Patents Represented by Attorney, Agent or Law Firm Mark R. Daniel
  • Welding process
    Patent number: 6009691
    Abstract: A process of welding plastic vials and closure suitable for sterile filling operations is disclosed. Following a mechanical seal, a heated die is used to fuse the container and closure into a hermetic seal capable of use in the pharmaceutical industry.
    Type: Grant
    Filed: February 25, 1998
    Date of Patent: January 4, 2000
    Assignee: Merck & Co., Inc.
    Inventor: Arthur L. Lifshey
  • Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment
    Patent number: 6008212
    Abstract: Compounds of formula I: ##STR1## as well as pharmaceutically acceptable salts thereof are disclosed. R.sup.2 is H and R.sup.3 is C1-3 alkyl, or R.sup.2 and R.sup.3 taken in combination represent C.sub.1-3 alkylidene. Pharmaceutical compositions and methods of treatment are also included. The compounds are useful against methicillin resistant staphylococci (MRSA).
    Type: Grant
    Filed: October 8, 1998
    Date of Patent: December 28, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Ronald W. Ratcliffe, Timothy A. Blizzard
  • Antagonists of gonadotropin releasing hormone
    Patent number: 6004984
    Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
    Type: Grant
    Filed: May 22, 1998
    Date of Patent: December 21, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Mark Goulet, Feroze Ujjainwalla, Thomas F. Walsh, Matthew J. Wyvratt, Jr.
  • Inhibitors of farnesyl-protein transferase
    Patent number: 6001835
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: March 25, 1997
    Date of Patent: December 14, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Christopher J. Dinsmore, Theresa M. Williams
  • End-sampling thief probe
    Patent number: 5996426
    Abstract: This invention relates to an end-sampling thief probe and a method of using this probe. The thief probe of the invention is useful in extracting a sample with minimal disturbance and provides an improved method for end-sampling.
    Type: Grant
    Filed: October 6, 1997
    Date of Patent: December 7, 1999
    Assignees: Merck & Co., Inc., Rutgers, The State University of new Jersey
    Inventors: Priscilla A. Robinson, Dean Brone, Erinn K. Gleason, Fernando J. Muzzio, Carolyn Wightman
  • Triterpene derivatives with immunosuppressant activity
    Patent number: 5998408
    Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.
    Type: Grant
    Filed: October 8, 1997
    Date of Patent: December 7, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Robert K. Baker, Frank Kayser, Jianming Bao, Andrew Kotliar, William H. Parsons, Kathleen M. Rupprecht
  • Antibiotic synthesis
    Patent number: 5998612
    Abstract: A method of preparing intermediates for carbapenem antibiotics characterized by treating a N-deprotected acetoxy conpound of the formula: ##STR1## in the presence of a Lewis acid or a silylating agent to yeild an intermediate; and cyclizing the intermediate in the presence of rhodium (II) acetate to form a bicyclic ketoester.
    Type: Grant
    Filed: June 12, 1992
    Date of Patent: December 7, 1999
    Inventors: Paul J. Reider, Edward J. J. Grabowski
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5998407
    Abstract: The present invention is directed to substituted benozdiazepine compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: October 1, 1998
    Date of Patent: December 7, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Samuel L. Graham, John S. Wai, Neville J. Anthony
  • Antagonists of gonadotropin releasing hormone
    Patent number: 5998432
    Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
    Type: Grant
    Filed: March 25, 1999
    Date of Patent: December 7, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Thomas F. Walsh, Feroze Ujjainwalla, Mark T. Goulet
  • Asymmetric conjugate addition reaction using a chiral additive
    Patent number: 5998625
    Abstract: This invention relates to a process for the preparation of a key intermediate using an chiral additive to effect an asymmetric conjugate addition.
    Type: Grant
    Filed: January 5, 1998
    Date of Patent: December 7, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Richard D. Tillyer, David M. Tschaen, Feng Xu
  • Conjugates useful in the treatment of prostate cancer
    Patent number: 5998362
    Abstract: Chemical conjugates which comprise oligopeptides, having amino acid sequences that are selectively proteolytically cleaved by free prostate specific antigen (PSA), hydrophilic oligopeptide blocking groups and known cytotoxic agents are disclosed. Such conjugates are useful in the treatment of prostatic cancer and benign prostatic hypertrophy (BPH).
    Type: Grant
    Filed: September 9, 1997
    Date of Patent: December 7, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Dong-Mei Feng, Victor M. Garsky, Raymond E. Jones, Jenny M. Wai
  • Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment
    Patent number: 5994343
    Abstract: The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2-position with a naphthosultam linked through a --Z--CH.sub.2 group. The naphthosultam is further substituted with various substituent groups including cationic groups. The compounds are represented by formula I: ##STR1## Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: September 10, 1998
    Date of Patent: November 30, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. Dininno, Kevin D. Dykstra
  • Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment
    Patent number: 5994345
    Abstract: Carbapenems substituted with a naphthosultam at position 2 and linked through a CH.sub.2 group are disclosed. Pharmaceutical compositions and methods of treatment are also included. The naphthosultam is substituted with at least one cationic group --A--Q--L--B. ##STR1## A--Q--L--B represents a side chain wherein in part: A is a C.sub.1-6 alkylene group, straight or branched, and optionally interrupted or terminated by 1-2 of --O--, --S--, NR.sup.a --, --C(O)-- and CH.dbd.CH--Q is ##STR2## L represents a C.sub.1-8 alkylene group, straight or branched, and unsubstituted or substituted with 1-3 R.sup.c groups andB represents ##STR3## The carbapenems of the present invention are useful against gram positive microorganisms, especially methicillin resistant Staphylococci.
    Type: Grant
    Filed: October 8, 1998
    Date of Patent: November 30, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Lovji D. Cama, Robert R. Wilkening, Ronald W. Ratcliffe, Kenneth J. Wildonger, Wanying Sun
  • Bis-aryl ethers, compositions containing such compounds and methods of treatment
    Patent number: 5994412
    Abstract: A compound represented by the formula I is disclosed: ##STR1## or a pharmaceutically acceptable salt or hydrate thereof. The compound has inhibitory activity against the oncoprotein Raf.Also included are pharmaceutical compositions, methods of treating cancer, cultures of the producing fungal microorganism and methods of fermentative production of the compound.
    Type: Grant
    Filed: July 2, 1998
    Date of Patent: November 30, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Seok H. Lee, Maria T. Diez, Fernando Pelaez, Marina Mojena Sanchez, M. Dolores Vilella Amils, Hans E. Huber, Denis R. Patrick, Otto D. Hensens, Rosalind G. Jenkins, Leeyuan Huang, Annie Z. Zhao, Deborah L. Zink, Anne Dombrowski, Gerald F. Bills
  • Antagonists of gonadotropin releasing hormone
    Patent number: 5985892
    Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
    Type: Grant
    Filed: March 25, 1999
    Date of Patent: November 16, 1999
    Assignee: Merck & Co., Ltd.
    Inventors: Thomas F. Walsh, Mark T. Goulet, Feroze Ujjainwalla, Robert L. Bugianesi
  • Antagonists of gonadotropin releasing hormone
    Patent number: 5985901
    Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
    Type: Grant
    Filed: May 22, 1998
    Date of Patent: November 16, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Mark Goulet, Feroze Ujjainwalla, Thomas F. Walsh, Matthew J. Wyvratt, Jr., Jonathan R. Young, Lin Chu
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5981562
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: January 21, 1997
    Date of Patent: November 9, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Christopher J. Dinsmore, George D. Hartman
  • Antagonists of gonadotropin releasing hormone
    Patent number: 5981550
    Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
    Type: Grant
    Filed: May 22, 1998
    Date of Patent: November 9, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Mark Goulet, Thomas F. Walsh, Feroze Ujjainwalla, Matthew J. Wyvratt, Jr., Jonathan R. Young, Lin Chu
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5977134
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: December 4, 1997
    Date of Patent: November 2, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Terrence M. Ciccarone, Wasyl Halczenko, John H. Hutchinson, William C. Lumma, Jr., Gerald E. Stokker, Craig A. Stump, Theresa M. Williams
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5972984
    Abstract: The present invention comprises low molecular weight peptidyl compounds that inhibit the farnesyl-protein transferase. Furthermore, these compounds differ from the mono- or dipeptidyl analogs previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.
    Type: Grant
    Filed: October 29, 1997
    Date of Patent: October 26, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Jeffrey M. Bergman, S. Jane deSolms, Chrisopher J. Dinsmore, Robert P. Gomez, Suzanne C. MacTough, Kelly M. Solinsky, Theresa M. Williams