Sulfonamide Derivative Selectively Inhibiting Mmp-13
    1.
    发明申请
    Sulfonamide Derivative Selectively Inhibiting Mmp-13 审中-公开
    磺酰胺衍生物选择性抑制Mmp-13

    公开(公告)号:US20080119513A1

    公开(公告)日:2008-05-22

    申请号:US11574801

    申请日:2004-09-06

    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; R1 is hydroxy and the like; R2 is hydrogen atom, optionally substituted lower alkyl, and the like; R12 is hydrogen atom; or R2 and R12 taken together with the adjacent carbon atom may form a ring; R3 is hydrogen atom, optionally substituted lower alkyl, and the like; R4 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)的活动引起的或与其相关的疾病。 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是键,-C≡C-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。

    Sulfonamide derivative having isoxazole ring
    2.
    发明授权
    Sulfonamide derivative having isoxazole ring 失效
    具有异恶唑环的磺酰胺衍生物

    公开(公告)号:US07825146B2

    公开(公告)日:2010-11-02

    申请号:US10565948

    申请日:2004-07-28

    IPC分类号: A61K31/422

    CPC分类号: C07D261/08 A61K31/42

    摘要: A compound represented by the general formula (I-A): wherein R1 is hydroxy and the like; R2 is optionally substituted lower alkyl and the like; R3 is hydrogen atom and the like; R4 is optionally substituted arylene and the like; R5 is a group represented by the formula: R6 is optionally substituted aryl and the like, its optically active substance, their pharmaceutically acceptable salt, or a solvate thereof; and a metalloproteinase inhibitor containing them.

    摘要翻译: 由通式(I-A)表示的化合物:其中R1是羟基等; R2是任选取代的低级烷基等; R3是氢原子等; R4是任选取代的亚芳基等; R5是由下式表示的基团:R6是任选取代的芳基等,其光学活性物质,其药学上可接受的盐或其溶剂化物; 和含有它们的金属蛋白酶抑制剂。

    Sulfonamide derivative having isoxazole ring
    3.
    发明申请
    Sulfonamide derivative having isoxazole ring 失效
    具有异恶唑环的磺酰胺衍生物

    公开(公告)号:US20060183770A1

    公开(公告)日:2006-08-17

    申请号:US10565948

    申请日:2004-07-28

    CPC分类号: C07D261/08 A61K31/42

    摘要: A compound represented by the general formula (I-A): wherein R1 is hydroxy and the like; R2 is optionally substituted lower alkyl and the like; R3 is hydrogen atom and the like; R4 is optionally substituted arylene and the like; R5 is a group represented by the formula: R6 is optionally substituted aryl and the like, its optically active substance, their pharmaceutically acceptable salt, or a solvate thereof; and a metalloproteinase inhibitor containing them.

    摘要翻译: 由通式(I-A)表示的化合物:其中R 1是羟基等; R 2是任选取代的低级烷基等; R 3是氢原子等; R 4是任选取代的亚芳基等; R 5是由下式表示的基团:R 6是任选取代的芳基等,其光学活性物质,其药学上可接受的盐或其溶剂化物; 和含有它们的金属蛋白酶抑制剂。

    Sulfonamide derivatives having oxadiazole rings
    5.
    发明授权
    Sulfonamide derivatives having oxadiazole rings 失效
    具有恶二唑环的磺酰胺衍生物

    公开(公告)号:US06495578B1

    公开(公告)日:2002-12-17

    申请号:US09959008

    申请日:2001-10-17

    IPC分类号: A61K314196

    CPC分类号: C07D413/04

    摘要: Sulfonamide derivatives having a matrix metalloprotease inhibiting effect, which are compounds represented by general formula (I), optical isomers of the same, pharmaceutically acceptable salts of both, or solvates of them: wherein R1 and R2 are each independently hydrogen atom, optionally substituted lower alkyl or the like; R3 is optionally substituted aryl, optionally substituted heteroaryl or the like; X is —CH═CH—, —O—, or —S—; Y is NHOH, hydroxy, or lower alkyloxy.

    摘要翻译: 具有基质金属蛋白酶抑制作用的磺酰胺衍生物,其为通式(I)表示的化合物,其光学异构体,它们的药学上可接受的盐或它们的溶剂合物:其中R1和R2各自独立地为氢原子,任选取代的低级 烷基等; R3是任选取代的芳基,任选取代的杂芳基等; X是-CH = CH-,-O-或-S-; Y是NHOH,羟基或低级烷氧基。

    6,7-UNSATURATED-7-CARBAMOYL SUBSTITUTED MORPHINAN DERIVATIVE
    9.
    发明申请
    6,7-UNSATURATED-7-CARBAMOYL SUBSTITUTED MORPHINAN DERIVATIVE 有权
    6,7-不饱和的7-羧基取代的摩尔衍生物

    公开(公告)号:US20120135978A1

    公开(公告)日:2012-05-31

    申请号:US13308483

    申请日:2011-11-30

    CPC分类号: C07D489/08

    摘要: A novel compound which is useful as an agent for treating and/or preventing emesis, vomiting and/or constipation.A compound represented by the formula (I): wherein R1 and R2 are each independently hydrogen, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted cycloalkyl, optionally substituted aryl etc., R3 is hydrogen, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl, optionally substituted lower alkoxy etc., R4 is hydrogen or lower alkyl, R5 is hydrogen, lower alkyl, cycloalkyl lower alkyl or lower alkenyl, or a pharmaceutically acceptably salt, or a solvate thereof is provided.

    摘要翻译: 可用作治疗和/或预防呕吐,呕吐和/或便秘的药剂的新型化合物。 由式(I)表示的化合物:其中R 1和R 2各自独立地为氢,任选取代的低级烷基,任选取代的低级烯基,任选取代的环烷基,任选取代的芳基等,R 3为氢,羟基,任选取代的低级烷基, 提供任选取代的低级烯基,任选取代的低级炔基,任选取代的低级烷氧基等,R4是氢或低级烷基,R5是氢,低级烷基,环烷基低级烷基或低级烯基,或其药学上可接受的盐或其溶剂化物 。

    Detergent composition comprising a sub-stoichiometric alkoxylated phosphate ester
    10.
    发明授权
    Detergent composition comprising a sub-stoichiometric alkoxylated phosphate ester 有权
    包含亚化学计量的烷氧基化磷酸酯的洗涤剂组合物

    公开(公告)号:US07435710B2

    公开(公告)日:2008-10-14

    申请号:US11622742

    申请日:2007-01-12

    IPC分类号: C11D1/72 C11D7/36

    CPC分类号: C11D1/345

    摘要: Provided is a detergent composition having components (A) and (B1): (A) a phosphate monoester (1), and (B1) a phosphate monoester (2), wherein n=1; components (A), (B1) and (B2): (A) a phosphate monoester (1), (B1) a phosphate monoester (2), wherein n=1, and (B2) a phosphate monoester (2), wherein n=2; components (A), (B1) and (B2): (A) a phosphate monoester (1), (B1) a phosphate monoester (2) wherein n=1, and (B2) a phosphate monoester (2), wherein n=2; components (A) and (C): (A) a phosphate monoester (1), and (C) a phosphate monoester (3); or a phosphate-based surfactant produced by reacting a compound obtained by adding to an alcohol an alkylene oxide of 2 to 4 carbon atoms, with phosphoric acid, a polyphosphoric acid or P2O5: The detergent composition is mild to the skin, is high in versatility, and has a good foaming property in weak acidic water or in hard water.

    摘要翻译: 本发明提供一种具有成分(A)和(B 1)的洗涤剂组合物:(A)磷酸酯单酯(1)和(B 1/3)磷酸酯单酯(2 ),其中n = 1; 组分(A),(B 1/2)和(B 2):(A)磷酸酯单酯(1),(B 1 H 2) 磷酸酯单酯(2),其中n = 1,和(B 2 H 2)磷酸酯单酯(2),其中n = 2; 组分(A),(B 1/2)和(B 2):(A)磷酸酯单酯(1),(B 1 H 2) 其中n = 1的磷酸酯单酯(2)和磷酸酯单酯(2)的(B 2)2,其中n = 2; 组分(A)和(C):(A)磷酸酯单酯(1)和(C)磷酸酯单酯(3); 或通过将通过向醇中加入2至4个碳原子的烯化氧获得的化合物与磷酸,多磷酸或P 2 O 5 O 5反应而制备的磷酸盐基表面活性剂, 洗涤剂组合物对皮肤温和,通用性高,在弱酸性水或硬水中具有良好的起泡性。