JP2009515992A5 - - Google Patents
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- JP2009515992A5 JP2009515992A5 JP2008541363A JP2008541363A JP2009515992A5 JP 2009515992 A5 JP2009515992 A5 JP 2009515992A5 JP 2008541363 A JP2008541363 A JP 2008541363A JP 2008541363 A JP2008541363 A JP 2008541363A JP 2009515992 A5 JP2009515992 A5 JP 2009515992A5
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- JP
- Japan
- Prior art keywords
- ring
- compound
- aliphatic
- optionally substituted
- independently
- 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 33
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 12
- 229910052757 nitrogen Inorganic materials 0.000 claims 11
- 125000000623 heterocyclic group Chemical group 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 229910052760 oxygen Inorganic materials 0.000 claims 7
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- 125000004429 atom Chemical group 0.000 claims 5
- 125000005843 halogen group Chemical group 0.000 claims 5
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 4
- 125000001931 aliphatic group Chemical group 0.000 claims 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 4
- 125000004452 carbocyclyl group Chemical group 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 239000001301 oxygen Substances 0.000 claims 4
- 239000011593 sulfur Substances 0.000 claims 4
- 229940124597 therapeutic agent Drugs 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 125000001118 alkylidene group Chemical group 0.000 claims 3
- 125000001475 halogen functional group Chemical group 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 239000003112 inhibitor Substances 0.000 claims 3
- 125000002950 monocyclic group Chemical group 0.000 claims 3
- 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
- 208000008839 Kidney Neoplasms Diseases 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
- 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
- 229910052799 carbon Inorganic materials 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
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms 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
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 229940080856 gleevec Drugs 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 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
- 201000010982 kidney cancer Diseases 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 125000000325 methylidene group Chemical group [H]C([H])=* 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
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 229960001592 paclitaxel Drugs 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 125000006413 ring segment Chemical group 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 229920006395 saturated elastomer Polymers 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
- -1 -OR 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
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms 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
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 239000012623 DNA damaging agent Substances 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 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
- 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
- 125000000217 alkyl 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
- 125000003118 aryl group Chemical group 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
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 claims 1
- 210000000481 breast Anatomy 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
- 229960004562 carboplatin Drugs 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 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
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims 1
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 230000002496 gastric effect Effects 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
- 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
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 claims 1
- 201000000050 myeloid neoplasm Diseases 0.000 claims 1
- 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 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
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 108060006633 protein kinase Proteins 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000003003 spiro group Chemical group 0.000 claims 1
- DKPFODGZWDEEBT-QFIAKTPHSA-N taxane Chemical class C([C@]1(C)CCC[C@@H](C)[C@H]1C1)C[C@H]2[C@H](C)CC[C@@H]1C2(C)C DKPFODGZWDEEBT-QFIAKTPHSA-N 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
- 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 *c1ccn[n]1 Chemical compound *c1ccn[n]1 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US73706405P | 2005-11-16 | 2005-11-16 | |
| PCT/US2006/044636 WO2007059299A1 (en) | 2005-11-16 | 2006-11-16 | Aminopyrimidines useful as kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2009515992A JP2009515992A (ja) | 2009-04-16 |
| JP2009515992A5 true JP2009515992A5 (https=) | 2011-01-06 |
Family
ID=37806123
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008541363A Pending JP2009515992A (ja) | 2005-11-16 | 2006-11-16 | キナーゼ阻害剤として有用なアミノピリミジン |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US20070179125A1 (https=) |
| EP (1) | EP1951716B1 (https=) |
| JP (1) | JP2009515992A (https=) |
| CN (1) | CN101360740A (https=) |
| AT (1) | ATE508126T1 (https=) |
| AU (1) | AU2006315334B2 (https=) |
| CA (1) | CA2629781A1 (https=) |
| DE (1) | DE602006021776D1 (https=) |
| WO (1) | WO2007059299A1 (https=) |
Families Citing this family (55)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1317450B1 (en) | 2000-09-15 | 2006-11-22 | 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 |
| KR101443651B1 (ko) * | 2005-10-18 | 2014-09-23 | 얀센 파마슈티카 엔.브이. | Flt-3 키나제의 억제 방법 |
| EP1954277B1 (en) | 2005-11-03 | 2017-01-18 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| EP2606890A1 (en) * | 2006-04-05 | 2013-06-26 | Novartis AG | Combinations comprising BCR-ABL/C-KIT/PDGF-R TK inhibitors for treating cancer |
| BRPI0710548B8 (pt) | 2006-04-20 | 2021-05-25 | Janssen Pharmaceutica Nv | inibidores de c-fms cinase, composição farmacêutica e forma de dosagem farmacêutica |
| US8697716B2 (en) | 2006-04-20 | 2014-04-15 | Janssen Pharmaceutica Nv | Method of inhibiting C-KIT kinase |
| MX2009004807A (es) | 2006-11-02 | 2009-06-15 | Vertex Pharma | Aminopiridinas y aminopirimidinas utiles como inhibidores de proteina cinasa. |
| NZ577768A (en) * | 2006-12-19 | 2012-01-12 | Vertex Pharma | Aminopyrimidines useful as inhibitors of protein kinases |
| ATE526328T1 (de) * | 2007-03-09 | 2011-10-15 | Vertex Pharma | Als inhibitoren von proteinkinasen geeignete aminopyrimidine |
| MX2009009590A (es) | 2007-03-09 | 2009-11-10 | Vertex Pharma | Aminopirimidinas utiles como inhibidores de proteinas cinasas. |
| MX2009009592A (es) | 2007-03-09 | 2009-11-10 | Vertex Pharma | Aminopiridinas utiles como inhibidores de proteinas cinasas. |
| AU2008240313A1 (en) | 2007-04-13 | 2008-10-23 | Aj Park | Aminopyrimidines useful as kinase inhibitors |
| JP5389786B2 (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 | キナーゼ阻害として有用なアミノピリミジン |
| AU2008247592A1 (en) | 2007-05-02 | 2008-11-13 | Vertex Pharmaceuticals Incorporated | Thiazoles and pyrazoles useful as kinase inhibitors |
| AU2008262291A1 (en) * | 2007-06-11 | 2008-12-18 | Miikana Therapeutics, Inc. | Substituted pyrazole compounds |
| CN101790532B (zh) | 2007-07-31 | 2013-11-20 | 沃泰克斯药物股份有限公司 | 5-氟-1H-吡唑并[3,4-b]吡啶-3-胺及其衍生物的制备方法 |
| US20110190280A1 (en) * | 2007-08-29 | 2011-08-04 | George Adjabeng | Thiazole And Oxazole Kinase Inhibitors |
| AU2008305294B2 (en) | 2007-09-21 | 2012-11-29 | Array Biopharma Inc. | Pyridin-2 -yl-amino-1, 2, 4 -thiadiazole derivatives as glucokinase activators for the treatment of diabetes mellitus |
| WO2009073224A1 (en) * | 2007-12-07 | 2009-06-11 | Ambit Biosciences Corp. | Methods of treating certain diseases using pyrimidine derivatives |
| UA103319C2 (en) | 2008-05-06 | 2013-10-10 | Глаксосмитклайн Ллк | Thiazole- and oxazole-benzene sulfonamide compounds |
| WO2010009985A2 (en) * | 2008-07-24 | 2010-01-28 | Nerviano Medical Sciences S.R.L. | Therapeutic combination comprising an aurora kinase inhibitor and antiproliferative agents |
| US20100136096A1 (en) * | 2008-12-02 | 2010-06-03 | Searete Llc, A Limited Liability Corporation Of The State Of Delaware | Systems for modulating inflammation |
| US20100135984A1 (en) * | 2008-12-02 | 2010-06-03 | Searete Llc, A Limited Liability Corporation Of The State Of Delaware | Anti-inflammatory compositions and methods |
| US20100137247A1 (en) * | 2008-12-02 | 2010-06-03 | Searete Llc, A Limited Liability Corporation Of The State Of Delaware | Anti-inflammatory compositions and methods |
| US20100136094A1 (en) * | 2008-12-02 | 2010-06-03 | Searete Llc, A Limited Liability Corporation Of The State Of Delaware | Systems for modulating inflammation |
| US20100135983A1 (en) * | 2008-12-02 | 2010-06-03 | Searete Llc, A Limited Liability Corporation Of The State Of Delaware | Anti-inflammatory compositions and methods |
| US20100136097A1 (en) * | 2008-12-02 | 2010-06-03 | Searete Llc, A Limited Liability Corporation Of The State Of Delaware | Systems for modulating inflammation |
| US20100137246A1 (en) * | 2008-12-02 | 2010-06-03 | Searete Llc, A Limited Liability Corporation Of The State Of Delaware | Anti-inflammatory compositions and methods |
| US20100136095A1 (en) * | 2008-12-02 | 2010-06-03 | Searete Llc, A Limited Liability Corporation Of The State Of Delaware | Systems for modulating inflammation |
| WO2010106016A1 (en) | 2009-03-17 | 2010-09-23 | Glaxo Group Limited | Pyrimidine derivatives used as itk inhibitors |
| JP2012521426A (ja) * | 2009-03-24 | 2012-09-13 | Msd株式会社 | オーロラa選択的阻害作用を有する新規アミノピリジン誘導体 |
| MX2014002208A (es) | 2011-08-25 | 2014-05-28 | Hoffmann La Roche | Inhibidores de serina/treonina quinasa. |
| BR112014015549A8 (pt) | 2011-12-22 | 2017-07-04 | Hoffmann La Roche | composto, método de inibição da atividade pak1, método para o tratamento, processo, composição, utilização de um composto e invenção |
| KR20140138293A (ko) | 2012-03-16 | 2014-12-03 | 액시킨 파마수티컬스 인코포레이티드 | 3,5-다이아미노피라졸 키나아제 억제제 |
| JP6378171B2 (ja) | 2012-04-24 | 2018-08-22 | 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Vertex Pharmaceuticals Incorporated | Dna−pk阻害剤 |
| CN104379582A (zh) * | 2012-06-15 | 2015-02-25 | 巴斯夫欧洲公司 | 包含达沙替尼和所选择的共晶体形成剂的多组分晶体 |
| SI3527563T1 (sl) | 2013-03-12 | 2022-01-31 | Vertex Pharmaceuticals Incorporated | Inhibitorji DNA-PK |
| NZ631142A (en) | 2013-09-18 | 2016-03-31 | Axikin Pharmaceuticals Inc | Pharmaceutically acceptable salts of 3,5-diaminopyrazole kinase inhibitors |
| RU2675270C2 (ru) | 2013-10-17 | 2018-12-18 | Вертекс Фармасьютикалз Инкорпорейтед | Сокристаллы и содержащие их фармацевтические композиции |
| US9546163B2 (en) | 2014-12-23 | 2017-01-17 | Axikin Pharmaceuticals, Inc. | 3,5-diaminopyrazole kinase inhibitors |
| AU2016270373A1 (en) | 2015-06-05 | 2018-01-04 | Vertex Pharmaceuticals Incorporated | Triazoles for the treatment of demyelinating diseases |
| KR101726648B1 (ko) * | 2016-02-29 | 2017-04-14 | 한국화학연구원 | 신규한 피리미딘 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 drak 관련 질환의 예방 또는 치료용 약학적 조성물 |
| MX377180B (es) | 2016-04-28 | 2025-03-07 | Theravance Biopharma R&D Ip Llc | Compuestos de pirimidina como inhibidores de la quinasa jak. |
| RU2758669C2 (ru) | 2016-09-27 | 2021-11-01 | Вертекс Фармасьютикалз Инкорпорейтед | Способ лечения рака с применением сочетания днк-поражающих агентов и ингибиторов днк-пк |
| CN110494432B (zh) | 2016-12-28 | 2022-08-12 | 米尼奥尔克斯治疗有限公司 | 异喹啉化合物,其制备方法及其在与β-半乳糖苷酶活性改变相关的病症中的治疗用途 |
| 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 |
| HRP20221221T1 (hr) | 2017-10-27 | 2022-12-09 | Theravance Biopharma R&D Ip, Llc | Pirimidinski spoj kao inhibitor jak kinaze |
| WO2020068873A1 (en) * | 2018-09-25 | 2020-04-02 | Black Diamond Therapeutics, Inc. | Tyrosine kinase inhibitor compositions, methods of making and methods of use |
| TW202106681A (zh) | 2019-04-24 | 2021-02-16 | 美商施萬生物製藥研發Ip有限責任公司 | 用於治療皮膚疾病之嘧啶jak抑制劑 |
| EP3958969B1 (en) | 2019-04-24 | 2024-01-10 | Theravance Biopharma R&D IP, LLC | Ester and carbonate pyrimidine compounds as jak kinase inhibitors |
| AU2021333760A1 (en) * | 2020-08-26 | 2023-04-06 | Nalo Therapeutics | Modulators of Myc family proto-oncogene protein |
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| WO2023164612A1 (en) * | 2022-02-25 | 2023-08-31 | Nalo Therapeutics | Modulators of myc family proto-oncogene protein |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2394727A1 (en) * | 1999-12-28 | 2001-07-05 | Pharmacopeia, Inc. | Pyrimidine and triazine kinase inhibitors |
| NZ526472A (en) * | 2000-12-21 | 2004-04-30 | Vertex Pharma | Pyrazole compounds useful as protein kinase inhibitors |
| JP2005500294A (ja) * | 2001-06-19 | 2005-01-06 | ブリストル−マイヤーズ スクイブ カンパニー | ホスホジエステラーゼ7に対するピリミジン阻害剤 |
| MY141867A (en) * | 2002-06-20 | 2010-07-16 | Vertex Pharma | Substituted pyrimidines useful as protein kinase inhibitors |
| WO2005040159A1 (en) * | 2003-10-17 | 2005-05-06 | Astrazeneca Ab | 4-(pyrazol-3-ylamino) pyrimidine derivatives for use in the treatment of cancer |
| EP1954277B1 (en) * | 2005-11-03 | 2017-01-18 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
-
2006
- 2006-11-16 CA CA002629781A patent/CA2629781A1/en not_active Abandoned
- 2006-11-16 US US11/600,588 patent/US20070179125A1/en not_active Abandoned
- 2006-11-16 CN CNA2006800511918A patent/CN101360740A/zh active Pending
- 2006-11-16 AU AU2006315334A patent/AU2006315334B2/en not_active Ceased
- 2006-11-16 EP EP06837883A patent/EP1951716B1/en not_active Not-in-force
- 2006-11-16 JP JP2008541363A patent/JP2009515992A/ja active Pending
- 2006-11-16 DE DE602006021776T patent/DE602006021776D1/de active Active
- 2006-11-16 WO PCT/US2006/044636 patent/WO2007059299A1/en not_active Ceased
- 2006-11-16 AT AT06837883T patent/ATE508126T1/de not_active IP Right Cessation
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