1.-9. (canceled)
10. A method for controlling the driving speed of a vehicle having a speed control device into which a set speed can be entered as driver command, said method comprising:
varying a reference variable of the speed control device within a specified or specifiable range of the set speed, based on an evaluation of a section of the road ahead of the driver, and based on maintaining a state of the vehicle with a fuel usage that is as low as possible, in a first operating mode of the speed control device;
detecting a change of the set speed;
changing over from the first operating mode to a second operating mode of the speed control device, when a change of the set speed has been detected;
in the second operating mode adjusting the reference variable based on the change, in such a manner that the speed control device is tuned to a higher driving speed in the case of an increase of the set speed resulting from the change, and to a lower driving speed in the case of a decrease of the set speed resulting from the change; and
changing back from the second operating mode to the first operating mode when an interruption criterion is satisfied.
11. The method according to the claim 10, further comprising:
determining a difference value of the change of the set speed;
determining an actual value of a reference variable at the change; and
setting the reference variable to a sum of the actual value of the reference variable and the difference value of the change.
12. The method according to claim 10, further comprising:
setting the reference variable to a sum of the actual value of the driving speed that exists at the change and the difference value of the change.
13. The method according to claim 10, further comprising:
changing back to the first operating mode as soon as a period of the interruption criterion has elapsed.
14. The method according to claim 10, further comprising:
changing back to the first operating mode as soon as a control deviation of the interruption criterion falls below a threshold value.
15. The method according to claim 10, further comprising:
switching from the second operating mode to a third operating mode as soon as the interruption criterion is fulfilled;
calculating a target value of the reference variable at the interruption criterion corresponding to the first operating mode;
determining an actual value of the reference variable at the interruption criterion;
bringing the reference variable from the actual value up to the target value of the reference variable in the third operating mode; and
changing from the third operating mode to the first operating mode after the approach.
16. A speed control device for the predictive control of the driving speed of a vehicle based on a specifiable set speed and based on a distance profile of a section of road ahead of the vehicle, wherein the speed control device is configured to modify the driving speed of the vehicle in response to a sudden change of the set speed, aligned with the change of the set speed, and to regulate it temporarily to a constant speed level.
17. The speed control device according to claim 16, wherein a distance profile of the section of the road ahead of the vehicle is determined in a predictive manner by means of a satellite-supported position determination system and a digital map.
18. A vehicle having a speed control device for controlling a driving speed of the vehicle, by executing a method according to claim 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. An (aza)indole derivative represented by the general formula (I):
wherein
T represents nitro, cyano or trifluoromethyl;
ring J represents an aryl ring or a 6-membered heteroaryl ring;
Q represents carboxy, lower alkoxycarbonyl, carbamoyl, mono(di)(lower alkyl)carbamoyl, sulfo, sulfamoyl or 5-tetrazolyl;
Y represents hydroxy;
X1, X2 and X3 independently represent CR2 or N with the proviso that all of X1, X2 and X3 do not represent N at the same time, and when two or more R2 exist, these R2 are optionally the same or different from each other; and
R1 and R2 independently represent a halogen atom, cyano, perfluoro(lower alkyl), -AA,
-A-D-E-G or \u2014N(-D-E-G)2 with the proviso that two (-D-E-G) are optionally different from each other;
in the formula, AA represents a hydrogen atom, hydroxy, thiol, \u2014CHO, carboxy, \u2014CONHR3, \u2014NHR3, \u2014N(R3)CHO, \u2014N(R3)CONHR4 or \u2014SO2NHR3;
A represents a single bond, \u2014O\u2014, \u2014S\u2014, \u2014CO\u2014, \u2014COO\u2014, \u2014CON(R3)\u2014, \u2014SO2\u2014, \u2014SO2N(R3)\u2014, \u2014N(R3)\u2014, \u2014N(R3)CO\u2014, \u2014N(R3)COO\u2014, \u2014N(R3)SO2\u2014 or \u2014N(R3)CONR4\u2014 wherein R3 and R4 independently represent a hydrogen atom or lower alkyl;
D represents optionally substituted lower alkylene, optionally substituted lower alkenylene, optionally substituted lower alkynylene, optionally substituted cycloalkylene, optionally substituted heterocycloalkylene, optionally substituted arylene or optionally substituted heteroarylene with the proviso that D is optionally further substituted by -E-G;
E represents a single bond, \u2014O\u2014, \u2014N(R5)\u2014, \u2014S\u2014, \u2014CO\u2014, \u2014COO\u2014, \u2014CON(R5)\u2014, \u2014SO2\u2014, \u2014SO2N(R5)\u2014, \u2014N(R5)CO\u2014, \u2014N(R5)COO\u2014, \u2014N(R5)SO2\u2014 or \u2014N(R5)CON(R6)\u2014 with the proviso that R5 and R6 independently represent a hydrogen atom or lower alkyl; and
G represents a hydrogen atom, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted cycloalkyl(lower alkyl), optionally substituted heterocycloalkyl(lower alkyl), optionally substituted aryl(lower alkyl) or optionally substituted heteroaryl(lower alkyl) with the proviso that when G is a hydrogen atom, E is a single bond, \u2014O\u2014,\u2014N(R5)\u2014, \u2014S\u2014, \u2014COO\u2014, \u2014CON(R5)\u2014, \u2014N(R5)CO\u2014, \u2014N(R5)CON(R6)\u2014 or \u2014SO2N(R5)\u2014, or R5 and R6 optionally bind together to form a ring, or with the proviso that when R1 and R2 or two R2 bound to the neighboring atoms exist, these R1 and R2 or two R2 optionally bind together to form a ring; respectively, or a prodrug thereof, or a pharmaceutically acceptable salt thereof.
2. The (aza)indole derivative as claimed in claim 1, wherein X1, X2 and X3 independently represent CR2 with the proviso that when two or more R2 exist, these R2 are optionally the same or different from each other, or a prodrug thereof, or a pharmaceutically acceptable salt thereof.
3. The (aza)indole derivative as claimed in claim 1, wherein T represents cyano, or a prodrug thereof, or a pharmaceutically acceptable salt thereof.
4. The (aza)indole derivative as claimed in claim 1, wherein Q represents carboxy, or a prodrug thereof, or a pharmaceutically acceptable salt thereof.
5. The (aza)indole derivative as claimed in claim 1, wherein ring J represents a benzene ring, or a prodrug thereof, or a pharmaceutically acceptable salt thereof.
6. The (aza)indole derivative as claimed in claim 4, wherein the group represented by the general formula (II):
is a group represented by the following general formula (IIa):
in the formula,
Z1, Z2 and Z3 independently represent CR7 or N;
Y1 represents hydroxyl; and
R7 represents a hydrogen atom, or a prodrug thereof, or a pharmaceutically acceptable salt thereof.
7. The (aza)indole derivative as claimed in claim 6, wherein
Z1 and Z3 represent CH, and Z2 represent CR8 or N;
Y1 represents hydroxyl; and
R8 represents a hydrogen atom, or a prodrug thereof, or a pharmaceutically acceptable salt thereof.
8. A xanthine oxidase inhibitor comprising as an active ingredient an (aza)indole derivative as claimed in claim 1, or a prodrug thereof, or a pharmaceutically acceptable salt thereof.
9. A pharmaceutical composition comprising as an active ingredient an (aza)indole derivative as claimed in claim 1, or a prodrug thereof, or a pharmaceutically acceptable salt thereof.
10. The pharmaceutical composition as claimed in claim 9, which is an agent for the treatment of a disease selected from the group consisting of hyperuricemia, gouty tophus, gouty arthritis, renal disorder associated with hyperuricemia and urinary calculi.
11. The pharmaceutical composition as claimed in claim 10, which is an agent for the treatment of hyperuricemia.
12. The pharmaceutical composition as claimed in claim 9, which is an agent for lowering serum uric acid level.
13. The pharmaceutical composition as claimed in claim 9, which is a uric acid production inhibitor.
14. The pharmaceutical composition as claimed in claim 9, which comprises a further combination with at least one drug selected from the group consisting of colchicines, a non-steroid anti-inflammatory drug, a steroid and a urine alkalizer as an active ingredient.
15. The (aza)indole derivative as claimed in claim 2, wherein T represents cyano, or a prodrug thereof, or a pharmaceutically acceptable salt thereof.
16. An (aza)indole derivative represented by the general formula (IA):
wherein
R1 represents a halogen atom, cyano, perfluoro(lower alkyl), -AA, -A-D-E-G or \u2014N(-D-E-G)2 with the proviso that two (-D-E-G) are optionally different from each other;
in the formula, AA represents a hydrogen atom, hydroxy, thiol, \u2014CHO, carboxy, \u2014CONHR3, \u2014NHR3, \u2014N(R3)CHO, \u2014N(R3)CONHR4 or \u2014SO2NHR3;
A represents a single bond, \u2014O\u2014, \u2014S\u2014, \u2014CO\u2014, \u2014COO\u2014, \u2014CON(R3)\u2014, \u2014SO2\u2014, \u2014SO2N(R3)\u2014, \u2014N(R3)\u2014, \u2014N(R3)CO\u2014, \u2014N(R3)COO\u2014, \u2014N(R3)SO2\u2014 or \u2014N(R3)CONR4\u2014 wherein R3 and R4 independently represent a hydrogen atom or lower alkyl;
D represents optionally substituted lower alkylene, optionally substituted lower alkenylene, optionally substituted lower alkynylene, optionally substituted cycloalkylene, optionally substituted heterocycloalkylene, optionally substituted arylene or optionally substituted heteroarylene with the proviso that D is optionally further substituted by -E-G;
E represents a single bond, \u2014O\u2014, \u2014N(R5)\u2014, \u2014S\u2014, \u2014CO\u2014, \u2014COO\u2014, \u2014CON(R5)\u2014, \u2014SO2\u2014, \u2014SO2N(R5)\u2014, \u2014N(R5)CO\u2014, \u2014N(R5)COO\u2014, \u2014N(R5)SO2\u2014 or \u2014N(R5)CON(R6)\u2014 with the proviso that R5 and R6 independently represent a hydrogen atom or lower alkyl; and
G represents a hydrogen atom, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted cycloalkyl(lower alkyl), optionally substituted heterocycloalkyl(lower alkyl), optionally substituted aryl(lower alkyl) or optionally substituted heteroaryl(lower alkyl) with the proviso that when G is a hydrogen atom, E is a single bond, \u2014O\u2014, \u2014N(R5)\u2014, \u2014S\u2014, \u2014COO\u2014, \u2014CON(R5)\u2014, \u2014N(R5)CO\u2014, \u2014N(R5)CON(R6)\u2014 or \u2014SO2N(R5)\u2014, or R5 and R6 optionally bind together to form a ring, or a prodrug thereof, or a pharmaceutically acceptable salt thereof.
17. The (aza)indole derivative as claimed in claim 16, which is selected from the group consisting of:
4-(3-cyano-indol-1-yl)-2-hydroxy-benzoic acid,
4-(3-cyano-5-methyl-indol-1-yl)-2-hydroxy-benzoic acid,
4-(3-cyano-6-chloro-indol-1-yl)-2-hydroxy-benzoic acid,
4-(3-cyano-5-fluoro-indol-1-yl)-2-hydroxy-benzoic acid,
4-(3-cyano-6-fluoro-indol-1-yl)-2-hydroxy-benzoic acid,
4-(3-cyano-6-trifluoromethyl-indol-1-yl)-2-hydroxy-benzoic acid,
4-(3-cyano-5-methoxy-indol-1-yl)-2-hydroxy-benzoic acid,
4-(5-chloro-3-cyano-indol-1-yl)-2-hydroxy-benzoic acid,
4-(3-cyano-5-hydroxy-indol-1-yl)-2-hydroxy-benzoic acid,
4-(3-cyano-4-hydroxy-indol-1-yl)-2-hydroxy-benzoic acid,
4-(3-cyano-6-hydroxy-indol-1-yl)-2-hydroxy-benzoic acid,
4-(3-cyano-6-methoxy-indol-1-yl)-2-hydroxy-benzoic acid,
4-(3-cyano-4-fluoro-indol-1-yl)-2-hydroxy-benzoic acid, and
4-(3-cyano-6-isopropyl-indol-1-yl)-2-hydroxy-benzoic acid.
18. The (aza)indole derivative as claimed in claim 1, which is selected from the group consisting of:
4-(3-cyano-5,6-difluoro-indol-1-yl)-2-hydroxy-benzoic acid,
4-(6-chloro-3-cyano-5-fluoro-indol-1-yl)-2-hydroxy-benzoic acid, and
4-(7-cyano-1,3-dioxolo4,5-findol-5-yl)-2-hydroxy-benzoic acid.