N-Hydroxy-2-(4-phenylpiperidin-1-ylsulphonyl)acetamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: N-Hydroxy-2-(4-phenylpiperidin-1-ylsulphonyl)acetamide
• 英文别名: N-hydroxy-2-(4-phenyl-piperidine-1-sulfonyl)-acetamide；N-hydroxy-2-(4-phenylpiperidin-1-yl)sulfonylacetamide
• 化学式: C₁₃H₁₈N₂O₄S
• 分子量: 298.363
• InChiKey: DZKBXUUQLMNCGH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  20
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  95.1
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• [EN] HYDROXAMIC ACID DERIVATIVES AS MATRIX METALLOPROTEASE (MMP) INHIBITORS<br/>[FR] DERIVES D'ACIDE HYDROXAMIQUE UTILISES COMME INHIBITEURS DE METALLOPROTEASES MATRICIELLES
  申请人：PFIZER LIMITED

  公开号：WO1999029667A1

  公开（公告）日：1999-06-17

  (EN) Compounds of formula (I) or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R 1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, $i(inter alia), tissue ulceration, wound repair and skin diseases.(FR) L'invention concerne des composés représentés par la formule (I); ou leurs sels acceptables sur le plan pharmaceutique ou vétérinaire, ou des solvates de chacune de ces entités, acceptables sur le plan pharmaceutique ou vétérinaire. Dans ladite formule, la ligne hachurée représente une liaison facultative; A représente C ou CH: B représente CH2, O ou est absent: R1 et R2 sont chacun indépendamment choisis parmi hydrogène, alkyle C1-C6 éventuellement substitué par alcoxy C1-C4 ou phényle, et alcényle C1-C6; ou, conjointement avec l'atome de carbone auquel ils sont attachés, ils forment un groupe cycloalkyle C3-C6 qui comprend éventuellement une liaison hétéroatomique choisie parmi O, SO, SO2 et NR6 ou qui est éventuellement benzo-condensé; R3 représente hydrogène, halo, R7 ou OR7; R4 représente hydrogène, alkyle C1-C4, alcoxy C1-C4, trifluorométhyle ou halo; R6 représente hydrogène ou alkyle C1-C4; R7 représente un système de noyau bicyclique ou monocyclique éventuellement substitué; m représente 1 ou 2; et n représente 0, 1 ou 2; à condition que B ne représente pas O lorsque A représente C. Lesdits composés sont des inhibiteurs de métalloprotéases matricielles utiles, entre autres, pour le traitement de l'ulcération des tissus, de la cicatrisation des blessures et des maladies cutanées.

  化合物的化学式为(I)，或其在药学或兽医学上可接受的盐，或者在药学或兽医学上可接受的溶剂化物，其中断裂线代表可选键；A为C或CH；B为CH2，O或不存在；R1和R2各自独立地选择氢，C1至C6烷基，可选择地被C1至C4烷氧基或苯基取代，以及C1至C6烯基；或者与它们附着的碳原子一起形成一个C3至C6环烷基，该环烷基可以选择地包括从O，SO，SO2和NR6中选择的杂原子连接或者可以选择地与苯融合；R3为氢，卤素，R7或OR7；R4为氢，C1至C4烷基，C1至C4烷氧基，三氟甲基或卤素；R6为氢或C1至C4烷基；R7为可选取代的单环或双环环系；m为1或2；n为0，1或2；但是当A为C时，B不为O。这些化合物是MMP抑制剂，可用于治疗组织溃疡、伤口修复和皮肤疾病等。
• MMP inhibitors for the treatment of ocular angiogenesis
  申请人：Pfizer Products Inc.

  公开号：EP0930067A2

  公开（公告）日：1999-07-21

  The present invention relates to the use of matrix metalloproteinase inhibitors, preferably those which display specificity for matrix metalloproteinases-2 or 9, in the treatment or prevention of ocular angiogenesis.

  本发明涉及基质金属蛋白酶抑制剂（最好是对基质金属蛋白酶-2 或 9 具有特异性的抑制剂）在治疗或预防眼部血管生成中的应用。
• HAIR TREATMENT COMPOSITION AND HAIR COSMETIC FOR DAMAGED HAIR
  申请人：Meiji Seika Kaisha, Ltd.

  公开号：EP1602354A1

  公开（公告）日：2005-12-07

  The present invention intends to provide a composition for hair treatment containing γ-polyglutamic acid or a salt thereof, a hair cosmetic for damaged hair containing such a composition, and their uses. The composition for hair treatment containing γ-polyglutamic acid or a salt thereof and the hair cosmetic for damaged hair of the present invention have excellent improvement effects on the strength and frictional force of hair, so that they can provide tension, elasticity, or the like to damage hair to prevent or alleviate split hair and broken hair as well as improvements in combing and touch. Furthermore, they also exert effects of moisture retention inherent to γ-polyglutamic acid or a salt thereof, preventing or improving effects on the generation of dandruff on the basis of such effects, preventing effects on the feeling of stickiness or creak, and various effectiveness including appropriate residual tendency to hair in a simultaneous manner, respectively.

  本发明旨在提供一种含有γ-聚谷氨酸或其盐的头发治疗组合物、一种含有这种组合物的用于受损头发的护发化妆品及其用途。本发明的含有γ-聚谷氨酸或其盐的头发治疗组合物和用于受损头发的护发化妆品对头发的强度和摩擦力有很好的改善效果，因此它们可以为受损头发提供张力、弹性等，以防止或减轻头发分叉和断裂，并改善梳理和触感。此外，它们还能分别发挥γ-聚谷氨酸或其盐固有的保湿效果、在此基础上防止或改善头皮屑产生的效果、防止粘腻感或吱吱作响的效果，以及包括同时对头发产生适当残留倾向在内的各种功效。
• Cosmetic composition and production thereof
  申请人：Kawasaki Yuji

  公开号：US20060018867A1

  公开（公告）日：2006-01-26

  It has been desired to develop a highly preservative and antibacterial cosmetic composition that can easily be applied to both emulsion and non-emulsion type cosmetics. It has also been desired to develop a method of improving a preservative and/or antibacterial effect(s) of a cosmetic composition comprising polyorganosiloxane-containing epsilon-polylysine and thereby reducing the amount of antibacterial preservative agent to be used. There is provided a cosmetic composition comprising one or a combination of two or more of polyorganosiloxane-containing epsilon-polylysine compounds obtained by reacting epsilon-polylysine with polyorganosiloxane or a physiologically acceptable salt thereof, and polyhydric alcohol.

  人们一直希望开发一种高防腐性和抗菌性的化妆品组合物，这种组合物既可用于乳液型化妆品，也可用于非乳液型化妆品。此外，还希望开发一种方法，以改善含有聚有机硅氧烷的ε-聚赖氨酸的化妆品组合物的防腐和/或抗菌效果，从而减少抗菌防腐剂的用量。本发明提供了一种化妆品组合物，该组合物包含一种或两种以上的含聚有机硅氧烷的ε-聚赖氨酸化合物的组合，这些ε-聚赖氨酸化合物是通过ε-聚赖氨酸与聚有机硅氧烷或其生理上可接受的盐以及多元醇反应而得到的。
• Hair treatment composition and hair cosmetic for damaged hair
  申请人：Hasebe Kouhei

  公开号：US20060165636A1

  公开（公告）日：2006-07-27

  The present invention intends to provide a composition for hair treatment containing γ-polyglutamic acid or a salt thereof, a hair cosmetic for damaged hair containing such a composition, and their uses. The composition for hair treatment containing γ-polyglutamic acid or a salt thereof and the hair cosmetic for damaged hair of the present invention have excellent improvement effects on the strength and frictional force of hair, so that they can provide tension, elasticity, or the like to damage hair to prevent or alleviate split hair and broken hair as well as improvements in combing and touch. Furthermore, they also exert effects of moisture retention inherent to γ-polyglutamic acid or a salt thereof, preventing or improving effects on the generation of dandruff on the basis of such effects, preventing effects on the feeling of stickiness or creak, and various effectiveness including appropriate residual tendency to hair in a simultaneous manner, respectively.

  本发明旨在提供一种含有γ-聚谷氨酸或其盐的头发治疗组合物、一种含有这种组合物的用于受损头发的护发化妆品及其用途。本发明的含有γ-聚谷氨酸或其盐的头发治疗组合物和用于受损头发的护发化妆品对头发的强度和摩擦力有很好的改善效果，因此它们可以为受损头发提供张力、弹性等，以防止或减轻头发分叉和断裂，并改善梳理和触感。此外，它们还能分别发挥γ-聚谷氨酸或其盐固有的保湿效果、在此基础上防止或改善头皮屑产生的效果、防止粘腻感或吱吱作响的效果，以及包括同时对头发产生适当残留倾向在内的各种功效。