Novel bicyclic compounds
AssigneeAsahi Kasei Pharma Corporation
InventorsShunichi Ikuta, Shiro Miyoshi, Kohei Ogawa
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AssigneeAsahi Kasei Pharma Corporation
InventorsShunichi Ikuta, Shiro Miyoshi, Kohei Ogawa
Estimating the term…
Compounds of the general formula (I): 1 or a salt thereof, wherein R1 is hydrogen, hydroxyl or halogen; R2 is NHSO2CH3, SO2NHCH3 or the like; R5 and R6 each independently is hydrogen, C1-6 alkyl, optionally substituted phenyl or optionally substituted benzyl; X is NH, sulfur, oxygen or methylene; Y is oxygen, NR7, sulfur, methylene or a bond; and * represents an asymmetric carbon atom. The compounds are useful as a medicine for treating or preventing diabetes, obesity, hyperlipidemia, digestive diseases, depression or urinary disturbances.
A compound of the general formula (I):
A compound of the general formula (I):
A compound of the general formula (II):
A compound of the general formula (II):
Dependencies are inferred from the claim text.
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Benzo [b] furans; Hydrogenated benzo [b] furans: with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to…
Drugs for disorders of the alimentary tract or the digestive system
Drugs for disorders of the metabolism: anorexiants; Antiobesity agents
Drugs for disorders of the metabolism: antihyperlipidemics
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This invention relates to novel compounds which are useful as a medicine for treating and preventing diabetes, obesity, hyperlipidemia, digestive diseases, depression and urinary disturbances.
Beta-adrenoreceptors are classified into three classes, β1-adrenoreceptor, β2-adrenoreceptor and β3-adrenoreceptor, and it is recognized that stimulation of β1 induces an increase in the heart rate and stimulation of β2 induces a relaxation of the smooth muscle tissue, thereby resulting in lowering the blood pressure. It is also recognized that stimulation of β3 facilitate the lipolysis in adipocytes, thereby resulting in increasing the thermogenesis. Therefore, compounds having β3-agonist activity were shown to be useful as a medicine for treating and preventing diabetes, obesity and hyperlipidemia (Nature, vol. 309, pp. 163-165 (1984); Int. J. Obes. Relat. Metab. Disord., vol. 20, pp. 191-199 (1996); Drug Development Research, vol. 32, pp. 69-76 (1994); J. Clin. Invest., vol. 101, pp. 2387-2393 (1998)). Recently, it was shown that β3-adrenoreceptor is expressed in the detrusor and a β3-agonist induces a relaxation of the detrusor (J. Urinol., vol. 161, pp. 680-685 (1999); J. Pharmacol. Exp. Ther., vol. 288, pp. 1367-1373 (1999)).
Some compounds showing a β3-agonist activity have been known. Compounds having high selectivity or having low β1- and β2-stimulating activities are particularly required when their usefulness as a medicine is taken into consideration. This is because compounds having both β1- and β2-stimulating activities induce side effects such as increase in the heart rate and lowering of the blood pressure, as set forth above.
The following Examples, Reference Examples and Test Examples specifically illustrate this invention but are not intended to limit it in any way.
In the following examples, each analysis was carried out as follows.
(1) Fast Atom Bombardment Mass Spectrum (FAB-MS)