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DDS COMPOUND AND PROCESS FOR THE PREPARATION THEREOF (Thu, 03 Apr 2003)
A DDS compound in which amino group at 1-position of (1S,9S)-1-amino-9-ethyl-5-fluoro-2,3-dihydro-9-hydroxy-4-methyl-1H,12H -benzoÄdeÜpyranoÄ3',4':6,7Ü-indolizinoÄ1,2-bÜquinoline-10,13(9 H,15H)-dione as a drug compound is bound to a carboxyl group of a carboxymethyldextran polyalcohol with a spacer containing one amino acid or two to eight amino acids linked by peptide bond(s); characterized in that an introduced amount of residue of the drug compound is in a range of from 3.2% to 8.4% by weight; a weight-average molecular weight of the carboxymethyldextran polyalcohol is in a range of from 240,000 to 480,000; and degree of carboxymethylation is in a range of from 0.14 to 0.47; and a method for preparing said DDS compound, which comprises the steps of, for example, adding an aqueous solution containing sodium periodate to an aqueous solution containing dextran at a temperature of 4 DEG C +/- 2 DEG C to oxidize the dextran, and then adding the resulting reaction mixture to an aqueous solution containing sodium borohydride at a temperature not higher than 15 DEG C to obtain a dextran polyalcohol.
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PROCESS FOR PRODUCING 4' - (2 - CARBOXYETHYL)PHENYL TRANS - 4 - AMINOMETHYL-CYCLOHEXANECARBOXYLATE OR THE ACID-ADDITSALTS THEREOF AND INTERMEDIATES FOR PRODUCING THE SAME (Thu, 04 Dec 1980)

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DDS COMPOUND AND PROCESS FOR THE PREPARATION THEREOF (Fri, 04 Jan 2002)
A DDS compound which comprises (1S,9S)-1-amino-9-ethyl -5-fluoro-2,3-dihydro-9- hydroxy-4-methyl-1H,12H-benzo[de]- pyrano[3',4':6,7]indolizino[1,2-b]quinoline- 10,13(9H,15H)- dione as the drug compound and carboxymethyldextran polyalcohol and in which the 1-position amino group of the former is bonded to the carboxyl groups of the latter through a spacer consisting of either one amino acid or 2 to 8 amino acids bonded by peptide linkages, characterized in that the amount of the drug compound residue introduced is 3.2 to 8.4 wt% and that the carboxymethyldextran polyalcohol has an average molecular weight of 240,000 to 480,000 and a degree of carboxymethylation of 0.14 to 0.47. A process for the preparation of the DDS compound which comprises the step of adding an aqueous solution of sodium periodate to an aqueous solution of dextran at a temperature of 4.ordm.C .plusmn. 2.ordm.C to oxidize the dextran, and then adding the resulting reaction fluid to an aqueous solution of sodium borohydride at a temperature of 15.ordm.C or below to thereby obtain dextran polyalcohol.
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DDS compound and process for the preparation thereof (Fri, 28 Sep 2001)
A DDS compound which comprises (1S,9S)-1-amino-9-ethyl -5-fluoro-2,3-dihydro-9-hydroxy-4-methyl-1H,12H-benzo[de]- pyrano[3',4':6,7]indolizino[1,2-b]quinoline-10,13(9H,15H)- dione as the drug compound and carboxymethyldextran polyalcohol and in which the 1-position amino group of the former is bonded to the carboxyl groups of the latter through a spacer consisting of either one amino acid or 2 to 8 amino acids bonded by peptide linkages, characterized in that the amount of the drug compound residue introduced is 3.2 to 8.4 wt% and that the carboxymethyldextran polyalcohol has an average molecular weight of 240,000 to 480,000 and a degree of carboxymethylation of 0.14 to 0.47. A process for the preparation of the DDS compound which comprises the step of adding an aqueous solution of sodium periodate to an aqueous solution of dextran at a temperature of 4ºC ± 2ºC to oxidize the dextran, and then adding the resulting reaction fluid to an aqueous solution of sodium borohydride at a temperature of 15ºC or below to thereby obtain dextran polyalcohol.
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NOVEL NITROXYL COMPOUNDS AND DRUGS AND REAGENTS CONTAINING THE SAME AS THE ACTIVE INGREDIENT (Thu, 27 Apr 2000)
Nitroxyl compounds represented by general formula (I) which are usable in acquiring information about active oxygen or in vivo free radicals as biological images such as magnetic resonance images or magnetoencephalograms, wherein A represents hydrogen or -L-(CH2)n-OCOR (wherein L represents -COO- or -alkylene-COO-; and R represents C1-4 alkyl); R1, R2, R3, and R4 represent each C1-4 alkyl; and n is a number of from 1 to 4. Drugs and reagents containing the above compounds are usable in preventing, treating or diagnosing ischemic diseases, digestive diseases, cancer, cranial nervous diseases accompanied by nerve degeneration, inflammation, cataracts, or drug-induced organopathy.
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LABELED DRUGS AND NITROXYL COMPOUNDS TO BE USED THEREIN (Thu, 22 Feb 2001)
Drugs containing as the active ingredient compounds having a radioactive element and an organic substituent carrying an unpaired electron in a single molecule, for example, labeled nitroxyl compounds represented by general formula (I): wherein L represents -CO- or -alkylene-CO-, R, R1, R2, R3, and R4 represent C1-4 alkyl, R5 represents H, C1-4 alkyl, carboxyl, or lower alkoxycarbonyl, m and k are either 0 or 1, and n is from 1 to 4, R6 represents methyl or ethyl, R7 represents H, methyl, ethyl, or carboxyl, A represents an aromatic ring having a radioactive element, and @ represents either a single or a double bond when m is 0, or a single bond when m is 1. Use of these drugs makes it possible to easily obtain data about the spin labeling positions, thus providing a means for obtaining exact data relating to active oxygen or free radicals in vivo as biological images by nuclear magnetic resonance or biological magnetic measurement.
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Derivatives of Pyrazine Carboxylic Acids and their preparation (Thu, 18 Jun 1970)
1,195,639. Pyrazine derivatives. DAIICHI SEIYAKU CO. Ltd. 19 Sept., 1968 [20 Sept., 1967 (2)], No. 44627/68. Heading C2C. Novel compounds (I) in which X is C 1-5 alkoxy, piperidino, morpholino or oxazolidino and Y is H or C 1-5 alkoxy are prepared by reacting the appropriate Y-substituted pyrazine-2-carboxylic acid with a C 1-5 alkanol and where required reacting the resulting ester with piperidine, morpholine or oxazolidine. Intermediates isolated are 6-chloro-pyrazine-2- carboxylic acid, prepared by reacting pyrazine-2- carboxylic acid-4-oxide with phosphoryl chloride and 6-methoxy-pyrazine-2-carboxylic acid, prepared by reacting the former-named intermediate with sodium methoxide.
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DRUGS AND REAGENTS CONTAINING N-ACYLOXYLATED CYCLOALKYL COMPOUNDS AS THE ACTIVE INGREDIENT (Thu, 13 Sep 2001)
Drugs or reagents containing as the active ingredient N-acyloxylated cycloalkyl compounds represented by general formula (I): (wherein A is optionally substituted C4 or C5 cycloalkyl which may have one double bond in the ring; and R is C1 - C3 alkyl or phenyl). The above compounds are hydroxyamine derivatives functioning as spin trapping agents and can rapidly react with free radicals or active oxygen in an objective organ in spite of their being excellent in stability during the preparation or administration thereof.
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DDS compound and process for the preparation thereof (Thu, 16 Oct 2003)
A DDS compound which comprises (1S,9S)-1-amino-9-ethyl -5-fluoro-2,3-dihydro-9-hydroxy-4-methyl-1H,12H-benzo[de]- pyrano[3',4':6,7]indolizino[1,2-b]quinoline-10,13(9H,15H)- dione as the drug compound and carboxymethyldextran polyalcohol and in which the 1-position amino group of the former is bonded to the carboxyl groups of the latter through a spacer consisting of either one amino acid or 2 to 8 amino acids bonded by peptide linkages, characterized in that the amount of the drug compound residue introduced is 3.2 to 8.4 wt% and that the carboxymethyldextran polyalcohol has an average molecular weight of 240,000 to 480,000 and a degree of carboxymethylation of 0.14 to 0.47. A process for the preparation of the DDS compound which comprises the step of adding an aqueous solution of sodium periodate to an aqueous solution of dextran at a temperature of 4C +/- 2C to oxidize the dextran, and then adding the resulting reaction fluid to an aqueous solution of sodium borohydride at a temperature of 15C or below to thereby obtain dextran polyalcohol.
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N-acyloxylated cycloalkyl compounds, composition containing the same and methods of use therefor (Wed, 31 Mar 2004)
Drugs or reagents containing as the active ingredient N-acyloxylated cycloalkyl compounds represented by general formula (I):embedded image wherein A is optionally substituted C4or C5cycloalkyl which may have one double bond in the ring; and R is C1-C3alkyl or phenyl). The above compounds are hydroxyamine derivatives functioning as spin trapping agents and can rapidly react with free radicals or active oxygen in an objective organ in spite of their being excellent in stability during the preparation or administration thereof.
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HYDROXYQUINOXALINECARBOXAMIDE DERIVATIVE (Fri, 02 Oct 2009)
The present invention provides a novel hydroxyquinoxaline carboxamide derivative that is useful for preventing and/or treating blood coagulation disorders. A compound represented by formula (i), or a pharmacologically acceptable salt thereof: (see above formula) wherein, each of R1 and R2 independently represents a group such as a hydrogen atom or a halogen atom; R3 represents a group such as a hydrogen atom; each of R4 and R5 independently represents a group such as a hydrogen atom, a halogen atom or a C1-4 alkyl group; each of R6 and R7 independently represents a hydrogen atom or a C1-4 alkyl group; X represents a group such as a C3-10 cycloalkyl group, C6-10 aryl group or a 5- to 10-membered heterocyclic group, which may be substituted with substituent(s) selected from substituent group .alpha.; Y represents a group such as -CO-, -O- or -NRa-, and Ra represents a group such as a hydrogen atom or a C1-4 alkyl group.
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AMINOPHENOL DERIVATIVES (Thu, 16 Mar 2000)
Aminophenol derivatives represented by general formula (1), salts thereof or optical isomers thereof, and a gastrin receptor antagonist, a cholecystokinin receptor antagonist and a remedy for digestive tract diseases containing the same, wherein X represents O or S; A represents alkylene; R?1¿ represents phenyl, etc.; R?2¿ and R?3¿ represent each H or alkyl; R?4¿ represents substituted carbamoylalkyl, etc.; and R?5¿ represents substituted amino, etc. The compounds have a potent gastrin or CCK-A receptor antagonism and a high selectivity for one of the CCK-A and gastrin receptor and are useful as a preventive or remedy particularly for digestive tract diseases such as peptic ulcer or a remedy for central nervous diseases.
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Aromatic amidine derivatives and salts thereof (Thu, 06 May 1993)
An anticoagulant agent which comprises, as an active ingredient, an aromatic amidine derivative represented by the following general formula (1) or a salt thereof: wherein the group represented by is a group selected from indolyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, naphthyl, tetrahydronaphthyl and indanyl; X is a single bond, an oxygen atom, a sulfur atom or a carbonyl group; and Y is a saturated or unsaturated 5- or 6-membered heterocyclic moiety or cyclic hydrocarbon moiety optionally having a substituent group, an amino group optionally having a substituent group or an aminoalkyl group optionally having a substituent group. The inventive compound has a high anticoagulant capacity based on its excellent FXa inhibition activity.
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Heterocyclic triazin or triazolo compounds having serotonin 2-receptor antagonistic activity. (Thu, 13 Dec 1990)
A heterocyclic compound represented by formula (I): and salts thereof, and intermediates therefor are disclosed. The compound of formula (I) and salts thereof exhibit selective serotonin 2-receptor antagonistic activity and are useful for the prevention or treatment of circulatory diseases, e.g., ischemic heart diseases, cerebral vessel disturbances, and peripheral circulation disturbances.
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Pyrrolo [2,1-b]thiazole derivatives (Thu, 31 Jan 1991)
A novel compound represented by the following formula (I): wherein R1 represents a hydrogen atom, an alkyl group or a cyclic alkyl group; R2 represents a hydroxyl group, an alkoxy group which may have one to three substituents in the alkyl group moiety, an arylthio group which may have one or more substituents in the aryl group moiety, an aryloxy group which may have one or more substituents in the aryl group moiety, an amino group, an alkylamino group or a cyclic amino group which may contain other hetero atoms as ring atoms selected from a nitrogen atom, an oxygen atom and a sulfur atom; R3 represents a hydrogen atom, an alkyl group, an aryl group which may have one or more substituents, or a hetero aryl group which may have one or more substituents; and ----- represents a single bond or a double bond; salts thereof, and pharmaceutical preparations for preventing and treating hepatic diseases containing the compound of the formula (I) or salts thereof as an active ingredient are disclosed.
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PYRAZOLE DERIVATIVE (Thu, 17 May 2007)
A compound represented by Formula (I): wherein Ar 1 represents Formula (II): Ar 2 represents a 5- or 6-membered aromatic heterocyclic group which may be substituted; and X represents Formula (III): a salt thereof, or a solvate of the compound or the salt. A potent platelet aggregation suppressant which does not inhibit COX-1 and COX-2 is provided.
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FIVE-MEMBERED HETEROCYCLIC DERIVATIVE (Thu, 02 Feb 2006)
The present invention relates to a compound represented by formula (I): a salt of the compound, or a solvate of the compound or the salt; a drug containing any of the compounds, the salts, and the solvates; a preventive and/or therapeutic agent for an ischemic disease containing any of the compounds, the salts, and the solvates; and a platelet coagulation inhibitor containing any of the compounds, the salts, and the solvates. The compound of the present invention is useful as a strong platelet coagulation inhibitor without inhibiting COX-1 or COX-2.
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NOVEL ETHYLENEDIAMINE DERIVATIVES (Thu, 22 Sep 2005)
A compound represented by the following general formula (1): Q1-Q2-T0-N(R1)-Q3-N(R2)-T1-Q4 (1) wherein R1 and R2 represent each hydrogen, etc.; Q1 represents optionally substituted and saturated or unsaturated 5- to 6-membered cyclic hydrocarbyl, etc.; Q2 represents a single bond, etc.; Q3 represents a group -C(R3a)(R4a)-{C(R3b)(R4b)}m1-{C(R3c)(R4c)}m2-{C(R3d)(R4d)}m3-{C(R3e)(R4e)}m4-C(R3f)(R4f)- (wherein R3a to R4e represent each hydrogen, etc.); T0 represents carbonyl, etc.; and T1 represents -COCONR-, etc.; its salt, solvates thereof or N-oxides of the same. These compounds are useful as preventives and/or remedies for cerebral infarction, cerebral embolism, myocardial infarction, angina, pulmonary infarction, pulmonary embolism, Burger’s disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombosis after artificial valve/joint replacement, thrombosis and reocclusion after reconstructing blood circulation, systemic inflammatory response syndrome (SIRS), multiorgan dysfunction syndrome (MODS), thrombosis in extracorporeal circulation and blood coagulation in blood collection.
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PENTACYCLIC COMPOUNDS (Thu, 05 Mar 1998)
The present invention relates to a novel taxol derivative having an antitumor activity which is represented by formula (1). ÄIn the formula (I), R<1>: a phenyl group, R<2>: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group or an alkoxyl group, R<3>: a hydrogen atom, a hydroxyl group, a halogen atom, an alkoxyl group, a group -O-R<31>, an acyloxy group or a group -O-CO-R<31>, (in which R<31>: an alkylamino group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group), R<4> and R<5>: a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group, Z<1>: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z<2>: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z<3>: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic groupÜ
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PYRAZOLE DERIVATIVES (Thu, 27 Jul 2000)
A compound represented by formula (I) or a salt thereof; wherein R<1> and R<2>, which may be the same or different, each represent a hydrogen atom, a halogen atom, a hydroxy group, an alkoxy group, an amino group, an alkylamino group, an aryl group or an alkyl group; R<3> and R<4>, which may be the same, or different, each represent a hydrogen atom, a halogen atom, an alkoxy group, an amino group, an alkylamino group, an aryl group or an alkyl group; R<5> represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group or an arylalkyl group; Q represents an amidino group, a cycloalkyl group, a phenyl group or amonocyclic heterocyclic group except a pyrimidinyl group bonded to the N atom at its 2-position; G represents a nitrogen-containing saturated heterocyclic structure represented by formula: wherein X<1> represents a nitrogen atom or CH, in which the ring may have a keto group and may have one or more substituents; Z represents a phenyl or heterocyclic group which may have one or more substituents, in which two substituents on the phenyl or heterocyclic group may be connected to each other to form a ring to provide a condensed bicyclic structure as a whole; the substituent on Z and the substituent on G may be connected to each other to form a condensed tricyclic or tetracyclic structure as a whole, and an antitumor agent containing the compound or a salt thereof as an active ingredient.
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