Abstract: Nonlinear optical compounds which contain a heteroaromatic ring and may further comprise a tricyanovinyl group attached to the heteroaromatic ring.

Abstract: Compounds are provided having structure (I), wherein the L groups are backbone segments, the Y and T groups are functional groups for interacting with target molecules of interest, the X groups are oxygen or sulfur and the E groups are H, conjugate groups or intermediate groups used during the synthesis of the compounds and wherein the compounds are prepared using H phosphonate type chemistry wherein the functional groups are added during an oxidation step or during a coupling step.

Abstract: The invention relates to pyrrolidine monomeric units and to oligomers which are joined via phosphate linkages, including phosphorothioate, phosphodiester and phosphoramidate linkages.

Abstract: The invention provides a cationic polynucleoside chain having multiple nucleosides, the nucleosides being coupled together by positively charged guanidyl linkages.

Abstract: Provided are compounds of the following formulae:A phosphonomethoxymethyoxymethyl purine/pyrimidine derivative of the formula ##STR1## wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroxyalkyl or alkanoyl andB is a purine or pyrimidine base.A 4'-phosphonomethoxytetrahydrofuranyl-1'-purine-pyrimidine of the formula ##STR2## wherein X and X' are the same or different and are hydrogen or alkyl, Y and Z are the same or different and are hydrogen, hydroxyl or alkyl or Y+Z is an alkenyl, an epoxide or cyclopropyl, andB is a purine or pyrimidine base.

Abstract: Provided are compounds of the following formulae:A phosphonomethoxymethyoxymethyl purine/pyrimidine derivative of the formula ##STR1## wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroxyalkyl or alkanoyl andB is a purine or pyrimidine base.A 4'-phosphonomethoxytetrahydrofuranyl-1'-purine-pyrimidine of the formula ##STR2## wherein X and X' are the same or different and are hydrogen or alkyl, Y and Z are the same or different and are hydrogen, hydroxyl or alkyl or Y+Z is an alkenyl, an epoxide or cyclopropyl, andB is a purine or pyrimidine base.

Abstract: In order to produce a purine of the general formula (I), ##STR1## in which R.sup.1 and R.sup.2 can be the same or different and denote H, OH, SH, NH.sub.2, N-(di)-alkyl, halogen, O-alkyl, S-alkyl, alkyl or aryl and alkyl represents an aliphatic residue with 1 to 4 carbon atoms and aryl represents a phenyl residue which is substituted if desired by CH.sub.3, OH, NH.sub.2 or halogen, from the corresponding 4-amino-5-nitrosopyrimidine of formula (II), ##STR2## in which R.sup.1 and R.sup.2 have the above-mentioned meaning, the compound of formula (II) is reductively formylated in a solvent at a temperature of 80.degree. to 220.degree. C. in the presence of formic acid and a catalyst based on a noble metal and the 4-amino-5-formylaminopyrimidine formed as an intermediate is cyclized.

Abstract: Herein is disclosed a novel and industrially advantageous process for synthesizing acyclic nucleosides such as acyclovir and ganciclovir from ribonucleosides, which process comprises adding an acid catalyst and an acid anhydride to a solution of a ribonucleoside such as guanosine and an ester derivative of an acyclic sugar, and heating the mixture, whereby a transglycosilation reaction takes place between the ribose moiety of the ribonucleoside and the ester derivative of the acyclic sugar.Herein is also disclosed an industrially favorable method for the separation of 9-substituted purine nucleosides which are important intermediates for the synthesis of acyclic nucleosides such as acyclovir, ganciclovir, and the like from ribonucleosides, which method comprises crystallizing only the 9-isomer from a solution or suspension containing both a 9-substituted purine nucleoside and a 7-substituted purine nucleoside by cooling the solution or/and by adding a crystallizing solvent thereto.

Abstract: The invention pertains to vitamin D amide derivatives of formula (I). These novel 1.alpha.-hydroxy vitamin D derivatives and their 20-epi analogues comprise compounds of formula (I) and corresponding 5,6-trans isomers, where Y represents an alkylene or alkenylene group containing up to four carbon atoms; R.sup.1 and R.sup.2 independently represent a hydrogen atom or a lower alkyl or cycloalkyl group, or R.sup.1 R.sup.2 N-- represents a heterocyclic group; and R.sup.3 and R.sup.4 independently represent a hydrogen atom or an O-protecting group. Active compounds, in which R.sup.3 and R.sup.4 are hydrogen atoms or metabolically labile O-protecting groups exhibit potent cell modulating effect, but minimal effect on calcium metabolism.

Abstract: Provided are compounds of the following formulae: A phosphonomethoxymethyoxymethyl purine/pyrimidine derivative of the formula ##STR1## wherein X and X' are the same or different and are hydrogen or alkyl. R and R' are the same or different and are hydrogen, alkyl, hydroxyalkyl or alkanoyl andB is a purine or pyrimidine base.A compound of formula (VI) ##STR2## wherein X is halogen, Y is S-phenyl, Se-phenyl or halogen and B is hypoxanthine, xanthine, guanine, 8-bromoguanine, 8-chloroguanine, 8-methylguanine, 8-thioguanine, 3-deazaguanine, purine, 2-aminopurine, 2,6-diaminopurine, adenine, 3-deazaadenine, 8-aminoguanine, 8-hydrazinoguanine, 8-hydroxyguanine, cytosine, 5-ethylcytosine, 5-methylcytosine, thymine, uracil, 5-chlorouracil, 5-bromouracil, 5-ethyluracil, 5-iodouracil, 5-propyluracil or 5-vinyluracil, 2-acetamido-6-diphenylcarbamoylpurine, 6-N-dimethylamino-methyladenine or 6-N-pivaloyladenine.

Abstract: An improved method for the preparation of acyclic nucleotide analogues comprises first condensing a cyclic carbonate with a purine or pyrimidine base and then reacting the alkylated base with an activated phosphonate. Novel cyclic carbonates are employed to yield the desired phosphonylmethoxyalkyl nucleotide analogues.

Abstract: Carboxy-peptidyl compounds of Formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophobic epidermolysis bullosa, coronary thrombosis associated with atherosclerotic plaque rupture, and aneurysmal aortic disease. This invention relates to a process of making the carboxy-peptidyl compounds of formula I.

Abstract: This invention is directed to novel purine-based compounds for inclusion into oligonucleotides. The compounds of the invention, when incorporated into oligonucleotides are especially useful as "antisense" agents--agents that are capable of specific hybridization with a nucleotide sequence of an RNA. The compounds of the invention may also be used for cross-linking oligonucleotides. Oligonucleotides are used for a variety of therapeutic and diagnostic purposes, such as treating diseases, regulating gene expression in experimental systems, assaying for RNA and for RNA products through the employment of antisense interactions with such RNA, diagnosing diseases, modulating the production of proteins, and cleaving RNA in site specific fashions. The compounds of the invention include novel heterocyclic bases, nucleosides, and nucleotides. When incorporated into oligonucleotides, the compounds of the invention can be useful for modulating the activity of RNA.

Abstract: This invention relates to adenosine kinase inhibitors and to nucleoside analogs, C-4' modified pyrrolo?2,3-d!pyrimidine and pyrazolo?3,4-d!pyrimidine nucleoside analogs having activity as adenosine kinase inhibitors. The invention relates to nucleoside analogs of this kind, having zero substitutions or two substitutions at the C-4' position of the furanose (sugar) moiety. The invention also relates to the preparation and use of these adenosine kinase inhibitors in the treatment of cardiovascular, and cerebrovascular diseases, inflammation and other diseases which can be regulated by increasing the local concentration of adenosine.

Abstract: Novel Carboxy-peptidyl compounds of Formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophobic epidermolysis bullosa, coronary thrombosis associated with atherosclerotic plaque rupture, and aneurysmal aortic disease. The matrix metalloendoproteinases are a family of zinc-containing proteinases including but not limited to stromelysin, collagenase, and gelatinase, that are capable of degrading the major components of articular cartilage and basement membranes. The inhibitors claimed herein may also be useful in preventing the pathological sequelae following a traumatic injury that could lead to a permanent disability. These compounds may also have utility as a means for birth control by preventing ovulation or implantation.

Abstract: Nucleotide analogs characterized by the presence of an amidate linked amino acid or an ester linked group which is bonded to the phosphorus atom of phosphonate nucleotide analogs are disclosed. The analogs comprise a phosphoamidate or ester bond that is hydrolyzed in vivo to yield a corresponding phosphonate nucleotide analog. Methods and intermediates for their synthesis and use are described.

Abstract: There are disclosed compounds of formula I, ##STR1## wherein Q represents CR.sup.1 R.sup.2,R represents O or CR.sup.3 R.sup.4,W represents O or CH.sub.2,R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen or halogen,X represents S(O).sub.n R.sup.5, alkyl C.sub.1-6 alkoxy C.sub.1-6, acylamino C.sub.1-6, CONR.sup.6 R.sup.7, NR.sup.8 R.sup.9, halogen, a 5- or 6-membered S containing heterocycle, or phenyl optionally substituted by alkyl C.sub.1-6,n represents 0, 1 or 2,R.sup.5 represents aryl or alkyl C.sub.1-6 optionally substituted by one or more substituents selected from hydroxy, alkoxy C.sub.1-6, halogen and aryl;R.sup.6, R.sup.7, R.sup.8 and R.sup.9 independently represent hydrogen or alkyl C.sub.1-6,Y represents NH.sub.2 or alkoxy C.sub.1-6, andZ represents an acidic moiety,in addition, when R represents CR.sup.3 R.sup.4, then --Q--Z may also represent hydroxy or --OP(O)(OH).sub.2,and pharmaceutically acceptable salts thereof, with certain provisos, for use as pharmaceuticals.

Abstract: Typical treatment of psoriasis and other diseases of skin cell hyperproliferation using pharmaceutical compositions containing mono-, di, and tri-phosphate esters of antiproliferative nucleoside analogs and related analogs, DNA chain-terminating dideoxynucleosides and other nucleoside analogs. The useful phosphate esters include phosphoramidates and phosphothiorates, as well as polyphosphates having C and S bridging atoms.

Abstract: The present invention is directed to improved methods to synthesize oligonucleotide analogs having an acetal linkage, such as a 3',5'-formacetal (3' --O--CH.sub.2 --O-- 5'), 3',5'-thioformacetal (3' --S--CH.sub.2 --O-- 5') or an analogous 2',5' linkage between adjacent nucleoside analog residues. Compositions comprising 5', 3' and 2' phosphinate nucleoside analogs useful in the methods are also provided.

Abstract: The present invention relates to certain purine nucleoside analogues containing a carbocyclic ring in place of the sugar residue, salts, esters and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical formulations containing them and to the use of such compounds in therapy, particularly the treatment or prophylaxis of certain vital infections.

Abstract: Compounds are provided having the structure: ##STR1## wherein the L groups are spanner or linker units, the Y and T group are functional groups for interacting with target molecules of interest, the X groups are oxygen or sulfur and the E groups are H, conjugate groups or intermediate groups used during the synthesis of the compounds are prepared using H phosphonate type chemistry wherein the functional groups are added during an oxidization step.

Abstract: Cycloalkyltriols containing heterocyclic substituents, in particular cyclopentyl- and cyclohexyltriols containing heterocyclic substituentsCompounds of the formulae I and II ##STR1## in which the substituents A, R.sup.1, R.sup.2 and R.sup.3 and n have the meanings given, have an antiviral and antiparasitic action.

Abstract: A therapeutic method is provided, employing an antiviral compound of the general formula: ##STR1## wherein Z is H, OR' or N(R).sub.2, wherein R' is H, (C.sub.1 -C.sub.4)alkyl, aryl, CHO, (C.sub.1 -C.sub.16)alkanoyl or O.dbd.P(OH).sub.2, Y is CH or N, and X is selected from the group consisting of H, N(R).sub.2, SR, OR' or halogen, wherein R is H, lower(C.sub.1 -C.sub.4)alkyl, aryl or mixtures thereof, and the pharmaceutically acceptable salts thereof.

Abstract: Conformationally locked 4',6'-cyclopropane-fused carbocyclic nucleoside analogues. The compounds are prepared by condensing a cyclopropane-fused carbocyclic allylic alcohol with substituted purine or pyrimidine bases. The condensation products are then modified to produce the adenosine, guanosine, cytidine, thymidine and uracil nucleoside analogues. The compounds are therapeutically useful as antimetabolites, or in the preparation of anti-metabolic agents.

Abstract: Derivatives of Acyclovir are provided having patent antiviral inhibitory activity. Phosphotriester derviatives are preferred which have the structure: ##STR1## where R is alkyl, especially CH.sub.3 or (CH.sub.3).sub.3 C.

Abstract: The invention relates to nucleic acid-binding oligomers possessing N-branching of the general formula (I), ##STR1## and their monomers, where the individual radicals have the meaning given in the description, and to their use as medicaments or as aids in diagnostics.

Abstract: Substituted pyridines and pyrimidines, processes for their preparation and their use as pesticides and fungicides.The invention relates to compounds of the formula ##STR1## in which A is N or CH, R is H, halogen, alkyl or cycloalkyl, R.sup.2 and R.sup.3 are H, halogen or an aliphatic radical or together form a ring, X is O, NH Or S(O).sub.q where q=0, 1 or 2, R.sup.4.sub.q is 0-4 radicals selected from the series consisting of halogen, optionally substituted alkyl or alkoxy, cycloalkyl and optionally substituted phenyl, n=0-2, m=1-3 and Y is optionally substituted methylene or imino.The invention furthermore relates to a process for their preparation and for their use as pesticides, in particular as insecticides, acaricides and fungicides. The compounds are furthermore suitable for controlling nematodes, helminths and molluscs, and for controlling endoparasites and ectoparasites in the field of veterinary medicine.

Abstract: Disclosed herein are angiotensin-II antagonists of the formula ##STR1## wherein R.sub.1 is, other than hydrogen and, inter alia, halogen, lower alkyl or cycloalkyl; R.sub.2 is, inter alia, optionally substituted benzimidazol-2-yl, 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-yl, butanesultam-1-yl, imidazol-4-yl, and tetrahydobenzimidazol-2-yl; R.sub.3 is, inter alia, lower alkyl; and, R.sub.4 is an acidic group, such as carboxyl or tetrazolyl.An exemplary compound is:(a) 4'-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazole-2-yl)-benzimidazol-1-yl] methyl]-biphenyl-2-carboxylic acid.

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: Compounds of the Formula ##STR1## wherein: K is N or N.fwdarw.O; Q is CH.sub.2 or O; T is ##STR2## or R.sub.3 O--CH.sub.2 ; X is a straight or branched chain alkylene, cycloalkylene or cycloalkenylene group, each of which is optionally substituted by at least one CH.sub.3, CH.sub.3 CH.sub.2, Cl, F, CF.sub.3 or CH.sub.3 O; Y is NR.sub.4, O or S; a=0 or 1; Z is of the formula ##STR3## Z.sub.1 is N, CR.sub.5, (CH).sub.m --CR.sub.5 or (CH).sub.m --N, m being 1 or 2; Z.sub.2 is N, NR.sub.6, O or S, n being 0 or 1; R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are independently H, alkyl, aryl or heterocyclyl; R.sub.a and R.sub.

Abstract: This invention relates to novel purine nucleoside phosphorylase inhibitors, to the methods and intermediates for their preparation and to their use as immuno-suppressants, antilymphoma, antileukemic, antiviral and antiprotozoal agents.

Abstract: A novel class of compounds, known as peptide nucleic acids, bind complementary ssDNA and RNA strands more strongly than a corresponding DNA. The peptide nucleic acids generally comprise ligands such as naturally occurring DNA bases attached to a peptide backbone through a suitable linker.

Abstract: This invention relates to novel purine nucleoside phosphorylase inhibitors, to the methods and intermediates for their preparation and to their use as immuno-suppressants, antilymphoma, antileukemic, antiviral and antiprotozoal agents.

Abstract: Novel pyrrolidine monomers bearing various functional groups are used to prepare oligomeric structures. The pyrrolidine monomers can be joined via standard phosphate linkages including phosphodiester and phosphorothioate linkages. Useful functional groups include nucleobases as well as polar groups, hydrophobic groups, ionic groups, aromatic groups and/or groups that participate in hydrogen-bonding.

Abstract: The protected cyclobutanone of the formula ##STR1## is treated with a dialkylaluminum chloride, an alkylaluminum dichloride, a trialkylaluminum compound, hydrogen in the presence of the catalysts ruthenium black or ruthenium on alumina, diphenyl-silane in the presence of tris(triphenylphosphine) rhodium (I) chloride, or iridium tetrachloride to yield the corresponding diprotected cyclobutanol. This compound is useful as an intermediate in the preparation of antiviral agents.

Abstract: An improved method for the preparation of acyclic nucleotide analogues comprises first condensing a cyclic carbonate with a purine or pyrimidine base and then reacting the alkylated base with an activated phosphonate. Novel cyclic carbonates are employed to yield the desired phosphonylmethoxyalkyl nucleotide analogues.

Abstract: Described are delta 17 and delta 20 olefinic and saturated 17 Beta-substituted 4-aza-5 alpha-androstan-3-ones and related compounds having 5 alpha reductase inhibitors for treatment of benign prostatic hyperplasia and other hyperandrogenic related disorders.

Abstract: Benzopyran derivatives which have an inhibitory effect on the Maillard reaction as well as an antioxidizing effect are described herein. These derivatives may be utilized in the treatment and/or prevention of diabetic complications such as, for example, coronary heart disease, peripheral circulatory insufficiency or failure, cerebrovascular hindrance, neurogenous diabetes, nephropathy, arteriosclerosis, arthrosclerosis, cataracts and retinopathy. Further, the derivatives may also be used in the treatment and/or prevention of diseases induced by aging and in the treatment and/or prevention of diseases caused by the formation of peroxidized fat.

Abstract: Novel bicyclic pyrimidine compounds for use as drugs and having formula (I). Said novel compounds and physiologically tolerable salts thereof may be used in therapeutics, particularly for suppressing tumour cell resistance to antineoplastic agents.

Abstract: Novel lyxose derivatives which selectively inhibit adenosine kinase and methods of preparing these compounds are provided. These compounds are useful in treating certain conditions in vivo which may be ameliorated by increased local concentrations of adenosine.

Abstract: Compounds of formula I, and pharmaceutically acceptable salts thereof, ##STR1## in which R1 is hydrogen (1-6C)alkyl or (1-4C)alkanoyl; A is --N.dbd.CQ--O--, N.dbd.CQ--NR.sup.8 --, --N.dbd.CQ--CH.dbd.N--or --N.dbd.CH--CQ.dbd.N--;Q is 2--furyl;R.sup.8 is hydrogen or C1-4C)alkyl;and R.sup.2 has any of the meanings given in the specification, processes for preparing the compounds and pharmaceutical compositions containing them. The compounds are useful as adenosine antagonists.

Abstract: This invention discloses various analogs of erythro-hydroxynonyladenine (EHNA) which have been modified by the addition of hydroxy groups or other moieties at the #8 or #9 carbon atoms of the side-chain portion of the molecule (i.e., the erythro-hydroxynonyl chain which is attached to the adenosine ring structure). It also discloses synthetic reagents and steps that can be used to create these and other analogs of EHNA which contain hydroxyl, halide, acid, ester, ether, amine, azide, or other moieties at such locations, or at other controllable locations such as the #5, #6, or #7 carbon atoms on the side-chain. Analogs containing such side-chain modifications can also be modified in the adenosine structure if desired. The hydroxylated analogs described herein have been shown to inhibit adenosine deaminase (ADA) at therapeutically useful levels. The relevant Ki values are in the range of 10.sup.-8 to 10.sup.-9, which is within a desired range of about 10.sup.-7 to about 10.sup.-10.

Abstract: An insecticidal composition containing a guanidine derivative of the formula: ##STR1## wherein R.sup.1 is an optionally substituted homocyclic or heterocyclic group, n is 0 or 1, R.sup.2 is a hydrogen atom or an optionally substituted hydrocarbon group, R.sup.3 is a primary, secondary or tertiary amino group, X is an electron attractive group such as nitro or trifluoroacetyl group, provided that when n is 0, R.sup.1 is an optionally substituted heterocyclic group or a salt thereof.

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: 2',3'-dideoxy-4'-thioribonucleosides useful as antiviral agents in the treatment and prevention of AIDS are disclosed. In accordance with one aspect of the invention there are provided compounds of the formula ##STR1## where X.dbd.H, N.sub.3 or F, and B is a member selected from the group consisting of pyrimidine, 5-azapyrimidine, 6-azapyrimidine, 3-deazapyrimidine, purine, 3-deazapurine, 7-deazapurine, 8-azapurine, and 2-azapurine bases. The intermediate 1-O-acetyl-5-O-t-butyldiphenylsilyl-4-thio-2,3-dideoxyribofuranose is useful in the production of certain of the 2',3'-dideoxy-4'-thioribonucleosides. Other intermediates include the 4-thio-2,3-dideoxyribofuranose having different hydroxyl protecting groups and leaving groups.

Abstract: This invention relates to pyrazolo pyrimidines for the treatment of atherosclerosis as inhibitors of acyl--CoA, cholesterol acyetransferase (ACAT), and their use as antihypercholesterolemic agents, pharmaceutical compositions and preparation, and having the formula (I): ##STR1## wherein: A and Q are selected independently from CH or N with no more than two nitrogens per ring:D, E, and G are selected independently from CR.sup.1 or N with no more than two nitrogens per ring;X is S(O).sub.r, O, NR.sup.4 or CH.sup.2 ;J is C.sub.2 -C.sub.10 alkyl, C.sub.3 -C.sub.10 branched alkyl, C.sub.3 -C.sub.10 alkenyl or C.sub.3 -C.sub.10 alkynyl;Y is O, S, H.sub.2 or NH:Z is NHR.sup.3, OR.sup.3 or R.sup.3 :R.sup.1 is selected independently from H, NO.sub.2, Br, Cl, F, CF.sub.3, CN, CH.sub.3 S(O).sub.r, C.sub.1 -C.sub.8 alkyl or alloxy, C.sub.3 -C.sub.8, branched alkyl, C.sub.1 -C.sub.4 carboalkoxy, NR.sup.5 R.sup.6 or NR.sup.5 COR.sup.6 ;R.sup.2 is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 branched alkyl, C.sub.3 -C.sub.

Abstract: A phenylalanine-glycine derivative of the general formula (I): ##STR1## wherein R represents a residue of an antitumor substance, or a salt or ester thereof, a process for preparation thereof, and a pharmaceutical composition containing the same are described.The novel conjugate of the phenylalanine-glycine derivative and the antitumor substance exhibits superior antitumor activity in comparison with the case wherein an antitumor substance is administered singly or as a mixture with phenylalanine.

Abstract: A composition of polymer molecules effective to bind, with substantially uniform binding affinity, to a single-stranded polynucleotide containing a target sequence of bases. The polymer molecules are composed of a sequence of base-pairing moieties effective to hydrogen bond to corresponding, complementary bases in the target sequence, under selected binding conditions, and a predominantly uncharged, achiral backbone supporting the base-pairing moieties at positions and in orientations which allow hydrogen bonding between the pairing moieties of the polymer and the corresponding complementary bases in the target sequence. The composition has diagnostic uses, in a solid-support assay system, and therapeutic uses involving inhibition or inactivation of target polynucleotides.

Abstract: The present invention relates to a method of effecting immunosuppression in a patient in need thereof comprising administering to said patient an effective immunosuppressive amount of certain 5'-vinylhalo-aristeromycin/adenosine analogs.

Abstract: Disclosed are processes for preparing compounds of the formula (I) and pharmaceutically acceptable salts or esters thereof: ##STR1## wherein R.sub.2 is a purine or pyrimidine base or an analogue or derivative thereof; and Z is S, S.dbd.O or SO.sub.2. The invention also relates to intermediates of use in the preparation of these compounds.