Additional -c(=x)- Bonded Directly To The Five-membered Hetero Ring (e.g., Pyrrole-3,4-dicarboxylic Acid Esters, Etc.) Patents (Class 548/536)
  • Patent number: 5075452
    Abstract: Compounds of the formula I ##STR1## in which A and X.sup.1 have the meaning given in patent claim 1 can be prepared in a simple manner, in a one-pot process and in high yields.
    Type: Grant
    Filed: December 6, 1989
    Date of Patent: December 24, 1991
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Richard Kirchlechner, Michael Casutt, Arno Basedow
  • Patent number: 5008245
    Abstract: Compounds selected from the group consisting of a compound of the formula ##STR1## and compound of the formula ##STR2## wherein x is 1 or 2,Y is carbobenzoxy or benzoyl, andXR is ##STR3## have use as elastase enzyme inhibitors. Particularly potent are the L-proline diastereomers.Elastase Enzyme inhibitory compositions comprise a carrier and an elastase enzyme inhibiting amount of the compounds of the invention.A method of selectively inhibiting the enzyme elastase in an animal or a human in need of such treatment comprises administering to the animal or human an enzyme elastase inhibiting amount of one of the compounds of the invention or a composition thereof.
    Type: Grant
    Filed: October 27, 1988
    Date of Patent: April 16, 1991
    Assignee: University of Kentucky Research Foundation
    Inventors: George A. Digenis, Bushra J. Agha
  • Patent number: 4985417
    Abstract: Method and formulation useful in treatment of glaucoma in a mammal wherein an effective amount of an active water soluble carbonic anhydrase inhibitor is administered, said inhibitor being a compound having the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is selected from the group consisting of H, NH.sub.2 CH.sub.2 --, --CH(Me)NH.sub.2, --CH(NH.sub.2)CHMe.sub.2, --CH(NH.sub.2)CH.sub.2 CHMe.sub.2, --CH(NH.sub.2)CH(Me)CH.sub.2 Me, 2-pyrrolidinyl residues wherein the R.sup.1 CO-- constitutes an .alpha.-aminoacyl group, N-acetylaminoacyl derivatives and the corresponding dipeptidyl radicals wherein R.sup.1 CO-- is a dipeptidyl residue containing two amino acid residues of the formula where R.sup.1 is --CHR.sup.7 NHCOCHR.sup.8 NH.sub.2, R.sup.6 NHCHR.sup.5 --, ##STR2## and R.sup.6 NHCH.sub.2 CHR.sup.5 --; R.sup.2 is selected from the group consisting of H, alkyl having from 1 to 6 carbon atoms, alkenyl having from 2 to 6 carbon atoms, and cycloalkyl;R.sup.
    Type: Grant
    Filed: May 2, 1989
    Date of Patent: January 15, 1991
    Inventors: Seymour F. Trager, G. Michael Blackburn
  • Patent number: 4977168
    Abstract: N.alpha.-substituted derivatives of N.alpha.-arylsulphonylaminoacyl p-amidinophenylalaninamides, their preparation, their use as medicaments and intermediates for their synthesis.
    Type: Grant
    Filed: January 23, 1987
    Date of Patent: December 11, 1990
    Assignee: Sanofi
    Inventors: Andre Bernat, Denis Delabassee, Daniel Frehel, Jean-Pierre Maffrand, Eric Vallee
  • Patent number: 4945111
    Abstract: Fungicidal N,N'-diacylaminals of the formula ##STR1## in which R.sup.1 is optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl or cycloalkenyl,R.sup.2 and R.sup.3 are hydrogen or various organic radicals, andX is oxygen or sulphur.
    Type: Grant
    Filed: August 11, 1988
    Date of Patent: July 31, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Winfried Lunkenheimer, Dieter Berg, Wilhelm Brandes
  • Patent number: 4933460
    Abstract: Novel 3-(piperidinyl)- and 3-(pyrrolidinyl)-1H-indazoles, intermediates and processes for the preparation thereof, and methods for treating psychoses, treating depression, alleviating pain, treating convulsions and treating hypertension utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: May 13, 1989
    Date of Patent: June 12, 1990
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventor: Joseph T. Strupczewski
  • Patent number: 4923890
    Abstract: The invention relates to selected difluoro compounds of formulae Ia, Ib and Ic (set out hereinafter) which are useful as inhibitors of human leukocyte elastase.
    Type: Grant
    Filed: May 19, 1987
    Date of Patent: May 8, 1990
    Assignee: ICI Americas Inc.
    Inventors: Diane A. Trainor, Mark M. Stein
  • Patent number: 4912128
    Abstract: Novel pyrrolidine-2-(1,3-dicarbonyl) derivatives, a process for their preparation, agents containing them, and their useThe invention relates to pyrrolidine derivatives of the general formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 have the meaning specified in the description, X denotes oxygen, imino or alkylimino,m is 0-5, n is 0-2 and s is 0 or 1, a process for their preparation, agents containing them, and their use.
    Type: Grant
    Filed: April 8, 1988
    Date of Patent: March 27, 1990
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Rainer Henning, Franz Hock, Hansjorg Urbach
  • Patent number: 4912127
    Abstract: The invention rleates to pyrrolidine derivatives of the general formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 have the meaning indicated in the description; X denotes oxygen, imino or N-alkylimino; m is 0-5; n is 0-2 and s is 0 or 1; a process for their preparation, agents containing them, and their use.
    Type: Grant
    Filed: April 8, 1988
    Date of Patent: March 27, 1990
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Rainer Henning, Franz Hock, Hansjorj Urbach
  • Patent number: 4910190
    Abstract: The invention concerns pharmaceutically useful trifluoromethyl ketone substituted di-, tri- and tetra-peptide derivatives of the formulae Ia, Ib, Ic set out hereinafter, and salts thereof, which are inhibitors of human leukocyte elastase. Also described herein are pharmaceutical compositions containing a peptide derivative and processes and intermediates for use in the manufacture of the peptide derivatives.
    Type: Grant
    Filed: January 20, 1987
    Date of Patent: March 20, 1990
    Assignee: ICI Americas Inc.
    Inventors: Scott H. Bergeson, Philip D. Edwards, John A. Schwartz, Andrew Shaw, Mark M. Stein, Diane A. Trainor, Richard A. Wildonger, Donald J. Wolanin
  • Patent number: 4870056
    Abstract: Acylated cyanamide compounds useful for ethanol deterrence of the formula RCONHCN, wherein R is a lipophilic acyl group or is derived from an (N-substituted)-alpha-aminoacyl group.
    Type: Grant
    Filed: October 21, 1987
    Date of Patent: September 26, 1989
    Assignee: Regents of the University of Minnesota
    Inventors: Herbert T. Nagasawa, Chul-Hoon Kwon
  • Patent number: 4864017
    Abstract: The present invention provides novel renin-inhibiting peptides of the formula X-A.sub.6 -B.sub.7 -C.sub.8 -D.sub.9 -E.sub.10 -F.sub.11 -G.sub.12 -H.sub.13 - I.sub.14 -Z, wherein the E.sub.10 -F.sub.11 moiety is a dihydroxyethylene isostere, X and Z are terminal groups, and the remaining variables are absent or are amino acid residues. Such inhibitors are useful for the control of hypertension.
    Type: Grant
    Filed: August 23, 1988
    Date of Patent: September 5, 1989
    Assignee: The Upjohn Company
    Inventor: Suvit Thaisrivongs
  • Patent number: 4785109
    Abstract: These is described a process for producing sulfonylureas of the formula ##STR1## wherein G is an unsubstituted or substituted furanyl, thienyl, pyrrolyl, pyridinyl or phenyl radical,X is alkyl, haloalkyl, alkoxy, alkylthio, halogen, haloalkoxy, alkylamino or dialkylamino,Y is alkyl, alkoxy or haloalkoxy,Z is a nitrogen atom or the methyne group --CH.dbd..This novel process comprises reacting a sulfonamide of the formulaG--SO.sub.2 --NH.sub.2,in the presence of a base, with a chloroformic acid ester of the formulaCl--CO--Q--T,or a sulfonyl chloride of the formulaG--SO.sub.2 Cl,in the presence of a base, with a urethane of the formulaH.sub.2 N--CO--Q--T;and converting the formed carbamate of the formulaG--SO.sub.2 --NH--CO--Q--Tby reaction with an amine of the formula ##STR2## into the sulfonylurea of the above formula. There are also described novel sulfonylcarbamates of the above formula as intermediates.
    Type: Grant
    Filed: January 30, 1987
    Date of Patent: November 15, 1988
    Assignee: Ciba-Geigy Corporation
    Inventors: Willy Meyer, Werner Fory, Werner Topfl
  • Patent number: 4746350
    Abstract: The invention concerns novel compounds of the formula I ##STR1## wherein: Y is selected from phenyl, furyl, thienyl and pyrrolyl rings (each optionally substituted by group X), optionally branched alkylene or alkylenethio(oxy)alkylene;X which may be the same or different are independently selected from halogen, nitro, alkyl, substituted alkyl, hydroxy, alkoxy, carboxy, alkoxycarbonyl, alkylthio, sulfamoyl, substituted sulfamoyl, amino, substituted amino and alkanoyl;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 and alkynyl;R.sup.3 is selected from alkyl; andR.sup.4 is selected from hydrogen, alkyl, and alkoxycarbonyl.
    Type: Grant
    Filed: April 14, 1986
    Date of Patent: May 24, 1988
    Assignee: Imperial Chemical Industries PLC
    Inventor: Keith G. Watson
  • Patent number: 4695580
    Abstract: Novel phenylserine derivatives of the formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof, pharmaceutical compositions, and a process for preparing the compounds are disclosed. The phenylserine derivatives and pharmaceutically acceptable acid addition salts are capable of inhibiting the biosynthesis of leucotrienes and/or antagonistic activity against SRS-A and hence are useful for prophylaxis and treatment of various allergic diseases (e.g. bronchial asthma, allergic nasitis, urticaria), ischemic heart diseases, ischemic encephalopathy, inflammation, or the like.
    Type: Grant
    Filed: December 19, 1984
    Date of Patent: September 22, 1987
    Assignee: Sumitomo Pharmaceuticals Company, Ltd.
    Inventors: Naohito Ohashi, Shoji Nagata, Masashi Nakatsuka, Kikuo Ishizumi, Junki Katsube, Shunji Aono, Teruo Sakurama
  • Patent number: 4691050
    Abstract: The present invention provides a process for the preparation of aromatic dicarboxylic acids by the carbonylation of aromatic diiodides. The aromatic diiodides are reacted with carbon monoxide in the presence of a soluble rhodium catalyst in a hydrocarbon acid reaction medium to prepare the aromatic dicarboxylic acids.
    Type: Grant
    Filed: May 23, 1986
    Date of Patent: September 1, 1987
    Assignee: Eastman Kodak Company
    Inventors: Carl M. Lentz, James R. Overton, David D. Cornell
  • Patent number: 4645844
    Abstract: Novel and known functionally substituted phenoxyalkyl-, thiophenoxyalkyl- and pyridyloxyalkylsilanes are prepared by reacting substantially equimolar amounts of an alkali- or alkaline earth metal phenoxide, thiophenoxide or pyridyloxide with a haloalkylsilane under anhydrous conditions using a dipolar, aprotic solvent in combination with a liquid hydrocarbon.
    Type: Grant
    Filed: July 20, 1983
    Date of Patent: February 24, 1987
    Assignee: M&T Chemicals Inc.
    Inventors: Abe Berger, Irwin B. Silverstein
  • Patent number: 4626545
    Abstract: Compounds of the formula ##STR1## and their use as angiotensin converting enzyme inhibitors and antihypertensives are disclosed.
    Type: Grant
    Filed: August 27, 1984
    Date of Patent: December 2, 1986
    Assignee: Merck & Co., Inc.
    Inventor: David Taub
  • Patent number: 4596819
    Abstract: Modified oxytocin-vasopressin di- or tri-peptides wherein an amide group is replaced by a group selected from ##STR1## --CH.sub.2 NH--, --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 SO--, --CH.sub.2 SO.sub.2 --, --CH.sub.2 CH.sub.2 -- and --CH.dbd.CH-- are described as well as methods for their manufacture, pharmaceutical compositions and methods for treatment, especially of cognitive disorders, depression, morphine dependency and parkinsonism by adjunctive therapy.
    Type: Grant
    Filed: January 23, 1984
    Date of Patent: June 24, 1986
    Assignee: Warner-Lambert Company
    Inventors: Ernest D. Nicolaides, Francis J. Tinney, James S. Kaltenbronn, Dana E. DeJohn, Elizabeth A. Lunney, W. Howard Roark, Joseph T. Repine
  • Patent number: 4551539
    Abstract: N-substituted 2,5-dimethylpyrroles and a method for their preparation. The method requires the reaction of a 2,5-hexadione such as acetonylacetone with a urethane or a phosphoroamidate. The reaction is carried out at elevated temperatures, preferably in a water-immiscible solvent.
    Type: Grant
    Filed: October 17, 1984
    Date of Patent: November 5, 1985
    Assignee: Borg-Warner Chemicals, Inc.
    Inventors: Ingenuin Hechenbleikner, William P. Enlow
  • Patent number: 4551540
    Abstract: N-substituted 2,5-dimethylpyrroles and a method for their preparation. The method requires the reaction of a 2,5-hexadione such as acetonylacetone with a urethane or a phosphoroamidate. The reaction is carried out at elevated temperatures, preferably in a water-immiscible solvent.
    Type: Grant
    Filed: October 17, 1984
    Date of Patent: November 5, 1985
    Assignee: Borg-Warner Chemicals, Inc.
    Inventors: Ingenuin Hechenbleikner, William P. Enlow
  • Patent number: 4511576
    Abstract: Certain pyrrolecarboxylic and pyrroleacetic acid derivatives substituted on the pyrrole ring with thioether groups, acyl groups, phenyl, substituted phenyl, phenoxy, substituted phenoxy, benzyl or halo and optionally substituted on the pyrrole nitrogen with alkyl, and the pharmaceutically acceptable salts thereof, are useful in lowering the blood glucose levels of hyperglycemic animals.
    Type: Grant
    Filed: August 10, 1982
    Date of Patent: April 16, 1985
    Assignee: Pfizer Inc.
    Inventor: Gerald F. Holland
  • Patent number: 4511390
    Abstract: Aralkylcarbamoyl peptide alcohols of the formula ##STR1## selectively stimulate nitrate and ammonium ion uptake by plants.
    Type: Grant
    Filed: June 10, 1983
    Date of Patent: April 16, 1985
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: James C. Kauer
  • Patent number: 4499102
    Abstract: Thiazolidine and pyrrolidine compounds which have the general formula ##STR1## and salts thereof for preventing or relieving diabetic complications and for reducing blood pressure, the processes for their preparation, and the compositions comprising them and pharmaceutically acceptable excipient(s).
    Type: Grant
    Filed: December 10, 1981
    Date of Patent: February 12, 1985
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Masayuki Oya, Tadashi Iso
  • Patent number: 4477635
    Abstract: Polymeric and copolymeric aminotriarylmethane dyes having polyester, polyethyleneimine, or polyurethane backbones, and a process for their preparation, are disclosed. The novel dyes are highly colored and resistant to leaching by solvents.
    Type: Grant
    Filed: January 4, 1982
    Date of Patent: October 16, 1984
    Assignee: Minnesota Mining and Manufacturing Company
    Inventor: Smarajit Mitra
  • Patent number: 4461642
    Abstract: The invention herein pertains to novel 2,5-bis-(perfluoroalkyl)-3,4-pyrroledicarboxylates and a method for their preparation. The novel pyrroles have been found to have utility as pre- and postemergent herbicides.
    Type: Grant
    Filed: March 8, 1982
    Date of Patent: July 24, 1984
    Assignee: Monsanto Company
    Inventors: Robert K. Howe, Len F. Lee
  • Patent number: 4417072
    Abstract: Substituted hydroquinone compounds of the formula ##STR1## wherein R.sub.1 to R.sub.4 are hydrogen or alkyl and Z is an aromatic ring or a group of the formula --X--Y--X--, wherein X is an aromatic ring and Y is an electron withdrawing group, are incorporated as developers into photographic materials. These materials are suitable for activation processings.
    Type: Grant
    Filed: September 29, 1981
    Date of Patent: November 22, 1983
    Assignee: Ciba-Geigy AG
    Inventors: Stephen R. Postle, Patrick D. P. Thomas, Brian R. D. Whitear
  • Patent number: 4388468
    Abstract: A process for the preparation of certain 4-alkyl substituted 5-aroyl-pyrrole alkanoic acids useful as intermediates for anti-inflammatory agents.
    Type: Grant
    Filed: August 18, 1981
    Date of Patent: June 14, 1983
    Assignee: Ethyl Corporation
    Inventor: Michael J. Dagani
  • Patent number: 4383112
    Abstract: Chiral Schiff bases according to the general formula: ##STR1## and transition metal complexes thereof, wherein C.sup.* is an asymmetric carbon atom, R.sup.1 and R.sup.2, which may be the same or different are alkyl, aralkyl, aryl or alkaryl, R.sup.3 is hydrogen, alkyl, aralkyl, aryl or alkaryl, R.sup.4 and R.sup.5, which may be the same or different, are hydrogen or lower alkyl or, where n is 1, may with the cyclic ring to which CR.sup.4 R.sup.
    Type: Grant
    Filed: July 8, 1980
    Date of Patent: May 10, 1983
    Assignee: Imperial Chemical Industries Limited
    Inventors: Dale A. Laidler, David J. Milner