Some content of this application is unavailable at the moment.
If this situation persist, please contact us atFeedback&Contact
1. (WO1997018206) MORPHOLINE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1997/018206 International Application No.: PCT/GB1996/002766
Publication Date: 22.05.1997 International Filing Date: 13.11.1996
Chapter 2 Demand Filed: 25.04.1997
IPC:
C07D 413/04 (2006.01) ,C07D 417/04 (2006.01)
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
04
directly linked by a ring-member-to-ring- member bond
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
04
directly linked by a ring-member-to-ring- member bond
Applicants:
MERCK SHARP & DOHME LIMITED [GB/GB]; Hertford Road Hoddesdon Hertfordshire EN11 9BU, GB (AllExceptUS)
SWAIN, Christopher, John [GB/GB]; GB (UsOnly)
TEALL, Martin, Richard [GB/GB]; GB (UsOnly)
WILLIAMS, Brian, John [GB/GB]; GB (UsOnly)
Inventors:
SWAIN, Christopher, John; GB
TEALL, Martin, Richard; GB
WILLIAMS, Brian, John; GB
Agent:
HISCOCK, Ian, James; Merck & Co., Inc. European Patent Dept. Terlings Park Eastwick Road Harlow, Essex CM20 2QR, GB
Priority Data:
9523244.314.11.1995GB
Title (EN) MORPHOLINE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS
(FR) DERIVES DE LA MORPHOLINE ET LEUR UTILISATION COMME AGENTS THERAPEUTIQUES
Abstract:
(EN) The present invention relates to compounds of formula (I) wherein X is a 5- or 6-membered C-linked heteroaromatic ring containing 1 to 4 nitrogen atoms and optionally containing in the ring one oxygen or sulphur atom; Y is a group of the formula -(CH2)nNR6R7, or a methylene- or ethylene-linked imidazolyl group; Z is hydrogen or C1-4alkyl optionally substituted by a hydroxy group; R1, R2, R3, R4, R5, R9a and R9b are a variety of substituents; R6 is hydrogen, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, phenyl, or C2-4alkyl substituted by C1-4alkoxy or hydroxy; R7 is hydrogen, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, phenyl, or C2-4alkyl substituted by one or two substituents selected from C1-4alkoxy, hydroxy or a 4-, 5- or 6-membered heteroaliphatic ring containing one or two heteroatoms selected from N, O and S; or R6 and R7, together with the nitrogen atom to which they are attached, form a saturated or partially saturated heterocyclic ring or a non-aromatic azabicyclic ring system; and n is zero, 1 or 2; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherapeutic neuralgia.
(FR) L'invention concerne des composés de la formule (I). Dans cette formule, X est un cycle hétéroaromatique à liaison carbone de 5 à 6 éléments et contenant de 1 à 4 atomes d'azote, ainsi qu'éventuellement un atome d'oxygène ou de soufre; Y est un groupe de la formule -(CH2)nNR6R7 ou un groupe imidazolyle à liaison méthylène ou éthylène: Z est un hydrogène ou un alkyle C1-4, éventuellement substitué par un groupe hydroxy; R1, R2, R3, R4, R5, R9a et R9b sont différents substituants; R6 est un hydrogène, alkyle C1-6, cycloalkyle C3-7, cycloalkyl C3-7 alkyle C1-4, phényle ou alkyle C2-4, substitué par alcoxy C1-4 ou hydroxy; R7 est un hydrogène, alkyle C1-6, cycloalkyle C3-7, cycloalkyl C3-7 alkyle C1-4, phényle ou alkyle C2-4 substitué par un ou deux substituants choisis parmi alcoxy C1-4, hydroxy ou un cycle hétéroaliphatique à 4, 5 ou 6 éléments, renfermant un ou deux hétéroatomes choisis parmi N, O et S; ou R6 et R7 forment ensemble et avec l'atome d'azote auquel ils sont liés, un hétérocycle saturé ou partiellement saturé, ou encore un système non aromatique azabicylique; et n est égal à zéro, 1 ou 2. L'invention concerne également les sels de ces composés acceptables sur le plan pharmaceutique. Ces composés sont particulièrement utiles dans le traitement ou la prévention de douleurs, d'inflammations, de migraines, de vomissements ou d'algies post-zostériennes.
Designated States: AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CU, CZ, DE, DK, EE, ES, FI, GB, GE, HU, IL, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, TJ, TM, TR, TT, UA, UG, US, UZ, VN
African Regional Intellectual Property Organization (ARIPO) (KE, LS, MW, SD, SZ, UG)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
EP0861251US5968934JP2000500154CA2235855AU1996075786