JP2019518059A5 - - Google Patents
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- Publication number
- JP2019518059A5 JP2019518059A5 JP2018565868A JP2018565868A JP2019518059A5 JP 2019518059 A5 JP2019518059 A5 JP 2019518059A5 JP 2018565868 A JP2018565868 A JP 2018565868A JP 2018565868 A JP2018565868 A JP 2018565868A JP 2019518059 A5 JP2019518059 A5 JP 2019518059A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituents
- het
- hydrogen
- substituted
- 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 149
- 125000001424 substituent group Chemical group 0.000 claims description 44
- 229910052739 hydrogen Inorganic materials 0.000 claims description 38
- 239000001257 hydrogen Substances 0.000 claims description 38
- 150000001875 compounds Chemical class 0.000 claims description 34
- 229910052799 carbon Inorganic materials 0.000 claims description 24
- 125000000623 heterocyclic group Chemical group 0.000 claims description 24
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 22
- 150000002431 hydrogen Chemical class 0.000 claims description 20
- 125000004432 carbon atom Chemical group C* 0.000 claims description 18
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 18
- 229910052717 sulfur Inorganic materials 0.000 claims description 16
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 14
- 125000001153 fluoro group Chemical group F* 0.000 claims description 10
- 125000005843 halogen group Chemical group 0.000 claims description 10
- 125000005842 heteroatom Chemical group 0.000 claims description 10
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 8
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 8
- 229910052760 oxygen Inorganic materials 0.000 claims description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 8
- 125000006273 (C1-C3) alkyl 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
- 206010028980 Neoplasm Diseases 0.000 claims description 4
- 206010052779 Transplant rejections Diseases 0.000 claims description 4
- 201000011510 cancer Diseases 0.000 claims description 4
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- 125000003566 oxetanyl group Chemical group 0.000 claims description 4
- 239000004480 active ingredient Substances 0.000 claims description 3
- 208000023275 Autoimmune disease Diseases 0.000 claims description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 2
- 206010020751 Hypersensitivity Diseases 0.000 claims description 2
- 208000004852 Lung Injury Diseases 0.000 claims description 2
- 208000034486 Multi-organ failure Diseases 0.000 claims description 2
- 208000010718 Multiple Organ Failure Diseases 0.000 claims description 2
- 150000001204 N-oxides Chemical class 0.000 claims description 2
- 206010033645 Pancreatitis Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 206010069363 Traumatic lung injury Diseases 0.000 claims description 2
- 125000003545 alkoxy group Chemical group 0.000 claims description 2
- 208000026935 allergic disease Diseases 0.000 claims description 2
- 230000007815 allergy Effects 0.000 claims description 2
- 208000006673 asthma Diseases 0.000 claims description 2
- 125000004429 atom Chemical group 0.000 claims description 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 208000027866 inflammatory disease Diseases 0.000 claims description 2
- 208000017169 kidney disease Diseases 0.000 claims description 2
- 231100000515 lung injury Toxicity 0.000 claims description 2
- 208000029744 multiple organ dysfunction syndrome Diseases 0.000 claims description 2
- 230000004770 neurodegeneration Effects 0.000 claims description 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 2
- 230000002265 prevention Effects 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- 229920006395 saturated elastomer Polymers 0.000 claims description 2
- 239000012453 solvate Substances 0.000 claims description 2
- 230000019100 sperm motility Effects 0.000 claims description 2
- 208000010110 spontaneous platelet aggregation Diseases 0.000 claims description 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16174712 | 2016-06-16 | ||
| EP16174712.6 | 2016-06-16 | ||
| PCT/EP2017/064672 WO2017216293A1 (en) | 2016-06-16 | 2017-06-15 | Azabenzimidazole derivatives as pi3k beta inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019518059A JP2019518059A (ja) | 2019-06-27 |
| JP2019518059A5 true JP2019518059A5 (https=) | 2020-07-27 |
| JP7158286B2 JP7158286B2 (ja) | 2022-10-21 |
Family
ID=56132833
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018565868A Active JP7158286B2 (ja) | 2016-06-16 | 2017-06-15 | ＰＩ３Ｋβ阻害剤としてのアザベンゾイミダゾール誘導体 |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US20190263804A1 (https=) |
| EP (1) | EP3472147B1 (https=) |
| JP (1) | JP7158286B2 (https=) |
| KR (1) | KR102472198B1 (https=) |
| CN (1) | CN109311843B (https=) |
| AU (1) | AU2017286380B2 (https=) |
| BR (1) | BR112018076169A2 (https=) |
| CA (1) | CA3025746A1 (https=) |
| EA (1) | EA037871B1 (https=) |
| ES (1) | ES2818620T3 (https=) |
| IL (1) | IL263653A (https=) |
| MX (1) | MX375484B (https=) |
| WO (1) | WO2017216293A1 (https=) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK3904350T3 (da) | 2018-04-12 | 2023-11-13 | Bayer Ag | N-(cyclopropylmethyl)-5-(methylsulfonyl)-n-{1-[1-(pyrimidin-2-yl)-1h-1,2,4-triazol-5-yl]ethyl}benzamidderivater og de tilsvarende pyridincarboxamidderivater som pesticider |
| WO2019209811A1 (en) | 2018-04-24 | 2019-10-31 | Bristol-Myers Squibb Company | Macrocyclic toll-like receptor 7 (tlr7) agonists |
| MX2020011275A (es) | 2018-04-25 | 2020-11-13 | Bayer Ag | Novedosos compuestos de heteroaril-triazol y hetroaril[-]tetrazol como plaguicidas. |
| US11554120B2 (en) | 2018-08-03 | 2023-01-17 | Bristol-Myers Squibb Company | 1H-pyrazolo[4,3-d]pyrimidine compounds as toll-like receptor 7 (TLR7) agonists and methods and uses therefor |
| US20220274947A1 (en) | 2019-07-23 | 2022-09-01 | Bayer Aktiengesellschaft | Novel heteroaryl-triazole compounds as pesticides |
| CN110551101B (zh) * | 2019-08-28 | 2020-11-24 | 沈阳药科大学 | 1、6-二取代-苯并五元杂环类衍生物及其用途 |
| TW202128664A (zh) | 2019-10-09 | 2021-08-01 | 德商拜耳廠股份有限公司 | 作為除害劑之新穎雜芳基三唑化合物 |
| JP2023512204A (ja) | 2020-01-27 | 2023-03-24 | ブリストル－マイヤーズ スクイブ カンパニー | トール様受容体７（ＴＬＲ７）アゴニストとしての１Ｈ－ピラゾロ［４，３－ｄ］ピリミジン化合物 |
| US20230131192A1 (en) | 2020-01-27 | 2023-04-27 | Bristol-Myers Squibb Company | 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS |
| US12485123B2 (en) | 2020-01-27 | 2025-12-02 | Bristol-Myers Squibb Company | 1H-pyrazolo[4,3-d]pyrimidine compounds as toll-like receptor 7 (TLR7) agonists |
| KR20220132601A (ko) | 2020-01-27 | 2022-09-30 | 브리스톨-마이어스 스큅 컴퍼니 | 톨-유사 수용체 7 (TLR7) 효능제로서의 1H-피라졸로[4,3-d]피리미딘 화합물 |
| CN115151546A (zh) | 2020-01-27 | 2022-10-04 | 百时美施贵宝公司 | 作为Toll样受体7(TLR7)激动剂的C3-取代的1H-吡唑并[4,3-d]嘧啶化合物 |
| US20230348468A1 (en) | 2020-01-27 | 2023-11-02 | Bristol-Myers Squibb Company | 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS |
| KR20220132589A (ko) | 2020-01-27 | 2022-09-30 | 브리스톨-마이어스 스큅 컴퍼니 | 톨-유사 수용체 7 (TLR7) 효능제로서의 1H-피라졸로[4,3-d]피리미딘 화합물 |
| WO2021154663A1 (en) | 2020-01-27 | 2021-08-05 | Bristol-Myers Squibb Company | 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS |
| US20230144824A1 (en) | 2020-01-27 | 2023-05-11 | Bristol-Myers Squibb Company | 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS |
| US20250382289A1 (en) * | 2022-02-18 | 2025-12-18 | Xizang Haisco Pharmaceutical Co., Ltd. | Pyrazolopyridine derivative and application thereof in medicine |
| WO2024222880A1 (zh) * | 2023-04-27 | 2024-10-31 | 西藏海思科制药有限公司 | 一种吡啶并吡唑衍生物的药物组合物及其在医药上的应用 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5177074A (en) * | 1991-03-26 | 1993-01-05 | Merck & Co., Inc. | Angiotensin ii antagonists incorporating a substituted thiophene or furan |
| EP1993537A4 (en) | 2006-03-02 | 2010-05-19 | Glaxosmithkline Llc | THIAZOLONES AS INHIBITORS OF P13-KINASES |
| WO2008014219A2 (en) | 2006-07-24 | 2008-01-31 | Smithkline Beecham Corporation | Thiozolidinedione derivatives as p13 kinase inhibitors |
| WO2009021083A1 (en) | 2007-08-09 | 2009-02-12 | Smithkline Beecham Corporation | Quinoxaline derivatives as pi3 kinase inhibitors |
| BRPI0817503B8 (pt) * | 2007-10-05 | 2021-05-25 | Sstarbio Pte Ltd | derivados de purina substituídos por pirimidina, composição farmacêutica compreendendo ditos compostos e uso dos mesmos para a prevenção ou tratamento de uma condição proliferativa |
| EP3613743B1 (en) | 2008-01-04 | 2022-03-16 | Intellikine, LLC | Processes for the preparation of 1h-pyrazolo[3,4-d]pyrimidin-4-amine derivatives |
| PE20121148A1 (es) | 2009-08-17 | 2012-09-07 | Intellikine Llc | Compuestos heterociclicos y usos de los mismos |
| KR20120081164A (ko) | 2009-09-29 | 2012-07-18 | 엑스커버리 홀딩 컴퍼니 엘엘씨 | Ｐｉ3ｋ(델타) 선택적 억제제 |
| UY33304A (es) | 2010-04-02 | 2011-10-31 | Amgen Inc | Compuestos heterocíclicos y sus usos |
| JP5719028B2 (ja) | 2010-10-06 | 2015-05-13 | グラクソスミスクライン エルエルシー | Ｐｉ３キナーゼ阻害剤としてのベンズイミダゾール誘導体 |
| WO2012116237A2 (en) | 2011-02-23 | 2012-08-30 | Intellikine, Llc | Heterocyclic compounds and uses thereof |
| WO2013028263A1 (en) * | 2011-08-24 | 2013-02-28 | Glaxosmithkline Llc | Pyrazolopyrimidine derivatives as pi3 kinase inhibitors |
| US8778937B2 (en) | 2011-12-20 | 2014-07-15 | Glaxosmithkline Llc | Benzimidazole boronic acid derivatives as PI3 kinase inhibitors |
| WO2013095761A1 (en) * | 2011-12-20 | 2013-06-27 | Glaxosmithkline Llc | Imidazopyridine derivatives as pi3 kinase inhibitors |
-
2017
- 2017-06-15 WO PCT/EP2017/064672 patent/WO2017216293A1/en not_active Ceased
- 2017-06-15 CN CN201780037153.5A patent/CN109311843B/zh active Active
- 2017-06-15 EP EP17729500.3A patent/EP3472147B1/en active Active
- 2017-06-15 MX MX2018015709A patent/MX375484B/es active IP Right Grant
- 2017-06-15 ES ES17729500T patent/ES2818620T3/es active Active
- 2017-06-15 AU AU2017286380A patent/AU2017286380B2/en not_active Ceased
- 2017-06-15 US US16/310,413 patent/US20190263804A1/en not_active Abandoned
- 2017-06-15 JP JP2018565868A patent/JP7158286B2/ja active Active
- 2017-06-15 EA EA201892734A patent/EA037871B1/ru not_active IP Right Cessation
- 2017-06-15 CA CA3025746A patent/CA3025746A1/en active Pending
- 2017-06-15 KR KR1020187037717A patent/KR102472198B1/ko active Active
- 2017-06-15 BR BR112018076169-9A patent/BR112018076169A2/pt not_active Application Discontinuation
-
2018
- 2018-12-11 IL IL263653A patent/IL263653A/en active IP Right Grant
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