Phosphorus Attached Directly Or Indirectly To Morpholine Ring By Nonionic Bonding Patents (Class 544/157)
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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: 5962440Abstract: Novel cyclic phosphonate ester inhibitors of MTP are provided which have the structure ##STR1## wherein R.sup.2, L.sup.2, A, B, L.sup.1, R.sup.1 and R.sup.5a are as set out herein. These compounds are useful in lowering serum cholesterol and triglycerides.Type: GrantFiled: October 20, 1998Date of Patent: October 5, 1999Assignee: Bristol-Myers Squibb CompanyInventor: Richard B. Sulsky
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Patent number: 5932733Abstract: The present invention discloses peptide aldehydes having a lactam group as part of the peptide backbone and having an original mimic group such as an amidinopiperidine or amidinophengyl tail. These compounds are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.Type: GrantFiled: June 7, 1995Date of Patent: August 3, 1999Assignee: Corvas International, Inc.Inventors: Joseph E. Semple, Odile E. Levy, Ruth F. Nutt, William C. Ripka
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Patent number: 5929236Abstract: Disclosed are compounds of the formula I wherein:Y represents --CO.sub.2 H, --CO.sub.2 R.sup.6, --C(O)NHR.sup.7, --SO.sub.2 H, --SO.sub.3 H, --SO.sub.3 R.sup.6, --SO.sub.2 NHR.sup.7, --C(O)--N(OH)--R.sup.8, or a group of the formula ##STR1## or a pharmaceutically acceptable addition salt or solvate thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I. Further disclosed is a method for treating or preventing respiratory depression, epileptic seizures or other central nervous system disorders, and for enhancing cognitive performance, by administering an effective amount of a compound of Formula I.Type: GrantFiled: September 22, 1995Date of Patent: July 27, 1999Assignee: Schering CorporationInventors: Shen-Chun Kuo, David J. Blythin, William Kreutner
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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: 5639732Abstract: The present invention is directed to novel phosphorous-containing inhibitors of cysteine or serine proteases. Methods for the use of the protease inhibitors are also described.Type: GrantFiled: July 10, 1996Date of Patent: June 17, 1997Assignee: Cephalon, Inc.Inventors: John P. Mallamo, Ron Bihovsky, Ming Tao, Gregory J. Wells
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Patent number: 5627173Abstract: Phosphonoacetic acid derivatives and their use for treating degenerative joint disorders Compounds of the formula I ##STR1## are suitable for producing pharmaceuticals for the treatment and prophylaxis of degenerative joint disorders, of rheumatic disorders accompanied by cartilage breakdown, such as rheumatoid arthritis, joint trauma and chondrolysis as a consequence of prolonged immobilization of the joint, of inflammations, septic shock, disorders with impaired leukocyte adhesion, disorders caused by an elevated concentration of tumor necrosis factor alpha, such as cachexia or Crohn's disease.Type: GrantFiled: January 23, 1996Date of Patent: May 6, 1997Assignee: Hoechst AktiengesellschaftInventors: Rolf Graeve, Werner Thorwart, Ruth Raiss, Klaus U. Weithmann, Stefan M ullner
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Patent number: 5532226Abstract: Novel benzylphosphonate compounds of the general formula I: ##STR1## are disclosed as useful in treating bone wasting diseases including postmenopausal osteoporosis in increasing in mammals bone formation and bone mass.Type: GrantFiled: December 9, 1993Date of Patent: July 2, 1996Assignee: Ortho Pharmaceutical CorporationInventors: Keith Demarest, Charles Schwender, David Wustrow
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Patent number: 5457094Abstract: Compounds of formula I ##STR1## wherein R, R.sub.1, R.sub.2 and q are as defined in the description, have valuable pharmacological properties and are especially effective as calcium metabolism regulators. They are prepared in a manner known per se.Type: GrantFiled: February 7, 1995Date of Patent: October 10, 1995Assignee: Ciba-Geigy CorporationInventor: Knut A. Jaeggi
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Patent number: 5442101Abstract: The invention relates to novel methylenebisphosphonic acid ester amide derivatives of general formula (I), in which formula W.sup.1, W.sup.2, W.sup.3 and W.sup.4 are independently the group OR.sup.1 or the group NR.sup.2 R.sup.3 wherein R.sup.1, R.sup.2 and R.sup.3 independently are hydrogen or straight or branched, optionally unsaturated C.sub.1 -C.sub.22 -alkyl, optionally substituted, optionally unsaturated C.sub.3 -C.sub.10 -cycloalkyl, aryl, aralkyl or silyl SiR.sub.3, or the groups R.sup.2 and R.sup.3 form together with the adjacent nitrogen atom a 3 to 10-membered saturated, partly saturated or aromatic heterocyclic ring, wherein in addition to the nitrogen atom, there may be one or two heteroatoms from the group N, O and S, provided that in formula (I) at least one of the groups W.sup.1, W.sup.2, W.sup.3 and W.sup.4 is hydroxy and at least one of the groups W.sup.1, W.sup.2, W.sup.3 and W.sup.4 is amino group NR.sup.2 R.sup.3, Q.sup.1 and Q.sup.Type: GrantFiled: October 20, 1993Date of Patent: August 15, 1995Assignee: Leiras OyInventors: Hannu Hanhijarvi, Heikki Nupponen, Jouko Vepsalainen, Esko Pohjala
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Patent number: 5403932Abstract: Compounds of the formula: ##STR1## which is further defined herein, possess anti-tumor activity.Type: GrantFiled: June 15, 1994Date of Patent: April 4, 1995Assignee: Research Corporation Technologies, Inc.Inventors: Richard F. Borch, Gregory W. Canute, Ronald R. Valente
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Patent number: 5360563Abstract: There are disclosed compounds of formulae I and Ia ##STR1## wherein R.sub.1 and R.sub.2 are each independently of the other C.sub.1 -C.sub.13 alkyl which may be interrupted by oxygen, C.sub.5 -C.sub.6 cycloalkyl or, together with the linking N-atom, are a group of formula ##STR2## R is hydrogen or methyl, R.sub.3 is hydrogen or C.sub.1 -C.sub.13 alkyl, andR.sub.4 and R.sub.5 are each independently of the other hydrogen, C.sub.1 -C.sub.18 alkyl which may be interrupted by oxygen, C.sub.5 -C.sub.6 cycloalkyl or, together with the linking N-atom, are a group of formula ##STR3## withe proviso that R.sub.3, R.sub.4 and R.sub.5 are not simultaneously hydrogen and HNR.sub.1 R.sub.2 are not identical with NR.sub.3 R.sub.4 R.sub.5.The compounds are suitable for use as lubricant additives.Type: GrantFiled: May 27, 1993Date of Patent: November 1, 1994Assignee: Ciba-Geigy CorporationInventors: Horst Zinke, Rolf Schumacher
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Patent number: 5332845Abstract: Novel phosphorylating reagents are provided which are useful in DNA synthesis and purification procedures. The reagents are substituted phosphines which are particularly useful in the phosphorylation of nucleoside and solid supported oligonucleotides at the 5'-hydroxyl position. Phosphorylation using these reagents is easily and accurately monitored colorimetrically.Type: GrantFiled: February 26, 1993Date of Patent: July 26, 1994Assignee: Chiron CorporationInventors: Michael S. Ureda, Thomas Horn
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Patent number: 5304549Abstract: Compounds of the formula ##STR1## wherein A is the group ##STR2## R.sup.1 is hydrogen, amino, protected amino, acylamino or lower alkyl optionally substituted by aryl, hydroxy, protected hydroxy, amino, protected amino, acylamino, maleimido, succinimido, naphthalimido, 2,3-dihydro-1,3-dioxo-1H-benz[d,e]isoquinol-2-yl, carboxy, protected carboxy, carbamoyl, mono(lower alkyl)carbamoyl, di(lower alkyl)carbamoyl, di(lower alkyl)amino, carboxy-lower alkanoylamino, pyrrolidino or morpholino; R.sup.2 is hydrogen or lower alkyl optionally substituted by aryl, amino, protected amino, di(lower alkyl)- amino, guanidino, carboxyl, protected carboxyl, carbamoyl, mono(lower alkyl) carbamoyl, di(lower alkyl)carbamoyl, di(lower alkoxy)phosphinyl, dihydroxyphosphinyl, pyrrolidino, piperidino or morpholino; R.sup.3 is hydrogen or lower alkyl optionally substituted by hydroxy, protected hydroxy, amino or protected amino; R.sup.4 is hydrogen, hydroxy, lower alkoxy or benzyloxy; and R.sup.Type: GrantFiled: January 21, 1992Date of Patent: April 19, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Michael J. Broadhurst, Paul A. Brown, William H. Johnson, Geoffrey Lawton
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Patent number: 5300687Abstract: Novel benzylphosphonate compounds of the general formula I: ##STR1## are disclosed as useful in treating bone wasting diseases including postmenopausal osteoporosis in increasing in mammals bone formation and bone mass.Type: GrantFiled: July 18, 1991Date of Patent: April 5, 1994Assignee: Ortho Pharmaceutical CorporationInventors: Charles Schwender, Keith Demarest, David Wustrow
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Patent number: 5250522Abstract: The present invention relates to the N-phosphonomethyl-biaryl substituted amino acid derivatives of formula I ##STR1## wherein X represents a direct bond, C.sub.1-4 -alkylene or C.sub.2 -C.sub.4 -alkenylene; R and R' represent independently hydrogen, carbocyclic aryl, 6-tetrahydronaphthyl, 5-indanyl, .alpha.-(trichloromethyl, carboxyl, esterified carboxyl or amidated carboxyl)substituted-(lower alkyl or aryl-lower alkyl), acyloxymethyl optionally monosubstituted on methyl carbon by C.sub.1-20 -alkyl, by C.sub.5 -C.sub.7 -cycloalkyl, by aryl or by aryl-lower alkyl; R.sub.1 represents monocyclic carbocyclic or monocyclic heterocyclic aryl; COR.sub.3 represents carboxyl or carboxyl derivatized in form of a pharmaceutically acceptable ester; R.sub.2 and R.sub.Type: GrantFiled: October 9, 1992Date of Patent: October 5, 1993Assignee: Ciba-Geigy CorporationInventor: Stephane De Lombaert
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Patent number: 5217958Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are inhibitors of renin and therefore useful as cardiovascular agents.Type: GrantFiled: April 12, 1990Date of Patent: June 8, 1993Assignee: E. R. Squibb & Sons, Inc.Inventor: Dinesh V. Patel
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Patent number: 5212304Abstract: The compounds of the invention include novel linking agents comprising 2-substituted-3-protected-1,3,2-oxazaphosphacycloalkanes and their phosphoramidite precursors. The compounds of the invention further include conjugates of the above linking agents with oligonucleotides and polymer supports. The compounds of the present invention are useful for linking organic moieties, such as fluorescent or chromogenic dyes, to polymer supports and oligonucleotides, particularly single- and double-stranded DNA and RNA fragments.Type: GrantFiled: July 8, 1988Date of Patent: May 18, 1993Assignee: Applied Biosystems, Inc.Inventors: Steven Fung, Sam L. Woo, Lloyd M. Smith
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Patent number: 5186733Abstract: Herbicides have the formula ##STR1## in which R is hydrogen, mono- or poly-halo, mono- or di-(C.sub.1 -C.sub.4 alkyl), C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, phenoxy or nitro;R.sub.1 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sub.3 is C.sub.1 -C.sub.6 alkyl;R.sub.2 is C.sub.2 -C.sub.4 alkyl, C.sub.3 -C.sub.6 cycloalkyl, phenyl, optionally substituted by C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 haloalkoxy, one or more halogens, or two C.sub.1 -C.sub.4 alkoxy groups, or one C.sub.1 -C.sub.4 alkyl and one C.sub.1 -C.sub.4 alkoxy group, phenyl-(C.sub.1 -C.sub.2)alkyl or pyridyl; orR.sub.1 and R.sub.2, and/or R.sub.3 and R.sub.4 respectively, taken together with the nitrogen atom, form a 4-8 member ring, optionally including an oxygen heteroatom;and R.sub.4 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, phenyl, optionally substituted by C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 haloalkoxy, one or more halogens, or two C.sub.1 -C.sub.Type: GrantFiled: November 12, 1991Date of Patent: February 16, 1993Assignee: Imperial Chemical Industries PLCInventors: Michael D. Broadhurst, Tsze H. Tsang, John Tomko
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Patent number: 5185334Abstract: Novel 2,2-disubstituted glycerol-like compounds are disclosed for use as anti-allergic and anti-inflammatory compounds. The compounds are antagonists of platelet activating factor ("PAF"). Also disclosed are methods of synthesizing and using the compounds of the invention as well as pharmaceutical compositions thereof. The compounds have the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are as defined in the specification.Type: GrantFiled: September 6, 1991Date of Patent: February 9, 1993Assignee: Schering CorporationInventors: Daniel Solomon, James J. Kaminski, Steven K. White, Laura S. Lehman de Gaeta, Ashit K. Ganguly
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Patent number: 5183811Abstract: A novel glycerol derivative which is effective to reduce blood pressure has the formula: ##STR1## wherein R.sup.1 is an alkyl group having 10-22 carbon atoms, R.sup.2 is lower acyl, benzoyl, aryl, mono-, di- or triarylalkyl, alkyl, cycloalkyl, or cycloalkylalkyl; Q is substituted or unsubstituted alkylene containing 1-4 carbon atoms, l is 0 or 1; Y is a nitrogen-containing heterocyclic group or a nitrogen-containing bridged heterocyclic group (--(Q).sub.l -- is attached to a carbon atom contained in a hetero-ring of the heterocyclic group) in which Y is the bridged heterocyclic group where l is 0; and each of R.sup.5, R.sup.6 and R.sup.7 is hydrogen, lower alkyl, aryl or aralkyl.Type: GrantFiled: July 19, 1990Date of Patent: February 2, 1993Assignee: Nippon Chemiphar Co., Ltd.Inventors: Mitsuo Masaki, Hiromitsu Takeda, Toshiro Kamishiro, Masao Yamamoto
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Patent number: 5177095Abstract: Substituted triazoles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I, are useful as angiotensin II antagonists.Type: GrantFiled: August 13, 1991Date of Patent: January 5, 1993Assignee: Merck & Co., Inc.Inventors: William J. Greenlee, Arthur A. Patchett, David Hangauer, Wallace Ashton, Kenneth J. Fitch, Thomas F. Walsh, Ralph A. Rivero, Daljit S. Dhanoa
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Patent number: 5174913Abstract: A corrosion inhibitor with excellent film forming and film persistency characteristics may be produced by first reacting in a condensation reaction a polybasic acid with a polyalcohol to form a partial ester. The partial ester is reacted with imidazoline and/or fatty diamines to salt the ester. If warranted, the salted partial ester may be reacted with a metal hydroxide, a metal oxide, and/or ammonia to further salt the ester. Surfactants may be added to tailor the inhibitor formulation to meet the specific needs of the user (i.e., the corrosion inhibitor may be formulated to produce an oil-soluble, highly water-dispersible corrosion inhibitor or an oil-dispersible, water-soluble corrosion inhibitor). Suitable carrier solvents may be employed where needed to effectively disperse the corrosion inhibitor formulation.Type: GrantFiled: September 20, 1991Date of Patent: December 29, 1992Assignee: Westvaco CorporationInventors: John A. Alford, Paul G. Boyd, Eugene R. Fischer
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Patent number: 5155100Abstract: The invention relates to the N-phosphonomethyl-biaryl substituted dipeptide derivatives of formula I ##STR1## wherein A represents a direct bond, lower alkylene, phenylene or cyclohexylene; m represents 1 or zero, provided that m represents 1 when A is a direct bond; R.sub.2 represents hydrogen, hydroxy, lower alkyl, aryl-lower alkyl, C.sub.5 -C.sub.Type: GrantFiled: May 1, 1991Date of Patent: October 13, 1992Assignee: Ciba-Geigy CorporationInventors: Mark D. Erion, Stephane De Lombaert
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Patent number: 5124322Abstract: Novel compounds of formula (I), salts, solvates and hydrates thereof: ##STR1## in which: R.sub.1 and R.sub.2 are independently hydrogen; alkyl; alkoxy; halogen; or CF.sub.3 ;R.sub.3 is hydrogen; acyl, such as ##STR2## where Z is optionally substituted aryl; or a group R--S-- where R is an organic residue such that the group R--S-- provides an in vivo-cleavable disulphide bond;R.sub.4 is C.sub.3-6 alkyl;R.sub.5 is hydrogen; alkyl; --CH.sub.2 --R.sub.10 where R.sub.10 is optionally substituted phenyl or heteroaryl; or a group ##STR3## where R.sub.11 is hydrogen; alkyl; or --CH.sub.2 --Ph is optionally substituted phenyl; and R.sub.12 is hydrogen or alkyl; andR.sub.6 is hydrogen; alkyl; or a group ##STR4## where R.sub.13 is hydrogen; or alkyl; and R.sub.14 is hydroxy; alkoxy; or --NR.sub.7a R.sub.8 where each of R.sub.7a and R.sub.8 is hydrogen or alkyl, or R.sub.7a and R.sub.Type: GrantFiled: June 19, 1989Date of Patent: June 23, 1992Assignee: Beecham Group p.l.c.Inventor: Ian Hughes
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Patent number: 5091526Abstract: Biologically active, enantiomerically substantially pure intermediates of trans-hexahydro-benzo[d]naphtho[2,1-b]azepines are prepared.The present invention involves a process for preparing compounds of the general formula 3: ##STR1## wherein: R* is ##STR2## Each R.sup.1 is independently H or alkyl; Q is methylene, --O-- or --S--;m and n are independently variable and may each have a value of 0, 1 or 2, with the provisos that the sum of m and n is not greater than 3, that m may not equal zero when Q is --O-- or --S--, and that when Q is --CH.sub.2 --, m and n cannot both be zero;X is hydrogen, halo, alkyl, alkylthio, alkylsulfinyl, alkylsufonyl, hydroxy, alkoxy or trifluoromethyl;Y is hydrogen, hydroxy, alkoxy, --OC(O)NR.sup.2 R.sup.3, --OC(O)--R.sup.9, --N(R.sup.1).sub.2, --NHC(O)R.sup.1 or --OP(O)(OH)OR.sup.1,R.sup.2 and R.sup.3 are the same or different and each is hydrogen (provided that both are not hydrogen), alkyl, aralkyl, cycloalkyl, aryl, hydroxyalkyl, or alkoxyalkyl;in addition, when one of R.sup.Type: GrantFiled: January 8, 1991Date of Patent: February 25, 1992Assignee: Schering CorporationInventors: Joel G. Berger, John W. Clader
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Patent number: 5036152Abstract: Novel alkoxycarbonylalkylphospholipids, alkylaminocarbonylalkylphospholipids, processes for the preparation thereof, and methods for treating inflammation utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: September 5, 1989Date of Patent: July 30, 1991Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Nicholas J. Hrib, Kirk D. Shoger, John J. Tegeler
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Patent number: 5030733Abstract: Novel hydroxy-, alkoxy- and benzyloxy-substituted phospholipids, a process for the preparation thereof, and methods for treating pain, phospholipase, A.sub.2 mediated inflammation and similar conditions utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: June 15, 1989Date of Patent: July 9, 1991Assignee: Hoechst-Roussel Pharmaceticals IncorporatedInventors: John J. Tegeler, Kirk D. Shoger
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Patent number: 4992549Abstract: Aminotriazines of the formula ##STR1## wherein E is nitrogen,Z is oxygen or sulfur,R.sup.3 is hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.4 -alkenyl or C.sub.1 -C.sub.4 -alkoxy,R.sup.4 is hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.2 -C.sub.4 alkoxyalkyl, C.sub.2 -C.sub.4 -alkoxyalkoxy, cyclopropyl, -NH.sub.2, C.sub.1 -C.sub.4 -alkylamino, di-C.sub.1 -C.sub.4 -alkylamino, or a saturated 5- to 7-membered nitrogen heterocycle bound by way of the nitrogen atom and selected from pyrrolidine, piperidine, morpholine, thiomorpholine, piperazine and hexamethyleneimine,R.sup.5 is cyano, --CZ--R.sup.Type: GrantFiled: December 15, 1989Date of Patent: February 12, 1991Assignee: Ciba-Geigy CorporationInventor: Werner Topfl
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Patent number: 4956467Abstract: Novel nucleophilic tertiary organophosphines and the specific cleavage of peptide bonds by nucleophilic tertiary organophosphines. This invention is of particular utility in providing chemical agents for use in the cleavage of proteins and the determination of the amino acid sequence of proteins.Type: GrantFiled: April 5, 1989Date of Patent: September 11, 1990Assignee: American Cyanamid CompanyInventors: Lois M. Hinman, Libby S. Miller
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Patent number: 4940707Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are lower-alkyl; or together are alkylene with 3-5 C-atoms in a straight chain; one of the residues R.sup.3 and R.sup.4 is hydrogen and the other is hydrogen or lower-alkyl; R.sup.6 and R.sup.7 are hydrogen or lower-alkyl; R.sup.5 and R.sup.8 are hydrogen, lower-alkyl, lower-alkoxy or halogen; X signifies --O--, --S--, --SO--, --SO.sub.2 -- or --NR.sup.9 ; R.sup.9 is hydrogen, lower-alkyl or acyl; Y is --S(O).sub.m R.sup.10 or --NHet and, where X is --NR.sup.9 --, --S--, --SO-- or --SO.sub.2 --, also --N(R.sup.11).sub.2 or --OR.sup.12 ; R.sup.10 is lower-alkyl; R.sup.11 and R.sup.12 are hydrogen, lower-alkyl or acyl; --NHet is a 5-8 membered, saturated or unsaturated, monocyclic heterocycle, attached via a N-atom; n is 2, 3 or 4 and m is 0, 1 or 2, are described. The compounds of formula I are useful as agents for the treatment of disorders such as neoplasms, dermatoses or ageing of the skin.Type: GrantFiled: February 14, 1989Date of Patent: July 10, 1990Assignee: Hoffman-La Roche Inc.Inventors: Michael Klaus, Peter Mohr, Ekkehard Weiss
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Patent number: 4935520Abstract: Phospholipids, inclusive of pharmaceutically acceptable salts thereof, of the formula ##STR1## wherein R.sup.1 is a C.sub.8-30 aliphatic hydrocarbon residue, R.sup.2, R.sup.3 and R.sup.4 are independently hydrogen or lower alkyl or ##STR2## represents cyclic ammonio and n is 0 or 1, exhibit inhibitory activity to multiplication of tumor cells and antimycotic (antifungal) and antiprotozoal activities, and are useful for inhibiting multiplication of tumor cells and prolonging the survival time of tumor-bearing warm-blooded animal, for treating or preventing a disease in an animal caused by a mycete (fungus) and for treating or preventing a plant disease.Type: GrantFiled: September 19, 1988Date of Patent: June 19, 1990Assignee: Takeda Chemical Industries, Ltd.Inventors: Shoshichi Nojima, Hiroaki Nomura
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Patent number: 4927835Abstract: Compounds of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof, wherein: R.sup.1 is cycloalkyl of 5 to 7 carbon atoms; aryl of 6 to 10 carbon atoms unsubstituted or substituted by straight or branched chain alkyl of 1 to 4 carbon atoms, halo or trifluoromethyl; or ##STR2## wherein A is oxygen, sulfur or NR.sup.5, wherein R.sup.5 is hydrogen, straight or branched chain alkyl of 1 to 4 carbon atoms or halo, and R.sup.6 is hydrogen, straight or branched chain alkyl of 1 to 4 carbon atoms or halo;R.sup.2 is straight or branched chain alkyl of 1 to 4 carbon atoms or cycloalkyl of 5 to 7 carbon atoms; andR.sup.3 and R.sup.4 are the same or different and each is hydrogen; straight or branched chain alkyl of 1 to 8 carbon atoms unsubstituted or substituted by hydroxy, acyloxy of 2 to 5 carbon atoms, carboxyl or carbamoyl;are useful for treating pain, inflammation and fever in humans and animals.Type: GrantFiled: March 1, 1989Date of Patent: May 22, 1990Assignee: Nippon Shinyaku Co., Ltd.Inventors: Masahiro Kise, Yoshihiko Yoshimoto, Hiroshi Fujisawa, Yasuo Sasaki, Shoji Yasufuku
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Patent number: 4888328Abstract: Novel alkoxycarbonylalkylalkylphospholipids and alkylaminocarbonylalkylphospholipids of the formula ##STR1## wherein A.sup.1 is a bivalent radical of the formula --C.sub.m H.sub.2m --wherein m is an integer having a value from 0 to 20, inclusive; A.sup.2 is a bivalent radical of the formula --C.sub.p H.sub.2p --wherein p is an integer having a value from 2 to 6, inclusive; X is a bivalent radial of the formula --O--or --N(R)--wherein R is selected from the group consisting of hydrogen, alkyl radicals having up to 6 carbon atoms, inclusive and phenyl radicals of the formula: ##STR2## where Z and a are as difined in the specification; Y is ##STR3## wherein R.sup.1 is an anlkyl radicals having up to 6 carbon atoms, inclusive and R.sup.2 and R.sup.3 are independently alkyl radicals having up to 6 carbon atoms, inclusive, or taken together with R.sup.1 and the nitrogen atom to which they are attached form a group of the formula ##STR4## wherein r is 0 or 1, and W is oxygen, CH.sub.2, sulfur or N(R.sup.Type: GrantFiled: March 10, 1988Date of Patent: December 19, 1989Assignee: Hoeschst-Roussel IncorporatedInventors: Nicholas J. Hrib, Kirk D. Shoger, John J. Tegeler
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Patent number: 4855456Abstract: This invention discloses intermediates and a process for the preparation of 6-desmethyl-6-.alpha.-hydroxymethyl derivatives of lovastatin and analogs thereof at the 8-acyl side chain.Type: GrantFiled: February 29, 1988Date of Patent: August 8, 1989Assignee: Merck & Co., Inc.Inventors: Ta Jyh Lee, William F. Hoffman
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Patent number: 4804654Abstract: Compounds of the formula ##STR1## wherein the symbols have assigned meanings, and their use as insecticides and/or miticides.Type: GrantFiled: March 4, 1987Date of Patent: February 14, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventor: Mohamed A. H. Fahmy
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Patent number: 4794183Abstract: Compounds of formula (I): ##STR1## [wherein: m is 1-3; A and B are oxygen or sulfur; and one of R.sup.1 and R.sup.2 is C.sub.10 -C.sub.22 alkyl and the other is a group of formula (II). ##STR2## where: n is 2 or 3; and --NR.sup.3 R.sup.4 R.sup.5 is an amino group] and salts thereof are effective anti-cancer agents.Type: GrantFiled: January 14, 1986Date of Patent: December 27, 1988Assignee: Sankyo Company LimitedInventors: Norio Nakamura, Hideki Miyazaki, Fusaaki Shimizu, Kazuhiko Sasagawa
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Patent number: 4776875Abstract: Compounds of the formula ##STR1## in which R.sub.1 and R.sub.2 denote alkyl, OH, CF.sub.3 or cyanoethyl, A preferably denotes --COOH, R.sub.3 denotes inter alia alkoxycarbonylalkoxy, fairly high-molecular (>C.sub.12) alkoxy, alkylcarbonylalkoxy or nitrobenzyloxy, are valuable herbicides and growth regulators.Type: GrantFiled: March 26, 1986Date of Patent: October 11, 1988Assignee: Hoechst AktiengesellschaftInventors: Heinz J. Loher, Klaus Bauer, Hermann Bieringer
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Patent number: 4652297Abstract: This invention relates to a new class of organic chemical compounds. More particularly, this invention is concerned with amido and hydrazido derivatives of N-phosphinothioylmethylglycine esters. This class of compounds has been found to be useful as herbicides.Type: GrantFiled: February 25, 1982Date of Patent: March 24, 1987Assignee: Monsanto CompanyInventors: John E. Franz, Robert J. Kaufman
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Patent number: 4650791Abstract: A novel phospholipid of the formula: ##STR1## wherein R.sup.1 is an alkyl group of 10 to 24 carbon atoms, R.sup.2 is a cyclic imide group and A.sup.+ is a cyclic ammonio group and a salt thereof have platelet activating factor inhibiting activity and are useful for prevention and treatment of circulatory disorders and allergic bronchial asthma.Type: GrantFiled: January 8, 1985Date of Patent: March 17, 1987Assignee: Takedo Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Kohei Nishikawa, Susumu Tsushima
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Patent number: 4649203Abstract: Novel ketoalkylphospholipids, inclusive of salts thereof, of the formula ##STR1## wherein R.sup.1 is an aliphatic hydrocarbon residue containing 10 to 20 carbon atoms,R.sup.2 is hydrogen or methoxy, andR.sup.3, R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1-5 alkyl, or ##STR2## represents a cyclic ammonio group, exhibit inhibitory activity against multiplication of tumor cells and antifungal activity.Type: GrantFiled: March 27, 1986Date of Patent: March 10, 1987Assignee: Takeda Chemical Industries, Ltd.Inventors: Shoshichi Nojima, Hiroaki Nomura, Susumu Tsushima
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Patent number: 4629491Abstract: The invention relates to novel urease inhibited fertilizer compositions containing urea and a urease inhibiting amount of one or more diaminophosphinyl compounds having oxidized sulfur functions, and methods and composition for inhibiting the activity of urease through use of such compounds.Type: GrantFiled: December 20, 1983Date of Patent: December 16, 1986Assignee: Allied CorporationInventors: Michael D. Swerdloff, Milorad M. Rogic, Larry L. Hendrickson
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Patent number: 4624695Abstract: The invention relates to novel urease inhibited fertilizer compositions containing urea and a urease inhibiting amount of one or more o-diaminophosphinyl derivatives of oximes, and methods and composition for inhibiting the activity of urease through use of such compounds.Type: GrantFiled: December 20, 1983Date of Patent: November 25, 1986Assignee: Allied CorporationInventors: Michael D. Swerdloff, Milorad M. Rogic, Larry L. Hendrickson
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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: 4608367Abstract: .gamma.-Pyrone phosphoric ester derivative represented by the general formula below is useful as an effective component of an insecticidal or miticidal composition for agricultural and horticultural uses. ##STR1## wherein R.sup.1 is hydrogen, lower alkyl group, lower alkenyl group, cycloalkyl group or phenyl group, R.sup.2 is hydrogen or lower alkyl group unsubstituted or substituted with halogen atom, A is --SR.sup.3 or --NR.sup.4 R.sup.5, B is OR.sup.6, R.sup.3 being lower alkyl group, cycloalkyl group or phenyl group, R.sup.4 being hydrogen or lower alkyl group, R.sup.5 being lower alkyl group, lower alkenyl group, cycloalkyl group, phenyl group or benzyl group, R.sup.4 and R.sup.5 may link to form piperidino or morpholino group, R.sup.6 being lower alkyl group, cycloalkyl group or phenyl group, Y is oxygen or sulfur atom.Type: GrantFiled: July 25, 1985Date of Patent: August 26, 1986Assignee: Otsuka Kagaku Kabushiki KaishaInventors: Yoshinori Endo, Hisashi Takao
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Patent number: 4605647Abstract: New oxaazaphosphorine compounds corresponding to the formula: ##STR1## in which R is alkyl, cycloalkyl or alkoxy,phenyl, phenylalkyl, phenoxy or thiophenoxy in which the phenyl ring may be substituted by alkyl or alkoxy or by halogen.mono- or di-alkylamino optionally mono- or di-substituted by halogen, orpyrrolidinyl, piperidyl or morpholinyl or optionally substituted piperazinyl.These compounds may be used for antineoplastic therapy especially in the treatment of tumors.Type: GrantFiled: July 5, 1985Date of Patent: August 12, 1986Assignee: ADIR, S.A.R.L.Inventors: Gilbert Lavielle, Claude Cudennec
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Patent number: 4588714Abstract: Compounds and compositions containing them, for insecticidal control having the formula ##STR1## in which R.sub.1 is an alkyl group having from 1 to 3 carbon atoms, R.sub.2 is an alkyl group having from 1 to 6 carbon atoms, and R.sub.3 and R.sub.4 are independently alkyl groups having from 1 to 6 carbon atoms, or R.sub.3 and R.sub.4 taken together form a ring having the formula ##STR2## in which m and n are each integers from 1 to 3 and X is oxygen or --CH.sub.2 --, together with insecticidal compositions containing such compounds, and methods for controlling insects.Type: GrantFiled: January 3, 1984Date of Patent: May 13, 1986Assignee: Stauffer Chemical CompanyInventors: William G. Haag, Charles G. Chavdarian
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Patent number: 4579956Abstract: Amino-phosphonates are prepared by reacting an enamine with a phosphite ester, for example, according to the equation ##STR1## where OR' is an alcohol moiety and NR.sub.2 is an amino moiety, both R and R' being preferably hydrocarbon such as alkyl or R.sub.2 is part of a ring structure. These compounds have many uses, for example, as corrosion inhibitors, scale inhibitors, fuel stabilizers, etc. In addition, amino-phosphonates can be converted to alpha, beta - unsaturated phosphonates according to the equation ##STR2## which are useful in forming flame retardant polymers and copolymers.Type: GrantFiled: October 20, 1978Date of Patent: April 1, 1986Assignee: Petrolite CorporationInventor: Derek Redmore
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Patent number: 4576933Abstract: Glycerol derivatives, inclusive of salts thereof, of the formula ##STR1## wherein R.sup.1 is alkyl or alkylcarbamoyl containing 10 to 30 carbon atoms, R.sup.2 and R.sup.3 are independently hydrogen, C.sub.1-6 alkyl or, taken together with the adjacent nitrogen atom, form cyclic amino, and ##STR2## represents cyclic ammonio, and of the formula ##STR3## wherein R.sup.1 is as defined above, R.sup.2' and R.sup.3' are C.sub.1-6 alkyl or, taken together with the adjacent nitrogen atom, form cyclic amino and R.sup.4', R.sup.5' and R.sup.6' are independently hydrogen or C.sub.1-6 alkyl, are useful as antihypertensive agents.Type: GrantFiled: April 29, 1983Date of Patent: March 18, 1986Assignee: Takeda Chemical Industries, Ltd.Inventors: Susumu Tsushima, Kohei Nishikawa
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Patent number: RE33489Abstract: Sterically hindered cyclic amines which are substituted by a photoactivatable acyl group at the basic nitrogen atom can be deacylated by irradiation with UV light. This is advantageous if the basicity of the amines proves troublesome during application. Examples of such photoactivatable acyl groups are phenylglyoxyl, phenylacetyl or naphthylacetyl groups.Type: GrantFiled: September 25, 1989Date of Patent: December 11, 1990Assignee: Ciba-Geigy CorporationInventors: Godwin Berner, Mario Slongo