HRP20140541T1 - Soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo(2,3-d)pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropannitrila - Google Patents
Soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo(2,3-d)pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropannitrila Download PDFInfo
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- HRP20140541T1 HRP20140541T1 HRP20140541AT HRP20140541T HRP20140541T1 HR P20140541 T1 HRP20140541 T1 HR P20140541T1 HR P20140541A T HRP20140541A T HR P20140541AT HR P20140541 T HRP20140541 T HR P20140541T HR P20140541 T1 HRP20140541 T1 HR P20140541T1
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- 150000003839 salts Chemical class 0.000 title claims 16
- 229940122245 Janus kinase inhibitor Drugs 0.000 title 1
- 201000010099 disease Diseases 0.000 claims 18
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 18
- 206010028980 Neoplasm Diseases 0.000 claims 14
- 201000011510 cancer Diseases 0.000 claims 13
- 208000017733 acquired polycythemia vera Diseases 0.000 claims 9
- 208000037244 polycythemia vera Diseases 0.000 claims 9
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 8
- 208000027866 inflammatory disease Diseases 0.000 claims 8
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims 6
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 5
- 210000002345 respiratory system Anatomy 0.000 claims 5
- 208000017520 skin disease Diseases 0.000 claims 5
- 206010028561 Myeloid metaplasia Diseases 0.000 claims 4
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 4
- 206010028537 myelofibrosis Diseases 0.000 claims 4
- HFNKQEVNSGCOJV-OAHLLOKOSA-N ruxolitinib Chemical class C1([C@@H](CC#N)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)CCCC1 HFNKQEVNSGCOJV-OAHLLOKOSA-N 0.000 claims 4
- 208000023275 Autoimmune disease Diseases 0.000 claims 3
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 3
- 101000997832 Homo sapiens Tyrosine-protein kinase JAK2 Proteins 0.000 claims 3
- 102000042838 JAK family Human genes 0.000 claims 3
- 108091082332 JAK family Proteins 0.000 claims 3
- 208000034578 Multiple myelomas Diseases 0.000 claims 3
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 3
- 206010060862 Prostate cancer Diseases 0.000 claims 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 3
- 102100033444 Tyrosine-protein kinase JAK2 Human genes 0.000 claims 3
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims 3
- 230000002489 hematologic effect Effects 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 210000003491 skin Anatomy 0.000 claims 3
- LGJWVXWQCTZSGC-XFULWGLBSA-N (3r)-3-cyclopentyl-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile;sulfuric acid Chemical compound OS(O)(=O)=O.C1([C@@H](CC#N)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)CCCC1 LGJWVXWQCTZSGC-XFULWGLBSA-N 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- 241000701085 Human alphaherpesvirus 3 Species 0.000 claims 2
- 241000701044 Human gammaherpesvirus 4 Species 0.000 claims 2
- 241000701806 Human papillomavirus Species 0.000 claims 2
- 206010048643 Hypereosinophilic syndrome Diseases 0.000 claims 2
- 206010020751 Hypersensitivity Diseases 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 208000009525 Myocarditis Diseases 0.000 claims 2
- 206010034277 Pemphigoid Diseases 0.000 claims 2
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims 2
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims 2
- 201000008736 Systemic mastocytosis Diseases 0.000 claims 2
- 208000026935 allergic disease Diseases 0.000 claims 2
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- 230000002757 inflammatory effect Effects 0.000 claims 2
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims 2
- 239000011976 maleic acid Substances 0.000 claims 2
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- 230000000699 topical effect Effects 0.000 claims 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims 2
- 230000003612 virological effect Effects 0.000 claims 2
- WOJBKXOVBVZSET-HFNHQGOYSA-N (z)-but-2-enedioic acid;(3r)-3-cyclopentyl-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile Chemical compound OC(=O)\C=C/C(O)=O.C1([C@@H](CC#N)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)CCCC1 WOJBKXOVBVZSET-HFNHQGOYSA-N 0.000 claims 1
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- 241000598436 Human T-cell lymphotropic virus Species 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
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
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- 208000031888 Mycoses Diseases 0.000 claims 1
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- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 201000011152 Pemphigus Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 206010063837 Reperfusion injury Diseases 0.000 claims 1
- 206010039705 Scleritis Diseases 0.000 claims 1
- 206010040880 Skin irritation Diseases 0.000 claims 1
- 208000031673 T-Cell Cutaneous Lymphoma Diseases 0.000 claims 1
- 208000024799 Thyroid disease Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 206010046851 Uveitis Diseases 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 230000000172 allergic effect Effects 0.000 claims 1
- 208000022531 anorexia 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
- 150000001875 compounds Chemical class 0.000 claims 1
- 208000010247 contact dermatitis Diseases 0.000 claims 1
- 201000007241 cutaneous T cell lymphoma Diseases 0.000 claims 1
- 206010061428 decreased appetite Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000005884 exanthem Diseases 0.000 claims 1
- 229940084434 fungoid Drugs 0.000 claims 1
- 208000024908 graft versus host disease Diseases 0.000 claims 1
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- 102000018358 immunoglobulin Human genes 0.000 claims 1
- 230000001771 impaired effect Effects 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 201000004614 iritis Diseases 0.000 claims 1
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- 230000000302 ischemic effect Effects 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
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- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 201000001976 pemphigus vulgaris Diseases 0.000 claims 1
- 208000025638 primary cutaneous T-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- 206010037844 rash Diseases 0.000 claims 1
- JFMWPOCYMYGEDM-XFULWGLBSA-N ruxolitinib phosphate Chemical compound OP(O)(O)=O.C1([C@@H](CC#N)N2N=CC(=C2)C=2C=3C=CNC=3N=CN=2)CCCC1 JFMWPOCYMYGEDM-XFULWGLBSA-N 0.000 claims 1
- 230000036556 skin irritation Effects 0.000 claims 1
- 231100000475 skin irritation Toxicity 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
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Claims (19)
1. Sol izabrana iz grupe koju čine:
(R)-3-(4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciklopentilpropan-nitrilna sol maleinske kiseline;
(R)-3-(4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciklopentilpropan-nitrilna sol sumporne kiseline; i
(R)-3-(4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciklopentilpropan-nitrilna sol fosforne kiseline.
2. Sol prema patentnom zahtjevu 1 koja predstavlja (R)-3-(4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciktopentilpropan-nitrilnu sol maleinske kiseline.
3. Sol prema patentnom zahtjevu 1 koja predstavlja (R)-3-(4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciklopentilpropan-nitrilnu sol sumporne kiseline.
4. Sol prema patentnom zahtjevu 1 koja predstavlja (R)-3-(4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciklopentilpropan-nitrilnu sol fosforne kiseline.
5. Sol prema patentnom zahtjevu 1, koja je značajno izolirana.
6. Postupak pripreme soli prema bilo kojem od patentnih zahtjeva od 1 do 5 koji podrazumijeva kombiniranje (R)-3-(4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciklopentilpropan-nitrila sa maleinskom kiselinom, sumpornom kiselinom ili fosfornom kiselinom.
7. Pripravak koji sadrži najmanje jednu sol prema bilo kojem od patentnih zahtjeva od 1 do 5 i najmanje jedan farmaceutski prihvatljiv nosač.
8. Pripravak prema patentnom zahtjevu 7 koji je pogodan za oralnu ili topičku primjenu.
9. Pripravak prema patentnom zahtjevu 7 koji je pogodan za topičku primjenu.
10. Postupak moduliranja aktivnosti JAK koji podrazumijeva dovođenje JAK u kontakt sa soli prema bilo kojem od patentnih zahtjeva od 1 do 5 u ex vivo uvjetima.
11. Postupak prema patentnom zahtjevu 10, naznačen time, što je navedena modulacija inhibitorna.
12. Sol prema bilo kojem od patentnih zahtjeva od 1 do 5 za upotrebu u tretmanu bolesti kod pacijenta, naznačenu time, što bolest predstavlja bolest koju karakterizira poremećena aktivnost JAK.
13. Sol za upotrebu prema patentnom zahtjevu 12,
naznačenu time, što navedena bolest predstavlja odbacivanje alotransplanta ili oboljenje transplatat-protiv domaćina; ili
naznačenu time, što navedena bolest predstavlja autoimunu bolest; ili
naznačenu time, što navedena bolest predstavlja poremećaj kože; ili
naznačenu time, što navedena bolest predstavlja virusnu bolest; ili
naznačenu time, što navedena bolest predstavlja rak; ili
naznačenu time, što navedenu bolest karakterizira mutirani JAK2; ili
naznačenu time, što navedena bolest predstavlja mijeloproliferativni poremećaj; ili
naznačenu time, što navedena bolest predstavlja upalnu bolest; ili
naznačenu time, što navedena bolest predstavlja ishemičku reperfuzijsku povredu ili neki drugi događaj koji je posljedica ishemije; ili
naznačenu time, što navedena bolest predstavlja anoreksiju ili kaheksiju koja nastaje kao posljedica ili prati rak; ili
naznačenu time, što navedena bolest predstavlja zamor koji nastaje kao posljedica ili prati rak.
14. Sol za upotrebu prema patentnom zahtjevu 13,
naznačenu time, što navedena autoimuna bolest predstavlja poremećaj kože, multiplu sklerozu, reumatoidni artritis, juvenilni artritis, dijabetes tipa I, lupus, upalnu bolest crijeva, Kronovu bolest, mijasteniju gravis, imunoglobulinsku nefropatiju, miokarditis ili autoimuni poremećaj štitne žlijezde; ili
naznačenu time, što navedena autoimuna bolest predstavlja bulozni poremećaj kože; ili naznačenu time, što navedeni poremećaj kože predstavlja atopijski dermatitis, psorijazu, preosjetljivost kože, iritaciju kože, osip, kontaktni dermatitis ili alergijsku kontaktnu preosjetljivost kože; ili
naznačenu time, što navedena virusna bolest predstavlja bolest izazvanu Epstein-Bar virusom (EBV), Hepatitis B, Hepatitis C, HIV, HTLV 1, Varicella-Zoster virusom (VZV) ili humanim papiloma virusom (HPV); ili
naznačenu time, što navedeni rak predstavlja solidan tumor; ili
naznačenu time, što navedeni rak predstavlja rak prostate, renalni rak, rak jetre, rak dojke, rak pluća, rak štitne žlijezde, Kaposijevu sarkomu, Kastelmanovu bolest ili rak gušterače; ili naznačenu time, što navedeni rak predstavlja hematološki rak; ili naznačenu time, što navedeni rak predstavlja rak kože; ili naznačenu time, što navedeni rak predstavlja multipli mijelom; ili
naznačenu time, što se najmanje jedna mutacija spomenutog mutiranog JAK2 nalazi u pseudo- kinaznoj domeni navedenog JAK2; ili
naznačenu time, što navedeni mijeloproliferativni poremećaj (MPD) predstavlja policitemiju vera (PV), esencijalnu trombocitemiju (ET), mijeloidnu metaplaziju sa mijelofibrozom (MMM), kroničnu mijelogenu leukemiju (CML), hroničnu mijelomonocitnu leukemiju (CMML), hipereozinofilni sindrom (HES) ili sistemsku bolest mast ćelija (SMCD); ili
naznačenu time, što navedena upalna bolest predstavlja upalnu bolest oka; ili
naznačenu time, što navedena upalna bolest predstavlja upalnu bolest dišnih puteva; ili naznačenu time, što navedena upalna bolest predstavlja upalnu miopatiju; ili naznačenu time, što navedena upalna bolest predstavlja miokarditis.
15. Sol za upotrebu prema patentnom zahtjevu 14, naznačenu time, što navedeni bulozni poremećaj kože predstavlja pemfigus vulgaris (PV) ili bulozni pemfigoid (BP) ; ili
naznačenu time, što navedeni rak predstavlja rak prostate; ili
naznačenu time, što navedeni hematološki rak predstavlja limfom, leukemiju ili multipli mijelom; ili
naznačenu time, što navedeni rak kože predstavlja kožni T-ćelijski limfom ili kožni B-ćelijski limfom; ili
naznačenu time, što navedeno upalno oboljenje oka predstavlja iritis, uveitis, skleritis ili konjuktivitis; ili
naznačenu time, što se navedeno upalno oboljenje dišnih puteva odnosi na gornji respiratorni trakt; ili
naznačenu time, što se navedeno upalno oboljenje dišnih puteva odnosi na donji respiratorni trakt.
16. Sol prema bilo kojem od patentnih zahtjeva 1 do 5 za upotrebu u tretmanu raka; poremećaja kože; upalnog procesa; reumatoidnog artritisa; raka prostate; psorijaze; multiplog mijeloma; mijeloidne metaplazije sa mijelofibrozom (MMM); policitemije vera (PV); esencijalne trombocitemije (ET); fungoidne mikoze; hematološkog raka; kronične mijeloidne leukemije (CML); akutne limfoblasne leukemije (ALL); ili kronične mijelomonocitne leukemije (CMML).
17. Sol prema bilo kojem od patentnih zahtjeva od 1 do 5 za upotrebu u tretmanu mijeloidne metaplazije sa mijelofibrozom (MMM); policitemije vera (PV) ili esencijalne trombocitemije (ET).
18. (R)-3-(4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciklopentilpropan-nitrilna kisela sol fosforne kiseline za upotrebu u tretmanu mijeloprotiferativnog poremećaja.
19. Spoj za upotrebu prema patentnom zahtjevu 18, naznačen time, što spomenuti mijeloproliferativni poremećaj predstavlja mijeloidna metaplazija sa mijelofibrozom (MMM); policitemija vera (PV) ili esencijalna trombocitemija (ET).
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US94370507P | 2007-06-13 | 2007-06-13 | |
PCT/US2008/066662 WO2008157208A2 (en) | 2007-06-13 | 2008-06-12 | Salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
EP08770794.9A EP2173752B2 (en) | 2007-06-13 | 2008-06-12 | Salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo(2,3-d)pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
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HRP20190385TT HRP20190385T1 (hr) | 2007-06-13 | 2019-02-28 | Upotreba soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h- pirazol-1-il)-3- ciklopentilpropionitrila |
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