Therapeutic use of compounds with &bgr;3-agonist activity

Details Therapeutic use of compounds with &bgr;3-agonist activity Therapeutic use of compounds with &bgr;3-agonist activity

2001-05-24

2001-10-30

Henley, III, Raymond (Department: 1614)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Phosphorus containing other than solely as part of an...

C514S338000, C514S340000, C514S365000, C514S387000, C514S419000, C514S539000, C514S597000, C514S605000, C514S652000

Reexamination Certificate

active

06310050

ABSTRACT:

A subject matter of the present invention is a novel use of compounds which are active with respect to the &bgr;
3
-adrenergic receptor. The invention more particularly relates to the use of &bgr;
3
-agonists in the preparation of medicaments which inhibit uterine contractions.
The &bgr;
3
-adrenergic receptor, also sometimes indicated as atypical &bgr; receptor, is mainly located in the adipose tissue and in the gastrointestinal tract.
Numerous patent applications have been published in recent years disclosing novel products having &bgr;
3
-agonist activity.
The products are indicated in several pathologies, such as obesity, diabetes, hyperglycemia or disorders of the gastrointestinal apparatus. To date, no patent application or scientific publication has envisaged the possibility of using compounds having a &bgr;
3
-agonist activity as inhibitors of uterine contraction in order to obtain a beneficial effect in the event of dysmenorrhea or a tocolytic activity.
The products normally used as tocolytic agents are &bgr;
2
-agonists and in particular ritodrine and salbutamol.
It is known that, because of the effects at the pulmonary or cardiac level caused by all &bgr;
2
-agonists, the use of ritodrine or salbutamol often results in significant side effects.
For the treatment of dysmenorrhea, the products normally used are nonsteroidal antiinflammatories, which have well known side effects, in particular at the gastric level.
&bgr;
3
-Adrenergic compounds were initially tested in the rat and it is only in recent years that researchers have developed tests for evaluating the activity of these compounds in human tissues.
Croci et al. report that selective &bgr;
3
-agonists, such as N-[(6-hydroxy-1,2,3,4-tetrahydronaphth-2-yl)methyl]-2-hydroxy-2-(3-chlorophenyl)ethanamine and N-[(7-methoxy-1,2,3,4-tetrahydronaphth-2-yl)methyl]-2-hydroxy-2-(3-chlorophenyl)ethanamine, are inactive with respect to the uterus of the rat (Br. J. Pharmacol., 116, Proc. Suppl., 204 P. 1995).
In the same way, Landi et al. show that N-[(2S)-7-carboxymethoxy-1,2,3,4-tetrahydronaphth-2-yl]-(2R)-2-(3-chlorophenyl)-2-hydroxyethanamine, a selective &bgr;
3
-agonist, does not have activity with respect to the uterus of the rat (Br. J. Pharmacol., 114, Proc. Suppl., 432P, 1995).
The activity which some &bgr;
3
-agonists exhibit with respect to the rat uterus is in fact to be attributed to their low selectivity with respect to &bgr;
2
-receptors (J. Pharmacol. Exp. Ther., 277, I, 22-27, 1996).
We have now found, in an entirely surprising fashion, that &bgr;
3
-agonists cause a relaxant effect on the muscles of the human uterus.
Thus, according to one of its aspects, a subject matter of the present invention is the use of a selective &bgr;
3
-agonist in the preparation of a medicament which inhibits uterine contractions in human beings.
More particularly, a subject matter of the invention is the use of a selective &bgr;
3
-agonist in the preparation of a medicament intended to treat dysmenorrhea or which has a tocolytic effect.
The &bgr;
3
-agonists which are a subject matter of the present invention are, for example, the products included in the following patents or patent applications: EP 436 435, EP 500 443, WO 98/20005, JP 10007647, US 5 705 515, EP 822 185, WO 97/46556, WO 97/43273, JP 09268171, FR 2 746 395, WO 97/37646, EP 801 060, WO 97/34905, WO 97/25311, WO 97/21666, WO 97/21665, JP 09118655, WO 97/15549, GB 2 305 665, EP 764 640, EP 764 632, WO 96/35671, WO 96/35685, JP 08259558, US 5 561 142, JP 08198866, JP 08165276, JP 08157470, EP 714 883, WO 96/16938, WO 96/04234, WO 96/04233, US 5 488 064, US 5 491 134, US 5 482 971, WO 95/29159, WO 95/33724, ZA 9409874, JP 07228543, WO 95/25104, EP 659 737, WO 95/11223, WO 95/08527, WO 95/07284, JP 07112958, WO 95/04047, JP 06345731, WO 94J29290, JP 06293664, WO 94/24090, EP 611 003, EP 608 568, WO 94/12166, US 5 321 036, WO 93/22277, WO 94/02493, EP 565 317, WO 93/15041 and WO 94/16938.


REFERENCES:
patent: 5488151 (1996-01-01), Baroni et al.
patent: 0626367 (1994-11-01), None
Manara et al., British Journal of Pharmacology (1996), 117, 435-442.
Bardou et al., European Journal of Pharmacology 353 (1998), 281-287.

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