Abstract: Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: wherein X is O or NR9 and Het, R1, R7, R8, R12—R15, Ra, Rb, Rc, Z, and n are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing such compounds. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier.

Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R?; J is sulfur or oxygen; R?, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.

Abstract: A new class of diketo acids constructed on nucleobase scaffolds, designed as inhibitors of HIV replication through inhibition of HIV integrase, is described. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS and ARC, either as the compounds, or as pharmaceutically acceptable salts, with pharmaceutically acceptable carriers, used alone or in combination with antivirals, immunomodulators, antibiotics, vaccines, and other therapeutic agents. Methods of treating AIDS and ARC and methods of treating or preventing infection by HIV are also described.

Abstract: The invention relates to a process for the preparation of certain pyrimidinone compounds.

Abstract: The present invention provides a genus of pyrimidine amides that are useful as openers of potassium ion channels. The compounds of the invention are of use in both therapeutic and diagnostic methods.

Abstract: GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein A, Q, R1, R2, R3a, R3b, R4, R5, R6 and n are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

Abstract: This invention provides compounds defined by Formula I or a pharmaceutically acceptable salt thereof, wherein R1, Q, R2, R3, and R4 are as defined in the specification. The invention also provides related pharmaceutical compositions, methods of use, and combinations.

Abstract: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to ?4 integrin.

Abstract: Uracil reductase inactivators, notably a 5-substituted uracil or 5,6-dihydro-5-substituted uracil, potentiate 5-flourouracil and find use particularly in the treatment of cancer. The 5-substituent is selected from bromo, ido, cyano, halo-substituted C1-4 alkyl, C2-6 alkenyl, 1-halo-C2-6 alkenyl and halo-substituted C2-6 alkynyl.

Abstract: Corticotropin-releasing factor (CRF) antagonists having the formulae wherein the dashed lines, A, B, Y, Z, G, R3, R4, R5, R6, R16 and R17 are as defined in the application, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment disorders including CNS and stress-related disorders.

Abstract: The present invention relates to a novel process for preparing known 1-amino-3-phenyluracil derivatives, to novel 1-amino-6-hydroxy-3-phenyldihydro-2,4(1H,3H)pyrimidinedione derivatives of the formula (II) in which R1 is hydrogen, cyano, nitro or halogen, R2 is cyano, nitro, halogen or optionally substituted alkyl or alkoxy, R3 is hydrogen, hydroxyl, mercapto, amino, hydroxyamino, hydrazino, halogen, or one of the radicals —R6, -Q-R6, —NH—R6, —NH—O—R6, —NH—SO2—R6, —N(SO2—R6)2, —CQ1-R6, —CQ1-Q2-R6, —CQ1-NH—R6, -Q2-CQ1-R6, —NH—CQ1-R6, —N(SO2—R6)(CQ1-R6), -Q2-CQ1-Q2-R6, —NH—CQ1-Q2-R6 or -Q2-CQ1-NH—R6, where Q is O, S, SO or SO2, Q1 and Q2 are each independently oxygen or sulphur and R6 is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heterocyclyl or heterocyclylalkyl, R4 is hydrogen, halogen or optionally substituted alkyl, and R5 is fluorine- and/or chlorine-substituted alkyl, as intermediates for the 1-amino-3-phenyluracil derivatives, and to a process f

Abstract: This invention concerns new biocidal compounds of formula (I) wherein R is H or CH3. Of particular interest are two isomers that are named malayamycin A and desmethylmalayamycin A. These isomers, which may be prepared by growing under controlled conditions a previously unknown strain of micro-organism from the species Streptomyces malaysiensis, are characterised by nmr and mass spectroscopic data. They have biocidal activity, including anti-fungal, anti-viral and anti-cancer activity, and are of special interest for use in agriculture, horticulture, animal and human health.

Abstract: The embodiments described herein concern 5-substituted pyrimidine derivatives of conformationally locked nucleoside analogues and to the use of these derivatives as anti-viral and anti-cancer agents. The compounds are of the formula: wherein B is uracil-1-yl or cytosin-1-yl having a 5-substituent selected from halogen, alkyl, alkenyl, and alkynyl, with the proviso that where B is uracil-1-yl, the 5-substituent is not methyl. The compounds are useful in the treatment of Herpes simplex virus (HSV).

Abstract: The present invention relates to pyrimidinedione derivatives of following formula (I) which are useful as antiviral agents, especially as agents for treatment of AIDS, pharmaceutically acceptable salts thereof, process for the preparation thereof and pharmaceutical compositions containing the same, wherein R represents cyclopropyl; cyclobutyl; cyclohexyl; unsubstituted or mono-, di- or trisubstituted phenyl with a group selected from hydroxy, C1–C4 alkyl, C1–C4 alkoxy, halogen, trifluoromethyl, cyano and amino; 1- or 2-naphthyl; 9-anthracenyl; 2-anthraquinonyl; unsubstituted or substituted pyridyl with a group selected from C1–C4 alkyl, C1–C4 alkoxy, cyano and halogen; 2-, 3- or 4-quinolinyl; oxiranyl; 1-benzotriazolyl; 2-benzoxazolyl; furanyl substituted with C1–C4 alkoxycarbonyl; C1–C4 alkylcarbonyl; or benzoyl, R1 represents halogen or C1–C4 alkyl, R2 and R3 represent independently hydrogen or C1–C4 alkyl, X represents oxygen atom, and Y represents oxygen atom, sulfur atom or carbonyl.

Abstract: The present application describes novel barbituric acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, L, R1, W, Z, Ua, Xa, Ya, and Za are defined in the present specification, which are useful as TNF-? converting enzyme (TACE) and matrix metalloproteinases (MMP) inhibitors.

Abstract: Methods and compounds useful for the inhibition of convulsive disorders, including epilepsy, are disclosed. The methods and compounds of the invention inhibit or prevent ictogenesis and epileptogenesis. Methods for preparing the compounds of the invention are also described.

Abstract: Substituted aryl ether derived compounds represented by the general structure (I) are described. X and Y are independent of each other and are represented by hydrogen, halogen, cyano, nitro, (C1-4)alkyl, (C1-4)haloalkyl, or (C1-4)haloalkoxy; Z is oxygen or sulfur; Q is selected form Q1 to Q6; Also described are the processes for the manufacture of these compounds and agriculturally suitable compositions containing these as active ingredients which are useful as herbicides for general or selective pre-emergent or post-emergent control of undesired plant species and defoliants.

Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein A, Q, R1, R2, R3a, R3b, R4, R5, R6 and n are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

Abstract: The present invention relates to hydrazinyl and nitrogen oxide pyrazoles of the formula I: wherein the ring of the formula (R5)-A-(SOmR4), m, X, R1 through R5 are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.

Abstract: Novel tumour selective anti-neoplastic agents are characterized, in that to customary antineoplastic agents are attached one or two very specific unbranched &OHgr;-hydroxyalkyl, (&OHgr;-hydroxy)alkenyl, &OHgr;-(2,3-dihydroxypropyloxy)alkyl or an (&OHgr;-(2,3-dihydroxypropyloxy))alkenyl groups R2 and R3 with 5 to 30 carbon atoms, forming a tumour selective conjugate as exemplified with the compounds of formulae I, II and III [] wherein R1 is a customary pharmaceutically acceptable inorganic or organic leaving group and A is 1,2-dimethylene, 1,3-trim ethylene, 1,2-cyclopentylene or 1,2-cyclohexylene.

Abstract: Substituted aryl ether derived compounds represented by general structure (I) are described. X and Y are independent of each other and are represented by hydrogen, halogen, cyano, nitro, (C1-4)alkyl, (C1-4)haloalkyl, or (C1-4)haloalkoxy; Z is oxygen or sulfur, Q is selected form Q1 to Q6; A is oxygen, sulfur, or imino; R1 is hydrogen, (C1-4)alkyl, (C1-4)haloalkyl, or amino and can be independent of each other in a single molecule; R2 and R3 are independent of each other and may be selected from the group consisting of hydrogen, halogen, cyano nitro, (C1-4)alkyl, (C1-4)haloalkyl, (C2-4)alkenyl, (C2-6)haloalkenyl and amino which may be optionally substituted with (C1-4)alkyl or (C1-4)haloalkyl; Ar is substituted or unsubstituted carbocyclic or heterocyclic aromatic ring being at least a five or six membered ring. This ring can be fused with another substituted or unsubstituted five or six membered carbocyclic or heterocyclic ring. When Q is Q5, unsubstituted or substituted phenyl is excluded.

Abstract: The present invention relates to novel pyrimidones of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention more particularly novel pyrimidones of the general formula (I).

Abstract: The invention relates to new substituted phenyluracils of the general formula (I) 1

Abstract: 1

Abstract: Compounds which are active against viruses have the following Formulas: wherein B is a purine or pyrimidine heterocyclic ring and is preferably selected from the group consisting of 6-aminopurine (adenine), 2,6-diaminopurine, 2-amino-6-azidopurine, 2-amino-6-cyclopropylaminopurine, 6-hydroxypurine (hypoxanthine), 2-amino-6-halo substituted purines, 2-amino-6-alkoxy substituted purines, 2-amino-6-hydroxypurine (guanine), 3-deazapurines, 7-deaza-purines, 8-azapurines, cytosine, 5-halo substituted cytosines, 5-alkyl substituted cytosines, thymine, uracil and 6-azapyrimidines; X is O; and, R1 and R2 are alkyl or aryl groups. The compounds of the present invention also include the R- and S-enantiomers of the above compounds. The R1X and/or R2X can also be amino acid residues with X as NH.

Abstract: Compounds having formula I are provided where the variables have the values described herein.

Abstract: The invention relates to new substituted phenyluracils of the general formula (I) in which n, Q, R1, R2, R3, R4, R5 and X have the meanings given in the description, to process and new intermediates for their preparation, and to their use as herbicides.

Abstract: Therefore, it is critical that the roles these enzymes play in biological processes outside of extracellular matrix degradation or remodeling be understood in order to assess their potential as targets for therapeutic intervention, and to design safe, conveniently produced, orally active inhibitors. Elastase inhibitors can differ with respect to their ability to inhibit different elastases. As a result, the spectrum of elastases inhibited by a specific drug candidate as well as the spectrum of activities these enzymes have with respect to proteins other than elastin are properties to consider in evaluating the drug candidates.

Abstract: Thymine analogs and methods for their use as diagnostic and therapeutic agents for tumors.

Abstract: A photosensitive layer contains an electron-transfer agent that makes use of a compound represented by the following general formula (1): 1

Abstract: Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented.

Abstract: The present invention relates to compounds of the formula wherein R1, R3, R5 and A are defined as in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment of inflammation and other inflammation associated disorders, such as osteoarthritis, rheumatoid arthritis, colon cancer and Alzheimer's disease, in mammals (preferably humans, dogs, cats and livestock).

Abstract: The present invention relates to novel thioquinazolinone derivative compounds and combinatorial libraries of the following formula: 1

Abstract: The invention concerns novel substituted 6-benzyl-4-oxopyrimnidines of general formula (A). These compounds inhibit reverse transcriptase encoded by human immunodeficiency virus (HIV) or pharmaceutically acceptable salts thereof, and find their application in the prevention and treatment of HIV infection and the treatment of the resulting acquired immune deficiency syndrome (AIDS). Pharmaceutical compositions containing the compounds and a method of use of the present compounds and other agents for the treatment of AIDS and viral infection by HIV are also envisaged.

Abstract: The present invention provides herbicidal active compound combinations which comprise, N-aryl-uracils and herbicidally active compounds and/or compounds which improve crop plant compatibility. The combinations find use in controlling monocotyledonous and dicotyledonous weeds in crops of useful plants.

Abstract: A pyrimidine derivative of formula (I) or (I′): wherein: Rx is a substituent as defined within; Q1 is optionally substituted phenyl, and Q1 bears a substituent of formula (Ia) wherein: X, Y1, Y2, Z, n, and m are as defined within; —NQ2 is an optionally substituted heterocyclic moiety containing one hydrogen heteroatom and optionally containing a further heteroatom; or a pharmaceutically acceptable salt in vivo hydrolysable ester thereof; are useful as anti-cancer agents. Processes for their manufacture and pharmaceutical compositions containing them are described.

Abstract: This invention relates to certain novel 2′-halomethylidene, 2′-ethenylidene and 2′-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease states.

Abstract: 2,4-pyrimidinedione derivatives of formula (I) having high antiviral activity against wild-type and mutant HIV-1 and low toxicity are useful for treating AIDS (I) wherein: R1 is a C6-10 aryl or C3-10 heteroaryl group optionally having one or more substituents selected from the group consisting of halogen, C1-6 alkyl, C1-6 alkyl substituted with one or more halogen atoms, C3-4 cycloalkyl, cyano, nitro, hydroxy, thiohydroxy, azido, C1-6 alkoxy, oximino, C1-3 alkyloximino, O—(C1-6 alkyl)-substituted oximino, C—1-6 alkylcarbonyl, C3-6 cycloalkylcarbonyl, hydroxymethyl, azidomethlyl, C1-6 alkoxymethyl, C1-6 acyloxynethyl, carbamoyloxymethyl, anminomethyl, N—(C1-3 alkyl)aminomethyl, N,N-di(C1-3 alkyl)aminomethyl, carboxy, C1-6 alkoxycarbonyl, aziridine, amino, hydroxyethylamino, cyclopropylamino, C1-6 alkylamino, di(C1-6 alkyl)amino, trifluoroacetamido, C1-6 acylamido, carbamoyl, hydroxyethylcarbamoyl, cyclopropylcarbamoyl, C1-6 alkylcarbamoyl, di(C1-6 alkyl)carbamoyl, aminocarbamoyl, dimethylamin

Abstract: Compounds of formula (I) are inhibitors of the enzyme Lp-PLA2 and are of use in therapy, in particular for treating athereosclerosis.

Abstract: The present invention relates to novel types of peptide nucleic acids (PNAS) with improved properties. In particular, it relates to positively charged PNA units having an ethylene linker between the backbone and the nucleobase, to oligonucleotide analogs comprising these units, to oligomers comprising these units, and to the use of positively charged PNAs as novel delivery agents with therapeutic and diagnostic applications including for antisense therapy.

Abstract: The invention relates to novel substituted phenyluracils of the general formula (I) 1

Abstract: Phenyluracils of the general formula (I) 1

Abstract: This invention is directed to poly-hydroxylated monocyclic N-heterocyclic derivatives selected from the following formulae: wherein Z1, Z2, R1, R2, R3, R4, R5, R6, and R7 are defined herein. These compounds are useful as anti-coagulants.

Abstract: A range is disclosed of pyrimidine derivatives (I) which can act as inhibitors of cyclin dependent kinases (CDK's) and which thereby can provide useful therapeutic compounds for use in treatment of tumours or other cell proliferation disorders. The compounds of this invention bind to CDK molecules in a manner that appears to differ from that of known CDK inhibitors such as olomoucine and roscovitine.

Abstract: The present invention creates a novel antiangiogenic agent and provides an antitumor agent which shows high safety as compared with conventional antitumor agents, has a sure effect and is able to be administered for a long period. That is, it provides an indole compound represented by the following formula (I), its pharmacologically acceptable salt or hydrates thereof. In the formula, R1 represents hydrogen atom, a halogen atom or cyano group; R2 and R3 are the same as or different from and each represents hydrogen atom, a C1-C4 lower alkyl group or a halogen atom; R4 represents hydrogen atom or a C1-C4 lower alkyl group; and the ring A represents cyanophenyl group, aminosulfonylphenyl group, aminopyridyl group, aminopyrimidyl group, a halopyridyl group or cyanothiophenyl group, provided that the case where all of R1, R2 and R3 are hydrogen atoms, where both R2 and R3 are hydrogen atoms or where the ring A is aminosulfonyl group and both R1 and R2 are halogen atoms is excluded.

Abstract: A method for the treatment for hepatitis delta infection in a host, that includes administering an effective amount of a nucleoside or a nucleoside analog that suppresses the expression of the hepatitis B surface or preS1 antigen in the host 100-fold or more relative to pretreatment values in vivo; or to not more than 1 microgram per milliliter in vivo. In a preferred embodiment, the nucleoside is L-FMAU, or a pharmaceutically acceptable salt or prodrug thereof.

Abstract: The invention relates to carboxylic acid derivatives of the formula I where the radicals have the meanings stated in the description, and to their use as drugs.

Abstract: This invention relates to a method of treating disorders responsive to the blockade of sodium ion channels using novel aryl-substituted pyrimidine compounds of Formula I: 1

Abstract: The method of this invention prepares acylated cyclic compounds by contacting phenyl esters as acylating agents with cyclic compounds in the presence of a cyanide or fluoride catalyst.

Abstract: Novel herbicidal and defoliant substituted aniline derived compounds represented by general structure (I) are described. W, X, Y, Z, and Q are as defined in the disclosure. Also described are the processes for the manufacture of these compounds and agriculturally suitable compositions containing these as active ingredients which are useful as herbicides for general or selective pre-emergent or post-emergent control of undesired plant species and defoliants at very low concentrations of these biologically active compounds.