4-oxo-2-phenyl-4H-chromene-8-carboxylic acid | 6587-14-0

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 黄酮类化合物
• 英文名称: 4-oxo-2-phenyl-4H-chromene-8-carboxylic acid
• 英文别名: 4-oxo-2-phenyl-4H-1-benzopyran-8-carboxylic acid；flavone 8-carboxylic acid；flavone-8-carboxylic acid；Flavon-8-carbonsaeure；4h-1-Benzopyran-8-carboxylic acid,4-oxo-2-phenyl-；4-oxo-2-phenylchromene-8-carboxylic acid
• CAS: 6587-14-0
• 化学式: C₁₆H₁₀O₄
• 分子量: 266.253
• InChiKey: LRTSDXDGOFQRSW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  20
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  63.6
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  4-oxo-2-phenyl-4H-chromene-8-carboxylic acid 、 氰基磷酸二乙酯 、 sodium carbonate 、 1-(3-氨基)-4-(2-甲氧基苯基)哌嗪 在 甲烷磺酸 、 三乙胺 作用下， 以 N-甲基乙酰胺 、 二氯甲烷 、 丙酮 为溶剂， 生成 Rec 15/2843
  参考文献：
  名称：

  Bicyclic heterocyclic derivatives having .alpha..sub.1 -adrenergic and

  摘要：

  本发明提供了双环杂环衍生物及其药学上可接受的盐，用于治疗高血压、尿道和下泌尿道收缩以及其他疾病。这些化合物还可用于体内或体外结合α1-肾上腺素能和5HT1A-5-羟色胺能受体。

  公开号：

  US05474994A1

文献信息

• [EN] FLAVAXATE DERIVATIVES AS MUSCARINIC RECEPTOR ANTAGONISTS<br/>[FR] DERIVES DE FLAVAXATE COMME ANTAGONISTES DE RECEPTEURS MUSCARINIQUES
  申请人：RANBAXY LAB LTD

  公开号：WO2004056811A1

  公开（公告）日：2004-07-08

  This invention generally relates to the derivatives of3.6-disubstituted azabicyclo [3.1.0] hexanes of the following formula [IA]. The compounds of this invention can function as muscarinic receptor antagonists, and can be used for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to a process for the preparation of the compounds of the present invention, pharmaceutical compositions containing the compounds of the present invention and the :h1ethods for treating the diseases mediated through muscarinic receptors.

  本发明通常涉及以下式[IA]的3.6-二取代的氮杂双环[3.1.0]己烷的衍生物。本发明的化合物可以作为毒蕈碱受体拮抗剂，可用于治疗通过毒蕈碱受体介导的呼吸系统、泌尿系统和胃肠道系统的各种疾病。本发明还涉及制备本发明化合物的方法、含有本发明化合物的药物组合物以及治疗通过毒蕈碱受体介导的疾病的方法。
• Certain isoquinoline derivatives having anti-tumor properties
  申请人：Laboratoires Glaxo SA

  公开号：US05663179A1

  公开（公告）日：1997-09-02

  Compounds are described of general formula (I) ##STR1## and salts and solvates thereof, including physiologically acceptable salts and solvates thereof, in which: Z represents either Het, ##STR2## Het represents an optionally substituted bicyclic or tricyclic ring selected from acricine isoquinolin-1-yl, isoquinolin-3-yl, The novel compounds of formula (I) can sensitize multi-drug resistant cancer cells to chemotherapeutic agents and may be formulated for use in therapy, particularly to improve or increase the efficacy of an anti-tumour drug.

  化合物的一般式(I)描述如下：##STR1##及其盐和溶剂化物，包括生理上可接受的盐和溶剂化物，其中：Z代表Het或##STR2## Het代表可选取自acricine isoquinolin-1-yl、isoquinolin-3-yl的含取代的双环或三环环状结构。式(I)的新型化合物能够增强多药耐药癌细胞对化疗药物的敏感性，并可制成治疗用药物，特别是为了改善或增强抗肿瘤药物的功效。
• N-substituted flavone-8-carboxamides
  申请人：Hokuriku Pharmaceutical Co.,Ltd

  公开号：EP0108986A1

  公开（公告）日：1984-05-23

  Derivatives of N-substituted flavone-8-carboxamides represented by general formula (I) wherein R, represents a hydrogen atom, a methyl group or an ethyl group, R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxyl group, a halogen atom or a nitro group, R3 represents a hydrogen atom or a lower alkyl group, k represents 0, 1, 2, or 3, m represents 0 or 1, X and Y, which must be different, represents a hydrogen atom or a methyl group, A represents an amino group having the wherein, R4 and R5, which may be the same or different, represent a lower alkyl group or a cyclic amino group together with the nitrogen atom and with or without an oxygen atom, R6 represents a lower alkyl group and n represents 2 or 3, are disclosed as well as pharmaceutical compositions thereof and method of treating therewith. The N-substituted flavone-8-carboxamides derivatives are useful as agents for treatment of dysurea.

  通式(I)代表的N-取代黄酮-8-羧酰胺的衍生物 其中，R 代表氢原子、甲基或乙基；R2 代表氢原子、低级烷基、低级烷氧基、卤素原子或硝基；R3 代表氢原子或低级烷基；k 代表 0、1、2 或 3；m 代表 0 或 1；X 和 Y（必须不同）代表氢原子或甲基；A 代表具有以下性质的氨基：(1)、(2)、(3)或(4)；(5)、(6)或(7)；(8)、(9)、(10)或(11)。 其中，R4 和 R5（可以相同或不同）代表低级烷基或环状氨基，与氮原子一起，有或没有氧原子，R6 代表低级烷基，n 代表 2 或 3，本发明公开了这些化合物及其药物组合物和处理方法。 N-取代的黄酮-8-羧酰胺衍生物可作为治疗尿失禁的药物。
• Heterobicyclic compounds as antagogists of alpha-1 adrenergic and SHT1A receptors
  申请人：RECORDATI S.A. CHEMICAL and PHARMACEUTICAL COMPANY

  公开号：EP0558245A1

  公开（公告）日：1993-09-01

  There are disclosed compounds of the general formula The heteroatom X is preferably oxygen, but may have other values. The group W is preferably a carbonyl group, but may have other values. The preferred heterocyclic ring is thus a 4-oxo-4H-1-benzopyran ring. This may have a wide range of R₂, R₃, R₆ and R₇ substituents. Y is a linking group, chosen from a wide range, but including -COO- , -CONH- , -O- , -SO₂- and -SO₂NH-. Z is an alkylene chain, and B is a complex amine. These compounds and their prodrugs, enantiomers, diastereoisomers, N-oxides and pharmaceutically acceptable salts are useful for the treatment of hypertension and urinary tract troubles associated with benign prostatic hypertrophy, and for the treatment of other diseases.

  已公开的化合物通式如下 杂原子 X 最好是氧，但也可以有其他值。基团 W 最好是羰基，但也可以有其他值。因此，优选的杂环是 4-氧代-4H-1-苯并吡喃环。它可以有多种 R₂、R₃、R₆ 和 R₇ 取代基。Y 是连接基团，可选范围很广，但包括-COO-、-CONH-、-O-、-SO₂- 和-SO₂NH-。Z 是亚烷基链，B 是复合胺。这些化合物及其原药、对映体、非对映异构体、N-氧化物和药学上可接受的盐类可用于治疗与良性前列腺肥大相关的高血压和尿路问题，也可用于治疗其他疾病。
• Use of flavone 8-acetic acid in vascular and cardiovascular interventions and acute coronary syndromes
  申请人：——

  公开号：US20010041687A1

  公开（公告）日：2001-11-15

  A method for treatment of a vascular or cardiovascular condition or acute coronary syndromes comprises administering an effective amount of a flavone 8-carboxylic acid to a mammal suffering from a vascular or cardiovascular condition or acute coronary syndromes. The flavone 8-carboxylic acid is typically flavone 8-acetic acid. The flavone 8-carboxylic acid can be administered alone or in combination with another agent such as a thrombolytic agent, an antithrombotic agent, an anticoagulant, or an antiplatelet agent. The invention also includes pharmaceutical compositions formulated for the treatment of a vascular or cardiovascular condition or acute coronary syndromes.

  一种治疗血管或心血管疾病或急性冠状动脉综合征的方法包括向患有血管或心血管疾病或急性冠状动脉综合征的哺乳动物施用有效量的黄酮-8-羧酸。黄酮-8-羧酸通常是黄酮-8-乙酸。黄酮-8-羧酸可单独给药，也可与另一种药剂如溶栓药、抗血栓药、抗凝药或抗血小板药联合给药。本发明还包括用于治疗血管或心血管疾病或急性冠状动脉综合征的药物组合物。