AR047850A1 - Derivados de amida de acido carboxilico. obtencion y composiciones farmaceuticas que los contienen. - Google Patents

Derivados de amida de acido carboxilico. obtencion y composiciones farmaceuticas que los contienen.

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Publication number
AR047850A1
AR047850A1 ARP040104655A ARP040104655A AR047850A1 AR 047850 A1 AR047850 A1 AR 047850A1 AR P040104655 A ARP040104655 A AR P040104655A AR P040104655 A ARP040104655 A AR P040104655A AR 047850 A1 AR047850 A1 AR 047850A1
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Argentina
Prior art keywords
mono
atoms
hal
con
unsubstituted
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ARP040104655A
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English (en)
Inventor
Bertram Cezanne
Dorsch Chem Dieter
Werner Mederski
Christos Tsaklakidis
Johannes Gleitz
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Merck Patent Gmbh
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Publication of AR047850A1 publication Critical patent/AR047850A1/es

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    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
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    • A61P25/00Drugs for disorders of the nervous system
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00Drugs for disorders of the cardiovascular system
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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    • C07D211/08Heterocyclic 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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    • C07D211/06Heterocyclic 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
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    • C07D211/18Heterocyclic 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
    • C07D211/30Heterocyclic 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 doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom
    • C07D211/32Heterocyclic 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 doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom by oxygen atoms
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    • C07D211/06Heterocyclic 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
    • C07D211/36Heterocyclic 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 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
    • C07D211/40Oxygen atoms
    • C07D211/44Oxygen atoms attached in position 4
    • C07D211/46Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
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    • C07D211/06Heterocyclic 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
    • C07D211/36Heterocyclic 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 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
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    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
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    • C07D211/06Heterocyclic 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
    • C07D211/36Heterocyclic 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 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
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    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
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    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
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    • C07D295/16Heterocyclic 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 acylated on ring nitrogen atoms
    • C07D295/18Heterocyclic 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 acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182Radicals derived from carboxylic acids
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    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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  • Hydrogenated Pyridines (AREA)
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Abstract

Los nuevos compuestos de la formula (1) en donde: D es un carbociclo o heterociclo aromático mono o bicíclico insustituido o mono o polisustituido con Hal, A, OR2, N(R2)2, NO2, CN, COOR2, CON(R2)2 o -C:::CH con 0 a 4 átomos de N, O y/o S, X es NR3 u O; Y es O, S, NH, N-CN o N-NO2; R1 es H, Ar, Het, cicloalquilo o A, que puede estar mono, di o trisustituido con OR2, SR2, S(O)mR2, SO2N(R2)2,SO3R2, S(=O)(=NR2)R2, NR2SO2R2, OSO2R2, OSO2N(R2)2, N(R2)2, CN, COOR2, CON(R2)2, Ar, Het o cicloalquilo; E es CH o N; Z está ausente o es un grupo (CH2)q insustituido o monosustituido con el O del carbonilo (=O), en donde uno o dos grupos CH2 pueden estar reemplazados por átomos de N, O y/o S y/o por un grupo -CH=CH-, Z' está ausente o es un grupo (CH2)q' insustituido o monosustituido con el O del carbonilo (=O), en donde uno o dos grupos CH2 pueden estar reemplazados por átomos de N, O y/o S y/o por un grupo -CH:::CH-, Q está ausente, es O, NR2, C=O, SO2 o C(R2)n; R2 es H, A, -[C(R3)2]n-Ar', -[C(R3)2]nHet', -[C(R3)2]n-cicloalquilo, -[C(R3)2]n-N(R3)2 o -[C(R3)2]n-OR3; R3 es H o A; R4, R4' cada uno, de modo independiente entre sí, está ausente, son A, OH u OA; R4 y R4' también son juntos metileno o etileno, T es un carbociclo o heterociclo mono o bicíclico saturado, insaturado o aromático con 0 a 4 átomos de N, O y/o S, que puede estar mono, di o trisustituido con =O, =S, =NH, =NR3, =NOR3, =NCOR3, =NCOOR3, =NOCOR3, R3, Hal, A, -[C(R3)2]n-Ar, -[C(R3)2]n-Het, -[C(R3)2]n- cicloalquilo, OR3, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3CON(R3)2, NR3SO2A, COR3, SO2NR2 y/o S(O)nA; A es alquilo no ramificado o ramificado con 1-10 átomos de C, en donde uno o dos grupos CH2 pueden estar reemplazados por átomos de O o S y/o por grupos -CH=CH- y/o también 1-7 átomos de H pueden estar reemplazados por F; Ar es fenilo, naftilo o bifenilo insustituido o mono, di o trisustituido con Hal, A, OR2, N(R2)2, NO2, CN, COOR2, CON(R2)2, NR2COA, NR2SO2A, COR2, SO2N(R2)2, -[C(R3)2]n- COOR2, -O-[C(R3)2]o-COOR2, SO3H o S(O)nA; Ar' es fenilo insustituido o mono, di o trisustituido con Hal, A, OR3, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3CON(R3)2, NR3SO2A, COR3, SO2N(R3)2, S(O)nA, -[C(R3)2]n-COOR3 u -O-[C(R3)2]o-COOR3; Het es un heterociclo mono o bicíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que puede estar insustituido o mono, di o trisustituido con el O del carbonilo (=O), =S, =N(R2)2, Hal, A, -[C(R3)2]n-Ar, -[C(R3)2]n-Het', -[C(R3)2]n- cicloalquilo, -[C(R3)2]n-OR2, -[C(R3)2]n-N(R3)2, NO2, CN, -[C(R3)2]n-COOR2, -[C(R3)2]n-CON(R2)2, -[C(R3)2]n-NR2COA, NR2CON(R2)2, -[C(R3)2]n-NR2SO2A, COR2, SO2N(R2)2 y/o S(O)nA; Het' es un heterociclo mono o bicíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que puede estar insustituido o mono o disustituido con el O del carbonilo, =S, =N(R3)2, Hal, A, OR3, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3CON(R3)2, NR3SO2A, COR3, SO2N(R3)2 y/o S(O)nA; Hal es F, Cl, Br o I; m es 1 o 2; n es 0, 1 o 2; o es 1, 2 o 3; p es 1, 2, 3, 4 o 5; q, q' son cada uno, de modo independiente entre sí, 0, 1, 2, 3 o 4, en donde al menos uno de los grupos Z o Z' está ausente, y 0<q + q <6, así como sus derivados, solvatos, sales y estereoisomeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones. Son inhibidores del factor de coagulacion Xa y se pueden emplear para la profilaxis y/o la terapia de enfermedades tromboembolicas y para el tratamiento de tumores. Obtencion y composiciones farmacéuticas.
ARP040104655A 2003-12-15 2004-12-15 Derivados de amida de acido carboxilico. obtencion y composiciones farmaceuticas que los contienen. AR047850A1 (es)

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DE10358539A DE10358539A1 (de) 2003-12-15 2003-12-15 Carbonsäureamidderivate

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AR047850A1 true AR047850A1 (es) 2006-03-01

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CA2549548A1 (en) 2005-06-23
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JP4990627B2 (ja) 2012-08-01
US20070123509A1 (en) 2007-05-31
BRPI0417153A (pt) 2007-03-06
DE10358539A1 (de) 2005-07-07
JP2007513987A (ja) 2007-05-31
AU2004296956B2 (en) 2010-11-11
EP1694643A1 (de) 2006-08-30
KR20060123305A (ko) 2006-12-01
AU2004296956A1 (en) 2005-06-23
CN1890216A (zh) 2007-01-03
US7951804B2 (en) 2011-05-31
WO2005056528A1 (de) 2005-06-23

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