JP2008517984A5 - - Google Patents
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- JP2008517984A5 JP2008517984A5 JP2007538500A JP2007538500A JP2008517984A5 JP 2008517984 A5 JP2008517984 A5 JP 2008517984A5 JP 2007538500 A JP2007538500 A JP 2007538500A JP 2007538500 A JP2007538500 A JP 2007538500A JP 2008517984 A5 JP2008517984 A5 JP 2008517984A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- hydrogen
- hydrocarbyl
- hydroxy
- cyano
- Prior art date
- Legal status (The legal status 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 status listed.)
- Granted
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- 229910052739 hydrogen Inorganic materials 0.000 claims 60
- 239000001257 hydrogen Substances 0.000 claims 60
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 58
- 125000001424 substituent group Chemical group 0.000 claims 49
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 48
- 150000001875 compounds Chemical class 0.000 claims 47
- -1 hydroxy, cyano, amino, methylamino, dimethylamino Chemical group 0.000 claims 46
- 229910052760 oxygen Inorganic materials 0.000 claims 46
- 125000004432 carbon atom Chemical group C* 0.000 claims 45
- 229910052757 nitrogen Inorganic materials 0.000 claims 35
- 125000000623 heterocyclic group Chemical group 0.000 claims 34
- 229910052736 halogen Inorganic materials 0.000 claims 33
- 150000002367 halogens Chemical class 0.000 claims 33
- 150000002431 hydrogen Chemical group 0.000 claims 33
- 125000004093 cyano group Chemical group *C#N 0.000 claims 31
- 125000001072 heteroaryl group Chemical group 0.000 claims 28
- 229910052731 fluorine Inorganic materials 0.000 claims 26
- 239000011737 fluorine Substances 0.000 claims 26
- 229910052717 sulfur Inorganic materials 0.000 claims 26
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 25
- 125000005647 linker group Chemical group 0.000 claims 24
- 229910052799 carbon Inorganic materials 0.000 claims 23
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 22
- 125000003118 aryl group Chemical group 0.000 claims 21
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 20
- 125000005842 heteroatom Chemical group 0.000 claims 20
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 18
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 17
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 16
- 229910052801 chlorine Inorganic materials 0.000 claims 16
- 239000000460 chlorine Substances 0.000 claims 16
- 125000002837 carbocyclic group Chemical group 0.000 claims 14
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 13
- 125000002252 acyl group Chemical group 0.000 claims 11
- 125000001620 monocyclic carbocycle group Chemical group 0.000 claims 11
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 10
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 10
- 229910052794 bromium Inorganic materials 0.000 claims 10
- 125000002950 monocyclic group Chemical group 0.000 claims 10
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims 10
- 125000004423 acyloxy group Chemical group 0.000 claims 9
- 125000004043 oxo group Chemical group O=* 0.000 claims 9
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- 125000004076 pyridyl group Chemical group 0.000 claims 8
- 125000002619 bicyclic group Chemical group 0.000 claims 7
- 125000004122 cyclic group Chemical group 0.000 claims 7
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 7
- 125000004430 oxygen atom Chemical group O* 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 229930195734 saturated hydrocarbon Natural products 0.000 claims 7
- 239000012453 solvate Substances 0.000 claims 7
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 6
- SQQWBSBBCSFQGC-JLHYYAGUSA-N ubiquinone-2 Chemical compound COC1=C(OC)C(=O)C(C\C=C(/C)CCC=C(C)C)=C(C)C1=O SQQWBSBBCSFQGC-JLHYYAGUSA-N 0.000 claims 6
- 125000004429 atom Chemical group 0.000 claims 5
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 5
- 150000001204 N-oxides Chemical class 0.000 claims 4
- 125000003282 alkyl amino group Chemical group 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 125000001153 fluoro group Chemical group F* 0.000 claims 4
- 230000002265 prevention Effects 0.000 claims 4
- 125000006164 6-membered heteroaryl group Chemical group 0.000 claims 3
- 102000008130 Cyclic AMP-Dependent Protein Kinases Human genes 0.000 claims 3
- 108010049894 Cyclic AMP-Dependent Protein Kinases Proteins 0.000 claims 3
- 108091008611 Protein Kinase B Proteins 0.000 claims 3
- 102000005765 Proto-Oncogene Proteins c-akt Human genes 0.000 claims 3
- 125000004442 acylamino group Chemical group 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 125000006518 morpholino carbonyl group Chemical group [H]C1([H])OC([H])([H])C([H])([H])N(C(*)=O)C1([H])[H] 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 2
- KDLHZDBZIXYQEI-UHFFFAOYSA-N Palladium Chemical compound [Pd] KDLHZDBZIXYQEI-UHFFFAOYSA-N 0.000 claims 2
- 230000002159 abnormal effect Effects 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 claims 2
- 238000006243 chemical reaction Methods 0.000 claims 2
- 125000006317 cyclopropyl amino group Chemical group 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 230000001419 dependent effect Effects 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims 2
- 241001553014 Myrsine salicina Species 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 125000005621 boronate group Chemical group 0.000 claims 1
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical group OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 claims 1
- 239000003054 catalyst Substances 0.000 claims 1
- 230000030833 cell death Effects 0.000 claims 1
- 230000010261 cell growth Effects 0.000 claims 1
- 125000004188 dichlorophenyl group Chemical group 0.000 claims 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- PNDPGZBMCMUPRI-UHFFFAOYSA-N iodine Chemical compound II PNDPGZBMCMUPRI-UHFFFAOYSA-N 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 230000000269 nucleophilic effect Effects 0.000 claims 1
- 229910052763 palladium Inorganic materials 0.000 claims 1
- 239000003197 protein kinase B inhibitor Substances 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- YOIAWAIKYVEKMF-UHFFFAOYSA-N trifluoromethanesulfonic acid Chemical group OS(=O)(=O)C(F)(F)F.OS(=O)(=O)C(F)(F)F YOIAWAIKYVEKMF-UHFFFAOYSA-N 0.000 claims 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US62182104P | 2004-10-25 | 2004-10-25 | |
| GB0423655A GB0423655D0 (en) | 2004-10-25 | 2004-10-25 | Pharmaceutical compounds |
| GB0423655.0 | 2004-10-25 | ||
| US60/621,821 | 2004-10-25 | ||
| US68411905P | 2005-05-24 | 2005-05-24 | |
| US60/684,119 | 2005-05-24 | ||
| PCT/GB2005/004119 WO2006046024A1 (en) | 2004-10-25 | 2005-10-25 | Ortho- condensed pyridine and pyrimidine derivatives (e. g. purines) as protein kinases inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2008517984A JP2008517984A (ja) | 2008-05-29 |
| JP2008517984A5 true JP2008517984A5 (enExample) | 2008-12-18 |
| JP5128284B2 JP5128284B2 (ja) | 2013-01-23 |
Family
ID=35715573
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007538500A Expired - Lifetime JP5128284B2 (ja) | 2004-10-25 | 2005-10-25 | プロテインキナーゼ阻害剤としてのオルト縮合ピリジンおよびピリミジン誘導体(例えばプリン類) |
Country Status (14)
| Country | Link |
|---|---|
| US (3) | US8546407B2 (enExample) |
| EP (2) | EP2272517B2 (enExample) |
| JP (1) | JP5128284B2 (enExample) |
| AR (1) | AR051342A1 (enExample) |
| AT (1) | ATE513549T1 (enExample) |
| CY (1) | CY1115946T1 (enExample) |
| DK (1) | DK2272517T4 (enExample) |
| ES (1) | ES2523266T5 (enExample) |
| MY (1) | MY179032A (enExample) |
| PL (1) | PL2272517T5 (enExample) |
| PT (1) | PT2272517E (enExample) |
| SI (1) | SI2272517T2 (enExample) |
| UY (1) | UY29176A1 (enExample) |
| WO (1) | WO2006046024A1 (enExample) |
Families Citing this family (74)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MY179032A (en) * | 2004-10-25 | 2020-10-26 | Cancer Research Tech Ltd | Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors |
| US8921376B2 (en) * | 2005-05-20 | 2014-12-30 | Vertex Pharmaceuticals Incorporated | Pyrrolopyridines useful as inhibitors of protein kinase |
| CN102127078A (zh) | 2005-07-14 | 2011-07-20 | 安斯泰来制药株式会社 | Janus激酶3的杂环类抑制剂 |
| US8163767B2 (en) | 2005-07-14 | 2012-04-24 | Astellas Pharma Inc. | Heterocyclic Janus Kinase 3 inhibitors |
| DE102005037733A1 (de) * | 2005-08-10 | 2007-02-15 | Merck Patent Gmbh | Adeninderivate |
| WO2007038215A1 (en) | 2005-09-22 | 2007-04-05 | Incyte Corporation | Tetracyclic inhibitors of janus kinases |
| ATE525374T1 (de) | 2005-12-13 | 2011-10-15 | Incyte Corp | Heteroarylsubstituierte pyrroloä2,3-büpyridine und pyrroloä2,3-büpyrimidine als januskinaseinhibitoren |
| WO2007084667A2 (en) * | 2006-01-19 | 2007-07-26 | Osi Pharmaceutical, Inc. | Fused heterobicyclic kinase inhibitors |
| JP2009536620A (ja) * | 2006-04-25 | 2009-10-15 | アステックス、セラピューティックス、リミテッド | 医薬組み合わせ物 |
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| EP2029592A1 (en) * | 2006-04-25 | 2009-03-04 | Astex Therapeutics Limited | Pharmaceutical compounds |
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| US8227603B2 (en) | 2006-08-01 | 2012-07-24 | Cytokinetics, Inc. | Modulating skeletal muscle |
| PT2583970E (pt) | 2006-08-02 | 2016-02-08 | Cytokinetics Inc | Certas entidades químicas, composições e métodos compreendendo imidazopirimidinas |
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| AR064416A1 (es) * | 2006-12-21 | 2009-04-01 | Cancer Rec Tech Ltd | Derivados de purina, piridina y pirimidina condensadas con heterociclos, moduladores de pka y/o pkb, composiciones farmaceuticas que los contienen, y usos para el tratamiento de enfermedades hiperproliferativas. |
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| EP2355821A1 (en) | 2008-11-11 | 2011-08-17 | Eli Lilly and Company | P70 s6 kinase inhibitor and egfr inhibitor combination therapy |
| AR074072A1 (es) | 2008-11-11 | 2010-12-22 | Lilly Co Eli | Compuesto de imidazol -piperidin -pirrol-pirimidin-6-ona, composicion farmaceutica que lo comprende y su uso para preparar un medicamento util para tratar el glioblastoma multiforme |
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| JP6172939B2 (ja) | 2009-05-22 | 2017-08-02 | インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation | Jak阻害薬としての3−[4−(7h−ピロロ[2,3−d]ピリミジン−4−イル)−1h−ピラゾール−1−イル]オクタン−またはヘプタン−ニトリル |
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| KR102303885B1 (ko) | 2010-05-21 | 2021-09-24 | 인사이트 홀딩스 코포레이션 | Jak 저해제에 대한 국소 제형 |
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-
2005
- 2005-10-21 MY MYPI20054963A patent/MY179032A/en unknown
- 2005-10-24 UY UY29176A patent/UY29176A1/es not_active IP Right Cessation
- 2005-10-25 DK DK10184485.0T patent/DK2272517T4/da active
- 2005-10-25 SI SI200531910T patent/SI2272517T2/sl unknown
- 2005-10-25 WO PCT/GB2005/004119 patent/WO2006046024A1/en not_active Ceased
- 2005-10-25 EP EP10184485.0A patent/EP2272517B2/en not_active Expired - Lifetime
- 2005-10-25 ES ES10184485.0T patent/ES2523266T5/es not_active Expired - Lifetime
- 2005-10-25 PL PL10184485T patent/PL2272517T5/pl unknown
- 2005-10-25 PT PT101844850T patent/PT2272517E/pt unknown
- 2005-10-25 AT AT05797685T patent/ATE513549T1/de not_active IP Right Cessation
- 2005-10-25 AR ARP050104467 patent/AR051342A1/es active IP Right Grant
- 2005-10-25 EP EP20050797685 patent/EP1812004B1/en not_active Expired - Lifetime
- 2005-10-25 US US11/577,963 patent/US8546407B2/en active Active
- 2005-10-25 JP JP2007538500A patent/JP5128284B2/ja not_active Expired - Lifetime
-
2013
- 2013-09-04 US US14/017,814 patent/US8809336B2/en not_active Expired - Lifetime
-
2014
- 2014-06-20 US US14/310,475 patent/US9006430B2/en not_active Expired - Lifetime
- 2014-11-27 CY CY20141100991T patent/CY1115946T1/el unknown
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