Abstract: Described herein are methods for modulation of the activity of the carotid body that afford therapeutic benefit for sleep-related breathing disorders and related conditions.

Abstract: Compounds of Formula I: (Formula should be inserted here) and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3, R4, R5, R6, R7, X1 and X2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.

Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.

Abstract: Compositions and formulations useful for treating inflammatory bowel diseases, intestinal cancers, and improving the integrity of the luminal surface of the gastrointestinal tract are disclosed. Typically, the composition increases level of cGMP in the intestinal mucosa or increases the activity of a PKG, preferably PKG2, in the intestinal mucosa. Preferably, the composition includes a phosphodiesterase type 5 (PDE5) inhibitor and is targeted to the intestinal mucosa, for example by enteric coating or attachment of an intestinal specific targeting moiety. Methods of using the compositions to treat intestinal and bowel diseases, and intestinal cancers, and methods of improving one or more physiological parameters of intestinal luminal integrity including, but are not limited to, reduced proliferation for example in the intestinal crypts, reduced apoptosis for example at the luminal surface, and induction of downstream effectors of PKG-mediated signaling are also disclosed.

Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.

Abstract: The present invention relates to a novel fused pyrimidine derivative having an inhibitory activity for tyrosine kinases, and a pharmaceutical composition for preventing or treating cancers, tumors, inflammatory diseases, autoimmune diseases, or immunologically mediated diseases comprising same as an active ingredient.

Abstract: The invention relates to a compound of formula (I) wherein A, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

Abstract: The present invention discloses a compound of formula (I) and citrate thereof as type 5 phosphodiesterase inhibitor, a preparation method thereof, and a pharmaceutical composition including the compound of formula (I) and citrate thereof. The experimental results of the present invention prove that the compound of formula (I) and citrate thereof can inhibit activity of type 5 phosphodiesterase, and can be used for treating erectile dysfunction, inhibiting platelet aggregation and treating thrombosis, decreasing pulmonary hypertension and treating cardiovascular diseases, treating asthma and treating diabetes gastroparesis.

Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, L1, L2, R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, pharmaceutical compositions containing them, and their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other disorders, diseases, and conditions for which inhibition of SYK is indicated.

Abstract: A method for treating a pulmonary hypertension condition such as pulmonary arterial hypertension (PAH) in a subject comprises administering to the subject a therapeutically effective amount of ambrisentan, wherein, at baseline, time from first diagnosis of the condition in the subject is not greater than about 2 years.

Abstract: The present invention relates to a compound of the following general formula (I): wherein: R1 is notably H, a halogen or an aryl group, R2 is notably a halogen or an aryl group, R3 is notably a halogen, or an aryl or heteroaryl group, as well as to its pharmaceutically acceptable salts, its hydrates or its polymorphic crystalline structures, its racemates, diastereoisomers or enantiomers, except the compound 1-(2,4-diaminopyrido[3,2-d]pyrimidin-7-yl)-3,6,6-trimethyl-6,7-dihydro-1H-indol-4(5H)-one.

Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1, R2, R3, R4, and B are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.

Abstract: The present invention relates to a compound having the general formula II, optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which is useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.

Abstract: The present invention provides a method of treating a cancer associated with a K-ras mutation in a subject in need thereof. The method comprises the steps of: (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) administering to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective.

Abstract: The present invention relates to a compound having the general formula I, optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which is useful in treating, ameliorating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.

Abstract: The present invention relates to a time-delayed sustained release pharmaceutical composition for oral administration, which comprises an immediate release phase and a prolonged sustained release phase, wherein said immediate release phase and prolonged sustained release phase respectively comprise Dapoxetine therein as an active ingredient.

Abstract: Provided herein are PAK inhibitors. Also provided herein are compositions and methods for treating an individual suffering from autism.

Abstract: A method for treating a disease is provided. The method includes steps of: providing a subject in need thereof; and administering one selected from a group consisting of KMUPS compound represented by formula I, a pharmaceutically acceptable salts thereof; and a pharmaceutical composition thereof to the subject in a dosage from 1 to 2.5 milligram per kilogram of body weight, wherein R2 and R4 are each selected independently from a group consisting of a C1˜C5 alkoxy group, a hydrogen, a nitro group and a halogen atom.

Abstract: The present invention relates to N-containing heterocyclic compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2, JAK3 or TYK2 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.

Abstract: The present invention relates to compounds of formula (I) and to pharmaceutically acceptable salts and pharmaceutical compositions thereof. The present invention also relates to use of the compounds of formula (I) in modulating the activity of protein kinases and in the treatment of disease, particularly a disease, disorder or syndrome associated with CDK 4 inhibition.

Abstract: The present invention relates to compositions, kits and methods for the administration of compositions and kits for supplementation with twelve carbon chain fatty acids or twelve carbon chain acylglycerols; and specifically for the supplementation with twelve carbon chain fatty acids such as lauric acid and twelve carbon chain acylglycerols such as monolaurin; and specifically for the co-supplementation with other vitamins, minerals and nutrients.

Abstract: The present invention relates to novel substituted 2-amino-3-(arylsulfonyl)pyrazolo[1,5-a]pyrimidines of general formula 1, to serotonin 5-HT6 receptor antagonists, to novel drug substances and pharmaceutical compositions, to medicaments, methods for preparation thereof, and to methods for prophylaxis and treatment of various CNS diseases, pathogenesis of which is associated with disturbance of monoaminergic signaling pathways, more specifically over- or hypo-activation of serotonin 5-HT6 receptors.

Abstract: Novel gyrase inhibitors and related compositions and methods are useful for impeding bacterial growth.

Abstract: The present invention encompasses compounds of general formula (1) wherein R1, R2 and R3 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.

Abstract: The present invention generally relates to the transdermal delivery of substances and, in some embodiments, to the transdermal delivery of beneficial substances by a hostile biophysical environment. In one aspect, various methods for the transdermal delivery of beneficial substances are disclosed. By creating a hostile biophysical environment, beneficial substances may be delivered, according to certain embodiments, through the stratum corneum of the skin into the body. Beneficial substances include, but are not limited to, pharmaceutical agents, drugs, vitamins, co-factors, peptides, dietary supplements, and others. The beneficial effects disclosed include, for instance, relief of pain and inflammation, prevention and healing of ulcers of the skin, relief of headache, improved sexual function and enjoyment, growth of hair on the scalp, improving muscle size and/or function, removing body fat and/or cellulite, treating cancer, treating viral infections and others.

Abstract: The present invention is for the anti-inflammatory compounds that have an inhibitory activity against protein tyrosine kinases and their pharmaceutical composition(s) containing the compound as the active ingredient. Since the compounds of the present invention can inhibit multiple protein kinases associated with inflammatory diseases and immune disorders, they are useful for their prevention or treatment.

Abstract: Novel heterocyclic compounds, which exhibit a dopamine receptor (preferably a D4 receptor) agonistic activity, and/or a PDE5 inhibitory activity, processes of preparing same, pharmaceutical compositions containing same and uses thereof in the treatment of sexual disorders such as decreased libido, orgasm disorder and erectile dysfunction are disclosed.

Abstract: The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

Abstract: The present invention relates generally to therapeutic formulations. More particularly, this present invention provides an oral delivery system for a therapeutic compound that is a base, a salt of a base or an amphoteric compound or a salt of a amphoteric compound with pharmacological, physiological or biochemical activity or a proactive form thereof. The present invention even more particularly provides a swallow formulation comprising a therapeutic compound that is a base, a salt of a base, an amphoteric compound or a salt of an amphoteric compound which facilitates the rapid delivery of the therapeutic compound to the circulatory system.

Abstract: Oral dosage forms as a biodegradable, water soluble film for delivering pharmaceutically active agents, particularly anti-migraine agents to patients through insertion into the mouth of patient and methods for administering pharmaceutically active agents to patients by insertion into the mouth to provide selective uptake of said agents through the mucosa and thus avoiding the gastrointestinal tract.

Abstract: Provided herein are PAK inhibitors. Also provided herein are compositions and methods for treating an individual suffering from Mild Cognitive Impairment.

Abstract: In one aspect, the invention relates to substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: Compound of Formula (I): are described, along with pharmaceutically acceptable salts thereof, compositions containing the same, and methods of use thereof in the treatment of cancer.

Abstract: A method of predicting the sensitivity of tumor cell growth to inhibition by a PI3K/AKT kinase pathway inhibitor, comprising: determining the localization profile of FOXO3a in a tumor cell, wherein a cytoplasmic localization profile of FOXO3a correlates with sensitivity to inhibition by a PI3K/AKT kinase inhibitor and a nuclear localization profile of FOXO3a correlates with resistance to inhibition by a PI3K/AKT kinase inhibitor.

Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.

Abstract: The present invention relates to compounds of Formula (Ia) or (Ib), the N-oxide forms, pharmaceutically acceptable addition salts, quaternary amines, stereoisomers, tautomers, racemics, metabolites, prodrugs, hydrates, or solvates thereof, wherein Y1, m, n, R1; X1; X2; R2; X3; X4; R3; and R4 have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to compounds that are kinase inhibitors useful for the treatment of disease states mediated by kinase, especially PLK4, in particular such compounds that are useful in the treatment of pathological processes which involve an aberrant cellular proliferation, such as tumor growth, rheumatoid arthritis, restenosis and atherosclerosis.

Abstract: Compositions and methods for treatment of sexual dysfunctions by administering to a subject a pharmaceutical composition comprising a delta opioid receptor agonist in an amount effective to delay the onset of ejaculation in the subject during sexual stimulation.

Abstract: The present invention relates to a thieno[3,2-d]pyrimidine derivative of formula (I), or a pharmaceutically acceptable salt, hydrate or solvate thereof, which has an excellent inhibitory activity on protein kinases, and a pharmaceutical composition comprising the same is effective in preventing or treating abnormal cell growth diseases.

Abstract: The invention features a method of treating a peripheral vascular disease or a condition associated with a peripheral vascular disease by administering to a subject an effective amount of at least one phosphodiesterase type 5 inhibitor and at least one nitric oxide donor. The invention also features compositions formulated for topical or oral administration including at least one phosphodiesterase type 5 inhibitor, at least one nitric oxide donor, and a pharmaceutically acceptable carrier, as well as kits including these compositions. These methods, compositions, and kits can optionally include other therapeutic agents.

Abstract: The present invention provides compounds of Formula I, including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

Abstract: The invention relates to substituted imidazo- and triazolopyrimidines and processes for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of haematological disorders, preferably of leucopenias and neutropenias.

Abstract: The present invention is concerned with deuterium-enriched pyrimidine compounds of formula I, their derivatives, enantiomers, diastereomers, solvates and pharmaceutical salts thereof, and their uses in the treatment, prevention and modulation of various diseases including chronic liver diseases, liver cirrhosis, liver fibrosis, hepatocellular carcinoma, liver cancer, renal cell carcinoma, kidney cancer, colorectal cancer, brain cancer, breast cancer, blood cancer, lung cancer, thyroid cancer, ovarian cancer, pancreas cancer, prostate cancer, stomach cancer, testicular cancer, uterus cancer, intestinal cancer, skin cancer, and other forms of cancer, carcinoid tumors, teratocarcinoma, tumor progression, metastasis and fibrosis in the neuroendocrine neoplasia, fibrotic processes as well as a disease state modulated directly or indirectly with 5-HT receptors, 5-HT1, 5-HT1A, 5-HT2 receptors, 5-HT2A and 5-HT2B receptors, dopamine receptors and multiple kinase pathways.

Abstract: The present invention relates to novel compounds which are able to modulate b-raf kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.

Abstract: The invention relates to liposomes for pulmonary application, advantageously comprising at least one first and at least one second phospholipid, cholesterol, and at least one active substance and/or colorant, wherein the first phospholipid is a phosphatidylcholine, preferably DSPC, and the second phospholipid is a phosphatidylcholine or an ethanolamine, preferably selected from the group DMPC, DPPC, DPPE. It is thereby advantageous if the first and the second phospholipid are present at a molar ratio of 0.5:1 to 10:1, preferably at a ratio of 6:1 to 2:1, in particular preferably at a ratio of 3:1. It is further advantageous if the molar ratio between phospholipids and cholesterol is between 10:1 and 1:1, preferably between 6:1 and 3:1, in particular preferably 4:1. The second phospholipid is further preferably DMPC or DPPE, in particular preferably DPPE. The size of the liposomes is advantageously between 0.05 ?m and 5 ?m, preferably between 0.2 ?m and 2.

Abstract: Methods of inhibiting kinases using kinase inhibitors having olefin moieties are disclosed.

Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders.

Abstract: A combination of a CDK4/8 inhibitor and an mTOR inhibitor for the treatment of cancer.

Abstract: The present invention relates to a compound of formula (I): Wherein R1 is a substituted or unsubstituted aromatic hetero- or homocyclic or a substituted or unsubstituted alicyclic hetero- or homocyclic group; R2 is an alkyl group with 1 to 18 carbon atoms or a substituted or unsubstituted cycloalkyl or aryl group; R3 is a substituted or unsubstituted aromatic hetero- or homocyclic or a substituted or unsubstituted alicyclic hetero- or homocyclic group; L is a single bond, an alkyl group having 1 to 6 carbon atoms, NHCO, O, S, NHCONH or NHCOO; X, Y and Z are independently 0, N, NH, S or CH; W is a single bond or an alkyl group having from 1 to 6 carbon atoms; or a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate of said compound or salt.

Abstract: The present invention is directed to compounds of formula I-II and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

Abstract: Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R)3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted ?m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—, ?phenyl-CH(OH)—, or phenyl-C(?NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them; also disclosed are a processes for preparing intermediates useful for preparing comp