Abstract: A method of the administration of drugs with binding affinity for plasma protein and drugs regulating the effective ingredient dose of drugs with binding affinity for plasma protein; and a preparation whereby the effective ingredient dose of drugs with binding affinity for plasma protein is regulated. The above administration method is characterized in that, in the administration of a first drug having binding affinity for plasma protein, a second drug having binding affinity for the same plasma protein is administered simultaneously with the first drug or before or after the administration of the first drug to thereby regulate the binding of the first drug to the plasma protein.

Abstract: An agent which comprises, as an active ingredient, a radiolabeled compound as represented by the following formula or a pharmaceutically acceptable salt thereof: wherein R1 denotes hydrogen, or a linear- or branched-chain alkyl group having 1-8 carbon atoms, R2 denotes hydrogen, hydroxyl or a halogen substituent, R3 denotes hydrogen or fluorine substituent, R4 denotes oxygen, sulfur, or a methylene substituent, and R denotes a radioactive halogen substituent. The agent is stable in vivo, and either stays in cells or is incorporated in DNA, thus serving for diagnosis of tissue proliferation activity or treatment of proliferative disease.

Abstract: A diagnostic imaging agent useful for selection of a therapy for cancerous bone metastasis is provided, which comprises 99mTc(V)-dimercaptosuccinic acid as an effective ingredient. The agent is administered to a patient, and a scintigram is taken. This is especially useful for identifying osteoclastic type or mixed type bone metastasis or for identifying a disease in which the bone resorption due to osteoclast is enhanced, and thus allows a proper selection of therapies for such diseases.

Abstract: The present invention relates to a process for synthesizing an anhydroecgonine derivative without using cocaine as a starting material, and a process for synthesizing a phenyltropane derivative by using said anhydroecgonine derivative as an intermediate for the synthesis. The present invention provides a process for synthesizing an anhydroecgonine derivative which comprises reacting a cycloheptatriene derivative represented by the formula (1): with a primary amine, a salt thereof or ammonia in the presence of a base to obtain an anhydroecgonine derivative, and a process for synthesizing a phenyltropane derivative by using said anhydroecgonine derivative. In the formula (1), n is an integer of 0 or 1; and R1 is a cyano group in the case of n being 0, and R1 is selected from an alkyl group and an aralkyl group in the case of n being 1.

Abstract: An object of the present invention is to provide a bisphosphonic acid derivative and said bisphosphonic acid derivative being labeled with a radioactive nuclide, which has properties of rapid accumulation to the bone and rapid urinary excretion. The present invention relates to a bisphosphonic acid derivative and said bisphosphonic acid derivative being labeled with a radioactive nuclide, which is represented by the following general formula (1), R—Y—A  (1) wherein A is a bisphosphonic acid or a salt thereof, having P—C—P bond; Y is a bonding portion such as a methylene, an amido etc.

Abstract: The present invention relates to a process for synthesizing an anhydroecgonine derivative without using cocaine as a starting material, and a process for synthesizing a phenyltropane derivative by using said anhydroecgonine derivative as an intermediate for the synthesis. The present invention provides a process for synthesizing an anhydroecgonine derivative which comprises reacting a cycloheptatriene derivative represented by the formula (1): with a primary amine, a salt thereof or ammonia in the presence of a base to obtain an anhydroecgonine derivative, and a process for synthesizing a phenyltropane derivative by using said anhydroecgonine derivative. In the formula (1), n is an integer of 0 or 1; and R1 is a cyano group in the case of n being 0, and R1 is selected from an alkyl group and an aralkyl group in the case of n being 1.

Abstract: The present invention relates to a process for synthesizing an anhydroecgonine derivative without using cocaine as a starting material, and a process for synthesizing a phenyltropane derivative by using said anhydroecgonine derivative as an intermediate for the synthesis.

Abstract: An optically active tropinonemonocarboxylic acid ester derivative useful as an intermediate for synthesis of optically active tropane derivatives was obtained by reacting succindialdehyde with an organic amine and acetonedicarboxylic acid ester to obtain a tropinonedicarboxylic acid ester derivative, and then subjecting this derivative to enzyme-catalyzed asymmetric dealkoxy-carbonylation. Since anhydroecgonine methyl ester derived from the optically active tropinone-monocarboxylic acid ester derivative by reduction and dehydration had the same direction of optical rotation as in the case of anhydroecgonine methyl ester obtained from natural cocaine, it was proved that the obtained optically active tropinonemonocarboxylic acid ester derivative had the same absolute configuration as that of natural cocaine. The yield of the optically active tropinonemonocarboxylic acid ester derivative from the asymmetric dealkoxycarbonylation was 30 to 50 mol %, and its optical purity was 70 to 97% ee.

Abstract: An optically active tropinonemonocarboxylic acid ester derivative useful as an intermediate for synthesis of optically active tropane derivatives was obtained by reacting succindialdehyde with an organic amine and acetonedicarboxylic acid ester to obtain a tropinonedicarboxylic acid ester derivative, and then subjecting this derivative to enzyme-catalyzed asymmetric dealkoxy-carbonylation. Since anhydroecgonine methyl ester derived from the optically active tropinone-monocarboxylic acid ester derivative by reduction and dehydration had the same direction of optical rotation as in the case of anhydroecgonine methyl ester obtained from natural cocaine, it was proved that the obtained optically active tropinonemonocarboxylic acid ester derivative had the same absolute configuration as that of natural cocaine. The yield of the optically active tropinonemonocarboxylic acid ester derivative from the asymmetric dealkoxycarbonylation was 30 to 50 mol %, and its optical purity was 70 to 97% ee.

Abstract: A diagnostic imaging agent useful for selection of a therapy for cancerous bone metastasis is provided, which comprises 99mTc(V)-dimercaptosuccinic acid as an effective ingredient. The agent is administered to a patient, and a scintigram is taken. This is especially useful for identifying osteoclastic type or mixed type bone metastasis or for identifying a disease in which the bone resorption due to osteoclast is enhanced, and thus allows a proper selection of therapies for such diseases.

Abstract: The present invention relates to a method for synthesis of an optically active halopyridyl-azacyclo-pentane derivative and the intermediate thereof which comprises preparing an optically active allene-1,3-dicarboxylic acid ester derivative from an optically active acetonedicarboxylic acid ester derivative and then proceeding through a 7-azabicyclo[2.2.1]heptane derivative to obtain the objective product.

Abstract: The present invention provides a single radioactive transition metal nitride heterocomplex which permits labeling of a physiologically active substance such as a peptide, hormone or the like without impairing the activity of the substance. The radioactive transition metal nitride heterocomplex of the present invention is represented by the following formula (I): (M≡N)XY  (I) wherein a radioactive transition metal M is radioactive technetium or radioactive rhenium, N is a nitrogen atom, X is a diphosphine compound or a diarsine compound, and Y is a bindentate ligand having a combination of electron-donating atoms.

Abstract: The present invention provides a method for preparing [F-18]-fluoride ion which comprises the step of bringing [O-18]-enriched water containing [F-18]-fluoride ion formed by proton irradiation of [O-18]-enriched water into contact with a strongly acidic cation exchange resin to remove impurity cations, the step of then bringing the [O-18]-enriched water containing [F-18]-fluoride ion treated above into contact with a weakly basic anion exchange resin to make [F-18]-fluoride ion adsorbed to the resin and, along therewith, to recover the [O-18]-enriched water which has passed through the resin, and the step of eluting and collecting the [F-18]-fluoride ion adsorbed to the weakly basic anion exchange resin.

Abstract: A method for diagnosis or therapeutics of tumor which is characterized by administering an amount of a glycoprotein having a molecule capable of specifically binding to a lectin to a subject in need of such diagnosis or treatment and use of the glycoprotein for the manufacture of a diagnostic and therapeutic agent useful in detection or therapeutics of tumor are disclosed.

Abstract: A diagnostic agent for glycometabolic function comprising a glucose derivative of the formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and each represents hydrogen or acyl having 2 to 8 carbon atoms, with the proviso that at least one of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is acyl and R.sup.5 represents X or --NHCOR.sup.6 X wherein X is a radioisotope of halogen and R.sup.6 is arylene or alkylene having 1 to 3 carbon atoms.

Abstract: There is disclosed a diagnostic imaging agent which comprises a compound wherein at least one bifunctional ligand is chemically bonded to an amino group of amino oligosaccharide having the molecular weight of 500 to 2000 and having a reduction-treated reducing end of a sugar chain, or to an aldehyde group of a dialdehyde-oligosaccharide, at least one constituent monosaccharide of which is oxidation-cleaved, having the molecular weight of 500 to 2000 and having a reduction-treated reducing end of a sugar chain, and said ligand is coordinated with at least one metal ion selected from the group consisting of metal ions having the atomic number of 21-29, 31, 32, 37-39, 42-44, 49 and 56-83.

Abstract: A diagnostic agent for hypoxia or mitochondrial dysfunction is disclosed, comprising a radioactive copper complex of a dithiosemicarbazone derivative or a radioactive copper complex of a diamine diol schiff base derivative. This agent has good transferability to the target tissue, reduction reaction affinity at a hypoxic site, high stability in a non-target site and rapidly disappears.

Abstract: The present invention provides a shielding member for radioactive substances which can be made compact in size and light in weight while maintaining its shielding ability, or improves the shielding ability while keeping the same size, thereby to store a large volume of radioactivity. At the same time, the present invention provides a manufacturing method for the above shielding member and a radioactive solution-producing apparatus using the above shielding member. The radioactive substance-shielding member uses two or more kinds of radiation shielding materials of different shielding abilities. A shielding body made of a shielding material of the highest shielding ability is arranged at an area which is the nearest to a radioactive source.

Abstract: A peptide having affinity with tumor or a salt thereof, which comprises an amino acid sequence containing 20 or less amino acid residues, said amino acid sequence being described as X.sub.1 -YCAREPPT-X.sub.2 wherein A, C, E, P, R, T and Y represent amino acid residues expressed by standard one-letter symbols, each of amino acid residues A, C, R and Y in the amino acid sequence YCAR may be in either L-form or D-form, X.sub.1 represents a basic organic compound having 1-3 amino groups, and X.sub.2 represents any given amino acid sequence, is provided together with a radioactive diagnostic agent and a radioactive therapeutic agent containing the above peptide or a salt thereof. The present tumor affinity peptide is high in radioactive metal labeling yield, useful for imaging and treating pathological tissues such as of breast cancer, ovarian cancer and colon cancer of mammals including human, and difficult to be readily metabolized in organisms and to accumulate in normal tissues especially at kidney and liver.

Abstract: A peptide having affinity with inflammation is disclosed, which contains at least one of the following amino acid sequences:LLGGPS (SEQ ID NO:1),LLGGPSV (SEQ ID NO:2),KEYKAKVSNKALPAPIEKTISK (SEQ ID NO:3),KEYKCKVSNKALPAPIEKTISK (SEQ ID NO:4),KTKPREQQYNSTYR (SEQ ID NO:5), andKTKPREQQYNSTYRVV (SEQ ID NO:6),wherein A, C, E, G, I, K, L, N, P, Q, R, S, T, V, and Y represent amino acid residues expressed by standard one-letter symbols. According to the present invention, a peptide and its chemically modified substances, radioactive metal labeled peptides derived therefrom, and radioactive diagnostics comprising such peptide are provided, which are useful for imaging inflammation region and easy in preparation handling, and accumulate at inflammation site immediately after administration while being excellent in clearance into urine. The imaging is possible in several ten minutes after administration.