The Hetero Ring Contains Chalcogen Patents (Class 540/467)
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Patent number: 5252567Abstract: This invention concerns compounds of the formula I: ##STR1## wherein R.sup.1 is (1-10C)alkyl, (3-8C)cycloalkyl, (3-8C)cycloalkyl-(1-4C)-alkyl, phenyl or phenyl(1-4C)alkyl, the phenyl moiety of the latter two optionally bearing one or more substituents; R.sup.2 is hydrogen, (1-4C)alkyl, amino or (1-4C)alkylamino; R.sup.6 is (1-4C)alkyl, amino or (1-4C)alkylamino; Q is a group of formula II, in which case R.sup.3 and R.sup.4 are independently hydrogen, (1-4C)alkyl, phenyl or benzyl the phenyl moiety of the latter two optionally bearing one or two substituents; R.sup.5 is hydrogen, (1-4C)alkyl or (2-4C)alkenyl; A and B are independently ethylene or trimethylene; Z is a direct bond between A and B, or an oxy, thio, carbonyl, methylene, ethylenedioxymethylene, ethylidene, or isopropylidene link, or Z is a group of the formula .dbd.N.Type: GrantFiled: December 18, 1990Date of Patent: October 12, 1993Assignee: Imperial Chemical Industries PLCInventors: Stuart D. Mills, Rodney B. Hargreaves, Bernard J. McLoughlin
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Patent number: 5247078Abstract: Poly(ethyleneoxy)amines, such as those having the structure:H.sub.2 N--(CH.sub.2).sub.a --(OCH.sub.2 CH.sub.2).sub.b --NH--(CH.sub.2 CH.sub.2 O).sub.c --(CH.sub.2).sub.d --Rwhere a and d are independently 2 to 3; b and c are independently 1 to 4 and R is --OH or --NH.sub.2, may be reacted over a transition metal catalyst such as one containing nickel to produce diaza crown ethers, such as, for example 4,13-diaza-18-crown-6. If the poly(ethyleneoxy)amine is a diamine having a hydroxyl group of the above formula, the reaction may produce the corresponding triamine in the presence of ammonia. These triamines also readily form diaza crown ethers at near complete conversions simply from nickel, platinum, and palladium metal catalysts alone or with other transition metals such as copper and/or chromium. The process avoids tedious, multiple step procedures and the high dilutions that accompany prior diaza crown ether preparations.Type: GrantFiled: May 2, 1991Date of Patent: September 21, 1993Assignee: Texaco Chemical CompanyInventors: Donald H. Champion, George P. Speranza, Terry L. Renken
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Patent number: 5239070Abstract: There are provided alkyl esters of 5-heterocyclic-pyridine-2,3-dicarboxylic acids useful as intermediates for the preparation of highly effective 5-heterocyclic-2-(2-imidazolin-2-yl)pyridine herbicidal agents and methods for the preparation thereof.Type: GrantFiled: June 11, 1991Date of Patent: August 24, 1993Assignee: American Cyanamid CompanyInventor: John M. Finn
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Patent number: 5217706Abstract: Novel magnetic resonance imaging agents comprise complexes of paramagnetic ions with hydrazide derivatives of polyaminocarboxylic acid chelating agents. These novel imaging agents are characterized by excellent NMR image-contrasting properties and by high solubilities in physiological solutions.A novel method of performing an NMR diagnostic procedure involves administering to a warm-blooded animal an effective amount of a complex as described above and then exposing the warm-blooded animal to an NMR imaging procedure, thereby imaging at least a portion of the body of the warm-blooded animal.Type: GrantFiled: June 3, 1992Date of Patent: June 8, 1993Assignee: Mallinckrodt Medical, Inc.Inventors: Raghavan Rajagopalan, Rebecca A. Wallace, Muthunadar P. Periasamy
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Patent number: 5206235Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.Type: GrantFiled: February 28, 1992Date of Patent: April 27, 1993Assignee: Merck & Co., Inc.Inventors: Michael H. Fisher, William R. Schoen, Matthew J. Wyvratt, Robert J. DeVita
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Patent number: 5187103Abstract: A chromogenic cryptand found to be especially selective in the determination of lithium in blood of the general formula (I): ##STR1## where: n=1 or 2,R.sub.1 and R.sub.2, same or different, are hydrogen, lower alkyl, lower alkenyl, or lower alkylidene; andQ is a chromogenic moiety capable of providing a detectable response upon complexation of said compound with lithium ion and has the structure: ##STR2## wherein: X is CH, C--OH or N; and Z is p-nitrophenylazo, 2,4-dinitrophenylazo, 2,4,6-trinitrophenylazo, p-nitrostyryl, p-benzoquinonemonoimino, bis-(4-dimethylaminophenyl) hydroxymethyl, 3-phenylisothiazolyl-5-azo, thiazolyl-5-azo; or isothiazolyl-5-azo.A reagent composition and synthesis of a preferred chromogenic cryptand are also disclosed.Type: GrantFiled: January 31, 1991Date of Patent: February 16, 1993Assignee: Miles Inc.Inventors: Bronislaw P. Czech, Eddy Chapoteau, Anand Kumar
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Patent number: 5162508Abstract: The invention relates to rare earth cryptates consisting of at least one rare earth salt complexed by a macropolycyclic compound corresponding to one of formulae I or II below, in which:the ring ##STR1## is the N.sub.2 O.sub.4 macrocycle, the N.sub.2 O.sub.3 macrocycle or a bis-bipyridine macrocycle;Y is a spacer arm or group which consists of a divalent organic radical selected from linear or branched C.sub.1 to C.sub.20 alkylene groups optionally containing one or more double bonds and/or optionally being interrupted by one or more heteroatoms such as oxygen, nitrogen, sulfur or phosphorus, or from C.sub.5 to C.sub.8 cycloalkylene groups or C.sub.6 to C.sub.Type: GrantFiled: July 26, 1991Date of Patent: November 10, 1992Assignee: Compagnie Oris IndustrieInventors: Jean-Marie Lehn, Mathis Gerard, Beatrice Alpha, Robert Deschenaux, Etienne Jolu
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Patent number: 5159065Abstract: The present invention involves, in addition to many unique substituted sapphyrins, a novel method for synthesizing sapphyrins with good efficiency and high yield. An improved 9-step synthesis of substituted sapphyrins, e.g., the two C.sub.2 symmetric sapphyrins, compounds 2 and 4 of FIG. 1C, is described herein. This synthesis involves as an important step the condensation between a tripyrrane diacid and a diformyl bipyrrole. The key tripyrrane component is prepared in three high-yield steps from readily available pyrrolic precursors and the bipyrrole portion is prepared in four steps from ethyl 3-methyl-4-methylpyrrole-2-carboxylate in roughly 33% yield overall.Type: GrantFiled: December 21, 1989Date of Patent: October 27, 1992Assignee: Board of Regents, The University of Texas SystemInventors: Jonathan L. Sessler, Michael J. Cyr
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Patent number: 5157149Abstract: A method of making substantially pure L-BPA is disclosed. The method includes the steps of reacting 4-bromobenzaldehyde with ethylene glycol to form 4-bromobenzaldehyde ethylene glycol acetal, sequentially reacting 4-bromobenzaldehyde ethyleneglycol acetal with Mg to produce the Grignard reagent and thereafter reacting with tributyl borate and then converting to an acid environment to form 4-boronobenzaldehyde, reacting 4-boronobenzaldehyde with diethanol amine to form 4-boronobenzaldehyde diethanolamine ester, condensing the 4-boronobenzaldehyde diethanolamine ester with 2-phenyl-2-oxazolin-5-one to form an azlactone, reacting the azlactone with an alkali metal hydroxide to form z-.alpha.-benzoylamino-4-boronocinnamic acid, asymmetrically hydrogenating the z-.alpha.Type: GrantFiled: June 4, 1991Date of Patent: October 20, 1992Assignee: The United States of America as represented by the United States Department of EnergyInventor: Edward G. Samsel
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Patent number: 5135563Abstract: The present invention relates to a pyrimidine derivative having the formula ##STR1## (wherein the variables are defined in the full text of the patent), a method for producing the same, and its use as a herbicide.Type: GrantFiled: July 5, 1991Date of Patent: August 4, 1992Assignee: Sumitomo Chemical Company, LimitedInventors: Mitsunori Hiratsuka, Naonori Hirata, Kazuo Saitoh, Hideyuki Shibata
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Patent number: 5134232Abstract: The invention discloses fluorescent chelator compounds that are especially useful to monitor and measure cytosolic concentrations of alkali metal cations such as Na.sup.+, K.sup.+, and Li.sup.+. The new compounds are comprised of: (1) crown ethers (that may or may not have substituent groups attached to the core carbons, but will always contain at least one core nitrogen) that are linked via the core nitrogen(s) to at least one (2) fluorophore that contains an additional heteroaromatic liganding center. In the currently preferred dye, SBFI, the core compound is crown ether 1,7-diaza-4,10,13-trioxacyclopentadecane and the heteroaromatic fluorophores are benzofurans that are linked to isophthalate groups. Selectivities for Na.sup.+ over K.sup.+ of about 20 are observed, resulting in effective dissociation constants for Na.sup.+ of about 20 mM against a background of 120 mM K.sup.+. Increasing [Na.sup.Type: GrantFiled: August 9, 1989Date of Patent: July 28, 1992Assignee: The Regents of the University of CaliforniaInventors: Roger Y. Tsien, Akwasi Minta
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Patent number: 5125957Abstract: A pyrimidine derivative represented by the formula ##STR1## wherein the variables are defined below in the specification, and their production and herbicidal activities are described.Type: GrantFiled: October 24, 1990Date of Patent: June 30, 1992Assignee: Sumitomo Chemical Company, LimitedInventors: Mitsunori Hiratsuka, Naonori Hirata, Kazuo Saito, Hideyuki Shibata
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Patent number: 5110585Abstract: The invention relates primarily to quaternized polycyclic compounds having the formula ##STR1## wherein m is an integer having a value of from 1 to 4; R is alkylene having from 3 to 8 carbon atoms and is optionally substituted with C.sub.1 to C.sub.4 alkyl; R.sub.2 together with the quaternary nitrogen, forms a 5 to 14 membered heterocyclic ring, said ring containing at least 2 hetero atoms selected from the group of nitrogen, sulfur and oxygen; R.sub.1 forms a double bond in the heterocyclic ring of the quaternized nitrogen or is alkyl, alkyleneoxyalkyl, alkylhydroxy, aryl, aralkyl, aralkenyl, alkaryl, alkylamidoalkyl and X.sup.- is an anion. The invention also relates to the preparation and use of said quaternized polycyclic compounds.Type: GrantFiled: March 1, 1989Date of Patent: May 5, 1992Assignee: ISP Investments Inc.Inventors: Ratan K. Chaudhuri, David J. Tracy, Robert B. Login, Michael W. Helioff
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Patent number: 5103004Abstract: Heterocyclically substituted N-sultamsulfonamides, processes for their preparation and their use as herbicides and plant growth regulators.Compounds of the formula I or their salts ##STR1## wherein R.sup.1 and R.sup.2 denote H, halogen, alkyl, alkenyl, alkynyl or alkoxy, which can be substituted, or denote --(CH.sub.2).sub.n --COOR.sup.11 ;R.sup.3 denotes H, alkyl, alkenyl or alkynyl;R.sup.4 denotes a heterocyclic radical of the formulae ##STR2## where E is CH or N; X is O or S and a, b, c, d, e in each case denote 0, 1 or 2, with the proviso that c+d+e.gtoreq.2, possess excellent herbicidal and plant growth-regulating properties.Type: GrantFiled: August 23, 1991Date of Patent: April 7, 1992Assignee: Hoesch AktiengellschaftInventors: Lothar Willms, Klaus Bauer, Hermann Bieringer, Helmut Burstell
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Patent number: 5089471Abstract: Non-peptidyl compounds characterized generally as .beta.-aminoacyl aminodiol carbamates are useful as renin inhibitors for the treatment of hypertension.Type: GrantFiled: October 1, 1987Date of Patent: February 18, 1992Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5089175Abstract: Hydroxyalkane carboxylic acid derivatives of general formula I ##STR1## in which n means the numbers 7 to 18,R.sub.1 represents a hydrogen atom or an acyl group with a maximum of 16 carbon atoms, andoptionally an alkylene group with 4 to 8 carbon atoms interrupted by an oxygen atom or a nitrogen atom, are useful for the production of pharmaceutical agents for local treatment of diseases of the skin and mucous membranes.Type: GrantFiled: February 16, 1990Date of Patent: February 18, 1992Assignee: Schering AktiengesellschaftInventors: Christopher G. Earnshaw, Gerald Kirsch, Petra Rach, Ruth Thieroff-Ekerdt, Michael Topert
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Patent number: 5087696Abstract: A conjugate compound has the structure (I), wherein R.sup.1 is --(CH.sub.2).sub.p --R.sup.6 --(CH.sub.2).sub.q -- where p and q are the same or different and are 0, 1 or 2, and --R.sup.6 -- is --(CH.sub.2).sub.n --, where n is 0 or 1, --NH--, --O--, --S-- or (II), R.sup.1 optionally being alkyl substituted, provided that neither p nor q is 0 unless R.sup.6 is --CH.sub.2 --; R.sup.2 are --CH.sub.2 CH.sub.2 -- or --CH.sub.2 CH.sub.2 CH.sub.2 --, optionally alkyl, alkoxyalkyl or hydroxyalkyl substituted; R.sup.3 are the same or different and are --H, alkyl, hydroxyalkyl, alkoxyalkyl, carboxyalkyl, carboxyalkyl ester, phosphate, sulphonate or phosphonate; R.sup.4 is one of the compounds of formula (III) optionally alkyl substituted, wherein R.sup.7 is --H, alkyl, hydroxyalkyl, or alkoxyalkyl provided that when R.sup.4 is (III d), R.sup.3 is not carboxyalkyl, R.sup.5 is a linker, and Ab is an antibody.Type: GrantFiled: December 14, 1987Date of Patent: February 11, 1992Assignee: Celltech LimitedInventors: David Parker, Thomas A. Millican
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Patent number: 5073185Abstract: Compounds of the formula I or their salts ##STR1## wherein R.sup.1 and R.sup.2 denote H, halogen, alkyl, alkenyl, alkynyl or alkoxy, which can be substituted, or denote --(CH.sub.2).sub.n --COOR.sup.11 ;R.sup.3 denotes H, alkyl, alkenyl or alkynyl;R.sup.4 denotes a heterocyclic radical of the formulae ##STR2## where E is CH or N; X is O or S and a, b, c, d, e in each case denote 0, 1 or 2, with the proviso that c+d+e.gtoreq.2, possess excellent herbicidal and plant growth-regulating properties.Type: GrantFiled: March 15, 1990Date of Patent: December 17, 1991Assignee: Hoechst AktiengesellschaftInventors: Lothar Willms, Klaus Bauer, Hermann Bieringer, Helmut Burstell
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Patent number: 5064956Abstract: The invention relates to a novel process to prepare selectively mono-N-alkylated polyazamacrocycles which requires an electrophile with between about one and five equivalents of a suitable macrocycle in a solvent which will not promote a proton transfer.Type: GrantFiled: July 9, 1990Date of Patent: November 12, 1991Assignee: The Dow Chemical CompanyInventor: William J. Kruper, Jr.
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Patent number: 5041545Abstract: Hydrazide functionalized 2-hydroxybenzophenone ultraviolet light and heat stabilizers and derivatives are disclosed having the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, Y, Z, all substituents thereof, and n are set forth in the Summary of the Invention. Y--N(R.sup.6)--Z is the hydrazide or derivative group and --X--R.sup.5 -- links the hydrazide group to an aromatic nucleus of the optionally substituted benzophenone group. Derivatives are, for example, acyl hydrazides, diacyl hydrazides (including imides), hydrazones and alkyl hydrazides. The compounds are useful as ultraviolet light absorbers and heat stabilizers for plastics.Type: GrantFiled: April 6, 1989Date of Patent: August 20, 1991Assignee: Atochem North America, Inc.Inventor: Terry N. Myers
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Patent number: 5015284Abstract: Compounds of the formula I, their stereoisomers or their salts ##STR1## wherein A denotes >C(R.sup.4).sub.2 or >C.dbd.C(R.sup.5).sub.2 ; R.sup.1 denotes H, an optionally substituted aliphatic or cycloaliphatic radical, forfuryl, tetrahydrofurfuryl or (substituted) phenyl; R.sup.2 denotes H, alkyl, alkenyl, alkynyl or alkoxy; R.sup.3 denotes a radical of the formulae ##STR2## X denotes O, S or NR.sup.12 and Y denotes O or S, possess excellent herbicidal and plant-growth regulating properties.Type: GrantFiled: April 6, 1989Date of Patent: May 14, 1991Assignee: Hoechst AktiengesellschaftInventors: Lothar Willms, Klaus Bauer, Hermann Bieringer, Helmut Burstell
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Patent number: 5003074Abstract: Compounds of formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are H, alkyl or aryl, m and n are 0 or 1, and A is a divalent organic radical which, with (CR.sup.1 R.sup.2).sub.m NF--SO.sub.2 (CR.sup.3 R.sup.4).sub.n groups, forms a 5- to 8-membered ring, are admirably suitable fluorinating agents for fluorinating carbon atoms, especially as stereospecific fluorinating agents, when the compounds contain a chiral carbon atom and are in optically active form. The compounds of formula I are prepared by reacting the corresponding silated sulfonamides, wherein the NF group is replaced by an N-SiR.sup.7 R.sup.8 R.sup.9 group and R.sup.7, R.sup.8 R.sup.9 are each independently C.sub.1 -C.sub.12 alkyl, cyclopentyl, cyclohexyl, benzyl or phenyl, with a fluorinating agent.Type: GrantFiled: September 28, 1988Date of Patent: March 26, 1991Assignee: Ciba-Geigy CorporationInventors: Thomas Allmendinger, Edmond Differding, Robert W. Lang
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Patent number: 4988723Abstract: Benzopyran derivatives of formula (I) wherein the substituents are as defined herein are provided. The compounds possess vasodilating activity and are useful in the treatment of hypertension. Pharmaceutical compositions and methods of treating hypertension are also provided.Type: GrantFiled: May 17, 1989Date of Patent: January 29, 1991Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Youichi Shiokawa, Koichi Takimoto, Kohei Takenaka, Takeshi Kato
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Patent number: 4987137Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof; ##STR1## wherein: R.sub.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen;R.sub.2 and R.sub.3 are both hydrogen or together represent a bond;R.sub.4 is hydrogen and R.sub.5 is hydrogen or R.sub.4 and R.sub.5 together represent an oxo group;R.sub.6 is C.sub.1-7 alkyl substituted by NR.sub.8 R.sub.9 where R.sub.8 and R.sub.9 are independently hydrogen or C.sub.1-4 alkyl or together are C.sub.3-7 polymethylene optionally containing a further heteroatom which is oxygen, sulphur or nitrogen substituted by R.sub.10 where R.sub.10 is hydrogen, C.sub.1-4 alkyl or benzyl, and optionally substituted by one or two C.sub.1-4 alkyl, C.sub.2-5 alkanoyl, C.sub.1-4 alkoxycarbonyl, aminocarbonyl optionally substituted by one or two C.sub.1-6 alkyl groups or by a benzyl group, cyano, phenyl or benzyl and wherein any phenyl or benzyl group is optionally substituted in the phenyl ring by one or two halo, CF.sub.3, C.sub.1-4 alkyl, C.sub.Type: GrantFiled: April 20, 1989Date of Patent: January 22, 1991Assignee: Beecham Wuelfing GmbH & Co., KGInventors: Dagmar Hoeltje, Dietrich Thielke
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Patent number: 4977148Abstract: The invention concerns novel phenoxyacetic acid amide derivatives of the formula I (and pharmaceutically acceptable salts thereof) in which R.sup.1 is hydrogen or fluoro, R.sup.2 is phenyl, cycloalkyl, alkyl or alkenyl as defined herein, and R.sup.3 is hydrogen, methyl or ethyl, or R.sup.2 and R.sup.3 together form polymethylene as defined herein. The invention also includes pharmaceutical compositions containing the amide derivatives, means for the manufacture of the said derivatives and for their use in the treatment of obesity and related conditions and/or in the manufacture of novel medicaments.Type: GrantFiled: March 8, 1990Date of Patent: December 11, 1990Assignee: Imperial Chemical IndustriesInventors: Brian R. Holloway, Ralph Howe, Balbir S. Rao, Donald Stribling
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Patent number: 4977141Abstract: Non-peptidyl compounds characterized generally as aminoacyl aminodiol carbamates are useful as renin inhibitors for the treatment of hypertension.Type: GrantFiled: October 1, 1987Date of Patent: December 11, 1990Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 4957941Abstract: A new class of anti-spasmodic compounds having two branch chains is provided. The compounds have the general formula: ##STR1## where Y is H or OH;j is an integer from 0 to 4;k is an integer from 0 to 4, and whereinm is an integer from 1 to 4;n is an integer from 1 to 4;p is an integer from 1 to 4; andX may be nonexistent or may be O, S, NH or CH.sub.2 or salts thereof, but when X is nonexistent the terminal group in which both the n-chain and the p-chain is a methyl group. ##STR2## The reaction was performed under reflux condensation. Following the reaction, which was usually complete within a few hours, the acid chlorides were vacuum distilled and reacted with a thiol compound as described above.The compounds of this invention are anti-muscarinic agents (cholinergic-muscarinic receptor antagonists) which inhibit the actions of acetylcholine on autonomic effectors innervated by postganglionic cholinergic nerves as well as on smooth muscle that lacks cholinergic innervation.Type: GrantFiled: January 9, 1990Date of Patent: September 18, 1990Assignee: United Pharmaceuticals, Inc.Inventor: William M. Davis
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Patent number: 4927836Abstract: The invention concerns novel phenoxyacetic acid amide derivatives of the formula I (and pharmaceutically acceptable salts thereof) in which R.sup.1 is hydrogen or fluoro, R.sup.2 is phenyl, cycloalkyl, alkyl or alkenyl as defined herein, and R.sup.3 is hydrogen, methyl or ethyl, or R.sup.2 and R.sup.3 together form polymethylene as defined herein. The invention also includes pharmaceutical compositions containing the amide derivatives, means for the manufacture of the said derivatives and for their use in the treatment of obesity and related conditions and/or in the manufacture of novel medicaments.Type: GrantFiled: June 29, 1988Date of Patent: May 22, 1990Assignee: Imperial Chemical Industries PLCInventors: Brian R. Holloway, Ralph Howe, Balbir S. Rao, Donald Stribling
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Patent number: 4925480Abstract: Compounds of the formula I or their salts ##STR1## wherein R.sup.1 and R.sup.2 denote H, halogen, alkyl, alkenyl, alkynyl or alkoxy, which can be substituted, or denote --(CH.sub.2).sub.n --COOR.sup.11 ;R.sup.3 denotes H, alkyl, alkenyl or alkynyl;R.sup.4 denotes a heterocyclic radical of the formulae ##STR2## where E is CH or N; X is O or S nd a, b, c, d, e in each case denote 0, 1 or 2, with the proviso that c+d+e.gtoreq.2, possess excellent herbicidal and plant growth-regulating properties.Type: GrantFiled: October 28, 1988Date of Patent: May 15, 1990Assignee: Hoechst AktiengesellschaftInventors: Lothar Willms, Klaus Bauer, Hermann Bieringer, Helmut Burstell
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Patent number: 4910304Abstract: N-substituted cyclic amines of the general formula I ##STR1## where A is an alkylene group or a --(CH.sub.2).sub.n --[--O--(CH.sub.2).sub.m ].sub.r group which may be monosubstituted or polysubstituted by radicals R without the radicals R in a defined compound having to be identical, R is alkyl, alkoxyalkyl, unsubstituted or alkyl-substituted or alkoxy-substituted cycloalkyl, cycloalkylalkyl, aryl or arylalkyl, n and m independently of one another are each from 2 to 8 and r is from 1 to 3, the --(CH.sub.2).sub.n --[O--(CH.sub.2).sub.m ].sub.r group consisting of from 5 to 12 members, are prepared by reacting a primary amine of the general formula IIR--NH.sub.Type: GrantFiled: March 31, 1989Date of Patent: March 20, 1990Assignee: BASF AktiengesellschaftInventors: Roman Fischer, Herbert Mueller, Dieter Voges
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Patent number: 4906281Abstract: Disclosed are herbicidal compounds of the formula ##STR1## wherein W is sulfur or oxygen;X is Br, Cl, F, alkyl, or haloalkyl; Y is Br, Cl, F, methyl, haloalkyl, haloalkoxy, nitro, or a radical of the formula --CH.sub.2 QR.sup.8 in which Q is O, S, S(O), or S(O).sub.2 and R.sup.8 is alkyl, alkenyl, alkynyl, optionally substituted phenyl; R is alkyl, haloalkyl, dialkylamino, carboxymethyl, hydroxy, or optionally substituted phenyl; R.sup.1 is hydrogen, alkyl, benzyl, haloalkyl, alkoxy, alkynyl, alkenyl, alkoxymethyl, cyanomethyl, hydroxycarbonylmethyl, alkoxycarbonylmethyl, or a group of the formula --SO.sub.2 R or --alkylene--SO.sub.2 R in which R is as defined above; or R and R.sup.1 together are a divalent alkylene radical; or a base addition salt of a compound as defined above in which R or R.sup.1 is or contains an acidic proton.Type: GrantFiled: July 1, 1988Date of Patent: March 6, 1990Assignee: FMC CorporationInventor: Jun H. Chang
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Patent number: 4886792Abstract: 10-dihydro-10-deoxo-11-azaerythronolide A compounds and pharmaceutically acceptable acid addition salts of said compounds; methods and intermediates for the manufacture thereof; their use as antiinflammatory agents and processes for their preparation.Type: GrantFiled: April 12, 1988Date of Patent: December 12, 1989Assignee: Sour PlivaInventors: Slobodan Djokic, Nevenka Lopotar, Gabrijela Kobrehel, Hrvoje Krnjevic, Olga Carevic
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Patent number: 4885363Abstract: Metal-chelating liquids having the formula ##STR1## wherein Y is oxygen or ##STR2## R.sub.Type: GrantFiled: December 23, 1987Date of Patent: December 5, 1989Assignee: E. R. Squibb & Sons, Inc.Inventors: Michael F. Tweedle, Glen T. Gaughan, James T. Hagan
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Patent number: 4870063Abstract: Novel compounds of the formula I ##STR1## in which R.sub.1 -R.sub.11 can be the same or different and stand for hydrogen, a straight or branced aliphatic or alicyclic C.sub.1 -C.sub.10 hydrocarbon radical, an aryl or an aryl-C.sub.1 -C.sub.4 -alkyl radical; n is zero or one, and m is zero, one or two; or R.sub.2 and R.sub.4 when taken together form a saturated aliphatic 5-, 6- or 7-membered ring which may be substituted with one or more C.sub.1 -C.sub.4 alkyl radicals; and pharmaceutically acceptable salts and easily hydroyzable esters thereof, methods for producing said new compounds, pharmaceutical compositions containing the new compounds, dosage units of the compositions, and methods of treating patients using said compositions and dosage units.The present compounds are valuable in the human and veterinary practice by reducing bone resorption and surprisingly also stimulating bone alkaline phosphatase. A substantial increase in bone mass is actually observed during treatment with the present compounds.Type: GrantFiled: August 10, 1987Date of Patent: September 26, 1989Assignee: Leo Pharmaceutical Products Ltd. A/SInventors: Ernst T. Binderup, Sven Liisberg
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Patent number: 4851524Abstract: Thio-bis-(hydrocarbyl substituted diacid materials), such as thio-bis-(polyalkyl lactone acid) and/or their precursors, the adducts of sulfur chloride and unsaturated diacid materials, e.g., 4,8-bis-polyalkyl-4, 8-dichloro-6-thiaundecane-1,2,10,11-tetracarboxylic acid bis-anhydride and especially their dehydrochlorinated analogs, when treated with an amine preferably polyalkylene polyamines such as tetraethylene pentamine, directly or in the presence of a metal template reagent, yield aminated thio-bis-(alkyl lactone acid) and thio-bis-(hydrocarbyl diacid) materials or their metal complexes which can be characterized in part, as macrocyclic and/or macrocyclic-like amide and/or imide structures, are useful as stable additives in lubricating compositions, e.g., as varnish inhibiting dispersants and/or inhibitors for lubricating oils and fuels.Type: GrantFiled: November 27, 1985Date of Patent: July 25, 1989Assignee: Exxon Research and Engineering CompanyInventors: Stanley J. Brois, Antonio Gutierrez
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Patent number: 4835271Abstract: A compound of the formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen;R.sub.2 and R.sub.3 are both hydrogen or together represent a bond;R.sub.4 is hydrogen and R.sub.5 is hydrogen or R.sub.4 and R.sub.5 together represent an oxo group;R.sub.6 is C.sub.1-7 alkyl substituted by NR.sub.8 R.sub.9 where R.sub.8 and R.sub.9 are independently hydrogen or C.sub.1-4 alkyl or together are C.sub.3-7 polymethylene optionally containing a further hetereoatom which is oxygen, sulphur or nitrogen substituted by R.sub.10 where R.sub.10 is hydrogen, C.sub.1-4 alkyl or benzyl, and optionally substituted by one or two C.sub.1-4 alkyl, C.sub.2-5 alkanoyl, C.sub.1-4 alkoxycarbonyl, aminocarbonyl optionally substituted by one or two C.sub.1-6 alkyl groups or by a benzyl group, cyano, phenyl or benzyl and wherein any phenyl or benzyl group is optionally substituted in the phenyl ring by one or two halo, CF.sub.3, C.sub.1-4 alkyl, C.sub.Type: GrantFiled: June 26, 1986Date of Patent: May 30, 1989Assignee: Beecham-Wuelfing GmbH & Co., KGInventors: Dagmar Hoeltje, Dietrich Thielke
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Patent number: 4818754Abstract: A compound of the formula (1) or a salt or solvate thereof: ##STR1## in which: R.sub.0 is hydrogen or C.sub.1-6 alkyl;R.sub.1 and R.sub.2 are both hydrogen; orR.sub.1 is hydrogen, C.sub.1-6 alkyl; and R.sub.2 is CN; CR.sub.5 R.sub.6 Y where R.sub.5 and R.sub.6 are independently selected from hydrogen and C.sub.1-4 alkyl and Y is selected from hydrogen, OR.sub.7 or SR.sub.7 where R.sub.7 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkanoyl, and NR.sub.8 R.sub.9 where R.sub.8 and R.sub.9 are independently hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkanoyl or together are C.sub.4-6 polymethylene; or COR.sub.10 is OH or C.sub.1-4 alkyl, or COR.sub.10 is a pharmaceutically acceptable ester or amide; orR.sub.2 is hydrogen, C.sub.1-6 alkyl, or phenyl optionally substituted by halogen, CF.sub.3, C.sub.1-4 alkoxy or C.sub.1-4 alkyl; and R.sub.1 is CN, CR.sub.5 R.sub.6 Y or COR.sub.10 as defined for R.sub.2 above; orR.sub.1 and R.sub.2 together form C.sub.3 -C.sub.Type: GrantFiled: April 16, 1987Date of Patent: April 4, 1989Assignee: Beecham Group p.l.c. of Beecham HouseInventors: Robert W. Ward, Roger E. Markwell, Ian Hughes
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Patent number: 4804658Abstract: This invention relates to novel imidazopyridine derivatives useful in the treatment of diseases or disorders mediated by platelet-activating factor. This invention further relates to pharmaceutical compositions of such imidazopyridine derivatives.Type: GrantFiled: September 15, 1986Date of Patent: February 14, 1989Assignee: G. D. Searle & Co.Inventors: Paul W. Manley, Roderick A. Porter
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Patent number: 4775406Abstract: The salts of 1-phenylimidazole-5-carboxylic acids substituted in the phenyl ring, of the general formula (I) ##STR1## exhibit a good plant growth-regulating activity. In the general formula the symbols have the following meaning:Y is an ammonium ion substituted up to fourfold by (substituted) alkyl, (substituted) alkenyl, alkynyl, (substituted) cycloalkyl, cycloalkenyl, and (substituted) phenyl, wherein the charged N may be part of a heterocyclic radial (NH.sub.4.sup.+ is excepted); phosphonium ion substituted fourfold by alkyl, (substituted) phenyl or (substituted) benzyl; sulfonium- or sulfoxonium ion substituted threefold by alkyl, (substituted) phenyl or (substituted) benzyl; the guanidinium ion or an O-alkylisourea cation;R.sup.1, R.sup.2 independently of each other are alkyl;R.sup.3 is alkyl, alkoxy or halogen; andn is 0, 1, 2 or 3.Type: GrantFiled: November 21, 1985Date of Patent: October 4, 1988Assignee: Hoechst AktiengesellschaftInventors: Roland Schmierer, Ernst-Friedrich Schulze, Helmut Bustell, Erwin Hacker
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Patent number: 4772695Abstract: A process for the preparation of vinyl carbamates of formula I ##STR1## is described which comprises heating an .alpha.-halogeno-carbamate of formula II ##STR2## in which X is a halogen atom at a temperature between 70.degree. and 250.degree. C. for a period of time between several minutes up to several hours. R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are the same or different. The process is applicable to a great variety of products in which R.sub.1, R.sub.2, R.sub.3, and R.sub.4 have different meanings. The process permits to prepare in a simple and economical fashion, vinyl carbamates, which have industrial value and novel vinyl carbamates.Type: GrantFiled: September 19, 1983Date of Patent: September 20, 1988Assignee: Societe Nationale des Poudres et ExplosifsInventors: Roy A. Olofson, Gary P. Wooden, Jonathan T. Martz
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Patent number: 4742055Abstract: A class of 3- and 5-amino thiatriazine compounds exhibiting pharmacological activity, including anti-ulcerogenic and gastrointestinal cytoprotective activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.Type: GrantFiled: April 27, 1984Date of Patent: May 3, 1988Assignee: Rorer Pharmaceutical CorporationInventors: William L. Studt, Donald E. Kuhla, Henry F. Campbell, Stuart A. Dodson
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Patent number: 4734406Abstract: Compounds of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and Y have the indicated meanings, their physiologically tolerated acid addition salts, and a process for the preparation of these compounds, are described. The compounds inhibit thromboxane synthetase and can thus be used as medicaments.Type: GrantFiled: March 11, 1986Date of Patent: March 29, 1988Assignee: Hoechst AktiengesellschaftInventors: Hans-Hermann Lau, Wilhelm Bartmann, Gerhard Beck, Gunther Wess
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Patent number: 4729995Abstract: Novel pyrimidine compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.1 ' are each hydrogen atom, a lower alkyl, benzyl, an alkali metal, or ammonium; R.sub.2 is hydrogen atom, a halogen atom, a lower alkyl, a lower alkoxy, an aryl, a group of the formula: ##STR2## (wherein R.sub.3 and R.sub.4 are each hydrogen atom, a lower alkyl, or an aryl), or a group of the formula: ##STR3## [wherein R.sub.5 and R.sub.6 are each an alkylene having 1 to 3 carbon atoms, and X is oxygen atom, methylene, or a group of the formula: >N-Y (wherein Y is hydrogen atom, a lower alkyl, benzyl, or an aryl)], which have excellent antiallergic activities and are useful for the prophylaxis and treatment of various allergic diseases, and a pharmaceutical composition containing said pyrimidine compound as an active ingredient.Type: GrantFiled: April 3, 1987Date of Patent: March 8, 1988Assignee: Toyo Boseki Kabushiki KaishaInventors: Hiroaki Taguchi, Takeo Katsushima, Masakazu Ban, Shoichi Aoki, Akihiko Watanabe
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Patent number: 4713187Abstract: Disclosed herein are additives which are useful as dispersants and detergents in lubricating oils and fuels. In particular, this invention is directed toward polyamino alkenyl or alkyl succinimides wherein one or more of the amino nitrogens of the succinimide is substituted with ##STR1## wherein R.sub.4 is hydrocarbyl of from 1 to 30 carbon atoms; R.sub.5 is hydrocarbyl of from 2 to 30 carbon atoms or --R.sub.6 --(OR.sub.6).sub.p -- wherein R.sub.6 is alkylene of 2 to 5 carbon atoms and p is an integer from 1 to 100; and m is an integer of from 0 to 1.Type: GrantFiled: March 2, 1987Date of Patent: December 15, 1987Assignee: Chevron Research CompanyInventors: Thomas F. Buckley, III, Robert H. Wollenberg
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Patent number: 4702851Abstract: Disclosed are additives which are useful as dispersants in lubricating oils, gasolines, marine crankcase oils and hydraulic oils. In particular, disclosed are additives prepared by (a) first reacting a polyamine with a cyclic carbonate; (b) reaction of this intermediate with an alkenyl or alkyl succinic anhydride; and (c) reaction of the product of (b) with a boron compound.Type: GrantFiled: October 8, 1986Date of Patent: October 27, 1987Assignee: Chevron Research CompanyInventor: Robert H. Wollenberg
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Patent number: 4695391Abstract: Disclosed are additives which are useful as dispersants in marine crankcase oils, hydraulic oils, and lubricating oils. In particular, disclosed are polyamino alkenyl or alkyl succinimides modified by reaction with a compound of the formula: ##STR1## wherein R.sub.4 is selected from the group consisting of a divalent hydrocarbyl group of from 2 to 30 carbon atoms with the proviso that the hydrocarbyl carbon atom bound to one ##STR2## group is not also bound to the other ##STR3## group and --R.sub.5 --OR.sub.5 --.sub.p wherein R.sub.5 is alkylene of from 2 to 5 carbon atoms and p is an integer of from 1 to 100; X is selected from the group consisting of bromo, chloro and --OR.sub.6 wherein R.sub.6 is selected from the group consisting of alkyl of from 1 to 6 carbon atoms, phenyl and phenyl substituted with 1 to 2 substituents selected from the group consisting of chloro, bromo, nitro, alkyl of from 1 to 6 carbon atoms and trifluoromethyl; and m is independently an integer of from 0 to 1.Type: GrantFiled: September 4, 1986Date of Patent: September 22, 1987Assignee: Chevron Research CompanyInventor: Thomas F. Buckley
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Patent number: 4687844Abstract: A process for the direct preparation of N,N-di-substituted derivatives of 4,13-diaza-18-crown-6 in which the substituents on both nitrogen atoms are identical and derive originally from an amine, by reacting a 1,8-diiodo-3,6-dioxooctane or derivatives thereof in which the substituents are located on positions 1, 2, 4, 5, 7 or 8 or combinations thereof, with a molar equivalent of a primary amine in the presence of a base and solvent.Type: GrantFiled: April 11, 1986Date of Patent: August 18, 1987Assignee: University of MarylandInventors: George W. Gokel, Vincent J. Gatto
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Patent number: 4659815Abstract: Chromogenic aza-12-crown-4 ethers which can be used for the spectrophotometric determination of lithium ion in aqueous solutions are disclosed. The compounds of the invention are particularly useful for the analysis of Li.sup.30 in the presence of Na.sup.+, a situation common in biological and geological systems. The compounds [e.g., 1-(2-oxy-5-nitrobenzyl)-1-hydro-1-aza-4,7,10-trioxacylclododecane], their methods of manufacture, and methods of utilizing the compounds for the analysis of lithium are disclosed and claimed.Type: GrantFiled: February 4, 1985Date of Patent: April 21, 1987Assignee: The President and Trustees of the Miami UniversityInventors: Gilbert E. Pacey, Ken-ichi Sasaki
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Patent number: 4656295Abstract: A process for isolating macrocyclic polyethers from open-chained polyglycols in a mixture by extraction with saturated hydrocarbons in the presence of at least 10 percent by weight ethylene glycol based on the weight of the mixture of macrocyclic polyethers and open-chained polyglycols.Type: GrantFiled: June 6, 1985Date of Patent: April 7, 1987Assignee: Consortium fur Elektrochemische Industrie GmbHInventor: Norbert Gamon
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Patent number: 4654339Abstract: Novel 3-amino-tetrahydro-1,3-thiazine-2,4-diones as well as skin treating compositions on the basis of a physiologically compatible carrier and customary additions containing these novel 3-amino-tetrahydro-1,3-thiazin-2,4-dione derivatives as active ingredients for thickening the epidermis. The skin treating compositions are applied 1-2 times daily on the skin for about 3 to 4 weeks. Due to the thickening of the epidermis they cause a strengthening of the skin protection, in particular against sun rays, cold and the contact with harmful environmental substances of all kinds. Moreover, the skin treating compositions are suitable for prophylactically fighting the so-called ageing of skin.Type: GrantFiled: October 9, 1984Date of Patent: March 31, 1987Assignee: Wella AktiengesellschaftInventors: Wolfgang Hanefeld, Rudi Rothlisberger, Friedrich Noser