Abstract: A compound of formula (I), or stereoisomers or pharmaceutically acceptable salts thereof, wherein, R1a, R1b, R2a, R2b, U1, U2, X1, X2 and L are as defined herein.

Abstract: Presented are mechanism based compositions and methods for treatment of SCD and SCD associated symptoms and disorders, particularly increased RBC sickling, HbS polymerization, hemolysis, tissue congestion and disruption and organ damage or failure in a mammal. The disclosed methods feature the identification of the heretofore unknown role of adenosine levels and signaling in the development of SCD and SCD associated symptoms and disorders. This discovery has lead to the identification of compositions for use as therapies for SCD and SCD associated disorders and symptoms in a mammal.

Abstract: Compositions and methods to treat lymphoma and cancer are disclosed. In particular, the method teaches treatment of lymphoma and cancer using anti-HERV-K(HML-2) therapies. Further taught are compositions and methods for characterizing patient samples to, for example, select or identify therapeutic options or assess the impact of therapies.

Abstract: A compound of formula (I), or stereoisomers or pharmaceutically acceptable salts thereof, formula (1), or stereoisomers or pharmaceutically acceptable salts thereof, wherein A, U1, U2, R1a, R1b, 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: 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 scleroderma, keloids, UV injury, or sunburn, and methods for improving or preventing scar formation.

Abstract: The invention relates to compounds, pharmaceutical compositions, and uses thereof, including therapeutic uses thereof, such as methods useful for treating cancer.

Abstract: This invention relates to novel compounds having the formula (I): and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.

Abstract: Ischemia-reperfusion injury remains a primary cause of morbidity and mortality in individuals who experience disruption of normal blood flow to one or more major organs. For example, there are no clinically proven strategies that prevent acute renal failure following cardiac surgery. The present invention provides a variety of methods for the treatment or prevention of ischemia-reperfusion injury. In one aspect of the invention, a method for treating or preventing ischemia-reperfusion injury includes administering to a subject an effective amount of a sphingosine kinase inhibitor. Sphingosine kinase inhibitors are very effective in the protection against IR-induced acute renal failure and liver failure. Moreover, the effects occur very early after administration, requiring only a very short time of treatment. Toxicology studies with sphingosine kinase inhibitors demonstrate that they have low toxicity, even in long-term treatment.

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: This invention provides 2-, 6, and 9-substituted purine derivatives, particularly 2(1-R hydroxymethylpropylamino)-6-benzylamino-9-isopropyl purine, having, in particular, antiproliferative properties, and suitable for use as pharmaceutical compositions and herbicidal compositions. Also provided are pharmaceutical compositions and herbicidal compositions comprising the 2-, 6, and 9-substituted purine derivatives, and methods of treatment using the 2-, 6, and 9-substituted purine derivatives.

Abstract: Methods for treating diseases in humans and vertebrate animals are provided using competitive antagonists of cellular metabolites combined with a protective agent for protecting host cells from toxic effects of the drugs. Also provided are kits comprising competitive antagonists and suitable protective agents. In addition, screening methods for identifying competitive antagonists, protective agents and potentiating agents, for use according to the methods of the invention, are provided.

Abstract: The invention provides compounds having the following general formula (I): wherein X, R1, R2, R7 and Z are as described here.

Abstract: A method for the treatment of recurrent herpes labialis in mammals, including humans, which method comprises administering to the mammal in need of such treatment, an effective amount of penciclovir or famciclovir, or a pharmaceutically acceptable salt thereof for a period of one day.

Abstract: HIV replication inhibitors of formula N-oxides, pharmaceutically acceptable addition salts, quaternary amines or stereoisomeric forms thereof, wherein -a1=a2-a3=a4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; -b1=b2-b3=b4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; n and m is 0, 1, 2, 3 and in certain cases also 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalomethylthio; —S(?O)pR6; C(?NH)R6; R2a is CN; amino; substituted amino; optionally substituted C1-6alkyl; halo; optionally substituted C1-6alkyloxy; substituted carbonyl; —CH?N—NH—C(?O)—R16; optionally substituted C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(?N—O—R8)—C1-4alkyl; R7 or —X—R7; R3 is CN; amino; C1-6alkyl; halo; optionally substituted C1-6

Abstract: The present invention relates to the oral solid pharmaceutical composition comprising lamivudine or a pharmaceutically acceptable salt thereof with isomalt as a filler. The present invention also relate to the combination of lamivudine and other Anti-HIV agents. Thus, for example, the present invention provides a stable tablet formulation comprising lamivudine, isomalt, crospovidone, calcium stearate and opadry white.

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: Methods of inhibiting cancer cell growth using HDAC10 inhibitors are provided. Methods of treating cancer in a subject using HDAC10 inhibitors are also provided. In certain embodiments, at least one second inhibitor selected from an autophagy inhibitor, an AMPK inhibitor, and methyl pyruvate is also used in the methods. Dose packs comprising HDAC10 inhibitors and at least one second inhibitor are provided. Methods of identifying HDAC10 inhibitors are also provided.

Abstract: The invention relates to substituted 6-(2-hydroxybenzylamino)purines of general formula I, to their activity as cyclin-dependent kinases 2, 5, 7 and 9 inhibitors and to their use as medicaments, particularly in the treatment of disorders involving cell proliferation or inflammation. The invention further includes pharmaceutical compositions containing the substituted 6-(2-hydroxybenzylamino)purines.

Abstract: The present invention provides novel compositions and methods for inhibiting restenosis, thrombosis, and/or inflammation in a patient undergoing a vascular intervention. More particularly, the present invention provides intravascular devices coated with one or more spleen tyrosine kinase (Syk) inhibitors. Methods for inhibiting restenosis, thrombosis, and/or inflammation in a patient by treatment with such intravascular devices are also provided. In addition, the present invention provides methods for treating sickle cell disease using Syk inhibitors.

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: The present invention relates to the discovery of an epigenetic relay pathway that controls hepatic stellate cell activation and the wound-healing response in fibrogenesis, including fibrogenesis of the injured liver. Methods of inhibiting fibrogenesis, including liver fibrogenesis and secondary disease states and conditions thereof, and in treating liver damage, including cirrhosis of the liver (which may be caused by viruses or chemicals, including alcohol), are aspects of the present invention. The methods utilize certain nucleoside compounds and/or antibodies which are optionally conjugated. Pharmaceutical compositions represent additional aspects of the invention.

Abstract: The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity.

Abstract: The present invention relates to compounds of azapeptide or azapeptidomimetic type of formula (I): in which R1, R2, R3, X1, X2, X3, X4 and Y are as defined in claim 1, to pharmaceutical compositions containing them and to such compounds as adjuvant for an anticancer or anti-infectious medicament.

Abstract: The present invention relates to pharmaceutical compositions for treating virus infections and/or diseases caused by virus infections comprising at least a diaryl urea compound optionally combined with at least one additional therapeutic agent. Useful combinations include e.g. BAY 43-9006 as a diaryl urea compound.

Abstract: A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.

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;

Abstract: A method and composition that allows for the penetration of lipid insoluble medicaments through cell membranes using small S-Allyl-containing molecules with phospholipid permeable molecules as carrier molecules. S-Allyl-containing compounds can include alliin, allicin, Allium sativum extract and DMSO. Lipid insoluble medicaments can include 1% xylocaine, curcumin, acyclovir, valacyclovir, famciclovir, terbenafin, griseofulvin, clotrimazole, ketoconazole, clindamycin, neomycin, polysporin, bactricin, among others. The lipid insoluble medicaments are mixed with the phospholipid permeable molecules and painted on the skin using a swab or other suitable tool, thereby allowing for penetration of the medicament and providing relief from pain potentially caused by a subsequent injection. The composition can also be administered through an inhaler or directly into mucous membranes.

Abstract: This invention relates to compounds of the general formula: in which Q is an ethynyl or ethenyl moiety; Ring A is an aryl, heteroaryl or heterocyclic ring or ring system; and the remaining variable groups are as defined herein, and to their preparation and use.

Abstract: The present invention relates to a method for enhancing the activity of kinase inhibitors in target cells, and more specifically for enhancing the activity of tyrosine kinase inhibitors (TKIs), said method comprising contacting a cell with a kinase inhibitor and a photosensitizing agent and irradiating said cell with light of a wavelength effective to activate the photosensitizing agent, and to the use of this method for enhancing the effects of kinase inhibitors or kinase inhibitor-based drugs in particular to achieve cell death, for example, in cancer treatment and other diseases or conditions in which kinase inhibitors, such as TKIs, have a beneficial effect.

Abstract: Platelets are induced to proliferate, form extensions and produce daughter cells by various methods, including culturing platelets under thrombocytopenic conditions. Expansion of platelet cell numbers increases the storage life of platelets. Modulation of RT activity can be used to produce new daughter platelets. Therefore, the invention provides a new therapeutic use for RT inhibitors that can now be used for treatment of thrombocytopenia and related disorders. Likewise, application of soluble protein factor that may be secreted and/or released by platelets cultured under thrombocytopenic conditions may also be used as a therapeutic agent to increase platelet numbers.

Abstract: The invention relates to new substituted 6-(2-aminobenzylamino)purines, represented by the general formula I, which can be used in CDK inhibition, in particular, in the treatment of viral infections and diseases involving cell proliferation. The invention further includes pharmaceutical preparations containing substituted 6-(2-aminobenzylamino)purines.

Abstract: The invention relates to adenine receptor ligands useful for treating, alleviating and/or preventing diseases and disorders related to adenine receptor function as well as pharmaceutical compositions comprising such compounds and methods for preparing such compounds. The invention is further directed to the use of these compounds, alone or in combination with other therapeutic agents, for the alleviating, preventing and/or treating diseases and disorders, especially the use as antinociceptive or neuroprotective drugs.

Abstract: The present invention is directed to a method of treating systemic lupus erythematosus comprising administering a compound of formula (I) wherein R1 is selected from the group consisting of CF3, a C1-C5 alkyl, and (CH2)nR4, wherein n is between 0 and 4; R2 is selected from the group consisting of (CH2)mR4 and (CH2)mAr, wherein m is between 0 and 5; R3 is selected from the group consisting of hydrogen and methyl; R4 is selected from the group consisting of phenyl, OH, a C1-C3 alkoxy, a C1-C3 dialkylamino, piperidino, and N-methylpiperazino; Ar represents ?wherein X is selected from the group consisting of F, C1, a C1-C3 alkoxy, and CF3. The compounds can be used in combination with a second compound used in the treatment of systemic lupus erythematosus.

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: A method for the treatment and/or prophylaxis of an osteonecrotic bone disease in a mammal in need thereof, such as, e.g., idiopathic or secondary osteonecrosis, avascular bone necrosis, glucocorticoid induced bone ischemia/osteonecrosis, Legg-Calve-Perthes disease and femoral head necrosis, the method comprising administering an effective dose of a strontium-containing compound (a) to the mammal. A method for the treatment and/or prophylaxis of an osteonecrotic bone disease, such as, e.g., idiopathic or secondary osteonecrosis, avascular hone necrosis, glucocorticoid induced bone ischemia/osteonecrosis and femoral head necrosis, in a mammal who is to be or is treated with a therapeutic agent (b) known to or suspected of inducing apoptosis and/or necrosis of bone cells, the method comprising administering a strontium-containing compound (a) in combination with (b).

Abstract: The invention discloses a formulation prepared by granulating at least one anti-retro viral drug and at least one pharmaceutically acceptable additive, using an organic solvent; milling the product; finally processing the milled product to form tablets or capsules.

Abstract: The present invention is an invention belonging to the life style improving cosmetic in the field of hair maintenance and enrichment. More particularly, it relates to cosmetic compositions having an improved hair care actions such as to prevent hair loss and/or to promote hair growth on the scalp and skin of a mammal.

Abstract: The invention relates generally to treatment of neurological disorders and nervous system injuries. The invention specifically provides methods of using modulators of particular target proteins to modulate degeneration of neurons or portions thereof, such as axons.

Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.

Abstract: The invention encompasses purine derivatives as gamma secretase modulators, useful for treating diseases associated with the deposition of beta-amyloid peptide in the brain, such as Alzheimer's disease, or of preventing or delaying the onset of dementia associated with such diseases. Pharmaceutical compositions and methods of use are included.

Abstract: A method for the treatment of recurrent herpes labialis in mammals, including humans, which method comprises administering to the mammal in need of such treatment, an effective amount of penciclovir or famciclovir, or a pharmaceutically acceptable salt thereof for a period of one day.

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.

Abstract: Provided are compositions comprising opioid antagonists, such as naltrexone naloxone, or nalmefene, or their pharmaceutically acceptable salts, and methods for treating conditions caused by the varicella-zoster virus therewith.

Abstract: Provided herein are nanoparticles and methods for using nanoparticles. The nanoparticles include at least three antiretroviral agents. When introduced to cells the nanoparticles cause an increase in the intracellular concentration of the antiretroviral agents to a level that is at least the IC50 against HIV-I or HIV-2. This concentration may be maintained for at least 21 days after the cells are contacted with the nanoparticle. When administered to a subject the nanoparticles cause the concentration of the antiretroviral agents to increase to at least 100 ng/ml in the serum of the subject, at least 0.5 ?g/gram tissue in an organ of the subject, or a combination thereof. Such a concentration may be maintained for at least 21 days after the administration.

Abstract: The present invention relates to the use of a compound of formula (I) for the manufacture of a medicament for the prevention or the treatment of HIV infection wherein the compound of formula (I) is a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein A and B each represents a radical of formula and wherein —C-D- represents a bivalent radical of formula —N?CH—NR17—??(c-1); or —NR17—CH?N—??(c-2); provided that when A represents a radical of formula (a) then B represents a radical of formula (b) and when A represents a radical of formula (b) then B represents a radical of formula (a).

Abstract: Certain 6,9-disubstituted purine derivatives and their pharmaceutically acceptable salts are provided. These 6,9-disubstituted purine derivatives and their pharmaceutically acceptable salts are useful in compositions for treating mammalian cells, and especially human skin cells, in order to ameliorate the adverse effects of aging, treat skin disease states, treat immunological responses resulting from or associated with inflammation, and the like.

Abstract: The invention features methods, compositions, and kits useful for the treatment of muscular dystrophy, e.g., Duchenne muscular dystrophy, in a patient.

Abstract: Provided herein are methods of treating a medical condition in which RAS activation is increased. The method comprises the step of administering to a subject a c-Src inhibitor in an amount effective to treat the medical condition. The invention also provides a method of treating or preventing a cardiac arrhythmia. The method comprises the step of administering to the subject a c-Src inhibitor in an amount effective to treat or prevent the cardiac arrhythmia. The invention additionally provides a method of delaying the onset of sudden cardiac death. The method comprises the step of administering to the subject a c-Src inhibitor in an amount effective to delay the onset of SCD. Methods of augmenting gap junction function and methods of increasing Connexin 43 levels in a subject in need thereof are further provided.

Abstract: Drug eluting stents (DES) useful for the treatment of restenosis are described. The stents comprise biocompatible polymers and adenosine receptor modulators.

Abstract: A method of inhibiting double-stranded DNA virus infection is disclosed. In one embodiment, the method involves exposing a papillomavirus to an effective amount of an inhibitor selected from the group of G1, S, G2, and M cell cycle inhibitors. In another embodiment, the method involves administering an inhibitor selected from the group of G1, S, G2, and M cell cycle inhibitors to a susceptible tissue or cell.