1. A compound of the formula (I)
in which
A represents a bond or \u2014C(R6AR6B)\u2014,
where
R6A represents hydrogen, (C1-C4)-alkyl or trifluoromethyl,
R6B represents hydrogen or (C1-C4)-alkyl,
R1 represents (C1-C6)-alkyl, (C2-C6)-alkenyl, (C2-C6)-alkynyl or (C3-C7)-cycloalkyl,
where (C1-C6)-alkyl, (C2-C6)-alkenyl and (C2-C6)-alkynyl may be substituted by 1 to 3 substituents independently of one another selected from the group consisting of deuterium, halogen, cyano, oxo, hydroxy, trifluoromethyl, (C3-C7)-cycloalkyl, (C1-C6)-alkoxy, trifluoromethoxy and phenyl,
in which (C3-C7)-cycloalkyl may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of (C1-C4)-alkyl, oxo, hydroxy, (C1-C4)-alkoxy and amino,
and
in which (C1-C6)-alkoxy may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of amino, hydroxy, (C1-C4)-alkoxy, hydroxycarbonyl and (C1-C4)-alkoxycarbonyl
and
in which phenyl may be substituted by 1 to 3 substituents independently of one another selected from the group consisting of halogen, cyano, nitro, (C1-C4)-alkyl, trifluoromethyl, hydroxy, hydroxymethyl, (C1-C4)-alkoxy, trifluoromethoxy, (C1-C4)-alkoxymethyl, hydroxycarbonyl, (C1-C4)-alkoxycarbonyl, aminocarbonyl, mono-(C1-C4)-alkylaminocarbonyl and di-(C1-C4)-alkylaminocarbonyl,
and
where (C3-C7)-cycloalkyl may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of fluorine, (C1-C4)-alkyl, (C1-C4)-alkoxy, hydroxy, amino and oxo,
R2 represents benzothienyl, phenyl, thienyl or furyl,
where benzothienyl, phenyl, thienyl and furyl may be substituted by 1 to 3 substituents independently of one another selected from the group consisting of halogen, cyano, nitro, (C1-C4)-alkyl, trifluoromethyl, hydroxy, (C1-C4)-alkoxy and trifluoromethoxy,
R3 represents a group of the formula
where
# represents the point of attachment to the nitrogen atom,
L represents (C1-C4)-alkanediyl,
where (C1-C4)-alkanediyl may be substituted by 1 to 3 substituents independently of one another selected from the group consisting of fluorine and (C1-C4)-alkyl,
R7A represents hydrogen or (C1-C4)-alkyl,
R7B represents hydrogen or (C1-C4)-alkyl,
or
R7A and R7B together with the carbon atom to which they are attached form a 3- to 6-membered carbocycle,
R8 represents hydroxycarbonyl, (C1-C4)-alkoxycarbonyl, aminocarbonyl, mono-(C1-C4)-alkylaminocarbonyl or di-(C1-C4)-alkylaminocarbonyl,
R9 represents hydroxy, trifluoromethoxy, (C1-C4)-alkoxy, hydroxycarbonyl, (C1-C4)-alkoxycarbonyl, aminocarbonyl, mono-(C1-C4)-alkylaminocarbonyl or di-(C1-C4)-alkylaminocarbonyl,
R4 represents phenyl, naphthyl or 5- to 10-membered heteroaryl,
where phenyl, naphthyl and 5- to 10-membered heteroaryl may be substituted by 1 to 3 substituents independently of one another selected from the group consisting of halogen, cyano, nitro, (C1-C4)-alkyl, difluoromethyl, trifluoromethyl, hydroxy, (C1-C4)-alkoxy, difluoromethoxy and trifluoromethoxy,
R5 represents hydrogen, deuterium, trifluoromethyl or (C1-C4)-alkyl,
and its salts, solvates and solvates of the salts.
2. The compound of claim 1, in which
A represents a bond or \u2014C(R6AR6B)\u2014,
where
R6A represents hydrogen,
R6B represents hydrogen,
R1 represents (C1-C6)-alkyl, (C2-C6)-alkenyl or (C3-C6)-cycloalkyl,
where (C1-C6)-alkyl and (C2-C6)-alkenyl may be substituted by 1 to 3 substituents independently of one another selected from the group consisting of fluorine, chlorine, cyano, oxo, hydroxy, trifluoromethyl, (C3-C6)-cycloalkyl, (C1-C4)-alkoxy, trifluoromethoxy and phenyl,
in which (C3-C6)-cycloalkyl may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of methyl, ethyl, oxo, hydroxy, methoxy, ethoxy and amino,
and
in which phenyl may be substituted by a substituent selected from the group consisting of fluorine, chlorine, cyano, methyl, ethyl, trifluoromethyl, methoxy, ethoxy, trifluoromethoxy, methoxymethyl, ethoxymethyl, hydroxycarbonyl, methoxycarbonyl, ethoxycarbonyl and aminocarbonyl,
and
where (C3-C6)-cycloalkyl may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of fluorine, methyl, ethyl, methoxy, ethoxy, hydroxy, amino and oxo,
R2 represents phenyl or thienyl,
where phenyl and thienyl may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of fluorine, chlorine, bromine, methyl, ethyl, trifluoromethyl, hydroxy, methoxy, ethoxy and trifluoromethoxy,
R3 represents a group of the formula
where
# represents the point of attachment to the nitrogen atom,
L represents methylene,
where methylene may be substituted by 1 or 2 methyl substituents,
R7A represents hydrogen or methyl,
R7B represents hydrogen or methyl,
or
R7A and R7B together with the carbon atom to which they are attached form a cyclopropyl ring,
R8 represents hydroxycarbonyl, methoxycarbonyl, ethoxycarbonyl, aminocarbonyl, methylaminocarbonyl, ethylaminocarbonyl, dimethylaminocarbonyl or diethylaminocarbonyl,
R9 represents hydroxy, trifluoromethoxy, methoxy, ethoxy, hydroxycarbonyl, methoxycarbonyl, ethoxycarbonyl, aminocarbonyl, methylaminocarbonyl, ethylaminocarbonyl, dimethylaminocarbonyl or diethylaminocarbonyl,
R4 represents phenyl,
where phenyl is substituted by 1 to 3 substituents independently of one another selected from the group consisting of fluorine, chlorine, cyano, methyl, ethyl, difluoromethyl, trifluoromethyl, methoxy, difluoromethoxy and trifluoromethoxy,
R5 represents hydrogen or methyl,
and its salts, solvates and solvates of the salts.
3. The compound of claim 1, in which
A represents a bond or \u2014C(R6AR6B)\u2014,
where
R6A represents hydrogen,
R6B represents hydrogen,
R1 represents (C2-C4)-alkyl, (C2-C4)-alkenyl or cyclopropyl, where (C2-C4)-alkyl and (C2-C4)-alkenyl may be substituted by 1 or 2 substituents independently of one another selected from the group consisting of fluorine, oxo, hydroxy and trifluoromethyl,
R2 represents phenyl,
where phenyl is substituted by a substituent selected from the group consisting of fluorine and chlorine,
R3 represents a group of the formula
where
# represents the point of attachment to the nitrogen atom,
L represents methylene,
R7A represents hydrogen or methyl,
R7B represents hydrogen or methyl,
or
R7A and R7B together with the carbon atom to which they are attached form a cyclopropyl ring,
R8 represents hydroxycarbonyl, methoxycarbonyl, ethoxycarbonyl or aminocarbonyl,
R9 represents hydroxy, methoxy, hydroxycarbonyl, methoxycarbonyl, ethoxycarbonyl or aminocarbonyl,
R4 represents a group of the formula
where
* represents the point of attachment to the group \u2014C(R5)(AC(\u2550O)NHR3)\u2014,
R10 represents hydrogen, chlorine, trifluoromethyl, trifluoromethoxy or methoxy,
R11 represents hydrogen, fluorine, chlorine, trifluoromethyl, trifluoromethoxy or methoxy,
where at least one of the radicals R10 and R11 is different from hydrogen,
R5 represents hydrogen or methyl,
and its salts, solvates and solvates of the salts.
4. A process for preparing compounds of the formula (I) as defined in claim 1, comprising:
A coupling a compound of the formula (II)
in which R1 and R2 each have the meanings given in claim 1,
in an inert solvent with activation of the carboxylic acid function with a compound of the formula (III)
in which A, R3, R4 and R5 each have the meanings given in claim 1,
or
B reacting a compound of the formula (IV)
in which R1 and R2 each have the meanings given in claim 1,
in an inert solvent in the presence of a base with a compound of the formula (V)
in which A, R3, R4 and R5 each have the meanings given in claim 1
and
X1 represents a leaving group,
or
C coupling a compound of the formula (VI)
in which A, R1, R2, R4 and R5 each have the meanings given in claim 1,
in an inert solvent with activation of the carboxylic acid function with a compound of the formula (VII)
H2N\u2014R3\u2003\u2003(VII),
in which R3 has the meaning given in claim 1,
and optionally converting the resulting compounds of formula (I) with the appropriate (i) solvents andor (ii) acids or bases into their solvates, salts andor solvates of the salts.
5. A pharmaceutical composition comprising a compound of claim 1 and an inert, non-toxic, pharmaceutically suitable auxiliary.
6. The pharmaceutical composition of claim 5, further comprising one or more active substances selected from the group consisting of diuretics, angiotensin AII antagonists, ACE inhibitors, beta-receptor blockers, mineralocorticoid receptor antagonists, organic nitrates, NO donors and positive-inotropic active substances.
7. A method for the treatment of acute and chronic heart failure, hypervolaemic and euvolaemic hyponatraemia, cirrhosis of the liver, ascites, oedema and the syndrome of inadequate ADH secretion (SIADH) comprising administering to a human or animal in need thereof an effective amount of at least one compound of claim 1.
8. A method for the treatment of acute and chronic heart failure, hypervolaemic and euvolaemic hyponatraemia, cirrhosis of the liver, ascites, oedema and the syndrome of inadequate ADH secretion (SIADH) comprising administering to a human or animal in need thereof an effective amount of at least one pharmaceutical composition of claim 5.
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 image projection system comprising:
A spatial light modulator (SLM) comprises a plurality of pixel elements, wherein each of the pixel elements further comprises a deflectable mirror, and at least a first electrode and a second electrode for controlling said deflectable mirror to deflect to different tilt angles to reflect and modulate an illumination light for displaying an image; and
a controller for applying a voltage to the second electrode wherein said voltage applied in an initial operation period is different from said voltage applied in an image display period.
2. The image projection system according to claim 1, wherein:
said deflectable mirror is configured to deflect along an oscillation axis and the second electrode is disposed farther away from the oscillation axis than the first electrode.
3. The image projection system according to claim 1, wherein:
the second electrode is disposed farther away from the deflectable mirror than the first electrode when the deflectable mirror is operated at a horizontal angular position.
4. The image projection system according to claim 1, wherein:
the controller applying said voltage to the second electrode according to an equation:
|Vi|>|Va|, where \u201cVi\u201d is the voltage applied during the initial operation period of the deflectable mirror and \u201cVa\u201d is the voltage applied during the image display period.
5. The image projection system according to claim 1, wherein:
the controller further controls a period for applying said voltage to the second electrode according to an equation: |Ti|>|Ta|, where \u201cTi\u201d is the initial operation period of the deflectable mirror and \u201cTa\u201d is the image display period of the deflectable mirror.
6. The image projection system according to claim 1, wherein:
the controller further applies said voltage with a ramp waveform to the second electrode.
7. The image projection system according to claim 1, wherein:
the controller further applies said voltages to said first and second electrodes according to following equations:
|V1|<|V2|, if S1>S2, while
|V1|>|V2|, if S1<S2,
where \u201cS1\u201d is an area size of the first electrode, \u201cS2\u201d is an area size of the second electrode, \u201cV1\u201d is a voltage applied to the first electrode and \u201cV2\u201d is a voltage applied to the second electrode during the initial operation period.
8. The image projection system according to claim 1, wherein:
the controller applies said voltages to said first and second electrodes to generate Coulomb forces applied to the deflectable mirror according to an equation: C1<C2, where \u201cC1\u201d is the Coulomb force generated from the first electrode to the deflectable mirror when said first electrode is operated at a horizontal position and \u201cC2\u201d is the Coulomb force generated from the second electrode to the deflectable mirror when said deflectable mirror is operated at said horizontal position during the initial operation period.
9. The image projection system according to claim 1, further comprising:
a light source to emit an illuminating light to the spatial light modulator, wherein the light source is controlled to not emit said illumination light during the initial operation period.
10. The image projection system according to claim 1, wherein:
the first electrode is connected to a memory, and the second electrode is connected to a common line wherein said common line is connected to provide signals to a plurality of the pixel elements.
11. An image projection system comprising:
a spatial light modulator (SLM) comprises a plurality of pixel elements, wherein each pixel comprises a deflectable mirror,
each of said pixel elements further comprises at least a first electrode and a second electrode for controlling said deflectable mirror to deflect to different tilt angles to reflect and modulate an illumination light for displaying an image; and
a controller for applying a voltage to the second electrode wherein said controller applies a different voltage when said deflectable mirror is operated at a stationary state and when the mirror is operated at a transition state.
12. The image projection system according to claim 11, wherein:
said deflectable mirror is configured to deflect along an oscillation axis and the second electrode is disposed farther away from the oscillation axis than the first electrode.
13. The image projection system according to claim 11, wherein:
the second electrode is disposed farther away from the deflectable mirror than the first electrode when the deflectable mirror is operated at a horizontal angular position.
14. The image projection system according to claim 11, wherein:
the controller applying said voltage to the second electrode according to an equation:
|Vt|>|Vs|, where \u201cVs\u201d is the voltage applied when the mirror is in the stationary tilting state and \u201cVt\u201d is the voltage applied when the mirror is in the transition state.
15. The image projection system according to claim 11, wherein:
the controller further applies said voltage with a ramp waveform to the second electrode when the deflectable mirror is operated in the transition state.
16. The image projection system according to claim 11, wherein:
the controller applies said voltage to the second electrode when the deflectable mirror is operated in the transition state to control a length of time of operating said deflectable mirror in the transition state.
17. The image projection system according to claim 11, wherein:
the controller further applies said voltage to the second electrode when the deflectable mirror is operated in the stationary state to control the deflectable mirror wherein said voltage applied to the second electrode is independent from a voltage applied to the first electrode.
18. The image projection system according to claim 11, wherein:
the controller applies said voltages to said first and second electrodes according to the following equations:
|i V1|<|Vosc| if S1>S2, and
|V1|>|Vosc| if i S1<S2,
where \u201cS1\u201d is an area size of the first electrode, \u201cS2\u201d is an area size of the second electrode, \u201cV1\u201d is the voltage applied to the first electrode, and \u201cVosc\u201d is the voltage applied to the second electrode for operating said deflectable mirror in an intermediate oscillation state.
19. The image projection system according to claim 11, wherein:
the controller applies said voltages to said first and second electrodes according to the following equations:
|V1|\u2267|Vh| if S1>S2, and
|V1|<|Vh| if S1<S2,
where \u201cS1\u201d is an area size of the first electrode, \u201cS2\u201d is an area size of the second electrode, \u201cV1\u201d is the voltage applied to the first electrode, and \u201cVh\u201d is the voltage applied to the second electrode to control the deflectable mirror to operate in the stationary state independent from the voltage applied to the first electrode.
20. The image projection system according to claim 11, wherein:
the first electrode is connected to a memory, and the second electrode is connected to a common line wherein said common line is connected to provide signals to a plurality of the pixel elements.
21. An image projection system comprising:
a spatial light modulator (SLM) comprises a plurality of pixel elements, wherein each pixel comprises a deflectable mirror,
each of said pixel elements further comprises at least a first electrode and a second electrode for controlling said deflectable mirror to deflect to different tilt angles to reflect and modulate an illumination light for displaying an image; and a controller for applying a voltage to the first and second electrodes to generate a greater Coulomb force from the second electrode than the Coulomb force from the first electrode.
22. The image projection system according to claim 21, wherein:
said deflectable mirror is configured to deflect along an oscillation axis and the second electrode is disposed farther away from the oscillation axis than the first electrode.
23. The image projection system according to claim 21, wherein:
the second electrode is disposed farther away from the deflectable mirror than the first electrode when the deflectable mirror is operated at a horizontal angular position.
24. The image projection system according to claim 21, wherein:
the controller applies said voltage to the second electrode when the deflectable mirror is operated in the transition state to control a length of time of operating said deflectable mirror in the transition state.
25. The image projection system according to claim 21, wherein:
the controller further applies said voltage with a ramp waveform to the second electrode.
26. The image projection system according to claim 21, wherein:
the first electrode is connected to memory, and the second electrode is connected to a common line which is provided for a plurality of the pixels;
the first electrode is connected to a memory, and the second electrode is connected to a common line wherein said common line is connected to provide signals to a plurality of the pixel elements.