SULFONAMIDE DERIVATIVE SELECTIVELY INHIBITING MMP-13
    102.
    发明公开
    SULFONAMIDE DERIVATIVE SELECTIVELY INHIBITING MMP-13 审中-公开
    SULFONAMIDDERIVAT,DAS SELEKTIV MMP-13 HEMMT

    公开(公告)号:EP1787979A1

    公开(公告)日:2007-05-23

    申请号:EP05781598.7

    申请日:2005-09-05

    IPC分类号: C07C311/00

    摘要: It is considered that MMP-13 inhibitors contribute to the treatment or prevention against the diseases caused by or related to activity of MMP-13, especially osteoarthritis (OA). Therefore, the development of MMP-13 inhibitors has been desired.
    A compound represented by the general formula (I):

    wherein Z is 1,4-phenylene and the like; R 1 is hydroxy and the like; R 2 is hydrogen atom, optionally substituted lower alkyl, and the like; R 12 is hydrogen atom; or R 2 and R 12 taken together with the adjacent carbon atom may form a ring; R 3 is hydrogen atom, optionally substituted lower alkyl, and the like; R 4 is halogen, lower alkyl, and the like; m is 0, 1, or 2; X is a bond, -C≡C-, and the like; Y is optionally substituted phenyl, optionally substituted naphthyl, and the like, its optically active substance, their pharmaceutically acceptable salt, or a solvate thereof.

    摘要翻译: 认为MMP-13抑制剂有助于治疗或预防由MMP-13,特别是骨关节炎(OA)引起的或与MMP-13的活性有关的疾病。 因此,期望MMP-13抑制剂的发展。 由通式(I)表示的化合物:其中Z是1,4-亚苯基等; R 1是羟基等; R 2是氢原子,任选取代的低级烷基等; R 12是氢原子; 或R 2和R 12与相邻碳原子一起可以形成环; R 3是氢原子,任选取代的低级烷基等; R 4是卤素,低级烷基等; m为0,1或2; X是一个债券,-C¡C等等; Y是任选取代的苯基,任选取代的萘基等,其光学活性物质,其药学上可接受的盐或其溶剂化物。

    3-PYRIDINIUM METHYLCEPHEM COMPOUND
    105.
    发明公开
    3-PYRIDINIUM METHYLCEPHEM COMPOUND 审中-公开
    3-吡啶鎓甲基化合物

    公开(公告)号:EP1721906A1

    公开(公告)日:2006-11-15

    申请号:EP05719869.9

    申请日:2005-03-03

    CPC分类号: C07D501/00

    摘要: A compound of Formula 1:

    (wherein A is optionally substituted lower alkylene (substituent: mono- or di- lower alkyl, lower alkylidene, or lower alkylene having two or more carbons); Z + is either of the groups shown below:

    (wherein R 1 and R 2 are each independently hydrogen, optionally substituted amino lower alkyl or optionally substituted cyclic amino; R 3 is hydrogen or amino; X is N or CR 4 (R 4 is hydrogen or optionally substituted lower alkyl)), a pharmaceutically acceptable salt or a solvate thereof.

    摘要翻译: 式1的化合物:其中A为任选取代的低级亚烷基(取代基:具有两个或更多个碳的单或二低级烷基,低级亚烷基或低级亚烷基); Z +为以下所示的基团之一:(其中R1 和R2各自独立地为氢,任选取代的氨基低级烷基或任选取代的环状氨基; R3为氢或氨基; X为N或CR4(R4为氢或任选取代的低级烷基)),其药学上可接受的盐或溶剂化物。

    NAPHTHYLIDINE DERIVATIVE HAVING HIV INTEGRASE INHIBITORY ACTIVITY
    106.
    发明公开
    NAPHTHYLIDINE DERIVATIVE HAVING HIV INTEGRASE INHIBITORY ACTIVITY 审中-公开
    美国艾滋病毒综合防治艾滋病毒综合征

    公开(公告)号:EP1714966A1

    公开(公告)日:2006-10-25

    申请号:EP05704349.9

    申请日:2005-02-02

    CPC分类号: C07D471/04

    摘要: [Problems to be Solved]
    To provide a novel compound having antiviral activity, especially inhibitory activity against HIV integrase, a pharmaceutical composition, especially anti-HIV drug, containing the same.
    [Means to Solve the Problem]
    A compound of the formula:

    (wherein:
    R 1 is optionally substituted aralkyl;
    R 2 and R 3 are each independently hydrogen, optionally substituted alkyl, optionally substituted amino, optionally substituted alkenyl or optionally substituted alkoxy (provided that each substituent for "optionally substituted" is a noncyclic group);
    R 4 is hydrogen, optionally substituted carboxy, optionally substituted formylamino, optionally substituted carbamoyl, optionally substituted amino (provided that a substituent on amino in "optionally substituted formylamino", "optionally substituted carbamoyl" and "optionally substituted amino" may form an optionally-substituted N-atom containing heterocyclic ring together with an adjacent N atom), optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, or optionally substituted heteroaryl) or a salt thereof.

    摘要翻译: [待解决的问题]提供具有抗病毒活性,特别是抗HIV整合酶抑制活性的新型化合物,含有该化合物的药物组合物,特别是抗HIV药物。 [解决问题的方法]下式化合物:其中:R 1为任选取代的芳烷基; R 2和R 3各自独立地为氢,任选取代的烷基,任选取代的氨基,任选取代的烯基或任选取代的烷氧基(提供 “任选取代的”的每个取代基是非环基团; R 4是氢,任选取代的羧基,任选取代的甲酰氨基,任选取代的氨基甲酰基,任选取代的氨基(条件是“任选取代的甲酰氨基”上的氨基上的取代基, 取代的氨基甲酰基“和”任选取代的氨基“可以与相邻的N原子一起形成任选取代的含有N原子的杂环),任选取代的烷基,任选取代的烯基,任选取代的芳基或任选取代的杂芳基)或其盐 。

    CEPHEM COMPOUNDS AND DRUGS CONTAINING THE COMPOUNDS
    107.
    发明授权
    CEPHEM COMPOUNDS AND DRUGS CONTAINING THE COMPOUNDS 失效
    头孢类及药物含有这些化合物

    公开(公告)号:EP0893446B1

    公开(公告)日:2006-10-04

    申请号:EP97914600.8

    申请日:1997-04-04

    摘要: Cephem compounds having groups of general formula (II) at the 3-position of the cephem ring, or salts or hydrates thereof, wherein Het is a mono- or poly-cyclic hetero-ring having one or more atoms selected from among N, O and S which may be the same or different from each other; R1 is hydrogen, optionally substituted lower alkyl or lower alkenyl; A is optionally substituted lower alkylene, lower alkenylene or a single bond while B is optionally substituted imino or a single bond, or alternatively A and B may be united to form a single bond; and D is a single bond or group (a).

    Intermediates for cephem compounds
    109.
    发明公开
    Intermediates for cephem compounds 失效
    ZwischenproduktefürCephemverbindungen

    公开(公告)号:EP1544197A1

    公开(公告)日:2005-06-22

    申请号:EP05006670.3

    申请日:1997-04-04

    IPC分类号: C07D401/04 C07D409/04

    摘要: A cephem compound, wherein the cephem ring has a substituent at the 3-position, which substituent is shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R 1 is hydrogen, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; A is an optionally substituted lower alkylene, an optionally substituted lower alkenylene or a single bond; B is an optionally substituted imino or a single bond; or A and B taken together may form a single bond; and D is a single bond or a group of the formula (a):

    摘要翻译: 头孢烯化合物,其中头孢烯环在3位上具有取代基,该取代基由式II表示,其中Het是包含一个或多个选自N, O和S可以相同或不同; R 1是氢,任选取代的低级烷基或任选取代的低级烯基; A是任选取代的低级亚烷基,任选取代的低级亚烯基或单键; B是任选取代的亚氨基或单键; 或A和B组合在一起可形成单一债券; 和D是单键或式(a)的基团: