1. A compound of Formula Ib:
or stereoisomer, tautomer, or pharmaceutically acceptable salt thereof, wherein:
R1 is selected from hydrogen, methyl, isobutyl, tert-butyl, cyclohexyl, cyclopentyl, phenyl and phenyl substituted with one to three substituents selected from the group consisting on methyl, ethyl and propyl;
R2 is selected from H and C1-C8 alkyl;
R3 is selected from hydrogen, methyl, isopropyl, n-propyl, isobutyl, sec-butyl, n-butyl, \u2014CH2OH and \u2014CH(OH)CH3,
R4 and R5 are independently selected from H and C1-C8 alkyl;
each alkyl is optionally and independently substituted with one or more substituents selected from F, Cl, Br, I, OH, OR, R, \u2550O, \u2550S, \u2550NR, \u2550N+(O)(R), \u2550N(OR), \u2550N+(O)(OR), \u2550N-N(R)2, \u2014C(\u2550Y)R, \u2014C(\u2550Y)OR, \u2014C(\u2550Y)N(R)2, \u2014N(R)2, \u2014N+(R)3, \u2014N(R)C(\u2550Y)R, \u2014N(R)C(\u2550Y)OR, \u2014N(R)C(\u2550Y)N(R)2, \u2014SR, \u2014OC(\u2550Y)R, \u2014OC(\u2550Y)OR, \u2014OC(\u2550Y)(N(R)2), \u2014OS(O)2(OR), \u2014OP(\u2550Y)(OR)2, \u2014OP(OR)2, \u2014P(\u2550Y)(OR)2, \u2014P(\u2550Y)(OR)NR2, \u2014S(O)R, \u2014S(O)2R, \u2014S(O)2NR, \u2014S(O)(OR), \u2014S(O)2(OR), \u2014SC(\u2550Y)R, \u2014SC(\u2550Y)OR, and \u2014SC(\u2550Y)NR2;
R is independently H, C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, C6-C20 aryl, C1-C20 heterocyclyl, or a protecting group selected from a trialkylsilyl, a dialkylphenylsilyl, benzoate, benzyl, benzyloxymethyl, methyl, methoxymethyl, a triarylmethyl, phthalimido and tetrahydropyranyl; and
Y is independently O, S, NR, N+(O)(R), N(OR), N+(O)(OR), or N-N(R)2.
2. A compound of formula:
or stereoisomer, tautomer, or pharmaceutically acceptable salt thereof, wherein:
Z is
R1 is selected from hydrogen, methyl, isobutyl, tert-butyl, cyclohexyl, cyclopentyl, phenyl and phenyl substituted with one to three substituents selected from the group consisting on methyl, ethyl and propyl;
each R2 is selected from H and C1-C8 alkyl;
R3 is selected from hydrogen, methyl, isopropyl, n-propyl, isobutyl, sec-butyl, n-butyl, \u2014CH2OH and \u2014CH(OH)CH3;
R4 and R5 are independently selected from H and C1-C8 alkyl;
each alkyl is optionally and independently substituted with one or more substituents selected from F, Cl, Br, I, OH, OR, R, \u2550O, \u2550S, \u2550NR, \u2550N+(O)(R), \u2550N(OR), \u2550N+(O)(OR), \u2550N-N(R)2, \u2014C(\u2550Y)R, \u2014C(\u2550Y)OR, \u2014C(\u2550Y)N(R)2, \u2014N(R)2, \u2014N+(R)3, \u2014N(R)C(\u2550Y)R, \u2014N(R)C(\u2550Y)OR, \u2014N(R)C(\u2550Y)N(R)2, \u2014SR, \u2014OC(\u2550Y)R, \u2014OC(\u2550Y)OR, \u2014OC(\u2550Y)(N(R)2), \u2014OS(O)2(OR), \u2014OP(\u2550Y)(OR)2, \u2014OP(OR)2, \u2014P(\u2550Y)(OR)2, \u2014P(\u2550Y)(OR)NR2, \u2014S(O)R, \u2014S(O)2R, \u2014S(O)2NR, \u2014S(O)(OR), \u2014S(O)2(OR), \u2014SC(\u2550Y)R, \u2014SC(\u2550Y)OR, and \u2014SC(\u2550Y)NR2;
R is independently H, C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, C6-C20 aryl, C1-C20 heterocyclyl, or a protecting group selected from a trialkylsilyl, a dialkylphenylsilyl, benzoate, benzyl, benzyloxymethyl, methyl, methoxymethyl, a triarylmethyl, phthalimido and tetrahydropyranyl;
Y is independently O, S, NR, N+(O)(R), N(OR), N+(O)(OR), or N-N(R)2; and
n is 1, 2, 3, 4, 5, 6, 7, or 8.
3. The compound of claim 1 wherein R2 is H.
4. The compound of claim 1 wherein R2 is methyl.
5. The compound of claim 1 wherein R3 is hydrogen.
6. The compound of claim 1 wherein R4 and R5 are each hydrogen.
7. The compound of claim 1 wherein the carbon atom bearing R3 is in the R configuration.
8. The compound of claim 1 wherein the carbon atom bearing R3 is in the S configuration.
9. The compound of claim 1 wherein the carbon atom bearing the boron atom is in the R configuration.
10. The compound of claim 1 wherein the carbon atom bearing the boron atom is in the S configuration.
11. The compound of claim 1 wherein R is a protecting group selected from a trialkylsilyl, a dialkylphenylsilyl, benzoate, benzyl, benzyloxymethyl, methyl, methoxymethyl, a triarylmethyl, phthalimido and tetrahydropyranyl.
12. A compound selected from the structures:
13. A compound selected from the structures:
14. A compound selected from the structures:
15. A compound of the structure:
16. The compound of claim 2 wherein R2 is H.
17. The compound of claim 2 wherein at least one of R2 is methyl.
18. The compound of claim 2 wherein R4 and R5 are each H.
19. A compound selected from the structures:
20. A composition comprising the compound according to claim 1 or claim 2 in an amount to inhibit FAP activity in vitro, and a pharmaceutically acceptable carrier, adjuvant, or vehicle.
21. A composition comprising the compound according to claim 1 or claim 2 in an amount to inhibit POP activity in vitro, and a pharmaceutically acceptable carrier, adjuvant, or vehicle.
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 brushless motor drive circuit driving a three-phase brushless motor with sine wave signals, the brushless motor drive circuit comprising:
a first AD converter which converts a voltage value depending upon a power supply voltage supplied from a power supply to drive a three-phase brushless motor, to a digital signal and outputs the digital signal;
an energization timing adjustment circuit which outputs an adjustment signal for adjusting a lead angle value or a lag angle value of energization timing of the three-phase brushless motor, in response to the digital signal which is output by the first AD converter; and
an energization timing setting circuit which sets the energization timing of the three-phase brushless motor,
wherein if a regenerated voltage is generated by decelerating the three-phase brushless motor with sine wave signals and the power supply voltage rises, then the energization timing setting circuit sets energization timing changed by the lead angle value or the lag angle value on the basis of the adjustment signal to further decelerate the three-phase brushless motor,
wherein if the power supply voltage is at least a preset threshold, then the first AD converter outputs a digital signal, and
wherein if the power supply voltage is at least a first threshold, then the first AD converter outputs a first digital signal corresponding to a first lead angle value or a first lag angle value, and
if the power supply voltage is at least a second threshold which is higher than the first threshold, then the first AD converter outputs a second digital signal corresponding to a second lead angle value which leads the first lead angle value or a second lag angle value which lags behind the first lag angle value.
2. The brushless motor drive circuit according to claim 1, wherein the thresholds of the first AD converter can be changed.
3. The brushless motor drive circuit according to claim 1, further comprising:
a power supply voltage detection comparator which is adapted to output an overvoltage signal if the power supply voltage is at least an overvoltage, the overvoltage being set to be higher than the threshold; and
an energization control circuit which outputs the control signal to intercept the three-phase brushless motor from the power supply in response to the overvoltage signal.
4. The brushless motor drive circuit according to claim 3, wherein the energization control circuit outputs the control signal to ground all coils included in the three-phase brushless motor in response to the overvoltage signal.
5. The brushless motor drive circuit according to claim 1, wherein the voltage value is a divided voltage obtained by dividing the power supply voltage.
6. The brushless motor drive circuit according to claim 1, further comprising:
an energization timing detection circuit which detects a current flowing through the power device and outputs a detected signal depending upon a magnitude of the detected current; and
a second AD converter which converts the detected signal to a digital signal and output the digital signal,
wherein the energization timing adjustment circuit outputs an adjustment signal for adjusting the lead angle value or the lag angle value of energization timing of the three-phase brushless motor, in response to the digital signal output by the first AD converter and the digital signal output by the second AD converter.
7. The brushless motor drive circuit according to claim 6, wherein the energization timing adjustment circuit adds up the digital signal output by the first AD converter and the digital signal output by the second AD converter, and outputs an obtained result as the adjustment signal.
8. The brushless motor drive circuit according to claim 7, wherein the energization timing adjustment circuit is an adder, the adder adding up the digital signal output by the first AD converter and the digital signal output by the second AD converter, and outputting an obtained result as the adjustment signal.
9. The brushless motor drive circuit according to claim 1, further comprising
an output waveform generation circuit which outputs drive signals for driving the three-phase brushless motor on the basis of the energization timing set by the energization timing setting circuit.
10. A brushless motor drive system comprising:
a three-phase brushless motor;
a power supply which generates a power supply voltage;
a power device which supplies the power supply voltage to the three-phase brushless motor with three-phase sine wave signals; and
a brushless motor drive circuit which controls the power device,
wherein the brushless motor drive circuit comprising:
a first AD converter which converts a voltage value depending upon a power supply voltage supplied from a power supply to drive a three-phase brushless motor, to a digital signal and outputs the digital signal;
an energization timing adjustment circuit which outputs an adjustment signal for adjusting a lead angle value or a lag angle value of energization timing of the three-phase brushless motor, in response to the digital signal which is output by the first AD converter; and
an energization timing setting circuit which sets the energization timing of the three-phase brushless motor,
wherein if a regenerated voltage is generated by decelerating the three-phase brushless motor with sine wave signals and the power supply voltage rises, then the energization timing setting circuit sets energization timing changed by the lead angle value or the lag angle value on the basis of the adjustment signal to further decelerate the three-phase brushless motor,
wherein if the power supply voltage is at least a preset threshold, then the first AD converter outputs a digital signal, and
wherein if the power supply voltage is at least a first threshold, then the first AD converter outputs a first digital signal corresponding to a first lead angle value or a first lag angle value, and
if the power supply voltage is at least a second threshold which is higher than the first threshold, then the first AD converter outputs a second digital signal corresponding to a second lead angle value which leads the first lead angle value or a second lag angle value which lags behind the first lag angle value.
11. The brushless motor drive system according to claim 10, wherein the thresholds of the first AD converter can be changed.
12. The brushless motor drive system according to claim 10, further comprising:
a power supply voltage detection comparator which is adapted to output an overvoltage signal if the power supply voltage is at least an overvoltage, the overvoltage being set to be higher than the threshold; and
an energization control circuit which outputs the control signal to intercept the three-phase brushless motor from the power supply in response to the overvoltage signal.
13. The brushless motor drive system according to claim 12, wherein the energization control circuit outputs the control signal to ground all coils included in the three-phase brushless motor in response to the overvoltage signal.
14. The brushless motor drive system according to claim 10, wherein the voltage value is a divided voltage obtained by dividing the power supply voltage.
15. The brushless motor drive system according to claim 10, further comprising:
an energization timing detection circuit which detects a current flowing through the power device and outputs a detected signal depending upon a magnitude of the detected current; and
a second AD converter which converts the detected signal to a digital signal and output the digital signal,
wherein the energization timing adjustment circuit outputs an adjustment signal for adjusting the lead angle value or the lag angle value of energization timing of the three-phase brushless motor, in response to the digital signal output by the first AD converter and the digital signal output by the second AD converter.
16. The brushless motor drive system according to claim 15, wherein the energization timing adjustment circuit adds up the digital signal output by the first AD converter and the digital signal output by the second AD converter, and outputs an obtained result as the adjustment signal.