1. A compound of the formula
in which
R is deuterium, halogen, or hydrogen;
R1 is aryl-C0-C4-alkyl or heterocyclyl-C0-C4-alkyl, which radicals are unsubstituted or substituted by 1-4 C1-C8 alkoxy, C1-C8 alkoxycarbonyl, C1-C8 alkyl, C0-C8 alkylcarbonyl, C1-C8 alkylsulphonyl, unsubstituted or substituted aryl, aryl-C0-C4 alkoxycarbonyl, cyano, halogen, unsubstituted or substituted heterocyclyl, hydroxy, nitro, oxide, oxo, tri-C1-C4 alkylsilyl, trifluoromethoxy or trifluoromethyl, wherein the heterocyclyl of the heterocyclyl-C0-C4-alkyl stands for a saturated, partially saturated or unsaturated, 4-8-membered monocyclic ring system, or a saturated, partially saturated or unsaturated, 7-12-membered bicyclic ring system, or a partially saturated or unsaturated, 9-12-membered tricyclic ring system which comprises an N, O or S atom in at least one of the rings, it being possible for an additional N, O or S atom to be present in one ring;
R2 is
a) deuterium, halogen, hydroxy, cyano or hydrogen; or
b) C2-C8 alkenyl, C2-C8 alkynyl, C1-C8 alkoxy, C1-C4 alkoxycarbonyl-C1-C4 alkyl, C1-C8 alkyl, C0-C4 alkylcarbonyl, aryl-C0-C4 alkyl, carboxy-C1-C4 alkyl, C3-C8 cycloalkyl or heterocyclyl-C0-C4 alkyl, which radicals are unsubstituted or substituted by 1-4 C1-C8 alkoxy, C1-C8 alkoxycarbonyl, C1-C8 alkyl, C0-C8 alkylcarbonyl, C1-C8 alkylsulphonyl, unsubstituted or substituted aryl, aryl-C0-C4 alkoxycarbonyl, cyano, halogen, unsubstituted or substituted heterocyclyl, hydroxy, nitro, oxide, oxo, tri-C1-C4 alkylsilyl, trifluoromethoxy or trifluoromethyl;
R3 is C1-C8 alkyl;
Q is oxygen;
m is a number 0, 1 or 2;
n is 1;
or a pharmaceutically acceptable salt thereof,
where
R1 is not C1-C8 alkyl-substituted aryl if R2 is hydrogen, and which compound shows an aromatase inhibitory activity at least 10 times higher, than the compound of the formula (I) with the opposite configuration around the asymmetric carbon atom labelled \u201c*\u201d.
2. A compound according to claim 1, where R is deuterium or hydrogen.
3. A compound according to claim 1, where R1 is optionally substituted phenyl, optionally substituted naphthyl, benzofuranyl, benzobthiophenyl, benzoimidazolyl, benzodisothiazolyl, benzodisoxazolyl, benzobthiophenyl, imidazolyl, indazolyl, oxazolyl, pyridyl, pyrrolyl, thiazolyl or thiophenyl.
4. A compound according to claim 1, where R2 is C1-C8 alkoxy, hydroxy, C1-C8 alkyl, optionally substituted aryl-C0-C4 alkyl, deuterium, halogen, cyano or hydrogen.
5. A method for the treatment of estrogen-dependent breast cancer, which comprises administering to a subject having the disease a therapeutically effective amount of a compound of the formula (I) or a pharmaceutically acceptable salt thereof according to claim 1.
6. A method for the treatment of gynaecomastia, which comprises administering to a subject having gynaecomastia a therapeutically effective amount of a compound of the formula (I) or a pharmaceutically acceptable salt thereof according to claim 1.
7. A pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof according to claim 1, and a pharmaceutically acceptable excipient.
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 digital imaging device for capturing an image and generating a color signal from the image for application to an output device having specific color sensitivities, said imaging device further being one of many devices of the same type useful with the output device, said digital imaging device comprising:
a color sensor for capturing the image and generating the color signal from the captured image, said color sensor having predetermined spectral sensitivities;
an optical section having predetermined spectral characteristics, said optical section interposed in image light from the image directed to the color sensor thereby imparting the predetermined spectral characteristics to the image light, the combination of the spectral sensitivities of the color sensor and the spectral characteristics of the optical section uniquely distinguishing the imaging device from other imaging devices of the same type; and
a set of matrix coefficients uniquely determined for the imaging device in order to generate an optimized color signal, wherein said matrix coefficients are (a) automatically calculated by a matrix coefficient calculation from image data obtained by the color sensor from a color chart and (b) used for correcting the spectral sensitivities of the color sensor and the spectral characteristics of the optical section for the color sensitivities of the output device.
2. An imaging device as claimed in claim 1 in which the optical section includes a lens for directing the image light from the image upon the color sensor, said lens having a predetermined lens spectral characteristic, and wherein the matrix coefficients correct the lens spectral characteristic for the color sensitivities of the output device.
3. An imaging device as claimed in claim 1 in which the optical section includes a blurry filter for spatially low pass filtering the image light directed upon the color sensor, said blur filter having a predetermined spectral characteristic, and wherein the matrix coefficients correct the spectral characteristic for the color sensitivities of the output device.
4. An imaging device as claimed in claim 1 in which the optical section includes an infrared cutoff filter for filtering the image light directed upon the color sensor, said infrared cutoff filter having a predetermined infrared spectral characteristic, and wherein the matrix coefficients correct the infrared spectral characteristic for the color sensitivities of the output device.
5. An imaging device as claimed in claim 1 wherein the color sensor includes a color filter array for color filtering the image light directed upon the color sensor, said color filter array having a predetermined color filter spectral characteristic, and wherein the matrix coefficients correct the color filter spectral characteristic for the color sensitivities of the display device.
6. An imaging device as claimed in claim 1 wherein the imaging device comprises a digital camera.
7. An imaging device as claimed in claim 1 wherein the imaging device comprises a digital scanner.
8. An imaging device as claimed in claim 1 wherein the output device comprises a display device.
9. An imaging device as claimed in claim 1 wherein the output device comprises a printing device.
10. An imaging device as claimed in claim 1 further comprising a color processing section for implementing a matrix coefficient on the color signal in order to generate the optimized color signal, said color processing section using the set of matrix coefficients that are uniquely determined for the imaging device in order to generate the optimized color signal.
11. An imaging device as claimed in claim 1 in which the optical section and the set of matrix, coefficients are included on a sub-assembly that is removable from the digital imaging device for purpose of servicing and repair of the imaging device.
12. An imaging device as claimed in claim 1 in which the output device is a reference device, and said matrix coefficients correct the spectral sensitivities of the color sensor and the spectral characteristics of the optical section for the reference color sensitivities of the output device.
13. An electronic imaging system including a component useful with an imaging device as claimed in claim 1, wherein the computer comprises a color processing section for implementing a matrix connection on thee color signal using the set of matrix coefficients in order to generate the optimized color signal, and the imaging device provides the color signal together with the matrix coefficients to the computer.
14. An imaging device as claimed in claim 1 in which the optical section includes a lens for directing the image light from the image upon the color sensor, said lens being removable from the imaging device and having a predetermined reference lens spectral characteristic, and wherein the matrix coefficients correct the reference lens spectral characteristic for the color sensitivities of the output device.
15. An imaging device as claimed in claim 1 in which the output device is represented by a connection space, and said matrix coefficients are part of a device profile for connecting the spectral sensitivities of the color sensor and the spectral characteristics of the optical section for the color sensitivities of the connection space.
16. A digital camera for capturing an image and generating a color signal from the image for input to an intended display device having specific color sensitivities, said camera further being one of many cameras of the same type useful with the display device, said camera comprising:
a color sensor for capturing the image and generating the color signal from the captured image, said color sensor having predetermined spectral sensitivities defining the color response of the color sensor;
a lens for directing image light from the image upon the color sensor, said lens having a predetermined lens spectral characteristic;
an infrared cutoff filter having a predetermined infrared spectral characteristic for filtering the image light directed upon the color sensor;
the combination of said spectral sensitivities of the color sensor and the spectral characteristics of the lens and the infrared cutoff filter uniquely distinguishing the digital camera from other digital cameras of the same type; and
a matrix storage containing a set of matrix coefficients uniquely determined for the camera in order to generate an optimized color signal, wherein said matrix coefficients are (a) automatically calculated by a matrix coefficient calculation from image data obtained by the color sensor from a color chart and (b) used for correcting the spectral sensitivities of the color sensor and the spectral characteristics of the lens and the infrared cutoff filter for the color sensitivities of the intended display device.
17. A digital camera as claimed in claim 16 further comprising a blur filter having a predetermined low pass spatial characteristic for low pass filtering the image light directed upon the color sensor, and wherein the matrix coefficients further correct the spectral characteristic of the blur filter for the color sensitivities of the intended display device.
18. A digital camera as claimed in claim 16 wherein the color sensor includes a color filter array for color filtering the image light directed upon the color sensor, said color filter array having a predetermined color filter spectral characteristics, and wherein the matrix coefficients correct the spectral characteristic of the color filter array for the color sensitivities of the intended display device.
19. A digital camera as claimed in claim 16 further comprising a color processing section for implementing a matrix correction of the color signal in order to generate the optimized color signal, said color processing section using the set of matrix coefficients in the matrix storage that are uniquely determined for this digital camera in order to generate the optimized color signal.
20. An electronic imaging system including a computer useful with a digital camera as claimed in claim 16, wherein the computer comprises a color processing section for implementing a matrix correction on the color signal using the set of matrix coefficients in the matrix storage in order to generate the optimized color signal, and the digital camera provides the color signal together with the matrix coefficients to the computer.
21. A digital camera for capturing an image and generating an optimized color signal from the image for input to an intended display device having specific color sensitivities, said camera further being one of many cameras of the same type useful with the display device, said camera comprising:
a color sensor comprising a color filter array and a photosensor for capturing the image and generating a color signal from the captured image, said color sensor having predetermined spectral sensitivities defining the color response of a specific color sensor employed in the digital camera;
an optical section including at least a lens for directing image light from the image upon the color sensor and an infrared cutoff filter for filtering the image light directed upon the color sensor, said optical section having optical spectral characteristics comprised of a specific lens spectral characteristic which together define the optical response of a specific optical section employed in the digital camera;
the combination of said spectral sensitivities of the color sensor and the spectral characteristics of the optical section uniquely distinguishing the digital camera from other digital cameras of the same type;
a memory containing matrix coefficients uniquely determined by a matrix coefficient calculation for use by the camera in order to generate the optimized color signal, wherein said matrix coefficients are (a) automatically computed from image data obtained by the color sensor from a color chart and (b) used for correcting the spectral sensitivities of the color sensor and the spectral characteristics of the optical section for the color sensitivities of the intended display device; and
a color processing section for implementing a matrix correction on the color signal using the matrix coefficients in the memory in order to generate the optimized color signal.
22. A digital camera as claimed in claim 21 wherein said optical section further includes a blur filter for spatially low pass filtering the image light directed upon the color sensor, said blur filter having a predetermined spectral characteristic, and wherein the matrix coefficients further correct the spectral characteristic of the blur filter for the color sensitivities of the intended display device.
23. A digital camera for capturing an image and generating a color signal from the image for input through an external processor to an intended display device having specific color sensitivities, said external processor including a color processing section for implementing a matrix correction on the color signal in order to generate an optimized color signal, said camera further being one of many cameras of the same type useful with the display device, said camera comprising:
a color sensor comprising a color filter array and a photosensor for capturing the image and generating the color signal from the captured image, said color sensor having predetermined spectral sensitivities defining the color response of the sensor;
an optical section including at least a lens for directing image light from the image upon the color sensor and an infrared cutoff filter for filtering the image light directed upon the color sensor, said optical section having optical spectral characteristics comprised of a specific lens spectral characteristic which together define the optical response of a specific optical section employed in the digital camera;
the combination of said spectral sensitivities of the color sensor and the spectral characteristics of the optical section uniquely distinguishing the digital camera from other digital cameras of the same type;
a memory containing matrix coefficients uniquely determined for the camera in order to generate the optimized color signal, wherein said matrix coefficients are (a) automatically calculated by a matrix coefficient calculation from image data obtained by the color sensor from a color chart and (b) used for correcting the spectral sensitivities of the color sensor and the spectral characteristics of the optical section for the color sensitivities of the intended display device; and
means for providing the color signal and the matrix coefficients to the external processor.
24. A digital camera as claimed in claim 23 wherein said optical section further includes a blur filter for spatially low pass filtering the image light directed upon the color sensor, said blur filter having a predetermined spectral characteristic controlling the response of the optical section, and wherein the matrix coefficients further correct the spectral characteristics of the filter for the color sensitivities of the intended display device.
25. A digital camera for capturing an image and generating a color signal from the captured image, said camera comprising:
a main assembly for housing the camera; and
a removable subassembly including a color sensor having specific color sensitivities for capturing the image and generating the color signal, an optical section including at least a lens and an infrared filter having respective lens and cutoff spectral characteristics, and a memory device containing matrix coefficients for color correcting the spectral sensitivities of the color sensor and the spectral characteristics of the optical section for the color sensitivities of the display device;
a signal processing section for processing the color signal generated by the color sensor;
electrical connecting means for replaceably interconnecting the signal processing section and the subassembly; and
a color processing section for implementing a matrix correction on the color signal using the matrix coefficients in the memory device in order to generate an optimized color signal.
26. A digital camera for capturing an image and outputting a color image signal to an external processor, said external processor including a color processing section for implementing a matrix correction on the color image signal in order to generate an optimized color signal from the captured image, said camera comprising:
a main assembly for housing the camera;
a removable subassembly including a color sensor having specific color sensitivities for capturing the image and generating a color signal, an optical section including at least a lens and an infrared filter having respective lens and cutoff spectral characteristics, and a memory device containing matrix coefficients for color correcting the spectral sensitivities of the color sensor and the spectral characteristics of the optical section for the color sensitivities of the display device;
a signal processing section for processing the color signal generated by the color sensor;
electrical connecting means for replaceably interconnecting the signal processing section and the subassembly; and
means for providing the color image signal and the matrix coefficients to the external processor.
27. A digital camera for capturing an image and generating a color signal from the image for input through an external processor operative in a connection space having specific color sensitivities defined by a set of color matching functions, said external processor including a color processing section for implementing a matrix correction on the color signal in order to generate an optimized color signal, said camera further being one of many cameras of the same type, said camera comprising:
a color sensor comprising a color filter array and a photosensor for capturing the image and generating the color signal from the captured image, said color sensor having predetermined spectral sensitivities defining the color response of the sensor;
an optical section including at least a lens for directing image light from the image upon the color sensor and an infrared cutoff filter for filtering the image light directed upon the color sensor, aid optical section having optical spectral characteristics comprised of a specific lens spectral characteristics which together define the optical response of a specific optical section employed in the digital camera;
the combination of said spectral sensitivities of the color sensor and the spectral characteristics of the optical section uniquely distinguishing the digital camera from other digital cameras of the same type;
a memory containing matrix coefficients uniquely determined for the camera in order to generate the optimized color signal, wherein said matrix coefficients being are (a) automatically calculated by a matrix coefficient calculation from image data obtained by the color sensor from a color chart and (b) used as part of a device profile for correcting the spectral sensitivities of the color sensor and the spectral characteristics of the optical section for the color sensitivities of the connection space; and
means for providing the color signal and the matrix coefficients to the external processor.
28. A digital camera as claimed in claim 27 wherein said optical section further includes a blur filter for spatially low pass filtering the image light directed upon the color sensor, said blur filter having a predetermined spectral characteristic controlling the response of the optical section, and wherein the matrix coefficients further correct the spectral characteristic of the blur filter for the color sensitivities of the connection space.
29. An imaging device as claimed in claim 1 wherein the matrix coefficient calculation comprises processing blocks for (a) measuring spectral characteristics of colors of the color chart as illuminated by an illuminant and computing colorimetric values for each colorilluminant combination from the measured spectral characteristics, thereby obtaining a set of colorimetric aims for the imaging device, (b) capturing an image of the color chart by using the color sensor, thereby obtaining color image data representative of the image of the color chart, (c) processing the color image data in a color-correction matrix comprising a set of adjustable, color-correction coefficients and generating reproduction signals for the colors of the color chart, and (d) iteratively adjusting the adjustable, color-correction coefficients until the error between the reproduction signals and the colorimetric aims is reduced to a predetermined level.
30. A digital camera as claimed in claim 16 wherein the matrix coefficient calculation comprises processing blocks for (a) measuring spectral characteristics of colors of the color chart as illuminated by an illuminant and computing colorimetric values for each colorilluminant combination from the measured spectral characteristics, thereby obtaining a set of colorimetric aims for the imaging device, (b) capturing an image of the color chart by using the color sensor, thereby obtaining color image data representative of the image of the color chart, (c) processing the color image data in a color-correction matrix comprising a set of adjustable, color-correction coefficients and generating reproduction signals for the colors of the color chart, and (d) iteratively adjusting the adjustable, color-correction coefficients until the error between the reproduction signals and the colorimetric aims is reduced to a predetermined level.
31. A digital camera as claimed in claim 21 wherein the matrix coefficient calculation comprises processing blocks for (a) measuring spectral characteristics of colors of the color chart as illuminated by an illuminant and computing colorimetric values for each colorilluminant combination from the measured spectral characteristics, thereby obtaining a set of colorimetric aims for the imaging device, (b) capturing an image of the color chart by using the color sensor, thereby obtaining color image data representative of the image of the color chart, (c) processing the color image data in a color-correction matrix comprising a set of adjustable, color-correction coefficients and generating reproduction signals for the colors of the color chart, and (d) iteratively adjusting the adjustable, color-correction coefficients until the error between the reproduction signals and the colorimetric aims is reduced to a predetermined level.
32. A digital camera as claimed in claim 23 wherein the matrix coefficient calculation comprises processing blocks for (a) measuring spectral characteristics of colors of the color chart as illuminated by an illuminant and computing colorimetric values for each colorilluminant combination from the measured spectral characteristics, thereby obtaining a set of colorimetric aims for the imaging device, (b) capturing an image of the color chart by using the color sensor, thereby obtaining color image data representative of the image of the color chart, (c) processing the color image data in a color-correction matrix comprising a set of adjustable, color-correction coefficients and generating reproduction signals for the colors of the color chart, and (d) iteratively adjusting the adjustable, color-correction coefficients until the error between the reproduction signals and the colorimetric aims is reduced to a predetermined level.
33. A digital camera as claimed in claim 27 wherein the matrix coefficient calculation comprises processing blocks for (a) measuring spectral characteristics of colors of the color chart as illuminated by an illuminant and computing colorimetric values for each color-illuminant combination from the measured spectral characteristics, thereby obtaining a set of colorimetric aims for the imaging device, (b) capturing an image of the color chart by using the color sensor, thereby obtaining color image data representative of the image of the color chart, (c) processing the color image data in a color-correction matrix comprising a set of adjustable, color-correction coefficients and generating reproduction signals for the colors of the color chart, and (d) iteratively adjusting the adjustable, color-correction coefficients until the error between the reproduction signals and the colorimetric aims is reduced to a predetermined level.