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HPLC apparatus for fractioning and preparing sample for NMR spectrometry and method of changing mobile phase (Wed, 25 Dec 2002)
A high-performance liquid chromatography apparatus and a process for conversion of mobile phase, enabling a trace amount of sample for NMR analysis to be efficiently separated and prepared, includes steps of separating a target ingredient from the sample by the high-performance liquid chromatography, trapping the target ingredient in a trapping column using a different mobile phase, replacing water by deuterium oxide and eluting this target ingredient from the trapping column using deuterated solvent other than deuterium oxide.
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HPLC APPARATUS FOR FRACTIONING AND PREPARING SAMPLE FOR NMR SPECTROMETRY AND METHOD OF CHANGING MOBILE PHASE (Thu, 18 May 2000)
Here is disclosed a high-performance liquid chromatography apparatus and a process for conversion of mobile phase enabling a trace amount of sample for NMR analysis to be efficiently separated and prepared. comprises steps of separating a target ingredient from the sample by the high-performance liquid chromatography, trapping the target ingredient in a trapping column using a different mobile phase, replacing water by deuterium oxide and eluting this target ingredient from the trapping column using deuterated solvent other than deuterium oxide.
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CRYSTAL OF INDOLE DERIVATIVE HAVING PIPERIDINE RING AND PROCESS FOR PRODUCTION THEREOF (Thu, 24 Jan 2008)
A crystal of 1-[1-[2-(7-methoxy-2,2-dimethyl-4-oxochroman-8-yl)-ethyl]piperidin-4-yl]-N-methyl-1H-indole-6-carboxamide fumarate which has peaks at chemical shifts of about 124.0 ppm and about 26.8 ppm in a 13 C solid NMR spectrum.
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Crystal of indole derivative having piperidine ring and process for production thereof (Fri, 30 Nov 2007)
A crystal of 1-[1-[2-(7-methoxy-2,2-dimethyl-4-oxochroman-8-yl)- ethyl]piperidin-4-yl]-N-methyl-1H-indole-6-carboxamide fumarate which has peaks at chemical shifts of about 124.0 ppm and about 26.8 ppm in a 13C solid NMR spectrum.
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CRYSTAL OF INDOLE DERIVATIVE HAVING PIPERIDINE RING AND PROCESS FOR PRODUCTION THEREOF (Fri, 17 Nov 2006)
A crystal of 1-[1-[2-(7-methoxy-2,2-dimethyl-4-oxochroman-8-yl)- ethyl]piperidin-4-yl]-N-methyl-1H-indole-6-carboxamide fumarate which has peaks at chemical shifts of about 124.0 ppm and about 26.8 ppm in a 13C solid NMR spectrum.
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CRYSTALLINE SULFONAMIDE-CONTAINING INDOLE COMPOUND AND PROCESS FOR PREPARING THE SAME (Fri, 25 Mar 2005)
Provided is a crystalline form of N-(3-cyano-4-methyl-1H-indol-7-yl)-3- cyanobenzenesulfonamide (see formula above) having a diffraction peak at a diffraction angle (2.theta. 0.2°) of 19.1° in a powder X-ray diffraction and having satisfactory properties including stability to light, rendering it suitable for use as the active ingredient of an antitumor agent.
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POLYMORPHIC CRYSTAL OF DONEPEZIL AND PROCESS FOR PRODUCING THE SAME (Fri, 25 Jun 2010)
[Problem] A novel polymorphic crystal (F) of donepezil that is a precursor for production of donepezil hydrochloride having an excellent effect as a medicine and is an active principle, which has excellent handling properties, and an industrial process for producing the novel polymorphic crystal (F). [Solution] The novel polymorphic crystal (F) of the present invention is characterized by a powder X-ray diffraction pattern, an IR absorption peak, a solid NMR spectrum, and the like, of donepezil represented by the following formula (I).
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Salts of indazole derivative and crystals thereof (Fri, 01 Jun 2018)
The present invention provides salts of (E)-N,N-dimethyl-4-((2-((5-((Z)-4,4,4-trifluoro-1-(3-fluoro-1H-indazol-5-yl)-2-phenylbut-1-en-1-yl)pyridin-2-yl)oxy)ethyl)amino)but-2-enamide represented by the formula I and acids, and crystals thereof, possessing a potential to be used as drug substance in pharmaceuticals.
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Salts of Indazole Derivative and Crystals Thereof (Fri, 17 May 2019)
The present invention provides salts of (E)-N,N-dimethyl-4-((2-((5-((Z)-4,4,4-trifluoro-1-(3-fluoro-1H-indazol-5-yl)-2-phenylbut-1-en-1-yl)pyridin-2-yl)oxy)ethyl)amino)but-2-enamide represented by the formula I and acids, and crystals thereof, possessing a potential to be used as drug substance in pharmaceuticals. embedded image
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CRYSTAL OF (6S,9aS)-N-BENZYL-6-[(4-HYDROXYPHENYL)METHYL]- 4,7-DIOXO-8-({6-[3-(PIPERAZIN-1-YL)AZETIDIN-1-YL]PYRIDIN- 2-YL}METHYL)-2-(PROP-2-EN-1-YL)-OCTAHYDRO-1H-PYRAZINO[2,1-c][1,2,4]TRIAZINE-1-CARBOXAMIDE COMPOUND (Thu, 03 May 2018)
The present invention provides a crystal of (6S,9aS)-N-benzyl-8-({6-[3-(4-ethylpiperazin-1-yl)azetidin-1-yl]pyridin-2-yl} methyl)-6-(2-fluoro-4-hydroxybenzyl)-4,7-dioxo-2-(prop-2-en-1-yl)hexahydr o-2H-pyrazino[2,1-c][1,2,4]triazine-1(6H)-carboxamide.
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Crystal of (6S,9aS)-N-benzyl-8-({6-[3-(4-ethylpiperazin-1- yl)azetidin-1-yl]pyridin-2-yl}methyl)-6-(2-fluoro-4- hydroxybenzyl)-4,7-dioxo-2-(prop-2-en-1-yl)hexahydro-2Hpyrazino[ 2,1-c][1,2,4]triazine-1-(6H)-carboxamide (Fri, 30 Dec 2016)
The present invention provides a crystal of (6S,9aS)-N-benzyl-8-({6-[3-(4-ethylpiperazin-1-yl)azetidin-1-yl]pyridin-2-yl}methyl)-6-(2-fluoro-4-hydroxybenzyl)-4,7-dioxo-2-(prop-2-en-1-yl)hexahydro-2H-pyrazino[2,1-c][1,2,4]triazine-1(6H)-carboxamide.
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Crystal (6S,9aS)-N-benzyl-8-({6-[3-(4-ethylpiperazin-1-yl)azetidin-1-yl]pyridin-2-yl}methyl)-6-(2-fluoro-4-hydroxybenzyl)-4,7-dioxo-2-(prop-2-en-1-yl)hexahydro-2H-pyrazino[2,1-c][1,2,4]triazine-1(6H)-carboxamide (Fri, 25 May 2018)
The present invention provides a crystal of (6S,9aS)-N-benzyl-8-({6-[3-4-ethylpiperazin-1-yl)azetidin-1-yl]pyridin-2-yl}methyl)-6-(2-fluoro-4-hydroxybenzyl)-4,7-dioxo-2-(prop-2-en-1-yl)hexahydro-2H-pyrazino[2,1-c][1,2,4]triazine-1(6H)-carboxamide. embedded image
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SALTS OF INDAZOLE DERIVATIVE AND CRYSTALS THEREOF (Fri, 01 Jun 2018)
The present invention provides salts of (E)-N,N-dimethyl-4-((2-((5-((Z)-4,4,4-trifluoro-1-(3-fluoro-1H-indazol-5-yl)-2-phenylbut-1-en-1-yl)pyridin-2-yl)oxy)ethyl)amino)but-2-enamide represented by the formula I and acids, and crystals thereof, possessing a potential to be used as drug substance in pharmaceuticals.
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SALT OF PYRAZOLOQUINOLINE DERIVATIVE, AND CRYSTAL THEREOF (Thu, 11 Feb 2016)
The present invention provides a salt of (S)-7-(2-methoxy-3,5-dimethylpyridin-4-yl)-1-(tetrahydrofuran-3-yl)-1H-pyrazolo[4,3-c]quinolin-4(5H)-one and an acid selected from the group consisting of hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, malonic acid, maleic acid, tartaric acid, methanesulfonic acid, benzenesulfonic acid and toluenesulfonic acid; or a crystal thereof with a potential to be used as drug substance in pharmaceuticals.
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CRYSTAL OF SULFONAMIDE-CONTAINING INDOLE COMPOUND AND PROCESS FOR PRODUCING THE SAME (Thu, 08 Jun 2006)
A crystalline form of N-(3-cyano-4-methyl-1 H -indol-7-yl)-3-cyanobenzenesulfonamide having a diffraction peak at a diffraction angle (2¸ ± 0.2°) of 19.1° in a powder X-ray diffraction.
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SALT OF SULFINYLBENZIMIDAZOLE COMPOUND, AND CRYSTAL AND AMORPHOUS FORM THEREOF (Tue, 16 Dec 2008)
Salts of 2-[({4-[(2,2-dimethyl-1,3-dioxan-5-yl)methoxy]-3,5-dimethylpyridin-2-yl} methyl)sulfinyl]-1H-benzimidazole, and crystals and amorphous forms thereof. ©KIPO&WIPO 2009
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CRYSTALLINE 1H-IMIDAZO[4,5-B]PYRIDIN-5-AMINE,7-[5-[(CYCLOHEXYLMETHYLAMINO)-METHYL]-1H-INDOL-2-YL]-2-METHYL, SULFATE (1:1), TRIHYDRATE AND ITS USES FOR THE TREATMENT OF INFLAMMATORY, AUTOIMMUNE AND PROLIFERATIVE DISEASES AND DISORDERS (Fri, 11 Aug 2006)
The invention relates to crystalline 1W-lmidazo[4,5-d]pyridi.pi.-5-amine, 7-[5- [(cyclohexylmethylamino)-methyl]-1H-indol-2-yl]-2-methylI sulfate (1:1), trihydrate, E6070, its method of preparation, and its therapeutic uses. Pharmaceutical compositions containing crystalline E6070 and a pharmaceutically acceptable carrier represent one embodiment of the invention. The invention also relates to methods for treating an inflammatory disorder, an autoimmune disorder, or a proliferative disorder comprising the step of administering to a patient in need thereof a therapeutically effective amount of crystalline E6070.
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HETEROARYL AMINES AS NOVEL ACETYLCHOLINESTERASE INHIBITORS (Wed, 29 Mar 1995)
These compounds, which are useful as acetylcholinesterase inhibitors, are of the formula: where one of R2, R3 and the side chain containing -C(Z)- may optionally be attached to the carbon atom designated by an asterisk in ring B rather than to a member of ring A; ring A is benzo, thieno, pyrido, pyrazino, pyrimido, furano, seleno, pyrrolo, thiazolo, or imidazolo; R1 is phenyl, phenyl-(C1-C6)alkyl, cinnamyl or heteroarylmethyl, wherein the heteroaryl moiety of said heteroarylmethyl is selected from imidazolyl, thiazolyl, thienyl, pyridyl and isoxazolyl, and wherein said phenyl and said heteroaryl moiety may optionally be substituted with one or two substituents independently selected from (C1-C6)alkyl, (C1-C6)alkoxy, phenyl, benzyl and halo; R2 and R3 are independently selected from hydrogen, (C1-C6)alkoxy, (C1-C6)alkyl optionally substituted with from one to three fluorine atoms, benzyloxy, hydroxy, phenyl, benzyl, halo, nitro, cyano, COOR4, CONHR4, NR4R5, NR4COR5, or SOpCH2-phenyl wherein p is 0, 1 or 2; or R2 and R3 are attached to adjacent carbon atoms and form, together with the carbons to which they are attached, a five or six membered ring wherein each member of the ring is carbon, nitrogen, oxygen or a carbonyl group; R4 and R5 are independently selected from hydrogen and (C1-C6)alkyl, or R4 and R5, when part of said NR4R5, optionally form, together with the nitrogen to which they are attached, a ring containing four to eight members wherein one atom of the ring is nitrogen and the others are carbon, oxygen or nitrogen, or R4 and R5, when part of said NR4COR5, optionally form, together with the nitrogen and carbon to which they are attached, a four to eight member lactam ring; X is nitrogen, CH or CCH3; Y is oxygen, sulphur or NR6; R6 is hydrogen, (C1-C6)alkyl, CO(C1-C6)alkyl or SO2-phenyl, wherein the phenyl moiety of said SO2-phenyl may optionally be substituted with from one to five substituents independently selected from (C1-C4) alkyl; n is an integer from 1 to 4; each q is independently 1 or 2; and Z is oxygen or sulphur; with the proviso that any CHq group wherein q is 1 must be attached to one and only one other CHq is 1; and pharmaceutically acceptable salts thereof...
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Salt of sulfinylbenzimidazole compound, and crystal and amorphous form thereof (Fri, 19 Sep 2008)
Salts of 2-[({4-[(2,2-dimethyl-1,3-dioxan-5-yl)methoxy]-3,5-dimethylpyridin-2-yl}methyl)sulfinyl]-1H-benzimidazole, and crystals and amorphous forms thereof.
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SALT OF SULFINYLBENZIMIDAZOLE COMPOUND, AND CRYSTAL AND AMORPHOUS FORM THEREOF (Thu, 09 Jul 2009)
Salts of 2-[({4-[(2.2-dimethyl-1,3-dioxan-5-yl)methoxy]-3,5-dimethylpyridin-2-yl}methyl)sulfinyl]-1H-benzimidazole and their crystalline and amorphous forms.
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