JP2020525477A5 - - Google Patents
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- Publication number
- JP2020525477A5 JP2020525477A5 JP2019572116A JP2019572116A JP2020525477A5 JP 2020525477 A5 JP2020525477 A5 JP 2020525477A5 JP 2019572116 A JP2019572116 A JP 2019572116A JP 2019572116 A JP2019572116 A JP 2019572116A JP 2020525477 A5 JP2020525477 A5 JP 2020525477A5
- Authority
- JP
- Japan
- Prior art keywords
- tumors
- compound
- formula
- lymphoma
- diethylphenyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 206010028980 Neoplasm Diseases 0.000 claims 13
- 150000001875 compounds Chemical class 0.000 claims 13
- -1 2,6-diethylphenyl Chemical group 0.000 claims 8
- 238000004519 manufacturing process Methods 0.000 claims 7
- 229910019142 PO4 Inorganic materials 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 239000010452 phosphate Substances 0.000 claims 6
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 4
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 4
- 206010025323 Lymphomas Diseases 0.000 claims 4
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 4
- 201000004681 Psoriasis Diseases 0.000 claims 4
- 230000004663 cell proliferation Effects 0.000 claims 4
- 201000005787 hematologic cancer Diseases 0.000 claims 4
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 4
- 208000032839 leukemia Diseases 0.000 claims 4
- 210000002307 prostate Anatomy 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 3
- 102100022681 40S ribosomal protein S27 Human genes 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 208000003950 B-cell lymphoma Diseases 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical group CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- 201000006107 Familial adenomatous polyposis Diseases 0.000 claims 2
- 201000008808 Fibrosarcoma Diseases 0.000 claims 2
- 208000032612 Glial tumor Diseases 0.000 claims 2
- 206010018338 Glioma Diseases 0.000 claims 2
- 206010018364 Glomerulonephritis Diseases 0.000 claims 2
- 208000017604 Hodgkin disease Diseases 0.000 claims 2
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 2
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 2
- 101000678466 Homo sapiens 40S ribosomal protein S27 Proteins 0.000 claims 2
- 101001019502 Homo sapiens Alpha-L-iduronidase Proteins 0.000 claims 2
- 101000659223 Homo sapiens Dual specificity protein kinase TTK Proteins 0.000 claims 2
- 101000962483 Homo sapiens Max dimerization protein 1 Proteins 0.000 claims 2
- 101001000302 Homo sapiens Max-interacting protein 1 Proteins 0.000 claims 2
- 101000896484 Homo sapiens Mitotic checkpoint protein BUB3 Proteins 0.000 claims 2
- 101000896657 Homo sapiens Mitotic checkpoint serine/threonine-protein kinase BUB1 Proteins 0.000 claims 2
- 101000794228 Homo sapiens Mitotic checkpoint serine/threonine-protein kinase BUB1 beta Proteins 0.000 claims 2
- 101000957106 Homo sapiens Mitotic spindle assembly checkpoint protein MAD1 Proteins 0.000 claims 2
- 101000957259 Homo sapiens Mitotic spindle assembly checkpoint protein MAD2A Proteins 0.000 claims 2
- 102100039185 Max dimerization protein 1 Human genes 0.000 claims 2
- 102100035880 Max-interacting protein 1 Human genes 0.000 claims 2
- 102100021718 Mitotic checkpoint protein BUB3 Human genes 0.000 claims 2
- 102100021691 Mitotic checkpoint serine/threonine-protein kinase BUB1 Human genes 0.000 claims 2
- 102100030144 Mitotic checkpoint serine/threonine-protein kinase BUB1 beta Human genes 0.000 claims 2
- 101000590284 Mus musculus 26S proteasome non-ATPase regulatory subunit 14 Proteins 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
- 206010029260 Neuroblastoma Diseases 0.000 claims 2
- 208000009905 Neurofibromatoses Diseases 0.000 claims 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 2
- 208000031481 Pathologic Constriction Diseases 0.000 claims 2
- 201000010208 Seminoma Diseases 0.000 claims 2
- 206010041067 Small cell lung cancer Diseases 0.000 claims 2
- 206010042971 T-cell lymphoma Diseases 0.000 claims 2
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims 2
- 208000036142 Viral infection Diseases 0.000 claims 2
- 230000001154 acute effect Effects 0.000 claims 2
- 206010003246 arthritis Diseases 0.000 claims 2
- 210000000941 bile Anatomy 0.000 claims 2
- 210000000481 breast Anatomy 0.000 claims 2
- 210000004027 cell Anatomy 0.000 claims 2
- 210000003679 cervix uteri Anatomy 0.000 claims 2
- 208000029664 classic familial adenomatous polyposis Diseases 0.000 claims 2
- 210000001072 colon Anatomy 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 210000003238 esophagus Anatomy 0.000 claims 2
- 206010020718 hyperplasia Diseases 0.000 claims 2
- 210000003734 kidney Anatomy 0.000 claims 2
- 210000004185 liver Anatomy 0.000 claims 2
- 210000004072 lung Anatomy 0.000 claims 2
- 210000004324 lymphatic system Anatomy 0.000 claims 2
- 230000036244 malformation Effects 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 230000017205 mitotic cell cycle checkpoint Effects 0.000 claims 2
- YFJAIURZMRJPDB-UHFFFAOYSA-N n,n-dimethylpiperidin-4-amine Chemical compound CN(C)C1CCNCC1 YFJAIURZMRJPDB-UHFFFAOYSA-N 0.000 claims 2
- 230000004770 neurodegeneration Effects 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 201000004931 neurofibromatosis Diseases 0.000 claims 2
- 239000003960 organic solvent Substances 0.000 claims 2
- 201000008968 osteosarcoma Diseases 0.000 claims 2
- 210000001672 ovary Anatomy 0.000 claims 2
- 210000000496 pancreas Anatomy 0.000 claims 2
- 210000000578 peripheral nerve Anatomy 0.000 claims 2
- 230000002980 postoperative effect Effects 0.000 claims 2
- 238000000634 powder X-ray diffraction Methods 0.000 claims 2
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 2
- 208000037803 restenosis Diseases 0.000 claims 2
- 210000003491 skin Anatomy 0.000 claims 2
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 2
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 2
- 239000007858 starting material Substances 0.000 claims 2
- 208000037804 stenosis Diseases 0.000 claims 2
- 230000036262 stenosis Effects 0.000 claims 2
- 210000002784 stomach Anatomy 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- 210000001685 thyroid gland Anatomy 0.000 claims 2
- 210000003932 urinary bladder Anatomy 0.000 claims 2
- 230000002792 vascular Effects 0.000 claims 2
- 230000009385 viral infection Effects 0.000 claims 2
- BRQRTBHRMBBOCZ-UHFFFAOYSA-N OP(O)(O)=O.CCc1cccc(CC)c1NC(=O)c1nn(C)c-2c1CCc1cnc(Nc3ccc(cc3OC)N3CCC(CC3)N(C)C)nc-21 Chemical compound OP(O)(O)=O.CCc1cccc(CC)c1NC(=O)c1nn(C)c-2c1CCc1cnc(Nc3ccc(cc3OC)N3CCC(CC3)N(C)C)nc-21 BRQRTBHRMBBOCZ-UHFFFAOYSA-N 0.000 claims 1
- 229940079156 Proteasome inhibitor Drugs 0.000 claims 1
- 230000000340 anti-metabolite Effects 0.000 claims 1
- 229940100197 antimetabolite Drugs 0.000 claims 1
- 239000002256 antimetabolite Substances 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 231100000024 genotoxic Toxicity 0.000 claims 1
- 230000001738 genotoxic effect Effects 0.000 claims 1
- 229940043355 kinase inhibitor Drugs 0.000 claims 1
- 230000000394 mitotic effect Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 229940127557 pharmaceutical product Drugs 0.000 claims 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 1
- 239000003207 proteasome inhibitor Substances 0.000 claims 1
- 238000001959 radiotherapy Methods 0.000 claims 1
- 239000003053 toxin Substances 0.000 claims 1
- 231100000765 toxin Toxicity 0.000 claims 1
- 108700012359 toxins Proteins 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP17305826.4 | 2017-06-29 | ||
| EP17305826 | 2017-06-29 | ||
| PCT/EP2018/067394 WO2019002454A1 (en) | 2017-06-29 | 2018-06-28 | NOVEL N- (2,6-DIETHYLPHENYL) -8 - ({4- [4- (DIMETHYLAMINO) PIPERIDIN-1-YL] -2-METHOXYPHENYL} AMINO) -1-METHYL-4,5-DIHYDRO-1H SALT -PYRAZOLO [4,3-H] QUINAZOLINE-3-CARBOXAMIDE, ITS PREPARATION AND FORMULATIONS CONTAINING THE SAME |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020525477A JP2020525477A (ja) | 2020-08-27 |
| JP2020525477A5 true JP2020525477A5 (enExample) | 2021-08-05 |
| JP7141416B2 JP7141416B2 (ja) | 2022-09-22 |
Family
ID=59313166
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019572116A Active JP7141416B2 (ja) | 2017-06-29 | 2018-06-28 | Ｎ－（２，６－ジエチルフェニル）－８－（｛４－［４－（ジメチルアミノ）ピペリジン－１－イル］－２－メトキシフェニル｝アミノ）－１－メチル－４，５－ジヒドロ－１Ｈ－ピラゾロ［４，３－ｈ］キナゾリン－３－カルボキサミドの新しい塩、その製造法、及びそれを含む製剤 |
Country Status (18)
| Country | Link |
|---|---|
| US (3) | US11160806B2 (enExample) |
| EP (1) | EP3645535B1 (enExample) |
| JP (1) | JP7141416B2 (enExample) |
| KR (1) | KR102609333B1 (enExample) |
| CN (1) | CN110896636B (enExample) |
| AR (1) | AR112040A1 (enExample) |
| AU (1) | AU2018293729B9 (enExample) |
| CA (1) | CA3068357C (enExample) |
| CL (1) | CL2019003848A1 (enExample) |
| EA (1) | EA039764B1 (enExample) |
| ES (1) | ES2900048T3 (enExample) |
| IL (1) | IL271628B2 (enExample) |
| MA (1) | MA49498A (enExample) |
| PL (1) | PL3645535T3 (enExample) |
| SG (1) | SG11201912651WA (enExample) |
| TW (1) | TWI750393B (enExample) |
| UY (1) | UY37778A (enExample) |
| WO (1) | WO2019002454A1 (enExample) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2025002962A1 (en) | 2023-06-30 | 2025-01-02 | Nerviano Medical Sciences S.R.L. | Use of a mps1 inhibitor for the treatment of hepatocellular carcinoma |
| WO2025021587A1 (en) | 2023-07-21 | 2025-01-30 | Nerviano Medical Sciences S.R.L. | Combination of a mps1 inhibitor and immune checkpoint inhibitors, uses and pharmaceutical compositions thereof |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUE027527T2 (en) * | 2008-06-26 | 2016-10-28 | Servier Lab | Pyrazolokinazoline derivatives as modulators of protein kinase activity |
-
2018
- 2018-06-21 UY UY0001037778A patent/UY37778A/es not_active Application Discontinuation
- 2018-06-28 MA MA049498A patent/MA49498A/fr unknown
- 2018-06-28 CN CN201880043442.0A patent/CN110896636B/zh active Active
- 2018-06-28 WO PCT/EP2018/067394 patent/WO2019002454A1/en not_active Ceased
- 2018-06-28 ES ES18732820T patent/ES2900048T3/es active Active
- 2018-06-28 PL PL18732820T patent/PL3645535T3/pl unknown
- 2018-06-28 EP EP18732820.8A patent/EP3645535B1/en active Active
- 2018-06-28 AR ARP180101781A patent/AR112040A1/es unknown
- 2018-06-28 EA EA202090115A patent/EA039764B1/ru unknown
- 2018-06-28 SG SG11201912651WA patent/SG11201912651WA/en unknown
- 2018-06-28 JP JP2019572116A patent/JP7141416B2/ja active Active
- 2018-06-28 US US16/624,488 patent/US11160806B2/en active Active
- 2018-06-28 KR KR1020207002339A patent/KR102609333B1/ko active Active
- 2018-06-28 AU AU2018293729A patent/AU2018293729B9/en active Active
- 2018-06-28 TW TW107122235A patent/TWI750393B/zh active
- 2018-06-28 CA CA3068357A patent/CA3068357C/en active Active
-
2019
- 2019-12-22 IL IL271628A patent/IL271628B2/en unknown
- 2019-12-26 CL CL2019003848A patent/CL2019003848A1/es unknown
-
2021
- 2021-09-30 US US17/490,318 patent/US20220016122A1/en not_active Abandoned
-
2024
- 2024-07-01 US US18/760,494 patent/US20240350501A1/en active Pending
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