Unii-TT7PL9xfe2 | 192868-49-8

• 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: Unii-TT7PL9xfe2
• 英文别名: [4-[4-amino-5-(4-fluorophenyl)-6,7-dimethoxyquinolin-2-yl]-1,4-diazepan-1-yl]-morpholin-4-ylmethanone
• CAS: 192868-49-8
• 化学式: C₂₇H₃₂FN₅O₄
• 分子量: 509.6
• InChiKey: IHSGHTLNHSMKII-UHFFFAOYSA-N

物化性质

• 沸点：
  678.5±55.0 °C(Predicted)
• 密度：
  1.295±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  37
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  93.4
• 氢给体数：
  1
• 氢受体数：
  8

文献信息

• Quinoline and quinazoline compounds useful in therapy
  申请人：Pfizer Inc.

  公开号：US20030220332A1

  公开（公告）日：2003-11-27

  The invention provides compounds of formula (I), 1 wherein R 1 represents C 1-4 alkoxy optionally substituted by one or more fluorine atoms; R 2 represents H or C 1-6 alkoxy optionally substituted by one or more fluorine atoms; R 3 represents one or more groups independently selected from H, halogen, C 1-4 alkoxy and CF 3 ; in addition, R 2 and one R 3 group may together represent —OCH 2 —, the methylene group being attached to the ortho-position of the pendant phenyl ring; R 4 represents a 4-, 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent or represents a cyclic group or an open chain group; and the pharmaceutically acceptable salts thereof. The compounds of formula (I) are useful in the treatment of inter alia benign prostatic hyperplasia.

  本发明提供了式(I)的化合物，其中R1代表C1-4烷氧基，该烷氧基可以选择性地被一个或多个氟原子取代；R2代表氢或C1-6烷氧基，该烷氧基可以选择性地被一个或多个氟原子取代；R3代表一个或多个基团，这些基团独立选择自氢、卤素、C1-4烷氧基和CF3；此外，R2和一个R3基团可以共同代表-OCH2-，该亚甲基基团连接到悬垂苯环的邻位；R4代表一个4、5或6元杂环环，其中包含1或2个从N、O和S中选择的杂原子，该环可以选择性地与苯环或一个5或6元杂环环融合，该环系作为一个整体可以选择性地被取代；X代表CH或N；L不存在或代表一个环状基团或开链基团；以及其药学上可接受的盐。式(I)的化合物在治疗良性前列腺增生等方面有用。
• Basic drug compositions with enhanced bioavailability
  申请人：Pfizer Products Inc.

  公开号：EP1027885A2

  公开（公告）日：2000-08-16

  A composition comprising a basic drug, a drug which forms a zwitterion, or a salt of either entity, admixed with a polymer selected from hydroxypropylmethylcellulose acetate succinate (HPMCAS), cellulose acetate trimellitate (CAT), cellulose acetate phthalate (CAP), hydroxypropylcellulose acetate phthalate (HPCAP), hydroxypropylmethyl-cellulose acetate phthalate (HPMCAP), and methylcellulose acetate phthalate (MCAP). The compositions having improved solubility, hence bioavailability, in the small intestine; Processes for testing such compositions, and methods of using such compositions. The compositions comprise the basic drug, zwitterion, or salt and one or more of the aforementioned polymers. The invention further relates to a method for increasing the bioavailability of a basic or a zwitterionic drug comprising co-administering the basic drug, the zwitterionic drug, or the salt, with one or more of the aforementioned polymers.

  一种组合物，包括一种碱性药物、一种形成齐聚物的药物或其中一种的盐，与一种选自羟丙基甲基纤维素醋酸琥珀酸酯（HPMCAS）的聚合物混合、邻苯二甲酸醋酸纤维素（CAP）、邻苯二甲酸羟丙基纤维素（HPCAP）、邻苯二甲酸羟丙基甲基纤维素 （HPMCAP）和邻苯二甲酸甲基纤维素（MCAP）。这些组合物在小肠中的溶解度有所提高，因此生物利用率也有所提高；测试此类组合物的工艺以及使用此类组合物的方法。这些组合物包括基本药物、齐聚物或盐以及一种或多种上述聚合物。本发明还涉及一种提高碱性药物或齐聚物生物利用度的方法，包括将碱性药物、齐聚物或盐与一种或多种上述聚合物共同给药。
• Hydrogel-driven drug dosage form
  申请人：——

  公开号：US20030086972A1

  公开（公告）日：2003-05-08

  A controlled release dosage form has a coated core with the core comprising a drug-containing composition and a water-swellable composition, each occupying separate regions within the core. The coating around the core is water-permeable, water-insoluble and has at least one delivery port therethrough. A variety of geometric arrangements are disclosed.

  一种控释剂型有一个带涂层的核心，核心由含药成分和水溶性成分组成，这两种成分分别占据核心的不同区域。核心周围的涂层可渗透水，不溶于水，并至少有一个输送口。本文公开了多种几何排列方式。
• QUINOLINE AND QUINAZOLINE COMPOUNDS USEFUL IN THERAPY
  申请人：Pfizer Research and Development Company, N.V./S.A.

  公开号：EP0877734B1

  公开（公告）日：2000-07-12
• HYDROGEL-DRIVEN DRUG DOSAGE FORM
  申请人：Pfizer Products Inc.

  公开号：EP1326587A2

  公开（公告）日：2003-07-16