Abstract: A sorbent material is disclosed for the one-step separation of bio-macromolecules in a single pass extraction of DNA from complex mixtures of molecules and chemicals. In one embodiment, the sorbent material comprises a silanized material at least partially coated or formed with a polymer selected from the group consisting of a poly(aryl methacrylate), a poly(aryl acrylate), a poly(heteroaryl methacrylate, a poly(heteroaryl acrylate) and a copolymer thereof.

Abstract: A peptide selected from the group consisting of Ala-Hyp-Gly, Hyp-Gly-Pro, Leu-Hyp, Glu-Hyp, Gly-Pro-Hyp, Pro-Ala, Hyp-Gly and Pro-Hyp, or a pharmaceutically acceptable salt thereof has a myoblast differentiation promoting effect superior to conventional arts.

Abstract: Methods for preparing intermediates of SGLT2 inhibitors are provided, including crystalline forms and methods of crystallizing intermediates.

Abstract: Activity-generating delivery molecules comprising the structure R3—(C?O)-Xaa-NH—R4 wherein Xaa is any D- or L-amino acid residue with a non-hydrogen, substituted or unsubstituted side chain, R3—(C?O)— and —NH—R4 are independently a long chain group, each long chain group containing one or more carbon-carbon double bonds, and salts, compositions and methods of use thereof. The activity-generating delivery compounds and compositions are useful for generating activity of an active agent in a cell, tissue, or subject.

Abstract: The invention features compounds and methods relating to hydroxy-proline analog inhibitors of the ASCT1 and ASCT2 neutral amino acid transporters useful for diagnostic purposes. These analogs are potent and selective inhibitors of ASCT2 and ASCT1-mediated amino acid transport as evidenced by significantly reduced glutamine or alanine transport-associated currents or radiolabeled substrate (amino acid) uptake in Xenopus oocytes expressing ASCT2 or ASCT1. Selectivity has been established in the same manner whereby reduced substrate associated current or substrate uptake is unobserved in Xenopus oocytes expressing ATA2, SN1, or EAAT(s) (excitatory amino acid transporter). The compounds and methods of the invention include radiolabeled inhibitors that can be used in research or clinical applications (e.g., for the treatment of cancer or ischemia-related central nervous system injury).

Abstract: The invention is directed to compounds according to formula (I): where R1 is L1C(O)OT or L1C(O)OL2C(O)OT; R2 is a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, or R1; n is an integer from 0 to 5; each R3 is independently halogen or R2; R4 and R5 are independently H, halogen, CN or CF3; L1 and L2 are each independently a bond, a substituted or unsubstituted C1-C10 alkylene, C2-C10 alkenylene, or C2-C10 alkynylene; and T is H, a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, nitrophenol, or cyclopropyl. The invention is also directed to a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and to methods for providing anesthesia in mammals by administering such a pharmaceutical composition.

Abstract: The present invention provides compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.

Abstract: The present invention relates to a compound of Formula (I) or (II) or a salt thereof, wherein R is described herein. The compounds are novel hydroxy-proline analog inhibitors of the ASCT1 and ASCT2 neutral amino acid transporters.

Abstract: This disclosure relates to novel detergents for use in various procedures including, for example, nucleic acid amplification reactions such as polymerase chain reaction (PCR). Methods for preparing the modified detergents are also described.

Abstract: A DPP-4 inhibitor comprising a peptide represented by the formula (1): Xe-Pro/Ala/Hyp-Xa-Xb-Xc-Xd (wherein Xe is an amino acid residue with an isoelectric point of 5.9 to 6.3; Pro/Ala/Hyp represents Pro, Ala, or Hyp; Xa is an amino acid residue other than Hyp, Pro, and Arg, or deletion; Xb is Gly, Pro, or deletion; Xc is Pro, Ala, or deletion; and Xd is an amino acid residue or deletion) as an active component. The inhibitor can be expected to bring out an effect of lowering blood glucose levels by enhancing effects of incretins; and the inhibitor may be used as a therapeutic agent for diabetes and, in addition, can act on the immune system or the like to be thus used in treatment for skin diseases or the like.

Abstract: A novel pharmaceutical combination comprising a cytotoxic antineoplastic agent selected from a the group consisting of paclitaxel, docetaxel, doxorubicin and gemcitabine or a pharmaceutically acceptable salt thereof and at least one cyclin dependent kinase (CDK) inhibitor; wherein the said combination exhibits synergistic effects when used in the treatment of cancer. The invention also relates to a method for the treatment of cancer, using a therapeutically effective amount of the said combination.

Abstract: The present invention relates to compounds of Formula (I), combinations and use thereof for disease therapy, or pharmaceutically acceptable salt or solvate thereof, including all tautomers, stereoismers and polymorphs thereof, which are iGluR receptor inhibitors, and hence are useful in the treatment of psychiatric diseases or neurological disorders or a disease or disorder associated with abnormal activities of iGluR receptors.

Abstract: The present invention relates to substituted aryl-benzylamine compounds, to processes for their production, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.

Abstract: The invention is directed to compounds according to formula (I): where R1 is L1C(O)OT or L1C(O)OL2C(O)OT; R2 is a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, or R1; n is an integer from 0 to 5; each R3 is independently halogen or R2; R4 and R5 are independently H, halogen, CN or CF3; L1 and L2 are each independently a bond, a substituted or unsubstituted C1-C10 alkylene, C2-C10 alkenylene, or C2-C10 alkynylene; and T is H, a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, nitrophenol, or cyclopropyl. The invention is also directed to a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and to methods for providing anesthesia in mammals by administering such a pharmaceutical composition.

Abstract: Disclosed herein are thiol mediated/activated prodrugs of SO2, particularly 2,4-dinitrophenylsulfonamide analogues, having Formula-I or pharmaceutically acceptable salts thereof exhibiting tunable release profiles of SO2 with significant therapeutic efficacy against bacterial infections. Further, the present invention provides pharmaceutical compositions comprising compound of Formula I or pharmaceutically acceptable salts thereof, along with pharmaceutically acceptable carriers/excipients.

Abstract: Amino acid compositions containing a carbohydrate and any one or more kinds of alanine, proline and glycine as amino acid can suppress a rapid increase in the blood glucose level immediately after ingestion and a decrease in the blood glucose level due to prolonged exercise, and can improve exercise performance. In addition, the present invention provides inhibitors of an increase in the blood glucose level immediately after carbohydrate ingestion, an inhibitor of a decrease in the blood glucose level due to a prolonged exercise, and an exercise performance improver. Therefore, the present invention provides an energy supplement useful for those who exercise (particularly prolonged exercise).

Abstract: The present invention relates to an enantiomerically pure (+)-trans enantiomer of a compound represented by the following formula (I): wherein R1, R2, R3, R4 and R9 are as defined in the specification; enantiomerically pure intermediates thereof, to processes for the preparation of the enantiomerically pure compound and its intermediates, and to a pharmaceutical composition comprising the enantiomerically pure compound. The compound of formula (I) is useful for the treatment of diseases or disorders mediated by the inhibition of cyclin dependant kinase, such as cancer.

Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having superior glucokinase activating activity, and is a compound represented by general formula (I), or pharmacologically acceptable salt thereof: [wherein, A represents, for example, an oxygen atom or sulfur atom, R1 represents, for example, a C1-C6 alkyl group, a C1-C6 alkoxy group or a C1-C6 halogenated alkyl group, A and R1 together with the carbon atom bonded thereto form a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R2 represents a phenyl group that may be substituted with 1 to 5 group(s) independently selected from Substituent Group ? or a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R3 represents a hydroxy group or a C1-C6 alkoxy group, and Substituent Group ? consists of, for example, a halogen atom, a C1-C6 alkyl group, a C1-C6 alkyl group substituted with 1 or 2 hyd

Abstract: The invention is directed to compounds according to formula (I): where R1 is L1C(O)OT or L1C(O)OL2C(O)OT; R2 is a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, or R1; n is an integer from 0 to 5; each R3 is independently halogen or R2; R4 and R5 are independently H, halogen, CN or CF3; L1 and L2 are each independently a bond, a substituted or unsubstituted C1-C10 alkylene, C2-C10 alkenylene, or C2-C10 alkynylene; and T is H, a substituted or unsubstituted C1-C10 alkyl, C2-C10 alkenyl, or C2-C10 alkynyl, nitrophenol, or cyclopropyl. The invention is also directed to a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and to methods for providing anesthesia in mammals by administering such a pharmaceutical composition.

Abstract: The invention features compounds and methods relating to novel hydroxy-proline analog inhibitors of the ASCT1 and ASCT2 neutral amino acid transporters. These analogs are potent and selective inhibitors of ASCT2 and ASCT1-mediated amino acid transport as evidenced by significantly reduced glutamine or alanine transport-associated currents or radiolabeled substrate (amino acid) uptake in Xenopus oocytes expressing ASCT2 or ASCT1. Selectivity has been established in the same manner whereby reduced substrate associated current or substrate uptake is unobserved in Xenopus oocytes expressing ATA2, SN1, or EAAT(s) (excitatory amino acid transporter). The compounds and methods of the invention can be used in research or clinical applications (e.g., for the treatment of cancer, microbial infection, or ischemia-related central nervous system injury).

Abstract: A compound of formula (I): which is substantially free of any of the corresponding compound of formula (IB): methods of making such compounds, and the further transformation of such compounds.

Abstract: This disclosure relates to novel detergents for use in various procedures including, for example, nucleic acid amplification reactions such as polymerase chain reaction (PCR). Methods for preparing the modified detergents are also described.

Abstract: The invention relates to naphthalene derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are glycine B antagonists and are therefore useful for the control and prevention of various disorders, including neurological disorders.

Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.

Abstract: The present invention refers to compounds derived from trisubstituted 1H-pyrrole rings and aromatic rings, which have the following formula (I): wherein: R1 and R2 represent, independently, an optionally substituted C6-C10 aryl radical or an optionally substituted heteroaryl radical; A and M represent, independently, a methylene group or a single bond, in which case the adjacent aromatic ring would be attached directly to the amide group; the Y?Z group represents together and indistinctly an oxygen atom, a sulfur atom, a cis-vinylidene group, an imino group, or a methine group with a sp2-hybridized carbon atom; X represents indistinctly a methine group, a cis-vinylidene group or a nitrogen atom; and W represents a hydroxyl group, an optionally substituted C1-C6 alkyl group, an optionally substituted heteroaryl group or an optionally substituted C6-C10 aryl group; or a salt, solvate or prodrug thereof, as well as to the process for their preparation and the use thereof for the treatment of cancer.

Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.

Abstract: Prodrugs of guanfacine with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and a method for providing therapeutic benefit in the treatment of ADHD/ODD (attention deficient hyperactivity disorder and oppositional defiance disorder) with guanfacine prodrugs are provided herein. Additionally, methods for minimizing or avoiding the adverse gastrointestinal side effects associated with guanfacine administration, as well as improving the pharmacokinetics of guanfacine are provided herein.

Abstract: The invention relates to compounds having the formula: wherein: Ar, r, R3, Z, X, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

Abstract: Provided are a coenzyme Q10 nanoparticle, a method of preparing the same and a composition having the nanoparticle. According to the present invention, Coenzyme Q10 may be dissolved in only a water-miscible organic solvent, and easily made into a nano-sized particle and solubilized under a low energy condition, for example, by simple stirring. The coenzyme Q10 may be dispersion-stabilized by an amino acid or protein. The coenzyme Q10 is formed in a nano-sized particle and solubilized, an absorption rate may be increased and simultaneously deliver the amino acid and protein with the nanoparticle. Thus, the coenzyme Q10 nanoparticle can be effectively used in food, cosmetics and medicine.

Abstract: The invention concerns novel use for Hydroxyproline in a pharmaceutical or dietary food or feed compositions for promoting growth e.g. of fish and/or for treating, ameliorating, or curing certain disorders including osteoporosis, psoriasis, enteritis and gingivitis.

Abstract: Compounds are provided which are useful in the treatment of androgen receptor-associated conditions, such as age-related diseases, which compounds have the structure wherein R1, R2 and R4, are as defined herein; G is an aryl, heterocyclo or heteroaryl group, wherein said group is mono- or polycyclic, and which is optionally substituted; n is an integer of 1 or 2; m is an integer of 1 or 2; Z is oxygen (—O—) or NR4h; a prodrug ester, all stereoisomers thereof and a pharmaceutically acceptable salt thereof. A method for treating androgen receptor-associated conditions such as age-related diseases is also provided.

Abstract: A problem that the present invention is to solve is to provide: a main body of a peptide molecule which is effective for inhibition of various maladies such as osteoporosis, osteoarthritis and pressure ulcer, particularly, a dipeptide which is easy to absorb into a body in an intestine; a collagen peptide which comprises the dipeptide as an essential dipeptide; and a malady inhibitor which comprises the dipeptide as an essential effective component. As a means of solving such a problem, a collagen peptide according to the present invention is characterized by comprising a dipeptide having a structure of Hyp-Gly as an essential dipeptide. A dipeptide according to the present invention is characterized by having a structure of Hyp-Gly. A malady inhibitor according to the present invention is characterized by comprising a dipeptide having a structure of Hyp-Gly as an essential effective component.

Abstract: The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula III, wherein R, R1, and R? are as defined in the specification, or a salt thereof, and a compound of formula IV wherein R, R1, R2 and R? are as defined in the specification, and processes of manufacturing these.

Abstract: To provide a pyrrolidine analogue having an inhibitory activity on the induction of allodynia, a method for producing the pyrrolidine analogue, and an agent for preventing a neurogenic pain. A pyrrolidine analogue which is a compound represented by the general formula (I) [wherein HOOC-? represents an aromatic substituent having at least one carboxy group attached to the benzene ring] or a salt or ester of the compound. The compound has a potent inhibitory effect on the induction of allodynia.

Abstract: The invention describes compounds useful for labelling molecules of interest (i.e. analytes), particularly biomolecules such as peptides, proteins, oligonucleotides and nucleic acids, and also methods for analysing, detecting and/or isolating these labelled molecules using mass spectrometry. The compound in one aspect is a mass marker for labelling of an analyte detectable by mass spectrometry such as neutral loss mass spectroscopy, in which the mass marker comprises a neutral loss mass modifier linked via a first collision cleavable linker to a reactive group having reactive functionality for attachment to the analyte. The neutral loss mass modifier upon cleavage from the analyte during mass spectroscopy is uncharged.

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 metabolic diseases and disorders such as, for example, type II diabetes mellitus.

Abstract: The present invention provides compounds comprising amino acid R groups, compositions comprising the same, and methods of inhibiting neuraminidase and/or treating influenza, Pseudomonas aeruginosa, or Bacteroides fragilis infection in a mammal.

Abstract: Compounds of formula I in which R1, R2, R3, each X, L, Y, Cy, Lp, D and n have the meanings as set out in the specification, and corresponding compounds in which the unsubstituted or substituted amidine group is replaced with an unsubstituted or substituted aminomethyl group, are useful as serine protease inhibitors.

Abstract: The subject invention pertains to pentafluorosulfonyl (SF5) substituted pyrroles, thiophenes, 3-pyrrolines and 2,5-dihydrothiophenes, as well as methods for their synthesis.

Abstract: Methods for regulating glucagon release and of treating hypoglycemia, and for screening drug candidates for treating hypoglycemia. The methods are useful for treating diabetes mellitus and screening drug candidates for potential efficacy.

Abstract: Compounds are provided which are useful in the treatment of androgen receptor-associated conditions, such as age-related diseases, which compounds have the structure wherein R1, R2 and R4, are as defined herein; G is an aryl, heterocyclo or heteroaryl group, wherein said group is mono- or polycyclic, and which is optionally substituted; n is an integer of 1 or 2; m is an integer of 1 or 2; Z is oxygen (—O—) or NR4h; a prodrug ester, all stereoisomers thereof and a pharmaceutically acceptable salt thereof. A method for treating androgen receptor-associated conditions such as age-related diseases is also provided.

Abstract: Benzenesulfonamide derivative compounds corresponding to the general formula (I): and their pharmaceutically acceptable addition salts; a process for preparation of such compounds; pharmaceutical compositions containing such compounds, and the use of such compounds as a pharmacologically active substance, in particular in the treatment of neurodegenerative diseases, cardiovascular diseases, inflammatory diseases; hypercholesterolemia, and diabetes.

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity.

Abstract: It was found that a fluoro derivative can be produced by reacting a hydroxy derivative with sulfuryl fluoride (SO2F2) in the presence of an organic base or in the presence of an organic base and “a salt or complex comprising an organic base and hydrogen fluoride”. According to the present production process, it is not necessary to use perfluoroalkanesulfonyl fluoride, which is not preferable in industrial use, and it is possible to advantageously produce optically-active fluoro derivatives, which are important intermediates of medicines, agricultural chemicals and optical materials, specifically 4-fluoroproline derivatives, 2?-deoxy-2?-fluorouridine derivatives, optically-active ?-fluorocarboxylate derivatives, and the like, even in a large scale.

Abstract: This invention relates to certain biphenyl amino acid compounds, compositions, and methods for treating or preventing obesity and related diseases.

Abstract: Provided are processes for the preparation of complexes that are useful in purifying compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The processes can reduce the number of steps needed to obtain the target compounds and the complexes formed in the processes are typically provided in a crystalline form.

Abstract: The present invention relates to an enantiomerically pure (+)-trans-enantiomer of a compound represented by the following formula (I): wherein R1, R2, R3, R4 and R9 are as defined in the specification; enantiomerically pure intermediates thereof, to processes for the preparation of the enantiomerically pure compound and its intermediates, and to a pharmaceutical composition comprising the enantiomerically pure compound. The compound of formula (I) is useful for the treatment of diseases or disorders mediated by the inhibition of cyclin dependant kinase, such as cancer.

Abstract: Novel preparative methods for fluoroalkyl arylsulfinyl compounds are disclosed. Fluorinated compounds as useful fluorinated compounds, intermediates, or building blocks are disclosed. Useful applications of the fluoroalkyl arylsulfinyl compounds are shown.

Abstract: This invention relates to a supplement, the use thereof and method for supplementing the concentration of free cellular L-proline in an organism, for restricting dehydration of such an organism, the supplement comprising an effective amount of free L-proline. The supplement is effective in reducing the levels of free radicals in organisms experiencing water stress. This invention further relates to a method of treating dehydration in humans and animals including the step of administering to an individual in need thereof an effective amount of a supplement according to the third aspect of the invention. An effective amount of free L-proline is typically between 20 and 1000 mg, preferably 100 mg free L-proline per kilogram body mass of the organism, three times a day.

Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.