Abstract:
The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises administering to that subject a therapeutically effective amount of a compound of formula I: wherein, generally, Q is R1 is benzyl, phenyl, thiophene or imidazolyl optionally substituted with C1-4alkyl or halogen, such as methyl, fluorine or bromine; R2 is hydrogen or C1-4alkyl such as methyl; R3 is phenyl; R4 is hydrogen; R5 is hydrogen or C1-6alkylcarbonyl such as methylcarbonyl; X is —SO2— or —C(O)N(R2)SO2— where R2 is preferably hydrogen; Y is a bond, CH2 or Z1 where Z1 is —N(Rf)— in which Rf is C1-6alkylcarbonyl such as ethylcarbonyl; and R6 is phenyl, pyrazolyl, pyridyl, pyrimidinyl or benzimidazolonyl optionally substituted with one or two groups chosen from C1-6alkyl and benzyl, such as methyl, ethyl and benzyl; or a pharmaceutically acceptable salt thereof.
Abstract translation:本发明提供治疗患有诸如精神分裂症的受试者的方法,所述疾病包括施用NK-3拮抗剂,其包括向该受试者施用治疗有效量的式I化合物:其中 通常,Q是R 1是苄基,苯基,噻吩或任选被C 1-4烷基或卤素取代的咪唑基,例如甲基,氟或溴; R 2是氢或C 1-4烷基,例如甲基; R 3是苯基; R 4是氢; R 5是氢或C 1-6烷基羰基,例如甲基羰基; X是-SO 2 - 或-C(O)N(R 2)SO 2 - ,其中R 2 O / >优选为氢; Y是键,CH 2或Z 1,其中Z 1是-N(R f), - 其中R 1是C 1-6烷基羰基,例如乙基羰基; R 6是苯基,吡唑基,吡啶基,嘧啶基或苯并咪唑烷基,任选地被一个或两个选自C 1-6烷基和苄基的基团取代,例如甲基,乙基和 苄基; 或其药学上可接受的盐。
Abstract:
Abstract of the DisclosureThe present invention relates to a hydrous kaolin product having improved optical properties, for example, when used in the production of paper products. The present invention comprises an improved barrier coating for paper and a method of making the coated paper. The present invention also comprises an improved method from making filled and coated paper products. The present invention uses a composition comprising kaolin having a shape factor of at least about 70:1, such as at least about 80:1 or at least about 100:1.
Abstract:
A device for restraining a miscreant includes a bell shaped tubular body adapted to envelop the torso of a miscreant. Openings at each end allow the body to be passed over the head to surround the torso of the miscreant. Restraining straps are each adapted to encircle one half of the tubular body. Each end of each of the straps may be locked at two diametrically opposed locations on the body. To deploy the device, it is held generally above the head of the miscreant and pulled downwardly over his head and torso. When the upper opening has passed the head of the miscreant to encircle his neck, one free end of each strap is pulled manually to cause lockable tightening thereof around the body of the device, thereby restraining the miscreant.
Abstract:
A class of 3-phenylimidazo[1,2-α]pyrimidine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH— linkage, and further substituted on the phenyl ring by alkyl, trifluoromethyl, alkoxy or one or two halogen atoms, especially fluoro, are selective ligands for GABAA receptors, in particular having good affinity for the α2 and/or α3 and/or α5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
Abstract translation:一类3-苯基咪唑并[1,2-a]嘧啶衍生物,其在苯环的间位被被氧原子或-NH-键直接连接或桥连的任选取代的芳基或杂芳基取代, 并且在苯环上被烷基,三氟甲基,烷氧基或一个或两个卤原子,特别是氟取代,是GABA A A受体的选择性配体,特别是对α2和/或α3具有良好的亲和力 和/或其α5亚基,因此有益于治疗和/或预防中枢神经系统的不良状况,包括焦虑,抽搐和认知障碍。
Abstract:
A method for determining a handover for a mobile station (1) in a multicellular communication system having a serving cell (3), a plurality of neighboring cells (4,5), and at least one control cell where the cells include at least one macrocell (2) and a plurality of microcells. The method includes the steps of comparing the received signal of the control cell with a parameter value.
Abstract:
Operating head assembly, e.g. cutter head of a coal or other mining machine having provision for feeding a supply of water or other fluid to the head during operation has provision for phasing the fluid delivery to limit it to the zone about the head in which the cutting action is taking place dependent on the direction of movement of the head. Delivery jets of the head are fed through individual valve units (22) each having an independently operable hydraulic or other actuator (28), the power input thereto being controlled by apertured timing faces (36, 38) on co-acting parts of the head (11) and body (10), power feed through the timing faces being controlled e.g. in correspondence to the position of change-over valve (44, 46) operating in response to controls which direct movement of the head. In an alternative construction the valve units are actuated mechanically by a camming formation which can be indexed depending on the direction of movement.