JP2011500685A5 - - Google Patents
Download PDFInfo
- Publication number
- 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
- Authority
- JP
- Japan
- Prior art keywords
- ring
- composition
- substituted
- compound
- halogen
- 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 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) | CN101902911B (enExample) |
| AU (3) | AU2008314632B2 (enExample) |
| CA (2) | CA2920996A1 (enExample) |
| TW (2) | TWI552752B (enExample) |
| WO (1) | WO2009051822A1 (enExample) |
Families Citing this family (101)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL2526933T3 (pl) | 2006-09-22 | 2015-08-31 | Pharmacyclics Llc | Inhibitory kinazy tyrozynowej Brutona |
| US20120101113A1 (en) | 2007-03-28 | 2012-04-26 | 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 |
| US7982036B2 (en) | 2007-10-19 | 2011-07-19 | Avila Therapeutics, Inc. | 4,6-disubstitued pyrimidines useful as kinase inhibitors |
| EP2300013B2 (en) | 2008-05-21 | 2024-11-13 | Takeda Pharmaceutical Company Limited | Phosphorous derivatives as kinase inhibitors |
| US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
| NZ603525A (en) | 2008-06-27 | 2015-02-27 | Celgene Avilomics Res Inc | Pyrimidine based compound and uses thereof |
| US8338439B2 (en) * | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| US11351168B1 (en) | 2008-06-27 | 2022-06-07 | Celgene Car Llc | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| CA2730930C (en) | 2008-07-16 | 2015-01-13 | Pharmacyclics, Inc. | Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors |
| KR101341876B1 (ko) * | 2008-09-05 | 2013-12-20 | 셀진 아빌로믹스 리서치, 인코포레이티드 | 비가역 인히비터 디자인을 위한 알고리즘 |
| JP5918693B2 (ja) * | 2009-05-05 | 2016-05-18 | ダナ ファーバー キャンサー インスティテュート インコーポレイテッド | Egfr阻害剤及び疾患の治療方法 |
| TW201103904A (en) | 2009-06-11 | 2011-02-01 | Hoffmann La Roche | Janus kinase inhibitor compounds and methods |
| JP2012529535A (ja) | 2009-06-12 | 2012-11-22 | ブリストル−マイヤーズ スクイブ カンパニー | キナーゼモジュレーターとして有用なニコチンアミド化合物 |
| WO2011017296A1 (en) * | 2009-08-04 | 2011-02-10 | Schering Corporation | 4, 5, 6-trisubstituted pyrimidine derivatives as factor ixa inhibitors |
| US9556426B2 (en) | 2009-09-16 | 2017-01-31 | Celgene Avilomics Research, Inc. | Protein kinase conjugates and inhibitors |
| CN102753556B (zh) * | 2009-10-14 | 2015-05-13 | 泽农医药公司 | 螺-羟吲哚化合物的合成方法 |
| AU2010339456A1 (en) * | 2009-12-30 | 2012-07-05 | Celgene Avilomics Research, Inc. | Ligand-directed covalent modification of protein |
| EA201290642A1 (ru) * | 2010-01-13 | 2013-05-30 | ГЛЭКСОСМИТКЛАЙН ЭлЭлСи | Соединения и способы |
| BR112012029647A2 (pt) | 2010-05-21 | 2016-08-02 | Chemilia Ab | novos derivados de pirimidinas |
| NZ772688A (en) | 2010-06-03 | 2022-09-30 | Pharmacyclics Llc | The use of inhibitors of bruton’s tyrosine kinase (btk) |
| CN105566229A (zh) | 2010-08-10 | 2016-05-11 | 西建阿维拉米斯研究公司 | Btk抑制剂的苯磺酸盐及其用途和制备方法 |
| US9238629B2 (en) | 2010-11-01 | 2016-01-19 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| SG10201508958WA (en) | 2010-11-01 | 2015-11-27 | Celgene Avilomics Res Inc | Heterocyclic Compounds And Uses Thereof |
| EP2637502B1 (en) | 2010-11-10 | 2018-01-10 | Celgene CAR LLC | Mutant-selective egfr inhibitors and uses thereof |
| JP5886411B2 (ja) | 2011-03-24 | 2016-03-16 | ノビガ・リサーチ・エービーNoviga Research AB | 新規のピリミジン誘導体 |
| EP2704572B1 (en) | 2011-05-04 | 2015-12-30 | Ariad Pharmaceuticals, Inc. | Compounds for inhibiting cell proliferation in egfr-driven cancers |
| EA031153B1 (ru) | 2011-06-10 | 2018-11-30 | Мерк Патент Гмбх | Применение пиримидиновых соединений с btk ингибирующей активностью |
| MY161925A (en) | 2011-07-27 | 2017-05-15 | Astrazeneca Ab | 2 - (2, 4, 5 - substituted -anilino) pyrimidine derivatives as egfr modulators useful for treating cancer |
| JP2014532658A (ja) | 2011-10-28 | 2014-12-08 | 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 | ブルトン型チロシンキナーゼ疾患または障害を治療する方法 |
| AU2013207712B2 (en) | 2012-01-13 | 2017-08-31 | Acea Biosciences Inc. | Heterocyclic compounds and uses as anticancer agents. |
| US9034885B2 (en) | 2012-01-13 | 2015-05-19 | Acea Biosciences Inc. | EGFR modulators and uses thereof |
| US9586965B2 (en) | 2012-01-13 | 2017-03-07 | Acea Biosciences Inc. | Pyrrolo[2,3-d]pyrimidine compounds as inhibitors of protein kinases |
| US9464089B2 (en) | 2012-01-13 | 2016-10-11 | Acea Biosciences Inc. | Heterocyclic compounds and uses thereof |
| WO2013108754A1 (ja) | 2012-01-17 | 2013-07-25 | アステラス製薬株式会社 | ピラジンカルボキサミド化合物 |
| JP6317319B2 (ja) | 2012-03-15 | 2018-04-25 | セルジーン シーエーアール エルエルシー | 上皮成長因子受容体キナーゼ阻害剤の固体形態 |
| CA2866857C (en) | 2012-03-15 | 2021-03-09 | Celgene Avilomics Research, Inc. | Salts of an epidermal growth factor receptor kinase inhibitor |
| US9353062B2 (en) | 2012-04-04 | 2016-05-31 | Hangzhouderenyucheng Biotechnology Ltd | Substituted quinolines as bruton's tyrosine kinases inhibitors |
| WO2013161848A1 (ja) * | 2012-04-27 | 2013-10-31 | カルナバイオサイエンス株式会社 | 新規1,2,4-トリアジン誘導体 |
| JP6469567B2 (ja) * | 2012-05-05 | 2019-02-13 | 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 | Egfr発動性がんの細胞増殖阻害用化合物 |
| WO2013173518A1 (en) * | 2012-05-16 | 2013-11-21 | Pharmacyclics, Inc. | Inhibitors of bruton's tyrosine kinase |
| WO2013184572A1 (en) | 2012-06-04 | 2013-12-12 | Pharmacyclics, Inc. | Crystalline forms of a bruton's tyrosine kinase inhibitor |
| AU2013293087B2 (en) | 2012-07-24 | 2017-08-31 | Pharmacyclics Llc | Mutations associated with resistance to inhibitors of Bruton's tyrosine kinase (BTK) |
| US9714450B2 (en) | 2012-08-31 | 2017-07-25 | New York University | Methods for diagnosing and treating schizophrenia |
| CN104583195B (zh) * | 2012-09-12 | 2018-08-17 | 山东亨利医药科技有限责任公司 | 作为酪氨酸激酶抑制剂的含氮杂芳环衍生物 |
| SG11201503842PA (en) | 2012-11-15 | 2015-06-29 | Pharmacyclics Inc | Pyrrolopyrimidine compounds as kinase inhibitors |
| EP2935226A4 (en) | 2012-12-21 | 2016-11-02 | Celgene Avilomics Res Inc | HETEROARYL COMPOUNDS AND USES THEREOF |
| US9561228B2 (en) | 2013-02-08 | 2017-02-07 | Celgene Avilomics Research, Inc. | ERK inhibitors and uses thereof |
| US9611283B1 (en) | 2013-04-10 | 2017-04-04 | Ariad Pharmaceuticals, Inc. | Methods for inhibiting cell proliferation in ALK-driven cancers |
| SI2989106T1 (sl) | 2013-04-25 | 2017-07-31 | Beigene, Ltd. | Zlite heterociklične spojine kot inhibitorji beljakovinske kinaze |
| EP2999702A4 (en) | 2013-05-21 | 2017-01-11 | Jiangsu Medolution Ltd. | Substituted pyrazolopyrimidines as kinases inhibitors |
| KR102173433B1 (ko) | 2013-07-11 | 2020-11-04 | 에이시아 바이오사이언시스 인코포레이티드. | 키나아제 억제제로써의 피리미딘 유도체 |
| US9421208B2 (en) | 2013-08-02 | 2016-08-23 | Pharmacyclics Llc | Methods for the treatment of solid tumors |
| IN2013MU02611A (enExample) | 2013-08-07 | 2015-06-12 | Cadila Healthcare Ltd | |
| EP3033079B1 (en) | 2013-08-12 | 2018-10-31 | Pharmacyclics LLC | Methods for the treatment of her2 amplified cancer |
| WO2015025197A1 (en) | 2013-08-22 | 2015-02-26 | Jubilant Biosys Limited | Substituted pyrimidine compounds, compositions and medicinal applications thereof |
| US9492471B2 (en) | 2013-08-27 | 2016-11-15 | Celgene Avilomics Research, Inc. | Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase |
| LT3702373T (lt) | 2013-09-13 | 2022-11-10 | Beigene Switzerland Gmbh | Anti-pd1 antikūnai ir jų naudojimas terapijai ir diagnostikai |
| KR20160063366A (ko) * | 2013-10-21 | 2016-06-03 | 메르크 파텐트 게엠베하 | Btk 저해제로서 헤테로아릴 화합물 및 이들의 용도 |
| CN111265531B (zh) | 2013-10-25 | 2023-11-10 | 药品循环有限责任公司 | 治疗和预防移植物抗宿主病的方法 |
| JP6879740B2 (ja) * | 2013-12-13 | 2021-06-02 | ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド | リンパ形質細胞性リンパ腫を処置する方法 |
| US9415049B2 (en) | 2013-12-20 | 2016-08-16 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| CA2942528A1 (en) | 2014-03-20 | 2015-09-24 | Pharmacyclics Inc. | Phospholipase c gamma 2 and resistance associated mutations |
| TWI726608B (zh) | 2014-07-03 | 2021-05-01 | 英屬開曼群島商百濟神州有限公司 | 抗pd-l1抗體及其作為治療及診斷之用途 |
| CA2959602A1 (en) | 2014-08-01 | 2016-02-04 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase |
| US9545407B2 (en) | 2014-08-07 | 2017-01-17 | Pharmacyclics Llc | Formulations of a bruton's tyrosine kinase inhibitor |
| US10005760B2 (en) | 2014-08-13 | 2018-06-26 | Celgene Car Llc | Forms and compositions of an ERK inhibitor |
| WO2016029839A1 (zh) * | 2014-08-25 | 2016-03-03 | 四川海思科制药有限公司 | 一种(取代的苯基)(取代的嘧啶)胺基衍生物及其制备方法和药物用途 |
| CN105085489B (zh) * | 2014-11-05 | 2019-03-01 | 益方生物科技(上海)有限公司 | 嘧啶或吡啶类化合物、其制备方法和医药用途 |
| IL315294A (en) | 2015-03-03 | 2024-10-01 | Pharmacyclics Llc | Pharmaceutical formulations of bruton's tyrosine kinase inhibitor |
| CN104860890B (zh) * | 2015-04-29 | 2018-03-13 | 上海泓博智源医药股份有限公司 | T790m突变型egfr的抑制剂及其在制备抗肿瘤药物中的应用 |
| JP6863901B2 (ja) * | 2015-05-13 | 2021-04-28 | 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 | キナーゼ阻害のためのヘテロアリール化合物 |
| MX2018002554A (es) | 2015-08-31 | 2018-08-14 | Pharmacyclics Llc | Combinaciones de inhibidores de btk para tratar mieloma multiple. |
| WO2017059702A1 (en) | 2015-10-09 | 2017-04-13 | Acea Biosciences, Inc | Pharmaceutical salts, physical forms, and compositions of pyrrolopyrimidine kinase inhibitors, and methods of making same |
| JP6983661B2 (ja) | 2015-12-24 | 2021-12-17 | 協和キリン株式会社 | α、β不飽和アミド化合物 |
| CN106928150B (zh) * | 2015-12-31 | 2020-07-31 | 恩瑞生物医药科技(上海)有限公司 | 丙烯酰胺苯胺衍生物及其药学上的应用 |
| WO2018007885A1 (en) | 2016-07-05 | 2018-01-11 | Beigene, Ltd. | COMBINATION OF A PD-l ANTAGONIST AND A RAF INHIBITOR FOR TREATING CANCER |
| EP4509183A3 (en) | 2016-08-16 | 2025-05-21 | BeiGene Switzerland GmbH | Crystalline form of (s)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof |
| AU2017313085B2 (en) | 2016-08-19 | 2024-06-20 | Beone Medicines I Gmbh | Use of a combination comprising a Btk inhibitor for treating cancers |
| MX390121B (es) | 2016-09-19 | 2025-03-20 | Mei Pharma Inc | Combinaciones de un inhibidor de btk y un inhibidor de pi3k para tratar neoplasias malignas hematológicas. |
| MA46783A (fr) | 2016-11-03 | 2019-09-11 | Juno Therapeutics Inc | Polythérapie de type thérapie cellulaire t et inhibiteur de btk |
| CN106749042B (zh) * | 2016-11-16 | 2019-01-22 | 大连医科大学 | 磺酰胺基嘧啶类化合物,组合物及用途 |
| MA46995A (fr) | 2016-12-03 | 2019-10-09 | Acerta Pharma Bv | Méthodes et compositions pour l'utilisation de lymphocytes t thérapeutiques en association avec des inhibiteurs de kinase |
| WO2018137681A1 (en) | 2017-01-25 | 2018-08-02 | Beigene, Ltd. | Crystalline forms of (s) -7- (1- (but-2-ynoyl) piperidin-4-yl) -2- (4-phenoxyphenyl) -4, 5, 6, 7-tetrahy dropyrazolo [1, 5-a] pyrimidine-3-carboxamide, preparation, and uses thereof |
| US11498922B2 (en) | 2017-04-07 | 2022-11-15 | ACEA Therapeutics, Inc. | Pharmaceutical composition comprising N-(3-((2-((3-fluoro-4-(4-methylpiperazin-1-yl phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenylacrylamide |
| WO2018235926A1 (ja) * | 2017-06-23 | 2018-12-27 | 協和発酵キリン株式会社 | α、β不飽和アミド化合物 |
| KR102757960B1 (ko) | 2017-06-26 | 2025-01-22 | 베이진 엘티디 | 간세포암(hepatocellular carcinoma: HCC)에 대한 면역 치료 |
| US11377449B2 (en) | 2017-08-12 | 2022-07-05 | Beigene, Ltd. | BTK inhibitors with improved dual selectivity |
| JP2019062834A (ja) * | 2017-10-03 | 2019-04-25 | アークレイ株式会社 | ヒトegfrのc797s(g2390c)変異検出用プローブ、ヒトegfrのc797s(g2390c)変異検出用キット、及びヒトegfrのc797s(g2390c)変異の検出方法 |
| CN111801334B (zh) | 2017-11-29 | 2023-06-09 | 百济神州瑞士有限责任公司 | 使用包含btk抑制剂的组合治疗惰性或侵袭性b-细胞淋巴瘤 |
| JP7410877B2 (ja) | 2018-05-03 | 2024-01-10 | ジュノー セラピューティクス インコーポレイテッド | キメラ抗原受容体(car)t細胞療法とキナーゼ阻害剤の併用療法 |
| CN108715834B (zh) * | 2018-06-01 | 2021-09-14 | 天晴干细胞股份有限公司 | 一种富含cd41+、cd81+微囊的血小板裂解液制备方法 |
| WO2020249001A1 (zh) | 2019-06-10 | 2020-12-17 | 百济神州瑞士有限责任公司 | 一种含有布鲁顿氏酪氨酸激酶抑制剂的口服固体片剂及其制备方法 |
| CA3213079A1 (en) | 2021-04-13 | 2022-10-20 | Kristin Lynne ANDREWS | Amino-substituted heterocycles for treating cancers with egfr mutations |
| EP4382520A4 (en) * | 2021-08-02 | 2025-07-16 | Abbisko Therapeutics Co Ltd | PYRIMIDINE-4,6-DIAMINE DERIVATIVE, ITS PREPARATION PROCESS AND ITS PHARMACEUTICAL USE |
| TW202317106A (zh) * | 2021-08-27 | 2023-05-01 | 南韓商柳韓洋行 | 作為egfr抑制劑之取代胺基吡啶化合物 |
| CN114621922A (zh) * | 2022-02-15 | 2022-06-14 | 中山大学附属第五医院 | 一种大鼠海绵体神经来源施旺细胞的提取纯化和培养方法 |
| US20250302954A1 (en) | 2022-05-11 | 2025-10-02 | Celgene Corporation | Methods to overcome drug resistance by re-sensitizing cancer cells to treatment with a prior therapy via treatment with a t cell therapy |
| US11786531B1 (en) | 2022-06-08 | 2023-10-17 | Beigene Switzerland Gmbh | Methods of treating B-cell proliferative disorder |
| JP2025530372A (ja) * | 2022-09-15 | 2025-09-11 | クルゲン(シャンハイ),インク. | 修飾タンパク質ならびにタンパク質結合剤および分解剤 |
| CN116444728B (zh) * | 2023-04-20 | 2025-02-28 | 浙江南洋华诚科技股份有限公司 | 一种风电电容器高耐压高耐温薄膜及其制备方法 |
Family Cites Families (55)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH0741461A (ja) | 1993-05-27 | 1995-02-10 | Eisai Co Ltd | スルホン酸エステル誘導体 |
| GB9325217D0 (en) * | 1993-12-09 | 1994-02-09 | Zeneca Ltd | Pyrimidine derivatives |
| US5977117A (en) * | 1996-01-05 | 1999-11-02 | Texas Biotechnology Corporation | Substituted phenyl compounds and derivatives thereof that modulate the activity of endothelin |
| US5994375A (en) * | 1996-02-12 | 1999-11-30 | Berlex Laboratories, Inc. | Benzamidine derivatives substituted by amino acid and hydroxy acid derivatives and their use as anti-coagulants |
| AU751573C (en) | 1998-03-27 | 2003-10-09 | Janssen Pharmaceutica N.V. | HIV inhibiting pyrimidine derivatives |
| ES2361146T3 (es) * | 1998-03-27 | 2011-06-14 | Janssen Pharmaceutica Nv | Derivados de la piramidina inhibitatoria de vih. |
| US6303652B1 (en) * | 1998-08-21 | 2001-10-16 | Hughes Institute | BTK inhibitors and methods for their identification and use |
| US6632820B1 (en) * | 1998-08-29 | 2003-10-14 | Astrazeneca Ab | Pyrimidine compounds |
| US6262088B1 (en) * | 1998-11-19 | 2001-07-17 | Berlex Laboratories, Inc. | Polyhydroxylated monocyclic N-heterocyclic derivatives as anti-coagulants |
| US6495558B1 (en) | 1999-01-22 | 2002-12-17 | Amgen Inc. | Kinase inhibitors |
| GB9905075D0 (en) * | 1999-03-06 | 1999-04-28 | Zeneca Ltd | Chemical compounds |
| GB9907658D0 (en) | 1999-04-06 | 1999-05-26 | Zeneca Ltd | Chemical compounds |
| AU5020400A (en) | 1999-05-20 | 2000-12-12 | E.I. Du Pont De Nemours And Company | Heteroaryloxypyrimidine insecticides and acaricides |
| DE60025837T2 (de) * | 1999-09-24 | 2006-11-02 | Janssen Pharmaceutica N.V. | Antivirale feste dispersionen |
| GB9924092D0 (en) | 1999-10-13 | 1999-12-15 | Zeneca Ltd | Pyrimidine derivatives |
| AU2700301A (en) * | 2000-01-31 | 2001-08-14 | Pfizer Products Inc. | Pyrimidine carboxamides useful as inhibitors of pde4 isozymes |
| CA2417500C (en) | 2000-07-28 | 2008-11-18 | Georgetown University Medical Center | Erbb-2 selective small molecule kinase inhibitors |
| US20020137755A1 (en) * | 2000-12-04 | 2002-09-26 | Bilodeau Mark T. | Tyrosine kinase inhibitors |
| US6881737B2 (en) | 2001-04-11 | 2005-04-19 | Amgen Inc. | Substituted triazinyl acrylamide derivatives and methods of use |
| MXPA04004178A (es) * | 2001-11-01 | 2004-09-06 | Janssen Pharmaceutica Nv | Heteroarilaminas como inhibidores de glucogeno cintasa cinasa 3beta. |
| DK1442024T3 (da) * | 2001-11-01 | 2008-06-30 | Janssen Pharmaceutica Nv | Aminobenzamidderivater som glycogensystasekinase 3 beta-inhibitorer |
| MXPA04005027A (es) * | 2001-11-28 | 2004-08-11 | Btg Int Ltd | Preventivos o remedios para la enfermedad de alzheimer, o inhibidores de la formacion de fibrillas de proteina amiloide, que incluyen un compuesto heteroarilo que contiene nitrogeno. |
| US6841664B2 (en) | 2002-07-25 | 2005-01-11 | Enanra Pharmaceuticals, Inc. | 6,11-4-carbon bridged ketolides |
| AR039540A1 (es) | 2002-05-13 | 2005-02-23 | Tibotec Pharm Ltd | Compuestos microbicidas con contenido de pirimidina o triazina |
| TW200406374A (en) * | 2002-05-29 | 2004-05-01 | Novartis Ag | Diaryl urea derivatives useful for the treatment of protein kinase dependent diseases |
| DE10226943A1 (de) * | 2002-06-17 | 2004-01-08 | Bayer Ag | Phenylaminopyrimidine und ihre Verwendung |
| US20040002395A1 (en) * | 2002-06-27 | 2004-01-01 | Poynor Raymond L. | Bridge weight for metal wood golf club |
| CA2439440A1 (en) * | 2002-09-05 | 2004-03-05 | Emory University | Treatment of tuberous sclerosis associated neoplasms |
| AU2002951853A0 (en) | 2002-10-04 | 2002-10-24 | Commonwealth Scientific And Industrial Research Organisation | Crystal structure of erbb2 and uses thereof |
| US20050014753A1 (en) | 2003-04-04 | 2005-01-20 | Irm Llc | Novel compounds and compositions as protein kinase inhibitors |
| CA2518961A1 (en) | 2003-04-07 | 2004-10-28 | Praecis Pharmaceuticals, Inc. | Methods of measuring the ability of a test compound to inactivate a biological target in cells of a subject |
| AU2004257260A1 (en) | 2003-07-10 | 2005-01-27 | Neurogen Corporation | Substituted heterocyclic diarylamine analogues |
| JPWO2005040135A1 (ja) * | 2003-10-24 | 2007-03-08 | 小野薬品工業株式会社 | 抗ストレス薬およびその医薬用途 |
| TW200529849A (en) * | 2003-11-28 | 2005-09-16 | Novartis Ag | Diaryl urea derivatives in the treatment of protein kinase dependent diseases |
| US20080207613A1 (en) * | 2004-01-12 | 2008-08-28 | Cytopia Research Pty Ltd | Selective Kinase Inhibitors |
| WO2005105988A2 (en) * | 2004-04-28 | 2005-11-10 | Vertex Pharmaceuticals Incorporated | Crystal structure of human jak3 kinase domain complex and binding pockets thereof |
| MXPA06014747A (es) * | 2004-06-28 | 2007-02-16 | Altana Pharma Ag | Pirimidinas 4,6-disustituidas y su uso como inhibidores de proteina cinasa. |
| EP1805208A2 (en) | 2004-10-20 | 2007-07-11 | Proteolix, Inc. | Labeled compounds for proteasome inhibition |
| MY169441A (en) | 2004-12-08 | 2019-04-11 | Janssen Pharmaceutica Nv | 2,4, (4,6) pyrimidine derivatives |
| DE102005016634A1 (de) | 2005-04-12 | 2006-10-19 | Merck Patent Gmbh | Neuartige Aza-Hetercyclen als Kinase-Inhibitoren |
| WO2006128129A2 (en) | 2005-05-26 | 2006-11-30 | Synta Pharmaceuticals Corp. | Method for treating cancer |
| WO2006128172A2 (en) | 2005-05-26 | 2006-11-30 | Synta Pharmaceuticals Corp. | Method for treating b cell regulated autoimmune disorders |
| JP5255438B2 (ja) * | 2005-07-26 | 2013-08-07 | 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 | プロテインキナーゼ阻害薬として有用なベンズイミダゾール |
| KR20080053954A (ko) * | 2005-11-03 | 2008-06-16 | 아이알엠 엘엘씨 | 단백질 키나제 억제제 |
| WO2007081630A2 (en) | 2005-12-21 | 2007-07-19 | Janssen Pharmaceutica, N.V. | Substituted pyrimidinyl kinase inhibitors |
| KR20080110998A (ko) | 2006-01-30 | 2008-12-22 | 엑셀리시스, 인코포레이티드 | Jak2 조절자로서 4아릴2아미노피리미딘 또는 4아릴2아미노알킬피리미딘 및 이들을 포함하는 약제학적 조성물 |
| WO2007127473A2 (en) | 2006-04-27 | 2007-11-08 | Intezyne Technologies, Inc. | Poly (ethylene glycol) containing chemically disparate endgroups |
| PL2526933T3 (pl) * | 2006-09-22 | 2015-08-31 | Pharmacyclics Llc | Inhibitory kinazy tyrozynowej Brutona |
| ES2403546T3 (es) | 2006-11-03 | 2013-05-20 | Pharmacyclics, Inc. | Sonda de actividad de la tirosina-cinasa de Bruton y procedimiento de utilización |
| ES2702362T3 (es) | 2007-01-31 | 2019-02-28 | Ym Biosciences Australia Pty | Compuestos a base de tiopirimidina y usos de los mismos |
| EP2014657A1 (de) * | 2007-06-21 | 2009-01-14 | Bayer Schering Pharma Aktiengesellschaft | Diaminopyrimidine als Modulatoren des EP2-Rezeptors |
| US7989465B2 (en) | 2007-10-19 | 2011-08-02 | Avila Therapeutics, Inc. | 4,6-disubstituted pyrimidines useful as kinase inhibitors |
| US7982036B2 (en) | 2007-10-19 | 2011-07-19 | Avila Therapeutics, Inc. | 4,6-disubstitued pyrimidines useful as kinase inhibitors |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| NZ603525A (en) | 2008-06-27 | 2015-02-27 | Celgene Avilomics Res Inc | Pyrimidine based compound and uses thereof |
-
2008
- 2008-10-17 US US12/253,424 patent/US7982036B2/en not_active Expired - Fee Related
- 2008-10-17 WO PCT/US2008/011911 patent/WO2009051822A1/en not_active Ceased
- 2008-10-17 TW TW103145233A patent/TWI552752B/zh not_active IP Right Cessation
- 2008-10-17 EP EP08839939A patent/EP2214486A4/en not_active Withdrawn
- 2008-10-17 AU AU2008314632A patent/AU2008314632B2/en not_active Ceased
- 2008-10-17 TW TW097139912A patent/TWI475996B/zh not_active IP Right Cessation
- 2008-10-17 CA CA2920996A patent/CA2920996A1/en not_active Abandoned
- 2008-10-17 JP JP2010529960A patent/JP5600063B2/ja not_active Expired - Fee Related
- 2008-10-17 CN CN200880121536.1A patent/CN101902911B/zh not_active Expired - Fee Related
- 2008-10-17 CA CA2702674A patent/CA2702674C/en not_active Expired - Fee Related
- 2008-10-17 CN CN201510792304.0A patent/CN105367503A/zh active Pending
-
2011
- 2011-02-01 US US13/018,624 patent/US8445498B2/en not_active Expired - Fee Related
-
2013
- 2013-05-02 US US13/875,755 patent/US9040541B2/en not_active Expired - Fee Related
-
2014
- 2014-05-30 JP JP2014112633A patent/JP2014156489A/ja active Pending
-
2015
- 2015-04-22 US US14/693,489 patent/US9393246B2/en not_active Expired - Fee Related
- 2015-05-18 AU AU2015202675A patent/AU2015202675B2/en not_active Expired - Fee Related
-
2016
- 2016-07-12 US US15/208,368 patent/US20160311780A1/en not_active Abandoned
- 2016-11-10 AU AU2016256754A patent/AU2016256754A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2013515786A5 (enExample) | ||
| ES2966917T3 (es) | Nuevo derivado de pirimidina que tiene el efecto de inhibir el crecimiento de células cancerosas y composición farmacéutica que contiene el mismo | |
| US10570141B2 (en) | Substituted pyrrolopyrimidine CDK inhibitor, pharmaceutical composition containing same and use thereof | |
| AU2016245864B2 (en) | Substituted quinazoline compounds and methods of use thereof | |
| ES2928169T3 (es) | Derivados de 4-(3H-indol-5-il)-N-(piridin-2-il)pirimidin-2-amina como inhibidores de proteína cinasa, y método de preparación y uso médico de los mismos | |
| JP6678655B2 (ja) | Rafキナーゼ阻害剤としての化合物および組成物 | |
| Eldehna et al. | Amido/ureidosubstituted benzenesulfonamides-isatin conjugates as low nanomolar/subnanomolar inhibitors of the tumor-associated carbonic anhydrase isoform XII | |
| ES2609296T3 (es) | Análogos de triazina y su uso como agentes terapéuticos y sondas de diagnóstico | |
| AU2012239791B2 (en) | Protein kinase inhibitors | |
| JP2018532737A5 (enExample) | ||
| JP2021522275A (ja) | サイクリン依存性キナーゼ阻害剤としての2−アミノ−ピリジンまたは2−アミノ−ピリミジン誘導体 | |
| CN117447479B (zh) | 一种靶向肿瘤免疫激酶的吡咯并吡嗪衍生物、制备方法及其应用 | |
| JP2018526413A5 (enExample) | ||
| JP2017511360A5 (enExample) | ||
| JP2016519673A5 (enExample) | ||
| CY1115171T1 (el) | Ιατρικο φαρμακο | |
| CA3238572A1 (en) | Selective parp1 inhibitor and application thereof | |
| JP2019501919A (ja) | スルファミド誘導体およびその製造方法と応用 | |
| EP3492469A1 (en) | Compound as selective jak inhibitor, and salt and therapeutic use thereof | |
| US9340491B2 (en) | Nitrile derivatives and their pharmaceutical use and compositions | |
| ES2958528T3 (es) | Macrociclos sustituidos útiles como inhibidores de quinasas | |
| US20240051940A1 (en) | Sulfonamides with egfr inhibition activities and their use thereof | |
| ES2969546T3 (es) | Técnica de combiterapia para el agente inhibidor de Axl y el inhibidor de la tirosina··cinasa del EGFR | |
| US20120329767A1 (en) | Methods and Compositions for Treating Cancer | |
| JP2018520167A (ja) | PI3K/mTOR阻害剤としての溶融キノリン化合物 |