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
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- 108010051742 Platelet-Derived Growth Factor beta Receptor Proteins 0.000 claims description 8
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- 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
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- 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
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- 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
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- 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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- QQONPFPTGQHPMA-UHFFFAOYSA-N propylene Natural products CC=C QQONPFPTGQHPMA-UHFFFAOYSA-N 0.000 claims description 4
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- 206010055171 Hypertensive nephropathy Diseases 0.000 claims description 2
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims description 2
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- 208000007766 Kaposi sarcoma Diseases 0.000 claims description 2
- 208000002260 Keloid Diseases 0.000 claims description 2
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- 208000032004 Large-Cell Anaplastic Lymphoma Diseases 0.000 claims description 2
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- 208000005777 Lupus Nephritis Diseases 0.000 claims description 2
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- 206010027406 Mesothelioma Diseases 0.000 claims description 2
- 208000034578 Multiple myelomas Diseases 0.000 claims description 2
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- 206010041067 Small cell lung cancer Diseases 0.000 claims description 2
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- 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
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- 125000002947 alkylene group Chemical group 0.000 claims description 2
- 239000002246 antineoplastic agent Substances 0.000 claims description 2
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- 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
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- 125000001624 naphthyl group Chemical group 0.000 claims description 2
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- 230000002062 proliferating effect Effects 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
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- 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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- 102000020233 phosphotransferase Human genes 0.000 description 1
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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 (enExample) | 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 (enExample) |
| EP (1) | EP2152079A4 (enExample) |
| JP (3) | JP5526020B2 (enExample) |
| CA (1) | CA2689989A1 (enExample) |
| TW (1) | TWI433677B (enExample) |
| WO (1) | WO2008151183A1 (enExample) |
Families Citing this family (72)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI433677B (zh) * | 2007-06-04 | 2014-04-11 | Avila Therapeutics Inc | 雜環化合物及其用途 |
| PT2300013T (pt) | 2008-05-21 | 2017-10-31 | Ariad Pharma Inc | Derivados de fósforo como inibidores de cinases |
| US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
| 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 |
| US11351168B1 (en) | 2008-06-27 | 2022-06-07 | Celgene Car Llc | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| CN105574346A (zh) * | 2008-09-05 | 2016-05-11 | 新基阿维罗米克斯研究公司 | 多肽偶联物与不可逆抑制剂的设计方法和检测方法 |
| AU2009298888A1 (en) | 2008-09-23 | 2010-04-08 | Georgetown University | 1,2-benzisothiazolinone and isoindolinone derivatives |
| JP5918693B2 (ja) | 2009-05-05 | 2016-05-18 | ダナ ファーバー キャンサー インスティテュート インコーポレイテッド | Ｅｇｆｒ阻害剤及び疾患の治療方法 |
| 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 |
| WO2011031896A2 (en) * | 2009-09-09 | 2011-03-17 | Avila Therapeutics, Inc. | Pi3 kinase inhibitors and uses thereof |
| US9556426B2 (en) * | 2009-09-16 | 2017-01-31 | Celgene Avilomics Research, Inc. | Protein kinase conjugates and inhibitors |
| CA2784807C (en) | 2009-12-29 | 2021-12-14 | Dana-Farber Cancer Institute, Inc. | Type ii raf kinase inhibitors |
| 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 |
| NZ607845A (en) | 2010-08-10 | 2015-03-27 | Celgene Avilomics Res Inc | Besylate salt of a btk inhibitor |
| EP2635285B1 (en) | 2010-11-01 | 2017-05-03 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| WO2012061299A1 (en) | 2010-11-01 | 2012-05-10 | Avila Therapeutics, Inc. | Heterocyclic compounds and uses thereof |
| US8796255B2 (en) | 2010-11-10 | 2014-08-05 | Celgene Avilomics Research, Inc | Mutant-selective EGFR inhibitors and uses thereof |
| EP2704572B1 (en) | 2011-05-04 | 2015-12-30 | Ariad Pharmaceuticals, Inc. | 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 |
| EP2770830A4 (en) | 2011-10-28 | 2015-05-27 | Celgene Avilomics Res Inc | METHODS OF TREATING A DISEASE OR DISEASE ASSOCIATED WITH TYROSINE KINASE BTK (BRUTON'S TYROSINE KINASE) |
| WO2013074986A1 (en) | 2011-11-17 | 2013-05-23 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-jun-n-terminal kinase (jnk) |
| MX356753B (es) | 2012-03-15 | 2018-06-12 | Celgene Avilomics Res Inc | Formas solidas de un inhibidor de cinasa del receptor del factor de crecimiento epidermico. |
| PT2825042T (pt) | 2012-03-15 | 2018-11-16 | Celgene Car Llc | Sais de um inibidor de cinases do recetor do fator de crescimento epidérmico |
| AU2013204563B2 (en) | 2012-05-05 | 2016-05-19 | Takeda Pharmaceutical Company Limited | Compounds for inhibiting cell proliferation in EGFR-driven cancers |
| US10112927B2 (en) | 2012-10-18 | 2018-10-30 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (CDK7) |
| US10000483B2 (en) | 2012-10-19 | 2018-06-19 | Dana-Farber Cancer Institute, Inc. | Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof |
| US9758522B2 (en) | 2012-10-19 | 2017-09-12 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged small molecules as inducers of protein degradation |
| US9126950B2 (en) | 2012-12-21 | 2015-09-08 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| WO2014124230A2 (en) | 2013-02-08 | 2014-08-14 | Celgene Avilomics Research, Inc. | Erk inhibitors and uses thereof |
| US9611283B1 (en) | 2013-04-10 | 2017-04-04 | Ariad Pharmaceuticals, Inc. | Methods for inhibiting cell proliferation in ALK-driven cancers |
| KR101665301B1 (ko) | 2013-08-07 | 2016-10-11 | 카딜라 핼쓰캐어 리미티드 | 야누스 키나제의 억제제로서 n-시아노메틸아미드 |
| 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 |
| JP6491202B2 (ja) | 2013-10-18 | 2019-03-27 | デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド | サイクリン依存性キナーゼ７（ｃｄｋ７）の多環阻害剤 |
| CA2927917C (en) | 2013-10-18 | 2022-08-09 | Syros Pharmaceuticals, Inc. | Heteroaromatic compounds useful for the treatment of proliferative diseases |
| US9415049B2 (en) | 2013-12-20 | 2016-08-16 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| EP3489232A3 (en) | 2014-04-04 | 2019-07-31 | Syros Pharmaceuticals, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| US9862688B2 (en) | 2014-04-23 | 2018-01-09 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged janus kinase inhibitors and uses thereof |
| US10017477B2 (en) | 2014-04-23 | 2018-07-10 | Dana-Farber Cancer Institute, Inc. | Janus kinase inhibitors and uses thereof |
| WO2016020791A1 (en) * | 2014-08-05 | 2016-02-11 | Novartis Ag | Ckit antibody drug conjugates |
| ES2741785T3 (es) | 2014-08-13 | 2020-02-12 | Celgene Car Llc | Formas y composiciones de un inhibidor de ERK |
| EP3236959B1 (en) | 2014-12-23 | 2025-09-24 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| CA2978518C (en) | 2015-03-27 | 2023-11-21 | Nathanael S. Gray | Inhibitors of cyclin-dependent kinases |
| CA2986441A1 (en) | 2015-06-12 | 2016-12-15 | 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 |
| MA46205A (fr) * | 2016-09-08 | 2019-07-17 | Sabila Biosciences Llc | Composés 1,2-dithiolane utiles dans la neuroprotection, les maladies et les états auto-immuns et cancéreux |
| 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 |
| 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 |
| CN110831936B (zh) | 2017-06-20 | 2023-03-28 | 特殊治疗有限公司 | 具有dub抑制剂活性的取代氰基吡咯烷 |
| WO2019236890A1 (en) * | 2018-06-07 | 2019-12-12 | 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 |
| WO2020005807A1 (en) | 2018-06-25 | 2020-01-02 | Dana-Farber Cancer Institute, Inc. | Taire family kinase inhibitors and uses thereof |
| 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 |
| MX2022014429A (es) | 2020-05-28 | 2022-12-07 | Mission Therapeutics Ltd | N-cianopirrolidinas con actividad como inhibidores de usp30. |
| US20230303547A1 (en) | 2020-06-04 | 2023-09-28 | Mission Therapeutics Limited | N-cyanopyrrolidines with activity as usp30 inhibitors |
| HUE072598T2 (hu) | 2020-06-08 | 2025-11-28 | Mission Therapeutics Ltd | 1-(5-(2-cianopiridin-4-il)oxazol-2-karbonil)-4-metilhexahidropirrolo[3,4-B]pirrol-5(1H)-karbonitril felhasználásra, mint USP30 inhibitor, mitokondriális diszfunkció, rák és fibrózisok kezelésében |
| GB202016800D0 (en) | 2020-10-22 | 2020-12-09 | Mission Therapeutics Ltd | Novel compounds |
| EP4441044A1 (en) | 2021-12-01 | 2024-10-09 | Mission Therapeutics Limited | Substituted n-cyanopyrrolidines with activity as usp30 inhibitors |
| CA3260486A1 (en) * | 2022-07-19 | 2024-01-25 | Chiesi Farm Spa | HETEROARYL DERIVATIVES USED AS DDR 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 |
| CA2446939C (en) * | 2001-05-16 | 2005-08-02 | Matthias Stein-Gerlach | Pyridylpyrimidine derivatives as effective compounds against prion diseases |
| US6878697B2 (en) * | 2001-06-21 | 2005-04-12 | Ariad Pharmaceuticals, Inc. | Phenylamino-pyrimidines and uses thereof |
| PT1442024E (pt) | 2001-11-01 | 2008-06-12 | Janssen Pharmaceutica Nv | Derivados aminobenzamida como inibidores da glicogénio sintase quinase 3$g(b) |
| CA2463822A1 (en) * | 2001-11-01 | 2003-05-08 | Janssen Pharmaceutica N.V. | Heteroaryl amines as glycogen synthase kinase 3beta inhibitors (gsk3 inhibitors) |
| 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 |
| WO2004013633A2 (en) * | 2002-07-29 | 2004-02-12 | Axxima Pharmaceuticals Ag | Method for isolating atp binding proteins by means of immobolized protein inhibitors |
| 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 |
| 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 |
| JPWO2005063709A1 (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 |
| DE602005023587D1 (de) | 2004-01-21 | 2010-10-28 | Univ Emory | Zusammensetzungen und verwendung von tyrosinkinase-hemmern zur behandlung von pathogenen infektionen |
| EP1751136B1 (en) * | 2004-05-07 | 2014-07-02 | 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 |
| CA2578122A1 (en) | 2004-08-27 | 2006-03-02 | Gpc Biotech Ag | Pyrimidine derivatives |
| KR101325424B1 (ko) | 2005-01-28 | 2013-11-04 | 노파르티스 아게 | Ｔｉｅ-2 키나제 활성의 조절에 반응하는 질환의 치료를위한 피리미딜아미노벤즈아미드의 용도 |
| MX2007011866A (es) | 2005-02-25 | 2007-10-10 | Novartis Ag | Combinacion farmaceutica de inhibidores de bcr-abl y raf. |
| 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 |
| CA2615579A1 (en) | 2005-07-20 | 2007-01-25 | Novartis Ag | Combination comprising a pyrimidylaminobenzamides and a flt-3 inhibitor for treating proliferative diseases |
| KR100674813B1 (ko) | 2005-08-05 | 2007-01-29 | 일양약품주식회사 | Ｎ-페닐-2-피리미딘-아민 유도체 및 그의 제조방법 |
| CN101321532B (zh) | 2005-12-06 | 2011-06-29 | 诺瓦提斯公司 | 用于治疗神经纤维瘤病的嘧啶基氨基苯甲酰胺衍生物 |
| KR20120049397A (ko) * | 2006-11-03 | 2012-05-16 | 노파르티스 아게 | 단백질 키나제 억제제로서의 화합물 및 조성물 |
| TWI433677B (zh) * | 2007-06-04 | 2014-04-11 | Avila Therapeutics Inc | 雜環化合物及其用途 |
| CN105574346A (zh) * | 2008-09-05 | 2016-05-11 | 新基阿维罗米克斯研究公司 | 多肽偶联物与不可逆抑制剂的设计方法和检测方法 |
-
2008
- 2008-06-03 TW TW097120571A patent/TWI433677B/zh active
- 2008-06-03 US US12/132,537 patent/US8242271B2/en not_active Expired - Fee Related
- 2008-06-03 CA CA2689989A patent/CA2689989A1/en not_active Abandoned
- 2008-06-03 EP EP08770044A patent/EP2152079A4/en not_active Withdrawn
- 2008-06-03 JP JP2010511276A patent/JP5526020B2/ja not_active Expired - Fee Related
- 2008-06-03 WO PCT/US2008/065646 patent/WO2008151183A1/en not_active Ceased
-
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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