摘要:
The present invention relates to novel cationic lipids, transfection agents, microparticles, nanoparticles, and short interfering nucleic acid (siNA) molecules. The invention also features compositions, and methods of use for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of gene expression and/or activity in a subject or organism. Specifically, the invention relates to novel cationic lipids, microparticles, nanoparticles and transfection agents that effectively transfect or deliver biologically active molecules, such as antibodies (e.g., monoclonal, chimeric, humanized etc.), cholesterol, hormones, antivirals, peptides, proteins, chemotherapeutics, small molecules, vitamins, co-factors, nucleosides, nucleotides, oligonucleotides, enzymatic nucleic acids, antisense nucleic acids, triplex forming oligonucleotides, 2,5-A chimeras, dsRNA, allozymes, aptamers, decoys and analogs thereof, and small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double- stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules, to relevant cells and/or tissues, such as in a subject or organism. Such novel cationic lipids, microparticles, nanoparticles and transfection agents are useful, for example, in providing compositions to prevent, inhibit, or treat diseases, conditions, or traits in a cell, subject or organism. The compositions described herein are generally referred to as formulated molecular compositions (FMC) or lipid nanoparticles (LNP).
摘要:
The invention provides methods to treating conditions such as prostate cancer, or for ameliorating one or more symptoms associated with prostate cancer, or for agents that modulate the biological activity of the androgen receptor. The invention also provides methods and compositions suitable for therapeutic applications.
摘要:
Novel and anti-estrogenic compounds are provided which are useful to treat a variety of disorders, particularly estrogen-dependant disorders. Preferred compounds have 1,3,5-estratiene nucleus, and are substituted at the C-17 or C-11 position with a molecular moiety which renders the compounds effective to competitively block the binding of estrogen to its receptor. Particularly preferred compounds are 17-desoxy-1,3,5-estratienes. Therapeutic methods and pharmaceutical compositions are provided as well.
摘要:
A compound of formula (I) and pharmaceutical acceptable salts, solvates, stereoisomers and prodrugs thereof, in isolation or in mixture, wherein, independently at each occurrence: R?1 and R2¿ are selected from hydrogen, oxygen so as to form nitro or oxime, amino, sulfate, and sulfonic acid, and organic groups having 1-30 carbons and optionally containing 1-6 heteroatoms selected from nitrogen, oxygen, phosphorous, silicon, and sulfur, where R?1 and R2¿ may, together with the N to which they are both bonded, form a heterocyclic structure that may be part of an organic group having 1-30 carbons and optionally containing 1-6 heteroatoms selected from nitrogen, oxygen and silicon, and where R1 may be a 2, or 3 atom chain to numeral 2 so that —N-R1 - forms part of a fused bicyclic structure to ring A; R?3 and R4¿ are selected from direct bonds to 6 and 7 respectively so as to form carbonyl groups, hydrogen, or a protecting group such that R3 and/or R4 is part of hydroxyl or carbonyl protecting group; numerals 1 through 17 each represent a carbon having substitution as described. The compounds may be formulated into pharmaceutical compositions, and used in the treatment and/or prevention of various conditions, including inflammation, asthma, an allergic disease, chronic obstructive pulmonary disease, atopic dermatitis, solid tumors, AIDS, ischemia, and cardiac arrhythmias.
摘要:
A pharmaceutical composition contains an extract obtainable from a plant of the genus Trichocaulon or Hoodia containing an appetite suppressant agent having the formula (1). A process for obtaining the extract and a process for synthesizing compound (1) and its analogues and derivatives is also provided. The invention also extends to the use of such extracts and compound (1) and its analogues for the manufacture of medicaments having appetite suppressant activity. The invention further provides novel intermediates for the synthesis of compound (1).
摘要:
The present invention relates to a surface cutting apparatus for hot-rolled steel products for cutting the top and bottom surfaces of a hot-rolled steel product continuously or intermittently by passing said steel product between a pair of rotary drums (38a,38b) rotating in the direction reverse to each other, said apparatus having a disk (39a,39b) for recognizing a gap between the rotary drums (38a,38b), which has a diameter larger than that of said rotary drum, at both ends or one end of at least one rotary drum (38a,38b).
摘要:
Extracts obtainable from Hoodia gordonii or lugardii containing an appetite suppressant agent having the formula (1) are disclosed for the manufacture of medicaments having appetite suppressant activity.
摘要:
Steroid sulfatase inhibitors containing as the active ingredient estra-1,3,5(10)-triene derivatives represented by the following general formula (I) or pharmacologically acceptable salts thereof: (I) wherein R?1 and R2¿ are the same or different and each represents hydrogen, lower alkyl, etc.; R3 represents hydrogen, etc.; R4 represents hydrogen, etc.; R5 represents hydrogen, etc.; and R6 represents cyano, amino, COR53 (wherein R53 represents substituted lower alkyl, etc.), optionally substituted aryl, an optionally substituted heterocycle, etc.
摘要:
Steroid derivatives of this invention interact with nuclear liver X receptor (LXR) and ubiquitous receptor (UR) and can be used to treat a variety of LXR- or UR-mediated disorders.
摘要:
A steroidal compound or a salt thereof having the following general formula: €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ A-B-C-N(O) 2 €ƒ€ƒ€ƒ€ƒ€ƒ(I) for the treatment of oxidative stress.