Abstract: The present invention relates to novel quinazoline derivatives with less skin irritation and an excellent action of strongly suppressing scratching behavior, and pharmaceutical compositions containing a quinazoline derivative as an active ingredient. The present invention is directed to the quinazoline derivatives represented by the general formula [1] or pharmaceutically acceptable salts thereof. In the general formula [1], R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 and R4 are the same or different and represent hydrogen, alkyl, alkoxy or halogen; R5 is combined with R6 to represent alkylene or represents hydrogen, hydroxy, alkyl, phenyl or alkoxy; R6 represents alkyl, cycloalkyl, phenyl, a 5- to 10-membered aromatic heterocyclic group containing one to three heteroatoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, or —N(R6-1)(R6-2).

Abstract: The present invention provides, inter alia, compounds of Formula (I) and pharmaceutically acceptable salts thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as a method for the treatment of a disease or condition selected from the group consisting of central nervous system disorders, cognitive disorders, schizophrenia, dementia and other disorders in a mammal. The present invention further provides compounds of Formula (Id) and pharmaceutically acceptable salts thereof as CYP3A4 selective inhibitors.

Abstract: An object is to provide a novel organometallic complex capable of emitting phosphorescence, an organometallic complex which exhibits deep red emission, and a light-emitting element which provides deep red emission. Provided is an organometallic complex having a structure represented by the following General Formula (G1). In the formula, R1 R2, R3, R4, R5, R6, R7, R8, and R9 represent substituents, and M is a central metal and represents either a Group 9 element or a Group 10 element.

Abstract: An improved two stage reaction process for production of mono-L-aspartyl chlorin e6. In a first stage, the activation reaction between chlorin e6 and a carbodiimide produces a previously unknown anhydride in an activation reaction product (Formula I). This reaction product is purified to remove a significant proportion of the precursors of di-L-aspartyl chlorin e6. The purified activation reaction product contains a higher concentration of the previously unknown anhydride. This purified reaction product is used in a second stage: a coupling reaction of the purified activation reaction product with aspartate. The coupling reaction produces a coupling reaction product that has significantly reduced di-L-aspartyl chlorin e6 concentration. This reduced di-L-aspartyl chlorin e6 concentration facilitates purification of mono-L-aspartyl chlorin e6 from the coupling reaction mixture.

Abstract: Process for preparing compounds of the diaminophenothiazinium type of formula (II) below. The products have a high degree of purity and are useful for the preparation of medicaments. In which the R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 groups having the same definition as in formula (I), and R representing a group chosen from: a phenyl or benzyl group, optionally substituted with one or more functions chosen from: a C1-C4 alkyl, a halogen atom, a C1-C4 haloalkyl and a nitro group, a linear, branched or cyclic C1-C8 alkyl group, a C1-C8 alkylamino group, a C1-C8 alkoxy group, a phenyloxy or benzyloxy group optionally substituted on the aromatic nucleus with one or more functions chosen from: a C1-C4 alkyl, a halogen atom, a C1-C4 haloalkyl and a nitro group, Z representing an atom chosen from O and S.

Abstract: Dihydroquinazolines of the formula: The dihydroquinalzolines are useful as antiviral agents in particular against cytomegaloviruses.

Abstract: Disclosed herein are methods of inhibiting a deubiquitinase (DUB), methods of treating pathogenic infections (e.g.

Abstract: Nanoscale pigment particles of phthalocyanine pigments are prepared by providing a unsubstituted phthalocyanine chromogen material and a substituted phthalocyanine chromogen material, reacting the unsubstituted phthalocyanine chromogen material and the substituted phthalocyanine chromogen material to form a mixture of unsubstituted phthalocyanine dye molecules and substituted phthalocyanine dye molecules, and causing the substituted phthalocyanine dye molecules to non-covalently associate with the unsubstituted phthalocyanine dye molecules, so as to limit an extent of particle growth and aggregation and result in nanoscale pigment particles.

Abstract: The present invention provides pyrazine derivatives of formula I and pharmaceutically acceptable salts thereof, wherein the designation of R1, R2, R3 and R4 is provided herein. The invention also provides syntheses for preparation of such compounds. The invention further provides methods of use of these compounds and pharmaceutical compositions containing them for treatment and/or prevention of diseases and for manufacture of medicaments. These compounds and pharmaceutical compositions have antioxidative and thrombolytic effects, and thus can be used for the treatment and/or prevention of cerebral stroke caused by ischemia, and used for manufacture of medicaments for the treatment and/or prevention of nervous system diseases caused by excessive amount of radicals and/or thrombosis, infectious diseases, metabolic system diseases, cardiovascular and cerebrovascular diseases, and age-related degenerative diseases.

Abstract: Provided is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, which has an AMPA (?-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid) receptor potentiating action. The compound of the present invention is useful as a prophylactic or therapeutic drug for depression, schizophrenia, Alzheimer's disease or attention deficit hyperactivity disorder (ADHD) and the like.

Abstract: A core of a cyclic structure represented by (—N—(CH2)n—)k is bonded to a dendrimer-type side chain with a specific branched structure at all nitrogen atoms in the core to produce a compound with a specific structure for producing a metal complex that exhibits a T1-reducing effect, and the resulting compound is coordinated to a metal ion that has a T1-reducing effect to obtain a metal complex that exhibits an excellent T1-reducing effect which is useful as an effective component of an MRI contrast agent and an MRI contrast agent using the same.

Abstract: Process for preparing diaminophenothiazinium type compounds having a step for purification of derivatives (II). The diaminophenothiazinium type compounds having the following formula (I): in which R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 may be chosen, independently of the others, from the group constituted of: a hydrogen atom, saturated or unsaturated, linear or branched C1-C6 alkyl groups, or C3-C6 cycloalkyl groups, optionally substituted with one or more functions chosen from a halogen atom, and a C1-C6 alkoxy, C1-C6 alkoxycarbonyl or —CONH2 function, aryl groups optionally substituted with one or more functions chosen from: a C1-C4 alkyl, a halogen atom, and a C1-C6 alkoxy, C1-C6 alkyloxycarbonyl or —CONH2 function, in addition, each of R5, R6, R7, R8, R9 and R10 may be chosen, independently of the others, from the halogen atoms: F, Cl, Br and I, and X? represents an organic or inorganic anion.

Abstract: A method of preparing a compound of formula (I), A method for treating cancer or inhibiting growth of cancer cells including administering to a patient mammal in need thereof a pharmaceutical preparation including the compound. A method of treating or preventing a physiological disorder caused by abnormal protein tyrosine kinase activity in a mammal including administering to a mammal a pharmaceutical preparation including the compound.

Abstract: The present invention is directed to compounds of the formula: (wherein variables A1, A2, A3, G1, G2, G3, G4, J, Ea, Eb, Ec, R6, R7, and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

Abstract: The present invention relates to new CGRP-antagonists of general formula I wherein R1, R2, R3, Ra, Rb, Rc, X, Y and Z are defined as mentioned hereinafter, the individual diastereomers, the individual enantiomers and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing these compounds, the use thereof and processes for the preparation thereof.

Abstract: The present invention relates to three novel crystalline forms of Erlotinib hydrochloride and method of preparation thereof. Erlotinib hydrochloride is N-(3-ethynylphenyl)-6,7-bis(2 -methoxy ethoxy)-4-quinazolinamine hydrochloride of formula-(I): The present invention provides stable novel crystalline forms of Erlotinib hydrochloride designated as Form-M, Form-N and Form-P, and processes for the preparation of the same. Erlotinib hydrochloride can be used as medicament for the treatment of hyperproliferative disorders, such as cancers, in humans.

Abstract: Provided herein are compounds, such as compounds of Formula I, that bind to androgen receptors and/or modulate activity of androgen receptors. Also provided are methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.

Abstract: The invention is directed to compounds of Formula I in which: R5, R6, B and Z are defined supra.

Abstract: The present invention relates to compounds having formula: which are useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.

Abstract: The present invention relates to a novel chlorin e6-folic acid conjugate, a preparation method thereof, and a pharmaceutical composition for the treatment of cancer comprising the same, and more particularly, to a novel compound prepared by linking chlorin e6 to folic acid, which effectively produces singlet oxygen in various media and has much better tumor selectivity than the known porphyrin-based photosensitizers, thereby being used effectively in photodynamic therapy for malignant tumors, a preparation method thereof, and a pharmaceutical composition for photodynamic treatment of solid tumors comprising the compound as an active ingredient.