Abstract: Apomorphine derivative compounds; pharmaceutically active compositions of apomorphine derivative compounds; and the use of apomorphine derivative compounds in methods for treating sexual dysfunction or for enhancing apomorphine effectiveness for patients treated with apomorphine are disclosed. The apomorphine derivatives may be esters, ethers, amides, mixed anhydrides, hemiacetals, glucuronates, sulfates or phosphonates. A preferred apomorphine derivative is norapomorphine.

Abstract: Synthetic processes and intermediates are disclosed for the preparation of N-arylacridancarboxylic acid derivatives. The derivatives are esters, thioesters, amides and sulfonimides. A key feature of the processes is the preparation of N-aryl substituted intermendiates by formation of a bond between the nitrogen atom of the acridan ring and a carbon atom of another aromatic or heteroaromatic ring compound. The arylation reaction is catalyzed by a palladium catalyst. The N-arylacridancarboxylic acid derivatives are useful in methods for producing light and in assays for peroxidase enzymes and enzyme inhibitors and in assays employing enzyme-labeled specific binding pairs.

Abstract: Novel heterocyclic compounds which generate chemiluminescence on reaction with a phosphatase enzyme are provided as well as a process for their preparation and intermediates useful therein. The compounds comprise a nitrogen, oxygen or sulfur-containing heterocyclic ring system bearing an exocyclic carbon—carbon double bond. The double bond is further substituted at the distal carbon with a phosphate group and an oxygen or sulfur atom-containing group. Novel compositions further comprising a cationic aromatic compound (CAC) in addition to the heterocyclic phosphate compound are provided. The addition of the CAC in the composition greatly increases the production of chemiluminescence and provides improved detection sensitivity. Compositions further comprising an anionic surfactant and a non-ionic surfactant provide additional improvements in detection sensitivity.

Abstract: The present invention is directed to novel water-soluble prodrugs of aliphatic or aromatic hindered hydroxyl group containing pharmaceuticals.

Abstract: The present invention is directed towards novel azaindole compounds which bind to the AMP site and are potent FBPase inhibitors. The present invention also is directed towards the clinical use of the novel FBPase inhibitors as a method of treatment or prevention of diseases responsive to lowered blood glucose levels.

Abstract: The present invention relates to the preparation of novel catalysts made from transition metal compounds and “tridentate” 4,5-diphosphinoacridine ligands (“acriphos”). The novel ligands employed herein are diphosphine compounds of 4,5-disubstituted acridine which coordinate transition metals in a three-fold way with the two phosphorus atoms and the acridine nitrogen. The invention also relates to the use of the novel catalysts for the catalysis of carbon monoxide conversion via the water-gas shift reaction (WGSR: CO+H2O→CO2+H2) and for the catalysis of the following reactions: hydroformylation, carbonylation, carboxylation, hydrogenation, hydrocyanogenation, hydrosilylation, polymerization, isomerization, cross-couplings and metathesis.

Abstract: The present invention provides bicyclic metabotropic glutamate receptor ligands, as well as compositions comprising such ligands, and and methods for their use.

Abstract: A process for preparing the anti-cancer drug camptothecin (CPT) and certain derivatives thereof. The process includes the reacting of three base reagents and a five-step process for synthesizing optically pure CPT in high overall yield from inexpensive starting materials.

Abstract: Claimed are newly synthesized phosphorus containing cytisine derivatives of the general formula wherein n is 0 or 1; X is O or S; R=CH3; C2H5; C3H7; 1-C3H7; C4H9; at n=1: X=O R=CH3 R1=1—C3H7; C6H5; CH3—O—C6H4—; with a proviso that n is 1, X is O. It is shown that some of the synthesized compounds exhibit substantial hepatoprotective and antienzyme activity.

Abstract: Nucleotide analogues having the general formula (I) and pharmaceutically acceptable derivatives: wherein n is 0 or an integer; X is O or S, CH2, CH-halogen, CH—N3, or C═CH2; Q and U are independently selected from: O, S, and CH(Ra) wherein Ra is hydrogen, OH, halogen, N3 ,NH2, SH, carboxyl, C1-6 alkyl or Ra is CH2(Rb) wherein Rb is hydrogen, OH, SH, NH2, C1-6 alkyl or carboxyl; or both Q and U are CH when Q and U are linked by a double bond; Z is selected from: O, a C1-6 alkoxy, a C1-6 thioalkyl, a C1-6 aminoalkyl, (CH2)m wherein m is 0 or an integer, and N(Rc)2 wherein both Rc are independently hydrogen or a C1-6 alkyl; and R2 is a purine or pyrimidine base or an analogue or derivative thereof. Members of this series of analogues possess anti-viral activity.

Abstract: Phospholipid derivatives of Formula X: wherein A is the ring system in which R is a linear or branched alkyl radical having 10 to 24 carbon atoms which may contain one or more double or triple bonds; R1 and R2 are independently hydrogen or linear alkyl radicals having 1 to 3 carbon atoms; y is 0, 1, 2 or 3; m and n are independently 0 or in an integer, with the proviso that m+n is between 2 and 8; or A is a tropanio or quinuclidinio ring system, which is linked via a carbon-carbon bond and is optionally substituted by one or more methyl groups; processes for the preparation of the derivatives, and methods for treating tumors therewith.

Abstract: A process for preparing 1H-imidazo[4,5-c]quinolin-4-amines is disclosed. The process involves reacting a 6H-imidazo[4,5-c]tetrazolo[1,5-a]quinoline with triphenylphosphine and hydrolyzing the product thereof.

Abstract: This invention relates to novel fused heterocycles which are useful as antagonists of the .alpha..sub.v .beta..sub.3 and related integrin receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.

Abstract: Compounds of the formula ##STR1## wherein X, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, A, B, D and E are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.

Abstract: The present invention relates to water soluble, camptothecin derivatives of formula (I). ##STR1## wherein A represents a moiety of the formula (IIA), (IIB) or (IIC): ##STR2## X is selected from the group consisting of alkyl, aryl, (CH.sub.2).sub.m OR.sup.1, (CH.sub.2).sub.m SR.sup.1 and (CH.sub.2).sub.m NR.sup.1 R.sup.2 wherein m is an integer of 0 to 6, and R.sup.1 and R.sup.2 are hydrogen, lower alkyl, aryl or together with the nitrogen form a 5-7 membered ring; q is an integer of 0 to 2; n represents the integer 1 or 2; p is an integer of 1 to 6; Y and W are selected from the group consisting of alkyl, aryl, alkoxy, aryloxy and amino, Q is oxygen or sulfur; P is phosphorus; J represents the atoms necessary to complete a 5 or 6 membered aromatic ring; and the pharmaceutically acceptable salts thereof; their use as topoisomerase inhibitors, their preparation; and their use in the treatment of cancer.

Abstract: Estratriene derivatives of the following formula have a powerful inhibitory effect on estrone sulfatase and are hence useful for the prophylaxis or treatment of diseases caused by estrogens, such as breast cancer, uterine cancer, ovarian cancer, endometriosis, adenomyosis uteri and mastopathy. ##STR1## wherein one of A and B represents C.dbd.O or CH.sub.2 and the other represents O or NH; and R represents --SO.sub.2 NR.sup.1 R.sup.2 or --PO(OM).sub.2 in which R.sup.1 and R.sup.2 each independently represent a hydrogen atom or a lower alkyl group and M represents a hydrogen atom or an alkali metal; provided that, when one of A and B represents NH, the other represents C.dbd.O.

Abstract: The present invention discloses the compounds of general formula (1) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 are optionally substituted carbonyl and amide derivatives which are useful as inhibitors of retroviral proteases, and are effective in treating conditions characterized by unwanted activity of these enzymes, such as acquired immume deficiency syndrome.

Abstract: Novel compounds are provided that comprise esters of antiviral phosphonomethoxy nucleotide analogs with carbonates and/or carbamates having the structure --OC(R.sup.2).sub.2 OC(O)X(R).sub.a, wherein R.sup.2 independently is H, C.sub.1 -C.sub.12 alkyl, aryl, alkenyl, alkynyl, alkyenylaryl, alkynylaryl, alkaryl, arylalkynyl, arylalkenyl or arylalkyl which is unsubstituted or is substituted with halo, azido, nitro or OR.sup.3 in which R.sup.3 is C.sub.1 -C.sub.12 alkyl; X is N or O; R is independently H, C.sub.1 -C.sub.12 alkyl, aryl, alkenyl, alkynyl, alkyenylaryl, alkynylaryl, alkaryl, arylalkynyl, arylalkenyl or arylalkyl which is unsubstituted or is substituted with halo, azido, nitro, --O--, --N.dbd., --NR.sup.4 --, --N(R.sup.4).sub.2 -- or OR.sup.3, R.sup.4 independently is --H or C.sub.1 -C.sub.

Abstract: Compounds of Formula I, and their N-oxides and agriculturally suitable salts, are disclosed which are useful for controlling undesired vegetation ##STR1## wherein X, Y, J, R.sup.1, and R.sup.2 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula I and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula I.

Abstract: The present application describes novel lactams and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein rings ring B is a 4-8 membered cyclic amide containing from 0-3 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.

Abstract: Compounds of formula (I) ##STR1## and their pharmaceutically acceptable salts inhibit matrix metalloproteases, such as stromelysin, gelatinase, matrilysin and collagenase, and are useful in the treatment of mammals having disease-states alleviated by the inhibition of such matrix metalloproteases.

Abstract: Activating groups for cyanine dyes used to label chain terminators in nucleotide sequencing, based on N-hydroxyphthalimide, are disclosed. From these activating groups, activated dyes of the present Invention are prepared which react with the derivitized nucleotide chain terminators to give a labeled chain terminator of the present Invention. The activating groups of the present Invention allow the dye-chain terminator reaction to occur at a much higher yield and with much greater selectivity for the mono-substituted product, compared with the prior art.

Abstract: A compound of the formula ##STR1## wherein alc.sub.1, alc.sub.2 and alc.sub.3 are alkyl of up to 8 carbon atoms, n is an integer from 0 to 8, R.sub.1 and R.sub.

Abstract: A series of guanine analogs and physiological salts thereof, which are useful as virus inhibitors and as antiviral agents in the treatment of viral disease, having the basic structures of: ##STR1## wherein B is H, CH.sub.3 or NH.sub.2 ; C is NH.sub.2 or SCH.sub.3 ; D is N or CH; E is O, S or Se; and G is selected from a group consisting of alkanes, alkenes, ethers, esters, hydrocarbons, amines and heterocyclic compounds, is herein disclosed. In I and III, A is O, S or Se while in II, A is NH.sub.2, OH, NHOH, OCH.sub.3 or SCH.sub.3. In I and II, F is 0, S or Se, while in III, F is F is 0, S, Se or NH. These compounds may be formulated with a physiological carrier, and used either alone or in combination with, for example, acyclovir or ganciclovir or another therapeutic agent, for the treatment of conditions resulting from viral infections.

Abstract: This invention provides compounds which are analogs to the hydrolysis transition-state of a cocaine benzoyl ester group. This invention also provides such analogs linked to carrier proteins, and antibodies thereto. This invention further provides pharmaceutical composition for decreasing concentration in a subject using the antibodies produced.

Abstract: Novel PMP, PME and HPMP and related compounds containing N-6 substituted 2,6-diaminopurine and adenine bases are provided. These compounds are useful in a variety of utilities, including as intermediates in the preparation of flame retardants, diagnostic reagents and therapeutics, including antivirals. Of particular note are compounds otherwise not known to possess anti-DNA viral activity that become potent inhibitors of DNA viruses upon substitution of the N-6 site, thereby providing a novel and unexpected and surprising use for such compounds.

Abstract: This invention provides compounds which are analogs to the hydrolysis transition-state of a cocaine benzoyl ester group. This invention also provides such analogs linked to carrier proteins, and antibodies thereto. This invention further provides pharmaceutical composition for decreasing concentration in a subject using the antibodies produced.

Abstract: This invention relates to certain phenylhetercyclic compounds, herbicidal compositions thereof and a method for their use as general and selective preemergent or postemergent herbicides or plant growth regulants.

Abstract: Compounds of formula ##STR1## wherein R and R' are each independently of the other hydrogen, C.sub.1 -C.sub.18 alkyl, COR.sub.1, COR.sub.2 or COOR.sub.1,X and X' are each independently of the other hydrogen, halogen, OH, NH.sub.2, COOH, C.sub.1 -C.sub.18 -alkyl, isocyclic or heterocyclic aromatic radicals, OR.sub.3, OCOR.sub.3, OCOR.sub.4, OCOR.sub.3, NHR.sub.3, N(R.sub.3).sub.2, NHCOR.sub.3, NHCOR.sub.4 or NHCOOR.sub.3,Y and Y' are each independently of the other hydrogen, halogen, OH, NH.sub.2, nitro, cyano, C.sub.1 -C.sub.18 alkyl, isocyclic or heterocyclic aromatic radicals, COR.sub.5, COR.sub.6, COOR.sub.5, COOR.sub.6, CONH.sub.2, SO.sub.2 R.sub.5, SO.sub.2 R.sub.6, SO.sub.2 NH.sub.2, SO.sub.3 H, PO(OR.sub.5).sub.2 or PO(OH).sub.2, andZ and Z' are each independently of the other hydrogen, halogen, OH, NH.sub.2, COOH, cyano, C.sub.1 -C.sub.18 alkyl, isocyclic or heterocyclic aromatic radicals, OR.sub.7, OR.sub.8, OCOR.sub.7, OCOR.sub.8, OCOOR.sub.7, NHR.sub.7, N(R.sub.7).sub.2, NHR.sub.8, CONH.sub.

Abstract: Phosphoramidates and phosphinic amides and related compounds are provided. Also provided are methods that use the compounds for modulating the activity of the endothelin family of peptides are provided. In particular, compounds having formula: ##STR1## in which A, B, R.sup.1 and R.sup.2 are as described are provided. Also provided are methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these compounds or prodrugs thereof. Methods for elucidating the physiological and pathophysiological roles of endothelin, as well as isolating endothelin receptors are also provided.

Abstract: The present invention relates to heterocyclic compounds of the formula ##STR1## in which R.sup.1 -R.sup.7, B, a and X have the meanings recited in the specification. These compounds are usable in the treatment of diseases of the rheumatoid variety and for the prevention of allergically induced diseases.

Abstract: A heterocyclic aromatic halide or an aryl halide is reacted with an amine compound in the presence of a base to give a heterocyclic aromatic amine or an arylamine, respectively. In this reaction, a catalyst comprising a palladium compound and a tertiary phosphine is used for the preparation of a heterocyclic aromatic amine, and a catalyst comprising a palladium compound and a trialkylphosphine is used for the preparation of an arylamine.

Abstract: Novel compounds are provided that comprise esters of antiviral phosphonomethoxy nucleotide analogs with carbonates and/or carbamates having the structure --OC(R.sup.2).sub.2 OC(O)X(R).sub.a, wherein R.sup.2 independently is H, C.sub.1 -C.sub.12 alkyl, aryl, alkenyl, alkynyl, alkyenylaryl, alkynylaryl, alkaryl, arylalkynyl, arylalkenyl or arylalkyl which is unsubstituted or is substituted with halo, azido, nitro or OR.sup.3 in which R.sup.3 is C.sub.1 -C12 alkyl; X is N or O; R is independently H, C.sub.1 -C.sub.12 alkyl, aryl, alkenyl, alkynyl, alkyenylaryl, alkynylaryl, alkaryl, arylalkynyl, arylalkenyl or arylalkyl which is unsubstituted or is substituted with halo, azido, nitro, --O--, --N.dbd., --NR.sup.4 --, --N(R.sup.4).sub.2 -- or OR.sup.3, R.sup.4 independently is --H or C.sub.1 -C.sub.

Abstract: A bisphosphite compound of the following formula (A): ##STR1## wherein --Ar--Ar-- is a bisarylene group represented by any one of the formulae (A-I) to (A-III) defined in the specification, and each of Z.sub.1 to Z.sub.4 is a C.sub.4-20 aromatic or heteroaromatic group which may have a substituent, wherein each of substituents on carbon atoms of an aromatic ring adjacent to the carbon atom bonded to the oxygen atom in each of Z.sub.1 to Z.sub.4, is a C.sub.0-2 group, and each pair of Z.sub.1 and Z.sub.2, and Z.sub.3 and Z.sub.4, are not bonded to each other.

Abstract: The invention relates to retroviral protease inhibitors of the general formula (I): W--(A).sub.n --B--(A*).sub.m --V where W, A, B, A*, V, n and m are as defined herein, including related prodrugs of general formula (I) comprising a solubilizing group which is labile in vivo.

Abstract: Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, infectious urinary tract stones, and bone cancer, are obtained by combining chemically a diphosphonate compound with a therapeutic agent effective against the foregoing diseases.

Abstract: Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.

Abstract: Compounds of the invention have the formula ##STR1## The compounds have fibrinogen receptor antagonist activity.

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: A polymeric conjugate consists essentially of: (i) from 60 to 99 mol % of N-(2-hydroxypropyl) methacryloylamide units represented by formula 1: ##STR1## (ii) from 1 to 40 mol % of 20-0-(N-methacryloylglycyl-aminoacyl) camptothecin units represented by formula 2 ##STR2## wherein ?A! is a spacer group having respective terminal amino and carbonyl groups which are separated by at least three atoms and O-CPT represents a residue of a camptothecin, the C-20 hydroxy group of the camptothecin being linked to the terminal carbonyl group of the spacer group ?A!; and (iii) from 0 to 10 mol % of N-methacryloylglycine or N-(2-hydroxy-propyl)methacryloylglycinamide units represented by formula 3: ##STR3## wherein Z represents hydroxy or a residue of formula --NH--CH.sub.2 --CH(OH)--CH.sub.3.

Abstract: Substituted quinoline compounds, processes for their preparation, composition containing them, and their use as safenersCompounds of the formula I and salts thereof ##STR1## in which R.sup.1 ?lacuna! CN, C(.dbd.Z)--Q(A.sub.i X.sub.i).sub.q --R, --C(.dbd.Z)--QR*, 1,2,3,4-tetrazol-5-yl, 1,3,4-triazol-2-yl, 1,3-oxazol-2-yl,and the remaining radicals are as defined in claim 1, are suitable for use as safeners for protecting crop plants such as, for example, cereals, rice and maize, against herbicide damage.Some of the compounds are known and some are novel and they can be prepared from quinolin-8-oxy derivatives by the processes of claim 7.

Abstract: Disclosed are quaternary nitrogen-containing, saturated or unsaturated monocyclic and bicyclic ring-containing bisphosphonate compounds, and pharmaceutically-acceptable salts and esters thereof. These compounds, which are useful for treating or preventing disorders of calcium and phosphate metabolism, have the following general structure: ##STR1## wherein (a) each X and Y are independently selected from nil, O, S, NR.sup.1 and N.sup.+ (R.sup.2).sub.2 ; if no R.sup.1 is N.sup.+ (R.sup.2).sub.2, then at least one of X or Y must be N.sup.+ (R.sup.2).sub.2 ;(b) m and n and m+n are integers from 0 to 5; p and q and p+q are integers from 0 to 3;(c) s is an integer from 0 to 2 and when m+n=0 and X is nil, s=2;(d) each R.sup.1 is independently selected from the group consisting of nil, N.sup.+ (R.sup.2).sub.2, R.sup.9 SR.sup.6, SR.sup.6, hydrogen, hydroxy; unsubstituted or substituted C.sub.1 -C.sub.8 alkyl, --OR.sup.3, --CO.sub.2 R.sup.3, --O.sub.2 CR.sup.3, NR.sup.3.sub.2, --N(R.sup.3)C(O)R.sup.3, --C(O)N(R.sup.3).

Abstract: A compound of the formula (I), or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein, X represents a moiety of formula (a), in which A.sup.1 represents --CH.dbd.CH.dbd., NH, S or O; A.sup.2 represents an oxo or a thioxo group; A.sup.3 represents H or an alkylcarbonyl group; and A.sup.4 represents hydroxy or NR.sup.s R.sup.t wherein R.sup.s and R.sup.t each independently represents H or alkyl; R.sup.0 and R.sup.1 each independently represents hydrogen or an alkyl group; R.sup.2 represents OCH.sub.2 CO.sub.2 H, or an ester or amide thereof, or R.sup.2 represents a moiety of formula (b), wherein R.sup.4 and R.sup.5 each independently represent hydrogen, alkyl, hydroxyalkyl, cycloalkyl or R.sup.4 together with R.sup.5 represents (CH.sub.2).sub.n wherein n is 2, 3 or 4; and R.sup.3 represents hydrogen, halogen, alkyl or alkoxy or R.sup.3 together with R.sup.

Abstract: A compound of the Formula I or Formula II ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, hydroxy, chlorine, fluorine, bromine, or an organic substituent having 1 to 5 carbon atoms and selected from acyloxy having a hydrocarbon stem of 1 to 4 carbon atoms, alkoxy, alkylthio, amino, alkylamino and dialkylamino;R.sup.3 and R.sup.4 are independently hydrogen, or organic phosphonic ester substituents having 1 to 12 carbon atoms and selected from alkyl, alkenyl, aryl, and aralkyl; andB is a heterocyclic group selected from the group consisting of pyrimidine, purine, triazine, deazapurine, and triazole, attached through a ring nitrogen atom thereof optionally substituted with 1 to 3 substituents selected from the group consisting of hydroxy, mercapto, amino, hydrazino, fluoro, chloro, bromo, iodo, C.sub.1 to C.sub.3 alkyl, C2-C3 alkenyl, C2-C3 haloalkenyl, C1-C3 alkoxy, and C1-C3 alkylthio;and the pharmaceutically acceptable acid addition, metal, and amine salts thereof.

Abstract: A process for preparing 1H-imidazo?4,5-c!quinolin-4-amines is disclosed. The process involves reacting a 6H-imidazo?4,5-c!tetrazolo?1,5-a!quinoline with triphenylphosphine and hydrolyzing the product thereof.

Abstract: N-(3-Fluoro-2-phosphonylmethoxypropyl) derivatives of purine and pyrimidine heterocyclic bases, method of producing them and their use as active principles of drugs.The invention relates to suppression of multiplication of viruses, particularly retroviruses, by application of the new compounds, N-(3-fluoro-2-phosphonylmethoxypropyl) derivatives of purine and pyrimidine heterocyclic bases. These compounds are obtained by the reaction of the N-(3-fluoro-2-hydroxypropyl) derivatives of purine and pyrimidine heterocyclic bases with diesters of p-toluenesulfonyloxymethylphosphonic acid in the presence of sodium hydride.

Abstract: The present invention relates to phosphonsulfonates and the pharmaceutically-acceptable salts and esters thereof, having the following structure according to formula (I): ##STR1## The present invention further relates to pharmaceutical compositions containing a safe and effective amount of a compound of the present invention, and pharmaceutically-acceptable excipients. Finally, the present invention relates to methods for treating or preventing pathological conditions characterized by abnormal calcium and phosphate metabolism in humans or other mammals, including treating or preventing osteoporosis and arthritis, especially rheumatoid arthritis and osteoarthritis. This method comprises administering to a human or other mammal in need of such treatment of a safe and effective amount of a compound or composition of the present invention.

Abstract: Provided are compounds of the following formulae:A phosphonomethoxymethyoxymethyl purine/pyridimidine 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 (II) or (VIII) ##STR2## wherein the broken line is an optional bond; X, R and X' are the same or different and are H or alkyl with 1 to 6 carbon atoms;wherein in the compound of formula (II), Y and Z are the same or different and are H; OH; alkyl having 1 to 6 carbon atoms; alkyl having 1 to 6 carbon atoms which is substituted with halogen, hydroxy, amino or azido; or Y and Z are taken together to form an oxygen atom or a methylene group; or Y is taken together with X' to complete a cyclic phosphonate having the structure of formula (III) ##STR3## wherein R.sup.

Abstract: A class of imidazo?1,2-a!pyridinyldiacid compounds is described for cognitive enhancement and for treatment of cognitive disorders and which have activity as a cognitive enhancer. Such compounds are also useful to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a compound of this class alone or in a composition in an amount effective as an agonist or partial agonist to modulate, or as an antagonist to inhibit, excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula: ##STR1## wherein each R.sup.20 is independently selected from hydrogen, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl; wherein each of Y.sub.m and Y.sub.

Abstract: The present invention relates to compound of formula (I) ##STR1## wherein A is benzene, naphthalene, 5,6,7,8,-tetrahydronaphthalene, quinoline, isoquinoline, indole or 7-azaindole;R.sub.1 is --H, --CN, --SO.sub.3 R.sub.4 --, --SO.sub.2 NHR.sub.5, ##STR2## --COOR.sub.6, --CONHCH.sub.2 (CHOH).sub.n CH.sub.2 OH, ##STR3## --NR.sub.7 R.sub.8, --N(CH.sub.2 CH.sub.2 OH).sub.2, --NHCH.sub.2 (CHOH).sub.n CH.sub.2 OH, --NHCONH.sub.2, --NH--C(NH.sub.2).dbd.NH, --NHCO(CHOH).sub.n CH.sub.2 OH, ##STR4## --NHSO.sub.2 R.sub.9, --OR.sub.10, --OCH.sub.2 (CHOH).sub.n CH.sub.2 OH, --OOC(CHOH).sub.n CH.sub.2 OH, --OPO(OH).sub.2, --CH.sub.2 NH.sub.2, --C(NH.sub.2).dbd.NH, --CH.sub.2 NHC(NH.sub.2).dbd.NH, ##STR5## --CH.sub.2 OH, --CH.sub.2 OOC(CHOH).sub.n CH.sub.2 OH, --CH.sub.2 OPO(OH).sub.2 or --PO(OH).sub.2 ;R.sub.2 is C.sub.1 -C.sub.6 alkyl, halogen, or hydroxy;R.sub.3 is --H or C.sub.1 -C.sub.6 alkyl;R.sub.4 is --H, C.sub.1 -C.sub.6 alkyl or --CH.sub.2 (CHOH).sub.n CH.sub.2 OH;R.sub.5 is --H, C.sub.1 -C.sub.6 alkyl, --CH.sub.