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Pub. No.:    WO/2000/027823    International Application No.:    PCT/GB1999/003733
Publication Date: 18.05.2000 International Filing Date: 09.11.1999
Chapter 2 Demand Filed:    24.05.2000    
C07D 207/34 (2006.01), C07D 233/54 (2006.01), C07D 233/88 (2006.01), C07D 233/90 (2006.01), C07D 263/34 (2006.01), C07D 277/56 (2006.01), C07D 401/04 (2006.01), C07D 401/12 (2006.01), C07D 403/04 (2006.01), C07D 403/06 (2006.01), C07D 403/12 (2006.01), C07D 405/04 (2006.01)
Applicants: JAMES BLACK FOUNDATION LIMITED [GB/GB]; 68 Half Moon Lane Dulwich London SE24 9JE (GB) (For All Designated States Except US).
KALINDJIAN, Sarkis, Barret [GB/GB]; (GB) (For US Only).
BUCK, Ildiko, Maria [GB/GB]; (GB) (For US Only).
LINNEY, Ian, Duncan [GB/GB]; (GB) (For US Only).
WRIGHT, Paul, Trevor [GB/GB]; (GB) (For US Only).
McDONALD, Iain, Mair [GB/GB]; (GB) (For US Only).
STEEL, Katherine, Isobel, Mary [GB/GB]; (GB) (For US Only).
HULL, Robert, Antony, David [GB/GB]; (GB) (For US Only).
ROBERTS, Sonia, Patricia [GB/GB]; (GB) (For US Only).
GAFFEN, John, David [GB/GB]; (GB) (For US Only).
VINTER, Jeremy, Gilbert [GB/GB]; (GB) (For US Only).
WALKER, Martin, Keith [GB/GB]; (GB) (For US Only).
BLACK, James, Whyte [GB/GB]; (GB) (For US Only).
WATT, Gillian, Fairfull [GB/GB]; (GB) (For US Only).
HARPER, Elaine, Anne [GB/GB]; (GB) (For US Only).
SHANKLEY, Nigel, Paul [GB/GB]; (GB) (For US Only).
TOZER, Matthew, John [GB/GB]; (GB) (For US Only).
DUNSTONE, David, John [GB/GB]; (GB) (For US Only).
PETHER, Michael, John [GB/GB]; (GB) (For US Only).
LILLEY, Elliot, James [GB/GB]; (GB) (For US Only).
SYKES, David, Andrew [GB/GB]; (GB) (For US Only).
LOW, Caroline, Minli, Rachel [GB/GB]; (GB) (For US Only).
GRIFFIN, Eric, Peter [GB/GB]; (GB) (For US Only).
WRIGHT, Laurence [GB/GB]; (GB) (For US Only)
Inventors: KALINDJIAN, Sarkis, Barret; (GB).
BUCK, Ildiko, Maria; (GB).
LINNEY, Ian, Duncan; (GB).
WRIGHT, Paul, Trevor; (GB).
McDONALD, Iain, Mair; (GB).
STEEL, Katherine, Isobel, Mary; (GB).
HULL, Robert, Antony, David; (GB).
ROBERTS, Sonia, Patricia; (GB).
GAFFEN, John, David; (GB).
VINTER, Jeremy, Gilbert; (GB).
WALKER, Martin, Keith; (GB).
BLACK, James, Whyte; (GB).
WATT, Gillian, Fairfull; (GB).
HARPER, Elaine, Anne; (GB).
SHANKLEY, Nigel, Paul; (GB).
TOZER, Matthew, John; (GB).
DUNSTONE, David, John; (GB).
PETHER, Michael, John; (GB).
LILLEY, Elliot, James; (GB).
SYKES, David, Andrew; (GB).
LOW, Caroline, Minli, Rachel; (GB).
GRIFFIN, Eric, Peter; (GB).
WRIGHT, Laurence; (GB)
Agent: FISHER, Adrian, John; Carpmaels & Ransford 43 Bloomsbury Square London WC1A 2RA (GB)
Priority Data:
9824536.8 09.11.1998 GB
9916786.8 16.07.1999 GB
Abstract: front page image
(EN)Compounds of formula (I) and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors. X and Y are independently =N-, -N(R?5¿)- =CH-, -S- or -O-. n is from 1 to 4; R?1¿ is H or C¿1? to C¿15? hydrocarbyl R?2¿ is selected from H, Me, Et, Pr and OH, R¿3? is selected from H, Me, Et and Pr; or (when n is greater than 1) each R?3¿ is independently selected from H, Me, Et and Pr, or two R?3¿ groups on neighbouring carbon atoms are linked to form a C¿3? to C¿6? carbocylic ring, or R?2¿ and R?3¿ on the same carbon atom together represent an =O group; R?4¿ is C¿1? to C¿15? hydrocarbyl Z is -(NR?7¿)¿a?-CO-(NR?8¿)¿b?- (wherein a is 0 or 1, b is 0 or 1, -CO-NR?7¿-CH¿2?-CO-NR?8¿-, -CO-O-, -CH¿2?-CH¿2?-, -CH=CH-, -CH¿2?-NR?8¿- or a bond; Q is -R?9¿V, or (II), (wherein R?9¿ is -CH¿2?-; -CH¿2?-CH¿2?-; or (III), R?9¿ and R?8¿, together with the nitrogen atom to which R?8¿ is attached, form a piperidine or pyrrolidine ring which is substituted by V; V is -CO-NH-SO¿2?-Ph, -SO¿2?-NH-CO-Ph, -CH¿2?OH, or a group of the formula -R?10¿U, (wherein U is -COOH, tetrazolyl, -CONHOH- or -SO¿3?H; and R?10¿ is a bond; C¿1? to C¿6? hydrocarbylene, -O-(C¿1? to C¿3? alkylene)-; -SO¿2?NR?11¿-CHR?12¿-; -CO-NR?11¿-CHR?12¿-, or -NH-(CO)¿c?-CH¿2?-, c being 0 or 1).
(FR)L'invention concerne des composés de formule (I), ainsi que leurs sels pharmaceutiquement acceptables, dans laquelle X et Y sont indépendamment =N-, -N(R?5¿)-, =CH-, -S- ou -O-; n est compris entre 1 et 4; R?1¿ est H ou hydrocarbyle C¿1?-C¿15?; R?2¿ est choisi entre H, Me, Et, Pr et OH; R?3¿ est choisi entre H, Me, Et et Pr, ou bien (quand n est supérieur à 1) chaque R?3¿ est choisi indépendamment entre H, Me, Et et Pr, ou bien deux groupes R?3¿ portés par des atomes de carbone adjacents sont liés de façon à former un anneau carbocyclique C¿3?-C¿6?, ou bien R?2¿ et R?3¿ portés par le même carbone représentent ensemble un groupe =O; R?4¿ est hydrocarbyle C¿1?-C¿15?; Z est -(NR?7¿)¿a?-CO-(NR?8¿)¿b?- (où a est 0 ou 1, b est 0 ou 1, CO-NR?7¿-CH¿2?-CO-NR?8¿-, -CO-O-, -CH¿2?-CH¿2?-, -CH=CH-, -CH¿2?-NR?8¿- ou une liaison); Q est -R?9¿V ou (II) (où R?9¿ est -CH¿2?-; -CH¿2?-CH¿2?-, ou (III), ou bien R?9¿ et R?8¿, avec l'atome d'azote sur lequel est fixé R?8¿, forment un anneau pipéridine ou pyrrolidine substitué par V; V est -CO-NH-SO¿2?-Ph, -SO¿2?-NH-CO-Ph, -CH¿2?OH ou un groupe de formule -R?10¿U (où U est -COOH, tétrazolyle, -CONHOH- ou -SO¿3?H; et R?10¿ est une liaison, hydrocarbylène C¿1?-C¿6?, -O-(alkylène C¿1?-C¿3?)-, -SO¿2?NR?11¿-CHR?12¿-, -CO-NR?11¿-CHR?12¿- ou -NH-(CO)¿c?-CH?2¿-, c étant 0 ou 1). Ces composés et leurs sels sont des ligands des récepteurs de la gastrine et de la cholécystokinine.
Designated States: AE, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CR, CU, CZ, DE, DK, DM, EE, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, TZ, UA, UG, US, UZ, VN, YU, ZA, ZW.
African Regional Intellectual Property Organization (GH, GM, KE, LS, MW, SD, SL, SZ, TZ, UG, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, CY, 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, GW, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)