SG10202113286RA - [1,2,3]triazolo[4,5-d]pyrimidine derivatives with affinity for the type-2 cannabinoid receptor - Google Patents

[1,2,3]triazolo[4,5-d]pyrimidine derivatives with affinity for the type-2 cannabinoid receptor

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Publication number
SG10202113286RA
SG10202113286RA SG10202113286RA SG10202113286RA SG10202113286RA SG 10202113286R A SG10202113286R A SG 10202113286RA SG 10202113286R A SG10202113286R A SG 10202113286RA SG 10202113286R A SG10202113286R A SG 10202113286RA SG 10202113286R A SG10202113286R A SG 10202113286RA
Authority
SG
Singapore
Prior art keywords
triazolo
affinity
type
pyrimidine derivatives
cannabinoid receptor
Prior art date
Application number
SG10202113286RA
Inventor
Luca Gobbi
Uwe Grether
Wolfgang Guba
Julian Kretz
Rainer E Martin
Matthias Westphal
Adriaan Pieter Ijzerman
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 SG10202113286RA publication Critical patent/SG10202113286RA/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10Laxatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
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    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P27/02Ophthalmic agents
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    • A61P27/00Drugs for disorders of the senses
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06Antimalarials
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    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/94Chemical 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
    • G01N33/948Sedatives, e.g. cannabinoids, barbiturates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/705Assays involving receptors, cell surface antigens or cell surface determinants
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
SG10202113286RA 2016-06-23 2017-06-20 [1,2,3]triazolo[4,5-d]pyrimidine derivatives with affinity for the type-2 cannabinoid receptor SG10202113286RA (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP16175924 2016-06-23

Publications (1)

Publication Number Publication Date
SG10202113286RA true SG10202113286RA (en) 2021-12-30

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Family Applications (2)

Application Number Title Priority Date Filing Date
SG10202113286RA SG10202113286RA (en) 2016-06-23 2017-06-20 [1,2,3]triazolo[4,5-d]pyrimidine derivatives with affinity for the type-2 cannabinoid receptor
SG11201809678VA SG11201809678VA (en) 2016-06-23 2017-06-20 [1,2,3]triazolo[4,5-d]pyrimidine derivatives with affinity for the type-2 cannabinoid receptor

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SG11201809678VA SG11201809678VA (en) 2016-06-23 2017-06-20 [1,2,3]triazolo[4,5-d]pyrimidine derivatives with affinity for the type-2 cannabinoid receptor

Country Status (24)

Country Link
US (1) US10457685B2 (en)
EP (2) EP4108665A1 (en)
JP (2) JP6962942B2 (en)
KR (2) KR102530131B1 (en)
CN (4) CN113943297A (en)
AR (1) AR108845A1 (en)
AU (2) AU2017283136C1 (en)
BR (1) BR112018075143A2 (en)
CA (2) CA3023043A1 (en)
CL (1) CL2018003610A1 (en)
CO (1) CO2018011231A2 (en)
CR (2) CR20220661A (en)
IL (2) IL292015B1 (en)
MA (1) MA45442A (en)
MX (1) MX2018014684A (en)
MY (1) MY197244A (en)
PE (1) PE20190109A1 (en)
PH (1) PH12018502733A1 (en)
RU (1) RU2741597C2 (en)
SG (2) SG10202113286RA (en)
TW (2) TWI824380B (en)
UA (1) UA123834C2 (en)
WO (1) WO2017220517A1 (en)
ZA (1) ZA201807133B (en)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017220516A1 (en) 2016-06-23 2017-12-28 F. Hoffmann-La Roche Ag Novel [1,2,3]triazolo[4,5-d]pyrimidine derivatives
CN109311886B (en) 2016-06-23 2021-11-09 豪夫迈·罗氏有限公司 [1,2,3] triazolo [4,5-d ] pyrimidine derivatives
EP3475283B1 (en) 2016-06-23 2021-08-11 F. Hoffmann-La Roche AG Novel[1,2,3]triazolo[4,5-d]pyrimidine derivatives
CN113387845B (en) * 2021-07-16 2022-12-20 国药集团化学试剂有限公司 Preparation method of phenylmethylsulfonyl fluoride

Family Cites Families (18)

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Publication number Priority date Publication date Assignee Title
JP2003512326A (en) * 1999-10-18 2003-04-02 ユニヴァーシティ オブ コネチカット Similar indole derivatives of cannabinoids
JPWO2006051704A1 (en) * 2004-11-15 2008-05-29 大正製薬株式会社 Imine compounds
EP1863778B1 (en) 2005-03-31 2015-12-30 Merck Sharp & Dohme Corp. Spirocyclic thrombin receptor antagonists
FR2887550A1 (en) 2005-06-24 2006-12-29 Sanofi Aventis Sa New 1-benzylpyrazole-3-acetamide compounds are cannabinoids receptor antagonists useful to treat/prevent immune disorders, pain, gastrointestinal disturbances, cardiovascular/kidney disorders and in cancer chemotherapy
MX2008012400A (en) * 2006-03-30 2008-10-10 Irm Llc Azolopyrimidines as inhibitors of cannabinoid 1 activity.
US8629157B2 (en) * 2009-01-05 2014-01-14 Boehringer Ingelheim International Gmbh Pyrrolidine compounds which modulate the CB2 receptor
EP2311443A1 (en) 2009-10-15 2011-04-20 Rheinische Friedrich-Wilhelms-Universität Pharmaceutical composition containing cannabinoid-receptor 2 antagonists
CN102924457A (en) * 2011-08-12 2013-02-13 上海恒瑞医药有限公司 Triazolopyrimidine derivatives, preparation method and uses thereof
UA111640C2 (en) * 2011-11-08 2016-05-25 Ф. Хоффманн-Ля Рош Аг DERIVATIVES [1,2,3] TRIAZOLO [4,5-d] PYRIMIDINE AS A cannabinoid receptor agonist 2
US9067943B2 (en) 2011-11-25 2015-06-30 Hoffmann-La Roche Inc. [1,2,3]triazolo[4,5-D]pyrimidine derivatives
PE20151539A1 (en) 2013-03-07 2015-10-28 Hoffmann La Roche NEW DERIVATIVES OF PIRAZOLE
EP2991988B1 (en) 2013-05-02 2017-05-31 F. Hoffmann-La Roche AG Pyrrolo[2,3-d]pyrimidine derivatives as cb2 receptor agonists
KR102330794B1 (en) 2013-05-02 2021-11-26 에프. 호프만-라 로슈 아게 Purine derivatives as cb2 receptor agonists
EP3483163B1 (en) * 2013-09-06 2021-06-23 F. Hoffmann-La Roche AG Triazolo[4,5-d]pyrimidine derivatives as cb2 receptor antagonists
EP3215506B1 (en) 2014-11-07 2019-01-02 F.Hoffmann-La Roche Ag Triazolo[4,5-d]pyrimidines as agonists of the cannabinoid receptor 2
WO2017220516A1 (en) 2016-06-23 2017-12-28 F. Hoffmann-La Roche Ag Novel [1,2,3]triazolo[4,5-d]pyrimidine derivatives
CN109311886B (en) 2016-06-23 2021-11-09 豪夫迈·罗氏有限公司 [1,2,3] triazolo [4,5-d ] pyrimidine derivatives
EP3475283B1 (en) 2016-06-23 2021-08-11 F. Hoffmann-La Roche AG Novel[1,2,3]triazolo[4,5-d]pyrimidine derivatives

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RU2018146657A3 (en) 2020-07-31
JP6962942B2 (en) 2021-11-05
ZA201807133B (en) 2019-09-25
EP4108665A1 (en) 2022-12-28
CR20180615A (en) 2019-03-05
CR20220661A (en) 2023-02-21
EP3475282A1 (en) 2019-05-01
CO2018011231A2 (en) 2019-02-08
CN113943297A (en) 2022-01-18
RU2741597C2 (en) 2021-01-27
JP2022009140A (en) 2022-01-14
AU2017283136B2 (en) 2021-04-29
MX2018014684A (en) 2019-02-28
US10457685B2 (en) 2019-10-29
KR20190019085A (en) 2019-02-26
IL292015A (en) 2022-06-01
PH12018502733A1 (en) 2019-10-28
TW202216718A (en) 2022-05-01
CA3206921A1 (en) 2017-12-28
EP3475282C0 (en) 2023-08-09
JP7308246B2 (en) 2023-07-13
BR112018075143A2 (en) 2019-03-26
CN115073476A (en) 2022-09-20
AU2021206925B2 (en) 2023-03-30
US20190127384A1 (en) 2019-05-02
IL262711A (en) 2018-12-31
UA123834C2 (en) 2021-06-09
TW201811791A (en) 2018-04-01
KR102530131B1 (en) 2023-05-10
PE20190109A1 (en) 2019-01-15
IL262711B2 (en) 2023-07-01
EP3475282B1 (en) 2023-08-09
AU2021206925A1 (en) 2021-08-19
CA3023043A1 (en) 2017-12-28
AR108845A1 (en) 2018-10-03
RU2018146657A (en) 2020-07-23
AU2017283136C1 (en) 2021-07-29
SG11201809678VA (en) 2018-11-29
KR20230062680A (en) 2023-05-09
JP2019522648A (en) 2019-08-15
IL292015B1 (en) 2024-03-01
TWI764908B (en) 2022-05-21
MY197244A (en) 2023-06-07
CL2018003610A1 (en) 2019-03-29
CN109348716A (en) 2019-02-15
WO2017220517A1 (en) 2017-12-28
AU2017283136A1 (en) 2018-11-15
CN115093418A (en) 2022-09-23
MA45442A (en) 2019-05-01
IL262711B1 (en) 2023-03-01
TWI824380B (en) 2023-12-01

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