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    • 2. 发明授权
    • Phosphonic acid derivatives and the treating agents of diseases related hyperphosphatemia
    • 膦酸衍生物和疾病相关高磷血症的治疗剂
    • US07691898B2
    • 2010-04-06
    • US11664830
    • 2005-10-05
    • Hiroshi TomiyamaMasayuki YokotaKazuo TokuzakiRyoko Tomita
    • Hiroshi TomiyamaMasayuki YokotaKazuo TokuzakiRyoko Tomita
    • A61K31/381C07D333/46C07F9/30
    • C07F9/6541C07F9/3834C07F9/3882C07F9/3891C07F9/59C07F9/6539C07F9/65517C07F9/655345C07F9/655354C07F9/6558C07F9/65586
    • This invention related to a series of new phosphonic acid derivatives having anti-hyperphosphatemia activity. wherein: A is selected from —(CH2)n—, —CO—, —(CH2)n—CO—(CH2)m—, —(CH2)n—CS—(CH2)m— or a branched alkylene group, B ring and C ring are selected from a benzene ring, naphthalene ring, azulene ring or, heterocycle or fused heterocycle compound, D is —(CH2)(n+1)—, —(CH2)—O—(CH2)m—, —(CH2)—S(O)o—(CH2)m—, —CF3 or —(CH2)n—NR10—(CH2)m— wherein a D ring is connected with the carbon atom composing the C ring, E is selected from an oxygen atom or a sulfur atom, P is a phosphine atom, R1˜R7, wherein R1 and R2, R4 and R5 are joined together with neighbored carbon atom to form 5˜7 membered saturated or unsaturated hydrocarbon ring, or 5˜6 membered fused heterocycle, R1, R2 and R3 are not a hydrogen atom if the B ring is a benzene ring and may be the same or different and are substituents, R8 and R9 are may be the same or different and are substituents, R10 is an alkyl group, n and m are 0-10 and o is 0-2.
    • 本发明涉及一系列具有抗高磷酸血症活性的新型膦酸衍生物。 其中:A选自 - (CH 2)n - , - CO - , - (CH 2)n -CO-(CH 2)m - , - (CH 2)n -C CS-(CH 2)m-或支链亚烷基, B环和C环选自苯环,萘环,薁环或杂环或稠合杂环化合物,D是 - (CH 2)(n + 1) - , - (CH 2)-O-(CH 2)m - , - (CH2)-S(O)o-(CH2)m-,-CF3或 - (CH2)n-NR10-(CH2)m-,其中D环与构成C环的碳原子连接,E 选自氧原子或硫原子,P为膦原子,R1〜R7,其中R1和R2,R4和R5与邻位碳原子连接在一起形成5〜7元饱和或不饱和烃环,或5 如果B环是苯环并且可以相同或不同,并且是取代基,则R 6,R 6和R 3不是氢原子,R 8和R 9可以相同或不同,并且是取代基R 10 是烷基,n和m是0-10,o是0-2。
    • 4. 发明授权
    • β-lactam compounds process for reproducing the same and serum cholesterol-lowering agents containing the same
    • 用于再现相同的β-内酰胺化合物的方法和含有它们的血清胆固醇降低剂
    • US07045515B2
    • 2006-05-16
    • US10450171
    • 2002-02-20
    • Hiroshi TomiyamaMasayuki YokotaAtsushi NodaAkira Ohno
    • Hiroshi TomiyamaMasayuki YokotaAtsushi NodaAkira Ohno
    • C07D205/08A61K31/397A61P3/06
    • C07D405/10C07D405/12
    • Novel β-lactam compounds represented by the following formula (I) or pharmaceutically acceptable salts thereof which are useful as serum cholesterol-lowering agents: (I) wherein A1, A3 and A4 represent each hydrogen, halogen C1-5 alkyl, C1-5 alkoxy, —COOR1, a group represented by the following general formula (b): (b) wherein R1 represents hydrogen or C1-5 alkyl, or a group represented by the following general formula (a): (a) wherein R2 represents —CH2OH, —CH2OC(O)—R1 or —CO2—R1; R3 represents —OH or —OC(O)—R1; R4 represents —(CH2)kR5(CH2)1- wherein K and 1 are each 0 or an integer of 1 or above provided k+1 is an integer of not more than 10; and R5 represents a single bond, —CH═CH—, —OCH2—, carbonyl or —CH(OH)—; provided that at least one of A1, A3 and A4 is a group represented by the above formula (a); A2 represents C1-5 alkyl, C1-5 alkoxy, C1-5 alkenyl, C1-5 hydroxyalkyl or C1-5 carbonylalkyl; and n, p, q and r are each an integer of 0, 1 or 2.
    • 由下式(I)表示的新型β-内酰胺化合物或其药学上可接受的盐可用作血清降胆固醇剂:(I)其中A 1,A 3, >和A 4各自表示氢,卤素C 1-5烷基,C 1-5烷氧基,-COOR 1, (b)表示的基团:(b)其中R 1表示氢或C 1-5烷基,或由以下通式(b)表示的基团: 以下通式(a):(a)其中R 2代表-CH 2 OH,-CH 2 OC(O)-R' SUB> 1或-CO 2 -R 1; R 3表示-OH或-OC(O)-R 1; R 4表示 - (CH 2)2 R 5(CH 2)2 - (CH 2) 其中K和1各自为0或1或更高的整数,k + 1为不大于10的整数; 和R 5表示单键,-CH-CH-,-OCH 2 - ,羰基或-CH(OH) - ; 条件是A 1,A 3和A 4中的至少一个是由上述式(a)表示的基团。 A 2表示C 1-5烷基,C 1-5烷氧基,C 1-5 - 烯基,C 1-5个羟基烷基或C 1-5烷基羰基; 并且n,p,q和r各自为0,1或2的整数。