AR051473A1 - Derivados de dicarboxamida, metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en la elaboracion de medicamentos para el tratamiento de enfermedades asociadas al factor de coagulacion xa. - Google Patents

Derivados de dicarboxamida, metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en la elaboracion de medicamentos para el tratamiento de enfermedades asociadas al factor de coagulacion xa.

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AR051473A1
AR051473A1 ARP050104572A ARP050104572A AR051473A1 AR 051473 A1 AR051473 A1 AR 051473A1 AR P050104572 A ARP050104572 A AR P050104572A AR P050104572 A ARP050104572 A AR P050104572A AR 051473 A1 AR051473 A1 AR 051473A1
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alkyl
alkoxy
carbonyl
optionally substituted
amino
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Hoffmann La Roche
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    • C07D213/02—Heterocyclic 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
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    • C07D213/60—Heterocyclic 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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    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
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    • 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
    • C07D295/12—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 singly or doubly bound nitrogen atoms
    • C07D295/135—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 singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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    • 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
    • C07D295/16—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 acylated on ring nitrogen atoms
    • C07D295/18—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 acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
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    • C07D401/12—Heterocyclic 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 linked by a chain containing hetero atoms as chain links
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    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
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  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)

Abstract

Estos compuestos inhiben el factor de coagulacion Xa y pueden utilizarse como medicamentos. Composiciones farmacéuticas que los contienen. Reivindicacion 1: Compuestos de la formula (1) D-NH-C(O)-E-A-B-Rc en la que A es -CONH o -NHCO-; B es fenilo opcionalmente sustituido, heteroarilo opcionalmente sustituido o heterociclilo opcionalmente sustituido; Rc es arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido o heterociclilo opcionalmente sustituido, uno o dos átomos de C de dicho anillo arilo, heteroarilo o heterociclilo pueden estar opcionalmente sustituidos con un grupo carbonilo; D es arilo opcionalmente sustituido con 1, 2 o 3 átomos de halogeno elegidos con independencia entre Cl, F, y Br o heteroarilo opcionalmente sustituido con 1, 2 o 3 átomos de halogeno elegidos con independencia entre Cl, F y Br; E es E-1, E-2 o E-3 como se muestra en los restos de formulas que los representan. R1 y R2 con independencia entre sí son H, halogeno, alquilo C1- 6, cicloalquilo C3-7 (cicloalquil C3-7)-alquilo C1-6, amino, amino monosustituido, amino disustituido, hidroxi, alcoxi C1-6, (amino monosustituido)-alquilo C1-6, (amino disustituido)-alquilo C1-6, hidroxil-alquilo C1-6 o R1 y R2 juntos forman =O o =C(R11)(R12), o R1 y R2 están unidos entre sí para formar heterociclilo opcionalmente sustituido, junto con el átomo de C al que R1 y R2 están unidos; R3 y R4 con independencia entre sí son H, alquilo C1-6, carboxilo, (alcoxi C1-6)-carbonilo, carbamoílo, (amino mono- o disustituido)-carbonilo, (heterociclilo opcionalmente sustituido)-carbonilo, (heteroarilo opcionalmente sustituido)-carbonilo, (arilo opcionalmente sustituido)-carbonilo, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, heterociclilo opcionalmente sustituido, hidroxil-alquilo C1-6, halo-alquilo C1-6, ciano-alquilo C1-6, (alcoxi C1-6)-alquilo C1-6, amino-alquilo C1-6, (amino mono- o disustituido)-alquilo C1-6, (arilo opcionalmente sustituido)-alquilo C1-6, (heterociclilo opcionalmente sustituido)-alquilo C1-6, (heteroarilo opcionalmente sustituido)-alquilo C1-6, (arilo opcionalmente sustituido)-(alcoxi C1-6)-alquilo C1-6, (heterociclilo opcionalmente sustituido)-(alcoxi C1-6)- alquilo C1-6, (heteroarilo opcionalmente sustituido)-(alcoxi C1-6)-alquilo C1-6, o R3 y R4 están unidos entre sí para formar cicloalquilo C3-7, junto con el átomo de C al que R3 y R4 están unidos; R5 y R6 con independencia entre sí son H, alquilo C1- 6, ciano, (alcoxi C1-6)-carbonilo, (alqueniloxi C2-6)-carbonilo, (alquiniloxi C2-6)-carbonilo, hidroxil-alquilo C1-6, (alcoxi C1-6)-carbonilo, carboxilo, (amino mono- o disustituido con alquilo C1-6)-carbonilo, aminocarbonilo, (heterociclilo opcionalmente sustituido)-carbonilo, (heteroarilo opcionalmente sustituido)-carbonilo o (arilo opcionalmente sustituido)-carbonilo; R7, R8, R9 y R10 con independencia entre sí son H, alquilo C1-6 o hidroxi; R11 y R12 con independencia entre sí son H, alquilo C1-6 o alquenilo C2-6; y las sales farmacéuticamente aceptables de los mismos; en los que el término ôfenilo opcionalmente sustituidoö significa un grupo fenilo opcionalmente sustituido de 1 a 5 veces por sustituyentes elegidos con independencia entre sí entre el grupo formado por halogeno, hidroxi, alquilo C1-6, halo-alquilo C1-6, alcoxi C1-6, alquilsulfonilo C1-6, alquilsulfinilo C1-6, alquiltio C1-6, amino, amino-alquilo C1-6, (amino mono- o disustituido)-alquilo C1-6, nitro, ciano, acilo, carbamoílo, amino mono o disustituido, aminocarbonilo, (amino mono- o disustituido)-carbonil-alcoxi C1-6, hidroxi-alquilo C1-6, carboxilo, (alcoxi C16)-carbonilo, aril-alcoxi C1-6, heteroaril-alcoxi C1-6, heterociclil-alcoxi C1- 6, (alcoxi C1-6)-carbonil-alcoxi C1-6, carbamoil-alcoxi C1-6 y carboxil-alcoxi C1-6; el término ôariloö significa fenilo o naftilo; el término ôarilo opcionalmente sustituidoö significa un grupo arilo opcionalmente sustituido e 1 a 5 veces por sustituyentes elegidos con independencia entre sí entre el grupo formado por halogeno, hidroxi, alquilo C1-6, halo-alquilo C1-6, alcoxi C1-6, alquilsulfonilo C1-6, alquilsulfinilo C1-6, alquiltio C1-6, amino, amino-alquilo C1-6, (amino mono- o disustituido)-alquilo C1-6, nitro, ciano, acilo, carbamoílo, amino mono- o disustituido, aminocarbonilo, (amino mono- o disustituido)-carbonilo, aminocarbonil-alcoxi C1-6, (amino mono- o disustituido)-carbonil-alcoxi C1-6, hidroxi-alquilo C1-6, carboxilo, (alcoxi C1-6)-carbonilo, aril-alcoxi C1-6, heteroaril-alcoxi C1-6, heterociclil-alcoxi C1-6, (alcoxi C1-6)-carbonil-alcoxi C1-6, carbamoil-alcoxi C1-6 y carboxil-alcoxi C1-6; el término ôheterocicliloö significa radicales monocíclicos no aromáticos de tres a ocho átomos en el anillo en los que uno o dos átomos del anillo son heteroátomos elegidos entre N, O o S(O)n (en el que n es un numero entero de 0 a 2), los demás átomos del anillo son C, y 1 o 2 átomos de C del anillo pueden reemplazarse por un grupo carbonilo; el término ôheterociclilo opcionalmente sustituidoö significa un grupo heterociclilo, que está opcionalmente sustituido con independencia entre sí con 1, 2 o 3 sustituyentes elegidos entre el grupo formado por halogeno, hidroxi, alquilo C1-6, halo-alquilo C1-6, alcoxi C1-6, alquilsulfonilo C1-6, alquilsulfinilo C1-6, alquiltio C1-6, amino, amino-alquilo C1-6, (amino mono- o disustituido)-alquilo C1-6, nitro, ciano, acilo, carbamoílo, amino mono- o disustituido, aminocarbonilo, (amino mono- o disustituido)-carbonilo, aminocarbonil-alcoxi C1-6, (amino mono- o disustituido)-carbonil-alcoxi C1-6, hidroxi-alquilo C1-6, carboxilo, (alcoxi C1-6)-carbonilo, aril-alcoxi C1-6, heteroaril-alcoxi C1-6, heterociclil-alcoxi C1-6, (alcoxi C1-6)-carbonil-alcoxi C1-6, carbamoil-alcoxi C1-6 y carboxil-alcoxi C1-6; el término ôheteroariloö significa un radical monocíclico o bicíclico de 5 a 12 átomos en el anillo que tiene por lo menos un anillo aromático que contiene 1, 2 o 3 heteroátomos en el anillo elegidos entre N, O y S, lo demás átomos del anillo son C, dando por supuesto que el punto de union del radical heteroarilo estará situado en un anillo aromático, y 1 o 2 átomos de C del anillo pueden reemplazarse por un grupo carbonilo; el término ôheteroarilo opcionalmente sustituidoö significa un grupo heteroarilo, que está opcionalmente sustituido con independencia entre sí por 1, 2 o 3 sustituyentes elegidos entre el grupo formado por halogeno, hidroxi, alquilo C1-6, halo-alquilo C1-6, alcoxi C1-6, alquilsulfonilo C1-6, alquilsulfinilo C1-6, alquiltio C1-6, amino, amino-alquilo C1-6, (amino mono- o disustituido)-alquilo C1-6, nitro, ciano, acilo, carbamoílo, amino mono- o disustituido, aminocarbonilo, (amino mono- o disustituido)-carbonilo, aminocarbonil-alcoxi C1-6, (amino mono- o disustituido)-carbonil-alcoxi C1-6, hidroxi-alquilo C1-6, carboxilo, (alcoxi C1-6)-carbonilo, aril-alcoxi C1-6, heteroaril-alcoxi C1-6, heterociclil-alcoxi C1-6, (alcoxi C1-6)-carbonil-alcoxi C1-6, carbamoil-alcoxi C1-6 y carboxil-alcoxi C1-6; el término ôamino monosustituidoö y ôamino disustituidoö significan -NHR y -NRR' respectivamente, en los que R y R' se eligen con independencia entre sí entre el grupo formado por hidroxi, alquilo C1-6, hidroxi-alquilo C1-6, (alcoxi C1-6)-alquilo C1-6, carbamoil alquilo C1-6, halo-alquilo C1-6, cicloalquilo C3-7, (cicloalquil C3-7)-alquilo C1-6, alcoxi C1-6, alquilsulfonilo C1- 6, alquilsulfinilo C1-6, alquiltio C1-6, (amino mono- o disustituido con alquilo C1-6)-sulfonilo, (amino mono- o disustituido con alquilo C1-6)-sulfinilo, (amino mono- o disustituido con alquilo C1-6)-tio o (amino mono- o disustituido con alquilo C1- 6)-alquilo C1-6 o (amino mono- o disustituido con alquilo C1-6)-carbonil-alquilo C1-6, acilo, (haloalquil C1-6)-carbonilo y (alcoxi C1-6)-carbonilo; el término ôaciloö significa -C(=O)R, en el que R es H o alquilo C1-6; el término ôhaloalquilo C1-6ö significa alquilo C1-6 sustituido con uno o varios átomos de halogeno iguales o diferentes elegidos con independencia entre sí entre el grupo formado por Cl, F, y Br. Reivindicacion 60: Compuestos de la formula (2) que son enantioméricamente puros. Reivindicacion 61: Compuestos de la formula (3). Reivindicacion 62: Compuestos de la formula (4) en la que tiene el significado definido en una cualquiera de las reivindicaciones 1-3. Reivindicacion 63: Compuestos de la formula (5) en la que D tiene el significado definido en una cualquiera de las reivindicaciones 1-3. Reivindicacion 64: Compuestos de la formula (6) en la que B, Rc y D tienen los significados definidos en una cualquiera de las reivindicaciones 1-3. Reivindicacion 65: Compuestos de la formula (7) en la que B, Rc y D tienen los significados definidos en una cualquiera de las reivindicaciones 1-3.
ARP050104572A 2004-11-03 2005-11-01 Derivados de dicarboxamida, metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en la elaboracion de medicamentos para el tratamiento de enfermedades asociadas al factor de coagulacion xa. AR051473A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP04105465 2004-11-03
EP05100132 2005-01-12

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AR (1) AR051473A1 (es)
AT (1) ATE496030T1 (es)
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US7550487B2 (en) * 2004-03-26 2009-06-23 Hoffmann-La Roche Inc. Pyrrolidine-3,4-dicarboxamide derivatives
WO2006138304A2 (en) * 2005-06-14 2006-12-28 Taigen Biotechnology Pyrimidine compounds
US7678917B2 (en) * 2005-09-01 2010-03-16 Hoffman-La Roche Inc. Factor Xa inhibitors
EP1847537A1 (en) * 2006-04-21 2007-10-24 F. Hoffmann-La Roche Ag Dicarboxamide derivatives
RU2011122942A (ru) 2011-06-08 2012-12-20 Общество С Ограниченной Ответственностью "Асинэкс Медхим" Новые ингибиторы киназ
US10399948B2 (en) 2015-02-10 2019-09-03 Vanderbilt University Negative allosteric modulators of metabotropic glutamate receptor 3
EP3078378B1 (en) 2015-04-08 2020-06-24 Vaiomer Use of factor xa inhibitors for regulating glycemia

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EP0630366B1 (en) * 1991-10-15 2003-01-02 G.D. Searle & Co. Substituted heterocyclic derivatives useful as platelet aggregation inhibitors
DE4400749A1 (de) * 1994-01-13 1995-07-20 Bayer Ag Neues hochenantioselektives Verfahren zur Herstellung von enantiomerenreinen Cyclopentan- und -penten-beta-Aminosäuren
DE19801646A1 (de) * 1998-01-17 1999-07-22 Bayer Ag Substituierte alpha,beta-annellierte Butyrolactone
CA2374793A1 (en) 1999-05-24 2000-11-30 Penglie Zhang Inhibitors of factor xa
ES2254385T3 (es) 2000-02-29 2006-06-16 Millennium Pharmaceuticals, Inc. Benzamidas e inhibidores relacionados del factor xa.
US7030141B2 (en) * 2001-11-29 2006-04-18 Christopher Franklin Bigge Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
JP4140294B2 (ja) 2002-07-05 2008-08-27 日産自動車株式会社 燃料電池システム
AU2003279735A1 (en) * 2002-10-02 2004-04-23 Bristol-Myers Squibb Company Lactam-containing diaminoalkyl, beta-aminoacids, alpha-aminoacids and derivatives thereof as factor xa inhibitors
DE10254336A1 (de) 2002-11-21 2004-06-03 Merck Patent Gmbh Carbonsäureamide
JP2004210716A (ja) * 2002-12-27 2004-07-29 Dai Ichi Seiyaku Co Ltd ジアミド誘導体
DE10302500A1 (de) 2003-01-23 2004-07-29 Merck Patent Gmbh Carbonsäureamidderivate
US7205318B2 (en) * 2003-03-18 2007-04-17 Bristol-Myers Squibb Company Lactam-containing cyclic diamines and derivatives as a factor Xa inhibitors
US7550487B2 (en) * 2004-03-26 2009-06-23 Hoffmann-La Roche Inc. Pyrrolidine-3,4-dicarboxamide derivatives
EP1847537A1 (en) * 2006-04-21 2007-10-24 F. Hoffmann-La Roche Ag Dicarboxamide derivatives

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MX2007005113A (es) 2007-06-26
BRPI0517964A (pt) 2008-10-28
JP2008518985A (ja) 2008-06-05
CA2585615C (en) 2013-11-26
US20090270360A1 (en) 2009-10-29
IL182811A (en) 2014-01-30
ATE496030T1 (de) 2011-02-15
JP4943340B2 (ja) 2012-05-30
KR100884146B1 (ko) 2009-02-17
EP1814855B1 (en) 2011-01-19
US7501413B2 (en) 2009-03-10
ZA200703488B (en) 2008-09-25
CA2585615A1 (en) 2006-05-11
AU2005300828A1 (en) 2006-05-11
RU2007120685A (ru) 2008-12-10
IL182811A0 (en) 2007-08-19
CN101094835A (zh) 2007-12-26
CN101094835B (zh) 2011-07-27
TW200630099A (en) 2006-09-01
WO2006048152A3 (en) 2006-09-21
AU2005300828B2 (en) 2012-03-08
KR20070085678A (ko) 2007-08-27
US20060106016A1 (en) 2006-05-18
WO2006048152A2 (en) 2006-05-11
EP1814855A2 (en) 2007-08-08
DE602005026047D1 (de) 2011-03-03
NO20072247L (no) 2007-06-26

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