Abstract: The present invention relates to amino acids, complexes, and compounds comprising deuterium and tritium isotopes preferably alpha deuterated amino acids, polypeptides, antibodies, derivatives and saccharide-amino acid complexes and conjugates. In some embodiments, the invention relates to methods of using compounds comprising deuterium for imaging biochemical concentrations and distributions in mammalian tissues using nuclear magnetic resonance spectroscopy. In some embodiments, the invention relates to the used of said amino acids derivatives and complexes in boron neutron capture therapy. In some embodiments, the present invention relates to the preparation of amino acids, polypeptides, antibodies, derivatives and saccharide complexes/conjugates comprising heavy hydrogen isotopes. In some embodiments, the invention relates to racemizing amino acids starting from compositions of any optical purity.

Abstract: A method of electrochemically preparing a crystalline, porous, metal-organic framework material comprising at least one at least bidentate organic compound coordinately bound to at least one metal ion, in a reaction medium comprising the at least one bidentate organic compound, wherein at least one metal ion is provided in the reaction medium by the oxidation of one anode comprising the corresponding metal.

Abstract: The present invention relates to dephenolic compounds, an example of which is shown below, which are functionalized, and polymers formed from the same. Polymers formed from the functionalized diphenolics are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.

Abstract: The present invention provides methods for preparing a polymeric compound of Formula I: or pharmaceutically acceptable salt thereof. The present invention also provides useful intermediates for preparing the compound of Formula I or pharmaceutically acceptable salt thereof.

Abstract: It is intended to provide a novel compound that has an excellent ?-secretase inhibitory effect and specifically inhibits A? production. The present invention provides a compound of the following formula (1) or a pharmaceutically acceptable salt thereof: wherein R1 represents a linear or branched alkyl group having 1 to 4 carbon atoms or a phenyl group; R2 represents a linear or branched alkyl group having 1 to 4 carbon atoms which may be substituted by one or more phenyl or halogenophenyl groups; R3 represents a linear or branched alkyl group having 1 to 4 carbon atoms which may be substituted by one or more hydroxyl groups; R4 represents a linear or branched alkyl group having 1 to 4 carbon atoms; and the symbol “*” represents a chiral center.

Abstract: Compounds are synthesized that contain nitrogen and hindered phenol functionalities of an aromatic amine and hindered phenol for use as oxidative stabilizers for organic materials, paints, lubricants, elastomers, and in other applications. The disclosed methods can efficiently synthesize target monomers and polymers without the use of expensive catalysts. Further, the disclosed methods can scale up to industrially useful quantities. In general, the methods provide an improved, highly efficient and economical process for the synthesis of macromonomers having nitrogen containing moiety and sterically hindered phenols and their corresponding polymers.

Abstract: Novel calcilytic compounds of Formula (I), pharmaceutical compositions, methods of synthesis, and methods of using them are provided.

Abstract: Novel calcilytic compounds and methods of using them are provided.

Abstract: A method of combating breast cancer in a mammalian individual, the method comprising administering to the individual an agent which reduces the function of the gamma secretase (GS) complex.

Abstract: A method of reducing side effects of damage in a human subject exposed to radiation includes administering to the human subject carbon nanotubes in a pharmaceutically acceptable carrier after or prior to exposure to radiation. A composition for reducing radical damage includes a carbon nanotube which is functionalized (1) for substantial water solubility and (2) with a radical trapping agent appended to the carbon nanotube forming a radical scavenger-carbon nanotube conjugate.

Abstract: Disclosed is a linear polyimide precursor having an intrinsic viscosity of not less than 0.5 dL/g and composed of a repeating unit represented by at least one formula selected from the group consisting of the general formula (1) below and the general formula (2) below. In the general formulae (1) and (2), X represents a divalent aromatic group other than a residue of 1,4-bis(4-aminophenoxy)benzene and a residue of bis(4-amino-3-methylphenyl)methane or an aliphatic group. Since this linear polyimide precursor has high glass transition temperature and high toughness, while exhibiting excellent solubility and thermoplasticity, it is suitably used as a raw material for an asymmetric polyimide which is useful as an adhesive resin for flexible printed circuits (FPC) or the like.

Abstract: The invention provides crystalline solid forms of (S)-4-((2S,3S)-7-carbamoyl-1,1-diethyl-3-methoxy-1,2,3,4-tetrahydronaphthalen-2-ylamino)-2-cyclohexylmethyl-butyric acid. The invention also provides pharmaceutical compositions comprising such crystalline solid forms, methods of using such crystalline solid forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline solid forms.

Abstract: The invention generally relates to hapten compounds comprising either (+)methamphetamine or (+)amphetamine conjugated to a linker. Generally speaking, hapten compounds of the invention may be used to elicit an immune response to one or more of (+)methamphetamine, (+)amphetamine, or (+)MDMA.

Abstract: A compound of formula (III): or a salt, solvate and chemically protected form thereof, wherein: R5 is an optionally substituted C5-20 aryl or C4-20alkyl group; L? is a single bond, —O— or —C(?O)—; A is selected from the group consisting of: formulae (i) (ii) (iii) wherein X and Y are selected from the group consisting of: O and CR3; S and CR3; NH and CR3; NH and N; O and N; S and N; N and S; and N and O, and where the dotted lines indicate a double bond in the appropriate location, and where Q is either N or CH; D is selected from: formulae (i) (ii) (iii) (iv) (v) (vii) (viii) (ix) B is selected from the group consisting of: formulae (A) (B) where RP6 is selected from fluoro and chloro; and R2 is either: (i) —CO2H; (ii) —CONH2; (iii) —CH2—OH; or (iv) tetrazol-5-yl.

Abstract: Separating different types of nanotubes from one another includes providing a sample of heterogeneous nanotubes comprising a first and second type of carbon nanotube; providing a first type of molecule; introducing the first type of molecule to the sample; binding the first type of molecule to the first type of carbon nanotube; and separating the first type of carbon nanotube from the sample. A second type of molecule may be introduced to the sample followed by binding the second type of molecule to the second type of carbon nanotube; and separating the second type of carbon nanotube from the sample. The sample may comprise a third type of carbon nanotube. A third type of molecule may be introduced to the sample followed by binding the third type of molecule to the third type of carbon nanotube; and separating the third type of carbon nanotube from the sample.

Abstract: Compositions and methods of producing components of protein biosynthetic machinery that include orthogonal tRNA's, orthogonal aminoacyl-tRNA synthetases, and orthogonal pairs of tRNA's/synthetases are provided. Methods for identifying these orthogonal pairs are also provided along with methods of producing proteins using these orthogonal pairs.

Abstract: The present invention herein provides, for instance, a stable isotope-labeled phenylalanine wherein a carbon atom of the phenyl group linked to an amino acid residue is 13C, 2 to 4 carbon atoms of the remaining 5 carbon atoms constituting the phenyl group are 12C atoms to which deuterium atoms are bonded, and the remaining carbon atoms are 13C atoms to which hydrogen atoms are linked, and a stable isotope-labeled tyrosine wherein a carbon atom of the phenyl group linked to an amino acid residue is 13C, the carbon atom bonded to the hydroxyl group (OH group) of the phenyl group is 12C or 13C, 2 to 4 carbon atoms of the remaining 4 carbon atoms constituting the phenyl group are 12C atoms to which deuterium atoms are bonded, and the remaining carbon atoms are 13C atoms to which hydrogen atoms are linked.

Abstract: Compounds of formula (I) are provided, wherein X is CH?CH, CH2O wherein the oxygen atom is bound to ring B, or OCH2 wherein the oxygen atom is bound to ring A; Y is hydrogen, straight or branched C1-C6 alkyl or a pharmaceutically acceptable inorganic cation; R1 is ethyl or cyclopropyl; and R2 and R3 are the same or different and are selected from F, Cl, Br, CF3 and OCF3. The compounds are useful for the treatment of autoimmune diseases, inflammatory diseases, organ transplant rejection, and malignant neoplasia. Pharmaceutical compositions comprising the compounds, methods of using the compounds, and methods for preparing the compounds are also provided.

Abstract: Compounds of formulas 1 through 17 provided in the specification specifically or selectively inhibit either the cytochrome P450RAI-1 enzyme or the cytochrome P450RAI-2 enzyme.

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 VI, or a salt thereof, wherein R1, R2, R3 and R? are as defined in the specification, and processes of manufacturing this compound including intermediates.

Abstract: This invention provides analogs of hemiasterlin, methods of synthesis of the analogs and use of the analogs as a cytotoxic anti-mitotic agents.

Abstract: The present invention refers to a process for preparing a compound of formula (I) through a carboxymethylation reaction occurring in the presence of a suitable alkylating agent and of a base, without the need of monitoring the pH of the reaction environment. The compound of formula (I) is a useful intermediate in the preparation of diagnostic contrast agents for MRI techniques.

Abstract: Crystals of a salt of 4?-{2-[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethylamino]ethoxy}-3-isopropyl-3?,5?-dimethylbiphenyl-4-carboxylic acid. The ? type, ? type and ? type crystals produced by treating hydrochloride of 4?-{2-[(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethylamino]ethoxy}-3-isopropyl-3?,5?-dimethylbiphenyl-4-carboxylic acid with specified solvents, which can be discriminated by the characteristic diffraction peaks of powder X-ray diffractometry and the like.

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

Abstract: Disclosed herein are aromatic amide derivatives of the formulae: wherein X1 and X2 are independently selected from the group consisting of —OH, —OR, —OM, —NH2, and —NHR; M is a metal; and R, R1, and R2 are independently selected hydrocarbyl groups.

Abstract: A compound of formula (I) wherein R1 represents aryl optionally substituted by a heterocyclic group or a heterocyclic group optionally substituted by aryl wherein each aryl or heterocyclic group is optionally substituted; the group —(CH2)m-T-(CH2)n—U—(CH2)p— is attached at either the 3 or 4 position in the phenyl ring as indicated by the numbers in formula (I) and represents a group selected from one or more of the following: O(CH2)2, O(CH2)3, NC(O)NR4(CH2)2, CH2S(O2)NR5(CH2)2, CH2N(R6)C(O)CH2, (CH2)2N(R6)C(O)(CH2)2, C(O)NR7CH2, C(O)NR7(CH2)2, and CH2N(R6)C(O)CH2O; V represents O, S, NR8 or a single bond; q represents 1, 2, or 3; W represents O, S, N(R9)C(O), NR10, or a single bond; R2 represents halo, a C1-4 alkyl group which is optionally substituted by one or more fluoro, a C1-4 alkoxy group which is optionally substituted by one or more fluoro, a C1-4 acyl group, aryl, an aryl C1-4 alkyl group, CN or NO2; r represents 0, 1, 2 or 3; R3 halo, a C1-4 alkyl group which is optionally substutited by one or more

Abstract: Novel Calcilytic compounds and methods of using them are provided.

Abstract: The present invention relates to amphiphilic squaraine dyes of the general formula (1) as shown below Formula (1) wherein, R1=—(CH2—CH2—O)n—CH3, n=4-8, or —(CH2)n—CO2X, n=3-6, X=H, succinamide and R2=—CH3 or —(CH2—CH2—O)n—CH3, n=4-8 and pharmaceutically acceptable derivatives thereof, for use as near infrared fluorescence probes in photodynamic diagnostic and biological, biochemical and industrial applications.

Abstract: This invention provides aryl and heteroaryl compounds of Formula (I) as described herein, and methods of their preparation. Also provided are pharmaceutical compositions made with the compounds of Formula (I) and methods for making such compositions. The compounds of Formula (I) may activate an erythropoietin receptor and thus, may be useful to induce red blood cell production. The compounds of Formula (I) and compositions including compounds of Formula (I) may be useful in a variety of applications including the management, treatment and/or control of diseases caused at least in part by deficient (or inefficient) EPO production relative to hemoglobin level.

Abstract: A carboxylic acid derivative of formula (I): wherein R1 is —COOH, —COOR6, etc.; A is a single bond, alkylene, etc.; R2 is alkyl, alkoxy, etc.; B is a carbocyclic ring or a heterocyclic ring; Q is alkylnene-Cyc2, etc.; D is a linking chain; and R3 is alkyl, a carbocyclic ring or a heterocyclic ring, or a non-toxic salt thereof. The compound of formula (I) binds to PGE2 receptor, especially subtypes EP3 and/or EP4 and show the antagonizing activity, are useful for the prevention and/or treatment of diseases induced pain, itch, urticaria, allergy, urinary frequency, urinary disturbance, Alzheimer's disease, cancer, dysmenorrhea, endometriosis, etc.

Abstract: The present invention provides a compound of formula I processes for preparing such compounds, their the utility in treating clinical conditions including lipid disorders (dyslipidemias) whether or not associated with insulin resistance, methods for their therapeutic use and pharmaceutical compositions containing them.

Abstract: The present invention relates to benzoyl-substituted alanines of the formula I in which the variables R1 to R12 are as defined in the description, and to their agriculturally useful salts, to processes and intermediates for their preparation, and to the use of these compounds or of compositions comprising these compounds for controlling unwanted plants.

Abstract: A new class of non-glycosidic and non-peptidic inhibitors of selectins with low molecular weight according to the general formula 1 is described, as well as methods for their production. These compounds represent a new class of non-toxic, in vivo anti-inflammatory effective inhibitors of selectins, and do not exhibit the disadvantages of the glycosidic inhibitor complexes, and are furthermore more potent in vitro, compared to the known drug bimosiamose. Furthermore, medicaments containing the compounds and their uses in the treatment of diseases are described.

Abstract: Polycarbonate is prepared by reactive extrusion on a reactive extruder. A method incorporates the steps of introducing a polycarbonate oligomer, an activated carbonate residue, and a transesterification catalyst to the extruder through a feed section. The extruder has the feed section, a polycarbonate exit section, and a reaction section between the feed section and the polycarbonate exit section. The reaction section is made up of at least one conveying section, kneading sections, and venting sections. The configuration of the reaction section requires that at least one venting section be disposed between each pair of kneading sections, and that the kneading sections and venting sections are selected such that the number of venting sections minus the number of kneading sections is greater than or equal to one. The method further contains the step of extruding the reaction components at a temperature in a range between 100° C. and 500° C.

Abstract: LXR nuclear receptor agonists have been previously shown to increase cholesterol efflux, raise plasma HDL cholesterol, stimulate cholesterol excretion, and reduce atherosclerotic lesions. However, these agonists have also been associated with the unwanted side effect of hypertriglyeridemia. This hypertriglyeridemia appears to be mediated by the LXR? subtype rather than LXR?, which suggests that LXR?-selective agonists are attractive candidates for modulation of human lipid metabolism. The present application provides novel LXR?-selective ligands that preferably modulate LXR? over LXR?. These ligands may be used to treat a variety of diseases associated with LXR, such as for example lipid metabolism disorders, atherosclerosis, Alzheimer disease, and inflammation.

Abstract: The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen or lower alkyl; R3, R4, R5 and R6 are each hydrogen, halogen, lower alkyl or lower alkoxy; R7 and R8 are each hydrogen, halogen, lower alkyl, halo-lower alkyl, lower alkoxy, cycloalkyl, aryl, heteroaryl, cyano, a hydroxyl group, lower acyl, carboxy or the like; R9 is —C(O)—R10, -A1-C(O)—R10, —O-A2-C(O)—R10 or a tetrazol-5-yl group, which exhibit potent and selective ?3-adrenoceptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

Abstract: The present invention provides a radiolabeled ligand which is highly selective and potent for glutamate transporters and is usable in specifically detecting the glutamate transporter. Specifically, the present invention provides a 3-[3-(benzoylamido)benzyloxy]aspartic acid having a radioactive substituent on the benzoyl group which is represented by the following formula (1), or an ester or salt thereof: wherein X represents a substituent containing a radioactive atom(s) which is selected from a straight or branched lower aliphatic alkyl group, a hydroxyl group, a straight or branched lower aliphatic alkoxy group, an amino group, a straight or branched lower aliphatic acylamido group, a halogen atom and a straight or branched lower aliphatic haloalkyl group; and R1 and R2 each represents a hydrogen atom, a straight or branched lower aliphatic alkyl group or an acetoxymethyl group.

Abstract: Compounds of the formula where the variables have the values described in the specification are antagonists of RAR?retinoid receptors.

Abstract: The invention relates to novel diazoketone derivatives. The invention also relates to processes for homologation of these diazoketone derivatives. The processes are useful for preparing compounds that are caspase inhibitors.

Abstract: Method for the preparation of asymmetric alkynylated ?-amino esters of the formula wherein R1 and R2 are independently optionally substituted alkyl cycloalkyl, aryl or heteroaryl, and Y is hydrogen or a nitrogen protecting group.

Abstract: Malodour formation reducing compounds alpha-N-(3-Methyl-5-phenylpentanoxycarbonyl)-L-glutamine, alpha-N-(2-Methyl-5-phenylpentanoxycarbonyl)-L-glutamine, and alpha-N-(2,4-Dimethyl-4-phenylbutanoxycarbonyl)-L-glutamine, and their salts, compositions comprising such compounds, including cosmetic products, personal care products, and deodorant products, and methods forming such products and their use. The compounds are useful to reduce the formation of human malodour resulting from bacterial degradation of compounds naturally present in sweat, in particular axilliary malodour.

Abstract: [PROBLEM] The compound that selectively binds to BLT2 and the preventive and/or therapeutic drug for BLT2-mediated disease such as skin disease are needed. [MEANS FOR SOLVING THE PROBLEMS] The present invention provides the compound with BLT2 binding activity, salt thereof, solvate thereof or prodrug thereof. Since the compound with BLT2 binding activity, particularly the compound represented by the formula (I) salt thereof, solvate thereof or prodrug thereof (symbols in formula have the same meanings as specification.) have BLT2 binding activity, it is useful for prevention and/or therapy of BLT2 mediated diseases, e.g., dermatosis, intestinal disease, HIV infection, acquired immunodeficiency syndrome, rejection to transplant, transplant rejection, graft-versus-host disease, autoimmune disease, allergic disease, inflammation, infection, ulcers, lymphoma, malignant tumor, leucaemia, arterial sclerosis, hepatitis, hepatic cirrhosis or cancer, etc.

Abstract: Novel thyroid receptor ligands are provided having the general formula I wherein X, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined herein. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolic dysfunction or which are dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.

Abstract: This invention relates to methods for treating heart failure, thromboembolic disorders, and pulmonary fibrosis, comprising administering an effective amount of a compound of formula (I) in which the several variables are as defined in the specification and claims.

Abstract: The present invention provides the S enantiomer of a compound of formula (I); wherein R1 represents 2,4-difluorophenyl or cyclohexyl as well as pharmaceutically acceptable salts, solvates, crystalline forms and prodrugs thereof, to processes for preparing such compounds, to their the utility in treating clinical conditions including lipid disorders (dyslipidemias) whether or not associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: Arylcycloalkyl derivatives having branched side chains, processes for their preparation and their use as pharmaceuticals The invention relates to arylcycloalkyl derivatives having branched side chains and to their physiologically acceptable salts and physiologically functional derivatives. What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistence is involved.

Abstract: The present invention is directed to compounds, compositions, and use of compounds the structural Formula (I)

Abstract: This invention relates to novel compounds, which are thyroid receptor ligands, and to methods of preparing such compounds. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolism dysfunction or which are dependent upon the expression of a T3 regulated gene, wherein a compound as described herein is administered in a therapeutically effective amount.

Abstract: Arylaminopropane analogues are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a method for the treatment of glaucoma using compositions containing one or more of the compounds of the present invention.

Abstract: Compounds of the general formula (I) wherein R1 represents halogen, R2 and R3 represent H or halogen, and R4 represents C3-8-cycloalkyl or optionally substituted phenyl, pharamceutical compositions containing such materials, and methods of using such materials in the treatment of various diseases are disclosed and claimed.