Use of phenoxyacetic acid derivatives for treating hyperactive bladder

A drug, bladder technology, applied in the field of new indications, can solve problems such as the treatment effect of overactive bladder that has not been mentioned

CN100518731CInactive Publication Date: 2009-07-29KISSEI PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Publication Date
2009-07-29
Estimated Expiration
Not applicable · inactive patent

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Abstract

A formulation comprises phenoxyacetic acid derivative or its salt. A formulation comprises phenoxyacetic acid derivative of formula (I) or its salt. [Image] X and Y : chiral carbon atom; R 1OH,1-6C alkoxy, aryl-1-6C alkoxy, primary amino or mono- / di-(1-6C alkyl)amino; R 2and R 3H, halo, 1-6C alkyl, trifluoromethyl or 1-6C alkoxy; and R 4H, 1-6C alkyl, halo(1-6C alkyl), hydroxy, 1-6C alkoxy, aryl-1-6C alkoxy, 1-6C alkoxy, cyano, nitro, amino, mono- or di(1-6C alkyl)amino, carbamoyl, mono- or di(1-6C alkyl)carbamoyl or NHCOR 5; R 5H or 1-6C alkyl. Provided that at least one of R 2and R 3is H. ACTIVITY : None given. MECHANISM OF ACTION : Adrenoreceptor-beta -3 agonist. Effect of (-)-2-[4-(2-{(1S,2R)-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethylamino}ethyl)-2,5-dimethylphenoxyl] acetic acid (A1) on the tone of monkey detrusor was studied. The detrusor of cynomolgus monkey was isolated and dissected. Tracheal, atrial and urethral dissections were also prepared. The results were as follows: EC 50value of (A1) / isoproterenol was 8.2X10 ->7>. (A1) Exhibited lesser effect on the trachea and atria. The detrusor selectivity of (A1) was 1200 times greater (compared with the trachea) and 80 times greater (compared with the atria). (A1) Showed no effect on endothelin-1-induced tonic contraction of the isolated urethra.
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Description

technical field

[0001] The present invention relates to a new field of indications for phenoxyacetic acid derivatives as described in European patent application EP1095932. The compounds described in this application have now been found to be suitable for the preparation of medicaments for the treatment of overactive bladder (overactive bladder: OAB). Therefore, by utilizing these active substances, a method of treating this urinary syndrome is provided. Background technique

[0002] Bladder dysfunction OAB is a prevalent chronic disease that is estimated to affect more than 50 million people in industrialized countries.

[0003] According to the nomenclature published by the International Continence Association in 2002, OAB is diagnosed by symptoms. Symptoms of OAB are urgency to urinate with or without acute incontinence, usually but not necessarily accompanied by frequency and nocturia. OAB is also characterized by involuntary detrusor contractions, which can be stimul...

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Embodiment Construction

[0013] The present invention relates to the use of phenoxyacetic acid derivatives as described in EP1095932 in the preparation of medicines for treating overactive bladder and pharmaceutical preparations for treating overactive bladder, the medicines or pharmaceutical preparations comprising The above-mentioned phenoxyacetic acid derivatives are used as active ingredients. According to EP1095932, the compounds forming the basis of the use and formulations according to the invention are beta-3-adrenoceptor agonists. In particular, these substances are useful in the treatment of neurogenic hyperbladder, neurogenic detrusor hyperactivity and in the treatment of congenital hyperbladder and congenital detrusor hyperactivity.

[0014] The compounds forming the basis of the applications and formulations of the present invention are represented by the following general formula I:

[0015] Chemical formula I:

[0016]

[0017] in

[0018] X is a chiral carbon atom of R or S, pref...