AR052900A1 - DERIVATIVES OF TIAZOL, A METHOD FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND THEIR USE IN THE PREPARATION OF MEDICINES FOR THE TREATMENT OF DISEASES MEDIATED BY ECE-1 - Google Patents

DERIVATIVES OF TIAZOL, A METHOD FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND THEIR USE IN THE PREPARATION OF MEDICINES FOR THE TREATMENT OF DISEASES MEDIATED BY ECE-1

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AR052900A1
AR052900A1 ARP060100432A ARP060100432A AR052900A1 AR 052900 A1 AR052900 A1 AR 052900A1 AR P060100432 A ARP060100432 A AR P060100432A AR P060100432 A ARP060100432 A AR P060100432A AR 052900 A1 AR052900 A1 AR 052900A1
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Argentina
Prior art keywords
4alkyl
alkylene
optionally substituted
halogen
alkyl
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ARP060100432A
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Spanish (es)
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Andrew Baxter
Sarah King
Austen Pimm
Chris Luckhurst
Mark Furber
James Reuberson
Millichip Ian
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Astrazeneca Ab
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Publication of AR052900A1 publication Critical patent/AR052900A1/en

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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • 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
    • C07D277/32—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 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
    • C07D277/38—Nitrogen atoms
    • C07D277/44—Acylated amino or imino radicals
    • C07D277/48—Acylated amino or imino radicals by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof, e.g. carbonylguanidines
    • 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
    • C07D277/32—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 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
    • C07D277/54—Nitrogen and either oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

Un proceso para su preparacion; composiciones farmacéuticas que los contienen; y su uso en terapia de la obstruccion pulmonar cronica. Reivindicacion 1: Un compuesto caracterizado porque responde a la formula (1), donde: R1 es arilo opcionalmente sustituido o heteroarilo opcionalmente sustituido; R2 es ciano, CF3, halogeno o XR7; R3 es arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido o cicloalquilo C3-7 [opcionalmente sustituido con halogeno o alquilo C1-4]; A es NR4 o CR5R6; R4, R5 y R6 representan en forma independiente entre sí hidrogeno o alquilo C1-4 o cicloalquilo C3-7 [opcionalmente sustituido con halogeno o alquilo C1-4]; X es un enlace simple, alquileno C1-6 [opcionalmente sustituido con halogeno], alquenileno C2-6 [opcionalmente sustituido con halogeno], alquinileno C2-6 [opcionalmente sustituido con halogeno], S(O)n, NR8C(O), C(O)NR9, NR10, C(O), OC(O), C(O)O, OalquilenoC1-4, S(O) nalquilenoC1-4, NR11C(O)alquilenoC1-4, C(O)NR12alquilenoC1-4, NR13alquilenoC1-4, C(O)alquilenoC1-4, OC(O)alquilenoC1-4, C(O) OalquilenoC1-4, alquilenoC1-4O, alquilenoC1-4S(O)n, alquilenoC1-4NR14C(O), alquilenoC1-4C(O)NR15, alquilenoC1-4NR16, alquilenoC1-4C(O), alquilenoC1-4OC(O), alquilenoC1-4OalquilenoC1-4, alquilenoC1-4S(O)nalquilenoC1-4, alquilenoC1-4NR17C(O) alquilenoC1-4, alquilenoC1-4C(O)NR18alquilenoC1-4, alquilenoC1-4NR19alquilenoC1-4, alquilenoC1-4C(O)alquilenoC1-4, alquilenoC1-4OC(O)alquilenoC1-4 o alquilenoC1-4C(O)OalquilenoC1-4; R7 es hidrogeno, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, cicloalquilo C3-7 [opcionalmente sustituido con halogeno o alquilo C1-4], un anillo heterociclilo alifálico de entre 4 y 8 miembros [opcionalmente sustituido con halogeno o alquilo C1-4], OR20, NR21R22, C(O)R23, CO2R24, OC(O)R25, C(O)NR26R27, S(O)nR28, SO2NR29R30, NR32C(O)R33, NR34C(O)OR35, fenoxi [opcionalmente sustituido con halogeno, ciano CF3 o alquilo C1-4] o heteroariloxi [opcionalmente sustituido con halogeno, ciano, CF3 o alquilo C1-4]; R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, R25, R26, R27, R28, R29, R30, R32, R33, R34 y R35 son, en forma independiente, hidrogeno alquilo C1-6 [opcionalmente sustituido con halogeno]; las porciones arilo y heteroarilo están opcionalmente sustituidas en forma independiente con uno o más de halogeno, ciano, nitro, OC(O)NR36R37, NR38R39, NR40C(O)R41, NR42C(O)NR43R44, S(O)2NR45R46, NR47S(O)2R48, C(O)NR49R50, CO2R51, NR52CO2R53, S(O)nR54, OS(O)2R55, alquilo C1-6 [opcionalmente monosustituido con S(O)2R56 , C(O) NR57R58 o NR31R62], C(O)R59, NR60C(O)R61, alquenileno C2-6 [opcionalmente sustituido con fenilo o heteroarilo], alquinileno C2-6 [opcionalmente sustituido con fenilo o heteroarilo], cicloalquilo C3-7, haloalquilo C1-6, alcoxiC1-6alquilenoC1-6, alcoxi C1-6, haloalcoxi C1-6, fenilo, fenil-alquilenoC1-4, fenoxi, feniltio, fenilS(O), fenilS(O)2, fenil-alcoxiC1-4, heteroarilo, heteroaril- alquiloC1-4, heteroariloxi, heteroaril-alcoxiC1-4 o un anillo heterocíclico alifático de entre 4 y 8 miembros [opcionalmente sustituido con halogeno o alquilo C1-4]; donde cualquiera de las porciones fenilo y heteroarilo inmediatamente precedentes están opcionalmente sustituidas con halogeno, nitro, NH2, NHalquiloC1-4, N(alquil C1-4)2, SalquiloC1-4, S(O)alquiloC1-4, S(O)2alquiloC1-4, S(O)2NH2, S(O)2NHalquiloC1-4, S(O)2N(alquilo C1-4)2, ciano, alquilo C1-4, alcoxi C1-4, C(O)NH2, C(O)NHalquiloC1-4, C(O)N(alquil C1-4)2, CO2H, CO2alquiloC1-4, NHC(O)alquiloC1-4, NHS(O)2alquiloC1-4, C(O)alquiloC1-4, CF3 o OCF3; R31, R36, R37, R38, R39, R40, R41, R42, R44, R45, R46, R47, R49, R50, R51, R52, R53, R57, R58, R59, R60, R61 y R62 son, en forma independiente, hidrogeno alquilo C1-6 [opcionalmente sustituido con halogeno, cicloalquilo C3-6 o fenilo {opcionalmente sustituido con halogeno o alquilo C1-4}]; CH2alqueniloC2-6, fenilo [a su vez opcionalmente sustituido con halogeno, nitro, NH2, NHalquiloC1-4, N(alquil C1-4)2, SalquiloC1-4, S(O)alquiloC1-4, S(O)2alquiloC1-4, S(O)2NH2, S(O) 2NHalquiloC1-4, S(O)2N(alquil C1-4)2, ciano, alquilo C1-4, alcoxi C1-4, C(O)NH2, C(O)NHalquiloC1-4, C(O)N(alquil C1-4)2, CO2H, CO2alquiloC1-4, NHC(O)alquiloC1-4, NHS(O)2alquiloC1-4, C(O)alquiloC1-4, CF3 o OCF3] o heteroarilo [a su vez opcionalmente sustituido con halogeno, nitro, NH2, NHalquiloC1-4, N(alquil C1-4)2, SalquiloC1-4, S(O)alquiloC1-4, S(O)2alquiloC1-4, S(O)2NH2, S(O) 2NHalquiloC1-4, S(O)2N(alquil C1-4)2, ciano, alquilo C1-4, alcoxi C1-4, C(O)NH2, C(O)NHalquiloC1-4, C(O)N(alquil C1-4)2, CO2H, CO2alquiloC1-4, NHC(O)alquiloC1-4, NHS(O)2alquiloC1-4, C(O)alquiloC1-4, CF3 o OCF3]; R48, R54, R55 y R56 son, en forma independiente, alquilo C1-6 [ opcionalmente sustituido con halogeno, cicloalquilo C3-6 o fenilo {opcionalmente sustituido con halogeno o alquilo C1-4}], CH2alqueniloC2-6, fenilo [a su vez opcionalmente sustituido con halogeno, nitro, NH2, NHalquiloC1-4, N(alquil C1-4)2, Salquilo C1-4, S(O)alquiloC1-4, S(O)2alquiloC1-4, S(O)2NH2, S(O)2NHalquiloC1-4, S(O)2N(alquil C1-4)2, ciano, alquilo C1-4, alcoxi C1-4, C(O)NH2, C(O)NHalquiloC1-4, C(O)N(alquil C1-4)2, CO2H, CO2alquiloC1-4, NHC(O)alquiloC1-4, NHS(O)2alquiloC1-4, C(O)alquiloC1-4, CF3 o OCF3] o heteroarilo [a su vez opcionalmente sustituido con halogeno, nitro, NH2, NHalquiloC1-4, N(alquil C1-4)2, SalquiloC1-4, S(O)alquiloC1-4, S(O)2alquiloC1-4, S(O)2NH2, S(O)2NHalquiloC1-4, S(O)2N(alquil C1-4)2, ciano, alquilo C1-4, alcoxi C1-4, C(O)NH2, C(O)NHalquiloC1-4, C(O)N(alquil C1-4)2, CO2H, CO2alquiloC1-4, NHC(O)alquiloC1-4, NHS(O)2alquiloC1-4, C(O)alquiloC1-4, CF3 o OCF3]; y n es 0,1 o 2; o una sal aceptable para uso farmacéutico del mismo. Reivindicacion 12: Un proceso para la preparacion de un compuesto de formula (1) de acuerdo con la reivindicacion 1, o una sal aceptable para uso farmacéutico del mismo, caracterizado porque comprende: a) cuando A es CRR5R6 acoplar un compuesto de formula (2), con un compuesto de formula (3); b) cuando A es NH hacer reaccionar un compuesto de formula (4), con un compuesto de formula (3) segun se define en a) en presencia de una azida de fosforilo; o c) cuando A es NH hacer reaccionar un compuesto de formula (5), con un compuesto de formula (3) segun se define en a); o d) cuando A es NR4 hacer reaccionar un compuesto de formula (6), con un compuesto de formula (7), y opcionalmente luego de a), b), c) o d) llevar a cabo uno o más de los siguientes pasos: convertir el compuesto a otro compuesto de la presente; o formar una sal aceptable para uso farmacéutico del compuesto.A process for its preparation; pharmaceutical compositions containing them; and its use in chronic pulmonary obstruction therapy. Claim 1: A compound characterized in that it responds to formula (1), wherein: R1 is optionally substituted aryl or optionally substituted heteroaryl; R2 is cyano, CF3, halogen or XR7; R3 is optionally substituted aryl, optionally substituted heteroaryl or C3-7 cycloalkyl [optionally substituted with halogen or C1-4 alkyl]; A is NR4 or CR5R6; R4, R5 and R6 independently represent each other hydrogen or C1-4 alkyl or C3-7 cycloalkyl [optionally substituted with halogen or C1-4 alkyl]; X is a single bond, C1-6 alkylene [optionally substituted with halogen], C2-6 alkenylene [optionally substituted with halogen], C2-6 alkynylene [optionally substituted with halogen], S (O) n, NR8C (O), C (O) NR9, NR10, C (O), OC (O), C (O) O, C1-4alkylene, S1 (O) C1-4 alkylene, NR11C (O) C1-4 alkylene, C (O) NR12 alkyleneC1- 4, NR13 C1-4 alkylene, C (O) C1-4 alkylene, OC (O) C1-4 alkylene, C1 (O) C1-4 alkylene, C1-4 alkylene, C1-4S alkylene (O) n, C1-4NR14C alkylene (O), C1 alkylene -4C (O) NR15, C1-4 alkylene16, C1-4C alkylene (O), C1-4OC alkylene (O), C1-4 alkyleneC1-4 alkylene, C1-4S alkylene (O) C1-4 alkylene, C1-4 alkylene (O) C1-4 alkylene , C1-4C alkylene (O) NR18C1-4 alkylene, C1-4 alkyleneC1-4 alkylene, C1-4C alkylene (O) C1-4 alkylene, C1-4OC alkylene (O) C1-4 alkylene or C1-4C alkylene (O) C1-4 alkylene; R7 is hydrogen, optionally substituted aryl, optionally substituted heteroaryl, C3-7 cycloalkyl [optionally substituted with halogen or C1-4 alkyl], an aliphatic heterocyclyl ring of 4 to 8 members [optionally substituted with halogen or C1-4 alkyl], OR20, NR21R22, C (O) R23, CO2R24, OC (O) R25, C (O) NR26R27, S (O) nR28, SO2NR29R30, NR32C (O) R33, NR34C (O) OR35, phenoxy [optionally substituted with halogen , cyano CF3 or C1-4 alkyl] or heteroaryloxy [optionally substituted with halogen, cyano, CF3 or C1-4 alkyl]; R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, R25, R26, R27, R28, R29, R30, R32, R33, R34 and R35 are independently hydrogen C1-6 alkyl [optionally substituted with halogen]; the aryl and heteroaryl portions are optionally independently substituted with one or more of halogen, cyano, nitro, OC (O) NR36R37, NR38R39, NR40C (O) R41, NR42C (O) NR43R44, S (O) 2NR45R46, NR47S ( O) 2R48, C (O) NR49R50, CO2R51, NR52CO2R53, S (O) nR54, OS (O) 2R55, C1-6 alkyl [optionally monosubstituted with S (O) 2R56, C (O) NR57R58 or NR31R62], C (O) R59, NR60C (O) R61, C2-6 alkenylene [optionally substituted with phenyl or heteroaryl], C2-6 alkynylene [optionally substituted with phenyl or heteroaryl], C3-7 cycloalkyl, C1-6 haloalkyl, C1-6 alkoxyC1 -6, C1-6 alkoxy, C1-6 haloalkoxy, phenyl, phenylC1-4 alkylene, phenoxy, phenylthio, phenylS (O), phenylS (O) 2, phenylC1-4alkoxy, heteroaryl, heteroarylC1-4alkyl, heteroaryloxy, heteroarylC 1-4 alkoxy or a 4 to 8 membered aliphatic heterocyclic ring [optionally substituted with halogen or C 1-4 alkyl]; wherein any of the immediately preceding phenyl and heteroaryl moieties are optionally substituted with halogen, nitro, NH2, NHC1-4alkyl, N (C1-4alkyl) 2, C1-4alkyl, S (O) C1-4alkyl, S (O) 2C1alkyl -4, S (O) 2NH2, S (O) 2NH1-4alkyl, S (O) 2N (C1-4alkyl) 2, cyano, C1-4alkyl, C1-4alkoxy, C (O) NH2, C ( O) NH1-4alkyl, C (O) N (C1-4alkyl) 2, CO2H, CO2C1-4alkyl, NHC (O) C1-4alkyl, NHS (O) 2C1-4alkyl, C (O) C1-4alkyl, CF3 or OCF3; R31, R36, R37, R38, R39, R40, R41, R42, R44, R45, R46, R47, R49, R50, R51, R52, R53, R57, R58, R59, R60, R61 and R62 are, independently , hydrogen C1-6 alkyl [optionally substituted with halogen, C3-6 cycloalkyl or phenyl {optionally substituted with halogen or C1-4 alkyl]]; CH2-C2-6 alkenyl, phenyl [in turn optionally substituted with halogen, nitro, NH2, NH1-4alkyl, N (C1-4alkyl) 2, C1-4alkyl, S (O) C1-4alkyl, S (O) 2C1-4alkyl , S (O) 2NH2, S (O) 2NH1-4alkyl, S (O) 2N (C1-4alkyl) 2, cyano, C1-4alkyl, C1-4alkoxy, C (O) NH2, C (O) NH1-4alkyl, C (O) N (C1-4alkyl) 2, CO2H, CO2C1-4alkyl, NHC (O) C1-4alkyl, NHS (O) 2C1-4alkyl, C (O) C1-4alkyl, CF3 or OCF3 ] or heteroaryl [in turn optionally substituted with halogen, nitro, NH2, NH1-4alkyl, N (C1-4alkyl) 2, C1-4alkyl, S (O) C1-4alkyl, S (O) 2C1-4alkyl, S (O) 2NH2, S (O) 2NH1-4alkyl, S (O) 2N (C1-4alkyl) 2, cyano, C1-4alkyl, C1-4alkoxy, C (O) NH2, C (O) NHalkylC1- 4, C (O) N (C1-4alkyl) 2, CO2H, CO2C1-4alkyl, NHC (O) C1-4alkyl, NHS (O) 2C1-4alkyl, C (O) C1-4alkyl, CF3 or OCF3]; R48, R54, R55 and R56 are, independently, C1-6 alkyl [optionally substituted with halogen, C3-6 cycloalkyl or phenyl {optionally substituted with halogen or C1-4 alkyl}], CH2alkenylC2-6, phenyl [a optionally substituted with halogen, nitro, NH2, NH1-4alkyl, N (C1-4alkyl) 2, C1-4alkyl, S (O) C1-4alkyl, S (O) 2C1-4alkyl, S (O) 2NH2, S (O) 2N C1-4alkyl, S (O) 2N (C1-4alkyl) 2, cyano, C1-4alkyl, C1-4alkoxy, C (O) NH2, C (O) NH1-4alkyl, C (O ) N (C1-4 alkyl) 2, CO2H, CO2 C1-4 alkyl, NHC (O) C1-4 alkyl, NHS (O) 2 C1-4 alkyl, C (O) C1-4 alkyl, CF3 or OCF3] or heteroaryl [in turn] optionally substituted with halogen, nitro, NH2, NH1-4alkyl, N (C1-4alkyl) 2, C1-4alkyl, S (O) C1-4alkyl, S (O) 2C1-4alkyl, S (O) 2NH2, S ( O) 2N C1-4alkyl, S (O) 2N (C1-4alkyl) 2, cyano, C1-4alkyl, C1-4alkoxy, C (O) NH2, C (O) NHC1-4alkyl, C (O) N (C1-4 alkyl) 2, CO2H, CO2 C1-4alkyl, NHC (O) C1-4alkyl, NHS (O) 2C1-4alkyl, C (O) C1-4alkyl, CF3 or OCF3]; and n is 0.1 or 2; or a salt acceptable for pharmaceutical use thereof. Claim 12: A process for the preparation of a compound of formula (1) according to claim 1, or a salt acceptable for pharmaceutical use thereof, characterized in that it comprises: a) when A is CRR5R6 coupling a compound of formula (2 ), with a compound of formula (3); b) when A is NH reacting a compound of formula (4), with a compound of formula (3) as defined in a) in the presence of a phosphoryl azide; or c) when A is NH reacting a compound of formula (5), with a compound of formula (3) as defined in a); od) when A is NR4 to react a compound of formula (6), with a compound of formula (7), and optionally after a), b), c) or d) carry out one or more of the following steps: convert the compound to another compound of the present; or form an acceptable salt for pharmaceutical use of the compound.

ARP060100432A 2005-02-11 2006-02-07 DERIVATIVES OF TIAZOL, A METHOD FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND THEIR USE IN THE PREPARATION OF MEDICINES FOR THE TREATMENT OF DISEASES MEDIATED BY ECE-1 AR052900A1 (en)

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