JP2018507230A5 - - Google Patents
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- Publication number
- JP2018507230A5 JP2018507230A5 JP2017546121A JP2017546121A JP2018507230A5 JP 2018507230 A5 JP2018507230 A5 JP 2018507230A5 JP 2017546121 A JP2017546121 A JP 2017546121A JP 2017546121 A JP2017546121 A JP 2017546121A JP 2018507230 A5 JP2018507230 A5 JP 2018507230A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- optionally substituted
- heteroalkyl
- acyl
- heteroacyl
- 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
- 125000000217 alkyl group Chemical group 0.000 claims description 207
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 190
- 125000005843 halogen group Chemical group 0.000 claims description 184
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 179
- 125000003118 aryl group Chemical group 0.000 claims description 177
- 125000002252 acyl group Chemical group 0.000 claims description 169
- 125000001072 heteroaryl group Chemical group 0.000 claims description 165
- 229910052760 oxygen Inorganic materials 0.000 claims description 142
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 133
- 229910052717 sulfur Inorganic materials 0.000 claims description 120
- 125000001424 substituent group Chemical group 0.000 claims description 85
- 229910052799 carbon Inorganic materials 0.000 claims description 81
- 229910052739 hydrogen Inorganic materials 0.000 claims description 80
- 125000005842 heteroatom Chemical group 0.000 claims description 76
- 229910052736 halogen Inorganic materials 0.000 claims description 74
- -1 hydroxy, amino Chemical group 0.000 claims description 66
- 150000001875 compounds Chemical class 0.000 claims description 65
- 125000003342 alkenyl group Chemical group 0.000 claims description 59
- 150000002367 halogens Chemical class 0.000 claims description 54
- 125000004429 atom Chemical group 0.000 claims description 46
- 125000000304 alkynyl group Chemical group 0.000 claims description 44
- 150000003839 salts Chemical class 0.000 claims description 41
- 125000000623 heterocyclic group Chemical group 0.000 claims description 39
- 125000004450 alkenylene group Chemical group 0.000 claims description 27
- 125000004474 heteroalkylene group Chemical group 0.000 claims description 27
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 27
- 125000005647 linker group Chemical group 0.000 claims description 27
- 125000001960 7 membered carbocyclic group Chemical group 0.000 claims description 14
- 229910052721 tungsten Inorganic materials 0.000 claims description 14
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 12
- 125000004430 oxygen atom Chemical group O* 0.000 claims description 12
- 125000004434 sulfur atom Chemical group 0.000 claims description 12
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 9
- 125000004122 cyclic group Chemical group 0.000 claims description 9
- 229910052757 nitrogen Inorganic materials 0.000 claims description 6
- 206010028980 Neoplasm Diseases 0.000 claims description 4
- 201000011510 cancer Diseases 0.000 claims description 4
- 210000004185 liver Anatomy 0.000 claims description 4
- 210000004369 blood Anatomy 0.000 claims description 2
- 239000008280 blood Substances 0.000 claims description 2
- 210000004556 brain Anatomy 0.000 claims description 2
- 210000001072 colon Anatomy 0.000 claims description 2
- 210000003128 head Anatomy 0.000 claims description 2
- 210000002216 heart Anatomy 0.000 claims description 2
- 239000001257 hydrogen Substances 0.000 claims description 2
- 210000003734 kidney Anatomy 0.000 claims description 2
- 210000004072 lung Anatomy 0.000 claims description 2
- 210000001165 lymph node Anatomy 0.000 claims description 2
- 210000003739 neck Anatomy 0.000 claims description 2
- 210000000496 pancreas Anatomy 0.000 claims description 2
- 210000002307 prostate Anatomy 0.000 claims description 2
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 45
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims 37
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 36
- 125000006832 (C1-C10) alkylene group Chemical group 0.000 claims 13
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 9
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 7
- 150000001732 carboxylic acid derivatives Chemical group 0.000 claims 4
- 125000002837 carbocyclic group Chemical group 0.000 claims 3
- 241000257303 Hymenoptera Species 0.000 claims 2
- 125000005549 heteroarylene group Chemical group 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 1
- 150000002148 esters Chemical class 0.000 description 24
- 229940002612 prodrug Drugs 0.000 description 20
- 239000000651 prodrug Substances 0.000 description 20
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 17
- 125000002947 alkylene group Chemical group 0.000 description 14
- 150000001408 amides Chemical class 0.000 description 4
- 125000002843 carboxylic acid group Chemical group 0.000 description 4
- 238000000034 method Methods 0.000 description 3
- 101150046160 POL1 gene Proteins 0.000 description 2
- 101100117436 Thermus aquaticus polA gene Proteins 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 238000013518 transcription Methods 0.000 description 2
- 230000035897 transcription Effects 0.000 description 2
- 206010006187 Breast cancer Diseases 0.000 description 1
- 208000026310 Breast neoplasm Diseases 0.000 description 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 230000028706 ribosome biogenesis Effects 0.000 description 1
- 210000003491 skin Anatomy 0.000 description 1
- 239000012453 solvate Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562128208P | 2015-03-04 | 2015-03-04 | |
| US62/128,208 | 2015-03-04 | ||
| PCT/US2016/020418 WO2016141042A2 (en) | 2015-03-04 | 2016-03-02 | Novel compositions, uses and methods for making them |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021014802A Division JP2021066741A (ja) | 2015-03-04 | 2021-02-02 | 新規な組成物、使用およびそれを作製するための方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018507230A JP2018507230A (ja) | 2018-03-15 |
| JP2018507230A5 true JP2018507230A5 (OSRAM) | 2019-04-11 |
| JP6878288B2 JP6878288B2 (ja) | 2021-05-26 |
Family
ID=56848519
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017546121A Active JP6878288B2 (ja) | 2015-03-04 | 2016-03-02 | 新規な組成物、使用およびそれを作製するための方法 |
| JP2021014802A Pending JP2021066741A (ja) | 2015-03-04 | 2021-02-02 | 新規な組成物、使用およびそれを作製するための方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021014802A Pending JP2021066741A (ja) | 2015-03-04 | 2021-02-02 | 新規な組成物、使用およびそれを作製するための方法 |
Country Status (7)
| Country | Link |
|---|---|
| US (9) | US9758518B2 (OSRAM) |
| EP (1) | EP3300501A4 (OSRAM) |
| JP (2) | JP6878288B2 (OSRAM) |
| CN (1) | CN107567448B (OSRAM) |
| CA (1) | CA2978571C (OSRAM) |
| MX (1) | MX2017011116A (OSRAM) |
| WO (1) | WO2016141042A2 (OSRAM) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9758518B2 (en) | 2015-03-04 | 2017-09-12 | Pimera, Inc. | Compositions, uses and methods for making them |
| CN106588920B (zh) * | 2016-12-27 | 2018-10-30 | 云南大学 | 1,3-二氮杂环并[1,2-a]喹啉类化合物及其制备方法和抗肿瘤应用 |
| CN110709400A (zh) * | 2017-03-28 | 2020-01-17 | 皮梅拉股份有限公司 | Pol1抑制剂的新型晶体形式 |
| US20220098210A1 (en) * | 2019-01-29 | 2022-03-31 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Quindoline compounds and uses thereof |
| US10947253B2 (en) | 2019-08-05 | 2021-03-16 | Ankh Life Sciences Limited | Fused polycyclic dimers |
| US12129265B2 (en) | 2020-07-21 | 2024-10-29 | Ankh Life Sciences Limited | Therapeutic agents and uses thereof |
| US12173005B1 (en) | 2023-12-21 | 2024-12-24 | King Faisal University | Pyrimido[1′,6′:1,5]pyrazolo[4,3-b][1,7]naphthyridine compounds as CK2 inhibitors |
Family Cites Families (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US1042801A (en) | 1909-10-28 | 1912-10-29 | Isidor Kitsee | Protecting kinematographic films. |
| NL7709746A (nl) | 1976-09-09 | 1978-03-13 | Hoechst Ag | Werkwijze ter bereiding van benzimidazo-(1,2-a)-chi- nolinen. |
| DE2929414A1 (de) | 1979-07-20 | 1981-02-05 | Hoechst Ag | Pyrimido- eckige klammer auf 5',4' zu 5,6 eckige klammer zu -pyrido- eckige klammer auf 1,2-a eckige klammer zu -benzimidazole, verfahren zu ihrer herstellung und deren verwendung |
| DE3502689A1 (de) | 1985-01-26 | 1986-07-31 | Hoechst Ag, 6230 Frankfurt | Elektrophotographisches aufzeichnungsmaterial |
| DE19509043A1 (de) | 1995-03-03 | 1996-09-05 | Bayer Ag | Cyanierung von Doppelbindungssystemen |
| US5624677A (en) | 1995-06-13 | 1997-04-29 | Pentech Pharmaceuticals, Inc. | Controlled release of drugs delivered by sublingual or buccal administration |
| HUP0302925A3 (en) * | 2000-10-03 | 2004-10-28 | Bristol Myers Squibb Co | Amino-substituted tetracyclic compouds useful as anti-inflammatory agents and pharmaceutical compositions comprising same |
| US7354916B2 (en) | 2003-04-07 | 2008-04-08 | Cylene Pharmaceuticals | Substituted quinobenzoxazine analogs |
| WO2004091504A2 (en) | 2003-04-07 | 2004-10-28 | Cylene Pharmaceuticals, Inc. | Substituted quinobenzoxazine analogs |
| US7507727B2 (en) | 2003-04-07 | 2009-03-24 | Cylene Pharmaceuticals, Inc. | Substituted quinobenzoxazine analogs and methods of using thereof |
| US7652134B2 (en) | 2004-09-17 | 2010-01-26 | Cylene Pharmaceuticals, Inc. | Methods for converting quinolone esters into quinolone amides |
| EP1802306A2 (en) | 2004-09-17 | 2007-07-04 | Cylene Pharmaceuticals, Inc. | Quinolone analog as cell proliferation inhibitors |
| EP1874731A4 (en) | 2005-04-15 | 2009-08-05 | Cylene Pharmaceuticals Inc | CHINOBENZOXAZINANALOGA AND METHOD FOR THE APPLICATION |
| WO2007019295A1 (en) | 2005-08-05 | 2007-02-15 | Cylene Pharmaceuticals, Inc. | Methods of preparing quinolone analogs |
| WO2007038215A1 (en) | 2005-09-22 | 2007-04-05 | Incyte Corporation | Tetracyclic inhibitors of janus kinases |
| US8142909B2 (en) | 2006-02-10 | 2012-03-27 | Universal Display Corporation | Blue phosphorescent imidazophenanthridine materials |
| JP2009535393A (ja) | 2006-05-01 | 2009-10-01 | ファイザー・プロダクツ・インク | 置換２−アミノ縮合複素環式化合物 |
| WO2008060693A2 (en) | 2006-05-17 | 2008-05-22 | Cylene Pharmaceuticals, Inc. | Tetracyclic imidazole analogs |
| CA2701630C (en) | 2007-10-05 | 2016-10-25 | Cylene Pharmaceuticals, Inc. | Quinolone analogs and methods related thereto |
| ATE542813T1 (de) | 2008-08-06 | 2012-02-15 | Pfizer | 6-substituierte 2- heterocyclylaminopyrazinverbindungen als chk-1- inhibitoren |
| US8368062B2 (en) | 2008-11-03 | 2013-02-05 | Lg Chem, Ltd. | Nitrogen-containing heterocyclic compound and organic electronic device using the same |
| US8124770B2 (en) | 2009-04-01 | 2012-02-28 | Beatriz Zayas | Fluorescent cellular markers |
| CN101781312B (zh) | 2009-12-30 | 2012-09-26 | 中国科学院广州生物医药与健康研究院 | 一种吲哚衍生物的合成方法 |
| WO2011156698A2 (en) | 2010-06-11 | 2011-12-15 | Abbott Laboratories | NOVEL PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS |
| KR101567610B1 (ko) | 2010-11-04 | 2015-11-09 | 주식회사 엘지화학 | 신규한 질소 함유 헤테로환 화합물 및 이를 이용한 유기 전자 소자 |
| BR112014008727A2 (pt) | 2011-10-21 | 2017-04-25 | Glaxosmithkline Llc | composto, composição farmacêutica, uso do composto ou sal, métodos para o tratamento de e/ou a prevenção de uma doença ou condição, para a intensificação da resposta imune em um indivíduo, e para regular por regulação positiva uma resposta imune a jak/stat em um indivíduo |
| KR101561730B1 (ko) | 2012-02-06 | 2015-10-22 | 주식회사 엘지화학 | 질소원소를 함유한 헤테로고리 유도체 및 이를 이용한 유기 전자 소자 |
| EP3074391B1 (en) | 2013-11-28 | 2019-07-31 | Tel Hashomer Medical Research Infrastructure And Services Ltd. | Rna polymerase i inhibitors and uses thereof |
| CN106459068B (zh) | 2014-05-09 | 2019-01-22 | 皮梅拉股份有限公司 | 新组合物、用途和制备它们的方法 |
| US9758518B2 (en) | 2015-03-04 | 2017-09-12 | Pimera, Inc. | Compositions, uses and methods for making them |
| CN106349244B (zh) | 2015-07-13 | 2018-07-27 | 首都医科大学 | 苯并咪唑并喹唑啉二甲氧苯氧乙酰-AA-OBzl，其合成，活性和应用 |
| CN119185322A (zh) | 2015-11-20 | 2024-12-27 | 生华生物科技股份有限公司 | 用于治疗癌症的四环喹诺酮类似物组合疗法 |
| CN110709400A (zh) | 2017-03-28 | 2020-01-17 | 皮梅拉股份有限公司 | Pol1抑制剂的新型晶体形式 |
-
2015
- 2015-11-06 US US14/935,155 patent/US9758518B2/en active Active
-
2016
- 2016-03-02 CN CN201680022357.7A patent/CN107567448B/zh active Active
- 2016-03-02 MX MX2017011116A patent/MX2017011116A/es unknown
- 2016-03-02 CA CA2978571A patent/CA2978571C/en active Active
- 2016-03-02 WO PCT/US2016/020418 patent/WO2016141042A2/en not_active Ceased
- 2016-03-02 JP JP2017546121A patent/JP6878288B2/ja active Active
- 2016-03-02 EP EP16759401.9A patent/EP3300501A4/en not_active Withdrawn
- 2016-03-02 US US15/555,024 patent/US10975076B2/en active Active
-
2017
- 2017-04-11 US US15/485,106 patent/US9951066B2/en active Active
- 2017-07-27 US US15/661,770 patent/US10590134B2/en active Active
-
2018
- 2018-01-08 US US15/864,965 patent/US10442801B2/en active Active
-
2019
- 2019-06-03 US US16/430,129 patent/US10745403B2/en active Active
-
2020
- 2020-01-10 US US16/739,354 patent/US11618752B2/en active Active
- 2020-07-09 US US16/925,220 patent/US11623928B2/en active Active
-
2021
- 2021-02-02 JP JP2021014802A patent/JP2021066741A/ja active Pending
- 2021-03-17 US US17/204,459 patent/US11866438B2/en active Active
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