Patents by Inventor Karl-Heinrich Fritzemeier

Karl-Heinrich Fritzemeier has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 8445469
    Abstract: A 18-Methyl-19-nor-17-pregn-4-ene-21,17-carbolactone of general formula I in which Z, R4, R6, R7 are as defined below with the proviso that the compound is not 18-Methyl-15?,16?-methylene-3-oxo-19-nor-17-pregn-4-ene-21,17-carbolactone.
    Type: Grant
    Filed: December 30, 2005
    Date of Patent: May 21, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Rolf Bohlmann, Dieter Bittler, Hermann Kuenzer, Peter Esperling, Hans-Peter Muhn, Karl-Heinrich Fritzemeier, Ulrike Fuhrmann, Katja Prelle, Steffen Borden
  • Publication number: 20110178052
    Abstract: Use of 9?-estra-1,3,5(10)-triene derivatives of formula (I) for the prevention and treatment of intestinal cancer, in particular adenoma and adenocarcinoma of the duodenum, ileum, colon, and rectum.
    Type: Application
    Filed: July 9, 2009
    Publication date: July 21, 2011
    Applicant: Bayer Schering Pharma Aktiengesellschaft
    Inventors: Karl-Heinrich Fritzemeier, Patrick Diel, Torsten Hertrampf
  • Publication number: 20090099250
    Abstract: The present invention describes non-steroidal compounds of the general formula (I) in which A is in which X1 means one or more groups on the phenyl ring and represents independently of one another a halogen, OH, (C1-C4)alkyl, (C1-C4)alkyl-O, (C3-C6)cycloalkyl-O, (C1-C14)acyl-O, (C1-C4)alkenyl, (C1-C4)alkynyl, perfluoro(C1-C4)alkyl radical, —CHO or CN, and X2 means one or more groups on the phenyl ring and represents independently of one another an H, halogen, OH, (C1-C4)alkyl, (C1-C4)alkyl-O, (C1-C4)alkenyl, (C1-C4)alkynyl, perfluoro-(C1-C4)alkyl radical, —CHO or CN, as Estrogens.
    Type: Application
    Filed: October 10, 2008
    Publication date: April 16, 2009
    Inventors: Ralf WYRWA, Olaf Peters, Rolf Bohlmann, Peter Droescher, Katja Prelle, Karl Heinrich Fritzemeier, Hans Peter Muhn
  • Publication number: 20090029953
    Abstract: The invention relates to novel 18-methyl-19-nor-17-pregn-4-en-21,17-carbolactones of general formula (I), where Z=O, H2, ?NOR or ?NNHSO2R, where R=H, a straight- or branched-chain 1-4 or 3-4 C alkyl group, R4=H, halogen, methyl or trifluoromethyl, R6 and/or R7 can be ?- or ?-positioned and independently=branched- or straight-chain 1-4 or 3-4 alkyl, or R6=H and R7=a- or ?-positioned, straight- or branched-chain 1-4 or 3-4 C alkyl, or R6 and R7=H, or R6 and R7 together=a- or ?-positioned methylene or an additional bond. The novel compounds have gestagenic and antimineralocorticoid activity and are suitable for the production of pharmaceutical preparations, for example, for oral contraception and the treatment of pre-, peri- and post-menopausal pain.
    Type: Application
    Filed: December 30, 2005
    Publication date: January 29, 2009
    Inventors: Rolf Bohlmann, Dieter Bittler, Hermann Kuenzer, Peter Esperling, Hans Peter Muhn, Karl Heinrich Fritzemeier, Ulrike Fuhrmann, Katja Prelle, Steffen Borden
  • Publication number: 20090029957
    Abstract: The invention refers to 8?-substituted estra-1,3,5(10)-triene derivatives of general formula I their use as pharmaceutical active ingredients, which have in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo a preferential action in the ovary in comparison to the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds.
    Type: Application
    Filed: July 11, 2008
    Publication date: January 29, 2009
    Inventors: Olaf Peters, Nico Braeuer, Ina Thieme, Katja Prelle, Peter Muhn, Karl Heinrich Fritzemeier
  • Patent number: 7414043
    Abstract: This invention describes the new 9?-substituted estratrienes of general formula I in which R3, R7, R7?, R13, R16 as well as R17 and R17? have the meanings that are indicated in the description and R9 means a straight-chain or branched-chain, optionally partially or completely halogenated alkenyl radical with 2 to 6 carbon atoms, an ethinyl or prop-1-inyl radical, as pharmaceutical active ingredients that exhibit in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo preferably a preferential action on the ovary in comparison to the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The invention also describes the use of these compounds for treating estrogen-deficiency-induced diseases and conditions.
    Type: Grant
    Filed: June 11, 2003
    Date of Patent: August 19, 2008
    Assignee: Schering AG
    Inventors: Dirk Kosemund, Gerd Mueller, Alexander Hillisch, Karl-Heinrich Fritzemeier, Peter Muhn
  • Publication number: 20080182829
    Abstract: This invention describes the new 8?-substituted estratrienes of general formula I in which R2, R3, R6, R6?, R7, R7?, R9, R11, R11?, R12, R14, R15, R15?, R16, R16?, R17, R17? have the meanings that are indicated in the description, and R8 means a straight-chain or branched-chain, optionally partially or completely halogenated alkyl or alkenyl radical with up to 5 carbon atoms, an ethinyl- or prop-1-inyl radical, as pharmaceutical active ingredients that have in vitro a higher affinity to estrogen receptor preparations of rat prostates than to estrogen receptor preparations of rat uteri and in vivo preferably a preferential action on bone rather than the uterus and/or a pronounced action with respect to stimulation of the expression of 5HT2a-receptors and 5HT2a-transporters, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds.
    Type: Application
    Filed: March 11, 2008
    Publication date: July 31, 2008
    Inventors: Olaf Peters, Alexander Hillisch, Ina Thieme, Walter Elger, Christa Hegele-Hartung, Uwe Kollenkirchen, Karl-Heinrich Fritzemeier, Vladimir Patchev
  • Publication number: 20080132476
    Abstract: This invention describes the new 9?-substituted estratrienes of general formula I in which R3, R7, R7?, R13, R16 as well as R17 and R17? have the meanings that are indicated in the description and R9 means a straight-chain or branched-chain, optionally partially or completely halogenated alkenyl radical with 2 to 6 carbon atoms, an ethinyl or prop-1-inyl radical, as pharmaceutical active ingredients that exhibit in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo preferably a preferential action on the ovary in comparison to the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The invention also describes the use of these compounds for treating estrogen-deficiency-induced diseases and conditions.
    Type: Application
    Filed: February 7, 2008
    Publication date: June 5, 2008
    Inventors: Dirk KOSEMUND, Gerd Mueller, Alexander Hillisch, Karl-Heinrich Fritzemeier, Peter Muhn
  • Patent number: 7378404
    Abstract: This invention describes the new 8?-substituted estratrienes of general formula I in which R2, R3, R6, R6?, R7, R7?, R9, R11, R11?, R12, R14, R15, R15?, R16, R16?, R17 and R17? have the meanings that are indicated in the description, and R8 means a straight-chain or branched-chain, optionally partially or completely halogenated alkyl or alkenyl radical with up to 5 carbon atoms, an ethinyl- or prop-1-inyl radical, as pharmaceutical active ingredients that have in vitro a higher affinity to estrogen receptor preparations of rat prostates than to estrogen receptor preparations of rat uteri and in vivo preferably a preferential action on bone rather than the uterus and/or a pronounced action with respect to stimulation of the expression of 5HT2a-receptors and 5HT2a-transporters, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds.
    Type: Grant
    Filed: April 12, 2001
    Date of Patent: May 27, 2008
    Assignee: Schering Aktiengesellschaft
    Inventors: Olaf Peters, Alexander Hillisch, Ina Thieme, Walter Elger, Christa Hegele-Hartung, Uwe Kollenkirchen, Karl-Heinrich Fritzemeier, Vladimir Patchev
  • Publication number: 20060270845
    Abstract: The invention describes new compounds as pharmaceutical active ingredients, which have in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo a preferential action on bone rather than the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The new compounds are 16?- and 16?-hydroxy-estra-1,3,5(10)-estratrienes, which carry additional substituents on the steroid skeleton and can have one or more additional double bonds in the B-, C- and/or D-rings.
    Type: Application
    Filed: August 3, 2006
    Publication date: November 30, 2006
    Inventors: Hermann Kuenzer, Rudolf Knauthe, Monika Lessl, Karl-Heinrich Fritzemeier, Christa Hegele-Hartung, Ulf Boemer, Gerd Mueller, Dirk Kosemund
  • Publication number: 20060252737
    Abstract: This invention describes the new 18-methyl-19-nor-17-pregn-4-ene-21,17-carbolactones of general formula I in which Z means an oxygen atom, two hydrogen atoms, a grouping ?NOR or ?NNHSO2R, whereby R is a hydrogen atom or a straight-chain or branched-chain alkyl group with 1 to 4 or 3 to 4 carbon atoms, R4 is a hydrogen atom, a halogen atom, a methyl group, or a trifluoromethyl group, R6 and/or R7 can be in ?- or ?-position, and, independently of one another, mean a straight-chain or branched-chain alkyl group with 1 to 4 or 3 to 4 carbon atoms, or R6 means a hydrogen atom, and R7 means an ?- or ?-position, straight-chain or branched-chain alkyl group with 1 to 4 or 3 to 4 carbon atoms, or R6 and R7 each mean a hydrogen atom, or R6 and R7 together mean an ?- or ?-position methylene group or an additional bond.
    Type: Application
    Filed: December 30, 2005
    Publication date: November 9, 2006
    Inventors: Rolf Bohlmann, Dieter Bittler, Hermann Kuenzer, Peter Esperling, Hans-Peter Muhn, Karl-Heinrich Fritzemeier, Ulrike Fuhrmann, Katja Prelle, Steffen Borden
  • Patent number: 7119082
    Abstract: This invention relates to new 19-nor-17?-pregna-1,3,5(10)-trien-17?-ols with a 21,16?-lactone ring with a long-chain substituent in 11?-position of general formula II in which R11 means a straight-chain alkyl radical with 6 to 17 carbon atoms, and R3 and R13 have the meanings that are explained in more detail in the description. The compounds act in a tissue-selective manner as pure antiestrogens and are suitable for the production of pharmaceutical agents because of these properties.
    Type: Grant
    Filed: March 27, 2003
    Date of Patent: October 10, 2006
    Assignee: Schering Aktiengesellschaft
    Inventors: Gerd Mueller, Jens Hoffmann, Karl-Heinrich Fritzemeier, Alexander Hillisch
  • Patent number: 7109360
    Abstract: The invention describes new compounds as pharmaceutical active ingredients, which have in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo a preferential action on bone rather than the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The new compounds are 16?- and 16?-hydroxy-estra-1,3,5(10)-estratrienes, which carry additional substituents on the steroid skeleton and can have one or more additional double bonds in the B-, C- and/or D-rings.
    Type: Grant
    Filed: February 4, 2000
    Date of Patent: September 19, 2006
    Assignee: Schering AG
    Inventors: Hermann Kuenzer, Rudolf Knauthe, Monika Lessl, Karl-Heinrich Fritzemeier, Christa Hegele-Hartung, Ulf Boemer, Gerd Mueller, Dirk Kosemund
  • Patent number: 7074829
    Abstract: This invention relates to new antiestrogens of the general formula in which the substituents have the meanings that are explained in more detail in the description. The new compounds are a) pure antiestrogens or b) antiestrogens with partial estrogenic action (tissue-selective estrogens). Based on these properties, the new compounds are suitable for the production of pharmaceutical agents: in the case of a), for example, for the treatment of breast cancer; in the case of b), for example, for hormone replacement therapy.
    Type: Grant
    Filed: February 21, 2003
    Date of Patent: July 11, 2006
    Assignee: Schering AG
    Inventors: Ulrich Klar, Rolf Bohlmann, Karsten Parczyk, Karl-Heinrich Fritzemeier, Monika Lessl, Rosemarie Lichtner
  • Publication number: 20050282791
    Abstract: This invention describes the new 18-nor steroids (gonatrienes) of general formula (I), in which R1, R2, R3, R6, R7, R8, R9, R11, R11?, R14, R15, R15, R16, R17 and R17? have the meanings that are indicated in the description, as pharmaceutical active ingredients that have in vitro a higher affinity to estrogen receptor preparations of rat prostates than to estrogen receptor preparations of rat uteri and in vivo a preferential action on bone in comparison to the uterus, and/or pronounced action relative to the stimulation of the expression of 5HT2a-receptors and transporters, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds.
    Type: Application
    Filed: July 20, 2005
    Publication date: December 22, 2005
    Inventors: Alexander Hillisch, Werner Boidol, Wolfgang Schwede, Peter Esperling, Gerhard Sauer, Christa Hegele-Hartung, Uwe Kollenkirchen, Karl-Heinrich Fritzemeier
  • Patent number: 6958327
    Abstract: The invention relates to novel 18-norsteroids (gonatrienes) of general formula (I), wherein R1, R2, R3, R6, R7, R8, R9, R11, R11?, R14, R15, R15?, R16, R17 and R17? have the meaning cited in the description, and to the use of said compounds as pharmaceutical active ingredients. Said compounds exhibit a high affinity in vitro for estrogen receptor preparations of rat prostate and in an estrogen receptor preparation of rat uterus. Said compounds exhibit in vivo preferential activity on bones as compared to the uterus and/or significant activity with regard to stimulating the expression of 5HT2a-receptors and transporter molecules. The invention also relates to the production of said compounds, therapeutic use and galenic form of said compounds contained in the novel compounds of invention.
    Type: Grant
    Filed: November 2, 2000
    Date of Patent: October 25, 2005
    Assignee: Schering, AG
    Inventors: Alexander Hillisch, Werner Boidol, Wolfgang Schwede, Peter Esperling, Gerhard Sauer, Christa Hegele-Hartung, Uwe Kollenkirchen, Karl-Heinrich Fritzemeier
  • Publication number: 20050148560
    Abstract: The present invention relates to the use of the ER? agonists 8?-Vinyl-estra-1,3,5(10)-trien-3,17?-diol and 17?-Fluor-9?-vinyl-estra-1,3,5(10)-trien-3,16?-diol for production of medicaments for the prevention and/or treatment of hypertensive heart disease, especially for the prevention and/or treatment of one or more of the conditions selected from the group of (1) hypertension, (2) cardiac hypertrophy and (3) heart failure.
    Type: Application
    Filed: November 24, 2004
    Publication date: July 7, 2005
    Inventors: Karl-Heinrich Fritzemeier, Christa Hegele-Hartung, Ludwig Neyses, Theo Pelzer, Olaf Peters
  • Publication number: 20050020695
    Abstract: The present invention discloses the use of ER?-selective ligands for production of medicaments for regulating fertility without additional use of a progestin. ER?-agonists are used for treatment of infertility and ER?-antagonists for contraception.
    Type: Application
    Filed: August 3, 2004
    Publication date: January 27, 2005
    Inventors: Christa Hegele-Hartung, Karl-Heinrich Fritzemeier, Hiroshi Yamanouchi, Olaf Peters, Dirk Kosemund, Gerd Mueller, Ingo Tornus, Gerd Schubert, Sven Ring
  • Patent number: 6844336
    Abstract: This invention describes the new 4-fluoroalkyl-2H-benzopyrans of general formula I, in which Z is a straight-chain or branched-chain alkyl group with up to 5 carbon atoms that is fluorinated in at least one place, preferably a trifluoromethyl group, and R1, R2, X, Y and n have the meanings that are indicated in the description. The new compounds have at their disposal strong antiestrogenic action. In addition, they can have at their disposal estrogenic action that occurs in a tissue-selective manner. They can be used for the production of pharmaceutical agents, especially for the treatment of estrogen-dependent diseases and tumors and pharmaceutical agents for hormone replacement therapy (HRT) as well as for the prevention and treatment of osteoporosis.
    Type: Grant
    Filed: March 15, 2001
    Date of Patent: January 18, 2005
    Assignee: Schering AG
    Inventors: Hermann Kuenzer, Rolf Jautelat, Ludwig Zorn, Christa Hegele-Hartung, Uwe Kollenkirchen, Karl-Heinrich Fritzemeier
  • Patent number: 6794409
    Abstract: The present invention discloses the use of ER&bgr;-selective ligands for production of medicaments for regulating fertility without additional use of a progestin. ER&bgr;-agonists are used for treatment of infertility and ER&bgr;-antagonists for contraception.
    Type: Grant
    Filed: February 27, 2002
    Date of Patent: September 21, 2004
    Assignee: Schering AG
    Inventors: Christa Hegele-Hartung, Karl-Heinrich Fritzemeier, Hiroshi Yamanouchi, Olaf Peters, Dirk Kosemund, Gerd Mueller, Ingo Tornus, Gerd Schubert, Sven Ring