or
Bookmark and Share
Certain arylaliphatic and heteroaryl-aliphatic piperazinyl pyrazines and their use in the treatment of serotonin-related diseases
   
Document Number
US Patent 7071180
Issued Date
July 4, 2006
Link
Map
Abstract
The invention relates to compounds of the general formula (I): ##STR00001## wherein Ar is optionally substituted aryl or heteroaryl; A is (i) --O--, --S--, --SO.sub.2--, --NH--, (ii) a C.sub.1-4-alkyl- or C.sub.1-6-acyl-substituted nitrogen atom or (iii) a C.sub.1-8-alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members; B is --C(R.sub.4)(R.sub.5)--, --OC(R.sub.4)(R.sub.5)--, --N(R.sub.6)C(R.sub.4)(R.sub.5)--, --N(R.sub.6)--, --O--, --S-- or --SO.sub.2--; R is optionally substituted C.sub.3-8-cycloalkyl, aryl or heteroaryl; R.sub.1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 ring members, which rings optionally are substituted in one or more positions, or a group --[C(R.sub.4)(R.sub.5)].sub.xN(R.sub.2a)(R.sub.3a)]; R.sub.2a, R.sub.3a, R.sub.4, R.sub.5, R.sub.6 and x are as defined in the claims, and n is 0 or 1; and pharmaceutically acceptable salts, hydrates and prodrug forms thereof. The compounds may be prepared by per se conventional methods and can be used for treating a human or animal subject suffering from a serotonin-related disorder, such as eating disorders, especially obesity, memory disorders, schizophrenia, mood disorders, anxiety disorders, pain, sexual dysfunctions, and urinary disorders. The invention also relates to such use as well as to pharmaceutical compositions comprising a compound of formula (I).
Tags:
Description:
Amusing 0%
Clever 0%
Complex 0%
Efficient 0%
Historic 0%
Important 0%
Innovative 0%
Interesting 0%
Practical 0%
Simple 0%
Number of Claims:
46
Comments:
no comments yet
Owner
Published
July 4, 2006
Application Number
10/873,852
Filed
June 22, 2004
US Classification
514/183   514/235.8 514/249 514/252.11 514/252.12 514/306 514/362 514/363 544/129 544/349 544/353 544/354 544/357 546/277.4 546/84 548/134 548/452 548/469 548/503 548/511 549/398 549/399
Int'l Classification
A61K   31/33   (20060101)   A61K   31/497   (20060101)   A61K   31/502   (20060101)   C07D   241/36   (20060101)   C07D   401/04   (20060101)  
Assistant Examiner
Attorney/Law Firm
Parent Case
This application is a continuation of U.S. application Ser. No. 10/269,670, filed on Oct. 11, 2002, which is a divisional of U.S. application Ser. No. 09/589,282, filed Jun. 8, 2000 (now U.S. Pat. No. 6,465,467, issued Oct. 15, 2002), which is a continuation-in-part of U.S. application Ser. No. 09/573,348, filed on May 19, 2000, abandoned, which claims the benefit of U.S. Provisional application Ser. No. 60/137,527, filed on Jun. 3, 1999, and of Swedish Application No. 9901884-8, filed on May 21, 1999, the entire contents each of which are incorporated by reference in their entirety.
Priority Data
May 21, 1999 [SE] 9901884
USPTO Field of Search
514/183   514/249   514/252.11   514/36   514/252.12   514/30   514/235.8   514/363   544/129   544/349   544/353   544/354   544/357   549/398   549/399   548/134  
Related Patents
7407957 - Phthalazinone derivatives - Owned by Maybridge Limited (Cornwall,GB) Kudos Pharmaceuticals Limited (Cambridge,GB)

A compound of formula (I): ##STR00001## for use in treating cancer or other diseases ameliorated by the inhibition of PARP, wherein: A and B together represent an optionally substituted, fused aromatic ring; X can be NR.sup.X or CR.sup.XR.sup.Y; if X=NR.sup.X then n is 1 or 2 and if X=CR.sup.XR.sup.Y then n is 1; R.sup.X is selected from the group consisting of H, optionally substituted C.sub.1-20 alkyl, C.sub.5-20 aryl, C.sub.3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; R.sup.Y is selected from H, hydroxy, amino; or R.sup.X and R.sup.Y may together form a spiro-C.sub.3-7 cycloalkyl or heterocyclyl group; R.sup.C1 and R.sup.C2 are independently selected from the group consisting of hydrogen and C.sub.1-4 alkyl, or when X is CR.sup.XR.sup.Y, R.sup.C1, R.sup.C2, R.sup.X and R.sup.Y, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; R.sup.1 is selected from H and halo; and Het is selected from: ##STR00002## where Y.sup.1 is selected from CH and N, Y.sup.2 is selected from CH and N, Y.sup.3 is selected from CH, CF and N, where only one or two of Y.sup.1, Y.sup.2 and Y.sup.3 can be N; and ##STR00003## where Q is O or S.

Claims
Description
About| FAQs| Terms & Disclaimer| Link to Us| Contact Us