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US 6,271,229 B1Granted
Method of treating gastrointestinal motility disorders
AssigneeNovo Nordisk A/S
InventorBeverley Greenwood
Life of this patent
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Abstract
The present invention relates to a novel method for treating a mammal suffering from gastrointestinal motility disorders.
Claims11
A method of treating a gastrointestinal hypermotility disorder in a subject in need thereof comprising administering to said subject an effective amount of a compound of formula I
- wherein
- X is oxygen or sulphur;
- R is hydrogen, amino, halogen, —CHO, —NO2, —R4, —Y, —NHCO—R4, —OR4, —SR4, —SOR4, —SO2R4, C3-10-cycloalkyl, C4-10-cycloalkenyl, C4-10-(cycloalkylalkyl), —Z1—C3-10-cycloalkyl, —Z1—C4-10-cycloalkenyl, —Z1—C4-10-(cycloalkylalkyl), —Z1—C4-10-(cycloalkenylalkyl), —Z1—C4-10-(methylenecycloalkylalkyl), —NH—R4, —NR4R5, —NH—OR4, —CH═NOR4, or an aromatic ring selected from the group consisting of phenyl, benzyloxycarbonyl, phenoxy, benzoyl, tetrahydronaphthyl, naphtyl, and indenyl, wherein each aromatic ring is optionally substituted with halogen, —NO2, —CN, C1-4-alkyl, C1-4-alkoxy, —OCF3, —CONH2, —CSNH2, phenoxy or phenyl;
- or R is —Z1—R6—Z2—R5, —Z1—R6—Z2—R7—Z3—R5, —Z1—CO—R5, —Z1—R6—CO—R5, —Z1—R6—CO2—R5, —Z1—R6—O2C—R5, —Z1—R6—CONH—R5, —Z1—R6—NHCO—R5, —Z1—R6—Y, —Z1—R6—Z2—Y, wherein Z1 and Z2 independently are oxygen or sulphur, and R4 and R5 independently are straight or branched C1-15-alkyl, straight or branched C2-15-alkenyl, straight or branched C2-15-alkynyl, each of which is optionally substituted with one or more halogen(s), C1-6-alkoxy, —CF3, —CN, —COOH, —OH, —NH2, C1-6-alkyl ester, —SH, —NHR4, —NR4R5, or a phenyl or phenoxy group, wherein the phenyl or phenoxy group is optionally substituted with halogen, —NO2, —CN, C1-4-alkyl, C1-4-alkoxy, —OCF3, —CONH2, —CSNH2, phenyl or phenoxy, and wherein R6 and R7 independently are straight or branched C1-10-alkylene, straight or branched C2-10-alkenylene, straight or branched C2-10-alkynylene, each of which is optionally substituted with one or more halogen(s), —CF3, —CN, —COOH, —OH, —NH2, C1-6-alkyl ester, —SH, —NHR4, —NR4R5, phenyl or phenoxy, and Y is a heterocyclic group selected from the group consisting of thienyl, tetrazolyl, thiadiazolyl, benzothiazolyl, phthalimido, pyridyl and 1,3-dioxolanyl wherein the heterocyclic group is optionally substituted at carbon or nitrogen atom(s) with straight or branched C1-6-alkyl, phenyl or benzyl, or a carbon atom of the heterocyclic group together with an oxygen atom form a carbonyl group;
- and
- G is an azabicyclic ring of formula II
- wherein
- the thiadiazole or oxadiazole ring is attached to any carbon atom of the azabicyclic ring;
- R1 and R2 may be present at any appropriate position of the thiadiazole or oxadiazole ring and independently are hydrogen, straight or branched C1-5-alkyl, straight or branched C2-5-alkenyl, straight or branched C2-5-alkynyl, straight or branched C1-10-alkoxy, —OH, halogen, —NH2, carboxy or straight or branched C1-5-alkyl substituted with —OH;
- m is 1;
- n is 2;
- p is 1;
- and
- is a single or double bond;
- or
- a pharmaceutically acceptable salt thereof.
13 more elements
Dependencies are inferred from the claim text.