KR101668514B1 - 항당뇨병제로서 유용한 신규 시클릭 아자벤즈이미다졸 유도체 - Google Patents
항당뇨병제로서 유용한 신규 시클릭 아자벤즈이미다졸 유도체 Download PDFInfo
- Publication number
- KR101668514B1 KR101668514B1 KR1020137024772A KR20137024772A KR101668514B1 KR 101668514 B1 KR101668514 B1 KR 101668514B1 KR 1020137024772 A KR1020137024772 A KR 1020137024772A KR 20137024772 A KR20137024772 A KR 20137024772A KR 101668514 B1 KR101668514 B1 KR 101668514B1
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- South Korea
- Prior art keywords
- alkyl
- cycloalkyl
- phenyl
- substituted
- heteroaryl
- Prior art date
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- 0 O=C1[C@]2OC[C@@](*c([n]c3c4)nc3nc(-c(cc3)ccc3-c3ccc(-[n]5ncnc5)nc3)c4Cl)[C@]2OC1 Chemical compound O=C1[C@]2OC[C@@](*c([n]c3c4)nc3nc(-c(cc3)ccc3-c3ccc(-[n]5ncnc5)nc3)c4Cl)[C@]2OC1 0.000 description 5
- SDMBVHDZFISZPP-UHFFFAOYSA-N Brc(cc1)ccc1-c1n[n](C2CC2)cc1 Chemical compound Brc(cc1)ccc1-c1n[n](C2CC2)cc1 SDMBVHDZFISZPP-UHFFFAOYSA-N 0.000 description 1
- CGPYBQNRXLDREJ-UHFFFAOYSA-N CS(c([nH]c1c2)nc1nc(I)c2Cl)(=O)=O Chemical compound CS(c([nH]c1c2)nc1nc(I)c2Cl)(=O)=O CGPYBQNRXLDREJ-UHFFFAOYSA-N 0.000 description 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/351—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
- A61K31/366—Lactones having six-membered rings, e.g. delta-lactones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- A—HUMAN NECESSITIES
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
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- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161446551P | 2011-02-25 | 2011-02-25 | |
| US61/446,551 | 2011-02-25 | ||
| PCT/US2012/026261 WO2012116145A1 (en) | 2011-02-25 | 2012-02-23 | Novel cyclic azabenzimidazole derivatives useful as anti-diabetic agents |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020157016044A Division KR20150075120A (ko) | 2011-02-25 | 2012-02-23 | 항당뇨병제로서 유용한 신규 시클릭 아자벤즈이미다졸 유도체 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20130128460A KR20130128460A (ko) | 2013-11-26 |
| KR101668514B1 true KR101668514B1 (ko) | 2016-10-21 |
Family
ID=46721223
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020137024772A Active KR101668514B1 (ko) | 2011-02-25 | 2012-02-23 | 항당뇨병제로서 유용한 신규 시클릭 아자벤즈이미다졸 유도체 |
| KR1020157016044A Ceased KR20150075120A (ko) | 2011-02-25 | 2012-02-23 | 항당뇨병제로서 유용한 신규 시클릭 아자벤즈이미다졸 유도체 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020157016044A Ceased KR20150075120A (ko) | 2011-02-25 | 2012-02-23 | 항당뇨병제로서 유용한 신규 시클릭 아자벤즈이미다졸 유도체 |
Country Status (27)
| Country | Link |
|---|---|
| US (1) | US8796258B2 (https=) |
| EP (2) | EP2677869B1 (https=) |
| JP (2) | JP5728099B2 (https=) |
| KR (2) | KR101668514B1 (https=) |
| CN (2) | CN103476258B (https=) |
| AU (1) | AU2012220595B2 (https=) |
| BR (2) | BR112013021236B1 (https=) |
| CA (1) | CA2826649C (https=) |
| CL (1) | CL2013002414A1 (https=) |
| CO (1) | CO6751268A2 (https=) |
| CR (1) | CR20130409A (https=) |
| DO (1) | DOP2013000193A (https=) |
| EA (2) | EA201690035A1 (https=) |
| EC (1) | ECSP13012900A (https=) |
| ES (1) | ES2652662T3 (https=) |
| GT (1) | GT201300208A (https=) |
| IL (1) | IL227640A0 (https=) |
| MA (1) | MA34916B1 (https=) |
| MX (1) | MX348131B (https=) |
| MY (1) | MY159058A (https=) |
| NI (1) | NI201300074A (https=) |
| PE (1) | PE20140859A1 (https=) |
| PH (1) | PH12013501686A1 (https=) |
| SG (1) | SG192941A1 (https=) |
| TN (1) | TN2013000309A1 (https=) |
| WO (1) | WO2012116145A1 (https=) |
| ZA (1) | ZA201306057B (https=) |
Families Citing this family (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8895596B2 (en) | 2010-02-25 | 2014-11-25 | Merck Sharp & Dohme Corp | Cyclic benzimidazole derivatives useful as anti-diabetic agents |
| 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 |
| EP2733141B1 (en) | 2011-07-15 | 2019-01-09 | Shionogi & Co., Ltd. | Azabenzimidazole derivative having ampk-activating activity |
| US8889730B2 (en) | 2012-04-10 | 2014-11-18 | Pfizer Inc. | Indole and indazole compounds that activate AMPK |
| RU2015109706A (ru) * | 2012-08-22 | 2016-10-10 | Мерк Шарп И Доум Корп. | Новые производные азабензимидазол гексагидрофуро[3, 2-в]фурана |
| WO2014031465A1 (en) * | 2012-08-22 | 2014-02-27 | Merck Sharp & Dohme Corp. | Novel azabenzimidazole tetrahydropyran derivatives |
| WO2014031517A1 (en) * | 2012-08-22 | 2014-02-27 | Merck Sharp & Dohme Corp. | Novel azabenzimidazole tetrahydrofuran derivatives |
| WO2014069426A1 (ja) * | 2012-10-31 | 2014-05-08 | 塩野義製薬株式会社 | Ａｍｐｋ活性化作用を有するベンズイミダゾールおよびアザベンズイミダゾール誘導体 |
| EP2951170B1 (en) | 2013-02-04 | 2018-10-24 | Janssen Pharmaceutica NV | Flap modulators |
| TWI644899B (zh) | 2013-02-04 | 2018-12-21 | 健生藥品公司 | Ｆｌａｐ調節劑 |
| EP2963013A4 (en) | 2013-02-27 | 2016-09-14 | Shionogi & Co | INDOLE AND AZAINDOLE DERIVATIVES HAVING AMPK ACTIVATION ACTIVITY EACH |
| WO2014139388A1 (en) | 2013-03-14 | 2014-09-18 | Merck Sharp & Dohme Corp. | Novel indole derivatives useful as anti-diabetic agents |
| JP6064062B2 (ja) | 2013-03-15 | 2017-01-18 | ファイザー・インク | Ａｍｐｋを活性化させるインダゾール化合物 |
| TR201806860T4 (tr) * | 2013-07-17 | 2018-06-21 | Boehringer Ingelheim Int | Yeni azabenzimidazol türevleri. |
| EP3063148B1 (en) * | 2013-10-31 | 2020-04-29 | Boehringer Ingelheim International GmbH | Azabenzimidazole derivatives |
| KR101532211B1 (ko) * | 2014-04-30 | 2015-06-30 | 세종대학교산학협력단 | Ampk 억제기능에 기반한 뇌졸중 치료용 약학적 조성물 및 방법 |
| WO2016001224A1 (en) * | 2014-06-30 | 2016-01-07 | Debiopharm International S.A. | Novel activators of amp-activated protein kinases |
| WO2016023789A1 (en) | 2014-08-11 | 2016-02-18 | Boehringer Ingelheim International Gmbh | Azabenzimidazole derivatives as amp protein kinase agonistes |
| US9980948B2 (en) | 2014-08-27 | 2018-05-29 | Shionogi & Co., Ltd. | Azaindole derivative having AMPK-activating activity |
| MX2017005158A (es) | 2014-10-28 | 2017-07-27 | Shionogi & Co | Derivado heterociclico que tiene actividad de activacion de proteina cinasa activada por adenosina monofostato (ampk). |
| WO2016113299A1 (en) * | 2015-01-16 | 2016-07-21 | Boehringer Ingelheim International Gmbh | New azabenzimidazole derivatives |
| JP6612880B2 (ja) * | 2015-01-16 | 2019-11-27 | 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 | Ａｍｐ活性化タンパク質キナーゼのアゴニストとしての新規アザベンゾイミダゾール誘導体 |
| TWI719970B (zh) * | 2015-03-23 | 2021-03-01 | 美商永斯醫療股份有限公司 | 針對ｉｃｏｓ之抗體 |
| CN108602821B (zh) * | 2015-12-14 | 2021-06-29 | 恒元生物医药科技(苏州)有限公司 | 1h-咪唑并[4,5-b]吡啶基bet溴结构域抑制剂 |
| 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 |
| US10208030B2 (en) * | 2016-04-08 | 2019-02-19 | Mankind Pharma Ltd. | GPR119 agonist compounds |
| US10526345B2 (en) * | 2016-04-08 | 2020-01-07 | Mankind Pharma Ltd. | Compounds as GPR119 agonists |
| US10954229B2 (en) | 2016-04-08 | 2021-03-23 | Mankind Pharma Ltd. | GPR119 agonist compounds |
| US20190135834A1 (en) * | 2016-04-26 | 2019-05-09 | Shionogi & Co., Ltd. | 5-substituted azabenzimidazole derivative having ???? activation action |
| 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 |
| CA3032830A1 (en) * | 2016-08-19 | 2018-02-22 | Rigel Pharmaceuticals, Inc. | Benzimidazole direct ampk activators |
| EP3555064B9 (en) | 2016-12-16 | 2023-03-01 | Pfizer Inc. | Glp-1 receptor agonists and uses thereof |
| CN108727267B (zh) * | 2017-05-26 | 2022-05-13 | 江苏新元素医药科技有限公司 | 一类urat1抑制剂及其应用 |
| CN108558876B (zh) * | 2018-05-28 | 2020-08-04 | 中南大学 | 吡唑[3,4-b]并吡啶类衍生物及其制备方法和应用 |
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| CA3183575A1 (en) | 2020-06-26 | 2021-12-30 | Iyassu Sebhat | Ampk activators |
| EP4227299A4 (en) * | 2020-10-12 | 2025-04-09 | Hangzhou Zhongmeihuadong Pharmaceutical Co., Ltd. | GLP-1 RECEPTOR AGONIST, BENZIMIDAZOLONE AND ITS USE |
| WO2022192079A1 (en) * | 2021-03-08 | 2022-09-15 | The Regents Of The University Of California | Compounds for protection of noise-induced hearing-loss |
| JP2024540522A (ja) | 2021-11-19 | 2024-10-31 | ザ・ブロード・インスティテュート・インコーポレイテッド | キナーゼを標的結合部分で標識するための二官能性キメラ分子及びその使用方法 |
| UY40035A (es) * | 2021-11-23 | 2023-05-31 | Kallyope Inc | Activadores de la ampk |
| CN121752550A (zh) | 2023-08-31 | 2026-03-27 | 深圳众格生物科技有限公司 | 芳基或杂芳基取代的氨基甲酸酯类化合物及其衍生物和用途 |
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