Abstract:
Compounds of formula (I) suppress the normal signalling activity CB1 receptors, and are thus useful in the treatment of diseases or conditions which are mediated by CB1 receptor signalling activity, such as treatment of obesity and overweight, prevention of weigh gain, treatment of diseases and conditions directly or indirectly associated with obesity and overweight: wherein A1 is hydrogen, —COOH, or tetrazolyl, and A2 is hydrogen, —COOH, or tetrazolyl, provided that one of A1 and A2 is either —COOH or tetrazolyl; p is 0 or 1 and A3 is phenyl or cycloalkyl, either of which is optionally substituted with R4 and/or R5; q is 0 or 1; R3 is hydrogen, C1-C4 alkyl, cycloalkyl, —CF3, or —OR9; R4 and R5 independently —R9, —CN, —F, —Cl, —Br, —OR9, —NR7R8, —NR7COR6, —NR7SO2R6, —COR6, —SR9, —SOR9, or —SO2R6; R6 is C1-C4 alkyl, cycloalkyl, —CF3 or —NR7R8; R7 and R8 are independently hydrogen, C1-C4 alkyl, —CF3, or cycloalkyl; R9 is hydrogen, C1-C4 alkyl, cycloalkyl, fully or partially fluorinated C1-C4 alkyl; R1 is (i) a bond, or (ii) —(CH2)aB1(CH2)b— wherein a and b are independently 0, 1, 2 or 3 provided that a+b is 1, 2 or 3; or (iii) —C(R10)(R11)—*, —C(R10)(R11)—O—*, —C(R10)(R11)CH2—*, —C(R10)(R11)CH2—O—*, —CH2C(R10)(R11)—*, —CH2C(R10)(R11)—O—*, —CH2—O—C(R10)(R11)—* or —C(R10)(R11)—O—CH2—*, wherein the bond indicated by an asterisk is attached to the pyrazole ring; R2 is a divalent radical of formula -Q1-A4-[Q2]w- wherein Q1, A4 Q2 and w are as defined in the specification; and R10 is hydrogen and R11 is (C1-C3)alkyl or —OH; or R10 and R11 are both (C1-C3)alkyl; or R10 and R11 taken together with the carbon atom to which they are attached form a (C3-C5)cycloalkyl ring.
Abstract:
A fluid dispenser contains and dispenses metered amounts of fluid, and in some embodiments comprises a reservoir for containing fluid; a chamber positioned substantially within the reservoir for containing a quantity of fluid; and a piston moveable within the chamber in a first direction to draw fluid into the chamber from the reservoir, and movable in a second direction to discharge a metered amount of fluid from the chamber. A user-manipulatable control can be coupled to the piston to move the piston with respect to the chamber, and in some cases to select the desired metered amount of fluid to be dispensed. Also, a pawl can be used to selectively permit and inhibit movement of the piston in the first and/or second directions to prevent partial doses from being dispensed from the fluid dispenser.
Abstract:
The invention relates to thienopyridazinones of formula (I): wherein: R1 is C1-6 alkyl, C2-6 alkenyl or C3-6 cycloalkyl which is optionally substituted by C1-6 alkyl, each of the above being optionally substituted by one or more halogen atoms; R2 is C1-6 alkyl; R3 is a group CO-G or SO2-G where G is a 5- or 6-membered ring containing a nitrogen atom and a second heteroatom selected from oxygen and sulphur adjacent to the nitrogen, and optionally substituted by up to 3 groups selected from hydroxyl and C1-4 alkyl; Q is CR5R6 where R5 and R6 are as defined in the specification; and R4 is a 5- to 10-membered mono- or bi-cyclic aromatic ring system, containing 0 to 4 heteroatoms independently selected from nitrogen, oxygen and sulphur, the ring system being optionally substituted as described in the specification, and pharmaceutically acceptable salts and solvates thereof. Processes for their preparation, pharmaceutical compositions containing them and their use in therapy, in particular in the modulation of autoimmune disease are also described.
Abstract:
A method for collecting performance test data during a performance test of an athlete from timing devices associated with a performance test includes automatically receiving an electronic time stamp message from each of the timing devices, each electronic time stamp message incorporating a time stamp generated by the timing device in response to entering into a triggered state during the performance test; and automatically inserting time data corresponding to the received time stamps into respective fields of an electronic performance test record associated with the unique athlete identifier. A system for collecting performance test data includes a plurality of timing devices each configured to generate one or more electronic time stamp messages each incorporating a time stamp generated in response to entering into a triggered state during a performance test; a synchronizing device configured to periodically transmit electronic synchronize instructions to the timing devices to synchronize the timing devices; and a control device configured to receive the electronic time stamp messages from the timing devices and to insert time data corresponding to the time stamps into respective fields of performance test records.
Abstract:
The present invention is directed to novel crystalline forms of 4-(2-fluorophenyl)-6-methyl-2-(piperazin-1-yl)thieno[2,3-d]pyrimidine salts, including 4-(2-fluorophenyl)-6-methyl-2-(piperazin-1-yl)thieno[2,3-d]pyrimidine hydrochloride crystalline forms. The present invention is also directed to compositions including such crystalline forms and methods for making and using such crystalline forms, e.g., in the treatment of gastrointestinal and/or genitourinary disorders.
Abstract:
The invention provides certain pyrrolo-, thieno-, furano- and pyrazolo-[3,4-d]pyridazinones, processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and methods of treatment involving their use.
Abstract:
Compounds of the formula (I) wherein X, R.sup.1, R.sup.2, and Ar.sup.1 as defined in the specification. The compounds are useful medicaments, particularly in the treatment of asthma or rhinitis.