RS51546B - Pyrazole derivatives as protein kinase modulators - Google Patents

Pyrazole derivatives as protein kinase modulators

Info

Publication number
RS51546B
RS51546B RSP-2010/0532A RSP20100532A RS51546B RS 51546 B RS51546 B RS 51546B RS P20100532 A RSP20100532 A RS P20100532A RS 51546 B RS51546 B RS 51546B
Authority
RS
Serbia
Prior art keywords
group
heteroaryl
alkoxy
phenyl
hydrocarbyl
Prior art date
Application number
RSP-2010/0532A
Other languages
Serbian (sr)
Inventor
Valerio Berdini
Gordon Saxty
Marinus Leendert Verdonk
Steven John Woodhead
Paul Graham Wyatt
Robert George Boyle
Hannah Fiona Sore
David Winter Walker
Ian Collins
Robert Downham
Robin Arthur Ellis Carr
Original Assignee
Astex Therapeutics Limited
Cancer Research Technology Limited
The Institute Of Cancer Research:Royal Cancer Hospital
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 Astex Therapeutics Limited, Cancer Research Technology Limited, The Institute Of Cancer Research:Royal Cancer Hospital filed Critical Astex Therapeutics Limited
Publication of RS51546B publication Critical patent/RS51546B/en

Links

Abstract

Jedinjenje formule (I):ili njegova so, solvat, tautomer ili N-oksid;u kome, A je zasićena ugljovodonična linker grupa koja sadrži od 1 do 7 atoma ugljenika, pri čemu linker grupa ima maksimalnu dužinu lanca od 5 atoma koji se pruža između R1 i NR2R3 i maksimalnu dužinu lanca od 4 atoma koji se pruža između E i NR2R3, pri čemu jedan od atoma ugljenika u linker grupi mogu biti izborno zamenjeni atomom kiseonika ili azota; i pri čemu atomi ugljenika linker grupe A mogu izborno da nose jedan ili više supstituenata koji su izabrani od okso, fluora i hidroksida, uz uslov da se hidroksi grupa kada je prisutna ne nalazi na atomu ugljenika α u odnosu na NR2R3 grupu i uz uslov da se okso grupa kada je prisutna nalazi na atomu ugljenika α u odnosu na NR2R3 grupu;E je monociklična, biciklična karbociklična ili heterociklična grupa u kojoj, E je nesupstituisan ili ima do 4 supstituenta R8 izabrana iz grupe koju čine hidroksi, okso (kada je E nearomatičan), hlor, brom, trifluorometil, cijano, C1-4 hidrokarbiloksi i C1-4 hidrokarbil izborno supstituisan sa C1-2 alkoksi ili hidroksil;R1 je aril ili heteroaril grupa koja je nesupstituisana ili nosi jedan ili više supstituenata koji su izabrani iz grupe koju čine hidroksi; C1-4 aciloksi; fluor; hlor; brom; trifluorometil; cijano; CONH2; nitro; C1-4 hidrokarbiloksi i C1-4 hidrokarbil, pri čemu je svaki od njih izborno supstituisan sa C1-2 alkoksi, karboksi ili hidroksi; C1-4 acilamino; benzoilamino; pirolidinokarbonil; piperidinokarbonil; morfolinokarbonil; piperazinokarbonil; pet i šesto-člane heteroaril i heteroariloksi grupe koje sadrže jedan ili dva heteroatoma izabrana od N, O i S; fenil; fenil-C1-4alkil; fenil- C1-4 alkoksi; heteroaril- C1-4 alkil; heteroaril- C1-4 alkoksi i fenoksi, pri čemu su svaka od heteroaril, heteroariloksi, fenil, fenil- C1-4 alkil, fenil- C1-4 alkoksi, heteroaril-C1-4 alkil, heteroaril-C1-4 alkoksi i fenoksi grupa izborno supstituisana sa 1, 2 ili 3 supstituenata koji su izabrani iz grupe koju čine C1-2 aciloksi, fluor, hlor, brom, trifluorometil, cijano, CONH2, C1-2 hidrokarbiloksi i C1-2 hidrokarbil, gde je svaki od njih izborno supstituisan sa metoksi ili hidroksil;R2 i R3 nezabvisno su izabrani iz grupe koju čine vodonik, C1-4 hidrokarbil i C1-4 acil, pri čemu su hidrokarbil i acil grupe izborno supstituisane sa jednim ili više supstituenata koji su izabrani iz grupe koju čine fluor, hidroksi, amino, metilamino, dimetilamino i metoksi;ili R2 i R3 zajedno sa atomom azota za koji su vezani formiraju cikličnu grupu koja je izabrana od imidazol grupe i zasićene monociklične heterociklične grupe koja ima 4-7 članova u prstenu i izborno sadrži drugi heteroatom kao član prstena izabran od O i N;ili jedan od RCompound of Formula (I): or a salt, solvate, tautomer or N-oxide thereof, wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, wherein the linker group has a maximum chain length of 5 atoms which is provided between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may be optionally replaced by an oxygen or nitrogen atom; and wherein the linker group A carbon atoms may optionally carry one or more substituents selected from oxo, fluorine and hydroxide, provided that the hydroxy group when present is not present on the carbon atom α relative to the NR2R3 group and provided that the oxo group when present is on the carbon atom α relative to the NR2R3 group; E is a monocyclic, bicyclic carbocyclic or heterocyclic group in which, E is unsubstituted or has up to 4 substituents R8 selected from the group consisting of hydroxy, oxo (when E non-aromatic), chlorine, bromine, trifluoromethyl, cyano, C1-4 hydrocarbloxy and C1-4 hydrocarbyl optionally substituted with C1-2 alkoxy or hydroxyl; R1 is an aryl or heteroaryl group which is unsubstituted or carries one or more substituents selected from the group consisting of hydroxy; C1-4 acyloxy; fluorine; chlorine; bromine; trifluoromethyl; cyano; CONH2; nitro; C1-4 hydrocarbloxy and C1-4 hydrocarbyl, each of which is optionally substituted with C1-2 alkoxy, carboxy or hydroxy; C1-4 acylamino; benzoylamino; pyrrolidinocarbonyl; piperidinocarbonyl; morpholinocarbonyl; piperazinocarbonyl; five and six-membered heteroaryl and heteroaryloxy groups containing one or two heteroatoms selected from N, O and S; phenyl; phenyl-C 1-4 alkyl; phenyl-C 1-4 alkoxy; heteroaryl-C 1-4 alkyl; heteroaryl-C 1-4 alkoxy and phenoxy, each of which is heteroaryl, heteroaryloxy, phenyl, phenyl-C 1-4 alkyl, phenyl-C 1-4 alkoxy, heteroaryl-C 1-4 alkyl, heteroaryl-C 1-4 alkoxy and phenoxy group optionally substituted with 1, 2 or 3 substituents selected from the group consisting of C1-2 acyloxy, fluorine, chlorine, bromine, trifluoromethyl, cyano, CONH2, C1-2 hydrocarbloxy and C1-2 hydrocarbyl, each of which is optionally substituted with methoxy or hydroxyl; R2 and R3 are independently selected from the group consisting of hydrogen, C1-4 hydrocarbyl and C1-4 acyl, wherein the hydrocarbyl and acyl groups are optionally substituted with one or more substituents selected from the group consisting of fluorine, hydroxy, amino, methylamino, dimethylamino and methoxy; or R2 and R3 together with the nitrogen atom to which they are attached form a cyclic group selected from imidazole group and a saturated monocyclic heterocyclic group having 4-7 ring members and optionally containing another heteroatom as ring member selected by O and N; or one of R

RSP-2010/0532A 2003-12-23 2004-12-23 Pyrazole derivatives as protein kinase modulators RS51546B (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US53219903P 2003-12-23 2003-12-23
GB0329617A GB0329617D0 (en) 2003-12-23 2003-12-23 Pharmaceutical compounds
US57784304P 2004-06-08 2004-06-08

Publications (1)

Publication Number Publication Date
RS51546B true RS51546B (en) 2011-06-30

Family

ID=30776233

Family Applications (1)

Application Number Title Priority Date Filing Date
RSP-2010/0532A RS51546B (en) 2003-12-23 2004-12-23 Pyrazole derivatives as protein kinase modulators

Country Status (11)

Country Link
CN (1) CN1922148B (en)
AT (1) ATE483689T1 (en)
DE (1) DE602004029501D1 (en)
DK (1) DK1706385T3 (en)
GB (1) GB0329617D0 (en)
ME (1) ME01934B (en)
PT (1) PT1706385E (en)
RS (1) RS51546B (en)
SI (1) SI1706385T1 (en)
UA (1) UA90461C2 (en)
ZA (1) ZA200605127B (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0704932D0 (en) * 2007-03-14 2007-04-25 Astex Therapeutics Ltd Pharmaceutical compounds
CN108339121A (en) * 2017-01-25 2018-07-31 苏州大学 Purposes of the protein kinase A inhibitor in preparing treatment platelet counts and increasing relevant disease drug
CN111056990B (en) * 2019-12-16 2022-06-17 爱斯特(成都)生物制药股份有限公司 Preparation method for synthesizing 1-tert-butyloxycarbonyl-4- (4-carboxyphenyl) piperidine

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9804734D0 (en) * 1998-03-05 1998-04-29 Pfizer Ltd Compounds
IL147757A0 (en) * 1999-07-30 2002-08-14 Abbott Gmbh & Co Kg 2-pyrazolin-5-ones

Also Published As

Publication number Publication date
ME01934B (en) 2011-06-30
PT1706385E (en) 2010-12-22
ZA200605127B (en) 2010-07-28
CN1922148B (en) 2012-03-21
ATE483689T1 (en) 2010-10-15
GB0329617D0 (en) 2004-01-28
CN1922148A (en) 2007-02-28
SI1706385T1 (en) 2011-01-31
DK1706385T3 (en) 2011-01-10
UA90461C2 (en) 2010-05-11
DE602004029501D1 (en) 2010-11-18

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