PE20020873A1 - Inhibidores de la metaloproteinasa de la matriz - Google Patents
Inhibidores de la metaloproteinasa de la matrizInfo
- Publication number
- PE20020873A1 PE20020873A1 PE2002000116A PE2002000116A PE20020873A1 PE 20020873 A1 PE20020873 A1 PE 20020873A1 PE 2002000116 A PE2002000116 A PE 2002000116A PE 2002000116 A PE2002000116 A PE 2002000116A PE 20020873 A1 PE20020873 A1 PE 20020873A1
- Authority
- PE
- Peru
- Prior art keywords
- hydrophobic group
- mmp
- hydrogen
- matrix metaloproteinase
- acceptor
- Prior art date
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- C07D471/00—Heterocyclic 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
- C07D471/02—Heterocyclic 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
- C07D471/04—Ortho-condensed systems
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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
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- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
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- 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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- A—HUMAN NECESSITIES
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- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- C07C235/42—Carboxylic 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
- C07C235/44—Carboxylic 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
- C07C235/58—Carboxylic 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
- C07C235/60—Carboxylic 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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- C07D213/02—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
- C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
- C07D213/30—Oxygen atoms
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- 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
- C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/36—Radicals substituted by singly-bound nitrogen atoms
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- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
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- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/14—Thiadiazoles; Hydrogenated thiadiazoles condensed with carbocyclic rings or ring systems
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- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
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- C07D285/20—1,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines condensed with carbocyclic rings or ring systems
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- C07D285/24—1,2,4-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
- C07D285/26—1,2,4-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
- C07D285/32—1,2,4-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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- C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
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- C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07D417/00—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
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- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
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- Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
Abstract
SE REFIERE A UN COMPUESTO QUE SE UNE ALOSTERICAMENTE CON EL DOMINIO CATALITICO DE LA MMP-13 Y QUE COMPRENDEN: UN GRUPO HIDROFOBICO; UN PRIMER Y UN SEGUN ACEPTOR DE ENLACE HIDROGENO; Y POR LO MENOS UN TERCER ACEPTOR DE ENLACE DE HIDROGENO Y UN SEGUNDO GRUPO HIDROFOBICO. LAS POSICIONES RELATIVAS DE LOS CENTROIDES SE DEFINEN POR LAS COORDENADAS CARTESIANAS EN A. EL PRIMER GRUPO HIDROFOBICO CONTIENE UN SISTEMA DE ANILLO BICICLICO CON 8-10 ATOMOS CON HETEROATOMOS QUE PUEDE ESTAR 4-SUSTITUIDO O 3,4-DISUSTITUIDO PERO CUYO ANCHO (INCLUYENDO LOS SUSTITUYENTES) ES MENOS QUE 4,0 A. CUANDO EL LIGANDO SE UNE A LA MMP-13, EL PRIMER, SEGUNDO Y TERCER ACEPTOR DE ENLACE HIDROGENO SE UNE RESPECTIVAMENTE CON Thr245, Thr 247, 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 INHIBEN LA ENZIMA DE LA METALOPROTEINASA DE LA MATRIZ -13 Y SON UTILES PARA EL TRATAMIENTO DE ENFERMEDADES QUE RESULTAN DE LA ROTURA DE TEJIDOS COMO ENFERMEDADES CARDIACAS, ESCLEROSIS MULTIPLE, ARTRITIS, ATEROSCLEROSIS, OSTEOPOROSIS
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US26882101P | 2001-02-14 | 2001-02-14 |
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EP (1) | EP1361873A4 (es) |
JP (1) | JP2004529874A (es) |
AR (1) | AR033859A1 (es) |
AU (1) | AU2002228302A1 (es) |
BR (1) | BR0207864A (es) |
CA (1) | CA2437643A1 (es) |
HN (1) | HN2002000037A (es) |
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SV (1) | SV2002000874A (es) |
UY (1) | UY27174A1 (es) |
WO (1) | WO2002064080A2 (es) |
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- 2002-02-13 PE PE2002000116A patent/PE20020873A1/es not_active Application Discontinuation
- 2002-02-13 UY UY27174A patent/UY27174A1/es not_active Application Discontinuation
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US20050004126A1 (en) | 2005-01-06 |
MXPA03007250A (es) | 2005-07-25 |
WO2002064080A3 (en) | 2002-12-12 |
HN2002000037A (es) | 2002-07-09 |
AU2002228302A1 (en) | 2002-08-28 |
AR033859A1 (es) | 2004-01-07 |
JP2004529874A (ja) | 2004-09-30 |
PA8539301A1 (es) | 2002-09-30 |
UY27174A1 (es) | 2002-09-30 |
WO2002064080A2 (en) | 2002-08-22 |
BR0207864A (pt) | 2004-03-09 |
EP1361873A4 (en) | 2005-10-26 |
US20030078276A1 (en) | 2003-04-24 |
CA2437643A1 (en) | 2002-08-22 |
SV2002000874A (es) | 2002-11-29 |
EP1361873A2 (en) | 2003-11-19 |
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