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A syn-isomer of a thiazolyl intermediate (Mon, 26 May 1997)
A stable crystalline syn-isomer of 2-(2-aminothiazol-4-yl)-2-methoxyimino acetyl chloride hydrochloride is substantially free of the anti-isomer and has the formula:
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Protein-ligand NOE matching for high-throughput structure determination (Tue, 03 Apr 2012)
A method of enhancing the throughput and applicability of NMR-based structure determination of protein-ligand complexes is disclosed. The method circumvents the need for protein sequence-specific resonance assignments and combines NMR data analysis and ligand docking methods into an integrated process. In one embodiment, NMR data is used to filter docking results to identify the most consistent binding modes, thereby providing structural information in a high-throughput fashion without the need for assigning protein resonances. Trial assignments for protein-ligand nuclear Overhauser effect (NOE) interactions are also produced by the method.
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MODIFIED FORMS OF HEPATITIS C VIRUS NS3 PROTEASE (Thu, 13 Jul 2000)
The present invention relates to modified Hepatitis C NS3 proteases and modified Hepatitis C NS4a-NS3 fusion proteases. These proteins are highly soluble and are useful for NMR spectroscopy, X-ray crystallography, and inhibitor screening. DNA constructs are also provided.
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Method of molecular structure recognition (Thu, 21 Nov 2002)
An analytical method and apparatus using principal component analysis of nuclear magnetic resonance (NMR) data for rapid molecular structure/function pattern recognition. The presence of a molecular substructure in an organic compound is determined by comparing principal components calculated from chemical shift values of the substructure in selected compounds with those calculated from the chemical shift values of the organic compound. Alternatively, principal components are calculated from the intensities of NMR signals for a full spectrum, or selected regions thereof, to determine whether an organic compound belongs to or is excluded from a set of structurally related compounds. Also, the presence of a pharmacophore in an organic compound can be determined by comparing the principal components derived from data on a set of compounds known to bind to a particular receptor, or have a common biological effect, with the principal components of the data set of the organic compound.
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METHOD OF MOLECULAR STRUCTURE RECOGNITION (Thu, 07 Nov 2002)
An analytical method and apparatus using principal component analysis of nuclear magnetic resonance (NMR) data for rapid molecular structure/function pattern recognition. The presence of a molecular substructure in an organic compound is determined by comparing principal components calculated from chemical shift values of the substructure in selected compounds with those calculated from the chemical shift values of the organic compound. Alternatively, principal components are calculated from the intensities of NMR signals for a full spectrum, or selected regions thereof, to determine whether an organic compound belongs to or is excluded from a set of structurally related compounds. Also, the presence of a pharmacophore in an organic compound can be determined by comparing the principal components derived from data on a set of compounds known to bind to a particular receptor, or have a common biological effect, with the principal components of the data set of the organic compound.
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Methods for the in vivo measurement of the concentration of NMR-detectable xenobiotic compounds (Thu, 14 Sep 1995)

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Antibiotic produced by Bacillus subtilis ATCC 55422 capable of inhibiting bacteria (Tue, 15 Nov 1994)
The invention is drawn to an antibiotic produced by Bacillus subtilis ATCC 55422 having a nominal molecular weight of 580 and the empirical formula C.sub.35 H.sub.48 O.sub.7, or a salt thereof. The antibiotic is useful in inhibiting the growth of bacteria, including Escherichia, Klebsiella, Proteus, Serratia, Bacillus and Staphylococcus.
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Synthesis of paclitaxel baccatin III by protecting the 7-hydroxyl using a strong base and an electrophile (Thu, 18 Nov 1999)
Process for synthesizing paclitaxel by treating baccatin III with a strong base in a solvent, adding an electrophile to the solution to form a 7-O-protected baccatin III derivative, reacting the 7-O-protected baccatin III derivative with a protected paclitaxel sidechain in a solvent such that the protected paclitaxel sidechain is coupled to the 13-hydroxyl of the 7-O-protected baccatin III, and subsequently deprotecting the protected paclitaxel sidechain and the 7-O protecting group to form paclitaxel, and intermediates used therein.
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NEW ANTITUMOR ANTIBIOTIC (Wed, 26 Oct 1994)
The invention includes a compound BMY-46164 isolated from a fermentation product of Actinomadura strain Q473-8, which compound has an empirical formula of C40H43N2O12Cl and a molecular weight of 778, or an acid or base addition salt thereof. Also included is a pharmaceutical composition comprising an antitumour or antibiotic amount of the above compound and one or more pharmaceutically acceptable excipients, a process for producing a pharmaceutically active compound derived from the fermentation of Actinomadura strain Q473-8, a biologically pure culture containing the above compound and a biologically pure concentrate containing a carrier and the above compound.
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A NOVEL ALPHA-(N-SULFONAMIDO)ACETAMIDE COMPOUND AS AN INHIBITOR OF BETA AMYLOID PEPTIDE PRODUCTION (Fri, 29 Apr 2011)
Patent 584545 Disclosed is the compound(2R)-2-[[(4-chlorophenyl)sulfonyl][[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoropentanamide. The use of the above compound for the manufacture of a medicament for treating Alzheimer���s disease, cerebral amyloid angipathy, mild cognitive impairment and/or Down syndrome is also disclosed. The process for preparing the said compound, as well as its intermediates, is also disclosed.
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7-0-ethers of taxane derivatives (Thu, 19 Mar 1998)

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ANTITUMOR ANTIBIOTIC, ITS PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING IT (Thu, 20 Nov 1997)

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Antitumor antibiotic (Tue, 03 Jan 1995)
A certain fermentation product of Actinomadura strain Q473-8 yield, when suitably treated, a novel compound having both antibiotic and antitumor activities.
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KEDARCIDIN ANTITUMOR CHROMOPHORE (Wed, 26 Jan 1994)
It is said that kedarcidin chromophore has the formula: It is prepared by eluting kedarcidin antibiotic through a silica gel column using benzene-methanol as eluant. The antibiotic is prepared by fermenting Streptoalloteichus sp. nov. strain L585-6 (ATCC 53650) and the chromophore moiety is reputed to have tumour-inhibiting properties. The chromophore is characterised by the following properties: (a) appears as a buff-coloured amorphous solid; (b) has a molecular weight of 1029 as determined by mass spectroscopy; (c) has the molecular formula C53H60N3O16Cl; (d) exhibits in silica gel thin layer chromatography an Rf value of 0.29 with the solvent system benzene-methanol (9:2 v/v) and an Rf value of 0.16 with the solvent system benzene-methanol (9:1 v/v); and (e) exhibits a high performance liquid chromatography retention time of 12 minutes with a C18 reversed phase silica gel column and the solvent system tetrahydrofuran - 0.2M aqueous ammonium acetate (2:3 v/v). The characterisation also includes IR, UV and proton and carbon-13 magnetic resonance spectra as described in the specification...
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Antitumor antibiotic (Tue, 19 Apr 1994)
A certain fermentation product of Actinomadura strain Q473-8 yields, when suitably treated, a novel compound having both antibiotic and antitumor activities.
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PREPARATION OF A CEPHALOSPORIN ANTIBIOTIC USING THE SYN-ISOMER OF A THIAZOLYL INTERMEDIATE (Fri, 24 Jan 1997)

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MODIFIED FORMS OF HEPATITIS C VIRUS NS3 PROTEASE (Thu, 13 Jul 2000)
The present invention relates to modified Hepatitis C NS3 proteases and modified Hepatitis C NS4a-NS3 fusion proteases. These proteins are highly soluble and are useful for NMR spectroscopy, X-ray crystallography, and inhibitor screening. DNA constructs are also provided.
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Modified forms of hepatitis C virus NS3 protease (Thu, 28 Sep 2000)
The present invention relates to modified Hepatitis C NS3 proteases and modified Hepatitis C NS4a-NS3 fusion proteases. These proteins are highly soluble and are useful for NMR spectroscopy, X-ray crystallography, and inhibitor screening. DNA constructs are also provided.
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ANTITUMOR ANTIBIOTIC FROM ACTINOMADURA (Wed, 28 Apr 1993)
A certain fermentation product of Actinomadura strain Q473-8 yields, when suitably treated, a novel compound having both antibiotic and antitumor activities.
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Alicyclic phospholipase A2 inhibitors (Fri, 20 Dec 1996)
The specification relates to derivatives of formula where X is H, F, Cl, Br, I COOR'', CONH2, COR''', CHO, CH2OH, CH2OR''', OH, OR''', CF3, alkyl, alkenyl, haloalkyl, NO2, P(O)(OH)2, SO2H or SO3H; R is optionally substituted alkyl, aryl, aralkyl, alkenyl or aralkenyl, each with at least 6 carbon atoms, with trhe proviso that R is not R1 is H or alkyl; R'' is H, alkyl, C(R3)2OC(O)R4, CH2CH2NR5R6, CH2CH2CH2NR5R6 or CH2C(O)N(R6)2; R''' is alkyl; R3 is H, methyl, ethyl or propyl; R4 is aryl, alkyl, cycloalkyl, alkoxy or cycloalkoxy; and R5 and R6 are independently alkyl, or R5 and R6 together form cycloalkyl or CH2CH2OCH2CH2. The derivatives are phospholipase A2 inhibitors with antinflammatory effects.
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