Abstract: The invention relates to a new crystalline form II of N-benzoyl-staurosporine; compositions containing the same; processes for the preparation thereof; and the use of crystalline form II of N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans. The invention relates to the amorphous forms of N-benzoyl-staurosporine; compositions containing the same; processes for the preparation thereof; and the use of amorphous N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans.

Abstract: The compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof specifically binds CCR5, so it is useful for preventing and/or treating CCR5-related diseases, for example, various inflammatory diseases (asthma, nephritis, nephropathy, hepatitis, arthritis, rheumatoid arthritis, rhinitis, conjunctivitis, ulcerative colitis, etc.), immunological diseases (autoimmune diseases, rejection in organ transplantation, immunosuppression, psoriasis, multiple sclerosis, etc.), infectious diseases (infection with human immunodeficiency virus, acquired immunodeficiency syndrome, etc.), allergic diseases (atopic dermatitis, urticaria, allergic bronchopulmonary aspergillosis, allergic eosinophilic gastroenteritis, etc.), ischemic reperfusion injury, acute respiratory distress syndrome, shock accompanying bacterial infection diabetes cancer metastasis and so on.

Abstract: The invention relates to a combination comprising an Erb-B and VEGF receptor inhibitor; and one or more pharmaceutically active agents; pharmaceutical compositions comprising said combination; methods of treatment comprising said combination; processes for making said combination; and a commercial package comprising said combination.

Abstract: The present invention relates to the use of midostaurin, in free form or in pharmaceutically acceptable salt form in the manufacture of a pharmaceutical composition for the treatment of gastrointestinal stromal tumors, and to a method of treatment of warm-blooded animals, preferably humans, in which a therapeutically effective dose of midostaurin is administered to an animal suffering from said disease or condition.

Abstract: The present invention relates to ophthalmic depot formulations comprising an active agent, e.g. embedded in a pharmacologically acceptable biocompatible polymer or a lipid encapsulating agent, e.g. for periocular or subconjunctival administration.

Abstract: Solid composition comprising (a) an anionic surfactant in combination with a water-soluble and basic polymer, or (b) a cationic surfactant in combination with a water-soluble and acidic polymer, and (c) at least one poorly water-soluble pharmaceutically active ingredient, and solid or liquid dosage forms, especially tablets, coated tablets, capsules or suppositories or aqueous solutions comprising the solid composition. The surfactant/polymer system is soluble in water and solubilises the active ingredient so that good bioavailability with therapeutical quantities may be attained. Aqueous solutions are suitable for nasal, parenteral or ophthalmic treatments.

Abstract: This invention relates to staurosporine derivatives are effective when used in combination with ionizing radiation for the delay of progression or treatment of a proliferative disease, especially a disease associated with a PAX/FKHR translocation including a PAX3/FKHR translocation and a PAX7/FKHR translocation, more especially a solid tumor disease such as a Sarcoma, most especially an Alveolar Rhabdomyosarcoma.

Abstract: Compositions and methods are provided for the alleviation of pathology induced by traumatic brain injury.

Abstract: The present invention relates to the use of specific compounds related to the indolocarbazole K252a, for the preparation of pharmaceutical compositions for the treatment of various forms of cancer.

Abstract: The invention concerns benzodiazepine derivatives of formula wherein Y it is SO2 or NR, wherein R is H or C1-C6 alkyl; X is H, C1-C12 alkyl, —CO, —SO, —SO2, or —CO—R2, SO—R2, SO2—R2, wherein R2 is selected from H, C1-C12 alkyl, (C3-C8 cycloalkyl) C0-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C2-C6 alkoxycarbonyl, phenyl, benzyl, naphtyl, biphenyl, or heterocycle, each para-, meta- or ortho-substituted independently of each other with 0 to 3 substituents selected from halogen, —CN, —NH2, —OH, —NO2, COOR3, wherein R3 is selected from H, C1-C12 alkyl, (C3-C8 cycloalkyl) C0-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, or C2-C6 alkoxy carbonyl; phenyl, benzyl, naphtyl, biphenyl, or heterocycle n is 0-6; R4 is selected from H, OH, COOH, CN, C1-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, C2-C6 alkoxycarbonyl, —CO, —SO, —SO2, or —CO—R5, SO—R5, SO2—R2, —OCO—R5, OSO—R5, SO2—R5, COOR5, SOOR5, SO2OR5, NHR5, NHCOR5, NHSO2R5, SR5, SCOR5, wherein R5 is selected from H, C1-C6 alkyl, C1-C6 alkoxy, C2-C6

Abstract: The present invention relates to a method of treating a warm-blooded animal, especially a human, having Mixed Lineage Leukemia (MLL rearranged ALL) comprising administering to said animal a therapeutically effective amount of a staurosporine derivative, especially PKC412 or a pharmaceutically acceptable salt thereof, alone or in combination with further therapeutic measures, for example, those defined herein; to the use of a staurosporine derivative for the preparation of a medicament for the treatment of MLL rearranged ALL; and to a commercial package comprising a staurosporine derivative together with instructions for its use in the treatment of MLL rearranged ALL.

Abstract: The present invention relates to a method of treating non-small cell lung cancer with FLT-3 kinase inhibitor such as PKC412. The invention also relates to a pharmaceutical combination of a FLT-3 kinase inhibitor and an activator of permeabilization of the mitochondrial outer membrane, such as an activator of BAK. It also relates to the use of a pharmaceutical combination of an activator of permeabilization of the mitochondrial outer membrane and a FLT-3 kinase inhibitor for the treatment of non-small cell lung cancer and the use of such a pharmaceutical composition for the manufacture of a medicament for the treatment of same.

Abstract: A combination which comprises (a) a staurosporine derivative and (b) an agent effective in preventing, delaying or treating transplant rejection in which the active ingredients (a) and (b) are present in each case in free form or in the form of a pharmaceutically acceptable salt and optionally at least one pharmaceutically acceptable carrier; for simultaneous, separate or sequential use.

Abstract: The invention provides a pharmaceutical combination comprising: a) a pyrimidylaminobenzamide compound; and b) a Flt-3 inhibitor, and a method for treating or preventing a proliferative disease using such a combination.

Abstract: The present invention relates to novel 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) in which A, D, G, W, X, Y and Z are as defined above, to a plurality of processes for the preparation and to their use as pesticides and/or herbicides and/or microbicides. Moreover, the invention relates to selective herbicidal compositions comprising both the 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) and a crop plant compatibility-improving compound.

Abstract: Novel compounds according to general formula 1, wherein G1 is NR5R6 or a fused polycyclic group that are specific OT receptor agonists and/or V1a receptor antagonists. Pharmaceutical compositions comprising such compounds are useful in the treatment of, inter alia, primary dysmenorrhoea.

Abstract: The present invention relates to a homology model for PLK, and the use thereof in assays for the identification of small molecule PLK modulators. The invention further relates to PLK modulators identified by said assays, and their use in the treatment of PLK-related disorders such as proliferative disorders.

Abstract: The present invention relates to the use of a combination comprising (a) imatinib or a pharmaceutically acceptable salt thereof and midostaurin or a pharmaceutically acceptable salt thereof for the preparation of a medicament for the treatment of gastrointestinal stromal tumors, e.g. imatinib-resistant gastro-intestinal stromal tumors.

Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is

Abstract: Methods of using compounds having certain inhibitory effect to treat cancer are disclosed. More specifically, methods of using myosin light chain kinase inhibitor (MLCK) to treat cancer are disclosed. MLCK inhibitors may cause reduction in MLC-P and induce apoptosis in neoplastic cells and prevent and or inhibit the tumor growth.

Abstract: Selective antagonists of A2B adenosine receptors like those of formula I are provide. The compounds and compositions are useful as pharmaceutical agents.

Abstract: A process for micronization of pharmaceutically active agents.

Abstract: The invention provides a method for treating myeloproliferative disorders, myelodysplastic syndromes and other diseases, in which activation of JAK2 contributes to pathology, in a mammal comprising administering to the mammal an effective amount of a fused pyrrolocarbazole derivative wherein the fused pyrrolocarbazole derivative inhibits the activity of JAK2.

Abstract: Polyarylcarboxamide compounds of formula (I) are useful as lipid lowering agents.

Abstract: The present invention relates to compounds of formula (I): wherein Rv, R1, R2, Rx, Ry, R3, R4, R5, R6, Rz and v are as defined within; pharmaceutically acceptable salts, solvates, solvates or such salts and prodrugs thereof and their use as ileal bile acid transport (IBAT) inhibitors for the treatment of hyperlipidaemia. Processes for their manufacture and pharmaceutical compositions containing them are also described.

Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.

Abstract: The present invention relates to compounds of formula (I) wherein Rv, R1, R2, Rx, Ry, M, Rz, v, R3, R4, R5 and R6 are as defined within; pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as ileal bile acid transport (IBAT) inhibitors for the treatment of hyperlipidaemia. Processes for their manufacture and pharmaceutical compositions containing them are also described.

Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharma-ceutically acceptable acid addition salt thereof, wherein —a1?a2—a3?a4— is a bivalent radical wherein one or two of a1 to a4 are nitrogen and the remaining a1 to a4 are —CH?; —Z1—Z2— is a bivalent radical; —A— is a bivalent radical of formula —N(R6)—Alk2— or a 5, 6 or 7-membered saturated heterocycle containing one or two nitrogen atoms; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; Alk1 and Alk2 are optionally substituted C1-6alkanediyl; R5 is a radical of formula (d-1), (d-2), (d-3), (d-4), (d-5) wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y2 is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl

Abstract: A compound having the general formula and methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.

Abstract: Pharmaceutical compositions and methods for treating epithelial cancers and precancerous lesions employ indole carbazole compounds, such as staurosporine. Compositions containing these compounds are administered to a patient in an effective amount and may be administered topically.

Abstract: This invention describes compounds of Formula (I) which are modulators of potassium channels and are useful for treating conditions affected by abnormal potassium channel activity including erectile dysfunction and irritable bowel syndrome.

Abstract: The present invention relates to novel benzimidazole compounds that have useful antiviral activity. More specifically, the invention encompasses benzimidazole compounds that inhibit membrane fusion associated events such as viral transmission, reduce viral load or otherwise treat viral infections. The invention also encompasses the use of benzimidazole compounds as inhibitors of membrane fusion associated events, such as viral transmission. In another embodiment, the invention encompasses processes for making benzimidazole compounds, methods of using the benzimidazole compounds and compositions comprising the benzimidazole compounds. Finally, the invention provides methods for treating, preventing or ameliorating symptoms associated with respiratory infection, particularly that caused by Respiratory Syncytial Virus utilizing the novel benzimidazole compounds of the invention.

Abstract: Compounds comprising an indazolyl group and a thiazolyl group, preferably 7-substituted 3-(thiazol-2-yl)-1H-indazole compounds in which the indazolyl group and a thiazolyl group are each independently optionally substituted, are useful for the treatment or prophylaxis of bacterial infections in mammals. The compounds are believed to function by inhibiting gyrase B.

Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts or prodrugs thereof, are useful as kinase inhibitors, wherein Y is —C(?O)NR1—, —NR1C(?O)—, —NR1C(?O)NR1—, —NR1SO2—, —SO2NR1—, —C(?O)—, —OC(?O)—, or —CO2—; B is alkyl, substituted alkyl, alkenyl, substituted alkenyl, hydroxy, alkoxy, aryl, cycloalkyl, heteroaryl, and heterocyclo; or when Y is —C(?O)NR1—, B also may be selected from —C(?O)R8, —C(?O)NR8R9, and —CO2R8; R1 is hydrogen, C1-4alkyl, or substituted C1-4alkyl; R2 is hydrogen or C1-4alkyl; R3 is hydrogen, methyl, perfluoromethyl, hydroxy, methoxy, halogen, cyano, NH2, or NH(CH3); and R4, R5, R6, R7, R8, and R9 are as defined in the specification.

Abstract: The invention provides compounds of general formula (I) in which m, A, R1 and Ar have the meanings defined in the specification; a process for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.

Abstract: Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.

Abstract: Methods for modulating the activity of the mammalian FXR receptor. The methods include methods of treating a hyper- or hypocholesterolemic mammal comprising contacting the mammal with synthetic compounds having FXR receptor activity.

Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereon wherein —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a

Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein Alk1 is C1-6alkanediyl optionally substituted with hydroxy, C1-4alkyloxy or C1-4alkylcarbonyloxy; -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical; R4 is hydrogen or C1-6alkyl; A is a bivalent radical of formula —NR6-Alk2-(b-1), or -Npiperidinyl-(CH2)m (b-2) wherein m is 0 or 1; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is h

Abstract: The invention provides compounds of formula (1) wherein R1 is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or an alkoxy group having 1 to 6 carbon atoms; and R2 is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or an alkoxy group having 1 to 6 carbon atoms; and pharmaceutically acceptable salts thereof. The invention also relates to a process for obtaining the compounds, compositions containing them and their therapeutic use. The compounds display excellent activity against mammalian cancer cell lines.

Abstract: Compounds of Formula 8 are provided: 1

Abstract: Disclosed are nucleosides which are useful in dignosing and treating viral infections, for example, infections caused by hepatitis B virus (HBV), and herpes viruses including Epstein Barr virus.

Abstract: A non-aqueous, particle-forming, fused pyrrolocarbazole-containing composition is disclosed. Upon contact with an aqueous medium, the particle-forming composition spontaneously disperses into suspended particles, thereby forming a stable suspension that provides greatly improved bioavailability of orally administered fused pyrrolocarbazole compounds.

Abstract: The present invention provides an antitumor agent comprising a staurosporin derivative or a pharmaceutically acceptable salt thereof, as an active ingredient, which is represented by the general formula (I): wherein R1 represents hydrogen, hydroxy or lower alkoxy, R2 and R3 are the same or different and represent hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted lower alkenyl, substituted or unsubstituted lower alkynyl, substituted or unsubstituted aryl, a substituted or unsubstituted heterocyclic group, halogen, nitro, formyl, etc., R4 represents hydrogen, etc., R5 represents NR11AR12A (wherein R11A and R12A represent hydrogen, substituted or unsubstituted lower alkyl, etc.), provided that R2 and R3 are not simultaneously hydrogen.

Abstract: A class of pyrazino[2,3-d]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 5-position, a substituted alkoxy moiety at the 3-position, and a range of substituents at the 2-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 and/or &agr;5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

Abstract: This invention provides compounds of Formula (I): wherein R1 and R2 are independent substituents or are fused to form spirocyclic rings; R3, RC, and R4 are as defined herein; and R5 is a substituted benzene ring or a substituted five or six membered heterocyclic ring having in its backbone 1, 2, or 3 heteroatoms including O, S, SO, SO2 or NR6; or pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods using the compounds as antagonists of the progesterone receptor.

Abstract: A bis(5-aryl-2-pyridyl) compound represented by formula (1) or a salt thereof: wherein A is a substituted or unsubstituted aromatic hydrocarbon group or a substituted or unsubstituted aromatic heterocyclic group, and X is a group selected from the group consisting of moieties having formulas (2) to (5): wherein, in formula (2), m is an integer of 1 or 2; in formula (3), n is an integer of 1 to 6; and in formula (4), R is hydrogen or a lower alkyl group and p is an integer of 1 to 6.

Abstract: Pharmaceutical compositions and methods for treating epithelial cancers and precancerous lesions employ indole carbazole compounds, such as staurosporine. Compositions containing these compounds are administered to a patient in an effective amount and may be administered topically.

Abstract: The present invention provides a preventive or therapeutic agent of a new type for diabetes mellitus and diabetic complications on the basis of an adenosine A2 receptor antagonist action. A purine compound represented by the formula (I), its pharmacologically acceptable salt or hydrates thereof has an adenosine A2 receptor antagonistic action and is useful for prevention or therapy of diabetes mellitus and diabetic complications. In addition, adenosine A2 receptor antagonists having different structures from those of the compounds described above, for example KW6002, are also effective for prevention or therapy of diabetes mellitus and diabetic complications. In the formula, W is —CH2CH2—, or —CH?CH— or —C?C—; R1 is: (in the formula, X is hydrogen atom, hydroxyl group, a lower alkyl group, a lower alkoxy group, etc.; and R5 and R6 are the same as or different from each other and each represents hydrogen atom, a lower alkyl group, a cycloalkyl group, etc.) and the like; R2 is an amino group, etc.

Abstract: Compounds of the formula Ia or IB where A is a saturated or monounsaturated heterocyclic, 4 - to 8-membered ring which contains one or two nitrogen atoms, and their tautomeric forms, possible enantiomeric and diastereomeric forms, their prodrugs and possible physiologically tolerated salts are useful as inhibitors of the enzyme poly(ADP-ribose)polymerase.