JP6940717B2 - ピロリジン化合物 - Google Patents
ピロリジン化合物 Download PDFInfo
- Publication number
- JP6940717B2 JP6940717B2 JP2021505713A JP2021505713A JP6940717B2 JP 6940717 B2 JP6940717 B2 JP 6940717B2 JP 2021505713 A JP2021505713 A JP 2021505713A JP 2021505713 A JP2021505713 A JP 2021505713A JP 6940717 B2 JP6940717 B2 JP 6940717B2
- Authority
- JP
- Japan
- Prior art keywords
- tert
- oxo
- methyl
- mmol
- pyrrolidine
- 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.)
- Active
Links
- 0 C[C@](CCN(C)C(OC(C)(C)C)=O)C(C)(Cc1cccc(Br)c1)C(*C(C)(C)C)=* Chemical compound C[C@](CCN(C)C(OC(C)(C)C)=O)C(C)(Cc1cccc(Br)c1)C(*C(C)(C)C)=* 0.000 description 3
- KFTBZGIWBBYBTI-HUUCEWRRSA-N CC(C)(C)OC(N(CC1)C[C@@H]1[C@@H](Cc1ccccc1)C(O)=O)=O Chemical compound CC(C)(C)OC(N(CC1)C[C@@H]1[C@@H](Cc1ccccc1)C(O)=O)=O KFTBZGIWBBYBTI-HUUCEWRRSA-N 0.000 description 1
- WKHNWNNHDXIQAY-FRUPOSBSSA-N CC(C)(C)OC([C@@H](Cc1cc(S(c2cc(C[C@@H]([C@@H](CC3)CN3C(OC(C)(C)C)=O)C(OC(C)(C)C)=O)ccc2)(=O)=O)ccc1)[C@@H](CC1)CN1C(OC(C)(C)C)=O)O Chemical compound CC(C)(C)OC([C@@H](Cc1cc(S(c2cc(C[C@@H]([C@@H](CC3)CN3C(OC(C)(C)C)=O)C(OC(C)(C)C)=O)ccc2)(=O)=O)ccc1)[C@@H](CC1)CN1C(OC(C)(C)C)=O)O WKHNWNNHDXIQAY-FRUPOSBSSA-N 0.000 description 1
- FTMWVSDGXUTWQJ-XUHBEUDXSA-N OC([C@@H](CC1C=CC=C(CN(Cc2cc(C[C@@H]([C@@H]3CNCC3)C(O)=O)ccc2)Cc2cc(/C=C(\[C@@H]3CNCC3)/C(O)=O)ccc2)C1)[C@@H]1CNCC1)=O Chemical compound OC([C@@H](CC1C=CC=C(CN(Cc2cc(C[C@@H]([C@@H]3CNCC3)C(O)=O)ccc2)Cc2cc(/C=C(\[C@@H]3CNCC3)/C(O)=O)ccc2)C1)[C@@H]1CNCC1)=O FTMWVSDGXUTWQJ-XUHBEUDXSA-N 0.000 description 1
- BRLGERLDHZRETI-BMBIFOQRSA-N OC([C@@H](Cc1cccc(CN(Cc2cccc(C[C@@H]([C@@H]3CNCC3)C(O)=O)c2)Cc2cc(C[C@@H](C3CNCC3)C(O)=O)ccc2)c1)[C@@H]1CNCC1)=O Chemical compound OC([C@@H](Cc1cccc(CN(Cc2cccc(C[C@@H]([C@@H]3CNCC3)C(O)=O)c2)Cc2cc(C[C@@H](C3CNCC3)C(O)=O)ccc2)c1)[C@@H]1CNCC1)=O BRLGERLDHZRETI-BMBIFOQRSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/06—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Epidemiology (AREA)
- Pyrrole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Priority Applications (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021143227A JP7508422B2 (ja) | 2019-06-07 | 2021-09-02 | ピロリジン化合物 |
| JP2024098153A JP7658014B2 (ja) | 2019-06-07 | 2024-06-18 | ピロリジン化合物 |
| JP2025052039A JP2025098178A (ja) | 2019-06-07 | 2025-03-26 | ピロリジン化合物 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP19382477 | 2019-06-07 | ||
| EP19382477.8 | 2019-06-07 | ||
| PCT/US2020/035825 WO2020247429A1 (en) | 2019-06-07 | 2020-06-03 | Pyrrolidine compounds |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021143227A Division JP7508422B2 (ja) | 2019-06-07 | 2021-09-02 | ピロリジン化合物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2021524498A JP2021524498A (ja) | 2021-09-13 |
| JP6940717B2 true JP6940717B2 (ja) | 2021-09-29 |
Family
ID=66821161
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021505713A Active JP6940717B2 (ja) | 2019-06-07 | 2020-06-03 | ピロリジン化合物 |
| JP2021143227A Active JP7508422B2 (ja) | 2019-06-07 | 2021-09-02 | ピロリジン化合物 |
| JP2024098153A Active JP7658014B2 (ja) | 2019-06-07 | 2024-06-18 | ピロリジン化合物 |
| JP2025052039A Pending JP2025098178A (ja) | 2019-06-07 | 2025-03-26 | ピロリジン化合物 |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021143227A Active JP7508422B2 (ja) | 2019-06-07 | 2021-09-02 | ピロリジン化合物 |
| JP2024098153A Active JP7658014B2 (ja) | 2019-06-07 | 2024-06-18 | ピロリジン化合物 |
| JP2025052039A Pending JP2025098178A (ja) | 2019-06-07 | 2025-03-26 | ピロリジン化合物 |
Country Status (25)
| Country | Link |
|---|---|
| US (3) | US11286249B2 (https=) |
| EP (1) | EP3980409A1 (https=) |
| JP (4) | JP6940717B2 (https=) |
| KR (3) | KR102629923B1 (https=) |
| CN (1) | CN114008021B (https=) |
| AU (1) | AU2020287599B2 (https=) |
| BR (1) | BR112021023347A2 (https=) |
| CL (1) | CL2021003202A1 (https=) |
| CO (1) | CO2021016295A2 (https=) |
| CR (1) | CR20210602A (https=) |
| DO (1) | DOP2021000254A (https=) |
| EA (1) | EA202193007A1 (https=) |
| EC (1) | ECSP21088515A (https=) |
| IL (2) | IL288174B2 (https=) |
| JO (1) | JOP20210319B1 (https=) |
| MA (1) | MA56115A (https=) |
| MX (2) | MX2021014913A (https=) |
| MY (1) | MY200810A (https=) |
| PE (1) | PE20220134A1 (https=) |
| PH (1) | PH12021553062A1 (https=) |
| SA (1) | SA521431048B1 (https=) |
| SG (1) | SG11202113244UA (https=) |
| UA (1) | UA128540C2 (https=) |
| WO (1) | WO2020247429A1 (https=) |
| ZA (1) | ZA202109251B (https=) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2023078333A1 (zh) | 2021-11-03 | 2023-05-11 | 上海拓界生物医药科技有限公司 | 一种取代的苯丙酸衍生物及其用途一种取代的苯丙酸衍生物及其用途 |
| WO2023146785A1 (en) | 2022-01-26 | 2023-08-03 | Eli Lilly And Company | Pyrrolidine compounds |
| CN120787221A (zh) | 2023-03-24 | 2025-10-14 | 上海京新生物医药有限公司 | 一种环状胺衍生物及其组合物与应用 |
| CN119894882A (zh) * | 2023-04-21 | 2025-04-25 | 深圳信立泰药业股份有限公司 | 一种叔胺类化合物及其制备方法和医药用途 |
| WO2024230805A1 (zh) | 2023-05-11 | 2024-11-14 | 江苏恒瑞医药股份有限公司 | 一种脂蛋白化合物晶型及其制备方法 |
| TW202509024A (zh) | 2023-05-19 | 2025-03-01 | 大陸商深圳信立泰藥業股份有限公司 | 一種磺醯胺類化合物及其製備方法和醫藥用途 |
| EP4734986A1 (en) | 2023-06-30 | 2026-05-06 | Eli Lilly and Company | Therapeutic uses and doses of lp(a) disrupter compounds |
| WO2025024216A1 (en) | 2023-07-21 | 2025-01-30 | Eli Lilly And Company | PYRROLIDINE COMPOUNDS Lp(a) LOWERING ACTIVITY |
| WO2025024218A1 (en) | 2023-07-21 | 2025-01-30 | Eli Lilly And Company | PYRROLIDINE COMPOUNDS WITH Lp(a) LOWERING ACTIVITY |
| WO2025024210A1 (en) | 2023-07-21 | 2025-01-30 | Eli Lilly And Company | Piperidine, morpholine and tetrahydro-pyridazine compounds with lp(a) lowering activity |
| CN121548568A (zh) | 2023-07-21 | 2026-02-17 | 伊莱利利公司 | 具有Lp(a)降低活性的哌啶化合物 |
| CN119490445A (zh) * | 2023-08-15 | 2025-02-21 | 深圳信立泰药业股份有限公司 | 一种酰基类化合物及其制备方法和医药用途 |
| US20250179055A1 (en) * | 2023-11-17 | 2025-06-05 | Innovstone Therapeutics Limited | Substituted 2-(pyrrolidine-3-yl)acetic acid derivative, preparation method and use thereof |
| WO2025108255A1 (zh) * | 2023-11-20 | 2025-05-30 | 上海齐鲁制药研究中心有限公司 | 一种多环类衍生物、其制备方法和应用 |
| WO2025237188A1 (zh) * | 2024-05-14 | 2025-11-20 | 石家庄以岭药业股份有限公司 | 一种LP(a)抑制剂化合物及其应用 |
| WO2025255324A1 (en) * | 2024-06-06 | 2025-12-11 | Lapis Therapeutics, Inc. | Inhibitors of lipoprotein(a) assembly |
| WO2026061518A1 (zh) * | 2024-09-23 | 2026-03-26 | 上海京新生物医药有限公司 | 一种环状胺衍生物的固体形式、制备方法及药物组合物 |
| JP7850336B1 (ja) | 2024-11-14 | 2026-04-22 | イーライ リリー アンド カンパニー | Lp(a)阻害剤化合物を含む経口組成物 |
| CN121609698A (zh) * | 2026-01-30 | 2026-03-06 | 山东京新药业有限公司 | 一种莫伐培林及中间体的制备方法 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2685325B1 (fr) * | 1991-12-20 | 1994-02-04 | Adir Cie | Nouveaux derives de pyrrolidine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent. |
| US7371777B2 (en) | 2001-08-17 | 2008-05-13 | Eisai Co., Ltd. | Cyclic compound and PPAR agonist |
| AU2003300438A1 (en) * | 2003-12-24 | 2005-08-03 | Esperion Therapeutics, Inc. | Ether compounds and compositions for cholesterol management and related uses |
| JP2007525408A (ja) * | 2003-12-24 | 2007-09-06 | エスペリオン セラピューティクス,インコーポレイテッド | コレステロール管理および関連使用のためのケトン化合物および組成物 |
| CA2694362A1 (en) | 2007-07-27 | 2009-02-05 | F. Hoffmann-La Roche Ag | 2-azetidinemethaneamines and 2-pyrrolidinemethaneamines as taar-ligands |
| KR20180086259A (ko) | 2016-02-03 | 2018-07-30 | 상하이 하이옌 파마슈티컬 테크놀로지 컴퍼니, 리미티드 | 헤테로 고리로 치환된 n-설포닐벤즈아미드 유도체, 이의 제조 방법과 약학적 용도 |
| CN112321475B (zh) | 2020-11-13 | 2022-06-10 | 四川大学 | 一种γ-氨基酸类似物及其合成方法 |
-
2020
- 2020-06-03 US US17/056,144 patent/US11286249B2/en active Active
- 2020-06-03 PH PH1/2021/553062A patent/PH12021553062A1/en unknown
- 2020-06-03 SG SG11202113244UA patent/SG11202113244UA/en unknown
- 2020-06-03 PE PE2021002037A patent/PE20220134A1/es unknown
- 2020-06-03 KR KR1020227043106A patent/KR102629923B1/ko active Active
- 2020-06-03 WO PCT/US2020/035825 patent/WO2020247429A1/en not_active Ceased
- 2020-06-03 CR CR20210602A patent/CR20210602A/es unknown
- 2020-06-03 UA UAA202106553A patent/UA128540C2/uk unknown
- 2020-06-03 BR BR112021023347A patent/BR112021023347A2/pt unknown
- 2020-06-03 IL IL288174A patent/IL288174B2/en unknown
- 2020-06-03 IL IL321703A patent/IL321703B1/en unknown
- 2020-06-03 KR KR1020247002433A patent/KR102720992B1/ko active Active
- 2020-06-03 MA MA056115A patent/MA56115A/fr unknown
- 2020-06-03 JP JP2021505713A patent/JP6940717B2/ja active Active
- 2020-06-03 EA EA202193007A patent/EA202193007A1/ru unknown
- 2020-06-03 EP EP20747210.1A patent/EP3980409A1/en active Pending
- 2020-06-03 CN CN202080041924.XA patent/CN114008021B/zh active Active
- 2020-06-03 AU AU2020287599A patent/AU2020287599B2/en active Active
- 2020-06-03 MY MYPI2021007256A patent/MY200810A/en unknown
- 2020-06-03 MX MX2021014913A patent/MX2021014913A/es unknown
- 2020-06-03 KR KR1020217040065A patent/KR102477481B1/ko active Active
-
2021
- 2021-09-02 JP JP2021143227A patent/JP7508422B2/ja active Active
- 2021-11-18 ZA ZA2021/09251A patent/ZA202109251B/en unknown
- 2021-11-30 CO CONC2021/0016295A patent/CO2021016295A2/es unknown
- 2021-12-01 JO JOJO/P/2021/0319A patent/JOP20210319B1/ar active
- 2021-12-01 CL CL2021003202A patent/CL2021003202A1/es unknown
- 2021-12-03 MX MX2025001789A patent/MX2025001789A/es unknown
- 2021-12-07 EC ECSENADI202188515A patent/ECSP21088515A/es unknown
- 2021-12-07 DO DO2021000254A patent/DOP2021000254A/es unknown
- 2021-12-07 SA SA521431048A patent/SA521431048B1/ar unknown
-
2022
- 2022-02-15 US US17/671,806 patent/US12441714B2/en active Active
-
2024
- 2024-06-18 JP JP2024098153A patent/JP7658014B2/ja active Active
-
2025
- 2025-03-26 JP JP2025052039A patent/JP2025098178A/ja active Pending
- 2025-07-11 US US19/267,125 patent/US20260055086A1/en active Pending
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