Additional -c(=x)- Bonded Directly To The Five-membered Hetero Ring (e.g., Pyrrole-3,4-dicarboxylic Acid Esters, Etc.) Patents (Class 548/536)
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Patent number: 5075452Abstract: 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: GrantFiled: December 6, 1989Date of Patent: December 24, 1991Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Richard Kirchlechner, Michael Casutt, Arno Basedow
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Patent number: 5008245Abstract: 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: GrantFiled: October 27, 1988Date of Patent: April 16, 1991Assignee: University of Kentucky Research FoundationInventors: George A. Digenis, Bushra J. Agha
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Patent number: 4985417Abstract: 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: GrantFiled: May 2, 1989Date of Patent: January 15, 1991Inventors: Seymour F. Trager, G. Michael Blackburn
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Patent number: 4977168Abstract: N.alpha.-substituted derivatives of N.alpha.-arylsulphonylaminoacyl p-amidinophenylalaninamides, their preparation, their use as medicaments and intermediates for their synthesis.Type: GrantFiled: January 23, 1987Date of Patent: December 11, 1990Assignee: SanofiInventors: Andre Bernat, Denis Delabassee, Daniel Frehel, Jean-Pierre Maffrand, Eric Vallee
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Patent number: 4945111Abstract: 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: GrantFiled: August 11, 1988Date of Patent: July 31, 1990Assignee: Bayer AktiengesellschaftInventors: Winfried Lunkenheimer, Dieter Berg, Wilhelm Brandes
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Patent number: 4933460Abstract: 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: GrantFiled: May 13, 1989Date of Patent: June 12, 1990Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventor: Joseph T. Strupczewski
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Patent number: 4923890Abstract: 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: GrantFiled: May 19, 1987Date of Patent: May 8, 1990Assignee: ICI Americas Inc.Inventors: Diane A. Trainor, Mark M. Stein
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Patent number: 4912128Abstract: 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: GrantFiled: April 8, 1988Date of Patent: March 27, 1990Assignee: Hoechst AktiengesellschaftInventors: Rainer Henning, Franz Hock, Hansjorg Urbach
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Patent number: 4912127Abstract: 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: GrantFiled: April 8, 1988Date of Patent: March 27, 1990Assignee: Hoechst AktiengesellschaftInventors: Rainer Henning, Franz Hock, Hansjorj Urbach
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Patent number: 4910190Abstract: 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: GrantFiled: January 20, 1987Date of Patent: March 20, 1990Assignee: 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
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Patent number: 4870056Abstract: 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: GrantFiled: October 21, 1987Date of Patent: September 26, 1989Assignee: Regents of the University of MinnesotaInventors: Herbert T. Nagasawa, Chul-Hoon Kwon
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Patent number: 4864017Abstract: 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: GrantFiled: August 23, 1988Date of Patent: September 5, 1989Assignee: The Upjohn CompanyInventor: Suvit Thaisrivongs
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Patent number: 4785109Abstract: 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: GrantFiled: January 30, 1987Date of Patent: November 15, 1988Assignee: Ciba-Geigy CorporationInventors: Willy Meyer, Werner Fory, Werner Topfl
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Patent number: 4746350Abstract: 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: GrantFiled: April 14, 1986Date of Patent: May 24, 1988Assignee: Imperial Chemical Industries PLCInventor: Keith G. Watson
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Patent number: 4695580Abstract: 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: GrantFiled: December 19, 1984Date of Patent: September 22, 1987Assignee: Sumitomo Pharmaceuticals Company, Ltd.Inventors: Naohito Ohashi, Shoji Nagata, Masashi Nakatsuka, Kikuo Ishizumi, Junki Katsube, Shunji Aono, Teruo Sakurama
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Patent number: 4691050Abstract: 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: GrantFiled: May 23, 1986Date of Patent: September 1, 1987Assignee: Eastman Kodak CompanyInventors: Carl M. Lentz, James R. Overton, David D. Cornell
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Patent number: 4645844Abstract: 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: GrantFiled: July 20, 1983Date of Patent: February 24, 1987Assignee: M&T Chemicals Inc.Inventors: Abe Berger, Irwin B. Silverstein
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Patent number: 4626545Abstract: Compounds of the formula ##STR1## and their use as angiotensin converting enzyme inhibitors and antihypertensives are disclosed.Type: GrantFiled: August 27, 1984Date of Patent: December 2, 1986Assignee: Merck & Co., Inc.Inventor: David Taub
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Patent number: 4596819Abstract: 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: GrantFiled: January 23, 1984Date of Patent: June 24, 1986Assignee: Warner-Lambert CompanyInventors: Ernest D. Nicolaides, Francis J. Tinney, James S. Kaltenbronn, Dana E. DeJohn, Elizabeth A. Lunney, W. Howard Roark, Joseph T. Repine
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Patent number: 4551539Abstract: 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: GrantFiled: October 17, 1984Date of Patent: November 5, 1985Assignee: Borg-Warner Chemicals, Inc.Inventors: Ingenuin Hechenbleikner, William P. Enlow
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Patent number: 4551540Abstract: 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: GrantFiled: October 17, 1984Date of Patent: November 5, 1985Assignee: Borg-Warner Chemicals, Inc.Inventors: Ingenuin Hechenbleikner, William P. Enlow
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Patent number: 4511576Abstract: 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: GrantFiled: August 10, 1982Date of Patent: April 16, 1985Assignee: Pfizer Inc.Inventor: Gerald F. Holland
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Patent number: 4511390Abstract: Aralkylcarbamoyl peptide alcohols of the formula ##STR1## selectively stimulate nitrate and ammonium ion uptake by plants.Type: GrantFiled: June 10, 1983Date of Patent: April 16, 1985Assignee: E. I. Du Pont de Nemours and CompanyInventor: James C. Kauer
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Patent number: 4499102Abstract: 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: GrantFiled: December 10, 1981Date of Patent: February 12, 1985Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Masayuki Oya, Tadashi Iso
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Patent number: 4477635Abstract: 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: GrantFiled: January 4, 1982Date of Patent: October 16, 1984Assignee: Minnesota Mining and Manufacturing CompanyInventor: Smarajit Mitra
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Patent number: 4461642Abstract: 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: GrantFiled: March 8, 1982Date of Patent: July 24, 1984Assignee: Monsanto CompanyInventors: Robert K. Howe, Len F. Lee
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Patent number: 4417072Abstract: 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: GrantFiled: September 29, 1981Date of Patent: November 22, 1983Assignee: Ciba-Geigy AGInventors: Stephen R. Postle, Patrick D. P. Thomas, Brian R. D. Whitear
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Patent number: 4388468Abstract: A process for the preparation of certain 4-alkyl substituted 5-aroyl-pyrrole alkanoic acids useful as intermediates for anti-inflammatory agents.Type: GrantFiled: August 18, 1981Date of Patent: June 14, 1983Assignee: Ethyl CorporationInventor: Michael J. Dagani
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Patent number: 4383112Abstract: 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: GrantFiled: July 8, 1980Date of Patent: May 10, 1983Assignee: Imperial Chemical Industries LimitedInventors: Dale A. Laidler, David J. Milner