Patents Represented by Attorney, Agent or Law Firm Melvin Winokur
  • Intramolecular glycosidation process for the synthesis of (2R, 2-alpha-R, 3a)-2-[1-(3,5- bis (trifluoromethyl) phenyl)ethoxy]-3-(4-fluorophenyl)-1,4-oxazine
    Patent number: 6403793
    Abstract: The present invention is concerned with novel processes for the preparation of (2R-cis)-2-[[1-[3.5-bis(trifluoromethyl)phenyl]ethenyl]oxy]-3-(4-fluorophenyl)-4-(phenylmethyl) mopholine. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
    Type: Grant
    Filed: June 8, 2001
    Date of Patent: June 11, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Philip J. Pye, Kai Rossen
  • Combination therapy for reducing the risks associated with cardiovascular disease
    Patent number: 6403571
    Abstract: The instant invention involves a combination therapy and pharmaceutical compositions comprised of a therapeutically effective amount of a cholesterol reducing agent such as an HMG-CoA reductase inhibitor in combination with a platelet aggregation inhibitor which is useful for inhibiting platelet aggregation, for inhibiting the formation of thrombotic occlusions, and for treating, preventing and reducing the risk of occurrence of cardiovascular and cerebrovascular events and related vaso-occlusive disorders.
    Type: Grant
    Filed: January 18, 2001
    Date of Patent: June 11, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Robert J. Gould, Steven A. Nichtberger, Patricia A. Rhymer, Lars Olofsson
  • HIV integrase inhibitors
    Patent number: 6403347
    Abstract: Natural products such as certain chaetochromins are described. These compounds are useful in the inhibition of HIV integrase, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: October 25, 1999
    Date of Patent: June 11, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Gerald F. Bills, Russell B. Lingham, Ali Shafiee, Keith C. Silverman, Sheo Bux Singh, Deborah L. Zink, Fernando Pelaez, Ana M. Teran
  • Pyrrolidine modulators of chemokine receptor activity
    Patent number: 6399619
    Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6 and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.
    Type: Grant
    Filed: April 4, 2000
    Date of Patent: June 4, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Scott Berk, Charles G. Caldwell, Kevin T. Chapman, Jeffrey Hale, Christopher Lynch, Malcolm MacCoss, Sander G. Mills, Christopher Willoughby
  • Combination of a GABA-A &agr; 2/3 agonist and a selective serotonin reuptake inhibitor
    Patent number: 6399608
    Abstract: A pharmaceutical product comprising an SSRI and a non-sedating anxiolytic compound, which is a modulator of the benzodiazepine binding site of the human GABAA receptor, having a binding affinity for the &agr;3 subunit of the human GABAA receptor of 10 nM or less, which elicits at least a 40% potentiation of the GABA EC20 response in stably transfected recombinant cell lines expressing the &agr;3 subunit of &agr;3 and which elicits at most a 30% potentiation of the GABA EC20 response in stably transfected cell lines expressing the &agr;1 subunit of the human GABAA receptor is disclosed for simultaneous, separate or sequential administration.
    Type: Grant
    Filed: July 20, 2000
    Date of Patent: June 4, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventor: Gerard Raphael Dawson
  • Trans-glycosidation process for the synthesis of (2R, 2-alpha-R, 3a)-2-[1-(3,5-bis(trifluoromethyl)phenyl)ethoxy]-3-(4-fluorophenyl)-1,4-oxazine
    Patent number: 6395898
    Abstract: The present invention is concerned with novel processes for the preparation of (2R, 2-alpha-R, 3a)-2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy-3-(4-fluorophenyl)-1,4-oxazine. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
    Type: Grant
    Filed: June 8, 2001
    Date of Patent: May 28, 2002
    Assignee: Merck & Co. Inc.
    Inventors: James M. McNamara, Matthew M. Zhao
  • Tetrahydroindazole derivatives as ligands for GABA-A &agr; 5 receptors
    Patent number: 6395905
    Abstract: 4-oxo-tetrahydroindozole-3-carboxamide compounds according to Formula (I), or a pharmaceutically acceptable salt thereof, are GABA-A Alpha 5 ligands useful for enhancing cognition:
    Type: Grant
    Filed: June 15, 2001
    Date of Patent: May 28, 2002
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Helen Jane Bryant, Mark Stuart Chambers
  • HIV integrase inhibitors
    Patent number: 6395743
    Abstract: Compounds useful in the inhibition of HIV integrase, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines are described. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. The culture Actinoplanes sp. MA7220 (ATCC 202188) is also disclosed, as well as processes for making compounds of the present invention employing the culture.
    Type: Grant
    Filed: October 12, 2000
    Date of Patent: May 28, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Brian Heimbuch, Sheo Singh, Deborah L. Zink, Magda Gagliardi, Olga Genilloud, Ana Teran
  • Process for the synthesis of (2S)-phenyl-3-piperidone
    Patent number: 6388083
    Abstract: The present invention is concerned with novel processes for the preparation of (2S)-phenyl-3-piperidone. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
    Type: Grant
    Filed: July 5, 2001
    Date of Patent: May 14, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Jaemoon Lee, David Askin, Thoa Hoang
  • Pyrazinone thrombin inhibitors
    Patent number: 6387911
    Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein A is
    Type: Grant
    Filed: November 21, 2000
    Date of Patent: May 14, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Christopher Burgey, Richard C. Isaacs, Bruce D. Dorsey, Kyle A. Robinson, Donnette Staas, Philip E. Sanderson, James Barrow
  • HIV integrase inhibitors
    Patent number: 6380249
    Abstract: Certain six-membered aromatic and heteroaromatic-dioxobutyric acid derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: June 1, 1999
    Date of Patent: April 30, 2002
    Assignees: Merck & Co., Inc., Tularik Inc.
    Inventors: Steven D. Young, Melissa Egbertson, Linda S. Payne, John S. Wai, Thorsten E. Fisher, James P. Guare, Jr., Mark W. Embrey, Lekhanh Tran, Linghang Zhuang, Joseph P. Vacca, H. Marie Langford, Jeffrey Melamed, Juan C. Jaen, David L. Clark, Julio C. Medina
  • Lactonization process
    Patent number: 6380401
    Abstract: Crystalline 3-hydroxylactone-containing products can be prepared in high yield and purity in a one-pot process by treating the corresponding 3,5-dihydroxy acid with a strong mineral acid in a cold, aprotic, water-miscible solvent to effect lactonization, followed by addition of excess acid to effect crystallization of the lactonized product from the reaction mixture.
    Type: Grant
    Filed: October 23, 2000
    Date of Patent: April 30, 2002
    Assignee: Merck & Co., Inc.
    Inventors: James McManus, Nicholas Anousis, John Genus, Christopher Hancock
  • Recovery of iodide from chemical process wastewater
    Patent number: 6379556
    Abstract: The recovery of iodide from chemical process wastewater is accomplished by loading the wastewater containing iodide onto a strongly basic anion-exchange resin in free-base form; eluting the sorbed iodide from the resin with aqueous strong acid (e.g., hydrochloric acid); loading the iodide-rich cuts onto a weakly basic anion-exchange resin in free-base form; and eluting the sorbed iodide with aqueous base (e.g., sodium hydroxide). The recovered iodide typically has sufficient purity to permit its re-use in the chemical process.
    Type: Grant
    Filed: September 13, 1999
    Date of Patent: April 30, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Ed Venkat, Ralph J. Magliette, Donald McKinney, Alan S. Michaels
  • Combination of an agent that binds to the androgen receptor and a bisphosphonic acid in the prevention and/or treatment of diseases involving calcium or phosphate metabolism
    Patent number: 6376477
    Abstract: The inhibition of natural bone formation experienced in the prophylaxis and/or treatment of bone resorption disease with a bisphosphonic acid or a pharmaceutically acceptable salt thereof is overcome by the concommitant administration of an agent that binds to the androgen receptor.
    Type: Grant
    Filed: December 19, 2000
    Date of Patent: April 23, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Azriel Schmidt, Shun-Ichi Harada, Gideon Rodan
  • Melanocortin receptor agonists
    Patent number: 6376509
    Abstract: Certain novel compounds and derivatives thereof are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
    Type: Grant
    Filed: May 29, 2001
    Date of Patent: April 23, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Raman Kumar Bakshi, Ravi P. Nargund, Zhixiong Ye
  • Alpha 1a adrenergic receptor antagonists
    Patent number: 6376503
    Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
    Type: Grant
    Filed: June 17, 1998
    Date of Patent: April 23, 2002
    Assignees: Merck & Co., Inc, Synaptic Pharmaceutical Corporation
    Inventors: Michael A. Patane, Mark G. Bock, Randall C. Newton, Bharat Lagu
  • Process for oxidation of steroidal compounds having allylic groups
    Patent number: 6369247
    Abstract: The instant invention involves a process for oxidizing compounds containing an allylic group, i.e. those containing an allylic hydrogen or allylic alcohol group, to the corresponding enones, using a ruthenium-based catalyst in the presence of a hydroperoxide. Particularly, &Dgr;-5-steroidal alkenes can be oxidized to the corresponding &Dgr;-5-7-keto alkenes.
    Type: Grant
    Filed: September 30, 1996
    Date of Patent: April 9, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Ross A. Miller, Andrew S. Thompson, Raman K. Bakshi, Edward G. Corley
  • Method for treating inflammatory diseases by administering a thrombin inhibitor
    Patent number: 6362190
    Abstract: The invention is a method for treating an inflammatory disease in a patient which comprises treating the patient with an oral composition comprising a thrombin inhibitor. Such diseases include but are not limited to nephritis, systemic lupus erythematosus, rheumatoid arthritis, glomerulonephritis and sarcoidosis.
    Type: Grant
    Filed: May 10, 2001
    Date of Patent: March 26, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Jules Shafer, Denise M. Visco
  • Integrin receptor antagonists
    Patent number: 6358970
    Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.
    Type: Grant
    Filed: June 21, 2000
    Date of Patent: March 19, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, George D. Hartman, James J. Perkins, Nathan Ihle
  • Pharmaceutical kit
    Patent number: D457246
    Type: Grant
    Filed: December 20, 1999
    Date of Patent: May 14, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Sidney Mazel, James M. Mundt