Phosphorus Attached Directly Or Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/5)
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Patent number: 6025344Abstract: The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives that inhibit N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, and to treat prostate diseases, especially using the compounds of the present invention for the inhibition of the growth of prostate cancer cells.Type: GrantFiled: May 27, 1997Date of Patent: February 15, 2000Assignee: Guilford Pharmaceuticals Inc.Inventors: Paul F. Jackson, Barbara S. Slusher, Kevin L. Tays, Keith M. Maclin
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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: 5985855Abstract: The present invention includes compositions and methods of treatment for glutamate abnormalities and associated nervous tissue insult in a animal by inhibition of NAALADase enzyme. Compositions include glutamate-derived hydroxyphosphinyl derivative compounds, acidic peptide analogs, phosphinic acid derivatives and mixtures thereof that inhibit NAALADase enzyme activity and their use for treating glutamate abnormalities such as created by global and focal ischemia.Type: GrantFiled: November 20, 1997Date of Patent: November 16, 1999Assignee: Guilford Pharmaceuticals Inc.Inventors: Barbara S. Slusher, Paul F. Jackson
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Patent number: 5968915Abstract: The present disclosure relates to dipeptidase inhibitors, and more particularly, to N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme inhibitors which are proposed as novel agents for the treatment of prostate cancer. NAALADase is enzyme which is a membrane-bound metalloprotease which hydrolyzes the dipeptide, N-acetyl-L-aspartate-L-glutamate (NAAG) to yield glutamate and N-acetylaspartate. The compounds of the present invention include phosphinic acid derivatives that inhibit NAALADase enzyme activity and which have been found useful for inhibiting the growth of prostate cancer cells.Type: GrantFiled: April 8, 1997Date of Patent: October 19, 1999Assignee: Guilford Pharmaceuticals Inc.Inventors: Paul F. Jackson, Barbara S. Slusher
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Patent number: 5824662Abstract: The present invention includes compositions and methods of treatment for glutamate abnormalities and associated nervous tissue insult in a animal by inhibition of NAALADase enzyme. Compositions include glutamate-derived hydroxyphosphinyl derivative compounds, acidic peptide analogs, phosphinic acid derivatives and mixtures thereof that inhibit NAALADase enzyme activity and their use for treating glutamate abnormalities such as created by global and focal ischemia.Type: GrantFiled: September 27, 1996Date of Patent: October 20, 1998Assignee: Guilford Pharmaceuticals Inc.Inventors: Barbara S. Slusher, Paul F. Jackson
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Patent number: 5808162Abstract: A novel chiral unsymmetric diphosphine compound of formula (I): ##STR1## wherein Ar.sup.1 and Ar.sup.2, which are different from each other, each represent a substituted or unsubstituted phenyl group, a substituted or unsubstituted naphthyl group, a pyridyl group, a quinolyl group, an isoquinolyl group, a furfuryl group, a benzofurfuryl group, a thienyl group, or a benzothienyl group, and a transition metal complex containing the diphosphine compound as a ligand. The complex catalyzes various asymmetric synthesis reactions, e.g., asymmetric hydrogenation or asymmetric hydrosilylation, exhibiting excellent performance in selectivity, conversion and catalytic activity, to provide a product of desired absolute configuration at high optical purity and in high yield.Type: GrantFiled: July 18, 1996Date of Patent: September 15, 1998Assignee: Takasago International CorporationInventors: Noboru Sayo, Xiaoyong Zhang, Tatsuya Omoto, Tohru Yokozawa, Tetsuro Yamasaki, Hidenori Kumobayashi
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Patent number: 5750729Abstract: In accordance with this invention novel compounds are provided that are selected from saturated and unsaturated pyrans and furans substituted with at least a phosphonate group and a heterocyclic base. These compounds are useful as antiinfectives, flame retardants, diagnostic oligonucleotides and immunogens.Type: GrantFiled: February 25, 1997Date of Patent: May 12, 1998Assignee: Gilead Sciences,Inc.Inventors: Petr Alexander, Ernest J. Prisbe
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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: 5679700Abstract: Novel phosphinic acid-containing peptidyl compounds of formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophobic epidermolysis bullosa, and coronary thrombosis associated with atherosclerotic plaque rupture. These inhibitors may also be useful in preventing the pathological sequelae following a traumatic injury that could lead to permanent disability. These compounds may also have utility as a means for birth control by preventing ovulation or implantation.Type: GrantFiled: November 9, 1995Date of Patent: October 21, 1997Assignee: Merck & Co., Inc.Inventors: Charles G. Caldwell, Philippe L. Durette, Joung L. Goulet, William K. Hagmann, Soumya P. Sahoo
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Patent number: 5672592Abstract: The present disclosure relates to dipeptidase inhibitors, and more particularly, to N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme inhibitors which are proposed as novel agents for the treatment of prostate cancer. NAALADase is enzyme which is a membrane-bound metalloprotease which hydrolyzes the dipeptide, N-acetyl-L-aspartate-L-glutamate (NAAG) to yield glutamate and N-acetylaspartate. The compounds of the present invention include phosphinic acid derivatives that inhibit NAALADase enzyme activity and which have been found useful for inhibiting the growth of prostate cancer cells.Type: GrantFiled: June 17, 1996Date of Patent: September 30, 1997Assignee: Guilford Pharmaceuticals Inc.Inventors: Paul F. Jackson, Barbara S. Slusher
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Patent number: 5656750Abstract: Squarylium compounds of the formula: ##STR1## (in which Q.sup.1 and Q.sup.2 are each a chromophoric group having an aromatic unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens, R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group, and R.sup.3 and R.sup.4 are each independently a hydrogen atom, or an acyl, aliphatic, cycloaliphatic, aromatic or heterocyclic group, subject to the proviso that one of R.sup.3 and R.sup.4 may be an amino or substituted amino group, or one of R.sup.3 and R.sup.4 is a hydrogen atom and the other is an organosulfonyl group, or R.sup.3 and R.sup.4 together with the intervening nitrogen atom form a nitrogenous heterocyclic ring) are useful as near infra-red absorbers.Type: GrantFiled: June 6, 1995Date of Patent: August 12, 1997Assignee: Polaroid CorporationInventors: Richard M. Allen, Peter K. Chu
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Patent number: 5622821Abstract: The invention provides lanthanide chelates capable of intense luminescence. The celates comprise a lanthanide chelator covalently joined to a coumarin-like or quinolone-like sensitizer. Exemplary sensitzers include 2- or 4-quinolones, 2- or 4-coumarins, or derivatives thereof e.g. carbostyril 124 (7-amino-4-methyl-2-quinolone), coumarin 120 (7-amino-4-methyl-2-coumarin), coumarin 124 (7-amino-4-(trifluoromethyl)-2-coumarin), aminomethyltrimethylpsoralen, etc.The chelates form high affinity complexes with lanthanides, such as terbium or europium, through chelator groups, such as DTPA. The chelates may be coupled to a wide variety of compounds to create specific labels, probes, diagnostic and/or therapeutic reagents, etc. The chelates find particular use in resonance energy transfer between chelate-lanthanide complexes and another luminescent agent, often a fluorescent non-metal based resonance energy acceptor.Type: GrantFiled: June 29, 1994Date of Patent: April 22, 1997Assignee: The Regents of the University of CaliforniaInventors: Paul R. Selvin, John Hearst
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Patent number: 5602115Abstract: The bisphosphonates of formula (III)R.sub.2 --X--(CW).sub.m1 --CR.sub.3 R.sub.4 --CH.sub.2 --CM[PO--(OR.sub.1).sub.2 ].sub.2 (III)bicyclic bisphosphonates (V), and cyclic bisphosphonates (VII) are useful as antiarthritic agents and do not have the side effects of anti-arthritic agents which are prostaglandin synthetase inhibitors.Type: GrantFiled: November 28, 1994Date of Patent: February 11, 1997Assignee: The Upjohn CompanyInventor: Richard A. Nugent
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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: 5565440Abstract: The present invention discloses a methane diphosphonate derivative, a process for producing said derivative and its pharmaceutical applications, said methane diphosphonate derivative indicated with general formula (1): ##STR1## (wherein, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently a pharmacologically acceptable cation, a hydrogen atom or a straight chain or branched alkyl group having 1-4 carbon atoms, R.sub.5 is a hydrogen atom or a trialkylsilyl group, m is an integer of 0 to 3, n is an integer of 1 to 3, R.sub.6 and R.sub.7 are independently a hydrogen atom or an alkyl group, and X represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group or an alkylthio group).Type: GrantFiled: June 28, 1994Date of Patent: October 15, 1996Assignee: Toray Industries, Inc.Inventors: Keijiro Takanishi, Norio Kawabe, Teruo Nakadate
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Patent number: 5525736Abstract: A process for the production of a 5-7 membered ring cyclic sulfonium salt compound, including a 5-7 membered ring cyclic sulfonium salt compound having a non-nucleophilic anion, is described. Members of the latter group are potentially useful as initiators for cationic polymerizations. The process comprises reacting a 1.4-, 1.5-, or 1.6-diol compound or a 5-7 membered ring cyclic ether compound with a mercapto compound and a strong protonic acid yielding the cyclic sulfonium salt compound. Some compounds described are also novel compounds per se.Type: GrantFiled: February 23, 1995Date of Patent: June 11, 1996Assignee: Ciba-Geigy CorporationInventors: Jan-Erik Nystrom, Per Engelhardt, Katarina Beierlein, Mikael Sellen, Bjorn Elman, Jan Vagberg, Martin Nylof
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Patent number: 5480645Abstract: Hydroxyamines N-acyl derivatives with benzochroman or 2,3-dihydrobenzofuran carboxy acids and relative pharmaceutical composition for the therapeutic treatment of those CNS, vascular, cardiovascular, dermatologic and ophthalmic pathologies wherein it is important to associate an inflammatory modulation effect to an antioxidant activity.Type: GrantFiled: December 29, 1993Date of Patent: January 2, 1996Assignee: LifeGroup S.p.A.Inventors: Francesco Della Valle, Silvana Lorenzi, Gabriele Marcolongo
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Patent number: 5468870Abstract: Dye-donor element for use according to thermal dye sublimation transfer comprising a support having thereon a dye layer containing a dye corresponding to the following formula ##STR1## wherein Z represents CN, COOR.sup.1 or CONR.sup.2 R.sup.3 ;R.sup.1, R.sup.2 and R.sup.3 each independently represent hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, or R.sup.2 and R.sup.3 together represent the necessary atoms to close a heterocyclic nucleus or substituted heterocyclic nucleus;Y represents OR.sup.4 or NR.sup.5 R.sup.6 or CN;R.sup.4 represents hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, SO.sub.2 R.sup.7, COR.sup.7, CSR.sup.7, POR.sup.7 R.sup.8 ;R.sup.5 and R.sup.6 each independently has one of the significances given to R.sup.4 or represent substituted or unsubstituted amino, or R.sup.5 and R.sup.Type: GrantFiled: October 20, 1994Date of Patent: November 21, 1995Assignee: AGFA-GAVAERT, N.V.Inventor: Luc J. Vanmaele
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Patent number: 5428027Abstract: Certain substituted semicarbazones, including all geometric and stereoisomers thereof, agricultural compositions containing them and their use as arthropodicides.Type: GrantFiled: October 28, 1993Date of Patent: June 27, 1995Assignee: E. I. Du Pont de Nemours and CompanyInventors: John P. Daub, George P. Lahm, Bradford S. Marlin
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Patent number: 5412141Abstract: The bisphosphonates of formula (III)R.sub.2 --X--(CW).sub.m1 --CR.sub.3 R.sub.4 --CH.sub.2 --CM[PO--(OR.sub.1).sub.2 ].sub.2 (III)bicyclic bisphosphonates (V), and cyclic bisphosphonates (VII) are useful as anti-arthritic agents and do not have the side effects of anti-arthritic agents which are prostaglandin synthetase inhibitors.Type: GrantFiled: February 19, 1993Date of Patent: May 2, 1995Assignee: The Upjohn CompanyInventor: Richard A. Nugent
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Patent number: 5410060Abstract: Arenebisphosphine oxides of the general formula ##STR1## where R.sup.1 to R.sup.4 independently of one another are each hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.5 -C.sub.10 -aryl, C.sub.5 -C.sub.12 -aryloxy or C.sub.7-C.sub.14 -arylalkoxy, R.sup.5 and R.sup.6 independently of one another may each be C.sub.1 -C.sub.6 -alkyl, C.sub.5 -C.sub.10 -cycloalkyl or C.sub.5 -C.sub.12 -aryl, each of which may furthermore contain one or two nitrogen or sulfur atoms in the ring system or carry one or two halogen atoms or C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -alkoxy groups as substituent on the ring system, or C.sub.1 -C.sub.6 -alkoxy, C.sub.3 -C.sub.8 -alkoxyalkoxy, C.sub.5 -C.sub.12 -aryloxy or C.sub.7 -C.sub.14 -arylalkoxy, or R.sup.5 and R.sup.6 together form a bridge of 2 to 10 carbon atoms, in which some of the carbon atoms may furthermore be part of an aromatic ring.Type: GrantFiled: December 2, 1993Date of Patent: April 25, 1995Assignee: BASF AktiengesellschaftInventors: Jochen Schroeder, Wolfgang Siegel, Matthias Lokai
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Patent number: 5405976Abstract: Dyes comprising an inner salt of a compound of the formula:Q.sup.1 =Z-Q.sup.2wherein:Q.sup.1 is a 4-(benz[b]-4H-pyrylium)methylidene, 4-(benz[b]-4H-thiopyrylium)methylidene or 4-(benz[b]-4H-selenopyrylium)methylidene grouping;Z is a 1,3-(2-hydroxy-4-oxo-2-cyclobutylidene) hydroxide or 1,3-(2-hydroxy-4,5-dioxo-2-cyclopentylidene) hydroxide ring; andQ.sup.2 is a 4-(benz[b]-4H-pyran-4-ylidene)methyl, 4-(benz[b]-4H-thiopyran-4-ylidene)methyl or 4-(benz[b]-4H-selenopyran-4-ylidene)methyl grouping;wherein at least one of the groupings Q.sup.1 and Q.sup.Type: GrantFiled: September 24, 1993Date of Patent: April 11, 1995Assignee: Polaroid CorporationInventors: Stephen J. Telfer, Robert P. Short, Stephen G. Stroud, Anthony J. Puttick, Socorro Ramos, Michael J. Zuraw
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Patent number: 5371228Abstract: Dye-donor element for use according to thermal dye sublimation transfer comprising a support having thereon a dye layer containing a dye corresponding to the following formula ##STR1## wherein Z represents CN, COOR.sup.1 or CONR.sup.2 R.sup.3 ;R.sup.1, R.sup.2 and R.sup.3 each independently represent hydrogen, alkyl, cycloalkyl, aryl, or R.sup.2 and R.sup.3 together represent the necessary atoms to close a heterocyclic nucleus;Y represents OR.sup.4 or NR.sup.5 R.sup.6 ;R.sup.4 represents hydrogen, alkyl, cycloalkyl, aryl, SO.sub.2 R.sup.7, COR.sup.7, CSR.sup.7, POR.sup.7 R.sup.8 ;R.sup.5 and R.sup.6 each independently has one of the significances given to R.sup.4 or represent amino, or R.sup.5 and R.sup.6 together represent the necessary atoms to close a heterocyclic nucleus, including a heterocyclic nucleus with an aliphatic or aromatic ring fused-on;R.sup.7 and R.sup.Type: GrantFiled: August 24, 1992Date of Patent: December 6, 1994Assignee: Agfa-Gevaert, N.V.Inventor: Luc J. Vanmaele
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Patent number: 5368985Abstract: Bisacylphosphine sulfides of formula I ##STR1## wherein R.sub.1 is unsubstituted C.sub.1 -C.sub.18 or C.sub.1 -C.sub.8 alkyl which is substituted by phenyl, --CN, C.sub.1 -C.sub.12 alkoxy or halogen, C.sub.2 -C.sub.18 alkenyl, unsubstituted C.sub.5 -C.sub.8 cycloalkyl or C.sub.5 -C.sub.8 cycloalkyl which is substituted by C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.12 alkoxy or halogen, unsubstituted C.sub.6 -C.sub.12 aryl or C.sub.6 -C.sub.12 aryl which is substituted by halogen, C.sub.1 -C.sub.12 alkyl or C.sub.1 -C.sub.12 alkoxy, or a 5- or 6-membered aromatic heterocyclic radical which contains oxygen, sulfur and/or nitrogen and is unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, andR.sub.2 and R.sub.3 are each independently of the other unsubstituted C.sub.1 -C.sub.18 alkyl or C.sub.1 -C.sub.8 alkyl which is substituted by phenyl, halogen or C.sub.1 -C.sub.12 alkoxy, C.sub.2 -C.sub.6 alkenyl, unsubstituted C.sub.5 -C.sub.8 cycloalkyl or C.sub.5 -C.sub.Type: GrantFiled: February 28, 1994Date of Patent: November 29, 1994Assignee: Ciba-Geigy CorporationInventors: Werner Rutsch, Gebhard Hug, Manfred Kohler
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Patent number: 5354873Abstract: Squarylium compounds of the formula: ##STR1## (in which Q.sup.1 and Q.sup.2 are each a chromophoric group having an aromatic unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens, R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group, and R.sup.3 and R.sup.4 are each independently a hydrogen atom, or an acyl, aliphatic, cycloaliphatic, aromatic or heterocyclic group, subject to the proviso that one of R.sup.3 and R.sup.4 may be an amino or substituted amino group, or one of R.sup.3 and R.sup.4 is a hydrogen atom and the other is an organosulfonyl group, or R.sup.3 and R.sup.4 together with the intervening nitrogen atom form a nitrogenous heterocyclic ring) are useful as near infra-red absorbers.Type: GrantFiled: November 20, 1992Date of Patent: October 11, 1994Assignee: Polaroid CorporationInventors: Richard M. Allen, Peter K. Chu, John W. Lee, Donald A. McGowan, Mark R. Mischke, Socorro M. Ramos, Stephen J. Telfer
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Patent number: 5347040Abstract: Onium salt capable of generating acid upon exposure to actinic radiation having the following structure:(R.sub.1).sub.a (R.sub.2).sub.b (R.sub.3).sub.c Q.sup.+ --A--M.sup.+ X.sup.- --B--X'.sup.-where:Q is S;R.sub.1, R.sub.2 and R.sub.3 are independently substituted or unsubstituted aromatic, aliphatic, or aralkyl groups having 7-18 carbon atoms;M.sup.+ is a cationic organic radical;A is a divalent radical selected from the group of hindered alkylene groups, substituted or unsubstituted aromatic or aralkyl groups;B is a divalent aromatic sensitizer which absorbs radiation having a wavelength longer than 300 nm and is capable of transferring an electron to Q,x.sup.- and X'.sup.- are anionic groups; and wherein A provides a spatial separation between Q and M, and B provides a spatial separation between X and X', such that the spatial separation provided by A between Q and M is substantially the same as the spatial separation provided by B between X and X'.Type: GrantFiled: December 9, 1992Date of Patent: September 13, 1994Assignee: E. I. Du Pont de Nemours and CompanyInventors: Arnost Reiser, Xiaohua He
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Patent number: 5229375Abstract: Phosphine oxide-terminated allene-ene-yne compounds are disclosed that possess DNA-cleaving, antimicobial and tumor growth-inhibiting properties. Methods of making and using those compounds are also disclosed.Type: GrantFiled: August 1, 1990Date of Patent: July 20, 1993Assignee: Scripps Clinic and Research FoundationInventors: Peter E. Maligres, Kyriacos C. Nicolaou
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Patent number: 5227498Abstract: Squarylium compounds of the formula: ##STR1## (in which Q.sup.1 and Q.sup.2 are each a chromophoric group having an unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens, R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group, and R.sup.3 and R.sup.4 are each independently a hydrogen atom, or an aliphatic, cycloaliphatic, aromatic or heterocyclic group, or one of R.sup.3 and R.sup.4 is a hydrogen atom and the other is an organosulfonyl group, or R.sup.3 and R.sup.4 together with the intervening nitrogen atom form a cycloaliphatic or aromatic ring) are useful as near infra-red absorbers.Type: GrantFiled: November 20, 1991Date of Patent: July 13, 1993Assignee: Polaroid CorporationInventors: John W. Lee, Donald A. McGowan, Mark R. Mischke, Socorro M. Ramos, Stephen J. Telfer
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Patent number: 5227499Abstract: Squarylium compounds of the formula: ##STR1## in which: Q.sup.1 and Q.sup.2 are each a Chromophoric group having an unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens;R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group; andR.sup.3, R.sup.4 and R.sup.5 are each independently a hydrogen atom, or an aliphatic, cycloaliphatic, aromatic or heterocyclic group, or an electron-withdrawing group able to lower the electron density at the carbon atom to which it is attached, subject to the provisoes that:two of R.sup.3, R.sup.4 and R.sup.5 may form a divalent group of which a single atom is double bonded to the carbon atom to which the two groups are attached, or all three of R.sup.3, R.sup.4 and R.sup.Type: GrantFiled: November 20, 1991Date of Patent: July 13, 1993Assignee: Polaroid CorporationInventors: Donald A. McGowan, Mark R. Mischke, Stephen J. Telfer
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Patent number: 5204334Abstract: Benzoheterocyclylalkylaminoalkanediphosphonic acids of formula I ##STR1## wherein R.sub.1 and R.sub.2, independently of one another, are hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, R.sub.3 is hydrogen or lower alkyl, X and Y, independently of one another, are oxy or thio, alk.sub.1 and alk.sub.2 are identical or different lower alkylene radicals, n is 0 or 1 and m and m', independently of one another, are 0, 1 or 2, the sum of n, m and m' being 1, 2 or 3, and their salts exhibit a pronounced regulatory action on the calcium metabolism of warm-blooded animals. They are prepared, for example, as follows: in a compound of the formula ##STR2## wherein R.sub.1, R.sub.2, n, m, m', X, Y, alk.sub.1 and alk.sub.2 are as defined above, R'.sub.3 is one of the groups R.sub.3 mentioned above or is an amino-protecting group R.sub.0, Z.sub.1 is a functionally modified phosphono group, and Z.sub.2 is a free or functionally modified phosphono group, converting functionally modified phosphono Z.sub.Type: GrantFiled: September 25, 1991Date of Patent: April 20, 1993Assignee: Ciba-Geigy CorporationInventors: Wolfgang Frostl, Knut A. Jaeggi
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Patent number: 5158943Abstract: A sulfur-containing hetrocyclic compound of the formula (I) ##STR1## wherein the ring A is an optionally substituted benzene ring, R is a hydrogen atom or an optionally substituted hydrocarbon residue, B is a carboxyl group which may be esterified or amidated, X is --CH(OH)-- or --CO--, and n is an integer of 0, 1 or 2, or its salt, which is useful in the prevention or treatment of osteoporosis.Type: GrantFiled: May 23, 1991Date of Patent: October 27, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Iwao Yamazaki
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Patent number: 5145990Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 is C.sub.2- C.sub.12 linear or branched unsubstituted alkyl; C.sub.1- C.sub.12 linear or branched substituted alkyl; C.sub.2 -C.sub.12 linear or branched monoalkenyl; C.sub.2 -C.sub.12 linear or branched alkynyl; C.sub.7 -C.sub.20 aralkyl, wherein the alkyl chain is linear or branched C.sub.1- C.sub.8 and the aryl moiety is C.sub.6- C.sub.12 ; C.sub.4- C.sub.10 cycloalkylalkyl; C.sub.3- C.sub.7 cycloalkyl; wherein these values for R.sub.1, other than C.sub.2- C.sub.12 linear or branched unsubstituted alkyl, can be substituted by one or more of C.sub.1 -C.sub.4 alkoxy, C.sub.3- C.sub.6 cycloalkyloxy, C.sub.3- C.sub.6 cycloalkylthio, C.sub.6- C.sub.12 aryloxy, C.sub.1- C.sub.4 alkylthio, C.sub.6- C.sub.12 arylthio, C.sub.7- C.sub.10 aralkyloxy, C.sub.7- C.sub.16 aralkyl-thio; and R.sub.5 is H or C.sub.1- C.sub.12 linear or branched alkyl; C.sub.2- C.sub.12 linear or branched monoalkenyl; C.sub.7- C.sub.Type: GrantFiled: January 9, 1991Date of Patent: September 8, 1992Assignee: Merck & Co., Inc.Inventors: William H. Parsons, William R. Schoen, Arthur A. Patchett
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Patent number: 5104985Abstract: Novel labdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: May 28, 1991Date of Patent: April 14, 1992Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Raymond W. Kosley, Jr., Robert J. Cherill
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Patent number: 5091527Abstract: The present invention provides phospholipase substrates of the general formula: ##STR1## wherein A is an alkylene or alkenylene radical containing up to 16 carbon atoms, R is a hydrgen atom or an alkyl, alkenyl or acyl radical containing up to 20 carbon atoms or an optionally alkyl-substituted aryl or aralkyl radical containing up to 8 carbon atoms in the alkyl moiety, X is the residue of an aromatic hydroxy or thiol compound and each Y, independently of one another, is an oxygen or sulphur atom and Z is --SO.sub.3.sup..crclbar. or a radical of the general formula: ##STR2## wherein R.sup.1 can be a hydrogen atom or a radical of the general formula --(CH.sub.2).sub.n NR.sub.3.sup.2, in which n is 2, 3 or 4 and R.sup.2 is a hydrogen atom or a methyl radical, or is an inositol or serine (--CH.sub.2 --CH(NH.sub.2)--COOH) or glycerol residue.The present invention also provides a process for the optical determination of phospholipases using these substrates, as well as a reagent containing them.Type: GrantFiled: March 2, 1989Date of Patent: February 25, 1992Assignee: Boehringer Mannheim GmbHInventors: Martina Junius, Ulrich Neumann, Herbert von der Eltz
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Patent number: 5071841Abstract: The present invention provides a sulfur-containing heterocyclic compound of the formula (I) ##STR1## wherein ring A is a benzene ring which may be substituted; R is a hydrogen atom or a hydrocarbon group which may be substituted; B is a carboxyl group which may be esterified or amidated; X is --CH(OH)-- or --CO--; k is 0 or 1; and k' is 0, 1 or 2 or a pharmaceutically acceptable salt thereof.Also, it provides a process for producing the compound (I) or a salt thereof and a pharmaceutical preparation for use in the treatment of osteoporosis comprising the compound (I) or salt thereof.The compounds (I) and salts thereof show excellent bone resorption inhibitory activity.Type: GrantFiled: December 28, 1989Date of Patent: December 10, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Masao Tsuda, Iwao Yamazaki
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Patent number: 5013827Abstract: Triggerable dioxetanes with a fluorescent molecule containing group bonded or tethered in the dioxetane so as to produce fluorescence from the group are described. The compounds are useful in immunoassays and in probes using enzymes or other chemicals for triggering the dioxetanes to produce light from the fluorescent molecule in the group as a signal.Type: GrantFiled: November 13, 1989Date of Patent: May 7, 1991Assignee: Board of Governors of Wayne State UniversityInventor: Arthur P. Schaap
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Patent number: 4948418Abstract: This invention pertains to novel heterocyclic 2,3-dihydrobenzofuran and chromane compounds, including stereoisomers, agriculturally suitable compositions containing them, and their use as broad spectrum herbicides.Type: GrantFiled: August 30, 1989Date of Patent: August 14, 1990Assignee: E. I. Du Pont de Nemours and CompanyInventor: Joseph E. Semple
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Patent number: 4933472Abstract: Substituted aminomethylenebis(phosphonic acid) derivatives represented by the general formula: ##STR1## in which R.sup.1, R.sup.2 R.sup.3 and R.sup.4 may be the same or different, each represents a hydrogen atom or a lower alkyl group; "m" is zero or represents an integer from 1 to 4; and a ring "A" represents a cycloalkenyl group having 5 to 8 carbon atoms, a bicycloheptyl group, a bicycloheptenyl group or a saturated heterocyclic group having 4 to 7 carbon atoms and containing an oxygen atom, a sulfur atom, a sulfinyl group (--SO--) or a sulfonyl group (--SO.sub.2 --),or pharmaceutically acceptable salts thereof.Type: GrantFiled: April 5, 1989Date of Patent: June 12, 1990Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Yasuo Isomura, Makoto Takeuchi, Shuichi Sakamoto, Tetsushi Abe
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Patent number: 4897402Abstract: Novel HMG-CoA reductase inhibitors are useful as antihypercholesterolemic agents and are represented by stuctural formulae (I) and (II): ##STR1## wherein A is O, S(O).sub.n or N--R.sub.13.Type: GrantFiled: June 29, 1988Date of Patent: January 30, 1990Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman
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Patent number: 4876247Abstract: The invention relates to methylenediphosphonic acid derivatives of the formula: ##STR1## in which: R.sub.1 represents:a C.sub.1 -C.sub.6 alkyl group,a C.sub.5 -C.sub.7 cycloalkyl group,a phenyl group optionally monosubstituted or polysubstituted by a halogen, a C.sub.1 -C.sub.6 alkyl group or a trifluoromethyl group, ora 5-membered or 6-membered heterocycle containing 1 or 2 heteroatoms chosen from nitrogen and sulfur,Alk denotes a linear or branched C.sub.1 -C.sub.6 alkylene group,R.sub.2 represents hydrogen, a C.sub.1 -C.sub.6 alkyl group or a --CONH.sub.2 group,R.sub.3 represents hydrogen, a C.sub.1 -C.sub.6 alkyl group, a benzyl group or a phenyl group optionally substituted by chlorine or methyl groups; or alternativelyR.sub.2 and R.sub.3, taken together, represent a (CH.sub.2).sub.m group, in which m=4 or 5, and finallyn represents 0 or the integer 1 or 2.These derivatives possess antirheumatic properties.Type: GrantFiled: October 30, 1987Date of Patent: October 24, 1989Assignee: SanofiInventors: Alain Barbier, Jean-Claude Breliere, Georges Garcia
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Patent number: 4814325Abstract: Dithiacycloalkenyl phosphoric esters of the following formula are effective for the control of soil and foliar insects, acarids and nematodes: ##STR1## wherein R.sub.1 is lower alkyl;R.sub.2 is lower alkoxy or lower alkylthio;R.sub.3 is hydrogen, lower alkyl or phenyl;R.sub.4, R.sub.5 and R.sub.6 are independently hydrogen or lower alkyl;Z is oxygen or sulfur;x is 0 or 1;y is 0, 1 or 2; andn is 0, 1 or 2.Type: GrantFiled: September 17, 1986Date of Patent: March 21, 1989Assignee: FMC CorporationInventors: Richard B. Phillips, David M. Roush
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Patent number: 4681954Abstract: Dibenzopyrone derivatives which possess depressant and/or antihypoxia activity are 7,8,9,10-tetrahydro-6-oxo-6H-dibenzo[b,d]pyranyloxy-propanes having the formula (1): ##STR1## where R represents hydrogen or (C.sub.1 -C.sub.4) alkyl; where A represents chlorine or hydroxyl; and where B represents hydrogen, (C.sub.1 -C.sub.4) alkyl, 7-coumarinyl, phosphono, phenyl, or phenyl substituted with amino, dimethylamino, hydroxyl methoxyl, carboxyl, carboxymethyl, or 2-carboxyethenyl. Also included are pharmaceutically acceptable salts of the compounds.Compounds of this invention are useful as sedatives or for the protection of warm blooded animals from the effects of oxygen depreviation.Type: GrantFiled: October 7, 1985Date of Patent: July 21, 1987Assignee: Pennwalt CorporationInventor: Ronald C. Griffith
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Patent number: 4640929Abstract: A novel 1,3-dithiane of the formula ##STR1## wherein R.sup.1 is a di-substituted amino group; R.sup.2 and R.sup.3 are such that one of them is an electron-withdrawing group with the other being a hydrogen atom, a hydrocarbon group or heterocyclic group of the class consisting of thienyl, triazolyl, and pyridyl, which may optionally be substituted or that R.sup.2 and R.sup.3 taken together with the adjacent carbon atom form a spiro ring provided that at least one of R.sup.2 and R.sup.3 is a carbonyl group; X.sup.1 and X.sup.2 each is a sulfur atom and at least one of X.sup.1 and X.sup.2 may be oxidized, or a salt thereof, possesses very useful pesticidal actions.Type: GrantFiled: August 23, 1983Date of Patent: February 3, 1987Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroyuki Mitsudera, Kazuo Konishi, Yasuo Sato
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Patent number: 4617295Abstract: Oxime N-alkyl-N-.alpha.-(alkylthio-phosphorothio)acyl carbamates represented the structure: ##STR1## wherein the R represents various imino radicals, Q is oxygen or sulfur and the numbered R groups represent various alkyl substituents, which exhibit superior insecticidal and miticidal activity.Type: GrantFiled: October 3, 1985Date of Patent: October 14, 1986Assignee: Union Carbide CorporationInventor: Themistocles D. J. D'Silva
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Patent number: 4568671Abstract: Oxime N-alkyl-N-.alpha.-(alkylthio-phosphorothio)acyl carbamates represented the structure: ##STR1## wherein the R represents various imino radicals, Q is oxygen or sulfur and the numbered R groups represent various alkyl substituents, which exhibit superior insecticidal and miticidal activity.Type: GrantFiled: June 30, 1983Date of Patent: February 4, 1986Assignee: Union Carbide CorporationInventor: Themistocles D. J. D'Silva
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Patent number: 4545991Abstract: Difficidin and derivative antibacterial compounds of the formula: ##STR1## where R.sub.a and R.sub.b are members independently selected from the group consisting of hydrogen; alkali metal and alkaline earth metal cations; ammonium; and substituted ammonium; and R.sup.1 is hydrogen or hydroxy.Type: GrantFiled: June 13, 1983Date of Patent: October 8, 1985Assignee: Merck & Co., Inc.Inventors: Sheldon B. Zimmerman, Kenneth E. Wilson, Richard L. Monaghan, Sagrario M. Del Val, Maria I. M. Fernandez, Otto D. Hensens, James E. Flor, Cheryl Deriso
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Patent number: 4522942Abstract: A compound of the formula: ##STR1## wherein R.sub.1 is a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a lower cycloalkyl group, a lower cycloalkyl(lower)alkyl group, a halo(lower)alkyl group, a lower alkoxy(lower)alkyl group, a di(lower)alkoxy(lower)alkyl group, a cyano(lower)alkyl group, a lower alkylthio(lower)alkyl group, a lower alkynylthio(lower)alkyl group, a lower dioxothiacycloalkyl group, a lower thiacycloalkyl group, a lower oxacycloalkyl group, a lower oxacycloalkyl(lower)alkyl group or a thienyl(lower)alkyl group, R.sub.2 is a lower alkyl group and R.sub.3 is a 3,5-dimethoxyphenyl group, a 3,4-methylenedioxyphenyl group or a 4,5-methylenedixoy-2-nitrophenyl group, which is useful as a fungicide.Type: GrantFiled: June 2, 1983Date of Patent: June 11, 1985Assignee: Sumitomo Chemical Company, LimitedInventors: Hideo Kohsaka, Sasaki Mitsuru, Yukio Ishiguri
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Patent number: 4522693Abstract: Acylphosphine sulfides of the formula ##STR1## where R.sup.1 is alkyl, cycloalkyl or an unsubstituted or substituted phenyl, naphthyl or heterocyclic radical; R.sup.2 has the meaning of R.sup.1 and can be identical to or different from R.sup.1, or is alkoxy, unsubstituted or substituted phenoxy or phenoxyalkyl, or R.sup.1 or R.sup.2 are linked together to form a ring, which may contain further alkyl substituents and fused-on benzene rings; R.sup.3 is alkyl, a cycloaliphatic radical, substituted phenyl, an unsubstituted or substituted naphthyl or heterocyclic radical or the group ##STR2## where X is unsubstituted or substituted phenylene or an aliphatic or cycloaliphatic divalent radical; and where one or more of R.sup.1, R.sup.2 and R.sup.3 may be olefinically unsaturated.These acylphosphine sulfides can be prepared from acylphosphines and sulfur and can be used as photoinitiators in photopolymerizable compositions.Type: GrantFiled: June 2, 1983Date of Patent: June 11, 1985Assignee: BASF AktiengesellschaftInventors: Andreas Henne, Anton Hesse, Guenter Heil, Gunnar Schornick
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Patent number: 4522817Abstract: A fungicidal composition which comprises as an active ingredient a fungicidally effective amount of a phosphoramidothionate of the formula: ##STR1## wherein R.sub.1 is a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a lower cycloalkyl group, a lower cycloalkyl(lower)alkyl group, a halogen atom-substituted lower alkyl group, a lower alkoxy(lower)alkyl group, a di(lower)alkoxy(lower)alkyl group, a cyano group-substituted lower alkyl group, a lower alkylthio(lower)alkyl group, a lower dioxothiacycloalkyl group, a lower thiacycloalkyl group, a lower oxacycloalkyl group, a furanyl(lower)alkyl group or a thiophenyl(lower)alkyl group, R.sub.2 is a lower alkyl group and R.sub.3 is a lower alkyl group or a lower alkoxy group, and an inert carrier or diluent.Type: GrantFiled: March 14, 1983Date of Patent: June 11, 1985Assignee: Sumitomo Chemical Company, LimitedInventors: Hideo Kohsaka, Mitsuru Sasaki, Yukio Ishiguri