triethyl-α-fluoro-phosphonoacetate

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 脂肪酰基
• 英文名称: triethyl-α-fluoro-phosphonoacetate
• 英文别名: triethyl 2-fluoro-phosphonoacetate；triethyl 2-fluorophosphonoacetate；triethylfluorophosphono-acetate；3-Ethoxycarbonylpentan-3-yl(fluorooxy)phosphinic acid
• 化学式: C₈H₁₆FO₅P
• 分子量: 242.184
• InChiKey: GTRURQZSAONDCW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  15
• 可旋转键数：
  6
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.88
• 拓扑面积：
  72.8
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  triethyl-α-fluoro-phosphonoacetate 、 1,8-二氮杂双环[5.4.0]十一碳-7-烯 以 正己烷 、 二氯甲烷 为溶剂， 以3.5 g (69%)的产率得到(2S,5Z)-2-amino-6-fluoro-7-[(1-iminoethyl)amino]-5-heptenoic acid, dihydrochloride
  参考文献：
  名称：

  Halogenated 2-amino-5,6 heptenoic acid derivatives useful as nitric oxide synthase inhibitors

  摘要：

  本发明揭示了卤代2-氨基-5,6-庚烯酸衍生物，用作一氧化氮合酶抑制剂。

  公开号：

  US20020049202A1

文献信息

• Derivatives of tetrapeptides as CCK agonists
  申请人：Abbott Laboratories

  公开号：US05270302A1

  公开（公告）日：1993-12-14

  Selective and potent Type-A CCK receptor agonists of formula (I): X--Y--Z--Q (I) or a pharmaceutically acceptable salt thereof, wherein, X is selected from ##STR1## Y is selected from ##STR2## Z is ##STR3## and Q is ##STR4## or pharmaceutically-acceptable salts thereof, useful in the treatment of gastrointestinal disorders (including gallbladder disorders), central nervous system disorders, insulin-related disorders and pain, as well as in appetite regulation.

  公式（I）的选择性和有效的Type-A CCK受体激动剂为：X--Y--Z--Q（I）或其药学上可接受的盐，其中，X选自##STR1##，Y选自##STR2##，Z为##STR3##，Q为##STR4##或其药学上可接受的盐，可用于治疗胃肠道疾病（包括胆囊疾病）、中枢神经系统疾病、胰岛素相关疾病和疼痛，以及食欲调节。
• Heterocyclic compounds and their use in the treatment of Type-II diabetes
  申请人：SmithKline Beecham PLC

  公开号：US05589492A1

  公开（公告）日：1996-12-31

  A compound of the formula A.sup.1 --X--(CH.sub.2).sub.n --O--A.sup.2 --A.sup.3 --CO.R.sup.2 (I) or a tautomeric form thereof and/or a pharmaceutically acceptable salt thereof, and/or a pharmaceutically acceptable solvate thereof, wherein: A.sup.1 represents a substituted or unsubstituted aromatic heterocyclyl group; A.sup.2 represents a benzene ring having three optional substituents; A.sup.3 represents a moiety of formula --(CH.sub.2).sub.m --CHR.sup.1 -- wherein R.sup.1 represents a halogen atom or a moiety of formula S(O).sub.p A.sup.4 wherein A.sup.4 represents hydrogen, substituted or unsubstituted alkyl, aryl, aralkyl, alkylcarbonyl or an aromatic heterocyclyl group and p represents zero or an integer 1 or 2 and m represents zero or an integer in the range of from 1 to 5, or A.sup.3 represents a moiety of formula --CH.dbd.CR.sup.1 -- wherein R.sup.1 is as defined above; R.sup.2 represents OR.sup.3 wherein R.sup.3 represents hydrogen, alkyl, aryl or aralkyl, or R.sup.2 represents --NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 each independently represent hydrogen or alkyl or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are attached form a heterocyclic ring; X represents O, S or NR wherein R represents a hydrogen atom, an alkyl group, an acyl group, an aralkyl group wherein the aryl moiety may be substituted or unsubstituted, or a substituted or unsubstituted aryl group; and n represents an integer in the range of from 2 to 6; a process for the preparation of such a compound, a pharmaceutical composition comprising such a compound and the use of such a compound and composition in medicine.

  一种具有以下结构的化合物：A.sup.1 --X--(CH.sub.2).sub.n --O--A.sup.2 --A.sup.3 --CO.R.sup.2 (I)或其互变异构体和/或其药学上可接受的盐，和/或其药学上可接受的溶剂，其中：A.sup.1代表取代或未取代的芳香杂环基团；A.sup.2代表具有三个可选取代基团的苯环；A.sup.3代表具有式--(CH.sub.2).sub.m --CHR.sup.1 --的基团，其中R.sup.1代表卤素原子或式S(O).sub.p A.sup.4的基团，其中A.sup.4代表氢、取代或未取代的烷基、芳基、芳基烷基、烷基羰基或芳香杂环基团，p代表零或整数1或2，m代表零或范围在1到5之间的整数，或A.sup.3代表具有式--CH.dbd.CR.sup.1 --的基团，其中R.sup.1如上定义；R.sup.2代表OR.sup.3，其中R.sup.3代表氢、烷基、芳基或芳基烷基，或R.sup.2代表--NR.sup.4 R.sup.5，其中R.sup.4和R.sup.5各自独立地代表氢或烷基，或R.sup.4和R.sup.5与它们连接的氮原子一起形成杂环环；X代表O、S或NR，其中R代表氢原子、烷基、酰基、芳基烷基，其中芳基可能是取代或未取代的，或取代或未取代的芳基；n代表范围在2到6之间的整数；一种制备这种化合物的方法，包括这种化合物的药物组合物和这种化合物及组合物在医学中的用途。
• Neuroprotective treatment methods using selective iNOS inhibitors
  申请人：Pharmacia Corporation

  公开号：US20030119826A1

  公开（公告）日：2003-06-26

  Therapeutic methods for the prevention and treatment of neurodegenerative conditions are described, the methods including administering to a subject in need thereof a neuroprotective effective amount of a selective inhibitor of inducible nitric oxide synthase.

  描述了预防和治疗神经退行性疾病的治疗方法，其中包括向需要的对象施用一种选择性抑制诱导型一氧化氮合酶的神经保护有效量。
• [EN] 7-AMINO ALKYLIDENYL-HETEROCYCLIC QUINOLONES AND NAPHTHYRIDONES<br/>[FR] NAPHTYRIDONES ET QUINOLONES 7-AMINO ALKYLIDENYL-HETEROCYCLIQUES
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2005033108A1

  公开（公告）日：2005-04-14

  The present invention relates to compounds having a structure according to Formula I wherein n, m, z, R, R2, R3, R4, R5, R6, A, E, X, Y a and b are as defined above; or an optical isomer, diastereomer or enantiomer thereof; a pharmaceutically acceptable salt, hydrate, or prodrug thereof.

  本发明涉及具有如下式I所示结构的化合物，其中n、m、z、R、R2、R3、R4、R5、R6、A、E、X、Y、a和b如上所定义；或其光学异构体、对映异构体或对映体；以及其药学上可接受的盐、水合物或前药。
• Agents and methods for treatment of cancer
  申请人：——

  公开号：US20030013702A1

  公开（公告）日：2003-01-16

  Agents and methods for chemoprevention and treatment of neoplasia are described, the agents including a selective inhibitor of inducible nitric oxide synthase and a combination of a selective inhibitor of inducible nitric oxide synthase and an inhibitor of cylcooxygenase-2 in a pharmaceutical composition. The agents and methods are used for chemoprevention and treatment of neoplasia including colorectal cancer and other cancers affecting epithelial cells throughout the body. The agents can also be used to treat the fibrosis that occurs with radiation therapy, as well as adenomatous polyps, including those with familial adenomatous polyposis (FAP).

  描述了用于化学预防和治疗肿瘤的药剂和方法，其中药剂包括一种选择性抑制诱导型一氧化氮合酶的药剂，以及一种选择性抑制诱导型一氧化氮合酶和环氧合酶-2的抑制剂的组合物在制药组合物中。这些药剂和方法用于化学预防和治疗包括结直肠癌和其他影响全身上皮细胞的肿瘤，还可用于治疗放射治疗引起的纤维化，以及腺瘤性息肉，包括家族性腺瘤性息肉症（FAP）的腺瘤。