Patent classifications
A61P5/10
Methods of use and combinations
The present invention relates to a compound of Formula 1, 2 or 3: ##STR00001##
wherein A is N or CR.sub.0, where R.sub.0 is hydrogen, C.sub.1-C.sub.6 linear or branched chain alkyl, etc., Z is CR.sub.e, or, N, where R.sub.e is hydrogen, C.sub.1-C.sub.6 linear or branched chain alkyl, etc.; R.sub.1 is hydrogen, C.sub.1-C.sub.6 linear or branched chain alkyl, etc.; R.sub.2 are independently hydrogen or C.sub.1-C.sub.6 linear or branched chain alkyl; R.sub.3 and R.sub.4 are independently hydrogen, C.sub.1-C.sub.6 linear or branched chain alkyl, etc.; R.sub.5 and R.sub.6 are independently hydrogen or C.sub.1-C.sub.6 linear or branched chain alkyl, etc.; R.sub.8 is hydrogen, C.sub.1-C.sub.6 linear or branched chain alkyl, etc.; R.sub.9 and R.sub.10 are independently hydrogen or C.sub.1-C.sub.6 linear or branched chain alkyl, etc.; Q is CO, (CH.sub.2).sub.q, (CHR.sub.s).sub.q, or (CR.sub.sR.sub.t).sub.q, where R.sub.s and R.sub.t are independently C.sub.1-C.sub.6 linear or branched chain alkyl, aryl, alkylaryl, heteroaryl or alkylheteroaryl; where q is 0, 1, 2, or 3; and, where n is 0, 1, 2, 3, 4 or 5; or, a pharmaceutically acceptable salt thereof, for the treatment of certain diseases, particularly those affected or mediated by the androgen receptor; to combinations comprising such compounds with a second pharmaceutically active ingredient; to compositions containing such combinations; and to such combinations for the treatment of various diseases, particularly, those affected or mediated by the androgen receptor.
MUTANT ADENO-ASSOCIATED VIRUS VIRIONS AND METHODS OF USE THEREOF
The present invention provides mutant adeno-associated virus (AAV) that exhibit altered capsid properties, e.g., reduced binding to neutralizing antibodies in serum and/or altered heparin binding and/or altered infectivity of particular cell types. The present invention further provides libraries of mutant AAV comprising one or more mutations in a capsid gene. The present invention further provides methods of generating the mutant AAV and mutant AAV libraries, and compositions comprising the mutant AAV. The present invention further provides recombinant AAV (rAAV) virions that comprise a mutant capsid protein. The present invention further provides nucleic acids comprising nucleotide sequences that encode mutant capsid proteins, and host cells comprising the nucleic acids. The present invention further provides methods of delivering a gene product to an individual, the methods generally involving administering an effective amount of a subject rAAV virion to an individual in need thereof.
Peptidomimetic macrocycles
The present invention provides peptidomimetic macrocycles capable of modulating growth hormone levels and methods of using such macrocycles for the treatment of disease.
PRODUCTION OF ACTIVATED CLOSTRIDIAL NEUROTOXINS
The present invention relates to a method of producing activated clostridial neurotoxins that are essentially free of unactivated products, to compositions comprising such and to their use in therapy.
MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS
The present invention relates to modulators of ATP-Binding Cassette (ABC) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
Compositions for an orally active 1,2,4-oxadiazole for the treatment of disease
The present invention relates to specific doses of and dosing regimens for using a 1,2,4-oxadiazole benzoic acid compound in treating or preventing diseases associated with nonsense mutations. In particular, the invention relates to specific doses and dosing regimens for the use of 3-[5-(2-fluoro-phenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid in mammals having diseases associated with nonsense mutations.
METHOD OF MANUFACTURING A PHARMACEUTICAL COMPOSITION
A method of manufacturing oxytocin or oxytocin receptor agonist comprising a step of combining an antisolvent with a solution comprising oxytocin or oxytocin receptor agonist so as to precipitate a product oxytocin or a product oxytocin receptor agonist from the solution.
Leuprolide injection
The present invention provides a sterile solution comprising leuprolide acetate in a pharmaceutically acceptable vehicle, wherein solution is present as a reservoir in a multiple dose pen injection device, the device being adapted to subcutaneously inject a portion of the said reservoir in a single daily dose and further being adapted to provide multiple portions of solution said while the reservoir remains sterile.
IgG Fc fragment for a drug carrier and method for the preparation thereof
Disclosed is an IgG Fc fragment useful as a drug carrier. A recombinant vector expressing the IgG Fc fragment, a transformant transformed with the recombinant vector, and a method of preparing an IgG Fc fragment are disclosed. When conjugated to a certain drug, the IgG Fc fragment improves the in vivo duration of action of the drug and minimizes the in vivo activity reduction of the drug.
PYRROLIDINE DERIVATIVES AS OXYTOCIN/VASOPRESSIN V1A RECEPTORS ANTAGONISTS
The present invention relates to a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2-methyl-1,1-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-methl9243yloxime, and/or an active metabolite thereof having antagonist action at the oxytocin receptor and/or vasopressin V1a receptor, to processes for their preparation, pharmaceutical compositions containing them and their use.