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
Links
- 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 (https=) | 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 (https=) |
| EP (1) | EP3094326A4 (https=) |
| JP (1) | JP2017502092A (https=) |
| WO (1) | WO2015108881A1 (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015108881A1 (en) | 2014-01-14 | 2015-07-23 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| AU2015206652A1 (en) | 2014-01-14 | 2016-08-04 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| DK3416957T3 (da) | 2016-02-19 | 2020-09-21 | Sprint Bioscience Ab | 6-heterocyclyl-4-morpholin-4-ylpyridin-2-on-forbindelser anvendelige ved behandlingen af cancer og diabetes |
| AU2017219846B2 (en) | 2016-02-19 | 2021-05-13 | Sprint Bioscience Ab | 6-aryl-4-morpholin-1-ylpyridone compounds useful for the treatment of cancer and diabetes |
| JP7199738B2 (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 | アザインドリルピリドンおよびジアザインドリルピリドン化合物 |
| WO2019038387A1 (en) | 2017-08-23 | 2019-02-28 | Sprint Bioscience Ab | PYRIDYLPYRIDONE COMPOUNDS |
| US11560374B2 (en) | 2017-08-23 | 2023-01-24 | Sprint Bioscience Ab | Morpholinylpyridone compounds |
| CN111094271B (zh) | 2017-08-23 | 2023-02-28 | 思普瑞特生物科学公司 | 吡啶胺-吡啶酮化合物和嘧啶胺-吡啶酮化合物 |
| US20220324830A1 (en) * | 2019-09-11 | 2022-10-13 | Prelude Therapeutics, Incorporated | CDK Inhibitors And Their Use As Pharmaceuticals |
| AU2022326573A1 (en) * | 2021-08-13 | 2024-02-15 | Deciphera Pharmaceuticals, Llc | Combination therapy of vps34 inhibitors and sting agonist for use in the treatment of cancer |
| EP4574830A4 (en) * | 2022-09-23 | 2025-11-26 | Guangzhou Vinnocent Pharmaceutical Ltd | PYRIDINE INHIBITOR, RINGED STEROID SYNTHETASE, ITS PREPARATION PROCESS AND ITS USE |
| AU2023378302A1 (en) * | 2022-11-10 | 2025-04-10 | «Target Medicals» Limited Liability Company | Inhibitors of human aldosterone synthase (cyp11b2) |
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| JP2006512314A (ja) | 2002-11-01 | 2006-04-13 | バーテックス ファーマシューティカルズ インコーポレイテッド | Ｊａｋインヒビターおよび他のプロテインキナーゼインヒビターとしての組成物の使用 |
| 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 |
| EP1685124A1 (en) | 2003-11-10 | 2006-08-02 | MERCK SHARP & DOHME LTD. | 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 |
| EP1814856A1 (en) | 2004-11-12 | 2007-08-08 | Galapagos N.V. | Nitrogen heteroaromatic compounds which bind to the active site of protein kinase enzymes |
| CA2591413A1 (en) | 2004-12-16 | 2006-06-22 | Vertex Pharmaceuticals Incorporated | Pyrid-2-ones useful as inhibitors of tec family protein kinases for the treatment of inflammatory, proliferative and immunologically-mediated diseases |
| US7601716B2 (en) | 2006-05-01 | 2009-10-13 | Cephalon, Inc. | Pyridopyrazines and derivatives thereof as ALK and c-Met inhibitors |
| WO2007135398A1 (en) | 2006-05-22 | 2007-11-29 | Astrazeneca Ab | Indole derivatives |
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| JP2010539239A (ja) | 2007-09-17 | 2010-12-16 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー | Ｐｉ３キナーゼ阻害剤としてのピリドピリミジン誘導体 |
| US20100311736A1 (en) | 2007-10-22 | 2010-12-09 | Glaxosmithkline Llc | Pyridosulfonamide derivatives as p13 kinase inhibitors |
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| US8309577B2 (en) | 2008-04-23 | 2012-11-13 | Bristol-Myers Squibb Company | Quinuclidine compounds as α-7 nicotinic acetylcholine receptor ligands |
| JP5599783B2 (ja) | 2008-05-30 | 2014-10-01 | アムジエン・インコーポレーテツド | Ｐｉ３キナーゼの阻害薬 |
| ES2566339T3 (es) | 2008-06-05 | 2016-04-12 | Glaxo Group Limited | Derivados de 4-carboxamida indazol útiles como inhibidores de PI3-quinasas |
| WO2010008847A2 (en) | 2008-06-24 | 2010-01-21 | Takeda Pharmaceutical Company Limited | Pi3k/m tor inhibitors |
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| JP5693452B2 (ja) | 2008-08-04 | 2015-04-01 | シーエイチディーアイ ファウンデーション，インコーポレーテッド | 特定のキヌレニン−３−モノオキシゲナーゼインヒビター、医薬組成物およびそれらの使用方法 |
| CA2743242A1 (en) | 2008-11-11 | 2010-05-20 | Eli Lilly And Company | P70 s6 kinase inhibitor and mtor inhibitor combination therapy |
| WO2010057877A1 (en) | 2008-11-18 | 2010-05-27 | Cellzome Limited | 7-pyridinyl- or phenyl- substituted triazolo [1, 5 -a] pyridines as pi3k inhibitors |
| TW201026695A (en) | 2008-12-12 | 2010-07-16 | Astrazeneca Ab | Piperidine compounds and uses thereof-596 |
| BRPI1010974A2 (pt) | 2009-05-22 | 2019-09-24 | Exelixis Inc | benzoxazepinas baseada em inibidores p13k/ m tor contra doenças proliferativas |
| CA2767089A1 (en) | 2009-07-15 | 2011-01-20 | Abbott Laboratories | Pyrrolopyridine inhibitors of kinases |
| WO2011026911A1 (en) | 2009-09-04 | 2011-03-10 | Novartis Ag | Bipyridines useful for the treatment of proliferative diseases |
| AU2010344973B2 (en) | 2010-02-05 | 2016-06-16 | Merck Patent Gmbh | Hetaryl-[1,8]naphthyridine derivatives |
| MX2012014537A (es) | 2010-07-05 | 2013-02-21 | Merck Patent Gmbh | Derivados de bipiridilo utiles para el tratamiento de enfermedades inducidas por cinasa. |
| 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 |
| CN103209960A (zh) | 2010-07-26 | 2013-07-17 | 百时美施贵宝公司 | 用作cyp17抑制剂的磺酰胺化合物 |
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| WO2012066065A1 (en) | 2010-11-17 | 2012-05-24 | Novartis Ag | Phenyl-heteroaryl amine compounds and their uses |
| AU2011346567A1 (en) | 2010-12-21 | 2013-07-25 | Novartis Ag | Bi-heteroaryl compounds as Vps34 inhibitors |
| DK2655375T3 (en) | 2010-12-23 | 2015-03-09 | Sanofi Sa | PYRIMIDINON DERIVATIVES, PREPARATION AND PHARMACEUTICAL USE THEREOF |
| WO2012101064A1 (en) | 2011-01-28 | 2012-08-02 | Novartis Ag | N-acyl pyrimidine biaryl compounds as protein kinase inhibitors |
| JP2014506878A (ja) | 2011-01-28 | 2014-03-20 | ノバルティス アーゲー | Ｃｄｋ９阻害剤としての置換ビ−ヘテロアリール化合物およびそれらの使用 |
| WO2012101066A1 (en) | 2011-01-28 | 2012-08-02 | Novartis Ag | Pyridine biaryl amine compounds and their uses |
| DE102011077104A1 (de) | 2011-06-07 | 2012-12-13 | Siemens Aktiengesellschaft | Verfahren zur Gewinnung von metallhaltigen Wertstoffen aus einem metallhaltige Wertstoffe enthaltenden suspensionsartigen Massestrom |
| 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 |
| WO2013096630A1 (en) | 2011-12-23 | 2013-06-27 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| 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 |
| RU2655604C2 (ru) | 2013-01-11 | 2018-05-29 | Фуджифилм Корпорэйшн | Азотсодержащее гетероциклическое соединение или его соль |
| US9242969B2 (en) | 2013-03-14 | 2016-01-26 | Novartis Ag | Biaryl amide compounds as kinase inhibitors |
| WO2015108881A1 (en) | 2014-01-14 | 2015-07-23 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| AU2015206652A1 (en) | 2014-01-14 | 2016-08-04 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
-
2015
- 2015-01-13 WO PCT/US2015/011250 patent/WO2015108881A1/en not_active Ceased
- 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
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