Abstract: This disclosure describes novel 2,3,6, substituted quinazolinones of the formula: ##STR1## wherein R.sub.1, R.sup.6 and X are described in the specification which have activity as angiotensin II (AII) antagonistis.
Type:
Grant
Filed:
April 23, 1993
Date of Patent:
October 25, 1994
Assignee:
American Cyanamid Company
Inventors:
Jeremy I. Levin, Aranapakam M. Venkatesan
Abstract: The invention provides novel 2,3-substituted pyrazolo[1,5-a]-1,3,5-triazin-4(3H)-ones having the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are described in the specification which have activity as angiotensin II (AII) antagonists.
Abstract: The invention provides compounds having the formula ##STR1## wherein R, X and R.sup.6 are defined in the specification which have activity as angiotensin II antagonists.
Abstract: The invention provides novel 2,3,6-substituted quinazolinones having the formula ##STR1## wherein X, R, R.sup.6 are described in the specification which have activity as angiotensin II (AII) antagonists.
Type:
Grant
Filed:
April 23, 1993
Date of Patent:
March 8, 1994
Assignee:
American Cyanamid Company
Inventors:
Aranapakam M. Venkatesan, Jeremy I. Levin
Abstract: Novel quinazolinone compounds of the formula: ##STR1## wherein R.sup.5, R.sup.6, R.sup.7, R.sup.8, R and X are defined in the specification, which have angiotensin II (AII) antagonizing activity, intermediates useful in the preparation of the compounds, methods of producing and using the compounds to alleviate angiotensin induced hypertension and treat congestive heart failure in mammals.
Abstract: Novel 2, 3, 6 substituted quinazolinones of the formula: ##STR1## wherein R, R.sup.6 and X are described in the specification are disclosed. The compounds which have activity as angiotensin II (AII) antagonists.
Abstract: The invention provides novel 2,3,6 substituted quinazolinones having the formula ##STR1## wherein R, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and X are described in the specification which have activity as angiotensin II (AII) antagonists.
Type:
Grant
Filed:
April 23, 1993
Date of Patent:
February 15, 1994
Assignee:
American Cyanamid Company
Inventors:
Jeremy I. Levin, Aranapakam M. Venkatesan
Abstract: The invention provides novel 2, 3, 6 substituted quinazolinones of the formula ##STR1## wherein, R, R.sup.6 and X are defined in the specification which have activity as angiotensin II (AII) antagonists.
Type:
Grant
Filed:
April 23, 1993
Date of Patent:
February 8, 1994
Assignee:
American Cyanamid Company
Inventors:
Jeremy I. Levin, Aranapakam M. Venkatesan
Abstract: 9-amino-7-(substituted amino)-6-demethyl-6-deoxytetracyclines having activity against a wide spectrum of organisms including organisms which are resistant to tetracyclines are disclosed. Also disclosed are intermediates and methods for making the novel compounds of the present invention.
Type:
Grant
Filed:
October 4, 1991
Date of Patent:
January 25, 1994
Assignee:
American Cyanamid Company
Inventors:
Joseph J. Hlavka, Phaik-Eng Sum, Yakov Gluzman, Ving J. Lee
Abstract: The invention provides novel 2,3,6-substituted quinazolinones having the formula ##STR1## wherein R.sup.6 is ##STR2## and X, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.8 are described in the specification which have activity as angiotensin II (AII) antagonists.
Type:
Grant
Filed:
April 23, 1993
Date of Patent:
January 25, 1994
Assignee:
American Cyanamid Company
Inventors:
Aranapakam M. Venkatesan, Jeremy I. Levin
Abstract: The invention provides novel 2,3,6 substituted quinazolinones of the formula ##STR1## wherein X, R and R.sup.6 are defined in the specification which have activity as angiotensin II (AII) antagonists.
Type:
Grant
Filed:
April 23, 1993
Date of Patent:
January 25, 1994
Assignee:
American Cyanamid Company
Inventors:
Jeremy I. Levin, Aranapakam M. Venkatesan
Abstract: The invention provides novel 2,3,6-substituted 5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4 (3H)-ones of the formula ##STR1## wherein X, R and R.sup.6 are described in the specification which have activity as angiotensin II (AII) antagonists.
Abstract: Pharmaceutical delivery systems containing 7-dimethyl-6-deoxy-6-demethyltetracycline or a non-toxic acid addition salt thereof comprising mixtures of a minor proportion of slow-release blended polymer coated spherical granules adapted to release part of the minocycline in a medium having a pH of below 3.9 and the rest in the range of from about 4.0 to about 7.5 and a major proportion of coated or uncoated quick-release granules adapted to release minocycline in a medium having a pH of less than about 3.9 and oral dosage unit form capsules containing the above are provided. These systems and formulations provide enhanced therapeutic blood levels of minocycline for at least about 24 hours when administered to a subject only once-a-day, regardless of whether the patient is fed or fasted. Methods for the preparation of the systems and formulations are provided as well.
Type:
Grant
Filed:
March 2, 1992
Date of Patent:
November 16, 1993
Assignee:
American Cyanamid Company
Inventors:
Nitin V. Sheth, Joseph J. Valorose, Jr., Keith A. Ellway, Madurai G. Ganesan, Kieran G. Mooney, Jerry B. Johnson
Abstract: The invention relates to a novel method for producing [4S-(4alpha, 12aalpha)]-9-amino-4-(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-3, 10,12,12a-tetrahydroxy-1,11-dioxo-2-naphthacenecarboxamide, hereinafter called 9-amino-6-demethyl-6-deoxytetracycline, which compound is a valuable intermediate for synthesis of tetracyclines.
Abstract: Compounds of the formula: ##STR1## wherein R.sup.1, R.sup.2 and m are defined in the specification are provided. These compounds are useful as antihypertensive agents.
Type:
Grant
Filed:
March 24, 1992
Date of Patent:
July 20, 1993
Assignee:
American Cyanamid Company
Inventors:
Howard Newman, Martin L. Sassiver, Andrew S. Tomcufcik
Abstract: An apparatus for filling finely powdered material into a long and narrow cavity or hole having a relatively small opening is provided. The apparatus features a discharge port for a particulate laden gas stream directed toward the opening of the hole to be filled but spaced apart from the opening of the cavity to be filled by a gap, so that in operation the powdered material continues across the gap and into the cavity due to its inertia while the gas escapes through the gap.
Type:
Grant
Filed:
October 30, 1992
Date of Patent:
June 29, 1993
Assignee:
American Cyanamid Company
Inventors:
Bart J. Zoltan, William F. Boulay, Donald R. Miller
Abstract: The N-phosphorylation of basic nitrogenous drug compounds to produce pro-drugs with enhanced water solubility or lipid solubility, or reduced toxicity, is disclosed. Drugs containing amine, amidine, guanidine, isourea, isothiourea and biguanide functions may be converted to such pro-drugs. The pro-drugs are hydrolyzed in the body, regenerating the original drugs with the release of a salt of phosphoric acid.
Abstract: Phospocholine derivatives having the formula: ##STR1## in which W, Z, Q and R are described in the specification are disclosed as useful for inhibiting the enzyme phospholipase A.sub.2. Methods of making and using the compounds are also disclosed.
Type:
Grant
Filed:
June 3, 1992
Date of Patent:
May 4, 1993
Assignee:
American Cyanamid Company
Inventors:
Allan Wissner, Robert E. Schaub, Kenneth E. Green, Philip R. Hamann
Abstract: Injectable aqueous compositions comprising folic acid and leucovorin and their salts, optionally including benzyl alcohol, sodium chloride and agents for adjusting pH are stabilized and buffered in the range of 6 to 10 by adding a combination of tromethamine and monothioglycerol. Such compositions remain stable for prolonged periods even when exposed to sunlight.
Abstract: New thioester and ester, amide and ketone isostere analogs of oleoyl coenzyme A, useful as antiatherosclerotic agents, are provided. The compounds have the formula: ##STR1## wherein A is selected from the group consisting of ##STR2## Y is selected from the group consisting of --S--, --O--, --NH-- and (--CH.sub.2 --).sub.n wherein n=1 to 4; and Z is selected from the group consisting of alkyl (C.sub.1 -C.sub.6), ##STR3## wherein R=Hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.