PE20121639A1 - Derivados de 3-hidroxi-5-arilizotiazol como moduladores de gpr40 - Google Patents
Derivados de 3-hidroxi-5-arilizotiazol como moduladores de gpr40Info
- Publication number
- PE20121639A1 PE20121639A1 PE2012000884A PE2012000884A PE20121639A1 PE 20121639 A1 PE20121639 A1 PE 20121639A1 PE 2012000884 A PE2012000884 A PE 2012000884A PE 2012000884 A PE2012000884 A PE 2012000884A PE 20121639 A1 PE20121639 A1 PE 20121639A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- arylizothiazole
- gpr40
- hydroxy
- halogen
- Prior art date
Links
- 102100026148 Free fatty acid receptor 1 Human genes 0.000 title abstract 2
- 101000912510 Homo sapiens Free fatty acid receptor 1 Proteins 0.000 title abstract 2
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical group C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical group 0.000 abstract 3
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 abstract 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical group C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 102000004169 proteins and genes Human genes 0.000 abstract 1
- 108090000623 proteins and genes Proteins 0.000 abstract 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Chemical group COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 abstract 1
- 102000005962 receptors Human genes 0.000 abstract 1
- 108020003175 receptors Proteins 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D275/00—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings
- C07D275/02—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings not condensed with other rings
- C07D275/03—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
REFERIDA A UN DERIVADO DE 3-HIDROXI-5-ARILIZOTIAZOL DE FORMULA (I), DONDE n Y k SON UN ENTERO DE 0 A 2; p ES UN ENTERO DE 0 A 4; j ES UN ENTERO DE 0 A 3; EL ANILLO A ES UN GRUPO ARILO C6-C14 O UN HETEROCICLO DE 3 A 14 MIEMBROS, OPCIONALMENTE SUSTITUIDOS CON L; EL ANILLO B ES BENCENO, PIRIDINA O PIRIMIDINA; X ES O, S, NR7; R1 ES HALOGENO, ALQUILO C1-C6, ALQUENILO C2-C6, ENTRE OTROS; R2 ES H, HALOGENO, ALQUILO C1-C6, ENTRE OTROS; R3, R4, R5, R6 Y R7 SON H, ALQUILO C1-C6, ALQUENILO C2-C6, ENTRE OTROS; L ES HALOGENO, OH, CN, ALQUILO C1-C10, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS MODULAN LA FUNCION DEL RECEPTOR 40 ACOPLADO A LA PROTEINA G (GPR40) Y SON UTILES EN EL TRATAMIENTO DE TRASTORNOS TALES COMO LA DIABETES
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2009295855 | 2009-12-25 | ||
| JP2010043420 | 2010-02-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20121639A1 true PE20121639A1 (es) | 2012-12-02 |
Family
ID=44195895
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2012000884A PE20121639A1 (es) | 2009-12-25 | 2010-12-24 | Derivados de 3-hidroxi-5-arilizotiazol como moduladores de gpr40 |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US8476287B2 (es) |
| EP (1) | EP2518060A4 (es) |
| JP (2) | JP5002077B2 (es) |
| KR (1) | KR20130004262A (es) |
| CN (2) | CN104710381A (es) |
| AU (1) | AU2010336225A1 (es) |
| BR (1) | BR112012015612A2 (es) |
| CA (1) | CA2785674A1 (es) |
| CL (1) | CL2012001722A1 (es) |
| CO (1) | CO6650337A2 (es) |
| CR (1) | CR20120345A (es) |
| EA (1) | EA201290574A1 (es) |
| EC (1) | ECSP12012056A (es) |
| GT (1) | GT201200217A (es) |
| HN (1) | HN2012001351A (es) |
| IL (1) | IL220616A0 (es) |
| MA (1) | MA33952B1 (es) |
| MX (1) | MX2012007474A (es) |
| NI (1) | NI201200113A (es) |
| NZ (1) | NZ601408A (es) |
| PE (1) | PE20121639A1 (es) |
| PH (1) | PH12012501456A1 (es) |
| RU (1) | RU2567755C2 (es) |
| SG (1) | SG181961A1 (es) |
| WO (1) | WO2011078371A1 (es) |
| ZA (1) | ZA201203416B (es) |
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| JPWO2011052756A1 (ja) | 2009-10-30 | 2013-03-21 | 持田製薬株式会社 | 新規３−ヒドロキシ−５−アリールイソキサゾール誘導体 |
| PH12012501456A1 (en) | 2009-12-25 | 2012-10-29 | Mochida Pharm Co Ltd | Novel 3-hydroxy -5- arylisothiazole derivative |
| US8581584B2 (en) * | 2010-05-26 | 2013-11-12 | Florida State University Research Foundation | Membrane proteins, mechanisms of action and uses thereof |
| JP5809157B2 (ja) | 2010-10-08 | 2015-11-10 | 持田製薬株式会社 | 環状アミド誘導体 |
| MX348131B (es) | 2011-02-25 | 2017-05-26 | Merck Sharp & Dohme | Novedosos derivados de azabencimidazol ciclico utiles como agentes antidiabeticos. |
| TW201247636A (en) | 2011-04-27 | 2012-12-01 | Mochida Pharm Co Ltd | Novel 3-hydroxyisothiazole 1-oxide derivatives |
| EP2716636A4 (en) | 2011-04-28 | 2014-11-26 | Mochida Pharm Co Ltd | CYCLIC AMIDE DERIVATIVE |
| WO2013154163A1 (ja) * | 2012-04-11 | 2013-10-17 | 持田製薬株式会社 | 新規５－アリール－１，２－チアジナン誘導体 |
| SI3459942T1 (sl) | 2012-04-24 | 2021-05-31 | Vertex Pharmaceuticals Incorporated | Inhibitorji DNA-PK |
| HK1210825A1 (en) | 2012-07-11 | 2016-05-06 | Elcelyx Therapeutics, Inc. | Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk |
| WO2014022528A1 (en) | 2012-08-02 | 2014-02-06 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| WO2014130608A1 (en) | 2013-02-22 | 2014-08-28 | Merck Sharp & Dohme Corp. | Antidiabetic bicyclic compounds |
| HUE041544T2 (hu) | 2013-03-12 | 2019-05-28 | Vertex Pharma | DNS-PK inhibitorok |
| WO2014139388A1 (en) | 2013-03-14 | 2014-09-18 | Merck Sharp & Dohme Corp. | Novel indole derivatives useful as anti-diabetic agents |
| WO2015051496A1 (en) | 2013-10-08 | 2015-04-16 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| PT3424920T (pt) | 2013-10-17 | 2020-07-07 | Vertex Pharma | Co-cristais de (s)-n-metil-8-(1-((2'-metil-[4,5'-bipirimidin]-6-il)amino)propan-2-il)quinolina-4-carboxamida e derivados deuterados dos mesmos como inibidores de adn-pk |
| EP3068788A1 (en) | 2013-11-14 | 2016-09-21 | Cadila Healthcare Limited | Novel heterocyclic compounds |
| WO2016137506A1 (en) * | 2015-02-27 | 2016-09-01 | Nantbioscience, Inc. | Pyrimidine derivatives as kinase inhibitors and their therapeutical applications |
| JP6616244B2 (ja) * | 2015-05-29 | 2019-12-04 | 北興化学工業株式会社 | 新規なヒドロキシフェニルボロン酸エステルとその製造方法、およびヒドロキシビフェニル化合物の製造法 |
| JP2019529475A (ja) | 2016-09-27 | 2019-10-17 | バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ | Ｄｎａ損傷剤とｄｎａ−ｐｋ阻害剤との組合せ物を使用する、がんを処置するための方法 |
| US11072602B2 (en) | 2016-12-06 | 2021-07-27 | Merck Sharp & Dohme Corp. | Antidiabetic heterocyclic compounds |
| EP3558298B1 (en) | 2016-12-20 | 2026-03-11 | Merck Sharp & Dohme LLC | Antidiabetic spirochroman compounds |
| BR102018007822A2 (pt) | 2017-04-20 | 2018-11-06 | Gilead Sciences, Inc. | composto, métodos para inibir pd-1, pd-l1 e/ou interação de pd-1/pd-l1 e para tratamento de câncer, composição farmacêutica, e, kit para tratamento de ou prevenção de câncer ou uma doença ou condição |
| KR102708681B1 (ko) | 2018-02-13 | 2024-09-26 | 길리애드 사이언시즈, 인코포레이티드 | Pd-1/pd-l1 억제제 |
| EP4600247A3 (en) | 2018-04-19 | 2025-11-19 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| UA126421C2 (uk) | 2018-07-13 | 2022-09-28 | Гіліад Сайєнсіз, Інк. | Інгібітори pd-1/pd-l1 |
| US11236085B2 (en) | 2018-10-24 | 2022-02-01 | Gilead Sciences, Inc. | PD-1/PD-L1 inhibitors |
| CN110066254B (zh) * | 2018-11-16 | 2021-03-19 | 温州大学 | 一种异噻唑-3-酮化合物的制备方法 |
| BR112022006546A2 (pt) | 2019-10-07 | 2022-08-30 | Kallyope Inc | Agonistas de gpr119 |
| CA3173731A1 (en) | 2020-02-28 | 2021-09-02 | Kallyope, Inc. | Gpr40 agonists |
| CN116323608A (zh) | 2020-05-19 | 2023-06-23 | 卡尔优普公司 | Ampk活化剂 |
| EP4172162A4 (en) | 2020-06-26 | 2024-08-07 | Kallyope, Inc. | AMPK ACTIVATORS |
| CN115433143B (zh) * | 2021-06-03 | 2023-10-13 | 中国科学院大连化学物理研究所 | 一种异噻唑啉酮类化合物的合成方法 |
| CN115386028B (zh) * | 2022-08-26 | 2023-06-23 | 长春理工大学 | 一种聚合度可控的聚山梨酸-d-薄荷醇酯及合成方法与应用 |
| CN117510431A (zh) * | 2023-11-08 | 2024-02-06 | 浙江雅辰药物科技股份有限公司 | 一种异噻唑-3-酮及其衍生物、合成方法 |
| WO2025140655A1 (en) * | 2023-12-30 | 2025-07-03 | Fujian Haixi Pharmaceuticals Co., Ltd. | Heteroaryl compounds as multi-target protein kinase inhibitors |
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-
2010
- 2010-12-24 PH PH1/2012/501456A patent/PH12012501456A1/en unknown
- 2010-12-24 MA MA35101A patent/MA33952B1/fr unknown
- 2010-12-24 WO PCT/JP2010/073464 patent/WO2011078371A1/ja not_active Ceased
- 2010-12-24 PE PE2012000884A patent/PE20121639A1/es not_active Application Discontinuation
- 2010-12-24 KR KR1020127019581A patent/KR20130004262A/ko not_active Withdrawn
- 2010-12-24 US US13/392,350 patent/US8476287B2/en not_active Expired - Fee Related
- 2010-12-24 RU RU2012131840/04A patent/RU2567755C2/ru not_active IP Right Cessation
- 2010-12-24 BR BR112012015612A patent/BR112012015612A2/pt not_active IP Right Cessation
- 2010-12-24 MX MX2012007474A patent/MX2012007474A/es active IP Right Grant
- 2010-12-24 CN CN201510033003.XA patent/CN104710381A/zh active Pending
- 2010-12-24 JP JP2011547676A patent/JP5002077B2/ja not_active Expired - Fee Related
- 2010-12-24 NZ NZ601408A patent/NZ601408A/en not_active IP Right Cessation
- 2010-12-24 SG SG2012047601A patent/SG181961A1/en unknown
- 2010-12-24 CA CA2785674A patent/CA2785674A1/en not_active Abandoned
- 2010-12-24 CN CN201080059173.0A patent/CN102712610B/zh not_active Expired - Fee Related
- 2010-12-24 EP EP10839599.7A patent/EP2518060A4/en not_active Withdrawn
- 2010-12-24 EA EA201290574A patent/EA201290574A1/ru unknown
- 2010-12-24 AU AU2010336225A patent/AU2010336225A1/en not_active Abandoned
-
2012
- 2012-05-10 ZA ZA2012/03416A patent/ZA201203416B/en unknown
- 2012-05-17 JP JP2012113868A patent/JP2012153726A/ja active Pending
- 2012-06-22 CL CL2012001722A patent/CL2012001722A1/es unknown
- 2012-06-24 IL IL220616A patent/IL220616A0/en unknown
- 2012-06-25 HN HN2012001351A patent/HN2012001351A/es unknown
- 2012-06-25 CR CR20120345A patent/CR20120345A/es unknown
- 2012-06-25 CO CO12106432A patent/CO6650337A2/es not_active Application Discontinuation
- 2012-06-25 GT GT201200217A patent/GT201200217A/es unknown
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- 2012-07-23 EC ECSP12012056 patent/ECSP12012056A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN102712610B (zh) | 2015-03-04 |
| BR112012015612A2 (pt) | 2016-03-15 |
| RU2012131840A (ru) | 2014-01-27 |
| GT201200217A (es) | 2014-02-10 |
| EP2518060A4 (en) | 2014-01-08 |
| CN102712610A (zh) | 2012-10-03 |
| JPWO2011078371A1 (ja) | 2013-05-09 |
| PH12012501456A1 (en) | 2012-10-29 |
| ZA201203416B (en) | 2013-08-28 |
| IL220616A0 (en) | 2012-08-30 |
| CA2785674A1 (en) | 2011-06-30 |
| NZ601408A (en) | 2013-12-20 |
| MA33952B1 (fr) | 2013-01-02 |
| JP5002077B2 (ja) | 2012-08-15 |
| SG181961A1 (en) | 2012-08-30 |
| WO2011078371A1 (ja) | 2011-06-30 |
| CL2012001722A1 (es) | 2012-12-14 |
| ECSP12012056A (es) | 2012-10-30 |
| US8476287B2 (en) | 2013-07-02 |
| CO6650337A2 (es) | 2013-04-15 |
| CN104710381A (zh) | 2015-06-17 |
| KR20130004262A (ko) | 2013-01-09 |
| CR20120345A (es) | 2012-11-01 |
| RU2567755C2 (ru) | 2015-11-10 |
| EP2518060A1 (en) | 2012-10-31 |
| US20120157459A1 (en) | 2012-06-21 |
| EA201290574A1 (ru) | 2012-12-28 |
| NI201200113A (es) | 2012-08-13 |
| HN2012001351A (es) | 2015-03-23 |
| MX2012007474A (es) | 2012-08-01 |
| AU2010336225A1 (en) | 2012-08-16 |
| JP2012153726A (ja) | 2012-08-16 |
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