Back to results
US 2006/0154933 A1Published application
Inhibitors of Cdc25 phosphatases
AssigneeScras
InventorsGregoire Prevost, Marie-Christine Brezak Pannetier, Marie-Odile Galcera Contour, Christophe Thurieau, Francoise Gramatica, Bernard Ducommun, Christophe Lanco
Life of this patent
Estimating the term…
Abstract
A method of inhibiting cdc25 phosphatases in warm-blooded animals comprising administering to warm-blooded animals in need thereof an effective amount of a compound of the formula wherein the substituents are defined as in the specification.
Claims6
1-17. (canceled)
A method of inhibiting cdc 25 phosphatases in warm-blooded animals comprising administering to warm-blooded animals in need thereof an amount of a compound of the formula
- wherein A is
- wherein two of R1, R2, R3, R4, and R5 are hydrogen and the other three are independently selected from the group consisting of hydrogen, halogen, alkyl, hydroxy, alkoxy, alkylcarbonyloxy, alkylthio and —NR6R7, it being understood that:
- either R1 and one of R2 and R4 are independently selected from the group consisting of hydroxy, alkylcarbonyloxy and —NR6R7,
- or R2 and one of R3 and R5 are independently selected from the group consisting of hydroxy, alkylcarbonyloxy and —NR6R7,
- or R4 and one of R3 and R5 are independently selected from the group consisting of hydroxy, alkylcarbonyloxy and —NR6R7,
- or also one of R1, R3 and R5 is selected from the group consisting of hydroxy, alkylcarbonyloxy and —NR6R7, and B—N(W)—X—Y remainder is attached to A by nitrogen, R6 and R7 are independently each time that they occur a hydrogen or alkyl or R6 and R7 together with the nitrogen atom form a heterocycle of 4 to 7 ring members comprising 1 to 2 heteroatoms, the members necessary to complete the heterocycle being independently selected from the group consisting of —CR8R9—, —O—, —S— and —NR10—, R8 and R9 independently are each time that they occur selected from the group consisting of hydrogen, alkyl, alkoxy, benzyloxycarbonylamino and dialkylamino, and R10 independently is each time that it occurs hydrogen or alkyl,
- wherein either R11 and one of R13, R14 and R15 are hydroxy while R13, R14 and R15 as well as R16 are hydrogen,
- or R12 and R16 are hydroxy while R11, R13, R14 and R15 are hydrogen;
- B is —(CH2)p—, p is an integer from 0 to 1;
- W is hydrogen or alkyl;
- X is selected from the group consisting of 4CH2)q—, —(CH2)q—NH and —CO—(CH2)r—, q is an integer from 1 to 6 and r is an integer from 0 to 6;
- or B—N(W)—X—Y is
- wherein B is as defined above, t is an integer from 0 to 2, s is an integer from 0 to 1 and R17 and R18 are independently hydrogen or alkyl;
- and:
- when X is —CH2)q— or —CO—(CH2)r—, then Y is
- wherein R19 is selected from the group consisting of hydrogen, halogen, nitro, alkyl, alkylthio, —NR21R22, —SO2—NR22R24, —NH—SO2—R25 and —O—P(O)(OR26)(OR)27, R21 and R22 independently are hydrogen or alkyl,
- R23 and R24 independently are hydrogen or alkyl, or R23 and R24 representing together with the nitrogen atom which carries them a heterocycle with 5 to 7 ring members, the additional members are independently selected from the group consisting of —CHR28—, —NR29—, —O— and —S—, R28— and R29 are independently each time that they occur, hydrogen or alkyl,
- R25 is selected from the group consisting of alkyl, haloalkyl, aryl, heteroaryl, aralkyl and heteroaralkyl, the aryl or heteroaryl nucleus of which is optionally substituted by at least one member independently selected from the group consisting of halogen, alkyl, haloalkyl, hydroxy, alkoxy and nitro, except for the optional nitrogen atoms of the heteroaryl nucleus for which the optional substituents are alkyl,
- R26 and R27 are independently alkyl,
- and R20 is selected from the group consisting of hydrogen, halogen, alkyl, alkoxy and alkylthio,
- when X is 4CH2)q—NH— or when B—N(W)—X—Y is
- then Y exclusively is —SO2—R30 wherein R30 is selected from the group consisting of alkyl, haloalkyl, aryl, heteroaryl, aralkyl and heteroaralkyl, the aryl or heteroaryl nucleus of which is optionally substituted by at least one member independently selected from the group consisting of halogen, alkyl, haloalkyl, hydroxy, alkoxy and nitro, except for the optional nitrogen atoms of the heteroaryl nucleus for which the optional substituents are alkyl;
- it being understood that when B—N(W)—X—Y is
- then B is —CH2)—;
- or a pharmaceutically acceptable salt thereof sufficient to inhibit cdc25 phosphatases.
22 more elements
Dependencies are inferred from the claim text.