March 31, 2014

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The following patent record is from the CAplusSM database.


Patent Number: WO 20140038943
Title: Azetidine derivatives and related compounds as serotonin receptor modulators and their preparation and use in the treatment of serotonin-mediated diseases
Inventor(s): Carruthers, Nicholas I.; Shireman, Brock T.; Tran, Vi T.; Wong, Victoria D.; Jablonowski, Jill A.; Chai, Wenying
Patent Assignee(s): Janssen Pharmaceutica N. V., Belg.
Source: PCT Int. Appl., 235pp. CODEN: PIXXD2
Language: English

The azetidines and related compds. of formula I are serotonin modulators useful in the treatment of serotonin-mediated diseases.  Compds. of formula I wherein R1 is H, C1-4 alkyl, monocyclic cycloalkyl, Ph and benzyl; A is (CHR2)n; B is (CHR3)m; m is 1, 2, and 3; n is 1 and 2; with proviso that if m is 2, then n is not 1; R2 and R3 are independently H and C1-4 alkyl; R4 is H, F, C1-4 alkyl; or R4 is OH when L is CH2, CF2, CHF, OCH2 and OCHCH3; L is O, CH2, OCH2, OCHCH3, CH2O, CF2, and CHF; Z is O, CO, OCH2, etc.; R5 is (un)substituted Ph, (un)substituted phenoxy, (un)substituted naphthyl, etc.; X is C and N; R6 and R7 are independently H, halo, CF3, thienyl, and CONH2 and derivs.; and pharmaceutically acceptable salts, pharmaceutically acceptable prodrugs, and pharmaceutically active metabolites thereof, are claimed. Example compd. II was prepd. by a multistep procedure (procedure given). All the invention compds. were evaluated for their serotonin receptor modulatory activity (data given).

Please note:  Abstracts and Titles for patent records in CAplus are routinely enhanced to better describe the claimed invention.


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