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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- Prior art keywords
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- Prior art date
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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 (enExample) | 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 (enExample) |
| EP (1) | EP2519235B1 (enExample) |
| JP (2) | JP5879270B2 (enExample) |
| KR (2) | KR20170086547A (enExample) |
| CN (2) | CN102740847B (enExample) |
| AU (2) | AU2010343055B2 (enExample) |
| BR (1) | BR112012018345B1 (enExample) |
| CA (1) | CA2783624C (enExample) |
| IL (2) | IL220155B (enExample) |
| MX (2) | MX2012007507A (enExample) |
| NZ (2) | NZ600631A (enExample) |
| PH (1) | PH12012501346A1 (enExample) |
| RU (1) | RU2636584C2 (enExample) |
| SG (1) | SG181962A1 (enExample) |
| TW (1) | TWI592405B (enExample) |
| WO (1) | WO2011090760A1 (enExample) |
Families Citing this family (318)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US7989465B2 (en) * | 2007-10-19 | 2011-08-02 | Avila Therapeutics, Inc. | 4,6-disubstituted pyrimidines useful as kinase inhibitors |
| US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
| PT2300013T (pt) | 2008-05-21 | 2017-10-31 | Ariad Pharma Inc | Derivados de fósforo como inibidores de cinases |
| EP2361248B1 (en) | 2008-06-27 | 2018-09-19 | Celgene CAR LLC | Heteroaryl compounds 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 |
| 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 |
| AR076550A1 (es) * | 2009-05-06 | 2011-06-22 | Portola Pharm Inc | Inhibidores de la janus tirosina kinasa (jak) |
| 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 |
| US9556426B2 (en) | 2009-09-16 | 2017-01-31 | Celgene Avilomics Research, Inc. | Protein kinase conjugates and inhibitors |
| US8466155B2 (en) * | 2009-10-02 | 2013-06-18 | Boehringer Ingelheim International Gmbh | Pyrimidines |
| 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 |
| WO2011146313A1 (en) | 2010-05-19 | 2011-11-24 | The University Of North Carolina At Chapel Hill | Pyrazolopyrimidine compounds for the treatment of cancer |
| WO2011144742A1 (en) | 2010-05-21 | 2011-11-24 | Chemilia Ab | Novel pyrimidine derivatives |
| MX2012014158A (es) | 2010-06-04 | 2013-02-07 | Hoffmann La Roche | Derivados de aminopirimidina como moduladores de proteina cinasa rica repeticiones leucina 2 (lrrk2). |
| NZ607845A (en) | 2010-08-10 | 2015-03-27 | Celgene Avilomics Res Inc | Besylate salt of a btk inhibitor |
| WO2012061299A1 (en) | 2010-11-01 | 2012-05-10 | Avila Therapeutics, Inc. | Heterocyclic compounds and uses thereof |
| EP2635285B1 (en) | 2010-11-01 | 2017-05-03 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| US8796255B2 (en) | 2010-11-10 | 2014-08-05 | Celgene Avilomics Research, Inc | Mutant-selective EGFR inhibitors and uses thereof |
| ES2653967T3 (es) | 2010-11-10 | 2018-02-09 | Genentech, Inc. | Derivados de pirazol aminopirimidina como moduladores de LRRK2 |
| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
| EP2688883B1 (en) | 2011-03-24 | 2016-05-18 | Noviga Research AB | Pyrimidine derivatives |
| PT2693881T (pt) | 2011-04-01 | 2019-12-09 | Univ Utah Res Found | Análogos de n-fenilpirimidin-2-amina substituídos como inibidores da axl cinase |
| CN103889962B (zh) * | 2011-04-01 | 2017-05-03 | 犹他大学研究基金会 | 作为受体酪氨酸激酶btk抑制剂的取代的n‑(3‑(嘧啶‑4‑基)苯基)丙烯酰胺类似物 |
| PE20140502A1 (es) | 2011-04-22 | 2014-05-02 | Signal Pharm Llc | Pirimidinas sustituidas de diaminocarboxamida y diaminocarbonitrilo, composiciones de las mismas y metodos de tratamiento con las mismas |
| CA2834049C (en) | 2011-04-25 | 2018-05-22 | Usher Iii Initiative, Inc. | Pyrazolopyridazines and methods for treating retinal-degenerative diseases and hearing loss associated with usher syndrome |
| EP2704572B1 (en) | 2011-05-04 | 2015-12-30 | Ariad Pharmaceuticals, Inc. | Compounds for inhibiting cell proliferation in egfr-driven cancers |
| PT3009431T (pt) | 2011-07-27 | 2017-12-26 | Astrazeneca Ab | Compostos de 2-(2,4,5-anilino-substituídos)pirimidina como moduladores úteis do egfr para o tratamento do cancro |
| BR112014007788A2 (pt) | 2011-10-03 | 2017-04-18 | Univ North Carolina Chapel Hill | compostos de pirrolopirimidina para tratamento do câncer |
| EP2770830A4 (en) * | 2011-10-28 | 2015-05-27 | Celgene Avilomics Res Inc | METHODS OF TREATING A DISEASE OR DISEASE ASSOCIATED WITH TYROSINE KINASE BTK (BRUTON'S TYROSINE KINASE) |
| WO2013106792A1 (en) | 2012-01-13 | 2013-07-18 | Acea Biosciences Inc. | Heterocyclic compounds and uses as anticancer agents. |
| 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 |
| US9464089B2 (en) | 2012-01-13 | 2016-10-11 | Acea Biosciences Inc. | Heterocyclic compounds and uses thereof |
| HRP20170226T1 (hr) | 2012-01-17 | 2017-04-07 | Astellas Pharma Inc. | Spoj pirazinkarboksamida |
| PT2825042T (pt) | 2012-03-15 | 2018-11-16 | Celgene Car Llc | Sais de um inibidor de cinases do recetor do fator de crescimento epidérmico |
| MX356753B (es) | 2012-03-15 | 2018-06-12 | Celgene Avilomics Res Inc | Formas solidas de un inhibidor de cinasa del receptor del factor de crecimiento epidermico. |
| 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 |
| MX2014013632A (es) | 2012-05-22 | 2015-02-05 | Univ North Carolina | Compuestos de pirimidina para el tratamiento de cancer. |
| PE20190736A1 (es) | 2012-06-13 | 2019-05-23 | Incyte Holdings Corp | Compuestos triciclicos sustituidos como inhibidores del receptor del factor de crecimiento de fibroblastos (fgfr) |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| EP2892538A4 (en) * | 2012-09-04 | 2016-04-20 | Celgene Avilomics Res Inc | METHOD FOR TREATING BRUTON TYROSINE KINASE ILLNESS OR DISORDER |
| EP2903972B1 (en) * | 2012-10-04 | 2019-12-04 | University of Utah Research Foundation | Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors |
| JP6313772B2 (ja) | 2012-10-04 | 2018-04-18 | ユニヴァーシティー オブ ユタ リサーチ ファウンデーション | チロシン受容体キナーゼｂｔｋ阻害剤である置換ｎ−（３−（ピリミジン−４−イル）フェニル）アクリルアミド類似体 |
| US9562047B2 (en) | 2012-10-17 | 2017-02-07 | The University Of North Carolina At Chapel Hill | Pyrazolopyrimidine compounds for the treatment of cancer |
| US8765762B2 (en) | 2012-10-25 | 2014-07-01 | Usher III, Initiative, Inc. | Pyrazolopyridazines and methods for treating retinal-degerative diseases and hearing loss associated with usher syndrome |
| US9227976B2 (en) | 2012-10-25 | 2016-01-05 | Usher Iii Initiative, Inc. | Pyrazolopyridazines and methods for treating retinal-degenerative diseases and hearing loss associated with usher syndrome |
| WO2014081709A2 (en) * | 2012-11-20 | 2014-05-30 | Celgene Avilomics Research, Inc. | Methods of treating a disease or disorder associated with bruton's tyrosine kinase |
| US20140142129A1 (en) * | 2012-11-20 | 2014-05-22 | Celgene Avilomics Research, Inc, | Methods of treating a disease or disorder associated with bruton's tyrosine kinase |
| WO2014081712A2 (en) * | 2012-11-20 | 2014-05-30 | Celgene Avilomics Research, Inc. | Methods of treating a disease or disorder associated with bruton's tyrosine kinase |
| US20140142128A1 (en) * | 2012-11-20 | 2014-05-22 | Celgene Avilomics Research, Inc. | Methods of treating a disease or disorder associated with bruton's tyrosine kinase |
| WO2014085225A1 (en) * | 2012-11-27 | 2014-06-05 | The University Of North Carolina At Chapel Hill | Pyrimidine compounds for the treatment of cancer |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| US9126950B2 (en) | 2012-12-21 | 2015-09-08 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| EP2948150A1 (en) | 2013-01-25 | 2015-12-02 | Rigel Pharmaceuticals, Inc. | Compounds and methods for treating inflammatory bowel diseases |
| WO2014124230A2 (en) | 2013-02-08 | 2014-08-14 | Celgene Avilomics Research, Inc. | Erk inhibitors and uses thereof |
| US20140357636A1 (en) * | 2013-02-21 | 2014-12-04 | Wayne Rothbaum | Treatment of Skeletal-Related Disorders |
| AR094929A1 (es) | 2013-02-28 | 2015-09-09 | Bristol Myers Squibb Co | Derivados de fenilpirazol como inhibidores potentes de rock1 y rock2 |
| CN105102448B (zh) | 2013-02-28 | 2018-03-06 | 百时美施贵宝公司 | 作为rock1和rock2抑制剂的苯基吡唑衍生物 |
| WO2014140582A1 (en) | 2013-03-14 | 2014-09-18 | Respivert Limited | Kinase inhibitors |
| DK2970205T3 (da) | 2013-03-14 | 2019-07-29 | Tolero Pharmaceuticals Inc | JAK2- og ALK2-inhibitorer og fremgangsmåder til anvendelse deraf |
| US9611283B1 (en) | 2013-04-10 | 2017-04-04 | Ariad Pharmaceuticals, Inc. | Methods for inhibiting cell proliferation in ALK-driven cancers |
| KR102269032B1 (ko) | 2013-04-19 | 2021-06-24 | 인사이트 홀딩스 코포레이션 | Fgfr 저해제로서 이환식 헤테로사이클 |
| SMT201700160T1 (it) | 2013-04-25 | 2017-05-08 | Beigene Ltd | Composti eterociclici fusi come inibitori di protein chinasi |
| HK1222644A1 (zh) * | 2013-05-06 | 2017-07-07 | Clovis Oncology, Inc. | 一种可作为表皮生长因子受体激酶抑制剂的盐式 |
| GB201309085D0 (en) | 2013-05-20 | 2013-07-03 | Redx Pharma Ltd | Compounds |
| NZ754039A (en) | 2013-06-26 | 2021-06-25 | Abbvie Inc | Primary carboxamides as btk inhibitors |
| AU2014287016B2 (en) * | 2013-07-11 | 2018-11-01 | Acea Biosciences Inc. | Pyrimidine derivatives as kinase inhibitors |
| CN105377835B (zh) * | 2013-07-11 | 2018-08-17 | 贝达药业股份有限公司 | 酪氨酸蛋白激酶调节剂及其应用方法 |
| CN105452257B (zh) | 2013-08-12 | 2017-09-05 | 大鹏药品工业株式会社 | 新型稠合嘧啶化合物或其盐 |
| 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 |
| ES2792183T3 (es) | 2013-09-13 | 2020-11-10 | Beigene Switzerland Gmbh | Anticuerpos anti-PD1 y su uso como productos terapéuticos y de diagnóstico |
| WO2015039613A1 (zh) * | 2013-09-18 | 2015-03-26 | 北京韩美药品有限公司 | 抑制btk和/或jak3激酶活性的化合物 |
| TR201911140T4 (tr) | 2013-10-21 | 2019-08-21 | Merck Patent Gmbh | Btk inhibitörleri olarak heteroaril bileşikleri ve bunların kullanımları. |
| US9795604B2 (en) | 2013-10-25 | 2017-10-24 | Pharmacyclics Llc | Methods of treating and preventing graft versus host disease |
| US9415049B2 (en) | 2013-12-20 | 2016-08-16 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| NZ715903A (en) | 2014-01-30 | 2017-06-30 | Signal Pharm Llc | Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use |
| US9622483B2 (en) | 2014-02-19 | 2017-04-18 | Corning Incorporated | Antimicrobial glass compositions, glasses and polymeric articles incorporating the same |
| US11039621B2 (en) | 2014-02-19 | 2021-06-22 | Corning Incorporated | Antimicrobial glass compositions, glasses and polymeric articles incorporating the same |
| US11039620B2 (en) | 2014-02-19 | 2021-06-22 | Corning Incorporated | Antimicrobial glass compositions, glasses and polymeric articles incorporating the same |
| CN104860941B (zh) * | 2014-02-25 | 2017-03-22 | 上海海雁医药科技有限公司 | 2,4‑二取代苯‑1,5‑二胺衍生物及其应用以及由其制备的药物组合物和药用组合物 |
| ES2921874T3 (es) | 2014-02-28 | 2022-09-01 | Nimbus Lakshmi Inc | Inhibidores de TYK2 y usos de los mismos |
| WO2015134805A1 (en) * | 2014-03-07 | 2015-09-11 | Celgene Avilomics Research, Inc. | Methods of treating a bruton's tyrosine kinase disease or disorder |
| US9603850B2 (en) | 2014-04-11 | 2017-03-28 | The University Of North Carolina At Chapel Hill | MerTK-specific pyrazolopyrimidine compounds |
| CN104974140B (zh) * | 2014-04-14 | 2017-11-24 | 上海海雁医药科技有限公司 | 2,3,4,6‑四取代苯‑1,5‑二胺衍生物、其制法与医药上的用途 |
| ES2881863T3 (es) * | 2014-04-16 | 2021-11-30 | Signal Pharm Llc | Métodos para tratar cáncer usando terapia de combinación de inhibidor de quinasa TOR con un inhibidor de histona desacetilasa |
| WO2015158310A1 (zh) * | 2014-04-18 | 2015-10-22 | 山东轩竹医药科技有限公司 | 一种酪氨酸激酶抑制剂及其用途 |
| CN104130265B (zh) * | 2014-04-29 | 2017-01-25 | 苏州景泓生物技术有限公司 | 一种含有螺环或桥环的嘧啶类化合物 |
| GB201410430D0 (en) | 2014-06-11 | 2014-07-23 | Redx Pharma Ltd | Compounds |
| CN106604742B (zh) | 2014-07-03 | 2019-01-11 | 百济神州有限公司 | 抗pd-l1抗体及其作为治疗剂及诊断剂的用途 |
| CN105315285B (zh) * | 2014-07-25 | 2017-12-08 | 上海海雁医药科技有限公司 | 2,4‑二取代7H‑吡咯并[2,3‑d]嘧啶衍生物、其制法与医药上的用途 |
| SG11201700777VA (en) | 2014-08-04 | 2017-02-27 | Nuevolution As | Optionally fused heterocyclyl-substituted derivatives of pyrimidine useful for the treatment of inflammatory, metabolic, oncologic and autoimmune diseases |
| AU2015303835B2 (en) | 2014-08-12 | 2020-04-09 | Monash University | Lymph directing prodrugs |
| ES2741785T3 (es) | 2014-08-13 | 2020-02-12 | Celgene Car Llc | Formas y composiciones de un inhibidor de ERK |
| JP6684780B2 (ja) * | 2014-08-25 | 2020-04-22 | ソーク インスティテュート フォー バイオロジカル スタディーズ | 新規ｕｌｋ１阻害剤およびそれを使用する方法 |
| CN105399686B (zh) * | 2014-09-16 | 2018-05-22 | 深圳微芯生物科技有限责任公司 | 嘧啶衍生物、其制备方法及其应用 |
| CN105399685B (zh) * | 2014-09-16 | 2018-05-22 | 深圳微芯生物科技有限责任公司 | 作为选择性jak3和/或jak1激酶抑制剂的芳杂环化合物的制备方法及其应用 |
| CN105481778B (zh) * | 2014-09-16 | 2019-06-04 | 深圳微芯生物科技股份有限公司 | 嘧啶衍生物、其制备方法及其应用 |
| SG10201902326XA (en) | 2014-09-17 | 2019-04-29 | Celgene Car Llc | Mk2 inhibitors and uses thereof |
| US10259820B2 (en) * | 2014-10-11 | 2019-04-16 | Shanghai Hansoh Biomedical Co., Ltd. | EGFR inhibitor, preparation method and use thereof |
| US10059689B2 (en) | 2014-10-14 | 2018-08-28 | Calitor Sciences, Llc | Substituted heteroaryl compounds and methods of use |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| US10532106B2 (en) | 2014-10-29 | 2020-01-14 | Bicyclerd Limited | Bicyclic peptide ligands specific for MT1-MMP |
| CN105601573B (zh) * | 2014-11-24 | 2021-07-02 | 中国科学院上海药物研究所 | 2-氨基嘧啶类化合物及其药物组合物和应用 |
| AU2015360547A1 (en) | 2014-12-11 | 2017-06-01 | Merck Patent Gmbh | Assays for BTK inhibitors |
| JP6903577B2 (ja) | 2014-12-16 | 2021-07-14 | シグナル ファーマシューティカルズ，エルエルシー | 皮膚におけるｃ−Ｊｕｎ Ｎ末端キナーゼの阻害の測定方法 |
| BR112017012795A2 (pt) | 2014-12-16 | 2018-01-02 | Signal Pharmaceuticals, Llc | Formulações de 2-(terc-butilamino)-4-((1r,3r,4r)-3- hidroxi-4-metilciclo-hexilamino)-pirimidina-5- carboxamida |
| CA2975260C (en) | 2015-01-29 | 2024-05-21 | Signal Pharmaceuticals Llc | Isotopologues of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide |
| JP6093486B2 (ja) | 2015-01-30 | 2017-03-08 | 大鵬薬品工業株式会社 | 縮合ピリミジン化合物の新規な塩及びその結晶 |
| AU2016213030B2 (en) * | 2015-01-30 | 2019-01-31 | Taiho Pharmaceutical Co., Ltd. | Preventive and/or therapeutic agent of immune disease |
| ES2895769T3 (es) | 2015-02-20 | 2022-02-22 | Incyte Corp | Heterociclos bicíclicos como inhibidores de FGFR |
| US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| TWI744225B (zh) | 2015-02-27 | 2021-11-01 | 美商林伯士拉克許米公司 | 酪胺酸蛋白質激酶２（ｔｙｋ２）抑制劑及其用途 |
| WO2017004134A1 (en) | 2015-06-29 | 2017-01-05 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| JP6853234B2 (ja) * | 2015-07-09 | 2021-03-31 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ | Ｂｔｋ阻害剤としてのピリミジン誘導体及びその使用 |
| MX2018001004A (es) | 2015-07-24 | 2018-06-07 | Celgene Corp | Metodos de sintesis de clorhidrato de (1r,2r,5r)-5-amino-2-metilci clohexanol e intermedios utiles en este. |
| CA2996177A1 (en) | 2015-08-31 | 2017-03-09 | Pharmacyclics Llc | Btk inhibitor combinations for treating multiple myeloma |
| EP4327809A3 (en) | 2015-09-02 | 2024-04-17 | Takeda Pharmaceutical Company Limited | Tyk2 inhibitors and uses thereof |
| CA2997106C (en) | 2015-09-08 | 2024-06-04 | Monash University | Lymph directing prodrugs |
| US10683308B2 (en) | 2015-09-11 | 2020-06-16 | Navitor Pharmaceuticals, Inc. | Rapamycin analogs and uses thereof |
| EP4116303A1 (en) | 2015-09-16 | 2023-01-11 | Loxo Oncology, Inc. | Pyrazolopyrimidine derivatives as btk inhibitors for the treatment of cancer |
| CN106554347B (zh) * | 2015-09-25 | 2020-10-30 | 浙江博生医药有限公司 | Egfr激酶抑制剂及其制备方法和应用 |
| 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 |
| EP3365334B1 (en) | 2015-10-21 | 2024-07-17 | Otsuka Pharmaceutical Co., Ltd. | Benzolactam compounds as protein kinase inhibitors |
| ES2941969T3 (es) | 2015-10-23 | 2023-05-29 | Navitor Pharm Inc | Moduladores de la interacción de Sestrina-GATOR2 y sus usos |
| WO2017106352A1 (en) | 2015-12-14 | 2017-06-22 | Raze Therapeutics, Inc. | Caffeine inhibitors of mthfd2 and uses thereof |
| EP3782994B1 (en) | 2015-12-16 | 2025-07-16 | Loxo Oncology, Inc. | Compounds useful as kinase inhibitors |
| CN107021963A (zh) | 2016-01-29 | 2017-08-08 | 北京诺诚健华医药科技有限公司 | 吡唑稠环类衍生物、其制备方法及其在治疗癌症、炎症和免疫性疾病上的应用 |
| HUE055197T2 (hu) | 2016-03-09 | 2021-11-29 | Raze Therapeutics Inc | 3-Foszfoglicerát-dehidrogenáz inhibitorok és alkalmazásuk |
| WO2017156179A1 (en) | 2016-03-09 | 2017-09-14 | Raze Therapeutics, Inc. | 3-phosphoglycerate dehydrogenase inhibitors and uses thereof |
| US10709708B2 (en) | 2016-03-17 | 2020-07-14 | The University Of North Carolina At Chapel Hill | Method of treating cancer with a combination of MER tyrosine kinase inhibitor and an epidermal growth factor receptor (EGFR) inhibitor |
| CA3019394A1 (en) | 2016-04-08 | 2017-10-12 | X4 Pharmaceuticals, Inc. | Methods for treating cancer |
| CN105968056A (zh) * | 2016-05-28 | 2016-09-28 | 大连医科大学 | 二芳基嘧啶类化合物，组合物及用途 |
| CN109640988A (zh) | 2016-06-21 | 2019-04-16 | X4 制药有限公司 | Cxcr4抑制剂及其用途 |
| WO2017223243A1 (en) | 2016-06-21 | 2017-12-28 | X4 Pharmaceuticals, Inc. | Cxcr4 inhibitors and uses thereof |
| CN109562106B (zh) | 2016-06-21 | 2023-03-21 | X4 制药有限公司 | Cxcr4抑制剂及其用途 |
| CN109475536B (zh) | 2016-07-05 | 2022-05-27 | 百济神州有限公司 | 用于治疗癌症的PD-l拮抗剂和RAF抑制剂的组合 |
| WO2018033853A2 (en) | 2016-08-16 | 2018-02-22 | Beigene, Ltd. | 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 |
| PT3500299T (pt) | 2016-08-19 | 2024-02-21 | Beigene Switzerland Gmbh | Combinação de zanubrutinib com um anticorpo anti-cd20 ou anti-pd-1 para utilização no tratamento do cancro |
| CN106316886A (zh) * | 2016-08-24 | 2017-01-11 | 泰州精英化成医药科技有限公司 | 顺式‑3‑（叔丁氧羰基氨基）环己烷甲酸的制备方法 |
| MA46285A (fr) | 2016-09-19 | 2019-07-31 | Mei Pharma Inc | Polythérapie |
| EP3848370B1 (en) | 2016-10-14 | 2025-05-07 | Takeda Pharmaceutical Company Limited | Tyk2 inhibitors and uses thereof |
| IL266109B2 (en) | 2016-10-21 | 2025-05-01 | Nimbus Lakshmi Inc | Tyk2 inhibitors and uses thereof |
| CN107973754B (zh) * | 2016-10-25 | 2020-04-14 | 清华大学 | 一种小分子抑制剂及其制备方法与其在多发性骨髓瘤治疗中的应用 |
| JP2020023441A (ja) * | 2016-11-02 | 2020-02-13 | 国立大学法人九州大学 | Ｅｇｆｒ阻害及び腫瘍治療に有用な新規化合物 |
| MX2019005029A (es) | 2016-11-03 | 2019-10-24 | Juno Therapeutics Inc | Terapia de combinación de una terapia de células t y un inhibidor de tirosina cinasa de bruton (btk). |
| EP3538091A4 (en) | 2016-11-08 | 2020-06-10 | Navitor Pharmaceuticals, Inc. | PHENYL AMINO PIPERIDINE MTORC INHIBITORS AND USES THEREOF |
| AU2017368050A1 (en) | 2016-11-29 | 2019-06-20 | Puretech Lyt, Inc. | Exosomes for delivery of therapeutic agents |
| WO2018106636A1 (en) | 2016-12-05 | 2018-06-14 | Raze Therapeutics, Inc. | Shmt inhibitors and uses thereof |
| JP2020502238A (ja) | 2016-12-23 | 2020-01-23 | バイスクルアールディー・リミテッド | 新規連結構造を有するペプチド誘導体 |
| CN106632273A (zh) * | 2016-12-29 | 2017-05-10 | 大连医科大学 | 含唑杂环的嘧啶类化合物，组合物及其用途 |
| US10624968B2 (en) | 2017-01-06 | 2020-04-21 | Bicyclerd Limited | Compounds for treating cancer |
| CN108329274B (zh) * | 2017-01-13 | 2021-09-03 | 正大天晴药业集团股份有限公司 | 布鲁顿酪氨酸激酶抑制剂 |
| CN110461847B (zh) | 2017-01-25 | 2022-06-07 | 百济神州有限公司 | (S)-7-(1-(丁-2-炔酰基)哌啶-4-基)-2-(4-苯氧基苯基)-4,5,6,7-四氢吡唑并[1,5-a]嘧啶-3-甲酰胺的结晶形式、其制备及用途 |
| CN108498477A (zh) * | 2017-02-27 | 2018-09-07 | 江苏奥赛康药业股份有限公司 | 一种2-氨基嘧啶类化合物的药用组合物及其制备方法 |
| IL269036B2 (en) | 2017-03-08 | 2023-03-01 | Nimbus Lakshmi Inc | tyk2 inhibitors, uses and methods for their production |
| EP3375778A1 (en) | 2017-03-14 | 2018-09-19 | Artax Biopharma Inc. | Aryl-piperidine derivatives |
| EP3375784A1 (en) | 2017-03-14 | 2018-09-19 | Artax Biopharma Inc. | Aza-dihydro-acridone derivatives |
| JP2020516682A (ja) | 2017-04-07 | 2020-06-11 | エイシア セラピューティクス， インコーポレイテッド | ピロロピリミジンキナーゼの薬学的な塩、物理的形態および組成物、ならびにその作製方法 |
| JOP20190233A1 (ar) | 2017-04-14 | 2019-10-02 | Biogen Ma Inc | نظائر بنزوازيبين بوصفها عوامل مثبطة لتيروزين كيناز بروتون |
| GB201706327D0 (en) | 2017-04-20 | 2017-06-07 | Otsuka Pharma Co Ltd | A pharmaceutical compound |
| US10857196B2 (en) | 2017-04-27 | 2020-12-08 | Bicycletx Limited | Bicyclic peptide ligands and uses thereof |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| EP3641772B1 (en) | 2017-06-22 | 2023-08-02 | Celgene Corporation | Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection |
| WO2019002842A1 (en) | 2017-06-26 | 2019-01-03 | Bicyclerd Limited | BICYCLIC PEPTIDE LIGANDS WITH DETECTABLE FRACTIONS AND USES THEREOF |
| TW202515616A (zh) | 2017-06-26 | 2025-04-16 | 英屬開曼群島商百濟神州有限公司 | 抗pd-1抗體或其抗原結合片段在製備治療用於患有肝細胞癌(hcc)之藥物的用途 |
| EP3658557B1 (en) | 2017-07-28 | 2024-06-05 | Takeda Pharmaceutical Company Limited | Tyk2 inhibitors and uses thereof |
| CN111183147B (zh) | 2017-08-04 | 2024-07-05 | 拜斯科技术开发有限公司 | Cd137特异性的双环肽配体 |
| CN110997677A (zh) | 2017-08-12 | 2020-04-10 | 百济神州有限公司 | 具有改进的双重选择性的Btk抑制剂 |
| US20200291096A1 (en) | 2017-08-14 | 2020-09-17 | Bicyclerd Limited | Bicyclic peptide ligand sting conjugates and uses thereof |
| WO2019034868A1 (en) | 2017-08-14 | 2019-02-21 | Bicyclerd Limited | CONJUGATES PEPTIDE BICYCLIC-LIGAND PPR-A AND USES THEREOF |
| US20200172529A1 (en) * | 2017-08-18 | 2020-06-04 | Beijing Hanmi Pharm. Co., Ltd. | Chemical Compound, Pharmaceutical Composition Thereof, and Use and Application Thereof |
| US11883497B2 (en) | 2017-08-29 | 2024-01-30 | Puretech Lyt, Inc. | Lymphatic system-directing lipid prodrugs |
| EP3675838A4 (en) | 2017-08-29 | 2021-04-21 | PureTech LYT, Inc. | LIPID PRODRUGS DIRECTED TO THE LYMPHATIC SYSTEM |
| KR102383561B1 (ko) * | 2017-09-07 | 2022-04-06 | 한국화학연구원 | 테트라히드로이소퀴놀린기로 치환된 피리미딘 유도체 화합물, 이의 광학이성질체, 또는 이의 약학적으로 허용 가능한 염, 및 이를 유효성분으로 포함하는 암 예방 또는 치료용 조성물 |
| EP3684366A4 (en) | 2017-09-22 | 2021-09-08 | Kymera Therapeutics, Inc. | CRBN LIGANDS AND USES OF THE LATEST |
| WO2019060742A1 (en) | 2017-09-22 | 2019-03-28 | Kymera Therapeutics, Inc | AGENTS FOR DEGRADING PROTEINS AND USES THEREOF |
| ES2925450T3 (es) | 2017-11-06 | 2022-10-18 | Bristol Myers Squibb Co | Compuestos de isofuranona útiles como inhibidores de HPK1 |
| EP3710006A4 (en) | 2017-11-19 | 2021-09-01 | Sunshine Lake Pharma Co., Ltd. | SUBSTITUTED HETEROARYL COMPOUNDS AND THEIR METHODS OF USE |
| WO2019108795A1 (en) | 2017-11-29 | 2019-06-06 | Beigene Switzerland Gmbh | Treatment of indolent or aggressive b-cell lymphomas using a combination comprising btk inhibitors |
| GB201721265D0 (en) | 2017-12-19 | 2018-01-31 | Bicyclerd Ltd | Bicyclic peptide ligands specific for EphA2 |
| US11608345B1 (en) | 2017-12-19 | 2023-03-21 | Puretech Lyt, Inc. | Lipid prodrugs of rapamycin and its analogs and uses thereof |
| TWI825046B (zh) | 2017-12-19 | 2023-12-11 | 英商拜西可泰克斯有限公司 | Epha2特用之雙環胜肽配位基 |
| US11304954B2 (en) | 2017-12-19 | 2022-04-19 | Puretech Lyt, Inc. | Lipid prodrugs of mycophenolic acid and uses thereof |
| EP3727362A4 (en) | 2017-12-19 | 2021-10-06 | PureTech LYT, Inc. | MYCOPHENOLIC ACID LIPID PRODRUGS AND THEIR USES |
| IL315310A (en) | 2017-12-26 | 2024-10-01 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
| EP3737675A4 (en) | 2018-01-12 | 2022-01-05 | Kymera Therapeutics, Inc. | Crbn ligands and uses thereof |
| WO2019140380A1 (en) | 2018-01-12 | 2019-07-18 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| SG11202006701TA (en) | 2018-01-29 | 2020-08-28 | Merck Patent Gmbh | Gcn2 inhibitors and uses thereof |
| IL312674A (en) | 2018-01-29 | 2024-07-01 | Merck Patent Gmbh | GCN2 inhibitors and uses thereof |
| TWI798334B (zh) | 2018-01-31 | 2023-04-11 | 大陸商迪哲（江蘇）醫藥股份有限公司 | Ｅｒｂｂ／ｂｔｋ抑制劑 |
| JP2021514953A (ja) | 2018-02-23 | 2021-06-17 | バイスクルテクス・リミテッド | 多量体二環式ペプチドリガンド |
| CA3091202A1 (en) | 2018-02-27 | 2019-09-06 | Artax Biopharma Inc. | Chromene derivatives as inhibitors of tcr-nck interaction |
| WO2019195753A1 (en) | 2018-04-05 | 2019-10-10 | Tolero Pharmaceuticals, Inc. | Axl kinase inhibitors and use of the same |
| ES2987356T3 (es) | 2018-04-24 | 2024-11-14 | Merck Patent Gmbh | Compuestos antiproliferación y usos de los mismos |
| IL278122B2 (en) | 2018-04-24 | 2024-01-01 | Vertex Pharma | Pteridinone compounds and uses thereof |
| GEP20227433B (en) | 2018-04-26 | 2022-10-25 | Pfizer | 2-amino-pyridine or 2-amino-pyrimidine derivatives as cyclin dependent kinase inhibitors |
| US20210121466A1 (en) | 2018-05-03 | 2021-04-29 | Juno Therapeutics, Inc. | Combination therapy of a chimeric antigen receptor (car) t cell therapy and a kinase inhibitor |
| SG11202010882XA (en) | 2018-05-04 | 2020-11-27 | Incyte Corp | Salts of an fgfr inhibitor |
| SI3788047T1 (sl) | 2018-05-04 | 2024-11-29 | Incyte Corporation | Trdne oblike inhibitorja fgfr in postopki priprave le-teh |
| SG11202012447YA (en) | 2018-06-15 | 2021-01-28 | Navitor Pharm Inc | Rapamycin analogs and uses thereof |
| GB201810316D0 (en) | 2018-06-22 | 2018-08-08 | Bicyclerd Ltd | Peptide ligands for binding to EphA2 |
| US11180531B2 (en) | 2018-06-22 | 2021-11-23 | Bicycletx Limited | Bicyclic peptide ligands specific for Nectin-4 |
| WO2020010227A1 (en) | 2018-07-06 | 2020-01-09 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| US11292792B2 (en) | 2018-07-06 | 2022-04-05 | Kymera Therapeutics, Inc. | Tricyclic CRBN ligands and uses thereof |
| CN112512597A (zh) | 2018-07-26 | 2021-03-16 | 大日本住友制药肿瘤公司 | 用于治疗与acvr1表达异常相关的疾病的方法以及用于此的acvr1抑制剂 |
| US10548889B1 (en) | 2018-08-31 | 2020-02-04 | X4 Pharmaceuticals, Inc. | Compositions of CXCR4 inhibitors and methods of preparation and use |
| EP3846793B1 (en) | 2018-09-07 | 2024-01-24 | PIC Therapeutics, Inc. | Eif4e inhibitors and uses thereof |
| US11066404B2 (en) | 2018-10-11 | 2021-07-20 | Incyte Corporation | Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors |
| WO2020081508A1 (en) | 2018-10-15 | 2020-04-23 | Nimbus Lakshmi, Inc. | Tyk2 inhibitors and uses thereof |
| US10919937B2 (en) | 2018-10-23 | 2021-02-16 | Bicycletx Limited | Bicyclic peptide ligands and uses thereof |
| CN109608444B (zh) * | 2018-11-27 | 2022-02-11 | 中国药科大学 | 含异吲哚啉酮的erk抑制剂及其制备方法与用途 |
| US11352350B2 (en) | 2018-11-30 | 2022-06-07 | Kymera Therapeutics, Inc. | IRAK degraders and uses thereof |
| WO2020112937A1 (en) | 2018-11-30 | 2020-06-04 | Nimbus Lakshmi, Inc. | Tyk2 inhibitors and uses thereof |
| GB201820288D0 (en) | 2018-12-13 | 2019-01-30 | Bicycle Tx Ltd | Bicycle peptide ligaands specific for MT1-MMP |
| GB201820295D0 (en) | 2018-12-13 | 2019-01-30 | Bicyclerd Ltd | Bicyclic peptide ligands specific for MT1-MMP |
| GB201820325D0 (en) | 2018-12-13 | 2019-01-30 | Bicyclerd Ltd | Bicyclic peptide ligands specific for psma |
| EP3670659A1 (en) | 2018-12-20 | 2020-06-24 | Abivax | Biomarkers, and uses in treatment of viral infections, inflammations, or cancer |
| WO2020128526A1 (en) | 2018-12-21 | 2020-06-25 | Bicycletx Limited | Bicyclic peptide ligands specific for pd-l1 |
| AU2020212001A1 (en) | 2019-01-23 | 2021-07-22 | Takeda Pharmaceutical Company Limited | TYK2 inhibitors and uses thereof |
| CN109776495A (zh) * | 2019-01-31 | 2019-05-21 | 李佳睿 | 抗肿瘤化合物及其制备方法与用途 |
| WO2020165600A1 (en) | 2019-02-14 | 2020-08-20 | Bicycletx Limited | Bicyclic peptide ligand sting conjugates and uses thereof |
| WO2020168197A1 (en) | 2019-02-15 | 2020-08-20 | Incyte Corporation | Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors |
| WO2020180959A1 (en) | 2019-03-05 | 2020-09-10 | Incyte Corporation | Pyrazolyl pyrimidinylamine compounds as cdk2 inhibitors |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| WO2020205560A1 (en) | 2019-03-29 | 2020-10-08 | Incyte Corporation | Sulfonylamide compounds as cdk2 inhibitors |
| MX2021011810A (es) | 2019-03-29 | 2021-10-26 | Astrazeneca Ab | Osimertinib para su uso en el tratamiento de cancer de pulmon de celulas no peque?as. |
| JP2022528887A (ja) | 2019-04-02 | 2022-06-16 | バイスクルテクス・リミテッド | バイシクルトキシンコンジュゲートおよびその使用 |
| SG11202110829YA (en) | 2019-04-05 | 2021-10-28 | Kymera Therapeutics Inc | Stat degraders and uses thereof |
| WO2020223469A1 (en) | 2019-05-01 | 2020-11-05 | Incyte Corporation | N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer |
| US11447494B2 (en) | 2019-05-01 | 2022-09-20 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| PL3966206T3 (pl) | 2019-05-10 | 2024-01-29 | Deciphera Pharmaceuticals, Llc | Heteroaryloaminopirymidynoamidowe inhibitory autofagii i sposoby ich zastosowania |
| HUE065486T2 (hu) | 2019-05-10 | 2024-05-28 | Deciphera Pharmaceuticals Llc | Fenilaminopirimidinamid autophágia inhibitorok és azok felhasználási eljárásai |
| KR20220034739A (ko) | 2019-05-31 | 2022-03-18 | 이케나 온콜로지, 인코포레이티드 | Tead 억제제 및 이의 용도 |
| 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 |
| AU2020297422B2 (en) | 2019-06-17 | 2024-03-21 | Deciphera Pharmaceuticals, Llc | Aminopyrimidine amide autophagy inhibitors and methods of use thereof |
| WO2020257495A1 (en) * | 2019-06-18 | 2020-12-24 | Purdue Research Foundation | Inhibitors of erythrocyte band 3 tyrosine phosphorylation and uses thereof |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| TWI862640B (zh) | 2019-07-30 | 2024-11-21 | 英商拜西可泰克斯有限公司 | 異質雙環肽複合物 |
| CN110305140B (zh) * | 2019-07-30 | 2020-08-04 | 上海勋和医药科技有限公司 | 二氢吡咯并嘧啶类选择性jak2抑制剂 |
| PH12022550361A1 (en) | 2019-08-14 | 2023-02-27 | Incyte Corp | Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors |
| EP4028385A4 (en) | 2019-09-11 | 2023-11-08 | Vincere Biosciences, Inc. | USP30 INHIBITORS AND USES THEREOF |
| US12215105B2 (en) | 2019-09-13 | 2025-02-04 | Nimbus Saturn, Inc. | HPK1 antagonists and uses thereof |
| CN112574207B (zh) * | 2019-09-30 | 2023-04-11 | 南京药石科技股份有限公司 | Erk1/2蛋白激酶抑制剂及其用途 |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| PE20221905A1 (es) | 2019-10-11 | 2022-12-23 | Incyte Corp | Aminas biciclicas como inhibidoras de la cdk2 |
| US11607416B2 (en) | 2019-10-14 | 2023-03-21 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| EP4056181A4 (en) * | 2019-11-08 | 2023-12-20 | Shenzhen Chipscreen Biosciences Co., Ltd. | USE OF A COMPOUND IN THE PREVENTION OR TREATMENT OF GRAFT-VERSE-HOST DISEASE |
| CN112933049B (zh) * | 2019-11-26 | 2024-02-06 | 深圳微芯生物科技股份有限公司 | 含无定型态芳杂环化合物的组合物、其制备方法及用途 |
| EP4069696A1 (en) | 2019-12-04 | 2022-10-12 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2021113462A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Derivatives of an fgfr inhibitor |
| TW202134234A (zh) | 2019-12-05 | 2021-09-16 | 美商奈維特製藥公司 | 雷帕黴素類似物及其用途 |
| EP4076520A4 (en) | 2019-12-17 | 2024-03-27 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| WO2021127283A2 (en) | 2019-12-17 | 2021-06-24 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| EP4076661A1 (en) | 2019-12-20 | 2022-10-26 | Nuevolution A/S | Compounds active towards nuclear receptors |
| EP4076657A1 (en) | 2019-12-20 | 2022-10-26 | Nuevolution A/S | Compounds active towards nuclear receptors |
| BR112022012410A2 (pt) | 2019-12-23 | 2022-08-30 | Kymera Therapeutics Inc | Degradadores smarca e usos dos mesmos |
| WO2021138391A1 (en) | 2019-12-30 | 2021-07-08 | Tyra Biosciences, Inc. | Indazole compounds |
| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| CN111620852B (zh) * | 2020-01-19 | 2023-05-09 | 镇江植生源农业科技有限公司 | 一种5-氯-嘧啶-2,4-二胺类化合物及其制备方法和应用 |
| WO2021159021A1 (en) | 2020-02-05 | 2021-08-12 | Puretech Lyt, Inc. | Lipid prodrugs of neurosteroids |
| BR112022017727A2 (pt) | 2020-03-03 | 2022-11-16 | Pic Therapeutics Inc | Inibidores de eif4e e usos dos mesmos |
| PH12022552458A1 (en) | 2020-03-19 | 2024-01-22 | Kymera Therapeutics Inc | Mdm2 degraders and uses thereof |
| WO2021198955A1 (en) | 2020-03-31 | 2021-10-07 | Nuevolution A/S | Compounds active towards nuclear receptors |
| EP4126875A1 (en) | 2020-03-31 | 2023-02-08 | Nuevolution A/S | Compounds active towards nuclear receptors |
| TW202210483A (zh) | 2020-06-03 | 2022-03-16 | 美商凱麥拉醫療公司 | Irak降解劑之結晶型 |
| US20230250110A1 (en) | 2020-06-03 | 2023-08-10 | Kymera Therapeutics, Inc. | Deuterated irak degraders and uses thereof |
| CN111646978B (zh) * | 2020-06-11 | 2021-12-21 | 浙江大学 | N2-取代烷氧芳环-2-氨基嘧啶类衍生物及应用 |
| WO2022006518A1 (en) * | 2020-07-02 | 2022-01-06 | The Cleveland Clinic Foundation | Compounds and methods of promoting oligodendrocyte precursor differentiation |
| KR20230074721A (ko) | 2020-08-17 | 2023-05-31 | 바이사이클티엑스 리미티드 | Nectin-4에 특이적인 이환 콘쥬게이트 및 이의 용도 |
| CN116249690A (zh) * | 2020-09-22 | 2023-06-09 | 百济神州有限公司 | 作为egfr抑制剂的吲哚啉化合物和衍生物 |
| WO2022072632A1 (en) * | 2020-09-30 | 2022-04-07 | Scorpion Therapeutics, Inc. | Bicyclic compounds for use in the treatment cancer |
| EP4232425A4 (en) | 2020-10-23 | 2024-07-24 | Nimbus Clotho, Inc. | Ctps1 inhibitors and uses thereof |
| CA3200814A1 (en) | 2020-12-02 | 2022-06-09 | Alfredo C. Castro | Tead inhibitors and uses thereof |
| WO2022120353A1 (en) | 2020-12-02 | 2022-06-09 | Ikena Oncology, Inc. | Tead inhibitors and uses thereof |
| TW202241891A (zh) | 2020-12-30 | 2022-11-01 | 美商凱麥拉醫療公司 | Irak降解劑及其用途 |
| KR20230152692A (ko) * | 2021-02-02 | 2023-11-03 | 리미널 바이오사이언시스 리미티드 | Gpr84 길항제 및 이의 용도 |
| EP4288427A1 (en) | 2021-02-02 | 2023-12-13 | Liminal Biosciences Limited | Gpr84 antagonists and uses thereof |
| US12252488B2 (en) | 2021-02-12 | 2025-03-18 | Nimbus Saturn, Inc. | HPK1 antagonists and uses thereof |
| IL304905A (en) | 2021-02-15 | 2023-10-01 | Kymera Therapeutics Inc | IRAK4 joints and their uses |
| JP2024506656A (ja) | 2021-02-15 | 2024-02-14 | カイメラ セラピューティクス， インコーポレイテッド | Ｉｒａｋ４分解剤およびその使用 |
| WO2022187856A1 (en) | 2021-03-05 | 2022-09-09 | Nimbus Saturn, Inc. | Hpk1 antagonists and uses thereof |
| US12071442B2 (en) | 2021-03-29 | 2024-08-27 | Nimbus Saturn, Inc. | Substituted pyrrolo[3,4-c]pyridines as HPK1 antagonists |
| CN115160319B (zh) * | 2021-04-01 | 2023-12-26 | 西安新通药物研究股份有限公司 | 含1,3-苯并二氧戊环结构的化合物及其制备方法与用途 |
| EP4313023A1 (en) | 2021-04-02 | 2024-02-07 | Biogen MA Inc. | Combination treatment methods of multiple sclerosis |
| WO2022217276A1 (en) | 2021-04-09 | 2022-10-13 | Nimbus Clio, Inc. | Cbl-b modulators and uses thereof |
| WO2022221170A1 (en) | 2021-04-12 | 2022-10-20 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| AU2022258968A1 (en) | 2021-04-16 | 2023-10-19 | Ikena Oncology, Inc. | Mek inhibitors and uses thereof |
| US12097261B2 (en) | 2021-05-07 | 2024-09-24 | Kymera Therapeutics, Inc. | CDK2 degraders and uses thereof |
| WO2022261159A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2022261160A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| US11981671B2 (en) | 2021-06-21 | 2024-05-14 | Incyte Corporation | Bicyclic pyrazolyl amines as CDK2 inhibitors |
| EP4392421A1 (en) | 2021-08-25 | 2024-07-03 | PIC Therapeutics, Inc. | Eif4e inhibitors and uses thereof |
| JP2024534127A (ja) | 2021-08-25 | 2024-09-18 | ピク セラピューティクス， インコーポレイテッド | ｅＩＦ４Ｅ阻害剤及びその使用 |
| WO2023076556A1 (en) | 2021-10-29 | 2023-05-04 | Kymera Therapeutics, Inc. | Irak4 degraders and synthesis thereof |
| US11976073B2 (en) | 2021-12-10 | 2024-05-07 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| WO2023114984A1 (en) | 2021-12-17 | 2023-06-22 | Ikena Oncology, Inc. | Tead inhibitors and uses thereof |
| JP2025504059A (ja) | 2022-01-31 | 2025-02-06 | カイメラ セラピューティクス， インコーポレイテッド | Ｉｒａｋデグレーダー及びその使用 |
| WO2023173053A1 (en) | 2022-03-10 | 2023-09-14 | Ikena Oncology, Inc. | Mek inhibitors and uses thereof |
| WO2023173057A1 (en) | 2022-03-10 | 2023-09-14 | Ikena Oncology, Inc. | Mek inhibitors and uses thereof |
| US12233056B2 (en) | 2022-04-06 | 2025-02-25 | Syntara Limited | Lysyl oxidase inhibitors for treating myeloid malignancies |
| WO2023211889A1 (en) | 2022-04-25 | 2023-11-02 | Ikena Oncology, Inc. | Polymorphic compounds and uses thereof |
| WO2023220655A1 (en) | 2022-05-11 | 2023-11-16 | 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 |
| US11878958B2 (en) | 2022-05-25 | 2024-01-23 | Ikena Oncology, Inc. | MEK inhibitors and uses thereof |
| US11786531B1 (en) | 2022-06-08 | 2023-10-17 | Beigene Switzerland Gmbh | Methods of treating B-cell proliferative disorder |
| JP2025527248A (ja) | 2022-08-02 | 2025-08-20 | リミナル・バイオサイエンシーズ・リミテッド | 置換ピリドンｇｐｒ８４アンタゴニスト及びその使用 |
| WO2024028364A1 (en) | 2022-08-02 | 2024-02-08 | Liminal Biosciences Limited | Aryl-triazolyl and related gpr84 antagonists and uses thereof |
| EP4565568A1 (en) | 2022-08-02 | 2025-06-11 | Liminal Biosciences Limited | Heteroaryl carboxamide and related gpr84 antagonists and uses thereof |
| CN115448906B (zh) * | 2022-09-26 | 2024-04-02 | 深圳大学 | 一种2-苯胺基嘧啶类衍生物及其制备方法与应用 |
| US20240208961A1 (en) | 2022-11-22 | 2024-06-27 | PIC Therapeutics, Inc. | Eif4e inhibitors and uses thereof |
| IL321486A (en) | 2023-06-23 | 2025-08-01 | Kymera Therapeutics Inc | Iraqi joints and their uses |
| TW202529769A (zh) | 2023-09-21 | 2025-08-01 | 日商武田藥品工業股份有限公司 | Ｔｙｋ２抑制劑及其用途 |
| TW202515850A (zh) * | 2023-09-22 | 2025-04-16 | 大陸商江蘇恆瑞醫藥股份有限公司 | 雜芳基類化合物、其製備方法及其在醫藥上的應用 |
| CN119707835A (zh) * | 2024-11-25 | 2025-03-28 | 沈阳药科大学 | 2-氨基嘧啶-5-甲酰胺类化合物及用于制备治疗和/或预防癌症药物中的用途 |
Family Cites Families (174)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4032637A (en) | 1972-09-26 | 1977-06-28 | Sandoz Ltd. | Method of promoting sleep |
| US4650750A (en) | 1982-02-01 | 1987-03-17 | Giese Roger W | Method of chemical analysis employing molecular release tag compounds |
| US5516931A (en) | 1982-02-01 | 1996-05-14 | Northeastern University | Release tag compounds producing ketone signal groups |
| US4709016A (en) | 1982-02-01 | 1987-11-24 | Northeastern University | Molecular analytical release tags and their use in chemical analysis |
| US5650270A (en) | 1982-02-01 | 1997-07-22 | Northeastern University | Molecular analytical release tags and their use in chemical analysis |
| GB8608335D0 (en) | 1986-04-04 | 1986-05-08 | Pfizer Ltd | Pharmaceutically acceptable salts |
| US5453510A (en) | 1990-07-13 | 1995-09-26 | Burroughs Wellcome Co. | Neuromuscular blocking agents |
| JPH0741461A (ja) | 1993-05-27 | 1995-02-10 | Eisai Co Ltd | スルホン酸エステル誘導体 |
| DK0813525T3 (da) | 1995-03-10 | 2004-02-16 | Berlex Lab | Benzamidinderivater, deres fremstilling og anvendelse som antikoagulanter |
| GB9523675D0 (en) * | 1995-11-20 | 1996-01-24 | Celltech Therapeutics Ltd | Chemical compounds |
| GB9619284D0 (en) | 1996-09-16 | 1996-10-30 | Celltech Therapeutics Ltd | Chemical compounds |
| GB9622363D0 (en) | 1996-10-28 | 1997-01-08 | Celltech Therapeutics Ltd | Chemical compounds |
| JP4135318B2 (ja) * | 1997-12-15 | 2008-08-20 | アステラス製薬株式会社 | 新規なピリミジン−５−カルボキサミド誘導体 |
| US6303652B1 (en) | 1998-08-21 | 2001-10-16 | Hughes Institute | BTK inhibitors and methods for their identification and use |
| AU5438299A (en) | 1998-08-29 | 2000-03-21 | Astrazeneca Ab | Pyrimidine compounds |
| AU762523C (en) | 1998-11-10 | 2004-02-12 | Janssen Pharmaceutica N.V. | HIV replication inhibiting pyrimidines |
| US6262088B1 (en) | 1998-11-19 | 2001-07-17 | Berlex Laboratories, Inc. | Polyhydroxylated monocyclic N-heterocyclic derivatives as anti-coagulants |
| US6127376A (en) | 1998-12-04 | 2000-10-03 | Berlex Laboratories, Inc. | Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants |
| GB9828511D0 (en) | 1998-12-24 | 1999-02-17 | Zeneca Ltd | Chemical compounds |
| US6495558B1 (en) | 1999-01-22 | 2002-12-17 | Amgen Inc. | Kinase inhibitors |
| WO2000046203A2 (en) | 1999-02-04 | 2000-08-10 | Millennium Pharmaceuticals, Inc. | G-protein coupled heptahelical receptor binding compounds and methods of use thereof |
| GB9914258D0 (en) | 1999-06-18 | 1999-08-18 | Celltech Therapeutics Ltd | Chemical compounds |
| ATE247645T1 (de) | 1999-06-29 | 2003-09-15 | Egyt Gyogyszervegyeszeti Gyar | Neue piperazinylalkylthiopyrimidine derivate, diese enthaltende pharmazeutische zusammenstellungen und verfahren zu deren herstellung |
| DE60043397D1 (de) | 1999-12-28 | 2010-01-07 | Pharmacopeia Inc | Cytokine, insbesondere tnf-alpha, hemmer |
| AU2001237041B9 (en) * | 2000-02-17 | 2005-07-28 | Amgen Inc. | Kinase inhibitors |
| GB0004888D0 (en) * | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| GB0004887D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| GB0004890D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| US7034019B2 (en) | 2000-05-08 | 2006-04-25 | Janssen Pharmaceutica N.V. | Prodrugs of HIV replication inhibiting pyrimidines |
| GB0016877D0 (en) * | 2000-07-11 | 2000-08-30 | Astrazeneca Ab | Chemical compounds |
| CA2417500C (en) | 2000-07-28 | 2008-11-18 | Georgetown University Medical Center | Erbb-2 selective small molecule kinase inhibitors |
| US6881737B2 (en) | 2001-04-11 | 2005-04-19 | Amgen Inc. | Substituted triazinyl acrylamide derivatives and methods of use |
| JO3429B1 (ar) | 2001-08-13 | 2019-10-20 | Janssen Pharmaceutica Nv | مشتقات برميدينات مثبطة فيروس الايدز |
| US6939874B2 (en) | 2001-08-22 | 2005-09-06 | Amgen Inc. | Substituted pyrimidinyl derivatives and methods of use |
| WO2003030909A1 (en) | 2001-09-25 | 2003-04-17 | Bayer Pharmaceuticals Corporation | 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer |
| CA2463822A1 (en) | 2001-11-01 | 2003-05-08 | Janssen Pharmaceutica N.V. | Heteroaryl amines as glycogen synthase kinase 3beta inhibitors (gsk3 inhibitors) |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| WO2003066601A1 (en) | 2002-02-08 | 2003-08-14 | Smithkline Beecham Corporation | Pyrimidine compounds |
| GB0206215D0 (en) | 2002-03-15 | 2002-05-01 | Novartis Ag | Organic compounds |
| WO2003081210A2 (en) | 2002-03-21 | 2003-10-02 | Sunesis Pharmaceuticals, Inc. | Identification of kinase inhibitors |
| US20040002395A1 (en) * | 2002-06-27 | 2004-01-01 | Poynor Raymond L. | Bridge weight for metal wood golf club |
| CN103169708B (zh) | 2002-07-29 | 2018-02-02 | 里格尔药品股份有限公司 | 用2,4‑嘧啶二胺化合物治疗或者预防自体免疫性疾病的方法 |
| 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 |
| WO2004050068A1 (en) | 2002-11-29 | 2004-06-17 | Janssen Pharmaceutica N.V. | Pharmaceutical compositions comprising a basic respectively acidic drug compound, a surfactant and a physiologically tolerable water-soluble acid respectively base |
| UA80767C2 (en) | 2002-12-20 | 2007-10-25 | Pfizer Prod Inc | Pyrimidine derivatives for the treatment of abnormal cell growth |
| EA011164B1 (ru) | 2003-02-07 | 2009-02-27 | Янссен Фармацевтика Н. В. | Производные пиримидина для профилактики вич-инфекции |
| DE602004021472D1 (en) * | 2003-02-20 | 2009-07-23 | Smithkline Beecham Corp | Pyrimiidinverbindungen |
| GB0305929D0 (en) | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
| US20050014753A1 (en) | 2003-04-04 | 2005-01-20 | Irm Llc | Novel compounds and compositions as protein kinase inhibitors |
| US20050043233A1 (en) | 2003-04-29 | 2005-02-24 | Boehringer Ingelheim International Gmbh | Combinations for the treatment of diseases involving cell proliferation, migration or apoptosis of myeloma cells or angiogenesis |
| US7504396B2 (en) | 2003-06-24 | 2009-03-17 | Amgen Inc. | Substituted heterocyclic compounds and methods of use |
| US7122542B2 (en) | 2003-07-30 | 2006-10-17 | Rigel Pharmaceuticals, Inc. | Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds |
| DK1663242T3 (da) | 2003-08-07 | 2011-08-01 | Rigel Pharmaceuticals Inc | 2,4-Pyrimidindiamin-forbindelser og anvendelse som antiproliferative midler |
| JP4607879B2 (ja) * | 2003-08-15 | 2011-01-05 | ノバルティス アーゲー | 新生物疾患、炎症および免疫障害の処置に有用な２，４−ピリミジンジアミン |
| GB0321710D0 (en) | 2003-09-16 | 2003-10-15 | Novartis Ag | Organic compounds |
| CA2538413A1 (en) | 2003-09-18 | 2005-03-24 | Novartis Ag | 2,4-di (phenylamino) pyrimidines useful in the treatment of proliferative disorders |
| US7511137B2 (en) | 2003-12-19 | 2009-03-31 | Rigel Pharmaceuticals, Inc. | Stereoisomers and stereoisomeric mixtures of 1-(2,4-pyrimidinediamino)-2-cyclopentanecarboxamide synthetic intermediates |
| GB2432834A (en) | 2004-01-12 | 2007-06-06 | Cytopia Res Pty Ltd | Selective Kinase Inhibitors |
| CN1930128A (zh) | 2004-01-16 | 2007-03-14 | 惠氏公司 | 受体酪氨酸激酶抑制剂的喹啉中间体及其合成 |
| ATE545413T1 (de) | 2004-03-15 | 2012-03-15 | Lilly Co Eli | Antagonisten des opioidrezeptors |
| US7558717B2 (en) | 2004-04-28 | 2009-07-07 | Vertex Pharmaceuticals Incorporated | Crystal structure of human JAK3 kinase domain complex and binding pockets thereof |
| JP4812763B2 (ja) | 2004-05-18 | 2011-11-09 | ライジェル ファーマシューティカルズ， インコーポレイテッド | シクロアルキル置換ピリミジンジアミン化合物およびそれらの用途 |
| EP1598343A1 (de) | 2004-05-19 | 2005-11-23 | Boehringer Ingelheim International GmbH | 2-Arylaminopyrimidine als PLK Inhibitoren |
| EP2592155B2 (en) | 2004-06-04 | 2019-09-11 | Genentech, Inc. | EGFR mutations |
| US7521457B2 (en) | 2004-08-20 | 2009-04-21 | Boehringer Ingelheim International Gmbh | Pyrimidines as PLK inhibitors |
| GB0419161D0 (en) | 2004-08-27 | 2004-09-29 | Novartis Ag | Organic compounds |
| CA2581454A1 (en) | 2004-09-23 | 2006-03-30 | Reddy Us Therapeutics, Inc. | Novel pyrimidine compounds, process for their preparation and compositions containing them |
| AU2005288865B2 (en) | 2004-09-30 | 2012-07-19 | Janssen Sciences Ireland Uc | HIV inhibiting 5-carbo- or heterocyclic substituted pyrimidines |
| MX2007004488A (es) | 2004-10-13 | 2007-09-11 | Wyeth Corp | Analogos de anilino-pirimidina n-bencenosulfonilo sustituidos. |
| EP1805208A2 (en) | 2004-10-20 | 2007-07-11 | Proteolix, Inc. | Labeled compounds for proteasome inhibition |
| TW200628463A (en) | 2004-11-10 | 2006-08-16 | Synta Pharmaceuticals Corp | Heteroaryl compounds |
| GB2420559B (en) | 2004-11-15 | 2008-08-06 | Rigel Pharmaceuticals Inc | Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses |
| ATE540035T1 (de) | 2004-11-24 | 2012-01-15 | Rigel Pharmaceuticals Inc | Spiro-2,4-pyrimidindiamin-verbindungen und ihre verwendungen |
| MY169441A (en) | 2004-12-08 | 2019-04-11 | Janssen Pharmaceutica Nv | 2,4, (4,6) pyrimidine derivatives |
| US8211929B2 (en) * | 2004-12-30 | 2012-07-03 | Exelixis, Inc. | Pyrimidine derivatives as kinase modulators and method of use |
| WO2006076706A1 (en) | 2005-01-14 | 2006-07-20 | Millennium Pharmaceuticals, Inc. | Cinnamide and hydrocinnamide derivatives with raf-kinase inhibitory activity |
| US7449458B2 (en) | 2005-01-19 | 2008-11-11 | Rigel Pharmaceuticals, Inc. | Prodrugs of 2,4-pyrimidinediamine compounds and their uses |
| WO2006086777A2 (en) | 2005-02-11 | 2006-08-17 | Memorial Sloan Kettering Cancer Center | Methods and compositions for detecting a drug resistant egfr mutant |
| CN101155799A (zh) * | 2005-03-16 | 2008-04-02 | 塔格根公司 | 嘧啶化合物和使用方法 |
| DE102005016634A1 (de) | 2005-04-12 | 2006-10-19 | Merck Patent Gmbh | Neuartige Aza-Hetercyclen als Kinase-Inhibitoren |
| US20060270694A1 (en) | 2005-05-03 | 2006-11-30 | Rigel Pharmaceuticals, Inc. | JAK kinase inhibitors and their uses |
| WO2006124874A2 (en) | 2005-05-12 | 2006-11-23 | Kalypsys, Inc. | Inhibitors of b-raf kinase |
| WO2006128172A2 (en) | 2005-05-26 | 2006-11-30 | Synta Pharmaceuticals Corp. | Method for treating b cell regulated autoimmune disorders |
| WO2006128129A2 (en) | 2005-05-26 | 2006-11-30 | Synta Pharmaceuticals Corp. | Method for treating cancer |
| WO2006129100A1 (en) | 2005-06-03 | 2006-12-07 | Glaxo Group Limited | Novel compounds |
| US20070203161A1 (en) | 2006-02-24 | 2007-08-30 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| RU2485106C2 (ru) | 2005-06-08 | 2013-06-20 | Райджел Фамэсьютикэлз, Инк. | Соединения, проявляющие активность в отношении jak-киназы (варианты), способ лечения заболеваний, опосредованных jak-киназой, способ ингибирования активности jak-киназы (варианты), фармацевтическая композиция на основе указанных соединений |
| CN101282945A (zh) * | 2005-06-08 | 2008-10-08 | 里格尔药品股份有限公司 | 抑制jak途径的组合物和方法 |
| AU2006283592A1 (en) | 2005-08-22 | 2007-03-01 | Amgen Inc. | Pyrazolopyridine and pyrazolopyrimidine compounds useful as kinase enzymes modulators |
| EP1948663B1 (en) | 2005-10-21 | 2011-09-14 | Exelixis, Inc. | Pyrazolo-pyrimidines as casein kinase ii (ck2) modulators |
| MY167260A (en) | 2005-11-01 | 2018-08-14 | Targegen Inc | Bi-aryl meta-pyrimidine inhibitors of kinases |
| KR20080053954A (ko) * | 2005-11-03 | 2008-06-16 | 아이알엠 엘엘씨 | 단백질 키나제 억제제 |
| US7713987B2 (en) | 2005-12-06 | 2010-05-11 | Rigel Pharmaceuticals, Inc. | Pyrimidine-2,4-diamines and their uses |
| WO2007120339A1 (en) | 2005-12-19 | 2007-10-25 | Genentech, Inc. | Pyrimidine kinase inhibitors |
| TW200736232A (en) * | 2006-01-26 | 2007-10-01 | Astrazeneca Ab | Pyrimidine derivatives |
| EP1979329A2 (en) | 2006-01-30 | 2008-10-15 | Exelixis, Inc. | 4-aryl-2-amino-pyrimidines or 4-aryl-2-aminoalkyl-pyrimidines as jak-2 modulators and methods of use |
| CA2642211C (en) | 2006-02-17 | 2012-01-24 | Rigel Pharmaceuticals, Inc. | 2,4-pyrimidinediamine compounds for treating or preventing autoimmune diseases |
| US8962643B2 (en) | 2006-02-24 | 2015-02-24 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the JAK pathway |
| WO2007113254A1 (en) | 2006-03-30 | 2007-10-11 | Tibotec Pharmaceuticals Ltd. | Hiv inhibiting 5-amido substituted pyrimidines |
| AU2007233739B2 (en) | 2006-03-30 | 2013-01-17 | Janssen Sciences Ireland Uc | HIV inhibiting 5-(hydroxymethylene and aminomethylene) substituted pyrimidines |
| GB0608386D0 (en) | 2006-04-27 | 2006-06-07 | Senexis Ltd | Compounds |
| CA2651732C (en) | 2006-05-18 | 2014-10-14 | Mannkind Corporation | Intracellular kinase inhibitors |
| DE102006027156A1 (de) | 2006-06-08 | 2007-12-13 | Bayer Schering Pharma Ag | Sulfimide als Proteinkinaseinhibitoren |
| CA2656290A1 (en) | 2006-07-05 | 2008-01-10 | Exelixis, Inc. | Methods of using igf1r and abl kinase modulators |
| EP2046759A1 (en) | 2006-07-21 | 2009-04-15 | Novartis AG | 2, 4 -di (arylaminio) -pyrimidine-5-carboxamide compounds as jak kinases inhibitors |
| DE102006041382A1 (de) | 2006-08-29 | 2008-03-20 | Bayer Schering Pharma Ag | Carbamoyl-Sulfoximide als Proteinkinaseinhibitoren |
| EP2526934B1 (en) | 2006-09-22 | 2015-12-09 | Pharmacyclics LLC | Inhibitors of bruton's tyrosine kinase |
| CA2673125C (en) * | 2006-10-19 | 2015-04-21 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| EP2089391B1 (en) | 2006-11-03 | 2013-01-16 | Pharmacyclics, Inc. | Bruton's tyrosine kinase activity probe and method of using |
| US8163902B2 (en) | 2006-11-21 | 2012-04-24 | Rigel Pharmaceuticals, Inc. | Prodrugs of 2,4-pyrimidinediamine compounds and their uses |
| BRPI0720264B1 (pt) * | 2006-12-08 | 2022-03-03 | Novartis Ag | Compostos e composições como inibidores de proteína cinase |
| EP2099771A1 (en) * | 2006-12-19 | 2009-09-16 | Genentech, Inc. | Pyrimidine kinase inhibitors |
| EP1939185A1 (de) | 2006-12-20 | 2008-07-02 | Bayer Schering Pharma Aktiengesellschaft | Neuartige Hetaryl-Phenylendiamin-Pyrimidine als Proteinkinaseinhibitoren zur Behandlung von Krebs |
| WO2008080965A2 (en) | 2006-12-29 | 2008-07-10 | Tibotec Pharmaceuticals Ltd. | Hiv inhibiting 5,6-substituted pyrimidines |
| JP5185283B2 (ja) | 2006-12-29 | 2013-04-17 | テイボテク・フアーマシユーチカルズ | Ｈｉｖ阻害６−置換ピリミジン |
| TW200902010A (en) | 2007-01-26 | 2009-01-16 | Smithkline Beecham Corp | Anthranilamide inhibitors of aurora kinase |
| AU2008210266B2 (en) | 2007-01-31 | 2013-09-05 | Ym Biosciences Australia Pty Ltd | Thiopyrimidine-based compounds and uses thereof |
| DE102007010801A1 (de) | 2007-03-02 | 2008-09-04 | Bayer Cropscience Ag | Diaminopyrimidine als Fungizide |
| JP2010522186A (ja) | 2007-03-20 | 2010-07-01 | スミスクライン ビーチャム コーポレーション | 化合物 |
| CA2681250A1 (en) | 2007-03-20 | 2008-09-25 | Smithkline Beecham Corporation | Chemical compounds |
| WO2008118822A1 (en) | 2007-03-23 | 2008-10-02 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| US7834024B2 (en) | 2007-03-26 | 2010-11-16 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the JAK pathway |
| US20120065201A1 (en) | 2007-03-28 | 2012-03-15 | Pharmacyclics, Inc. | Inhibitors of bruton's tyrosine kinase |
| US8809273B2 (en) | 2007-03-28 | 2014-08-19 | Pharmacyclics, Inc. | Inhibitors of Bruton's tyrosine kinase |
| TWI433677B (zh) | 2007-06-04 | 2014-04-11 | Avila Therapeutics Inc | 雜環化合物及其用途 |
| CA2693594A1 (en) * | 2007-07-17 | 2009-01-22 | Rigel Pharmaceuticals, Inc. | Cyclic amine substituted pyrimidinediamines as pkc inhibitors |
| WO2009017838A2 (en) * | 2007-08-01 | 2009-02-05 | Exelixis, Inc. | Combinations of jak-2 inhibitors and other agents |
| US20090088371A1 (en) | 2007-08-28 | 2009-04-02 | Rigel Pharmaceuticals, Inc. | Combination therapy with syk kinase inhibitor |
| EP2190826A2 (en) | 2007-08-28 | 2010-06-02 | Irm Llc | 2-biphenylamino-4-aminopyrimidine derivatives as kinase inhibitors |
| AU2008296479A1 (en) | 2007-08-28 | 2009-03-12 | Dana Farber Cancer Institute | Amino substituted pyrimidine, pyrollopyridine and pyrazolopyrimidine derivatives useful as kinase inhibitors and in treating proliferative disorders and diseases associated with angiogenesis |
| 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 |
| US20110028405A1 (en) | 2007-12-20 | 2011-02-03 | Richard John Harrison | Sulfamides as zap-70 inhibitors |
| ES2610880T3 (es) | 2008-02-22 | 2017-05-03 | Rigel Pharmaceuticals, Inc. | Uso de 2,4-pirimidinadiaminas para el tratamiento de la aterosclerosis |
| EP2276747A1 (en) | 2008-03-11 | 2011-01-26 | Cellzome Limited | Sulfonamides as zap-70 inhibitors |
| US8205348B2 (en) | 2008-03-19 | 2012-06-26 | Zashiki-Warashi Manufacturing Inc. | Tile spacer and holder therefor |
| CL2009000600A1 (es) | 2008-03-20 | 2010-05-07 | Bayer Cropscience Ag | Uso de compuestos de diaminopirimidina como agentes fitosanitarios; compuestos de diaminopirimidina; su procedimiento de preparacion; agente que los contiene; procedimiento para la preparacion de dicho agente; y procedimiento para combatir plagas de animales y/u hongos dañinos patogenos de plantas. |
| DE102008018910A1 (de) * | 2008-04-14 | 2009-12-31 | Basf Coatings Ag | Verfahren zur Herstellung effektpigmenthaltiger Farbrezepturen |
| WO2009127642A2 (en) | 2008-04-15 | 2009-10-22 | Cellzome Limited | Use of lrrk2 inhibitors for neurodegenerative diseases |
| US8138339B2 (en) * | 2008-04-16 | 2012-03-20 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| KR20100132550A (ko) * | 2008-04-16 | 2010-12-17 | 포톨라 파마슈티컬스, 인코포레이티드 | ｓｙｋ 또는 ＪＡＫ 키나제 억제제로서의 ２,６－디아미노-피리미딘－５－일－카르복스아미드 |
| MX353206B (es) | 2008-04-16 | 2018-01-08 | Portola Pharmaceuticals Inc Star | 2,6-diamino-pirimidin-5-il-carboxamidas como inhibidores de syk o jak quinasas. |
| US8871753B2 (en) | 2008-04-24 | 2014-10-28 | Incyte Corporation | Macrocyclic compounds and their use as kinase inhibitors |
| PT2300013T (pt) | 2008-05-21 | 2017-10-31 | Ariad Pharma Inc | Derivados de fósforo como inibidores de cinases |
| EP2361248B1 (en) * | 2008-06-27 | 2018-09-19 | Celgene CAR LLC | Heteroaryl compounds and uses thereof |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| MX2011000661A (es) | 2008-07-16 | 2011-05-25 | Pharmacyclics Inc | Inhibidores de tirosina cinasa de bruton para el tratamiento de tumores solidos. |
| US20110245284A1 (en) | 2008-09-03 | 2011-10-06 | Bayer Cropscience Ag | Alkoxy- and Alkylthio-Substituted Anilinopyrimidines |
| US20110245156A1 (en) | 2008-12-09 | 2011-10-06 | Cytokine Pharmasciences, Inc. | Novel antiviral compounds, compositions, and methods of use |
| CA2965031C (en) | 2009-01-15 | 2018-12-04 | F. Hoffmann-La Roche Ag | Antibodies against phosphorylated tyrosines on erythropoietin receptor (epor) |
| US20120270237A9 (en) | 2009-04-03 | 2012-10-25 | Cellzone AG | Methods for the identification of kinase interacting molecules and for the purification of kinase proteins |
| 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 |
| EP3009428B1 (en) | 2009-05-08 | 2018-02-21 | Astellas Pharma Inc. | Diamino heterocyclic carboxamide compound |
| WO2010146132A1 (en) | 2009-06-18 | 2010-12-23 | Cellzome Limited | Sulfonamides and sulfamides as zap-70 inhibitors |
| US7741330B1 (en) | 2009-10-12 | 2010-06-22 | Pharmacyclics, Inc. | Pyrazolo-pyrimidine inhibitors of Bruton's tyrosine kinase |
| WO2011079231A1 (en) | 2009-12-23 | 2011-06-30 | Gatekeeper Pharmaceutical, Inc. | Compounds that modulate egfr activity and methods for treating or preventing conditions therewith |
| US20130137709A1 (en) | 2010-05-05 | 2013-05-30 | Nathanael S. Gray | Compounds that modulate EGFR activity and methods for treating or preventing conditions therewith |
| US20120071497A1 (en) | 2010-06-03 | 2012-03-22 | Pharmacyclics, Inc. | Methods of treating abc-dlbcl using inhibitors of bruton's tyrosine kinase |
| NZ604040A (en) | 2010-06-03 | 2015-02-27 | Pharmacyclics Inc | The use of inhibitors of bruton’s tyrosine kinase (btk) |
| WO2011153553A2 (en) | 2010-06-04 | 2011-12-08 | The Regents Of The University Of California | Methods and compositions for kinase inhibition |
| NZ607845A (en) | 2010-08-10 | 2015-03-27 | Celgene Avilomics Res Inc | Besylate salt of a btk inhibitor |
| US20130317029A1 (en) | 2010-11-01 | 2013-11-28 | Portola Pharmaceuticals, Inc. | Oxypyrimidines as syk modulators |
| EP2635285B1 (en) | 2010-11-01 | 2017-05-03 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| WO2012061299A1 (en) | 2010-11-01 | 2012-05-10 | Avila Therapeutics, Inc. | Heterocyclic compounds and uses thereof |
| US8796255B2 (en) | 2010-11-10 | 2014-08-05 | Celgene Avilomics Research, Inc | Mutant-selective EGFR inhibitors and uses thereof |
| CN102558149A (zh) | 2010-12-29 | 2012-07-11 | 中国医学科学院药物研究所 | 嘧啶衍生物、及其制法和药物组合物与用途 |
| EP2704572B1 (en) | 2011-05-04 | 2015-12-30 | Ariad Pharmaceuticals, Inc. | Compounds for inhibiting cell proliferation in egfr-driven cancers |
| DK2710007T3 (da) | 2011-05-17 | 2020-01-27 | Principia Biopharma Inc | Kinasehæmmere |
| EP2771010A4 (en) | 2011-10-19 | 2015-04-01 | Pharmacyclics Inc | USE OF BRUTON TYROSINE KINASE (BTK) INHIBITORS |
| 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 |
| MX356753B (es) | 2012-03-15 | 2018-06-12 | Celgene Avilomics Res Inc | Formas solidas de un inhibidor de cinasa del receptor del factor de crecimiento epidermico. |
| EA201590822A1 (ru) | 2012-11-02 | 2016-01-29 | Фармасайкликс, Инк. | Адъювантная терапия ингибитором киназы семейства tec |
| JP6800750B2 (ja) | 2013-08-02 | 2020-12-16 | ファーマサイクリックス エルエルシー | 固形腫瘍の処置方法 |
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2012
- 2012-06-04 IL IL220155A patent/IL220155B/en active IP Right Grant
- 2012-11-02 US US13/667,396 patent/US8710222B2/en active Active
-
2014
- 2014-04-16 US US14/253,903 patent/US9409921B2/en active Active
- 2014-11-11 IL IL235621A patent/IL235621A0/en unknown
-
2016
- 2016-02-01 JP JP2016017045A patent/JP2016117749A/ja not_active Ceased
- 2016-07-27 US US15/221,421 patent/US10010548B2/en active Active
-
2017
- 2017-02-02 AU AU2017200697A patent/AU2017200697A1/en not_active Abandoned
-
2018
- 2018-06-29 US US16/024,514 patent/US10596172B2/en active Active
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