CA2749529C - Quinazolinone derivatives useful as vanilloid antagonists - Google Patents

Quinazolinone derivatives useful as vanilloid antagonists Download PDF

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Publication number
CA2749529C
CA2749529C CA2749529A CA2749529A CA2749529C CA 2749529 C CA2749529 C CA 2749529C CA 2749529 A CA2749529 A CA 2749529A CA 2749529 A CA2749529 A CA 2749529A CA 2749529 C CA2749529 C CA 2749529C
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Canada
Prior art keywords
formula
compound
c6alkyl
hydroxy
compounds
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Active
Application number
CA2749529A
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English (en)
French (fr)
Other versions
CA2749529A1 (en
Inventor
Weichun Chen
Hong-Yong Kim
Jessica Liang
Michael Mutz
Mahavir Prashad
Christopher Towler
Ruoqiu Wu
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Bausch and Lomb Ireland Ltd
Original Assignee
Novartis AG
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Application filed by Novartis AG filed Critical Novartis AG
Priority to CA2946304A priority Critical patent/CA2946304A1/en
Publication of CA2749529A1 publication Critical patent/CA2749529A1/en
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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C07D239/91—Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • 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
    • A61P17/04—Antipruritics
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C07D239/90—Oxygen atoms with acyclic radicals attached in position 2 or 3

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CA2749529A 2009-01-13 2010-01-12 Quinazolinone derivatives useful as vanilloid antagonists Active CA2749529C (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CA2946304A CA2946304A1 (en) 2009-01-13 2010-01-12 Quinazolinone derivatives useful as vanilloid antagonists

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US14425009P 2009-01-13 2009-01-13
US61/144,250 2009-01-13
PCT/EP2010/050243 WO2010084050A2 (en) 2009-01-13 2010-01-12 Quinazolinone derivatives useful as vanilloid antagonists

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CA2946304A Division CA2946304A1 (en) 2009-01-13 2010-01-12 Quinazolinone derivatives useful as vanilloid antagonists

Publications (2)

Publication Number Publication Date
CA2749529A1 CA2749529A1 (en) 2010-07-29
CA2749529C true CA2749529C (en) 2017-04-04

Family

ID=42167396

Family Applications (2)

Application Number Title Priority Date Filing Date
CA2749529A Active CA2749529C (en) 2009-01-13 2010-01-12 Quinazolinone derivatives useful as vanilloid antagonists
CA2946304A Abandoned CA2946304A1 (en) 2009-01-13 2010-01-12 Quinazolinone derivatives useful as vanilloid antagonists

Family Applications After (1)

Application Number Title Priority Date Filing Date
CA2946304A Abandoned CA2946304A1 (en) 2009-01-13 2010-01-12 Quinazolinone derivatives useful as vanilloid antagonists

Country Status (28)

Country Link
US (2) US8349852B2 (cg-RX-API-DMAC10.html)
EP (1) EP2387440B1 (cg-RX-API-DMAC10.html)
JP (1) JP2012515150A (cg-RX-API-DMAC10.html)
KR (1) KR20110104996A (cg-RX-API-DMAC10.html)
CN (1) CN102281920A (cg-RX-API-DMAC10.html)
AR (1) AR075006A1 (cg-RX-API-DMAC10.html)
AU (1) AU2010206233B2 (cg-RX-API-DMAC10.html)
BR (1) BRPI1006909A2 (cg-RX-API-DMAC10.html)
CA (2) CA2749529C (cg-RX-API-DMAC10.html)
CO (1) CO6400202A2 (cg-RX-API-DMAC10.html)
CR (1) CR20110369A (cg-RX-API-DMAC10.html)
CU (1) CU20110148A7 (cg-RX-API-DMAC10.html)
EA (1) EA201101063A1 (cg-RX-API-DMAC10.html)
EC (1) ECSP11011195A (cg-RX-API-DMAC10.html)
ES (1) ES2614612T3 (cg-RX-API-DMAC10.html)
IL (1) IL213869A0 (cg-RX-API-DMAC10.html)
MA (1) MA32957B1 (cg-RX-API-DMAC10.html)
MX (1) MX2011007444A (cg-RX-API-DMAC10.html)
NZ (1) NZ593877A (cg-RX-API-DMAC10.html)
PE (1) PE20110776A1 (cg-RX-API-DMAC10.html)
PL (1) PL2387440T3 (cg-RX-API-DMAC10.html)
PT (1) PT2387440T (cg-RX-API-DMAC10.html)
SG (1) SG172808A1 (cg-RX-API-DMAC10.html)
TN (1) TN2011000326A1 (cg-RX-API-DMAC10.html)
TW (1) TW201036951A (cg-RX-API-DMAC10.html)
UY (1) UY32381A (cg-RX-API-DMAC10.html)
WO (1) WO2010084050A2 (cg-RX-API-DMAC10.html)
ZA (1) ZA201104873B (cg-RX-API-DMAC10.html)

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CN108863949B (zh) * 2018-07-09 2021-01-15 湖南博隽生物医药有限公司 一种用于治疗慢性炎性痛的辣椒素受体拮抗剂及合成方法
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