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AR063100A1 - Derivados de pirazol como moduladores del receptor 5-ht2a de serotonina utiles para el tratamiento de los trastornos relacionados con dicho receptor - Google Patents

Derivados de pirazol como moduladores del receptor 5-ht2a de serotonina utiles para el tratamiento de los trastornos relacionados con dicho receptor

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Publication number
AR063100A1
AR063100A1 ARP070104362A ARP070104362A AR063100A1 AR 063100 A1 AR063100 A1 AR 063100A1 AR P070104362 A ARP070104362 A AR P070104362A AR P070104362 A ARP070104362 A AR P070104362A AR 063100 A1 AR063100 A1 AR 063100A1
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AR
Argentina
Prior art keywords
alkoxy
alkyl
group
haloalkyl
halogen
Prior art date
Application number
ARP070104362A
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English (en)
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Arena Pharm Inc
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Application filed by Arena Pharm Inc filed Critical Arena Pharm Inc
Publication of AR063100A1 publication Critical patent/AR063100A1/es

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    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole 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
    • C07D231/16—Halogen atoms or nitro radicals
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    • 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
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    • 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
    • A61P9/12—Antihypertensives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • 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
    • C07D405/02—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
    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Anesthesiology (AREA)
  • Communicable Diseases (AREA)
  • Psychology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Los compuestos y sus composiciones farmacéuticas están dirigidos a métodos utiles en el tratamiento del insomnio y los trastornos del sueno relacionados, la agregacion plaquetaria, la coronariopatía, el infarto miocárdico, el accidente isquémico transitorio, la angina, el accidente cerebrovascular, la fibrilacion auricular, reducir el riesgo de formacion de coágulos sanguíneos, el asma o sus síntomas, la agitacion o sus síntomas, los trastornos de conducta, la psicosis inducida por fármacos, la psicosis excitativa, el síndrome de Gilles de la Tourette, el trastorno maníaco, la psicosis orgánica o sin especificar (NOS, no especificada de otra manera por sus siglas en inglés), los trastornos psicoticos, la psicosis, la esquizofrenia aguda, la esquizofrenia cronica, la esquizofrenia sin especificar y los trastornos relacionados, los trastornos relacionados con la diabetes, la leticoencefalopatía multifocal progresiva y similares. Reivindicacion 1: Un compuesto de formula (1) o una sal, solvato o hidrato fárrnacéuticamente aceptable de éste; donde: R1 y R2 se selecciona cada uno independientemente del grupo que consiste en H, C1-6 alquilo, C1-6 alquilarilo, arilo, C3-7 cicloalquilo, C1-6 haloalquilo, halogeno, heteroarilo y nitro; y donde C1-6 alquilo, arilo y heteroarilo están opcionalmente sustituidos con 1, 2, 3, 4 o 5 sustituyentes seleccionados independientemente del grupo que consiste en C1-6 acilo, C1-6 aciloxi, C2-6 alquenilo, C1-6 alcoxi, C1-6 alquilo, C1-6 alquilcarboxamida, C1-6 alquilsulfonamida, C1-6 alquilsulfinilo, C1-6 alquilsulfonilo, C1-6 alquiltio, C1-6 alquilureilo, C1-6 alquilamino, C2-6 alquinilo, amino, carbo-C1-6-alcoxi, carboxamida, carboxi, ciano, C3-7 cicloalquilo, C2-6 dialquilamino, C2-6 dialquilcarboxamida, C2-6 dialquilsulfonamida, C1-6 haloalcoxi, C1-6 haloalquilo, C1-6 haloalquilsulfinilo, C1-6, haloalquilsulfonilo, C1-6 haloalquiltio, halogeno, hidroxilo, nitro, sulfonamida y tiol; o R1 y R2 junto con los átomos de carbono a los que están unidos forman un grupo C3-7 carbociclilo o un C3-7 heterociclilo cada uno opcionalmente sustituido con 1, 2, 3. 4 o 5 sustituyentes seleccionados independientemente del grupo que consiste en C1-6 acilo, C1-6 aciloxi, C2-6 alquenilo, C1-6 alcoxi, C1-6 alquilo, C1-6 a!quilcarboxamida, C1-6 alquilsulfonamida, C1-6 alquilsulfinilo, C1-6 alquilsulfonilo, C1-6 alquiltio. C1-5 alquilureilo, C1-6 alquilamino, C1-6 alquinilo, amino, carbo-C1-6- alcoxi, carboxamida, carboxi, ciano, C3-7 cicloalquilo, C2-6 dialquilamino, C2-6 dialquilcarboxamida, C2-6 dialquilsulfonamida, C1-6 haloalcoxi, C1-6 haloalquilo, C1-6 haloalquilsulfinilo, C1-6 haloalquilsulfonilo, C1-6 haloalquiltio, halogeno, hidroxilo, nitro, oxo, sulfonamida y tiol; R3 se selecciona del grupo que consiste en H, C1-6 alquilo y arilo; y donde arilo está opcionalmente sustituido con 1, 2, 3, 4 o 5 sustituyentes seleccionados independientemente del grupo que consiste en C1- 6 acilo, C1-6 aciloxi, C2-6 alquenilo, C1-6 alcoxi, C1-6 alquilo, C1-6 alquilcarboxamida, C1-6 alquilsulfonamida, C1-6 alquilsulfinilo, C1-6 alquilsulfnil, C1-6 alquiltio, C1-6 a!quilureilo, C1-6 alquilamino, C2-6 alquinilo. amino, carbo-C1-6- alcoxi, carboxamida, carboxi, ciano, C3-7 cicloalquilo, C2-6 dialquilamino, C2-6 dialquilcarboxamida, C2-6 dialquilsulfonamida, C1-6 haloalcoxi, C1-6 haloalquilo, C1-6 haloalquilsulfinilo, C1-6 haloalquilsulfonilo, C1-6 haloalquiltio, halogeno, hidroxilo, nitro, sulfonamida y tiol; A y X son cada uno -CH2CH2-, cada uno opcionalmente sustituido con 1, 2, 3 o 4 sustituyentes seleccionados independientemente del grupo que consiste en C1-4 alcoxi, C1-3 alquilo, carboxi, ciano, C1-3 haloalquilo, halogeno, hidroxilo y oxo; J es -CH2CH2- o -C(=NOMe)CH2- cada uno opcionalmente sustituido con 1, 2, 3 o 4 sustituyentes seleccionados independientemente del grupo que consisten en C1-4 alcoxi, C1-3 alquilo, carboxi, ciano, C1-3 haloalquilo, halogeno, hidroxilo y oxo; y Ar es arilo o heteroarilo cada uno opcionalmente sustituido con 1, 2, 3, 4 o 5 sustituyentes seleccionados independientemente del grupo que consiste en C1-6 acilo, C1-6 aciloxi, C2-6 alquenilo, C1-6 alcoxi, C1-6 alquilo, C1-6 alquilcarboxamida, C1-6 alquilsulfonamida, C1-6 alquilsulfinilo, C1-6 alquilsulfonilo, C1-6 alquiltio, C1-6 alquilureilo, C1-6 alquilamino, C2-6 alquinilo, amino, carbo-C1-6-alcoxi, carboxamida, carboxi, ciano, C3-7 cicloalquilo, C2-6 dialquilamino, C2-6 dialquilcarboxamida, C2-6 dialquilsulfonamida, C1-6 haloalcoxi, C1-6 haloalquilo, C1-6 haloalquilsulfinilo, C1-6 haloalquilsulfonilo, C1-6 haloalquiltio, halogeno, C3-7 heterociclilo, hidroxilo, nitro, sulfonamida y tiol; siempre que dicho compuesto sea distinto de: 1-(4-(1H-pirazol-3-carbonil)piperazin-1-il)-2-(4-fluoro-1H-indol-3-il)etano-1,2-diona.
ARP070104362A 2006-10-03 2007-10-02 Derivados de pirazol como moduladores del receptor 5-ht2a de serotonina utiles para el tratamiento de los trastornos relacionados con dicho receptor AR063100A1 (es)

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US (6) US9434692B2 (es)
EP (1) EP2066641B1 (es)
JP (2) JP5346292B2 (es)
CN (2) CN102838546B (es)
AR (1) AR063100A1 (es)
AU (1) AU2007305235C1 (es)
CA (1) CA2664398C (es)
CL (1) CL2007002859A1 (es)
ES (1) ES2494846T3 (es)
JO (1) JO2954B1 (es)
PA (1) PA8749401A1 (es)
PE (1) PE20081454A1 (es)
TW (1) TWI415845B (es)
WO (1) WO2008042388A1 (es)

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