AR003444A1 - NEW COMPOUNDS OF ACETIDINONE, A PROCEDURE FOR THE PREPARATION OF THE SAME AND USE OF THE SAME FOR THE MANUFACTURE OF A MEDICINAL PRODUCT AND PHARMACEUTICAL COMPOSITION THAT CONTAINS THEM. - Google Patents
NEW COMPOUNDS OF ACETIDINONE, A PROCEDURE FOR THE PREPARATION OF THE SAME AND USE OF THE SAME FOR THE MANUFACTURE OF A MEDICINAL PRODUCT AND PHARMACEUTICAL COMPOSITION THAT CONTAINS THEM.Info
- Publication number
- AR003444A1 AR003444A1 ARP960103400A AR10340096A AR003444A1 AR 003444 A1 AR003444 A1 AR 003444A1 AR P960103400 A ARP960103400 A AR P960103400A AR 10340096 A AR10340096 A AR 10340096A AR 003444 A1 AR003444 A1 AR 003444A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- aryl
- same
- cycloalkyl
- heteroaryl
- Prior art date
Links
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Los compuestos de acetidinona de fórmula (I), en la cual: R1 y R2, que pueden ser iguales o diferentes, se seleccionan cada uno de hidrógeno, halógenoo alquilo C(1-8); R4 y R5, que pueden ser iguales o diferentes, se seleccionan cada uno dehid rógeno, alquilo C(1-6), alquenilo C(2-6), arilo, aril-alquilo(C1-4) y heteroaril-alquilo (C1-4), cada uno de los cuales puede estar sustituido opcionalmente, o R4 y R5 pueden estar unidos para formar el restode un anillo de cicloalquilo(C3- 7); X es un grupo enlazador; Y es un grupo arilo opcionalmente sustituido; Z es oxígeno y R3 es alquilo C(1-8),cicloalquilo C(3-8), cicloalquil C(3-8)-alquilo C(1-6), heteroarilo, heteroaril-alquilo (C1-4), arilo, o aril-alquilo(C1-4) , cada uno de loscuales puede estar sustituido opcionalmente, o Z es S(O)n, en el cual n es 0, 1 ó 2 y R3 es alquilo C(1-8), cicloalquilo C(3-8), cicloalquil C(3-8)-alquiloC(1-6), arilo, aril-alquilo (C1-4), heteroarilo, oheteroaril-alquilo (C1-4) , cada uno de los cuales puede estar sustituido opcinalmente; y con exclusiónde compuestos en los cuales: X es un enlace directo; un grupo X1(CH2)m en el cual X1 es CO, CONR6, COO, CONR6CO, ó CONHO en los cuales R6 eshidrógeno oalquilo C(1-6) y m es 0 ó un número entero de 1 a 12; o una cadena de alquileno C(1-12) interrumpida opcionalmente por X1; Z es S(O)n en el cual n es 0, 1 ó 2y R3 es alquilo c(1-8), cicloalquilo C(3-8), cicloalquil C(3-8)-alquilo C(1-6),arilo o aril-alquilo (C1-4) , cada uno de los cuales puede estar sustituidoopcionalmente; y R4 y R5 son ambos hidrógeno. Son inhibidores de la enzima Lp-PLA2 y son útiles en terapia, en particular para el tratamiento de laaterosclerosis.The acetidinone compounds of formula (I), in which: R1 and R2, which may be the same or different, are each selected from hydrogen, halogen or C (1-8) alkyl; R4 and R5, which may be the same or different, are each selected from hydrogen dehydrogen, C (1-6) alkyl, C (2-6) alkenyl, aryl, aryl (C1-4) alkyl and heteroaryl-C1 (alkyl). -4), each of which may be optionally substituted, or R4 and R5 may be linked to form the moiety of a (C3-7) cycloalkyl ring; X is a linker group; Y is an optionally substituted aryl group; Z is oxygen and R3 is C (1-8) alkyl, C (3-8) cycloalkyl, C (3-8) cycloalkyl-C (1-6) alkyl, heteroaryl, heteroaryl (C1-4) alkyl, aryl , or aryl (C1-4) alkyl, each of which may be optionally substituted, or Z is S (O) n, where n is 0, 1 or 2 and R3 is C (1-8) alkyl, C (3-8) cycloalkyl, C (3-8) cycloalkyl-C (1-6) alkyl, aryl, aryl-C1-4alkyl, heteroaryl, or heteroaryl-C1-4alkyl, each of which may be optionally substituted; and excluding compounds in which: X is a direct bond; a group X1 (CH2) m in which X1 is CO, CONR6, COO, CONR6CO, or CONHO in which R6 is hydrogen or C (1-6) alkyl and m is 0 or an integer from 1 to 12; or a C (1-12) alkylene chain optionally interrupted by X1; Z is S (O) n in which n is 0, 1 or 2 and R3 is c (1-8) alkyl, C (3-8) cycloalkyl, C (3-8) cycloalkyl-C (1-6) alkyl , aryl or aryl (C1-4) alkyl, each of which may be optionally substituted; and R4 and R5 are both hydrogen. They are inhibitors of the Lp-PLA2 enzyme and are useful in therapy, particularly for the treatment of atherosclerosis.
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9513442.5A GB9513442D0 (en) | 1995-07-01 | 1995-07-01 | Novel compounds |
| GBGB9515056.1A GB9515056D0 (en) | 1995-07-22 | 1995-07-22 | Novel compounds |
| GBGB9515206.2A GB9515206D0 (en) | 1995-07-25 | 1995-07-25 | Novel compounds |
| GBGB9516985.0A GB9516985D0 (en) | 1995-08-18 | 1995-08-18 | Novel compounds |
| GBGB9525132.8A GB9525132D0 (en) | 1995-12-08 | 1995-12-08 | Novel compounds |
| GBGB9608651.7A GB9608651D0 (en) | 1996-04-26 | 1996-04-26 | Novel compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR003444A1 true AR003444A1 (en) | 1998-08-05 |
Family
ID=51982972
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP960103400A AR003444A1 (en) | 1995-07-01 | 1996-06-28 | NEW COMPOUNDS OF ACETIDINONE, A PROCEDURE FOR THE PREPARATION OF THE SAME AND USE OF THE SAME FOR THE MANUFACTURE OF A MEDICINAL PRODUCT AND PHARMACEUTICAL COMPOSITION THAT CONTAINS THEM. |
Country Status (1)
| Country | Link |
|---|---|
| AR (1) | AR003444A1 (en) |
-
1996
- 1996-06-28 AR ARP960103400A patent/AR003444A1/en not_active Application Discontinuation
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