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HUP0001125A2 - Kondenzált pirimidinszármazékok és nyílt láncú analógjaik, valamint az ezeket tartalmazó gyógyszerkészítmények - Google Patents

Kondenzált pirimidinszármazékok és nyílt láncú analógjaik, valamint az ezeket tartalmazó gyógyszerkészítmények

Info

Publication number
HUP0001125A2
HUP0001125A2 HU0001125A HUP0001125A HUP0001125A2 HU P0001125 A2 HUP0001125 A2 HU P0001125A2 HU 0001125 A HU0001125 A HU 0001125A HU P0001125 A HUP0001125 A HU P0001125A HU P0001125 A2 HUP0001125 A2 HU P0001125A2
Authority
HU
Hungary
Prior art keywords
group
hydrogen atom
alkyl
optionally substituted
carbocyclic
Prior art date
Application number
HU0001125A
Other languages
English (en)
Inventor
Guy W. Bemis
John E. Cochran
John Patrick Duffy
Vincent P. Galullo
Edmund Martin Harrington
Mark A. Murcko
Francesco Gerald Salituro
Michael Su
Keith P. Wilson
Original Assignee
Vertex Pharmaceuticals Incorporated
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 US08/822,373 external-priority patent/US5945418A/en
Application filed by Vertex Pharmaceuticals Incorporated filed Critical Vertex Pharmaceuticals Incorporated
Publication of HUP0001125A2 publication Critical patent/HUP0001125A2/hu
Publication of HUP0001125A3 publication Critical patent/HUP0001125A3/hu

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    • 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
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Abstract

A találmány a sejtproliferációban, a sejthalálban és azextracelluláris stimulusokra adott válaszreakcióban szerepet játszóp38 emlős protein kináz (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig) és(Ih) általános képletű inhibitoraira - amelyek képletében Q1, Q2 és Q3 aromás karbocikusos vagy heterociklusos csoport; ahol Q1és Q3 1-4-szeresen szubsztituált; és Q2 adott esetben legfeljebbnégyszeresen szubsztituált; R' hidrogénatom, vagy adott esetben szubsztituált alkil-, alkenil-,alkinil- vagy fenilcsoport; X tio-,oxi-, szulfonil-,szulfinil-,-S(O)2-N(R2)-, -N(R2) -S(O)2-, -N(R2)-C(O)O-,-O-C(O)-N(R2)-, karbonil-, -C(O)O-,-O-C(O) -, -C(O)-N(R2)-, -N(R2)-C(O)-, -N(R2)-, -C(R2)2 vagy -C(OR2)2- csoport; R hidrogénatom,-R2,-N(R2)2,-OR2, -SR2, -C(O)-N(R2)2, -S(O)2-N(R2)2vagy -C(O)-OR2 csoport, ahol két szomszédos R adott esetben egymássalés az Y szubsztituensekkel karbociklusos vagy heterociklusos gyűrűtképez; R2 hidrogénatom, vagy adott esetben szubsztituált alkil- vagyalkenilcsoport; Y nitrogénatom vagy szénatom; A - ha jelen van - nitrogénatom vagy=C(R')- csoport; n értéke 0 vagy l; R1 hidrogénatom, alkil-, hidroxi- vagy alkoxicsoport; R4 adott esetben alkil-, karbociklus vagy heterociklusos csoport; és R5 hidrogénatom, -C(R')2OH, -C(O)R4, -C(O)OR4 -C(R3)2OPO3H2 vagy -PO3H2 képletű csoport - vonatkozik. A találmány kiterjed a találmányszerinti inhibitorokat tartalmazó gyógyszerkészítményekre is. Ó
HU0001125A 1996-12-18 1997-12-17 Fused pyrimidine derivatives and their open chain analogues, pharmaceutical compositions thereof HUP0001125A3 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US3428896P 1996-12-18 1996-12-18
US08/822,373 US5945418A (en) 1996-12-18 1997-03-20 Inhibitors of p38
US08/862,925 US6147080A (en) 1996-12-18 1997-06-10 Inhibitors of p38
PCT/US1997/023392 WO1998027098A1 (en) 1996-12-18 1997-12-17 SUBSTITUTED NITROGEN CONTAINING HETEROCYCLES AS INHIBITORS OF p38 PROTEIN KINASE

Publications (2)

Publication Number Publication Date
HUP0001125A2 true HUP0001125A2 (hu) 2000-10-28
HUP0001125A3 HUP0001125A3 (en) 2002-01-28

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HU0001125A HUP0001125A3 (en) 1996-12-18 1997-12-17 Fused pyrimidine derivatives and their open chain analogues, pharmaceutical compositions thereof

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US (1) US6147080A (hu)
EP (1) EP0951467B1 (hu)
JP (1) JP4171072B2 (hu)
CN (2) CN1153770C (hu)
AP (1) AP1136A (hu)
AT (1) ATE236165T1 (hu)
AU (1) AU738000B2 (hu)
BG (1) BG64533B1 (hu)
BR (1) BR9714415A (hu)
CA (1) CA2274825C (hu)
CZ (1) CZ299600B6 (hu)
DE (1) DE69720522T2 (hu)
DK (1) DK0951467T3 (hu)
EA (1) EA002855B1 (hu)
EE (1) EE04191B1 (hu)
ES (1) ES2202658T3 (hu)
HK (1) HK1023340A1 (hu)
HU (1) HUP0001125A3 (hu)
ID (1) ID21919A (hu)
IL (1) IL130349A0 (hu)
IS (1) IS5069A (hu)
NO (1) NO315047B1 (hu)
NZ (1) NZ336146A (hu)
PL (1) PL202464B1 (hu)
PT (1) PT951467E (hu)
SK (1) SK284578B6 (hu)
TR (1) TR199902194T2 (hu)
TW (1) TW521071B (hu)
WO (1) WO1998027098A1 (hu)

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WO1999061039A2 (en) * 1998-05-22 1999-12-02 MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. Novel composition for modulating ischemic cell death
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WO1999064400A1 (en) * 1998-06-12 1999-12-16 Vertex Pharmaceuticals Incorporated INHIBITORS OF p38
EP1277740A1 (en) * 1998-06-12 2003-01-22 Vertex Pharmaceuticals Incorporated Inhibitors of p38
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
WO2000017175A1 (en) * 1998-09-18 2000-03-30 Vertex Pharmaceuticals Incorporated INHIBITORS OF p38
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AU1909200A (en) 1998-11-04 2000-05-22 Smithkline Beecham Corporation Pyridin-4-yl or pyrimidin-4-yl substituted pyrazines
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