Patents by Inventor Thomas N. Salzmann

Thomas N. Salzmann 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).

  • Patent number: 5985844
    Abstract: Compounds of the formula: ##STR1## where R is hydrogen, hydroxyl, alkyl or acyl, R' and R" together are oxo, hydroxyimino or alkoxyimino, and R' and R" independently are hydrogen, hydroxyl, acyloxy, or amino substituted by any of hydrogen, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, alkoxycarbonyl, aralkoxycarbonyl, alkylsulfonyl or arylsulfonyl, and n is 0 or 1, and the pharmaceutically acceptable salts thereof. The compounds are macrolide antibiotics and are also useful as intermediates to the synthesis of other macrolide antibiotics. Pharmaceutical compositions and methods of their use are also provided for.
    Type: Grant
    Filed: March 26, 1992
    Date of Patent: November 16, 1999
    Assignee: Merck & Co., Inc.
    Inventors: James V. Heck, William J. Leanza, Ronald W. Ratcliffe, Thomas N. Salzmann, Kothandaraman Shankaran, Michael J. Szymonifka, Robert R. Wilkening
  • 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
  • Patent number: 5362723
    Abstract: Carbapenems having the formula: ##STR1## are useful antibacterial agents.
    Type: Grant
    Filed: May 20, 1992
    Date of Patent: November 8, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. DiNinno, Thomas N. Salzmann, David A. Muthard
  • Patent number: 5350846
    Abstract: Carbapenems of the formula: ##STR1## are useful intermediates to antibacterial agents.
    Type: Grant
    Filed: January 25, 1993
    Date of Patent: September 27, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. DiNinno, Thomas N. Salzmann
  • Patent number: 5247074
    Abstract: Carbapenems of the formula: ##STR1## are useful intermediates to antibacterial agents.
    Type: Grant
    Filed: May 20, 1992
    Date of Patent: September 21, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. Dininno, Thomas N. Salzmann, Eugene D. Thorsett
  • Patent number: 5240920
    Abstract: Carbapenems having the formula: ##STR1## where X is O or S(O).sub.0-2 ; are useful antibacterial agents, especially with respect to activity against methicillin resistant Staphylococcus aureus (MRSA).
    Type: Grant
    Filed: May 4, 1992
    Date of Patent: August 31, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. DiNinno, Thomas N. Salzmann, Mark L. Greenlee
  • Patent number: 5208329
    Abstract: Carbapenems of the formula ##STR1## are useful intermediates to antibacterial agents.
    Type: Grant
    Filed: February 14, 1992
    Date of Patent: May 4, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. Dininno, Thomas N. Salzmann
  • Patent number: 5196529
    Abstract: Carbapenems of the formula ##STR1## are useful as intermediates to antibacterial agents.
    Type: Grant
    Filed: October 9, 1990
    Date of Patent: March 23, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. Dininno, Thomas N. Salzmann, Mark L. Greenlee
  • Patent number: 5183887
    Abstract: New antibacterial spirocyclic 6-amido carbapenems of the structural formulas: ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-8 substituted or unsubstituted alkyl, or C.sub.6-10 substituted or unsubstituted aryl; R.sup.5 is hydrogen or a protecting group for alcohol; R.sup.6 is hydrogen or a protecting group for amido nitrogen; R.sup.7 is hydrogen or a protecting group for amido nitrogen; and R.sup.8 is hydroxy, hydrogen, C.sub.1-8 substituted or unsubstituted thioalkyl, C.sub.6-10 substituted or unsubstituted thioaryl, 5 or 6 membered, substituted or unsubstituted thioheteroaryl; and a process for their synthesis through novel spirocyclic 4-amido azetidinones are disclosed.
    Type: Grant
    Filed: July 9, 1991
    Date of Patent: February 2, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Mark L. Greenlee, Thomas N. Salzmann, Frank P. DiNinno
  • Patent number: 5182385
    Abstract: Carbapenems of the formula: ##STR1## are useful intermediates to antibacterial agents.
    Type: Grant
    Filed: October 9, 1990
    Date of Patent: January 26, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. Dininno, Thomas N. Salzmann
  • Patent number: 5177202
    Abstract: Carbapenems of the formula ##STR1## are useful intermediates to antibacterial agents.
    Type: Grant
    Filed: October 9, 1990
    Date of Patent: January 5, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. Dininno, Mark L. Greenlee, Thomas N. Salzmann
  • Patent number: 5162332
    Abstract: Selected 17.beta.-Polyaroyl-4-aza-5.alpha.-androst-1-en-3-ones as steroidal reductase inhibitors of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethylR.sup.2 is polycyclic aromatic radical which can be substituted with one or more of: --OH, protected --OH, --OC.sub.1 --C.sub.4 alkyl, C.sub.1 -C.sub.4 alkyl, or nitro, wherein the doted line represents a double bond which can be present, and pharmaceutically acceptable salts or esters thereof, and a pharmaceutical formulation. The above compounds are active as steroidal reductase inhibitors and thus are useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.
    Type: Grant
    Filed: October 9, 1991
    Date of Patent: November 10, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Nathan G. Steinberg, Gary H. Rasmusson, Thomas N. Salzmann
  • Patent number: 5151512
    Abstract: Carbapenem intermediates having the formula: ##STR1## where Z is; ##STR2## M is a removable protecting group for carboxy and P' is a removable protecting group for hydroxy are useful intermediates for preparing antibacterial agents, especially with respect to activity against methicillin resistant Staphylococcus aureus (MRSA).
    Type: Grant
    Filed: October 15, 1990
    Date of Patent: September 29, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. DiNinno, Mark L. Greenlee, Thomas N. Salzmann
  • Patent number: 5151430
    Abstract: Specific 17.beta.-thiobenzoyl-4-aza-5.alpha.-androst-1-en-3-ones as antiandrogenic agents of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethyl andR.sup.2 is phenyl substituted with one or more of: --SH, --SC.sub.1 --C.sub.4 alkyl, --SO--C.sub.1 --C.sub.4 alkyl, --SO.sub.2 --C.sub.1 --C.sub.4 alkyl, --SO.sub.2 N--(C.sub.1 -C.sub.4 alkyl).sub.2, C.sub.1 -C.sub.4 alkyl, --(CH.sub.2).sub.m SH, --S(CH.sub.2).sub.n OCOCH.sub.3, where m is 1-4, n is 1-3, and providing C.sub.1 -C.sub.4 alkyl is only present when one of the above sulfur-containing radicals is present, wherein the dotted line can represent a double bond, and pharmaceutically acceptable esters and salts thereof. Also included is a pharmaceutical formulation thereof. The above compounds are active as antiandrogenic agents and thus are useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.
    Type: Grant
    Filed: August 16, 1991
    Date of Patent: September 29, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Nathan G. Steinberg, Gary H. Rasmusson, Thomas N. Salzmann
  • Patent number: 5138050
    Abstract: New antibacterial 6-amido-1-methylcarbapenems and process for their synthesis involving new azetidinone intermediates.
    Type: Grant
    Filed: March 7, 1991
    Date of Patent: August 11, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Ravindra N. Guthikonda, Frank P. DiNinno, Thomas N. Salzmann
  • Patent number: 5132420
    Abstract: Carbapenem intermediates having the formula: ##STR1## where Z is ##STR2## M is a removable protecting group for carboxy and P' is a removable protecting group for hydroxy, are useful intermediates for preparing antibacterial agents, especially with respect to activity against methicillin resistant Staphylococcus aureus (MRSA).
    Type: Grant
    Filed: October 11, 1990
    Date of Patent: July 21, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Frank P. Dininno, Mark L. Greenlee, Thomas N. Salzmann
  • Patent number: 5124323
    Abstract: Carbapenems having the formula: ##STR1## In which Q.sup.+ is quinolinium or isoquinolinium, are useful antibacterial agents.
    Type: Grant
    Filed: July 17, 1991
    Date of Patent: June 23, 1992
    Assignee: Merck
    Inventors: Frank P. DiNinno, Thomas N. Salzmann, David A. Muthard
  • Patent number: 5104984
    Abstract: A process is described for the stereochemically controlled synthesis of intermediates useful in producing 1-betamethylcarbapenem antibiotic intermediates involving reacting a beta lactam with a chiral thia- or oxazolidinone enolate to preferentially produce a beta-methyl intermediate which can be transformed into a carbapenem antibiotic.
    Type: Grant
    Filed: July 11, 1990
    Date of Patent: April 14, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Thomas N. Salzmann, Lelia M. Fuentes, Ichiro Shinkai
  • Patent number: 5098908
    Abstract: Novel 17.beta.-hydroxybenzoyl-4-aza-5.alpha.-androst-1-en-3-ones as tetosterone reductase inhibitors of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethy andR.sup.2 is phenyl substituted with one or more of: --OH, --OFC.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkyl, --(CH.sub.2).sub.m H, --(CH.sub.2).sub.n COOH, including protected --OH, where m is 1-4, n is 1-3, and providing C.sub.1 -C.sub.4 alkyl is only present when one of the above oxygen containing radicals is present, wherein the dotted line represents a double bond which can be present, pharmaceutically acceptable salts and esters thereof, and a pharmaceutical formulation thereof. The above compounds are active as testosterone reductase inhibitors and thus are useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.
    Type: Grant
    Filed: June 20, 1990
    Date of Patent: March 24, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Nathan G. Steinberg, Gary H. Rasmusson, Thomas N. Salzmann
  • Patent number: 5061802
    Abstract: New 17.beta.-aminobenzoyl-4-aza-5.alpha.-androst-1-en-3-ones as benign prostatic hypertrophy agents of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethyl andR.sup.2 is phenyl substituted with --N(R.sup.3).sub.2, which can be protected, where R.sub.3 is independently H or C.sub.1 -C.sub.4 alkyl, wherein the phenyl ring can also be further substituted by C.sub.1 -C.sub.4 alkyl, wherein the dotted line can represent a double bond, and pharmaceutically acceptable salts thereof, and a pharmaceutical formulation thereof. The above compounds are active as benign prostatic hypertrophy therapy agents and are useful topically for the treatment of acne, seborrhea, female hirsutism, and particularly effective systemically in the treatment of benign prostatic hypertrophy.
    Type: Grant
    Filed: June 20, 1990
    Date of Patent: October 29, 1991
    Assignee: Merck & Co. Inc.
    Inventors: Nathan G. Steinberg, Gary H. Rasmusson, Thomas N. Salzmann