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AssigneeJames Black Foundation Limited
InventorsSarkis Barret Kalindjian, Ildiko Maria Buck, Caroline Minli Rachel Low, Matthew John Tozer
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Compounds of formula (I) and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors. X and Y are independently ═N—, —N(R5)—(R5 being selected from H, Me, Et, Pr, Bn, OH and —CH2COOR6, wherein R6 represents H, Me, Et, Pr or Bn), ═CH—, —O— or —S—; n is from 1 to 4; A is an optionally substituted 5- or 6-membered carbocyclic ring wherein (a) 1 or 2 C atoms may optionally be replaced by N, O and/or S atoms, (b) A is fused with the aromatic group in formula (I) to form a fused bicycle, and (c) the ring containing X and Y is linked to a C atom of A; R1 is H or C1 to C15 hydrocarbyl wherein up to three C atoms may optionally be replaced by N, O and/or S atoms and up to three H atoms may optionally be replaced by halogen atoms; R2 is selected from H, Me, Et, Pr and OH, each R2 being independently selected from H, Me, Et, Pr and OH when n is greater than 1; R3 (when n is 1) is selected from H, Me, Et and Pr; or (when n is greater than 1) each R3 is independently selected from H, Me, Et and Pr, or two R3 groups on neighbouring carbn atoms are linked to form a C3 to C6 carbocylic ring, or two R3 groups are absent from neighbouring carbon atoms which are linked by a double bond; or R2 and R3 on the same carbon atom together represent an ═O group; R4 is C1 to C15 hydrocarbyl wherein up to two C atoms may optionally be replaced by N, O and/or S atoms and up to three H atoms may optionally be replaced by halogen atoms; V is —CO—NH—SO2—Ph, —SO2—NH—CO—Ph, —CH2OH, or a group of the formula —R7U, (wherein U is —COOH, tetrazolyl, —CONHOH or —SO3H; and R7 is a bond; C1 to C6 hydrocarbylene, optionally substituted by hydroxy, amino or acetamido; —O—(C1 to C3 alkylene)—; —SO2NR8—CHR9—; —CO—NR8—CHR9—, R8 and R9 being independently selected from H and methyl; or —NH—(CO)c—CH2, c being 0 or 1); or a pharmaceutically acceptable salt thereof. Compositions comprising a compound a formula (I) are also described. 1
A compound of formula (I)
A compound according to any preceding claim wherein X is ═NH— and Y is —NH—, or vice versa.
A compound according to any preceding claim wherein R1 is C3 to C12 alicyclic;
A compound according to any preceding claim wherein R1 is cyclohexyl or bicyclooctyl.
A compound according to any preceding claim wherein V is —CO—NH—SO2—Ph, —SO2—NH—CO—Ph, —OCH2COOH, tetrazolyl or (CH2)sCOOH, wherein s is from 0, 1 or 2.
A compound according to any preceding claim wherein V is CH2COOH, COOH or tetrazolyl.
A compound according to any preceding claim wherein R2 and R3 are H, and n is from 1 to 3.
A compound according to any preceding claim wherein R2 and R3 together form an ═O group and n is 1.
A compound according to any preceding claim wherein R4 is C3 to C15 carbocyclic.
A compound which is degraded in vivo to yield a compound according to any one of the preceding claims.
A method of making a compound according to formula (Ia) wherein
A product containing as first active ingredient a compound of formula (I) and as second active ingredient a proton pump inhibitor, as a combined preparation for simultaneous, separate or sequential use in the treatment of patients suffering from gastrointestinal disorders.
Use of a proton pump inhibitor for the preparation of a medicament for the treatment of gastrointestinal disorders, said treatment comprising the simultaneous or sequential administration of said proton pump inhibitor and a compound of formula (I), wherein said proton pump inhibitor enhances the effect of the compound of formula (I) on gastrin-related disorders in patients suffering from gastrointestinal disorders.
Use of a compound of formula (I) for the preparation of a medicament for the treatment of gastrointestinal disorders, said treatment comprising the simultaneous or sequential administration of said proton pump inhibitor and a compound of formula (I), wherein said compound of formula (I) enhances the effect of the proton pump inhibitor on the reduction of acid secretion in patients suffering from gastrointestinal disorders.
Use of a compound of formula (I) for the preparation of a medicament for reducing adverse effects associated with administration of proton pump inhibitors in patients suffering from gastrointestinal disorders.
Use of a proton pump inhibitor for the preparation of a medicament for reducing adverse effects associated with administration of a compound of formula (I) in patients suffering from gastrointestinal disorders.
Dependencies are inferred from the claim text.