JP2015526468A5 - - Google Patents
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- Publication number
- JP2015526468A5 JP2015526468A5 JP2015528552A JP2015528552A JP2015526468A5 JP 2015526468 A5 JP2015526468 A5 JP 2015526468A5 JP 2015528552 A JP2015528552 A JP 2015528552A JP 2015528552 A JP2015528552 A JP 2015528552A JP 2015526468 A5 JP2015526468 A5 JP 2015526468A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- aryl
- heteroaryl
- cycloheteroalkyl
- cycloalkyl
- 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.)
- Pending
Links
- 125000000217 alkyl group Chemical group 0.000 claims 193
- 125000003118 aryl group Chemical group 0.000 claims 60
- 125000001072 heteroaryl group Chemical group 0.000 claims 55
- 150000001875 compounds Chemical class 0.000 claims 46
- 125000001424 substituent group Chemical group 0.000 claims 44
- 229910052736 halogen Inorganic materials 0.000 claims 37
- 150000002367 halogens Chemical class 0.000 claims 33
- 229910052739 hydrogen Inorganic materials 0.000 claims 31
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 27
- 239000001257 hydrogen Substances 0.000 claims 27
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 24
- 150000003839 salts Chemical class 0.000 claims 23
- 125000000304 alkynyl group Chemical group 0.000 claims 20
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 20
- 125000000753 cycloalkyl group Chemical group 0.000 claims 18
- 125000004093 cyano group Chemical group *C#N 0.000 claims 14
- 229910052757 nitrogen Inorganic materials 0.000 claims 11
- 125000003342 alkenyl group Chemical group 0.000 claims 10
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 125000005418 aryl aryl group Chemical group 0.000 claims 7
- -1 -C 3-7 cycloalkyl Chemical group 0.000 claims 5
- 150000001204 N-oxides Chemical class 0.000 claims 5
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- 125000006717 (C3-C10) cycloalkenyl group Chemical group 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 102000014156 AMP-Activated Protein Kinases Human genes 0.000 claims 2
- 108010011376 AMP-Activated Protein Kinases Proteins 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- 230000004913 activation Effects 0.000 claims 2
- 125000005025 alkynylaryl group Chemical group 0.000 claims 2
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 238000002560 therapeutic procedure Methods 0.000 claims 2
- 229910052727 yttrium Inorganic materials 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 1
- RYMZZMVNJRMUDD-UHFFFAOYSA-N SJ000286063 Natural products C12C(OC(=O)C(C)(C)CC)CC(C)C=C2C=CC(C)C1CCC1CC(O)CC(=O)O1 RYMZZMVNJRMUDD-UHFFFAOYSA-N 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- OLNTVTPDXPETLC-XPWALMASSA-N ezetimibe Chemical compound N1([C@@H]([C@H](C1=O)CC[C@H](O)C=1C=CC(F)=CC=1)C=1C=CC(O)=CC=1)C1=CC=C(F)C=C1 OLNTVTPDXPETLC-XPWALMASSA-N 0.000 claims 1
- 229960000815 ezetimibe Drugs 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- RYMZZMVNJRMUDD-HGQWONQESA-N simvastatin Chemical compound C([C@H]1[C@@H](C)C=CC2=C[C@H](C)C[C@@H]([C@H]12)OC(=O)C(C)(C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 RYMZZMVNJRMUDD-HGQWONQESA-N 0.000 claims 1
- 229960002855 simvastatin Drugs 0.000 claims 1
- MFFMDFFZMYYVKS-SECBINFHSA-N sitagliptin Chemical compound C([C@H](CC(=O)N1CC=2N(C(=NN=2)C(F)(F)F)CC1)N)C1=CC(F)=C(F)C=C1F MFFMDFFZMYYVKS-SECBINFHSA-N 0.000 claims 1
- 229960004034 sitagliptin Drugs 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261692018P | 2012-08-22 | 2012-08-22 | |
| US61/692,018 | 2012-08-22 | ||
| PCT/US2013/055528 WO2014031515A1 (en) | 2012-08-22 | 2013-08-19 | Novel azabenzimidazole hexahydrofuro[3,2-b]furan derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2015526468A JP2015526468A (ja) | 2015-09-10 |
| JP2015526468A5 true JP2015526468A5 (enExample) | 2015-10-29 |
Family
ID=50150322
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015528552A Pending JP2015526468A (ja) | 2012-08-22 | 2013-08-19 | 新規なアザベンズイミダゾールヘキサヒドロフロ[3,2−b]フラン誘導体 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US9290517B2 (enExample) |
| EP (1) | EP2888005B1 (enExample) |
| JP (1) | JP2015526468A (enExample) |
| KR (1) | KR20150045436A (enExample) |
| CN (1) | CN104718004A (enExample) |
| AR (1) | AR092201A1 (enExample) |
| AU (1) | AU2013306030A1 (enExample) |
| BR (1) | BR112015003109A2 (enExample) |
| CA (1) | CA2881836A1 (enExample) |
| RU (1) | RU2015109706A (enExample) |
| TW (1) | TW201412751A (enExample) |
| WO (1) | WO2014031515A1 (enExample) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014031465A1 (en) | 2012-08-22 | 2014-02-27 | Merck Sharp & Dohme Corp. | Novel azabenzimidazole tetrahydropyran derivatives |
| WO2014031468A1 (en) | 2012-08-22 | 2014-02-27 | Merck Sharp & Dohme Corp. | Novel benzimidazole hexahydrofuro[3,2-b]furan derivatives |
| WO2014031441A1 (en) * | 2012-08-22 | 2014-02-27 | Merck Sharp & Dohme Corp. | Novel benzimidazole tetrahydrofuran derivatives |
| EP2888008B1 (en) | 2012-08-22 | 2018-12-26 | Merck Sharp & Dohme Corp. | Novel azabenzimidazole tetrahydrofuran derivatives |
| WO2014031445A1 (en) | 2012-08-22 | 2014-02-27 | Merck Sharp & Dohme Corp. | Novel benzimidazole tetrahydropyran derivatives |
| CA2903657A1 (en) | 2013-02-27 | 2014-09-04 | Shionogi & Co., Ltd. | Indole and azaindole derivatives each having ampk-activating activity |
| DK3022210T3 (en) * | 2013-07-17 | 2018-06-06 | Boehringer Ingelheim Int | NEW AZABENZIMIDAZOLD DERIVATIVES. |
| AU2015309863B2 (en) | 2014-08-27 | 2019-12-05 | Shionogi & Co., Ltd. | Azaindole derivative having AMPK-activating effect |
| KR20170077131A (ko) | 2014-10-28 | 2017-07-05 | 시오노기세야쿠 가부시키가이샤 | Ampk 활성화 작용을 갖는 복소환 유도체 |
| US10307402B2 (en) | 2015-01-16 | 2019-06-04 | Boehringer Ingelheim International Gmbh | Azabenzimidazole derivatives as agonists of the AMP-activated protein kinase |
| ES2821049T3 (es) * | 2015-06-18 | 2021-04-23 | 89Bio Ltd | Derivados de piperidina 1,4 sustituidos |
| US10919875B2 (en) | 2015-06-18 | 2021-02-16 | 89Bio Ltd | Substituted 4-benzyl and 4-benzoyl piperidine derivatives |
| CN105503927B (zh) * | 2016-01-11 | 2017-04-26 | 沧州普瑞东方科技有限公司 | 一种合成3,6‑二氢‑2h‑吡(噻)喃‑4‑硼酸酯的方法 |
| JPWO2017146186A1 (ja) | 2016-02-26 | 2018-12-20 | 塩野義製薬株式会社 | Ampk活性化作用を有する5−フェニルアザインドール誘導体 |
| CN109476661A (zh) | 2016-05-20 | 2019-03-15 | 盐野义制药株式会社 | 具有ampk活化作用的5-取代苯并咪唑及5-取代氮杂苯并咪唑衍生物 |
| CN106478653B (zh) * | 2016-10-16 | 2018-10-12 | 云南民族大学 | 异山梨醇—单咪唑盐类化合物及其制备方法 |
| US11590161B2 (en) | 2018-08-13 | 2023-02-28 | Viscera Labs, Inc. | Therapeutic composition and methods |
| US11524029B2 (en) | 2018-08-13 | 2022-12-13 | Viscera Labs, Inc. | Therapeutic composition and methods |
| CA3132446A1 (en) * | 2019-03-05 | 2020-09-10 | Centre For Addiction And Mental Health | Modulators of ampa receptor signaling |
| CN111423435B (zh) * | 2020-03-30 | 2021-10-15 | 厦门大学 | (1H-咪唑并[4,5-b]吡啶-6-基)吡啶衍生物及其应用 |
| JP2023526625A (ja) | 2020-05-19 | 2023-06-22 | キャリーオペ,インク. | Ampkアクチベーター |
| CN116390925A (zh) * | 2020-06-26 | 2023-07-04 | 卡尔优普公司 | Ampk活化剂 |
| US20240024490A1 (en) * | 2021-04-09 | 2024-01-25 | The Broad Institute, Inc. | Bifunctional molecules for selective modification of target substrates |
| JP2025526423A (ja) * | 2022-07-28 | 2025-08-13 | エーシー・イミューン・エス・アー | 新規化合物 |
| CN115944612A (zh) * | 2022-12-23 | 2023-04-11 | 敖虎山 | 胰高血糖素拮抗剂阿度格列凡的新用途 |
| KR102638391B1 (ko) * | 2023-05-30 | 2024-02-20 | 삼화페인트공업주식회사 | 다이알칸설포닐 아이소소바이드 화합물의 제조 방법, 리튬이차전지용 전해액 첨가제, 리튬이차전지용 전해액 및 리튬이차전지 |
| CN117838690B (zh) * | 2023-10-09 | 2024-09-13 | 中国药科大学 | 一种治疗以ampk激活为治疗靶点的疾病的复方药物及其应用 |
Family Cites Families (41)
| Publication number | Priority date | Publication date | Assignee | Title |
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| JPS58193541A (ja) | 1982-05-07 | 1983-11-11 | Konishiroku Photo Ind Co Ltd | 熱現像画像記録材料 |
| JPH0245181B2 (ja) | 1983-03-16 | 1990-10-08 | Fuji Photo Film Co Ltd | Netsugenzokaraakankozairyo |
| GB8313322D0 (en) | 1983-05-14 | 1983-06-22 | Ciba Geigy Ag | Heterocyclic-(cyclo)aliphatic carboxylic acids |
| GB8313321D0 (en) | 1983-05-14 | 1983-06-22 | Ciba Geigy Ag | Preparation of mercaptan substituted carboxylic acids |
| GB8313320D0 (en) | 1983-05-14 | 1983-06-22 | Ciba Geigy Ag | Coating compositions |
| PT100905A (pt) | 1991-09-30 | 1994-02-28 | Eisai Co Ltd | Compostos heterociclicos azotados biciclicos contendo aneis de benzeno, ciclo-hexano ou piridina e de pirimidina, piridina ou imidazol substituidos e composicoes farmaceuticas que os contem |
| JPH06298731A (ja) | 1993-04-13 | 1994-10-25 | Fuji Photo Film Co Ltd | 複素環化合物の製造方法 |
| DE69416518T2 (de) * | 1993-07-23 | 1999-07-01 | Merrell Pharmaceuticals Inc., Cincinnati, Ohio | Neue 9-n-bicyclische nucleosidverbindungen nützlich als selektive inhibitoren von proinflammatorische cytokinen |
| AU2395095A (en) | 1994-04-29 | 1995-11-29 | G.D. Searle & Co. | Method of using (h+/k+) atpase inhibitors as antiviral agents |
| WO1998039342A1 (en) | 1997-03-07 | 1998-09-11 | Metabasis Therapeutics, Inc. | Novel indole and azaindole inhibitors of fructose-1,6-bisphosphatase |
| ZA981936B (en) | 1997-03-07 | 1999-09-06 | Metabasis Therapeutics Inc | Novel benzimidazole inhibitors of fructose 1,6-bisphosphatase. |
| US6312662B1 (en) | 1998-03-06 | 2001-11-06 | Metabasis Therapeutics, Inc. | Prodrugs phosphorus-containing compounds |
| EE04904B1 (et) | 1998-07-15 | 2007-10-15 | Teijin Limited | Tiobensimidasooli derivaadid ja farmatseutiline kompositsioon |
| DE69910045T2 (de) | 1998-09-09 | 2004-04-22 | Metabasis Therapeutics Inc., San Diego | Neue heteroaromatische fructose 1,6-bisphosphatase inhibitoren |
| CA2365118A1 (en) | 2000-01-17 | 2001-07-26 | Teijin Limited | Inhibitor against human chymase activity |
| KR100763779B1 (ko) | 2000-01-17 | 2007-10-05 | 데이진 가부시키가이샤 | 벤즈이미다졸 유도체 |
| EP1342717A4 (en) * | 2000-11-15 | 2005-02-16 | Banyu Pharma Co Ltd | benzimidazole derivatives |
| US7030150B2 (en) | 2001-05-11 | 2006-04-18 | Trimeris, Inc. | Benzimidazole compounds and antiviral uses thereof |
| CA2442761A1 (en) | 2001-08-24 | 2003-03-06 | Teijin Limited | Drugs comprising chymase inhibitors and ace inhibitors as effective ingredients |
| US7119205B2 (en) | 2003-05-16 | 2006-10-10 | Abbott Laboratories | Thienopyridones as AMPK activators for the treatment of diabetes and obesity |
| JP2007521296A (ja) | 2003-07-01 | 2007-08-02 | メルク エンド カムパニー インコーポレーテッド | 高眼圧の治療のための眼科用組成物 |
| US20070161582A1 (en) | 2003-08-08 | 2007-07-12 | Dusan Mijikovic | Pharmaceutical compositions and methods for metabolic modulation |
| US20050148643A1 (en) | 2003-08-19 | 2005-07-07 | Agouron Pharmaceuticals, Inc. | Carbamate compositions and methods fo rmodulating the activity of the CHK1 enzyme |
| WO2005018672A1 (ja) | 2003-08-22 | 2005-03-03 | Teijin Pharma Limited | キマーゼ阻害剤を有効成分として含有する薬剤 |
| JP2007512359A (ja) | 2003-11-19 | 2007-05-17 | メタバシス・セラピューティクス・インコーポレイテッド | 新規なリン含有甲状腺ホルモン様物質 |
| WO2006094209A2 (en) | 2005-03-03 | 2006-09-08 | Sirtris Pharmaceuticals, Inc. | N-benzimidazolylalkyl-substituted amide sirtuin modulators |
| EP1884513A4 (en) | 2005-05-23 | 2010-04-28 | Japan Tobacco Inc | PYRAZOLE COMPOUND AND THERAPEUTIC AGENT FOR DIABETES COMPRISING THE SAME |
| EP1907369A4 (en) | 2005-07-04 | 2009-07-22 | Reddys Lab Ltd Dr | THIAZOLE DERIVATIVES USEFUL AS AMPK ACTIVATORS |
| FR2903695B1 (fr) | 2006-07-13 | 2008-10-24 | Merck Sante Soc Par Actions Si | Utilisation de derives d'imidazole activateurs de l'ampk, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| AU2009296820B2 (en) * | 2008-09-26 | 2014-03-20 | Merck Sharp & Dohme Llc | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
| US8410284B2 (en) * | 2008-10-22 | 2013-04-02 | Merck Sharp & Dohme Corp | Cyclic benzimidazole derivatives useful as anti-diabetic agents |
| US8563746B2 (en) * | 2008-10-29 | 2013-10-22 | Merck Sharp & Dohme Corp | Cyclic benzimidazole derivatives useful as anti-diabetic agents |
| US8329914B2 (en) * | 2008-10-31 | 2012-12-11 | Merck Sharp & Dohme Corp | Cyclic benzimidazole derivatives useful as anti-diabetic agents |
| JP2013520502A (ja) * | 2010-02-25 | 2013-06-06 | メルク・シャープ・エンド・ドーム・コーポレイション | 有用な抗糖尿病薬である新規な環状ベンズイミダゾール誘導体 |
| WO2012033149A1 (ja) | 2010-09-10 | 2012-03-15 | 塩野義製薬株式会社 | Ampk活性化作用を有するヘテロ環縮合イミダゾール誘導体 |
| PH12013501686A1 (en) * | 2011-02-25 | 2017-10-25 | Merck Sharp & Dohme | Novel cyclic azabenzimidazole derivatives useful as anti-diabetic agents |
| EP2888008B1 (en) | 2012-08-22 | 2018-12-26 | Merck Sharp & Dohme Corp. | Novel azabenzimidazole tetrahydrofuran derivatives |
| WO2014031445A1 (en) | 2012-08-22 | 2014-02-27 | Merck Sharp & Dohme Corp. | Novel benzimidazole tetrahydropyran derivatives |
| WO2014031441A1 (en) | 2012-08-22 | 2014-02-27 | Merck Sharp & Dohme Corp. | Novel benzimidazole tetrahydrofuran derivatives |
| WO2014031465A1 (en) | 2012-08-22 | 2014-02-27 | Merck Sharp & Dohme Corp. | Novel azabenzimidazole tetrahydropyran derivatives |
| WO2014031468A1 (en) | 2012-08-22 | 2014-02-27 | Merck Sharp & Dohme Corp. | Novel benzimidazole hexahydrofuro[3,2-b]furan derivatives |
-
2013
- 2013-08-19 RU RU2015109706A patent/RU2015109706A/ru not_active Application Discontinuation
- 2013-08-19 WO PCT/US2013/055528 patent/WO2014031515A1/en not_active Ceased
- 2013-08-19 US US14/419,774 patent/US9290517B2/en active Active
- 2013-08-19 EP EP13830277.3A patent/EP2888005B1/en active Active
- 2013-08-19 CA CA2881836A patent/CA2881836A1/en not_active Abandoned
- 2013-08-19 CN CN201380055225.0A patent/CN104718004A/zh active Pending
- 2013-08-19 JP JP2015528552A patent/JP2015526468A/ja active Pending
- 2013-08-19 AU AU2013306030A patent/AU2013306030A1/en not_active Abandoned
- 2013-08-19 KR KR20157003910A patent/KR20150045436A/ko not_active Withdrawn
- 2013-08-19 BR BR112015003109A patent/BR112015003109A2/pt not_active Application Discontinuation
- 2013-08-22 AR ARP130102977 patent/AR092201A1/es unknown
- 2013-08-22 TW TW102130132A patent/TW201412751A/zh unknown
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