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Inventor:
Hester, Jr.; Jackson B.
Address:
Galesburg, MI
No. of patents:
55
Patents:


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Patent Number Title Of Patent Date Issued
7049443 Amide-containing compound having improved solubility and method of improving the solubility of a May 23, 2006
The present invention is directed to novel amide-containing compounds which have an improved solubility and a method of improving the solubility of amide-containing compounds. The amide-containing compounds include oxazolidinone compounds and the bioavailability of these oxazolidinon
6911549 Method of preparing a taxol derivative June 28, 2005
This invention provides 7-deoxy-taxol analogs of Formula I: ##STR1##The compounds of Formula I (including II and III) are useful for the same cancers for which taxol has been shown active, including human ovarian cancer, breast cancer, and malignant melanoma as well as lung cancer, g
6825225 Bicyclic isoxazolinones as antibacterial agents November 30, 2004
The present invention provides compounds of formula I useful as anti microbial agents ##STR1##wherein X, Y, R.sup.1, and n are as defined in thereof.
6642238 Oxazolidinone thioamides with piperazine amide substituents November 4, 2003
The present invention provides a compound of formula I ##STR1##which have potent activities against gram-positive and gram-negative bacteria.
6537986 Oxazolidinone antibacterial agents having a thiocarbonyl funtionality March 25, 2003
The present invention provides compounds of Formula 1 ##STR1##or pharmaceutical acceptable salts thereof wherein A, G and R.sub.1 are as defined in the claims which are antibacterial agents.
6420360 Sultam and sultone derived oxazolidinones July 16, 2002
The present invention provides a compound of formula I ##STR1##These compounds are useful as antibiotic agents.
6387896 Bicyclic oxazolidinones as antibacterial agents May 14, 2002
The present invention provides compounds of formula I useful as antimicrobial agents ##STR1##wherein W, X, Y, R.sup.1, R.sup.2 and n are as defined in thereof.
6362189 Oxazolidinone antibacterial agents having a thiocarbonyl functionality March 26, 2002
The present invention provides compounds of Formula 1 ##STR1##or pharmaceutical acceptable salts thereof wherein A, G and R.sub.1 are as defined in the claims which are antibacterial agents.
6348459 Sultam and sultone derived oxazolidinones February 19, 2002
The present invention provides a compound of formula I ##STR1##These compounds are useful as antibiotic agents.
6342513 Oxazolidinone antibacterial agents having a thiocarbonyl functionality January 29, 2002
The present invention provides compounds of Formula 1: ##STR1##or pharmaceutical acceptable salts thereof wherein A, G and R.sub.1 are as defined in the claims which are antibacterial agents.
6281210 Benzoic acid esters of oxazolidinones having a hydroxyacetylpiperazine substituent August 28, 2001
The present invention provides a compound of formula I ##STR1##which have potent activities against gram positive and gram-negative bacteria.
6255304 Oxazolidinone antibacterial agents having a thiocarbonyl functionality July 3, 2001
The present invention provides compounds of Formula 1 ##STR1##or pharmaceutical acceptable salts thereof wherein A, G and R, are as defined in the claims which are antibacterial agents.
6218413 Oxazolidinone antibacterial agents having a thiocarbonyl functionality April 17, 2001
The present invention provides compounds of Formula 1 ##STR1##or pharmaceutical acceptable salts thereof wherein A, G and R.sub.1 are as defined in the claims which are antibacterial agents.
5998406 Oxazolidinone derivatives and pharmaceutical compositions December 7, 1999
A compound of Formula I: ##STR1## or a pharmaceutically acceptable salt thereof, which is antimicrobial agents, effective against various human and veterinary pathogens, including gram positive aerobic organisms, gram negative organisms, and anaerobic organisms.
5874475 Antiarrhythmic (S)-enantiomers of methanesulfonamides February 23, 1999
Compounds of formula (I) and pharmacologically acceptable salts thereof wherein: n is 1 to 3, R is an alkyl, R.sub.1 is hydrogen or alkyl, R.sub.2 is alkyl, R.sub.3 is an alkyl; b) alkyl substituted with an aryl, heteroaryl or cycloalkyl; c) alkyl substituted with one to eight fluorine
5708169 5-amidomethyl .alpha.,.beta.-saturated and -unsaturated 3-aryl butyrolactone antibacterial agent January 13, 1998
The present invention provides for new 5-amidomethyl, .alpha.,.beta.-saturated and--unsaturated butyrolactone antibacterial agents of formula I ##STR1## characterized by 3-aryl substituents that include, for example, indolinyl and phenyl substituted with zero (0) to two(2) haloge
5668157 Cyanoguanidines as K-channel blockers September 16, 1997
Cyanoguanidine compounds of formula (I) and its pharmaceutically acceptable acid addition salts wherein R.sub.1 is hydrogen or methyl; R.sub.2 is C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.5 cycloalkyl, C.sub.3 -C.sub.5 cycloalkenyl hyd
5643942 Methods, composition and solutions for treating alopecia July 1, 1997
This invention relates to the method for treating the form of alopecia commonly known as "male pattern baldness" which comprises regular topical application to the affected areas of the human scalp of a composition containing as at least one of its active ingredients of Formula I. It als
5633374 Pyrimidine, cyanoguanidines as K-channel blockers May 27, 1997
Pyrimidine-cyanoguanidine compounds of Formula I and its pharmaceutically acceptable acid addition salts ##STR1## wherein R.sub.1 is hydrogen or methyl;R.sub.2 is C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.5 cycloalkyl, C.sub.3 -C.sub.5
5567722 Cyanoguanidines as K-channel blockers October 22, 1996
Cyanoguanidine compounds of Formula I and its pharmaceutically acceptable acid addition salts ##STR1## wherein R.sub.1 is hydrogen or methyl;R.sub.2 is C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.5 cycloalkyl, C.sub.3 -C.sub.5 cycloa
5436337 Amines to sensitize multidrug-resistant cells July 25, 1995
The sensitizing amines of the present invention, illustrated by the steroidal amines (I) ##STR1## the alkyl amines (II), bicyclic amines (III), bicyclic ethers (IV), tricyclic compounds (V), indoles (VI) and various species are useful in treating individuals who have cancer has b
5155268 Antiarrhythmic N-aminoalkylene alkyl and aryl sulfonamides October 13, 1992
The present invention provides novel sulfonanilide and benzene-alkylaminium compounds which are the products of processes utilizing novel intermediates. Both the novel compounds and the novel intermediates are useful for the therapeutic or prophylactic treatment of arrhythmic activit
4902794 Triazolo-benzodiazepines February 20, 1990
1-Substituted-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines of the formula (III): ##STR1## wherein R is selected from the group consisting of hydroxy, esters thereof, and alkoxy, in which the alkyl group is of 1 to 3 carbon atoms, inclusive; wherein R.sub.1 is selected from t
4880781 Renin inhibitory peptides containing an N-alkyl-histidine moiety November 14, 1989
The present invention provides novel renin-inhibiting peptides and novel processes and intermediates for the preparation of both novel and known renin-inhibiting peptide analogs. Such inhibitors are useful for the diagnosis and control of renin-dependent hypertension.
4479959 Process for inducing hypnosis October 30, 1984
Therapeutic compositions for treating humans and animals comprising, in dosage unit form, a 8-Chloro-1-hydroxymethyl-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine compound of the formula ##STR1## including the N-oxides, esters, and pharmacologically acceptable acid additio
4444781 Process for inducing hypnosis April 24, 1984
Therapeutic compositions for treating humans and animals comprising, in dosage unit form, a 8-chloro-1-methanol-6-(o-chlorophenyl)-4H-s-triazolo[4,3-a][1,4]-benzodiaz epine compound of the formula: ##STR1## Including the N-oxides and pharmacologically acceptable acid addition
4415583 Process for inducing hypnosis November 15, 1983
Therapeutic compositions for treating humans and animals comprising, in dosage unit form, a 1-hydroxymethyl-6-(o-chlorophenyl)-4H-s-triazolo[4,3-a][1,4]benzodiazepine compound of the formula: ##STR1## including the N-oxides esters and pharmacologically acceptable acid additio
4296239 Amino-4H-s-triazolo[4,3-a][1,4]benzodiazepines October 20, 1981
6-Amino-4H-s-triazolo[4,3-a][1,4]benzodiazepines of the formula ##STR1## wherein R is hydrogen or C.sub.1 to C.sub.3 -alkyl, R.sub.1 is hydrogen or halogen, and the two R.sub.2 groups are taken together with the nitrogen to which they are bonded to complete a nitrogen ring moiety sel
4264615 Compositions and process April 28, 1981
Pharmaceutical compositions comprising, in unit dosage form, from about 0.5 mg. to about 100 mg. of a compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen, methyl or ethyl, and R.sub.3 is hydrogen, fluorine, chlorine, bromine, --CN, --NO.sub.2, --CF.sub.3, or
4250094 1-(Aminoalkyl) substituted-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines February 10, 1981
1-(Aminoalkyl) substituted-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines of the formula II: ##STR1## wherein R.sub.0 is selected from the group consisting of hydrogen, methyl, or ethyl; wherein R' and R" are selected from the group consisting of hydrogen and alkyl of 1 to
4226772 1-[(Dialkylamino)met hyl]-6-phenyl-4H-s-[4,3,-a][1,4]triazolobenzodiazepine N.sup.1 -oxide October 7, 1980
The compound of the formula ##STR1## wherein R' and R" are alkyl of 1 to 3 carbon atoms, inclusive; wherein R.sub.1 is hydrogen, fluoro, chloro, bromo, nitro, trifluoromethyl or alkylthio in which the alkyl moiety is of 1 to 3 carbon atoms, inclusive; and wherein R.sub.2 is pheny
4141902 1-Halomethyl-6-phenyl-4H-s-[4,3-a][1,4]benzodiazepines February 27, 1979
1-Substituted-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines of the formula II: ##STR1## wherein R.sub.0 is selected from the group consisting of hydrogen, methyl, ethyl, fluorine, chlorine, and bromine, and X is selected from fluorine, chlorine, and bromine; wherein R.sub.1 i
4082761 Triazolo[4,3-a][1,4]benzodiazepinium quaternary salts April 4, 1978
This invention relates to novel benzodiazepinium compounds of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, lower alkyl of 1 through 3 carbon atoms, hydroxy, mercapto, amino, monoalkylamino of 1 through 3 carbon atoms, arylamino wherein the aryl mo
4081452 Novel derivatives of 4H-s-triazolo[4,3-.alpha.][1,4]benzodiazepines March 28, 1978
Compounds of the formula: ##STR1## wherein R'.sub.o and R".sub.o are hydrogen or alkyl of 1 to 3 carbon atoms, inclusive; R.sub.1 is hydrogen, fluoro, chloro, bromo, nitro, trifluoromethyl, or alkylthio in which the alkyl moiety is of 1 to 3 carbon atoms, inclusive; R.sub.2 is ph
4075221 Process for preparing triazolobenzodiazepines February 21, 1978
An improved process for the production of 1-dialkyl-amino-ethyl-6-aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines of the formula II: ##STR1## wherein R.sub.1 is alkyl of 1 to 3 carbon atoms, inclusive; wherein R.sub.2 is hydrogen, methyl or phenyl; wherein the ring A is unsubst
4039551 1-[(Hydroxyamino)methyl]-6-aryl-4H-s-triazolo[4,3-a][1,4]benzodiazepines August 2, 1977
Compounds of the formula ##STR1## wherein R.sub.o is hydrogen or alkyl of 1-3 carbon atoms, inclusive; wherein R.sub.1 is hydrogen, fluoro, chloro, bromo, nitro, trifluoromethyl or alkylthio in which the alkyl moiety is of 1 to 3 carbon atoms, inclusive; and wherein R.sub.2 is ph
4021441 1-[(Allylamino)-methyl]-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines May 3, 1977
Compounds of the formula II: ##STR1## wherein R is cyclopropyl, cyclopropylmethyl, or allyl; wherein R', R", and R.sub.1 are hydrogen or alkyl of 1 to 3 carbon atoms inclusive; and wherein R.sub.2, R.sub.3, and R.sub.4 are hydrogen, alkyl as defined above, fluoro, chloro, bromo,
4018788 6-(O-Halophenyl)-1-methyl-4H-s-triazolo[4,3-a][1,4]-benzodiazepine April 19, 1977
6-(o-halophenyl)-1-methyl-4H-s-triazolo[4,3-a][1,4]-benzodiazepines of the following formula: ##STR1## wherein the substituent "Hal" is either of the halogens having an atomic number up to 35, inclusive, i.e., fluoro, chloro or bromo, and their pharmacologically acceptable acid a
4012413 Organic compounds and process March 15, 1977
Compounds of the formula: ##STR1## wherein R is hydrogen, methyl, or ethyl; wherein R' and R" are hydrogen, alkyl of 1 to 3 carbon atoms, inclusive, wherein R.sub.1 is hydrogen or methyl defined as above; wherein R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are selected from the group
4009175 1-[(Aminooxy)-methyl]-6-substituted-4H-s-triazolo[4,3-a][1,4] benzodiazepines February 22, 1977
Compounds of the formula: ##STR1## wherein R'o and R"o are hydrogen or alkyl of 1 to 3 carbon atoms, inclusive; R.sub.1 is hydrogen, fluoro, chloro, bromo, nitro, trifluoromethyl, or alkylthio in which the alkyl moiety is of 1 to 3 carbon atoms, inclusive; R.sub.2 is phenyl, o-ch
4000153 Triazolobenzodiazepine intermediates December 28, 1976
Intermediates of the formula VI: ##STR1## wherein R is hydrogen or alkyl of 1 to 3 carbon atoms, inclusive, wherein R.sub.2 is hydrogen, fluoro, or chloro; wherein R.sub.3 is hydrogen or fluoro with the proviso that R.sub.3 is not fluoro, if R.sub.2 is chloro; wherein R.sub.4 is
4000151 Triazolyl benzophenone compounds December 28, 1976
Intermediates of the formula IV: ##STR1## wherein R is selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms, inclusive; and wherein R.sub.2, R.sub.3, and R.sub.4 are selected from the group consisting of hydrogen, fluoro, chloro, bromo, nitro, and trifl
3996230 1-Piperazino-6-(2-pyridyl)-4H-s-triazolo[4,3-a][1,4]benzodiazepines December 7, 1976
1-Piperazino-6-(2-pyridyl)-4H-s-triazolo[4,3-a][1,4]benzodiazepines of the formula II: ##SPC1##wherein R is hydrogen, alkyl of 1 to 3 carbon atoms, inclusive, or .beta.-hydroxyethyl; wherein R.sub.1 is hydrogen or alkyl defined as above; and wherein R.sub.2 and R.sub.3 are hydrogen,
3995043 Composition and process November 30, 1976
Pharmaceutical compositions comprising, in unit dosage form, from about 0.5 mg. to about 100 mg. of a compound of the formula ##SPC1##Wherein R and R' are hydrogen, methyl or ethyl, R.sub.1 is hydrogen or lower alkyl of 1 through 3 carbon atoms, R.sub.2 is hydrogen, lower alkyl of 1
3994941 Preparation of 1-(2-phthalimidoethyl)-4H-s-tiazolo[4,3-a][1,4]benzodiazepines November 30, 1976
A process for the production of compounds of the formula III: ##SPC1##wherein ring A is unsubstituted or substituted by fluoro, chloro, bromo, trifluoromethyl, or nitro, and wherein Ar is phenyl, o-chlorophenyl, o-fluorophenyl, or 2-pyridyl, is claimed in which the starting compound is
3994940 Preparation of 1-(2-(dimethylamino)ethyl)-6-phenyl-4H-5-triazolo(4,3-a)(1,4)benzodiazep ines November 30, 1976
A process for the production of known compounds of the formula IV ##SPC1##wherein R.sub.1 is hydrogen or alkyl of 1 to 3 carbon atoms, inclusive; wherein R.sub.2 is hydrogen, chloro, or fluoro; wherein R.sub.3 is hydrogen, or fluoro with the proviso that R.sub.3 is not fluoro if R.sub.2
3993660 2-[3-(Phthalimidomethyl)-5-methyl-4H-1,2,4-triazol-4-yl]benzophenones November 23, 1976
A process to make 6-phenyl-4H-s-triazolo[4,3-a][1,4]-benzodiazepines by converting 2-[3-(hydroxymethyl)-4H-1,2,4-triazol-4-yl]benzophenones to 2-[3-[(phthalimido or methanesulfonyl)methyl]-4H-1,2,4-triazol-4-yl]benzophenones and converting these compounds to the highly active 6-p
3991070 Process for preparing halo triazolo benzodiazepine November 9, 1976
Preparing 1-halo-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines by reacting an N-halosuccinimide with a 2-[3-(phthalimidomethyl)triazolyl]benzophenone to form the 2-[5-halo-3-(phthalimidomethyl)triazolyl] benzophenone and reacting the 2-[5-halo-3-(phthalimidomethyl)triazol-4-yl]be
3980790 8-Chloro-1-methyl-6-(O-chlo rophenyl)-4H-s-triazolo[4,3-a]-[1,4]benzodiazepine compositions and September 14, 1976
Therapeutic compositions for treating humans and animals comprising, in dosage unit form, a 8-chloro-1-methyl-6-(o-chlorophenyl)-4H-s-triazolo[4,3-a][1,4]benzodiazepi ne compound of the formula ##SPC1##Including the N-oxides and pharmacologically acceptable acid addition salts the
3980789 8-Chloro-1-methyl-6-phenyl-4H-s-triazolo[4,3-a][1,4]-benzodiazepine compositions and method of t September 14, 1976
Therapeutic compositions for treating humans and animals comprising, in dosage unit form, a 8-Chloro-1-methyl-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine compound of the formula ##SPC1##Including the N-oxides and pharmacologically acceptable acid addition salts thereof in co
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