JP2013505245A5 - - Google Patents
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- JP2013505245A5 JP2013505245A5 JP2012529871A JP2012529871A JP2013505245A5 JP 2013505245 A5 JP2013505245 A5 JP 2013505245A5 JP 2012529871 A JP2012529871 A JP 2012529871A JP 2012529871 A JP2012529871 A JP 2012529871A JP 2013505245 A5 JP2013505245 A5 JP 2013505245A5
- Authority
- JP
- Japan
- Prior art keywords
- independently
- halogen
- hydrogen
- saturated
- oxo
- 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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- 229910052736 halogen Inorganic materials 0.000 claims 141
- 150000002367 halogens Chemical class 0.000 claims 140
- 229910052739 hydrogen Inorganic materials 0.000 claims 140
- 239000001257 hydrogen Substances 0.000 claims 140
- 150000002431 hydrogen Chemical group 0.000 claims 109
- 229920006395 saturated elastomer Polymers 0.000 claims 99
- 125000001931 aliphatic group Chemical group 0.000 claims 88
- 229910052757 nitrogen Inorganic materials 0.000 claims 72
- 125000003118 aryl group Chemical group 0.000 claims 65
- 125000000217 alkyl group Chemical group 0.000 claims 62
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 60
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims 57
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 53
- 229910052717 sulfur Inorganic materials 0.000 claims 52
- 229910052760 oxygen Inorganic materials 0.000 claims 51
- 125000005842 heteroatom Chemical group 0.000 claims 48
- 125000001188 haloalkyl group Chemical group 0.000 claims 46
- 125000000753 cycloalkyl group Chemical group 0.000 claims 45
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 44
- 239000011593 sulfur Substances 0.000 claims 44
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 43
- 125000002619 bicyclic group Chemical group 0.000 claims 43
- 239000001301 oxygen Substances 0.000 claims 43
- 125000002950 monocyclic group Chemical group 0.000 claims 41
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 33
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 29
- 125000004980 cyclopropylene group Chemical group 0.000 claims 25
- 150000002825 nitriles Chemical group 0.000 claims 23
- 125000004043 oxo group Chemical group O=* 0.000 claims 22
- 150000003839 salts Chemical class 0.000 claims 22
- 108091000080 Phosphotransferase Proteins 0.000 claims 20
- 102000020233 phosphotransferase Human genes 0.000 claims 20
- 150000001875 compounds Chemical class 0.000 claims 12
- 125000003275 alpha amino acid group Chemical group 0.000 claims 8
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 7
- 101100115718 Arabidopsis thaliana CYS5 gene Proteins 0.000 claims 6
- 108010064266 CYS7 Proteins 0.000 claims 6
- 102000001253 Protein Kinase Human genes 0.000 claims 6
- 101100498074 Schizosaccharomyces pombe (strain 972 / ATCC 24843) cys11 gene Proteins 0.000 claims 6
- 230000033115 angiogenesis Effects 0.000 claims 6
- 125000004122 cyclic group Chemical group 0.000 claims 6
- 108060006633 protein kinase Proteins 0.000 claims 6
- 101150012469 CYS2 gene Proteins 0.000 claims 5
- 102100025802 Cystin-1 Human genes 0.000 claims 5
- 101000855767 Homo sapiens Cystin-1 Proteins 0.000 claims 5
- 101100222745 Schizosaccharomyces pombe (strain 972 / ATCC 24843) met17 gene Proteins 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 125000003107 substituted aryl group Chemical group 0.000 claims 5
- 101100115720 Arabidopsis thaliana CYS6 gene Proteins 0.000 claims 4
- -1 CYS8 Proteins 0.000 claims 4
- 101100330293 Schizosaccharomyces pombe (strain 972 / ATCC 24843) cys12 gene Proteins 0.000 claims 4
- 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 102100037813 Focal adhesion kinase 1 Human genes 0.000 claims 3
- 101000878536 Homo sapiens Focal adhesion kinase 1 Proteins 0.000 claims 3
- 101000932478 Homo sapiens Receptor-type tyrosine-protein kinase FLT3 Proteins 0.000 claims 3
- 101000934996 Homo sapiens Tyrosine-protein kinase JAK3 Proteins 0.000 claims 3
- 101100426732 Neurospora crassa (strain ATCC 24698 / 74-OR23-1A / CBS 708.71 / DSM 1257 / FGSC 987) cys-9 gene Proteins 0.000 claims 3
- 102100020718 Receptor-type tyrosine-protein kinase FLT3 Human genes 0.000 claims 3
- 102100025387 Tyrosine-protein kinase JAK3 Human genes 0.000 claims 3
- 108010053099 Vascular Endothelial Growth Factor Receptor-2 Proteins 0.000 claims 3
- 102100033177 Vascular endothelial growth factor receptor 2 Human genes 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 101150067142 CYS3 gene Proteins 0.000 claims 2
- 101150006642 CYS4 gene Proteins 0.000 claims 2
- ZEOWTGPWHLSLOG-UHFFFAOYSA-N Cc1ccc(cc1-c1ccc2c(n[nH]c2c1)-c1cnn(c1)C1CC1)C(=O)Nc1cccc(c1)C(F)(F)F Chemical compound Cc1ccc(cc1-c1ccc2c(n[nH]c2c1)-c1cnn(c1)C1CC1)C(=O)Nc1cccc(c1)C(F)(F)F ZEOWTGPWHLSLOG-UHFFFAOYSA-N 0.000 claims 2
- 102100023593 Fibroblast growth factor receptor 1 Human genes 0.000 claims 2
- 101710182386 Fibroblast growth factor receptor 1 Proteins 0.000 claims 2
- 102100023600 Fibroblast growth factor receptor 2 Human genes 0.000 claims 2
- 101710182389 Fibroblast growth factor receptor 2 Proteins 0.000 claims 2
- 102100027842 Fibroblast growth factor receptor 3 Human genes 0.000 claims 2
- 101710182396 Fibroblast growth factor receptor 3 Proteins 0.000 claims 2
- 102100027844 Fibroblast growth factor receptor 4 Human genes 0.000 claims 2
- 101000917134 Homo sapiens Fibroblast growth factor receptor 4 Proteins 0.000 claims 2
- 101001106413 Homo sapiens Macrophage-stimulating protein receptor Proteins 0.000 claims 2
- 101000950695 Homo sapiens Mitogen-activated protein kinase 8 Proteins 0.000 claims 2
- 101000912503 Homo sapiens Tyrosine-protein kinase Fgr Proteins 0.000 claims 2
- 101000818543 Homo sapiens Tyrosine-protein kinase ZAP-70 Proteins 0.000 claims 2
- 102100037808 Mitogen-activated protein kinase 8 Human genes 0.000 claims 2
- 102000007399 Nuclear hormone receptor Human genes 0.000 claims 2
- 108020005497 Nuclear hormone receptor Proteins 0.000 claims 2
- 102000018471 Proto-Oncogene Proteins B-raf Human genes 0.000 claims 2
- 108010091528 Proto-Oncogene Proteins B-raf Proteins 0.000 claims 2
- 102000001332 SRC Human genes 0.000 claims 2
- 108060006706 SRC Proteins 0.000 claims 2
- 102100026150 Tyrosine-protein kinase Fgr Human genes 0.000 claims 2
- 102100021125 Tyrosine-protein kinase ZAP-70 Human genes 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 2
- 125000004438 haloalkoxy group Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 239000013038 irreversible inhibitor Substances 0.000 claims 2
- 229940037201 oris Drugs 0.000 claims 2
- 125000006727 (C1-C6) alkenyl group Chemical group 0.000 claims 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000006728 (C1-C6) alkynyl group Chemical group 0.000 claims 1
- FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical compound C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 claims 1
- 102100034111 Activin receptor type-1 Human genes 0.000 claims 1
- 102100025422 Bone morphogenetic protein receptor type-2 Human genes 0.000 claims 1
- 102100023060 Casein kinase I isoform gamma-2 Human genes 0.000 claims 1
- 102100025567 Citron Rho-interacting kinase Human genes 0.000 claims 1
- 101710087170 Citron rho-interacting kinase Proteins 0.000 claims 1
- 102100038113 Cyclin-dependent kinase 14 Human genes 0.000 claims 1
- 102100031679 Cyclin-dependent kinase-like 1 Human genes 0.000 claims 1
- 102100031683 Cyclin-dependent kinase-like 4 Human genes 0.000 claims 1
- 102100031480 Dual specificity mitogen-activated protein kinase kinase 1 Human genes 0.000 claims 1
- 101710146526 Dual specificity mitogen-activated protein kinase kinase 1 Proteins 0.000 claims 1
- 102000050554 Eph Family Receptors Human genes 0.000 claims 1
- 108091008815 Eph receptors Proteins 0.000 claims 1
- 108091008794 FGF receptors Proteins 0.000 claims 1
- 102100034051 Heat shock protein HSP 90-alpha Human genes 0.000 claims 1
- 101000799140 Homo sapiens Activin receptor type-1 Proteins 0.000 claims 1
- 101000934635 Homo sapiens Bone morphogenetic protein receptor type-2 Proteins 0.000 claims 1
- 101001049881 Homo sapiens Casein kinase I isoform gamma-2 Proteins 0.000 claims 1
- 101000884374 Homo sapiens Cyclin-dependent kinase 14 Proteins 0.000 claims 1
- 101000777728 Homo sapiens Cyclin-dependent kinase-like 1 Proteins 0.000 claims 1
- 101000777775 Homo sapiens Cyclin-dependent kinase-like 4 Proteins 0.000 claims 1
- 101001016865 Homo sapiens Heat shock protein HSP 90-alpha Proteins 0.000 claims 1
- 101001103039 Homo sapiens Inactive tyrosine-protein kinase transmembrane receptor ROR1 Proteins 0.000 claims 1
- 101001005128 Homo sapiens LIM domain kinase 1 Proteins 0.000 claims 1
- 101000916644 Homo sapiens Macrophage colony-stimulating factor 1 receptor Proteins 0.000 claims 1
- 101000628949 Homo sapiens Mitogen-activated protein kinase 10 Proteins 0.000 claims 1
- 101000950710 Homo sapiens Mitogen-activated protein kinase 6 Proteins 0.000 claims 1
- 101000950669 Homo sapiens Mitogen-activated protein kinase 9 Proteins 0.000 claims 1
- 101000663003 Homo sapiens Non-receptor tyrosine-protein kinase TNK1 Proteins 0.000 claims 1
- 101001103036 Homo sapiens Nuclear receptor ROR-alpha Proteins 0.000 claims 1
- 101000692455 Homo sapiens Platelet-derived growth factor receptor beta Proteins 0.000 claims 1
- 101000878540 Homo sapiens Protein-tyrosine kinase 2-beta Proteins 0.000 claims 1
- 101001026790 Homo sapiens Tyrosine-protein kinase Fes/Fps Proteins 0.000 claims 1
- 101000851018 Homo sapiens Vascular endothelial growth factor receptor 1 Proteins 0.000 claims 1
- 102100039615 Inactive tyrosine-protein kinase transmembrane receptor ROR1 Human genes 0.000 claims 1
- 102100026023 LIM domain kinase 1 Human genes 0.000 claims 1
- 229940124647 MEK inhibitor Drugs 0.000 claims 1
- 102100024299 Maternal embryonic leucine zipper kinase Human genes 0.000 claims 1
- 101710154611 Maternal embryonic leucine zipper kinase Proteins 0.000 claims 1
- 102000004232 Mitogen-Activated Protein Kinase Kinases Human genes 0.000 claims 1
- 108090000744 Mitogen-Activated Protein Kinase Kinases Proteins 0.000 claims 1
- 102100026931 Mitogen-activated protein kinase 10 Human genes 0.000 claims 1
- 102100037801 Mitogen-activated protein kinase 6 Human genes 0.000 claims 1
- 102100037809 Mitogen-activated protein kinase 9 Human genes 0.000 claims 1
- 101100490437 Mus musculus Acvrl1 gene Proteins 0.000 claims 1
- 102100037669 Non-receptor tyrosine-protein kinase TNK1 Human genes 0.000 claims 1
- 108091007960 PI3Ks Proteins 0.000 claims 1
- 102000038030 PI3Ks Human genes 0.000 claims 1
- 102100026547 Platelet-derived growth factor receptor beta Human genes 0.000 claims 1
- 102100037787 Protein-tyrosine kinase 2-beta Human genes 0.000 claims 1
- 102100031463 Serine/threonine-protein kinase PLK1 Human genes 0.000 claims 1
- 102100024537 Tyrosine-protein kinase Fer Human genes 0.000 claims 1
- 102100037333 Tyrosine-protein kinase Fes/Fps Human genes 0.000 claims 1
- 108091008605 VEGF receptors Proteins 0.000 claims 1
- 108010053100 Vascular Endothelial Growth Factor Receptor-3 Proteins 0.000 claims 1
- 102000009484 Vascular Endothelial Growth Factor Receptors Human genes 0.000 claims 1
- 102100033178 Vascular endothelial growth factor receptor 1 Human genes 0.000 claims 1
- 102100033179 Vascular endothelial growth factor receptor 3 Human genes 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000005605 benzo group Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000030533 eye disease Diseases 0.000 claims 1
- 102000052178 fibroblast growth factor receptor activity proteins Human genes 0.000 claims 1
- 229930182817 methionine Natural products 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000003607 modifier Substances 0.000 claims 1
- 108010056274 polo-like kinase 1 Proteins 0.000 claims 1
- 108010067366 proto-oncogene protein c-fes-fps Proteins 0.000 claims 1
- 230000003381 solubilizing effect Effects 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 125000002653 sulfanylmethyl group Chemical group [H]SC([H])([H])[*] 0.000 claims 1
- 125000004434 sulfur atom Chemical group 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
- 0 C[C@@]1(*)C(NC(N*=CC=C(C=*C)Oc2ccnc(*)c2)=O)=CC=C(*)C(*)=C1 Chemical compound C[C@@]1(*)C(NC(N*=CC=C(C=*C)Oc2ccnc(*)c2)=O)=CC=C(*)C(*)=C1 0.000 description 2
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24298809P | 2009-09-16 | 2009-09-16 | |
| US61/242,988 | 2009-09-16 | ||
| PCT/US2010/048916 WO2011034907A2 (en) | 2009-09-16 | 2010-09-15 | Protein kinase conjugates and inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015174949A Division JP6397389B2 (ja) | 2009-09-16 | 2015-09-04 | プロテインキナーゼコンジュゲート及びインヒビター |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013505245A JP2013505245A (ja) | 2013-02-14 |
| JP2013505245A5 true JP2013505245A5 (enExample) | 2013-11-07 |
| JP5806670B2 JP5806670B2 (ja) | 2015-11-10 |
Family
ID=43759252
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012529871A Active JP5806670B2 (ja) | 2009-09-16 | 2010-09-15 | プロテインキナーゼコンジュゲート及びインヒビター |
| JP2015174949A Ceased JP6397389B2 (ja) | 2009-09-16 | 2015-09-04 | プロテインキナーゼコンジュゲート及びインヒビター |
| JP2018163436A Expired - Fee Related JP6889689B2 (ja) | 2009-09-16 | 2018-08-31 | プロテインキナーゼコンジュゲート及びインヒビター |
| JP2021086337A Pending JP2021121219A (ja) | 2009-09-16 | 2021-05-21 | プロテインキナーゼコンジュゲート及びインヒビター |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015174949A Ceased JP6397389B2 (ja) | 2009-09-16 | 2015-09-04 | プロテインキナーゼコンジュゲート及びインヒビター |
| JP2018163436A Expired - Fee Related JP6889689B2 (ja) | 2009-09-16 | 2018-08-31 | プロテインキナーゼコンジュゲート及びインヒビター |
| JP2021086337A Pending JP2021121219A (ja) | 2009-09-16 | 2021-05-21 | プロテインキナーゼコンジュゲート及びインヒビター |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US9556426B2 (enExample) |
| EP (1) | EP2478361A4 (enExample) |
| JP (4) | JP5806670B2 (enExample) |
| KR (1) | KR20120093220A (enExample) |
| CN (2) | CN105063001A (enExample) |
| AU (2) | AU2010295690B2 (enExample) |
| BR (1) | BR112012005962A8 (enExample) |
| CA (1) | CA2773985A1 (enExample) |
| IL (1) | IL218678A0 (enExample) |
| IN (1) | IN2012DN02534A (enExample) |
| MX (1) | MX339811B (enExample) |
| NZ (2) | NZ598705A (enExample) |
| RU (1) | RU2012114902A (enExample) |
| SG (1) | SG179172A1 (enExample) |
| WO (1) | WO2011034907A2 (enExample) |
Families Citing this family (83)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT2201840E (pt) | 2006-09-22 | 2012-02-14 | Pharmacyclics Inc | Inibidores da tirosina quinase de bruton |
| US8809273B2 (en) | 2007-03-28 | 2014-08-19 | Pharmacyclics, Inc. | Inhibitors of Bruton's tyrosine kinase |
| PL2300013T5 (pl) | 2008-05-21 | 2025-04-28 | Takeda Pharmaceutical Company Limited | Pochodne fosforu jako inhibitor kinazy |
| US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
| AU2009270856B2 (en) | 2008-07-16 | 2013-07-25 | Pharmacyclics Llc | Inhibitors of Bruton's tyrosine kinase for the treatment of solid tumors |
| CN102405284B (zh) * | 2008-09-05 | 2016-01-20 | 新基阿维罗米克斯研究公司 | 设计不可逆抑制剂的算法 |
| EP2478361A4 (en) | 2009-09-16 | 2014-05-21 | Celgene Avilomics Res Inc | CONJUGATES AND INHIBITORS OF PROTEIN KINASE |
| WO2011060321A1 (en) | 2009-11-16 | 2011-05-19 | Chdi, Inc. | Transglutaminase tg2 inhibitors, pharmaceutical compositions, and methods of use thereof |
| CN102812167A (zh) | 2009-12-30 | 2012-12-05 | 阿维拉制药公司 | 蛋白的配体-介导的共价修饰 |
| EA201890869A3 (ru) | 2010-06-03 | 2019-03-29 | Фармасайкликс, Инк. | Применение ингибиторов тирозинкиназы брутона (btk) |
| HUE029196T2 (en) | 2010-06-04 | 2017-02-28 | Hoffmann La Roche | Aminoprimidine derivatives as LRRK2 modulators |
| BR112013011600B1 (pt) | 2010-11-10 | 2022-01-11 | Genentech, Inc | Derivados de pirazol aminopirimidina, seu uso e composição que os compreende |
| EP2704572B1 (en) | 2011-05-04 | 2015-12-30 | Ariad Pharmaceuticals, Inc. | Compounds for inhibiting cell proliferation in egfr-driven cancers |
| US8889716B2 (en) | 2011-05-10 | 2014-11-18 | Chdi Foundation, Inc. | Transglutaminase TG2 inhibitors, pharmaceutical compositions, and methods of use thereof |
| WO2013009810A1 (en) * | 2011-07-13 | 2013-01-17 | Tempero Pharmaceuticals, Inc. | Methods of treatment |
| WO2013009812A1 (en) * | 2011-07-13 | 2013-01-17 | Tempero Pharmaceuticals, Inc | Methods of treatment |
| WO2013009827A1 (en) * | 2011-07-13 | 2013-01-17 | Tempero Pharmaceuticals, Inc. | Methods of treatment |
| WO2013009830A1 (en) * | 2011-07-13 | 2013-01-17 | Tempero Pharmaceuticals, Inc. | Methods of treatment |
| ES2654177T3 (es) | 2011-07-27 | 2018-02-12 | Astrazeneca Ab | Derivados de 2-(2,4,5-anilino sustituido)pirimidina como moduladores de EGFR útiles para tratar el cáncer |
| EP2822935B1 (en) | 2011-11-17 | 2019-05-15 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-jun-n-terminal kinase (jnk) |
| AR089182A1 (es) * | 2011-11-29 | 2014-08-06 | Hoffmann La Roche | Derivados de aminopirimidina como moduladores de lrrk2 |
| LT2840080T (lt) * | 2012-04-17 | 2018-02-12 | Fujifilm Corporation | Heterociklinis junginys, turintis azotą, arba jo druska |
| 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 |
| CA3218491A1 (en) | 2012-06-04 | 2013-12-12 | Pharmacyclics Llc | Crystalline forms of a bruton's tyrosine kinase inhibitor |
| RU2019102203A (ru) * | 2012-07-11 | 2019-03-05 | Блюпринт Медсинс Корпорейшн | Ингибиторы рецептора фактора роста фибробластов |
| WO2014018567A1 (en) | 2012-07-24 | 2014-01-30 | Pharmacyclics, Inc. | Mutations associated with resistance to inhibitors of bruton's tyrosine kinase (btk) |
| JP2015537033A (ja) | 2012-11-15 | 2015-12-24 | ファーマサイクリックス，インク． | キナーゼ阻害剤としてのピロロピリミジン化合物 |
| US10202356B2 (en) | 2013-03-14 | 2019-02-12 | Tolero Pharmaceuticals, Inc. | JAK2 and ALK2 inhibitors and methods for their use |
| TWI647220B (zh) | 2013-03-15 | 2019-01-11 | 美商西建卡爾有限責任公司 | 雜芳基化合物及其用途 |
| KR102350704B1 (ko) | 2013-03-15 | 2022-01-13 | 셀젠 카르 엘엘씨 | 헤테로아릴 화합물 및 이의 용도 |
| CN111793068A (zh) | 2013-03-15 | 2020-10-20 | 西建卡尔有限责任公司 | 杂芳基化合物和其用途 |
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| AR097204A1 (es) | 2013-08-02 | 2016-02-24 | Pharmacyclics Inc | Métodos de tratamiento de tumores sólidos |
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| US10526660B2 (en) | 2013-09-12 | 2020-01-07 | Dana-Farber Cancer Institute, Inc. | Methods for evaluating and treating Waldenstrom's macroglobulinemia |
| PT3395814T (pt) | 2013-10-25 | 2022-07-27 | Blueprint Medicines Corp | Inibidores do recetor do fator de crescimento de fibroblastos |
| WO2015108992A1 (en) | 2014-01-15 | 2015-07-23 | Blueprint Medicines Corporation | Heterobicyclic compounds and their use as fgfr4 receptor inhibitors |
| CA2942528A1 (en) | 2014-03-20 | 2015-09-24 | Pharmacyclics Inc. | Phospholipase c gamma 2 and resistance associated mutations |
| CA2944669A1 (en) | 2014-04-04 | 2015-10-08 | Syros Pharmaceuticals, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
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| MX2017001671A (es) | 2014-08-07 | 2017-07-04 | Pharmacyclics Llc | Formulaciones novedosas de un inhibidor de la tirosina cinasa de bruton. |
| IL315294A (en) | 2015-03-03 | 2024-10-01 | Pharmacyclics Llc | Pharmaceutical formulations of bruton's tyrosine kinase inhibitor |
| KR20240070721A (ko) | 2015-06-03 | 2024-05-21 | 프린시피아 바이오파마, 인코퍼레이티드 | 티로신 키나제 억제제 |
| EP3386968B1 (en) | 2015-12-09 | 2025-04-02 | The Board of Trustees of the University of Illinois | Benzothiophene-based selective estrogen receptor downregulator compounds |
| WO2017197055A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| CN109790143A (zh) | 2016-05-10 | 2019-05-21 | C4医药公司 | 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体 |
| EP3454862B1 (en) | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
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- 2010-09-15 SG SG2012018545A patent/SG179172A1/en unknown
- 2010-09-15 AU AU2010295690A patent/AU2010295690B2/en not_active Ceased
- 2010-09-15 IN IN2534DEN2012 patent/IN2012DN02534A/en unknown
- 2010-09-15 RU RU2012114902/04A patent/RU2012114902A/ru not_active Application Discontinuation
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2015
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2016
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2018
- 2018-08-31 JP JP2018163436A patent/JP6889689B2/ja not_active Expired - Fee Related
-
2021
- 2021-05-21 JP JP2021086337A patent/JP2021121219A/ja active Pending
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