JP2014505735A5 - - Google Patents
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- JP2014505735A5 JP2014505735A5 JP2013554626A JP2013554626A JP2014505735A5 JP 2014505735 A5 JP2014505735 A5 JP 2014505735A5 JP 2013554626 A JP2013554626 A JP 2013554626A JP 2013554626 A JP2013554626 A JP 2013554626A JP 2014505735 A5 JP2014505735 A5 JP 2014505735A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- composition according
- formula
- compound
- mtor inhibitor
- 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.)
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- 239000008194 pharmaceutical composition Substances 0.000 claims 24
- 229940124302 mTOR inhibitor Drugs 0.000 claims 15
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims 15
- 150000001875 compounds Chemical class 0.000 claims 12
- 206010028980 Neoplasm Diseases 0.000 claims 8
- 206010028537 myelofibrosis Diseases 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 6
- 239000002552 dosage form Substances 0.000 claims 6
- 208000003476 primary myelofibrosis Diseases 0.000 claims 6
- 230000002062 proliferating effect Effects 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 5
- MFAQYJIYDMLAIM-UHFFFAOYSA-N torkinib Chemical compound C12=C(N)N=CN=C2N(C(C)C)N=C1C1=CC2=CC(O)=CC=C2N1 MFAQYJIYDMLAIM-UHFFFAOYSA-N 0.000 claims 5
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 4
- HFNKQEVNSGCOJV-OAHLLOKOSA-N ruxolitinib Chemical compound C1([C@@H](CC#N)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)CCCC1 HFNKQEVNSGCOJV-OAHLLOKOSA-N 0.000 claims 4
- HKVAMNSJSFKALM-GKUWKFKPSA-N Everolimus Chemical group C1C[C@@H](OCCO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 HKVAMNSJSFKALM-GKUWKFKPSA-N 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- -1 7H-pyrrolo [2,3-d] pyrimidin-4-yl Chemical group 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 208000033833 Myelomonocytic Chronic Leukemia Diseases 0.000 claims 2
- 208000037538 Myelomonocytic Juvenile Leukemia Diseases 0.000 claims 2
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 2
- 208000033755 Neutrophilic Chronic Leukemia Diseases 0.000 claims 2
- 201000008736 Systemic mastocytosis Diseases 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 208000035269 cancer or benign tumor Diseases 0.000 claims 2
- 208000021668 chronic eosinophilic leukemia Diseases 0.000 claims 2
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims 2
- 201000010903 chronic neutrophilic leukemia Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 125000001475 halogen functional group Chemical group 0.000 claims 2
- 206010020718 hyperplasia Diseases 0.000 claims 2
- 201000005992 juvenile myelomonocytic leukemia Diseases 0.000 claims 2
- 239000002207 metabolite Substances 0.000 claims 2
- FVSKHRXBFJPNKK-UHFFFAOYSA-N propionitrile Chemical compound CCC#N FVSKHRXBFJPNKK-UHFFFAOYSA-N 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- 101100480622 Caenorhabditis elegans tat-5 gene Proteins 0.000 claims 1
- 229960005167 everolimus Drugs 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 230000027405 negative regulation of phosphorylation Effects 0.000 claims 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161444581P | 2011-02-18 | 2011-02-18 | |
| US61/444,581 | 2011-02-18 | ||
| US201161503785P | 2011-07-01 | 2011-07-01 | |
| US201161503789P | 2011-07-01 | 2011-07-01 | |
| US61/503,789 | 2011-07-01 | ||
| US61/503,785 | 2011-07-01 | ||
| PCT/US2012/025581 WO2012112847A1 (en) | 2011-02-18 | 2012-02-17 | mTOR/JAK INHIBITOR COMBINATION THERAPY |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014505735A JP2014505735A (ja) | 2014-03-06 |
| JP2014505735A5 true JP2014505735A5 (enExample) | 2015-03-12 |
| JP5936628B2 JP5936628B2 (ja) | 2016-06-22 |
Family
ID=45755586
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013554626A Active JP5936628B2 (ja) | 2011-02-18 | 2012-02-17 | ｍＴＯＲ／ＪＡＫ阻害剤併用療法 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US9993480B2 (enExample) |
| EP (1) | EP2675451B9 (enExample) |
| JP (1) | JP5936628B2 (enExample) |
| KR (1) | KR102024948B1 (enExample) |
| CN (1) | CN103732226B (enExample) |
| AU (1) | AU2012219395B2 (enExample) |
| BR (1) | BR112013020798B1 (enExample) |
| CA (1) | CA2827673C (enExample) |
| EA (1) | EA026317B1 (enExample) |
| ES (1) | ES2547916T3 (enExample) |
| MX (1) | MX357939B (enExample) |
| PL (1) | PL2675451T3 (enExample) |
| PT (1) | PT2675451E (enExample) |
| WO (1) | WO2012112847A1 (enExample) |
Families Citing this family (49)
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| TWI630207B (zh) | 2005-12-13 | 2018-07-21 | 英塞特控股公司 | 作為傑納斯激酶（ＪＡＮＵＳ ＫＩＮＡＳＥ）抑制劑之經雜芳基取代之吡咯并〔２，３-ｂ〕吡啶及吡咯并〔２，３-ｂ〕嘧啶 |
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| EP3070090B1 (en) | 2007-06-13 | 2018-12-12 | Incyte Holdings Corporation | Use of salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3- cyclopentylpropanenitrile |
| TWI665200B (zh) | 2009-01-15 | 2019-07-11 | 英塞特公司 | 製造ｊａｋ抑制劑之方法及相關中間化合物 |
| EP3643312A1 (en) | 2009-05-22 | 2020-04-29 | Incyte Holdings Corporation | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors |
| AR076794A1 (es) | 2009-05-22 | 2011-07-06 | Incyte Corp | Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen |
| AR078012A1 (es) | 2009-09-01 | 2011-10-05 | Incyte Corp | Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus |
| EP3050882B1 (en) | 2010-03-10 | 2018-01-31 | Incyte Holdings Corporation | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
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| CN103415515B (zh) | 2010-11-19 | 2015-08-26 | 因塞特公司 | 作为jak抑制剂的环丁基取代的吡咯并吡啶和吡咯并嘧啶衍生物 |
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| AU2013337824B2 (en) | 2012-11-01 | 2018-03-08 | Incyte Holdings Corporation | Tricyclic fused thiophene derivatives as JAK inhibitors |
| PL2919766T3 (pl) | 2012-11-15 | 2021-10-04 | Incyte Holdings Corporation | Postacie dawkowania ruksolitynibu o przedłużonym uwalnianiu |
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| PT3773593T (pt) | 2018-03-30 | 2024-06-25 | Incyte Corp | Tratamento da hidradenite supurativa com inibidores de jak |
| EP3775284A1 (en) | 2018-03-30 | 2021-02-17 | Incyte Corporation | Biomarkers for inflammatory skin disease |
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| IL282643B2 (en) | 2018-10-31 | 2025-08-01 | Incyte Corp | A selective jak1 inhibitor for use in a method of treating hematological disease |
| WO2021013942A1 (en) * | 2019-07-24 | 2021-01-28 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of myeloperoxidase inhibitors for the treatment of cardiovascular diseases in patients suffering from myeloproliferative neoplasms |
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