EA200300621A1 - Биарильные производные никотинамида, полезные в качестве ингибиторов изоферментов pde4 - Google Patents

Биарильные производные никотинамида, полезные в качестве ингибиторов изоферментов pde4

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Publication number
EA200300621A1
EA200300621A1 EA200300621A EA200300621A EA200300621A1 EA 200300621 A1 EA200300621 A1 EA 200300621A1 EA 200300621 A EA200300621 A EA 200300621A EA 200300621 A EA200300621 A EA 200300621A EA 200300621 A1 EA200300621 A1 EA 200300621A1
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EA
Eurasian Patent Office
Prior art keywords
alkyl
pde4
inhibitors
useful
isoerminents
Prior art date
Application number
EA200300621A
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English (en)
Inventor
Роберт Джеймс Чамберс
Томас Виктор Маги
Энтони Марфат
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Пфайзер Продактс Инк.
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Application filed by Пфайзер Продактс Инк. filed Critical Пфайзер Продактс Инк.
Publication of EA200300621A1 publication Critical patent/EA200300621A1/ru

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    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
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Abstract

Соединения, полезные в качестве ингибиторов PDE4 при лечении заболеваний, регулируемых активацией и дегрануляцией эозинофилов, особенно астмы, хронического бронхита и хронического обструктивного заболевания легких, формулы (I), где j равно 0 или 1 при условии, что когда j равно 0, n должно быть равно 2; k равно 0 или 1; m равно 0, 1 или 2; n равно 1 или 2; Wпредставляет собой -O-; либо -S(=O)-, где t равно 0, 1 или 2; либо -N(R)-; Wпредставляет собой -O-CRR- или отсутствует; Y представляет собой =C(R)- или -[N⇒(O)]-, где k равно 0 или 1; Rи Rпредставляют собой -H; -F; -CF; -(C-C)алкил; -(C-C)циклоалкил; фенил или бензил, замещенные заместителями Rв количестве от 0 до 3; либо Rи Rвзяты вместе, но только в случае, когда m равно 1, с образованием спирогруппировки; Rи Rимеют такое же значение, как Rи R, за исключением того, что один из них должен представлять собой -H; Rи Rпредставляют собой -H; -F; -Cl; -CN; -NO; -(C-C)алкил; -(C-C)алкинил; фторированный -(C-C)алкил; -ORи -C(=O)NRR; Rпредставляет собой -H; -(C-C)алкил; фенил; бензил или -OR; R, Rи Rв дополнение к другим значениям могут быть взяты вместе с образованием, например, формы (II); Q, Qи Z являются такими, как определено в заявке.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200300621A 2001-01-31 2001-12-06 Биарильные производные никотинамида, полезные в качестве ингибиторов изоферментов pde4 EA200300621A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US26549201P 2001-01-31 2001-01-31
PCT/IB2001/002341 WO2002060875A1 (en) 2001-01-31 2001-12-06 Nicotinamide biaryl derivatives useful as inhibitors of pde4 isozymes

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EA200300621A1 true EA200300621A1 (ru) 2003-12-25

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US (2) US6649633B2 (ru)
EP (1) EP1355884A1 (ru)
JP (1) JP2004520386A (ru)
KR (1) KR20030074761A (ru)
CN (1) CN1518542A (ru)
BG (1) BG108038A (ru)
BR (1) BR0116852A (ru)
CA (1) CA2436535A1 (ru)
CR (1) CR7025A (ru)
CZ (1) CZ20031895A3 (ru)
EA (1) EA200300621A1 (ru)
EC (2) ECSP034709A (ru)
EE (1) EE200300360A (ru)
HU (1) HUP0400637A2 (ru)
IL (1) IL156413A0 (ru)
IS (1) IS6846A (ru)
MA (1) MA26983A1 (ru)
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NZ (1) NZ526453A (ru)
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PL (1) PL364135A1 (ru)
SK (1) SK8792003A3 (ru)
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ZA (1) ZA200304894B (ru)

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AU2004226353A1 (en) * 2003-04-01 2004-10-14 Laboratoires Serono Sa Inhibitors of phosphodiesterases in infertility
GB0309781D0 (en) * 2003-04-29 2003-06-04 Glaxo Group Ltd Compounds
GB0317516D0 (en) * 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as PDE4 inhibitors
US7153870B2 (en) 2003-07-25 2006-12-26 Pfizer Inc. Nicotinamide derivatives useful as PDE4 inhibitors
GB0317498D0 (en) * 2003-07-25 2003-08-27 Pfizer Ltd Compounds
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