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1. WO1992000011 - LEUKOTRIENE B4 ANTAGONISTS

Publication Number WO/1992/000011
Publication Date 09.01.1992
International Application No. PCT/US1991/004386
International Filing Date 27.06.1991
Chapter 2 Demand Filed 28.01.1992
IPC
A61K 31/19 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
19Carboxylic acids, e.g. valproic acid
A61K 31/35 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
335having oxygen as the only ring hetero atom, e.g. fungichromin
35having six-membered rings with one oxygen as the only ring hetero atom
A61K 31/40 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
C07C 235/60 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
235Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
42having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
44with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
58with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho- position to carbon atoms of the same non-condensed six-membered aromatic ring
60having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07D 295/192 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
295Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
16acylated on ring nitrogen atoms
18by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
182Radicals derived from carboxylic acids
192from aromatic carboxylic acids
C07D 311/58 2006.1
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
A61K 31/19
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic, hydroximic acids
19Carboxylic acids, e.g. valproic acid
A61K 31/35
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
335having oxygen as the only ring hetero atom, e.g. fungichromin
35having six-membered rings with one oxygen as the only ring hetero atom
A61K 31/40
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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 43/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
C07C 235/60
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
235Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
42having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
44with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
58with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring
60having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
Applicants
  • G.D. SEARLE & CO. [US]/[US] (AllExceptUS)
  • DJURIC, Stevan, Wakefield [GB]/[US] (UsOnly)
  • DOCTER, Stephen, Hermann [US]/[US] (UsOnly)
  • YU, Stella, Siu-Tzyy [US]/[US] (UsOnly)
Inventors
  • DJURIC, Stevan, Wakefield
  • DOCTER, Stephen, Hermann
  • YU, Stella, Siu-Tzyy
Agents
  • WILLIAMS, Roger, A.
  • WOLFF, Hans Joachim
Priority Data
545,43028.06.1990US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) LEUKOTRIENE B4 ANTAGONISTS
(FR) ANTAGONISTES DE LEUKOTRIENE B4
Abstract
(EN) This invention relates to compounds of formula (I) and the stereoisomers and pharmaceutically acceptable salts thereof, wherein R is alkyl, alkenyl, alkynyl, or cycloalkylalkyl; R1 is alkyl; R2 is hydrogen or alkyl; R6 is alkyl; n is 1 to 5; p is 0 to 6; x is 0 or 2; and R4 and R5 are independently hydrogen or alkyl or together with N form a cycloalkylamine. The compounds of formula (I) are leukotriene B4 antagonists and are useful as anti-inflammatory agents and in treating disease conditions mediated by LTB4.
(FR) Cette invention se rapporte à des composés de formule (I) et aux stéréoisomères et aux sels pharmaceutiquement acceptables de ces composés où R représente alkyle, alcényle, alkynyle ou cycloalkylalkyle; R1 représente alkyle; R2 représente hydrogène ou alkyle; R6 représente alkyle; n représente de 1 à 5; p représente de 0 à 6; x représente 0 ou 2; et R4 et R5 sont indépendamment hydrogène ou alkyle ou forment avec N une cycloalkylamine. Les composés de formule (I) sont des antagonistes de leukotriène B4 et sont utiles comme agents anti-inflammatoires et dans le traitement de maladies où agit le LTB4.
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