Abstract: This invention provides novel peptides that function in vivo to stimulate insulin release from pancreatic beta cells in a glucose-dependent fashion. These insulin secretagogue peptides are shown to stimulate insulin release in rat islet cells in vitro, and in vivo. The peptides of the present invention provide a new therapy for patients with decreased endogenous insulin secretion, in particular type 2 diabetics. In particular, the invention is a polypeptide selected from a specific group of VIP/PACAP-related polypeptides, or functional equivalents thereof. The invention is also directed to a method of treating a metabolic disease in a mammal comprising administering a therapeutically effective amount of the insulin secretagogue peptides to said mammal. Also disclosed are methods of making the peptides, both recombinant and synthetic.
Type:
Grant
Filed:
September 27, 2000
Date of Patent:
December 6, 2005
Assignee:
Bayer Pharmaceuticals Corporation
Inventors:
Clark Pan, Manami Tsutsumi, Armen B. Shanafelt
Abstract: The invention relates generally to naphthyridine derivatives of the formula wherein one of U, X, Y and Z is nitrogen and the others are C—R, where R is hydrogen or a substituent. More specifically, the invention relates to 1,6-naphthyridine derivatives and pharmaceutical compositions containing such derivatives. Methods of the invention comprise administration of a naphthyridine derivative of the invention for the treatment of diabetes and related disorders.
Type:
Grant
Filed:
October 10, 2003
Date of Patent:
November 15, 2005
Assignee:
Bayer Pharmaceuticals Corporation
Inventors:
Yamin Wang, William H. Bullock, Libing Chen
Abstract: This invention relates to substituted imidazole derivatives which have been found to suppress appetite and induce weight loss. The invention also provides methods for synthesis of the compounds, pharmaceutical compositions comprising the compounds, and methods of using such compositions for inducing weight loss and treating obesity and obesity-related disorders.
Type:
Grant
Filed:
September 24, 2002
Date of Patent:
November 1, 2005
Assignee:
Bayer Pharmaceuticals Corporation
Inventors:
Roger A. Smith, Stephen J. O'Connor, Stephan-Nicholas Wirtz, Wai C. Wong, Soongyu Choi, Harold C. E. Kluender, Ning Su, Gan Wang, Furahi Achebe, Shihong Ying
Abstract: The invention relates to cyclopentabenzofuran derivatives, process for their preparation, the use of cyclopentabenzofuran derivatives for the production of a medicament for the therapy of NF-?B-dependent diseases and medicaments which contain the cyclopentabenzofuran derivatives.
Type:
Grant
Filed:
May 30, 2002
Date of Patent:
September 13, 2005
Assignee:
Bayer Aktiengesellschaft
Inventors:
Walter Guarnieri, Thomas Jaetsch, Andreas Schoop, Jörg Baumgarten, Axel Kretschmer, Horst-Peter Antonicek
Abstract: The present invention relates to 7-alkyl- and cycloalkyl-substituted imidazotriazinones, to processes for their preparation and to their use as medicaments, in particular as inhibitors of cGMP-metabolizing phosphodiesterases.
Type:
Grant
Filed:
May 20, 2004
Date of Patent:
September 13, 2005
Assignee:
Bayer Aktiengesellschaft
Inventors:
Ulrich Niewöhner, Mazen Es-Sayed, Helmut Haning, Thomas Schenke, Gunter Schmidt, Karl-Heinz Schlemmer, Erwin Bischoff, Klaus Dembowsky, Elisabeth Perzborn
Abstract: The invention relates to new imidazotriazines, processes for their preparation, and their use for the production of medicaments for the treatment and/or prophylaxis of neurodegenerative disorders, in particular Parkinson's disease.
Type:
Grant
Filed:
June 10, 2002
Date of Patent:
August 30, 2005
Assignee:
Bayer HealthCare AG
Inventors:
Jens-Kerim Ergüden, Marcus Bauser, Nils Burkhardt, Dietmar Flubacher, Arno Friedl, Irene Gerlach, Volker Hinz, Reinhard Jork, Paul Naab, Maria Theresia Niewöhner, Thorsten Oliver Repp, Karl-Heinz Schlemmer, Jürgen Stoltefuss, David Brückner, Martin Hendrix, Dagmar Schauss, Adrian Tersteegen, Ulrich Niewöhner
Abstract: The present invention relates to pyrrolo[2.1-a]dihydroisoquinolines which are inhibitors of phosphodiesterase 10a and can be used for combating cancer.
Type:
Grant
Filed:
December 4, 2001
Date of Patent:
August 16, 2005
Assignee:
Bayer Pharmaceuticals Corporation
Inventors:
Maria Theresia Niewöhner, Marcus Bauser, Jens-Kerim Ergüden, Dietmar Flubacher, Paul Naab, Thorsten-Oliver Repp, Jürgen Stoltefuss, Nils Burkhardt, Andrea Sewing, Michael Schauer, Karl-Heinz Schlemmer, Olaf Weber, Stephen J. Boyer, Mark Miglarese, Ulrich Niewöhner
Abstract: The present invention relates to the use of known 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position and cGMP PDE-inhibitory properties for the production of medicaments for the treatment of cardiac insufficiency, psoriasis, female infertility, cancer, diabetes, ophthalmic disorders such as glaucoma, disorders of gastric motility, cystic fibrosis, premature labour, pulmonary hypertension, bladder disorders, prostate hyperplasia, nitrate-induced tolerance, pre-eclampsia, alopecia, Parkinson's disease, pain, tinnitus or the renal syndrome.
Type:
Grant
Filed:
July 17, 2002
Date of Patent:
August 16, 2005
Assignee:
Bayer HealthCare AG
Inventors:
Maria Theresia Niewöhner, Erwin Bischoff, Helmut Haning, Afssaneh Rahbar, Tiemo-Joerg Bandel, Wolfgang Barth, Ulrich Niewöhner
Abstract: The present invention relates to chromans, to processes for their preparation and to their use in medicaments, in particular as agents for treating disorders of the central nervous system.
Type:
Grant
Filed:
September 18, 2002
Date of Patent:
July 19, 2005
Assignee:
Bayer HealthCare AG
Inventors:
Dietrich Scherling, Wolfgang Karl, Dietrich Seidel, Corinna Weinz, Rudolf Schohe-Loop, Frank Mauler
Abstract: This invention relates to novel 2,6-substituted chroman derivatives which are useful in the treatment of beta-3 adrenoreceptor-mediated conditions.
Type:
Grant
Filed:
September 17, 2003
Date of Patent:
July 19, 2005
Assignee:
Bayer Pharmaceuticals Corporation
Inventors:
Stephen J. O'Connor, Gaetan H. Ladouceur, William H. Bullock, Ann-Marie Campbell, Miao Dai, Robert Dally, Jacques Dumas, Holia N. Hatoum-Mokdad, Uday Khire, Wendy Lee, Qingjie Liu, Derek B. Lowe, Steven R. Magnuson, Ning Qi, Tatiana E. Shelekhin, Quanrong Shen, Roger A. Smith, Ming Wang
Abstract: The invention relates to novel aryl and heteroaryl sulfonates of formula (Ia) and to methods for producing them and to novel aryl and heteroaryl sulfonates of formula (I) for treating and/or preventing diseases, especially for treating pain and neurodegenerative diseases, A representing (C6-C10)-aryl or 5-10-membered heteroaryl, D representing (C6-C10)-arylene or 5-10-membered heteroarylene, R1 representing (C4-C8)-alkyl, (C2-C8)-alkyl, the carbon chain being interrupted by one or two heteroatoms or groups chosen from the following group: —O—, —S—, —SO— and —SO2—, (C2-C8)-alkenyl or (C2-C8)-alkinyl, in formula (Ia); and R1 representing (C3-C8)-alkyl, (C2-C8)-alkyl, the carbon chain being interrupted by one or two heteroatoms or groups chosen from the following group: —O—, —S—,—SO— and —SO2—, (C2-C8)-alkenyl or (C2-C8)-alkinyl.
Type:
Grant
Filed:
March 19, 2001
Date of Patent:
July 19, 2005
Assignee:
Bayer Aktiengesellschaft
Inventors:
Markus Heil, Heinrich Meier, Paul Naab, Arnd Voerste, Jean-Marie-Viktor de Vry, Dirk Denzer, Frank Mauler, Klemens Lustig, Volker Hinz, Swen Allerheiligen
Abstract: This invention related to novel sulfonamide substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.
Type:
Grant
Filed:
September 19, 2003
Date of Patent:
June 7, 2005
Assignee:
Bayer Pharmaceuticals Corporation
Inventors:
Gaetan H. Ladouceur, Richard D. Connell, Jeremy Baryza, Ann-Marie Campbell, Timothy G. Lease, James H. Cook
Abstract: The invention relates generally to naphthyridine derivatives of the formula wherein one of U, X, Y and Z is nitrogen and the others are C—R, where R is hydrogen or a substituent. More specifically, the invention relates to 1,8-naphthyridine derivatives and pharmaceutical compositions containing such derivatives. Methods of the invention comprise administration of a naphthyridine derivative of the invention for the treatment of diabetes and related disorders.
Type:
Grant
Filed:
September 23, 2002
Date of Patent:
May 31, 2005
Assignee:
Bayer Pharmaceuticals Corporation
Inventors:
Yamin Wang, William H. Bullock, David E. Gunn, Qingjie Liu, Sidney X. Liang, Donglei Liu, Steven R. Magnuson, Tindy Li, Eric S. Mull, Jill E. Wood, Ning Qi
Abstract: The 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP-metabolizing phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for the treatment of cardiovascular and cerebrovascular disorders and/or disorders of the urogenital system, in particular for the treatment of erectile dysfunction.
Type:
Grant
Filed:
February 12, 2003
Date of Patent:
May 10, 2005
Assignee:
Bayer Healthcare AG
Inventors:
Maria Niewohner, Mazen Es-Sayed, Helmut Haning, Thomas Schenke, Karl-Heinz Schlemmer, Jörg Keldenich, Erwin Bischoff, Elisabeth Perzborn, Klaus Dembowsky, Peter Serno, Marc Nowakowski, Ulrich Niewöhner
Abstract: Novel imidazotriazinones of general formula (I), a method for the production and the pharmaceutical use thereof are disclosed.
Type:
Grant
Filed:
February 20, 2001
Date of Patent:
April 12, 2005
Assignee:
Bayer Aktiengesellschaft
Inventors:
Maria Niewöhner, Mazen Es-Sayed, Thomas Lampe, Helmut Haning, Gunter Schmidt, Karl-Heinz Schlemmer, Erwin Bischoff, Klaus Dembowsky, Elisabeth Perzborn, Ulrich Niewöhner
Abstract: The invention provides polypeptides that act both as an agonist of the GLP-1 receptor and an antagonist of the glucagon receptor. Such polypeptides are useful for treating individuals with type 2 diabetes or other metabolic disorders.
Type:
Grant
Filed:
October 3, 2002
Date of Patent:
March 8, 2005
Assignee:
Bayer Pharmaceuticals Corporation
Inventors:
Clark Pan, James Whelan, Kevin B. Clairmont
Abstract: The present invention relates to 7-alkyl- and cycloalkyl-substituted imidazotriazinones, to processes for their preparation and to their use as medicaments, in particular as inhibitors of cGMP-metabolizing phosphodiesterases.
Type:
Grant
Filed:
September 20, 2002
Date of Patent:
January 4, 2005
Assignee:
Bayer Aktiengesellschaft
Inventors:
Ulrich Niewöhner, Mazen Es-Sayed, Helmut Haning, Thomas Schenke, Gunter Schmidt, Karl-Heinz Schlemmer, Erwin Bischoff, Klaus Dembowsky, Elisabeth Perzborn
Abstract: The invention relates to imidazo[1.3.5]triazinones, a method for their production and methods of use, in particular as inhibitors of cyclic GMP metabolizing phosphodiesterases.
Type:
Grant
Filed:
November 4, 2002
Date of Patent:
October 12, 2004
Assignee:
Bayer Aktlengesellschaft
Inventors:
Ulrich Niewöhner, Helmut Haning, Thomas Lampe, Mazen Es-Sayed, Gunter Schmidt, Erwin Bischoff, Klaus Dembowsky, Elisabeth Perzborn, Karl-Heinz Schlemmer
Abstract: This invention is related to novel carboxyl substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.
Type:
Grant
Filed:
August 21, 2002
Date of Patent:
September 28, 2004
Assignee:
Bayer Pharmaceuticals Corporation
Inventors:
Richard D. Connell, Timothy G. Lease, Jeremy L. Baryza