Patents Represented by Attorney Lawrence S. Levinson
  • Patent number: 4754041
    Abstract: Antibacterial activity is exhibited by 2-azetidinones activated in the 1-position with an --SO.sub.3 H group and having in the 3-position an acylamino group of the formula ##STR1## wherein X is --(CH.sub.2).sub.
    Type: Grant
    Filed: September 29, 1986
    Date of Patent: June 28, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: David Kronenthal
  • Patent number: 4752616
    Abstract: Arylthioalkylphenylcarboxylic acids are provided which have the structure ##STR1## wherein Ar represents an aryl group including phenyl or naphthyl which may or may not include one or more substituents, A is ##STR2## R is hydrogen, alkali metal or lower alkyl, m is 0, 1, 2, or 3, n is 0, 1, or 2, p is 1 to 5, q, is 0, 1, 2, or 3, r is 0, 1, 2, or 3. These compounds are cardiovascular agents which exhibit thromboxane antagonist activity and thus are useful in the treatment of thrombotic disease.
    Type: Grant
    Filed: June 29, 1987
    Date of Patent: June 21, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Steven E. Hall, Philip D. Stein
  • Patent number: 4752645
    Abstract: Vasodilating activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: May 21, 1987
    Date of Patent: June 21, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Jagabandhu Das, David Floyd, John Krapcho
  • Patent number: 4752469
    Abstract: Cultivation of the microorganism Chromobacterium violaceum A.T.C.C. No. 31532 yields two novel compounds which have been designated SQ 28,504 and SQ 28,546 in addition to EM5117, a previously disclosed antibacterial compound.
    Type: Grant
    Filed: January 9, 1984
    Date of Patent: June 21, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Richard B. Sykes, J. Scott Wells, Raymond Cooper
  • Patent number: 4752613
    Abstract: Compounds represented by the formula ##STR1## wherein X is halogen, lower alkyl, arylalkyl, alkoxy or hydroxy; wherein the phenyl ring is mono or disubstituted, R' is --COOH or ##STR2## wherein R" is lower alkyl or aryl and n and m are independently zero, one, two or three which are potent thromboxane A.sub.2 receptor antagonists.
    Type: Grant
    Filed: August 3, 1987
    Date of Patent: June 21, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: David M. Floyd, Philip D. Stein
  • Patent number: 4751245
    Abstract: N-(6,6-dimethyl-2-hepten-4-ynyl)-1-naphthalenemethanamine derivatives are provided having the general formula ##STR1## wherein R.sub.1 is methoxy, iminomethyl or 1-iminoethyl and R.sub.2 and R.sub.3 are each hydrogen; or R.sub.1 is methyl and one of R.sub.2 and R.sub.3 is hydrogen and the other is halogen.The above compounds as well as acid-addition salts thereof are useful as antifungal agents.
    Type: Grant
    Filed: June 25, 1986
    Date of Patent: June 14, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Gregory S. Bisacchi, Robert Zahler
  • Patent number: 4751220
    Abstract: In accordance with the present invention an orally active monosulfactam antibiotics having a crystalline structure and thereby improved stability are disclosed. The antibiotics comprise the dierythromycin (M.sup..sym.=erythromycin.H.sup..sym.) salt or the dicholine (M.sup..sym. =HOCH.sub.2 CH.sub.2 N.sup..sym. (CH.sub.3).sub.3) salt of the acid (M.sup..sym. =H.sup..sym.) having the formula ##STR1## that is, [3S(Z)]-2[[[1-(2-amino-4-thiazolyl)-2-[[2,2-dimethyl-4-oxo-1-(sulfooxy)-3- azetidinyl]-amino]-2-oxoethylidene]amino]oxy]acetic acid.
    Type: Grant
    Filed: December 19, 1986
    Date of Patent: June 14, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: W. Lawrence Parker, Edward M. Cohen, William H. Koster
  • Patent number: 4749715
    Abstract: 7-Oxabicycloheptane substituted amino prostaglandin analogs are provided having the structural formula ##STR1## wherein n is 1 to 5; R.sup.1 is CO.sub.2 H, CO.sub.2 lower alkyl or ##STR2## and R.sup.2 is ##STR3## wherein R.sup.3 is lower alkyl, aralkyl, --NHalkyl or --NHaryl, or R.sup.2 is ##STR4## wherein q is 1 to 12, and R.sup.4 is lower alkyl, lower alkenyl, lower alkynyl, aryl, arylalkyl, lower alkoxy, aryloxy, arylalkyloxy, amino, alkylamino arylamino, arylalkylamino, lower alkyl-S--, aryl-S--, arylalkyl-S--, ##STR5## (wherein n' is 0, 1 or 2), alkylaminoalkyl, arylaminoalkyl, arylalkylaminoalkyl, alkoxyalkyl, aryloxyalkyl or arylalkoxyalkyl.The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease and are useful in the preparation of radiolabelled analogs.
    Type: Grant
    Filed: March 2, 1987
    Date of Patent: June 7, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Steven E. Hall
  • Patent number: 4749792
    Abstract: Analgesic activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein R.sub.1, R.sub.2 and R.sub.4 are each independently hydrogen, alkyl, carboxyalkyl, halosubstituted alkyl, hydroxyalkyl, aminoalkyl, mercaptoalkyl, alkylthioalkyl, (cycloalkyl)alkyl, (heteroaryl)alkyl, arylalkyl, carbamoylalkyl, guanidinylalkyl, or heteroaryl, and R.sub.3 is hydroxymethylene or carbonyl.
    Type: Grant
    Filed: September 26, 1984
    Date of Patent: June 7, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Sesha I. Natarajan, Eric M. Gordon
  • Patent number: 4749781
    Abstract: Compounds of the formula ##STR1## are disclosed. These compounds intervene in the conversion of angiotensinogen to angiotensin II by inhibiting renin and thus are useful as antihypertensive agents.
    Type: Grant
    Filed: September 19, 1986
    Date of Patent: June 7, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Eric M. Gordon
  • Patent number: 4748239
    Abstract: Vasodilating activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: April 24, 1987
    Date of Patent: May 31, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: David Floyd, John Krapcho
  • Patent number: 4748117
    Abstract: A new method is provided for forming crystals of amphotericin B directly in fermentation broth which crystals are easily separable without use of costly solvent extraction techniques which method includes a direct microbial cell autolysis step to induce crystal formation.
    Type: Grant
    Filed: April 16, 1986
    Date of Patent: May 31, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Raphael Y. Ko, Laszlo J. Szarka
  • Patent number: 4747829
    Abstract: A pre-filled syringe is provided with a retractile needle. The needle end of a syringe is enclosed in a sterile chamber within a casing sealed by a cap with a break-off tip. The barrel of the syringe is movable within the casing from a remote pre-injection position to a forward injection position and back again. When the barrel is moved forward a first end of the needle passes through the opening of the cap and then the opposite end comes in contact with the injectant. When the barrel is withdrawn to a pre-injection position, the needle is retracted within the casing and is prevented from re-entering the opening in the cap.
    Type: Grant
    Filed: January 21, 1987
    Date of Patent: May 31, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Jean-Louis Jacob, Gaetan Sanschagrin, Jean Thibodeau, France Guay
  • Patent number: 4746656
    Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sub.1 is aryl or heterocyclo;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is hydrogen, alkyl, alkenyl, alkynyl, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, halo substituted alkyl, or ##STR2## Y.sub.1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.m --S--, amino, substituted amino, carbamoyl, ##STR3## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR4## Y.sub.3 is hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.m --S--, ##STR5## amino, or substituted amino; Y.sub.4 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.
    Type: Grant
    Filed: July 21, 1986
    Date of Patent: May 24, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 4744989
    Abstract: A method is provided for preparing stable liposome precursors in the form of a water-soluble carrier material coated with a predetermined amount of a thin film of liposome components, which method includes the steps of dissolving at least one liposome-forming amphipathic lipid, optionally, at least one biologically active compound, and, optionally, at least one adjuvant in a suitable organic solvent and employing the resulting organic solution to coat a suitable water-soluble carrier material to form thin film of predetermined amount of liposome components thereon. Upon exposing the coated carrier material to water, the thin films of liposome components hydrate and the carrier material dissolves to give liposome preparations.
    Type: Grant
    Filed: March 21, 1986
    Date of Patent: May 17, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Nicholas I. Payne, Peter Timmins, Cheryl V. Ambrose
  • Patent number: 4745196
    Abstract: This invention is directed to orally active antihypertensive agents of the formula ##STR1## wherein R.sub.1 is certain alkyl or aralkyl groups.
    Type: Grant
    Filed: January 6, 1986
    Date of Patent: May 17, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Donald S. Karanewsky, Edward W. Petrillo, Jr.
  • Patent number: 4745202
    Abstract: Aerocavin, a novel antibiotic substance having the structure ##STR1## and aerocyanidin, a novel antibiotic substance having the structure ##STR2## can be prepared by cultivation of the microorganism Aerocavin caviae SC 14,030 A.T.C.C. No. 53434.
    Type: Grant
    Filed: February 20, 1987
    Date of Patent: May 17, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Wen-Chih Liu, William L. Parker, Pushpa Singh, Richard B. Sykes
  • Patent number: 4743697
    Abstract: A process is provided for preparing a 7-oxabicycloheptane amino alcohol intermediate of the general structure ##STR1## which is useful in preparing thromboxane A.sub.2 receptor antagonists. This intermediate is prepared by reacting mesonhydride with an aryl amine ##STR2## wherein R is alkyl, CH.sub.2 OH, CO.sub.2 H or CO.sub.2 alkyl, to form the acid ##STR3## which is reduced by treatment with lithium aluminum hydride or diisobutylaluminum hydride or Red-Al to form the alcohol ##STR4## wherein R.sup.1 is CH.sub.2 OH when R is CO.sub.2 H, CO.sub.2 alkyl or CH.sub.2 OH, and R.sup.1 is alkyl when R is alkyl; where in the above alcohol R.sup.1 is CH.sub.2 OH, such alcohol compound is treated with an alkyl chloroformate in the presence of base such as an alkali metal alkoxide to form the alcohol ##STR5## which undergoes cleavage by treatment with alkali metal, ammonia and acid to form the amino alcohol intermediate.Where in the above alcohol R.sup.
    Type: Grant
    Filed: May 21, 1987
    Date of Patent: May 10, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: John K. Thottathil
  • Patent number: 4743685
    Abstract: Antibacterial activity is exhibited by 2-azetidinones having a 3-acylamino substituent and having an activating group in the 1-position of the formula ##STR1##
    Type: Grant
    Filed: September 15, 1986
    Date of Patent: May 10, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Hermann Breuer, Uwe D. Treuner, William H. Koster, Robert Zahler
  • Patent number: 4742067
    Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.
    Type: Grant
    Filed: July 30, 1986
    Date of Patent: May 3, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Sesha I. Natarajan, Eric M. Gordon