发明名称 CERTAIN ALKYLENE DIAMINE-SUBSTITUTED HETEROCYCLES
摘要 The present invention also provides a general method to whereby mono-, bi-, or tri-cyclic heterocycles may be modified to obtain potent antagonists at the NPY1 receptor. The present invention provides novel, potent, non-peptidic antagonists of NPY receptors, particularly, the NPY1 receptors, designed fro m a selection of mono-, bi-, or tri-cyclic heterocyclic cores. This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y. The nov el compounds encompassed by the present invention are those of formula (I)-(XV) , wherein X is N or CR14; W is S, O, or NR15; Y is N or CR3; E, F, and G are each, independently, CR3 or N; I and J are each, independently, C=O, S, O, CR3R16 or NR15 when single bonded to both adjacent ring atoms, or N, or CR3 when double bonded to an adjacent ring atom; K is N or CR3 when double bonde d to L or J, or O, S, C=O, CR3R16, or NR15 when single bonded to both adjacent ring atoms, or N or CR3 when double bonded to an adjacent ring atom; L is N or CR16 when single bonded to all atoms to which it is attached, or C (carbon) when double bonded to K; the 6- or 7-membered ring that contains I, J, K, an d L may contain from 1 to 3 double bonds, from 0 to 2 heteroatoms, and from 0 to 2C=O groups, wherein the carbon atom of such groups are part of the ring and the oxygen atom is a substituent on the ring; Q is O or NR15. Such compounds inhibit the activity of neuropeptide Y at those receptors are useful in treating physiological disorders associated with an excess of neuropeptide Y , including eating disorders, such as, for example, obesity and bulimia, and certain cardiovascular diseases, for example, hypertension.
申请公布号 CA2379640(A1) 申请公布日期 2001.04.05
申请号 CA20002379640 申请日期 2000.09.29
申请人 NEUROGEN CORPORATION;PFIZER INC. 发明人 HORVATH, RAYMOND F.;GRIFFITH, DAVID A.;CARPINO, PHILIP A.;HODGETTS, KEVIN JULIAN;TRAN, JENNIFER;DE LOMBAERT, STEPHANE
分类号 A61K31/437;A61K31/4375;A61K31/4409;A61K31/4706;A61K31/505;A61K31/519;A61K31/522;A61P1/12;A61P3/04;A61P3/06;A61P3/10;A61P5/06;A61P5/48;A61P7/04;A61P9/00;A61P9/04;A61P9/06;A61P9/10;A61P9/12;A61P11/02;A61P11/06;A61P13/12;A61P15/00;A61P15/10;A61P25/00;A61P25/04;A61P25/06;A61P25/08;A61P25/18;A61P25/20;A61P25/22;A61P25/24;A61P25/28;A61P29/00;A61P43/00;C07D213/73;C07D213/74;C07D215/46;C07D239/48;C07D471/04;C07D471/14;C07D473/34;C07D475/06;C07D475/08;C07D487/04;C07D495/04;(IPC1-7):C07D487/04;C07D209/00;C07D221/00;C07D231/00;C07D235/00;C07D239/00;C07D249/00;A61K31/436;A61K31/44;A61K31/47;G01N33/566 主分类号 A61K31/437
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