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METHOD FOR ENHANCING NMR CHEMICAL STRUCTURE DETERMINATION (Fri, 18 Apr 2003)A method for enhancing the NMR spectroscopy structural analysis of compounds and particularly the structural analysis of compounds used in developing viable drugs, by increasing signal to noise (S/N) ratio of obtained spectra by collecting and storing NMR in a standard data matrix and generating a point by point weighting function for each dimension of the matrix.
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Method for enhanced NMR chemical structure determination (Fri, 05 Dec 2003)
A method for enhancing the NMR spectroscopy structural analysis of compounds and particularly the structural analysis of compounds used in developing viable drugs, by increasing signal to noise (S/N) ratio of obtained spectra by collecting and storing NMR in a standard data matrix and generating a point by point weighting function for each dimension of the matrix.
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Method for enhancing NMR chemical structure determination (Thu, 24 Apr 2003)
A method for enhancing the NMR spectroscopy structural analysis of compounds and particularly the structural analysis of compounds used in developing viable drugs, by increasing signal to noise (S/N) ratio of obtained spectra by collecting and storing NMR in a standard data matrix and generating a point by point weighting function for each dimension of the matrix..
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Fluorine NMR spectroscopy for biochemical screening (Fri, 04 Mar 2005)
High-Throughput Screening (HTS) of large compound libraries is the method of drug-lead discovery. It is now well accepted that for a functional assay, quality is more important than quantity. A biochemical NMR method originally proposed by Percival and Withers (Biochemistry, 1992, 31, 498–505) is extended to the screening of Ser/Thr kinases. The method requires the presence of a CF3 (or CF) moiety on the substrate and utilizes 19F NMR spectroscopy for the detection of the starting and enzymatically modified substrates. Experiments can be performed in real time or in an endpoint assay format using protein and substrate concentrations comparable to the ones used by other HTS techniques. Application of this technique to the phosphorylation of a substrate by the protein Ser/Thr kinase AKT1 is presented.
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Fluorine NMR spectroscopy for biochemical screening (Fri, 26 Sep 2008)
High-Throughput Screening (HTS) of large compound libraries is the method of drug-lead discovery. It is now well accepted that for a functional assay, quality is more important than quantity. A biochemical NMR method originally proposed by Percival and Withers (Biochemistry, 1992, 31, 498-505) is extended to the screening of Ser/Thr kinases. The method requires the presence of a CF3 (or CF) moiety on the substrate and utilizes 19F NMR spectroscopy for the detection of the starting and enzymatically modified substrates. Experiments can be performed in real time or in an endpoint assay format using protein and substrate concentrations comparable to the ones used by other HTS techniques. Application of this technique to the phosphorylation of a substrate by the protein Ser/Thr kinase AKT1 is presented.
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METHOD FOR ENHANCING NMR CHEMICAL STRUCTURE DETERMINATION (Fri, 25 Apr 2003)
A method for enhancing the NMR spectroscopy structural analysis of compounds and particularly the structural analysis of compounds used in developing viable drugs, by increasing signal to noise (S/N) ratio of obtained spectra by collecting and storing NMR in a standard data matrix and generating a point by point weighting function for each dimension of the matrix.
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Crystal forms of azithromycin (Sat, 29 Oct 2005)
Patent 529118 Disclosed is a crystalline form G of azithromycin, having a 13C solid state NMR spectrum comprising peaks with chemical shifts of 179.5 ppm - being a single peak with a splitting of 0-3 ppm; 10.4 ppm; 9.9 ppm; 7.6 ppm; 6.5 ppm; wherein the peaks may show variation of chemical shift of +/- 0.2 ppm. Also disclosed is a method of preparing form G, comprising the steps of dissolving azithromycin in a 1:1 mixture of water and methanol to form a mixture and heating the mixture to between 45��C to 55��C for between 4 hours to 5 hours, and then cooling to produce form G azithromycin.
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Method for enhancing nmr chemical structure determination (Fri, 21 Feb 2003)
A method for enhancing the NMR spectroscopy structural analysis of compounds and particularly the structural analysis of compounds used in developing viable drugs, by increasing signal to noise (S/N) ratio of obtained spectra by collecting and storing NMR in a standard data matrix and generating a point by point weighting function for each dimension of the matrix.
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SOLID FORMS OF A MACROCYCLIC KINASE INHIBITOR (Thu, 05 May 2016)
This invention relates to crystalline solvates of (10R)-7-amino-12-fluoro-2,10,16- trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benz- oxadiazacyclotetradecine-3-carbonitrile, useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to pharmaceutical compositions comprising such crystalline solvates, and to methods of using such solvates and compositions in the treatment of abnormal cell growth in mammals, especially humans.
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CRYSTALLINE FORM OF LORLATINIB FREE BASE (Wed, 01 Feb 2017)
This invention relates to a crystalline form of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4- (metheno)pyrazolo[4,3-h][2,5,11]benzoxadiazacyclo-tetradecine-3-carbonitrile (lorlatinib) free base (Form 7). This invention also relates to pharmaceutical compositions comprising Form 7.
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Crystalline form of lorlatinib free base (Fri, 10 Feb 2017)
This invention relates to acrystalline form of (10R)-7-amino-12-fluoro-2,10,16-trimethyl- 5-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benzoxadiazacyclo- tetradecine-3-carbonitrile (lorlatinib) free base (Form 7). This invention also relates to pharmaceutical compositions comprising Form 7, and to methods of using Form 7 and such compositions in the treatment of abnormal cell growth, such as cancer, in a mammal.
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SALTS AND POLYMORPHS OF 8-FLUORO-2-{4-[(METHYLAMINO}METHYL]PHENYL}-1,3,4,5-TETRAHYDRO-6H-AZEPINO[5,4,3-CD]INDOL-6-ONE (Thu, 20 Dec 2012)
The present invention relates to novel polymorphic forms of 8-fluoro-2-{4- [(methylamino)methyl]phenyf}-1,3,4,5-tetrahydro-6H-azepino(5,4,3-cd]indol-6-one;(I), and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer.
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CRYSTALLINE FORMS OF 1-((2R,4R)-2-(1H-BENZO[D]IMIDAZOL-2-YL)-1-METHYLPIPERIDIN-4-YL)-3-(4-CYANOPHENYL)UREA MALEATE (Wed, 03 Jan 2018)
This invention relates to a crystalline form of 1-((2R,4R)-2-(1H-benzo[d]imidazol- 2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea maleate, and to pharmaceutical compositions thereof, to intermediates and methods for the production and isolation of such crystalline forms and compositions, and to methods of using such crystalline forms and compositions in the treatment of abnormal cell growth in mammals, especially humans.
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CRYSTALLINE FORM OF LORLATINIB FREE BASE (Fri, 24 Aug 2018)
This invention relates to acrystalline form of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-5-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h] [2,5,11]benzoxadiazacyclo-tetradecine-3-carbonitrile (lorlatinib) free base (Form 7). This invention also relates to pharmaceutical compositions comprising Form 7, and to methods of using Form 7 and such compositions in the treatment of abnormal cell growth, such as cancer, in a mammal.
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CRYSTALLINE FORMS OF 1-((2R,4R)-2-(1H-BENZO[D]IMIDAZOL-2-YL)-1-METHYLPIPERIDIN-4-YL)-3-(4-CYANOPHENYL)UREA MALEATE (Fri, 30 Mar 2018)
This invention relates to a crystalline form of 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea maleate, and to pharmaceutical compositions thereof, to intermediates and methods for the production and isolation of such crystalline forms and compositions, and to methods of using such crystalline forms and compositions in the treatment of abnormal cell growth in mammals, especially humans.
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Crystal forms of azithromycin (Fri, 02 Sep 2005)
The invention relates to novel crystal forms of azithromycin, an antibiotic useful in the treatment of infections.
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Crystal forms of azithromycin (Fri, 30 Apr 2004)
The invention relates to novel crystal forms of azithromycin, an antibiotic useful in the treatment of infections.
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CRYSTALLINE FORMS OF 1-((2R,4R)-2-(1H-BENZO[D]IMIDAZOL-2-YL)-1-METHYLPIPERIDIN-4-YL)-3-(4-CYANOPHENYL)UREA MALEATE (Fri, 28 Oct 2016)
This invention relates to a crystalline form of 1-((2R,4R)-2-(1H-benzo[d]imidazol- 2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea maleate, and to pharmaceutical compositions thereof, to intermediates and methods for the production and isolation of such crystalline forms and compositions, and to methods of using such crystalline forms and compositions in the treatment of abnormal cell growth in mammals, especially humans.
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CRYSTALLINE FORMS OF 1-((2R,4R)-2-(1H-BENZO[D]IMIDAZOL-2-YL)-1-METHYLPIPERIDIN-4-YL)-3-(4-CYANOPHENYL)UREA MALEATE (Tue, 25 Oct 2016)
This invention relates to a crystalline form of 14(2R,4R)-2-(1H- benzo[d]imidazol-2- yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea maleate, and to pharmaceutical compositions thereof, to intermediates and methods for the production and isolation of such crystalline forms and compositions.
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Cyclic peptide compounds for pain treatment and their production process (Thu, 09 Jul 1998)
This invention provides processes for producing novel cyclic peptide compounds, which comprise cultivating Ctenomyces serratus FERM BP-5731 and then isolating the cyclic peptide compounds from the fermentation broth. The compounds produced by these processes include a cyclic peptide compound of the following formula (I): The present invention also relates to a pharmaceutical composition comprising the same, which is useful in the treatment of severe pain, detoxication of narcotics dependency or acute narcotics intoxication or the like.
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