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    ORAL DRUG CAPABLE OF RELEASE AT OBJECTIVE PLACE IN INTESTINE
    111.
    发明专利
    ORAL DRUG CAPABLE OF RELEASE AT OBJECTIVE PLACE IN INTESTINE 失效

    公开(公告)号：JPH0372417A

    公开(公告)日：1991-03-27

    申请号：JP11863590

    申请日：1990-05-10

    Applicant: CHUGAI PHARMACEUTICAL CO LTD

    Inventor： IKUSHIMA HEIJI

    IPC: A61K9/56 ,  A61K9/16 ,  A61K9/22 ,  A61K9/26 ,  A61K9/28 ,  A61K9/48 ,  A61K9/50 ,  A61K9/58

    Abstract: PURPOSE:To provide the subject oral drug composed of a core containing a specified main active component, etc., the first layer covering the core, the second layer covering the first layer and the third layer, capable of release at an objective place in the intestine without release the main active component till arrival at the desired place in the intestine and capable of controlling the speed of release. CONSTITUTION:An oral drug composed of (A) a core containing the main active component and a vehicle, (B) the first layer covering the core and consisting of an enteric component (e.g. hydroxypropyl methyl cellulose phthalate) or a water soluble component (e.g. acetyl cellulose) which may contain an insoluble component, (C) the second layer covering the first layer and consisting of a non-enteric component capable of dissolution by a reaction with one or more components in the core and (D) the third layer consisting of an enteric component and covering the second layer. In the intestine, the third layer is dissolved by the intestinal juice and the intestinal juice is infiltrated into the second layer without dissolution of thereof to arrive at the first layer. Thereby, the first layer begins to be dissolved and the solution is brought into contact with the core. The components in the core are diffused into the solution thereby and brought into contact with the second layer to start dissolution of the second layer, thus releasing the main active component.

    PROTECTING DRUG OF TUNICA MUCOSA NASI
    114.
    发明专利
    PROTECTING DRUG OF TUNICA MUCOSA NASI 失效

    公开(公告)号：JPH0347128A

    公开(公告)日：1991-02-28

    申请号：JP18149489

    申请日：1989-07-13

    Applicant: CHUGAI PHARMACEUTICAL CO LTD

    Inventor： UCHIDA YASUHIRO ,  KATO NOBUAKI ,  AZUMA SAYUMI ,  TAKEDA YASUHISA

    IPC: C08B5/14 ,  A61K31/715 ,  A61P27/16 ,  A61P37/08 ,  C08B37/02

    Abstract: PURPOSE:To obtain protecting drug of tunica mucosa nasi useful for prevention and curing of nasal allergy such as pollinosis having tunica mucosa nasi- protecting action without adverse effect containing alkali metallic salt of saccharides sulfate as active ingredient. CONSTITUTION:Alkali metallic salt of saccharides (e.g., maltose or dextran) sulfate is contained in the aimed protecting drug. Said alkali metallic salt is obtained by treating said saccharides with, e.g., pyridine-SO3 complex or chlorosulfonic acid in DMF according to normal method. Alkali metallic salt of sulfate of polysaccharide such as cellulose or dextran is especially preferable as said salt. Said protecting drug of tunica mucosa nasi is the most preferably made to formulation in liquid and sprayed to tunica mucosa nasi. To increase staying property on tunica mucosa nasi, making to formulation with using polymer material (e.g. hydroxypropyl methyl cellulose) having 300-2000cps (20 deg.C) is preferable.

    REMEDY FOR HYPERPARATHYROIDISM
    115.
    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

    Applicant: CHUGAI PHARMACEUTICAL CO LTD

    Inventor： NISHII YASUHO ,  TAKITA YUMIKO

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

    Abstract: 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.

    BSF2 ANTAGONIST
    119.
    发明专利
    BSF2 ANTAGONIST 失效

    公开(公告)号：JPH02188600A

    公开(公告)日：1990-07-24

    申请号：JP794489

    申请日：1989-01-17

    Applicant: CHUGAI PHARMACEUTICAL CO LTD

    Inventor： KOISHIHARA YASUO ,  MURAYAMA EIGOROU ,  FUKUI HIROYASU

    IPC: A61K38/00 ,  A61P9/00 ,  A61P29/00 ,  A61P35/00 ,  C07K7/08 ,  C07K14/52 ,  C07K14/54

    Abstract: NEW MATERIAL:A polypeptide in which plurality of amino acids are lost from N ends and/or C ends of human B cell stimulation factor 2 expressed by the formula, etc., and having antagonism action to the human B cell stimulation factor 2. USE:A remedy and diagnostic for artrial myxoma, carcinoma of uterine cervix, endotoxin, shock, myeloma, chronic rheumatism, etc. PREPARATION:For example, a method for successively bonding amino acids whose alpha-amino groups are protected according to normal Merrifield solid method by BOC method so as to synthesize a peptide chain is used and proceeding of coupling of the protected amino acid is carried out using Kaiser test while monitoring to provide the polypeptide in which plurality of amino acids are lost from N ends and/or C ends of human B cell stimulation factor 2.

    NOVEL 3,4-DIAMINOQUINOLINE AND PYRIDINE-BASED COMPOUND
    120.
    发明专利
    NOVEL 3,4-DIAMINOQUINOLINE AND PYRIDINE-BASED COMPOUND 失效

    公开(公告)号：JPH02167265A

    公开(公告)日：1990-06-27

    申请号：JP25312989

    申请日：1989-09-28

    Applicant: CHUGAI PHARMACEUTICAL CO LTD

    Inventor： MIURA YUTAKA ,  YOSHIDA MITSUTAKA ,  FUJIMURA YASUO ,  TAKAKU SAKAE ,  NODA YUKIFUMI

    IPC: C07D215/42 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/445 ,  A61K31/47 ,  A61K31/495 ,  A61K31/535 ,  A61P25/02 ,  A61P25/26 ,  A61P25/28 ,  C07D213/74

    Abstract: NEW MATERIAL:4-aminopyridine derivative expressed by formula I or acid- added salt of said derivative (R1 is H, hydroxyl group, lower alkoxy, morpholino or -NH-B, etc.; B is lower alkyl, cycloalkyl or phenyl; R2 and R3 are H, lower alkyl, lower alkylcarbonyl, or the two join and containing N to form azacycloalkyl or morpholino, etc.; R4 and R5 are H, or join to form quinoline ring or 5,6,7,8-tetrahydroquinoline ring together with ring A, with a proviso that for a case of R1, R4 and R5 are equally H, the case that R2 and R3 are equally H, or equally methyl, is excepted. For a case that R1 is H; R4 and R5 join to form quinoline ring together with the ring A, the case that R2 and R3 are equally H or ethyl, is excepted). USE:Useful as a remedy for Alzheimer-type dementia. PREPARATION:A compound expressed by formula II (RA and RB are H, etc.) is reacted with enamine corresponding to the aimed compound to afford the compound expressed by formula I.

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