PE20190109A1 - Nuevos derivados de [1,2,3]triazolo[4,5-d]pirimidina - Google Patents
Nuevos derivados de [1,2,3]triazolo[4,5-d]pirimidinaInfo
- Publication number
- PE20190109A1 PE20190109A1 PE2018003112A PE2018003112A PE20190109A1 PE 20190109 A1 PE20190109 A1 PE 20190109A1 PE 2018003112 A PE2018003112 A PE 2018003112A PE 2018003112 A PE2018003112 A PE 2018003112A PE 20190109 A1 PE20190109 A1 PE 20190109A1
- Authority
- PE
- Peru
- Prior art keywords
- triazolo
- pyrimidine
- compound
- ring
- new derivatives
- 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 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- KRHYYFGTRYWZRS-UHFFFAOYSA-M Fluoride anion Chemical compound [F-] KRHYYFGTRYWZRS-UHFFFAOYSA-M 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- -1 benzene-1-sulfonyl Chemical group 0.000 abstract 1
- 229930003827 cannabinoid Natural products 0.000 abstract 1
- 239000003557 cannabinoid Substances 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 208000004296 neuralgia Diseases 0.000 abstract 1
- 208000021722 neuropathic pain Diseases 0.000 abstract 1
- 125000001715 oxadiazolyl group Chemical group 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- PXQLVRUNWNTZOS-UHFFFAOYSA-N sulfanyl Chemical group [SH] PXQLVRUNWNTZOS-UHFFFAOYSA-N 0.000 abstract 1
- 238000011282 treatment Methods 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
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- G—PHYSICS
- G01—MEASURING; TESTING
- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
- G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
- G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
- G01N33/94—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving narcotics or drugs or pharmaceuticals, neurotransmitters or associated receptors
- G01N33/948—Sedatives, e.g. cannabinoids, barbiturates
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- G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
- G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
- G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
- G01N2333/705—Assays involving receptors, cell surface antigens or cell surface determinants
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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- Health & Medical Sciences (AREA)
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- Life Sciences & Earth Sciences (AREA)
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- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
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- General Chemical & Material Sciences (AREA)
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- Immunology (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Pulmonology (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Neurosurgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurology (AREA)
- Ophthalmology & Optometry (AREA)
- Molecular Biology (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Obesity (AREA)
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Abstract
Referido a derivados [1,2,3]triazolo[4,5-d]pirimidina de formula (I) con afinidad para el receptor de cannabinoide de tipo 2 (CB2); en donde R1 es un anillo seleccionado de entre fenilo y [1,2,5] oxadiazolilo, en el que dicho anillo se sustituye con un sustituyente seleccionado de entre halosulfonilo, halosulfonilalquilo, entre otros; R2 y R3 se seleccionan, independientemente, entre H, -OH, halogeno, tiohidroxilo, entre otros; R4 es alquilo o fenilhaloalquilo; y n es 0 o 1, o una sal o ester farmaceuticamente aceptable del mismo. Un compuesto seleccionado es fluoruro de 2-({5-terc-butil-7-[(3S)-3-hidroxipirrolidin-1-il]-3H-[1,2,3]triazolo[4,5-d]pirimidin-3-il}]metil)benceno-1-sulfonilo. Tambien se refiere a un procedimiento para la preparacion de dicho compuesto y su uso como medicamento en el tratamiento o profilaxis del dolor, dolor neuropatico, ateroesclerosis, entre otros
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16175924 | 2016-06-23 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20190109A1 true PE20190109A1 (es) | 2019-01-15 |
Family
ID=56203225
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2018003112A PE20190109A1 (es) | 2016-06-23 | 2017-06-20 | Nuevos derivados de [1,2,3]triazolo[4,5-d]pirimidina |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US10457685B2 (es) |
| EP (2) | EP4108665A1 (es) |
| JP (2) | JP6962942B2 (es) |
| KR (2) | KR20230062680A (es) |
| CN (4) | CN109348716A (es) |
| AR (1) | AR108845A1 (es) |
| AU (2) | AU2017283136C1 (es) |
| BR (1) | BR112018075143A2 (es) |
| CA (2) | CA3206921A1 (es) |
| CL (1) | CL2018003610A1 (es) |
| CO (1) | CO2018011231A2 (es) |
| CR (2) | CR20220661A (es) |
| IL (2) | IL292015B2 (es) |
| MA (1) | MA45442A (es) |
| MX (1) | MX2018014684A (es) |
| MY (1) | MY197244A (es) |
| PE (1) | PE20190109A1 (es) |
| PH (1) | PH12018502733B1 (es) |
| RU (1) | RU2741597C2 (es) |
| SG (2) | SG10202113286RA (es) |
| TW (2) | TWI824380B (es) |
| UA (1) | UA123834C2 (es) |
| WO (1) | WO2017220517A1 (es) |
| ZA (1) | ZA201807133B (es) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017220544A1 (en) | 2016-06-23 | 2017-12-28 | F. Hoffmann-La Roche Ag | Novel[1,2,3]triazolo[4,5-d]pyrimidine derivatives |
| WO2017220516A1 (en) | 2016-06-23 | 2017-12-28 | F. Hoffmann-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 |
| AU2021382384A1 (en) * | 2020-11-23 | 2023-03-23 | F. Hoffmann-La Roche Ag | New process for the manufacture of tetrazole derivatives |
| CN113387845B (zh) * | 2021-07-16 | 2022-12-20 | 国药集团化学试剂有限公司 | 一种苯甲基磺酰氟的制备方法 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1223929B1 (en) * | 1999-10-18 | 2006-08-23 | The University Of Connecticut | Cannabimimetic indole derivatives |
| WO2006051704A1 (ja) * | 2004-11-15 | 2006-05-18 | Taisho Pharmaceutical Co., Ltd. | イミン化合物 |
| MX2007012091A (es) | 2005-03-31 | 2007-11-20 | Schering Corp | Antagonistas espirociclicos de los receptores de trombina. |
| FR2887550A1 (fr) | 2005-06-24 | 2006-12-29 | Sanofi Aventis Sa | Derives de 1-benzylpyrazole-3-acetamide, leur preparation et leur application en therapeutique |
| CA2645967C (en) * | 2006-03-30 | 2011-05-24 | Irm Llc | Compounds and compositions as inhibitors of cannabinoid receptor 1 activity |
| JP5583694B2 (ja) * | 2009-01-05 | 2014-09-03 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Cb2受容体を調節するピロリジン化合物 |
| EP2311443A1 (en) | 2009-10-15 | 2011-04-20 | Rheinische Friedrich-Wilhelms-Universität | Pharmaceutical composition containing cannabinoid-receptor 2 antagonists |
| CN102924457A (zh) * | 2011-08-12 | 2013-02-13 | 上海恒瑞医药有限公司 | 三唑并嘧啶类衍生物、其制备方法及其用途 |
| 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 |
| PT2964646T (pt) | 2013-03-07 | 2017-06-29 | Hoffmann La Roche | Novos derivados de pirazol |
| AU2014261546B2 (en) * | 2013-05-02 | 2018-01-18 | F. Hoffmann-La Roche Ag | Pyrrolo[2,3-d]pyrimidine derivatives as CB2 receptor agonists |
| RS57461B1 (sr) | 2013-05-02 | 2018-09-28 | Hoffmann La Roche | Derivati purina kao agonisti cb2 receptora |
| MX391724B (es) | 2013-09-06 | 2025-03-21 | Hoffmann La Roche | Nuevos derivados de triazolo[4,5-d]pirimidina. |
| EA031735B1 (ru) | 2014-11-07 | 2019-02-28 | Ф. Хоффманн-Ля Рош Аг | ТРИАЗОЛО[4,5-d]ПИРИМИДИНЫ В КАЧЕСТВЕ АГОНИСТОВ КАННАБИНОИДНЫХ РЕЦЕПТОРОВ ТИПА 2 |
| WO2018015088A1 (en) | 2016-06-23 | 2018-01-25 | F. Hoffmann-La Roche Ag | Novel [1,2,31triazolo[4,5-d]pyrimidine derivatives |
| WO2017220516A1 (en) | 2016-06-23 | 2017-12-28 | F. Hoffmann-La Roche Ag | Novel [1,2,3]triazolo[4,5-d]pyrimidine derivatives |
| WO2017220544A1 (en) | 2016-06-23 | 2017-12-28 | F. Hoffmann-La Roche Ag | Novel[1,2,3]triazolo[4,5-d]pyrimidine derivatives |
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2017
- 2017-06-20 KR KR1020237014572A patent/KR20230062680A/ko active Pending
- 2017-06-20 BR BR112018075143-0A patent/BR112018075143A2/pt not_active Application Discontinuation
- 2017-06-20 CN CN201780036295.XA patent/CN109348716A/zh active Pending
- 2017-06-20 MX MX2018014684A patent/MX2018014684A/es unknown
- 2017-06-20 JP JP2018566249A patent/JP6962942B2/ja not_active Expired - Fee Related
- 2017-06-20 WO PCT/EP2017/064994 patent/WO2017220517A1/en not_active Ceased
- 2017-06-20 UA UAA201900294A patent/UA123834C2/uk unknown
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