Additional Ring Containing Patents (Class 546/337)
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Patent number: 4895847Abstract: Novel 2,3-dihydro-1H-indene derivatives and salts thereof represented by the general formula (1), ##STR1## [wherein R.sup.1 and R.sup.2 are each a hydrogen atom, a lower alkyl group, a phenyl group which may have halogen atoms and/or alkyl groups as the substituents on the phenyl ring; R.sup.3 is a halogen atom or a lower alkyl group; R.sup.4 is a hydrogen atom, a halogen atom, a phenyl-lower alkyl group, a cycloalkyl-lower alkyl group or the like; R.sup.5 is a hydroxyimino group, an alkylamino group or a group of the formula --NHR.sup.8 (wherein R.sup.8 is a hydrogen atom, a halogen-substituted lower alkanoyl group or the like); R.sup.6 is a hydrogen atom or a phenyl group; and R.sup.7 is a hydrogen atom or a lower alkyl group].Type: GrantFiled: September 21, 1988Date of Patent: January 23, 1990Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Yasuo Oshiro, Hiraki Ueda, Kazuyuki Nakagawa
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Patent number: 4889865Abstract: Mono, di and tri-esters of 1,8-dihydroxy-10-phenyl-9-anthrone or -9-anthranol have the formula ##STR1## wherein p is 0 or 1,(a) when p=0, t=1 and R.sub.2 represents hydrogen or --COR.sub.3,(b) when p=1, t=0 and R.sub.1 and R.sub.2 each independently represent hydrogen or --COR.sub.3,R.sub.3 represents linear or branched alkyl having 1-17 carbon atoms, cycloalkyl, phenyl or phenyl substituted by lower alkyl, lower alkoxy, halogen, a nitro function, --CF.sub.3 or a hydroxyl function, and mixtures of said esters. These esters are prepared by reacting 1,8-dihydroxy-10-phenyl-9-anthrone with an activated form of an acid. The esters are useful in human or veterinary medicine and in cosmetic compositions.Type: GrantFiled: February 21, 1989Date of Patent: December 26, 1989Assignee: Centre International de Recherches Dermatologiques C.I.R.D.Inventors: Braham Shroot, Gerard Lang, Jean Maignan, Serge Restle, Christopher Hensby, Michel Colin
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Patent number: 4886822Abstract: A substituted anilide derivative of the formula ##STR1## wherein R.sub.1 represents a mononuclear or binuclear heterocyclic group which contains 1 to 3 nitrogen atoms as ring members and may have a substituent.A represents a single bond, a carbonyl group, a sulfur atom, or a lower alkylene group which may be substituted by a hydroxyl group,R.sub.2 represents a hydrogen atom, a halogen atom, a lower alkyl group, a trifluoromethyl group, a lower alkenyloxy group, or a C.sub.1 -C.sub.14 alkoxy group which may have a substituent,R.sub.3 and R.sub.4 are identical or different, and each represents a hydrogen atom, a lower alkyl group, a phenyl group, or a phenyl(lower alkyl) group which may have a substitutent, or taken together, may form a saturated nitrogen-containing heterocyclic group together with the nitrogen atom to which they are bonded, andB represents a single bond or a lower alkylene group which may have a substituent,or an acid addition salt thereof.Type: GrantFiled: April 8, 1988Date of Patent: December 12, 1989Assignee: Kowa Company, Ltd.Inventors: Kimiyuki Shibuya, Yoshio Takahashi, Seiichi Sato, Hiromichi Shigyo, Tomio Ohta, Yasumi Uchida
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Patent number: 4876343Abstract: An improved process for the preparation of statine, the phenyl analog of statine, the cyclohexyl analog of statine and derivatives thereof is described, as well as other valuable intermediates used in the process.Type: GrantFiled: June 15, 1988Date of Patent: October 24, 1989Assignee: Warner-Lambert CompanyInventors: John C. Hodges, Sylvester Klutchko
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Patent number: 4863936Abstract: Various substituted aminoalkylamino-2-pyridine derivatives are disclosed which are useful as histamine H.sub.1 -antagonists.Type: GrantFiled: October 21, 1986Date of Patent: September 5, 1989Assignee: Smith Kline & French Laboratories LimitedInventor: George S. Sach
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Patent number: 4841059Abstract: Antibacterially active new 1,8-bridged 4-quinolone-3-carboxylic acid derivatives of the formula ##STR1## in which Y is carboxyl or a derivative thereofR.sup.1, R.sup.2, R.sup.3, R.sup.4, X.sup.1, X.sup.2 and X.sup.5 are H or various radicals,Z is O, NH, substituted NH, ##STR2## m and n are 0 or 1, andA, B, D, and E are CH or substituted C or up to three of them are N,and physiologically acceptable salts thereof. Novel intermediates are described as well as processes for making the intermediates and end products.Type: GrantFiled: October 15, 1987Date of Patent: June 20, 1989Assignee: Bayer AktiengesellschaftInventors: Michael Schriewer, Klaus Grohe, Hans-Joachim Zeiler, Karl G. Metzger
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Patent number: 4837316Abstract: Alkylamide derivatives having the formula, These compounds have a strong antiulcer action depend on histamine H.sub.2 -receptor antagonistic action and a cytoprotective action upon gastric mucous membrance.Type: GrantFiled: August 27, 1986Date of Patent: June 6, 1989Assignee: Fujirebio Kabushiki KaishaInventors: Yasuo Sekine, Nobuhiro Hirakawa, Noriaki Kashiwaba, Tetsuaki Yamaura, Hisako Harada, Teruo Kutsuma, Hajime Matsumoto, Akihiro Sekine, Yoshikazu Isowa
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Patent number: 4826531Abstract: Acrylic acid derivatives having the formula (I): ##STR1## and stereoisomers thereof, wherein W is R.sup.1 O.sub.2 C--C.dbd.CH--ZR.sup.2, R.sup.1 and R.sup.2 are alkyl or fluoroalkyl groups, and Z is oxygen or sulphur; A, B, D and E are hydrogen, halogen, hydroxy or optionally substituted alkyl, alkoxy, aralkyl, arylalkoxy, alkenyl, alkynyl, aryl, aryloxy, arylthio, heteroaryloxy, heteroarylthio, acyloxy, amino, arylazo or acylamino, nitro, cyano, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --CR.sup.3 .dbd.NR.sup.4, --N.dbd.CR.sup.3 R.sup.4 or --S(O).sub.n R.sup.3 groups; any two of the groups A, B, D and E, when they are in adjacent positions on the ring, optionally join to form a fused ring, n is 0, 1 or 2; and R.sup.3 and R.sup.4 are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl or optionally substituted aryl or aralkyl; and metal complexes thereof. These compounds are useful as fungicides, insecticides, nematicides or plant growth regulators.Type: GrantFiled: April 17, 1987Date of Patent: May 2, 1989Assignee: Imperial Chemical Industries PLCInventors: Vivienne M. Anthony, John M. Clough, Paul DeFraine, Christopher R. A. Godfrey, Patrick J. Crowley, Kenneth Anderton
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Patent number: 4808750Abstract: Novel fluorophenoxyphenoxypropionates and derivatives thereof possess herbicidal activity selectively in the presence of broadleaf crops. Preemergent and postemergent applications are contemplated.Type: GrantFiled: July 14, 1986Date of Patent: February 28, 1989Assignee: The Dow Chemical CompanyInventors: Richard B. Rogers, B. Clifford Gerwick, III
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Patent number: 4798893Abstract: A method for the synthesis of the 2-propanone (I) is described starting from alkoxide (II) through the lactone (IV). ##STR1## Excellent control of the location of the substitution on the phenyl ring is achieved and the reaction proceeds in high yield.Type: GrantFiled: September 21, 1987Date of Patent: January 17, 1989Assignee: McNeilab, Inc.Inventors: David A. Cherry, Cynthia A. Maryanoff, John E. Mills, Roy A. Olofson, James D. Rodgers
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Patent number: 4797411Abstract: The invention relates to cycloalkyl-substituted 4-pyridyl derivatives of formula (I) ##STR1## wherein R is C.sub.1 -C.sub.4 alkyl;each of R.sub.1 and R.sub.2 is, independently, hydrogen or C.sub.1 -C.sub.4 alkyl;n is an integer of 1 to 5; and either(a) A is >C.dbd.O and B is --O--, --NH-- or --CH.sub.2 --; or(b) A is --CH.sub.2 --and B is --O--, --NH--, --CH.sub.2 -- or >C.dbd.O; or(c) A is --O-- and B is >C.dbd.O or --CH.sub.2 --; or(d) A is --NH-- and B is >C.dbd.O or --CH.sub.2 --,and their pharmaceutically acceptable salts.The compounds of the invention show aromatase inhibiting activity and can be useful, e.g., in treating hormone-dependent tumors and prostatic hyperplasia.Type: GrantFiled: July 13, 1987Date of Patent: January 10, 1989Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Angelo Crugnola, Enrico di Salle, Paolo Lombardi
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Patent number: 4794197Abstract: All-cis-1,3,5-Triamino-2,4,6-trihydroxycyclohexane derivatives corresponding to the general formula I ##STR1## wherein the symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are identical or different and represent hydrogen atoms, alkyl groups or --CO-alkyl groups wherein the alkyl in the alkyl or --CO-alkyl group has 1 to 18 carbon atoms and the alkyl and --CO-alkyl groups may contain, independently of one another, one or more identical or different functional groups, and at least one of the groups R.sub.1 to R.sub.6 is one of the above mentioned unsubstituted or substituted alkyl groups or --CO-alkyl groups, and their salts with pharmacologically conventionally used inorganic or organic acids and their quaternary ammonium salts, processes for their preparation and their use, and pharmaceutical preparations containing these compounds.Type: GrantFiled: January 31, 1986Date of Patent: December 27, 1988Inventors: Walter Schneider, Isidor Erni, Hans K. Hegetschweiler
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Patent number: 4794121Abstract: Alkylcarboxamides of pyridylalkylamines, useful in human and verterinary medicine, correspond to the general formula I: ##STR1## wherein n=0 or 1,R.sub.3 represents an alkyl group of C.sub.1 to C.sub.3 or a hydrogen atom,R.sub.1 represents a hydrogen atom,R.sub.2 represents a group: ##STR2## in which: X and Y are different,X and Y each represent a linear or branched saturated or unsaturated hydrocarbon chain comprising from 1 to 16 carbon atoms;X and Y together determine a saturated or unsaturated cyclic radical substituted or not comprising from 3 to 12 carbon atoms.Type: GrantFiled: September 18, 1986Date of Patent: December 27, 1988Assignee: PanmedicaInventors: Claude Laruelle, Marcel Lepant, Bernard Raynier
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Patent number: 4788130Abstract: Novel 2,3-dihydro-1H-indene derivatives and salts thereof represented by the general formula (1), ##STR1## [wherein R.sup.1 and R.sup.2 are each a hydrogen atom, a lower alkyl group, a phenyl group which may have halogen atoms and/or alkyl groups as the substituents on the phenyl ring; R.sup.3 is a halogen atom or a lower alkyl group; R.sup.4 is a hydrogen atom, a halogen atom, a phenyl-lower alkyl group, a cycloalkyl-lower alkyl group or the like; R.sup.5 is a hydroxyimino group, an alkylamino group or a group of the formula --NHR.sup.8 (wherein R.sup.8 is a hydrogen atom, a halogen-substituted lower alkanoyl group or the like); R.sup.6 is a hydrogen atom or a phenyl group; and R.sup.7 is a hydrogen atom or a lower alkyl group].Type: GrantFiled: August 29, 1985Date of Patent: November 29, 1988Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Yasuo Oshiro, Hiraki Ueda, Kazuyuki Nakagawa
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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: 4777286Abstract: Process and compounds for producing intermediates for the production of renin inhibitors.Type: GrantFiled: June 18, 1985Date of Patent: October 11, 1988Assignee: The Upjohn CompanyInventor: Heinrich J. Schostarez
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Patent number: 4769466Abstract: Compounds are provided of the following general structure: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are independently selected from hydrogen or methyl; A is amino, C.sub.1 -C.sub.4 monoalkylamino, C.sub.2 -C.sub.8 dialkylamino, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl or cyclopropylamino; and where W and Q are independently selected from 2-pyridinyl, 3-pyridinyl or 4-pyridinly or phenyl, provided W and Q are not both phenyl.Type: GrantFiled: February 6, 1987Date of Patent: September 6, 1988Assignee: Pennwalt CorporationInventors: Ronald C. Griffith, James J. Napier
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Patent number: 4767865Abstract: The present invention provides novel 3'-pyridinylalkenylindole-2-carboxylic acids and derivatives thereof of the formula I and II ##STR1## which are useful as thromboxane A.sub.2 (TXA.sub.2) synthetase inhibitors and as such represent potent pharmacological agents.Type: GrantFiled: June 29, 1987Date of Patent: August 30, 1988Assignee: The Upjohn CompanyInventors: Roy A. Johnson, Chiu-Hong Lin
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Patent number: 4766132Abstract: Compounds of formula: ##STR1## and stereoisomers thereof, wherein R.sup.1 is unsubstituted or substituted aryl or heteroaryl; R.sup.2 is H, alkyl, alkenyl or alkynyl; X is O, NH, or S; R.sup.3 being alkyl, alkenyl, alkynyl or COR.sup.4 where R.sup.4 has an R.sup.3 value, when X is O; R.sup.3 being --CO-- alkyl when X is NH; and R.sup.3 being alkyl, alkenyl or CSNR.sup.5 R.sup.6 where R.sup.5 and R.sup.6, which may be the same or different, are H, alkyl, alkenyl or, together with the adjacent N atom, constitute a ring, when X is S; or XR.sup.3 together represent --CN; and salts and metal complexes thereof, have fungicidal and plant growth regulating activity.Type: GrantFiled: January 29, 1986Date of Patent: August 23, 1988Assignee: Imperial Chemical Industries PLCInventor: Ian T. Kay
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Patent number: 4758573Abstract: Compounds of the general formula ##STR1## and pharmaceutically acceptable salts thereof have antithrombotic activity. Het represents 1-[1H-imidazolyl], 1-N-morpholinyl or pyridyl. A representative compound is 6-[2-(1H-Imidazol-1-yl)-1-yl-1-[[(4-methoxyphenyl)methoxy]methyl]ethoxy]he xanoic acid.Type: GrantFiled: February 3, 1986Date of Patent: July 19, 1988Assignee: G. D. Searle & Co.Inventors: Paul W. Manley, Lai M. Fook
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Patent number: 4753674Abstract: There are disclosed a herbicidal composition containing, as an active ingredient, a phenoxyalkylamide derivative represented by the formula ##STR1## wherein X, n, Y, Z, R.sup.1, R.sup.2 and R.sup.3 have the same meanings as defined in the specification, and a method for controlling weeds by the use of the same. The herbicidal composition according to this invention shows a superior weed-killing activity by pre- and post-emergence treatment in soil.Type: GrantFiled: February 13, 1984Date of Patent: June 28, 1988Assignee: UBE Industries, Ltd.Inventors: Tetsuo Takematsu, Yasutomo Takeuchi, Mitsuaki Takenaka, Seiji Takamura, Minoru Nishimura, Tatsuo Okada, Yasuhisa Fukuda
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Patent number: 4743603Abstract: New derivatives of 2-(3-pyridyl)-2-phenylaminoacetic acid, of the formula: ##STR1## with: R.sub.0 : --CN, --COOH, CONH.sub.2, COOR.sub.4,R.sub.1 : H, lower alkyl, cycloalkyl, phenyl, if appropriate substituted, aralkyl if appropriate substituted,R.sub.2 : H, lower alkyl, if appropriate substituted,Ar: phenyl if appropriate substituted,Z: halogen, lower alkyl, lower alkoxy, lower alkylthio.They can be employed in agriculture for combating phytopathogenic fungi such as the sclerotiniaceae.Type: GrantFiled: May 27, 1986Date of Patent: May 10, 1988Assignee: Rhone-Poulenc AgrochimieInventor: Jean P. Bulot
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Patent number: 4743610Abstract: N-[.omega.(3-pyridinyl)alkyl]benzamides which are useful as inhibitors of thromboxane synthetase enzyme and/or as cardioprotective agents in the prevention of myocardial infarction.Type: GrantFiled: March 16, 1987Date of Patent: May 10, 1988Assignee: American Cyanamid CompanyInventors: William B. Wright, Jr., Andrew S. Tomcufcik
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Patent number: 4735959Abstract: There are described novel carboxylic acid derivatives of the formula ##STR1## and derivatives of the formula ##STR2## and the addition salts thereof, which exhibit an effect on the intermediary metabolism. Furthermore, the compounds of Formula Ia as well as the compounds of Formula I possess blood-sugar lowering properties.Type: GrantFiled: May 14, 1985Date of Patent: April 5, 1988Assignee: Dr. Karl Thomae GmbHInventors: Wolfgang Grell, Gerhart Griss, Robert Sauter, Rudolf Hurnaus, Eckhard Rupprecht, Nikolaus Kaubisch, Joachim Kahling, Bernhard Eisele
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Patent number: 4731373Abstract: Glycerine derivatives of the formula ##STR1## wherein the residues R.sup.1, R.sup.2 and R.sup.3 have the significance given in the description,and their hydrates, which inhibit blood platelet activating factor (PAF), are descried.Type: GrantFiled: December 10, 1984Date of Patent: March 15, 1988Assignee: Hoffman-La Roche Inc.Inventors: Richard Barner, Kasper Burri, Jean-Marie Cassal, Paul Hadvary, Georges Hirth, Klaus Muller
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Patent number: 4730053Abstract: The present invention is related to new S-(Carbamoyl-phenylselenyl) derivatives of mercaptanes of the general formula (I) ##STR1## and to a process for the treatment of diseases caused by cell injury due to the increased formation of active oxygen metabolites.Type: GrantFiled: November 25, 1985Date of Patent: March 8, 1988Assignee: A. Nattermann & Cie GmbHInventors: Norbert Dereu, Albrecht Wendel, Helmut Sies, Sigurd Leyck, Axel Romer, Erich Graf
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Patent number: 4725602Abstract: Acetylenes of the following formula (I): ##STR1## wherein Y, m, R.sup.1, R.sup.2, R.sup.3, n and R.sup.4 are defined herein and R.sup.5 is hydrogen, alkyl, cycloalkyl or substituted alkyl are useful vasodilators and antihypertensives.Type: GrantFiled: October 24, 1985Date of Patent: February 16, 1988Assignee: McNeilab, Inc.Inventor: John R. Carson
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Patent number: 4716175Abstract: Certain substituted amides of saturated fatty acids are potent inhibitors of the enzyme acyl-CoA:cholesterol acyltransferase and are thus useful agents for inhibiting the intestinal absorption of cholesterol.Type: GrantFiled: February 24, 1987Date of Patent: December 29, 1987Assignee: Warner-Lambert CompanyInventors: Milton L. Hoefle, Ann Holmes, Bruce D. Roth
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Patent number: 4696930Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 is --alkylene'-13 NH.sub.2 or --alkylene'--A'; R.sub.2, R.sub.3 and R.sub.4 are independently hydrogen or methyl; A and A' are, independently, unsubstituted or lower alkyl or aryl substituted pyridinyl, imidazolyl, or pyrimidinyl; and when, an asymmetric carbon is present, enantiomers thereof, or racemic mixtures thereof; or pharmaceutically acceptable salts thereof, are described. These compounds are useful as antiarrhythmic agents.Type: GrantFiled: April 12, 1985Date of Patent: September 29, 1987Assignee: Hoffmann-La Roche Inc.Inventors: John G. Mullin, Jr., Keiji Nakamura, Jefferson W. Tilley, Hiroshi Watanabe
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Patent number: 4684733Abstract: An improved process for the preparation of certain antiarrhythmic agents in which a carbon atom of a piperidine or pyrrolidine ring is bonded directly or through a methylene group to the nitrogen of a substituted benzamido group from bromo- or hydroxy-substituted benzenes.Type: GrantFiled: July 28, 1986Date of Patent: August 4, 1987Assignee: Riker Laboratories, Inc.Inventor: Charles M. Leir
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Patent number: 4683239Abstract: Octahydroindolizine compounds of formula (I): ##STR1## wherein Q is --NR--, --(CH.sub.2).sub.z --, --CH.dbd.CH--, --C.tbd.C--, --OCH.sub.2 --, --SCH.sub.2 --, --SO.sub.2 --, --SO--, --CO--, or an oxygen or a sulfur atom and where R, R.sup.1 and R.sup.2 are substituents such as alkyl and x, y and z are independently the integers 0-3. Also, pharmaceutical compositions containing (I), intermediates and methods for treating pain.Type: GrantFiled: April 10, 1986Date of Patent: July 28, 1987Assignee: McNeilab, Inc.Inventors: Richard J. Carmosin, John R. Carson
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Patent number: 4675328Abstract: Polycyclic salts of the formulaA-XN+CH.sub.2 --(Y).sub.n --(CH.sub.2).sub.p --(Z).sub.q --L--(T).sub.r --M IwhereinA.sup.- is the anion of a strong organic or inorganic acid;XN.sup.+ is pyridinium, pyrimidinium, thiazolium or imidazolium substituted by R.sup.1, R.sup.2 and R.sup.3 ;n, q and r individually are the integer 1 or 0 and p is an integer from 1 to 15;Y is CH.sub.2, C(H,OH) or C(O):Z is O, S, CH.sub.2, C(O), NQ.sup.1, SO.sub.2, C(O)O, OC(O), C(O)N(Q.sup.1) or N(Q.sup.1)C(O);L is p-phenylene substituted by R.sup.4 ; andM is phenyl substituted by R.sup.5 and R.sup.6,T has one of the meanings given above, for Z or is C(CH.sub.3).sub.2, C.sub.2 H.sub.4, C(Q.sup.2).dbd.C(Q.sup.3), C.tbd.C, CH.sub.2 C(O), C(O)CH.sub.2, CH.sub.2 O or OCH.sub.2,R.sup.1 is a group Ar, Ar-C.sub.1-4 -alkyl, ArO or ArC(O),Ar is phenyl substituted by R.sup.7, R.sup.8 and R.sup.9 ;R.sup.2 and R.sup.3 individually are H, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy or C.sub.6 H.sub.Type: GrantFiled: January 15, 1986Date of Patent: June 23, 1987Assignee: Hoffmann-LaRoche Inc.Inventors: Jean-Marie Cassal, Albrecht Edenhofer, Henri Ramuz
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Patent number: 4663333Abstract: The compounds of this invention are acylaminoalkylpyridines representd by the formula ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein n, m and p are independently an integer of from 1 to 8 provided n+m+p is equal to or less than 10; X is thio, sulfinyl or sulfonyl; Alk.sub.1 is straight or branched chain lower alkylene of 1 to 6 carbon atoms, R.sub.3 is lower alkyl, Alk.sub.2 is straight or branched chain alkylene of 1 to 4 carbon atoms; R.sub.4 is selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl and lower alkoxy; and the pharmaceutically acceptable salts thereof. The compounds of the present invention are useful in the treatment of inflammation, allergy and hypersensitivity reactions and other disorders of the immune system.Type: GrantFiled: December 20, 1985Date of Patent: May 5, 1987Assignee: G. D. Searle & Co.Inventors: Richard A. Mueller, Richard A. Partis, James R. Deason
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Patent number: 4636505Abstract: Acylanilides of the formula ##STR1## wherein R.sup.1 and R.sup.2, the same or different, each is cyano, carbamoyl, nitro, halogeno, perfluoroalkyl or other defined substituents;R.sup.3 is hydrogen or halogen;R.sup.4 is hydrogen or alkyl, or is joined to R.sup.5 ;R.sup.5 is hydrogen, hydroxy, alkoxy or acyloxy or is joined to R.sup.4 ;R.sup.6 is alkyl or halogenoalkyl, or has the formula --A.sup.3 --R.sup.8 or --A.sup.4 --X.sup.2 --A.sup.5 --R.sup.9 ;A.sup.1 and A.sup.4, the same or different, each is alkylene;A.sup.2, A.sup.3 and A.sup.5, the same or different, each is a direct link or alkylene;X.sup.1 and X.sup.2, the same or different, each is oxygen, sulphur, sulphinyl, sulphonyl, imino or alkylimino;R.sup.7 and R.sup.9, the same or different, each is alkyl, alkenyl, hydroxyalkyl, cycloalkyl, phenyl optionally substituted, naphthyl or heterocyclic optionally substituted;and R.sup.8 is phenyl, naphthyl or heterocyclic as defined above for R.sup.7 or R.sup.Type: GrantFiled: July 15, 1983Date of Patent: January 13, 1987Assignee: Imperial Chemical Industries PLCInventor: Howard Tucker
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Patent number: 4622339Abstract: Norbornane- and norbornene-carboxylic acid amides of the formula ##STR1## in which ##STR2## represents the part structure ##STR3## A represents a ##STR4## or --CH.sub.2 --CH.sub.2 -- group, R.sup.1 and R.sup.2 each independently is hydrogen or an alkyl radical with 1-6 carbon atoms,R.sup.3 is alkyl or alkenyl which has 1-8 carbon atoms and is optionally substituted by halogen or alkyl with 1 or 2 carbon atoms, cycloalkyl or cycloalkeny wtih 3 to 7 carbon atoms, an aromatic radical which has 6 or 10 carbon atoms and and is optionally substituted by halogen, by alkyl with 1 or 2 carbon atoms or by halogenoalkyl with 1 or 2 carbon atoms, or is a five-membered or six-membered heteroaromatic radical,R.sup.4 is hydrogen or a hydroxyl group,R.sup.5 and R.sup.6 each independently is hydrogen or alkyl with 1 to 4 carbon atoms, andn is a number from 2 to 6,and, if R.sup.1 is hydrogen, also physiologically acceptable salts thereof, perform as thromboxan antagonists.Type: GrantFiled: January 11, 1985Date of Patent: November 11, 1986Assignee: Bayer AktiengesellschaftInventors: Folker Lieb, Hermann Oediger, Hans-Joachim Kabbe, Ulrich Niewohner, Elisabeth Perzborn, Friedel Seuter
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Patent number: 4558150Abstract: Intermediates of the formula ##STR1## are disclosed. These compounds are useful in the preparation of amino thiol dipeptides possessing angiotensin converting enzyme inhibition activity and enkephalinase inhibition activity.Type: GrantFiled: December 10, 1984Date of Patent: December 10, 1985Assignee: E. R. Squibb & Sons, Inc.Inventors: Eric M. Gordon, Jollie D. Godfrey, Jr.
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Patent number: 4520027Abstract: The invention concerns novel esters of 4-(1-hydroxy-2-[(acylamino)alkylamino]ethyl)phenols of the formula: ##STR1## and salts thereof, wherein R.sup.1 and R.sup.2 are (3-5C)alkyl, R.sup.3 and R.sup.4 are hydrogen or methyl, A is a direct bond or methylene, and Q is various heteroaromatic containing groups. The esters possess topical anti-inflammatory properties and the invention provides pharmaceutical compositions containing the esters and processes for their chemical manufacture.Type: GrantFiled: December 23, 1982Date of Patent: May 28, 1985Assignee: Imperial Chemical Industries PLCInventors: Peter R. Marsham, David S. Thomson
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Patent number: 4503232Abstract: The invention provides a novel method for the preparation of an .alpha.-ketoamide imine having a characteristic structure expressed by the formula ##STR1## in which R is a group such as an alkyl, aryl or the like group, in a one-step reaction in which a halogen-containing organic compound reacts with a primary amine and carbon monoxide in the presence of a carbonylation catalyst. The product compound is useful as an intermediate for the synthesis of various kinds of organic compounds including medicines and agricultural chemicals.Type: GrantFiled: September 24, 1982Date of Patent: March 5, 1985Assignee: Agency of Industrial Science & TechnologyInventors: Toshiaki Kobayashi, Masato Tanaka
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Patent number: 4501746Abstract: Novel N,N-disubstituted carboxamide derivatives useful as herbicides, fungicides and aquatic plant growth regulators.Type: GrantFiled: September 15, 1982Date of Patent: February 26, 1985Assignee: Eli Lilly and CompanyInventor: Eriks V. Krumkalns
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Patent number: 4500714Abstract: Benzamide derivatives of the formula: ##STR1## wherein R.sub.1 is a hydrogen atom, a methyl group or a methoxy group; R.sub.2 is a straight-chain or branched-chain alkyl group having 2 to 8 carbon atoms, a substituted phenyl group, or group --NHR.sub.4, R.sub.4 being a hydrogen atom, a straight-chain or branched-chain or cyclic alkyl group having 1 to 6 carbon atoms, or a phenyl group that may have a substituent on the nucleus; R.sub.3 is a hydrogen atom or one or two alkyl groups having 1 to 4 carbon atoms and n is 0 or 1, a process for preparing these derivatives, and pharmaceutical compositions containing the same are provided.The compounds of the above formula have the action to reduce the blood glucose level and, therefore, are useful as medicines.Type: GrantFiled: October 7, 1982Date of Patent: February 19, 1985Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Masamitsu Honda, Hideaki Nagai, Shoko Takishima, Akinori Kawamura, Noriko Kawamura, Takashi Dan, Masuo Koizumi, Yasushi Murakami, Yoshikazu Hinohara, Hideki Nakano, Yoshio Takagaki
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Patent number: 4486593Abstract: The present invention provides novel 2-, 3-, or 4-pyridinylmethylamino arylic acids which are useful as thromboxane A.sub.2 (TXA.sub.2) synthetase inhibitors and 5-lipoxygenase inhibitors and as such represent useful pharmacological agents.Type: GrantFiled: January 19, 1983Date of Patent: December 4, 1984Assignee: The Upjohn CompanyInventor: Chiu-Hong Lin
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Patent number: 4486598Abstract: Novel compounds of the following general formula: ##STR1##Type: GrantFiled: February 22, 1982Date of Patent: December 4, 1984Assignee: The Upjohn CompanyInventor: Paul A. Aristoff
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Patent number: 4460580Abstract: The invention relates to novel N-alkylated aminoalcohols of the formula ##STR1## in which Ar is a radical of aromatic character which is unsubstituted or substituted by hydroxyl, n has the values nought or 1 and Alk is an alkylene radical having 2 to 5 carbon atoms and the nitrogen atom and the oxygen atom or, if n is nought, the salicylamide radical are separated from one another by at least two carbon atoms in the straight-chain, and their salts. The main action of the novel compounds consists in a stimulation of cardiac .beta.-receptors; the compounds also effect a blockage of adrenergic .alpha.-receptors and a lowering in the blood pressure. They can therefore be used as .beta.-stimulators, especially as agents having a positively inotropic action for the treatment of cardiac insufficiency.Type: GrantFiled: June 24, 1982Date of Patent: July 17, 1984Assignee: Ciba-Geigy CorporationInventors: Franz Ostermayer, Markus Zimmermann
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Patent number: 4454324Abstract: An improved process for the preparation of 4-methoxy-2'-{2-(1-methyl-2-piperidyl)ethyl}benzanilide has been developed. The process comprises essentially three steps starting with methyl anthranilate and 2-picoline and features a novel low-pressure hydrogenation sequence.Type: GrantFiled: April 1, 1983Date of Patent: June 12, 1984Assignee: Mead Johnson & CompanyInventor: Gary D. Madding
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Patent number: 4423222Abstract: Suitably substituted 2-aminomethyl pyridines and suitably substituted 2-pyridinylcarbinols are reacted with 3-(2,2-dichloroethenyl)-2,2-dimethylcyclopropane carboxoyl chloride in an inert solvent to form a group of biologically active organic compounds. These compounds are active as fungicides, herbicides, or both.Type: GrantFiled: May 21, 1982Date of Patent: December 27, 1983Assignee: The Dow Chemical CompanyInventors: Mary L. Ash, Richard G. Pews
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Patent number: 4410697Abstract: The invention relates to a new method for the preparation of N-aryl-N'-(mono- or disubstituted)-urea derivatives having the general formula (I), ##STR1## wherein Aryl is an optionally substituted phenyl group, andR.sup.1 and R.sup.2 each stand for an optionally substituted alkyl, cycloalkyl, alkoxy or phenyl group, orR.sup.1 and R.sup.2 may form, together with the adjacent nitrogen atom, a nitrogen-containing heterocyclic group which may contain a further hetero atom, orone of R.sup.1 and R.sup.2 may also stand for hydrogen,with the proviso that if one of R.sup.1 and R.sup.2 is an optionally substituted phenyl group, the other may represent only hydrogen atom or an optionally substituted alkyl or alkoxy group,by reacting a carbamate of the general formula (II) with an amine of the general formula (III),R.sup.1 R.sup.2 N--CO--X (II)Aryl--NH.sub.2 (III)or a carbamate of the general formula (IV) with an amine of the general formula (V),Aryl--NH--CO--X (IV)R.sup.1 R.sup.2 NH (V)wherein R.sup.1, R.sup.Type: GrantFiled: August 28, 1981Date of Patent: October 18, 1983Assignee: Reanal FinomvegyszergyarInventors: Sandor Torok, Lajos Voroshazy, Peter Galambos, Ivan Daroczi, Zoltan Ormenyi
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Patent number: 4409227Abstract: 4-(((Heterocyclo)thio)methyl)benzoic acids, esters, amides and pharmaceutically-acceptable salts thereof having hypoglycemic activity in mammals, including a method of use and pharmaceutically-acceptable compositions.Type: GrantFiled: March 9, 1982Date of Patent: October 11, 1983Assignee: The Dow Chemical Co.Inventor: Donald P. Matthews
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Patent number: 4388312Abstract: New quinone derivatives of the formula: ##STR1## wherein R.sup.1 is methyl or methoxy, or two of R.sup.1 combine to represent --CH.dbd.CH--CH.dbd.CH--, R is amino which may be substituted or --OR.sup.4 wherein R.sup.4 is hydrogen, C.sub.1-4 alkyl or --CH.sub.2 --CH.dbd.C(CH.sub.3 --CH.sub.2 --.sub.m H (wherein m is an integer of 1 to 10), and n is an integer of 1 to 10 when R is amino which may be substituted, or n is an integer of 2 to 10 when R is --OR.sup.4, and their hydroquinone forms, have useful physiological activities such as blood-pressure decreasing and antiallergic activities.Type: GrantFiled: August 26, 1980Date of Patent: June 14, 1983Assignee: Takeda Chemical Industries, Ltd.Inventors: Shinji Terao, Mitsuru Shiraishi, Kaneyoshi Kato
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Patent number: 4387099Abstract: Novel 1-heterocyclyloxy- or 1-aryloxy-3-amido-alkylamino-2-propanol derivatives, processes for their manufacture, pharmaceutical compositions containing them and methods of using them in the treatment of heart diseases. The compounds possess .beta.-adrenergic blocking activity. Representative of the compounds disclosed is 1-(4-indolyloxy)-3-.beta.-isobutyramidoethylamino-2-propanol.Type: GrantFiled: February 12, 1982Date of Patent: June 7, 1983Assignee: Imperial Chemical Industries LimitedInventor: Leslie H. Smith
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Patent number: 4358606Abstract: Novel esters of phenylalkyloxy- or phenylalkylthioacylamino acids and pyridylalkyloxy- or pyridylalkylthioacylamino acids, synthesis thereof, intermediates therefor, and the use of said esters for the control of weeds.Type: GrantFiled: June 19, 1981Date of Patent: November 9, 1982Assignee: Zoecon CorporationInventors: Shy-Fuh Lee, Clive A. Henrick