JP2010526098A5 - - Google Patents
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- JP2010526098A5 JP2010526098A5 JP2010506664A JP2010506664A JP2010526098A5 JP 2010526098 A5 JP2010526098 A5 JP 2010526098A5 JP 2010506664 A JP2010506664 A JP 2010506664A JP 2010506664 A JP2010506664 A JP 2010506664A JP 2010526098 A5 JP2010526098 A5 JP 2010526098A5
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- JP
- Japan
- Prior art keywords
- ring
- compound
- compound according
- aliphatic
- cancer
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims description 127
- 125000001931 aliphatic group Chemical group 0.000 claims description 42
- 125000005842 heteroatom Chemical group 0.000 claims description 34
- 229910052757 nitrogen Inorganic materials 0.000 claims description 30
- 229910052760 oxygen Inorganic materials 0.000 claims description 26
- 229910052717 sulfur Inorganic materials 0.000 claims description 26
- 125000000217 alkyl group Chemical group 0.000 claims description 24
- 125000004429 atom Chemical group 0.000 claims description 22
- 125000000623 heterocyclic group Chemical group 0.000 claims description 22
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 20
- 125000005843 halogen group Chemical group 0.000 claims description 14
- 239000000203 mixture Substances 0.000 claims description 14
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 14
- 239000003814 drug Substances 0.000 claims description 12
- 125000001072 heteroaryl group Chemical group 0.000 claims description 12
- 229910052739 hydrogen Inorganic materials 0.000 claims description 12
- 238000000034 method Methods 0.000 claims description 12
- 229940124597 therapeutic agent Drugs 0.000 claims description 12
- 125000001118 alkylidene group Chemical group 0.000 claims description 10
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 8
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 8
- 229910052799 carbon Inorganic materials 0.000 claims description 8
- 125000001475 halogen functional group Chemical group 0.000 claims description 8
- 125000002950 monocyclic group Chemical group 0.000 claims description 8
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 8
- 239000001301 oxygen Chemical group 0.000 claims description 8
- 150000003839 salts Chemical class 0.000 claims description 8
- 239000011593 sulfur Chemical group 0.000 claims description 8
- 206010028980 Neoplasm Diseases 0.000 claims description 7
- 201000011510 cancer Diseases 0.000 claims description 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 7
- 208000035475 disorder Diseases 0.000 claims description 7
- 230000002062 proliferating effect Effects 0.000 claims description 7
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims description 6
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 6
- 239000002067 L01XE06 - Dasatinib Substances 0.000 claims description 6
- 239000005536 L01XE08 - Nilotinib Substances 0.000 claims description 6
- 125000003118 aryl group Chemical group 0.000 claims description 6
- 125000004122 cyclic group Chemical group 0.000 claims description 6
- 229960002448 dasatinib Drugs 0.000 claims description 6
- 239000003112 inhibitor Substances 0.000 claims description 6
- HHZIURLSWUIHRB-UHFFFAOYSA-N nilotinib Chemical compound C1=NC(C)=CN1C1=CC(NC(=O)C=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)=CC(C(F)(F)F)=C1 HHZIURLSWUIHRB-UHFFFAOYSA-N 0.000 claims description 6
- 229960001346 nilotinib Drugs 0.000 claims description 6
- 229920006395 saturated elastomer Polymers 0.000 claims description 6
- 201000001441 melanoma Diseases 0.000 claims description 5
- -1 Each R 9 is —R ′ Chemical group 0.000 claims description 4
- ZBNZXTGUTAYRHI-UHFFFAOYSA-N Dasatinib Chemical compound C=1C(N2CCN(CCO)CC2)=NC(C)=NC=1NC(S1)=NC=C1C(=O)NC1=C(C)C=CC=C1Cl ZBNZXTGUTAYRHI-UHFFFAOYSA-N 0.000 claims description 4
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims description 4
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 4
- 239000005517 L01XE01 - Imatinib Substances 0.000 claims description 4
- 239000005551 L01XE03 - Erlotinib Substances 0.000 claims description 4
- 229930012538 Paclitaxel Natural products 0.000 claims description 4
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 claims description 4
- 206010038389 Renal cancer Diseases 0.000 claims description 4
- 239000012472 biological sample Substances 0.000 claims description 4
- 210000003169 central nervous system Anatomy 0.000 claims description 4
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims description 4
- 229960004316 cisplatin Drugs 0.000 claims description 4
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 4
- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims description 4
- 125000001153 fluoro group Chemical group F* 0.000 claims description 4
- 229940080856 gleevec Drugs 0.000 claims description 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 4
- KTUFNOKKBVMGRW-UHFFFAOYSA-N imatinib Chemical compound C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)C=C1 KTUFNOKKBVMGRW-UHFFFAOYSA-N 0.000 claims description 4
- 201000010982 kidney cancer Diseases 0.000 claims description 4
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 4
- 229960001592 paclitaxel Drugs 0.000 claims description 4
- 125000006413 ring segment Chemical group 0.000 claims description 4
- 229940120982 tarceva Drugs 0.000 claims description 4
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims description 4
- 206010025323 Lymphomas Diseases 0.000 claims description 3
- 206010029260 Neuroblastoma Diseases 0.000 claims description 3
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 3
- 102000001253 Protein Kinase Human genes 0.000 claims description 3
- 230000002401 inhibitory effect Effects 0.000 claims description 3
- 208000032839 leukemia Diseases 0.000 claims description 3
- 201000000050 myeloid neoplasm Diseases 0.000 claims description 3
- 108060006633 protein kinase Proteins 0.000 claims description 3
- 125000006645 (C3-C4) cycloalkyl group Chemical group 0.000 claims description 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 2
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 claims description 2
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical compound C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 claims description 2
- WEVYNIUIFUYDGI-UHFFFAOYSA-N 3-[6-[4-(trifluoromethoxy)anilino]-4-pyrimidinyl]benzamide Chemical compound NC(=O)C1=CC=CC(C=2N=CN=C(NC=3C=CC(OC(F)(F)F)=CC=3)C=2)=C1 WEVYNIUIFUYDGI-UHFFFAOYSA-N 0.000 claims description 2
- 206010005003 Bladder cancer Diseases 0.000 claims description 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- KLWPJMFMVPTNCC-UHFFFAOYSA-N Camptothecin Natural products CCC1(O)C(=O)OCC2=C1C=C3C4Nc5ccccc5C=C4CN3C2=O KLWPJMFMVPTNCC-UHFFFAOYSA-N 0.000 claims description 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 239000012623 DNA damaging agent Substances 0.000 claims description 2
- 150000004922 Dasatinib derivatives Chemical group 0.000 claims description 2
- 208000032612 Glial tumor Diseases 0.000 claims description 2
- 206010018338 Glioma Diseases 0.000 claims description 2
- XDXDZDZNSLXDNA-TZNDIEGXSA-N Idarubicin Chemical compound C1[C@H](N)[C@H](O)[C@H](C)O[C@H]1O[C@@H]1C2=C(O)C(C(=O)C3=CC=CC=C3C3=O)=C3C(O)=C2C[C@@](O)(C(C)=O)C1 XDXDZDZNSLXDNA-TZNDIEGXSA-N 0.000 claims description 2
- XDXDZDZNSLXDNA-UHFFFAOYSA-N Idarubicin Natural products C1C(N)C(O)C(C)OC1OC1C2=C(O)C(C(=O)C3=CC=CC=C3C3=O)=C3C(O)=C2CC(O)(C(C)=O)C1 XDXDZDZNSLXDNA-UHFFFAOYSA-N 0.000 claims description 2
- 239000005411 L01XE02 - Gefitinib Substances 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- 229940124647 MEK inhibitor Drugs 0.000 claims description 2
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 206010039491 Sarcoma Diseases 0.000 claims description 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 2
- 229940123237 Taxane Drugs 0.000 claims description 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims description 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 2
- 229940045799 anthracyclines and related substance Drugs 0.000 claims description 2
- 230000000340 anti-metabolite Effects 0.000 claims description 2
- 229940100197 antimetabolite Drugs 0.000 claims description 2
- 239000002256 antimetabolite Substances 0.000 claims description 2
- 239000005441 aurora Substances 0.000 claims description 2
- VSRXQHXAPYXROS-UHFFFAOYSA-N azanide;cyclobutane-1,1-dicarboxylic acid;platinum(2+) Chemical compound [NH2-].[NH2-].[Pt+2].OC(=O)C1(C(O)=O)CCC1 VSRXQHXAPYXROS-UHFFFAOYSA-N 0.000 claims description 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims description 2
- 229940127093 camptothecin Drugs 0.000 claims description 2
- VSJKWCGYPAHWDS-FQEVSTJZSA-N camptothecin Chemical group C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-FQEVSTJZSA-N 0.000 claims description 2
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 2
- 229960004562 carboplatin Drugs 0.000 claims description 2
- 201000010881 cervical cancer Diseases 0.000 claims description 2
- 208000029742 colonic neoplasm Diseases 0.000 claims description 2
- VSJKWCGYPAHWDS-UHFFFAOYSA-N dl-camptothecin Natural products C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)C5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-UHFFFAOYSA-N 0.000 claims description 2
- 229960004679 doxorubicin Drugs 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims description 2
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims description 2
- 229910052731 fluorine Inorganic materials 0.000 claims description 2
- 235000019000 fluorine Nutrition 0.000 claims description 2
- 206010017758 gastric cancer Diseases 0.000 claims description 2
- XGALLCVXEZPNRQ-UHFFFAOYSA-N gefitinib Chemical compound C=12C=C(OCCCN3CCOCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 XGALLCVXEZPNRQ-UHFFFAOYSA-N 0.000 claims description 2
- 229910052736 halogen Inorganic materials 0.000 claims description 2
- 150000002367 halogens Chemical class 0.000 claims description 2
- 201000010536 head and neck cancer Diseases 0.000 claims description 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 2
- 229960000908 idarubicin Drugs 0.000 claims description 2
- 229940084651 iressa Drugs 0.000 claims description 2
- 201000007270 liver cancer Diseases 0.000 claims description 2
- 208000014018 liver neoplasm Diseases 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 208000020816 lung neoplasm Diseases 0.000 claims description 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 2
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 claims description 2
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims description 2
- 229960001756 oxaliplatin Drugs 0.000 claims description 2
- DWAFYCQODLXJNR-BNTLRKBRSA-L oxaliplatin Chemical compound O1C(=O)C(=O)O[Pt]11N[C@@H]2CCCC[C@H]2N1 DWAFYCQODLXJNR-BNTLRKBRSA-L 0.000 claims description 2
- 201000002528 pancreatic cancer Diseases 0.000 claims description 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 2
- 201000011549 stomach cancer Diseases 0.000 claims description 2
- 125000001424 substituent group Chemical group 0.000 claims description 2
- 229940063683 taxotere Drugs 0.000 claims description 2
- 125000000335 thiazolyl group Chemical group 0.000 claims description 2
- 201000002510 thyroid cancer Diseases 0.000 claims description 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 2
- 229960004528 vincristine Drugs 0.000 claims description 2
- OGWKCGZFUXNPDA-XQKSVPLYSA-N vincristine Chemical compound C([N@]1C[C@@H](C[C@]2(C(=O)OC)C=3C(=CC4=C([C@]56[C@H]([C@@]([C@H](OC(C)=O)[C@]7(CC)C=CCN([C@H]67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)C[C@@](C1)(O)CC)CC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-XQKSVPLYSA-N 0.000 claims description 2
- OGWKCGZFUXNPDA-UHFFFAOYSA-N vincristine Natural products C1C(CC)(O)CC(CC2(C(=O)OC)C=3C(=CC4=C(C56C(C(C(OC(C)=O)C7(CC)C=CCN(C67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)CN1CCC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-UHFFFAOYSA-N 0.000 claims description 2
- WAEXFXRVDQXREF-UHFFFAOYSA-N vorinostat Chemical compound ONC(=O)CCCCCCC(=O)NC1=CC=CC=C1 WAEXFXRVDQXREF-UHFFFAOYSA-N 0.000 claims description 2
- 229960000237 vorinostat Drugs 0.000 claims description 2
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 claims 1
- 0 CC=NOC(*)=N Chemical compound CC=NOC(*)=N 0.000 description 10
- 108091000080 Phosphotransferase Proteins 0.000 description 2
- 102000020233 phosphotransferase Human genes 0.000 description 2
- XCGAGBWTJLMLSN-UHFFFAOYSA-N CN(CC1)CC11CCN(C)CC1 Chemical compound CN(CC1)CC11CCN(C)CC1 XCGAGBWTJLMLSN-UHFFFAOYSA-N 0.000 description 1
- 150000001539 azetidines Chemical class 0.000 description 1
- 238000010835 comparative analysis Methods 0.000 description 1
- 125000004857 imidazopyridinyl group Chemical group N1C(=NC2=C1C=CC=N2)* 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000001727 in vivo 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
- 230000002071 myeloproliferative effect Effects 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91557907P | 2007-05-02 | 2007-05-02 | |
| US60/915,579 | 2007-05-02 | ||
| PCT/US2008/062330 WO2008137622A2 (en) | 2007-05-02 | 2008-05-02 | Aminopyrimidines useful as kinase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013168846A Division JP2013231085A (ja) | 2007-05-02 | 2013-08-15 | キナーゼ阻害として有用なアミノピリミジン |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010526098A JP2010526098A (ja) | 2010-07-29 |
| JP2010526098A5 true JP2010526098A5 (enExample) | 2012-06-07 |
| JP5572087B2 JP5572087B2 (ja) | 2014-08-13 |
Family
ID=39708615
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010506664A Expired - Fee Related JP5572087B2 (ja) | 2007-05-02 | 2008-05-02 | キナーゼ阻害として有用なアミノピリミジン |
| JP2013168846A Withdrawn JP2013231085A (ja) | 2007-05-02 | 2013-08-15 | キナーゼ阻害として有用なアミノピリミジン |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013168846A Withdrawn JP2013231085A (ja) | 2007-05-02 | 2013-08-15 | キナーゼ阻害として有用なアミノピリミジン |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20110046104A1 (enExample) |
| EP (1) | EP2155730A2 (enExample) |
| JP (2) | JP5572087B2 (enExample) |
| CN (1) | CN101679387A (enExample) |
| AU (1) | AU2008247595A1 (enExample) |
| CA (1) | CA2688584A1 (enExample) |
| MX (1) | MX2009011811A (enExample) |
| WO (1) | WO2008137622A2 (enExample) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2001290912A1 (en) | 2000-09-15 | 2002-03-26 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| US6660731B2 (en) | 2000-09-15 | 2003-12-09 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| WO2004072029A2 (en) | 2003-02-06 | 2004-08-26 | Vertex Pharmaceuticals Incorporated | Pyrazolopyridazines useful as inhibitors of protein kinases |
| JP5249770B2 (ja) | 2005-11-03 | 2013-07-31 | 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 | キナーゼインヒビターとして有用なアミノピリジン |
| CA2668429A1 (en) | 2006-11-02 | 2008-05-15 | Vertex Pharmaceuticals Incorporated | Aminopyridines and aminopyrimidines useful as inhibitors of protein kinases |
| NZ577768A (en) | 2006-12-19 | 2012-01-12 | Vertex Pharma | Aminopyrimidines useful as inhibitors of protein kinases |
| CN101663295B (zh) | 2007-03-09 | 2014-11-05 | 沃泰克斯药物股份有限公司 | 可用作蛋白激酶抑制剂的氨基嘧啶类化合物 |
| JP5393489B2 (ja) | 2007-03-09 | 2014-01-22 | 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 | 蛋白キナーゼの阻害剤として有用なアミノピリミジン |
| NZ579483A (en) | 2007-03-09 | 2012-07-27 | Vertex Pharma | Aminopyridines useful as inhibitors of protein kinases |
| MX2009011059A (es) | 2007-04-13 | 2009-11-26 | Vertex Pharma | Aminopirimidinas utiles como inhibidores de cinasas. |
| WO2008137619A2 (en) | 2007-05-02 | 2008-11-13 | Vertex Pharmaceuticals Incorporated | Thiazoles and pyrazoles useful as kinase inhibitors |
| CA2688584A1 (en) * | 2007-05-02 | 2008-11-13 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| AU2008247594A1 (en) * | 2007-05-02 | 2008-11-13 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| WO2009018415A1 (en) | 2007-07-31 | 2009-02-05 | Vertex Pharmaceuticals Incorporated | Process for preparing 5-fluoro-1h-pyrazolo [3, 4-b] pyridin-3-amine and derivatives thereof |
| SG11201406584TA (en) | 2012-04-24 | 2014-11-27 | Vertex Pharma | Dna-pk inhibitors |
| EP2922847A1 (en) | 2012-11-20 | 2015-09-30 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of indoleamine 2,3-dioxygenase |
| RS62649B1 (sr) | 2013-03-12 | 2021-12-31 | Vertex Pharma | Inhibitori dnk-pk |
| KR102411227B1 (ko) | 2013-10-17 | 2022-06-21 | 버텍스 파마슈티칼스 인코포레이티드 | Dna-pk 억제제로서 (s)-n-메틸-8-(1-((2'-메틸-[4,5'-비피리미딘]-6-일)아미노)프로판-2-일)퀴놀린-4-카복스아미드 및 이의 듀테로화된 유도체의 공결정 |
| MX394860B (es) | 2016-09-27 | 2025-03-24 | Vertex Pharma | Metodo para tratar cancer usando una combinacion de agentes que dañan adn e inhibidores de proteina cinasa dependiente de adn (adn-pk). |
| EP3672957A1 (en) * | 2017-11-23 | 2020-07-01 | BioMed X GmbH | Pyrimidine derivatives as tropomyosin receptor kinase a (trka) inhibitors |
Family Cites Families (55)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3133081A (en) * | 1964-05-12 | J-aminoindazole derivatives | ||
| US3935183A (en) * | 1970-01-26 | 1976-01-27 | Imperial Chemical Industries Limited | Indazole-azo phenyl compounds |
| BE754242A (fr) * | 1970-07-15 | 1971-02-01 | Geigy Ag J R | Diamino-s-triazines et dinitro-s-triazines |
| US3998951A (en) * | 1974-03-13 | 1976-12-21 | Fmc Corporation | Substituted 2-arylquinazolines as fungicides |
| DE2458965C3 (de) * | 1974-12-13 | 1979-10-11 | Bayer Ag, 5090 Leverkusen | 3-Amino-indazol-N-carbonsäure-Derivate, Verfahren zu ihrer Herstellung sowie sie enthaltende Arzneimittel |
| DOP1981004033A (es) * | 1980-12-23 | 1990-12-29 | Ciba Geigy Ag | Procedimiento para proteger plantas de cultivo de la accion fitotoxica de herbicidas. |
| SE8102193L (sv) * | 1981-04-06 | 1982-10-07 | Pharmacia Ab | Terapeutiskt aktiv organisk forening och dess anvendning |
| SE8102194L (sv) * | 1981-04-06 | 1982-10-07 | Pharmacia Ab | Terapeutiskt aktiv organisk forening och farmaceutisk beredning innehallande denna |
| JPS58124773A (ja) * | 1982-01-20 | 1983-07-25 | Mitsui Toatsu Chem Inc | ５−メチルチオピリミジン誘導体とその製造法と農園芸用殺菌剤 |
| US5710158A (en) * | 1991-05-10 | 1998-01-20 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase |
| CA2203517A1 (en) * | 1994-11-10 | 1996-05-23 | Alan M. Laibelman | Pharmaceutical pyrazole compositions useful as inhibitors of protein kinases |
| IL117659A (en) * | 1995-04-13 | 2000-12-06 | Dainippon Pharmaceutical Co | Substituted 2-phenyl pyrimidino amino acetamide derivative process for preparing the same and a pharmaceutical composition containing same |
| US6716575B2 (en) * | 1995-12-18 | 2004-04-06 | Sugen, Inc. | Diagnosis and treatment of AUR1 and/or AUR2 related disorders |
| GB9619284D0 (en) * | 1996-09-16 | 1996-10-30 | Celltech Therapeutics Ltd | Chemical compounds |
| US6267952B1 (en) * | 1998-01-09 | 2001-07-31 | Geltex Pharmaceuticals, Inc. | Lipase inhibiting polymers |
| ATE245641T1 (de) * | 1998-02-17 | 2003-08-15 | Tularik Inc | Antivirale pyrimidinderivate |
| CA2339188A1 (en) * | 1998-08-21 | 2000-03-02 | Dupont Pharmaceuticals Company | Isoxazolo¬4,5-d|pyrimidines as crf antagonists |
| US6184226B1 (en) * | 1998-08-28 | 2001-02-06 | Scios Inc. | Quinazoline derivatives as inhibitors of P-38 α |
| GB9828511D0 (en) * | 1998-12-24 | 1999-02-17 | Zeneca Ltd | Chemical compounds |
| GB9914258D0 (en) * | 1999-06-18 | 1999-08-18 | Celltech Therapeutics Ltd | Chemical compounds |
| US20020065270A1 (en) * | 1999-12-28 | 2002-05-30 | Moriarty Kevin Joseph | N-heterocyclic inhibitors of TNF-alpha expression |
| JP4783532B2 (ja) * | 2000-02-05 | 2011-09-28 | 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 | Ｅｒｋのインヒビターとして有用なピラゾール組成物 |
| KR20030024659A (ko) * | 2000-02-17 | 2003-03-26 | 암겐 인코포레이티드 | 키나제 억제제 |
| GB0004887D0 (en) * | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| BR0111754A (pt) * | 2000-06-28 | 2003-04-29 | Astrazeneca Ab | Uso de um composto, método para inibir aurora 2 quinase em um animal de sangue quente, composto, e, composição farmacêutica |
| US6613776B2 (en) * | 2000-09-15 | 2003-09-02 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| US6610677B2 (en) * | 2000-09-15 | 2003-08-26 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| DE60122176T2 (de) * | 2000-09-15 | 2007-07-05 | Vertex Pharmaceuticals Inc., Cambridge | Isoxazole und ihre verwendung als erk-inhibitoren |
| AU2001290912A1 (en) * | 2000-09-15 | 2002-03-26 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| US7473691B2 (en) * | 2000-09-15 | 2009-01-06 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| US6660731B2 (en) * | 2000-09-15 | 2003-12-09 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| DE10061863A1 (de) * | 2000-12-12 | 2002-06-13 | Basf Ag | Verfahren zur Herstellung von Triethylendiamin (TEDA) |
| US6716851B2 (en) * | 2000-12-12 | 2004-04-06 | Cytovia, Inc. | Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators or caspases and inducers of apoptosis and the use thereof |
| BR0116493A (pt) * | 2000-12-21 | 2003-09-30 | Vertex Pharma | Compostos de pirazol úteis como inibidores de proteìna cinase |
| MY130778A (en) * | 2001-02-09 | 2007-07-31 | Vertex Pharma | Heterocyclic inhibitiors of erk2 and uses thereof |
| MXPA03008888A (es) * | 2001-03-29 | 2005-03-07 | Vertex Pharma | Inhibidores de n-terminal c-jun cinasas (jnk) y otras proteinas cinasas. |
| DE60214701T2 (de) * | 2001-04-13 | 2007-09-13 | Vertex Pharmaceuticals Inc., Cambridge | Inhibitoren von c-jun-n-terminalen-kinasen (jnk) und anderen proteinkinasen |
| EP1383771A1 (en) * | 2001-04-20 | 2004-01-28 | Vertex Pharmaceuticals Incorporated | 9-deazaguanine derivatives as inhibitors of gsk-3 |
| JP4316893B2 (ja) * | 2001-05-16 | 2009-08-19 | 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 | Ｓｒｃおよび他のプロテインキナーゼのインヒビター |
| CA2450769A1 (en) * | 2001-06-15 | 2002-12-27 | Vertex Pharmaceuticals Incorporated | 5-(2-aminopyrimidin-4-yl) benzisoxazoles as protein kinase inhibitors |
| CA2452603A1 (en) * | 2001-07-03 | 2003-01-16 | Vertex Pharmaceuticals Incorporated | Isoxazolyl-pyrimidines as inhibitors of src and lck protein kinases |
| US6698980B2 (en) * | 2001-07-30 | 2004-03-02 | Stewart Mining Products Inc. | Rock stabilizing apparatus and method |
| ATE466581T1 (de) * | 2001-12-07 | 2010-05-15 | Vertex Pharma | Verbindungen auf pyrimidin-basis als gsk-3-hemmer |
| AU2003225800A1 (en) * | 2002-03-15 | 2003-09-29 | Hayley Binch | Azolylaminoazine as inhibitors of protein kinases |
| US20040009981A1 (en) * | 2002-03-15 | 2004-01-15 | David Bebbington | Compositions useful as inhibitors of protein kinases |
| WO2003077921A1 (en) * | 2002-03-15 | 2003-09-25 | Vertex Pharmaceuticals, Inc. | Azinylaminoazoles as inhibitors of protein kinases |
| US6846928B2 (en) * | 2002-03-15 | 2005-01-25 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of protein kinases |
| US20030207873A1 (en) * | 2002-04-10 | 2003-11-06 | Edmund Harrington | Inhibitors of Src and other protein kinases |
| EP1506189A1 (en) * | 2002-04-26 | 2005-02-16 | Vertex Pharmaceuticals Incorporated | Pyrrole derivatives as inhibitors of erk2 and uses thereof |
| MY141867A (en) * | 2002-06-20 | 2010-07-16 | Vertex Pharma | Substituted pyrimidines useful as protein kinase inhibitors |
| US7361665B2 (en) * | 2002-07-09 | 2008-04-22 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases |
| US7262200B2 (en) * | 2002-10-25 | 2007-08-28 | Vertex Pharmaceuticals Incorporated | Indazolinone compositions useful as kinase inhibitors |
| JP5249770B2 (ja) * | 2005-11-03 | 2013-07-31 | 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 | キナーゼインヒビターとして有用なアミノピリジン |
| CA2688584A1 (en) * | 2007-05-02 | 2008-11-13 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| AU2008247594A1 (en) * | 2007-05-02 | 2008-11-13 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
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2008
- 2008-05-02 CA CA002688584A patent/CA2688584A1/en not_active Abandoned
- 2008-05-02 AU AU2008247595A patent/AU2008247595A1/en not_active Abandoned
- 2008-05-02 WO PCT/US2008/062330 patent/WO2008137622A2/en not_active Ceased
- 2008-05-02 CN CN200880021067A patent/CN101679387A/zh active Pending
- 2008-05-02 EP EP08747432A patent/EP2155730A2/en not_active Withdrawn
- 2008-05-02 MX MX2009011811A patent/MX2009011811A/es not_active Application Discontinuation
- 2008-05-02 JP JP2010506664A patent/JP5572087B2/ja not_active Expired - Fee Related
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2009
- 2009-10-30 US US12/598,277 patent/US20110046104A1/en not_active Abandoned
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2013
- 2013-08-15 JP JP2013168846A patent/JP2013231085A/ja not_active Withdrawn