Benzo Is The Other Cyclo Patents (Class 544/62)
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Patent number: 5109135Abstract: 2- and 3-Aminomethyl-6-arylcarbonyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazines , useful as analgesic agents, are prepared either by reaction of a 2- or 3-aminomethyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazine with an arylcarboxylic acid halide in the presence of a Lewis acid or by reaction of a 2- or 3-aminomethyl-4-amino-3,4-dihydro-2H-1,4-benzoxazine with a 1-lower-alkyl-3-aryl-1,3-diketone or with a .beta.-aryl-.beta.-ketopropionaldehyde under dehydrating conditions and heating the resulting hydrazone in an acid medium.Type: GrantFiled: August 13, 1991Date of Patent: April 28, 1992Assignee: Sterling Drug Inc.Inventors: Thomas E. D'Ambra, Malcolm R. Bell
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Patent number: 5089043Abstract: A heterocyclic oxy-phenoxyacetic acid derivative of the formula: ##STR1## , or its salt, which is useful as a herbicide.Type: GrantFiled: November 6, 1990Date of Patent: February 18, 1992Assignee: Shionogi & Co., Ltd.Inventors: Yoshio Hayase, Kohei Matsumoto, Kazuo Kamei, Kinya Ide, Toshio Takahashi
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Patent number: 5071841Abstract: The present invention provides a sulfur-containing heterocyclic compound of the formula (I) ##STR1## wherein ring A is a benzene ring which may be substituted; R is a hydrogen atom or a hydrocarbon group which may be substituted; B is a carboxyl group which may be esterified or amidated; X is --CH(OH)-- or --CO--; k is 0 or 1; and k' is 0, 1 or 2 or a pharmaceutically acceptable salt thereof.Also, it provides a process for producing the compound (I) or a salt thereof and a pharmaceutical preparation for use in the treatment of osteoporosis comprising the compound (I) or salt thereof.The compounds (I) and salts thereof show excellent bone resorption inhibitory activity.Type: GrantFiled: December 28, 1989Date of Patent: December 10, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Masao Tsuda, Iwao Yamazaki
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Patent number: 5070090Abstract: Novel (thio)morpholinyl and piperazinyl alkylphenol ethers having antirhinoviral activity, compositions containing these compounds as active ingredient, and a method of inhibiting, combating or preventing the growth of viruses in warm-blooded animals suffering from diseases caused by these viruses.Type: GrantFiled: April 25, 1990Date of Patent: December 3, 1991Assignee: Janssen Pharmaceutica N.V.Inventors: Raymond A. Stokbroekx, Marcel J. M. Van der Aa
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Patent number: 5061813Abstract: Novel compounds are disclosed having the formula ##STR1## and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are as defined herein. These compounds are useful, for example, as cardiovascular agents and especially as anti-ischemic agents.Type: GrantFiled: April 2, 1990Date of Patent: October 29, 1991Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 5037825Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, acyl, lower-alkyl or --CHO, --CH.sub.2 OR.sup.10, --COR.sup.7 or OR.sup.13 ; R.sup.2, R.sup.3 and R.sup.4 are, independently, hydrogen, lower-alkyl, lower-alkoxy or halogen; R.sup.5 and R.sup.6 are, independently, hydrogen or lower-alkyl; R.sup.7 is hydroxy, lower-alkoxy or NR.sup.8 R.sup.9 ; R.sup.8 and R.sup.9 are, independently, hydrogen or lower-alkyl; X and Y are, independently, >CR.sup.14 R.sup.15, --O--, --S--, >SO, >SO.sub.2 or >NR.sup.18 ; R.sup.10 and R.sup.18 are, independently, hydrogen, lower-alkyl or acyl; M is --C(R.sup.11).dbd.C(R.sup.12)--, --CONH-- or --NH--CO--; R.sup.11, R.sup.12, R.sup.14 and R.sup.15 are, independently, hydrogen or lower-alkyl, R.sup.Type: GrantFiled: July 10, 1989Date of Patent: August 6, 1991Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Peter Mohr, Ekkehard Weiss
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Patent number: 5028711Abstract: Benzopyran derivatives of the general formula I ##STR1## are disclosed. The compounds are therapeutic active compounds.Type: GrantFiled: July 6, 1989Date of Patent: July 2, 1991Assignee: Beiersdorf AktiengesellschaftInventors: Wolfgang Stenzel, Theo Schotten, Ben Armah
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Patent number: 5021413Abstract: Analgesic compounds are of the general formula (I): ##STR1## in which, R.sup.1 and R.sup.2 each represents hydrogen or C.sub.1 -C.sub.6 alkyl, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a heterocycle; E represents methylene, sulfur, oxygen or imino group optionally substituted with C.sub.1 -C.sub.6 alkyl or aralkyl; ring A is aryl or heteroaryl ring, optionally substituted; R.sup.3 is hydrogen or C.sub.1 -C.sub.6 alkyl and R.sup.4 is hydrogen or R.sup.3 and R.sup.4 together represent a group of formula (IV):--(CR.sup.a R.sup.a).sub.m --C(.dbd.Y)-- (IV)(wherein R.sup.a and R.sup.a is C.sub.1 -C.sub.6 alkyl or hydrogen, up to a maximum of 3 alkyl groups, m is 1, 2, or 3, and Y is two hydrogens or oxygen); provided that when E represents a methylene group, then R.sup.3 is a C.sub.1 -C.sub.6 alkyl group or R.sup.3 and R.sup.4 together represent a group of the formula (IV).Type: GrantFiled: August 22, 1989Date of Patent: June 4, 1991Assignee: Sankyo Company LimitedInventors: Atsusuke Terada, Yoshio Iizuka, Kazuyuki Wachi, Kenji Fujibayashi
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Patent number: 5017576Abstract: Quinoline derivatives of formula: ##STR1## in which either R.sub.1 denotes trifluoromethyl, R.sub.2 and R.sub.3 form, together with the nitrogen atom to which they are attached, morpholino and R.sub.4 denotes a 4-methylphenyl, 4-chlorophenyl, 2-, 3- or 4-fluorophenyl, 4-methoxyphenyl, 4-methyl-3-fluorophenyl, 2,4-difluorophenyl or 4-aminophenyl,or R.sub.1 denotes trifluoromethyl, R.sub.2 and R.sub.3 form, together with the nitrogen atom to which they are attached, thiomorpholino, or R.sub.2 denotes methyl and R.sub.3 denotes 2-methoxyethyl and R.sub.4 denotes 4-methylphenyl,or R.sub.1 denotes chlorine fluorine, or methoxy, R.sub.2 and R.sub.3 form, together with the nitrogen atom to which they are attached, morpholino, and R.sub.4 denotes 4-methylphenyl, are useful as anxiolytics, hypnotics, anticonvulsants and antiepileptics.Type: GrantFiled: September 11, 1989Date of Patent: May 21, 1991Assignee: Rhone-Poulenc SanteInventors: Marie-Christine Dubroeucq, Jean-Marc Paris, Christian Renault
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Patent number: 5013732Abstract: 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-tosyloxyalkyl- or haloalkyl-1H-indole with an amine.Type: GrantFiled: July 30, 1990Date of Patent: May 7, 1991Assignee: Sterling Drug Inc.Inventor: Malcolm R. Bell
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Patent number: 5000777Abstract: 1,5-substituted imidazole derivatives of formula I ##STR1## the stereochemically isomeric forms thereof, and the salts thereof, have useful herbicidal properties. The substituents R.sup.1, R.sup.2, R.sup.3, R.sup.4, X.sup.1, X.sup.2, X.sup.3, A, L and m have the meanings defined herein.Type: GrantFiled: November 21, 1989Date of Patent: March 19, 1991Assignees: Ciba-Geigy Corporation, Janssen PharmaceuticaInventors: Henry Szczepanski, Lourens Wals
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Patent number: 4996328Abstract: Novel bis-(indolyl)ethylenes, process for their production and record systems utilizing such bis-(indolyl)ethylene chromogens are described.Bis-(indolyl)ethylenes of the following general formula are prepared: ##STR1## wherein each L.sup.1 and L.sup.2 is the same or different and is each independently selected from indole moieties (J1) through (J4) (L.sup.1 need not be the same as L.sup.2), ##STR2## wherein in (J1) through (J4) above, each of R.sup.5, R.sup.6, R.sup.13, R.sup.14, R.sup.21, R.sup.22, R.sup.29 and R.sup.30 need not be the same and is each independently selected from hydrogen, alkyl (C.sub.1 -C.sub.8), cycloalkyl, alkylaroxy, alkylalkoxy, and substituted or unsubstituted aryl, such as phenyl, naphthyl, or heterocyclyl.Each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.15, R.sup.16, R.sup.17, R.sup.18, R.sup.19, R.sup.20, R.sup.23, R.sup.24, R.sup.25, Rphu 26, R.sup.27, and R.sup.Type: GrantFiled: March 8, 1989Date of Patent: February 26, 1991Assignee: Appleton Papers Inc.Inventor: Ponnampalam Mathiaparanam
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Patent number: 4975455Abstract: Compounds of general formula (I): ##STR1## in which: R denotes a hydrogen atom, a halogen atom or a hydroxy, lower alkyl, lower alkyloxy, carboxyl, (lower alkyloxy)carbonyl, (lower arylalkyloxy)carbonyl, aminocarbonyl, (lower mono- or dialkyl)aminocarbonyl or (lower arylalkyl)aminocarbonyl group, an aminocarbonyl group N-substituted with a heterocyclic radical, or a thio, (lower alkyl)thio, sulfonyl or (lower alkyl)sulfonyl group,R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be identical or different, denote a hydrogen atom, a halogen atom or a lower alkyl, lower alkenyl, lower alkyloxy or lower alkenyloxy group, optionally substituted with one or more halogen atoms,their isomers, enantiomers, diastereoisomers and also, when R denotes a carboxyl, their addition salts with a pharmaceutically acceptable base and, when R contains a basic group, their addition salts with a pharmaceutically acceptable acid.Type: GrantFiled: April 11, 1989Date of Patent: December 4, 1990Assignee: Adir et CieInventors: Jean-Daniel Brion, Guillaume Le Baut, Patrick Ducrey, Sylvie Piessard-Robert, Claude Cudennec, Genevieve Seurre
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Patent number: 4973590Abstract: Known quinolone carboxylic acid derivatives of the formula ##STR1## are treated so as to become readily administrable parenterally, the treatment comprising dissolving the active compound using an acid, allowing the solution to stand for about 0.15 to 150 hours at a temperature from room temperature to the boiling point of the solution, filtering the solution, precipitating the active compound from the solution using a basic reagent, and converting the precipitated active compound into a form which can be administered parenterally.Type: GrantFiled: April 15, 1988Date of Patent: November 27, 1990Assignee: Bayer AktiengesellschaftInventors: Michael Preiss, Ulrich Schorsch, Arthur Haaf, Paul Naab, Rudolf Zerbes
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Patent number: 4970308Abstract: Chromogenic di-[bis-(indolyl)ethylenyl] tetrahalophthalides are disclosed of the formula ##STR1## wherein each X.sup.1, X.sup.2, X.sup.3, and X.sup.4 is independently selected from chlorine or bromine;wherein each of R.sup.1 and R.sup.7 is independently selected from cycloalkyl, aralkyl, alkoxyalkyl, or aroxyalkyl;wherein each of R.sup.2 and R.sup.8 is independently selected from alkyl (C.sub.1 -C.sub.8) or aryl (substituted or unsubstituted);wherein each of R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.9, R.sup.10, R.sup.11, and R.sup.12 is independently selected from hydrogen, alkyl (C.sub.1 -C.sub.8), cycloalkyl, aryl (substituted or unsubstituted), halogen, alkoxy (C.sub.1 -C.sub.8), aroxy, cycloalkoxy, dialkylamino including symmetrical and unsymmetrical (C.sub.1 -C.sub.Type: GrantFiled: August 23, 1989Date of Patent: November 13, 1990Assignee: Appleton Papers Inc.Inventor: Ponnampalam Mathiaparanam
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Patent number: 4959379Abstract: Fungicidal 7-substituted 2-carboxamido-benzothiazole 3-oxides of the formula ##STR1## in which n stands for the numbers 0, 1, 2 or 3,R.sup.1 stands for hydrogen or optionally substituted alkyl,R.sup.2 stands for hydrogen, hydroxyl, ureido or for an optionally substituted radical from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkinyl, alkoxy, alkenyloxy, aralkoxy, aralkyl, aryl, heterocyclyl and heterocyclylakyl, orR.sup.1 and R.sup.2 together stand for an alkylene chain which is optionally substituted and optionally interrupted by hetero atoms,R.sup.3 stands for halogen, alkyl or halogenoalkyl andR.sup.4 stands for halogen, alkyl or halogenoalykl.The intermediates of the formula ##STR2## are also new.Type: GrantFiled: March 21, 1989Date of Patent: September 25, 1990Assignee: Bayer AktiengesellschaftInventors: Klaus Wagner, Gerd Hanssler
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Patent number: 4954509Abstract: A compound, or a solvate or salt thereof, of formula (I): ##STR1## in which: RCO is an acyl group in which the group R contains a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic ring and R.sub.1 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 forms a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 --, group; R.sub.4 and R.sub.5, which may be the same or different and may be attached to the same or different carbon atoms of the isoquinoline nucleus, are each hydrogen, halogen, hydroxy, C.sub.1-6 alkyl, aryl, or R.sub.4 together with R.sub.5 form a --(CH.sub.2).sub.p -- group, where p is an integer of from 1 to 5 and one or more of the --(CH.sub.2)-- moieties is optionally substituted by a C.Type: GrantFiled: February 17, 1989Date of Patent: September 4, 1990Assignee: Dr. Lo. Zambeletti S.p.A.Inventors: Vittorio Vecchietti, Giuseppe Giardina
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Patent number: 4925840Abstract: The invention relates to novel 3-phenyl-4-cyanopyrrole derivatives of the general formula ##STR1## wherein X has the following meanings:A: hydrogen or CO--R.sub.1, wherein R.sub.1 is C.sub.1 -C.sub.6 alkyl which is unsubstituted or substituted by halogen or C.sub.1 -C.sub.3 alkoxy; or is C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, or C.sub.1 -C.sub.6 alkoxy which is unsubstituted or substituted by halogen or C.sub.1 -C.sub.3 alkoxy; or is C.sub.3 -C.sub.6 alkenyloxy, C.sub.3 -C.sub.6 cycloalkyl, or tetrahydrofur-2-yl;B: S--R.sub.2, wherein R.sub.2 is C.sub.1 -C.sub.3 haloalkyl;C: CH(Y)R.sub.3, wherein R.sub.3 is hydrogen or C.sub.1 -C.sub.8 haloalkyl and Y is hydroxy, halogen or OC(O)R.sub.4, wherein R.sub.4 is C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 haloalkyl, C.sub.2 -C.sub.6 alkenyl, or C.sub.1 -C.sub.6 alkoxycarbonyl; orD: CH.sub.2 --Z, wherein Z is the group ##STR2## wherein each of R.sub.7 and R.sub.8 independently of the other is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.Type: GrantFiled: August 3, 1988Date of Patent: May 15, 1990Assignee: Ciba-Geigy CorporationInventors: Robert Nyfeler, Josef Ehrenfraund
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Patent number: 4923861Abstract: Novel 6-[2-[2-(substituted amino)-3-quinolinyl]-ethenyl and ethyl]tetrahydro-4-hydroxypyran-2-ones and/or oxides and the corresponding dihydroxy ring opened acids and esters are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase) and are thus useful hypolipidemic and hypocholesterolemic agents.Type: GrantFiled: February 7, 1989Date of Patent: May 8, 1990Assignee: Warner-Lambert CompanyInventors: Joseph A. Picard, Drago R. Sliskovic
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Patent number: 4868300Abstract: Compounds of the formula ##STR1## wherein: z is O or I;X is ##STR2## a and b are 0, 1, or 2 and a+b=0, 1 or 2; R, R.sup.1, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each independently hydrogen, alkyl or aralkyl;R.sub.n is hydrogen, alkyl, aralkyl, acyl, carbalkoxy, carbamyl, carbalkoxyalkyl, hydroxyalkyl, alkoxyalkyl or amidino;R.sup.5 groups on vicinal carbon atoms may together form a carbon-carbon double bond when a or b=2;R groups on vicinal carbon atoms may together form a carbon-carbon double bond when R.sub.n is hydrogen and z=1;R.sup.4 and R.sup.5 geminal groups may together form a spiro substituent, --(CH.sub.2).sub.d --, where d is 2 to 5;R.sup.5 and R.sup.6 groups may together form a carbon-nitrogen double bond when R.sub.3 is hydrogen and a+b=1;R.sup.2 is hydrogen or --(CH.sub.2).sub.y --Y where y is 1-3;Y is hydrogen, --O--R.alpha., --S-R.alpha. or ##STR3## R.alpha. is hydrogen, alkyl, cycloalkyl or acyl; R.beta. is hydrogen or alkyl; andR.alpha. and R.beta.Type: GrantFiled: July 21, 1987Date of Patent: September 19, 1989Assignee: Rorer Pharmaceutical CorporationInventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt, William C. Faith, Bruce F. Molino
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Patent number: 4845118Abstract: The invention relates to compounds of the formula ##STR1## in which A represents ##STR2## T denotes --S--, --SO-- or --SO.sub.2 --, and R.sup.1 to R.sup.9 have the meanings given in the description, to a process for their preparation, to pharmaceutical compositions containing them, and to their use as inhibitors of gastric acid secretion.Type: GrantFiled: December 22, 1987Date of Patent: July 4, 1989Assignee: Hoechst AktiengesellschaftInventors: Hans-Jochen Lang, Robert Rippel, Andreas W. Herling, Klaus Weidmann
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Patent number: 4845094Abstract: 2-phenylbenzoxepin derivatives having a hypoglycemic activity, hypotensive activity, and platelet coagulation inhibiting activity, a process for production of the derivatives, and pharmaceutical compositions containing the derivatives.Type: GrantFiled: June 19, 1987Date of Patent: July 4, 1989Assignee: Suntory LimitedInventors: Toshio Tatsuoka, Kayoko Nomura, Fumio Satoh, Takafumi Ishihara, Seiji Miyano, Kunihiro Sumoto
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Patent number: 4831151Abstract: Compounds of the formula ##STR1## wherein the various substituents are defined hereinbelow and the pharmaceutically acceptable acid addition salts thereof, possess pharmacological properties. In particular, they possess antibacterial, antimycotic, protozoacidal and/or anthelmintic properties.Type: GrantFiled: April 21, 1986Date of Patent: May 16, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Helmut Link, Marc Montavon, Eva M. Karpitschka, Wilhelm Klotzer, Renate Mussner
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Patent number: 4826976Abstract: This invention relates to a color-shifted dye compounds containing at least one thermally unstable carbamate moiety which are useful in thermal imaging. These compounds may be represented by the formula [M--(X).sub.q ].sub.p D wherein M is a carbamate moiety; X is --N.dbd., --SO.sub.2 -- or --CH.sub.2 --; D taken with X and M represents the radical of a color-shifted organic dye, said carbamate moiety M comprising a tert-alkoxycarbonyl group, ##STR1## wherein R' is halomethyl or alkyl.Type: GrantFiled: December 18, 1987Date of Patent: May 2, 1989Assignee: Polaroid CorporationInventors: Alan L. Borror, Ernest W. Ellis, Donald A. McGowan
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Patent number: 4826836Abstract: Fungicidally active novel saccharine salts of aminomethyl heterocyclic compounds of the formula ##STR1## in which R represents optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted thienyl,R.sup.1 represents hydrogen or alkyl,R.sup.2 represents alkyl,R.sup.3 represents alkyl andR.sup.4 represents alkyl, alkenyl or alkinyl, orR.sup.3 and R.sup.4, together with the nitrogen atom to which they are bonded, represent an optionally substituted saturated heterocyclic radical which can contain further hetero atoms,X represents oxygen or sulphur,Y represents oxygen, sulphur or the methylene group,m represents 0 or 1 andn represents 0 or 1.Type: GrantFiled: November 5, 1987Date of Patent: May 2, 1989Assignee: Bayer AktiengesellschaftInventors: Joachim Weissmuller, Wolfgang Kramer, Paul Reinecke, Gerd Hanssler
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Patent number: 4818755Abstract: Cardiotonic fused aromatic bicyclic ring substituted thiazole compounds and their salts, methods for increasing cardiac contractility in humans and other mammals by the use of said compounds, pharmaceutical compositions including said compounds and methods for compound preparation.Type: GrantFiled: July 28, 1986Date of Patent: April 4, 1989Assignee: Rorer Pharmaceutical CorporatonInventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt, Bruce F. Molino
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Patent number: 4814345Abstract: Novel 1-phenyl-2-aminocarbonylindole compounds are disclosed having the general formula I ##STR1## wherein R.sub.1 is an aliphatic or aromatic acyl group or an optionally substituted benzyl group; R.sub.2 is hydrogen or a lower alkyl radical; R.sub.3 is a hydrogen, a halogen, a lower alkyl radical, or a lower alkoxy radical; R.sub.4 is hydrogen, a halogen, a lower alkyl radical, or a lower alkoxy radical; R.sub.5 has the significance given R.sub.3 ; R.sub.6 has the significance given for R.sub.4, or R.sub.6 is nitro or trifluoromethyl; R.sub.7 and R.sub.8 each represent hydrogen or a lower alkyl radical, or together with a nitrogen atom form a heterocyclic group; and Z signifies an alkylene chain optionally substituted by hydroxy or acyloxy. The compounds have pharmacological, in particular antiarrhythmic, properties.Type: GrantFiled: November 20, 1987Date of Patent: March 21, 1989Assignee: Kali-Chemie Pharma GmbHInventors: Heinrich-Wilhelm Ohlendorf, Wilhelm Kaupmann, Ulrich Kuhl, Gerd Buschmann, Stephen J. Magda
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Patent number: 4808718Abstract: Novel fused polycyclic and bridged compounds are disclosed which are useful as calcium entry blockers.Type: GrantFiled: May 6, 1986Date of Patent: February 28, 1989Assignee: Merck & Co., Inc.Inventors: George D. Hartman, Wasyl Halczenko, Brian T. Phillips
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Patent number: 4803198Abstract: New 1-phenyl-2-aminocarbonylindole compounds are described which have the general formula I ##STR1## where R.sub.1 is a hydrogen atom, or a lower alkyl, alkenyl, cycloalkylalkyl radical, R.sub.2 is a hydrogen atom or a lower alkyl radical, R.sub.3 is a hydrogen or halogen atom, or a lower alkyl, hydroxyl or lower alkoxy radical, R.sub.4 is a hydrogen or halogen atom, or a lower alkyl, hydroxyl or lower alkoxy radical, or, if R.sub.3 is a hydrogen atom, R.sub.4 may be a nitro or trifluoromethyl radical, or R.sub.3 and R.sub.4 together denote a methylenedioxy or ethylenedioxy radical, R.sub.5 has the meanings given for R.sub.3, R.sub.6 has the meanings given for R.sub.4, R.sub.7 is a hydrogen atom or, if R.sub.5 and R.sub.6 are lower alkoxy radicals, R.sub.7 may also be a lower alkoxy radical, R.sub.8 and R.sub.9 are each a hydrogen atom or a lower alkyl radical or, together with the nitrogen atom, form a heterocyclic group, and Z is an alkylene chain which is optionally substituted by hydroxyl.Type: GrantFiled: July 15, 1986Date of Patent: February 7, 1989Assignee: Kali-Chemie Pharma GmbHInventors: Heinrich-Wilhelm Ohlendorf, Wilhelm Kaupmann, Ulrich Kuehl, Gerd Buschmann, Stephen J. Magda
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Patent number: 4794116Abstract: Esters, acetal ethers, thioethers and nitrogen substituted derivatives of certain bicyclic compounds are disclosed which are useful as anti-allergic, anti-inflammatory and/or cytoprotective agents and in treatment of hyperproliferative skin disease. Pharmaceutical compositions and methods of treatment employing such compounds are also disclosed.Type: GrantFiled: July 22, 1987Date of Patent: December 27, 1988Assignee: Schering CorporationInventors: David J. Blythin, Ho-Jane Shue
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Patent number: 4777168Abstract: A class of bicyclic benzo-oxy heterocyclic ether and thioether compounds exhibiting parmacological activity, including anti-secretory and anti-ulcerogenic activity, pharaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.Type: GrantFiled: January 7, 1988Date of Patent: October 11, 1988Assignee: Rorer Pharmaceutical CorporationInventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt, Kent W. Neuenschwander
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Patent number: 4774246Abstract: Quinoline compounds having the formula: ##STR1## wherein R is a phenyl or substituted phenyl group or an aromatic heterocyclic group, R.sub.1 is a hydrogen or a carboxy-protecting group and Z is an amine group or an aliphatic heterocyclic group. The compounds have antibacterial activity.Type: GrantFiled: September 12, 1986Date of Patent: September 27, 1988Assignee: Abbott LaboratoriesInventor: Daniel T. Chu
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Patent number: 4772622Abstract: Novel diamino oxadiazoles, wherein one of the amine functions is connected to a basicly-substituted heterocyclic group through a linear or cyclic connecting group, which are useful for the suppression of gastric acid secretions in mammals. Compositions employing these compounds and processes for the preparation of such compounds from known N-cyano-S-methylisothiourea precursors by treatment with hydroxylamine and for alkylation of amine groups are also disclosed.Type: GrantFiled: June 16, 1986Date of Patent: September 20, 1988Assignee: Merck & Co., Inc.Inventors: Susan F. Britcher, William C. Lumma, Jr.
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Patent number: 4772706Abstract: An improved process for the preparation of 7-substituted amino-1-alkyl- or cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids is described where tetrafluorobenzoyl chloride is converted in three operations via 1-alkyl or 1-cycloalkyl-1,4-dihydro-6,7,8-trifluoro-4-oxoquinoline-3-carbonitrile which in a separate step or in situ is displaced and hydrolyzed to the desired product.Type: GrantFiled: January 13, 1986Date of Patent: September 20, 1988Assignee: Warner-Lambert CompanyInventors: James N. Wemple, James R. Zeller, John M. Domagala
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Patent number: 4767762Abstract: This invention relates to novel isoxazolo-naphthyridine, isoxazolo-quinoline, isothiazolo-naphthyridine, and isothiazolo-quinoline, derivatives having antibacterial properties.Type: GrantFiled: December 11, 1986Date of Patent: August 30, 1988Assignee: Abbott LaboratoriesInventor: Daniel T. Chu
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Patent number: 4766211Abstract: Chromogenic quinazolines of formula ##STR1## wherein R is an aryl radical or a heterocyclic radical,Z.sub.1 is oxygen or sulfur,Z.sub.2 is oxygen, sulfur or ##STR2## R' is hydrogen, alkyl which is unsubstituted or substituted by halogen, cyano or lower alkoxy, or is cycloalkyl, phenyl, benzyl, phenethyl or acyl, or --NRR' is a 5- or 6-membered heterocyclic radical,Q is an aliphatic radical which may be interrupted by a further member Z.sub.2,Y is the radical of a couplable compound, and the ringA is unsubstituted or substituted by halogen, cyano, nitro, lower alkyl, lower alkoxy or lower alkoxycarbonyl.These quinazolines are exceedingly fast to sublimation and are particularly suitable color formers in pressure-sensitive or heat-sensitive recording materials and give strong and lightfast yellow and orange colorations.Type: GrantFiled: August 27, 1986Date of Patent: August 23, 1988Assignee: Ciba-Geigy CorporationInventors: Rudolf Zink, Ian J. Fletcher
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Patent number: 4748182Abstract: This invention relates to aromatic 2-aminoalkyl derivatives of 1,2-benzoisothiazol-3(2H)one-1,1-dioxides, processes for the preparation of same, and to their use as anxiolytic and antihypertensive agents.Type: GrantFiled: March 5, 1986Date of Patent: May 31, 1988Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Marcel Hibert, Maurice W. Gittos
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Patent number: 4743609Abstract: This invention provides a class of new indole derivatives which are useful as medicinal compounds having a mild inhibitory effect on the gastric acid secretion as well as a remarkably cytoprotective effects on gastric muscosa, and which are represented by the general formula: ##STR1##Type: GrantFiled: February 10, 1986Date of Patent: May 10, 1988Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Masaaki Hosoi, Fumio Nakano, Kenji Matsuyama, Hiroshi Takeshita, Kenji Niiyama, Susumu Nakagawa
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Patent number: 4743601Abstract: There are disclosed novel compounds of the formula ##STR1## where X is hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, nitro or trifluoromethyl; R.sub.1 is hydrogen or loweralkyl; R.sub.2 is hydrogen, loweralkyl, arylloweralkyl or --(CH.sub.2).sub.m R.sub.7 wherein m is 1, 2 or 3 and R.sub.7 is cyano or amino; R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R.sub.5 and R.sub.6 are independently hydrogen or loweralkyl, or R.sub.5 +R.sub.6 taken together with the carbon atom to which they are attached constitute a cyclobutane, cyclopentane, cyclohexane, cycloheptane, pyrrolidine, piperidine, morpholine or thiomorpholine ring, or R.sub.5 is hydrogen and R.sub.6 is aryl or --CH.sub.2 OR.sub.8 wherein R.sub.8 is hydrogen, loweralkyl or loweralkylcarbonyl, which are useful for enhancing memory.Type: GrantFiled: July 13, 1987Date of Patent: May 10, 1988Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Karl Schonafinger, Helen H. Ong
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Patent number: 4731364Abstract: 2-Alkyl-, 2-alkenyl- and 2-alkynyl-2,3-dihydro-2-(1H-azolyl(C.sub.1 -C.sub.2)alkyl)benzo[b]thiophenes especially 2-alkyl-, 2-alkenyl- and 2-alkynyl-2,3-dihydro-3-hydroxy-2-(1H-1-imidazolylmethyl)-4-,5-,6- and 7-halobenzo[b]thiophenes and related derivatives having antifungal activity are disclosed. Pharmaceutical compositions comprising compounds of the invention and their use in treating fungal infections in susceptible hosts such as humans are also disclosed.Type: GrantFiled: August 12, 1985Date of Patent: March 15, 1988Assignee: Schering CorporationInventors: Dinanath F. Rane, Russell E. Pike
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Patent number: 4728647Abstract: Compounds of formula: ##STR1## in which V and W are H, halogen, alkyl (1-4C) or alkoxy (1-4C), amino, or acylamino,Z is phenyl, optionally substituted, thienyl, or pyridyl,R.sub.1 is alkyl (1-6C), alkoxyalkyl, cycloalkyl (3-6C), phenyl, phenylalkyl, or cycloalkylalkyl,R.sub.2 is alkyl (1-6C), alkoxyalkyl, cycloalkyl (3-6C), phenyl, phenylalkyl, cycloalkylalkyl, or morpholino, andNR.sub.1 R.sub.2 can also be pyrrolidino, optionally substituted piperidino, optionally substituted morpholino, thiomorpholino, optionally substituted piperazino, or an optionally substituted piperazinone, are useful as anxiolytic agents.Type: GrantFiled: May 28, 1986Date of Patent: March 1, 1988Assignee: Rhone-Poulenc SanteInventors: Jesus Benavides, Marie-Christine Dubroeucq, Gerard Le Fur, Christian Renault
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Novel antibacterial 7-amino-1(substituted cyclopropyl)-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids
Patent number: 4705788Abstract: Novel antibacterially active 7-amino-1-(substituted cyclopropyl)-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids of the formula ##STR1## in which X.sup.1 and X.sup.2 can be identical or different and represent hydrogen or halogen,R.sub.1, R.sub.2 and R.sub.3 represent hydrogen, methyl, chlorine or fluorine, the radicals R.sub.1 -R.sub.3 never all being identical, andR.sup.4 and R.sup.5, together with the nitrogen atom to which they are bonded, form a 5-membered or 6-membered heterocyclic ring which may be substituted.Type: GrantFiled: February 27, 1986Date of Patent: November 10, 1987Assignee: Bayer AktiengesellschaftInventors: Michael Schriewer, Klaus Grohe, Hans-Joachim Zeiler, Karl G. Metzger -
Patent number: 4692445Abstract: A class of bicyclic benzenoid 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: November 12, 1986Date of Patent: September 8, 1987Assignee: Rorer Pharmaceutical CorporationInventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt
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Patent number: 4673682Abstract: Isoquinoline-4-carboxylic acid derivatives of the formula I ##STR1## in which m, n, R.sup.1, R.sup.2, R.sup.3, A and X have the meansings indicated, and physiologically acceptable acid addition salts thereof, a process for their preparation, pharmaceutical formulations based on these compounds and the use thereof as antiarrythmic agents.Type: GrantFiled: September 7, 1983Date of Patent: June 16, 1987Assignee: Hoechst AktiengesellschaftInventors: Elmar Konz, Joachim Kaiser
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Patent number: 4672062Abstract: 3-amino-2,3-dihydro-1-benzoxepine compounds corresponding to the general Formula I ##STR1## wherein R.sub.1 and R.sub.2 may each be hydrogen, halogen, lower alkyl or lower alkoxy, or if one of R.sub.1 and R.sub.2 is hydrogen, the other may also be nitro or trifluoromethyl, R.sub.3 represents hydrogen or a lower alkyl group which optionally may be substituted by hydroxy, lower alnoxy, an optionally substituted phenyl group or an optionally substituted amino group, and R.sub.4 represents hydrogen or lower alkyl, or R.sub.3 and R.sub.4 together with the nitrogen atom form a 5 or 6 member heterocycle. The compounds exhibit pharmacological, especially antidepressive, activity.Type: GrantFiled: November 4, 1985Date of Patent: June 9, 1987Assignee: Kali-Chemie Pharma GmbHInventors: Heinrich-Wilhelm Ohlendorf, Michael Ruhland, Klaus-Ullrich Wolf
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Patent number: 4668673Abstract: A class of bicyclic benzo-oxy heterocyclic 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: July 2, 1986Date of Patent: May 26, 1987Assignee: William H. Rorer, Inc.Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt, Kent W. Neuenschwander
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Patent number: 4666920Abstract: Antibacterially effective 1,7-diamino-1,4-dihydro-4-oxo-3-(aza)quinolinecarboxylic acids of the formula ##STR1## in which A is nitrogen or C--R.sup.1,R.sup.1 is nitro or halogen,R.sup.2 and R.sup.3 each independently is C.sub.1 -C.sub.3 -alkyl, or together with the nitrogen atom to which they are bonded, form a 5-membered or 6-membered heterocyclic ring, which can additionally contain the atoms or groups --O--, --S--, --SO--, --SO.sub.2 -- or .dbd.N--R.sup.4 as a ring member and can optionally be mono-, di- or tri-substituted on the carbon atoms by C.sub.1 -C.sub.3 -alkyl, hydroxyl, alkoxy with 1-3 carbon atoms, amino, methylamino or ethylamino,R.sup.Type: GrantFiled: March 15, 1985Date of Patent: May 19, 1987Assignee: Bayer AktiengesellschaftInventors: Klaus Grohe, Hans-Joachim Zeiler, Karl G. Metzger
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Patent number: 4665202Abstract: The invention relates to pharmaceutical preparations containing compounds of formula I ##STR1## in which X.sub.1 and X.sub.2, independently of each other, represent hydrogen, halogen, unsubstituted or substituted amino or a quaternary ammonium salt; etherified or esterified hydroxy; free, etherified, esterified or oxidized mercapto; nitro; functionally modified formyl; free or functionally modified carboxyl; acyl; an unsubstituted or substituted hydrocarbon radical, or an unsubstituted or substituted heterocyclic radical; with the proviso that at least one of the radicals X.sub.1 and X.sub.2 is bonded by a carbon atom to the ring system and with the proviso that X.sub.1 and X.sub.2 cannot be together halogen and formyl; in which Y represents oxygen, sulfur, sulfinyl or sulfonyl but must be sulfur, sulfinyl or sulfonyl, if X.sub.1 is hydrogen and X.sub.Type: GrantFiled: August 24, 1984Date of Patent: May 12, 1987Assignee: Zyma SAInventors: Christian G. Rimbault, Philippe M. Narbel
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Patent number: 4659708Abstract: The subject 8-[6-(N-heterocyclic-substituted)hexylamino]-6-methoxy lepidine erivatives have the formula: ##STR1## wherein Z represents methyl or, together with the two contiguous carbon atoms, the benzo moiety of a benzopiperazinyl derivative when Y is --N(R')--, n is an integer from 0 to 2; Y represents --O--, --S--, --S(O)--, --S(O).sub.2 --, and --N(R')--; R' represents hydrogen, alkyl, lower alkyl, R" substituted lower alkyl, cycloalkyl, aryl, sulfonyl, saturated 1,4-diazepinyl, lower alkyl N-cyanocarboximidothioate, or --C(O)R'"; R" represents at least one of hydroxy, alkoxy, aralkoxy, amino, lower alkyl substituted amino, phenyl, halogenated phenyl, or sufonyl; and R'" represents lower alkyl, alkoxy, aralkoxy, amino, lower alkyl substituted amino or aryl substituted amino; and pharmaceutically acceptable salts thereof. These derivatives afford improvement in means for the chemotherapy of leishmaniasis when administered parenterally or orally to infected animals.Type: GrantFiled: August 20, 1981Date of Patent: April 21, 1987Assignee: The United States of America as represented by the Secretary of the ArmyInventors: Leslie M. Werbel, Edgar A. Steck
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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