WO1987005903A3 - Orally active nonaddicting analgesics - Google Patents

Orally active nonaddicting analgesics Download PDF

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Publication number
WO1987005903A3
WO1987005903A3 PCT/US1987/000253 US8700253W WO8705903A3 WO 1987005903 A3 WO1987005903 A3 WO 1987005903A3 US 8700253 W US8700253 W US 8700253W WO 8705903 A3 WO8705903 A3 WO 8705903A3
Authority
WO
WIPO (PCT)
Prior art keywords
nonaddicting
normorphine
analogs
analgesics
orally active
Prior art date
Application number
PCT/US1987/000253
Other languages
French (fr)
Other versions
WO1987005903A2 (en
Inventor
John A Lawson
Graw Joseph I De
Gilda Harris Loew
Original Assignee
Stanford Res Inst Int
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Stanford Res Inst Int filed Critical Stanford Res Inst Int
Priority to JP62501220A priority Critical patent/JPH085889B2/en
Priority to DE3790166A priority patent/DE3790166C2/en
Publication of WO1987005903A2 publication Critical patent/WO1987005903A2/en
Publication of WO1987005903A3 publication Critical patent/WO1987005903A3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
    • C07D489/02—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids

Abstract

Stereoisomerically pure forms of normorphine analogs which have superior analgesic and nonaddicting qualities. In addition, a method of separating diastereomeric forms of N-sec-alkyl-substituted analogs utilizes the hydrocarbyl (1-8C) diesters of the normorphine derivatives. A new method for preparing the N-methylalkylmethyl derivatives of normorphine and norcodeine and their conventional analogs is also disclosed. This method employs the corresponding methyl alkyl ketones and a reducing agent.
PCT/US1987/000253 1986-03-24 1987-02-06 Orally active nonaddicting analgesics WO1987005903A2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
JP62501220A JPH085889B2 (en) 1986-03-24 1987-02-06 Orally active non-addictive analgesics
DE3790166A DE3790166C2 (en) 1986-03-24 1987-02-06 Pure stereoisomers of N-cyclopropyl-methyl-nor-morphine cpds.

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US843,150 1986-03-24
US06/843,150 US4749706A (en) 1986-03-24 1986-03-24 Orally active nonaddicting analgesics

Publications (2)

Publication Number Publication Date
WO1987005903A2 WO1987005903A2 (en) 1987-10-08
WO1987005903A3 true WO1987005903A3 (en) 1987-11-05

Family

ID=25289190

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1987/000253 WO1987005903A2 (en) 1986-03-24 1987-02-06 Orally active nonaddicting analgesics

Country Status (8)

Country Link
US (1) US4749706A (en)
EP (1) EP0261148B1 (en)
JP (1) JPH085889B2 (en)
CA (1) CA1313868C (en)
DE (2) DE3790166C2 (en)
GB (1) GB2198435B (en)
NL (1) NL8720049A (en)
WO (1) WO1987005903A2 (en)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5366979A (en) * 1990-06-07 1994-11-22 Pharmaco Development Partners Orally active nonaddicting analgesics
KR950000705A (en) * 1993-06-19 1995-01-03 권기범 14-Substituted Morfinan Derivatives and Pharmaceuticals Containing the Same
US6190691B1 (en) 1994-04-12 2001-02-20 Adolor Corporation Methods for treating inflammatory conditions
US5962477A (en) * 1994-04-12 1999-10-05 Adolor Corporation Screening methods for cytokine inhibitors
US6573282B1 (en) 1995-09-12 2003-06-03 Adolor Corporation Peripherally active anti-hyperalgesic opiates
US5849761A (en) * 1995-09-12 1998-12-15 Regents Of The University Of California Peripherally active anti-hyperalgesic opiates
WO2005037212A2 (en) * 2003-10-14 2005-04-28 Phoenix Pharmalabs, Inc. Treatment of chemical dependency with substantially nonaddicting normorphine and norcodeine derivatives
US8188067B2 (en) * 2004-04-01 2012-05-29 Teva Pharmaceutical Industries Ltd. Formulations of 6-mercaptopurine
US8691989B2 (en) * 2008-06-20 2014-04-08 Phoenix Pharmalabs, Inc. Methods of synthesis of morphinans
WO2014031403A1 (en) * 2012-08-22 2014-02-27 Phoenix Pharmalabs, Inc. Use of morphine analogs for animal health
WO2017066619A1 (en) 2015-10-16 2017-04-20 Teva Pharmaceutical Industries Ltd. Treatment of non-alcoholic fatty liver disease or non-alcoholic steatohepatitis with delayed-release 6-mercaptopurine

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4218454A (en) * 1977-07-08 1980-08-19 Sri International N-αMethylcyclopropylmethyl derivatives of normorphine and noroodeine, and analgesic compositions and methods employing the normorphine derivatives

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4269843A (en) * 1978-05-24 1981-05-26 Sri International N-Sec-alkyl analogs of norcodeine and normorphine and analgesic compositions and methods employing the normorphine derivatives

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4218454A (en) * 1977-07-08 1980-08-19 Sri International N-αMethylcyclopropylmethyl derivatives of normorphine and noroodeine, and analgesic compositions and methods employing the normorphine derivatives

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
CHEMICAL ABSTRACTS, Volume 87, No. 17, 24 October 1977, (Columbus, Ohio, US), G.H. LOEW et al.: "New N-Substituent Variations in the Morphine Series", see page 28, Abstract 127012g, & Opiates Endog. Opioid Pept., Proc. Int. Narc. Res. Club Meet. 197l, 399-402 *
J. March: "Advanced Organic Chemistry. Reactions, Mechanisms, and Structure", 2nd Edition, 1977, McGraw-Hill International Book Co., (Auckland, US), pages 819-820 see page 819, "Reaction 6-16" *
Journal of Medical Chemistry, Volume 21, No. 5, 1978, American Chemical Society, (US), J.I. DEGRAW et al.: "Analgesics. 1. Synthesics and Analgesic Properties of N-sec-alkyl- and N-tert-Alkyl- Normorphines", pages 415-422 see the whole document cited in the application *

Also Published As

Publication number Publication date
EP0261148B1 (en) 1992-01-02
GB2198435A (en) 1988-06-15
DE3790166T1 (en) 1988-06-23
NL8720049A (en) 1988-01-04
US4749706A (en) 1988-06-07
GB2198435B (en) 1990-12-12
JPH085889B2 (en) 1996-01-24
WO1987005903A2 (en) 1987-10-08
JPS63502825A (en) 1988-10-20
CA1313868C (en) 1993-02-23
EP0261148A1 (en) 1988-03-30
DE3790166C2 (en) 1998-08-13
GB8726032D0 (en) 1987-12-09

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