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Process for preparing EDTA-free heparins, heparin fractions and fragments (Tue, 05 May 1992)
Heparins, heparin fractions or fragments, optionally salified with pharmaceutically acceptable cations, having molecular weight ranging from 1.000 to 30.000 D, characterized by an EDTA content lower than 0.1%, by the absence, in the .sup.1 H--NMR spectra, of the signals due to EDTA between 2.50 and 4.00 p.p.m. and substantially free from bleeding effect and optionally free from signals, in the .sup.13 C--NMR spectrum, from 80 to 86 ppm.
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CONJUGATES OBTAINED BY REDUCTIVE AMINATION OF SEROTYPE 5 PNEUMOCOCCUS CAPSULAR POLYSACCHARIDE (Thu, 12 Aug 2004)
The invention relates to conjugates obtained by reductive amination of serotype 5 pneumococcus capsular polysaccharide. The reductive amination conditions differ from conventional conditions in that they avoid the creation of an undesired compound which is harmful to the immunogenicity of the conjugates. In carbon NMR spectrometry, the undesired compound is characterized by a resonance signal of 13 -14 ppm. The aminated polysaccharides involved in the production of the conjugates have a carbon NMR spectrum devoid of a resonance signal of 13 -14 ppm. The reductive amination conditions according to the invention are twofold. According to a first method, the reductive amination is performed at a pH which is slightly acidic (4-6, 5) for a maximum of 4 hours. According to a second method, the polysaccharide is initially reduced, then fragmented and finally undergoes the reductive amination per se in conventional or unconventional conditions. According to the method used, the structure of the aminated polysaccharide can vary (conversion or not of the Sug residue of the repeater unit into N-acetyl quinovosamine and N-acetyl fucosamine) but said variations, as recorded in carbon NMR spectrometry, have no effect on immunogenicity.
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Conjugates obtained by reductive amination of serotype 5 pneumococcus capsular polysaccharide (Thu, 21 Jul 2005)
The invention relates to conjugates obtained by reductive amination of serotype 5 pneumococcus capsular polysaccharide. The reductive amination conditions differ from conventional conditions in that they avoid the creation of an undesired compound which is harmful to the immunogenicity of the conjugates. In carbon NMR spectrometry, the undesired compound is characterized by a resonance signal of 13 -14 ppm. The aminated polysaccharides involved in the production of the conjugates have a carbon NMR spectrum devoid of a resonance signal of 13 -14 ppm. The reductive amination conditions according to the invention are twofold. According to a first method, the reductive amination is performed at a pH which is slightly acidic (4-6, 5) for a maximum of 4 hours. According to a second method, the polysaccharide is initially reduced, then fragmented and finally undergoes the reductive amination per se in conventional or unconventional conditions. According to the method used, the structure of the aminated polysaccharide can vary (conversion or not of the Sug residue of the repeater unit into N-acetyl quinovosamine and N-acetyl fucosamine) but said variations, as recorded in carbon NMR spectrometry, have no effect on immunogenicity.
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Conjugates obtained by reductive amination of serotype 5 pneumococcus capsular polysaccharide (Thu, 31 Jul 2008)
Patent 541254 Disclosed are conjugates obtained by reductive amination of serotype 5 pneumococcus capsular polysaccharide. The reductive amination conditions differ from conventional conditions in that they avoid the creation of an undesired compound which is harmful to the immunogenicity of the conjugates. In carbon NMR spectrometry, the undesired compound is characterized by a resonance signal of 13 -14 ppm. The aminated polysaccharides involved in the production of the conjugates have a carbon NMR spectrum devoid of a resonance signal of 13 -14 ppm. The reductive amination conditions are twofold. According to a first method, the reductive amination is performed at a pH which is slightly acidic (4-6.5) for a maximum of 4 hours. According to a second method, the polysaccharide is initially reduced, then fragmented and finally undergoes the reductive amination per se in conventional or unconventional conditions. According to the method used, the structure of the aminated polysaccharide can vary (conversion or not of the Sug residue of the repeater unit into N-acetyl quinovosamine and N-acetyl fucosamine) but said variations, as recorded in carbon NMR spectrometry, have no effect on immunogenicity...
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CONJUGATES OBTAINED BY REDUCTIVE AMINATION OF SEROTYPE 5 PNEUMOCOCCUS CAPSULAR POLYSACCHARIDE (Fri, 23 Sep 2005)
The invention relates to conjugates obtained by reductive amination of serotype 5 pneumococcus capsular polysaccharide. The reductive amination conditions differ from conventional conditions in that they avoid the creation of an undesired compound which is harmful to the immunogenicity of the conjugates. In carbon NMR spectrometry, the undesired compound is characterized by a resonance signal of 13 -14 ppm. The aminated polysaccharides involved in the production of the conjugates have a carbon NMR spectrum devoid of a resonance signal of 13 -14 ppm. The reductive amination conditions according to the invention are twofold. According to a first method, the reductive amination is performed at a pH which is slightly acidic (4-6, 5) for a maximum of 4 hours. According to a second method, the polysaccharide is initially reduced, then fragmented and finally undergoes the reductive amination per se in conventional or unconventional conditions. According to the method used, the structure of the aminated polysaccharide can vary (conversion or not of the Sug residue of the repeater unit into N-acetyl quinovosamine and N-acetyl fucosamine) but said variations, as recorded in carbon NMR spectrometry, have no effect on immunogenicity. © KIPO & WIPO 2007
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Amycomycin, a process for its production and its use as a pharmaceutical (Fri, 19 Dec 2003)
Patent 519400 Described is a compound of the structural formula shown. Also described is a compound of the molecular formula C65H115NO18. characterized by NMR data. Also described is a pharmaceutical composition comprising either of the compounds described above.
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Method of acquiring multidimensional NMR spectra by frequency-dependent folding (Wed, 11 Oct 2006)
The method involves using SHARC (shaped arrayed data acquisition) protocol to acquire multidimensional NMR-spectrum data, and selecting a frequency range with a cluster. The frequency range is selected using successive selective pulses, such that the convolution multidimensional spectrum can be received and assigned in appropriate spectral windows of indirect dimensions. The frequency range selection process and reception and assignment of convolution multidimensional spectra are repeated for several times until the desired frequency ranges are assigned in appropriate spectral windows. An independent claim is included for the use of the multidimensional NMR-spectrum data acquisition method.
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MUMBAISTATIN, A PROCESS FOR ITS PRODUCTION AND ITS USE AS A PHARMACEUTICAL (Wed, 11 Apr 2001)
The present invention relates to a compound named Mumbaistatin which is obtainable by cultivation of the microorganism HIL-008003 (DSM 11641), and to its pharmaceutically acceptable salts and derivatives. Mumbaistatin is a glucose-6-phosphate translocase inhibitor and can be used in the treatment of diabetes mellitus. The present invention further relates to a process for the production of Mumbaistatin, to the microorganism HIL-008003 (DSM 11641), to the use of Mumbaistatin and its pharmaceutically acceptable salts and derivatives as pharmaceuticals, in particular to their use in the treatment of diabetes mellitus, and to pharmaceutical compositions comprising Mumbaistatin or a pharmaceutically acceptable salt or derivative thereof.
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EDTA-free heparins, heparin fractions and fragments, processes for their preparation and pharmaceutical compositions containing them (Thu, 19 Nov 1987)
Heparins, heparin fractions or fragments, optionally salified with pharmaceutically acceptable cations, having molecular weight ranging from 1.000 to 30.000 D, characterized by an EDTA content lower than 0.1%, by the absence, in the <1>H-NMR spectra, of the signals due to EDTA between 2.50 and 4.00 p.p.m. and substantially free from bleeding effect and optionally free from signals, in the <1><3>C-NMR spectrum, from 80 to 86 p.p.m.
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Process for recovering heparinic oligosaccharides with an affinity for cell growth factors (Tue, 23 Jul 1991)
The oligosaccharides of the invention are composed essentially of chains: PA1 possessing a specific affinity for the anionic and cationic cell growth factor which recognize herparin, PA1 comprising at least one sequence of 5 residues matching those present in naturally occurring heparin and possessing a strongly anionic character such as that indicated in the NMR spectrum shown in FIG. 1, as well as their pharmacologically acceptable salts.
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3-aroylindole derivatives and their use as CB2 receptor agonists (Fri, 26 Nov 2004)
Patent 525609 Compounds of formula (I) are disclosed, and their preparation and pharmaceutical compositions containing them. The compounds are CB2 cannabinoid receptor agonists, in which: Ar represents: a) a phenyl mono-, di- or trisubstituted by one or more groups chosen from: a halogen atom, a (C1-C4)alkyl, a trifluoromethyl, an amino, a nitro, a hydroxyl, a (C1-C4)alkoxy, a (C1-C4)alkylsulphanyl or a (C1-C4)alkylsulphonyl; b) a naphthyl which is unsubstituted or substituted once or twice by a halogen atom, a (C1-C4)alkyl or a trifluoromethyl; A represents a C2-C6 alkylene radical; Y represents a group chosen from SR4, SOR4, SO2R4, SO2NR5R6, N(R7)SO2R4, OR4 or NR7SO2NR5R6; R1, R3 and R���3 represent, each independently of one another, hydrogen, a hydroxyl, a halogen atom, a (C1-C4)alkyl, a trifluoromethyl or a (C1-C4)alkoxy; R2 represents hydrogen or a (C1-C4)alkyl; R4 represents a (C1-C4)alkyl or a trifluoromethyl; R5 and R6 each independently represent hydrogen or a (C1-C4)alkyl; R7 represents hydrogen or a (C1-C4)alkyl and its optional salts and/or its solvates...
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CONIOSULPHIDES AND THEIR DERIVATIVES, METHOD FOR THEIR PRODUCTION AND USE AS MEDICAMENTS (Wed, 10 Nov 2004)
The invention relates to compounds of formula (I), which are formed from the micro-organism Coniochaeta ellipsoidea Udagawa, DSM 13856, or from one of its mutations and/or variants during fermentation and which optionally are chemically converted into derivatives. The invention also relates to a method for producing compounds of formula (I) and to the use of the same as medicaments. In addition, the invention relates to the use of a compound of formula (VI) for producing a medicament for the treatment and prophylaxis of degenerative neuropathies or Alzheimer's disease.
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Gabusectin derivatives, method for the production thereof and use of the same (Thu, 14 Aug 2003)
The invention relates to compounds of formula (I) which are formed by the micro-organism ST 003236 (DSM 14476) during fermentation. The invention also relates to a method for producing said compounds and to the derivation thereof, to pharmaceuticals containing a compound of formula (I) and to the use of the same for producing a pharmaceutical.
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HYDROXYPHENYLUNDECANE DERIVATIVES, A PROCESS FOR THEIR PRODUCTION AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM (Tue, 22 Sep 2009)

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Percyquinnin (Thu, 14 Sep 2006)
The present invention relates to a compound named Percyquinnin which is l n obtainable by cultivation of the fungus ST 001837 (DMS 13303), and to its pharmaceutically acceptable salts. The present invention further relates to a process for the production of Percyquinnin, to the microorganism ST 001837 (DSM 13303), to the use of Percyquinnin and its pharmaceutically acceptable O salts as pharmaceuticals, in particular to their use as inhibitor of lipase, and to IN pharmaceutical compositions comprising Percyquinnin or a pharmaceutically 0 10 acceptable salt thereof.
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A METHOD OF LINKING NUCLEOSIDES WITH A SILOXANE BRIDGE (Wed, 28 Oct 1992)
The invention relates to a method of linking nucleosides with a siloxane bridge comprising reaching a 3'-silylated-5'-protected nucleoside with an unprotected nucleoside in the presence of a base catalyst.
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DRECHSLERA ANOLE DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND THEIR USE (Thu, 07 Aug 2008)

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N-SUBSTITUTED HETEROCYCLIC DERIVATIVES, THEIR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS IN WHICH THEY ARE PRESENT (Tue, 29 Oct 1996)
Angiotensin II antagonists have the formula: or a salt thereof. X is O or S. R1 and R2 independently are H, C1-6alkyl, C1-4alkoxy, amino, aminomethyl, carboxy, C1-4alkoxycarbonyl, cyano, tetrazolyl, methyltetrazolyl, methylsulphonylamino, trifluoromethylsulphonylamino, trifluoromethylsulphonylaminomethyl, N-cyanoacetamide, N-hydroxyacetamide, N-(4-carboxy-1,3-thiazol-2-yl)acetamide, ureido, 2-cyano-guanidino-carbonyl, 2-cyano-guanidino-methyl, imidazol-1-ylcarbonyl, or 3-cyano-2-methylisothioureido-methyl; with the proviso that at least one of R1 or R2 is not H. R3 is H, C1-6alkyl (optionally substituted by one or more halogen atoms), C2-6alkenyl, C3-7cycloalkyl, phenyl, phenylC1-3alkyl, phenylC2-3alkenyl. Phenyl is optionally mono- or polysubstituted by halogen, C1-4alkyl, C1-4halogenoalkyl, C1-4polyhalogenoalkyl, OH, or C1-4alkoxy. R4 is C1-6alkyl (optionally substituted by one or more halogen atoms) and R5 is C3-7cycloalkyl, or C3-7cycloalkyl-methyl. Cycloalkyl is optionally substituted by one or more halogen atoms...
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Hydroxyphenylundecane, a process for their production and their use (Thu, 24 Jun 2004)
The present invention relates to novel hydroxyphenylundecane derivatives of the formula (I), embedded image a method for the preparation of said compounds by cultivation of the fungus Cryphonectria parasitica, DSM 14453, and their use as pharmaceuticals, i.e. for the treatment of Alzheimer's Disease, Parkinson's Disease, Huntington's Diseases, stroke, psychosis and/or depressions.
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Process for the preparation of acetyl-amidiniophenylalanyl-cyclohexylglycyl-pyridinioalaninamides (Fri, 27 Feb 2004)
Patent 520427 A process for the preparation of compounds of the formula I, which comprises converting the compound of the formula II by catalytic hydrogenation and conversion of the cyano group into the amidino group into the compound of the formula III or its salt with the acid HX, followed by reaction with a compound of the formula IV or its salt with the acid HX to give a compound of the formula I, where the anions X are physiologically acceptable anions.
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