What is claimed is:
1. A compound having the formula
5
wherein:
R1 is alkyl, cycloalkyl, heterocycloalkyl, alkylcycloalkyl, alkylheterocycloalkyl, aryl or heteroaryl; provided that the point of attachment is a carbon atoms;
R2is hydrogen, alkyl or (CH2)R5;
R3 is hydrogen or alkyl;
X is hydrogen, halogen, perhaloalkyl, hydroxy, alkoxy, or perhaloalkoxy;
R4 is aryl or heteroaryl;
R5 is alkyl, alkenyl or alkynyl;
n is an integer from 1 to 3; and
the dotted line is an optional double bond; or a pharmaceutical salt thereof.
2. A compound of claim 1 wherein R1 is cycloalkyl of 3 to 8 carbon atoms.
3. A compound of claim 2 wherein said cycloalkyl is substituted with an alkyl of 1 to 6 carbon atoms.
4. A compound of claim 1 wherein X is 4-fluoro- or 5-fluoro-.
5. A compound of claim 1 wherein R4 is phenyl or pyridyl.
6. A compound of claim 5 wherein R4 is phenyl, pyrid-3yl or pyrid-4yl.
7. A compound of claim 1 which is 1-methyl-cyclohexanecarboxylic acid (1R)-1-benzyl-2-4-(5-fluoro-2-methoxy-phenyl)-piperidin-1-yl-ethyl-methyl-amide, or a pharmaceutical salt thereof.
8. A compound of claim 1 which is 1-methyl-cyclohexanecarboxylic acid (1 R)-1-benzyl-2-4-(5-fluoro-2-methoxy-phenyl)-1,2,5,6-tetrahydro-4H-pyridin-1-yl-ethyl-methyl-amide, or a pharmaceutical salt thereof.
9. A compound of claim 1 which is (R)-Cyclohexanecarboxylic acid1-benzyl-2-4-(2-methoxy-phenyl)-3,6-dihydro-2H-pyridin-1-yl-ethyl-amide, or a pharmaceutical salt thereof.
10. A compound of claim 1 which is (R)-1-Methyl-cyclohexanecarboxylic acid1-benzyl-2-4-(2-methoxy-phenyl)-3,6-dihydro-2H-pyridin-1-yl-ethyl-amide, or a pharmaceutical salt thereof
11. A compound of claim 1 which is (R)-1-Methyl-cyclohexanecarboxylic acid 1-benzyl-2-4-(2-methoxy-phenyl)-piperidin-1-yl-ethyl-amide, or a pharmaceutical salt thereof
12. A compound of claim 1 which is (R)-Cyclohexanecarboxylic acid1-benzyl-2-4-(2-methoxy-phenyl)-piperidin-1-yl-ethyl-amide, or a pharmaceutical salt thereof.
13. A compound of claim 1 which is 1-Methyl-cyclohexanecarboxylic acid(1R)-2-4-(2-methoxy-phenyl)-piperidin-1-yl-1-pyridin-3-ylmethyl-ethyl-amide, or a pharma-ceutical salt thereof.
14. A compound of claim 1 which is 1-Methyl-cyclohexanecarboxylic acid(1R)-2-4-(2-methoxy-phenyl)-piperidin-1-yl-1-pyridin-4-ylmethyl-ethyl-amide, or a pharma-ceutical salt thereof.
15. A compound of claim 1 which is Cyclohexanecarboxylic acid(1R)-2-4-(2-methoxy-phenyl)-piperidin-1-yl-1-pyridin-3-ylmethyl-ethyl-methyl-amide, or a pharmaceutical salt thereof.
16. A compound of claim 1 which is Cyclohexanecarboxylic acid(1R)-2-4-(2-methoxy-phenyl)-piperidin-1-yl-1-pyridin-4-ylmethyl-ethyl-methyl-amide, or a pharmaceutical salt thereof.
17. A compound of claim 1 which is (R)-Cyclohexanecarboxylic acid1-(4-methoxybenzyl)-2-4-(2-methoxy-phenyl)-piperidin-1-yl-ethyl-amide, or a pharmaceutical salt thereof.
18. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.
19. A method of treating a patient suffering from a disorder of the central nervous system associated with the 5-hydroxytryptamine 1A receptor subtype comprising administering a therapeutically effective amount of a compound having the formula
6
wherein:
R1 is alkyl, cycloalkyl, heterocycloalkyl, alkylcycloalkyl, alkylheterocycloalkyl, aryl or heteroaryl; provided that the point of attachment is a carbon atoms;
R2 is hydrogen, alkyl or (CH2)R5;
R3 is hydrogen or alkyl;
X is hydrogen, halogen, perhaloalkyl, hydroxy, alkoxy, or perhaloalkoxy;
R4 is aryl or heteroaryl;
R5 is alkyl, alkenyl or alkynyl;
n is an integer from 1 to 3; and
the dotted line is an optional double bond; or a pharmaceutical salt thereof.
20. The method of claim 19 wherein the disorder is depression, anxiety or panic.
21. The method of claim 19 wherein the disorder is sleep disorder or sexual dysfunction.
22. The method of claim 19 wherein the disorder is drug or alcohol addiction.
23. The method of claim 19 wherein the disorder is a cognitive disorder.
24. The method of claim 19 wherein the disorder is a neurodegenerative disease.
25. The method of claim 24 wherein the neurodegenerative diseases is Parkinson’s disease or Alzheimer’s disease.
26. The method of claim 19 wherein the disorder is migraine.
27. The method of claim 19 wherein the disorder is obesity.
28. The method of claim 19 further comprising administration of a serotonin reuptake inhibitor.
29. The method of claim 28 wherein the serotonin reuptake inhibitor is selected from the group consising of fluoxetine, fluvoxamine, paroxetine, sertraline and venlafaxine.
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 mining machine comprising:
a frame;
a motor;
a drive shaft having a first end, a distal end, and an axis;
a driven component coupled to the drive shaft at the distal end; and
a connector assembly between the motor and the drive shaft, the connector assembly including
a connection mechanism operable to drivingly connect the motor and the drive shaft, and
an adjustment mechanism operable to adjust the connection mechanism between a connected condition, in which the connection mechanism drivingly connects the motor and the drive shaft, and a disconnected condition, in which the driving connection between the motor and the drive shaft is disengaged, the adjustment mechanism including an actuator pivotable, about the axis, between a connected position corresponding to the connected condition of the adjustment mechanism and a disconnected position corresponding to the disconnected condition of the adjustment mechanism, the actuator being axially fixed relative to the frame, the adjustment mechanism further including a first threaded member connected to the actuator for pivoting movement with the actuator, the first threaded member being axially movable relative to the actuator, and a second threaded member rotatable fixed to the frame and cooperating with the first threaded member.
2. The mining machine of claim 1, wherein the connection mechanism includes a spline engagement between the motor and the drive shaft.
3. The mining machine of claim 2, wherein the motor includes a sleeve having an inner surface providing a first spline, and wherein the drive shaft has a second spline proximate the first end, the first spline and the second spline being engageable to provide a driving connection between the motor and the drive shaft.
4. The mining machine of claim 1, wherein the drive shaft is movable along the axis, the adjustment mechanism being operable to move the drive shaft along the axis between the connected condition and the disconnected condition.
5. The mining machine of claim 4, wherein the adjustment mechanism includes a telescoping member connected between the actuator and the drive shaft, pivoting movement of the actuator causing selective extension and retraction of the telescoping member and axial movement of the drive shaft.
6. The mining machine of claim 1, wherein the first threaded member and the second threaded member are connected for coordinated axial movement, and wherein pivoting movement of the actuator causes pivoting movement of the first threaded member relative to the second threaded member, pivoting movement of the first threaded member relative to the second threaded member causes axial movement of the first threaded member relative to the actuator, and axial movement of the first threaded member causes axial movement of the drive shaft.
7. The mining machine of claim 1, wherein the adjustment mechanism includes a locking assembly, the locking assembly being operable to selectively retain the adjustment mechanism in at least one of the connected condition and the disconnected condition.
8. The mining machine of claim 7, wherein the locking assembly is operable to selectively retain the adjustment mechanism in each of the connected condition and the disconnected condition.
9. The mining machine of claim 8, wherein the locking assembly includes
a projection connected to the actuator, and
a first recess and a second recess defined by the frame, the projection being selectively engaged in the first recess to retain the actuator in the connected position and in the second recess to retain the actuator in the disconnected position.
10. The mining machine of claim 9, wherein the locking assembly further includes a spring member operable to bias the projection into engagement with the first recess and with the second recess.
11. The mining machine of claim 1, further comprising a second connection assembly between the drive shaft and the driven component, the second connection assembly maintaining a driving connection between the drive shaft and the driven component in the connected condition and the disconnected condition.
12. The mining machine of claim 1, wherein the actuator is pivotable in a first direction to cause adjustment of the connection mechanism from the connected condition toward the disconnected condition, the actuator being pivotable in a second direction to cause adjustment of the connection mechanism from the disconnected condition toward the connected condition.
13. The mining machine of claim 1, wherein the mining machine includes one of a longwall shearer and a feeder-breaker.
14. The mining machine of claim 13, wherein the driven component includes gear box drivingly connected to a corresponding one of a shearer and a lump breaker.
15. A connector assembly for a mining machine, the mining machine including a frame, a motor, a drive shaft having a first end, a distal end, and an axis, and a driven component coupled to the drive shaft at the distal end, the connector assembly being between the motor and the drive shaft, the connector assembly comprising:
a connection mechanism operable to drivingly connect the motor and the drive shaft; and
an adjustment mechanism operable to adjust the connection mechanism between a connected condition, in which the connection mechanism drivingly connects the motor and the drive shaft, and a disconnected condition, in which the driving connection between the motor and the drive shaft is disengaged, the adjustment mechanism including an actuator pivotable, about the axis, between a connected position corresponding to the connected condition of the adjustment mechanism and a disconnected position corresponding to the disconnected condition of the adjustment mechanism, the actuator being axially fixed relative to the frame, the adjustment mechanism further including a first threaded member connected to the actuator for pivoting movement with the actuator, the first threaded member being axially moveable relative to the actuator, and a second threaded member rotatably fixed to the frame and cooperating with the first threaded member.
16. A method of operating a mining machine, the mining machine including a frame, a motor, a drive shaft having a first end, a distal end, and an axis, a driven component coupled to the drive shaft at the distal end, and a connector assembly between the motor and the drive shaft, the method comprising:
providing a connection mechanism operable to drivingly connect the motor and the drive shaft;
providing an adjustment mechanism operable to adjust the connection mechanism, the adjustment mechanism including an actuator pivotable about the axis, the actuator being axially fixed relative to the frame, the adjustment mechanism further including a first threaded member connected to the actuator for pivoting movement with the actuator, the first threaded member being axially moveable relative to the actuator, and a second threaded member rotatably fixed to the frame and cooperating with the first threaded member;
adjusting the connection mechanism to one of a connected condition, in which the connection mechanism drivingly connects the motor and the drive shaft, and a disconnected condition, in which the driving connection between the motor and the drive shaft is disengaged; and
pivoting the actuator about the axis from a position corresponding to the one of the connected condition and the disconnected condition to a position corresponding to the other of the connected condition and the disconnected condition.