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Analysis of Vi saccharides (Thu, 03 Feb 2011)
Salmonella typhi Vi saccharide can be assayed in two new ways. First, its proton NMR spectrum can be used, with comparison to an internal Standard permitting quantitative analysis. Second, anion exchange chromatography with amperometric detection can be used on hydrolysed saccharide.
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ANALYSIS OF VI SACCHARIDES (Thu, 17 Dec 2009)
Salmonella typhi Vi saccharide can be assayed in two new ways. First, its proton NMR spectrum can be used, with comparison to an internal Standard permitting quantitative analysis. Second, anion exchange chromatography with amperometric detection can be used on hydrolysed saccharide.
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Analysis of Vi saccharides (Wed, 08 Jun 2011)
Salmonella typhi Vi saccharide can be assayed in two new ways. First, its proton NMR spectrum can be used, with comparison to an internal Standard permitting quantitative analysis. Second, anion exchange chromatography with amperometric detection can be used on hydrolysed saccharide.
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ANALYSIS OF VI SACCHARIDES (Thu, 17 Dec 2009)
Salmonella typhi Vi saccharide can be assayed in two new ways. First, its proton NMR spectrum can be used, with comparison to an internal Standard permitting quantitative analysis. Second, anion exchange chromatography with amperometric detection can be used on hydrolysed saccharide.
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THIANGAZOLE, IT PREPARATION, COMPOSITIONS AND USE THEREOF (Tue, 26 Jul 1994)
This compound, which has anthelmintic, acaricidal and insecticidal activity is of the formula: Also included is the preparation of the above compound and a compound obtained from the culture broth of the myxobacterium Polyangium spec. DSM 6267, having one or more of the following parameters, or a pharmaceutically acceptable acid addition salt thereof: m.p. 1400C; UV (methanol):��max(���/lg ���)=211 (sh), 218 (sh), 223 (37884/4.578), 228 (sh), 288 (36384/4.561), 300 (sh); (sh = shoulder); IR (CHCl3): 3432 (m), 1664 (s), 1633 (s), 1577 (m), 1567 (m), 1536 (m), 1465 (w), 1449 (w), 1413 (w), 1370 (w), 1168 (m), 1102 (m), 1015 (m), 963, (m) cm-1; (s = strong, m = medium-strength, w = low intensity); 1H-NMR (CDCl3, 300.133 MHz); �� = /.48 (m, 2H), 7.35 (m, 3H), 7.13 (d, 1H, J = 16.2 Hz), 7.04 (d, 1H, J = 16.2 Hz), 6.91 (m, 1H), 3.85 (d, 1H, J = 11.2 Hz), 3.81 (d, 1H, J = 10.6 Hz), 3.74 (d, 1H, J = 11.4 Hz), 3.37 (d, 1H, J = 11.2 Hz), 3.27 (d, 1H, J = 11.4 Hz), 3.20 (d, 1H, J = 11.3 Hz), 2...
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X-RAY STRUCTURE OF HUMAN FPPS AND USE FOR SELECTING FPPS BINDING COMPOUNDS (Thu, 13 Jul 2006)
The present invention relates to crystalline human farnesyl diphosphate synthase (FPPS), to the three-dimensional structure of free FPPS, as well as the three-dimensional structures of FPPS in complex with substrates such as IPP (isopentenyl diphosphate) and/or with inhibitors, such as Zometa~ or Aredia~. Further, methods for preparing crystals of human FPPS are described. According to the invention the crystals can be used to determine the structures of FPPS homologs, mutants, complexes with ligands, FPPS crystal forms and similar molecules of unknown structure. The invention further relates to the use of FPPS crystals to select new FPPS ligands, e.g., by X-ray screening and to design and/or identify inhibitors against FPPS. Furthermore, the invention relates to NMR methods for selecting and/or identifying new low molecular weight binders to FPPS, which represent new therapeutic agents.
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X-ray structure of human FPPS and use for selecting FPPS binding compounds (Thu, 12 Jul 2007)
The present invention relates to crystalline human farnesyl diphosphate synthase (FPPS), to the three-dimensional structure of free FPPS, as well as the three-dimensional structures of FPPS in complex with substrates such as IPP (isopentenyl diphosphate) and/or with inhibitors, such as Zometa® or Aredia®. Further, methods for preparing crystals of human FPPS are described. According to the invention the crystals can be used to determine the structures of FPPS homologs, mutants, complexes with ligands, FPPS crystal forms and similar molecules of unknown structure. The invention further relates to the use of FPPS crystals to select new FPPS ligands, e.g., by X-ray screening and to design and/or identify inhibitors against FPPS. Furthermore, the invention relates to NMR methods for selecting and/or identifying new low molecular weight binders to FPPS, which represent new therapeutic agents.
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X-RAY STRUCTURE OF HUMAN FPPS AND USE FOR SELECTING FPPS BINDING COMPOUNDS (Wed, 10 Oct 2007)
The present invention relates to crystalline human farnesyl diphosphate synthase (FPPS), to the three-dimensional structure of free FPPS, as well as the three-dimensional structures of FPPS in complex with substrates such as IPP (isopentenyl diphosphate) and/or with inhibitors, such as Zometa® or Aredia® Further, methods for preparing crystals of human FPPS are described. According to the invention the crystals can be used to determine the structures of FPPS homologs, mutants, complexes with ligands, FPPS crystal forms and similar molecules of unknown structure. The invention further relates to the use of FPPS crystals to select new FPPS ligands, e.g., by X-ray screening and to design and/or identify inhibitors against FPPS. Furthermore, the invention relates to NMR methods for selecting and/or identifying new low molecular weight binders to FPPS, which represent new therapeutic agents. © KIPO & WIPO 2007
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PROCESSES FOR THE PREPARATION OF 4-OXO-OCTAHYDRO-INDOLE-1-CARBOCYLIC ACID METHYL ESTER AND DERIVATIVES THEREOF (Fri, 29 Jun 2012)
Patent 590753 A process for the production of (3aR, 4S, 7aR)-4-hydroxy-4-m-tolylethynyl-octahydro-indole-1-carboxylic acid methyl ester of the formula (I), which comprises reacting 3-ethynyltoluene with of carbamic acid (2-chloroethyl)(3-oxocyclohexyl)-alkyl ester of formula (III) represented herein, to form the compound of formula (I) and optionally converting the compound of formula (I) to a pharmaceutically acceptable salt, wherein the compound of formula (III) is obtained by cyclisation of 1-carbalkoxy-4-ketoperhydroindole of the formula (II) as shown herein.
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SALT AND SOLVATES OF A TETRAHYDROISOQUINOLINE DERIVATIVE (Wed, 29 May 2013)
(S)-2-(Diphenylacetyl)-1,2,3,4-tetrahydro-6-methoxy-5-(phenylmethoxy)-3-isoquinoline carboxylic acid in substantially pure form is described together with its sodium salt and solvates. Methods for preparing the compound, its sodium salt and its solvates and pharmaceutical compositions comprising them are also described.
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Cyclosporin derivatives, their production and pharmaceutical compositions containing them (Thu, 31 May 1984)
These compounds of formula I in which A is for the title named compounds respectively, formulas II, III, or IV may be prepared by (a) for cyclosporin G cultivating Tolypocladium inflatum Gams NRRL 8044 in a nutrient medium and isolating cyclosporin G, (b) for dihydrocyclosporin G, reducing cyclosporin G, and (c) for iso-cyclosporin G, rearranging cyclosporin G. These compounds exhibit anti-inflammatory and immuno-suppressive activity and pharmaceutical compositions containing them are described and claimed.
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Modified meningococcal fHBP polypeptides (Thu, 05 Jan 2017)
The factor H binding activity of meningococcal fHBP can be uncoupled from its bactericidal sensitivity. NMR studies have identified various amino acid residues involved in the fHBP/fH interaction and one or more of these residues is modified in a fHBP to reduce or eliminate its ability to bind to fH.
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TETRACYCLIC TRITERPENE (Wed, 26 Mar 1997)
Dammara compounds have immunosuppressant and antiinflammatory activity and are useful as pharmaceuticals, particularly for use as immunosuppressant and antiinflammatory agents. 17α dammara compounds are novel and are included per se, for example the compound of formula IC [17α)-23-(E)-dammara-20,23-dien-3β,25-diol] which may be obtained from the flour of the shoots of the Palmyrah palm, Borassus flabellifer L. In addition processes for the synthesis of this and other dammara compounds and intermediates thereof are described.
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MODIFIED MENINGOCOCCAL FHBP POLYPEPTIDES (Thu, 05 May 2011)
The factor H binding activity of meningococcal fHBP can be uncoupled from its bactericidal sensitivity. NMR studies have identified various amino acid residues involved in the fHBP/fH interaction and one or more of these residues is modified in a fHBP to reduce or eliminate its ability to bind to fH.
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MODIFIED MENINGOCOCCAL FHBP POLYPEPTIDES (Thu, 27 Nov 2014)
The factor H binding activity of meningococcal fHBP can be uncoupled from its bactericidal sensitivity. NMR studies have identified various amino acid residues involved in the fHBP/fH interaction and one or more of these residues is modified in a fHBP to reduce or eliminate its ability to bind to fH.
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X-RAY STRUCTURE OF HUMAN FPPS AND USE FOR SELECTING FPPS BINDING COMPOUNDS (Thu, 13 Jul 2006)
The present invention relates to crystalline human farnesyl diphosphate synthase (FPPS), to the three-dimensional structure of free FPPS, as well as the three-dimensional structures of FPPS in complex with substrates such as IPP (isopentenyl diphosphate) and/or with inhibitors, such as Zometa® or Aredia®. Further, methods for preparing crystals of human FPPS are described. According to the invention the crystals can be used to determine the structures of FPPS homologs, mutants, complexes with ligands, FPPS crystal forms and similar molecules of unknown structure. The invention further relates to the use of FPPS crystals to select new FPPS ligands, e.g., by X-ray screening and to design and/or identify inhibitors against FPPS. Furthermore, the invention relates to NMR methods for selecting and/or identifying new low molecular weight binders to FPPS, which represent new therapeutic agents.
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Rapamycin derivatives useful as immunosuppressants (Wed, 25 Mar 1998)
The specification discloses compounds of Formula I wherein variables R1,R3, R4, R5, X and Y are disclosed in the specification and R2 is selected from the following formulae: The compound comprises demethoxy derivatives of rapamycin which have a pharmaceutical use, especially as immunosuppressants.
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HETEROCYCLIC DIONES AS PESTICIDE AND PLANT GROWTH REGULATORS (Tue, 28 Apr 1992)
These compounds which may be used in pesticidal and herbicidal compositions are of the formula: in which any free hydrogen may be replaced by an agriculturally acceptable substituent; and B is an optionally substituted aryl or heteroaryl group.
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USE OF CYCLIC DEPSIPEPTIDES TO INHIBIT KALLIKREIN 7 (Wed, 12 May 2010)
The present application relate to cyclic depsipeptides, or derivatives thereof, having the formula (I), and uses thereof, e.g. as inhibitors of kallikrein 7.
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Novel macrolides and the use thereof (Tue, 28 Mar 1995)
Compounds of this formula are useful in the preparation of a medicament that is suitable for the prophylaxis and treatment of diseases that respond to the inhibition of the osteoclast proton pump: R1 is hydroxy, 2-hydroxyethoxy, C1-C4alkoxy, C1-C4alkanoyloxy, halogen, amino, azido, keto, p-nitrobenzenesulphonyl or pyranyloxy of the formula R3 is hydroxy, C1-C4alkanoyloxy or organic sulphonyloxy, and R4 is hydroxy, C1-C4alkanoyloxy or carbamoyloxy; R2 is hydrogen, hydroperoxy, hydroxy or C1-C4alkoxy; Y is a group of the formula wherein R5 is hydroxy or C1-C4alkanoyloxy, and R6 and R7 are, independently, hydrogen or methyl. Some of these compounds were already known but others are claimed.
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