Patentscope RSS feed

DDS COMPOUND AND PROCESS FOR THE PREPARATION THEREOF (Wed, 02 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.
>> Read More

PROCESS FOR PRODUCING 4' - (2 - CARBOXYETHYL)PHENYL TRANS - 4 - AMINOMETHYL-CYCLOHEXANECARBOXYLATE OR THE ACID-ADDITSALTS THEREOF AND INTERMEDIATES FOR PRODUCING THE SAME (Wed, 03 Dec 1980)

>> Read More

DDS COMPOUND AND PROCESS FOR THE PREPARATION THEREOF (Thu, 03 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.
>> Read More

DDS compound and process for the preparation thereof (Thu, 27 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.
>> Read More

NOVEL NITROXYL COMPOUNDS AND DRUGS AND REAGENTS CONTAINING THE SAME AS THE ACTIVE INGREDIENT (Wed, 26 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.
>> Read More

LABELED DRUGS AND NITROXYL COMPOUNDS TO BE USED THEREIN (Wed, 21 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.
>> Read More

Derivatives of Pyrazine Carboxylic Acids and their preparation (Wed, 17 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.
>> Read More

DRUGS AND REAGENTS CONTAINING N-ACYLOXYLATED CYCLOALKYL COMPOUNDS AS THE ACTIVE INGREDIENT (Wed, 12 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.
>> Read More

DDS compound and process for the preparation thereof (Wed, 15 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.
>> Read More

N-acyloxylated cycloalkyl compounds, composition containing the same and methods of use therefor (Tue, 30 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.
>> Read More

HYDROXYQUINOXALINECARBOXAMIDE DERIVATIVE (Thu, 01 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.
>> Read More

Pyrrolo [2,1-b]thiazole derivatives (Wed, 30 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.
>> Read More

AMINOPHENOL DERIVATIVES (Wed, 15 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.
>> Read More

FIVE-MEMBERED HETEROCYCLIC DERIVATIVE (Wed, 01 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.
>> Read More

HYDRAZONE DERIVATIVE (Wed, 04 Jan 2006)
A compound represented by the following formula (I): wherein R 1 represents hydrogen, aryl which may have a substituent, a saturated or unsaturated 5- to 7-membered heterocyclic group which may have a substituent, etc.; R 2 represents hydrogen, aryl which may have a substituent, a saturated or unsaturated 5- to 7-membered heterocyclic group which may have a substituent, etc.; R 3 represents hydrogen, etc.; Ar represents a divalent group derived from aromatic hydrocarbon, etc.; X represents a single bond, linear or branched alkylene having from 1 to 3 carbon atoms which may have a substituent, etc.; and G represents halogen, a saturated or unsaturated 5- or 6-membered cyclic hydrocarbon group which may have a substituent, a saturated or unsaturated 5- to 7-membered heterocyclic group which may have a substituent, etc ., a salt thereof or a solvate thereof; and an agent for inhibiting aggregation and/or deposition of an amyloid protein or an amyloid-like protein, which comprises the compound, a salt thereof or a solvate thereof
>> Read More

PYRAZOLE DERIVATIVES AND SALTS THEREOF (Wed, 30 May 2001)
This invention provides compounds having antitumor effect, namely a compound represented by the following formula (I) or (Ia) having various substituents in which G and G<1> are condensed tricyclic heterocyclic rings or salts thereof, and a compound represented by the following formula (Ib) having various substituents or salts thereof.
>> Read More

NOVEL SULFONYL DERIVATIVES (Wed, 06 Jun 2001)
Sulfonyl derivatives represented by the following general formula (I): Q<1>-Q<2>-T<1>-Q<3>-SO2-Q and drugs containing the same (wherein Q<1> is an optionally substituted, saturated or unsaturated, five- or six-membered cyclic hydrocarbon group, a five- or six-membered heterocyclic group, or the like; Q<2> is a single band, oxygen, sulfur, C1-C6 alkylene or the like; Q is optionally substituted arylalkenyl, heteroarylalkenyl or the like; and T<1> is carbonyl or the like). These compounds have potent FXa-inhibitory effects and promptly exert satisfactory and persistent antithrombotic effects through oral administration, thus being useful as anticoagulant agents little accompanied with side effects.
>> Read More

Aromatic amidine derivatives and salts thereof (Wed, 05 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.
>> Read More

AMIDOPYRAZOLE DERIVATIVE (Wed, 06 Sep 2006)
A platelet coagulation inhibitor which inhibits neither COX-1 nor COX-2 is provided. The inhibitor is a compound represented by general formula (I): wherein Ar 1 and Ar 2 independently represent a 5- or 6-membered aromatic heterocyclic group optionally substituted with 1 to 3 substituents, or a phenyl group optionally substituted with 1 to 3 substituents; R1 represents a lower acyl group, carboxyl group, a lower alkoxycarbonyl group, a lower alkoxy group, a lower alkyl group optionally substituted with 1 or 2 substituents, a carbamoyl group optionally substituted with 1 or 2 substituents, an oxamoyl group optionally substituted with 1 or 2 substituents, an amino group optionally substituted with 1 or 2 substituents, a 4- to 7-membered alicyclic heterocyclic group optionally substituted with 1 or 2 substituents, a phenyl group optionally substituted with 1 to 3 substituents, or a 5- or 6-membered aromatic heterocyclic group optionally substituted with 1 to 3 substituents; and R2 represents hydrogen atom, a halogeno group, or the like.
>> Read More

NOVEL ETHYLENEDIAMINE DERIVATIVES (Wed, 21 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.
>> Read More