Heterocyclic Compounds

Matches 351 - 400 out of 970	< 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 >

Document	Document Title
WO/1996/023509A1	COMBINATION THERAPY FOR HIV INFECTION USING THE HIV PROTEASE INHIBITOR INDINAVIR ADN THE REVERSE TRANSCRIPTASE INHIBITOR 3TC, OPTIONALLY TOGETHER WITH AZT, DDI OR DDC The combination of the HIV protease inhibitor Compound J, 3TC, and, optionally AZT, ddI, or ddC, is useful in the inhibition of HIV protease, the inhibition of HIV reverse transcriptase, the prevention or treatment of infection by HIV an...
WO/1996/022978A1	SUBSTITUTED PHENYL COMPOUNDS AS ENDOTHELIN ANTAGONISTS Compounds of formula (I) are described, wherein: R1 is CN, CH2CN, CH=CHCN, CHO, or CH=CHCO2H; R2 is aryl lower alkoxy, heteroaryl lower alkoxy, aryl lower alkylthio or heteroaryl lower alkylthio in which each of the aryl and heteroaryl m...
WO/1996/021646A1	SUBSTITUTED 2-PHENYLPYRIDINES AS HERBICIDES The invention concerns substituted 2-phenylpyridines of formula (I), in which: n = 0, 1; R1, R3 and R4 represent H, OH, SH, NO2, NH2, CN, COOH, CONH2, halogen, alkyl, alkyl halide, alkoxy, alkoxy halide, alkyl amino, dialkyl amino, alkyl...
WO/1996/018643A1	TACHYKININ ANTAGONISTS Compounds of formula (I), wherein R1 is mono- or di-substituted phenyl, n is zero or 1, X1 is oxygen, sulfur or =NCN, X2 and X3 are oxygen or sulfur, R2 is hydrogen or methyl, R3 is phenyl, halo-substituted phenyl, 2-naphthyl, IH-indol-3...
WO/1996/016045A1	DERIVATIVES OF 'alpha'-HALOGEN CARBONYL COMPOUNDS, PROCESS AND INTERMEDIATE PRODUCTS FOR PREPARING THE SAME 'alpha'-halogen carbonyl derivatives have the general formula (I), in which R is a formyl group, a CO2H group or a rest capable of being hydrolysed into COOH and the other substituents have the following meanings: R2 stands for halogen, ...
WO/1996/015109A1	ENDOTHELIN ANTAGONISTS A compound of formula (I), in which: R1 is lower alkyl, cyclo(lower)alkyl, optionally substituted aryl, optionally substituted heterocyclic group, cyclo(lower)alkyl(lower)alkyl, or ar(lower)alkyl; R2 is hydrogen, hydroxy or protected hyd...
WO/1996/012716A1	NUCLEOSIDE DERIVATIVES AND PROCESS FOR PREPARING THEREOF According to the present invention, nucleoside derivatives represented by formula (I), wherein: R1 represents hydrogen, phosphate or phosphonate group, R2 represents substituted or unsubstituted pyrimidine or purine base, and Z represent...
WO/1996/009303A1	SUBSTITUTED PYRAZOLYL-PYRAZOLE DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND THEIR USE AS AGENTS WITH HERBICIDAL ACTION The invention relates to new substituted pyrazol derivatives of general formula (I) in which: R1, R2, R3, R4, R5 and R6 have the meanings given in the description, agents with herbicidal action containing at least one compound of formula...
WO/1995/035283A1	TRI-SUBSTITUTED PHENYL DERIVATIVES USEFUL AS PDE IV INHIBITORS Compounds of general formula (1) are described, formula wherein =W- is (1) =C(Y)- where Y is a halogen atom, or an alkyl or -XRa group where X is -O-, -S(O)m- [where m is zero or an integer of value 1 or 2], or -N(Rb)- [where Rb is a hyd...
WO/1995/032188A1	SUBSTITUTED 3-PHENYLPYRAZOLES FOR USE AS HERBICIDES Substituted 3-phenylpyrazoles of formula (I), where R1 is H, or a substituent; R2 is CN, CF3, halogen; R3 is H, alkyl, halogenalkyl; R4 is C1-C4 alkyl, C1-C4 halogenalkyl; R5 is H, NO2, halogen, -COOR, optionally substituted aminocarbony...
WO/1995/032200A1	OXATHIOLANES, METHOD FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME The present invention pertains to the field of organic chemistry, and particularly therapeutic chemistry. The invention provides cis-form 5-(cytosinyl-1) 1,3-oxathiolanes of general formula (I), wherein R is an acyl or aralkoyl radical, ...
WO/1995/029174A1	PROCESS FOR THE DIASTEREOSELECTIVE SYNTHESIS OF NUCLEOSIDE ANALOGUES A diastereoselective process for the preparation of compounds of formula (I), wherein W is S, S=O, SO2, or O; X is S, S=O, SO2, or O; R1 is hydrogen or acyl, and R2 is a purine or pyrimidine base or an analogue or derivative thereof, is ...
WO/1995/029176A1	SUBSTITUTED 1,3-OXATHIOLANES WITH ANTIVIRAL PROPERTIES This invention relates to single enantiomers of novel cis-substituted 1,3-oxathiolanes, of formula (I) wherein R1 is hydrogen, and R2 is cytosine or 5-fluorocytosine, and pharmaceutically acceptable salts and esters thereof. This inventi...
WO/1995/018804A1	WATER SOLUBLE ONIUM SALT OF TAXO-DITERPENOID Onium salts of taxo-diterpenoid-Cn, 2-0-aza-arenes are employed as water soluble prodrugs. For example, taxol-2'-methylpyridinium tosylate (MPT) is characterized by an elevated aqueous solubility, rapid activation by serum protein, good ...
WO/1995/018613A1	SELF-ASSEMBLED TAXO-DIPERPENOID NANOSTRUCTURES Onium salts of taxo-diterpenoid-Cn,2-O-aza-arenes form water soluble self-assembling nanostructures above a critical aggregation concentration. The onium salt of aza-arene includes a delocalized charge which renders derivatized taxo-dite...
WO/1995/015958A1	COMPOUNDS HAVING BOTH POTENT CALCIUM ANTAGONIST AND ANTIOXIDANT ACTIVITY AND USE THEREOF AS CYTOPROTECTIVE AGENTS Compounds having both calcium antagonist and antioxidant activity are disclosed. The compounds are useful in preventing or alleviating damage to tissues at the cellular level. Methods of treatment which employ these properties of the com...
WO/1995/006641A1	SUBSTITUTED 1-AMINO-3-PHENYLURACILS WITH HERBICIDAL ACTIVITIES Substituted 1-amino-3-phenyluracils (I), where the variables have the following meanings: R1 = H, F, Cl; Y = O, S; W = -CH=N-OH, -CH=N-O-(alkyl), -CH=N-O-(alkylene)-O-(alkyl), -CH=N-O-CH2-COOH, -CH=N-O-CH(alkyl)-COOH, -CH=N-O-CH2-CO-O-(a...
WO/1995/005366A1	VASOCONSTRICTIVE SUBSTITUTED ARYLOXYALKYL DIAMINES The present invention is concerned with compounds having formula (I), the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein R1 is hydrogen or C1-6alkyl; R2 is hydrogen or C1...
WO/1994/029301A1	STEREOSELECTIVE SYNTHESIS OF NUCLEOSIDE ANALOGUES USING BICYCLIC INTERMEDIATE The present invention relates to a process for producing predominantly pure cis nucleoside analogues using a novel bicyclic intermediate of formula (III), wherein X is S, or O; Y is S, CH2, O or CH(R); wherein R is azido or halogen; and ...
WO/1994/025442A1	3-(HETERO)ARYL CARBOXYLIC ACID DERIVATIVES, METHODS OF PREPARING THEM AND INTERMEDIATES USED IN THEIR PREPARATION The invention concerns 3-(Hetero)aryl carboxylic acid derivatives of formula (I) in which R is a formyl group, a CO2H group or a group which can be hydrolysed to give a COOH group and the other substituents are as follows: R2 and R3 are ...
WO/1994/019344A1	AMIDE COMPOUNDS WITH PHARMACOLOGICAL ACTIVITY Compounds of formula X-NH-CO-Z and pharmaceutically acceptable salts thereof, and the use of a compound of said formula or a pharmaceutically salt thereof, wherein X is a monocyclic or polycyclic aromatic group, Z is of sub-formula (h), ...
WO/1994/018193A1	NOVEL HETEROCYCLIC AMINOMETHYL-4 PIPERIDINE DERIVATIVES, THEIR PREPARATION AND APPLICATION IN THERAPY Heterocyclic aminomethyl-4 piperidine derivatives corresponding to general formula (1), and the therapeutically acceptable salts of these molecules. The invention also concerns the use of compounds of general formula (1) in therapy and p...
WO/1994/014802A1	PROCESS FOR PREPARING SUBSTITUTED 1,3-OXATHIOLANES WITH ANTIVIRAL PROPERTIES Disclosed are processes for preparing compounds of formula (I) and pharmaceutically acceptable salts or esters thereof, wherein R2 is a purine or pyrimidine base or an analogue or derivative thereof; and Z is S, S = O or SO2. The inventi...
WO/1994/013676A1	PYRROLOPYRIMIDINES AS CRF ANTAGONISTS The compounds of formula (I), wherein B, R3, R4, R5 and R6 are as defined herein, are useful in the treatment of stress-related and other diseases. These compounds have corticotropin-releasing factor antagonist activity and as such are o...
WO/1994/009793A1	ENANTIOMERICALLY PURE beta-D-DIOXOLANE NUCLEOSIDES WITH SELECTIVE ANTI-HEPATITIS B VIRUS ACTIVITY The invention is a method for the treatment of humans infected with HBV that includes administering an HBV treatment amount of an enatiomerically pure beta-D-dioxolanyl purine nucleoside of formula (I), wherein R is OH, Cl, NH2 or H, and...
WO/1994/008992A1	HETEROCYCLIC ETHER COMPOUNDS THAT ENHANCE COGNITIVE FUNCTION Novel heterocyclic ether compounds of formula (I), wherein A, B and R2 are specifically defined, or pharmaceutically-acceptable salts or prodrugs thereof, which are selective and potent ligands at cholinergic channel receptors, useful in...
WO/1994/004154A1	ENANTIOMERICALLY PURE beta-D-DIOXOLANE-NUCLEOSIDES A method and composition for the treatment of humans infected with HIV that includes the administration of an HIV treatment amount of an enantiomerically pure beta-D-dioxolanyl purine nucleoside of formula (I), wherein R is OH, Cl, NH2, ...
WO/1994/001415A1	CONDENSED HETEROCYCLIC DERIVATIVE AND WEEDKILLER A condensed heterocyclic derivative represented by general formula (I) and a weedkiller, wherein R represents hydroxy, R3 and R4 represent each alkoxy, W represents oxygen, Yn represents hydrogen, Z represents methine, and A represents a...
WO/1993/024482A1	HETEROCYCLICALLY BISUBSTITUTED SULPHONYL AMINO(THIO)CARBONYL COMPOUNDS, The invention relates to novel heterocyclically bisubstituted sulphonyl amino(thio)carbonyl compounds of formula (I) in which Q is oxygen or sulphur, R?1¿ and R?2¿ are the same or different and mutually independently stand for a possib...
WO/1993/017028A1	SENSITIZING AGENTS FOR USE IN BORON NEUTRON CAPTURE THERAPY Compounds of formula (I) and (II) in which B contains a carboranyl group and one of R3 and R4 is a carboranyl group or a boronic acid or ester are useful sensitizing agents for boron neutron capture therapy.
WO/1993/016800A1	CATALYTIC SOLUTION A catalyst solution comprising one or more compounds of a metal catalyst and an organic solvent selected from the group consisting of a glycol derivative, an alkyl pyrrolidone, and an alkoxy ethyl ether, wherein no additional chloride co...
WO/1993/011122A1	PIPERAZINE DERIVATIVES AS 5-HT1A ANTAGONISTS Compounds of formula (I) where A is a C1 or C2 alkylene chain optionally substituted by lower alkyl, Z is a bicyclic oxygen-containing radical (e.g. 2,3-dihydro-1,4-benzodioxin-5-yl), R is hydrogen or lower alkyl, R1 is aryl or aryl(lowe...
WO/1993/004057A2	HERBICIDES CONTAINING 3-AMINOBENZO[B]THIOPHENES AS AN ANTIDOTE Disclosed are herbicides containing at least one 3-aminobenzo[b]thiophene (I) with an antagonistic action (in which R?1¿ = -COX or -COOX; X = H, halogen, optionally substituted amino, optionally substituted C¿1?-C¿10? alkyl, optionall...
WO/1993/003726A1	MUSCARINIC AGONISTS Substituted 1,4,5,6-tetrahydropyrimidine compositions, substituted 1,2,3,6-tetrahydropyrimidine compositions and substituted 3,4,5,6-tetrahydropyrimidine compositions are disclosed. They are useful for stimulating muscarinic receptors in...
WO/1993/003020A1	HERBICIDAL QUINOXALINYLOXY ETHERS This invention relates to certain herbicidal quinoxalinyloxy compositions and a method for their use as a general herbicide or as a selective preemergent or postemergent herbicides for controlling the growth of undesired vegetation in cr...
WO/1993/003027A1	1,3-OXATHIOLANE NUCLEOSIDE ANALOGUES The invention relates to 1,3-oxathiolane nucleoside analogues and their use in the treatment of viral infections. More specifically, this invention relates to (-)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl) -(1H)-pyrimidin-2...
WO/1992/022546A1	SUBSTITUTED 1,5-DIHYDRO-3H-2,4-BENZODIOXEPINES AS OPTICALLY ACTIVE GLYDERALDEHYDES OR GLYCIDALDEHYDES Stable, optically active enantiomers of substituted glyceraldehydes or glycidaldehydes are synthesized by using osmium-catalyzed asymmetric dihydroxylation of an olefin which is a substituted 1,5-dihydro-3H-2,4-benzodioxepine. For exampl...
WO/1992/021674A1	CYCLIC ALKYLIDENE SUBSTITUTED PYRIDINE HERBICIDES Fully substituted pyridines having a cyclic alkylidene substituent, useful as herbicides, compositions and methods of use thereof.
WO/1992/021676A1	CRYSTALLINE OXATHIOLANE DERIVATIVES (-)cis-4-Amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(IH)- pyrimidine-2-one in crystalline form, in particular as needle-shaped or bipyramidyl crystals, pharmaceutical formulations thereof, methods for their preparation and their use i...
WO/1992/020669A1	PROCESSES FOR THE DIASTEREOSELECTIVE SYNTHESIS OF NUCLEOSIDES The present invention relates to highly diastereoselective processes for production of cis-nucleosides and nucleoside analogues and derivatives in high optical purity and intermediates useful in those processes.
WO/1992/020696A1	PROCESSES FOR THE DIASTEREOSELECTIVE SYNTHESIS OF NUCLEOSIDES The present invention relates to highly diastereoselective processes for production of cis-nucleosides and nucleoside analogues and derivatives in high optical purity and intermediates useful in those processes.
WO/1992/020344A1	ANTIVIRAL COMBINATIONS CONTAINING NUCLEOSIDE ANALOGS Combinations comprising a compound of formula (I) or a pharmaceutically acceptable derivative thereof and an inhibitor of HIV replication, pharmaceutical formulations thereof and their use in the treatment of HIV infections.
WO/1992/019246A1	USE OF A 1,3-OXATHIOLAN DERIVATIVE FOR THE TREATMENT OF HEPATITIS B INFECTION The use of a 1,3-oxathiolane nucleoside analogue and pharmaceutically acceptable derivatives thereof for the treatment of hepatitis B virus infections is disclosed. Pharmaceutical formulations are also provided.
WO/1992/018517A1	METHOD OF TREATING OR PREVENTING HEPATITIS B VIRUS Anti-hepatitis B virus compounds (-)3'-thia-2',3'-dideoxycytidine, (-)5-fluoro-3'-thia-2',3'-dideoxycytidine, (�) $g(b)-dioxolane cytosine and (-)-L-$g(b)-dioxolane cytosine. A method of treating a patient suffering from hepatitis B vi...
WO/1992/018475A2	NEW CENTRALLY ACTING SUBSTITUTED PHENYLAZACYCLOALKANES A compound of formula (I), or a pharmaceutically acceptable salt thereof wherein n is 0-3; R1 and R2 are independently H (provided only one is H at the same time), -OH (provided R4 is other than hydrogen), CN, CH2CN, 2- or 4-CF3, CH2CF3,...
WO/1992/015568A1	BENZENESULFONYLUREA DERIVATIVES The present invention relates to novel benzenesulfonylurea derivatives, having a herbicidal activity, which is described in the structure of general formula (I), wherein R1 is H, C1-C3 alkyl, C1-C3 haloalkyl, halogen, CN, NO2, C1-C3 alko...
WO/1992/015309A1	ANTIVIRAL NUCLEOSIDE COMBINATION Synergistic combinations of nucleoside derivatives, pharmaceutical formulations containing said combinations and use of the combinations in the treatment of retroviral infections are disclosed.
WO/1992/015308A1	USE OF 5-FLUORO-2'-DEOXY-3'-THIACYTIDINE FOR THE TREATMENT OF HEPATITIS B The use of a 1,3-oxathiolane nucleoside analogue and pharmaceutically acceptable derivatives thereof for the treatment of hepatitis B virus infections is disclosed. Pharmaceutical formulations are also provided.
WO/1992/014711A1	SUBSTITUTED PYRIDINE COMPOUNDS Disclosed herein are herbicidal pyridine compounds substituted at the 2- or 6-position with an OR2 moiety where R2 is hydrogen, lower alkyl, halomethyl, lower cyanoalkyl, alkenyl or alkynyl, as well as herbicidal compositions and herbici...
WO/1992/014729A1	ANTIVIRAL 1,3-DIOXOLANE NUCLEOSIDES AND SYNTHESIS THEREOF A synthesis of 1,3-dioxolane nucleosides that includes condensing a 2-O-protected-5-O-acylated-1,3-dioxolane with a purine or pyrimidine base in the presence of a titanium containing Lewis acid to provide predominately the desired $g(b)-...

Matches 351 - 400 out of 970	< 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 >