Abstract: The invention relates to a method of treating or preventing Parkinson's disease in a subject comprising administering a compound of Formula I wherein, R1 is —NHC(O) C3-6 cycloalkyl and R2 is hydrogen; or R1 and R2 along with the carbon atoms to which they are attached form a six membered aromatic ring, wherein the ring is substituted with one or more groups selected from hydrogen, halogen and C1-6 alkyl; R3 and R4 are independently selected from group comprising hydrogen, halogen, C1-3 alkyl, OC1-3 alkyl, NO2, SC1-3 alkyl, C1-3 haloalkyl, OC1-3 haloalkyl, and SC1-3 haloalkyl; or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides substituted tetrahydroquinolinone and related compounds of formula (I), which are therapeutically useful as modulators of Retinoic acid receptor-related orphan receptors (RORs), more particularly as ROR? modulators. These compounds are useful in the treatment and prevention of diseases and/or disorder, in particular their use in diseases and/or disorder mediated by ROR? receptor. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted tetrahydroquinolinone or related compounds of formula (I), together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

Abstract: Disclosed are compounds of general formulas I-III that may be used to inhibit the action of fatty acid amide hydrolase (FAAH), monoacylglycerol lipase (MAGL) or dual FAAH/MAGL.

Abstract: The present invention provides a reproxalap ophthalmic solution, and methods of using the same for treating dry eye disease.

Abstract: The present disclosure relates to the identification of Nurr1 as a key regulator of metabolism, and the use of Nurr1 agonist to treat metabolic disorders such as diabetes, obesity, metabolic syndrome and hepatic steatosis.

Abstract: The present invention provides compositions and methods of use for treating, preventing, or ameliorating a disease, disorder, or condition associated with a chemokine receptor such as CXCR4.

Abstract: The present application relates to maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)aniline]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, crystalline forms thereof, to processes for its preparation, to pharmaceutical compositions comprising it and to its use in the control of disorders.

Abstract: Methods of selectively inhibiting Akt3 are provided. It has been discovered that 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide selectively inhibits Akt3. Because Akt3 modulates the suppressive function of natural Tregs and the polarization of induced Tregs, 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide can be used for modulating immune responses.

Abstract: Some aspects of this disclosure provide clinical media that support viability, re-plating efficiency, and repopulation capacity of cells and tissues during storage for up to 48 hours or longer. The clinical media provided herein are also useful for clinical irrigation. Cell or tissue preparations comprising a cell population or tissue and a clinical medium as provided herein are also provided, as are methods for generating such preparations. Methods for using the clinical media and cell and tissue preparations provided herein, for example, for administering an effective amount of cells or tissue to a subject in need thereof, are also disclosed.

Abstract: Derivatives of quinoline and naphthyridine, methods of making such compounds, and methods of using such compounds for the treatment or prophylaxis of HIV infection and certain cancers.

Abstract: Disclosed herein are compounds, compositions, and methods of their use for the treatment of diabetes.

Abstract: The present invention includes novel RAD52 inhibitors for preventing or treating cancers in a subject in need thereof. The present invention further includes a method of preventing or treating cancers in a subject in need thereof, the method comprising administering to the subject an effective amount of a compound of the invention. In certain embodiments, the subject is further administered at least one additional therapeutic agent.

Abstract: A method of preparing liposomal statins includes preparing a lipid solution including phosphatidylcholine, cholesterol, vitamin-E and an organic solvent and removing the solvent, forming a lipid cake. The lipid cake may then be hydrated with a first aqueous media. The hydrated cake may be mixed in a mixer and subjected to one or more freeze/thaw cycles and then extruded to form liposomes. A cryo-protective agent may be added to the liposomes and the liposomes may be lyophilized to provide a powder. A statin is added to the organic lipid solution or to the first aqueous media used for hydrating the lipid cake.

Abstract: The present invention provides compositions and methods of use for treating, preventing, or ameliorating a disease, disorder, or condition associated with a chemokine receptor such as CXCR4.

Abstract: Methods of selectively inhibiting Akt3 are provided. It has been discovered that 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide selectively inhibits Akt3. Because Akt3 modulates the suppressive function of natural Tregs and the polarization of induced Tregs, 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide can be used for modulating immune responses.

Abstract: A method for treating a disease or disorder in a patient who is currently taking a cytochrome P450 inhibitor comprising administering to the patient a dose of pimavanserin or a pharmaceutical acceptable salt thereof, wherein the dose is at least 20% lower than a dose of pimavanserin or a pharmaceutical acceptable salt thereof that would otherwise have been recommended to the patient if the patient were not currently taking the cytochrome P450 inhibitor.

Abstract: Compounds and compositions for selectively inhibiting Akt3 are provided. Methods of using the compounds are also provided. Because Akt3 modulates the suppressive function of natural Tregs and the polarization of induced Tregs, the disclosed compounds are useful for modulating immune responses.

Abstract: The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).

Abstract: The present invention relates to a medium composition for production of botulinum toxin and, more particularly, to a medium composition for culture of Clostridium sp. capable of producing botulinum toxin. The medium composition of the present invention comprises a porcine peptone and at least one plant-derived peptone selected from the group consisting of a garden pea hydrolysate, a cotton seed hydrolysate and a wheat gluten hydrolysate. When the medium according to the present invention, which contains plant-derived peptones, porcine peptones and minerals, is used for culture of Clostridium botulinum, the growth rate of the bacterium in the medium is higher than that in each of the medium that is in current use and the medium comprising plant-derived peptones alone. In addition, when the medium of the present invention is used, a high concentration of botulinum toxin can be produced by culturing the bacterium in a safe manner.

Abstract: Methods of selectively inhibiting Akt3 are provided. It has been discovered that 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide selectively inhibits Akt3. Because Akt3 modulates the suppressive function of natural Tregs and the polarization of induced Tregs, 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide can be used for modulating immune responses.

Abstract: Compositions of the invention comprise 1,2-dithiolane, dithiol and related compounds useful as therapeutic agents for the treatment and prevention of diseases and conditions associated with aberrant EGFR activity.

Abstract: Compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.

Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).

Abstract: Methods and compositions are described for reducing airway reactivity and the susceptibility to asthmatic bronchoconstriction that involve increasing sphingolipid content in airways and lungs of a mammalian subject.

Abstract: Aminoquinoline compounds useful for treating chronic pain, addiction, and other conditions are provided. The aminoquinoline compound is represented by Formula (I) which is defined in the specification.

Abstract: The invention provides a neurokinin 3 receptor (NKR3) antagonist for use in the treatment, prevention or amelioration of hot flushes in a human subject, for example a menopausal woman or a patient undergoing cancer therapy which affects secretion of sex steroids. The invention also provides a NKR3 antagonist together with a further active agent, and a composition and a kit comprising a NKR3 antagonist and a further active agent. The invention further provides a NKR3 agonist or exogenous NKB for the induction of hot flushes in a human subject.

Abstract: The present invention provides a compound of the Formula I: wherein A is: and W, Y, X, R1, R2, R3, and R4 are as defined herein, or a pharmaceutically acceptable salt thereof, for use as an inhibitor of the EP4 receptor.

Abstract: The present invention is directed to topical ophthalmic compositions of a lipophilic compound and an oligomeric or polymeric carrier wherein the compositions are useful in the treatment and prevention of macular degeneration. The invention also includes methods of treating macular degeneration by using a topical ophthalmic composition of a lipophilic compound and an oligomeric or polymeric carrier.

Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6 and n are as described herein, compositions including the compounds and methods of using the compounds. The present compounds are useful as fatty-acid binding protein (FABP) 4 and/or 5 inhibitors and may be used for the treatment or prophylaxis of lipodystrophy, type 2 diabetes, dyslipidemia, atherosclerosis, liver diseases involving inflammation, steatosis and/or fibrosis, such as non-alcoholic fatty liver disease, in particular non-alcoholic steatohepatitis, metabolic syndrome, obesity, chronic inflammatory and autoimmune inflammatory diseases.

Abstract: The present invention relates to the use of crenolanib, in a pharmaceutically acceptable salt form for the treatment of FLT3 mutated proliferative disorders driven by constitutively activated mutant FLT3, and to a method of treatment of warm-blooded animals, preferably humans, in which a therapeutically effective dose of crenolanib is administered to an animal suffering from said disease or condition:

Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).

Abstract: Various 2-aminoquinoline compounds as can be used, in vivo or in vitro, for selective inhibition of neuronal nitric oxide synthase.

Abstract: Compositions and methods for the treatment of Bowen's disease, an orphan disease, are described. In addition, compositions and methods for the treatment of recurrent respiratory papillomatosis (RRP), an orphan disease, are described. Compositions and methods for the treatment of stage 1 melanoma are also described. The compositions comprise one or more active ingredients selected from the group consisting of: chloroquine, amodiaquine, and an antibiotic such as metronidazole. The methods comprise administering a therapeutically effective amount of such compositions to a subject in need thereof.

Abstract: The present invention provides for the treatment, prevention, and/or reduction of a risk of a disease, disorder, or condition in which aldehyde toxicity is implicated in the pathogenesis, including ocular disorders, skin disorders, conditions associated with injurious effects from blister agents, and autoimmune, inflammatory, neurological and cardiovascular diseases by the use of a primary amine to scavenge toxic aldehydes, such as MDA and HNE.

Abstract: A method for treating polycystic ovarian syndrome and related conditions with a compound (I): or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to the use of crenolanib, in a pharmaceutically acceptable salt form for the treatment of FLT3 mutated proliferative disorders driven by constitutively activated mutant FLT3, and to a method of treatment of warm-blooded animals, preferably humans, in which a therapeutically effective dose of crenolanib is administered to an animal suffering from said disease or condition:

Abstract: A new medical therapy, and more particularly certain quinoline compounds which are anti-angiogenic integrin aplha5beta1 inhibitors, for use in the treatment of fibrosis, or a fibrosis-related disease, such as a fibrotic disease affecting the lung, liver, kidney, skin, epidermis, endodermis, muscle, tendon, cartilage, heart, stomach, large intestine, small intestine, colon, uterus, nervous system, testis, adrenal gland, artery, vein, biliary tract, or eye.

Abstract: The present invention discloses a method of treating gefitinib-resistant non-small-cell lung cancer, comprising administering an effective amount of D561-0775. A pharmaceutical composition comprising D561-0775 admixed with a pharmaceutical carrier for treating Gefitinib-resistant non-small-cell lung cancer is also disclosed therein.

Abstract: An advantage of some aspects of the invention is to provide an antibody against an amyloid precursor protein signal peptide. The invention provides an amyloid precursor protein signal peptide.

Abstract: A method of treating an Hepatitis C Virus infection in a patient, comprising providing a therapeutically effective amount, to a patient in need thereof, of a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein: G1 is a group of the formula or where n is 0, 1, 2, 3, or 4 and Het is a 5- or 6-membered heteroaryl group containing 1 to 4 heteroatoms independently chosen from N, O, and S, which Het is optionally substituted.

Abstract: A compound of Formula I, or an isomer, pharmaceutically acceptable salt or solvate thereof, is provided. Also, a composition containing a compound of Formula I, or an isomer, pharmaceutically acceptable salt or solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluents, is provided. Further, use of a compound of Formula I, or an isomer, pharmaceutically acceptable salt or solvate thereof for anti-apoptosis is provided, preventing or treating a disease or disorder associated with apoptosis; especially for protecting cardiomyocyte, preventing or treating a disease or disorder associated with cardiomyocyte apoptosis.

Abstract: Compounds, compositions and methods useful for treating infectious diseases are provided. In particular, 3-aryl quinoline compounds, their synthesis, pharmaceutical compositions thereof and methods of treating infectious diseases such as malaria, are disclosed.

Abstract: Various 2-aminoquinoline compounds as can be used, in vivo or in vitro, for selective inhibition of neuronal nitric oxide synthase.

Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6 and n are as described herein, compositions including the compounds and methods of using the compounds. The present compounds are useful as fatty-acid binding protein (FABP) 4 and/or 5 inhibitors and may be used for the treatment or prophylaxis of lipodystrophy, type 2 diabetes, dyslipidemia, atherosclerosis, liver diseases involving inflammation, steatosis and/or fibrosis, such as non-alcoholic fatty liver disease, in particular non-alcoholic steatohepatitis, metabolic syndrome, obesity, chronic inflammatory and autoimmune inflammatory diseases.

Abstract: The present application relates to cycloalkylpyridin-2-amines derivates of formula (1) or stereoisomers thereof or pharmaceutically acceptable salts thereof. The present application also relates to the process for the preparation of compounds of formula (I). The present application further describes the compounds of formula (1) as cholesteryl ester-transfer protein (CETP) inhibitors. The present application further relates to pharmaceutical compositions comprising compounds of formula (1) or stereoisomers thereof or pharmaceutically acceptable salts thereof.

Abstract: Provided herein are 4-methylpyrazole (4-MP) formulations, stable under storage conditions of up to about 55° C.

Abstract: The invention relates to compounds of the formulae (I), (II) and (III) in which R1, R2, R3, R4, Y, W1, W2, L, A, Alk, Cyc, Ar, Het1, Het2, Hal and n have the meaning indicated in Claim 1, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitization of cancer cells to anticancer agents and/or ionizing radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumors, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I) by reaction of compounds of the formulae (II) and (III) and optionally conversion of a base or acid of the compounds of the formula (I) into one of their salts.

Abstract: Provided herein are cell lines and assays that can be utilized to identify taste receptor modulators.

Abstract: The present invention relates to the use of crenolanib, in a pharmaceutically acceptable salt form for the treatment of FLT3 mutated proliferative disorders driven by constitutively activated mutant FLT3, and to a method of treatment of warm-blooded animals, preferably humans, in which a therapeutically effective dose of crenolanib is administered to an animal suffering from said disease or condition:

Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.