Abstract: Compounds of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, A, D, X, Y and Z have the meaning as defined in the claims, exhibit protein tyrosine kinase and protein serin/threonine kinase inhibitory activity.

Abstract: In accordance with the present invention there is provided a pharmaceutical combination useful for the treatment of leukemia comprising at least one active compound of formula (I): 1

Abstract: This invention relates to inhibitors of p38, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders mediated by p38.

Abstract: Nitrate salts of antimicrobial agents for the preparation of antimicrobial medicaments, specifically antiviral, antifungal and antibacterial medicaments.

Abstract: The present invention relates to a method of inducing proliferation of bone marrow cells in a subject, compromising administering to the subject an effective amount of an adenosine A1 receptor agonist. The present invention further relates to a method for preventing reduction in level of leukocytes in a subject as a result of a treatment comprising administering to the individual an effective amount of an adenosine A1 receptor agonist. In addition, the invention relates to a method of treatment of an individual comprising administering to the subject a therapeutic drug in combination with an adenosine A1 receptor agonist.

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: This invention relates to inhibitors of p38, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders mediated by p38.

Abstract: The invention relates to glyceryl nucleotides of the formula Ia in which a) one of the radicals A1, A2 and A3 is a hydrogen atom or a radical selected from hydroxyl, mercapto, alkyl, alkenyl, polyoxyalkenyl, aryl, acyl, alkyloxy, alkenyloxy, polyoxyalkenyloxy, acyloxy, aryloxy, alkylthio, alkenylthio, acylthio and arylthio, where the alkyl, alkenyl and acyl radicals are optionally substituted by from 1 to 3 aryl radicals; and b1) two of the remaining radicals A1, A2 and A3 are two nucleoside groups which are different from each other; or b2) one of the remaining radicals A1, A2 and A3 is a nucleoside group and the other of the remaining radicals is a hydroxycarbonyl group, where at least one of the nucleoside groups is not a naturally occurring nucleoside group; to processes for preparing these compounds, to pharmaceutical remedies which comprise these compounds, and to the use of these compounds for treating cancer diseases and infectious diseases.

Abstract: The present invention relates to novel compounds according to the to the general formulas I, II, III, IV or V: 1

Abstract: Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of indole-3-carbinol metabolites wherein the structures and substituents of the compounds are selected to enhance the compounds' overall efficacy, particularly with respect to therapeutic activity, oral bioavailability, long-term safety, patient tolerability, and therapeutic window. The compounds are useful not only in treatment of cancer but also in prevention of cancer.

Abstract: The present invention relates to 3′ substituted-2′, 3′-didehydro-2′, 3′-dideoxy-&bgr;-L-nucleosides and their pharmaceutically acceptable salts and prodrugs thereof, for the treatment of infectious viral diseases, in general, particularly HBV and HIV viral infections and more particularly, HBV and HIV viral infections that are resistant to other antiviral drugs.

Abstract: Novel heterocyclic compounds having a six membered ring structure fused to a five membered ring structure are found to be useful for the treatment and prevention of symptoms or manifestations associated with disorders affected by Interleukin-12 (“IL-12”) intracellular signaling, such as, for example, Th1 cell-mediated disorders. The therapeutic compounds, pharmaceutically acceptable derivatives (e.g., resolved enantiomers, diastereomers, tautomers, salts and solvates thereof) or prodrugs thereof, have the following general formula: Each X, Y and Z are independently selected from a member of the group consisting of C(R3), N, N(R3) and S.

Abstract: The present invention provides a method for treating a cancer in a mammal comprising administering an effective amount of an indole compound, in combination with an alkylating agent; to a mammal afflicted with cancer.

Abstract: A phosphonate nucleotide compound represented by the following formula (I) or a salt thereof, or a hydrate or solvate thereof: wherein, R1 is a hydroxyl group; each of R2 and R3 is independently a hydrogen atom, a C1-C22 alkyl group, an alkanoyloxymethyl group, an alkanoylthioethyl group, or an ethyl group substituted by one or more halogen atoms; R4 is a hydrogen atom, a C1-C4 alkyl group, a C1-C4 hydroxyalkyl group, or a C1-C4 alkyl group substituted by one or more halogen atoms; and X is CH or a nitrogen atom.

Abstract: Disclosed are polymeric compounds which are useful as prodrugs, comprising a chain of monomeric nucleosides, nucleoside analogs or abasic nucleosides, wherein at least one of the nucleosides or nucleoside analogs or a heterocyclic derivative thereof is pharmaceutically active and the nucleosides, nucleoside analogs or abasic nucleosides are linked by a phosphodiester group, a phosphorothioate group or an H—, alkyl or alkenyl phosphonate group.

Abstract: The present invention provides a therapeutic method to treat non-malignant diseases characterized by the excessive tissue growth, e.g., hyperplastic diseases, comprising administering to a mammal (e.g.

Abstract: The present invention is directed to particular bisphosphonate compounds, and in particular, to bisphosphonate conjugates that are useful in the treatment of soft tissues surrounding bone and bone-related diseases, such as bone cancer and osteoporosis.

Abstract: The present invention relates to compounds of formula (I), in which B, D, E, G, X, Y, Z, R1, R2 and s have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of formula (I) are valuable pharmacologically active compounds. They are vitronectin receptor antagonist and inhibitors of cell adhesion and are suitable for the therapy and prophylaxis of illnesses which are based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-matrix interaction processes or which can be prevented, alleviated or cured by influencing such interactions. For example, they can be applied for inhibiting bone resorption by osteoclasts and thus for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or prolifertion of cells of the vascular smooth musculature.

Abstract: Preventives and remedies with an excellent immunopotentiating effect for infections, sepsis and/or septic shock. More specifically, immunopotentiators/preventitives and remedies for infections and remedies for sepsis and septic shock comprising as the active ingredient reduced riboflavin and/or reduced riboflavin derivatives or pharmacologically acceptable salts thereof.

Abstract: The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which R1, R2, R3 and A are each as defined, and to processes for their preparation and to their use as medicaments, in particular as medicaments for the treatment of cardiovascular disorders.

Abstract: The present invention relates to methods of treatment of certain metabolic diseases, and to novel compounds and their prodrugs, and/or pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds useful in treating such diseases. In particular, this invention relates to the use of novel compounds and compositions for treatment of cardiovascular diseases, diabetes, cancers, acidosis, and obesity through the inhibition of malonyl-CoA decarboxylase (MCD). These compounds have the formulae (I) and (II), wherein Y, C, R1, R2, R6, and R7 are defined herein.

Abstract: Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.

Abstract: Dihydrate of 4-[[9-[(3-cyclopentyloxy-4-methoxy)benzyl]-6,8-dimethylpurin]-2-yl-3-oxypropyl]pyridine N-oxide, drugs containing the same and a compound useful as an intermediate in the production of this dihydrate.

Abstract: Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.

Abstract: Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.

Abstract: This invention relates to compounds, pharmaceutical compositions, and methods for the treatment or prevention of neural or cardiovascular tissue damage related to cerebral ischemia and reperfusion injury in an animal by administering Poly(ADP-ribose) polymerase (“PARP”) inhibitors.

Abstract: The present invention relates to an acyclic nucleoside phosphonate derivative which is useful as an antiviral agent (particularly, against hepatitis B virus), pharmaceutically acceptable salts, stereoisomers, and a process for the preparation thereof.

Abstract: In accordance with the present invention there is provided a nucleoside analogue of formula (I) or (Ia) which is useful as an antiviral agent.

Abstract: The present invention relates to cosmetic compositions containing a biotin compound and/or a complexing agent, one and/or the other bearing at least one reactive chemical function allowing covalent attachment to the hair, at least one cosmetic active agent being covalently attached to one of these two compounds, or to both of them.

Abstract: Pharmaceutical compositions for treating bone lesions in multiple myeloma or pharmaceutical compositions for treating multiple myeloma which contain as an active ingredient a compound having both of an effect of suppressing bone resorption accompanying multiple myeloma and an effect of inhibiting multiple myeloma, more particularly, 1-hydroxy-2-(imidazo[1,2-a]pyridin-3-yl)ethane-l,l-bisphosphonic acid or its salt.

Abstract: Novel pyridopyrimidine-based compounds are found to be useful for the treatment or prevention of symptoms or manifestations associated with diseases or disorders affected by cytokine intracellular signaling.

Abstract: The present invention provides methods of treating smallpox and other poxvirus infections with a pharmaceutically effective amount of LY582563 or LY217896.

Abstract: Disclosed is triazolopurine derivatives represented by the general formula (I): wherein R1 and R2 are as defined in the description. This compounds exhibit affinity for adenosine A3 receptor and are therefore useful as the ingredient of pharmaceutical compositions.

Abstract: The invention relates to compositions and methods for use in treating skeletal system disorders in a vertebrate at risk for bone loss, and in treating conditions that are characterized by the need for bone growth, in treating fractures, and in treating cartilage disorders. More specifically, the invention concerns the use of NO-bisphosphonate assembly for enhancing bone growth.

Abstract: Compounds represented by the formula: 1

Abstract: A fluorescent nitrogenous base and nucleosides including the fluorescent nitrogenous base are provided. Nucleosides including the fluorescent nitrogenous base are capable of Watson-Crick base pairing with naturally occurring nucleosides. The nucleosides including the fluorescent nitrogenous base have many uses including but not limited to use in probes, in the synthesis of nucleic acids, and in investigating nucleic acid interactions with other nucleic acids and/or with proteins.

Abstract: A method of treating a patient suffering from or susceptible to ischemic heart disease, peripheral vascular disease or stroke or which subject is suffering pain, a CNS disorder or sleep apnea which comprises administering a therapeutically effective amount of an adenosine derivative which is an agonist at the adenosine A1 receptor and which exhibits little or no agonist activity of the A3 receptor.

Abstract: The present invention relates to compositions comprising analogues of purine nucleosides containing a ring-expanded (“fat”) heterocyclic ring, in place of purine, and an unmodified or modified sugar residue, pharmaceutically acceptable derivatives of such compositions, as well as methods of use thereof. In particular, these compositions may be utilized in the treatment of certain cancers, bacterial, fungal, parasitic, and viral infections, including, but not limited to, Acquired Immunodeficiency Syndrome (AIDS), hepatitis, Epstein-Barr and cytomegalovirus.

Abstract: The present invention features methods for treating conditions of insulin resistance, hyperglycemia and/or diabetes. In a broad embodiment, the methods comprise the step of administering to a mammal in need of treatment a therapeutically effective amount of an ILK inhibitor. ILK inhibitors in accordance with the present invention includes small molecules, antibodies, peptides, and antisense compounds. In one embodiment, antisense compounds in accordance with the present invention comprise antisense oligomers.

Abstract: This invention relates to methods for transdifferentiation of body tissues which can be used to generate specific cell types needed for regenerating organs or body parts, following cellular degeneration, injury or amputation. The present invention also describes the use of tissue transdifferentiation for treating cancer and autoimmune diseases.

Abstract: Antisense compounds, compositions and methods are provided for modulating the expression of phosphatidylinositol-4-phosphate 5-kinase, type II beta. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding phosphatidylinositol-4-phosphate 5-kinase, type II beta. Methods of using these compounds for modulation of phosphatidylinositol-4-phosphate 5-kinase, type II beta expression and for treatment of diseases associated with expression of phosphatidylinositol-4-phosphate 5-kinase, type II beta are provided.

Abstract: Antisense compounds, compositions and methods are provided for modulating the expression of profilin 1. The compositions comprise antisense compounds, particularly antisense oligonucleotides, targeted to nucleic acids encoding profilin 1. Methods of using these compounds for modulation of profilin 1 expression and for treatment of diseases associated with expression of profilin 1 are provided.

Abstract: The present application is directed to pyrazolopyrirnidine and furopyrimidine analogs of the formula (I) 1

Abstract: Compositions are provided for delivery of polynucleotides to cells for the purpose of inhibiting gene expression. Antisense polynucleotide-containing complexes are described. The salt and serum stability and small size of the complexes permits delivery to cells in vitro and in vivo.

Abstract: The invention is based on the discovery that compounds of Formula I are unexpectedly highly potent and selective inhibitors of the adenosine A1 receptor. Adenosine A1 antagonists can be useful in the prevention and/or treatment of numerous diseases, including cardiac and circulatory disorders, degenerative disorders of the central nervous system, respiratory disorders, and many diseases for which diuretic treatment is suitable.

Abstract: The present invention provides novel compounds of the Formula (I) its prodrug forms, or pharmaceutically acceptable salts thereof. Preferred (I) compounds of the present invention comprise a pyrrolo pyridinyl, pyrrolo pyrimidinyl or indole nucleus. The compounds of this invention are inhibitors of Factor Xa (FXa), Factor VIIa (FVIIa) and/or serine proteases, Urokinase (uPA), and have utility as anti-coagulants for the treatment or prevention of thromboembolic disorders in mammals and as anticancer agents.

Abstract: In accordance with the present invention there is provided a method for treating or preventing a Flaviviridea viral infection in a host comprising administering a therapeutically effective amount of at least one compound of formula (I) or (II) 1

Abstract: The invention provides antisense antiviral compounds and methods of their use in inhibition of growth of viruses of the picornavirus, calicivirus, togavirus, coronavirus, and flavivirus families, as in treatment of a viral infection. The antisense antiviral compounds are substantially uncharged oligomers having a targeting base sequence that is substantially complementary to a viral target sequence which spans the AUG start site of the first open reading frame of the viral genome.

Abstract: The application is related to the field of nucleic acids with identified utility, and more particularly, to genes, related nucleic acids, their complements, polypeptides, and methods of using the same for blood vessel, cartilage, and bone formation, as well as inhibition thereof. The application describes discoveries made using the zebrafish embryo technique, as well as other techniques that are described herein. The discoveries include genes, related nucleic acids, and their complements, as well as sequences, polypeptides, other molecules, and methods for using them, e.g., TDE1, PTV, MOESIN, and HKE4. Also described are polypeptide products, inhibition of expression, administration of materials and products, screening procedures, and techniques for making drugs. Moreover, uses of these discoveries in appropriate contexts are set forth.

Abstract: Resolved enantiomers of the formula (IA) and (IB) wherein B is a purine or pyrimidine base or aza and/or deaza analogs thereof are useful in antiviral pharmaceutical compositions to treat retroviral infections.