Patents Examined by Bernard I. Dentz
  • Patent number: 5008286
    Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.
    Type: Grant
    Filed: August 28, 1989
    Date of Patent: April 16, 1991
    Assignee: Burroughs Wellcome Co.
    Inventor: Kenneth W. Bair
  • Patent number: 5008273
    Abstract: Amino acid derivatives of general formula ##STR1## (the definitions of the various symbols being explained in the specification) are suitable for treating high blood pressure and for cardioprotection. The new compounds are prepared and used in the usual way.
    Type: Grant
    Filed: September 6, 1989
    Date of Patent: April 16, 1991
    Assignee: Boehringer Ingelheim GmbH
    Inventors: Gerd Schnorrenberg, Otto Roos, Walter Losel, Ingrid Wiedemann, Wolfram Gaida, Wolfgang Hoefke, Dietrich Arndts, Ilse Streller
  • Patent number: 5008409
    Abstract: A process for preparing a compound of Formula (I): ##STR1## wherein R is phenyl or phenyl substituted with hydroxy, lower alkoxy, halogen or lower alkyl; Y is unsubstituted or substituted methylene, ethylene, vinylene or oxygen; m is 0 or 1; n is 0, 1 or 2; and q is 1, 2, 3 or 4; with the limitation that when m is 0, n is not 0, and when m is 1, n is not 2, which process comprises:(a) reacting an aldehyde of Formula (II); ##STR2## wherein R, Y, m and n are as defined above, under reaction conditions for the Wittig Reaction with a ylide of Formula (III):(R.sup.1).sub.3 P.dbd.CH(CH.sub.2).sub.q COOM (III)wherein R.sup.1 is C.sub.1 -C.sub.
    Type: Grant
    Filed: December 7, 1989
    Date of Patent: April 16, 1991
    Assignee: Shionogi & Co., Ltd.
    Inventors: Masayuki Narisada, Mitsuaki Ohtani, Fumihiko Watanabe, Kyozo Kawata
  • Patent number: 5006533
    Abstract: 3-Bromo-2,6-dimethoxybenzamides useful as neuroleptic agents are described.
    Type: Grant
    Filed: November 22, 1989
    Date of Patent: April 9, 1991
    Assignee: Boehringer Ingelheim GmbH
    Inventors: Rainer Sobotta, Adolf Langbein, Herbert Merz, Rudolf Bauer, Joachim Mierau
  • Patent number: 5006532
    Abstract: 3-Hydroxyazabenzo[b]thiophene derivatives having optionally 2-aryl, 2-aralkyl, 2-alkyl or 2-alkenyl substituents were prepared by, among other methods, ring closure of an appropriately substituted benzylthio-alkoxycarbonyl-pyridine. These compounds are found to be useful in the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases such as psoriasis and atopic eczema, cardiovascular disorders, inflammatory diseases and other leukotriene mediated diseases.
    Type: Grant
    Filed: December 8, 1989
    Date of Patent: April 9, 1991
    Assignee: Merck & Co. Inc., Inc.
    Inventors: Robert K. Baker, Arsenio A. Pessolano, Kathleen M. Rupprecht, Philippe L. Durette
  • Patent number: 5006527
    Abstract: Novel N-(4-piperindyl)bicyclic condensed 2-imidazolamine derivatives and their pharmaceutically acceptable acid addition salts having anti-histaminic properties, compositions containing the same, and methods of treating allergic diseases in warm-blooded animals.
    Type: Grant
    Filed: December 4, 1989
    Date of Patent: April 9, 1991
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frans E. Janssens, Joseph L. G. Torremans, Gasto S. M. Diels
  • Patent number: 5004748
    Abstract: The invention relates to substituted pyridine-2,4-dicarboxylic acid derivatives of the formula I ##STR1## in which R.sup.1 and R.sup.2 have the meanings given. The invention also relates to a process for the preparation of the abovementioned compounds and to their use as medicaments, in particular as fibrosuppressants and immunosuppressants.
    Type: Grant
    Filed: March 4, 1988
    Date of Patent: April 2, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ekkehard Baader, Martin Bickel, Dietrich Brocks, Volkmar Gunzler, Stephan Henke, Hartmut Hanauske-Abel
  • Patent number: 5001238
    Abstract: This invention relates to the process for the preparation of certain 2-phenylalkylthio- and phenylalkylsulfinyl-imidazo[4,5-c]pyridines useful for the treatment of osteoporosis.
    Type: Grant
    Filed: June 19, 1990
    Date of Patent: March 19, 1991
    Assignee: American Home Products Corporation
    Inventors: Chia-Cheng Shaw, Razzak Noureldin, Gregory Gavin
  • Patent number: 4999359
    Abstract: A compound, or a solvate or salt thereof, of formula I: ##STR1## in which: R.CO-- is an acyl group containing a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic group;R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4-12 cycloalkylalkyl groups or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group, optionally substituted with a hetero-atom;R.sub.3 is hydrogen, C.sub.1-6 alkyl, or phenyl or R.sub.3 together with R.sub.1 form a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- group;R.sub.4 is C.sub.1-6 alkyl, or phenyl;R.sub.5 is hydrogen or together with R.sub.4 forms a --(CH.sub.2).sub.n -- group in which n=1, 2 or 3; and `Het` is an optionally substituted single or fused ring heterocyclic group, containing from 5 to 12 ring atoms and comprising up to four hetero-atoms in the or each ring selected from oxygen, nitrogen and sulphur, with the proviso that when, simultaneously, R.sub.
    Type: Grant
    Filed: March 14, 1989
    Date of Patent: March 12, 1991
    Assignee: Dr. Lo Zambeletti S.p.A.
    Inventors: Vittorio Vecchietti, Giuseppe Giardina
  • Patent number: 4999426
    Abstract: Compounds of formula I ##STR1## in which R is H, or an aliphatic or aromatic radical, R.sup.1 is alkyl, R.sup.2 is alkyl, alkoxy, aryl, aryloxy, aralkyl, alkaryl, aralkyloxy, alkaryloxy, alkaralkyl or alkaralkyloxy, and one of R.sup.1 and R.sup.2 is H and the other has the meaning given above. These compounds are intermediates for the preparation of herbicidal sulfonylureas.
    Type: Grant
    Filed: July 26, 1989
    Date of Patent: March 12, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Adrian Waldner, Willy Meyer
  • Patent number: 4999350
    Abstract: The present invention relates to (RS)-2-(2,3-dihydro-5-hydroxy-4,6,7-trimethylbenzofuranyl) acetic acids and 2-(2,3-dihydro-5-acyloxy-4,6,7-trimethylbenzofuranyl) acetic acids and esters thereof, the process for producing them and their relevant therapeutical use as mucoregulators and antiischemic agents.
    Type: Grant
    Filed: April 13, 1989
    Date of Patent: March 12, 1991
    Assignee: Biomedica Foscama Industria Chimico-Farmaceutica S.p.A.
    Inventors: Mario Brufani, Stefano Ceccarelli, Patrizia Giannetti, Agnese Paesano, Romolo Scuri, Sergio Zanarella
  • Patent number: 4997945
    Abstract: The carbamate salt of 2-(2'-thienyl)-alkylamines and particularly the ethylamine and its method of synthesis are disclosed. The carbamate salt of 2-(2'-thienyl)ethylamine is a stable, easily transportable crystalline material that can be converted to 2-(2'-thienyl)ethylamine, a useful intermediate in the synthesis of 5[(2-chlorophenyl)methyl]-4,5,6,7-tetrahydrothieno-[3,2-c]pyridine hydrochloride, also known as ticlopidine hydrochloride. The synthesis is carried out by reacting an amine of formula (I): ##STR1## with CO.sub.
    Type: Grant
    Filed: January 25, 1990
    Date of Patent: March 5, 1991
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Hiralal N. Khatri
  • Patent number: 4996213
    Abstract: Compounds represented by the general formula ##STR1## in which R.sub.1 and R.sub.2 are independently selected from hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl or benzyl, or R.sub.1 and R.sub.2 may form together with the nitrogen atom to which they are attached a C.sub.4 -C.sub.8 saturated heterocycle, R.sub.3 and R.sub.4 are independently selected from hydrogen or C hd 1-C.sub.6 alkyl, R.sub.5 is selected from hydrogen or halogen, or C.sub.1 -C.sub.4 alkyl, C.sub.1 -C hd 4 alkoxy, nitro or trifluoromethyl, n is 1, 2 or 3, and one of the symbols A, B, C or D represents N and the others represent CH, as well as the N-oxids and the the pharmaceutically acceptable acid addition salts and their salts with bases. The compounds have nervous system affecting properties.
    Type: Grant
    Filed: June 6, 1989
    Date of Patent: February 26, 1991
    Assignee: SANOFI
    Inventors: Etienne Mendes, Jean-Claude Vernieres, Jacques Simiaud, Peter E. Keane
  • Patent number: 4994473
    Abstract: Insecticides of the general formula ##STR1## wherein R.sub.1 is an optionally substituted 5- to 10-member heterocyclic moiety; R.sub.2 is an optionally substituted alkyl, cycloalkyl or alkenyl moiety; X is oxygen, sulfur or --NH--; and R.sub.3 is: (a) an optionally substituted 3-phenoxyphenalkyl, 3-phenoxypyridylalkyl, 3-(pyridyloxy)phenalkyl, 3-phenylaminophenoalkyl, 3-benzylphenalkyl or 3-benzyloxyphenalkyl moiety; (b) a benzylfuranylmethyl moiety; (c) a 3- or 4-substituted benzyl or tetrafluorobenzyl moiety; (d) 4-phenoxy-2-butyn-2-yl; or (e) 2-methyl-3-phenylbenzyl.
    Type: Grant
    Filed: October 31, 1988
    Date of Patent: February 19, 1991
    Assignee: ICI Americas Inc.
    Inventor: Michael D. Broadhurst
  • Patent number: 4994453
    Abstract: The disclosure deals with pyrazolopyridine compounds of the formula ##STR1## wherein the variables are defined in the specification. The compounds are useful in the treatment of bronchial asthma, immunosuppression, diabetes, etc.
    Type: Grant
    Filed: September 15, 1989
    Date of Patent: February 19, 1991
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Youichi Shiokawa, Atsushi Akahane, Hirohito Katayama, Takafumi Mitsunaga
  • Patent number: 4992447
    Abstract: Compounds of the formula ##STR1## where R.sup.1 is lower alkyl, R.sup.2 is chlorophenyl, Y is alkylene, X is heterocyclic and Z is a fused ring are useful as antiinflammatory and antiallergy agents.
    Type: Grant
    Filed: May 8, 1989
    Date of Patent: February 12, 1991
    Assignee: Pfizer Inc.
    Inventors: Kelvin Cooper, Peter E. Cross, Michael J. Fray, Kenneth Richardson
  • Patent number: 4992568
    Abstract: o-Iodoaryl allyl ethers undergo facile palladium-promoted cyclization to benzofurans.
    Type: Grant
    Filed: August 25, 1989
    Date of Patent: February 12, 1991
    Assignee: Iowa State University Research Foundation, Inc.
    Inventor: Richard C. Larock
  • Patent number: 4990518
    Abstract: This invention relates to substituted imidazopyridine derivatives having the follow formula ##STR1## or a pharmaceutically acceptable acid addition salt thereof: wherein the variables are described in the specification are useful in the treatment of diseases or disorders mediated by platelet-activating factor. This invention also relates to pharmaceutical compositions of such substituted imidazopyridines.
    Type: Grant
    Filed: September 13, 1989
    Date of Patent: February 5, 1991
    Assignee: G. D. Searle & Co.
    Inventors: Ish K. Khanna, Richard M. Weier
  • Patent number: 4990517
    Abstract: 7-(1-Pyrrolidinyl)-3-quinolone- and -naphthyridonecarboxylic acid derivatives as antibacterial agents and feed additives, of the formula ##STR1## in which X.sup.1 is halogen,X.sup.2 is hydrogen, halogen, amino or other radical,R.sup.1 is alkyl, cycloalkyl, optionally substituted phenyl or other radical,R.sup.2 is hydrogen, alkyl or a dioxolylmethyl radical,R.sup.3 is ##STR2## A is N, CH, C-halogen, or the like, or forms a bridge with R.sup.1, and addition products thereof.
    Type: Grant
    Filed: June 30, 1989
    Date of Patent: February 5, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Uwe Petersen, Thomas Schenke, Andreas Krebs, Klaus Grohe, Michael Schriewer, Ingo Haller, Karl G. Metzger, Rainer Endermann, Hans-Joachim Zeiler
  • Patent number: 4990506
    Abstract: A compound which is a 3-(acylaminomethyl)imidazo[1,2-a]pyridine derivative of formula (I) ##STR1## in which R.sub.1 denotes hydrogen; linear or branched C.sub.1 -C.sub.4 alkyl; or benzyl;R.sub.2 denotes linear or branched C.sub.1 -C.sub.6 alkyl; cyclohexyl; trichloromethyl; 1-propenyl; allyl; phenyl; 4-chlorophenyl; or benzyl:or R.sub.1 and R.sub.2 together denote a C.sub.3 -C.sub.5 aliphatic chain:X denotes halogen; C.sub.1 -C.sub.3 alkyl; methylthio; trifluoromethyl; optionally esterified carboxy of formula --COOR in which R denotes hydrogen or C.sub.1 -C.sub.6 alkyl; cyano; optionally mono- or dialkylated aminocarbonyl of formula --CONR.sub.3 R.sub.4 in which R.sub.3 and R.sub.4 independently denote hydrogen or C.sub.1 -C.sub.4 alkyl or together denote a chain of formula --(CH.sub.2).sub.2 --Z--(CH.sub.2).sub.2 -- in which Z denotes a direct bond, oxygen, sulphur, or a divalent group of formula --CH.sub.2 --, --NH-- or --N(C.sub.1 -C.sub.4 alkyl)--; alkylamino of formula NHR.sub.5 in which R.sub.
    Type: Grant
    Filed: October 24, 1989
    Date of Patent: February 5, 1991
    Assignee: Synthelabo
    Inventors: Pascal George, Claudie Giron, Jacques Froissant