JP2017514809A5 - - Google Patents
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- Publication number
- JP2017514809A5 JP2017514809A5 JP2016563080A JP2016563080A JP2017514809A5 JP 2017514809 A5 JP2017514809 A5 JP 2017514809A5 JP 2016563080 A JP2016563080 A JP 2016563080A JP 2016563080 A JP2016563080 A JP 2016563080A JP 2017514809 A5 JP2017514809 A5 JP 2017514809A5
- Authority
- JP
- Japan
- Prior art keywords
- aliphatic
- occurrence
- independently selected
- membered
- nitrogen
- 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
- 125000001931 aliphatic group Chemical group 0.000 claims description 157
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 111
- 229910052760 oxygen Inorganic materials 0.000 claims description 90
- 229910052757 nitrogen Inorganic materials 0.000 claims description 82
- 229910052717 sulfur Inorganic materials 0.000 claims description 78
- 229910052739 hydrogen Inorganic materials 0.000 claims description 72
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 63
- 125000005842 heteroatom Chemical group 0.000 claims description 63
- 239000001301 oxygen Chemical group 0.000 claims description 63
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 56
- 239000001257 hydrogen Substances 0.000 claims description 56
- 239000011593 sulfur Chemical group 0.000 claims description 56
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 41
- 150000003839 salts Chemical class 0.000 claims description 39
- 229910052736 halogen Inorganic materials 0.000 claims description 36
- 150000002367 halogens Chemical class 0.000 claims description 36
- 125000000623 heterocyclic group Chemical group 0.000 claims description 36
- 150000001875 compounds Chemical class 0.000 claims description 34
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 29
- 125000004429 atom Chemical group 0.000 claims description 28
- 229910052731 fluorine Inorganic materials 0.000 claims description 25
- 229910052799 carbon Inorganic materials 0.000 claims description 20
- 125000003118 aryl group Chemical group 0.000 claims description 18
- 229920006395 saturated elastomer Polymers 0.000 claims description 18
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims description 14
- 125000001072 heteroaryl group Chemical group 0.000 claims description 14
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 12
- 125000002947 alkylene group Chemical group 0.000 claims description 12
- 150000002431 hydrogen Chemical class 0.000 claims description 9
- 102000015532 Nicotinamide phosphoribosyltransferase Human genes 0.000 claims description 8
- 108010064862 Nicotinamide phosphoribosyltransferase Proteins 0.000 claims description 8
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 6
- 230000001404 mediated effect Effects 0.000 claims description 6
- 125000002619 bicyclic group Chemical group 0.000 claims description 4
- 125000004432 carbon atom Chemical group C* 0.000 claims description 4
- 210000004027 cell Anatomy 0.000 claims description 4
- -1 cycloaliphatic Chemical group 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 230000000694 effects Effects 0.000 claims description 4
- 230000002401 inhibitory effect Effects 0.000 claims description 4
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 3
- 239000011737 fluorine Substances 0.000 claims description 3
- 230000002265 prevention Effects 0.000 claims description 3
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 2
- 208000023275 Autoimmune disease Diseases 0.000 claims description 2
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical class C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims description 2
- 206010028980 Neoplasm Diseases 0.000 claims description 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 2
- 210000001744 T-lymphocyte Anatomy 0.000 claims description 2
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical class C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims description 2
- 230000002159 abnormal effect Effects 0.000 claims description 2
- 201000011510 cancer Diseases 0.000 claims description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 2
- 208000035475 disorder Diseases 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000003463 hyperproliferative effect Effects 0.000 claims description 2
- 230000004968 inflammatory condition Effects 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 125000002950 monocyclic group Chemical group 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 229940124597 therapeutic agent Drugs 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 9
- 238000000034 method Methods 0.000 description 9
- 230000010261 cell growth Effects 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461981273P | 2014-04-18 | 2014-04-18 | |
| US61/981,273 | 2014-04-18 | ||
| JO74/2015 | 2015-04-16 | ||
| JOP20150074 | 2015-04-16 | ||
| PCT/US2015/026275 WO2015161142A1 (en) | 2014-04-18 | 2015-04-17 | Quinoxaline compounds and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017514809A JP2017514809A (ja) | 2017-06-08 |
| JP2017514809A5 true JP2017514809A5 (OSRAM) | 2018-05-10 |
| JP6510556B2 JP6510556B2 (ja) | 2019-05-08 |
Family
ID=54324592
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016563080A Expired - Fee Related JP6510556B2 (ja) | 2014-04-18 | 2015-04-17 | キノキサリン化合物及びその使用 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US10144742B2 (OSRAM) |
| EP (1) | EP3131881A4 (OSRAM) |
| JP (1) | JP6510556B2 (OSRAM) |
| CN (1) | CN106458934B (OSRAM) |
| BR (1) | BR112016024298A2 (OSRAM) |
| CA (1) | CA2946130A1 (OSRAM) |
| EA (1) | EA201692091A1 (OSRAM) |
| TW (1) | TW201625578A (OSRAM) |
| WO (1) | WO2015161142A1 (OSRAM) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107438598A (zh) | 2015-01-20 | 2017-12-05 | 米伦纽姆医药公司 | 喹唑啉和喹啉化合物及其用途 |
| US12486318B2 (en) | 2016-06-15 | 2025-12-02 | Yale University | Anti-guanosine antibody as a molecular delivery vehicle |
| WO2018075600A1 (en) | 2016-10-18 | 2018-04-26 | Seattle Genetics, Inc. | Targeted delivery of nicotinamide adenine dinucleotide salvage pathway inhibitors |
| JP7595413B2 (ja) | 2016-11-30 | 2024-12-06 | ケース ウエスタン リザーブ ユニバーシティ | １５－ｐｇｄｈ阻害剤とコルチコステロイドおよび／またはｔｎｆ阻害剤との組み合わせならびにその使用 |
| CN106883188B (zh) * | 2017-01-19 | 2020-06-30 | 上海交通大学 | 一种5-氢-1, 4-苯并二氮杂卓类化合物及其合成方法 |
| CA3052466A1 (en) * | 2017-02-06 | 2018-08-09 | Case Western Reserve University | Compositions and methods of modulating short-chain dehydrogenase activity |
| CN110891568A (zh) | 2017-04-07 | 2020-03-17 | 凯斯西储大学 | 用于治疗冠状动脉病症的短链脱氢酶活性的抑制剂 |
| US11931414B2 (en) | 2017-04-27 | 2024-03-19 | Seagen Inc. | Quaternized nicotinamide adenine dinucleotide salvage pathway inhibitor conjugates |
| US20210137960A1 (en) * | 2018-02-01 | 2021-05-13 | Yale University | Compositions and methods for inhibition of nuclear-penetrating antibodies |
| EP3870166A4 (en) * | 2018-10-22 | 2022-09-28 | Yale University | IDENTIFICATION OF PPM1D MUTATIONS AS NOVEL BIOMARKERS OF NAMPTI SENSITIVITY |
| CA3120858A1 (en) | 2018-11-21 | 2020-05-28 | Case Western Reserve University | Compositions and methods of modulating short-chain dehydrogenase activity |
| WO2021102370A1 (en) * | 2019-11-21 | 2021-05-27 | University Of Pittsburgh - Of The Commonwealth System Of Higher Education | METHODS AND MATERIALS FOR INHIBITING NF-kB ACTIVITY |
| WO2022109311A1 (en) * | 2020-11-20 | 2022-05-27 | University Of Pittsburgh - Of The Commonwealth System Of Higher Education | Methods and materials for increasing nicotinamide phosphoribosyltransferase activity |
| US20230321086A1 (en) * | 2020-11-20 | 2023-10-12 | Universiy of Pittsburgh - of the Commonwealth System of Higher Education | Methods and materials for inhibiting nicotinamide phosphoribosyltransferase activity |
| AU2021401429A1 (en) * | 2020-12-18 | 2023-07-06 | The Scripps Research Institute | Compounds and use thereof for treatment of neurodegenerative, degenerative and metabolic disorders |
| CN114573517B (zh) * | 2022-03-10 | 2024-04-26 | 新乡医学院 | 一种喹喔啉类化合物及其制备方法与应用 |
| WO2023178035A1 (en) | 2022-03-14 | 2023-09-21 | Slap Pharmaceuticals Llc | Multicyclic compounds |
| EP4568668A2 (en) * | 2022-08-11 | 2025-06-18 | MapLight Therapeutics, Inc. | Gpr6 inverse agonists |
| TW202509018A (zh) * | 2023-05-09 | 2025-03-01 | 美商安進公司 | 用作１５－前列腺素脫氫酶調節劑的６，６－稠合雙環醯胺和組成物 |
| WO2025117536A1 (en) * | 2023-11-29 | 2025-06-05 | University Of Pittsburgh – Of The Commonwealth System Of Higher Education | Hormone receptor modulators |
Family Cites Families (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU1918299A (en) * | 1998-02-23 | 1999-09-06 | Warner-Lambert Company | Substituted quinoxaline derivatives as interleukin-8 receptor antagonists |
| AR043059A1 (es) * | 2002-11-12 | 2005-07-13 | Bayer Pharmaceuticals Corp | Derivados de indolil pirazinona utiles para el tratamiento de trastornos hiper-proliferativos |
| WO2004089416A2 (en) * | 2003-04-11 | 2004-10-21 | Novo Nordisk A/S | Combination of an 11beta-hydroxysteroid dehydrogenase type 1 inhibitor and an antihypertensive agent |
| US7189724B2 (en) | 2003-04-15 | 2007-03-13 | Valeant Research And Development | Quinoxaline derivatives having antiviral activity |
| WO2005007099A2 (en) * | 2003-07-10 | 2005-01-27 | Imclone Systems Incorporated | Pkb inhibitors as anti-tumor agents |
| JP2007099641A (ja) * | 2005-09-30 | 2007-04-19 | Tsumura & Co | インドールキノキサリン類化合物、その製造方法およびそれを用いた医薬組成物 |
| CN1966500B (zh) * | 2005-11-17 | 2011-03-30 | 中国科学院上海药物研究所 | 一类喹喔啉类衍生物、制法及用途 |
| US8119656B2 (en) | 2007-12-07 | 2012-02-21 | The Board Of Regents Of The University Of Texas System | Inhibitors of the influenza virus non-structural 1 protein |
| WO2009086303A2 (en) * | 2007-12-21 | 2009-07-09 | University Of Rochester | Method for altering the lifespan of eukaryotic organisms |
| RU2011111728A (ru) | 2008-08-29 | 2012-10-10 | Топотаргет А/С (Dk) | Новые производные мочевины и тиомочевины |
| CN101514192B (zh) * | 2009-04-02 | 2012-05-23 | 山东大学 | 具有逆转肿瘤细胞多药耐药活性的喹喔啉酮类衍生物及其制备方法 |
| CN102639503B (zh) | 2009-06-09 | 2014-10-15 | 顶标公司 | 作为烟酰胺磷酸核糖基转移酶抑制剂的吡啶基衍生物 |
| ES2534226T3 (es) | 2009-09-03 | 2015-04-20 | Bioenergenix | Compuestos heterocíclicos para la inhibición de PASK |
| CN102869261A (zh) | 2010-03-01 | 2013-01-09 | 瑞科西有限公司 | 化合物及其治疗应用 |
| US20130317027A1 (en) | 2010-03-01 | 2013-11-28 | Myrexis, Inc. | Compounds and therapeutic uses thereof |
| WO2011121055A1 (en) | 2010-03-31 | 2011-10-06 | Topotarget A/S | Pyridinyl derivatives comprising a cyanoguanidine or squaric acid moiety |
| WO2011121434A1 (en) | 2010-04-01 | 2011-10-06 | Council Of Scientific & Industrial Research | NICOTINAMIDE PHOSPHORIBOSYLTRANSFERASE (NMPRTase) INHIBITOR FOR GLIOMA THERAPY |
| CN106243023A (zh) | 2010-09-03 | 2016-12-21 | 福马Tm有限责任公司 | 用于抑制nampt的胍化合物和组合物 |
| RU2617424C2 (ru) | 2010-09-03 | 2017-04-25 | ФОРМА ТиЭм, ЭлЭлСИ | Новые соединения и композиции для ингибирования nampt |
| AR082885A1 (es) | 2010-09-03 | 2013-01-16 | Genentech Inc | Compuestos y composiciones para la inhibicion de nampt |
| CN103347860A (zh) | 2010-11-15 | 2013-10-09 | Abbvie公司 | Nampt抑制剂 |
| BR112013015397A2 (pt) * | 2010-12-23 | 2016-09-20 | Merck Sharp & Dohme | composto, composição farmacêutica, e, uso de um composto |
| JP5980812B2 (ja) | 2011-01-05 | 2016-08-31 | バイオエナジェニックス | Ｐａｓｋの阻害のための複素環化合物 |
| US20120225846A1 (en) | 2011-03-02 | 2012-09-06 | Bioenergenix | Heterocyclic compounds for the inhibition of pask |
| WO2012119046A2 (en) | 2011-03-02 | 2012-09-07 | Bioenergenix | Heterocyclic compounds for the inhibition of pask |
| US10953012B2 (en) | 2011-04-26 | 2021-03-23 | Bioenergenix Llc | Heterocyclic compounds for the inhibition of pask |
| WO2012150952A1 (en) | 2011-05-04 | 2012-11-08 | Forma Tm, Llc | Novel compounds and compositions for the inhibition of nampt |
| MX347459B (es) | 2011-05-09 | 2017-04-26 | Forma Tm Llc | Nuevos compuestos y composiciones para la inhibición de nampt. |
| JP2014518223A (ja) | 2011-06-20 | 2014-07-28 | アルツハイマーズ・インスティテュート・オブ・アメリカ・インコーポレイテッド | 化合物とその治療用途 |
| CA2855510A1 (en) | 2011-11-11 | 2013-05-16 | Abbvie Inc. | Nampt inhibitors |
| WO2013082150A1 (en) | 2011-11-30 | 2013-06-06 | The Curators Of The University Of Missouri | Small molecule inhibitors of nicotinamide phosphoribosyltransferase (nampt) |
| WO2013130935A1 (en) | 2012-03-02 | 2013-09-06 | Genentech, Inc. | Amido-benzyl sulfoxide derivatives |
| JP2015508785A (ja) | 2012-03-02 | 2015-03-23 | ジェネンテック， インコーポレイテッド | ピリジニル及びピリミジニルスルホキシド及びスルホン誘導体 |
| DE102012004054A1 (de) | 2012-03-02 | 2013-09-05 | Volkswagen Ag | Rollfalzkopf, Anlage und Verfahren zum Rollfalzen mit einem Tandemrollensatz |
| WO2013130943A1 (en) | 2012-03-02 | 2013-09-06 | Genentech, Inc. | Alkyl-and di-substituted amido-benzyl sulfonamide derivatives |
| US9790233B2 (en) * | 2012-04-16 | 2017-10-17 | Case Western Reserve University | Compositions and methods of modulating 15-PGDH activity |
| WO2013170191A1 (en) | 2012-05-11 | 2013-11-14 | Genentech, Inc. | Methods of using antagonists of nad biosynthesis from nicotinamide |
| WO2013170115A1 (en) | 2012-05-11 | 2013-11-14 | Abbvie Inc. | Pyridazine and pyridine derivatives as nampt inhibitors |
| HK1208221A1 (en) | 2012-05-11 | 2016-02-26 | Abbvie Inc. | Nampt inhibitors |
| CN104271572A (zh) | 2012-05-11 | 2015-01-07 | 艾伯维公司 | 用作nampt抑制剂的噻唑羧酰胺衍生物 |
| WO2013170113A1 (en) | 2012-05-11 | 2013-11-14 | Abbvie Inc. | Nampt inhibitors |
| MA37808A1 (fr) | 2012-06-27 | 2018-03-30 | Alzheimers Institute Of America Inc | Composés et leurs utilisations thérapeutiques |
| PL3087051T3 (pl) | 2013-12-24 | 2021-02-22 | Oncotartis Inc. | Związki benzamidowe i nikotynamidowe oraz sposoby ich stosowania |
-
2015
- 2015-04-17 EA EA201692091A patent/EA201692091A1/ru unknown
- 2015-04-17 JP JP2016563080A patent/JP6510556B2/ja not_active Expired - Fee Related
- 2015-04-17 WO PCT/US2015/026275 patent/WO2015161142A1/en not_active Ceased
- 2015-04-17 CN CN201580032478.5A patent/CN106458934B/zh not_active Expired - Fee Related
- 2015-04-17 US US15/304,947 patent/US10144742B2/en not_active Expired - Fee Related
- 2015-04-17 TW TW104112475A patent/TW201625578A/zh unknown
- 2015-04-17 CA CA2946130A patent/CA2946130A1/en not_active Abandoned
- 2015-04-17 EP EP15779407.4A patent/EP3131881A4/en not_active Withdrawn
- 2015-04-17 BR BR112016024298A patent/BR112016024298A2/pt not_active Application Discontinuation
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