HRP20192203T1 - 3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- ili heptan-nitril kao jak inhibitori - Google Patents
3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- ili heptan-nitril kao jak inhibitori Download PDFInfo
- Publication number
- HRP20192203T1 HRP20192203T1 HRP20192203TT HRP20192203T HRP20192203T1 HR P20192203 T1 HRP20192203 T1 HR P20192203T1 HR P20192203T T HRP20192203T T HR P20192203TT HR P20192203 T HRP20192203 T HR P20192203T HR P20192203 T1 HRP20192203 T1 HR P20192203T1
- Authority
- HR
- Croatia
- Prior art keywords
- pyrrolo
- pyrazol
- pyrimidin
- compound
- disease
- Prior art date
Links
- 229940122245 Janus kinase inhibitor Drugs 0.000 title 1
- SDAXRHHPNYTELL-UHFFFAOYSA-N heptanenitrile Chemical compound CCCCCCC#N SDAXRHHPNYTELL-UHFFFAOYSA-N 0.000 title 1
- YSIMAPNUZAVQER-UHFFFAOYSA-N octanenitrile Chemical compound CCCCCCCC#N YSIMAPNUZAVQER-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 14
- 150000003839 salts Chemical class 0.000 claims 11
- 238000000034 method Methods 0.000 claims 8
- 150000003016 phosphoric acids Chemical class 0.000 claims 7
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 208000017520 skin disease Diseases 0.000 claims 5
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 4
- 208000003476 primary myelofibrosis Diseases 0.000 claims 4
- OFOSNWSCZOAXGX-UHFFFAOYSA-N 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]heptanenitrile Chemical compound C1=NN(C(CC#N)CCCC)C=C1C1=NC=NC2=C1C=CN2 OFOSNWSCZOAXGX-UHFFFAOYSA-N 0.000 claims 3
- UZUXXRPDJQFESS-UHFFFAOYSA-N 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]octanenitrile Chemical compound C1=NN(C(CC#N)CCCCC)C=C1C1=NC=NC2=C1C=CN2 UZUXXRPDJQFESS-UHFFFAOYSA-N 0.000 claims 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 201000011152 Pemphigus Diseases 0.000 claims 3
- 201000004681 Psoriasis Diseases 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 201000001976 pemphigus vulgaris Diseases 0.000 claims 3
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 3
- UZUXXRPDJQFESS-CQSZACIVSA-N (3r)-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]octanenitrile Chemical compound C1=NN([C@@H](CC#N)CCCCC)C=C1C1=NC=NC2=C1C=CN2 UZUXXRPDJQFESS-CQSZACIVSA-N 0.000 claims 2
- UZUXXRPDJQFESS-AWEZNQCLSA-N (3s)-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]octanenitrile Chemical compound C1=NN([C@H](CC#N)CCCCC)C=C1C1=NC=NC2=C1C=CN2 UZUXXRPDJQFESS-AWEZNQCLSA-N 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 206010010741 Conjunctivitis Diseases 0.000 claims 2
- 208000032027 Essential Thrombocythemia Diseases 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
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 2
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 2
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 2
- 208000009525 Myocarditis Diseases 0.000 claims 2
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 claims 2
- 206010034277 Pemphigoid Diseases 0.000 claims 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims 2
- 206010039705 Scleritis Diseases 0.000 claims 2
- 201000008736 Systemic mastocytosis Diseases 0.000 claims 2
- 206010046851 Uveitis Diseases 0.000 claims 2
- 208000000594 bullous pemphigoid Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 208000010247 contact dermatitis Diseases 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 230000002757 inflammatory effect Effects 0.000 claims 2
- 201000004614 iritis Diseases 0.000 claims 2
- 230000000302 ischemic effect Effects 0.000 claims 2
- 206010028537 myelofibrosis Diseases 0.000 claims 2
- 239000003960 organic solvent Substances 0.000 claims 2
- 230000003612 virological effect Effects 0.000 claims 2
- OFOSNWSCZOAXGX-CYBMUJFWSA-N (3r)-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]heptanenitrile Chemical compound C1=NN([C@@H](CC#N)CCCC)C=C1C1=NC=NC2=C1C=CN2 OFOSNWSCZOAXGX-CYBMUJFWSA-N 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 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
- 206010006895 Cachexia Diseases 0.000 claims 1
- 208000005024 Castleman disease Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 201000004624 Dermatitis 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
- 208000005176 Hepatitis C Diseases 0.000 claims 1
- 208000007514 Herpes zoster Diseases 0.000 claims 1
- 241000598436 Human T-cell lymphotropic virus Species 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
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- 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
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 201000002481 Myositis 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
- 206010063837 Reperfusion injury Diseases 0.000 claims 1
- 208000018569 Respiratory Tract disease 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
- 241000700605 Viruses Species 0.000 claims 1
- 208000017733 acquired polycythemia vera Diseases 0.000 claims 1
- 125000003158 alcohol group Chemical group 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 230000000172 allergic effect Effects 0.000 claims 1
- 229910000147 aluminium phosphate Inorganic materials 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
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims 1
- 239000006071 cream Substances 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
- 230000000694 effects Effects 0.000 claims 1
- 201000005884 exanthem Diseases 0.000 claims 1
- 239000000499 gel Substances 0.000 claims 1
- 208000024908 graft versus host disease Diseases 0.000 claims 1
- 208000002672 hepatitis B Diseases 0.000 claims 1
- 230000009610 hypersensitivity Effects 0.000 claims 1
- 102000018358 immunoglobulin Human genes 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 208000017169 kidney disease Diseases 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
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- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 201000005962 mycosis fungoides Diseases 0.000 claims 1
- 239000002674 ointment Substances 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- SXSYSSSLJADJBV-ZOWNYOTGSA-N phosphoric acid;(3s)-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]heptanenitrile Chemical compound OP(O)(O)=O.C1=NN([C@H](CC#N)CCCC)C=C1C1=NC=NC2=C1C=CN2 SXSYSSSLJADJBV-ZOWNYOTGSA-N 0.000 claims 1
- CVRIPRBTANZXKX-UHFFFAOYSA-N phosphoric acid;3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]octanenitrile Chemical compound OP(O)(O)=O.C1=NN(C(CC#N)CCCCC)C=C1C1=NC=NC2=C1C=CN2 CVRIPRBTANZXKX-UHFFFAOYSA-N 0.000 claims 1
- 208000037244 polycythemia vera 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
- 210000003491 skin Anatomy 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
Classifications
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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
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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
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/525—Isoalloxazines, e.g. riboflavins, vitamin B2
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- Animal Behavior & Ethology (AREA)
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- Diabetes (AREA)
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- Communicable Diseases (AREA)
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- Orthopedic Medicine & Surgery (AREA)
- Obesity (AREA)
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- Urology & Nephrology (AREA)
- Dermatology (AREA)
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- Tropical Medicine & Parasitology (AREA)
- Pain & Pain Management (AREA)
- Biotechnology (AREA)
- Ophthalmology & Optometry (AREA)
- Biomedical Technology (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurosurgery (AREA)
Claims (20)
1. Spoj, koji je izabran između:
3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]oktannitrila; i
3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]heptannitrila;
ili njegove farmaceutski prihvatljive soli.
2. Spoj prema zahtjevu 1, koji je:
(a) 3-[4-(7H-pirolo[2,3-d]primidin-4-il)-1H-pirazol-1-il]oktannitril, ili njegova farmaceutski prihvatljiva sol;
(b) (3R)-3-[4-(7H-pirolo[2,3-d]primidin-4-il)-1H-pirazol-1-il]oktannitril, ili njegova farmaceutski prihvatljiva sol;
(c) (3S)-3-[4-(7H-pirolo[2,3-d]primidin-4-il)-1H-pirazol-1-il]oktannitril, ili njegova farmaceutski prihvatljiva sol;
(d) sol fosforne kiseline 3-[4-(7H-pirolo[2,3-d]primidin-4-il)-1H- pirazol-1-il]oktannitrila;
(e) sol fosforne kiseline (3R)-3-[4-(7H-pirolo[2,3-d]primidin-4-il)-1H-pirazol-1-il]oktannitrila;
(f) sol fosforne kiseline (3S)-3-[4-(7H-pirolo[2,3-d]primidin-4-il)-1H-pirazol-1-il]oktannitrila;
(g) 3-[4-(7H-pirolo[2,3-d]primidin-4-il)-1H-pirazol-1-il]heptannitril, ili njegova farmaceutski prihvatljiva sol;
(h) (3R)-3-[4-(7H-pirolo[2,3-d]primidin-4-il)-1H-pirazol-1-il]heptannitril, ili njegova farmaceutski prihvatljiva sol;
(i) (3S)-3-[4-(7H-pirolo[2,3-d]primidin-4-il)-1H-pirazol-1-il]heptannitril, ili njegova farmaceutski prihvatljiva sol;
(j) sol fosforne kiseline 3-[4-(7H-pirolo[2,3-d]primidin-4-il)-1H-pirazol-1-il]heptannitrila ;
(k) sol fosforne kiseline (3R)-3-[4-(7H-pirolo[2,3-d]primidin-4-il)-1H-pirazol-1-il]heptannitrila; ili
(l) sol fosforne kiseline(3S)-3-[4-(7H-pirolo[2,3-d]primidin-4-il)-1H-pirazol-1-il]heptannitrila .
3. Sastav koji obuhvaća spoj ili sol prema zahtjevu 1 ili zahtjevu 2, i bar jedan farmaceutski prihvatljivi nosač.
4. Sastav prema zahtjevu 3 koji je pogodan za
(a) vanjsku primjenu; ili
(b) za transdermalnu primjenu.
5. Sastav prema zahtjevu 4 (b) koji je u obliku transdermalnog flastera, masti, losiona, kreme, ili gela.
6. Spoj ili sol prema zahtjevu 1 ili zahtjevu 2 za upotrebu u liječenju bolesti pacijenta, pri čemu je spomenuta bolest povezana sa JAK aktivnosti.
7. Spoj ili sol prema zahtjevu 1 ili zahtjevu 2 za upotrebu u liječenju
(a) autoimune bolesti;
(b) karcinoma;
(c) mijeloproliferativnog poremećaja;
(d) upalne bolesti;
(e) virusne bolesti;
(f) odbacivanja transplantiranog organa;
(g) ishemijske povrede reperfuzijom ili bolesti koja je povezana sa upalnim ishemijskim događajem;
(h) anoreksije ili kaheksije;
(i) slabosti;
(j) odbacivanja alografta ili bolesti grafta protiv domaćina;
(k) reumatoidnog artritisa;
(l) psorijaze;
(m) dermatitisa;
(n) iritisa;
(o) uveitisa;
(p) skleritisa; ili
(q) konjuktivitisa.
8. Spoj za upotrebu prema zahtjevu 7(a) pri čemu je spomenuta autoimuna bolest:
(a) poremećaj kože, multipla skleroza, reumatoidni artritis, psorijazni artritis, juvenilni artritis, tip I dijabetesa, lupus, psorijaza, upalna bolest crijeva, Crohnova bolest, mijastenija gravis, imunoglobulinske nefropatije, miokarditis ili autoimuni poremećaj štitnjače;
(b) bulozni kožni poremećaj;
(c) reumatoidni artritis; ili
(d) poremećaj kože.
9. Spoj za upotrebu prema zahtjevu 8(b) gdje spomenuti bulozni kožni poremećaj je pemfigus vulgaris (PV) ili bulozni pemfigoid (BP).
10. Spoj za upotrebu prema zahtjevu 8(d) gdje je spomenuti kožni poremećaj
(a) atopični dermatitis ili psorijaza; ili
(b) preosjetljivost kože, iritacija kože, kožni osip, kontaktni dermatitis ili alergijska kontaktna preosjetljivost.
11. Spoj za upotrebu prema zahtjevu 7(b) gdje je spomenuti karcinom
(a) solidni tumor;
(b) karcinom prostate, karcinom bubrega, karcinom jetre, karcinom dojke, karcinom pluća, karcinom štitnjače, Kaposi sarkom, Castlemanova bolest ili karcinom gušterače;
(c) limfom, leukemija, ili multipli mijelom; ili
(d) kožni T-stanični limfom ili kožni B-stanični limfom.
12. Spoj za upotrebu prema zahtjevu 7(c) gdje je spomenuti mijeloproliferativni poremećaj policitemija vera (PV), esencijalna trombocitemija (ET), primarna mijelofibroza (PMF), kronična mijelogena leukemija (CML), kronična mijelomonocitna leukemija (CMML), hipereozinofilni sindrom (HES), idiopatska mijelofibroza (IMF), ili sistemska bolest mastocita (SMCD).
13. Spoj za upotrebu prema zahtjevu 7(d), gdje je spomenuta upalna bolest iritis, uveitis, skleritis, konjuktivitis, upalna bolest respiratornog trakta, upalna miopatija, ili miokarditis.
14. Spoj za upotrebu prema zahtjevu 7(e) gdje je spomenuta virusna bolest Epstein Barr virus (EBV), Hepatitis B, Hepatitis C, HIV, HTLV 1, Varicell-Zoster virus (VZV) ili Humani Papilloma virus (HPV).
15. Postupak za dobivanje soli fosforne kiseline spoja formule III:
gdje R1 je H ili metil, koji obuhvaća kombinaciju spoja formule III s fosfornom kiselinom.
16. Postupak prema zahtjevu 15, gdje je spomenuti postupak postupak za dobivanje:
(a) soli fosforne kiseline 3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]oktannitrila ; ili
(b) soli fosforne kiseline 3-[4-(7H-pirolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il]heptannitrila .
17. Postupak prema zahtjevu 15 ili zahtjevu 16, gdje se spomenuta kombinacija izvodi u prisustvu organskog otapala.
18. Postupak prema zahtjevu 17, gdje je organsko otapalo alkohol.
19. Postupak prema zahtjevu 18, gdje je alkohol izabran iz grupe koja obuhvaća metanol, etanol, izopropanol, i butanol.
20. Postupak prema zahtjevu 15 ili zahtjevu 16, gdje se kombiniranje izvodi na temperaturi koja je
(a) veća od oko 20 °C; ili
(b) 60 °C.
Applications Claiming Priority (3)
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US18058209P | 2009-05-22 | 2009-05-22 | |
PCT/US2010/035728 WO2010135621A1 (en) | 2009-05-22 | 2010-05-21 | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors |
EP10721227.6A EP2432472B1 (en) | 2009-05-22 | 2010-05-21 | 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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