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    • 3. 发明授权
    • Lactol derivatives, their production and use
    • 乳糖衍生物,其生产和使用
    • US5496834A
    • 1996-03-05
    • US300738
    • 1994-09-02
    • Takashi SohdaYukio FujisawaSatoru OiJunji Mizoguchi
    • Takashi SohdaYukio FujisawaSatoru OiJunji Mizoguchi
    • A61K38/00C07K5/06C07K5/078A61K31/44A61K31/35A61K31/40
    • C07K5/06139C07K5/06043A61K38/00
    • The present invention provides novel compound of the formulas (Ia) or (I): ##STR1## wherein Q is one or two amino acid residues which may be substituted; R.sup.3 is a carboxyl group which may be esterified or an acyl group; A is an alkylene group; B is hydrogen or an alkyl group which may be substituted or an acyl group; or a salt thereof; ##STR2## wherein R.sup.1 and R.sup.2 may be the same or different and each is hydrogen or a hydrocarbon residue which may be substituted; R.sup.3, A and B have the same definitions as those shown above; m and n each is 0 or 1; provided that where both m and n are both equal to 0, R.sup.3 is a carboxyl group which may be esterified or an acyl group having not less than 7 carbon atoms; or a salt thereof.The compound (Ia) or (I) shows cathepsin L inhibitory and bone resorption inhibitory activities and are useful as a prophylactic/therapeutic agent for osteoporosis.
    • 本发明提供新的式(Ia)或(I)化合物:其中Q是一个或两个可被取代的氨基酸残基; R3是可被酯化的羧基或酰基; A是亚烷基; B是氢或可以被取代的烷基或酰基; 或其盐; (I)其中R 1和R 2可以相同或不同,各自为氢或可被取代的烃残基; R3,A和B具有与上述相同的定义; m和n各自为0或1; 条件是当m和n都等于0时,R 3是可被酯化的羧基或具有不少于7个碳原子的酰基; 或其盐。 化合物(Ia)或(I)表示组织蛋白酶L抑制和骨吸收抑制活性,可用作骨质疏松症的预防/治疗剂。
    • 9. 发明授权
    • Oxazolidinedione derivatives and their use
    • 恶唑二酮衍生物及其用途
    • US06552058B1
    • 2003-04-22
    • US09667247
    • 2000-09-22
    • Takashi SohdaHitoshi IkedaYu MomoseSachiko Imai
    • Takashi SohdaHitoshi IkedaYu MomoseSachiko Imai
    • C07D26318
    • C07D263/44C07D413/12C07D413/14C07D417/12
    • Novel 2,4-oxazolidinedione compounds of the formula: wherein R is a hydrocarbon residue or a heterocyclic group each of which may be substituted; Y is —CO—, —CH(OH)— or —NR3— (wherein R3 is an alkyl group which may be substituted); m is 0 or 1; n is 0, 1 or 2; X is CH or N; A is bivalent straight or branched hydrocarbon chain residue having 1 to 7 carbon atoms; R1 and R2 each are hydrogen or an alkyl group, or R1 and R2 are combined with each other to form a 5- to 6-membered heterocyclic group optionally containing nitrogen; L and M each are hydrogen, or L and M are combined with each other to form a bond, or pharmaceutically acceptable salts thereof, having excellent hypoglycemic and hypolipidemic activities and are useful as anti-diabetics or hypolipidemic agents.
    • 下式的新型2,4-恶唑烷二酮化合物:其中R是可以被取代的烃残基或杂环基; Y是-CO - , - CH(OH) - 或-NR 3 - (其中R 3是可被取代的烷基); m为0或1; n为0,1或2; X是CH或N; A是具有1至7个碳原子的二价直链或支链烃链残基; R 1和R 2各自为氢或烷基,或者R 1和R 2彼此结合形成任选含有氮的5至6元杂环基; L和M各自为氢,或L和M彼此结合以形成具有优异的降血糖和降血脂活性的键或其药学上可接受的盐,并且可用作抗糖尿病药或降血脂药。
    • 10. 发明授权
    • Anticachectic composition
    • 防寒组成
    • US06365607B1
    • 2002-04-02
    • US09605628
    • 2000-06-28
    • Yu MomoseEtsuya MatsutaniTakashi Sohda
    • Yu MomoseEtsuya MatsutaniTakashi Sohda
    • A61K3144
    • A61K31/4439A61K31/422A61K31/427
    • A medicinal composition for the prophylaxis and treatment of cachexia which comprises a compound of the formula: wherein R represents a hydrocarbon group that may be substituted or a heterocyclic group that may be substituted; Y represents a group of the formula —CO—, —CH(OH)—, or —NR3— (R3 represents an alkyl group that may be substituted); m is 0 or 1; n is 0, 1 or 2; X represents CH or N; A represents a bond or a bivalent aliphatic hydrocarbon group having 1 to 7 carbon atoms; Q represents oxygen or sulfur; R1 represents hydrogen or an alkyl group; ring E may have further 1 to 4 substituents, which may form a ring in combination with R1; L and M respectively represent hydrogen or may be combined with each other to form a bond, provided that when m and n are 0, X represents CH, A represents a bond, Q represents sulfur, R1, L and M respectively represent hydrogen, and ring E does not have further substituents, R does not represent dihydrobenzopyranyl; or a salt thereof.
    • 一种用于预防和治疗恶病质的药物组合物,其包含下式化合物:其中R表示可被取代的烃基或可被取代的杂环基; Y表示式-CO-,-CH(OH) - 或-NR 3 - (R 3表示可被取代的烷基)的基团; m为0或1; n为0,1或2; X表示CH或N; A表示碳原子数1〜7的键或2价脂肪族烃基, Q表示氧或硫; R1表示氢或烷基; 环E可以具有另外1至4个取代基,其可以与R 1组合形成环; L和M分别表示氢或可以彼此结合形成键,条件是当m和n为0时,X表示CH,A表示键,Q表示硫,R 1,L和M表示氢, 环E不具有其它取代基,R不表示二氢苯并吡喃基; 或其盐。