CN103339134B - 三环吡咯并衍生物、它们的制备方法和它们作为激酶抑制剂的应用 - Google Patents
三环吡咯并衍生物、它们的制备方法和它们作为激酶抑制剂的应用 Download PDFInfo
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- CN103339134B CN103339134B CN201280006541.4A CN201280006541A CN103339134B CN 103339134 B CN103339134 B CN 103339134B CN 201280006541 A CN201280006541 A CN 201280006541A CN 103339134 B CN103339134 B CN 103339134B
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- formula
- compound
- methyl
- pyrrolo
- quinazoline
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- 0 CC(*)CC1=C(C(*)=O)C(PCC(*)=O)=C*1* Chemical compound CC(*)CC1=C(C(*)=O)C(PCC(*)=O)=C*1* 0.000 description 9
- XXAMFNNNPGXANE-NYYWCZLTSA-N C/C=C(/C(O)=O)\c(cc1)c(C)c2c1cnc(CSC)n2 Chemical compound C/C=C(/C(O)=O)\c(cc1)c(C)c2c1cnc(CSC)n2 XXAMFNNNPGXANE-NYYWCZLTSA-N 0.000 description 1
- TWMZQWXFZRNGKA-UHFFFAOYSA-N CC(C)(C)OC(NC(CC1)CCC1[n]1c(-c2nc(SC)ncc2CC2)c2c(C(OC)=O)c1)=O Chemical compound CC(C)(C)OC(NC(CC1)CCC1[n]1c(-c2nc(SC)ncc2CC2)c2c(C(OC)=O)c1)=O TWMZQWXFZRNGKA-UHFFFAOYSA-N 0.000 description 1
- FKGZSCFWHZJIAF-UHFFFAOYSA-N CCOC(c1c(C)[nH]c(-c2n3)c1CCc2cnc3SC)=O Chemical compound CCOC(c1c(C)[nH]c(-c2n3)c1CCc2cnc3SC)=O FKGZSCFWHZJIAF-UHFFFAOYSA-N 0.000 description 1
- JMVYZFNQFINKCP-TXEJJXNPSA-N CSc1nc(-c2c(CC3)c(C(N)=N)c[n]2[C@H](CC2)CC[C@H]2N)c3cn1 Chemical compound CSc1nc(-c2c(CC3)c(C(N)=N)c[n]2[C@H](CC2)CC[C@H]2N)c3cn1 JMVYZFNQFINKCP-TXEJJXNPSA-N 0.000 description 1
- DWNWCFXWCGHGEY-UHFFFAOYSA-N CSc1nc(c2c(cc3)c(CO)c[nH]2)c3cn1 Chemical compound CSc1nc(c2c(cc3)c(CO)c[nH]2)c3cn1 DWNWCFXWCGHGEY-UHFFFAOYSA-N 0.000 description 1
- YQUFJQISWIFZLH-UHFFFAOYSA-N CSc1ncc(CCc2c-3[nH]cc2C(N)=O)c-3n1 Chemical compound CSc1ncc(CCc2c-3[nH]cc2C(N)=O)c-3n1 YQUFJQISWIFZLH-UHFFFAOYSA-N 0.000 description 1
- REMFNIZOGHOJHI-CUUXFQNZSA-N C[C@H](C(CCc(c1n2)cnc2SC)C1N)C(OC)=O Chemical compound C[C@H](C(CCc(c1n2)cnc2SC)C1N)C(OC)=O REMFNIZOGHOJHI-CUUXFQNZSA-N 0.000 description 1
- UECMCGVVQAQYOJ-UHFFFAOYSA-N C[n]1c(c2c(cc3)cnc(SC)n2)c3c(C(N)=O)c1 Chemical compound C[n]1c(c2c(cc3)cnc(SC)n2)c3c(C(N)=O)c1 UECMCGVVQAQYOJ-UHFFFAOYSA-N 0.000 description 1
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- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
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- Biomedical Technology (AREA)
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- Oncology (AREA)
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- Zoology (AREA)
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- Genetics & Genomics (AREA)
- Dermatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11152190.2 | 2011-01-26 | ||
| EP11152190 | 2011-01-26 | ||
| PCT/EP2012/050773 WO2012101032A1 (en) | 2011-01-26 | 2012-01-19 | Tricyclic pyrrolo derivatives, process for their preparation and their use as kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103339134A CN103339134A (zh) | 2013-10-02 |
| CN103339134B true CN103339134B (zh) | 2015-12-23 |
Family
ID=45562287
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280006541.4A Active CN103339134B (zh) | 2011-01-26 | 2012-01-19 | 三环吡咯并衍生物、它们的制备方法和它们作为激酶抑制剂的应用 |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US8975267B2 (https=) |
| EP (1) | EP2668190B1 (https=) |
| JP (2) | JP5925809B2 (https=) |
| CN (1) | CN103339134B (https=) |
| BR (1) | BR112013018515B1 (https=) |
| ES (1) | ES2602791T3 (https=) |
| RU (1) | RU2591191C2 (https=) |
| WO (1) | WO2012101032A1 (https=) |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| US8541576B2 (en) * | 2010-12-17 | 2013-09-24 | Nerviano Medical Sciences Srl | Substituted pyrazolo-quinazoline derivatives as kinase inhibitors |
| EP2668190B1 (en) | 2011-01-26 | 2016-08-17 | Nerviano Medical Sciences S.r.l. | Tricyclic pyrrolo derivatives, process for their preparation and their use as kinase inhibitors |
| GB201216018D0 (en) | 2012-09-07 | 2012-10-24 | Cancer Rec Tech Ltd | Pharmacologically active compounds |
| GB201216017D0 (en) | 2012-09-07 | 2012-10-24 | Cancer Rec Tech Ltd | Inhibitor compounds |
| ES2649156T3 (es) | 2013-01-14 | 2018-01-10 | Incyte Holdings Corporation | Compuestos bicíclicos de carboxamida aromática útiles como inhibidores de quinasas Pim |
| PE20191245A1 (es) | 2013-01-15 | 2019-09-18 | Incyte Holdings Corp | Compuestos de tiazolcarboxamidas y piridinacarboxamida utiles como inhibidores de quinasa pim |
| EA201690458A1 (ru) | 2013-08-23 | 2016-07-29 | Инсайт Корпорейшн | Фуро- и тиенопиридинкарбоксамиды, используемые в качестве ингибиторов pim-киназы |
| GB201403536D0 (en) * | 2014-02-28 | 2014-04-16 | Cancer Rec Tech Ltd | Inhibitor compounds |
| SG11201608303QA (en) | 2014-04-04 | 2016-11-29 | Del Mar Pharmaceuticals | Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer |
| CA2944610C (en) * | 2014-04-07 | 2024-01-09 | Netherlands Translational Research Center B.V. | (5,6-dihydro)pyrimido[4,5-e]indolizines |
| US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| US9822124B2 (en) | 2014-07-14 | 2017-11-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors |
| ES2966392T3 (es) | 2015-04-17 | 2024-04-22 | Crossfire Oncology Holding B V | Biomarcadores pronósticos para quimioterapia inhibidora de TTK |
| ITRM20150212A1 (it) * | 2015-05-15 | 2016-11-15 | Univ Degli Studi Di Palermo | 4,5,6,9-tetraidropirrolo[2',3':3,4] cicloepta[1,2-d] isossazoli, procedimento per la loro produzione e loro uso come antitumorali |
| WO2016196244A1 (en) | 2015-05-29 | 2016-12-08 | Incyte Corporation | Pyridineamine compounds useful as pim kinase inhibitors |
| BR112018000808A2 (pt) | 2015-07-16 | 2018-09-04 | Array Biopharma Inc | compostos de pirazolo[1,5-a]piridina substituída como inibidores de ret cinase |
| TWI734699B (zh) | 2015-09-09 | 2021-08-01 | 美商英塞特公司 | Pim激酶抑制劑之鹽 |
| CN105130980B (zh) * | 2015-09-09 | 2018-05-22 | 沈阳药科大学 | N-3-苯并咪唑噻唑胺类衍生物及其制备方法与应用 |
| US9920032B2 (en) | 2015-10-02 | 2018-03-20 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
| EP3368039A1 (en) | 2015-10-26 | 2018-09-05 | The Regents of The University of Colorado, A Body Corporate | Point mutations in trk inhibitor-resistant cancer and methods relating to the same |
| FI3439662T3 (fi) | 2016-04-04 | 2024-09-04 | Loxo Oncology Inc | (s)-n-(5-((r)-2-(2,5-difluorifenyyli)pyrrolidin-1-yyli)pyratsolo[1,5-a]pyrimidin-3-yyli)-3-hydroksipyrrolidiini-1-karboksamidin nesteformulaatioita |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| AU2017246547B2 (en) | 2016-04-04 | 2023-02-23 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| EP3458456B1 (en) | 2016-05-18 | 2020-11-25 | Loxo Oncology Inc. | Preparation of (s)-n-(5-((r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide |
| TWI752098B (zh) | 2016-10-10 | 2022-01-11 | 美商亞雷生物製藥股份有限公司 | 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
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| JP6118383B2 (ja) | 2017-04-19 |
| JP2016053042A (ja) | 2016-04-14 |
| EP2668190A1 (en) | 2013-12-04 |
| US9309253B2 (en) | 2016-04-12 |
| HK1189229A1 (zh) | 2014-05-30 |
| WO2012101032A1 (en) | 2012-08-02 |
| RU2013139353A (ru) | 2015-03-10 |
| BR112013018515A2 (pt) | 2016-10-18 |
| RU2591191C2 (ru) | 2016-07-10 |
| ES2602791T3 (es) | 2017-02-22 |
| JP5925809B2 (ja) | 2016-05-25 |
| US20130296305A1 (en) | 2013-11-07 |
| JP2014503567A (ja) | 2014-02-13 |
| EP2668190B1 (en) | 2016-08-17 |
| US20150141408A1 (en) | 2015-05-21 |
| BR112013018515B1 (pt) | 2021-06-29 |
| US8975267B2 (en) | 2015-03-10 |
| CN103339134A (zh) | 2013-10-02 |
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