摘要:
The invention relates to heterocyclic derivatives of the formula (I): A—B—X1—T1(R2)—L1—T2(R3)—X2—Q or pharmaceutically acceptable salts thereof, which possess antithrombotic and anticoagulant properties due to their inhibition of Factor Xa and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect.
摘要:
The invention concerns novel (oxamido- and ureido-phenylsulfonyl)nitromethane derivatives and pharmaceutically acceptable salts thereof which are inhibitors of the enzyme aldose reductase and are of value, for example, in the treatment of certain peripheral effects of diabetes and galactosemia. Also disclosed are pharmaceutical compositions containing one of the derivatives and processes for the manufacture and use of the derivatives.
摘要:
Amide derivatives of the formula: ##STR1## wherein either R.sup.1 is aryl or heterocyclic and A.sup.1 is a direct link, or R.sup.1 is aryl or heterocyclic, or hydrogen, or halogeno, hydroxy, amino, guanidino, mercapto, carboxy, carbamoyl, or a substituted derivative thereof, and A.sup.1 is alkylene, alkenylene, cycloalkylene or cycloalkenylene; wherein X is carbonyl or hydroxymethylene or substituted derivatives thereof; wherein A.sup.2 is alkylene, alkenylene or alkylidene; wherein R.sup.2 is hydrogen or alkyl which is unsubstituted or which bears an aryl substituent, or R.sup.2 has the formula --Q.sup.2 --R.sup.20 as defined below; wherein R.sup.3 is hydrogen, alkyl or a carbonyl-containing group; wherein R.sup.4 is hydrogen or alkyl which is unsubstituted or which bears a halogeno, hydroxy, amino, guanidino, carboxy, carbamoyl, mercapto, alkoxy, alkylamino, dialkylamino, cyclic amino, alkylthio, alkanoylamino, alkoxycarbonylamino, alkoxycarbonyl, alkoxycarbonyl, aryl or heterocyclyl substituent;wherein --NR.sup.5 --CR.sup.6 R.sup.16 --Q.sup.1 --R.sup.10 is an amino acid residue, R.sup.5, R.sup.6 and R.sup.16 being defined in claim 1, wherein Q.sup.1 and Q.sup.2, which may be the same or different, each is carbonyl (--CO--) or methylene (--CH.sub.2 --); and wherein R.sup.10 and R.sup.20, which may be the same or different, is hydroxy, amino or a substituted derivative thereof or hydroxyamino or arylthio; or a salt thereof where appropriate; processes for their manufacture and pharmaceutical compositions containing them. The compounds are inhibitors of angiotensin converting enzyme and may be used in the treatment of hypertension.
摘要:
The invention concerns .alpha.-aminoacyl derivatives of phenyl-, phenoxy-, thiophenoxy- and phenylsulphinylalkanoic acids together with their amides, esters and pharmaceutically acceptable salts; processes for their preparation; and pharmaceutical compositions for therapeutic use in inhibiting the formation of thrombi and also in reducing the persistence of thrombi formed in the blood of warm blooded animals. Representative compounds of the invention are methyl 4-(aminoacetyl)phenoxyacetate, 4-(aminoacetyl)phenoxyacetic acid and methyl 4-(aminoacetyl)-thiophenoxyacetate, preferably as their hydrochlorides.
摘要:
6-Dimethylamino-4-hydroxycinnolin-3-yl carboxylic acid; ethyl 6-n-but-2-ylamino-4-hydroxycinnolin-3-yl carboxylate or the pharmaceutically-acceptable acid-addition salts thereof. The compounds are active as inhibitors of effects following the combination of reagin-like antibodies and their antigens.
摘要:
Cinnolin-3-yl carboxylic acids and esters, amides and like derivatives, processes for the preparation of these compounds, and pharmaceutical compositions comprising any one of these compounds. A representative compound is ethyl 6-ethylcinnolin-3-yl carboxylate. The compounds are active as inhibitors of effects following the combination of reagin-like antibodies and their antigens.
摘要:
A radio frequency communications system (100) includes wireless terminals (102) and base sites (104). The wireless terminals communicate with the base sites over a radio frequency channel (106). The base sites are interconnected to each other and other network elements via a packet network. The communication system has a radio frequency channel (400) with time slots (406, 408) for transmission of both delay-sensitive data, such as streaming audio and video, and non-delay-sensitive data. A method and apparatus are provided for determining whether a time slot in the radio frequency channel is to be allocated to delay-sensitive data or non-delay-sensitive data (704, 706, 708). Each packet of data transmitted over the wireless channel has a type of service field (900). The type of service field has a precedence or priority value (902) and a service type (904). The priority values are used to determine which packet should be transmitted across the radio frequency channel next and the service type determines the transmission protocol.
摘要:
A compound of formula (I), or a pharmaceutically-acceptable salt thereof, wherein A is an optionally substituted 5- or 6-membered monocyclic aromatic ring containing 1, 2 or 3 ring heteroatoms; B is optionally substituted phenylene or a 6-membered heterocyclic ring containing 1, 2 or 3 nitrogen heteroatoms; R and R1 are hydrogen or (1-4C)alkyl; n is 1 or 2; R2 and R3 are hydrogen, (1-6C)alkyl, (4-7C)cycloalkyl, or (2-6C)alkenyl, or R2 and R3 may form along with the nitrogen to which they are attached a 5-, 6- or 7-membered heterocyclic ring, wherein each R2 or R3 group or any heterocyclic ring formed from R2 and R3 may be optionally substituted with various substituent groups, and wherein Q may be optionally substituted by various substituent groups, which posseses antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention relates to processes for the preparation of the compounds represented by formula (I), to pharmaceutical compositions containing them, and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect.
摘要:
The invention relates to heterocyclic derivatives of formula (I) and (Ia), or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect.
摘要:
Significant improvements in papermaking control can be achieved by employing an array of sensors that are positioned underneath the wire of the machine to measure the conductivity of the aqueous wet stock. The conductivity of the wet stock is directly proportional to the total water weight within the wet stock; consequently, the sensor provides information which can be used to monitor and control the quality of the paper sheet produced. Because CD water weight profile is obtained practically instantaneously, the MD and CD variations are essentially decoupled. Quality improvements to the sheet fabricated will be achieved by providing fast control of the actuators on the machine and by tuning components on the machine to eliminate the sources of variations. Further, the dry stock weight of a sheet of wet stock that is resting on a water permeable moving wire of the papermaking machine can be made employing a water weight sensor element that is positioned adjacent to the wire and that generates signals indicative of the water weight of the sheet of wet stock on the wire. Moreover, the moisture level cross-direction (CD) profile of a sheet of material that is produced can also be measured.