BR0116115A - Derivados de carboxamida e seu uso no tratamento de doenças tromboembólicas e tumores - Google Patents

Derivados de carboxamida e seu uso no tratamento de doenças tromboembólicas e tumores

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Publication number
BR0116115A
BR0116115A BR0116115-6A BR0116115A BR0116115A BR 0116115 A BR0116115 A BR 0116115A BR 0116115 A BR0116115 A BR 0116115A BR 0116115 A BR0116115 A BR 0116115A
Authority
BR
Brazil
Prior art keywords
tumors
treatment
thromboembolic diseases
carboxamide derivatives
het
Prior art date
Application number
BR0116115-6A
Other languages
English (en)
Inventor
Dieter Dorsch
Werner Mederski
Christos Tsaklakidis
Betram Cezanne
Johannes Gleitz
Christopher Barnes
Original Assignee
Merck Patent Ges Mit Beschaenk
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 Merck Patent Ges Mit Beschaenk filed Critical Merck Patent Ges Mit Beschaenk
Publication of BR0116115A publication Critical patent/BR0116115A/pt

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/263—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
    • C07D207/27—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A61K47/186—Quaternary ammonium compounds, e.g. benzalkonium chloride or cetrimide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
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    • A61K9/2826—Sugars or sugar alcohols, e.g. sucrose; Derivatives thereof
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    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/26—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring
    • C07C271/28—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring to a carbon atom of a non-condensed six-membered aromatic ring
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    • C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
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    • C07C275/28—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C275/30—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton being further substituted by halogen atoms, or by nitro or nitroso groups
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    • C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
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    • C07C317/32—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
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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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Abstract

"DERIVADOS DE CARBOXAMIDA E SEU USO NO TRATAMENTO DE DOENçAS TROMBOEMBóLICAS E TUMORES". A presente invenção refere-se a compostos da fórmula (I), onde as variáveis têm o significado que segue, D é fenila ou piridila, cada uma delas é não-substituída ou monossubstituída ou polissubstituída por Hal, A, OR^ 2^, N(R^ 2^)~ 2~, NO~ 2~, CN, COOR^ 2^ ou CON(R^ 2^)~ 2~; R^ 1^ e H, Ar, Het, cicloalquila ou A, que pode ser substituído por OR^ 2^, SR^ 2^, N(R^ 2^)~ 2~, Ar, Het, cicloalquila, CN, COOR^ 2^ ou CON(R^ 2^)~ 2~; R^ 2^ é H ou A; E é fenileno, que pode ser monossubstituído ou polissubstituído por Hal, A, OR^ 2^, N(R^ 2^)~ 2~, NO~ 2~, CN, COOR^ 2^ OU CON(R^ 2^)~ 2~, ou é piperidino-1,4-diila; W é Ar, Het ou N(R^ 2^)~ 2~ e, se E = piperidino-1,4-diila, é alternativamente R^ 2^ ou cicloalquila, X é NH ou O, são inibidores do fator de coagulação Xa e podem ser empregados para a profilaxia e/ou terapia de doenças tromboembólicas e para o tratamento de tumores.
BR0116115-6A 2000-12-16 2001-11-21 Derivados de carboxamida e seu uso no tratamento de doenças tromboembólicas e tumores BR0116115A (pt)

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DE10063008A DE10063008A1 (de) 2000-12-16 2000-12-16 Carbonsäureamidderivate
PCT/EP2001/013545 WO2002048099A1 (de) 2000-12-16 2001-11-21 Carbonsäureamidderivate und ihre verwendung in der behandlung von thromboembolischen erkrankungen und tumoren

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