Abstract: The invention relates to (hetero)arylsulfonylamino based peptidomimetics of formula (I), wherein R1, R2, R3, A, B, D, Q, k and n are defined as disclosed, or a pharmaceutically acceptable salt or ester thereof. Compounds of formula (I) possess high affinity and selectivity for the somatostatin receptor subtypes SSTR1 and/or SSTR4 and can be used for the treatment or diagnosis of diseases or conditions wherein an interaction with SSTR1 and/or SSTR4 is indicated to be useful.

Abstract: The invention relates to (hetero)arylsulfonylamino based peptidomimetics of formula (I), wherein A, D, E, J, Q1 R1, R2, R3, p and j are defined as disclosed, or a pharmaceutically acceptable salt or ester thereof. Compounds of formula (I) possess high affinity and selectivity for the somatostatin receptor subtypes sst1 and/or sst4 and can be used for the treatment or diagnosis of diseases or conditions wherein sst1 and/or sst4 agonists or antagonists are indicated to be useful.

Abstract: The invention relates to (hetero)arylsulfonylamino based peptidomimetics of formula (I), wherein R1, R2, R3, A, B, D, Q, k and n are defined as disclosed, or a pharmaceutically acceptable salt or ester thereof. Compounds of formula (I) possess high affinity and selectivity for the somatostatin receptor subtypes SSTR1 and/or SSTR4 and can be used for the treatment or diagnosis of diseases or conditions wherein an interaction with SSTR1 and/or SSTR4 is indicated to be useful.

Abstract: The invention relates to 1-naphthalenesulfonylamino based peptidomimetics of formula (I), wherein B, R1 and R2 are as defined in the claims, and pharmaceutically acceptable salts thereof. Compounds of formula (I) possess high affinity and selectivity for the somatostatin receptor subtype SSTR4 or the somatostatin receptor subfamily SSTR1/SSTR4.

Abstract: The invention relates to (hetero)arylsulfonylamino based peptidomimetics of formula (I), wherein R1, R2, R3, A, B, D, Q, k and n are defined as disclosed, or a pharmaceutically acceptable salt or ester thereof. Compounds of formula (I) possess high affinity and selectivity for the somatostatin receptor subtypes SSTR1 and/or SSTR4 and can be used for the treatment or diagnosis of diseases or conditions wherein an interaction with SSTR1 and/or SSTR4 is indicated to be useful.

Abstract: A compound of formula I, 1

Abstract: A compound of formula I, wherein A, Ra, Rb, R1 to R5, m and t are as defined as disclosed, or a pharmaceutically acceptable salt or ester thereof, useful as an alpha-2 antagonist. The compounds I can be used for the treatment of diseases or conditions where alpha-2 antagonists are indicated to be effective.

Abstract: A compound, suitable as an alpha-2B-adrenoceptor antagoist, having a structure of formula (I) 1

Abstract: A method for the treatment or prevention of a disease mediated by the alpha-2B-adrenoceptor in a mammal. The method includes administering to the mammal an effective amount of a selective (alpha-2B-adrenoceptor antagonist, where the antagonist is a compound selected from the group consisting of compounds A, B, C, D and E disclosed in Scheme I, or a pharmaceutically acceptable salt of the compound.

Abstract: Imidazole derivatives of formula I wherein n is 0 or 1, R1 is hydrogen or C1-C4-alkyl, R2 is hydrogen or R2 and R3 together form a double bond, R3 is hydrogen or C1-C4-alkyl or R2 and R3 together form a double bond, R4 is hydrogen, C1-C4-alkyl, hydroxy or C1-C4-alkoxy, R5 is hydrogen or C1-C4-alkyl or R4 and R5 together with the carbon atom to which they are attached form a carbonyl group, R6, R7 and R8 are each the same or different and are independently hydrogen, C1-C4-alkyl or C2-C4-alkenyl, C3-C7-cycloalkyl, hydroxy, C1-C4-alkoxy, C1-C4-hydroxyalkyl, thiol, C1-4-alkylthio, C1-4-alkylthiol, halogen, trifluoromethyl, nitro or optionally substituted amino, X is —CHR9—(CHR10)m—, m is 0 or 1, and R9 and R10 are each the same or different and are independently hydrogen or C1-C4-alkyl; or a pharmaceutically acceptable ester or salt thereof, their preparation, use and pharmaceutical compositions comprising them are described.

Abstract: The present invention relates to a method for the treatment or prevention of a disease mediated by the alpha-2B-adrenoceptor in a mammal. Said method comprises administering to said mammal an effective amount of a selective alpha-2B-adrenoceptor antagonist, wherein said antagonist is a compound selected from the group consisting of compounds A, B, C, D and E disclosed in Scheme I, or a pharmaceutically acceptable salt of said compound.

Abstract: Imidazole derivatives of formula I 1

Abstract: A compound of formula I, 1

Abstract: Imidazole derivatives of formula (I) wherein n is 0 or 1, R1 is hydrogen or C1-C4-alkyl, R2 is hydrogen or R2 and R3 together form a double bond, R3 is hydrogen or C1-C4-alkyl or R2 and R3 together form a double bond, R4 is hydrogen, C1-C4-alkyl, hydroxy or C1-C4-alkoxy, R5 is hydrogen or C1-C4-alkyl or R4 and R5 together with the carbon atom to which they are attached form a carbonyl group, R6, R7 and R8 are each the same or different and are independently hydrogen, C1-C4-alkyl or C2-C4-alkenyl, C3-C7-cycloalkyl, hydroxy, C1-C4-alkoxy, C1-C4-hydroxyalkyl, thiol, C1-4-alkylthio, C1-4-alkylthiol, halogen, trifluoromethyl, nitro or optionally substituted amino, X is —CHR9—(CHR10)m—, m is 0 or 1, and R9 and R10 are each the same or different and are independently hydrogen or C1-C4-alkyl; or a pharmaceutically acceptable ester or salt thereof, their preparation, use and pharmaceutical compositions comprising them are described.

Abstract: The levo-isomers of certain imidazole derivatives, particularly medetomidine, have been found to be inverse agonists of adrenergic .alpha.-2 receptors and are therefore useful in the prevention or treatment of conditions associated with overexpression or hypersensitization of the adrenergic .alpha.-2 receptors, such as obesity, a withdrawal symptom to an adrenergic .alpha.-2 receptor agonist, a neurological disorder, multiple system atrophy, diabetes mellitus, benign prostatic hyperplasia, and drug-induced sensitization of adrenergic .alpha.-2 receptors. The pharmaceutical composition is preferably transdermal.