Patent classifications
A61P11/08
Formulations
In a metered dose inhaler, comprising a canister and metering valve, containing a suspension aerosol formulation comprising particles of formoterol fumarate dihydrate and fluticasone propionate suspended in an HFA propellant, a method of reducing deposition of particles on the surfaces of the canister and the metering valve, the method comprising the step of adding a wetting agent to the formulation.
Compounds as modulators of protein kinases
The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
Inhalable Formulation of Fluticasone Propionate and Albuterol Sulfate
This invention relates to a fixed-dose dry powder inhalation formulation comprising fluticasone propionate and albuterol sulfate, together with an α-lactose monohydrate carrier. In the formulation, the albuterol sulfate stabilises fluticasone propionate.
COMPOUNDS MODULATING C-FMS AND/OR C-KIT ACTIVITY AND USES THEREFOR
Compounds active on the receptor protein tyrosine kinases c-kit and/or c-fms are provided herewith. Also provided herewith are compositions useful for treatment of c-kit mediated diseases or conditions and/or c-fms-mediated diseases or conditions, and methods for the use thereof.
FLUORINATED PYRIDAZIN-3-ONES FOR THE USE THEREOF IN THE TREATMENT OF LUNG DISEASES
The present invention concerns compounds belonging to the family of fluorinated pyridazin-3-ones, for the use thereof in the treatment of broncho-pulmonary conditions. In compounds having a formula, or a pharmaceutically acceptable salt of the compound, the formula includes R1 representing H, an alkyl, an aryl or a heteroaryl; either E2 and E3 representing, separately from each other, H, an alkyl, an aryl or a heteroaryl, or R2 and R3 being bridged within a same cycle or via several cycles; and F representing CF.sub.3, (CF.sub.2)nCF.sub.3 or CF.sub.2H, with n representing an integer of between 1 and 7.
Surface exposed Haemophilus influenzae protein (protein E; pE)
The present invention relates to a surface exposed protein (protein E; pE), a virulence factor, which can be detected in Haemophilus influenzae, having an amino acid sequence as described in SEQ ID NO 1, an immunogenic fragment of said surface exposed protein, and a recombinant immunogenic protein (pE(A)) or truncated variants thereof based on said surface exposed protein. Nucleic acid sequences, vaccines, plasmids and phages, non human hosts, recombinant nucleic acid sequences, fusion proteins and fusion products are also described. A method of producing the said protein or truncated fragments thereof recombinantly is also disclosed.
2-phenyl-3,4-dihydropyrrolo[2,1-Ff] [1,2,4]triazinone derivatives as phosphodiesterase inhibitors and uses thereof
The present invention relates to compounds of formula I ##STR00001##
or pharmaceutically acceptable salt, solvate or hydrate thereof, wherein R.sub.1 is C.sub.1-C.sub.3alkyl optionally substituted with F, C.sub.3-C.sub.6cycloalkyl, C.sub.1-C.sub.3alkoxy; X represents a bond or C.sub.1-C.sub.3alkylene optionally substituted with OH, ONO, ONO.sub.2; R.sub.2 is H, OH, ONO, ONO.sub.2, C(O)OH, C(O)OC.sub.1-C.sub.3alkyl, CHO, CN, C.sub.1-C.sub.3alkoxy, OC(O)H, OC(O)—C.sub.1-C.sub.3alkyl, C(O)N(R.sub.6)OR.sub.7, OC.sub.1-C.sub.3alkylene-C(O)OH, OC.sub.1-C.sub.3alkylene-C(O)OC.sub.1-C.sub.3alkyl, OC.sub.1-C.sub.3alkylene-C(O)N(R.sub.6)OR.sub.7, S(O.sub.0-2)C.sub.1-C.sub.3alkyl, CR.sub.8═N—OR.sub.9, CR.sub.8═N—NR.sub.10R.sub.11, CR.sub.8═NR.sub.12 or CR.sub.8═N—ONO.sub.2; R.sub.3 is C.sub.1-C.sub.6alkyl optionally substituted with F, OH, ONO, ONO.sub.2, C.sub.1-C.sub.3alkoxy, C.sub.3-C.sub.6cycloalkyl; C.sub.3-C.sub.6cycloalkyl, C.sub.2-C.sub.6alkenyl, C.sub.2-C.sub.6alkynyl; R.sub.4 is C.sub.1-C.sub.6alkyl optionally substituted with C.sub.3-C.sub.6cycloalkyl, C.sub.1-C.sub.6alkoxy, F, ONO, ONO.sub.2; C.sub.2-C.sub.6alkenyl, C.sub.2-C.sub.6alkynyl, C.sub.3-C.sub.6cycloalkyl; R.sub.5 is H, SO.sub.2NR.sub.13R.sub.14, NHSO.sub.2NR.sub.13R.sub.14; R.sub.6 is H or C.sub.1-C.sub.3alkyl; R.sub.7 is H, C.sub.1-C.sub.3alkyl, C.sub.1-C.sub.3alkoxy, C.sub.1-C.sub.3alkyl substituted with phenyl, benzyl or a heterocyclic ring, wherein said phenyl, benzyl or said heterocyclic ring are independently optionally substituted by C.sub.1-C.sub.3alkyl, F; R.sub.8 is H, CH.sub.3 or C.sub.2H.sub.5; R.sub.9: H, C.sub.1-C.sub.3alkyl optionally substituted with OH, ONO, ONO.sub.2, CN, COOH, COOC.sub.1-C.sub.3alkyl, C.sub.1-C.sub.3alkoxy, OC(O)H, OC(O)—C.sub.1-C.sub.3alkyl, C(O)N(R.sub.6)OR.sub.7, OC.sub.1-C.sub.3alkylene-C(O)OH, OC.sub.1-C.sub.3alkylene-C(O)OC.sub.1-C.sub.3alkyl, OC.sub.1-C.sub.3alkylene-C(O)N(R.sub.6)OR.sub.7, S(O.sub.0-2)C.sub.1-C.sub.3alkyl; R.sub.10 and R.sub.11 are each independently H, C.sub.1-C.sub.3alkyl optionally substituted with OH, ONO, ONO.sub.2, CN, COOH, COOC.sub.1-C.sub.3, C.sub.1-C.sub.3alkoxy, OC(O)H, OC(O)—C.sub.1-C.sub.3alkyl, C(O)N(R.sub.6)OR.sub.7, OC.sub.1-C.sub.3alkylene-C(O)OH, OC.sub.1-C.sub.3alkylene-C(O)OC.sub.1-C.sub.3alkyl, OC.sub.1-C.sub.3alkylene-C(O)N(R.sub.6)OR.sub.7, S(O.sub.0-2)C.sub.1-C.sub.3alkyl, or together with the nitrogen atom to which they are attached form a heterocyclic ring, wherein preferably said heterocyclic ring is selected from aziridine, azetidine, pyrollidine, piperidine, morpholine, piperazine and homopiperazine, wherein said heterocyclic ring is optionally substituted with C.sub.1-C.sub.3 alky
Melanocortin Receptor Ligands
The present invention is directed to compounds according to formula,
(R.sup.2R.sup.3)-A.sup.1-c(A.sup.2-A.sup.3-A.sup.4-A.sup.5-A.sup.6-A.sup.7-A.sup.8-A.sup.9)-A.sup.10-R.sup.1,
and pharmaceutically-acceptable salts thereof that act as ligands for one or more of the melanocortin receptors, to methods of using such compounds to treat mammals and to pharmaceutical compositions comprising said compounds.
LIQUID INHALATION FORMULATION COMPRISING RPL554
The present invention relates to a liquid pharmaceutical composition suitable for administration by inhalation which comprises a diluent and a suspension of particles of 9,10-dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one (RPL554) or a pharmaceutically acceptable salt thereof. Also described is a liquid pharmaceutical composition according to the invention for use in the treatment of the human or animal body.
Inhalable Formulation
This invention provides a process for preparing an inhalable active pharmaceutical ingredient comprising the steps of heating a suspension of an active pharmaceutical ingredient in a liquefied propellant in a vessel, evaporating the propellant and collecting the resultant powder.