Nitrogen In The Acyclic Chain Patents (Class 558/390)
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Patent number: 6248893Abstract: 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: GrantFiled: June 8, 2000Date of Patent: June 19, 2001Assignee: Eastman Kodak CompanyInventors: Kevin W. Williams, Shiying Zheng, Thap DoMinh
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Patent number: 6232342Abstract: 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: GrantFiled: June 11, 1999Date of Patent: May 15, 2001Assignee: SmithKline Beecham CorporationInventors: 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
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Patent number: 6225346Abstract: 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: GrantFiled: August 10, 1999Date of Patent: May 1, 2001Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Asaad S. Nematalla, Gerald McMahon
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Patent number: 6191165Abstract: 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: GrantFiled: May 30, 1997Date of Patent: February 20, 2001Assignee: Allelix Neuroscience Inc.Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
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Patent number: 6121316Abstract: 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: GrantFiled: September 10, 1997Date of Patent: September 19, 2000Assignee: Hoechst AktiengesellschaftInventors: Wilfried Schwab, Ruth Raiss
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Patent number: 6103929Abstract: 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: GrantFiled: November 16, 1999Date of Patent: August 15, 2000Assignee: Eastman Chemical CompanyInventors: Daniel John Bayston, Jonathan Luke William Griffin, Arne Grumann, Mario Eugenio Cosimino Polywka, Ronald Michael Scott
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Patent number: 6090982Abstract: 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: GrantFiled: November 16, 1999Date of Patent: July 18, 2000Assignee: Eastman Chemical CompanyInventors: Daniel John Bayston, Jonathan Luke William Griffin, Arne Gruman, Mario Eugenio Cosimino Polywka, Ronald Michael Scott
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Patent number: 6031124Abstract: 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: GrantFiled: September 25, 1998Date of Patent: February 29, 2000Assignee: Medeva Europe LimitedInventors: Martin Edward Fox, Jane Marie Paul
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Patent number: 5981569Abstract: 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: GrantFiled: June 5, 1995Date of Patent: November 9, 1999Assignees: 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
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Patent number: 5965588Abstract: Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: March 26, 1998Date of Patent: October 12, 1999Assignee: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Patent number: 5891917Abstract: 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: GrantFiled: October 24, 1997Date of Patent: April 6, 1999Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Asaad S. Nematalla, Gerald McMahon
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Patent number: 5892095Abstract: 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: GrantFiled: January 30, 1997Date of Patent: April 6, 1999Assignee: Tokyo Ohka Kogyo Co., Ltd.Inventors: Hideo Hada, Hiroshi Komano, Toshimasa Nakayama
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Patent number: 5888481Abstract: 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: GrantFiled: September 29, 1995Date of Patent: March 30, 1999Assignee: AlliedSignal Inc.Inventors: Keith A. Horn, Richard B. Heath, David B. Schwind
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Patent number: 5856518Abstract: 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: GrantFiled: November 26, 1997Date of Patent: January 5, 1999Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Toshifumi Akiba, Tutomu Ebata, Tatsuru Saito, Sadahiro Shimizu, Keiichi Hirai, Naoki Ohta, Toshiaki Tojo
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Patent number: 5856490Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification have retinoid-like biological activity.Type: GrantFiled: September 4, 1997Date of Patent: January 5, 1999Assignee: AllerganInventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
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Patent number: 5811424Abstract: 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: GrantFiled: July 1, 1996Date of Patent: September 22, 1998Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Masaru Shibata, Kazuhiko Sugiyama, Norihisa Yonekura, Junetsu Sakai, Yoshiyuki Kojima, Shigeru Hayashi
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Patent number: 5775329Abstract: 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: GrantFiled: June 7, 1995Date of Patent: July 7, 1998Assignee: Gensia, Inc.Inventors: Ernest K. Metzner, Mark D. Erion
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Patent number: 5763639Abstract: 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: GrantFiled: March 3, 1997Date of Patent: June 9, 1998Assignee: BASF AktiengesellschaftInventors: Ulrich Annen, Hans-Peter Seelmann-Eggebert, Rudi Widder, Reinhard Muller
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Patent number: 5703265Abstract: 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: GrantFiled: May 10, 1996Date of Patent: December 30, 1997Assignee: Eastman Kodak CompanyInventors: John C. Wilson, Peter S. Alexandrovich
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Patent number: 5679715Abstract: 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: GrantFiled: June 7, 1995Date of Patent: October 21, 1997Inventor: Richard Y. Harris
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Patent number: 5643947Abstract: 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: GrantFiled: May 24, 1995Date of Patent: July 1, 1997Assignee: G. D. Searle & Co.Inventors: Claude L. Gillet, Philippe R. Bovy, Hugo Gorissen, Michel P. Snyers
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Patent number: 5620831Abstract: 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: GrantFiled: March 28, 1995Date of Patent: April 15, 1997Assignee: Taiyo Ink Manufacturing Co., Ltd.Inventor: Osamu Kawana
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Patent number: 5496855Abstract: 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: GrantFiled: January 27, 1995Date of Patent: March 5, 1996Assignee: SmithKline Beecham Corp.Inventors: Jerry L. Adams, Ravi S. Garigipati, Margaret E. Sorenson, James D. Winkler
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Patent number: 5493053Abstract: 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: GrantFiled: December 21, 1994Date of Patent: February 20, 1996Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron, Jr.
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Patent number: 5486539Abstract: 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: GrantFiled: March 1, 1994Date of Patent: January 23, 1996Assignee: G. D. Searle & Co.Inventors: Chi-Dean Liang, John P. McKearn, John M. Farah, Jr., Richard A. Mueller
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Patent number: 5476960Abstract: 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: GrantFiled: April 7, 1994Date of Patent: December 19, 1995Assignee: Akzo Nobel N.V.Inventors: Alison A. Fleming, Robert F. Farmer, James F. Gadberry
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Patent number: 5457224Abstract: 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: GrantFiled: June 7, 1994Date of Patent: October 10, 1995Assignee: Knoll AktiengesellschaftInventors: Oskar Ehrmann, Herbert Nagel
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Patent number: 5451604Abstract: 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: GrantFiled: July 26, 1993Date of Patent: September 19, 1995Assignee: G. D. Searle & Co.Inventors: Richard A. Mueller, Thomas E. Barta, John P. McKearn, Susan A. Gregory, Richard A. Partis, Francis J. Koszyk
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Patent number: 5432196Abstract: 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: GrantFiled: January 13, 1994Date of Patent: July 11, 1995Assignee: Knoll AGInventors: Joerg Rosenberg, Rolf Neidhardt, Guenter Blaich
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Patent number: 5416111Abstract: 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: GrantFiled: December 16, 1993Date of Patent: May 16, 1995Assignee: G.D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5399690Abstract: 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: GrantFiled: February 10, 1993Date of Patent: March 21, 1995Assignee: Eastman Kodak CompanyInventors: Donald R. Diehl, Glenn M. Brown, Margaret J. Helber
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Patent number: 5395853Abstract: 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: GrantFiled: November 24, 1993Date of Patent: March 7, 1995Assignee: Burroughs Wellcome Co.Inventors: William P. Jackson, Clifford J. Harris, Richard J. Arrowsmith, John G. Dann, Kevin J. O'Connor, Robert F. G. Booth
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Patent number: 5389619Abstract: 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: GrantFiled: March 29, 1993Date of Patent: February 14, 1995Assignee: BASF AktiengesellschaftInventors: Reinhard Doetzer, Hubert Sauter, Horst Wingert, Reinhard Kirstgen, Albrecht Harreus, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5374762Abstract: .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: GrantFiled: April 6, 1994Date of Patent: December 20, 1994Assignee: Akzo Nobel N.V.Inventors: Alison A. Fleming, Robert F. Farmer, James F. Gadberry
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Patent number: 5374763Abstract: .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: GrantFiled: April 6, 1994Date of Patent: December 20, 1994Assignee: Akzo Nobel n.v.Inventors: Alison A. Fleming, Robert F. Farmer, James F. Gadberry
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Patent number: 5371265Abstract: .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: GrantFiled: April 7, 1994Date of Patent: December 6, 1994Assignee: Akzo Nobel N.V.Inventors: Alison A. Fleming, Robert F. Farmer, James F. Gadberry
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Patent number: 5367113Abstract: 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: GrantFiled: June 23, 1993Date of Patent: November 22, 1994Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron, Jr.
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Patent number: 5354777Abstract: 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: GrantFiled: February 23, 1993Date of Patent: October 11, 1994Assignee: Bayer AktiengesellschaftInventors: Peter Wachtler, Wilfried Paulus, Georg-Wilhelm Ludwig
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Patent number: 5344830Abstract: 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: GrantFiled: December 10, 1992Date of Patent: September 6, 1994Assignee: Merck & Co., Inc.Inventors: Sander G. Mills, Richard J. Budhu, Conrad P. Dorn, William J. Greenlee, Malcolm MacCoss, Mu T. Wu
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Patent number: 5334745Abstract: 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: GrantFiled: May 28, 1993Date of Patent: August 2, 1994Assignee: BASF AktiengesellschaftInventors: Martin Brudermueller, Tom Witzel, Franz Merger
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Patent number: 5326755Abstract: 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: GrantFiled: September 10, 1992Date of Patent: July 5, 1994Assignee: Roussel UCLAFInventors: Robert J. Blade, George S. Cockerill
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Patent number: 5319126Abstract: .alpha.-aminonitrile compounds derived from a fatty alkyl alkylene diamine containing two reactible amino functionalities are disclosed.Type: GrantFiled: January 29, 1993Date of Patent: June 7, 1994Assignee: Akzo n.v.Inventors: Alison A. Fleming, Robert F. Farmer, James F. Gadberry
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Patent number: 5300640Abstract: 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: GrantFiled: December 19, 1991Date of Patent: April 5, 1994Assignee: Sumitomo Chemical Company, LimitedInventors: Mitsumori Hiratsuka, Naonori Hirata, Kazuo Saito, Hideyuki Shibata
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Patent number: 5292918Abstract: 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: GrantFiled: October 6, 1992Date of Patent: March 8, 1994Assignee: Schering CorporationInventors: Jacques Gosteli, Ingrid Mergelsberg, Markus Tanner
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Patent number: 5290814Abstract: 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: GrantFiled: November 5, 1992Date of Patent: March 1, 1994Assignee: Burroughs Wellcome Co.Inventors: William P. Jackson, Clifford J. Harris, Richard J. Arrowsmith, John G. Dann, Kevin J. O'Connor, Robert F. G. Booth
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Patent number: 5254724Abstract: 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: GrantFiled: October 30, 1991Date of Patent: October 19, 1993Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron, Jr.
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Patent number: 5247119Abstract: 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: GrantFiled: May 28, 1992Date of Patent: September 21, 1993Assignee: G. D. Searle & Co.Inventors: Kerry W. Fowler, John M. Farah, Jr., John P. McKearn, Richard A. Mueller, Susan A. Gregory
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Patent number: 5167696Abstract: 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: GrantFiled: February 7, 1991Date of Patent: December 1, 1992Assignee: Imperial Chemical Industries PLCInventors: Ewan J. T. Chrystal, John E. D. Barton, David Cartwright
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Patent number: 5166402Abstract: 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: GrantFiled: November 1, 1990Date of Patent: November 24, 1992Assignee: Bayer AktiengesellschaftInventors: Michael Haug, Hans-Joachim Santel, Robert R. Schmidt, Harry Strang
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Patent number: 5120869Abstract: 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: GrantFiled: November 7, 1989Date of Patent: June 9, 1992Assignee: Imperial Chemical Industries plcInventor: David Cartwright