Patents by Inventor Tesfaye Biftu

Tesfaye Biftu 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).

  • Publication number: 20060211682
    Abstract: The present invention is directed to hexahydrodiazepinone compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Application
    Filed: July 27, 2004
    Publication date: September 21, 2006
    Inventors: Gui-Bai Liang, Tesfaye Biftu, Danqing Feng, Ann Weber
  • Patent number: 7101871
    Abstract: The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: October 14, 2003
    Date of Patent: September 5, 2006
    Assignee: Merck & Co., Inc.
    Inventors: Tesfaye Biftu, Gui-Bai Liang, Xiaoxia Qian, Ann E. Weber, Danqing Dennis Feng
  • Publication number: 20060178358
    Abstract: Compounds described by the Formula (I): (I) or pharmaceutically acceptable salts, or N-oxides thereof. The compounds are useful for the treatment and prevention of protozoal diseases in mammals and birds. A method for controlling coccidiosis in poultry comprises administering an effective amount of the compound alone, or in combination with one or more anticoccidial agent(s). A composition for controlling coccidiosis in poultry comprises the compound alone, or in combination with one or more anticoccidial agent(s). Methods for the treatment and prevention of mammalian protozoal diseases, such as, for example, toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, and opportunistic infections comprise administering the compound alone, or in combination with one or more antiprotozoal agent(s).
    Type: Application
    Filed: March 2, 2004
    Publication date: August 10, 2006
    Inventors: Matthew Wyvratt, Tesfaye Biftu, Michael Fisher, Dennis Schmatz
  • Publication number: 20040254167
    Abstract: The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compound and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Application
    Filed: July 9, 2004
    Publication date: December 16, 2004
    Inventors: Tesfaye Biftu, Gui-Bai Liang, Xiaoxia Qian, Ann E. Weber, Danqing Dennis Feng
  • Publication number: 20040176396
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof are useful in the treatment of cytokine mediated diseases such as arthritis and in the treatment and/or prevention of protozoal diseases such as coccidiosis.
    Type: Application
    Filed: November 12, 2003
    Publication date: September 9, 2004
    Inventors: Tesfaye Biftu, Richard Beresis, Richard Berger, Steven L Coletti, James B Doherty, Dennis D Feng, Gui-Bai Liang, Dennis M Schmatz, Xiaoxia Qian, David A Claremon, Nigel J Liverton, Charles J McIntyre, Ernest W Kovacs
  • Patent number: 6432980
    Abstract: Trisubstituted pyrroles are antiprotozoal agents useful in the treatment and prevention of protozoal diseases in human and animals, including the control of coccidiosis in poultry.
    Type: Grant
    Filed: November 10, 2000
    Date of Patent: August 13, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Tesfaye Biftu, Danqing D. Feng, Gui-Bai Liang, Mitree M. Ponpipom, Xiaoxia Qian, Narindar Girotra, Michael H. Fischer, Matthew J. Wyvratt
  • Patent number: 6420392
    Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. Also disclosed is a method to treat disorders mediated by PAF and/or leukotrienes that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier, to a patient in need of such therapy.
    Type: Grant
    Filed: October 9, 1996
    Date of Patent: July 16, 2002
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Tesfaye Biftu, Xiong Cai, Sajjat Hussoin, Gurmit Grewal, T Y Shen
  • Patent number: 6291480
    Abstract: Trisubstituted pyrroles are antiprotozoal agents useful in the treatment and prevention of protozoal diseases in human and animals, including the control of coccidiosis in poultry.
    Type: Grant
    Filed: November 10, 2000
    Date of Patent: September 18, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Tesfaye Biftu, Danqing Dennis Feng, Gui-Bai Liang, Mitree M. Ponpipom, Xiaoxia Qian, Michael H. Fisher, Matthew J. Wyvratt
  • Patent number: 6201016
    Abstract: Enantiomerically enriched disubstituted tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. It has been determined that 5-lipoxygenase activity, oral availability, and stability in vivo (for example, glucuronidation rate) can vary significantly among the optical isomers of the disclosed compounds.
    Type: Grant
    Filed: February 17, 1995
    Date of Patent: March 13, 2001
    Assignee: CytoMed Incorporated
    Inventors: Xiong Cai, Gurmit Grewal, Sajjat Hussoin, Aberra Fura, Ralph Scannell, Tesfaye Biftu
  • Patent number: 6177451
    Abstract: The present invention provides methods of treatment utilizing pharmaceutical compositions comprising an effective nicotine agonist amount of epibatidine (1) or a synthetic 7-azabicyclo[2.2.1]-heptane or heptene derivative thereof, and a pharmaceutically acceptable earner, excipient or diluent.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: January 23, 2001
    Assignee: UCB, S.A.
    Inventors: Changgeng Qian, Tongchuan Li, Tesfaye Biftu, Tsung-Ying Shen
  • Patent number: 6077846
    Abstract: This invention relates to the treatment of conditions that can be treated with a nicotinic agonist by administering to a patient an effective amount of a 7-azabicyclo[2.2.1]-heptane or heptene.
    Type: Grant
    Filed: December 17, 1996
    Date of Patent: June 20, 2000
    Assignee: UCB, S.A.
    Inventors: Changgeng Qian, Tongchuan Li, Tesfaye Biftu, Tsung-Ying Shen
  • Patent number: 6034106
    Abstract: Oxadiazole substituted benzenesulfonamides are selective .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.
    Type: Grant
    Filed: June 4, 1997
    Date of Patent: March 7, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Tesfaye Biftu, Michael H. Fisher, Danqing Dennis Feng, Chan-Hwa Kuo, Gui-Bai Liang, Elizabeth M. Naylor, Ann E. Weber
  • Patent number: 5792776
    Abstract: Disubstituted tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF and/or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: June 27, 1994
    Date of Patent: August 11, 1998
    Assignee: Cytomed, Inc.,
    Inventors: Tesfaye Biftu, Ralph Scannell, Xiong Cai, Sajjat Hussoin
  • Patent number: 5780503
    Abstract: Disubstituted tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF and/or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 14, 1998
    Assignee: Cytomed, Inc.
    Inventors: Tesfaye Biftu, Ralph Scannell, Xiong Cai, Sajjat Hussoin
  • Patent number: 5741809
    Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. Also disclosed is a method to treat disorders mediated by PAF and/or leukotrienes that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier, to a patient in need of such therapy.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: April 21, 1998
    Assignee: Cytomed, Inc.
    Inventors: Tesfaye Biftu, Xiong Cai, Sajjat Hussoin, Gurmit Grewal, T. Y. Shen
  • Patent number: 5681966
    Abstract: Enantiomerically enriched disubstituted tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.It has been determined that 5-lipoxygenase activity, oral availability, and stability in vivo (for example, glucuronidation rate) can vary significantly among the optical isomers of the disclosed compounds.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 28, 1997
    Assignee: Cytomed, Inc.
    Inventors: Xiong Cai, Gurmit Grewal, Sajjat Hussoin, Aberra Fura, Ralph Scannell, Tesfaye Biftu
  • Patent number: 5506262
    Abstract: Disclosed herein are compounds of structural formula (I) ##STR1## which are useful as cholesterol lowering agents. These compounds are also useful as inhibitors of squalene synthetase, inhibitors of fungal growth, inhibitors of farnesyl-protein transferase and farnesylation of the oncogene protein Ras. These compounds are also useful in the treatment of cancer.
    Type: Grant
    Filed: November 10, 1993
    Date of Patent: April 9, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Robert M. Burk, William H. Parsons, John J. Acton, III, Gregory D. Berger, Tesfaye Biftu, Robert L. Bugianesi, Yuan-Ching P. Chiang, Claude Dufresne, Narindar N. Girotra, Robert W. Marquis, Jr., Chan-Hwa Kuo, Sandra P. Plevyak, Mitree M. Ponpipom, Lori L. Whiting, James D. Bergstrom, Conrad Santini
  • Patent number: 5463083
    Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i,e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. Also disclosed is a method to treat disorders mediated by PAF and/or leukotrienes that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier, to a patient in need of such therapy.
    Type: Grant
    Filed: January 6, 1994
    Date of Patent: October 31, 1995
    Assignee: Cytomed, Inc.
    Inventors: Tesfaye Biftu, Xiong Cai, Sajjet Hussion, Gurmit Grewal, T. Y. Shen
  • Patent number: 5447717
    Abstract: This invention relates to compounds of structural formula (I): ##STR1## which are squalene synthase inhibitors and thus useful as cholesterol lowering agents and antifungal agents. These compounds are also inhibitors of farnesyl protein transferass and farnesylation of the oncogene protein Ras and thus useful in treating cancer.
    Type: Grant
    Filed: February 25, 1993
    Date of Patent: September 5, 1995
    Assignee: Merck & Co., Inc.
    Inventor: Tesfaye Biftu
  • Patent number: 5369125
    Abstract: This invention relates to compounds of structural formula (I): ##STR1## which are squalene synthase inhibitors and thus useful as cholesterol lowering agents and antifungal agents. These compounds are also inhibitors of farnesyl protein transferase and farnesylation of the oncogene protein Ras and thus useful in treating cancer.
    Type: Grant
    Filed: March 19, 1993
    Date of Patent: November 29, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Gregory D. Berger, James D. Bergstrom, Tesfaye Biftu, Robert L. Bugianesi, Robert M. Burk, Narindar N. Girotra, C. H. Kuo, William H. Parsons, Mitree M. Ponpipom, Lori L. Whiting