摘要:
Novel quinazoline derivatives possessing activity as estrogen receptor beta (ERnull) modulators are provided which have the general formula I 1 wherein X is O or S; A and B are each independently CRnullnull or N; R, Rnull and Rnull are each independently hydrogen, alkyl, benzyl, p-methoxybenzyl, allyl, or Si(R4)3, wherein at least one of R, Rnull and Rnull is hydrogen; Rnullnull is hydrogen, halogen, CF3, OR5, S(O)nR6, NR7R8, cycloalkyl or alkyl; R1, R2 and R3 are each independently hydrogen, halogen, CF3, OR5, S(O)nR6, NR7R8, cycloalkyl or alkyl; R4 is a alkyl; R5, R6, R7 and R8 in each functional group are each independently hydrogen, cycloalkyl or alkyl; and n is an integer from 0 to 2. In addition, a method is provided for preventing, inhibiting or treating the progression or onset of pathological conditions associated with the estrogen receptor and to pharmaceutical compositions containing such compounds.
摘要翻译:提供具有雌激素受体β(ERbeta)调节剂活性的新型喹唑啉衍生物,其具有通式I,其中X为O或S; A和B各自独立地为CR“或N; R,R'和R“各自独立地为氢,烷基,苄基,对甲氧基苄基,烯丙基或Si(R4)3,其中R,R'和R”中的至少一个为氢; R“'是氢,卤素,CF 3,OR 5,S(O)n R 6,NR 7 R 8,环烷基或烷基; R 1,R 2和R 3各自独立地为氢,卤素,CF 3,OR 5,S(O)n R 6,NR 7 R 8,环烷基或烷基; R4是烷基; 各官能团中的R 5,R 6,R 7和R 8各自独立地为氢,环烷基或烷基; n为0-2的整数。此外,提供了用于预防,抑制或治疗与雌激素受体相关的病理状况的进展或发作的方法以及含有这些化合物的药物组合物。
摘要:
A biologically active peptide selected from growth factors, peptide hormones, interferons and cytokines and analogues and derivatives thereof, and bearing at least one chelating group linked to an amino group of said peptide, the chelating group being capable of complexing a detectable element and such amino group having no significant binding affinity to target receptors, are complexed with a detectable element and are useful as a pharmaceutical, e.g. a radiopharmaceutical for in vivo imaging of target tissues or for therapy.
摘要:
The invention relates to compositions and methods for use in treating skeletal system disorders in a vertebrate at risk for bone loss, and in treating conditions that are characterized by the need for bone growth, in treating fractures, and in treating cartilage disorders. More specifically, the invention concerns the use of inhibitors of microtubule assembly for enhancing bone growth.
摘要:
A substantially hydrophilic conjugate is provided having a peptide that is capable of passing the blood-brain barrier covalently linked to a water-soluble nonpeptidic polymer such as polyethylene glycol. The conjugate exhibits improved solubility and in vivo stability and is capable of passing the blood-brain barrier of an animal.
摘要:
A composition including one or more growth factors suitable for the treatment of osteogenesis, tenogenesis, or chondrogenesis, wherein the growth factors are obtained from cultured chondrocytes.
摘要:
Methods and compositions are provided for protecting or enhancing erythropoietin-responsive cell, tissue, organ and bodily part function and viability in vivo, in situ or ex vivo in mammals including human beings by systemic or local administration of an erythropoietin receptor activity modulator, such as an erythropoietin.
摘要:
According to the subject invention, dispersible dry powder pharmaceutical-based compositions are provided, including methods for their manufacture and dry powder dispersion devices. A dispersible dry powder pharmaceutical-based composition is one having a moisture content of less than about 10% by weight (% w) water, usually below about 5% w and preferably less than about 3% w; a particle size of about 1.0-5.0 nullm mass median diameter (MMD), usually 1.0-4.0 nullm MMD, and preferably 1.0-3.0 nullm MMD; a delivered dose of about >30%, usually >40%, preferably >50%, and most preferred >60%; and an aerosol particle size distribution of about 1.0-5.0 nullm mass median aerodynamic diameter (MMAD), usually 1.5-4.5 nullm MMAD, and preferably 1.5-4.0 nullm MMAD. Such compositions are of pharmaceutical grade purity.
摘要:
Complexes of a protein selected from the group consisting of VEGF-B167, VEGF-C, VEGF-D and processed VEGF-B186 and analogs thereof and the neuropilin-1 (NP-1) receptor, the extracellular domain or a ligand-binding fragment or analogue thereof; the use of such complexes in assays for growth factor proteins having substantially the same binding affinity for a cell surface receptor as VEGF-B167, VEGF-C, VEGF-D or processed VEGF-B186 and/or in promoting or antagonizing a cellular response mediated by VEGF-B167, VEGF-C, VEGF-D and/or processed VEGF-B186; and specific binding partners, e.g. antibodies, for such complexes.
摘要:
A method of preventing fertility in a non-human animal includes administering a GnRH antagonist to the animal in an amount sufficient to prevent fertility.
摘要:
Modified insulinotropic peptides are disclosed. The modified insulinotropic peptides are capable of forming a peptidase stabilized insulinotropic peptide. The modified insulinotropic peptides are capable of forming covalent bonds with one or more blood components to form a conjugate. The conjugates may be formed in vivo or ex vivo. The modified peptides are administered to treat humans with diabetes and other related diseases.