Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

Abstract: Methods are provided of treating cardiac hypertrophy in a mammalian subject comprising administering to the subject an anti-hypertrophic effective amount of an ion channel TR-PV1 inhibitor. The methods include treatment of a symptom of cardiac hypertrophy in the subject comprises cardiac remodeling, cardiac fibrosis, apoptosis, hypertension, or heart failure.

Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

Abstract: The present invention relates to (2-ureidoacetamido)alkyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor 2.

Abstract: Methods are provided of treating cardiac hypertrophy in a mammalian subject comprising administering to the subject an anti-hypertrophic effective amount of an ion channel TR-PV1 inhibitor. The methods include treatment of a symptom of cardiac hypertrophy in the subject comprises cardiac remodeling, cardiac fibrosis, apoptosis, hypertension, or heart failure.

Abstract: The present invention provides sorafenib analogs for use in a method of treating a disease mediated by p21, said method comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula I. The present invention also provides methods of inhibiting p21 in a cell comprising contacting the cell with an effective amount of a compound of formula I.

Abstract: The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.

Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.

Abstract: The present invention provides combination therapy methods of treating proliferative diseases (such as cancer) comprising a first therapy comprising administering to an individual an effective amount of a taxane in a nanoparticle composition, and a second therapy which may include, for example, radiation, surgery, administration of chemotherapeutic agents, or combinations thereof. Also provided are methods of administering to an individual a drug taxane in a nanoparticle composition based on a metronomic dosing regime.

Abstract: The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: Anti-cancer compositions and methods are described herein. In particular, compositions including one or more of leelamine, a leelamine derivative, abietylamine, an abietylamine derivative, and an abietic acid derivative are described. Methods for treatment of pathological conditions particularly cancer, in a subject using one or more of leelamine, a leelamine derivative, abietylamine, an abietylamine derivative, and an abietic acid derivative are described herein.

Abstract: In one aspect, the invention relates to substituted 4-phenoxyphenol analogs, derivatives thereof, and related compounds, which are useful as inhibitors of proliferating cell nuclear antigen (PCNA); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating hyperproliferative disorders associated with PCNA using the compounds and compositions. 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: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.

Abstract: The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for inhibiting the growth of a microbe; treating a mammal having a microbial infection, malaria, mucositis, an ophthalmic infection, an otic infection, a cancer, or a Mycobacterium infection; killing or inhibiting the growth of a Plasmodium species; inhibiting the growth of a Mycobacterium species; modulating an immune response in a mammal; or antagonizing unfractionated heparin, low molecular weight heparin, or a heparin/low molecular weight heparin derivative.

Abstract: The present invention relates to a method of removing undifferentiated stem cells and dedifferentiated stem cells from a sample of cells. The invention further relates to preventing dedifferentiation of differentiated cells. Both methods comprise of administering to said cells an effective amount of compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, n, p, Z and T are defined herein.

Abstract: The invention relates to urea derivatives of formula (I) as inhibitors of glycogen synthase kinase 3?, GSK-3, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which GSK-3 is involved, such as Alzheimer's disease or non-insulin dependent diabetes mellitus.

Abstract: The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.

Abstract: Embodiments of the present invention are directed to compositions and methods for the treatment of purpura. Preferred compositions comprise an ? adrenergic receptor agonist selected from selective ?1 adrenergic receptor agonist, selective ?2 adrenergic receptor agonist, non-selective ?1/?2 adrenergic receptor agonist, agents with ?2 adrenergic receptor agonist activity and combinations thereof, in a pharmaceutically acceptable carrier in order to treat and improve the cosmetic appearance of hemorrhagic (purpuric) lesions in the skin.

Abstract: 4-(methylsulfonylamino)phenyl analogues as potent vanilloid receptor antagonists and pharmaceutical compositions comprising the same. The compounds are useful as analgesics to prevent, alleviate or treat pain diseases or inflammatory disease including pain, acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflammatory bowel disease, inflammatory disease and urgent urinary incontinence.

Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.

Abstract: A pest control agent containing a compound represented by the following Formula (1), wherein A represents a carbon atom, a nitrogen atom, or the like, K represents a non-metal atom group necessary for forming a cyclic linking group derived from a 5- or 6-membered aromatic ring, in combination with A and two carbon atoms to which A bonds, X represents a hydrogen atom, a halogen atom, or the like, n represents an integer of from 0 to 4, T represents —C(?G1)-Q1 (wherein G1 and G2 represent an oxygen atom or the like, Q1 represents a phenyl group which may have a substituent, a heterocyclic group which may have a substituent, or the like), or the like, Q2 represents a phenyl group or the like, G3 represents an oxygen atom or the like, and R1 and R2 each independently represent a hydrogen atom, a C1-C6 alkyl group, or a group represented by -L-D, or the like (provided that at least either R1 or R2 represents a group represented by -L-D); as an active ingredient exhibits an excellent effect.

Abstract: Disclosed herein are compounds of formula (I) or pharmaceutically acceptable salts, prodrugs, or combinations thereof, wherein X1, L, Rx, Ry, Rz, R1, R2, A, m, n, p, q, and r are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.

Abstract: Disclosed are pactamycin analogs, pharmaceutical compositions including the analogs, and methods of using the analogs, such as to inhibit tumor growth or a pathogenic infection such as a bacterial or parasitic infection. The pactamycin analogs have a general formula where R1 is H, lower aliphatic, amide, acyl, or aminoacyl; R2 is —C(O)NR8R9 where R8 and R9 independently are hydrogen or lower aliphatic, or R1 and R2 together form a cyclic structure; R3 and R4 independently are hydrogen, hydroxyl, or lower aliphatic, or R2 and R3 together form a cyclic structure; R5 is hydrogen or acyl; R6 and R7 independently are hydrogen, hydroxyl, halogen, lower aliphatic, or amino.

Abstract: Compounds of formula Ia and Ib wherein A, B, C, R1 and R14 are described herein.

Abstract: The present application is directed to compounds that are TRPV1 antagonictc and have formula (I) wherein variables Ar1, L1, R1, R2, R3, R4, R5, Y1, Y2, and Y3, are as defined in the description, which are useful for treating disorders caused by or exacerbated by vanilloid receptor activity.

Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.

Abstract: A manufacturing process for the preparation of radiolabeled compounds of formula (I) includes reacting compounds of formula (II) with a source of radionuclide of a halogen in the presence of an oxidant under acidic condition, wherein: *I is 123I, 124I, 125I or 131I; R is lower alkyl, optionally substituted with one or more fluorine atoms; Q is C(O), O, NR?, S, S(O)2, C(O)2, (CH2)p; Y is C(O), O, NR?, S, S(O)2, C(O)2, (CH2)p; R? is H, C(O), S(O)2, C(O)2; Z is H, C1-C4 alkyl, benzyl, substituted benzyl or trialkylsilyl; m is 0, 1, 2, 3, 4 or 5; n is 0, 1, 2, 3, 4, 5 or 6; and p is 0, 1, 2, 3, 4, 5 or 6.

Abstract: The invention provides novel classes of HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided as well as methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention.

Abstract: A carbonic anhydrase IX (CA IX) inhibitor which comprises a compound of general formula: R—NH—CX—NH—(CH2)n—Ar-Q-SO2—NH2 or a pharmaceutically-acceptable salt, derivative or prodrug thereof; wherein n=0, 1 or 2; Q is O or NH; X is O or S; and R comprises an organic substituent group.

Abstract: The invention relates to cyclopentanecarboxamide derivatives of formula 1, to their use as Fatty Acid Synthase inhibitors, to methods for their therapeutic use and to pharmaceutical compositions containing them, wherein R1, R2, R3, LO, W, AR1, n are as defined in claim 1.

Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

Abstract: Spray dried solid dispersions comprising a sparingly soluble drug and hydroxypropylmethylcellulose acetate succinate (HPMCAS) provide increased aqueous solubility and/or bioavailability in a use environment.

Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.

Abstract: A solid composition of a low-solubility drug and a concentration-enhancing polymer has a portion of the drug in a semi-ordered state.

Abstract: The invention provides for novel (bis)urea and (bis)thiourea compounds which are inhibitors of lysine-specific demethylase 1 (LSD1). Such compounds may be used to treat disorders, including cancer.

Abstract: Ghrelin O-acyltransferase (GOAT) is inhibited with designed small molecules of the general formula: Methods comprise contacting the GOAT with an inhibitor and detecting a resultant inhibition.

Abstract: Compounds of formula Ia and Ib and wherein A, B, C and R1 are described herein.

Abstract: A liquid antibacterial soap comprising trichlorocarbanilide, wherein the composition includes, 0.1-5 wt. % trichlorocarbanilide, 0-40 wt. % water, 0.1-40 wt. % of a surfactant or mixture of surfactants, 10-60 wt. % of lower glycols to render the composition visually clear and stable, and 0.1-10 wt. % of a mixture of additional adjuvant ingredients.

Abstract: The invention provides novel classes of HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided as well as methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention.

Abstract: The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: This invention relates to tetrahydro-naphthalene derivatives and salts thereof which are useful as an active ingredient of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, urge urinary incontinence, chronic pain, neuropathic pain, post-operative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.

Abstract: The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: The present invention relates to the use of a compound represented by the general formula (I), and pharmaceutically acceptable salts thereof, wherein: n is an integer from 2 to 5; p is an integer from 0 to 4; R1 is selected from the group consisting of a hydroxyl group, an alkoxy group, a thiol group, a thioether group, and an amino group, wherein at least two of R1 is a hydroxyl group, a thiol group or an amino group, with the proviso that wherein n is 2, R1 is not on the carbon-2 position and the carbon-5 position of the phenyl group; R2 and R3 are independently a methylene group or a nucleophile, with the proviso that at least one of R2 and R3 is a nucleophile group; Z is an oxygen (O) atom or sulfur (S) atom; T is hydrogen or an optionally substituted aliphatic group; in the manufacture of a medicament for treating a patient in need of cell therapy.

Abstract: Embodiments of the present invention are directed to compositions and methods for the treatment of purpura. Preferred compositions comprise an ? adrenergic receptor agonist selected from selective ?1 adrenergic receptor agonist, selective ?2 adrenergic receptor agonist, non-selective ?1/?2 adrenergic receptor agonist, agents with ?2 adrenergic receptor agonist activity and combinations thereof, in a pharmaceutically acceptable carrier in order to treat and improve the cosmetic appearance of hemorrhagic (purpuric) lesions in the skin.

Abstract: The present invention is directed to aspartic protease inhibitors. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.

Abstract: Ghrelin O-acyltransferase (GOAT) is inhibited with designed small molecules. Methods comprise contacting the GOAT with an inhibitor and detecting a resultant inhibition.

Abstract: Compounds of the formula I, II or III: or pharmaceutically acceptable salts thereof, wherein m, n, q, Ar, R1, R2, R3, R4 and R5 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formulas I-III.

Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.

Abstract: A composition for use in inhibiting the binding of a Norovirus to the histo-blood group antigen on the surface of epithelia. The composition contains a therapeutically effective amount of a binding-inhibiting compound selected from Compounds 1 through 15, and at least one diluent, carrier or excipient. The Compounds competitively bind a Norovirus that has the capability of binding with the histo-blood group antigens of secretor blood type, including A, B, AB, and O blood types. The compositions can be administered to a human prior to or after infection by a Norovirus, to prevent or ameliorate an infection.