Abstract: This invention is directed to compounds of formula (I): where A, B, D, E, m, and R1-R5 are as described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, clathrates, or prodrugs thereof, which compounds are useful in treating respiratory diseases associated with influenza A viruses, such as for example H5N1 and its mutations. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
Abstract: The present invention relates to antibodies, and antigen-binding antibody fragments, directed against an RG1 polypeptide. The invention further relates to methods for utilizing the antibodies, and antibody fragments, for diagnostic and therapeutic applications.
Abstract: An injection device for holding and activating a two-chamber ampulla has components whose relative movement causes the pistons of the two-chamber ampulla to be moved in order to mix the substances, as well as devices for injecting the product which is mixed in this way. For this purpose, a receptacle (103) into which the two-chamber ampulla (111) can be inserted and secured is held in a housing (101), and the receptacle (103) can be displaced by means of a carriage (108). A tappet (104) which acts on the pistons (111A, 111B) is movably held in the receptacle (103). A traction cable (114) which is deflected by means of a roller (109) which is mounted on the carriage (108) and one of whose ends is connected to the receptacle (103) and the other end of which is connected to a tension spring (110) which is held on the housing (101) is provided in order to carry out a mixing stroke, insertion stroke, injection stroke and a return stroke.
Abstract: This invention relates to the new epothilone derivatives of general formula I, in which substituents Y, Z, R2a, R2b, R3, R4a, R4b, D-E, R5, R6, R7, R8 and X have the meanings that are indicated in more detail in the description. The new compounds interact with tubulin by stabilizing microtubuli that are formed. They are able to influence the cell-splitting in a phase-specific manner and are suitable for treating malignant tumors, for example, ovarian, stomach, colon, adeno-, breast, lung, head and neck carcinomas, malignant melanomas, acute lymphocytic and myelocytic leukemia. In addition, they are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases (psoriasis, arthritis). To avoid uncontrolled proliferation of cells and for better compatibility of medical implants, they can be applied or introduced into polymer materials.
Type:
Grant
Filed:
August 10, 1998
Date of Patent:
August 5, 2008
Assignee:
Bayer Schering Pharma AG
Inventors:
Ulrich Klar, Wolfgang Schwede, Werner Skuballa, Bernd Buchmann
Abstract: This invention is directed to the crystalline potassium salt of a lipoxin A4 analog of Formula (I): processes for preparing the crystalline potassium salts, methods for using them to treat disease-states characterized by inflammation, and pharmaceutical compositions comprising such crystalline potassium salts.
Abstract: This invention is directed to a crystalline acid of a lipoxin A4 analog of Formula (II): wherein: R1 is —O—, —S(O)t— (where t is 0, 1 or 2), or a straight or branched alkylene chain; and R2 is aryl (optionally substituted by one or more substituents selected from alkyl, alkoxy, halo, haloalkyl and haloalkoxy) or aralkyl (optionally substituted by one or more substituents selected from f alkyl, alkoxy, halo, haloalkyl and haloalkoxy); and wherein the compound of Formula (II) is a single stereoisomer or any mixture of stereoisomers. This crystalline acid is useful in treating disease-states characterized by inflammation, such as inflammatory and autoimmune disorders or pulmonary or respiratory tract inflammations in humans. Methods of preparing the crystalline acid are also described.
Abstract: The present invention relates to non-steroidal progestins of the general formula (I) wherein R1 and R2 are independently of each other —H or —F, R3 is —CH3 or —CF3, and Ar is or a pharmaceutically acceptable derivative or analogue thereof. These progestins are suitable for selectively modulating progesterone receptor mediated effects in different target tissues, particularly in uterine tissue versus breast tissue. Therefore, the progestins of the present invention, optionally in combination with estrogens, may be used for contraception (in particular in estrogen-free oral contraceptives), hormone replacement therapy and the treatment of gynecological disorders. The present invention furthermore relates to methods for selectively modulating progesterone receptor mediated effects in different target tissues or organs.
Type:
Grant
Filed:
March 11, 2003
Date of Patent:
June 17, 2008
Assignee:
Bayer Schering Pharma AG
Inventors:
Norbert Schmees, Manfred Lehmann, Ulrike Fuhrmann, Peter Muhn, Christa Hegele-Hartung, Michael Klotzbuecher
Abstract: The invention relates to ?15-D-homosteroids of general formula (I) process for their production and pharmaceutical compositions that contain these compounds. The compounds of general formula I according to the invention have androgenic activity.
Type:
Grant
Filed:
August 23, 2004
Date of Patent:
June 17, 2008
Assignee:
Bayer Schering Pharma AG
Inventors:
Ralf Wyrwa, Sven Ring, Guenter Kaufmann, Walter Elger, Birgitt Schneider
Abstract: The present invention relates to antibodies, and antigen-binding antibody fragments, directed against an RG1 polypeptide. The invention further relates to methods for utilizing the antibodies, and antibody fragments, for diagnostic and therapeutic applications.
Abstract: The invention relates to new protected 3,5-dihydroxy-2,2-dimethyl-valeroarnides for the synthesis of edothilones and derivatives and process for the production and the use of the new compounds for the production of epothilones or epothilone derivatives.
Type:
Grant
Filed:
June 10, 2005
Date of Patent:
May 6, 2008
Assignee:
Bayer Schering Pharma AG
Inventors:
Jurgen Westermann, Johannes Platzek, Orlin Petrov
Abstract: The invention relates to 11?-halogen steroids with general formula (I), whereby R11 is halogen, X—Y-Z represents a group with one of the two structures CH?C—C or CH2—C?C and the other radicals have the meaning that is indicated in the claims, also the production and use of these compounds for the production of pharmaceutical agents as well as pharmaceutical preparations that contain 11?-halogen steroids.
Type:
Grant
Filed:
January 24, 2002
Date of Patent:
April 22, 2008
Assignee:
Bayer Schering Pharma AG
Inventors:
Rolf Bohlmann, Hermann Kuenzer, Reinhard Nubbemeyer, Dieter Zopf
Abstract: The invention relates to 3,5-dihydroxy-2,2-dimethyl-valeronitriles for the synthesis of epothilones and epothilone derivatives and process for the production of these new intermediate products in the synthesis and the use for the production of epothilones or epothilone derivatives.
Type:
Grant
Filed:
July 26, 2005
Date of Patent:
April 15, 2008
Assignee:
Bayer Schering Pharma AG
Inventors:
Jurgen Westermann, Johannes Platzek, Orlin Petrov
Abstract: The present invention relates to antibodies, and antigen-binding antibody fragments, directed against an RG1 polypeptide. The invention further relates to methods for utilizing the antibodies, and antibody fragments, for diagnostic and therapeutic applications.
Abstract: This invention relates to processes for the production of 3-oxo-pregnane-21,17-carbolactones of formula II as well as 3-oxo-pregn-4-ene-21,17-carbolactones of formula III by the metal-free oxidation of 17-(3-hydroxypropyl)-3,17-dihydroxyandrostanes of formula I In addition, the invention relates to the dichloromethane hemisolvate of 6B,7B;15?,16?-diethylene-3-oxo-17?-pregnan-5?-ol-21,17-carbolactone (IV) as such.
Abstract: Macrocyclic pyrimidine derivatives of general formula I in which R1 to R5, X, Y, A, B, m and n have the meanings that are contained in the description, as inhibitors of the cyclin-dependent kinase, their processes for production as well as their use as medications for treating various diseases are described.
Type:
Grant
Filed:
August 20, 2003
Date of Patent:
December 25, 2007
Assignee:
Bayer Schering Pharma AG
Inventors:
Ulrich Luecking, Gerhard Siemeister, Martina Schaefer, Hans Briem
Abstract: The present invention relates to novel human extracellular matrix polypeptides, designated RG1, polynucleotides encoding the polypeptides, methods for producing the polypeptides, expression vectors and genetically engineered host cells for expression of the polypeptides. The invention further relates to methods for utilizing the polynucleotides and polypeptides in research, diagnosis, and therapeutic applications.
Abstract: This invention relates to pyrimidine derivatives of general formula I in which R1, R2, X, A and B have the meanings that are contained in the description, as inhibitors of the cyclin-dependent kinases, their production as well as their use as medications for treating various diseases.
Type:
Grant
Filed:
May 11, 2004
Date of Patent:
November 6, 2007
Assignee:
Bayer Schering Pharma AG
Inventors:
Thomas Brumby, Rolf Jautelat, Olaf Prien, Martina Schäfer, Gerhard Siemeister, Ulrich Lücking, Christoph Huwe
Abstract: A novel method of synthesis for the manufacture of upstream products for the production of compounds with general formulas 8, 10, and 12 is described. In this synthesis, compounds with general formula 4,B are produced in a microbiological reaction.
Type:
Grant
Filed:
July 24, 2003
Date of Patent:
August 28, 2007
Assignee:
Bayer Schering Pharma AG
Inventors:
Ludwig Zorn, Rolf Bohlmann, Norbert Gallus, Hermann Kuenzer, Hans-Peter Muhn, Reinhard Nubbemeyer
Abstract: The present invention provides compositions and methods that modulate MDL-1 activity in a cell, in vivo or in vitro. In particular, the present invention provides methods for treatment of inflammatory diseases using synthetic or recombinant compositions that modulate MDL-1 activity in a mammalian cell, in vivo or in vitro. More particularly, the present invention provides protein compositions useful for the treatment of diseases having an inflammatory process mediated by MDL-1.
Type:
Application
Filed:
January 26, 2007
Publication date:
August 2, 2007
Applicant:
BAYER SCHERING PHARMA AG
Inventors:
Daryl Faulds, Stefano Fiorucci, Ying-Ping Jiang, Yi Liu, John Parkinson