Double Bonded Divalent Chalcogen Containing Patents (Class 544/130)
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Patent number: 4812451Abstract: Novel 1-[(aminoalkyl and aminoalkylamino)carbonyl and thiocarbonyl-.alpha.,.alpha.-diaryl-pyrrolidine, piperidine and homopiperidineacetamides and acetonitriles having the formula: ##STR1## wherein; n is zero, one or two;X is oxygen or sulfur;Z is ##STR2## 10 or --(CH.sub.2); p is 0 to 5 inclusive with the proviso that when Z is ##STR3## p is at least one; Y is aminocarbonyl or cyano;Ar.sup.1 and Ar.sup.2 are 2, 3 or 4-pyrido, phenyl or substituted phenyl;R is hydrogen or loweralkyl;R.sup.1, R.sup.2 and R.sup.3 are hydrogen, cycloalkyl, loweralkyl, phenyl, substituted phenyl, phenylloweralkyl, and R.sup.2 and R.sup.3 taken with the adjacent nitrogen may form a heterocyclic residue, and diastereoisomers when possible and pharmaceutical salts; and the method and pharmaceutical compositions for treating cardiac arrhythmias therewith are disclosed.Type: GrantFiled: March 27, 1986Date of Patent: March 14, 1989Assignee: A. H. Robins Company, IncorporatedInventors: James R. Shanklin, Jr., James M. Wilkinson, II
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Patent number: 4812452Abstract: Novel 1-[(aminoalkyl and aminoalkylamino)carbonyl and thiocarbonyl]-.alpha.,.alpha.-diaryl-pyrrolidine, piperidine and homopiperidineacetamides and acetonitriles having the formula: ##STR1## wherein; n is zero, one or two;X is oxygen or sulfur;Z is ##STR2## or --(CH.sub.2); p is 0 to 5 inclusive with the proviso that when Z is ##STR3## p is at least one; Y is aminocarbonyl or cyano;Ar.sup.1 and Ar.sup.2 are 2, 3 or 4-pyrido, phenyl or substituted phenyl;R is hydrogen or loweralkyl;R.sup.1, R.sup.2 and R.sup.3 are hydrogen, cycloalkyl, loweralkyl, phenyl, substituted phenyl, phenylloweralkyl, and R.sup.2 and R.sup.3 taken with the adjacent nitrogen may form a heterocyclic residue, and diastereoisomers when possible and pharmaceutical salts; and the method and pharmaceutical compositions for treating cardiac arrhythmias therewith are disclosed.Type: GrantFiled: March 27, 1986Date of Patent: March 14, 1989Assignee: A. H. Robins Company, IncorporatedInventors: James R. Shanklin, Jr., James M. Wilkinson, II
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Patent number: 4810703Abstract: Novel 1-[(aminoalkyl and aminoalkylamino)carbonyl and thiocarbonyl-.alpha.,.alpha.-diaryl-pyrrolidine, piperidine and homopiperidineacetamides and acetonitriles having the formula: ##STR1## wherein; n is zero, one or two;X is oxygen or sulfur;Z is ##STR2## or --(CH.sub.2); p is 0 to 5 inclusive with the proviso that when Z is ##STR3## p is at least one; Y is aminocarbonyl or cyano;Ar.sup.1 and Ar.sup.2 are 2, 3 or 4-pyrido, phenyl or substituted phenyl;R is hydrogen or loweralkyl;R.sup.1, R.sup.2 and R.sup.3 are hydrogen, cycloalkyl, loweralkyl, phenyl, substituted phenyl, phenylloweralkyl, and R.sup.2 and R.sup.3 taken with the adjacent nitrogen may form a heterocyclic residue, and diastereoisomers when possible and pharmaceutical salts; and the method and pharmaceutical compositions for treating cardiac arrhythmias therewith are disclosed.Type: GrantFiled: July 7, 1986Date of Patent: March 7, 1989Assignee: A. H. Robins Company, IncorporatedInventors: James R. Shanklin, Jr., James M. Wilkinson, II
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Patent number: 4808727Abstract: The pharmaceutically acceptable salts corresponding to the imidazolium hydrogen carbonates of the formula ##STR1## wherein the symbol Q is arylene or heteroarylene, the group --NR.sup.1 R.sup.2 is a basic amino group, R.sup.3 is hydrogen, lower alkyl, lower hydroxyalkyl, lower alkoxyalkyl, lower haloalkyl, lower alkylthio, lower alkoxy or the group --(A).sub.n --Ra, R.sup.4 is a saturated or partially unsaturated lower hydrocarbon group, a basic amino group or the group --N.dbd.CRc--Rb, --CHRcRd, --NH--CHRcRd, --NH--CO--Re or --CHRc--CO--Re, R.sup.5 is hydrogen, lower alkyl, lower hydroxyalkyl, lower alkoxyalkyl, lower haloalkyl, aryl or a fused benzene ring, R.sup.Type: GrantFiled: September 29, 1987Date of Patent: February 28, 1989Assignee: Hoffmann-LaRoche Inc.Inventor: Helmut Link
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Patent number: 4797149Abstract: Disclosed herein are 3,5-pyridinedicarboxylic acid derivatives having heteroatom substitution at the 4 position which are useful as herbicides and herbicide precursors.Type: GrantFiled: June 22, 1987Date of Patent: January 10, 1989Assignee: Monsanto CompanyInventors: Len F. Lee, Maria L. Miller
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Patent number: 4797413Abstract: Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.Type: GrantFiled: June 26, 1987Date of Patent: January 10, 1989Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Gerald S. Ponticello, Marcia E. Christy
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Patent number: 4788187Abstract: A class of benzocyclobutene aminoalkylene ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.Type: GrantFiled: February 26, 1988Date of Patent: November 29, 1988Assignee: Rorer Pharmaceutical CorporationInventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt
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Patent number: 4783537Abstract: Novel .alpha.-aryl-.alpha.-(.omega.-aminoalkyl)-.alpha.-[hydroxy(aralkyl and cycloalkyl)]acetic acid derivatives and .alpha.-aryl-.alpha.-(.omega.-aminoalkyl)-.alpha.[alkanoyloxy(aralkyl and cycloalkyl)]acetic acid derivatives, such as N,N-dimethyl-2-(hydroxyphenylmethyl)-4-dimethylamino-2-phenylbutanamide, 2-(hydroxyphenylmethyl)-5-dimethylamino-2-phenylpentanenitrile, ethyl 2-(hydroxyphenylmethyl)-5-dimethylamino-2-phenylpentanoate, and N,N-dimethyl-2[(acetyloxy)phenylmethyl]-4-dimethylamino-2-phenylbutanamide , useful in the treatment of cardiovascular disease.Type: GrantFiled: November 13, 1985Date of Patent: November 8, 1988Assignee: Pennwalt CorporationInventor: Robert J. Murray
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Patent number: 4782086Abstract: Fungicidally active novel E-isomers of N.sup..alpha. -(2-cyano-2-alkoximino-acetyl)-amino acid derivatives and peptides of the general formula (I) ##STR1## in which R represents alkyl, alkenyl, alkinyl, cyanoalkyl, azolylalkyl or optionally substituted phenylalkyl, or represents optionally substituted cycloalkyl;R.sup.1 represents hydrogen, alkyl, optionally substituted phenyl or optionally substituted benzyl, or represents alkoxycarbonylamino;R.sup.2 represents hydrogen or alkyl;R.sup.3 represents hydrogen, alkyl, alkoxycarbonylalkyl, hydroxycarbonylalkyl, aminocarbonylalkyl, azolylalkyl, cyanoalkyl, hydroxyalkyl, alkenyl, alkinyl or optionally substituted cycloalkyl, or represents optionally substituted phenyl or phenylalkyl, or represents the groupingR.sup.4 --SO.sub.n --Z--R.sup.4 n and Z having various meanings, andX is --OH--OR.sup.1 or --NR.sup.2 R.sup.3.Type: GrantFiled: February 20, 1987Date of Patent: November 1, 1988Assignee: Bayer AktiengesellschaftInventors: Winfried Lunkenheimer, Hans Scheinpflug, Wilhelm Brandes
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Patent number: 4771049Abstract: Novel labdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: March 16, 1987Date of Patent: September 13, 1988Assignee: Hoechst-Roussel PharmaceuticalsInventors: Raymond W. Kosley, Jr., Robert J. Cherill
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Patent number: 4767769Abstract: Compounds of formula I ##STR1## in which R.sub.1 and R.sub.2, which may be the same or different, are hydrogen, a C.sub.1 to C.sub.3 alkyl group or R.sub.1 and R.sub.2 together with the nitrogen to which they are attached form an optionally substituted heterocyclic ring; R.sub.3 and R.sub.4, which may be the same or different are hydrogen, a C.sub.1 to C.sub.3 alkyl or an optionally substituted C.sub.3 to C.sub.6 cycloalkyl group, or R.sub.3 and R.sub.4 together with the nitrogen to which they are attached form an optionally substituted heterocyclic ring; m is 0, 1 or 2; p is 0, 1 or 2; E is an alkylene group connected to or interrupted by an oxygen or a sulphur atom; J is hydrogen or a substituent group; and their pharmaceutically acceptable salts have utility as histamine H.sub.2 -receptor antagonists.Type: GrantFiled: June 23, 1987Date of Patent: August 30, 1988Assignee: The Boots Company PLCInventors: Michael H. Hockley, Roger B. Titman
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Patent number: 4753934Abstract: Compounds of the formula ##STR1## wherein A, B, R.sub.1, X and Q are substituents of various types, and acid addition salts thereof. The compounds are useful as fungicides.Type: GrantFiled: September 29, 1986Date of Patent: June 28, 1988Assignee: Celamerck GmbH & Co. KGInventors: Josef Nickl, Helmut Pieper, Jurgen Curtze, Christo Drandarevski, Sigmund Lust
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Patent number: 4742057Abstract: A thiazole compound of allergically activity of the formula: ##STR1## wherein R.sup.1 is amino optionally having suitable substituent(s),R.sup.2 is hydrogen, lower alkyl or aryl,R.sup.3 is hydrogen, nitro, amino optionally having suitable substituent(s), hydroxy or lower alkoxy,A is lower alkylene,Q is hydrogen or halogen, anda heavy solid line means a single or double bond,or a pharmaceutically acceptable salt thereof, processes for the preparation thereof and pharmaceutical composition comprising the same.Type: GrantFiled: November 20, 1986Date of Patent: May 3, 1988Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Ikuo Ueda, Masaaki Matsuo, Takashi Manabe, Hiroshi Matsuda
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Patent number: 4740232Abstract: Herbicidally active 5-amino-1-phenylpyrazoles of the formula ##STR1## in which R is CN, or an ester or amido group,R.sup.1 is an organic radical,R.sup.2 is an organic radical, hydrogen or an acyl or thioacyl radical,R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 can be hydrogen or various organic radicals but at least one is a haloalkyl, haloalkoxy, haloalkylthio, haloalkylsulphinyl or haloalkylsulphonyl radical, but R is not CN at the same time as R.sup.5 is CF.sub.3. The compounds ##STR2## are intermediates therefor and are also herbicidal.Type: GrantFiled: July 11, 1985Date of Patent: April 26, 1988Assignee: Bayer AktiengesellschaftInventors: Reinhold Gehring, Jorg Stetter, Otto Schallner, Ludwig Eue, Hans-Joachim Santel, Robert R. Schmidt
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Patent number: 4739106Abstract: A process for preparing a 2-carbamoyloxyalkyl-1,4-dihydropyridine derivative represented by the general formula: ##STR1## which comprises: (a) reacting a 3-amino-3-carbamoyloxyalkylacrylic acid derivative represented by the general formula: ##STR2## with a benzylidene compound represented by the general formula: ##STR3## (b) reacting the 3-amino-3-carbamoyloxyalkylacrylic acid derivative of the general formula II with an aldehyde compound represented by the general formula: ##STR4## and a .beta.-keto-ester compound represented by the general formula:R.sup.4 --CO--CH.sub.2 --COOR.sup.2 (V)(c) reacting a 3-carbamoyloxyalkylpropiolic acid derivative represented by the general formula: ##STR5## with the benzylidene compound of the general formula III and ammonia or its salt; or(d) reacting the 3-carbamoyloyalkylpropiolic acid derivative of the general formula VI with the aldehyde compound of the general formula IV, the .beta.-keto-ester compound of the general formula V and ammonia or its salt.Type: GrantFiled: May 16, 1986Date of Patent: April 19, 1988Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Tetsuji Miyano, Kunio Suzuki, Nobuo Harada
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Patent number: 4737508Abstract: Novel compounds including 1-aryl-1-(1H-imidazol-1-ylmethyl)-1,3-dihydroisobenzofurans such as 1-(4-chlorophenyl)-1-(1H-imidazol-1-ylmethyl)-1,3-dihydroisobenzofuran, and 1-aryl-1-(1H-1,2,4-trizazol-1-ylmethyl)-1,3-dihydroisobenzofurans are disclosed. The corresponding benzo[c]thiopenes, isochromans, and isothiochromans and antifungal pharmaceutical compositions containing same, and methods of using said pharmaceutical compositions to elicit an antifungal response in warm blooded animals having a susceptible antifungal infection are also disclosed.Type: GrantFiled: February 1, 1985Date of Patent: April 12, 1988Assignee: Schering CorporationInventors: Raymond G. Lovey, Arthur J. Elliott
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Patent number: 4721710Abstract: The present invention relates to derivatives of piperidinedione of formula: ##STR1## in which R is alkyl or forms with N a possibly substituted morpholino or piperidino group, n=2 or 3, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 represent H or lower alkyl; R.sub.3 and R.sub.4 taken together may represent (CH.sub.2).sub.m where m=4 or 5 and R.sub.2 and R.sub.3 taken together may represent (CH.sub.2).sub.p where p=3 or 4 and in this case R.sub.1 and R.sub.4 =H, R.sub.5 is H or alkyl. It also relates to a process for manufacturing the product of formula (I) and to the drugs containing a product of formula (I).Type: GrantFiled: March 10, 1986Date of Patent: January 26, 1988Assignee: SanofiInventors: Claude Bernhart, Werner Cautreels, Patrick Gautier
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Patent number: 4710510Abstract: The present invention provides new pyrrolobenzimidazoles of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl or cycloalkyl radical; R.sub.2 is a hydrogen atom, cyano group or alkyl or alkenyl radical or a carbonyl group substituted by hydroxyl, alkyl, alkoxy, amino, alkylamino, dialkylamino or hydrazino or together with R.sub.1 forms a cycloalkylene radical or R.sub.1 and R.sub.2 together form an alkylidene or cycloalkylidene radical; R.sub.3, R.sub.4 and R.sub.Type: GrantFiled: December 10, 1985Date of Patent: December 1, 1987Assignee: Boehringer Mannheim GmbHInventors: Alfred Mertens, Jens-Peter Holck, Wolfgang Kampe, Bernd Muller-Beckmann, Klaus Strein, Wolfgang Schaumann
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Patent number: 4705805Abstract: Certain 2,2'-dithiobis-N-substituted or unsubstituted benzamides or derivatives thereof are useful as antithrombotic agents because of their ability to suppress aggregation of blood platelets.Type: GrantFiled: February 17, 1987Date of Patent: November 10, 1987Inventors: Koji Yamada, Tamotsu Hashimoto, Masao Naruse, Yo Murayama, Hideki Ninno
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Patent number: 4685956Abstract: Herbicidally active 1-aryl-5-hydrazinopyrazoles of the formula ##STR1## in which R.sup.1 represents hydrogen or alkyl,R.sup.2 represents cyano or nitro,R.sup.3 represents hydrogen, or represents in each case optionally substituted alkyl, alkenyl, alkinyl or cycloalkyl, or represents a radical ##STR2## or represents a radical --SO.sub.2 --R.sup.7, R.sup.4 represents hydrogen, or represents in each case optionally substituted alkyl, alkenyl, alkinyl or cycloalkyl, or represents a radical ##STR3## or represents a radical --SO.sub.2 --R.sup.7, R.sup.5 represents hydrogen: or, in the case where R.sup.4 represents hydrogen, also represents a radical ##STR4## or represents a radical --SO.sub.2 --R.sup.7, or represents in each case optionally substituted alkyl, alkenyl, alkinyl or cycloalkyl, wherein, in each case,X represents oxygen or sulphur,R.sup.Type: GrantFiled: July 14, 1986Date of Patent: August 11, 1987Assignee: Bayer AktiengesellschaftInventors: Reinhold Gehring, Otto Schallner, Jorg Stetter, Hans-Joachim Santel, Robert R. Schmidt
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Patent number: 4684644Abstract: The present invention is directed to a class of basic monocarboxyamide derivatives of actagardine. Actagardine (INN) is an antibiotic substance produced by actinoplanes strains such as Actinoplanes Sp. ATCC 31048 and Actinoplanes Sp. ATCC 31049 which are described in U.S. Pat. No. 4,022,884. Actagardine shows antimicrobial in vitro and in vivo activity against gram-positive organisms. Its complete chemical structure is not yet known but there is only information on its chemical functions and main fragments. In particular, it has been found that actagardine has two carboxylic functions and a primary amino function and can therefore be represented as follows: ##STR1## The compounds of the invention are monoamide derivatives at one of the carboxy functions of actagardine.Type: GrantFiled: March 21, 1986Date of Patent: August 4, 1987Assignee: Gruppo Lepetit S.p.A.Inventors: Adriano Malabarba, Bruno Cavalleri
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Patent number: 4683228Abstract: A guanidine derivative of the formula I: ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, ring X and D are a variety of radicals defined in the specification and A is a 3-8C alkylene chain which is substituted by a hydroxy radical and into which is optionally inserted, as part of the backbone of the chain, one or two groups selected from oxygen and sulphur atoms and NH and 1-6C N-alkyl radicals; and the pharmaceutically-acceptable acid additions salts thereof. Pharmaceutical compositions and methods of manufacture are also described. The compound of the formula I is a histamine H-2 antagonist and is therefore useful in ulcer therapy.Type: GrantFiled: January 22, 1985Date of Patent: July 28, 1987Assignees: ICI Americas Inc., Imperial Chemical Industries PLCInventors: Karin M. Kirkland, Derrick M. Mant
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Patent number: 4661483Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1## and pharmaceutically acceptable salts of the compounds (II) in which Z is hydrogen are disclosed.Type: GrantFiled: May 5, 1986Date of Patent: April 28, 1987Assignee: Merck & Co., Inc.Inventors: William F. Hoffman, Clarence S. Rooney, Ta J. Lee
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Patent number: 4652573Abstract: Compounds having calcium channel antagonist activity of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each independently amino, trifluoromethyl, pentafluoroethyl, alkoxy, lower alkenyl, or lower alkynyl or branched or unbranched lower alkyl, which is unsubstituted or is substituted with cyano, hydroxy, acyloxy, hydrazino, lower alkyl amino, or di(lower alkyl)-amino or 5 or 6 membered saturated nitrogen-containing heterocyclic-1-yl, which is unsubstituted or is substituted with oxo, hydroxy, alkyl, and hydroxy (lower alkyl) R.sub.3 is straight- or branched-chain C.sub.1 to C.sub.12 alkyl, alkenyl, alkynyl, or cycloalkyl, and is either unsubstituted or substituted with hydroxy, acyloxy, cyano, di(lower alkyl) amino 5- or 6-membered saturated nitrogen-containing heterocyclic-1-yl or R.sub.3 is --A-R.sub.4, A is a straight- or branched-chain hydrocarbon moiety containing from 2 to 12 carbon atoms and from 0 to 2 double bonds, R.sub.4 is selected from the group consisting of: ##STR2## R.sub.Type: GrantFiled: March 14, 1985Date of Patent: March 24, 1987Assignee: Nelson Research & Development Co.Inventors: Gevork Minaskanian, Vithal J. Rajadhyaksha
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Patent number: 4647675Abstract: Novel compounds of the general formula I ##STR1## where A.sup..crclbar. is an anion, R is hydrogen or unsubstituted or substituted alkyl or cycloalkyl, R.sup.1 and R.sup.2 independently of one another are each hydrogen or unsubstituted or substituted alkyl or cycloalkyl, or one of the radicals may furthermore be aryl, or R.sup.1 and R.sup.2, together with the nitrogen atom, form a saturated heterocyclic structure, the radicals R.sup.3 independently of one another are each hydrogen or C.sub.1 -C.sub.4 -alkyl, R.sup.4 and R.sup.5 independently of one another are each unsubstituted or substituted alkyl or cycloalkyl, or one of the radicals may furthermore be hydrogen, aryl or hetaryl, R.sup.4 and R.sup.5, together with the nitrogen atom, form a saturated heterocyclic structure, n is 1, 2 or 3, X is hydrogen, chlorine, bromine, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or nitro and Y is hydrogen or chlorine, are particularly useful for dyeing paper stocks.Type: GrantFiled: July 11, 1985Date of Patent: March 3, 1987Assignee: BASF AktiengesellschaftInventors: Udo Mayer, Andreas Oberlinner
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Patent number: 4632986Abstract: Thiocarbamylsulfenamides are readily recovered from solutions of the thiocarbamylsulfenamides by the addition of a dilute aqueous caustic solution, to flash off the solvent separating the thiocarbamylsulfenamide from the resulting water slurry and drying the thiocarbamylsulfenamide.Type: GrantFiled: July 29, 1985Date of Patent: December 30, 1986Assignee: The BFGoodrich CompanyInventors: Enrique G. Reynes, John O. Leising
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Patent number: 4623486Abstract: Certain novel p-aminomethylbenzoyl derivatives of 4-hydroxy-2-methyl-N-(2-pyridinyl)-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide and several other closely-related known oxicams have been prepared. These particular compounds are useful in therapy as prodrug forms of the known anti-inflammatory and analgesic oxicams. Preferred member compounds include 2-methyl-4-[4-(morpholinomethyl)benzoyloxy]-N-(2-pyridinyl)-2H-1,2-benzoth iazine-3-carboxamide 1,1-dioxide, 2-methyl-4-[4-(piperidinomethyl)benzoyloxy]-N-(2-pyridinyl)-2H-1,2-benzoth iazine-3-carboxamide 1,1-dioxide, 2-methyl-N-(6-methyl-2-pyridinyl)-4-[4-(piperidinomethyl)benzoyloxy]-2H-1, 2-benzothiazine-3-carboxamide 1,1-dioxide, 2-methyl-4-[4-(4-methylpiperazinomethyl)benzoyloxy]-N-(2-pyridinyl)-2H-1,2 -benzothiazine-3-carboxamide 1,1-dioxide and 2-methyl-4-[4-(pyridiniummethyl)benzoyloxy]-N-(2-pyridinyl)-2H-1,2-benzoth iazine-3-carboxamide 1,1-dioxide chloride. Methods for preparing these compounds from known starting materials are provided.Type: GrantFiled: May 29, 1985Date of Patent: November 18, 1986Assignee: Pfizer Inc.Inventor: Joseph G. Lombardino
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Patent number: 4618634Abstract: Novel compounds containing piperidine groups, of the general formula ##STR1## in which R.sub.1 is hydrogen, O--, cyanomethyl, C.sub.1 -C.sub.12 -alkyl, C.sub.3 -C.sub.12 -alkenyl or -alkynyl, C.sub.7 -C.sub.12 -aralkyl or C.sub.1 -C.sub.12 -acyl, m is an integer from 1 to 12, n is an integer from 1 to 3 and A is an amine radical, are suitable as light stabilizers, heat stabilizers and oxidation stabilizers for synthetic polymers. Processes for their preparation are also described.Type: GrantFiled: February 27, 1985Date of Patent: October 21, 1986Assignee: Ciba-Geigy S.p.A.Inventors: Giuseppe Cantatore, Valerio Borzatta
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Patent number: 4610983Abstract: This invention relates to a novel N-acyl acidic amino acid diamide derivative represented by the general formula or a salt thereof: ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, represents a hydrogen atom or a substituted or unsubstituted alkyl, cycloalkyl, alkenyl or aralkyl group, or R.sup.1 and R.sup.2 and/or R.sup.3 and R.sup.4, when taken together with the respective adjacent nitrogen atoms, form a substituted or unsubstituted heterocyclic group; R.sup.5 represents a substituted or unsubstituted cycloalkyl, acyl or heterocyclic group; A represents a bond or a substituted or unsubstituted alkylene, alkenylene or alkadienylene group; and n is 1, 2 or 3. Said compound has an anti-ulcer activity which is effective to human beings and animals. This disclosure relates to such a compound, to a process for the production thereof and to an anti-ulcer agent containing the same.Type: GrantFiled: December 3, 1984Date of Patent: September 9, 1986Assignee: Toyama Chemical Co., Ltd.Inventors: Noboru Takagawa, Shiro Hirai, Takuya Kodama, Hiroshi Hirano, Yasuo Kiba, Mikio Kawabata, Tatsuya Miyaura, Yasuyuki Suzuki
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Patent number: 4604393Abstract: This invention relates to novel piperidines substituted on the nitrogen atom with a (phenyloxo alkyl) group as well as the processes for their production.Type: GrantFiled: January 30, 1984Date of Patent: August 5, 1986Inventors: Pierre-Jean Cornu, Claude Perrin, Bernard Dumaitre, Gilles Streichenberger
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Patent number: 4596800Abstract: A compound of formula (I) ##STR1## or a pharmaceutically acceptable salt thereof, in which R.sup.1 is hydrogen, halogen, or trifluoromethyl;R.sup.2 is hydrogen or halogen;R.sup.3 is hydrogen or methyl;R.sup.4 is --O(CH.sub.2).sub.a CO.sub.2 H or an ester or amide derivative thereof, O(CH.sub.2).sub.b M or --CO.sub.2 H or an ester or amide derivative thereofwhereina is an integer from 1 to 6,b is an integer from 2 to 7, andM is hydroxy, C.sub.1-6 alkoxy or ##STR2## wherein R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-6 alkyl or ##STR3## together form a five or six membered ring; R.sup.5 is C.sub.1-6 alkyl; C.sub.1-6 alkyl substituted by carboxy or esters and amides thereof; or phenyl optionally substituted by C.sub.1-6 alkyl, halogen, alkoxy or trifluoromethyl;R.sup.8 is hydrogen or C.sub.1-6 alkyl or R.sup.8 together withR.sup.5 form a carbocyclic ring; andn is 1 or 2.Processes for preparing these compounds and their use in therapy is also described.Type: GrantFiled: July 19, 1985Date of Patent: June 24, 1986Assignee: Beecham Group p.l.c.Inventors: Anthony T. Ainsworth, Richard M. Hindley
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Patent number: 4593023Abstract: A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, thereof, in which R.sup.1 is hydrogen, halogen, or trifluoromethyl,R.sup.2 is hydrogen or halogen,R.sup.3 is hydrogen or methyl.R.sup.4 is --O(CH.sub.2).sub.a CO.sub.2 H, --O(CH.sub.2).sub.b M, --CO.sub.2 H or an esteror amide derivative thereof in whicha is an integer from 1 to 6,b is an integer from 2 to 7, andM is hydroxy, C.sub.1-6 alkoxy or ##STR2## in which R.sup.5 and R.sup.6 are each hydrogen or C.sub.1-6 alkyl or ##STR3## together form a five or six membered ring, and n is 1 or 2; a process for preparing such a compound and its use in medicine and agriculture.Type: GrantFiled: May 17, 1985Date of Patent: June 3, 1986Assignee: Beecham Group p.l.c.Inventor: Richard M. Hindley
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Patent number: 4593102Abstract: Novel pyrrolidine, piperidine and homopiperidinecarboxamide and thiocarboxamide compounds having the formula: ##STR1## wherein X is --S--, --S(O)-- or --S(O).sub.2 --; A is a loweralkalene chain and A.sup.1 and A.sup.2 are alkalene chains when p and d are one; R, R.sup.1 and R.sup.2 are hydrogen, loweralkyl, phenyl cycloalkyl or phenylalkyl and R.sup.1 and R.sup.2 may form a heterocyclic residue with the adjacent nitrogen atom; Q is a selected aromatic radical, and the pharmaceutically acceptable acid addition salts useful as cardiac antiarrhythmia agents are disclosed.Novel chemical intermediates, unsubstituted on pyrrolidine, piperidine and homopiperidine nitrogen but with --(A.sup.2).sub.p --X--(A.sup.2).sub.d --Q side chain are also disclosed.Type: GrantFiled: July 1, 1985Date of Patent: June 3, 1986Assignee: A. H. Robins Company, Inc.Inventor: James R. Shanklin, Jr.
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Patent number: 4581354Abstract: 3-Arylcarbonyl- and 3-cycloalkylcarbonyl-1-aminoalkyl-1H-indoles, useful as analgesic, anti-rheumatic and anti-inflammatory agents, are prepared by reacting a 3-arylcarbonyl- or 3-cycloalkylcarbonylindole with an aminoalkyl halide in the presence of an acid-acceptor; by reacting a 1-aminoalkyl-1H-indole with an arylcarboxylic acid halide or a cycloalkanecarboxylic acid halide in the presence of a Lewis acid; or by reacting a 3-arylcarbonyl- or 3-cycloalkanecarbonyl-1-tosyloxyalky- or haloalkyl-1H-indole with an amine.Type: GrantFiled: July 15, 1985Date of Patent: April 8, 1986Assignee: Sterling Drug Inc.Inventor: Malcolm R. Bell
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Patent number: 4579845Abstract: This invention relates to novel tri-substituted guanidines linked to a piperidine ring.More specifically, it relates to cyanoguanidines of formula I ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 are substituentsn is an integer of zero to 1n' is an integer of zero to 1A and B are --CH.sub.2 --, CHOH, --CO-- or a single bondas well as the acid addition salts thereof with a mineral or organic acid.The compounds have interesting pharmacological properties which make them useful as active ingredient of medicines, e.g. antihypertensives.Type: GrantFiled: December 8, 1983Date of Patent: April 1, 1986Assignee: Bouchara S.A.Inventors: Pierre-Jean Cornu, Claude Perrin, Bernard Dumaitre, Gilles Streichenberger
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Patent number: 4576749Abstract: Antibacterial activity is exhibited by 2-azetidinones having a 3-acylamino substituent and a 1-substituent of the formula ##STR1## (or a salt or ester thereof).Type: GrantFiled: April 13, 1984Date of Patent: March 18, 1986Assignee: E. R. Squibb & Sons, Inc.Inventors: Robert Zahler, William H. Koster, William A. Slusarchyk
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Patent number: 4556714Abstract: Compounds of the formula I ##STR1## in which m is zero, 1 or 2 and n is 2, 3 or 4, R.sup.1 is hydrogen or C.sub.1 -C.sub.4 -alkyl, A is the n-valent radical of a polyol and R.sup.2 and R.sup.3 are monovalent radicals as defined in claim 1, are outstanding light stabilizers for organic materials, particularly for organic polymers.Type: GrantFiled: January 16, 1984Date of Patent: December 3, 1985Assignee: Ciba-Geigy CorporationInventor: Friedrich Karrer
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Patent number: 4547537Abstract: Compounds of the formula L-T, where L is an unsubstituted or substituted tetrahydro-1,4-oxazine-2-one group and T is a substituted 4-piperidinyl hindered amine moiety, are effective light stabilizers for polyolefins and other organic polymers.Type: GrantFiled: August 2, 1984Date of Patent: October 15, 1985Assignee: Ciba-Geigy CorporationInventors: Roger F. Malherbe, Michael H. Ackerman
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Patent number: 4539318Abstract: Novel tertiary aminohydroxypropoxy substituted thiadiazole compounds exhibit .alpha..sub.1 -adrenoceptor and serotonin antagonism and are also useful as antihypertensive agents.Type: GrantFiled: June 4, 1984Date of Patent: September 3, 1985Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Gerald S. Ponticello
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Patent number: 4530925Abstract: Compounds are described of the formulae (1a) and (1b) ##STR1## in which: --COR.sup.1 is an ester group,n is 1 or 2,W is C.sub.1-7 alkylene,X is cis or trans --CH.dbd.CH or --CH.sub.2 CH.sub.2 --,Y is a saturated heterocyclic amino group,R.sup.2 is substituted or unsubstituted phenylalkyl, thienylalkyl or naphthylalkyl or cinnamyl, andR.sup.3 is --H or C.sub.1-5 alkanoyl, including their salts.These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic or antiasthmatic agents.Type: GrantFiled: March 14, 1984Date of Patent: July 23, 1985Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, John Bradshaw
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Patent number: 4486429Abstract: Compounds of the formula I: ##STR1## in which R represents a hydrogen atom or an alkyl radical containing from 1 to 8 carbon atoms and R.sub.1 and R.sub.2, which may be identical or different independently represent a hydrogen atom, an alkyl radical containing from 1 to 4 carbon atoms, a --CONH.sub.2 radical, a --CO.sub.2 alk.sub.1 radical in which alk.sub.1 represents an alkyl radical containing from 2 to 8 carbon atoms, or an--SO.sub.2 alk.sub.2 radical in which alk.sub.2 represents an alkyl radical containing from 1 to 8 carbon atoms, or R.sub.1 and R.sub.2 together with the nitrogen atom form a heterocycle provided that R.sub.1 and R.sub.2 are not both hydrogen, as well as the alkali metal, alkaline earth metal, ammonium or amine salts of compounds of formula I in which R represents a hydrogen atom. These compounds are useful in treating hyperchlorhydria, gastric or gastroduodenal ulcers, gastritis, hiatal hernias and gastric or gastroduodenal ailments accompanied by gastric hyperacidity.Type: GrantFiled: October 20, 1982Date of Patent: December 4, 1984Assignee: Roussel UclafInventors: Mario Bianchi, Fernando Barzaghi
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Patent number: 4483984Abstract: 3,7-Substituted phenoxiodinin-5-ium compounds are effective against a variety of aerobic and anaerobic bacteria as well as fungi. The compounds of this invention may be prepared by the direct iodination of a suitably substituted diphenyl ether with iodosyl sulfate in concentrated sulfuric acid. The resulting bisulfate anion may be exchanged with a desired anion by standard metathetic processes.Type: GrantFiled: December 15, 1983Date of Patent: November 20, 1984Assignee: The Dow Chemical CompanyInventor: Edward E. Flagg
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Patent number: 4482549Abstract: Compounds are described of the formula ##STR1## in which --COR.sup.1 is a complex ester or thioester group,W is alkylene,X is cis or trans --CH.dbd.CH or --CH.sub.2 CH.sub.2 --,n is 1 or 2,Y is a saturated heterocyclic amino group having 5-8 ring members, andR.sup.2 is unsubstituted or substituted phenylalkyl, thienzlalkyl, naphthylalkyl or cinnamyl, and their salts and solvates.These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic and antiasthmatic agents.Type: GrantFiled: February 8, 1984Date of Patent: November 13, 1984Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, Norman F. Hayes, John Bradshaw, Malcolm Carter, Alan Wadsworth
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Patent number: 4478836Abstract: The present invention concerns new derivatives of 1-aryl 2-aminomethyl cyclopropane carboxamides (Z) of general formula I: ##STR1## in which: R represents a hydrogen or halogen atom, a lower alkyl group, a lower alkoxy group, or a hydroxy. nitro or amino group;n represents the value 1 or 2;R.sub.1 and R.sub.2 represent a hydrogen atom, a lower alkyl group, an aryl or lower alkaryl group, possibly substituted, preferably in para position, by a halogen atom, preferably a chlorine atom;R.sub.1 and R.sub.2 may also form a heterocycle having 5 or 6 members with the adjacent nitrogen atom;R.sub.3 and R.sub.4 represent a hydrogen atom or a lower alkyl group;R.sub.3 and R.sub.Type: GrantFiled: June 22, 1982Date of Patent: October 23, 1984Assignee: Pierre Fabre S.A.Inventors: Gilbert Mouzin, Henri Cousse, Bernard Bonnaud, Michel Morre, Antoine Stenger
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Patent number: 4470932Abstract: Carboxylic acid anhydrides of the general formulaR--CO--O--CO--R' (I)in whichR and R' are identical or different and represent an optionally substituted alkyl group having 1 to 18 carbon atoms, an optionally substituted cycloalkyl group having 3 to 12 carbon atoms or an optionally substituted aryl group, or represent an optionally substituted 5-membered or 6-membered heterocyclic radical which additionally can be fused to a benzene ring,are obtained in high yields by a process in which a trimethylsilyl carboxylate of the general formulaR--CO--OSi(CH.sub.3).sub.3 (II)in whichR has the meaning given above, is reacted with a carboxylic acid-halide of the general formulaR'CO--X (III)in whichR' has the meaning given above, andX represents a halogen atom, if appropriate in the presence of a catalyst and, if appropriate, in the presence of a diluent, at a temperature between 20.degree. and 250.degree. C.The carboxylic acid anhydrides are valuable intermediate products for organic syntheses.Type: GrantFiled: October 22, 1982Date of Patent: September 11, 1984Assignee: Bayer AktiengesellschaftInventor: Kurt Findeisen
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Patent number: 4447428Abstract: Prostanoid compounds are described having the formula: ##STR1## where A is a cyclopentane ring, which is substituted by oxo and/or hydroxy or etherified hydroxy and may be saturated or unsaturated; X is --CH.dbd.CH--or --(CH.sub.2).sub.2 --; R is alkyl having a terminal --COOH or ester group; and Y is amino or substituted amino, particularly heterocyclic amino.The compounds have bronchodilator activity and/or inhibit blood platelet aggregation.The preparation and pharmaceutical formulation of the compounds is also described.Type: GrantFiled: July 15, 1983Date of Patent: May 8, 1984Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Harry Finch, Roger F. Newton
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Patent number: 4440943Abstract: 3,7-Substituted phenoxiodinin-5-ium compounds are effective against a variety of aerobic and anaerobic bacteria as well as fungi. The compounds of this invention may be prepared by the direct iodination of a suitably substituted diphenyl ether with iodosyl sulfate in concentrated sulfuric acid. The resulting bisulfate anion may be exchanged with a desired anion by standard metathetic processes.Type: GrantFiled: March 15, 1982Date of Patent: April 3, 1984Assignee: The Dow Chemical CompanyInventor: Edward E. Flagg
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Patent number: 4438111Abstract: Prostanoids are described of the formulae ##STR1## (and the salts thereof) in which: X is cis or trans--CH.dbd.CH-- or CH.sub.2 CH.sub.2 --;R.sup.1 is C.sub.1-7 alkyl terminated by --COOR.sup.10 where R.sup.10 is H, C.sub.1-6 alkyl or aralkyl;Y is a saturtaed heterocyclic amino group; andR.sup.4 is thienylalkyl or furanylalkyl in which the ring may be substituted.These compounds inhibit blood platelet aggregation and have bronchodilatory action, and may be formulated for use as anti-asthmatics and antithrombotic agents.Type: GrantFiled: September 17, 1982Date of Patent: March 20, 1984Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis
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Patent number: 4438112Abstract: Prostanoids are described of the formulae ##STR1## (and the salts thereof) in which: X is cis or trans --CH.dbd.CH-- or CH.sub.2 CH.sub.2 --;R.sup.1 is C.sub.1-7 alkyl terminated by --COOR.sup.10 where R.sup.10 is H, C.sub.1-6 alkyl or aralkyl;Y is a saturated heterocyclic amino group; andR.sup.4 is aralkyl (in which the aryl portion is substituted by alkylthio, alkylsulphinyl, alkylsulphonyl, alkanoylamino, aroylamino, phenalkyl, aminosulphonyl, alkanoylaminosulphonyl, phenylsulphonyl, nitro, tetrazolyl, substituted phenyl or thienyl).These compounds inhibit blood platelet aggregation and have bronchodilatory action, and may be formulated for use as anti-asthmatics and antithrombotic agents.Type: GrantFiled: September 17, 1982Date of Patent: March 20, 1984Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, John Bradshaw
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Patent number: RE32761Abstract: 3-Arylcarbonyl- and 3-cycloalkylcarbonyl-1-aminoalkyl-1H-indoles, useful as analgesic, anti-rheumatic and anti-inflammatory agents, are prepared by reacting a 3-arylcarbonyl- or 3-cycloalkylcarbonylindole with an aminoalkyl halide in the presence of an acid-acceptor; by reacting a 1-aminoalkyl-1H-indole with an arylcarboxylic acid halide or a cycloalkanecarboxylic acid halide in the presence of a Lewis acid; or by reacting a 3-arylcarbonyl- or 3-cycloalkanecarbonyl-1-tosyloxyalky- or haloalkyl-1H-indole with an amine.Type: GrantFiled: March 23, 1987Date of Patent: October 4, 1988Assignee: Sterling Drug Inc.Inventor: Malcolm R. Bell