Patents Assigned to Knoll Aktiengesellschaft
  • Patent number: 6617360
    Abstract: 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: Grant
    Filed: October 30, 2000
    Date of Patent: September 9, 2003
    Assignee: Knoll Aktiengesellschaft
    Inventors: Clifford James Bailey, Robert Brian Jones, Helen Christine Jackson
  • Publication number: 20030022315
    Abstract: 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: Application
    Filed: August 3, 2001
    Publication date: January 30, 2003
    Applicant: BASF Aktiengesellschaft and Knoll Aktiengesellschaft
    Inventors: Hermann Bujard, Manfred Gossen
  • Patent number: 6509493
    Abstract: 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: Grant
    Filed: January 17, 2001
    Date of Patent: January 21, 2003
    Assignee: Knoll Aktiengesellschaft
    Inventors: Wolfgang Falkenberg, Marco Thyes, Conny Wenz, Ulrich Schneider
  • Patent number: 6500830
    Abstract: 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: Grant
    Filed: July 3, 2000
    Date of Patent: December 31, 2002
    Assignee: Knoll Aktiengesellschaft
    Inventors: Peter Klein, Marco Thyes, Dieter Hix
  • Patent number: 6458842
    Abstract: 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: Grant
    Filed: July 31, 1996
    Date of Patent: October 1, 2002
    Assignee: Knoll Aktiengesellschaft
    Inventors: Jeffrey Dickinson, Karrar Ahmad Khan, John Neville Hague, Alan Smith
  • Patent number: 6353002
    Abstract: 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 n
    Type: Grant
    Filed: December 27, 2000
    Date of Patent: March 5, 2002
    Assignee: Knoll Aktiengesellschaft
    Inventors: Alan Martin Birch, Paul Anthony Bradley
  • Patent number: 6326496
    Abstract: 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: Grant
    Filed: November 15, 1999
    Date of Patent: December 4, 2001
    Assignee: Knoll Aktiengesellschaft
    Inventor: James Patrick Brennan
  • Patent number: 6312687
    Abstract: 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: Grant
    Filed: October 25, 1999
    Date of Patent: November 6, 2001
    Assignee: Knoll Aktiengesellschaft
    Inventors: Walter Graham Guthrie, David Vincent Roper
  • Patent number: 6271348
    Abstract: 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: Grant
    Filed: January 24, 2000
    Date of Patent: August 7, 2001
    Assignees: BASF Aktiengesellschaft, Knoll Aktiengesellschaft
    Inventors: Hermann Bujard, Manfred Gossen
  • Publication number: 20010010819
    Abstract: 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: Application
    Filed: February 14, 2001
    Publication date: August 2, 2001
    Applicant: Knoll Aktiengesellschaft
    Inventors: Roswitha Stenzel, Martin Kaul, Lothar Daum, Joachim Kempeni, Christa Raab, Sibylle Schaefer
  • Patent number: 6251945
    Abstract: 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: Grant
    Filed: January 14, 1999
    Date of Patent: June 26, 2001
    Assignee: Knoll Aktiengesellschaft
    Inventors: Heinz Einig, Harald Hach, Raymond Eason, Bernd W. Müller, Richard C. Thompson
  • Patent number: 6252136
    Abstract: 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: Grant
    Filed: September 29, 1998
    Date of Patent: June 26, 2001
    Assignees: BASF Aktiengesellschaft, Knoll Aktiengesellschaft
    Inventors: Hermann Bujard, Manfred Gossen, Jochen G. Salfeld, Jeffrey W. Voss
  • Patent number: 6239165
    Abstract: 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: Grant
    Filed: July 25, 2000
    Date of Patent: May 29, 2001
    Assignee: Knoll Aktiengesellschaft
    Inventors: Ann Margaret Dyer, Alan Smith
  • Patent number: 6235281
    Abstract: 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: Grant
    Filed: August 7, 1996
    Date of Patent: May 22, 2001
    Assignee: Knoll Aktiengesellschaft
    Inventors: Roswitha Stenzel, Martin Kaul, Lothar Daum, Joachim Kempeni, Christa Raab, Sibylle Schaefer
  • Patent number: 6225469
    Abstract: 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: Grant
    Filed: February 17, 1999
    Date of Patent: May 1, 2001
    Assignee: Knoll Aktiengesellschaft
    Inventors: Nicholas John Holman, Stefan Koser
  • Patent number: 6218405
    Abstract: 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 sy
    Type: Grant
    Filed: June 16, 1999
    Date of Patent: April 17, 2001
    Assignee: KNOLL Aktiengesellschaft
    Inventors: Alan Martin Birch, Paul Anthony Bradley
  • Patent number: 6215001
    Abstract: 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 carbo
    Type: Grant
    Filed: October 7, 1999
    Date of Patent: April 10, 2001
    Assignee: Knoll Aktiengesellschaft
    Inventors: David John Calderwood, Adrian John Fisher, James Edward Jeffery, Colin Gerhart Pryce Jones, Paul Rafferty
  • Patent number: 6200791
    Abstract: 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: Grant
    Filed: August 17, 1998
    Date of Patent: March 13, 2001
    Assignee: Knoll Aktiengesellschaft
    Inventors: Margarete Schwarz, Wolfgang Zahn
  • Patent number: 6201004
    Abstract: 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 ne
    Type: Grant
    Filed: September 1, 1999
    Date of Patent: March 13, 2001
    Assignee: Knoll Aktiengesellschaft
    Inventors: Alan Martin Birch, Paul Anthony Bradley
  • Patent number: 6197349
    Abstract: 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: Grant
    Filed: November 6, 1997
    Date of Patent: March 6, 2001
    Assignee: Knoll Aktiengesellschaft
    Inventors: Kirsten Westesen, Britta Siekmann