Abstract: A polymer comprising a first repeating unit represented by Formula 1: wherein, in Formula 1, groups and variables are the same as described in the specification.

Abstract: The present invention relates to inhibitors of the activity of Complex (III) of the mitochondrial electron transport chain and use thereof in treatment and/or prevention of cancers presenting tumour-initiating cells. The present invention further relates to pharmaceutical compositions containing said inhibitors alone or in combination with other pharmaceutically active agents, and their use as medicaments or as agrochemicals where their properties as inhibitors of the mitochondrial respiration is of benefit.

Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.

Abstract: The present disclosure is directed to a reactive ester agent for conjugating a click-reactive group to a carrier molecule or solid support. The reactive ester agent has the general formula IA, wherein the variables R1, R2, R3, Ra and L are described throughout the application.

Abstract: The present invention provides a chiral phase-transfer catalyst of the following formula (I): The compound (I) can be produced by reacting a 2,2?-dimethylene bromide-1,1?-biphenyl derivative, which can be produced through comparatively small number of steps, with an easily available secondary amine.

Abstract: A quaternary ammonium salt represented by formula (5) (wherein R1 represents an alkyl group having 1 to 4 carbon atoms, R2 represents an alkyl group having 1 to 10 carbon atoms, R3 represents an alkyl group having 1 to 10 carbon atoms that is optionally substituted with one or more phenyl groups; or a phenyl group that optionally has one or more groups selected from the group consisting of alkyl groups having 1 to 10 carbon atoms and a trifluoromethyl group, R4 represents an alkyl group having 1 to 4 carbon atoms, R5 represents an alkyl group having 1 to 10 carbon atoms, C* represents an asymmetric carbon atom, and X? represents a halide ion) can be used as a catalyst having good stability under basic conditions.

Abstract: Compounds and methods are disclosed that are useful for noninvasive imaging in the near-infrared spectral range. The cyanine compounds of Formula I are presented: wherein Q is a portion of a polymethine bridge: Also included are bioconjugates of the compounds of Formula I, methods of labeling biomolecules with the compounds, and methods of imaging.

Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.

Abstract: The present invention is related to novel tricyclic compounds of formula (I) having TRPA1 receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use as pharmacological tools, or as irritant incapacitants, or in the treatment of diseases linked to the modulation of the TRPA1 receptors in animals, in particular humans.

Abstract: An optically active bisbenzyl compound or a racemic bisbenzyl compound represented by formula (2) that has axial chirality. An optically active azepine derivative or a racemic azepine derivative represented by formula (3). Methods of producing an optically active quaternary ammonium salt compound represented by formula (8).

Abstract: This invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.

Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract: Provided are novel organic electroluminescent compounds and organic electroluminescent devices using the same. Since the organic electroluminescent compound exhibits good luminous efficiency and excellent life property compared to the existing material, it may be used to manufacture OLED devices having superior operation life and consuming less power due to improved power efficiency.

Abstract: The present invention discloses an optically active quarternary ammonium salt having axial asymmetry and a method for producing an ?-amino acid and a derivative thereof using the same. The optically active quarternary ammonium salt having axial asymmetry of the present invention is a chiral phase-transfer catalyst that has a simple structure and that can be produced in a smaller number of process steps. The compound of the present invention is very useful as a phase-transfer catalyst in the synthesis of an ?-alkyl-?-amino acid and a derivative thereof as well as an ?,?-dialkyl-?-amino acid and a derivative thereof. Therefore, the compound of the present invention can be used in the development of novel foods and pharmaceuticals.

Abstract: The present invention discloses an optically active quarternary ammonium salt having axial asymmetry and a method for producing an ?-amino acid and a derivative thereof using the same. The optically active quarternary ammonium salt having axial asymmetry of the present invention is a chiral phase-transfer catalyst that has a simple structure and that can be produced in a smaller number of process steps. The compound of the present invention is very useful as a phase-transfer catalyst in the synthesis of an ?-alkyl-?-amino acid and a derivative thereof as well as an ?,?-dialkyl-?-amino acid and a derivative thereof. Therefore, the compound of the present invention can be used in the development of novel foods and pharmaceuticals.

Abstract: The present invention relates to novel noncardiotoxic compounds and pharmaceutical compositions useful in the treatment of a variety of disorders including the treatment of depression, allergies, psychoses, cancer and gastrointestinal disorders. In particular, the present invention describes pharmaceutical compositions that mitigate life-threatening arrhythmias such as torsade de pointes. Torsade de pointes is a particular cardiac problem associated with many therapeutic agents and has been implicated as a possible cause of sudden death, particularly in those individuals with a past history of disturbances of cardiac rhythm, myocardial infarction, congenital repolarization abnormalities and cardiac risk factors such as hyperlipidemia and age. This arrhythmia is a variant of paroxysmal ventricular tachycardia associated with a prolonged QTc interval or prominent U waves on the ECG.

Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract: Provided herein are tetrazolone FASN inhibitors of the formula (I): or a pharmaceutically acceptable form thereof; wherein the variables RA, RB and RC are defined herein. Also provided herein are pharmaceutical compositions of the compounds provided herein as well as methods of their use for the treatment of various disorders such as hyperproliferative disorders, inflammatory disorders, obesity-related disorders and microbial infections.

Abstract: The present invention relates to novel Tricyclic Heterocycle Derivatives, pharmaceutical compositions comprising the Tricyclic Heterocycle Derivatives and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. R1 is formula (Ia), (Ib) or (Ic); R2 is alkvl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl. any of which can be optionally substituted with R11; M1 is —CH—. —C(halo)- or —N—; Y is —C(O)—, —S—. —S(O)—, —S(O)2—, —CH2— or —O—, such that Y is not —O— when an adjacent atom is N.

Abstract: The invention relates to compounds according to general formula (1) and/or their enantiomers, diastereomers as well as their pharmaceutically compatible salts, and to the use thereof for producing a medicament suited for treating diseases associated with misfolded proteins.

Abstract: Polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.

Abstract: The invention relates to certain fused ring compounds, or pharmaceutically acceptable salts thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.

Abstract: The present invention provides a production method of an allylic amine represented by the formula (III): wherein R3 is as defined in the specification, which comprises reacting by an allylic alcohol represented by the formula (II): wherein R3 is as defined in the specification, with sulfamic acid, in the presence of a phosphoramidite ligand represented by the formula (I): wherein each symbol is as defined in the specification, and an iridium complex. According to the present invention, a primary allylic amine can be produced directly from an allylic alcohol, without use of an activator for an allylic alcohol and conversion of an allylic alcohol into an activated compound thereof.

Abstract: A process for the preparation of 10,11-dihydro-10-hydroxy-5H-dibenz[b,f]azepine-5-carboxyamide by hydrolysis of 5-cyano-10,11-dihydro-10-hydroxy-5H-dibenz[b,f]azepine with peroxy compounds in alkali medium and in the presence of solvents.

Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract: A material for organic electroluminescence device with specific structure having poor symmetry. An an organic electroluminescence device comprising a cathode, an anode and an organic thin film layer which is sandwiched between the cathode and the anode and comprises at least one layer, wherein at least one layer in the organic thin film layer contains a material for the organic electroluminescence device described above. An organic electroluminescence device with excellent efficiency of light emission, without pixel defects and which is superior in heat resistance is obtained.

Abstract: The present invention is related to novel tricyclic compounds of formula (I) having TRPA1 receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use as pharmacological tools, or as irritant incapacitants, or in the treatment of diseases linked to the modulation of the TRPA1 receptors in animals, in particular humans.

Abstract: A guanidine compound having a biaryl skeleton represented by the following formula (1), which is useful as a catalyst for various asymmetric reactions.

Abstract: Disclosed herein are analogs of clozapine and pharmaceutically acceptable salts, esters, amides, or prodrugs thereof; methods of synthesizing the analogs; and methods of using the analogs for treating neuropsychiatric disorders. In some embodiments, the analogs are amino substituted diaryl[a,d]cycloheptenes.

Abstract: The present disclosure relates to 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: An optically active quaternary ammonium salt compound represented by formula (1), wherein R1 represents a halogen, a C1-8 alkyl which is optionally substituted and which is linear, branched, or cyclic, a C2-8 alkenyl which is optionally substituted, a C2-8 alkynyl which is optionally substituted, a C6-14 aryl which is optionally substituted, a C3-8 heteroaryl which is optionally substituted, a C1-8 alkoxy which is optionally substituted and which is linear, branched, or cyclic, or a C7-16 aralkyl which is optionally substituted; R2 and R21 each independently represents hydrogen, halogen, nitro, a C1-8 alkyl which is optionally substituted and which is linear, branched, or cyclic, a C2-8 alkenyl which is optionally substituted, a C2-8 alkynyl which is optionally substituted, a C6-14 aryl which is optionally substituted, a C1-8 alkoxy which is optionally substituted and which is linear, branched, or cyclic, or a C7-16 aralkyl which is optionally substituted; one of combinations of R1 and R21, and R2 and R

Abstract: The present invention discloses an optically active quarternary ammonium salt having axial asymmetry and a method for producing an ?-amino acid and a derivative thereof using the same. The optically active quarternary ammonium salt having axial asymmetry of the present invention is a chiral phase-transfer catalyst that has a simple structure and that can be produced in a smaller number of process steps. The compound of the present invention is very useful as a phase-transfer catalyst in the synthesis of an ?-alkyl-?-amino acid and a derivative thereof as well as an ?,?-dialkyl-?-amino acid and a derivative thereof. Therefore, the compound of the present invention can be used in the development of novel foods and pharmaceuticals.

Abstract: A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.

Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.

Abstract: The present invention provides a chiral phase-transfer catalyst of the following formula (I): The compound (I) can be produced by reacting a 2,2?-dimethylene bromide-1,1?-biphenyl derivative, which can be produced through comparatively small number of steps, with an easily available secondary amine.

Abstract: The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).

Abstract: The invention relates to compounds according to general formula (1) and/or their enantiomers, diastereomers as well as their pharmaceutically compatible salts, and to the use thereof for producing a medicament suited for treating diseases associated with misfolded proteins.

Abstract: An organic electroluminescence element, which contains at least one organic layer that includes a luminescent layer between a pair of electrodes, wherein the organic layer contains at least one compound represented by formula (1): wherein R11 and R12 each independently represent an aryl or heteroaryl group; when R11 or R12 is a phenyl group, it has no nitrogen-containing heterocyclic group on R11 or R12 as a substituent; Ar11 and Ar12 each independently represent a group represented by formula (2): wherein Ar21 represents an arylene or heteroarylene group; R21, R22, R23, and R24 each independently represent a substituent or a hydrogen atom; L2 represents a substituted or unsubstituted o-arylene or vinylene group, —NR— (R represents a substituent), —O—, or —S—; and m is 0 or 1.

Abstract: Specific phenylalanine derivatives or pharmaceutically acceptable salts thereof have an antagonistic effect on the ?4 integrins and, therefore, are usable as therapeutic agents or preventive agents for diseases in which ?4 integrin-depending adhesion process participates in the pathology, such as inflammatory diseases, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection.

Abstract: Disclosed herein are analogs of clozapine and pharmaceutically acceptable salts, esters, amides, or prodrugs thereof; methods of synthesizing the analogs; and methods of using the analogs for treating neuropsychiatric disorders. In some embodiments, the analogs are amino substituted diaryl[a,d]cycloheptenes.

Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).

Abstract: Drug substances comprising a pharmaceutically acceptable organic acid addition salt 6f amine containing pharmaceutically active compounds useful for the treatment of a therapeutic ailment administration and exhibiting prophylactic properties when employed in non-therapeutic administration.

Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.

Abstract: A process for the preparation of 10,11-dihydro-10-hydroxy-5H-dibenz[b,f]azepine-5-carboxyamide by hydrolysis of 5-cyano-10,11-dihydro-10-hydroxy-5H-dibenz[b,f]azepine with peroxy compounds in alkali medium and in the presence of solvents.

Abstract: This disclosure provides a new class of compounds referred to as “reversed chloroquines” (RCQs), which are highly effective against CQR and CQS malaria parasites. RCQs are hybrid molecules, which include an antimalarial quinoline analog (such as chloroquine) moiety and a CQR reversal moiety. Exemplary RCQ chemical structures are provided. Also provided are pharmaceutical compositions including the disclosed RCQ compounds, and methods of using such compounds and compositions for the treatment of malaria and inhibition of CQR or CQS Plasmodium sp. (such as P. falciparum).

Abstract: A process for the preparation of 10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide (1) by ring opening of 11a,10b-dihydro-6H-dibenz/b,f/oxireno[d]azepine-6-carboxamide (5), characterised in that the ring opening is carried out under conditions of elevated pressure.

Abstract: The present invention provides compounds of the general formulas: wherein Y is NR or —(CH2)n; R is H or alkyl; “Z” represents optionally substituted phenyl or a 6-membered aromatic ring having one nitrogen atom; “W” represents a optionally substituted phenyl or 5-membered aromatic ring having one nitrogen atom; “X” represents an optionally substituted 5-membered aromatic ring having one sulfur atom; as well as methods and pharmaceutical compositions utilizing these compounds for the inducing temporary delay of urination or treatment of disorders remedied by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, or bleeding and coagulation disorders.

Abstract: A production method of 6-aminomethyl-6,11-dihydro-5H-dibenz[b,e]azepin characterized in that said compound is produced via N-[(6,11-dihydro-5H-dibenz[b,e]azepin-6-yl)methyl]-o-hydroxymethylbenzamide which is prepared by reducing 2-(11H-dibenz[b,e]azepin-6-ylmethyl)-1H-isoindole-1,3(2H)-dione employing a metal hydride or a metal hydride complex in a water based alcohol, and N-[(6,11-dihydro-5H-dibenz[b,e]azepin-6-yl)methyl]-o-hydroxymethylbenzamide which is useful for the aforesaid production method.

Abstract: The present invention provides substituted 11-phenyl-dibenzazepine compounds which are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.

Abstract: An organic electroluminescence element comprising: an anode layer, a cathode layer, and an organic luminescence layer therebetween, the organic luminescence layer having a carbazole derivative with a glass-transition temperature of 110° C. or higher, and a phosphorescent dopant. This structure makes it possible to provide an organic electroluminescence element which can make use of the triplet exciton state of the carbazole derivative even at room temperature and which has a practical life and superior heat-resistance.