摘要:
According to the present invention, there are provided novel carboxystyrene derivatives of the general formula (I): wherein the symbols are as defined hereinabove. Also provided herein are leukotriene antagonists and phospholipase inhibitors containing the carboxystyrene derivative or pharmaceutically acceptable salt thereof as an effective ingredient.
摘要:
Disclosed are an aminostyryl compound represented by Formula I: ##STR1## wherein A represents a linking group having 3 to 4 chain members; B represents an unsubstituted or substituted 5 to 6-membered monocyclic type heterocyclic residue containing 1 to 2 hetero atoms, an unsubstituted or substituted condensed heterocyclic residue which contains 5 to 6-membered monocyclic type heterocycle containing 1 to 2 hetero atoms, a naphthyl group or an alkyl group having 5 to 7 carbon atoms,a composition having leukotriene antagonism which contains an aminostyryl compound represented by Formula I as the effective ingredient, and a method of antagonizing SRS based on leukotriene antagonistic activity by employing the same.
摘要:
4-Imidazoline derivatives represented by the formula (I) and/or formula (II): ##STR1## wherein R.sup.1 represents C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 alkynyl, C.sub.3 -C.sub.8 cycloalkyl, or optionally substituted aralkyl; R.sup.2 and R.sup.3 independently represent hydrogen, C.sub.3 -C.sub.20 alkyl, C.sub.3 -C.sub.20 alkenyl, C.sub.3 -C.sub.20 alkynyl, C.sub.3 -C.sub.20 alkoxy, C.sub.3 -C.sub.20 alkenyloxy, C.sub.3 -C.sub.20 alkynyloxy, C.sub.3 -C.sub.8 cyloalkyl, C.sub.1 -C.sub.10 alkylthio, or optionally substituted aralkyl or aralkyloxy; R.sup.4 represents C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, or optionally substituted aralkyl; provided that R.sup.2 and R.sup.3 cannot be hydrogen at the same time, and pharmaceutically acceptable salts thereof. A pharmaceutical formulation containing the compound is also provided.
摘要:
Disclosed is a pharmaceutical composition having circulation ameliorating effect and antiulcer effect containing a prostaglandin I.sub.2 analogue represented by the formula shown below or a non-toxic salt or a cyclodextrin inclusion compound thereof as the effective ingredient: ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group having 1 to 12 carbon atoms, a cycloalkyl group having 4 to 7 carbon atoms or a phenyl group, A represents a pentyl group, a cyclopentyl group, a cyclohexyl group, a 1-methyl-3-hexynyl group, a 2-methyl-3-hexynyl group, a 1-methylhexyl group, a 2-phenethyl group, a 1,1-dimethylpentyl group, a 2-methylpentyl group, a 1-cyclohexylethyl group, a 2-methylhexyl group, a 1-methyl-3-pentynyl group or a 2,6-dimethyl-5-heptenyl group; the double bond between the carbon atoms at 4- and 5-positions is E or Z or a mixture thereof; the asymmetric center in the substituent represented by A is in the R-configuration or the S-configuration or a mixture thereof.Pharmaceutical compositions containing, as an active ingredient, prostaglandin I.sub.2 analogues of the present invention have potent platelet aggregation inhibiting effect, blood pressure depressing effect, vasodilative effect and antiulcer effect, and are also low in toxicity.
摘要:
Disclosed is a pharmaceutical having circulation ameliorating effect and antiulcer effect containing a prostaglandin I.sub.2 analogue represented by the formula shown below or a non-toxic salt of its salt or a cyclodextrin inclusion compound thereof as the effective ingredient: ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group having 1 to 12 carbon atoms, a cycloalkyl group having 4 to 7 carbon atoms or a phenyl group; A represents a pentyl group, a cyclopentyl group, a cyclohexyl group, a 1-methyl-3-hexynyl group, a 2-methyl-3-hexynyl group, a 1-methylhexyl group, a 2-phenethyl group, a 1,1-dimethylpentyl group, a 2-methylpentyl group, a 1-cyclohexylethyl group, a 2-methylhexyl group, a 1-methyl-3-pentynyl group or 1 2,6-dimethyl-5-heptenyl group; the double bond between the carbon atoms at 4- and 5-positions is E or Z or a mixture thereof, the asymmetric center in the substituent represented by A is R-configuration or S-configuration or a mixture thereof.The pharmaceuticals containing, as an active ingredient, prostaglandin I.sub.2 analogues of the present invention have potent platelet aggregation inhibiting effect, blood pressure depressing effect, vasodilative effect and antiulcer effect, and are also low in toxicity.
摘要:
There are disclosed a (2-chloro-3-oxo-1-alkenyl)-bicyclo[3.3.0 octene derivative represented by the formula: ##STR1## wherein R.sup.1 represents --CH.sub.2 CH.sub.2 CH.sub.2 COOR.sup.5, --CH.sub.2 CH.sub.2 --O--CH.sub.2 COOR.sup.5, --CH.dbd.CHCH.sub.2 COOR.sup.5 or --CH.sub.2 CH.sub.2 C.tbd.C--COOR.sup.5 group where R.sup.5 in the groups represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; R.sup.2 represents a hydrogen atom, an acyl group having 1 to 7 carbon atoms, a tri(1 to 7 carbon atoms)-hydrocarbylsilyl group or a group forming an acetal bonding with an oxygen atom of a hydroxy group; R.sup.3 represents a straight or branched alkyl group having 3 to 10 carbon atoms, a cycloalkyl group having 4 to 7 carbon atoms, which may be substituted by at least one alkyl group having 1 to 4 carbon atoms, a straight or branched alkenyl group having 3 to 12 carbom atoms, a straight or branched alkynyl group having 3 to 8 carbon atoms, a phenyl group or a phenoxy group which may have substituents, an alkoxy group having 1 to 6 carbon atoms or an alkyl group substituted by a cycloalkyl group having 5 to 8 carbon atoms, and a process for preparing the same which comprises reacting an aldehyde represented by the formula: ##STR2## wherein R.sup.1 and R.sup.2 have the same meanings as defined above, with kotophosphonate represented by the formula: ##STR3## wherein R.sup.3 has the same meaning as defined above and R.sup.4 represents an alkyl group having 1 to 10 carbon atoms, in the presence of a base.
摘要:
An optical pickup apparatus comprising: a diffraction grating including a first grating for diffracting a first laser light beam, and a second grating for diffracting a second laser light beam which is shorter in wavelength than the first laser light beam, the diffraction grating being disposed in a common optical path for guiding the first laser light beam and the second laser light beam to an optical disc; and a photo detector including in a first light receiving area, a main light receiving unit, a front sub-light receiving unit, and a rear sub-light receiving unit that receive reflected light beams, which are reflected by the optical disc, of a main beam, of a front sub-beam, and of a rear sub-beam, respectively, the first laser light beam being diffracted by the diffraction grating into the main beam, the front sub-beam formed in front of the main beam, and the rear sub-beam formed at the back of the main beam, wherein the first grating is set such that the front sub-light receiving unit and the rear sub-light receiving unit in the first light receiving area are disposed at positions which substantially avoid unnecessary diffracted light beam spots which are generated by projecting to the first light receiving area unnecessary diffracted light beams, the unnecessary diffracted light beams generated by the second grating from the first laser light beam.
摘要:
Methods of using a compound, its pharmaceutically acceptable salts, and/or its pro-drug esters, in isolated form, to treat cancer, and methods for isolating, for formulating, and for administering the compound, salt, and/or pro-drug ester as an antitumor agent, wherein the compound, salt, or pro-drug ester has the following structure: wherein: R1, R2, R5, R7, and R8 are each separately selected from the group consisting of a hydrogen atom, a halogen atom, and saturated C1-C24 alkyl, unsaturated C1-C24 alkenyl, cycloalkyl, cycloalkenyl, alkoxy, cycloalkoxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, amino, substituted amino, nitro, substituted nitro, phenyl, and substituted phenyl groups, R3, R4, and R6 are each separately selected from the group consisting of a hydrogen atom, a halogen atom, and saturated C1-C12 alkyl, unsaturated C1-C12 alkenyl, cycloalkyl, alkoxy, cycloalkoxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, amino, substituted amino, nitro, and substituted nitro groups, X1 and X2 are separately selected from the group consisting of an oxygen atom, and a sulfur atom, and the dashed bond represents a bond selected from the group consisting of a carbon-carbon single bond and a carbon-carbon double bond. Most preferably, R3 and R4 are hydrogen, and each are involved in hydrogen bonds, and/or the dashed bond is a double bond, such that the chemical backbone of the compound substantially retains a substantially planar conformation.
摘要:
An optical head device including a lens holder which holds an objective lens, six wires for supporting the lens holder and a holder support member which movably supports the lens holder by the six wires in a tracking, focusing and tilt direction. The six wires comprise two pairs, each of the pairs comprising a composite wire composed of two wires and a single wire composed of one wire which are respectively disposed on an upper side and a lower side of the lens holder in the focusing direction. The spring constant of the composite wire is set to be approximately equal to a spring constant of the single wire. Alternatively, the six wires may be disposed on the same circumference with respect to a drive center in the tilt direction or the spring constant of one wire of the pair may be set to be smaller than spring constants of the other two wires of the pair.
摘要:
An optical pickup device includes a light source irradiating a record medium with plural light spots of light emitted therefrom, a plurality of light detecting elelments to which reflected light of the light spots are guided, respectively, to adequately synthesize and compare outputs of said light detecting elements, thereby reading information recorded in tracks of the record medium, and detecting an tracking error and a focusing error, and a hologram element which splits light emitted from the light source into plural beams is disposed in an optical path between the light source and the record medium, said hologram element is split by a split line, said split line elongating in a direction perpendicular to a track of the medium on an optical axis, and a hologram pattern having a diffraction function which is substantially directed in the track direction is disposed on at least one side of said split line, thereby differentiating diffraction conditions on both sides of said split line from each other.