HRP20210036T1 - Soli inhibitora pi3k i postupci za njihovo dobivanje - Google Patents
Soli inhibitora pi3k i postupci za njihovo dobivanje Download PDFInfo
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- HRP20210036T1 HRP20210036T1 HRP20210036TT HRP20210036T HRP20210036T1 HR P20210036 T1 HRP20210036 T1 HR P20210036T1 HR P20210036T T HRP20210036T T HR P20210036TT HR P20210036 T HRP20210036 T HR P20210036T HR P20210036 T1 HRP20210036 T1 HR P20210036T1
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- 150000003839 salts Chemical class 0.000 title claims 14
- 238000000034 method Methods 0.000 title claims 7
- 239000012828 PI3K inhibitor Substances 0.000 title 1
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 title 1
- 201000010099 disease Diseases 0.000 claims 13
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 13
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical class Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 11
- 208000003950 B-cell lymphoma Diseases 0.000 claims 8
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 7
- 206010021245 Idiopathic thrombocytopenic purpura Diseases 0.000 claims 6
- 208000031981 Thrombocytopenic Idiopathic Purpura Diseases 0.000 claims 6
- 206010047115 Vasculitis Diseases 0.000 claims 6
- 201000003710 autoimmune thrombocytopenic purpura Diseases 0.000 claims 6
- 238000000634 powder X-ray diffraction Methods 0.000 claims 6
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 claims 4
- 208000035186 Hemolytic Autoimmune Anemia Diseases 0.000 claims 3
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 3
- 201000000448 autoimmune hemolytic anemia Diseases 0.000 claims 3
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 3
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 2
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 2
- 201000004331 Henoch-Schoenlein purpura Diseases 0.000 claims 2
- 206010019617 Henoch-Schonlein purpura Diseases 0.000 claims 2
- 241000711549 Hepacivirus C Species 0.000 claims 2
- 206010020751 Hypersensitivity Diseases 0.000 claims 2
- 208000031814 IgA Vasculitis Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 208000005777 Lupus Nephritis Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 108091000080 Phosphotransferase Proteins 0.000 claims 2
- 208000007048 Polymyalgia Rheumatica Diseases 0.000 claims 2
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 2
- 206010043540 Thromboangiitis obliterans Diseases 0.000 claims 2
- 206010069351 acute lung injury Diseases 0.000 claims 2
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 claims 2
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims 2
- 208000026935 allergic disease Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 238000001938 differential scanning calorimetry curve Methods 0.000 claims 2
- 230000002489 hematologic effect Effects 0.000 claims 2
- 208000015446 immunoglobulin a vasculitis Diseases 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 206010025135 lupus erythematosus Diseases 0.000 claims 2
- 102000020233 phosphotransferase Human genes 0.000 claims 2
- 239000000725 suspension Substances 0.000 claims 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 2
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000032671 Allergic granulomatous angiitis Diseases 0.000 claims 1
- 206010002412 Angiocentric lymphomas Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 208000027496 Behcet disease Diseases 0.000 claims 1
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 208000020084 Bone disease Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000033386 Buerger disease Diseases 0.000 claims 1
- 208000011691 Burkitt lymphomas Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 208000006344 Churg-Strauss Syndrome Diseases 0.000 claims 1
- 208000010007 Cogan syndrome Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000019707 Cryoglobulinemic vasculitis Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 208000018428 Eosinophilic granulomatosis with polyangiitis Diseases 0.000 claims 1
- 208000007465 Giant cell arteritis Diseases 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 206010018372 Glomerulonephritis membranous Diseases 0.000 claims 1
- 206010072579 Granulomatosis with polyangiitis Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000011200 Kawasaki disease Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 241000721454 Pemphigus Species 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000007452 Plasmacytoma Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 206010065857 Primary Effusion Lymphoma Diseases 0.000 claims 1
- 206010036711 Primary mediastinal large B-cell lymphomas Diseases 0.000 claims 1
- 208000033766 Prolymphocytic Leukemia Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000004732 Systemic Vasculitis Diseases 0.000 claims 1
- 208000001106 Takayasu Arteritis Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- 208000033559 Waldenström macroglobulinemia Diseases 0.000 claims 1
- 230000007815 allergy Effects 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 210000003719 b-lymphocyte Anatomy 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 238000001816 cooling Methods 0.000 claims 1
- 201000003278 cryoglobulinemia Diseases 0.000 claims 1
- 230000001086 cytosolic effect Effects 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 201000006569 extramedullary plasmacytoma Diseases 0.000 claims 1
- 230000003325 follicular Effects 0.000 claims 1
- 201000003444 follicular lymphoma Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 210000001102 germinal center b cell Anatomy 0.000 claims 1
- 201000009277 hairy cell leukemia Diseases 0.000 claims 1
- 238000010438 heat treatment Methods 0.000 claims 1
- 230000009610 hypersensitivity Effects 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 201000003445 large cell neuroendocrine carcinoma Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 210000003563 lymphoid tissue Anatomy 0.000 claims 1
- 208000006116 lymphomatoid granulomatosis Diseases 0.000 claims 1
- 201000007919 lymphoplasmacytic lymphoma Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000007924 marginal zone B-cell lymphoma Diseases 0.000 claims 1
- 208000021937 marginal zone lymphoma Diseases 0.000 claims 1
- 201000008350 membranous glomerulonephritis Diseases 0.000 claims 1
- 231100000855 membranous nephropathy Toxicity 0.000 claims 1
- 201000005328 monoclonal gammopathy of uncertain significance Diseases 0.000 claims 1
- 208000001725 mucocutaneous lymph node syndrome Diseases 0.000 claims 1
- 210000004877 mucosa Anatomy 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 206010028417 myasthenia gravis Diseases 0.000 claims 1
- 206010028537 myelofibrosis Diseases 0.000 claims 1
- 201000000050 myeloid neoplasm 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
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 210000004180 plasmocyte Anatomy 0.000 claims 1
- 201000006292 polyarteritis nodosa Diseases 0.000 claims 1
- 230000000306 recurrent effect Effects 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 208000010721 smoldering plasma cell myeloma Diseases 0.000 claims 1
- 206010062113 splenic marginal zone lymphoma Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 206010043207 temporal arteritis Diseases 0.000 claims 1
- 238000001757 thermogravimetry curve Methods 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 206010046766 uterine cancer Diseases 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
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- 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
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- 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
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Claims (14)
1. Sol koja je sol klorovodične kiseline (R)-4-(3-((S)-1-(4-amino-3-metil-1H-pirazolo[3,4-d]pirimidin-1-il)etil)-5-kloro-2-etoksi-6-fluorofenil)pirolidin-2-ona, koja je kristalna.
2. Sol prema zahtjevu 1 koja je u stehiometrijskom odnosu 1:1 (R)-4-(3-((S)-1-(4-amino-3-metil-1H-pirazolo[3,4-d]pirimidin-1-il)etil)-5-kloro-2-etoksi-6-fluorofenil)pirolidin-2-ona prema klorovodičnoj kiselini.
3. Sol prema zahtjevu 1 ili 2, naznačena sa DSC termogramom koji ima endotermni signal na 207 ± 3 °C.
4. Sol prema bilo kojem od patentnih zahtjeva 1-3 koja ima DSC termogram kao što je dolje prikazano:
[image]
5. Sol prema bilo kojem od patentnih zahtjeva 1-4 koja ima TGA termogram kao što je dolje prikazano:
[image]
6. Sol prema bilo kojem od zahtjeva 1-5 koja ima:
(a) najmanje jedan XRPD signal, u smislu 2-teta, odabran od 11.3° ± 0.2°, 16.4° ± 0.2°, 21.0° ± 0.2°, 23.0° ± 0.2°, 28.1° ± 0.2°, 31.2° 6 0.2°, i 32.8° 6 0.2°;
(b) najmanje dva XRPD signala, u smislu 2-teta, odabrana od 11.3° ± 0.2°, 16.4° ± 0.2°, 21.0° ± 0.2°, 23.0° ± 0.2°, 28.1° ± 0.2°, 31.2° ± 0.2°, i 32.8° ± 0.2°;
(c) najmanje tri XRPD signala, u smislu 2-teta, odabrana od 11.3° ± 0.2°, 16.4° ± 0.2°, 21.0° ± 0.2°, 23.0° ± 0.2°, 28.1° ± 0.2°, 31.2° ± 0.2°, i 32.8° ± 0.2°;
(d) najmanje četiri XRPD signala, u smislu 2-teta, odabrana od 11.3° ± 0.2°, 16.4° ± 0.2°, 21.0° ± 0.2°, 23.0° ± 0.2°, 28.1° ± 0.2°, 31.2° ± 0.2°, i 32.8° ± 0.2°;
(e) najmanje pet XRPD signala, u smislu 2-teta, odabrana od 11.3° ± 0.2°, 16.4° ± 0.2°, 21.0° ± 0.2°, 23.0° ± 0.2°, 28.1° ± 0.2°, 31.2° ± 0.2°, i 32.8° ± 0.2°.
7. Sol prema bilo kojem od zahtjeva 1-5 koja ima profil XRPD kao što je dolje prikazano:
[image]
8. Farmaceutski sastav koji sadrži sol prema bilo kojem od zahtjeva 1-7 i farmaceutski prihvatljivi nosač.
9. Postupak za inhibiranje aktivnosti PI3Kδ kinaze, in vitro, koji obuhvaća dovođenje u kontakt kinaze sa soli prema bilo kojem od zahtjeva 1-7.
10. Sol prema bilo kojem od zahtjeva 1 do 7, za upotrebu u liječenju bolesti kod pacijenta, pri čemu je spomenuta bolest izabrana od idiopatske trombocitopenijske purpure (ITP), autoimune hemolitične anemije, vaskulitisa, sistemskog lupusa eritematozusa, lupusa nefritisa, pemfigusa, autoimune hemolitične anemije (AIHA), membranozne nefropatije, kronične limfocitne leukemije (CLL), Ne-hodgkinovog limfoma (NHL), leukemije dlakastih stanica, limfoma Mantle stanica, Burkitovog limfoma, malog limfocinog limfoma, folikularnog limfoma, limfoplazmacitnog limfoma, limfoma ekstranodalne marginalne zone, Hodgkinovog limfoma, Waldenstromove makrogloblinemije, prolimfocitne leukemije, akutne limfoblastne leukemije, mijelofibroze, limfoma limfatičnog tkiva povezanog sa mukozom (MALT), limfoma B-stanica, mediastinalnog (timičnog) limfoma velikih B-stanica, limfomatoidne granulomatoze, limfoma marginalne zone slezene, primarnog efuzionog limfoma, intravaskularnog limfoma velikih B-stanica, leukemije plazma stanica, ekstramedularnog plazmacitoma, pritajenog mijeloma (tj. asimptomatskog mijeloma), monoklonalne gamapatije neodređenog značaja (MGUS) I limfoma B stanica;
ili je bolest idiopatska trombocitopenijska purpura (ITP) izabrana od relapsnog ITP i refraktornog ITP;
ili je bolest vaskulitis izabran od Behçetove bolesti, Coganovog sindroma, temporalni arteritis, reumatske polimijalgije (PMR), Takayasujevog arteritisa, Buergerove bolesti (thromboangiitis obliterans), vaskulitisa centralnog nervnog sistema, Kawasakijeve bolesti, poliarteritis nodoza, Churg-straussovog sindroma, vaskulitisa mješovite krioglobulinemije (esencijalnog ili induciranog virusom hepatitisa C (HCV)), Henoch-Schonleinove purpure (HSP), vaskulitisa induciranog hiperpreosetljivošću, mikroskopskog angilitisa, Wegenerove granulomatoze, i sistemskog vaskulitisa (AASV) induciranog sa anti-neutrofilnim citoplazmatskim antitijelom (ANCA);
ili je bolest ne-Hodgkinov limfom (NHL) odabran od relapsnog NHL, refraktornog NHL, i rekurentnog folikularnog NHL;
ili je bolest limfom B stanica, pri čemu spomenuti limfom B stanice je difuzni krupnostanični limfom B-stanica (DLBCL);
ili je bolest limfom B stanica, pri čemu spomenuti limfom B stanica je aktiviranim B-stanicama sličan (ABC) difuzni krupnostanični B limfom, ili difuzni krupnostanični B limfom (GCB) B stanica germinalnog centra;
ili je bolest osteoartritis, restenoza, ateroskleroza, poremećaji kostiju, artritis, dijabetska retnopatija, psorijaza, benigna hipertrofija prostate, upala, angiogeneza, pankreatitis, bolest bubrega, upalna bolest crijeva, mijastenija gravis, multipla skleroza, ili Sjögrenov sindrom;
ili je bolest reumatoidni artritis, alergija, astma, glomerulonefritis, lupus, ili upala povezana sa bilo kojim od prethodno spomenutih;
ili je bolest lupus koji je sistemski lupus eritematozus ili lupus nefritis;
ili je bolest rak grudi, rak prostate, rak debelog crijeva, rak endometrijuma, rak mozga, rak mokraćnog mjehura, rak kože, rak maternice, rak jajnika, rak pluća, rak gušterače, rak bubrega, rak želudca, ili hematološki rak;
ili je bolest hematološki rak koji je akutna mijeloblastna leukemija ili kronična mijeloidna leukemija;
ili je bolest akutna povreda pluća (ALI) ili adultni respiratorni distres sindrom (ARDS).
11. Postupak za dobivanje soli prema bilo kojem od patentnih zahtjeva 1-7, koji obuhvaća reakciju spoja Formule I:
[image]
sa klorovodičnom kiselinom da bi se oblikovala spomenuta sol.
12. Postupak prema zahtjevu 11, pri čemu spomenuta klorovodična kiselina je 1 M klorovodična kiselina u vodi.
13. Postupak prema zahtjevu 11 ili 12, pri čemu se spomenuta reakcija izvodi na temperaturi od oko 45 °C do 55 °C.
14. Postupak prema bilo kojem od zahtjeva 11-13, što postupak dalje obuhvaća:
dodavanje klorovodične kiseline spoju Formule I na sobnoj temperaturi da bi se oblikovala suspenzija; zagrijavanje spomenute suspenzije do temperature od oko 45 °C do 55 °C da bi se oblikovao rastvor; i hlađenje rastvora do temperature od oko 0 °C do 5 °C da bi spomenuta sol kristalizala.
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