摘要:
There are provided novel 4-(2-furoyl)aminopiperidines represented by the general formula (I), their synthetic intermediates, processes for their preparation and medicaments containing them. In the above formula, X is CH or N, and Y is a group of the following general formula (II), formula (II-a) or formula (III): wherein a, b and c are each an integer of 0-6; Z is CH2 or NH; W is O or S; T is O or N—R15 wherein R15 is H, a C1-C6 alkyl group, a benzyl group or a phenethyl group; and R1 is H, a C1-C6 alkoxycarbonyl group, a benzyloxycarbonyl group, or the like. The 4-(2-furoyl)aminopiperidine derivatives according to this invention possess opioid μ antagonistic activity and are useful for the treatment or prevention of side effects which are caused by μ receptors agonist and which are selected from constipation, nausea/emesis or itch, or for the treatment or prevention of idiopathic constipation, postoperative ileus, paralytic ileus, irritable bowel syndrome or chronic pruritus.
摘要:
There are provided novel 4(2-furoyl)aminopiperidines represented by the general formula (I), their synthetic intermediates, processes for their preparation and medicaments containing them. In the above formula, X is OH or N, and Y is a group of the following general formula (II), formula (II-a) or formula (III): wherein a, b and c are each an integer of 0-6; Z is CH2 or NH; W is O or S; T is O or N—R15 wherein R15 is H, a C1-C6 alkyl group, a benzyl group or a phenethyl group; and R1 is H, a C1-C6 alkoxycarbonyl group, a benzyloxy-carbonyl group, or the like. The 4-(2-furoyl)aminopiperidine derivatives according to this invention possess opioid μ antagonistic activity and are useful for the treatment or prevention of side effects which are caused by μ receptors agonist and which are selected from constipation, nausea/emesis or itch, or for the treatment or prevention of idiopathic constipation, postoperative ileus, paralytic ileus, irritable bowel syndrome or chronic pruritus.
摘要:
There is disclosed a multidrug resistance inhibitor for overcoming a multidrug resistance of cancer, or an agent for enhancing the activity of anti-cancer agents, which comprises as an active ingredient a compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein n is an integer of 5 to 12,R.sub.1 and R.sub.2 are each independently benzyl, of which a phenyl ring may be substituted by 1 to 5 substituents selected from hydroxy, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy and halogen, and/or by methylenedioxy, with the proviso that R.sub.1 and R.sub.2 are simultaneously not a compound of formula (II) ##STR2##
摘要:
Isoprene derivatives of formula (I) ##STR1## wherein m is an integer of 0 to 3, n is an integer of 5 to 12, A is cyclo(C.sub.3 -C.sub.6)alkylene, phenylene, fluorenylene, pyrrolidinylene, piperazinylene, 9-aza-3-oxabicyclo�3.3.1!-nonylene, R.sub.1 and R.sub.2 are each independently benzyl, of which a phenyl ring may be substituted by 1 to 5 substituents selected from the group consisting of hydroxy, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy and halogen, X is a single bond or a divalent radical of --(CH.sub.2).sub.p NH--, p is an integer of 0 to 3, or a pharmaceutically acceptable salt thereof. Those compounds are useful as multidrug resistance inhibitors for overcoming multidrug resistance of cancer and agents for enhancing an activity of anti-cancer agents.
摘要:
A combustion device for a melting furnace, capable of heating a melting target object and the ceiling portion of the furnace with the radiant heat of the flame, including a combustion space above the location of the melting target object, including a fuel injection nozzle having a plurality of fuel injecting portions, which portions include orifices disposed side by side horizontally relative to the direction of fuel injection, and formed side by side vertically relative to the same. The orifices are formed radially side by side as seen laterally, with a direction along a middle angle in the angular range between the fuel injection direction of the uppermost fuel injection orifice and the fuel injection direction of the lowermost fuel injection orifice being directed obliquely upwards. The fuel injection orifices of the upper fuel injecting portion are formed radially side by side as seen in the plane view.
摘要:
The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen, lower acyl, lower alkoxycarbonyl or the like; R3 is lower alkyl, halo-lower alkyl, cycloalkyl, heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl or the like; R4 is cyano, lower alkoxycarbonyl, carboxy or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.
摘要翻译:本发明提供由通式(I)表示的化合物或其药学上可接受的盐,其中R 1和R 2各自为氢,低级酰基,低级烷氧基羰基等; R 3是低级烷基,卤素 - 低级烷基,环烷基,杂环烷基,任选取代的芳基,任选取代的杂芳基等; R4是氰基,低级烷氧基羰基,羧基等,其表现出强烈的COMT抑制活性。 本发明还提供含有所述化合物的药物组合物及其用途。
摘要:
An apparatus adapted to correct an image data acquired by an image detector including a plurality of detecting elements, includes: a first correction unit adapted for obtaining an offset-corrected image by removing an offset component due to the image detector from the image data, a second correction unit adapted for correcting a pixel value of the offset-corrected image on the basis of a gain of corresponding one of the plurality of detecting elements; and a third correction unit adapted for correcting a value of a selected pixel of the offset-corrected image, the selected pixel being selected based on the pixel value of the offset-corrected image, by generating a pixel value in place of a value of the selected pixel obtained by said second correction unit.
摘要:
A reception apparatus of the present invention is provided with a reception unit 301 for receiving a stream including a data signal, a display unit 305 for displaying based on the stream received by the reception unit 301, an authentication process unit 302 for authenticating a sender of the stream received by the reception unit 301, a signal separating unit 303 for separating the data signal from the stream received by the reception unit 301, and a control unit 310 for controlling so as to prohibit the screen unit 305 from displaying a screen based on the data signal separated by the signal separating unit 303 during authentication of the stream by the authentication process unit 302. Thereby, the reception apparatus appropriately plays contents without inflicting a disadvantage or stress on a user.
摘要:
A fine carbon fiber having an outer diameter of about 1 to about 80 nm and an aspect ratio of 10 to 30,000, comprising a hollow center portion and a multi-layer sheath structure of a plurality of carbon layers, the layers forming annual rings, wherein the sheath-forming carbon layers form an incomplete sheath, i.e., the carbon layers are partially broken or disrupted in a longitudinal direction, and the outer diameter of the carbon fiber and/or the diameter of the hollow center portion are not uniform in a longitudinal direction. The carbon fiber is obtained by instantaneously reacting a carrier gas at a high temperature and an organic compound gas kept at a temperature below the decomposition temperature of the transition metal compound and has a conductivity equivalent to that of a conventional vapor phase method and is useful as a filler material in resins, rubbers, paints and the like.