The Chalcogen Or The Acyclic Nitrogen Is Bonded Directly To The Six Membered Hetero Ring Patents (Class 546/292)
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Patent number: 6342504Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.Type: GrantFiled: December 21, 1999Date of Patent: January 29, 2002Assignee: Corvas International, Inc.Inventors: Terence Kevin Brunck, Susan Y. Tamura, Joseph Edward Semple, Robert John Ardecky, Yu Ge, William Charles Ripka
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Patent number: 6339045Abstract: N-(substituted or unsubstituted)-4-substituted-6-(substituted or unsubstituted) phenoxy-2-pyridine carboxamide or thiocarboxamide represented by the general formula (I) and a process for producing the compound. A herbicide containing as an effective ingredient N-(substituted or unsubstituted)-4-substituted-6-(substituted or unsubstituted) phenoxy-2-pyridine carboxamide or thiocarboxamide represented by the general formula (I).Type: GrantFiled: August 12, 1998Date of Patent: January 15, 2002Assignee: Kureha Kagaku Kogyo Kabushiki KaishaInventors: Hisashi Kanno, Yoshikazu Kubota, Tsutomu Sato, Koki Sato
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Patent number: 6329360Abstract: The hetero-linked phenylglycinolamides are prepared by reaction of the corresponding hetero-linked phenylacetic acids with appropriate phenylglycinols. The hetero-linked phenylglycinolamides are suitable as active compounds in medicaments.Type: GrantFiled: September 18, 2000Date of Patent: December 11, 2001Assignee: Bayer AktiengesellschaftInventors: Siegfried Goldmann, Ulrich Müller, Richard Connell, Hilmar Bischoff, Dirk Denzer, Rudi Grützmann, Martin Beuck
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Patent number: 6316459Abstract: O-Benzyloxime ethers of the formula I where X is substituted or unsubstituted CH2, NOalkyl Y is O, S, NR5 R1, R2, R5 are H, alkyl Z1, Z2 are H, halogen, methyl, methoxy, cyano R3, R4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl, N(R6)2, where R6 is H, alkyl, substituted or unsubstituted phenyl, —CO—N(R7)2, where R7 is H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted aryloxy, substituted or unsubstituted arylthio, substituted or unsubstituted hetaryl, substituted or unsubstituted hetaryloxy, substituted or unsubstituted hetarylthio, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heterocyType: GrantFiled: October 25, 1994Date of Patent: November 13, 2001Inventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
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Publication number: 20010034357Abstract: The present invention is directed to a series of substituted pyridine compounds, a method for selectively controlling neurotransmitter release in mammals using these compounds, and pharmaceutical compositions containing these compounds. Preferred compounds are 3′-(5′- and/or 6′-substituted) pyridyl ethers.Type: ApplicationFiled: February 2, 2000Publication date: October 25, 2001Inventors: Nan-Horng Lin, Liming Dong
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Aryl- and hetaryl-sulfonamide derivatives, their preparation and their use as endothelin antagonists
Patent number: 6133442Abstract: Compounds of formula I ##STR1## wherein R.sup.1 signifies phenyl, substituted phenyl or heterocyclyl;R.sup.2 signifies phenyl or substituted phenyl;R.sup.3 signifies hydrogen, lower-alkyl, cyano, carboxy, esterified carboxy, phenyl, substituted phenyl, heterocyclyl or a residue --CONR.sup.5 R.sup.6 or --NR.sup.5 COR.sup.7 ;R.sup.4 signifies hydrogen or lower-alkyl;R.sup.5 signifies hydrogen or a residue R.sup.7, andR.sup.6 signifies --(CH.sub.2).sub.m R.sup.7 ; orR.sup.5 and R.sup.6 together with the N atom associated with them signify a heterocyclic residue;R.sup.7 signifies phenyl, substituted phenyl, cycloalkyl, heterocyclyl, lower-alkyl, cyano-lower-alkyl, hydroxy-lower-alkyl, di-lower-alkylamino-lower-alkyl, carboxy-lower-alkyl, lower-alkoxycarbonyl-lower-alkyl, lower-alkoxycarbonylamino-lower-alkyl or phenyl-lower-alkoxycarbonyl;R.sup.a signifies hydrogen, lower-alkyl or hydroxy;R.sup.b signifies hydrogen or lower-alkyl;Z signifies hydroxy, amino or a residue --OR.sup.8, --OC(O)NHR.sup.8, --OC(O)OR.sup.Type: GrantFiled: March 5, 1999Date of Patent: October 17, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael Loffler, Marcel Muller, Werner Neidhart, Henri Ramuz -
Patent number: 6130226Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor .alpha., nuclear factor .kappa.B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.Type: GrantFiled: March 18, 1999Date of Patent: October 10, 2000Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire
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Patent number: 6054470Abstract: This invention relates to compounds of formula (1): ##STR1## wherein Ring a, A, B, C, D, E, R and Q are defined herein. These compounds possess the ability to disrupt the interaction between regulatory proteins possessing one or more SH2 domains and their native ligands.Type: GrantFiled: December 9, 1998Date of Patent: April 25, 2000Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Rajashekhar Betageri, Pierre L. Beaulieu, Jean-Marie Ferland, Montse Llinas-Brunet, Neil Moss, Usha Patel, John R. Proudfoot, Mario Cardozo
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Patent number: 6017937Abstract: A pyridine derivative or a salt thereof expressed by the following formula 1: ##STR1## wherein W represents a group expressed by the following formula 2 or formula 3; ##STR2## wherein R.sub.1 represents an alkenyloxy group; n represents 1 or 2;Ra represents a lower alkyl group; andRb represents a halogen atom; and whereineach of R.sub.2 and R.sub.3 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, or halogenated alkyl group;Y represents a group expressed by --S--, --NH-- or --CONH--;m represents an integer of 0 to 2; andp represents 0 or 1.The pyridine derivative has an anti-ulcer effect or an antibacterial activity against Helicobacter pyroli to be available for prevention or cure of ulcers.Type: GrantFiled: April 7, 1998Date of Patent: January 25, 2000Assignee: Shiseido Co., Ltd.Inventors: Chikao Nishino, Fumitaka Sato, Tomohiro Uetake, Hirotada Fukunishi, Nao Kojima
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Patent number: 6017934Abstract: A compound which inhibits human thrombin and where has the structure ##STR1##Type: GrantFiled: January 20, 1998Date of Patent: January 25, 2000Assignee: Merck & Co., Inc.Inventors: Philip E. Sanderson, Terry A. Lyle, Craig Coburn
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Patent number: 6015905Abstract: A process for preparing 2-(6-substituted pyrid-2-yloxymethyl)phenyacetates especially useful as intermediates for producing agricultural fungicides. The invention provides a compound having the formula (I): wherein A and D are independently selected from the group comprising halo, hydroxy, halo(C.sub.1-4)alkyl, C.sub.1-4 alkoxy, thio(C.sub.1-4)alkoxy, halo(C.sub.1-4)alkoxy, phenyl, phenoxy, nitro, amino, aclyamino, cyano, carboxy, C.sub.1-4 alkoxycarbonyl and C.sub.1-4 alkylcarbonyloxy, or D is C.sub.1-4 alkyl, and m is 0 or an integer of from 1 to 3. The process comprises treating a compound of formula (II): ##STR1## wherein A, D and m are defined as above and M is a metal atom, with a compound of formula (III): ##STR2## wherein L is a leaving group.Type: GrantFiled: December 2, 1997Date of Patent: January 18, 2000Assignee: Zeneca LimitedInventors: David John Ritchie, Gordon Richard Munns, Julie Forrester, Michael Charles Henry Standen, Paul Anthony Worthington, Raymond Vincent Heavon Jones
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Patent number: 5972975Abstract: Substituted 2-aminopyridine compounds of Formula (I) and pharmaceutically acceptable salts which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders.Type: GrantFiled: May 22, 1997Date of Patent: October 26, 1999Assignee: Merck & Co., Inc.Inventors: Craig Esser, William Hagmann, William Hoffman, Shrenik Shah, Kenny Wong, Renee Chabin, Ravindra Guthikonda, Malcolm Maccoss, Charles Caldwell, Philippe Durette
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Patent number: 5959116Abstract: A pyridine-2,3-dicarboxylic acid diester of the formula Va ##STR1## where the radicals R.sup.2 and R.sup.4 have the meanings set out in the specification and where R.sup.8 is a C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.5 -alkenyl or C.sub.3 -C.sub.5 -alkynyl radical, which may be substituted by halogen, phenyl or C.sub.1 -C.sub.4 -alkoxy.Type: GrantFiled: July 12, 1996Date of Patent: September 28, 1999Assignee: BASF AktiengesellschaftInventors: Gerhard Hamprecht, Peter Munster, Matthias Gerber, Helmut Walter, Karl-Otto Westphalen
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Patent number: 5942623Abstract: The invention relates to a process for the preparation of 2-(pyrid-2-yloxymethyl)phenylacetates of formula (I) useful as intermediates for agricultural pesticides, which comprises reacting a 2-pyridine of formula (II), wherein L is a leaving group and A, D and m are as defined in the description with a compound MO--CH.sub.2 R where M is a metal atom and R is the residue of a metal salt of phenylacetic acid. It also includes the compounds MO--CH.sub.2 R, a process for their preparation and a "one-pot" process for the preparation of 2-(pyrid-2-yloxymethyl) phenylacetates from 3-isochromanone.Type: GrantFiled: February 19, 1998Date of Patent: August 24, 1999Assignee: ZENECA LimitedInventors: Alfred Glyn Williams, Gordon Richard Munns, Paul Anthony Worthington
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Patent number: 5919792Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.Type: GrantFiled: October 28, 1997Date of Patent: July 6, 1999Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman, William F. Hoffman, Nathan C. Ihle
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Patent number: 5883282Abstract: There is provided a 3-(3-aryloxyphenyl)-1-(substituted methyl)-s-triazine-2,4,6-oxo or thiotrione compound having the structural formula I ##STR1## Further provided are a composition and a method comprising that compound for the control of undesirable plant species.Type: GrantFiled: May 20, 1997Date of Patent: March 16, 1999Assignee: American Cyanamid CompanyInventors: Alvin Donald Crews, Jr., Philip Mark Harrington, Gary Mitchell Karp, Simon David Gill, Petra Dieterich
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Patent number: 5877297Abstract: Boron compound completing reagents, intermediate reagents of those reagents and methods of synthesizing these reagents. These reagents, including those shown as General Formula CII may be used, after further reactions described herein, to complex with boronic compounds, such as phenylboronic acid or derivatives thereof. ##STR1## In one embodiment, group Z comprises a spacer selected from a saturated or unsaturated chain up to about 0 to 6 carbon equivalents in length, an unbranched saturated or unsaturated chain of from about 6 to 18 carbon equivalents in length with at least one of intermediate amide and disulfide moieties, and a polyethylene glycol chain of from 3 to 12 carbon equivalents in length; group R.sub.2 is one of an alkyl and a methylene with an electronegative moiety; and BAS is a biologically active species.Type: GrantFiled: October 22, 1997Date of Patent: March 2, 1999Assignee: Prolinx, Inc.Inventors: Mark L. Stowolitz, Robert J. Kaiser, Kevin P. Lund
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Patent number: 5872224Abstract: Boron compound complexing reagents, boron compound complexes, and methods of synthesizing these reagents and complexes are disclosed. These reagents and complexes include those shown in General Formula CIV, and General Formula CVI. In one embodiment, the reagent of General Formula CIV may be used to form a complex with a boron compound, such as a complex shown in General Formula CVI. ##STR1## In one embodiment, group Z comprises a spacer selected from a saturated or unsaturated chain of up to about 6 carbon equivalents in length, an unbranched saturated or unsaturated chain of from about 6 to 18 carbon equivalents in length with at least one of intermediate amide and disulfide moieties, and a polyethylene glycol chain of from about 3 to 12 carbon equivalents in length; group R.sub.3 is selected from one of an H, an alkyl, and a methylene or ethylene moiety with an electronegative substituent; and BAS and BAS* are biologically active species.Type: GrantFiled: October 22, 1997Date of Patent: February 16, 1999Assignee: Prolinx, Inc.Inventors: Mark L. Stolowitz, Robert J. Kaiser, Kevin P. Lund
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Patent number: 5869623Abstract: Boron compound complexing reagents, intermediate reagents of those reagents, and methods of synthesizing these reagents are disclosed. These reagents, including those shown as General Formula II may be used, after further reactions described herein, to complex with boronic compounds, such as phenylboronic acid or derivatives thereof. ##STR1## In one embodiment, group Z comprises a spacer selected from a saturated or unsaturated chain of up to about 6 carbon equivalents in length, an unbranched saturated or unsaturated chain from about 6 to 18 carbon equivalents in length with at least one intermediate amide or disulfide moieties, and a polyethylene glycol chain of from about 3 to 12 carbon equivalents in length; group R.sub.2 is one of an alkyl and a methylene group with an electronegative moiety; and BAS is a biologically active species.Type: GrantFiled: October 22, 1997Date of Patent: February 9, 1999Assignees: Systemix, Prolinx, Inc.Inventors: Mark L. Stolowitz, Robert J. Kaiser, Kevin P. Lund, Steven M. Torkelson
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Patent number: 5859210Abstract: Boron compound complexing reagents, boron compound complexes, and methods of synthesizing these reagents and complexes are disclosed. These reagents and complexes include those shown in General Formula IV and General Formula VI. In one embodiment, the reagent of General Formula IV may be used to form a complex with a boron compound, such as a complex shown in General Formula VI. ##STR1## In one embodiment, group Z comprises a spacer selected from a saturated or unsaturated chain of up to about 6 carbon equivalents in length, an unbranched saturated or unsaturated chain of from about 6 to 18 carbon equivalents in length with at least one of intermediate amide or disulfide moieties, and a polyethylene glycol chain of from about 3 to 12 carbon equivalents in length; group R.sub.3 is selected from one of an H, an alkyl, and a methylene or ethylene moiety with an electronegative substituent; and BAS and BAS* are biologically active species.Type: GrantFiled: October 22, 1997Date of Patent: January 12, 1999Assignees: Prolinx, Inc., SystemixInventors: Mark L. Stowolitz, Robert J. Kaiser, Kevin P. Lund, Steven M. Torkelson
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Patent number: 5849361Abstract: Methine dyes of the formula ##STR1## where K is a carbocyclic or heterocyclic radical,X is nitrogen or a radical of the formula C--Q.sup.1, andQ.sup.1, Q.sup.2 and Q.sup.3 are hydrogen, substituted or unsubstituted C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, substituted or unsubstituted phenyl, C.sub.1 -C.sub.6 -alkoxy, benzyloxy, substituted or unsubstituted phenoxy, C.sub.1 -C.sub.6 -alkylthio, halogen, cyano, formylamino or a radical of the formula R.sup.3, --CO--OR.sup.1, --CO--NHR.sup.1, --CO--NH--CO--R.sup.1, --CO--NH--CO--R.sup.3, --CO--NH--SO.sub.2 R.sup.3, --NH--CO--R.sup.1, --NH--CO--OR.sup.1, --NH--CO--NR.sup.1 R.sup.2, NH--CS--OR.sup.1, --NH--CS--NR.sup.1 R.sup.2, --NH--CO--R.sup.3, --NH--SO.sub.2 --R.sup.1, --NH--SO.sub.2 --R.sup.3 or --NH--SO.sub.2 --NR.sup.1 R.sup.2, wherein R.sup.1 and R.sup.2 are substituted or unsubstituted C.sub.1 -C.sub.13 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl or substituted or unsubstituted phenyl, or else --NR.sup.1 R.sup.2 is amino, and R.sup.Type: GrantFiled: June 6, 1997Date of Patent: December 15, 1998Assignee: BASF AktiengesellschaftInventors: Rudiger Sens, Andreas Johann Schmidt, Friedrich-Wilhelm Raulfs, Karl-Heinz Etzbach
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Patent number: 5847192Abstract: Boron compound complexing reagents and methods of synthesizing these reagents are disclosed. These reagents, including those shown as General Formula I and General Formula II may be used, after further reactions described herein, to complex with boronic compounds, such as phenylboronic acid or derivatives thereof.Type: GrantFiled: August 5, 1996Date of Patent: December 8, 1998Assignees: Prolinx, Inc., SystemixInventors: Mark L. Stolowitz, Robert J. Kaiser, Kevin P. Lund, Steven M. Torkelson
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Patent number: 5837878Abstract: Boron compound complexing reagents, boron compound complexes, and methods of synthesizing these reagents and complexes are disclosed. These reagents and complexes include those shown in General Formula CIII, General Formula CIV, and General Formula CVI. In one embodiment, the reagents of General Formula CIII may be used to produce, after condensation with a bioactive species (BAS), the reagent of General Formula CIV. The reagent of General Formula CIV may be used to form a complex with a boron compound, such as a complex shown in General Formula CVI.Type: GrantFiled: August 5, 1996Date of Patent: November 17, 1998Assignee: Prolinx, Inc.Inventors: Mark L. Stolowitz, Robert J. Kaiser, Kevin P. Lund
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Patent number: 5821239Abstract: There are disclosed various substituted 4-amino-3-pyridinol compounds of the formula below, ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification, which are useful for alleviating various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.Type: GrantFiled: February 16, 1996Date of Patent: October 13, 1998Assignee: Frommer Lawrence & Huag LLPInventors: Gregory Micahel Shutske, Kevin James Kapples, John Dick Tomer, Nicholas Joseph Hrib, John Gerard Jurcak
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Patent number: 5811370Abstract: Azamethine dyes of the formula ##STR1## where W is oxygen, sulfur or a radical of the formula --NH--CO--, --NH--COO-- oder --NH--SO.sub.2 --,Z.sup.1 is C.sub.1 -C.sub.4 -alkyl with or without substitution, phenyl or C.sub.1 -C.sub.4 -alkoxy,Z.sup.2 and Z.sup.3 are each hydrogen or C.sub.1 -C.sub.4 -alkyl with or without substitution, provided --CZ.sup.1 Z.sup.2 Z.sup.3 is not linear and is not isopropyl,Z.sup.4 is hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy,Z.sup.5 and Z.sup.6 are each C.sub.1 -C.sub.10 -alkyl with or without substitution, C.sub.3 -C.sub.4 -alkenyl, C.sub.5 -C.sub.7 -cycloalkyl, phenyl or tolyl, or together with the nitrogen atom joining them together a heterocyclic radical or Z.sup.4 and Z.sup.5 are together a bridge member, andT is a radical of a cyclic acidic--CH compound H.sub.2 T,are useful for thermal transfer.Type: GrantFiled: May 8, 1997Date of Patent: September 22, 1998Assignee: BASF AktiengesellschaftInventors: Rudiger Sens, Andreas Johann Schmidt, Stefan Beckmann, Karl-Heinz Etzbach
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Patent number: 5792779Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions and have the following structure: ##STR1## for example: ##STR2##Type: GrantFiled: February 19, 1997Date of Patent: August 11, 1998Assignee: Merck & Co., Inc.Inventors: Philip E. Sanderson, Terry A. Lyle, Joseph P. Vacca, William C. Lumma, Stephen F. Brady, Thomas J. Tucker
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Patent number: 5777148Abstract: Boron compound complexing reagents, intermediate reagents of those reagents and methods of synthesizing these reagents are disclosed. These reagents, including those shown as General Formula I and General Formula II may be used, after further reactions described herein, to complex with boronic compounds, such as phenylboronic acid or derivatives thereof.Type: GrantFiled: August 5, 1996Date of Patent: July 7, 1998Assignee: Prolinx, Inc.Inventors: Mark L. Stowolitz, Robert J. Kaiser, Kevin P. Lund
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Patent number: 5773623Abstract: Methine dyes of the formula ##STR1## where K is a 5- or 6-membered carbocyclic or heterocyclic radical,X is nitrogen or a radical of formula C--Q.sup.1, andQ.sup.1, Q.sup.2 and Q.sup.3 are each independently of the others hydrogen, C.sub.1 -C.sub.6 -alkyl with or without interruption by 1 or 2 oxygen atoms in ether function, benzyl, C.sub.3 -C.sub.8 -cycloalkyl, substituted or unsubstituted phenyl, C.sub.1 -C.sub.4 -fluoroalkyl, C.sub.1 -C.sub.6 -alkoxy, benzyloxy, substituted or unsubstituted phenoxy, C.sub.1 -C.sub.6 -alkylthio, halogen, cyano, formylamino or a radical of the formula R.sup.3, --COR.sup.1, --CO--NHR.sup.1, --CO--NH--CO--R.sup.1, --CO--NH--CO--R.sup.4, --CO--NH--SO.sub.2 R.sup.4, --NH--CO--R.sup.1, --NH--CO--OR.sup.1, --NH--CO--NR.sup.1 R.sup.2, --NH--CSOR.sup.1, --NH--CS--NR.sup.1 R.sup.2, --NH--CO--R.sup.4, --NH--SO.sub.2 --R.sup.1, --NH--SO.sub.2 --R.sup.4 or --NH--SO.sub.2 --NR.sup.1 R.sup.2, where R.sup.1 and R.sup.2 are each independently of the other C.sub.1 -C.sub.Type: GrantFiled: March 29, 1996Date of Patent: June 30, 1998Assignee: BASF AktiengesellschaftInventors: Andreas Johann Schmidt, Rudiger Sens
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Patent number: 5760063Abstract: The subject invention, provides arylhydrazone compounds having the Formula 1: ##STR1## wherein A and B are independently aryl or heteroaryl and A and B independently are substituted with at least one group selected from alkyl, halogen, CN, COOR.sup.7, NR.sup.7 R.sup.8, CONR.sup.7 R.sup.8, NO.sub.2, SR.sup.7, SOR.sup.7, SO.sub.2 R.sup.7, NHCOR.sup.7, NHSO.sub.2 R.sup.7, OR.sup.7, hydroxyalkyl, and aminoalkyl. The compounds of this invention are useful for treating a wide variety of bacterial infections, including diseases of the skin, e.g., acne and skin ulcers, gastroenteritis, colitis, meningitis, keratinitis, conjunctivitis, diseases of the urinary and genital tracts, etc.Type: GrantFiled: September 13, 1996Date of Patent: June 2, 1998Assignee: Scriptgen Pharmaceuticals, Inc.Inventors: Kelvin T. Lam, David G. Powers
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Patent number: 5756524Abstract: A compound of formula I ##STR1## X is O or S; A is 6-alkoxy-3-pyridyl optionally substituted by halogen;Y is hydrogen or alkyl;R.sup.3 is alkyl or a metal salt complex thereof. This invention contains fungicidal compositions and are used to combat cytopathogenic fungi.Type: GrantFiled: September 18, 1996Date of Patent: May 26, 1998Assignee: Agrevo UK LimitedInventors: Peter Dominic Riordan, Susan Elizabeth Osbourn, Ian Kenneth Boddy
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Patent number: 5750547Abstract: The present invention is concerned with novel anticancer agents having potent antineoplastic activity without systemic toxicity and mutagenicity. The novel anticancer agents of the present invention are derivatives of formula I: ##STR1## wherein: A is O or NH; andB is an aryl group selected from the group consisting of phenyl, indane, fluorene, indazole, indole, and pyridine, the aryl group being substituted with at least one substituent selected from the group consisting of hydrogen, C.sub.1-16 alkyl optionally substituted with one or more OH or SH, lower alkoxy, C.sub.3-6 cycloallyl, lower alkylthio, nitro, cyano, lower alkene, lower alkyne, OH, SH, carboxy lower alkyl, carboxy lower alkyl esters, amino, N-lower alkyl, N,N-dilower alkyl and halogen; or a prodrug thereof, with the provisos that when A is NH and B is phenyl:a) B is substituted with at least one substituent other than hydrogen;b) B is not:1) mono-substituted in the 4 position with C.sub.1-2 alkyl, tert-butyl or n-butyl halogen, OH, carboxy C.Type: GrantFiled: June 7, 1996Date of Patent: May 12, 1998Assignee: Universite LavalInventors: Rene C. Gaudreault, Patrick Poyet
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Patent number: 5744627Abstract: Boron compound complexing reagents, boron compound complexes, and methods of synthesizing these reagents and complexes are disclosed. These reagents and complexes include those shown in General Formula III, General Formula IV, and General Formula VI. In one embodiment, the reagents of General Formula III may be used to produce, after condensation with a bioactive species (BAS), the reagent of General Formula IV. The reagent of General Formula IV may be used to form a complex with a boron compound, such as a complex shown in General Formula VI.Type: GrantFiled: August 5, 1996Date of Patent: April 28, 1998Assignees: Prolinx, Inc., SystemixInventors: Mark L. Stowolitz, Robert J. Kaiser, Kevin P. Lund, Steven M. Torkelson
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Patent number: 5726314Abstract: Novel quaternary pyridinium compounds useful in inhibiting acetylcholinesterase in mammals of the general structure: ##STR1## or pharmaceutically acceptable salts thereof, where R.sub.5 is pentafluorophenyl, phenyl monosubstituted with K, phenyl disubstituted with K, phenyl trisubstituted with K, or naphthyl; R.sub.6 is H, C.sub.1-6 alkyl, phenyl, pentafluorophenyl, phenyl mono, di, or trisubstituted with K, C.sub.1-6 alkyl with an attached phenyl group, C.sub.1-6 alkyl with an attached phenyl group mono, di, or trisubstituted with K; K is halogen, COOH, OH, CN, NO.sub.2, NH.sub.2, C.sub.1-6 alkyl, C.sub.1-6 fluorinated alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylamine, C.sub.1-6 alkyl--O--CO--, C.sub.1-6 alkyl--CO--NH--, C.sub.1-6 alkyl--NH--CO--NH--, C.sub.1-6 alkyl--NH--CO--O--, C.sub.1-6 alkyl--NH--CO--, or (C.sub.1-6 alkyl).sub.2 N--CO--; X is OH, C.sub.1-6 alkyl--NH--CO--O--, (C.sub.1-6 alkyl).sub.2 --N--CO--O--, C.sub.1-6 fluoroalkyl--NH--CO--, or (C.sub.1-6 fluoroalkyl).sub.Type: GrantFiled: September 30, 1996Date of Patent: March 10, 1998Assignee: Georgia Tech Research Corp.Inventors: James C. Powers, Jerry J. Buccafusco, Kenneth M. Starks
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Patent number: 5721259Abstract: A method of treatment of tumors is provided based upon a compound of the formula ##STR1## wherein one of R.sup.1 is NHR.sup.4 or NR.sup.4 R.sup.5 or R.sup.3 is NHR.sup.4, NR.sub.4 R.sup.5 or OH, and the other is hydrogen;R.sup.2 is hydrogen or C.sub.1-4 lower alkyl;R.sup.4 is hydrogen, hydroxyl or C.sub.1-4 lower alkyl; andR.sup.5 is C.sub.1-4 lower alkyl; ora pharmaceutically acceptable salt or hydrate thereof.In a further aspect there is provided a method for the treatment of a tumor in a mammal which comprises administration of a compound which is 3- or 5-hydroxy-4-methyl-2-formylpyridine thiosemicarbazone to said mammal.Type: GrantFiled: August 22, 1996Date of Patent: February 24, 1998Assignee: Yale UniversityInventors: Alan C. Sartorelli, Tai-Shun Lin
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Patent number: 5721366Abstract: This invention relates to compounds having the following formula ##STR1## or a pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation, to pharmaceutical compositions of such phenylamidines derivatives, and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.Type: GrantFiled: May 23, 1995Date of Patent: February 24, 1998Assignee: G. D. Searle & CoInventors: Norman Anthony Abood, Daniel Lee Flynn, Robert Bruce Garland, Lori Ann Schretzman, Kenneth Williams, Jeffery Alan Zablocki, Susan Landis Hockerman
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Patent number: 5714615Abstract: Methods for using novel quaternary pyridinium compounds in inhibiting acetylcholinesterase in mammals, specifically using the quaternary pyridinium compounds in the prophylaxis and treatment of organophosphate poisoning and mammalian dementia by mimicking or opposing the actions of the natural neurotransmitter acetylcholine.Type: GrantFiled: February 8, 1994Date of Patent: February 3, 1998Assignee: Georgia Tech Research CorporationInventors: James C. Powers, Jerry J. Buccafusco, Kenneth M. Starks
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Patent number: 5688817Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.Type: GrantFiled: April 28, 1995Date of Patent: November 18, 1997Assignee: Centre Int'l. De Recherches Dermatologiques GaldermaInventors: Jean-Michel Bernardon, William Robert Pilgrim
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Patent number: 5684198Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable esters thereof,which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the aides and pharmaceutical compositions containing them.Type: GrantFiled: August 23, 1996Date of Patent: November 4, 1997Assignee: Imperial Chemical Industries, PLCInventors: Keith Russell, Cyrus John Ohnmacht, Keith Hopkinson Gibson
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Patent number: 5658930Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.Type: GrantFiled: June 7, 1995Date of Patent: August 19, 1997Assignee: Corvas International, Inc.Inventors: Susan Yoshiko Tamura, Joseph Edward Semple, William Charles Ripka, Robert John Ardecky, Yu Ge, Stephen H. Carpenter, Terence K. Brunck
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Patent number: 5656645Abstract: The present invention discloses heterocyclic aromatic peptide aldehydes which have an oxopyrimidine or oxopyridine group and an argininal tail which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.Type: GrantFiled: June 7, 1995Date of Patent: August 12, 1997Assignee: Corvas International, Inc.Inventors: Susan Yoshiko Tamura, Joseph Edward Semple, William Charles Ripka, Robert John Ardecky, Yu Ge, Stephen H. Carpenter, Terence K. Brunck
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Patent number: 5654301Abstract: The present invention relates to compounds of the formula ##STR1##Type: GrantFiled: January 12, 1993Date of Patent: August 5, 1997Assignee: Research Corporation Technologies, Inc.Inventors: Harold L. Kohn, Darrell Watson
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Patent number: 5620996Abstract: The invention relates to sulfonamidocarbonylpyridine-2-carboxesteramides and their pyridine-N-oxides according to the formula I ##STR1## Said compounds are used as pharmaceuticals against fibrotic disorders, as fibrosuppressants and as inhibitors of proline hydroxylase.Type: GrantFiled: March 24, 1995Date of Patent: April 15, 1997Assignee: Hoechst AktiengesellschaftInventors: Klaus Weidmann, Martin Bickel, Volkmar G unzler-Pukall
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Patent number: 5594151Abstract: The present invention relates to a novel class of phenylboronic acid complexing reagents useful for the preparation of bioconjugates, and the method of making and using such reagents. In the present invention, in the place of prior art Avidin-Biotin and Digoxigenin-anti-Digoxigenin systems, phenylboronic acid complexing reagents are utilized in conjunction with phenylboronic acid reagents (many of which are known in the prior art) to facilitate chemical conjugation without the use of intermediary biological macromolecules. Reagents suitable for the modification of a bioactive species for the purpose of incorporating a phenylboronic acid complexing moiety for subsequent conjugation to a different bioactive species having pendant phenylboronic acid moleties are of General Formula I or General Formula II. ##STR1## wherein group X is selected from either H, OH, NH.sub.2, NHCH.sub.3, NHOH and NHOCH.sub.Type: GrantFiled: January 28, 1994Date of Patent: January 14, 1997Assignee: Prolinx, Inc.Inventor: Mark L. Stolowitz
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Patent number: 5565477Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable esters thereof, which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the amides and pharmaceutical compositions containing them.Type: GrantFiled: June 7, 1995Date of Patent: October 15, 1996Assignee: Imperial Chemical Industries PLCInventors: Keith Russell, Cyrus J. Ohnmacht, Keith H. Gibson
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Patent number: 5563159Abstract: There is disclosed a dithiocarbonimide derivative of the formula: ##STR1## wherein B is a C.sub.1 -C.sub.6 alkyl group; X is an NH group or an oxygen atom and Y is a nitrogen atom or a CH group, A is a phenyl group, a heterocyclic group, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkenyl group, a bicycloalkyl group or a tricycloalkyl group, all of which may be substituted. Also disclosed are a fungicidal/insecticidal/acaricidal agent containing the dithiocarbonimide derivative as an active ingredient, an intermediate for use in the production of the dithiocarbonimide derivative, and a process for producing the dithiocarbonimide derivative from the intermediate.Type: GrantFiled: December 2, 1994Date of Patent: October 8, 1996Assignee: Sumitomo Chemical Company, LimitedInventors: Tomoyuki Kusaba, Tadashi Ohsumi, Tsuguhiro Katoh, Makoto Fujimura, Norio Kimura, Kazuya Ujihara, Kimitoshi Umeda
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Patent number: 5547951Abstract: Compounds of the class of pyrido[2,3-b][1,4]benzoxazepin (and thiazepin)-6(5H)-ones and -thiones, having the following general structural formula ##STR1## wherein either X or Z is sulfur and the other substituent is oxygen or both X and Z are sulfur, which are inhibitors of HIV-1 reverse transcriptase and useful in the treatment of HIV-1 infection. An exemplary compound is 2-chloro-5-(methylthioethyl)pyrido[2,3-b][1,4]benzoxazepin-6(5H)one.Type: GrantFiled: August 17, 1994Date of Patent: August 20, 1996Assignee: Boehringer Ingelheim Pharamceuticals, Inc.Inventors: Karl D. Hargrave, Gunther Schmidt, deceased
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Patent number: 5530014Abstract: The cyclohexadiene derivatives are prepared by reaction of cyclohexanones with amines and subsequent dehydration. The compounds are suitable as active compounds in medicaments on account of their property of being selective modulators of calcium channel-dependent potassium channels.Type: GrantFiled: August 18, 1995Date of Patent: June 25, 1996Assignee: Bayer AktiengesellschaftInventors: Klaus Urbahns, Hans-Georg Heine, Bodo Junge, Rudolf Schohe-Loop, Hartmund Wollweber, Henning Sommermeyer, Thomas Glaser, Reilinde Wittka, Jean-Marie-Viktor De Vry
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Patent number: 5521179Abstract: The present invention relates to certain novel heterocyclic amides which are 1-pyridylacetamide compounds of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these heterocyclic amides, processes for preparing the heterocyclic amides, pharmaceutical compositions containing such heterocyclic amides and methods for their use.Type: GrantFiled: April 8, 1993Date of Patent: May 28, 1996Assignee: Zeneca LimitedInventors: Peter R. Bernstein, Andrew Shaw, Royston M. Thomas, Peter Warner, Donald J. Wolanin
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Patent number: 5486529Abstract: The present invention relates to certain novel heterocyclic ketones which are 1-pyridylacetamide ketones of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these heterocyclic ketones, processes for preparing the heterocyclic ketones, pharmaceutical compositions containing such heterocyclic ketones and methods for their use.Type: GrantFiled: April 8, 1993Date of Patent: January 23, 1996Assignee: Zeneca LimitedInventors: Peter R. Bernstein, Andrew Shaw, Royston M. Thomas, Chris A. Veale, Peter Warner, Donald J. Wolanin
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Patent number: RE37087Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I in which R1, R2, R3, R4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.Type: GrantFiled: June 20, 1991Date of Patent: March 6, 2001Assignee: Schering AktiengesellschaftInventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles