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1. EP1322628 - SUBSTITUTED UREA NEUROPEPTIDE Y Y5 RECEPTOR ANTAGONISTS

Office
European Patent Office
Application Number 01975194
Application Date 12.09.2001
Publication Number 1322628
Publication Date 02.07.2003
Publication Kind A2
IPC
C07D 205/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
205Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
02not condensed with other rings
04having no double bonds between ring members or between ring members and non-ring members
A61K 31/17
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
16Amides, e.g. hydroxamic acids
17having the group N-C(O)-N or N-C(S)-N, e.g. urea, thiourea, carmustine
A61K 31/18
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
16Amides, e.g. hydroxamic acids
18Sulfonamides
A61K 31/397
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
397having four-membered rings, e.g. azetidine
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
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
CPC
A61P 1/14
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
14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
A61P 1/16
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
16for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 3/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
A61P 3/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
04Anorexiants; Antiobesity agents
A61P 3/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
06Antihyperlipidemics
A61P 3/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
08for glucose homeostasis
10for hyperglycaemia, e.g. antidiabetics
Applicants SCHERING CORP
Inventors GREENLEE WILLIAM J
HUANG YING
KELLY JOSEPH M
MC COMBIE STUART W
STAMFORD ANDREW W
WU YUSHENG
Designated States
Priority Data 0128324 12.09.2001 US
23225500 14.09.2000 US
Title
(DE) SUBSTITUIERTE HARNSTOFFE ALS NEUROPEPTID Y Y5 REZEPTOR ANTAGONISTEN
(EN) SUBSTITUTED UREA NEUROPEPTIDE Y Y5 RECEPTOR ANTAGONISTS
(FR) ANTAGONISTES DU RECEPTEUR Y.Y5 DE NEUROPEPTIDE D'UREASE SUBSTITUE
Abstract
(EN)
Compounds represented by structural formula (I) including its N-oxides wherein Y is (a) or (b); R1 is H or (C1-C6)alkyl; R2 is H,(C1-C6)alkyl,(C3-C9)cycloalkyl or (C3-C7)cycloalkyl(C1-C6)alkyl; R3 is (c), (d), (e), (f), (g), (h) or (i); R4 is 1-3 substituents independently selected from the group consisting of H, -OH, halogen, haloalkyl,(C1-C6) alkyl, (C3-C7) cycloalkyl, (C3-C7) cycloalkyl (C1-C6) alkyl, -CN, -O(C1-C6) alkyl, -O(C3-C7) cycloalkyl, -O(C1-C6) alkyl (C3-C7) cycloalkyl, -S(C1-C6) alkyl, -S(C3-C7) cycloalkyl, -S(C1-C6) alkyl(C3-C7) cycloalkyl, -NH2, -NR9R10, -NO2, -CONH2, -CONR9R10 and NR2COR10; or where applicable, a geometric or optical isomer or a racemic mixture thereof, are claimed, as well as additional novel compounds; also claimed are pharmaceutical compositions and methods of using the aforesaid compounds in the treatment of obesity, eating disorders such as hyperphagia and diabetes.

(FR)
La présente invention concerne des composés représentés par la formule structurelle (I) comprenant ses oxyde de N. Dans cette formule Y est (I') R1 est H ou (C1-C6)alkyle; R2 est H, (C1-C6)alkyle, (C3-C9)cycloalkyle ou (C3-C7)cycloalkyle(C1-C6)alkyle; R3 est (II'); Z est OR10, -N(R9)(R10) ou - NH2; j est 0, 1 ou 2; k est 1 ou 2; l est 0, 1 ou 2; m est 0, 1 ou 2; R4 est 1- 3 substituants indépendamment sélectionné dans le groupe constitué de H, -OH, halogène, haloalkyle, (C1-C6)alkyle, (C3-C7)cycloalkyle, (C3-C7)cycloalkyle(C1-C6)alkyle, -CN, -O(C1-C6)alkyle, -O(C3-C7)cycloalkyle, -O(C1-C6)alkyle(C3-C7)cycloalkyle, -S(C1-C6)alkyle, -S(C3-C7)cycloalkyle, -S(C1-C6)alkyle(C3-C7)cycloalkyle, -NH2, -NR9R10, -NO2, -CONH2, -CONR9R10 et NR2COR10; R5 est 1-3 substituants indépendamment sélectionné dans le groupe constitué de H, halogène, -OH, haloalkyle, haloalcoxy, -CN, -NO2, (C1-C6)alkyle, (C3-C7)cycloalkyle, (C3-C7)cycloalkyle(C1-C6)alkyle, -O(C1-C6)alkyle, -O(C3-C7)cycloalkyle, -O(C1-C6)alkyleC3-C7)cycloalkyle, -CONH2 et -CONR9R10; R6 est -SO2(C1-C6)alkyle, -SO2(C3-C7)cycloalkyle, -SO2(C1-C6)alkyle(C3-C7)cycloalkyle, -SO2(C1-C6)haloalkyle, -SO2(hydroxy(C2-C6)alkyle), -SO2(amino(C2-C6)alkyle), -SO2(alcoxy(C2-C6)alkyle), -SO2(alkylamino(C2-C6)alkyle), -SO2(dialkylamino(C2-C6)alkyle), -SO2(aryle), -SO2(hétéroaryle), -SO2(aryle(C2-C6-alkyle), SO2NH2, -SO2NR9R10, -C(O)C1-C6alkyle, -C(O)C3-C7cycloalkyle, -C(O)aryle, - C(O)hétéroaryle, -C(O)NR9R10, -C(O)NH2, -C(S)NR9R10, -C(S)NH2, aryle, hétéroaryle, -(CH2)nC(O)NH2, -(CH2)nC(O)NR9R10,-C(=NCN)alkylthio, -C(=NCN)NR9R10, (C1-C6)alkyle, (C3-C7)cycloalkyle, (C3-C7)cycloalkyle(C1-C6)alkyle, aryle(C1-C6)alkyle, hétéroaryle(C1-C6)alkyle ou -C(O)OR9, n= 1 à 6; R7 = H ou alkyle; R8 est H, (C1-C6)alkyle, (C3-C7)cycloalkyle, (C3-C7)cycloalkyle(C1-C6)alkyle, aryle, hétéroaryle, -SO2(C1-C6)alkyle, -SO2(C3-C7)cycloalkyle, -SO2(C1-C6)alkyle(C3-C7)cycloalkyle, -SO2(C1-C6)haloalkyle ou -SO2(aryle); R9 est (C1-C6)alkyle, (C3-C7)cycloalkyle, (C3-C7)cycloalkyle(C1-C6)alkyle, aryle(C1-C6)alkyle, aryle ou hétéroaryle; et, R10 est hydrogène, (C1-C6)alkyle, (C3-C7)cycloalkyle, (C3-C7)cycloalkyle(C1-C6)alkyle, aryle(C1-C6)alkyle, aryle ou hétéroaryle; ou une addition de sel et/ou d'hydrate de ces composés répondant aux normes pharmaceutiques, ou des promédicaments de ces composés, ou R9 et R10 pris ensemble peuvent former un cycle à 4-7 branches contenant 1 ou 2 hétéro-atomes. Cette invention concerne aussi un isomère géométrique ou optique ou un mélange racémique de ces composés, de même que de nouveau composés, des compositions parmaceutiques et des procédés d'utilisation des composés susmentionnés dans le traitement contre l'obésité, le traitement des troubles liés à l'alimentation tels que l'hyperphagie et le dabète.