Publication number: 20080188456
Abstract: A method for repelling arthropods involving treating an object or area with an arthropod repelling effective amount of at least one compound having the formula wherein X is O, S, NH, N-NH2, N-CH3 or CH2, R? is H or alkyl, R? is alkyl, n is 0, 1, 2, 3 or 4, and mixtures thereof, optionally including a carrier material or canier. The compound is preferably selected from homopiperazine, 1-methylhomopiperazine, 1-methylpyrrolidine, (R)-(?)-2-methylpiperazine, (S)-(+)-2-methylpiperazine, 2-methylpiperazine, 1-methylpiperazine, pyrrolidine, 1-methylpiperidine, piperidine, 1-ethylpiperazine, 1-methylimidazolidine, 1-methylthiomorpholine, 1,4-dimethylpiperazine, homopiperidine, imidazolidine, 4-methylpiperidine, thiomorpholine, 1-amino-4-methylpiperazine, 4-methylmorpholine, azocane, 2,6-dimethylpiperazine, 2,5-dimethylpiperazine, piperazine, 1-methlyhomopiperidine, or mixtures thereof.
Type:
Application
Filed:
December 10, 2007
Publication date:
August 7, 2008
Inventors:
Ulrich R. Bernier, Kenneth Posey, Daniel L. Kline, Donald Barnard, Kamal Chauhan
Patent number: 7030138
Abstract: A compound of a formula (1) and pharmacologically acceptable salts thereof: wherein R1 represents hydrogen, halogen, alkyl or hydroxyl; R2 represents hydrogen or halogen; R3 represents hydrogen, alkyl, hydroxyl, carboxyalkyl, alkoxycarbonylalkyl, alkylsulfonyl, alkoxycarbonylalkylsulfonyl, craboxyalkylsulfonyl or carboxyalkylcarbonyl; each of R4 and R5 represents hydrogen, halogen, alkyl, carbamoyl, alkoxy, carboxyl, alkoxycarbonyl, monoalkylcarbamoyl or dialkylcarbamoyl; R6 represents a heterocycle, hydrogen, alkyl, cycloalkyl, aralkyl, carboxyalkyl, alkoxycarbonyalkyl, aliphatic or aromatic acyl, carbamoyl, alkylsulfonyl, aryl, formimidoyl, 1-iminoalkyl, N-alkylforminidoyl or iminoarylmethyl; each of R7 and R8 represents hydrogen or alkyl; n represents 0, 1 or 2. The compound exhibits excellent activated blood coagulation factor X inhibitory activity and prevents or treats blood coagulation-related diseases.
Type:
Grant
Filed:
October 3, 2003
Date of Patent:
April 18, 2006
Assignee:
Sankyo Company, Limited
Inventors:
Koichi Fujimoto, Naoki Tanaka, Ikuko Shimada, Fumitoshi Asai
Patent number: 6890920
Abstract: Novel quaternary ammonium compounds of the formula and any stereoisomers thereof, wherein R1, R2 and R3 independently represent C1-C6 alkyl, optionally substituted with phenyl or hydroxyl, or both, and wherein any two of R1, R2 and R3 may form a ring together with the quaternary ammonium nitrogen; R4 represents —H, —CH3, or —CO—R4-1, wherein R4-1 represents —(C1-C4 alkyl), —(C1-C4 alkoxy), or —NR4-2R4-3, wherein R4-2 and R4-3 independently represent —H or —(C1-C4 alkyl); R5, R6 and R7 independently represent —H, —OCH3, —OH, —CONH2, —SO2NH2, —F, —Cl, —Br, —I, —CF3, or —(C1-C4 alkyl), optionally substituted with one or two —OH, —(C1-C4 alkoxy), —COOH, or —CO—O—(C1-C3 alkyl); and X? represents an anion of a pharmaceutically acceptable acid, the compounds for use as medicaments, use of the compounds for the manufacture of specific medicaments, and pharmaceutical compositions comprising the compounds. The present invention also concerns a method of treatment involving administration of the compounds.
Type:
Grant
Filed:
October 25, 2002
Date of Patent:
May 10, 2005
Assignee:
Pharmacia & Upjohn Company
Inventors:
Ivan Richards, Sue K. Cammarata, Craig D. Wegner, Michael Hawley, Mark Peter Warchol, Mark Kontny, Walter Morozowich, Karen Patrice Kolbasa, Malcolm Wilson Moon, Dominique Bonafoux, Sergey Gregory Wolfson, Patrick James Lennon
Patent number: 6767907
Abstract: 4-Aryl-1-(indanmethyl, dihydrobenzofuranmethyl or dihydrobenzothiophenemethyl)piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I), wherein one of X and Y is CH2 and the other one is CH2, O or S; Z is N, C, CH or COH; Ar is an optionally substituted aryl group; R1 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, acyl, thioacyl, alkylsulfonyl, trifluoromethylsulfonyl, arylsulfonyl, a group R9VCO— where V is O or S and R9 is alkyl or aryl, or a group R10R11NCO— or R10R11NCS— wherein R10 and R11 are hydrogen, alkyl or aryl, or R10 and R11 are linked to form a ring; R2 is hydrogen, alkyl, cykcloalkyl or cycloalkylalkyl; or R1 and R2 are linked to form a ring; R3-R5 are hydrogen, halogen, alkyl, alkylcarbonyl, phenylcarbonyl, alkoxy, alkylthio, hydroxy, alkylsulfonyl, cyano, trifluoromethyl, cycloalkyl, cycloalkylalkyl or nitro; R6 and R7 are hydrogen or alkyl or they are linked to constitute 3-7 membered ring; R8 is hydrogen or alkyl; have effects at c
Type:
Grant
Filed:
April 14, 2000
Date of Patent:
July 27, 2004
Assignee:
H. Lundbeck A/S
Inventors:
Jens Kristian Perregaard, John Willie Stenberg, Bitten Hansen
Patent number: 6753327
Abstract: An amide of the formula I
and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings:
A —(CH2)p—R1, where R1 can be pyrrolidine, morpholine, piperidine, —NR5R6 and
and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and
B can be phenyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by up to 2 R8 radicals, and
D can be a bond, —(CH2)m, —CH═CH—, —C≡C—, and
Y is phenyl, pyridine, pyrimidine and pyrazine and
n is a number 0, 1 or 2, and
m,q are, independently of one another, a number 0, 1, 2, 3 or 4.
Type:
Grant
Filed:
October 11, 2000
Date of Patent:
June 22, 2004
Assignee:
Abbott GmbH & Co. KG
Inventors:
Wilfried Lubisch, Achim Möller, Hans-Jörg Treiber, Monika Knopp