JP2010529134A5 - - Google Patents
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- JP2010529134A5 JP2010529134A5 JP2010511276A JP2010511276A JP2010529134A5 JP 2010529134 A5 JP2010529134 A5 JP 2010529134A5 JP 2010511276 A JP2010511276 A JP 2010511276A JP 2010511276 A JP2010511276 A JP 2010511276A JP 2010529134 A5 JP2010529134 A5 JP 2010529134A5
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- Prior art keywords
- compound
- halogen
- nhc
- cancer
- oxo
- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims description 71
- 229910052736 halogen Inorganic materials 0.000 claims description 56
- 150000002367 halogens Chemical class 0.000 claims description 56
- 125000001931 aliphatic group Chemical group 0.000 claims description 42
- 229910052739 hydrogen Inorganic materials 0.000 claims description 36
- 239000001257 hydrogen Substances 0.000 claims description 36
- 229920006395 saturated elastomer Polymers 0.000 claims description 28
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims description 26
- -1 1-imidazolyl Chemical group 0.000 claims description 24
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 24
- 102100026547 Platelet-derived growth factor receptor beta Human genes 0.000 claims description 24
- 150000002431 hydrogen Chemical group 0.000 claims description 20
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 19
- 229910052760 oxygen Inorganic materials 0.000 claims description 19
- 239000001301 oxygen Substances 0.000 claims description 19
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 18
- 201000010099 disease Diseases 0.000 claims description 18
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 18
- 125000005842 heteroatom Chemical group 0.000 claims description 18
- 125000001183 hydrocarbyl group Chemical group 0.000 claims description 18
- 229910052757 nitrogen Inorganic materials 0.000 claims description 18
- 229910052717 sulfur Chemical group 0.000 claims description 18
- 239000011593 sulfur Chemical group 0.000 claims description 18
- 101000692455 Homo sapiens Platelet-derived growth factor receptor beta Proteins 0.000 claims description 16
- 238000000034 method Methods 0.000 claims description 15
- 125000003118 aryl group Chemical group 0.000 claims description 14
- GVNVAWHJIKLAGL-UHFFFAOYSA-N 2-(cyclohexen-1-yl)cyclohexan-1-one Chemical compound O=C1CCCCC1C1=CCCCC1 GVNVAWHJIKLAGL-UHFFFAOYSA-N 0.000 claims description 12
- 101150065749 Churc1 gene Proteins 0.000 claims description 12
- 206010016654 Fibrosis Diseases 0.000 claims description 12
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 12
- 102100038239 Protein Churchill Human genes 0.000 claims description 12
- 125000002950 monocyclic group Chemical group 0.000 claims description 12
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 12
- 125000000217 alkyl group Chemical group 0.000 claims description 10
- 230000000694 effects Effects 0.000 claims description 10
- 239000003112 inhibitor Substances 0.000 claims description 10
- 108010051742 Platelet-Derived Growth Factor beta Receptor Proteins 0.000 claims description 8
- 102100030485 Platelet-derived growth factor receptor alpha Human genes 0.000 claims description 8
- 101710148465 Platelet-derived growth factor receptor alpha Proteins 0.000 claims description 8
- 125000004429 atom Chemical group 0.000 claims description 8
- 125000002619 bicyclic group Chemical group 0.000 claims description 8
- 230000004761 fibrosis Effects 0.000 claims description 8
- 230000002401 inhibitory effect Effects 0.000 claims description 8
- 239000003814 drug Substances 0.000 claims description 7
- 206010006187 Breast cancer Diseases 0.000 claims description 6
- 208000026310 Breast neoplasm Diseases 0.000 claims description 6
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims description 6
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 claims description 6
- 201000010260 leiomyoma Diseases 0.000 claims description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 6
- 150000003839 salts Chemical class 0.000 claims description 6
- 230000001404 mediated effect Effects 0.000 claims description 5
- LBUJPTNKIBCYBY-UHFFFAOYSA-N 1,2,3,4-tetrahydroquinoline Chemical compound C1=CC=C2CCCNC2=C1 LBUJPTNKIBCYBY-UHFFFAOYSA-N 0.000 claims description 4
- 206010003210 Arteriosclerosis Diseases 0.000 claims description 4
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- 206010069351 acute lung injury Diseases 0.000 claims description 4
- 230000001476 alcoholic effect Effects 0.000 claims description 4
- 239000012472 biological sample Substances 0.000 claims description 4
- 230000007882 cirrhosis Effects 0.000 claims description 4
- 208000019425 cirrhosis of liver Diseases 0.000 claims description 4
- 125000004980 cyclopropylene group Chemical group 0.000 claims description 4
- 125000001188 haloalkyl group Chemical group 0.000 claims description 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 4
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- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 4
- QQONPFPTGQHPMA-UHFFFAOYSA-N propylene Natural products CC=C QQONPFPTGQHPMA-UHFFFAOYSA-N 0.000 claims description 4
- 208000005069 pulmonary fibrosis Diseases 0.000 claims description 4
- 125000004076 pyridyl group Chemical group 0.000 claims description 4
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- 229940124597 therapeutic agent Drugs 0.000 claims description 4
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- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims description 2
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- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims description 2
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims description 2
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims description 2
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- 206010006895 Cachexia Diseases 0.000 claims description 2
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- 206010008342 Cervix carcinoma Diseases 0.000 claims description 2
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- 208000007342 Diabetic Nephropathies Diseases 0.000 claims description 2
- 201000009273 Endometriosis Diseases 0.000 claims description 2
- 102000010834 Extracellular Matrix Proteins Human genes 0.000 claims description 2
- 108010037362 Extracellular Matrix Proteins Proteins 0.000 claims description 2
- 208000007659 Fibroadenoma Diseases 0.000 claims description 2
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- 206010020751 Hypersensitivity Diseases 0.000 claims description 2
- 206010020772 Hypertension Diseases 0.000 claims description 2
- 206010055171 Hypertensive nephropathy Diseases 0.000 claims description 2
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims description 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims description 2
- 208000007766 Kaposi sarcoma Diseases 0.000 claims description 2
- 208000002260 Keloid Diseases 0.000 claims description 2
- 206010023330 Keloid scar Diseases 0.000 claims description 2
- 208000032004 Large-Cell Anaplastic Lymphoma Diseases 0.000 claims description 2
- 206010023825 Laryngeal cancer Diseases 0.000 claims description 2
- 208000004852 Lung Injury Diseases 0.000 claims description 2
- 208000005777 Lupus Nephritis Diseases 0.000 claims description 2
- 206010025323 Lymphomas Diseases 0.000 claims description 2
- 206010027406 Mesothelioma Diseases 0.000 claims description 2
- 208000034578 Multiple myelomas Diseases 0.000 claims description 2
- 208000001132 Osteoporosis Diseases 0.000 claims description 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 2
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims description 2
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- 206010038923 Retinopathy Diseases 0.000 claims description 2
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- 206010041067 Small cell lung cancer Diseases 0.000 claims description 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 2
- 206010042971 T-cell lymphoma Diseases 0.000 claims description 2
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims description 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims description 2
- 206010069363 Traumatic lung injury Diseases 0.000 claims description 2
- 208000008385 Urogenital Neoplasms Diseases 0.000 claims description 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 2
- 238000009825 accumulation Methods 0.000 claims description 2
- 208000002517 adenoid cystic carcinoma Diseases 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 claims description 2
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims description 2
- 125000002947 alkylene group Chemical group 0.000 claims description 2
- 239000002246 antineoplastic agent Substances 0.000 claims description 2
- 208000011775 arteriosclerosis disease Diseases 0.000 claims description 2
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- 208000006673 asthma Diseases 0.000 claims description 2
- 201000009036 biliary tract cancer Diseases 0.000 claims description 2
- 208000020790 biliary tract neoplasm Diseases 0.000 claims description 2
- 201000003149 breast fibroadenoma Diseases 0.000 claims description 2
- 201000011510 cancer Diseases 0.000 claims description 2
- 210000003169 central nervous system Anatomy 0.000 claims description 2
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- 229940127089 cytotoxic agent Drugs 0.000 claims description 2
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- 210000004696 endometrium Anatomy 0.000 claims description 2
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- 210000001035 gastrointestinal tract Anatomy 0.000 claims description 2
- 208000005017 glioblastoma Diseases 0.000 claims description 2
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- 208000027866 inflammatory disease Diseases 0.000 claims description 2
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims description 2
- GWVMLCQWXVFZCN-UHFFFAOYSA-N isoindoline Chemical compound C1=CC=C2CNCC2=C1 GWVMLCQWXVFZCN-UHFFFAOYSA-N 0.000 claims description 2
- 210000001117 keloid Anatomy 0.000 claims description 2
- 206010023841 laryngeal neoplasm Diseases 0.000 claims description 2
- 210000004185 liver Anatomy 0.000 claims description 2
- 201000007270 liver cancer Diseases 0.000 claims description 2
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- 231100000515 lung injury Toxicity 0.000 claims description 2
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- 125000001624 naphthyl group Chemical group 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 201000000742 primary sclerosing cholangitis Diseases 0.000 claims description 2
- 230000002062 proliferating effect Effects 0.000 claims description 2
- 210000002307 prostate Anatomy 0.000 claims description 2
- 230000005855 radiation Effects 0.000 claims description 2
- 201000002793 renal fibrosis Diseases 0.000 claims description 2
- 201000007416 salivary gland adenoid cystic carcinoma Diseases 0.000 claims description 2
- 208000010157 sclerosing cholangitis Diseases 0.000 claims description 2
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- 208000020431 spinal cord injury Diseases 0.000 claims description 2
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- 230000007863 steatosis Effects 0.000 claims description 2
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- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 claims description 2
- 201000002510 thyroid cancer Diseases 0.000 claims description 2
- 208000019553 vascular disease Diseases 0.000 claims description 2
- 230000029663 wound healing Effects 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims 1
- VPXLBSOCFQUCMB-UHFFFAOYSA-N CC(C=C1)N(Cc(cc2)ccc2C(Nc2cc(Nc3nc(-c4cnccc4)ccn3)c(C)cc2)=O)C1=O Chemical compound CC(C=C1)N(Cc(cc2)ccc2C(Nc2cc(Nc3nc(-c4cnccc4)ccn3)c(C)cc2)=O)C1=O VPXLBSOCFQUCMB-UHFFFAOYSA-N 0.000 description 1
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- 108091000080 Phosphotransferase Proteins 0.000 description 1
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- 230000031146 intracellular signal transduction Effects 0.000 description 1
- 229940043355 kinase inhibitor Drugs 0.000 description 1
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- 102000020233 phosphotransferase Human genes 0.000 description 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 description 1
- 108060006633 protein kinase Proteins 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94187307P | 2007-06-04 | 2007-06-04 | |
| US60/941,873 | 2007-06-04 | ||
| US97204807P | 2007-09-13 | 2007-09-13 | |
| US60/972,048 | 2007-09-13 | ||
| PCT/US2008/065646 WO2008151183A1 (en) | 2007-06-04 | 2008-06-03 | Heterocyclic compounds and uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013155820A Division JP5845215B2 (ja) | 2007-06-04 | 2013-07-26 | 複素環化合物およびその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010529134A JP2010529134A (ja) | 2010-08-26 |
| JP2010529134A5 true JP2010529134A5 (cg-RX-API-DMAC7.html) | 2012-05-24 |
| JP5526020B2 JP5526020B2 (ja) | 2014-06-18 |
Family
ID=40089003
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010511276A Expired - Fee Related JP5526020B2 (ja) | 2007-06-04 | 2008-06-03 | 複素環化合物およびその使用 |
| JP2013155820A Expired - Fee Related JP5845215B2 (ja) | 2007-06-04 | 2013-07-26 | 複素環化合物およびその使用 |
| JP2015227445A Pending JP2016033142A (ja) | 2007-06-04 | 2015-11-20 | 複素環化合物およびその使用 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013155820A Expired - Fee Related JP5845215B2 (ja) | 2007-06-04 | 2013-07-26 | 複素環化合物およびその使用 |
| JP2015227445A Pending JP2016033142A (ja) | 2007-06-04 | 2015-11-20 | 複素環化合物およびその使用 |
Country Status (6)
| Country | Link |
|---|---|
| US (4) | US8242271B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP2152079A4 (cg-RX-API-DMAC7.html) |
| JP (3) | JP5526020B2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2689989A1 (cg-RX-API-DMAC7.html) |
| TW (1) | TWI433677B (cg-RX-API-DMAC7.html) |
| WO (1) | WO2008151183A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (72)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8242271B2 (en) * | 2007-06-04 | 2012-08-14 | Avila Therapeutics, Inc. | Heterocyclic compounds and uses thereof |
| US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
| PL2300013T5 (pl) | 2008-05-21 | 2025-04-28 | Takeda Pharmaceutical Company Limited | Pochodne fosforu jako inhibitor kinazy |
| 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 |
| CA2986640C (en) | 2008-06-27 | 2019-03-26 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| EP2352827A4 (en) * | 2008-09-05 | 2016-07-20 | Celgene Avilomics Res Inc | ALGORITHM FOR DESIGNING IRREVERSIBLE INHIBITORS |
| US9040715B2 (en) | 2008-09-23 | 2015-05-26 | Georgetown University | 1,2-benzisothiazolinone and isoindolinone derivatives |
| KR101705158B1 (ko) | 2009-05-05 | 2017-02-09 | 다나-파버 캔서 인스티튜트 인크. | Ｅｇｆｒ 억제제 및 질환 치료방법 |
| EP2440058A4 (en) | 2009-06-12 | 2012-11-21 | Dana Farber Cancer Inst Inc | MELTED HETEROCYCLIC COMPOUNDS AND APPLICATIONS THEREOF |
| CN101928277B (zh) * | 2009-06-24 | 2012-09-19 | 浙江九洲药业股份有限公司 | 4-甲基-3-[[4-(3-吡啶基)-2-嘧啶基]氨基]安息香酸的制备方法、相关中间体及其应用 |
| CN102548987B (zh) * | 2009-07-14 | 2014-04-16 | 江苏迈度药物研发有限公司 | 作为激酶抑制剂的氟取代化合物及其使用方法 |
| CA2773848A1 (en) * | 2009-09-09 | 2011-03-17 | Avila Therapeutics, Inc. | Pi3 kinase inhibitors and uses thereof |
| IN2012DN02534A (cg-RX-API-DMAC7.html) * | 2009-09-16 | 2015-08-28 | Avila Therapeutics Inc | |
| CA2784807C (en) | 2009-12-29 | 2021-12-14 | Dana-Farber Cancer Institute, Inc. | Type ii raf kinase inhibitors |
| SG181965A1 (en) | 2009-12-30 | 2012-08-30 | Avila Therapeutics Inc | Ligand-directed covalent modification of protein |
| RU2013109393A (ru) | 2010-08-10 | 2014-09-20 | Сэлджин Авиаломикс Ресеарч, Инк. | Безилатная соль ингибитора втк |
| JP5956999B2 (ja) | 2010-11-01 | 2016-07-27 | セルジーン アヴィロミクス リサーチ， インコーポレイテッド | ヘテロアリール化合物およびその使用 |
| TWI545115B (zh) | 2010-11-01 | 2016-08-11 | 阿維拉製藥公司 | 雜環化合物及其用途 |
| EP2637502B1 (en) | 2010-11-10 | 2018-01-10 | Celgene CAR LLC | Mutant-selective egfr inhibitors and uses thereof |
| AU2012250517B2 (en) | 2011-05-04 | 2016-05-19 | Takeda Pharmaceutical Company Limited | Compounds for inhibiting cell proliferation in EGFR-driven cancers |
| US9428472B2 (en) | 2011-08-16 | 2016-08-30 | Georgetown University | Methods of treating bacterial infections with 1,2-benzisothiazolinone and isoindolinone derivatives |
| 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 |
| WO2013074986A1 (en) * | 2011-11-17 | 2013-05-23 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-jun-n-terminal kinase (jnk) |
| US9056839B2 (en) | 2012-03-15 | 2015-06-16 | Celgene Avilomics Research, Inc. | Solid forms of an epidermal growth factor receptor kinase inhibitor |
| US9108927B2 (en) | 2012-03-15 | 2015-08-18 | Celgene Avilomics Research, Inc. | Salts of an epidermal growth factor receptor kinase inhibitor |
| JP6469567B2 (ja) | 2012-05-05 | 2019-02-13 | アリアド・ファーマシューティカルズ・インコーポレイテッド | Ｅｇｆｒ発動性がんの細胞増殖阻害用化合物 |
| EP2909194A1 (en) * | 2012-10-18 | 2015-08-26 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| WO2014063054A1 (en) | 2012-10-19 | 2014-04-24 | Dana-Farber Cancer Institute, Inc. | Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof |
| USRE48175E1 (en) | 2012-10-19 | 2020-08-25 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged small molecules as inducers of protein degradation |
| WO2014100748A1 (en) | 2012-12-21 | 2014-06-26 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| EA201591051A1 (ru) | 2013-02-08 | 2016-06-30 | Селджен Авиломикс Рисерч, Инк. | Ингибиторы erk и варианты их применения |
| US9611283B1 (en) | 2013-04-10 | 2017-04-04 | Ariad Pharmaceuticals, Inc. | Methods for inhibiting cell proliferation in ALK-driven cancers |
| WO2015019365A1 (en) | 2013-08-07 | 2015-02-12 | Cadila Healthcare Limited | N-cyanomethylamides as inhibitors of janus kinase |
| 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 |
| ES2676734T3 (es) | 2013-10-18 | 2018-07-24 | Syros Pharmaceuticals, Inc. | Compuestos heteroatómicos útiles para el tratamiento de enfermedades proliferativas |
| US10047070B2 (en) | 2013-10-18 | 2018-08-14 | Dana-Farber Cancer Institute, Inc. | Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7) |
| US9415049B2 (en) | 2013-12-20 | 2016-08-16 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| SG11201608242XA (en) | 2014-04-04 | 2016-10-28 | Syros Pharmaceuticals Inc | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| WO2015164614A1 (en) | 2014-04-23 | 2015-10-29 | Dana-Farber Cancer Institute, Inc. | Janus kinase inhibitors and uses thereof |
| WO2015164604A1 (en) | 2014-04-23 | 2015-10-29 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged janus kinase inhibitors and uses thereof |
| WO2016020791A1 (en) | 2014-08-05 | 2016-02-11 | Novartis Ag | Ckit antibody drug conjugates |
| TW201613892A (en) | 2014-08-13 | 2016-04-16 | Celgene Avilomics Res Inc | Forms and compositions of an ERK inhibitor |
| EP3236959B1 (en) | 2014-12-23 | 2025-09-24 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| WO2016160617A2 (en) | 2015-03-27 | 2016-10-06 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
| AU2016276963C1 (en) | 2015-06-12 | 2021-08-05 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
| US10011611B2 (en) | 2015-08-14 | 2018-07-03 | Reaction Biology Corp. | Histone deacetylase inhibitors and methods for use thereof |
| JP7028766B2 (ja) | 2015-09-09 | 2022-03-02 | ダナ－ファーバー キャンサー インスティテュート， インコーポレイテッド | サイクリン依存性キナーゼの阻害剤 |
| CN107805240A (zh) * | 2016-09-08 | 2018-03-16 | 中国科学院合肥物质科学研究院 | 一种新型的pdgfr激酶抑制剂及其用途 |
| WO2018049127A1 (en) * | 2016-09-08 | 2018-03-15 | Sabila Biosciences Llc | 1,2-dithiolane compounds useful in neuroprotection, autoimmune and cancer diseases and conditions |
| GB201616511D0 (en) | 2016-09-29 | 2016-11-16 | Mission Therapeutics Limited | Novel compounds |
| GB201616627D0 (en) | 2016-09-30 | 2016-11-16 | Mission Therapeutics Limited | Novel compounds |
| GB201708652D0 (en) | 2017-05-31 | 2017-07-12 | Mission Therapeutics Ltd | Novel compounds and uses |
| EP3642196B1 (en) | 2017-06-20 | 2022-08-17 | Mission Therapeutics Limited | Substituted cyanopyrrolidines with activity as dub inhibitors |
| US20210261537A1 (en) * | 2018-06-07 | 2021-08-26 | Disarm Therapeutics, Inc. | Inhibitors of sarm1 |
| CN108623490A (zh) * | 2018-06-22 | 2018-10-09 | 苏州市贝克生物科技有限公司 | (2z)-4-(二甲基氨基)-2-丁烯酸盐酸盐的合成方法 |
| CN112367991A (zh) | 2018-06-25 | 2021-02-12 | 达纳-法伯癌症研究所股份有限公司 | Taire家族激酶抑制剂及其用途 |
| EP3897670A4 (en) | 2018-12-19 | 2022-09-07 | Disarm Therapeutics, Inc. | MRSA1 INHIBITORS IN COMBINATION WITH NEUROPROTECTIVE AGENTS |
| EP3902542A4 (en) | 2018-12-28 | 2022-09-07 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 and uses thereof |
| GB201905371D0 (en) | 2019-04-16 | 2019-05-29 | Mission Therapeutics Ltd | Novel compounds |
| GB201905375D0 (en) | 2019-04-16 | 2019-05-29 | Mission Therapeutics Ltd | Novel compounds |
| JP7289375B2 (ja) * | 2019-06-06 | 2023-06-09 | ディスアーム セラピューティクス， インコーポレイテッド | Ｓａｒｍ１の阻害剤 |
| GB201912674D0 (en) | 2019-09-04 | 2019-10-16 | Mission Therapeutics Ltd | Novel compounds |
| CN111253335B (zh) * | 2020-03-12 | 2023-06-06 | 浙江扬帆新材料股份有限公司 | 一种n-取代苯并异噻唑啉-3-酮衍生物的新合成方法 |
| CN111269217B (zh) * | 2020-04-07 | 2021-01-08 | 苏州信诺维医药科技有限公司 | 一种嘧啶胺类化合物、其制备方法及应用 |
| KR20230006487A (ko) | 2020-04-08 | 2023-01-10 | 미션 테라퓨틱스 엘티디 | Usp30 억제제로서의 활성을 갖는 n-시아노피롤리딘 |
| CN115667252A (zh) | 2020-05-28 | 2023-01-31 | 特殊治疗有限公司 | 用于治疗线粒体功能障碍的作为usp30抑制剂的n-(1-氰基-吡咯烷-3-基)-5-(3-(三氟甲基)苯基)噁唑-2-甲酰胺衍生物和对应噁二唑衍生物 |
| WO2021245186A1 (en) | 2020-06-04 | 2021-12-09 | Mission Therapeutics Limited | N-cyanopyrrolidines with activity as usp30 inhibitors |
| KR20230022215A (ko) | 2020-06-08 | 2023-02-14 | 미션 테라퓨틱스 엘티디 | 미토콘드리아 기능장애, 암 및 섬유증의 치료에 사용하기 위한 USP30 억제제로서 1-(5-(2-시아노피리딘-4-일)옥사졸-2-카보닐)-4-메틸헥사하이드로피롤로[3,4-b]피롤-5(1H)-카보니트릴 |
| GB202016800D0 (en) | 2020-10-22 | 2020-12-09 | Mission Therapeutics Ltd | Novel compounds |
| US20250034122A1 (en) | 2021-12-01 | 2025-01-30 | Mission Therapeutics Limited | Substituted n-cyanopyrrolidines with activity as usp30 inhibitors |
| AU2023312198A1 (en) * | 2022-07-19 | 2025-02-27 | Chiesi Farmaceutici S.P.A. | HETEROARYL DERIVATIVES AS DDRs INHIBITORS |
Family Cites Families (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5521184A (en) | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| GB9914258D0 (en) | 1999-06-18 | 1999-08-18 | Celltech Therapeutics Ltd | Chemical compounds |
| GB0022438D0 (en) | 2000-09-13 | 2000-11-01 | Novartis Ag | Organic Compounds |
| US20040157855A1 (en) | 2001-04-05 | 2004-08-12 | Michael Heinrich | Use of n-phenyl-2-pyrimidineamine derivativea against mast cell-based diseases like allergic disorders |
| US20030176443A1 (en) | 2001-05-16 | 2003-09-18 | Matthias Stein-Gerlach | Pyridylpyrimidine derivatives as effective compounds against prion diseases |
| AU2002315388A1 (en) | 2001-06-21 | 2003-01-08 | Ariad Pharmaceuticals, Inc. | Novel phenylamino-pyrimidines and uses thereof |
| IL161662A0 (en) | 2001-11-01 | 2004-09-27 | Janssen Pharmaceutica Nv | Heteroaryl amines as glycogen synthase kinase 3 beta inhibitors (gsk3 inhibitors) |
| JP2005507420A (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３β阻害剤としてのアミノベンズアミド誘導体 |
| GB0201508D0 (en) | 2002-01-23 | 2002-03-13 | Novartis Ag | Organic compounds |
| GB0202873D0 (en) | 2002-02-07 | 2002-03-27 | Novartis Ag | Organic compounds |
| GB0215676D0 (en) | 2002-07-05 | 2002-08-14 | Novartis Ag | Organic compounds |
| US20060105445A1 (en) | 2002-07-29 | 2006-05-18 | Klaus Godl | Medium and method for enriching, purifying or depleting atp binding proteins from a pool of proteins |
| MY139563A (en) * | 2002-09-04 | 2009-10-30 | Bristol Myers Squibb Co | Heterocyclic aromatic compounds useful as growth hormone secretagogues |
| CA2439440A1 (en) | 2002-09-05 | 2004-03-05 | Emory University | Treatment of tuberous sclerosis associated neoplasms |
| GB0222514D0 (en) * | 2002-09-27 | 2002-11-06 | Novartis Ag | Organic compounds |
| US7279576B2 (en) * | 2002-12-31 | 2007-10-09 | Deciphera Pharmaceuticals, Llc | Anti-cancer medicaments |
| US7144911B2 (en) | 2002-12-31 | 2006-12-05 | Deciphera Pharmaceuticals Llc | Anti-inflammatory medicaments |
| WO2005065074A2 (en) | 2003-09-09 | 2005-07-21 | Temple University Of The Commonwealth System Of Higher Education | Protection of tissues and cells from cytotoxic effects of ionizing radiation by abl inhibitors |
| GB0325031D0 (en) | 2003-10-27 | 2003-12-03 | Novartis Ag | Organic compounds |
| WO2005049021A1 (en) | 2003-11-03 | 2005-06-02 | Oy Helsinki Transplantation R & D Ltd | Materials and methods for inhibiting neointimal hyperplasia |
| ES2651615T3 (es) * | 2003-12-25 | 2018-01-29 | Nippon Shinyaku Co., Ltd. | Amidoderivado y medicamento |
| JPWO2005063720A1 (ja) | 2003-12-25 | 2007-07-19 | 日本新薬株式会社 | アミド誘導体及び医薬 |
| AU2005209231B8 (en) | 2004-01-21 | 2011-07-28 | Emory University | Compositions and methods of use for tyrosine kinase inhibitors to treat pathogenic infection |
| AU2005245386B2 (en) * | 2004-05-07 | 2008-11-27 | Amgen Inc. | Nitrogenated heterocyclic derivatives as protein kinase modulators and use for the treatment of angiogenesis and cancer |
| WO2005115385A1 (en) | 2004-05-24 | 2005-12-08 | Ab Science | Use of c-kit inhibitors for treating acne |
| WO2006017353A2 (en) | 2004-07-13 | 2006-02-16 | GOVERNMENT OF THE UNITED STATES, as represented byTHE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES | Treatment of viral infections |
| JP2008510766A (ja) | 2004-08-27 | 2008-04-10 | ゲーペーツェー ビオテック アーゲー | ピリミジン誘導体 |
| MX2007009135A (es) | 2005-01-28 | 2007-09-06 | Novartis Ag | Uso de pirimidilaminobenzamidas para el tratamiento de enfermedades que responden a la modulacion de la actividad de la cinasa tie-2. |
| CN101160131A (zh) | 2005-02-25 | 2008-04-09 | 诺瓦提斯公司 | Bcr-abl和raf抑制剂的药物组合产品 |
| JP5129123B2 (ja) | 2005-05-02 | 2013-01-23 | ノバルティス アーゲー | 全身性肥満細胞症の処置のためのピリミジルアミノベンズアミド誘導体の使用 |
| SA06270147B1 (ar) | 2005-06-09 | 2009-12-22 | نوفارتيس ايه جي | عملية لتخليق 5-(مثيل–1h–إيميدازول–1-يل )–3-(ثلاثي فلـورو مثيل)–بنزامـين |
| KR20080036992A (ko) | 2005-07-20 | 2008-04-29 | 노파르티스 아게 | 증식성 질환을 치료하기 위한 피리미딜아미노벤즈아미드 및ｆｌｔ-3 억제제를 포함하는 조합물 |
| KR100674813B1 (ko) | 2005-08-05 | 2007-01-29 | 일양약품주식회사 | Ｎ-페닐-2-피리미딘-아민 유도체 및 그의 제조방법 |
| CA2629132C (en) | 2005-12-06 | 2014-05-27 | Novartis Ag | Pyrimidylaminobenzamide derivatives for the treatment of neurofibromatosis |
| US20100048539A1 (en) * | 2006-11-03 | 2010-02-25 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| US8242271B2 (en) * | 2007-06-04 | 2012-08-14 | Avila Therapeutics, Inc. | Heterocyclic compounds and uses thereof |
| EP2352827A4 (en) * | 2008-09-05 | 2016-07-20 | Celgene Avilomics Res Inc | ALGORITHM FOR DESIGNING IRREVERSIBLE INHIBITORS |
-
2008
- 2008-06-03 US US12/132,537 patent/US8242271B2/en not_active Expired - Fee Related
- 2008-06-03 EP EP08770044A patent/EP2152079A4/en not_active Withdrawn
- 2008-06-03 TW TW097120571A patent/TWI433677B/zh active
- 2008-06-03 CA CA2689989A patent/CA2689989A1/en not_active Abandoned
- 2008-06-03 WO PCT/US2008/065646 patent/WO2008151183A1/en not_active Ceased
- 2008-06-03 JP JP2010511276A patent/JP5526020B2/ja not_active Expired - Fee Related
-
2012
- 2012-05-31 US US13/485,037 patent/US8586600B2/en not_active Expired - Fee Related
-
2013
- 2013-07-26 JP JP2013155820A patent/JP5845215B2/ja not_active Expired - Fee Related
- 2013-11-15 US US14/080,890 patent/US9067929B2/en not_active Expired - Fee Related
-
2015
- 2015-05-21 US US14/718,700 patent/US20150252019A1/en not_active Abandoned
- 2015-11-20 JP JP2015227445A patent/JP2016033142A/ja active Pending
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