144035-83-6Relevant academic research and scientific papers
Cancer treatment method
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, (2008/06/13)
The invention relates to a method for treating cancer including administering to a mammal therapeutically effective amounts of an anti-neoplastic agent and a PDE4 inhibitor, treatment combinations containing the same as well as a method for attenuating unwanted cancer treatment side effects including myelosuppression and mucositis.
COMPOUNDS CONTAINING PHENYL LINKED TO ARYL OR HETEROARYL BY AN ALIPHATIC- OR HETEROATOM-CONTAINING LINKING GROUP
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, (2008/06/13)
This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase
Process development of the PDE IV inhibitor 3-(cyclopentyloxy)-n-(3,5-dichloropyrid-4-yl)-4-methoxybenzamide
Cook, David C.,Jones, Ronald H.,Kabir, Humayun,Lythgoe, David J.,McFarlane, Ian M.,Pemberton, Clive,Thatcher, Alan A.,Thompson, David M.,Walton, John B.
, p. 157 - 168 (2013/09/08)
Development of an industrial process for 3-(cyclopentyloxy)-N-(3,5-dichloropyrid-4-yl)-4-methoxybenzamide, a potent PDE IV type inhibitor, is described. The rapid identification of scalable reaction conditions allowed pilot-scale synthesis of kilogramme quantities for early clinical evaluation. However, as more compound was demanded, better reaction conditions were required in the interests of safety, economics, and environmental impact. This led to the derivation of a high-yielding and very robust procedure which included various safeguards to ensure that high-quality product was obtained and that new trace impurities were effectively removed. The large-scale oxidation of a benzaldehyde derivative to the corresponding benzoic acid using hydrogen peroxide under aqueous alkaline conditions is described.
Compounds containing phenyl linked to aryl or heteroaryl by an aliphatic-or heteroatom-containing linking group
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, (2008/06/13)
This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.
Selective Type IV Phosphodiesterase Inhibitors as Antiasthmatic Agents. The Syntheses and Biological Activities of 3-(Cyclopentyloxy)-4-methoxybenzamides and Analogues
Ashton, Michael J.,Cook, David C.,Fenton, Garry,Karlsson, Jan-Anders,Palfreyman, Malcolm N.,et al.
, p. 1696 - 1703 (2007/10/02)
The syntheses and biological activities of a number of benzamide derivatives, designed from rolipram, which are selective inhibitors of cyclic AMP-specific phosphodiesterase (PDE IV), are described.The effects of changes to the alkoxy groups, amide linkag
PHENYLCARBOXAMIDE COMPOUNDS WHICH HAVE USEFUL PHARMACEUTICAL ACITVITY
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, (2008/06/13)
Compounds of formula (1) are described wherein Y represents a halogen atom or a group -OR1 where R1 represents an optionally substituted alkyl group; R2 represents an optionally substituted cyclonlkylcycloalkeny1 or polycycloalkyl group; R3 represents a hydrogen atom or an alkyl, aryl or aralkyl group; R4 represents an aryl or heteroaryl group; X represents -O-, -S-, -CH2- or -N(R5)-, where RS is a hydrogen atom or an alkyl group; n is zero or an integer or value 1, 2 or 3; and the salts, solvates and hydrates thereof. The compounds are selective phosphodiesterase IV inhibitors and are useful for the prophylaxis or treatment of inflammatory diseases
