JP2013515786A5 - - Google Patents
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- JP2013515786A5 JP2013515786A5 JP2012547280A JP2012547280A JP2013515786A5 JP 2013515786 A5 JP2013515786 A5 JP 2013515786A5 JP 2012547280 A JP2012547280 A JP 2012547280A JP 2012547280 A JP2012547280 A JP 2012547280A JP 2013515786 A5 JP2013515786 A5 JP 2013515786A5
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- JP
- Japan
- Prior art keywords
- ring
- substituted
- nitrogen
- groups
- membered
- 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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- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 122
- 229910052757 nitrogen Inorganic materials 0.000 claims description 90
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 78
- 229910052760 oxygen Inorganic materials 0.000 claims description 78
- 239000001301 oxygen Substances 0.000 claims description 78
- 125000005842 heteroatom Chemical group 0.000 claims description 74
- 229910052717 sulfur Inorganic materials 0.000 claims description 66
- 239000011593 sulfur Substances 0.000 claims description 66
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 65
- 229920006395 saturated elastomer Polymers 0.000 claims description 61
- 229910052736 halogen Inorganic materials 0.000 claims description 56
- 150000002367 halogens Chemical group 0.000 claims description 56
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 49
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 45
- 208000035475 disorder Diseases 0.000 claims description 43
- 239000000203 mixture Substances 0.000 claims description 42
- 125000001931 aliphatic group Chemical group 0.000 claims description 36
- 125000003118 aryl group Chemical group 0.000 claims description 34
- 150000001875 compounds Chemical class 0.000 claims description 33
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 31
- 230000001404 mediated effect Effects 0.000 claims description 29
- 125000000623 heterocyclic group Chemical group 0.000 claims description 26
- 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
- 229910052739 hydrogen Inorganic materials 0.000 claims description 24
- 239000001257 hydrogen Substances 0.000 claims description 24
- 125000002619 bicyclic group Chemical group 0.000 claims description 23
- 102100029823 Tyrosine-protein kinase BTK Human genes 0.000 claims description 21
- 125000001183 hydrocarbyl group Chemical group 0.000 claims description 21
- 230000000694 effects Effects 0.000 claims description 18
- 125000004429 atom Chemical group 0.000 claims description 15
- 101000934996 Homo sapiens Tyrosine-protein kinase JAK3 Proteins 0.000 claims description 13
- 102100025387 Tyrosine-protein kinase JAK3 Human genes 0.000 claims description 13
- 125000004980 cyclopropylene group Chemical group 0.000 claims description 12
- 125000004043 oxo group Chemical group O=* 0.000 claims description 12
- 150000003839 salts Chemical class 0.000 claims description 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 9
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 9
- 230000002401 inhibitory effect Effects 0.000 claims description 9
- 206010009944 Colon cancer Diseases 0.000 claims description 8
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 8
- 108010009978 Tec protein-tyrosine kinase Proteins 0.000 claims description 8
- 108091000080 Phosphotransferase Proteins 0.000 claims description 7
- 102100040177 Tyrosine-protein kinase Tec Human genes 0.000 claims description 7
- 102000020233 phosphotransferase Human genes 0.000 claims description 7
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 claims description 6
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 6
- 208000023275 Autoimmune disease Diseases 0.000 claims description 6
- 206010028980 Neoplasm Diseases 0.000 claims description 6
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 6
- 102100023345 Tyrosine-protein kinase ITK/TSK Human genes 0.000 claims description 6
- 125000000217 alkyl group Chemical group 0.000 claims description 6
- 210000000988 bone and bone Anatomy 0.000 claims description 6
- 125000002837 carbocyclic group Chemical group 0.000 claims description 6
- 229910052799 carbon Inorganic materials 0.000 claims description 6
- 206010012601 diabetes mellitus Diseases 0.000 claims description 6
- 201000010099 disease Diseases 0.000 claims description 6
- 150000002431 hydrogen Chemical group 0.000 claims description 6
- 208000027866 inflammatory disease Diseases 0.000 claims description 6
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 6
- 201000002528 pancreatic cancer Diseases 0.000 claims description 6
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 6
- 102100027907 Cytoplasmic tyrosine-protein kinase BMX Human genes 0.000 claims description 5
- 208000020084 Bone disease Diseases 0.000 claims description 4
- 208000012659 Joint disease Diseases 0.000 claims description 4
- 208000003019 Neurofibromatosis 1 Diseases 0.000 claims description 4
- 125000002947 alkylene group Chemical group 0.000 claims description 4
- 201000011510 cancer Diseases 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 208000002761 neurofibromatosis 2 Diseases 0.000 claims description 4
- 229940124597 therapeutic agent Drugs 0.000 claims description 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 3
- 125000001424 substituent group Chemical group 0.000 claims description 3
- -1 (isopropyl) — Chemical class 0.000 claims description 2
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims description 2
- 208000014697 Acute lymphocytic leukaemia Diseases 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
- 206010005949 Bone cancer Diseases 0.000 claims description 2
- 208000018084 Bone neoplasm Diseases 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- 208000011231 Crohn disease Diseases 0.000 claims description 2
- 208000018522 Gastrointestinal disease Diseases 0.000 claims description 2
- 208000002250 Hematologic Neoplasms Diseases 0.000 claims description 2
- 208000017604 Hodgkin disease Diseases 0.000 claims description 2
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims description 2
- 208000010747 Hodgkins lymphoma 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
- 206010027476 Metastases Diseases 0.000 claims description 2
- 208000034578 Multiple myelomas Diseases 0.000 claims description 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims description 2
- 208000001132 Osteoporosis Diseases 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 2
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma 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
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 239000002246 antineoplastic agent Substances 0.000 claims description 2
- 208000035269 cancer or benign tumor Diseases 0.000 claims description 2
- 208000032852 chronic lymphocytic leukemia Diseases 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
- 201000009277 hairy cell leukemia Diseases 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
- 230000003463 hyperproliferative effect 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
- 201000009020 malignant peripheral nerve sheath tumor Diseases 0.000 claims description 2
- 230000009401 metastasis Effects 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
- 230000002062 proliferating effect Effects 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
- 201000000596 systemic lupus erythematosus Diseases 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
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 5
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims 1
- 235000018417 cysteine Nutrition 0.000 claims 1
- 238000000034 method Methods 0.000 description 64
- 239000012472 biological sample Substances 0.000 description 8
- 0 C=CC(Nc1cccc(Nc(nc2)nc(Nc3cccc(OCCN4CCOCC4)c3)c2F)c1)=* Chemical compound C=CC(Nc1cccc(Nc(nc2)nc(Nc3cccc(OCCN4CCOCC4)c3)c2F)c1)=* 0.000 description 6
- 125000002950 monocyclic group Chemical group 0.000 description 4
- 239000013610 patient sample Substances 0.000 description 4
- LGJZMPRRWYSPEO-SFQUDFHCSA-N C/C(/CNC)=C\C(Cc(cc1)ccc1Nc(nc(Nc(cc1F)ccc1OCCOC)nc1)c1F)O Chemical compound C/C(/CNC)=C\C(Cc(cc1)ccc1Nc(nc(Nc(cc1F)ccc1OCCOC)nc1)c1F)O LGJZMPRRWYSPEO-SFQUDFHCSA-N 0.000 description 1
- GGEOYJGWHQNNHP-UHFFFAOYSA-N C=CC(Nc1cc(Nc(nc(Nc(cc2)ccc2Oc2cccnc2)nc2)c2F)ccc1)=O Chemical compound C=CC(Nc1cc(Nc(nc(Nc(cc2)ccc2Oc2cccnc2)nc2)c2F)ccc1)=O GGEOYJGWHQNNHP-UHFFFAOYSA-N 0.000 description 1
- JLNPVKWXVQQYCF-UHFFFAOYSA-N CN(CC1)CCN1C(CC1)CCN1c(cc1)cc(OC)c1Nc(nc1)nc(Nc2cc(NC(C=C)O)ccc2)c1Cl Chemical compound CN(CC1)CCN1C(CC1)CCN1c(cc1)cc(OC)c1Nc(nc1)nc(Nc2cc(NC(C=C)O)ccc2)c1Cl JLNPVKWXVQQYCF-UHFFFAOYSA-N 0.000 description 1
- HNQFCJXQIKQHIS-UHFFFAOYSA-N CN(CC1)CCN1C(CC1)CCN1c(cc1OC)ccc1Nc(nc1)nc(Nc2cc(CC(CC3CCC3)=O)ccc2)c1Cl Chemical compound CN(CC1)CCN1C(CC1)CCN1c(cc1OC)ccc1Nc(nc1)nc(Nc2cc(CC(CC3CCC3)=O)ccc2)c1Cl HNQFCJXQIKQHIS-UHFFFAOYSA-N 0.000 description 1
- WEBHZZXCRDNUKD-UHFFFAOYSA-N CN(CC1)CCN1C(CC1)CCN1c(cc1OC)ccc1Nc(nc1)nc(Nc2cc(NC(C=C)=O)ccc2)c1F Chemical compound CN(CC1)CCN1C(CC1)CCN1c(cc1OC)ccc1Nc(nc1)nc(Nc2cc(NC(C=C)=O)ccc2)c1F WEBHZZXCRDNUKD-UHFFFAOYSA-N 0.000 description 1
- DZLZWTGJBRJWRJ-UHFFFAOYSA-N CN(CC1)CCN1C(CC1)CCN1c(cc1OC)ccc1Nc(nc1)nc(Nc2ccc(CC(C=C3CCC3)=N)cc2)c1Cl Chemical compound CN(CC1)CCN1C(CC1)CCN1c(cc1OC)ccc1Nc(nc1)nc(Nc2ccc(CC(C=C3CCC3)=N)cc2)c1Cl DZLZWTGJBRJWRJ-UHFFFAOYSA-N 0.000 description 1
- SRPAPHNCPQGRQQ-ZZXKWVIFSA-N COCCOc(cc1)ccc1Nc(nc1)nc(Nc2cc(CC(/C=C/Cc3ncc[nH]3)=O)ccc2)c1F Chemical compound COCCOc(cc1)ccc1Nc(nc1)nc(Nc2cc(CC(/C=C/Cc3ncc[nH]3)=O)ccc2)c1F SRPAPHNCPQGRQQ-ZZXKWVIFSA-N 0.000 description 1
- 206010066476 Haematological malignancy Diseases 0.000 description 1
- 125000003342 alkenyl group Chemical group 0.000 description 1
- 125000000304 alkynyl group Chemical group 0.000 description 1
- 238000010835 comparative analysis Methods 0.000 description 1
- 230000031146 intracellular signal transduction Effects 0.000 description 1
- 229940043355 kinase inhibitor Drugs 0.000 description 1
- 230000036210 malignancy Effects 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US12/648,693 US8338439B2 (en) | 2008-06-27 | 2009-12-29 | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| US12/648,693 | 2009-12-29 | ||
| PCT/US2010/062432 WO2011090760A1 (en) | 2009-12-29 | 2010-12-29 | Heteroaryl compounds and uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016017045A Division JP2016117749A (ja) | 2009-12-29 | 2016-02-01 | ヘテロアリール化合物およびそれらの使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013515786A JP2013515786A (ja) | 2013-05-09 |
| JP2013515786A5 true JP2013515786A5 (cg-RX-API-DMAC7.html) | 2014-02-20 |
| JP5879270B2 JP5879270B2 (ja) | 2016-03-08 |
Family
ID=44307129
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012547280A Expired - Fee Related JP5879270B2 (ja) | 2009-12-29 | 2010-12-29 | ヘテロアリール化合物およびそれらの使用 |
| JP2016017045A Ceased JP2016117749A (ja) | 2009-12-29 | 2016-02-01 | ヘテロアリール化合物およびそれらの使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016017045A Ceased JP2016117749A (ja) | 2009-12-29 | 2016-02-01 | ヘテロアリール化合物およびそれらの使用 |
Country Status (16)
| Country | Link |
|---|---|
| US (5) | US8338439B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP2519235B1 (cg-RX-API-DMAC7.html) |
| JP (2) | JP5879270B2 (cg-RX-API-DMAC7.html) |
| KR (2) | KR101747159B1 (cg-RX-API-DMAC7.html) |
| CN (2) | CN106146407A (cg-RX-API-DMAC7.html) |
| AU (2) | AU2010343055B2 (cg-RX-API-DMAC7.html) |
| BR (1) | BR112012018345B1 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2783624C (cg-RX-API-DMAC7.html) |
| IL (2) | IL220155B (cg-RX-API-DMAC7.html) |
| MX (2) | MX341825B (cg-RX-API-DMAC7.html) |
| NZ (2) | NZ700236A (cg-RX-API-DMAC7.html) |
| PH (1) | PH12012501346A1 (cg-RX-API-DMAC7.html) |
| RU (1) | RU2636584C2 (cg-RX-API-DMAC7.html) |
| SG (1) | SG181962A1 (cg-RX-API-DMAC7.html) |
| TW (1) | TWI592405B (cg-RX-API-DMAC7.html) |
| WO (1) | WO2011090760A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (318)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| PT2300013T (pt) | 2008-05-21 | 2017-10-31 | Ariad Pharma Inc | Derivados de fósforo como inibidores de cinases |
| US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
| CA3031835C (en) * | 2008-06-27 | 2021-09-07 | 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 |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| KR101705158B1 (ko) | 2009-05-05 | 2017-02-09 | 다나-파버 캔서 인스티튜트 인크. | Ｅｇｆｒ 억제제 및 질환 치료방법 |
| WO2010129802A1 (en) * | 2009-05-06 | 2010-11-11 | Portola Pharmaceuticals, Inc. | Inhibitors of jak |
| US8586751B2 (en) | 2009-06-12 | 2013-11-19 | Bristol-Myers Squibb Company | Nicotinamide compounds useful as kinase modulators |
| 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 |
| US8466155B2 (en) * | 2009-10-02 | 2013-06-18 | Boehringer Ingelheim International Gmbh | Pyrimidines |
| CA2785738A1 (en) | 2009-12-30 | 2011-07-07 | Avila Therapeutics, Inc. | Ligand-directed covalent modification of protein |
| EP2571361A4 (en) | 2010-05-19 | 2013-11-13 | Univ North Carolina | PYRAZOLOPYRIMIDINE COMPOUNDS FOR CANCER TREATMENT |
| MX2012013274A (es) | 2010-05-21 | 2013-05-28 | Chemilia Ab | Novedosos derivados de la pirimidina. |
| US8354420B2 (en) | 2010-06-04 | 2013-01-15 | Genentech, Inc. | Aminopyrimidine derivatives as LRRK2 inhibitors |
| PH12013500246A1 (en) | 2010-08-10 | 2019-10-11 | Celgene Avilomics Res Inc | Besylate salt of a btk inhibitor |
| NZ710636A (en) | 2010-11-01 | 2017-02-24 | Celgene Avilomics Res Inc | Heterocyclic compounds and uses thereof |
| US9238629B2 (en) | 2010-11-01 | 2016-01-19 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| JP5957003B2 (ja) | 2010-11-10 | 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 | 変異体選択的ｅｇｆｒ阻害剤およびその使用 |
| KR101566091B1 (ko) | 2010-11-10 | 2015-11-04 | 에프. 호프만-라 로슈 아게 | Lrrk2 조절제로서 피라졸 아미노피리미딘 유도체 |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| 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 |
| US8703767B2 (en) | 2011-04-01 | 2014-04-22 | University Of Utah Research Foundation | Substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase BTK inhibitors |
| EP2693881B1 (en) | 2011-04-01 | 2019-09-04 | University of Utah Research Foundation | Substituted n-phenylpyrimidin-2-amine analogs as inhibitors of the axl kinase |
| HUE064883T2 (hu) | 2011-04-22 | 2024-04-28 | Signal Pharm Llc | Szubsztituált diaminokarboxamid- és diaminokarbonitril-pirimidinek, azok készítményei és azokkal történõ kezelési eljárások |
| EP2701510B1 (en) | 2011-04-25 | 2017-02-15 | Usher III Initiative | Pyrazolopyridazines and methods for treating retinal-degenerative diseases and hearing loss associated with usher syndrome |
| EA201391626A1 (ru) | 2011-05-04 | 2014-03-31 | Ариад Фармасьютикалз, Инк. | Соединения для ингибирования клеточной пролиферации в egfr-стимулированных типах рака |
| CN105198862B (zh) | 2011-07-27 | 2018-01-23 | 阿斯利康(瑞典)有限公司 | 取代的n‑(4‑氟‑2‑甲氧基‑5‑硝基苯基)嘧啶‑2‑胺化合物及其盐 |
| WO2013052417A1 (en) | 2011-10-03 | 2013-04-11 | The University Of North Carolina At Chapel Hill | Pyrrolopyrimidine compounds for the treatment of cancer |
| AR088570A1 (es) | 2011-10-28 | 2014-06-18 | Celgene Avilomics Res Inc | Metodos para tratar una enfermedad o trastorno relacionado con la tirosina quinasa de bruton |
| WO2013106792A1 (en) | 2012-01-13 | 2013-07-18 | Acea Biosciences Inc. | Heterocyclic compounds and uses as anticancer agents. |
| US9464089B2 (en) * | 2012-01-13 | 2016-10-11 | Acea Biosciences Inc. | Heterocyclic compounds 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 |
| US9034885B2 (en) | 2012-01-13 | 2015-05-19 | Acea Biosciences Inc. | EGFR modulators and uses thereof |
| AR089727A1 (es) | 2012-01-17 | 2014-09-10 | Astellas Pharma Inc | Compuesto de pirazin-carboxamida |
| 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 |
| ES2698298T3 (es) | 2012-03-15 | 2019-02-04 | Celgene Car Llc | Sales de un inhibidor de quinasa receptor de factor de crecimiento epidérmico |
| AU2013204563B2 (en) * | 2012-05-05 | 2016-05-19 | Takeda Pharmaceutical Company Limited | Compounds for inhibiting cell proliferation in EGFR-driven cancers |
| US9133134B2 (en) | 2012-05-16 | 2015-09-15 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase |
| EP2852579A4 (en) * | 2012-05-22 | 2015-12-30 | Univ North Carolina | PYRIMIDINE COMPOUNDS FOR CANCER TREATMENT |
| BR112014030812B1 (pt) | 2012-06-13 | 2022-11-08 | Incyte Holdings Corporation | Compostos tricíclicos substituídos como inibidores de fgfr, seus usos, composição farmacêutica e método para inibir uma enzima fgfr |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
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| EA201391626A1 (ru) | 2011-05-04 | 2014-03-31 | Ариад Фармасьютикалз, Инк. | Соединения для ингибирования клеточной пролиферации в egfr-стимулированных типах рака |
| MX355728B (es) | 2011-05-17 | 2018-04-27 | Univ California | Inhibidores de cinasas. |
| WO2013059738A2 (en) | 2011-10-19 | 2013-04-25 | Pharmacyclics, Inc. | Use of inhibitors of bruton's tyrosine kinase (btk) |
| CN103159742B (zh) | 2011-12-16 | 2015-08-12 | 北京韩美药品有限公司 | 5-氯嘧啶类化合物及其作为egfr酪氨酸激酶抑制剂的应用 |
| 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 |
| MX2015005633A (es) | 2012-11-02 | 2016-02-03 | Pharmacyclics Inc | Terapia adyuvante con inhibidores de quinasa de la familia tec. |
| US9421208B2 (en) | 2013-08-02 | 2016-08-23 | Pharmacyclics Llc | Methods for the treatment of solid tumors |
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