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 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.
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.
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; Hydrogenated iso-indoles with oxygen and nitrogen atoms in positions 1 and 3
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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.
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 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 409/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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 - Drugs for immunological or allergic disorders
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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.
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 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 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 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with carbocyclic ring systems
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 - Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta[a]hydrophenanthrene skeleton
A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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 - Two oxygen atoms, e.g. isatoic anhydride
A61K 31/536 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with carbocyclic ring systems
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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.
