Nitrogen-containing heterocyclic compounds and medicaments...

Details Nitrogen-containing heterocyclic compounds and medicaments... Nitrogen-containing heterocyclic compounds and medicaments...

C - Chemistry, Metallurgy

07

D

C07D 401/10 (2006.01) A61K 31/517 (2006.01) C07D 239/84 (2006.01) C07D 401/12 (2006.01)

Patent

CA 2318579

The present invention provides a novel nitrogen--containing heterocyclic compound useful as a phosphodiesterase-4 inhibitor, and a medicament comprising the same. Further, the present invention provides a nitrogen--containing heterocyclic compound represented by the following formula, its salt or hydrates thereof, and a medicament comprising the same. (SEE ABOVE FORMULA) Wherein the ring A is an aromatic hydrocarbon ring which may have a heteroatom, the ring B represents (a) a saturated hydrocarbon ring, (b) an unsaturated hydrocarbon ring, (c) a saturated heterocyclic ring or (d) an unsaturated heterocyclic ring, all of which may have a substituent group, R1 represents hydrogen atom, a halogen atom, a C1-6 alkyl group which may be substituted with a halogen atom, a C1-6 alkoxy group which may be substituted with a halogen atom, etc. , R2 and R3 are the same as or different from and represent hydrogen atom, a C1-6 alkyl group which may have a substituent group, a C3-7 cycloalkyl group which may have a substituent group, etc. , R4, R5, R6 and R' are the same as or different from each other and each represent hydrogen atom, a halogen atom, a C1-6 alkyl group which may be substituted with a halogen atom, a C3-7 cycloalkyl group which may have a substituent group, a C1-6 alkoxy group which may have a substituent group, etc., neighboring R3, R4, R5 and R6 may be combined to form a ring which may be substituted with a C1-6 alkyl group which may contain a heteroatom, L represents a single bond, (a) a C1-6 alkylene group, (b) a C2-6 alkenylene group, (c) a C2-6 alkynylene group, all of which may have a substituent group, or a group represented by the formula -E-G- (wherein E represents oxygen atom, sulfur atom, the formula -CO-, -SO-, -SO2-, -N(R8) -(R8 is hydrogen atom, a C1-6 alkyl group or an acyl group) ,-N (R9) -CO- (R9 is hydrogen atom or a C1-6 alkyl group) , or -(CH2)m- which may have a substituent group (m is an integer of 0 to 6), and G represents a sulfonyl group, the formula -N(R10)- (R10 represents hydrogen atom, a C1-6 alkyl group or an acyl group) or -(CH2)n- (n is an integer of 0 to 6)), and X and Y are the same as or different from each other and each represents nitrogen atom, =CH- or a carbon atom which may be substituted with a C1-6 alkyl group which may have a substituent group, provided that X and Y are not simultaneously carbon atoms which may be substituted with a C1-3 alkyl group. 139

L'invention concerne des dérivés hétérocycliques azotés représentés par la formule (I) ci-après, ou des sels ou des hydrates de ces dérivés, qui sont utilisés comme inhibiteur de phosphodiestérase 4. L'invention concerne également un médicament renfermant l'un de ces composés. Dans la formule (I), X et Y représentent chacun un atome de carbone ou d'azote, étant entendu que X et Y ne peuvent pas être tous deux des atomes de carbone; le noyau A représente un noyau (hétéro)aromatique; le noyau B représente un noyau carboné (in)saturé éventuellement substitué ou un hétérocycle; R<1> représente hydrogène, halogéno, ou un alkyle ou un cycloalkyle éventuellement substitué; R<2> et R<3>, qui sont identiques ou différents, représentent chacun hydrogène, un alkyle ou un cycloalkyle éventuellement substitué, etc.; R<4>, R<5>, R<6> et R<7>, qui sont identiques ou différents, représentent chacun hydrogène ou un substituant approprié, étant entendu que deux groupes adjacents quelconques peuvent être liés pour former un noyau; et L représente une liaison simple ou un élément de connexion.

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