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332 条记录 (耗时 0.018 秒)

    22-OXACHOLECALCIFEROL DERIVATIVE AND ITS PRODUCTION
    32.
    发明专利
    22-OXACHOLECALCIFEROL DERIVATIVE AND ITS PRODUCTION 失效

    公开(公告)号：JPH0672994A

    公开(公告)日：1994-03-15

    申请号：JP35436292

    申请日：1992-11-27

    申请人： CHUGAI PHARMACEUTICAL CO LTD

    发明人： KATO MASAHIRO ,  MIKAMI TETSUHIRO ,  WATANABE HIROYOSHI ,  KUBODERA NOBORU ,  OCHI KIYOSHIGE

    IPC分类号： A61K31/59 ,  A61P3/02 ,  A61P5/12 ,  A61P29/00 ,  A61P35/00 ,  C07C401/00 ,  C07J7/00 ,  C07J51/00 ,  C07J71/00

    摘要： PURPOSE:To efficiently obtain the new derivative for antitumor agents, antilithium agents, etc., by reacting specific hydroxypregnenes with acrylamides and then successively subjecting the reactional product to treatment with an organic metal, introduction of double bond, irradiation of ultraviolet rays and thermal isomerization reaction. CONSTITUTION:A compound of formula I (R4 is H or (protected) hydroxyl group; R5 is (protected) hydroxyl group; R6 and R7 are H or together form double bond) is made to react with acrylic amides of formula II (R8 is 1-5C dialkylamino) in an organic solvent or a water-organic solvent system to afford a compound of formula III and the compound of formula III is made to react with an organometallic compound of the formula R9X (R9 is 1-5C alkyl; X is alkali metal, alkaline earth metal halide, etc.) to give a compound of formula IV (R2 and R3 are 1-5C alkyl). Then the compound of formula IV wherein R6 and R7 are H is subjected to halogenation at allyl position and dehydrohalogenation reaction to introduce a double bond thereto and then subjected to irradiation with ultraviolet rays in an organic solvent and successively subjected to thermal isomerization to provide the objective 22- oxacholecalciferol derivative expressed by formula V (R1 is H or OH).

    THYROID FUNCTION IMPROVER
    33.
    发明专利
    THYROID FUNCTION IMPROVER 失效

    公开(公告)号：JPH0616554A

    公开(公告)日：1994-01-25

    申请号：JP17395292

    申请日：1992-07-01

    申请人： ASAHI CHEMICAL IND

    发明人： KAWAKUBO HIROSHI ,  HASE TADASHI ,  ENDOU TOYOSHI

    IPC分类号： A61K31/435 ,  A61P5/12 ,  A61P43/00 ,  C07D491/048 ,  C07D495/04

    摘要： PURPOSE:To obtain a thyroid function improver for preventing and improving functional disorder of thyroid tissue and symptoms and sequela caused by the disorder, comprising a benzothienopyridine as an active ingredient. CONSTITUTION:The thyroid function improver comprises a compound of formula I of formula II (R1 is alkoxy, amino, hydrazino or N-containing heterocyclic group; R2 and R3 are halogen, alkyl, aryl, alkenyl, acyl, etc.; m and n are 0-4; etc.) such as benzo[b]thieno[2, 3-c]pyridine-3-carboxylic acid methyl ester as an active ingredient. In the case of pharmaceutical manufacturing of the compound into capsule, tablet, granule or powder form, 1-80wt.% of the compound is contained, in the case of to injection, 0.01-20wt.% of the compound is contained and in the case of into syrup and suspension is 0.01-20wt.% of the compound is contained. The improver is effective against thyroidism, Basedow's disease, Plummer's disease, cretin disease, insanity and intelectural disturbance caused by hypothyroidism, Paget's disease, osteoporosis, etc.

    34.
    发明专利
    失效

    公开(公告)号：JPH05271279A

    公开(公告)日：1993-10-19

    申请号：JP16971392

    申请日：1992-06-26

    IPC分类号： A61K38/22 ,  A61P3/00 ,  A61P5/12 ,  A61P19/10 ,  A61P43/00 ,  C07K14/00 ,  C07K14/575 ,  C07K14/635 ,  C12N1/21 ,  C12N15/00 ,  C12N15/09 ,  C12N15/16 ,  C12P21/02 ,  C12R1/19 ,  C07K7/10

    摘要： PURPOSE:To provide a new derivative of human parathyroid hormone (human PH) useful as pharmaceuticals. CONSTITUTION:An agonist derivative obtained by substituting the 8th and 18th methionine residues of human PTH with other amino acids, an agonist derivative obtained by substituting the 34th to 47th amino acids of human PTH with cysteine and an antagonist derivative devoid of 3 to 6 residues in an N- terminal amino acid sequence are prepared by a gene recombination technique. A human PTH derivative stable to oxidation can be produced by converting the methionine group with other fat-soluble amino acid residue, a PTH antagonist derivative can be produced by the deletion of the N-terminal amino acid and a human PTH derivative convertible to a more excellent compound can be obtained by converting the intermediate amino acid with cysteine, thereby forming a dimer or introducing other functional group.

    125 I-LABELED RADIOACTIVE SUBSTANCE OF (NLE8,NLE18,TYR34)-H-PTH(1-34)NH2
    35.
    发明专利
    125 I-LABELED RADIOACTIVE SUBSTANCE OF (NLE8,NLE18,TYR34)-H-PTH(1-34)NH2 失效

    公开(公告)号：JPH0592995A

    公开(公告)日：1993-04-16

    申请号：JP1384991

    申请日：1991-01-10

    申请人： ASAHI CHEMICAL IND

    发明人： MORITA KO ,  KUZUKI SHIGEO ,  NODA TOSHIHARU

    IPC分类号： A61K38/22 ,  A61P5/12 ,  C07K5/10 ,  C07K7/06 ,  C07K7/08 ,  C07K14/575 ,  G01N33/53 ,  G01N33/534

    摘要： PURPOSE:To obtain the subject radioactive labeled substance composed of a new human parathyroid hormone derivative and useful for the parathyroid function assay, etc., by labeling tyrosine residue at a specific position of a peptide having a specific amino acid sequence with plural 125I atoms. CONSTITUTION:A protected peptide is synthesized by converting the carboxyl group of a C-terminal tyrosine group to amide group and successively condensing amino acids according to the amino acid sequence of the peptide by liquid-phase synthesis after protecting the alpha-amino group and side-chain functional group. The protected peptide is treated with anhydrous hydrogen fluoride, etc. to eliminate the protecting groups and purified by gel-filtration, ion-exchange column chromatography and highperformance liquid chromatography to obtain the human parathyroid hormone (h-PTH) expressed by formula. The objective radioactive substance containing the peptide of formula wheremn the 34th Tyr is labeled with one or two 125I atoms is produced by incorporating and reacting the h-PTH with a phosphate buffer solution containing 125-Nal and chloramine T.

    PRODUCTION OF BACILLUS NATTO-CONTAINING FUNCTIONAL FOOD
    38.
    发明专利
    PRODUCTION OF BACILLUS NATTO-CONTAINING FUNCTIONAL FOOD 失效

    公开(公告)号：JPH03139261A

    公开(公告)日：1991-06-13

    申请号：JP27665389

    申请日：1989-10-24

    申请人： SHINOZAKI MASANORI

    发明人： SHINOZAKI MASANORI

    IPC分类号： A23L1/28 ,  A23L1/304 ,  A61K33/18 ,  A61P5/12

    摘要： PURPOSE:To produce a Bacillus natto-containing functional food, having overall health promoting function and excellent also in palatability by centrifuging, precipitating and collecting raw Bacillus natto and binding the resultant deodorized bacterial cells of the Bacillus natto to iodine. CONSTITUTION:Pure cultured bacterial cells of Bacillus natto are suspended in sterilized water to provided raw bacterial cells of the Bacillus natto, which are then treated with a centrifuge and precipitated to afford bacterial cells of the Bacillus natto. The resultant bacterial cells of the Bacillus natto are subsequently mixed with organic acids and saccharides consisting essentially of natural iodine or an iodine compound and a seasoning and a perfume, as desired, are added to the obtained mixture. The prepared mixture is solidified into an optional shape with gelatin or the aforementioned mixture is dried and then powdered or granulated. The seasoning and perfume, as desired, are added thereto. Alternately, an adequate amount of water is added to the above- mentioned bacterial cells of the Bacillus natto and the organic acids and saccharides consisting essentially of the natural iodine or iodine compound are subsequently mixed with the the obtained bacterial liquid of the Bacillus natto. The seasoning and perfume, as desired, are added thereto.

    REMEDY FOR HYPERPARATHYROIDISM
    40.
    发明专利
    REMEDY FOR HYPERPARATHYROIDISM 失效

    公开(公告)号：JPH0347127A

    公开(公告)日：1991-02-28

    申请号：JP8866990

    申请日：1990-04-03

    申请人： CHUGAI PHARMACEUTICAL CO LTD

    发明人： NISHII YASUHO ,  TAKITA YUMIKO

    IPC分类号： A61K31/59 ,  A61P5/12 ,  A61P5/20

    摘要： PURPOSE:To obtain the subject remedy useful as remedy for secondary hyperparathyroidism accompanying to renal failure, etc., having characteristics such as not inducing high hypocalcium disease even in continuous using containing 1alpha-hydroxyvitamin Ds as active ingredient. CONSTITUTION:1alpha-hydroxyvitamin Ds expressed by the formula [R is 4-6C branched alkyl substituted with 1 or 2 OH or (1-cyclopropyl-1'-hydroxy)methyl] is contained in the aimed remedy. The compound expressed by the formula has a characteristic exhibiting almost same-10 times of 1alpha,25-dihydroxyvitamin D3 in differentiation-inducing ability to myelocytic leukemia cell although having weak effect to hypocalcium value. The compound expressed by the formula is able to be administrated in a range of, e.g., 0.01-10mug/1 time in a case of parenteral administration (intravenous injection) or 0.01-10mug/day in a case of oral administration.