Patents by Inventor Paul Sohar

Paul Sohar has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Process for the preparation of imidazolyl macrolide immunosuppressants
    Patent number: 5777105
    Abstract: Imidazolmethyloxy-substituted tricyclo-macrolide immunosuppressants are prepared by reacting a tricyclo-macrolide with an imidazolmethyl trichloroacetimidate in the presence of an acid. The invention further provides a crystalline salt of imidazolmethyloxy-substituted tricyclo-macrolide, as well as novel compounds useful in the process of the present invention.
    Type: Grant
    Filed: July 23, 1996
    Date of Patent: July 7, 1998
    Assignee: Merck & Co., Inc.
    Inventors: David J. Mathre, Richard F. Shuman, Paul Sohar, Zhiguo Song
  • Synthesis of hydroxysulfone and related compounds
    Patent number: 5760249
    Abstract: This invention is concerned with an improved process for the synthesis of hydroxysulfone, which is a key intermediate in the synthesis of carbonic anhydrase inhibitors, especially dorzolamide. Carbonic anhydrase inhibitors are known to be effective in treating elevated intraocular pressure or glaucoma.
    Type: Grant
    Filed: August 28, 1996
    Date of Patent: June 2, 1998
    Assignees: Merck & Co., Inc., Zeneca Limited
    Inventors: David J. Mathre, Paul Sohar, David Moody, Andrew J. Blacker
  • Process to derivatives of piperizinylcamphorsulfonyl oxytocin antagonists
    Patent number: 5693805
    Abstract: A process for the manufacture of oxytocin receptor antagonists of the following formula (I) ##STR1## and their crystalline salts is disclosed.
    Type: Grant
    Filed: September 12, 1995
    Date of Patent: December 2, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Anthony M. DeMarco, Edward J.J. Grabowski, Guo-Jie Ho, David J. Mathre, Khateeta M. Emerson, Richard F. Shuman, Paul Sohar
  • Enantioselective synthesis of 5,6-dihydro-(S)-4-(ethylamino)-(S)-6-methyl-4H-thieno?2,3-B!thiopyran-2- sulfonamide 7,7-dioxide
    Patent number: 5688968
    Abstract: A key step in the synthesis of 5,6-dihydro-(S)-4-(ethylamino)-(S)-6-methyl-4H-thieno?2,3-b!thiopyran-2-su lfonamide 7,7-dioxide (dorzolamide) and related compounds is a Ritter reaction with an unexpected tendency to proceed with retention of chirality.
    Type: Grant
    Filed: January 6, 1995
    Date of Patent: November 18, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Thomas J. Blacklock, David J. Mathre, Paul Sohar
  • Synthesis of an intermediate for the preparation of 5,6-dihydro-(s)-4-(ethylamino)-(s)-6-methyl-4h-thieno [2,3-b]thiopyran-2-sulfonamide 7,7-dioxide intermediates and related compounds
    Patent number: 5574176
    Abstract: This invention is concerned with an improved process for the synthesis of and intermediate en route to 5,6-dihydro-(s)-4-(ethylamino)-(s)-6-methyl-4h-thieno[2,3-b]thiopyran-2-su lfonamide 7,7-dioxide and related compounds. The instant process reduces the reaction time for the synthesis of the key intermediate from 3 to 4 days to from about 2 to about 4 hours while retaining the high enantiomeric purity of the product.
    Type: Grant
    Filed: April 26, 1995
    Date of Patent: November 12, 1996
    Assignee: Merck & Co., Inc.
    Inventors: David J. Mathre, Paul Sohar, Lynn M. Brown
  • Enantiospecific synthesis of S-(+)-5,6-dihydro-4-(R-amino)-4H-thieno(2,3-b)thiopyran-2-sulfonamide-7, 7-dioxide
    Patent number: 5157129
    Abstract: 5,6-Dihydro-4-(R-amino)-4H-thieno[2,3-b]-thiopyran-2-sulfonamide-7,7-dioxid e is a potent carbonic anhydrase inhibitor useful in the treatment of ocular hypertension and glaucoma. The S-(+)-enantiomer of that compound, the more active enantiomer, is prepared by a process involving an intermediate step of an enantioselective reduction of a carbonyl group employing an oxazaborolidine chiral catalyst.
    Type: Grant
    Filed: April 18, 1990
    Date of Patent: October 20, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Thomas J. Blacklock, Todd K. Jones, Edward J. J. Grabowski, David J. Mathre, Julie J. Mohan, Paul Sohar, F. Edward Roberts, Lyndon C. Xavier
  • Process for racemizing an enantiomer of 5,6-dihydro-4-alkylamino-4H-thieno(or furo) [2,3-B]-thiopyran-2-sulfonamide-7,7-dioxide
    Patent number: 5011942
    Abstract: Compounds classified as 5,6-dihydro-4-alkylamino-4H-thieno (or furo) [2,3-b]thiopyran-2-sulfonamide-7,7-dioxide are carbonic anhydrase inhibitors useful in the treatment of ocular hypertension, and most of the carbonic anhydrase inhibitory activity resides in only one of the enantiomers. The undesired enantiomer is utilized by racemization by thermolysis of an N-acyl derivative in a basic environment followed by removal of the acyl group. The racemate may then be resolved into the enantiomers.
    Type: Grant
    Filed: February 5, 1990
    Date of Patent: April 30, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Thomas J. Blacklock, Edward J. J. Grabowski, Paul Sohar
  • Process for the preparation of 1,1-dioxo-7-substituted cephems
    Patent number: 4992541
    Abstract: The present invention relates to an improved process for the preparation of the compounds of formula (I) ##STR1## which involve the direct oxidation without N-protection of the compound of the formula (II) ##STR2##
    Type: Grant
    Filed: August 1, 1989
    Date of Patent: February 12, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Thomas J. Blacklock, John W. Butcher, Paul Sohar, Theresa Lamanec
  • (S)-Alkyl 3-(thien-2-ylthio)butyrate and analogs and synthesis thereof
    Patent number: 4968814
    Abstract: (S)-Alkyl 3-(thien-2-ylthio)butyrate and analogs are intermediates in the synthesis of the chiral (S,S)-5,6-dihydro-4-ethylamino-6-methyl-4H-thieno[2,3-b]thiopyran-2-sulfon amide-7,7-dioxide and analogs thereof, topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma.
    Type: Grant
    Filed: April 18, 1990
    Date of Patent: November 6, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Thomas J. Blacklock, Edward J. J. Grabowski, Paul Sohar
  • Process for the preparation of cephamycin antibiotics
    Patent number: 4220762
    Abstract: An improved process for preparing the antibiotic compound 7.beta.-(2-thienylacetamido)-7-methoxy-3-carbamoyloxymethyl-3-cephem-4-car boxylic acid, from the N-blocked esters of the compound 7.beta.-(D-5-amino-5-carboxyvaleramido)-3-carbamoyloxymethyl-7-methoxy-3-c ephem-4-carboxylic acid (Cephamycin C), by conducting the transacylation of the latter in a homogeneous solution containing a trimethylsilyl enol ether.
    Type: Grant
    Filed: March 30, 1979
    Date of Patent: September 2, 1980
    Assignee: Merck & Co., Inc.
    Inventors: George M. Love, Paul Sohar
  • Process for the preparation of cephamycin antibiotics
    Patent number: 4218563
    Abstract: An improved process for preparing the antibiotic compound 7.beta.-(2-thienylacetamido)-7-methoxy-3-carbamoyloxymethyl-3-cephem-4-car boxylic acid, from the N-blocked esters of the compound 7.beta.-(D-5-amino-5-carboxyvaleramido)-3-carbamoyloxymethyl-7-methoxy-3-c ephem-4-carboxylic acid (Cephamycin C), by conducting the transacylation of the latter in a homogenous solution containing N-trimethylsilyl loweralkyl carbamates.
    Type: Grant
    Filed: March 30, 1979
    Date of Patent: August 19, 1980
    Assignee: Merck & Co., Inc.
    Inventors: George M. Love, Paul Sohar, Leonard M. Weinstock
  • Process for preparing monomer of bile acid sequestrant polymer
    Patent number: 4093657
    Abstract: The invention disclosed herein relates to a novel process for preparing the monomer, 3-[N-(3-chloropropyl)methylamino]-N,N,N-trimethyl-propan-1-aminium chlorid e, which comprises reacting N,N-bis(3-chloropropyl)methylamine with trimethylamine. The 3,3-ionene monomer thus obtained is a key intermediate for making the linear, unbranched, non-cross-linked polymer, poly-[{methyl-(3-trimethylammoniopropyl)imino}trimethylene dichloride], which is valuable as an oral bile acid sequestrant.
    Type: Grant
    Filed: April 9, 1976
    Date of Patent: June 6, 1978
    Assignee: Merck & Co., Inc.
    Inventors: Erwin F. Schoenewaldt, Paul Sohar