BRPI0509715A - diarylamine derivatives as calcium blocking channels - Google Patents

diarylamine derivatives as calcium blocking channels

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Publication number
BRPI0509715A
BRPI0509715A BRPI0509715-0A BRPI0509715A BRPI0509715A BR PI0509715 A BRPI0509715 A BR PI0509715A BR PI0509715 A BRPI0509715 A BR PI0509715A BR PI0509715 A BRPI0509715 A BR PI0509715A
Authority
BR
Brazil
Prior art keywords
alkyl
calcium
substituted
moiety
channels
Prior art date
Application number
BRPI0509715-0A
Other languages
Portuguese (pt)
Inventor
Hassan Pajouhesh
Hossein Pajouhesh
Yanbing Ding
Terrance P Snutch
Original Assignee
Neuromed Pharmaceuticals Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from US10/821,584 external-priority patent/US20040259866A1/en
Priority claimed from US10/928,564 external-priority patent/US20050227999A1/en
Application filed by Neuromed Pharmaceuticals Ltd filed Critical Neuromed Pharmaceuticals Ltd
Publication of BRPI0509715A publication Critical patent/BRPI0509715A/en

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    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
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    • C07D211/26—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
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    • C07D295/15—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
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Abstract

DERIVADOS DE DIARILAMINA COMO CANAIS BLOQUEADORES DE CáLCIO. A presente invenção refere-se a compostos de piperazina/4-amino piperidina N-diarilaminoalquila substituídos da fórmula 1, onde cada um de A e 6 é independentemente uma porção carbocíclica ou heterocíclica, aromática ou não aromática, de 6 membros ou é uma amino- alquila e onde um e somente um de A e B pode ser H ou alquila (1-8 C) ou onde A e B juntos formam uma porção carbocíclica ou heterocíclica, aromática ou não-aromática, de 6 membros opcionalmente substituída; R¬ 1¬ é H ou alquila (1-8 C), Z é N ou CHNR¬ 2¬ onde R¬ 2¬é H ou alquila (1-8 C), X é alquileno (1-4 C) de cadeia linear onde opcionalmente pelo menos um carbono adjacente a um nitrogênio está na forma de C=O; cada R¬ 3¬ é um substituinte independente; n=0-2; Ar é um anel aromático ou heteroaromático de 6 membros; onde cada porção cíclica incluída em A ou em B e cada porção Ar na fórmula (1) pode ser substituída por um ou mais substituintes. Estes compostos e sais ou conjugados dos mesmos são capazes de bloquear canais de cálcio do tipo N ou do tipo T e são úteis para tratar condições mediadas por atividade de canal de íon cálcio tais como dor crónica.DIARYLAMINE DERIVATIVES AS CALCIUM BLOCKING CHANNELS. The present invention relates to substituted N-diarylaminoalkyl piperazine / 4-amino piperidine compounds of formula 1, wherein each of A and 6 is independently a 6-membered aromatic or non-aromatic carbocyclic or heterocyclic moiety or is an amino alkyl and where one and only one of A and B may be H or alkyl (1-8 C) or where A and B together form an optionally substituted 6-membered carbocyclic or heterocyclic moiety; R¬ 1¬ is H or (1-8 C) alkyl, Z is N or CHNR¬ 2¬ where R¬ 2¬ is H or (1-8 C) alkyl, X is chain (1-4 C) alkylene linear where optionally at least one carbon adjacent to a nitrogen is in the form of C = O; each R¬ 3¬ is an independent substituent; n = 0-2; Ar is a 6 membered aromatic or heteroaromatic ring; wherein each cyclic moiety included in A or B and each Ar moiety in formula (1) may be substituted by one or more substituents. These compounds and salts or conjugates thereof are capable of blocking N-type or T-type calcium channels and are useful for treating conditions mediated by calcium ion channel activity such as chronic pain.

BRPI0509715-0A 2004-04-09 2005-04-08 diarylamine derivatives as calcium blocking channels BRPI0509715A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US10/821,584 US20040259866A1 (en) 1998-06-30 2004-04-09 Calcium channel blockers comprising two benzhydril moieties
US10/928,564 US20050227999A1 (en) 2004-04-09 2004-08-27 Diarylamine derivatives as calcium channel blockers
PCT/CA2005/000544 WO2005097779A1 (en) 2004-04-09 2005-04-08 Diarylamine derivatives as calcium channel blockers

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