PE20030537A1 - Benzamida, heteroarilamida y amidas inversas - Google Patents
Benzamida, heteroarilamida y amidas inversasInfo
- Publication number
- PE20030537A1 PE20030537A1 PE2002001077A PE2002001077A PE20030537A1 PE 20030537 A1 PE20030537 A1 PE 20030537A1 PE 2002001077 A PE2002001077 A PE 2002001077A PE 2002001077 A PE2002001077 A PE 2002001077A PE 20030537 A1 PE20030537 A1 PE 20030537A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- benzamide
- cycloalkyl
- cr11r12
- triazin
- Prior art date
Links
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 title abstract 6
- 150000001408 amides Chemical class 0.000 title abstract 2
- -1 ALKYL Chemical group 0.000 abstract 3
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Chemical group BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- TUJKJAMUKRIRHC-UHFFFAOYSA-N hydroxyl Chemical class [OH] TUJKJAMUKRIRHC-UHFFFAOYSA-N 0.000 abstract 2
- 208000010125 myocardial infarction Diseases 0.000 abstract 2
- KZBUYRJDOAKODT-UHFFFAOYSA-N Chlorine Chemical group ClCl KZBUYRJDOAKODT-UHFFFAOYSA-N 0.000 abstract 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 1
- 238000001321 HNCO Methods 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- OWIKHYCFFJSOEH-UHFFFAOYSA-N Isocyanic acid Chemical compound N=C=O OWIKHYCFFJSOEH-UHFFFAOYSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 102100037602 P2X purinoceptor 7 Human genes 0.000 abstract 1
- 101710189965 P2X purinoceptor 7 Proteins 0.000 abstract 1
- 206010003246 arthritis Diseases 0.000 abstract 1
- 229910052794 bromium Inorganic materials 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 239000000460 chlorine Substances 0.000 abstract 1
- QUPDWYMUPZLYJZ-UHFFFAOYSA-N ethyl Chemical compound C[CH2] QUPDWYMUPZLYJZ-UHFFFAOYSA-N 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 208000028867 ischemia Diseases 0.000 abstract 1
- 201000008482 osteoarthritis Diseases 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 230000010410 reperfusion Effects 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
- C07D405/12—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 linked by a chain containing hetero atoms as chain links
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- C07D253/02—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00 not condensed with other rings
- C07D253/06—1,2,4-Triazines
- C07D253/065—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members
- C07D253/07—1,2,4-Triazines having 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
- C07D253/075—Two hetero atoms, in positions 3 and 5
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- 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
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- C07D263/18—Oxygen atoms
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- Ophthalmology & Optometry (AREA)
Abstract
SE REFIERE A BENZAMIDA, HETEROARILAMIDA, AMIDA DE FORMULA I DONDE A ES CONH, HNCO; X, Y, Z SON =(CR6), =(CR7), =(CR8), =N, ENTRE OTROS; R1 ES HETEROCICLO LIGADO A N, CONTIENE N, NH, O, S(O)n; R2 ES CLORO, BROMO, ALQUILO, CF3, CN; R3 ES ALQUILO, CICLOALQUIL-(CR11R12)s, ARIL-(CR11R12)q-(CH2)-, ENTRE OTROS; R4 Y R5 SON H, ALQUILO, OH-ALQUILO, CICLOALQUILO; R4 Y R5 JUNTO A N FORMAN UN HETEROCICLO; R6, R7, R8 SON H, HALOGENO, CIANO, HIDROXILO, ALQUILO; R11 Y R12 SON H, FLUORO, CIANO, HIDROXILO, CF3, CF3O, ALQUILO, ENTRE OTROS; CUANDO R3 ES CICLOALQUIL-(CR11R12)s; R1 Y R2 SON H; s ES 1-2, CICLOALQUILO ES DIFERENTE A ADAMANTILO. SON COMPUESTOS PREFERIDOS 2-CLORO-N-[2-(2-CLOROFENIL)ETIL]-5-(3,5-DIOXO-4,5-DIHIDRO-3H-[1,2,4]TRIAZIN-2-IL)BENZAMIDA; 2-CLORO-5-(3,5-DIOXO-4,5-DIHIDRO-3H-[1,2,4]TRIAZIN-2-IL)-N-[2-(2-FLUOROFENIL)ETIL]BENZAMIDA; 2-CLORO-5-(3,5-DIOXO-4,5-DIHIDRO-3H-[1,2,4]TRIAZIN-2-IL)-N-(2,2-DIFENILETIL)BENZAMIDA; ENTRE OTROS; LOS COMPUESTOS SON INHIBIDORES DEL CANAL IONICO CONTROLADO POR LIGANDO P2X7 Y PUEDEN SER UTILES PARA EL TRATAMIENTO DE INFLAMACION, OSTEOARTRITIS, ARTRITIS, ARTRITIS REUMATOIDEA, CANCER, REPERFUSION, ISQUEMIA EN APOPLEJIA, INFARTO DE MIOCARDIO, ENFERMEDADES AUTOINMUNES
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US33678101P | 2001-11-12 | 2001-11-12 |
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PE2002001077A PE20030537A1 (es) | 2001-11-12 | 2002-11-05 | Benzamida, heteroarilamida y amidas inversas |
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US (2) | US7214677B2 (es) |
EP (1) | EP1448535B1 (es) |
JP (1) | JP4365218B2 (es) |
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CA (1) | CA2466724C (es) |
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DE10005284A1 (de) | 2000-02-07 | 2001-08-09 | Bayer Ag | Verfahren zur Herstellung von 1-Amino-3-aryl-uracilen |
PA8557501A1 (es) | 2001-11-12 | 2003-06-30 | Pfizer Prod Inc | Benzamida, heteroarilamida y amidas inversas |
WO2003042190A1 (en) * | 2001-11-12 | 2003-05-22 | Pfizer Products Inc. | N-alkyl-adamantyl derivatives as p2x7-receptor antagonists |
PA8591801A1 (es) * | 2002-12-31 | 2004-07-26 | Pfizer Prod Inc | Inhibidores benzamidicos del receptor p2x7. |
MXPA05012086A (es) * | 2003-05-12 | 2006-02-22 | Pfizer Prod Inc | Inhibidores de benzamida del receptor p2x7. |
BRPI0512651A (pt) | 2004-06-29 | 2008-03-25 | Pfizer Prod Inc | método para a preparação de derivados de 5-4-(2-hidroxietil)-3,5-dioxo-4,5 dihidro-3h-1,2,4-trizin-2-ila com atividade inibidora de p2x7 por reaçaõ do derivado não substituìdo na posição 4 da trizina com um oxirano na presença de um ácido de lewis |
BRPI0512915A (pt) * | 2004-06-29 | 2008-04-15 | Warner Lambert Co | terapias de combinação utilizando inibidores benzamida do receptor p2x7 |
WO2006003500A1 (en) | 2004-06-29 | 2006-01-12 | Pfizer Products Inc. | Method for preparing 5-`4-(2-hydroxy-propyl)-3,5-dioxo-4,5-dihydro-3h`1,2,4!triazin-2-yl!-benzamide derivatives by deprotecting the hydroxyl-protected precursers |
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