JP2011500685A5 - - Google Patents
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- JP2011500685A5 JP2011500685A5 JP2010529960A JP2010529960A JP2011500685A5 JP 2011500685 A5 JP2011500685 A5 JP 2011500685A5 JP 2010529960 A JP2010529960 A JP 2010529960A JP 2010529960 A JP2010529960 A JP 2010529960A JP 2011500685 A5 JP2011500685 A5 JP 2011500685A5
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- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims description 93
- 239000000203 mixture Substances 0.000 claims description 69
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 53
- 229910052736 halogen Inorganic materials 0.000 claims description 52
- 150000002367 halogens Chemical group 0.000 claims description 52
- 125000001931 aliphatic group Chemical group 0.000 claims description 42
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 41
- 125000005842 heteroatom Chemical group 0.000 claims description 38
- 229910052760 oxygen Inorganic materials 0.000 claims description 38
- 208000035475 disorder Diseases 0.000 claims description 37
- 229910052757 nitrogen Inorganic materials 0.000 claims description 34
- 229910052717 sulfur Inorganic materials 0.000 claims description 34
- 229910052739 hydrogen Inorganic materials 0.000 claims description 33
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 32
- 239000001257 hydrogen Substances 0.000 claims description 32
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims description 32
- 239000001301 oxygen Substances 0.000 claims description 32
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 28
- 239000011593 sulfur Substances 0.000 claims description 28
- 230000000694 effects Effects 0.000 claims description 27
- GVNVAWHJIKLAGL-UHFFFAOYSA-N 2-(cyclohexen-1-yl)cyclohexan-1-one Chemical compound O=C1CCCCC1C1=CCCCC1 GVNVAWHJIKLAGL-UHFFFAOYSA-N 0.000 claims description 24
- 101150065749 Churc1 gene Proteins 0.000 claims description 24
- 102100038239 Protein Churchill Human genes 0.000 claims description 24
- 229920006395 saturated elastomer Polymers 0.000 claims description 24
- 125000001183 hydrocarbyl group Chemical group 0.000 claims description 22
- 150000003839 salts Chemical class 0.000 claims description 18
- 125000003118 aryl group Chemical group 0.000 claims description 16
- 125000002619 bicyclic group Chemical group 0.000 claims description 16
- 230000002401 inhibitory effect Effects 0.000 claims description 16
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 15
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 15
- 101000934996 Homo sapiens Tyrosine-protein kinase JAK3 Proteins 0.000 claims description 12
- 102100029823 Tyrosine-protein kinase BTK Human genes 0.000 claims description 12
- 102100025387 Tyrosine-protein kinase JAK3 Human genes 0.000 claims description 12
- 230000001404 mediated effect Effects 0.000 claims description 11
- 108010009978 Tec protein-tyrosine kinase Proteins 0.000 claims description 10
- 125000004980 cyclopropylene group Chemical group 0.000 claims description 10
- 125000000623 heterocyclic group Chemical group 0.000 claims description 10
- 239000012472 biological sample Substances 0.000 claims description 9
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 9
- 206010028980 Neoplasm Diseases 0.000 claims description 8
- 125000004429 atom Chemical group 0.000 claims description 8
- 150000002431 hydrogen Chemical group 0.000 claims description 8
- 125000002950 monocyclic group Chemical group 0.000 claims description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 8
- 208000023275 Autoimmune disease Diseases 0.000 claims description 6
- 102100040177 Tyrosine-protein kinase Tec Human genes 0.000 claims description 6
- 201000011510 cancer Diseases 0.000 claims description 6
- 208000027866 inflammatory disease Diseases 0.000 claims description 6
- 102000001253 Protein Kinase Human genes 0.000 claims description 5
- 125000004043 oxo group Chemical group O=* 0.000 claims description 5
- 208000003019 Neurofibromatosis 1 Diseases 0.000 claims description 4
- 125000000217 alkyl group Chemical group 0.000 claims description 4
- 125000002837 carbocyclic group Chemical group 0.000 claims description 4
- 201000010099 disease Diseases 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 208000002761 neurofibromatosis 2 Diseases 0.000 claims description 4
- -1 propylene- Chemical class 0.000 claims description 4
- 125000001424 substituent group Chemical group 0.000 claims description 4
- 229940124597 therapeutic agent Drugs 0.000 claims description 4
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 2
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 2
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims description 2
- 206010005003 Bladder cancer Diseases 0.000 claims description 2
- 208000019838 Blood disease Diseases 0.000 claims description 2
- 208000020084 Bone disease Diseases 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 2
- 239000004215 Carbon black (E152) Substances 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 2
- 208000011231 Crohn disease Diseases 0.000 claims description 2
- 208000018522 Gastrointestinal disease Diseases 0.000 claims description 2
- 208000012659 Joint disease Diseases 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims description 2
- 208000015914 Non-Hodgkin lymphomas Diseases 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
- 208000004337 Salivary Gland Neoplasms Diseases 0.000 claims description 2
- 206010061934 Salivary gland cancer Diseases 0.000 claims description 2
- 206010052779 Transplant rejections Diseases 0.000 claims description 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 125000002947 alkylene group Chemical group 0.000 claims description 2
- 239000002246 antineoplastic agent Substances 0.000 claims description 2
- 210000000988 bone and bone Anatomy 0.000 claims description 2
- 208000035269 cancer or benign tumor Diseases 0.000 claims description 2
- 229910052799 carbon Inorganic materials 0.000 claims description 2
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims description 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 2
- 229940127089 cytotoxic agent Drugs 0.000 claims description 2
- 208000010643 digestive system disease Diseases 0.000 claims description 2
- 208000018685 gastrointestinal system disease Diseases 0.000 claims description 2
- 208000005017 glioblastoma Diseases 0.000 claims description 2
- 125000001188 haloalkyl group Chemical group 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
- 208000014951 hematologic disease Diseases 0.000 claims description 2
- 208000018706 hematopoietic system disease Diseases 0.000 claims description 2
- 229930195733 hydrocarbon Natural products 0.000 claims description 2
- 150000002430 hydrocarbons Chemical class 0.000 claims description 2
- 230000003463 hyperproliferative effect Effects 0.000 claims description 2
- 230000036039 immunity Effects 0.000 claims description 2
- 208000002551 irritable bowel syndrome Diseases 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 208000020816 lung neoplasm Diseases 0.000 claims description 2
- 206010025135 lupus erythematosus Diseases 0.000 claims description 2
- 230000036210 malignancy Effects 0.000 claims description 2
- 230000003211 malignant effect Effects 0.000 claims description 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 2
- 201000009020 malignant peripheral nerve sheath tumor Diseases 0.000 claims description 2
- 201000006417 multiple sclerosis Diseases 0.000 claims description 2
- 208000007538 neurilemmoma Diseases 0.000 claims description 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 2
- 208000029974 neurofibrosarcoma Diseases 0.000 claims description 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 2
- 201000002528 pancreatic cancer Diseases 0.000 claims description 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 230000002062 proliferating effect Effects 0.000 claims description 2
- QQONPFPTGQHPMA-UHFFFAOYSA-N propylene Natural products CC=C QQONPFPTGQHPMA-UHFFFAOYSA-N 0.000 claims description 2
- 208000023504 respiratory system disease Diseases 0.000 claims description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 2
- 210000004116 schwann cell Anatomy 0.000 claims description 2
- 206010039667 schwannoma Diseases 0.000 claims description 2
- 208000017520 skin disease Diseases 0.000 claims description 2
- 239000007787 solid Substances 0.000 claims description 2
- 206010041823 squamous cell carcinoma Diseases 0.000 claims description 2
- 230000009885 systemic effect Effects 0.000 claims description 2
- 230000009424 thromboembolic effect Effects 0.000 claims description 2
- 238000002054 transplantation Methods 0.000 claims description 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 2
- 239000000523 sample Substances 0.000 claims 2
- 125000001960 7 membered carbocyclic group Chemical group 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 201000009277 hairy cell leukemia Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 description 30
- 0 *c1cccc(NC2=CC(Nc3cc(NC(C=C)=O)ccc3)=NCN2)c1 Chemical compound *c1cccc(NC2=CC(Nc3cc(NC(C=C)=O)ccc3)=NCN2)c1 0.000 description 13
- NCFLMBPNYFEFKD-UHFFFAOYSA-N N#CC1(CC1)C(Nc1cccc(Nc2ncnc(Nc(cc3)cc(Cl)c3F)c2)c1)=O Chemical compound N#CC1(CC1)C(Nc1cccc(Nc2ncnc(Nc(cc3)cc(Cl)c3F)c2)c1)=O NCFLMBPNYFEFKD-UHFFFAOYSA-N 0.000 description 2
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 description 1
- ZBVCFJYVESEWGO-UHFFFAOYSA-N C#CC(C1)C=CC=C1Nc1ncnc(Nc2cccc(C#C)c2)c1 Chemical compound C#CC(C1)C=CC=C1Nc1ncnc(Nc2cccc(C#C)c2)c1 ZBVCFJYVESEWGO-UHFFFAOYSA-N 0.000 description 1
- VMUSSBBJCXBDBU-UHFFFAOYSA-N C=CC(N(C1)C=CC1Nc1ncnc(Nc(cc2)ccc2Oc2ccccc2)c1)=O Chemical compound C=CC(N(C1)C=CC1Nc1ncnc(Nc(cc2)ccc2Oc2ccccc2)c1)=O VMUSSBBJCXBDBU-UHFFFAOYSA-N 0.000 description 1
- WNVGOSPWYUICTQ-UHFFFAOYSA-N C=CC(N(CCC1)CC1Nc1cc(Nc(cc2)ccc2Oc2ccccc2)ncn1)=O Chemical compound C=CC(N(CCC1)CC1Nc1cc(Nc(cc2)ccc2Oc2ccccc2)ncn1)=O WNVGOSPWYUICTQ-UHFFFAOYSA-N 0.000 description 1
- RQRPPTFYXPRMQJ-WSDLNYQXSA-N C=CC(Nc1cc(N/C(/N=C\N)=C/CCCN(CC2)c3c2cccc3)ccc1)=O Chemical compound C=CC(Nc1cc(N/C(/N=C\N)=C/CCCN(CC2)c3c2cccc3)ccc1)=O RQRPPTFYXPRMQJ-WSDLNYQXSA-N 0.000 description 1
- TVZJFXDFZGMEPL-UHFFFAOYSA-N C=CC(Nc1cc(Nc2ncnc(Oc3cc(C(F)(F)F)ccc3)c2)ccc1)=O Chemical compound C=CC(Nc1cc(Nc2ncnc(Oc3cc(C(F)(F)F)ccc3)c2)ccc1)=O TVZJFXDFZGMEPL-UHFFFAOYSA-N 0.000 description 1
- RNTKTHMANBLYCF-UHFFFAOYSA-N C=CC(Nc1cccc(Nc2cc(Oc(cc3)ccc3Oc3ccccc3)ncn2)n1)=O Chemical compound C=CC(Nc1cccc(Nc2cc(Oc(cc3)ccc3Oc3ccccc3)ncn2)n1)=O RNTKTHMANBLYCF-UHFFFAOYSA-N 0.000 description 1
- BUQSZIWLZKNBLC-UHFFFAOYSA-N C=CC(Nc1cccc(Nc2ncnc(Nc(cc3)cc(C4CC4)c3OCC3=CC(F)=CCC3)c2)c1)=O Chemical compound C=CC(Nc1cccc(Nc2ncnc(Nc(cc3)cc(C4CC4)c3OCC3=CC(F)=CCC3)c2)c1)=O BUQSZIWLZKNBLC-UHFFFAOYSA-N 0.000 description 1
- BPGCSHREUPSOBZ-UHFFFAOYSA-N C=CS(Nc1cccc(Nc2ncnc(OC(C=CC3)=CC3C(F)(F)F)c2)c1)(=O)=O Chemical compound C=CS(Nc1cccc(Nc2ncnc(OC(C=CC3)=CC3C(F)(F)F)c2)c1)(=O)=O BPGCSHREUPSOBZ-UHFFFAOYSA-N 0.000 description 1
- DVLDHCKDNMHWQB-UHFFFAOYSA-N CC(C(c1cccc(Nc2ncnc(Nc(cc3)ccc3Oc3ccccc3)c2)c1)=O)=C Chemical compound CC(C(c1cccc(Nc2ncnc(Nc(cc3)ccc3Oc3ccccc3)c2)c1)=O)=C DVLDHCKDNMHWQB-UHFFFAOYSA-N 0.000 description 1
- KWMYVFPDXNCCKH-UHFFFAOYSA-N CC(C)=CC(c1cccc(Nc2ncnc(Nc(cc3)ccc3Oc3ccccc3)c2)c1)=O Chemical compound CC(C)=CC(c1cccc(Nc2ncnc(Nc(cc3)ccc3Oc3ccccc3)c2)c1)=O KWMYVFPDXNCCKH-UHFFFAOYSA-N 0.000 description 1
- DBHFVPQUYSHLFK-UHFFFAOYSA-N CN(C(C=C)=O)c1cccc(Nc2cc(Nc(cc3Cl)ccc3F)ncn2)c1 Chemical compound CN(C(C=C)=O)c1cccc(Nc2cc(Nc(cc3Cl)ccc3F)ncn2)c1 DBHFVPQUYSHLFK-UHFFFAOYSA-N 0.000 description 1
- LTASRTYKQQODNV-VMPITWQZSA-N CN(C)C/C=C/C(N(C)c1cc(Nc2ncnc(Nc(cc3Cl)ccc3F)c2)ccc1)=O Chemical compound CN(C)C/C=C/C(N(C)c1cc(Nc2ncnc(Nc(cc3Cl)ccc3F)c2)ccc1)=O LTASRTYKQQODNV-VMPITWQZSA-N 0.000 description 1
- XNOSGIQEBKFECM-BJMVGYQFSA-N CN(C)C/C=C/C(Nc1cccc(Nc2cc(Nc(cc3)cc(Cl)c3OCc3cc(F)ccc3)ncn2)c1)=O Chemical compound CN(C)C/C=C/C(Nc1cccc(Nc2cc(Nc(cc3)cc(Cl)c3OCc3cc(F)ccc3)ncn2)c1)=O XNOSGIQEBKFECM-BJMVGYQFSA-N 0.000 description 1
- PZTOMZJQXJFNPK-QPJJXVBHSA-N CN(C)C/C=C/C(Nc1cccc(Nc2ncnc(Nc(cc3Cl)ccc3F)c2)n1)=O Chemical compound CN(C)C/C=C/C(Nc1cccc(Nc2ncnc(Nc(cc3Cl)ccc3F)c2)n1)=O PZTOMZJQXJFNPK-QPJJXVBHSA-N 0.000 description 1
- KEBFJKIAGQTKMY-UHFFFAOYSA-N CN(c1ccccc1)c1cc(Nc2cc(NC(C=C)=O)ccc2)ccn1 Chemical compound CN(c1ccccc1)c1cc(Nc2cc(NC(C=C)=O)ccc2)ccn1 KEBFJKIAGQTKMY-UHFFFAOYSA-N 0.000 description 1
- ZBNNJYMQAROQAO-SNAWJCMRSA-N Cc(ccc(NC(/C=C/CN(C)C)=O)c1)c1Nc1ncnc(Nc(cc2Cl)ccc2F)c1 Chemical compound Cc(ccc(NC(/C=C/CN(C)C)=O)c1)c1Nc1ncnc(Nc(cc2Cl)ccc2F)c1 ZBNNJYMQAROQAO-SNAWJCMRSA-N 0.000 description 1
- PBKRZTJKEIMCGU-UHFFFAOYSA-N O=C(C1(CC1)S=O)Nc1cc(Nc2cc(NC(CC3)=CC(Cl)=C3OCc3ccccn3)ncn2)ccc1 Chemical compound O=C(C1(CC1)S=O)Nc1cc(Nc2cc(NC(CC3)=CC(Cl)=C3OCc3ccccn3)ncn2)ccc1 PBKRZTJKEIMCGU-UHFFFAOYSA-N 0.000 description 1
- HPIAUZVKQHGXGR-UHFFFAOYSA-N O=C(C1(CC1)S=O)Nc1cccc(Nc2ncnc(Nc(cc3)cc(Cl)c3F)c2)c1 Chemical compound O=C(C1(CC1)S=O)Nc1cccc(Nc2ncnc(Nc(cc3)cc(Cl)c3F)c2)c1 HPIAUZVKQHGXGR-UHFFFAOYSA-N 0.000 description 1
- XRNZNVGHFYMJHD-UHFFFAOYSA-N O=C(CCl)Nc1cccc(Nc2ncnc(Nc(cc3Cl)ccc3F)c2)c1 Chemical compound O=C(CCl)Nc1cccc(Nc2ncnc(Nc(cc3Cl)ccc3F)c2)c1 XRNZNVGHFYMJHD-UHFFFAOYSA-N 0.000 description 1
- 108091000080 Phosphotransferase Proteins 0.000 description 1
- 125000003342 alkenyl group Chemical group 0.000 description 1
- 230000002860 competitive effect Effects 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 210000002768 hair cell Anatomy 0.000 description 1
- 230000031146 intracellular signal transduction Effects 0.000 description 1
- 210000003734 kidney Anatomy 0.000 description 1
- 229940043355 kinase inhibitor Drugs 0.000 description 1
- 208000032839 leukemia Diseases 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 102000020233 phosphotransferase Human genes 0.000 description 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 description 1
- 108060006633 protein kinase Proteins 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US98143207P | 2007-10-19 | 2007-10-19 | |
| US60/981,432 | 2007-10-19 | ||
| US5200208P | 2008-05-09 | 2008-05-09 | |
| US61/052,002 | 2008-05-09 | ||
| PCT/US2008/011911 WO2009051822A1 (en) | 2007-10-19 | 2008-10-17 | Heteroaryl compounds and uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014112633A Division JP2014156489A (ja) | 2007-10-19 | 2014-05-30 | ヘテロアリール化合物およびその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011500685A JP2011500685A (ja) | 2011-01-06 |
| JP2011500685A5 true JP2011500685A5 (enExample) | 2012-11-22 |
| JP5600063B2 JP5600063B2 (ja) | 2014-10-01 |
Family
ID=40567710
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010529960A Expired - Fee Related JP5600063B2 (ja) | 2007-10-19 | 2008-10-17 | ヘテロアリール化合物およびその使用 |
| JP2014112633A Pending JP2014156489A (ja) | 2007-10-19 | 2014-05-30 | ヘテロアリール化合物およびその使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014112633A Pending JP2014156489A (ja) | 2007-10-19 | 2014-05-30 | ヘテロアリール化合物およびその使用 |
Country Status (8)
| Country | Link |
|---|---|
| US (5) | US7982036B2 (enExample) |
| EP (1) | EP2214486A4 (enExample) |
| JP (2) | JP5600063B2 (enExample) |
| CN (2) | CN105367503A (enExample) |
| AU (3) | AU2008314632B2 (enExample) |
| CA (2) | CA2920996A1 (enExample) |
| TW (2) | TWI475996B (enExample) |
| WO (1) | WO2009051822A1 (enExample) |
Families Citing this family (101)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2529621B1 (en) | 2006-09-22 | 2016-10-05 | Pharmacyclics LLC | Inhibitors of bruton's tyrosine kinase |
| US8809273B2 (en) | 2007-03-28 | 2014-08-19 | Pharmacyclics, Inc. | Inhibitors of Bruton's tyrosine kinase |
| US7989465B2 (en) * | 2007-10-19 | 2011-08-02 | Avila Therapeutics, Inc. | 4,6-disubstituted pyrimidines useful as kinase inhibitors |
| JP5600063B2 (ja) | 2007-10-19 | 2014-10-01 | セルジーン アビロミクス リサーチ， インコーポレイテッド | ヘテロアリール化合物およびその使用 |
| JP2011523646A (ja) | 2008-05-21 | 2011-08-18 | アリアド・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のリン誘導体 |
| US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
| US8338439B2 (en) * | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| AU2009262068C1 (en) * | 2008-06-27 | 2015-07-02 | Celgene Car Llc | Heteroaryl compounds and uses thereof |
| US11351168B1 (en) | 2008-06-27 | 2022-06-07 | Celgene Car Llc | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| CN102159214A (zh) | 2008-07-16 | 2011-08-17 | 药品循环公司 | 用于实体肿瘤的治疗的布鲁顿酪氨酸激酶的抑制剂 |
| JP2012501654A (ja) * | 2008-09-05 | 2012-01-26 | アビラ セラピューティクス， インコーポレイテッド | 不可逆的インヒビターの設計のためのアルゴリズム |
| KR101705158B1 (ko) * | 2009-05-05 | 2017-02-09 | 다나-파버 캔서 인스티튜트 인크. | Ｅｇｆｒ 억제제 및 질환 치료방법 |
| TW201103904A (en) | 2009-06-11 | 2011-02-01 | Hoffmann La Roche | Janus kinase inhibitor compounds and methods |
| CN102458402B (zh) | 2009-06-12 | 2013-10-02 | 百时美施贵宝公司 | 用作激酶调节剂的烟酰胺化合物 |
| EP2462123B1 (en) | 2009-08-04 | 2013-10-02 | Merck Sharp & Dohme Corp. | 4,5,6-trisubstituted pyrimidine derivatives as factor ixa inhibitors |
| CN102713618B (zh) | 2009-09-16 | 2015-07-15 | 新基阿维罗米克斯研究公司 | 蛋白激酶复合物和抑制剂 |
| PE20170202A1 (es) * | 2009-10-14 | 2017-03-24 | Xenon Pharmaceuticals Inc | Metodos sinteticos para compuestos espiro-oxoindol |
| WO2011082285A1 (en) | 2009-12-30 | 2011-07-07 | Avila Therapeutics, Inc. | Ligand-directed covalent modification of protein |
| CN102791131A (zh) * | 2010-01-13 | 2012-11-21 | 葛兰素史密斯克莱有限责任公司 | 化合物和方法 |
| BR112012029647A2 (pt) | 2010-05-21 | 2016-08-02 | Chemilia Ab | novos derivados de pirimidinas |
| MX380504B (es) | 2010-06-03 | 2025-03-12 | Pharmacyclics Llc | El uso de inhibidores de la tirosina quinasa de bruton (btk). |
| PH12013500246A1 (en) | 2010-08-10 | 2019-10-11 | Celgene Avilomics Res Inc | Besylate salt of a btk inhibitor |
| JP5956999B2 (ja) | 2010-11-01 | 2016-07-27 | セルジーン アヴィロミクス リサーチ， インコーポレイテッド | ヘテロアリール化合物およびその使用 |
| BR112013010564B1 (pt) | 2010-11-01 | 2021-09-21 | Celgene Car Llc | Compostos heterocíclicos e composições compreendendo os mesmos |
| EP2637502B1 (en) | 2010-11-10 | 2018-01-10 | Celgene CAR LLC | Mutant-selective egfr inhibitors and uses thereof |
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- 2008-10-17 CN CN201510792304.0A patent/CN105367503A/zh active Pending
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- 2008-10-17 WO PCT/US2008/011911 patent/WO2009051822A1/en not_active Ceased
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