CA2990460C - (4-((3r,4r)-3-methoxytetrahydro-pyran-4-ylamino)piperidin-1-yl)(5-methyl-6-(((2r,6s)-6-(p-tolyl)tetrahydro-2h-pyran-2-yl)methylamino)pyrimidin-4-yl)methanone citrate - Google Patents

(4-((3r,4r)-3-methoxytetrahydro-pyran-4-ylamino)piperidin-1-yl)(5-methyl-6-(((2r,6s)-6-(p-tolyl)tetrahydro-2h-pyran-2-yl)methylamino)pyrimidin-4-yl)methanone citrate Download PDF

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Publication number
CA2990460C
CA2990460C CA2990460A CA2990460A CA2990460C CA 2990460 C CA2990460 C CA 2990460C CA 2990460 A CA2990460 A CA 2990460A CA 2990460 A CA2990460 A CA 2990460A CA 2990460 C CA2990460 C CA 2990460C
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Prior art keywords
pain
pyran
salt
crystalline form
ray powder
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English (en)
French (fr)
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CA2990460A1 (en
Inventor
Markus Ostermeier
Ulrike Werthmann
Riccardo Giovannini
Sara Frattini
Stefan Scheurer
Heiner Ebel
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Centrexion Therapeutics Corp
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Centrexion Therapeutics Corp
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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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/166—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/351—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
    • 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
    • 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]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CA2990460A 2015-07-02 2016-07-01 (4-((3r,4r)-3-methoxytetrahydro-pyran-4-ylamino)piperidin-1-yl)(5-methyl-6-(((2r,6s)-6-(p-tolyl)tetrahydro-2h-pyran-2-yl)methylamino)pyrimidin-4-yl)methanone citrate Active CA2990460C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP15175066 2015-07-02
EP15175066.8 2015-07-02
PCT/US2016/040728 WO2017004537A1 (en) 2015-07-02 2016-07-01 (4-((3r,4r)-3-methoxytetrahydro-pyran-4-ylamino)piperidin-1-yl)(5-methyl-6-(((2r,6s)-6-(p-tolyl)tetrahydro-2h-pyran-2-yl)methylamino)pyrimidin-4yl)methanone citrate

Publications (2)

Publication Number Publication Date
CA2990460A1 CA2990460A1 (en) 2017-01-05
CA2990460C true CA2990460C (en) 2023-10-17

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CA2990460A Active CA2990460C (en) 2015-07-02 2016-07-01 (4-((3r,4r)-3-methoxytetrahydro-pyran-4-ylamino)piperidin-1-yl)(5-methyl-6-(((2r,6s)-6-(p-tolyl)tetrahydro-2h-pyran-2-yl)methylamino)pyrimidin-4-yl)methanone citrate

Country Status (13)

Country Link
US (4) US10213428B2 (enExample)
EP (1) EP3317270B1 (enExample)
JP (1) JP6917910B2 (enExample)
CN (1) CN108026087B (enExample)
AU (1) AU2016287584B2 (enExample)
BR (1) BR112017028492B1 (enExample)
CA (1) CA2990460C (enExample)
ES (1) ES2811098T3 (enExample)
IL (1) IL256530A (enExample)
MX (1) MX383744B (enExample)
PL (1) PL3317270T3 (enExample)
PT (1) PT3317270T (enExample)
WO (1) WO2017004537A1 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
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WO2011073154A1 (en) * 2009-12-17 2011-06-23 Boehringer Ingelheim International Gmbh New ccr2 receptor antagonists and uses thereof
WO2017004537A1 (en) * 2015-07-02 2017-01-05 Centrexion Therapeutics Corporation (4-((3r,4r)-3-methoxytetrahydro-pyran-4-ylamino)piperidin-1-yl)(5-methyl-6-(((2r,6s)-6-(p-tolyl)tetrahydro-2h-pyran-2-yl)methylamino)pyrimidin-4yl)methanone citrate
WO2025228900A1 (en) 2024-04-30 2025-11-06 Boehringer Ingelheim International Gmbh Arylamide substituted indazoles and the use thereof as medicament
US20250333414A1 (en) 2024-04-30 2025-10-30 Boehringer Ingelheim International Gmbh Hetaryl substituted indazoles and benzimidazoles as sting antagonists and the use thereof as medicament
WO2025228899A1 (en) 2024-04-30 2025-11-06 Boehringer Ingelheim International Gmbh Further heterocyclic compounds as sting antagonists and the use thereof as medicament
WO2025228892A1 (en) 2024-04-30 2025-11-06 Boehringer Ingelheim International Gmbh Monoaryl and hetaryl substituted indazoles and benzimidazoles as sting antagonists and the use thereof as medicament
WO2025228889A1 (en) 2024-04-30 2025-11-06 Boehringer Ingelheim International Gmbh Monoarylic heterocyclic compounds as sting antagonists and the use thereof as medicament
WO2025228902A1 (en) 2024-04-30 2025-11-06 Boehringer Ingelheim International Gmbh Heterocyclic acids as sting antagonists and the use thereof as medicament

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