CA2724774C - Pyrazolospiroketone acetyl-coa carboxylase inhibitors - Google Patents
Pyrazolospiroketone acetyl-coa carboxylase inhibitors Download PDFInfo
- Publication number
- CA2724774C CA2724774C CA2724774A CA2724774A CA2724774C CA 2724774 C CA2724774 C CA 2724774C CA 2724774 A CA2724774 A CA 2724774A CA 2724774 A CA2724774 A CA 2724774A CA 2724774 C CA2724774 C CA 2724774C
- Authority
- CA
- Canada
- Prior art keywords
- mmol
- minutes
- hplc
- retention time
- solution
- 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.)
- Expired - Fee Related
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
- C07D491/20—Spiro-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Diabetes (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Child & Adolescent Psychology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Plant Substances (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US5665208P | 2008-05-28 | 2008-05-28 | |
| US61/056,652 | 2008-05-28 | ||
| US5868908P | 2008-06-04 | 2008-06-04 | |
| US61/058,689 | 2008-06-04 | ||
| US17151909P | 2009-04-22 | 2009-04-22 | |
| US61/171,519 | 2009-04-22 | ||
| PCT/IB2009/005649 WO2009144554A1 (en) | 2008-05-28 | 2009-05-18 | Pyrazolospiroketone acetyl-c0a carboxylase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2724774A1 CA2724774A1 (en) | 2009-12-03 |
| CA2724774C true CA2724774C (en) | 2013-06-25 |
Family
ID=40974611
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2724774A Expired - Fee Related CA2724774C (en) | 2008-05-28 | 2009-05-18 | Pyrazolospiroketone acetyl-coa carboxylase inhibitors |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US8318762B2 (enExample) |
| EP (1) | EP2297163B1 (enExample) |
| JP (1) | JP5435592B2 (enExample) |
| CA (1) | CA2724774C (enExample) |
| ES (1) | ES2545231T3 (enExample) |
| WO (1) | WO2009144554A1 (enExample) |
Families Citing this family (65)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009144554A1 (en) | 2008-05-28 | 2009-12-03 | Pfizer, Inc. | Pyrazolospiroketone acetyl-c0a carboxylase inhibitors |
| PT2499139E (pt) * | 2009-11-10 | 2014-02-10 | Pfizer | Inibidores de n1-pirazolospirocetona acetil-coa carboxilase |
| PL2547679T3 (pl) | 2010-03-19 | 2016-02-29 | Pfizer | Pochodne 2,3-dihydro-1H-inden-1-ylo-2,7-diazaspiro[3.5]nonanu i ich zastosowanie jako antagonistów lub odwrotnych agonistów receptora greliny |
| CA2812526A1 (en) | 2010-05-06 | 2011-11-10 | Vertex Pharmaceuticals Incorporated | Heterocyclic chromene-spirocyclic piperidine amides as modulators of ion channels |
| HRP20161178T1 (hr) | 2010-09-30 | 2016-11-04 | Pfizer Inc. | N1-PIRAZOLOSPIROKETONSKI INHIBITORI ACETIL-CoA-KARBOKSILAZE |
| HUE025078T2 (en) | 2010-10-29 | 2016-01-28 | Pfizer | N1 / N2-lactam-acetyl-CoA carboxylase inhibitors |
| BR112013019211A2 (pt) | 2011-02-02 | 2021-07-06 | Vertex Pharma | amidas de piperidina espirocíclicas de pirrolopirazina como moduladores de canais de íon |
| CN103443105A (zh) * | 2011-02-18 | 2013-12-11 | 沃泰克斯药物股份有限公司 | 作为离子通道调节剂的苯并二氢吡喃-螺环哌啶酰胺 |
| US8828996B2 (en) | 2011-03-14 | 2014-09-09 | Vertex Pharmaceuticals Incorporated | Morpholine-spirocyclic piperidine amides as modulators of ion channels |
| PE20141187A1 (es) * | 2011-04-22 | 2014-09-18 | Pfizer | Inhibidores sustituidos de aeitl-coa carboxilasa |
| CA2841757A1 (en) | 2011-07-15 | 2013-01-24 | Etzer Darout | Gpr 119 modulators |
| RU2013157388A (ru) | 2011-07-22 | 2015-08-27 | Пфайзер Инк. | Хинолинильные модуляторы глюкагонового рецептора |
| JP6043355B2 (ja) | 2011-08-31 | 2016-12-14 | ファイザー・インク | ヘキサヒドロピラノ[3,4−d][1,3]チアジン−2−アミン化合物 |
| EP2567959B1 (en) | 2011-09-12 | 2014-04-16 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| GEP201706656B (en) | 2011-11-11 | 2017-04-25 | Pfizer | 2-thiopyrimidinones |
| SG11201405477XA (en) | 2012-04-06 | 2014-11-27 | Pfizer | Diacylglycerol acyltransferase 2 inhibitors |
| US8889730B2 (en) | 2012-04-10 | 2014-11-18 | Pfizer Inc. | Indole and indazole compounds that activate AMPK |
| ES2585262T3 (es) | 2012-05-04 | 2016-10-04 | Pfizer Inc | Compuestos heterocíclicos de hexahidropiran[3,4-d][1,3]tiazin-2-amina sustituidos como inhibidores de PPA, BACE1 y BACE2 |
| CA2882389A1 (en) | 2012-09-20 | 2014-03-27 | Pfizer Inc. | Alkyl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| CN102898374B (zh) * | 2012-11-05 | 2016-03-23 | 上海毕得医药科技有限公司 | 一种1h-吲唑类衍生物的制备方法 |
| WO2014091352A1 (en) | 2012-12-11 | 2014-06-19 | Pfizer Inc. | Hexahydropyrano [3,4-d][1,3]thiazin-2-amine compounds as inhibitors of bace1 |
| CA2893333C (en) | 2012-12-19 | 2017-10-24 | Pfizer Inc. | Carbocyclic-and heterocyclic-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| WO2014125394A1 (en) | 2013-02-13 | 2014-08-21 | Pfizer Inc. | HETEROARYL-SUBSTITUTED HEXAHYDROPYRANO [3,4-d][1,3] THIAZIN-2-AMINE COMPOUNDS |
| US9233981B1 (en) | 2013-02-15 | 2016-01-12 | Pfizer Inc. | Substituted phenyl hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| BR112016004118A2 (pt) | 2013-09-12 | 2017-10-17 | Pfizer | uso de inibidores da acetil-coa carboxilase para tratamento de acne vulgar |
| JP6348582B2 (ja) | 2013-10-09 | 2018-06-27 | ファイザー・インク | プロスタグランジンep3受容体の拮抗薬 |
| CA2927527C (en) | 2013-11-20 | 2021-06-01 | Sanwa Kagaku Kenkyusho Co., Ltd. | Novel 3-azabicyclo[3.1.0]hexane derivative and use thereof as u-opioid receptor antagonist |
| CN103910682B (zh) * | 2013-11-28 | 2016-03-02 | 大连理工大学 | 一种基于邻苯二胺环化的苯并咪唑类化合物制备方法 |
| EP3119757B1 (en) | 2014-03-17 | 2018-05-16 | Pfizer Inc | Diacylglycerol acyltransferase 2 inhibitors for use in the treatment of metabolic and related disorders |
| WO2015150995A1 (en) | 2014-04-04 | 2015-10-08 | Pfizer Inc. | Bicyclic-fused heteroaryl or aryl compounds and their use as irak4 inhibitors |
| CR20160455A (es) | 2014-04-10 | 2016-12-16 | Pfizer | 2-AMINO-6-METIL-4,4a,5,6-TETRAHIDROPIRANO[3,4-d][1,3]TIAZIN-8a(8H)-IL-1,3-TIAZOL-4-ILA |
| WO2016092413A1 (en) | 2014-12-10 | 2016-06-16 | Pfizer Inc. | Indole and indazole compounds that activate ampk |
| EP3237401B1 (en) | 2014-12-22 | 2019-03-06 | Pfizer Inc | Antagonists of prostaglandin ep3 receptor |
| MA42035A (fr) | 2015-05-05 | 2018-03-14 | Pfizer | 2-thiopyrimidinones |
| US10308615B2 (en) | 2015-05-29 | 2019-06-04 | Pfizer Inc. | Heterocyclic compounds as inhibitors of Vanin-1 enzyme |
| ES2832893T3 (es) | 2015-06-17 | 2021-06-11 | Pfizer | Compuestos tricíclicos y su uso como inhibidores de la fosfodiesterasa |
| WO2016203335A1 (en) | 2015-06-18 | 2016-12-22 | Pfizer Inc. | Novel pyrido[2,3-b]pyrazinones as bet-family bromodomain inhibitors |
| AU2016305590A1 (en) | 2015-08-13 | 2018-02-15 | Pfizer Inc. | Bicyclic-fused heteroaryl or aryl compounds |
| RS61719B1 (sr) | 2015-08-27 | 2021-05-31 | Pfizer | Biciklična fuzionisana hetaroaril ili aril jedinjenja kao modulatori irak4 |
| WO2017037567A1 (en) | 2015-09-03 | 2017-03-09 | Pfizer Inc. | Regulators of frataxin |
| EP3353174A1 (en) | 2015-09-24 | 2018-08-01 | Pfizer Inc | N-[2-(3-amino-2,5-dimethyl-1,1-dioxido-5,6-dihydro-2h-1,2,4-thiadiazin-5-yl)-1,3-thiazol-4-yl]amides useful as bace inhibitors |
| WO2017051276A1 (en) | 2015-09-24 | 2017-03-30 | Pfizer Inc. | N-[2-(2-amino-6,6-disubstituted-4, 4a, 5, 6-tetrahydropyrano [3,4-d][1,3] thiazin-8a (8h)-yl) -1, 3-thiazol-4-yl] amides |
| JP2018531924A (ja) | 2015-09-24 | 2018-11-01 | ファイザー・インク | テトラヒドロピラノ[3,4−d][1,3]オキサジン誘導体、およびbace阻害剤としてのその使用 |
| JP6503515B2 (ja) | 2015-12-29 | 2019-04-17 | ファイザー・インク | ケトヘキソキナーゼ阻害薬としての置換3−アザビシクロ[3.1.0]ヘキサン |
| MX2019000536A (es) | 2016-07-14 | 2019-04-01 | Pfizer | Nuevas pirimidinas carboxamidas como inhibidores de enzima vanina-1. |
| AR109179A1 (es) | 2016-08-19 | 2018-11-07 | Pfizer | Inhibidores de diacilglicerol aciltransferasa 2 |
| JP6803410B2 (ja) * | 2017-02-14 | 2020-12-23 | 富士フイルム株式会社 | インダゾール化合物の製造方法およびインダゾール化合物 |
| WO2019133445A1 (en) | 2017-12-28 | 2019-07-04 | Inception Ibd, Inc. | Aminothiazoles as inhibitors of vanin-1 |
| BR112021003039A2 (pt) | 2018-08-31 | 2021-05-18 | Pfizer Inc. | combinações para o tratamento de nash/nafld e doenças relacionadas |
| WO2020102575A1 (en) | 2018-11-16 | 2020-05-22 | Inception Ibd, Inc. | Heterocyclic aminothiazoles and uses thereof |
| US12611401B2 (en) | 2019-05-20 | 2026-04-28 | Pfizer Inc. | Combinations comprising benzodioxol as GLP-1R agonists for use in the treatment of NASH/NAFLD and related diseases |
| CN110734401A (zh) * | 2019-10-10 | 2020-01-31 | 长沙麓兴生物科技有限公司 | 一种氮未取代-4-甲酰基吡唑的制备方法 |
| PE20231066A1 (es) | 2020-02-07 | 2023-07-17 | Gasherbrum Bio Inc | Agonistas heterociclicos de glp-1 |
| CN111574530B (zh) * | 2020-04-21 | 2022-07-26 | 徐州医科大学 | 一种acc抑制剂及其医药用途 |
| EP4143183B1 (en) | 2020-04-29 | 2025-10-22 | Gasherbrum Bio, Inc. | Heterocyclic glp-1 agonists |
| WO2021259203A1 (zh) * | 2020-06-22 | 2021-12-30 | 正大天晴药业集团股份有限公司 | 一种cdk4/6抑制剂的制备方法 |
| CN112625030A (zh) * | 2020-12-25 | 2021-04-09 | 杭州澳赛诺生物科技有限公司 | 一种一锅法合成n-保护3-溴代吡唑的合成方法 |
| JP2025509281A (ja) | 2022-03-09 | 2025-04-11 | ガシャーブラム・バイオ・インコーポレイテッド | ヘテロ環式glp-1アゴニスト |
| EP4508047A1 (en) | 2022-04-14 | 2025-02-19 | Gasherbrum Bio, Inc. | Heterocyclic glp-1 agonists |
| CN120019059A (zh) * | 2022-07-29 | 2025-05-16 | 辉瑞公司 | 新型acc抑制剂 |
| WO2024118524A1 (en) | 2022-11-28 | 2024-06-06 | Cerevel Therapeutics, Llc | Azaindole compounds and their use as phosphodiesterase inhibitors |
| KR20250157491A (ko) | 2022-12-15 | 2025-11-04 | 가셔브룸 바이오, 인크. | Glp-1 효능제 활성을 갖는 화합물의 염 및 고체 형태 |
| EP4634162A1 (en) | 2022-12-16 | 2025-10-22 | Syngenta Crop Protection AG | Benzimidazole derivatives |
| WO2025036472A1 (en) * | 2023-08-16 | 2025-02-20 | Pharmaengine, Inc. | Spirocyclic mta-cooperative prmts inhibitor |
| WO2025133948A1 (en) | 2023-12-21 | 2025-06-26 | Pfizer Inc. | Acetyl coa-carboxylase (acc) inhibitors |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ534582A (en) | 2002-02-27 | 2006-03-31 | Pfizer Prod Inc | ACC inhibitors |
| US7105526B2 (en) | 2002-06-28 | 2006-09-12 | Banyu Pharmaceuticals Co., Ltd. | Benzimidazole derivatives |
| JPWO2004092179A1 (ja) | 2003-04-14 | 2006-07-06 | 日本曹達株式会社 | スピロ誘導体、製造法および抗酸化薬 |
| JP2005119987A (ja) | 2003-10-15 | 2005-05-12 | Ajinomoto Co Inc | アシルスルホンアミド誘導体 |
| WO2005113069A2 (en) | 2004-05-14 | 2005-12-01 | Research Development Foundation | Use of circumin and analogues as inhibitors of acc2 |
| KR20080036041A (ko) | 2005-07-19 | 2008-04-24 | 머크 앤드 캄파니 인코포레이티드 | 아세틸 조효소 카복실라제(acc) 억제제로서의스피로크로마논 유도체 |
| WO2007013691A1 (ja) | 2005-07-29 | 2007-02-01 | Takeda Pharmaceutical Company Limited | スピロ環化合物 |
| DE102006016566B4 (de) * | 2005-09-22 | 2008-06-12 | Beru Ag | Zusammengesetzter Leiter, insbesondere für Glühkerzen für Dieselmotoren |
| US8071770B2 (en) | 2005-11-18 | 2011-12-06 | Merck Sharp & Dohme Corp. | Spirohydantoin aryl CGRP receptor antagonists |
| CN101384568B (zh) | 2006-02-15 | 2012-12-12 | 雅培制药有限公司 | 乙酰辅酶a羧化酶(acc)抑制剂及其在糖尿病、肥胖症和代谢综合征中的应用 |
| EP2097420B1 (en) | 2006-11-29 | 2012-04-04 | Pfizer Products Inc. | Spiroketone inhibitors of acetyl-coa carboxylase |
| PE20081559A1 (es) | 2007-01-12 | 2008-11-20 | Merck & Co Inc | DERIVADOS DE ESPIROCROMANONA SUSTITUIDOS COMO INHIBIDORES DE ACETIL CoA CARBOXILASA |
| JPWO2008102749A1 (ja) * | 2007-02-20 | 2010-05-27 | 武田薬品工業株式会社 | 複素環化合物 |
| CA2683695C (en) | 2007-04-12 | 2013-06-18 | Pfizer Inc. | 3-amido-pyrrolo[3,4-c]pyrazole-5(1h,4h,6h) carbaldehyde derivatives |
| US7981904B2 (en) * | 2008-03-20 | 2011-07-19 | Takeda Pharmaceutical Company Limited | Acetyl CoA carboxylase inhibitors |
| WO2009144554A1 (en) | 2008-05-28 | 2009-12-03 | Pfizer, Inc. | Pyrazolospiroketone acetyl-c0a carboxylase inhibitors |
| CA2724603A1 (en) | 2008-05-28 | 2009-12-03 | Pfizer Inc. | Pyrazolospiroketone acetyl-coa carboxylase inhibitors |
| US8524730B2 (en) | 2008-07-04 | 2013-09-03 | Msd K.K. | Spirochromanone carboxylic acids |
| WO2010008521A1 (en) * | 2008-07-14 | 2010-01-21 | Cropsolution, Inc. | Modulators of acetyl-coenzyme a carboxylase and methods of use thereof |
| PT2499139E (pt) | 2009-11-10 | 2014-02-10 | Pfizer | Inibidores de n1-pirazolospirocetona acetil-coa carboxilase |
| JP2013510191A (ja) | 2009-11-10 | 2013-03-21 | ファイザー・インク | N−2ピラゾロスピロケトンアセチル−CoAカルボキシラーゼ阻害薬 |
| HRP20161178T1 (hr) | 2010-09-30 | 2016-11-04 | Pfizer Inc. | N1-PIRAZOLOSPIROKETONSKI INHIBITORI ACETIL-CoA-KARBOKSILAZE |
-
2009
- 2009-05-18 WO PCT/IB2009/005649 patent/WO2009144554A1/en not_active Ceased
- 2009-05-18 CA CA2724774A patent/CA2724774C/en not_active Expired - Fee Related
- 2009-05-18 ES ES09754182.5T patent/ES2545231T3/es active Active
- 2009-05-18 EP EP09754182.5A patent/EP2297163B1/en not_active Not-in-force
- 2009-05-18 US US12/934,375 patent/US8318762B2/en active Active
- 2009-05-18 JP JP2011511101A patent/JP5435592B2/ja not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| JP5435592B2 (ja) | 2014-03-05 |
| US20110028390A1 (en) | 2011-02-03 |
| US8318762B2 (en) | 2012-11-27 |
| WO2009144554A1 (en) | 2009-12-03 |
| ES2545231T3 (es) | 2015-09-09 |
| CA2724774A1 (en) | 2009-12-03 |
| JP2011521939A (ja) | 2011-07-28 |
| EP2297163B1 (en) | 2015-07-08 |
| EP2297163A1 (en) | 2011-03-23 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request | ||
| MKLA | Lapsed |
Effective date: 20220518 |