Patents Represented by Attorney Merle J. Smith

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  • Substituted pyrano[4,3-d]-thiazolo[3,2-a]pyrimidines
    Patent number: 4128648
    Abstract: 2,3,8,9-Tetrahydro-5H,6H-pyrano[4,3-d]thiazolo[3,2-a]pyrimidines of the structure ##STR1## are provided wherein R.sup.1 and R.sup.2 may be the same or different and are hydrogen, lower alkyl, halogen, cyano, carbethoxy, carboxyl, trifluoromethyl or lower alkoxy, and n is 2 or 3, and m is 0 to 2. These compounds are useful in the treatment of auto-immune disorders, such as rheumatoid arthritis.
    Type: Grant
    Filed: March 24, 1978
    Date of Patent: December 5, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: George C. Rovnyak
  • 4-Halo derivatives of pyrazolo[1,5-a]-quinoxaline-3-carboxylic acids and esters
    Patent number: 4128716
    Abstract: New 4-halo derivatives of pyrazolo[1,5-a]quinoxaline-3-carboxylic acid, esters and their salts have the formula ##STR1## R.sub.1 is hydrogen, lower alkyl or a salt forming ion; R.sub.2 is hydrogen, lower alkyl, halogen or lower alkoxy; and X is halogen.The new compounds are useful as intermediates and as anti-inflammatory agents.
    Type: Grant
    Filed: September 13, 1977
    Date of Patent: December 5, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Uwe D. Treuner
  • Hydrazinocarbonylamino cephalosporins
    Patent number: 4128724
    Abstract: New .alpha.-hydrazinocarbonylamino cephalosporins which have the formula ##STR1## are useful as antimicrobial agents.
    Type: Grant
    Filed: January 12, 1978
    Date of Patent: December 5, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Hermann Breuer, Uwe D. Treuner
  • Amino acid derivatives
    Patent number: 4128721
    Abstract: New derivatives of amino acids which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.
    Type: Grant
    Filed: February 21, 1978
    Date of Patent: December 5, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Miguel A. Ondetti
  • Derivatives of 5,6-dihydrobenzo[5,6]cyclohepta[1,2-B]pyrazolo-[4,3-E]pyridin-11 (1H)-ones and 11 (1H)-imines
    Patent number: 4128717
    Abstract: New derivatives of 5,6-dihydrobenzo[5,6]cyclohepta-[1,2-b]pyrazolo[4,3-e]pyridin-11 (1H)-ones and imines, respectively, have the general formula ##STR1## They and the salts thereof are useful as psychotropic and antiinflammatory agents.
    Type: Grant
    Filed: July 20, 1977
    Date of Patent: December 5, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Hans Hoehn, Jack Bernstein, B. Richard Vogt
  • Reduction of blood pressure with carboxyalkylacyl-pipecolic acid derivatives
    Patent number: 4128653
    Abstract: New carboxyalkylacylamino acids which are derivatives of proline, pipecolic acid and azetidine-2-carboxylic acid and have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.
    Type: Grant
    Filed: February 11, 1977
    Date of Patent: December 5, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: David W. Cushman, Miguel A. Ondetti
  • 4H-pyrazolo[1,5-a]pyrazolo[4',3':5,6]pyrido[3,4-e]pyrimidin-5(8H)one and derivatives thereof
    Patent number: 4128645
    Abstract: New 4H-pyrazolo[1,5-a]pyrazolo[4',3':5,6]pyrido[3,4-e]pyrimidin-5(8H)one and new derivatives thereof have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.
    Type: Grant
    Filed: September 1, 1977
    Date of Patent: December 5, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Theodor Denzel, Hans Hoehn
  • Substituted thiazolo [3,2-a]-thiopyrano[4,3-d]pyrimidines
    Patent number: 4128647
    Abstract: 2,3,8,9-Tetrahydro-5H,6H-thiazolo[3,2-a]thiopyrano[4,3-d]pyrimidines of the structure ##STR1## are provided wherein R is hydrogen, lower alkyl, halogen, acyl, cyano, carboxyl, trifluoromethyl or lower alkoxy, n is 0 or 2 and m is 2 or 3. These compounds are useful in the treatment of auto-immune disorders, such as rheumatoid arthritis.
    Type: Grant
    Filed: March 24, 1978
    Date of Patent: December 5, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: George C. Rovnyak
  • Pyrazolo(1,5-c)quinazoline derivatives and related compounds
    Patent number: 4128644
    Abstract: Compounds are provided having the structure ##STR1## wherein R.sup.1 is hydrogen, alkyl of 1-3 carbons, phenyl optionally substituted by R.sup.4 ; R.sup.2 is cyano; ##STR2## (wherein Z is a single bond or ##STR3## X is O or S); ##STR4## (wherein R.sup.9 is hydrogen or alkyl, Q is CH or N); ##STR5## wherein R.sup.6 is amino, alkylamino, dialkylamino, haloalkyl or ##STR6## and R.sup.4 and R.sup.5 are the same or different and represent hydrogen, lower alkyl, lower alkoxy, alkanoyloxy, benzyloxy, substituted benzyloxy, hydroxy, halogen (Cl, Br and F), nitro and trifluoromethyl; and R.sup.7, R.sup.8, m and n are defined hereinafter.
    Type: Grant
    Filed: July 29, 1977
    Date of Patent: December 5, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: B. Richard Vogt
  • Method for treating blackhead disease
    Patent number: 4127664
    Abstract: A method is provided for treating or preventing blackhead disease in birds by administering to birds, especially to poultry, such as turkeys, benzimidazoles having the structure ##STR1## wherein R.sup.1 is lower alkyl or phenyl-lower alkyl, and R.sup.2 is lower alkyl, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, phenyl, benzyl and phenylethyl dispersed in a non-toxic physiologically acceptable carrier.
    Type: Grant
    Filed: November 11, 1977
    Date of Patent: November 28, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Rudiger D. Haugwitz, Larry R. Cruthers
  • Substituted thiopyrano(4,3-b)pyrans
    Patent number: 4127667
    Abstract: 3,4,7,8-Tetahydro-2H,5H-thiopyrano[4,3-b]pyrans of the structure ##STR1## are provided wherein X is O, S or SO.sub.2, R is hydrogen, halogen, lower alkyl, lower alkoxy, cyano or trifluoromethyl, and R' is carbethoxy, carboxy, alkali metal carboxylate and cyano. These compounds are useful as antiinflammatory agents and anti-hypertensive agents.
    Type: Grant
    Filed: April 5, 1978
    Date of Patent: November 28, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: George C. Rovnyak
  • 4H-pyrazolo[1,5-a]pyrazolo[4',3':5,6]pyrido[3,4-e]pyrimidin-5(8H)one and derivatives thereof
    Patent number: 4127657
    Abstract: New 4H-pyrazolo[1,5-a]pyrazolo[4',4':5,6]pyrido[3,4-e]pyrimidin-5(8H)one and new derivatives thereof have the general formula ##STR1## The compounds are useful as anti-inflammatory agents and central nervous system depressants.
    Type: Grant
    Filed: September 1, 1977
    Date of Patent: November 28, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Theodor Denzel, Hans Hoehn
  • Effervescent tablet and method
    Patent number: 4127645
    Abstract: An effervescent tablet, preferably in the form of a pressed tablet, useful in inhibiting or reducing dental plaque is provided, the tablet including a core portion containing an effervescent couple, and an outer portion which coats or surrounds the core portion, the outer portion containing a sugar alcohol, such as sorbitol. The effervescent tablet will preferably include a source of calcium ion to fortify teeth against demineralization. In addition, a method of inhibiting or reducing dental caries by use of the above described tablet as well as a method for protecting an effervescent couple from moisture absorption are also provided.
    Type: Grant
    Filed: June 13, 1977
    Date of Patent: November 28, 1978
    Assignee: Life Savers, Inc.
    Inventors: Frank Witzel, K. Warren Clark
  • Benzo-cyclitolamines
    Patent number: 4127717
    Abstract: Compounds having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein n is 1 or 2; m is 2, 3 or 4; R.sub.1 is alkanoyl; and R.sub.2 is a tertiary amino group; have hypotensive activity.
    Type: Grant
    Filed: March 20, 1978
    Date of Patent: November 28, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Frederic P. Hauck, Joyce Reid
  • Substituted piperidinylpropanols
    Patent number: 4127579
    Abstract: Compounds having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein n is 0, 1 or 2; R.sub.1 is alkanoyl; and R.sub.2 is ##STR2## R.sub.3 is alkyl; R.sub.4 is cyano or hydroxy; R.sub.5 is hydroxy or alkanoyloxy; R.sub.6 is hydrogen or alkanoyl; and m is 2, 3 or 4; have useful hypotensive properties.
    Type: Grant
    Filed: November 25, 1977
    Date of Patent: November 28, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Frederic P. Hauck, Rita T. Fox, John R. Watrous
  • Triazolylbenzophenones
    Patent number: 4127587
    Abstract: Triazoloisoindoles are provided having the structure ##STR1## wherein X, Y and R are as defined hereinafter. These compounds have antiinflammatory activity and anthelmintic activity. Pharmaceutical compositions containing such compounds and methods for using such compounds are also provided.
    Type: Grant
    Filed: January 12, 1978
    Date of Patent: November 28, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Peter C. Wade, Thomas P. Kissick
  • Diene intermediates for indantetrols
    Patent number: 4127578
    Abstract: Diene intermediates for indantetrols are provided having the structure ##STR1## wherein X is a single bond or a straight or branched chain alkylene group containing from 1 to 10 carbons, Y is ##STR2## wherein R.sub.7 is hydrogen, lower alkyl, arylalkyl or lower alkoxy and ##STR3## is taken together to form a piperidyl or pyrrolidyl radical, R.sub.8 and R'.sub.8 are lower alkyl or monocyclic cycloalkyl, n is 1 to 3, m and m' are 0, 1 or 2.
    Type: Grant
    Filed: September 12, 1977
    Date of Patent: November 28, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Frederic P. Hauck, Joyce Reid, Venkatachala L. Narayanan, Christopher M. Cimarusti, Rudiger D. Haugwitz, Joseph E. Sundeen
  • 4,5-Seco-steroids
    Patent number: 4127589
    Abstract: Novel 4,5-seco-steroids having anti-inflammatory activity are disclosed herein.
    Type: Grant
    Filed: February 6, 1975
    Date of Patent: November 28, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Christopher M. Cimarusti, Seymour D. Levine
  • Various 1,5,10,11-tetrahydrobenzo[4,5]cyclohepta[1,2-B]pyrazolo-[4,3-E]pyridine derivatives
    Patent number: 4127715
    Abstract: Compounds of the formulas ##STR1## wherein R.sub.1 is lower alkyl, phenyl, benzyl or phenethyl; R.sub.2 is hydrogen, lower alkyl or phenyl; ##STR2## N IS AN INTEGER FROM 3 TO 6; R.sub.3 and R.sub.4 are each lower alkyl or R.sub.3 and R.sub.4 taken together with the N-atom form a heterocyclic ring of the formula ##STR3## wherein R.sub.5 is hydrogen, lower alkyl, or lower alkoxy; and pharmaceutically acceptable acid addition salts thereof are disclosed. These compounds and their salts possess central nervous system activity and are useful as anti-anxiety agents.
    Type: Grant
    Filed: February 27, 1978
    Date of Patent: November 28, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Hans Hoehn, Jack Bernstein, Berthold R. Vogt
  • 3-HETEROTHIOMETHYL UREIDO CEPHALOSPORINS
    Patent number: 4127716
    Abstract: L-Isomer compounds of the formula ##STR1## wherein R.sub.1 is phenyl, thienyl or furyl; R.sub.4 represents certain heterocyclic groups; R.sub.3 is hydrogen, lower alkyl, phenyl-lower alkyl, substituted phenyl-lower alkyl, diphenyl-lower alkyl, tri(lower alkyl)stannyl, tri(lower alkyl)silyl, a salt forming ion, or the group ##STR2## wherein R is lower alkyl, phenyl, phenyl-lower alkyl, or substituted phenyl and phenyl-lower alkyl are disclosed. These compounds are useful as antibacterial agents.
    Type: Grant
    Filed: February 2, 1977
    Date of Patent: November 28, 1978
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Hermann Breuer, Uwe D. Treuner