Abstract: The present application provides solid forms of (R)-6-(2-fluorophenyl)-N-(3-(2-(2-methoxyethylamino)ethyl)phenyl)-5,6-dihydrobenzo[h]quinazolin-2-amine dihydrochloride, and methods of preparing and using same.

Abstract: This invention provides novel processes for the preparation of compounds such as 3-[(1S,2S)-2-hydroxycyclohexyl]-6-[(6-methylpyridin-3-yl)methyl]benzo[h]-quinazolin-4(3H)-one, salts and derivatives thereof. The compounds synthesized by the processes of the invention are useful for treating Alzheimer's disease and other diseases (e.g., cognitive impairment, schizophrenia, pain disorders, and sleep disorders) mediated by the muscarinic M1 receptor.

Abstract: The present application provides solid forms of (R)-6-(2-fluorophenyl)-N-(3-(2-(2-methoxyethylamino)ethyl)phenyl)-5,6-dihydrobenzo[h]quinazolin-2-amine dihydrochloride, and methods of preparing and using same.

Abstract: Provided are a new electron transport material and an organic electroluminescent device including the same. The electron transport material according to the present invention may have the excellent luminescence property and reduce the driving voltage to increase the power efficiency, such that the organic electroluminescent device using less consumption power may be manufactured.

Abstract: The present invention relates to a method for preparing nitrogen compounds using carbon dioxide, and to the use of the method in the production of vitamins, pharmaceutical products, adhesives, acrylic fibres, synthetic leathers, pesticides, herbicides, antifungal agents and fertilisers. The invention also relates to a method for producing vitamins, pharmaceutical products, adhesives, acrylic fibres, synthetic leathers, pesticides, herbicides, antifungal agents and fertilisers, which includes a step of preparing nitrogen compounds using the method of the invention. The invention further relates to a method for preparing labelled nitrogen compounds using carbon dioxide and to the uses thereof.

Abstract: A condensed cyclic compound represented by Formula 1 wherein in Formula 1, groups X1 to X8, L11, L12, R11, R12 and variables a11, a12, b11, b12 are described in the specification.

Abstract: The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.

Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against bacterial infections (e.g., biofilms).

Abstract: The present invention relates to novel pyrimidine derivatives and their use in perfume compositions. The novel pyrimidine derivatives of the present invention are represented by the following formula: wherein m and n are integers of 0 or 1, with the proviso that when m is 0, n is 1 and when m is 1, n is 0; and wherein the dashed circle represents either single or double bonds.

Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ.

Abstract: Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

Abstract: The present invention relates to novel pyrimidine derivatives and their use in perfume compositions. The novel pyrimidine derivatives of the present invention are represented by the following formula: wherein m and n are integers of 0 or 1, with the proviso that when m is 0, n is 1 and when m is 1, n is 0; and wherein the dashed circle represents either single or double bonds.

Abstract: A dye compound of formula 1: where R and R? are substituents independently selected from the group consisting of a hydrogen atom, C1 to C4 alkyl and a solubilizing moiety comprising a substituted or unsubstituted C10 to C70 hydrocarbyl group. At least one of R and R? is not a hydrogen atom or C1 to C4 alkyl. R? and R?? can be independently selected from the group consisting of a hydrogen atom, C1 to C6 alkyl groups or halogens; and X is a squaric acid moiety. A property of the dye compound is that it absorbs radiation having a wavelength in the range of about 700 nm to about 1400 nm.

Abstract: The present invention is directed to benzoquinazilinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

Abstract: The present invention is directed to pyranyl aryl methyl benzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

Abstract: A color-forming composition contains (A) a radical generator, (B) a compound represented by the following formula (1) and (C) a binder polymer: wherein, in the formula (1), R1 represents a group which reacts with a radical generated from the radical generator (A) to be released and forms a dye after the release, and T represents a nitrogen-containing hetero ring.

Abstract: A perimidine coupler of formula 1: where R and R? are substituents independently selected from the group consisting of a hydrogen atom, C1 to C4 alkyl or a solubilizing moiety comprising a substituted or unsubstituted C10 to C70 hydrocarbyl group. At least one of R and R? is not a hydrogen atom or C1 to C4 alkyl. R? and R?? can be independently selected from the group consisting of a hydrogen atom, C1 to C6 alkyl groups and halogens.

Abstract: The present invention is directed to benzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

Abstract: The present invention is directed to pyranyl aryl methyl benzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

Abstract: A method of producing 6-amino-cyclopenta[g]quinazolines, in enantiomerically enriched form, is provided. In particular, the method may be applicable to the synthesis of N—{N-{4-[N-((6S)-2 -hydroxymethyl-4-oxo-3,4,7,8-tetrahydro-6H-cyclo-penta[g]quinazolin-6-yl)-N-(prop-2 -ynyl)amino]benzoyl}-L-?-glutamyl}-D-glutamic acid (ONX-0801).

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

Abstract: Bridged bicyclic aryl or 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: Macrocyclic benzofused pyrimidine compounds, compositions comprising such compounds, methods for making the compounds, and methods of treating and preventing the progression of diseases, conditions and disorders using such compounds and compositions are described herein.

Abstract: The present invention relates to novel quinazoline compounds and their use in perfume compositions. The novel quinazoline compounds of the present invention are represented by the following formula: an isomer or a mixture of isomers thereof, wherein the broken line represents a single or double bond.

Abstract: A compound having the following formula (II) or a pharmacologically acceptable salt thereof is used as a P2X4 receptor antagonist: wherein each of R11 and R12 is hydrogen, C1-8 alkyl or the like; R13 is hydrogen, C1-8 alkyl or the like; R14 is C1-8 alkoxy, hydroxyl, cyano, a heterocyclic group optionally having a substituent or the like; and the condensed ring consisting of W1 and the neighboring benzene ring is naphthalene ring or the like.

Abstract: The present invention is directed to quinolinone-pyrazolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

Abstract: The present invention is directed to dihydrobenzoquinazilinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

Abstract: Provided are a new electron transport material and an organic electroluminescent device including the same. The electron transport material according to the present invention may have the excellent luminescence property and reduce the driving voltage to increase the power efficiency, such that the organic electroluminescent device using less consumption power may be manufactured.

Abstract: Disclosed are compounds of formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, U, W, X, R1, R2, R6, R7, R30 and R31 are as described above in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

Abstract: The present invention is directed to benzoquinazilinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

Abstract: A new method for the synthesis of L-Glutamyl-?-D-Glutamic acid and its use in the synthesis of (2R)-((4S)-carboxy-4-(4,N-(((6S)-2-(hydroxymethyl)-4-oxo-3,4,7,8-tetrahydro-3H-cyclopenta[g]quinazolin-6-yl)-N-(prop-2-ynyl)amino)benzamido)butanamido)pentanedioic acid, 1 are provided. Also provided is an efficient method for the isolation and purification of the trisodium salt of the abovementioned acid, 2, in a form suitable for long term storage and use in a parenteral dosing form.

Abstract: Novel 4-(3-butynyl)aminopyrimidine derivatives represented by general formula [I] are useful as pest control agents. In general formula [I], R1 is a mono- or bi-cyclic ring which may contain 0 to 3 heteroatoms, for example, phenyl or oxazolyl; R2 is a hydrogen atom, —R, —OR, —C(O)OR, —C(O)NHR, —CONR2 (wherein R is straight-chain or branched C1-8 alkyl, or the like), hydroxyalkyl, or the like; R3 is a hydrogen atom, a halogen atom, acyloxy represented by (straight-chain or branched C1-8 aliphatic hydrocarbon group) —CO—O—, or the like; and R4 is a hydrogen atom, a halogen atom, C1-6 alkyl, or the like, or alternatively, R4 and R3 together with the carbon atoms on the pyrimidine ring may form a thiophene ring, a pyrrole ring, an imidazole ring, a benzene ring, a pyrimidine ring, a furan ring, a pyrazine ring, or a pyrrolidine ring.

Abstract: The present invention relates to novel pyrimidine derivatives and their use in perfume compositions. The novel pyrimidine derivatives of the present invention are represented by the following formula: wherein m and n are integers that when m is 0, n is 1; when m is 1, n is 0 or 1; or when m is 2, n is 0; wherein (CH)m and (CH)n are each independently optionally substituted with a substituent selected from the group consisting of methyl and ethyl; wherein X is selected from the group consisting of N, O, and S; and wherein R1 and R2 each independently represent H or a hydrocarbon group, or R1 and R2 together represent a fused ring or a ring system, with the proviso that when R1 is H, R2 is not H.

Abstract: Compounds, compositions and methods are provided that comprise selective ?-glucuronidase inhibitors for both aerobic and anaerobic bacteria, especially enteric bacteria normally associated with the gastrointestinal tract. The compounds, compositions and methods can be for inhibiting bacterial ?-glucuronidases and for improving efficacy of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds by attenuating the side effects caused by reactivation by bacterial ?-glucuronidases of glucuronidated metabolites of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds.

Abstract: The present invention is directed to benzoquinazilinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

Abstract: Cyclopenta[g]quinazolines of the formula (I): wherein: A is a group OR or NR0R1 wherein R0 and R1 are each independently hydrogen C1-4 alkyl, C3-4 alkenyl, C3-4 alkynyl, C2-4 hydroxyalkyl, C2-4 halogenoalkyl or C1-4 cyanoalkyl, or R0 and R1 together with the intermediate N form a five- or six-membered heterocyclic ring; p is an integer in the range 1 to 4; R2 is hydrogen, C1-4 alkyl, C3-4 alkenyl, C3-4 alkynyl, C2-4 hydroxyalkyl, C2-4 halogenoalkyl or C1-4 cyanoalkyl; Ar1 is phenylene, thiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl which may optionally bear one or two substituents selected from halogeno, hydroxy, amino, nitro, cyano, trifluoromethyl, C1-4 alkyl and C1-4 alkoxy; and R3 is a group of one of the following formulae: -A1-Ar2-A2-Y1-A5-CON(R)CH(Y4) Y5-A8-X—Ar4 and pharmaceutically acceptable salts or esters thereof are of therapeutic value particularly in the treatment of cancer.

Abstract: Disclosed herein are novel antioxidant inflammation modulators, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds and compositions thereof are also provided.

Abstract: A method of producing 6-amino-cyclopenta[g]quinazolines, in enantiomerically enriched form, is provided. In particular, the method may be applicable to the synthesis of N-{N-{4-[N-((6S)-2-hydroxymethyl-4-oxo-3,4,7,8-tetrahydro-6H-cyclo-penta[g]quinazolin-6-yl)-N-(prop-2-ynyl)amino]benzoyl}-L-?-glutamyl}-D-glutamic acid (ONX-0801).

Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against bacterial infections.

Abstract: A compound having the following formula (II) or a pharmacologically acceptable salt thereof is used as a P2X4 receptor antagonist: wherein each of R11 and R12 is hydrogen, C1-8 alkyl or the like; R13 is hydrogen, C1-8 alkyl or the like; R14 is C1-8 alkoxy, hydroxyl, cyano, a heterocyclic group optionally having a substituent or the like; and the condensed ring consisting of W1 and the neighboring benzene ring is naphthalene ring or the like.

Abstract: The present invention is directed to dihydrobenzoquinazilinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

Abstract: Provided are rosuvastatin degradation products and their use as a reference standard (including reference marker) for analysis of rosuvastatin.

Abstract: The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.

Abstract: The present invention is directed to aminobenzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

Abstract: The present invention relates to substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

Abstract: A perimidine-based squarylium dye contains a compound represented by Formula (I), the compound containing an isomer A and satisfying the following formula: Pa?95(%) wherein the isomer A is an isomer of the peak shown in the longest retention time among all peaks due to isomers obtained by analysis of the compound by means of reversed-phase high-performance liquid chromatography, and Pa represents a value of the peak area of the isomer A relative to the peak area of all peaks

Abstract: Specific phenylalanine derivatives and analogues thereof have an antagonistic activity to ?4 integrin. They are used as therapeutic agents for various diseases concerning ?4 integrin.

Abstract: The present invention relates to novel pyrimidine derivatives and their use in perfume compositions. The novel pyrimidine derivatives of the present invention are represented by the following formula: wherein m and n are integers that when m is 0, n is 1; when m is 1, n is 0 or 1; or when m is 2, n is 0; wherein (CH)m and (CH)n are each independently optionally substituted with a substituent selected from the group consisting of methyl and ethyl; wherein X is selected from the group consisting of N, O, and S; and wherein R1 and R2 each independently represent H or a hydrocarbon group, or R1 and R2 together represent a fused ring or a ring system, with the proviso that when R1 is H, R2 is not H.

Abstract: The present invention is directed to aminobenzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

Abstract: Macrocyclic benzofused pyrimidine compounds, compositions comprising such compounds, methods for making the compounds, and methods of treating and preventing the progression of diseases, conditions and disorders using such compounds and compositions are described herein.