摘要:
Compounds of formula (1), salts and pro-drugs wherein: R1, R2, R3 and R4 are hydrogen, alkyl, hydroxyalkyl, halogen, haloalkyl, alkoxy, haloalkoxy, alkoxycarbonyl, carboxyl, hydroxyl, nitro, amino, monalkylamino, dialkylamino, acylamino, alkoxycarbonylamino, alkylsulphonyl, arylsulphonyl, alkylsulphonylamino, arylsulphonylamino, aminosulphonyl or cyano, or any two of R1 to R4 that are adjacent on the ring may together represent the moiety —O—(CH2)n—O— wherein n is 1 to 3; R5 is hydrogen or alkyl; R6 is hydrogen or alkyl; and X is selected from the group consisting of: (a) groups of formula OR7 wherein R7 is hydrogen or alkyl which is optionally substituted with a substituent selected from alkylsulfonylalkyl, saturated or partially unsaturated heterocyclic, alkoxy, carboxyl, nitro, amino, monalkylamino, dialkylamino, halogen, and alkoxycarbonyl, provided that when R7 is hydrogen or ethyl, then R1, R2, R3 and R4 cannot be selected from hydrogen, halogen and alkyl; and (b) groups of formula NR8R9 wherein R8 and R9 together with the nitrogen atom to which they are attached form a saturated or partially unsaturated heterocyclic group which optionally contains at least one more heteroatom selected from nitrogen, oxygen and sulphur atoms, said saturated or partially unsaturated heterocyclic group optionally further being substituted by one or more substituents selected from alkyl, halogen, haloalkyl, alkoxy, alkoxycarbonyl, carboxyl, nitro, amino, monalkylamino, dialkylamino and hydroxyl, provided that: (i) when R8+R9+N=piperazine, and ≧1 of R1 to R4 are hydrogen, hydroxyl, nitro, amino, alkylamino, dialkylamino, alkoxycarbonylamino, halogen, alkoxy or alkyl, the nitrogen atom at the 4-position of the piperazine is not alkyl substituted, (ii) when each of R1, R2, R3, R4, R5 and R6 is hydrogen, X is not unsubstituted piperazinyl or unsubstituted morpholino, (iii) when each of R1, R2, R4, R5 and R6 is hydrogen and R3 hydrogen, bromine or hydroxyl, X is not methoxy, (iv) when each of R2 and R3 is methoxy or they together represent —O—CH2—O— and each of R1, R4, R5 and R6 is hydrogen, X is not unsubstituted piperidine, are Cavx channel blockers and are of use in the treatment of various conditions including pain.
摘要:
A method and system for improving the effectiveness of coaches and video game designers for games like soccer, American football, basketball, lacrosse or ice hockey by using RF technology and software. A base station is equipped with a computer programmed with algorithms to track the players and game equipment and thereby produce data of interest to a coach or game designer.
摘要:
A system and method for providing statistics gathering within a packet network is disclosed. The system comprises a network processor, a traffic manager, a host processor, and a field programmable gate array. The network processor adds a header to received multimedia packets and the traffic manager measures and enforces multimedia flow rates. The host processor performs multimedia flow quality measurement services on a per flow basis, wherein the multimedia flow quality measurement services comprise maintaining current statistics for multimedia flows within the network processor including aggregate and minimum/maximum statistics for the multimedia flow. The field programmable gate array (FPGA) copies a received multimedia packet or a portion of the received multimedia packet, wherein the copy is utilized by the FPGA to perform statistics gathering via use of a latency engine, a lost packet calculation engine, a real-time transport control protocol packet jitter engine and a real-time transport protocol packet jitter engine.
摘要:
The invention encompasses formulations that demonstrate the feasibility of oral absorption comprising GLP-1 compounds and specified delivery agents.
摘要:
The present invention provides compounds having H.sub.3 histamine receptor antagonist activity of formula (1.0) wherein R.sub.2 is a hydrogen or a methyl or ethyl group; R.sub.3 is a hydrogen or a methyl or ethyl group; n is 0, 1, 2, 3, 4, 5, or 6; and R.sub.1 is selected from the group consisting of (a) C.sub.3 to C.sub.8 cycloalkyl; (b) phenyl or substituted pneyly; (c) alkyl; (d) heterocyclic; (e) decahydronaphthalene; and (f) octahydroindene; with the proviso that when X is H, A can be --CH.sub.2 CH.sub.2, --COCH.sub.2 --CON(CH.sub.3)--, --CH.dbd.CH--, .alpha., --CH.sub.2 --NH--, --CH.sub.3 --N(CH.sub.3)--, --CH(OH)CH.sub.2 --, --NH--CH.sub.2 --, --N(CH.sub.3)--CH.sub.2 --, --CH.sub.2 O--, --CH.sub.2 S--, and --NHCOO--; when X is NH.sub.2, HN(CH.sub.3), N(CH.sub.3).sub.2, OH, OCH.sub.3, CH.sub.3, SH and SCH.sub.3 ; A can be --NHCO--, --N(CH.sub.3)--CO--, --NHCH.sub.2 --, --N(CH.sub.3)--CH.sub.2 --, --CH.dbd.XH--, --COCH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH( )H)CH.sub.2 --, or .beta.; and when R.sub.1 and X taken together denote a 5,6 or 6,6 saturated bicyclic ring structure, X can be NH, O, or S. The pharmaceutically acceptable salts, hydrates, and individual stereoisomers of compounds of structural formula (1.0), as well as mixtures thereof, are also contemplated as falling within the scope of the present invention. The invention also provides pharmaceutical compositions comprising a pharmaceutically acceptable carrier in combination with an effective amount of a compound of said formula and a method of treating conditions in which antagonism of histamine H.sub.3 receptors may be of therapeutic importance.
摘要:
An automated bank teller machine (ATM) is provided which is characteristically easy to configure, regardless of whether a replenish-from-the-front (RFTF) configuration or a replenish-from-the-rear (RFTR) configuration is chosen. In particular, the ATM according to the present invention includes a security chest module, a top module, and an interface module. These components are common to both configurations can be built and stored in advance, and can be thereafter configured as desired. In another embodiment, an ATM is provided that permits more than one customer to use the ATM at the same time.
摘要:
The present invention provides compounds having H.sub.3 histamine receptor antagonist activity of the general formula: ##STR1## where X is H, A is --CH.sub.2 CH.sub.2 --, --COCH.sub.2 --, --CONH--, --CON(CH.sub.3)--, --CH.dbd.CH--, --C.tbd.C--, --CH.sub.2 --NH--, --CH.sub.2 --NCH.sub.3 --, --CH(OH)CH.sub.2 --, --NH--CH.sub.2 --, --N(CH.sub.3) --CH.sub.2 --, --NHSO.sub.2 --, --CH.sub.2 O--, --CH.sub.2 S--, CH.sub.2 SO.sub.2 --, or --CH.sub.2 S(O)--;R.sub.2 is a hydrogen or a methyl or ethyl group;R.sub.3 is a hydrogen or a methyl or ethyl group;n is 0, 1, 2, 3, 4, 5, or 6; andR.sub.1 is selected from the group consisting of (a) C.sub.3 to C.sub.8 cycloalkyl; (b) H; (c) phenyl or substituted phenyl; (d) alkyl; (e) heterocyclic; and (f) bicyclic alkyl; andwhenX is NH.sub.2, NHCH.sub.3, N(CH.sub.3).sub.2, OH, OCH.sub.3, NHR.sub.4, OR.sub.4, SH, SR.sub.4, or SO.sub.2 R.sub.4 ; A is --NHCO--, --N(CH.sub.3)--CO--, --NHCH.sub.2 --, --N(CH.sub.3)--CH.sub.2 --, --NHSO.sub.2 --, --CH.dbd.CH--, --CH.dbd.CHF--, --COCH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH(OH)CH.sub.2 --, or --C.tbd.C--;R.sub.2 is a hydrogen or a methyl or ethyl group;R.sub.3 is a hydrogen or a methyl or ethyl group;n is 0, 1, 2, 3, 4, 5, or 6;R.sub.1 is selected from the group consisting of (a) C.sub.3 to C.sub.8 cycloalkyl; (b) H; (c) phenyl or substituted phenyl; (d) alkyl; (e) heterocyclic; and (f) bicyclic alkyl andR.sub.4 is designated to mean that X is contained within a ring such as octahydroindole.
摘要:
Coordinating real-world gatherings to promote an online community, the method including: encouraging participants of the online community to participate in a real-world gathering by providing incentives for the participants; promoting familiarity among the participants by providing and introducing online community titles of the participants at the real-world gathering; and providing online benefits or rewards to the participants for participating in the real-world gathering. Keywords include socializing in the real world, community building and bridging the gap between the game world and the real world.