1,4-dihydroxy-5,6,7,8-tetrahydro-2-naphthaldehyde | 149492-69-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 英文名称: 1,4-dihydroxy-5,6,7,8-tetrahydro-2-naphthaldehyde
• 英文别名: 1,4-dihydroxy-5,6,7,8-tetrahydronaphthalene-2-carboxaldehyde；1,4-dihydroxy-5,6,7,8-tetrahydronaphthalene-2-carbaldehyde
• CAS: 149492-69-3
• 化学式: C₁₁H₁₂O₃
• 分子量: 192.214
• InChiKey: MDFDHPAVAYJTRG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  14
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  57.5
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-吲哚酮 、 1,4-dihydroxy-5,6,7,8-tetrahydro-2-naphthaldehyde 在 哌啶 作用下， 以 乙醇 为溶剂， 反应 3.0h， 生成 (E)-3-(1',4'-dihydroxy-5',6',7',8'-tetrahydronaphth-2'-yl)methylen-2-oxindole
  参考文献：
  名称：

  Buzzetti; Brasca; Crugnola, Il Farmaco, 1993, vol. 48, # 5, p. 615 - 636

  摘要：

  DOI：
• 作为产物：
  描述：

  1,4-萘醌 在 platinum(IV) oxide 氢气 、 四氯化钛 作用下， 以 二氯甲烷 、 溶剂黄146 为溶剂， 25.0 ℃ 、310.27 kPa 条件下， 反应 3.0h， 生成 1,4-dihydroxy-5,6,7,8-tetrahydro-2-naphthaldehyde
  参考文献：
  名称：

  Buzzetti, Franco; Pinciroli, Vittorio; Brasca, M. Gabriella, Gazzetta Chimica Italiana, 1995, vol. 125, # 2, p. 69 - 76

  摘要：

  DOI：

文献信息

• N-substituted .beta.-aryl- and .beta.-heteroaryl-.alpha.-cyanoacrylamide
  申请人：Pharmacia S.p.A.

  公开号：US05652250A1

  公开（公告）日：1997-07-29

  The present invention relates to new compounds of formula ##STR1## wherein A is a bicyclic ring chosen from naphthalene, tetrahydronaphthalene, quinoline, isoquinoline and indole. B is a R.sup.2 substituted benzene ring or an unsubstituted pyridine or thiophene ring; R is hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, nitro, cyano, carboxy or a group NR.sup.3 R.sup.4 wherein each of R.sup.3 and R.sup.4 is independently hydrogen or C.sub.1 -C.sub.6 alkyl; R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkanoyl; R.sup.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, nitro, cyano, carboxy, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkanoyloxy or a group NR.sup.3 R.sup.4 wherein R.sup.3 and R.sup.4 are as defined above; n is zero or an integer of 1 to 2; x is zero or an integer of 1 to 5; and the pharmaceutically acceptable salts thereof. The compounds of the invention are useful as tyrosine kinase inhibitors.

  本发明涉及公式##STR1##的新化合物，其中A是从萘、四氢萘、喹啉、异喹啉和吲哚中选择的双环环；B是R.sup.2取代的苯环或未取代的吡啶或噻吩环；R是氢、C.sub.1-C.sub.6烷基、卤素、硝基、氰基、羧基或基团NR.sup.3R.sup.4，其中R.sup.3和R.sup.4中的每一个独立地是氢或C.sub.1-C.sub.6烷基；R.sup.1是氢、C.sub.1-C.sub.6烷基或C.sub.1-C.sub.6烷酰基；R.sup.2是氢、C.sub.1-C.sub.6烷基、卤素、硝基、氰基、羧基、羟基、C.sub.1-C.sub.6烷氧基、C.sub.1-C.sub.6烷酰氧基或基团NR.sup.3R.sup.4，其中R.sup.3和R.sup.4如上定义；n为零或1至2的整数；x为零或1至5的整数；以及其药学上可接受的盐。本发明的化合物可用作酪氨酸激酶抑制剂。
• Arylidene-heterocyclic derivatives and process for their preparation
  申请人：Farmitalia Carlo Erba S.r.l.

  公开号：US05639884A1

  公开（公告）日：1997-06-17

  The invention relates to compounds of formula ##STR1## wherein Ar is mono- or bicyclic ring system chosen from benzene, naphthalene, tetrahydronaphthalene, quinoline and indole; Het is ##STR2## R is hydrogen, halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 acyloxy, cyano, nitro, amino or --COOR.sub.3 in which R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.1 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 acyloxy, cyano, nitro, amino or --COOR.sub.3 in which R.sub.3 is as defined above; R.sub.2 is hydrogen, halogen, hydroxy or C.sub.1 -C.sub.6 alkyl; and the pharmaceutically acceptable salts thereof, and wherein when at the same time the (Ar)R.sub.1 R.sub.2 group represents unsubstituted phenyl or 4-chloro-, 4-cyano-, 4-amino- or 3,4-dimethoxy-phenyl and Het is a 4-homophthalimide group, then R is other than hydrogen, which are useful as anti-proliferative agents.

  本发明涉及以下式的化合物：##STR1## 其中Ar是从苯、萘、四氢萘、喹啉和吲哚中选择的单环或双环环系统; Het是##STR2## R是氢、卤素、羟基、C.sub.1-C.sub.6烷氧基、C.sub.2-C.sub.6酰氧基、氰基、硝基、氨基或--COOR.sub.3，其中R.sub.3是氢或C.sub.1-C.sub.6烷基; R.sub.1是氢、羟基、C.sub.1-C.sub.6烷基、C.sub.1-C.sub.6烷氧基、C.sub.2-C.sub.6酰氧基、氰基、硝基、氨基或--COOR.sub.3，其中R.sub.3如上所定义; R.sub.2是氢、卤素、羟基或C.sub.1-C.sub.6烷基;以及其药学上可接受的盐，其中当（Ar）R.sub.1R.sub.2基同时表示未取代的苯基或4-氯、4-氰、4-氨基或3,4-二甲氧基苯基，而Het是4-同型邻二酰亚胺基团时，则R不是氢，这些化合物可用作抗增殖剂。
• Indolinone combinatorial libraries and related products and methods for the treatment of disease
  申请人：Tang Cho Peng

  公开号：US20050197382A1

  公开（公告）日：2005-09-08

  The present invention relates to organic molecules capable of modulating, regulating and/or inhibiting protein kinase signal transduction. Such compounds are useful for the treatment of diseases related to unregulated protein kinase signal transduction, including cell proliferative diseases such as cancer, atherosclerosis, arthritis and restenosis and metabolic diseases such as diabetes. The present invention features indolinone compounds that potently inhibit protein kinases and related products and methods. Inhibitors specific to the FLK protein kinase can be obtained by adding chemical substituents to the 3-[(indole-3-yl)methylene]-2-indolinone, in particular at the 1′ position of the indole ring. Indolinone compounds that specifically inhibit the FLK and platelet derived growth factor protein kinases can harbor a tetrahydroindole or cyclopentano-b-pyrrol moiety. Indolinone compounds that are modified with substituents, particularly at the 5 position of the oxindole ring, can effectively activate protein kinases. This invention also features novel hydrosoluble indolinone compounds that are tyrosine kinase inhibitors and related products and methods.

  本发明涉及有机分子，能够调节、调控和/或抑制蛋白激酶信号转导。这些化合物对于治疗与不受调节的蛋白激酶信号转导相关的疾病非常有用，包括细胞增殖性疾病，如癌症、动脉粥样硬化、关节炎、再狭窄和代谢性疾病，如糖尿病。本发明涉及具有强效抑制蛋白激酶和相关产品以及方法的吲哚酮化合物。特定于FLK蛋白激酶的抑制剂可以通过在吲哚环的1'位置添加化学取代基来获得3-[(吲哚-3-基)亚甲基]-2-吲哚酮。特异性抑制FLK和血小板衍生生长因子蛋白激酶的吲哚酮化合物可以具有四氢吲哚或环戊烯基-β-吡咯基。在氧吲哚环的5位取代基的修饰下，吲哚酮化合物可以有效激活蛋白激酶。本发明还涉及新型水溶性吲哚酮化合物，它们是酪氨酸激酶抑制剂和相关产品和方法。
• Arylidene-heterocyclic derivatives, process for their preparation and their use as tyrisine kinase inhibitors
  申请人：PHARMACIA S.p.A.

  公开号：EP0549348A1

  公开（公告）日：1993-06-30

  The invention relates to compounds of formula wherein Ar is mono-or bicyclic ring system chosen from benzene, naphthalene, tetrahydronaphthalene, quinoline and indole; Het is R is hydrogen, halogen, hydroxy, C₁-C₆ alkoxy, C₂-C₆ acyloxy, cyano, nitro, amino or -COOR₃ in which R₃ is hydrogen or C₁-C₆ alkyl; R₁ is hydrogen, hydroxy, C₁-C₆ alkyl, C₁-C₆ alkoxy, C₂-C₆ acyloxy, cyano, nitro, amino or -COOR₃ in which R₃ is as defined above; R₂ is hydrogen, halogen, hydroxy or C₁-C₆ alkyl; and the pharmaceutically acceptable salts thereof, and wherein when at the same time the (Ar) R₁ R₂ group represents unsubstituted phenyl or 4-chloro-, 4-cyano-, 4-amino- or 3,4-dimethoxy-phenyl and Het is a 4-homophthalimide group, then R is other than hydrogen, which are useful as anti-proliferative agents.

  本发明涉及式化合物 式中 Ar 是单环或双环系统，选自苯、萘、四氢萘、喹啉和吲哚； Het 是 R 是氢、卤素、羟基、C₁-C₆ 烷氧基、C₂-C₆酰氧基、氰基、硝基、氨基或 -COOR₃，其中 R₃ 是氢或 C₁-C₆ 烷基； R₁ 是氢、羟基、C₁-C₆ 烷基、C₁-C₆ 烷氧基、C₂-C₆ 酰氧基、氰基、硝基、氨基或 -COOR₃，其中 R₃ 如上定义； R₂是氢、卤素、羟基或 C₁-C₆烷基；以及它们的药学上可接受的盐，其中当（Ar）R₁ R₂基团同时代表未取代的苯基或 4-氯-、4-氰基-、4-氨基-或 3,4-二甲氧基-苯基且 Het 是 4-高邻苯二甲酰亚胺基团时，则 R 是氢以外的其它基团，它们可用作抗增殖剂。
• SUBSTITUTED BETA-ARYL AND BETA-HETEROARYL-ALPHA-CYANOACRYLAMIDE DERIVATIVES AS TYROSINE KINASE INHIBITORS
  申请人：PHARMACIA S.p.A.

  公开号：EP0700388A1

  公开（公告）日：1996-03-13