摘要:
A method of producing β-form thiamine hydrochloride crystals which comprises moistening α-form thiamine hydrochloride crystals in the presence of β-form thiamine hydrochloride crystals as seed crystals and stirring the mixture and a method of producing pharmaceutical preparations containing β-form thiamine hydrochloride crystals which comprises moistening α-form thiamine hydrochloride crystals, together with a binder, with water in the presence of β-form thiamine hydrochloride crystals as seed crystals and stirring the mixture. β-Form thiamine hydrochloride crystals which are stable and resistant to caking and pharmaceutical preparations containing the same can be produced in a simple and easy manner.
摘要:
It has been discovered that certain natural mRNAs serve as metabolite-sensitive genetic switches wherein the RNA directly binds a small organic molecule. This binding process changes the conformation of the mRNA, which causes a change in gene expression by a variety of different mechanisms. Modified versions of these natural "riboswitches" (created by using various nucleic acid engineering strategies) can be employed as designer genetic switches that are controlled by specific effector compounds. Such effector compounds that activate a riboswitch are referred to herein as trigger molecules. The natural switches are targets for antibiotics and other small molecule therapies. In addition, the architecture of riboswitches allows actual pieces of the natural switches to be used to construct new nonimmunogenic genetic control elements, for example the aptamer (molecular recognition) domain can be swapped with other non-natural aptamers (or otherwise modified) such that the new recognition domain causes genetic modulation with user-defined effector compounds. The changed switches become part of a therapy regimen-turning on, or off, or regulating protein synthesis. Newly constructed genetic regulation networks can be applied in such areas as living biosensors, metabolic engineering of organisms, and in advanced forms of gene therapy treatments.
摘要:
The invention describes novel nitrosated and/or nitrosylated cardiovascular compounds or pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated cardiovascular compound, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides novel compositions and kits comprising at,least one cardiovascular compound of the invention, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; and (k) treating nephropathy. The nitrosated and/or nitrosylated cardiovascular compounds are preferably nitrosated and/or nitrosylated P-adrenergic antagonists, nitrosated and/or nitrosylated angiotensinconverting enzyme (ACE) inhibitors, nitrosated and/or nitrosylated anti-hyperlipidemic compounds, and nitrosated and/or nitrosylated antithrombotic and vasodilator compounds.
摘要:
This invention relates 4-amino-azepan-3-ones of formula (1) which are useful as protease inhibitors, particularly of cathepsin S, and as such are useful for preventing a number of diseases amongst which are atherosclerotic lesions and pulmonary diseases such as asthma and allergic reactions.
摘要:
A compound of formula (I): wherein R1 is a C5 to C39 alkyl or alkenyl group and R2 is selected from (a), (b) and (c): wherein one of W, X, Y and Z is a covalent bond and the remaining groups are independently selected from H, M, SO3M and P(O)R3R4 provided at least one of W, X, Y and Z is SO3M or P(O)R3R4; each M is independently a hydrogen ion, an ammonium ion or a metal ion; A is an anion; each of R3 and R4 is independently selected from OH, OM and OR5 wherein R5 may be a C1 to C39 hydrocarbyl group or the residue of a further compound of the present invention including an R2 group of formula (a).
摘要:
It has been discovered that certain natural mRNAs serve as metabolite-sensitive genetic switches wherein the RNA directly binds a small organic molecule. This binding process changes the conformation of the mRNA, which causes a change in gene expression by a variety of different mechanisms. Modified versions of these natural "riboswitches" (created by using various nucleic acid engineering strategies) can be employed as designer genetic switches that are controlled by specific effector compounds. Such effector compounds that activate a riboswitch are referred to herein as trigger molecules. The natural switches are targets for antibiotics and other small molecule therapies. In addition, the architecture of riboswitches allows actual pieces of the natural switches to be used to construct new nonimmunogenic genetic control elements, for example the aptamer (molecular recognition) domain can be swapped with other non-natural aptamers (or otherwise modified) such that the new recognition domain causes genetic modulation with user-defined effector compounds. The changed switches become part of a therapy regimen-turning on, or off, or regulating protein synthesis. Newly constructed genetic regulation networks can be applied in such areas as living biosensors, metabolic engineering of organisms, and in advanced forms of gene therapy treatments.
摘要:
Es wird ein neues Verfahren zur Herstellung von Thiamin beschrieben. Hierbei wird Grewe-Diamin mit einem Orthoameisensäureester erhitzt, das erhaltene Pyrimidinderivat der Formel mit einem Keton der Formel umgesetzt und die so erhaltene Verbindung der Formel in Thiamin übergeführt.
摘要:
Es wird ein neues Verfahren zur Herstellung von Thiamin beschrieben. Hierbei wird Grewe-Diamin mit einem Orthoameisensäureester erhitzt, das erhaltene Pyrimidinderivat der Formel mit einem Keton der Formel umgesetzt und die so erhaltene Verbindung der Formel in Thiamin übergeführt.