EA021056B1 - Оксазолзамещенные индазолы в качестве ингибиторов pi3-киназ, содержащая их фармацевтическая композиция и их применение в лечении расстройств, опосредованных ненадлежащей активностью pi3-киназ - Google Patents
Оксазолзамещенные индазолы в качестве ингибиторов pi3-киназ, содержащая их фармацевтическая композиция и их применение в лечении расстройств, опосредованных ненадлежащей активностью pi3-киназ Download PDFInfo
- Publication number
- EA021056B1 EA021056B1 EA201190227A EA201190227A EA021056B1 EA 021056 B1 EA021056 B1 EA 021056B1 EA 201190227 A EA201190227 A EA 201190227A EA 201190227 A EA201190227 A EA 201190227A EA 021056 B1 EA021056 B1 EA 021056B1
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- EA
- Eurasian Patent Office
- Prior art keywords
- pharmaceutically acceptable
- methyl
- oxazol
- compound
- acceptable salt
- Prior art date
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- 230000000694 effects Effects 0.000 title claims 17
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title claims 11
- 208000035475 disorder Diseases 0.000 title claims 11
- 230000001404 mediated effect Effects 0.000 title claims 11
- 239000008194 pharmaceutical composition Substances 0.000 title claims 4
- 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 title 1
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 title 1
- 150000002473 indoazoles Chemical class 0.000 title 1
- 125000002971 oxazolyl group Chemical group 0.000 title 1
- 239000002935 phosphatidylinositol 3 kinase inhibitor Substances 0.000 title 1
- 150000003839 salts Chemical class 0.000 claims 23
- 150000001875 compounds Chemical class 0.000 claims 17
- 108091000080 Phosphotransferase Proteins 0.000 claims 16
- 102000020233 phosphotransferase Human genes 0.000 claims 16
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 15
- GRVDJDISBSALJP-UHFFFAOYSA-N methyloxidanyl Chemical group [O]C GRVDJDISBSALJP-UHFFFAOYSA-N 0.000 claims 10
- 125000000623 heterocyclic group Chemical group 0.000 claims 8
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 8
- 229910052757 nitrogen Inorganic materials 0.000 claims 7
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 6
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 4
- HNQIVZYLYMDVSB-UHFFFAOYSA-N methanesulfonimidic acid Chemical compound CS(N)(=O)=O HNQIVZYLYMDVSB-UHFFFAOYSA-N 0.000 claims 4
- MCIDWGZGWVSZMK-UHFFFAOYSA-N 2-[6-(1h-indol-4-yl)-1h-indazol-4-yl]-5-[(4-propan-2-ylpiperazin-1-yl)methyl]-1,3-oxazole Chemical compound C1CN(C(C)C)CCN1CC1=CN=C(C=2C=3C=NNC=3C=C(C=2)C=2C=3C=CNC=3C=CC=2)O1 MCIDWGZGWVSZMK-UHFFFAOYSA-N 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 208000002193 Pain Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 208000006454 hepatitis Diseases 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000003112 inhibitor Substances 0.000 claims 3
- 230000002401 inhibitory effect Effects 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims 3
- 208000002250 Hematologic Neoplasms Diseases 0.000 claims 2
- 208000034486 Multi-organ failure Diseases 0.000 claims 2
- 208000010718 Multiple Organ Failure Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 206010033645 Pancreatitis Diseases 0.000 claims 2
- 206010052779 Transplant rejections Diseases 0.000 claims 2
- 208000036142 Viral infection Diseases 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 201000005787 hematologic cancer Diseases 0.000 claims 2
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 2
- 231100000283 hepatitis Toxicity 0.000 claims 2
- 239000007943 implant Substances 0.000 claims 2
- 208000017169 kidney disease Diseases 0.000 claims 2
- 231100000516 lung damage Toxicity 0.000 claims 2
- 208000029744 multiple organ dysfunction syndrome Diseases 0.000 claims 2
- 230000004770 neurodegeneration Effects 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 125000004430 oxygen atom Chemical group O* 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 208000023504 respiratory system disease Diseases 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 230000019100 sperm motility Effects 0.000 claims 2
- 208000010110 spontaneous platelet aggregation Diseases 0.000 claims 2
- 230000009385 viral infection Effects 0.000 claims 2
- ZWAJLVLEBYIOTI-OLQVQODUSA-N (1s,6r)-7-oxabicyclo[4.1.0]heptane Chemical compound C1CCC[C@@H]2O[C@@H]21 ZWAJLVLEBYIOTI-OLQVQODUSA-N 0.000 claims 1
- -1 1H-indol4-yl Chemical group 0.000 claims 1
- 201000002909 Aspergillosis Diseases 0.000 claims 1
- 208000036641 Aspergillus infections Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000008035 Back Pain Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 206010065390 Inflammatory pain Diseases 0.000 claims 1
- 208000004554 Leishmaniasis Diseases 0.000 claims 1
- 206010062106 Respiratory tract infection viral Diseases 0.000 claims 1
- 206010039085 Rhinitis allergic Diseases 0.000 claims 1
- 208000007536 Thrombosis Diseases 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 201000010105 allergic rhinitis Diseases 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 230000005713 exacerbation Effects 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 208000014674 injury Diseases 0.000 claims 1
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
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- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 210000002345 respiratory system Anatomy 0.000 claims 1
- 230000008733 trauma Effects 0.000 claims 1
- 206010044652 trigeminal neuralgia Diseases 0.000 claims 1
- 230000003612 virological effect Effects 0.000 claims 1
Classifications
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Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US17403309P | 2009-04-30 | 2009-04-30 | |
| PCT/EP2010/055666 WO2010125082A1 (en) | 2009-04-30 | 2010-04-28 | Oxazole substituted indazoles as pi3-kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201190227A1 EA201190227A1 (ru) | 2012-05-30 |
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