Abstract: The present invention provides a composition comprising a nicotine-containing material and an anti-cancer agent usable in the treatment and/or prevention or reduction of the risk of cancer and precancerous conditions as well as for preventing or reducing the risk of cancer recurrence. Furthermore, a composition comprising a nicotine-containing material and an anti-inflammatory agent usable in the treatment and/or prevention or reduction of the risk of inflammation, is provided. The nicotine containing composition can also include both an anti-cancer agent and an anti-inflammatory agent A device for administering the composition of the present invention to subjects can be a cigarette, smoking pipe, smokeless tobacco, electronic cigarette, transdermal patch or the like.

Abstract: The present invention relates to a bifunctional hydroxy-bisphosphonic acid derivative of formula (I) below: or a pharmaceutically-acceptable salt thereof, a method for producing the same, pharmaceutical compositions containing the same, and the use thereof as a medicament, as well as a compound of formula (II) below: or a pharmaceutically-acceptable salt thereof, and the use thereof for producing a vectorized molecule of therapeutic or diagnostic purpose.

Abstract: The present invention features interferon-free therapies for the treatment of HCV. Preferably, the treatment is over a shorter duration, such as no more than 12 weeks. In one aspect, the therapies comprise administering at least two direct acting antiviral agents and ribavirin to a subject with HCV infection. For example, the therapies comprise administering to the subject effective amounts of therapeutic agent 1, therapeutic agent 2 (or therapeutic agent 3), an inhibitor of cytochrome P450 (e.g., ritonavir), and ribavirin.

Abstract: The present invention relates to compounds and compositions for use in the treatment or prevention of retroviral infections in felines, in particular cats, and to the use of said derivatives for the manufacture of a medicament for the treatment or prevention of feline leukemia virus (FeLV) infections occurring alone or together with feline immunodeficiency virus (FIV) infections in cats.

Abstract: The present invention relates to 2?-Fluoro-6?-methylene carbocyclic nucleosides, pharmaceutical compositions containing these nucleosides and their use in the treatment or prophylaxis of a number of viral infections and secondary disease states and conditions thereof, especially including Hepatitis B virus (HBV) and secondary disease states and conditions thereof (cirrhosis and liver cancer), Heptatitis C virus (HCV), Herpes Simplex virus I and II (HSV-1 and HSV-2), cytomegalovirus (CMV), Varicella-Zoster Virus (VZV) and Epstein Barr virus (EBV) and secondary cancers which occur thereof (lymphoma, nasopharyngeal cancer, including drug resistant (especially including lamivudine and/or adefovir resistant) and other mutant forms of these viruses, especially HBV.

Abstract: The present invention provides a compound of formula I; wherein R1 is an alkyl pyrazole or an alkyl carboxamide, and R2 is a hydroxycycloalkyl; or a pharmaceutically acceptable salt thereof, and compositions containing these compounds, for use to treat a brain tumor, particularly glioblastoma. The invention provides effective treatment of a brain tumor and can be used by oral administration of a compound of Formula I as further described herein. The invention also provides a method to treat a subject having a brain tumor such as glioblastoma, wherein the method comprises administering to the subject an effective amount of a compound of Formula I. Gene signatures correlated with successful treatment using these methods are also disclosed.

Abstract: The present invention is directed to compounds, compositions and methods for treating or preventing cancer and viral infections, in particular, HIV, HCV, Norovirus, Saporovirus, HSV-1, HSV-2, Dengue virus, Yellow fever, and HBV in human patients or other animal hosts. The compounds are certain 6-substituted purine monophosphates, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof. In particular, the compounds show potent antiviral activity against HIV-1, HIV-2, HCV, Norovirus, Saporovirus, HSV-1, HSV-2, Dengue virus, Yellow fever, and HBV.

Abstract: The invention features compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.

Abstract: The present invention is related to 2-amino-4-arylthiazole derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.

Abstract: In part, the present disclosure is directed to prodrug derivatives of (E)-N-methyl-N-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1, 8-naphthyridin-3-yl)acrylamide compounds with significant solubility and bioavailability profiles.

Abstract: The invention is directed to an intravaginal drug delivery device comprising at least one pharmaceutically active substance, and a polyurethane copolymer, wherein the copolymer has the structure according to formula (I): The invention is further directed to administering one or more pharmaceutically active substances to a patient in need thereof.

Abstract: The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.

Abstract: The present invention provides a quinolone compound that inhibits the chronic progression of Parkinson's disease or protects dopamine neurons from disease etiology, thereby suppressing the progression of neurological dysfunction, so as to prolong the period of time until L-dopa is administered while also improving neuronal function; the quinolone compound of the invention is represented by Formula (1): wherein: R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 represents substituted or unsubstituted phenyl or the like; R4 represents halogen or the like; R5 represents hydrogen or the like; R6 represents hydrogen or the like; and R7 represents hydrogen or the like.

Abstract: This invention is directed to a composition comprising dry granulated tenofovir DF and emtricitabine, and a method for making same. Dry granulation was unexpectedly found to be important in preparing a tenofovir DF containing composition suitable for inclusion in a combination dosage form containing emtricitabine, efavirenz and tenofovir DF.

Abstract: In accordance with this invention a novel pharmaceutical product containing efavirenz, emtricitabine and tenofovir DF are provided as a multicomponent unitary oral dosage form, component 1 comprising tenofovir DF (and, optionally, emtricitabine) and component 2 comprising efavirenz, wherein components 1 and 2 are in a stabilizing configuration. In preferred embodiments component 1 is made by dry granulation.

Abstract: A series of thieno[2,3-b]pyridine derivatives, attached at the 2-position to a substituted anilino moiety, which are substituted in the 3-position by a carbonyl group linked to a pyrrolidin-1-yl ring which in turn forms part of a heteroatom-containing fused bicyclic ring system, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.

Abstract: The invention features a method for treating patients who have an EGFR-driven cancer, which is, or has become, refractory to a tyrosine kinase inhibitor, such as eriotinib and gefitinib, by administering a compound of formula (I) to the patient. The invention also features treating EGFR-driven cancers having an EGFR mutation identified herein.

Abstract: The present invention relates to a combination therapy for treating an HIV infection or inhibiting integrase comprising (S)-6-(3-Chloro-2-fluorobenzyl)-1-(1-hydroxymethyl-2-methylpropyl)-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (“Compound A”) or a pharmaceutically acceptable solvate or salt thereof in combination with at least one other anti-HIV agent. In some embodiments of the present invention, the other anti-HIV agents are chosen from reverse transcriptase inhibitors and protease inhibitors. In certain embodiments of the present invention, the other anti-HIV agents are chosen from AZT, 3TC, PMPA, efavirenz, indinavir, nelfinavir, a combination of AZT/3TC, and a combination of PMPA/3TC. Since Compound A has a high inhibitory activity specific for integrases, when used in combinations with other anti-HIV agents it can provide a combination therapy with fewer side effects for humans.

Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.

Abstract: The present invention relates to compounds and methods for treating retroviral infections, HIV, Hepatitis B, and/or HTLV viral infections. Some compounds of the invention are described by formula I: or a pharmaceutically acceptable salt, stereoisomer, a diastereomer, an enantiomer or racemate thereof.

Abstract: The invention relates to a method of treatment or prophylaxis of demyelinating disease, in particular the neurodegenerative phase of demyelinating disease, which comprises administration of an acid sensing ion channel (ASIC) antagonist. The invention also relates to a pharmaceutical composition comprising an ASIC antagonist in combination with an additional therapeutic agent, in particular an anti-inflammatory or immunmodulatory agent.

Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain 3-substituted-4-oxo-3,4-dihydro-imidazo[5,1-d][1,2,3,5]tetrazine-8-carboxylic acid amide (collectively referred to herein as 3TM compounds). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit cell proliferation, and in the treatment of proliferative disorders such as cancer, etc., and methods of preparing such compounds.

Abstract: A conjugated compound of formula Q-Z—R4 wherein Q is a TLR7 and/or TLR8 agonist and Z—R4 is a lipid covalently linked to an amino acid or peptide coupled to a polyamine group, and a process for the manufacture of the conjugated compound, as well as a complex formed between the conjugated compound and a polyanionic molecule and a pharmaceutical composition containing the conjugated compound or complex. Also described is the use of the conjugated compound or complex in the treatment of infection, cancer or immune disorders or for use in vaccines.

Abstract: The present invention relates in general to the field of targeted drug delivery of anti-cancer drugs. More precisely, the present invention concerns polymer drug conjugates, namely, conjugates of poly(organo)phosphazenes and anti-cancer drugs, wherein the conjugates are suitable to selectively release anti-cancer drugs in tumor tissue. In addition, the present invention relates to a method for manufacturing such poly(organo)phosphazene molecule conjugates, to poly(organo)phosphazene molecule conjugates for use in medicine, in particular, to poly(organo)phosphazene molecule conjugates for use in the treatment of cancer, and to pharmaceutical compositions comprising such poly(organo)phosphazene molecule conjugates.

Abstract: The present invention relates to a crystalline form of tenofovir dipivoxil fumarate, a crystalline composition and a pharmaceutical composition comprising the crystalline form, and also to a process for preparing the same and the use for prophylaxis or treatment of a disease associated with a viral infection. The crystalline form has an X-ray powder diffraction pattern using Cu-K? radiation, expressed in terms of lattice spacing “d” comprising peaks at about 18.4714 ?, 5.0350 ?, 4.6380 ?, 4.5347 ?, 4.3838 ?, 4.2874 ? and 3.6304 ?.

Abstract: The invention generally relates to compositions and methods for treating hepatitis B virus infection. More particularly, the invention relates to treating hepatitis B virus infection and related conditions in humans using unique and synergistic combinations of lamivudine and adefovir that maximize favorable therapeutic outcomes while minimizing or preventing viral resistance, which commonly occurs from using lamivudine or adefovir alone, and reducing the side effects of adefovir.

Abstract: The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N+—O? or CR3; Y is N, N+—O? or CR3a; R1 and R2 are independently selected from hydrogen and various substituents as defined in the claims; or R1 and R2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R3 is selected from hydrogen and various substituents; and R3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.

Abstract: The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract: The present invention relates to therapeutic combinations of [2-(6-amino-purin-9-yl)-1-methyl-ethoxymethyl]-phosphonic acid diisopropoxycarbonyloxymethyl ester (tenofovir disoproxil fumarate, Viread®) and (2R, 5S, cis)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one(emtricitabine, Emtriva™, (-)-cis FTC) and their physiologically functional derivatives. The combinations may be useful in the treatment of HIV infections, including infections with HIV mutants bearing resistance to nucleoside and/or non-nucleoside inhibitors. The present invention is also concerned with pharmaceutical compositions and formulations of said combinations of tenofovir disoproxil fumarate and emtricitabine, and their physiologically functional derivatives, as well as therapeutic methods of use of those compositions and formulations.

Abstract: The present invention is related to 2-amino-4-arylthiazole derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.

Abstract: The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds, salts and hydrates of the prodrugs, compositions comprising the prodrugs, intermediates and methods for synthesizing the prodrugs and methods of using the prodrugs in a variety of applications.

Abstract: Iontophoresis for delivering ophthalmic compositions (in particular. collyriums) preferably containing riboflavin, or other cross-linking agents, designed to imbibe the corneal stroma in the practice of the corneal collagen cross-linking (CXL) for the keratoconus treatment, and the corresponding ophthalmic compositions adapted to be administrated by iontophoresis in the treatment of keratoconus by corneal collagen cross-linking. Additionally, an ophthalmic composition for the treatment of keratoconus by corneal iontophoresis characterized by the fact that it includes cross-linking agents having buffering properties and whose initial pH value is included between 5 and 6, and/or bio-enhancers, and/or photo-enhancers.

Abstract: This invention relates to specific compounds and their pharmaceutically acceptable salts of the general formula: wherein Q is —CR?CR?— and Ring A is an aryl, heteroaryl or heterocyclic ring or ring system. This invention also relates to pharmaceutical compositions comprising such specific compounds or their pharmaceutically acceptable salts and a pharmaceutically acceptable carrier or adjuvant.

Abstract: A medical device includes an implantable structure and a coating layer including a water-insoluble therapeutic agent and one or more additives selected from heparin, heparan sulfate, dextran and dextran sulfate, and physiologically-acceptable salts thereof. The one or more additives can be present in an amount effective to increase the rate of release of the water-insoluble therapeutic agent from the coating layer. The implantable medical device structure can be an expandable structure such as a balloon or stent. Also described are methods of making and using such implantable medical devices and coating layers.

Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.

Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:

Abstract: A method and antisense compound for inhibiting the growth of pathogenic bacterial cells are disclosed. The compound contains no more than 12 nucleotide bases and has a targeting nucleic acid sequence of no fewer than 10 bases in length that is complementary to a target sequence containing or within 10 bases, in a downstream direction, of the translational start codon of a bacterial mRNA that encodes a bacterial protein essential for bacterial replication. The compound binds to a target mRNA with a Tm of between 50° to 60° C. The relatively short antisense compounds are substantially more active than conventional antisense compounds having a targeting base sequence of 15 or more bases.

Abstract: Substituted 1-oxa-2,8-diaza-spiro[4,5]dec-2-ene compounds and processes for their production, the use thereof for producing pharmaceutical compositions, pharmaceutical compositions containing these compounds and methods of treatment using these compounds.

Abstract: Provided in some embodiments are compositions comprising a compound having a structure according to Formula A or Formula B: or a pharmaceutically acceptable salt, tautomer or hydrate thereof, where X2 is a bond or linker, X3 is bond or —PO4—, and X1, R1, R2, R3, and n are described herein. Also provided in some embodiments are methods for making and using such compounds and compositions.

Abstract: Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a compound relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.

Abstract: The present invention relates to new therapies to treat pain and related diseases, as well as pharmaceutical compounds for use in said therapies.

Abstract: The invention provides multilayer tablets that contain rilpivirine hydrochloride, emtricitabine, and tenofivir disoproxil fumarate. The tablets are useful for the treatment of HIV.

Abstract: The present invention provides an isolated HIV-1 mutant and isolated nucleic acid molecules comprising HIV-RT coding sequences harboring a novel mutation in the S68 codon, and in particular, deletions of the S68 codon. This novel deletion reduces the sensitivity of HIV to various nucleoside reverse transcriptase inhibitors. Methods of using this mutation for selecting effective antiretroviral agents in vitro and in vivo, methods for monitoring infection progression in HIV-infected individuals and methods for avoiding the emergence of and/or to treat individuals infected with HIV comprising mutations, including deletions, at the S68 codon of HIV-RT are provided.

Abstract: 2-aryl-4-quinolones are converted into phosphates by reacting with tetrabenzyl pyrophosphate to form dibenzyl phosphates thereof, which are then subject to hydrogenation to replace dibenzyl groups with H, followed by reacting with Amberlite IR-120 (Na+ form) to form disodium salts. The results of preliminary screening revealed that these phosphates showed significant anti-cancer activity. A novel intermediate, 2-selenophene 4-quinolone and N,N-dialkylaminoalkyl derivatives of 2-phenyl-4-quinolones are also synthesized. These novel intermediates exhibited significant anticancer activities.

Abstract: Compounds of formula (I) wherein A represents a nucleobase or a derivative thereof, n is equal to 0 or 1 and R?, R? are carbonic chain, and R10 is hydrogen or a carbonic chain for their use as antiviral agents.

Abstract: Compounds of Formula 1, as shown below and defined herein: and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by FAK.

Abstract: The present invention relates to phosphonated Rifamycins, and methods of making and using such compounds. These compounds are useful as antibiotics for prophylaxis and/or the treatment of bone and joint infections, especially for the prophylaxis and/or treatment of osteomyelitis.

Abstract: The invention features compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.

Abstract: The present invention relates to formulations of antiviral compounds, in particular [2-(6-amino-purin-9-yl)-1-methyl-ethoxymethyl]-phosphonic acid (tenofovir, PMPA), suitable for topical application, and to their use in the reduction of or prevention of acquisition and transmission of herpes simplex virus.

Abstract: This invention provides a combination of antagonists of the hedgehog signaling pathway with a BCR-ABL inhibitor. The combination of the present invention may be used for treating cancers known to be associated with protein tyrosine kinases such as, for example, Src, BCR-ABL and c-kit.