1468 results about "Methyl Donors" patented technology

Auristatin peptides, including MeVal-Val-Dil-Dap-Norephedrine (MMAE) and MeVal-Val-Dil-Dap-Phe (MMAF), were prepared and attached to Ligands through various linkers, including maleimidocaproyl-val-cit-PAB. The resulting ligand drug conjugates were active in vitro and in vivo.

Based on the above and on the remarkable properties of the 2′-O,4′-C-methylene bridged LNA monomers it was decided to synthesise oligonucleotides comprising one or more 2′-O,4′-C-methylene-β-D-xylofuranosyl nucleotide monomer(s) as the first stereoisomer of LNA modified oligonucleotides. Modelling clearly indicated the xylo-LNA monomers to be locked in an N-type furanose conformation. Whereas the parent 2′-deoxy-β-D-xylofuranosyl nucleosides were shown to adopt mainly an N-type furanose conformation, the furanose ring of the 2′-deoxy-β-D-xylofuranosyl monomers present in xylo-DNA were shown by conformational analysis and computer modelling to prefer an S-type conformation thereby minimising steric repulsion between the nucleobase and the 3′-O-phopshate group (Seela, F.; Wömer, Rosemeyer, H. Helv. Chem. Acta 1994, 77, 883). As no report on the hybridisation properties and binding mode of xylo-configurated oligonucleotides in an RNA context was believed to exist, it was the aim to synthesise 2′-O,4′-C-methylene-β-D-xylofuranosyl nucleotide monomer and to study the thermal stability of oligonucleotides comprising this monomer. The results showed that fully modified or almost fully modified Xylo-LNA is useful for high-affinity targeting of complementary nucleic acids. When taking into consideration the inverted stereochemistry at C-3′ this is a surprising fact. It is likely that Xylo-LNA monomers, in a sequence context of Xylo-DNA monomers, should have an affinity-increasing effect.

The invention discloses polyhexamethylene guanidine propionic acid and preparing method thereof. The preparing method employs stepwise synthesis, which includes steps of: sufficiently mixing dicyandiamide and alanine under high temperature to synthesize aminoguanidine propionic acid, mixing the aminoguanidine propionic acid, triethylidenepropyldiamine and initiator under high temperature to synthesize the polyhexamethylene guanidine propionic acid. Advantages of the invention are: sterilization effect is excellent, toxity is actually nontoxic level, effect of sterilization is better than existent technique, due to overcoming strong hygroscopicity in existence, the polyhexamethylene guanidine propionic acid can be produced to stable powder, thereby being widely used in fields such as weave, plastic, daily chemicals and water treatment.

Elevated levels of homocysteine have been implicated as an important risk factor for cardiovascular and other diseases. A composition for decreasing levels of plasma homocysteine and a method for administering the composition are provided, the composition containing dextromethorphan (DM), folic acid and vitamins B6 and B12. The composition provides a synergistic therapeutic effect so that lower amounts of the above ingredients may be employed to minimize any undesirable side effects caused by the use of high levels of a component such as DM. Preferred compositions for cardiovascular diseases further include lecithin, vitamin E, betacarotene, procyanidins/flavonoids, trimethylglycine, garlic oil and minerals. Other compositions for treating glaucoma include bilberry, bioflavonoids and beta-carotene and for treating tardive dyskinesia include an antioxidant such a grape seed extract and pine bark extract, lecithin and oligomeric proanthocyanidins. The compositions may be administered using any suitable means such as orally or intravenous.

Salts and crystalline forms of 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}-sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide are suitable active pharmaceutical ingredients for pharmaceutical compositions useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.

The present invention provides a compound of the formula: wherein ring A is an optionally substituted 5 to 10-membered aromatic ring; R¹ and R² are the same or different and each is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X is a bond and the like; and L is a divalent hydrocarbon group, and a salt thereof, except 3-(aminomethyl)-2,6,7-trimethyl-4-phenyl-1(2H)-isoquinolinone, 3-(aminomethyl)-2-methyl-4-phenyl-1(2H)-isoquinolinone, 3-(aminomethyl)-6-chloro-2-methyl-4-phenyl-1(2H)-isoquinolinone and 3-(aminomethyl)-2-isopropyl-4-phenyl-1(2H)-isoquinolinone. The compound shows a superior peptidase-inhibitory activity and is useful as an agent for the prophylaxis or treatment of diabetes and the like.

This invention relates to combinations comprising 3-[(R)-2-(N,N-dimethylamino)ethylthio-Sar]-4-(gammahydroxymethylleucine)cyclosporine, or a pharmaceutically acceptable salt, solvate or hydrate thereof; and certain nucleoside analogues, and their use in the treatment of hepatitis C virus.

Methylotrophic or methanotrophic bacteria such as Methylobacterium are transformed with a gene of interest, and expression of the gene is regulated by means of a cumate repressor protein and an operator sequence which is operatively linked to the gene of interest, and the addition of an external agent. Specifically, the cymR repressor and cmt operator from Pseudomonas putida may serve to regulate gene expression in methylotrophic or methanotrophic bacteria with the addition of cumate.

The present invention relates to a combination therapy for treating an HIV infection or inhibiting integrase comprising (S)-6-(3-Chloro-2-fluorobenzyl)-1-(1-hydroxymethyl-2-methylpropyl)-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (“Compound A”) or a pharmaceutically acceptable solvate or salt thereof in combination with at least one other anti-HIV agent. In some embodiments of the present invention, the other anti-HIV agents are chosen from reverse transcriptase inhibitors and protease inhibitors. In certain embodiments of the present invention, the other anti-HIV agents are chosen from AZT, 3TC, PMPA, efavirenz, indinavir, nelfinavir, a combination of AZT/3TC, and a combination of PMPA/3TC. Since Compound A has a high inhibitory activity specific for integrases, when used in combinations with other anti-HIV agents it can provide a combination therapy with fewer side effects for humans.

The invention relates to a preparation method and application of a formaldehyde fluorescent probe, and belongs to the technical field of analytical chemistry. The formaldehyde fluorescent probe is a ratio-type fluorescent probe with double emission bands. The excitation wavelength is 318 nm; and the fluorescence peak at 359nm decreases gradually with the increasing of the concentration of formaldehyde, and at the same time a new emission band is produced at 451 nm and the fluorescence peak gradually increases. The formaldehyde fluorescent probe can resist the interference of acetaldehyde, glyoxal, methylglyoxal, benzaldehyde, alanine, glycine, serine, arginine, cysteine, glutathione and glucose, has high detection accuracy, high sensitivity and strong anti-interference capability. In addition, the formaldehyde fluorescent probe of the invention can detect the formaldehyde in a biological sample (cell environment), realizes formaldehyde fluorescence imaging in living cell level, and has potential practical application value. The synthesis of the formaldehyde fluorescent probe only needs a one-step reaction, which is simple and high in yield.

Cosmetic, dermatological and dietary compositions for treatment of aging of the skin are provided that contain a compound useful in promoting skin health and youthful appearance, such as extract of Lotus in combination with methyl donors, in a suitable carrier or vehicle along with methods of treatment to reduce signs of aging such as loss of elasticity, age spots, enlarged pores, fine lines, wrinkles and to promote over-all younger looking skin by using said compositions to help repair damage and to help neutralize free radicals.

The present invention discloses filter paper sheet gas chromatography-mass spectrum analysis process of organic acid/amino acid metabolic product in urine. The process includes elution of urine collected with filter paper, oximation reaction, extraction, methyl silane derivation, and united detection with chromatographic instrument and mass spectrograph. The process of the present invention is superior in that the filter paper collection of urine favors remote analysis of genetic metabolic diseases; the oximation reaction processing favors alpha-ketonic acid detection for diagnosis of branched chain ketonic acid metabolic disorder; the extraction has high recovery rate of organic acid/amino acid metabolic product, high repeatability, less chromatographic impurity peaks and no pollution to chromatographic capillary column and mass spectrographic ion source; and the united detection is suitable for screening analysis of great amount of samples.

The invention provides certain benzoxazine compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R¹, R², R^a, R^b, R^c, R^d, R^g, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT.