Abstract: The present invention addresses 2, 5-substituted aryl pyrroles of the formula: ##STR1## or a pharmaceutically acceptable salts thereof, as well as compositions containing such compounds and methods of treatment. The compounds are useful for treating Cytokine mediated diseases, which refers to diseases or conditions in which excessive or unregulated production or activity of one or more cytokines occurs. Interleukin-1 (IL-1), Interleukin-6 (IL-6), Interleukin-8 (IL-8) and Tumor Necrosis Factor (TNF) are cytokines which are involved in immunoregulation and other physiological conditions, such as inflammation. The compounds also have glucagon antagonist activity.
Type:
Grant
Filed:
August 8, 1996
Date of Patent:
November 17, 1998
Assignee:
Merck & Co., Inc.
Inventors:
Stephen E. de Laszlo, Nigel J. Liverton, Gerald S. Ponticello, Harold G. Selnick, Nathan B. Mantlo
Abstract: There is disclosed a novel compound having the formula ##STR1## which exhibits antifungal activity.
Type:
Grant
Filed:
July 11, 1997
Date of Patent:
September 1, 1998
Assignee:
Merck & Co., Inc.
Inventors:
Wendy H. Clapp-Shapiro, Bruce W. Burgess, Robert A. Giacobbe, Guy H. Harris, Suzanne Mandala, Jon Polishook, Mark Rattray, Rosemary A. Thornton, Deborah L. Zink, Angeles Cabello, Maria Teresa Diez, Isabel Martin, Fernando Pelaez
Abstract: The present invention addresses 2-substituted aryl pyrroles, as well as compositions containing such compounds and methods of treatment. Cytokine mediated diseases refers to diseases or conditions in which excessive or unregulated production or activity of one or more cytokines occurs. Interleukin-1 (IL-1), Interleukin-6 (IL-6), Interleukin-8 (IL-8) and Tumor Necrosis Factor (TNF) are cytokines which are involved.
Type:
Grant
Filed:
August 8, 1996
Date of Patent:
August 11, 1998
Assignee:
Merck & Co., Inc.
Inventors:
Stephen E. de Laszlo, Nigel J. Liverton, Gerald S. Ponticello, Harold G. Selnick, Nathan B. Mantlo
Abstract: Ceretain aza cyclohexapeptide compounds have been found to have superior antibiotic properties. Novel processes for their preparation are also described.
Type:
Grant
Filed:
October 28, 1996
Date of Patent:
August 11, 1998
Assignee:
Merck & Co., Inc.
Inventors:
James M. Balkovec, Frances Aileen Bouffard, Regina M. Black
Abstract: There is disclosed an isolated gene coding for an enzyme involved in proline biosynthesis in Zalerion arboricola. There is also disclosed a method of using the gene to produce a strain of Z. arboricola containing high titers of a desirable fermentation product.
Type:
Grant
Filed:
June 18, 1996
Date of Patent:
August 4, 1998
Assignee:
Merck & Co., Inc.
Inventors:
Rosemarie Kelly, Prakash S. Masurekar, Elizabeth A. Register
Abstract: The present invention is directed to steroidal or terpenoidal compounds which inhibit farnesyl-protein transferase (FPTase). The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer.
Type:
Grant
Filed:
September 5, 1997
Date of Patent:
August 4, 1998
Assignee:
Merck & Co., Inc.
Inventors:
Sheo B. Singh, Russell B. Lingham, Keith C. Silverman, Deborah L. Zink, Isabel Martin, Fernando Pelaez, Manuel Sanchez
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:
December 5, 1996
Date of Patent:
July 14, 1998
Assignee:
Merck & Co., Inc.
Inventors:
Mark Goulet, Wallace T. Ashton, Lin Chu, Michael H. Fisher, Narindar N. Girotra, Peter Lin, Matthew J. Wyvratt
Abstract: There are disclosed novel compounds having the formula ##STR1## which exhibit antifungal activity.
Type:
Grant
Filed:
October 21, 1996
Date of Patent:
June 23, 1998
Assignee:
Merck & Co., Inc.
Inventors:
Angela Basilio, Fernando Pelaez, Maria Teresa Diez, Francisca Vicente, Sandra A. Morris, James E. Curotto, Gerald F. Bills, Sarah J. Dreikorn, Otto D. Hensens, Jerrold M. Liesch, Rosalind G. Jenkins, John R. Thompson
Abstract: A closure device for containers comprising a cap having a piercing member, the cap moving first downward and then upward relative to a container to which it is affixed, when first rotated in the direction used to open the container, the piercing member capable of causing rupture of a seal on the container during the downward motion and the upward motion resulting in removal of the cap.
Abstract: There is disclosed a novel compound having the formula ##STR1## which exhibits antifungal activity.
Type:
Grant
Filed:
January 27, 1997
Date of Patent:
May 26, 1998
Assignee:
Merck & Co., Inc.
Inventors:
Jerrold M. Liesch, Maria S. Meinz, Janet C. Onishi, Sandra A. Morris, Robert E. Schwartz, Gerald F. Bills, Robert A. Giacobbe, Wendy S. Horn, Deborah L. Zink, Angeles Cabello, Maria T. Diez, Isabella Martin, Fernando Pelaez, Francisca Vicente
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:
December 5, 1996
Date of Patent:
May 26, 1998
Assignee:
Merck & Co., Inc.
Inventors:
Mark Goulet, Lin Chu, Wallace T. Ashton, Michael H. Fisher, Matthew J. Wyvratt, Roy G. Smith, Robert L. Bugianesi, Mitree M. Ponpipom, Yi Tien Yang, Peter Lin
Abstract: There are disclosed compounds of the general formula ##STR1## wherein all substituents are defined herein. The compounds are useful as antibiotic and antifungal agents.
Type:
Grant
Filed:
June 13, 1995
Date of Patent:
April 21, 1998
Assignee:
Merck & Co., Inc.
Inventors:
James M. Balkovec, James F. Dropinski, Frances Aileen Bouffard
Abstract: There is disclosed a novel compound having the formula ##STR1## which exhibits antifungal activity.
Type:
Grant
Filed:
October 21, 1996
Date of Patent:
January 27, 1998
Assignee:
Merck & Co., Inc.
Inventors:
Sandra A. Morris, Gerald F. Bills, James E. Curotto, Sarah J. Dreikorn, Angela Basilio, Maria Teresa Diez, Fernando Pelaez, Francisca Vicente, Bruce W. Burgess, Stanley L. Streicher, Deborah L. Zink, John R. Thompson
Abstract: There is disclosed a compound having the formula ##STR1## which is produced by the fungus, Arthrinium arundinis ATCC 74359, and exhibits antifungal activity.
Type:
Grant
Filed:
January 27, 1997
Date of Patent:
January 27, 1998
Assignee:
Merck & Co., Inc.
Inventors:
Jerrold M. Liesch, Maria S. Meinz, Janet C. Onishi, Robert E. Schwartz, Gerald F. Bills, Robert A. Giacobbe, Deborah L. Zink, Angeles Cabello, Maria T. Diez, Isabella Martin, Fernando Pelaez, Francisca Vicente
Abstract: There is disclosed a novel compound having the formula ##STR1## which exhibits antifungal activity.
Type:
Grant
Filed:
October 21, 1996
Date of Patent:
December 30, 1997
Assignee:
Merck & Co., Inc.
Inventors:
Sandra A. Morris, James E. Curotto, Gerald F. Bills, Sarah J. Dreikorn, Stanley L. Streicher, Deborah L. Zink, John R. Thompson, Angela Basilio, Fernando Pelaez, Maria Teresa Diez, Francisca Vicente
Abstract: This invention is concerned with novel compounds represented by structural formula I ##STR1## which are useful in the treatment of arrhythmia.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
December 23, 1997
Assignee:
Merck & Co, Inc.
Inventors:
David A. Claremon, Nigel Liverton, Harold G. Selnick
Abstract: A series of novel spirocycles of general structural formula: ##STR1## or a pharmaceutically acceptable salt, hydrate or crystal form thereof are presented, whereinR.sup.1 =H.sub.3 CSO.sub.2 NH--, H.sub.3 CO--, alkylSO.sub.2 --, alkylCONH--, NO.sub.2 --;R.sup.2 =H, --OCH.sub.3 ;R.sup.3 and R.sup.4 taken together are .dbd.O, or R.sup.3 is H and R.sup.4 is OH;R.sup.5 =R.sup.6 taken together are --CH.sub.2 --CH.sub.2 --, .dbd.CH.sub.2 ;R.sup.7 is ##STR2## which are Class III antiarrhythmic agents and positive inotropic or cardiotonic agents.
Type:
Grant
Filed:
November 2, 1995
Date of Patent:
December 16, 1997
Assignee:
Merck & Co., Inc.
Inventors:
John J. Baldwin, David A. Claremon, Jason M. Elliott, Gerald S. Ponticello, David C. Remy, Harold G. Selnick
Abstract: This invention is concerned with novel compounds represented by structural formula I ##STR1## which are useful in the treatment of arrhythmia.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
November 25, 1997
Assignee:
Merck & Co., Inc.
Inventors:
David A. Claremon, Roger M. Freidinger, Nigel Liverton, Harold G. Selnick, Garry R. Smith
Abstract: This invention is concerned with novel compounds represented by structural formula I ##STR1## which are useful in the treatment of arrhythmia.
Type:
Grant
Filed:
August 19, 1996
Date of Patent:
November 25, 1997
Assignee:
Merck & Co., Inc.
Inventors:
David A. Claremon, Roger M. Freidinger, Nigel Liverton, Harold G. Selnick, Garry R. Smith