CA3071575A1 - Thiazolopyridine derivatives as adenosine receptor antagonists - Google Patents

Thiazolopyridine derivatives as adenosine receptor antagonists Download PDF

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Publication number
CA3071575A1
CA3071575A1 CA3071575A CA3071575A CA3071575A1 CA 3071575 A1 CA3071575 A1 CA 3071575A1 CA 3071575 A CA3071575 A CA 3071575A CA 3071575 A CA3071575 A CA 3071575A CA 3071575 A1 CA3071575 A1 CA 3071575A1
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CA
Canada
Prior art keywords
thiazolo
compound
methoxy
pyridin
formula
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CA3071575A
Other languages
English (en)
French (fr)
Inventor
Eva-Maria TANZER
Kai Schiemann
Markus Klein
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Patent GmbH
Original Assignee
Merck Patent GmbH
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 Merck Patent GmbH filed Critical Merck Patent GmbH
Publication of CA3071575A1 publication Critical patent/CA3071575A1/en
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/429—Thiazoles condensed with heterocyclic ring systems
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • 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)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Virology (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Epoxy Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Saccharide Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA3071575A 2017-08-01 2018-07-02 Thiazolopyridine derivatives as adenosine receptor antagonists Pending CA3071575A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP17184272.7 2017-08-01
EP17184272 2017-08-01
PCT/EP2018/067797 WO2019025099A1 (en) 2017-08-01 2018-07-02 THIAZOLOPYRIDINE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS

Publications (1)

Publication Number Publication Date
CA3071575A1 true CA3071575A1 (en) 2019-02-07

Family

ID=59506176

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3071575A Pending CA3071575A1 (en) 2017-08-01 2018-07-02 Thiazolopyridine derivatives as adenosine receptor antagonists

Country Status (22)

Country Link
US (1) US11186592B2 (enExample)
EP (1) EP3661941B1 (enExample)
JP (1) JP7336434B2 (enExample)
KR (1) KR102717280B1 (enExample)
CN (1) CN110997681B (enExample)
AU (1) AU2018309265B2 (enExample)
CA (1) CA3071575A1 (enExample)
DK (1) DK3661941T3 (enExample)
ES (1) ES2940407T3 (enExample)
FI (1) FI3661941T3 (enExample)
HR (1) HRP20230251T1 (enExample)
HU (1) HUE061308T2 (enExample)
IL (1) IL272284B2 (enExample)
LT (1) LT3661941T (enExample)
PL (1) PL3661941T3 (enExample)
PT (1) PT3661941T (enExample)
RS (1) RS64035B1 (enExample)
SG (1) SG11202000823WA (enExample)
SI (1) SI3661941T1 (enExample)
TW (1) TWI850199B (enExample)
WO (1) WO2019025099A1 (enExample)
ZA (1) ZA202001295B (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR117844A1 (es) * 2019-01-22 2021-09-01 Merck Patent Gmbh Derivados de tiazolopiridina como antagonistas del receptor de adenosina
CN112174943A (zh) * 2019-07-03 2021-01-05 四川大学 一种吲哚-2-酮类化合物在制备防治口腔细菌产品中的用途
EP4351640A1 (en) 2021-06-07 2024-04-17 Ares Trading S.A. Combination treatment of cancer
MX2025000931A (es) 2022-08-02 2025-03-07 Merck Patent Gmbh Nuevas formas cristalinas de [7-(3,6-dihidro-2h-piran-4-il)-4-metoxi-tiazolo[4,5-c]piridin-2-il]-amida de acido (s)-7-oxa-2-aza-espiro[4.5]decano-2-carboxilico y formas cocristalinas de las mismas

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4207554A (en) 1972-08-04 1980-06-10 Med-El Inc. Method and apparatus for automated classification and analysis of cells
US4125828A (en) 1972-08-04 1978-11-14 Med-El Inc. Method and apparatus for automated classification and analysis of cells
GB9624482D0 (en) 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
CA2242425C (en) 1996-02-13 2006-07-18 Zeneca Limited Quinazoline derivatives as vegf inhibitors
NZ331191A (en) 1996-03-05 2000-03-27 Zeneca Ltd 4-anilinoquinazoline derivatives and pharmaceutical compositions thereof
GB9718972D0 (en) 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
GB9714249D0 (en) 1997-07-08 1997-09-10 Angiogene Pharm Ltd Vascular damaging agents
US6579868B1 (en) 1998-01-05 2003-06-17 Eisai Co., Ltd. Purine derivatives and adenosine A2 receptor antagonists serving as preventives/remedies for diabetes
GB9900334D0 (en) 1999-01-07 1999-02-24 Angiogene Pharm Ltd Tricylic vascular damaging agents
GB9900752D0 (en) 1999-01-15 1999-03-03 Angiogene Pharm Ltd Benzimidazole vascular damaging agents
WO2001002400A1 (en) 1999-07-02 2001-01-11 Eisai Co., Ltd. Fused imidazole compounds and remedies for diabetes mellitus
BR0111230A (pt) 2000-05-31 2003-06-10 Astrazeneca Ab Composto, e, uso e processo para a preparação do mesmo
RU2251419C2 (ru) * 2000-06-21 2005-05-10 Ф. Хоффманн-Ля Рош Аг Производные бензотиазола
KR20030014425A (ko) 2000-07-07 2003-02-17 앤지오젠 파마슈티칼스 리미티드 혈관 손상제인 콜치놀 유도체
EE200300015A (et) 2000-07-07 2004-10-15 Angiogene Pharmaceuticals Limited Kolhinooli derivaadid kui angiogeneesi inhibiitorid
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US6713499B2 (en) * 2001-12-12 2004-03-30 Hoffman-La Roche Inc. 7-Amino-benzothiazole derivatives
JP2005516917A (ja) 2001-12-12 2005-06-09 アメリカ合衆国 細胞外アデノシン阻害剤およびアデノシン受容体阻害剤を用いて免疫応答および炎症を増強するための方法
WO2004092171A2 (en) 2003-04-09 2004-10-28 Biogen Idec Ma Inc. Triazolo[1,5-a]pyrimidines and pyrazolo[1,5-a]pyrimidines useful as a2a adenosin e receptor antagonists
US6872833B2 (en) * 2003-04-14 2005-03-29 Hoffmann-La Roche Inc. Adenosine receptor ligands
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WO2005028484A1 (en) * 2003-09-19 2005-03-31 F. Hoffmann-La Roche Ag Thiazolopyridine derivatives as adenosine receptor ligands
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KR101077295B1 (ko) * 2006-05-18 2011-10-26 에프. 호프만-라 로슈 아게 아데노신 a2b 수용체 길항물질로서의 티아졸로-피라미딘/피리딘 우레아 유도체
US8168785B2 (en) * 2009-06-17 2012-05-01 Biotie Therapies, Inc. Benzothiazole derivatives
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Also Published As

Publication number Publication date
FI3661941T3 (fi) 2023-03-23
AU2018309265A1 (en) 2020-03-19
RU2020107737A3 (enExample) 2021-11-23
RS64035B1 (sr) 2023-04-28
KR20200035439A (ko) 2020-04-03
SG11202000823WA (en) 2020-02-27
US20200181171A1 (en) 2020-06-11
IL272284A (en) 2020-03-31
US11186592B2 (en) 2021-11-30
PL3661941T3 (pl) 2023-05-08
IL272284B1 (en) 2023-09-01
DK3661941T3 (da) 2023-03-13
AU2018309265B2 (en) 2022-06-02
CN110997681A (zh) 2020-04-10
SI3661941T1 (sl) 2023-04-28
JP7336434B2 (ja) 2023-08-31
WO2019025099A1 (en) 2019-02-07
RU2020107737A (ru) 2021-09-02
LT3661941T (lt) 2023-04-11
BR112020001978A2 (pt) 2020-08-18
NZ760516A (en) 2026-01-30
EP3661941A1 (en) 2020-06-10
IL272284B2 (en) 2024-01-01
PT3661941T (pt) 2023-03-16
ZA202001295B (en) 2023-09-27
HUE061308T2 (hu) 2023-06-28
JP2020528922A (ja) 2020-10-01
ES2940407T3 (es) 2023-05-08
CN110997681B (zh) 2022-11-15
KR102717280B1 (ko) 2024-10-14
HRP20230251T1 (hr) 2023-04-14
EP3661941B1 (en) 2022-12-14
TW201920201A (zh) 2019-06-01
TWI850199B (zh) 2024-08-01

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