Phosphorus Attached Directly Or Indirectly To A 1,2-diazine Ring By Nonionic Bonding Patents (Class 544/232)
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Patent number: 6291425Abstract: This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.Type: GrantFiled: September 1, 1999Date of Patent: September 18, 2001Assignee: Guilford Pharmaceuticals Inc.Inventors: Jia-He Li, Jie Zhang
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Patent number: 6288123Abstract: The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 5, 1995Date of Patent: September 11, 2001Assignee: Cambridge NeuroSciences, Inc.Inventors: Stanley M. Goldin, James B. Fischer, Andrew Gannett Knapp, N. Laxma Reddy, David Berlove, Graham J. Durant, Subbarao Katragadda, Lain-Yen Hu, Sharad Magar, Wenhong Fan, Elizabeth Yost, Jun Qing Guo
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Patent number: 6194576Abstract: Nucleotide analogues having the general formula (I) and pharmaceutically acceptable derivatives: wherein n is 0 or an integer; X is O or S, CH2, CH-halogen, CH—N3, or C═CH2; Q and U are independently selected from: O, S, and CH(Ra) wherein Ra is hydrogen, OH, halogen, N3 ,NH2, SH, carboxyl, C1-6 alkyl or Ra is CH2(Rb) wherein Rb is hydrogen, OH, SH, NH2, C1-6 alkyl or carboxyl; or both Q and U are CH when Q and U are linked by a double bond; Z is selected from: O, a C1-6 alkoxy, a C1-6 thioalkyl, a C1-6 aminoalkyl, (CH2)m wherein m is 0 or an integer, and N(Rc)2 wherein both Rc are independently hydrogen or a C1-6 alkyl; and R2 is a purine or pyrimidine base or an analogue or derivative thereof. Members of this series of analogues possess anti-viral activity.Type: GrantFiled: October 4, 1999Date of Patent: February 27, 2001Assignee: BioChem Pharma, Inc.Inventors: Nghe Nguyen-Ba, Miguel Quimpere, Laval Chan Chun Kong, William L. Brown, Gervais Dionne
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Patent number: 6174924Abstract: The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 5, 1995Date of Patent: January 16, 2001Assignee: Cambridge NeuroScience, Inc.Inventors: Stanley M. Goldin, James B. Fischer, Andrew Gannett Knapp, N. Laxma Reddy, David Berlove, Graham J. Durant, Subbarao Katragadda, Lain-Yen Hu, Sharad Magar, Wenhong Fan, Elizabeth Yost, Jun Qing Guo
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Patent number: 6143791Abstract: The present invention provides therapeutically useful substituted guanidines, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more of such guanidines.Type: GrantFiled: June 7, 1995Date of Patent: November 7, 2000Assignee: Cambridge NeuroScience, Inc.Inventors: Stanley M. Goldin, James B. Fischer, Andrew Gannett Knapp, N. Laxma Reddy, David Berlove, Graham J. Durant, Subbarao Katragadda, Lain-Hu Hu, Sharad Magar, Wenhong Fan, Elizabeth Yost, Jun Qing Guo
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Patent number: 6127371Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: October 1, 1999Date of Patent: October 3, 2000Assignee: SmithKline Beecham CorporationInventors: John Duncan Elliott, Deborah Lynne Bryan
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Patent number: 6121251Abstract: Compounds with fungicidal and insecticidal properties having formula I ##STR1## wherein W is ##STR2## n is 0 or 1; Y is O, S, NR.sub.1, or R.sub.6 ;the ring bond containing R.sub.4 and R.sub.5 is a single or double bond;X is independently selected from hydrogen, halo, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy and --HC.dbd.CH--CH.dbd.CH-- thereby forming a napthyl ring;R is independently selected from (C.sub.1 -C.sub.12)alkyl and halo(C.sub.1 -C.sub.12)alkyl;R.sub.1 is independently selected from (C.sub.1 -C.sub.12)alkyl, (C.sub.2 -C.sub.8)alkenyl and aryl;R.sub.2 is independently selected from hydrogen, (C.sub.1 -C.sub.12)alkyl (C.sub.1 -C.sub.12)alkoxy, halo(C.sub.1 -C.sub.12)alkyl, halo(C.sub.1 -C.sub.12)alkoxy, hydroxy(C.sub.1 -C.sub.12)alkyl, (C.sub.1 -C.sub.12)alkoxy(C.sub.1 -C.sub.12)alkyl, (C.sub.1 -C.sub.12)alkoxycarbonyl(C.sub.1 -C.sub.12)alkyl, (C.sub.2 -C.sub.8)alkenyl, halo(C.sub.2 -C.sub.8)alkenyl, (C.sub.3 -C.sub.10)alkynyl, halo(C.sub.3 -C.sub.10)alkynyl, (C.sub.3 -C.sub.Type: GrantFiled: September 26, 1997Date of Patent: September 19, 2000Assignee: Rohm and Haas CompanyInventors: Steven Howard Shaber, Edward Michael Szapacs, Ronald Ross
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Patent number: 6069248Abstract: The present invention provides a process for the synthesis of triazolopyridazine based compounds represented by Formula A: ##STR1## These compounds have utility as angiotensin related antihypertensive agents.Type: GrantFiled: August 17, 1999Date of Patent: May 30, 2000Assignee: Axys Pharmaceuticals, Inc.Inventors: Armen M. Boldi, Charles R. Johnson
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Patent number: 6057304Abstract: The disclosure relates to quinoxaline derivatives of Formula I ##STR1## wherein R.sup.1, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are as defined in the disclosure, as well as their production and use in medicinal agents.Type: GrantFiled: June 5, 1995Date of Patent: May 2, 2000Assignee: Schering AktiengesellschaftInventors: Andreas Huth, Ralph Schmiechen, Ilse Beetz, Ingrid Schumann, Lechoslaw Turski, Peter Andreas Loschmann, David Norman Stephens, Dieter Seidelmann, Martin Kruger, Dieter Rahtz, Peter Holscher
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Patent number: 6002003Abstract: Activating groups for cyanine dyes used to label chain terminators in nucleotide sequencing, based on N-hydroxyphthalimide, are disclosed. From these activating groups, activated dyes of the present Invention are prepared which react with the derivitized nucleotide chain terminators to give a labeled chain terminator of the present Invention. The activating groups of the present Invention allow the dye-chain terminator reaction to occur at a much higher yield and with much greater selectivity for the mono-substituted product, compared with the prior art.Type: GrantFiled: April 14, 1998Date of Patent: December 14, 1999Assignee: Beckman Instruments, Inc.Inventors: Gene G.-Y. Shen, Thomas S. Dobashi
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Patent number: 5962437Abstract: A method of treating viral infections, and in particular HIV-1, hepatitis B virus and herpes viruses, is disclosed. The method comprising administering to a subject in need of such treatment an infection-combating amount of a phospholipid or phospholipid derivative.Type: GrantFiled: May 2, 1997Date of Patent: October 5, 1999Assignee: Wake Forest UniversityInventors: Louis S. Kucera, Susan L. Morris-Natschke, Khalid S. Ishaq
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Patent number: 5886177Abstract: Novel ethylene glycol compounds bearing various functional groups are used to prepare oligomeric structures. The ethylene glycol monomers can be joined via standard phosphate linkages including phosphorothioate, phosphodiester, and phosphoramidate linkages. Useful functional groups include nucleobases as well as polar groups, hydrophobic groups, ionic groups, aromatic groups and/or groups that participate in hydrogen-bonding.Type: GrantFiled: August 8, 1996Date of Patent: March 23, 1999Assignee: ISIS Pharmaceuticals, Inc.Inventors: Phillip Dan Cook, Oscar L. Acevedo, Peter W. Davis, David J. Ecker, Normand Hebert
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Patent number: 5874577Abstract: Unprotected adenine, 6-chloropurine, 2,6-diaminopurine, and 2-amino-6-chloropurine have been directly coupled with 2-(diethoxyphosphonomethoxy)ethanol under a disclosed method to provide acyclic phosphonate nucleotide analogues which are intermediates for antiviral agents such as 9-?2-(phosphonomethoxy)ethyl!adenine (PMEA) and its analogues having a structure of formula I: ##STR1## wherein Z represents N or CH; R.sub.1 represents hydrogen, alkyl, aryl, or arylalkyl; R.sub.2 and R.sub.3 are independently selected from H, OH, halo, NH.sub.2, C.sub.6 H.sub.5 CH.sub.2 O, or R.sub.4 R.sub.5 N wherein R.sub.4 and R.sub.5 are independently selected from alkyl, aryl, or arylalkyl.Type: GrantFiled: April 2, 1997Date of Patent: February 23, 1999Assignee: MediChem Research, Inc.Inventors: Wei Chen, Michael T. Flavin, Ze-Qi Xu
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Patent number: 5773592Abstract: A broad class of pharmaceutical agents which react directly with electron carriers or with reactive species produced by electron transport to release a pharmacologically active molecule to effect a therapeutic functional change in the organism by a receptor or nonrecepter mediated action.Type: GrantFiled: May 30, 1995Date of Patent: June 30, 1998Inventor: Randell Lee Mills
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Patent number: 5750525Abstract: Compounds of formula I are described ##STR1## in which R.sup.1, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 have the meanings mentioned in the application as well as their production and use in pharmaceutical agents.Type: GrantFiled: March 8, 1996Date of Patent: May 12, 1998Assignee: Schering AktiengesellschaftInventors: Andreas Huth, Lechoslaw Turski
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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: 5726311Abstract: Disclosed is a compound of the formula ##STR1## wherein R.sup.1 is H, NH.sub.2, or OCH.sub.3, R.sup.2 is an optionally substituted cyclic group optionally containing one or more heteroatoms, R.sup.3 and R.sup.4 are independently H or C.sub.1-4 alkyl, m is 0-4, n is 0-6, p is 0.1, X is CN, CSNH.sub.2, PO(OH).sub.2, COOH, SO.sub.2 NH.sub.2, NH.sub.2, OH, CNHNH.sub.2, tetrazole, triazole, or COR.sup.5 where R.sup.5 is C.sub.1-4 alkyl, CF.sub.3, NH.sub.2, or OC.sub.1-4 alkyl, and Y is O or NH that is useful as a pharmaceutical.Type: GrantFiled: June 7, 1995Date of Patent: March 10, 1998Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Shri Niwas, John A. Secrist, III, John A. Montgomery, Mark David Erion, Wayne C. Guida, Steve E. Ealick
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Patent number: 5714479Abstract: A heteroaromatic ring-fused cyclopentene derivative of the formula: ##STR1## wherein the variables are as defined in the specification; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: February 20, 1996Date of Patent: February 3, 1998Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Kiyofumi Ishikawa, Toshio Nagase, Toshiaki Mase, Takashi Hayama, Masaki Ihara, Masaru Nishikibe, Mitsuo Yano
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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: 5712285Abstract: A class of pyrrolo?2,3 -b!pyridine derivatives, linked via the 3-position thereof by a methylene group to a tetrahydropyridinyl moiety, the latter moiety being substituted in turn by an aryl- or heteroaryl-substituted divalent monocyclic radical, are ligands for dopamine receptorsubtypes within the body, in particular the D.sub.4 subtype, and are accordingly of use in the treatment and/or prevention of disorders of the dopamine system, including schizophrenia and depression.Type: GrantFiled: April 3, 1996Date of Patent: January 27, 1998Assignee: Merck, Sharp & Dohme, Ltd.Inventors: Neil Roy Curtis, Janusz Jozef Kulagowski, Paul David Leeson, Mark Peter Ridgill
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Patent number: 5710288Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification, are capable of lowering intraocular pressure in the eye of a mammal.Type: GrantFiled: May 3, 1996Date of Patent: January 20, 1998Assignee: AllerganInventors: Robert M. Burk, David F. Woodward
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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: 5684151Abstract: Disclosed are progestin agonists having the following formula: ##STR1## W is absent or --CH.dbd.CH--; R.sup.1 are independently selected from the group consisting of halogen, --CF.sub.3, and NO.sub.2, or both R.sup.1 may be joined to form a bi-radical which is --CH.dbd.CHCH.dbd.CH--;R.sup.3 are independently selected from the group consisting of hydrogen, C.sub.1-6 branched or linear alkyl, halogen and --CF.sub.3, with the proviso that R.sup.3 at the 3-position must be H where R.sup.3 at the 4-position is H, or both R.sup.3 may be joined to form a bi-radical selected from the group consisting of --CH.dbd.CHCH.dbd.CH--, --C(NC.sub.1-4 alkyl.sub.2)=CHCH.dbd.CH-- and --(CH.sub.2).sub.4 --;R.sup.5 is selected from the group consisting of H and Me;with the proviso that only one of R.sup.1 and R.sup.3 forms the fused bi-radical; and the stereoisomers.Type: GrantFiled: March 6, 1995Date of Patent: November 4, 1997Assignee: Ortho Pharmaceutical CorporationInventor: Donald W. Combs
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Patent number: 5668279Abstract: Novel substituted phthalazinones of the formula (I) ##STR1## are useful as neurotensin antagonists.Type: GrantFiled: April 6, 1995Date of Patent: September 16, 1997Assignee: Merck & Co., Inc.Inventors: Prasun K. Chakravarty, Elizabeth M. Naylor, Anna Chen
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Patent number: 5635494Abstract: Compounds with fungicidal and insecticidal properties having formula I ##STR1## wherein W is CH.sub.3 --O-A.dbd.C--CO(V)CH.sub.3 ; n is 0 or 1;A is N or CH;V is O or NH;whereinY is O, S, NR.sub.1, or R.sub.6, the ring bond containing R.sub.4 and R.sub.5 is a single or double bond and R.sub.4 and R.sub.5 are independently selected from hydrogen and substituted or unsubstituted alkyl and aryl groups.Type: GrantFiled: April 21, 1995Date of Patent: June 3, 1997Assignee: Rohm and Haas CompanyInventors: Ronald Ross, Steven H. Shaber, Edward M. Szapacs
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Patent number: 5635504Abstract: Compounds of the formula ##STR1## wherein: ##STR2## A is are dual inhibitors of NEP and ACE. Compounds wherein A is ##STR3## are selective ACE inhibitors.Type: GrantFiled: March 1, 1996Date of Patent: June 3, 1997Assignee: Bristol-Myers Squibb Co.Inventors: Denis E. Ryono, Chong-Oing Sun
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Patent number: 5635495Abstract: Compounds useful in the treatment of inflammation structurally represented as ##STR1## wherein X,X.sup.1 and R groups are as herein defined.Type: GrantFiled: April 6, 1995Date of Patent: June 3, 1997Assignee: The Upjohn CompanyInventors: David R. White, Edward L. Fritzen, Jr.
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Patent number: 5609867Abstract: This invention provides novel antitumor agents having the formula: ##STR1## wherein A, B, G, W, R.sup.1, R.sup.2, R.sup.3, n, m and Z are described in the specification which have activity as anticancer agents and inhibit leukemia and solid tumor growth in a mammal.Type: GrantFiled: August 29, 1995Date of Patent: March 11, 1997Assignee: American Cyanamid CompanyInventor: Hwei-Ru Tsou
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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: 5591729Type: GrantFiled: January 4, 1995Date of Patent: January 7, 1997Assignee: E. I. Du Pont de Nemours and CompanyInventors: Charles R. Harrison, George P. Lahm, Thomas M. Stevenson
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Patent number: 5580863Abstract: This invention relates to a compound represented by the formula: ##STR1## wherein B represents a hydrogen atom or a lower alkyl group; ring A represents a benzene ring which may have one or more substituents; .multidot..multidot..multidot..multidot..multidot. represents a single or double bond; Q.sub.1 represents the group represented by the formula, ##STR2## or a hydrocarbon residue substituted with the group represented by the formula, ##STR3## wherein X represents a bond or a spacer having a chain length of 1 to 4 atoms as the linear moiety which may have one or more side chains; R.sup.1 and R.sup.2, whether identical or not, independently represent a hydrogen atom or a lower alkyl, or may bind together to form a ring; Q.sub.2 represents a hydrogen atom, a hydrocarbon residue which may be substituted or a heterocyclic ring residue which may be substituted; or a salt thereof.Type: GrantFiled: May 13, 1994Date of Patent: December 3, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Shigehisa Taketomi, Tsuneo Oda
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Patent number: 5567841Abstract: .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; R.sup.4 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: June 5, 1995Date of Patent: October 22, 1996Assignee: Bristol-Myers Squibb CompanyInventors: David R. Magnin, Scott A. Biller, John K. Dickson, Jr., R. Michael Lawrence, Richard B. Sulsky
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Patent number: 5563268Abstract: Heterobiaryl derivatives of the formulaR.sub.1 NH--X.sub.1 --X.sub.2 --X.sub.3 --Y.sub.1 --Y.sub.2 --Y.sub.3 --Y.sub.4 --E (I)whereinR.sub.1, X.sub.1 to X.sub.3 and Y.sub.1 to Y.sub.4 are as defined herein, the tautomers, stereoisomers and mixtures thereof, and the salts, particularly the physiologically acceptable salts, thereof with organic or inorganic acids or bases. The derivatives have valuable pharmacological properties, such as inhibiting cell-cell aggregation and cell-matrix interactions.Type: GrantFiled: January 19, 1995Date of Patent: October 8, 1996Assignee: Dr. Karl Thomae GmbHInventors: Guenter Linz, Helmut Pieper, Frank Himmelsbach, Volkhard Austel, Thomas Mueller, Johannes Weisenberger, Elke Seewaldt-Becker
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Patent number: 5559135Abstract: Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, benign prostatic hyperplasia, inflammatory diseases including Raynaud's disease and asthma.Type: GrantFiled: September 14, 1994Date of Patent: September 24, 1996Assignee: Merck & Co., Inc.Inventors: Wallace T. Ashton, Linda L. Chang, William J. Greenlee
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Patent number: 5545647Abstract: 3-Phenylpyrrolidine compounds of the formula ##STR1## effectively inhibit phosphodiesterase (PDE) IV activities and can be used as medicaments for conditions such as asthma.Type: GrantFiled: March 6, 1995Date of Patent: August 13, 1996Assignee: Mitsubishi Chemical CorporationInventors: Toshihiko Tanaka, Akihiro Yamamoto, Akira Amenomori
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Patent number: 5491145Abstract: Novel compound of the general formula: ##STR1## wherein R.sup.1 stands for a hydrogen atom, an optionally substituted lower alkyl group or a halogen atom; R.sup.2 and R.sup.3 respectively stand for a hydrogen atom or an optionally substituted lower alkyl group, provided that either R.sup.2 or R.sup.3 is a hydrogen atom, the other being an optionally substituted lower alkyl group, or R.sup.2 and R.sup.3 may, taken together with the adjacent --C=C-- group, form a 5- to 7-membered ring; X stands for an oxygen atom or S(O).sub.p (p stands for an integer from 0 to 2; Y stands for a group of the formula: ##STR2## (R.sup.4 and R.sup.5 respectively stand for a hydrogen atom or an optionally substituted lower alkyl group) or a divalent group derived from an optionally substituted 3- to 7-membered homocyclic or heterocyclic ring; R.sup.6 and R.sup.7 each stands for a hydrogen atom, an optionally substituted lower lakyl group, an optionally substituted cycloalkyl group or an optionally substituted aryl group, or R.sup.Type: GrantFiled: November 21, 1994Date of Patent: February 13, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Akio Miyake, Yasuhiko Kawano, Yasuko Ashida
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Patent number: 5474974Abstract: There are provided new 3-hydroxy-4-aryl-5-oxo-pyrazoline derivatives of the formula (I) ##STR1## The new 3-hydroxy-4-aryl-5-oxo-pyrazoline derivatives of the formula (I) have a particularly pronounced activity against animal pests, in particular against insects and arachnids, and against weeds.Type: GrantFiled: April 28, 1994Date of Patent: December 12, 1995Assignee: Bayer AktiengesellschaftInventors: Bernd-Wieland Kruger, Reiner Fischer, Heinz-Jurgen Bertram, Thomas Bretschneider, Stefan Bohm, Andreas Krebs, Thomas Schenke, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt, Christoph Erdelen, Ulrike Wachendorff-Neumann, Wilhelm Stendel
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Patent number: 5463071Abstract: Compounds of the formula ##STR1## wherein X.sub.1 to X.sub.5 are as defined herein, the tautomers, the stereoisomers including the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases. The compounds are useful for inhibiting undesirable cell aggregation.Type: GrantFiled: November 8, 1993Date of Patent: October 31, 1995Assignee: Dr. Karl Thomae GmbHInventors: Frank Himmelsbach, Guenter Linz, Volkhard Austel, Helmut Pieper, Thomas Mueller, Johannes Weisenberger, Elke Seewaldt-Becker
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Patent number: 5434150Abstract: The invention relates to cyclic imino derivatives of general formula ##STR1## wherein A to G, R.sub.1, Z.sub.1 to Z.sub.6, X and Y are defined as in claim 1, the tautomers, stereoisomers and mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, preferably aggregation-inhibiting properties, pharmaceutical compositions which contain these compounds and processes for preparing them.Type: GrantFiled: August 28, 1992Date of Patent: July 18, 1995Assignee: Dr. Karl Thomae GmbHInventors: Volhard Austel, Helmut Pieper, Frank Himmelsbach, Guenter Linz, Thomas Mueller, Johannes Weisenberger, Elke Seewaldt-Becker
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Patent number: 5428163Abstract: A broad class of pharmaceutical agents which react directly with electron carriers or with reactive species produced by electron transport to release a pharmacologically active molecule to effect a therapeutic functional change in the organism by a receptor or nonrecepter mediated action.Type: GrantFiled: December 4, 1989Date of Patent: June 27, 1995Inventor: Randell L. Mills
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Patent number: 5418233Abstract: Heterobiaryl derivatives of the formulaR.sub.1 NH--X.sub.1 --X.sub.2 --X.sub.3 --Y.sub.1 --Y.sub.2 --Y.sub.3 --Y.sub.4 --E (I)whereinR.sub.1, X.sub.1 to X.sub.3 and Y.sub.1 to Y.sub.4 are as defined herein, the tautomers, stereoisomers and mixtures thereof, and the salts, particularly the physiologically acceptable salts, thereof with organic or inorganic acids or bases. The derivatives have valuable pharmacological properties, such as inhibiting cell-cell aggregation and cell-matrix interactions.Type: GrantFiled: October 14, 1992Date of Patent: May 23, 1995Assignee: Karl Thomae GmbHInventors: Guenter Linz, Helmut Pieper, Frank Himmelsbach, Austel: Volkhard, Thomas Mueller, Johannes Weisenberger, Elke Seewaldt-Becker
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Patent number: 5405841Abstract: The invention relates to new phosphorylated aza compounds, to processes for their preparation and to their use as pesticides, in particular as soil-acting insecticides and nematicide.The new compounds have the general formula (I) ##STR1## in which R.sup.1 -R.sup.5, X and Y are defined as in the specification, with the exception of compound O-ethyl S-propyl 3-(6-chloro-3-pyridinylmethyl)-2-nitroimino-imidazolidine-1-thiophosphate.Type: GrantFiled: November 30, 1993Date of Patent: April 11, 1995Assignee: Bayer AktiengesellschaftInventors: Fritz Maurer, Jurgen Hartwig, Christoph Erdelen
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Patent number: 5389620Abstract: A heteroaromatic ring-fused cyclopentene derivative of the formula: ##STR1## wherein the variables are as defined in the specification; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 14, 1993Date of Patent: February 14, 1995Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Kiyofumi Ishikawa, Toshio Nagase, Toshiaki Mase, Takashi Hayama, Masaki Ihara, Masaru Nishikibe, Mitsuo Yano
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Patent number: 5380718Abstract: Arthropodicidal tetrahydropyridazines of Formulae I and II, ##STR1## wherein Q,X,X.sup.1 Y, and G are as defined in the text, compositions containing them and their use in the control of arthropods.Type: GrantFiled: November 12, 1992Date of Patent: January 10, 1995Assignee: E. I. Du Pont de Nemours and CompanyInventors: Charles R. Harrison, George P. Lahm, Thomas M. Stevenson
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Patent number: 5358924Abstract: There are provided new 3-hydroxy-4-aryl-5-oxo-pyrazoline derivatives of the formula (I) ##STR1## in which A and B are identical or different and independently of one another in each case represent hydrogen, alkyl, alkenyl, alkynyl, alkoxyalkyl, alkythioalkyl, cycloalkyl or optionally substituted aryl orA and B together represent the bivalent radical of a saturated or unsaturated, optionally substituted, mono-, bi-, tri- or polycyclic system,X represents alkyl, halogen or alkoxy,Y represents hydrogen, alkyl, halogen, alkoxy or halogenoalkyl,Z represents alkyl, halogen or alkoxy,n represents a number 0, 1, 2 or 3,G represents hydrogen (a) or the groups ##STR2## in which E represents a metal ion equivalent or an ammonium ion,L and M represents oxygen and/or sulphur,and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 have the meaning given in the text of the application.Type: GrantFiled: December 31, 1992Date of Patent: October 25, 1994Assignee: Bayer AktiengesellschaftInventors: Bernd-Wieland Kruger, Reiner Fischer, Heinz-Jurgen Bertram, Thomas Bretschneider, Stefan Bohm, Andreas Krebs, Thomas Schenke, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt, Christoph Erdelen, Ulrike Wachendorff-Neumann, Wilhelm Stendel
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Patent number: 5334586Abstract: The present invention relates to novel heterocycle-substituted diphosphonic acids, and the pharmaceutically-acceptable salts and esters thereof, in which the diphosphonate-substituted carbon atom moiety is attached to a carbon atom in a nitrogen-containing six membered ring heterocycle, preferably a piperidine ring. The heterocycle-substituted diphosphonic acid compounds have the general structure: ##STR1## wherein Z is a nitrogen-containing six membered ring heterocycle moiety selected from piperidinyl, diazinyl and triazinyl; m, n and m+n are from 0 to 10; Q is a covalent bond or a moiety selected from oxygen, sulfur or nitrogen; and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are substituent groups.The present invention further relates to pharmaceutical compositions containing these novel compounds. Finally this invention relates to methods for treating or preventing diseases characterized by abnormal calcium and phosphate metabolism by utilizing a compound or pharmaceutical composition of the present invention.Type: GrantFiled: October 21, 1991Date of Patent: August 2, 1994Assignee: Procter & Gample Pharmaceuticals, Inc.Inventors: Frank H. Ebetino, James J. Benedict
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Patent number: 5294616Abstract: A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.Type: GrantFiled: March 25, 1992Date of Patent: March 15, 1994Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman, Laura M. Turchi, William L. Laswell
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Patent number: 5284838Abstract: The invention relates to 2,2-dimethylchroman-3-ol derivatives of the formula: ##STR1## in which: A, between N and CO, represents the group --CH.dbd.CH--E.dbd.CH-- or the group ##STR2## Z represents a halogen or a cyano, acetyl, trifluoroacetyl, nitro, alkylthio, carboxyl, phosphono, dial-koxyphosphoryl or alkoxycarbonyl group, the alkylthio and alkoxy groups containing from 1 to 3 carbon atoms;E represents a nitrogen atom or a group C(R.sub.4);R.sub.1 represents hydrogen, a methyl group or a hydroxyl group and R.sub.2 and R.sub.3 each independently represent hydrogen or a methyl group, it being possible for only one of the substituents R.sub.1, R.sub.2 and R.sub.3 to be methyl; andR.sub.4 represents a hydrogen atom, a halogen atom, a methyl group or a hydroxyl group;and to the pharmaceutically acceptable salts of the phosphono or carboxyl group.These derivatives have an antiarrhythmic, antiasthma and antihypertensive activity.Type: GrantFiled: February 18, 1993Date of Patent: February 8, 1994Assignee: Elf SanofiInventors: Georges Garcia, Richard Roux, Dino Nisato, Patrick Gautier
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Patent number: 5280022Abstract: A compound of the formula (I): ##STR1## wherein W is a group of the formula:A--O--(CH.sub.2 .sub.n --wherein A is a cyclic group which may be substituted, n is an of 2 to 10, or W is a group of the formula:R.sup.1 --X--(CH.sub.2).sub.n' --wherein R.sup.1 is an alkyl group which may be substituted, X is an oxygen atom or a sulfur atom which may be oxidized, n' is an integer of 4 to 10; R.sup.2 is a hydrogen atom or a lower alkanoyl group; R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different and are a hydrogen atom or a lower alkyl group, or a salt thereof, is useful as a bone resorption inhibitor.Type: GrantFiled: December 18, 1991Date of Patent: January 18, 1994Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Shigehisa Taketomi
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Patent number: RE36187Abstract: This invention relates to the use of acyclic substituted pyrrolo?2,3-d!pyrimidine nucleoside analogs in the treatment of viral infections. Such substituted compounds retain antiviral properties present in their parent compounds, yet exhibit significantly decreased levels of cytotoxicity, thereby having therapeutic potential as antiviral agents.Type: GrantFiled: August 5, 1994Date of Patent: April 6, 1999Assignee: The Regents of the University of MichiganInventors: Leroy B. Townsend, John G. Drach, Charles Shipman, Jr., Jeffrey S. Pudlo