Patents Examined by Richard Raymond
  • Patent number: 4448976
    Abstract: Disclosed is a chiral, total synthesis of thienamycin from D-glucose which proceeds via intermediates I, II and III to known aldehyde IV which is known to be useful in the total synthesis of thienamycin (V): ##STR1## wherein: R is lower alkyl having 1-6 carbon atoms or bi-valent alkyl having 2-6 carbon atoms which joins the two sulfur atoms; R.sup.1 is lower alkyl or aralkyl, such as benzyl and the like; and R.sup.2 is hydrogen or a removable protecting group, such as triorganosilyl wherein the organo groups are independently selected from lower alkyl, phenyl and phenylloweralkyl.
    Type: Grant
    Filed: February 7, 1983
    Date of Patent: May 15, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Philippe L. Durette
  • Patent number: 4448722
    Abstract: Storage-stable aqueous compositions containing dissolved water-soluble novel acid addition salts of poly(N-substituted sulfonamido) phthalocyanines which are prepared by the interaction of a single acid or a mixture of acids and poly(N-substituted sulfonamido) phthalocyanines, are useful for direct dyeing, particularly the dyeing of cellulose.
    Type: Grant
    Filed: September 27, 1982
    Date of Patent: May 15, 1984
    Assignee: The Hilton-Davis Chemical Co.
    Inventor: Nathan N. Crounse
  • Patent number: 4447624
    Abstract: Process for the preparation of thiophenes having the structure ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 can be various substituents. The compounds can be converted to the corresponding 2-amino compounds from which azo dyes can be prepared.
    Type: Grant
    Filed: June 21, 1982
    Date of Patent: May 8, 1984
    Assignee: Eastman Kodak Company
    Inventors: James J. Krutak, Robert J. Maleski
  • Patent number: 4447622
    Abstract: The laevo and dextro forms of dl-3,4-trans-2,2-disubstituted-3,4-diarylchromans and similar derivatives thereof have substantially double the post-coital anti-fertility activity of the known racemic compound. The resolution of such known compound into the l- and d-isomeric forms may be carried out using di-p-toluoyl-l-tartaric acid monohydrate or di-p-toluoyl-d-tartaric acid.
    Type: Grant
    Filed: September 22, 1981
    Date of Patent: May 8, 1984
    Assignee: Council of Scientific and Industrial Research Rafi Marg
    Inventors: Mohammad Salman, Suprabhat Ray, Ved P. Kamboj, Nitya Anand
  • Patent number: 4447442
    Abstract: This disclosure describes novel 3-substituted amino-1-phenyl-2-pyrazolines and 3-substituted amino-1-mono and disubstituted phenyl-2-pyrazolines and their C.sub.4 and C.sub.5 analogs, useful for meliorating the inflammation and/or the progressive joint deterioration characteristic of arthritic disease, preventing the onset of asthmatic symptoms and allergic diseases, or as analgesic, antibacterial or antifungal agents.
    Type: Grant
    Filed: August 9, 1982
    Date of Patent: May 8, 1984
    Assignee: American Cyanamid Company
    Inventors: John P. Dusza, Joseph P. Joseph, Seymour Berstein
  • Patent number: 4447635
    Abstract: Novel N-substituted imido-dicarboxylic acid diaryl ester compounds of the general formula ##STR1## in which R.sup.1 represents an optionally substituted aliphatic, cycloaliphatic, araliphatic, aromatic, heterocyclic radical andR.sup.2 and R.sup.3 can be identical or different and represent an optionally substituted aryl radical, and a process for their preparation characterized in that a carbamic acid aryl ester of the general formulaR.sup.1 --NH--CO--OR.sup.2 (II)in which R.sup.1 and R.sup.2 have the abovementioned meanings, is reacted with a carbonic acid aryl ester halide of the general formulaX--CO--OR.sup.3 (III)in whichR.sup.3 has the abovementioned meaning andX represents a halogen atom, optionally in the presence of a diluent, optionally at a temperature between 100.degree. and 300.degree. C.The new compounds (I) can be used as intermediate products for the preparation of known herbicidal active compounds from the 1,3,5-triazine,2,4-(1H,3H)-dione series.
    Type: Grant
    Filed: June 30, 1982
    Date of Patent: May 8, 1984
    Assignee: Bayer Aktiengesellschaft
    Inventors: Karlfried Dickore, Engelbert Kuhle
  • Patent number: 4447431
    Abstract: The invention relates to novel tri-substituted imidazole derivatives, especially compounds of the general formula I ##STR1## in which R.sub.1 and R.sub.2 represent, independently of each other, carbocyclic aryl and heteroaryl,A represents a divalent hydrocarbon radical, andR.sub.3 represents carboxy, esterified carboxy or amidated carboxy,their isomers and their salts, especially pharmaceutically acceptable salts, with the proviso that, if A represents methylene or ethylidene and R.sub.3 represents ethoxycarbonyl, at least one of the radicals R.sub.1 and R.sub.2 is different from phenyl, and the further proviso that, if A represents ethylidene and R.sub.3 represents carboxy, at least one of the radicals R.sub.1 and R.sub.2 is different from phenyl, p-methoxyphenyl and p-chlorophenyl, processes for their manufacture, pharmaceutical preparations containing such compounds, and their use, for example as active substances in medicaments.
    Type: Grant
    Filed: September 28, 1982
    Date of Patent: May 8, 1984
    Assignee: Ciba-Geigy Corporation
    Inventor: Alfred Sallmann
  • Patent number: 4446319
    Abstract: Novel aminocyclitols, namely the compounds of the formula ##STR1## wherein X is hydroxyl group, a halogen or an acyloxy group; Y is hydrogen or a halogen; and OR.sup.1 is an optionally protected hydroxyl group; and their production.These aminocyclitols are important intermediates for preparing valiolamine having .alpha.-glucosidase inhibitory activity.
    Type: Grant
    Filed: April 26, 1982
    Date of Patent: May 1, 1984
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Satoshi Horii, Hiroshi Fukase
  • Patent number: 4443599
    Abstract: There is provided a process for the preparation of an enantiomer of a compound of formula (I) which process comprises separation thereof from a mixture of diastereoisomers of a compound of the formula (I): ##STR1## wherein R is acetyl, .alpha.-hydroxyethyl or a protected derivative thereof, and R.sup.1 and R.sup.2 are substituted or unsubstituted hydrocarbon groups, or are joined so as to form a carbocyclic or heterocyclic ring; at least one of R.sup.1 and R.sup.2 containing a chiral center, such that the enantiomer can be separated thereby; and R.sup.3 and R.sup.4 are independently hydrogen or an organic group bonded via a carbon atom to the tetrahydro-oxazine ring, or R.sup.3 and R.sup.4 are joined so as to form together with the carbon atom to which they are attached an optionally substituted C.sub.3-7 cycloalkyl or optionally substituted heterocyclyl ring.The enantiomer is of use in the preparation of optically active carbapenem antibiotics.
    Type: Grant
    Filed: May 12, 1982
    Date of Patent: April 17, 1984
    Assignee: Beecham Group p.l.c.
    Inventor: Terence C. Smale
  • Patent number: 4443447
    Abstract: Antimicrobial compounds of the following formula are disclosed: ##STR1## wherein X is selected from the group consisting of --O--, --CH.sub.2 and ##STR2## m is 0 or 1; R.sub.1 is selected from the group consisting of hydrogen, nitro, amino, lower alkyl, lower alkanamido, lower N,N-dialkylamino, formamido, hydroxy, lower alkoxy, halogen, lower haloalkanamido and pyrryl; n is 1 or 2; and R.sub.2 is selected from the group consisting of hydrogen, methyl, fluoro, chloro and nitro. Acyl chlorides, esters, alkylaminoalkyl ester salts, amides and pharmaceutically acceptable carboxylate salts are also disclosed. Pharmaceutical compositions containing these compounds, methods of using these compound and synthetic intermediates are also disclosed.
    Type: Grant
    Filed: October 25, 1982
    Date of Patent: April 17, 1984
    Assignee: Riker Laboratories, Inc.
    Inventors: John F. Gerster, Richard M. Stern
  • Patent number: 4443598
    Abstract: Intermediates for preparing an antibacterial 1-dethia-1-oxacephalosporins which are represented by the following formula: ##STR1## wherein R is a monovalent group (minus the carbonyl) from an acyl derived from a carboxylic or carbonic acid;Y.sup.1 is a divalent group of the following formula: ##STR2## wherein COB is carboxy or protected carboxy;X is hydrogen or a nucleophilic group; andZ is a leaving groupare prepared from a compound of the following formula: ##STR3## wherein R and Y.sup.1 are as defined above by the action of an acid. The new compounds of this invention shown by the following formula: ##STR4## wherein A is amino or substituted amino;E is hydrogen or methoxy; andY is a divalent group of the following formula: ##STR5## in which COB, X, and Z are as defined above are convertible into other compounds of the same formula by applying conventional methods in .beta.-lactam chemistry.
    Type: Grant
    Filed: May 4, 1982
    Date of Patent: April 17, 1984
    Assignee: Shionogi & Co., Ltd.
    Inventors: Mitsuru Yoshioka, Uyeo Shoichiro, Yoshio Hamashima, Ikuo Kikkawa, Teruji Tsuji, Wataru Nagata
  • Patent number: 4443609
    Abstract: This invention relates to tetrahydrothiazole phosphonic acids or phosphonates and to the preparation thereof by reacting dihydrothiazoles with phosphorous acid or esters thereof.
    Type: Grant
    Filed: May 19, 1980
    Date of Patent: April 17, 1984
    Assignee: Petrolite Corporation
    Inventors: Bernardus A. Oude Alink, Derek Redmore
  • Patent number: 4442117
    Abstract: There are described novel homoserine derivatives of the formula (I) ##STR1## which possess valuable microbicidal properties. In the formula: Ar is substituted phenyl or naphthyl; R.sub.1 is C.sub.2 -C.sub.6 alkyl optionally interrupted by oxygen or sulfur, 2-furyl, 2-tetrahydrofuryl, 1H-1,2,4-triazolylmethyl, 1-imidazolylmethyl, 1-pyrazolylmethyl, C.sub.2 -C.sub.4 alkenyl or cyclopropyl, each of which is optionally substituted by halogen; R.sub.2 is hydrogen or methyl; R.sub.3 is hydrogen or C.sub.1 -C.sub.4 alkyl; and B is halogen or an ester, thioester, sulfonic acid ester or sulfonic acid amide group. Additionally, where B is halogen, R.sub.1 may be halomethyl. The novel derivatives can be used for combating microorganisms harmful to plants, particularly for combating phytopathogenic fungi, and they have for practical requirements a very favorable curative and protective action for protecting cultivating plants, without the plants being impaired as a result of undesirable secondary effects.
    Type: Grant
    Filed: October 23, 1980
    Date of Patent: April 10, 1984
    Assignee: Ciba-Geigy Corporation
    Inventors: Walter Kunz, Wolfgang Eckhardt, Adolf Hubele, Peter Riebli
  • Patent number: 4440781
    Abstract: A method for producing a psychotropic response, especially for alleviating the symptoms of alcohol withdrawal, comprises administering to a human or animal subject in need thereof a psychotropically effective non-toxic amount of an oxyoctadecanoate. A composition for use in the present method is provided.
    Type: Grant
    Filed: June 11, 1982
    Date of Patent: April 3, 1984
    Assignee: The Vinoxen Company, Inc.
    Inventors: Herman P. Benecke, Bob E. Sherwood
  • Patent number: 4440938
    Abstract: The invention relates to a process for the preparation of ranitidine of formula (I) ##STR1## which comprises reacting a thiol of formula (II) ##STR2## with an alkylating agent of formula (III) ##STR3## The ethyleneimino derivative of formula (III) is a novel compound.
    Type: Grant
    Filed: September 30, 1982
    Date of Patent: April 3, 1984
    Assignee: Glaxo Group Limited
    Inventor: John Bradshaw
  • Patent number: 4440755
    Abstract: A composition for promoting the healing of a wound of an animal consisting of lime, alum and salt in selected proportions.
    Type: Grant
    Filed: September 6, 1983
    Date of Patent: April 3, 1984
    Inventor: Edgar C. Weathers
  • Patent number: 4440943
    Abstract: 3,7-Substituted phenoxiodinin-5-ium compounds are effective against a variety of aerobic and anaerobic bacteria as well as fungi. The compounds of this invention may be prepared by the direct iodination of a suitably substituted diphenyl ether with iodosyl sulfate in concentrated sulfuric acid. The resulting bisulfate anion may be exchanged with a desired anion by standard metathetic processes.
    Type: Grant
    Filed: March 15, 1982
    Date of Patent: April 3, 1984
    Assignee: The Dow Chemical Company
    Inventor: Edward E. Flagg
  • Patent number: 4439428
    Abstract: This invention relates to substituted phosphonic acid derivatives, and to their use as herbicides.
    Type: Grant
    Filed: October 14, 1982
    Date of Patent: March 27, 1984
    Assignee: Imperial Chemical Industries PLC
    Inventor: John M. Cox
  • Patent number: 4439442
    Abstract: The object of the invention is a new naftidrofuryl salt, naftidrofuryl citrate, which is therapeutically useful because it promotes metabolism and circulatory properties and because of its vaso-active properties in the treatment of arthritis of the limbs, Reynaud's Syndrome and cerebral circulatory insufficiency.
    Type: Grant
    Filed: May 14, 1982
    Date of Patent: March 27, 1984
    Assignee: SANOFI
    Inventors: Jacques A. Chick, Alain Heymes, Carlo Blasioli
  • Patent number: 4439444
    Abstract: Amidobenzamides acting as histamine H.sub.2 receptors blocking agents, of formula ##STR1## wherein A is CO or SO.sub.2 and B is alkyl, phenyl, pyridyl, pyridyl-1-oxyde, pyrazinyl or thienyl; their salts; process for their preparation by reaching 2-(5-dimethyl-aminomethylfuran-2-ylmethylthio)ethylamine with a derivative of formula ##STR2## and optional salification and pharmaceutical compositions containing same.
    Type: Grant
    Filed: July 7, 1982
    Date of Patent: March 27, 1984
    Assignee: Sanofi
    Inventors: Dino Nisato, Sergio Boveri, Alberto Bianchetti, Romeo Roncucci, Paolo Carminati