摘要:
Pharmaceutical compositions are provided for lowering the activity of HMG-CoA reductase and/or lowering serum cholesterol, comprising an amount effective to lower the activity of HMG-CoA reductase and/or lower serum cholesterol of a side chain derivatized 15-oxygenated sterol having the formula (I): ##STR1## the basic ring structure being saturated or unsaturated, wherein R.sub.1 is --OH, .dbd.O, --OR.sub.7, ##STR2## a sulfate group, a sugar moiety, or a Mg, Na, or K salt of a sulfate group;R.sub.2 is --H, --OH, .dbd.O, mono- or di-halogen, or a C.sub.1 to C.sub.6 alkyl group, which may be unsaturated or substituted with halogen;R.sub.3 is --H, --OH, halogen, or a C.sub.1 to C.sub.6 alkyl group, which may be unsaturated or substituted with halogen;R.sub.4 is nonexistent when there is a double bond between the 8 and 14 carbons or .alpha.H, .beta.H, or an .alpha.C.sub.1 to C.sub.6 alkyl group;R.sub.5 is --OH, .dbd.O, .dbd.NOH, or ##STR3## R.sub.6 is --CH.sub.2 CH(CH.sub.3).sub.2 or CH.sub.2 N(CH.sub.3).sub.2, in which one or more of the hydrogen atoms is replaced by OH or halogen;R.sub.7 is a C.sub.1 to C.sub.6 alkyl group;R.sub.8 is a C.sub.1 to C.sub.20 aliphatic group, which may be substituted or unsubstituted, or a phenyl group; andn is an integer of from 2 to 6; andoptionally a pharmaceutically acceptable carrier or excipient, with the proviso that R.sub.6 is not --CH.sub.2 CH(CH.sub.3)(CH.sub.2 OH). Methods of using the pharmaceutical compositions containing the side chain derivatized 15-oxygenated sterols are also provided.A new process is also provided for preparing side chain derivatized 15-oxygenated sterols. This process includes oxidative cleavage of the saturated side chain of the sterol with trifluoroperacetic acid to give a side chain trifluoroacetate and subsequent hydrolysis of this ester. The resultant side chain alcohol is a valuable and advanced intermediate for the preparation of side chain derivatives of 15-oxygenated sterols.
摘要:
Disclosed herein are methods of doping a patterned substrate in a reaction chamber. The methods may include forming a first conformal film layer which has a dopant source including a dopant, and driving some of the dopant into the substrate to form a conformal doping profile. In some embodiments, forming the first film layer may include introducing a dopant precursor into the reaction chamber, adsorbing the dopant precursor under conditions whereby it forms an adsorption-limited layer, and reacting the adsorbed dopant precursor to form the dopant source. Also disclosed herein are apparatuses for doping a substrate which may include a reaction chamber, a gas inlet, and a controller having machine readable code including instructions for operating the gas inlet to introduce dopant precursor into the reaction chamber so that it is adsorbed, and instructions for reacting the adsorbed dopant precursor to form a film layer containing a dopant source.
摘要:
Methods of depositing a film on a substrate surface include surface mediated reactions in which a film is grown over one or more cycles of reactant adsorption and reaction. In one aspect, the method is characterized by the following operations: (a) exposing the substrate surface to a first reactant in vapor phase under conditions allowing the first reactant to adsorb onto the substrate surface; (b) exposing the substrate surface to a second reactant in vapor phase while the first reactant is adsorbed on the substrate surface; and (c) exposing the substrate surface to plasma to drive a reaction between the first and second reactants adsorbed on the substrate surface to form the film.
摘要:
The present invention relates to a process for the preparation of epothilone analogs by initially forming novel ring-opened epothilones and carrying out a macrolactamization reaction thereon. The subject process is amenable to being carried out in a single reaction vessel without isolation of the intermediate compound and provides at least about a three-fold increase in yield over prior processes for preparing the desired epothilone analogs.
摘要:
Disclosed herein are methods of doping a patterned substrate in a reaction chamber. The methods may include forming a first conformal film layer which has a dopant source including a dopant, and driving some of the dopant into the substrate to form a conformal doping profile. In some embodiments, forming the first film layer may include introducing a dopant precursor into the reaction chamber, adsorbing the dopant precursor under conditions whereby it forms an adsorption-limited layer, and reacting the adsorbed dopant precursor to form the dopant source. Also disclosed herein are apparatuses for doping a substrate which may include a reaction chamber, a gas inlet, and a controller having machine readable code including instructions for operating the gas inlet to introduce dopant precursor into the reaction chamber so that it is adsorbed, and instructions for reacting the adsorbed dopant precursor to form a film layer containing a dopant source.
摘要:
The present invention concerns an enzymatic oxidative deamination process of a dipeptide monomer to prepare an intermediate useful to prepare compounds having endopeptidase and angiotensin converting enzyme inhibition activity.
摘要:
N-protected-L-homocysteine disulfide of the formula ##STR1## or an activated form thereof is reacted with (S)-2-amino-6,6-dimethoxyhexanoic acid, methyl ester to give the disulfide intermediate of the formula ##STR2## Cleavage of the disulfide bond followed by acid catalyzed cyclization produces the N-protected lactam of formula III which is useful for preparing the pharmaceutically active compound omapatrilat.
摘要:
Methods of depositing a film on a substrate surface include surface mediated reactions in which a film is grown over one or more cycles of reactant adsorption and reaction. In one aspect, the method is characterized by intermittent delivery of dopant species to the film between the cycles of adsorption and reaction.
摘要:
Methods of depositing a film on a substrate surface include surface mediated reactions in which a film is grown over one or more cycles of reactant adsorption and reaction. In one aspect, the method is characterized by intermittent delivery of dopant species to the film between the cycles of adsorption and reaction.
摘要:
Methods of depositing a film on a substrate surface include surface mediated reactions in which a film is grown over one or more cycles of reactant adsorption and reaction. In one aspect, the method is characterized by the following operations: (a) exposing the substrate surface to a first reactant in vapor phase under conditions allowing the first reactant to adsorb onto the substrate surface; (b) exposing the substrate surface to a second reactant in vapor phase while the first reactant is adsorbed on the substrate surface; and (c) exposing the substrate surface to plasma to drive a reaction between the first and second reactants adsorbed on the substrate surface to form the film.