Abstract: The present disclosure provides compositions and methods for selectively killing senescent cells, wherein the composition comprises piperlongumine derivative thereof. The selective killing of senescent cells may delay aging and/or treat age-related disorders.

Abstract: Described herein are compositions for, and methods of treating, Raynaud's phenomenon. The compositions comprise a TRPM-8 antagonist formulated in a topical formulation in an amount effective to treat Raynaud's phenomenon.

Abstract: The present disclosure relates to a device configured to be adhered to the surface of a mammal for recording physiological signals. The device may include a housing enclosing a circuit board and a flexible wing extending from the housing. The device may include an electrode coupled to the flexible wing and an electrical trace for transmitting an electrical signal between the electrode and the circuit board. The electrical trace may have an insulator with a conductive material and resistors printed on the surface of the insulator. The trace layer may include conductive vias for transmitting the signal from a bottom of the trace layer to a top of the trace layer. The housing may include a battery having a battery terminal connector configured to provide electrical access to both terminals on a single side of the battery. The housing may include a floating trigger button.

Abstract: The present invention relates to compounds of formula (C) (C), wherein ring A, RB2 and RB3 are as defined in claim 1.

Abstract: The present invention relates to compounds of formula (C) (C), wherein ring A, RB2 and RB3 are as defined in claim 1.

Abstract: The invention is directed to a method of treating a cancer in an animal and a method of increasing DNA repair activity in an animal. The methods comprise administering to an animal in need thereof an effective amount of a small molecule substance that interferes with the activity of CUL4A, such as a 1,3-benzoxathiol-2-one compound, a pyridine thione compound, a 2,6-diamino-4-thiopyran-3,5-dicarbonitrile compound, or a 1,2,4-triazole-3-thiol compound.

Abstract: The present disclosure relates to novel co-crystals of a CDK inhibitor and an MEK inhibitor and the preparation methods thereof. Specifically, the present disclosure provides hydrates or anhydrates which are named as Form I, Form II and Form III. The novel co-crystals provided in the present disclosure have good stability, low hygroscopicity and high solubility, and have an important value for further optimization and development of the drug.

Abstract: Inhibitors of EYA tyrosine phosphatase having the structure of Formula I are provided herein. The compounds are useful for the treatment of certain proliferative diseases and cancer.

Abstract: The present disclosure provides methods of treating a cognitive disorder associated with abnormal dendritic spines, such as Fragile X Syndrome, Fragile X Associated Tremor/Ataxia Syndrome, autism, or mental retardation, using PKC activators.

Abstract: Topical compositions having as the active ingredient a lipid, fatty acid ester, natural wax, sterol, or combinations thereof referred to herein as “lipophilic vehicle” or “LV” and methods of use, have been developed for the amelioration or prevention of pain or the sequelae of pain. The composition may be in the form of an ointment, cream, gel, lotion, spray, foam, paste, patch, suspension or dispersion. The composition is variably effective to treat visceral, somatic and neuropathic pain both acute and chronic as well as muscle pain and stiffness and joint pain and stiffness.

Abstract: The invention relates to compounds of formula (I) wherein R1, R2, X1, X2, Y, Ra, Rb, Q have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis and also in the treatment of cancer disorders.

Abstract: Compounds of the formula (I), in which R1, R3, R5, R6, R7, R, X and Y have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours.

Abstract: The invention relates to 3-(2?,2?-dimethylpropanoylamino)-tetrahydropyridin-2-one, and its pharmaceutical compositions and its use for preparing a medicament intended to prevent or treat inflammatory disorders.

Abstract: The present invention relates to new biphenyl-3-carboxylic acid modulators of beta-3-adrenoceptor activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention relates to a method for treating ocular inflammatory diseases in a subject in need of such treatment, which comprises administering a pharmaceutical composition comprising a therapeutically effective amount of at least one agonist of Formyl peptide receptor 2.

Abstract: The present invention provides compounds of formula I wherein Q is Q1 or Q2; A1, A2, A3 and A4 are independently of each other C—H, C—R7, or nitrogen; R1 is C1-C8haloalkyl; R2 is aryl or aryl substituted by one to five R11, or heteroaryl or heteroaryl substituted by one to five R11; and R3, R4, R5, R6 and R7 are as defined in the claims. The invention also provides methods of controlling insects, acarines, nematodes or molluscs which methods comprise applying to a pest, to a locus of a pest, or to a plant susceptible to attack by a pest an insecticidally, acaricidally, nematicidally or molluscicidally effective amount of a compound of formula (I).

Abstract: Compounds including various oligomers of piperlongumine and/or piperlongumine analogues as well as certain piperlongumine analogues that exhibit improved toxicity to cancer cells are disclosed. Also provided are compositions that comprise the compounds, methods of making compositions comprising the compounds, methods of making the compounds, and the use of compounds in methods for treating cancer.

Abstract: Provided herein are 2-phenoxy- and 2-phenylsulfonamide derivatives with CCR3 antagonistic activity. These compounds are useful for the treatment of diseases associated with CCR3 activity, including but not limited to, atopic dermatitis, allergic rhinitis, rheumatoid arthritis, Grave's disease, HIV infection, Alzheimer's disease, atherosclerosis and other inflammatory and/or immunological disorders.

Abstract: Compounds of formula II are described: wherein D, n, Ra, Rb, and Rc are as herein defined, along with pharmaceutical compositions and methods of using compounds of formula II for treating or reducing the risk of peritoneal carcinomatosis in a patient.

Abstract: The present invention relates to lactam derivatives of formula (I) wherein Y, R1, R2 and R3 are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.

Abstract: Disclosed herein are methods of preventing or treating inflammatory diseases using sulfonamide analogs of 3-aminolactam compounds, each with aromatic “tail groups”. Compounds as defined by formulae (I) and (I?), and the medical uses of the compounds, are described herein.

Abstract: The invention provides compounds, compositions and uses of compounds of general formula (I) or pharmaceutically acceptable salts thereof, which are 3-aminocaprolactam derivatives, for the preparation of a medicament intended to treat an inflammatory disorder: wherein X is —CO—Y—(R1)n or SO2—Y—(R1)n; and Y is a cycloalkyl or polycycloalkyl group (such as an adamantyl, adamantanemethyl, bicyclooctyl, cyclohexyl, cyclopropyl group); or is a cycloalkenyl or polycycloalkenyl group.

Abstract: The invention relates to the generation of a library of compounds enriched in agonist and antagonists for members of the G-protein coupled class of receptors (GPCRs). The library contains compounds of general formula (II) wherein: y is any integer from 1 to 8; X is —CO—R1 or —SO2—R1; each R1 is independently selected from an alkyl, haloalkyl, alkenyl, alkynyl, alkylaminoalkyl, alkylaminodialkyl, or charged alkylaminotrialkyl, radical of 1 to 20 carbon atoms; or each R1 is independently selected from oxyalkyl, aminoalkyl, aminodialkyl, or charged aminotrialkyl radical; and wherein the R1 radical has a “key” carbon next to the carbonyl of the carbon amide or the sulfonyl group of the sulfonamide which is di-substituted with the same or different groups selected from: alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl and alkylamino radicals.

Abstract: [Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that a compound of the present invention or a salt thereof exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. The present invention further relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound of the present invention or a salt thereof, and an excipient.

Abstract: Compounds of formula (I), pharmaceutical compositions comprising them, and methods for their use are described.

Abstract: The present invention provides the use of a neutral endopeptidase inhibitor, in the manufacture of a medicament for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The invention also relates to the use of a compound of Formula I: wherein R1, R2, R3, R5, X, A3, B1, s and n are defined herein, for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The present invention further provides a combination of pharmacologically active agents for use in the treatment, amelioration and/or prevention of contrast-induced nephropathy.

Abstract: The invention provides the use of a compound of formula (I) or a solvate or hydrate thereof, wherein the substituents are as defined in the description, and combinations thereof, for the treatment of pruritus or a dermatological disorder or disease.

Abstract: The invention provides compounds, pharmaceutical compositions and uses of compounds and salts thereof of general formula (I), for the preparation of a medicament for treatment of an inflammatory disorder, but excluding (S)-3-(1?-methylcyclohexylcarbonylamino)-caprolactam: wherein z is 1, 2, 3 or 4; A is —CO— or —SO2—; Q is linear or branched alkyl, alkenyl, alkynyl, alkoxy, oxyalkyl, aminoalkyl, alkylamino, alklylaminoalkyl, haloalkyl, aryl or substituted aryl; T1 and T2 together constitute a cycloalkyl, cycloalkenyl or polycycloalkyl radical composed of n additional carbon atoms, where n is between 2 and 7; and each hydrogen atom bonded to the carbon atoms in the ring generated by T1 and T2 may be independently be substituted by a group R1, where R1 is independently selected from an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl or alkylamino radical of 1 to 20 carbon atoms; or each R1 is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl or aminodialky

Abstract: A method for treating pain, migraine, inflammation, gastrointestinal tract disorders, disorders of the genito-urinary tract, ophthalmic diseases or obesity in a subject, the method including administering to the subject an effective amount of a compound of a general formula, specific examples of which include 3-(4-Butyloxy-benzylamino)-pyrrolidin-2-one, 3-[4-(4-trifluorobutyloxy)-benzylamino]-pyrrolidin-2-one, 3-(4-Pentyloxy-benzylamino)-pyrrolidin-2-one, 3-[4-(5-trifluoropentyloxy)-benzylamino]-pyrrolidin-2-one, and 3-(4-Phenylethyl-benzylamino)-pyrrolidin-2-one.

Abstract: Disclosed are N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. In Formula (I), R1, R2, R3, R4, R3?, R10 and R11 are as described herein. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of treating cognitive disorders using compounds of Formula (I).

Abstract: The invention relates to compounds of formula I: along with pharmaceutical compositions containing the same and methods of use thereof for the treatment of autoimmune disease.

Abstract: 3-aminopyrrolidone compounds and pharmaceutically acceptable salts thereof that are active as sodium and/or calcium channel modulators and therefore useful in preventing, alleviating and curing a wide range of pathologies, including, but not limited to cardiovascular, inflammatory, ophthalmic, urologic, metabolic and gastrointestinal diseases.

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: The invention relates to the use of Broad-Spectrum Chemokine Inhibitors (BSCIs), and in particular members of the acylaminolactam class of pharmaceutical agents, for the prevention, prophylaxis, treatment or amelioration of symptoms of inflammatory diseases. In particular, improved compositions consisting of BSCI agents combined with one or more additional active pharmaceutical agents in order to achieve improved anti-inflammatory efficacy with a reduced side-effect profile are described and claimed.

Abstract: The invention provides for compounds of formula I wherein the substitutents are as described herein. Further provided are methods of using such compounds for the treatment of eating disorders, metabolic disorders, obesity, cognitive disorders, neurological disorders, pain disorders, inflammation disorders, in the promotion of smoking cessation and for the treatment of other psychiatric disorders Also provided are pharmaceutical compositions containing such compounds and pharmaceutical combinations of the compounds of the invention with other therapeutic agents.

Abstract: The invention provides compounds, pharmaceutical compositions and uses of compounds and salts thereof of general formula (I), for the preparation of a medicament for treatment of an inflammatory disorder, but excluding (S)-3-(1?-methylcyclohexylcarbonylamino)-caprolactam: wherein z is 1, 2, 3 or 4; A is —CO— or —SO2—; Q is linear or branched alkyl, alkenyl, alkynyl, alkoxy, oxyalkyl, aminoalkyl, alkylamino, alklylaminoalkyl, haloalkyl, aryl or substituted aryl; T1 and T2 together constitute a cycloalkyl, cycloalkenyl or polycycloalkyl radical composed of n additional carbon atoms, where n is between 2 and 7; and each hydrogen atom bonded to the carbon atoms in the ring generated by T1 and T2 may be independently be substituted by a group R1, where R1 is independently selected from an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl or alkylamino radical of 1 to 20 carbon atoms; or each R1 is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl or aminodialky

Abstract: The invention provides compounds, compositions and uses of compounds of general formula (I) or pharmaceutically acceptable salts thereof, which are 3-aminocaprolactam derivatives, for the preparation of a medicament intended to treat an inflammatory disorder: wherein X is —CO—Y—(R1)n or SO2—Y—(R1)n; and Y is a cycloalkyl or polycyloalkyl group (such as an adamantyl, adamantanemethyl, bicyclooctyl, cyclohexyl, cyclopropyl group); or is a cycloalkenyl or polycycloalkenyl group.

Abstract: This invention provides novel heterocyclic derived matrix metalloprotease inhibitors of the formula: and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing matrix metalloproteases. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.

Abstract: The invention relates to compounds of formula I in which A, R1, R2, R3, R4, R5, R6, R7 and n have the meanings stated in the claims. The compounds are particularly suitable as antiarrhythmic active ingredients, in particular for the treatment and prophylaxis of atrial arrhythmias, for example atrial fibrillation (AF) or atrial flutter.

Abstract: This invention provides novel heterocyclic derived matrix metalloprotease inhibitors of the formula: and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing matrix metalloproteases. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.

Abstract: The invention provides compounds, pharmaceutical compositions and uses of compounds and salts thereof of general formula (I), for the preparation of a medicament for treatment of an inflammatory disorder, but excluding (S)-3-(r-methylcyclohexyl-carbonylamino)-caprolactam: wherein z is 1, 2, 3 or 4; A is —CO— or —SO2-; Q is linear or branched alkyl, alkenyl, alkynyl, alkoxy, oxyalkyl, aminoalkyl, alkylamino, alkylaminoalkyl, haloalkyl, aryl or substituted aryl; T1 and T2 together constitute a cycloalkyl, cycloalkenyl or polycycloalkyl radical composed of n additional carbon atoms, where n is between 2 and 7; and each hydrogen atom bonded to the carbon atoms in the ring generated by T1 and T2 may be independently be substituted by a group R1, where R1 is independently selected from an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl or alkylamino radical of 1 to 20 carbon atoms; or each R1 is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl or aminodialkyl radi

Abstract: Co-crystals comprising at least one nutraceutical compound and at least one co-crystal former with or without impurities. These co-crystals may be included in compositions (optionally also including other components such as pharmaceutically acceptable excipients, other nutritional supplements, etc.) having utility as pharmaceuticals, nutraceuticals, nutritional supplements, and foodstuffs.

Abstract: Compounds of formula (I), pharmaceutical compositions comprising them, and methods for their use are described.

Abstract: The present invention relates to a new class of plant growth regulators. In particular, the invention relates to fused azepinone derivative of general formula (I) or an agriculturally acceptable salt thereof wherein X is CO2R2 or H; Y is OH; NHNR3R4, NHNHC(?Z)NR5R6 or NHNHC(?Z)CR7R8R9; or X and Y together with the two carbon atoms to which they are attached form a ring of formula (A) and a method for treatment of plants with such compounds in order to induce growth regulating responses.

Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-+related disease.

Abstract: The invention provides compounds, compositions and uses of compounds of general formula (I) or (I?), or pharmaceutically acceptable salts thereof, which are 3-aminocaprolactam derivatives, for the preparation of a medicament intended to treat an inflammatory disorder.

Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4-P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

Abstract: The invention provides compounds, pharmaceutical compositions and uses of compounds and salts thereof of general formula (I), for the preparation of a medicament for treatment of an inflammatory disorder, but excluding (S)-3-(r-methylcyclohexyl-carbonylamino)-caprolactam: wherein z is 1, 2, 3 or 4; A is —CO— or —SO2-; Q is linear or branched alkyl, alkenyl, alkynyl, alkoxy, oxyalkyl, aminoalkyl, alkylamino, alkylaminoalkyl, haloalkyl, aryl or substituted aryl; T1 and T2 together constitute a cycloalkyl, cycloalkenyl or polycycloalkyl radical composed of n additional carbon atoms, where n is between 2 and 7; and each hydrogen atom bonded to the carbon atoms in the ring generated by T1 and T2 may be independently be substituted by a group R1, where R1 is independently selected from an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl or alkylamino radical of 1 to 20 carbon atoms; or each R1 is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl or aminodialkyl radi

Abstract: Solid dispersion comprising (4R)-4-[N?-methyl-N?-(3,5-bistrifluoromethyl-benzoyl)-amino]-4-(3,4-dichlorobenzyl)-but-2-enoic acid N—[(R)-epsilon-caprolactam-3-yl]-amide or a pharmaceutically acceptable salt or solvate thereof and a carrier. Pharmaceutical compositions comprising such solid dispersion are useful to treat patients who have functional motility disorders of the viscera, especially irritable bowel syndrome or functional dyspepsia, or urinary bladder disorders, especially urinary incontinence.

Abstract: This invention relates to novel cyclic malonamides having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.