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1. EP2336107 - Proton pump inhibitors

Office European Patent Office
Application Number 11154246
Application Date 30.09.2005
Publication Number 2336107
Publication Date 22.06.2011
Publication Kind B1
IPC
C07D 207/335
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
207Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
30having two double bonds between ring members or between ring members and non-ring members
32with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
33with substituted hydrocarbon radicals, directly attached to ring carbon atoms
335Radicals substituted by nitrogen atoms not forming part of a nitro radical
A61K 6/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
6Preparations for dentistry
A61K 31/4025
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
4025not condensed and containing further heterocyclic rings, e.g. cromakalim
A61K 31/4439
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
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
4439containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61P 1/00
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
A61P 1/04
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
04for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
CPC
A61K 31/4025
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
4025not condensed and containing further heterocyclic rings, e.g. cromakalim
A61K 31/41
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
A61K 31/4439
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
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non condensed pyridines; Hydrogenated derivatives thereof
4427containing further heterocyclic ring systems
4439containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/501
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
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
50Pyridazines; Hydrogenated pyridazines
501not condensed and containing further heterocyclic rings
A61K 31/506
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
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506not condensed and containing further heterocyclic rings
A61P 1/00
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
Applicants TAKEDA PHARMACEUTICAL
Inventors KAJINO MASAHIRO
HASUOKA ATSUSHI
TARUI NAOKI
TAKAGI TERUFUMI
Designated States
Priority Data 05790387 30.09.2005 EP
2004289169 30.09.2004 JP
2005044740 21.02.2005 JP
Title
(DE) Protonenpumpenhemmer
(EN) Proton pump inhibitors
(FR) Inhibiteurs de pompe a protons
Abstract
(EN)
A compound represented by the formula (II-a) wherein X 1 is -SO 2 -, -SO 2 -N (R 7 ) - (wherein R 7 is a hydrogen atom or an optionally substituted hydrocarbon group), -N(R 8 )-SO 2 - (wherein R 8 is a hydrogen atom or an optionally substituted hydrocarbon group), -N(R 9 )- (wherein R 9 is a hydrogen atom or an optionally substituted hydrocarbon group) or -O-, Y 1 is a C 1-8 alkylene group optionally having 1 to 3 substituents selected from a halogen atom and hydroxy, R 10 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R 11 is (i) a hydrogen atom, (ii) an optionally substituted hydrocarbon group, (iii) a 2- or 3-thienyl group optionally substituted by 1 to 3 substituents, (iv) a 2- or 3-benzo[b]thienyl group optionally substituted by 1 to 5 substituents (v) a 2- or 3-furyl group optionally substituted by 1 to 3 substituents, (vi) a 2-, 3- or 4-pyridyl group optionally substituted by 1 to 3 substituents, (vii) a 3- or 4-pyrazolyl group optionally substituted by 1 to 3 substituents, (viii) a 2-, 4- or 5-pyrimidinyl group optionally substituted by 1 to 3 substituents, R 12 and R 13 are each independently a hydrogen atom, an optionally substituted hydrocarbon group, an acyl group, a halogen atom, a cyano group or a nitro group (provided that R 12 and R 13 are not simultaneously hydrogen atoms), and R 14 and R 15 are each independently a hydrogen atom or an optionally substituted hydrocarbon group, or a salt thereof.

(FR)
Les inhibiteurs selon l'invention ont une excellente activité de pompage de protons et peuvent être transformés in vivo en inhibiteurs de pompe à protons pour présenter un effet antiulcéreux et similaire, et contiennent des composés représentés par la formule générale (I) ou des sels de ceux-ci ou des prodrogues de ceux-ci. Dans la formule (I), X et Y sont chacun indépendamment une valence libre ou un espaceur dont la chaîne principale a de 1 à 20 atomes de carbone ; R1 est un groupement hydrocarboné éventuellement substitué ou un groupement hétérocyclique éventuellement substitué ; R2, R3 et R4 sont chacun indépendamment hydrogène, un groupement hydrocarboné éventuellement substitué, thiényle éventuellement substitué, benzo[b]thiényle éventuellement substitué, furyle éventuellement substitué, pyridyle éventuellement substitué, pyrazolyle éventuellement substitué, pyrimidinyle éventuellement substitué, acyle, halogéno, cyano ou nitro ; et R5 et R6 sont chacun indépendamment hydrogène ou un groupement hydrocarboné éventuellement substitué.