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    CYCLIC COMPOUND AND ITS USE FOR MEDICINE
    2.
    发明专利
    CYCLIC COMPOUND AND ITS USE FOR MEDICINE 失效

    公开(公告)号：JP2000191588A

    公开(公告)日：2000-07-11

    申请号：JP20675198

    申请日：1998-07-22

    申请人： JAPAN TOBACCO INC

    发明人： SHINKAI HISASHI ,  KOSEKI HIDEKAZU ,  OTA TAKESHI

    IPC分类号： A61K31/19 ,  A61K31/195 ,  A61K31/215 ,  A61P3/08 ,  A61P3/10 ,  C07C59/205 ,  C07C59/21 ,  C07C59/80 ,  C07C69/716 ,  C07C69/738 ,  C07C233/63

    摘要： PROBLEM TO BE SOLVED: To obtain a new compound not causing a serious adverse effect such as hypoglycemia by administration, having an action only on a hyperglycemic state, useful as a therapeutic agent for diabetic and a preventive for a chronic complication of diabetic. SOLUTION: This compound is shown by formula I [A is a group of formula II or formula III (R2 is a halogen-substituted lower alkyl; R3 is a halogen or a lower alkyl; R4 is a lower alkyl) or the like; and R1 is H, a lower alkyl, an aryl, a cycloalkyl or an aralkyl] such as trans-4-[4-(fluoromethyl) cyclohexyl]-4-oxobutanoic acid. The compound of formula I is obtained, for example, by a method for partially hydrolyzing a compound of formula IV (R6 is a lower alkyl such as methyl, ethyl, propyl or butyl) as a starting substance, reacting the hydrolyzate with oxalyl chloride and reacting the reaction product with a fluorinating agent and hydrolyzing the reaction product to give a compound of formula V (X1 is a halogen such as F).

    NOVEL THIAZOLIDINEDIONE DERIVATIVE AND OXAZOLE DERIVATIVE
    3.
    发明专利
    NOVEL THIAZOLIDINEDIONE DERIVATIVE AND OXAZOLE DERIVATIVE 失效

    公开(公告)号：JPH0717974A

    公开(公告)日：1995-01-20

    申请号：JP16661693

    申请日：1993-07-06

    申请人： JAPAN TOBACCO INC

    发明人： SHINKAI HISASHI ,  SHIRAKAWA EIJI ,  ONOKI SHOJI ,  FURUKAWA NOBORU ,  UCHIDA ITSURO

    IPC分类号： A61K31/425 ,  A61P3/06 ,  A61P3/08 ,  A61P3/10 ,  C07D263/32 ,  C07D417/12 ,  C07D417/14

    摘要： PURPOSE:To provide the novel compound having excellent blood sugar and blood lipid level reducing activity, thus useful as a medicine for diabetes and complications thereof or related diseases such as hyperlipemia. CONSTITUTION:The compound of formula I (R is aromatic hydrocarbon, alicyclic hydrocarbon or heterocycle; R1 and R2 are each H or lower alkyl; R3 is H, OH or lower alkyl; R4 is lower alkyl; X is O, S or secondary amino; A is (CH2)m; m is 0-2; B is (CH2)n; n is 0-2), e.g. 5-{4-[2-[5-methyl-2-(4- methoxyphenylthio)methyl-4-oxazolyl]ethoxy]benzyl}-2,4-thiazolidinedione. The compound of the formula I can be obtained by reaction between a compound of formula II and a compound of formula III in the presence of a base (e.g. sodium hydride) in a solvent (e.g. benzene) under cooling to warming.

    6-(heterocycle-substituted benzyl)-4-oxoquinoline compound and use of the same as hiv integrase inhibitor
    4.
    发明专利
    6-(heterocycle-substituted benzyl)-4-oxoquinoline compound and use of the same as hiv integrase inhibitor 有权
    6-（杂环取代的苯甲基）-4-氧杂环丁烷化合物及其作为HIV整合酶抑制剂的用途

    公开(公告)号：JP2008110960A

    公开(公告)日：2008-05-15

    申请号：JP2007164676

    申请日：2007-06-22

    申请人： Japan Tobacco Inc ,  日本たばこ産業株式会社

    发明人： SATO MOTOHIDE ,  ARAMAKI HISAAKI ,  YAMASHITA MASAKI ,  INOUE AKIFUMI ,  KAWAKAMI HIROSHI ,  SHINKAI HISASHI ,  NAKAMURA HIROSHI ,  MATSUZAKI YUJI ,  WAMAKI SHUICHI

    IPC分类号： C07D215/56 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61P31/18 ,  A61P43/00 ,  C07D401/10 ,  C07D413/10 ,  C07D417/10 ,  C12N9/99 ,  C12N15/09

    CPC分类号： C07D215/56 ,  C07D401/10 ,  C07D413/10 ,  C07D417/10

    摘要： PROBLEM TO BE SOLVED: To provide a new 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof, or a solvate of the compound or the salt useful as an anti-HIV agent. SOLUTION: The invention relates to a compound represented by the general formula [I], a pharmaceutically acceptable salt thereof, or a solvate of the compound or the salt; and a pharmaceutical composition, an anti-HIV agent, and an HIV integrase inhibitor, each comprising the compound. The compound has an action of inhibiting the HIV integrase activity, and therefore is useful as an anti-HIV agent or a therapeutic or prophylactic agent for AIDS. By using in combination with other anti-HIV agent such as a protease inhibitor and a reverse transcriptase inhibitor, the compound can act as a more effective anti-HIV agent. Further, because of its high inhibitory activity specifically against an integrase, the compound can act as an agent which is safe for a human body and has few adverse side-effects. COPYRIGHT: (C)2008,JPO&INPIT

    摘要翻译： 要解决的问题：提供新的4-氧代喹啉化合物或其药学上可接受的盐，或者可用作抗HIV剂的化合物或盐的溶剂合物。 解决方案：本发明涉及由通式[I]表示的化合物，其药学上可接受的盐或化合物或其盐的溶剂合物; 以及各自包含该化合物的药物组合物，抗HIV剂和HIV整合酶抑制剂。 该化合物具有抑制HIV整合酶活性的作用，因此可用作抗HIV剂或用于AIDS的治疗或预防剂。 通过与其他抗HIV剂如蛋白酶抑制剂和逆转录酶抑制剂组合使用，该化合物可以作为更有效的抗HIV剂。 此外，由于其对整合酶具有高的抑制活性，所以该化合物可以作为对人体安全并且几乎没有不良副作用的药剂。 版权所有（C）2008，JPO＆INPIT

    COMPOUND HAVING IMMUNOPOTENTIATING ACTIVITY
    6.
    发明专利
    COMPOUND HAVING IMMUNOPOTENTIATING ACTIVITY 失效

    公开(公告)号：JP2000178248A

    公开(公告)日：2000-06-27

    申请号：JP35486398

    申请日：1998-12-14

    申请人： JAPAN TOBACCO INC

    发明人： HAGIWARA ATSUSHI ,  SHINKAI HISASHI ,  INAGAKI KOJI

    IPC分类号： C07D333/20 ,  A61K31/00 ,  A61K31/165 ,  A61K31/167 ,  A61K31/18 ,  A61K31/34 ,  A61K31/341 ,  A61K31/38 ,  A61K31/381 ,  A61P31/00 ,  A61P31/04 ,  A61P31/12 ,  A61P35/00 ,  A61P37/00 ,  A61P37/02 ,  A61P37/04 ,  C07C233/56 ,  C07C327/42 ,  C07D307/52 ,  C07D333/58

    摘要： PROBLEM TO BE SOLVED: To obtain the subject new compound having an excellent ability to enhance the production of IL-2 and T cell activating actions and useful especially as a therapeutic agent, etc., for infectious diseases caused by antiviral agents or microorganisms and capable of providing a pharmaceutical composition having immunopotentiation as a mode of action. SOLUTION: This compound is represented by formula I [R1 is phenyl, naphthyl, a 3-7C cycloalkyl or the like; R2 is a 1-4C alkyl, a 1-4C alkoxy, a halogen, trifluoromethyl or the like; R3 to R5 are each H or a 1-4C alkyl; X1 and X2 are each O atom or S atom, with the proviso that both are not simultaneously the O atom; (m) and (n) are each O or 1], e.g. 2-(3,5- bistrifluoromethylphenylamino)-N-(furan-2-ylmethyl)-2-thioxoacetamide. The compound represented by formula I is obtained by carrying out an acylating reaction of, e.g. a compound represented by formula II (Rc is a protecting group of a carboxylic acid; Hal is a halogen) with a compound represented by formula III, reacting the resultant compound with a Lawesson's reagent or diphosphorus pentasulfide and then reacting the prepared compound with a compound represented by formula IV in a solvent.

    LPL POTENTIATOR
    10.
    发明专利
    LPL POTENTIATOR 失效

    公开(公告)号：JP2001226358A

    公开(公告)日：2001-08-21

    申请号：JP2000304587

    申请日：2000-10-04

    申请人： JAPAN TOBACCO INC

    发明人： SHINKAI HISASHI ,  MOTOMURA TAKANAO ,  HAMAKAWA NORIAKI

    IPC分类号： A61K31/4184 ,  A61K31/423 ,  A61P3/06 ,  A61P9/10 ,  A61P43/00 ,  C07D235/18 ,  C07D263/56 ,  C07D263/57

    摘要： PROBLEM TO BE SOLVED: To provide a new compound having LPL potentiating action and a therapeutic agent for hyperlipemia or arteriosclerosis using the above compound. SOLUTION: This LPL potentiator contains, as an active ingredient, a compound represented by a general formula 1 [wherein Y is O or Nr8], its pharmaceutically permissible salt or a hydrate or a solvate thereof, e.g. a compound represented by a general formula 2. The compound represented by general formula 1 has LPL potentiating action and can lower triglyceride in blood and increase HDL cholesterol and is useful as a prophylactic or therapeutic agent for hyperlipemia, arteriosclerotic diseases, etc.