HRP20160014T1 - Derivati 1-((5-heteroariltiazol-2-il)aminokarbonil)pirolidin-2-karboksamida kao inhibitori fosfatidilinozitol 3-kinaze (pi3k), koji su korisni u lijeäśenju proliferativnih bolesti - Google Patents
Derivati 1-((5-heteroariltiazol-2-il)aminokarbonil)pirolidin-2-karboksamida kao inhibitori fosfatidilinozitol 3-kinaze (pi3k), koji su korisni u lijeäśenju proliferativnih bolesti Download PDFInfo
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- HRP20160014T1 HRP20160014T1 HRP20160014TT HRP20160014T HRP20160014T1 HR P20160014 T1 HRP20160014 T1 HR P20160014T1 HR P20160014T T HRP20160014T T HR P20160014TT HR P20160014 T HRP20160014 T HR P20160014T HR P20160014 T1 HRP20160014 T1 HR P20160014T1
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- cancer
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- 201000010099 disease Diseases 0.000 title claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title claims 3
- 108091007960 PI3Ks Proteins 0.000 title 1
- 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 title 1
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 title 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 230000002062 proliferating effect Effects 0.000 title 1
- 206010028980 Neoplasm Diseases 0.000 claims 23
- 201000011510 cancer Diseases 0.000 claims 13
- 150000001875 compounds Chemical class 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 208000003174 Brain Neoplasms Diseases 0.000 claims 4
- 206010009944 Colon cancer Diseases 0.000 claims 4
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 4
- 208000029742 colonic neoplasm Diseases 0.000 claims 4
- 206010017758 gastric cancer Diseases 0.000 claims 4
- 208000014018 liver neoplasm Diseases 0.000 claims 4
- 201000001441 melanoma Diseases 0.000 claims 4
- 230000009826 neoplastic cell growth Effects 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 201000011549 stomach cancer Diseases 0.000 claims 4
- 206010006187 Breast cancer Diseases 0.000 claims 3
- 208000026310 Breast neoplasm Diseases 0.000 claims 3
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 206010004146 Basal cell carcinoma Diseases 0.000 claims 2
- 206010004593 Bile duct cancer Diseases 0.000 claims 2
- 206010005003 Bladder cancer Diseases 0.000 claims 2
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- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- 206010048832 Colon adenoma Diseases 0.000 claims 2
- 206010014733 Endometrial cancer Diseases 0.000 claims 2
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 2
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 2
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims 2
- 208000032612 Glial tumor Diseases 0.000 claims 2
- 206010018338 Glioma Diseases 0.000 claims 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 208000028018 Lymphocytic leukaemia Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 208000034578 Multiple myelomas Diseases 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 2
- 206010038389 Renal cancer Diseases 0.000 claims 2
- 206010039491 Sarcoma Diseases 0.000 claims 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 2
- 208000017733 acquired polycythemia vera Diseases 0.000 claims 2
- 208000009621 actinic keratosis Diseases 0.000 claims 2
- 201000005188 adrenal gland cancer Diseases 0.000 claims 2
- 208000024447 adrenal gland neoplasm Diseases 0.000 claims 2
- 208000026900 bile duct neoplasm Diseases 0.000 claims 2
- 210000004027 cell Anatomy 0.000 claims 2
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- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 208000003747 lymphoid leukemia Diseases 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 208000020984 malignant renal pelvis neoplasm Diseases 0.000 claims 2
- 210000000214 mouth Anatomy 0.000 claims 2
- 208000025113 myeloid leukemia Diseases 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
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- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
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- OAWXZFGKDDFTGS-BYPYZUCNSA-N (2s)-pyrrolidine-1,2-dicarboxylic acid Chemical group OC(=O)[C@@H]1CCCN1C(O)=O OAWXZFGKDDFTGS-BYPYZUCNSA-N 0.000 claims 1
- 208000005440 Basal Cell Neoplasms Diseases 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 201000008275 breast carcinoma Diseases 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 210000002429 large intestine Anatomy 0.000 claims 1
- 239000008177 pharmaceutical agent Substances 0.000 claims 1
- 210000000813 small intestine Anatomy 0.000 claims 1
- 201000002314 small intestine cancer Diseases 0.000 claims 1
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Claims (9)
1. Spoj, naznačen time, da je to
(S)-pirolidin-1,2-dikarboksilna kiselina-2-amid-1-({4-metil-5-[2-(2,2,2-trifluoro-1,1-dimetil-etil)-piridin-4-il]-tiazol-2-il}-amid), sljedeće strukture:
[image]
u slobodnom obliku ili u obliku farmaceutski prihvatljive soli.
2. Spoj prema zahtjevu 1, u slobodnom obliku ili u obliku farmaceutski prihvatljive soli, naznačen time, da se upotrebljava kao farmaceutsko sredstvo.
3. Uporaba spoja prema zahtjevu 1, u slobodnom obliku ili u obliku farmaceutski prihvatljive soli, naznačena time, daje za proizvodnju lijeka za liječenje raka.
4. Uporaba prema zahtjevu 3, naznačena time, da je rak odabran od sljedećih: sarkom, rak pluća, rak bronhija, rak prostate, rak dojke, rak gušterače, gastrointestinalni rak, rak debelog crijeva, rak rektuma, karcinom debelog crijeva, kolorektalni adenom, rak tiroidne žlijezde, rak jetre, rak unutrašnjih jetrenih žučnih vodova, hepatocelularni rak, rak nadbubrežne žlijezde, rak želudca, gastrički rak, gliom, glioblastom, endometrijski rak, melanom, rak bubrega, rak renalne karlice, rak mokraćnog mjehura, rak tijela maternice, rak grlića maternice, rak vagine, rak jajnika, multipli mijelom, rak ezofagusa, leukemija, akutna mijelogena leukemija, kronična mijelogena leukemija, limfocitna leukemija, mijeloidna leukemija, rak mozga, karcinom mozga, rak usne šupljine i ždrijela, rak grkljana, rak malih crijeva, non-Hodgkinov limfom, melanom, tubularni adenom debelog crijeva, neoplazija, neoplazija epitelijalnog karaktera, limfomi, mamarijski karcinom, karcinom bazalnih stanica, karcinom rožnatih stanica, aktinska keratoza, tumorske bolesti uključujući čvrste tumore, tumor vrata ili glave, policitemija vera, esencijalna trombocitemija, mijelofibroza s mijeloidnom metaplazijom, i bolest Walden-stroem.
5. Farmaceutski sastav, naznačen time, da obuhvaća terapeutski učinkovitu količinu spoja prema zahtjevu 1, u slobodnom obliku ili u obliku farmaceutski prihvatljive soli, te jedno ili više farmaceutski prihvatljivih pomoćnih sredstava.
6. Kombinirani farmaceutski sastav, naznačen time, da je prilagođen za istovremenu ili uzastopnu primjenu, pri čemu obuhvaća terapeutski učinkovitu količinu spoja prema zahtjevu 1, u slobodnom obliku ili u obliku farmaceutski prihvatljive soli, i terapeutski učinkovitu količinu jednog ili više kombinacijskih sudionika, te jedno ili više farmaceutski prihvatljivih pomoćnih sredstava.
7. Farmaceutski sastav prema zahtjevu 5, ili kombinirani farmaceutski sastav prema zahtjevu 6, naznačen time, da se upotrebljava za liječenje raka.
8. Spoj prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen/a time, da se upotrebljava za liječenje raka.
9. Spoj prema zahtjevu 8, ili njegova farmaceutski prihvatljiva sol, naznačen/a time, da se upotrebljava za liječenje raka odabranog između sljedećih: sarkom, rak pluća, rak bronhija, rak prostate, rak dojke, rak gušterače, gastrointestinalni rak, rak debelog crijeva, rak rektuma, karcinom debelog crijeva, kolorektalni adenom, rak tiroidne žlijezde, rak jetre, rak unutrašnjih jetrenih žučnih vodova, hepatocelularni rak, rak nadbubrežne žlijezde, rak želudca, gastrički rak, gliom, glioblastom, endometrijski rak, melanom, rak bubrega, rak renalne karlice, rak mokraćnog mjehura, rak tijela maternice, rak grlića maternice, rak vagine, rak jajnika, multipli mijelom, rak ezofagusa, leukemija, akutna mijelogena leukemija, kronična mijelogena leukemija, limfocitna leukemija, mijeloidna leukemija, rak mozga, karcinom mozga, rak usne šupljine i ždrijela, rak grkljana, rak malih crijeva, non-Hodgkinov limfom, melanom, tubularni adenom debelog crijeva, neoplazija, neoplazija epitelijalnog karaktera, limfomi, mamarijski karcinom, karcinom bazalnih stanica, karcinom rožnatih stanica, aktinska keratoza, tumorske bolesti uključujući čvrste tumore, tumor vrata ili glave, policitemija vera, esencijalna trombocitemija, mijelofibroza s mijeloidnom metaplazijom, i bolest Walden-stroem.
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