7-¬carboxyalkyl or alkenyl|-6-¬alkyl or alkenyl|...

C - Chemistry – Metallurgy – 07 – D

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Details

C07D 321/10 (2006.01) A61K 31/557 (2006.01) C07D 307/00 (2006.01) C07D 319/08 (2006.01) C07D 405/06 (2006.01) C07D 407/06 (2006.01) C07D 409/06 (2006.01) C07D 493/08 (2006.01)

Patent

CA 2180010

The present invention relates to 7-[carboxyalkyl or alkenyl]-6-[alkyl or alkenyl]-3-3-oxo-2,4-dioxobicyclo[3.2.1] octanes and derivatives thereof. In particular, hydroxyl, nitro, amino, amido, azido, oxime, thiol, ether and thiol ether derivatives of said carboxy group are contemplated. In particular, 7-[6-carboxy-2-hexenyl]-6-[3-hydroxy-1-octenyl] of 3-oxo-2,4-dioxobicyclo-[3.2.1] octane and derivatives thereof are disclosed. These compounds are useful as ocular hypotensives and as (a) thromboxane mimetics for the prevention of hemorrhaging as follows: during surgery; tooth extraction; hemorrhaging associated with gastro-intestinal diseases and conditions such as hemorrhoids, inflammatory bowel diseases and gastric and peptic ulcers, as a result of stroke; as a complication in retinal diseases resulting in impaired vision and associated with menstruation, childbirth and uterine dysfunction and (b) selective vasoconstrictors for treating systemic hypotension, e.g. in restoring normal blood pressure in hemorrhagic, anaphylactic or septic shock victims, to provide local anti-inflammatory effects in the eye, skin and nose; to limit plasma exudation in burns, etc, and optimizing blood-born delivery of drugs and diagnostics in encapsulating vehicles.

7-[carboxyalkyle ou alcényle]-6-[alkyle ou alcényle]-3-oxo-2,4-dioxobicyclo[3.2.1]octanes et leurs dérivés, en particulier dérivés hydroxyle, nitro, amino, amido, azido, oxime, thiol, éther et thiol éther dudit groupe carboxyle. Le 7-[6-carboxy-2-hexényle]-6-[3-hydroxy-1-octényle] de 3-oxo-2,4-dioxobicyclo-[3.2.1] octane et ses dérivés sont spécifiquement décrits. Ces composés sont utiles en tant qu'hypotenseurs oculaires et (a) comme imitateurs de thromboxane pour la prévention des hémorragies dans les cas suivants: intervention chirurgicale, extraction dentaire, hémorragie associée aux maladies gastro-intestinales et aux troubles tels que les hémorroïdes, les maladies et les ulcères gastriques et peptiques, conséquence d'accidents vasculaires cérébraux, complication de maladies de la rétine entraînant une détérioration de la vision et troubles associés à la menstruation, à l'accouchement et aux dysfonctions utérines; et (b) comme vasoconstricteurs sélectifs pour traiter l'hypotension systémique, par exemple pour restaurer la pression sanguine normale chez les victimes de choc hémorragique, anaphylactique ou septique, pour engendrer des effets anti-inflammatoires dans l'oeil, sur la peau et dans le nez, pour limiter l'exsudation de plasma dans les brûlures, etc., ainsi que pour optimiser l'administration par les voies sanguines de médicaments et d'agents diagnostiques dans des excipients encapsulés.

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