Patents by Inventor Witold Neugebauer
Witold Neugebauer 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: 9809621Abstract: It is provided PACE4 inhibitors and their uses for treating infection, cancer. Particularly, it is provided a method or use for the treatment of a cancer in a subject, comprising administering to the subject a therapeutically effective amount of the PACE4 inhibitors or the composition disclosed.Type: GrantFiled: August 30, 2012Date of Patent: November 7, 2017Assignee: SOCPRA SCIENCES SANTÉ ET HUMAINES S.E.C.Inventors: Robert Day, Witold A. Neugebauer, Yves Dory
-
Patent number: 9573974Abstract: Disclosed herein are PACE4 inhibitors, compositions comprising PACE4 inhibitors and their uses thereof for lowering PACE4 activity, reducing cell proliferation, reducing tumor growth, reducing metastasis formation, preventing and/or treating cancer. Also provided are methods for lowering PACE4 activity, reducing the proliferation of a cell, reducing tumor growth and/or treating and preventing cancer. Methods for screening PACE4 inhibitors and cell proliferation inhibitors are further provided.Type: GrantFiled: January 8, 2014Date of Patent: February 21, 2017Assignee: LA SOCIETE DE COMMERCIALISATION DES PRODUITS DE LA RECHERCHE APPLIQUEE SOCPRA-SCIENCES SANTE ET HUMAINES S.E.C.Inventors: Robert Day, Martin Fugére, Witold A. Neugebauer
-
Publication number: 20150141324Abstract: It is provided furin inhibitors and their uses for treating pathogen infection. Particularly, it is provided a method or use for the treatment of a pathogen infection, in a subject, comprising administering to the subject a therapeutically effective amount of the furin inhibitors or the composition disclosed, thereby preventing or treating pathogen infection, in the subject.Type: ApplicationFiled: August 31, 2012Publication date: May 21, 2015Applicant: SOCPRA SCIENCES SANTE ET HUMAINES S.E.C.Inventors: Robert Day, Witold A. Neugebauer, Yves Dory
-
Publication number: 20140256646Abstract: Disclosed herein are PACE4 inhibitors, compositions comprising PACE4 inhibitors and their uses thereof for lowering PACE4 activity, reducing cell proliferation, reducing tumor growth, reducing metastasis formation, preventing and/or treating cancer. Also provided are methods for lowering PACE4 activity, reducing the proliferation of a cell, reducing tumor growth and/or treating and preventing cancer. Methods for screening PACE4 inhibitors and cell proliferation inhibitors are further provided.Type: ApplicationFiled: January 8, 2014Publication date: September 11, 2014Applicant: Societe De Commercialisation Des Produits De La Recherche Appliquee Socpra SanInventors: Robert Day, Martin Fugére, Witold A. Neugebauer
-
Publication number: 20140206622Abstract: It is provided PACE4 inhibitors and their uses for treating infection, cancer. Particularly, it is provided a method or use for the treatment of a cancer in a subject, comprising administering to the subject a therapeutically effective amount of the PACE4 inhibitors or the composition disclosed.Type: ApplicationFiled: August 30, 2012Publication date: July 24, 2014Applicant: SOCPRA SCIENCES SANTE ET HUMAINES S.E.C.Inventors: Robert Day, Witold A. Neugebauer, Yves Dory
-
Patent number: 8658591Abstract: Disclosed herein are PACE4 inhibitors, compositions comprising PACE4 inhibitors and their uses thereof for lowering PACE4 activity, reducing cell proliferation, reducing tumor growth, reducing metastasis formation, preventing and/or treating cancer. Also provided are methods for lowering PACE4 activity, reducing the proliferation of a cell, reducing tumor growth and/or treating and preventing cancer. Methods for screening PACE4 inhibitors and cell proliferation inhibitors are further provided.Type: GrantFiled: July 6, 2009Date of Patent: February 25, 2014Inventors: Robert Day, Martin Fugère, Witold A. Neugebauer
-
Publication number: 20120129774Abstract: The present invention provides for novel kinin B1 receptors peptide agonists of formula (1) having very good to excellent affinities and selectivity for the B1 receptor, in vitro and in vivo increased resistance to enzymatic degradation, superior pharmacokinetic properties to those of naturally occurring agents, capacity to significantly enhance delivery of chemotherapeutic substances across the blood brain barrier and within peripheral tissues for the treatment of tumors, capacity to protect and restore kidney, heart, brain and other organ functions, when given alone or in combination with other therapies in the treatment of hypertension, diabetes and other cardiovascular diseases particularly, but not limited to, atherosclerosis and arteriosclerosis.Type: ApplicationFiled: November 11, 2011Publication date: May 24, 2012Inventors: Fernand GOBEIL, Witold A. NEUGEBAUER, Domenico REGOLI, David FORTIN
-
Patent number: 8076453Abstract: The present invention provides for novel kinin B1 receptors peptide agonists of formula (I) having very good to excellent affinities and selectivity for the B1 receptor, in vitro and in vivo increased resistance to enzymatic degradation, superior pharmacokinetic properties to those of naturally occurring agents, capacity to significantly enhance delivery of chemotherapeutic substances across the blood brain barrier and within peripheral tissues for the treatment of tumors, capacity to protect and restore kidney, heart, brain and other organ functions, when given alone or in combination with other therapies in the treatment of hypertension, diabetes and other cardiovascular diseases particularly, but not limited to, atherosclerosis and arteriosclerosis. Formula (I): aay-aax-aa0-aa1-aa2-aa3-aa4-aa5-Ser6-Pro7-D-Phe8-X.Type: GrantFiled: May 31, 2006Date of Patent: December 13, 2011Assignee: Societe De Commercialisation Des Produits De La Recheche Appliquee-Socpra-Science Sante Et Humaines S.E.C.Inventors: Fernand Gobeil, Jr., Witold A. Neugebauer, Domenico Regoli, David Fortin
-
Publication number: 20090054347Abstract: The present invention provides for novel kinin B1 receptors peptide agonists of formula (I) having very good to excellent affinities and selectivity for the B1 receptor, in vitro and in vivo increased resistance to enzymatic degradation, superior pharmacokinetic properties to those of naturally occurring agents, capacity to significantly enhance delivery of chemotherapeutic substances across the blood brain barrier and within peripheral tissues for the treatment of tumors, capacity to protect and restore kidney, heart, brain and other organ functions, when given alone or in combination with other therapies in the treatment of hypertension, diabetes and other cardiovascular diseases particularly, but not limited to, atherosclerosis and arteriosclerosis. Formula (I): aay-aax-aa0-aa1-aa2-aa3-aa4-aa5-Ser6-Pro7-D-Phe8-X.Type: ApplicationFiled: May 31, 2006Publication date: February 26, 2009Inventors: Fernand Gobeil, JR., Witold A. Neugebauer, Domenico Regoli, David Fortin
-
Publication number: 20080064642Abstract: The present invention provides for new peptidic and peptidoid Bradykinin B1 receptor antagonists of formula (1) having good to excellent affinities and selectivity for the BKB1 receptor, and increased resistance to enzymatic degradation, superior pharmacokinetic properties, both in vitro and in vivo, with capability to significantly prevent and treat conditions wherein BKB1Rs are induced and over-expressed.Type: ApplicationFiled: August 19, 2005Publication date: March 13, 2008Applicant: UNIVERSITE DE SHERBROOKEInventors: Brigitte Guerin, Bruno Battistini, Fernand Gobeil, Francois Nantel, Witold Neugebauer, Gerard Plante, Domenico Regoli, Pierre Sirois
-
Patent number: 7211566Abstract: The present invention provides for a novel peptidic antagonist for the bradykinin B1 (BKB1) receptor having very good to excellent affinities and selectivity for the BKB1 receptor, in vitro and in vivo increase resistance to enzymatic degradation, superior pharmacokinetic properties, capability to significantly reduce microvascular leakage observed alongside diabetic-induced increase in vascular permeability, capability to significantly reduced the state of hyperalgesia alongside diabetes, capability to significantly reduce the infiltration of pro-inflammatory cells and general state of inflammation alongside allergic asthma.Type: GrantFiled: April 1, 2003Date of Patent: May 1, 2007Assignee: Universite De SherbrookeInventors: Domenico Regoli, Witold Neugebauer, Fernand Gobeil, Bichov Gabra, Pierre Sirois
-
Patent number: 7041785Abstract: The present invention relates to novel antagonists to a B1-bradykinin (B1-BK) receptor which have a good affinity and selectivity therefor, some of which being at least partially resistant to enzymatic degradation. The synthesis of the B1 receptors is induced during inflammation. Symptoms associated with inflammation (elevated hydrostatic pressure and plasma leakage or extravasation) have been observed in diabetic animal models (streptozotocin-induced diabetes (STZ)) as well as in spontaneously hypertensive rats (SHR). The present inventors confirm the presence of B1-BK receptors in these two models. B1-BK antagonists abolished the vasocontraction induced by B1-BK in SHR and STZ, and reduced the glycemia of diabetic animals to normal levels.Type: GrantFiled: August 14, 1997Date of Patent: May 9, 2006Assignee: Université de SherbrookeInventors: Domenico Recoli, Gerard E. Plante, Fernand Gobeil, Witold A. Neugebauer, Adriana Zucollo, Orlando L. Catanzaro
-
Publication number: 20040198666Abstract: The present invention provides for a novel peptidic antagonist for the bradykinin B1 (BKB1) receptor having very good to excellent affinities and selectivity for the BKB1 receptor, in vitro and in vivo increase resistance to enzymatic degradation, superior pharmacokinetic properties, capability to significantly reduce microvascular leakage observed alongside diabetic-induced increase in vascular permeability, capability to significantly reduced the state of hyperalgesia alongside diabetes, capability to significantly reduce the infiltration of pro-inflammatory cells and general state of inflammation alongside allergic asthma.Type: ApplicationFiled: April 1, 2003Publication date: October 7, 2004Inventors: Domenico Regoli, Witold A. Neugebauer, Fernand Gobeil, Bichoy Gabra, Pierre Sirois
-
Patent number: 6541450Abstract: This invention describes analogues of human parathyroid hormone which have increased activities in bone restoration, and increased bioavailability. The peptides described are derivatives of hPTH-(1-31) which are cyclized for example, by formation of lactams between either Glu22 and Lys26 or Lys26 and Asp30. In addition, the natural Lys27 may be substituted by either a Leu or other hydrophobic residues, such as Ile, norleucine, Met, Val, Ala, Trp, or Phe. Typically, these analogues have enhanced abilities to stimulate adenylyl cyclase in rat osteosarcoma cells, and show increased activities in bone restoration, using the ovariectomized rat model. The analogues also show enhanced activities and bioavailabilities, as demonstrated by their hypotensive effects in the rat. An assay which correlates hypotensive activity with osteogenic activity is also described.Type: GrantFiled: March 28, 2000Date of Patent: April 1, 2003Assignee: National Research Council of CanadaInventors: Jean-Rene Barbier, Paul Morley, Witold Neugebauer, James F. Whitfield, Gordon E. Willick
-
Patent number: 6110892Abstract: This invention describes analogues of human parathyroid hormone which have increased activities in bone restoration, and increased bioavailabilities. The peptides described are derivatives of hPTH-(1-31) which are cyclized for example, by formation of lactams between either Glu.sup.22 and Lys.sup.26 or Lys.sup.26 and Asp.sup.30. In addition, the natural Lys.sup.27 may be substituted by either a Leu or other hydrophobic residues, such as Ile, norleucine, Met, Val, Ala, Trp, or Phe. Typically, these analogues have enhanced abilities to stimulate adenylyl cyclase in rat osteosarcoma cells, and show increased activities in bone restoration, using the ovariectomized rat model. The analogues also show enhanced activities and bioavailabilities, as demonstrated by their hypotensive effects in the rat. An assay which correlates hypotensive activity with osteogenic activity is also described.Type: GrantFiled: August 1, 1997Date of Patent: August 29, 2000Assignee: National Research Council of CanadaInventors: Jean-Rene Barbier, Paul Morley, Witold Neugebauer, Virginia J. S. Ross, James F. Whitfield, Gordon E. Willick
-
Patent number: 5955425Abstract: This invention describes analogs of human parathyroid hormone which have increased activities in bone restoration, and increased bioavailabilities. The peptides described are derivatives of hPTH-(1-31) which have lactams formed for example, between either Glu.sup.22 and Lys.sup.26 or Lys.sup.26 and Asp.sup.30. In addition, the natural Lys.sup.27 may be substituted by either a Leu or other hydrophobic residues, such as Ile, norleucine, Met, Val, Ala, Trp, or Phe. Typically, these analogs have enhanced abilities to stimulate adenylyl cyclase in rat osteosarcoma cells, and show increased activities in bone restoration, using the ovariectomized rat model. The analogs also show enhanced activities and bioavailabilities, as demonstrated by their hypotensive effects in the rat.Type: GrantFiled: August 2, 1996Date of Patent: September 21, 1999Assignee: National Research Council of CanadaInventors: Paul Morley, Witold Neugebauer, Virginia J. S. Ross, James F. Whitfield, Gordon E. Willick, Jean-Rene Barbier
-
Patent number: 5556940Abstract: Certain analogues of human parathyroid hormone (hPTH) have been found to be effective for the treatment of osteoporosis, while showing decreased side effects. Analogues showing this effect include all sequences from hPTH-(1-28)-NH.sub.2 to hPTH-(1-31)-NH.sub.2 and all sequences from [Leu.sup.27 ]-hPTH-(1-28)-NH.sub.2 to [Leu.sup.27 ]-hPTH-(1-33)-NH.sub.2. Also included are cyclic analogues cyclo(Lys.sup.26 -Asp.sup.30) [Leu.sup.27 ]-hPTH-(1-34)NH.sub.2 and cyclo (Lys.sup.27 -Asp.sup.30 )-hPTH-(1-34)-NH.sub.2. Analogues in the form of the carboxyl terminal amide are particularly effective.Type: GrantFiled: June 20, 1994Date of Patent: September 17, 1996Assignee: National Research Council of CanadaInventors: Gordon E. Willick, James F. Whitfield, Witold Surewicz, Wing L. Sung, Witold Neugebauer