PE20141578A1 - Derivados de [1,2,3]triazolo[4,5-d]pirimidina como agonistas del receptor de canabinoides 2 - Google Patents

Derivados de [1,2,3]triazolo[4,5-d]pirimidina como agonistas del receptor de canabinoides 2

Info

Publication number
PE20141578A1
PE20141578A1 PE2014000737A PE2014000737A PE20141578A1 PE 20141578 A1 PE20141578 A1 PE 20141578A1 PE 2014000737 A PE2014000737 A PE 2014000737A PE 2014000737 A PE2014000737 A PE 2014000737A PE 20141578 A1 PE20141578 A1 PE 20141578A1
Authority
PE
Peru
Prior art keywords
triazolo
pyrimidine
alkyl
canabinoid
derivatives
Prior art date
Application number
PE2014000737A
Other languages
English (en)
Inventor
Caterina Bissantz
Uwe Grether
Atsushi Kimbara
Matthias Nettekoven
Stephan Roever
Mark Rogers-Evans
Original Assignee
Hoffmann La Roche
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20141578A1 publication Critical patent/PE20141578A1/es

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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
    • 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
    • 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
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • 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
    • A61K9/0012—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
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • 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
    • 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/10—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

Abstract

SE REFIERE A COMPUESTOS DE FORMULA (I), EN DONDE: A ES ALQUILENO, HIDROXIALQUILENO, -C(O)-, ENTRE OTROS; R1 ES H, ALQUILO, HALOALQUILO, HIDROXILO, ENTRE OTROS; R2 ES ALQUILO, HALOALQUILO, HIDROXIALQUILO, ALCOXIALQUILO, ENTRE OTROS; R3 ES HALOGENO O -NR4R5, DONDE UNO DE R4 Y R5 ES H O ALQUILO Y EL OTRO ES ALQUILO O CICLOALQUILO; O R4 Y R5 JUNTO CON EL ATOMO DE NITROGENO AL QUE ESTAN UNIDOS FORMAN UN HETEROCICLILO O HETEROCICLILO SUSTITUIDO. SON COMPUESTO PREFERIDOS: 5-TERT-BUTIL-2-(2-CLORO-BENCIL)-7-MORFOLIN-4-IL-2H-[1,2,3]-TRIAZOLO[4,5-d]PIRIMIDINA; 5-TERT-BUTIL-2-(2-CLORO-4-FLUOR-BENCIL)-7-MORFOLIN-4-IL-2H-[1,2,3]-TRIAZOLO[4,5-d]PIRIMIDINA; ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCESO DE OBTENCION DE LA FORMULA (I) Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON UTILES PARA EL TRATAMIENTO DE ATEROSCLEROSIS, GLAUCOMA, DIABETES MELLITUS, APOPLEJIA
PE2014000737A 2011-11-25 2012-11-22 Derivados de [1,2,3]triazolo[4,5-d]pirimidina como agonistas del receptor de canabinoides 2 PE20141578A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP11190777 2011-11-25

Publications (1)

Publication Number Publication Date
PE20141578A1 true PE20141578A1 (es) 2014-10-25

Family

ID=47278275

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2014000737A PE20141578A1 (es) 2011-11-25 2012-11-22 Derivados de [1,2,3]triazolo[4,5-d]pirimidina como agonistas del receptor de canabinoides 2

Country Status (31)

Country Link
US (1) US9067943B2 (es)
EP (1) EP2782915B1 (es)
JP (1) JP6077558B2 (es)
KR (1) KR20140097201A (es)
CN (1) CN104039791B (es)
AR (1) AR088970A1 (es)
AU (1) AU2012342471B2 (es)
BR (1) BR112014012479A2 (es)
CA (1) CA2850697A1 (es)
CL (1) CL2014001309A1 (es)
CO (1) CO6930360A2 (es)
CR (1) CR20140222A (es)
CY (1) CY1116984T1 (es)
DK (1) DK2782915T3 (es)
EA (1) EA024108B1 (es)
ES (1) ES2550967T3 (es)
HR (1) HRP20151423T1 (es)
HU (1) HUE028020T2 (es)
IL (1) IL232304A (es)
MA (1) MA35663B1 (es)
MX (1) MX346248B (es)
PE (1) PE20141578A1 (es)
PL (1) PL2782915T3 (es)
PT (1) PT2782915E (es)
RS (1) RS54319B1 (es)
SG (1) SG11201402198XA (es)
SI (1) SI2782915T1 (es)
TW (1) TWI598350B (es)
UA (1) UA111643C2 (es)
WO (1) WO2013076182A1 (es)
ZA (1) ZA201403441B (es)

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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
CA2915766C (en) * 2013-09-06 2023-09-26 F. Hoffmann-La Roche Ag Triazolo[4,5-d]pyrimidine derivatives and their use as cannabinoid receptor 2 agonists
CA2960794A1 (en) * 2014-11-07 2016-05-12 F. Hoffmann-La Roche Ag Triazolo[4,5-d]pyrimidines as agonists of the cannabinoid receptor 2
WO2017004133A1 (en) * 2015-06-29 2017-01-05 Nimbus Iris, Inc. Irak inhibitors and uses thereof
EP3475280B1 (en) * 2016-06-23 2020-04-08 H. Hoffnabb-La Roche Ag Novel [1,2,3]triazolo[4,5-d]pyrimidine derivatives
JP6964099B2 (ja) * 2016-06-23 2021-11-10 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft 新規［１，２，３］トリアゾロ［４，５−ｄ］ピリミジン誘導体
JP7090036B2 (ja) * 2016-06-23 2022-06-23 エフ．ホフマン－ラ ロシュ アーゲー 新規な［１，２，３］トリアゾロ［４，５－ｄ］ピリミジン誘導体
WO2017220517A1 (en) * 2016-06-23 2017-12-28 F. Hoffmann-La Roche Ag [1,2,3]triazolo[4,5-d]pyrimidine derivatives with affinity for the type-2 cannabinoid receptor
AU2019263682A1 (en) * 2018-05-04 2020-11-19 Inflazome Limited Novel compounds
CN112007156A (zh) * 2019-05-30 2020-12-01 复旦大学 大麻素受体药物在制备治疗心肌细胞坏死性凋亡药剂中的应用
CN112755189A (zh) * 2019-11-02 2021-05-07 复旦大学 1型大麻素受体拮抗剂在制备治疗心肌细胞焦亡药剂中的应用
AR127456A1 (es) * 2021-10-28 2024-01-24 Hoffmann La Roche Sintesis de [1,2,3]triazol[4,5-d]pirimidinas
CN115246832A (zh) * 2022-06-15 2022-10-28 深圳湾实验室 一类去泛素化酶usp25和usp28靶向抑制剂及制备和应用

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Publication number Publication date
BR112014012479A2 (pt) 2017-06-06
NZ622847A (en) 2015-05-29
CY1116984T1 (el) 2017-04-05
ES2550967T3 (es) 2015-11-13
EP2782915B1 (en) 2015-09-30
DK2782915T3 (en) 2015-10-19
EA201491002A1 (ru) 2014-09-30
IL232304A (en) 2016-02-29
CL2014001309A1 (es) 2014-10-17
AU2012342471B2 (en) 2017-06-08
CN104039791A (zh) 2014-09-10
CO6930360A2 (es) 2014-04-28
TWI598350B (zh) 2017-09-11
SG11201402198XA (en) 2014-09-26
US9067943B2 (en) 2015-06-30
MX346248B (es) 2017-03-13
CR20140222A (es) 2014-06-20
KR20140097201A (ko) 2014-08-06
CA2850697A1 (en) 2013-05-30
SI2782915T1 (sl) 2015-12-31
AR088970A1 (es) 2014-07-23
EP2782915A1 (en) 2014-10-01
HRP20151423T1 (hr) 2016-01-29
ZA201403441B (en) 2015-08-26
IL232304A0 (en) 2014-06-30
RS54319B1 (en) 2016-02-29
CN104039791B (zh) 2016-11-09
TW201329080A (zh) 2013-07-16
MA35663B1 (fr) 2014-11-01
PL2782915T3 (pl) 2016-03-31
US20130137676A1 (en) 2013-05-30
UA111643C2 (uk) 2016-05-25
JP2014533711A (ja) 2014-12-15
AU2012342471A1 (en) 2014-04-10
MX2014005692A (es) 2014-07-28
PT2782915E (pt) 2015-11-19
WO2013076182A1 (en) 2013-05-30
JP6077558B2 (ja) 2017-02-08
EA024108B1 (ru) 2016-08-31
HUE028020T2 (en) 2016-11-28

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