UY25232A1 - Compuestos terapéuticamente activos basados en el reemplazo bioisostero del catecol por el indazol en inhibidores de pde 4 . - Google Patents

Compuestos terapéuticamente activos basados en el reemplazo bioisostero del catecol por el indazol en inhibidores de pde 4 .

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Publication number
UY25232A1
UY25232A1 UY25232A UY25232A UY25232A1 UY 25232 A1 UY25232 A1 UY 25232A1 UY 25232 A UY25232 A UY 25232A UY 25232 A UY25232 A UY 25232A UY 25232 A1 UY25232 A1 UY 25232A1
Authority
UY
Uruguay
Prior art keywords
therapeutically active
diseases
indazol
replacement
compound
Prior art date
Application number
UY25232A
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English (en)
Inventor
Anthony Marfat
Original Assignee
Pfizer Prod Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of UY25232A1 publication Critical patent/UY25232A1/es

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/525—Isoalloxazines, e.g. riboflavins, vitamin B2
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
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  • Health & Medical Sciences (AREA)
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  • Pulmonology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Communicable Diseases (AREA)
  • Otolaryngology (AREA)
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  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Composiciones terapéuticamente activas útiles para tratamiento o prevención de enfermedades y afecciones que comprenden enfermedades inflamatorias, respiratorias, infecciosas, y otras que incluyen enfermedades de reabsorción ósea y lesiones de reperfusión. También en asma, psoriasis, artritis y otras enfermerdades que implican la producción de TNF.Comprende un compuesto inhibidor de la isoenzima 4 de la fosfodiesterasa (PDE4) y del factor de necrosis tumoral y donde un indazol es componente esencial de la estructura química general de dicho compuesto, y donde el mismo constituye un reemplazo biosostérico de un componente de catecol o de derivado funcional del mismo en un compuesto conocido que tiene la misma dicha actividad terapéutica y los mismos componentes restantes de estructura química global. El agente deseado terapeuticamente activo de formula IA y IB, donde R es H, alquilo, (CH2)n , con n 0,1,2; R1 es H, alquilo, alquenilo; R2a y R2b son H y los sustituyentes (IC,ID,IE,IF) Ejemplo: 1-((1-Ciclopentil-3-etil-1H-indazol-6-il)-4-(1,3ditian-2-ilideno-ciclohexano-carbonitrilo
UY25232A 1997-11-04 1998-11-04 Compuestos terapéuticamente activos basados en el reemplazo bioisostero del catecol por el indazol en inhibidores de pde 4 . UY25232A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US6416097P 1997-11-04 1997-11-04

Publications (1)

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UY25232A1 true UY25232A1 (es) 2000-12-29

Family

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UY25232A UY25232A1 (es) 1997-11-04 1998-11-04 Compuestos terapéuticamente activos basados en el reemplazo bioisostero del catecol por el indazol en inhibidores de pde 4 .

Country Status (34)

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US (2) US6716978B2 (es)
EP (1) EP1040100A1 (es)
JP (1) JP2001521925A (es)
KR (1) KR20010031783A (es)
CN (1) CN1281441A (es)
AP (1) AP1122A (es)
AR (1) AR016413A1 (es)
AU (1) AU754184B2 (es)
BG (1) BG104391A (es)
BR (1) BR9813938A (es)
CA (1) CA2309175A1 (es)
CZ (1) CZ20001623A3 (es)
DZ (1) DZ2639A1 (es)
EA (1) EA200000385A1 (es)
HN (1) HN1998000172A (es)
HR (1) HRP20000262A2 (es)
HU (1) HUP0100330A3 (es)
ID (1) ID24942A (es)
IL (1) IL135714A0 (es)
IS (1) IS5452A (es)
MA (1) MA26562A1 (es)
NO (1) NO20002127L (es)
NZ (1) NZ503995A (es)
OA (1) OA11353A (es)
PA (1) PA8462601A1 (es)
PE (1) PE131099A1 (es)
PL (1) PL340799A1 (es)
SK (1) SK6262000A3 (es)
TN (1) TNSN98199A1 (es)
TR (1) TR200001256T2 (es)
UY (1) UY25232A1 (es)
WO (1) WO1999023076A1 (es)
YU (1) YU25400A (es)
ZA (1) ZA9810042B (es)

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