N-(6-methoxy-1,3-benzothiazol-2-yl)naphthalene-2-carboxamide

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: N-(6-methoxy-1,3-benzothiazol-2-yl)naphthalene-2-carboxamide
• 化学式: C₁₉H₁₄N₂O₂S
• 分子量: 334.4
• InChiKey: PFTSDFZZUYZYAD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.8
• 重原子数：
  24
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.05
• 拓扑面积：
  79.5
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• Use of phenethyl acrylamides, novel phenethyl acrylamides, method for the production thereof and agents containing the same
  申请人：——

  公开号：US20030191190A1

  公开（公告）日：2003-10-09

  The invention relates to the use of phenethyl acrylamides of formula I for controlling phytopathogenic fungi, wherein the substituents of said phenethyl acrylamides have the following significations: X signifies halogen, alkyl, halogenalkyl, alkoxy halogenalkoxy and —O—C(R a , R b )—C≡C—R 6 ; R a , R b and R c have the signification given in the description; m, n independently signify 1 to 4, the radicals X or Y being potentially different if m or n is higher than 1; Y signifies halogen, nitro, cyano, alkyl, CF 3 , alkoxy and phenyl; R 1 , R 2 independently signify hydrogen, halogen, alkyl, alkoxy, halogenalkoxy and CF 3 ; R 3 , R 4 , R 5 , and R 6 independently signify hydrogen, alkyl and alkoxy, or R 3 and R 4 together form a cyclopropyl ring, whereby the C—R 5 and C—R 6 bonds can be in position E or Z in relation to each other. The invention also relates to novel phenethyl acrylamides, a method for the productio thereof, and agents containing the same.

  该发明涉及使用式I的苯乙基丙烯酰胺来控制植物病原真菌，其中所述苯乙基丙烯酰胺的取代基具有以下含义：X表示卤素、烷基、卤代烷基、烷氧基、卤代烷氧基和—O—C(Ra，Rb)—C≡C—R6；Ra，Rb和Rc在描述中给出了相应的含义；m，n独立地表示1到4，如果m或n大于1，则基团X或Y可能不同；Y表示卤素、硝基、氰基、烷基、三氟甲基、烷氧基和苯基；R1，R2独立地表示氢、卤素、烷基、烷氧基、卤代烷氧基和三氟甲基；R3，R4，R5和R6独立地表示氢、烷基和烷氧基，或者R3和R4一起形成环丙基环，其中C—R5和C—R6键可以在彼此之间的位置E或Z。该发明还涉及新型苯乙基丙烯酰胺、其生产方法以及含有该化合物的制剂。
• [EN] BENZOTHIAZOLE AND THIAZOLE'5,5-B!PYRIDINE COMPOSITIONS AND THEIR USE AS UBIQUITIN LIGASE INHIBITORS<br/>[FR] COMPOSITIONS DE BENZOTHIAZOLE ET DE THIAZOLE'5,5-B!PYRIDINE ET LEUR UTILISATION COMME INHIBITEURS DE L'UBIQUITINE LIGASE
  申请人：RIGEL PHARMACEUTICALS INC

  公开号：WO2005037845A1

  公开（公告）日：2005-04-28

  This invention describes compounds and pharmaceutical compositions useful as ubiquitin agent inhibitors. The compounds and pharmaceutical compositions of the invention are useful as inhibitors of the biochemical pathways of organisms in which ubiquitination is involved. The invention also comprises the use of the compounds and pharmaceutical compositions of the invention for the treatment of conditions that require inhibition of ubiquitination. Furthermore, the invention comprises methods of inhibiting ubiquitination in a cell comprising contacting a cell in which inhibition of ubiquitination is desired with a pharmaceutical composition according to the invention.

  这项发明描述了化合物和制药组合物，作为泛素代理抑制剂。该发明的化合物和制药组合物作为抑制泛素化参与的生物化学途径的抑制剂是有用的。该发明还包括使用该发明的化合物和制药组合物治疗需要抑制泛素化的情况。此外，该发明还包括通过使用该发明的制药组合物接触需要抑制泛素化的细胞来抑制细胞内泛素化的方法。
• Benzothiazole compositions and their use as ubiquitin ligase inhibitors
  申请人：Ramesh V. Usha

  公开号：US20050130974A1

  公开（公告）日：2005-06-16

  This invention describes compounds and pharmaceutical compositions useful as ubiquitin agent inhibitors. The compounds and pharmaceutical compositions of the invention are useful as inhibitors of the biochemical pathways of organisms in which ubiquitination is involved. The invention also comprises the use of the compounds and pharmaceutical compositions of the invention for the treatment of conditions that require inhibition of ubiquitination. Furthermore, the invention comprises methods of inhibiting ubiquitination in a cell comprising contacting a cell in which inhibition of ubiquitination is desired with a pharmaceutical composition according to the invention.

  本发明描述了化合物和药物组合物，可用作泛素代理抑制剂。本发明的化合物和药物组合物可用作生物体中涉及泛素化的生化途径的抑制剂。本发明还包括使用本发明的化合物和药物组合物治疗需要抑制泛素化的疾病的方法。此外，本发明还包括通过将本发明的药物组合物接触到需要抑制泛素化的细胞中来抑制细胞泛素化的方法。
• Salicylohydrazide derivatives, processes and intermediates for their preparation, compositions comprising them, and their use
  申请人：——

  公开号：US20020019374A1

  公开（公告）日：2002-02-14

  Salicylohydrazide derivatives of the formula I 1 in which the index and the substituents have the following meanings: X is halogen, NO 2 , cyano, alkyl or alkoxy; m is 0, 1, 2 or 3, it being possible for the substituents X to differ from each other if n is greater than 1; R 1 is NO 2 , NH 2 or NH—CO—A; A is hydrogen, alkyl, alkoxy, NH 2 , NHCH 3 or N(CH 3 ) 2 ; R 2 is hydrogen, cyano, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy or alkylthio; it being possible for the hydrocarbon radicals to be unsubstituted or substituted, R 3 is phenyl, naphthyl, cycloalkyl, 5-membered or 6-membered hetaryl or 5-membered or 6-membered heterocyclyl containing one to three N atoms and/or one O or S atom or one or two O and/or S atoms, the ring systems being unsubstituted or substituted; the preparation of these compounds, compositions comprising them, and their use for controlling harmful fungi.

  化合物I1的苯甲酰肼衍生物，其中指数和取代基具有以下含义：X为卤素，NO2，氰基，烷基或烷氧基；m为0，1，2或3，如果n大于1，则取代基X可以不同；R1为 ，NH2或NH-CO-A；A为氢，烷基，烷氧基，NH2，NH 或N(CH3)2；R2为氢，氰基，烷基，烯基，炔基，卤代烷基，烷氧基或烷硫基；碳氢基团可以是未取代或取代的；R3为苯基，萘基，环戊基，含有1至3个N原子和/或1个O或S原子或1或2个O和/或S原子的5元或6元杂环基或5元或6元杂环基，其环系统可以是未取代或取代的；这些化合物的制备，包括它们的组合物，以及它们用于控制有害真菌的用途。
• Phenethylacrylamide, methods for the production thereof and agents containing the same
  申请人：Grammenos Wassilios

  公开号：US20050181948A1

  公开（公告）日：2005-08-18

  The present invention relates to novel phenethylacrylamides of the formula I in which the substituents R 1 , R 2 , R 3 and R 4 have the following meanings: R 1 is hydrogen, halogen, C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy, C 3 -C 8 -cycloalkyl, C 1 -C 4 -haloalkoxy or C 1 -C 4 -haloalkyl; R 2 is hydrogen, halogen, C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy, C 3 -C 10 -cycloalkyl, C 1 -C 4 -haloalkoxy or C 1 -C 4 -haloalkyl; R 3 is C 1 -C 4 -alkyl, C 1 -C 4 -haloalkyl, propargyl, C 3 -C 4 -alkenyl or a radical of the formula —H 2 C—C≡C—C(R a , R a )—R c , wherein R a , R b independently of one another are hydrogen or methyl and R c is hydrogen or C 1 -C 4 -alkyl; R 4 is methyl or C 1 -haloalkyl; and Het is a 5- or 6-membered heteroaromatic ring, to processes for their preparation, and to the use of phenethylacrylamides of the formula I for controlling phytopathogenic harmful fungi.

  本发明涉及公式I的新型苯乙基丙烯酰胺，其中取代基R1、R2、R3和R4的含义如下：R1为氢、卤素、C1-C4烷基、C1-C4烷氧基、C3-C8环烷基、C1-C4卤代烷氧基或C1-C4卤代烷基；R2为氢、卤素、C1-C4烷基、C1-C4烷氧基、C3-C10环烷基、C1-C4卤代烷氧基或C1-C4卤代烷基；R3为C1-C4烷基、C1-C4卤代烷基、丙炔基、C3-C4烯基或式—H2C—C≡C—C(Ra, Ra)—Rc的基团，其中Ra、Rb各自独立地为氢或甲基，Rc为氢或C1-C4烷基；R4为甲基或C1卤代烷基；Het为5-或6-成员的杂芳环，本发明还涉及制备这些苯乙基丙烯酰胺的过程，以及利用公式I的苯乙基丙烯酰胺控制植物病原真菌的用途。