Nitrogen In The Acyclic Chain Patents (Class 558/390)
  • Patent number: 6248893
    Abstract: Infrared radiation-sensitive compounds have been found that are represented by Structure DYE as follows: wherein R is a secondary or tertiary amine that contains no heterocyclic group, R1 and R2 are independently carbocyclic aromatic groups, and M+ is a monovalent cation. These compounds have a &lgr;max above 700 nm and are can be used in a number of photosensitive or heat-sensitive imaging materials.
    Type: Grant
    Filed: June 8, 2000
    Date of Patent: June 19, 2001
    Assignee: Eastman Kodak Company
    Inventors: Kevin W. Williams, Shiying Zheng, Thap DoMinh
  • Patent number: 6232342
    Abstract: The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease, hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting and bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.
    Type: Grant
    Filed: June 11, 1999
    Date of Patent: May 15, 2001
    Assignee: SmithKline Beecham Corporation
    Inventors: Thomas Joseph Carr, Renee Louise Desjarlais, Timothy Francis Gallagher, Stacie Marie Halbert, Hye-Ja Oh, Scott Kevin Thompson, Daniel Frank Veber, Dennis Shinji Yamashita, Jack Hwekwo Yen
  • Patent number: 6225346
    Abstract: The present invention relates to molecules capable of modulating tyrosine signal transduction to prevent and treat cell proliferative disorders or cell differentiation disorders associated with particular tyrosine kinases by inhibiting one or more abnormal tyrosine kinase activities.
    Type: Grant
    Filed: August 10, 1999
    Date of Patent: May 1, 2001
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, Li Sun, Asaad S. Nematalla, Gerald McMahon
  • Patent number: 6191165
    Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 30, 1997
    Date of Patent: February 20, 2001
    Assignee: Allelix Neuroscience Inc.
    Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
  • Patent number: 6121316
    Abstract: 2-Cyano-3,5-dihydroxyhex-2-enecarboxamide derivatives ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of diseases or dissorders whose course involves increased connective tissue or cartilage degradation.
    Type: Grant
    Filed: September 10, 1997
    Date of Patent: September 19, 2000
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wilfried Schwab, Ruth Raiss
  • Patent number: 6103929
    Abstract: Disclosed is a process for the preparation of cyclopropylglycine by a 5-step process wherein cyclopropanecarboxaldehyde is reacted with an .alpha.-aminoalkylaromatic compound to obtain an imine which is reacted with a cyanide to produce an aminonitrile compound; the aminonitrile compound is hydrolyzed to the corresponding aminocarboxylic acid and finally the arylalkyl residue is removed from the amino group by hydrogenolysis.
    Type: Grant
    Filed: November 16, 1999
    Date of Patent: August 15, 2000
    Assignee: Eastman Chemical Company
    Inventors: Daniel John Bayston, Jonathan Luke William Griffin, Arne Grumann, Mario Eugenio Cosimino Polywka, Ronald Michael Scott
  • Patent number: 6090982
    Abstract: Disclosed is a process for the preparation of cyclopropylglycine by a 5-step process wherein cyclopropanecarboxaldehyde is reacted with an .alpha.-aminoalkylaromatic compound to obtain an imine which is reacted with a cyanide to produce an aminonitrile compound; the aminonitrile compound is hydrolyzed to the corresponding aminocarboxylic acid and finally the arylalkyl residue is removed from the amino group by hydrogenolysis.
    Type: Grant
    Filed: November 16, 1999
    Date of Patent: July 18, 2000
    Assignee: Eastman Chemical Company
    Inventors: Daniel John Bayston, Jonathan Luke William Griffin, Arne Gruman, Mario Eugenio Cosimino Polywka, Ronald Michael Scott
  • Patent number: 6031124
    Abstract: The subject invention pertains to compounds of the formula Y.sup.1 Y.sup.2 N--(CH.sub.2).sub.4 --CH.dbd.C(Ph)--X wherein Y.sup.1 and Y.sup.2 are independently H or a removable blocking group, or Y.sup.1 and Y.sup.2 together are a removable divalent blocking group; and X is COOCH.sub.3 or a group convertible thereto. Such a compound may be cyclised, by Michael addition, to give methylphenidate, if necessary after removing blocking group(s) and converting X to COOCH.sub.3. The subject invention also pertains to methods for preparing compounds of the invention.
    Type: Grant
    Filed: September 25, 1998
    Date of Patent: February 29, 2000
    Assignee: Medeva Europe Limited
    Inventors: Martin Edward Fox, Jane Marie Paul
  • Patent number: 5981569
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction and particularly KDR/FLK-1 receptor signal transduction in order to regulate and/or modulate vasculogenesis and angiogenesis. The invention is based, in part, on the demonstration that KDR/FLK-1 tyrosine kinase receptor expression is associated with endothelial cells and the identification of vascular endothelial growth factor (VEGF) as the high affinity ligand of FLK-1. These results indicate a major role for KDR/FLK-1 in the signaling system during vasculogenesis and angiogenesis. Engineering of host cells that express FLK-1 and the uses of expressed FLK-1 to evaluate and screen for drugs and analogs of VEGF involved in FLK-1 modulation by either agonist or antagonist activities is also described.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: November 9, 1999
    Assignees: Yissum Research Development Company of the Hebrew University of Jerusalem, Sugen, Inc.
    Inventors: Harald App, Gerald M. McMahon, Peng Cho Tang, Aviv Gazit, Alexander Levitzki
  • Patent number: 5965588
    Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: March 26, 1998
    Date of Patent: October 12, 1999
    Assignee: G.D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 5891917
    Abstract: The present invention relates to molecules capable of modulating tyrosine signal transduction to prevent and treat cell proliferative disorders or cell differentiation disorders associated with particular tyrosine kinases by inhibiting one or more abnormal tyrosine kinase activities.
    Type: Grant
    Filed: October 24, 1997
    Date of Patent: April 6, 1999
    Assignee: Sugen, Inc.
    Inventors: Peng Cho Tang, Li Sun, Asaad S. Nematalla, Gerald McMahon
  • Patent number: 5892095
    Abstract: Disclosed is a novel positive-working or negative-working chemical-sensitization photoresist composition useful in the photolithographic patterning works for the manufacture of electronic devices. The photoresist composition is characterized by a unique acid-generating agent capable of releasing an acid by the pattern-wise exposure of the resist layer to actinic rays so as to increase or decrease the solubility of the resist layer in an aqueous alkaline developer solution. The acid-generating agent proposed is a novel cyano group-containing oxime sulfonate di- or triester compound represented by the general formulaA?C(CN).dbd.N--O--SO.sub.2 --R!.sub.n,in which each R is, independently from the others, an unsubstituted or substituted monovalent hydrocarbon group such as alkyl groups, A is a divalent or tervalent organic group or, preferably, phenylene group and the subscript n is 2, when A is a divalent group, or 3, when A is a tervalent group or, preferably 2.
    Type: Grant
    Filed: January 30, 1997
    Date of Patent: April 6, 1999
    Assignee: Tokyo Ohka Kogyo Co., Ltd.
    Inventors: Hideo Hada, Hiroshi Komano, Toshimasa Nakayama
  • Patent number: 5888481
    Abstract: The invention relates to novel cinnamamides, a process for their manufacture and their use as UV absorbers. The cinnamamides of the invention may be used as UV absorbers in a variety of engineered resins such as polyamides (especially nylon 6 and 6,6), polycarbonates, polyacetals, polysulfones, polyimides, polyaryletherketones, and polyesters, (especially PET and PBT), as well as, other polymers such as polyvinylchloride and polyolefins (polyethylenes and polypropylenes).
    Type: Grant
    Filed: September 29, 1995
    Date of Patent: March 30, 1999
    Assignee: AlliedSignal Inc.
    Inventors: Keith A. Horn, Richard B. Heath, David B. Schwind
  • Patent number: 5856518
    Abstract: This invention is to provide a compound represented by the following formula (I) and a compound represented by the following formula (II) useful as an antibacterial agent which is obtained by the compound of folmula (I), and also to provide a novel synthetic process for the inexpensive, short-step and industrially advantageous production thereof.
    Type: Grant
    Filed: November 26, 1997
    Date of Patent: January 5, 1999
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Toshifumi Akiba, Tutomu Ebata, Tatsuru Saito, Sadahiro Shimizu, Keiichi Hirai, Naoki Ohta, Toshiaki Tojo
  • Patent number: 5856490
    Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification have retinoid-like biological activity.
    Type: Grant
    Filed: September 4, 1997
    Date of Patent: January 5, 1999
    Assignee: Allergan
    Inventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
  • Patent number: 5811424
    Abstract: The present invention provides an amino-acid amide derivative represented by the formula: ##STR1## (wherein R.sup.1 represents a lower alkyl group (optionally having at least one same or different substituent of a halogen atom), R.sup.2 represents an ethyl group, R.sup.3 represents a hydrogen atom, R.sup.4 represents a hydrogen atom, R.sup.5, R.sup.6, and R.sup.7 independently represent a hydrogen atom or a lower alkyl group, R.sup.8 represents a hydrogen atom, Z.sup.1 and Z.sup.2 independently represent an oxygen atom or a sulfur atom, Z.sup.3 represents an oxygen atom or a sulfur atom, Q represents a phenyl group, m represents an integer from 0 to 2, and n represents 0 or 1), and an agricultural or horticultural fungicide including an effective amount of the same. The amino-acid amide derivatives exhibit a superior control of plant diseases, particularly downy mildew and late blight, and are not harmful to plants.
    Type: Grant
    Filed: July 1, 1996
    Date of Patent: September 22, 1998
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Masaru Shibata, Kazuhiko Sugiyama, Norihisa Yonekura, Junetsu Sakai, Yoshiyuki Kojima, Shigeru Hayashi
  • Patent number: 5775329
    Abstract: The present invention relates generally to methods of diagnosis, evaluation and treatment of coronary artery disease in mammals using substituted catecholamines and compounds therefore. It also relates to the preparation, use and administration of these compounds which are useful in the diagnosis, evaluation and treatment of coronary artery disease by means of a feedback controlled drug delivery system that delivers exercise simulating agents which are capable of eliciting acute responses similar to those elicited by aerobic exercise.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 7, 1998
    Assignee: Gensia, Inc.
    Inventors: Ernest K. Metzner, Mark D. Erion
  • Patent number: 5763639
    Abstract: A process for preparing quaternized glycine nitriles of formula I ##STR1## comprising reaction of the corresponding precursor amine, aldehyde, hydrocyanic acid or alkali metal cyanide, and subsequent quaternization with an alkylating agent, wherein the reaction and quaternization are carried out successively in aqueous medium without isolation of an intermediate.
    Type: Grant
    Filed: March 3, 1997
    Date of Patent: June 9, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Ulrich Annen, Hans-Peter Seelmann-Eggebert, Rudi Widder, Reinhard Muller
  • Patent number: 5703265
    Abstract: A compound having the structure: ##STR1## is disclosed. R.sup.1 is defined in the specification. The compounds are charged control agents for use in electrostatographic toners and developers.
    Type: Grant
    Filed: May 10, 1996
    Date of Patent: December 30, 1997
    Assignee: Eastman Kodak Company
    Inventors: John C. Wilson, Peter S. Alexandrovich
  • Patent number: 5679715
    Abstract: The invention relates to a method of treating multiple sclerosis comprising administering an effective amount of (R)-(-)-N,2-dimethyl-N-2-propynylphenethylamine alone or in conjunction with an effective amount of interferon beta or an effective amount of amantadine.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 21, 1997
    Inventor: Richard Y. Harris
  • Patent number: 5643947
    Abstract: A class of .omega.-amino-.alpha.-phenylalkanonitrile derivatives is described having use in treatment of cardiovascular dysfunctions such as hypertension. Compounds of most interest are those of the formula: ##STR1## wherein each of R.sub.1 and R.sub.2 is methoxy, R.sub.3 is hydrido, R.sub.4 is isopropyl, R.sub.5 is methyl and R.sub.6 is selected from linear alkyl, phenylpropyl, phenylbutyl and phenylpentyl.
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: July 1, 1997
    Assignee: G. D. Searle & Co.
    Inventors: Claude L. Gillet, Philippe R. Bovy, Hugo Gorissen, Michel P. Snyers
  • Patent number: 5620831
    Abstract: Disclosed are novel cyanoguanidine derivatives which are usable as an epoxy resin curing agent and are represented by the following general formula (1). A thermosetting resin composition and a photocurable and thermosetting resin composition containing the following cyanoguanidine derivatives and other derivatives as the epoxy resin curing agent are also disclosed. ##STR1## wherein R.sup.1 represents a substituent selected from the group consisting of the following substituents (a) through (k).
    Type: Grant
    Filed: March 28, 1995
    Date of Patent: April 15, 1997
    Assignee: Taiyo Ink Manufacturing Co., Ltd.
    Inventor: Osamu Kawana
  • Patent number: 5496855
    Abstract: This invention relates to the novel compounds and pharmaceutical compositions of Formulas (I) and (II).This invention also relates to a method of treating or reducing inflammation in a mammal in need thereof, which comprises administering to said mammal an effective amount of a compound or composition of Formula (I) or (II).
    Type: Grant
    Filed: January 27, 1995
    Date of Patent: March 5, 1996
    Assignee: SmithKline Beecham Corp.
    Inventors: Jerry L. Adams, Ravi S. Garigipati, Margaret E. Sorenson, James D. Winkler
  • Patent number: 5493053
    Abstract: A new and versatile route to N'-[5-[[4-[[5-(acetylhydroxyamino)pentyl]amino]-1,4-dioxobutyl]hydroxyamin o]pentyl]-N-(5-aminopentyl)-N-hydroxybutanediamide, desferrioxamine B (DFO) is described. N-Benzyloxy-1,5-diaminopentane is selectively protected at the primary amino site. The product is reacted at the benzyloxyamine with an anhydride to produce a carboxylic acid which is, in turn, acylated regio-specifically with a diamine at the primary amine to give a benzyloxyamine. The previous two steps are repeated to afford a DFO reagent. Acetylation of the DFO reagent, followed by hydrogenolysis and tert-butoxycarbonyl group removal, furnishes DFO.
    Type: Grant
    Filed: December 21, 1994
    Date of Patent: February 20, 1996
    Assignee: University of Florida Research Foundation, Inc.
    Inventor: Raymond J. Bergeron, Jr.
  • Patent number: 5486539
    Abstract: A class of substituted phenylacetonitrile-alkylaminoalkyl-ortho-substituted aryl compounds having immunosuppressive properties is described. Compounds of this class would be useful in reducing recipient rejection of transplanted organs and for treatment of autoimmune or inflammatory diseases. Compounds of particular interest are of the formula ##STR1## wherein m is one or two; wherein n is a number selected from one to five, inclusive; wherein R.sup.1 is selected from hydrido, alkyl, hydroxyalkyl, cycloalkyl, cycloalkylalkyl, alkoxyalkyl, alkenyl and alkynyl; wherein R.sup.6 is selected from loweralkyl; wherein each of R.sup.8, R.sup.9, R.sup.10 and R.sup.12 through R.sup.16 is independently selected from hydrido, hydroxy, alkyl, hydroxyalkyl, alkoxy, alkenyl, alkynyl, alkylcarbonyl, alkoxycarbonyl, alkylcarbonylalkenyl, alkylaminocarbonyl and alkoxyalkyl; with the proviso that at least one of R.sup.12 and R.sup.
    Type: Grant
    Filed: March 1, 1994
    Date of Patent: January 23, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Chi-Dean Liang, John P. McKearn, John M. Farah, Jr., Richard A. Mueller
  • Patent number: 5476960
    Abstract: An .alpha.-aminonitrile compound derived from the reaction, in the presence of a cyanide source of (1) a bisulfite adduct of a carbonyl compound selected from the group consisting of an aldehyde and a ketone with (2) a fatty alkyl alkylene diamine containing two reactible amino functionalities which is of the formula RNHR.sub.1 NH.sub.2, where R is fatty alkyl and R.sub.1 is lower alkylene of up to six carbon atoms.
    Type: Grant
    Filed: April 7, 1994
    Date of Patent: December 19, 1995
    Assignee: Akzo Nobel N.V.
    Inventors: Alison A. Fleming, Robert F. Farmer, James F. Gadberry
  • Patent number: 5457224
    Abstract: A process for the resolution of racemic verapamil which comprises reacting the free base of the compound with optically active dibenzoyltartaric acid or ditoluoyltartaric acid in the molar ratio from 1:1 to 1:2 in a methanol/water mixture in the ratio from 1:1 to 3:1 or acetone/water mixture in the ratio from 0.5:1 to 2:1, separating the mixture of diastereomers obtained in this way by crystallization, and then converting the diastereomers into the free bases and these into their salts, if required, with physiologically tolerated acids.
    Type: Grant
    Filed: June 7, 1994
    Date of Patent: October 10, 1995
    Assignee: Knoll Aktiengesellschaft
    Inventors: Oskar Ehrmann, Herbert Nagel
  • Patent number: 5451604
    Abstract: A class of halogenated phenylacetonitrile alkylaminoalkylphenyl compounds having immunosuppressive properties is described. Compounds of this class would be useful in reducing recipient rejection of transplanted organs and for treatment of autoimmune or inflammatory diseases. Compounds of particular interest are of the formula ##STR1## wherein m is a number selected from three to five, inclusive; wherein n one or two; wherein R.sup.1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, tert-butyl, iso-butyl, n-pentyl, isopentyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, cyclohexylmethyl, benzyl and phenethyl; wherein R.sup.2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, tert-butyl, iso-butyl, n-pentyl, isopentyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, cyclohexylmethyl, benzyl and phenethyl; wherein each of R.sup.3 through R.sup.
    Type: Grant
    Filed: July 26, 1993
    Date of Patent: September 19, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Thomas E. Barta, John P. McKearn, Susan A. Gregory, Richard A. Partis, Francis J. Koszyk
  • Patent number: 5432196
    Abstract: A process for preparing an aqueous active substance solution which can be sterilized by filtration entails mixing anipamil hydrochloride with a phospholipid in the ratio of from 1:2 to 2:1 by weight, converting the resulting mixture into a gel by adding water at elevated temperature, and subsequently adding water to the gel at elevated temperature until the active substance is present in the required concentration.
    Type: Grant
    Filed: January 13, 1994
    Date of Patent: July 11, 1995
    Assignee: Knoll AG
    Inventors: Joerg Rosenberg, Rolf Neidhardt, Guenter Blaich
  • Patent number: 5416111
    Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols containing a cyano group and having an N-phenyl-amino-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.
    Type: Grant
    Filed: December 16, 1993
    Date of Patent: May 16, 1995
    Assignee: G.D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 5399690
    Abstract: Solid particle dispersions of dyes according to the formula: ##STR1## wherein D is selected from the group consisting of ##STR2## and ketomethylene nuclei are disclosed as filter dyes for photographic elements.In this formula, E.sup.1 and E.sup.2 are each independently electron withdrawing groups. R.sup.1 and R.sup.6 are each independently R or NHR, where R is aryl. R.sup.2 and R.sup.3 are each independently alkyl or aryl, or represent the carbon atoms necessary to form a fused ring with the phenyl ring to which the N atom is attached. R.sup.4 and R.sup.7 are each independently hydrogen, alkyl or aryl. R.sup.5 is alkyl. Z represents the atoms necessary to complete a 5 or 6 memebered heterocyclic nucleus. M.sup.+ is a cation. L.sup.1 through L.sup.7 are each independently methine groups. m is 0, 1, 2, or 3. n is 0 or 1. p is 0, 1, 2, 3, or 4. q is 0, 1, 2, or 3. At least one of R.sup.1 or D includes an aryl ring substituted with a carboxy or sulfonamido substituent.
    Type: Grant
    Filed: February 10, 1993
    Date of Patent: March 21, 1995
    Assignee: Eastman Kodak Company
    Inventors: Donald R. Diehl, Glenn M. Brown, Margaret J. Helber
  • Patent number: 5395853
    Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein m is 0 or 1;W is hydrogen, a C.sub.1-16 straight, branched, or cyclic alkyl group, or a C.sub.2-16 straight, branched, or cyclic alkenyl or alkynyl group, orPh(CH.sub.2).sub.n -- where Ph is phenyl and n is an integer of from 0 to 2, the phenyl group being optionally substituted by one or more atoms or groups independently selected from halogen, hydroxy, nitro, C.sub.1-4 alkoxy and C.sub.1-4 alkyl wherein one or more of the hydrogen atoms in said alkyl group is optionally replaced by halogen, orR.sup.1 NHCO-- where R.sup.1 is hydrogen or a C.sub.1-6 alkyl group, orR.sup.2 CONH-- where R.sup.2 is hydrogen or a C.sub.1-6 alkyl group; ##STR2## Y is --(CH.sub.2).sub.q, where q is an integer of from 1 to 3, or --CH.dbd.CH-- (E or Z);Z is a C.sub.
    Type: Grant
    Filed: November 24, 1993
    Date of Patent: March 7, 1995
    Assignee: Burroughs Wellcome Co.
    Inventors: William P. Jackson, Clifford J. Harris, Richard J. Arrowsmith, John G. Dann, Kevin J. O'Connor, Robert F. G. Booth
  • Patent number: 5389619
    Abstract: Compounds of the formula I ##STR1## where n, W, X, Y, Z, R.sup.1, R.sup.2, and R.sup.3 are as defined herein exhibit fungicidal, insecticidal, and acaracidal activity.
    Type: Grant
    Filed: March 29, 1993
    Date of Patent: February 14, 1995
    Assignee: BASF Aktiengesellschaft
    Inventors: Reinhard Doetzer, Hubert Sauter, Horst Wingert, Reinhard Kirstgen, Albrecht Harreus, Gisela Lorenz, Eberhard Ammermann
  • Patent number: 5374762
    Abstract: .alpha.-aminonitrile compounds derived from a fatty alkyl alkylene diamine containing two reactible amino functionalities are disclosed which are of the formula ##STR1## where R is C.sub.12 -C.sub.22 fatty alkyl, R.sub.1 is alkylene, R.sub.2 is aryl, and R.sub.3 is alkyl, aryl, or hydrogen.
    Type: Grant
    Filed: April 6, 1994
    Date of Patent: December 20, 1994
    Assignee: Akzo Nobel N.V.
    Inventors: Alison A. Fleming, Robert F. Farmer, James F. Gadberry
  • Patent number: 5374763
    Abstract: .alpha.-aminonitrile compounds derived from a fatty alkyl alkylene diamine containing two reactible amino functionalities are disclosed which are of the formula ##STR1## where R is C.sub.12 -C.sub.22 fatty alkyl, R.sub.1 is alkylene, R.sub.2 is alkyl, and R.sub.3 is alkyl or hydrogen.
    Type: Grant
    Filed: April 6, 1994
    Date of Patent: December 20, 1994
    Assignee: Akzo Nobel n.v.
    Inventors: Alison A. Fleming, Robert F. Farmer, James F. Gadberry
  • Patent number: 5371265
    Abstract: .alpha.-aminonitrile compounds derived from a fatty alkyl alkylene diamine containing two reactible amino functionalities are disclosed which are of the formula ##STR1## where R is C.sub.12 -C.sub.22 fatty alkyl, R.sub.1 is alkylene, R.sub.2 is aryl, and R.sub.3 is aryl or hydrogen.
    Type: Grant
    Filed: April 7, 1994
    Date of Patent: December 6, 1994
    Assignee: Akzo Nobel N.V.
    Inventors: Alison A. Fleming, Robert F. Farmer, James F. Gadberry
  • Patent number: 5367113
    Abstract: Synthesis of desferrioxamine B and analogs and homologs thereof beginning with O-protected, N-protected hydroxylamine, which is N-alkylated to produce a protected N-4-cyanoalkylhydroxylamine which is acylated with a suitable anhydride. The resulting half-acid amide is subjected to a series of high yield condensations and reductions which vide desferrioxamine B in high overall yield. Alternatively, polyether analogs of desferrioxamine B can be prepared by reacting an activated polyether with the O-protected, N-protected hydroxylamine and subjecting the resulting product to a series of similar steps.
    Type: Grant
    Filed: June 23, 1993
    Date of Patent: November 22, 1994
    Assignee: University of Florida Research Foundation, Inc.
    Inventor: Raymond J. Bergeron, Jr.
  • Patent number: 5354777
    Abstract: New cyanoalkene derivatives of the formula (I) ##STR1## are described, in which R and R.sup.1 have the meaning given in the description, and a process for their preparation.The new cyanoalkene derivatives are used for combating microorganisms for the protection of industrial materials.
    Type: Grant
    Filed: February 23, 1993
    Date of Patent: October 11, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Peter Wachtler, Wilfried Paulus, Georg-Wilhelm Ludwig
  • Patent number: 5344830
    Abstract: Diacylpiperazines of general structure ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, and asthma, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
    Type: Grant
    Filed: December 10, 1992
    Date of Patent: September 6, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Sander G. Mills, Richard J. Budhu, Conrad P. Dorn, William J. Greenlee, Malcolm MacCoss, Mu T. Wu
  • Patent number: 5334745
    Abstract: 3-Aminopropionitriles of the general formula I ##STR1## where R.sup.1,R.sup.2,R.sup.3,R.sup.4 and R.sup.5 independently of one another are each hydrogen, C.sub.1 -C.sub.20 -alkyl, C.sub.1 -C.sub.8 -aminoalkyl, C.sub.1 -C.sub.8 -cyanoalkyl, C.sub.3 -C.sub.20 -cycloalkyl, C.sub.7 -C.sub.20 -aralkyl or aryl,are prepared by a process in which an amine of the general formula II ##STR2## is reacted with an acrylonitrile of the general formula III ##STR3## where the substituents have the abovementioned meanings, in a molar ratio of from 0.9:1 to 100:1 over a heterogeneous catalyst at from 40.degree. to 200.degree. C. and from 1 to 350 bar.
    Type: Grant
    Filed: May 28, 1993
    Date of Patent: August 2, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Martin Brudermueller, Tom Witzel, Franz Merger
  • Patent number: 5326755
    Abstract: The present application discloses pesticidally active compounds of formula I:QQ.sup.1 CR.sup.1 .dbd.CR.sup.2 CR.sup.3 .dbd.CR.sup.4 C(.dbd.X.sup.1)NR.sup.5 R.sup.6or a salt thereof, wherein Q is an monocyclic aromatic ring, or Q is a dihalovinyl group or a group R.sup.7 --C.dbd.C-- where R.sup.7 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halogen or hydrogen; Q.sup.1 is a 1,2-cyclopropyl ring optionally substituted by one or more groups selected from C.sub.1-3 alkyl, halo, C.sub.1-3 haloalkyl, alkynyl, or cyano; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl; X.sup.1 is oxygen or sulphur; R.sup.5 is C.sub.1-8 hydrocarbyl optionally substituted, halo, cyano, trifluoromethyl, trifluoromethylthio or C.sub.1-6 alkoxy; and R.sup.6 is selected from:(A) --Y.dbd.X.sup.2 --(R.sup.8).sub.a where X.sup.2 is O or S, Y is carbon, R.sup.8 is hydrogen, C.sub.
    Type: Grant
    Filed: September 10, 1992
    Date of Patent: July 5, 1994
    Assignee: Roussel UCLAF
    Inventors: Robert J. Blade, George S. Cockerill
  • Patent number: 5319126
    Abstract: .alpha.-aminonitrile compounds derived from a fatty alkyl alkylene diamine containing two reactible amino functionalities are disclosed.
    Type: Grant
    Filed: January 29, 1993
    Date of Patent: June 7, 1994
    Assignee: Akzo n.v.
    Inventors: Alison A. Fleming, Robert F. Farmer, James F. Gadberry
  • Patent number: 5300640
    Abstract: A novel herbicidal pyrimidine derivative represented by the formula ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y.sup.1, Y.sup.2, Y.sup.3, X and Z are as defined herein.
    Type: Grant
    Filed: December 19, 1991
    Date of Patent: April 5, 1994
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Mitsumori Hiratsuka, Naonori Hirata, Kazuo Saito, Hideyuki Shibata
  • Patent number: 5292918
    Abstract: A process for preparing an (S,S) or (R,R) diastereoisomer of the formula: ##STR1## or salts, esters or amides thereof, wherein R.sup.3 and R.sup.4 independently represent hydrogen, alkyl, aryl or aryl substituted with halogen, alkyl, nitro or alkoxy, and n and m independently represent integers from one to six, comprising combining a cyanide compound of the formula:M.sup.1 C.tbd.N (III)wherein M.sup.1 is hydrogen, trimethylsilyl or a metal, with an optional proton source, a solvent and a Lewis acid of the formula:M.sup.2 X.sub.4, AlCl.sub.3 or BF.sub.3 (IV)wherein M.sup.2 is Sn or Ti and X represents chloro, bromo, fluoro or iodo, with an .alpha.-amino acid compound or salts or esters thereof, followed by addition of an acyl or acetal compound to give the diastereoisomer of formula (X).
    Type: Grant
    Filed: October 6, 1992
    Date of Patent: March 8, 1994
    Assignee: Schering Corporation
    Inventors: Jacques Gosteli, Ingrid Mergelsberg, Markus Tanner
  • Patent number: 5290814
    Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein m is 0 or 1;W is hydrogen, a C.sub.1-16 straight, branched, or cyclic alkyl group, or a C.sub.2-16 straight, branched, or cyclic alkenyl or alkynyl group, or Ph(CH.sub.2).sub.n -- where Ph is phenyl and n is an integer of from 0 to 2, the phenyl group being optionally substituted by one or more atoms or groups independently selected from halogen, hydroxy, nitro, C.sub.1-4 alkoxy and C.sub.1-4 alkyl wherein one or more of the hydrogen atoms in said alkyl group is optionally replaced by halogen, or R.sup.1 NHCO-- where R.sup.1 is hydrogen or a C.sub.1-6 alkyl group, or R.sup.2 CONH-- where R.sup.2 is hydrogen or a C.sub.1-6 alkyl group; X is ##STR2## where A is halogen; Y is --(CH.sub.2).sub.q, where q is an integer of from 1 to 3, or --CH.dbd.CH-- (E or Z);Z is a C.sub.
    Type: Grant
    Filed: November 5, 1992
    Date of Patent: March 1, 1994
    Assignee: Burroughs Wellcome Co.
    Inventors: William P. Jackson, Clifford J. Harris, Richard J. Arrowsmith, John G. Dann, Kevin J. O'Connor, Robert F. G. Booth
  • Patent number: 5254724
    Abstract: Synthesis of desferrioxamine B and analogs and homologs thereof beginning with O-protected, N-protected hydroxylamine, which is N-alkylated to produce a protected N-4-cyanoalkylhydroxylamine which is acylated with a suitable anhydride. The resulting half-acid amide is subjected to a series of high yield condensations and reductions which provide desferrioxamine B in high overall yield. Alternatively, polyether analogs of desferrioxamine B can be prepared by reacting an activated polyether with the O-protected, N-protected hydroxylamine and subjecting the resulting product to a series of similar steps.
    Type: Grant
    Filed: October 30, 1991
    Date of Patent: October 19, 1993
    Assignee: University of Florida Research Foundation, Inc.
    Inventor: Raymond J. Bergeron, Jr.
  • Patent number: 5247119
    Abstract: A class of substituted phenylacetonitrilehydroxyalkylaminoalkyl-ortho-substituted aryl compounds having immunosuppressive properties is described. Compounds of this class would be useful in reducing recipient rejection of transplanted organs and for treatment of autoimmune or inflammatory diseases. Compounds of particular interest are of the formula ##STR1## wherein each of m and n is a number independently selected from one to five, inclusive; wherein R.sup.1 is selected from hydrido, alkyl, hydroxyalkyl, cycloalkyl, cycloalkylalkyl, alkoxyalkyl, alkenyl and alkynyl; wherein R.sup.6 is selected from loweralkyl; wherein each of R.sup.8, R.sup.9, R.sup.10 and R.sup.12 through R.sup.16 is independently selected from hydrido, hydroxy, alkyl, hydroxyalkyl, alkoxy, alkenyl, alkynyl, alkylcarbonyl, alkoxycarbonyl, alkylcarbonylalkenyl, alkylaminocarbonyl and alkoxyalkyl; or a tautomer thereof or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: May 28, 1992
    Date of Patent: September 21, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Kerry W. Fowler, John M. Farah, Jr., John P. McKearn, Richard A. Mueller, Susan A. Gregory
  • Patent number: 5167696
    Abstract: A compound of formula (I): ##STR1## in which Ar is an optionally substituted aryl or heterocyclic ring system; W is O or NR.sup.1 where R.sup.1 is hydrogen or lower alkyl;A is .dbd.CH or >CH.sub.2 and G is .dbd.C--R.sup.2, >CR.sup.3 R.sup.4 or >C.dbd.R.sup.5 such that --G--A-- is --CR.sup.2 .dbd.CH--, where R.sup.2 is H or CR.sup.6 R.sup.7 XR.sup.8 ; or --G--A-- is CR.sup.3 R.sup.4 --CH.sub.2 where CR.sup.3 R.sup.4 is CH--CR.sup.6 R.sup.7 XR.sup.8, CH--OCR.sup.6 R.sup.7 XR.sup.8, C(R.sup.9)OCOR.sup.10, CR.sup.9 R.sup.10, C(R.sup.9)OR.sup.10, C(OR.sup.9)OR.sup.10, or CH--CH.sub.2 (CO.sub.2 R.sup.11); or --G--A-- is --CR.sup.5 --CH.sub.2 -- where R.sup.5 is .dbd.CR.sup.7 XR.sup.8, .dbd.NOCR.sup.6 R.sup.7 XR.sup.8, .dbd.NOR.sup.11 or .dbd.NOCOR.sup.11 ;X is (CH.sub.2).sub.n, CH.dbd.CH, CH(OR.sup.20)CH.sub.2, or COCH.sub.2 ;n is 0, 1 or 2;R.sup.6 and R.sup.7 are independently selected from H, optionally substituted alkyl, alkenyl or alkynyl, halogen, NR.sup.9 R.sup.10, or R.sup.6 and R.sup.
    Type: Grant
    Filed: February 7, 1991
    Date of Patent: December 1, 1992
    Assignee: Imperial Chemical Industries PLC
    Inventors: Ewan J. T. Chrystal, John E. D. Barton, David Cartwright
  • Patent number: 5166402
    Abstract: Herbicidal .alpha.-(5-aryloxy-naphthalen-1-yl-oxy)propionic acid derivatives of the formula ##STR1## in which R.sup.1 stands for hydrogen, halogen, cyano or trifluoromethyl,R.sup.2 stands for hydrogen or halogen,R.sup.3 stands for halogen, cyano, trifluoromethyl or trifluoromethoxy,R.sup.4 stands for hydrogen or halogen,R.sup.5 stands for hydrogen or halogen andZ stands for halogen, hydroxyl, amino, alkylamino, alkenylamino, alkinylamino, arylamino, aralkylamino, alkoxycarbonylalkylamino, cyanamino, dialkylamino, dialkenylamino, alkylsulphonylamino, arylsulphonylamino, hydroxylamino, alkoxyamino, hydrazino, alkylsulphonylhydrazino, arylsulphonylhydrazino, alkylthio, arylthio, aralkylthio, alkoxycarbonylalkylthio or for the --O--R.sup.6 group,wherein R.sup.6 can be various organic radicals.The starting material naphthol of the formula ##STR2## is also new.
    Type: Grant
    Filed: November 1, 1990
    Date of Patent: November 24, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Michael Haug, Hans-Joachim Santel, Robert R. Schmidt, Harry Strang
  • Patent number: 5120869
    Abstract: A herbicidal compound of formula (I): ##STR1## wherein X is O, S(O).sub.n or NR.sup.a where R.sup.a is H or alkyl and n is 0, 1 or 2;R.sup.1 is H or halo;R.sup.2 is N or CR.sup.3 where R.sup.3 is halo or NO.sub.2 ;R.sup.4 is H, halo, NO.sub.2, alkyl, haloalkyl, CN, CO.sub.2 alkyl, cycloalkyl, phenyl, COalkyl, COphenyl, CHO,OH, NH.sub.2, NHCOalkyl or alkoxyR.sup.5 is H, halo or optionally substituted alkyl;R.sup.6 is H, halo or optionally substituted alkyl; provided that at least one of R.sup.5 and R.sup.6 is halo;R.sup.7 is CN, CHO, COOR.sup.8, CONR.sup.8 R.sup.9, where R.sup.8 is H, optionally substituted alkyl, alkenyl, alkynyl or aryl and R.sup.9 is a group R.sup.8, SO.sub.2 alkyl, NR.sup.10 R.sup.11 or N.sup.+ R.sup.10 R.sup.11 R.sup.12 Z.sup.- where Z is an agriculturally acceptable anion e.g. chloride and R.sup.10, R.sup.11 and R.sup.12 are independently selected from hydrogen and alkyl. Processes for the preparation of these compounds and compositions containing them are also described.
    Type: Grant
    Filed: November 7, 1989
    Date of Patent: June 9, 1992
    Assignee: Imperial Chemical Industries plc
    Inventor: David Cartwright