Processing

Please wait...

Settings

Settings

Goto Application

1. WO1996011920 - BENZOPYRAN AND BENZO-FUSED COMPOUNDS, THEIR PREPARATION AND THEIR USE AS LEUKOTRIENE B¿4? (LTB¿4?) ANTAGONISTS

Publication Number WO/1996/011920
Publication Date 25.04.1996
International Application No. PCT/IB1995/000401
International Filing Date 26.05.1995
Chapter 2 Demand Filed 04.03.1996
IPC
C07D 311/22 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
311Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
02ortho- or peri-condensed with carbocyclic rings or ring systems
04Benzo pyrans, not hydrogenated in the carbocyclic ring
22with oxygen or sulfur atoms directly attached in position 4
C07D 311/58 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
311Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
02ortho- or peri-condensed with carbocyclic rings or ring systems
04Benzo pyrans, not hydrogenated in the carbocyclic ring
58other than with oxygen or sulfur atoms in position 2 or 4
CPC
A61P 11/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
A61P 11/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
06Antiasthmatics
A61P 29/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29Non-central analgesic, antipyretic or anti-inflammatory agents, e.g antirheumatic agents; Non-steroidal anti-inflammatory drugs (NSAIDs)
A61P 37/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
A61P 37/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
02Immunomodulators
06Immunosuppressants, e.g. drugs for graft rejection
C07D 311/22
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
311Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
02ortho- or peri-condensed with carbocyclic rings or ring systems
04Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
22with oxygen or sulfur atoms directly attached in position 4
Applicants
  • PFIZER INC. [US]/[US] (AllExceptUS)
  • DOMBROSKI, Mark, A. [US]/[US] (UsOnly)
  • KOCH, Kevin [US]/[US] (UsOnly)
  • PISCOPIO, Anthony, Daniel [US]/[US] (UsOnly)
Inventors
  • DOMBROSKI, Mark, A.
  • KOCH, Kevin
  • PISCOPIO, Anthony, Daniel
Agents
  • SPIEGEL, Allen, J.
Priority Data
08/322,87613.10.1994US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) BENZOPYRAN AND BENZO-FUSED COMPOUNDS, THEIR PREPARATION AND THEIR USE AS LEUKOTRIENE B4 (LTB4) ANTAGONISTS
(FR) COMPOSES DE BENZOPYRANNE ET COMPOSES BENZO-FUSIONNES, LEUR PREPARATION ET LEUR UTILISATION COMME ANTAGONISTES DE LEUCOTRIENE B4 (LTB4)
Abstract
(EN)
This invention relates to novel benzopyran and other benzo-fused leukotriene B4 (LTB4) antagonists of formula (I), and the pharmaceutically acceptable salts thereof, wherein A1 is O, CH2, S, NH or N(C1-C6)alkyl; R3 is hydrogen or hydroxy; A2 is (a), (b) or (c); R1 is selected from the group consisting of tetrazolyl, carboxy, $i(cis) or $i(trans) -(CH2)m-CX1=CX2-CO2H, -(CH2)mCX3X4X5, -CO-NG1G2, (d), and a substituted five or six membered aromatic ring optionally having one or two heteroatoms where the heteroatoms are optionally independently selected from the group consisting of O, S and N; R2 is hydrogen, fluoro, chloro, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C4)perfluoroalkyl, (C1-C4)perfluoroalkoxy, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl, phenylsulfinyl, (C1-C6)alkylsulfonyl or phenylsulfonyl; to pharmaceutical compositions containing such compounds or a pharmaceutically acceptable salt thereof, and to methods of using such compounds as LTB4 antagonists. The compounds and the pharmaceutically acceptable salts of this invention inhibit the action of LTB4 and are therefore useful in the treatment of LTB4 induced illnesses such as inflammatory disorders including rheumatoid arthritis, osteoarthritis, inflammatory bowel disease, psoriasis and other skin disorders such as eczema, erythema, pruritus and acne, stroke and other forms of reperfusion injury, graft rejection, autoimmune diseases, asthma, and other conditions where marked neutrophil infiltration occurs.
(FR)
L'invention concerne de nouveaux antagonistes de leucotriène B4 (LTB4) au benzopyranne et benzo-fusionnés ayant la formule (I), ainsi que leurs sels pharmaceutiquement acceptables. Dans la formule (I), A1 représente O, CH2, S, NH ou N(C1-C6)alkyle; R3 représente hydrogène ou hydroxy; A2 représente (a), (b) ou (c); R1 est sélectionné dans le groupe constitué de tétrazolyle, carboxy, $i(cis)- ou $i(trans)-(CH2)m-CX1 = CX2-CO2H, -(CH2)mCX3X4X5, -CO-NG1G2, (d), et un cycle aromatique à cinq ou six éléments ayant le cas échéant un ou deux hétéroatomes, les hétéroatomes étant le cas échéant sélectionnés indépendamment dans le groupe constitué d'O, S et N; R2 désigne hydrogène, fluoro, chloro, (C1-C6)alkyle, (C1-C6)alcoxy, (C1-C4)perfluoroalkyle, (C1-C4)perfluoroalcoxy, (C1-C6)alkylthio, (C1-C6)alkylsulfinyle, phénylsulfinyle, (C1-C6)alkylsulfonyle ou phénylsulfonyle. L'invention concerne également des compositions pharmaceutiques contenant ces composés ou un sel pharmaceutiquement acceptable de ceux-ci, et des procédés d'utilisation de ces composés comme antagonistes de LTB4. Ces composés et leurs sels pharmaceutiquement acceptables inhibent l'action de LTB4 et sont par conséquent utiles pour traiter des maladies induites par le LTB4, telles que des maladies inflammatoires, y compris la polyarthrite rhumatoïde, l'ostéoarthrite, la colopathie fonctionnelle, le psoriasis et d'autres maladies de la peau telles que l'eczéma, des érythèmes, des prurits et l'acné, des ictus et d'autres types de lésions dus à des reperfusions, des rejets de greffes, des maladies auto-immunitaires, l'asthme et d'autres états caractérisés par une infiltration marquée de neutrophiles.
Latest bibliographic data on file with the International Bureau