BR0012601A - Precursores de drogas com efeito antipalúdico, derivados ciclizados, processos de obtenção de precursores de tiazólio e de haloalquilaminas, composições farmacêuticas, e, utilização de sais de bis-amÈnio quaternário - Google Patents

Precursores de drogas com efeito antipalúdico, derivados ciclizados, processos de obtenção de precursores de tiazólio e de haloalquilaminas, composições farmacêuticas, e, utilização de sais de bis-amÈnio quaternário

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Publication number
BR0012601A
BR0012601A BR0012601-2A BR0012601A BR0012601A BR 0012601 A BR0012601 A BR 0012601A BR 0012601 A BR0012601 A BR 0012601A BR 0012601 A BR0012601 A BR 0012601A
Authority
BR
Brazil
Prior art keywords
alkyl
group
precursors
represent
formula
Prior art date
Application number
BR0012601-2A
Other languages
English (en)
Inventor
Henri Vial
Michele Calas
Marie-Laure Ancelin
Jean-Jacques Bourguignon
Valerie Vidal
Bric Rubi
Original Assignee
Centre Nat Rech Scient
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
Application filed by Centre Nat Rech Scient filed Critical Centre Nat Rech Scient
Publication of BR0012601A publication Critical patent/BR0012601A/pt

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—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
    • C07D295/04—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
    • C07D295/14—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
    • C07D295/155—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 separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/541—Organic ions forming an ion pair complex with the pharmacologically or therapeutically active agent
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/01—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms
    • C07C211/02—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C211/09—Diamines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/23—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C323/39—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton at least one of the nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom
    • C07C323/40—Y being a hydrogen or a carbon atom
    • C07C323/41—Y being a hydrogen or an acyclic carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C327/00—Thiocarboxylic acids
    • C07C327/20—Esters of monothiocarboxylic acids
    • C07C327/30—Esters of monothiocarboxylic acids having sulfur atoms of esterified thiocarboxyl groups bound to carbon atoms of hydrocarbon radicals substituted by nitrogen atoms, not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C327/00—Thiocarboxylic acids
    • C07C327/20—Esters of monothiocarboxylic acids
    • C07C327/32—Esters of monothiocarboxylic acids having sulfur atoms of esterified thiocarboxyl groups bound to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • C07C327/34—Esters of monothiocarboxylic acids having sulfur atoms of esterified thiocarboxyl groups bound to carbon atoms of hydrocarbon radicals substituted by carboxyl groups with amino groups bound to the same hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/24—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/30—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrrole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

"PRECURSORES DE DROGAS COM EFEITO ANTIPALúDICO, DERIVADOS CICLIZADOS, PROCESSOS DE OBTENçãO DE PRECURSORES DE TIAZóLIO E DE HALOALQUILAMINAS, COMPOSIçõES FARMACêUTICAS, E, UTILIZAçãO DE SAIS DE BISAMÈNIO QUATERNáRIO". A invenção refere-se a precursores de drogas com efeito antipalúdico caracterizados pelo fato de que se trata de sais de bis-amónio quaternário de fórmula geral ( I ) em que<UM>A<MV> e <UM>A<MV><39>, iguais ou diferentes, são, respectivamente, ou um grupo A~ 1~, e A<39>~ 1~, de fórmula ( 1 ) em que n=2 a 4; R<39>~ 1~, é hidrogênio, alquila com C1 a C5, eventualmente substituído por um arila, um hidróxi, um alcóxi, em que o alquila compreende de 1 a 5 C, ou arilóxi e W é halogênio ou um grupo nucleófugo, ou um grupo A~ 2~ que representa um formila -CHO, ou acetila -COCH~ 3. B~ 1~ e B<39>~ 1~, iguais ou diferentes, representam: respectivamente, ou os grupos B~ 1~ e B<39>~ 1~, se <UM>A<MV> e <UM>A<MV><39> representam respectivamente <UM>A<MV>~ 1~ e <UM>A<MV><39>~ 1~, <UM>B<MV>~ 1~ e <UM>B,MV><39>~ 1~ representando um grupo R~ 1~, que apresenta a mesma definição que <UM>R<MV>~ 1~, acima, mas não pode ser um átomo de hidrogênio, ou, respectivamente, os grupos <UM>B<MV>~ 2~ e <UM>B<MV><39>~ 2~, se <UM>A<MV> e <UM>A<MV><39> representam <UM>A<MV>~ 2~, <UM>B<MV>~ 2~ ou B<39><sym>~ 2~ sendo o grupo <UM>R<MV>~ 1~ como definido acima, ou um grupamento de fórmula ( 2 ) em que -Ra é RS- ou RCO-, em que R é um alquila com C1 a C6, substituído, conforme o caso, um fenila ou benzila, em que o fenila é substituído, conforme o caso, sendo que estes são eventualmente substituídos R~ 2~ é hidrogênio alquila, com C1 a C5, ou um grupo -CH~ 2~-COO-alquila ( C1 a C5 ); e R~ 3~ é hidrogênio, alquila ou alquenila com C1 a C5, substituído, conforme o caso, um fosfato, um alcóxi, em que o alquila tem C1 a C3, ou arilóxi; ou um alquil ( ou aril ) carbonilóxi; ou R~ 2~ e R~ 3~ formam, em conjunto, um ciclo com 5 ou 6 C; R e R~ 3~ podendo ser ligados para formar um ciclo. <244> representa: ou uma ligação simples, quando <UM>A<MV> e <UM>A<MV><39> representam <UM>A<MV>~ 1~ e <UM>A<MV><39>~ 1~,: ou quando <UM>A<MV> e <UM>A<MV><39> representam <UM>A<MV>~ 1~, e B~ 2 e B~<39>~ 2~ representam: ou, quando <UM>A<MV> E <UM>A<MV><39> são CHO ou COCH3 e B~ 2~ e B<39>~ 2~ são R~ 1~, um grupamento de fórmula ( 4 ), ou um grupamento de fórmula ( 5 ) em que ( a ) representa uma ligação no sentido de Z e ( b ) uma ligação no sentido do átomo de nitrogênio. Z é um alquila com C9 a C21, conforme o caso com inserção de uma ou de várias ligações múltiplas, e/ou de um ou vários heteroátomos O e/ou S, e/ou de um ou de vários ciclos aromáticos, e os sais farmaceuticamente aceitáveis destes compostos. Aplicações destes precursores e derivados ciclizados de tiazólio como drogas anti-parasitárias, em particular antipalúdicos e anti-babesioses.
BR0012601-2A 1999-07-21 2000-07-21 Precursores de drogas com efeito antipalúdico, derivados ciclizados, processos de obtenção de precursores de tiazólio e de haloalquilaminas, composições farmacêuticas, e, utilização de sais de bis-amÈnio quaternário BR0012601A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR9909471A FR2796642B1 (fr) 1999-07-21 1999-07-21 Precurseurs de sels de bis-ammonium quaternaire et leurs applications comme prodrogues ayant une activite anti-parasitaire
PCT/FR2000/002122 WO2001005742A1 (fr) 1999-07-21 2000-07-21 Precurseurs de sels de bis-ammonium quaternaire et leurs applications comme prodrogues ayant une activite anti-parasitaire

Publications (1)

Publication Number Publication Date
BR0012601A true BR0012601A (pt) 2002-05-21

Family

ID=9548361

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0012601-2A BR0012601A (pt) 1999-07-21 2000-07-21 Precursores de drogas com efeito antipalúdico, derivados ciclizados, processos de obtenção de precursores de tiazólio e de haloalquilaminas, composições farmacêuticas, e, utilização de sais de bis-amÈnio quaternário

Country Status (21)

Country Link
US (1) US6972343B1 (pt)
EP (1) EP1196371B1 (pt)
JP (1) JP4431853B2 (pt)
CN (2) CN1181043C (pt)
AP (1) AP1412A (pt)
AT (1) ATE308507T1 (pt)
AU (1) AU783267C (pt)
BR (1) BR0012601A (pt)
CA (1) CA2379891C (pt)
DE (1) DE60023703T2 (pt)
DK (1) DK1196371T3 (pt)
ES (1) ES2252050T3 (pt)
FR (1) FR2796642B1 (pt)
HK (1) HK1047922B (pt)
HU (1) HU229084B1 (pt)
IL (2) IL147710A0 (pt)
MX (1) MXPA02000711A (pt)
OA (1) OA11994A (pt)
PL (1) PL200314B1 (pt)
WO (1) WO2001005742A1 (pt)
ZA (1) ZA200200903B (pt)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007513888A (ja) * 2003-11-24 2007-05-31 ユニバーシティ オブ ノース カロライナ アット チャペル ヒル 縮合環ジカチオン性抗原虫剤及びそれらのプロドラッグ
FR2926993B1 (fr) * 2008-02-06 2011-03-11 Sanofi Aventis Association entre un sel de bis-thiazolium ou l'un de ses precurseurs et l'artemisinine ou l'un de ses derives pour le traitement du paludisme
CN101711527B (zh) * 2009-12-31 2013-02-20 蚌埠丰原医药科技发展有限公司 一种杀菌组合物及其制备方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3131220A (en) * 1958-07-09 1964-04-28 Smith Kline French Lab Tetrasubstituted polymethylenediamine salts
GB1006790A (en) * 1963-04-28 1965-10-06 Takeda Chemical Industries Ltd New thiamine derivatives and the preparation thereof
FR2751967B1 (fr) * 1996-07-31 1998-10-09 Virbac Sa Agents antipaludeens et antibabesioses et compositions pharmaceutiques les contenant

Also Published As

Publication number Publication date
AU783267B2 (en) 2005-10-06
ZA200200903B (en) 2003-07-30
MXPA02000711A (es) 2003-07-14
DE60023703D1 (de) 2005-12-08
CN1733699A (zh) 2006-02-15
HUP0202108A3 (en) 2005-06-28
IL147710A (en) 2007-08-19
EP1196371B1 (fr) 2005-11-02
AP2002002412A0 (en) 2002-03-31
DK1196371T3 (da) 2006-03-20
ATE308507T1 (de) 2005-11-15
CA2379891C (fr) 2014-03-25
CN100467440C (zh) 2009-03-11
EP1196371A1 (fr) 2002-04-17
WO2001005742A1 (fr) 2001-01-25
US6972343B1 (en) 2005-12-06
FR2796642A1 (fr) 2001-01-26
PL200314B1 (pl) 2008-12-31
AP1412A (en) 2005-05-17
AU783267C (en) 2006-08-17
CN1372539A (zh) 2002-10-02
IL147710A0 (en) 2002-08-14
PL353592A1 (en) 2003-12-01
CN1181043C (zh) 2004-12-22
CA2379891A1 (fr) 2001-01-25
AU7006900A (en) 2001-02-05
DE60023703T2 (de) 2006-07-27
HK1047922B (zh) 2006-10-13
JP4431853B2 (ja) 2010-03-17
HK1047922A1 (en) 2003-03-14
JP2003505357A (ja) 2003-02-12
OA11994A (fr) 2006-04-18
HUP0202108A2 (en) 2002-10-28
HU229084B1 (en) 2013-07-29
FR2796642B1 (fr) 2001-10-19
ES2252050T3 (es) 2006-05-16

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