Abstract:
The present invention relates to an aerosol dispensing apparatus (1), more particularly to aerosol dispensing valves incorporating a controlled metered dispensing function wherein the metering chamber (7) holding the next aerosolized dose is in fluidic communication with the reservoir (3) allowing homogenous mixing of the next aerosolized dose to be dispensed.
Abstract:
The present invention relates to certain substituted 17β-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I), wherein R?1 and R2¿ i) are independently hydrogen or lower alkyl and the bond between the carbons bearing R?1 and R2¿ is a single or a double bond, or ii) taken together are a -CH¿2?- group forming a cyclopropane ring, and the bond between the carbons bearing R?1 and R2¿ is a single bond; R3 is preferably hydrogen, halogen or lower alkyl, R4 is preferably hydrogen or lower alkyl, X is preferably CH¿2?, Y is preferably hydrogen and Z is preferably CONR?14R15 and R14 and R15¿ are a variety of organic groups, and pharmaceutically acceptable salts thereof, preparation, medical use and pharmaceutical formulations.
Abstract:
The present invention relates to water soluble, camptothecin derivatives of formula (I), wherein A represents a moiety of formula (IIA), (IIB) or (IIC), X is selected from the group consisting of alkyl, aryl, (CH2)mOR , (CH2)mSR and (CH2)mNR R wherein m is an integer of 0 to 6, and R and R are hydrogen, lower alkyl, aryl or together with the nitrogen form a 5-7 membered ring; q is an integer of 0 to 2; n represents the integer 1 or 2; p is an integer of 1 to 6; Y and W are selected from the group consisting of alkyl, aryl, alkoxy, aryloxy and amino, Q is oxygen or sulfur; P is phosphorus; J represents the atoms necessary to complete a 5 or 6 membered aromatic ring; and the pharmaceutically acceptable salts thereof; their use as topoisomerase inhibitors, their preparation; and their use in the treatment of cancer.
Abstract:
A breath actuated dry powder medicament inhaler (10) has a primary air passageway (14) therethrough defining a venturi (14c) in the medial portion thereof. A second air passageway (16) is provided which contains a compound deaggregating swirl chamber (16c) and is fluidly connected to the venturi (14c). A dry powder storage chamber (18) and cooperatively associated metering plate (18b) act to introduce a predetermined amount of compound into the swirl chamber upon actuation of the metering plate. The primary air passageway (14) is configured within the inhalator apparatus so as to create an optimized air flow trajectory through the mouth of the user to minimize dry powder compound impingement upon the outside radius of the throat.
Abstract:
The present invention relates to the compounds of formula (I), wherein: R1 is hydrogen, hydroxy or amino; R2 is hydrogen, hydroxy, methoxy or methoxymethoxy; R3 is hydrogen, hydroxy, amino, methoxy, methoxymethoxy or, taken together with R2, methylenedioxy (also known as 1,3 dioxolo); R4 is hydrogen, hydroxy, methoxy, methoxymethoxy, benzyl, di(C¿1-4?)alkylaminomethyl or, taken together with R?3¿, methylenedioxy; R5 is hydrogen or hydroxy; provided that at least one of R1 through R5 is other than hydrogen; and i) X2 is hydroxy or methoxy with X?1, X3 and X4¿ being hydrogen or ii) X1 taken together with X2, X2 taken together with X3 or X3 taken together with X4, is methylenedioxy, provided that each of the remaining respective X?1, X2, X3 and X4¿ substituents are hydrogen, intermediates in the synthesis of them, pharmaceutical formulation containing them, their use as inhibitors of topoisomerase and their use in the treatment of tumors.
Abstract:
Aminobutanoic acids of formula (I) where R -R are a variety of substituents, novel intermediates, a pharmaceutical composition for treating inflammatory diseases, demyelinating diseases, and tumor metastasis, methods for such treatment and processes for preparing compounds of formula (I).
Abstract:
This invention relates to a new process for preparing certain optically active purine substituted cyclopentene derivatives including the antiviral agent, carbovir, and novel intermediates used in this process. In particular, this invention concerns a synthesis of (1R-cis)-4-hydroxymethyl-2-cyclopenten-1-ol, an intermediate in this process.
Abstract:
Novel pyrrolidine compounds of formula (I) which are useful for inhibiting the function of Type IV phosphodiesterase (PDE-IV) as wll as methods for making the same are disclosed. Applications in treating inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, are also disclosed.