IT1287130B1 - New fused poly:hydro-imino:ethano-phenanthrene derivatives - useful as delta opioid agonists or antagonists having e.g. analgesic, antiallergic anti-inflammatory or immunosuppressant activity - Google Patents

New fused poly:hydro-imino:ethano-phenanthrene derivatives - useful as delta opioid agonists or antagonists having e.g. analgesic, antiallergic anti-inflammatory or immunosuppressant activity

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Publication number
IT1287130B1
IT1287130B1 ITMI962291A IT1287130B1 IT 1287130 B1 IT1287130 B1 IT 1287130B1 IT MI962291 A ITMI962291 A IT MI962291A IT 1287130 B1 IT1287130 B1 IT 1287130B1
Authority
IT
Italy
Prior art keywords
alkyl
alkoxy
mcor
cycloalkylalkyl
alkenyl
Prior art date
Application number
Other languages
Italian (it)
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
Application filed by Smithkline Beecham Spa filed Critical Smithkline Beecham Spa
Publication of ITMI962291A0 publication Critical patent/ITMI962291A0/en
Priority to IT96MI002291 priority Critical patent/IT1287130B1/en
Priority to ES97901009T priority patent/ES2188888T3/en
Priority to HU9900974A priority patent/HUP9900974A3/en
Priority to ARP970100077A priority patent/AR005423A1/en
Priority to EP97901009A priority patent/EP0880526B1/en
Priority to AT97901009T priority patent/ATE229958T1/en
Priority to KR1019980705261A priority patent/KR19990077125A/en
Priority to US09/101,213 priority patent/US6365594B1/en
Priority to NZ326331A priority patent/NZ326331A/en
Priority to CN97192879A priority patent/CN1090190C/en
Priority to PL97327943A priority patent/PL327943A1/en
Priority to BR9707136-6A priority patent/BR9707136A/en
Priority to CA002242609A priority patent/CA2242609A1/en
Priority to CZ982182A priority patent/CZ218298A3/en
Priority to TR1998/01348T priority patent/TR199801348T2/en
Priority to DE69717967T priority patent/DE69717967T2/en
Priority to PCT/EP1997/000120 priority patent/WO1997025331A1/en
Priority to IL12522697A priority patent/IL125226A0/en
Priority to JP9524871A priority patent/JP2000503019A/en
Priority to AU14410/97A priority patent/AU706370B2/en
Priority to TW086100197A priority patent/TW357148B/en
Publication of ITMI962291A1 publication Critical patent/ITMI962291A1/en
Priority to NO983169A priority patent/NO983169L/en
Application granted granted Critical
Publication of IT1287130B1 publication Critical patent/IT1287130B1/en

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Polyhydro-10,4b-imino ethano-phenanthrene derivatives of formula (I), their solvates and salts are new; Q = (CH)n; R1 = H; Me; 2-6C alkyl, 3-7C cycloalkyl, 4-6C cycloalkylalkyl all optionally substituted by OH; 3-5C alkenyl; aryl; aralkyl; 2- or 3-furyl; (CH2)mCOR; or A-B; m = 0-5; R = 1-6C alkyl, OH, 1-5C alkoxy, 3-6C alkenyloxy, alkaryl or NR10R11; R10, R11 = H, 1-6C alkyl, 4-6C cycloalkylalkyl, 3-5C alkenyl, aryl or aralkyl; A = 1-10C alkylene; B = optionally substituted aryl or heteroaryl; R2 = H, OH, 1-5C alkoxy, halo, NO2, NR'10R11 or SR'10; R'10 = R10 or COR1; R3 = H, 1-6C alkyl, OH, 1-5C alkoxy, halo, (CH2)mCOR, SR10,NO2, NR10R10, NHCOR10, or NHSO2R10; R4, R5 = H, OH, 1-5C alkoxy, or phenoxy; or R4+R5 = O; or R4+R3 = OCH2O; R6 = phenyl or a 5- or 6-membered heteroaryl containing 1-3 heteroatoms both substituted by 1-3 R3; CZR12, CH2WA', COCOR12; NR'13R14; PZR12; S(O)iR12; Z = O or S; R12 = 1-18C alkyl, OH, 1-18C alkoxy, aralkoxy, or NR13R14; R13, R14 = H; Me; 2-6C alkyl, 3-7C cycloalkyl or 3-6C cycloalkylalkyl all optionally substituted by 1-3 F; 3-6C alkenyl; aryl aralkyl; or optionally substituted heterocyclyl; or R13+R14 = 3-6C alkylene optionally interrupted by O or NR1; W = O, S or NR14; A' = H, alkyl or COR14; R'13 = R13 or (CH2)mCOR; i = 1-2; R7 = H, 1-18C alkyl, 2-18C alkenyl, halo, 1-6C haloalkyl, (CH2)mCOR or phenyl or a 5- or 6-membered heteroaryl containing 1-3 heteroatoms both substituted by R3; R8 = H or 1-6C alkyl; n = 0-1; and either (a) when n = 0; X, Y = O, S, CQ' or NR9; or (b) when n = 1; X=Y=N or X,Y = N and CH; Q' = H, R6 or R7; R9 = H 1-6C alkyl, 3-7C cycloalkyl or 4-6C cycloalkylalkyl or optionally substituted by OH (provided that methyl is unsubstituted) or NR10R11; 3-5C alkenyl; aryl; aralkyl; or (CH2)mCOR'; R' = OH, 1-5C alkoxy, 3-6C alkenyloxy, alkaryl or NR"10R"11; R"10, R"11 = H, 1-6C alkyl or 4-6C cycloalkylalkyl.
IT96MI002291 1996-01-10 1996-11-05 New fused poly:hydro-imino:ethano-phenanthrene derivatives - useful as delta opioid agonists or antagonists having e.g. analgesic, antiallergic anti-inflammatory or immunosuppressant activity IT1287130B1 (en)

Priority Applications (22)

Application Number Priority Date Filing Date Title
IT96MI002291 IT1287130B1 (en) 1996-11-05 1996-11-05 New fused poly:hydro-imino:ethano-phenanthrene derivatives - useful as delta opioid agonists or antagonists having e.g. analgesic, antiallergic anti-inflammatory or immunosuppressant activity
PL97327943A PL327943A1 (en) 1996-01-10 1997-01-08 Condensed heterocyclic derivatives of morphonoide (ii)
CA002242609A CA2242609A1 (en) 1996-01-10 1997-01-08 Heterocycle-condensed morphinoid derivatives (ii)
ARP970100077A AR005423A1 (en) 1996-01-10 1997-01-08 MORPHINOID DERIVATIVES CONDENSED WITH HETERO CYCLES (II), THEIR USE AS A THERAPEUTIC SUBSTANCE AND TO PREPARE MEDICINES, PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND PROCEDURE TO PREPARE SUCH DERIVATIVES.
EP97901009A EP0880526B1 (en) 1996-01-10 1997-01-08 Heterocycle-condensed morphinoid derivatives (ii)
AT97901009T ATE229958T1 (en) 1996-01-10 1997-01-08 HETEROCYCLIC CONDENSED MORPHINE DERIVATIVES
KR1019980705261A KR19990077125A (en) 1996-01-10 1997-01-08 The heterocyclic-condensed morphine derivative (II)
US09/101,213 US6365594B1 (en) 1996-01-10 1997-01-08 Heterocycle-condensed morphinoid derivatives (II)
NZ326331A NZ326331A (en) 1996-01-10 1997-01-08 Heterocycle-condensed morphinoid derivatives and medicaments
CN97192879A CN1090190C (en) 1996-01-10 1997-01-08 Heterocycle-condensed morphinoid derivatives (II)
ES97901009T ES2188888T3 (en) 1996-01-10 1997-01-08 MORFINOID DERIVATIVES 8II) CONDENSED WITH HETEROCICLES.
BR9707136-6A BR9707136A (en) 1996-01-10 1997-01-08 Morphoid derivatives condensed in heterocycle (ii)
HU9900974A HUP9900974A3 (en) 1996-01-10 1997-01-08 Heterocycle-condensed morphinoid derivatives, process for the preparation thereof, their use and pharmaceutical compositions containing them
CZ982182A CZ218298A3 (en) 1996-01-10 1997-01-08 Heterocyclic condensed morphiate derivative (ii), process of its preparation and application
TR1998/01348T TR199801348T2 (en) 1996-01-10 1997-01-08 Heterosyclic condensate morphinoid t�revleri (II).
DE69717967T DE69717967T2 (en) 1996-01-10 1997-01-08 HETEROCYCLIC CONDENSED MORPHINE DERIVATIVES
PCT/EP1997/000120 WO1997025331A1 (en) 1996-01-10 1997-01-08 Heterocycle-condensed morphinoid derivatives (ii)
IL12522697A IL125226A0 (en) 1996-01-10 1997-01-08 Heterocycle-condensed morphinoid derivatives (II)
JP9524871A JP2000503019A (en) 1996-01-10 1997-01-08 Heterocyclic fused morphinoid derivative (II)
AU14410/97A AU706370B2 (en) 1996-01-10 1997-01-08 Heterocycle-condensed morphinoid derivatives (II)
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
NO983169A NO983169L (en) 1996-01-10 1998-07-09 Heterocycle-condensed morphinoid derivatives (31)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
IT96MI002291 IT1287130B1 (en) 1996-11-05 1996-11-05 New fused poly:hydro-imino:ethano-phenanthrene derivatives - useful as delta opioid agonists or antagonists having e.g. analgesic, antiallergic anti-inflammatory or immunosuppressant activity

Publications (3)

Publication Number Publication Date
ITMI962291A0 ITMI962291A0 (en) 1996-11-05
ITMI962291A1 ITMI962291A1 (en) 1998-05-05
IT1287130B1 true IT1287130B1 (en) 1998-08-04

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Family Applications (1)

Application Number Title Priority Date Filing Date
IT96MI002291 IT1287130B1 (en) 1996-01-10 1996-11-05 New fused poly:hydro-imino:ethano-phenanthrene derivatives - useful as delta opioid agonists or antagonists having e.g. analgesic, antiallergic anti-inflammatory or immunosuppressant activity

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IT (1) IT1287130B1 (en)

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ITMI962291A0 (en) 1996-11-05
ITMI962291A1 (en) 1998-05-05

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