TW357148B - Heterocycle-condensed morphinoid derivatives (II) the invention relates to a substituted mono heterocycle-condensed morphinoid derivatives as analgesics and for treating pathological conditions - Google Patents

Heterocycle-condensed morphinoid derivatives (II) the invention relates to a substituted mono heterocycle-condensed morphinoid derivatives as analgesics and for treating pathological conditions

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Publication number
TW357148B
TW357148B TW086100197A TW86100197A TW357148B TW 357148 B TW357148 B TW 357148B TW 086100197 A TW086100197 A TW 086100197A TW 86100197 A TW86100197 A TW 86100197A TW 357148 B TW357148 B TW 357148B
Authority
TW
Taiwan
Prior art keywords
alkyl
hydrogen
branched
linear
alkoxy
Prior art date
Application number
TW086100197A
Other languages
English (en)
Inventor
Giulio Dondio
Silvano Ronzoni
Pier Andrea Gatti
Davide Graziani
Original Assignee
Smithkline Beecham Spa
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
Priority claimed from ITMI960029 external-priority patent/IT1282950B1/it
Priority claimed from IT96MI002291 external-priority patent/IT1287130B1/it
Application filed by Smithkline Beecham Spa filed Critical Smithkline Beecham Spa
Application granted granted Critical
Publication of TW357148B publication Critical patent/TW357148B/zh

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/18Bridged systems
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12Antidiarrhoeals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/14Antitussive agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56Ring systems containing three or more rings
    • C07D209/58[b]- or [c]-condensed
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/20Spiro-condensed systems
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    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/0834Compounds having one or more O-Si linkage
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    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
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    • C08G77/00Macromolecular compounds obtained by reactions forming a linkage containing silicon with or without sulfur, nitrogen, oxygen or carbon in the main chain of the macromolecule
    • C08G77/48Macromolecular compounds obtained by reactions forming a linkage containing silicon with or without sulfur, nitrogen, oxygen or carbon in the main chain of the macromolecule in which at least two but not all the silicon atoms are connected by linkages other than oxygen atoms
    • C08G77/50Macromolecular compounds obtained by reactions forming a linkage containing silicon with or without sulfur, nitrogen, oxygen or carbon in the main chain of the macromolecule in which at least two but not all the silicon atoms are connected by linkages other than oxygen atoms by carbon linkages
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    • C08KUse of inorganic or non-macromolecular organic substances as compounding ingredients
    • C08K5/00Use of organic ingredients
    • C08K5/54Silicon-containing compounds
    • C08K5/541Silicon-containing compounds containing oxygen
    • C08K5/5415Silicon-containing compounds containing oxygen containing at least one Si—O bond
    • C08K5/5419Silicon-containing compounds containing oxygen containing at least one Si—O bond containing at least one Si—C bond
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    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08LCOMPOSITIONS OF MACROMOLECULAR COMPOUNDS
    • C08L83/00Compositions of macromolecular compounds obtained by reactions forming in the main chain of the macromolecule a linkage containing silicon with or without sulfur, nitrogen, oxygen or carbon only; Compositions of derivatives of such polymers
    • C08L83/04Polysiloxanes
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    • C08G77/00Macromolecular compounds obtained by reactions forming a linkage containing silicon with or without sulfur, nitrogen, oxygen or carbon in the main chain of the macromolecule
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    • C08G77/00Macromolecular compounds obtained by reactions forming a linkage containing silicon with or without sulfur, nitrogen, oxygen or carbon in the main chain of the macromolecule
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    • C08G77/04Polysiloxanes
    • C08G77/22Polysiloxanes containing silicon bound to organic groups containing atoms other than carbon, hydrogen and oxygen
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    • C08G77/00Macromolecular compounds obtained by reactions forming a linkage containing silicon with or without sulfur, nitrogen, oxygen or carbon in the main chain of the macromolecule
    • C08G77/04Polysiloxanes
    • C08G77/22Polysiloxanes containing silicon bound to organic groups containing atoms other than carbon, hydrogen and oxygen
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    • C08G77/04Polysiloxanes
    • C08G77/22Polysiloxanes containing silicon bound to organic groups containing atoms other than carbon, hydrogen and oxygen
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    • H05ELECTRIC TECHNIQUES NOT OTHERWISE PROVIDED FOR
    • H05KPRINTED CIRCUITS; CASINGS OR CONSTRUCTIONAL DETAILS OF ELECTRIC APPARATUS; MANUFACTURE OF ASSEMBLAGES OF ELECTRICAL COMPONENTS
    • H05K3/00Apparatus or processes for manufacturing printed circuits
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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Rheumatology (AREA)
  • Addiction (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Saccharide Compounds (AREA)
TW086100197A 1996-01-10 1997-01-10 Heterocycle-condensed morphinoid derivatives (II) the invention relates to a substituted mono heterocycle-condensed morphinoid derivatives as analgesics and for treating pathological conditions TW357148B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ITMI960029 IT1282950B1 (it) 1996-01-10 1996-01-10 Derivati eterociclo-condensati di morfinoidi
IT96MI002291 IT1287130B1 (it) 1996-11-05 1996-11-05 Derivati eterociclo-condensati di morfinoidi

Publications (1)

Publication Number Publication Date
TW357148B true TW357148B (en) 1999-05-01

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Application Number Title Priority Date Filing Date
TW086100197A TW357148B (en) 1996-01-10 1997-01-10 Heterocycle-condensed morphinoid derivatives (II) the invention relates to a substituted mono heterocycle-condensed morphinoid derivatives as analgesics and for treating pathological conditions

Country Status (21)

Country Link
US (1) US6365594B1 (zh)
EP (1) EP0880526B1 (zh)
JP (1) JP2000503019A (zh)
KR (1) KR19990077125A (zh)
CN (1) CN1090190C (zh)
AR (1) AR005423A1 (zh)
AT (1) ATE229958T1 (zh)
AU (1) AU706370B2 (zh)
BR (1) BR9707136A (zh)
CA (1) CA2242609A1 (zh)
CZ (1) CZ218298A3 (zh)
DE (1) DE69717967T2 (zh)
ES (1) ES2188888T3 (zh)
HU (1) HUP9900974A3 (zh)
IL (1) IL125226A0 (zh)
NO (1) NO983169L (zh)
NZ (1) NZ326331A (zh)
PL (1) PL327943A1 (zh)
TR (1) TR199801348T2 (zh)
TW (1) TW357148B (zh)
WO (1) WO1997025331A1 (zh)

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US6103722A (en) * 1997-07-23 2000-08-15 The Medical College Of Wisconsin Research Foundation Inc. Ischemic preconditioning
IT1312083B1 (it) * 1999-04-20 2002-04-04 Smithkline Beecham Spa Derivati morfinoidi, procedimento per la loro preparazione e loroimpiego terapeutico.
AU6635800A (en) * 1999-08-13 2001-03-13 Southern Research Institute Pyridomorphinans, thienomoprhinans and use thereof
US6465479B1 (en) * 1999-08-13 2002-10-15 Southern Research Institute Pyridomorphinans and use thereof
US6284769B1 (en) * 1999-12-03 2001-09-04 The Board Of Trustees Of The University Of Illinois Nonpeptide kappa opioid receptor antagonists
GB0025056D0 (en) * 2000-10-12 2000-11-29 Smithkline Beecham Spa Novel compounds
GB0025057D0 (en) * 2000-10-12 2000-11-29 Smithkline Beecham Spa Novel compounds
ES2304477T3 (es) 2000-10-31 2008-10-16 Rensselaer Polytechnic Institute Procedimiento de preparacion de compuestos con afinidad a receptores opioides.
EP1660088A4 (en) * 2003-08-27 2009-04-29 Southern Res Inst PYRIDOMORPHINANES, PYRIDAZINOMORPHINANES AND USE THEREOF
JP5198067B2 (ja) 2004-11-05 2013-05-15 レンセラール ポリテクニック インスティチュート 4−ヒドロキシベンゾモルファン
CN1298720C (zh) * 2005-03-18 2007-02-07 中国科学院上海有机化学研究所 C环连接有五元杂环的青藤碱衍生物和合成方法
WO2006126529A1 (ja) 2005-05-25 2006-11-30 Shionogi & Co., Ltd. 6,7-不飽和-7-カルバモイル置換モルヒナン誘導体
CN101210016B (zh) * 2006-12-29 2011-07-20 中国科学院上海药物研究所 一类杂环并吗啡喃类化合物、制备方法及用途
US20100130512A1 (en) * 2007-05-16 2010-05-27 Rensselaer Polytechnic Institute Fused-ring heterocycle opioids
KR101519682B1 (ko) 2007-08-09 2015-05-19 렌슬러 폴리테크닉 인스티튜트 4급 오피오이드 카르복스아미드
JP5555890B2 (ja) * 2009-03-19 2014-07-23 アルカーメス ファーマ アイルランド リミテッド 高い経口バイオアベイラビリティを有するモルフィナン誘導体
WO2011008636A1 (en) * 2009-07-15 2011-01-20 Mallinckrodt Inc. 3-oxy-hydromorphone derivatives
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US8436175B2 (en) 2010-03-22 2013-05-07 Rensselaer Polytechnic Institute Carboxamide bioisosteres of opiates
HUE041981T2 (hu) 2010-08-23 2019-06-28 Alkermes Pharma Ireland Ltd Eljárások antipszichotikum által kiváltott súlygyarapodás kezelésére
US9029543B2 (en) 2011-04-05 2015-05-12 Alkermes, Inc. Process for the synthesis of quaternary amine compounds
CA2840643C (en) 2011-06-29 2017-11-21 Alkermes, Inc. Peripherally acting opioid compounds
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KR19990077125A (ko) 1999-10-25
JP2000503019A (ja) 2000-03-14
DE69717967T2 (de) 2003-08-28
WO1997025331A1 (en) 1997-07-17
ES2188888T3 (es) 2003-07-01
US6365594B1 (en) 2002-04-02
ATE229958T1 (de) 2003-01-15
CA2242609A1 (en) 1997-07-17
CZ218298A3 (cs) 1999-08-11
DE69717967D1 (de) 2003-01-30
AU706370B2 (en) 1999-06-17
NZ326331A (en) 2000-01-28
AR005423A1 (es) 1999-06-23
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EP0880526B1 (en) 2002-12-18
AU1441097A (en) 1997-08-01
PL327943A1 (en) 1999-01-04
CN1090190C (zh) 2002-09-04
HUP9900974A2 (hu) 1999-08-30
IL125226A0 (en) 1999-03-12
CN1213372A (zh) 1999-04-07
HUP9900974A3 (en) 2000-09-28

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