Patents Assigned to Knoll Aktiengesellschaft
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Patent number: 6617360Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1 and R2 are independently H or methyl (for example N,N-dimethyl-1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutyl amine hydrochloride optionally in the form of its monohydrate) is used for reducing Insulin resistance in humans in whom Impaired Glucose Tolerance and Non-Insulin Dependent Diabetes Mellitus have not presented.Type: GrantFiled: October 30, 2000Date of Patent: September 9, 2003Assignee: Knoll AktiengesellschaftInventors: Clifford James Bailey, Robert Brian Jones, Helen Christine Jackson
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Publication number: 20030022315Abstract: Methods of regulating gene expression in subjects using tetracycline-responsive fusion proteins are disclosed. In one embodiment, the method involves introducing into a cell the subject a nucleic acid molecule encoding a fusion protein which inhibits transcription, the fusion protein comprising a first polypeptide which binds to a tet operator sequence, operatively linked to a heterologous second polypeptide which inhibits transcription in eukaryotic cells; and modulating the concentration of a tetracycline, or analogue thereof, in the subject. The first polypeptide can binds to a tet operator sequence in the absence, but not the presence, of tetracycline. Alternatively, the first polypeptide can binds to a tet operator sequence in the presence, but not the absence, of tetracycline.Type: ApplicationFiled: August 3, 2001Publication date: January 30, 2003Applicant: BASF Aktiengesellschaft and Knoll AktiengesellschaftInventors: Hermann Bujard, Manfred Gossen
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Patent number: 6509493Abstract: A process for preparing ethyl atropate by reacting ethyl phenylacetate with paraformaldehyde in the presence of a base is described and entails employing as ethyl phenylacetate a product which contains not more than 0.03% of the corresponding methyl phenylacetate, and carrying out the reaction in N-methyl-pyrrolidone or N,N-dimethylformamide.Type: GrantFiled: January 17, 2001Date of Patent: January 21, 2003Assignee: Knoll AktiengesellschaftInventors: Wolfgang Falkenberg, Marco Thyes, Conny Wenz, Ulrich Schneider
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Patent number: 6500830Abstract: A process for preparing doxazosin mesylate in modification A which comprises dissolving doxazosin with methanesulfonic acid in methanol or a mixture of an aprotic, polar organic solvent and methanol, removing any turbidity from the resulting solution, and stirring the resulting clear solution until no further precipitate separates out, removing, washing with methanol, heating the precipitate in the moist state in ethanol and, after cooling, isolating the resulting product is described.Type: GrantFiled: July 3, 2000Date of Patent: December 31, 2002Assignee: Knoll AktiengesellschaftInventors: Peter Klein, Marco Thyes, Dieter Hix
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Patent number: 6458842Abstract: There is disclosed a liquid pharmaceutical composition comprising a therapeutic agent which comprises: one or more thyroid hormone or hormones; from about 40% to about 96% ethanol by volume; a pH adjusting agent so that the measured pH of the composition is from about 9 to about 12; and from about 4% to about 50% water by volume; which has utility in the treatment of disorders associated with an impairment of the thyroid hormone function in animals including human beings. The liquid composition may be delivered by a metered dosage delivery system such as an aerosol or pump-action spray.Type: GrantFiled: July 31, 1996Date of Patent: October 1, 2002Assignee: Knoll AktiengesellschaftInventors: Jeffrey Dickinson, Karrar Ahmad Khan, John Neville Hague, Alan Smith
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Patent number: 6353002Abstract: Compounds of formula I and pharmaceutically acceptable salts thereof in which A is methylene or —O—; B is methylene or —O—; G1—G2—G3 form a heteroaromatic or heteroaliphatic chain; g is 0, 1 or 2; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T is an optionally substituted aryl or heteroaryl group, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behaviour, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the nType: GrantFiled: December 27, 2000Date of Patent: March 5, 2002Assignee: Knoll AktiengesellschaftInventors: Alan Martin Birch, Paul Anthony Bradley
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Patent number: 6326496Abstract: A process for the preparation of a compound of formula I in which R1 represents an amine protecting group wherein a compound of formula II in which R1 is as defined above is reduced by a metal hydride in the presence of an inorganic salt in the presence of a diluent.Type: GrantFiled: November 15, 1999Date of Patent: December 4, 2001Assignee: Knoll AktiengesellschaftInventor: James Patrick Brennan
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Patent number: 6312687Abstract: A stabilized aqueous enzyme concentrate composition which comprises: a) 1000 to 1800 units/ml of lactoperoxidase; b) 1500 to 2750 units/ml of glucose oxidase; c) 10 to 20% w/v of an alkali metal halide salt; and d) a chelating buffering agent present in an amount such that the pH of the composition is in the range of 5.5 to 6.5.Type: GrantFiled: October 25, 1999Date of Patent: November 6, 2001Assignee: Knoll AktiengesellschaftInventors: Walter Graham Guthrie, David Vincent Roper
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Patent number: 6271348Abstract: Methods of regulating gene expression in subjects using tetracycline-responsive fusion proteins are disclosed. In one embodiment, the method involves introducing into a cell the subject a nucleic acid molecule encoding a fusion protein which inhibits transcription, the fusion protein comprising a first polypeptide which binds to a tet operator sequence, operatively linked to a heterologous second polypeptide which inhibits transcription in eukaryotic cells; and modulating the concentration of a tetracycline, or analogue thereof, in the subject. The first polypeptide can binds to a tet operator sequence in the absence, but not the presence, of tetracycline. Alternatively, the first polypeptide can binds to a tet operator sequence in the presence, but not the absence, of tetracycline.Type: GrantFiled: January 24, 2000Date of Patent: August 7, 2001Assignees: BASF Aktiengesellschaft, Knoll AktiengesellschaftInventors: Hermann Bujard, Manfred Gossen
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Publication number: 20010010819Abstract: The invention relates to the use of TNF antagonists for producing drugs for the treatment of disorders characterized by elevated serum levels of interleukin-6.Type: ApplicationFiled: February 14, 2001Publication date: August 2, 2001Applicant: Knoll AktiengesellschaftInventors: Roswitha Stenzel, Martin Kaul, Lothar Daum, Joachim Kempeni, Christa Raab, Sibylle Schaefer
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Patent number: 6251945Abstract: A pharmaceutical mixture comprising a profen and one or more additional active compounds is described which has a total active compound content of over 85% and contains up to 1%, based on the content of the profen, of a nonionic surfactant having an HLB of ≧9 and a customary disintegrant and a lubricant.Type: GrantFiled: January 14, 1999Date of Patent: June 26, 2001Assignee: Knoll AktiengesellschaftInventors: Heinz Einig, Harald Hach, Raymond Eason, Bernd W. Müller, Richard C. Thompson
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Patent number: 6252136Abstract: Transgenic animals carrying two transgenes, the first coding for a transactivator fusion protein comprising a tet repressor and a polypeptide which directly or indirectly activates in eucaryotic cells, and the second comprising a gene operably linked to a minimal promoter operably linked to at least one tet operator sequence, are disclosed. Isolated DNA molecules (e.g., targeting vectors) for integrating a polynucleotide sequence encoding a transactivator of the invention at a predetermined location within a second target DNA molecule by homologous recombination are also disclosed. Transgenic animals having the DNA molecules of the invention integrated at a predetermined location in a chromosome by homologous recombination are also encompassed by the invention. Methods to regulate the expression of a tet operator linked-gene of interest by administering tetracycline or a tetracycline analogue to an animal of the invention are also disclosed.Type: GrantFiled: September 29, 1998Date of Patent: June 26, 2001Assignees: BASF Aktiengesellschaft, Knoll AktiengesellschaftInventors: Hermann Bujard, Manfred Gossen, Jochen G. Salfeld, Jeffrey W. Voss
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Patent number: 6239165Abstract: A liquid pharmaceutical formulation comprising a) 2 to 7% w/v of Zotepine; b) 0.5 to 35% w/v of an organic acid selected from the group consisting of ascorbic acid, citric acid, fumaric acid, glutaric acid, lactic acid, malic acid, sorbic acid and tartaric acid; c) 15 to 60% v/v of ethanol and d) a liquid diluent to 100%; which may be used as drops or in a drink.Type: GrantFiled: July 25, 2000Date of Patent: May 29, 2001Assignee: Knoll AktiengesellschaftInventors: Ann Margaret Dyer, Alan Smith
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Patent number: 6235281Abstract: The invention relates to the use of TNF antagonists for producing drugs for the treatment of disorders characterized by elevated serum levels of interleukin-6.Type: GrantFiled: August 7, 1996Date of Patent: May 22, 2001Assignee: Knoll AktiengesellschaftInventors: Roswitha Stenzel, Martin Kaul, Lothar Daum, Joachim Kempeni, Christa Raab, Sibylle Schaefer
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Patent number: 6225469Abstract: An improved process for the preparation of 1,2,4-triazolo[1,5-a]pyrimidine compounds comprising the reaction involving a compound of formula II and a compound of formula III in the presence of an oxidizing agent and a reducing agent, wherein a metal salt is added to form a complex with the oxidized reducing agent produced in the process, and this complex is separated from the desired product.Type: GrantFiled: February 17, 1999Date of Patent: May 1, 2001Assignee: Knoll AktiengesellschaftInventors: Nicholas John Holman, Stefan Koser
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Patent number: 6218405Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof in which A is methylene or —O—; B is methylene or —O—; G1—G2—G3 form a heteroaromatic or heteroaliphatic chain; g is 0, 1 or 2; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T is an optionally substituted aryl or heteroaryl group, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendrocrine syType: GrantFiled: June 16, 1999Date of Patent: April 17, 2001Assignee: KNOLL AktiengesellschaftInventors: Alan Martin Birch, Paul Anthony Bradley
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Patent number: 6215001Abstract: Compounds of the formula I and pharmaceutically acceptable salts thereof in which R1 represents hydrogen, halo, cyano, cyanoalkyl, alkyl, alkoxy, phenoxy, phenyl, alkoxycarbonyl, —NR13R14, —N(R15)SO2R16, halogenated alkoxy, halogenated alkyl, arylalkoxy, hydroxy, phenylalkyl, alkoxycarbonylvinyl, —S(O)nR7, alkoxycarbonylalkyl, carboxyalkyl, —CONR13R12 carbamoylvinyl, —OSO2R21, 4,5-dihydrothiazol-2-yl, 4,4-dimethyl-2-oxazolin-2-yl or —NR60R61; or R1 represents a group of formula —(O)z—L3G wherein z equals 0 or 1, L3 represents a C1-4 alkylene chain, G represents a group of formula a), b), c), or d): a) —NR22R23; b) —S(O)mR26; c) CONR27R28; d) —OR29; R2 and R3 independently represent hydrogen, halo, alkyl, alkoxy, —NR13R14, halogenated alkoxy, halogenated alkyl, hydroxy, —S(O)nR7 or —NR60R61; L1 represents e) a bond, or f) alkylene, cycloalkylene or cycloalkylidene; T represents a bond or O, S, SO, SO2, a carboType: GrantFiled: October 7, 1999Date of Patent: April 10, 2001Assignee: Knoll AktiengesellschaftInventors: David John Calderwood, Adrian John Fisher, James Edward Jeffery, Colin Gerhart Pryce Jones, Paul Rafferty
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Patent number: 6200791Abstract: A process for purifying thrombin-like proteases from snake venoms is described, which consists in freeing the proteases from impurities in three chromatographic steps: a) affinity or anion exchange, b) adsorption onto a glass matrix at alkaline pH values, and c) size exclusion gel or glass matrix at acidic pH values.Type: GrantFiled: August 17, 1998Date of Patent: March 13, 2001Assignee: Knoll AktiengesellschaftInventors: Margarete Schwarz, Wolfgang Zahn
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Patent number: 6201004Abstract: Compounds of formula I and pharmaceutically acceptable salts thereof in which A is methylene or —O—; B is methylene or —O—; G1—G2—G3 form a heteroaromatic or heteroaliphatic chain; g is 0, 1 or 2; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T is an optionally substituted aryl or heteroaryl group, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neType: GrantFiled: September 1, 1999Date of Patent: March 13, 2001Assignee: Knoll AktiengesellschaftInventors: Alan Martin Birch, Paul Anthony Bradley
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Patent number: 6197349Abstract: Particles comprising (a) a supercooled melt of a poorly water-soluble substance and (b) a stabilizing agent, which have a mean particle size of between 30 and 500 nm, and disperse compositions containing them, as administration forms and delivery systems for drugs, vaccines and other biologically active agents such as herbicides, pesticides, insecticides, fungicides, fertilizers, vitamins, nutrition additives and cosmetics.Type: GrantFiled: November 6, 1997Date of Patent: March 6, 2001Assignee: Knoll AktiengesellschaftInventors: Kirsten Westesen, Britta Siekmann