Nitrogen, Other Than As Nitro Or Nitroso, Attached Directly To The Isoquinoline Ring System By Nonionic Bonding Patents (Class 514/310)
  • Patent number: 5032591
    Abstract: A pharmaceutical product comprising a potassium channel activator antihypertensive agent and a .beta.-blocker antihypertensive agent as a combined preparation for simultaneous, separate or sequential use in therapy of hypertension.
    Type: Grant
    Filed: January 4, 1989
    Date of Patent: July 16, 1991
    Assignee: Beecham Group p.l.c.
    Inventors: John M. Evans, Robin E. Buckingham
  • Patent number: 5010087
    Abstract: Novel tricyclic compounds having a TXA.sub.2 -antagonizing activity represented by formula (I): ##STR1## which strongly antagonize an action of thromboxane A.sub.2 and are expected to have preventive and therapeutic effects on ischemica diseases, cerebro-vascular diseases, etc.
    Type: Grant
    Filed: July 18, 1989
    Date of Patent: April 23, 1991
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
  • Patent number: 5006534
    Abstract: Substituted benzyl ethers, benzyl thioethers, and benzylamines of the formula ##STR1## in which R.sup.1 and R.sup.2 are identical or different and represent hydrogen, alkyl, alkenyl, cycloalkyl, alkoxy, alkylthio, halogenoalkyl, sulphonylalkyl, halogenoalkoxy, halogenoalkylthio, aralkoxy, aralkylthio, halogen, nitro, cyano or hydroxyl, or represent a group of the formula ##STR2## wherein R.sup.4 and R.sup.5 are identical or different and represent hydrogen, alkyl, alkenyl, cycloalkyl, aralkyl, aryl or acyl,R.sup.3 represents a group of the formula ##STR3## in which R.sup.6 represents hydrogen, alkyl or acyl,R.sup.7 represents hydrogen or alkyl andn represents a number from 3 to 10,B represents --CH.sub.2 --X-- or --X--CH.sub.2 --,wherein X represents O, S or NR.sup.7,and wherein R.sup.7 has the abovementioned meaning and the group ##STR4## represents a benzo-fused heterocyclic system, A in the heterocyclic radical being 3-, 4- or 5-membered and containing nitrogen, oxygen and/or sulphur as hetero-atoms.
    Type: Grant
    Filed: January 30, 1989
    Date of Patent: April 9, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus-Helmut Mohrs, Romanis Fruchtmann, Christian Kohlsdorfer
  • Patent number: 4997835
    Abstract: Substituted 2-acylpyridine-.alpha.-(N)-hetarylhydrazones are described, which are suitable as active substances for the treatment of antimicrobial and in particular antimycobacterial diseases, as well as active substances for the treatment of malaria or malignant tumours. The compounds have a marked synergistic activity combined with inhibitors of folate synthase, dihydrofolic acid reductase, DNA-synthesis and RNA-synthesis.
    Type: Grant
    Filed: March 7, 1989
    Date of Patent: March 5, 1991
    Inventors: Klaus-Jurgen Schaper, Joachim K. Seydel
  • Patent number: 4988720
    Abstract: A method for the treatment and/or prophylaxis of hyperglycemia in mammals including administration to the mammal of an effective, nontoxic amount of either a compound of formula (I), ##STR1## or a pharmaceutically acceptable acid addition salt thereof; or of a compound of formula (II), ##STR2## or a pharmaceutically acceptable acid addition salt thereof.
    Type: Grant
    Filed: April 11, 1989
    Date of Patent: January 29, 1991
    Assignee: Beecham Group P.L.C.
    Inventor: Michael A. Cawthorne
  • Patent number: 4983600
    Abstract: Aroyl ureas and carbamic acid derivatives of formulaA--CO--NHCW--Y--Band pharmaceutically acceptable salts thereof whereinA is a specified aromatic radical including optionally substituted phenylW is O or SY is NH or S andB is a specified saturated azacyclic ring, eg tropan-3-yl or quinuclidin-3-yl,possess 5-HT.sub.3 -antagonistic activity and are, for example, useful in treatment of migraine, emesis, anxiety, gastro-intestinal disorders and as anti-psychotics.
    Type: Grant
    Filed: October 16, 1989
    Date of Patent: January 8, 1991
    Assignee: John Wyeth & Brother Limited
    Inventors: Terence J. Ward, Janet C. White, Gerald Bradley
  • Patent number: 4975438
    Abstract: Compounds of the formula ##STR1## Y is O or S, *A is paraphenylene or *--(CH.sub.2).sub.n --(X).sub.m --(CH.sub.2).sub.r --, X is O, S or --CH.dbd.CH--, n or r, independently, are integers from 0 to 3, s is an integer from 0 to 1, m is an integer from 0 to 1, provided that when m is 1, n+s must be at least 2, R.sub.1 and R.sub.2, independently, are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, Het, Aryl, R.sub.3, R.sub.4 and R.sub.8, independently, are hydrogen, lower alkyl, aryl, R.sub.5 and R.sub.6, independently, are hydrogen or lower alkyl, R.sub.7 is hydrogen, lower alkyl, cycloalkyl, Het-lower alkyl or aryl, Het is a monocyclic 5- or 6-membered hetero aromatic or a bicyclic heteroaromatic radical containing one or two hetero atoms selected from nitrogen, oxygen and sulfur, which radical may be substituted by lower alkyl, halogen or aryl, and the asterisk denotes the point of attachment,and when R.sub.6 and R.sub.7 are different, their enantiomers and racemic mixtures thereof, when R.sub.1 and R.sub.
    Type: Grant
    Filed: September 6, 1988
    Date of Patent: December 4, 1990
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Robert W. Guthrie, Richard W. Kierstead, Jefferson W. Tilley
  • Patent number: 4966906
    Abstract: Novel 1-aryl-3-quinolinecarboxamides and 1-aryl-3-isoquinolinecarboxamides, processes for the preparation thereof, and methods for treating pain and inflammation utilizing compounds and compositions thereof are disclosed.
    Type: Grant
    Filed: July 14, 1988
    Date of Patent: October 30, 1990
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Edward J. Glamkowski, R. Richard L. Hamer
  • Patent number: 4963563
    Abstract: Compounds of the formula: ##STR1## wherein n=1 or 2; R.sub.1 is lower alkoxy, lower alkyl, halo, ester, carbamate, or substituted amino; and R.sub.2 is thienyl or furyl; or R.sub.2 is ##STR2## wherein R.sub.3 and R.sub.4 are independently selected from hydrogen, halo, hydroxy, methoxy, thioalkoxy, substituted amino and lower alkyl; and pharmaceutically acceptable salts thereof.These compounds are useful as inhibitors of alpha-2-adrenergic receptors and for the treatment of glaucoma and/or controlling intraocular pressure.
    Type: Grant
    Filed: October 13, 1989
    Date of Patent: October 16, 1990
    Assignee: Abbott Laboratories
    Inventors: John F. DeBernardis, Robert E. Zelle
  • Patent number: 4956371
    Abstract: Novel substituted isoquinoline compounds are disclosed together with novel 2-phenylethylamides useful as precursors or intermediates for the production of the isoquinolines. The substituted isoquinolines exhibit activity in antagonizing the effects of platelet activating factor (PAF).
    Type: Grant
    Filed: September 19, 1989
    Date of Patent: September 11, 1990
    Assignee: Euroceltique, S.A.
    Inventors: T. Scott Shoupe, Stephen M. Coutts, Lloyd J. Dolby
  • Patent number: 4952589
    Abstract: This invention relates to aminoalkylphenoxyalkyl substituted heterocycles. These compounds antagonize the action of histamine on histamine H.sub.2 -receptors in the brain. A compound of the invention is 2-[3-[3-(piperidinomethyl)phenoxy]propylamino]benzthiazole.
    Type: Grant
    Filed: June 3, 1987
    Date of Patent: August 28, 1990
    Assignee: Smith Kline & French Laboratories Limited
    Inventors: Thomas H. Brown, Robert C. Mitchell, Ian R. Smith, Rodney C. Young
  • Patent number: 4942163
    Abstract: 3-(1-Naphthalenyl)-1(2H)-isoquinolinones and 3-(1-naphthalenyl)-1-isoquinolineamines are useful as cancer chemotherapeutic agents.
    Type: Grant
    Filed: March 7, 1989
    Date of Patent: July 17, 1990
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Carl H. Behrens
  • Patent number: 4906643
    Abstract: N-(3-hydroxy-4-piperidinyl)substituted benzamides, their N-oxide forms and pharmaceutically acceptable acid-addition salts having gastrointestinal motility stimulating properties, compositions containing the same, and methods of treating warm blooded animals suffering from a decreased peristalsis of the gastrointestinal system.
    Type: Grant
    Filed: June 10, 1988
    Date of Patent: March 6, 1990
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Georges H. P. Van Daele, Freddy F. Vlaeminck, Karel J. Van Loon
  • Patent number: 4886803
    Abstract: Compounds are described of formula (I) ##STR1## wherein R.sup.1 is a hydrogen atom, an alkyl group, an alkoxy group, a dialkylamino group or a halogen atom; n is 1 to 4; R.sup.2 is a hydrogen atom, an alkyl group, an unsubstituted or substituted aminoalkyl group, an acyl group, an unsubstituted or substituted aralkyl group, a carboxyalkyl group, an alkoxycarbonyalkyl group or ##STR2## wherein X is an unsubstituted or substituted-phenyl, -benzyl, -benzoyl or -furoyl group; A is -NR.sup.3 - where R.sup.3 is hydrogen or alkyl, an alkylene or an alkylidene; and B is a heterocyclic group selected from triazolyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, benzimidazolyl, benzothiazolyl, quinolyl and isoquinolyl, said heterocyclic group being optionally substituted by one or more alkyl, alkoxy, nitro or phenyl group, and the physiologically acceptable acid addition salts thereof. The compound of formula (I) are or cardiotonic activity and thus may be useful for the treatment of circulatory diseases.
    Type: Grant
    Filed: July 15, 1987
    Date of Patent: December 12, 1989
    Assignee: Nisshin Flour Milling Co., Ltd.
    Inventors: Noriyoshi Sueda, Yoshikuni Suzuki, Toshiji Sugai, Hiroaki Yamada, Makoto Yanai
  • Patent number: 4885299
    Abstract: The invention relates to new 2-(2,3-dihydro-2-oxo-3-benzofuranyl)acetic acid compounds of general formula I: ##STR1## in which: R.sub.1 denotes a hydrogen atom, a linear or branched alkyl radical having 1 to 4 carbon atoms or a phenyl radical optionally substituted with a halogen atom or with an alkoxy radical containing 1 to 4 carbon atoms or an alkyl radical having 1 to 4 carbon atoms,R.sub.2 denotes a hydrogen or halogen atom, a hydroxyl radical, an alkyl radical having 1 to 4 carbon atoms or an alkoxy radical containing 1 to 4 carbon atoms,R denotes a hydroxyl radical, a linear or branched alkoxy radical having 1 to 4 carbon atoms, a benzyloxy radical or a radical of general formula A: ##STR2## in which: X and Y, which may be identical or different, each denote a linear or branched alkyl radical containing 1 to 5 carbon atoms, a radical of general formula A.sub.
    Type: Grant
    Filed: January 17, 1989
    Date of Patent: December 5, 1989
    Assignee: ADIR Et Cie
    Inventors: Gilbert Lavielle, Jean Lepagnol
  • Patent number: 4866075
    Abstract: The invention concerns compounds of formula: ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, halogen, lower alkoxy or hydroxy; R.sub.2 represents hydrogen or lower alkyl; A represents an alkylene, oxoalkylene or hydoxyalkylene chain each having 2 to 6 carbon atoms, R.sub.3 and R.sub.4 may be in the same or different rings and independently represent hydrogen, lower alkyl, lower alkoxy, amino or halogen and one of X and Y represents nitrogen the other represents CR.sub.5 wherein R.sub.5 is one of the values for R.sub.3 or R.sub.5 is the bond to the NHCO group; or a pharmaceutically acceptable salt thereof, which compounds possess antihypertensive activity whilst exhibiting reduced CNS depressant properties. Also disclosed are processes for preparing the compounds and pharmaceutical compositions containing them.
    Type: Grant
    Filed: August 12, 1988
    Date of Patent: September 12, 1989
    Assignee: John Wyeth and Brother Limited
    Inventors: John L. Archibald, Terence J. Ward, Janet C. White
  • Patent number: 4866076
    Abstract: The invention provides a class of sulphonamide-containing tetrahydroisoquinolinyl compounds having thromboxane antagonist activity.
    Type: Grant
    Filed: July 21, 1988
    Date of Patent: September 12, 1989
    Assignee: Smith Kline & French Laboratories Limited
    Inventor: Andrew D. Gribble
  • Patent number: 4863945
    Abstract: Pyrrolobenzimidazoles of the formula: ##STR1## are useful for treatment of heart and circulatory diseases. R.sub.1 is substituted phenyl; or optionally substituted naphthyl or a five- or six-membered heterocyclic group which can be condensed with a phenyl ring to form a bicyclic radical. R.sub.2 is hydrogen, alkyl, alkenyl or cycloalkenyl; R.sub.3 is alkyl, alkenyl or hydroxyalkyl or with R.sub.2 together forms cycloakylene; or R.sub.2 and R.sub.3 together form alkylidene or cycloalkylidene. R.sub.4 is hydrogen or lower alkanoyl. X is a valency bond, alkylene, vinylene, imino or carbonylamino. T stands for two hydrogen atoms. When X is a valency bond, R.sub.1 can also be hydrogen, hydrocarbyl which may also contain oxygen, amino, sulfur, carbonyl and sulfonyl groups. When X is imino or carbonylamino or when R.sub.1 is a bicyclic radical, T can also be oxygen. The compounds also include the tautomers and physiologically acceptable salts with inorganic and organic acids.
    Type: Grant
    Filed: December 10, 1987
    Date of Patent: September 5, 1989
    Assignee: Boehringer Mannheim GmbH
    Inventors: Walter-Gunar Friebe, Alfred Mertens, Klaus Strein, Erwin Boehm
  • Patent number: 4847280
    Abstract: A method for the treatment and/or prophylaxis of hyperglycaemia in human or non-human mammals which comprises administering to the mammal in need of such treatment and/or prophylaxis an effective non-toxic amount of:a compound of formula (I): ##STR1## or a pharmaceutically acceptable acid addition salt thereof, or a compound of formula (II): ##STR2## or a pharmaceutically acceptable acid addition salt thereof, and compositions for use in such method.
    Type: Grant
    Filed: May 23, 1986
    Date of Patent: July 11, 1989
    Assignee: Beecham Group plc
    Inventor: Michael A. Cawthorne
  • Patent number: 4847266
    Abstract: The present invention relates to a new and improved method for the preparation of a compound of the formula I ##STR1## in which R stands for halogen, giving rise to high yields of substantially pure 6.beta.-halopenicillanic acids, obtained in one step.
    Type: Grant
    Filed: April 28, 1987
    Date of Patent: July 11, 1989
    Assignee: Leo Pharmaceutical Products Ltd.
    Inventors: Erik I. Hansen, Mogens P. Kran-Nielsen, Welf Von Daehne
  • Patent number: 4843077
    Abstract: Isoquinoline derivatives of compounds of the general formula ##STR1## that exhibit cardiotonic and/or phosphodiesterase fraction III inhibiting properties and/or renal vasodilating are pharmacologically active in the treatment of cardiac conditions. Methods for synthesizing and using the compounds are described.
    Type: Grant
    Filed: June 9, 1987
    Date of Patent: June 27, 1989
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Jeffery S. Hinkle, O. William Lever, Jr.
  • Patent number: 4835140
    Abstract: The combination of clindamycin and primaquine or pharmaceutical salts thereof is effective in treating patients with Pneumocystis carinii pneumonia.
    Type: Grant
    Filed: August 20, 1987
    Date of Patent: May 30, 1989
    Assignee: Indiana University Foundation
    Inventors: James W. Smith, Marilyn S. Bartlett, Sherry F. Queener
  • Patent number: 4812573
    Abstract: The invention relates to a class of tetrahydroisoquinolinylalkanoic acids containing an aryl sulphonamide group which have activity as thromboxane A.sub.2 antagonists.
    Type: Grant
    Filed: June 27, 1988
    Date of Patent: March 14, 1989
    Assignee: SmithKline & French Laboratories, Ltd.
    Inventors: Graham J. Durant, Andrew D. Gribble, Robert A. Slater
  • Patent number: 4806548
    Abstract: This invention relates to an improved anti-ulcer composition for prophylaxis and treatment of stomach and duodenum ulcers, including stress ulcers. The composition provides potent anti-ulcer activity with a dramatic reduction in toxicity and harmful side effects. The composition comprises a histamine H.sub.2 antagonist based on a guanidine derivative, preferably [N-cyano-H'-methyl-N"]-2(4-methyl-imidazolyl)-methylthio-[ethylguanidine]; and at least one 4-phenyl-tetrahydroisoquinoline antidepressant, preferably the [+] isomer of 4-phenyl-2-methyl-8-amino-1,2,3,4-tetrahydroisoquinoline hydrogen maleate. The composition may also contain a spasmolytic agent, preferably 2-metoxycarbonyl-4-(beta-piperidino ethyl) -metoxycarbonyl-4-(beta-peperidinoethyl) benzophenone. The ratio of antagonist to antidepressant ranges from 2:1 to 60:1, and the ratio of their sum to the spasmolytic agent, when used, ranges from 2.2:1 to 42.5:1.
    Type: Grant
    Filed: August 4, 1987
    Date of Patent: February 21, 1989
    Assignee: T P O Pharmachim
    Inventors: Nedyalka S. Ivanova, Tshavdar B. Ivanov, Margarita D. Dryanska, Orhideya B. Zabunova, Lilyana D. Dalleva, Milka P. Nikolova, Nikolina D. Berova, Rossitza S. Rakovska, Maria S. Stoyanova, Sascha R. Mihaylova, Milka A. Luna, Jossif N. Nissimou, Snejana G. Vitkova, Vladimir K. Matov, Boris K. Dimitrov, Grigor M. Metshkov
  • Patent number: 4801593
    Abstract: A method of treating or preventing viral infections, in particular rhinovirus infections comprising the administration of an effective amount of a 2-phenyltetralin derivative or a heterocyclic analogue thereof. Pharmaceutical compositions containing these compounds, and some novel compounds are also disclosed.
    Type: Grant
    Filed: August 11, 1980
    Date of Patent: January 31, 1989
    Assignee: Burroughs Wellcome Co.
    Inventors: Harold F. Hodson, John F. Batchelor, John W. T. Selway, Jeremy G. Vinter, Ramachanderan Iyer
  • Patent number: 4794123
    Abstract: This invention relates to a method of treating ulcers or hypersecretion in a mammal which comprises administering a compound of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein --B--B.sup.1 -- represents a chain of formula--CR.sup.5 .dbd.CR.sup.6 -- (Ib)or--(CHR.sup.5).sub.n --CR.sup.6 .dbd. (Ic);R represents an optionally substituted aryl or heteroaryl radical; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, or a defined substituent or any adjacent pair of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 together with the carbon atoms to which they are attached complete a five or six membered saturated or unsaturated carbocyclic or heterocyclic ring, said ring being optionally substituted by a defined substituent said heterocyclic ring having at least one heteroatom selected from oxygen, nitrogen and sulphur. Novel compositions and compounds of formula I are also disclosed.
    Type: Grant
    Filed: October 13, 1987
    Date of Patent: December 27, 1988
    Assignee: John Wyeth & Brother Limited
    Inventors: Roger Crossley, Peter J. Meade
  • Patent number: 4793998
    Abstract: The cyclization and hydrolysis of certain ACE inhibitors is minimized when they are formulated with a stabilizer and at least one lubricant and/or excipient.
    Type: Grant
    Filed: October 20, 1986
    Date of Patent: December 27, 1988
    Assignee: Warner-Lambert Company
    Inventors: Kuchi S. Murthy, Michael R. Harris, Gerard C. Hokanson, Robert G. Reisch, Jr., Frank Waldman, Mahdi B. Fawzi
  • Patent number: 4786639
    Abstract: A method for the treatment and/or prophylaxis of reversible airways obstruction and asthma in mammals, which method comprises administering to the mammal in need of said treatment an effective amount of a compound of formula (I): ##STR1## wherein R.sub.1 -R.sub.8 and X are as set forth herein.
    Type: Grant
    Filed: November 4, 1986
    Date of Patent: November 22, 1988
    Assignee: Beecham Group p.l.c.
    Inventor: John M. Evans
  • Patent number: 4782083
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: one of R.sub.1 and R.sub.2 is hydrogen or C.sub.1-4 alkyl and the other is C.sub.1-4 alkyl or R.sub.1 and R.sub.2 together are C.sub.2-5 -polymethylene;either R.sub.3 is hydrogen, hydroxy, C.sub.1-6 alkoxy or C.sub.1-7 acyloxy and R.sub.4 is hydrogen or R.sub.3 and R.sub.4 together are a bond;R.sub.5 is hydrogen C.sub.1-6 alkyl optionally substituted by halogen hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 alkoxycarbonyl, carboxy or amino optionally substituted by one or two independent C.sub.1-6 alkyl groups, or C.sub.2-6 alkenyl, amino optionally substituted by a C.sub.1-6 alkyl or C.sub.1-6 alkenyl group or by a C.sub.1-6 alkanoyl group optionally substituted by up to three halo atoms, by a phenyl group optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen, or aryl or hetroaryl, either being optionally substituted by one or more groups or atoms selected from the class of C.sub.1-6 alkyl, C.sub.
    Type: Grant
    Filed: August 29, 1986
    Date of Patent: November 1, 1988
    Assignee: Beecham Group P.L.C.
    Inventors: Frederick Cassidy, Geoffrey Stemp, John M. Evans
  • Patent number: 4772603
    Abstract: A method for the treatment and/or prophylaxis of congestive heart failure, angina, occlusive peripheral vascular disease or cerebral vascular disease in mammals, such as humans, which method comprises administering to the mammal in need of such treatment and/or prophylaxis an effective and/or prophylactic amount of a compound of formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, and X are set forth in the specification herein.
    Type: Grant
    Filed: November 4, 1986
    Date of Patent: September 20, 1988
    Assignee: Beecham Group p.l.c.
    Inventor: John M. Evans
  • Patent number: 4757079
    Abstract: Novel compounds of the formula: ##STR1## are described wherein Z is a bicyclic aryl group containing between 9 and 10 ring atoms, up to two of which may be nitrogen and up to one of which may be oxygen or sulfur; A is an ethenyl group which may be lower-alkyl-substituted; and R and R' each represent H or an aliphatic group of 1-4 carbon atoms; or a pharmaceutically acceptable acid addition salt thereof.
    Type: Grant
    Filed: June 24, 1986
    Date of Patent: July 12, 1988
    Assignee: Dynamac Corporaton
    Inventor: Allan P. Gray
  • Patent number: 4749698
    Abstract: Compounds having the general structure ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are defined herein, which exhibit antihypertensive activity.
    Type: Grant
    Filed: July 8, 1985
    Date of Patent: June 7, 1988
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: Edward S. Neiss, John T. Suh, John R. Regan, Jerry W. Skiles, Jeffrey N. Barton, James J. Mencel, Paul Menard
  • Patent number: 4745115
    Abstract: Compounds of the general formula I ##STR1## in which: R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl or together are a group X which is C.sub.3-6 polymethylene optionally in which one carbon atom is replaced by O, S or NR.sub.6 wherein R.sub.6 is hydrogen or C.sub.1-6 alkyl;R.sub.3 is a mono- or fused bi-cyclic heteroaromatic group having up to ten atoms in the aromatic ring(s), not more than four of which are selected from nitrogen, oxygen or sulphur, optionally C-substituted by one or more substituents selected from halogen, CF.sub.3, nitro, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.2-7 alkanoyl or cyano; or is phenyl or naphthyl, optionally substituted by one or more substituents selected from halogen, CF.sub.3, nitro, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.2-7 alkanoyl, carboxyl, C.sub.1-6 alkoxycarbonyl, cyano, CONR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are selected from hydrogen or C.sub.1-6 alkyl or together are a group X; NR.sub.9 R.sub.
    Type: Grant
    Filed: October 18, 1985
    Date of Patent: May 17, 1988
    Assignee: Beecham Group p.l.c.
    Inventors: Roger E. Markwell, Stephen A. Smith, David J. Hunter
  • Patent number: 4738963
    Abstract: A method for the treatment and/or prophylaxis of incontinence in mammals, which method comprises administering to the mammal in need of said treatment an effective amount of a compound of formula (I): ##STR1## wherein R.sub.1 -R.sub.8 and X are as set forth herein.
    Type: Grant
    Filed: May 27, 1986
    Date of Patent: April 19, 1988
    Assignee: Beecham Group p.l.c.
    Inventors: Thomas C. Hamilton, Robin E. Buckingham
  • Patent number: 4735957
    Abstract: New thiazole derivatives of the formula: ##STR1## wherein R.sup.1 is lower alkyl, carboxy, a drivative of carboxy, hydroxymethyl, halomethyl, lower alkylthiomethyl, hydroxyiminomethyl or alkenyl which may be substituted with lower alkoxycarbonyl, pyridyl or cyano,R.sup.2 is hydrogen, hydroxy, lower alkyl, pyridyl, amino, lower alkylamino, pyridylamino, arylamino, acylamino, N-(lower)alkylN-acylamino, guanidino optionally substituted with dimethylaminomethylene, or ar(lower)alkylamino optionally substituted with lower alkoxy,R.sup.3 is lower alkyl, halo(lower)alkyl or N-containing unsaturated heterocyclic group which may be substituted with halogen, lower alkyl, lower alkoxy, carboxy, a derivative of carboxy, hydroxy, pyridyl, amino, lower alkylamino, pyridylamino, arylamino, acylamino, N-(lower)alkyl-N-acylamino, guanidino, N-oxide or ar(lower)alkylamino optionally substituted with lower alkoxy,Q is --CO--, andn is an integer of 0 or 1,provided that when both of R.sup.1 and R.sup.
    Type: Grant
    Filed: November 18, 1986
    Date of Patent: April 5, 1988
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takao Takaya, Hisashi Takasugi
  • Patent number: 4725605
    Abstract: This invention relates to a method of treating ulcers or hypersecretion in a mammal which comprises administering a compound of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein --B--B.sup.1 -- represents a chain of formula--CR.sup.5 .dbd.CR.sup.6 -- (Ib)or--(CHR.sup.5).sub.n --CR.sup.6 .dbd. (Ic);R represents an optionally substituted aryl or heteroaryl radical; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, or a defined substituent or any adjacent pair of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 together with the carbon atoms to which they are attached complete a five or six membered saturated or unsaturated carbocyclic or heterocyclic ring, said ring being optionally substituted by a defined substituent said heterocyclic ring having at least one heteroatom selected from oxygen, nitrogen and sulphur. Novel compositions and compounds of formula I are also disclosed.
    Type: Grant
    Filed: May 22, 1986
    Date of Patent: February 16, 1988
    Assignee: John Wyeth & Brother Limited
    Inventors: Roger Crossley, Peter J. Meade
  • Patent number: 4696939
    Abstract: Compounds of the formula ##STR1## and their pharmaceutically acceptable salts, wherein the substituents are as defined herein, having antihypertensive activity.
    Type: Grant
    Filed: November 29, 1985
    Date of Patent: September 29, 1987
    Assignee: USV Pharmaceutical Corporation
    Inventors: John T. Suh, John J. Piwinski, Howard Jones, Edward S. Neiss
  • Patent number: 4694000
    Abstract: The invention relates to novel quinazoline and isoquinoline derivatives of the general formula: ##STR1## and acid addition salts and copper complexes thereof, wherein X represents nitrogen or a CH group,Y represents oxygen or an NH group,R.sub.1 and R.sub.2 represent hydrogen, alkyl(1-6 C), alkoxy (1-6 C), halogen or trifluoromethyl,R.sub.3 represents a substituted or unsubstituted 2-pyridyl group andR.sub.4 represents hydrogen, an alkyl(1-6 C) group unsubstituted or substituted by halogen, alkoxy (1-6 C) or phenyl groups, a cyclic alkyl group or a substituted or unsubstituted aromatic group.
    Type: Grant
    Filed: December 6, 1984
    Date of Patent: September 15, 1987
    Assignee: Akzo N.V.
    Inventors: Hendrik Timmerman, Henderikus Van der Goot
  • Patent number: 4657908
    Abstract: The invention relates to carbonyl derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention where is provided a guanidine derivative of the formula I: ##STR1## in which R.sup.1 and R.sup.2, same or different, are hydrogen or 1-10C alkyl, 3-8C cycloalkyl or 4-14C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, Cl or Br atoms, provided that one of R.sup.1 and R.sup.2 is halogen substituted, or R.sup.2 is hydrogen and R.sup.1 is R.sup.5 -E-W in which W is 2-6C alkylene optionally substituted by 1 or 2 1-4C alkyls, E is O, S, SO, SO.sub.2 or NR.sup.6 in which R.sup.6 is H or 1-6C alkyl, R.sup.5 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R.sup.5 and R.sup.6 are joined to form a pyrrolidine, piperidine, morpholine, piperazine or N-methylpiperazine ring, or R.sup.2 is H and R.sup.
    Type: Grant
    Filed: February 12, 1985
    Date of Patent: April 14, 1987
    Assignees: ICI Americas, Inc., Imperial Chemical Industries PLC
    Inventors: Tobias O. Yellin, David J. Gilman, Philip N. Edwards, Michael S. Large, Derrick F. Jones, Keith Oldham
  • Patent number: 4656188
    Abstract: Angiotensin converting enzyme inhibitors are useful in the treatment of senile macular degeneration.
    Type: Grant
    Filed: October 9, 1985
    Date of Patent: April 7, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Daniel F. Veber, John J. Baldwin
  • Patent number: 4649146
    Abstract: The invention relates to novel pharmaceutical compounds for treatment for ulcer of the formula: ##STR1## wherein R.sup.1 is lower alkyl, carboxy, hydroxymethyl, halomethyl, lower alkylthiomethyl or hydroxyiminomethyl,R.sup.2 is hydrogen, hydroxy, lower alkyl, pyridyl, amino, lower alkylamino, pyridylamino or guanidino optionally substituted with dimethylaminomethylene,R.sup.3 is dihydroisoquinolyl which may be substituted with halogen, lower alkyl, lower alkoxy, carboxy, hydroxy, pyridyl, amino, lower alkylamino, pyridylamino or guanidino,Q is --CO--, andn is an integer of 0 or 1, andpharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: January 27, 1984
    Date of Patent: March 10, 1987
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Takao Takaya, Hisashi Takasugi
  • Patent number: 4632927
    Abstract: A class of bicyclic nitrogen heterocyclic ether and thioether compounds exhibiting pharmacological activity including cytoprotective, H.sub.2 -antagonist, 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 are disclosed.
    Type: Grant
    Filed: March 20, 1984
    Date of Patent: December 30, 1986
    Assignee: William H. Rorer, Inc.
    Inventors: Henry F. Campbell, Donald E. Kuhla, William L. Studt, Stuart A. Dodson
  • Patent number: 4578393
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl or together are a group X which is C.sub.3-6 polymethylene optionally interrupted by O, S or NR.sub.6 wherein R.sub.6 is hydrogen or C.sub.1-6 alkyl;R.sub.3 is phenyl, optionally substituted by one or more substituents selected from halogen, CF.sub.3, nitro, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.2-7 alkanoyl, carboxyl, C.sub.1-6 alkoxycarbonyl, cyano, CONR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are selected from hydrogen or C.sub.1-6 alkyl or together are a group X; NR.sub.9 R.sub.10 wherein R.sub.9 and R.sub.10 are selected from hydrogen, C.sub.1-6 alkyl, C.sub.2-7 alkanoyl or C.sub.1-6 alkylsulphonyl or together are a group X; SO.sub.2 NR.sub.11 R.sub.12 wherein R.sub.11 and R.sub.12 are selected from hydrogen or C.sub.1-6 alkyl or together are a group X or S(O).sub.m R.sub.13 wherein m is 1 or 2 and R.sub.13 is C.sub.
    Type: Grant
    Filed: October 22, 1984
    Date of Patent: March 25, 1986
    Assignee: Beecham Group p.l.c.
    Inventors: Roger E. Markwell, Stephen A. Smith
  • Patent number: 4578390
    Abstract: Hydroxybenzylamino derivatives have been prepared from an appropriate hydroxybenzaldehyde and an amine followed by reduction. These compounds are found to be active topical anti-inflammatory agents.
    Type: Grant
    Filed: April 13, 1983
    Date of Patent: March 25, 1986
    Assignee: Merck & Co., Inc.
    Inventors: Norman P. Jensen, Michael N. Chang
  • Patent number: 4563476
    Abstract: Substituted 5-hydroxy-2,3-dihydrobenzofuran and analogs such as the substituted 6-hydroxy-2,3-dihydrobenzopyrans were prepared from an appropriately substituted (5-hydroxy-2,3-dihydrobenzofuran-6-yl) formaldehyde or analog thereof with an aryl amine followed by reduction. These compounds were found to be potent topical anti-inflammatory agents.
    Type: Grant
    Filed: November 21, 1983
    Date of Patent: January 7, 1986
    Assignee: Merck & Co., Inc.
    Inventors: Michael N. Chang, Milton L. Hammond, Norman P. Jensen, Robert A. Zambias
  • Patent number: 4520025
    Abstract: A class of bicyclic nitrogen 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 are disclosed.
    Type: Grant
    Filed: July 21, 1982
    Date of Patent: May 28, 1985
    Assignee: William H. Rorer, Inc.
    Inventors: Henry F. Campbell, Donald E. Kuhla, William L. Studt, Stuart A. Dodson