Abstract: In a crawling insect trap, an inwardly sloping decline covered with and loosely adhering particulate material, where upon crawling insect when attempting to walk up said decline, causes the loosely adhering particulate material to give way and causing the insect to fall into the interior of the trap.
Abstract: Herein disclosed are 1H-benz[de]isoquinoline-2(3H)-acetic acid derivatives. The derivatives are characterized by being derived from 1,3-dioxo-1H-benz[de]-isoquinoline-2H-acetic acid by replacing one of the oxygen atoms with sulfur and by optional substitution at position 6 with a phenylthio group. The derivatives inhibit lens aldose reductase in a diabetic subject.
Abstract: This invention discloses novel 1-oxo-5H-pyrimido[2,1-c][1,4]benzoxa(or thia)zine-2-carboxylic acid lower alkyl esters, derivatives thereof, process for their preparation, pharmaceutical compositions thereof and methods for using the compounds. The compounds of this invention are useful in the treatment of anaphylactic reactions and allergic conditions in a mammal.
Abstract: Herein disclosed are 6-substituted derivatives of 1,3-dioxo-1H-benz[de]isoquinoline-2(3H)-acetic acid. The derivatives inhibit lens aldose reductase.
Abstract: 3-Oxo-5H-pyrimido[2,1-c][1,4]benzoxazine derivatives, optionally substituted with a hydroxymethyl, carboxy or loweer alkoxycarbonyl at position 1 and optionally substituted at positions 8 or 9, with a lowr alkyl or halo are disclosed. The derivatives are antiallergy agents and methods for their preparation and use are given.
Abstract: The N-substituted dimeric cyclopeptide derivatives of formula ##STR1## in which A is a peptide residue having one to four amino acid residues; R.sup.1 is lower alkyl, phenyl or pheny(lower) alkylene; R.sup.2 is lower alkyl, cyclo(lower)alkyl or lower alkoxycarbonyl(lower)alkylene; R.sup.3 is a neutral amino acid side chain and a method for the preparation of the compounds of formula I are disclosed. The compounds of formula I are useful for treating microbial infections. Pharmaceutical compositions also are disclosed.
Type:
Grant
Filed:
September 11, 1978
Date of Patent:
February 24, 1981
Assignee:
Ayerst McKenna and Harrison Inc.
Inventors:
Amedeo Failli, Hans U. Immer, Manfred K. Gotz
Abstract: The invention concerns novel piperidine derivatives of the formula (I) ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein R.sup.1 represents (lower)alkyl, R.sup.2 represents a phenyl group optionally substituted by one or more (lower)alkyl, (lower)alkoxy, halogen, amino, (lower)alkylamino, di(lower)alkylamino or trifluoromethyl substituents and X represents=O; ##STR2## [where R.sup.3 and R.sup.4 both represent hydrogen, both represent the same (lower)alkyl or one is hydrogen and the other is (lower)alkyl or R.sup.3 and R.sup.4 together represent an alkylene group such that the ##STR3## is a cyclic ketal group containing 2 or 3 carbon atoms]; or ##STR4## [where OR is hydroxy, etherified hydroxy or esterified hydroxy]. The compounds possess anti-depressant activity.
Abstract: The invention relates to the use of thiazoles in the treatment of ulcers and/or hypersecretion in mammals. The invention also provides in a preferred aspect a pharmaceutical composition for use in the treatment of ulcers or hypersecretion comprising a compound of formula I ##STR1## where R.sup.1 is hydrogen, alkyl of 1-6 carbon atoms, or phenyl, R is hydrogen, n-alkyl of 1-4 carbon atoms (which may be substituted by chlorine), or cyclopropyl, R.sup.3 is hydrogen or COR.sup.4 where R.sup.4 is as defined for R and R and R.sup.4 may be the same or different and a pharmaceutically acceptable carrier.
Abstract: Derivatives of 1,3-dihydro-3-(2-hydroxyethyl) -2H-isoindol-1-one are disclosed. The derivatives are useful for treating ulcers in a mammal and for preventing or decreasing the secretion or availability of excessive amounts of gastric or hydrochloric acid in a mammal suffering from hyperchlorhydria and/or associated conditions.
Type:
Grant
Filed:
September 24, 1979
Date of Patent:
January 13, 1981
Assignee:
American Home Products Corporation
Inventors:
Wilbur Lippman, Christopher A. Demerson, Leslie G. Humber, Jean-Marie Ferland
Abstract: Peptides of formula I ##STR1## in which X is (CH.sub.2).sub.2, S--CH.sub.2 or CH.sub.2 --S or a therapeutically acceptable acid addition salt thereof are disclosed. The peptides of formula I are useful as agents for the treatment of acromegaly and the management of diabetes in a mammal. Compositions and methods for the preparation of the peptides of formula I are also disclosed.
Type:
Grant
Filed:
August 13, 1979
Date of Patent:
January 13, 1981
Assignee:
Ayerst McKenna and Harrison Inc.
Inventors:
Nedumparampil A. Abraham, Francesco Bellini, Hans U. Immer, Marvin M. Kobric
Abstract: Derivatives of 4,5-dihydro-4-oxofuran-2-carboxylic acid characterized by having two substituents at position 5 and in addition being optionally further substituted at position 3 with a lower alkyl group, as well as esters therefor are disclosed. The foregoing compounds are useful hypolipidemic agents in a mammal. Novel methods for the preparation of these compounds also are disclosed.
Type:
Grant
Filed:
May 10, 1979
Date of Patent:
January 13, 1981
Assignee:
American Home Products Corporation
Inventors:
Ivo L. Jirkovsky, Dushan Dvornik, Mitchell N. Cayen
Abstract: Novel 4-pyridinamine derivatives having the formula ##STR1## and their pharmaceutically acceptable acid addition salts (wherein A is C.sub.1 to C.sub.4 alkylene, each of B.sub.1 and B.sub.2, together with the two carbon atoms joined thereto, forms arylene or heteroarylene, R.sub.3 and R.sub.4 are independently hydrogen or lower alkyl and n is 0 or 1) are described. They show CNS activity and may be used as anti-depressant drugs.
Abstract: The N-substituted cyclopeptide derivatives of formula I ##STR1## in which R.sup.1 is lower alkyl, R.sup.2 is lower alkyl or cyclo(lower)alkyl, R.sup.3 is a neutral amino acid side chain and Y is a peptide residue having three to nine amino acid residues and a method for the preparation of the compounds of formula I are disclosed. The compounds of formula I are useful antibacterial and antifungal agents. Pharmaceutical compositions also are disclosed.
Type:
Grant
Filed:
September 11, 1978
Date of Patent:
December 2, 1980
Assignee:
American Home Products Corporation
Inventors:
Amedeo Failli, Hans U. Immer, Manfred K. Gotz
Abstract: Indole derivatives characterized by having a 1,2,3,4-tetrahydrocarbazole or 1,2,3,4-tetrahydrocyclopent[b]indole nucleus with a hydroxyalkanamine substituent are disclosed. The nucleus is optionally further substituted at various positions. The derivatives are useful diuretic agents, and methods for their preparation and use are also disclosed.
Type:
Grant
Filed:
August 6, 1979
Date of Patent:
November 25, 1980
Assignee:
American Home Products Corporation
Inventors:
Gervais Dionne, Andre A. Asselin, Leslie G. Humber
Abstract: New 4-aminoquinoline derivatives having the formula ##STR1## wherein X is halogen or trifluoromethyl at the designated 7- or 8-position; Z is hydrogen, halogen, lower alkyl, lower alkoxy, nitro, di(lower alkyl)amino or trifluoromethyl, n is from 1 to 4, R.sup.1 is hydrogen or lower alkyl, R.sup.2 is lower alkyl, R.sup.3 is lower alkyl and A is lower alkylene, and their pharmaceutically acceptable acid addition salts show anti-inflammatory activity.
Abstract: Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano-[3,4-b]indole or 1,3,4,9-tetrahydrothiopyrano[3,4-b]indole nucleus with a hydroxyalkanamine or lower alkoxyalkanamine substituent and a lower alkyl group at position 1 are disclosed. The nucleus is optionally further substituted at position 9 and on the aromatic ring. The derivatives are useful diuretic agents, and methods for their preparation and use are also disclosed.
Type:
Grant
Filed:
May 14, 1979
Date of Patent:
November 25, 1980
Assignee:
American Home Products Corporation
Inventors:
Andre A. Asselin, Leslie G. Humber, Gervais Dionne, Clara Revesz, Amedeo Failli
Abstract: The invention concerns benzoquinolizines of the general formula (I) ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein R.sup.1 and R.sup.2 which may be the same or different, each represent hydrogen, lower alkyl, lower alkoxy or halogen and R represents --CXNHR.sup.3 (where X is O, S or .dbd.NH and R.sup.3 is hydrogen or lower alkyl) or --(CH.sub.2).sub.n R.sup.4 (where n is 0 or 1 and R.sup.4 is aryl). These compounds lower blood pressure. Some are also anti-ulcer agents. The compounds in which R.sup.1, R.sup.2 and R are as defined above, with the proviso that when R is phenyl, R.sup.1 and R.sup.2 are not both lower alkoxy, are novel.
Abstract: Compounds of formula ##STR1## in which X represents oxygen or sulphur;Y represents --CHOH-- or ##STR2## Z represents ##STR3## or a direct bond; R represents cycloalkyl group having 5 to 7 carbon atoms or an optionally substituted aryl or heteroaryl radical, or when --Z-- is a direct bond R also represents hydrogen;R.sup.1 represents hydrogen or lower alkyl.andR.sup.2 represents hydrogen, halogen, lower alkyl or lower alkoxy;ora pharmaceutically acceptable acid addition or quaternary ammonium salt thereof, are disclosed which reduce heart rate or have hyperglycaemic activity.
Abstract: The tripeptide derivatives of formulaH--L--Pro--N(R.sup.1)CH(R.sup.2)CO--Y--R.sup.3 (1)in which R.sup.1 is hydrogen, lower alkyl or NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 each are lower alkyl, R.sup.2 is hydrogen or lower alkyl, R.sup.3 is amino, lower alkylamino, di(lower)alkylamino or amino(lower)alkylamino and Y is one of the amino acid residues Gly or D-Ala with the proviso that when R' is NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are as defined herein and R.sup.2 and Y are as defined herein, R.sup.3 is lower alkylamino, di(lower)alkylamino or amino(lower)alkylamino, .Iadd.and with the further proviso that when R.sup.1 is hydrogen, R.sup.2 is hydrogen or lower alkyl and Y is Gly then R.sup.3 is amino(lower)alkylamino, .Iaddend.and a method for their preparation are disclosed. The tripeptide derivatives of formula 1 possess central nervous system activity and methods for their use are given.
Type:
Grant
Filed:
February 26, 1979
Date of Patent:
January 27, 1981
Assignee:
Ayerst, McKenna & Harrison, Ltd.
Inventors:
Amedeo Failli, Hans U. Immer, Manfred K. Gotz