摘要:
Novel benzoxazine derivatives of the formula (I): ##STR1## are provided as well as their pharmaceutically acceptable salts and a method for their use as potassium channel activating agents 2-(3,4-Dihydro-2, 2-dimethyl-6-phenylsulfonyl-2H-1,4-benzoxazin-4-yl)pyridine N-oxide is illustrative of a benzoxazine derivative of formula (I). Also provided are intermediate compounds such as those of formula (II): ##STR2##
摘要:
Oxazinobenzazole derivatives represented by the formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, each independently represents a hydrogen atom or a lower alkyl group; R.sup.5 and R.sup.6 jointly form, in conjunction with the two adjacent carbon atoms, a substituted or unsubstituted 5- or 6-membered heterocyclic ring having at least two nitrogen atoms and optionally having one or more heteroatom(s) selected from the group consisting of an oxygen atom, a sulphur atom and a nitrogen atom; and m is an integer of 0 or 1, and pharmaceutically acceptable salts thereof. The compounds of the present invention are useful as antispasmodic medicaments.
摘要:
A tetrahydrobenzimidazole derivative represented by formula (I): ##STR1## wherein Het represents a heterocyclic group which may be substituted with 1 to 3 substituents selected from the group consisting of a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a cycloalkyl-lower alkyl group, an aralkyl group, a lower alkoxy group, a nitro group, a hydroxyl group, a lower alkoxycarbonyl group, and a halogen atom; and X represents a single bond or --NH-- which is bonded to the carbon atom or nitrogen atom of the heterocyclic ring, or a pharmaceutically acceptable salt thereof.The compound of formula (I) and a salt thereof exhibits antagonism against 5-HT.sub.3 receptor.
摘要:
4,5,6,7-Tetrahydrobenzimidazole derivatives represented by general formula (I) ##STR1## wherein groups represents the following: R.sup.1, R.sup.2, R.sup.3 : independently represent hydrogen atom, hydroxy group, a halogen atom, a lower alkyl group which may optionally be substituted with a halogen atom, a lower alkoxy group, a lower alkylthio group, an aralkyloxy group, an aryloxy group, a lower alkanoyl group, carboxy group, a lower alkoxycarbonyl group or nitro group;R.sup.4, R.sup.5, R.sup.6 : hydrogen atom or a lower alkyl group;X: oxygen atom or sulfur atom;or salts thereof which are believed to have a 5-HT.sub.3 antagonizing activity.
摘要:
A process is provided for preparing a tetrahydrobenzimidazole derivative represented by Formula (Ib): ##STR1## wherein Het representa s heterocyclic group which may be substituted with 1 to 3 substituents selected from the group consisting of a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a cycloalkyl-lower alkyl group, an aralkyl group, a lower alkoxycarbonyl group, and a halogen atom; and X.sup.2 represents a single bond connected to the carbon atom of the heterocyclic ring as represented by Het. The process comprises reacting a heterocyclic compound represented by Formula (IIIa):Het--X.sup.2 --H (IIIa)wherein Het and X.sup.2 are as defined above, with a carboxylic acid represented by Formula (II): ##STR2## or a reactive derivative thereof.
摘要:
A substituted-amidinobenzene derivative of the following general formula (I) or a salt thereof, and a pharmaceutical composition comprising said derivative or a salt thereof and a pharmaceutically acceptable carrier. ##STR1## (the symbols in the above formula have the following meanings: R.sup.1 : a group which can be converted into an amidino group in vivo;R.sup.2 and R.sup.3 : the same or different and each represents a carboxyl group or a group which can be converted into a carboxyl group in vivo;X.sup.1 and X.sup.2 : the same or different and each represents a lower alkylene group;m: 0, 1 or 2;n: 0 or 1, provided that n=1 when m=0.They have GPIIb/IIIa receptor antagonizing activity and are useful as medicines for ameliorating ischemic cardiac disorders, adminicula in cardiosurgery operations or in vascular surgery operations, medicines for ameliorating cerebrovascular disorders, And medicines for ameliorating peripheral artery disorders. In addition, they are useful as a prodrug excellent in peroral absorbability and sustainment of the effect.
摘要:
An amidinonaphthyl derivative represented by the following general formula (I) which has coagulation factor X inhibiting action and is useful as an anti-thrombus agent and the like, a salt thereof, an intermediate thereof and a pharmaceutical composition which comprises the amidinonaphthyl derivative. An amidinonaphthyl derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof. ##STR1## (symbols in the formula have the following meanings; R.sup.1 : a hydrogen atom or a group represented by the formula --A--W--R.sup.4,A: a group represented by the formula ##STR2## a group represented by the formula ##STR3## or a group represented by the formula --SO.sub.2 --, X: an oxygen atom or a sulfur atom, W: a single bond or a group represented by the formula --NR.sup.5 --, R.sup.4 : a hydroxyl group, a lower alkoxy group, etc., R.sup.5 : a hydrogen atom, a carbamoyl group, a lower alkoxycarbonyl group, etc., R.sup.2 : a lower alkyl group, R.sup.3 : a hydrogen atom, a halogen atom, a carboxyl group, B: a lower alkylene group or a carbonyl group, and n: 0 or 1).
摘要:
Disclosed are benzamidine derivatives of the following general formula (I), salts thereof, hydrates thereof or solvates thereof, and pharmaceutical compositions comprising the derivatives, salts thereof, hydrates thereof or solvates thereof along with pharmaceutically-acceptable carriers. ##STR1## The derivatives and their compositions have GPIIb/IIIa receptor antagonistic activity and are useful for the treatment and prophylaxis of vascular system disorders as medicines for ameliorating ischemic cardiac disorders, adminicula in cardiosurgery operations or in vascular surgery operations, medicines for ameliorating cerebrovascular disorders, and medicines for ameliorating peripheral artery disorders.
摘要:
An alignment jig including: a base jig which is used when aligning and bonding a nozzle plate which is provided with nozzle orifices ejecting liquid of a liquid-jet head with/to a fixing member holding a nozzle plate side of the plurality of liquid-jet heads, and which is provided with an optical system on a bottom plane thereof; a mask having transparency, one plane of which is bonded to a plane of the base jig opposite to the optical system, and the other plane of which is provided with a reference mark for being aligned with an alignment mark provided for the nozzle plate; and a spacer jig which is bonded to a plane of the mask where the reference mark of the mask is provided, and which holds the fixing member.
摘要:
An alignment apparatus, which is used when positioning and joining a plurality of workpieces relative to each other, each workpiece having a plurality of alignment marks for alignment, the alignment apparatus includes: a transparent mask provided with reference marks with which the alignment marks are aligned; a mirror disposed between the mask and the workpiece; an optical unit having an optical axis pointed in a direction of the mirror via the reference mark from a side of the mask opposite to the mirror, the optical unit enabling the reference mark and a virtual image of the reference mark reflected in the mirror to be observed simultaneously; andan adjusting unit for making optical axis adjustment of the optical axis, based on the observation by the optical unit, such that a real image of the reference mark and the virtual image of the reference mark reflected in the mirror are superposed.