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: 5721361
    Abstract: 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: Grant
    Filed: June 11, 1996
    Date of Patent: February 24, 1998
    Assignee: The Monsanto Company
    Inventors: Patrick J. Lennon, Susan L. Henke, Karl W. Aston
  • Patent number: 5693630
    Abstract: 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: Grant
    Filed: October 26, 1994
    Date of Patent: December 2, 1997
    Assignee: Astra Aktiebolag
    Inventors: Stefan Bengtsson, Sven Hellberg, Nina Mohell, Lian Zhang, Gerd Hallnemo, David Jackson, Bengt Ulff
  • Patent number: 5677444
    Abstract: 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: Grant
    Filed: September 15, 1995
    Date of Patent: October 14, 1997
    Assignee: Japan as represented by Director General of Agency of Industrial Science and Technology
    Inventors: Tohru Tsuchiya, Isao Shibuya, Yoichi Taguchi, Akihiro Oishi, Kazumasa Honda
  • Patent number: 5654298
    Abstract: 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: Grant
    Filed: April 16, 1991
    Date of Patent: August 5, 1997
    Assignee: Imperial Chemical Industries
    Inventors: Stuart Dennett Mills, Rodney Brian Hargreaves, Bernard Joseph McLoughlin
  • Patent number: 5646277
    Abstract: 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: Grant
    Filed: May 16, 1996
    Date of Patent: July 8, 1997
    Assignee: BASF Aktiengellschaft
    Inventors: Eberhard Fuchs, Tom Witzel
  • Patent number: 5631275
    Abstract: 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: Grant
    Filed: June 5, 1995
    Date of Patent: May 20, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinrich Englert, Dieter Mania, Jens Hartung, Heinz G ogelein, Joachim Kaiser, Uwe Gerlach
  • Patent number: 5622821
    Abstract: 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: Grant
    Filed: June 29, 1994
    Date of Patent: April 22, 1997
    Assignee: The Regents of the University of California
    Inventors: Paul R. Selvin, John Hearst
  • Patent number: 5608057
    Abstract: 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: Grant
    Filed: August 23, 1995
    Date of Patent: March 4, 1997
    Assignee: Shin-Etsu Vinyl Acetate Co., Ltd.
    Inventors: Yoshihiro Honma, Shozo Tanaka, Mitsuyoshi Oshima, Soji Tanioka, Fumiaki Kawamoto
  • Patent number: 5599791
    Abstract: 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: Grant
    Filed: July 1, 1993
    Date of Patent: February 4, 1997
    Assignee: Gruppo Lepetit SPA
    Inventors: Paolo Tavecchia, Sergio Lociuro, Romeo Ciabatti, Enrico Selva
  • Patent number: 5594134
    Abstract: 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: Grant
    Filed: March 31, 1995
    Date of Patent: January 14, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Guo-Jie Ho, David J. Mathre
  • Patent number: 5591846
    Abstract: 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: Grant
    Filed: October 27, 1993
    Date of Patent: January 7, 1997
    Assignee: Bracco International B.V.
    Inventors: Ramachandran S. Ranganathan, Thangavel Arunchalam, Edmund R. Marinelli, Radhakrishna K. Pillai
  • Patent number: 5565561
    Abstract: 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: Grant
    Filed: April 27, 1995
    Date of Patent: October 15, 1996
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hartwig M uller, Erwin Bischoff, Volker-Bernd Fiedler, Karlheinz Weber, Burkhard Fugmann, Bruno Rosen
  • Patent number: 5539104
    Abstract: 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: Grant
    Filed: April 29, 1994
    Date of Patent: July 23, 1996
    Assignee: SmithKline Beecham Corp.
    Inventors: James F. Callahan, William F. Huffman
  • Patent number: 5510477
    Abstract: 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: Grant
    Filed: March 1, 1994
    Date of Patent: April 23, 1996
    Assignee: The Procter & Gamble Company
    Inventors: Alan D. Willey, Larry E. Miller
  • Patent number: 5508396
    Abstract: 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: Grant
    Filed: April 13, 1995
    Date of Patent: April 16, 1996
    Assignee: Huels Aktiengesellschaft
    Inventor: Klaus-Dieter Steffen
  • Patent number: 5507843
    Abstract: 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: Grant
    Filed: September 19, 1994
    Date of Patent: April 16, 1996
    Assignee: Shell Oil Company
    Inventors: Jiang-Jen Lin, Pen-Chung Wang, Sarah L. Weaver
  • Patent number: 5502185
    Abstract: 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: Grant
    Filed: December 19, 1994
    Date of Patent: March 26, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Eberhard Fuchs, Tom Witzel
  • Patent number: 5493021
    Abstract: 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: Grant
    Filed: December 21, 1994
    Date of Patent: February 20, 1996
    Assignee: Rhone-Poulenc Chimie
    Inventors: David Barratt, Laurent Gilbert
  • Patent number: 5440032
    Abstract: 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: Grant
    Filed: June 10, 1991
    Date of Patent: August 8, 1995
    Assignee: Ube Industries, Ltd.
    Inventors: Kazuhiko Hirosawa, Yasuhiro Kurokawa, Tomohiko Yamamoto, Masaru Matsunishi, Yoshihiro Nawata
  • Patent number: 5438133
    Abstract: 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: Grant
    Filed: January 27, 1994
    Date of Patent: August 1, 1995
    Assignee: Eastman Kodak Company
    Inventors: Christopher P. Moore, Trevor J. Wear, James F. Stoddart, Dominique Armspach
  • Patent number: 5426103
    Abstract: 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: Grant
    Filed: June 15, 1993
    Date of Patent: June 20, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Lawrence J. MacPherson, James L. Stanton
  • Patent number: 5376529
    Abstract: 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: Grant
    Filed: December 13, 1991
    Date of Patent: December 27, 1994
    Assignee: MicroProbe Corporation
    Inventors: Jeffrey Van Ness, Nicolaas M. J. Vermeulen
  • Patent number: 5352251
    Abstract: 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: Grant
    Filed: March 30, 1993
    Date of Patent: October 4, 1994
    Assignee: Shell Oil Company
    Inventors: Jiang-Jen Lin, James R. Macias, Earl J. Haury, Sarah L. Weaver, Charles L. Edwards, Pen-Chung Wang, Garo G. Vaporciyan
  • Patent number: 5338861
    Abstract: 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: Grant
    Filed: July 24, 1992
    Date of Patent: August 16, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Artur Botta, Hans-Josef Buysch, Otto Immel, Lothar Puppe
  • Patent number: 5304552
    Abstract: 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: Grant
    Filed: April 16, 1993
    Date of Patent: April 19, 1994
    Assignee: G.D. Searle & Co.
    Inventor: Gunnar J. Hanson
  • Patent number: 5276165
    Abstract: 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: Grant
    Filed: November 25, 1992
    Date of Patent: January 4, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Hans-Juergen Weyer, Rolf Fischer
  • Patent number: 5264479
    Abstract: 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: Grant
    Filed: April 20, 1993
    Date of Patent: November 23, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans-Detlef Heinz, Friedrich Fahnler
  • Patent number: 5254682
    Abstract: 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: Grant
    Filed: June 11, 1991
    Date of Patent: October 19, 1993
    Assignee: 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: 5244888
    Abstract: 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: Grant
    Filed: July 9, 1991
    Date of Patent: September 14, 1993
    Assignee: Abbott Laboratories
    Inventors: John F. DeBernardis, Michael D. Meyer, Kevin B. Sippy
  • Patent number: 5216149
    Abstract: 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 th
    Type: Grant
    Filed: June 7, 1991
    Date of Patent: June 1, 1993
    Assignee: Midwest Research Institute
    Inventors: Robert J. Evans, Helena L. Chum
  • Patent number: 5212163
    Abstract: 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: Grant
    Filed: September 9, 1991
    Date of Patent: May 18, 1993
    Assignee: Beecham Group p.l.c.
    Inventors: Robert W. Ward, Roger E. Markwell, David J. Hunter
  • Patent number: 5206362
    Abstract: 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: Grant
    Filed: February 19, 1992
    Date of Patent: April 27, 1993
    Assignee: Texaco Chemical Company
    Inventors: George P. Speranza, Donald H. Champion
  • Patent number: 5196415
    Abstract: 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: Grant
    Filed: January 29, 1992
    Date of Patent: March 23, 1993
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: James A. Monn, Andrew Thurkauf, Shunichi Yamaguchi, Michael A. Rogawski, Kenner C. Rice, Mariena V. Mattson, Arthur E. Jacobson
  • Patent number: 5153316
    Abstract: 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: Grant
    Filed: June 4, 1991
    Date of Patent: October 6, 1992
    Inventors: Gary D. Crouse, Michael P. Lynch, Jeffery D. Webster, John P. Wright
  • Patent number: 5145842
    Abstract: 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: Grant
    Filed: July 30, 1990
    Date of Patent: September 8, 1992
    Assignee: Alder Research Center Limited Partnership
    Inventors: Paul E. Driedger, James Quick
  • Patent number: 5124444
    Abstract: 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: Grant
    Filed: July 24, 1989
    Date of Patent: June 23, 1992
    Assignee: MicroProbe Corporation
    Inventors: Jeffrey Van Ness, Nicolaas Vermuelen, B. Melina Cimler
  • Patent number: 5118805
    Abstract: 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: Grant
    Filed: April 22, 1991
    Date of Patent: June 2, 1992
    Assignee: Allied-Signal Inc.
    Inventors: Jeffrey H. Glans, Murali K. Akkapeddi
  • Patent number: 5110585
    Abstract: 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: Grant
    Filed: March 1, 1989
    Date of Patent: May 5, 1992
    Assignee: ISP Investments Inc.
    Inventors: Ratan K. Chaudhuri, David J. Tracy, Robert B. Login, Michael W. Helioff
  • Patent number: 5106730
    Abstract: 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: Grant
    Filed: July 27, 1990
    Date of Patent: April 21, 1992
    Assignee: MicroProbe Corporation
    Inventors: Jeffrey Van Ness, Nicolaas M. J. Vermeulen
  • Patent number: 5098916
    Abstract: 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: Grant
    Filed: March 29, 1990
    Date of Patent: March 24, 1992
    Assignee: G. D. Searle & Co.
    Inventors: Nancy M. Gray, Brian K. Cheng
  • Patent number: 5063208
    Abstract: A renin inhibiting compound having an aminodiol functional group is useful for treating hypertension, congestive heart failure and glaucoma and inhibits retroviral protease.
    Type: Grant
    Filed: June 29, 1990
    Date of Patent: November 5, 1991
    Assignee: Abbott Laboratories
    Inventors: Saul H. Rosenberg, Kenneth P. Spina, Steven R. Crowley
  • Patent number: 5059687
    Abstract: 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: Grant
    Filed: April 12, 1990
    Date of Patent: October 22, 1991
    Assignee: Stamicarbon B.V.
    Inventors: Christiaan Schroder, Albert A. Van Geenen, Josefina M. A. Schiffer
  • Patent number: 5047402
    Abstract: 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: Grant
    Filed: April 12, 1989
    Date of Patent: September 10, 1991
    Assignee: ICI Americas Inc.
    Inventor: Victor G. Matassa
  • Patent number: 5041545
    Abstract: 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: Grant
    Filed: April 6, 1989
    Date of Patent: August 20, 1991
    Assignee: Atochem North America, Inc.
    Inventor: Terry N. Myers
  • Patent number: 5028704
    Abstract: 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: Grant
    Filed: February 8, 1990
    Date of Patent: July 2, 1991
    Assignee: Ciba-Geigy Corporation
    Inventor: Stephen K. Boyer
  • Patent number: 5019572
    Abstract: Imidazole compounds including imidazoles and imidazolium salts, and their use as transglutaminase inhibitors are disclosed.
    Type: Grant
    Filed: February 7, 1990
    Date of Patent: May 28, 1991
    Assignee: Merck & Co., Inc.
    Inventors: David A. Claremon, John J. Baldwin, David C. Remy
  • Patent number: 5011941
    Abstract: 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: Grant
    Filed: September 14, 1990
    Date of Patent: April 30, 1991
    Assignee: GAF Chemicals Corporation
    Inventors: Ratan K. Chaudhuri, David J. Tracy, Robert B. Login
  • Patent number: 5008104
    Abstract: 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: Grant
    Filed: June 22, 1989
    Date of Patent: April 16, 1991
    Assignee: GAF Chemicals Corporation
    Inventors: Ratan K. Chaudhuri, David J. Tracy, Robert B. Login
  • Patent number: 5006651
    Abstract: 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: Grant
    Filed: September 22, 1989
    Date of Patent: April 9, 1991
    Assignee: Hoffman-La Roche Inc.
    Inventors: Michael J. Broadhurst, Balraj K. Handa, William H. Johnson, Geoffrey Lawton, Peter J. Machin
  • Patent number: 4943633
    Abstract: 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: Grant
    Filed: June 22, 1988
    Date of Patent: July 24, 1990
    Assignee: Air Products and Chemicals, Inc.
    Inventors: Richard V. C. Carr, Thomas A. Johnson