1. A compound represented by the formula (I):
52
wherein R1, R2, R3, and R4 are each independently hydrogen atom, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aralkyl, an optionally substituted non-aromatic heterocyclic group, acyl, optionally substituted amino, alkyloxy, hydroxy, cyano, or nitro; or
R1and R2, R3 and R4, and R2 and R3 each taken together with the adjacent nitrogen atom form the same or different 3- to 7-membered ring optionally containing O, N, or S, provided that R1and R2 and R3 and R4 do not form a ring when R2 and R3 taken together form a ring;
R5 and R6 are each independently hydrogen atom, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkyloxy, alkylthio, optionally substituted alkyloxycarbonyl, optionally substituted aryl, optionally substituted heteroaryl, halogen, hydroxy, mercapto, optionally substituted amino, carboxy, cyano, or nitro;
RB and RC are each independently hydrogen atom, alkyl, or alkyloxy; provided that in the case of both of RB and RC are hydrogen atom, R1 is hydrogen atom or alkyl, R2 is substituted amino, alkyloxy, hydroxy, cyano, or nitro; and R3 and R4are each independently hydrogen atom, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aralkyl, optionally substituted non-aromatic heterocyclic group, acyl, optionally substituted amino, alkyloxy, hydroxy, cyano, or nitro; or R3 and R4 each taken together with the adjacent nitrogen atom form the same or different 3- to 7-membered ring optionally containing O, S, or N;
X is N(R7), NHNH, O, or S wherein R7 is hydrogen atom or optionally substituted alkyl;
Y is optionally substituted 5-membered non-aromatic heterocycle-diyl or optionally substituted 5-membered heteroaryl-diyl;
Z is optionally substituted aryl or ptionally substituted heteroaryl; it optical active compound, its prodrug thereof, or their pharmaceutically acceptable salt, or their solvate.
2. A compound of claim 1, represented by the formula (II):
53
wherein R8, R9, R10, and R11 are each independently hydrogen atom, optionally substituted alkyl, alkenyl, alkynyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aralkyl, a non-aromatic heterocyclic group, acyl, substituted amino, alkyloxy, hydroxy, cyano, or nitro;
RB and RC are each independently hydrogen atom, alkyl, or alkyloxy; provided that in the case of both of RB and RC are hydrogen atom, R8 is hydrogen atom or alkyl, R9 is substituted amino, alkyloxy, hydroxy, cyano, or nitro; and R10 and R11 are each independently hydrogen atom, optionally substituted alkyl, alkenyl, alkynyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aralkyl, non-aromatic heterocyclic group, acyl, optionally substituted amino, alkyloxy, hydroxy, cyano, or nitro;
W is O, S, or N(RA) wherein RA is hydrogen atom or optionally substituted alkyl;
R5, R6, X, and Z are as defined in claim 1;
it optical active compound, its prodrug thereof, or their pharmaceutically acceptable salt, or their solvate.
3. A compound of claim 1, represented by the formula (III):
54
wherein R5, R6, and Z are as defined in claim 1, R8, R9, R10, R11, RB and RC are as defined in claim 2, their optical active compounds, the prodrugs thereof, or their pharmaceutically acceptable salts, or their solvates,
4. A compound of claim 1, represented by the formula (IV):
55
wherein R8, R9, R10 and R11 are as defined in claim 2;
R12 is hydrogen atom or alkyl;
RD and RE are each independently hydrogen atom or alkyl; provided that in the case of both of RD and RE are hydrogen atom, R8 is hydrogen atom or alkyl, R9 is substituted amino, alkyloxy, hydroxy, cyano, or nitro; and R10 and R11 are each independently hydrogen atom, optionally substituted alkyl, alkenyl, alkynyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aralkyl, non-aromatic heterocyclic group, acyl, optionally substituted amino, alkyloxy, hydroxy, cyano, or nitro;
V is optionally substituted aryl;
it optical active compound, its prodrug thereof, or their pharmaceutically acceptable salt, or their solvate.
5. A compound of claim 1 represented by the formula (V):
56
wherein R5 and R6 are each independently hydrogen atom, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkyloxy, alkylthio, optionally substituted alkyloxycarbonyl, optionally substituted aryl, optionally substituted heteroaryl, halogen atoms, hydroxy, mercapto, optionally substituted amino, carboxy, cyano, or nitro;
RF and RG are each independently hydrogen atom, alkyl, or alkyloxy;
X is N(R7), NHNH, O, or S wherein R7 is hydrogen atom or optionally substituted alkyl;
Y is optionally substituted 5-membered non-aromatic heterocycle-diyl or optionally substituted 5-membered heteroaryl-diyl;
Z is optionally substituted aryl or optionally substituted heteroaryl;
Q1 is NR1R2, OR1, or SR1, T1 is OR3 or SR3 wherein R1, R2 and R3 are each independently hydrogen atom, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aralkyl, optionally substituted non-aromatic heterocyclic group, acyl, optionally substituted amino, alkyloxy, hydroxy, cyano, or nitro; or
R1and R3, and R2 and R3 each taken together with the adjacent heteroatom form 5- to 7-membered ring;
it optical active compound, its prodrug thereof, or their pharmaceutically acceptable salt, or their solvate.
6. A compound of calim 5, represented by the formula (VI):
57
wherein Q2 is NR8R9, OR8, or SR8, T2 is OR10 or SR10 wherein R8, R9 and R10 are each independently hydrogen atom, optionally substituted alkyl, alkenyl, alkynyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aralkyl, optionally substituted non-aromatic heterocyclic group, acyl, optionally substituted amino, alkyloxy, hydroxy, cyano, or nitro;
W is O, S, or N(RA) wherein RA is hydrogen atom or optionally substituted alkyl;
R1, R6, RF, RG, X, and Z are as defined in claim 5;
its regioisomer, its optical active compound, its prodrug thereof, or their pharmaceutically acceptable salt, or their solvate.
7. A compound of claim 5, represented by the formula (VII):
58
wherein R5, R6, RF, RG, and Z are as defined in claim 5;
Q2 and T2 are as defined in claim 6;
its regioisomer, its optical active compound, its prodrug thereof, or their pharmaceutically acceptable salt, or their solvate.
8. A compound of calim 5, represented by the formula (VIII):
59
wherein R2 is hydrogen or alkyl;
RH and RJ are each independently hydrogen atom or alkyl;
the other symbols are as defined in claim 6:
its regioisomer, its optical active compound, its prodrug thereof, or their pharmaceutically acceptable salt, or their solvate.
9. A compound, its regioisomer, its optical active compound, its prodrug thereof, or their pharmaceutically acceptable salt, or their solvate of claim 1 or 5, wherein R1, R2, R3, and R4 are each independently hydrogen atom, optionally substituted alkyl, alkenyl, alkynyl, or acyl.
10. A compound, its regioisomer, its optical active compound, its prodrug thereof, or their pharmaceutically acceptable salt, or their solvate of any one of claims 2 to 4 or claims 6 to 8, wherein R8, R9, R10, and R11 are each independently hydrogen atom, optionally substituted alkyl, alkenyl, alkynyl, or acyl.
11. A pharmaceutical composition which contains as active ingredient a compound as described in any one of claims 1 to 10.
12. A pharmaceutical composition for use as an antitumor agent which contains as active ingredient a compound as described in any one of claims 1 to 10.
13. A pharmaceutical composition for use as a cytostatic agent which contains as active ingredient a compound as described in any one of claims 1 to 10.
14. A pharmaceutical composition for use as an inhibitor against a signal derived from Ras oncogene products which contains as active ingredient a compound as described in any one of claims 1 to 10.
15. Use of a compound of any one of claims 1 to 10 for the preparation of a pharmaceutical composition for treating cancer.
16. A method of treating a mammal, including a human, to alleviate a pathological effect of cancer, which comprises administration to the mammal of a compound as described in any one of claims 1 to 10.
The claims below are in addition to those above.
All refrences to claim(s) which appear below refer to the numbering after this setence.
1. A flexible connector assembly comprising:
an enclosure adapted to house an electrical circuit, the enclosure having an opening defining a longitudinal axis and a lateral axis;
a flexible cable having a first end and a second end opposite the first end, the first end electrically connected to the electrical circuit and fixed in location with reference to the enclosure; and
a movable connector having a mating end adapted to be connected to a mating connector, the movable connector electrically and mechanically coupled to the second end of the flexible cable, the movable connector slidably captured by the enclosure, such that the mating end of the movable connector is provided in the opening of the enclosure and is adapted for movement along the longitudinal axis and the lateral axis.
2. The flexible connector assembly of claim 1, further comprising:
a main printed circuit board, the electrical circuit mounted to the main printed circuit board; and
a connector printed circuit board electrically and mechanically coupled to the second end of the flexible cable, the movable connector mounted on the connector printed circuit board, such that the movable connector is electrically and mechanically coupled to the second end of the flexible cable.
3. The flexible connector assembly of claim 2, wherein the connector printed circuit board is adapted to rest on a support rail of the enclosure.
4. The flexible connector assembly of claim 3, further comprising:
a frame having an opening and connected to the connector printed circuit board, such that the mating end of the movable connector is provided through the opening of the frame.
5. The flexible connector assembly of claim 3, wherein the flexible cable comprises a ribbon cable.
6. A load control device for controlling the amount of power delivered from an AC power source to an electrical load, the load control device comprising:
a load control printed circuit board;
a flexible cable having a first end electrically and mechanically coupled to the load control printed circuit board, the flexible cable further comprising a second end opposite the first end;
a connector printed circuit board electrically and mechanically coupled to the second end of the flexible cable; and
a connector mounted on the connector printed circuit board, such that the connector is electrically coupled to the second end of the flexible cable, and thus to the load control printed circuit board;
wherein the connector is adapted to move along a longitudinal axis and a lateral axis of the load control device to allow for alignment of the connector.
7. The load control device of claim 6, further comprising:
an enclosure attached to and surrounding the load control printed circuit board, the connector slidably captured by the enclosure.
8. The load control device of claim 7, wherein the connector printed circuit board is adapted to rest on a support rail of the enclosure.
9. The load control device of claim 8, further comprising:
a frame having an opening and connected to the connector printed circuit board, such that the connector is provided through the opening of the frame.
10. The load control device of claim 9, wherein the flexible cable comprises a ribbon cable.
11. The load control device of claim 6, further comprising:
a controllably conductive device adapted to be coupled in series electrical connection between the electrical load and the AC power source; and
a controller for controlling the controllably conductive device so as to adjust the amount of power delivered to the electrical load;
wherein the controllably conductive device and the controller are mounted to the load control printed circuit board.
12. The load control device of claim 11, further comprising:
a user interface module adapted to be electrically and mechanically coupled to the connector and comprising an actuator operable to receive a user input, the controller responsive to the actuator when the user interface module is coupled to the connector;
wherein the connector is adapted to move along the longitudinal axis and the lateral axis of the load control device to allow for alignment of the actuator of the user interface module.
13. The load control device of claim 12, further comprising:
a faceplate having an opening, the actuator of the user interface module adapted to be provided in the opening of the faceplate;
wherein the connector is adapted to move along the longitudinal axis and the lateral axis of the load control device to align the actuator within the opening of the faceplate.
14. The load control device of claim 12, wherein the user interface module further comprises a visual display for displaying a representation of an amount of power being delivered to the electrical load, the controller operatively coupled to the visual display when the user interface module is coupled to the connector.
15. A load control device for controlling the amount of power delivered from an AC power source to an electrical load, the load control device comprising:
a load control printed circuit board;
a flexible cable having a first end electrically and mechanically coupled to the printed circuit board;
a connector electrically and mechanically coupled to a second end of the flexible cable, such that the connector is electrically coupled to the printed circuit board;
a user interface module electrically and mechanically coupled to the connector and comprising an actuator operable to receive a user input; and
a faceplate having an opening, the actuator of the user interface module adapted to be provided in the opening of the faceplate;
wherein the second connector is adapted to move along the longitudinal axis and the lateral axis of the load control device to align the actuator within the opening of the faceplate.
16. The load control device of claim 15, further comprising:
a connector printed circuit board electrically and mechanically coupled to the second end of the flexible cable, the connector mounted on the connector printed circuit board, such that the connector is electrically and mechanically coupled to a second end of the flexible cable.
17. The load control device of claim 16, further comprising:
an enclosure attached to and surrounding the load control printed circuit board, the connector slidably captured by the enclosure;
wherein the connector printed circuit board is adapted to rest on a support rail of the enclosure.
18. The load control device of claim 17, further comprising:
a frame having an opening and connected to the connector printed circuit board, such that the user interface module is coupled to the connector through the opening of the frame.
19. The load control device of claim 15, further comprising:
a controllably conductive device adapted to be coupled in series electrical connection between the electrical load and the AC power source; and
a controller for controlling the controllably conductive device so as to adjust the amount of power delivered to the electrical load;
wherein the controllably conductive device and the controller are mounted to the load control printed circuit board.
20. The load control device of claim 19, wherein the user interface module further comprises a visual display for displaying a representation of an amount of power being delivered to the electrical load, the controller operatively coupled to the visual display when the user interface module is coupled to the connector.