Phosphorus Attached Directly Or Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 540/542)
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Publication number: 20030008849Abstract: Compounds of the formula: 1Type: ApplicationFiled: December 27, 2000Publication date: January 9, 2003Inventors: Jeremy I. Levin, James M. Chen, Derek C. Cole, Mila T. Du, Leif M. Laakso
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Patent number: 6503898Abstract: This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors, to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating viral infection. A representative compound of the invention is the compound of formula: wherein R22 and R23 are allyl.Type: GrantFiled: July 10, 1998Date of Patent: January 7, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Patrick Yuk-Sun Lam, Prabhakar Kondaji Jadhav, Charles Joseph Eyermann, Carl Nicholas Hodge, George Vincent De Lucca, James David Rodgers
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Publication number: 20020198178Abstract: Pyrrolidine compounds of Formula I: 1Type: ApplicationFiled: October 10, 2001Publication date: December 26, 2002Inventors: Christopher A. Willoughby, Keith Rosauer, Kevin T. Chapman, Sander G. Mills, Dong-Ming Shen, Min Shu
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Publication number: 20020177706Abstract: Novel cyclo azaphospha hydrocarbons according to formula I 1Type: ApplicationFiled: April 11, 2002Publication date: November 28, 2002Inventors: Thomas Hoyer, Morten Dahl Sorensen
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Patent number: 6458783Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formulas their enantiomers, diastereomers, and pharmaceutically acceptable salts, prodrugs and solvates thereof.Type: GrantFiled: April 21, 2000Date of Patent: October 1, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Charles Z. Ding, John T. Hunt, Katerina Leftheris, Rajeev S. Bhide
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Patent number: 6399598Abstract: The invention provides compounds of formula as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptacle salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases. Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.Type: GrantFiled: March 1, 2000Date of Patent: June 4, 2002Assignee: The Procter & Gamble CompanyInventors: Stanislaw Pikul, Neil Gregory Almstead, Rimma Sandler Bradley, Kelly Lynn McDow-Dunham, Biswanath De, Michael George Natchus, Yetunde Olabisi Taiwo, Thomas Lee Cupps
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Publication number: 20020052364Abstract: Compounds of formula I are described, their production and use in pharmaceutical agents.Type: ApplicationFiled: November 27, 2001Publication date: May 2, 2002Inventors: Ernese Csuzdi, Tamas Hamori, Gizella Abraham, Sandor Solyom, Istvan Tarnawa, Pal Berzsenyl, Ferenc Andrasi, lstvan Ling, Antal Simay, Melinda Gal, Katalin Horvath, Eszter Szentkuti, Marta Szollosy, Istvan Pallagi
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Patent number: 6358976Abstract: This invention relates to novel fused heterocycles which are useful as antagonists of the &agr;v&bgr;3 and related integrin receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.Type: GrantFiled: February 22, 2000Date of Patent: March 19, 2002Inventors: John Wityak, Aleksandra Ewa Tobin
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Publication number: 20010056088Abstract: Hydroxamic acids having the formula 1Type: ApplicationFiled: June 14, 2001Publication date: December 27, 2001Applicant: American Cyanamid CompanyInventors: Jeremy I. Levin, James M. Chen
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Patent number: 6172050Abstract: Phospholipid derivatives of Formula X: wherein A is the ring system in which R is a linear or branched alkyl radical having 10 to 24 carbon atoms which may contain one or more double or triple bonds; R1 and R2 are independently hydrogen or linear alkyl radicals having 1 to 3 carbon atoms; y is 0, 1, 2 or 3; m and n are independently 0 or in an integer, with the proviso that m+n is between 2 and 8; or A is a tropanio or quinuclidinio ring system, which is linked via a carbon-carbon bond and is optionally substituted by one or more methyl groups; processes for the preparation of the derivatives, and methods for treating tumors therewith.Type: GrantFiled: August 4, 1997Date of Patent: January 9, 2001Assignee: Asta Medica AktiengesellschaftInventors: Gerhard Nössner, Bernhard Kutscher, J{umlaut over (u)}rgen Engel, Wolfgang Schumacher, Jurij Stekar, Peter Hilgard
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Patent number: 6156746Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formula ##STR1## and their enantiomers, diastereomers, and their pharmaceutically acceptable salts, including prodrugs and solvates thereof.The compounds of formula I are useful in the treatment of a variety of cancers. In addition, the formula I compounds may also be useful in the treatment of diseases other than cancer.Type: GrantFiled: July 15, 1999Date of Patent: December 5, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Katerina Leftheris, John T. Hunt, Charles Z. Ding
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Patent number: 6130231Abstract: This invention relates to novel fused heterocycles which are useful as antagonists of the .alpha..sub.v .beta..sub.3 and related integrin receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.Type: GrantFiled: November 26, 1997Date of Patent: October 10, 2000Assignee: DuPont PharmaceuticalsInventors: John Wityak, Aleksandra Ewa Tobin
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Patent number: 6121258Abstract: The invention provides compounds of formula ##STR1## as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases.Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.Type: GrantFiled: August 26, 1997Date of Patent: September 19, 2000Assignee: The Procter & Gamble CompanyInventors: Stanislaw Pikul, Neil Gregory Almstead, Rimma Sandler Bradley, Kelly Lynn McDow-Dunham, Biswanath De, Michael George Natchus, Yetunde Olabisi Taiwo, Thomas Lee Cupps
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Patent number: 6037334Abstract: Compounds of formula I ##STR1## in which R.sub.1, R.sup.2 are the same or different and denote a hydrogen atom, an alkyl group, a cycloalkyl group, a hydroxyalkyl group, an alkenyl group, an alkinyl group or an aralkyl group or R.sup.1 and R.sup.2 together denote an alkylene residue which, together with the bound oxygen atoms and the phosphorus atom carrying the oxygen atoms, forms a saturated 5-membered to 8-membered ring;R.sup.3 denotes an optionally substituted amino group, an alkyl group, a cycloalkyl residue or an optionally substituted aryl residue;n denotes an integer between 1 and 4,as well as hydrates, solvates and physiologically tolerated salts thereof, their optically active forms, processes for their production as well as pharmaceutical preparations having factor Xa-inhibitory properties which contain these compounds.Type: GrantFiled: July 15, 1999Date of Patent: March 14, 2000Assignee: Roche Diagnostics GmbHInventors: Ralf Kucznierz, Herbert Leinert, Wolfgang von der Saal, Richard Neidlein, Christiane Kehr
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Patent number: 5998443Abstract: This invention relates to the fields of pharmaceutical and organic chemistry and provides novel phosphorous-containing benzothiophene compounds which are useful for the treatment of the various medical indications associated with post-menopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus and cervix. The present invention further relates to intermediate compounds and processes useful for preparing the pharmaceutically active compounds of the present invention, and pharmaceutical compositions.Type: GrantFiled: October 8, 1997Date of Patent: December 7, 1999Assignee: Eli Lilly and CompanyInventors: Henry U. Bryant, Jeffrey A. Dodge, Jeffrey S. Nissen
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Patent number: 5990352Abstract: A salt useful as an active species in an organic reaction and represented by the following chemical formula (1): ##STR1## wherein n stands for an integer of from 1 to 8, Z.sup.n- represents an n-valent anion of an active hydrogen compound, a, b, c and d each stands for a positive integer, and Rs represent the same or different hydrocarbon groups. In addition, a simple and efficient process is provided for producing a poly(alkylene oxide) by polymerizing an alkylene oxide compound in the presence of the salt represented by the chemical formula (1).Type: GrantFiled: February 5, 1997Date of Patent: November 23, 1999Assignee: Mitsui Chemicals, Inc.Inventors: Tadahito Nobori, Masahiro Kouno, Toshiaki Suzuki, Kazumi Mizutani, Shinji Kiyono, Yoshiho Sonobe, Usaji Takaki
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Patent number: 5990307Abstract: This invention relates to a process for the preparation of the formula I compound [2-((8,9)-dioxo-2,6-diazabicyclo[5.2.0]-non-1(7)-en-2-yl)ethyl]phosphonic acid, a NMDA antagonist useful as an anticonvulsant and neuroprotectant in situations involving excess release of excitatory amino acids. ##STR1## In the process of the present invention, 3-aminopropyl carbamic acid 1,1-dimethylethyl ester is reacted with a dialkyl vinylphosphonate to obtain N-[3-(t-butyloxycarbonyl-amino)propyl]-2-aminoethylphosphonic acid dialkyl ester (d) in 80% yield. Reaction of (d) with a 3,4-dialkoxycyclobut-3-en-1,2-dione gives [3-[[2-(dialkoxyphosphoryl)ethyl]-(2-alkoxy-3,4-dioxo-1,2-cyclobuten-1-yl) amino]propyl] carbamic acid 1,1-dimethylethyl ester (e) in 96% yield. Deprotection and cyclization of (e) in trifluoroacetic acid gives [2-((8,9)-dioxo-2,6-diazabicyclo[5.2.0]-non-1(7)-en-2-yl)ethyl]phosphonic acid dialkyl ester (c) in 58% yield.Type: GrantFiled: July 31, 1998Date of Patent: November 23, 1999Assignee: American Home Products CorporationInventors: Andre A. Asselin, William A. Kinney, Jean Schmid
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Patent number: 5985856Abstract: The present invention is drawn to water soluble derivatives aliphatic acid aromatic secondary and tertiary amine containing drugs. The present invention is further drawn to methods of making water soluble derivatives of aliphatic and aromatic secondary and tertiary amine containing drugs.Type: GrantFiled: December 30, 1998Date of Patent: November 16, 1999Assignee: University of KansasInventors: Valentino Stella, Jeffrey P. Krise, Jan J. Zygmunt, Ingrid Gunda Georg
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Patent number: 5977101Abstract: Vitronectin receptor antagonists having the formula: ##STR1## which are useful for the treatment of inflammation, cancer and cardiovascular disorders, such as atherosclerosis and restenosis, and diseases wherein bone resorption is a factor, such as osteoporsis.Type: GrantFiled: December 20, 1996Date of Patent: November 2, 1999Assignee: SmithKline Beecham CorporationInventors: Fadia El-Fehail Ali, William Bondinell, William Francis Huffman, M. Amparo Lago, Richard McCulloch Keenan, Chet Kwon, William Henry Miller, Thomas Nguyen, Dennis T. Takata
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Patent number: 5958969Abstract: This invention relates to the field of pharmaceutical and organic chemistry and provides benzothiophene compounds, intermediates, formulations, and methods.Type: GrantFiled: September 3, 1997Date of Patent: September 28, 1999Assignee: Eli Lilly and CompanyInventors: Henry Uhlman Bryant, Michael John Martin, Ken Matsumoto
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Covalent lipid-phosphono-carboxylic acid conjugates and application thereof as antiviral medicaments
Patent number: 5955452Abstract: The present invention concerns new lipid derivatives of phosphonocarboxylic acids of the general formula I, ##STR1## in which the meaning of the symbols is elucidated in the description, tautomers thereof and their physiologically tolerated salts of inorganic and organic bases as well as processes for the production thereof and pharmaceutical agents containing these compounds.Type: GrantFiled: August 26, 1998Date of Patent: September 21, 1999Assignee: Roche Diagnostics GmbHInventors: Harald Zilch, Dieter Herrmann, Hans-George Opitz, Gerd Zimmermann, Edgar Voss -
Patent number: 5955461Type: GrantFiled: December 12, 1997Date of Patent: September 21, 1999Assignee: Schering AktiengesellschaftInventors: Andreas Huth, Lechoslaw Turski
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Patent number: 5914351Abstract: Compounds of the formula ##STR1## wherein Q is a hydrazone derivative;R.sup.1 is hydrogen, halogen, alkyl or alkoxy;R.sup.2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl, trifluoromethoxy, alkylthio, nitro or cyano; andR.sup.6 is a substituted carboxamide, carbothioamide, phosphonosoamide, or phosphonothioamide,useful as anti-HIV agents.Type: GrantFiled: December 12, 1997Date of Patent: June 22, 1999Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./CIE.Inventors: Walter Gerhard Brouwer, Ewa Maria Osika
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Patent number: 5889001Abstract: Tricyclic diazepines of the formula: ##STR1## wherein A, B, D, E, F, Y and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.Type: GrantFiled: June 13, 1997Date of Patent: March 30, 1999Assignee: American Cyanamid CompanyInventors: Jay Donald Albright, Marvin Fred Reich, Fuk-Wah Sum, Efren Guillermo Delos Santos
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Patent number: 5854237Abstract: Tricyclic diazepines of the formula: ##STR1## wherein A, B, D, E, F, Y and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.Type: GrantFiled: June 17, 1997Date of Patent: December 29, 1998Assignee: American Cyanamid CompanyInventors: Jay Donald Albright, Marvin Fred Reich, Fuk-Wah Sum, Efren Guillermo Delos Santos
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Patent number: 5849735Abstract: Tricyclic compound of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and process for preparing such compounds.Type: GrantFiled: December 22, 1995Date of Patent: December 15, 1998Assignee: American Cyanamid CompanyInventors: Jay D. Albright, Aranapakam M. Venkatesan, Efren G. Delos Santos
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Patent number: 5817602Abstract: Thiadiazabicyclodecanes of formula (I) wherein, Z is oxygen or sulfur; R is an optional substituent and W is an optionally condensed or substituted phenyl radical and the salts, complexes and stereisomers thereof, have good selective pre- and post-emergence herbicidal properties.Type: GrantFiled: December 21, 1995Date of Patent: October 6, 1998Assignee: Novartis CorporationInventors: Georg Pissiotas, Hans Moser, Hans-Georg Brunner
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Patent number: 5786353Abstract: Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.Type: GrantFiled: July 11, 1997Date of Patent: July 28, 1998Assignee: American Cyanamid CompanyInventors: Jay Donald Albright, Marvin Fred Reich, Fuk-Wah Sum, Xuemei Du
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Patent number: 5747487Abstract: Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in viva vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.Type: GrantFiled: April 25, 1996Date of Patent: May 5, 1998Assignee: American Cyanamid CompanyInventors: Jay Donald Albright, Marvin Fred Reich
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Patent number: 5739128Abstract: Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.Type: GrantFiled: April 24, 1996Date of Patent: April 14, 1998Assignee: American Cyanamid CompanyInventors: Jay Donald Albright, Marvin Fred Reich, Fuk-Wah Sum, Xuemei Du
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Patent number: 5736538Abstract: Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.Type: GrantFiled: April 25, 1996Date of Patent: April 7, 1998Assignee: American Cyanamid CompanyInventors: Jay Donald Albright, Xuemei Du
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Patent number: 5736540Abstract: Tricyclic diazepines of the formula: ##STR1## wherein A, B, D, E, F, Y and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.Type: GrantFiled: May 8, 1996Date of Patent: April 7, 1998Assignee: American Cyanamid CompanyInventors: Jay Donald Albright, Marvin Fred Reich, Fuk-Wah Sum, Efren Guillermo Delos Santos
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Patent number: 5733905Abstract: Tricyclic diazepines of the formula: ##STR1## wherein A, B, D, E, F, Y and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.Type: GrantFiled: May 8, 1996Date of Patent: March 31, 1998Assignee: American Cyanamid CompanyInventors: Jay Donald Albright, Marvin Fred Reich, Fuk-Wah Sum, Efren Guillermo Delos Santos
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Patent number: 5731299Abstract: The present invention relates to phosphonsulfonates and the pharmaceutically-acceptable salts and esters thereof, having the following structure according to formula (I): ##STR1## The present invention further relates to pharmaceutical compositions containing a safe and effective amount of a compound of the present invention, and pharmaceutically-acceptable excipients. Finally, the present invention relates to methods for treating or preventing pathological conditions characterized by abnormal calcium and phosphate metabolism in humans or other mammals, including treating or preventing osteoporosis and arthritis, especially rheumatoid arthritis and osteoarthritis. This method comprises administering to a human or other mammal in need of such treatment of a safe and effective amount of a compound or composition of the present invention.Type: GrantFiled: May 7, 1993Date of Patent: March 24, 1998Assignee: The Procter & Gamble CompanyInventors: Frank Hallock Ebetino, Allan Vincent Bayless, Susan Mary Dansereau
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Patent number: 5719278Abstract: Tricyclic compound of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and process for preparing such compounds.Type: GrantFiled: May 31, 1996Date of Patent: February 17, 1998Assignee: American Cyanamid CompanyInventors: Jay D. Albright, Efren G. Delos Santos, Xuemei Du, Marvin F. Reich
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Patent number: 5712396Abstract: .alpha.-Phosphonosulfonate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula ##STR1## wherein R.sup.2 is OR.sup.5 or R.sup.5a ; R.sup.3 and R.sup.5 are independently H, alkyl, arylalkyl, aryl or cycloalkyl; R.sup.5a is H, alkyl, arylalkyl or aryl; R4 is H, alkyl, aryl, arylalkyl, or cycloalkyl;, Z is H, halogen, lower alkyl or lower alkenyl; and R.sup.1 is a lipophilic group which contains at least 7 carbons and is alkyl, alkenyl, alkynyl, mixed alkenyl-alkynyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl; as further defined above; including pharmaceutically acceptable salts and or prodrug esters of the phosphonic (phosphinic) and/or sulfonic acids.Type: GrantFiled: July 5, 1994Date of Patent: January 27, 1998Inventors: David R. Magnin, Scott A. Biller, John K. Dickson, Jr., R. Michael Lawrence, Richard B. Sulsky
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Patent number: 5698541Abstract: The invention concerns compounds of the general formula I ##STR1## in which R denotes a lower alkyl which can be substituted if desired by hydroxy, alkoxy, amino, dialkylamino, alkylmercapto, alkylsulfinyl, alkanesulfonyl, cycloalkyl, aryl or a heterocyclic ring, or it denotes lower alkenyl, cycloalkyl, cycloalkenyl, aryl or a heterocyclic ring andR.sub.1 and R.sub.2 can be, independently of one another, hydrogen, lower alkyl, cycloalkyl, aryl or arylmethyl,their optically active salts as well as their pharmacologically acceptable salts, processes for their production as well as pharmaceutical agents which contain these compounds for treating diseases of calcium metabolism. Moreover the invention concerns compounds of formula II as intermediate products for the production of compounds of formula I.Type: GrantFiled: September 25, 1996Date of Patent: December 16, 1997Assignee: Boehringer Mannheim GmbHInventors: Gerd Zimmermann, Angelika Esswein, Christos Tsaklakidis, Frieder Bauss
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Patent number: 5686445Abstract: Tricyclic compounds of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and processes for preparing such compounds.Type: GrantFiled: April 25, 1996Date of Patent: November 11, 1997Assignee: American Cyanamid CompanyInventors: Jay Donald Albright, Xuemei Du
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Patent number: 5686466Abstract: A novel compound of the formula: ##STR1## wherein Ar represents an optionally substituted tricyclic condensed benzene ring group which includes at least one heterocyclic ring as a component ring; n represents an integer from 2 to 10; R.sup.1 represents H or an optionally substituted hydrocarbon group, which may be different from one another in the repetition of n; and Y represents an optionally substituted 4-piperidinyl, 1-piperazinyl or 4-benzyl-1-piperidinyl group, or a salt thereof, inhibiting excellent cholinesterase inhibitory activity and monoamine reuptake inhibitory activity, thus being useful as therapeutic and/or prophylactic medicaments of senile dementia.Type: GrantFiled: March 20, 1996Date of Patent: November 11, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Giichi Goto, Yuji Ishihara, Keisuke Hirai
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Patent number: 5659035Abstract: A method for the production of azacycloalkane-2,2-diphosphonic acids of general formula; ##STR1## where n is a whole number of from 2 to 16, Y is H, an alkyl or alkenyl, a substituted alkyl, or an aryl, such that the group "Y" remains unchanged during the reaction,by reaction of a lactam with a phosphorus trihalide in the presence of phosphorous acid and/or water, in which the reaction mixture also includes an organic amine and/or or an organic amine salt, said reaction being followed by hydrolysis of the reaction mixture and purification of the reaction product to obtain the diphosphonic acid.The method is exemplified by the preparation of azacycloheptane-2,2-diphosphonic acid, and azacyclononane-2,2-diphosphonic acid.Type: GrantFiled: December 8, 1994Date of Patent: August 19, 1997Assignee: Albright & Wilson LimitedInventors: Michael Bamber, Gary Woodward
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Patent number: 5633237Abstract: A class of imidazo[1,2-a]pyridinylalkyl phosphonic acid compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a compound of this class alone or in a composition in an amount effective as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula: ##STR1## and the carboxylic and phosphonic alkyl esters and salts thereof; wherein R.sup.9 is selected from hydrido, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl; wherein each of Y.sub.m and Y.sub.Type: GrantFiled: July 6, 1994Date of Patent: May 27, 1997Assignee: G.D. Searle & Co.Inventors: Donald W. Hansen, Jr., Gilbert W. Adelstein, Karen B. Peterson, Sofya Tsymbalov
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Patent number: 5631372Abstract: A process for producing 1-substituted-4-fluoro-1,4-diazoniabicyclo[2.2.2]octane salts having the formula ##STR1## wherein the Z substituent is OH, OR, OC(O)R, SO.sub.3, SO.sub.2 R, NO.sub.2, NO, or PO(OR).sub.2, wherein R is an aryl or C.sub.1 -C.sub.8 alkyl group; n is 0, 1 or 2; each of R.sub.1, R.sub.2, R.sub.3, P.sub.4 and R.sub.5 independently represent hydrogen, C.sub.1 to C.sub.8 alkyl, or aryl 1-substituted-1,4-diazoniabicyclo[2.2.2]octane or 1,4-diazoniabicyclo[2.2.2]octane mono-N-oxide is reacted to attach the Z group and then the result is reacted with molecular fluorine in the presence of a solvent that substantially does not react with fluorine and a fluoride scavenger that results in an X counter ion. These compounds are useful as fluorinating agents for the introduction of fluorine into organic compounds.Type: GrantFiled: May 6, 1996Date of Patent: May 20, 1997Assignee: AlliedSignal Inc.Inventors: Andrew J. Poss, George A. Shia, Dennis M. Lavery
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Patent number: 5624918Abstract: The present invention provides a phosphonic diester derivative of the following general formula (1): ##STR1## wherein A represents an oxygen atom or a sulfur atom; R.sup.1, R.sup.2, R.sup.9 and R.sup.10 are the same or different and they each represent a hydrogen atom, a lower alkoxy group, a nitro group, a lower alkyl group, a halogen-substituted lower alkyl group or a halogen atom; R.sup.3 represents a phenyl group, --B--R.sup.6 (wherein B represents an oxygen atom or a sulfur atom and R.sup.6 represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, a phenyl group, a phenyl(lower)alkyl group optionally having a halogen atom as a substituent on the phenyl ring, a phenoxy(lower)alkyl group, a lower alkoxycarbonyl(lower)alkyl group, a carboxy(lower)alkyl group or a lower alkenyl group) or --NR.sup.7 R.sup.8 (wherein R.sup.7 and R.sup.Type: GrantFiled: February 5, 1995Date of Patent: April 29, 1997Assignee: Otsuka Pharmaceutical Factory, Inc.Inventors: Yasuhisa Kurogi, Kazuyoshi Miyata, Shizuo Nakamura, Mitsuyoshi Kondo, Takeshi Iwamoto, Chieko Naba, Yoshihiko Tsuda, Yasuhide Inoue, Jun Kanaya, Keigo Sato
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Patent number: 5610294Abstract: This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors, to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating viral infection. A representative compound of the invention is the compound of formula: ##STR1## wherein R.sup.22 and R.sup.23 are allyl.Type: GrantFiled: February 16, 1994Date of Patent: March 11, 1997Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Patrick Y. Lam, Prabhakar K. Jadhav, Charles J. Eyermann, Carl N. Hodge, George V. De Lucca, James D. Rodgers
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Patent number: 5602113Abstract: Disclosed are novel pyrido[2,3,-b][1,5]benzodiazepines. These compounds are useful in the treatment of AIDS, ARC and related disorders associated with HIV infection.Type: GrantFiled: December 29, 1994Date of Patent: February 11, 1997Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Karl D. Hargrave, Ernest Cullen, John R. Proudfoot, Karl G. Grozinger, Kollol Pal, Julian Adams
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Patent number: 5597824Abstract: A compound of the formula: ##STR1## wherein B is a purin-9-yl group or a heterocyclic isostere of a purin-9-yl group; or a pyrimidin-1-yl group or a heterocyclic isostere of a pyrimidin-1-yl group; A is --CH-- or A--G taken together is --C(.dbd.O)--, --C(.dbd.CH.sub.2)--, --C(OH)(CH.sub.2 OH)-- or ##STR2## and G and D are functional groups; or a pharmaceutically acceptable salt or ester thereof.Type: GrantFiled: June 25, 1992Date of Patent: January 28, 1997Assignee: Abbott LaboratoriesInventors: Daniel W. Norbeck, Jacob J. Plattner, Terry J. Rosen
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Patent number: 5593979Abstract: Disclosed are novel pyrido[2,3-b][1,4]benzodiazepines. These compounds are useful in the treatment of AIDS, ARC and related disorders associated with HIV infection.Type: GrantFiled: December 29, 1994Date of Patent: January 14, 1997Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Karl D. Hargrave, Ernest Cullen, John R. Proudfoot, Karl G. Grozinger, Kollol Pal, Julian Adams
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Patent number: 5580979Abstract: The present invention makes available novel compounds represented by the general formula ##STR1## wherein Y represents a phosphate analog. Which compounds are useful for inhibiting an interaction between a protein containing an SH2 domain and a phophotyrosine-containing polypeptide.Type: GrantFiled: March 15, 1994Date of Patent: December 3, 1996Assignee: Trustees of Tufts UniversityInventor: William W. Bachovchin
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Patent number: 5550117Abstract: Disclosed are novel dipyrido[3,2-b:2',3'-e][1,4]diazepines and their use in the treatment of HIV-1 infection.Type: GrantFiled: December 29, 1994Date of Patent: August 27, 1996Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Karl D. Hargrave, Ernest Cullen, John R. Proudfoot, Karl G. Grozinger, Kollol Pal, Julian Adams
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Patent number: RE37781Abstract: This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors, to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating viral infection. A representative compound of the invention is the compound of formula: wherein R22 and R23 are allyl.Type: GrantFiled: March 10, 1999Date of Patent: July 2, 2002Assignee: DuPont Pharmaceuticals CompanyInventors: Patrick Y. Lam, Prabhakar K. Jadhav, Charles J. Eyermann, Carl N. Hodge, George V. De Lucca, James D. Rodgers