Abstract: The present invention relates to an amorphous solid dispersion with improved stability comprising 9-[2-[[bis[(pivaloyloxy)methyl]phosphono]methoxy]ethyl]adenine as a nucleotide analogue, a pharmaceutical composition comprising the same, and a method for preparing the same.

Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable faints thereof according to wherein all of the variables are defined herein.

Abstract: The present invention provides compounds having the following Formula IA and IB, which are useful as MCHR1 antagonists, and includes prodrugs and pharmaceutically acceptable salts thereof:

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: 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: A compound of formula 1 and/or its salts, tautomers or solvates is used to treat hematological malignancies. In an embodiment, an organic acid salt of compound 1 is provided for general use in treatment of neoplasms, and in a further embodiment the salt is stabilized with carbohydrate.

Abstract: A method and compound for treating skeletal muscle mass deficiency in a human subject are disclosed. The composition is an oligomer of morpholino subunits and phosphorus-containing intersubunit linkages joining a morpholino nitrogen of one subunit to a 5? exocyclic carbon of an adjacent subunit, contains between 10-40 nucleotide bases, has a base sequence effective to hybridize to an expression-sensitive region of processed or preprocessed human myostatin RNA transcript, identified, in its processed form, by SEQ ID NO:6, and is capable of uptake by target muscle cells in the subject. In practicing the method, the compound is administered in an amount and at a dosage schedule to produce an overall reduction in the level of serum myostatin measured in the patient, and preferably to bring the myostatin level within the a range determined for normal, healthy individuals.

Abstract: A tablet for insertion into a vagina including 0.01 to 500 mg of a vaginal medication, such as a microbicide, such as cellulose acetate 1,2-benzenedicarboxylate (CAP); 100 to 500 mg of mannitol powder; 50 to 300 mg of inert microcrystalline cellulose; 10 to 80 mg of hydroxypropyl methylcellulose; 50 to 250 mg of glycerol and optionally 2 to 4 mg of at least one preservative which protects against microbicidal contamination and discourages the growth of yeast in the vagina. The tablet which includes CAP as the vaginal medication is vaginally administered before coitus in methods for preventing the sexual transmission of HIV-1, HIV-2, herpesvirus, or an infection caused by Neisseria gonorrhoeae, Chlamydia trachomatis, Trichomonas vaginalis, Haemophilus ducreyi or Treponema pallidum. The tablet which includes CAP as the vaginal medication is vaginally administered to prevent or treat bacterial vaginosis.

Abstract: Disclosed are prodrugs of A2B adenosine receptor antagonists, and their use in treating mammals for various disease states.

Abstract: This application relates to a purine derivative and pharmaceutical compositions which are useful for treating a hepatitis B viral infection or a hepatitis C viral infection.

Abstract: The use of enhancers with possibly riboflavin, as well as the corresponding compositions for the treatment of keratoconus or other ectasic corneal disorders by the method of corneal cross-linking.

Abstract: It has been discovered that certain natural mRNAs serve as metabolite-sensitive genetic switches wherein the RNA directly binds a small organic molecule. This binding process changes the conformation of the mRNA, which causes a change in gene expression by a variety of different mechanisms. Modified versions of these natural “riboswitches” (created by using various nucleic acid engineering strategies) can be employed as designer genetic switches that are controlled by specific effector compounds. Such effector compounds that activate a riboswitch are referred to herein as trigger molecules. The natural switches are targets for antibiotics and other small molecule therapies.

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: The present invention relates to formulations of nucleotide reverse transcriptase inhibitors (NRTIs), preferably [2-(6-Amino-purin-9-yl)-1-methyl-ethoxymethyl]-phosphonic acid (tenofovir, PMPA), or a physiologically functional derivative thereof, suitable for topical application and their use in the prevention of HIV infections.

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: Disclosed herein are Aurora kinase Inhibitors represented by Structural Formula (I): Values for the variables in Structural Formula (I) are defined herein.

Abstract: Described herein are pyrrolo[2,3-d]pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing these compounds, and methods for their preparation.

Abstract: An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastric diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, etc. This problem can be solved with a pyrrolopyrimidine or pyrrolopyridine derivative substituted with a cyclic amino group represented by formula [I] below which has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.

Abstract: The present disclosure provides biologically active 2,4-pyrimidinediamine compounds of formulae (I)-(III): and salts thereof, compositions comprising these compounds, and methods of using these compounds in a variety of applications.

Abstract: The present invention relates to formulations of nucleotide reverse transcriptase inhibitors (NRTIs), preferably [2-(6-Amino-purin-9-yl)-1-methyl-ethoxymethyl]-phosphonic acid (tenofovir, PMPA), or a physiologically functional derivative thereof, suitable for topical application and their use in the prevention of HIV infections.

Abstract: The present invention provides a PEGylated and fatty acid grafted chitosan oligosaccharide comprising a structural unit represented by the following Formula (I) and a structural unit represented by the following Formula (II) and synthesize method, wherein the chitosan oligosaccharide has a molecular weight of less than 200,000 Da, and a degree of deacetylation of 70%-100%, and part of free amino groups of chitosan oligosaccharide chain are replaced by a fatty acid or PEG, where n refers to degree of polymerization of the PEG, and R is an alkyl group having 11-21 carbon atoms. The grafting ratio of fatty acids is 1%-50%, and the grafting ratio of PEG is 0.05%-50%. The present invention also comprise a pharmaceutical composition comprising the PEGylated and fatty acid grafted chitosan oligosaccharide as a carrier, and use of the PEGylated and fatty acid grafted chitosan oligosaccharide in preparation of a pharmaceutical composition.

Abstract: The present invention is directed to the following: methods of treating or preventing stent thrombosis using pharmaceutical compositions comprising cangrelor and optionally bivalirudin; methods of reducing mortality in a subject undergoing stent implantation using pharmaceutical compositions comprising cangrelor and optionally bivalirudin; medicaments comprising cangrelor and optionally bivalirudin useful for treating or preventing stent thrombosis, or useful for reducing mortality in a subject undergoing stent implantation; pharmaceutical compositions comprising cangrelor and bivalirudin; and methods of preparing a medicament comprising cangrelor and optionally bivalirudin useful for treating or preventing stent thrombosis, or useful for reducing mortality in a subject undergoing stent implantation.

Abstract: The embodiments provide compounds of the general Formula I and compound 105S, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.

Abstract: Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.

Abstract: Anti-herpetic material such as 2-amino purine derivatives to prevent or treat autoimmune disease or a disease originating from an abnormal functioning of the sympathetic chain in a human subject. The disease is often of a tissue or organ associated with decreased blood flow to the tissue or organ (correlated with hypertonicity of the vessels feeding the tissue or organ). The treatment reduces inflammation, scarring, destruction, and pain in the tissue or organ affected and returns the tissue or organ to nearly normal functioning, while showing none of the side effects of previous treatments. Prolonged use of the anti-herpetic compounds reduces prodrome, vesicle formation and viral shedding. The anti-herpetic compounds may be administered alone or in combination with a compound that reduces the rate of renal excretion of the anti-herpetic compound. The anti-herpetic compounds are particularly useful when administered at a level equivalent in activity to 250 mg/kg famciclovir per day.

Abstract: There is provided a pharmaceutical composition comprising an antimycotic agent and an antiviral agent, useful for prophylaxis and/or treatment of an associated infection and/or disease and a method of manufacturing thereof.

Abstract: The present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of the formula: wherein R1, R2, R3, R5, R6 and R8 are each independently a member selected from the group consisting of H, C1-6 alkyl and OH; R4, R7 and R9 are each independently selected from the group consisting of C1-6 alkoxy and OH; R10 is a member selected from the group consisting of H, —OH, —OP(O)Me2, —O—(CH2)n—OH and —O—(CH2)m—O—(CH2)o—CH3, wherein subscripts n and m are each independently from 2 to 8 and subscript o is from 1 to 6; each of L1 and L4 are independently selected from the group consisting of: each of L2 and L3 are independently selected from the group consisting of: and salts, hydrates, isomers, metabolites and prodrugs thereof.

Abstract: An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be involved, such as depression, anxiety, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastric diseases, drug dependence, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, cephalic external wound, inflammation, immunity-related diseases, alopecia, irritable bowel syndrome, sleep disorders, epilepsy, dermatitides, schizophrenia, etc. This problem can be solved with a pyrrolopyrimidine or pyrrolopyridine derivative substituted with a cyclic amino group represented by formula [I] below which has a high affinity for CRF receptors and is effective against diseases in which CRF is considered to be involved.

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 shows that cilostazol, a phosphodiesterase 3 inhibitor has additional beneficial effects to atorvastatin on myocardial remodeling by inducing and preserving eNOS phosphorylation. The present invention demonstrates a cardioprotective effect of Cilostazol indicating the therapeutic potency of this drug. In addition, the present invention demonstrates that the additional effect of Cilostazol and atorvastatin therapy against ischemia injury is due to the augmentation of phosphatodylicositol 3-kinase/AKT (PI3-/AKT), PKA and p-eNOS signaling.

Abstract: The present invention is directed to phosphonic acid compounds useful as serine protease inhibitors, compositions thereof and methods for treating inflammatory and serine protease mediated disorders.

Abstract: A method of treatment of: i) HIV-1 infections in mammals, including humans; or ii) HBV infections in mammals, including humans; which method comprises the administration to the human in need of such treatment, an effective amount of the (R)-enantiomer of the triphosphate of a compound of formula (A) or a pharmaceutically acceptable salt thereof; and compounds for use in the method.

Abstract: Compounds of the following formula are provided for use with kinases: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.

Abstract: The present invention provides sustained-release opiate compositions. In particular, the present invention provides sustained-release opiate compositions that include an opiate attached to a blood albumin binder. The present invention also relates to methods of administering an opiate with a sustained release pharmacokinetic profile.

Abstract: The invention provides compounds that inhibit CK2 and/or Pim kinases and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, infections, and certain immunological disorders.

Abstract: A process for the synthesis of bisfuran intermediates of formula (0) useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed. Furthermore disclosed is a HIV protease inhibitor of formula (IV) as well as various intermediates thereof.

Abstract: The invention relates to (among other things) oligomer-nitrogenous base conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over unconjugated nitrogenous base compounds.

Abstract: Disclosed are compounds and compositions of Formula (I), pharmaceutically acceptable salts and solvates thereof, and their preparation and uses for treating viral infections mediated at least in part by a virus in the Flaviviridae family of viruses:

Abstract: Disclosed are compounds and compositions of Formula (I), pharmaceutically acceptable salts and solvates thereof, and their preparation and uses for treating viral infections mediated at least in part by a virus in the Flaviviridae family of viruses:

Abstract: The invention provides a novel class of compounds, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 7. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine.

Abstract: Intravaginal drug delivery devices, including intravaginal rings, are provided herein. The devices comprise a polyether urethane composition and a pharmaceutically effective amount of at least one vaginally administrable drug homogeneously distributed throughout the polyether urethane. The devices are capable of exhibiting a substantially zero order release profile of drug over extended periods of time. Also disclosed are methods for making the devices and methods of using the devices to prevent or treat a biological condition.

Abstract: This invention relates to benzimidazole carbamates and (thio)carbamates corresponding to Formula I: Here, X1 and X2 are independently O or S, wherein at least one of X1 and X2 is O; Y1 and Y2 are independently O or S, wherein at least one of Y1 and Y2 is O; R1 is alkyl having from 1-4 carbon atoms; R2, R3, and R4 are independently hydrogen or a cation; R5 and R6 are independently hydrogen, halogen, alkyl (having from 1-8 carbon atoms), —OR7, —SR8, —CO—R9, —OSO2—Ar, or —S(O)R10; R7 is alkyl having from 1-8 carbon atoms; R8 is alkyl (having from 1-8 carbon atoms) or aryl; R9 is alkyl (having from 1-8 carbon atoms), cycloalkyl (having from 3-6 carbon atoms), or aryl; Ar is aryl; and R10 is alkyl (having from 1-8 carbon atoms) or aryl. The compounds generally are soluble and stable in water, and have antiparasitic (particularly anthelmintic) activity in vivo that is comparable to known water-insoluble benzimidazole carbamates (e.g., albendazole and fenbendazole).

Abstract: Pharmaceutical compositions for intravenous administration comprising the compound of Formula I or pharmaceutically acceptable salts, hydrates or prodrugs thereof are described herein. Methods of preparing the pharmaceutical compositions and methods for treating nausea and/or emesis with the pharmaceutical compositions are also described herein.

Abstract: Solid forms comprising a compound useful in the treatment, prevention and management of various conditions and diseases are provided herein. In particular, provided herein are solid forms comprising (2-carbamoyl-5-chloro-1H-indol-3-yl)-[3-((E)-2-cyano-vinyl)-5-methyl-phenyl]-(R)-phosphinic acid methyl ester, including salts thereof, having utility for the treatment, prevention and management of conditions and disorders including, but not limited to, human immunodeficiency virus infection.

Abstract: The present invention provides methods of treating human immunodeficiency virus (HIV) and/or hepatitis B virus (HBV) infection, including administering a compound described in the invention in an amount effective treat the HIV and/or HBV infection and at least substantially inhibit the development of resistance to said antiviral compounds in the subject. Pharmaceutical compositions are also provided.

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

Abstract: The present application provides methods and compositions for improving the bioavailability of a lipid-containing antiviral compound, and in particular, an antiviral lipid-containing compound. In one embodiment, pharmaceutically acceptable compositions are provided that include an antiviral lipid-containing compound, or salt, ester, or prodrug thereof and one or more bioavailability enhancing compounds, such as inhibitors of cytochrome P450 enzymes.

Abstract: The invention is related to phosphorus substituted anti-viral inhibitory compounds, 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: This invention relates to novel compounds that are azapeptides, and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel azapeptide compounds that are derivatives of the HIV protease inhibitor atazanavir sulfate. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administering HIV protease inhibitors. The invention also relates to the use of one or more of the disclosed compounds as reagents in analytical studies involving atazanavir.

Abstract: The Present Invention Provides Tenofovir Disoproxil Succinate, Tenofovir Disoproxil L-Tartrate, Tenofovir Disoproxil oxalate, Tenofovir disoproxil saccharate, Tenofovir disoproxil citrate, Tenofovir disoproxil salicylate and various solid forms thereof, methods for the preparation thereof and their use in pharmaceutical applications, in particular in anti-HIV medicaments. The forms of Tenofovir disoproxil can be used in combination with other anti-HIV medicaments such as Efavirenz and Emtricitabine.