Title:
NOVEL ADENINE DERIVATIVE AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2015/009008
Kind Code:
A1
Abstract:
The present invention relates to a novel adenine derivative and a pharmaceutical use thereof and, more specifically, to a novel adenine derivative having a structure of chemical formula 1 or a pharmaceutically acceptable salt thereof and to a composition for preventing or treating degenerative brain disease, the composition containing the novel adenine derivative or the pharmaceutically acceptable salt thereof. The novel adenine derivative and the pharmaceutically acceptable salt thereof according to the present invention are adenosine A3 receptor agonists, and have an action of inhibiting the migration or infiltration of inflammatory cells (microglia, macrophages, neutrophils, etc.), to disease areas and the activities thereof. In addition, the adenine derivative according to the present invention was verified to suppress and treat brain injury more remarkably compared with the known adenosine A3 receptor agonists in a cerebral ischemia experimental model, exhibit significant effects by drug administration 10 hours after cerebral infarction, and allow long-term survival despite brain injury due to cerebral ischemia, and thus can be useful as an agent for treating and preventing degenerative brain disease including a stroke.
Inventors:
KIM WON KI (KR)
CHOI YONGSEOK (KR)
CHOI YONGSEOK (KR)
Application Number:
PCT/KR2014/006354
Publication Date:
January 22, 2015
Filing Date:
July 15, 2014
Export Citation:
Assignee:
UNIV KOREA RES & BUS FOUND (KR)
International Classes:
C07D473/34; A61K31/52; A61P25/00
Foreign References:
| KR20130065899A | 2013-06-20 | |||
| EP0212535A1 | 1987-03-04 | |||
| US5688774A | 1997-11-18 |
Other References:
LERNER, LEON M. ET AL.: "Inhibition of Adenosine Deaminase by Alcohols Derived from Adenine Nucleosides", BIOCHEMISTRY, vol. 11, no. 15, 1972, pages 2772 - 2777
ROSSI, RALPH R. ET AL.: "Specificity of Inhibition of Adenosine Deaminase by Trialcohols Derived from Nucleosides", JOURNAL OF MEDICINAL CHEMISTRY, vol. 16, no. 5, 1973, pages 457 - 460
STOLARSKI, RYSZARD ET AL.: "Acyclo Nucleosides and Nucleotides: Synthesis, Conformation and Other Properties, and Behaviour in Some Enzyme Systems, of 2',3'-Seco Purine Nucleosides, Nucleotides and 3',5'-Cyclic Phosphate, Analogses of cAMP and cGMP", JOURNAL OF BIOSCIENCES, vol. 41, no. 7-8, 1986, pages 758 - 770
SUFRIN, JANICE R. ET AL.: "Antitrypanosomal Activity of Purine Nucleosides Can Be Enhanced by Their Conversion to O-acetylated Derivatives", ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, vol. 40, no. 11, 1996, pages 2567 - 2572, XP055064182
CHEN, C. M. ET AL.: "Biological Activity of Ribose-Modified N6-(DELTA2-Isopentenyl)adenosine Derivative", CAN. J. BIOCHEM., vol. 52, 1974, pages 1154 - 1161
JACOBSON, KENNETH A. ET AL.: "A3-adenosine receptors: design of selective ligands and therapeutic prospects", DRUG FUTURE, vol. 20, no. 7, 1995, pages 689 - 699, XP002911460
JACOBSON, KENNETH A. ET AL.: "Structure-Activity realationships of 9-Alkyl-adenine and Ribose-Modified Adenosine Derivatives at Rat A3 Adenosine Receptors", J. MED. CHEM., vol. 38, 1995, pages 1720 - 1735
ROSSI, RALPH R. ET AL.: "Specificity of Inhibition of Adenosine Deaminase by Trialcohols Derived from Nucleosides", JOURNAL OF MEDICINAL CHEMISTRY, vol. 16, no. 5, 1973, pages 457 - 460
STOLARSKI, RYSZARD ET AL.: "Acyclo Nucleosides and Nucleotides: Synthesis, Conformation and Other Properties, and Behaviour in Some Enzyme Systems, of 2',3'-Seco Purine Nucleosides, Nucleotides and 3',5'-Cyclic Phosphate, Analogses of cAMP and cGMP", JOURNAL OF BIOSCIENCES, vol. 41, no. 7-8, 1986, pages 758 - 770
SUFRIN, JANICE R. ET AL.: "Antitrypanosomal Activity of Purine Nucleosides Can Be Enhanced by Their Conversion to O-acetylated Derivatives", ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, vol. 40, no. 11, 1996, pages 2567 - 2572, XP055064182
CHEN, C. M. ET AL.: "Biological Activity of Ribose-Modified N6-(DELTA2-Isopentenyl)adenosine Derivative", CAN. J. BIOCHEM., vol. 52, 1974, pages 1154 - 1161
JACOBSON, KENNETH A. ET AL.: "A3-adenosine receptors: design of selective ligands and therapeutic prospects", DRUG FUTURE, vol. 20, no. 7, 1995, pages 689 - 699, XP002911460
JACOBSON, KENNETH A. ET AL.: "Structure-Activity realationships of 9-Alkyl-adenine and Ribose-Modified Adenosine Derivatives at Rat A3 Adenosine Receptors", J. MED. CHEM., vol. 38, 1995, pages 1720 - 1735
Attorney, Agent or Firm:
LEE, Cheo Young et al. (KR)
이처영 (KR)
이처영 (KR)
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