JP2017502092A5 - - Google Patents
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- JP2017502092A5 JP2017502092A5 JP2016563905A JP2016563905A JP2017502092A5 JP 2017502092 A5 JP2017502092 A5 JP 2017502092A5 JP 2016563905 A JP2016563905 A JP 2016563905A JP 2016563905 A JP2016563905 A JP 2016563905A JP 2017502092 A5 JP2017502092 A5 JP 2017502092A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- pharmaceutically acceptable
- acceptable salt
- hydrogen
- alkyl
- 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.)
- Pending
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- 150000001875 compounds Chemical class 0.000 claims description 76
- 150000003839 salts Chemical class 0.000 claims description 69
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 64
- 229910052739 hydrogen Inorganic materials 0.000 claims description 58
- 239000001257 hydrogen Substances 0.000 claims description 58
- 125000000217 alkyl group Chemical group 0.000 claims description 47
- 229910052757 nitrogen Inorganic materials 0.000 claims description 41
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 38
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 36
- 229910052760 oxygen Inorganic materials 0.000 claims description 36
- 239000001301 oxygen Chemical group 0.000 claims description 36
- 229910052717 sulfur Chemical group 0.000 claims description 36
- 239000011593 sulfur Chemical group 0.000 claims description 36
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 34
- 125000005842 heteroatom Chemical group 0.000 claims description 34
- 125000000623 heterocyclic group Chemical group 0.000 claims description 23
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 22
- 125000001931 aliphatic group Chemical group 0.000 claims description 20
- 125000001624 naphthyl group Chemical group 0.000 claims description 18
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 18
- 150000002431 hydrogen Chemical class 0.000 claims description 17
- 125000005843 halogen group Chemical group 0.000 claims description 16
- 125000002947 alkylene group Chemical group 0.000 claims description 14
- 239000000203 mixture Substances 0.000 claims description 13
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 12
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 10
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 6
- 201000010099 disease Diseases 0.000 claims description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 4
- 101000605630 Homo sapiens Phosphatidylinositol 3-kinase catalytic subunit type 3 Proteins 0.000 claims description 4
- 102100038329 Phosphatidylinositol 3-kinase catalytic subunit type 3 Human genes 0.000 claims description 4
- 229910052799 carbon Inorganic materials 0.000 claims description 4
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 230000000694 effects Effects 0.000 claims description 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 4
- 125000001153 fluoro group Chemical group F* 0.000 claims description 4
- 125000001072 heteroaryl group Chemical group 0.000 claims description 4
- 208000027866 inflammatory disease Diseases 0.000 claims description 4
- 230000002062 proliferating effect Effects 0.000 claims description 4
- 229940124597 therapeutic agent Drugs 0.000 claims description 4
- 206010002198 Anaphylactic reaction Diseases 0.000 claims description 2
- 208000023275 Autoimmune disease Diseases 0.000 claims description 2
- 206010005003 Bladder cancer Diseases 0.000 claims description 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- 206010007572 Cardiac hypertrophy Diseases 0.000 claims description 2
- 208000006029 Cardiomegaly Diseases 0.000 claims description 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 206010014733 Endometrial cancer Diseases 0.000 claims description 2
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims description 2
- 208000032612 Glial tumor Diseases 0.000 claims description 2
- 206010018338 Glioma Diseases 0.000 claims description 2
- 206010019280 Heart failures Diseases 0.000 claims description 2
- 206010020751 Hypersensitivity Diseases 0.000 claims description 2
- 206010020772 Hypertension Diseases 0.000 claims description 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 206010038389 Renal cancer Diseases 0.000 claims description 2
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims description 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 2
- 208000007536 Thrombosis Diseases 0.000 claims description 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims description 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 2
- 208000038016 acute inflammation Diseases 0.000 claims description 2
- 230000006022 acute inflammation Effects 0.000 claims description 2
- 208000026935 allergic disease Diseases 0.000 claims description 2
- 230000007815 allergy Effects 0.000 claims description 2
- 230000036783 anaphylactic response Effects 0.000 claims description 2
- 208000003455 anaphylaxis Diseases 0.000 claims description 2
- 201000010881 cervical cancer Diseases 0.000 claims description 2
- 208000037976 chronic inflammation Diseases 0.000 claims description 2
- 230000006020 chronic inflammation Effects 0.000 claims description 2
- 208000029742 colonic neoplasm Diseases 0.000 claims description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 201000004101 esophageal cancer Diseases 0.000 claims description 2
- 206010017758 gastric cancer Diseases 0.000 claims description 2
- 208000005017 glioblastoma Diseases 0.000 claims description 2
- 201000010536 head and neck cancer Diseases 0.000 claims description 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 2
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 claims description 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 2
- 201000010982 kidney cancer Diseases 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 208000020816 lung neoplasm Diseases 0.000 claims description 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 2
- 201000001441 melanoma Diseases 0.000 claims description 2
- 201000002528 pancreatic cancer Diseases 0.000 claims description 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 2
- 201000011549 stomach cancer Diseases 0.000 claims description 2
- 201000002510 thyroid cancer Diseases 0.000 claims description 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 2
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 claims description 2
- 239000005483 tyrosine kinase inhibitor Substances 0.000 claims description 2
- 150000004917 tyrosine kinase inhibitor derivatives Chemical group 0.000 claims description 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 125000006714 (C3-C10) heterocyclyl group Chemical group 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 230000005764 inhibitory process Effects 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 241000162682 Heterogen Species 0.000 claims 1
- 229910017464 nitrogen compound Inorganic materials 0.000 claims 1
- 150000002830 nitrogen compounds Chemical class 0.000 claims 1
- 230000003287 optical effect Effects 0.000 description 3
- 239000003112 inhibitor Substances 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- LSBIUXKNVUBKRI-UHFFFAOYSA-N Cc1cc(C)ncn1 Chemical compound Cc1cc(C)ncn1 LSBIUXKNVUBKRI-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461927064P | 2014-01-14 | 2014-01-14 | |
| US61/927,064 | 2014-01-14 | ||
| US201462054757P | 2014-09-24 | 2014-09-24 | |
| US62/054,757 | 2014-09-24 | ||
| PCT/US2015/011250 WO2015108881A1 (en) | 2014-01-14 | 2015-01-13 | Heteroaryls and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017502092A JP2017502092A (ja) | 2017-01-19 |
| JP2017502092A5 true JP2017502092A5 (OSRAM) | 2018-02-08 |
Family
ID=53543368
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016563905A Pending JP2017502092A (ja) | 2014-01-14 | 2015-01-13 | ヘテロアリール及びその使用 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US10202373B2 (OSRAM) |
| EP (1) | EP3094326A4 (OSRAM) |
| JP (1) | JP2017502092A (OSRAM) |
| WO (1) | WO2015108881A1 (OSRAM) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10202373B2 (en) | 2014-01-14 | 2019-02-12 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| WO2015108861A1 (en) | 2014-01-14 | 2015-07-23 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| WO2017140841A1 (en) | 2016-02-19 | 2017-08-24 | Sprint Bioscience Ab | 6-aryl-4-morpholin-1-ylpyridone compounds useful for the treatment of cancer and diabetes |
| SMT202000529T1 (it) | 2016-02-19 | 2020-11-10 | Sprint Bioscience Ab | Composti di 6-eterociclil-4-morfolina-4-ilpiridin-2-one utili per il trattamento di cancro e diabete |
| DK3672948T3 (da) | 2017-08-23 | 2022-12-05 | Sprint Bioscience Ab | Pyridinamin-pyridon- og pyrimidinamin-pyridonforbindelser |
| JP7199736B2 (ja) | 2017-08-23 | 2023-01-06 | スプリント バイオサイエンス アクティエボラーグ | モルホリニルピリドン化合物 |
| CN111094244B (zh) | 2017-08-23 | 2023-07-11 | 思普瑞特生物科学公司 | 吡啶基吡啶酮化合物 |
| PT3672967T (pt) | 2017-08-23 | 2021-12-28 | Sprint Bioscience Ab | Compostos de azaindolilpiridona e diazaindolilpiridona |
| AU2020345950A1 (en) | 2019-09-11 | 2022-03-31 | Prelude Therapeutics Incorporated | CDK inhibitors and their use as pharmaceuticals |
| TW202320797A (zh) * | 2021-08-13 | 2023-06-01 | 美商迪賽孚爾製藥有限公司 | 使用ｖｐｓ３４抑制劑之組合療法 |
| EP4574830A4 (en) * | 2022-09-23 | 2025-11-26 | Guangzhou Vinnocent Pharmaceutical Ltd | PYRIDINE INHIBITOR, RINGED STEROID SYNTHETASE, ITS PREPARATION PROCESS AND ITS USE |
| CN120282963A (zh) * | 2022-11-10 | 2025-07-08 | 目标医疗有限责任公司 | 人醛固酮合成酶(cyp11b2)抑制剂 |
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| WO2004041789A1 (en) | 2002-11-01 | 2004-05-21 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of jak and other protein kinases |
| FR2850652B1 (fr) | 2003-01-31 | 2008-05-30 | Aventis Pharma Sa | Nouveaux derives d'uree cyclique, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de kinases |
| CA2545384A1 (en) | 2003-11-10 | 2005-05-26 | Merck Sharp & Dohme Limited | Substituted nitrogen-containing six-membered amino-heterocycles as vanilloid-1 receptor antagonists for treating pain |
| SE0402735D0 (sv) | 2004-11-09 | 2004-11-09 | Astrazeneca Ab | Novel compounds |
| JP2008519814A (ja) | 2004-11-12 | 2008-06-12 | ガラパゴス・ナムローゼ・フェンノートシャップ | プロテインキナーゼ酵素の活性部位と結合する窒素複素環式芳香族化合物 |
| US8101770B2 (en) | 2004-12-16 | 2012-01-24 | Vertex Pharmaceuticals Incorporated | Pyridones useful as inhibitors of kinases |
| US7601716B2 (en) | 2006-05-01 | 2009-10-13 | Cephalon, Inc. | Pyridopyrazines and derivatives thereof as ALK and c-Met inhibitors |
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| BRPI0716239A2 (pt) | 2006-08-30 | 2013-08-13 | Cellzome Ltd | derivados de triazol como inibidores de cinase |
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| EA018824B1 (ru) | 2008-11-11 | 2013-10-30 | Эли Лилли Энд Компани | КОМБИНИРОВАННАЯ ТЕРАПИЯ ИНГИБИТОРОМ КИНАЗЫ p70 S6 И ИНГИБИТОРОМ mTOR |
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| US8071605B2 (en) | 2008-12-12 | 2011-12-06 | Astrazeneca Ab | Piperidine compounds for use in the treatment of bacterial infections |
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| US20110130380A1 (en) | 2009-09-04 | 2011-06-02 | Barsanti Paul A | Heteroaryl Kinase Inhibitors |
| SG182803A1 (en) | 2010-02-05 | 2012-09-27 | Merck Patent Gmbh | Hetaryl-[1,8]naphthyridine derivatives |
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| ES2550939T3 (es) | 2010-07-16 | 2015-11-13 | Nivalis Therapeutics, Inc. | Nuevos compuestos de dihidropiridin-2-(1H)-ona como inhibidores de la S-nitrosoglutatión reductasa y antagonistas del receptor de la neurocinina-3 |
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| KR101502500B1 (ko) | 2011-07-01 | 2015-03-16 | 주식회사 엘지화학 | 비수 전해액 및 이를 이용한 리튬 이차전지 |
| UA111382C2 (uk) | 2011-10-10 | 2016-04-25 | Оріон Корпорейшн | Інгібітори протеїнкінази |
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| EP2817292B1 (en) | 2012-02-22 | 2019-12-18 | Sanford-Burnham Medical Research Institute | Sulfonamide compounds and uses as tnap inhibitors |
| EP2855472B1 (en) | 2012-04-05 | 2016-09-14 | Boehringer Ingelheim International GmbH | Naphthyridinone derivatives as inhibitors of cytomegalovirus dna polymerase |
| FR2992314B1 (fr) | 2012-06-22 | 2015-10-16 | Sanofi Sa | Nouveaux derives de 2,3-dihydro-1h-imidazo{1,2-a}pyrimidin-5-one et 1,2,3,4-tetrahydro-pyrimido{1,2-a}pyrimidin-6-one comportant une morpholine substituee, leur preparation et leur utilisation pharmaceutique |
| WO2014058691A1 (en) | 2012-10-08 | 2014-04-17 | Merck Sharp & Dohme Corp. | Inhibitors of irak4 activity |
| WO2014083327A1 (en) | 2012-11-27 | 2014-06-05 | Md Pharma Ab | Adenine derivatives suitable for the treatment of (inter alia) muscular dystrophy |
| GB201223265D0 (en) | 2012-12-21 | 2013-02-06 | Selvita Sa | Novel benzimidazole derivatives as kinase inhibitors |
| JP6114313B2 (ja) | 2013-01-11 | 2017-05-24 | 富士フイルム株式会社 | 含窒素複素環化合物またはその塩 |
| US9242969B2 (en) | 2013-03-14 | 2016-01-26 | Novartis Ag | Biaryl amide compounds as kinase inhibitors |
| US10202373B2 (en) | 2014-01-14 | 2019-02-12 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| WO2015108861A1 (en) | 2014-01-14 | 2015-07-23 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
-
2015
- 2015-01-13 US US15/111,429 patent/US10202373B2/en active Active
- 2015-01-13 JP JP2016563905A patent/JP2017502092A/ja active Pending
- 2015-01-13 EP EP15737300.2A patent/EP3094326A4/en not_active Withdrawn
- 2015-01-13 WO PCT/US2015/011250 patent/WO2015108881A1/en not_active Ceased
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