Novo Nordisk A/s

High Point Pharmaceuticals, LLC

Novo Nordiskals

Novo Nordish A/s

Rolf Hohlweg

Knud Erik Andersen

Uffe Bang Olsen

Tine Krogh Jo Slashedrgensen

Peter Madsen

Zdenek Polivka

Henrik Sune Andersen

Karel Sindelar

Alexandra Silhankova

Otylie Konigova

Martina Kovandova

Vladimir Valenta

Erik Fischer

Svend Treppendahl

Frantisek Miksik

Jane Marie Lundbeck

Brett Watson

Tine Krogh J&oslash;rgensen

Silhankova Alexandra

Polivka Zdenek

Florenzio Zaragossa Dorwald

Florencio Zaragoza Dorwald

Erik B Nielsen

Sindelar Karel

Bernd Peschke

Inge Thoger Christensen

Erling Guddal

Florenzio Zaragossa D&ouml;rwald

Silh&aacute;nkov&aacute; Alexandra

Sindel&aacute;r Karel

Kaler Sindelar

Zden&eacute;k Polivka

Nils Langeland Johansen

Florencio Zaragoza Dörwald

Jan Lindy Sorensen

Polivka Zden&eacute;k

Enud Erik Andersen

Christian Thomsen

Philip Just Larsen

Joel Martin

Johannes Cornelis De Jong

Sidelar Karel

Tine Krogh Jorgensen

Tine Krough Jo Slashedrgensen

Tine Krogh Jo Slashedrgenen

Tomas Kalisz

Florenzio Zaragossa Do Slashedrwald

Christain Thomsen

Jan Lindy Sörensen

Novel compounds which interact with the histamine H3 receptor are defined. These compounds are particularly useful in the treatment of a variety of diseases or conditions in which histamine H3 interactions are beneficial. Thus, the compounds may find use, e.g., in the treatment of diseases of the central nervous system, the peripheral nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system. The novel compounds have a core consisting of a 6 membered aromatic ring containing at least one nitrogen atom and two carbon atoms in the ring and, at the remaining positions in the ring, there is either a carbon or a nitrogen atom.

Medicaments

Certain novel benzothiazoles and benzoxazoles, e.g., 2-(piperazin-1-yl)benzothiazoles and 2-(piperazin-1-yl)benzoxazoles, optionally substituted in the 3 and/or 4 positions of the piperazine rings, having histamine H3 antagonistic activity can be used in pharmaceutical compositions.

Benzothiazoles having histamine H3 receptor activity

Certain novel benzothiazoles and benzoxazoles, e.g., 2-(piperazin-1-yl)benzothiazoles and 2-(piperazin-1-yl)benzoxazoles, optionally substituted in the 3 and/or 4 positions of the piperazine rings,! of the general formula (1): having histamine H3 antagonistic activity can be used in pharmaceutical compositions.

3-(1,3-Benzodioxol-5-yl)-6-(4-cyclopropylpiperazin-1-yl)pyridazine and salts and solvates thereof, having histamine H3 antagonistic activity can be used in pharmaceutical compositions. 

3-(1,3-benzodioxol-5-yl)-6-(4-cyclopropylpiperazin-1-yl)-pyridazine, its salts and solvates and its use as histamine H3 receptor antagonist

Compound of formula (I) wherein W, X, Y, Z is &#x2014;C(R)&#x2550; or N; Ris hydrogen or alkyl, V is N or C (i.e. carbon), A is a bond or an alkylene linker with 1 to 3 carbon atoms, with the proviso that when A is a bond, V must be CH, R is ethyl, propyl, a branched Calkyl or a cyclic Calkyl, m and n is 1-3, D is heteroaryl optionally substituted with halogen, hydroxy, cyano, alkyl, cycloalkyl, alkoxy, &#x2014;(CH)&#x2014;(C&#x2550;O)&#x2014;NRR, or D is aryl optionally substituted with one or more of the groups independently selected from hydrogen, halogen, hydroxy, cyano, alkyl, cycloalkyl, haloalkyl, alkoxy, haloalkoxy, alkylsulfonyl, alkylsulfinyl, heterocyclyl, heterocyclylalkyl, heterocyclyl-alkoxy, heterocyclylcarbonyl, alkylcarbonyl, alkoxycarbonyl, alkylcarboxy, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, alkylcarbonylamino, alkylcarbonylaminoalkyl, arylcarbonylamino, aryl-carbonylaminoalkyl, heteroarylcarbonylamino or heteroarylcarbonylaminoalkyl, &#x2014;(CH)&#x2014;(C&#x2550;O)&#x2014;NRR, wherein o is 0-3, p is 0 or 1, and Rand Rindependently are hydrogen, alkyl or cycloalkyl; or Rand R, can together with the attached nitrogen form a heterocyclyl group, and salts and solvates thereof have binding affinity for the histamine H3 receptor. 

Heterocyclic H3 antagonists

6-(4-Cyclopropylpiperazin-1-yl)-2'-methyl-[3,4&#x2032;]bipyridinyl and salts and hydrates thereof interact with the histamine H3 receptor are defined.

6-(4-cyclopropylpiperazin-1-yl)-2'-methyl-[3, 4&#x2032;]-bipyridine and its uses as a medicament

The present invention relates, inter alia, to novel piperazines of the following formula: to the use of these compounds in the preparation of pharmaceutical compositions, to pharmaceutical compositions comprising the compounds, and to methods of treatment employing these compounds or compositions. The compounds show a high and selective binding affinity for the histamine H3 receptor, indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases or disorders related to the histamine H3 receptor.

Piperazines

Novel substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.

Substituted hexahydropyrrolo[1,2-a]pyrazines, octahydropyrido[1,2-a]-pyrazines and decahydropyrazino[1,2-a]azepines

Novel aminoazetidine, -pyrrolidine, and -piperidine derivatives, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.

Aminoazetidine,-pyrrolidine and -piperidine derivatives

N-substituted azaheterocyclic carboxylic acids and their use

N-Substituted azaheterocyclic compounds

Heterocyclic compounds

The present invention relates to the use of small organic compounds acting as opioid receptor ligands for the treatment of vasomotor disturbances. In particular the present invention relates to the use of triaza-spiro compounds of formula

1,3,8-triazaspiro&lsqb;4.5&rsqb;decanones with high affinity for opioid receptor subtypes

Growing community of inventors

Kvistgaard, Denmark

Rolf Hohlweg