AR078944A1 - Inhibidores de n1-pirazoloespirocetona acetil-coa carboxilasa - Google Patents
Inhibidores de n1-pirazoloespirocetona acetil-coa carboxilasaInfo
- Publication number
- AR078944A1 AR078944A1 ARP100104147A ARP100104147A AR078944A1 AR 078944 A1 AR078944 A1 AR 078944A1 AR P100104147 A ARP100104147 A AR P100104147A AR P100104147 A ARP100104147 A AR P100104147A AR 078944 A1 AR078944 A1 AR 078944A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- aryl
- coa carboxylase
- membered heteroaryl
- pirazoloespirocetona
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 4
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 2
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 125000001475 halogen functional group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000003566 oxetanyl group Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 1
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 1
- 102000000452 Acetyl-CoA carboxylase Human genes 0.000 abstract 1
- 108010016219 Acetyl-CoA carboxylase Proteins 0.000 abstract 1
- 108010018763 Biotin carboxylase Proteins 0.000 abstract 1
- -1 C1-3-dialkyl Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000003368 amide group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- AQYSYJUIMQTRMV-UHFFFAOYSA-N hypofluorous acid Chemical compound FO AQYSYJUIMQTRMV-UHFFFAOYSA-N 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- 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
- C07D471/10—Spiro-condensed systems
-
- 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
- A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring 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
-
- 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
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
-
- 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
- A61P9/12—Antihypertensives
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Cardiology (AREA)
- Immunology (AREA)
- Child & Adolescent Psychology (AREA)
- Gastroenterology & Hepatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Peptides Or Proteins (AREA)
Abstract
Composiciones farmacéuticas del mismo; y el uso del mismo en el tratamiento de enfermedades, afecciones o trastornos modulados por la inhibicion de una(s) enzima(s) acetil-CoA carboxilasa(s) en un animal. Reivindicacion 1: Un compuesto de formula (1) en la que R1 es alquilo C1-6, cicloalquilo C3-7, tetrahidrofuranilo u oxetanilo; en el que dicho alquilo C1-6 está opcionalmente sustituido con 1 a 2 sustituyentes seleccionados independientemente entre alcoxi C1-3, hidroxi, fluor, fenilo, tetrahidrofuranilo u oxetanilo; R2 es hidrogeno, halo, alquilo C1-3 o ciano; cada uno de R3 es independientemente hidrogeno o alquilo C1-3; R4 es un arilo C6-10, heteroarilo de 5 a 12 miembros o arilo heterocíclico condensado de 8 a 12miembros; en el que cada uno de dicho arilo C6-10, heteroarilo de 5 a 12 miembros o arilo heterocíclico condensado de 8 a 12 miembros está opcionalmente sustituido con uno a tres sustituyentes seleccionados independientemente entre alquilo C1-3, alcoxi C1-3, halo, amino, alquil C1-3-amino, dialquil C1-3-amino, hidroxi, ciano, amido, fenilo, heteroarilo de 5 a 6 miembros o heterociclilo de 5 a 6 miembros; o una sal farmacéuticamente aceptable del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US25982309P | 2009-11-10 | 2009-11-10 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR078944A1 true AR078944A1 (es) | 2011-12-14 |
Family
ID=43357094
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100104147A AR078944A1 (es) | 2009-11-10 | 2010-11-08 | Inhibidores de n1-pirazoloespirocetona acetil-coa carboxilasa |
Country Status (39)
| Country | Link |
|---|---|
| US (4) | US8288405B2 (es) |
| EP (3) | EP2947082A1 (es) |
| JP (1) | JP5114610B1 (es) |
| KR (2) | KR101478517B1 (es) |
| CN (1) | CN102695708B (es) |
| AP (1) | AP3283A (es) |
| AR (1) | AR078944A1 (es) |
| AU (1) | AU2010317501B2 (es) |
| BR (1) | BR112012011072A2 (es) |
| CA (1) | CA2778886C (es) |
| CL (1) | CL2012000999A1 (es) |
| CO (1) | CO6541569A2 (es) |
| CR (1) | CR20120190A (es) |
| CU (1) | CU24077B1 (es) |
| DK (1) | DK2499139T3 (es) |
| DO (1) | DOP2012000128A (es) |
| EA (1) | EA020153B1 (es) |
| EC (1) | ECSP12011880A (es) |
| ES (1) | ES2444543T3 (es) |
| GE (1) | GEP20146169B (es) |
| HN (1) | HN2012000973A (es) |
| HR (1) | HRP20140025T1 (es) |
| IL (1) | IL219373A (es) |
| MA (1) | MA33734B1 (es) |
| MX (1) | MX2012005429A (es) |
| NI (1) | NI201200089A (es) |
| NZ (1) | NZ599815A (es) |
| PE (1) | PE20121469A1 (es) |
| PH (1) | PH12012500903A1 (es) |
| PL (1) | PL2499139T3 (es) |
| PT (1) | PT2499139E (es) |
| RS (1) | RS53156B (es) |
| SI (1) | SI2499139T1 (es) |
| TN (1) | TN2012000192A1 (es) |
| TW (1) | TWI394756B (es) |
| UA (1) | UA102336C2 (es) |
| UY (1) | UY33020A (es) |
| WO (1) | WO2011058474A1 (es) |
| ZA (1) | ZA201204231B (es) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2297163B1 (en) | 2008-05-28 | 2015-07-08 | Pfizer Inc. | Pyrazolospiroketone acetyl-CoA carboxylase inhibitors |
| PE20120493A1 (es) | 2009-06-29 | 2012-05-20 | Incyte Corp | Pirimidinonas como inhibidores de pi3k |
| CA2778886C (en) | 2009-11-10 | 2014-01-07 | Pfizer Inc. | N1-pyrazolospiroketone acetyl-coa carboxylase inhibitors |
| US8759359B2 (en) | 2009-12-18 | 2014-06-24 | Incyte Corporation | Substituted heteroaryl fused derivatives as PI3K inhibitors |
| EP2345643A1 (en) * | 2009-12-29 | 2011-07-20 | Polichem S.A. | New tertiary 8-hydroxyquinoline-7-carboxamide derivatives and uses thereof |
| AR081823A1 (es) | 2010-04-14 | 2012-10-24 | Incyte Corp | DERIVADOS FUSIONADOS COMO INHIBIDORES DE PI3Kd |
| WO2011163195A1 (en) | 2010-06-21 | 2011-12-29 | Incyte Corporation | Fused pyrrole derivatives as pi3k inhibitors |
| PT2621493T (pt) | 2010-09-30 | 2016-11-14 | Pfizer | Inibidores de n1-pirazolospirocetona acetil-coa carboxilase |
| PL2632925T3 (pl) * | 2010-10-29 | 2015-10-30 | Pfizer | N1/N2-laktamowe inhibitory karboksylazy acetylo-CoA |
| ES2764848T3 (es) | 2010-12-20 | 2020-06-04 | Incyte Holdings Corp | N-(1-(fenilo sustituido)etilo)-9H-purina-6-aminas como inhibidores de PI3K |
| WO2012125629A1 (en) | 2011-03-14 | 2012-09-20 | Incyte Corporation | Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors |
| WO2012135009A1 (en) | 2011-03-25 | 2012-10-04 | Incyte Corporation | Pyrimidine-4,6-diamine derivatives as pi3k inhibitors |
| EA022375B1 (ru) * | 2011-04-22 | 2015-12-30 | Пфайзер Инк. | ПРОИЗВОДНЫЕ ПИРАЗОЛОСПИРОКЕТОНОВ ДЛЯ ПРИМЕНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ АЦЕТИЛ-КоА-КАРБОКСИЛАЗ |
| KR20230038593A (ko) | 2011-09-02 | 2023-03-20 | 인사이트 홀딩스 코포레이션 | Ｐｉ３ｋ 억제제로서 헤테로시클릴아민 |
| AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
| JP6423372B2 (ja) | 2013-02-28 | 2018-11-14 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | 強力なｒｏｃｋ１およびｒｏｃｋ２阻害剤としてのフェニルピラゾール誘導体 |
| AR094929A1 (es) | 2013-02-28 | 2015-09-09 | Bristol Myers Squibb Co | Derivados de fenilpirazol como inhibidores potentes de rock1 y rock2 |
| ES2731773T3 (es) | 2013-03-14 | 2019-11-19 | Celgene Quanticel Res Inc | Inhibidores de la histona desmetilasa |
| BR112016004118A2 (pt) | 2013-09-12 | 2017-10-17 | Pfizer | uso de inibidores da acetil-coa carboxilase para tratamento de acne vulgar |
| WO2015056782A1 (ja) | 2013-10-17 | 2015-04-23 | 塩野義製薬株式会社 | 新規アルキレン誘導体 |
| WO2015191677A1 (en) | 2014-06-11 | 2015-12-17 | Incyte Corporation | Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors |
| US9896436B2 (en) | 2014-09-16 | 2018-02-20 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| MX2017003464A (es) | 2014-09-16 | 2017-07-13 | Celgene Quanticel Res Inc | Inhibidores de histona desmetilasa. |
| US9758517B2 (en) * | 2014-09-17 | 2017-09-12 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| KR102411448B1 (ko) | 2014-11-10 | 2022-06-20 | 고쿠리츠다이가쿠호진 요코하마 고쿠리츠다이가쿠 | 산소 발생용 애노드 |
| PH12017501538B1 (en) | 2015-02-27 | 2024-02-14 | Incyte Holdings Corp | Salts of p13k inhibitor and processes for their preparation |
| US9988401B2 (en) | 2015-05-11 | 2018-06-05 | Incyte Corporation | Crystalline forms of a PI3K inhibitor |
| US9732097B2 (en) | 2015-05-11 | 2017-08-15 | Incyte Corporation | Process for the synthesis of a phosphoinositide 3-kinase inhibitor |
| AU2018291163B2 (en) | 2017-06-30 | 2024-07-18 | Quixgen, Inc. | Novel spirolactone compounds |
| HUE061885T2 (hu) | 2017-11-21 | 2023-08-28 | Pfizer | 4-(4-(4-(1-Izopropil-7-oxo-1,4,6,6,7-tetrahidrospiro[indazol-5,4'-piperidin] -1'-karbonil)-6-metoxipiridin-2-il)-benzoesav kristályos 2-amino-2-(hidroximetil)-propán-1,3-diol sója |
| WO2019178480A1 (en) * | 2018-03-15 | 2019-09-19 | Yale University | Pyrazole-containing macrophage migration inhibitory factor inhibitors |
| CN112469418A (zh) | 2018-06-01 | 2021-03-09 | 因赛特公司 | 治疗pi3k相关病症的给药方案 |
| CN115666558A (zh) | 2020-05-21 | 2023-01-31 | 盐野义制药株式会社 | 脂肪性肝病的治疗用药物 |
| US10989621B1 (en) | 2020-08-20 | 2021-04-27 | Trinity Bay Equipment Holdings, LLC | Online pipe integrity testing system and method |
| CN112028834B (zh) * | 2020-09-11 | 2022-03-29 | 济南悟通生物科技有限公司 | 一种阿贝西利的中间体的合成方法 |
| WO2023090411A1 (ja) | 2021-11-19 | 2023-05-25 | 塩野義製薬株式会社 | 心疾患または骨格筋の疾患の治療用医薬 |
| CN115124542A (zh) * | 2022-07-08 | 2022-09-30 | 河南师范大学 | 羟基苯取代吡唑酮并吲唑[螺]吡唑酮类化合物的合成方法 |
| CN120019059A (zh) * | 2022-07-29 | 2025-05-16 | 辉瑞公司 | 新型acc抑制剂 |
| WO2025133948A1 (en) * | 2023-12-21 | 2025-06-26 | Pfizer Inc. | Acetyl coa-carboxylase (acc) inhibitors |
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| US984083A (en) | 1910-03-28 | 1911-02-14 | William J Faber | Floor-plane. |
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| PE20081559A1 (es) * | 2007-01-12 | 2008-11-20 | Merck & Co Inc | DERIVADOS DE ESPIROCROMANONA SUSTITUIDOS COMO INHIBIDORES DE ACETIL CoA CARBOXILASA |
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| JP5404601B2 (ja) * | 2007-04-12 | 2014-02-05 | ファイザー・インク | 新規な３−アミド−ピロロ［３，４−ｃ］ピラゾール−５（１Ｈ，４Ｈ，６Ｈ）カルバルデヒド誘導体 |
| US20100211592A1 (en) * | 2007-07-20 | 2010-08-19 | Mark Jonathon Brownlee | Email response time expectation system |
| US7981904B2 (en) | 2008-03-20 | 2011-07-19 | Takeda Pharmaceutical Company Limited | Acetyl CoA carboxylase inhibitors |
| EP2297163B1 (en) * | 2008-05-28 | 2015-07-08 | Pfizer Inc. | Pyrazolospiroketone acetyl-CoA carboxylase inhibitors |
| EP2297164A1 (en) * | 2008-05-28 | 2011-03-23 | Pfizer Inc. | Pyrazolospiroketone acetyl-coa carboxylase inhibitors |
| WO2010002010A1 (en) | 2008-07-04 | 2010-01-07 | Banyu Pharmaceutical Co.,Ltd. | Novel spirochromanone carboxylic acids |
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| CA2778886C (en) * | 2009-11-10 | 2014-01-07 | Pfizer Inc. | N1-pyrazolospiroketone acetyl-coa carboxylase inhibitors |
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| PT2621493T (pt) * | 2010-09-30 | 2016-11-14 | Pfizer | Inibidores de n1-pirazolospirocetona acetil-coa carboxilase |
| EA022375B1 (ru) * | 2011-04-22 | 2015-12-30 | Пфайзер Инк. | ПРОИЗВОДНЫЕ ПИРАЗОЛОСПИРОКЕТОНОВ ДЛЯ ПРИМЕНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ АЦЕТИЛ-КоА-КАРБОКСИЛАЗ |
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2010
- 2010-10-29 CA CA2778886A patent/CA2778886C/en active Active
- 2010-10-29 KR KR1020127014916A patent/KR101478517B1/ko not_active Expired - Fee Related
- 2010-10-29 RS RS20140068A patent/RS53156B/sr unknown
- 2010-10-29 CN CN201080059647.1A patent/CN102695708B/zh not_active Expired - Fee Related
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