HRP20200934T1 - Kruti oblici i formulacije (s)-4-(8-amino-3-(1-(but-2-inoil)pirolidin-2-il)imidazo[1,5-a]pirazin-1-il)-n-(piridin-2-il)benzamida - Google Patents

Kruti oblici i formulacije (s)-4-(8-amino-3-(1-(but-2-inoil)pirolidin-2-il)imidazo[1,5-a]pirazin-1-il)-n-(piridin-2-il)benzamida Download PDF

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HRP20200934T1
HRP20200934T1 HRP20200934TT HRP20200934T HRP20200934T1 HR P20200934 T1 HRP20200934 T1 HR P20200934T1 HR P20200934T T HRP20200934T T HR P20200934TT HR P20200934 T HRP20200934 T HR P20200934T HR P20200934 T1 HRP20200934 T1 HR P20200934T1
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cancer
preparation according
pyrazin
imidazo
pyrrolidin
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HRP20200934TT
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Tim INGALLINERA
Tjeerd A. Barf
Edwin Aret
Cecile Krejsa
Jerry Evarts
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Acerta Pharma B.V.
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Publication of HRP20200934T1 publication Critical patent/HRP20200934T1/hr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • 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
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Claims (17)

1. Pripravak koji sadrži slobodnu bazu kristalnog (S)-4-(8-amino-3-(1-(but-2-inoil)pirolidin-2-il)imidazo[1,5-a]pirazin-1-il)-N-(piridin-2-il)benzamida pri čemu je slobodna baza kristalnog (S)-4-(8-amino-3-(1-(but-2-inoil)pirolidin-2-il)imidazo[1,5-a]pirazin-1-il)-N-(piridin-2-il)benzamida naznačena time što ima prijenos uzorka rendgenske difrakcije praha koji sadrži vrhove kod 6.4, 8.6, 10.5, 11.6, i 15.7 °2θ ± 0.2 °2θ, pri čemu je uzorak rendgenske difrakcije praha dobiven korištenjem izvora Cu-Kα1 zračenja.
2. Pripravak prema patentnom zahtjevu 1, pri čemu je slobodna baza kristalnog (S)-4-(8-amino-3-(1-(but-2-inoil)pirolidin-2-il)imidazo[1,5-a]pirazin-1-il)-N-(piridin-2-il)benzamida naznačena time što ima prijenos uzorka rendgenske difrakcije praha koji dalje sadrži vrhove kod 10.9, 12.7, 13.4, 14.3, 14.9, i 18.2 °2θ ± 0.2 °2θ, pri čemu je uzorak rendgenske difrakcije praha dobiven korištenjem izvora Cu-Kα1 zračenja.
3. Pripravak prema bilo kojem od patentnih zahtjeva 1 ili 2, pri čemu je slobodna baza kristalnog (S)-4-(8-amino-3-(1-(but-2-inoil)pirolidin-2-il)imidazo[1,5-a]pirazin-1-il)-N-(piridin-2-il)benzamida naznačena time što ima prijenos uzorka rendgenske difrakcije praha koji dalje sadrži jedan ili više vrhova odabranih iz skupine koja se sastoji od 11.3, 15.1, 16.1, 17.3, 19.2, 19.4, 19.8, 20.7, 21.1, 21.4, 21.6, 21.9, 22.6, 23.3, 23.6, 24.9, 25.2, 25.4, 25.7, 26.1, 26.4, 26.8, 26.9, 27.7, 28.6, 29.1, 29.4, 30.1, 30.5, 31.7, 31.9, 32.2, 32.6, 33.1, 33.4, 34.5, 35.9, 36.1, 36.8, 37.4, 38.1, 38.9, i 39.5 °2θ ± 0.2 °2θ, pri čemu je uzorak rendgenske difrakcije praha dobiven korištenjem izvora Cu-Kα1 zračenja.
4. Pripravak prema bilo kojem od patentnih zahtjeva 1 do 3, pri čemu je slobodna baza kristalnog (S)-4-(8-amino-3-(1-(but-2-inoil)pirolidin-2-il)imidazo[1,5-a]pirazin-1-il)-N-(piridin-2-il)benzamida naznačena time što ima Ramanov spektar koji sadrži vrhove kod 1620, 1609, 1547, 1514, i 1495 cm-1 ± 2 cm-1.
5. Pripravak prema patentnom zahtjevu 4, pri čemu je slobodna baza kristalnog (S)-4-(8-amino-3-(1-(but-2-inoil)pirolidin-2-il)imidazo[1,5-a]pirazin-1-il)-N-(piridin-2-il)benzamida naznačena time što ima Ramanov spektar koji dalje sadrži jedan ili više vrhova odabranih iz skupine koja se sastoji od 1680, 1574, 1454, 1433, 1351, 1312, 1255, 1232, 1187, 1046, 995, 706, 406, i 280 cm-1 ± 2 cm-1.
6. Pripravak prema bilo kojem od patentnih zahtjeva 1 do 5, pri čemu je slobodna baza kristalnog (S)-4-(8-amino-3-(1-(but-2-inoil)pirolidin-2-il)imidazo[1,5-a]pirazin-1-il)-N-(piridin-2-il)benzamida naznačena time što ima infracrveni (IR) spektar koji sadrži vrhove kod 1621, 1608, 1403, 1303, i 764 cm-1 ± 4 cm-1.
7. Pripravak prema patentnom zahtjevu 6, pri čemu je slobodna baza kristalnog (S)-4-(8-amino-3-(1-(but-2-inoil)pirolidin-2-il)imidazo[1,5-a]pirazin-1-il)-N-(piridin-2-il)benzamida naznačena time što ima IR spektar koji dalje uključuje jedan ili više vrhova odabranih iz skupine koja se sastoji od 3367, 3089, 2246, 1682, 1574, 1514, 1504, 1454, 1428, 1345, 1248, 1194, 1177, 1149, 1109, 1049, 1023, 1003, 947, 900, 858, 842, 816, 734, 729, 701, 689, 665, 623, i 612 cm-1 ± 4 cm-1.
8. Pripravak prema bilo kojem od patentnih zahtjeva 1 do 7, pri čemu je slobodna baza kristalnog (S)-4-(8-amino-3-(1-(but-2-inoil)pirolidin-2-il)imidazo[1,5-a]pirazin-1-il)-N-(piridin-2-il)benzamida, te je dodatno naznačen nepostojanjem vode u kristalnoj strukturi.
9. Pripravak prema bilo kojem od patentnih zahtjeva 1 do 8, naznačen time što nadalje sadrži ekstra granularni acidulant.
10. Pripravak prema patentnom zahtjevu 9, naznačen time što je ekstra granularni acidulant izabran iz skupine koja se sastoji od fumarne kiseline, jantarne kiseline, -vinske kiseline, L-vinske kiseline, racemske vinske kiseline, askorbinske kiseline, izaskorbinske kiseline (poznate i kao eritorbinska kiselina i D-araboaskorbinska kiselina), alginske kiseline ili njihove soli, Protacid F 120 NM, Protacid AR 1112 (također poznat kao Kelacid NF), i Carbopol 971P (karboksipolimetilen), i njihovih kombinacija.
11. Pripravak prema patentnom zahtjevu 9, naznačen time što je ekstra granularni acidulant alginska kiselina, ili njezina natrijeva ili kalijeva sol, u koncentraciji između 5% do 33% težinski.
12. Pripravak prema bilo kojem od patentnih zahtjeva 1 do 11, naznačen time što pripravak nadalje sadrži najmanje jednu farmaceutski prihvatljivu pomoćnu tvar.
13. Pripravak prema patentnom zahtjevu 12 naznačen time što se upotrebljava u liječenju hiperproliferativne bolesti, pri čemu je hiperproliferativna bolest odabrana iz skupine koja sadrži kroničnu limfocitnu leukemiju, ne-Hodgkinov limfom, difuzni veliki B-stanični limfom, limfom plaštenih stanica, folikularni limfom, B limfoproliferativnu bolest B-stanica, akutnu limfoblastičnu leukemiju B-stanica, Waldenstromovu makroglobulinemiju, Burkittovu leukemiju, Hodgkinovu bolest, multipli mijelom, akutnu mijeloičnu leukemiju, juvenilnu mijelomonocitnu leukemiju, leukemiju vlasastih stanica, mastocitnu leukemiju, mastocitozu, mijeloproliferativne poremećaje (MPD), mijeloproliferativne neoplazme, policitemija vera (PV), esencijalnu trombocitemiju (ET), primarnu mijelofibrozu (PMF), mijelodisplastični sindrom, kroničnu mijeloičnu leukemiju (BCR-ABL1-pozitivna), kroničnu neutrofilnu leukemiju, kroničnu eozinofilnu leukemiju, limfom primarnog središnjeg živčanog sustava (CNS), primarni multifokalni limfom perifernog živčanog sustava (PNS), rak timusa, rak mozga, glioblastom, rak pluća, karcinom skvamoznih stanica, rak kože (npr., melanom), rak očiju, retinoblastom, intraokularni melanom, karcinom usne šupljine i orofarinksa, rak mokraćnog mjehura, rak želuca, karcinom gušterače, karcinom dojke, rak grlića maternice, rak glave i vrata, renalni karcinom, rak bubrega, rak jetre, rak jajnika, rak prostate, rak debelog crijeva, rak kostiju (npr., metastatski rak kostiju), rak jednjaka, rak testisa, ginekološki karcinom, rak štitnjače, rak epidermoida, karcinom povezan s AIDS-om (npr., limfom), virusom izazvan karcinom grlića maternice (humani papiloma virus), nazofaringealni karcinom (virus Epstein-Barr), Kaposijev sarkom, primarni izljevni limfom (Kaposijev sarkom herpes virus), hepatocelularni karcinom (virusi hepatitisa B i hepatitisa C), leukemije T-stanica (virus ljudske leukemije stanica T tipa 1), benignu hiperplaziju kože, restenozu, benignu hipertrofiju prostate, angiogenezu tumora, kroničnu upalnu bolest, reumatoidni artritis, aterosklerozu, upalnu bolest crijeva, kožne bolesti poput psorijaze, ekcema i sklerodermije, dijabetes, dijabetičku retinopatiju, retinopatiju nedonoščadi, staračku makularnu degeneraciju, hemangiom, ulcerozni kolitis, atopijski dermatitis, pouchitis, spondiloartritis, uveitis, Behcetovu bolest, reumatsku polimialgiju, arteritis orijaških stanica, sarkoidozu, Kawasakijevu bolest, juvenilni idiopatski artritis, hidratenitis suppurativa, Sjögrenov sindrom, psorijatični artritis, juvenilni reumatoidni artritis, ankilozirajući spondilitis, Crohnovu bolest, lupus i lupusni nefritis.
14. Pripravak prema patentnom zahtjevu 12 naznačen time što se upotrebljava u liječenju hiperproliferativne bolesti, pri čemu je hiperproliferativna bolest kronična limfocitna leukemija.
15. Pripravak prema patentnom zahtjevu 12 naznačen time što se upotrebljava u liječenju hiperproliferativne bolesti, pri čemu je hiperproliferativna bolest limfom plaštenih stanica.
16. Pripravak prema patentnom zahtjevu 12 naznačen time što se upotrebljava u liječenju hiperproliferativne bolesti, pri čemu je hiperproliferativna bolest difuzni veliki B-stanični limfom.
17. Pripravak prema patentnom zahtjevu 12 naznačen time što se upotrebljava u liječenju hiperproliferativne bolesti, pri čemu je hiperproliferativna bolest folikularni limfom.
HRP20200934TT 2015-07-02 2020-06-10 Kruti oblici i formulacije (s)-4-(8-amino-3-(1-(but-2-inoil)pirolidin-2-il)imidazo[1,5-a]pirazin-1-il)-n-(piridin-2-il)benzamida HRP20200934T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201562188468P 2015-07-02 2015-07-02
US201562271708P 2015-12-28 2015-12-28
EP16735945.4A EP3317281B1 (en) 2015-07-02 2016-07-01 Solid forms and formulations of (s)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-n-(pyridin-2-yl)benzamide
PCT/IB2016/053988 WO2017002095A1 (en) 2015-07-02 2016-07-01 Solid forms and formulations of (s)-4-(8-amino-3-(1 -(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-n-(pyridin-2-yl)benzamide

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HRP20200934T1 true HRP20200934T1 (hr) 2020-09-18

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HRP20230417TT HRP20230417T1 (hr) 2015-07-02 2016-07-01 Kruti oblici i formulacije (s)-4-(8-amino-3-(1-(but-2-inoil)pirolidin-2-il)imidazo[1,5-a]pirazin-1-il)-n-(piridin-2-il)benzamida
HRP20211511TT HRP20211511T1 (hr) 2015-07-02 2016-07-01 Čvrsti oblici i formulacije (s)-4-(8-amino-3-(1-(but-2-inoil)pirolidin-2-il)imidazo[1,5-a]pirazin-1-il)-n-(piridin-2-il)benzamida
HRP20200934TT HRP20200934T1 (hr) 2015-07-02 2020-06-10 Kruti oblici i formulacije (s)-4-(8-amino-3-(1-(but-2-inoil)pirolidin-2-il)imidazo[1,5-a]pirazin-1-il)-n-(piridin-2-il)benzamida

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HRP20211511TT HRP20211511T1 (hr) 2015-07-02 2016-07-01 Čvrsti oblici i formulacije (s)-4-(8-amino-3-(1-(but-2-inoil)pirolidin-2-il)imidazo[1,5-a]pirazin-1-il)-n-(piridin-2-il)benzamida

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