PA8539301A1 - Inhibidores de la metaloproteinasa de la matriz - Google Patents

Inhibidores de la metaloproteinasa de la matriz

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Publication number
PA8539301A1
PA8539301A1 PA20028539301A PA8539301A PA8539301A1 PA 8539301 A1 PA8539301 A1 PA 8539301A1 PA 20028539301 A PA20028539301 A PA 20028539301A PA 8539301 A PA8539301 A PA 8539301A PA 8539301 A1 PA8539301 A1 PA 8539301A1
Authority
PA
Panama
Prior art keywords
mmp
hydrophobic group
matrix
hydrogen link
acceptors
Prior art date
Application number
PA20028539301A
Other languages
English (en)
Inventor
William Howard Roark
Daniel Fred Ortwine
Charles Andrianjara
Gregory Alexander Pavlousky
Original Assignee
Warner Lambert Co
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 Warner Lambert Co filed Critical Warner Lambert Co
Publication of PA8539301A1 publication Critical patent/PA8539301A1/es

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P11/06Antiasthmatics
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    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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    • C07C235/44Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/58Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/60Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
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    • C07D213/04Heterocyclic 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
    • C07D213/24Heterocyclic 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 substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D213/04Heterocyclic 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
    • C07D213/24Heterocyclic 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 substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D285/01Five-membered rings
    • C07D285/02Thiadiazoles; Hydrogenated thiadiazoles
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    • C07D285/221,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
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    • C07D285/181,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines
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    • C07D285/261,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with oxygen atoms directly attached to the ring sulfur atom substituted in position 6 or 7 by sulfamoyl or substituted sulfamoyl radicals
    • C07D285/321,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with oxygen atoms directly attached to the ring sulfur atom substituted in position 6 or 7 by sulfamoyl or substituted sulfamoyl radicals 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 in position 3
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Abstract

SE PROVEEN COMPUESTOS QUE SE UNEN ALOSTERICAMENTE CON EL DOMINIO CATALITICO DE LA MMP-13 Y QUE COMPRENDE: UN GRUPO HIDROFOBICO; UN PRIMER Y UN SEGUNDO ACEPTORES DE ENLACE DE HIDROGENO; Y POR LO MENOS UNO Y, CON PREFERENCIA LOS DOS -ES DECIR, UN TERCER ACEPTOR DE ENLACE DE HIDROGENO Y UN SEGUNDO GRUPO G¿HIDROFOBICO. LAS CARACTERISTICAS ANTERIORES SE DEFINEN EN LA MEMORIA DESCRIPTIVA. CUANDO EL LIGANDO SE UNE A LA MMP-13, EL PRIMER, EL SEGUNDO Y EL TERCER (SI ESTA PRESENTE) ACEPTORES DE ENLACE DE HIDROGENO SE UNEN RESPECTIVAMENTE CON THR245, THR 247 Y MET 253, EL PRIMER GRUPO HIDROFOBICO SE SITUA DENTRO DEL CANAL S1' DE LA MMP-13 Y EL SEGUNDO GRUPO HIDROFOBICO (SI ESTA PRESENTE) ESTA RELATIVAMENTE ABIERTO AL SOLVENTE. LOS COMPUESTOS, ESPECIFICAMENTE, INHIBEN LA ENZIMA DE LA METALOPROTEASA DE LA MATRIZ-13 Y, POR LO TANTO, RESULTAN DE UTILIDAD EN EL TRATAMIENTO DE ENFERMEDADES QUE RESULTAN DE LA ROTURA DE LOS TEJIDOS, TALES COMO POR EJEMPLO, LA ENFERMEDAD CARDIACA, LA ESCLEROSIS MULTIPLE, ARTRITIS, ATEREOSCLEROSIS Y OSTEOPOROSIS.
PA20028539301A 2001-02-14 2002-02-08 Inhibidores de la metaloproteinasa de la matriz PA8539301A1 (es)

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EP (1) EP1361873A4 (es)
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AR (1) AR033859A1 (es)
AU (1) AU2002228302A1 (es)
BR (1) BR0207864A (es)
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PE (1) PE20020873A1 (es)
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UY (1) UY27174A1 (es)
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US20030078276A1 (en) 2003-04-24
SV2002000874A (es) 2002-11-29
AU2002228302A1 (en) 2002-08-28
MXPA03007250A (es) 2005-07-25
US20050004126A1 (en) 2005-01-06
EP1361873A4 (en) 2005-10-26
JP2004529874A (ja) 2004-09-30
UY27174A1 (es) 2002-09-30
AR033859A1 (es) 2004-01-07
WO2002064080A2 (en) 2002-08-22
BR0207864A (pt) 2004-03-09
CA2437643A1 (en) 2002-08-22
EP1361873A2 (en) 2003-11-19

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