JP2015508085A5 - - Google Patents
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- Publication number
- JP2015508085A5 JP2015508085A5 JP2014558027A JP2014558027A JP2015508085A5 JP 2015508085 A5 JP2015508085 A5 JP 2015508085A5 JP 2014558027 A JP2014558027 A JP 2014558027A JP 2014558027 A JP2014558027 A JP 2014558027A JP 2015508085 A5 JP2015508085 A5 JP 2015508085A5
- Authority
- JP
- Japan
- Prior art keywords
- formula
- conh
- compound
- het
- boronic acid
- 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
- 150000001875 compounds Chemical class 0.000 claims description 18
- 230000002503 metabolic effect Effects 0.000 claims description 3
- 238000000034 method Methods 0.000 claims description 2
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 10
- 239000003814 drug Substances 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 206010028980 Neoplasm Diseases 0.000 claims 7
- 230000002265 prevention Effects 0.000 claims 6
- 239000012453 solvate Substances 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 5
- 238000006069 Suzuki reaction reaction Methods 0.000 claims 4
- -1 benzo-1,3-dioxolyl Chemical group 0.000 claims 4
- 125000005620 boronic acid group Chemical group 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 241000222722 Leishmania <genus> Species 0.000 claims 2
- 241000186367 Mycobacterium avium Species 0.000 claims 2
- 239000011149 active material Substances 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 210000002784 stomach Anatomy 0.000 claims 2
- 125000003831 tetrazolyl group Chemical group 0.000 claims 2
- 208000010507 Adenocarcinoma of Lung Diseases 0.000 claims 1
- 206010027654 Allergic conditions Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 201000003076 Angiosarcoma Diseases 0.000 claims 1
- 208000018084 Bone neoplasm Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 208000005145 Cerebral amyloid angiopathy Diseases 0.000 claims 1
- 206010008111 Cerebral haemorrhage Diseases 0.000 claims 1
- 208000005243 Chondrosarcoma Diseases 0.000 claims 1
- 208000010859 Creutzfeldt-Jakob disease Diseases 0.000 claims 1
- 201000003883 Cystic fibrosis Diseases 0.000 claims 1
- 201000010374 Down Syndrome Diseases 0.000 claims 1
- 208000006168 Ewing Sarcoma Diseases 0.000 claims 1
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 1
- 208000007465 Giant cell arteritis Diseases 0.000 claims 1
- 208000001258 Hemangiosarcoma Diseases 0.000 claims 1
- 241000711549 Hepacivirus C Species 0.000 claims 1
- 241000701044 Human gammaherpesvirus 4 Species 0.000 claims 1
- 241000725303 Human immunodeficiency virus Species 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 241000186362 Mycobacterium leprae Species 0.000 claims 1
- 208000034176 Neoplasms, Germ Cell and Embryonal Diseases 0.000 claims 1
- 201000004404 Neurofibroma Diseases 0.000 claims 1
- 208000036110 Neuroinflammatory disease Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 241000224016 Plasmodium Species 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 208000025747 Rheumatic disease Diseases 0.000 claims 1
- 241000700584 Simplexvirus Species 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 206010044688 Trisomy 21 Diseases 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 210000003679 cervix uteri Anatomy 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 208000035250 cutaneous malignant susceptibility to 1 melanoma Diseases 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 210000000981 epithelium Anatomy 0.000 claims 1
- 210000003238 esophagus Anatomy 0.000 claims 1
- 210000003754 fetus Anatomy 0.000 claims 1
- 125000004612 furopyridinyl group Chemical group O1C(=CC2=C1C=CC=N2)* 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 210000004602 germ cell Anatomy 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 210000003128 head Anatomy 0.000 claims 1
- 230000002489 hematologic effect Effects 0.000 claims 1
- 210000005096 hematological system Anatomy 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 230000001900 immune effect Effects 0.000 claims 1
- 210000000987 immune system Anatomy 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 230000004968 inflammatory condition Effects 0.000 claims 1
- 210000000936 intestine Anatomy 0.000 claims 1
- 208000037906 ischaemic injury Diseases 0.000 claims 1
- 125000001786 isothiazolyl group Chemical group 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 210000000867 larynx Anatomy 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 201000005249 lung adenocarcinoma Diseases 0.000 claims 1
- 208000037841 lung tumor Diseases 0.000 claims 1
- 210000004324 lymphatic system Anatomy 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 1
- 210000001616 monocyte Anatomy 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 210000003739 neck Anatomy 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 230000000552 rheumatic effect Effects 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 1
- 206010043207 temporal arteritis Diseases 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 230000001732 thrombotic effect Effects 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- 210000003932 urinary bladder Anatomy 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
- 238000002360 preparation method Methods 0.000 description 2
- 239000000376 reactant Substances 0.000 description 2
- OKTJSMMVPCPJKN-NJFSPNSNSA-N Carbon-14 Chemical compound [14C] OKTJSMMVPCPJKN-NJFSPNSNSA-N 0.000 description 1
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 description 1
- YZCKVEUIGOORGS-NJFSPNSNSA-N Tritium Chemical compound [3H] YZCKVEUIGOORGS-NJFSPNSNSA-N 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 229910052805 deuterium Inorganic materials 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 230000002285 radioactive effect Effects 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 230000002194 synthesizing effect Effects 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 238000003354 tissue distribution assay Methods 0.000 description 1
- 229910052722 tritium Inorganic materials 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12001154.9 | 2012-02-21 | ||
| EP12001154 | 2012-02-21 | ||
| PCT/EP2013/000188 WO2013124025A1 (en) | 2012-02-21 | 2013-01-22 | Furopyridine derivatives |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015508085A JP2015508085A (ja) | 2015-03-16 |
| JP2015508085A5 true JP2015508085A5 (https=) | 2016-03-10 |
| JP6097770B2 JP6097770B2 (ja) | 2017-03-15 |
Family
ID=47628096
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014558027A Expired - Fee Related JP6097770B2 (ja) | 2012-02-21 | 2013-01-22 | フロピリジン誘導体 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20150038527A1 (https=) |
| EP (1) | EP2817313B1 (https=) |
| JP (1) | JP6097770B2 (https=) |
| CN (1) | CN104114558B (https=) |
| AR (1) | AR090105A1 (https=) |
| AU (1) | AU2013224420B2 (https=) |
| CA (1) | CA2863717C (https=) |
| ES (1) | ES2606638T3 (https=) |
| TW (1) | TW201336850A (https=) |
| WO (1) | WO2013124025A1 (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2015117950A (ru) * | 2012-10-26 | 2016-12-20 | Ф. Хоффманн-Ля Рош Аг | 3,4-дизамещенный 1н-пиразол и 4,5-дизамещенный тиазол в качестве ингибиторов тирозинкиназы syk |
| CZ2014295A3 (cs) * | 2014-04-30 | 2015-10-14 | Masarykova Univerzita | Substituované furo[3,2-b]pyridiny pro použití jako léčiva |
| EP3313834A1 (en) * | 2015-06-29 | 2018-05-02 | Merck Patent GmbH | Tbk/ikk inhibitor compounds and uses thereof |
| EP3746071A4 (en) | 2018-01-29 | 2021-09-01 | Merck Patent GmbH | GCN2 INHIBITORS AND THEIR USES |
| KR20200116481A (ko) * | 2018-01-29 | 2020-10-12 | 메르크 파텐트 게엠베하 | Gcn2 억제제 및 이의 용도 |
| US20220143049A1 (en) | 2019-03-21 | 2022-05-12 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| KR102904576B1 (ko) * | 2019-05-09 | 2025-12-24 | 브리스톨-마이어스 스큅 컴퍼니 | 치환된 벤즈이미다졸론 화합물 |
| EP4054579A1 (en) | 2019-11-08 | 2022-09-14 | Institut National de la Santé et de la Recherche Médicale (INSERM) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| US20250304593A1 (en) * | 2022-05-12 | 2025-10-02 | Skyhawk Therapeutics, Inc. | Compositions useful for modulating splicing |
| JP2025531008A (ja) | 2022-08-09 | 2025-09-19 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング | フロピリミジン誘導体 |
| WO2024033280A1 (en) | 2022-08-09 | 2024-02-15 | Merck Patent Gmbh | Furopyridin and furopyrimidin, inhibitors of pi4k, for use in the treatment of parasite infection and malaria |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE247469T1 (de) * | 1995-06-07 | 2003-09-15 | Pfizer | Heterocyclische kondensierte pyrimidin-derivate |
| GB9624482D0 (en) | 1995-12-18 | 1997-01-15 | Zeneca Phaema S A | Chemical compounds |
| BR9707495A (pt) | 1996-02-13 | 1999-07-27 | Zeneca Ltd | Derivado de quinazolina processo para a preparação do mesmo composição farmacêutica e processo para a produç o de um efeito antiangiogênico e/ou de redução de permeabilidade vascular em um animal de sangue quente |
| US6291455B1 (en) | 1996-03-05 | 2001-09-18 | Zeneca Limited | 4-anilinoquinazoline derivatives |
| GB9718972D0 (en) | 1996-09-25 | 1997-11-12 | Zeneca Ltd | Chemical compounds |
| GB9714249D0 (en) | 1997-07-08 | 1997-09-10 | Angiogene Pharm Ltd | Vascular damaging agents |
| US6187777B1 (en) * | 1998-02-06 | 2001-02-13 | Amgen Inc. | Compounds and methods which modulate feeding behavior and related diseases |
| GB9900334D0 (en) | 1999-01-07 | 1999-02-24 | Angiogene Pharm Ltd | Tricylic vascular damaging agents |
| GB9900752D0 (en) | 1999-01-15 | 1999-03-03 | Angiogene Pharm Ltd | Benzimidazole vascular damaging agents |
| OA12514A (en) * | 1999-12-24 | 2006-05-29 | Aventis Pharma Ltd | Azaindoles. |
| NZ522074A (en) | 2000-05-31 | 2004-06-25 | Astrazeneca Ab | Indole derivatives with vascular damaging activity |
| US20020004511A1 (en) * | 2000-06-28 | 2002-01-10 | Luzzio Michael Joseph | Thiophene derivatives useful as anticancer agents |
| IL153484A0 (en) | 2000-07-07 | 2003-07-06 | Angiogene Pharm Ltd | Colchinol derivatives as angiogenesis inhibitors |
| CN1255392C (zh) | 2000-07-07 | 2006-05-10 | 安吉奥金尼药品有限公司 | 作为血管生成抑制剂的秋水仙醇衍生物 |
| WO2008118823A2 (en) | 2007-03-26 | 2008-10-02 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| SG2014015085A (en) | 2008-04-16 | 2014-06-27 | Portola Pharm Inc | 2,6-diamino-pyrimidin-5-yl-carboxamides as syk or jak kinases inhibitors |
| TWI453207B (zh) | 2008-09-08 | 2014-09-21 | Signal Pharm Llc | 胺基三唑并吡啶，其組合物及使用其之治療方法 |
| AU2011295441B2 (en) * | 2010-08-27 | 2015-04-09 | Merck Patent Gmbh | Furopyridine derivatives |
| DE102011009961A1 (de) * | 2011-02-01 | 2012-08-02 | Merck Patent Gmbh | 7-Azaindolderivate |
-
2013
- 2013-01-22 AU AU2013224420A patent/AU2013224420B2/en not_active Ceased
- 2013-01-22 ES ES13701707.5T patent/ES2606638T3/es active Active
- 2013-01-22 US US14/379,770 patent/US20150038527A1/en not_active Abandoned
- 2013-01-22 JP JP2014558027A patent/JP6097770B2/ja not_active Expired - Fee Related
- 2013-01-22 EP EP13701707.5A patent/EP2817313B1/en active Active
- 2013-01-22 CN CN201380010420.1A patent/CN104114558B/zh not_active Expired - Fee Related
- 2013-01-22 WO PCT/EP2013/000188 patent/WO2013124025A1/en not_active Ceased
- 2013-01-22 CA CA2863717A patent/CA2863717C/en active Active
- 2013-02-20 TW TW102105912A patent/TW201336850A/zh unknown
- 2013-02-21 AR ARP130100518A patent/AR090105A1/es unknown
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