JP2021500332A5 - - Google Patents
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- Publication number
- JP2021500332A5 JP2021500332A5 JP2020521577A JP2020521577A JP2021500332A5 JP 2021500332 A5 JP2021500332 A5 JP 2021500332A5 JP 2020521577 A JP2020521577 A JP 2020521577A JP 2020521577 A JP2020521577 A JP 2020521577A JP 2021500332 A5 JP2021500332 A5 JP 2021500332A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- hydrogen
- alkoxy
- halogen
- ring
- 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
- 229910052739 hydrogen Inorganic materials 0.000 claims 101
- 239000001257 hydrogen Substances 0.000 claims 96
- 229910052736 halogen Inorganic materials 0.000 claims 74
- 150000002367 halogens Chemical class 0.000 claims 74
- 125000005843 halogen group Chemical group 0.000 claims 65
- 150000002431 hydrogen Chemical class 0.000 claims 58
- 125000005842 heteroatom Chemical group 0.000 claims 51
- 125000004093 cyano group Chemical group *C#N 0.000 claims 47
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 39
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 38
- 229910052760 oxygen Inorganic materials 0.000 claims 35
- 150000001875 compounds Chemical class 0.000 claims 30
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 23
- 125000000623 heterocyclic group Chemical group 0.000 claims 21
- 229910052757 nitrogen Inorganic materials 0.000 claims 20
- 125000001424 substituent group Chemical group 0.000 claims 20
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 19
- 125000001072 heteroaryl group Chemical group 0.000 claims 17
- 229910052717 sulfur Inorganic materials 0.000 claims 15
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 14
- 125000000753 cycloalkyl group Chemical group 0.000 claims 14
- -1 C 1- C 6 alkyl Chemical class 0.000 claims 13
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 13
- 125000000217 alkyl group Chemical group 0.000 claims 13
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 13
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 13
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 11
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 9
- 239000011593 sulfur Substances 0.000 claims 9
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 8
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 8
- 229910052799 carbon Inorganic materials 0.000 claims 7
- 125000002619 bicyclic group Chemical group 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 5
- 125000004429 atom Chemical group 0.000 claims 5
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 5
- 125000004043 oxo group Chemical group O=* 0.000 claims 5
- 229920006395 saturated elastomer Polymers 0.000 claims 5
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 4
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 4
- 206010051920 Glomerulonephropathy Diseases 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 229910052731 fluorine Inorganic materials 0.000 claims 4
- 239000011737 fluorine Substances 0.000 claims 4
- 150000003951 lactams Chemical class 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 208000034656 Contusions Diseases 0.000 claims 3
- 102000003623 TRPC6 Human genes 0.000 claims 3
- 108050001421 Transient receptor potential channel, canonical 6 Proteins 0.000 claims 3
- 208000034526 bruise Diseases 0.000 claims 3
- 125000002950 monocyclic group Chemical group 0.000 claims 3
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- CZSRBTBSPLWAAW-UHFFFAOYSA-N 1-[7-fluoro-6-methoxy-1-[[2-(trifluoromethyl)phenyl]methyl]benzimidazol-2-yl]piperidin-3-amine Chemical compound C=1C=CC=C(C(F)(F)F)C=1CN1C2=C(F)C(OC)=CC=C2N=C1N1CCCC(N)C1 CZSRBTBSPLWAAW-UHFFFAOYSA-N 0.000 claims 2
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 2
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 2
- 208000009304 Acute Kidney Injury Diseases 0.000 claims 2
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 2
- 206010018372 Glomerulonephritis membranous Diseases 0.000 claims 2
- 206010019280 Heart failures Diseases 0.000 claims 2
- 208000019693 Lung disease Diseases 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 206010029164 Nephrotic syndrome Diseases 0.000 claims 2
- 208000033626 Renal failure acute Diseases 0.000 claims 2
- 206010040047 Sepsis Diseases 0.000 claims 2
- 208000006011 Stroke Diseases 0.000 claims 2
- 230000001154 acute effect Effects 0.000 claims 2
- 201000011040 acute kidney failure Diseases 0.000 claims 2
- 208000012998 acute renal failure Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 208000033679 diabetic kidney disease Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 201000008350 membranous glomerulonephritis Diseases 0.000 claims 2
- 231100000855 membranous nephropathy Toxicity 0.000 claims 2
- 201000006938 muscular dystrophy Diseases 0.000 claims 2
- 201000008171 proliferative glomerulonephritis Diseases 0.000 claims 2
- 208000002815 pulmonary hypertension Diseases 0.000 claims 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000001960 7 membered carbocyclic group Chemical group 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 208000010159 IgA glomerulonephritis Diseases 0.000 claims 1
- 206010021263 IgA nephropathy Diseases 0.000 claims 1
- 206010061481 Renal injury Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 208000020832 chronic kidney disease Diseases 0.000 claims 1
- 208000022831 chronic renal failure syndrome Diseases 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 208000037806 kidney injury Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 1
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 1
- 230000001105 regulatory effect Effects 0.000 claims 1
- 125000006413 ring segment Chemical group 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762574465P | 2017-10-19 | 2017-10-19 | |
| US62/574,465 | 2017-10-19 | ||
| US201862671090P | 2018-05-14 | 2018-05-14 | |
| US62/671,090 | 2018-05-14 | ||
| PCT/US2018/056484 WO2019079578A1 (en) | 2017-10-19 | 2018-10-18 | BENZIMIDAZOLE DERIVATIVES AND USES THEREOF |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021500332A JP2021500332A (ja) | 2021-01-07 |
| JP2021500332A5 true JP2021500332A5 (enExample) | 2021-10-28 |
| JP7450534B2 JP7450534B2 (ja) | 2024-03-15 |
Family
ID=66173507
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020521577A Active JP7450534B2 (ja) | 2017-10-19 | 2018-10-18 | ベンズイミダゾール誘導体及びその用途 |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US11332459B2 (enExample) |
| EP (1) | EP3697410B1 (enExample) |
| JP (1) | JP7450534B2 (enExample) |
| KR (1) | KR102697255B1 (enExample) |
| CN (1) | CN111417394B (enExample) |
| AU (1) | AU2018351059B2 (enExample) |
| CA (1) | CA3079081A1 (enExample) |
| CL (1) | CL2020001020A1 (enExample) |
| CO (1) | CO2020004669A2 (enExample) |
| ES (1) | ES3004333T3 (enExample) |
| HR (1) | HRP20250272T1 (enExample) |
| HU (1) | HUE070649T2 (enExample) |
| IL (1) | IL273839B (enExample) |
| MA (1) | MA50413A (enExample) |
| MX (1) | MX2020003993A (enExample) |
| NZ (1) | NZ763311A (enExample) |
| PH (1) | PH12020550265A1 (enExample) |
| PL (1) | PL3697410T3 (enExample) |
| SA (1) | SA520411787B1 (enExample) |
| SG (1) | SG11202003502VA (enExample) |
| TW (1) | TWI816704B (enExample) |
| UY (1) | UY37941A (enExample) |
| WO (1) | WO2019079578A1 (enExample) |
| ZA (1) | ZA202002762B (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102551319B1 (ko) | 2018-05-14 | 2023-07-05 | 길리애드 사이언시즈, 인코포레이티드 | Mcl-1 억제제 |
| WO2020210597A1 (en) * | 2019-04-11 | 2020-10-15 | Amgen Inc. | Benzimidazole derivatives and their uses |
| TWI778443B (zh) | 2019-11-12 | 2022-09-21 | 美商基利科學股份有限公司 | Mcl1抑制劑 |
| AU2020391106B2 (en) | 2019-11-26 | 2024-03-21 | Gilead Sciences, Inc. | Processes and intermediates for preparing MCL1 inhibitors |
| EP4135696A1 (en) * | 2020-04-16 | 2023-02-22 | Boehringer Ingelheim International GmbH | Inhibitors of trpc6 for treating respiratory conditions |
| AR121846A1 (es) | 2020-04-16 | 2022-07-13 | Teijin Pharma Ltd | Derivado de arilo o heteroarilo |
| WO2022108984A1 (en) | 2020-11-19 | 2022-05-27 | Gilead Sciences, Inc. | Processes and intermediates for preparing macrocyclic mcl1 inhibitors |
| WO2023276828A1 (ja) * | 2021-06-29 | 2023-01-05 | 国立大学法人大阪大学 | 腎障害の予防および／または治療用医薬組成物、並びにオートファジー活性化剤 |
Family Cites Families (46)
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| FR2618435B1 (fr) | 1987-07-23 | 1989-10-27 | Synthelabo | Derives de benzimidazole, leur preparation et leur application en therapeutique |
| US5670501A (en) | 1994-09-01 | 1997-09-23 | Discovery Therapeutics, Inc. | N-substituted 9-alkyladenines |
| JP4101053B2 (ja) | 2000-08-10 | 2008-06-11 | 田辺三菱製薬株式会社 | プロリン誘導体及びその医薬用途 |
| EA006507B1 (ru) | 2001-10-15 | 2005-12-29 | Янссен Фармацевтика Н.В. | Новые замещенные 4-фенил-4-[1h-имидазол-2-ил] пиперидиновые производные и их применение в качестве селективных непептидных агонистов дельта-опиоидов |
| BR0213325A (pt) | 2001-10-15 | 2004-10-13 | Janssen Pharmaceutica Nv | Derivados de 4-fenil-4-[1h-imidazol-2-il]-piperidina substituìda para a redução de dano isquêmico |
| JP4595542B2 (ja) | 2002-07-30 | 2010-12-08 | 萬有製薬株式会社 | ベンズイミダゾール誘導体を有効成分とするメラニン凝集ホルモン受容体拮抗剤 |
| PL377215A1 (pl) | 2002-10-17 | 2006-01-23 | Amgen Inc. | Pochodne benzimidazolu oraz ich zastosowanie w charakterze ligandów receptora waniloidowego |
| US20070105890A1 (en) | 2003-11-26 | 2007-05-10 | Dainippon Sumitomo Pharma Co., Ltd | Novel condensed imidazole derivative |
| DE102004017932A1 (de) | 2004-04-14 | 2005-11-03 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel |
| WO2006010283A1 (en) | 2004-07-28 | 2006-02-02 | Universität Zürich | Prevention and treatment of thrombus formation |
| US20100267717A1 (en) | 2005-07-29 | 2010-10-21 | 4Sc Ag | Novel Heterocyclic NF-kB Inhibitors |
| US7601745B2 (en) | 2004-09-27 | 2009-10-13 | 4Sc Ag | Heterocyclic NF-kB inhibitors |
| DE102005012875B4 (de) | 2005-03-19 | 2006-11-16 | Sanofi-Aventis Deutschland Gmbh | Verwendung von Amino substituierten 8-N-Benzimidazolen |
| DE102005012874A1 (de) | 2005-03-19 | 2006-09-21 | Sanofi-Aventis Deutschland Gmbh | Amid substituierte 8-N-Benzimidazole, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| US7632454B2 (en) * | 2005-04-06 | 2009-12-15 | North Carolina State University | Dense, shaped articles constructed of a refractory material and methods of preparing such articles |
| EP1739078A1 (de) | 2005-05-30 | 2007-01-03 | Jerini AG | C5a-Rezeptor-Antagonisten |
| CN101365476A (zh) | 2005-10-07 | 2009-02-11 | 瓦拉塔药品公司 | Dpp-iv抑制剂和胃泌素化合物的联合使用 |
| JP2009541454A (ja) | 2006-07-03 | 2009-11-26 | ノイロサーチ アクティーゼルスカブ | モノアミン再摂取阻害剤及びカリウムチャネル活性剤の併用 |
| CN101528729A (zh) | 2006-08-23 | 2009-09-09 | 辉瑞产品公司 | 作为gsk-3抑制剂的嘧啶酮化合物 |
| US20080186971A1 (en) | 2007-02-02 | 2008-08-07 | Tarari, Inc. | Systems and methods for processing access control lists (acls) in network switches using regular expression matching logic |
| WO2008100977A2 (en) | 2007-02-14 | 2008-08-21 | N.V. Organon | Carbamates therapeutic release agents as amidase inhibitors |
| WO2008153701A1 (en) | 2007-05-24 | 2008-12-18 | Schering Corporation | Compounds for inhibiting ksp kinesin activity |
| CN101835749A (zh) | 2007-07-30 | 2010-09-15 | 奥斯拜客斯制药有限公司 | 取代的吲哚 |
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| KR20100101055A (ko) | 2009-03-07 | 2010-09-16 | 주식회사 메디젠텍 | 세포핵에서 세포질로의 ｇｓｋ３의 이동을 억제하는 화합물을 함유하는 세포핵에서 세포질로의 ｇｓｋ３ 이동 관련 질환의 치료 또는 예방용 약학적 조성물 |
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| EP2698367A1 (en) | 2012-08-14 | 2014-02-19 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | Benzimidazoles for the treatment of cancer |
| GB201223265D0 (en) | 2012-12-21 | 2013-02-06 | Selvita Sa | Novel benzimidazole derivatives as kinase inhibitors |
| CN105263910A (zh) | 2013-02-18 | 2016-01-20 | 斯克利普斯研究所 | 具有治疗潜力的血管加压素受体调节剂 |
| AU2014244083B2 (en) | 2013-03-13 | 2018-09-27 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Methods for modulating chemotherapeutic cytotoxicity |
| SI3010503T1 (sl) | 2013-06-21 | 2020-07-31 | Zenith Epigenetics Ltd. | Novi biciklični inhibitorji bromodomene |
| US9828348B2 (en) | 2013-11-08 | 2017-11-28 | Purdue Pharma L.P. | Benzimidazole derivatives and use thereof |
| KR102494596B1 (ko) | 2014-07-31 | 2023-01-31 | 재단법인 한국파스퇴르연구소 | 2-아미노-벤즈이미다졸 유도체 및 5-리폭시게나아제 및/또는 프로스타글란딘 e 합성효소 억제제로서의 이들의 용도 |
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| GB201603311D0 (en) | 2016-02-25 | 2016-04-13 | Jakobsson Per Johan | New uses and methods |
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| US10501421B1 (en) * | 2017-01-27 | 2019-12-10 | Vanderbilt University | Substituted benzimidazoles as modulators of Ras signaling |
-
2018
- 2018-10-18 HU HUE18867844A patent/HUE070649T2/hu unknown
- 2018-10-18 AU AU2018351059A patent/AU2018351059B2/en active Active
- 2018-10-18 NZ NZ763311A patent/NZ763311A/en unknown
- 2018-10-18 JP JP2020521577A patent/JP7450534B2/ja active Active
- 2018-10-18 WO PCT/US2018/056484 patent/WO2019079578A1/en not_active Ceased
- 2018-10-18 HR HRP20250272TT patent/HRP20250272T1/hr unknown
- 2018-10-18 IL IL273839A patent/IL273839B/en unknown
- 2018-10-18 MA MA050413A patent/MA50413A/fr unknown
- 2018-10-18 MX MX2020003993A patent/MX2020003993A/es unknown
- 2018-10-18 KR KR1020207013744A patent/KR102697255B1/ko active Active
- 2018-10-18 CA CA3079081A patent/CA3079081A1/en active Pending
- 2018-10-18 PL PL18867844.5T patent/PL3697410T3/pl unknown
- 2018-10-18 EP EP18867844.5A patent/EP3697410B1/en active Active
- 2018-10-18 SG SG11202003502VA patent/SG11202003502VA/en unknown
- 2018-10-18 CN CN201880077655.5A patent/CN111417394B/zh active Active
- 2018-10-18 US US16/754,349 patent/US11332459B2/en active Active
- 2018-10-18 ES ES18867844T patent/ES3004333T3/es active Active
- 2018-10-19 TW TW107137075A patent/TWI816704B/zh active
- 2018-10-19 UY UY0001037941A patent/UY37941A/es not_active Application Discontinuation
-
2020
- 2020-04-14 PH PH12020550265A patent/PH12020550265A1/en unknown
- 2020-04-16 CO CONC2020/0004669A patent/CO2020004669A2/es unknown
- 2020-04-16 CL CL2020001020A patent/CL2020001020A1/es unknown
- 2020-04-17 SA SA520411787A patent/SA520411787B1/ar unknown
- 2020-05-14 ZA ZA2020/02762A patent/ZA202002762B/en unknown
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