PE20141588A1 - Nuevos derivados de [1,2,3]triazolo[4,5-d]pirimidina como agonistas del receptor de canabinoides 2 - Google Patents
Nuevos derivados de [1,2,3]triazolo[4,5-d]pirimidina como agonistas del receptor de canabinoides 2Info
- Publication number
- PE20141588A1 PE20141588A1 PE2014000649A PE2014000649A PE20141588A1 PE 20141588 A1 PE20141588 A1 PE 20141588A1 PE 2014000649 A PE2014000649 A PE 2014000649A PE 2014000649 A PE2014000649 A PE 2014000649A PE 20141588 A1 PE20141588 A1 PE 20141588A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- triazolo
- pyrimidine
- compounds
- canabinoid
- Prior art date
Links
- GIIGHSIIKVOWKZ-UHFFFAOYSA-N 2h-triazolo[4,5-d]pyrimidine Chemical class N1=CN=CC2=NNN=C21 GIIGHSIIKVOWKZ-UHFFFAOYSA-N 0.000 title 1
- 239000000018 receptor agonist Substances 0.000 title 1
- 229940044601 receptor agonist Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- -1 2-CHLORO-BENZYL Chemical class 0.000 abstract 2
- OGYGFUAIIOPWQD-UHFFFAOYSA-N 1,3-thiazolidine Chemical compound C1CSCN1 OGYGFUAIIOPWQD-UHFFFAOYSA-N 0.000 abstract 1
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- 208000010412 Glaucoma Diseases 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical group 0.000 abstract 1
- TUJKJAMUKRIRHC-UHFFFAOYSA-N hydroxyl Chemical class [OH] TUJKJAMUKRIRHC-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 201000002793 renal fibrosis Diseases 0.000 abstract 1
Classifications
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- 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
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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
- A61K31/495—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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- A—HUMAN NECESSITIES
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- 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
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- 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
- C07D491/02—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 two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- 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)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurology (AREA)
- Dermatology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Ophthalmology & Optometry (AREA)
- Immunology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Physical Education & Sports Medicine (AREA)
- Urology & Nephrology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Hospice & Palliative Care (AREA)
- Pulmonology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Transplantation (AREA)
- Gastroenterology & Hepatology (AREA)
- Psychiatry (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
Abstract
SE REFIERE A COMPUESTOS DE FORMULA (I), EN DONDE: A ES ALQUILO, HIDROXIALQUILO, CH2C(O), C(O), SO2 O ESTA AUSENTE; R1 ES H, ALQUILO, HALOALQUILO, HIDROXILO, ALCOXI, ENTRE OTROS; R2 ES HALOGENO, NR3R4 O OR5; DONDE UNO DE R3 Y R4 ES H O ALQUILO Y EL OTRO ES ALQUILO O CICLOALQUILO; O R3 Y R4 JUNTO CON EL ATOMO DE N AL QUE ESTAN UNIDOS FORMAN UN HETEROCICLILO O HETEROCICLILO SUSTITUIDO; R5 ES ALQUILO, CICLOALQUILO, HALOALQUILO, ENTRE OTROS. SON COMPUESTO PREFERIDOS: 5-TERT-BUTIL-3-(2-CLORO-BENCIL)-7-MORFOLIN-4-IL-3H-[1,2,3]-TRIAZOLO[4,5-d]PIRIMIDINA; 3-(5-TERT-BUTIL-3-(2-CLOROBENCIL)-3H-[1,2,3]TRIAZOLO[4,5-d]PIRIMIDIN-7-IL)TIAZOLIDINA; ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCESO DE OBTENCION DE DICHOS COMPUESTOS Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON UTILES PARA EL TRATAMIENTO DE ATEROSCLEROSIS, GLAUCOMA, DIABETES MELLITUS, FIBROSIS RENAL
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11188333 | 2011-11-08 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20141588A1 true PE20141588A1 (es) | 2014-10-25 |
Family
ID=47116003
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2014000649A PE20141588A1 (es) | 2011-11-08 | 2012-11-05 | Nuevos derivados de [1,2,3]triazolo[4,5-d]pirimidina como agonistas del receptor de canabinoides 2 |
Country Status (31)
| Country | Link |
|---|---|
| US (2) | US8741906B2 (es) |
| EP (1) | EP2776442B1 (es) |
| JP (1) | JP6138141B2 (es) |
| KR (1) | KR102032337B1 (es) |
| CN (1) | CN103930426B (es) |
| AR (1) | AR088663A1 (es) |
| AU (1) | AU2012334173B2 (es) |
| BR (1) | BR112014011055B1 (es) |
| CA (1) | CA2850458C (es) |
| CL (1) | CL2014001174A1 (es) |
| CO (1) | CO6920295A2 (es) |
| CY (1) | CY1117147T1 (es) |
| DK (1) | DK2776442T3 (es) |
| EA (1) | EA023581B1 (es) |
| ES (1) | ES2553704T3 (es) |
| HR (1) | HRP20160052T1 (es) |
| HU (1) | HUE025543T2 (es) |
| IL (1) | IL231949A (es) |
| MX (1) | MX342309B (es) |
| MY (1) | MY170878A (es) |
| PE (1) | PE20141588A1 (es) |
| PH (1) | PH12014500813A1 (es) |
| PL (1) | PL2776442T3 (es) |
| PT (1) | PT2776442E (es) |
| RS (1) | RS54436B1 (es) |
| SG (1) | SG11201402197UA (es) |
| SI (1) | SI2776442T1 (es) |
| TW (2) | TWI704150B (es) |
| UA (1) | UA111640C2 (es) |
| WO (1) | WO2013068306A1 (es) |
| ZA (1) | ZA201402905B (es) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA111640C2 (uk) * | 2011-11-08 | 2016-05-25 | Ф. Хоффманн-Ля Рош Аг | ПОХІДНІ [1,2,3]ТРИАЗОЛО[4,5-d]ПІРИМІДИНУ ЯК АГОНІСТИ КАНАБІНОЇДНОГО РЕЦЕПТОРА 2 |
| US9067943B2 (en) * | 2011-11-25 | 2015-06-30 | Hoffmann-La Roche Inc. | [1,2,3]triazolo[4,5-D]pyrimidine derivatives |
| JP6514119B2 (ja) | 2013-03-07 | 2019-05-15 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | 新規ピラゾール誘導体 |
| NO2978755T3 (es) | 2013-03-26 | 2018-06-02 | ||
| PE20151977A1 (es) | 2013-05-02 | 2016-01-07 | Hoffmann La Roche | Nuevos derivados de purina |
| KR20160002857A (ko) | 2013-05-02 | 2016-01-08 | 에프. 호프만-라 로슈 아게 | CB2 수용체 작용제로서의 피롤로[2,3-d]피리미딘 유도체 |
| KR20220140651A (ko) * | 2013-09-06 | 2022-10-18 | 에프. 호프만-라 로슈 아게 | 신규의 트라이아졸로[4,5-d]피리미딘 유도체 |
| SG11201700777VA (en) | 2014-08-04 | 2017-02-27 | Nuevolution As | Optionally fused heterocyclyl-substituted derivatives of pyrimidine useful for the treatment of inflammatory, metabolic, oncologic and autoimmune diseases |
| JP6669743B2 (ja) * | 2014-11-07 | 2020-03-18 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | カンナビノイド受容体２のアゴニストとしてのトリアゾロ［４，５−ｄ］ピリミジン |
| CN107743491B (zh) * | 2015-05-08 | 2020-08-21 | 豪夫迈·罗氏有限公司 | 用于治疗和预防病毒感染的新的氧硫杂环戊烷甲酸及其衍生物 |
| CN105541738B (zh) * | 2016-01-21 | 2018-04-06 | 西北师范大学 | 一种三氮唑取代的苯乙酮类化合物的制备方法 |
| CN109311895B (zh) | 2016-06-23 | 2021-06-18 | 豪夫迈·罗氏有限公司 | 新型[1,2,3]三唑并[4,5-d]嘧啶衍生物 |
| EP3475280B1 (en) | 2016-06-23 | 2020-04-08 | H. Hoffnabb-La Roche Ag | Novel [1,2,3]triazolo[4,5-d]pyrimidine derivatives |
| WO2018015088A1 (en) | 2016-06-23 | 2018-01-25 | F. Hoffmann-La Roche Ag | Novel [1,2,31triazolo[4,5-d]pyrimidine derivatives |
| CN109348716A (zh) * | 2016-06-23 | 2019-02-15 | 豪夫迈·罗氏有限公司 | 对2型大麻素受体具有亲和力的[1,2,3]三唑并[4,5-d]嘧啶衍生物 |
| JP2021535202A (ja) * | 2018-08-20 | 2021-12-16 | ベッソール ファルマ、エルエルシー | 新規カンナビノイドおよびカンナビノイド酸ならびにそれらの誘導体 |
| ES3025805T3 (en) | 2019-05-13 | 2025-06-09 | Ecolab Usa Inc | 1,2,4-triazolo[1,5-a] pyrimidine derivative as copper corrosion inhibitor |
| EP4076657A1 (en) | 2019-12-20 | 2022-10-26 | Nuevolution A/S | Compounds active towards nuclear receptors |
| EP4076661A1 (en) | 2019-12-20 | 2022-10-26 | Nuevolution A/S | Compounds active towards nuclear receptors |
| EP4126875A1 (en) | 2020-03-31 | 2023-02-08 | Nuevolution A/S | Compounds active towards nuclear receptors |
| WO2021198955A1 (en) | 2020-03-31 | 2021-10-07 | Nuevolution A/S | Compounds active towards nuclear receptors |
| US20230279006A1 (en) * | 2020-07-08 | 2023-09-07 | Klotho Therapeutics, Inc. | Novel compounds and methods for increasing klotho gene expression |
| JP2023549973A (ja) * | 2020-11-23 | 2023-11-29 | エフ． ホフマン－ラ ロシュ アーゲー | テトラゾール誘導体の製造のための新規方法 |
| AR127456A1 (es) | 2021-10-28 | 2024-01-24 | Hoffmann La Roche | Sintesis de [1,2,3]triazol[4,5-d]pirimidinas |
| JP2025519497A (ja) | 2022-06-07 | 2025-06-26 | エフ． ホフマン－ラ ロシュ アーゲー | １－［５－ｔｅｒｔ－ブチル－３－［（１－メチルテトラゾール－５－イル）メチル］トリアゾロ［４，５－ｄ］ピリミジン－７－イル］ピロリジン－３－オールの製造方法 |
| JP2025531720A (ja) | 2022-09-01 | 2025-09-25 | エフ． ホフマン－ラ ロシュ アーゲー | 抗ｃｂ２抗体及び細胞表面ｃｂ２発現を測定するためのフローサイトメトリーアッセイにおけるそれらの使用 |
| JP2025530036A (ja) * | 2022-09-01 | 2025-09-10 | エフ． ホフマン－ラ ロシュ アーゲー | ビカシナビンの投与レジメン |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4076711A (en) * | 1976-04-05 | 1978-02-28 | Schering Corporation | Triazolo [4,5-d]-pyrimidines |
| US5204353A (en) * | 1987-04-07 | 1993-04-20 | Ciba-Geigy Corporation | 3-benzyl-3H-1,2,3-triazolo[4,5-d]pyrimidines, compositions thereof, and method of treating epilepsy therewith |
| HUT74464A (en) * | 1993-10-12 | 1996-12-30 | Du Pont Merck Pharma | 1n-alkyl-n-arylpyrimidinamines and derivatives thereof, and pharmaceutical compositions containing them |
| CN1142817A (zh) * | 1993-10-12 | 1997-02-12 | 杜邦麦克制药有限公司 | 1n-烷基-n-芳基嘧啶胺及其衍生物 |
| ATE554092T1 (de) | 2006-12-14 | 2012-05-15 | Bristol Myers Squibb Co | Azabicyclische heterocyclen als cannabinoid- rezeptormodulatoren |
| US7655685B2 (en) | 2007-11-02 | 2010-02-02 | Jenrin Discovery, Inc. | Cannabinoid receptor antagonists/inverse agonists useful for treating metabolic disorders, including obesity and diabetes |
| CA2709784A1 (en) | 2007-12-21 | 2009-07-09 | University Of Rochester | Method for altering the lifespan of eukaryotic organisms |
| US8598184B2 (en) * | 2008-03-03 | 2013-12-03 | Tiger Pharmatech | Protein kinase inhibitors |
| AR080711A1 (es) * | 2010-03-31 | 2012-05-02 | Lilly Co Eli | Compuesto de piperazin-purina composicion farmaceutica que lo comprende y su uso para preparar un medicamento util para el tratamiento o prevencion del dolor |
| UA111640C2 (uk) * | 2011-11-08 | 2016-05-25 | Ф. Хоффманн-Ля Рош Аг | ПОХІДНІ [1,2,3]ТРИАЗОЛО[4,5-d]ПІРИМІДИНУ ЯК АГОНІСТИ КАНАБІНОЇДНОГО РЕЦЕПТОРА 2 |
| US9067943B2 (en) * | 2011-11-25 | 2015-06-30 | Hoffmann-La Roche Inc. | [1,2,3]triazolo[4,5-D]pyrimidine derivatives |
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