摘要:
The invention relates to 2-alkyl-6-cycloamino-3-(pyridin-4-yl)imidazo[1,2-b]pyridazine derivatives of the general formula (I) where: R2 is a C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-4-alkyl, C1-4-alkyloxy-C-M-alkyl, C3-7-cycloalkyloxy-C1-4-alkyl>C3-7-cycloalkyl-C1-4-alkyloxy-C1-4-alkyl, hydroxy-C1-6-alkyl, C1-4-fluoroalkyl group; R3 is a hydrogen atom or a substituent selected from halogen atoms and the C1-3 alkyl, —NR4R5, hydroxyl or C1-4 alkyloxy groups; A is a C1-7-alkylene group optionally substituted by one or two Ra groups; B is a C1-7-alkylene group optionally substituted by one or two Rb groups; L is either a nitrogen atom optionally substituted by an Rc or Rd group or a carbon atom substituted by an Re1 group and an Rd group or by two Re2 groups; Rd is a group selected from a hydrogen atom or a C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-alkylthio-C1-6-alkyl, C1-6-alkyloxy-C1-6-alkyl, C1-6-fluoroalkyl, hydroxy-C1-6-alkyl group; Rf is a C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-alkyloxy-C1-6-alkyl, C3-7-cycloalkyloxy-C1-4-alkyl, C3-7-cycloalkyl-C1-4-alkyloxy-C1-4-alkyl, hydroxy-C1-6-allyl, C1-6-fluoroalkyl or benzyl group. The invention also relates to a method for preparing same and to the therapeutic application thereof.
摘要:
The present invention extends to the compound of formula I: or a prodrug, pharmaceutically acceptable salt, or solvate of said compound. Furthermore, the present invention is directed to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula I, and a pharmaceutically acceptable carrier.Furthermore, the present invention is directed to the use of a compound of formula I as an inhibitor of tryptase, comprising introducing the compound into a composition comprising tryptase. In addition, the present invention is directed to the use of a compound of formula I for treating a patient suffering from, or subject to, a physiological condition in need of amelioration of an inhibitor of tryptase comprising administering to the patient a therapeutically effective amount of the compound of claim 1 The present invention is directed also to the preparation of a compound of formula I.
摘要:
A crane tower device includes a basket that supports a tower crane and sits within a bay formed by the vertical columns of a building under construction. The basket and the tower crane are supported by support stubs that are attached to the vertical columns. Because the lateral and vertical load is principally distributed vertically to the vertical columns rather than horizontally, no reinforcement of the horizontal beams, floors or any other portion of the building structure are needed, which results in substantial cost savings.
摘要:
A method for eliminating errors in foreground object detection in digitized images comprises providing a reference camera and a secondary camera, vertically aligning each said camera with a baseline that is approximately perpendicular to a ground plane, wherein said reference camera is placed lower than said secondary camera, selecting a foreground pixel in a reference view of a first point in a foreground object, finding a conjugate pixel of the foreground pixel in a secondary view, using the foreground and conjugate pixels to determine an image base pixel of a base point in the reference view, wherein said base point is a point on the ground plane below the first point, and using the foreground and image base pixels to find a location where the ground plane is first visible.
摘要:
A golf putter head is generally triangular, when viewed from the top, with a flat, front face and a trailing, central tail. When viewed from the side, the head has a generally straight front face and a flat or slightly curved or rounded bottom surface. The shaft for the grip is anchored to the head at a generally central position on the top of the head, with the axis of the shaft from the ball contact point on the face of the putter head being about one-half the diameter of a legal U.S. golf ball. The head is formed and/or weighted so that the shaft is on the horizontal center of gravity of the putter head, and the vertical center of gravity is about midway between the top and bottom surfaces of the head.
摘要:
This invention relates to compounds of the formula ##STR1## where R.sub.1 -R.sub.6, X and Y are as defined in the specification, which are useful for the treatment of various memory dysfunctions characterized by a cholinergic deficit and thus may be indicated in the treatment of Alzheimer's disease.
摘要:
This invention relates to compounds of the formula ##STR1## where R.sub.1 -R.sub.6, X and Y are as defined in the specification, which are useful for the treatment of various memory dysfunctions characterized by a cholinergic deficit and thus may be indicated in the treatment of Alzheimer's disease.
摘要:
This invention relates to N-heteroaryl-4-pyrimidinamines of the formula ##STR1## where R.sub.1 is hydrogen, loweralkyl, aryl, or arylloweralkyl; R.sub.2 and R.sub.3 are independently hydrogen or loweralkyl, or R.sub.2 and R.sub.3 taken together are aryl; R.sub.4 and R.sub.5 are independently hydrogen or loweralkyl, or R.sub.4 and R.sub.5 taken together are aryl; X is hydrogen, halogen, cyano, nitro, amino, loweralkyl, loweralkoxy, trifluoromethyl or ##STR2## where Y is hydrogen, halogen or loweralkyl; m is an integer of 1 to 3; and the pharmaceutically acceptable acid addition salts thereof and where applicable the geometrical and optical isomers and racemic mixtures thereof. The compounds of this invention display utility as memory enhancing agents and as analgesic agents.
摘要:
The invention relates to 1-aryloxy-2,3,4,5-tetrahydro-3-benzazepines of the formula ##STR1## wherein Y is the same or different and is hydrogen and lower alkoxy; X is hydrogen, halogen, lower alkyl, lower alkoxy, CF.sub.3, No.sub.2, CN and NH.sub.2 ; R is hydrogen, lower alkyl, cycloalkyllower alkyl, ##STR2## Ar lower alkyl of the formula ##STR3## where Z is hydrogen, lower alkyl, lower alkoxy, halogen CF.sub.3, NO.sub.2 and NH.sub.2 ; Aryloxy lower alkyl of the formula ##STR4## where Z is as previously defined; and an alkylene amine of the formula ##STR5## where R.sub.1 and R.sub.2 are the same or different and are hydrogen and lower alkyl, n is an integer of 1 or 2; and the pharmaceutically acceptable acid addition salts thereof.
摘要:
There are disclosed compounds of the formula, ##STR1## wherein m, n, p, R, R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification; which compounds are useful for enhancing memory and also as analgesic and antidepressant agents.