Methanesulfonamide,N,N'-(1R,2R)-1,2-cyclohexanediylbis[1,1,1-trifluoro-

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 有机磺酸及其衍生物
• 英文名称: Methanesulfonamide,N,N'-(1R,2R)-1,2-cyclohexanediylbis[1,1,1-trifluoro-
• 英文别名: 1,1,1-trifluoro-N-[2-(trifluoromethylsulfonylamino)cyclohexyl]methanesulfonamide
• 化学式: C₈H₁₂F₆N₂O₄S₂
• 分子量: 378.3
• InChiKey: GKSGSDYYIYURPD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  22
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  109
• 氢给体数：
  2
• 氢受体数：
  12

文献信息

• [EN] MERCAPTOIMIDAZOLES AS CCR2 RECEPTOR ANTAGONISTS<br/>[FR] MERCAPTOIMIDAZOLES SERVANT D'ANTAGONISTES DU RÉCEPTEUR CCR2
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2006015986A1

  公开（公告）日：2006-02-16

  The present invention relates to a compound of formula (I), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein R1 represents hydrogen, C1-6alkyl, C3-7cycloalkyl, C1-6alkyloxyC1-6alkyl, di(C1-6alkyl)amino C1-6alkyl, aryl or heteroaryl; each R2 independently represents halo, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, polyhalo C1-6alkyl, polyhalo C1-6alkyloxy, cyano, aminocarbonyl, amino, mono-or di(C1-4alkyl)amino, nitro, aryl or aryloxy; R3 represents cyano, C(=O)-O-R5, C(=O)-ΝR6aR6b or C(=O)-R7; or a cyclic ring system; R4 represents hydrogen or C1-6alkyl; n is 1, 2, 3, 4 or 5; R10 represents hydrogen, C1-6alkyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, arylcarbonyl, heteroarylcarbonyl, -C(=0)-NH-R5, -C(=S)-NH-R5 or -S(=O)2-R5. The invention also relates to processes for preparing the compounds of formula (I), their use as CCR2 antagonists and pharmaceutical compositions comprising them.

  本发明涉及一种式(I)的化合物，一种N-氧化物，一种药学上可接受的加合盐，一种季铵盐和其立体化学异构体形式，其中R1代表氢，C1-6烷基，C3-7环烷基，C1-6烷氧基C1-6烷基，二(C1-6烷基)氨基C1-6烷基，芳基或杂环芳基；每个R2独立地代表卤素，C1-6烷基，C1-6烷氧基，C1-6烷硫基，多卤素C1-6烷基，多卤素C1-6烷氧基，氰基，氨基甲酰基，氨基，单或双(C1-4烷基)氨基，硝基，芳基或芳氧基；R3代表氰基，C(=O)-O-R5，C(=O)-ΝR6aR6b或C(=O)-R7；或者是一个环状环系统；R4代表氢或C1-6烷基；n为1、2、3、4或5；R10代表氢，C1-6烷基，C1-6烷基羰基，C1-6烷氧羰基，芳基羰基，杂环芳基羰基，-C(=0)-NH-R5，-C(=S)-NH-R5或-S(=O)2-R5。该发明还涉及制备式(I)化合物的方法，它们作为CCR2拮抗剂的用途以及包含它们的药物组合物。
• [EN] MERCAPTOIMIDAZOLES AS CCR2 RECEPTOR ANTAGONISTS<br/>[FR] MERCAPTOIMIDAZOLES EN TANT QU'AGONISTES DU RECEPTEUR CCR2
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2004069809A1

  公开（公告）日：2004-08-19

  The present invention relates to a compound of formula (I),a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein R1 is hydrogen, C1-6alkyl, C3-7cycloalkyl, aryl or heteroaryl; R2 is halo, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, cyano, aminocarbonyl, amino, mono-or di(C1-4alkyl)amino, nitro, aryl or aryloxy; R3 is hydrogen, cyano, C1-6alkyl optionally substituted with hydroxy, C(=O)-O-R5, C(=O)-NR6aR6b, S(=O)2-NR6aR6b, C(=O)-R7; R4 is hydrogen, cyano, C1-6alkyl optionally substituted with hydroxy, C(=O)-O-R5, C(=O)-NR6aR6b, S(=O)2-NR6aR6b, C(=O)-R7; n is 1, 2, 3, 4 or 5;provided that at least one of R3 or R4 is other than hydrogen; and that if R3 represents C(=O)-OH, C(=O)-O-C1-6alkyl or C(=O)-O-C2-6alkenyl, then R4 is other than hydrogen; and that if R3 represents CH2OH and R1 represents hydrogen, then R4 is other than hydrogen; and that if R3 represents C(=O)-NH-C1-4alkyl-NH2 and R1 represents hydrogen, then R4 is other than hydrogen; and that if R3 represents formula (II) and R1 represents hydrogen, then R4 is other than hydrogen; having CCR2 receptor antagonistic properties. The invention also relates to processes for preparing the compounds of formula (I) and pharmaceutical compositions comprising them.

  本发明涉及一种式(I)的化合物，一种N-氧化物，一种药学上可接受的加合盐，一种季铵盐及其立体化异构体，其中R1是氢，C1-6烷基，C3-7环烷基，芳基或杂环芳基；R2是卤素，C1-6烷基，C1-6烷氧基，C1-6烷硫基，多卤代C1-6烷基，多卤代C1-6烷氧基，氰基，氨基甲酰基，氨基，单或双(C1-4烷基)氨基，硝基，芳基或芳氧基；R3是氢，氰基，C1-6烷基，可选择地取代羟基的C(=O)-O-R5，C(=O)-NR6aR6b，S(=O)2-NR6aR6b，C(=O)-R7；R4是氢，氰基，C1-6烷基，可选择地取代羟基的C(=O)-O-R5，C(=O)-NR6aR6b，S(=O)2-NR6aR6b，C(=O)-R7；n为1、2、3、4或5；但要求R3或R4至少有一个不是氢；如果R3代表C(=O)-OH，C(=O)-O-C1-6烷基或C(=O)-O-C2-6烯基，则R4不是氢；如果R3代表CH2OH且R1代表氢，则R4不是氢；如果R3代表C(=O)-NH-C1-4烷基-NH2且R1代表氢，则R4不是氢；如果R3代表式(II)且R1代表氢，则R4不是氢；具有CCR2受体拮抗性质。该发明还涉及制备式(I)化合物的方法和包含其的药物组合物。
• NOVEL CATALYTIC SYSTEMS FOR THE RING-OPENING (CO)POLYMERIZATION OF LACTONES
  申请人：Bourissou Didier

  公开号：US20110054144A1

  公开（公告）日：2011-03-03

  The present invention relates to the use of a system composed of a base and of a sulphonamide, as a catalyst for the ring-opening (co)polymerization of lactones. The present invention also relates to novel sulphonamides and to a process for the ring-opening (co)polymerization of lactones comprising the use of sulphonamides in combination with a base as a catalytic system.

  本发明涉及使用由基础和磺酰胺组成的系统作为内酯的环开启（共）聚合催化剂。本发明还涉及新型磺酰胺和一种内酯的环开启（共）聚合过程，该过程包括使用磺酰胺与碱一起作为催化系统。
• Gas sensors
  申请人：——

  公开号：US20040026246A1

  公开（公告）日：2004-02-12

  This invention provides an assembly comprising a sensing electrode and a counter electrode in contact with a membrane body formed from a solid polymer electrolyte system comprising a fluorinated polymer matrix and a charge carrying component which is dispersed in the matrix the electrodes and membrane being housed in a housing having a gas diffusion barrier through which gas may flow. The charge carrying components are fluorinated organic proton conductors (such as heptadecafluorooctane sulphonic acid, bis-trifluoromethane sulphonamide, N-(2,6-diethylphenyl)-1,1,1-trifluoromethane sulphonamide, N-benzyltrifluoromethane sulphonamide and N, N-1,2-cyclohexanediylbis (1,1,1-trifluoromethane sulphonamide)). The polymer matrix is a homopolymer or copolymer of vinylidene fluoride preferably with fluorinated comonomers. The solid polymer electrolyte system preferably contains plasticising additive(s) and is cast as a coating onto one or more electrodes eg. Platinum gas diffusion electrodes forming an assembly for use in a gas sensor especially a CO sensor.

  本发明提供了一种组件，包括一个感应电极和一个对电极，感应电极和对电极与由固体聚合物电解质系统形成的膜体接触，固体聚合物电解质系统包括含氟聚合物基质和分散在基质中的电荷携带成分，电极和膜体被放置在一个具有气体扩散屏障的壳体中，气体可以从气体扩散屏障中流过。电荷携带成分是氟化有机质子导体（如十七氟辛烷磺酸、双三氟甲烷磺酰胺、N-（2,6-二乙基苯基）-1,1,1-三氟甲烷磺酰胺、N-苄基三氟甲烷磺酰胺和 N,N-1,2-环己烷二基双（1,1,1-三氟甲烷磺酰胺））。聚合物基体最好是偏氟乙烯与含氟共聚单体的均聚物或共聚物。固体聚合物电解质系统最好含有增塑添加剂，并作为涂层浇铸到一个或多个电极上，如铂气体扩散电极，形成一个用于气体传感器（尤其是一氧化碳传感器）的组件。
• Mercaptoimidazoles as ccr2 receptor antagonists
  申请人：Van Lommen Rosalia Eugeen Guy

  公开号：US20060058289A1

  公开（公告）日：2006-03-16

  The present invention relates to a compound of formula (I) having CCR2 receptor antagonistic properties, particularly anti-infflammatory properties.

  本发明涉及一种具有 CCR2 受体拮抗特性，特别是抗炎特性的式 (I) 化合物。