(2-chloro-4-methyl-3-quinolinyl)methanol | 209909-11-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: (2-chloro-4-methyl-3-quinolinyl)methanol
• 英文别名: 2-chloro-4-methyl-3-quinolinemethanol；(2-Chloro-4-methylquinolin-3-yl)methanol
• CAS: 209909-11-5
• 化学式: C₁₁H₁₀ClNO
• 分子量: 207.659
• InChiKey: GNRUWYXCBKXDAQ-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：
  0.18
• 拓扑面积：
  33.1
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (2-chloro-4-methyl-3-quinolinyl)methanol 、 (+)-5-ethyl-5-hydroxy-1,3,4,5,8,9-hexahydrooxepino[3,4-c]pyridin-3,9-dione 生成 5-ethyl-5-hydroxy-12-methyl-1,4,5,13-tetrahydro-3H,15H-oxepino[3',4':6,7]-indolizino[1,2-b]quinoline-3,15-dione
  参考文献：
  名称：

  Comptothecin analogues, preparation methods therefor, use thereof as drugs, and pharmaceutical compositions containing said analogues

  摘要：

  该化合物的结构如下所示，其中取代基的定义如规范中所述，以及其无毒、药用可接受的盐，可用于治疗病毒感染、寄生虫病和癌症的治疗。

  公开号：

  US06339091B1
• 作为产物：
  描述：

  邻氨基苯乙酮 生成 (2-chloro-4-methyl-3-quinolinyl)methanol
  参考文献：
  名称：

  Analogues of camptothecin, their use as medicaments and the pharmaceutical compositions containing them

  摘要：

  该化合物的化学式，其中取代基的定义如规范中所述，这些化合物在癌症治疗中很有用。

  公开号：

  US06815546B2

文献信息

• New analogues of camptothecin, their use as medicaments and the pharmaceutical compositions containing them
  申请人：——

  公开号：US20030004150A1

  公开（公告）日：2003-01-02

  A compound of the formula 1 wherein the substituents are defined as in the specification which compounds are useful in the treatment of cancer.

  其中取代基如规范中所定义的化合物的化学式，这些化合物在癌症治疗中很有用。
• New tetracyclic analogues of camptothecins, their preparation processes, their use as medicaments and the pharmaceutical compositions containing them
  申请人：——

  公开号：US20010000521A1

  公开（公告）日：2001-04-26

  The invention relates to new tetracyclic analogues of camptothecin, their preparation processes, their use as medicaments and the pharmaceutical compositions containing them. Said analogues, which include in particular 3-hydroxy-3-(4-oxo-4,6-dihydroindolizino [1,2-b] quinoline-2-yl)pentanoic acid, have a powerful biological activity inhibiting topoisomerase I and/or topoisomerase II.

  本发明涉及新的四环类拓扑异构酶抑制剂喜树碱类似物，其制备方法，其作为药物的使用以及含有它们的制药组合物。这些类似物，尤其包括3-羟基-3-（4-氧代-4,6-二氢吲哚并［1,2-b］喹啉-2-基）戊酸，具有强大的生物活性，能够抑制拓扑异构酶I和/或拓扑异构酶II。
• [EN] NOVEL CAMPTOTHECIN ANALOGUES, PREPARATION METHODS THEREFOR, USE THEREOF AS DRUGS, AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAID ANALOGUES<br/>[FR] NOUVEAUX ANALOGUES DE LA CAMPTOTHECINE, DES PROCEDES DE PREPARATION, LEUR APPLICATION COMME MEDICAMENTS ET LES COMPOSITIONS PHARMACEUTIQUES LES CONTENANT
  申请人：SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES (SCRAS)

  公开号：WO1997000876A1

  公开（公告）日：1997-01-09

  (EN) A camptothecin analogue characterised in that the hydroxy lactone of the camptothecin is a $g(b)-hydroxy lactone or the corresponding $g(b)-hydroxyacid, resulting from the opening of said lactone, or a derivative of said $g(b)-hydroxyacid, or a pharmaceutically acceptable salt thereof, is disclosed. In particular, compounds of formulae (I) and (II) are disclosed. Methods for preparing the compounds of formulae (I) and (II), pharmaceutical compositions containing said compounds, and their use, particularly as topoisomerase inhibitors and antitumoral drugs, are also disclosed.(FR) L'invention concerne un analogue de la camptothécine, caractérisé en ce que l'hydroxy lactone de la camptothécine est une $g(b)-hydroxy lactone ou le $g(b)-hydroxy acide correspondant, résultant de l'ouverture de cette lactone, ou un dérivé de ce $g(b)-hydroxy acide, ou un sel pharmaceutiquement acceptable de ces derniers, et en particulier des composés de formule générale (I) et (II). L'invention concerne également des procédés de préparation des composés de formule (I) et (II) ci-dessus, des compositions pharmaceutiques les contenant et leur utilisation notamment en tant qu'inhibiteurs de topoisomérase et anti-tumoraux.

  一种卡铂替吉诺类似物，其特征在于卡铂替吉诺的羟基内酯是$g(b)-羟基内酯或由该内酯开环所得的相应$g(b)-羟基酸，或该$g(b)-羟基酸的衍生物，或其药学上可接受的盐。具体地，揭示了式（I）和式（II）的化合物。还揭示了制备式（I）和式（II）化合物的方法，包含该化合物的制药组合物以及它们的用途，特别是作为拓扑异构酶抑制剂和抗肿瘤药物。
• [EN] PRO-DRUGS AND COUNTERPARTS OF CAMPTOTHECIN, THEIR APPLICATION AS MEDICINES<br/>[FR] FORMES PRODROGUES ET ANALOGUES DE LA CAMPTOTHECINE, LEUR APPLICATION COMME MEDICAMENTS
  申请人：SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATIONS SCIENTIFIQUES (S.C.R.A.S.)

  公开号：WO1998028304A1

  公开（公告）日：1998-07-02

  (EN) The invention concerns novel counterparts of camptothecin and in particular products complying with the following formulae: 8-ethyl-8,9-dihydro-8-hydroxy-1-benzyl-2$i(H),10$i(H),12$i(H-)[1,3]oxazino[5,6-$i(f)]oxepino[3',4':6,7]indolizino[1,2-$i(b)]quinolein-10,13(15$i(H))-dione; 5-ethyl-9,10-difluoro-4,5-dihydro-5-(2-amino-1-oxoethoxy)-1$i(H)-oxepino[3',4':6,7]indolizino[1,2-$i(b)]quinolein-3,15(4$i(H),13$i(H))-dione; 5-ethyl-9,10-difluoro-4,5-dihydro-5-(2-amino-1-oxopropoxy)-1$i(H)-oxepino[3',4':6,7]indolizino[1,2-$i(b)]quinolein-3,15(4$i(H),13$i(H))-dione. The invention also concerns their method of preparation, their application as medicines, the pharmaceutical compositions containing them and their use in producing tumoricidal, antiviral and parasiticide medicines.(FR) L'invention concerne de nouveaux analogues de la camptothécine et en particulier les produits répondant aux formules suivantes: 8-éthyl-8,9-dihydro-8-hydroxy-1-benzyl-2$i(H), 10$i(H), 12$i(H)-[1,3]oxazino[5,6-$i(f)]oxépino[3',4':6,7]indolizino[1,2-$i(b)]quinoléine-10,13(15$i(H))-dione; 5-éthyl-9,10-difluoro-4,5-dihydro-5-(2-amino-1-oxoéthoxy)-1$i(H)-oxépino[3',4':6,7]indolizino[1,2-$i(b)]quinoléine-3,15(4$i(H),13$i(H))-dione; 5-éthyl-9,10-difluoro-4,5-dihydro-5-(2-amino-1-oxopropoxy)-1$i(H)-oxépino[3',4':6,7]indolizino[1,2-$i(b)]quinoléine-3,15(4$i(H),13$i(H))-dione; leur procédé de préparation, leur application comme médicaments, les compositions pharmaceutiques les renfermant et leur utilisation pour la réalisation de médicaments antitumoraux, antiviraux ou antiparasitaires.

  本发明涉及新型的喜树碱衍生物，特别是符合以下化学式的产品：8-乙基-8,9-二氢-8-羟基-1-苄基-2$i(H),10$i(H),12$i(H)-[1,3]噁唑[5,6-$i(f)]氧杂环[3',4':6,7]吲哚并[1,2-$i(b)]喹啉-10,13(15$i(H))-二酮；5-乙基-9,10-二氟-4,5-二氢-5-(2-氨基-1-氧乙氧基)-1$i(H)-氧杂环[3',4':6,7]吲哚并[1,2-$i(b)]喹啉-3,15(4$i(H),13$i(H))-二酮；5-乙基-9,10-二氟-4,5-二氢-5-(2-氨基-1-氧丙氧基)-1$i(H)-氧杂环[3',4':6,7]吲哚并[1,2-$i(b)]喹啉-3,15(4$i(H),13$i(H))-二酮。本发明还涉及它们的制备方法，作为药物的应用，含有它们的制药组合物以及用于生产抗肿瘤、抗病毒和杀虫药物的用途。
• Camptothecin tetracyclic analogues, preparation, method, applications as medicines and pharmaceutical compositions containing them
  申请人：Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)

  公开号：US06436951B1

  公开（公告）日：2002-08-20

  The invention relates to new tetracyclic analogues of camptothecin, their preparation processes, their use as medicaments and the pharmaceutical compositions containing them. Said analogues, which include in particular 3-hydroxy-3-(4-oxo-4,6-dihydroindolizino [1,2-b] quinoline-2-yl)pentanoic acid, have a powerful biological activity inhibiting topoisomerase I and/or topoisomerase II.

  本发明涉及卡培托普汀的新四环类似物、其制备过程、其作为药物的用途以及含有它们的制药组合物。这些类似物，尤其包括3-羟基-3-(4-氧代-4,6-二氢吲哚并[1,2-b]喹啉-2-基)戊酸，具有强大的生物活性，能够抑制拓扑异构酶I和/或拓扑异构酶II。