Chalcogen Bonded Directly To A Ring Carbon Of The Six-membered Hetero Ring Patents (Class 514/335)
  • Patent number: 4863936
    Abstract: Various substituted aminoalkylamino-2-pyridine derivatives are disclosed which are useful as histamine H.sub.1 -antagonists.
    Type: Grant
    Filed: October 21, 1986
    Date of Patent: September 5, 1989
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: George S. Sach
  • Patent number: 4772612
    Abstract: Novel circulation active dihydropyridines of the formula ##STR1## in which X is CO, SO.sub.2 or CONH,R.sup.4 is H, OH, alkyl, halogen, acyloxy, alkoxyalkoxy, aralkyloxy, or together with R.sup.5 forms a heterocyclic ring, andthe other radicals are conventional in the dihydropyridine art,and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: June 3, 1986
    Date of Patent: September 20, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Siegfried Goldmann, Jurgen Stoltefuss, Gerhard Franckowiak, Rainer Gross, Matthias Schramm, Gunter Thomas
  • Patent number: 4772615
    Abstract: Analogs of nipecotic acid are the novel compounds of the present invention. The analogs are GABA uptake inhibitors for use to treat epilepsy and, thus, the invention is also pharmaceutical compositions and methods of use therefor.
    Type: Grant
    Filed: October 14, 1987
    Date of Patent: September 20, 1988
    Assignee: Warner-Lambert Company
    Inventor: Michael R. Pavia
  • Patent number: 4766135
    Abstract: Novel fungicidal pyridyl cyclopropane carboxamides having the general structural formula ##STR1## wherein R is selected from the group consisting of haloalkyl, preferably C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.8 alkyl, aryl, substituted aryl, and arylalkyl wherein the preferred aryl is phenyl, the alkyl is C.sub.1 -C.sub.3 alkyl and the preferred substitutions are Cl, Br, F and nitro, alkanoyl, preferably C.sub.1 -C.sub.4 alkanoyl, ##STR2## wherein R.sub.3 and R.sub.4 can be alkyl, alkanoyl, alkoxycarbanoyl, benzyl pyridyl and substituted pyridyl, R.sub.1 is C.sub.1 -C.sub.3 alkoxy or C.sub.1 -C.sub.3 haloalkoxy, preferably methoxy or halomethoxy and halogen wherein the halogen is chlorine, bromine or fluorine, R.sub.2 is hydrogen or methyl, and fungicidally acceptable organic and inorganic salts thereof which are highly effective fungicides for use both as preventive and curative fungicides are disclosed herein. These compounds provide excellent control of fungal growth.
    Type: Grant
    Filed: April 15, 1987
    Date of Patent: August 23, 1988
    Assignee: Stauffer Chemical Co.
    Inventors: Don R. Baker, Keith H. Brownell
  • Patent number: 4766132
    Abstract: Compounds of formula: ##STR1## and stereoisomers thereof, wherein R.sup.1 is unsubstituted or substituted aryl or heteroaryl; R.sup.2 is H, alkyl, alkenyl or alkynyl; X is O, NH, or S; R.sup.3 being alkyl, alkenyl, alkynyl or COR.sup.4 where R.sup.4 has an R.sup.3 value, when X is O; R.sup.3 being --CO-- alkyl when X is NH; and R.sup.3 being alkyl, alkenyl or CSNR.sup.5 R.sup.6 where R.sup.5 and R.sup.6, which may be the same or different, are H, alkyl, alkenyl or, together with the adjacent N atom, constitute a ring, when X is S; or XR.sup.3 together represent --CN; and salts and metal complexes thereof, have fungicidal and plant growth regulating activity.
    Type: Grant
    Filed: January 29, 1986
    Date of Patent: August 23, 1988
    Assignee: Imperial Chemical Industries PLC
    Inventor: Ian T. Kay
  • Patent number: 4764519
    Abstract: The disclosure relates to a class of 2-(pyridylalkylamino)-3-hydroxypyridines which are active as histamine H.sub.1 -antagonists.
    Type: Grant
    Filed: May 1, 1987
    Date of Patent: August 16, 1988
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: David G. Cooper, Peter D. Miles, Rodney C. Young
  • Patent number: 4757071
    Abstract: 2,6-Dimethyl-4-(2- or 3-substituted phenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid diesters, having vasodilating and blood pressure lowering effects, in the ester moiety at the 3-position of which a heterocyclic group is linked to an alkylene group through an ester bond (carbonyloxy group). The diesters are used for treatment of cardiac diseases, cerebrovascular diseases and hypertension.
    Type: Grant
    Filed: December 9, 1985
    Date of Patent: July 12, 1988
    Assignee: Nisshin Flour Milling Co., Ltd.
    Inventors: Hiroyasu Koyama, Yoshikuni Suzuki, Koichiro Hagihara
  • Patent number: 4731370
    Abstract: This invention relates to a novel 1,4-dihydropyridine derivative of the formula ##STR1## wherein R2 is pyridyl, or a salt thereof. These compounds have a vasodilating activity and a platelet aggregation inhibiting activity. Also disclosed are pharmaceutical compositions containing the same.
    Type: Grant
    Filed: June 10, 1986
    Date of Patent: March 15, 1988
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Isao Watanabe, Kaishu Momonoi, Toru Hiraiwa, Satoshi Ono, Joji Nakano, Katsuyuki Nagumo, Hiroyasu Takagi
  • Patent number: 4713387
    Abstract: This invention relates to a 1,4-dihydropyridine derivative of the formula ##STR1## wherein Y represents an oxygen or sulfur atom or a vinylene group, Z represents an oxygen or sulfur atom or an alkylene group, R.sup.2 represents an imidazolyl or pyridyl group and the remaining substituents are herein defined. These compounds have a vasodilating activity and a platelet aggregation inhibiting activity.
    Type: Grant
    Filed: June 21, 1985
    Date of Patent: December 15, 1987
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Isao Watanabe, Kaishu Momonoi, Toru Hiraiwa, Satoshi Ono, Joji Nakano, Katsuyuki Nagumo, Hiroyasu Takagi
  • Patent number: 4698352
    Abstract: This invention relates to a novel 4-oxo-1,4-dihydronicotinic acid derivative ##STR1## or a salt thereof, wherein R.sup.1 is hydrogen or carboxyl-protecting group;R.sup.2 is substituted phenyl and naphthyl, or a substituted or unsubstituted heterocyclic group; andR.sup.3 is haloalkyl, aminoalkyl, or substituted or unsubstituted alkenyl, phenylalkenyl, naphthylalkenyl, phenylalkyl, naphthylalkyl, phenylalkynyl, naphthylalkynyl, heterocyclic alkyl, heterocyclic alkenyl, phenyl, naphthyl, cycloalkyl, cycloalkenyl, carboxylic acyl, iminoalkyl, heterocyclic or bridged hydrocarbon, which has a broad antibacterial spectrum and a low toxicity, and are useful for treatment of diseases of human beings and animals, to a process for producing the same and to an antibacterial agent containing the same.
    Type: Grant
    Filed: October 27, 1983
    Date of Patent: October 6, 1987
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Hirokazu Narita, Yoshinori Konishi, Jun Nitta, Shunjiro Misumi, Hideyoshi Nagaki, Isao Kitayama, Yoriko Nagai, Yasuo Watanabe, Nobuyuki Matsubara, Shinzaburo Minami, Isamu Saikawa
  • Patent number: 4696933
    Abstract: The invention relates to amide derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention there is provided a guanidine derivative of the formula I: ##STR1## in which R.sup.1 is a hydrogen or 1-10C alkyl, 3-8C cycloalkyl, 4-14C cycloalkyl, 3-6C alkenyl, 3-6C alkynyl, 1-6C alkanoyl, 6-10C aryl, 7-11C aralkyl or 7-11C aroyl, the aryl, aralkyl and aroyl radical being optionally substituted; ring X is a heterocyclic ring as defined in the specification; A is phenylene or 5-7C cycloalkylene, or a 1-8C alkylene into which is optionally inserted one or two groups; D is O or S; and R.sup.2 and R.sup.3 are hydrogen or a variety of radicals described in the specification: and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing processes and pharmaceutical compositions are also described.
    Type: Grant
    Filed: February 12, 1985
    Date of Patent: September 29, 1987
    Assignees: ICI Americas Inc., Imperial Chemical Industries PLC
    Inventors: Tobias O. Yellin, David J. Gilman
  • Patent number: 4694004
    Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is hydrogen,R.sup.2 is hydrogen, lower alkyl, ar(lower)alkyl, lower alkenyl or aryl,R.sup.3 is lower alkyl, ar(lower)alkyl, lower alkenyl or aryl, orR.sup.2 and R.sup.3 are taken together to form (C.sub.2 -C.sub.6)-alkylidene group optionally substituted with aryl or taken together with the attached nitrogen atom to form a saturated or unsaturated, 5- or 6-membered heterocyclic group optionally substituted with aryl or lower alkyl; orR.sup.1 and R.sup.2 are taken together with the attached nitrogen atoms to form a saturated or unsaturated, 5- or 6-membered heterocyclic group or 1,2-diazaspiroalkane-1,2-diyl group,R.sup.3 is hydrogen, lower alkyl, ar(lower)alkyl, lower alkenyl or aryl;R.sup.4 is lower alkyl optionally substituted with di(lower)alkylamino or a heterocyclic group, or a heterocyclic group optionally having suitable substituent(s),R.sup.
    Type: Grant
    Filed: June 19, 1985
    Date of Patent: September 15, 1987
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Osamu Nakaguti, Norihiko Shimazaki, Yoshio Kawai, Masashi Hashimoto, Michie Nakatuka
  • Patent number: 4666922
    Abstract: There is disclosed a method for immunomodulation employing as active agents certain substituted 1,8-naphthyridines and 1,5,8-azanaphthyridines.
    Type: Grant
    Filed: March 13, 1986
    Date of Patent: May 19, 1987
    Assignee: Schering Corporation
    Inventors: Sidney R. Smith, Marvin I. Siegel
  • Patent number: 4659725
    Abstract: Pyridine derivatives are disclosed which are useful as histamine H.sub.1 -antagonists.
    Type: Grant
    Filed: June 19, 1986
    Date of Patent: April 21, 1987
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: Robert J. Ife
  • Patent number: 4659722
    Abstract: Disclosed is the compound of the formula: ##STR1## wherein X is oxygen, sulfur or ##STR2## R.sub.1 is 3-pyridyl or 4-pyridyl, R.sub.2 is C.sub.1 .about.C.sub.12 -alkyl; C.sub.3 - or C.sub.4 -alkenyl; C.sub.5 - or C.sub.6 -cycloalkyl which may be substituted by C.sub.1 - or C.sub.2 -alkyl; pyridyl; pyridylmethyl; phenethyl cyanoalkyl having 1 or 2 carbon atoms; methoxyethyl; 1-methylmethoxypropyl; phenyl; phenyl which is substituted by one or more of C.sub.1 .about.C.sub.4 -alkyl, C.sub.1 .about.C.sub.4 -alkoxy, nitro, halogen, trifluoromethyl, allyl and methoxycarbonyl; benzyl; benzyl which is substituted by one or more of methyl, nitro, methoxy and chloro; .alpha.-methylbenzyl; C.sub.1 .about.C.sub.6 -alkyl which is substituted by halogen when X is oxygen or ##STR3## C.sub.2 - or C.sub.3 -alkyl which is substituted by dimethylamino, furfuryl or thienylmethyl; R.sub.3 is hydrogen, C.sub.1 .about.C.sub.4 -alkyl, cyanomethyl, methoxycarbonylmethyl, or 1-propoxycarbonylmethyl. These compounds are bactericides.
    Type: Grant
    Filed: August 1, 1985
    Date of Patent: April 21, 1987
    Assignee: Nippon Kayaku Kabushiki Kaisha
    Inventors: Taizo Nakagawa, Eiichi Tanaka, Kengo Koike, Hiromi Yoshida, Hiroshi Yoshida
  • Patent number: 4657908
    Abstract: The invention relates to carbonyl derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention where is provided a guanidine derivative of the formula I: ##STR1## in which R.sup.1 and R.sup.2, same or different, are hydrogen or 1-10C alkyl, 3-8C cycloalkyl or 4-14C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, Cl or Br atoms, provided that one of R.sup.1 and R.sup.2 is halogen substituted, or R.sup.2 is hydrogen and R.sup.1 is R.sup.5 -E-W in which W is 2-6C alkylene optionally substituted by 1 or 2 1-4C alkyls, E is O, S, SO, SO.sub.2 or NR.sup.6 in which R.sup.6 is H or 1-6C alkyl, R.sup.5 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R.sup.5 and R.sup.6 are joined to form a pyrrolidine, piperidine, morpholine, piperazine or N-methylpiperazine ring, or R.sup.2 is H and R.sup.
    Type: Grant
    Filed: February 12, 1985
    Date of Patent: April 14, 1987
    Assignees: ICI Americas, Inc., Imperial Chemical Industries PLC
    Inventors: Tobias O. Yellin, David J. Gilman, Philip N. Edwards, Michael S. Large, Derrick F. Jones, Keith Oldham
  • Patent number: 4657919
    Abstract: Described are compounds of the formula ##STR1## wherein R is hydrogen, lower alkyl, halo, cyano, hydroxy, amino, lower alkylamino, --CH.sub.2 NH.sub.2, --CH.sub.2 OH or --COOR"; R' is hydrogen, lower cycloalkyl or lower alkyl; R' is lower alkenyl, lower alkynyl, lower cycloalkyl, --(W).sub.n Y wherein W is straight or branched chain lower alkyl or lower alkenyl, n is 0 to 5, and Y is Ar, lower cycloalkyl, lower alkenyl, lower alkynyl, --COOZ wherein Z is lower alkyl, ##STR2## or NAB wherein A and B are, independently, lower alkyl, benzyl or substituted benzyl, and Ar is 2, 3 or 4-pyridyl, pyridazinyl, pyrimidinyl, quinolyl, isoquinolyl, phthalazinyl, quinazolinyl, thiazolyl, phenyl, benzyl, furyl, tetrahydrofuryl or thienyl, unsubstituted or substituted with lower alkyl, lower alkoxy, halo, amino, or --CF.sub.3 ; R"' is --COOR", ##STR3## and X is oxygen or nitrogen; or a pharmaceutically acceptable salt thereof, and their use in the treatment of impaired ventricular myocardial contractility.
    Type: Grant
    Filed: July 12, 1985
    Date of Patent: April 14, 1987
    Assignee: E. I. Du Pont de Nemours & Co.
    Inventors: David M. Stout, Diane M. Yamamoto, Cynthia Barcelon-Yang
  • Patent number: 4650806
    Abstract: 3-Z-5-(Q-CO)-6-methyl-2(1H)-pyridinones (I) or salts thereof, where Q is 2(or 3)-furanyl or 2(or 3)-thienyl when Z is hydrogen or cyano, or where Q is 4(or 3)-pyridinyl or 4(or 3)-pyridinyl having one or two methyl substituents only when Z is cyano, are useful as cardiotonic agents. Processes for preparing said compounds (I) are shown.
    Type: Grant
    Filed: January 14, 1985
    Date of Patent: March 17, 1987
    Assignee: Sterling Drug Inc.
    Inventors: George Y. Lesher, Baldev Singh
  • Patent number: 4644004
    Abstract: Pyridinecarboxylic esters of dopamine and of its N-alkyl derivatives, salts thereof with pharmaceutically acceptable organic or inorganic acids, process for preparing them and pharmaceutical compositions containing them which are particularly useful in the treatment of cardiovascular and renal disorders.
    Type: Grant
    Filed: February 8, 1985
    Date of Patent: February 17, 1987
    Assignee: Simes S.p.A.
    Inventors: Cesare Casagrande, Emilio Mussini, Vittorio Vecchietti
  • Patent number: 4610993
    Abstract: Described is a method for treating an animal for bovine mastitis wherein said animal is administered an effective amount of at least one selected pyridine-N-oxide disulfide compound to treat or prevent bovine mastitis.
    Type: Grant
    Filed: August 8, 1984
    Date of Patent: September 9, 1986
    Assignee: Olin Corporation
    Inventors: John H. Wedig, John G. Babish, Jeffrey Davidson
  • Patent number: 4609665
    Abstract: Described is a method for treating an animal for swine exudative epidermitis wherein said animal is administered an effective amount of at least one selected pyridine-N-oxide disulfide compound.
    Type: Grant
    Filed: August 8, 1984
    Date of Patent: September 2, 1986
    Assignee: Olin Corporation
    Inventors: Jeffrey Davidson, John G. Babish, John H. Wedig
  • Patent number: 4594352
    Abstract: There are described compounds of formula: ##STR1## in which one of R and R.sup.1 is F or Cl and the other is H, F or Cl;X is a 1,4-phenylene or pyridyl bound in positions 2 and 5, optionally substituted;Y is a phenyl, 2- or 3-pyridyl, optionally substituted.The compounds of formula I are endowed with a high insecticide activity which is mainly directed against insect larvae and eggs.
    Type: Grant
    Filed: April 19, 1984
    Date of Patent: June 10, 1986
    Assignee: Montedison S.p.A.
    Inventors: Pietro Massardo, Franco Bettarini, Gabriele Giovarruscio, Paolo Piccardi, Franca Reggiori, Vincenzo Caprioli, Angelo Longoni
  • Patent number: 4590195
    Abstract: 1,4-Dihydropyridine derivatives of the formula: ##STR1## wherein R is aryl or heteroaryl; R.sup.1 and R.sup.2 are each C.sub.1 -C.sub.4 alkyl or 2-methoxyethyl; n is 2, 3 or 4; R.sup.3 is H, C.sub.1 -C.sub.4 alkyl, CH.sub.2 CO.sub.2 (C.sub.1 -C.sub.4 alkyl) or CH.sub.2 CN; and R.sup.4 is a group of the formula COR.sup.5, CSR.sup.5, C(.dbd.NR.sup.6)R.sup.7 or SO.sub.2 R.sup.5, wherein R.sup.5 is C.sub.1 -C.sub.4 alkyl, NH.sub.2, NH(C.sub.1 -C.sub.4 alkyl), NH(C.sub.3 -C.sub.6 cycloalkyl), N(C.sub.1 -C.sub.4 alkyl).sub.2, NHCH.sub.2 CO.sub.2 (C.sub.1 -C.sub.4 alkyl), NHCH.sub.2 CONH.sub.2, NHCH.sub.2 CO.sub.2 H, NH(CH.sub.2).sub.2 NH.sub.2, NHNH.sub.2, NHNRCO.sub.2 (C.sub.1 -C.sub.4 alkyl), NH-aryl, NHCO-aryl or a heterocyclic, NH-heterocyclic or NHCO-heterocyclic group, or when R.sup.4 is C(.dbd.O)R.sup.5, R.sup.5 may be H or CF.sub.3 ; R.sup.6 is H, CN, CO.sub.2 (C.sub.1 -C.sub.4 alkyl), CO(C.sub.1 -C.sub.4 alkyl), SO.sub.2 (C.sub.1 -C.sub.4 alkyl), SO.sub.2 -aryl, SO.sub.2 NH.sub.2, SO.sub.2 N(C.sub.1 -C.
    Type: Grant
    Filed: March 5, 1984
    Date of Patent: May 20, 1986
    Assignee: Pfizer Inc.
    Inventors: David Alker, Peter E. Cross, Simon F. Campbell
  • Patent number: 4579856
    Abstract: Compounds of the formula: ##STR1## wherein X is oxygen or sulfur; Z is oxygen or sulfur; R is pyridyl optionally substituted with 1 to 3 substituents independently selected from halogen, lower alkyl or lower alkoxy optionally substituted with 1 to 3 of the same or different halogen atoms or nitro; R.sup.1 is lower alkyl; and R.sup.2 is a 5- or 6-membered heterocyclic ring containing 1 to 3 ring nitrogens and the remainder of the ring atoms carbon atoms, a quinoline ring or a phenyl ring, all optionally substituted with 1 to 3 substituents independently selected from halogen, trihalomethyl, lower alkyl or lower alkoxy are fungicidal.
    Type: Grant
    Filed: September 23, 1983
    Date of Patent: April 1, 1986
    Assignee: Chevron Research Company
    Inventor: David C. K. Chan
  • Patent number: 4576955
    Abstract: The invention provides a compound of the formula I ##STR1## wherein Y is a heterocyclic radical of formula ##STR2## wherein R is hydrogen or lower alkyl, R.sup.1 is hydrogen, hydroxy, lower alkyl, hydroxyloweralkyl, loweralkoxyloweralkyl, loweralkoxy, halogen, formyl, phenyl, phenylalkyl, halophenyl, or acetal [CH(OR.sup.4).sub.2 where R.sup.4 is lower alkyl or two R.sup.4 radicals are joined to form a lower alkylene chain], m is 1 or 2, the dotted lines in formula V represent an optional double bond in one of the indicated positions, A is a saturated or unsaturated alkylene radical having from 1 to 6 carbon atoms, which may be substituted by lower alkyl of 1 to 6 carbon atoms, S is sulphur and R.sup.3 is lower alkyl, phenyl or aralkyl of 7 to 12 carbon atoms and Z.sup.- is an anion, and acid addition salts thereof, with the provisos that (1) when more than one R.sup.1 radical is present in the molecule then the R.sup.
    Type: Grant
    Filed: October 13, 1983
    Date of Patent: March 18, 1986
    Assignee: John Wyeth & Brother, Ltd.
    Inventors: Roger Crossley, Kay H. Dickinson
  • Patent number: 4542140
    Abstract: .alpha.-Cyanoacrylic acid lower alkyl esters, and their corresponding amides, characterized by having a heterocyclic containing mercapto radical as one .beta.-substituent and an alkylthio, alkenylthio or a heterocyclic containing mercapto radical as another .beta.-substituent are useful for treating ulcers and for suppressing gastric acid secretion.
    Type: Grant
    Filed: October 20, 1983
    Date of Patent: September 17, 1985
    Assignee: American Home Products Corporation
    Inventors: Jehan Bagli, Tibor Bogri, Bozidar Palameta, Luis E. Borella
  • Patent number: 4539316
    Abstract: Compounds of the formula ##STR1## wherein R.sup.12 is a leaving group, Z is S, O or CH.sub.2 and A is a phenyl, furyl, thienyl or pyridyl ring substituted by a ##STR2## moiety, in which R.sup.8 and R.sup.9 are various substituents or, when taken together with the nitrogen, may be a specified heterocyclic ring, are intermediates in the preparation of histamine H.sub.2 -antagonist anti-ulcer agents of the formula ##STR3## in which R.sup.1 and R.sup.2 are any of several specified substituents.
    Type: Grant
    Filed: October 1, 1984
    Date of Patent: September 3, 1985
    Assignee: Bristol-Myers Company
    Inventors: Aldo A. Algieri, Ronnie R. Crenshaw
  • Patent number: 4532246
    Abstract: Pyridine derivatives are disclosed which are useful as histamine H.sub.1 -antagonists.
    Type: Grant
    Filed: December 20, 1983
    Date of Patent: July 30, 1985
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: Robert J. Ife
  • Patent number: 4521428
    Abstract: Novel 4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridines of formula ##STR1## wherein R is an unsubstituted or by an alkyl group of from 1 to 4 carbon atoms substituted pyridyl, pyridyl 1-oxide or naphthyl group and Alk is a straight or branched chain alkylene group of from 2 to 4 carbon atoms are anorexigenic agents useful for treating obesity.
    Type: Grant
    Filed: August 16, 1983
    Date of Patent: June 4, 1985
    Assignee: Sanofi
    Inventors: Dino Nisato, Marco Frigerio, Giovanna F. Miranda
  • Patent number: 4521535
    Abstract: The invention relates to 4-pyridone-3-carboxylic acid derivatives, a process for the preparation thereof and pharmaceutical compositions containing same. The 4-pyridone-3-carboxylic acid derivatives are useful as antibacterial agents and/or as agents having a stimulating activity on the central nervous system.
    Type: Grant
    Filed: April 19, 1982
    Date of Patent: June 4, 1985
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Alexander E. Wick
  • Patent number: 4514408
    Abstract: N-substituted nicotinamide 1-oxide having histamine H.sub.2 receptor blocking activity of formula ##STR1## wherein X is a nitrogen atom or a CH group and Am represents a mono- or disubstituted amino group, a pyrrolidino, morpholino, thiomorpholino, hexamethyleneimino group, or an optionally substituted piperidino or piperazino group; their salts; a process for their preparation; and pharmaceutical compositions containing them as active ingredients.
    Type: Grant
    Filed: August 12, 1983
    Date of Patent: April 30, 1985
    Assignee: Sanofi
    Inventors: Dino Nisato, Sergio Boveri
  • Patent number: 4508719
    Abstract: Compounds of formula I: ##STR1## are described in which R.sup.1 is a linear or branched alkyl radical containing between 1 and 5 carbon atoms, the alkyl radical being unsubstituted or substituted by an alkoxy group; R.sup.2 is an unsubstituted phenyl of phenyl substituted by a nitro group; R.sup.3 is hydrogen or a linear or branched alkyl residue containing between 1 and 4 carbon atoms, the alkyl radical being unsubstituted or substituted by at least one alkoxy or fluorine atom or both alkoxy and fluorine atoms; R.sup.4 is hydrogen or a linear or branched alkyl containing between 1 and 4 carbon atoms, the alkyl radical being unsubstituted or substituted by alkoxy, carbalkoxy, dialkylamino, 1-aryl or 1-heteroarylpiperazinyl, aryl or a monocyclic 5 or 6 membered heterocycle in which at least one of the heteroatoms is N,O,S such as 1-piperidinyl, 4-morpholinyl or R.sub.4 is alkenyl or cyclo(C.sub.3 -C.sub.
    Type: Grant
    Filed: May 26, 1983
    Date of Patent: April 2, 1985
    Assignee: Pierrel S.p.A.
    Inventors: Silvia Z. Tricerri, Cesare Casagrande, Franco De Marchi, Massimo Nicola
  • Patent number: 4505917
    Abstract: Selected (1-oxo-2-pyridyl) disulfides are used as active ingredients in animal feed compositions and in methods for increasing the growth and feed efficiency of monogastric animals. A useful new compound of this invention is 2-carboxyphenyl (1-oxo-2-pyridyl) disulfide.
    Type: Grant
    Filed: September 21, 1982
    Date of Patent: March 19, 1985
    Assignee: SmithKline Beckman Corporation
    Inventors: Govind K. Menon, Winfred J. Sanders
  • Patent number: 4496564
    Abstract: The invention relates to amide derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention there is provided a guanidine derivative of the formula I: ##STR1## in which R.sup.1 is a hydrogen or 1-10C alkyl, 3-8C cycloalkyl, 4-14C cycloalkylalkyl, 3-6C alkenyl, 3-6C alkynyl, 1-6C alkanoyl, 6-10C aryl, 7-11C aralkyl or 7-11C aroyl, the aryl, aralkyl and aroyl radical being optionally substituted; ring X is a heterocyclic ring as defined in the specification; A is phenylene or 5-7C cycloalkylene, or a 1-8C alkylene into which is optionally inserted one or two groups; D is O or S; and R.sup.2 and R.sup.3 are hydrogen or a variety of radicals described in the specification: and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing processes and pharmaceutical compositions are also described.
    Type: Grant
    Filed: March 1, 1982
    Date of Patent: January 29, 1985
    Assignees: ICI Americas Inc., Imperial Chemical Industries PLC
    Inventors: Tobias O. Yellin, David J. Gilman