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1. WO1997030048 - 1,4-DIHYDROPYRIDINE COMPOUNDS AS BRADYKININ ANTAGONISTS

Publication Number WO/1997/030048
Publication Date 21.08.1997
International Application No. PCT/IB1997/000058
International Filing Date 27.01.1997
Chapter 2 Demand Filed 30.06.1997
IPC
C07D 211/90 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
211Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
80having two double bonds between ring members or between ring members and non-ring members
84with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
90Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
C07D 451/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
451Heterocyclic compounds containing 8-azabicyclo octane, 9-azabicyclo nonane, or 3-oxa-9-azatricyclo nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
02containing not further condensed 8-azabicyclo octane or 3-oxa-9-azatricyclo nonane ring systems, e.g. tropane; Cyclic acetals thereof
04with hetero atoms directly attached in position 3 of the 8-azabicyclo octane or in position 7 of the 3-oxa-9-azatricyclo nonane ring system
C07D 453/02 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
453Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
02containing not further condensed quinuclidine ring systems
CPC
A61P 1/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
08for nausea, cinetosis or vertigo; Antiemetics
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 11/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
08Bronchodilators
A61P 17/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
02for treating wounds, ulcers, burns, scars, keloids, or the like
A61P 25/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
02for peripheral neuropathies
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)
Applicants
  • PFIZER PHARMACEUTICALS INC. [JP]/[JP] (JP)
  • PFIZER INC. [US]/[US] (AT, AU, BE, BF, BG, BJ, BR, BY, CA, CF, CG, CH, CI, CM, CN, CZ, DE, DK, ES, FI, FR, GA, GB, GN, GR, HU, IE, IL, IS, IT, KR, KZ, LK, LU, LV, MC, ML, MR, MX, NE, NL, NO, NZ, PL, PT, RO, RU, SE, SG, SI, SK, SN, TD, TG, TR, UA, UZ, VN)
  • IKEDA, Takafumi [JP]/[JP] (UsOnly)
Inventors
  • IKEDA, Takafumi
Agents
  • SPIEGEL, Allen, J.
Priority Data
PCT/IB96/0013219.02.1996CA
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) 1,4-DIHYDROPYRIDINE COMPOUNDS AS BRADYKININ ANTAGONISTS
(FR) COMPOSES DE 1,4-DIHYDROPYRIDINE UTILISES COMME ANTAGONISTES DE LA BRADYKININE
Abstract
(EN)
A compound of formula (I), and its pharmaceutically acceptable salts, wherein A1 and A2 are each halo; X is CO, S(O)2 or S(O)-(CH2)n wherein S atom is directly attached to the phenyl and n is 0, 1 or 2; and R1 is 8-azabicyclo[3.2.1]octyl, quinuclidinyl, bicyclo[3.3.0]octyl, C3-10 cycloalkyl, 2,3,5,6-tetrahydro-4H-thiopyranyl or C3-6 cycloalkyl-C1-4 alkyl, optionally substituted with C1-4 alkyl, hydroxy, dioxaranyl or oxo. The novel dihydropyridine compounds of this invention have excellent bradykinin antagonistic activity and are thus useful for the treatment of medical conditions caused by bradykinin such as inflammation, cardiovascular disease, pain, common cold, allergies, asthma, pancreatitis, burns, virus infection, head injury, multiple trauma or the like in mammalian, especially humans.
(FR)
L'invention a trait à un composé de la formule (I) ainsi qu'à ses sels acceptables du point de vue pharmaceutique. Dans cette formule, A1 et A2 représentent chacun un halo, X représente CO, S(O)2 ou S(O)-(CH2)n où un atome de S est directement lié au phényle et où n vaut 0 ou 2. Dans cette même formule (I), R1 représente un 8-azabicyclo[3.2.1] octyle, un quinuclidinyle, un bicyclo[3.3.0] octyle, un cycloalkyle comportant de 3 à 10 atomes de carbone, un 2,3,5,6-tétrahydro-4H-thiopyranyle ou un cycloalkyl-C1-4 alkyle comportant de 3 à 6 atomes de carbone, éventuellement substitué par un alkyle comportant de 1 à 4 atomes de carbone, un hydroxy, un dioxaranyle ou un oxo. Les nouveaux composés à base de dihydropyridine décrits dans cette invention, qui se révèlent comme de remarquables antagonistes de la bradykinine, sont des plus utiles dans le traitement d'inflammations, de maladies cardio-vasculaires, de la douleur, du rhume banal, d'allergies, de l'asthme, de pancréatites, de brûlures, d'infections virales, de traumatismes crâniens, de traumatismes multiples ou analogue, chez les mammifères et notamment, les humains.
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