Patents by Inventor Ulf H. Dolling

Ulf H. Dolling 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).

  • HIV integrase inhibitors
    Patent number: 7598264
    Abstract: Hydroxy (tetra- or hexa-)hydronaphthyridine dione compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I) wherein a, R1?, R2?, R3?, R4? and R5? are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: March 9, 2005
    Date of Patent: October 6, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Wei Han, Melissa Egbertson, John S. Wai, Linghang Zhuang, Rowena D. Ruzek, Debra S. Perlow, Mark Cameron, Bruce S. Foster, Ulf H. Dolling, R. Scott Hoerrner, Philip J. Pye, Remy Angelaud, Danny E. Mancheno, David Askin
  • Stereoselective synthesis of a 4,4-disubstituted cyclohexanepropanoic acid
    Patent number: 7411088
    Abstract: There is provided stereoselective route to a compound of formula I: wherein R represents H or an alkali metal, Ar1 represents 4-chlorophenyl and Ar2 represents 2,5-difluorophenyl.
    Type: Grant
    Filed: February 16, 2005
    Date of Patent: August 12, 2008
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme Ltd.
    Inventors: Karel Marie Joseph Brands, Sarah Elizabeth Brewer, Antony John Davies, Ulf H. Dolling, Deborah Camille Hammond, David Ross Lieberman, Jeremy Peter Scott
  • Process for making a thrombin inhibitor
    Publication number: 20020103379
    Abstract: The invention is a process for preparing 3-fluoro-2-pyridylmethyl-3-(2,2-difluoro-2-(2-pyridyl)ethylamino)-6-chloropyrazin-2-one-1-acetamide which comprises coupling 1
    Type: Application
    Filed: December 6, 2001
    Publication date: August 1, 2002
    Inventors: Ulf H. Dolling, Ramon Alabaster, Michael S. Ashwood, Ian F. Cottrell, Cameron J. Cowden, Antony J. Davies, David Hands, Debra J. Wallace, Robert D. Wilson
  • Chemical synthesis of 1,2,4-triazolinone derivative
    Patent number: 6407255
    Abstract: The present invention relates to a process for the preparation of morpholine derivatives of formula (I) which are useful as a therapeutic agents.
    Type: Grant
    Filed: September 10, 2001
    Date of Patent: June 18, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Ian Frank Cottrell, Ulf H Dolling, David Hands, Robert Darrin Wilson
  • Chemical synthesis of morpholine derivatives
    Publication number: 20020019524
    Abstract: 1
    Type: Application
    Filed: September 10, 2001
    Publication date: February 14, 2002
    Applicant: Merck Sharp & Dohme Limited
    Inventors: Ian Frank Cottrell, Ulf H. Dolling, David Hands, Robert Darrin Wilson
  • Chemical synthesis of morpholine derivatives
    Patent number: 6297376
    Abstract: The present invention relates to a process for the preparation of mopholine derivatives of formula (I) which are useful as a therapeutic agents.
    Type: Grant
    Filed: December 15, 2000
    Date of Patent: October 2, 2001
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Ian Frank Cottrell, Ulf H Dolling, David Hands, Robert Darrin Wilson
  • Stabilized carbapenem intermediates and improved process for carbapenem synthesis
    Patent number: 6180783
    Abstract: A stabilized carbapenem intermediate compound represented by the formula 1: or a salt thereof is disclosed, wherein P represents a carboxyl protecting group and X represents a charge balancing group. In addition, a process for synthesizing a compound represented by formula 2: is disclosed wherein X+ is a charge balancing group, comprising: deprotecting a compound of the formula 1 to produce a compound 2.
    Type: Grant
    Filed: June 9, 1998
    Date of Patent: January 30, 2001
    Assignee: Merck & Co., Inc.
    Inventors: John M. Williams, Renato T. Skerlj, Karel M. J. Brands, Ulf H. Dolling, Ronald B. Jobson
  • Asymmetric conjugate addition reaction
    Patent number: 6172235
    Abstract: This invention relates to a key intermediate in the synthesis of an endothelin antagonist and the synthesis of this key intermediate using an asymmetric conjugate addition reaction.
    Type: Grant
    Filed: April 27, 1999
    Date of Patent: January 9, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Ulf H. Dolling, Lisa F. Frey, Richard D. Tillyer, David M. Tschaen
  • Process for synthesizing carbapenem side chain intermediates
    Patent number: 6063931
    Abstract: A process of synthesizing a compound of the formula 1: ##STR1## is described. A compound of the formula 2: ##STR2## is reacted with diphenylphosphinic chloride to activate the carboxylic acid group, and then reacted with methanesulfonyl chloride to produce a compound of formula 4: ##STR3## Compound 4 is then reacted with a group II metal sulfide source in water to produce a compound of formula 1.
    Type: Grant
    Filed: June 29, 1998
    Date of Patent: May 16, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Karel M. J. Brands, John M. Williams, Ulf H. Dolling, Ronald B. Jobson, Antony J. Davies, Ian F. Cottrell, Mark Cameron, Michael S. Ashwood
  • Process for synthesizing carbapenem side chain intermediates
    Patent number: 6060607
    Abstract: A process of synthesizing a compound of the formula 1: ##STR1## is described. A compound of the formula 2: ##STR2## is reacted with diphenylphosphinic chloride to activate the carboxylic acid group, and then reacted with methanesulfonyl chloride to produce a compound of formula 4: ##STR3## Compound 4 is then reacted with a group II metal sulfide source in water to produce a compound of formula 1.
    Type: Grant
    Filed: June 16, 1999
    Date of Patent: May 9, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Karel M. J. Brands, John M. Williams, Ulf H. Dolling, Ronald B. Jobson, Antony J. Davies, Ian F. Cottrell, Mark Cameron, Michael S. Ashwood
  • Stereoselective deoxygenation reaction
    Patent number: 5962688
    Abstract: This invention relates to a key intermediate in the synthesis of an endothelin antagonist, the synthesis of this key intermediate and the synthesis of an endothelin antagonist using this intermediate in a stereoselective deoxygenation reaction.
    Type: Grant
    Filed: August 8, 1997
    Date of Patent: October 5, 1999
    Assignees: Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd.
    Inventors: Paul N. Devine, Ulf H. Dolling, Lisa F. Frey, Richard D. Tillyer, David M. Tschaen, Yoshiaki Kato
  • Finasteride processes
    Patent number: 5886184
    Abstract: Disclosed is a new process for producing finasteride which involves reacting the magnesium halide salt of 17.beta.-carboalkoxy-4-aza-5.alpha.-androst-1-en-3-one with t-butylamino magnesium halide, present in at least a 2:1 molar ratio to the ester, formed from t-butyl amine and an aliphatic/aryl magnesium halide at ambient temperature in an inert organic solvent under an inert atmosphere followed by heating and recovering the product finasteride.Also disclosed are two polymorphic crystalline Forms I and II of finasteride, and methods of their production.
    Type: Grant
    Filed: March 26, 1997
    Date of Patent: March 23, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Ulf H. Dolling, James A. McCauley, Richard J. Varsolona
  • Compounds formed by an asymmetric conjugate addition reaction
    Patent number: 5849914
    Abstract: This invention relates to a key intermediate in the synthesis of an endothelin antagonist and the synthesis of this key intermediate using an asymmetric conjugate addition reaction.
    Type: Grant
    Filed: August 4, 1997
    Date of Patent: December 15, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Ulf H. Dolling, Lisa F. Frey, Richard D. Tillyer, David M. Tschaen
  • Process of preparing phenyl heterocycles useful as COX-2 inhibitors
    Patent number: 5840924
    Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of inflammation and other cyclooxygenase-2 mediated diseases.
    Type: Grant
    Filed: June 16, 1997
    Date of Patent: November 24, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Richard Desmond, Ulf H. Dolling, Lisa F. Frey, Richard D. Tillyer, David M. Tschaen
  • Process for making dihydropyrimidinones
    Patent number: 5786472
    Abstract: The present invention provides a process for forming 5-(alkyl or alkoxy)carbonyl-6-alkyl-4-(aryl or alkyl)-3,4-2(1H)-dihydropyrimidinones by combining a .beta.-keto ester or diketone, an aldehyde and urea in the presence of a boron reagent, a metal salt (e.g., Cu.sub.2 O) and a catalyst (e.g., acid). The reaction is typically run in one pot in a solvent to afford dihydropyrimidinones in higher yields and with easier work up than previously known methods.
    Type: Grant
    Filed: December 12, 1996
    Date of Patent: July 28, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Essa Hsinyi Hu, Daniel R. Sidler, Ulf H. Dolling, Michael A. Patane
  • Synthesis of .alpha.-chloro or fluoro ketones
    Patent number: 5786515
    Abstract: A simple, high yielding synthesis of a-chloro ketones is described, involving acylation of Grignard and organolithium reagents with N-methoxy-N-methylchloroacetamide. The efficiency of the process is further enhanced by recycling N,O-dimethylhydroxylamine.
    Type: Grant
    Filed: August 30, 1996
    Date of Patent: July 28, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Ulf H. Dolling, Lisa F. Frey, Richard D. Tillyer, David M. Tschaen
  • New finasteride processes
    Patent number: 5468860
    Abstract: Disclosed is a new process for producing finasteride which involves reacting the magnesium halide salt of 17.beta.B-carboalkoxy-4-aza-5.alpha.-androst-1-en-3-one with t-butylamino magnesium halide, present in at least a 2:1 molar ratio to the ester, formed from t-butyl amine and an aliphatic/aryl magnesium halide at ambient temperature in an inert organic solvent under an inert atmosphere followed by heating and recovering said product finasteride.Also disclosed are two polymorphic crystalline Forms I and II of finasteride, and methods of their production.
    Type: Grant
    Filed: January 29, 1993
    Date of Patent: November 21, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Ulf H. Dolling, James A. McCauley, Richard J. Varsolona
  • Preparation of 2-aryl carbapenems via a boronic acid coupling reaction
    Patent number: 5442057
    Abstract: The present invention is directed to a process of making 2-Aryl Carbapenems of Formula 1 from a compound of formula 2.
    Type: Grant
    Filed: April 12, 1994
    Date of Patent: August 15, 1995
    Inventors: Ann Decamp, Ulf H. Dolling, Yulan Li, Dale L. Rieger, Nobuyoshi Yasuda, Lyndon C. Xavier
  • Boron containing intermediates useful in the preparation of carbapenems
    Patent number: 5338875
    Abstract: The present invention is directed to intermediates of the following formula which are useful in the preparation of Carbapenem-antibiotics ##STR1##
    Type: Grant
    Filed: November 19, 1992
    Date of Patent: August 16, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Ann DeCamp, Ulf H. Dolling, Yulan Li, Dale L. Rieger, Nobuyoshi Yasuda, Lyndon C. Xavier
  • Methods of synthesizing benign prostatic hypertropic agents and their intermediates
    Patent number: 5237061
    Abstract: A process for preparing compounds of the formula ##STR1## which comprises reacting an imidazolide of the formula ##STR2## with an amine of the formula NHR.sub.4 R.sub.5 in the presence of a Grignard reagent to form a compound of formula I or reacting an imidazolide of formula II with a compound of the formula R.sub.6 Mgx to form a compound of formula I.
    Type: Grant
    Filed: October 31, 1988
    Date of Patent: August 17, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Apurba Bhattacharya, Ulf H. Dolling, Joseph S. Amato, John M. Williams