RS54882B1 - Derivati piramidina kao fak inhibitori - Google Patents
Derivati piramidina kao fak inhibitoriInfo
- Publication number
- RS54882B1 RS54882B1 RS20160420A RSP20160420A RS54882B1 RS 54882 B1 RS54882 B1 RS 54882B1 RS 20160420 A RS20160420 A RS 20160420A RS P20160420 A RSP20160420 A RS P20160420A RS 54882 B1 RS54882 B1 RS 54882B1
- Authority
- RS
- Serbia
- Prior art keywords
- pyrimidin
- ethyl
- ylamino
- phenyl
- methyl
- Prior art date
Links
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- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
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Abstract
Jedinjenja izabrane iz grupe,,A1" N-(2-{2-[2-(4-Metansulfonil-fenilamino)-pirimidin-4-il]-etil}-fenil-N-rnetil-metansulfonamid,,A2" N-Metil-N-(2-{2-[2-(2-okso-1,2,3,4-tetrahidro-hinolin-6-ilamino)-pirimidin-4-il]-etil}-fenil-N-metansulfonamid,,A3" 6-{4-[2-(3-Metan sulfonil-fenil)-etil]-pirimidin-2-ilamino)-3,4-dihidro-1H-hinolin-2-on,,A4" (4-metansulfonil-fenil)-{4-[2-(3-metansulfonil-fenil)-etil]-pirimidin-2-il)-amin,,A5" N-Metil-N-(2-{2-[2-(2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-fenil)-metansulfonamid,,A6" N-Metil-N-(3-(2-[2-(2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-piridin-2-il)-metansulfonamid,,A7" N-Metil-N-(3-{2-[2-(2-okso-1,2,3,4-tetrahidro-hinolin-6-ilamino)-pirimidin-4-il]-etil}-piridin-2-il)-metansulfonamid,,A8" N-(3-{2-[2-(4-metansulfonil-fenilamino)-pirimidin-4-il]-etil}-piridin-2-il)-metilmetansulfonamid,,A9" (2-{2-[2-(2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-fenil)-acetonitril,,A10" N-Metil-N-(3-{2-[2-(2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-piridin-2-il)-acetamid,,A11" (4-Fluor-2-{2-[2-(2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il}-fenil)-acetonitril„A12" N-Metil-N-(3-{2-[2-(2-okso-2,3-dihidro-1H-indol-5 -ilamino)-pirimidin-4-il]-etil}-piridin-2-il)-formamid,,A13" 1-(2{2-[2-(2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-fenil)-ciklobutankarbonitril..A14" N- '2 (3-{2-[2-(2-okso-2,3-dihidro-1 H-indol 5- ilamino)-pirimidin-4-il]-etil}-piridin-2-ilamino)-formamid,,A15" (2-{2-[2-(2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-5-trifluormetil-fenil)-acetonitril,,A16" 3-(3-{2-(2okso-2.3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-piridin-2 il)-azetidin-3-karbonitril,,A17" (2-{2-[2-(2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-5-trifluormetil-fenil)-acetonitril,,A18" (5-Fluor-2-{2-[2-(2-okso-2,3-dihidro-1 H-indol-5- ilamino)-pirimidin-4-il]-etil}-fenil)-acetonitril,,A19" 1-(2-{2-[2-(2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-4- trifluorometil-fenil)-ciklobutankarbonitril,,A20" N-Metil-N-(3-{2-[2-(2-okso-2,3-dihidro-benzoksazol-6-ilamino)-pirimidin-4-il]-etil}-piridin-2-il)-metanesulfonamidA21" N-Metil-N-(3-{2-[2-(1-metil-2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-piridin-2-il)-metanesulfonamid,,A22" N-(3-{2-[2-(3-cijan-fenilamino)-pirimidin-4-il]-etil}-piridin-2-il)-N-metil-metansulfonamid,,A24" N-Metil-N-[3-(2-{2-[(6-okso-1,6-dihidro-piradizin-3-ilmetil)-amino]-pirimidin-4-il}-piridin-2-il]-metansulfonamid,,A25" N-(3-{2-[2-(1,3-dimetil-2-okso-2,3-diidro-1-H-benzimidazol-5-ilamino)-pirimidin-4-il]-etil}-piridin-2-il)-N-metil-metansulfonamid,,A26" N-(3-{[5-cijan-2-(2-okso-2,3-dihidro-benzoksazol-6-ilamino)-pirimidin-4-ilamino]-metil}-piridin-2-il)-N-metil-metansulfonamid,,A27" N-Metil-N-(2-{2-[(2-okso-2,3-dihidro-benzoksazo-6-ilamino)-pirimidin-4-il]-etil}-fenil)-metansulfonamid,,A28" N-(2-{2-[2-(3-cijan-fenilamino)-pirimidin-4-il]-etil}-fenil)-N-metil-metansulfonamid,,A29" N-(2-{2-[2-(3-cijan-4-fluor-fenilamino)-pirimidin-4-il]-etil}-fenil)-N-metil-metansulfonamid,,A30" N-Metil-N-(2-{2-[(2-okso-2,3-dihidro-benzotiazol-5-ilamino)-pirimidin-4-il]-etil}-fenil)-metansulfonamid,,A31" N-(2-{2-(1-Acetil-2,3-dihidro-1H-indol-5-ilamino)- pirimidin-4-il]-etil}-fenil)-N-metil-metansulfonamid,,A32" 2-[3-(4-{2-[2-(Metansulfonil-metil-amino)-fenil]-etil}-pirimidin-2-ilamino)-fenil]-N-metil-acetamid,,A33" N-Metil-N-[2-(2-{2-[4-(3-okso-morfoln-4-il)-fenilamino]-pirimidin-4-il}-etil)-fenil)-metansulfonamid,,A34" N-[4-(4-{2-[2-(Metansulfonil-metil-amino)-fenil]-etil}-pirimidin-2-ilamino)-fenil]-nikotinamid,,A35" N-Metil-N-[2-(2-{2-[4-(2-okso-pirolidin-1-il)-fenilamino-]-pirimidin-4-il}-etil]-metansulfonamid,,A36" N-[2-(2-{2-[3,5-dihlor-4-(2-okso-pirolidin-1-il)-fenilamino]-pirimidin-4-il}-etil]-fenil]-N-metil-metansulfonamid,,A37" N-[2-(2-{2-[3-cijan-4-(2-okso-piperidin-1-il)-fenilamino]-pirimidin-4-il}-etil]-fenil]-N-metil-metansulfonamid,,A38" N-[2-(2-{2-[4-(1,3-diokso-1,3-dihidro-izoindol-2-il)- fenilamino]-pirimidin-4-N}-etil]-fenil]-N-metil-metansulfonamid,,A39" N-Metil-N-[3-(2-{2-[4-(2-okso-pirolidin-1-il)- fenilamino]-pirimidin-4-il}-etil)-piridin-2-il]-metansulfonamid,,A40" N-[4-(4-{2-[2-(Metansulfonil-metil-amino)-piridin-3-il]-etil}-pirimidin-2-ilamino)-fenil]-nikotinamid,A41" N-Metil-N-[3-(2-{2-[4-(2-okso-morfolin-4-il)- fenilamino]-pirimidin-4-il}-etil)-piridin-2-il]-metansuifonamid,A42" N-[3-(2-{2-[3-cijan-4-(2-okso-piperidin-1-il)- fenilamino]-pirimidin-4-il}-etil)-piridin-2-il]-N-metil-metansulfonamid,,A43" N-[3-(2-{2-[4-(1,3-diokso-1,3-dihidro-izoindol-2-il) fenilamino]-pirimidin-4-il}-etil)-piridin-2-il)-N-metil-metansulfonamid,,A44" N-Metil-N-(5-metil-3-{2-[2-(2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-piridin-2-il)-metansulfonamid 1-(4-fluor-2-{2-[2-(2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-fenil)-ciklobutankarbonitril,,A46" 1-(5-fluor-2-{2-[2-(2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-fenil)-ciklobutankarbonitril,,A47" 1-(2-{2-[2-(2-okso-2,3-dihidro-1H-indol-5-ilamino)-pirimidin-4-il]-etil}-5-trifluormetil-fenil)- ciklobutankarbonitril,,A48" (5-Fluor-4-fenetil-pirimidin-2-il)-fenil-amin,,A49" (5-Metil-4-fenetil-pirimidin-2-il)-fenil-amin,,A50" (5-fenetil-5-trifluormetil-pirimidin-2-il)-fenil-amin,,A52" (5-Brom-4-fenetil-pirimidin-2-il)-fenil-amin,,A56" 6-{5-Fluor-4-[2-(4-fluor-fenil)-etil]-pirimidin-2-ilamino}-3,4-dihidro-1H-hinolin-2-on,,A65" 6-{4-[2-(4-fluor-fenil)-etil]-5-metil-pirimidin-2-ilamino}-3,4-dihidro-1H-hinolin-2-on,,A71" [5-(1-Metil-1H-pirazol-4-il)-4-fenetil-pirimidin-2-il]-fenil-amin,,A74" [5-{4-[2-(4-Fluor-fenil)-etil]-5-trifluormetil-pirimidin-2-ilamino}-1,3-dihidro-indol-2-on,,A77" 6-{4-[2-(4-Fluor-fenil)-etil]-5-trifluormetil-pirimidin-2-ilamino}-3,4-dihidro-1H-hinolin-2-on„A101" 6-(5-Brom-4-fenetil-pirimidin-2-ilamino(-3,4-dihidro-1H-hinolin-2-on„A102" 5-(4-fenetil-5-trifluormetil-pirimidin-2-ilamino)-1,3-dihidro-indol-2-on„A103" 6-(4-fenetil-5-trifluormetil-pirimidin-2-ilamino)-3,4-dihidro-1H-hinolin-2-on„A104" 6-(5-metii-4-{2-[3-(propan-1-sulfonil)-fenil]-etil}-pirimidin-2-ilamino)-3,4-dihidro-1H-hinolin-2-on„A105" 6-(5-Fluor-4-{2-[3-(propan-1-sulfonil)-fenil]-etil}-pirimidin-2-ilamino)-3,4-dihidro-1H-hinolin-2-on„A106" [6-(4-terc.-Butil-fenoksi)-piridin-3-il]-(5-fluor-4-fenetil-pirimidin-2-il)-amin„A107" (5-Fluor-4-fenetil-pirimidin-2-il)-(6-trifluormetil-piridin-3-il)-amin„A108" (5-Fluor-4-fenetil-pirimidin-2-il)-(6-fluor-piridin-3-il)-amin„A109" 5-(5-Fluor-4-fenetil-pirimidin-2-ilamino)-piridin-2-karbonitril„A110" N-[5-(5-Fluor-fenetil-pirimidin-2-ilamino)-piridin-2-il]-acetamid„A111" N-Metil-N-(2-{2-[2-(2-okso-2,3 dihidro-1H-indol-5-ilamino)-5-trifluormetil-pirimidin-4-il]etil)-fenil)-metansulfonamidkao i farmaceutski primenjene soli, tautomera i stereoizomera, uključujući njihove smese u svim odnosima.Prijava sadrži još 2 patentna zahteva.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE102010034699A DE102010034699A1 (de) | 2010-08-18 | 2010-08-18 | Pyrimidinderivate |
PCT/EP2011/003597 WO2012022408A1 (de) | 2010-08-18 | 2011-07-19 | Pyrimidinderivate als fak inhibitoren |
EP11743438.1A EP2606034B1 (de) | 2010-08-18 | 2011-07-19 | Pyrimidinderivate als fak inhibitoren |
Publications (1)
Publication Number | Publication Date |
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RS54882B1 true RS54882B1 (sr) | 2016-10-31 |
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RS20160420A RS54882B1 (sr) | 2010-08-18 | 2011-07-19 | Derivati piramidina kao fak inhibitori |
Country Status (17)
Country | Link |
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US (1) | US8906916B2 (sr) |
EP (1) | EP2606034B1 (sr) |
JP (2) | JP6049617B2 (sr) |
CN (1) | CN103052627B (sr) |
AR (1) | AR082722A1 (sr) |
AU (1) | AU2011291110B2 (sr) |
CA (1) | CA2808540C (sr) |
DE (1) | DE102010034699A1 (sr) |
DK (1) | DK2606034T3 (sr) |
ES (1) | ES2572740T3 (sr) |
HR (1) | HRP20160562T1 (sr) |
HU (1) | HUE027846T2 (sr) |
IL (1) | IL224751A (sr) |
PL (1) | PL2606034T3 (sr) |
RS (1) | RS54882B1 (sr) |
SI (1) | SI2606034T1 (sr) |
WO (1) | WO2012022408A1 (sr) |
Families Citing this family (13)
Publication number | Priority date | Publication date | Assignee | Title |
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DE102010034699A1 (de) * | 2010-08-18 | 2012-02-23 | Merck Patent Gmbh | Pyrimidinderivate |
US20130324532A1 (en) * | 2011-02-17 | 2013-12-05 | Cancer Therapeutics Crc Pty Limited | Fak inhibitors |
DK2675794T3 (da) | 2011-02-17 | 2019-05-06 | Cancer Therapeutics Crc Pty Ltd | Selektive fak-inhibitorer |
US9013997B2 (en) * | 2012-06-01 | 2015-04-21 | Broadcom Corporation | System for performing distributed data cut-through |
WO2014027199A1 (en) * | 2012-08-14 | 2014-02-20 | Cancer Therapeutics Crc Pty Ltd | Fak and flt3 inhibitors |
AU2013302319A1 (en) * | 2012-08-17 | 2015-02-26 | Cancer Therapeutics Crc Pty Limited | VEGFR3 inhibitors |
JP2015524826A (ja) * | 2012-08-17 | 2015-08-27 | キャンサー・セラピューティクス・シーアールシー・ピーティーワイ・リミテッド | Vegfr3阻害剤 |
TW201412740A (zh) * | 2012-09-20 | 2014-04-01 | Bayer Pharma AG | 經取代之吡咯并嘧啶胺基苯并噻唑酮 |
JPWO2014174745A1 (ja) * | 2013-04-26 | 2017-02-23 | 国立大学法人京都大学 | Eg5阻害剤 |
WO2015054477A1 (en) | 2013-10-09 | 2015-04-16 | The General Hospital Corporation | Methods of diagnosing and treating b cell acute lymphoblastic leukemia |
WO2015123722A1 (en) * | 2014-02-19 | 2015-08-27 | Bionomics Limited | Inhibitors |
EP4070795A1 (en) * | 2014-08-25 | 2022-10-12 | Salk Institute for Biological Studies | Novel ulk1 inhibitors and methods using same |
WO2019117813A1 (en) * | 2017-12-15 | 2019-06-20 | National University Of Singapore | Focal adhesion kinase targeted therapeutics for the treatment of glaucoma and fibrosis |
Family Cites Families (23)
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GB9624482D0 (en) | 1995-12-18 | 1997-01-15 | Zeneca Phaema S A | Chemical compounds |
IL125686A (en) | 1996-02-13 | 2002-11-10 | Zeneca Ltd | Quinazoline derivatives, processes for their preparation, pharmaceutical preparations containing them and their use in the manufacture of a drug with an anti-angiogenic effect and / or an effect of reducing vascular permeability |
WO1997032856A1 (en) | 1996-03-05 | 1997-09-12 | Zeneca Limited | 4-anilinoquinazoline derivatives |
GB9718972D0 (en) | 1996-09-25 | 1997-11-12 | Zeneca Ltd | Chemical compounds |
GB9714249D0 (en) | 1997-07-08 | 1997-09-10 | Angiogene Pharm Ltd | Vascular damaging agents |
GB9900334D0 (en) | 1999-01-07 | 1999-02-24 | Angiogene Pharm Ltd | Tricylic vascular damaging agents |
GB9900752D0 (en) | 1999-01-15 | 1999-03-03 | Angiogene Pharm Ltd | Benzimidazole vascular damaging agents |
IL152682A0 (en) | 2000-05-31 | 2003-06-24 | Astrazeneca Ab | Indole derivatives with vascular damaging activity |
WO2002004434A1 (en) | 2000-07-07 | 2002-01-17 | Angiogene Pharmaceuticals Limited | Colchinol derivatives as vascular damaging agents |
RU2003103603A (ru) | 2000-07-07 | 2004-08-20 | Энджиоджен Фармасьютикалз Лимитед (Gb) | Производные колхинола в качестве ингибиторов ангиогенеза |
ATE407678T1 (de) * | 2001-10-17 | 2008-09-15 | Boehringer Ingelheim Pharma | Pyrimidinderivate, arzneimittel enthaltend diese verbindungen, deren verwendung und verfahren zu ihrer herstellung |
AU2003224257A1 (en) * | 2002-04-09 | 2003-10-27 | Astex Technology Limited | Heterocyclic compounds and their use as modulators of p38 map kinase |
UA80767C2 (en) * | 2002-12-20 | 2007-10-25 | Pfizer Prod Inc | Pyrimidine derivatives for the treatment of abnormal cell growth |
AU2003285614B2 (en) | 2002-12-20 | 2009-05-14 | Pfizer Products, Inc. | Pyrimidine derivatives for the treatment of abnormal cell growth |
KR20080004585A (ko) * | 2005-04-08 | 2008-01-09 | 바이엘 파마슈티칼스 코포레이션 | 피리미딘 유도체 및 암의 치료에서의 이의 용도 |
EP2134689B1 (en) | 2007-03-16 | 2014-04-23 | The Scripps Research Institute | Inhibitors of focal adhesion kinase |
WO2009105498A1 (en) | 2008-02-19 | 2009-08-27 | Smithkline Beecham Corporation | Anilinopyridines as inhibitors of fak |
MX360970B (es) * | 2008-06-27 | 2018-11-23 | Avila Therapeutics Inc | Compuestos de heteroarilo y usos de los mismos. |
UY32240A (es) | 2008-11-14 | 2010-06-30 | Boeringer Ingelheim Kg | Nuevas 2,4-diaminopirimidinas, sus sales farmacéuticamente aceptables, composiciones conteniéndolas y aplicaciones. |
AR074209A1 (es) * | 2008-11-24 | 2010-12-29 | Boehringer Ingelheim Int | Derivados de pirimidina utiles para el tratamiento del cancer |
DE102010034699A1 (de) * | 2010-08-18 | 2012-02-23 | Merck Patent Gmbh | Pyrimidinderivate |
DK2675794T3 (da) * | 2011-02-17 | 2019-05-06 | Cancer Therapeutics Crc Pty Ltd | Selektive fak-inhibitorer |
US20130324532A1 (en) * | 2011-02-17 | 2013-12-05 | Cancer Therapeutics Crc Pty Limited | Fak inhibitors |
-
2010
- 2010-08-18 DE DE102010034699A patent/DE102010034699A1/de not_active Withdrawn
-
2011
- 2011-07-19 AU AU2011291110A patent/AU2011291110B2/en not_active Ceased
- 2011-07-19 WO PCT/EP2011/003597 patent/WO2012022408A1/de active Application Filing
- 2011-07-19 ES ES11743438.1T patent/ES2572740T3/es active Active
- 2011-07-19 US US13/817,251 patent/US8906916B2/en not_active Expired - Fee Related
- 2011-07-19 JP JP2013524362A patent/JP6049617B2/ja not_active Expired - Fee Related
- 2011-07-19 RS RS20160420A patent/RS54882B1/sr unknown
- 2011-07-19 SI SI201130848A patent/SI2606034T1/sl unknown
- 2011-07-19 CN CN201180039922.8A patent/CN103052627B/zh not_active Expired - Fee Related
- 2011-07-19 HU HUE11743438A patent/HUE027846T2/en unknown
- 2011-07-19 PL PL11743438T patent/PL2606034T3/pl unknown
- 2011-07-19 EP EP11743438.1A patent/EP2606034B1/de active Active
- 2011-07-19 DK DK11743438.1T patent/DK2606034T3/en active
- 2011-07-19 CA CA2808540A patent/CA2808540C/en not_active Expired - Fee Related
- 2011-08-18 AR ARP110102997A patent/AR082722A1/es unknown
-
2013
- 2013-02-17 IL IL224751A patent/IL224751A/en active IP Right Grant
-
2016
- 2016-05-24 HR HRP20160562TT patent/HRP20160562T1/hr unknown
- 2016-08-04 JP JP2016153334A patent/JP6441861B2/ja not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
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HRP20160562T1 (hr) | 2016-06-17 |
JP6441861B2 (ja) | 2018-12-19 |
CN103052627A (zh) | 2013-04-17 |
AU2011291110A1 (en) | 2013-04-04 |
HUE027846T2 (en) | 2016-11-28 |
CA2808540A1 (en) | 2012-02-23 |
CA2808540C (en) | 2018-09-11 |
US8906916B2 (en) | 2014-12-09 |
CN103052627B (zh) | 2015-08-19 |
AR082722A1 (es) | 2012-12-26 |
EP2606034A1 (de) | 2013-06-26 |
JP6049617B2 (ja) | 2016-12-21 |
ES2572740T3 (es) | 2016-06-02 |
US20130158005A1 (en) | 2013-06-20 |
IL224751A (en) | 2015-03-31 |
AU2011291110B2 (en) | 2015-01-22 |
EP2606034B1 (de) | 2016-03-09 |
PL2606034T3 (pl) | 2016-07-29 |
JP2013534227A (ja) | 2013-09-02 |
DE102010034699A1 (de) | 2012-02-23 |
WO2012022408A1 (de) | 2012-02-23 |
SI2606034T1 (sl) | 2016-07-29 |
DK2606034T3 (en) | 2016-05-02 |
JP2017036268A (ja) | 2017-02-16 |
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