Shionogi Company Limited

Masahiro Sakagami

Takayuki Okuno

Kenji Takaya

Hiroshi Hashizume

Naoki Kouyama

Hiroshi Yoshida

Satoru Tanaka

Keisuke Tonogaki

Hitomi Araki

Hiroshi Yari

This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof,whereinRis optionally substituted lower alkyl,Y is &#x2014;S(O)&#x2014; wherein n is 1 or 2, or &#x2014;CO&#x2014;,Ris hydrogen or lower alkyl,Ris hydrogen or lower alkyl,X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, andZ is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like.

Amine derivative having NPY Y5 receptor antagonistic activity

A compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, where Ris optionally substituted lower alkyl, Y is &#x2014;S(O)&#x2014;, Ris hydrogen or optionally substituted lower alkyl, Ris hydrogen or optionally substituted lower alkyl, X is a group of the formula: where Rand Rare each independently hydrogen, a group of the formula: is optionally substituted cycloalkylene, p is 0, and q is 1 or 2, Z is optionally substituted carbocyclyl or optionally substituted heterocyclyl, and provided that a compound wherein Z is fused heterocyclyl consisting of three rings or optionally substituted pyrimidinyl is excluded.

The present invention discloses novel piperidine and pyrrolidine derivatives having NPY Y5 receptor antagonistic activity. Specifically, the present invention discloses a compound represented by the formula (I), a pharmaceutically acceptable salt or a solvate thereof: whereinA is substituted or unsubstituted monocyclic aryl or monocyclic heterocyclyl; X is a single bond or C(&#x2550;O); Y is a single bond, CRRNRor C(&#x2550;O)NR; Rand Rare independently hydrogen or substituted or unsubstituted alkyl; Ris substituted or unsubstituted aryl or heterocyclyl; Ris halogen, substituted or unsubstituted alkyl, alkoxy, aryloxy or heterocyclyloxy, etc.; p is an integer of 0 to 2; q is 0 or 1; m is 0 or 1; n is an integer of 0 to 5; and B is aromatic carbocycle, monocyclic heterocycle or bicyclic fused hetero ring.

Piperidine and pyrrolidine derivatives having NPY Y5 receptor antagonism

The present invention discloses novel cyclohexane derivatives having NPY Y5 receptor antagonistic activity. Specifically, the present invention discloses a compound represented by the formula (I), or a pharmaceutically acceptable salt or a solvate thereof: wherein A is substituted or unsubstituted aryl or heterocyclyl; a combination of X and Y is a combination selected from (X, Y)&#x2550;(C(&#x2550;O)N(R), C(&#x2550;O)N(R)), (C(&#x2550;O)N(R), imidazole-1,3-diyl), (N(R), C(&#x2550;O)N(R)), (O, C(&#x2550;O)N(R)), (C(R)(R), N(R)) or (a single bond, C(&#x2550;O)N(R)); R, Rand Rare independently hydrogen or substituted or unsubstituted alkyl; Ris substituted or unsubstituted aryl or heterocyclyl; Ris halogen, oxo, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryloxy; m is 0 or 1; and n is an integer of 0 to 5; and B is aromatic carbocycle, monocyclic heterocycle or fused bicyclic heterocycle.

Cyclohexane derivative having NPY Y5 receptor antagonism

This invention provides an anorectic or anti-obesity composition comprising a compound of the formula (I): 

Amine derivatives having NPY Y5 receptor antagonistic activity and the uses thereof

This invention provides a compound of the formula (I): 

Compounds having NPY Y5 receptor antagonistic activity

This invention provides an anorectic or anti-obesity composition comprising a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof,wherein

Amine-derivatives having NPY Y5 receptor antagonistic activity and the uses thereof

This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof,whereinRis substituted or unsubstituted alkyl or the like,Ris hydrogen or substituted or unsubstituted alkyl,Ring A is monocyclic or bicyclic aromatic heterocycle,Ris substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heterocycle,Ris halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl or the like,m is an integer between 0 and 2,n is an integer between 0 and 5,R is halogen, oxo, cyano, nitro, substituted or unsubstituted alkyl or the like, andp is an integer between 0 and 2as novel compounds having NPY Y5 antagonistic activity.

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Sapporo, Japan

Masahiro Sakagami