Abstract: The present invention relates to a new process for the preparation of a crystalline polymorph of a vasopressin V2 agonist.

Abstract: The invention provides a new polymorph of 1-(2-methyl-4-(2,3,4,5-tetrahydro-1-benzazepin-1-ylcarbonyl)benzyl-carbamoyl)-L-proline-N,N-dimethylamide, pharmaceutical compositions containing it and its use in therapy.

Abstract: The invention provides cyclopropanecarboxylic acid 4-(6-chloro-3-methyl-4,10-dihydro-3H-2,3,4,9-tetraazabenzo[f]azulene-9-carbonyl)-2-fluoro-benzylamide para-toluenesulphonate, pharmaceutical compositions containing it, and its use in therapy.

Abstract: The present invention concerns compounds inter alia according to general formula 1a. Compounds according to the invention are vasopressin V1a receptor antagonists. Pharmaceutical compositions of the compounds are useful as treatment of dysmenorrhoea.

Abstract: The present invention concerns compounds, according to general formula (I), which find utility preferably for the treatment of cancer.

Abstract: The invention concerns compounds according to general formulae 1, wherein G1 is an amine. Compounds according to the invention are vasopressin V2 receptor agonists. Pharmaceutical compositions of the compounds are useful as antidiuretic agents.

Abstract: Compounds of general formula 1, or a pharmaceutically acceptable salt thereof, wherein R1 is selected from H, lower alkyl, R4—CO, R4—O2CCH2, R5—OCO and R5—SO2; R2 is selected from lower alkyl, cycloalkyl optionally substituted with an alkyl or alkyloxy group, (C5-C12)cycloalkylalkyl optionally substituted with an alkyl or alkyloxy group, aralkyl optionally substituted with up to three groups chosen from F, Cl, Br, I, OH, lower alkyl, O-(lower alkyl), O-benzyl, NH2, NO2, NH-acyl, CN and CF3, and aralkyloxymethyl optionally substituted with up to three groups chosen from F, Cl, Br, OH, lower alkyl and O-(lower alkyl); or R1 and R2 together are an o-xylylene group optionally substituted on the aromatic ring with a group selected from F, Cl, Br, OH, lower alkyl and O-(lower alkyl); R3 is selected from H, OH and O-lower alkyl; R4 is selected from H, lower alkyl and phenyl; and R5 is selected from lower alkyl, phenyl and benzyl. The compounds are useful as pharmaceutical compositions.

Abstract: This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, V1 and V2 are both H, OMe or F, or one of V1 and V2 is Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N3, NH2, NHBn or NH-acyl and the other is H, or V1 and V2 together are ?O, —O(CH2)pO— or —S(CH2)pS—; W1 is either O or S; X1 and X2 are both H, or together are ?O or ?S; Y is OR5 or NR6R7; R1, R2, R3 and R4 are independently selected from H, lower alkyl, lower alkyloxy, F, Cl and Br; R5 is selected from H and lower alkyl; R6 and R7 are independently selected from H and lower alkyl, or together are —(CH2)n—; n=3, 4, 5, 6; and p is 2 or 3. The compounds are agonists at the vasopressin V2 receptor and are useful as antidiuretics and procoagulants. The invention further comprises pharmaceutical compositions incorporating these vasopressin agonists, which compositions are particularly useful in the treatment of central diabetes insipidus, nocturnal enuresis and nocturia.