摘要:
The invention relates to pharmaceutical compositions and methods useful in the treatment of obesity which methods comprise administering to animal, including a human or companion animal, in need of such treatment an effective amount of a compound of the structural formula or a pharmaceutically acceptable salt, racemate or enantiomer thereof, wherein R is hydroxy, esterified hydroxy or etherified hydroxy; R1 and R2 are, independently, halogen, trifluoromethyl or lower alkyl; R3 is halogen, trifluoromethyl, lower alkyl, aryl, aryl-lower alkyl, cycloalkyl or cycloalkyl-lower alkyl, carbocyclic arylmethyl, carbocyclic aroyl, carbocyclic arylhydroxymethyl; or R3 is the radical wherein R8 is hydrogen, lower alkyl, aryl, cycloalkyl, aryl-lower alkyl or cycloalkyl-lower alkyl; R6 is hydroxy or acyloxy; R10 is hydrogen or lower alkyl; or R9 and R10, taken together with the carbon atom to which they are attached, form a carbonyl group; R4 is hydrogen, halogen, trifluoromethyl or lower alkyl; R5 and R6 are, independently, hydrogen or lower alkyl or R5 and R6, taken together with the carbon atom to which they are attached, form a carbonyl group; X is O, S or —NR7; R7 is hydrogen or lower alkyl; W is O or S; and Z is carboxyl or carboxyl derivatized as a pharmaceutically acceptable ester or amide. The invention further provides for pharmaceutical compositions and methods of using the compounds of structural formula (I), or the pharmaceutically acceptable salts, racemates and enantiomers thereof, in combination with an anorectic agent, in treating obesity.
摘要翻译:本发明涉及可用于治疗肥胖症的药物组合物和方法,该方法包括向需要这种治疗的动物,包括人或伴侣动物施用有效量的结构式化合物或其药学上可接受的盐,外消旋体或 其中R是羟基,酯化的羟基或醚化羟基; R 1和R 2独立地是卤素,三氟甲基或低级烷基; R 3是卤素,三氟甲基,低级烷基,芳基,芳基 - 低级烷基,环烷基或环烷基 - 低级烷基, 碳环芳基甲基,碳环芳酰基,碳环芳基羟甲基; 或R 3是其中R 8是氢,低级烷基,芳基,环烷基,芳基 - 低级烷基或环烷基 - 低级烷基的基团; R 6是羟基或酰氧基; R 10是氢或低级烷基; 或R 9和R 10与它们所连接的碳原子一起形成羰基; R 4是氢,卤素,三氟甲基或低级烷基; R 5和R 6独立地是氢或低级烷基或R 5和R 6,取代 与它们所连接的碳原子一起形成羰基; X是O,S或-NR 7; R 7是氢或低级烷基; W是O或S; 并且Z是作为药学上可接受的酯或酰胺衍生的羧基或羧基。本发明还提供了药物组合物和使用结构式(I)化合物或其药学上可接受的盐,外消旋体和对映异构体与厌食症 代理,治疗肥胖。
摘要:
The invention relates to pharmaceutical compositions and methods useful in the treatment of obesity which methods comprise administering to animal, including a human or companion animal, in need of such treatment an effective amount of a compound of the structural formula or a pharmaceutically acceptable salt, racemate or enantiomer thereof, wherein R is hydroxy, esterified hydroxy or etherified hydroxy; R1 and R2 are, independently, halogen, trifluoromethyl or lower alkyl; R3 is halogen, trifluoromethyl, lower alkyl, aryl, aryl-lower alkyl, cycloalkyl or cycloalkyl-lower alkyl, carbocyclic arylmethyl, carbocyclic aroyl, carbocyclic arylhydroxymethyl; or R3 is the radical wherein R8 is hydrogen, lower alkyl, aryl, cycloalkyl, aryl-lower alkyl or cycloalkyl-lower alkyl; R9 is hydroxy or acyloxy; R10 is hydrogen or lower alkyl; or R9 and R10, taken together with the carbon atom to which they are attached, form a carbonyl group; R4 is hydrogen, halogen, trifluoromethyl or lower alkyl; R5 and R6 are, independently, hydrogen or lower alkyl or R5 and R6, taken together with the carbon atom to which they are attached, form a carbonyl group; X is O, S or —NR7; R7 is hydrogen or lower alkyl; W is O or S; and Z is carboxyl or carboxyl derivatized as a pharmaceutically acceptable ester or amide. The invention further provides for pharmaceutical compositions and methods of using the compounds of structural formula (I), or the pharmaceutically acceptable salts, racemates and enantiomers thereof, in combination with an anorectic agent, in treating obesity.
摘要翻译:本发明涉及可用于治疗肥胖症的药物组合物和方法,该方法包括向需要这种治疗的动物,包括人或伴侣动物施用有效量的结构式化合物或其药学上可接受的盐,外消旋体或 其中R是羟基,酯化的羟基或醚化羟基; R 1和R 2独立地是卤素,三氟甲基或低级烷基; R 3是卤素,三氟甲基,低级烷基,芳基,芳基 - 低级烷基,环烷基或环烷基 - 低级烷基, 碳环芳基甲基,碳环芳酰基,碳环芳基羟甲基; 或R 3是其中R 8是氢,低级烷基,芳基,环烷基,芳基 - 低级烷基或环烷基 - 低级烷基的基团; R 9是羟基或酰氧基; R 10是氢或低级烷基; 或R 9和R 10与它们所连接的碳原子一起形成羰基; R 4是氢,卤素,三氟甲基或低级烷基; R 5和R 6独立地是氢或低级烷基或R 5和R 6,取代 与它们所连接的碳原子一起形成羰基; X是O,S或-NR 7; R 7是氢或低级烷基; W是O或S; 并且Z是作为药学上可接受的酯或酰胺衍生的羧基或羧基。本发明还提供了药物组合物和使用结构式(I)化合物或其药学上可接受的盐,外消旋体和对映异构体与厌食症 代理,治疗肥胖。
摘要:
A method provides for joining an outer sheet and an inner sheet, in particular of an attachment part of a motor vehicle body. On the visible sides of an attachment part, a welding or brazing seam is produced between a fold of an outer sheet and an inner sheet. The outer sheet is held in a bed, and the inner sheet is pressed against the fold on an inner side thus forming a joining groove. To ensure that during beam welding or beam grazing the inner sheet is held in position on the fold, it is prevented from moving away without clamping by stops on an outer side. These stops are disposed in a row along the welding or brazing seam and in dependence upon the progress of the joining procedure can be moved individually out of a path of a welding or brazing head.
摘要:
The invention relates to a machining device for machining a workpiece (W), wherein a rotatably mounted machining tool (2a) is held in a machining unit (2), and the machining unit (2) can be moved axially along the axis of rotation (X) of the machining tool (2a) by means of a feed device (10). The machining device comprises a pressure plate (6), mounted in a freely movable manner by means of a bearing device (4), and a measuring device (8) for position detection. According to the invention, the pressure plate (6) and the bearing device (4) constitute part of a pressure-exerting unit (12), and the pressure-exerting unit (12) can be moved axially with respect to the machining unit (2) in the direction of the axis of rotation (X) and independently of the machining unit (2) by means of a drive device (14) assigned to said pressure-exerting unit.
摘要:
The present invention provides methods to decrease or maintain body weight and/or body fat in patients, e.g. humans and animals, for example in the treatment of overweight or obese patients, or as a means to produce leaner meat in food stock animals, e.g., cattle, chickens, pigs, alone or in combination with second therapeutic agent; methods to treat diabetes and/or glucose intolerance; and methods to treat metabolic syndrome disorders in patients in need thereof, by administering a CCR2 therapeutic agent, kits for the above-identified therapeutic uses, and methods of identifying CCR2 therapeutic agents for treating the above-described therapeutic uses.
摘要:
A method for producing attached parts for a motor vehicle, for example doors, dampers, mudguards formed by internal (1) and external (2) sheets. The external sheet (2) is inward bent in the visible areas of the door or attached part, the sheet edges being practically parallel to the plane of attached parts in the invisible (not apparently visible) areas of the door or attached part. The internal sheet (1) is pushed against the external sheet (2) in a flanged area in such a way that a small accurately defined gap for laser welding is produced. The internal (1) and external (2) sheets are welded to each other in the form of an overlap joint in the opposite invisible areas, thereby compensating tolerances.
摘要:
A device (1) is provided for connecting a metal sheet (23, 33′) at the edges, particularly body sheet metal in automobiles. The device (1) includes at least one folding bed (2) for receiving at least two metal sheets, folding jaws (3) which are functionally connected to associated folding jaw supports (4), at least one thermal jointing tool (5), and at least one mass electrode (9, 9′). At least the joining tool is not attached to the folding jaws, and the joining tool contains a lever oriented away from the folding bed as a linear feed device. The lever (6) has a center of rotation (10) outside the folding bed, wherein the joining tool can swivel in the manner of a knee lever into an operating and/or non-operating position.
摘要:
The invention relates to a machining device for machining a workpiece, wherein a rotatably mounted machining tool (2a) is held in a machining unit (2), and the axis of rotation (X) of the machining tool (2a) can be aligned with the workpiece surface to be machined, and therefore the axis of rotation (X) coincides with the geometric normal (N) in the machining point of the workpiece surface. The machining device comprises a pressure plate (6) mounted in a freely rotatable manner on the machining device via a bearing device (4), and a measuring device (8) for detecting a deviation in the position of the pressure plate (6). According to the invention, the bearing device (4) has a bearing body (40b) having at least one spherical surface region, and a bearing receptacle (40a) which surrounds the bearing body (40b) at the spherical surface regions in a form-fitting manner.
摘要:
An electrical ignition device (1) has a metal container (2) for a firing resistor or bridge, a first (3) and a second (4) terminal pin and at least one ignition charge (5, 6).So that firing of the ignition charge does not occur in the event of electrical discharges between terminal pins and a housing, it is proposed that the container (2) be capable of being embedded in a plastic material by injection moulding and inserted in the housing, that a first outward extension (8) be provided on the container (2) which is electrically conductively connected to the first terminal pin (3), and that a second outward extension (9) be provided on the container (2) which can be formed so as to extend to the housing leaving a small clearance and of which an outer end is not embedded in the plastic material.
摘要:
A method for producing attached parts for a motor vehicle, for example doors, dampers, mudguards formed by internal (1) and external (2) sheets. The external sheet (2) is inward bent in the visible areas of the door or attached part, the sheet edges being practically parallel to the plane of attached parts in the invisible (not apparently visible) areas of the door or attached part. The internal sheet (1) is pushed against the external sheet (2) in a flanged area in such a way that a small accurately defined gap for laser welding is produced. The internal (1) and external (2) sheets are welded to each other in the form of an overlap joint in the opposite invisible areas, thereby compensating tolerances.