Abstract: Compounds of general formula (I); or a stereoisomers, tautomers, pharmaceutically acceptable salts, or prodrugs thereof, wherein R1, R2, R3, R4, R5, R6, R8 and R9 are as defined herein, are useful for the treatment of diseases and conditions which are mediated by excessive or inappropriate Hsp90 activity such as cancers, viral infection and inflammatory diseases or conditions.

Abstract: Compounds according to formula (I), compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases. Formula (I): or a pharmaceutically acceptable salt, solvate, clathrate of hydrate thereof, wherein X is O or S(O)t; Ra is O or S.

Abstract: The invention pertains to methods for treating ectopic pregnancy. More particularly, the present invention relates to methods for treating unruptured ectopic pregnancy using a non-surgical method comprising the administration of an EGFR inhibitor alone or in combination with an anti-metabolite e.g. methotrexate (MTX). The methodology is potentially applicable to treatment of unruptured ectopic pregnancies of all sizes.

Abstract: The subject invention concerns materials and methods for treating oncological disorders in a person or animal using any agent or compound that inhibits uptake of glucose into a cell. The subject invention also concerns methods for inducing apoptosis and inhibiting the proliferation or survival of a cell. In one embodiment, the methods comprise administering an effective amount of an agent or compound that inhibits the activity of one or more glucose transporter proteins, such as Glut-1. An antibody that binds to and inhibits a glucose transporter protein can be used in the present methods.

Abstract: Compounds of formula I are provided: wherein Ar1 and Ar2 are substituted aromatic rings and L1 and L2 are independent divalent linking groups. The compounds are useful as platelet ADP receptor inhibitors, for treating thrombosis and for reducing the likelihood and/or severity of a secondary ischemic event in a patient.

Abstract: This invention relates to novel 4-aminoquinazolines, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of the EGFR and HER-2.

Abstract: The invention relates to a pharmacological action of a compound which functions as a PPAR? agonist on the barrier function of the corneal epithelium. A PPAR? agonist such as rivoglitazone, DRF-2593, GW-544 or BMS-298585 exhibits an excellent effect of enhancing the corneal epithelial barrier function in a test for enhancement of corneal epithelial barrier function, and therefore is useful as a preventive agent or a therapeutic agent for ocular infection or ocular unidentified complaint caused by a decrease in the corneal epithelial barrier function. Further, the PPAR? agonist can enhance the corneal epithelial barrier function of diabetic patients, patients with decreased corneal epithelial barrier function due to aging and patients who underwent refractive surgery such as PRK (photorefractive keratectomy) or LASIK (laser in situ keratomileusis) or cataract surgery.

Abstract: Embodiments herein provide compounds and methods of making and using such compounds for prevention and treatment of multidrug resistant bacteria. In particular, embodiments are directed to anti-bacterial agents from benzo[d]heterocyclic scaffolds for prevention and treatment of multidrug resistant bacteria.

Abstract: This invention relates generally to a therapeutic use of epidermal growth factor receptor inhibitors to reduce fibrosis, e.g., liver fibrosis, or pre-cirrhosis in a subject.

Abstract: The present invention relates methods for treating disease conditions selected from the list consisting of benign or malignant tumors, diseases of the airways and lungs, diseases of the gastrointestinal tract, the bile duct and the gall bladder by administration to a patient in need thereof of a therapeutically effective amount of a bicyclic heterocyclic groups of general formula wherein said substituents are as defined herein.

Abstract: The present invention is directed to two novel polymorph form (Form A and Form B) of lapatinib ditosylate, wherein Form A is the hydrate ditosylate salt of lapatinib, and Form B is anhydrate ditosylate salt of lapatinib. The present invention is further directed to amorphous form of lapatinib ditosylate and its solid dispersion. The present invention further provides processes for the preparation of Form A, Form B, Amorphous form and solid dispersion of lapatinib ditosyalte, and a pharmaceutical composition comprising the said forms. Form A and Form B were characterized by X-RPD, DSC, TGA and FT-IR, and can be prepared from recrystallizing lapatinib ditosylate in a mixture of tetrahydrofuran (THF) and water.

Abstract: The invention relates to quinazoline derivatives of formula (1) wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, —CH2—, —S—, —SO—, —SO2—, —NR7CO—, —CONR8—, —SO2NR9—, —NR10SO2— or —NR11— (wherein R7, R8, R9, R10 and R11 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl); R4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alkyl group may carry a terminal optionally substituted group sele

Abstract: Disclosed is a human serum albumin (HSA) linker and HSA linker with binding, diagnostic, and therapeutic agents conjugated thereto. Also disclosed is a conjugate in which the HSA linker is covalently bonded to amino and carboxy terminal binding moieties that are first and second single-chain Fv molecules (scFvs). Exemplified conjugates are useful, e.g., in reducing tumor cell proliferation, e.g., for therapeutic therapeutic applications. Also disclosed are methods and kits for the diagnostic and therapeutic application of an HSA linker conjugate.

Abstract: This invention relates to novel 4-aminoquinazolines and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering inhibitors of the EGFR and HER-2.

Abstract: A compound of general formula I wherein: Ra is a benzyl, 1-phenylethyl, or 3-chloro-4-fluorophenyl group; Rb is a dimethylamino, N-methyl-N-ethylamino, diethylamino, N-methyl-N-isopropylamino, N-methyl-N-cyclopropylamino, N-methyl-N-(2-methoxyethyl)amino, N-ethyl-N-(2-methoxyethyl)amino, bis(2-methoxyethyl)amino, morpholino, N-methyl-N-(tetrahydrofuran-3-yl)amino, N-methyl-N-(tetrahydrofuran-2-ylmethyl)amino, N-methyl-N-(tetrahydrofuran-3-ylmethyl)amino, N-methyl-N-(tetrahydropyran-4-yl)amino, or N-methyl-N-(tetrahydropyran-4-ylmethyl)amino group; and Rc is a cyclopropylmethoxy, cyclobutyloxy, cyclopentyloxy, tetrahydrofuran-3-yloxy, tetrahydrofuran-2-ylmethoxy, tetrahydrofuran-3-ylmethoxy, tetrahydropyran-4-yloxy, or tetrahydropyran-4-ylmethoxy group, or a tautomer, stereoisomer, or salt thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction med

Abstract: The present invention is directed to pharmaceutical compositions and methods of using combination therapies containing [4-(6-fluoro-7-methylamino-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl)-phenyl]-5-chloro-thiophen-2-yl-sulfonylurea, or a pharmaceutically acceptable salt thereof, for the treatment of thrombosis diseases.

Abstract: The present invention provides compounds of formula (I), their use as inhibitors of tubulin polymerization as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, n, m and X have defined meanings.

Abstract: It is found that compounds having PPAR? agonistic activity induced abnormal blood coagulation or muscular disorder. A pharmaceutical combination comprising vitamin K and a compound having PPAR? agonistic activity can prevent the abnormal blood coagulation. A pharmaceutical composition comprising vitamin K can prevent muscular disorder.

Abstract: The truncated ErbB2 receptor (p95ErbB2) is shown to differ from the full-length ErbB2 receptor in its association with other ErbB receptors. The truncated receptor preferentially associated with ErbB3, whereas full length ErbB2 heterodimerizes with either EGFR or ErbB3. Consistent with p95ErbB2 heterodimerization with ErbB3, it is shown that heregulin (an ErbB3 ligand) stimulates p95ErbB2 phosphorylation in breast cancer cell lines. Described herein are methods of identifying patients suitable for treatment with a p95ErbB2 inhibitor, and methods of treating such patients.

Abstract: There is described a pharmaceutical composition comprising dexanabinol, or a derivative thereof, in combination with a second therapeutic agent that targets BRAF or MEK, and a pharmaceutically acceptable adjuvant, diluent or carrier. There is also described a method of treating a patient suffering from melanoma and uses related thereto.

Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

Abstract: The disclosure relates to methods of using an adrenergic ?-1 receptor antagonist or its pharmaceutically acceptable salts for treating and/or preventing interstitial cystitis, overactive bladder or detrusor overactivity.

Abstract: The present invention relates to compounds of Formula I and pharmaceutically acceptable salts thereof, processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as anti-inflammatory agents.

Abstract: The invention relates to antibacterial compounds of formula I wherein one or two of U, V, W, and X represent N, the rest represent CH or, in the case of X, may also represent CRa wherein Ra is fluorine; R1 represents alkoxy, halogen or cyano; R2 represents H, CH2OH, CH2N3, CH2NH2, alkylcarbonylaminomethyl or triazol-1-ylmethyl; R3 represents H, or, when n is 1, R3 may also represent OH, NH2, NHCOR6 or triazol-1-yl; A represents CR4; K represents O, NH, OCH2, NHCO, NHCH2, CH2NH, CH2CH2, CH?CH, CHOHCHOH or CHR5; R4 represents H or together with R5 forms a bond, or also R4 can represent OH when K is not O, NH, OCH2 or NHCO; R5 represents OH or together with R4 forms a bond; R6 represents alkyl; m is 0 or 1 and n is 0 or 1; and G is as defined in the description; and to salts of such compounds.

Abstract: The present disclosure relates generally to methods for the detection and quantitation of the p95 component of HER2/neu (ERbB2). Such methods may comprise assaying the biological sample for expression of HER2 ICD; assaying the biological sample for expression of a HER2 ECD; quantitating an expressed amount of the HER2 ICD and an expressed amount of the HER2 ECD in the biological sample; and determining the amount of p95 expressed in the biological sample based on a difference between the expressed amount of the HER2 ICD and the expressed amount of the HER2 ECD. The methods of the present disclosure may be used to predict whether a subject will be responsive to a receptor tyrosine kinase inhibitor and/or may be used to select subjects for inclusion/exclusion in a clinical trial.

Abstract: The present invention relates to a pharmaceutical combination for the treatment of diseases which involves cell proliferation, migration or apoptosis of myeloma cells, or angiogenesis. The invention also relates to a method for the treatment of said diseases, comprising co-administration of effective amounts of specific active compounds and/or co-treatment with radiation therapy, in a ratio which provides an additive and synergistic effect, and to the combined use of these specific compounds and/or radiotherapy for the manufacture of corresponding pharmaceutical combination preparations.

Abstract: The disclosure relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. Also provided are pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. Provided are methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1B1 and allelic variants thereof. Finally, provided is a method for determining the efficacy of a compound as described herein in treating cancer.

Abstract: The present disclosure provides methods for determining if PTEN is elevated or reduced in one or more tumor cells relative to one or more normal cells in the same biological sample by obtaining a biological sample comprising one or more tumor cells and one or more normal cells; assaying the biological sample for expression of PTEN; quantitating an amount of PTEN expression in the one or more tumor cells and an amount of PTEN expression in the one or more normal cells; comparing the amount of PTEN expression in the tumor cells to the amount of PTEN expression in the normal cells; and determining that PTEN is elevated in the tumor cells where the amount of expression of PTEN is greater in the tumor cells as compared to the normal cells or determining that PTEN is reduced in the tumor cells where the amount of expression of PTEN is less in the tumor cells than in the normal cells.

Abstract: The present invention relates to new indazole inhibitors of tyrosine kinase activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions.

Abstract: Substituted quinazoline compounds of the following formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, and X are defined herein. It also discloses a pharmaceutical composition containing one of these compounds.

Abstract: This invention relates to compounds of the formula X) or XI) (X) (XI) wherein: each —R1, —R2 and —R3 is independently -Q1, —OH or —H, where at least one of —R1, —R2 and —R3 is not —H or —OH; each —R4 and —R5 is independently -Q2 or —H; each -Q1 is independently selected from: —F, —Cl, —RA, —ORA, —SH, —SRA, where each —RA is independently selected from methyl and ethyl, which may substituted by one or more fluoro or chloro groups; and each -Q2 is selected from: —F, —Cl, —RB, —ORB, —SH, —SRB, where each —RB is independently selected from methyl and ethyl, which may substituted by one or more fluoro or chloro groups; which are useful in the treatment of melanoma.

Abstract: The invention relates to substituted N-(4-oxo-3,4-dihydroquinazolin-2-yl)butanamid derivatives which modulate androgen receptors to treat conditions such as: osteoporosis, peridontal disease, bone fracture, frailty, and sarcopenia.

Abstract: This invention relates to novel quinazoline derivatives, and their pharmaceutically acceptable salts. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by inhibiting cell surface tyrosine receptor kinases.

Abstract: Disclosed are methods of treating breast cancer by administering to a mammal aminoflavone, and optionally one or more additional anti-cancer agents. According to example embodiments, the methods include methods of treating cancers resistant to endocrine therapy.

Abstract: A method of treating cancer is described including administration of a 4-quinazolineamine and at least one other anti-neoplastic agent as well as a pharmaceutical combination including the 4-quinazolineamines.

Abstract: Compositions and methods for the treatment and diagnosis of cancer are disclosed.

Abstract: An adjunctive accessory article (25) for controlled release of at least a single physiologically active agent form an indwelling medical device so equipped is provided. The article is configurable as a tubular element upon a portion of the indwelling medical device, with barriers or facilitating coverings overlaying the carrier in furtherance of the controlled release of the active agent. To the extent that requires, affixation means for stable placement upon an indwelling device are further contemplated. Finally, a variety of application systems are described in connection to deployment of sleeve articles upon a portion of an indwelling device.

Abstract: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.

Abstract: A quinazoline derivative of the Formula (I): wherein the substituents are as defined in the text for use in the production of an anti-proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm-blooded animal such as man.

Abstract: The present invention is related to a method and kit (or device) for the detection and/or the quantification of biomarkers related to tumorigenesis. Said method is advantageously used to propose or adapt an anti-tumoral therapeutic protocol to be administered to a subject. Furthermore, said method and kit (or device) are a technical platform for the identification of new compounds, which are preferably used at (a) specific step(s) of an anti-tumoral therapeutic protocol.

Abstract: The invention provides methods for identifying patients who will respond well to cancer treatment with a therapeutic regimen that comprises the use of a histone deacetylase inhibitor (HDACi) and one or more further chemotherapeutic agents. The invention also relates to methods of treating such patients with a therapeutic regimen comprising the use of a histone deacetylase inhibitor (HDACi) and one or more further chemotherapeutic agents.

Abstract: Disclosed herein are controlled-release formulations of a core comprising a core active agent (e.g., alfuzosin) and a wax excipient substantially coated with an extended-release coating.

Abstract: The invention provides compositions and methods for determining the likelihood of successful treatment with dual therapy such as lapatinib. The methods comprise determining the genomic polymorphism or expression level of a gene present in a predetermined region of a gene of interest and correlating the polymorphism or expression level to the predictive response. Patients identified as likely responsive are then treated with the appropriate therapy.

Abstract: The present invention provides an agent for preventing or treating a trastuzumab-resistant cancer, which contains one or more medicaments selected from a cofilin inhibitor, a PAK1 inhibitor, a LIMK inhibitor, a RHO inhibitor, a ROCK1 inhibitor and a ROCK2 inhibitor.

Abstract: The present application is generally directed to compounds, compositions and methods of combination therapy for the treatment of neoplastic disorders.

Abstract: The present disclosure relates to a method, kit and controls for detecting phosphorylated Tyr1248 in the c-erbB-2 protein as a predictor of breast cancer progression and as a predictor of therapeutic efficacy of drugs that inhibit both epidermal growth factor receptor and erbB2 protein kinases.

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof, wherein the groups R2, R3, R4, Q, X and Y are as defined in the specification, is useful in the treatment of bone conditions related to increased calcium depletion or resorption.

Abstract: A novel solid composition and methods for making and using the solid composition are provided. The solid composition comprises: (a) at least one active agent with a solubility of less than about 0.3 mg/ml in an aqueous solution with a pH of at most about 6.8 at a temperature of about 37° C.; and (b) a hydrophilic polymer matrix composition comprising: i) a hydrophilic polymer selected from the group consisting of METHOCEL™, POLYOX™ WSR 1105 and combinations thereof; and optionally ii) a hydrophobic polymer selected from the group consisting of Ethocel 20 premium; and (c) an alkalizer selected from the group consisting of calcium carbonate, magnesium oxide heavy and sodium bicarbonate; wherein the composition provides at least about 70% release of the active between about 7 to about 12 hours following oral administration.

Abstract: A pharmaceutical dosage form comprises a solid dispersion product of at least one tyrosine kinase inhibitor, at least one pharmaceutically acceptable polymer, and at least one pharmaceutically acceptable solubilizer.