AR036133A1 - Pirazinas, formulacion farmaceutica, usos de estos compuestos para la manufactura de medicamentos, procesos para la preparacion de estos compuestos, y compuestos intermediarios - Google Patents

Pirazinas, formulacion farmaceutica, usos de estos compuestos para la manufactura de medicamentos, procesos para la preparacion de estos compuestos, y compuestos intermediarios

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Publication number
AR036133A1
AR036133A1 ARP020102534A ARP020102534A AR036133A1 AR 036133 A1 AR036133 A1 AR 036133A1 AR P020102534 A ARP020102534 A AR P020102534A AR P020102534 A ARP020102534 A AR P020102534A AR 036133 A1 AR036133 A1 AR 036133A1
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Argentina
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alkyl
nr4r5
alkynyl
cycloalkyl
alkenyl
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ARP020102534A
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English (en)
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Astrazeneca Ab
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Publication of AR036133A1 publication Critical patent/AR036133A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—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
    • 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
    • C07D213/60—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
    • C07D213/73—Unsubstituted amino or imino radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/16—Masculine contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18—Feminine contraceptives
    • 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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D213/00—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
    • 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
    • C07D213/60—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
    • 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
    • C07D401/12—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
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Gynecology & Obstetrics (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Pirazinas que tienen la fórmula (1) en la cual: Y es CONR3, NR3CO, SO2NR3, NR3SO2, CH2NR3, NR3CH2, NR3CONR3, alquileno C1-6, CH2CO, COCH2, CH=CH, OCH2 o CH2O; X es CH ó N; P es fenilo o un anillo heteroaromático de 5 o 6 miembros que contiene uno o más heteroátomos seleccionados entre N, O ó S y dicho anillo fenilo o anillo heteroaromático de 5 o 6 miembros puede estar fusionado optativamente con un anillo saturado, parcialmente saturado o insaturado de 5 o 6 miembros que contiene átomos seleccionados entre C, N, O ó S; Q es fenilo o un anillo heteroaromático de 5 o 6 miembros que contiene átomos seleccionados entre N, O ó S en donde al menos un átomo es nitrógeno; R1 es halo, nitro, alquilo C0-6CN, alquilo C0-6OR8, fluormetilo, difluormetilo, trifluormetilo, alquilo C0-6 NR8R9, alquilo C0-6 CONR8R9,alquilo C0-6 NR8(CO)R9, NR8(CO)OR9, alquilo C0-6 O(CO)R8, alquilo C0-6 SO2R8, alquilo C0-6 SOR8, alquilo C0-6COR8, alquilo C0-6O(CO)OR8, alquilo C1-6 CO2R8, O alquilo C0-6 SO2R8, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquil C0-6 cicloalquilo C3-6, alquil C0-6 arilo o alquil C0-6 heteroarilo, en donde cualquier alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquil C0-6 cicloalquilo C3-6, alquil C0-6 arilo o alquil C0-6 heteroarilo puede estar optativamente sustituido con uno o más A; R2 es halo, nitro, CHO, alquil C0-6 CN, O alquil C1-6 CN, alquil C0-6 OR4, O alquil C1-6 OR4, fluormetilo, difluormetilo, trifluormetilo, fluormetoxi, difluormetoxi, trifluormetoxi, alquil C0-6 NR4R5, O alquil C1-6 NR4R5, O alquil C1-6 O alquil C1-6 NR4R5, NR4OR5, alquil C0-6 CO2R4, O alquil C1-6 CO2R4, alquil C0-6 CONR4R5, O alquil C1-6 CONR4R5, O alquil C1-6 NR4(CO)R5, alquil C0-6 NR4(CO)R5, O(CO)NR4R5, NR4(CO)OR5, NR4(CO)NR4R5, O(CO)OR4, O(CO)R4, O alquil C1-6 COR4, NR4(CO)(CO)R4, NR4(CO)/CO)NR4R5, SR4, alquil C0-6 (SO2)NR4R5, O alquil C1-6 NR4(SO2)R5, O alquil C0-6 (SO2)NR4R5, alquil C0-6 (SO)NR4R5, O alquil C1-6 (SO)NR4R5, SO3R4, alquil C1-6 NR4(SO2)NR4R5, alquil C0-6NR4(SO)R5, O alquil C0-6 NR4(SO)R5, O alquil C0-6 SO2R4, alquil C0-6 SO2R4, alquil C0-6 SOR4, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquil C0-6 cicloalquilo C3-6, alquil C0-6 arilo o alquil C0-6 heteroarilo, en donde cualquier alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquil C0-6 cicloalquilo C3-6, alquil C0-6 arilo o alquil C0-6 heteroarilo puede estar optativamente sustituido con uno o más A; m es 0, 1, 2, 3 ó 4; n es 0, 1, 3, 4 ó 5; R3 es hidrógeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquil C0-6 cicloalquilo C3-6, alquil C1-6 NR6R7 ó alquil C1-6 CONR6R7; R4 y R5 se seleccionan independientemente entre hidrógeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquil C0-6 cicloalquilo C3-6, alquil C0-6 arilo, alquil C0-6 heteroarilo y alquil C1-6 NR6R7; R4 y R5 pueden formar en conjunto un anillo heterocíclico de 5 o 6 miembros que contiene uno o más heteroátomos seleccionados entre N, O ó S, en donde dicho anillo heterocíclico puede estar sustituido optativamente con A; R6 y R7 se seleccionan independientemente entre hidrógeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6 y alquil C0-6 cicloalquilo C3-6; R6 y R7 pueden formar en conjunto un anillo heterocíclico de 5 o 6 miembros que contiene uno o más heteroátomos seleccionados entre N, O ó S, en donde dicho anillo heterocíclico puede estar sustituido optativamente con A; R8 y R9 se seleccionan independientemente entre hidrógeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquil C0-6 arilo, alquil C0-6 heteroarilo y alquil C0-6 cicloalquilo C3-6; R8 y R9 pueden formar en conjunto un anillo heterocíclico de 5 o 6 miembros que contiene uno o más heteroátomos seleccionados entre N, O ó S, en donde dicho anillo heterocíclico puede estar sustituido optativamente con A; R14 es hidrógeno, metilo, flúor, cloro o bromo; en donde cualquier alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquil C0-6 cicloalquilo C3-6, alquil C0-6 arilo, alquil C0-6 heteroarilo definido bajo R3 a R9 puede estar sustituido con uno o más A; A es halo nitro, CHO, CN, OR4, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquil C0-6 cicloalquilo C3-6; fluormetilo, difluormetilo, trifluormetilo, fluormetoxi, difluormetoxi, trifluormetoxi, alquil C0-6 NR4R5, O alquil C1-6 NR4R5, NR4R5, CO2R8, CONR4R5, NR4(CO)R4, O(CO)R4, COR4, SR4, (SO2)NR4R5, (SO)NR4R5, SO3R4, SO2R4 ó SOR4, como una base libre o su sal farmacéuticamente aceptable, con la condición de que Y no sea metileno o etileno cuando ambos P y Q son fenilo e Y no sea metileno cuando P es metoxipirazina y Q es fenilo; formulación farmacéutica, usos de estos compuestos para la manufactura de medicamentos, procesos para la preparación de estos compuestos, y compuestos intermediarios. Los compuestos se incluyen en medicamentos que resultan útiles en el tratamiento de enfermedades neurodegenerativas y esquizofrenia, diabetes y neuropatía diabética y pérdida del cabello.
ARP020102534A 2001-07-05 2002-07-05 Pirazinas, formulacion farmaceutica, usos de estos compuestos para la manufactura de medicamentos, procesos para la preparacion de estos compuestos, y compuestos intermediarios AR036133A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
SE0102438A SE0102438D0 (sv) 2001-07-05 2001-07-05 New compounds

Publications (1)

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AR036133A1 true AR036133A1 (es) 2004-08-11

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ARP020102534A AR036133A1 (es) 2001-07-05 2002-07-05 Pirazinas, formulacion farmaceutica, usos de estos compuestos para la manufactura de medicamentos, procesos para la preparacion de estos compuestos, y compuestos intermediarios

Country Status (7)

Country Link
US (1) US20040186113A1 (es)
EP (1) EP1406877A1 (es)
JP (1) JP2004536110A (es)
AR (1) AR036133A1 (es)
SE (1) SE0102438D0 (es)
UY (1) UY27368A1 (es)
WO (1) WO2003004475A1 (es)

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KR102056586B1 (ko) 2011-09-30 2019-12-18 버텍스 파마슈티칼스 인코포레이티드 Ａｔｒ 억제제를 이용한 췌장암 및 비소세포 폐암의 치료
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