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 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) | CN106146407A (enExample) |
| AU (2) | AU2010343055B2 (enExample) |
| BR (1) | BR112012018345B1 (enExample) |
| CA (1) | CA2783624C (enExample) |
| IL (2) | IL220155B (enExample) |
| MX (2) | MX2012007507A (enExample) |
| NZ (2) | NZ700236A (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 (320)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7989465B2 (en) * | 2007-10-19 | 2011-08-02 | Avila Therapeutics, Inc. | 4,6-disubstituted pyrimidines useful as kinase inhibitors |
| AU2008314632B2 (en) | 2007-10-19 | 2015-05-28 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
| KR101860057B1 (ko) | 2008-05-21 | 2018-05-21 | 어리어드 파마슈티칼스, 인코포레이티드 | 키나아제 억제제로서 포스포러스 유도체 |
| US11351168B1 (en) | 2008-06-27 | 2022-06-07 | Celgene Car Llc | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| EP2361248B1 (en) | 2008-06-27 | 2018-09-19 | Celgene CAR LLC | Heteroaryl compounds and uses thereof |
| KR101705158B1 (ko) | 2009-05-05 | 2017-02-09 | 다나-파버 캔서 인스티튜트 인크. | Ｅｇｆｒ 억제제 및 질환 치료방법 |
| 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 |
| CN102713618B (zh) | 2009-09-16 | 2015-07-15 | 新基阿维罗米克斯研究公司 | 蛋白激酶复合物和抑制剂 |
| US8466155B2 (en) * | 2009-10-02 | 2013-06-18 | Boehringer Ingelheim International Gmbh | Pyrimidines |
| 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 |
| MX2012013274A (es) | 2010-05-21 | 2013-05-28 | Chemilia Ab | Novedosos derivados de la pirimidina. |
| PT2576541T (pt) | 2010-06-04 | 2016-07-08 | Hoffmann La Roche | Derivados de aminopirimidina como moduladores de lrrk2 |
| EP2603081B1 (en) | 2010-08-10 | 2016-10-05 | Celgene Avilomics Research, Inc. | Besylate salt of a btk inhibitor |
| TWI545115B (zh) | 2010-11-01 | 2016-08-11 | 阿維拉製藥公司 | 雜環化合物及其用途 |
| US9238629B2 (en) | 2010-11-01 | 2016-01-19 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| WO2012064706A1 (en) * | 2010-11-10 | 2012-05-18 | Avila Therapeutics, Inc. | Mutant-selective egfr inhibitors and uses thereof |
| CA2812669C (en) | 2010-11-10 | 2018-11-06 | F. Hoffmann-La Roche Ag | Pyrazole aminopyrimidine derivatives as lrrk2 modulators |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| RU2013147417A (ru) | 2011-03-24 | 2015-04-27 | Кемилиа Аб | Новые производные пиримидина |
| ES2759615T3 (es) | 2011-04-01 | 2020-05-11 | Univ Utah Res Found | Análogos de N-fenilpirimidina-2-amina sustituidos como inhibidores de la quinasa AXL |
| JP6147727B2 (ja) | 2011-04-01 | 2017-06-14 | 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阻害剤としての置換ｎ−（３−（ピリミジン−４−イル）フェニル）アクリルアミド類似体 |
| KR101962488B1 (ko) | 2011-04-22 | 2019-03-26 | 시그날 파마소티칼 엘엘씨 | 치환된 디아미노카르복스아미드 및 디아미노카르보니트릴 피리미딘, 그의 조성물, 및 그를 사용하는 치료 방법 |
| PL2701510T3 (pl) | 2011-04-25 | 2017-07-31 | Usher Iii Initiative Inc | Pirazolopirydazyny oraz sposoby leczenia zwyrodnieniowych chorób siatkówki i utraty słuchu związanych z zespołem ushera |
| EP2704572B1 (en) | 2011-05-04 | 2015-12-30 | Ariad Pharmaceuticals, Inc. | Compounds for inhibiting cell proliferation in egfr-driven cancers |
| ES2791308T3 (es) | 2011-07-27 | 2020-11-03 | Astrazeneca Ab | Derivados de 2-(2,4,5-anilino sustituido)pirimidina como moduladores de EGFR útiles para tratar el cáncer |
| JP2014532060A (ja) | 2011-10-03 | 2014-12-04 | ザ・ユニヴァーシティ・オヴ・ノース・キャロライナ・アト・チャペル・ヒル | 癌を治療するためのピロロピリミジン化合物 |
| AR088570A1 (es) | 2011-10-28 | 2014-06-18 | Celgene Avilomics Res Inc | Metodos para tratar una enfermedad o trastorno relacionado con la tirosina quinasa de bruton |
| US9586965B2 (en) | 2012-01-13 | 2017-03-07 | Acea Biosciences Inc. | Pyrrolo[2,3-d]pyrimidine compounds as inhibitors of protein kinases |
| US10799504B2 (en) | 2012-01-13 | 2020-10-13 | ACEA Therapeutics, Inc. | Heterocyclic compounds and uses as anticancer agents |
| US9464089B2 (en) | 2012-01-13 | 2016-10-11 | Acea Biosciences Inc. | Heterocyclic compounds and uses thereof |
| US9034885B2 (en) | 2012-01-13 | 2015-05-19 | Acea Biosciences Inc. | EGFR modulators and uses thereof |
| EP2805940B1 (en) | 2012-01-17 | 2016-11-23 | Astellas Pharma Inc. | Pyrazine carboxamide compound |
| CN104302178B (zh) | 2012-03-15 | 2018-07-13 | 西建卡尔有限责任公司 | 表皮生长因子受体激酶抑制剂的固体形式 |
| PT2825042T (pt) | 2012-03-15 | 2018-11-16 | Celgene Car Llc | Sais de um inibidor de cinases do recetor do fator de crescimento epidérmico |
| US20150166591A1 (en) * | 2012-05-05 | 2015-06-18 | Ariad Pharmaceuticals, Inc. | Methods and compositions for raf kinase mediated diseases |
| US9133134B2 (en) | 2012-05-16 | 2015-09-15 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase |
| KR20150018789A (ko) | 2012-05-22 | 2015-02-24 | 더 유니버시티 오브 노쓰 캐롤라이나 엣 채플 힐 | 암의 치료를 위한 피리미딘 화합물 |
| HUE042374T2 (hu) | 2012-06-13 | 2019-06-28 | Incyte Holdings Corp | Szubsztituált triciklusos vegyületek mint FGFR inhibitorok |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| US20150216865A1 (en) * | 2012-09-04 | 2015-08-06 | Celgene Avilomics Research, Inc. | Methods of treating a bruton's tyrosine kinase disease or disorder |
| EP3680238A1 (en) * | 2012-10-04 | 2020-07-15 | University of Utah Research Foundation | Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors |
| CA2887465A1 (en) | 2012-10-04 | 2014-04-10 | University Of Utah Research Foundation | Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors |
| US9562047B2 (en) | 2012-10-17 | 2017-02-07 | The University Of North Carolina At Chapel Hill | Pyrazolopyrimidine compounds for the treatment of cancer |
| 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 |
| 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 |
| EP2922827A4 (en) * | 2012-11-20 | 2016-06-08 | Celgene Avilomics Res Inc | METHOD FOR THE TREATMENT OF A DISEASE OR DISEASE RELATED TO BRUTON 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 |
| EP2922546A4 (en) * | 2012-11-20 | 2016-06-08 | Celgene Avilomics Res Inc | METHOD FOR THE TREATMENT OF A DISEASE OR DISEASE RELATED TO BRUTON TYROSINE KINASE |
| 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 |
| US9771330B2 (en) | 2012-11-27 | 2017-09-26 | 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 |
| WO2014100748A1 (en) * | 2012-12-21 | 2014-06-26 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| US20140213555A1 (en) * | 2013-01-25 | 2014-07-31 | Rigel Pharmaceuticals, Inc. | Compounds and method for treating autoimmune diseases |
| KR20150119012A (ko) * | 2013-02-08 | 2015-10-23 | 셀진 아빌로믹스 리서치, 인코포레이티드 | Erk 억제제 및 이의 용도 |
| WO2014130856A2 (en) * | 2013-02-21 | 2014-08-28 | Wayne Rothbaum | Treatment of skeletal-related disorders |
| WO2014134391A1 (en) | 2013-02-28 | 2014-09-04 | Bristol-Myers Squibb Company | Phenylpyrazole derivatives as potent rock1 and rock2 inhibitors |
| TW201444798A (zh) | 2013-02-28 | 2014-12-01 | 必治妥美雅史谷比公司 | 作爲強效ｒｏｃｋ１及ｒｏｃｋ２抑制劑之苯基吡唑衍生物 |
| BR112015022993B1 (pt) | 2013-03-14 | 2021-12-14 | Sumitomo Dainippon Pharma Oncology, Inc. | Inibidores de jak2 e alk2, composição farmacêutica compreendendo os referidos inibidores e uso destes |
| EP2970190A1 (en) | 2013-03-14 | 2016-01-20 | Respivert Limited | Kinase inhibitors |
| US9611283B1 (en) | 2013-04-10 | 2017-04-04 | Ariad Pharmaceuticals, Inc. | Methods for inhibiting cell proliferation in ALK-driven cancers |
| HUE036571T2 (hu) | 2013-04-19 | 2018-07-30 | Incyte Holdings Corp | Biciklusos heterociklusok mint FGFR inhibitorok |
| LT2989106T (lt) | 2013-04-25 | 2017-04-10 | Beigene, Ltd. | Kondensuoti heterocikliniai junginiai kaip baltymų kinazės inhibitoriai |
| 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 |
| RS58273B1 (sr) | 2013-06-26 | 2019-03-29 | Abbvie Inc | Primarni karboksamidi kao btk inhibitori |
| 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 |
| ES2761572T3 (es) * | 2013-07-11 | 2020-05-20 | Acea Therapeutics Inc | Derivados de pirimidina como inhibidores de quinasa |
| KR101828187B1 (ko) | 2013-08-12 | 2018-02-09 | 다이호야쿠힌고교 가부시키가이샤 | 신규 축합 피리미딘 화합물 또는 그 염 |
| 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 |
| EA034666B1 (ru) | 2013-09-13 | 2020-03-04 | Бейджин Свитзерланд Гмбх | Антитело против pd-1 и его применение для лечения рака или вирусной инфекции и фрагмент антитела |
| CN104262328B (zh) * | 2013-09-18 | 2016-09-07 | 北京韩美药品有限公司 | 抑制btk和/或jak3激酶活性的化合物 |
| HRP20191430T1 (hr) | 2013-10-21 | 2019-11-01 | Merck Patent Gmbh | Spojevi heteroarila kao inhibitori btk i njihove uporabe |
| KR102671643B1 (ko) | 2013-10-25 | 2024-05-31 | 파마싸이클릭스 엘엘씨 | 이식편 대 숙주 질환의 치료 및 예방 방법 |
| 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 |
| US11039620B2 (en) | 2014-02-19 | 2021-06-22 | 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 |
| US9622483B2 (en) | 2014-02-19 | 2017-04-18 | 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 |
| WO2015131080A1 (en) | 2014-02-28 | 2015-09-03 | Nimbus Lakshmi, Inc. | Tyk2 inhibitors and uses thereof |
| 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 |
| JP6321821B2 (ja) | 2014-04-14 | 2018-05-09 | シャンハイ ハイヤン ファーマシューティカル テクノロジー カンパニー リミテッドＳｈａｎｇｈａｉ Ｈａｉｙａｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌ Ｔｅｃｈｎｏｌｏｇｙ Ｃｏ．， Ｌｔｄ． | ２，３，４，６−４置換ベンゼン−１，５−ジアミン誘導体、その製造方法および医薬品における使用 |
| US20150297605A1 (en) * | 2014-04-16 | 2015-10-22 | Signal Pharmaceuticals, Llc | Methods for treating cancer using tor kinase inhibitor combination therapy |
| 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 |
| KR102130600B1 (ko) | 2014-07-03 | 2020-07-08 | 베이진 엘티디 | Pd-l1 항체와 이를 이용한 치료 및 진단 |
| 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 |
| MY195016A (en) | 2014-08-04 | 2023-01-03 | Nuevolution As | Optionally Fused Heterocyclyl-Substituted Derivatives of Pyrimidine Useful for The Treatment of Inflammatory, Metabolic, Oncologic and Autoimmune Diseases |
| EP4578865A3 (en) | 2014-08-12 | 2025-07-30 | Monash University | Lymph directing prodrugs |
| TW201613892A (en) | 2014-08-13 | 2016-04-16 | Celgene Avilomics Res Inc | Forms and compositions of an ERK inhibitor |
| EP4070795A1 (en) * | 2014-08-25 | 2022-10-12 | Salk Institute for Biological Studies | Novel ulk1 inhibitors and methods using same |
| 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 |
| SMT202100311T1 (it) | 2014-09-17 | 2021-07-12 | Celgene Car Llc | Inibitori di mk2 e loro usi |
| AU2015330506B2 (en) * | 2014-10-11 | 2020-01-30 | Jiangsu Hansoh Pharmaceutical Group Co., Ltd. | EGFR inhibitor, and preparation and application thereof |
| WO2016060963A1 (en) | 2014-10-14 | 2016-04-21 | Sunshine Lake Pharma Co., Ltd. | Substituted heteroaryl compounds and methods of use |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| DK3215518T3 (da) | 2014-10-29 | 2021-05-25 | Bicyclerd Ltd | Bicykliske peptidligander, der er specifikke 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 |
| CN107209186A (zh) | 2014-12-11 | 2017-09-26 | 默克专利有限公司 | Btk抑制剂的测定 |
| ES2877642T3 (es) | 2014-12-16 | 2021-11-17 | Signal Pharm Llc | Formulaciones de 2-(terc-butilamino)-4-((1R,3R,4R)-3-hidroxi-4-metilciclohexilamino)-pirimidin-5-carboxamida |
| ES2882954T3 (es) | 2014-12-16 | 2021-12-03 | Signal Pharm Llc | Usos médicos que comprenden métodos para la medición de la inhibición de la quinasa c-Jun N-terminal en la piel |
| US20180022710A1 (en) | 2015-01-29 | 2018-01-25 | 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 |
| KR101858421B1 (ko) * | 2015-01-30 | 2018-05-15 | 다이호야쿠힌고교 가부시키가이샤 | 면역 질환의 예방 및/또는 치료제 |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MX388991B (es) | 2015-02-20 | 2025-03-20 | Incyte Corp | Heterociclos biciclicos como inhibidores de receptores del factor de crecimiento fibroblastico (fgfr) |
| WO2016138352A1 (en) | 2015-02-27 | 2016-09-01 | Nimbus Lakshmi, Inc. | Tyk2 inhibitors and uses thereof |
| WO2017004134A1 (en) | 2015-06-29 | 2017-01-05 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| CN108137559B (zh) * | 2015-07-09 | 2021-11-02 | 默克专利有限公司 | 用作btk抑制剂的嘧啶衍生物及其用途 |
| WO2017019487A1 (en) | 2015-07-24 | 2017-02-02 | Celgene Corporation | Methods of synthesis of (1r,2r,5r)-5-amino-2-methylcyclohexanol hydrochloride and intermediates useful therein |
| US20170209462A1 (en) | 2015-08-31 | 2017-07-27 | Pharmacyclics Llc | Btk inhibitor combinations for treating multiple myeloma |
| TWI707852B (zh) | 2015-09-02 | 2020-10-21 | 美商林伯士拉克許米公司 | Tyk2 抑制劑及其用途 |
| WO2017041139A1 (en) | 2015-09-08 | 2017-03-16 | Monash University | Lymph directing prodrugs |
| WO2017044720A1 (en) | 2015-09-11 | 2017-03-16 | Navitor Pharmaceuticals, Inc. | Rapamycin analogs and uses thereof |
| WO2017046604A1 (en) | 2015-09-16 | 2017-03-23 | Redx Pharma Plc | 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 |
| KR20180067584A (ko) | 2015-10-09 | 2018-06-20 | 아세아 테라퓨틱스 인코포레이티드 | 피롤로피리미딘 키나아제 억제제의 약학적 염, 물리적 형태 및 조성물, 및 이들의 제조 방법 |
| LT3365334T (lt) * | 2015-10-21 | 2024-09-10 | Otsuka Pharmaceutical Co., Ltd. | Benzolaktamo junginiai kaip baltymų kinazės inhibitoriai |
| MX389001B (es) | 2015-10-23 | 2025-03-20 | Navitor Pharm Inc | Moduladores de 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 |
| MA55064A (fr) | 2015-12-16 | 2021-09-29 | Loxo Oncology Inc | Composés utilisés comme inhibiteurs de kinase |
| 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 |
| HRP20211220T1 (hr) | 2016-03-09 | 2021-10-29 | Raze Therapeutics Inc. | Inhibitori 3-fosfoglicerat dehidrogenaze i njihova upotreba |
| 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 |
| CN109153722A (zh) | 2016-04-08 | 2019-01-04 | X4 制药有限公司 | 用于治疗癌症的方法 |
| 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 |
| EP3471726A4 (en) | 2016-06-21 | 2019-10-09 | X4 Pharmaceuticals, Inc. | CXCR4 INHIBITORS AND USES THEREOF |
| WO2017223243A1 (en) | 2016-06-21 | 2017-12-28 | X4 Pharmaceuticals, Inc. | Cxcr4 inhibitors and uses thereof |
| JP7054529B2 (ja) | 2016-06-21 | 2022-04-14 | エックス４ ファーマシューティカルズ， インコーポレイテッド | Ｃｘｃｒ４阻害剤およびその使用 |
| 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 |
| TWI865873B (zh) | 2016-08-16 | 2024-12-11 | 瑞士商百濟神州瑞士有限責任公司 | (s)-7-(1-丙烯醯基六氫吡啶-4-基)-2-(4-苯氧基苯基)-4,5,6,7-四氫吡唑並[1,5-a]嘧啶-3-甲醯胺的晶型、其製備和用途 |
| FI3500299T3 (fi) | 2016-08-19 | 2024-02-14 | Beigene Switzerland Gmbh | Tsanubrutinibin yhdistelmä cd20-tai pd-1-vasta-aineen kanssa käytettäväksi syövän hoidossa |
| 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 |
| EP3515414B1 (en) | 2016-09-19 | 2022-11-30 | MEI Pharma, Inc. | Combination therapy |
| WO2018071794A1 (en) | 2016-10-14 | 2018-04-19 | Nimbus Lakshmi, Inc. | Tyk2 inhibitors and uses thereof |
| EP3528816A4 (en) | 2016-10-21 | 2020-04-08 | 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 |
| CN110139669A (zh) | 2016-11-03 | 2019-08-16 | 朱诺治疗学股份有限公司 | T细胞疗法和btk抑制剂的组合疗法 |
| EP3538091A4 (en) | 2016-11-08 | 2020-06-10 | Navitor Pharmaceuticals, Inc. | PHENYL AMINO PIPERIDINE MTORC INHIBITORS AND USES THEREOF |
| CN110177544A (zh) | 2016-11-29 | 2019-08-27 | 普尔泰克健康有限公司 | 用于递送治疗剂的外泌体 |
| US11091451B2 (en) | 2016-12-05 | 2021-08-17 | Raze Therapeutics, Inc. | SHMT inhibitors and uses thereof |
| EP3559018A1 (en) | 2016-12-23 | 2019-10-30 | Bicyclerd Limited | Peptide derivatives having novel linkage structures |
| 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 |
| EP3565638B8 (en) | 2017-01-06 | 2024-04-10 | BicycleRD Limited | Bicycle conjugate 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 |
| EP3573989A4 (en) | 2017-01-25 | 2020-11-18 | Beigene, Ltd. | CRYSTALLINE FORMS OF (S) -7- (1- (BUT-2-YNOYL) PIPERIDIN-4-YL) -2- (4-PHENOXYPHENYL) -4, 5, 6, 7-TETRAHY DROPYRAZOLO [1, 5-A ] PYRIMIDINE-3-CARBOXAMIDE, PREPARATION AND ASSOCIATED USES |
| 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 |
| EP4338802A3 (en) | 2017-03-08 | 2024-09-04 | Takeda Pharmaceutical Company Limited | Tyk2 inhibitors, uses, and methods for production thereof |
| EP3375784A1 (en) | 2017-03-14 | 2018-09-19 | Artax Biopharma Inc. | Aza-dihydro-acridone derivatives |
| EP3375778A1 (en) | 2017-03-14 | 2018-09-19 | Artax Biopharma Inc. | Aryl-piperidine 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 |
| EP3615550A1 (en) | 2017-04-27 | 2020-03-04 | 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 |
| BR112019027402A2 (pt) | 2017-06-22 | 2020-07-07 | Celgene Corporation | tratamento de carcinoma hepatocelular caracterizado por infecção pelo vírus da hepatite b |
| EP3645549A1 (en) | 2017-06-26 | 2020-05-06 | BicycleRD Limited | Bicyclic peptide ligands with detectable moieties and uses thereof |
| US11597768B2 (en) | 2017-06-26 | 2023-03-07 | Beigene, Ltd. | Immunotherapy for hepatocellular carcinoma |
| ES2994013T3 (en) | 2017-07-28 | 2025-01-15 | Takeda Pharmaceuticals Co | Tyk2 inhibitors and uses thereof |
| JP7670481B2 (ja) | 2017-08-04 | 2025-04-30 | バイスクルテクス・リミテッド | Ｃｄ１３７に対して特異的な二環式ペプチドリガンド |
| 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 |
| US20200283482A1 (en) | 2017-08-14 | 2020-09-10 | Bicyclerd Limited | Bicyclic peptide ligand prr-a conjugates and uses thereof |
| KR20200041954A (ko) * | 2017-08-18 | 2020-04-22 | 북경한미약품 유한공사 | 화합물, 이의 약제학적 조성물, 및 이의 용도 및 응용 |
| EP3675838A4 (en) | 2017-08-29 | 2021-04-21 | PureTech LYT, Inc. | LIPID PRODRUGS DIRECTED TO THE LYMPHATIC SYSTEM |
| US11883497B2 (en) | 2017-08-29 | 2024-01-30 | Puretech Lyt, Inc. | Lymphatic system-directing lipid prodrugs |
| 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 |
| WO2019060693A1 (en) | 2017-09-22 | 2019-03-28 | Kymera Therapeutics, Inc. | CRBN LIGANDS AND USES THEREOF |
| AU2018338314B2 (en) | 2017-09-22 | 2024-12-12 | Kymera Therapeutics, Inc | Protein degraders and uses thereof |
| EP3707138B1 (en) | 2017-11-06 | 2022-07-13 | Bristol-Myers Squibb Company | Isofuranone compounds useful as hpk1 inhibitors |
| WO2019099311A1 (en) | 2017-11-19 | 2019-05-23 | Sunshine Lake Pharma Co., Ltd. | Substituted heteroaryl compounds and methods of use |
| US11786529B2 (en) | 2017-11-29 | 2023-10-17 | Beigene Switzerland Gmbh | Treatment of indolent or aggressive B-cell lymphomas using a combination comprising BTK inhibitors |
| US11304954B2 (en) | 2017-12-19 | 2022-04-19 | Puretech Lyt, Inc. | Lipid prodrugs of mycophenolic acid 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 |
| EP3727362A4 (en) | 2017-12-19 | 2021-10-06 | PureTech LYT, Inc. | MYCOPHENOLIC ACID LIPID PRODRUGS AND THEIR USES |
| 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 |
| 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 |
| EP3737666A4 (en) | 2018-01-12 | 2022-01-05 | Kymera Therapeutics, Inc. | PROTEIN DEGRADATION AGENTS AND ASSOCIATED USES |
| CN111867581B (zh) | 2018-01-29 | 2023-12-26 | 默克专利股份有限公司 | Gcn2抑制剂及其用途 |
| EP4616913A3 (en) | 2018-01-29 | 2025-12-10 | 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 |
| CA3091775A1 (en) | 2018-02-23 | 2019-08-29 | Bicycletx Limited | Multimeric bicyclic peptide ligands |
| JP7317032B2 (ja) | 2018-02-27 | 2023-07-28 | アルタックス バイオファーマ インコーポレイテッド | Ｔｃｒ－ｎｃｋ相互作用の阻害剤としてのクロメン誘導体 |
| EP3773591A4 (en) | 2018-04-05 | 2021-12-22 | Sumitomo Dainippon Pharma Oncology, Inc. | AXL KINASE INHIBITORS AND THEIR USE |
| AU2019257651B2 (en) | 2018-04-24 | 2023-05-25 | Vertex Pharmaceuticals Incorporated | Pteridinone compounds and uses thereof |
| AU2019261308B2 (en) | 2018-04-24 | 2022-09-08 | Merck Patent Gmbh | Antiproliferation compounds and uses thereof |
| EP3784664B1 (en) | 2018-04-26 | 2025-02-19 | Pfizer Inc. | 2-amino-pyridine or 2-amino-pyrimidine derivatives as cyclin dependent kinase inhibitors |
| CN112584902A (zh) | 2018-05-03 | 2021-03-30 | 朱诺治疗学股份有限公司 | 嵌合抗原受体（car）t细胞疗法和激酶抑制剂的组合疗法 |
| EP3788047B1 (en) | 2018-05-04 | 2024-09-04 | Incyte Corporation | Solid forms of an fgfr inhibitor and processes for preparing the same |
| BR112020022373A2 (pt) | 2018-05-04 | 2021-02-02 | Incyte Corporation | sais de um inibidor de fgfr |
| PL3813946T3 (pl) | 2018-06-15 | 2024-09-02 | Janssen Pharmaceutica Nv | Analogi rapamycyny i ich zastosowania |
| US11180531B2 (en) | 2018-06-22 | 2021-11-23 | Bicycletx Limited | Bicyclic peptide ligands specific for Nectin-4 |
| GB201810316D0 (en) | 2018-06-22 | 2018-08-08 | Bicyclerd Ltd | Peptide ligands for binding to EphA2 |
| EP3817748A4 (en) | 2018-07-06 | 2022-08-24 | Kymera Therapeutics, Inc. | TRICYCLIC CRBN LIGANDS AND USES THEREOF |
| WO2020010227A1 (en) | 2018-07-06 | 2020-01-09 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| US11040038B2 (en) | 2018-07-26 | 2021-06-22 | Sumitomo Dainippon Pharma Oncology, Inc. | Methods for treating diseases associated with abnormal ACVR1 expression and ACVR1 inhibitors for use in the same |
| US10548889B1 (en) | 2018-08-31 | 2020-02-04 | X4 Pharmaceuticals, Inc. | Compositions of CXCR4 inhibitors and methods of preparation and use |
| WO2020051424A1 (en) | 2018-09-07 | 2020-03-12 | Pic Therapeutics | Eif4e inhibitors and uses thereof |
| US11066404B2 (en) | 2018-10-11 | 2021-07-20 | Incyte Corporation | Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors |
| US11414431B2 (en) | 2018-10-15 | 2022-08-16 | Nimbus Lakshmi, Inc. | Substituted pyrazolo[1,5-a]pyrimidines as TYK2 inhibitors |
| EP3870597A1 (en) | 2018-10-23 | 2021-09-01 | 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 |
| SG11202105424PA (en) | 2018-11-30 | 2021-06-29 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
| CN113271938A (zh) | 2018-11-30 | 2021-08-17 | 林伯士拉克许米公司 | Tyk2抑制剂和其用途 |
| 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 |
| US11174264B2 (en) | 2019-01-23 | 2021-11-16 | Nimbus Lakshmi, Inc. | 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 |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | 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 |
| KR20210144844A (ko) | 2019-03-29 | 2021-11-30 | 아스트라제네카 아베 | 비-소세포 폐암의 치료에 사용하기 위한 오시머티닙 |
| 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 |
| KR20220006139A (ko) | 2019-04-05 | 2022-01-14 | 카이메라 쎄라퓨틱스 인코포레이티드 | Stat 분해제 및 이의 용도 |
| WO2020223558A1 (en) | 2019-05-01 | 2020-11-05 | Incyte Corporation | Tricyclic amine compounds as cdk2 inhibitors |
| 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 |
| SI3966206T1 (sl) | 2019-05-10 | 2023-12-29 | Deciphera Pharmaceuticals, Llc | Heteroarilaminopirimidinski amidni zaviralci avtofagije in načini njihove uporabe |
| HRP20231730T1 (hr) | 2019-05-10 | 2024-05-10 | Deciphera Pharmaceuticals, Llc | Fenilaminopirimidin amidni inhibitori autofagije i postupci njihove primjene |
| CN114502540A (zh) | 2019-05-31 | 2022-05-13 | 医肯纳肿瘤学公司 | Tead抑制剂和其用途 |
| 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 |
| US12521438B2 (en) | 2019-06-10 | 2026-01-13 | Kymera Therapeutics, Inc. | SMARCA degraders and uses thereof |
| CA3143489A1 (en) | 2019-06-17 | 2020-12-24 | 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 |
| TW202115024A (zh) | 2019-08-14 | 2021-04-16 | 美商英塞特公司 | 作為cdk2 抑制劑之咪唑基嘧啶基胺化合物 |
| JP2022548594A (ja) | 2019-09-11 | 2022-11-21 | ビンシア・バイオサイエンシーズ・インコーポレイテッド | Ｕｓｐ３０阻害剤及びその使用 |
| CA3150108A1 (en) | 2019-09-13 | 2021-03-18 | Neelu Kaila | 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 |
| KR20220100879A (ko) | 2019-10-14 | 2022-07-18 | 인사이트 코포레이션 | Fgfr 저해제로서의 이환식 헤테로사이클 |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| TW202120092A (zh) * | 2019-11-08 | 2021-06-01 | 大陸商深圳微芯生物科技股份有限公司 | 化合物用於預防或治療移植物抗宿主病的用途 |
| JP2023503385A (ja) * | 2019-11-26 | 2023-01-27 | シェンチェン チップスクリーン バイオサイエンシズ カンパニー、リミテッド | 非晶質形態の芳香族複素環式化合物を含む組成物、並びにその調製方法及びその使用 |
| WO2021113479A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| KR20220131900A (ko) | 2019-12-04 | 2022-09-29 | 인사이트 코포레이션 | Fgfr 억제제의 유도체 |
| KR20220128345A (ko) | 2019-12-05 | 2022-09-20 | 아나쿠리아 테라퓨틱스, 인코포레이티드 | 라파마이신 유사체 및 이의 용도 |
| JP2023509366A (ja) | 2019-12-17 | 2023-03-08 | カイメラ セラピューティクス， インコーポレイテッド | Ｉｒａｋ分解剤およびそれらの使用 |
| WO2021127283A2 (en) | 2019-12-17 | 2021-06-24 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| TWI872177B (zh) | 2019-12-20 | 2025-02-11 | 丹麥商紐韋盧森公司 | 對核受體具有活性之化合物 |
| US11447479B2 (en) | 2019-12-20 | 2022-09-20 | Nuevolution A/S | Compounds active towards nuclear receptors |
| PH12022551522A1 (en) | 2019-12-23 | 2024-01-29 | Kymera Therapeutics Inc | Smarca degraders and uses thereof |
| WO2021138391A1 (en) | 2019-12-30 | 2021-07-08 | Tyra Biosciences, Inc. | Indazole compounds |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | 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 |
| IL295362A (en) | 2020-02-05 | 2022-10-01 | Puretech Lyt Inc | Lipid prodrugs of neurosteroids |
| EP4114529A1 (en) | 2020-03-03 | 2023-01-11 | PIC Therapeutics, Inc. | Eif4e inhibitors and uses thereof |
| PH12022552458A1 (en) | 2020-03-19 | 2024-01-22 | Kymera Therapeutics Inc | Mdm2 degraders and uses thereof |
| US11613532B2 (en) | 2020-03-31 | 2023-03-28 | Nuevolution A/S | Compounds active towards nuclear receptors |
| MX2022012260A (es) | 2020-03-31 | 2022-11-30 | Nuevolution As | Compuestos activos frente a receptores nucleares. |
| TW202204331A (zh) | 2020-04-07 | 2022-02-01 | 美商米突倍基公司 | Cd38抑制劑 |
| 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 |
| US20230257350A1 (en) * | 2020-07-02 | 2023-08-17 | 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 |
| WO2022063106A1 (en) * | 2020-09-22 | 2022-03-31 | Beigene, Ltd. | Indoline compounds and derivatives as egfr inhibitors |
| WO2022072632A1 (en) * | 2020-09-30 | 2022-04-07 | Scorpion Therapeutics, Inc. | Bicyclic compounds for use in the treatment cancer |
| US12331046B2 (en) | 2020-10-23 | 2025-06-17 | Nimbus Clotho, Inc. | CTPS1 inhibitors and uses thereof |
| WO2022120353A1 (en) | 2020-12-02 | 2022-06-09 | Ikena Oncology, Inc. | Tead inhibitors and uses thereof |
| KR20230131189A (ko) | 2020-12-02 | 2023-09-12 | 이케나 온콜로지, 인코포레이티드 | Tead 억제제 및 이의 용도 |
| MX2023007852A (es) | 2020-12-30 | 2023-07-07 | Kymera Therapeutics Inc | Degradadores de cinasas asociadas al receptor de interleucina-1 (irak) y usos de los mismos. |
| MX2023009059A (es) | 2021-02-02 | 2023-09-15 | Liminal Biosciences Ltd | Antagonistas de gpr84 y usos de estos. |
| KR20230153387A (ko) | 2021-02-02 | 2023-11-06 | 리미널 바이오사이언시스 리미티드 | Gpr84 길항제 및 이의 용도 |
| CN117120090A (zh) | 2021-02-12 | 2023-11-24 | 林伯士萨顿公司 | Hpk1拮抗剂和其用途 |
| IL304905A (en) | 2021-02-15 | 2023-10-01 | Kymera Therapeutics Inc | IRAK4 joints and their uses |
| WO2022174268A1 (en) | 2021-02-15 | 2022-08-18 | Kymera Therapeutics, Inc. | Irak4 degraders and uses thereof |
| CN117295737A (zh) | 2021-03-05 | 2023-12-26 | 林伯士萨顿公司 | Hpk1拮抗剂和其用途 |
| WO2022213062A1 (en) | 2021-03-29 | 2022-10-06 | Nimbus Saturn, Inc. | Hpk1 antagonists and uses thereof |
| 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 |
| US20240216330A1 (en) | 2021-04-02 | 2024-07-04 | Biogen Ma Inc. | Combination treatment methods of multiple sclerosis |
| KR20240007155A (ko) | 2021-04-09 | 2024-01-16 | 님버스 클리오, 인코포레이티드 | Cbl-b 조절제 및 이의 용도 |
| WO2022221170A1 (en) | 2021-04-12 | 2022-10-20 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| JP2024514879A (ja) | 2021-04-16 | 2024-04-03 | イケナ オンコロジー， インコーポレイテッド | Ｍｅｋ阻害剤及びその使用 |
| AU2022271290A1 (en) | 2021-05-07 | 2023-11-23 | Kymera Therapeutics, Inc. | Cdk2 degraders and uses thereof |
| EP4352060A1 (en) | 2021-06-09 | 2024-04-17 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| TW202313611A (zh) | 2021-06-09 | 2023-04-01 | 美商英塞特公司 | 作為ｆｇｆｒ抑制劑之三環雜環 |
| 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 |
| IL314437A (en) | 2022-01-31 | 2024-09-01 | Kymera Therapeutics Inc | IRAK joints and their uses |
| 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 |
| WO2023230205A1 (en) | 2022-05-25 | 2023-11-30 | 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 |
| IL318577A (en) | 2022-08-02 | 2025-03-01 | Liminal Biosciences Ltd | ARYL-TRIAZOLYL AND RELATED GPR84 ANTAGONISTS AND THEIR USES |
| 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 |
| TW202416950A (zh) | 2022-08-02 | 2024-05-01 | 英商利米那生物科技有限公司 | 雜芳基甲醯胺及相關gpr84拮抗劑及其用途 |
| 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 |
| WO2024112894A1 (en) | 2022-11-22 | 2024-05-30 | PIC Therapeutics, Inc. | Eif4e inhibitors and uses thereof |
| WO2024264017A2 (en) | 2023-06-23 | 2024-12-26 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| WO2025062372A1 (en) | 2023-09-21 | 2025-03-27 | Takeda Pharmaceutical Company Limited | Tyk2 inhibitors for use in the treatment of inflammatory bowel disease |
| 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 |
| 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 |
| 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 |
| 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 |
| EP0813525B9 (en) | 1995-03-10 | 2004-02-04 | Berlex Laboratories, Inc. | Benzamidine derivatives their preparation and their use as anti-coagulants |
| 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 |
| ATE401312T1 (de) | 1997-12-15 | 2008-08-15 | Astellas Pharma Inc | Pyrimidin-5-carboxamid-derivate |
| US6303652B1 (en) | 1998-08-21 | 2001-10-16 | Hughes Institute | BTK inhibitors and methods for their identification and use |
| ATE342892T1 (de) | 1998-08-29 | 2006-11-15 | Astrazeneca Ab | Pyrimidine verbindungen |
| PL204427B1 (pl) | 1998-11-10 | 2010-01-29 | Janssen Pharmaceutica Nv | Hamująca replikację wirusa HIV pochodna pirymidyny, sposób jej wytwarzania i zastosowanie oraz kompozycja farmaceutyczna |
| 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 |
| EP1150955A2 (en) | 1999-02-04 | 2001-11-07 | 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 |
| HRP20010969B1 (en) | 1999-06-29 | 2005-04-30 | Egis Gy�Gyszergy�R Rt. | Novel piperazinylalkylthiopyrimidine derivatives, |
| EP1246823A1 (en) | 1999-12-28 | 2002-10-09 | Pharmacopeia, Inc. | Pyrimidine and triazine kinase inhibitors |
| WO2001060816A1 (en) | 2000-02-17 | 2001-08-23 | Amgen Inc. | Kinase inhibitors |
| GB0004887D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| GB0004888D0 (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 |
| US7427689B2 (en) | 2000-07-28 | 2008-09-23 | Georgetown University | 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 |
| JP2005507423A (ja) | 2001-11-01 | 2005-03-17 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | グリコーゲン合成酵素キナーゼ３ベータ阻害剤（ｇｓｋ３阻害剤）としてのヘテロアリールアミン |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| JP2005522438A (ja) | 2002-02-08 | 2005-07-28 | スミスクライン ビーチャム コーポレーション | ピリミジン化合物 |
| GB0206215D0 (en) | 2002-03-15 | 2002-05-01 | Novartis Ag | Organic compounds |
| JP2005534286A (ja) | 2002-03-21 | 2005-11-17 | サネシス ファーマシューティカルズ， インコーポレイテッド | キナーゼインヒビターの同定 |
| US20040002395A1 (en) * | 2002-06-27 | 2004-01-01 | Poynor Raymond L. | Bridge weight for metal wood golf club |
| JP2006514989A (ja) | 2002-07-29 | 2006-05-18 | ライジェル ファーマシューティカルズ | ２，４−ピリミジンジアミン化合物による自己免疫疾患の治療および予防方法 |
| 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 |
| JP5602333B2 (ja) | 2003-02-07 | 2014-10-08 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | Ｈｉｖ感染の予防のためのピリミジン誘導体 |
| EP1597251B1 (en) | 2003-02-20 | 2009-06-10 | SmithKline Beecham Corporation | Pyrimidine compounds |
| 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 |
| KR20120062863A (ko) | 2003-07-30 | 2012-06-14 | 리겔 파마슈티칼스, 인크. | 자가면역 질환의 치료 또는 예방에 사용하기 위한 2,4-피리미딘디아민 화합물 |
| SI1663242T1 (sl) | 2003-08-07 | 2011-09-30 | Rigel Pharmaceuticals Inc | 2,4-pirimidindiaminske spojine in uporabe kot antiproliferativna sredstva |
| PL2287156T3 (pl) * | 2003-08-15 | 2013-11-29 | Novartis Ag | 2,4-Di(fenyloamino)-pirymidyny stosowane w leczeniu chorób nowotworowych, chorób zapalnych i zaburzeń układu immunologicznego |
| GB0321710D0 (en) * | 2003-09-16 | 2003-10-15 | Novartis Ag | Organic compounds |
| EP1663992A1 (en) | 2003-09-18 | 2006-06-07 | 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 |
| ES2389203T3 (es) | 2004-01-12 | 2012-10-24 | Ym Biosciences Australia Pty Ltd | Inhibidores de quinasa selectivos |
| WO2005070890A2 (en) | 2004-01-16 | 2005-08-04 | Wyeth | Quinoline intermediates of receptor tyrosine kinase inhibitors and the synthesis thereof |
| CA2557794A1 (en) | 2004-03-15 | 2005-10-06 | Eli Lilly And Company | Opioid receptor antagonists |
| US7558717B2 (en) | 2004-04-28 | 2009-07-07 | Vertex Pharmaceuticals Incorporated | Crystal structure of human JAK3 kinase domain complex and binding pockets thereof |
| CA2566531A1 (en) | 2004-05-18 | 2005-12-15 | Rigel Pharmaceuticals, Inc. | Cycloalkyl substituted pyrimidinediamine compounds and their uses |
| EP1598343A1 (de) | 2004-05-19 | 2005-11-23 | Boehringer Ingelheim International GmbH | 2-Arylaminopyrimidine als PLK Inhibitoren |
| ES2564127T5 (es) | 2004-06-04 | 2020-03-26 | Genentech Inc | Mutaciones en EGFR |
| 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 |
| US7622486B2 (en) | 2004-09-23 | 2009-11-24 | Reddy Us Therapeutics, Inc. | Pyridine compounds, process for their preparation and compositions containing them |
| EP1797048B1 (en) | 2004-09-30 | 2011-08-17 | Tibotec Pharmaceuticals | Hiv inhibiting 5-carbo- or heterocyclic substituted pyrimidines |
| WO2006044457A1 (en) | 2004-10-13 | 2006-04-27 | Wyeth | N-benzenesulfonyl substituted anilino-pyrimidine analogs |
| EP2100899A3 (en) | 2004-10-20 | 2009-09-30 | Proteolix, Inc. | Compounds for proteasome enzyme inhibition |
| WO2006053109A1 (en) | 2004-11-10 | 2006-05-18 | 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 |
| WO2006068770A1 (en) | 2004-11-24 | 2006-06-29 | Rigel Pharmaceuticals, Inc. | Spiro-2, 4-pyrimidinediamine compounds and their uses |
| MY169441A (en) | 2004-12-08 | 2019-04-11 | Janssen Pharmaceutica Nv | 2,4, (4,6) pyrimidine derivatives |
| JP5208516B2 (ja) * | 2004-12-30 | 2013-06-12 | エグゼリクシス， インコーポレイテッド | キナーゼモジュレーターとしてのピリミジン誘導体および使用方法 |
| AU2006204724A1 (en) | 2005-01-14 | 2006-07-20 | Millennium Pharmaceuticals, Inc. | Cinnamide and hydrocinnamide derivatives with raf-kinase inhibitory activity |
| DK1856135T3 (da) | 2005-01-19 | 2010-04-12 | Rigel Pharmaceuticals Inc | Prodrugs af 2,4-pyrimidindiamin-forbindelser og deres anvendelser |
| EP2505591A1 (en) | 2005-02-11 | 2012-10-03 | Memorial Sloan-Kettering Cancer Center | Methods and compositions for detecting a drug resistant EGFR mutant |
| US20060247250A1 (en) * | 2005-03-16 | 2006-11-02 | Targegen, Inc. | Pyrimidine inhibitors of kinases |
| DE102005016634A1 (de) * | 2005-04-12 | 2006-10-19 | Merck Patent Gmbh | Neuartige Aza-Hetercyclen als Kinase-Inhibitoren |
| WO2007027238A2 (en) | 2005-05-03 | 2007-03-08 | 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 |
| 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 |
| ES2651349T3 (es) * | 2005-06-08 | 2018-01-25 | Rigel Pharmaceuticals, Inc. | Composiciones y métodos para la inhibición de la ruta JAK |
| AU2006283592A1 (en) | 2005-08-22 | 2007-03-01 | Amgen Inc. | Pyrazolopyridine and pyrazolopyrimidine compounds useful as kinase enzymes modulators |
| US8101625B2 (en) | 2005-10-21 | 2012-01-24 | Exelixis, Inc. | Pyrimidinones as Casein Kinase II (CK2) modulators |
| MX391408B (es) | 2005-11-01 | 2025-03-21 | Impact Biomedicines Inc | Inhibidores de biaril meta-pirimidina de cinasas. |
| CA2626479A1 (en) * | 2005-11-03 | 2007-05-18 | Irm Llc | Protein kinase inhibitors |
| US7713987B2 (en) | 2005-12-06 | 2010-05-11 | Rigel Pharmaceuticals, Inc. | Pyrimidine-2,4-diamines and their uses |
| EP1968950A4 (en) * | 2005-12-19 | 2010-04-28 | Genentech Inc | PYRIMIDINKINASEINHIBITOREN |
| TW200736232A (en) * | 2006-01-26 | 2007-10-01 | Astrazeneca Ab | Pyrimidine derivatives |
| JP2009525337A (ja) | 2006-01-30 | 2009-07-09 | エクセリクシス， インク． | Ｊａｋ−２調節因子としての４−アリール−２−アミノ−ピリミジン類又は４−アリール−２−アミノアルキル−ピリミジン類と使用方法 |
| PT1984357E (pt) | 2006-02-17 | 2013-12-23 | Rigel Pharmaceuticals Inc | Compostos de 2,4-pirimidinadiamina para tratamento ou prevenção de doenças autoimunes |
| ES2622493T3 (es) | 2006-02-24 | 2017-07-06 | Rigel Pharmaceuticals, Inc. | Composiciones y métodos para la inhibición de la ruta de JAK |
| RU2452737C2 (ru) | 2006-03-30 | 2012-06-10 | Тиботек Фармасьютикалз Лтд. | 5-(гидроксиметилен- и аминометилен)замещенные пиримидины, ингибирующие вич |
| AU2007233737B2 (en) | 2006-03-30 | 2012-11-29 | Janssen Sciences Ireland Uc | HIV inhibiting 5-amido substituted pyrimidines |
| GB0608386D0 (en) | 2006-04-27 | 2006-06-07 | Senexis Ltd | Compounds |
| JP5682051B2 (ja) | 2006-05-18 | 2015-03-11 | ファーマサイクリックス，インク． | 細胞内キナーゼ阻害剤 |
| 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 |
| RU2009105826A (ru) | 2006-07-21 | 2010-08-27 | Новартис АГ (CH) | 2,4-ди(ариламино)питимидин-5-карбоксамидные соединения в качестве ингибиторов jak-киназ |
| DE102006041382A1 (de) | 2006-08-29 | 2008-03-20 | Bayer Schering Pharma Ag | Carbamoyl-Sulfoximide als Proteinkinaseinhibitoren |
| HUE028086T2 (en) | 2006-09-22 | 2016-11-28 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase |
| DK2089369T3 (da) * | 2006-10-19 | 2011-05-09 | Rigel Pharmaceuticals Inc | 2,4-pyrimidindiaminderivater som hæmmere af JAK-kinaser til behandling af autoimmune sygdomme |
| ES2403546T3 (es) | 2006-11-03 | 2013-05-20 | Pharmacyclics, Inc. | Sonda de actividad de la tirosina-cinasa de Bruton y procedimiento de utilización |
| JP5264759B2 (ja) | 2006-11-21 | 2013-08-14 | 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 | ２，４−ピリミジンジアミン化合物のプロドラッグ塩およびそれらの使用 |
| EA017405B9 (ru) * | 2006-12-08 | 2014-05-30 | АйАрЭм ЭлЭлСи | Соединения и композиции в качестве ингибиторов протеинкиназы |
| CA2670645A1 (en) * | 2006-12-19 | 2008-07-03 | 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 |
| US9006243B2 (en) | 2006-12-29 | 2015-04-14 | Janssen R&D Ireland | HIV inhibiting 6-substituted pyrimidines |
| CN106045965A (zh) | 2006-12-29 | 2016-10-26 | 爱尔兰詹森科学公司 | 抑制hiv的5,6‑取代的嘧啶类化合物 |
| PE20081636A1 (es) | 2007-01-26 | 2009-01-10 | Smithkline Beecham Corp | Inhibidores de antranilamida para aurora quinasa |
| WO2008092199A1 (en) | 2007-01-31 | 2008-08-07 | Cytopia Research Pty Ltd | Thiopyrimidine-based compounds and uses thereof |
| DE102007010801A1 (de) | 2007-03-02 | 2008-09-04 | Bayer Cropscience Ag | Diaminopyrimidine als Fungizide |
| BRPI0809189A2 (pt) | 2007-03-20 | 2014-09-09 | Smithkline Beecham Corp | Composto ou um sal do mesmo, composição farmacêutica, métodos para tratar um distúrbio em um mamífero e para tratar câncer em um mamífero, e, uso de um composto |
| EA200901138A1 (ru) | 2007-03-20 | 2010-04-30 | Смитклайн Бичем Корпорейшн | Производные дианилинопиримидина как ингибиторы киназы wee1, фармацевтическая композиция и применение |
| 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 |
| US8809273B2 (en) | 2007-03-28 | 2014-08-19 | Pharmacyclics, Inc. | Inhibitors of Bruton's tyrosine kinase |
| US20120065201A1 (en) | 2007-03-28 | 2012-03-15 | Pharmacyclics, Inc. | Inhibitors of bruton's tyrosine kinase |
| EP2152079A4 (en) | 2007-06-04 | 2011-03-09 | Avila Therapeutics Inc | HETEROCYCLIC COMPOUNDS AND USES THEREOF |
| NZ582485A (en) * | 2007-07-17 | 2012-05-25 | 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 |
| WO2009032703A1 (en) | 2007-08-28 | 2009-03-12 | Irm Llc | 2- (het) arylamino-6-aminopyridine derivatives and fused forms thereof as anaplastic lymphoma kinase inhibitors |
| AU2008314632B2 (en) | 2007-10-19 | 2015-05-28 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| US7989465B2 (en) | 2007-10-19 | 2011-08-02 | Avila Therapeutics, Inc. | 4,6-disubstituted pyrimidines useful as kinase inhibitors |
| CA2710118A1 (en) | 2007-12-20 | 2009-07-02 | Cellzome Limited | Sulfamides as zap-70 inhibitors |
| CA2715962C (en) | 2008-02-22 | 2017-03-07 | Rigel Pharmaceuticals, Inc. | Use of 2,4-pyrimidinediamines for the treatment of atherosclerosis |
| 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 |
| DK2321283T3 (en) | 2008-04-16 | 2016-10-31 | Portola Pharm Inc | 2,6-diamino-pyrimidine-5-ylcarboxamides as inhibitors of Syk OR JAK Kinases |
| US8138339B2 (en) * | 2008-04-16 | 2012-03-20 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| EP2323993B1 (en) * | 2008-04-16 | 2015-06-03 | Portola Pharmaceuticals, Inc. | 2,6-diamino- pyrimidin- 5-yl-carboxamides as syk or jak kinases inhibitors |
| JP2011518836A (ja) | 2008-04-24 | 2011-06-30 | インサイト・コーポレイション | 大環状化合物およびそれらのキナーゼ阻害剤としての使用 |
| KR101860057B1 (ko) | 2008-05-21 | 2018-05-21 | 어리어드 파마슈티칼스, 인코포레이티드 | 키나아제 억제제로서 포스포러스 유도체 |
| 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 |
| AU2009270856B2 (en) | 2008-07-16 | 2013-07-25 | Pharmacyclics Llc | Inhibitors of Bruton's tyrosine kinase for the treatment of solid tumors |
| WO2010025833A1 (de) | 2008-09-03 | 2010-03-11 | Bayer Cropscience Ag | Alkoxy- und alkylthio-substituierte anilinopyrimidine |
| US20110245156A1 (en) | 2008-12-09 | 2011-10-06 | Cytokine Pharmasciences, Inc. | Novel antiviral compounds, compositions, and methods of use |
| CA2748758C (en) | 2009-01-15 | 2017-06-13 | F. Hoffmann-La Roche Ag | Antibodies against phosphorylated tyrosines on erythropoietin receptor (epor) |
| EP2414337B1 (en) | 2009-04-03 | 2013-05-01 | Cellzome GmbH | Methods for the identification of kinase interacting molecules and for the purification of kinase proteins |
| KR101705158B1 (ko) * | 2009-05-05 | 2017-02-09 | 다나-파버 캔서 인스티튜트 인크. | Ｅｇｆｒ 억제제 및 질환 치료방법 |
| HUE026647T2 (en) | 2009-05-08 | 2016-07-28 | Astellas Pharma Inc | Diamino heterocyclic carboxamide compound |
| WO2010146132A1 (en) | 2009-06-18 | 2010-12-23 | Cellzome Limited | Sulfonamides and sulfamides as zap-70 inhibitors |
| US7718662B1 (en) | 2009-10-12 | 2010-05-18 | Pharmacyclics, Inc. | Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase |
| US20110207736A1 (en) | 2009-12-23 | 2011-08-25 | Gatekeeper Pharmaceuticals, 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 |
| CA3113343C (en) | 2010-06-03 | 2024-10-08 | Pharmacyclics Llc | USE OF BRUTON'S TYROSINE KINASE INHIBITORS IN THE TREATMENT OF FOLLICULAR LYMPHOMA |
| US20120071497A1 (en) | 2010-06-03 | 2012-03-22 | Pharmacyclics, Inc. | Methods of treating abc-dlbcl using inhibitors of bruton's tyrosine kinase |
| WO2011153553A2 (en) | 2010-06-04 | 2011-12-08 | The Regents Of The University Of California | Methods and compositions for kinase inhibition |
| EP2603081B1 (en) | 2010-08-10 | 2016-10-05 | Celgene Avilomics Research, Inc. | Besylate salt of a btk inhibitor |
| TWI545115B (zh) | 2010-11-01 | 2016-08-11 | 阿維拉製藥公司 | 雜環化合物及其用途 |
| US9238629B2 (en) | 2010-11-01 | 2016-01-19 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| WO2012061415A1 (en) | 2010-11-01 | 2012-05-10 | Portola Pharmaceuticals, Inc. | Oxypyrimidines as syk modulators |
| WO2012064706A1 (en) | 2010-11-10 | 2012-05-18 | Avila Therapeutics, 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 |
| JP6068451B2 (ja) | 2011-05-17 | 2017-01-25 | ザ・リージエンツ・オブ・ザ・ユニバーシテイ・オブ・カリフオルニア | キナーゼ阻害剤 |
| BR112014009276A8 (pt) | 2011-10-19 | 2017-06-20 | Pharmacyclics Inc | uso de inibidores de tirosina quinase de bruton (btk) |
| CN103159742B (zh) | 2011-12-16 | 2015-08-12 | 北京韩美药品有限公司 | 5-氯嘧啶类化合物及其作为egfr酪氨酸激酶抑制剂的应用 |
| CN104302178B (zh) | 2012-03-15 | 2018-07-13 | 西建卡尔有限责任公司 | 表皮生长因子受体激酶抑制剂的固体形式 |
| CN111329989A (zh) | 2012-11-02 | 2020-06-26 | 药品循环有限责任公司 | Tec家族激酶抑制剂辅助疗法 |
| 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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