JP2013523756A5 - - Google Patents
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- Publication number
- JP2013523756A5 JP2013523756A5 JP2013502782A JP2013502782A JP2013523756A5 JP 2013523756 A5 JP2013523756 A5 JP 2013523756A5 JP 2013502782 A JP2013502782 A JP 2013502782A JP 2013502782 A JP2013502782 A JP 2013502782A JP 2013523756 A5 JP2013523756 A5 JP 2013523756A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- chr
- occurrence
- alkyl
- independently
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 125000000217 alkyl group Chemical group 0.000 claims 56
- 125000000623 heterocyclic group Chemical group 0.000 claims 36
- 229910052739 hydrogen Inorganic materials 0.000 claims 18
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 17
- 229910052799 carbon Inorganic materials 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 13
- 125000004452 carbocyclyl group Chemical group 0.000 claims 11
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 10
- 125000003118 aryl group Chemical group 0.000 claims 10
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 9
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 9
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 8
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 6
- 125000003107 substituted aryl group Chemical group 0.000 claims 5
- -1 and N Inorganic materials 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000006620 amino-(C1-C6) alkyl group Chemical group 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000000172 Medulloblastoma Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 230000001093 anti-cancer Effects 0.000 claims 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 1
- 125000004618 benzofuryl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 210000001185 bone marrow Anatomy 0.000 claims 1
- 125000000609 carbazolyl group Chemical group C1(=CC=CC=2C3=CC=CC=C3NC12)* 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 231100000433 cytotoxic Toxicity 0.000 claims 1
- 230000001472 cytotoxic effect Effects 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 125000005956 isoquinolyl group Chemical group 0.000 claims 1
- 125000001786 isothiazolyl group Chemical group 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 201000008129 pancreatic ductal adenocarcinoma Diseases 0.000 claims 1
- LYKMMUBOEFYJQG-UHFFFAOYSA-N piperoxan Chemical compound C1OC2=CC=CC=C2OC1CN1CCCCC1 LYKMMUBOEFYJQG-UHFFFAOYSA-N 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 125000005493 quinolyl group Chemical group 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 230000001568 sexual effect Effects 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 125000004306 triazinyl group Chemical group 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31956210P | 2010-03-31 | 2010-03-31 | |
| US61/319,562 | 2010-03-31 | ||
| PCT/US2011/030437 WO2011123493A1 (en) | 2010-03-31 | 2011-03-30 | Substituted pyrrolotriazines as protein kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013523756A JP2013523756A (ja) | 2013-06-17 |
| JP2013523756A5 true JP2013523756A5 (https=) | 2014-05-15 |
| JP5752232B2 JP5752232B2 (ja) | 2015-07-22 |
Family
ID=44065331
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013502782A Expired - Fee Related JP5752232B2 (ja) | 2010-03-31 | 2011-03-30 | プロテインキナーゼ阻害剤としての置換ピロロトリアジン化合物 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US8791257B2 (https=) |
| EP (1) | EP2552922A1 (https=) |
| JP (1) | JP5752232B2 (https=) |
| CN (1) | CN102918045A (https=) |
| WO (1) | WO2011123493A1 (https=) |
Families Citing this family (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
| US20150087687A1 (en) | 2012-03-23 | 2015-03-26 | Dennis Brown | Compositions and methods to improve the therapeutic benefit of indirubin and analogs thereof, including meisoindigo |
| ES2704744T3 (es) | 2012-06-13 | 2019-03-19 | Incyte Holdings Corp | Compuestos tricíclicos sustituidos como inhibidores de FGFR |
| US8901305B2 (en) * | 2012-07-31 | 2014-12-02 | Bristol-Myers Squibb Company | Aryl lactam kinase inhibitors |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| EA035095B1 (ru) | 2013-04-19 | 2020-04-27 | Инсайт Холдингс Корпорейшн | Бициклические гетероциклы в качестве ингибиторов fgfr |
| US10253027B2 (en) * | 2013-07-08 | 2019-04-09 | Bristol-Myers Squibb Company | Aryl lactam kinase inhibitors |
| WO2015081783A1 (zh) * | 2013-12-06 | 2015-06-11 | 江苏奥赛康药业股份有限公司 | 吡咯并[2,1-f][1,2,4]三嗪类衍生物及其制备方法和用途 |
| US10214537B2 (en) * | 2014-10-22 | 2019-02-26 | Bristol-Myers Squibb Company | Bicyclic heteroaryl amine compounds |
| US10023576B2 (en) | 2014-10-22 | 2018-07-17 | Bristol-Myers Squibb Company | Heteroaryl substituted pyrrolotriazine amine compounds as PI3K inhibitors |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| MX373169B (es) | 2015-02-20 | 2020-04-24 | Incyte Holdings Corp | Heterociclos bicíclicos como inhibidores de receptores del factor de crecimiento fibroblástico (fgfr). |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| US10053465B2 (en) | 2015-08-26 | 2018-08-21 | Incyte Corporation | Pyrrolopyrimidine derivatives as TAM inhibitors |
| US9994679B2 (en) * | 2016-01-11 | 2018-06-12 | Industrial Technology Research Institute | Polymerization process of polyarylene sulfide |
| US10184028B2 (en) | 2016-01-11 | 2019-01-22 | Industrial Technology Research Institute | Method for preparing a polymer |
| US10287396B2 (en) | 2016-01-11 | 2019-05-14 | Industrial Technology Research Institute | Polymer |
| US10377705B2 (en) | 2016-01-11 | 2019-08-13 | Industrial Technology Research Institute | Method for preparing polyarylene sulfide (PAS) monomer |
| MD3436461T2 (ro) | 2016-03-28 | 2024-05-31 | Incyte Corp | Compuși pirolotriazină ca inhibitori TAM |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| SI3687996T1 (sl) | 2017-09-27 | 2022-04-29 | Incyte Corporation | Soli pirolotriazinskih derivatov, ki so uporabne kot zaviralci TAM |
| CN112262139B (zh) * | 2018-01-26 | 2023-07-25 | 百时美施贵宝公司 | 作为激酶抑制剂的氨基吡咯并三嗪 |
| CR20200590A (es) | 2018-05-04 | 2021-04-26 | Incyte Corp | Formas sólidas de un inhibidor de fgfr y procesos para prepararlas |
| MA52493A (fr) | 2018-05-04 | 2021-03-10 | Incyte Corp | Sels d'un inhibiteur de fgfr |
| MD3813800T2 (ro) | 2018-06-29 | 2025-10-31 | Incyte Corp | Formulări de inhibitor al AXL/MER |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| TWI891666B (zh) | 2019-10-14 | 2025-08-01 | 美商英塞特公司 | 作為ｆｇｆｒ抑制劑之雙環雜環 |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| BR112022010664A2 (pt) | 2019-12-04 | 2022-08-16 | Incyte Corp | Derivados de um inibidor de fgfr |
| EP4069696A1 (en) | 2019-12-04 | 2022-10-12 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| EP4114401A1 (en) | 2020-03-06 | 2023-01-11 | Incyte Corporation | Combination therapy comprising axl/mer and pd-1/pd-l1 inhibitors |
| TW202202506A (zh) | 2020-07-13 | 2022-01-16 | 中國商北京泰德製藥股份有限公司 | 作為atr激酶抑制劑的吡唑並嘧啶化合物 |
| TW202304459A (zh) | 2021-04-12 | 2023-02-01 | 美商英塞特公司 | 包含ｆｇｆｒ抑制劑及ｎｅｃｔｉｎ－４靶向劑之組合療法 |
| EP4352059A1 (en) | 2021-06-09 | 2024-04-17 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2022261159A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| CN115417892A (zh) * | 2022-09-30 | 2022-12-02 | 福州大学 | 一种异噁唑取代的硼氮杂环化合物及其合成方法 |
| CN120530116A (zh) * | 2022-11-04 | 2025-08-22 | 百时美施贵宝公司 | Ret-ldd蛋白抑制剂 |
| CN118184669B (zh) * | 2023-03-17 | 2025-09-23 | 北京伯汇生物技术有限公司 | 作为多靶点激酶抑制剂的大环化合物 |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2517034A1 (en) | 2003-03-13 | 2004-09-30 | Synta Pharmaceuticals Corp. | Fused pyrrole compounds |
| US7306631B2 (en) | 2004-03-30 | 2007-12-11 | The Procter & Gamble Company | Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof |
| US7514460B2 (en) | 2004-12-22 | 2009-04-07 | 4Sc Ag | Benzazole analogues and uses thereof |
| US7442700B2 (en) | 2005-07-01 | 2008-10-28 | Bristol-Myers Squibb Company | Pyrrolotriazine compounds useful as kinase inhibitors and methods of treating kinase-associated conditions therewith |
| US7514435B2 (en) * | 2005-11-18 | 2009-04-07 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| KR101461680B1 (ko) | 2005-12-02 | 2014-11-19 | 바이엘 헬스케어 엘엘씨 | 과다-증식성 장애 및 맥관형성과 관련된 질환의 치료에유용한 치환된 4-아미노-피롤로트리아진 유도체 |
| US7659274B2 (en) | 2006-01-25 | 2010-02-09 | Osi Pharmaceuticals, Inc. | Unsaturated mTOR inhibitors |
| CN101395158A (zh) | 2006-03-07 | 2009-03-25 | 百时美施贵宝公司 | 可作为激酶抑制剂的吡咯并三嗪苯胺前体药物化合物 |
| HRP20140688T1 (hr) | 2006-07-07 | 2014-10-24 | Bristol-Myers Squibb Company | Inhibitori piroltriazin kinaze |
| WO2008057402A2 (en) | 2006-11-02 | 2008-05-15 | Cytovia, Inc. | N-aryl-isoxazolopyrimidin-4-amines and related compounds as activators of caspases and inducers of apoptosis and the use thereof |
| SI2114980T1 (sl) | 2007-01-12 | 2012-11-30 | Biocryst Pharm Inc | Protivirusni nukleozidni analogi |
| CN101687874B (zh) | 2007-04-18 | 2013-01-30 | 百时美施贵宝公司 | 吡咯并三嗪激酶抑制剂 |
| US8124759B2 (en) * | 2007-05-09 | 2012-02-28 | Abbott Laboratories | Inhibitors of protein kinases |
| ES2413806T3 (es) | 2008-03-20 | 2013-07-17 | Amgen Inc. | Moduladores de la aurora cinasa y método de uso |
| EP2313102A2 (en) | 2008-07-03 | 2011-04-27 | Biota Scientific Management | Bycyclic nucleosides and nucleotides as therapeutic agents |
-
2011
- 2011-03-30 CN CN2011800266739A patent/CN102918045A/zh active Pending
- 2011-03-30 EP EP11714884A patent/EP2552922A1/en not_active Withdrawn
- 2011-03-30 WO PCT/US2011/030437 patent/WO2011123493A1/en not_active Ceased
- 2011-03-30 US US13/638,210 patent/US8791257B2/en active Active
- 2011-03-30 JP JP2013502782A patent/JP5752232B2/ja not_active Expired - Fee Related
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