August 6, 2012

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The following patent record is from the CAplusSM database.

CAPLUS COPYRIGHT 2012 ACS

Patent Number: US 2012069503
Title: Preparation of N-[(4-substituted piperazin-1-yl)carbonyl]-heteroaryl sulfonamides and analogs as Kv potassium channel blockers
Inventor(s): Dupont-Passelaigue, Elisabeth; Le Roy, Isabelle; Pignier, Christophe
Patent Assignee(s): Pierre Fabre Medicament, Fr.
Source: PCT Int. Appl., 55pp. CODEN: PIXXD2
Language: English

Abstract:
The invention is related to the preparation of heteroaryl sulfonamides I [R1 = one or more substituents of the Ph core X selected from halo, CF3, OCF3, etc.; Z = (CH2)n; n = 0-2; A = O, S; D = CO, CH2O, O; B = N when n = 1-2 and D = CO; or B = CH when n = 0 and D = CH2O or when n = 1 and D = O; R2 = H, Me, F, Cl, OMe; V = (un)substituted pyridinyl, quinolinyl] and their pharmaceutically acceptable salts as blockers of Kv potassium channels, and more particularly of Kv1.5, Kv4.3 or Kv11.1 channels.  Thus, ring opening of 1H-benzo[d][1,3]oxazine-2,4-dione with 2-(1,4-diazepan-1-yl)-4-methylbenzothiazole (preparation given) in the presence of DMAP and reaction of 2-[[4-(4-methylbenzo[d]thiazol-2-yl)-1,4-diazepan-1-yl]carbonyl]aniline with quinoline-8-sulfonyl chloride in the presence of pyridine gave sulfonamide II.  I blocked Kv1.5 channel in a FLIPR assay.  I are useful for treating and/or preventing atrial fibrillation, heart rhythm disorders of the auricles and/or the ventricles, pathologies in which the cell cycle and/or cell proliferation and/or regeneration are impaired, such as cancer or chronic inflammation (no data).

Please note:  Titles and abstracts for patent records in CAplus are routinely enhanced to better describe the claimed invention. In this example, CAS enhanced both the abstract and title using additional information found in the patent. The original title of the PCT publication is Derivatives of heteroarylsulfonamides, their preparation and their application in human therapy. For the CAplus record, this title was enhanced to read Preparation of N-[(4-substituted piperazin-1-yl)carbonyl]-heteroaryl sulfonamides and analogs as Kv potassium channel blockers.

 

View the full-text patent here.

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