Chalcogen Double Bonded Directly To A Ring Carbon Of The Hetero Ring Which Is Adjacent To The Ring Nitrogen (e.g., Laurolactam, Etc.) Patents (Class 540/451)
-
Patent number: 5721361Abstract: A process for preparing a substituted polyazamacrocycle is provided which comprises contacting a diamine or triamine and a dicarboxylic acid or ester or anhydride thereof in the presence of a suitable base and a suitable solvent to produce the substituted polyazamacrocycle provided that when an ester of said dicarboxylic acid is used, said suitable base is optional, and when said dicarboxylic acid or an anhydride of said dicarboxylic acid is used, the reaction mixture further comprises a suitable coupling agent.Type: GrantFiled: June 11, 1996Date of Patent: February 24, 1998Assignee: The Monsanto CompanyInventors: Patrick J. Lennon, Susan L. Henke, Karl W. Aston
-
Patent number: 5693630Abstract: Compounds of the general formula ##STR1## or pharmaceutically acceptable salts thereof, wherein Z is a saturated or unsaturated 3 to 6 carbon chain,m is 2 or 3,R.sub.1 is a hydrogen atom, or a straight or branched C.sub.1-4 alkyl group,R.sub.2, R.sub.3 and R.sub.13 are situated in the ortho, meta, or para position of the phenyl ring and are the same or different and selected from the following groups: H, OH, OR.sub.14, halogen, CO.sub.2 R.sub.9, CN, CF.sub.3, NO.sub.2, NH.sub.2, COCH.sub.3,OSO.sub.2 CF.sub.3,OSO.sub.2 CH.sub.3,CONR.sub.10 R.sub.11, OCOR.sub.12, whereinR.sub.9, R.sub.12 and R.sub.14 is a straight or branched C.sub.1-4 alkyl group,R.sub.10 and R.sub.11 are the same or different and represents hydrogen or a straight or branched C.sub.1-6 alkyl group,R is 1) ##STR2## processes for their preparation, pharmaceutical preparations containing them and the use of the compounds in the treatment psychiatric disorders.Type: GrantFiled: October 26, 1994Date of Patent: December 2, 1997Assignee: Astra AktiebolagInventors: Stefan Bengtsson, Sven Hellberg, Nina Mohell, Lian Zhang, Gerd Hallnemo, David Jackson, Bengt Ulff
-
Patent number: 5677444Abstract: A novel and simple method is proposed for the synthetic preparation of an N,N-disubstituted .beta.-ketothioamide compound represented by the general formulaR.sup.1 R.sup.2 N--CS--CH.sub.2 --CO--R.sup.3,in which R.sup.1 and R.sup.2 are each a monovalent hydrocarbon group or each a divalent hydrocarbon group jointly forming a cyclic structure together with the nitrogen atom and R.sup.3 is a hydrogen atom, a monovalent hydrocarbon group or a divalent hydrocarbon group forming a cyclic structure jointly with R.sup.1, R.sup.1 being a divalent hydrocarbon group and R.sup.2 being a monovalent hydrocarbon group. The method comprises:(a) mixing an N,N-disubstituted amide compound represented by the general formulaR.sup.1 R.sup.2 N--CO--R.sup.3,and a bis(trialkylsilyl)thioketene compound represented by the general formula(R.sub.3 Si).sub.2 C.dbd.C.dbd.Type: GrantFiled: September 15, 1995Date of Patent: October 14, 1997Assignee: Japan as represented by Director General of Agency of Industrial Science and TechnologyInventors: Tohru Tsuchiya, Isao Shibuya, Yoichi Taguchi, Akihiro Oishi, Kazumasa Honda
-
Patent number: 5654298Abstract: This invention concerns novel aminopyridinium compounds of the formula I wherein R.sup.1, R.sup.2, R.sup.3, R.sup.5 and R.sup.6 are selected from the following combinations: ##STR1## (a) one of R.sup.2 and R.sup.6 is a basic group selected from amino, alkylamino, dialkylamino of up to eight carbon atoms, pyrrolidino, piperidino and morpholino, or is alkyl, alkenyl, alkoxyalkyl, alkoxy, alkylthio, phenyl, phenylalkyl, cycloalkyl or cycloalkylalkyl; and the other of R.sup.2 and R.sup.6 is hydrogen, alkyl or one of the above defined basic groups;R.sup.1 is alkyl, alkenyl, cycloalkyl, phenyl, phenylalkyl, cycloalkylalkyl; and R.sup.3 and R.sup.5 are independently hydrogen, alkyl or alkenyl;(b) R.sup.2 is a basic group as defined above, R.sup.5 and R.sup.6 together form alkylene or, together with the appendant carbon atoms of the pyridine ring, complete a benzene ring; has any of the meanings defined in(a) above; and R.sup.3 is hydrogen, alkyl or alkenyl; and(c) R2 has any of the meanings defined above and R.sup.Type: GrantFiled: April 16, 1991Date of Patent: August 5, 1997Assignee: Imperial Chemical IndustriesInventors: Stuart Dennett Mills, Rodney Brian Hargreaves, Bernard Joseph McLoughlin
-
Patent number: 5646277Abstract: Cyclic lactams are prepared by reacting amino carbonitriles with water in liquid phase in a fixed bed reactor in the presence of heterogeneous catalysts which have no soluble constituents under the reaction conditions.Type: GrantFiled: May 16, 1996Date of Patent: July 8, 1997Assignee: BASF AktiengellschaftInventors: Eberhard Fuchs, Tom Witzel
-
Patent number: 5631275Abstract: This invention relates to substituted benzenesulfonylureas and -thioureas, processes for their preparation, and uses of the pharmaceutical products based on these compounds. The substituted benzenesulfonylureas and -thioureas are of the formula I ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 E, and y are as defined in the specification. The compounds of formula I have antiarrhythmic activity.Type: GrantFiled: June 5, 1995Date of Patent: May 20, 1997Assignee: Hoechst AktiengesellschaftInventors: Heinrich Englert, Dieter Mania, Jens Hartung, Heinz G ogelein, Joachim Kaiser, Uwe Gerlach
-
Patent number: 5622821Abstract: The invention provides lanthanide chelates capable of intense luminescence. The celates comprise a lanthanide chelator covalently joined to a coumarin-like or quinolone-like sensitizer. Exemplary sensitzers include 2- or 4-quinolones, 2- or 4-coumarins, or derivatives thereof e.g. carbostyril 124 (7-amino-4-methyl-2-quinolone), coumarin 120 (7-amino-4-methyl-2-coumarin), coumarin 124 (7-amino-4-(trifluoromethyl)-2-coumarin), aminomethyltrimethylpsoralen, etc.The chelates form high affinity complexes with lanthanides, such as terbium or europium, through chelator groups, such as DTPA. The chelates may be coupled to a wide variety of compounds to create specific labels, probes, diagnostic and/or therapeutic reagents, etc. The chelates find particular use in resonance energy transfer between chelate-lanthanide complexes and another luminescent agent, often a fluorescent non-metal based resonance energy acceptor.Type: GrantFiled: June 29, 1994Date of Patent: April 22, 1997Assignee: The Regents of the University of CaliforniaInventors: Paul R. Selvin, John Hearst
-
Patent number: 5608057Abstract: Proposed are an N-(.alpha.-acyloxyethyl) compound, e.g., (N-(.alpha.-acetoxyethyl)-2-pyrrolidone, which is a novel compound and can be converted into an industrially very important N-vinyl compound, e.g., N-vinyl-2-pyrrolidone, by a thermal decomposition reaction under relatively mild conditions as well as a method for the preparation of such an N-(.alpha.-acyloxyethyl) compound. The N-(.alpha.-acyloxyethyl) compound can be synthesized in a high yield by the addition reaction of an NH group-containing compound, e.g., 2-pyrrolidone, with a vinyl carboxylate, e.g., vinyl acetate, in the presence of an alkaline compound such as alkali metal hydroxides.Type: GrantFiled: August 23, 1995Date of Patent: March 4, 1997Assignee: Shin-Etsu Vinyl Acetate Co., Ltd.Inventors: Yoshihiro Honma, Shozo Tanaka, Mitsuyoshi Oshima, Soji Tanioka, Fumiaki Kawamoto
-
Patent number: 5599791Abstract: The present invention is directed to novel amide derivatives of antibiotic GE 2270 compounds and a process for preparing them. Said amide derivatives are antimicrobial agents active against gram positive bacteria as well as gram negative bacteria.Type: GrantFiled: July 1, 1993Date of Patent: February 4, 1997Assignee: Gruppo Lepetit SPAInventors: Paolo Tavecchia, Sergio Lociuro, Romeo Ciabatti, Enrico Selva
-
Patent number: 5594134Abstract: A process of synthesizing N-acyl auxiliary compounds is disclosed. A compound of the formula: ##STR1## is reacted with an anhydride in the presence of a lithium salt and an amine base to produce the N-acylated auxiliary.Type: GrantFiled: March 31, 1995Date of Patent: January 14, 1997Assignee: Merck & Co., Inc.Inventors: Guo-Jie Ho, David J. Mathre
-
Patent number: 5591846Abstract: New nonionic radiographic contrast agents having the formula ##STR1## wherein Y is a single bond, ##STR2## R.sub.1, R.sub.1 ' and R.sub.2 are the same or different and are hydrogen, alkyl or hydroxyalkyl.Hydroxyalkyl refers to such alkyl groups having 1 or more hydroxy groups. Preferred hydroxyalkyl groups include: ##STR3## R.sub.3 and R.sub.4 are the same or different and are hydrogen, methyl or --CH.sub.2 CH.sub.2 OH; R.sub.5 is hydrogen, alkyl, --CH.sub.2 CH.sub.2 OH, CH.sub.2 OH or OH and R.sub.6 is alkyl, --CH.sub.2 CH.sub.2 OH, CH.sub.2 OH, OH or hydrogen and may be the same or different than R.sub.5 and m is zero or one, with the proviso that no methylene or methine carbon atom of the heterocyclic ring is attached to both a nitrogen and an oxygen atom with the additional proviso that when Y is a single bond, m is not zero. These new contrast agents are water soluble and have desirable low osmolality and anticoagulant properties.Type: GrantFiled: October 27, 1993Date of Patent: January 7, 1997Assignee: Bracco International B.V.Inventors: Ramachandran S. Ranganathan, Thangavel Arunchalam, Edmund R. Marinelli, Radhakrishna K. Pillai
-
Patent number: 5565561Abstract: The invention relates to the natural substance cyclamenol of the formula ##STR1## a process for its preparation from microorganisms of the order of the Actinomycetales, in particular from the Streptomyces strain MHW 846, chemical derivatives thereof, and its use as a medicament, in particular for acute and chronic inflammatory disorders in human and veterinary medicine.Type: GrantFiled: April 27, 1995Date of Patent: October 15, 1996Assignee: Bayer AktiengesellschaftInventors: Hartwig M uller, Erwin Bischoff, Volker-Bernd Fiedler, Karlheinz Weber, Burkhard Fugmann, Bruno Rosen
-
Patent number: 5539104Abstract: This invention relates to a method of inhibiting platelet aggregation using 1,4-diazocine compounds which are mimics of the peptide sequence Arg--Gly--Asp.Type: GrantFiled: April 29, 1994Date of Patent: July 23, 1996Assignee: SmithKline Beecham Corp.Inventors: James F. Callahan, William F. Huffman
-
Patent number: 5510477Abstract: High quality acyl lactam imides are prepared by reacting an acyl lactam of the formula ##STR1## where 5 carbon atoms and an acylating acid of the formula R'CO.sub.2 H or by reacting a lactam, an anhydride of the formula (RCO).sub.2 O where R is 1 to 5 carbon atoms and an acylating acid, preferably in the presence of a base catalyst. The process affords acyl lactam imides in high yield and at lower reaction temperatures by providing for the removal of volatile carboxylic acid by-products under vacuum or by the use of a stripping gas. The acyl lactam imides are particularly suited for use as bleach activators in detergent compositions.Type: GrantFiled: March 1, 1994Date of Patent: April 23, 1996Assignee: The Procter & Gamble CompanyInventors: Alan D. Willey, Larry E. Miller
-
Patent number: 5508396Abstract: A process for preparing an N-alkyllactam, comprising the steps of:(a) reacting a lactam with an alkali metal alkoxide at 130.degree.-170.degree. C. and removing the alcohol formed by distillation;(b) reacting the product from step (a), if desired in a mixture with the product from step (e), with an alkyl halide in a solvent which is(i) an ethylene glycol dialkyl ether of the formula R--O--(CH.sub.2 --CH.sub.2 --O).sub.m R, where R in C.sub.1 -C.sub.Type: GrantFiled: April 13, 1995Date of Patent: April 16, 1996Assignee: Huels AktiengesellschaftInventor: Klaus-Dieter Steffen
-
Patent number: 5507843Abstract: The present invention is directed to the use of multiple cyclic nitrogen-containing alkoxylate compounds as additives in fuel compositions. The invention is also directed to the use of these multiple cyclic nitrogen-containing alkoxylate compounds for decreasing intake valve deposits, controlling octane requirement increases and reducing octane requirement. The invention is further directed to a class of multiple cyclic nitrogen-containing alkoxylate compounds.Type: GrantFiled: September 19, 1994Date of Patent: April 16, 1996Assignee: Shell Oil CompanyInventors: Jiang-Jen Lin, Pen-Chung Wang, Sarah L. Weaver
-
Patent number: 5502185Abstract: Cyclic lactams are prepared by reacting an aminocarboxylic acid compound of the formula IH.sub.2 N--(CH.sub.2).sub.m --COR.sup.1 Iwhere R.sup.1 is --OH, --O--C.sub.1 -C.sub.12 -alkyl or --NR.sup.2 R.sup.3 and R.sup.2 and R.sup.3, independently of one another, are each hydrogen, C.sub.1 -C.sub.12 -alkyl or C.sub.5 -C.sub.8 -cycloalkyl and m is an integer from 3 to 12, with water by a process in which the reaction is carried out in the liquid phase using a heterogeneous catalyst.Type: GrantFiled: December 19, 1994Date of Patent: March 26, 1996Assignee: BASF AktiengesellschaftInventors: Eberhard Fuchs, Tom Witzel
-
Patent number: 5493021Abstract: Lactams, in particular epsilon-caprolactam (a basic starting material for the production of nylon 6), are selectively prepared by cyclizing/reacting the corresponding aminonitriles with water, in the presence of a catalytically effective amount of a deactivation-resistant solid metal phosphate having the general formula (II):MH.sub.h (PO.sub.4).sub.n .multidot.(Imp).sub.pin which M is a divalent, trivalent, tetravalent or pentavalent element selected from among those of Groups 2a, 3b, 4b, 5b, 6b, 7b, 8, 2b, 3a, 4a and 5a of the Periodic Table, or mixture thereof, or M=0; Imp is a basic impregnating compound which comprises an alkali or alkaline earth metal, or mixture thereof, together with an electrical neutrality-ensuing counteranion therefor; n is 1, 2 or 3; h is 0, 1 or 2; and p is a number ranging from 0 to 1/3, corresponding to the molar ratio between the moiety Imp and the moiety MH.sub.h (PO.sub.4).sub.n.Type: GrantFiled: December 21, 1994Date of Patent: February 20, 1996Assignee: Rhone-Poulenc ChimieInventors: David Barratt, Laurent Gilbert
-
Patent number: 5440032Abstract: Disclosed is a method for purifying a lactam-containing organic solution which comprises processing an organic solution containing at least one lactam with an anion exchange resin to remove an anionic surface active substance contained in said organic solution, and then extracting with water to separate an objective component contained in the organic solution to an aqueous solution.Type: GrantFiled: June 10, 1991Date of Patent: August 8, 1995Assignee: Ube Industries, Ltd.Inventors: Kazuhiko Hirosawa, Yasuhiro Kurokawa, Tomohiko Yamamoto, Masaru Matsunishi, Yoshihiro Nawata
-
Patent number: 5438133Abstract: Cyclodextrin catenanes capable of forming inclusion complexes and a method of preparing them are disclosed. The catenanes comprise one or two per-2,6- di-O-alkyl-.beta.-cyclodextrin macrocycles wherein each per-2,6-di-O-alkyl-.beta.-cyclodextrin macrocycle is interpenetrated by another macrocycle. Such modified cyclodextrins may be used for the electrochemical and optical sensing of small organic molecules, especially small aromatic molecules.Type: GrantFiled: January 27, 1994Date of Patent: August 1, 1995Assignee: Eastman Kodak CompanyInventors: Christopher P. Moore, Trevor J. Wear, James F. Stoddart, Dominique Armspach
-
Patent number: 5426103Abstract: The invention relates to macrocyclic lactam derivatives of formula I ##STR1## wherin R is hydrogen or acyl; m is an integer from 4 to 9 inclusive; n is 1 or 2; p is zero, 1 or 2; X is --CONH-- or --NHCO--; Y is S, O or CH.sub.2 ; R.sub.1 is --COOH; or R.sub.1 is ##STR2## in which R.sub.2 is hydrogen, lower alkyl, aryl-lower alkyl, amino-lower alkyl, hydroxy-lower alkyl, acyloxy-lower alkyl, lower alkoxy-lower alkyl, mercapto-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, or carboxy-lower alkyl, R.sub.3 is hydrogen or lower alkyl, and q is zero or an integer from 1 to 5 inclusive; or R.sub.1 is ##STR3## in which R.sub.4 is hydrogen, lower alkyl, lower alkoxy, hydroxy or acyloxy, and r is 1 or 2; or R.sub.1 is ##STR4## in which s is 1 or 2; or R.sub.1 is ##STR5## in which R.sub.5 and R.sub.6 independently represent hydrogen, lower alkyl, C.sub.5 - or C.sub.Type: GrantFiled: June 15, 1993Date of Patent: June 20, 1995Assignee: Ciba-Geigy CorporationInventors: Lawrence J. MacPherson, James L. Stanton
-
Patent number: 5376529Abstract: This invention relates to novel methods for the release of nucleic acids from cells in complex biological samples or specimens to prepare and make available the nucleic acid material present for a hybridization assay or for extraction. Novel methods for hybridization of nucleic acids are also presented. In particular methods are described for isolating nucleic acid from a sample containing a complex biological mixture of nucleic acid and non-nucleic acids wherein the sample is combined with a hybridization medium comprising a lactam which promotes and enables nucleic acid pairing when complementary nucleic acid is introduced. The lactam is preferably about 5 to about 70% of the hybridization medium and is most preferably 2-pyrrolidone, N-ethyl-2-pyrrolidone, N-cyclohexyl-2-pyrrolidone, N-dodecyl-2-pyrrolidone, N-methyl-2-pyrrolidone, N-hydroxyethyl-2-pyrrolidone, N-methyl-2-piperidone, 2-.epsilon.-caprolactam, N-methyl-2-caprolactam, 2-piperidone or N-(4-hydroxybenzyl)pyrrolidone.Type: GrantFiled: December 13, 1991Date of Patent: December 27, 1994Assignee: MicroProbe CorporationInventors: Jeffrey Van Ness, Nicolaas M. J. Vermeulen
-
Patent number: 5352251Abstract: The present invention is directed to the use of cyclic amide alkoxylate compounds as additives in fuel compositions having a major amount of a mixture of hydrocarbons in the gasoline boiling range and a minor amount of one or more cyclic amide alkoxylate compounds of the formula: ##STR1## wherein x is from 2 to 20 and y is from 1 to 50. R.sub.1 and R.sub.2 are independently hydrogen, hydrocarbyl of 1 to 100 carbon atoms or substituted hydrocarbyl of 1 to 100 carbon atoms. R.sub.3 is hydrocarbyl of 1 to 100 carbon atoms or substituted hydrocarbyl of 1 to 100 carbon atoms and R.sub.4 is independently hydrocarbyl of 2 to 100 carbon atoms or substituted hydrocarbyl of 2 to 100 carbon atoms. R.sub.5 is hydrogen, hydrocarbyl of 1 to 100 carbon atoms, or substituted hydrocarbyl of 1 to 100 carbon atoms or acyl of 1 to 20 carbon atoms.Type: GrantFiled: March 30, 1993Date of Patent: October 4, 1994Assignee: Shell Oil CompanyInventors: Jiang-Jen Lin, James R. Macias, Earl J. Haury, Sarah L. Weaver, Charles L. Edwards, Pen-Chung Wang, Garo G. Vaporciyan
-
Patent number: 5338861Abstract: Substituted lactams of the formula ##STR1## can be prepared from lactam N-carboxylates or lactim O-carboxylates of the formulae ##STR2## by thermal or mixed thermal and catalysed CO.sub.2 elimination at 80.degree.-450.degree. C. Lactams substituted on the N atom by aliphatic groups such as those produced herein are useful as industrial aprotic solvents.Type: GrantFiled: July 24, 1992Date of Patent: August 16, 1994Assignee: Bayer AktiengesellschaftInventors: Artur Botta, Hans-Josef Buysch, Otto Immel, Lothar Puppe
-
Aza-bicyclo-terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension
Patent number: 5304552Abstract: Compounds characterized generally as piperidinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein B is selected from a piperidinyl group, an isoindolyl group and an azabicyclononyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from ##STR2## wherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: April 16, 1993Date of Patent: April 19, 1994Assignee: G.D. Searle & Co.Inventor: Gunnar J. Hanson -
Patent number: 5276165Abstract: A process for the preparation of N-substituted lactams of the formula I ##STR1## where Z is C.sub.2 - to C.sub.10 -alkylene, C.sub.7 - to C.sub.12 -aralkylene, phenylene or naphthylene, andR.sup.1 is C.sub.1 - to C.sub.20 -alkyl, C.sub.6 - to C.sub.10 -aryl or C.sub.7 - to C.sub.12 -aralkyl,by hydrogenating a compound of the formula II ##STR2## where W is C.sub.2 - to C.sub.10 -alkylene, C.sub.2 - to C.sub.10 -alkenylene, C.sub.7 - to C.sub.12 -aralkylene, phenylene or naphthylene, andX and Y together form an oxa or imido bridge of the formula ##STR3## or alternatively are identical or different and are hydroxyl, C.sub.1 - to C.sub.20 -alkoxy, C.sub.6 - to C.sub.10 -aryloxy or C.sub.7 - to C.sub.12 -aralkoxy, and, if X and Y are different, Y, in addition to the abovementioned meanings, may also be hydrogen,at superatmospheric pressure and at elevated temperature in the presence of a catalyst and in the presence of an amine, which comprises using a secondary and/or tertiary amine of the formula IIINH.sub.n R.Type: GrantFiled: November 25, 1992Date of Patent: January 4, 1994Assignee: BASF AktiengesellschaftInventors: Hans-Juergen Weyer, Rolf Fischer
-
Patent number: 5264479Abstract: The invention relates to lactam mixtures which give lactam melts having increased viscosity, to their production and to their use, preferably in the activated anionic polymerization of lactams (to cast polyamides). According to the invention, certain unsaturated aromatic vinyl compound/diene block copolymers (B) which dissolve in the lactam melt are added to the lactam (melt)s (A) in quantities of 1 to 15% by weight, a component (C) which is compatible with the diene block copolymers (B) and which dissolves completely or partly in the lactam melt optionally being added as an additional component. The block copolymers (B) used contain 10 to 85% by weight aromatic vinyl units and 15 to 90% by weight diene units. The block copolymers (B) may even be partly hydrogenated, epoxidized or grafted.The preferred lactam is .epsilon.-caprolactam.Lactam melts of increased viscosity are particularly suitable for taking up reinforcing materials and fillers (D) and for the production of filled cast polyamides.Type: GrantFiled: April 20, 1993Date of Patent: November 23, 1993Assignee: Bayer AktiengesellschaftInventors: Hans-Detlef Heinz, Friedrich Fahnler
-
Patent number: 5254682Abstract: Compounds of the formula: ##STR1## are disclosed. These compounds inhibit the angiotensinogen-cleaving action of the natural proteolytic enzyme, renin, and are useful in treating, preventing or managing renin-associated hypertension, hyperaldosteronism, congestive heart failure, and glaucoma.Type: GrantFiled: June 11, 1991Date of Patent: October 19, 1993Assignee: Merck & Co., Inc.Inventors: Daljit S. Dhanoa, Arthur A. Patchett, William J. Greenlee, William H. Parsons, Thomas A. Halgren, Ann E. Weber, Lihu Yang
-
Patent number: 5244888Abstract: Substituted 8-alkoxy-1,2,3,3a,8,8a-hexahydroindeno[1,2-c]pyrroles; 5-alkoxy-2,3,4,4a,9,9a-hexahydro-1-H-indeno[2,1-c]pyridines; and 9-alkoxy-2,3,3a,4,5,9a-hexahydro-1H-benz[e]isoindoles are selective 5-HT receptor agents and are thus useful in the treatment of anxiety, depression, and hypertension.Type: GrantFiled: July 9, 1991Date of Patent: September 14, 1993Assignee: Abbott LaboratoriesInventors: John F. DeBernardis, Michael D. Meyer, Kevin B. Sippy
-
Patent number: 5216149Abstract: A process of using fast pyrolysis in a carrier gas to convert a plastic waste feedstream having a mixed polymeric composition in a manner such that pyrolysis of a given polymer to its high value monomeric constituent occurs prior to pyrolysis of other plastic components therein comprising: selecting a first temperature program range to cause pyrolysis of said given polymer to its high value monomeric constituent prior to a temperature range that causes pyrolysis of other plastic components; selecting a catalyst and support for treating said feed streams with said catalyst to effect acid or base catalyzed reaction pathways to maximize yield or enhance separation of said high value monomeric constituent in said temperature program range; differentially heating said feed stream at a heat rate within the first temperature program range to provide differential pyrolysis for selective recovery of optimum quantities of the high value monomeric constituent prior to pyrolysis of other plastic components; separating thType: GrantFiled: June 7, 1991Date of Patent: June 1, 1993Assignee: Midwest Research InstituteInventors: Robert J. Evans, Helena L. Chum
-
Patent number: 5212163Abstract: Novel compounds of formula (I) and salts, solvates and hydrates thereof, processes for their preparation and their use in the treatment of conditions in which degradation of connective tissue and other proteinaceous components of the body occurs: ##STR1## in which, R is hydrogen, C.sub.1-6 alkyl or optionally substituted benzyl; R.sub.1 is hydrogen or C.sub.1-6 alkyl; R.sub.2 is C.sub.3-6 alkyl; R.sub.3 is hydrogen, alkyl, --CH.sub.2 --Z where Z is optionally substituted phenyl or heteroaryl, or R.sub.3 is a group ##STR2## where R.sub.7 is hydrogen, alkyl or --CH.sub.2 --Ph where Ph is optionally substituted phenyl and R.sub.8 is hydrogen or alkyl; and R.sub.4 is --CH.sub.2 --(CH.sub.2).sub.n OR.sub.5 or --CH.sub.2 --(CH.sub.2).sub.n OCOR.sub.6 or --CH(R.sub.9)COR.sub.10, where n is an integer from 1 to 6; R.sub.5, R.sub.6 and R.sub.9 are hydrogen or C.sub.1-6 alkyl; and R.sub.10 is hydroxy or --O--C.sub.1-6 alkyl or --NR.sub.5 R.sub.6 (where R.sub.5 and R.sub.Type: GrantFiled: September 9, 1991Date of Patent: May 18, 1993Assignee: Beecham Group p.l.c.Inventors: Robert W. Ward, Roger E. Markwell, David J. Hunter
-
Patent number: 5206362Abstract: Disclosed is a two-step method for the preparation of cyclic urea products which comprises: heating a diamine with urea in a mole ratio of about 1 at a temperature from about 120.degree. C. to 140.degree. C. until a mole of ammonia is liberated and slowly heating the intermediate with an alcohol or polyether solvent to a temperature from about 160.degree. C. to 200.degree. C. to produce the cyclic urea products.Type: GrantFiled: February 19, 1992Date of Patent: April 27, 1993Assignee: Texaco Chemical CompanyInventors: George P. Speranza, Donald H. Champion
-
Patent number: 5196415Abstract: This invention is in the field of clinical neurology and relates specifically to compounds, compositions and methods for treatment of patients with generalized epilepsy or partial (symptomatic) epilepsy using compounds of the formula: ##STR1## This invention also relates to compounds, compositions and methods of treatment for drug craving in patients addicted to cocaine.Type: GrantFiled: January 29, 1992Date of Patent: March 23, 1993Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: James A. Monn, Andrew Thurkauf, Shunichi Yamaguchi, Michael A. Rogawski, Kenner C. Rice, Mariena V. Mattson, Arthur E. Jacobson
-
Patent number: 5153316Abstract: The present invention relates to novel phenylimidazolone compounds of the formula ##STR1## wherein A is a bond or C.dbd.T;R is --H, Alk, halo-Alk, cyano-Alk, or phenyl;R.sup.1 is --H, Alk, halogen, halo-Alk, --CN; or when A is a bond, R and R.sup.1 may together form a saturated, partially saturated, or unsaturated three to seven member carbon ring, and the ring may be substituted at any position independently with one or more Alk, --O--Alk, --CN, halogen, --OH, or .dbd.O groups;T is O or S;U is --H;V is --OH, or U and V may together form a bond;W is halogen or --CN, and when W is halogen, R.sup.1 is --CN;X is --H or halogen;Y is --H, halogen, --CN, Alk, --CF.sub.3, or --OCF.sub.3 ;Z is --H, halogen, --OH, Alk, aryloxy, C.sub.1-6 acyl, --NH.sub.2, --NO.sub.2, --NR.sup.2 SO.sub.2 R.sup.2, --N(SO.sub.2 R.sup.2).sub.2, --NR.sup.2 COR.sup.Type: GrantFiled: June 4, 1991Date of Patent: October 6, 1992Inventors: Gary D. Crouse, Michael P. Lynch, Jeffery D. Webster, John P. Wright
-
Patent number: 5145842Abstract: Compositions having protein kinase C-modulatory, anti-inflammatory and other activities are disclosed. The compounds are derived from aromatic heterocyclic compounds of the indole, indene, benzofuran and benzothiophene class.Type: GrantFiled: July 30, 1990Date of Patent: September 8, 1992Assignee: Alder Research Center Limited PartnershipInventors: Paul E. Driedger, James Quick
-
Patent number: 5124444Abstract: This invention relates to novel methods for the extraction of nucleic acid. In particular methods are described for isolating nucleic acid from a sample containing a complex biological mixture of nucleic acid and non-nucleic acids wherein the sample is combined with an extraction solution comprising a lactam and then the nucleic acid material is isolated from the resulting combined solution. The resulting combined solution is mixed and becomes biphasic and the nucleic acid material is isolated from the aqueous phase by precipitation with ethanol. The lactam is preferably about 5 to about 70% of the extraction solution and is most preferably 2-pyrrolidone, N-ethyl-2-pyrrolidone, N-cyclohexyl-2-pyrrolidone, N-dodecyl-2-pyrrolidone, N-methyl-2-pyrrolidone, N-hydroxyethyl-2-pyrrolidone, N-methyl-2-piperidone, 2-.epsilon.-caprolactam, N-methyl-2-caprolactam, 2-piperidone or N-(4-hydroxybenzyl)pyrrolidone. Methods for selectively isolating DNA, ribosomal RNA and plasmid DNA are also disclosed.Type: GrantFiled: July 24, 1989Date of Patent: June 23, 1992Assignee: MicroProbe CorporationInventors: Jeffrey Van Ness, Nicolaas Vermuelen, B. Melina Cimler
-
Patent number: 5118805Abstract: Novel compositions of phosphoroustriscaprolactams, including tris(caprolactyl)phosphite which may be produced in accordance with the methods disclosed, finding particular utility as catalysts for esterification and other condensation reactions.Type: GrantFiled: April 22, 1991Date of Patent: June 2, 1992Assignee: Allied-Signal Inc.Inventors: Jeffrey H. Glans, Murali K. Akkapeddi
-
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
-
Patent number: 5106730Abstract: This invention relates to novel methods for the release of nucleic acids from cells in complex biological samples or specimens to prepare and make available the nucleic acid material present for a hybridization assay or for extraction. Novel methods for hybridization of nucleic acids are also presented. In particular methods are described for isolating nucleic acid from a sample containing a complex biological mixture of nucleic acid and non-nucleic acids wherein the sample is combined with a hybridization medium comprising a lactam which promotes and enables nucleic acid pairing when complementary nucleic acid is introduced. The lactam is preferably about 5 to about 70% of the hybridization medium and is most preferably 2-pyrrolidone, N-ethyl-2-pyrrolidone, N-cyclohexyl-2-pyrrolidone, N-dodecyl-2-pyrrolidone, N-methyl-2-pyrrolidone, N-hydroxyethyl-2-pyrrolidone, N-methyl-2-piperidone, 2-.epsilon.-caprolactam, N-methyl-2-caprolactam, 2-piperidone or N-(4-hydroxybenzyl)pyrrolidone.Type: GrantFiled: July 27, 1990Date of Patent: April 21, 1992Assignee: MicroProbe CorporationInventors: Jeffrey Van Ness, Nicolaas M. J. Vermeulen
-
Patent number: 5098916Abstract: Certain propanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are of the formula ##STR1## wherein each R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y and Z is independently selected from hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, phenalkyl, phenyl, alkoxy, phenoxy, phenalkoxy, alkoxyalkyl, halo, haloalkyl and hydroxyalkyl; wherein R.sup.3 and R.sup.4 may be taken together to form oxo;wherein each of R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13 and R.sup.14 is independently selected from hydrido, alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, cycloalkylalkyl, alkoxyalkyl, henalkyl and phenyl; wherein G within the nitrogen-containing cyclohetero moiety is selected from ##STR2## wherein R.sup.15 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, phenalkyl, alkoxyalkyl and hydroxyalkyl; wherein each of R.sup.16 and R.sup.Type: GrantFiled: March 29, 1990Date of Patent: March 24, 1992Assignee: G. D. Searle & Co.Inventors: Nancy M. Gray, Brian K. Cheng
-
Patent number: 5063208Abstract: A renin inhibiting compound having an aminodiol functional group is useful for treating hypertension, congestive heart failure and glaucoma and inhibits retroviral protease.Type: GrantFiled: June 29, 1990Date of Patent: November 5, 1991Assignee: Abbott LaboratoriesInventors: Saul H. Rosenberg, Kenneth P. Spina, Steven R. Crowley
-
Patent number: 5059687Abstract: A process for the condensation of imides and alcohols or amines to ester acyl lactams, ester amide acyl lactams or amide acyl lactams by reacting a polyol or polyamine in the liquid phase with an acyl lactam compound is disclosed.Type: GrantFiled: April 12, 1990Date of Patent: October 22, 1991Assignee: Stamicarbon B.V.Inventors: Christiaan Schroder, Albert A. Van Geenen, Josefina M. A. Schiffer
-
Patent number: 5047402Abstract: This invention provides a series of novel cyclic amides of formula I in which the group >Z--Y--X< is selected from >C.dbd.CH--N<, >N-CH.dbd.CH<, >C.dbd.N--N< and >N--N.dbd.C< and the other radicals have the meanings defined in the following specification. The compounds of formula I are leukotriene antagonists. The invention also provides pharmaceutically acceptable salts of the formula I compounds; pharmaceutical compositions containing the formula I compound, or their salts, for use in the treatment of, for example, allergic or inflammatory diseases, or endotoxic or traumatic shock conditions; and processs for the manufacture of the formula I compounds, as well as intermediates for use in such manufacture.Type: GrantFiled: April 12, 1989Date of Patent: September 10, 1991Assignee: ICI Americas Inc.Inventor: Victor G. Matassa
-
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
-
Patent number: 5028704Abstract: The present invention relates to compounds of the formula ##STR1## wherein R.sub.c is carboxy, esterified carboxy or amidated carboxy;R.sub.2 is hydrogen or lower alkyl or joins with R.sub.a and R.sub.b and the atoms therebetween to form a fused ring ##STR2## and either R.sub.a is methyl and R.sub.b is ##STR3## or R.sub.2 and R.sub.b and the atoms therebetween form a group wherein R.sub.3 and R.sub.4 are either both hydrogen, or together are propylene, butylene, or with the two atoms to which they are attached form a benzene ring. Methods of manufacture and use thereof in the production of angiotensin converting enzyme inhibitors are disclosed.Type: GrantFiled: February 8, 1990Date of Patent: July 2, 1991Assignee: Ciba-Geigy CorporationInventor: Stephen K. Boyer
-
Patent number: 5019572Abstract: Imidazole compounds including imidazoles and imidazolium salts, and their use as transglutaminase inhibitors are disclosed.Type: GrantFiled: February 7, 1990Date of Patent: May 28, 1991Assignee: Merck & Co., Inc.Inventors: David A. Claremon, John J. Baldwin, David C. Remy
-
Patent number: 5011941Abstract: The invention relates primarily to quaternized compounds having the formula ##STR1## wherein n and n' are each independently integers having a value of from 1 to 25; p is an integer having a value of from 1 to 4; Y and Y' are each independently H or CH.sub.3 ; R is linear alkyl, alkenyl, or amidoalkyl having from 8 to 22 carbon atoms and is optionally substituted with C.sub.1 to C.sub.4 alkyl; Z is linear alkylene having from 3 to 8 carbon atoms and is optionally substituted with lower alkyl and A.sup.- is an anion.Type: GrantFiled: September 14, 1990Date of Patent: April 30, 1991Assignee: GAF Chemicals CorporationInventors: Ratan K. Chaudhuri, David J. Tracy, Robert B. Login
-
Patent number: 5008104Abstract: The invention relates primarily to quaternized compounds having the formula ##STR1## wherein n and n' are each independently integers having a value of from 1 to 25; p is an integer having a value of from 1 to 4; Y and Y' are each independently H or CH.sub.3 ; R is linear alkyl, alkenyl, or amidoalkyl having from 8 to 22 carbon atoms and is optionally substituted with C.sub.1 to C.sub.4 alkyl; Z is linear alkylene having from 3 to 8 carbon atoms and is optionally substituted with lower alkyl and A.sup.- is an anion.Type: GrantFiled: June 22, 1989Date of Patent: April 16, 1991Assignee: GAF Chemicals CorporationInventors: Ratan K. Chaudhuri, David J. Tracy, Robert B. Login
-
Patent number: 5006651Abstract: The invention relates compounds of the formula ##STR1## wherein R.sup.1 -R.sup.5 and X have the significance given in the description, and their pharmaceutically acceptable salts. The compounds of formula I inhibit the enzyme collagenase and can be used in the form of medicaments for the control or prevention of degenerative joint diseases such as rheumatoid arthritis and osteoarthritis.Type: GrantFiled: September 22, 1989Date of Patent: April 9, 1991Assignee: Hoffman-La Roche Inc.Inventors: Michael J. Broadhurst, Balraj K. Handa, William H. Johnson, Geoffrey Lawton, Peter J. Machin
-
Patent number: 4943633Abstract: This invention relates to an improved process for the preparation of cyanoalkyl lactams by the reaction of an unsaturated nitrile with a lactam, said cyanoalkyl lactam of the formula ##STR1## wherein R is H, or methyl, R.sub.1 is H, methyl or ethyl and n is a number ranging from 2-11 and wherein each of the methylene groups may carry a lower alkyl substituent as shown. The improvement comprises: reacting said lactam with an alpha-beta unsaturated nitrile having from 3-6 carbon atoms in the presence of a catalytic amount of a diazabicycloalkene of the formula ##STR2## wherein R, R.sub.1 and n have the above meaning. Typically, acrylonitrile is reacted with .epsilon.-caprolactam in the presence of diazabicycloundecene.Type: GrantFiled: June 22, 1988Date of Patent: July 24, 1990Assignee: Air Products and Chemicals, Inc.Inventors: Richard V. C. Carr, Thomas A. Johnson