Additional Ring Containing Patents (Class 546/337)
  • Patent number: 4895847
    Abstract: 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: Grant
    Filed: September 21, 1988
    Date of Patent: January 23, 1990
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Yasuo Oshiro, Hiraki Ueda, Kazuyuki Nakagawa
  • Patent number: 4889865
    Abstract: 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: Grant
    Filed: February 21, 1989
    Date of Patent: December 26, 1989
    Assignee: Centre International de Recherches Dermatologiques C.I.R.D.
    Inventors: Braham Shroot, Gerard Lang, Jean Maignan, Serge Restle, Christopher Hensby, Michel Colin
  • Patent number: 4886822
    Abstract: 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: Grant
    Filed: April 8, 1988
    Date of Patent: December 12, 1989
    Assignee: Kowa Company, Ltd.
    Inventors: Kimiyuki Shibuya, Yoshio Takahashi, Seiichi Sato, Hiromichi Shigyo, Tomio Ohta, Yasumi Uchida
  • Patent number: 4876343
    Abstract: 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: Grant
    Filed: June 15, 1988
    Date of Patent: October 24, 1989
    Assignee: Warner-Lambert Company
    Inventors: John C. Hodges, Sylvester Klutchko
  • Patent number: 4863936
    Abstract: Various substituted aminoalkylamino-2-pyridine derivatives are disclosed which are useful as histamine H.sub.1 -antagonists.
    Type: Grant
    Filed: October 21, 1986
    Date of Patent: September 5, 1989
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: George S. Sach
  • Patent number: 4841059
    Abstract: 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: Grant
    Filed: October 15, 1987
    Date of Patent: June 20, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Michael Schriewer, Klaus Grohe, Hans-Joachim Zeiler, Karl G. Metzger
  • Patent number: 4837316
    Abstract: 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: Grant
    Filed: August 27, 1986
    Date of Patent: June 6, 1989
    Assignee: Fujirebio Kabushiki Kaisha
    Inventors: Yasuo Sekine, Nobuhiro Hirakawa, Noriaki Kashiwaba, Tetsuaki Yamaura, Hisako Harada, Teruo Kutsuma, Hajime Matsumoto, Akihiro Sekine, Yoshikazu Isowa
  • Patent number: 4826531
    Abstract: 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: Grant
    Filed: April 17, 1987
    Date of Patent: May 2, 1989
    Assignee: Imperial Chemical Industries PLC
    Inventors: Vivienne M. Anthony, John M. Clough, Paul DeFraine, Christopher R. A. Godfrey, Patrick J. Crowley, Kenneth Anderton
  • Patent number: 4808750
    Abstract: Novel fluorophenoxyphenoxypropionates and derivatives thereof possess herbicidal activity selectively in the presence of broadleaf crops. Preemergent and postemergent applications are contemplated.
    Type: Grant
    Filed: July 14, 1986
    Date of Patent: February 28, 1989
    Assignee: The Dow Chemical Company
    Inventors: Richard B. Rogers, B. Clifford Gerwick, III
  • Patent number: 4798893
    Abstract: 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: Grant
    Filed: September 21, 1987
    Date of Patent: January 17, 1989
    Assignee: McNeilab, Inc.
    Inventors: David A. Cherry, Cynthia A. Maryanoff, John E. Mills, Roy A. Olofson, James D. Rodgers
  • Patent number: 4797411
    Abstract: 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: Grant
    Filed: July 13, 1987
    Date of Patent: January 10, 1989
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Angelo Crugnola, Enrico di Salle, Paolo Lombardi
  • Patent number: 4794197
    Abstract: 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: Grant
    Filed: January 31, 1986
    Date of Patent: December 27, 1988
    Inventors: Walter Schneider, Isidor Erni, Hans K. Hegetschweiler
  • Patent number: 4794121
    Abstract: 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: Grant
    Filed: September 18, 1986
    Date of Patent: December 27, 1988
    Assignee: Panmedica
    Inventors: Claude Laruelle, Marcel Lepant, Bernard Raynier
  • Patent number: 4788130
    Abstract: 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: Grant
    Filed: August 29, 1985
    Date of Patent: November 29, 1988
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Yasuo Oshiro, Hiraki Ueda, Kazuyuki Nakagawa
  • Patent number: 4783537
    Abstract: 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: Grant
    Filed: November 13, 1985
    Date of Patent: November 8, 1988
    Assignee: Pennwalt Corporation
    Inventor: Robert J. Murray
  • Patent number: 4777286
    Abstract: Process and compounds for producing intermediates for the production of renin inhibitors.
    Type: Grant
    Filed: June 18, 1985
    Date of Patent: October 11, 1988
    Assignee: The Upjohn Company
    Inventor: Heinrich J. Schostarez
  • Patent number: 4769466
    Abstract: 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: Grant
    Filed: February 6, 1987
    Date of Patent: September 6, 1988
    Assignee: Pennwalt Corporation
    Inventors: Ronald C. Griffith, James J. Napier
  • Patent number: 4767865
    Abstract: 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: Grant
    Filed: June 29, 1987
    Date of Patent: August 30, 1988
    Assignee: The Upjohn Company
    Inventors: Roy A. Johnson, Chiu-Hong Lin
  • Patent number: 4766132
    Abstract: 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: Grant
    Filed: January 29, 1986
    Date of Patent: August 23, 1988
    Assignee: Imperial Chemical Industries PLC
    Inventor: Ian T. Kay
  • Patent number: 4758573
    Abstract: 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: Grant
    Filed: February 3, 1986
    Date of Patent: July 19, 1988
    Assignee: G. D. Searle & Co.
    Inventors: Paul W. Manley, Lai M. Fook
  • Patent number: 4753674
    Abstract: 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: Grant
    Filed: February 13, 1984
    Date of Patent: June 28, 1988
    Assignee: UBE Industries, Ltd.
    Inventors: Tetsuo Takematsu, Yasutomo Takeuchi, Mitsuaki Takenaka, Seiji Takamura, Minoru Nishimura, Tatsuo Okada, Yasuhisa Fukuda
  • Patent number: 4743603
    Abstract: 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: Grant
    Filed: May 27, 1986
    Date of Patent: May 10, 1988
    Assignee: Rhone-Poulenc Agrochimie
    Inventor: Jean P. Bulot
  • Patent number: 4743610
    Abstract: 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: Grant
    Filed: March 16, 1987
    Date of Patent: May 10, 1988
    Assignee: American Cyanamid Company
    Inventors: William B. Wright, Jr., Andrew S. Tomcufcik
  • Patent number: 4735959
    Abstract: 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: Grant
    Filed: May 14, 1985
    Date of Patent: April 5, 1988
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Wolfgang Grell, Gerhart Griss, Robert Sauter, Rudolf Hurnaus, Eckhard Rupprecht, Nikolaus Kaubisch, Joachim Kahling, Bernhard Eisele
  • Patent number: 4731373
    Abstract: 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: Grant
    Filed: December 10, 1984
    Date of Patent: March 15, 1988
    Assignee: Hoffman-La Roche Inc.
    Inventors: Richard Barner, Kasper Burri, Jean-Marie Cassal, Paul Hadvary, Georges Hirth, Klaus Muller
  • Patent number: 4730053
    Abstract: 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: Grant
    Filed: November 25, 1985
    Date of Patent: March 8, 1988
    Assignee: A. Nattermann & Cie GmbH
    Inventors: Norbert Dereu, Albrecht Wendel, Helmut Sies, Sigurd Leyck, Axel Romer, Erich Graf
  • Patent number: 4725602
    Abstract: 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: Grant
    Filed: October 24, 1985
    Date of Patent: February 16, 1988
    Assignee: McNeilab, Inc.
    Inventor: John R. Carson
  • Patent number: 4716175
    Abstract: 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: Grant
    Filed: February 24, 1987
    Date of Patent: December 29, 1987
    Assignee: Warner-Lambert Company
    Inventors: Milton L. Hoefle, Ann Holmes, Bruce D. Roth
  • Patent number: 4696930
    Abstract: 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: Grant
    Filed: April 12, 1985
    Date of Patent: September 29, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: John G. Mullin, Jr., Keiji Nakamura, Jefferson W. Tilley, Hiroshi Watanabe
  • Patent number: 4684733
    Abstract: 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: Grant
    Filed: July 28, 1986
    Date of Patent: August 4, 1987
    Assignee: Riker Laboratories, Inc.
    Inventor: Charles M. Leir
  • Patent number: 4683239
    Abstract: 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: Grant
    Filed: April 10, 1986
    Date of Patent: July 28, 1987
    Assignee: McNeilab, Inc.
    Inventors: Richard J. Carmosin, John R. Carson
  • Patent number: 4675328
    Abstract: 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: Grant
    Filed: January 15, 1986
    Date of Patent: June 23, 1987
    Assignee: Hoffmann-LaRoche Inc.
    Inventors: Jean-Marie Cassal, Albrecht Edenhofer, Henri Ramuz
  • Patent number: 4663333
    Abstract: 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: Grant
    Filed: December 20, 1985
    Date of Patent: May 5, 1987
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis, James R. Deason
  • Patent number: 4636505
    Abstract: 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: Grant
    Filed: July 15, 1983
    Date of Patent: January 13, 1987
    Assignee: Imperial Chemical Industries PLC
    Inventor: Howard Tucker
  • Patent number: 4622339
    Abstract: 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: Grant
    Filed: January 11, 1985
    Date of Patent: November 11, 1986
    Assignee: Bayer Aktiengesellschaft
    Inventors: Folker Lieb, Hermann Oediger, Hans-Joachim Kabbe, Ulrich Niewohner, Elisabeth Perzborn, Friedel Seuter
  • Patent number: 4558150
    Abstract: 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: Grant
    Filed: December 10, 1984
    Date of Patent: December 10, 1985
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Eric M. Gordon, Jollie D. Godfrey, Jr.
  • Patent number: 4520027
    Abstract: 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: Grant
    Filed: December 23, 1982
    Date of Patent: May 28, 1985
    Assignee: Imperial Chemical Industries PLC
    Inventors: Peter R. Marsham, David S. Thomson
  • Patent number: 4503232
    Abstract: 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: Grant
    Filed: September 24, 1982
    Date of Patent: March 5, 1985
    Assignee: Agency of Industrial Science & Technology
    Inventors: Toshiaki Kobayashi, Masato Tanaka
  • Patent number: 4501746
    Abstract: Novel N,N-disubstituted carboxamide derivatives useful as herbicides, fungicides and aquatic plant growth regulators.
    Type: Grant
    Filed: September 15, 1982
    Date of Patent: February 26, 1985
    Assignee: Eli Lilly and Company
    Inventor: Eriks V. Krumkalns
  • Patent number: 4500714
    Abstract: 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: Grant
    Filed: October 7, 1982
    Date of Patent: February 19, 1985
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Masamitsu Honda, Hideaki Nagai, Shoko Takishima, Akinori Kawamura, Noriko Kawamura, Takashi Dan, Masuo Koizumi, Yasushi Murakami, Yoshikazu Hinohara, Hideki Nakano, Yoshio Takagaki
  • Patent number: 4486593
    Abstract: 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: Grant
    Filed: January 19, 1983
    Date of Patent: December 4, 1984
    Assignee: The Upjohn Company
    Inventor: Chiu-Hong Lin
  • Patent number: 4486598
    Abstract: Novel compounds of the following general formula: ##STR1##
    Type: Grant
    Filed: February 22, 1982
    Date of Patent: December 4, 1984
    Assignee: The Upjohn Company
    Inventor: Paul A. Aristoff
  • Patent number: 4460580
    Abstract: 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: Grant
    Filed: June 24, 1982
    Date of Patent: July 17, 1984
    Assignee: Ciba-Geigy Corporation
    Inventors: Franz Ostermayer, Markus Zimmermann
  • Patent number: 4454324
    Abstract: 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: Grant
    Filed: April 1, 1983
    Date of Patent: June 12, 1984
    Assignee: Mead Johnson & Company
    Inventor: Gary D. Madding
  • Patent number: 4423222
    Abstract: 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: Grant
    Filed: May 21, 1982
    Date of Patent: December 27, 1983
    Assignee: The Dow Chemical Company
    Inventors: Mary L. Ash, Richard G. Pews
  • Patent number: 4410697
    Abstract: 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: Grant
    Filed: August 28, 1981
    Date of Patent: October 18, 1983
    Assignee: Reanal Finomvegyszergyar
    Inventors: Sandor Torok, Lajos Voroshazy, Peter Galambos, Ivan Daroczi, Zoltan Ormenyi
  • Patent number: 4409227
    Abstract: 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: Grant
    Filed: March 9, 1982
    Date of Patent: October 11, 1983
    Assignee: The Dow Chemical Co.
    Inventor: Donald P. Matthews
  • Patent number: 4388312
    Abstract: 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: Grant
    Filed: August 26, 1980
    Date of Patent: June 14, 1983
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shinji Terao, Mitsuru Shiraishi, Kaneyoshi Kato
  • Patent number: 4387099
    Abstract: 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: Grant
    Filed: February 12, 1982
    Date of Patent: June 7, 1983
    Assignee: Imperial Chemical Industries Limited
    Inventor: Leslie H. Smith
  • Patent number: 4358606
    Abstract: 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: Grant
    Filed: June 19, 1981
    Date of Patent: November 9, 1982
    Assignee: Zoecon Corporation
    Inventors: Shy-Fuh Lee, Clive A. Henrick