Bis(hetero)aryl carboxamide derivatives for use as pgi2...

C - Chemistry – Metallurgy – 07 – D

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C07D 231/14 (2006.01) A61K 31/166 (2006.01) A61P 13/00 (2006.01) C07C 235/42 (2006.01) C07D 207/32 (2006.01) C07D 207/325 (2006.01) C07D 211/14 (2006.01) C07D 213/34 (2006.01) C07D 213/64 (2006.01) C07D 213/82 (2006.01) C07D 231/12 (2006.01) C07D 239/34 (2006.01) C07D 261/18 (2006.01) C07D 333/38 (2006.01)

Patent

CA 2515235

The present invention relates to aryl or heteroaryl amido alkane derivatives of formula (I) wherein R6 represents carboxy or tetrazolyl, which are useful as an active ingredient of pharmaceutical preparations. The aryl or heteroaryl amido alkanes of the present invention have PGI2 antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with PGI2 activity.Such diseases include urological diseases or disorder as follows: bladder outlet obstruction, overactive bladder, urinary incontinence, detrusor hyper-reflexia, detrusor instability, reduced bladder capacity, frequency of micturition, urge incontinence, stress incontinence, bladder hyperreactivity, benighn prostatic hypertrophy (BPH), prostatitis, urinary frequency, nocturia, urinary urgency, pelvic hypersensitivity, urethritis, pelvic pain syndrome, prostatodynia, cystitis, or idiophatic bladder hypersensitivity.The compounds of the present invention are also useful for treatment of pain including, but not limited to inflammatory pain, neuropathic pain, acute pain, chronic pain, dental pain, premenstrual pain, visceral pain, headaches, and the like; hypotension;hemophilia and hemorrhage; and inflammation, since the diseases also relate to PGI2.

L'invention concerne des dérivés d'amido-alcane aryle ou hétéroaryle de formule générale (I), dans laquelle R?6¿ représente carboxy ou tétrazolyle, qui sont utiles en tant qu'ingrédients actifs dans des compositions pharmaceutiques. Les amido-alcanes aryle ou hétéroaryle de l'invention présentent une activité antagoniste de la PG12, et peuvent être utilisés pour la prophylaxie et le traitement de maladies associées à l'activité de la PG12. Parmi ces maladies, on peut citer les maladies ou des troubles urologiques suivants: obstacle sur les voies excrétrices, vessie hyperactive, incontinence urinaire, hyperréflectivité du muscle vésical, instabilité du muscle vésical, capacité réduite de la vessie, fréquence des mictions, incontinence par impériosité, incontinence à l'effort, hyperactivité de la vessie, hypertrophie prostatique bénigne (BPH), prostatite, fréquence urinaire, nycturie, urgence urinaire, hypersensibilité pelvienne, urétrite, syndrome de douleur pelvienne, prostatalgie, cystite, ou hypersensibilité idiopathique de la vessie. Les composés de l'invention s'avèrent également utiles pour le traitement de la douleur, par exemple, entre autres, douleur inflammatoire, douleur neuropathique, douleur aiguë, douleur chronique, douleur dentaire, douleur prémenstruelle, douleur viscérale, maux de tête, et analogues; hypotension; hémophilie et hémorragie; et inflammation, les maladies étant associées à la PGI2.

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