Abstract: There is provided compounds of formula I (I) or pharmaceutically-acceptable salts thereof, wherein L, R1, R2, R3, R4 and n have meanings provided in the description, which compounds are useful in the treatment of cancers.

Abstract: The present disclosure discloses a biaryl urea ROR?t inhibitor, and specifically relates to a biaryl urea derivative, as represented by formula I, with an ROR?t inhibiting activity, and a preparation process thereof, and a pharmaceutical composition comprising the compound. Further disclosed is use of the compound for treating an ROR?t-related disease.

Abstract: A pyridoxine-based compound of formula 1: exhibits a high level of antiepileptic activity. At doses of 25, 50 and 100 mg/kg, compound 1 completely suppresses the epileptic electrical activity of the brain within an hour after intraperitoneal administration to rats on the penicillin model of epilepsy. The rats' corazol model of epilepsy shows a decrease in intensity and duration of seizures with the administration of compound 1 at doses of 25 and 100 mg/kg intraperitoneally and 100 and 200 mg/kg orally, and the complete prevention of seizures in some cases at a dosage of 250 mg/kg with oral administration. Compound 1 is low toxic. The LD50 parameter in rats exceeds 2000 and 5000 mg/kg of body weight with intraperitoneal and oral administration respectively. The technical solution provides a new highly effective and safe drug for the treatment of epilepsy.

Abstract: The present invention discloses a biaryl urea ROR?t inhibitor, and specifically relates to a biaryl urea derivative, as represented by formula I, with an ROR?t inhibiting activity, and a preparation process thereof, and a pharmaceutical composition comprising the compound. Further disclosed is use of the compound for treating an ROR?t-related disease.

Abstract: Described herein are methods, compositions and kits related to manipulating hematopoietic stem cells and more particularly to methods, compositions and kits related to increasing the number of hematopoietic stem cells in vitro and in vivo. Also described are methods, compositions and kits related to making an expanded population of hematopoietic stem cells (HSCs) and methods, compositions and kits related to using the expanded population of HSCs.

Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.

Abstract: The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.

Abstract: The present description relates to compounds of Formula I (A+ X?), a diastereoisomer, an enantiomer, or a mixture thereof, pharmaceutical composition comprising same and uses thereof for gastrointestinal endoscopic and medical imaging applications, and for the treatment of visceral pain: Where R1 and R2 are as defined herein

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

Abstract: Embodiments of the invention include methods of treating, preventing, and/or reduce the risk or severity of a condition selected from the group consisting of muscle wasting, muscle weakness, cachexia, and a combination thereof in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction in the risk of muscle wasting. In at least particular cases, the small molecules are inhibitors of STAT3.

Abstract: Disclosed are sulfonamide compounds of Formula (I): or stereoisomers, N-oxides, prodrugs, or pharmaceutically acceptable salts thereof, wherein ring A, R1, R2, R3, R4 and R5 are defined herein. Also disclosed are methods of using such compounds in the treatment of conditions related to CYP17 enzyme, such as cancer, and pharmaceutical compositions comprising such compounds.

Abstract: Compounds having cytotoxic and/or anti-mitotic activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4 and R5 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having structure (I).

Abstract: The present invention relates to novel pyridine or pyrimidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors. The invention relates specifically to the use of these compounds and their pharmaceutical compositions to treat disorders associated with chemokine receptor modulation.

Abstract: The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin.

Abstract: This invention relates generally to the discovery of sulfonamide-containing compounds that are inhibitors of ?-secretase.

Abstract: The present invention provides N-alkylthio ?-lactams and disulfide compounds (e.g., alkyl-coenzyme A asymmetric disulfides or aryl-alkyl disulfides), compositions containing such compounds, and methods of their use as anti-bacterial agents.

Abstract: The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives thereof wherein X1, R1, R2, R3, R4, and R5 are defined as set forth in the specification. The compounds are useful as potassium ion channel inhibitors.

Abstract: The present invention provides new compounds of formula I, II or III, which have Src homology-2 containing protein tyrosine phosphatase-1 (SHP-1) agonist activity. Also provided are treatment methods using the compounds of formula I, II or III.

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

Abstract: Disclosed are sulfonamide compounds of Formula (I): or stereoisomers, N-oxides, prodrugs, or pharmaceutically acceptable salts thereof, wherein ring A, R1, R2, R3, R4 and R5 are defined herein. Also disclosed are methods of using such compounds in the treatment of conditions related to CYP17 enzyme, such as cancer, and pharmaceutical compositions comprising such compounds.

Abstract: The present application provides a method for screening compounds for cancer treatment comprising treating cancer cells with a candidate compound for sufficient time for detectable expression of a gene selected from GADD45 family; and detecting the level of expression of the gene as compared to the level of expression in the absence of the candidate compound; wherein an increased level of expression in the presence of the candidate compound as compared to expression in the absence of the candidate compound indicates that the candidate compound acts as an inhibitor of the cancer cells. In some embodiments, the method can be used for screening compounds for treatment of sorafenib-resistant hepatocellular carcinoma. The present application further provides a method for treating hepatocellular carcinoma comprising administering to a subject having hepatocellular carcinoma a therapeutic effective amount of an agonist of GADD45 family.

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, ester or stereoisomer thereof, wherein R1 to R3 and X have the significances given herein. The present invention is also directed to processes for making said compounds and uses of said compounds, in particular their use as medicaments, more particularly their use as medicaments in the treatment of cancer.

Abstract: An improved process for the preparation of aryl substituted olefinic amines such as (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)yl]-4-penten-2-amine and (2S)-(4E)-N-methyl-5-[3-(5-methoxypyridin)yl]-4-penten-2-amine and new intermediates used in said process.

Abstract: The present invention relates to new compositions and methods for protecting neuronal cells from ischemic or hypoxic events. More precisely, this invention provides new combinatorial therapies that efficiently protect neuronal cells from ischemia or hypoxia.

Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.

Abstract: The present invention relates to compositions and methods for the treatment of neurological disorders related to glutamate excitotoxicity and Amyloid ? toxicity. More specifically, the present invention relates to novel combinatorial therapies of Multiple Sclerosis, Alzheimer's disease, Alzheimer's disease related disorders, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, neuropathic pain, alcoholic neuropathy, alcoholism or alcohol withdrawal, or spinal cord injury.

Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.

Abstract: Peptidyl sensors comprise a metal-binding peptide and one or two kinase recognition sequences with a hydroxyamino acid that can be phosphorylated in the presence of a kinase.

Abstract: The present invention relates generally to pharmaceutical agents, and in particular, to metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of dual acting MMP-2 and MMP-9 inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP-2 and MMP-9 inhibitors for the treatment of pain and other diseases. Additionally, the present invention relates to methods for treating pain, addiction and/or withdrawal symptoms in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.

Abstract: The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.

Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted heterocyclic amine derivative compound 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 for targeting adaptive responses to chemotherapy are described. In various embodiments, a method comprises administering at least one compound that inhibits S6K1, mTORC, or upstream or downstream pathway components of S6K1 or mTORC, in association with administration of at least one antagonist of PPAR?, PPAR?, or PGC1?. In various embodiments, the compound that inhibits S6K1, mTORC, or upstream or downstream pathway components of S6K1 or mTORC is rapamycin, everolimus, temsirolimus, or imatinib. The antagonist of PPAR?, PPAR?, or PGC1? can be GW7647, GW6471, GW501516, GSK3787, or GSK0660.

Abstract: Novel sulphur-containing compounds and pharmaceutically acceptable salts thereof are disclosed, which have utility as anti-proliferative agents against mammalian cells. The invention provides a method for synthesizing the sulphur-containing compounds.

Abstract: The invention relates to compounds of Formula (1) and to processes for the preparation of intermediates used in the preparation of compositions containing and the uses of such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or solvate or physiologically hydrolysable, solubilising or immobilisable derivative thereof; wherein: any one or two of X.

Abstract: The present invention is directed to novel compounds. These compounds can be useful in inhibiting the activity of protein prenyltransferases including GGTase I and/or RabGGTase. The compounds can also be used as anti-cancer therapeutics including as part of methods for treating cancer, in assays, and in kits.

Abstract: The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin.

Abstract: The present invention relates to combinations and methods for the treatment of neurological disorders related to glutamate excitotoxicity and Amyloid ? toxicity. More specifically, the present invention relates to novel combinatorial therapies of Multiple Sclerosis, Alzheimer's disease, Alzheimer's disease related disorder, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, neuropathic pain, alcoholic neuropathy, alcoholism or alcohol withdrawal, or spinal cord injury, based on Baclofen and Acamprosate combination.

Abstract: The present invention provides single chain antibody-directed polymeric prodrugs containing multifunctional linkers. Methods of making the polymeric delivery systems and methods of treating mammals using the same are also disclosed.

Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.

Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, asthma and COPD.

Abstract: [Object] A compound which is useful as an EP1 receptor antagonist is provided. [Means for Solution] The present inventors investigated EP1 receptor antagonists, and confirmed that a compound having a sulfonamide structure, in which the nitrogen atom of the sulfonamide structure is substituted with 2-fluoropropyl group, 3-fluoro-2-methylpropyl group or the like, has a potent EP1 receptor antagonistic action, thereby completing the present invention. The sulfonamide compound of the present invention has a potent EP1 receptor antagonistic action and can be used as an agent for preventing and/or treating a lower urinary tract symptom or the like.

Abstract: The present invention relates to novel pyridylmethyl-sulfonamide compounds of formula (I) where: n is 0 to 4; m is 0 to 4; R1 is halogen, CN, NO2, OH, SH, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, etc.; and/or two radicals R1 together form a fused ring; R2 is H, C1-C4-alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C2-C4-alkynyl, C3-C8-cycloalkyl, C1-C4-alkyl-C3-C8-cycloalkyl or benzyl; R3 is halogen, CN, NO2, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy or C1-C4-haloalkoxy; Y is —O—, C1-C4-alkanediyl, —O—CH2—, —CH2—O—, —C(NORn)—, —S—, —S(?O)—, —S(?O)2— or —N(Rn)—; and the N-oxides, and salts thereof and their use for combating phytopathogenic harmful fungi, and also to compositions and seed comprising at least one such compound.

Abstract: The present invention relates to compositions and methods for the treatment of Alzheimer's disease and related disorders. More specifically, the present invention relates to novel combinatorial therapies of Alzheimer's disease and related disorders. In particular, the invention concerns compounds which, alone or in combination(s), can effectively modulate synapse function and/or angiogenesis and/or cell stress response. The invention also relates to methods of producing a drug or a drug combination for treating Alzheimer's disease and to methods of treating Alzheimer's disease or a related disorder.

Abstract: Disclosed are water soluble polymeric conjugates comprising the structure POLY-[Y—S—S-A]x, where POLY is a water soluble polymer; Y is a hydrocarbon-based spacer group, x is 1 to 25, S—S is a disulfide group attached to an sp3 hybridized carbon of Y; and A is a covalently linked residue of a pharmacologically active molecule. Preferably, the water soluble polymer is a PEG polymer. Also disclosed are polymeric reagents useful to prepare such conjugates, and methods of their formation and use.

Abstract: The present invention relates to novel oral pharmaceutical compositions in lyophilized form, in which the dissolution and the bioavailability of the active ingredient that they contain are improved. The compositions according to the invention comprise in particular a polyvinyl acetate/polyvinylpyrrolidone copolymer. The oral lyophilisates according to the invention are particularly suitable for the production of medicaments based on active ingredients which have low solubility or very low solubility in water or which are virtually insoluble in water.

Abstract: The present invention provides compounds that are effective in treating central nervous system disorders and maintaining normal brain function. Methods of making and using the compounds are also provided.

Abstract: Compounds of formula (I): in which R1, R2, R7, R8, R9, R10 and A have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.

Abstract: In accordance with the present invention, novel multifunctional compounds have been developed which have orthogonal reactive groups thereon, thereby facilitating preparation of compounds having multiple functional properties (e.g., a targeting moiety and a biologically active moiety). Such constructs are useful for a variety of applications, e.g., for the delivery of biologically compatible materials, and release thereof in active form. Therefore, in accordance with the present invention, there are provided multifunctional linkers of defined structure, as well as various derivatives thereof bearing one or more biologically active components thereon. Also provided in accordance with the present invention are methods for the preparation of such constructs, as well as various uses thereof.

Abstract: The present invention relates to methods and compositions for treating neuropathic pain and neuropsychiatric disorders by administering agents that are effective in reducing the effective amount, inactivating, and/or inhibiting the activity of a Na+—K+-2Cl? (NKCC) cotransporter. In certain embodiments, the Na+—K+-2Cl? co-transporter is NKCC1.