Patents Represented by Attorney Joseph F. DiPrima

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  • Benzodiazepine derivatives, compositions containing them and their use in therapy
    Patent number: 5410049
    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 cyclocalkyl;R.sup.2 represents a group ##STR2## wherein X is O, S or NR.sup.8 where R.sup.8 is H or C.sub.1-4 alkyl; 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 alkyl, C.sub.3-7 cycloalkyl, C.sub.4-7 cycloalkylalkyl or optionally substituted aryl;n is 0, 1, 2 or 3; are CCK and/or gastrin receptor antagonists. They and compositions thereof are useful in therapy.
    Type: Grant
    Filed: December 17, 1992
    Date of Patent: April 25, 1995
    Assignee: Merck Sharpe & Dohme Ltd.
    Inventor: Mark S. Chambers
  • 2-(3-pyridyl)-carbapenem antibacterial agents
    Patent number: 5409920
    Abstract: Carbapenems of the formula ##STR1## are useful antibacterial agents.
    Type: Grant
    Filed: October 5, 1990
    Date of Patent: April 25, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Ravindra N. Guthikonda, Frank P. DiNinno
  • Thiadiazoles useful in the treatment of senile dementia
    Patent number: 5405853
    Abstract: A class of novel thiadiazoles, substituted on one of the ring carbon atoms with a non-aromatic azacyclic or azabicyclic ring system, and substituted on the other ring carbon atom with a substituent of low lipophilicity, or a hydrocarbon substituent; are potent muscarinic agonists, and have good CNS penetrability. The compounds are therefore useful in the treatment of neurological and mental illnesses, and are also of benefit in the treatment of severe painful conditions.
    Type: Grant
    Filed: December 13, 1993
    Date of Patent: April 11, 1995
    Assignee: Merck Sharpe & Dohme Ltd.
    Inventors: Raymond Baker, Angus M. MacLeod, John Saunders, Kevin Merchant
  • Solution preparation system
    Patent number: 5402834
    Abstract: Solutions are prepared by accurately dispensing and weighing concentrated solutions of salts, acids and bases as well as water or organic solvent, and mixing to achieve homogeneity. The final solution may be stored or used directly from the system.
    Type: Grant
    Filed: November 25, 1992
    Date of Patent: April 4, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Michael D. Levin, William F. Richardson, Alan B. Todtenkopf
  • Spirocycles
    Patent number: 5403846
    Abstract: Compounds of the general formula: ##STR1## or a pharmaceutically acceptable salt, hydrate or crystal form enantiomer, diastereomer or mixtures thereof are Class III antiarrhythmic agents.
    Type: Grant
    Filed: November 22, 1993
    Date of Patent: April 4, 1995
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, David A. Claremon, Gerald S. Ponticello, Harold G. Selnick
  • Quinazolinones substituted with phenoxyphenylacetic acid derivatives
    Patent number: 5401745
    Abstract: Phenoxyphenylacetic acids and derivatives of general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebal and cardiac ischemia, myocardial infarction, inflammatory diseases, Raynaud's disease, and endotoxic shock, and asthma.
    Type: Grant
    Filed: March 19, 1993
    Date of Patent: March 28, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Scott W. Bagley, Prasun K. Chakravarty, Anna Chen, Daljit S. Dhanoa, Kenneth J. Fitch, William J. Greenlee, Elizabeth M. Naylor, James R. Tata, Thomas F. Walsh, David L. Williams, Jr.
  • Bridged biphenyl carbapenem antibacterial compounds
    Patent number: 5401735
    Abstract: Carbapenems of the formula: ##STR1## are disclosed as useful antibacterial agents.
    Type: Grant
    Filed: August 2, 1993
    Date of Patent: March 28, 1995
    Assignee: Merck & Co., Inc.
    Inventor: Frank P. Dininno
  • Antibiotic peptides bearing aminoalkylthioether moieties
    Patent number: 5399552
    Abstract: Certain aminoalkyl thioethers represented by the formula ##STR1## their acid addition salts and quaternary ammonium salts are described. The compounds have useful antimicrobial properties.
    Type: Grant
    Filed: October 17, 1991
    Date of Patent: March 21, 1995
    Assignee: Merck & Co, Inc
    Inventor: Frances A. Bouffard
  • Glycosidation route to 4"-epi-methylamino-4"-deoxyavermectin B.sub.1
    Patent number: 5399717
    Abstract: A stereocontrolled glycosidation with thiophenyl 4-(N-allyloxycarbonyl)-epi-methylamino-4-deoxyoleandrose and 5-O-allyloxycarbonyl avermectin B.sub.1 monosaccharide using N-iodosuccinimide produces exclusively the .alpha.-anomer of a precursor of 4"-epi-methylamino-4"-deoxyavermectin B.sub.1 in 90% yield. Deprotection and crystallization as the benzoic acid salt yields 4"-epi-methylamino-4"-deoxyavermectin B.sub.1 (emamectin benzoate), a potent insecticide.
    Type: Grant
    Filed: September 29, 1993
    Date of Patent: March 21, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Raymond Cvetovich, Mallory F. Loewe
  • Antiparasitic agents
    Patent number: 5399582
    Abstract: There are disclosed novel compounds which are derived from the fermentation of a strain of Nodulisporium sp. The compounds are highly potent ectoparasiticidal, antiparasitic and, insecticidal gents.
    Type: Grant
    Filed: November 1, 1993
    Date of Patent: March 21, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Anne W. Dombrowski, Richard G. Endris, Gregory L. Helms, Otto D. Hensens, John G. Ondeyka, Dan A. Ostlind, Jon D. Polishook, Deborah L. Zink
  • Biologically active compounds
    Patent number: 5399587
    Abstract: The present invention relates to novel potassium channel agonists which are useful in activating the calcium activated Maxi-K potassium channel in mammalian neuronal and smooth muscle tissue. The claimed compounds are of the general formula: ##STR1## In addition, a novel microbiological process for producing the claimed compounds is described.
    Type: Grant
    Filed: December 13, 1993
    Date of Patent: March 21, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Maria L. Garcia, Robert A. Giacobbe, Otto D. Hensens, Gregory J. Kaczorowski, Seok H. Lee, Owen B. McManus, Deborah L. Zink
  • Process of synthesizing binaphthyl derivatives
    Patent number: 5399771
    Abstract: A process of synthesizing a compound of the formula 1: ##STR1## is disclosed, which comprises reacting a compound of the formula 2: ##STR2## with diphenylphosphine in the presence of an amine base and a nickel catalyst to produce a compound of formula 1.
    Type: Grant
    Filed: June 1, 1994
    Date of Patent: March 21, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Dongwei Cai, Joseph F. Payack, Thomas R. Verhoeven
  • 6-amido-1-methyl-2-(substituted-thio)carbapenems
    Patent number: 5395931
    Abstract: New antibacterial 6-amido-1-methyl-2-(substituted-thio)-carbapenems and process for their synthesis involving new azetidinone intermediates.
    Type: Grant
    Filed: May 20, 1992
    Date of Patent: March 7, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Mark L. Greenlee, Frank P. DiNinno, Thomas N. Salzmann
  • Process of making chiral 2-aryl-1,4-butanediamine derivatives as useful neurokinin-A antagonists
    Patent number: 5391819
    Abstract: Disclosed herein is a process of making chiral 2-aryl-1,4-butanediamine derivatives useful as neurokinin-A antagonists of Formula 7 ##STR1##
    Type: Grant
    Filed: September 30, 1992
    Date of Patent: February 21, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Paul E. Finke, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills
  • Benzimidazolinones substituted with phenoxyphenylacetic acid derivatives
    Patent number: 5391566
    Abstract: Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, pulmonary hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, inflammatory diseases including Raynaud's disease and asthma.
    Type: Grant
    Filed: July 20, 1993
    Date of Patent: February 21, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Prasun K. Chakravarty, Elizabeth M. Naylor, James R. Tata, Thomas F. Walsh
  • Substituted imidazo-fused 5-membered ring heterocycles as angiotensin II antagonists
    Patent number: 5389660
    Abstract: There are disclosed new substituted imidazo-fused 5-membered ring heterocyclic compounds and derivatives thereof which are useful as angiotensin II antagonists.
    Type: Grant
    Filed: October 7, 1992
    Date of Patent: February 14, 1995
    Assignee: Merck & Co., Inc.
    Inventors: William J. Greenlee, David B. R. Johnston, Malcolm MacCoss, Nathan B. Mantlo, Arthur A. Patchett, Prasun K. Chakravarty, Thomas F. Walsh
  • Process for the preparation of 1-[3-acetylthio-2(s)-methylpropanoyl]-l-proline
    Patent number: 5387697
    Abstract: The intermediate 1-[3-acetylthio-2(s)-methylpropanoyl]-1-proline is prepared by reacting L-proline with (R)-3-acetylthio-2-methyl propanoyl chloride at 0-5.degree. C., with pH controlled at 7.5-8.5, using 2.5M potassium hydroxide and potassium phosphate buffer, which gives >97% pure material after crystallizing from the reaction mixture.
    Type: Grant
    Filed: June 13, 1994
    Date of Patent: February 7, 1995
    Assignee: Merck & Co., Inc.
    Inventor: Azucena C. Hen
  • Lipopeptide derivatives
    Patent number: 5385884
    Abstract: There are disclosed lipopeptide derviatives of the general formula: ##STR1## where the substituents are defined herein which have antifungal and antiprotozoal activity. There are also disclosed pharmaceutical compositions containing these compounds.
    Type: Grant
    Filed: August 27, 1991
    Date of Patent: January 31, 1995
    Assignee: Merck & Co. Inc.
    Inventors: Milton L. Hammond, Robert E. Schwartz, James M. Balkovec
  • Disubstituted 6-aminoquinazolinones
    Patent number: 5385894
    Abstract: Novel disubstituted 6-aminoquinazolinones of the Formula (I), are useful as angiotensin II antagonists: ##STR1##
    Type: Grant
    Filed: April 4, 1994
    Date of Patent: January 31, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Stephen E. de Laszlo, Tomasz W. Glinka, William J. Greenlee, Prasun K. Chakravarty, Arthur A. Patchett
  • Lipopeptide derivatives
    Patent number: 5386009
    Abstract: The present invention is directed to water-soluble derivatives of antibiotic lipopeptides. The derivatives have good solubility properties in aqueous medium, rendering them more useful as therapeutic agents.
    Type: Grant
    Filed: March 19, 1990
    Date of Patent: January 31, 1995
    Assignee: Merck & Co. Inc.
    Inventors: Milton L. Hammond, Robert E. Schwartz, James M. Balkovec