N-[4-((1R)-1-{[(R)-tert-butylsulfinyl]amino}ethyl)-2-methylphenyl]methanesulfonamide | 886842-77-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N-[4-((1R)-1-{[(R)-tert-butylsulfinyl]amino}ethyl)-2-methylphenyl]methanesulfonamide
• 英文别名: N-[4-[(1R)-1-[[(R)-tert-butylsulfinyl]amino]ethyl]-2-methylphenyl]methanesulfonamide
• CAS: 886842-77-9
• 化学式: C₁₄H₂₄N₂O₃S₂
• 分子量: 332.488
• InChiKey: ZGAQDLDKMQOIAQ-BIBXISHDSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  21
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  103
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  N-[4-((1R)-1-{[(R)-tert-butylsulfinyl]amino}ethyl)-2-methylphenyl]methanesulfonamide 在 盐酸 、 O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate 、 三乙胺 作用下， 以 1,4-二氧六环 、 甲醇 、 N,N-二甲基甲酰胺 为溶剂， 反应 5.5h， 生成 7-TERT-BUTYL-4-METHYL-N-((1R)-1-{3-METHYL-4-[(METHYLSULFONYL)AMINO]PHENYL}-ETHYL)QUINOLINE-3-CARBOXAMIDE
  参考文献：
  名称：

  AMIDE DERIVATIVES AS ION-CHANNEL LIGANDS AND PHARMACEUTICAL COMPOSITIONS AND METHODS OF USING THE SAME

  摘要：

  披露了具有以下公式表示的化合物：公式（I）。这些化合物可以制备为药物组合物，并可用于预防和治疗包括人类在内的哺乳动物的各种疾病，例如疼痛、炎症、创伤性损伤等。

  公开号：

  US20120088746A1
• 作为产物：
  描述：

  4-羟基-3-甲基苯乙酮 在 tris(dibenzylideneacetone)dipalladium(0) chloroform complex sodium tetrahydroborate 、 caesium carbonate 、 三乙胺 作用下， 以 四氢呋喃 、 二氯甲烷 为溶剂， 反应 38.17h， 生成 N-[4-((1R)-1-{[(R)-tert-butylsulfinyl]amino}ethyl)-2-methylphenyl]methanesulfonamide
  参考文献：
  名称：

  AMIDE DERIVATIVES AS ION-CHANNEL LIGANDS AND PHARMACEUTICAL COMPOSITIONS AND METHODS OF USING THE SAME

  摘要：

  披露了具有以下公式表示的化合物：公式（I）。这些化合物可以制备为药物组合物，并可用于预防和治疗包括人类在内的哺乳动物的各种疾病，例如疼痛、炎症、创伤性损伤等。

  公开号：

  US20120088746A1

文献信息

• Substituted sulfonylaminoarylmethyl cyclopropanecarboxamide as VR1 receptor antagonists
  申请人：Hanazawa Takeshi

  公开号：US20060211741A1

  公开（公告）日：2006-09-21

  This invention provides a compound of the formula (I): wherein A and B are independently CR 12 or N; D and E are each independently CR 9 or N; R 1 represents (C 1 -C 6 )alkyl; R 2 represents hydrogen, halogen, hydroxy, (C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl, hydroxy(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy or (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl; R 3 , R 4 , R 5 , R 6 , R 10 and R 11 each independently represent hydrogen, halogen, (C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, hydroxy(C 1 -C 6 )alkyl or (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl; or R 3 and R 4 are taken together with the carbon atom to which they are attached to form a 3- to 7-membered carbocyclic ring or heterocyclic ring in which one or two non-adjacent carbon atoms are optionally replaced by an oxygen atom, a sulfur atom or NH; R 7 and R 9 each independently represent hydrogen, halogen, (C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl, hydroxy(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, hydroxy(C 1 -C 6 )alkoxy, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkoxy, (C 1 -C 6 )alkylthio, (C 1 -C 6 )alkylsulfinyl, (C 1 -C 6 )alkylsulfonyl, NH 2 , [(C 1 -C 6 )alkyl]NH—, [(C 1 -C 6 )alkyl] 2 N—, H 2 N—(C 1 -C 6 )alkoxy, (C 1 -C 6 )alkyl-NH—(C 1 -C 6 )alkoxy, [(C 1 -C 6 )alkyl] 2 N(C 1 -C 6 )alkoxy; H 2 N—(C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl, (C 1 C 6 )alkyl-NH—(C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl, [(C 1 -C 6 )alkyl] 2 N(C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl or 5- or 6-membered heterocyclic ring containing at least one nitrogen atom; R 8 represents halogen, (C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl, hydroxy(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, hydroxy(C 1 -C 6 )alkoxy, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkylsulfonyl, halo(C 1 -C 6 )alkylsulfinyl, halo(C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkylthio, [(C 1 -C 6 )alkyl]NH— or [(C 1 -C 6 )alkyl] 2 N—; or R 7 and R 8 , when E is CR 9 , are taken together with the carbon atoms to which they are attached form a 5-8 membered carbocyclic or heterocyclic ring, in which one or two non-adjacent carbon atoms are optionally replaced by oxygen, sulfur, N or NH groups, wherein the carbocyclic ring or the heterocyclic ring is unsubstituted or substituted with one or more substituents each independently selected from the group consisting of hydroxy, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy and hydroxy(C 1 -C 6 )alkyl; and R 12 represents hydrogen, halogen, (C 1 -C 6 )alkyl or hydroxy(C 1 -C 6 )alkyl; or a pharmaceutically acceptable salt or solvate thereof. These compounds are useful for the treatment of disease conditions caused by overactivation of VR1 receptor such of pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.

  这项发明提供了一个化合物的结构式(I)：其中A和B分别独立地为CR12或N；D和E分别独立地为CR9或N；R1代表(C1-C6)烷基；R2代表氢、卤素、羟基、(C1-C6)烷基、卤代(C1-C6)烷基、羟基(C1-C6)烷基、(C1-C6)氧烷基或(C1-C6)氧烷基-(C1-C6)烷基；R3、R4、R5、R6、R10和R11分别独立地代表氢、卤素、(C1-C6)烷基、卤代(C1-C6)烷基、(C1-C6)氧烷基、羟基(C1-C6)烷基或(C1-C6)氧烷基-(C1-C6)烷基；或者R3和R4一起与它们连接的碳原子形成一个3-至7-成员的碳环或杂环，其中一个或两个非相邻的碳原子可以选择性地被氧原子、硫原子或NH取代；R7和R9分别独立地代表氢、卤素、(C1-C6)烷基、卤代(C1-C6)烷基、羟基(C1-C6)烷基、(C1-C6)氧烷基、羟基(C1-C6)氧烷基、(C1-C6)氧烷基-(C1-C6)烷基、(C1-C6)氧烷基-(C1-C6)氧烷基、(C1-C6)烷基硫、(C1-C6)烷基亚硫基、(C1-C6)烷基磺基、NH2、[(C1-C6)烷基]NH—、[(C1-C6)烷基]2N—、H2N—(C1-C6)氧烷基、(C1-C6)烷基-NH—(C1-C6)氧烷基、[(C1-C6)烷基]2N(C1-C6)氧烷基；H2N—(C1-C6)氧烷基-(C1-C6)烷基、(C1C6)烷基-NH—(C1-C6)氧烷基-(C1-C6)烷基、[(C1-C6)烷基]2N(C1-C6)氧烷基-(C1-C6)烷基或含有至少一个氮原子的5-或6-成员杂环，R8代表卤素、(C1-C6)烷基、卤代(C1-C6)烷基、羟基(C1-C6)烷基、(C1-C6)氧烷基、羟基(C1-C6)氧烷基、(C1-C6)氧烷基-(C1-C6)烷基、(C1-C6)氧烷基-(C1-C6)氧烷基、卤代(C1-C6)烷基磺基、卤代(C1-C6)烷基亚硫基、卤代(C1-C6)烷基氧基、卤代(C1-C6)烷基硫基、[(C1-C6)烷基]NH—或[(C1-C6)烷基]2N—；或者当E为CR9时，R7和R8一起与它们连接的碳原子形成一个5-8成员的碳环或杂环，其中一个或两个非相邻的碳原子可以选择性地被氧、硫、N或NH基团取代，其中碳环或杂环未取代或取代有一个或多个取代基，每个取代基独立地选自羟基、(C1-C6)烷基、(C1-C6)氧烷基和羟基(C1-C6)烷基；R12代表氢、卤素、(C1-C6)烷基或羟基(C1-C6)烷基；或其药学上可接受的盐或溶剂。这些化合物对于治疗由VR1受体过度激活引起的疾病状况，如哺乳动物中的疼痛等，是有用的。这项发明还提供了包含上述化合物的药物组合物。
• Substituted N-sulfonylaminobenzyl-2-phenoxyacetamide compounds as VR1 receptor agonists
  申请人：Inoue Tadashi

  公开号：US20060100460A1

  公开（公告）日：2006-05-11

  This invention provides a compound of the formula (I): wherein R 1 represents a (C 1 -C 6 )alkyl group; R 2 represents a hydrogen atom, a halogen atom, a hydroxy group, a (C 1 -C 6 ) alkyl group or a (C 1 -C 6 ) alkoxy group; R 3 , R 4 , R 5 and R 6 each independently represents a hydrogen atom, a (C 1 -C 6 ) alkyl, or a halogen atom; R 7 represents a hydrogen atom, a halogen atom, a hydroxy group, a (C 1 -C 6 ) alkyl group optionally substituted with a piperidino group, a (C- 1 -C 6 )alkoxy group optionally substituted with a 3-7 membered cycloalkyl ring, a hydroxy(C 1 -C 6 )alkoxy group, a (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl group, a (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkoxy group, a halo (C 1 -C 6 )alkyl group, a (C 1 -C 6 )alkylthio group, a (C 1 -C 6 )alkylsulfinyl group or a (C 1 -C 6 )alkylsulfonyl group; R 5 represents a (C 1 -C 6 )alkyl group, a halo(C 1 -C 6 )alkyl group, a (C 1 -C 6 )alkoxy group, a hydroxy(C 1 -C 6 )alkoxy group, a (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl group or a (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkoxy group; or R 7 and R 8 , when adjacent to each other, taken together with the carbon atoms to which they are attached form a 5-8 membered carbocyclic or heterocyclic ring, wherein the carbocyclic ring or the heterocyclic ring is unsubstituted or substituted with one or more substituents selected from the group consisting of a hydroxy group, a (C 1 -C 6 )alkyl group, a (C 1 -C 6 )alkoxy group and a hydroxy(C 1 -C 6 )alkyl group; and R 9 represents a hydrogen atom or a halogen atom; or a pharmaceutically acceptable salt or solvate thereof. These compounds are useful for the treatment of disease conditions caused by overactivation of VR1 receptor, such as pain or the like in mammalian. The present invention also provides a pharmaceutical composition comprising the compound of formula (I).

  这项发明提供了一种化合物，其化学式为（I）：其中R1代表（C1-C6）烷基基团；R2代表氢原子、卤原子、羟基、（C1-C6）烷基基团或（C1-C6）氧烷基基团；R3、R4、R5和R6分别独立地代表氢原子、（C1-C6）烷基或卤原子；R7代表氢原子、卤原子、羟基、（C1-C6）烷基基团，可选地取代有哌啶基团的（C1-C6）烷基基团，可选地取代有3-7个成员的环烷基环的（C-1-C6）氧烷基基团，羟基（C1-C6）氧烷基基团，（C1-C6）氧烷基（C1-C6）烷基基团，（C1-C6）氧烷基（C1-C6）氧烷基基团，卤代（C1-C6）烷基基团，（C1-C6）烷基硫基基团，（C1-C6）烷基亚硫基基团或（C1-C6）烷基砜基基团；R8代表（C1-C6）烷基基团，卤代（C1-C6）烷基基团，（C1-C6）氧烷基基团，羟基（C1-C6）氧烷基基团，（C1-C6）氧烷基（C1-C6）烷基基团或（C1-C6）氧烷基（C1-C6）氧烷基基团；或者R7和R8，当相邻时，与它们连接的碳原子一起形成一个5-8成员的脂环或杂环环，其中脂环或杂环环未取代或取代有一个或多个选自羟基、（C1-C6）烷基、（C1-C6）氧烷基和羟基（C1-C6）烷基的取代基；R9代表氢原子或卤原子；或其药学上可接受的盐或溶剂。这些化合物可用于治疗由VR1受体过度激活引起的疾病症状，如哺乳动物中的疼痛等。本发明还提供了一种包含化合物（I）的药物组成物。
• Substituted N-sulfonylaminophenylethyl-2-phenoxyacetamide compounds as VR1 receptor antagonists
  申请人：Hanazawa Takeshi

  公开号：US20060205980A1

  公开（公告）日：2006-09-14

  This invention provides a compound of the formula (I): wherein R 1 represents (C 1 -C 6 )alkyl; R 2 represents a hydrogen atom, a halogen atom, a hydroxy group, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, hydroxy(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl or halo(C 1 -C 6 )alkyl; R 3 represents a halogen atom, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, hydroxy(C 1 -C 6 )alkoxy, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl, (C 1 -C 6 )alkylthio, (C 1 -C 6 )alkylsulfinyl, (C 1 -C 6 )alkylsulfonyl, [(C 1 -C 6 )alkyl]NH—, or [(C 1 -C 6 )alkyl] 2 N—; R 4 represents a halogen atom, (C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, hydroxy(C 1 -C 6 )alkoxy, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkoxy, [(C 1 -C 6 )alkyl]NH—, or [(C 1 -C 6 )alkyl] 2 N—; R 5 represents a halogen atom, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, hydroxy(C 1 -C 6 )alkoxy, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl, (C 1 -C 6 )alkylthio, (C 1 -C 6 )alkylsulfinyl, (C 1 -C 6 )alkylsulfonyl, [(C 1 -C 6 )alkyl]NH—, [(C 1 -C 6 )alkyl] 2 N—, H 2 N—(C 1 -C 6 )alkoxy, (C 1 -C 6 )alkyl-NH—(C 1 -C 6 )alkoxy, [(C 1 -C 6 )alkyl] 2 N(C 1 -C 6 )alkoxy, H 2 N—(C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl, (C 1 -C 6 )alkyl-NH—(C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl, or [(C 1 -C 6 )alkyl] 2 N(C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl; and * indicates a chiral centre; or a pharmaceutically acceptable salt or solvate thereof. These compounds are useful for the treatment of disease conditions caused by overactivation of VR1 receptor such of pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.

  本发明提供了一种化合物的公式（I）： 其中，R1代表（C1-C6）烷基；R2代表氢原子，卤素原子，羟基，（C1-C6）烷基，（C1-C6）烷氧基，羟基（C1-C6）烷基，（C1-C6）烷氧基-（C1-C6）烷基或卤代（C1-C6）烷基；R3代表卤素原子，（C1-C6）烷基，（C1-C6）烷氧基，羟基（C1-C6）烷氧基，（C1-C6）烷氧基-（C1-C6）烷基，（C1-C6）烷氧基-（C1-C6）烷氧基，卤代（C1-C6）烷基，（C1-C6）烷基硫醇，（C1-C6）烷基亚砜基，（C1-C6）烷基磺酰基，[(C1-C6)烷基]NH—或[(C1-C6)烷基]2N—；R4代表卤素原子，（C1-C6）烷基，卤代（C1-C6）烷基，（C1-C6）烷氧基，羟基（C1-C6）烷氧基，（C1-C6）烷氧基-（C1-C6）烷基，（C1-C6）烷氧基-（C1-C6）烷氧基，[(C1-C6)烷基]NH—或[(C1-C6)烷基]2N—；R5代表卤素原子，（C1-C6）烷基，（C1-C6）烷氧基，羟基（C1-C6）烷氧基，（C1-C6）烷氧基-（C1-C6）烷基，（C1-C6）烷氧基-（C1-C6）烷氧基，卤代（C1-C6）烷基，（C1-C6）烷基硫醇，（C1-C6）烷基亚砜基，（C1-C6）烷基磺酰基，[(C1-C6)烷基]NH—，[(C1-C6)烷基]2N—，H2N—（C1-C6）烷氧基，（C1-C6）烷基-NH—（C1-C6）烷氧基，[(C1-C6)烷基]2N（C1-C6）烷氧基，H2N—（C1-C6）烷氧基-（C1-C6）烷基，（C1-C6）烷基-NH—（C1-C6）烷氧基-（C1-C6）烷基或[(C1-C6)烷基]2N（C1-C6）烷氧基-（C1-C6）烷基；*表示一个手性中心；或其药学上可接受的盐或溶剂。 这些化合物可用于治疗哺乳动物中由VR1受体过度激活引起的疾病状况，例如疼痛等。本发明还提供了包含上述化合物的药物组合物。
• SUBSTITUTED SULFONYLAMINOARYLMETHYL CYCLOPROPANECARBOXAMIDE AS VR1 RECEPTOR ANTAGONISTS
  申请人：HANAZAWA TAKESHI

  公开号：US20100035880A1

  公开（公告）日：2010-02-11

  This invention provides a compound of the formula (I): wherein A and B are independently CR 12 or N; D and E are each independently CR 9 or N; R 1 represents (C 1 -C 6 )alkyl; R 2 represents hydrogen, halogen, hydroxy, (C 1 -C 6 ) alkyl, halo(C 1 -C 6 ) alkyl, hydroxy(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy or (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl; R 3 , R 4 , R 5 , R 6 , R 10 and R 11 each independently represent hydrogen, halogen, (C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, hydroxy(C 1 -C 6 )alkyl or (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl; or R 3 and R 4 are taken together with the carbon atom to which they are attached to form a 3- to 7-membered carbocyclic ring or heterocyclic ring in which one or two non-adjacent carbon atoms are optionally replaced by an oxygen atom, a sulfur atom or NH; R 7 and R 9 each independently represent hydrogen, halogen, (C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl, hydroxy(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, hydroxy(C 1 -C 6 )alkoxy, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkoxy, (C 1 -C 6 )alkylthio, (C 1 -C 6 )alkylsulfinyl, (C 1 -C 6 )alkylsulfonyl, NH 2 , [(C 1 -C 6 )alkyl]NH—, [(C 1 -C 6 )alkyl] 2 N—, H 2 N—(C 1 -C 6 )alkoxy, (C 1 -C 6 )alkyl-NH—(C 1 -C 6 )alkoxy, [(C 1 -C 6 )alkyl] 2 N(C 1 -C 6 )alkoxy; H 2 N—(C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl, (C 1 -C 6 )alkyl-NH—(C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl, [(C 1 -C 6 )alkyl] 2 N(C 1 -C 6 )alkoxy-(C 1 -C 6 )alkyl or 5- or 6-membered heterocyclic ring containing at least one nitrogen atom; R 8 represents halogen, (C 1 -C 6 )alkyl, halo(C 1 -C 6 )alkyl, hydroxy(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, hydroxy(C 1 -C 6 )alkoxy, (C 1 -C 8 )alkoxy-(C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy-(C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkylsulfonyl, halo(C 1 -C 6 )alkylsulfinyl, halo(C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkylthio, [(C 1 -C 6 )alkyl]NH— or [(C 1 -C 6 )alkyl] 2 N—; or R 7 and R 8 , when E is CR 9 , are taken together with the carbon atoms to which they are attached form a 5-8 membered carbocyclic or heterocyclic ring, in which one or two non-adjacent carbon atoms are optionally replaced by oxygen, sulfur, N or NH groups, wherein the carbocyclic ring or the heterocyclic ring is unsubstituted or substituted with one or more substituents each independently selected from the group consisting of hydroxy, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy and hydroxy(C 1 -C 6 )alkyl; and R 12 represents hydrogen, halogen, (C 1 -C 6 )alkyl or hydroxy(C 1 -C 6 )alkyl; or a pharmaceutically acceptable salt or solvate thereof. These compounds are useful for the treatment of disease conditions caused by overactivation of VR1 receptor such of pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.

  本发明提供了一种公式（I）的化合物：其中A和B分别独立表示CR12或N; D和E分别独立表示CR9或N; R1表示（C1-C6）烷基; R2表示氢，卤素，羟基，（C1-C6）烷基，卤代（C1-C6）烷基，羟基（C1-C6）烷基，（C1-C6）氧烷基或（C1-C6）氧烷基-（C1-C6）烷基; R3、R4、R5、R6、R10和R11分别独立表示氢，卤素，（C1-C6）烷基，卤代（C1-C6）烷基，（C1-C6）氧烷基，羟基（C1-C6）烷基或（C1-C6）氧烷基-（C1-C6）烷基; 或R3和R4与它们所附着的碳原子一起形成3-至7-成员的碳环或杂环，其中一个或两个非相邻的碳原子可以选择地被氧原子，硫原子或NH代替; R7和R9分别独立表示氢，卤素，（C1-C6）烷基，卤代（C1-C6）烷基，羟基（C1-C6）烷基，（C1-C6）氧烷基，羟基（C1-C6）氧烷基，（C1-C6）氧烷基-（C1-C6）烷基，（C1-C6）氧烷基-（C1-C6）氧烷基，（C1-C6）烷基硫，（C1-C6）烷基亚磺酰基，（C1-C6）烷基磺酰基，NH2，[(C1-C6)烷基] NH-，[(C1-C6)烷基] 2N-，H2N-（C1-C6）氧烷基，（C1-C6）烷基-NH-（C1-C6）氧烷基，[(C1-C6)烷基] 2N（C1-C6）氧烷基; H2N-（C1-C6）氧烷基-（C1-C6）烷基，（C1-C6）烷基-NH-（C1-C6）氧烷基-（C1-C6）烷基，[(C1-C6)烷基] 2N（C1-C6）氧烷基-（C1-C6）烷基或含有至少一个氮原子的5-或6-成员杂环，R8表示卤素，（C1-C6）烷基，卤代（C1-C6）烷基，羟基（C1-C6）烷基，（C1-C6）氧烷基，羟基（C1-C6）氧烷基，（C1-C8）氧烷基-（C1-C6）烷基，（C1-C6）氧烷基-（C1-C6）氧烷基，卤代（C1-C6）烷基磺酰基，卤代（C1-C6）烷基亚磺酰基，卤代（C1-C6）氧烷基，卤代（C1-C6）烷基硫，[(C1-C6)烷基] NH-或[(C1-C6)烷基] 2N-; 或者当E为CR9时，R7和R8与它们所附着的碳原子一起形成5-8成员的碳环或杂环，其中一个或两个非相邻的碳原子可以选择地被氧，硫，N或NH基团代替，其中碳环或杂环未被取代或被一个或多个取代基取代，每个取代基独立地选择自羟基，（C1-C6）烷基，（C1-C6）氧烷基和羟基（C1-C6）烷基; R12表示氢，卤素，（C1-C6）烷基或羟基（C1-C6）烷基; 或其药学上可接受的盐或溶剂。这些化合物对于治疗由VR1受体过度激活引起的疾病状况，如哺乳动物中的疼痛等非常有用。本发明还提供了包含上述化合物的药物组成物。
• SUBSTITUTED N-SULFONYLAMINOBENZYL-2-PHENOXY ACETAMIDE COMPOUNDS
  申请人：Pfizer, Inc.

  公开号：EP1824837B1

  公开（公告）日：2008-08-13