Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/23)
  • Patent number: 4946845
    Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are the same and are lower alkoxy or optionally substituted phenoxy,R.sup.3 is lower alkyl, lower alkoxy, or halo and m is 0, 1 or 2 or R.sup.3 is optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted phenyl lower alkoxy, amino, lower alkylamino, lower dialkylamino, cyano, or S(O).sub.n R wherein R is lower alkyl; optionally substituted phenyl; optionally substituted phenyl lower alkyl; or optionally substituted heterocyclic aryl of three to nine ring atoms containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the pharmaceutically acceptable acid addition salts thereof; and m is 1 and n is 0, 1 or 2;at least one of X or Y is C(O)W and the other X or Y is different and is hydrogen, C(O)W or R.sup.
    Type: Grant
    Filed: November 25, 1988
    Date of Patent: August 7, 1990
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: D. V. Krishna Murthy, Michael C. Venuti, John M. Young
  • Patent number: 4946860
    Abstract: Disclosed are novel benzothiopyranyl derivatives as 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors useful as antihypercholesterolemic agents represented by the formula: ##STR1## their corresponding dihydroxy acids, and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: November 3, 1989
    Date of Patent: August 7, 1990
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: Robert L. Morris, Jeffrey N. Barton
  • Patent number: 4946859
    Abstract: 4-(2-Methyl-2-hydroxypropylamino)-5,6-dihydrothieno[2,3-b]thiopyran-2-sulfo namide-7,7-dioxide is a major mammalian metabolite of 4-(2-methylpropylamino)-5,6-dihydrothieno[2,3-b]thiopyran-2-sulfonamide-7, 7-dioxide and is itself an active carbonic anhydrase inhibitor useful in the treatment of ocular hypertension by topical administration.
    Type: Grant
    Filed: July 31, 1989
    Date of Patent: August 7, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Jacob M. Hoffman, Jr., Ling L. Lee, Sandor L. Varga, Anthony G. Zacchei
  • Patent number: 4935441
    Abstract: Compounds of the formula I ##STR1## wherein rings A and B are each unsubstituted or substituted; Y is oxygen, sulfur, sulfinyl or sulfonyl; one of the symbols Z.sub.1 and Z.sub.2 is halogen and the other formyl; and pharmaceutically acceptable salts of such compounds that contain a salt-forming group are useful for the treatment of diseases of the respiratory tract and of liver diseases. They are prepared by methods known per se.
    Type: Grant
    Filed: May 28, 1986
    Date of Patent: June 19, 1990
    Assignee: Zyma SA
    Inventor: Christian G. Rimbault
  • Patent number: 4929627
    Abstract: Benzo-fused cycloalkane and oxa- and thia-cycloalkane trans-1,2-diamine compounds of the formula: ##STR1## wherein A, B, C, D, n, X, Y, R, R.sup.1, R.sup.2 and R.sup.3 are as defined in the specification, e.g., trans-3,4-dichloro-N-methyl-N-[2-(pyrrolidin-1-yl)-5-methoxy-1,2,3,4-tetra hydronaphth-1-yl]benezeneacetamide, and the pharmaceutically acceptable salts or N-oxides thereof, are useful as analgesics and/or diuretics.
    Type: Grant
    Filed: June 7, 1989
    Date of Patent: May 29, 1990
    Assignee: E. I. Du Pont De Nemours and Company
    Inventors: Penio Pennev, Parthasarathi Rajagopalan, Richard M. Scribner
  • Patent number: 4921871
    Abstract: The present invention relates to novel enolamide type compounds, pharmaceutical compositions, and methods of use thereof, useful in the treatment of diseases in which products of lipoxygenase enzyme activity or the action of leukotrienes contribute to the pathological condition.
    Type: Grant
    Filed: November 16, 1987
    Date of Patent: May 1, 1990
    Assignee: Warner-Lambert Company
    Inventors: Mary E. Carethers, Wiaczeslaw A. Cetenko, David T. Connor, Elizabeth A. Johnson, John S. Kiely, Charles F. Schwender, Jagadish C. Sircar, Roderick J. Sorenson, Paul C. Unangst, Robert F. Bruns
  • Patent number: 4918203
    Abstract: Disclosed is a practical and efficient process for preparing 6-substituted 4-chromanones from phenolic acrylate ester compounds derivable from para-substituted phenolic or thiophenolic compounds and beta-unsubstituted acrylic acid compounds which are esterifiable therewith. The process includes effecting rearrangement of a phenolic or thiophenolic acrylate ester in the presence of a rearrangement effective amount of hydrogen fluoride to the corresponding hydroxy - or mercapto (vinyl ketone) wherein the carbonyl carbon atom of the vinyl carboxy group is directly attached to the benzene ring ortho to the hydroxy or mercapto group. Thereafter, the vinyl ketone is cyclized to the corresponding 6-substituted 4-chromanone in the presence of a cyclization-effective amount of hydrogen fluoride. The 6-substituted 4-chromanones prepared by the process are useful as intermediates for preparing pharmaceutical agents.
    Type: Grant
    Filed: February 3, 1988
    Date of Patent: April 17, 1990
    Assignee: Mallinckrodt Inc.
    Inventors: Jerry R. Patton, Narayanasamy Gurusamy
  • Patent number: 4897402
    Abstract: Novel HMG-CoA reductase inhibitors are useful as antihypercholesterolemic agents and are represented by stuctural formulae (I) and (II): ##STR1## wherein A is O, S(O).sub.n or N--R.sub.13.
    Type: Grant
    Filed: June 29, 1988
    Date of Patent: January 30, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, George D. Hartman
  • Patent number: 4895868
    Abstract: Compounds of formula I ##STR1## in which: the R groups are independently hydrogen or lower alkyl; one of A and B is O or S and the other is --C(O)--, A being attached to the thiochroman ring at the 6 or 7-position;n is 0-5; andZ is H, an acid or acid derivative, an alcohol or alcohol derivative, acetal or acetal derivative or ketone or ketone derivative, or a pharmaceutically acceptable salt, have retinoid-like activity.
    Type: Grant
    Filed: June 29, 1988
    Date of Patent: January 23, 1990
    Assignee: Allergan, Inc.
    Inventor: Roshantha A. S. Chandraratna
  • Patent number: 4885298
    Abstract: The invention relates to pharmaceutical preparations containing compounds of formula I ##STR1## in which X represents unsubstituted or substituted amino or a quaternary ammonium salt; halogen, free, etherified or esterified hydroxy; free, etherified, esterified or oxidized mercapto; free or functionally modified carboxyl, free or functionally modified sulfo; acyl; nitro; an unsubstituted or substituted hydrocarbon radical or an unsubstituted or substituted heterocyclic radical, Y represents oxygen, sulfur, sulfinyl or sulfonyl but must be oxygen, sulfinyl or sulfonyl, if X is 1H-imidazol-1-yl, and rings A and B are each unsubstituted or substituted; or pharmaceutically acceptable salts of such compounds that contain a salt-forming group, and to novel compounds of formula I. The compounds are useful e.g. for the treatment of diseases of the respiratory tract and of liver diseases. They are prepared by methods known per se.
    Type: Grant
    Filed: August 2, 1988
    Date of Patent: December 5, 1989
    Assignee: Zyma SA
    Inventor: Christian G. Rimbault
  • Patent number: 4863922
    Abstract: Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.
    Type: Grant
    Filed: June 15, 1988
    Date of Patent: September 5, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello, Marcia E. Christy
  • Patent number: 4861913
    Abstract: Bicyclic sulfonamido derivatives represented by the formula: ##STR1## wherein R.sub.1 is a hydrogen or lower alkyl; R.sub.2 is an alkyl, substituted or unsubstituted aryl, aralkyl or heterocycle; R.sub.3 is a hydrogen or methyl; X is an alkylene or alkenylene which may be substituted by a fluorine atom or atoms an may contain an oxygen, sulfur and/or phenylene in the chain; Y is straight or branched alkylene or alkenylene, oxygen, or sulfur; m is 0 or 1; and n is 0, 1 or 2, or their salt, said derivatives being useful as antithrombotic, anti-vasoconstricting, and anti-bronchoconstricting drugs.
    Type: Grant
    Filed: November 5, 1986
    Date of Patent: August 29, 1989
    Assignee: Shionogi & Co., Ltd.
    Inventors: Masayuki Narisada, Mitsuaki Ohtani, Fumihiko Watanabe, Sanji Hagishita, Kaoru Seno, Susumu Kamata, Nobuhiro Haga, Tatsuo Tsuri, Tadahiko Tsushima, Kenji Kawada
  • Patent number: 4855213
    Abstract: Polymethine dyes are disclosed containing an acidic electron accepting terminal nucleus comprised of an isocyano group. The dyes are useful as spectral sensitizers in ultravioilet responsive imaging compositions.
    Type: Grant
    Filed: April 20, 1988
    Date of Patent: August 8, 1989
    Assignee: Eastman Kodak Company
    Inventor: Margaret E. Logan
  • Patent number: 4853410
    Abstract: Racemic and chiral (2R,4R)-4-c-hydroxy-2-4-(substituted)chroman(and thiochroman)-4-acetic acids and their pharmaceutically acceptable salts, their use in the treatment of diabetic complications and intermediates therefor.
    Type: Grant
    Filed: October 9, 1987
    Date of Patent: August 1, 1989
    Assignee: Pfizer Inc.
    Inventor: Christopher A. Lipinski
  • Patent number: 4843075
    Abstract: A benzothiopyrano[4,3-c]pyridazine compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each is hydrogen, halogen, trifluoromethyl, hydroxy, amino, nitro, cyano, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or C.sub.2-5 alkanoylamido, R.sup.3 is hydrogen, C.sub.1-8 alkyl, hydroxy-C.sub.1-4 alkyl, C.sub.2-5 alkanoyloxy-C.sub.1-4 alkyl, pyridyl, aryl, aryl-C.sub.1-4 alkyl, or aryl or aryl-C.sub.1-4 alkyl substituted by at least one substituent selected from the group consisting of halogen, trifluoromethyl, hydroxy, hydroxy, amino, nitro, cyano, C.sub.1-4 alkyl, C.sub.1-4 alkoxy and C.sub.2-5 alkanoylamido on the aromatic ring, n is 0, 1 or 2, and the bond between the 4-position and the 4a-position is a single bond or double bond, a method for production thereof and a use thereof.The compounds possess anti-anxietic activity and are useful as drugs.
    Type: Grant
    Filed: July 17, 1987
    Date of Patent: June 27, 1989
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Toru Nakao, Minoru Kawakami, Yasuto Morimoto, Shuzo Takehara, Tetsuya Tahara
  • Patent number: 4833254
    Abstract: Novel heteroarotinoid compositions characterized by the formulae: ##STR1## where: X is S or O; OAc is the acetate group ##STR2## and R is --H, --OH, --OCH.sub.3, or --OC.sub.2 H.sub.5 and includes ##STR3## for formulae (1) and (2). Such compositions exhibit activity as anticancer agents.
    Type: Grant
    Filed: May 11, 1987
    Date of Patent: May 23, 1989
    Assignee: The Board of Regents for the Oklahoma Agricultural and Mechanical Colleges acting for and on behalf of Oklahoma State University
    Inventors: Kenneth D. Berlin, Warren T. Ford, Shirish N. Rajadhyaksha, Jonathan B. Gale, Lyle W. Spruce
  • Patent number: 4831177
    Abstract: Compounds of formula X ##STR1## in which R.sub.6 is aryl, R.sub.7 is hydrogen, --OH or alkyl, R.sub.8 is alkyl, R.sub.9 is hydrogen, alkyl, alkenyl, aryl, furyl or --CCl.sub.3, when n is 1, R.sub.10 is alkyl, aryl, camphoryl, --CF.sub.3 or fluoro, or when n is 2, R.sub.10 is alkylene or arylene are latent curing catalysts for acid-curable stoving varnishes. On irradiation, the active curing catalysts which lead to acid-catalysed curing of the resins are formed from the compounds of the formula x.
    Type: Grant
    Filed: May 4, 1987
    Date of Patent: May 16, 1989
    Assignee: Ciba-Geigy Corporation
    Inventors: Rudolf Kirchmayr, Werner Rutsch
  • Patent number: 4829080
    Abstract: An aromatic benzopyranyl or benzothiopyranyl compound of the formula ##STR1## wherein n is 0 or 1,X represents ##STR2## R' represents H, OH, acyloxy or NH.sub.2, R" represents H or alkoxy orR' and R" taken together form an oxo, methano or hydroxyimino radical,R.sub.8 represents H, ##STR3## R.sub.9 represents H, alkyl, mono or polyhydroxyalkyl, aryl, aralkyl, a residue of a sugar or ##STR4## p equals 1, 2 or 3, r' and r" represent H, alkyl, monohydroxyalkyl, polyhydroxyalkyl, aryl, benzyl, the residue of an amino acid or an aminated sugar, or together form a heterocycle,R.sub.1, R.sub.2, R.sub.3 and R.sub.4 represents H or lower alkyl,R.sub.5, R.sub.6 and R.sub.7 represent H or methyl or when n=1, R.sub.5 and R.sub.7 taken together form with the benzene ring a naphthalene ring (R.sub.5 -R.sub.7 .dbd.--CH.dbd.CH--), andthe salts of said compounds as well as their geometric and optical isomers.These compounds are useful in pharmaceutical and cosmetic compositions.
    Type: Grant
    Filed: March 12, 1987
    Date of Patent: May 9, 1989
    Assignee: L'Oreal
    Inventors: Jean Maignan, Gerard Lang, Gerard Malle, Serge Restle, Braham Shroot
  • Patent number: 4826984
    Abstract: Novel heteroarotinoid compositions characterized by the formulae: ##STR1## where R is H, CH.sub.3 or C.sub.2 H.sub.5 and X is S, S O, O, NCH.sub.3, Si(CH.sub.3).sub.2, N.sup.+ (H)CH.sub.3 [Cl.sup.- ], N.sup.+ (H)CH.sub.3 [Br.sup.- ] or N.sup.+ (alkyl) CH.sub.3 [Cl.sup.- or Br.sup.-) where alkyl is CH.sub.3, C.sub.2 H.sub.5, CH.sub.2 .dbd.CHCH.sub.2 or C.sub.6 H.sub.5 CH.sub.2. Such compositions exhibit activity as anticancer agents.
    Type: Grant
    Filed: January 27, 1987
    Date of Patent: May 2, 1989
    Assignee: The Board of Regents for the Oklahoma Agricultural and Mechanical College acting for and on behalf of Oklahoma State University
    Inventors: Kenneth D. Berlin, Elizabeth M. Holt, Warren T. Ford, Mark D. Thompson
  • Patent number: 4824968
    Abstract: Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.
    Type: Grant
    Filed: June 26, 1987
    Date of Patent: April 25, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Gerald S. Ponticello, J. Mark Wiggins
  • Patent number: 4820848
    Abstract: Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.
    Type: Grant
    Filed: April 4, 1988
    Date of Patent: April 11, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Gerald S. Ponticello, Charles N. Habecker
  • Patent number: 4816474
    Abstract: Disclosed are compounds of the formula ##STR1## wherein A represents the divalent radical --S--CR.sub.4 .dbd.CR.sub.5 -- in which R.sub.4 and R.sub.5 independently represent hydrogen or lower alkyl; R.sub.1 represents hydrogen, lower alkyl or aryl-lower alkyl; R.sub.2 represents hydrogen, lower alkyl or aryl-lower alkyl; or R.sub.1 and R.sub.2 combined represent alkylene of 4 to 6 carbon atoms; R.sub.3 represents hydrogen or lower alkyl; an S-oxide thereof; or a pharmaceutically acceptable salt thereof; which are useful as presynaptic dopamine receptor agonists for the treatment of central nervous system disorders; processes for preparing same; and pharmaceutical compositions comprising said compounds.
    Type: Grant
    Filed: February 27, 1987
    Date of Patent: March 28, 1989
    Assignee: Ciba-Geigy Corporation
    Inventor: Alan J. Hutchison
  • Patent number: 4810804
    Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## where X is S, O or NR.sub.1 where R.sub.1 is hydrogen or lower alkyl; n is 0-5; R is H or lower alkyl and A is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative thereof, or --CHO or an acetal derivative thereof, or --COR.sub.2 or a ketal derivative thereof where R.sub.2 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4; or a pharmaceutically acceptable salt.
    Type: Grant
    Filed: March 26, 1987
    Date of Patent: March 7, 1989
    Assignee: Allergan, Inc.
    Inventor: Roshantha A. S. Chandraratna
  • Patent number: 4808597
    Abstract: Certain carboxylic acids of the formula ##STR1## and the pharmaceutically-acceptable salts thereof, and certain esters and amides thereof, are useful for inhibiting the degradation of articular cartilage when administered to a mammalian subject afflicted with an arthritic disease. X is O, S, SO, SO.sub.2, NH, NCH.sub.3 or NCOCH.sub.3 ; and n is zero or one.
    Type: Grant
    Filed: June 2, 1988
    Date of Patent: February 28, 1989
    Assignee: Pfizer Inc.
    Inventors: William W. Hoffman, Allen R. Kraska
  • Patent number: 4803286
    Abstract: Certain amino-2-hydroxypropyloximinoheterocycles are .beta.-adrenoceptor antagonists useful in the treatment of elevated intraocular pressure, hypertension, angina and arrhythmia.
    Type: Grant
    Filed: August 19, 1987
    Date of Patent: February 7, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello, David C. Remy, David A. Claremon, Stella W. King
  • Patent number: 4801605
    Type: Grant
    Filed: February 27, 1987
    Date of Patent: January 31, 1989
    Assignee: Ciba-Geigy Corporation
    Inventor: Alan J. Hutchison
  • Patent number: 4797413
    Abstract: Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.
    Type: Grant
    Filed: June 26, 1987
    Date of Patent: January 10, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello, Marcia E. Christy
  • Patent number: 4792556
    Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are the same and are lower alkoxy or optionally substituted phenoxy,R.sup.3 is lower alkyl, lower alkoxy, or halo and m is 0, 1 or 2 or R.sup.3 is optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted phenyl lower alkoxy, amino, lower alkylamino, lower dialkylamino, cyano, or S(O).sub.n R wherein R is lower alkyl; optionally substituted phenyl; optionally substituted phenyl lower alkyl; or optionally substituted heterocyclic aryl of three to nine ring atoms containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the pharmaceutically acceptable acid addition salts thereof; and m is 1 and n is 0, 1 or 2;at least one of X or Y is C(O)W and the other X or Y is different and is hydrogen, C(O)W or R.sup.
    Type: Grant
    Filed: April 28, 1986
    Date of Patent: December 20, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: D. V. K. Murthy, Michael C. Venuti, John M. Young
  • Patent number: 4788213
    Abstract: Novel p-[2(4,4-dimethyl-6-heterophenyl)substituted phenyl derivatives and salts thereof which are useful for combatting neoplasms and dermatoses including oral and topical compositions containing said derivatives which are suitable for such uses.
    Type: Grant
    Filed: May 5, 1983
    Date of Patent: November 29, 1988
    Assignee: Hoffman-La Roche Inc.
    Inventors: Michael Klaus, Peter Loeliger
  • Patent number: 4785004
    Abstract: Novel asymmetric thioethers of the formula ##STR1## in which the general symbols have the following meanings: R.sup.0 represents hydrogen or C.sub.1-7 -alkanoyl,R.sup.1 represents C.sub.1-3 -alkyl which may be substituted by one or more halogen atoms having an atomic number of at most 17,R.sup.2 represents an aliphatic radical having from 5 to 15 carbon atoms,A represents ethylene, a single bond or vinylene,B.sup.1 represents C.sub.1-7 -alkylene or phenylene,B.sup.2 represents a single bond, ethylene or phenylene, andM represents an aromatic radical of the partial formula ##STR2## in which the symbols have the following meanings: R.sup.3 represents hydrogen or C.sub.1-4 -alkyl,X represents NH, O, S or if R.sup.4 represents hydrogen, a single bond,one of the symbols R.sup.4 and R.sup.5 represents hydrogen and the other represents the group --CO--R.sup.6, orR.sup.4 and R.sup.5 together represent the radical --CO--C(R.sup.6).dbd.C(R.sup.7)--or--CO--C(R.sup.7).dbd.C(R.sup.6)--orR.sup.4 R.sup.
    Type: Grant
    Filed: December 15, 1986
    Date of Patent: November 15, 1988
    Assignee: Ciba-Geigy Corporation
    Inventors: Andreas Von Sprecher, Werner Breitenstein, Andreas Beck, Robert W. Lang, Konrad Oertle
  • Patent number: 4762853
    Abstract: 1-Oxo-1,3,4,7-tetrahydrobenzofuranes of the formula ##STR1## in which X is O or S,R is optionally substituted phenyl or heteroaryl,R.sup.1 is OH, monoalkylamino or dialkylamino, andR.sup.2 is an acyl or esterified carboxy radical,or pharmacologically acceptable salts thereof, which are active in circulation, e.g. they increase myocardial contractility, increase the flow of Ca.sup.2+ into the cell, increase blood pressure, reduce blood sugar, reduce swelling of mucous membranes and affect the salt and/or fluid balance.
    Type: Grant
    Filed: October 10, 1986
    Date of Patent: August 9, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Siegfried Goldmann, Matthias Schramm, Gunter Thomas, Rainer Gross
  • Patent number: 4751323
    Abstract: This invention relates to a polyaromatic cyanate which corresponds to the formula ##STR1## wherein Ar is an aromatic radical;B is a C.sub.7-20 polycyclic aliphatic radical;D is independently in each occurrence any non-active hydrogen-containing substituent;q, r and s are independently in each occurrence the integers b 0, 1, 2, l or b 3l ; with the proviso that the sum of q, 4 and s is greater than or equal to 2;t is independently in each occurrence an integer of between about 0 and 4 inclusive; andx is a number between about 0 and 5 inclusive.Another aspect of this invention is a novel polytriazine which comprises the reaction product of the polyaromatic cyanate esters of this invention. The novel polytriazines may further comprise the reaction product of the novel polyaromatic cyanates of this invention in admixture with other cyanates known in the art as useful for the preparation of polytriazines.
    Type: Grant
    Filed: November 16, 1983
    Date of Patent: June 14, 1988
    Assignee: The Dow Chemical Company
    Inventors: Edmund P. Woo, Daniel J. Murray
  • Patent number: 4742077
    Abstract: Compounds of formula I ##STR1## wherein R.sub.1 represents a group of formula ##STR2## whereby R.sub.4 and R.sub.5 are the same or different and represent hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl and X represents oxygen, sulfur, imino, lower alkylimino, --(CH.sub.2)--, --(S.CH.sub.2)-- or --(O.CH.sub.2)--,R.sub.2 represents hydrogen or lower alkyl,R.sub.3 represents a group of formula ##STR3## whereby R.sub.6, R.sub.7 and R.sub.8 are the same or different and represent hydrogen or alkyl or R.sub.6 together with R.sub.7 or R.sub.7 together with R.sub.8 represent --(CH.sub.2).sub.m -- wherein m is 3 to 6,R.sub.9 represents alkyl, alkenyl, trialkylsilyl or alkyl substituted by hydroxy, lower alkoxy, lower halogenalkyl or aryl andn stands for 1, 2 or 3,which possess pharmaceutical in particular antimycotic activity as well as activity against phytopathogenic fungi.
    Type: Grant
    Filed: September 8, 1986
    Date of Patent: May 3, 1988
    Assignee: Sandoz Ltd.
    Inventor: Anton Stutz
  • Patent number: 4720586
    Abstract: There are provided compounds of formula I, ##STR1## in which R.sub.1 represents OH,R.sub.2 and R.sub.3, which may be the same or different, each independently represent hydrogen, fluorine, chlorine, bromine, alkyl C1 to 6, nitro, nitrile, (CH.sub.2).sub.p R.sub.9 or SR.sub.9,W represents a single bond, a 1,2; 1,3; or 1,4-disubstituted benzene ring; a --CH.dbd.CH--group or a 1,4-cyclohexanediyl group;X respresents NH, O, S, SO.sub.2, CO, CH.sub.2, CONH or --COO;Y represents (CH.sub.2)q, CO, CS, SO.sub.2 and R.sub.20 represents hydrogen,or Y represents CR.sub.15 R.sub.16 CR.sub.17 R.sub.18,wherein the carbon atom bearing R.sub.15 and R.sub.16 is adjacent to X and in whichR.sub.15 and R.sub.18, together with the carbon atom to which they are attached form a carbonyl group, and R.sub.15, R.sub.16 and R.sub.20 each represent hydrogen, orR.sub.15 and R.sub.20 together form a chain --CH.sub.2 --, and R.sub.16, R.sub.17 and R.sub.18 each represent hydrogen, orR.sub.15, R.sub.16, R.sub.17 and R.sub.
    Type: Grant
    Filed: October 18, 1984
    Date of Patent: January 19, 1988
    Assignee: Fisons, plc
    Inventors: John Dixon, Francis Ince
  • Patent number: 4703057
    Abstract: The invention relates to 1-tert.-butylamino-3-(4-hydroxy-8-thiochromanyloxy)-2-propanol.
    Type: Grant
    Filed: September 30, 1986
    Date of Patent: October 27, 1987
    Assignee: ADIR Et Compagnie
    Inventors: Bernard Marchand, Yves M. Gargouil
  • Patent number: 4699919
    Abstract: This invention relates to bicyclic catechol derivatives having the general formulae I and II ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and Z represent various substituents, to a preparation process of the same comprising reacting a compound of formula III ##STR2## wherein R.sub.1 and R.sub.2 have the meanings given above with an appropriately substituted propionic or butyric acid (or an ester or a salt of the same) of formula IV ##STR3## wherein R.sub.3 has the meaning given above, and to therapeutical compositions wherein the active ingredient is one of these compounds.
    Type: Grant
    Filed: September 16, 1986
    Date of Patent: October 13, 1987
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques
    Inventors: Michel Follet, Marc Bonato
  • Patent number: 4684661
    Abstract: The invention relates to novel homopropargylamines of formula I ##STR1## wherein n is 2 or 3,R.sub.1 is a group of formula IIa, IIb or IIc ##STR2## in which R.sub.6 and R.sub.7 independently are H, halogen, CF.sub.3, lower alkyl or lower alkoxy,s is a number of 3 to 5,X is O, S, OCH.sub.2, SCH.sub.2, CH.sub.2 or NR.sub.8, andR.sub.8 is H or lower alkyl,R.sub.2 is H or lower alkyl, eitherR.sub.3 and R.sub.4, independently, are H or lower alkyl, orR.sub.3 and R.sub.4 together are (CH.sub.2).sub.u, in which u is a number of 3 to 5, andR.sub.5 is H, alkenyl or is a group selected from alkyl, trialkylsilyl, dialkylphenylsilyl, phenyl, phenylalkyl and cycloalkyl, in which alkyl, phenyl and cycloalkyl groups or moieties are unsubstituted or substituted by OH, lower alkyl, lower alkoxy, phenyl or halogen,in free base form or acid addition salt form thereof, their preparation, their chemotherapeutical and agricultural use and to compositions comprising such novel compounds and suitable for such use.
    Type: Grant
    Filed: November 20, 1985
    Date of Patent: August 4, 1987
    Assignee: Sandoz Ltd.
    Inventor: Anton Stuetz
  • Patent number: 4678793
    Abstract: Novel p-[2(4,4-dimethyl-6-heterophenyl)substituted phenyl derivatives and salts thereof which are useful for combatting neoplasms and dermatoses including oral and topical compositions containing said derivatives which are suitable for such uses.
    Type: Grant
    Filed: April 1, 1985
    Date of Patent: July 7, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Klaus, Peter Loeliger
  • Patent number: 4677115
    Abstract: Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.
    Type: Grant
    Filed: May 14, 1986
    Date of Patent: June 30, 1987
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Marcia E. Christy, Gerald S. Ponticello
  • Patent number: 4668691
    Abstract: 1-Oxo-1,3,4,7-tetrahydrobenzofuranes of the formula ##STR1## in which X is O or S,R is optionally substituted phenyl or heteroaryl,R.sup.1 is OH, monoalkylamino or dialkylamino, andR.sup.2 is an acyl or esterified carboxy radical, or pharmacologically acceptable salts thereof, which are active in circulation, e.g. they increase myocardial contractility, increase the flow of Ca.sup.2+ into the cell, increase blood pressure, reduce blood sugar, reduce swelling of mucous membranes and affect the salt and/or fluid balance.
    Type: Grant
    Filed: April 18, 1985
    Date of Patent: May 26, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Siegfried Goldmann, Matthias Schramm, G/u/ nter Thomas, Rainer Gross
  • Patent number: 4665202
    Abstract: The invention relates to pharmaceutical preparations containing compounds of formula I ##STR1## in which X.sub.1 and X.sub.2, independently of each other, represent hydrogen, halogen, unsubstituted or substituted amino or a quaternary ammonium salt; etherified or esterified hydroxy; free, etherified, esterified or oxidized mercapto; nitro; functionally modified formyl; free or functionally modified carboxyl; acyl; an unsubstituted or substituted hydrocarbon radical, or an unsubstituted or substituted heterocyclic radical; with the proviso that at least one of the radicals X.sub.1 and X.sub.2 is bonded by a carbon atom to the ring system and with the proviso that X.sub.1 and X.sub.2 cannot be together halogen and formyl; in which Y represents oxygen, sulfur, sulfinyl or sulfonyl but must be sulfur, sulfinyl or sulfonyl, if X.sub.1 is hydrogen and X.sub.
    Type: Grant
    Filed: August 24, 1984
    Date of Patent: May 12, 1987
    Assignee: Zyma SA
    Inventors: Christian G. Rimbault, Philippe M. Narbel
  • Patent number: 4638070
    Abstract: This invention relates to heterocyclic amino-alcohol derivatives of the formula ##STR1## These compounds are useful as antihypertensives.
    Type: Grant
    Filed: June 30, 1980
    Date of Patent: January 20, 1987
    Assignee: Continental Pharma
    Inventors: Georges E. Lambelin, Romeo R. Roncucci, Joseph Roba, Claude L. Gillet
  • Patent number: 4636575
    Abstract: Compounds of formula II and X ##STR1## wherein X is O, S, SO.sub.2, methylene, isopropylidene or NCOR.sub.7 where R.sub.7 is alkyl or phenyl, Y is a direct bond or methylene, n is 1 or 2, R.sub.4 is alkyl, phenyl, naphthyl, cycloalkyl, aralkyl, camphoryl, CF.sub.3, CCl.sub.3, F or NH.sub.2 ; or is alkylene, phenylene or naphthylene, R.sub.5 is hydrogen or halogen, R.sub.6 is hydrogen, alkyl, phenyl or cyano, R.sub.8 is substituted phenyl, substituted naphthyl, anthryl or phenanthryl, R.sub.9 is alkyl R.sub.10 is alkyl or substituted phenyl, and R.sub.11 is alkyl, substituted phenyl, naphthyl, camphoryl, alkylene, phenylene or naphthylene, are latent curing catalysts for acid-curable stoving lacquers. They are distinguished by satisfactory solubility in the acid-curable resin systems, can be stored virtually indefinitely in the dark and, when exposed to shortwave light, make it possible to cure the resins by acid catalysts at a relatively low temperature.
    Type: Grant
    Filed: December 17, 1984
    Date of Patent: January 13, 1987
    Assignee: Ciba-Geigy Corporation
    Inventor: Rudolf Kirchmayr
  • Patent number: 4628107
    Abstract: Novel chromone-8-aldehydes and thiochromone-8-aldehydes, useful in making pharmaceutically active dihydropyridines, of the formula ##STR1## in which R.sub.1 represents hydrogen, a C.sub.1 -C.sub.10 aliphatic hydrocarbon radical, a C.sub.1 -C.sub.10 alkyl carboxylate, or an aromatic or heteroaromatic ring which optionally has 1-5 identical or different halogen, C.sub.1 -C.sub.10 -alkyl, C.sub.1 -C.sub.10 -alkoxy, C.sub.1 -C.sub.10 -alkylthio, C.sub.1 -C.sub.10 -alkylsulphinyl, cyano, hydroxyl, nitro, C.sub.1 -C.sub.5 -monofluoroalkyl or polyfluoroalkyl, C.sub.1 -C.sub.5 monofluoroalkoxy or polyfluoroalkoxy, C.sub.1 -C.sub.6 monofluoroalkylthio or polyfluoroalkylthio, amino, C.sub.1 -C.sub.5 -monoalkylamino or C.sub.1 -C.sub.5 dialkylamino substituents,R.sub.2 represents hydrogen or 1 to 3 halogen atoms, A represents a single bond, a C.sub.1 -C.sub.20 alkylene chain or a C.sub.2 -C.sub.
    Type: Grant
    Filed: June 28, 1985
    Date of Patent: December 9, 1986
    Assignee: Bayer Aktiengesellschaft
    Inventors: Siegfried Goldmann, Gerhard Franckowiak, Matthias Schramm, Gunter Thomas, Rainer Gross
  • Patent number: 4624696
    Abstract: Cyclohexenone derivatives of the formula ##STR1## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the meanings stated in the description, herbicides which contain these compounds and a method for controlling undesirable plant growth.
    Type: Grant
    Filed: October 9, 1985
    Date of Patent: November 25, 1986
    Assignee: BASF Aktiengesellschaft
    Inventors: Michael Keil, Rainer Becker, Dieter Jahn, Dieter Kolassa, Ulrich Schirmer, Wolfgang Will, Bruno Wuerzer, Norbert Meyer
  • Patent number: 4614745
    Abstract: The invention relates to novel thiopyrones, especially novel benzothiopyranones of the general formula ##STR1## in which R.sub.1 represents hydrogen or an aliphatic radical, n represents 0, 1 or 2, Ph represents substituted or unsubstituted 1,2-phenylene and A represents a group of the formula --NH--CO--R in which R represents carboxy or esterified carboxy, and to their salts, processes for the manufacture of compounds of the formula (I) and their salts, pharmaceutical preparations containing such compounds and to the use of compounds of the formula (I) and their salts as the active ingredients of medicaments and/or for the manufacture of pharmaceutical preparations. The compounds of the formula (I) and their salts have anti-allergic properties.
    Type: Grant
    Filed: April 12, 1985
    Date of Patent: September 30, 1986
    Assignee: Ciba-Geigy Corporation
    Inventors: Atso Ilvespaa, Georges Haas
  • Patent number: 4609744
    Abstract: Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are leukotriene antagonists. These compounds inhibit SRS-A and leukotriene synthesis and are antagonists of SRS-A and are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.
    Type: Grant
    Filed: March 19, 1984
    Date of Patent: September 2, 1986
    Assignee: Merck Frosst Canada Inc.
    Inventors: Robert N. Young, Joshua Rokach, Haydn R. Williams, Masatoshi Kakushima, Yvan Guindon
  • Patent number: 4587342
    Abstract: Novel 2,4-diaminopyrimidines having substituted heterobicyclomethyl moieties in the 5-position have superior antibacterial properties.
    Type: Grant
    Filed: October 31, 1983
    Date of Patent: May 6, 1986
    Inventors: Susan M. Daluge, Paul M. Skonezny
  • Patent number: 4585786
    Abstract: The invention relates to hydroxy-4-2H-1-benzothiopyran-2-ones, represented by the following formula: ##STR1## in which, when R.sub.1 is hydrogen, R and AR' can form a tetrahydronaphtyl cycle; R and R.sub.1 can form a carbonyl group; R is a hydroxyl group when R.sub.1 is hydrogen; AR is a biphenyl or phenoxyphenyl group, which is substituted or non-substituted by a halogen, and AR' is a substituted or non-substituted phenyl group which may form with R a tetrahydronaphtyl cycle or a thienyl group. These compounds have interesting properties and may be used in particular as rodenticides.
    Type: Grant
    Filed: March 27, 1985
    Date of Patent: April 29, 1986
    Assignee: Lipha, Lyonnaise Industrielle Pharmaceutique
    Inventor: Jean-Jacques Berthelon
  • Patent number: 4581435
    Abstract: Alkyl-substituted thiapolycyclic polyahls such as dimethyl-9-thiabicyclononane diamines form polymers that have improved physical properties.
    Type: Grant
    Filed: April 27, 1984
    Date of Patent: April 8, 1986
    Assignee: The Dow Chemical Company
    Inventor: David W. Hughes