JP2017522339A5 - - Google Patents
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- Publication number
- JP2017522339A5 JP2017522339A5 JP2017504727A JP2017504727A JP2017522339A5 JP 2017522339 A5 JP2017522339 A5 JP 2017522339A5 JP 2017504727 A JP2017504727 A JP 2017504727A JP 2017504727 A JP2017504727 A JP 2017504727A JP 2017522339 A5 JP2017522339 A5 JP 2017522339A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- heteroaryl
- aryl
- heterocyclyl
- 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
- 125000003118 aryl group Chemical group 0.000 claims description 105
- 125000001072 heteroaryl group Chemical group 0.000 claims description 104
- 125000000623 heterocyclic group Chemical group 0.000 claims description 94
- 229910052739 hydrogen Inorganic materials 0.000 claims description 78
- 239000001257 hydrogen Substances 0.000 claims description 76
- 125000000217 alkyl group Chemical group 0.000 claims description 75
- 150000002431 hydrogen Chemical class 0.000 claims description 54
- 229910052736 halogen Inorganic materials 0.000 claims description 50
- 150000002367 halogens Chemical class 0.000 claims description 50
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 43
- 125000001188 haloalkyl group Chemical group 0.000 claims description 40
- 150000001875 compounds Chemical class 0.000 claims description 36
- 125000003545 alkoxy group Chemical group 0.000 claims description 35
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 34
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 28
- 230000037361 pathway Effects 0.000 claims description 28
- 239000000203 mixture Substances 0.000 claims description 24
- 102000004226 Prostaglandin-E Synthases Human genes 0.000 claims description 23
- 108090000748 Prostaglandin-E Synthases Proteins 0.000 claims description 23
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 23
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical class [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 22
- 125000002947 alkylene group Chemical group 0.000 claims description 21
- 102100022364 Polyunsaturated fatty acid 5-lipoxygenase Human genes 0.000 claims description 19
- 150000003839 salts Chemical class 0.000 claims description 19
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 18
- -1 —OR 11 Chemical group 0.000 claims description 18
- 208000027866 inflammatory disease Diseases 0.000 claims description 17
- 208000002193 Pain Diseases 0.000 claims description 14
- 206010028980 Neoplasm Diseases 0.000 claims description 13
- 201000011510 cancer Diseases 0.000 claims description 13
- 108010093579 Arachidonate 5-lipoxygenase Proteins 0.000 claims description 12
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 12
- 201000001320 Atherosclerosis Diseases 0.000 claims description 11
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 11
- 208000006673 asthma Diseases 0.000 claims description 11
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 11
- 201000010099 disease Diseases 0.000 claims description 11
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 11
- 208000024827 Alzheimer disease Diseases 0.000 claims description 10
- 101000620009 Homo sapiens Polyunsaturated fatty acid 5-lipoxygenase Proteins 0.000 claims description 10
- 125000003342 alkenyl group Chemical group 0.000 claims description 10
- 125000000304 alkynyl group Chemical group 0.000 claims description 9
- 208000002874 Acne Vulgaris Diseases 0.000 claims description 8
- 206010020751 Hypersensitivity Diseases 0.000 claims description 8
- 206010000496 acne Diseases 0.000 claims description 8
- 230000007815 allergy Effects 0.000 claims description 8
- 208000023516 stroke disease Diseases 0.000 claims description 8
- 208000035285 Allergic Seasonal Rhinitis Diseases 0.000 claims description 7
- 102000001381 Arachidonate 5-Lipoxygenase Human genes 0.000 claims description 7
- 208000023275 Autoimmune disease Diseases 0.000 claims description 7
- 208000015943 Coeliac disease Diseases 0.000 claims description 7
- 208000011231 Crohn disease Diseases 0.000 claims description 7
- 201000004624 Dermatitis Diseases 0.000 claims description 7
- 206010061218 Inflammation Diseases 0.000 claims description 7
- 206010039085 Rhinitis allergic Diseases 0.000 claims description 7
- 201000010105 allergic rhinitis Diseases 0.000 claims description 7
- 206010003246 arthritis Diseases 0.000 claims description 7
- 229910052799 carbon Inorganic materials 0.000 claims description 7
- 208000015181 infectious disease Diseases 0.000 claims description 7
- 230000004054 inflammatory process Effects 0.000 claims description 7
- 206010025135 lupus erythematosus Diseases 0.000 claims description 7
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims description 6
- 206010065390 Inflammatory pain Diseases 0.000 claims description 6
- 208000026935 allergic disease Diseases 0.000 claims description 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 6
- 125000004122 cyclic group Chemical group 0.000 claims description 6
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 claims description 6
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims description 6
- 208000004296 neuralgia Diseases 0.000 claims description 6
- 208000021722 neuropathic pain Diseases 0.000 claims description 6
- 229920006395 saturated elastomer Polymers 0.000 claims description 6
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 6
- 150000003462 sulfoxides Chemical class 0.000 claims description 6
- 230000002757 inflammatory effect Effects 0.000 claims description 5
- 230000002401 inhibitory effect Effects 0.000 claims description 5
- 101150050490 Alox5 gene Proteins 0.000 claims description 4
- 101710156627 Polyunsaturated fatty acid 5-lipoxygenase Proteins 0.000 claims description 4
- 230000037396 body weight Effects 0.000 claims description 4
- 238000004519 manufacturing process Methods 0.000 claims description 4
- 150000001721 carbon Chemical group 0.000 claims description 3
- MZOFCQQQCNRIBI-VMXHOPILSA-N (3s)-4-[[(2s)-1-[[(2s)-1-[[(1s)-1-carboxy-2-hydroxyethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-[[2-[[(2s)-2,6-diaminohexanoyl]amino]acetyl]amino]-4-oxobutanoic acid Chemical compound OC[C@@H](C(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(O)=O)NC(=O)CNC(=O)[C@@H](N)CCCCN MZOFCQQQCNRIBI-VMXHOPILSA-N 0.000 claims description 2
- 208000023584 Alzheimer disease 10 Diseases 0.000 claims description 2
- 102000004190 Enzymes Human genes 0.000 claims description 2
- 108090000790 Enzymes Proteins 0.000 claims description 2
- 108060008682 Tumor Necrosis Factor Proteins 0.000 claims description 2
- 102000000852 Tumor Necrosis Factor-alpha Human genes 0.000 claims description 2
- 210000004369 blood Anatomy 0.000 claims description 2
- 239000008280 blood Substances 0.000 claims description 2
- 210000004027 cell Anatomy 0.000 claims description 2
- XEYBRNLFEZDVAW-ARSRFYASSA-N dinoprostone Chemical compound CCCCC[C@H](O)\C=C\[C@H]1[C@H](O)CC(=O)[C@@H]1C\C=C/CCCC(O)=O XEYBRNLFEZDVAW-ARSRFYASSA-N 0.000 claims description 2
- 229960002986 dinoprostone Drugs 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 125000005843 halogen group Chemical group 0.000 claims description 2
- 230000005764 inhibitory process Effects 0.000 claims description 2
- VNYSSYRCGWBHLG-AMOLWHMGSA-N leukotriene B4 Chemical compound CCCCC\C=C/C[C@@H](O)\C=C\C=C\C=C/[C@@H](O)CCCC(O)=O VNYSSYRCGWBHLG-AMOLWHMGSA-N 0.000 claims description 2
- XEYBRNLFEZDVAW-UHFFFAOYSA-N prostaglandin E2 Natural products CCCCCC(O)C=CC1C(O)CC(=O)C1CC=CCCCC(O)=O XEYBRNLFEZDVAW-UHFFFAOYSA-N 0.000 claims description 2
- 230000009870 specific binding Effects 0.000 claims description 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 12
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 9
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 7
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 7
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 6
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 3
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 3
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 3
- 125000005865 C2-C10alkynyl group Chemical group 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 1
- 101100240517 Caenorhabditis elegans nhr-11 gene Proteins 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 210000000265 leukocyte Anatomy 0.000 claims 1
- 229940094443 oxytocics prostaglandins Drugs 0.000 claims 1
- 150000003180 prostaglandins Chemical class 0.000 claims 1
- 0 O=C1OC(CN2C*C2)C*1 Chemical compound O=C1OC(CN2C*C2)C*1 0.000 description 9
- 238000000034 method Methods 0.000 description 8
- 208000006929 Alzheimer disease 7 Diseases 0.000 description 1
- UQFQONCQIQEYPJ-UHFFFAOYSA-N C[n]1nccc1 Chemical compound C[n]1nccc1 UQFQONCQIQEYPJ-UHFFFAOYSA-N 0.000 description 1
- 208000006011 Stroke Diseases 0.000 description 1
- 125000005055 alkyl alkoxy group Chemical group 0.000 description 1
- 210000003912 basophilic leucocyte Anatomy 0.000 description 1
- 230000002860 competitive effect Effects 0.000 description 1
- 208000028774 intestinal disease Diseases 0.000 description 1
- 230000007170 pathology Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462031337P | 2014-07-31 | 2014-07-31 | |
| US62/031,337 | 2014-07-31 | ||
| PCT/EP2015/067644 WO2016016421A1 (en) | 2014-07-31 | 2015-07-31 | 2-amino-benzimidazole derivatives and their use as 5-lipoxygenase and/or prostaglandin e synthase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017522339A JP2017522339A (ja) | 2017-08-10 |
| JP2017522339A5 true JP2017522339A5 (https=) | 2018-08-16 |
| JP6785217B2 JP6785217B2 (ja) | 2020-11-18 |
Family
ID=55216797
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017504727A Active JP6785217B2 (ja) | 2014-07-31 | 2015-07-31 | ２−アミノ−ベンゾイミダゾール誘導体ならびにこれらの５−リポキシゲナーゼおよび／またはプロスタグランジンｅシンターゼ阻害剤としての使用 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US11447486B2 (https=) |
| EP (1) | EP3177597B1 (https=) |
| JP (1) | JP6785217B2 (https=) |
| KR (1) | KR102494596B1 (https=) |
| CN (1) | CN106879256B (https=) |
| AU (1) | AU2015295248B2 (https=) |
| BR (1) | BR112017001918A2 (https=) |
| CA (1) | CA2955565A1 (https=) |
| ES (1) | ES2795748T3 (https=) |
| RU (1) | RU2732416C2 (https=) |
| SG (1) | SG11201700439VA (https=) |
| WO (1) | WO2016016421A1 (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6849197B2 (ja) * | 2016-02-12 | 2021-03-24 | ファーマクシス リミテッド | リジルオキシダーゼのインドールおよびアザインドールハロアリルアミン誘導体阻害剤およびその使用 |
| GB201617630D0 (en) | 2016-10-18 | 2016-11-30 | Cellcentric Ltd | Pharmaceutical compounds |
| CN107141282B (zh) * | 2017-03-29 | 2019-11-05 | 重庆文理学院 | 一种苯并咪唑杂氮环丁酮衍生物及其在抗肿瘤药物中的应用 |
| HRP20250272T1 (hr) | 2017-10-19 | 2025-04-25 | Teijin Pharma Limited | Derivati benzimidazola i njihova uporaba |
| GB201806320D0 (en) | 2018-04-18 | 2018-05-30 | Cellcentric Ltd | Process |
| JP2021534215A (ja) * | 2018-08-24 | 2021-12-09 | ゼニオプロ ゲーエムベーハー | 病的症状の治療における使用のための芳香族分子 |
| EP3939975A4 (en) * | 2019-03-15 | 2022-11-30 | Nippon Soda Co., Ltd. | HETEROCYCLIC COMPOUND AND AGRICULTURAL OR HORTICULTURAL BACTERICIDE |
| EP4081199A4 (en) * | 2019-12-23 | 2024-01-17 | SRI International | LIPOXYGENASE INHIBITORS |
| CN115667224A (zh) * | 2020-02-26 | 2023-01-31 | 斯克里普斯研究学院 | 具有抗炎活性的scl15a4小分子的抑制剂 |
| KR20240035820A (ko) | 2021-07-09 | 2024-03-18 | 플렉시움 인코포레이티드 | Ikzf2를 조절하는 아릴 화합물 및 약학 조성물 |
| WO2023107705A1 (en) | 2021-12-10 | 2023-06-15 | Incyte Corporation | Bicyclic amines as cdk12 inhibitors |
Family Cites Families (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4002623A (en) * | 1974-08-07 | 1977-01-11 | Pfizer Inc. | Anti-inflammatory 1-[3-(dialkylamino)propyl]-2-acylaminobenzimidazoles and 2-acylamino-3-[3-(dialkylamino)-propyl]imidazo[4,5-b]pyridines |
| DE2730720C2 (de) * | 1977-07-07 | 1979-07-12 | Basf Ag, 6700 Ludwigshafen | Verfahren zur Herstellung von praktisch reinem l-Amino-8-nitro-43dihydroxy-anthrachinon |
| US4835161A (en) * | 1986-02-03 | 1989-05-30 | Janssen Pharmaceutica N.V. | Anti-histaminic compositions containing n-heterocyclyl-4-piperidinamines |
| JPH06759B2 (ja) * | 1989-09-22 | 1994-01-05 | ファイザー製薬株式会社 | 新規なベンゾイミダゾール化合物 |
| GB9825652D0 (en) * | 1998-11-23 | 1999-01-13 | Celltech Therapeutics Ltd | Chemical compounds |
| PA8535601A1 (es) * | 2000-12-21 | 2002-11-28 | Pfizer | Derivados benzimidazol y piridilimidazol como ligandos para gabaa |
| EP1429765A2 (en) * | 2001-09-14 | 2004-06-23 | Methylgene, Inc. | Inhibitors of histone deacetylase |
| ES2367422T3 (es) * | 2001-10-09 | 2011-11-03 | Amgen Inc. | Derivados de imidazol como agentes antiinflamatorios. |
| AU2003220970A1 (en) * | 2002-03-01 | 2003-09-16 | Smithkline Beecham Corporation | Diamino-pyrimidines and their use as angiogenesis inhibitors |
| EP1388341A1 (en) * | 2002-08-07 | 2004-02-11 | Aventis Pharma Deutschland GmbH | Acylamino-substituted heteroaromatic compounds and their use as pharmaceuticals |
| US20040117213A1 (en) * | 2002-11-27 | 2004-06-17 | Pache Eugene P. | System and method for selective and detailed delivery of information over a network |
| US7531553B2 (en) * | 2003-03-21 | 2009-05-12 | Amgen Inc. | Heterocyclic compounds and methods of use |
| US20060194871A1 (en) | 2003-04-11 | 2006-08-31 | Barvian Kevin K | Heterocyclic mchr1 antagoists |
| DE10349587A1 (de) * | 2003-10-24 | 2005-05-25 | Merck Patent Gmbh | Benzimidazolylderivate |
| US7470712B2 (en) | 2004-01-21 | 2008-12-30 | Bristol-Myers Squibb Company | Amino-benzazoles as P2Y1 receptor inhibitors |
| WO2005079791A1 (en) * | 2004-02-12 | 2005-09-01 | Boehringer Ingelheim Pharmaceuticals, Inc. | Thiophene -2- carboxylic acid - (1h - benzimidazol - 2 yl) - amide derivatives and related compounds as inhibitors of the tec kinase itk (interleukin -2- inducible t cell kinase) for the treatment of inflammation, immunological and allergic disorders |
| AU2005225471B2 (en) | 2004-03-26 | 2011-05-12 | Methylgene Inc. | Inhibitors of histone deacetylase |
| CN101489553A (zh) | 2006-07-03 | 2009-07-22 | 神经研究公司 | 单胺再摄取抑制剂和钾通道激活剂的组合 |
| JP2009542604A (ja) | 2006-07-06 | 2009-12-03 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ４−ヘテロシクロアルキルピリミジン、それらの調製方法及び医薬としての使用 |
| EP2471507B1 (en) | 2006-09-29 | 2017-03-01 | Johnson & Johnson Vision Care, Inc. | Ophthalmic devices used in the treatment of ocular allergies |
| AR074343A1 (es) | 2008-11-14 | 2011-01-12 | Amgen Inc | Derivados de piridina y pirimidina como inhibidores de la fosfodiesterasa 10 |
| CN101955483A (zh) | 2009-07-13 | 2011-01-26 | 上海药明康德新药开发有限公司 | 2-取代[1,2,4]三唑[1,5-a]苯并咪唑的合成方法 |
| CA2798325A1 (en) * | 2010-05-13 | 2011-11-17 | Amgen Inc. | Heteroaryloxyheterocyclyl compounds as pde10 inhibitors |
| US8546344B2 (en) * | 2010-10-28 | 2013-10-01 | Viropharma Incorporated | Crystalline phases of 5,6-dichloro-2-(isopropylamino)-1-β-L-ribofuranosyl)-1H-benzimidazole |
| US8466186B2 (en) * | 2010-12-10 | 2013-06-18 | Boehringer Ingelheim International Gmbh | Compounds |
| CN103044337A (zh) | 2011-10-13 | 2013-04-17 | 南京理工大学 | 2-(n-烷基)氨基咪唑衍生物的合成方法 |
| US10292390B2 (en) * | 2011-11-04 | 2019-05-21 | Wisconsin Alumni Research Foundation | Inhibition and dispersion of bacterial biofilms with 2-aminobenzimidazole derivatives |
| CN103121969A (zh) | 2012-12-04 | 2013-05-29 | 中国科学院昆明植物研究所 | 苯并咪唑及其衍生物，其药物组合物及其应用 |
| CN103450093A (zh) * | 2013-09-06 | 2013-12-18 | 中国药科大学 | 2-苄氨基苯并咪唑类化合物及其用途 |
-
2015
- 2015-07-31 JP JP2017504727A patent/JP6785217B2/ja active Active
- 2015-07-31 SG SG11201700439VA patent/SG11201700439VA/en unknown
- 2015-07-31 CA CA2955565A patent/CA2955565A1/en not_active Abandoned
- 2015-07-31 BR BR112017001918A patent/BR112017001918A2/pt not_active Application Discontinuation
- 2015-07-31 ES ES15748009T patent/ES2795748T3/es active Active
- 2015-07-31 CN CN201580053161.XA patent/CN106879256B/zh active Active
- 2015-07-31 WO PCT/EP2015/067644 patent/WO2016016421A1/en not_active Ceased
- 2015-07-31 US US15/327,560 patent/US11447486B2/en active Active
- 2015-07-31 RU RU2017103148A patent/RU2732416C2/ru active
- 2015-07-31 AU AU2015295248A patent/AU2015295248B2/en active Active
- 2015-07-31 EP EP15748009.6A patent/EP3177597B1/en active Active
- 2015-07-31 KR KR1020177005644A patent/KR102494596B1/ko active Active
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