DK3110409T3 - Jak1-inhibitorer til behandlingen af myelodysplastiske syndromer - Google Patents
Jak1-inhibitorer til behandlingen af myelodysplastiske syndromer Download PDFInfo
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- DK3110409T3 DK3110409T3 DK15710994.3T DK15710994T DK3110409T3 DK 3110409 T3 DK3110409 T3 DK 3110409T3 DK 15710994 T DK15710994 T DK 15710994T DK 3110409 T3 DK3110409 T3 DK 3110409T3
- Authority
- DK
- Denmark
- Prior art keywords
- pyrimidin
- pyrrolo
- pyrazol
- pharmaceutically acceptable
- acceptable salt
- Prior art date
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
Claims (33)
1. JAK-selektiv inhibitor valgt fra: 3- [l-(6-chlorpyridin-2-yl)pyrrolidin-3-yl]-3-[4-(7H-pyrrolo[2,3-d]pyrimidin- 4- yl)-lH-pyrazol-l-yl]propannitril; 3- (l-[l,3]oxazolo[5,4-b]pyridin-2-ylpyrrolidin-3-yl)-3-[4-(7H-pyrrolo[2,3- d]pyrimidin-4-yl)-lH-pyrazol-l-yl]propannitril; 4- [(4-{3-cyano-2-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-lH-pyrazol-l-yl]propyl}piperazin-l-yl)carbonyl]-3-fluorbenzonitril; 4-[(4-{3-cyano-2-[3-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-lH-pyrrol-l-yl]propyl}piperazin-l-yl)carbonyl]-3-fluorbenzonitril; {l-{l-[3-fluor-2-(trifluormethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-lH-pyrazol-l-yl]azetidin-3-yl}acetonitril; 4-{3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-lH-pyrazol-l-yl]azetidin-l-yl}-N-[4-fluor-2-(trifluormethyl)phenyl]piperidin-l-carboxamid; [3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-lH-pyrazol-l-yl]-l-(l-{[2-(trifluormethyl)pyrimidin-4-yl]carbonyl}piperidin-4-yl)azetidin-3-yl]acetonitril; /Trans-l-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-lH-pyrazol-l-yl]-3-(4-{ [2-(trifluormethyl)pyrimidin-4-yl]carbonyl}piperazin-l-yl)cyclobutyl]acetonitril; {trans-3-(4-{[4-[(3-hydroxyazetidin-l-yl)methyl]-6-(trifluormethyl)pyridin-2-yl]oxy}piperidin-l-yl)-l-[4-(7H-pyrrolo[2,3- d]pyrimidin-4-yl)-lH-pyrazol-l-yl]cyclobutyl}acetonitril; {trans-3-(4-{[4-{[(2S)-2-(hydroxymethyl)pyrrolidin-l-yl]methyl}-6-(trifluormethyl)pyridin-2-yl]oxy}piperidin-l-yl)-l-[4-(7H-pyrrolo[2,3- d]pyrimidin-4-yl)-lH-pyrazol-l-yl]cyclobutyl}acetonitril; {trans-3-(4-{[4-{[(2R)-2-(hydroxymethyl)pyrrolidin-l-yl]methyl}-6- (trifluormethyl)pyridin-2-yl]oxy}piperidin-l-yl)-l-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-lH-pyrazol-l-yl]cyclobutyl}acetonitril; 4- (4-{3-[(dimethylamino)methyl]-5-fluorphenoxy}piperidin-l-yl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-lH-pyrazol-l-yl]butannitril; 5- {3-(cyanomethyl)-3-[4-(7H-pyrrOlo[2,3-d]pyrimidin-4-yl)-l H-pyrazol-1-yl]azetidin-l-yl}-N-isopropylpyrazin-2-carboxamid; 4- {3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-lH-pyrazol-l-yl]azetidin-l-yl}-2,5-difluor-N-[(lS)-2,2,2-trifluor-l-methylethyl]benzamid; 5- {3-(cyanomethyl)-3-[4-(lH-pyrrolo[2,3-b]pyridin-4-yl)-lH-pyrazol-l-yl]azetidin-l-yl}-N-isopropylpyrazin-2-carboxamid; {l-(c/s-4-{[6-(2-hydroxyethyl)-2-(trifluormethyl)pyrimidin-4-yl]oxy}cyclohexyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-lH-pyrazol-l-yl]azetidin-3-yl}acetonitril; {l-(c/s-4-{[4-[(ethylamino)methyl]-6-(trifluormethyl)pyridin-2-yl]oxy}cyclohexyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-lH-pyrazol-l-yl]azetidin-3-yl}acetonitril; {l-(c/s-4-{[4-(l-hydroxy-l-methylethyl)-6-(trifluormethyl)pyridin-2-yl]oxy}cyclohexyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-lH-pyrazol-l-yl]azetidin-3-yl}acetonitril; {l-(c/s-4-{[4-{[(3R)-3-hydroxypyrrolidin-l-yl]methyl}-6-(trifluormethyl)pyridin-2-yl]oxy}cyclohexyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-lH-pyrazol-l-yl]azetidin-3-yl}acetonitril; {l-(c/s-4-{[4-{[(3S)-3-hydroxypyrrolidin-l-yl]methyl}-6-(trifluormethyl)pyridin-2-yl]oxy}cyclohexyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-lH-pyrazol-l-yl]azetidin-3-yl}acetonitril; {trans-3-(4-{[4-({[(lS)-2-hydroxy-l-methylethyl]amino}methyl)-6-(trifluormethyl)pyridin-2-yl]oxy}piperidin-l-yl)-l-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-lH-pyrazol-l-yl]cyclobutyl}acetonitril; {trans-3-(4-{[4-({[(2R)-2-hydroxypropyl]amino}methyl)-6-(trifluormethyl)pyridin-2-yl]oxy}piperidin-l-yl)-l-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-lH-pyrazol-l-yl]cyclobutyl}acetonitril; {trans-3-(4-{[4-({[(2S)-2-hydroxypropyl]amino}methyl)-6-(trifluormethyl)pyridin-2-yl]oxy}piperidin-l-yl)-l-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-lH-pyrazol-l-yl]cyclobutyl}acetonitril; og {trans-3-(4-{[4-(2-hydroxyethyl)-6-(trifluormethyl)pyridin-2-yl]oxy} piperidin-l-yl)-l-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-lH-pyrazol-l-yl]cyclobutyl}acetonitril; eller et farmaceutisk acceptabelt salt deraf, til anvendelse i en fremgangsmåde til behandling af et myelodysplastisk syndrom hos en patient med behov derfor, hvilken fremgangsmåde omfatter at administreres til patienten en terapeutisk effektiv mængde JAKl-selektiv inhibitor, eller et farmaceutisk acceptabelt salt deraf.
2. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge krav 1, hvor JAKl-selektiv-inhihitoren er selektiv for JAK1 over JAK2, JAK3, og TYK2.
3. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge krav 1 eller 2, hvor det myelodysplastiske syndrom er refraktorisk cytopæni med unilineær dysplasi (RCUD).
4. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge krav 1 eller 2, hvor det myelodysplastiske syndrom er refraktorisk anæmi med ring-sideroblaster (RARS).
5. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge krav 1 eller 2, hvor det myeloplastiske syndrom er refraktorisk cytopæni med multilineær dysplasi.
6. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge krav 1 eller 2, hvor det myelodysplastiske syndrom er refraktorisk anæmi med blastoverskud 1 (RAEB-1).
7. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge krav 1 eller 2, hvor det myelodysplastiske syndrom er refraktorisk anæmi med overskud af blasts-2 (RAEB-2).
8. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge krav 1 eller 2, hvor det myelodysplastiske syndrom er myelodysplastisk syndrom, ikke-klassificeret (MDS-U).
9. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge krav 1 eller 2, hvor det myelodysplastiske syndrom er myelodysplastisk syndrom associeret med isoleret del (5q).
10. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge krav 1 eller 2, hvor det myelodysplastiske syndrom er refraktorisk til erythropoiese-stimulerende midler.
11. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge et hvilket som helst af kravene 1 til 10, hvor patienten er rød blodlegeme-transfusionsafhængig.
12. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge et hvilket som helst af kravene 1 til 11, hvor fremgangsmåden yderligere omfatter administrering af et yderligere terapeutisk middel valgt fra et IMiD-, et anti-IL-6-middel, et anti-TNF-a-middel, et hypomethyleringsmiddel, eller et biologisk respons-modificeringsmiddel (BRM).
13. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge krav 12, hvor anti-TNF-a-midlet er valgt fra infliximab og etanercept.
14. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge krav 12, hvor hypomethyleringsmidlet er en DNA-methyltransferaseinhibitor.
15. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge krav 14, hvor DNA-methyltransferaseinhibitoren er valgt fra 5-azacytidin og decitabin.
16. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge krav 12, hvor IMiD er valgt fra thalidomid, lenalidomid, pomalidomid, CC-11006, og CC-10015.
17. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge et hvilket som helst af kravene 1 til 11, hvor fremgangsmåden yderligere omfatter administrering af et yderligere terapeutisk middel valgt fra anti-thymocytglobulin, rekombinant human granulocyt-koloni-stimulerende faktor (G CSF), granulocyt-monocyt CSF (GM-CSF), et erythropoiese-stimuleringsmiddel (ESA), og cyclosporin.
18. JAK1 selektiv inhibitor som er {l-{l-[3-fluor-2-(trifluormethyl)isonicotinoyl]-piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-lH-pyrazol-l-yl]azetidin-3-yl}acetonitril, eller et farmaceutisk acceptabelt salt deraf, til anvendelse i en fremgangsmåde til behandling af et myelodysplastisk syndrom hos en patient med behov derfor.
19. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge krav 18, hvor det myelodysplastiske syndrom er refraktorisk cytopæni med unilineær dysplasi (RCUD).
20. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge krav 18, hvor det myelodysplastiske syndrom er refraktorisk anæmi med ring-sideroblaster (RARS).
21. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge krav 18, hvor det myelodysplastiske syndrom er refraktorisk cytopæni med multilineær dysplasi.
22. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge krav 18, hvor det myelodysplastiske syndrom er refraktorisk anæmi med overskud af blasts-1 (RAEB-1).
23. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge krav 18, hvor det myelodysplastiske syndrom er refraktorisk anæmi med overskud af blasts-2 (RAEB-2).
24. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge krav 18, hvor det myelodysplastiske syndrom er myelodysplastisk syndrom, ikke-klassificeret (MDS-U).
25. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge krav 18, hvor det myelodysplastiske syndrom er myelodysplastisk syndrom associeret med isoleret del (5q).
26. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge krav 18, hvor det myelodysplastiske syndrom er refraktorisk til erythropoiese-stimuleringsmidler.
27. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge et hvilket som helst af kravene 18 til 26, hvor patienten er rød blodlegeme-transfusionsafhængig.
28. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge et hvilket som helst af kravene 18 til 27, hvor fremgangsmåden yderligere omfatter administrering af et yderligere terapeutisk middel valgt fra et IMiD-, et anti-IL-6-middel, et anti-TNF-a-middel, et hypomethyleringsmiddel, eller et biologisk respons-modificeringsmiddel (BRM).
29. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge krav 28, hvor anti-TNF-a-midlet er valgt fra infliximab og etanercept.
30. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge krav 28, hvor hypomethyleringsmidlet er en DNA-methyltransferaseinhibitor.
31. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge krav 30, hvor DNA-methyltransferaseinhibitoren er valgt fra 5-azacytidin og decitabin.
32. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge krav 28, hvor IMiD er valgt fra thalidomid, lenalidomid, pomalidomid, CC-11006, og CC-10015.
33. JAKl-selektiv-inhihitoren, eller et farmaceutisk acceptabelt salt deraf, til anvendelse ifølge et hvilket som helst af kravene 18 til 27, hvor fremgangsmåden yderligere omfatter administrering af et yderligere terapeutisk middel valgt fra anti-thymocytglobulin, rekombinant human granulocyt-koloni-stimulerende faktor (G CSF), granulocyt-monocyt CSF (GM-CSF), et erythropoiese-stimuleringsmiddel (ESA), og cyclosporin.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201461946124P | 2014-02-28 | 2014-02-28 | |
PCT/US2015/017963 WO2015131031A1 (en) | 2014-02-28 | 2015-02-27 | Jak1 inhibitors for the treatment of myelodysplastic syndromes |
Publications (1)
Publication Number | Publication Date |
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DK3110409T3 true DK3110409T3 (da) | 2018-10-22 |
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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DK15710994.3T DK3110409T3 (da) | 2014-02-28 | 2015-02-27 | Jak1-inhibitorer til behandlingen af myelodysplastiske syndromer |
Country Status (28)
Country | Link |
---|---|
US (4) | US20150246046A1 (da) |
EP (1) | EP3110409B1 (da) |
JP (1) | JP6576941B2 (da) |
KR (1) | KR20160136323A (da) |
CN (2) | CN112494652A (da) |
AU (1) | AU2015222913B2 (da) |
CA (1) | CA2940659C (da) |
CL (1) | CL2016002144A1 (da) |
CR (1) | CR20160449A (da) |
CY (1) | CY1120857T1 (da) |
DK (1) | DK3110409T3 (da) |
EA (1) | EA201691745A1 (da) |
ES (1) | ES2688553T3 (da) |
HR (1) | HRP20181661T1 (da) |
HU (1) | HUE041456T2 (da) |
IL (1) | IL247475B (da) |
LT (1) | LT3110409T (da) |
MX (1) | MX2016011103A (da) |
MY (1) | MY185392A (da) |
PE (1) | PE20161388A1 (da) |
PL (1) | PL3110409T3 (da) |
PT (1) | PT3110409T (da) |
RS (1) | RS57723B1 (da) |
SG (2) | SG11201607083VA (da) |
SI (1) | SI3110409T1 (da) |
UA (1) | UA121857C2 (da) |
WO (1) | WO2015131031A1 (da) |
ZA (1) | ZA201606610B (da) |
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SG176111A1 (en) | 2009-05-22 | 2011-12-29 | Incyte Corp | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors |
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SG10201705662WA (en) | 2013-01-15 | 2017-08-30 | Incyte Corp | Thiazolecarboxamides and pyridinecarboxamide compounds useful as pim kinase inhibitors |
CN105189509B (zh) | 2013-03-06 | 2017-12-19 | 因赛特公司 | 用于制备jak抑制剂的方法及中间体 |
TR201905814T4 (tr) | 2013-05-17 | 2019-05-21 | Incyte Corp | Jak inhibitörü olarak bipirazol tuzu. |
RS60469B1 (sr) | 2013-08-07 | 2020-07-31 | Incyte Corp | Dozni oblici sa produženim oslobađanjem za jak1 inhibitor |
PE20160532A1 (es) | 2013-08-23 | 2016-05-21 | Incyte Corp | Compuesto de carboxamida de furo y tienopiridina utiles como inhibidores de cinasas pim |
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