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PE20110776A1 - Derivados de quinazolinona utiles como antagonistas de vanilloides - Google Patents

Derivados de quinazolinona utiles como antagonistas de vanilloides

Info

Publication number
PE20110776A1
PE20110776A1 PE2011001336A PE2011001336A PE20110776A1 PE 20110776 A1 PE20110776 A1 PE 20110776A1 PE 2011001336 A PE2011001336 A PE 2011001336A PE 2011001336 A PE2011001336 A PE 2011001336A PE 20110776 A1 PE20110776 A1 PE 20110776A1
Authority
PE
Peru
Prior art keywords
alkyl
halogen
antagonists
formula
vanylloids
Prior art date
Application number
PE2011001336A
Other languages
English (en)
Inventor
Weichun Chen
Hong-Yong Kim
Jessica Liang
Michael Mutz
Mahavir Prashad
Christopher Towler
Ruoqiu Wu
Original Assignee
Novartis Ag
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42167396&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20110776(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20110776A1 publication Critical patent/PE20110776A1/es

Links

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

Landscapes

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

Abstract

SE REFIERE A LA FORMA CRISTALINA B DEL 4-(7-HIDROXI-2-ISOPROPIL-4-OXO-4H-QUINAZOLIN-3-IL)-BENZONITRILO CUYO PATRON DE DIFRACCION DE RAYOS X TIENE LOS PICOS EN VALORES 2? DE 9.3, 10.6 Y 14.4 ± 0.2 º2?. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA Y A UN PROCESO DE OBTENCION DE COMPUESTOS DE QUINAZOLINONA DE FORMULA (I) DONDE R1 ES ALQUILO(C1-C6), CICLOALQUILO(C3-C6), DI-(TRIFLUORO-METIL)-ALQUILO(C1-C6), ENTRE OTROS; R2 ES HALOGENO, ALQUILO(C1-C6), HIDROXI-ALQUILO(C1-C6), ENTRE OTROS; R3 ES H, HALOGENO, ALQUENILO(C2-C6), ENTRE OTROS; R4 ES H; R5 ES H O HIDROXILO; R6 ES H, HALOGENO, ALQUINILO(C2-C6), ENTRE OTROS; m ES DE 1 A 5; DONDE EL PROCESO COMPRENDE: A) HACER REACCIONAR UN COMPUESTO DE FORMULA (II) CON UN COMPUESTO DE ANILINA DE FORMULA (III) BAJO CONDICIONES DE CONDENSACION Y CICLACION SIMULTANEAS O EN SECUENCIA DONDE R*4 ES R1*-C(=O)- O H, R1* ES R1. DICHOS COMPUESTOS SON ANTAGONISTAS DE VANILLOIDES SIENDO UTILES EN EL TRATAMIENTO DEL DOLOR, OSTEOARTRITIS, FIBROMIALGIA, ASMA
PE2011001336A 2009-01-13 2010-01-12 Derivados de quinazolinona utiles como antagonistas de vanilloides PE20110776A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US14425009P 2009-01-13 2009-01-13

Publications (1)

Publication Number Publication Date
PE20110776A1 true PE20110776A1 (es) 2011-11-04

Family

ID=42167396

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2011001336A PE20110776A1 (es) 2009-01-13 2010-01-12 Derivados de quinazolinona utiles como antagonistas de vanilloides

Country Status (28)

Country Link
US (2) US8349852B2 (es)
EP (1) EP2387440B1 (es)
JP (1) JP2012515150A (es)
KR (1) KR20110104996A (es)
CN (1) CN102281920A (es)
AR (1) AR075006A1 (es)
AU (1) AU2010206233B2 (es)
BR (1) BRPI1006909A2 (es)
CA (2) CA2946304A1 (es)
CO (1) CO6400202A2 (es)
CR (1) CR20110369A (es)
CU (1) CU20110148A7 (es)
EA (1) EA201101063A1 (es)
EC (1) ECSP11011195A (es)
ES (1) ES2614612T3 (es)
IL (1) IL213869A0 (es)
MA (1) MA32957B1 (es)
MX (1) MX2011007444A (es)
NZ (1) NZ593877A (es)
PE (1) PE20110776A1 (es)
PL (1) PL2387440T3 (es)
PT (1) PT2387440T (es)
SG (1) SG172808A1 (es)
TN (1) TN2011000326A1 (es)
TW (1) TW201036951A (es)
UY (1) UY32381A (es)
WO (1) WO2010084050A2 (es)
ZA (1) ZA201104873B (es)

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AR087814A1 (es) * 2011-09-16 2014-04-16 Fovea Pharmaceuticals Derivados de anilina, su preparacion y su aplicacion terapeutica
KR101789430B1 (ko) * 2016-06-28 2017-10-25 동국대학교 산학협력단 Smo 저해 활성을 갖는 신규 화합물 및 이를 유효성분으로 포함하는 암 예방 또는 치료용 조성물
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
US20200261456A1 (en) * 2019-02-15 2020-08-20 Novartis Ag Methods for treating ocular surface pain
JP6994061B2 (ja) 2019-02-15 2022-01-14 ノバルティス アーゲー ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの製剤
JP2022520410A (ja) * 2019-02-15 2022-03-30 ノバルティス アーゲー ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの結晶形態及びその製剤
JP2022541013A (ja) 2019-07-15 2022-09-21 ノバルティス アーゲー 肝臓ｘ受容体アゴニストでマイボーム腺機能不全を治療するための方法
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JP2023536938A (ja) * 2020-08-06 2023-08-30 ノバルティス アーゲー ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの結晶形態及びその製剤
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