JP2010526098A5 - - Google Patents
Download PDFInfo
- Publication number
- 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
- Authority
- 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.)
- Granted
Links
- 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 |
|---|---|---|---|---|
| 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 |
| 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 |
| 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. |
| EP2134709A1 (en) | 2007-03-09 | 2009-12-23 | Vertex Pharmaceuticals, Inc. | Aminopyridines useful as inhibitors of protein kinases |
| NZ579485A (en) | 2007-03-09 | 2012-02-24 | Vertex Pharma | Aminopyrimidines useful as inhibitors of protein kinases |
| NZ580343A (en) | 2007-04-13 | 2012-03-30 | Vertex Pharma | Aminopyrimidines useful as 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 |
| 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 |
| SMT201800608T1 (it) | 2012-04-24 | 2019-01-11 | Vertex Pharma | Inibitori di dna-pk |
| KR20150087400A (ko) | 2012-11-20 | 2015-07-29 | 버텍스 파마슈티칼스 인코포레이티드 | 인돌아민 2,3-디옥시게나제의 억제제로서 유용한 화합물 |
| AU2014244555B2 (en) | 2013-03-12 | 2018-06-28 | Vertex Pharmaceuticals Incorporated | DNA-PK inhibitors |
| 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 |
| 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 |
| KR20200090198A (ko) * | 2017-11-23 | 2020-07-28 | 바이오메드 엑스 게엠베하 | 트로포미오신 수용체 키나제 A(TrkA) 저해제로서의 피리미딘 유도체 |
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. |
| SE8102194L (sv) * | 1981-04-06 | 1982-10-07 | Pharmacia Ab | Terapeutiskt aktiv organisk forening och farmaceutisk beredning innehallande denna |
| SE8102193L (sv) * | 1981-04-06 | 1982-10-07 | Pharmacia Ab | Terapeutiskt aktiv organisk forening och dess anvendning |
| 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 |
| JPH10509708A (ja) * | 1994-11-10 | 1998-09-22 | コア セラピューティクス，インコーポレイティド | プロテイン・キナーゼのインヒビターとして有用な医薬ピラゾール組成物 |
| 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 |
| KR20010041015A (ko) * | 1998-02-17 | 2001-05-15 | 윌리엄 제이. 리플린 | 항바이러스성 피리미딘 유도체 |
| 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 |
| IL145757A (en) * | 2000-02-05 | 2007-12-03 | Vertex Pharma | History of pyrazole and pharmaceutical preparations containing them |
| WO2001060816A1 (en) * | 2000-02-17 | 2001-08-23 | Amgen Inc. | Kinase inhibitors |
| GB0004887D0 (en) * | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| MXPA02011974A (es) * | 2000-06-28 | 2004-09-06 | Astrazeneca Ab | Derivados de quinazolina sustituidos y su uso como inhibidores. |
| US6638926B2 (en) * | 2000-09-15 | 2003-10-28 | 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 |
| US7473691B2 (en) * | 2000-09-15 | 2009-01-06 | 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 |
| NZ525016A (en) * | 2000-09-15 | 2004-10-29 | Vertex Pharma | Isoxazoles and their use as inhibitors of ERK |
| US6613776B2 (en) * | 2000-09-15 | 2003-09-02 | 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 |
| CA2432799C (en) * | 2000-12-21 | 2008-08-19 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| MY130778A (en) * | 2001-02-09 | 2007-07-31 | Vertex Pharma | Heterocyclic inhibitiors of erk2 and uses thereof |
| CA2441733A1 (en) * | 2001-03-29 | 2002-10-10 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases |
| EP1389206B1 (en) * | 2001-04-13 | 2006-09-13 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases |
| EP1383771A1 (en) * | 2001-04-20 | 2004-01-28 | Vertex Pharmaceuticals Incorporated | 9-deazaguanine derivatives as inhibitors of gsk-3 |
| US6884804B2 (en) * | 2001-05-16 | 2005-04-26 | Vertex Pharmaceuticals Incorporated | Inhibitors of Src and other protein kinases |
| US6825190B2 (en) * | 2001-06-15 | 2004-11-30 | Vertex Pharmaceuticals Incorporated | Protein kinase inhibitors and uses thereof |
| US6689778B2 (en) * | 2001-07-03 | 2004-02-10 | Vertex Pharmaceuticals Incorporated | Inhibitors of Src and Lck protein kinases |
| US6698980B2 (en) * | 2001-07-30 | 2004-03-02 | Stewart Mining Products Inc. | Rock stabilizing apparatus and method |
| EP1474147B1 (en) * | 2001-12-07 | 2010-05-05 | Vertex Pharmaceuticals Incorporated | Pyrimidine-based compounds useful as gsk-3 inhibitors |
| AU2003225800A1 (en) * | 2002-03-15 | 2003-09-29 | Hayley Binch | Azolylaminoazine as inhibitors of protein kinases |
| EP1485100B1 (en) * | 2002-03-15 | 2010-05-05 | Vertex Pharmaceuticals Incorporated | Azinylaminoazoles as inhibitors of protein kinases |
| ATE468336T1 (de) * | 2002-03-15 | 2010-06-15 | Vertex Pharma | Azolylaminoazine als proteinkinasehemmer |
| ES2289279T3 (es) * | 2002-03-15 | 2008-02-01 | Vertex Pharmaceuticals Incorporated | Composiciones utiles como inhibidores de proteinquinasas. |
| US20030207873A1 (en) * | 2002-04-10 | 2003-11-06 | Edmund Harrington | Inhibitors of Src and other protein kinases |
| US7304061B2 (en) * | 2002-04-26 | 2007-12-04 | Vertex Pharmaceuticals Incorporated | Heterocyclic inhibitors of ERK2 and uses thereof |
| MY141867A (en) * | 2002-06-20 | 2010-07-16 | Vertex Pharma | Substituted pyrimidines useful as protein kinase inhibitors |
| JP4570955B2 (ja) * | 2002-07-09 | 2010-10-27 | バーテクス ファーマスーティカルズ インコーポレイテッド | プロテインキナーゼ阻害活性を持つイミダゾール類 |
| AU2003286711A1 (en) * | 2002-10-25 | 2004-05-13 | Vertex Pharmaceuticals Incorporated | Indazolinone compositions useful as kinase inhibitors |
| WO2007056163A2 (en) * | 2005-11-03 | 2007-05-18 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as 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 |
-
2008
- 2008-05-02 CA CA002688584A patent/CA2688584A1/en not_active Abandoned
- 2008-05-02 CN CN200880021067A patent/CN101679387A/zh active Pending
- 2008-05-02 MX MX2009011811A patent/MX2009011811A/es not_active Application Discontinuation
- 2008-05-02 WO PCT/US2008/062330 patent/WO2008137622A2/en not_active Ceased
- 2008-05-02 AU AU2008247595A patent/AU2008247595A1/en not_active Abandoned
- 2008-05-02 EP EP08747432A patent/EP2155730A2/en not_active Withdrawn
- 2008-05-02 JP JP2010506664A patent/JP5572087B2/ja not_active Expired - Fee Related
-
2009
- 2009-10-30 US US12/598,277 patent/US20110046104A1/en not_active Abandoned
-
2013
- 2013-08-15 JP JP2013168846A patent/JP2013231085A/ja not_active Withdrawn
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2010526098A5 (enExample) | ||
| JP2010526097A5 (enExample) | ||
| JP2010528021A5 (enExample) | ||
| JP2009515992A5 (enExample) | ||
| JP2010526096A5 (ja) | 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 | |
| JP2010522194A5 (enExample) | ||
| JP2010523700A5 (enExample) | ||
| JP2009514887A5 (enExample) | ||
| JP2009514881A5 (enExample) | ||
| JP2009514880A5 (enExample) | ||
| Chatterjee et al. | HSP90 inhibitors in lung cancer: promise still unfulfilled | |
| WO2016161361A4 (en) | Compositions and methods of targeting mutant k-ras | |
| JP2018532737A5 (enExample) | ||
| RU2018119173A (ru) | Производное бензофурана, способ его получения и его применение в медицине | |
| JP2017531041A5 (enExample) | ||
| JP2017533266A5 (enExample) | ||
| JP2012153722A5 (enExample) | ||
| JP2016525135A5 (enExample) | ||
| JP2019502763A5 (enExample) | ||
| JP2021501208A5 (enExample) | ||
| RU2015147447A (ru) | Производные доластатина 10 и ауристатинов | |
| JP2015500884A5 (enExample) | ||
| JP6927882B2 (ja) | 癌の新治療法 | |
| JP2022538817A (ja) | Ｆｌｔ３阻害剤および化学療法剤を含む急性骨髄白血病を治療するための薬学的組成物 | |
| JP2009504771A5 (enExample) |