Phosphorus Attached Directly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 548/111)
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Patent number: 5274147Abstract: A process for preparing a dinuclear manganese complex of formula (A) ##STR1## wherein: Mn represents manganese in the III or IV oxidation state, each X is independently a co-ordinating or bridging species selected from H.sub.2 O, O.sub.2.sup.-, O.sup.2-, OH.sup.-, SH.sup.-, S.sup.2-,>S=O, Cl.sup.-, N.sub.3.sup.-, SCN.sup.-, N.sup.3-, RCOO.sup.-, NH.sub.2.sup.- and NR.sub.Type: GrantFiled: July 6, 1992Date of Patent: December 28, 1993Assignee: Lever Brothers Company, Division of Conopco, Inc.Inventors: Judith Kerschner, Jean H. Koek, Ronald P. Potman, Lodewijk Van der Wolf
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Patent number: 5268388Abstract: Certain substituted semicarbazones, including all geometric and stereoisomers thereof, agricultural compositions containing them and their use as arthropodicides.Type: GrantFiled: November 2, 1992Date of Patent: December 7, 1993Assignee: E. I. Du Pont de Nemours and CompanyInventors: John P. Daub, George P. Lahm, Bradford S. Marlin
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Patent number: 5254691Abstract: A phosphorylating agent represented by the following general formula [1]: ##STR1## wherein R represents a protective group of the phosphoric acid; and X represents a heterocyclic residue represented by the following general formula [2]: ##STR2## wherein Y represents a single bond or an oxygen or sulfur atom; Z represents a heterocyclic nucleus comprising at least one nitrogen atom as a ring-forming element and may be condensed with another aromatic ring; and W represents one or more substituents other than a hydrogen atom. The phosphorylating agent is stable, can rapidly proceed phosphodiester bond-forming reactions in good selectivity under mild conditions and thus makes it possible to perform a reaction even in a relatively large scale.Type: GrantFiled: February 22, 1993Date of Patent: October 19, 1993Assignee: Fuji Photo Film Co., Ltd.Inventor: Hideto Mori
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Patent number: 5234917Abstract: Angiotensin II receptor antagonists having the formula: ##STR1## which are useful in regulating hypertension and in the treatment of congestive heart failure, renal failure, and glaucoma pharmaceutical compositions including these antagonists, and methods of using these compounds to produce angiotensin II receptor antagonism in mammals.Type: GrantFiled: November 30, 1990Date of Patent: August 10, 1993Inventors: Joseph A. Finkelstein, Judith Hempel, Richard M. Keenan, James Samanen, Joseph Weinstock
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Patent number: 5220021Abstract: Unsaturated geminal phosphonates (III) ##STR1## either as the esters, free acids or salts are useful in the treatment of arthritis.Type: GrantFiled: September 6, 1991Date of Patent: June 15, 1993Assignee: The Upjohn CompanyInventors: Colin J. Dunn, Richard A. Nugen
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Patent number: 5210200Abstract: A dye compound of a general formula (I): ##STR1##where R.sub.1 represents a hydrogen atom, or a substituent; R.sub.2 and R.sub.3 independently represent a substituent; X represents a nitrogen atom or --C(R.sub.5).dbd.; R.sub.5 represents a substituent; and R.sub.4 represents an aromatic group or an unsaturated heterocyclic group as bonded to the nitrogen atom in the formula via an unsaturated carbon atom, which dye compound is fast to heat and light and is useful for color image formation and as a filter dye; and a thermal transfer dye donating material having a dye donating layer containing a thermal transferring dye on a support, where the thermal transferring dye is represented by: ##STR2##where X.sup.2 represents --N.dbd., or --C(R.sup.22).dbd.; R.sup.21, R.sup.22, R.sup.23 and R.sup.24 independently represent a hydrogen atom, or a non-metallic substituent; R.sup.25, R.sup.26, R.sup.27 and R.sup.Type: GrantFiled: November 27, 1991Date of Patent: May 11, 1993Assignee: Fuji Photo Film Co., Ltd.Inventors: Yasuhiro Shimada, Hisashi Mikoshiba, Hideo Usui
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Patent number: 5208235Abstract: Novel compounds having the formula ##STR1## where X R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore for example, as antihypertensive agents.Type: GrantFiled: March 10, 1992Date of Patent: May 4, 1993Assignee: E. R. Squibb & Sons, Inc.Inventor: Michael A. Poss
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Patent number: 5208234Abstract: Novel compounds having the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.Type: GrantFiled: March 10, 1992Date of Patent: May 4, 1993Assignee: E. R. Squibb & Sons, Inc.Inventor: Michael A. Poss
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Patent number: 5187159Abstract: 1,3-Benzodioxoles and 1,3-benzodithioles substituted with a 6-fused imidazole of Formula I which are useful as angiotensin II antagonists.Type: GrantFiled: October 7, 1991Date of Patent: February 16, 1993Assignee: Merck & Co., Inc.Inventors: William J. Greenlee, Ralph A. Rivero
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Patent number: 5182339Abstract: A pyrazoloazoleazomethine dye represented by formula (I) ##STR1## wherein, R.sub.1 represents a substituent having a Hammett's substituent constant value of at least 0.6; Za, Zb, and Zc each represents ##STR2## (wherein R.sub.2 represents a hydrogen atom or a substituent), or .dbd.N--; when Zc=Zb is a carbon-carbon double bond, it may form a part of an aromatic ring; R.sub.3, R.sub.4, and R.sub.5 each represents a hydrogen atom or a substituent; and n represents 1 or 2; said dye may form a dimer or higher polymer by combining with each other or to a polymer through a divalent or higher valent group at R.sub.1, Za, Zb, or Zc.Type: GrantFiled: December 5, 1990Date of Patent: January 26, 1993Assignee: Fuji Photo Film Co., Ltd.Inventors: Shigeki Yokoyama, Tadahisa Sato, Keizo Kimura, Nobuo Furutachi, Osamu Takahashi
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Patent number: 5162540Abstract: (3aS,6aR)-[(R)-(1-phenylethyl)-3,4-methoxybenzyl dihydro-1H-furo-[3,4-d]-imidazol-2,4(3H,3aH)-dione and 1H-furo-[3,4-d]-imidazol-2,4-(3H,3aH)-dione derivatives which are useful as intermediates for preparing (+) biotin, also known as vitamin H.Type: GrantFiled: October 17, 1991Date of Patent: November 10, 1992Assignee: Lonza Ltd.Inventors: John McGarrity, Leander Tenud
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Patent number: 5138069Abstract: Substituted imidazoles such as ##STR1## are useful as angiotensin II blockers. These compounds have activity in treating hypertension and congestive heart failure.Type: GrantFiled: December 6, 1988Date of Patent: August 11, 1992Assignee: E. I. Du Pont de Nemours and CompanyInventors: David J. Carini, John J. V. Duncia, Pancras C. B. Wong
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Patent number: 5128328Abstract: The compound of the formula: ##STR1## positioned so that the gem-diphosphonic acid carbon atom is in the 4- or 5-position; R.sup.1 is alkyl or arylalkyl; R.sup.2 is hydrogen, 2- or 3-pyridinyl or 3-,5- or 6-alkylpyridin-2-yl; or a pharmaceutically acceptable salt thereof, with the proviso that when the gem-bisphosphonic acid substituted carbon atom is in 4-position, R.sup.1 is other than alkyl, used in the treatment of disease states involving calcium metabolism.Type: GrantFiled: October 25, 1991Date of Patent: July 7, 1992Assignee: American Home Products CorporationInventors: Arie Zask, Richard D. Coghlan
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Patent number: 5116827Abstract: The N-phosphorylation of basic nitrogenous drug compounds to produce pro-drugs with enhanced water solubility or lipid solubility, or reduced toxicity, is disclosed. Drugs containing amine, amidine, guanidine, isourea, isothiourea and biguanide functions may be converted to such pro-drugs. The pro-drugs are hydrolyzed in the body, regenerating the original drugs with the release of a salt of phosphoric acid.Type: GrantFiled: March 18, 1991Date of Patent: May 26, 1992Assignee: American Cyanamid CompanyInventors: Keith C. Murdock, Ving J. Lee
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Patent number: 5103007Abstract: Lipid derivatives represented by the formula: ##STR1## wherein R.sup.1 stands for an optionally substituted higher alkyl group, R.sup.2 stands for an optionally substituted lower alkyl group or an optionally substituted nitrogen-containing heterocyclic group, R.sup.3 stands for a tertiary amino group or a quaternary ammonium group, J stands for oxygen atom or S(O)t (where t deontes 0, 1 or 2), m and n respectively denotes 1 or 2, p denotes 0, 1 or 2, q and r respectively denote an integer of 2 to 5.and salts thereof have antitumor activities including differentiation-inducing activity and are useful as antitumor agents.Type: GrantFiled: October 27, 1989Date of Patent: April 7, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Hiroshi Akimoto, Keizo Inoue
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Patent number: 5096915Abstract: The invention provides compounds of formula I ##STR1## in which X, Y and R.sup.1-5 are as defined in the description. The compounds have valuable fungicidal activity.Type: GrantFiled: March 28, 1990Date of Patent: March 17, 1992Assignee: Schering AgrochemicalsInventors: John H. Parsons, Donald J. Simpson, Philip J. Dudfield
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Patent number: 5081245Abstract: A compound represented by the formula: ##STR1## wherein R represents a hydrogen atom or a lower alkyl group;R.sup.1 represents a higher alkyl group which may be substituted;R.sup.2 represents a hydrogen atom or a lower alkyl group, a lower alkanoyl group or a nitrogen-containing 5- to 7-membered heterocyclic group each of which may be substituted; X represents a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --wherein p represents an integer of 1 to 5, a divalent group represented by the formula:--O(CH.sub.2).sub.q --wherein q represents an integer of 3 to 8, or a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --J--(CH.sub.2).sub.q --wherein J represents an oxygen atom or a group represented by the formula: --S(O).sub.Type: GrantFiled: August 18, 1989Date of Patent: January 14, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Hiroshi Akimoto, Eiko Imamiya, Keizo Inoue
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Patent number: 5077283Abstract: The N-phosphorylation of basic nitrogenous drug compounds to produce pro-drugs with enhanced water solubility or lipid solubility, or reduced toxicity, is disclosed. Drugs containing amine, amidine, quanidine, isourea, isothiourea and biguanide functions may be converted to such pro-drugs. The pro-drugs are hydrolyzed in the body, regenerating the original drugs with the release of a salt of phosphoric acid.Type: GrantFiled: March 18, 1991Date of Patent: December 31, 1991Assignee: American Cyanamid CompanyInventors: Keith C. Murdock, Ving J. Lee
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Patent number: 5026867Abstract: A pyrazoloazoleazomethine dye represented by formula (I) ##STR1## wherein, R.sub.1 represents a substituent having a Hammett's substituent constant value of at least 0.6; Za, Zb, and Zc each represents ##STR2## (wherein R.sub.2 represents a hydrogen atom or a substituent), or .dbd.N--; when Zc.dbd.Zb is a carbon-carbon double bond, it may form a part of an aromatic ring; R.sub.3, R.sub.4, and R.sub.5 each represents a hydrogen atom or a substituent; and n represents 1 or 2; said dye may form a dimer or higher polymer by combining with each other or to a polymer through a divalent or higher valent group at R.sub.1, Za, Zb, or Zc.Type: GrantFiled: February 5, 1990Date of Patent: June 25, 1991Inventors: Shigeki Yokoyama, Tadahisa Sato, Keizo Kimura, Nobuo Furutachi, Osamu Takahashi
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Patent number: 5011938Abstract: 7-Substituted bicyclic pyrazolidinone compounds as antimicrobials and the corresponding intermediates, are discussed or provided. The use of the antimicrobial compounds in pharmaceutical compositions and in methods for treating bacterial infections is set forth.Type: GrantFiled: April 3, 1990Date of Patent: April 30, 1991Assignee: Eli Lilly and CompanyInventors: Charles J. Barnett, Richard E. Holmes, Louis N. Jungheim, Sandra K. Sigmund, Robert J. Ternansky
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Patent number: 5006515Abstract: Pharmaceuticals containing or composed of at least one compound of the formula I and/or one of its physiologically tolerated salts where appropriate, where the compounds of the formula I can, where appropriate, be in the form of pure stereoisomers or mixtures thereof; formula I is: ##STR1## in which R.sup.1 =organic radical or halogen,A=C,C single or C,C double bond,n=0, 1 or 2, and ##STR2## R.sup.2 and R.sup.3 =H or optionally substituted aliphatic radical. The pharmaceuticals are suitable for the prophylaxis and/or treatment of diseases of the immune system, especially of tumors, infections and/or autoimmune diseases of the human or animal body and for use as adjuvants for vaccines.Some of the compounds of the formula I are new; the compounds can be prepared by special processes.Type: GrantFiled: October 26, 1988Date of Patent: April 9, 1991Assignee: Hoechst AktiengesellschaftInventors: Wilfried Schwab, Robert R. Bartlett, Ulrich Gebert, Hans U. Schorlemmer, Gerhard Dickneite, Hans H. Sedlacek
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Patent number: 4940718Abstract: 7-Substituted bicyclic pyrazolidinone compounds as antimicrobials and the corresponding intermediates, are discussed or provided. The use of the antimicrobial compounds in pharmaceutical compositions and in methods for treating bacterial infections is set forth.Type: GrantFiled: October 2, 1989Date of Patent: July 10, 1990Assignee: Eli Lilly and CompanyInventors: Charles J. Barnett, Richard E. Holmes, Louis N. Jungheim, Sandra K. Sigmund, Robert J. Ternansky
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Patent number: 4921968Abstract: A pyrazoloazoleazomethine dye represented by formula (I) ##STR1## wherein, R.sub.1 represents a substituent having a Hammett's substituent constant value of at least 0.6; Za, Zb, and Zc each represents .dbd.CH--, ##STR2## (wherein R.sub.2 represents a hydrogen atom or a substituent), or .dbd.N--; when Zc=Zb is a carbon-carbon double bond, it may form a part of an aromatic ring; R.sub.3, R.sub.4, and R.sub.5 each represents a hydrogen atom or a substituent; and n represents 1 or 2; said dye may form a dimer or higher polymer by combining with each other or to a polymer through a divalent or higher valent group at R.sub.1, Za, Zb, or Zc.Type: GrantFiled: December 9, 1987Date of Patent: May 1, 1990Assignee: Fuji Photo Film Co., Ltd.Inventors: Shigeki Yokoyama, Tadahisa Sato, Keizo Kimura, Nobuo Furutachi, Osamu Takahashi
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Patent number: 4900838Abstract: N-acylated derivatives of bis(2-imidazolin-2-ylhydrazones) of 9,10-anthracenedicarboxaldehyde, useful as anti-cancer agents against certain strains in mice, are disclosed and described, including processes for manufacture and use.Type: GrantFiled: September 22, 1988Date of Patent: February 13, 1990Assignee: American Cyanamid CompanyInventor: Keith C. Murdock
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Patent number: 4885286Abstract: A novel phosphonamidothionate derivative represented by the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined in the disclosure. The present novel compound has excellent properties with respect to not only pesticidal activity but also maintenance of the pesticidal activity over a prolonged period of time after application. The present novel compound can be prepared by a new unique process in which the direct phosphorylation of a carbamate compound is involved.Type: GrantFiled: February 19, 1988Date of Patent: December 5, 1989Assignee: Asahi Kasei Kogyo Kabushiki KaishaInventors: Hiromichi Yoshikawa, Teruyuki Misumi
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Patent number: 4880933Abstract: Novel intermediates for insecticides of the formula (I) ##STR1## wherein Y represents nitro or cyano;A represents an ethylene or trimethylene radical, which is optionally substituted; andZ can have many possible meanings.Type: GrantFiled: December 8, 1987Date of Patent: November 14, 1989Assignee: Nihon Tokushu Noyaku Seizo K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Koichi Moriya, Katsuhiko Shibuya
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Patent number: 4876350Abstract: Process for the production of (+) biotin. A compound of the formula: ##STR1## wherein R.sub.1 is e.g., an (R)-1-phenylalkyl group, and R.sub.2 is, e.g., hydrogen. The desired diastereomer of the formula: ##STR2## is separated out. If R.sub.2 is H, a protective group is introduced by reaction with, e.g., an aliphatic acid chloride. The diastereomer is converted by reaction with a thiocarboxylic acid salt derivative into the corresponding thiolacetone, which is reacted with a Grignard reactant and subsequently water is split off. Alternatively, the corresponding thiolacetone is reacted with a compound of the formula:(C.sub.6 H.sub.5).sub.3 P.sup..sym. (CH.sub.2).sub.4 COOR.sub.3.X.sup..crclbar.wherein R.sub.3 is, e.g., H, and X is a halogen atom, in the presence of a base to provide a compound of the formula: ##STR3## Such compound is catalytically hydrogenated and then converted into (+) biotin by cleavage of the protective groups.Type: GrantFiled: December 16, 1987Date of Patent: October 24, 1989Assignee: Lonza Ltd.Inventors: John McGarrity, Leander Tenud
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Patent number: 4873339Abstract: Imidazole derivatives of the formula: ##STR1## wherein R.sub.1 is an (R)- or (S)-1-phenylalkyl group, an (R)- or (S)-1-alkoxycarbonyl-1-phenylmethyl group or an (R)- or (S)-1-aryloxycarbonyl-1-phenylmethyl group, R.sub.2 is hydrogen, a substituted or unsubstituted alkanoyl group, a substituted or unsubstituted benzoyl group, a substituted or unsubstituted benzyl group, an alkoxycarbonyl group, an aryloxycarbonyl group, an alkoxyalkyl group, a pyranyl group, a substituted or unsubstituted benzenesulfonyl group, an alkylsufonyl group, a diarylphosphinyl group, a dialkoxyphosphinyl group or a trialkylsilyl group, and A is a sulfur or oxygen atom. The imidazole derivatives are intermediate products for the production of (+) biotin.Type: GrantFiled: November 30, 1988Date of Patent: October 10, 1989Assignee: Lonza Ltd.Inventors: John McGarrity, Leander Tenud, Thomas Meul
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Patent number: 4851540Abstract: Process for the production of imidazole derivatives of the formula: ##STR1## wherein R.sub.1 is an (R)- or (S)-1-phenylalkyl group, an (R)- or (S)-1-alkoxycarbonyl-1-phenylmethyl group or an (R)- or (S)-1-aryloxycarbonyl-1-phenylmethyl group, R.sub.2 is hydrogen, a substituted or unsubstituted alkanoyl group, an unsubstituted or a substituted benzoyl group, a substituted or an unsubstituted benzyl group, an alkoxycarbonyl group, and aryloxycarbonyl group, an alkoxyalkyl group, a pyranyl group, a substituted or unsubstituted benzenesulfonyl group, an alkylsulfonyl group, a diarylphosphinyl group, a dialkoxyphosphinyl group or a trialkylsilyl group, and A is a sulfur or oxygen atom.Type: GrantFiled: December 1, 1987Date of Patent: July 25, 1989Assignee: Lonza Ltd.Inventors: John McGarrity, Leander Tenud, Thomas Meul
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Patent number: 4839349Abstract: The application is also directed to a pesticidal composition comprising the above-recited compound and a carrier.Type: GrantFiled: June 3, 1988Date of Patent: June 13, 1989Assignee: Uniroyal Chemical Company, Inc.Inventors: Rupert A. Covey, Richard C. Moore
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Patent number: 4783451Abstract: An organophosphorus compound having the formula: ##STR1## wherein X is ##STR2## Z is an oxygen atom or a sulfur atom, and each of R.sub.1 and R.sub.2 is an alkyl group which may be substituted by halogen, alkoxy or alkylthio. The compound is useful as an insecticide, miticide, nematicide or soil pesticide.Type: GrantFiled: June 25, 1986Date of Patent: November 8, 1988Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Takahiro Haga, Tadaaki Toki, Toru Koyanagi, Hiroshi Okada, Kiyomitsu Yoshida, Osamu Imai
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Patent number: 4780473Abstract: Compounds are disclosed having fungicidal activity and are of general formula I ##STR1## where at least three of A, C, D and E are --CX.dbd. and the other is --CX.dbd. or --N.dbd., where X is hydrogen, C.sub.1-8 -alkyl (optionally substituted by halogen), halo, nitro or phenoxy, in which the phenyl is optionally substituted by one or more groups selected from halo and trifluoromethyl;R.sup.1 is --SO.sub.2 R.sup.3 or ##STR2## and R.sup.2 is ##STR3## where R.sup.6 is hydrogen, C.sub.1-8 -alkyl (optionally substituted by one or more groups selected from halogen and hydroxy), C.sub.1-8 -alkanoyl, benzoyl, cyclohexylcarbonyl or aminocarbonyl (in which the amino is substituted by benzoyl or chlorobenzenesulphonyl);R.sup.3, R.sup.4, and R.sup.5 may be the same or different and have the meanings given to R.sup.6 or can be di-C.sub.1-8 -alkylamino; and Z is oxygen or sulphur; and when R.sup.1 is ##STR4## R.sup.2 can also be --CN.Type: GrantFiled: December 14, 1987Date of Patent: October 25, 1988Assignee: Schering Agrochemicals Ltd.Inventors: Alister C. Baillie, Antony D. Buss, John H. Parsons, Philip E. Russell
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Patent number: 4743618Abstract: Novel compounds useful as dopamine receptor agonists for the treatment of various diseases of the central nervous system such as Parkinson's disease and related disorders having the structural formula ##STR1## where R.sub.2, R.sub.3 and R.sub.4 are each selected from the group consisting of H, and OA; A is selected from the group consisting of hydrocarbyl radicals; ##STR2## where X is S or O: and pharmaceutically acceptable salts thereof. Also disclosed is a method for inducing a dopaminergic response in a patient by adminstering a pharmacologically-effective amount of one of the foregoing compounds.Type: GrantFiled: July 28, 1986Date of Patent: May 10, 1988Assignee: Nelson Research & Development Co.Inventor: Alan S. Horn
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Patent number: 4742060Abstract: Novel insecticides of the formula ##STR1## in which n is 0 or 1,X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R.sup.9 variously represent hydrogen or specified organic radicals.Type: GrantFiled: January 21, 1986Date of Patent: May 3, 1988Assignee: Nihon Tokushu Noyaku Seizo K. K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Koichi Moriya
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Patent number: 4720488Abstract: A compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 each represent C.sub.1 -C.sub.5 alkoxy or C.sub.1 -C.sub.5 alkylthio, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 each represent hydrogen or C.sub.1 -C.sub.5 alkyl, R.sup.7, R.sup.8 and R.sup.9 each represent hydrogen, C.sub.1 -C.sub.5 alkyl or halogen, and X represents oxygen or sulfur. A process for preparing the compound (I) and a pesticidal composition containing the compound (I) are also provided.Type: GrantFiled: December 8, 1986Date of Patent: January 19, 1988Assignee: Shionogi & Co., Ltd.Inventors: Yoshio Hayase, Mitsuhiro Ichinari, Kazuo Kamei, Junji Taguchi, Katsuaki Oba, Toshio Takahashi
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Patent number: 4692542Abstract: The invention relates to phosphorylating agents containing at least one protected hydroxyl group and at least one leaving group. According to the invention, a methylsulphonylethyl group (Mse) is used as the hydroxyl protecting group. Typical examples of such phosphorylating agents are the compounds (MseO).sub.2 POL, (MseO)POLL', (MseO).sub.2 PL and (MseO)PLL', in which L and L' are leaving groups. The invention also relates to processes for preparing these phosphorylating agents and processes for the phosphorylation of organic hydroxyl or amine compounds, in particular nucleosides and (poly)nucleotides.Type: GrantFiled: June 20, 1984Date of Patent: September 8, 1987Assignee: Stichting Katholieke UniversiteitInventors: Godefridus I. Tesser, Christianus A. A. Claesen
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Patent number: 4645761Abstract: An organophosphorus compound having the formula: ##STR1## wherein each of X.sub.1, X.sub.2 and X.sub.3 is a hydrogen atom; an alkyl, alkoxy or alkenyl group which may be substituted by halogen, alkoxy, alkylthio, cycloalkyl or phenyl; a phenyl group which may be substituted by halogen; or a cycloalkyl group, each of Y.sub.1, Y.sub.2 and Y.sub.3 is an oxygen atom or a sulfur atom, Z is a carbonyl group; or a methylene group which may be substituted by a cycloalkyl group, by a phenyl group which may be substituted by halogen, or by an alkyl, alkoxy or alkenyl group which may be substituted by halogen, alkoxy alkylthio, cycloalkyl or phenyl, and each of R.sub.1 and R.sub.2 is an alkyl group which may be substituted by halogen, alkoxy or alkylthio.Type: GrantFiled: December 18, 1985Date of Patent: February 24, 1987Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Takahiro Haga, Tadaaki Toki, Toru Koyanagi, Hiroshi Okada, Kiyomitsu Yoshida, Osamu Imai
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Patent number: 4614533Abstract: Herbicidally active 5-amino-1-phenyl-pyrazoles, most of which are new, of the formula ##STR1##Type: GrantFiled: January 10, 1985Date of Patent: September 30, 1986Assignee: Bayer AktiengesellschaftInventors: Otto Schallner, Reinhold Gehring, Erich Klauke, Jorg Stetter, Heinz-Jurgen Wroblowsky, Robert R. Schmidt, Hans-Joachim Santel
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Patent number: 4607031Abstract: An ethyl benzylphosphinate derivative represented by the general formula (I) ##STR1## wherein Y represents a hydrogen or fluorine atom, X represents a methylene group or an oxygen atom, and n is 2, 3 or 4.The said compounds can be produced by reacting a compound represented by the following formula (II) ##STR2## wherein Y is as defined above, with a compound represented by the following formula (III) ##STR3## wherein X and n are as defined, and M is an alkali metal atom, in an inert medium. These compounds are useful as a calcium antagonist.Type: GrantFiled: May 22, 1985Date of Patent: August 19, 1986Assignee: Kanebo Ltd.Inventors: Koichiro Yoshino, Tominori Morita, Masaru Moriyama, Keizo Ito, Goro Tsukamoto
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Patent number: 4590182Abstract: An organophosphorus compound represented by the general formula: ##STR1## where each of X.sub.1 and X.sub.3 is a hydrogen atom; an alkyl or alkoxy group which may be substituted by halogen, alkoxy, alkylthio, phenoxy, halogenated phenoxy, phenylthio or halogenated phenylthio; a carboxyl group; an alkoxycarbonyl group; or a phenyl group which may be substituted by halogen, each of X.sub.2 and X.sub.4 is a hydrogen atom or an alkyl group, provided that X.sub.2 and X.sub.3 may together form an alkylene group, each of Y.sub.1, Y.sub.2 and Z is an oxygen atom or a sulfur atom, and each of R.sub.1 and R.sub.2 is an alkyl group.Type: GrantFiled: November 7, 1984Date of Patent: May 20, 1986Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Takahiro Haga, Tadaaki Toki, Toru Koyanagi, Hiroshi Okada, Kiyomitsu Yoshida, Osamu Imai
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Patent number: 4524211Abstract: There are prepared 1-amino-2-mercapto-2-methylpropyl phosphonic acid or 1-amino-2-mercapto-2-methylpropyl alkylphosphinic acids of the formula ##STR1## in which Y is hydroxy or an alkyl group by reacting thiazoline-(3) with a phosphonic acid dialkyl ester or an alkylphosphinic acid alkyl ester and then hydrolytically splitting the thiazolidinyl phosphonic acid dialkyl ester or thiazolidinyl alkylphosphinic acid alkyl ester. The thiazolidinyl compounds are new compounds. The 1-amino-2-mercapto-2-methylpropyl phosphonic acid and the 1-amino-2-mercapto-2-methylpropyl alkylphosphinic acids are needed for pharmaceutical purposes.Type: GrantFiled: November 16, 1983Date of Patent: June 18, 1985Assignee: Degussa AktiengesellschaftInventors: Karlheinz Drauz, Hans G. Koban, Jurgen Martens, Werner Schwarze
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Patent number: 4474947Abstract: Benzazoles, including benzatriazoles and benzimidazoles are employed in phospate triester oligonucleotide synthesis. The benzazoles form arylbenzazolide coupling agents, and phosphorodibenzazolides. Processes employing these reagents are also disclosed.Type: GrantFiled: April 8, 1982Date of Patent: October 2, 1984Assignee: BiosearchInventors: Derek Hudson, Ronald M. Cook
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Patent number: 4469686Abstract: The invention is directed to substituted phosphinic and phosphonic acids, a process for the preparation thereof and the use thereof for the treatment of inflammatory conditions, degenerative joint diseases and Wilson's disease.Type: GrantFiled: January 30, 1981Date of Patent: September 4, 1984Assignee: Hoffmann-La Roche Inc.Inventor: Kenneth J. M. Andrews
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Patent number: 4443609Abstract: This invention relates to tetrahydrothiazole phosphonic acids or phosphonates and to the preparation thereof by reacting dihydrothiazoles with phosphorous acid or esters thereof.Type: GrantFiled: May 19, 1980Date of Patent: April 17, 1984Assignee: Petrolite CorporationInventors: Bernardus A. Oude Alink, Derek Redmore
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Patent number: 4435533Abstract: This invention relates to novel 4-hydroxy-5-(substituted phosphinyl)ethyleneureas of the general Formula I ##STR1## to methods of making the same, to flame resistant compositions containing such compounds and to the use of compositions containing such compounds to impart flame resistance to cellulose and cellulose containing materials.In the compounds of the Formula I X or Y may be hydrogen or alkyl, R.sub.1 and R.sub.2 may be the same or different radicals including alkoxy, cycloalkoxy, aryloxy, arylalkoxy, alkyl, aryl as well as such radicals containing substituents such as halogen; in addition, R.sub.1 and/or R.sub.2 may be hydroxy.Type: GrantFiled: July 30, 1981Date of Patent: March 6, 1984Inventors: Alexandros K. Tsolis, Ioannis A. Mikroyannidis
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Patent number: 4426379Abstract: Compounds of the formula ##STR1## wherein R is hydrogen, lower alkyl or lower alkoxy, R.sup.1 and R.sup.2 are independently lower alkyl and Y is either oxygen or sulfur possess insecticidal activity.Type: GrantFiled: January 27, 1982Date of Patent: January 17, 1984Assignee: Chevron Research CompanyInventor: Laroy H. Edwards
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Patent number: 4413999Abstract: The invention provides amidoxime derivatives of the general formula ##STR1## wherein R.sub.1 is an alkyl group of 1 to 8 carbon atoms, phenyl, a heterocyclic ring structure of 5 to 8 atoms containing one or more nitrogen or oxygen atoms or combinations thereof or a bicyclic condensed ring system optionally containing at least one heterocyclic ring which groups may each be optionally substituted. R.sub.2 is a mono or bicyclic heterocyclic radical containing at least two nitrogen atoms which radical is also optionally substituted. R.sub.3 and R.sub.4 are independently H, or an alkyl of 1 to 4 carbon atoms or one, but not both, is ##STR2## and the other, H, wherein R.sub.5 or R.sub.6 are alkyls of 2 to 5 carbon atoms optionally substituted by R.sub.1, or a phenyl optionally substituted by R.sub.1 or R.sub.5 or R.sub.6 is combined with R.sub.1 to jointly form cyclic imidoximes or imidedioximes.Type: GrantFiled: March 5, 1982Date of Patent: November 8, 1983Assignee: Research Products Rehovot Ltd.Inventors: Charles Linder, Gershon Aviv
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Patent number: 4379147Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 independently of one another are each a chlorine atom or the methyl group, Y is the group ##STR2## or --CH.dbd.N--R.sub.5, in which R.sub.3 is methyl or ethyl, R.sub.4 is alkyl having 1 to 4 carbon atoms, alkoxy having 1 or 2 carbon atoms, alkylthio having 1 to 4 carbon atoms, or phenyl, X is an oxygen atom or a sulfur atom, and R.sub.5 is an unsubstituted or substituted pyridinyl group which is linked by way of one of its carbon atoms, to the main part of the molecule, and which has substituents selected from the group comprising halogen and alkyl having 1 to 4 carbon atoms, including the acid addition salts thereof, processes for producing the novel compounds by reaction of 2-(anilinomethyl)-2-imidazoline derivatives either with (thio)phosphoric acid dialkyl ester halides or alkyl(thio) phosphonic acid alkyl ester halides, or with N-pyridinylformiminoalkoxy derivatives.Type: GrantFiled: February 1, 1982Date of Patent: April 5, 1983Assignee: Ciba-Geigy CorporationInventors: Manfred Boger, Urs Burckhardt, Haukur Kristinsson, Gunter Mattern, Walter Traber
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Patent number: 4339443Abstract: There are described pesticidal compositions comprising one or more compounds of the formula I, ##STR1## in which Ra is a group R.sup.2 or --OR.sup.2,E is oxygen or sulphur,Rm is --O.sup..crclbar. M.sup..sym. or --NRyRz,M.sup..sym. is one equivalent of an agriculturally acceptable cation,R.sup.1 and R.sup.2, which may be the same or different, each represent hydrogen, alkyl, alkenyl, alkynyl or aryl; the alkyl, alkenyl, alkynyl or aryl optionally being substituted by one or more halogen, alkoxy, nitro, alkyl, --CF.sub.3, nitrile, or carboxylic acid or a salt, ester, or amide thereof, andRy and Rz, which may be the same or different, each represent hydrogen or alkyl,or an agriculturally acceptable derivative thereof.There are also described methods for making and using compounds of formula I.Type: GrantFiled: August 28, 1979Date of Patent: July 13, 1982Assignee: FBC LimitedInventors: Alister C. Baillie, Brian J. Wright, Kenneth Wright
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Patent number: 4322527Abstract: Compounds of the formula I ##STR1## wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.18 alkyl, C.sub.5 -C.sub.12 cycloalkyl, phenyl or C.sub.7 -C.sub.9 phenylalkyl and R.sub.2 is hydrogen or C.sub.1 -C.sub.18 alkyl, or, if R.sub.1 is hydrogen, R.sub.2 is a divalent 1,1,3,3,-tetramethylpropylene radical fused in the 2-position and 3-position or the 9-position and 10-position, and X is sulfur or a group --CH(R).sub.3 --, in which R.sub.3 is hydrogen or a radical of the formula II --CH(R.sub.4)--CH(R.sub.5)SR.sub.6, and each of R.sub.4 and R.sub.5 independently is hydrogen or C.sub.1 -C.sub.6 alkyl and R.sub.6 is C.sub.1 -C.sub.20 alkyl, while the alkyl group can be interrupted by one or more sulfur atoms, and A is a primary or secondary aliphatic or alicyclic, aromatic or araliphatic amine which contains substituents of the same type or mixed substituents, or a heterocyclic amine or a hydrazine derivative. These compounds are useful stabilizers for organic material.Type: GrantFiled: May 5, 1980Date of Patent: March 30, 1982Assignee: Ciba-Geigy CorporationInventor: Michael Rasberger