b) 10 to 200 g per litre polyethylene glycol.
The invention also provides methods and kits associated with, or making use of the solutions, and compositions for the preparation of the solutions.
A61K 47/26 - Hydrates de carbone, p.ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharides; Leurs dérivés, p.ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
The invention provides a colon cleansing solution comprising: a) 300 to 2000 mmol per litre ascorbate anion provided by ascorbic acid, one or more salts of ascorbic acid, or a mixture thereof; and h) 10 to 200 g per litre polyethylene glycol. The invention also provides methods and kits associated with, or making use of the solutions. The invention also provides a method of cleansing the colon of a subject comprising: —administering to the subject an effect amount of a first cleansing solution; and then after a time interval—administering to the subject an effective amount of a second cleansing solution, wherein the two cleansing solutions are as described in the specification.
The invention provides a colon cleansing solution comprising: a) 300 to 2000 mmol per litre ascorbate anion provided by ascorbic acid, one or more salts of ascorbic acid, or a mixture thereof; and b) 10 to 200 g per litre polyethylene glycol. The invention also provides methods and kits associated with, or making use of the solutions. The invention also provides a method of cleansing the colon of a subject comprising: —administering to the subject an effect amount of a first cleansing solution; and then after a time interval—administering to the subject an effective amount of a second cleansing solution, wherein the two cleansing solutions are as described in the specification.
The invention provides a colon cleansing solution comprising: a) 300 to 2000 mmol per litre ascorbate anion provided by ascorbic acid, one or more salts of ascorbic acid, or a mixture thereof; and b) 10 to 200 g per litre polyethylene glycol. The invention also provides methods and kits associated with, or making use of the solutions. The invention also provides a method of cleansing the colon of a subject comprising: —administering to the subject an effect amount of a first cleansing solution; and then after a time interval —administering to the subject an effective amount of a second cleansing solution, wherein the two cleansing solutions are as described in the specification.
b) 10 to 200 g per litre polyethylene glycol.
The invention also provides methods an kits associated with, or making use of the solutions, and compositions for the preparation of the solutions.
A61K 47/26 - Hydrates de carbone, p.ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharides; Leurs dérivés, p.ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 47/10 - Alcools; Phénols; Leurs sels, p.ex. glycérol; Polyéthylène glycols [PEG]; Poloxamères; Alkyléthers de PEG/POE
A61K 31/375 - Acide ascorbique, c. à d. vitamine C; Ses sels
A61K 31/047 - Composés hydroxylés, p.ex. alcools; Leurs sels, p.ex. alcoolates ayant plusieurs groupes hydroxyle, p.ex. sorbitol
A61K 33/04 - Soufre, sélénium ou tellure; Leurs composés
A61K 33/14 - Chlorures des métaux alcalins; Chlorures des métaux alcalino-terreux
The invention provides a colon cleansing solution comprising:
a) 300 to 800 mmol per liter ascorbate anion provided by a mixture of:
b) 10 to 200 g per liter polyethylene glycol.
The invention also provides methods and kits associated with, or making use of the solutions, and compositions for the preparation of the solutions.
A61K 47/26 - Hydrates de carbone, p.ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharides; Leurs dérivés, p.ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
The invention provides a colon cleansing solution comprising: a) 300 to 2000 mmol per litre ascorbate anion provided by ascorbic acid, one or more salts of ascorbic acid, or a mixture thereof; and b) 10 to 200 g per litre polyethylene glycol. The invention also provides methods and kits associated with, or making use of the solutions. The invention also provides a method of cleansing the colon of a subject comprising: —administering to the subject an effect amount of a first cleansing solution; and then after a time interval—administering to the subject an effective amount of a second cleansing solution, wherein the two cleansing solutions are as described in the specification.
The present invention relates to compounds useful as CCR9 modulators, to compositions containing them, to methods of making them, and to methods of using them. In particular, the present invention relates to compounds capable of modulating the function of the CCR9 receptor by acting as partial agonists, antagonists or inverse agonists. Such compounds may be useful to treat, prevent or ameliorate a disease or condition associated with CCR9 activation, including inflammatory and immune disorder diseases or conditions such as inflammatory bowel diseases (IBD).
C07D 209/50 - Iso-indoles; Iso-indoles hydrogénés avec des atomes d'azote en positions 1 et 3
C07D 413/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant au moins trois hétérocycles
C07D 401/04 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique
C07D 401/06 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
C07D 403/04 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique
C07D 403/06 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne carbonée ne contenant que des atomes de carbone aliphatiques
C07D 409/04 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique
C07D 417/04 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique
C07D 405/04 - Composés hétérocycliques contenant à la fois un ou plusieurs hétérocycles comportant des atomes d'oxygène comme uniques hétéro-atomes du cycle et un ou plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique
C07D 413/12 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une chaîne contenant des hétéro-atomes comme chaînons
b) 10 to 200 g per liter polyethylene glycol.
The invention also provides methods and kits associated with, or making use of the solutions, and compositions for the preparation of the solutions.
A61K 47/26 - Hydrates de carbone, p.ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharides; Leurs dérivés, p.ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 31/047 - Composés hydroxylés, p.ex. alcools; Leurs sels, p.ex. alcoolates ayant plusieurs groupes hydroxyle, p.ex. sorbitol
A61K 33/04 - Soufre, sélénium ou tellure; Leurs composés
A61K 33/14 - Chlorures des métaux alcalins; Chlorures des métaux alcalino-terreux
A61K 47/18 - Amines; Amides; Urées; Composés d’ammonium quaternaire; Acides aminés; Oligopeptides ayant jusqu’à cinq acides aminés
The present invention relates to colon cleansing solutions, compositions and methods of cleansing the colon using colon cleansing solutions. The invention provides colon cleansing solutions that are more palatable for intestinal lavage subjects than current solutions and that are also effective when ingested in smaller volumes than current solutions. Also described are methods of cleansing the colon of a subject before a diagnostic, therapeutic or surgical procedure using the solutions of the present invention.
The invention provides a method of cleansing the colon of a subject before a diagnostic, therapeutic or surgical procedure comprising: - administering to the subject an effective amount of a first colon cleansing solution; - administering to the subject an effective amount of a second colon cleansing solution, the second colon cleansing solution being as defined in the application; whereby the first colon cleansing solution is taken over a time period t(d1) followed by optional additional clear fluid over a time period t(cf1), and then following a time interval t(dose interval), the second colon cleansing solution is taken over a time period t(d2) followed by optional additional clear fluid over a time period t(cf2), whereby the subject undergoes the surgical, therapeutic or diagnostic procedure at a time t2 after the beginning of the colon cleansing method, and whereby the time interval after the completion of the second additional clear fluid and the start of the surgical, therapeutic or diagnostic procedure is t(procedure interval).
The present invention relates to compounds useful as CCR9 modulators, to compositions containing them, to methods of making them, and to methods of using them. In particular, the present invention relates to compounds capable of modulating the function of the CCR9 receptor by acting as partial agonists, antagonists or inverse agonists. Such compounds may be useful to treat, prevent or ameliorate a disease or condition associated with CCR9 activation, including inflammatory and immune disorder diseases or conditions such as inflammatory bowel diseases (IBD).
C07D 413/14 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes d'azote et d'oxygène comme uniques hétéro-atomes du cycle contenant au moins trois hétérocycles
C07D 401/04 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique
C07D 401/06 - Composés hétérocycliques contenant plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle, au moins un cycle étant un cycle à six chaînons avec un unique atome d'azote contenant deux hétérocycles liés par une chaîne carbonée contenant uniquement des atomes de carbone aliphatiques
C07D 403/04 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique
C07D 403/06 - Composés hétérocycliques contenant plusieurs hétérocycles, comportant des atomes d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une chaîne carbonée ne contenant que des atomes de carbone aliphatiques
C07D 409/04 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre comme uniques hétéro-atomes du cycle contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique
C07D 417/04 - Composés hétérocycliques contenant plusieurs hétérocycles, au moins un cycle comportant des atomes de soufre et d'azote comme uniques hétéro-atomes du cycle, non prévus par le groupe contenant deux hétérocycles liés par une liaison directe de chaînon cyclique à chaînon cyclique
A61K 31/395 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p.ex. guanéthidine ou rifamycines
The present invention relates to compounds useful as CCR9 modulators, to compositions containing them, to methods of making them, and to methods of using them. In particular, the present invention relates to compounds capable of modulating the function of the CCR9 receptor by acting as partial agonists, antagonists or inverse agonists. Such compounds may be useful to treat, prevent or ameliorate a disease or condition associated with CCR9 activation, including inflammatory and immune disorder diseases or conditions such as inflammatory bowel diseases (IBD).
A61P 37/00 - Médicaments pour le traitement des troubles immunologiques ou allergiques
A61K 31/437 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p.ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique contenant un cycle à cinq chaînons ayant l'azote comme hétéro-atome du cycle, p.ex. indolizine, bêta-carboline
A61K 31/519 - Pyrimidines; Pyrimidines hydrogénées, p.ex. triméthoprime condensées en ortho ou en péri avec des hétérocycles
b) 10 to 200 g per litre polyethylene glycol.
The invention also provides methods and kits associated with, or making use of the solutions, and compositions for the preparation of the solutions.
A61K 47/26 - Hydrates de carbone, p.ex. polyols ou sucres alcoolisés, sucres aminés, acides nucléiques, mono-, di- ou oligosaccharides; Leurs dérivés, p.ex. polysorbates, esters d’acide gras de sorbitan ou glycyrrhizine
A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
A61K 31/047 - Composés hydroxylés, p.ex. alcools; Leurs sels, p.ex. alcoolates ayant plusieurs groupes hydroxyle, p.ex. sorbitol
A61K 33/04 - Soufre, sélénium ou tellure; Leurs composés
A61K 33/14 - Chlorures des métaux alcalins; Chlorures des métaux alcalino-terreux
A61K 47/18 - Amines; Amides; Urées; Composés d’ammonium quaternaire; Acides aminés; Oligopeptides ayant jusqu’à cinq acides aminés
b) 10 to 200 g per liter polyethylene glycol.
The invention also provides methods an kits associated with, or making use of the solutions, and compositions for the preparation of the solutions.
A solution in water comprising the following components at the following concentrations: (a) N×(70 to 130) g/L polyethylene glycol (PEG) having an average molecular weight of 2500 to 4500; (b) N×(1.6 to 4.0) g/L sodium chloride; (c) N×(0.2 to 0.6) g/L potassium chloride; (d) N×(0.6 to 2.2) g/L sodium bicarbonate; (e) N×an amount of preservative; (f) optionally N x an amount of flavouring; and (g) optionally N×an amount of sweetener, where N is in the range of 2 to 8. The solution is a concentrate for dilution. In use it is diluted N-fold with water to provide a solution for administration to a subject for the treatment of constipation or faecal impaction. Also provided are solutions, kits, unit doses and methods that comprise or use the solutions.
Disclosed are compositions comprising polyethylene glycol (PEG) having a weight average molecular weight of 800 or greater and a concentration of 30mg/ml or greater for use in preventing and/or treating head and neck squamous cell carcinoma (HNSCC). Methods of preventing and/or treating HNSCC are also disclosed.
Disclosed are compositions comprising polyethylene glycol (PEG) having a weight average molecular weight of 800 or greater and a concentration of 30mg/ml or greater for use in preventing and/or treating epidermal growth factor receptor (EGFR) dependent cancers, other than head and neck squamous cell carcinoma (HNSCC). Methods of treating and/or preventing EGFR-dependent cancers are also disclosed.
The invention provides acolon cleansing solutioncomprising: a) 300 to 800 mmol per litre ascorbate anion provided by a mixtureof: (i) ascorbic acid and (ii) one or more salts of ascorbic acid the components (i) and (ii) being present in a molar ratio of from 1:4.5 to 1:7.0; and b) 10 to 200 g per litre polyethylene glycol. The invention also provides methods an kits associated with, or making use of the solutions, and compositions for the preparation of the solutions.
The invention provides a colon cleansing solution comprising: a) 300 to 800 mmol per litre ascorbate anion provided by a mixture of: (i) ascorbic acid and (ii) one or more salts of ascorbic acid the components (i) and (ii) being present in a molar ratio of from 1:4.5 to 1:7.0; and b) 10 to 200 g per litre polyethylene glycol. The invention also provides methods and kits associated with, or making use of the solutions, and compositions for the preparation of the solutions.
The invention provides acolon cleansing solutioncomprising: a) 300 to 800 mmol per litre ascorbate anion provided by a mixtureof: (i) ascorbic acid and (ii) one or more salts of ascorbic acid the components (i) and (ii) being present in a molar ratio of from 1:4.5 to 1:7.0; and b) 10 to 200 g per litre polyethylene glycol. The invention also provides methods an kits associated with, or making use of the solutions, and compositions for the preparation of the solutions.
The invention provides a colon cleansing solution comprising: a) 300 to 2000 mmol per liter ascorbate anion provided by ascorbic acid, one or more salts of ascorbic acid, or a mixture thereof; and b) 10 to 200 g per liter polyethylene glycol. The invention also provides methods and kits associated with, or making use of the solutions. The invention also provides a method of cleansing the colon of a subject comprising: —administering to the subject an effective amount of a first cleansing solution; and then after a time interval —administering to the subject an effective amount of a second cleansing solution, where in the two cleansing solutions are as described in the specification.
The present invention relates to compositions comprising cetilistat, including its salts, esters, amides, solvates, polymorphs, and mixtures thereof. The invention also relates to formulations comprising such compositions, to processes for preparation of the compositions and formulations, and to their methods of use for weight management, including weight loss.
A61K 31/536 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p.ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec au moins un azote et au moins un oxygène comme hétéro-atomes d'un cycle, p.ex. 1,2-oxazines condensées en ortho ou en péri avec des systèmes carbocycliques
The invention provides a colon cleansing solution comprising: a) 300 to 2000 mmol per litre ascorbate anion provided by ascorbic acid, one or more salts of ascorbic acid,or a mixture thereof; and b) 10 to 200 g per litre polyethylene glycol. The invention also provides methods and kits associated with, or making use of the solutions. The invention also provides a method of cleansing the colon of a subject comprising: -administering to the subject an effective amount of a first cleansing solution;and then after a time interval -administering to the subject an effective amount of a second cleansing solution, where in the two cleansing solutions are as described in the specification.
The invention provides a colon cleansing solution comprising: a) 300 to 2000 mmol per litre ascorbate anion provided by ascorbic acid, one or more salts of ascorbic acid, or a mixture thereof; and b) 10 to 200 g per litre polyethylene glycol. The invention also provides methods and kits associated with, or making use of the solutions. The invention also provides a method of cleansing the colon of a subject comprising: - administering to the subject an effective amount of a first cleansing solution; and then after a time interval -administering to the subject an effective amount of a second cleansing solution, where in the two cleansing solutions are as described in the specification. Solutions of the invention are surprisingly effective colon cleansing solutions as measured by stool output, providing satisfactory clearance of stools from the colon with ingestion of a smaller total volume of solution than with standard 2 or 4 litre solutions of the prior art. Many subjects find the ingestion of a large volume unpleasant or difficult and poor patient compliance is a problem.
The invention provides an aqueous liquid enema composition having a measured osmolality within the range of 350 to 2000 mOsmol/kg comprising (or consisting essentially of) polyethylene glycol. Associated applicators and methods of cleansing are also provided.
The present invention concerns aqueous solutions comprising polyethylene glycol for use as a medicament, particularly in the treatment of constipation and faecal impaction. The solutions may be preserved to suppress the growth of microbial organisms. Kits comprising a preserved aqueous solution and a separate tablet or capsule comprising electrolytes are also provided.
The present invention concerns a solid formulation for oral administration as a solid comprising polyethylene glycol and a further solid such as mannitol. The formulation may be used to prevent gastrointestinal disorders such as constipation in healthy subjects. In some embodiments, the solid formulation is chewable or suckable.
The present invention relates to methods for and of treating, ameliorating or preventing colorectal cancer (CRC) in humans using polyethylene glycol (PEG) or a PEG block-copolymer such as Pluronic® F68. Compositions for use in treating, ameliorating and/or preventing CRC comprising PEG are also disclosed. Such compositions may be used in the methods of the invention.
1,1-dioxo-1-ursodeoxycholamino-tetrahydrothiopyran-4-carboxylic acid, and salts, esters, and amides thereof, may be used in the treatment or prevention of a condition associated with fatty liver.
C07J 33/00 - Stéroïdes normaux ayant un hétérocycle contenant du soufre non condensé ou condensé en spiro avec le squelette du cyclopenta[a]hydrophénanthrène
A61K 31/58 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrène; Leurs dérivés, p.ex. stéroïdes contenant des hétérocycles, p.ex. danazol, stanozolol, pancuronium ou digitogénine
A61P 1/16 - Médicaments pour le traitement des troubles du tractus alimentaire ou de l'appareil digestif des troubles de la vésicule biliaire ou du foie, p.ex. protecteurs hépatiques, cholagogues, cholélitholytiques
The present invention concerns solid compressed oral pharmaceutical compositions comprising a mixture of at least two sulphate salts selected from the group consisting of sodium, potassium and magnesium for use, in particular, in cleansing the colon or treating faecal impaction, constipation, faecal retention, intestinal gas and cramping, or flatulence in a mammal. Methods of producing such compositions are also disclosed.
The invention provides a solution in water comprising the following components at the following concentrations: (a) N x (70 to 130) g/L polyethylene glycol (PEG) having an average molecular weight of 2500 to 4500; (b) N x (1.6 to 4.0) g/L sodium chloride; (c) N x (0.2 to 0.6) g/L potassium chloride; (d) N x (0.6 to 2.2) g/L sodium bicarbonate; (e) N x an amount of preservative; (f) optionally N x an amount of flavouring; and (g) optionally N x an amount of sweetener where N is in the range of 2 to 8. The solution is a concentrate for dilution. In use it is diluted N-fold with water to provide a solution for administration to a subject for the treatment of constipation or faecal impaction. Also provided are solutions, kits, unit doses and methods that comprise or use the solutions.
The invention provides a solution in water comprising the following components at the following concentrations: (a) N x (70 to 130) g/L polyethylene glycol (PEG) having an average molecular weight of 2500 to 4500; (b) N x (1.6 to 4.0) g/L sodium chloride; (c) N x (0.2 to 0.6) g/L potassium chloride; (d) N x (0.6 to 2.2) g/L sodium bicarbonate; (e) N x an amount of preservative; (f) optionally N x an amount of flavouring; and (g) optionally N x an amount of sweetener where N is in the range of 2 to 8. The solution is a concentrate for dilution. In use it is diluted N-fold with water to provide a solution for administration to a subject for the treatment of constipation or faecal impaction. Also provided are solutions, kits, unit doses and methods that comprise or use the solutions.
The invention provides a dry composition for admixture with water, wherein the composition is optionally presented in two or more parts and comprises, per litre of solution to be made, the following components: (a) 85 to 115 g polyethylene glycol (PEG) having an average molecular weight of 2500 to 4500; (b) 6 to 9 g sodium sulphate; (c) 2 to 3 g sodium chloride; (d) 0.5 to 1.5 g potassium chloride; (e) 5 to 15 g of an organic acid component; and (f) orange flavouring. Also provided are solutions, kits, unit doses and methods that comprise or use the compositions.
The invention provides a dry composition for admixture with water, wherein the composition is optionally presented in two or more parts and comprises, per litre of solution to be made, the following components: (a) 85 to 115 g polyethylene glycol (PEG) having an average molecular weight of 2500 to 4500; (b) 6 to 9 g sodium sulphate; (c) 2 to 3 g sodium chloride; (d) 0.5 to 1.5 g potassium chloride; (e) 5 to 15 g of an organic acid component; and (f) orange flavouring. Also provided are solutions, kits, unit doses and methods that comprise or use the compositions.
Disclosed is a crystal of 2-hexadecyloxy-6-methyl-4H-3,1-benzoxazin-4-one useful as a preventive or therapeutic agent for obesity and the like. Specifically disclosed is a crystal of 2-hexadecyloxy-6-methyl-4H-3,1-benzoxazin-4-one having a powder X-ray diffraction pattern in which characteristic peaks appear at powder X-ray diffraction interplanar spacings (d) of around 16.54 ± 0.2, 13.26 ± 0.2, 4.70 ± 0.2, 4.38 ± 0.2, and 3.67 ± 0.2 Ǻ.
C07D 265/26 - Deux atomes d'oxygène, p.ex. anhydride isatoïque
A61K 31/536 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p.ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec au moins un azote et au moins un oxygène comme hétéro-atomes d'un cycle, p.ex. 1,2-oxazines condensées en ortho ou en péri avec des systèmes carbocycliques
A61P 1/04 - Médicaments pour le traitement des troubles du tractus alimentaire ou de l'appareil digestif des ulcères, des gastrites ou des œsophagites par reflux, p.ex. antiacides, antisécrétoires, protecteurs de la muqueuse
A61P 3/04 - Anorexigènes; Médicaments de l'obésité
A process for the preparation of a mixture of 3',6'-dihydroxy-6-nitrospiro[2-benzofuran-3,9'-xanthene]-1-one and 3',6'-dihydroxy-5-nitrospiro[2-benzofuran-3,9'- xanthene]-1-one comprising the steps of:- (a) reacting 4-nitrophthalic acid or 4-nitrophthalic anhydride with benzene-1,3- diol in methanesulphonic acid; (b) quenching the reaction in step (a) with a solvent to precipitate product; (c) isolating the precipitate; (d) heating the precipitate in water in order to hydrolyse any methansulphonic acid ester present.
A process for the preparation of cholyl-L-lysine comprising the steps of:- (a) reacting N-ε-CBZ-cholyl-L-lysine with a hydrogen source in the presence of a catalyst in a solvent comprising one or more alkanols; (b) removing the catalyst; (c) optionally diluting the resulting reaction mixture with water and optionally adjusting the pH of the resultant reaction mixture to a pH less than or equal to about 4; (d) removing the bulk of the alkanol whilst ensuring that the alkanol content of the resultant mixture is maintained above about 3% w/w of the remaining mixture; (e) extracting the resultant mixture from step (d) with an organic solvent; (f) adjusting the pH of the aqueous layer to a pH of about 4.5 or greater to precipitate cholyl-L-lysine; (g) isolate the precipitate.
