3,3'-disulfonic acid and are water soluble, have a rigid backbone, possess ordered anionic spacing and have a number average molecular weight of <20,000. The process relates to the synthesis of narrow poly- and mono-dipersed oligomers comprising the steps of: 1) restricting the crude olydispersed anionic oligomer mixture to a narrow polydispersed anionic oligomer mixture to a narrow polydispersed anionic oligomer mixture; and/or 2) isolating the monodispersed anionic oligomer; and 3) optionally converting the narrow poly- or mono-dispersed anionic oligomer salt from Step 1 or 2 to a desired pharmaceutically-acceptable salt, especially a solim or potassium salt.

Abstract: The present invention provides a process for the preparation of a compound of formula ##STR1## wherein R is a straight or branched alkyl group of from one to twelve carbon atoms; M represents hydrogen or a pharmaceutically acceptable cation; and A is selected from optionally substituted carbocyclic phenyl.

Abstract: A compound having the formula ##STR1## or a pharmaceutically acceptable salt thereof, whereinX, Z, Y, A, D, E, F, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.11, R.sup.12 have the meanings set forth in the specification, pharmaceutical compositions comprising the same, and a method of treating therewith.The compounds are useful as potassium channel openers.

Abstract: The present invention provides a novel N-hydroxyurea compound of chemical formula (I) wherein R.sup.1 and R.sup.2 are each independently hydrogen or C.sub.1 -C.sub.4 alkyl; Ar is phenyl or mono-, di- or trisubstituted phenyl; A is a valence bond or a C.sub.1 -C.sub.6 alkylene chain, optionally having one double bond or one triple bond in the chain, and optionally having one or more C.sub.1 -C.sub.4 alkyl groups attached to the chain: X is oxygen or sulfur, n is an integer of 3 to 6; M is hydrogen, pharmaceutically acceptable cation or a metabolically cleavable group: and X and A may be attached at any available position on the ring. These compounds are useful for treatment or alleviation of inflammatory diseases, allergy and cardiovascular diseases in mammals and as the active ingredient in pharmaceutical compositions for treating such conditions.

Abstract: A benzene, pyridine or pyrimidine derivative having the below shown formula is novel and useful as an anti-arteriosclerotic agent. ##STR1## wherein R.sup.1 stands for a lower alkyl group, an amino group which may be substituted, or the like; R.sup.2 stands for a group represented by the formula: ##STR2## (wherein R.sup.16 stands for an alkyl group having 1 to 6 carbon atoms, or the like) or the like; R.sup.3 stands for a group represented by the formula: --O--(CH.sub.2).sub.m --Y (Y stands for an imidazolyl or piperazinyl group, or the like and m is 1 to 6) or the like; R.sup.5 stands for a hydrogen atom, a lower alkyl group, or the like; A stands for a group represented by the formula: ##STR3## (wherein R.sup.6 stands for a hydrogen atom, a lower alkyl group, or the like), --N.dbd., or the like; and B stands for a group represented by the formula: ##STR4## (wherein R.sup.4 stands for a hydrogen or the like), --N.dbd., or the like.

Abstract: Urea derivatives of formula (I) ##STR1## wherein the valuable groups are as defined in the specification, which possess both an ACAT inhibitory activity and an antioxidative activity. Those derivatives are useful in the prophylaxis and treatment of hypercholesterolemia and atherosclerosis.

Abstract: Compounds of formula (I) are provided: ##STR1## wherein: R.sup.1 represents an alkyl group; or a group of formula (II), (III), (IV) or (V): ##STR2## and wherein the groups R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are hydrogen or various organic groups; and pharmaceutically acceptable salts thereof; as well as methods for the preparation of such compounds and their use in the treatment and prophylaxis of hypercholesteremia and arteriosclerosis.

Abstract: Useful ureas have the formula ##STR1##

Abstract: Urea derivatives of formula (1) ##STR1## wherein the valuable groups are as defined in the specification, which possess both an ACAT inhibitory activity and an antioxidative activity. Those derivatives are useful in the prophylaxis and treatment of hypercholesterolemia and atherosclerosis.

Abstract: Compounds of formula (I) are provided: ##STR1## wherein: R.sup.1 represents an alkyl group; or a group of formula (II), (III), (IV) or (V): ##STR2## and wherein the groups R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are hydrogen or various organic groups; and pharmaceutically acceptable salts thereof; as well as methods for the preparation of such compounds and their use in the treatment and prophylaxis of hypercholesteremia and arteriosclerosis.