- PROCESS FOR THE PREPARATION OF PIPERAZINYL AND DIAZEPANYL BENZAMIDE DERIVATIVES
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The present invention is directed to a novel process for the preparation of piperazinyl and diazapanyl benzamide derivatives, useful for the treatment of disorders and conditions mediated by a histamine receptor, preferably the H3 receptor.
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Page/Page column 61
(2008/12/06)
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- NOVEL COMPOUNDS
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There is provided a compound of formula (I): or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.
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Page/Page column 117
(2008/12/06)
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- 1-Alkyl-4-acylpiperazines as a new class of imidazole-free histamine H 3 receptor antagonists
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With the aim of identifying structurally novel, centrally acting histamine H3 antagonists, arrays of monoacyldiamines were screened. This led to the discovery of a series of 1-alkyl-4-acylpiperazines which were potent antagonists at the human histamine H3 receptor. The most potent amides had antagonist potencies in the subnanomolar range.
- Zaragoza, Florencio,Stephensen, Henrik,Knudsen, Sanne M.,Pridal, Lone,Wulff, Birgitte S.,Rimvall, Karin
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p. 2833 - 2838
(2007/10/03)
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- Antiatherosclerotic and antithrombotic 1-benzopyran-4-ones and 2-amino-1,3-benzoxazine-4-ones
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This invention relates to compounds of Formula I STR1 which are useful in association with a pharmaceutical carrier as antiatherosclerotic agents. In addition, various compounds of Formula I are useful inhibitors of cell proliferation.
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- Use of 2-Oxazolidinones As Latent Aziridine Equivalents. III. Preparation of N-Substituted Piperazines.
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A number of N-aryl and N-alkyl substituted piperazines 1 were prepared from variously substituted 2-oxazolidinone derivatives 3.The method involved treatment of 3 with HBr in glacial acetic acid followed by heating the resulting ring-opened salts 5 in alcoholic solvent.The piperazines 1a-1q were isolated by crystallization in yields ranging from 23-91percent.
- Poindexter, Graham S.,Bruce, Marc A.,LeBoulluec, Karen L.,Monkovic, Ivo
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p. 7331 - 7334
(2007/10/02)
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- Antiatherosclerotic and antithrombotic 2-amino-6-phenyl-4H-pyran-4-ones
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This invention relates to compounds of Formula I STR1 which are useful as antiatherosclerotic agents and inhibitors of cell proliferation for the treatment of proliferative diseases. In addition, various compounds of Formula I are useful inhibitors of platelet aggregation.
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- 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinolinecarboxylic acids and antibacterial agents containing them
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An antibacterial 1-cyclopropyl-6-fluoro-1,4- dihydro-4-oxo-7-(1-piperazinyl)-3-quinolinecarboxylic acid of the formula STR1 in which R represents branched or straight-chain propyl or butyl which is optionally substituted by hydroxy or methoxy, unsubstituted tert.-butyl, 2-methylthioethyl, trifluoromethylthiomethyl, 2-trifluoromethylthioethyl, cycloalkyl with 3 to 6 carbon atoms, cycloalkenyl having 5 to 6 carbon atoms optionally substituted by hydroxyl, 1,1-dioxidotetrahydrothiophen-3-yl, cyclopropylmethyl, 1-phenethyl, furylmethyl, allyl or propargyl optionally substituted by phenyl and their pharmaceutically usable hydrates, acid addition salts, metal and guanidinium salts and prodrug forms.
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