WO2002060875A8 - Nicotinamide biaryl derivatives useful as inhibitors of pde4 isozymes - Google Patents

Nicotinamide biaryl derivatives useful as inhibitors of pde4 isozymes

Info

Publication number
WO2002060875A8
WO2002060875A8 PCT/IB2001/002341 IB0102341W WO02060875A8 WO 2002060875 A8 WO2002060875 A8 WO 2002060875A8 IB 0102341 W IB0102341 W IB 0102341W WO 02060875 A8 WO02060875 A8 WO 02060875A8
Authority
WO
WIPO (PCT)
Prior art keywords
alkyl
inhibitors
nicotinamide
derivatives useful
biaryl derivatives
Prior art date
Application number
PCT/IB2001/002341
Other languages
French (fr)
Other versions
WO2002060875A1 (en
Inventor
Robert James Chambers
Thomas Victor Magee
Anthony Marfat
Original Assignee
Pfizer Prod Inc
Robert James Chambers
Thomas Victor Magee
Anthony Marfat
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 to SK879-2003A priority Critical patent/SK8792003A3/en
Priority to MXPA03006887A priority patent/MXPA03006887A/en
Application filed by Pfizer Prod Inc, Robert James Chambers, Thomas Victor Magee, Anthony Marfat filed Critical Pfizer Prod Inc
Priority to HU0400637A priority patent/HUP0400637A2/en
Priority to JP2002561026A priority patent/JP2004520386A/en
Priority to EA200300621A priority patent/EA200300621A1/en
Priority to IL15641301A priority patent/IL156413A0/en
Priority to CA002436535A priority patent/CA2436535A1/en
Priority to EEP200300360A priority patent/EE200300360A/en
Priority to PL01364135A priority patent/PL364135A1/en
Priority to BR0116852-5A priority patent/BR0116852A/en
Priority to EP01273556A priority patent/EP1355884A1/en
Priority to KR10-2003-7010074A priority patent/KR20030074761A/en
Priority to NZ526453A priority patent/NZ526453A/en
Publication of WO2002060875A1 publication Critical patent/WO2002060875A1/en
Priority to IS6846A priority patent/IS6846A/en
Priority to BG108038A priority patent/BG108038A/en
Priority to NO20033397A priority patent/NO20033397L/en
Publication of WO2002060875A8 publication Critical patent/WO2002060875A8/en

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    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • C07D213/82Amides; Imides in position 3
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructive pulmonary disease, of the formula (I): where j is 0 or 1 provided that when j is 0, n must be 2; k is 0 or 1; m is 0, 1, or 2; n is 1 or 2; W1 is -0-; or -S(=O)t-, where t is 0, 1, or 2; or -N(R3)-; W2 is -O-CRARB- or is absent; Y is =C(R1a)- or -[N∊(O)k]- where k is 0 or 1; R?A and RB¿ are -H; -F; -CF¿3?; -(C1-C4)alkyl; -(C3-C7)cycloalkyl; phenyl; or benzyl substituted with 0 to 3 substituents R?10; or RA and RB¿ are taken together, but only in the case where m is 1, to form a spiro moiety; R?C and RD¿ have the same meaning as R?A and RB¿ except that one of them must be -H, R?1 and R2¿ are -H; -F; -Cl; -CN; -NO¿2?; (C1-C4)alkyl; -(C2-C4)alkynal; fluorinated-(C1-C3)alkyl; -OR?16¿; and -C(=O)NR22aR22b; R3 is -H; -(C¿1?-C3)alkyl; phenyl; benzyl; or -OR?16; R4, R5 and R6¿ in addition to other meanings may be taken together to form, e.g., form (II): Q1, Q2 and Z are as defined in the application.
PCT/IB2001/002341 2001-01-31 2001-12-06 Nicotinamide biaryl derivatives useful as inhibitors of pde4 isozymes WO2002060875A1 (en)

Priority Applications (16)

Application Number Priority Date Filing Date Title
NZ526453A NZ526453A (en) 2001-01-31 2001-12-06 Nicotinamide biaryl derivatives useful as inhibitors of PDE4 isozymes
EEP200300360A EE200300360A (en) 2001-01-31 2001-12-06 Biaryl derivatives of nicotinamide used as inhibitors of PDE4 isozymes
HU0400637A HUP0400637A2 (en) 2001-01-31 2001-12-06 Nicotinamide biaryl derivatives useful as inhibitors of pde4 isozymes and pharmaceutical compositions containing them
JP2002561026A JP2004520386A (en) 2001-01-31 2001-12-06 Nicotinamide biaryl derivatives useful as inhibitors of PDE4 isozymes
EA200300621A EA200300621A1 (en) 2001-01-31 2001-12-06 BIARRYLIC DERIVATIVES OF NICOTINAMIDE, USEFUL AS AN INHIBITORS OF PDE4 ISOERMINENTS
IL15641301A IL156413A0 (en) 2001-01-31 2001-12-06 Nicotinamide biaryl derivatives useful as inhibitors of pde4 isozymes
CA002436535A CA2436535A1 (en) 2001-01-31 2001-12-06 Nicotinamide biaryl derivatives useful as inhibitors of pde4 isozymes
SK879-2003A SK8792003A3 (en) 2001-01-31 2001-12-06 Nicotinamide biaryl derivatives useful as inhibitors of PDE4 isozymes and pharmaceutical composition containing them
PL01364135A PL364135A1 (en) 2001-01-31 2001-12-06 Nicotinamide biaryl derivatives useful as inhibitors of pde4 isozymes
EP01273556A EP1355884A1 (en) 2001-01-31 2001-12-06 Nicotinamide biaryl derivatives useful as inhibitors of pde4 isozymes
BR0116852-5A BR0116852A (en) 2001-01-31 2001-12-06 Biarylated nicotinamide derivatives useful as pde4 isozyme inhibitors
KR10-2003-7010074A KR20030074761A (en) 2001-01-31 2001-12-06 Nicotinamide biaryl derivatives useful as inhibitors of pde4 isozymes
MXPA03006887A MXPA03006887A (en) 2001-01-31 2001-12-06 Nicotinamide biaryl derivatives useful as inhibitors of pde4 isozymes.
IS6846A IS6846A (en) 2001-01-31 2003-06-16 Nicotinamide baryl derivatives useful for inhibiting PDE4 isotopic enzymes
BG108038A BG108038A (en) 2001-01-31 2003-07-28 Nicotinamide biaryl derivatives useful as inhibitors of pde4 isozymes
NO20033397A NO20033397L (en) 2001-01-31 2003-07-30 Nicotinamide biaryl derivatives useful as inhibitors of PDE4 isozymes

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US26549201P 2001-01-31 2001-01-31
US60/265,492 2001-01-31

Publications (2)

Publication Number Publication Date
WO2002060875A1 WO2002060875A1 (en) 2002-08-08
WO2002060875A8 true WO2002060875A8 (en) 2003-07-31

Family

ID=23010671

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2001/002341 WO2002060875A1 (en) 2001-01-31 2001-12-06 Nicotinamide biaryl derivatives useful as inhibitors of pde4 isozymes

Country Status (25)

Country Link
US (2) US6649633B2 (en)
EP (1) EP1355884A1 (en)
JP (1) JP2004520386A (en)
KR (1) KR20030074761A (en)
CN (1) CN1518542A (en)
BG (1) BG108038A (en)
BR (1) BR0116852A (en)
CA (1) CA2436535A1 (en)
CR (1) CR7025A (en)
CZ (1) CZ20031895A3 (en)
EA (1) EA200300621A1 (en)
EC (2) ECSP034710A (en)
EE (1) EE200300360A (en)
HU (1) HUP0400637A2 (en)
IL (1) IL156413A0 (en)
IS (1) IS6846A (en)
MA (1) MA26983A1 (en)
MX (1) MXPA03006887A (en)
NO (1) NO20033397L (en)
NZ (1) NZ526453A (en)
OA (1) OA12540A (en)
PL (1) PL364135A1 (en)
SK (1) SK8792003A3 (en)
WO (1) WO2002060875A1 (en)
ZA (1) ZA200304894B (en)

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EP1389468A4 (en) * 2001-05-23 2007-01-10 Tanabe Seiyaku Co Compositions for promoting healing of bone fracture
MXPA03010672A (en) * 2001-05-23 2004-03-02 Tanabe Seiyaku Co Therapeutic compositions for repairing chondropathy.
WO2003071870A1 (en) * 2002-02-26 2003-09-04 Schlesinger Stephen L Use of leukotriene receptor antagonist for treatment of scarring
EP1424101A3 (en) * 2002-11-29 2004-08-18 NOZAKI, Masako Use of a leukotriene C4 and D4 receptor antagonist for the preparation of a medicament for treating or preventing brain inflammation and sepsis
JP2006516548A (en) 2002-12-30 2006-07-06 アンジオテック インターナショナル アクツィエン ゲゼルシャフト Drug delivery from rapidly gelled polymer compositions
EP1624893A2 (en) * 2003-04-01 2006-02-15 Applied Research Systems ARS Holding N.V. Inhibitors of phosphodiesterases in infertility
GB0309781D0 (en) * 2003-04-29 2003-06-04 Glaxo Group Ltd Compounds
GB0317498D0 (en) * 2003-07-25 2003-08-27 Pfizer Ltd Compounds
US20050020587A1 (en) * 2003-07-25 2005-01-27 Pfizer Inc Nicotinamide derivatives useful as PDE4 inhibitors
GB0317482D0 (en) * 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as pde4 inhibitors
GB0317516D0 (en) * 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as PDE4 inhibitors
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