HRP20200955T1 - Dozni oblici s produženim oslobađanjem za jak1 inhibitor - Google Patents
Dozni oblici s produženim oslobađanjem za jak1 inhibitor Download PDFInfo
- Publication number
- HRP20200955T1 HRP20200955T1 HRP20200955TT HRP20200955T HRP20200955T1 HR P20200955 T1 HRP20200955 T1 HR P20200955T1 HR P20200955T T HRP20200955T T HR P20200955TT HR P20200955 T HRP20200955 T HR P20200955T HR P20200955 T1 HRP20200955 T1 HR P20200955T1
- Authority
- HR
- Croatia
- Prior art keywords
- azetidin
- pyrazol
- pyrimidin
- trifluoromethyl
- fluoro
- Prior art date
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- 239000002552 dosage form Substances 0.000 title claims 41
- 238000013268 sustained release Methods 0.000 title claims 29
- 239000012730 sustained-release form Substances 0.000 title claims 29
- 229940116839 Janus kinase 1 inhibitor Drugs 0.000 title 1
- KTBSXLIQKWEBRB-UHFFFAOYSA-N 2-[1-[1-[3-fluoro-2-(trifluoromethyl)pyridine-4-carbonyl]piperidin-4-yl]-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-3-yl]acetonitrile Chemical compound C1=CN=C(C(F)(F)F)C(F)=C1C(=O)N1CCC(N2CC(CC#N)(C2)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)CC1 KTBSXLIQKWEBRB-UHFFFAOYSA-N 0.000 claims 50
- 150000003839 salts Chemical class 0.000 claims 42
- 230000036470 plasma concentration Effects 0.000 claims 16
- 239000012458 free base Substances 0.000 claims 12
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 9
- 238000013265 extended release Methods 0.000 claims 8
- 208000003476 primary myelofibrosis Diseases 0.000 claims 8
- 235000012054 meals Nutrition 0.000 claims 7
- 206010028537 myelofibrosis Diseases 0.000 claims 7
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 6
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 6
- 208000023275 Autoimmune disease Diseases 0.000 claims 5
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 5
- 229960003943 hypromellose Drugs 0.000 claims 5
- 238000000034 method Methods 0.000 claims 5
- 208000006386 Bone Resorption Diseases 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 125000004567 azetidin-3-yl group Chemical group N1CC(C1)* 0.000 claims 4
- 230000024279 bone resorption Effects 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 4
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims 4
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 3
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 3
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 3
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 3
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 3
- 239000008108 microcrystalline cellulose Substances 0.000 claims 3
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 claims 2
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 2
- 206010048643 Hypereosinophilic syndrome Diseases 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 201000008736 Systemic mastocytosis Diseases 0.000 claims 2
- 208000017733 acquired polycythemia vera Diseases 0.000 claims 2
- 208000019664 bone resorption disease Diseases 0.000 claims 2
- 208000010247 contact dermatitis Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 229960001021 lactose monohydrate Drugs 0.000 claims 2
- 235000019359 magnesium stearate Nutrition 0.000 claims 2
- 210000000056 organ Anatomy 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 208000037244 polycythemia vera Diseases 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- CEGWJIQFBNFMHQ-UHFFFAOYSA-N 2-[1-[1-[3-fluoro-2-(trifluoromethyl)pyridine-4-carbonyl]piperidin-4-yl]-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-3-yl]acetonitrile;hexanedioic acid Chemical group OC(=O)CCCCC(O)=O.C1=CN=C(C(F)(F)F)C(F)=C1C(=O)N1CCC(N2CC(CC#N)(C2)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)CC1 CEGWJIQFBNFMHQ-UHFFFAOYSA-N 0.000 claims 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 206010012442 Dermatitis contact Diseases 0.000 claims 1
- 208000010201 Exanthema Diseases 0.000 claims 1
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 108060003951 Immunoglobulin Proteins 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 1
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 206010028561 Myeloid metaplasia Diseases 0.000 claims 1
- 208000009525 Myocarditis Diseases 0.000 claims 1
- 208000001132 Osteoporosis 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
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 1
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 206010040880 Skin irritation Diseases 0.000 claims 1
- 208000024799 Thyroid disease Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 230000000172 allergic effect Effects 0.000 claims 1
- 208000007502 anemia Diseases 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- 239000002585 base Substances 0.000 claims 1
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims 1
- 201000005884 exanthem Diseases 0.000 claims 1
- 208000024908 graft versus host disease Diseases 0.000 claims 1
- 230000003054 hormonal effect Effects 0.000 claims 1
- 238000001794 hormone therapy Methods 0.000 claims 1
- 230000009610 hypersensitivity Effects 0.000 claims 1
- 102000018358 immunoglobulin Human genes 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 229960001375 lactose Drugs 0.000 claims 1
- 239000008101 lactose Substances 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 229940057948 magnesium stearate Drugs 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 206010037844 rash Diseases 0.000 claims 1
- 210000003491 skin Anatomy 0.000 claims 1
- 208000017520 skin disease Diseases 0.000 claims 1
- 230000036556 skin irritation Effects 0.000 claims 1
- 231100000475 skin irritation Toxicity 0.000 claims 1
- 231100000046 skin rash Toxicity 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 238000005550 wet granulation Methods 0.000 claims 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
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- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
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- 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
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- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
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- Bioinformatics & Cheminformatics (AREA)
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- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
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- Dermatology (AREA)
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- Endocrinology (AREA)
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- Oncology (AREA)
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- Urology & Nephrology (AREA)
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- Obesity (AREA)
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Claims (30)
1. {1-{1-[3-Fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegova farmaceutski prihvatljiva sol, za upotrebu u postupku liječenja autoimune bolesti, raka, mijeloproliferativnog poremećaja, upalne bolesti, bolesti resorpcije kostiju, odbacivanja transplanta organa kod pacijenta kojem je potrebno, koji obuhvaća oralno davanje spomenutom pacijentu jednom dnevno doze od 200 mg, 300 mg, ili 600 mg na osnovu slobodne baze {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il} acetonitrila, ili njegove farmaceutski prihvatljive soli, gdje doza sadrži jedan ili više doznih oblika s produženim oslobađanjem pri čemu svaki sadrži {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegovu farmaceutski prihvatljivu sol.
2. {1-{1-[3-Fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegova farmaceutski prihvatljiva sol, za upotrebu prema patentnom zahtjevu 1, gdje postupak obuhvaća davanje spomenutom pacijentu jednog ili više doznih oblika s produženim oslobađanjem kao jednodnevne doze od 600 mg na osnovi slobodne baze {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7Hpirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrila, ili njegove farmaceutski prihvatljive soli.
3. {1-{1-[3-Fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegova farmaceutski prihvatljiva sol, za upotrebu prema zahtjevu 1, gdje:-
a) jedan ili više doznih oblika s produženim oslobađanjem su šest doznih oblika od 100 mg na osnovi slobodne baze {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrila, ili njegove farmaceutski prihvatljive soli; ili
b) jedan ili više doznih oblika s produženim oslobađanjem su tri dozna oblika od 200 mg na osnovi slobodne baze {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrila, ili njegove farmaceutski prihvatljive soli; ili
c) jedan ili više doznih oblika s produženim oslobađanjem su dva dozna oblika od 300 mg na osnovi slobodne baze {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrila, ili njegove farmaceutski prihvatljive soli; ili
d) jedan ili više doznih oblika s produženim oslobađanjem je jedan dozni oblik od 600 mg na osnovi slobodne baze {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrila, ili njegove farmaceutski prihvatljive soli.
4. {1-{1-[3-Fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegova farmaceutski prihvatljiva sol, za upotrebu prema zahtjevu 1, gdje postupak obuhvaća davanje spomenutom pacijentu jednog ili više doznih oblika s produženim oslobađanjem kao jednodnevne doze od 200 mg na osnovi slobodne baze {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrila, ili njegove farmaceutski prihvatljive soli.
5. {1-{1-[3-Fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegova farmaceutski prihvatljiva sol, za upotrebu prema zahtjevu 1, gdje postupak obuhvaća davanje spomenutom pacijentu jednog ili više doznog oblika s produženim oslobađanjem kao jednodnevne doze od 300 mg na osnovi slobodne baze {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrila, ili njegove farmaceutski prihvatljive soli.
6. {1-{1-[3-Fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegova farmaceutski prihvatljiva sol, za upotrebu prema bilo kojem od zahtjeva 1 do 5, gdje spomenuta autoimuna bolest je kožni poremećaj, multipla skleroza, reumatoidni artritis, psorijazni artritis, juvenilni artritis, tip I dijabetesa, lupus, upalna bolest crijeva, Crohnova bolest, mijastenija gravis, imunoglobulinske nefropatije, miokarditis, autoimuni tiroidni poremećaj, atopijski dermatitis, psorijaza, preosjetljivost kože, iritacija kože, osip kože, kontaktni dermatitis ili alergijska kontaktna preosjetljivost.
7. {1-{1-[3-Fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegova farmaceutski prihvatljiva sol, za upotrebu prema bilo kojem od zahtjeva 1 do 5, gdje je spomenuta autoimuna bolest reumatoidni artritis.
8. {1-{1-[3-Fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegova farmaceutski prihvatljiva sol, za upotrebu prema bilo kojem od zahtjeva 1 do 5, gdje je spomenuta autoimuna bolest psorijaza.
9. {1-{1-[3-Fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegova farmaceutski prihvatljiva sol, za upotrebu prema bilo kojem od zahtjeva 1 do 5, gdje spomenuti rak je rak prostate, rak bubrega, rak jetre, rak dojke, rak pluća, rak štitnjače, Kaposijev sarkom, Castelmanova bolest, rak gušterače, limfom, leukemija, multipli mijelom, policitemija vera (PV), esencijalna trombocitemija (ET), mijeloidna metaplazija sa mijelofibrozom (MMM), primarna mijelofibroza (PMF), kronična mijelogena leukemija (CML), kronična mijelomonocitna leukemija (CMML), hipereozinofilni sindrom (HES), idiopatska mijelofibroza (IMF), ili sustavna bolest mastocita(SMCD).
10. {1-{1-[3-Fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegova farmaceutski prihvatljiva sol, za upotrebu prema bilo kojem od zahtjeva 1 do 5, gdje:-
a) spomenuti mijeloproliferativni poremećaj je primarna mijelofibroza (PMF); ili
b) spomenuti mijeloproliferativni poremećaj je primarna mijelofibroza (PMF) i spomenuti postupak dovodi do reducirane anemije.
11. {1-{1-[3-Fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegova farmaceutski prihvatljiva sol, za upotrebu prema bilo kojem od zahtjeva 1 do 5, gdje je spomenuta bolest transplanta organa odbacivanje alografta ili bolest presatka protiv domaćina.
12. {1-{1-[3-Fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegova farmaceutski prihvatljiva sol, za upotrebu prema bilo kojem od zahtjeva 1 do 3, gdje je spomenuta bolest resorpcije kostiju osteoporoza, osteoartritis, resorpcija kostiju povezana sa hormonskom neravnotežom, resorpcija kostiju povezana sa hormonalnom terapijom, resorpcija kostiju povezana sa autoimunom bolesti, ili resorpcija kostiju povezana sa rakom.
13. {1-{1-[3-Fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegova farmaceutski prihvatljiva sol, za upotrebu prema bilo kojem od zahtjeva 1 do 3, gdje:-
a) oralno davanje jednog ili više doznog oblika s produženim oslobađanjem pojedincu koji posti osigurava srednje vrijeme za maksimalnu koncentraciju u plazmi (Tmax) {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrila od 0.5 sati do 3 sati; ili
b) oralno davanje jednog ili više doznog oblika s produženim oslobađanjem pojedincu koji posti osigurava srednje vrijeme za maksimalnu koncentraciju u plazmi (Tmax) {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrila od najmanje 0.5 sati.
14. {1-{1-[3-Fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegova farmaceutski prihvatljiva sol, za upotrebu prema bilo kojem od zahtjeva 1 do 3, gdje:-
a) oralno davanje jednog ili više doznog oblika sa produženim oslobađanjem individui koja posti osigurava odnos srednje vrijednosti maksimalne koncentracije u plazmi (Cmax) do srednje vrijednosti 12-satne koncentracije u plazmi (C12h) {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrila od 5 do 50; ili
b) oralno davanje jednog ili više doznog oblika s produženim oslobađanjem pojedincu koji posti osigurava odnos srednje vrijednosti maksimalne koncentracije u plazmi (Cmax) do srednje vrijednosti 12-satne koncentracije u plazmi (C12h) {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrila od 9 do 40; ili
c) oralno davanje jednog ili više doznog oblika s produženim oslobađanjem pojedincu koji posti osigurava odnos srednje vrijednosti maksimalne koncentracije u plazmi (Cmax) do srednje vrijednosti 12-satne koncentracije u plazmi (C12h) {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrila od 15 do 30.
15. {1-{1-[3-Fluoro-2-(trifluorometil)izoniotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegova farmaceutski prihvatljiva sol, za upotrebu prema bilo kojem od zahtjeva 1 do 5, gdje: -
a) oralno davanje jednog ili više doznih oblika s produženim oslobađanjem pojedincu koji posti osigurava srednju vrijednost polu života (t1/2) {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrila od 1 h do 20 h; ili
b) oralno davanje jednog ili više doznih oblika s produženim oslobađanjem pojedincu poslije obroka bogatog mastima osigurava srednje vrijeme do maksimalne koncentracije u plazmi (Tmax) {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril od 1 h do 9 h; ili
c) oralno davanje jednog ili više doznih oblika s produženim oslobađanjem pojedincu poslije obroka bogatog mastima osigurava srednje vrijeme za maksimalnu koncentraciju u plazmi (Tmax) od {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrila od najmanje 1.5 h.
16. {1-{1-[3-Fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegova farmaceutski prihvatljiva sol, za upotrebu prema bilo kojem od zahtjeva 1 do 3, gdje:-
a) oralno davanje jednog ili više doznih oblika s produženim oslobađanjem poslije obroka bogatog mastima osigurava odnos srednje vrijednosti maksimalne koncentracije u plazmi (Cmax) prema srednjoj vrijednosti 12-satne koncentracije u plazmi (C12h) {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrila od 10 do 70; ili
b) oralno davanje jednog ili više doznih oblika s produženim oslobađanjem poslije obroka bogatog mastima osigurava odnos srednje vrijednosti maksimalne koncentracije u plazmi (Cmax) prema srednjoj vrijednosti 12-satne koncentracije u plazmi (C12h) {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrila od 15 do 50; ili
c) oralno davanje jednog ili više doznih oblika s produženim oslobađanjem poslije obroka bogatog mastima osigurava odnos srednje vrijednosti maksimalne koncentracije u plazmi (Cmax) prema srednjoj vrijednosti 12-satne koncentracije u plazmi (C12h) {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrila od 25 do 45.
17. {1-{1-[3-Fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegova farmaceutski prihvatljiva sol, za upotrebu prema bilo kojem od zahtjeva 1 do 3, gdje:-
a) oralno davanje jednog ili više doznih oblika s produženim oslobađanjem poslije obroka bogatog mastima osigurava srednju vrijednost polu-života (t1/2) {1-{1-[3-fluoro-2-(trifluorometil)izonilkotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrila od 1 h do 7 h; ili
b) oralno davanje jednog ili više doznih oblika s produženim oslobađanjem poslije obroka bogatog mastima osigurava srednju vrijednost polu-života (t1/2) {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrila od 2 h do 5 h.
18. {1-{1-[3-Fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegova farmaceutski prihvatljiva sol, za upotrebu prema bilo kojem od zahtjeva 1 do 3, gdje jedan ili više doznih oblika s produženim oslobađanjem su svaki tableta.
19. {1-{1-[3-Fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il} -3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegova farmaceutski prihvatljiva sol, za upotrebu prema bilo kojem od zahtjeva 1 do 3, gdje jedan ili više doznih oblika s produženim oslobađanjem su dobiveni postupkom koji obuhvaća vlažnu granulaciju.
20. {1-{1-[3-Fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegova farmaceutski prihvatljiva sol, za upotrebu prema bilo kojem od zahtjeva 1 to 3, gdje:-
a) jedan ili više doznih oblika s produženim oslobađanjem svaki sadrži jednu ili više od hipromeloza; ili
b) jedan ili više doznih oblika s produženim oslobađanjem svaki sadrži jedan ili više od pomoćnih tvari nezavisno izabranih od hipromeloza i mikrokristalnih celuloza.
21. {1-{1-[3-Fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegova farmaceutski prihvatljiva sol, za upotrebu prema bilo kojem od zahtjeva 1 do 3, gdje jedan ili više doznih oblika s produženim oslobađanjem svaki sadrži jedan ili više pomoćnih tvari nezavisno izabranih od hipromeloze, mikrokristalnih celuloza, magnezijevog stearata, laktoze, i monohidrat laktoze.
22. {1-{1-[3-Fluoro-2-(trifluorometil)izonikiotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegova farmaceutski prihvatljiva sol, za upotrebu prema bilo kojem od zahtjeva 1 do 15, gdje jedan ili više doznih oblika s produženim oslobađanjem svaki sadrži prvu hipromelozu naznačenu time, što ima prividni viskozitet pri koncentraciji od 2% u vodi od 80 mPa.s do 120 mPa.s i drugu hipromelozu naznačenu time, što ima prividni viskozitet na koncentraciji pri 2% u vodi od 3000 mPa.s do 5600 mPa.s.
23. {1-{1-[3-Fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegova farmaceutski prihvatljiva sol, za upotrebu prema bilo kojem od zahtjeva 1 do 3, gdje jedan ili više doznih oblika s produženim oslobađanjem svaki sadrži 10% do 15% u odnosu na masu jedne ili više hipromeloza.
24. {1-{1-[3-Fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegova farmaceutski prihvatljiva sol, za upotrebu prema bilo kojem od zahtjeva 1 do 3, gdje:-
a) jedan ili više doznih oblika s produženim oslobađanjem svaki sadrži 16% do 22% u odnosu na masu mikrokristalne celuloze; i/ili
b) jedan ili više doznih oblika s produženim oslobađanjem svaki sadrži 45% do 55% u odnosu na masu monohidrata laktoze.
25. {1-{1-[3-Fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegova farmaceutski prihvatljiva sol, za upotrebu prema bilo kojem od zahtjeva 1 do 3, gdje jedan ili više doznih oblika s produženim oslobađanjem svaki sadrži 0.3% do 0.7% u odnosu na masu magnezijevog stearata.
26. {1-{1-[3-Fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegova farmaceutski prihvatljiva sol, za upotrebu prema bilo kojem od zahtjeva 1 do 3, gdje spomenuta sol je {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il} acetonitrilna sol adipinske kiseline.
27. Jedan ili više doznih oblika s produženim oslobađanjem, koji zajedno osiguravaju pacijentu jednom dnevno oralnu dozu od oko 600 mg na osnovI slobodne baze {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrila, ili njegove farmaceutski prihvatljive soli.
28. Doza koja obuhvaća jedan ili više doznih oblika s produženim oslobađanjem, koje osiguravaju pacijentu jednom dnevno oralnu dozu od oko 600 mg na osnovI slobodne baze {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrila, ili njegove farmaceutski prihvatljive soli.
29. Jedan ili više doznih oblika s produženim oslobađanjem gdje svaki obuhvaća {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegovu farmaceutski prihvatljivu sol; gdje spomenuti jedan ili više doznih oblika s produženim oslobađanjem zajedno osiguravaju pacijentu jednodnevnu oralnu dozu od 200 mg, 300 mg, ili 600 mg na osnovi slobodne baze {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrila, ili njegove farmaceutski prihvatljive soli.
30. Doza, koja se sastoji od jednog ili više doznih oblika sa produženim oslobađanjem gdje svaki obuhvaća {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitril, ili njegovu farmaceutski prihvatljivu sol; gdje spomenuta doza osigurava pacijentu jednodnevnu oralnu dozu od 200 mg, 300 mg, ili 600 mg na osnovu slobodne baze {1-{1-[3-fluoro-2-(trifluorometil)izonikotinoil]piperidin-4-il}-3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]azetidin-3-il}acetonitrila, ili njegove farmaceutski prihvatljive soli.
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