摘要:
Compositions and methods are disclosed for administration of synergistic levels of a diuretic and a natriuretic peptide, especially a recombinant form of human BNP, or hBNP. Theses compositions and methods are useful for the treatment of congestive heart failure.
摘要:
The present invention provides methods and compositions for treating hypertension. The methods generally involve administering a factor which increases angiogenesis and/or vascular permeability. Compositions for use in the methods are also provided.
摘要:
The invention relates to a method of purifying basic fibroblast growth factor. The method involves the use of strong cation exchange chromatography followed by hydrophobic interaction chromatography and then by weak cation exchange chromatography.
摘要:
Compositions and devices for the controlled release delivery of a peptide or protein drug are produced by dispersing a glassy matrix phase comprising the peptide or protein drug and a thermoprotectant in a bioerodable, biocompatible polymer at a temperature that is below the glass transition temperature of the glassy matrix phase and above the melting point of the polymer. The method and composition of the invention may be employed for the local delivery of angiogenic amounts of basic fibroblast growth factor or vascular endothelial growth factor.
摘要:
The invention concerns the use of agonists and antagonists of peripheral-type benzodiazepine receptors (PTBR) in the diagnosis and treatment of cardiac hypertrophy and other circulatory conditions. The invention specifically concerns the use of PTBR antagonists in the prevention or treatment of decompensated cardiac hypertrophy and, eventually, heart failure. The invention also concerns the use of PTBR agonists in the management of conditions calling for increased blood flow or cardiac output, including injury or functional compromise of the heart, increased demand for physical exercise, or an acquired or inherited predisposition to cardiac contractile disfunction. Pharmaceutical compositions for the treatment of such conditions and screening methods to identify PTBR agonists and antagonists are also included.
摘要:
The invention is directed to methods to inhibit TGF-β and/or p38-α kinase using compounds of formula (1) or the pharmaceutically acceptable salts thereof wherein R3 is a noninterfering substituent; each Z is CR2 or N, wherein no more than two Z positions in ring A are N, and wherein two adjacent Z positions in ring A cannot be N; each R2 is independently a noninterfering substituent; L is a linker; n is 0 or 1; and Ar' is the residue of a cyclic aliphatic, cyclic heteroaliphatic, aromatic or heteroaromatic moiety optionally substituted with 1-3 noninterfering substituents.
摘要:
Analogues of the Kunitz Protease Inhibitor (KPI) domain of amyloid precursor protein bind to an inhibit activity of serine proteases, including kallikrein, plasmin and coagulation factors such as factors VIIa, IXa, Xa, XIa, and XIIa. Pharmaceutical compositions containing the KPI analogs, along with methods for using such compositions, are useful for ameliorating and treating clinical conditions associated with increased serine protease activity, such as blood loss related to cardiopulmonary bypass surgery. Nucleic acid sequences encoding these analogs and systems for expression of the peptides of the invention are provided.
摘要:
Compounds of formulae α or β, and the pharmaceutically acceptable salts thereof, wherein each of Z?1 and Z2¿ is independently CR4 or N; where each R4 is independently H or is alkyl (1-6C) or aryl, each of said alkyl or aryl optionally including one or more heteroatoms selected from O, S and N and optionally substituted by one or more of halo, OR, SR, NR¿2?, RCO, COOR, CONR2, OOCR, or NROCR where R is H or alkyl (1-6C), or by one or more CN or =O, or by one or more aliphatic or aromatic 5- or 6-membered rings optionally containing 1-2 heteroatoms; R?1¿ is formula (I); wherein X1 is CO or an isostere thereof; m is 0 or 1; Y is optionally substituted alkyl, optionally substituted aryl, or optionally substituted arylalkyl or two Y taken together may form an alkylene (2-3C) bridge; n is 0 or 2; Z3 is CH or N; X2 is CH, CH¿2? or an isostere thereof; and Ar consists of one or two phenyl moieties directly coupled to X?2¿ optionally substituted by halo, nitro, alkyl(1-6C), alkenyl(1-6C), alkynyl(1-6C), CN or CF¿3?, or by RCO, COOR, CONR2, NR2, OR, SR, OOCR or NROCR wherein R is H or alkyl(1-6C) or by phenyl, itself optionally substituted by the foregoing substituents; R?2¿ is H, or is alkyl(1-6C) or aryl, each or said alkyl or aryl optionally including one heteroatome which is O, S or N, and optionally substituted by one or more of halo, OR, SR, NR¿2?, RCO, COOR, CONR2, OOCR, or NROCR where R is H or alkyl(1-6C), alkynyl(1-6C), or by one or more CN or =O, or by one or more aliphatic or aromatic 5- or 6-membered rings optionally containing 1-2 heteroatoms; R?3¿ is H, halo, NO¿2?, alkyl(1-6C), alkenyl(1-6C), alkynyl(1-6C), CN, OR, SR, NR2, RCO, COOR, CONR2, OOCR, or NROCR where R is H or alkyl(1-6C) are disclosed. These compounds are selective inhibitors of p38α kinase.
摘要:
The invention relates to the design, construction and use of eukaryotic cell lines useful in the identification of inhibitors of β-amyloid processing. More specifically, the invention relates to in vitro assays capable of identifying or quantifying a 4.2 kDa β-amyloid protein. The present invention also provides for DNA and protein molecules for the design, construction and use of eukaryotic cell lines useful in the identification of inhibitors of β-amyloid processing.