WO2006127899A3 - (r)-n-methylnaltrexone, processes for its synthesis and its pharmaceutical use - Google Patents

(r)-n-methylnaltrexone, processes for its synthesis and its pharmaceutical use Download PDF

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Publication number
WO2006127899A3
WO2006127899A3 PCT/US2006/020233 US2006020233W WO2006127899A3 WO 2006127899 A3 WO2006127899 A3 WO 2006127899A3 US 2006020233 W US2006020233 W US 2006020233W WO 2006127899 A3 WO2006127899 A3 WO 2006127899A3
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WO
WIPO (PCT)
Prior art keywords
synthesis
methylnaltrexone
processes
pharmaceutical use
mntx
Prior art date
Application number
PCT/US2006/020233
Other languages
French (fr)
Other versions
WO2006127899A2 (en
Inventor
Harold D Doshan
Julio Perez
Original Assignee
Progenics Pharm Inc
Harold D Doshan
Julio Perez
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=36997886&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=WO2006127899(A3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority to DK06771163.0T priority Critical patent/DK1913001T3/en
Priority to SI200631663T priority patent/SI1913001T1/en
Priority to CA2609662A priority patent/CA2609662C/en
Priority to CN200680022957XA priority patent/CN101208344B/en
Priority to BRPI0611162-9A priority patent/BRPI0611162A2/en
Application filed by Progenics Pharm Inc, Harold D Doshan, Julio Perez filed Critical Progenics Pharm Inc
Priority to JP2008513707A priority patent/JP5213704B2/en
Priority to EP06771163.0A priority patent/EP1913001B1/en
Priority to AU2006249911A priority patent/AU2006249911C1/en
Priority to MX2007014880A priority patent/MX2007014880A/en
Priority to PL06771163T priority patent/PL1913001T3/en
Priority to ES06771163T priority patent/ES2429160T3/en
Publication of WO2006127899A2 publication Critical patent/WO2006127899A2/en
Publication of WO2006127899A3 publication Critical patent/WO2006127899A3/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/485Morphinan derivatives, e.g. morphine, codeine
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    • A61K9/0012Galenical forms characterised by the site of application
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D489/00Heterocyclic 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:
    • C07D489/02Heterocyclic 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
    • C07D489/04Salts; Organic complexes
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D489/00Heterocyclic 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:
    • C07D489/06Heterocyclic 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 a hetero atom directly attached in position 14
    • C07D489/08Oxygen atom
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/15Medicinal preparations ; Physical properties thereof, e.g. dissolubility
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10TTECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION
    • Y10T436/00Chemistry: analytical and immunological testing
    • Y10T436/14Heterocyclic carbon compound [i.e., O, S, N, Se, Te, as only ring hetero atom]
    • Y10T436/141111Diverse hetero atoms in same or different rings [e.g., alkaloids, opiates, etc.]

Abstract

This invention relates to stereoselective synthesis of R-MNTX and intermediates thereof, pharmaceutical preparations comprising R-MNTX or intermediates thereof and methods for their use.
PCT/US2006/020233 2005-05-25 2006-05-25 (r)-n-methylnaltrexone, processes for its synthesis and its pharmaceutical use WO2006127899A2 (en)

Priority Applications (11)

Application Number Priority Date Filing Date Title
ES06771163T ES2429160T3 (en) 2005-05-25 2006-05-25 (R) -N-methylnaltrexone, processes for its synthesis and pharmaceutical use
EP06771163.0A EP1913001B1 (en) 2005-05-25 2006-05-25 (r)-n-methylnaltrexone, processes for its synthesis and its pharmaceutical use
CA2609662A CA2609662C (en) 2005-05-25 2006-05-25 (r)-n-methylnaltrexone, process for its synthesis and its pharmaceutical use
CN200680022957XA CN101208344B (en) 2005-05-25 2006-05-25 (R)-N-methylnaltrexone, processes for its synthesis and its pharmaceutical use
BRPI0611162-9A BRPI0611162A2 (en) 2005-05-25 2006-05-25 (r) -n-methylnaltrexone, process for its synthesis and pharmaceutical use
DK06771163.0T DK1913001T3 (en) 2005-05-25 2006-05-25 (R) -N-METHYLNALTREXON, METHODS OF SYNTHESIS AND PHARMACEUTICAL APPLICATION
JP2008513707A JP5213704B2 (en) 2005-05-25 2006-05-25 (R) -N-methylnaltrexone, synthesis method thereof and pharmaceutical use thereof
SI200631663T SI1913001T1 (en) 2005-05-25 2006-05-25 (r)-n-methylnaltrexone, processes for its synthesis and its pharmaceutical use
AU2006249911A AU2006249911C1 (en) 2005-05-25 2006-05-25 (R)-N-methylnaltrexone, processes for its synthesis and its pharmaceutical use
MX2007014880A MX2007014880A (en) 2005-05-25 2006-05-25 (r)-n-methylnaltrexone, processes for its synthesis and its pharmaceutical use.
PL06771163T PL1913001T3 (en) 2005-05-25 2006-05-25 (r)-n-methylnaltrexone, processes for its synthesis and its pharmaceutical use

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US68461605P 2005-05-25 2005-05-25
US60/684,616 2005-05-25

Publications (2)

Publication Number Publication Date
WO2006127899A2 WO2006127899A2 (en) 2006-11-30
WO2006127899A3 true WO2006127899A3 (en) 2007-02-08

Family

ID=36997886

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2006/020233 WO2006127899A2 (en) 2005-05-25 2006-05-25 (r)-n-methylnaltrexone, processes for its synthesis and its pharmaceutical use

Country Status (20)

Country Link
US (6) US7674904B2 (en)
EP (3) EP3219717A1 (en)
JP (4) JP5213704B2 (en)
CN (2) CN102721756A (en)
AR (1) AR057035A1 (en)
AU (1) AU2006249911C1 (en)
BR (1) BRPI0611162A2 (en)
CA (1) CA2609662C (en)
DK (1) DK1913001T3 (en)
ES (1) ES2429160T3 (en)
GT (1) GT200600226A (en)
HK (1) HK1244267A1 (en)
HN (1) HN2006019068A (en)
MX (1) MX2007014880A (en)
MY (1) MY151036A (en)
PL (1) PL1913001T3 (en)
PT (1) PT1913001E (en)
SI (1) SI1913001T1 (en)
TW (1) TWI383984B (en)
WO (1) WO2006127899A2 (en)

Cited By (3)

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US8524731B2 (en) 2005-03-07 2013-09-03 The University Of Chicago Use of opioid antagonists to attenuate endothelial cell proliferation and migration
US9518062B2 (en) 2009-07-16 2016-12-13 Mallinckrodt Llc Compounds and compositions for use in phototherapy and in treatment of ocular neovascular disease and cancers
US9526723B2 (en) 2008-03-21 2016-12-27 The University Of Chicago Treatment with opioid antagonists and mTOR inhibitors

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DK2368553T3 (en) * 2003-04-08 2015-02-09 Progenics Pharm Inc Pharmaceutical preparation comprising methylnaltrexone
CN1767855A (en) * 2003-04-08 2006-05-03 普罗热尼奇制药公司 Combination therapy for constipation comprising a laxative and a peripheral opioid antagonist
US20050004155A1 (en) * 2003-04-08 2005-01-06 Boyd Thomas A. Use of methylnaltrexone to treat irritable bowel syndrome
US20060205753A1 (en) * 2005-01-20 2006-09-14 Israel Robert J Use of methylnaltrexone and related compounds to treat post-operative gastrointestinal dysfunction
US9662325B2 (en) 2005-03-07 2017-05-30 The University Of Chicago Use of opioid antagonists to attenuate endothelial cell proliferation and migration
MX2007010833A (en) 2005-03-07 2009-02-17 Univ Chicago Use of opioid antagonists to attenuate endothelial cell proliferation and migration.
US8518962B2 (en) 2005-03-07 2013-08-27 The University Of Chicago Use of opioid antagonists
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AR057325A1 (en) 2005-05-25 2007-11-28 Progenics Pharm Inc SYNTHESIS OF (S) -N-METHYLNTREXONE, PHARMACEUTICAL COMPOSITIONS AND USES
AR057035A1 (en) * 2005-05-25 2007-11-14 Progenics Pharm Inc SYNTHESIS OF (R) -N-METHYLNTREXONE, PHARMACEUTICAL COMPOSITIONS AND USES
US20080194611A1 (en) * 2005-06-03 2008-08-14 Alverdy John C Modulation of Cell Barrier Dysfunction
WO2007140272A2 (en) 2006-05-26 2007-12-06 Pharmacofore, Inc. Controlled release of phenolic opioids
TW200815451A (en) * 2006-08-04 2008-04-01 Wyeth Corp 6-carboxy-normorphinan derivatives, synthesis and uses thereof
TWI489984B (en) 2006-08-04 2015-07-01 Wyeth Corp Formulations for parenteral delivery of compounds and uses thereof
TW200817048A (en) * 2006-09-08 2008-04-16 Wyeth Corp Dry powder compound formulations and uses thereof
EP2099764B1 (en) 2006-09-20 2011-07-27 Mallinckrodt Inc. Preparation of substituted morphinan-6-ones and salts and intermediates thereof
EP2101773A2 (en) * 2006-11-22 2009-09-23 Progenics Pharmaceuticals, Inc. (r)-n-stereoisomers of 7,8-saturated-4,5-epoxy-morphinanium analogs
BRPI0719587A2 (en) * 2006-11-22 2013-12-17 Progenics Pharm Inc (S) - 7,8-SATURATED-4,5-EPOXY-MORFINAN ANALOG STEREO ISOMERS
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