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1. EP1896465 - HETEROCYCLIC NON-PEPTIDE GNRH ANTAGONISTS

Office European Patent Office
Application Number 06755630
Application Date 27.06.2006
Publication Number 1896465
Publication Date 12.03.2008
Publication Kind A1
IPC
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506
not condensed and containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
5
Drugs for disorders of the endocrine system
02
of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C07D 413/12
A61K 31/506
A61P 5/02
C07D 403/12
C07D 417/12
CPC
C07D 403/12
C07D 413/12
C07D 417/12
Applicants TAKEDA CAMBRIDGE LTD
Inventors SHOWELL GRAHAM A
MILLER DAVID J
GLEN ANGELA
CUBILLO DE DIOS MARIA A
MERCHANT KEVIN
MANDAL AJAY KUMAR
Designated States
Priority Data 0513176 28.06.2005 GB
0521278 19.10.2005 GB
0608846 04.05.2006 GB
2006002344 27.06.2006 GB
Title
(DE) HETEROCYCLISCHE NICHT-PEPTIDISCHE GNRH-ANTAGONISTEN
(EN) HETEROCYCLIC NON-PEPTIDE GNRH ANTAGONISTS
(FR) ANTAGONISTES NON-PEPTIDES HETEROCYCLIQUES DE GNRH
Abstract
(EN)
A compound of formula (I): wherein either B is absent and A and Z are the same or different and are each hydrogen, halogen, alkyl, hydroxy, alkoxy, -CN, -C(Rc)2OH, -N(Rd)C(=X)Rc, -C(=X)N(Rc)(Rd), -S(O)m-Rc, -N(Rc)(Rd)S(O)2, -S(O)2N(Rc)(Rd), -N(Re)2, aryl optionally substituted with Ra or -O-aryl optionally substituted with Ra; or B is present and is -(CH2)n-, -C(Rb)2- or -O-, or B taken together with A or Z can be -C=C(Rb)-, -C(Rb)=C-, -CH2-CH(Rb)- or -CH(Rb)-CH2-; D is -O- or -S(O)m,-; E is a bond or is -(CH2)n-, -N(Rd)-, -(CH2)nN(Rd)- or -N(Rd)(CH2)n-; F is -C(=X)-; G is -(CH2)n-, -N(Rd)-, -(CH2)nN(Rd)- or -N(Rd)(CH2)n; J is a bond, -O-, -N(RC)C(=X)-, -C(=X)N(Rc)-, -S(O)m,-, -N(Rc)S(O)m-, -S(O)nN(Rc)-, -N(Re)- or -N(Rg)(Rh); K is a bond, alkylene, cycloalkylene, cycloalkenylene, arylene, heterocycloalkylene, heterocycloalkylene or heteroarylene; and L is hydrogen or a terminal group; has therapeutic utility.

(FR)
Composé de formule (I) possédant une utilité thérapeutique. Dans ladite formule soit B est absent et A et Z sont identiques ou différents et représentent chacun hydrogène, halogène, alkyle, hydroxy, alcoxy, -CN, -C(Rc)2OH, -N(Rd)C(=X)Rc, -C(=X)N(Rc)(Rd), -S(O)m-Rc, -N(Rc)(Rd)S(O)2, -S(O)2N(Rc)(Rd), -N(Re)2, aryle éventuellement substitué par Ra ou -O-aryle éventuellement substitué par Ra; soit B est présent et représente -(CH2)n-, -C(Rb)2- ou -O-, soit B conjointement avec A ou Z peut être représenté par -C=C(Rb)-, -C(Rb)=C-, -CH2-CH(Rb)- ou-CH(Rb)-CH2-; D représente -O- ou -S(O)m,-; E représente une liaison ou -(CH2)n-, -N(Rd)-, -(CH2)nN(Rd)- ou -N(Rd)(CH2)n-; F représente -C(=X)-; G représente -(CH2)n-, -N(Rd)-, -(CH2)nN(Rd)- ou -N(Rd)(CH2)n; J représente une liaison, -O-, -N(RC)C(=X)-, -C(=X)N(Rc)-, -S(O)m,-, -N(Rc)S(O)m-, -S(O)nN(Rc)-, -N(Re)- ou -N(Rg)(Rh); K représente une liaison, alkylène, cycloalkylène, cycloalcénylène, arylène, hétérocycloalkylène, hétérocycloalkylène ou hétéroarylène; et L représente hydrogène ou un groupe terminal.