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    • 44. 发明授权
    • Retinoid prodrug compound
    • 维甲酸前药化合物
    • US08633335B2
    • 2014-01-21
    • US12682966
    • 2007-10-31
    • Hideaki MuratakeKoichi Shudo
    • Hideaki MuratakeKoichi Shudo
    • C07C51/367
    • C07C237/52C07C233/65C07C235/84C07C235/88C07C237/48C07C271/30C07C2602/10C07F7/081
    • A compound represented by the following general formula (I): [R1 to R5 represent hydrogen atom, an alkyl group, or a trialkylsilyl group, X represents —NH—CO—, —CO—NH—, —N(COR6)—CO—, —CO—N(COR7)— (R6 and R7 represent a lower alkoxy group, or a carboxy-substituted phenyl group) etc.; and Z represents —Y—CH(R12)—COOH, —CHO, —CH═CH—COOH, or —COOR13 (Y represents a single bond, —CH2—, —CH(OH)—, —CO—, —CO—NH—, or —CO—NH—CH2—CO—NH—, R12 represents hydrogen atom or a lower alkyl group, and R13 represents hydrogen atom, —CH(R14)—COOH(R14 represents hydrogen atom, a lower alkyl group, or hydroxy group), —[CH2CH2—O]n—CH2—CH2—OH, —CH2—O—[CH2CH2—O]m—CH2—OH, or —[CH(CH3)—CO—O]p—CH(CH3)—COOH (m, n and p represent an integer of 1 to 100))], a salt thereof or an ester thereof, which has a property of being converted into a retinoid after absorption in vivo.
    • 由以下通式(I)表示的化合物:[R1至R5表示氢原子,烷基或三烷基甲硅烷基,X表示-NH-CO-,-CO-NH-,-N(COR6)-CO - ,-CO-N(COR 7) - (R 6和R 7表示低级烷氧基或羧基取代的苯基)等。 Z表示-Y-CH(R 12)-COOH,-CHO,-CH = CH-COOH或-COOR 13(Y表示单键,-CH 2 - , - CH(OH) - , - CO- -NH-或-CO-NH-CH 2 -CO-NH-,R 12表示氢原子或低级烷基,R 13表示氢原子,-CH(R 14)-COOH(R ​​14表示氢原子,低级烷基 ,或羟基), - [CH 2 CH 2 -O] n -CH 2 -CH 2 -OH,-CH 2 -O- [CH 2 CH 2 -O] m -CH 2 -OH或 - [CH(CH 3)-CO-O] CH(CH 3)-COOH(m,n和p表示1〜100的整数))],其盐或其酯,其在体内吸收后具有转化为类视黄醇的性质。
    • 48. 发明申请
    • Novel Compound Having Heterocyclic Ring
    • 具有杂环的新型化合物
    • US20090299059A1
    • 2009-12-03
    • US12225819
    • 2007-03-30
    • Hideyuki SuzukiShoji HizatateIwao UtsunomiyaKoichi Shudo
    • Hideyuki SuzukiShoji HizatateIwao UtsunomiyaKoichi Shudo
    • C07D413/10
    • C07D273/06C07D255/02C07D413/10C07D413/14C07D417/14C07D471/14Y02P20/55
    • The invention provides a novel oxazolidinone derivative represented by the formula (I): wherein Ring A is optionally substituted or fused and represents (A-1) at least 7-membered monocyclic hetero ring containing at least three N atoms; (A-2) at least 6-membered monocyclic hetero ring containing at least two N atoms and at least one O atom; or (A-3) at least 7-membered monocyclic hetero ring containing at least two N atoms and at least one S atom; X1 is a single bond, —O—, —S—, —NR2—, —CO—, —CS—, —CONR3—, —NR4CO—, —SO2NR5—, and —NR6SO2— (wherein R2-R6 are independently hydrogen or lower alkyl), or lower alkylene or lower alkenylene in which one of the preceding groups may intervene; Ring B is optionally substituted carbocycle or optionally substituted heterocycle; R1 is hydrogen, or an organic residue which is able to bind to the 5-position of oxazolidinone ring in oxazolidinone antimicrobial agent, and an antibacterial agent containing the same.
    • 本发明提供由式(I)表示的新型恶唑烷酮衍生物:其中环A任选被取代或稠合并且代表(A-1)含有至少三个N原子的至少七元单环杂环; (A-2)至少含有至少两个N原子和至少一个O原子的6元单环杂环; 或(A-3)至少含有至少两个N原子和至少一个S原子的7元单环杂环; X 1是单键,-O - , - S - , - NR 2 - , - CO - , - C - , - CONR 3 - , - NR 4 CO-,-SO 2 NR 5 - 和-NR 6 SO 2 - 或低级烷基)或其中一个前述基团可以介入的低级亚烷基或低级亚烯基; 环B是任选取代的碳环或任选取代的杂环; R1是氢,或能够与恶唑烷酮抗微生物剂中的恶唑烷酮环的5位结合的有机残基,以及含有该残基的抗菌剂。