Title (en)

A METHOD OF REDUCING BODY WEIGHT AND FOOD INTAKE USING A DOPAMINE D2 RECEPTOR AGONIST

Publication

EP 0483152 A4 19921202 (EN)

Application

EP 90906612 A 19900419

Priority

US 34909189 A 19890509

Abstract (en)

[origin: WO9013294A1] This invention provides a method for treating the symptoms of obesity which comprises administering to a human or other mammal suffering from the symptoms of obesity an effective amount of a compound selected from the group consisting of the optically active compounds especially the (-) negative stereoisomers represented by formula (I), wherein R1 is selected from the group consisting of methyl, substituted or unsubstituted phenyls, pyridyl, hydroxyphenyl, (a), (b) (c), (d), (e), (f), (g), X is oxygen or sulfur, Y is selected from the group consisting of hydroxy, nitro, cyano, azido, amino, acylamino, carboxyamido, trifluoromethyl, sulfate, sulfonamido, halogen, hydrocarbyl and hetero atom-substituted hydrocarbyl radicals, wherein said heteroatoms are selected from the group consisting of halogen, nitrogen, oxygen, sulfur and phosphorus and said hydrocarbyl radicals comprise from 1 to 12 carbon atoms, and a is an integer of from zero to 3, R2, R3 and R4 are each selected from the group consisting of H and OA, A is H or is selected from the group consisting of hydrocarbyl radicals, (h) and (i), R5 is selected from the group consisting of hydrocarbyl radicals; n is an integer between 1 and 3; and R6 is an alkyl chain having between 1 and 3 carbon atoms with the provision that at least one of R2, R3 and R4 is H, that at least one of R2, R3 and R4 is not H, and that R2 and R4 are not both OA, and pharmaceutically acceptable salts thereof. Preferably, R2 is oxygen. Most preferably, R2 is OA and A is H, and the compound is the (-) isomer.

IPC 1-7

A61K 31/44; A61K 31/415; A61K 31/405; A61K 31/38; A61K 31/385; A61K 31/34; A61K 31/275; A61K 31/135

IPC 8 full level

A61K 31/135 (2006.01); A61K 31/275 (2006.01); A61K 31/34 (2006.01); A61K 31/38 (2006.01); A61K 31/40 (2006.01); A61K 31/415 (2006.01); A61K 31/44 (2006.01)

CPC (source: EP)

A61K 31/135 (2013.01); A61K 31/275 (2013.01); A61K 31/34 (2013.01); A61K 31/38 (2013.01); A61K 31/40 (2013.01); A61K 31/415 (2013.01); A61K 31/44 (2013.01)

Citation (search report)

• [XD] SOC. NEUROSCI. ABSTR., vol. 12, 1986, page 1557, abstract no. 420.18; I. RUSK et al.: "Dopamine D1 and D2 receptors in relation to palatable food consumption in the rat"
• [X] SOC. NEUROSCI. ABSTR., vol. 14, no. 1, 1988, page 614, abstract no. 249.6; I.N. RUSK et al.: "Microstructural analysis of feeding suppression and other behavioral changes induced by N-0437, a selective dopamine D2 agonist"
• [Y] EUROPEAN JOURNAL OF PHARMACOLOGY, vol. 162, no. 1, 14th March 1989, pages 143-150, Elsevier Science Publishers B.V. (Biomedical Division); W. TIMMERMAN et al.: "Microdialysis and striatal dopamine release: stereoselective actions of the enantiomers of N-0437"
• [X] PHYSIOLOGY & BEHAVIOR, vol. 44, nos. 4-5, 1988, pages 545-553, Pergamon Press plc, US; I.N. RUSK et al.: "Profile of the selective dopamine D-2 receptor agonist N-0437: its effects on palatability- and deprivation-induced feeding, and operant responding for food"
• See references of WO 9013294A1

Designated contracting state (EPC)

AT BE CH DE DK ES FR GB IT LI LU NL SE

DOCDB simple family (publication)

WO 9013294 A1 19901115; AU 5439890 A 19901129; EP 0483152 A1 19920506; EP 0483152 A4 19921202

DOCDB simple family (application)

US 9002135 W 19900419; AU 5439890 A 19900419; EP 90906612 A 19900419