Abstract: The present invention provides compounds of Formula (I): 1

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

Abstract: This invention relates to new oxazolidinones having a cyclopropyl moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and enterococci, Bacteroides spp., Clostridia spp. species, as well as acid-fast organisms such as Mycobacterium tuberculosis and other mycobacterial species. The compounds are represented by structural formula I: its enantiomer, diastereomer, or pharmaceutically acceptable salt or ester thereof.

Abstract: Antiatherosclerotic agents are provided which are represented by Formulas I or II: wherein R is wherein R9, R10, R11, R12, R13, and R14 are each, independently, hydrogen or a lower alkyl of 1-6 carbon atoms; R6, and R7 are each, independently, hydrogen, lower alkyl of 1-6 carbon atoms, or CH2COOR8, where R8 is a lower alkyl of 1-6 carbon atoms; and X is O or S; R1 is hydrogen or a lower alkyl of 1-6 carbon atoms; R2, R3, and R4 are each, independently, hydrogen or halogen; and R5 is a lower alkyl of 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.

Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.

Abstract: Novel aromatic and heterocyclic thiazolyl thiourea compounds, pharameutical compositions including such, and methods for their use are disclosed. The compounds are effective agents for the treatment of HIV infection, including non-nucleoside inhibitor-resistant, and multi-drug resistant strains of HIV.

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: Compounds of the formula I: 1

Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ═C(R1a)— or —[N□(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; —G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted bi

Abstract: Novel chiral derivitaves of non-nucleoside inhibitors (NNI), particularly R-isomers of halopyridyl and thiazoyl thiourea compounds are provided as potent inhibitors of reverse transcriptase (RT), and particularly of retroviral RT, most particularly HIV RT. The stereospecific compounds and compositions of the invention inhibit replication of retrovirus, particularly human immunodeficiency virus-1 (HIV-1) and drug resistant strains.

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 current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.

Abstract: This invention relates to novel processes for preparing heteroaryl-substituted urea compounds of formula (I): 1

Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.

Abstract: The invention provides compounds of the formula: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 and R3 are independently hydrogen atom or an optionally substituted hydrocarbon group; n is an integer of 0-3; or salts thereof, which are useful as medicines having an osteogenesis promoting effect and chondrogensis promoting effect. The present invention relates to an amine compound having an excellent effect of inhibiting production and/or secretion of amyloid-b protein, a production and use thereof. Especially, it is effective for preventing and/or treating, for example, neurodegenerative diseases, amyloid angiopathy, neurological disorders caused by cerebrovascular disorders, and so forth.

Abstract: Compounds of the formula: as well as pharmaceutically usable salts and esters thereof, wherein R1, R2 and R3 have the significance ascribed herein, inhibit binding of adhesive proteins to the surface of different types of cell and accordingly influence cell-cell and cell-matrix interactions. These compounds can be used in the form of pharmaceutical preparations for the control or prevention of neoplasms, tumor metastasing, tumor growth, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, fibrosis, kidney failure, as well as infection caused by viruses, bacteria or fungi.

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: A compound having the formula selected from the group consisting of wherein either R3p and R4p are identical and selected from the group consisting of —OH, protected —OH and acyloxy of 1 to 8 carbon atoms, R2p is selected from the group consisting of —CN, —F, Br and I and R1p and R5p are hydrogen or R5p is —F and R1p and R2p are hydrogen or R1p and R2p are F and R5p is hydrogen, or R4p and R5p are identical and selected from the group consisting of —OH, protected —OH and acyloxy of 1 to 8 carbon atoms, R3p is selected from the group consisting of F and —CN and R1p and R2p are hydrogen, R8 is hydrogen or an amine protective group and R10 is the remainder in which the hydroxy or amino are protected wherein R′1 is selected from the group consisting of alkyl of 1 to 4 carbon atoms, —CN, carboxy and alkoxy carbonyl of 1 to 4 carbon atoms.

Abstract: Compounds of formula (I) as well as pharmaceutically usable salts and esters thereof, wherein R1, R2 and R3 have the significance described in the specification, inhibit the binding of adhesive proteins to the surface of different types of cell and accordingly influence cell-cell and cell-matrix interactions. They can be used in the form of pharmaceutical preparations in the control or prevention of neoplasms, tumor metastasizing, tumor growth, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, fibrosis, kidney failure as well as infections caused by viruses, bacteria or fungi.

Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.

Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.

Abstract: Disclosed is a carbamyl chloride of an aminoarylcarbonyl compound having the structural formula I: wherein R is an alkyl, alkenyl, or aryl group; A is an aryl (including heteroaryl) ring group; each R′ is independently an alkyl group which may form a ring with Z or Z′; p is 0, 1, 2, or 3; each Z, Z′, and Y is independently hydrogen or a substituent; and n is 0, 1, or 2.

Abstract: Thiazolimine derivatives of the formula I ##STR1## where: X and Y independently of one another are each hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl;Z is hydrogen; C.sub.l -C.sub.8 -alkyl, C.sub.2 -C.sub.8 -alkenyl, C.sub.2 -C.sub.8 -alkynyl, C.sub.1 -C.sub.8 -alkoxy, C.sub.1 -C.sub.8 -alkylthio, it being possible for these groups to be substituted by one to five halogen or C.sub.1 -C.sub.4 -alkoxy; aryl, hetaryl, benzyl, it being possible for these groups to be substituted by C.sub.l -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.l -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, halogen, nitro or cyano; or one of the groups below: ##STR2## R.sup.1 and R.sup.2 are each hydrogen, halogen; C.sub.1 -C.sub.4 -alkyl, C.sub.2 -C.sub.4 -alkenyl, C.sub.2 -C.sub.4 -alkynyl, it being possible for these groups to be substituted by one to five halogens or by C.sub.1 -C.sub.4 -alkoxy;n is 1 or 2;m is 0, 1 or 2R.sup.3 -R.sup.

Abstract: The present invention relates to a pharmaceutical composition containing as active agent, solid particles of a compound selected from the group consisting of:compound of formula I: ##STR1## compound of formula II: ##STR2## and mixtures thereof. said particles having a particle size smaller than 200 .mu.m, the mean particle size of the said active solid particles being greater than 10 .mu.m.It also relates to a pharmaceutical composition which contains at least one pharmaceutically acceptable acid.

Abstract: One pot synthesis of 1,2,4-triazoles uses thioimidate intermediate and 1,2-dichloroethane solvent.

Abstract: The present invention concerns novel compounds represented by the Formula: ##STR1## wherein: A is R.sup.1.sub.q (R.sup.3 R.sup.60 N).sub.m (Z)(NR.sup.2).sub.n ; m and q are each 0 or 1, with the proviso that when q is 1, m is 0 and when q is 0, m is 1; Z is C.dbd.O or SO.sub.2 ; n is 1 with the proviso that, when Z is C.dbd.O, m is 1; X is --NH--, --CH.sub.2 --, or --OCH.sub.2 --; Y is [2-imidazoline, 2-oxazolin] 2-thiazoline, [or 4-imidazole] R.sup.1 is H, lower alkyl, or phenyl, with the proviso that, when R.sup.1 is H, m is 1; R.sup.2, R.sup.3, R.sup.60 are each independently H, lower alkyl, or phenyl; R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are each independently hydrogen, lower alkyl, --CF.sub.3, lower alkoxy, halogen, phenyl, lower alkeny, hydroxyl, lower alkylsulfonamido, or lower cycloalkyl, wherein R.sup.2 and R.sup.

Abstract: An amide derivative represented by the following general formula (I) or a salt thereof and a pharmaceutical composition containing the amide derivative and a pharmaceutically acceptable vehicle. ##STR1## (The symbols in the formula have the following meanings. (whereinA: heteroarylene;X: bond, O, S, --NR.sup.5 --, --NR.sup.5 CO--, --NR.sup.5 CONH--, --NR.sup.5 SO.sub.2 -- or --NR.sup.5 C(.dbd.NH)NH--;R.sup.1 : --H, -optionally substituted lower alkyl, -optionally substituted aryl, -optionally substituted heteroaryl or -optionally substituted cycloalkyl;R.sup.2a, R.sup.2b : --H or -lower alkyl, which may be the same or different;R.sup.3 : --H or -lower alkyl;R.sup.4a, R.sup.4b : --H or --OH, which may be the same different, or R.sup.4a and R.sup.4b are taken together to form .dbd.O or .dbd.N.about.O-lower alkyl; andR.sup.5 : --H or -lower alkyl.

Abstract: Described are novel photochromic six-membered heterocyclic-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted six-membered heterocyclic group fused to one side of the naphtho portion of the naphthopyran and having certain substituents at the position ortho to the oxygen atom of the naphthopyran ring. These compounds may be represented by the following graphic formula: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans, and spiro(indoline) type compounds.

Abstract: A substituted 2,4-imidazolidinedione compound corresponding to the formula I ##STR1## a process for production thereof and the use of these compounds in a pharmaceutical preparation are described. Substituents R1, R2, R3 and R4 have the same meaning as defined in the specification.

Abstract: A sulfonamide derivatives of formula (I) ##STR1## a non-toxic salts, an acid addition salts or a solvates thereof which has an inhibitory effect on elastase.

Abstract: The present invention relates to new substituted oxazolidinones of the general formula (1) ##STR1## in which the substituents have the meaning indicated in the description, processes for their preparation and their use as medicaments, in particular as antibacterial medicaments.

Abstract: Described are novel pentahydrophenanthro?9,10-b!pyrans and tetrahydrocyclopenta?c!-naphtho?1,2-b!pyrans. Also described are polymeric organic host materials that contain or that are coated with such compounds.

Abstract: The present invention relates to molecules capable of modulating tyrosine signal transduction to prevent and treat cell proliferative disorders or cell differentiation disorders associated with particular tyrosine kinases by inhibiting one or more abnormal tyrosine kinase activities.

Abstract: 4-Aminobenzoylguanidines of the formula I ##STR1## in which A, R.sub.1, R.sub.2 and R.sub.3 have the meanings given, and the physiologically unobjectionable salts thereof exhibit antiarrhythmic properties and are active as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter.

Abstract: Treatment of AIDS, inhibition of the replication of HIV and related viruses thereof, and formulations using thiourea derivative compounds or salts thereof is disclosed. Also disclosed are novel thiourea derivative compounds.

Abstract: A novel thiazole derivative represented by general formula (I), which has a selected agonistic activity for 5-HT.sub.3 receptor, a pharmaceutical composition thereof, and a process for producing the same. In the said formula, R.sup.1 represents hydrogen or lower alkoxy; R.sup.2 and R.sup.3 are such that R.sup.2 represents hydrogen and R.sup.3 represents a group, --Y--Het, wherein Y represents a single bond or lower alkylene and Het represents a nitrogenous heterocyclic group, or alternatively R.sup.2 and R.sup.3 are combined together to form a group, --(CH.sub.2).sub.m --NR.sup.4 --(CH.sub.2).sub.n --, wherein m and n are each 1 or 2 and R.sup.4 represents lower alkyl; and X represents --NH--, --NHC(.dbd.O)NH--, --C(.dbd.O)NH-- or --NHC(.dbd.O)--.

Abstract: Herbicidal novel tetrazolinone derivatives of the formula: ##STR1## wherein R.sup.1 is alkyl, haloalkyl, cycloalkyl, alkenyl, haloalkenyl, alkynyl, alkoxy or phenyl which is optionally substituted, andR.sup.2 is alkyl, haloalkyl, cycloalkyl, alkenyl, haloalkenyl, alkynyl, alkoxy or phenyl which is optionally substituted, orR.sup.1 and R.sup.2 form, together with the nitrogen atom to which R.sup.1 and R.sup.2 are bonded, a 5- or 6-membered heterocyclic ring, optionally fused to a carbocyclic ring optionally and independently substituted by C.sub.1-4 alkyl, andR.sup.3 is a 5-membered heterocyclic radical containing at least one hereto atom selected from the group consisting of nitrogen, oxygen, and sulfur, optionally substituted by at least one substitutent selected from the group consisting of halogen, benzyl, phenyl, halogen-substituted phenyl, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylthio, C.sub.1-4 alkyl-sulfonyl and C.sub.

Abstract: An iminothiazoline compound of the formula: ##STR1## which is useful as a herbicide.

Abstract: Benzyl derivatives of the formula I ##STR1## where A is CH.sub.2, CHCl, CH-alkyl, CH-alkoxy, CH-alkylthio or N-alkoxy,B is OH, alkylthio, alkoxy or alkylamino,U, V, W are hydrogen, halogen, alkyl or alkoxy,D is ##STR2## where R' is hydrogen or alkyl andR is hydrogen, alkyl, cycloalkyl, haloalkyl, halocycloalkyl, cycloalkylalkyl, alkoxyalkyl, alkylthioalkyl, arylthioalkyl, aryloxyalkyl, aryl, arylalkyl, hetaryl, hetaryl-alkyl, hetaryloxyalkyl or heterocyclyl, and fungicides containing these compounds.

Abstract: Azole derivatives, process for their preparation, and their useAzole derivatives of the formula (I) ##STR1## in which A, L, O, R.sup.1, X, Y, Z and q have the meanings given, process for their preparation, pharmaceutical preparations and the use of the compounds are described. Azole derivatives of the formula I where the symbols have for example the following meanings:R.sup.1 is (C.sub.2 -C.sub.10)-alkyl,Z is nitrogen,X and Y are independently of one another CR.sup.2,L is --CH.sub.2 --,q is zero or 1,A is a biphenyl radical which is substituted for example by R.sup.15,R.sup.2 is halogen or hydrogen,R.sup.15 is SO.sub.2 --NH--CO--OR.sup.6 andR.sup.6 is phenyl,are highly active antagonists of angiotensin II receptors.

Abstract: Novel 2,2-disubstituted glycerol-like compounds are disclosed for use as anti-allergic and anti-inflammatory compounds. The compounds are antagonists of platelet activating factor ("PAF"). Also disclosed are methods of synthesizing and using the compounds of the invention as well as pharmaceutical compositions thereof. The compounds have the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are as defined in the specification.

Abstract: An iminothiazoline compound of the formula: ##STR1## which is useful as a herbicide.

Abstract: A cycloalkylurea compound of the formula (I): ##STR1## wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, which compound inhibits ACAT and is useful as hypolipidemic and antiatherosclerotic medicine.

Abstract: Benzyl derivatives of the formula I ##STR1## where A isCH.sub.2, CHCl, CH-alkyl, CH-alkoxy, CH-alkylthio or N-alkoxy,B isOH, alkylthio, alkoxy or alkylamino,U, V, W arehydrogen, halogen, alkyl or alkoxy,D is ##STR2## where R' ishydrogen or alkyl andR ishydrogen, alkyl, cycloalkyl, haloalkyl, halocycloalkyl, cycloalkylalkyl, alkoxyalkyl, alkylthioalkyl, arylthioalkyl, aryloxyalkyl, aryl, arylalkyl, hetaryl, hetaryl-alkyl, hetaryloxyalkyl or heterocyclyl, and fungicides containing these compounds.

Abstract: The invention relates to novel heterocyclyltriazolinones of the general formula (I) ##STR1## in which R.sup.1 represents hydrogen, hydroxyl, cyano or alkyl, alkenyl, alkinyl, cycloalkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, arylsulphonyl, amino or heterocyclyl, each of which is optionally substituted,R.sup.2 represents hydrogen, hydroxyl, mercapto, halogen or alkyl, alkenyl, alkinyl, cycloalkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, arylalkyl, amino or heterocyclyl, each of which is optionally substituted, andHet represents an optionally substituted heterocycle of the formula ##STR2## in which X in each case represents oxygen, sulphur, an NH group or an N-alkyl group,a process for their preparation and their use as herbicides.

Abstract: There is disclosed an iminothiazoline compound of the formula: ##STR1## wherein R.sup.1 is halogen, halo(lower)alkyl, halo(lower)alkoxy or halo(lower)alkylthio; R.sup.2 is lower alkyl, chlorine; bromine or iodine; R.sup.3 is (lower alkyl)carbonyl, (lower cycloalkyl)carbonyl, (lower cycloalkoxy)carbonyl, (lower alkoxy)carbonyl or (lower alkyl)sulfonyl, all of which are optionally substituted with at least one substituent selected from halogen, lower alkyl, lower alkoxy, lower cycloalkyl and lower cycloalkoxy; and R.sup.4 is halogen. Also disclosed are a process for producing this compound, a herbicidal composition comprising this compound as an active ingredient, and a method for controlling undesired weeds by use of this compound as a herbicide.

Abstract: A 2-Acylaminothiazole of formula: ##STR1## in which R.sub.1 is H, an alkyl or a substituted alkyl; R.sub.IV is a cycloalkyl, an aromatic group such as phenyl or a heterocyclic group which are unsubstituted or substituted; R.sub.V is a substituted alkyl, a substituted carboxy such as an ester or an amide; or R.sub.IV and R.sub.V together represent a phenoxyalkylene group which may be substituted on the phenyl; and Z is a heterocyclic e.g. indolyl group; or a salt of compound (I).

Abstract: Thiourea compounds represented by the general formula: ##STR1## wherein A is an aromatic ring group which may be substituted; R.sup.1 is a hydrogen atom or a lower alkyl or aryl group which may be substituted, or may combine with A to form a cyclic ring; and --COB is an acyl group of a carboxylic acid or an esterified carboxyl group or salts thereof are provided as agents for inhibiting the formation of AGE (Advanced Glycosidation End Product), which are employable for treating diseases caused by AGE-formation, such as diabetic complications, senile cataract, atherosclerosis etc.

Abstract: This invention relates to new heterocyclic derivatives of guanidine and more particularly to such derivatives which have hypoglycemic activity, their methods of use for treating hyperglycemia and novel intermediate compounds for their preparation.