JP2015503521A5 - - Google Patents
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- Publication number
- JP2015503521A5 JP2015503521A5 JP2014549176A JP2014549176A JP2015503521A5 JP 2015503521 A5 JP2015503521 A5 JP 2015503521A5 JP 2014549176 A JP2014549176 A JP 2014549176A JP 2014549176 A JP2014549176 A JP 2014549176A JP 2015503521 A5 JP2015503521 A5 JP 2015503521A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- substituted
- hal
- phenyl
- hydrogen atom
- 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
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 18
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 14
- 150000003839 salts Chemical class 0.000 claims 11
- 239000000203 mixture Substances 0.000 claims 10
- 125000001845 4 membered carbocyclic group Chemical group 0.000 claims 9
- 125000001054 5 membered carbocyclic group Chemical group 0.000 claims 9
- 125000004008 6 membered carbocyclic group Chemical group 0.000 claims 9
- 150000001875 compounds Chemical class 0.000 claims 9
- 201000010099 disease Diseases 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 230000033115 angiogenesis Effects 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 206010012601 diabetes mellitus Diseases 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 125000004430 oxygen atom Chemical group O* 0.000 claims 5
- 125000004011 3 membered carbocyclic group Chemical group 0.000 claims 4
- 125000001960 7 membered carbocyclic group Chemical group 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 201000004624 Dermatitis Diseases 0.000 claims 3
- 208000032612 Glial tumor Diseases 0.000 claims 3
- 206010018338 Glioma Diseases 0.000 claims 3
- 206010061218 Inflammation Diseases 0.000 claims 3
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 208000002193 Pain Diseases 0.000 claims 3
- 206010033645 Pancreatitis Diseases 0.000 claims 3
- 208000031481 Pathologic Constriction Diseases 0.000 claims 3
- 201000004681 Psoriasis Diseases 0.000 claims 3
- 208000017442 Retinal disease Diseases 0.000 claims 3
- 206010038910 Retinitis Diseases 0.000 claims 3
- 206010038923 Retinopathy Diseases 0.000 claims 3
- 206010039710 Scleroderma Diseases 0.000 claims 3
- 206010064930 age-related macular degeneration Diseases 0.000 claims 3
- 208000010668 atopic eczema Diseases 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 201000011066 hemangioma Diseases 0.000 claims 3
- 206010020718 hyperplasia Diseases 0.000 claims 3
- 230000004054 inflammatory process Effects 0.000 claims 3
- 208000017169 kidney disease Diseases 0.000 claims 3
- 208000002780 macular degeneration Diseases 0.000 claims 3
- 201000001441 melanoma Diseases 0.000 claims 3
- 210000002307 prostate Anatomy 0.000 claims 3
- 208000017520 skin disease Diseases 0.000 claims 3
- 230000036262 stenosis Effects 0.000 claims 3
- 208000037804 stenosis Diseases 0.000 claims 3
- 230000005747 tumor angiogenesis Effects 0.000 claims 3
- 239000004480 active ingredient Substances 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 230000003463 hyperproliferative effect Effects 0.000 claims 2
- 125000002950 monocyclic group Chemical group 0.000 claims 2
- -1 3-substituted phenyl Chemical group 0.000 claims 1
- TVDXVEYZPBAGQH-UHFFFAOYSA-N 5-[(4-phenylpiperidin-3-yl)amino]quinazoline-8-carboxamide Chemical compound C12=CN=CN=C2C(C(=O)N)=CC=C1NC1CNCCC1C1=CC=CC=C1 TVDXVEYZPBAGQH-UHFFFAOYSA-N 0.000 claims 1
- DMKGGPGYGHAZLX-UHFFFAOYSA-N 5-[[4-(3-chloro-4-fluorophenyl)piperidin-3-yl]amino]quinazoline-8-carboxamide Chemical compound C12=CN=CN=C2C(C(=O)N)=CC=C1NC1CNCCC1C1=CC=C(F)C(Cl)=C1 DMKGGPGYGHAZLX-UHFFFAOYSA-N 0.000 claims 1
- NSHZNQHXFGNGRZ-UHFFFAOYSA-N 5-[[4-(4-chloro-3-fluorophenyl)piperidin-3-yl]amino]quinazoline-8-carboxamide Chemical compound C12=CN=CN=C2C(C(=O)N)=CC=C1NC1CNCCC1C1=CC=C(Cl)C(F)=C1 NSHZNQHXFGNGRZ-UHFFFAOYSA-N 0.000 claims 1
- QXQBUHCSEYQBBD-UHFFFAOYSA-N 5-[[4-(4-fluorophenyl)piperidin-3-yl]amino]quinazoline-8-carboxamide Chemical compound C12=CN=CN=C2C(C(=O)N)=CC=C1NC1CNCCC1C1=CC=C(F)C=C1 QXQBUHCSEYQBBD-UHFFFAOYSA-N 0.000 claims 1
- SFFJZCPGYSFVNX-UHFFFAOYSA-N 5-[[4-[3-(trifluoromethyl)phenyl]pyrrolidin-3-yl]amino]quinazoline-8-carboxamide Chemical compound C12=CN=CN=C2C(C(=O)N)=CC=C1NC1CNCC1C1=CC=CC(C(F)(F)F)=C1 SFFJZCPGYSFVNX-UHFFFAOYSA-N 0.000 claims 1
- QFZWBDDVPDKVEO-UHFFFAOYSA-N 5-[[4-[3-fluoro-4-(trifluoromethyl)phenyl]piperidin-3-yl]amino]quinazoline-8-carboxamide Chemical compound C12=CN=CN=C2C(C(=O)N)=CC=C1NC1CNCCC1C1=CC=C(C(F)(F)F)C(F)=C1 QFZWBDDVPDKVEO-UHFFFAOYSA-N 0.000 claims 1
- ZIRLUWNUUJIIGT-UHFFFAOYSA-N 5-[[4-[4-(trifluoromethoxy)phenyl]pyrrolidin-3-yl]amino]quinazoline-8-carboxamide Chemical compound C12=CN=CN=C2C(C(=O)N)=CC=C1NC1CNCC1C1=CC=C(OC(F)(F)F)C=C1 ZIRLUWNUUJIIGT-UHFFFAOYSA-N 0.000 claims 1
- 208000019802 Sexually transmitted disease Diseases 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 125000005936 piperidyl group Chemical group 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- GYBHRTQLUQOYID-UHFFFAOYSA-N quinazoline-8-carboxamide Chemical compound N1=CN=C2C(C(=O)N)=CC=CC2=C1 GYBHRTQLUQOYID-UHFFFAOYSA-N 0.000 claims 1
- 125000004434 sulfur atom Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161579377P | 2011-12-22 | 2011-12-22 | |
| US61/579,377 | 2011-12-22 | ||
| PCT/US2012/070085 WO2013096194A1 (en) | 2011-12-22 | 2012-12-17 | Novel heterocyclic carboxamides as modulators of kinase activity |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017155667A Division JP6553686B2 (ja) | 2011-12-22 | 2017-08-10 | キナーゼ活性のモジュレータとしての新規な複素環カルボキサミド |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015503521A JP2015503521A (ja) | 2015-02-02 |
| JP2015503521A5 true JP2015503521A5 (https=) | 2017-08-03 |
| JP6193880B2 JP6193880B2 (ja) | 2017-09-06 |
Family
ID=47459185
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014549176A Expired - Fee Related JP6193880B2 (ja) | 2011-12-22 | 2012-12-17 | キナーゼ活性のモジュレータとしての新規な複素環カルボキサミド |
| JP2017155667A Expired - Fee Related JP6553686B2 (ja) | 2011-12-22 | 2017-08-10 | キナーゼ活性のモジュレータとしての新規な複素環カルボキサミド |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017155667A Expired - Fee Related JP6553686B2 (ja) | 2011-12-22 | 2017-08-10 | キナーゼ活性のモジュレータとしての新規な複素環カルボキサミド |
Country Status (23)
| Country | Link |
|---|---|
| US (3) | US9139568B2 (https=) |
| EP (1) | EP2794571B1 (https=) |
| JP (2) | JP6193880B2 (https=) |
| KR (1) | KR102098358B1 (https=) |
| CN (1) | CN104169258B (https=) |
| AU (2) | AU2012355494B2 (https=) |
| BR (1) | BR112014015327B1 (https=) |
| CA (1) | CA2856448C (https=) |
| DK (1) | DK2794571T3 (https=) |
| EA (2) | EA027968B1 (https=) |
| ES (1) | ES2614232T3 (https=) |
| HR (1) | HRP20170099T1 (https=) |
| HU (1) | HUE032918T2 (https=) |
| IL (1) | IL233199B (https=) |
| LT (1) | LT2794571T (https=) |
| MX (1) | MX353062B (https=) |
| PL (1) | PL2794571T3 (https=) |
| PT (1) | PT2794571T (https=) |
| RS (1) | RS55621B1 (https=) |
| SG (2) | SG11201402387WA (https=) |
| SI (1) | SI2794571T1 (https=) |
| WO (1) | WO2013096194A1 (https=) |
| ZA (1) | ZA201403517B (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9586938B2 (en) | 2010-07-29 | 2017-03-07 | Merck Patent Gmbh | Cyclic amine azaheterocyclic carboxamides |
| SG11201402387WA (en) * | 2011-12-22 | 2014-09-26 | Merck Patent Gmbh | Novel heterocyclic carboxamides as modulators of kinase activity |
| SG11201505999VA (en) | 2013-03-11 | 2015-08-28 | Merck Patent Gmbh | 6-[4-(1 h-imidazol-2-yl)piperidin-1 -yl]pyrimidin-4-amine derivatives as modulators of kinase activity |
| JP2021515767A (ja) | 2018-03-07 | 2021-06-24 | バイエル・アクチエンゲゼルシヤフト | Ｅｒｋ５阻害剤の同定及び使用 |
| CN115073369A (zh) * | 2022-05-31 | 2022-09-20 | 汉瑞药业(荆门)有限公司 | 一种5-溴喹啉-8-甲醛的制备方法 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1465651A (en) * | 1974-04-19 | 1977-02-23 | Wyeth John & Brother Ltd | Carbocyclic-fused ring pyridine derivatives |
| US4933447A (en) * | 1987-09-24 | 1990-06-12 | Ss Pharmaceutical Co., Ltd. | Quinoline derivatives |
| JPH01156960A (ja) * | 1987-09-24 | 1989-06-20 | Ss Pharmaceut Co Ltd | キノリン誘導体 |
| TW200306819A (en) | 2002-01-25 | 2003-12-01 | Vertex Pharma | Indazole compounds useful as protein kinase inhibitors |
| TW200407324A (en) * | 2002-05-17 | 2004-05-16 | Bristol Myers Squibb Co | Bicyclic modulators of androgen receptor function |
| WO2004092154A1 (en) | 2003-04-03 | 2004-10-28 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of protein kinases |
| AU2004278413B2 (en) | 2003-09-30 | 2008-07-31 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| JP4800216B2 (ja) | 2003-10-24 | 2011-10-26 | エグゼリクシス， インコーポレイテッド | ｐ７０Ｓ６キナーゼモジュレーターおよび使用方法 |
| DE602004014969D1 (de) | 2003-11-21 | 2008-08-21 | Novartis Ag | 1h-imidazochinolinderivate als proteinkinaseinhibitoren |
| CN1889958A (zh) | 2003-12-09 | 2007-01-03 | 美国政府健康及人类服务部 | 抑制免疫应答或治疗增生性疾病的方法 |
| WO2005117909A2 (en) | 2004-04-23 | 2005-12-15 | Exelixis, Inc. | Kinase modulators and methods of use |
| CA2590961C (en) | 2004-12-28 | 2013-11-26 | Exelixis, Inc. | [1h-pyrazolo[3,4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-threonine kinase modulators (p70s6k, atk1 and atk2) for the treatment of immunological, inflammatory and proliferative diseases |
| GB0501999D0 (en) | 2005-02-01 | 2005-03-09 | Sentinel Oncology Ltd | Pharmaceutical compounds |
| EP1902032A1 (en) | 2005-06-22 | 2008-03-26 | Astex Therapeutics Limited | Pharmaceutical compounds |
| NZ595087A (en) | 2009-02-11 | 2013-03-28 | Merck Patent Gmbh | Novel amino azaheterocyclic carboxamides |
| SG11201402387WA (en) * | 2011-12-22 | 2014-09-26 | Merck Patent Gmbh | Novel heterocyclic carboxamides as modulators of kinase activity |
| JP6223563B2 (ja) * | 2013-10-14 | 2017-11-01 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 選択的に置換されたキノリン化合物 |
| CN105636945B (zh) * | 2013-10-14 | 2017-11-17 | 卫材R&D管理有限公司 | 选择性取代的喹啉化合物 |
-
2012
- 2012-12-17 SG SG11201402387WA patent/SG11201402387WA/en unknown
- 2012-12-17 PT PT128086402T patent/PT2794571T/pt unknown
- 2012-12-17 PL PL12808640T patent/PL2794571T3/pl unknown
- 2012-12-17 CN CN201280063286.7A patent/CN104169258B/zh not_active Expired - Fee Related
- 2012-12-17 CA CA2856448A patent/CA2856448C/en active Active
- 2012-12-17 HU HUE12808640A patent/HUE032918T2/hu unknown
- 2012-12-17 SI SI201230854A patent/SI2794571T1/sl unknown
- 2012-12-17 AU AU2012355494A patent/AU2012355494B2/en not_active Ceased
- 2012-12-17 DK DK12808640.2T patent/DK2794571T3/en active
- 2012-12-17 EA EA201400736A patent/EA027968B1/ru not_active IP Right Cessation
- 2012-12-17 EA EA201791073A patent/EA201791073A1/ru unknown
- 2012-12-17 US US14/359,937 patent/US9139568B2/en not_active Expired - Fee Related
- 2012-12-17 WO PCT/US2012/070085 patent/WO2013096194A1/en not_active Ceased
- 2012-12-17 RS RS20170071A patent/RS55621B1/sr unknown
- 2012-12-17 KR KR1020147017395A patent/KR102098358B1/ko not_active Expired - Fee Related
- 2012-12-17 HR HRP20170099TT patent/HRP20170099T1/hr unknown
- 2012-12-17 LT LTEP12808640.2T patent/LT2794571T/lt unknown
- 2012-12-17 EP EP12808640.2A patent/EP2794571B1/en active Active
- 2012-12-17 BR BR112014015327-2A patent/BR112014015327B1/pt not_active IP Right Cessation
- 2012-12-17 ES ES12808640.2T patent/ES2614232T3/es active Active
- 2012-12-17 SG SG10201604799TA patent/SG10201604799TA/en unknown
- 2012-12-17 JP JP2014549176A patent/JP6193880B2/ja not_active Expired - Fee Related
- 2012-12-17 MX MX2014007364A patent/MX353062B/es active IP Right Grant
-
2014
- 2014-05-15 ZA ZA2014/03517A patent/ZA201403517B/en unknown
- 2014-06-17 IL IL233199A patent/IL233199B/en active IP Right Grant
-
2015
- 2015-09-08 US US14/847,561 patent/US20160058763A1/en not_active Abandoned
-
2016
- 2016-08-03 US US15/227,017 patent/US10080753B2/en active Active
-
2017
- 2017-08-10 JP JP2017155667A patent/JP6553686B2/ja not_active Expired - Fee Related
- 2017-10-06 AU AU2017239625A patent/AU2017239625B2/en not_active Ceased
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