JP2009514887A5 - - Google Patents
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- JP2009514887A5 JP2009514887A5 JP2008539091A JP2008539091A JP2009514887A5 JP 2009514887 A5 JP2009514887 A5 JP 2009514887A5 JP 2008539091 A JP2008539091 A JP 2008539091A JP 2008539091 A JP2008539091 A JP 2008539091A JP 2009514887 A5 JP2009514887 A5 JP 2009514887A5
- Authority
- JP
- Japan
- Prior art keywords
- ring
- compound
- aliphatic
- compound according
- optionally substituted
- 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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- 150000001875 compounds Chemical class 0.000 claims 73
- 125000001931 aliphatic group Chemical group 0.000 claims 40
- 229910052757 nitrogen Inorganic materials 0.000 claims 23
- 125000001072 heteroaryl group Chemical group 0.000 claims 19
- 229910052760 oxygen Inorganic materials 0.000 claims 18
- 229910052717 sulfur Inorganic materials 0.000 claims 18
- 125000005842 heteroatom Chemical group 0.000 claims 17
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 17
- 125000000217 alkyl group Chemical group 0.000 claims 16
- 229910052736 halogen Inorganic materials 0.000 claims 16
- 150000002367 halogens Chemical class 0.000 claims 16
- 125000000623 heterocyclic group Chemical group 0.000 claims 13
- 239000000203 mixture Substances 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 11
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 10
- 125000003118 aryl group Chemical group 0.000 claims 8
- 150000001334 alicyclic compounds Chemical group 0.000 claims 7
- 125000004429 atom Chemical group 0.000 claims 7
- 125000005843 halogen group Chemical group 0.000 claims 7
- 125000001118 alkylidene group Chemical group 0.000 claims 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 5
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 claims 4
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 4
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- AWJUIBRHMBBTKR-UHFFFAOYSA-N isoquinoline Chemical compound C1=NC=CC2=CC=CC=C21 AWJUIBRHMBBTKR-UHFFFAOYSA-N 0.000 claims 4
- 239000001301 oxygen Chemical group 0.000 claims 4
- 125000006413 ring segment Chemical group 0.000 claims 4
- 239000011593 sulfur Chemical group 0.000 claims 4
- 229940124597 therapeutic agent Drugs 0.000 claims 4
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 125000001153 fluoro group Chemical group F* 0.000 claims 3
- 125000001475 halogen functional group Chemical group 0.000 claims 3
- 125000002950 monocyclic group Chemical group 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 229920006395 saturated elastomer Polymers 0.000 claims 3
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 claims 2
- -1 C 3 alicyclic compound Chemical group 0.000 claims 2
- 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 2
- 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 2
- 239000005517 L01XE01 - Imatinib Substances 0.000 claims 2
- 239000005551 L01XE03 - Erlotinib Substances 0.000 claims 2
- 239000002067 L01XE06 - Dasatinib Substances 0.000 claims 2
- 239000005536 L01XE08 - Nilotinib Substances 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 229930012538 Paclitaxel Natural products 0.000 claims 2
- 206010038389 Renal cancer Diseases 0.000 claims 2
- 239000012472 biological sample Substances 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 2
- 210000003169 central nervous system Anatomy 0.000 claims 2
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims 2
- 229960004316 cisplatin Drugs 0.000 claims 2
- 229960002448 dasatinib Drugs 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 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 2
- 229940080856 gleevec Drugs 0.000 claims 2
- 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 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 201000010982 kidney cancer Diseases 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 229960001346 nilotinib Drugs 0.000 claims 2
- 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 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 229960001592 paclitaxel Drugs 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 229940120982 tarceva Drugs 0.000 claims 2
- 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 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- 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 1
- 125000001963 4 membered heterocyclic group Chemical group 0.000 claims 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- KLWPJMFMVPTNCC-UHFFFAOYSA-N Camptothecin Natural products CCC1(O)C(=O)OCC2=C1C=C3C4Nc5ccccc5C=C4CN3C2=O KLWPJMFMVPTNCC-UHFFFAOYSA-N 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 239000012623 DNA damaging agent Substances 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 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 1
- 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 1
- 239000005411 L01XE02 - Gefitinib Substances 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 229940124647 MEK inhibitor Drugs 0.000 claims 1
- 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 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 102000001253 Protein Kinase Human genes 0.000 claims 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 229940123237 Taxane Drugs 0.000 claims 1
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical group C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000002723 alicyclic group Chemical group 0.000 claims 1
- 229940045799 anthracyclines and related substance Drugs 0.000 claims 1
- 230000000340 anti-metabolite Effects 0.000 claims 1
- 229940100197 antimetabolite Drugs 0.000 claims 1
- 239000002256 antimetabolite Substances 0.000 claims 1
- 239000005441 aurora Substances 0.000 claims 1
- 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 1
- 229940127093 camptothecin Drugs 0.000 claims 1
- 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 1
- 125000004452 carbocyclyl group Chemical group 0.000 claims 1
- 229960004562 carboplatin Drugs 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 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 1
- 229960004679 doxorubicin Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 229940121647 egfr inhibitor Drugs 0.000 claims 1
- 235000019000 fluorine Nutrition 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 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 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 229960000908 idarubicin Drugs 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 229940084651 iressa Drugs 0.000 claims 1
- PXZQEOJJUGGUIB-UHFFFAOYSA-N isoindolin-1-one Chemical compound C1=CC=C2C(=O)NCC2=C1 PXZQEOJJUGGUIB-UHFFFAOYSA-N 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 claims 1
- 201000000050 myeloid neoplasm Diseases 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 150000002829 nitrogen Chemical class 0.000 claims 1
- 229960001756 oxaliplatin Drugs 0.000 claims 1
- 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 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 108060006633 protein kinase Proteins 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 229940063683 taxotere Drugs 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
- 229960004528 vincristine Drugs 0.000 claims 1
- 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 1
- 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 1
- WAEXFXRVDQXREF-UHFFFAOYSA-N vorinostat Chemical compound ONC(=O)CCCCCCC(=O)NC1=CC=CC=C1 WAEXFXRVDQXREF-UHFFFAOYSA-N 0.000 claims 1
- 229960000237 vorinostat Drugs 0.000 claims 1
- 0 *c1c(*)[n]nc1Nc1nc(S*)nc(*)c1* Chemical compound *c1c(*)[n]nc1Nc1nc(S*)nc(*)c1* 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US73295105P | 2005-11-03 | 2005-11-03 | |
| US60/732,951 | 2005-11-03 | ||
| US73355705P | 2005-11-04 | 2005-11-04 | |
| US60/733,557 | 2005-11-04 | ||
| PCT/US2006/043096 WO2007056221A2 (en) | 2005-11-03 | 2006-11-03 | Aminopyrimidines useful as kinase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012271604A Division JP2013049731A (ja) | 2005-11-03 | 2012-12-12 | キナーゼインヒビターとして有用なアミノピリミジン |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009514887A JP2009514887A (ja) | 2009-04-09 |
| JP2009514887A5 true JP2009514887A5 (enExample) | 2010-12-09 |
| JP5328361B2 JP5328361B2 (ja) | 2013-10-30 |
Family
ID=38023840
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008539091A Expired - Fee Related JP5328361B2 (ja) | 2005-11-03 | 2006-11-03 | キナーゼインヒビターとして有用なアミノピリミジン |
| JP2008539071A Expired - Fee Related JP5249771B2 (ja) | 2005-11-03 | 2006-11-03 | キナーゼインヒビターとして有用なアミノピリミジン |
| JP2008539070A Expired - Fee Related JP5249770B2 (ja) | 2005-11-03 | 2006-11-03 | キナーゼインヒビターとして有用なアミノピリジン |
| JP2012271604A Pending JP2013049731A (ja) | 2005-11-03 | 2012-12-12 | キナーゼインヒビターとして有用なアミノピリミジン |
| JP2012276504A Pending JP2013075904A (ja) | 2005-11-03 | 2012-12-19 | キナーゼインヒビターとして有用なアミノピリジン |
Family Applications After (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008539071A Expired - Fee Related JP5249771B2 (ja) | 2005-11-03 | 2006-11-03 | キナーゼインヒビターとして有用なアミノピリミジン |
| JP2008539070A Expired - Fee Related JP5249770B2 (ja) | 2005-11-03 | 2006-11-03 | キナーゼインヒビターとして有用なアミノピリジン |
| JP2012271604A Pending JP2013049731A (ja) | 2005-11-03 | 2012-12-12 | キナーゼインヒビターとして有用なアミノピリミジン |
| JP2012276504A Pending JP2013075904A (ja) | 2005-11-03 | 2012-12-19 | キナーゼインヒビターとして有用なアミノピリジン |
Country Status (18)
| Country | Link |
|---|---|
| US (7) | US7528142B2 (enExample) |
| EP (3) | EP1954277B1 (enExample) |
| JP (5) | JP5328361B2 (enExample) |
| KR (3) | KR20080067693A (enExample) |
| CN (3) | CN101316843B (enExample) |
| AR (3) | AR057874A1 (enExample) |
| AU (3) | AU2006311797A1 (enExample) |
| BR (3) | BRPI0619708A2 (enExample) |
| CA (3) | CA2627808A1 (enExample) |
| ES (2) | ES2435081T3 (enExample) |
| IL (3) | IL191043A0 (enExample) |
| MX (3) | MX2008005717A (enExample) |
| NO (3) | NO20082517L (enExample) |
| NZ (4) | NZ594385A (enExample) |
| RU (5) | RU2427578C2 (enExample) |
| SG (2) | SG166827A1 (enExample) |
| TW (3) | TW200734327A (enExample) |
| WO (3) | WO2007056221A2 (enExample) |
Families Citing this family (77)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK1318997T3 (da) | 2000-09-15 | 2006-09-25 | Vertex Pharma | Pyrazolforbindelser der er nyttige som proteinkinase-inhibitorer |
| US6660731B2 (en) | 2000-09-15 | 2003-12-09 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| SE0104140D0 (sv) * | 2001-12-07 | 2001-12-07 | Astrazeneca Ab | Novel Compounds |
| WO2004072029A2 (en) | 2003-02-06 | 2004-08-26 | Vertex Pharmaceuticals Incorporated | Pyrazolopyridazines useful as inhibitors of protein kinases |
| SI1853588T1 (sl) * | 2005-02-16 | 2008-10-31 | Astrazeneca Ab | Kemične spojine |
| BRPI0610184A2 (pt) * | 2005-05-16 | 2012-09-25 | Astrazeneca Ab | composto, sal farmaceuticamente aceitável de um composto, processo para preparar um composto ou um sal farmaceuticamente aceitável do mesmo, uso de um composto ou um sal farmaceuticamente aceitável do mesmo, métodos para a inibição da atividade de trk, para o tratamento ou profilaxia de cáncer e para a produção de um efeito anti-proliferativo em um animal de sanque quente, e, composição farmacêutica |
| CN101340909B (zh) * | 2005-10-18 | 2012-01-11 | 詹森药业有限公司 | 抑制flt3激酶的方法 |
| DK1945631T3 (da) * | 2005-10-28 | 2012-10-22 | Astrazeneca Ab | 4- (3-aminopyrazole) pyrimidinderivater til anvendelse som tyrosinkinaseinhibitorer til behandling af cancer |
| TW200734327A (en) | 2005-11-03 | 2007-09-16 | Vertex Pharma | Aminopyrimidines useful as kinase inhibitors |
| EP1951716B1 (en) * | 2005-11-16 | 2011-05-04 | Vertex Pharmaceuticals, Inc. | Aminopyrimidines useful as kinase inhibitors |
| US8697716B2 (en) | 2006-04-20 | 2014-04-15 | Janssen Pharmaceutica Nv | Method of inhibiting C-KIT kinase |
| MX2008013531A (es) | 2006-04-20 | 2009-01-20 | Janssen Pharmaceutica Nv | Inhibidores de c-fms cinasa. |
| WO2008057940A1 (en) | 2006-11-02 | 2008-05-15 | Vertex Pharmaceuticals Incorporated | Aminopyridines and aminopyrimidines useful as inhibitors of protein kinases |
| WO2008077086A1 (en) | 2006-12-19 | 2008-06-26 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as inhibitors of protein kinases |
| WO2008112642A1 (en) | 2007-03-09 | 2008-09-18 | 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 |
| EP2137183B1 (en) * | 2007-03-09 | 2011-09-28 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as inhibitors of protein kinases |
| JP2010523700A (ja) | 2007-04-13 | 2010-07-15 | 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 | キナーゼインヒビターとして有用なアミノピリミジン |
| WO2008129255A1 (en) * | 2007-04-18 | 2008-10-30 | Astrazeneca Ab | 5-aminopyrazol-3-yl-3h-imidazo [4,5-b] pyridine derivatives and their use for the treatment of cancer |
| CN101801959A (zh) * | 2007-05-02 | 2010-08-11 | 沃泰克斯药物股份有限公司 | 可用作激酶抑制剂的氨基嘧啶类化合物 |
| CN101679378A (zh) | 2007-05-02 | 2010-03-24 | 沃泰克斯药物股份有限公司 | 用作激酶抑制剂的噻唑和吡唑 |
| AU2008247595A1 (en) * | 2007-05-02 | 2008-11-13 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| US20100137398A1 (en) * | 2007-05-04 | 2010-06-03 | Novartis Ag | Use of hdac inhibitors for the treatment of gastrointestinal cancers |
| UA99459C2 (en) * | 2007-05-04 | 2012-08-27 | Астразенека Аб | 9-(pyrazol-3-yl)- 9h-purine-2-amine and 3-(pyraz0l-3-yl)-3h-imidazo[4,5-b]pyridin-5-amine derivatives and their use for the treatment of cancer |
| AU2008257044A1 (en) * | 2007-05-24 | 2008-12-04 | Vertex Pharmaceuticals Incorporated | Thiazoles and pyrazoles useful as kinase inhibitors |
| JP2010529193A (ja) * | 2007-06-11 | 2010-08-26 | ミイカナ セラピューティクス インコーポレイテッド | 置換ピラゾール化合物 |
| AR067762A1 (es) * | 2007-07-31 | 2009-10-21 | Vertex Pharma | Proceso para preparar 5-fluoro-1h-pirazolo (3,4-b) piridin-3-amina y derivados de la misma |
| US8461149B2 (en) * | 2007-08-15 | 2013-06-11 | Vertex Pharmaceuticals Incorporated | Compounds useful as protein kinase inhibitors |
| ES2393824T3 (es) | 2007-09-21 | 2012-12-28 | Array Biopharma, Inc. | Derivados de piridin-2-il-amino-1,2,4-tiadiazol como activadores de glucoquinasa para el tratamiento de diabetes mellitus |
| WO2009086012A1 (en) * | 2007-12-20 | 2009-07-09 | Curis, Inc. | Aurora inhibitors containing a zinc binding moiety |
| US20110033461A1 (en) * | 2008-03-12 | 2011-02-10 | Vladimir Ratushny | Combination Therapy for the Treatment of Cancer |
| WO2009114677A1 (en) * | 2008-03-13 | 2009-09-17 | Bristol-Myers Squibb Company | Pyridazine derivatives as factor xia inhibitors |
| WO2009117439A2 (en) * | 2008-03-17 | 2009-09-24 | The Scripps Research Institute | Combined chemical and genetic approaches for generation of induced pluripotent stem cells |
| CN102119157A (zh) * | 2008-06-11 | 2011-07-06 | 阿斯利康(瑞典)有限公司 | 用于治疗癌症和骨髓增生性疾病的三环2,4-二氨基-l,3,5-三嗪衍生物 |
| MY156789A (en) * | 2008-09-05 | 2016-03-31 | Celgene Avilomics Res Inc | Algorithm for designing irreversible inhibitors |
| JP2012504157A (ja) * | 2008-09-30 | 2012-02-16 | アストラゼネカ アクチボラグ | 複素環式jakキナーゼ阻害剤 |
| MX2011006725A (es) | 2008-12-22 | 2011-09-15 | Millennium Pharm Inc | Combinacion de inhibidores de aurora cinasa y anticuerpos anti-cd20. |
| AU2010258825B2 (en) * | 2009-06-09 | 2014-08-21 | Nantbio, Inc. | Ureidophenyl substituted triazine derivatives and their therapeutical applications |
| IN2012DN02534A (enExample) | 2009-09-16 | 2015-08-28 | Avila Therapeutics Inc | |
| US20110269244A1 (en) | 2009-12-30 | 2011-11-03 | Petter Russell C | Ligand-directed covalent modification of protein |
| US8933070B2 (en) | 2010-07-02 | 2015-01-13 | University Health Network | Methods of targeting PTEN mutant diseases and compositions therefor |
| SG187633A1 (en) * | 2010-07-30 | 2013-03-28 | Oncotherapy Science Inc | Quinoline derivatives and melk inhibitors containing the same |
| WO2012112674A2 (en) | 2011-02-15 | 2012-08-23 | The Johns Hopkins University | Compounds and methods of use thereof for treating neurodegenerative disorders |
| EP2736895B1 (en) | 2011-07-27 | 2016-01-06 | Astrazeneca AB | 2-(2,4,5-substituted-anilino) pyrimidine derivatives as egfr modulators useful for treating cancer |
| MX2014002208A (es) | 2011-08-25 | 2014-05-28 | Hoffmann La Roche | Inhibidores de serina/treonina quinasa. |
| EP2754659A4 (en) * | 2011-09-05 | 2015-08-26 | Zhejiang Hisun Pharm Co Ltd | 4-SUBSTITUTE (3-SUBSTITUTE-1H-PYRAZOLE-5-AMINO) -PYRIMIDIN DERIVATIVE HAVING AN INHIBITORY EFFECT ON PROTEIN KINASE AND USE THEREOF |
| CN104185420B (zh) | 2011-11-30 | 2017-06-09 | 埃默里大学 | 用于治疗或预防逆转录病毒和其它病毒感染的抗病毒jak抑制剂 |
| KR20140103972A (ko) | 2011-12-22 | 2014-08-27 | 에프. 호프만-라 로슈 아게 | 세린/트레오닌 키나아제 억제제로서의 2,4-다이아민-피리미딘 유도체 |
| AU2013205306B2 (en) | 2012-03-16 | 2015-09-17 | Axikin Pharmaceuticals, Inc. | 3,5-diaminopyrazole kinase inhibitors |
| IN2014KN02601A (enExample) | 2012-04-24 | 2015-05-08 | Vertex Pharma | |
| US20130310340A1 (en) | 2012-05-16 | 2013-11-21 | Rigel Pharmaceuticals, Inc. | Method of treating muscular degradation |
| EP2852388A4 (en) | 2012-05-23 | 2016-01-13 | Univ Johns Hopkins | COMPOUNDS AND METHOD FOR USE THEREOF FOR THE TREATMENT OF NEURODEEGENERATIVE DISEASES |
| CA2880896C (en) | 2012-06-26 | 2021-11-16 | Del Mar Pharmaceuticals | Methods for treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or ahi1 dysregulations or mutations employing dianhydrogalactitol, diacetyldianhydrogalactitol, dibromodulcitol, or analogs or derivatives thereof |
| AU2013337297A1 (en) | 2012-11-05 | 2015-05-21 | Nantbio, Inc. | Substituted indol-5-ol derivatives and their therapeutical applications |
| SMT202100687T1 (it) | 2013-03-12 | 2022-01-10 | Vertex Pharma | Inibitori della dna-pk |
| WO2014145403A1 (en) | 2013-03-15 | 2014-09-18 | Nantbio, Inc. | Substituted indol-5-ol derivatives and their therapeutic applications |
| CN105492011A (zh) | 2013-04-08 | 2016-04-13 | 丹尼斯·M·布朗 | 不理想给药化学化合物的治疗增效 |
| CA2949048A1 (en) * | 2013-05-22 | 2014-11-27 | The Regents Of The University Of California | Aurora kinase inhibitors |
| NZ631142A (en) | 2013-09-18 | 2016-03-31 | Axikin Pharmaceuticals Inc | Pharmaceutically acceptable salts of 3,5-diaminopyrazole kinase inhibitors |
| ES2705342T3 (es) | 2013-10-17 | 2019-03-22 | Vertex Pharma | Co-cristales de (S)-N-metil-8-(1-((2'-metil-[4,5'-bipirimidin]-6-il)amino)propan-2-il)quinolin-4-carboxamida y derivados deuterados de la misma como inhibidores de DNA-PK |
| US10335494B2 (en) | 2013-12-06 | 2019-07-02 | Millennium Pharmaceuticals, Inc. | Combination of aurora kinase inhibitors and anti-CD30 antibodies |
| CN107250116B (zh) | 2014-12-23 | 2020-10-27 | 艾士盟医疗公司 | 3,5-二氨基吡唑激酶抑制剂 |
| HK1252425A1 (zh) | 2015-06-05 | 2019-05-24 | Vertex Pharmaceuticals Incorporated | 用於治疗脱髓鞘疾病的三唑类药物 |
| JP2018524292A (ja) | 2015-07-21 | 2018-08-30 | ミレニアム ファーマシューティカルズ, インコーポレイテッドMillennium Pharmaceuticals, Inc. | オーロラキナーゼインヒビターと化学療法剤の投与 |
| WO2017156350A1 (en) | 2016-03-09 | 2017-09-14 | K-Gen, Inc. | Methods of cancer treatment |
| EP3518931A4 (en) | 2016-09-27 | 2020-05-13 | Vertex Pharmaceuticals Incorporated | METHOD FOR TREATING CANCER WITH A COMBINATION OF DNA-DAMAGING SUBSTANCES AND DNA-PK INHIBITORS |
| CN117756789A (zh) * | 2016-12-14 | 2024-03-26 | 英特维特国际股份有限公司 | 作为选择性Janus激酶抑制剂的氨基吡唑类化合物 |
| PT3562821T (pt) | 2016-12-28 | 2021-03-03 | Minoryx Therapeutics S L | Compostos de isoquinolina, métodos para a sua preparação e utilizações terapêuticas dos mesmos em condições associadas à alteração da atividade da beta-galactosidade |
| CN106841420A (zh) * | 2016-12-30 | 2017-06-13 | 广州中大南沙科技创新产业园有限公司 | 一种LC‑MS/MS测定大鼠血浆中Ly‑7u浓度的方法 |
| US11874276B2 (en) | 2018-04-05 | 2024-01-16 | Dana-Farber Cancer Institute, Inc. | STING levels as a biomarker for cancer immunotherapy |
| CN113645976A (zh) | 2019-03-29 | 2021-11-12 | 阿斯利康(瑞典)有限公司 | 用于治疗非小细胞肺癌的奧希替尼 |
| CN110132795A (zh) * | 2019-05-20 | 2019-08-16 | 华核(天津)新技术开发有限公司 | 放射性去污效率测试方法 |
| US20220305048A1 (en) | 2019-08-26 | 2022-09-29 | Dana-Farber Cancer Institute, Inc. | Use of heparin to promote type 1 interferon signaling |
| WO2021178485A1 (en) * | 2020-03-06 | 2021-09-10 | National Health Research Institutes | Pyrimidine compounds and their pharmaceutical uses |
| WO2021222637A1 (en) | 2020-04-30 | 2021-11-04 | United States Government As Represented By The Department Of Veterans Affairs | Krüppel-like factor 15 (klf15) small molecule agonists in kidney disease |
| WO2023107705A1 (en) | 2021-12-10 | 2023-06-15 | Incyte Corporation | Bicyclic amines as cdk12 inhibitors |
| WO2025049402A1 (en) * | 2023-08-28 | 2025-03-06 | Quanta Therapeutics, Inc. | Kras modulators and uses thereof |
Family Cites Families (119)
| 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 |
| MA18829A1 (fr) | 1979-05-18 | 1980-12-31 | Ciba Geigy Ag | Derives de la pyrimidine,procedes pour leur preparation,compositions pharmaceutiques contenant ces composes et leur utilisation therapeutique |
| 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 |
| EP0136976A3 (de) | 1983-08-23 | 1985-05-15 | Ciba-Geigy Ag | Verwendung von Phenylpyrimidinen als Pflanzenregulatoren |
| DE3725638A1 (de) | 1987-08-03 | 1989-02-16 | Bayer Ag | Neue aryloxy (bzw. thio)aminopyrimidine |
| 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 |
| US5597920A (en) | 1992-04-30 | 1997-01-28 | Neurogen Corporation | Gabaa receptor subtypes and methods for screening drug compounds using imidazoquinoxalines and pyrrolopyrimidines to bind to gabaa receptor subtypes |
| JPH0665237A (ja) | 1992-05-07 | 1994-03-08 | Nissan Chem Ind Ltd | 置換ピラゾール誘導体および農園芸用殺菌剤 |
| DE69434721T2 (de) | 1993-10-01 | 2006-11-09 | Novartis Ag | Pharmacologisch wirksame pyrimidinderivate und verfahren zu deren herstellung |
| KR970706813A (ko) * | 1994-11-10 | 1997-12-01 | 찰스 홈시 | 단백질 키나아제의 억제물질로서 유용한 제약용 피라졸 조성물(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 |
| CA2230896A1 (en) | 1995-09-01 | 1997-03-13 | Signal Pharmaceuticals, Inc. | Pyrimidine carboxylates and related compounds and methods for treating inflammatory conditions |
| US5935966A (en) | 1995-09-01 | 1999-08-10 | Signal Pharmaceuticals, Inc. | Pyrimidine carboxylates and related compounds and methods for treating inflammatory conditions |
| GB9523675D0 (en) | 1995-11-20 | 1996-01-24 | Celltech Therapeutics Ltd | Chemical compounds |
| US6716575B2 (en) | 1995-12-18 | 2004-04-06 | Sugen, Inc. | Diagnosis and treatment of AUR1 and/or AUR2 related disorders |
| JP4386967B2 (ja) | 1996-07-13 | 2009-12-16 | グラクソ、グループ、リミテッド | プロテインチロシンキナーゼ阻害剤としての縮合複素環式化合物 |
| JPH10130150A (ja) | 1996-09-05 | 1998-05-19 | Dainippon Pharmaceut Co Ltd | 酢酸アミド誘導体からなる医薬 |
| GB9619284D0 (en) * | 1996-09-16 | 1996-10-30 | Celltech Therapeutics Ltd | Chemical compounds |
| WO1998014450A1 (en) | 1996-10-02 | 1998-04-09 | Novartis Ag | Pyrimidine derivatives and processes for the preparation thereof |
| BR9712530A (pt) | 1996-10-11 | 1999-10-19 | Warner Lambert Co | Inibidores de ésteres de asparato de enzima de conversão de interleucina-1beta |
| BR9814817A (pt) | 1997-10-10 | 2002-01-08 | Cytovia Inc | Inibidores de apoptose de dipeptìdio e o uso dos mesmos |
| US6267952B1 (en) | 1998-01-09 | 2001-07-31 | Geltex Pharmaceuticals, Inc. | Lipase inhibiting polymers |
| JP2000026421A (ja) | 1998-01-29 | 2000-01-25 | Kumiai Chem Ind Co Ltd | ジアリ―ルスルフィド誘導体及び有害生物防除剤 |
| BR9908004A (pt) | 1998-02-17 | 2001-12-18 | Tularik Inc | Composto, composição e método para prevençãoou supressão de uma infecção viral |
| EP1076563B1 (en) | 1998-03-16 | 2005-05-11 | Cytovia, Inc. | Dipeptide caspase inhibitors and the use thereof |
| NZ508314A (en) | 1998-06-02 | 2004-03-26 | Osi Pharm Inc | Pyrrolo[2,3d]pyrimidine compositions and their use |
| CN1312807A (zh) | 1998-06-19 | 2001-09-12 | 希龙公司 | 糖元合成酶激酶3的抑制剂 |
| 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 |
| DK1119567T3 (da) | 1998-10-08 | 2005-07-25 | Astrazeneca Ab | Quinazolinderivater |
| GB9828640D0 (en) | 1998-12-23 | 1999-02-17 | Smithkline Beecham Plc | Novel method and compounds |
| GB9828511D0 (en) | 1998-12-24 | 1999-02-17 | Zeneca Ltd | Chemical compounds |
| AU2482700A (en) | 1999-01-13 | 2000-08-01 | Warner-Lambert Company | 1-heterocycle substituted diarylamines |
| US6921748B1 (en) | 1999-03-29 | 2005-07-26 | Uutech Limited | Analogs of gastric inhibitory polypeptide and their use for treatment of diabetes |
| PT1165085E (pt) | 1999-03-30 | 2006-10-31 | Novartis Ag | Derivados de ftalazina para tratar doencas inflamatorias |
| EP1185528A4 (en) | 1999-06-17 | 2003-03-26 | Shionogi Biores Corp | INHIBITORS OF IL-12 PRODUCTION |
| GB9914258D0 (en) * | 1999-06-18 | 1999-08-18 | Celltech Therapeutics Ltd | Chemical compounds |
| JP2003531103A (ja) | 1999-08-12 | 2003-10-21 | 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 | c−JUNN−末端キナーゼ(JNK)および他のタンパク質キナーゼの阻害剤 |
| ATE396978T1 (de) | 1999-10-07 | 2008-06-15 | Amgen Inc | Triazin-kinase-hemmer |
| IL149103A0 (en) | 1999-11-30 | 2002-11-10 | Pfizer Prod Inc | 2,4-diaminopyrimidine compounds useful as immunosuppressants |
| KR100840727B1 (ko) | 1999-12-02 | 2008-06-23 | 오에스아이 파마슈티컬스, 인코포레이티드 | 아데노신 a1, a2a 및 a3 수용체 특이 화합물 및 그의 사용방법 |
| MY125768A (en) | 1999-12-15 | 2006-08-30 | Bristol Myers Squibb Co | N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases |
| US6376489B1 (en) | 1999-12-23 | 2002-04-23 | Icos Corporation | Cyclic AMP-specific phosphodiesterase inhibitors |
| US20020065270A1 (en) * | 1999-12-28 | 2002-05-30 | Moriarty Kevin Joseph | N-heterocyclic inhibitors of TNF-alpha expression |
| EP1246823A1 (en) | 1999-12-28 | 2002-10-09 | Pharmacopeia, Inc. | Pyrimidine and triazine kinase inhibitors |
| EP1200422A2 (en) * | 2000-02-05 | 2002-05-02 | Vertex Pharmaceuticals Incorporated | Pyrazole compositions useful as inhibitors of erk |
| MXPA02007957A (es) | 2000-02-17 | 2002-11-29 | Amgen Inc | Inhibidores de cinasas. |
| GB0004887D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| GB0004890D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| DE60111509T2 (de) | 2000-04-03 | 2006-05-11 | Vertex Pharmaceuticals Inc., Cambridge | Inhibitoren von Serin-Proteasen, insbesondere der Hepatitis-C-Virus NS23-Protease |
| JP2004501083A (ja) | 2000-04-18 | 2004-01-15 | アゴーロン・ファーマシューティカルズ・インコーポレイテッド | プロテインキナーゼを阻害するためのピラゾール |
| EE200200715A (et) * | 2000-06-28 | 2004-08-16 | Astrazeneca Ab | Asendatud kinasoliini derivaadid ja nende kasutamine inhibiitoritena |
| CZ303213B6 (cs) | 2000-07-21 | 2012-05-23 | Schering Corporation | Peptidové inhibitory serinové proteázy NS3 a farmaceutický prostredek |
| SK2002003A3 (en) | 2000-08-31 | 2004-04-06 | Pfizer Prod Inc | Pyrazole derivatives and their use as protein kinase inhibitors |
| AU2001290940A1 (en) * | 2000-09-15 | 2002-03-26 | Vertex Pharmaceuticals Incorporated | Isoxazoles and their use as inhibitors of erk |
| 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 |
| DK1318997T3 (da) | 2000-09-15 | 2006-09-25 | Vertex Pharma | Pyrazolforbindelser der er nyttige som proteinkinase-inhibitorer |
| US6613776B2 (en) | 2000-09-15 | 2003-09-02 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| US7547702B2 (en) | 2000-09-20 | 2009-06-16 | Ortho-Mcneil Pharmaceutical, Inc. | 4-amino-quinazolines |
| US6641579B1 (en) * | 2000-09-29 | 2003-11-04 | Spectrasonics Imaging, Inc. | Apparatus and method for ablating cardiac tissue |
| DE10061863A1 (de) * | 2000-12-12 | 2002-06-13 | Basf Ag | Verfahren zur Herstellung von Triethylendiamin (TEDA) |
| WO2002047690A1 (en) | 2000-12-12 | 2002-06-20 | Cytovia, Inc. | Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators of caspases and inducers of apoptosis and the use thereof |
| 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 |
| HUP0400639A3 (en) | 2000-12-21 | 2010-03-29 | Vertex Pharma | Pyrazole compounds useful as protein kinase inhibitors and pharmaceutical compositions containing them |
| MY130778A (en) * | 2001-02-09 | 2007-07-31 | Vertex Pharma | Heterocyclic inhibitiors of erk2 and uses thereof |
| US6759983B2 (en) * | 2001-03-28 | 2004-07-06 | Strategic Analysis, Inc. | Method and device for precise geolocation of low-power, broadband, amplitude-modulated signals |
| EP1373257B9 (en) | 2001-03-29 | 2008-10-15 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases |
| WO2002083667A2 (en) | 2001-04-13 | 2002-10-24 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases |
| WO2002085909A1 (en) | 2001-04-20 | 2002-10-31 | 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 |
| US6825190B2 (en) * | 2001-06-15 | 2004-11-30 | Vertex Pharmaceuticals Incorporated | Protein kinase inhibitors and uses thereof |
| WO2003004492A1 (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 |
| WO2003026665A1 (en) | 2001-09-26 | 2003-04-03 | Bayer Pharmaceuticals Corporation | 2-phenylamino-4-(5-pyrazolylamino)-pyrimidine derivatives as kinase inhibitors, in particular, src kinase inhibitors |
| US6569499B2 (en) * | 2001-10-02 | 2003-05-27 | Xerox Corporation | Apparatus and method for coating photoreceptor substrates |
| JP2005516005A (ja) * | 2001-12-07 | 2005-06-02 | 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 | Gsk−3阻害剤として有用なピリミジンベースの化合物 |
| US7863282B2 (en) | 2003-03-14 | 2011-01-04 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of protein kinases |
| EP1485100B1 (en) * | 2002-03-15 | 2010-05-05 | Vertex Pharmaceuticals Incorporated | Azinylaminoazoles as inhibitors of protein kinases |
| ES2289279T3 (es) | 2002-03-15 | 2008-02-01 | Vertex Pharmaceuticals Incorporated | Composiciones utiles como inhibidores de proteinquinasas. |
| ATE468336T1 (de) | 2002-03-15 | 2010-06-15 | Vertex Pharma | Azolylaminoazine als proteinkinasehemmer |
| ATE433973T1 (de) * | 2002-03-15 | 2009-07-15 | Vertex Pharma | Azolylaminoazine als inhibitoren von proteinkinasen |
| 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 |
| WO2004005283A1 (en) * | 2002-07-09 | 2004-01-15 | Vertex Pharmaceuticals Incorporated | Imidazoles, oxazoles and thiazoles with protein kinase inhibiting activities |
| DE60308387T2 (de) | 2002-08-02 | 2007-09-20 | Vertex Pharmaceuticals Inc., Cambridge | Pyrazolenthaltende zusammensetzungen und ihre verwendung als gsk-3 inhibitoren |
| US7262200B2 (en) | 2002-10-25 | 2007-08-28 | Vertex Pharmaceuticals Incorporated | Indazolinone compositions useful as kinase inhibitors |
| JP2004224944A (ja) * | 2003-01-24 | 2004-08-12 | Kuraray Plast Co Ltd | 高周波接着性に優れた熱可塑性樹脂組成物 |
| KR20060123164A (ko) | 2003-10-17 | 2006-12-01 | 아스트라제네카 아베 | 암 치료에 사용하기 위한 4-(피라졸-3-일아미노)피리미딘유도체 |
| MY141220A (en) * | 2003-11-17 | 2010-03-31 | Astrazeneca Ab | Pyrazole derivatives as inhibitors of receptor tyrosine kinases |
| GB0402653D0 (en) * | 2004-02-06 | 2004-03-10 | Cyclacel Ltd | Compounds |
| JP2009502922A (ja) | 2005-07-28 | 2009-01-29 | 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 | カスパーゼ阻害剤プロドラッグ |
| AU2006279376B2 (en) | 2005-08-18 | 2011-04-14 | Vertex Pharmaceuticals Incoporated | Pyrazine kinase inhibitors |
| WO2007023382A2 (en) | 2005-08-25 | 2007-03-01 | Pfizer Inc. | Pyrimidine amino pyrazole compounds, potent kinase inhibitors |
| CA2622352C (en) * | 2005-09-30 | 2014-05-27 | Miikana Therapeutics, Inc. | Substituted pyrazole compounds |
| TW200734327A (en) | 2005-11-03 | 2007-09-16 | Vertex Pharma | Aminopyrimidines useful as kinase inhibitors |
| EP1951716B1 (en) | 2005-11-16 | 2011-05-04 | Vertex Pharmaceuticals, Inc. | Aminopyrimidines useful as kinase inhibitors |
| WO2008057940A1 (en) | 2006-11-02 | 2008-05-15 | Vertex Pharmaceuticals Incorporated | Aminopyridines and aminopyrimidines useful as inhibitors of protein kinases |
| WO2008077086A1 (en) | 2006-12-19 | 2008-06-26 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as inhibitors of protein kinases |
| ES2523863T3 (es) * | 2006-12-29 | 2014-12-02 | Janssen R&D Ireland | Pirimidinas 5,6-sustituidas inhibidoras del VIH |
| WO2008112642A1 (en) | 2007-03-09 | 2008-09-18 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as inhibitors of protein kinases |
| EP2137183B1 (en) | 2007-03-09 | 2011-09-28 | 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 |
| CN101675041A (zh) | 2007-03-20 | 2010-03-17 | 沃泰克斯药物股份有限公司 | 用作激酶抑制剂的氨基嘧啶类化合物 |
| WO2008131103A2 (en) * | 2007-04-17 | 2008-10-30 | Vertex Pharmaceuticals Incorporated | Drug discovery methods for aurora kinase inhibitors |
| AU2008247595A1 (en) | 2007-05-02 | 2008-11-13 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| CN101801959A (zh) | 2007-05-02 | 2010-08-11 | 沃泰克斯药物股份有限公司 | 可用作激酶抑制剂的氨基嘧啶类化合物 |
| CN101679378A (zh) | 2007-05-02 | 2010-03-24 | 沃泰克斯药物股份有限公司 | 用作激酶抑制剂的噻唑和吡唑 |
| AU2008257044A1 (en) | 2007-05-24 | 2008-12-04 | Vertex Pharmaceuticals Incorporated | Thiazoles and pyrazoles useful as kinase inhibitors |
| MX384179B (es) | 2009-03-20 | 2025-03-14 | Vertex Pharma | Proceso para producir moduladores del regulador de conductancia transmembrana de fibrosis quística. |
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