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Indole alkaloid derivatives having opioid receptor agonistic effect, and therapeutic compositions and methods relating to same UPDATE

外国特許コード F130007259
整理番号 P07-074US-D1
掲載日 2013年4月3日
出願国 アメリカ合衆国
出願番号 201213549564
公報番号 20120276195
公報番号 8648090
出願日 平成24年7月16日(2012.7.16)
公報発行日 平成24年11月1日(2012.11.1)
公報発行日 平成26年2月11日(2014.2.11)
優先権データ
  • 2007US-60986370 (2007.11.8) US
  • 2008US-12266579 (2008.11.7) US
発明の名称 (英語) Indole alkaloid derivatives having opioid receptor agonistic effect, and therapeutic compositions and methods relating to same UPDATE
発明の概要(英語) (US8648090)
Indole alkaloid derivatives having an opioid receptor agonistic effect, their synthesis, and therapeutic compositions containing these derivatives, and methods of treating conditions with these compounds and therapeutic compositions, are provided.
特許請求の範囲(英語) [claim1]
1. A compound having the formula:

wherein R1 is a halogen atom, hydrogen atom, or a nitro group or alkoxy group and R2 is a hydrogen atom or halogen atom or nitro group.
[claim2]
2. A compound having the formula:

wherein R1.dbd.F, R2.dbd.H; R1.dbd.Cl, R2.dbd.H; R1.dbd.H, R2.dbd.Cl; R1.dbd.Br, R2.dbd.H; R1.dbd.H, R2.dbd.Br; R1.dbd.NO2, R2.dbd.H; R1.dbd.H, R2.dbd.NO2; or R1.dbd.OMe, R2.dbd.H.
[claim3]
3. A pharmaceutical composition comprising a therapeutic amount of a compound of claim 1 or a pharmaceutically acceptable salt thereof.
[claim4]
4. The pharmaceutical composition of claim 3 in a pharmaceutically deliverable form selected from the group consisting of solutions, suspensions, emulsions, tablets, pills, pellets, granules, lozenges, capsules, capsules containing liquids, powders, sustained-release formulations, syrups, elixirs, creams, gels, suppositories, emulsions, aerosols, and sprays.
[claim5]
5. A pharmaceutical composition containing 0.1% to 100% of said compound of claim 1 or a pharmaceutically acceptable salt thereof.
[claim6]
6. A method for eliciting a therapeutic effect in a patient in need thereof, comprising the step of administering to said patient an effective dose of the 2,3-ethylene glycol bridged indoline adduct compound of claim 1 or a pharmaceutically acceptable salt thereof, wherein said therapeutic effect is an analgesic effect.
[claim7]
7. The method of claim 6 wherein said step of administering is performed by a delivery route selected from the group consisting of oral, transdermal, inhalation, injection, infusion, and suppository.
[claim8]
8. The method of claim 6 wherein said patient is an animal.
[claim9]
9. The method of claim 6 wherein said patient is a mammal.
[claim10]
10. The method of claim 6 wherein said patient is a human.
[claim11]
11. The method of claim 6 wherein patient is a human and the therapeutic effect is pain treatment, where an effective total daily dosage of said compound ranges from about 0.1 mg to about 1,000 mg active compound/kg body weight of said patient.
[claim12]
12. A method for making the 2,3-ethylene glycol bridged indoline adduct compound of claim 1, comprising the steps of: reacting a Corynanthe-type indole alkaloid with hypervalent iodine in the presence of ethylene glycol effective to provide a 2,3-ethylene glycol bridged indoline adduct, effective to mask a 2,3-n bond of an indole nucleus of said adduct.
[claim13]
13. The method of claim 12 further comprising introducing a halogen atom at a C10 position of the adduct via electrophilic aromatic substitution, providing a C10-halogenated adduct derivative.
  • 発明者/出願人(英語)
  • TAKAYAMA HIROMITSU
  • KITAJIMA MARIKO
  • MATSUMOTO KENJIRO
  • HORIE SYUNJI
  • CHIBA UNIVERSITY
  • JOSAI UNIVERSITY
国際特許分類(IPC)

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