AR043184A1 - Pirazoles y metodos de elaboracion y uso de estos - Google Patents

Pirazoles y metodos de elaboracion y uso de estos

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Publication number
AR043184A1
AR043184A1 ARP040100462A ARP040100462A AR043184A1 AR 043184 A1 AR043184 A1 AR 043184A1 AR P040100462 A ARP040100462 A AR P040100462A AR P040100462 A ARP040100462 A AR P040100462A AR 043184 A1 AR043184 A1 AR 043184A1
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Argentina
Prior art keywords
cycloalkyl
alkyl
ring
sulfyl
heteroaryl
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ARP040100462A
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English (en)
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Biogen Idec Inc
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Publication of AR043184A1 publication Critical patent/AR043184A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/14—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 three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • 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
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—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
    • C07D405/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D417/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Immunology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Communicable Diseases (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presente se basa en el descubrimiento de que los compuestos de fórmula (1) inesperadamente poseen alta afinidad para Alk5 y/o Alk4, y pueden ser útiles como antagonistas de éstos para prevenir y/o tratar numerosas enfermedades, entre ellas, trastornos fibróticos, e inhibición de los receptores de T 6 Fbeta Reivindicación 1: Un compuesto de fórmula (1) o un N-óxido, o una sal farmacéuticamente aceptable de dicho compuesto; en donde cada Ra es independientemente alquilo, alquenilo, alquinilo, alcoxi, acilo, halo, hidroxi, amino, nitro, oxo, tioxo, ciano, guanadino, amidino, carboxi, sulfo, mercapto, alquilsulfanilo, alquilsulfinilo, alquilsulfonilo, aminocarbonilo, alquilcarbonilamino, arilcarbonilamino, heteroarilcarbonilamino, alquilsulfonilamino, arilsulfonilamino, heteroarilsulfonilamino, alcoxicarbonilo, alquilcarboniloxi, urea, tiourea, sulfamoilo, sulfamida, carbamoilo, cicloalquilo, cicloalquiloxi, cicloalquilsulfanilo, cicloalquilcarbonilo, heterocicloalquilo, heterocicloalquiloxi, heterocicloalquilsulfanilo, heterocicloalquilcarbonilo, arilo, ariloxi, arilsulfanilo, aroilo, heteroarilo, heteroariloxi, heteroarilsulfanilo o heteroaroilo; R1 es un enlace, alquileno, alquenileno, alquinileno, o -(CH2)r1-O-(CH2)r2-, donde cada uno de r1 y r2 es independientemente 2 o 3; R2 es cicloalquilo, heterocicloalquilo, cicloalquenilo, heterocicloalquenilo, arilo, heteroarilo o un enlace; R3 es -C(O)-, -C(O)O-, -OC(O)-, -C(O)-N(Rb), -N(Rb)-C(O)-, -O-C(O)-N(Rb)-, -N(Rb)-C(O)-O-, -O-S(O)p-N(Rb), -N(Rb)-S(O)p-O-, -N(Rb)-C(O)-N(Rc)-, -N(Rb)-S(O)p-N(Rb)-, -C(O)-N(Rb)-S(O)p-, -S(O)p-N(Rb)-C(O)-, -S(O)p-N(Rb)-, -N(Rb)-S(O)p-, -N(Rb)-, -S(O)p-, -O-, -S-, o -(C(Rb)(Rc))q-, o un enlace; en donde cada uno de Rb y Rc es independientemente H, hidroxi, alquilo, arilo,.aralquilo, heterocicloalquilo, heteroarilo o heteroaralquilo, p es 1 o 2; y q es 1-4; R4 es H, alquilo, alquenilo, alquinilo, cicloalquilo, (cicloalquil)alquilo, heterocicloalquilo, (heterocicloalquil)alquilo, cicloalquenilo, (cicloalquenil)alquilo, heterocicloalquenilo, (heterocicloalquenil)alquilo, arilo, aralquilo, heteroarilo, o heteroaralquilo; R5 es H, alquilo no sustituido, alquilo halo-sustituido, alcoxi, alquilsulfinilo, amino, alquenilo, alquinilo, cicloalquilo, cicloalcoxi, cicloalquilsulfinilo, heterocicloalquilo, heterocicloalcoxi, heterocicloalquilsulfinilo, arilo, ariloxi, arilsulfinilo, heteroarilo, heteroariloxi o heteroarilsulfinilo; R6 es (1) un heterociclilo de 5 a 6miembros que contiene 1 a 3 heteroátomos de anillo seleccionados entre el grupo que consiste en -O-; -S-, -N= y -NRd-, donde Rd es H, alquilo, cicloalquilo, cicloalquilalquilo, arilo, aralquilo, heterocicloalquilo, heterocicloalquilalquilo, heteroarilo o heteroaralquilo; dicho heterociclilo está sustituido con Re y opcionalmente sustituido con uno o dos Rf; donde Re es oxo, tioxo, alcoxi, alquilsulfinilo, -NH2-, -NH(alquilo no sustituido), o -N(alquilo no sustituido)2 y Rf es alquilo, alquenilo, alquinilo, alcoxi, acilo, halo, hidroxi, amino, nitro, oxo, tioxo, ciano, guanadino, amidino, carboxi, sulfo, mercapto, alquilsulfanilo, alquilsulfinilo, alquilsulfonilo, aminocarbonilo, alquilcarbonilamino, alquilsulfonilamino, alcoxicarbonilo, alquilcarboniloxi, urea, tiourea, sulfamoilo, sulfamida, carbamoilo, cicloalquilo, cicloalquiloxi, cicloalquilsulfanilo, heterocicloalquilo, heterocicloalquiloxi, heterocicloalquilsulfanilo, arilo, ariloxi, arilsulfanilo, aroilo, heteroarilo, heteroariloxi, heteroarilsulfanilo, o heteroaroilo; o (2) un anillo heteroarilo fusionado seleccionado entre el grupo que consiste en los restos de fórmulas (2) donde el anillo A es un anillo aromático que contiene 0 a 4 heteroátomos de anillo, y e anillo B es un anillo aromático o no aromático de 5 a 7 miembros, que contiene 0 a 4 heteroátomos de anillo, siempre que por lo menos uno de anillo A y anillo B contenga uno o más heteroátomos de anillo; el anillo A´ es un anillo aromático que contiene 0 a 4 heteroátomos de anillo, y el anillo B´ es un anillo saturado o insaturado, de 5 a 7 miembros, que contiene 0 a 4 heteroátomos de anillo, siempre que por lo menos uno de anillo A´ y anillo B´ contenga uno o más heteroátomos de anillo; cada heteroátomo de anillo es -O-, -S-, -N=, o NRg-; cada X1 es en forma independiente N o C; cada X2 es en forma independiente -O-; -S-; -N=, -NRg-, o -CHRh-; donde Rg es H, alquilo, cicloalquilo, cicloalquilalquilo, arilo, aralquilo, heterocicloalquilo, heterocicloalquilalquilo, heteroarilo o heteroaralquilo; cada uno de Rh y Ri es independientemente alquilo, alquenilo, alquinilo, alcoxi, acilo, halo, hidroxi, amino, nitro, oxo, tioxo, ciano, guanadino, amidino, carboxi, sulfo, mercapto, alquilsulfanilo, alquilsulfinilo, alquilsulfonilo, aminocarbonilo, alquilcarbonilamino, arilcarbonilamino, heteroarilcarbonilamino, alquilsulfonilamino, arilsulfonilamino, heteroarilsulfonilamino, alcoxicarbonilo, alquilcarboniloxi, urea, tiourea, sulfamoilo, sulfamida, carbamoilo, cicloalquilo, cicloalquiloxi, cicloalquilsulfanilo, cicloalquilcarbonilo, heterocicloalquilo, heterocicloalquiloxi, heterocicloalquilsulfanilo, heterocicloalquilcarbonilo, arilo, ariloxi, arilsulfanilo, aroilo, heteroarilo, heteroariloxi, heteroarilsulfanilo, o heteroaroilo; n es 0 a 2; y m es 0 a 3; siempre que cuando m es 2, dos grupos Ra adyacentes pueden unirse para formar una porción cíclica opcionalmente sustituida, de 4 a 8 miembros; siempre que si R6 es 2-naftiridinilo, 4-quinolinilo, imidazo[1,2-a]piridilo, o benzimidazolilo, entonces -R1-R2-R3-R4 no es H, alquilo no sustituido, -CH2-C(O)-N(H)-alquilo, -CH2-C(O)-N(alquilo)2 o bencilo.
ARP040100462A 2003-02-12 2004-02-13 Pirazoles y metodos de elaboracion y uso de estos AR043184A1 (es)

Applications Claiming Priority (1)

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US44677703P 2003-02-12 2003-02-12

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AR043184A1 true AR043184A1 (es) 2005-07-20

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Country Link
US (1) US20060264440A1 (es)
EP (1) EP1596656A4 (es)
JP (1) JP2006517592A (es)
KR (1) KR20050101547A (es)
CN (1) CN1770980A (es)
AR (1) AR043184A1 (es)
AU (1) AU2004210855A1 (es)
BR (1) BRPI0407454A (es)
CA (1) CA2514382A1 (es)
CL (1) CL2004000234A1 (es)
EA (1) EA010161B1 (es)
GE (1) GEP20084391B (es)
IS (1) IS7966A (es)
MX (1) MXPA05008524A (es)
NO (1) NO20054200L (es)
NZ (1) NZ542289A (es)
PL (1) PL378072A1 (es)
RS (1) RS20050616A (es)
UA (1) UA82223C2 (es)
WO (1) WO2004072033A2 (es)
ZA (1) ZA200506408B (es)

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