WO2006136829A3 - Pyrazole derivatives and their use as pka and pkb modulators - Google Patents

Pyrazole derivatives and their use as pka and pkb modulators Download PDF

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Publication number
WO2006136829A3
WO2006136829A3 PCT/GB2006/002286 GB2006002286W WO2006136829A3 WO 2006136829 A3 WO2006136829 A3 WO 2006136829A3 GB 2006002286 W GB2006002286 W GB 2006002286W WO 2006136829 A3 WO2006136829 A3 WO 2006136829A3
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WIPO (PCT)
Prior art keywords
absent
pka
bond
linker selected
pkb
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PCT/GB2006/002286
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French (fr)
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WO2006136829A2 (en
Inventor
Research Technology Lim Cancer
Hannah Fiona Sore
Robert George Boyle
Christopher Hamlett
Gordon Saxty
Marinus Leendert Verdonk
David Winter Walker
Steven John Woodhead
Steven Howard
Original Assignee
Astex Therapeutics Ltd
Cancer Res Inst Royal
Astrazeneca Ab
Research Technology Lim Cancer
Hannah Fiona Sore
Robert George Boyle
Christopher Hamlett
Gordon Saxty
Marinus Leendert Verdonk
David Winter Walker
Steven John Woodhead
Steven Howard
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Priority claimed from GB0512654A external-priority patent/GB0512654D0/en
Application filed by Astex Therapeutics Ltd, Cancer Res Inst Royal, Astrazeneca Ab, Research Technology Lim Cancer, Hannah Fiona Sore, Robert George Boyle, Christopher Hamlett, Gordon Saxty, Marinus Leendert Verdonk, David Winter Walker, Steven John Woodhead, Steven Howard filed Critical Astex Therapeutics Ltd
Priority to JP2008517590A priority Critical patent/JP2008543919A/en
Priority to EP06755590A priority patent/EP1919875A2/en
Publication of WO2006136829A2 publication Critical patent/WO2006136829A2/en
Publication of WO2006136829A3 publication Critical patent/WO2006136829A3/en

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    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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Abstract

The invention provides a compound of the formula (I) or a salt, solvate, tautomer or N-oxide thereof; wherein A is a saturated hydrocarbon linker group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; L1 is a bond or a linker selected from C1-C4 alkenylene, C1-C4 alkynylene, -CONR’, -NR’CO, -S-, -C(O)-, -C(NR11)-, -C(S)-, -N(R11)2, C(=CHR11), -SO- and -SO2-; or L1 together with t R16 forms an 8-12 membered fused bicyclic heteroaryl ring system; L3 is a bond or a linker selected from CONH and HNCO; provided that L1 and L3 cannot both be linkers simultaneously; and provided also that L1 and L3 cannot both be a bond simultaneously; R16 is an optionally substituted 5- to 12-membered monocyclic or bicyclic carbocyclic or heterocyclic ring; L2 is absent or is a linker selected from C]-C4 alkylene, Ci-C4 alkenylene, Ci-C4 alkynylene, -CONR’-, -NR’CO-, -O-, -S-, -C(O)-, C(=CHR11), C(S)-, -N(R11)2, C3-4 cycloalkanediyl, -SO- and -SO2-; R17 is absent or is C1-6 alkyl or an optionally substituted 5 to 12 membered carbocyclic or heterocyclic ring; provided that when R17 is absent, then L2 is also absent; and R2, R3, R4, R5, R11 and R’ are as defined in the claims. Compounds (I) modulate (PKA) and (PKB).
PCT/GB2006/002286 2005-06-21 2006-06-21 Pyrazole derivatives and their use as pka and pkb modulators WO2006136829A2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
JP2008517590A JP2008543919A (en) 2005-06-21 2006-06-21 Pharmaceutical compounds
EP06755590A EP1919875A2 (en) 2005-06-21 2006-06-21 Pyrazole derivatives and their use as pka and pkb modulators

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US69262005P 2005-06-21 2005-06-21
US60/692,620 2005-06-21
GB0512654A GB0512654D0 (en) 2005-06-21 2005-06-21 Pharmaceutical compounds
GB0512654.5 2005-06-21
US74365806P 2006-03-22 2006-03-22
US60/743,658 2006-03-22

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WO2006136829A2 WO2006136829A2 (en) 2006-12-28
WO2006136829A3 true WO2006136829A3 (en) 2007-02-15

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JP (1) JP2008543919A (en)
WO (1) WO2006136829A2 (en)

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CA2548374C (en) 2003-12-23 2014-05-27 Astex Therapeutics Limited Pyrazole derivatives as protein kinase modulators
EP1902032A1 (en) 2005-06-22 2008-03-26 Astex Therapeutics Limited Pharmaceutical compounds
US8541461B2 (en) 2005-06-23 2013-09-24 Astex Therapeutics Limited Pharmaceutical combinations comprising pyrazole derivatives as protein kinase modulators
HUE032640T2 (en) 2005-11-08 2017-10-30 Vertex Pharma Heterocyclic modulators of ATP-binding cassette transporters
US7671221B2 (en) * 2005-12-28 2010-03-02 Vertex Pharmaceuticals Incorporated Modulators of ATP-Binding Cassette transporters
AU2012244242B2 (en) * 2005-12-28 2015-05-21 Vertex Pharmaceuticals Incorporated 1-(benzo [D] [1,3] dioxol-5-yl) -N- (phenyl) cyclopropane- carboxamide derivatives and related compounds as modulators of ATP-Binding Cassette transporters for the treatment of Cystic Fibrosis
US7691902B2 (en) * 2005-12-28 2010-04-06 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
GB0704932D0 (en) 2007-03-14 2007-04-25 Astex Therapeutics Ltd Pharmaceutical compounds
US8969386B2 (en) 2007-05-09 2015-03-03 Vertex Pharmaceuticals Incorporated Modulators of CFTR
US8507534B2 (en) 2007-12-07 2013-08-13 Vertex Pharmaceuticals Incorporated Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid
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JP2013523833A (en) 2010-04-07 2013-06-17 バーテックス ファーマシューティカルズ インコーポレイテッド 3- (6- (1- (2,2-difluorobenzo [D] [1,3] dioxol-5-yl) cyclopropanecarboxamido) -3-methylpyridin-2-yl) benzoic acid pharmaceutical composition and Its administration
EP2651930B1 (en) * 2010-12-16 2015-10-28 Boehringer Ingelheim International GmbH Biarylamide inhibitors of leukotriene production
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WO2015073231A1 (en) 2013-11-12 2015-05-21 Vertex Pharmaceuticals Incorporated Process of preparing pharmaceutical compositions for the treatment of cftr mediated diseases
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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8946278B2 (en) 2007-02-07 2015-02-03 Glaxosmithkline Llc Inhibitors of AkT activity

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