1. A compound of the general formula I:
196
wherein
X1 is bond or OCH2,
197
(in which R2 is hydrogen or lower alkyl and n is an integer of 1 or 2)
(in which R3 is hydrogen or lower alkyl),
198
(in which R4 is hydrogen or lower
199
CH2CH2, CHCH or
(in which Y2 is lower alkylene),
R1 is hydrogen or an amino protective group,
A is phenyl, indolyl or carbazolyl, each of which may be substituted with one or two substituent(s) selected from the group consisting of halogen, hydroxy, hydroxy(lower)alkyl and benzyloxy, and
B is hydrogen; halogen; lower alkyl; lower alkoxycarbonyl; cyclo(lower)alkyl; or a heterocyclic group, naphthyl, 1,2,3,4-tetrahydronaphthyl, benzyl or phenyl, each of which may be substituted with one or two substituent(s) selected from the group consisting of halogen, lower alkoxy, mono(or di or tri)halo(lower)alkoxy, carboxy(lower)alkoxy, lower alkoxycarbonyl(lower)alkoxy, phenoxy, lower alkyl, mono(or di or tri)halo(lower)alkyl, cyano, carboxy, lower alkoxycarbonyl, lower alkanoyl, benzoyl, mono(or di)(lower)alkylcarbamoyl, (lower alkylsulfonyl)carbamoyl, (lower alkylsulfonyl)-amino, (lower alkoxycarbonyl)amino, amino, nitro, pyridyl, triazolyl, thiazolyl optionally substituted with phenyl or lower alkyl, and phenyl optionally substituted with mono(or di or tri)halo(lower)alkyl,
or a salt thereof.
2. A compound of claim 1, wherein
X1 is bond or OCH2,
200
(in which R2 is hydrogen or lower alkyl and n is an integer of 1 or 2)
in which
201
(in which R3 is hydrogen or lower alkyl),
202
(in which R4 is hydrogen or lower
203
CH2CH2, CHCH or
(in which Y2 is lower alkylene),
R1 is hydrogen,
A is phenyl which may be substituted with one or two substituent(s) selected from the group consisting of halogen, hydroxy, hydroxy(lower)alkyl and benzyloxy,
B is pyrrolyl, imidazolyl, pyrazolyl, pyridyl, pyrazinyl, piperidyl, indolyl, benzimidazolyl, quinolyl, isoquinolyl, quinoxalinyl, cinnolinyl, indazolyl, oxazolyl, isoxazolyl, thiazolyl, thienyl, furyl, benzofuranyl, benzothienyl, naphthyl, benzyl or phenyl, each of which may be substituted with one or two substituent(s) selected from the group consisting of halogen, lower alkoxy, mono(or di or tri)halo(lower)alkoxy, carboxy(lower)alkoxy, lower alkoxycarbonyl-(lower)alkoxy, phenoxy, lower alkyl, mono(or di or tri)halo(lower)alkyl, cyano, carboxy, lower alkoxycarbonyl, lower alkanoyl, benzoyl, mono(or di)(lower)alkylcarbamoyl, (lower alkylsulfonyl)-carbamoyl, (lower alkylsulfonyl)amino, (lower alkoxycarbonyl)amino, amino, nitro, pyridyl, triazolyl, thiazolyl optionally substituted with phenyl or lower alkyl, and phenyl optionally substituted with mono(or di or tri)halo(lower)alkyl.
3. A compound of claim 2, wherein
X1 is OCH2,
204
(in which R2 is hydrogen and n is an integer of 1) or
R1 is hydrogen,
A is phenyl which may be substituted with one or two substituent(s) selected from the group consisting of halogen, hydroxy, hydroxy(lower)alkyl and benzyloxy,
B is pyrrolyl, pyridyl, naphthyl or phenyl, each of which may be substituted with one or two substituent(s) selected from the group consisting of halogen, lower alkoxy, carboxy(lower)alkoxy, lower alkoxycarbonyl(lower)alkoxy, lower alkyl, mono(or di or tri)halo(lower)alkyl, cyano, carboxy, lower alkoxycarbonyl, lower alkanoyl, mono(or di)(lower)alkylcarbamoyl, (lower alkylsulfonyl)carbamoyl, (lower alkylsulfonyl) amino, (lower alkoxycarbonyl) amino and nitro.
4. A compound of claim 3, which is
(1) N-4-(2S)-3-hydroxy-2-(2S)-2-hydroxy-3-phenoxypropylaminopropylphenyl-1H-pyrrole-2-carboxamide;
(2) N-4-(2S)-3-hydroxy-2-(2S)-2-hydroxy-3-phenoxypropylaminopropylphenyl-N-phenylurea;
(3) N-4-(2S)-3-hydroxy-2-(2S)-2-hydroxy-3-phenoxypropylaminopropylphenyl-1-naphthamide;
(4) N-(3-fluorophenyl)-N-4-(2S)-3-hydroxy-2-(2S)-2-hydroxy-3-phenoxypropylaminopropylphenylurea;
(5) N-4-(2S)-3-hydroxy-2-(2S)-2-hydroxy-3-phenoxypropylaminopropylphenyl-N-(3-methoxyphenyl)urea,
or a salt thereof.
5. A process for preparing a compound of claim 1,
or a salt thereof, which comprises,
(i) reacting a compound II of the formula:
205
wherein X1 and A are each as defined in claim 1, or a salt thereof, with a compound III of the formula:
206
wherein X2, R1 and B are each as defined in claim 1, or a salt thereof, to give a compound I of the formula:
207
wherein X1, X2, R1, A and B are each as defined in claim 1,
or a salt thereof, or
(ii) subjecting a compound Ia of the formula:
208
wherein X1, X2, A and B are each as defined in claim 1, and Ra1 is an amino protective group, or a salt thereof, to elimination reaction of the amino protective group, to give a compound Ib of the formula:
209
wherein X1, X2, A and B are each as defined in claim 1, or a salt thereof, or
(iii) reacting a compound IV of the formula:
210
wherein X1, R1 and A are each as defined in claim 1, or a salt thereof, with a compound V of the formula:
211
wherein B is as defined in claim 1, and W1 is a leaving group,
or a salt thereof, to give a compound Ic of the formula:
212
wherein X1, R1, A and B are each as defined in claim 1, or a salt thereof, or
(iv) reacting a compound Id of the formula:
213
wherein X1, R1, A and B are each as defined in claim 1, and
m is an integer of 1 or 2,
or a salt thereof, with a compound VI of the formula:
W2R2VI
wherein Ra2 is lower alkyl, and W2 is an acid residue,
to give a compound Ie of the formula:
214
wherein X1, R1, A and B are each as defined in claim 1,
Ra2 is lower alkyl, and
m is an integer of 1 or 2,
or a salt thereof, and
(v) reacting a compound IV of the formula:
215
wherein X1, R1 and A are each as defined in claim 1, or a salt thereof, with a compound VII of the formula:
216
wherein B is as defined in claim 1, and
k is 0 or an integer of 1,
or a salt thereof, to give a compound If of the formula:
217
wherein X1, R1, A and B are each as defined in claim 1, and
k is 0 or an integer of 1, or a salt thereof.
6. A pharmaceutical composition which comprises, as an active ingredient, a compound of claim 1 or a pharmaceutically acceptable salt thereof in admixture with pharmaceutically acceptable carriers or excipients.
7. Use of a compound of claim 1 or a pharmaceutically acceptable salt thereof for the manufacture of a medicament.
8. A compound of claim 1 or a pharmaceutically acceptable salt thereof for use as a medicament.
9. A method for the prophylactic andor therapeutic treatment of pollakiuria, urinary incontinence, obesity or diabetes, which comprises administering a compound of claim 1 or a pharmaceutically acceptable salt thereof to a human being or an animal.
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 processing apparatus, comprising:
circuitry configured to
cause an aperture diaphragm to move from a starting position toward first and second diaphragm positions of the aperture diaphragm such that the aperture diaphragm reaches the first diaphragm position at the beginning of an exposure period, and
cause the aperture diaphragm to move from the first diaphragm position to the second diaphragm position during the exposure period.
2. The image processing apparatus according to claim 1, wherein the first diaphragm position is predetermined.
3. The image processing apparatus according to claim 1, wherein the circuitry is further configured to
cause the aperture diaphragm to move to the starting position before causing the aperture diaphragm to move from the starting position.
4. The image processing apparatus according to claim 3, wherein the circuitry is configured to
cause the aperture diaphragm to move to the starting position and away from the second diaphragm position.
5. The image processing apparatus according to claim 1, wherein the circuitry is further configured to
determine which of the first diaphragm position and the second diaphragm position an initial position of the aperture diaphragm is closest to, and
determine the starting position based on the determination of which of the first diaphragm position and the second diaphragm position is closest to the initial position.
6. The image processing apparatus according to claim 5, wherein the initial position is between the first and second diaphragm positions.
7. The image processing apparatus according to claim 1, wherein the circuitry is configured to
cause the aperture diaphragm to continuously move from the starting position to the first diaphragm position and the second diaphragm position without interruption.
8. The image processing apparatus according to claim 1, wherein the aperture diaphragm moves from the starting position to the first diaphragm position at a first speed and from the first diaphragm position to the second diaphragm position at a second speed, which is different from the first speed.
9. The image processing apparatus according to claim 8, wherein the second speed is greater than the first speed.
10. The image processing apparatus according to claim 1, wherein the aperture diaphragm moves in a closing direction from the starting position toward the first and second diaphragm positions.
11. The image processing apparatus according to claim 1, wherein the aperture diaphragm moves in an opening direction from the starting position toward the first and second diaphragm positions.
12. The image processing apparatus according to claim 1, wherein the circuitry is further configured to determine the exposure period for capturing an image.
13. The image processing apparatus according to claim 1, wherein the exposure period is used to capture an image.
14. An image processing system, comprising:
circuitry configured to
cause an aperture diaphragm to move from a starting position toward first and second diaphragm positions of the aperture diaphragm such that the aperture diaphragm reaches the first diaphragm position at the beginning of an exposure period, and
cause the aperture diaphragm to move from the first diaphragm position to the second diaphragm position during the exposure period.
15. A method of an image processing apparatus for image capture, the method comprising:
causing, by circuitry of the image processing apparatus, an aperture diaphragm to move from a starting position toward first and second diaphragm positions of the aperture diaphragm such that the aperture diaphragm reaches the first diaphragm position at the beginning of an exposure period; and
causing, by the circuitry, the aperture diaphragm to move from the first diaphragm position to the second diaphragm position during the exposure period.
16. A lens, comprising:
circuitry configured to
cause an aperture diaphragm to move from a starting position toward first and second diaphragm positions of the aperture diaphragm such that the aperture diaphragm reaches the first diaphragm position at the beginning of an exposure period, and
cause the aperture diaphragm to move from the first diaphragm position to the second diaphragm position during the exposure period.