摘要:
The present invention provides a novel compound having an excellent AMPA receptor inhibitory action and/or kainate inhibitory action. A compound represented by the following formula, a salt thereof or hydrates thereof. In the formula, Q indicates NH, O or S; and R1, R2, R3, R4 and R5 are the same as or different from each other and each indicates hydrogen atom, a halogen atom, a C1-6 alkyl group or a group represented by the formula —X-A (wherein X indicates a single bond, an optionally substituted C1-6 alkylene group etc.; and A indicates an optionally substituted C6-14 aromatic hydrocarbocyclic group or 5- to 14-membered aromatic heterocyclic group etc.).
摘要:
An amorphous object of (3E)-1-[l(s)-1-(4-fluorophenyl)ethyl]-3-[3-methoxy-4-(4methyl-1H-imidazol-1-yl)benzylidene]piperidine-2-one, which is represented by the formula (1) and has Aβ-production inhibitory activity. The amorphous object has such satisfactory properties that it has excellent solubility, is stable, does not readily become a crystalline form, and has low hygroscopicity. It is hence suitable for use in pharmaceutical preparations.
摘要:
Disclosed is a compound represented by the formula (I) below or a pharmacologically acceptable salt thereof. Also disclosed is a use of the compound or salt as a pharmaceutical product. (In the formula, Ar1 represents an imidazolyl group which may be substituted with a C1-6 alkyl group; Ar2 represents a phenyl group which may be substituted with a C1-6 alkoxy group; X1 represents a single bond; R1 and R2 respectively represent a C1-6 alkyl group or the like which may be substituted with a substituent such as a 5- to 14-membered aromatic heterocyclic group; and R3 represents a hydrogen atom or the like.)
摘要翻译:公开了由下式(I)表示的化合物或其药理学上可接受的盐。 还公开了化合物或盐作为药物产品的用途。 (式中,Ar 1表示可被C 1-6烷基取代的咪唑基,Ar 2表示可被C 1-6烷氧基取代的苯基,X 1表示单键; R 1,R 2分别表示 可以被诸如5至14元芳族杂环基团的取代基取代的C 1-6烷基等; R 3表示氢原子等。
摘要:
A system for comparing dental X-ray images includes a positional displacement calculator calculating a positional displacement between dental X-ray test and reference images by using phase-only correlation, a positional displacement corrector correcting the positional displacement, a base point extractor defining, as a base image, any one of the dental X-ray test and reference images, and defining, as a corresponding image, the other one of the two dental images, and extracting base points from the base image, a corresponding point extractor extracting corresponding points, which correspond to the base points, from the corresponding image, a correspondence calculator calculating correspondence between the base points and the corresponding points, a nonlinear distortion corrector correcting a nonlinear distortion between the base image and the corresponding image, based on the correspondence, and a similarity calculator finding, by using phase-only correlation, a similarity between the base image and the corresponding image.
摘要:
The invention provides crystals of dihydrochloride monohydrate of the compound of the following formula having an Aβ production inhibiting effect which crystals are characterized by exhibiting a diffraction peak at an angle of diffraction (2θ±0.2°) of 10.9° in powder X-ray diffractometry. Further, the invention also provides the compound in the form of various salts, crystal forms and amorphous forms which are suitable for the development of drugs.
摘要:
An ophthalmic laser treatment apparatus comprises: a laser source that emits a laser beam for treatment of an affected part of a patient's eye; an optical fiber that transmits the laser beam emitted from the laser source; and a delivery optical system that irradiates the laser beam emitted from the optical fiber to the affected part of the patient's eye, the delivery optical system including: a plurality of diffraction optical elements each being configured to shape a beam profile of the laser beam at an emission end face of the optical fiber into a beam profile having one of a uniform intensity and a lower intensity in the center than on the periphery on the affected part and also to shape the laser beam to have a different spot size on the affected part of the patient's eye; and a changing unit which selectively disposing one of the diffraction optical elements on an optical path.
摘要:
A fishing lure includes a lure body which is formed in an appearance imitating a small fish. A lower jaw which is vertically pivotable is provided on the front end of the lure body, and the pivot angle of the lower jaw is adjustable. The lower jaw is pivotally supported by the lure body at the base, and has an angle adjusting mechanism to control the pivot angle of the lower jaw around the pivot.
摘要:
The present invention relates to a novel two cyclic cinnamide compound and a pharmaceutical agent comprising the compound as an active ingredient. The two cyclic cinnamide compound represented by the general formula (I): wherein represents a single bond or a double bond; Ar1 represents a phenyl group or pyridinyl group that may be substituted with 1 to 3 substituents; R1 and R2 each represent a C1-6 alkyl group, a hydroxyl group, or the like; Z1 represents a methylene group or vinylene group, which may be substituted with 1 or 2 substituents selected from Substituent Group A1, an oxygen atom, or an imino group that may be substituted with a substituent selected from Substituent Group A1; and p, q, and r each represent an integer of 0 to 2, which has an effect of reducing Aβ40 and Aβ42 production, and thus is particularly useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ such as Alzheimer's disease or Down's syndrome.
摘要翻译:本发明涉及一种新型的两种环状肉桂酰胺化合物和包含该化合物作为活性成分的药剂。 由通式(I)表示的两种环状肉桂酰胺化合物:其中表示单键或双键; Ar 1代表可被1至3个取代基取代的苯基或吡啶基; R 1和R 2各自表示C 1-6烷基,羟基等; Z 1表示亚甲基或亚乙烯基,其可以被1或2个选自取代基组A1,氧原子或亚氨基的取代基取代,所述取代基可以被选自取代基 A1组; 并且p,q和r各自表示0〜2的整数,其具有降低Abeta40和Abeta42产生的作用,因此特别可用作由Abeta如阿尔茨海默病或阿尔茨海默病引起的神经变性疾病的预防或治疗剂 唐氏综合症。
摘要:
The present invention relates to a compound represented by the formula (I): or a pharmacologically acceptable salt thereof, wherein R1, R2, R3, and R4 are the same or different and each represent a hydrogen atom or a C1-6 alkyl group; X1 represents a C1-6 alkylene group that may be substituted; Xa represents a methoxy group or a fluorine atom; Xb represents an oxygen atom or a methylene group, provided that Xb is only an oxygen atom when Xa is a methoxy group; and Ar1 represents an aryl group, pyridinyl group, aryloxy group, or pyridinyloxy group that may have a substituent such as a halogen atom; and to use of the compound or salt as a pharmaceutical agent.
摘要翻译:本发明涉及由式(I)表示的化合物或其药理学上可接受的盐,其中R 1,R 2,R 3, SUP>和R 4相同或不同,各自表示氢原子或C 1-6烷基; X 1表示可以被取代的C 1-6亚烷基; X a a表示甲氧基或氟原子; X B表示氧原子或亚甲基,条件是当X a a为甲氧基时,X B b仅为氧原子; 和Ar 1表示可以具有卤素原子等取代基的芳基,吡啶基,芳氧基或吡啶氧基; 并使用化合物或盐作为药剂。
摘要:
A method for coating a porous polyurethane resin substrate with an aromatic isocyanate coating composition is provided comprising the steps of (i) providing a porous substrate of a polyurethane foam resin comprising at least one surface upon which the aromatic isocyanate coating composition is to be applied; (ii) applying at least one coating of a primary layer to the substrate surface, the primary layer comprising an aqueous solution of a compound that includes at least one —OH reactive group in its non-aqueous, dry state, and capable, upon drying, of forming a self-supporting, continuous film on the substrate surface at room temperature; (iii) optionally subjecting the applied primary layer to forced drying conditions at a temperature below the softening point of the porous polyurethane resin substrate; and (iv) after allowing the primary layer to substantially dry, applying a secondary layer comprising an aromatic isocyanate compound to the primary layer to form a continuous, film-forming coating on the substrate surface, preferably one having the property of being water-impermeable or water-impermeable and water vapor-permeable.