Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.

Abstract: Novel modified release pharmaceutical composition comprising at least one active agent(s); a polymer system in an amount less than about 80% w/w of the composition comprising at least two swellable pH independent polymers wherein at least one is hydrophilic; optionally other pharmaceutically acceptable excipients is provided. Process for preparation of such compositions and methods of using them is also provided. The compositions are formulated into suitable dosage forms that provide therapeutic concentrations of active agent for extended periods of time.

Abstract: Pharmaceutical sustained release composition comprising at least one active agent(s), or its tautomeric forms, analogues, isomers, polymorphs, solvates, or salts thereof; preferably an antiviral active agent is provided. Also provided is a process of preparation of such composition and method of using them. The sustained release compositions of the present invention are able to deliver the active agent in a desired manner for an extended period of time.

Abstract: The invention provides a compound for use in the prophylaxis or treatment of a disease state or condition mediated by protein kinase B, the compound having the formula (I): or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR5; J1-J2 is N?C(R6), (R7)C?N, (R8)N—C(O), (R8)2C—C(O), N?N or (R7)C?C(R6); A is an optionally substituted saturated C1-7 hydrocarbon linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, one of the carbon atoms in the linker group being optionally replaced by oxygen or nitrogen; E is a monocyclic or bicyclic carbocyclic or heterocyclic group or an acyclic group X-G wherein X is CH2, O, S or NH and G is a C1-4 alkylene chain wherein one of the carbon atoms is optionally replaced by O, S or NH; R1 is hydrogen or an aryl or heteroaryl group; R2 and R3 are each hydrogen, optionally substituted C1-4 hydrocarbyl or optionally substituted C1-4 acyl; or NR2R3 forms an imidazole g

Abstract: Disclosed are A1 adenosine receptor antagonists having the general formula The compounds are useful for treating various disease states, in particular disease states for which diuretic treatment is appropriate.

Abstract: The present invention provides compositions and methods for reversibly inhibiting S-adenosyl-L-homocysteine (SAH) hydrolase. The compounds of the present invention can be used as an anti-hemorrhagic viral infection agent, an immunosuppressant, a homocysteine lowering agent, or an anti-neoplasm agent. The compositions and methods of the present invention can be used for the prevention and treatment of hemorrhagic virus infection, autoimmune diseases, autograft rejection, neoplasm, hyperhomocysteineuria, cardiovascular disease, stroke, Alzheimer's disease, multiple sclerosis or diabetes.

Abstract: A method for reducing psychological opioid dependence includes selecting a patient addicted to an opioid and administering to the patient an opioid agonist-antagonist for at least 14 days, thereby reducing craving for the opioid in the patient. An opioid agonist-antagonist is administered in a patient needing an average adherence to a treatment protocol of at least 95 percent. A non-injectable formulation containing an agonist-antagonist also is disclosed.

Abstract: A pharmaceutical acceptable composition is provided. The composition comprises an effective amount of a non-steroidal anti-inflammatory drug (NSAID), a local anesthetic, and an antiviral drug.

Abstract: The invention encompasses a series of bicyclic heterocyclic compounds of Formula I which are inhibitors of HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.

Abstract: Provided are cyclobutyl nucleosides and methods for their use in treatment of infections including Retroviridae (including HIV), Hepadnaviridae (including HBV), or Flaviviridae (including BVDV and HCV) infection, or conditions related to abnormal cellular proliferation, in a host, including animals, and especially humans.

Abstract: Compounds useful in the treatment of autoimmune disease are described by the following general formula: n=0-2 m=0-2 m is not necessarily equal to n; where R1, R3?NH2, F, Cl, C1-C4 alkoxy or phenoxy group, but R1 is not necessarily equal to R3; and R2?H, F, Cl, NH2, or NH—R—XH; X?CH2,NH, O, or S.

Abstract: A modified release pharmaceutical composition of famciclovir contains at least 60% by weight famciclovir with at least 5% by weight of a release retardant. Particularly useful as a release retardant include polymers, especially a mixture of polyvinyl acetate and polyvinylpyrrolidone. A method of making such pharmaceutical compositions using a extruder and a granulation method is particularly useful.

Abstract: The subject invention provides novel compositions of biologically active compounds which can advantageously be used in blocking cellular proliferation and/or treatment of cancer.

Abstract: A pharmaceutical formulation for the treatment of HIV is provided. The formulation is a combination of a nucleoside reverse transcriptase inhibitor and a nucleotide reverse transcriptase inhibitor in which the combination has an increased stability over prior art combination therapies. The invention also provides a pharmaceutical product containing the formulation.

Abstract: Disclosed herein are compositions and methods for the treatment of skeletal muscle and/or the protection of skeletal muscle against injury. The adenosine A3 receptor has been identified as a new therapeutic target for the treatment of skeletal muscle. Adenosine A3 receptor agonists are used treat subjects with skeletal muscle ischemia and reperfusion (I/R) injuries, individuals with skeletal muscle disorders, and individuals suffering from skeletal muscle injury resulting from physical exertion.

Abstract: Provided herein is a method of protecting a neuron from dysfunction induced by an HIV neurotoxin, comprising contacting the cell with a therapeutically effective dose of a dopamine D1 receptor agonist. Also provided is a method of treating or preventing HIV-1 associated dementia (HAD) in a subject in need of such treatment or prevention, comprising administering to the subject a therapeutically effective dose of a dopamine D1 receptor agonist and estrogenic compound.

Abstract: The invention relates to a combination comprising a quinoline compound or its sail, according to general formula (I) and at least one HIV infection therapeutic agent selected from the group consisting of entry inhibitors, reverse-transcriptase inhibitors, strand-transfer inhibitors, protease inhibitors, and maturation inhibitors. Said combination has therapeutic synergy in the treatment of an HIV infection compared with the quinoline compound, or HIV infection therapeutic agent alone.

Abstract: Methods of treating an individual who has been identified as having glycolysis dependent cancer are disclosed. The methods comprise the step of: administering to such an individual a combination of an anti-cancer composition that renders the cancer incapable of glycolysis and an autophagy inhibitor. Pharmaceutical compositions and kits comprising that renders the cancer incapable of glycolysis and an autophagy inhibit are also disclosed. Methods of treating an individual who has a disease characterized b cell degeneration and cell death due to autophagy are disclosed. The methods comprise administering to the individual a permeable form of a metabolic substrate that can be oxidized in the tricarboxylic acid cycle to produce NADH. Methods for identifying an autophagy inhibitor comprising performing a test assay using an apopto sis-resistant cell are disclosed.

Abstract: Methods for treating and preventing middle ear infections by transmembrane administration of medicament-containing transmembrane carrier compositions comprising a chemical penetration enhancer, such as propylene glycol. The compositions are applied to the ear so as to contact the outer surface of an intact tympanic membrane to deliver the medicament across the membrane and into the middle ear. The medicaments delivered according to the methods of the invention include antibiotic, anti-viral, anti-fungal and anti-inflammatory agents that are useful in treatment and/or prophylaxis of middle ear infections and their sequelae.

Abstract: The invention relates to sulphonamidoanilines of formula I, wherein A is N or CH, W, X, Y and Z are N or CH under the proviso that at least one of the three symbols W, X and Y represent CH, R1 represents NR4R5 or OR4, wherein R4 represents optionally substituted alkyl, optionally substituted cycloalkyl optionally comprising one or two nitrogen or oxygen atoms, or substituted aryl, and R5 represents hydrogen or unsubstituted or substituted alky, or R4 and R5 together with the nitrogen to which they are attached represent an optionally substituted five- or six-membered nitrogen containing monocyclic ring, an optionally substituted nitrogen containing fully saturated bicyclic ring, or an spirocyclic fully saturated ring system containing one or two nitrogen atoms, R2 is hydrogen, lower alkenyl or alkyl, R3 is alkyl which is unsubstituted or mono-, di- or trisubstituted by halogen; alkenyl or aryl, and their salts; processes for their preparation, their application in the treatment of the human or animal body

Abstract: The present invention therefore provides a compound of formula (I) and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases S, K, F, L and B. Of particular interest are diseases associated with Cathepsin S. In addition this invention also discloses processes for the preparation of such inhibitors.

Abstract: A method of treating atherosclerosis in a subject is carried out by administering the subject 2-aminopurine or a pharmaceutically salt thereof in a treatment effective amount. Optionally, the subject may also be administered an additional hypolipidemic agent. Compositions useful for carrying out the present invention are also described.

Abstract: This invention is in the field of animal feed, more in particular in the field of fish feed. Surprisingly, it has been found that the seasonal mobility period of fish may be lengthened by interfering with the diet of the fish. We found that it is possible to increase the seasonal mobility period of fish to such an extent that it is even active at temperatures as low as 2 degrees Celsius. Such may be accomplished by adding naturally occurring substances to the feed of the fish. Examples of these naturally occurring substances are immune enhancing ingredients like beta-glucans and/or small amounts of phytohormones like auxin or gibberellic acid. Also, combinations of these substances, in particular the combination of beta-glucans and phytohormones, were shown to have a synergistic effect in that they lengthened the seasonal mobility period of the fish more than the individual components on their own.

Abstract: The present invention relates to HSP90 inhibitors and their use in the treatment of cell proliferative diseases such as cancer. The said derivatives may further act as HDAC inhibitors.

Abstract: Sustained release spherical or non-spherical pellets comprising (a) an active ingredient (b) a wax-like agent, and (c) a spheronizing agent are provided. Oral dosage forms comprising said pellets and methods for preparing and using such pellets and dosage forms are also provided.

Abstract: Compounds of formula I in free or salt form, wherein R1, R2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adenosine A2A receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.

Abstract: The present invention concerns combinations of a pyrimidine containing NNRTI with nucleoside reverse transcriptase inhibitors and/or nucleotide reverse transcriptase inhibitors useful for the treatment of HIV infected patients or for the prevention of HIV transmission or infection.

Abstract: The present invention provides compositions and methods for reversibly inhibiting S-adenosyl-L-homocysteine (SAH) hydrolase. The compounds of the present invention can be used in combination with an anti-hemorrhagic viral infection agent, an immunosuppressant, a homocysteine lowering agent, or an anti-neoplasm agent. The compositions and methods of the present invention can be used for the prevention and treatment of lupus, hemorrhagic virus infection, autoimmune diseases, autograft rejection, neoplasm, hyperhomocysteineuria, cardiovascular disease, stroke, Alzheimer's disease, or diabetes.

Abstract: Selective antagonists of A2A adenosine receptors like those of formula I are provided, wherein Y forms a ring. The novel A2A Blockers are useful for the treatment of Parkinson's disease and other diseases.

Abstract: The invention relates to substituted 9-alkyladenines of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1-R6 are defined as set forth in the specification. The invention is also directed to the use of such compounds to inhibit adenosine A1 receptor activation in a mammal. The compounds of the present invention are useful as diuretics, renal protectives against acute or chronic renal failure, as well as agents to improve the therapeutic outcome resulting from defibrillation or cardiopulmonary resuscitation by preventing post-resuscitation bradycardia, bradyarrythmia and cardioplegia, to restore cardiac function following a cardioplegic procedure, and to treat or prevent intermittent claudication.

Abstract: Compounds which are active against viruses have the following formulas: wherein B is a purine or pyrimidine heterocyclic ring or base. In a preferred embodiment, the purine include 6-aminopurine (adenine), 6-hydroxypurine (hypoxanthine), 2-amino-6-hydroxypurine (guanine), 2,6-diamino-purine, 2-amino-6-azidopurine, 2-amino-6-halo substituted purines such as 2-amino-6-chloropurine, 2-amino-6-fluoropurine, 2-amino-6-alkoxypurines such as 2-amino-6-methoxypurine, 2-amino-6-cyclopropylaminopurine, 2-amino-6-alkylamino or 2-amino-6-dialkylamino substituted purines, 2-amino-6-thiopurine, 2-amino-6-alkylthio substituted purines, 3-deazapurines, 7-deazapurines and 8-azapurines. The pyrimidine incorporates cytosine, uracil and thymine, 5-halo substituted cytosines and uracils, 5-alkyl substituted cytosines and uracils including derivatives with a saturated or unsaturated alkyl group and 6-azapyrimidines.

Abstract: Compounds represented by the formula: A is (CH2)nR2, —CH?CH2, CH2—CH?CH2, O(CH2)nR2, CH(OH)CH3, CH(OH)CH2OH, CH2—CH(OH)CH3, CH2CH(OH)CH2OH, or CH(OH)CH(OH)CH3, R,R1 individually is H, NH2OH, Cl, Br, I, aryl, substituted aryl, heterocycle, NR3R4, OR3 or SR3, R2 is H, OH, F, N3, NH2, CO2H, SH, alkyl, substituted alkyl, S-alkyl, O-acyl, CONH2, or CONH-alkyl, n is 1-3, y is O, S or NH, W is O or S, Z, Z? individually is OR3, OR4, O(CH2)m—O—(CH2)xCH3, NH—CH(alkyl)CO2R3, alkyl, substituted alkyl, OCH2CH2S—C(O)CH3, OCH2CH2S—C(O)CH(CH3)2, OCH2CH2S—C(O)C(CH3)3, OCH2CH2—SC(O)aryl, OCH2CH2—S—S—OCH2CH2OH, OCH2OC(O)C(CH3)3, OCH2—O—C(O)OCH(CH3)2, or OCH2—O—C(O)CH(CH3)2 R3, R4 individually is H, alkyl, substituted alkyl, aryl, or substituted aryl; Both R3 and R4 can form a monocyclic ring of 4-7 atoms with N or optionally a further heteroatom in the ring; m is 1-3, x is 0-19; and pharmaceutically acceptable salts thereof and prodrugs thereof are provided.

Abstract: PDE4 inhibition is achieved by novel compounds of the Formula I: wherein R1 and R2 are as defined herein.

Abstract: The invention relates to the inhibition of DNA methyltransferase isoforms DNMT1 and DNMT3b2. The invention provides compounds and methods for inhibiting DNMT1 and DNMT3b2.

Abstract: Novel purine compounds and tautomers and pharmaceutically acceptable salts thereof are described, as are pharmaceutical compositions comprising the same, complexes comprising the same, e.g., HSP90 complexes, and methods of using the same.

Abstract: The present invention relates to the use of an inhibitor of CDK2 and/or CDK7 and/or CDK9, or a pharmaceutically acceptable salt thereof, in the preparation of a medicament for treating a disease associated with antinuclear antibodies, wherein the inhibitor of CDK2 and/or CDK7 and/or CDK9 or pharmaceutically acceptable salt thereof is administered in an amount sufficient to down-regulate the levels of antinuclear antibodies. A further aspect of the invention relates to a combination comprising an inhibitor of CDK2 and/or CDK7 and/or CDK9, or a pharmaceutically acceptable salt thereof, and methylprednisolone, and its use in the treatment of diseases associated with antinuclear antibodies, such as SLE.

Abstract: PDE4 inhibition is achieved by novel compounds of the Formula I: wherein R1 and R2 are as defined herein.

Abstract: Purine derivatives of formula (IA1) or (IB1), compositions containing them and use thereof as medicinal products, in particular in oncology, are described

Abstract: This invention relates to methods of inhibiting the Hsp90 chaperone protein, and methods of treatment comprising administration of compounds of formula (IA) (IB) and (II)

Abstract: PDE4 inhibition is achieved by novel compounds of the Formula I: wherein R1 and R2 are as defined herein.

Abstract: PDE4 inhibition is achieved by novel compounds of the Formula I: wherein R1 and R2 are as defined herein.

Abstract: PDE4 inhibition is achieved by novel compounds of the Formula I: wherein R1 and R2 are as defined herein.

Abstract: The present invention relates to compounds of formula I wherein R1 is as defined in the specification and to esters thereof which are hydrolyzable under physiological conditions and to the pharmaceutically acceptable salts thereof. The compounds of the invention are inhibitors of COMT and, thus, are useful for the treatment of diseases for which COMT inhibition is beneficial. The invention further relates to the treatment, control, or prevention of diseases such as depression, schizophrenia, Parkinson's disease, and to improve cognition.

Abstract: The present invention provides methods and compositions for countering the adverse effects of aging on mammalian cells in vitro and in vivo, especially human skin cells and human skin, and treatment of hyperproliferative and related skin diseases in mammals by administering compositions containing 6,9-disubstituted purine derivatives.

Abstract: The use of adenosine-5?-triphosphate-2?,3?-dialdehyde (oATP) as a medicament useful for the treatment of inflammatory conditions is disclosed.

Abstract: A treatment for cancer using a combination therapy including an inhibitor of the PI3K/Akt pathway in combination with roscovitine. It is shown that the combination of roscovitine and API-2 (Triciribine) or roscovitine and LY294002 induce the apoptosis of androgen-dependent (LNCaP) and androgen-independent (PC3) prostate cancer cells. Two important results have been observed. First, cells that respond to roscovitine alone (LNCaP) initiate apoptosis sooner when co-treated. Second, cells that do not respond to roscovitine alone (PC3) apoptose when co-treated, although with delayed kinetics. In the absence of roscovitine, AKT inhibitors had no effect on LNCaP or PC3 survival, and in both cell lines, the combined treatment activated the mitochondrial pathway of apoptosis. Importantly, normal epithelial cells (RPWE) remained viable in the presence of roscovitine and AKT inhibitors.

Abstract: Heterocyclic derivatives based on N6-substituted adenine of, e.g.,a formula: wherein R2 is hydrogen, R6 is R6?-X, X is —NH—, and R6? is substituted phenyl or substituted benzyl. The derivatives possess anticancer, mitotic, imunosuppressive and antisenescent properties for plant, animal and human cells, and methods of their preparation are disclosed. Included are also pharmaceutical compositions, cosmetic preparations and growth regulators, which contain these derivatives as active compound and the use of these derivatives for the preparation of drugs, cosmetic preparations, in biotechnological processes, in cosmetics and in agriculture.

Abstract: Famciclovir monohydrate and its pharmaceutical use.

Abstract: The present invention provides compositions and methods for differentiating and transdifferentiating mammalian cells into cells of an osteoblast lineage, using compounds of the following formula: wherein R4 is a functional group including, for example, C1-4alkyl, C3-8cycloalkyl, hydroxyl-C1-4alkyl, aryl-C0-3alkyl, substituted with 0-2 R4a groups, and heterocyclo-C0-2alkyl, optionally substituted with C1-4alkyl; R5 is hydrogen and R6 is a functional group including, for example, halogen, C1-4alkyl, —C(O)—C1-4alkyl, —SO2—N(R2b R2b), halo—C1-4alkyl, —O-aryl and —N(R7 R8), or when R5 and R6 are on adjacent ring atoms they are optionally taken together to form —O—(CH2)1-2—O—; and all pharmaceutically acceptable salts and hydrates thereof.

Abstract: A mammal undergoing an energy-based therapy is treated by administering at least one vasoconstrictive agent to the mammal prior to or during the procedure. The at least one vasoconstrictive agent is added in amounts sufficient to reduce or prevent vasodilation. This treatment method increases or promotes the size of the coagulation zone created after energy-based therapy.