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).

  • NOVEL BENZIMIDAZOLE TETRAHYDROFURAN DERIVATIVES
    Publication number: 20150218149
    Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
    Type: Application
    Filed: August 15, 2013
    Publication date: August 6, 2015
    Inventors: James M. Apgar, Tesfaye Biftu, Ping Chen, Danqing Feng, Jacqueline D. Hicks, Ahmet Kekec, Kenneth J. Leavitt, Bing Li, Iyassu Sebhat, Xiaoxia Qian, Lan Wei, Robert R. Wilkening, Zhicai Wu
  • NOVEL BENZIMIDAZOLE HEXAHYDROFURO[3,2-B]FURAN DERIVATIVES
    Publication number: 20150218183
    Abstract: The novel benzimidazole hexahydrofuro[3,2-B]furan derivatives of the present invention are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
    Type: Application
    Filed: August 16, 2013
    Publication date: August 6, 2015
    Inventors: James M. Apgar, Ashok Arasappan, Tesfaye Biftu, Ping Chen, Danqing Feng, Erin Guidry, Jacqueline Hicks, Ahmet Kekec, Kenneth J. Leavitt, Bing Li, Iyassu Sebhat, Xiaoxia Qian, Lan Wei, Robert R. Wilkening, Zhicai Wu
  • NOVEL AZABENZIMIDAZOLE TETRAHYDROPYRAN DERIVATIVES
    Publication number: 20150210685
    Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPKactivated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
    Type: Application
    Filed: August 16, 2013
    Publication date: July 30, 2015
    Inventors: James M. Apgar, Tesfaye Biftu, Ping Chen, Danqing Feng, Jacqueline D. Hicks, Ahmet Kekec, Kenneth J. Leavitt, Bing Li, Iyassu Sebhat, Xiaoxia Qian, Lan Wei, Robert R. Wilkening, Zhicai Wu
  • NOVEL AZABENZIMIDAZOLE TETRAHYDROFURAN DERIVATIVES
    Publication number: 20150203487
    Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
    Type: Application
    Filed: August 19, 2013
    Publication date: July 23, 2015
    Inventors: James M. Apgar, Tesfaye Biftu, Ping Chen, Danqing Feng, Jacqueline D. Hicks, Ahmet Kekec, Kenneth J. Leavitt, Bing Li, Iyassu Sebhat, Xiaoxia Qian, Lan Wei, Robert R. Wilkening, Zhicai Wu, Ashok Arasappan
  • ALIPHATIC SPIROLACTAM CGRP RECEPTOR ANTAGONISTS
    Publication number: 20150203496
    Abstract: The present invention is directed to aliphatic spirolactam derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. 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 CGRP is involved.
    Type: Application
    Filed: May 3, 2013
    Publication date: July 23, 2015
    Inventors: Ian M. Bell, Mark Fraley, Tesfaye Biftu, Cheng Zhu, Anilkumar Nair, Helen Mitchell
  • NOVEL BENZIMIDAZOLE TETRAHYDROPYRAN DERIVATIVES
    Publication number: 20150197516
    Abstract: Novel compounds described herein are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPKactivated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
    Type: Application
    Filed: August 15, 2013
    Publication date: July 16, 2015
    Inventors: James M. Apgar, Tesfaye Biftu, Ping Chen, Danqing Feng, Jacqueline D. Hicks, Ahmet Kekec, Kenneth J. Leavitt, Bing Li, Iyassu Sebhat, Xiaoxia Qian, Lan Wei, Robert R. Wilkening, Zhicai Wu
  • Dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
    Patent number: 9073930
    Abstract: The present invention is directed to novel substituted dihydropyrrolopyrazoles of structural Formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme 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: February 12, 2013
    Date of Patent: July 7, 2015
    Assignee: Merck Sharp & Dohme
    Inventors: Ann E. Weber, Tesfaye Biftu
  • TREATING DIABETES WITH DIPEPTIDYL PEPTIDASE-IV INHIBITORS
    Publication number: 20150175609
    Abstract: The present invention is directed to novel substituted dihydropyrrolopyrazoles of structural Formula I which are inhibitors of the dipeptidyl peptidase-N enzyme 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 18, 2013
    Publication date: June 25, 2015
    Inventors: Tesfaye Biftu, Tanweer A. Khan
  • AMINOTETRAHYDROPYRANS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OF DIABETES
    Publication number: 20150126443
    Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme 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: January 7, 2015
    Publication date: May 7, 2015
    Inventors: Tesfaye Biftu, Ann E. Weber
  • SPIROLACTAM CGRP RECEPTOR ANTAGONISTS
    Publication number: 20150111914
    Abstract: The present invention is directed to spirolactam analogues which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. 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 CGRP is involved.
    Type: Application
    Filed: May 3, 2013
    Publication date: April 23, 2015
    Inventors: Ian M. Bell, Mark Fraley, Tesfaye Biftu, Cheng Zhu, Anilkumar Nair
  • PYRIDINE CGRP RECEPTOR ANTAGONISTS
    Publication number: 20150099771
    Abstract: The present invention is directed to pyridine derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. 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 CGRP is involved.
    Type: Application
    Filed: May 3, 2013
    Publication date: April 9, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Mark Fraley, Tesfaye Biftu, Cheng Zhu, Anilkumar Nair
  • NOVEL CRYSTALLINE FORMS OF A DIPEPTIDYL PEPTIDASE-IV INHIBITORS
    Publication number: 20150099891
    Abstract: Novel crystalline forms of (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine are potent inhibitors of dipeptidyl peptidase-IV and are useful for the treatment of non-insulin dependent (Type 2) diabetes mellitus. The invention also relates to pharmaceutical compositions containing these novel forms, processes to prepare these forms and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes.
    Type: Application
    Filed: October 6, 2014
    Publication date: April 9, 2015
    Inventors: Itzia Z. Arroyo, Davida Krueger, Ping Chen, Aaron J. Moment, Tesfaye Biftu, Faye Sheen, Yanfeng Zhang
  • HETEROCYCLIC CGRP RECEPTOR ANTAGONISTS
    Publication number: 20150087641
    Abstract: The present invention is directed to heterocyclic compounds which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. 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 CGRP is involved.
    Type: Application
    Filed: May 3, 2013
    Publication date: March 26, 2015
    Inventors: Ian M. Bell, Mark Fraley, Tesfaye Biftu, Cheng Zhu, Anilkumar Nair
  • Substituted seven-membered heterocyclic compounds as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes
    Patent number: 8980929
    Abstract: The present invention is directed to novel amino-substituted seven-membered heterocyclic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme 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: May 16, 2011
    Date of Patent: March 17, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jacqueline D. Hicks, Tesfaye Biftu, Ping Chen, Xiaoxia Qian, Robert R. Wilkening
  • Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
    Patent number: 8951965
    Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme 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: June 2, 2014
    Date of Patent: February 10, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tesfaye Biftu, Ann E. Weber
  • THROMBIN INHIBITORS
    Publication number: 20150038498
    Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: (I) or a pharmaceutically acceptable salt thereof, wherein Q is CH2, NR4, O, S, S(O) or S(O2), wherein R4 is H, C1-6 alkyl, aryl, or C3-8 cycloalkyl; R1 is a heterocycle or —(CR5R6)1-2NH2, wherein R5 and R6, each time in which they occur, are independently H, C1-6 alkyl, —CH2F, —CHF2, CF3 or —CH2OH; R2 is OH, NH2 or NHSO2CH3; and R3 is C1-6 alkyl.
    Type: Application
    Filed: March 22, 2013
    Publication date: February 5, 2015
    Inventors: Timothy Allen Blizzard, Tesfaye Biftu
  • PREPARATION AND USE OF BICYCLIC HIMBACINE DERIVATIVES AS PAR-1 RECEPTOR ANTAGONISTS
    Publication number: 20150025046
    Abstract: The present invention relates to bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: X is —O—, —N(R), —C(R8)(R9) or —C(O)—; and Y is —O—, —N(R), —C(R8)(R9) or —C(O)— and the remaining variables are described herein. The compounds of the invention are effective inhibitors of the PAR-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ACS, secondary prevention of myocardial infarction or stroke, or PAD.
    Type: Application
    Filed: February 27, 2013
    Publication date: January 22, 2015
    Inventors: Mihir Mandal, Timothy A. Blizzard, Helen Chen, Harry Chobanian, Yan Guo, Barbara Pio, Zhicai Wu, Tesfaye Biftu, William J. Greenlee, Johnny Zhaoning Zhu
  • DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
    Publication number: 20150011590
    Abstract: The present invention is directed to novel substituted dihydropyrrolopyrazoles of structural Formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme 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: February 12, 2013
    Publication date: January 8, 2015
    Applicant: Merck Sharp & Dohme Corporation
    Inventors: Ann E. Weber, Tesfaye Biftu
  • Crystalline forms of a dipeptidyl peptidase-IV inhibitor
    Patent number: 8895603
    Abstract: Novel crystalline forms of (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine are potent inhibitors of dipeptidyl peptidase-IV and are useful for the treatment of non-insulin dependent (Type 2) diabetes mellitus. The invention also relates to pharmaceutical compositions containing these novel forms, processes to prepare these forms and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes.
    Type: Grant
    Filed: June 25, 2012
    Date of Patent: November 25, 2014
    Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Ltd.
    Inventors: Itzia Arroyo, Davida Krueger, Ping Chen, Aaron Moment, Tesfaye Biftu, Faye Sheen, Yanfeng Zhang
  • Substituted aminotetrahydrothiopyrans and derivatives thereof as dipeptidyl peptidase-IV inhibitors for the treatment of diabetes
    Patent number: 8853212
    Abstract: The present invention is directed to novel substituted aminotetrahydrothiopyrans and derivatives thereof of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme 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: February 17, 2011
    Date of Patent: October 7, 2014
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Robert R. Wilkening, James M. Apgar, Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Lan Wei