Patents Represented by Attorney Joseph F. DiPrima
  • Patent number: 6486195
    Abstract: The most thermodynamically stable crystalline form of the benzoic acid salt of 4″-deoxy-4″-epi-methylamino avermectin B1a/B1b as the hemihydrate is obtained by crystallization from organic solvents containing a controlled amount of water.
    Type: Grant
    Filed: January 20, 1995
    Date of Patent: November 26, 2002
    Assignee: Merck & Co., Inc.
    Inventors: Raymond Cvetovich, James A. McCauley, Richard Demchak, Richard J. Varsolona
  • Patent number: 5837228
    Abstract: A bioerodible controlled release dosage form is disclosed comprising a polymer formed by condensing beneficial agents having a hydroxyl functionality of two or more with diketene acetals or divinyl ethers which delivers beneficial agents to a biological environment of use. A statistically significant portion of the beneficial agent is covalently bonded within the polymer matrix.
    Type: Grant
    Filed: September 2, 1992
    Date of Patent: November 17, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Chung Shih, Gaylen M. Zentner, Randall V. Sparer, R. Lee Seward
  • Patent number: 5830875
    Abstract: Novel avermectin and milbemycin derivatives are disclosed, where the C-24 and C-25 carbon atoms are substituted by hydrogen, alkyl, alkenyl, substituted alkyl or substituted alkenyl groups. These compounds can be further substituted at the 4"-, 5-, 13-, and 23-positions. The new C-24 and C-25 substituted avermect prepared by cleavage of known and suitably protected avermectin and milbemycin compounds. The new compounds are potent anti-parasitic agents, in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.
    Type: Grant
    Filed: October 30, 1989
    Date of Patent: November 3, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Helmut Mrozik, Thomas L. Shih
  • Patent number: 5583130
    Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. The compounds are prepared by substitution of an amino-lactam with a substituted amide function. Growth promoting compositions containing such bezno-fused lactams as the active ingredient thereof are also disclosed.
    Type: Grant
    Filed: September 25, 1992
    Date of Patent: December 10, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Richard J. Bochis, Michael H. Fisher, Robert J. Devita, William R. Schoen, Matthew J. Wyvratt
  • Patent number: 5508435
    Abstract: .beta.- or .gamma.-Ketoesters and .beta.- or .gamma.-ketoamides are asymmetrically reduced with a Ru(II)-BINAP derived catalyst at about 40.degree. C. and about 50N/mm.sup.2 of hydrogen in the presence of a strong acid.
    Type: Grant
    Filed: January 5, 1994
    Date of Patent: April 16, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Joseph D. Armstrong, III, Lisa DiMichele, Alan W. Douglas, Jennifer L. Keller, Steven A. King, Andrew S. Thompson, Thomas R. Verhoeven
  • Patent number: 5468733
    Abstract: The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation in vivo. These CAAX analogs inhibit the farnesylation of Ras. Furthermore, these CAAX analogues differ from those previously described as inhibitors of Ras farnesyl 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: September 30, 1993
    Date of Patent: November 21, 1995
    Assignee: Merck & Co., Inc.
    Inventors: S. Jane deSolms, Elizabeth A. Giuliani, Samuel L. Graham
  • Patent number: 5466811
    Abstract: This invention relates to a the use of new oxodioxolenylmethyl carbamates to produce bioreversible neutral prodrugs from primary and secondary amines.
    Type: Grant
    Filed: July 18, 1994
    Date of Patent: November 14, 1995
    Assignee: Merck & Co., Inc.
    Inventor: Jose Alexander
  • Patent number: 5464762
    Abstract: Stereospecific (S)-6-bromo-2-tetraol is a key intermediate in the chemical synthesis of the chiral drug candidate, MK499, a ventricular arrythmias suppressant. The yeast strain Trichosporon capitatum (MY 1890) was employed for the bioconversion of 6-bromo-2-tetralone to the corresponding alcohol.
    Type: Grant
    Filed: June 24, 1994
    Date of Patent: November 7, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Michel M. Chartrain, Jayanthi Reddy, David M. Tschaen
  • Patent number: 5464122
    Abstract: This invention consists of an ophthalmic dispensing tip formed by injection molding, which has a one-piece molded tip to be used with a mating cap, the tip having an internally molded breakaway barrier membrane inside the flow channel, and the cap having a shaped stud fitting inside the tip, so that the final clockwise half-turn of the cap pushes the stud against the barrier and displaces it, thereby creating a restricted path through which the contents are dispensed.
    Type: Grant
    Filed: June 24, 1994
    Date of Patent: November 7, 1995
    Assignee: Merck & Co., Inc.
    Inventor: Arthur L. Lifshey
  • Patent number: 5455239
    Abstract: A compound of the formula I is disclosed. ##STR1## R.sup.13 represents hydrogen, NH.sub.2, C1-4 alkyl, C1-4 alkylamino or di(C1-4) alkylamino-;Y represents CH or N;Y" represents (a) CR.sup.y' R.sup.z' with R.sup.y' and R.sup.z' hydrogen, C1-6 alkyl, C.sub.3-8 cycloalkyl or C.sub.1-6 alkyl substituted with C.sub.3-8 cycloalkyl, or (b) N substituted with OR.sup.14 with R.sup.14 representing H, C.sub.1-4 alkyl or C.sub.1-4 alkyl substituted with COOH.Ar represents: ##STR2## One of R.sup.1 and R.sup.2 independently represent H, W as defined below or one of the groups (a) through (d) below, and the other represents H or W. Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: August 5, 1993
    Date of Patent: October 3, 1995
    Assignee: Merck & Co. Inc.
    Inventors: Lovji D. Cama, James V. Heck
  • Patent number: 5451579
    Abstract: A carbapenem antibiotic of the formula I ##STR1## is disclosed. The variable X.sup..crclbar. represents a counterion. Pharmaceutical compositions and methods of use are also disclosed.
    Type: Grant
    Filed: February 15, 1994
    Date of Patent: September 19, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Mark L. Greenlee, Frank P. DiNinno, Milton L. Hammond
  • Patent number: 5451582
    Abstract: Compounds of formula (I), and salts and prodrugs thereof ##STR1## wherein: R.sup.1 is H, certain optionally substituted C.sub.1.6 alkyl, or C.sub.3-7 cycloalkyl;R.sup.2 is (CH.sub.2).sub.q -tetrazolyl optionally substituted in the tetrazole ring by C.sub.1-4 alkyl, (CH.sub.2).sub.q -imidazolyl (where q is 0, 1, 2 or 3), CONHSO.sub.2 R.sup.9, SO.sub.2 NHCOR.sup.9 (where R.sup.9 is C.sub.1-6 alkyl, optionally substituted aryl or trifluoromethyl). SO.sub.2 NHR.sup.10 (where R.sup.10 is a nitrogen containing heterocycle), cyclopropyl or (CH.sub.2), CO.sub.2 H, where n is 1 or 2;R.sup.3 is C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ;R.sup.4 is C.sub.1-7 straight or branched chain alkyl; andx is 0, 1, 2 or 3;are CCK and/or gastrin receptor antagonists. They and compositions thereof are useful in therapy.
    Type: Grant
    Filed: February 12, 1993
    Date of Patent: September 19, 1995
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Mark S. Chambers, Victor G. Matassa, Stephen R. Fletcher
  • Patent number: 5451588
    Abstract: A class of substituted imidazole, triazole and tetrazole derivatives are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.
    Type: Grant
    Filed: November 22, 1993
    Date of Patent: September 19, 1995
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Victor G. Matassa, Leslie J. Street
  • Patent number: 5449682
    Abstract: Substituted heterocycles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I are useful as angiotensin II antagonists. ##STR1## wherein the substituents are as defined in the claims.
    Type: Grant
    Filed: May 17, 1993
    Date of Patent: September 12, 1995
    Assignee: Merck & Co., Inc.
    Inventors: William J. Greenlee, David Hangauer, Arthur A. Patchett, Thomas F. Walsh, Kenneth J. Fitch, Daljit S. Dhanoa, Ralph A. Rivero
  • Patent number: 5449819
    Abstract: Disclosed is a process for removing by-product phosphorus-containing (PO.sub.x) materials, alendronate and alendronate byproducts from crude mother liquors in an omega amino-1-hydroxy-C.sub.2 -C.sub.6 alkylidene-1,1-bisphosphonic acid synthesis process, e.g. alendronate sodium. Calcium chloride is added first to the crude mother liquors, then calcium oxide to precipitate the PO.sub.x materials, then neutralized to about pH 7 to complete precipitation. Substantially all of the alendronate sodium active ingredient is removed from the precipitate. Following filtration, the PO.sub.x filtercake can then be disposed of by incineration, landfilling or reclamation of usable phosphorus as fertilizer. The remaining filtrate can then be further treated in an environmentally acceptable manner by wastewater treatment or recycling to the process.
    Type: Grant
    Filed: June 6, 1994
    Date of Patent: September 12, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Edamanal S. Venkataramani, Andrew L. Forman, Ralph J. Magliette, Jr., Donald McKinney
  • Patent number: 5444067
    Abstract: This invention relates to compounds represented by formula I: ##STR1## which are agonists of angiotensin II. The invention is also concerned with the use of aforementioned agonists in the treatment of states meditated by angiotensin.
    Type: Grant
    Filed: August 30, 1993
    Date of Patent: August 22, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Salah Kivlighn, Victor J. Lotti, Ralph A. Rivero, Peter K. S. Siegl, Gloria J. Zingaro
  • Patent number: 5441959
    Abstract: Novel substituted quinazolinones of the formula (I) are useful as angiotensin II antagonists.
    Type: Grant
    Filed: August 18, 1993
    Date of Patent: August 15, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Prasun K. Chakravarty, Stephen E. de Laszlo, Tomasz W. Glinka, William J. Greenlee, Nathan B. Mantlo, Arthur A. Patchett
  • Patent number: 5442056
    Abstract: The present invention is directed to a process of making 2-aryl carbapenems of formula 1 from a compound of formula A.
    Type: Grant
    Filed: May 17, 1994
    Date of Patent: August 15, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Ann E. DeCamp, Edward J. J. Grabowski, Mark A. Huffman, Lyndon C. Xavier, Nobuyoshi Yasuda
  • Patent number: 5439918
    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 treatment of cancer.
    Type: Grant
    Filed: March 14, 1994
    Date of Patent: August 8, 1995
    Assignee: Merck & Co., Inc.
    Inventors: S. Jane deSolms, Samuel L. Graham
  • Patent number: 5439914
    Abstract: Compounds of the general structural formula: ##STR1## or a pharmaceutically acceptable salt, hydrate or crystal form thereof, wherein;X is O or CH.sub.2R.sup.1 is H if R.sup.2 is not H or if R.sup.2 is H then R.sup.1 is ##STR2## R.sup.2 is --H if R.sup.1 is not H or if R.sup.1 is H then R.sup.2 is; ##STR3## and R.sup.3 is ##STR4## are Class HI antiarrhythmic agents.
    Type: Grant
    Filed: February 18, 1994
    Date of Patent: August 8, 1995
    Assignee: Merck & Co., Inc.
    Inventors: David A. Claremon, Gerald S. Ponticello, Harold G. Selnick