AR032279A1 - METHOD FOR INHIBITING ONE OR MORE ACTIVITIES OF PROTEINIC KINASE, COMPOSED OF 2 - PIRAZOLIN-5-ONA PROTEINIC QUINASE INHIBITOR AND PHARMACEUTICAL COMPOSITION THAT INCLUDES IT - Google Patents

METHOD FOR INHIBITING ONE OR MORE ACTIVITIES OF PROTEINIC KINASE, COMPOSED OF 2 - PIRAZOLIN-5-ONA PROTEINIC QUINASE INHIBITOR AND PHARMACEUTICAL COMPOSITION THAT INCLUDES IT

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Publication number
AR032279A1
AR032279A1 ARP000103955A ARP000103955A AR032279A1 AR 032279 A1 AR032279 A1 AR 032279A1 AR P000103955 A ARP000103955 A AR P000103955A AR P000103955 A ARP000103955 A AR P000103955A AR 032279 A1 AR032279 A1 AR 032279A1
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AR
Argentina
Prior art keywords
group
proteinic
cycloalkyl
inhibiting
pharmaceutical composition
Prior art date
Application number
ARP000103955A
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Spanish (es)
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Abbott Gmbh & Co Kg
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Publication date
Application filed by Abbott Gmbh & Co Kg filed Critical Abbott Gmbh & Co Kg
Publication of AR032279A1 publication Critical patent/AR032279A1/en

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    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/4152—1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P17/06—Antipsoriatics
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P37/08—Antiallergic agents
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A61P5/16—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D231/18—One oxygen or sulfur atom
    • C07D231/20—One oxygen atom attached in position 3 or 5
    • C—CHEMISTRY; METALLURGY
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    • 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
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    • 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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    • 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

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Abstract

Un método para inhibir una o más actividades de quinasa proteínica que comprende la administracion de un compuesto de 2-pirazolin-5-ona representado por al formula (1) y sales fisiologicamente aceptables y metabolitos biologicamente activos del mismo, en donde R se selecciona del grupo un grupo sustituido o sin sustituir que consiste de: grupo alifático, aromático, un grupo cicloalquilo (C3-6), un grupo heterocíclico, un grupo aralquilo, un grupo cicloalquil-alquilo (C3-6) y un grupo del heterociclil-alquilo; R1 es hidrogeno o -A-Z; R2 es hidrogeno o se selecciona del grupo sustituido o sin sustituir que consiste de: grupo alquilo inferior, un grupo aromático, un grupo cicloalquilo (C3-6), un grupo heterocíclico, un grupo aralquilo, un grupo cicloalquil-alquilo (C3-6), y un grupo heterociclil-alquilo; en donde A y Z son como se describen en la memoria. Un compuesto de 2-pirazolin-5-ona representado por la formula (2) y sales fisiologicamente aceptables del mismo, en donde R se selecciona del grupo sustituido o sin sustituir que consiste de: indol, imidazol, 1,2,3-triazol, 1,2,4-triazol, benzimidazol, 4,5,6,7-tetrahidroindol, benzoindol, azaindol, indazol, piridina, quinolina, pirimidina, benceno, pirazina, pirrol, pirazol, oxazol y tiazol; R1 es hidrogeno o -A-Z-; en donde A y Z son como se describen en la memoria. Una composicion farmacéutica que comprende el compuesto descripto y un vehículo o diluyente farmacéuticamente aceptable.A method for inhibiting one or more protein kinase activities comprising the administration of a 2-pyrazolin-5-one compound represented by formula (1) and physiologically acceptable salts and biologically active metabolites thereof, wherein R is selected from group a substituted or unsubstituted group consisting of: aliphatic, aromatic group, a cycloalkyl (C3-6) group, a heterocyclic group, an aralkyl group, a cycloalkyl-alkyl (C3-6) group and a heterocyclyl-alkyl group ; R1 is hydrogen or -A-Z; R2 is hydrogen or is selected from the substituted or unsubstituted group consisting of: lower alkyl group, an aromatic group, a cycloalkyl (C3-6) group, a heterocyclic group, an aralkyl group, a cycloalkyl-C3-6 alkyl group ), and a heterocyclyl-alkyl group; where A and Z are as described in memory. A 2-pyrazolin-5-one compound represented by formula (2) and physiologically acceptable salts thereof, wherein R is selected from the substituted or unsubstituted group consisting of: indole, imidazole, 1,2,3-triazole , 1,2,4-triazole, benzimidazole, 4,5,6,7-tetrahydroindole, benzoindole, azaindole, indazole, pyridine, quinoline, pyrimidine, benzene, pyrazine, pyrrole, pyrazole, oxazole and thiazole; R1 is hydrogen or -A-Z-; where A and Z are as described in memory. A pharmaceutical composition comprising the described compound and a pharmaceutically acceptable carrier or diluent.

ARP000103955A 1999-07-30 2000-07-31 METHOD FOR INHIBITING ONE OR MORE ACTIVITIES OF PROTEINIC KINASE, COMPOSED OF 2 - PIRAZOLIN-5-ONA PROTEINIC QUINASE INHIBITOR AND PHARMACEUTICAL COMPOSITION THAT INCLUDES IT AR032279A1 (en)

Applications Claiming Priority (1)

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US14656399P 1999-07-30 1999-07-30

Publications (1)

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AR032279A1 true AR032279A1 (en) 2003-11-05

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EP (1) EP1218373A2 (en)
JP (1) JP2003506368A (en)
KR (1) KR20020091829A (en)
CN (1) CN1193026C (en)
AR (1) AR032279A1 (en)
AU (1) AU6388900A (en)
BG (1) BG106392A (en)
BR (1) BR0012896A (en)
CA (1) CA2380644A1 (en)
CZ (1) CZ2002302A3 (en)
HK (1) HK1049154A1 (en)
HU (1) HUP0400540A3 (en)
IL (1) IL147757A0 (en)
MX (1) MXPA02001088A (en)
NO (1) NO20020487L (en)
NZ (1) NZ516850A (en)
PL (1) PL354144A1 (en)
SK (1) SK1512002A3 (en)
TR (1) TR200200928T2 (en)
WO (1) WO2001009121A2 (en)
ZA (1) ZA200200477B (en)

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