AR043062A1 - Ureas sustituidas y carbamatos utiles para el tratamiento de la enfermedad de alzheimer - Google Patents
Ureas sustituidas y carbamatos utiles para el tratamiento de la enfermedad de alzheimerInfo
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- AR043062A1 AR043062A1 ARP030104378A ARP030104378A AR043062A1 AR 043062 A1 AR043062 A1 AR 043062A1 AR P030104378 A ARP030104378 A AR P030104378A AR P030104378 A ARP030104378 A AR P030104378A AR 043062 A1 AR043062 A1 AR 043062A1
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- Prior art keywords
- alkyl
- heteroaryl
- aryl
- optionally substituted
- alkoxy
- Prior art date
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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
- C07C311/47—Y being a hetero atom
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- A61P25/00—Drugs for disorders of the nervous system
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- C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
- C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C271/20—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by nitrogen atoms not being part of nitro or nitroso groups
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- C07C271/42—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
- C07C271/52—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by nitrogen atoms not being part of nitro or nitroso groups
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- C07C275/04—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 acyclic carbon atoms
- C07C275/20—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 acyclic carbon atoms of an unsaturated carbon skeleton
- C07C275/24—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 acyclic carbon atoms of an unsaturated carbon skeleton containing six-membered aromatic rings
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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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- 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
- 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
- C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
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- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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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- 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
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- C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings 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
- C07D309/14—Nitrogen atoms not forming part of a nitro radical
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- C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
- C07D311/58—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4
- C07D311/68—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4 with nitrogen atoms directly attached in position 4
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Abstract
Los compuestos son útiles para el tratamiento de la enfermedad de Alzheimer y otras enfermedades similares. Los compuestos incluyen inhibidores de la enzima beta-secretasa que son útiles para el tratamiento de la enfermedad de Alzheimer y otras enfermedades caracterizadas por el depósito de péptido A beta en un mamífero. Los compuestos de la invención son útiles en composiciones farmacéuticas y métodos de tratamiento para reducir la formación de péptido A beta. Reivindicación 1: Un compuesto de la fórmula (1) o sales o ésteres farmacéuticamente aceptable de los mismos; en donde X está ausente -(C=O)-, -(C=S)-, -S(O)n1- o -(C=N-Z), en donde Z=R20 o -OR20, y en donde n1 es 0, 1 o 2; T está ausente, NR20, u O, con la condición de que cuando X es -(C=O), T no está ausente; en donde cada R20 es en forma independiente H, -CN, alquilo o alquenilo, haloalquilo C1-6 o cicloalquilo C4-7, con la condición de que cuando Z es R20 o -OR20, R20 no es -CN; en donde R1 es -(CH2)1-2-S(O)0-2-(alquilo C1-6), o alquilo C1-10 substituido en forma opcional con 1, 2, o 3 grupos seleccionados en forma independiente de halógeno, -OH, -O, -SH, -C:::N, -CF3, -alcoxi C1-3, amino, mono- o dialquilamino, -N(R)C(O)R'-, -OC(=O)-amino y -OC(=O)-mono- o dialquilamino, o alquenilo C2-6 o alquinilo C2-6, cada uno de los cuales está substituido en forma opcional con 1, 2, o 3 grupos seleccionados en forma independiente de halógeno, -OH, -SH, -C:::N, -CF3, alcoxi, amino, y mono- o dialquilamino, o arilo, heteroarilo, heterociclilo, -alquil C1-6-arilo, -alquil C1-6-heteroarilo, o -alquil C1-6-heterociclilo, donde las porciones de anillo de cada uno son substituidas en forma opcional con 1, 2, 3, o 4 grupos seleccionados en forma independiente de halógeno, -OH, -SH, -C:::N, -NR105R'105, -CO2R, -N(R)COR', o -N(R)SO2R', -C(=O)-alquilo C1-4, -SO2-amino, -SO2-mono o dialquilamino, -C(=O)-amino, -C(=O)-mono o dialquilamino, -SO2-alquilo C1-4, o alcoxi C1-6 substituido en forma opcional con 1, 2, o 3 grupos which are seleccionados en forma independiente de halógeno, o cicloalquilo C3-7 substituido en forma opcional con 1, 2, o 3 grupos seleccionados en forma independiente de halógeno, -OH, -SH, -C:::N, -CF3, alcoxi C1-3, amino, -alquilo C1-6 y mono- o dialquilamino, o alquilo C1-10 substituido en forma opcional con 1, 2, o 3 grupos seleccionados en forma independiente de halógeno, -OH, -SH, -C:::N, -CF3, -alcoxi C1-3, amino, mono- o dialquilamino y -alquilo C1-3, o alquenilo C2-10 o alquinilo C2-10 cada uno de los cuales es substituido en forma opcional con 1, 2, o 3 grupos seleccionados en forma independiente de halógeno, -OH, -SH, -C:::N, -CF3, alcoxi C1-3, amino, alquilo C1-6 y mono- o dialquilamino; y el grupo heterociclilo es además opcionalmente substituido con oxo; R y R' son en forma independiente hidrógeno, alquilo C1-10, alquilarilo C1-10 o alquilheteroarilo C1-10; en donde Rc es (I) -[-(CH2)(0-8)-(CH)(alquil1) (alquil2)], donde alquil1 y alquil2 son lineales o ramificados alcanilo C2-10, alquenilo o alquinilo, y en donde alquil1 y alquil2 se unen al mismo o diferente carbono de metileno con las valencias de metileno que permanecen abiertas ocupadas por hidrógeno, formando de dicho modo una cadena alquilo ramificada de entre 8 y 20 átomos de carbono en total; los grupos alquilo, alquil1 y alquil2 son substituidos en forma opcional con uno, dos o tres substituyentes seleccionados de un grupo compuesto por alquilo, halógeno, -OH, -SH, -C:::N, -CF3, alcoxi, -O-fenilo, -C(O)alquilo C1-3, -NR1-aR1-b donde R1-a y R1-b son -H o alquilo C1-6, -OC=ONR1-aR1-b, -S(=O)0-2, -NR1-aC=O NR1-aR1-b, -C=ONR1-aR1-b, y -S(=O)2NR1-aR1-b; (II) -(C(Rc-x)(Rc-y))(0-4)-Rc-ciclo en donde cada Rc-x y Rc-y es en forma independiente seleccionado entre H, C1 -C6 alquilo C1-6, C1 -C6 alcoxi C1-6, alquenilo C2-6 o alquinilo -(CH2)0-4-Rc-ciclo donde Rc-ciclo es tal como se lo define debajo y Rc-x y Rc-y pueden tomarse juntos con el carbono del metileno al cual se unen en forma conjunta para formar un anillo espirocíclico de 3 a 7 átomos compuestos por carbono y hasta 2 de O, S(O)(0-2) y NRa', en donde Ra' es H o alquilo C1-4; en donde el anillo espirocíclico puede fusionarse con otro anillo a fin de brindar un sistema de anillo bicíclico compuesto por carbono y hasta 2 de O, S(O)(0-2) y NRa'. y comprendiendo hasta 9 átomos en total, incluyendo, Rc-ciclo es cualquier anillo arilo, heteroarilo, o cicloalquilo o un sistema de anillos fusionado que consiste en no más de tres anillos, donde cada uno es igual o diferente y es un anillo arilo, heteroarilo, o cicloalquilo en donde Rc-ciclo es substituido en forma opcional con hasta cuatro substituyentes seleccionados en forma independiente de: (1) alquilo C1-6 substituido en forma opcional con uno dos o tres substituyentes seleccionados del grupo compuesto por alquilo C1-3, halógeno, -OH, -SH, -C:::N, -CF3, alcoxi C1-3, y -NR1-aR1-b, (2) alquenilo C2-6 o alquinilo con una o dos uniones no saturadas, substituido en forma opcional con uno, dos o tres substituyentes seleccionados del grupo compuesto por -F, -Cl, -OH, -SH, -C:::N, -CF3, alcoxi C1-3, y -NR1-aR1-b, (3) halógeno, (4) alcoxi C1-6, (5) -alcoxi C1-6 substituido en forma opcional con uno, dos, o tres de -F, (6) -NRN-6RN-7 donde RN-6 y RN-7 son iguales o diferentes y se seleccionan de un grupo compuesto por: (a) -H, (b) -alquilo C1-6 substituido en forma opcional con un substituyente seleccionado de un grupo compuesto por: (i) -OH, y (ii) -NH2, (c) -alquilo C1-6 substituido en forma opcional con uno a tres -F, -Cl, -Br, o -I, (d) -cicloalquilo C3-7, (e) -(alquil C1-2)-(cicloalquilo C3-7), (f) -(alquil C1-6)-O-(alquilo C1-3), (g) -alquenilo C2-6 con una o dos uniones dobles, (h) -alquinilo C2-6 con uno o dos uniones triples, (i) cadena -alquilo C1-6 con una unión doble y una unión triple, (j) -R1-arilo donde R1-arilo es tal como se lo describe precedentemente, y (k) -R1-heteroarilo donde R1-heteroarilo es tal como se lo describe precedentemente, (7) -OH, (8) -C:::N, (9) cicloalquilo C3-7, substituido en forma opcional con uno, dos o tres substituyentes seleccionados del grupo compuesto por -F, -Cl, -OH, -SH, -C:::N, -CF3, alcoxi C1-3, y -NR1-aR1-b, (10) -CO-(alquilo C1-4), (11) -SO2-NR1-aR1-b, (12) -CO-NR1-aR1-b, (13) -SO2-(alquilo C1-4), y cuando existe un átomo de carbono saturado en Rc-ciclo (14) oxo, (15) oxima (16) anillos quetales de 5 a 7 miembros, y (17) un anillo espirocíclico compuesto por 3 a 7 átomos que comprenden carbono y cuando el tamano del anillo es de 4-7 átomos opcionalmente hasta 2 de O, S(O)(0-2) y NRa'. (IV) -(CRc-xRc-y)0-4-heteroarilo, (III) -(CRc-xRc-y)0-4-aril-arilo (IV) -(CRc-xRc-y)0-4-aril-heteroarilo, (V) -(CRc-xRc-y)0-4-heteroaril-arilo, (VI) -(CRc-xRc-y)0-4-heteroaril-heteroarilo, (VII) -(CRc-xRc-y)0-4-aril-heterociclo, (VIII) -(CRc-xRc-y)0-4-heteroaril-heterociclo, (IX) -(CRc-xRc-y)0-4-heterociclo-arilo, (X) -(CRc-xRc-y)0-4-heterociclo-heteroarilo, (XI) -(CRc-xRc-y)0-4-heterociclo-heterociclo, (XII) -[C(Rc-1)(Rc-2)]1-3-[CO]0-1-N-(Rc-3)2 donde cada Rc-1 es igual o diferente y es seleccionado de un grupo compuesto por: H, alquilo C1-4 y alcoxi C1-4 y donde cada Rc-2 y Rc-3 es en forma independiente seleccionado de (A) -alquilo C1-6, substituido en forma opcional con uno, dos o tres substituyentes seleccionados del grupo compuesto por alquilo C1-3, -F, -Cl, -Br, -I, -OH, -SH, -C:::N, -CF3, alcoxi C1-6, -O- fenilo, y -NR1-aR1-b, (B) alquenilo C2-6 o alquinilo con una o dos uniones no saturadas, substituido en forma opcional con uno, dos o tres substituyentes seleccionados del grupo compuesto por alquilo C1-3, -F, -Cl, -Br, -I, -OH, -SH, -C:::N, -CF3, alcoxi C1-6, -O-fenilo, y -NR1-aR1-b, (C) -(CH2)1-2-S(O)0-2-(alquilo C1-6) (D) -(CH2)0-4-cicloalquilo C3-7 substituido en forma opcional con uno, dos o tres substituyentes seleccionados del grupo compuesto por alquilo C1-3, -F, -Cl, -Br, -I, -OH, -SH, -C:::N, -CF3, alcoxi C1-6, -O- fenilo, -NR1-aR1-b, (E) -(CH2)0-4-heterociclo de 5-7 miembros substituido en forma opcional con uno, dos o tres substituyentes seleccionados del grupo compuesto por alquilo C1-3, -F, -Cl, -Br, -I, -OH, -SH, -C:::N, -CF3, alcoxi C1-6, -O-fenilo, oxo, -NR1-aR1-b, (XIII) -CH(arilo)2 donde cada arilo es igual o diferente, (XIV) -CH(heteroarilo)2 donde cada heteroarilo es igual o diferente y son tal como se los define precedentemente, (XVIII) -CH(arilo)(heteroarilo), en donde RN is R'100, -(CRR')1-6R'100, -(CRR')0-6R100, -(CRR')1-6-O-R'100, -(CRR')1-6-S-R'100, -(CRR')1-6-C(=O)-R100, -(CRR')1-6SO2-R100, -(CRR')1-6-NR100-R'100 o -SO2R'100, con la condición de que cuando RN es -SO2R'100, X no es -S(=O)n- o -C(=S)-; en donde R100 y R'100 representan en forma independiente arilo, heteroarilo, -aril-W-arilo, -aril-W-heteroarilo, -aril-W-heterociclilo, -heteroaril-W-arilo, -heteroaril-W-heteroarilo, -heteroaril-W-heterociclilo, -heterociclil-W-arilo, -heterociclil-W-heteroarilo, -heterociclil-W-heterociclilo, -CH [(CH2)0-2-O-R150]-(CH2)0-2-arilo, -CH [(CH2)0-2-O-R150]-(CH2)0-2-heterociclilo o -CH[(CH2)0-2-O-R150]-(CH2)0-2-heteroarilo, donde las porciones de anillos de cada uno son substituidas en forma opcional con 1, 2, o 3 grupos seleccionados en forma independiente de -OR, -NO2, halógeno, -C:::N, -OCF3, -CF3, -(CH2)0-4-O-P(=O)(OR)(OR'), -(CH2)0-4-CO-NR105R'105, -(CH2)0-4-O-(CH2)0-4-CONR102R102', -(CH2)0-4-CO-(alquilo C1-12), -(CH2)0-4-CO-(alquenilo C2-12), -(CH2)0-4-CO-(alquinilo C2-12), -(CH2)0-4-CO-(CH2)0-4 (cicloalquilo C3-7), -(CH2)0-4-R110, -(CH2)0-4-R120, -(CH2)0-4-R130, -(CH2)0-4-CO-R110, -(CH2)0-4-CO-R120, -(CH2)0-4-CO-R130, -(CH2)0-4-CO-R140, -(CH2)0-4-CO-O-R150, -(CH2)0-4-SO2-NR105R'105, -(CH2)0-4-SO-(alquilo C1-8), -(CH2)0-4-SO2 (alquilo C1-12), -(CH2)0-4-SO2-(CH2)0-4-(cicloalquilo C3-7), -(CH2)0-4-N(R150)-CO-O-R150, -(CH2)0-4-N(R150)-CO-N(R150)2, -(CH2)0-4-N(R150)-CS-N(R150)2, -(CH2)0-4-N(R150)-CO-R105, -(CH2)0-4-NR105R'105, -(CH2)0-4-R140, -(CH2)0-4-O-CO-(alquilo), -(CH2)0-4-O-P(O)-(O-R110)2, -(CH2)0-4-O-CO-N(R150)2, -(CH2)0-4-O
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US7557137B2 (en) * | 2002-08-05 | 2009-07-07 | Bristol-Myers Squibb Company | Gamma-lactams as beta-secretase inhibitors |
BR0314071A (pt) * | 2002-09-06 | 2005-07-05 | Pharmacia & Upjohn Co Llc | Derivados de pró-droga de 1,3-diamino-2-hidroxipropano |
UY27967A1 (es) * | 2002-09-10 | 2004-05-31 | Pfizer | Acetil 2-hindroxi-1,3-diaminoalcanos |
WO2004043916A1 (en) * | 2002-11-12 | 2004-05-27 | Merck & Co., Inc. | Phenylcarboxamide beta-secretase inhibitors for the treatment of alzheimer's disease |
GB0305918D0 (en) * | 2003-03-14 | 2003-04-23 | Glaxo Group Ltd | Novel compounds |
GB0309221D0 (en) * | 2003-04-23 | 2003-06-04 | Glaxo Group Ltd | Novel compounds |
GB0317491D0 (en) * | 2003-07-25 | 2003-08-27 | Novartis Ag | Organic compounds |
KR100793095B1 (ko) * | 2003-10-01 | 2008-01-10 | 주식회사 프로메디텍 | Bace 저해효능을 가진 신규한 술폰 아미드 유도체 |
GB0323204D0 (en) * | 2003-10-03 | 2003-11-05 | Novartis Ag | Organic compounds |
US7291744B2 (en) * | 2003-11-13 | 2007-11-06 | Bristol-Myers Squibb Company | N-ureidoalkyl-amino compounds as modulators of chemokine receptor activity |
-
2003
- 2003-11-26 WO PCT/US2003/037998 patent/WO2004050609A1/en active Application Filing
- 2003-11-26 JP JP2004557383A patent/JP2006508166A/ja active Pending
- 2003-11-26 PE PE2003001203A patent/PE20040762A1/es not_active Application Discontinuation
- 2003-11-26 CA CA002507484A patent/CA2507484A1/en not_active Abandoned
- 2003-11-26 US US10/723,220 patent/US7351738B2/en not_active Expired - Fee Related
- 2003-11-26 BR BR0316629-5A patent/BR0316629A/pt not_active IP Right Cessation
- 2003-11-26 MX MXPA05005649A patent/MXPA05005649A/es active IP Right Grant
- 2003-11-26 AU AU2003293155A patent/AU2003293155A1/en not_active Abandoned
- 2003-11-26 EP EP03790144A patent/EP1565428A1/en not_active Withdrawn
- 2003-11-26 DO DO2003000765A patent/DOP2003000765A/es unknown
- 2003-11-27 PA PA20038589701A patent/PA8589701A1/es unknown
- 2003-11-27 TW TW092133639A patent/TW200505828A/zh unknown
- 2003-11-27 AR ARP030104378A patent/AR043062A1/es not_active Application Discontinuation
- 2003-11-27 UY UY28101A patent/UY28101A1/es not_active Application Discontinuation
-
2008
- 2008-04-01 US US12/060,544 patent/US20080306136A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
US20040209925A1 (en) | 2004-10-21 |
US20080306136A1 (en) | 2008-12-11 |
BR0316629A (pt) | 2005-10-11 |
CA2507484A1 (en) | 2004-06-17 |
TW200505828A (en) | 2005-02-16 |
JP2006508166A (ja) | 2006-03-09 |
WO2004050609A1 (en) | 2004-06-17 |
MXPA05005649A (es) | 2005-08-16 |
PE20040762A1 (es) | 2004-11-06 |
EP1565428A1 (en) | 2005-08-24 |
US7351738B2 (en) | 2008-04-01 |
PA8589701A1 (es) | 2004-11-26 |
AU2003293155A1 (en) | 2004-06-23 |
UY28101A1 (es) | 2004-06-30 |
WO2004050609A8 (en) | 2005-07-21 |
DOP2003000765A (es) | 2004-05-31 |
AU2003293155A8 (en) | 2004-06-23 |
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