Abstract: The present invention relates to a new method for the synthesis of purine LNA (Locked Nucleic Acid) analogues which provides a higher overall yield. The method comprising a regioselective 9-N purine glycosylation reaction followed by a one-pot nucleophilic aromatic substitution reaction of the 6-substituent in the purine ring and simultaneous nucleophile-induced intramolecular ring closure of the C-branched carbohydrate to form novel purine LNA analogues. The novel strategy is illustrated by the synthesis of the novel compound (1S,3R,4R,7S)-7-benzyloxy-1-methanesulfonylmethyl-3-(guanin-9-yl)-2,5-dioxabicyclo[2.2.1]heptane which is easily converted into (1S,3R,4R,7S)-7-hydroxy-1-hydroxymethyl-3-((2-N-isobutyrylguanin-9-yl)-2,5-dioxabicyclo[2.2.1]heptane after isobutyryl protection of the 2-amino purine group and subsequent substitution of 1-methanesulfonyl with benzoate, debenzoylation and debenzylation.

Abstract: Disclosed are compounds of the formula: wherein R3, R6a, R6b and R8 are substituted as disclosed herein. The compounds are effective in effecting PDE IV inhibition in patients in need thereof.

Abstract: Novel compounds and pharmaceutical compositions thereof, and methods of using same in treating anxiety, depression, and other psychiatric and neurological disorders. The novel compounds provided by this invention are those of the following formulae: wherein R1, R13, X, Y, Z, G and Q are as defined herein.

Abstract: With the above and other objects in view, the present invention comprises compounds having the general formula (I): wherein: R1 is a C2-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, C3-8 cycloalkenyl or cycloalkynyl, wherein said alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl or cycloalkynyl is optionally substituted with hydroxy, C1-5 alkoxy, C3-5 cycloalkoxy, halogen, oxo, carbamido, hydroxycarbamido, oximido, C1-5 alkyloximido, C3-5 cycloalkyloximido, C1-5 acyloximido or C3-5 cycloacyloximido; Q is methylene or ethylene; R3 is aryl or heteroaryl wherein said aryl or heteroaryl has one to three substituents selected from the group consisting of C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C3-6 cycloalkenyl, cycloalkynyl, C3-5 alkylene, C3-5 cycloalkylene, haloC1-6 alkyl, haloC1-6 cycloalkyl, hydroxy, C1-5 alkoxy, C3-5 cycloalkoxy, C1-2 alkylenedioxy, C1-6 acyl, C3-6 cycloacyl, C1-6 acyloxy, C3-6 cycloacyloxy, halogen, nitro or cyano; R8 is C1-5 alkyl or C3-5 cycl

Abstract: Compounds of Formula I and II and their pharmaceutically acceptable, salts, esters and prodrugs thereof are selective alpha-1D adrenoceptor anatagonists and may be useful for treating disease states.

Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

Abstract: The present invention concerns the compounds of formula ##STR1## the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein each R.sup.1 is independently hydrogen, halogen, C.sub.1-6 alkyl, nitro, hydroxy or C.sub.1-4 alkyloxy; Alk is C.sub.1-6 alkanediyl; n is 1 or 2; D is an optionally substituted mono-, bi- or tricyclic nitrogen containing heterocycle having central .alpha..sub.2 -adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine.

Abstract: This invention relates to sulfamides of formula (I) ##STR1## that are inhibitors of metalloproteases, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.

Abstract: The subject invention concerns a compound of the formula (i): ##STR1## in which Q represents heteroaryl or heterocyclo optionally substituted with one or more substituents selected from the group consisting of C.sub.1-6 alkyl (optionally substituted with one or more halogens), C.sub.1-6 alkyl--S(O)n-- (where n is 0, 1 or 2), --CO.sub.2 H (or C.sub.1-6 alkyl esters thereof or C.sub.1-6 alkyl amides thereof), halogen, C.sub.1-6 alkoxy, CN, NO.sub.2 and NR.sub.7 R.sub.8;R.sub.1 -R.sub.5, which may be the same or different, each represent C.sub.1-6 alkyl (optionally substituted with one or more halogens), C.sub.1-6 alkyl--S(O)n-- (where n is 0, 1 or 2), --CO.sub.2 H (or C.sub.1-16 alkyl esters thereof or C.sub.1-6 alkyl amides thereof), halogen, C.sub.1-6 alkoxy, CN, NO.sub.2, NR.sub.7 R.sub.8 or H (provided R.sub.1 -R.sub.6 are not all H simultaneously);R.sub.6 represents H, C.sub.1-6 alkyl, --CO.sub.2 H (or C.sub.1-6 alkyl esters thereof or C.sub.1-6 alkyl amides thereof), --CN, C.sub.

Abstract: Compounds and pharmaceutical compositions, including resolved enantiomers and/or diastereomers, hydrates, salts, solvates and mixtures thereof, have the formula:CORE MOIETY--(R).sub.jIn these compounds, j is an integer from one to three; the core moiety is a cyclic core, the cyclic core being non-cyclic or at least one five- to seven-member non-heterocyclic ring or heterocycle; and R is selected from the group consisting of amine, hydrogen, halogen, hydroxyl, substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(2-10) alkenyl, cyclic or heterocyclic group or formula I. At least one R having formula I: ##STR1## In formula I, n is an integer from four to twenty; and each R.sub.1 or R.sub.2 is independently hydrogen, substituted or unsubstituted C.sub.(1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl or cyclic or heterocyclic group.

Abstract: Therapeutic compounds with at least one carboxylic acid, ester or amide-substituted side chain have the formula:CORE MOIETY --(R).sub.jwherein j is an integer from one to three. The core moiety is non-cyclic or cyclic (carbocyclic or heterocyclic). R may be selected from among hydrogen, halogen, hydroxyl, amino, substituted or unsubstituted C.sub.(1-10) alkyl, C.sub.(2-10) alkenyl, carbocyclic or heterocyclic groups and at least one R has the formula I: ##STR1## wherein: one or two p are the integer one, otherwise p is two; and n is an integer from three to twenty; R.sub.1 is selected from the group consisting of substituted and unsubstituted CH.sub.2 ; NR.sub.3, R.sub.3 being hydrogen, substituted or unsubstituted C.sub.(1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl or C.sub.(1-20) hydroxyalkyl, or carbocyclic or heterocyclic group; O; --CHR.sub.4 O--, R.sub.4 being substituted or unsubstituted C.sub.(1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl, C.sub.(1-20) hydroxyalkyl, or R.sub.

Abstract: Disclosed are compounds having the formulae: ##STR1## wherein: Q.sub.3,Q.sub.6a,Q.sub.6b and Q.sub.8 are independently a bond, C.sub.1-8 alkylene, C.sub.2-8 alkenylene and C.sub.2-6 alkynylene, andR.sub.3, R.sub.6a, R.sub.6b, and R.sub.8 are independently hydrogen, aryl or heteroaryl, optionally substituted by halogen, hydroxy, alkoxy, nitro, cyano and carboxy, provided that:Q.sub.3 R.sub.3 is not hydrogen or methyl in formulae (I) or (II); and at least one of R.sub.3 and R.sub.8 is aryl or heteroaryl in formula (I).The compounds are effective PDE IV inhibitors and possess improved PDE IV inhibition and improved selectivity with regard to PDE III inhibition.

Abstract: A new class of xanthine compounds, variously substituted at the 1, 3, 7 and 8 positions, is characterized by an ability to modulate the activity of key enzymes involved in drug metabolism. These compounds generally are useful in affecting drug metabolism and, particularly, in extending the circulating half-life of compounds that are metabolized via P-450-mediated pathways.

Abstract: The present invention relates to novel compounds of the formula (I): ##STR1## wherein Q.sub.3 R.sub.3 and Q.sub.8 R.sub.8 are described herein. The compounds possess PDE-IV inhibitory activity and improved selectivity with regard to PDE-III inhibition. Also disclosed are pharmaceutical compositions and methods of treatment utilizing the disclosed compounds.

Abstract: The present invention relates to a compound of the formula and the pharmaceutically acceptable salts thereof wherein W is a bicyclic heterocyclic ring system. The compounds are .alpha.-1 adrenergic antagonists and are useful in the treatment of BPH; also disclosed are .alpha.-1 antagonist compositions and a method for antagonizing .alpha.-1 adrenoreceptors and treating BPH.

Abstract: O.sup.6 -hetarylalkyl- or naphthylalkylguanine derivatives of the formula ##STR1## wherein Y is H, ribosyl, deoxyribosyl, or R"XCHR',wherein X is O or S, R" and R"' are alkyl, or substituted derivatives thereof,R' is H, or alkyl or hydroxyalkylR is(i) a cyclic group having at least one 5- or 6-membered heterocyclic ring, optionally with a carbocylic or heterocyclic ring fused thereto, the or each heterocyclic ring having at least one hereto atom chosen from O, N, or S, or a substituted derivative thereof; or(ii) naphthyl or a substituted derivative thereofand pharmaceutically acceptable salts thereof, exhibit the ability to deplete O.sup.6 -alkylguanine-DNA alkyltransferase (ATase) activity.A process for preparation of the compounds is described. The compounds have utility in combination with alkylating agents in the chemotherapeutic treatment of tumour cells.

Abstract: Compounds of structural Formula (I) ##STR1## and pharmacologically acceptable salts and esters thereof possess 5.alpha.-reductase inhibitory activity. These compounds inhibit 5.alpha.-reductase type 1 and type 2. The compounds of structural Formula I are useful in the systemic, including oral, and parenteral, including topical, treatment and prevention of hyperandrogenic conditions including prostatic carcinoma, benign prostatic hyperplasia, acne vulgaris, seborrhea, androgenic alopecia (also called androgenetic alopecia) which includes male- and female-pattern baldness, female hirsutism, and prostatitis. A class of compounds of the present invention are also potent antiandrogens. The present invention also relates to novel compositions containing such compounds, methods of their use and methods of their manufacture.

Abstract: The present invention comprises a compound of formula I: ##STR1## R.sub.1 of Formula I is substituted amino represented by formula NR.sup.5 R.sup.6 wherein R.sup.5 and R.sup.6 are independently selected from the group consisting of hydrogen, C.sub.1-4 alkyl, and unsubstituted amino with the proviso that R.sup.5 and R.sup.6 are not both hydrogen, and further that R.sup.5 and R.sup.6 are not both amino. R.sub.2 and R.sub.3 of Formula I are independently selected from the group consisting of hydrogen; C.sub.1-4 alkyl; amino; substituted or unsubstituted thiol; and halogen. Moreover, R.sub.4 of Formula I is represented by the formula R.sup.12 -X.sup.12 wherein R.sup.12 is a saturated or unsaturated linear hydrocarbon chain of 5-20 carbons optionally containing one or more interruptions within the chain by a heteroatom, and optionally substituted with one or more .dbd.O, or .dbd.S. Finally, X.sup.12 is selected from the group consisting of hydroxy, an aminoalkyl group, and a known amino acid bound by its .alpha.

Abstract: A cyclopropane derivative represented by formula (I): ##STR1## wherein B represents a group of a purine derivative. Another aspect of the invention provides (3-oxa-2-oxobicyclo?3,1,0!hexan-1-yl)methanol and a method of preparing a cyclopropane derivative of formula (I) from this compound by replacing the hydroxyl group of the compound with a leaving group followed by reaction with a purine derivative.

Abstract: Compounds of the formula (i) ##STR1## have therapeutic utility via inhibition of TNF or phophodiesterase.

Abstract: A 2,6,9-trisubstituted purine composition having the following formula: ##STR1## where X is a amino, oxo, thio, of sulfone moiety, R.sub.1 is a lower alkyl, substituted lower alkyl, cycloalkyl, substituted cycloalkyl, cycloheteroalkyl, substituted cycloheteroalkyl, aryl, substituted aryl, heterocycle, hetaryl, substituted hetaryl, aralkyl, heteroaralkyl, heteroalkyl, alkyl alkenyl, alkyl alkynyl, alkyl cycloalkyl, or alkyl cycloheteroalkyl, each having from 1 to 20 carbon atoms; R.sub.2 is hydrogen, lower alkyl, substituted lower alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heterocycle, hetaryl, substituted hetaryl, aralkyl, heteroaralkyl, heteroalkyl, alkyl alkenyl, alkyl alkynyl, alkyl cycloalkyl, or alkyl cycloheteroalkyl; and R.sub.3 is halogen, hydroxyl, thio, alkoxy, alkylthio, lower alkyl, --NR.sub.4 R.sub.5 or a component having the formula: ##STR2## wherein when R.sub.3 is 2-hydroxyethylamino and R.sub.2 is methyl, R.sub.

Abstract: 1,3-Disubstituted-zanthines have therapeutic utility via TNF or phosphodiesterase inhibition.

Abstract: Compounds of general formula I and their salts and solvates are antifungal agents and as such are useful in the treatment of various fungal infections. Pharmaceutical compositions including these compounds and processes for their preparation are also provided.

Abstract: A cyclopropane derivative represented by formula (I): ##STR1## wherein B represents a group of a purine derivative. Another aspect of the invention provides (3-oxa-2-oxobicyclo?3,1,0!hexan-1-yl)methanol and a method of preparing a cyclopropane derivative of formula (I) from this compound by replacing the hydroxyl group of the compound with a leaving group followed by reaction with a purine derivative.

Abstract: A method of promoting drainage of mucous secretions in the congested airways of a bedridden/immobilized patient or an intubated/mechanically-ventilated patient is disclosed. The method comprises administering to the airways of the patient a uridine phosphate such as uridine 5'-triphosphate (UTP) or P.sup.1,P.sup.4 -di(uridine-5')tetraphosphate, an analog of UTP, or any other analog, in an amount effective to promote drainage of fluid in the congested airways, including sinuses, by hydrating mucous secretions or by stimulating ciliary beat frequency in the airways. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include any liquid suspension (including nasal drops or eye drops or spray), oral form (liquid or pill), aerosol inhalation, powder form, topical, injected, intra-operative instillation or suppository form.

Abstract: This invention is directed to purine derivatives of the following formulae: ##STR1## wherein Z.sup.1 is --O--, --N(R.sup.10)-- or --CH.sub.2 O--;Z.sup.2 is --O--, --N(R.sup.10)-- or --OCH.sub.2 --;R.sup.1 and R.sup.4 are each independently hydrogen, halo, alkyl, --OR.sup.10, --C(O)OR.sup.10, --C(O)N(R.sup.10)R.sup.11, --N(R.sup.10)R.sup.11, --N(R.sup.10)C(O)R.sup.10, or --N(H)S(O).sub.2 R.sup.13 ;R.sup.2 is --C(NH)NH.sub.2, --C(NH)N(H)OR.sup.10, --C(NH)N(H)C(O)OR.sup.13, --C(NH)N(H)C(O)R.sup.10, --C(NH)N(H)S(O).sub.2 R.sup.13, or --C(NH)N(H)C(O)N(H)R.sup.10 ;R.sup.3 is halo, alkyl, haloalkyl, haloalkoxy, ureido, cyano, guanidino, --OR.sup.10, --C(NH)NH.sub.2, --C(NH)N(H)OR.sup.10, --C(O)N(R.sup.10)R.sup.11, --R.sup.12 --C(O)N(R.sup.10)R.sup.11, --CH(OH)C(O)N(R.sup.10)R.sup.11, --N(R.sup.10)R.sup.11, --R.sup.12 --N(R.sup.10)R.sup.11, --C(O)OR.sup.10, --R.sup.12 --C(O)OR.sup.10, --N(R.sup.10)C(O)R.sup.

Abstract: Substituted xanthines of formula ##STR1## in which A represents a radical of the formula ##STR2## in which R.sup.3, R.sup.4, R.sup.6 and R.sup.7 denote hydrogen, cycloalkyl, aryl having 6 to 10 carbon atoms, or denote straight-chain of branched alkyl or alkenyl, each of which is optionally substituted; T, V, X and Y are identical or different and denote an oxygen or sulphur atom; R.sup.5 and R.sup.8 are identical or different and denote hydrogen, halogen, cycloalkyl having 3 to 8 carbon atoms or straight-chain or branched alkyl or alkenyl in each case having up to 8 carbon atoms, optionally substituted or R.sup.5 and R.sup.8 denote aryl having 6 to 10 carbon atoms or a 5- to 7-membered aromatic, optionally benzo-fused heterocycle having up to 3 heteroatoms S, N and/or O, each of which is optionally substituted; L represents an oxygen or sulphur atom; R.sup.2 represents mercapto, hydroxyl, straight-chain or branched alkoxy having up to 8 carbon atoms or the group of the formula ##STR3## in which R.sup.

Abstract: The invention relates to new xanthine derivatives of general formula I, processes for preparing them and their use as pharmaceutical compositions.

Abstract: This invention relates to a process for preparing xanthine derivatives of formula I: ##STR1## characterized in that a uracil derivative of formula A or B ##STR2## is dissolved in a suitable organic-aqueous solvent and cyclized in the presence of LiOH.

Abstract: Adenosine and xanthine derivatives, and compositions comprising those compounds, are potent selective agonists and antagonists of adenosine receptors. The derivatives and compositions are used to treat conditions, including certain cardiac arrhythmias.

Abstract: Xanthine derivatives, and compositions comprising those compounds, are potent selective antagonists of adenosine receptors. The derivatives and compositions are used to treat conditions, including certain cardiac arrhythmias. The compounds, specifically, are C-8 epoxide derivatives of xanthine having the general formulae of: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different, and can be H or an alkyl group of 1-4 carbons, and n=0-4; and ##STR2## wherein R.sub.1 and R.sub.2 are the same or different, and can be H or an alkyl group of 1-4 carbons, R.sub.3 is either O or (CH.sub.2).sub.1-4, and n=0-4.

Abstract: Methods for the treatment of Parkinson's disease comprising administering to a patient an agent which contains, as an active ingredient, a xanthine derivative or a pharmaceutically acceptable salt thereof. The xanthine derivative is represented by the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen, lower alkyl, lower alkenyl, or lower alkynyl; and R.sup.4 is cycloalkyl, --(CH.sub.2).sub.n --R.sup.5, wherein R.sup.5 represents substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group; and n is an integer of 0 to 4, or ##STR2## wherein Y.sup.1 and Y.sup.2 represent independently hydrogen, halogen, or lower alkyl; and Z is substituted or unsubstituted aryl, ##STR3## wherein R.sup.6 is hydrogen, hydroxy, lower alkyl, lower alkoxy, halogen, nitro, or amino; and m is an integer of 1 to 4, or a substituted or unsubstituted heterocyclic group; and X.sup.1 and X.sup.2 are independently O or S.

Abstract: Xanthines of the formula I ##STR1## wherein R.sub.1 is a C.sub.1 -C.sub.4 alkyl group:R.sub.2 is a C.sub.1 -C.sub.4 alkyl group;R.sub.3 tetrahydropyran-4-yl or 1,3-dithiolan or;R.sub.3 represents one of the groups of formula ##STR2## and pharmaceutically acceptable acid addition salts thereof. These are adenosine antagonists, capable of acting as cholinomimetics, useful for the treatment of CNS disorders such as senile dementia and Alzheimer's disease.

Abstract: The present invention relates to a compound of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein W is a bicyclic heterocyclic ring system. The compounds are .alpha.-1 adrenergic antagonists and are useful in the treatment of BPH; also disclosed are .alpha.-1 antagonist compositions and a method for antagonizing .alpha.-1 receptors and treating BPH.

Abstract: Agents for the treatment of Parkinson's disease contain, as an active ingredient, a xanthine derivative or a pharmaceutically acceptable salt thereof. The xanthine derivative is represented by the formula: ##STR1## in which R.sup.1, R.sup.2 are R.sup.3 are independently hydrogen, lower alkyl, lower alkenyl, or lower alkynyl; and R.sup.4 represents cycloalkyl, --(CH.sub.2).sub.n --R.sup.5 (in which R.sup.5 represents substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group; and n is an integer of 0 to 4), or ##STR2## in which Y.sup.1 and Y.sup.2 represent independently hydrogen, halogen, or lower alkyl; and Z represents substituted or unsubstituted aryl, ##STR3## in which R.sup.6 represents hydrogen, hydroxy, lower alkyl, lower alkoxy, halogen, nitro, or amino; and m represents an integer of 1 to 4, or a substituted or unsubstituted heterocyclic group; and X.sup.1 and X.sup.2 represent independently O or S.

Abstract: A quinoline compound represented by the formula (1) or a salt thereof: ##STR1## wherein the definition of each substituents are described in the specification, which have angiotensin II antagonism and hypotensive action and are useful as an agent for the prevention and treatment of cardiovascular system diseases such as hypertension, heart failure and the like.

Abstract: The present invention provides sulfur-containing xanthine derivatives which are 1,3-disubstituted with a C.sub.1 -C.sub.12 alkyl, which may be further substituted with a hydroxy, amino, or halo group, and are 8-substituted with either a cycloalkyl, furyl, thienyl, or substituted phenyl group. These derivatives possess increased selectivity or potency at adenosine receptors.

Abstract: Adenosine and xanthine derivatives, and compositions comprising those compounds, are potent selective agonists and antagonists of adenosine receptors. The derivatives and composition are used to treat conditions, including certain cardiac arrhythmias.

Abstract: There is disclosed compounds and pharmaceutical compositions having a xanthine core of the formula: ##STR1## wherein each of one or two R is independently ##STR2## wherein n is an integer from about 3 to about 18 forming a hydrocarbon chain, wherein the hydrocarbon chain may have one or more double bonds (preferably in a cis configuration), and may be substituted by a hydroxyl, halo or dimethylamino group and/or interrupted by an oxygen atom. The compounds lower elevated levels of unsaturated, non-arachidonate phosphatidic acid (PA) and diacylglycerol (DAG) derived from said PA within seconds of the primary stimulus and their contact with cells. The modulatory effect depends on the nature of the target cell and the stimulus applied.

Abstract: The invention relates to cyclic imino derivatives of general formula ##STR1## wherein A to G, R.sub.1, Z.sub.1 to Z.sub.6, X and Y are defined as in claim 1, the tautomers, stereoisomers and mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, preferably aggregation-inhibiting properties, pharmaceutical compositions which contain these compounds and processes for preparing them.

Abstract: Compounds of the formula I in the form of the racemates or enantiomers thereof, ##STR1## in which R.sub.1 and R.sub.2 independently of one another are hydrogen or a protective group, and B is a purine or pyrimidine radical or an analogue thereof, can be used as antiviral active ingredients or for the preparation of biologically active oligonucleotides.

Abstract: A compound of formula I ##STR1## wherein R.sub.1 is C.sub.1-4 alkyl, C.sub.3-4 alkenyl or (C.sub.3-5 cycloalkyl)-methyl, R.sub.2 is C.sub.1-4 alkyl, [hydroxy- or (C.sub.1-4 alkoxy)-substituted C.sub.1-3 alkyl]-methyl, (C.sub.3-5 cycloalkyl)-methyl, tetrahydrofuran 2-yl-methyl or 1,3-dioxolan-2-yl-methyl, R.sub.3 and R.sub.4 are each hydrogen, hydroxymethyl, methoxymethyl or N,N-dimethylcarbamoyloxymethyl, R.sub.5 is hydroxy or methoxy, R.sub.6 is hydrogen, hydroxy, methoxy or halogen and R.sub.7 is in the 2- or 3-position and is hydroxy, methoxy or halogen, or together with R.sub.5 is 3,4-methylendioxy, or together with R.sub.6 is 2,3-methylenedioxy and their physiologically-hydrolysable and -acceptable esters are useful in the treatment (symptomatic and prophylactic) of obstructive or inflammatory airways disease, in particular asthma, and disease characterised by or having an aetiology comprising morbid eosinophil accumulation or activation, e.g. hypereosinophilia.

Abstract: Oxazolyl derivatives of formula (I) ##STR1## wherein --A.sup.1 .dbd.A.sup.2 --A.sup.3 .dbd.A.sup.4 -- represents a bivalent radical having the formula--CH.dbd.CH--CH.dbd.CH-- (a-1),--N.dbd.CH--CH.dbd.CH-- (a-2),--CH.dbd.N--CH.dbd.CH-- (a-3),--CH.dbd.CH--N.dbd.CH-- (a-4),--CH.dbd.CH--CH.dbd.N-- (a-5),--N.dbd.CH--N.dbd.CH-- (a-6)or--CH.dbd.N--CH.dbd.N-- (a-7);R represents hydrogen or C.sub.1-4 alkyl; R.sup.1 represents hydrogen, C.sub.1-6 alkyl or hydroxyC.sub.1-6 alkyl; m represents 1 or 2; D represents C.sub.1-4 alkanediyl; B represents NR.sup.2, CH.sub.2, O, S, SO or SO.sub.2 wherein R.sup.2 is hydrogen or C.sub.1-4 alkyl; n represents 0, 1 or 2; L represents hydrogen; C.sub.1-12 alkyl; C.sub.3-6 cycloalkyl; C.sub.3-6 alkenyl optionally substituted with aryl; C.sub.1-6 alkylcarbonyl; C.sub.1-6 alkyloxycarbonyl; arylcarbonyl; arylC.sub.1-6 alkyloxycarbonyl; or a radical of formula --Alk--R.sup.3 (b-1); --Alk--Y--R.sup.4 (b-2); --Alk--Z.sup.1 --C(.dbd.X)--Z.sup.2 --R.sup.5 (b-3); or --CH.sub.2 --CHOH--CH.sub.

Abstract: The present invention relates to labdane-derivatives of the formula ##STR1## a process for their preparation and the use of these substances as medicaments, preferably as medicaments having a positive ionotropic effect, an effect of lowering intraocular pressure and lowing blood pressure.

Abstract: There are disclosed substituted thiophene and furan derivatives of Formula I which are useful as angiotensin II antagonists.

Abstract: A process for preparing 1,3-dipropyl-8-(3-oxocyclopentyl)-xanthine.

Abstract: Sulfonamides of the general formula I ##STR1## where R.sup.1 is hydrogen of C.sub.1 -C.sub.4 -alkyl,R.sup.2 is hydrogen or substituted or unsubstituted C.sub.1 -C.sub.6 -alkyl; C.sub.3 -C.sub.4 -alkenyl; C.sub.3 -C.sub.4 -alkynyl or substituted or unsubstituted saturated or singly unsaturated 5- to 7- membered heteroaryl;R.sup.3 and R.sup.4 are halogen; substituted or unsubstituted C.sub.1 -C.sub.4 -alkoxy C.sub.1 -C.sub.4 -alkylthio, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkenyloxy, C.sub.2 -C.sub.6 -alkenylthio, C.sub.2 -C.sub.6 -alkynyl, C.sub.2 -C.sub.6 -alkynyloxy, C.sub.2 -C.sub.6 -alkynylthio, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -cycloalkylthio, C.sub.5 -C.sub.6 -cycloalkenyl, C.sub.3 -C.sub.6 -cycloalkoxy, C.sub.5 -C.sub.6 -cycloalkenyloxy, C.sub.5 -C.sub.6 -cycloalkenylthio, phenyl, phenoxy, phenylthio, benzyl, benzyloxy or benzylthio;the group given for R.sup.2, or NR.sup.7 R.sup.8, where R.sup.7 and R.sup.8 are hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.

Abstract: The present invention relates to polyoxygenated labdane-derivatives of the formula ##STR1## a process for their preparation and the use of these substances as medicaments, preferably as medicaments having a positive inotropic effect, an effect of lowering intraocular pressure and lowering blood pressure.

Abstract: Disclosed is a hexitol derivative represented by the formula (I): ##STR1## wherein Q represents a formula selected from the group consisting of ##STR2## wherein a represents NH, O or S;each of b, c and d independently represents CH or N;each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, lower alkyl, trifluoromethyl, aryl, lower alkanoyloxy, amino, lower alkylamino, lower alkanoylamino, lower alkanoyl, aroyl, halogen, nitro, (CH.sub.2).sub.m OR.sup. 7, (CH.sub.2).sub.m SR.sup.7, (CH.sub.2).sub.m CO.sub.2 R.sup.7 where R.sup.7 represents hydrogen or lower alkyl and m represents an integer of 0 to 3;each of R.sup.5 and R.sup.6 independently represents hydrogen or lower alkyl;U represents >N-- or ##STR3## W represents a single bond, --O-- or --S--; X represents ##STR4## wherein each of Y.sup.1 and Y.sup.2 independently represents hydrogen, lower alkyl, hydroxyl, lower alkanoyloxy, nitrile or phenyl; or Y.sup.1 and Y.sup.2 are combined together to form oxygen;each of Y.sup.3 and Y.