JP2015518039A5 - - Google Patents
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- Publication number
- JP2015518039A5 JP2015518039A5 JP2015514587A JP2015514587A JP2015518039A5 JP 2015518039 A5 JP2015518039 A5 JP 2015518039A5 JP 2015514587 A JP2015514587 A JP 2015514587A JP 2015514587 A JP2015514587 A JP 2015514587A JP 2015518039 A5 JP2015518039 A5 JP 2015518039A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- alkoxy
- halo
- cancer
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 258
- 125000003545 alkoxy group Chemical group 0.000 claims 42
- 150000001875 compounds Chemical class 0.000 claims 36
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 36
- 206010028980 Neoplasm Diseases 0.000 claims 18
- 125000005843 halogen group Chemical group 0.000 claims 17
- 201000011510 cancer Diseases 0.000 claims 15
- 125000004093 cyano group Chemical group *C#N 0.000 claims 14
- 125000001475 halogen functional group Chemical group 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 11
- 239000001257 hydrogen Substances 0.000 claims 11
- 229910052760 oxygen Inorganic materials 0.000 claims 9
- 125000005842 heteroatom Chemical group 0.000 claims 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 8
- 229910052717 sulfur Inorganic materials 0.000 claims 8
- 229910052736 halogen Inorganic materials 0.000 claims 7
- 150000002367 halogens Chemical class 0.000 claims 7
- 150000002431 hydrogen Chemical class 0.000 claims 7
- 125000001424 substituent group Chemical group 0.000 claims 7
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 6
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 6
- 230000002265 prevention Effects 0.000 claims 6
- 206010005003 Bladder cancer Diseases 0.000 claims 5
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 5
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 5
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 5
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 125000002950 monocyclic group Chemical group 0.000 claims 5
- 201000005112 urinary bladder cancer Diseases 0.000 claims 5
- 102100027842 Fibroblast growth factor receptor 3 Human genes 0.000 claims 4
- 101710182396 Fibroblast growth factor receptor 3 Proteins 0.000 claims 4
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 239000002246 antineoplastic agent Substances 0.000 claims 4
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 206010006187 Breast cancer Diseases 0.000 claims 3
- 208000026310 Breast neoplasm Diseases 0.000 claims 3
- 206010009944 Colon cancer Diseases 0.000 claims 3
- 108091008794 FGF receptors Proteins 0.000 claims 3
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 3
- 208000034578 Multiple myelomas Diseases 0.000 claims 3
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 3
- 206010060862 Prostate cancer Diseases 0.000 claims 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 102000052178 fibroblast growth factor receptor activity proteins Human genes 0.000 claims 3
- 201000005202 lung cancer Diseases 0.000 claims 3
- 208000020816 lung neoplasm Diseases 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 230000001404 mediated effect Effects 0.000 claims 3
- 230000035772 mutation Effects 0.000 claims 3
- ZEOWTGPWHLSLOG-UHFFFAOYSA-N Cc1ccc(cc1-c1ccc2c(n[nH]c2c1)-c1cnn(c1)C1CC1)C(=O)Nc1cccc(c1)C(F)(F)F Chemical compound Cc1ccc(cc1-c1ccc2c(n[nH]c2c1)-c1cnn(c1)C1CC1)C(=O)Nc1cccc(c1)C(F)(F)F ZEOWTGPWHLSLOG-UHFFFAOYSA-N 0.000 claims 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 2
- 102100023593 Fibroblast growth factor receptor 1 Human genes 0.000 claims 2
- 101710182386 Fibroblast growth factor receptor 1 Proteins 0.000 claims 2
- 102100023600 Fibroblast growth factor receptor 2 Human genes 0.000 claims 2
- 101710182389 Fibroblast growth factor receptor 2 Proteins 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 2
- 125000004452 carbocyclyl group Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 201000007270 liver cancer Diseases 0.000 claims 2
- 208000014018 liver neoplasm Diseases 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 102100027844 Fibroblast growth factor receptor 4 Human genes 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 208000034951 Genetic Translocation Diseases 0.000 claims 1
- 101000917134 Homo sapiens Fibroblast growth factor receptor 4 Proteins 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 1
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 1
- 150000001204 N-oxides Chemical class 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims 1
- 125000005189 alkyl hydroxy group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 229940043355 kinase inhibitor Drugs 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 201000002740 oral squamous cell carcinoma Diseases 0.000 claims 1
- 230000002018 overexpression Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 1
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 230000005945 translocation Effects 0.000 claims 1
- 0 CC1(C=CC(Nc2ncc3ncc(*)nc3n2)=CC=C1)I Chemical compound CC1(C=CC(Nc2ncc3ncc(*)nc3n2)=CC=C1)I 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261653081P | 2012-05-30 | 2012-05-30 | |
| GB1209613.7 | 2012-05-30 | ||
| US61/653,081 | 2012-05-30 | ||
| GBGB1209613.7A GB201209613D0 (en) | 2012-05-30 | 2012-05-30 | New compounds |
| US201361782233P | 2013-03-14 | 2013-03-14 | |
| US61/782,233 | 2013-03-14 | ||
| PCT/GB2013/051427 WO2013179033A1 (en) | 2012-05-30 | 2013-05-30 | Pteridines as fgfr inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015518039A JP2015518039A (ja) | 2015-06-25 |
| JP2015518039A5 true JP2015518039A5 (enExample) | 2016-07-21 |
| JP6363068B2 JP6363068B2 (ja) | 2018-07-25 |
Family
ID=46546195
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015514587A Active JP6363068B2 (ja) | 2012-05-30 | 2013-05-30 | Ｆｇｆｒ阻害剤としてのプテリジン |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US9447098B2 (enExample) |
| EP (1) | EP2855480B1 (enExample) |
| JP (1) | JP6363068B2 (enExample) |
| KR (1) | KR102149759B1 (enExample) |
| CN (1) | CN104507944B (enExample) |
| AU (1) | AU2013269316C1 (enExample) |
| BR (1) | BR112014029709B1 (enExample) |
| CA (1) | CA2874967C (enExample) |
| DK (1) | DK2855480T3 (enExample) |
| ES (1) | ES2739348T3 (enExample) |
| GB (1) | GB201209613D0 (enExample) |
| HR (1) | HRP20191202T1 (enExample) |
| HU (1) | HUE045663T2 (enExample) |
| IN (1) | IN2014MN02069A (enExample) |
| LT (1) | LT2855480T (enExample) |
| MX (1) | MX359418B (enExample) |
| RU (1) | RU2702906C2 (enExample) |
| SI (1) | SI2855480T1 (enExample) |
| WO (1) | WO2013179033A1 (enExample) |
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| GB201007286D0 (en) | 2010-04-30 | 2010-06-16 | Astex Therapeutics Ltd | New compounds |
| GB201020179D0 (en) | 2010-11-29 | 2011-01-12 | Astex Therapeutics Ltd | New compounds |
| GB201118675D0 (en) | 2011-10-28 | 2011-12-14 | Astex Therapeutics Ltd | New compounds |
| GB201118656D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118652D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118654D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| DE102013008159A1 (de) | 2012-05-14 | 2013-11-14 | Thoratec Corporation | Mantelsystem für Katheterpumpe |
| GB2504176A (en) | 2012-05-14 | 2014-01-22 | Thoratec Corp | Collapsible impeller for catheter pump |
| GB201209613D0 (en) * | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| GB201209609D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| GB201307577D0 (en) | 2013-04-26 | 2013-06-12 | Astex Therapeutics Ltd | New compounds |
| US10736900B2 (en) | 2014-03-26 | 2020-08-11 | Astex Therapeutics Ltd | Combinations of an FGFR inhibitor and an IGF1R inhibitor |
| BR112016022056B1 (pt) | 2014-03-26 | 2023-04-11 | Astex Therapeutics Limited | Combinação, composição farmacêutica, uso de uma combinação ou uma composição farmacêutica, e, produto farmacêutico |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| WO2015160980A1 (en) | 2014-04-15 | 2015-10-22 | Thoratec Corporation | Heart pump providing adjustable out flow |
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