JP2010513567A5 - - Google Patents
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- JP2010513567A5 JP2010513567A5 JP2009543169A JP2009543169A JP2010513567A5 JP 2010513567 A5 JP2010513567 A5 JP 2010513567A5 JP 2009543169 A JP2009543169 A JP 2009543169A JP 2009543169 A JP2009543169 A JP 2009543169A JP 2010513567 A5 JP2010513567 A5 JP 2010513567A5
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- aliphatic
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- disease
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- 150000001875 compounds Chemical class 0.000 claims description 68
- 125000001931 aliphatic group Chemical group 0.000 claims description 44
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 38
- 239000003814 drug Substances 0.000 claims description 36
- 229910052757 nitrogen Inorganic materials 0.000 claims description 30
- 229940079593 drug Drugs 0.000 claims description 26
- 125000000623 heterocyclic group Chemical group 0.000 claims description 26
- 229910052739 hydrogen Inorganic materials 0.000 claims description 26
- 239000001257 hydrogen Substances 0.000 claims description 24
- 239000000203 mixture Substances 0.000 claims description 19
- 125000001072 heteroaryl group Chemical group 0.000 claims description 18
- 239000003795 chemical substances by application Substances 0.000 claims description 16
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 14
- 125000004429 atom Chemical group 0.000 claims description 14
- 201000010099 disease Diseases 0.000 claims description 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 14
- 206010012601 diabetes mellitus Diseases 0.000 claims description 12
- 238000000034 method Methods 0.000 claims description 11
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims description 10
- 125000005843 halogen group Chemical group 0.000 claims description 10
- 229910052717 sulfur Inorganic materials 0.000 claims description 10
- 229940124597 therapeutic agent Drugs 0.000 claims description 10
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 8
- 125000001475 halogen functional group Chemical group 0.000 claims description 8
- 125000005842 heteroatom Chemical group 0.000 claims description 8
- 150000002431 hydrogen Chemical class 0.000 claims description 8
- 201000002364 leukopenia Diseases 0.000 claims description 8
- 231100001022 leukopenia Toxicity 0.000 claims description 8
- 201000006417 multiple sclerosis Diseases 0.000 claims description 8
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 8
- 229910052760 oxygen Inorganic materials 0.000 claims description 8
- 239000001301 oxygen Substances 0.000 claims description 8
- 239000000126 substance Substances 0.000 claims description 8
- 208000020925 Bipolar disease Diseases 0.000 claims description 6
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 6
- 125000001118 alkylidene group Chemical group 0.000 claims description 6
- 125000005605 benzo group Chemical group 0.000 claims description 6
- 201000000980 schizophrenia Diseases 0.000 claims description 6
- 239000011593 sulfur Substances 0.000 claims description 6
- 206010065040 AIDS dementia complex Diseases 0.000 claims description 4
- 208000024827 Alzheimer disease Diseases 0.000 claims description 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 4
- 208000023105 Huntington disease Diseases 0.000 claims description 4
- 206010020880 Hypertrophy Diseases 0.000 claims description 4
- 208000001132 Osteoporosis Diseases 0.000 claims description 4
- 208000018737 Parkinson disease Diseases 0.000 claims description 4
- 125000003118 aryl group Chemical group 0.000 claims description 4
- 239000012472 biological sample Substances 0.000 claims description 4
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 4
- 229910052799 carbon Inorganic materials 0.000 claims description 4
- 210000004413 cardiac myocyte Anatomy 0.000 claims description 4
- 239000002552 dosage form Substances 0.000 claims description 4
- 238000000338 in vitro Methods 0.000 claims description 4
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 4
- 238000011084 recovery Methods 0.000 claims description 4
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 4
- 125000006413 ring segment Chemical group 0.000 claims description 4
- 229920006395 saturated elastomer Polymers 0.000 claims description 4
- -1 —OR Chemical group 0.000 claims description 4
- 208000006011 Stroke Diseases 0.000 claims description 3
- 125000004605 1,2,3,4-tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 claims description 2
- 125000004607 1,2,3,4-tetrahydroquinolinyl group Chemical group N1(CCCC2=CC=CC=C12)* 0.000 claims description 2
- 125000005938 2,3-dihydro-1H-isoindolyl group Chemical group 0.000 claims description 2
- 125000004008 6 membered carbocyclic group Chemical group 0.000 claims description 2
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims description 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 2
- 102000002254 Glycogen Synthase Kinase 3 Human genes 0.000 claims description 2
- 108010014905 Glycogen Synthase Kinase 3 Proteins 0.000 claims description 2
- 108010025020 Nerve Growth Factor Proteins 0.000 claims description 2
- 102000007072 Nerve Growth Factors Human genes 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 239000002260 anti-inflammatory agent Substances 0.000 claims description 2
- 229940121363 anti-inflammatory agent Drugs 0.000 claims description 2
- 230000001028 anti-proliverative effect Effects 0.000 claims description 2
- 125000000928 benzodioxinyl group Chemical group O1C(=COC2=C1C=CC=C2)* 0.000 claims description 2
- 125000002619 bicyclic group Chemical group 0.000 claims description 2
- 230000000973 chemotherapeutic effect Effects 0.000 claims description 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- 229910052736 halogen Inorganic materials 0.000 claims description 2
- 150000002367 halogens Chemical class 0.000 claims description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 2
- 239000002955 immunomodulating agent Substances 0.000 claims description 2
- 229940121354 immunomodulator Drugs 0.000 claims description 2
- 229960003444 immunosuppressant agent Drugs 0.000 claims description 2
- 239000003018 immunosuppressive agent Substances 0.000 claims description 2
- 208000033065 inborn errors of immunity Diseases 0.000 claims description 2
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims description 2
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- 201000010901 lateral sclerosis Diseases 0.000 claims description 2
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 2
- 125000002950 monocyclic group Chemical group 0.000 claims description 2
- 125000002757 morpholinyl group Chemical group 0.000 claims description 2
- 208000005264 motor neuron disease Diseases 0.000 claims description 2
- 239000003900 neurotrophic factor Substances 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 125000004193 piperazinyl group Chemical group 0.000 claims description 2
- 125000003386 piperidinyl group Chemical group 0.000 claims description 2
- 208000028529 primary immunodeficiency disease Diseases 0.000 claims description 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- 239000003981 vehicle Substances 0.000 claims description 2
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 claims 1
- 0 *c1c(*)[n]nc1* Chemical compound *c1c(*)[n]nc1* 0.000 description 2
- 108091000080 Phosphotransferase Proteins 0.000 description 2
- 102000020233 phosphotransferase Human genes 0.000 description 2
- 150000001539 azetidines Chemical class 0.000 description 1
- 238000010835 comparative analysis Methods 0.000 description 1
- 230000031146 intracellular signal transduction Effects 0.000 description 1
- 229940043355 kinase inhibitor Drugs 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US87572906P | 2006-12-19 | 2006-12-19 | |
| US95302707P | 2007-07-31 | 2007-07-31 | |
| PCT/US2007/088058 WO2008077086A1 (en) | 2006-12-19 | 2007-12-19 | Aminopyrimidines useful as inhibitors of protein kinases |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010513567A JP2010513567A (ja) | 2010-04-30 |
| JP2010513567A5 true JP2010513567A5 (enExample) | 2011-01-13 |
Family
ID=39226891
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009543169A Pending JP2010513567A (ja) | 2006-12-19 | 2007-12-19 | プロテインキナーゼの阻害剤として有用なアミノピリミジン |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US8426425B2 (enExample) |
| EP (1) | EP2099787B1 (enExample) |
| JP (1) | JP2010513567A (enExample) |
| AT (1) | ATE474835T1 (enExample) |
| AU (1) | AU2007333650A1 (enExample) |
| CA (1) | CA2673353A1 (enExample) |
| DE (1) | DE602007007985D1 (enExample) |
| ES (1) | ES2347721T3 (enExample) |
| MX (1) | MX2009006690A (enExample) |
| NZ (1) | NZ577768A (enExample) |
| WO (1) | WO2008077086A1 (enExample) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6660731B2 (en) | 2000-09-15 | 2003-12-09 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| US6638926B2 (en) | 2000-09-15 | 2003-10-28 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| CA2432799C (en) | 2000-12-21 | 2008-08-19 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| MY141867A (en) | 2002-06-20 | 2010-07-16 | Vertex Pharma | Substituted pyrimidines useful as protein kinase inhibitors |
| US7601718B2 (en) | 2003-02-06 | 2009-10-13 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of protein kinases |
| WO2007056163A2 (en) | 2005-11-03 | 2007-05-18 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| ES2445791T3 (es) | 2006-10-21 | 2014-03-05 | Abbvie Deutschland Gmbh & Co Kg | Compuestos hetererocíclicos y su uso como inhibidores de la glucógeno sintasa cinasa 3 |
| DE602007004750D1 (de) | 2006-11-02 | 2010-03-25 | Vertex Pharma | Als inhibitoren von proteinkinasen geeignete aminopyridine und aminopyrimidine |
| WO2008077086A1 (en) | 2006-12-19 | 2008-06-26 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as inhibitors of protein kinases |
| MX2009009590A (es) | 2007-03-09 | 2009-11-10 | Vertex Pharma | Aminopirimidinas utiles como inhibidores de proteinas cinasas. |
| NZ579485A (en) | 2007-03-09 | 2012-02-24 | Vertex Pharma | Aminopyrimidines useful as inhibitors of protein kinases |
| EP2134709A1 (en) | 2007-03-09 | 2009-12-23 | Vertex Pharmaceuticals, Inc. | Aminopyridines useful as inhibitors of protein kinases |
| NZ580343A (en) | 2007-04-13 | 2012-03-30 | Vertex Pharma | Aminopyrimidines useful as kinase inhibitors |
| JP5389785B2 (ja) | 2007-05-02 | 2014-01-15 | 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 | キナーゼ阻害剤として有用なチアゾールおよびピラゾール |
| CA2694381A1 (en) | 2007-05-02 | 2008-11-13 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| AU2008282156B2 (en) | 2007-07-31 | 2014-07-17 | Vertex Pharmaceuticals Incorporated | Process for preparing 5-fluoro-1H-pyrazolo [3, 4-b] pyridin-3-amine and derivatives thereof |
| CN101768111B (zh) * | 2009-01-07 | 2012-12-26 | 上海开拓者化学研究管理有限公司 | 一种2-氯-5-氟吡啶-3-甲酸的制备方法 |
| CN103119035B (zh) | 2010-09-27 | 2015-09-30 | 雅培股份有限两合公司 | 杂环化合物和它们作为糖原合成酶激酶-3抑制剂的用途 |
| US9090592B2 (en) | 2010-12-30 | 2015-07-28 | AbbVie Deutschland GmbH & Co. KG | Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors |
| SMT201800608T1 (it) | 2012-04-24 | 2019-01-11 | Vertex Pharma | Inibitori di dna-pk |
| AU2014244555B2 (en) | 2013-03-12 | 2018-06-28 | Vertex Pharmaceuticals Incorporated | DNA-PK inhibitors |
| US9657007B2 (en) * | 2013-09-22 | 2017-05-23 | Calitor Sciences, Llc | Substituted aminopyrimidine compounds and methods of use |
| HUE041877T2 (hu) | 2013-10-17 | 2019-06-28 | Vertex Pharma | (S)-N-Metil-8-(1-((2'-metil-[4,5'-bipirimidin]-6-il)amino)propán-2-il)kinolin-4-karboxamid kokristályai és deuterált származékai DNS-PK inhibitorokként |
| LT3089971T (lt) | 2014-01-01 | 2020-10-12 | Medivation Technologies Llc | Junginiai ir panaudojimo būdai |
| CA2945263A1 (en) | 2014-04-09 | 2015-10-15 | Christopher Rudd | Use of gsk-3 inhibitors or activators which modulate pd-1 or t-bet expression to modulate t cell immunity |
| US10118904B2 (en) | 2015-06-05 | 2018-11-06 | Vertex Pharmaceuticals Incorporated | Triazoles for the treatment of Demyelinating Diseases |
| US11110108B2 (en) | 2016-09-27 | 2021-09-07 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of DNA-damaging agents and DNA-PK inhibitors |
| WO2018106641A1 (en) * | 2016-12-06 | 2018-06-14 | Vertex Pharmaceuticals Incorporated | Pyrazoles for the treatment of demyelinating diseases |
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| DE602007004750D1 (de) * | 2006-11-02 | 2010-03-25 | Vertex Pharma | Als inhibitoren von proteinkinasen geeignete aminopyridine und aminopyrimidine |
| WO2008077086A1 (en) | 2006-12-19 | 2008-06-26 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as inhibitors of protein kinases |
| EP2134709A1 (en) | 2007-03-09 | 2009-12-23 | Vertex Pharmaceuticals, Inc. | Aminopyridines useful as inhibitors of protein kinases |
| MX2009009590A (es) | 2007-03-09 | 2009-11-10 | Vertex Pharma | Aminopirimidinas utiles como inhibidores de proteinas cinasas. |
| NZ579485A (en) | 2007-03-09 | 2012-02-24 | Vertex Pharma | Aminopyrimidines useful as inhibitors of protein kinases |
| JP2010522194A (ja) | 2007-03-20 | 2010-07-01 | 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 | キナーゼ阻害薬として有用なアミノピリミジン |
| EP2148931A2 (en) | 2007-04-17 | 2010-02-03 | Vertex Pharmaceuticals Incorporated | Drug discovery methods for aurora kinase inhibitors |
| CA2688584A1 (en) | 2007-05-02 | 2008-11-13 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| CA2694381A1 (en) | 2007-05-02 | 2008-11-13 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| JP5389785B2 (ja) | 2007-05-02 | 2014-01-15 | 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 | キナーゼ阻害剤として有用なチアゾールおよびピラゾール |
| AU2008257044A1 (en) | 2007-05-24 | 2008-12-04 | Vertex Pharmaceuticals Incorporated | Thiazoles and pyrazoles useful as kinase inhibitors |
| AU2010226400B2 (en) | 2009-03-20 | 2016-07-14 | Vertex Pharmaceuticals Incorporated | Process for making modulators of cystic fibrosis transmembrane conductance regulator |
-
2007
- 2007-12-19 WO PCT/US2007/088058 patent/WO2008077086A1/en not_active Ceased
- 2007-12-19 EP EP07855256A patent/EP2099787B1/en active Active
- 2007-12-19 AT AT07855256T patent/ATE474835T1/de active
- 2007-12-19 JP JP2009543169A patent/JP2010513567A/ja active Pending
- 2007-12-19 AU AU2007333650A patent/AU2007333650A1/en not_active Abandoned
- 2007-12-19 MX MX2009006690A patent/MX2009006690A/es active IP Right Grant
- 2007-12-19 NZ NZ577768A patent/NZ577768A/en not_active IP Right Cessation
- 2007-12-19 ES ES07855256T patent/ES2347721T3/es active Active
- 2007-12-19 DE DE602007007985T patent/DE602007007985D1/de active Active
- 2007-12-19 CA CA002673353A patent/CA2673353A1/en not_active Abandoned
-
2009
- 2009-06-17 US US12/486,235 patent/US8426425B2/en not_active Expired - Fee Related
-
2013
- 2013-03-13 US US13/798,875 patent/US20140256703A1/en not_active Abandoned
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