Ring Or Polycyclo Ring System In Substituent E Is Attached Indirectly To The Carboxamide Nitrogen Or To An Amino Nitrogen In Substituent E By Acyclic Nonionic Bonding Patents (Class 564/185)
  • Patent number: 5041665
    Abstract: A process for preparing a squarylium compound useful as a photoconductive material for an electrophotographic photoreceptor, in which process comprises reacting an arylhydroxycyclobutenedione salt or a hydroxycyclobutenedione derivative with an aniline derivative is disclosed. The process comprises dropwise adding a solution of the arylhydroxycyclobutenedione salt or hydroxycyclobutenedione derivative in a solvent, to an alcohol solution of the aniline derivative in an alcohol solvent. An electrophotographic photoreceptor produced by using the thus obtained squarylium compound exhibits and sensitivity, satisfactory chargeability, low dark decay, low residual potential, and excellent stability after repeated use.
    Type: Grant
    Filed: December 1, 1988
    Date of Patent: August 20, 1991
    Assignee: Fuji Xerox Co., Ltd.
    Inventors: Yutaka Akasaki, Akihiko Tokida, Kaoru Torikoshi, Akira Imai, Hidemi Suto
  • Patent number: 5021414
    Abstract: A phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined bis-phenolic nucleus including a hydroxyphenyl-hydroxynaphthyl; hydroxyphenyl-hydroxyindanyl, hydroxyphenyl-hydroxybenzothienyl or di-hydroxyphenyl-ethylene or vinylene nucleus;wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages,wherein R.sup.1 is hydrogen, or alkyl, alkenyl, cycloalkyl, halogenoalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 -- or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --S--, --SO-- or --SO.sub.2 --,wherein R.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene;wherein R.sup.12 is hydrogen or alkyl, and wherein R.sup.22 is hydrogen, cyano or nitro;or a salt thereof when appropriate.
    Type: Grant
    Filed: December 18, 1989
    Date of Patent: June 4, 1991
    Assignee: Imperial Chemical Industries PLC
    Inventors: William R. Pilgrim, Derek W. Young, Brian S. Tait, Graham C. Crawley, Philip N. Edwards, George B. Hill
  • Patent number: 4992588
    Abstract: O-acrylaminomethylbenzyl halides (I) ##STR1## in which X is Cl or Br and R.sup.1 is alkyl or aryl, are obtained by reacting an o-aminomethylbenzyl alkyl ether (II) ##STR2## with an acylating agent, and then reacting the resulting acid amide, preferably without intermediate isolation, with an aqueous hydrohalic acid.
    Type: Grant
    Filed: July 31, 1985
    Date of Patent: February 12, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Josef Mueller, Walter-Weilant Wiersdorff, Werner Kirschenlohr, Gerd Schwantje
  • Patent number: 4987257
    Abstract: Disclosed is a diacetylene compound comprising, as structural units, (a) at least one member selected from diacetylene group-containing organic groups of the formulae (I) and (II):R.sup.I --C.tbd.C--C.tbd.C--R.sup.II -- (I)and--R.sup.III --C.tbd.C--C.tbd.C--R.sup.IV -- (II)wherein R.sup.I is hydrogen or a (C1-16) monovalent organic group, and R.sup.II, R.sup.III and R.sup.IV are a (C1-13) divalent organic group, (b) at least one organic group having at least one carbon-to-carbon double bond, and (c) at least one connecting group connecting the units (a) and (b), which connecting group is selected from amide, imide, ester, ether, amino, imino, urethane, sulfonyl and carbonyl bonds. A cured shaped article made of this compound exhibits isotropically a high elastic modulus and has excellent mechanical properties.
    Type: Grant
    Filed: February 23, 1990
    Date of Patent: January 22, 1991
    Assignee: Director-General of Agency of Industrial Science and Technology
    Inventors: Katsuyuki Nakamura, Satoru Yamazaki, Jinichiro Kato, Kensaku Tokushige
  • Patent number: 4957533
    Abstract: Compounds of the formula (I): ##STR1## wherein: X=O, S, or NOH;R.sup.1 is H or CH.sub.3 ;n=1, 2, or 3;R.sup.2, R.sup.3, and R.sup.4 are as defined in one of the following paragraphs(a) R.sup.2 and R.sup.3 are independently Cl or Br, and R.sup.4 is H;(b) R.sup.2, R.sup.3 and R.sup.4 are independently Cl or Br;(c) R.sup.2 is F, R.sup.3 is Cl, and R.sup.4 is H; or(d) R.sup.2 and R.sup.3 are CH.sub.3 or C.sub.2 H.sub.5, and R.sup.4 is H;R.sup.5, R.sup.6 and R.sup.7 are as defined in one of the following paragraphs(a) one of R.sup.6 and R.sup.7 is CF.sub.3, R.sup.5 and the other of R.sup.6 and R.sup.7 is H;(b) R.sup.5 and R.sup.6 are H; and R.sup.7 is F, Cl, or Br;(c) R.sup.5 and R.sup.7 are independently F, Cl or Br and R.sup.6 is H;(d) R.sup.5 and R.sup.6 are independently F, Cl, or Br, and R.sup.7 is H;(e) R.sup.6 and R.sup.7 are independently F, Cl, or Br, and R.sup.5 is H; or(f) R.sup.6 is phenoxy and R.sup.5 and R.sup.7 are Hare plant fungicides.
    Type: Grant
    Filed: September 1, 1988
    Date of Patent: September 18, 1990
    Assignee: Eli Lilly and Company
    Inventors: Wendell R. Arnold, James D. Davenport
  • Patent number: 4950795
    Abstract: Compounds of the formula I ##STR1## in which n is 1-30 and X, Y, R, Ar.sup.1 and Ar.sup.2 are as defined in claim 1 can be prepared by reaction of a benzil dialkyl ketal with a diol. Depending on the molar ratio of the two reaction components, products having a different polycondensation degree n are obtained. The compounds can be used as photoinitiators.
    Type: Grant
    Filed: August 18, 1988
    Date of Patent: August 21, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Rinaldo Husler, Rudolf Kirchmayr, Werner Rutsch, Manfred Rembold
  • Patent number: 4933493
    Abstract: Novel 4-phenyl-1,3-benzodiazepines, novel intermediates thereof, and methods of preparing same are described. These benzodiazepines are useful as antidepressants, analgetics and anticonvulsants.
    Type: Grant
    Filed: April 6, 1989
    Date of Patent: June 12, 1990
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Lawrence L. Martin, Manfred Worm, Charles A. Crichlow
  • Patent number: 4904661
    Abstract: A phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined bis-phenolic nucleus including a hydroxyphenyl-hydroxynaphthyl; hydroxyphenyl-hydroxyindanyl, hydroxyphenyl-hydroxybenzothienyl or di-hydroxyphenyl-ethylene or vinylene nucleus;wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages,wherein R.sup.1 is hydrogen, or alkyl, alkenyl, cycloalkyl, halogenoalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 -- or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --S--, --SO-- or --SO.sub.2 --, wherein R.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene;wherein R.sup.12 is hydrogen or alkyl, and wherein R.sup.22 is hydrogen, cyano or nitro;or a salt thereof when appropriate.
    Type: Grant
    Filed: December 16, 1987
    Date of Patent: February 27, 1990
    Assignee: Imperial Chemical Industries PLC
    Inventors: William R. Pilgrim, Derek W. Young, Brian S. Tait, Graham C. Crawley, Philip N. Edwards, George B. Hill
  • Patent number: 4885313
    Abstract: Novel 3,4-dihydroxyphenylethylamine derivatives possess dopaminergic activity in animals and are therefore useful in the treatment of iner alia congestive heart failure, renal failure and reversible obstructive airways disease.The compounds are generally administered in the form of a pharmaceutical composition comprising the active ingredient in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier.
    Type: Grant
    Filed: December 2, 1987
    Date of Patent: December 5, 1989
    Assignee: Fisons plc
    Inventors: John Dixon, Francis Ince
  • Patent number: 4873335
    Abstract: Compounds of the formula: ##STR1## are produced, with the variables as indicated within.
    Type: Grant
    Filed: December 2, 1987
    Date of Patent: October 10, 1989
    Assignee: Schering Corporation
    Inventors: Doris P. Schumacher, Bruce L. Murphy, Jon E. Clark
  • Patent number: 4853381
    Abstract: The invention provides compounds of the general formula (I) ##STR1## whereinAr represents a phenyl group optionally substituted by one or more substituents selected from halogen atoms, or the groups C.sub.1-6 alkyl, C.sub.1-6 alkoxy, nitro, --(CH.sub.2).sub.q R [where R is hydroxy, --NR.sup.3 R.sup.4 (where R.sup.3 and R.sup.4 each represent a hydrogen atom or a C.sub.1-4 alkyl group, or --NR.sup.3 R.sup.4 forms a saturated heterocyclic amino group which has 5-7 ring members and optionally contains in the ring one or more atoms selected from --O--, or --S-- or a group --NH-- or --N(CH.sub.3)--), --NR.sup.5 COR.sup.6 (where R.sup.5 represents a hydrogen atom or a C.sub.1-4 alkyl group, and R.sup.6 represents a hydrogen atom or a C.sub.1-4 alkyl, C.sub.1-4 alkoxy, phenyl or --NR.sup.3 R.sup.4 group), --NR.sup.5 SO.sub.2 R.sup.7 (where R.sup.7 represents a C.sub.1-4 alkyl, phenyl or --NR.sup.3 R.sup.4 group), --COR.sup.8 (where R.sup.8 represents hydroxy, C.sub.1-4 alkoxy or --NR.sup.3 R.sup.4), --SR.sup.
    Type: Grant
    Filed: October 15, 1986
    Date of Patent: August 1, 1989
    Assignee: Glaxo Group Limited
    Inventors: Harry Finch, Lawrence H. C. Lunts, Alan Naylor, Ian F. Skidmore, Ian B. Campbell
  • Patent number: 4822902
    Abstract: Certain N-acetonylbenzamides exhibit low toxicity to plants are particularly useful for control of fungi, especially Phycomycetes.
    Type: Grant
    Filed: July 26, 1984
    Date of Patent: April 18, 1989
    Assignee: Rohm and Haas Company
    Inventors: H. Edwin Carley, Ashok K. Sharma
  • Patent number: 4782150
    Abstract: Water-soluble triphendioxazine compounds which have valuable fiber-reactive dyestuff properties and correspond to the general formula (1) and dye materials, in particular cellulose fiber materials, containing carboxamide and/or hydroxy groups in fast shades. ##STR1## in which: B is a group --O--, --S--, --NH-- or --N(R')-- in which R' is alkyl having 1 to 6 carbon atoms;R* is hydrogen or optionally substituted lower alkyl or optionally substituted aryl;W and W.sup.1 independently of one another are each a divalent aliphatic radical or a cycloaliphatic radical which is optionally substituted by lower alkyl or an aliphatic-cycloaliphatic radical which is optionally substituted by lower alkyl, it being possible for the aliphatic radicals to be interrupted by one or more groups --O--, --S--, --SO.sub.2 --, --CO--, 1,4-piperidino, --NH-- and --N(R.sup.o)-- in which R.sup.o has the meaning of R' or is lower alkanoyl;the groupings --B--W.sup.
    Type: Grant
    Filed: August 11, 1987
    Date of Patent: November 1, 1988
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hartmut Springer, Walter Helmling, Gunther Schwaiger
  • Patent number: 4762548
    Abstract: Herbicidally active thiolcarbamates are employed in combination with a certain amide extender compound, the latter in sufficient quantity to minimize soil degradation and to prolong the soil life of the former. As a result, the herbicidal effectiveness of the thiolcarbamate herbicide is significantly enhanced and prolonged, rendering a single application or multiple applications of the herbicide effective over a longer period of time. Such herbicidal compositions can optionally contain a non-phytotoxic antidotally effective amount of thiolcarbamate herbicide antidote.
    Type: Grant
    Filed: August 12, 1985
    Date of Patent: August 9, 1988
    Assignee: Stauffer Chemical Co.
    Inventors: Reed A. Gray, Ferenc M. Pallos
  • Patent number: 4743595
    Abstract: A process for efficiently preparing 2-amino-5-nitrophenol derivatives in which benzoxazole derivatives are subjected to nucleophilic substitution reaction at the 5 position thereof to obtain corresponding benzoxazole derivatives, and the oxazole ring of the benzoxazole derivatives is then subjected to ring-opening to obtain 2-amino-5-nitrophenol derivatives. The 2-amino-5-nitrophenol derivatives are useful as industrial starting materials, reducing agents or antioxidants and intermediates for cyan-image-forming couplers.
    Type: Grant
    Filed: June 12, 1985
    Date of Patent: May 10, 1988
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Isamu Itoh, Mitsunori Ono, Hidetoshi Kobayashi, Kazuyoshi Yamakawa
  • Patent number: 4740508
    Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.
    Type: Grant
    Filed: April 22, 1985
    Date of Patent: April 26, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Harold N. Weller, III, Eric M. Gordon
  • Patent number: 4736066
    Abstract: Intermediates of the formula ##STR1## are disclosed. These compounds are useful in preparing substituted peptide compounds which possess hypotensive and analgesic activity.
    Type: Grant
    Filed: May 25, 1984
    Date of Patent: April 5, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Sesha I. Natarajan, Eric M. Gordon
  • Patent number: 4692553
    Abstract: Cyclohexenone derivatives of the formula ##STR1## where R.sup.1 is hydrogen, methoxycarbonyl, ethoxycarbonyl, methyl or cyano, R.sup.2 is alkyl, R.sup.3 is alkyl, alkenyl, haloalkenyl, or propargyl, R.sup.4 is hydrogen or alkyl, R.sup.5 is hydrogen, alkyl, acyl, formyl, cycloalkylcarbonyl, methoxyalkylcarbonyl, unsubstituted or substituted benzoyl, alkoxycarbonyl, benzyloxycarbonyl, phenoxycarbonyl, alkylthiocarbonyl, N,N-dialkylcarbamyl, N-alkylcarbamyl, N-cycloalkylcarbamyl, N-alkoxy-N-alkylcarbamyl, unsubstituted or substituted N-phenylcarbamyl, alkylsulfonyl, alkenylsulfonyl, haloalkylsulfonyl, N-alkylsulfamyl, N,N-dialkylsulfamyl, N-acyl-N-alkylsulfamyl, N-alkyl-N-methoxycarbonylsulfamyl, dialkoxyphosphoryl, dialkoxythiophosphoryl, 2-haloalkanoyl, acyloxyacetyl or alkoxyoxalyl, and R.sup.6 is alkyl, halogen, hydroxyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkylsulfinyl, alkylsulfonyl, nitro or amino, and salts of these compounds, and the use of these compounds for controlling unwanted plant growth.
    Type: Grant
    Filed: July 26, 1985
    Date of Patent: September 8, 1987
    Assignee: BASF Aktiengesellschaft
    Inventors: Michael Keil, Ulrich Schirmer, Dieter Jahn, Rainer Becker, Bruno Wuerzer, Norbert Meyer
  • Patent number: 4691044
    Abstract: Mixtures of substances which are obtainable by reacting elementary sulfur with compounds of the formula I ##STR1## are described. The radical X contains an olefinic double bond. R is a hydrocarbon radical, p is 0, 1 or 2 and t is 1, 2 or 3. The mixtures of substances according to the invention can be employed as antioxidants in organic polymers and in lubricants. They can also be used as high-pressure additives or anti-wear additives.
    Type: Grant
    Filed: August 28, 1985
    Date of Patent: September 1, 1987
    Assignee: Ciba-Geigy Corporation
    Inventor: Samuel Evans
  • Patent number: 4643763
    Abstract: The invention concerns novel compounds of the formula I ##STR1## wherein: m is an integer selected from 1 to 4;n is zero or an integer selected from 1 to 4;x are selected from halogen, nitro, cyano, alkyl, substituted alkyl, hydroxy, alkoxy, alkylthio, sulfamoyl, substituted sulfamoyl, amino, substituted amino, the group --(CH.sub.2).sub.p C(.dbd.A)Z in which p is zero or one A is oxygen or sulfur, and Z is hydrogen, hydroxy, alkoxy, alkylthio, alkyl, substituted alkyl, amino or substituted amino; the group --NHC(.dbd.B(NR.sup.7 R.sup.8 in which B is oxygen or sulfur and R.sup.7 and R.sup.8 are hydrogen or alkyl;R.sup.1 is selected from hydrogen, acyl and an inorganic or organic cation;R.sup.2 is selected from alkyl, substituted alkyl, alkenyl, haloalkenyl, alkynyl and haloalkynyl;R.sup.3 is selected from alkyl, fluoroalkyl, alkenyl, alkynyl, and phenyl; andR.sup.4 is selected from hydrogen, halogen, alkyl, cyano and alkoxycarbonyl.
    Type: Grant
    Filed: September 10, 1985
    Date of Patent: February 17, 1987
    Assignee: ICI Australia Limited
    Inventors: Graeme J. Farquharson, Keith G. Watson, Graham J. Bird
  • Patent number: 4623729
    Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.
    Type: Grant
    Filed: July 22, 1982
    Date of Patent: November 18, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Sesha I. Natarajan, Eric M. Gordon
  • Patent number: 4616082
    Abstract: New hydroquinone ether compounds of formula I are described: ##STR1## wherein p is 1 or 2 and Q is 0 or 1, provided that p+q is 1 or 2, R is a residue of formula II ##STR2## and R.sub.o, R.sub.oo, R.sub.1, R.sub.2, R.sub.3, Q, n and k are as defined in the specification,The new compounds are useful e.g. as stabilizers in photographic material.
    Type: Grant
    Filed: June 7, 1985
    Date of Patent: October 7, 1986
    Assignee: Ciba-Geigy AG
    Inventor: Frederick H. Howell
  • Patent number: 4600796
    Abstract: A process for preparing a class of polyols resulting from the reaction of a bicyclic amide acetal with an alkanolamine is described.
    Type: Grant
    Filed: June 3, 1985
    Date of Patent: July 15, 1986
    Assignee: Ashland Oil, Inc.
    Inventor: Anil B. Goel
  • Patent number: 4595531
    Abstract: Benzodiazocines corresponding to the formula ##STR1## are converted to benzodiazepines corresponding to the formula ##STR2## of claim 1 by subjecting the benzodiazocine (a) if it is halogen-substituted in the 3-position to a thermal treatment which may also take place in the presence of a nucleophilic agent for the reaction or (b) if the 3-position is hydroxy substituted to treatment with a Lewis acid which is a chlorinating or brominating agent. Whenever the diazepine obtained as the final product has a 2-halogenomethyl group it may then be converted to benzodiazepine which is otherwise substituted in the 2-position.
    Type: Grant
    Filed: April 24, 1984
    Date of Patent: June 17, 1986
    Assignee: Kali-Chemie AG
    Inventors: Wolfgang Milkowski, Renke Budden, Siegfried Funke, Rolf Huschens, Hans-Gunther Liepmann, Werner Stuhmer, Horst Zeugner
  • Patent number: 4562201
    Abstract: The present invention relates to new compounds of the formula ##STR1## where X is ##STR2## alkylene, or --S-- where R.sub.1 is hydrogen, alkyl, or aryl; W is hydrogen, hydroxy, amino, alkyloxy, aryloxy, O-alkyl, or O-aralkyl; (Y).sub.A is --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 may be hydrogen, substituted alkyls, aryls, or together with N form a 5 to 7 membered heterocyclic group; and Ar is a substituted or unsubstituted aryl. These compounds are useful in the treatment of various cardiac arrhythmias.
    Type: Grant
    Filed: July 26, 1982
    Date of Patent: December 31, 1985
    Assignee: American Hospital Supply Corporation
    Inventors: David M. Stout, William L. Matier
  • Patent number: 4559172
    Abstract: This invention relates to a novel acylation process which comprises using as the acylating agent an o-hydroxy-substituted aromatic oxime ester represented by the general formula (I) ##STR1## and mixing said acylating agent with an amine substance represented by the general formula (III) ##STR2## to form a compound represented by the general formula (IV) ##STR3##
    Type: Grant
    Filed: May 1, 1984
    Date of Patent: December 17, 1985
    Assignee: Nitto Boseki
    Inventors: Ikuo Hayashi, Keizo Ogihara, Tadao Itikawa, Kiyoshi Shimizu
  • Patent number: 4558150
    Abstract: Intermediates of the formula ##STR1## are disclosed. These compounds are useful in the preparation of amino thiol dipeptides possessing angiotensin converting enzyme inhibition activity and enkephalinase inhibition activity.
    Type: Grant
    Filed: December 10, 1984
    Date of Patent: December 10, 1985
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Eric M. Gordon, Jollie D. Godfrey, Jr.
  • Patent number: 4480082
    Abstract: The reaction product of (i) an aromatic amide having the amine group of the amide attached to an aromatic ring, and (ii) a mono- or di-epoxide, has been found to be a good fortifier of epoxy resins. Epoxy resins have been found to attain increased strength and modulus (yet not brittle) by compounding:(a) a resin-forming polyepoxide,(b) an amine curing agent for (a), and(c) the above fortifier; and heat curing the mixture. Strengths as high as 130-150 MPa and modulus values to as high as 5000 MPa have been achieved yet with a ductile mode of fracture.
    Type: Grant
    Filed: July 25, 1983
    Date of Patent: October 30, 1984
    Assignee: Canadian Patents & Development Limited
    Inventors: Paul D. McLean, Andrew Garton, Robert F. Scott, Susan E. Gransden
  • Patent number: 4418069
    Abstract: The present invention is related to new benzisoselenazolones having the general formula I ##STR1## new products having the general formula II ##STR2## used as intermediary products in the production of the compounds of formula I and a method for the treatment of rheumatic diseases using a compound of formula I as active agent.
    Type: Grant
    Filed: July 9, 1981
    Date of Patent: November 29, 1983
    Assignee: A. Nattermann & Cie GmbH
    Inventors: Andre Welter, Leon Christiaens, Ferdinand Wirtz-Peitz
  • Patent number: 4418077
    Abstract: Fluorinated aminobutyric acid and diaminobutane compounds in vivo are inhibitors of gamma-aminobutyric acid transaminase and have the following formula: ##STR1## wherein: Y represents hydrogen or fluorine;Z represents --CH.sub.2 NR.sub.1 R.sub.2, where R.sub.1 and R.sub.2 are as defined below, or --COR.sub.3 where R.sub.3 is as defined below;R.sub.a represents hydrogen or R.sub.4, where R.sub.4 is as defined below;R.sub.1 represents hydrogen, C.sub.1 -C.sub.6 alkyl or phenyl-(C.sub.1 -C.sub.4 alkyl);R.sub.2 represents hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl-(C.sub.1 -C.sub.4 alkyl) or, when R.sub.a is hydrogen, R.sub.4, where R.sub.4 is as defined below;R.sub.3 represents hydroxy, or when R.sub.a is hydrogen, C.sub.1 -C.sub.8 alkoxy, --NR.sub.5 R.sub.6, where R.sub.5 and R.sub.6 are as defined below, or an aminocarboxylic acid residue derived by removal of an hydrogen atom from the amino moiety of an L-aminocarboxylic acid;each R.sub.4, independently, represents C.sub.2 -C.sub.
    Type: Grant
    Filed: August 21, 1981
    Date of Patent: November 29, 1983
    Assignee: Merrell Toraude et Compagnie
    Inventors: Philippe Bey, Fritz Gerhart, Michel Jung, Daniel Schirlin
  • Patent number: 4408072
    Abstract: Processes for reacting arylvinyl oxides and alkoxyethylamines to provide novel N-substituted alkoxyethylamines; processes for reacting the novel N-substituted amines with nitriles to provide novel amidoamines; processes for preparing novel diamines from the amidoamines, together with the novel nitrogen-containing products so produced, such products being useful for the preparation of various imidazothiazoles including tetramisole.
    Type: Grant
    Filed: May 8, 1981
    Date of Patent: October 4, 1983
    Assignee: American Cyanamid Company
    Inventor: Sivaraman Raghu
  • Patent number: 4381305
    Abstract: New derivatives of 1,2-ethylenediamine and salts thereof endowed with vascular antispasmodic and antiallergic activity; processes for preparing them, some new intermediates useful in their preparation and pharmaceutical compositions containing them.
    Type: Grant
    Filed: June 5, 1981
    Date of Patent: April 26, 1983
    Assignee: Simes S.p.A.
    Inventors: Cesare Casagrande, Giorgio Ferrari
  • Patent number: 4376783
    Abstract: The novel acylated guanidines, ureas and substituted ureas correspond to the general formula: ##STR1## in which R.sub.1 repesents a substituted or unsubstituted aromatic ring, R.sub.2 represents an alkyl, aryl, or arylalkyl group, R.sub.4 repesents hydrogen or a variously substituted aryl group, X is oxygen or an imine group: NH and Y represent an alkyl aryl alkyloxy or aryloxy group or a hydrogen atom when X represents oxygen or the group COR.sub.3 with R.sub.3 representing an aromatic group, an aryloxy, aralkyloxy or alkyloxy group when X represents the NH group. They are prepared by heating an appropriate compound under reflux with an oxyaminoalcohol, in a suitable solvent. The products are useful as medicaments for the treatment of arterial hypertension, ischemica diseases of the heart and rhythmic disorders of the latter.
    Type: Grant
    Filed: March 4, 1981
    Date of Patent: March 15, 1983
    Assignee: Compagnie Francaise de Sucerie
    Inventors: Jesus Anatol, deceased, by Marie-Francoise Anatol, legal representative, by Andre-Manuel Anatol, legal representative, Jean Berecoechea, Pierre Duchene-Marullaz, Alain Eschalier
  • Patent number: 4370486
    Abstract: Biphenyl compounds of the formula ##STR1## in which the substituents have the meanings given in the description,are obtained by amidomethylation of the corresponding starting compounds and, if appropriate, subsequent sulphonation. The new compounds are used, for example, for the preparation of dyestuff precursors, dyestuffs, plastics and medicaments.
    Type: Grant
    Filed: August 14, 1981
    Date of Patent: January 25, 1983
    Assignee: Bayer Aktiengesellschaft
    Inventor: Horst Harnisch
  • Patent number: 4356322
    Abstract: A series of novel derivatives of phenoxyalkanolamine of the general formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are the same or different and are hydrogen, alkyl of 1 to 2 carbon atoms, methoxy, halogen, nitro, amino or acylamino residues, and the salts thereof, are described, as are methods for their synthesis. The compounds are highly active .beta..sub.1 -specific sympathicomimetics with a partially antagonistic component.
    Type: Grant
    Filed: March 24, 1980
    Date of Patent: October 26, 1982
    Assignee: Veb Arzneimittelwerk Dresden
    Inventors: Dieter Lehmann, Klaus Femmer, Gottfried Faust
  • Patent number: 4355045
    Abstract: The invention relates to topically anti-inflammatory 1-phenylethanolamine derivatives of the general formula I: ##STR1## or acid-addition salts thereof, to pharmaceutical compositions thereof, and to analogy processes for their manufacture. A representative compound is 1-(4-amino-3,5-dichlorophenyl)-2-[1,1-dimethyl-2-(2-phenylacetamido)ethyla mino]ethanol. The derivatives are useful in particular for the treatment of inflammatory diseases or conditions of the skin.
    Type: Grant
    Filed: August 3, 1978
    Date of Patent: October 19, 1982
    Assignee: Imperial Chemical Industries Limited
    Inventors: John Preston, Austin J. Reeve
  • Patent number: 4349690
    Abstract: The present invention provides novel 9-deoxy-9-methylene-6-keto-PGE derivatives which are useful for platelet aggregation inhibition and gastric cyctoprotection.
    Type: Grant
    Filed: April 23, 1981
    Date of Patent: September 14, 1982
    Assignee: The Upjohn Company
    Inventor: Gordon L. Bundy
  • Patent number: 4346101
    Abstract: Benzamide derivative analgesic compounds of the formula ##STR1## wherein P, Q, R.sub.1, R.sub.2, X and Y are as defined in the specification, e.g., 3,4-Dichloro-N-[[8-(dimethylamino)-1,4-dioxaspiro[4.5]dec-8-yl]methyl]benz amide, and their pharmacologically acceptable salts, have analgesic drug properties with a low ratio of analgesic to sedative activity for use as analgesic drugs in mammalian animals, including humans.
    Type: Grant
    Filed: December 8, 1980
    Date of Patent: August 24, 1982
    Assignee: The Upjohn Company
    Inventor: Daniel Lednicer
  • Patent number: 4335136
    Abstract: 4,5-Diaryl-.alpha.-(polyfluoroalkyl)-1H-pyrrole-2-methanamines such as 4,5-bis(4-fluorophenyl)-.alpha..alpha.-bis-(trifluoromethyl)-1H-pyrrole-2- methanamine, useful in treatment of inflammation.
    Type: Grant
    Filed: March 4, 1981
    Date of Patent: June 15, 1982
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Saul C. Cherkofsky
  • Patent number: 4331815
    Abstract: In the manufacture of an N-benzyl-N-isopropyl amide by reaction of N-benzyl-N-isopropylamine with an acid chloride, the amide product is obtained in better purity and yield by employing excess benzylisopropylamine as the acid accepting agent and recovering the amine for re-use by reacting the amine hydrochloride by-product with aqueous sodium hydroxide.
    Type: Grant
    Filed: September 26, 1980
    Date of Patent: May 25, 1982
    Assignee: Gulf Oil Corporation
    Inventor: Roger P. Cahoy
  • Patent number: 4329344
    Abstract: This invention provides compounds, having major tranquilizing activity, of the formula (II): ##STR1## wherein R.sub.1 is a phenyl group optionally substituted by a fluorine, chlorine or bromine atom or an alkyl or alkoxyl group of up to 3 carbon atoms; R.sub.2 is a hydrogen atom or an alkyl group of up to 4 carbon atoms; R.sub.3 is a hydrogen atom or an amino group, a nitro group or a group of the formula NHCOR.sub.4 or NHCO.sub.2 R.sub.4 where R.sub.4 is an alkyl group of up to 4 carbon atoms optionally substituted by one, two or three chlorine atoms or by three fluorine atoms attached to the same carbon atom; n is 0, 1 or 2; and X is a group of the sub-formula (a), (b), (c) or (d): ##STR2## wherein R.sub.5 is an alkyl group of up to 4 carbon atoms; or a N-oxide thereof of the nitrogen atom to which the CHR.sub.2 --(CH.sub.2).sub.n --R.sub.1 moiety is attached; and salts thereof; pharmaceutical compositions containing them; processes for their preparation; and intermediates useful in said process.
    Type: Grant
    Filed: May 12, 1980
    Date of Patent: May 11, 1982
    Assignee: Beecham Group Limited
    Inventor: Michael S. Hadley
  • Patent number: 4313956
    Abstract: Novel, transient prodrug forms of the phenolic dihydroxy sympathomimetic amines have (i) the structural formula (I): ##STR1## wherein X is O, S or NR.sup.5 ; n is 1 or 2; R.sup.1 is the monodehydroxylated residue of a phenolic, nuclear dihydroxy natural sympathetic or sympathomimetic amine when n is 1, and the didehydroxylated residue of a phenolic, nuclear dihydroxy natural sympathetic or sympathomimetic amine when n is 2; R.sup.
    Type: Grant
    Filed: December 28, 1979
    Date of Patent: February 2, 1982
    Assignee: INTERx Research Corp.
    Inventors: Nicholas S. Bodor, Kenneth B. Sloan, Stefano A. Pogany
  • Patent number: 4311706
    Abstract: Novel, transient prodrug forms of dopa and dopamine have (i) the structural formula (I): ##STR1## wherein each R is independently selected from the group consisting of hydrogen, R.sup.3 -CO- and ##STR2## wherein X is O, S or NR.sup.6 ; R.sup.1 is hydrogen or --COOR.sup.8 ; R.sup.2 is hydrogen or OR; R.sup.
    Type: Grant
    Filed: January 22, 1980
    Date of Patent: January 19, 1982
    Assignee: INTERx Research Corporation
    Inventors: Nicholas S. Bodor, Kenneth B. Sloan, Stefano A. Pogany
  • Patent number: 4309425
    Abstract: Sulfonamides, such as N-[N-(2-chloro-5-(trifluoromethyl)phenyl]-N-[2,4-dinitro-6-(trifluoromethy l)phenyl]aminothio]-N,4-dimethylbenzenesulfonamide, are useful for control of arthropod pests of plants and animals and fungus disease of plants.
    Type: Grant
    Filed: April 11, 1980
    Date of Patent: January 5, 1982
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Jiin-Duey Cheng
  • Patent number: 4309424
    Abstract: Novel 4-phenyl-1,3-benzodiazepines, novel intermediates thereof, and methods of preparing same are described. These benzodiazepines are useful as antidepressants, analgetics and anticonvulsants.
    Type: Grant
    Filed: November 5, 1979
    Date of Patent: January 5, 1982
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Lawrence L. Martin, Manfred Worm, Charles A. Crichlow
  • Patent number: 4292445
    Abstract: The present invention relates to novel amido and sulfonamido derivatives of 2-decarboxy-2-amino-methyl-PG-type compounds. These analogs are useful as nasal decongestants, antifertility agents, and as cytoprotection agents.
    Type: Grant
    Filed: April 28, 1980
    Date of Patent: September 29, 1981
    Assignee: The Upjohn Company
    Inventor: Norman A. Nelson
  • Patent number: 4281190
    Abstract: A process for preparing N-[2-(p-hydroxyphenyl)ethyl]-p-chlorobenzamide, a penultimate precursor for bezafibrate, is described.
    Type: Grant
    Filed: August 14, 1980
    Date of Patent: July 28, 1981
    Assignee: Morton-Norwich Products, Inc.
    Inventor: Nicholas Harris
  • Patent number: 4277420
    Abstract: Preparation of novel prochiral olefinic compounds which can be asymmetrically hydrogenated to enantiomers, which are converted to ephedrine and pseudoephedrine by described procedures.
    Type: Grant
    Filed: September 24, 1979
    Date of Patent: July 7, 1981
    Assignee: Monsanto Company
    Inventor: Karl E. Koenig
  • Patent number: 4245099
    Abstract: A 2-acyl-6-aminomethylphenol derivative having the formula (I): ##STR1## wherein R.sup.1 represents a straight chain or branched chain alkyl group of 1 to 6 carbon atoms unsubstituted or substituted with 1 to 3 halogen atoms; a hydrogen atom or a group having the formula (II):--C.sub.n H.sub.2n --R.sup.7 (II)wherein n represents 0 or an integer of 1 to 6; R.sup.7 represents a cycloalkyl group of 3 to 8 carbon atoms unsubstituted or substituted with at least one lower alkyl group; a phenyl group unsubstituted or substituted with at least one lower alkyl group, a halogen atom, a lower alkoxy group or a lower alkylthio group; a lower alkoxy group; a lower alkylthio group; a lower alkylsulfinyl group; a lower alkylsulfonyl group; an N-lower alkylamino group; an N,N-di-lower alkylamino group; or a pyridyl, furyl or thienyl group; R.sup.
    Type: Grant
    Filed: July 24, 1979
    Date of Patent: January 13, 1981
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Itoh, Mitoshi Konno, Takao Tokuhiro, Sadahiko Iguchi, Masaki Hayashi
  • Patent number: 4232014
    Abstract: Aminoalkylindans of the formula ##STR1## wherein A represents an alkylene group having 2 to 5 carbons in a straight chain, R.sub.1 represents a lower alkyl having 1 to 3 carbons or is a lower alkoxy having 1 to 3 carbons, B represents --CH.sub.2 -- or ##STR2## and R.sub.2 represents phenyl or phenyl-lower alkyl and the phenyl group in such substituents is unsubstituted or is substituted with 1 to 3 lower alkoxy groups, and acid addition salts of the amines.The compounds have hypotensive activity.
    Type: Grant
    Filed: January 12, 1979
    Date of Patent: November 4, 1980
    Assignee: Marion Laboratories, Inc.
    Inventors: Ian W. Mathison, William E. Solomons