Phosphorus Attached Directly Or Indirectly To Morpholine Ring By Nonionic Bonding Patents (Class 544/157)
  • Patent number: 5962437
    Abstract: 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: Grant
    Filed: May 2, 1997
    Date of Patent: October 5, 1999
    Assignee: Wake Forest University
    Inventors: Louis S. Kucera, Susan L. Morris-Natschke, Khalid S. Ishaq
  • Patent number: 5962440
    Abstract: 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: Grant
    Filed: October 20, 1998
    Date of Patent: October 5, 1999
    Assignee: Bristol-Myers Squibb Company
    Inventor: Richard B. Sulsky
  • Patent number: 5932733
    Abstract: 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: Grant
    Filed: June 7, 1995
    Date of Patent: August 3, 1999
    Assignee: Corvas International, Inc.
    Inventors: Joseph E. Semple, Odile E. Levy, Ruth F. Nutt, William C. Ripka
  • Patent number: 5929236
    Abstract: 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: Grant
    Filed: September 22, 1995
    Date of Patent: July 27, 1999
    Assignee: Schering Corporation
    Inventors: Shen-Chun Kuo, David J. Blythin, William Kreutner
  • Patent number: 5914351
    Abstract: 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: Grant
    Filed: December 12, 1997
    Date of Patent: June 22, 1999
    Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./CIE.
    Inventors: Walter Gerhard Brouwer, Ewa Maria Osika
  • Patent number: 5639732
    Abstract: 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: Grant
    Filed: July 10, 1996
    Date of Patent: June 17, 1997
    Assignee: Cephalon, Inc.
    Inventors: John P. Mallamo, Ron Bihovsky, Ming Tao, Gregory J. Wells
  • Patent number: 5627173
    Abstract: 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: Grant
    Filed: January 23, 1996
    Date of Patent: May 6, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Rolf Graeve, Werner Thorwart, Ruth Raiss, Klaus U. Weithmann, Stefan M ullner
  • Patent number: 5532226
    Abstract: 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: Grant
    Filed: December 9, 1993
    Date of Patent: July 2, 1996
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Keith Demarest, Charles Schwender, David Wustrow
  • Patent number: 5457094
    Abstract: 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: Grant
    Filed: February 7, 1995
    Date of Patent: October 10, 1995
    Assignee: Ciba-Geigy Corporation
    Inventor: Knut A. Jaeggi
  • Patent number: 5442101
    Abstract: 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: Grant
    Filed: October 20, 1993
    Date of Patent: August 15, 1995
    Assignee: Leiras Oy
    Inventors: Hannu Hanhijarvi, Heikki Nupponen, Jouko Vepsalainen, Esko Pohjala
  • Patent number: 5403932
    Abstract: Compounds of the formula: ##STR1## which is further defined herein, possess anti-tumor activity.
    Type: Grant
    Filed: June 15, 1994
    Date of Patent: April 4, 1995
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Richard F. Borch, Gregory W. Canute, Ronald R. Valente
  • Patent number: 5360563
    Abstract: 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: Grant
    Filed: May 27, 1993
    Date of Patent: November 1, 1994
    Assignee: Ciba-Geigy Corporation
    Inventors: Horst Zinke, Rolf Schumacher
  • Patent number: 5332845
    Abstract: 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: Grant
    Filed: February 26, 1993
    Date of Patent: July 26, 1994
    Assignee: Chiron Corporation
    Inventors: Michael S. Ureda, Thomas Horn
  • Patent number: 5304549
    Abstract: 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: Grant
    Filed: January 21, 1992
    Date of Patent: April 19, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael J. Broadhurst, Paul A. Brown, William H. Johnson, Geoffrey Lawton
  • Patent number: 5300687
    Abstract: 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: Grant
    Filed: July 18, 1991
    Date of Patent: April 5, 1994
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Charles Schwender, Keith Demarest, David Wustrow
  • Patent number: 5250522
    Abstract: 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: Grant
    Filed: October 9, 1992
    Date of Patent: October 5, 1993
    Assignee: Ciba-Geigy Corporation
    Inventor: Stephane De Lombaert
  • Patent number: 5217958
    Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are inhibitors of renin and therefore useful as cardiovascular agents.
    Type: Grant
    Filed: April 12, 1990
    Date of Patent: June 8, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Dinesh V. Patel
  • Patent number: 5212304
    Abstract: 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: Grant
    Filed: July 8, 1988
    Date of Patent: May 18, 1993
    Assignee: Applied Biosystems, Inc.
    Inventors: Steven Fung, Sam L. Woo, Lloyd M. Smith
  • Patent number: 5186733
    Abstract: 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: Grant
    Filed: November 12, 1991
    Date of Patent: February 16, 1993
    Assignee: Imperial Chemical Industries PLC
    Inventors: Michael D. Broadhurst, Tsze H. Tsang, John Tomko
  • Patent number: 5185334
    Abstract: 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: Grant
    Filed: September 6, 1991
    Date of Patent: February 9, 1993
    Assignee: Schering Corporation
    Inventors: Daniel Solomon, James J. Kaminski, Steven K. White, Laura S. Lehman de Gaeta, Ashit K. Ganguly
  • Patent number: 5183811
    Abstract: 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: Grant
    Filed: July 19, 1990
    Date of Patent: February 2, 1993
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Mitsuo Masaki, Hiromitsu Takeda, Toshiro Kamishiro, Masao Yamamoto
  • Patent number: 5177095
    Abstract: Substituted triazoles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I, are useful as angiotensin II antagonists.
    Type: Grant
    Filed: August 13, 1991
    Date of Patent: January 5, 1993
    Assignee: 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
  • Patent number: 5174913
    Abstract: 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: Grant
    Filed: September 20, 1991
    Date of Patent: December 29, 1992
    Assignee: Westvaco Corporation
    Inventors: John A. Alford, Paul G. Boyd, Eugene R. Fischer
  • Patent number: 5155100
    Abstract: 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: Grant
    Filed: May 1, 1991
    Date of Patent: October 13, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Mark D. Erion, Stephane De Lombaert
  • Patent number: 5124322
    Abstract: 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: Grant
    Filed: June 19, 1989
    Date of Patent: June 23, 1992
    Assignee: Beecham Group p.l.c.
    Inventor: Ian Hughes
  • Patent number: 5091526
    Abstract: 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: Grant
    Filed: January 8, 1991
    Date of Patent: February 25, 1992
    Assignee: Schering Corporation
    Inventors: Joel G. Berger, John W. Clader
  • Patent number: 5036152
    Abstract: Novel alkoxycarbonylalkylphospholipids, alkylaminocarbonylalkylphospholipids, processes for the preparation thereof, and methods for treating inflammation utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: September 5, 1989
    Date of Patent: July 30, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Nicholas J. Hrib, Kirk D. Shoger, John J. Tegeler
  • Patent number: 5030733
    Abstract: 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: Grant
    Filed: June 15, 1989
    Date of Patent: July 9, 1991
    Assignee: Hoechst-Roussel Pharmaceticals Incorporated
    Inventors: John J. Tegeler, Kirk D. Shoger
  • Patent number: 4992549
    Abstract: 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: Grant
    Filed: December 15, 1989
    Date of Patent: February 12, 1991
    Assignee: Ciba-Geigy Corporation
    Inventor: Werner Topfl
  • Patent number: 4956467
    Abstract: 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: Grant
    Filed: April 5, 1989
    Date of Patent: September 11, 1990
    Assignee: American Cyanamid Company
    Inventors: Lois M. Hinman, Libby S. Miller
  • Patent number: 4940707
    Abstract: 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: Grant
    Filed: February 14, 1989
    Date of Patent: July 10, 1990
    Assignee: Hoffman-La Roche Inc.
    Inventors: Michael Klaus, Peter Mohr, Ekkehard Weiss
  • Patent number: 4935520
    Abstract: 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: Grant
    Filed: September 19, 1988
    Date of Patent: June 19, 1990
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shoshichi Nojima, Hiroaki Nomura
  • Patent number: 4927835
    Abstract: 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: Grant
    Filed: March 1, 1989
    Date of Patent: May 22, 1990
    Assignee: Nippon Shinyaku Co., Ltd.
    Inventors: Masahiro Kise, Yoshihiko Yoshimoto, Hiroshi Fujisawa, Yasuo Sasaki, Shoji Yasufuku
  • Patent number: 4888328
    Abstract: 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: Grant
    Filed: March 10, 1988
    Date of Patent: December 19, 1989
    Assignee: Hoeschst-Roussel Incorporated
    Inventors: Nicholas J. Hrib, Kirk D. Shoger, John J. Tegeler
  • Patent number: 4855456
    Abstract: 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: Grant
    Filed: February 29, 1988
    Date of Patent: August 8, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Ta Jyh Lee, William F. Hoffman
  • Patent number: 4804654
    Abstract: Compounds of the formula ##STR1## wherein the symbols have assigned meanings, and their use as insecticides and/or miticides.
    Type: Grant
    Filed: March 4, 1987
    Date of Patent: February 14, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Mohamed A. H. Fahmy
  • Patent number: 4794183
    Abstract: 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: Grant
    Filed: January 14, 1986
    Date of Patent: December 27, 1988
    Assignee: Sankyo Company Limited
    Inventors: Norio Nakamura, Hideki Miyazaki, Fusaaki Shimizu, Kazuhiko Sasagawa
  • Patent number: 4776875
    Abstract: 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: Grant
    Filed: March 26, 1986
    Date of Patent: October 11, 1988
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz J. Loher, Klaus Bauer, Hermann Bieringer
  • Patent number: 4652297
    Abstract: 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: Grant
    Filed: February 25, 1982
    Date of Patent: March 24, 1987
    Assignee: Monsanto Company
    Inventors: John E. Franz, Robert J. Kaufman
  • Patent number: 4650791
    Abstract: 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: Grant
    Filed: January 8, 1985
    Date of Patent: March 17, 1987
    Assignee: Takedo Chemical Industries, Ltd.
    Inventors: Hiroaki Nomura, Kohei Nishikawa, Susumu Tsushima
  • Patent number: 4649203
    Abstract: 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: Grant
    Filed: March 27, 1986
    Date of Patent: March 10, 1987
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shoshichi Nojima, Hiroaki Nomura, Susumu Tsushima
  • Patent number: 4629491
    Abstract: 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: Grant
    Filed: December 20, 1983
    Date of Patent: December 16, 1986
    Assignee: Allied Corporation
    Inventors: Michael D. Swerdloff, Milorad M. Rogic, Larry L. Hendrickson
  • Patent number: 4624695
    Abstract: 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: Grant
    Filed: December 20, 1983
    Date of Patent: November 25, 1986
    Assignee: Allied Corporation
    Inventors: Michael D. Swerdloff, Milorad M. Rogic, Larry L. Hendrickson
  • Patent number: 4617295
    Abstract: 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: Grant
    Filed: October 3, 1985
    Date of Patent: October 14, 1986
    Assignee: Union Carbide Corporation
    Inventor: Themistocles D. J. D'Silva
  • Patent number: 4608367
    Abstract: .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: Grant
    Filed: July 25, 1985
    Date of Patent: August 26, 1986
    Assignee: Otsuka Kagaku Kabushiki Kaisha
    Inventors: Yoshinori Endo, Hisashi Takao
  • Patent number: 4605647
    Abstract: 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: Grant
    Filed: July 5, 1985
    Date of Patent: August 12, 1986
    Assignee: ADIR, S.A.R.L.
    Inventors: Gilbert Lavielle, Claude Cudennec
  • Patent number: 4588714
    Abstract: 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: Grant
    Filed: January 3, 1984
    Date of Patent: May 13, 1986
    Assignee: Stauffer Chemical Company
    Inventors: William G. Haag, Charles G. Chavdarian
  • Patent number: 4579956
    Abstract: 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: Grant
    Filed: October 20, 1978
    Date of Patent: April 1, 1986
    Assignee: Petrolite Corporation
    Inventor: Derek Redmore
  • Patent number: 4576933
    Abstract: 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: Grant
    Filed: April 29, 1983
    Date of Patent: March 18, 1986
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Susumu Tsushima, Kohei Nishikawa
  • Patent number: RE33489
    Abstract: 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: Grant
    Filed: September 25, 1989
    Date of Patent: December 11, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Godwin Berner, Mario Slongo