Benzene Ring In Acid Moiety Patents (Class 514/555)
  • Patent number: 5681838
    Abstract: The present invention relates to novel substituted amino compounds of the formula I:R.sup.1 -(A).sub.a -(B).sub.b -(D).sub.c -(CH.sub.2).sub.m -N(R.sup.2)-(CH.sub.2).sub.n -R.sup.3as defined in the present application, and to a process for preparing such compounds. The invention also includes pharmaceutical compositions containing the present compounds, and the preparation of such compositions. The invention also relates to the use of the present compounds as inhibitors of blood-platelet aggregation, formation of metastases by carcinoma cells, and the binding of osteoclasts to bone surfaces, in the treatment of hosts in need thereof.
    Type: Grant
    Filed: July 18, 1995
    Date of Patent: October 28, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerhard Zoller, Bernd Jablonka, Melitta Just, Otmar Klingler, Gerhard Breipohl, Jochen Knolle, Wolfgang Konig
  • Patent number: 5658954
    Abstract: A specially formulated environmental insecticide is provided which effectively controls whiteflies and other insects but is safe to humans, farm animals, pets, crops, and fish. The cost-effective non-polluting insecticide can be in the form of a 100% concentrate or an aqueous solution. The sprayable easy-to-use insecticide can comprise a synergistic blend of cottonseed oil amides, coconut oil amides, tall oil amides and a nonionic surfactant, as well as a chelating agent, a viscosity control agent and free amine.
    Type: Grant
    Filed: January 29, 1996
    Date of Patent: August 19, 1997
    Inventor: Eugene F. Targosz
  • Patent number: 5637616
    Abstract: A method for the topical or systemic treatment of disorders mediated by proteases which result in skin or mucosal lesions, and in particular, pemphigus, cicatricial pemphigoid, bullous pemphigoid, lichen planus, and canker sores, is disclosed wherein the host is treated with an effective amount of N-acetyl ysteine or a derivative thereof, or its pharmaceutically acceptable salt, optionally in a pharmaceutically acceptable diluent or carrier for systemic or topical delivery.
    Type: Grant
    Filed: October 5, 1993
    Date of Patent: June 10, 1997
    Assignee: Arcturus Pharmaceutical Corporation
    Inventors: Richard J. Sharpe, Maureen H. McAloon, Stephen J. Galli, Kenneth A. Arndt
  • Patent number: 5626838
    Abstract: The present invention provides novel methods for prevention or treatment of primary and recurring squamous cell carcinoma of the oral cavity or oropharynx comprising topical administration, to the oral cavity or oropharynx, of an effective amount of an NSAID, especially a composition administering from about 0.001% to about 0.2% ketorolac to the oral cavity, alone or as an adjunct to surgery and/or radiation therapy.
    Type: Grant
    Filed: March 13, 1995
    Date of Patent: May 6, 1997
    Assignee: The Procter & Gamble Company
    Inventor: Paul F. Cavanaugh, Jr.
  • Patent number: 5614510
    Abstract: The invention relates to an inositol phosphate containing pharmaceutical composition which comprises a nitrogen-containing compound for improvement of the bioavailability of the inositol phosphate in mammals including man at non-parenteral administration. The invention also covers the use of at least one nitrogen-containing compound for the preparing of an inositol phosphate containing medicament with improved bioavailibility of inositol phosphate in mammals including man at non-parenteral administration.
    Type: Grant
    Filed: August 22, 1994
    Date of Patent: March 25, 1997
    Assignee: Perstorp AB
    Inventor: Lars Persson
  • Patent number: 5614554
    Abstract: The present invention provides a reverse transcriptase inhibitor and an antiviral agent comprising at least one member selected from the group consisting of sulfated tyrosines and physiologically acceptable salts thereof as an effective component; and exhibiting less toxicity and a remarkable inhibitory effect against a reverse transcriptase existing in viruses as well as a remarkable anti-AIDS viral activity.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: March 25, 1997
    Assignee: Nippon Flour Mills Co., Ltd.
    Inventors: Keijiro Uchino, Takashi Mizuno, Sachie Murakami, Hideki Nakashima, Naoki Yamamoto, Hiroshi Ogawara
  • Patent number: 5567686
    Abstract: A method and pharmaceutical for protecting against mutational damage in mammalian cells, irrespective of the nature of the mutagenic event or source of radiational or chemical insult or the like.
    Type: Grant
    Filed: September 13, 1993
    Date of Patent: October 22, 1996
    Assignee: Arch Development Corporation
    Inventor: David J. Grdina
  • Patent number: 5510385
    Abstract: A pharmaceutical composition for oral use containing the salt of S(+)-2-(4-isobutylphenyl)propionic acid with a basic aminoacid selected between L-arginine and L-lysine is described.
    Type: Grant
    Filed: June 7, 1994
    Date of Patent: April 23, 1996
    Assignee: Zambon Group S.p.A.
    Inventors: Federico Stroppolo, Daniele Bonadeo, Gian F. Fornasini, Annibale Gazzaniga
  • Patent number: 5496857
    Abstract: A specially formulated environmental insecticide is provided which effectively controls whiteflies and other insects but is safe to humans, farm animals, pets, crops, and fish. The cost-effective non-polluting insecticide can be in the form of a 100% concentrate or an aqueous solution. The sprayable easy-to-use insecticide can comprise a synergistic blend of cottonseed oil amides, coconut oil amides, tall oil amides and a nonionic surfactant, as well as a chelating agent, a viscosity control agent and free amine.
    Type: Grant
    Filed: March 17, 1994
    Date of Patent: March 5, 1996
    Inventor: Eugene F. Targosz
  • Patent number: 5449668
    Abstract: The invention relates to a new vitamin D compound of the general formula ##STR1## wherein: R.sub.1 is a hydrogen atom or a hydroxy group;R.sub.2 is a (C.sub.1 -C.sub.3)alkyl group, a hydroxy(C.sub.1 -C.sub.3)alkyl group, a (C.sub.1 -C.sub.2)alkoxymethyl group or a (C.sub.2 -C.sub.3)alkenyl or alkynyl group;R.sub.3 is a branched or non-branched, saturated or unsaturated aliphatic 3- to 5 -membered hydrocarbon or oxahydrocarbon biradical, having at least 3 atoms in the main chain and being optionally substituted with one or more substituents selected from epoxy, fluoro and hydroxy;R.sub.4 is a sec. or tert. (C.sub.3 -C.sub.6)alkyl group or a (C.sub.3 -C.sub.6)cycloalkyl group; andA and B are each individually hydrogen atoms or methyl groups, orA and B form together a methylene group.The invention further relates to a method of preparing these compounds and to their use in pharmacotherapy and cosmetics.
    Type: Grant
    Filed: June 4, 1993
    Date of Patent: September 12, 1995
    Assignee: Duphar International Research B.V.
    Inventors: Jose P. Sestelo, Antonio Mourino, Jose L. Mascarenas, Sebastianus J. Halkes, Jan Zorgdrager, Gerhardus D. H. Dijkstra, Jan-Paul van de Velde
  • Patent number: 5385931
    Abstract: The invention relates to new sulphonamide derivatives of benzo-cyclic or benzo-heterocyclic acids and their derivatives of general formula I ##STR1## in which: R represents a straight-chain or branched lower alkyl radical having 1 to 9 C;a phenyl radical which is unsubstituted or substituted by one or more groups:straight-chain or branched lower alkyl having 1 to 4 C, halogeno, alkoxy, nitro, amino, dialkylamino or CF.sub.3 ;a substituted or unsubstituted naphthalene;a thiophenyl radical;R.sub.1 represents a hydrogen or a straight-chain or branched lower alkyl or a benzyl;R.sub.2 represents a hydrogen, a straight-chain or branched lower alkyl group, a substituted or unsubstituted phenyl group or an aralkyl group;R.sub.3 represents a hydrogen or a straight-chain or branched lower alkyl (1 to 6 C);--X-- represents a divalent functional radical chosen from the following: --CH.sub.2 --; ##STR2## where R.sub.
    Type: Grant
    Filed: December 28, 1990
    Date of Patent: January 31, 1995
    Assignee: Pierre Fabre Medicament
    Inventors: Dennis Bigg, Alain Duflos, Jean-Pierre Rieu
  • Patent number: 5331011
    Abstract: Disclosed is an N-benzyl-N-phenoxyethylamine selected from the group consisting of the N-benzyl-N-phenoxyethylamine represented by the following formula (I): ##STR1## and an agriculturally acceptable acid addition salt represented by the following formula (II): ##STR2## wherein m represents a number of 1 or 2 with a proviso that when m is 1 and a chlorine atom in the ring A is present at para(4)-position of the ring A, two chlorine atoms in the ring B are present at 2,3-, 2,5-, 2,6-, 3,4- or 3,5-positions of the ring B, and HX represents an acid.
    Type: Grant
    Filed: April 7, 1993
    Date of Patent: July 19, 1994
    Assignee: Mitsubishi Gas Chemical Co., Inc.
    Inventors: Mitsunori Oda, Kazutoshi Kikkawa, Akinori Tanaka, Satoko Imaruoka, Shigeo Yoshinaka
  • Patent number: 5132118
    Abstract: A method and composition for the preventive and curative treatment of exercise-induced pulmonary hemorrhage in animals. The method comprises administration to the animal of a mixture of urea, alkaline potassium salts and magnesium salts. The composition comprises a mixture of urea, alkaline potassium salts, and magnesium salts, and if required, a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: November 29, 1990
    Date of Patent: July 21, 1992
    Inventor: John A. Mills
  • Patent number: 5114716
    Abstract: An anti-oxidant system contains, in combination, at least one stabilized ascorbyl ester, at least one tocopherol or a mixture of tocopherols, or cafeic acid or a derivative thereof, at least one complexing agent and at least one non-thiol polypeptide. The anti-oxidant system is employed to stabilize fatty bodies and cosmetic compositions.
    Type: Grant
    Filed: July 28, 1989
    Date of Patent: May 19, 1992
    Assignee: Societe Anonyme Dite: L'Oreal
    Inventors: Quang L. N'Guyen, Jacqueline Griat, Francois Millecamps, Gerard Lang, Serge Forestier
  • Patent number: 5011854
    Abstract: A hydroxamic acid compound represented by the general formula (I) or a salt thereof; ##STR1## wherein R.sup.1 represents a hydrogen atom, or a substituted or unsubstituted alkanoyl group, R.sup.2 represents an unsubstituted alkanoyl, substituted lower alkanoyl or substituted lower alkyl group, and m represents an integer of 3 to 7, which are useful for the prevention and/or treatment of diseases caused by lipoxygenase-mediated metablites.
    Type: Grant
    Filed: December 7, 1989
    Date of Patent: April 30, 1991
    Assignee: Kyowa Hakko Kogyo Co. Ltd.
    Inventors: Mitsuru Takahashi, Shigeto Kitamura, Hiroshi Kase, Masaji Kasai, Isao Kawamoto, Takao Iida, Hiroshi Sano, Hiromitsu Saito, Koji Yamada, Chikara Murakata
  • Patent number: 5001156
    Abstract: Lipophilic quaternary ammonium salicylate, characterized in that it corresponds to the formula: ##STR1## in which: (i) R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be identical or different, denote an alkyl or alkylcycloalkyl radical, optionally substituted or interrupted;(ii) R.sub.3 and/or R.sub.4 denote(s) a group:R.sub.8 [OC.sub.2 H.sub.3 R.sub.7 ].sub.n [OCH.sub.2 CHOH--CH.sub.2 ].sub.pin which 0.ltoreq.n.ltoreq.4 and p denotes 0 or 1; R.sub.8 denotes H or an alkyl, alkenyl, alkylcycloalkyl or alkylaryl radical;(iii) R.sub.4 denotes an alkylphenyl radical;(iv), (v) R.sub.1 and R.sub.2 can form a saturated or unsaturated aromatic or non-aromatic heterocycle;(vi) R.sub.1, R.sub.2 and R.sub.3 form polycyclic derivatives with the nitrogen atoms; R.sub.5 denotes a group corresponding to the formula: ##STR2## in which n is an integer varying between 0 and 10.
    Type: Grant
    Filed: December 1, 1987
    Date of Patent: March 19, 1991
    Assignee: L'Oreal
    Inventors: Michel Philippe, Henri Sebag, Michel Hocquaux, Bernard Jacquet, Jean P. Laugier
  • Patent number: 4960772
    Abstract: A pharmaceutical and cosmetic composition for topical application comprises in a physiologically acceptable medium a combination of benzoyl peroxide and a quaternary ammonium salt selected from a quaternary ammonium alkyl sulfate of sulfonate, an aryl sulfonate and an alkyl aryl sulfonate.
    Type: Grant
    Filed: February 23, 1989
    Date of Patent: October 2, 1990
    Assignee: L'Oreal
    Inventors: Henri Sebag, Irina Beck
  • Patent number: 4959394
    Abstract: The L-arginine salt of N-(D)-{[2-(2,6-dichlorophenylamino}phenyl]acetyl]aspartic acid, represented by the formula ##STR1## in which AmH .sym. represents the cation derived from L-arginine Am of the formula ##STR2## and its hydrates exhibit and excellent water-solubility and a physiologically favorable pH value and also a pleasant taste in aqueous solutions and are therefore excellently suitable for enternal and parenteral forms of administration. It is manufactured by reacting L-arginine with D-{[2-(2,6-dichlorophenylamino)phenyl]-acetyl}aspartic acid.
    Type: Grant
    Filed: November 17, 1989
    Date of Patent: September 25, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Gerhard Baschang, Alfred Sallman
  • Patent number: 4945112
    Abstract: Guanidiniumdodecylbenzene sulfonates of the formula ##STR1## where R is the group --H, --CH.sub.3 or ##STR2## and X is 1, 2, 3 or 4, and fungicides containing these compounds.
    Type: Grant
    Filed: March 16, 1989
    Date of Patent: July 31, 1990
    Assignee: BASF Aktiengesellschaft
    Inventors: Matthias Zipplies, Hubert Sauter, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 4897422
    Abstract: Compounds of the formula: ##STR1## where R.sub.1 is amino or methyl; R.sub.2 is C.sub.1 -C.sub.2 alkyl; R.sub.3 is one or more substituents selected from hydrogen, halogen or trihalomethyl; R.sub.4 is one or more substituents selected from hydrogen, halogen, trihalomethyl, C.sub.1 to C.sub.4 alkoxy or C.sub.1 to C.sub.4 alkyl; and M is hydrogen, a pharmaceutically acceptable cation, aroyl, or C.sub.1 to C.sub.6 alkoyl are inhibitors of 5- and/or 12-lipoxygenase enzymes.
    Type: Grant
    Filed: February 10, 1987
    Date of Patent: January 30, 1990
    Assignee: Abbott Laboratories
    Inventor: James B. Summers, Jr.
  • Patent number: 4895842
    Abstract: A phenylalanine derivative having the formula (I): ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen provided that both R.sup.1 and R.sup.2 are not hydrogen at the same time;C.sub.1 -C.sub.8 alkyl which may be substituted with hydroxy, hydroxycarbonyl, C.sub.1 -C.sub.4 alkoxycarbonyl, C.sub.1 -C.sub.4 alkylmercapto, C.sub.1 -C.sub.4 alkoxy, carbamoyl, sulfamoyl, pyridyl, or phenyl which may further be substituted with nitro, C.sub.1 -C.sub.4 alkoxy, or halogen;C.sub.6 -C.sub.8 cycloalkyl which may be substituted with hydroxy, C.sub.1 -C.sub.4 alkoxy, hydroxylcarbonyl, C.sub.1 -C.sub.4 alkoxycarbonyl, or C.sub.1 -C.sub.4 alkyl;phenyl which may be substituted with halogen, nitro, trifluoromethyl, C.sub.1 -C.sub.4 alkoxy C.sub.1 C.sub.4 alkylmercapto, C.sub.1 -C.sub.4 alkylcarbonyl, phenylcarbonyl, hydroxycarbonyl, C.sub.1 -C.sub.4 alkoxycarbonyl, carbamoyl, sulfamoyl, amidino, pyridylcarbonyl, or C.sub.1 -C.sub.6 alkyl which may further be substituted with C.sub.1 -C.sub.
    Type: Grant
    Filed: September 29, 1986
    Date of Patent: January 23, 1990
    Assignees: Shosuke Okamoto, Showa Denko Kabushiki Kaisha
    Inventors: Shosuke Okamoto, Yoshio Okada, Akiko Okunomiya, Taketoshi Naito, Yoshio Kimura, Morihiko Yamada, Norio Ohno, Yasuhiro Katsuura, Yumi Seki
  • Patent number: 4891386
    Abstract: A new compound, namely lidocaine salicylate monohydrate of formula: ##STR1## has been proposed, which has shown strong local anesthetic and cardiac antiarrhythmic activity.
    Type: Grant
    Filed: September 17, 1984
    Date of Patent: January 2, 1990
    Assignee: Molteni & C. Dei F.lli Alitti S.p.A.
    Inventor: Franca A. Gasparotti
  • Patent number: 4883786
    Abstract: Novel derivatives of L-carnitine or of L-acylcarnitines or of esters thereof, obtained by salification with suitable acids or acidic aminoacids, monosalified with potassium ion.These derivatives show cardiotropic properties in the therapy of myocardial anoxia, of ischemia, of arrythmic syndromes, of cardiac failures in general and in cases of increased energy request due to fatigue at cardiac and muscular level.
    Type: Grant
    Filed: December 8, 1988
    Date of Patent: November 28, 1989
    Assignee: Magis Farmaceutici Srl
    Inventor: Laura Puricelli
  • Patent number: 4880840
    Type: Grant
    Filed: June 30, 1987
    Date of Patent: November 14, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans Lindel, Axel Ingendoh, Friedrich Berschauer, Anno de Jong, Martin Scheer
  • Patent number: 4876282
    Abstract: The present invention provides 1-phenyl-(naphthalenyl)alkylamines which are selective inhibitors of serotonin uptake.
    Type: Grant
    Filed: November 25, 1987
    Date of Patent: October 24, 1989
    Assignee: Eli Lilly and Company
    Inventors: David W. Robertson, David T. Wong
  • Patent number: 4818767
    Abstract: The compounds of formula (I) ##STR1## wherein R.sub.1 is hydrogen or an alkyl radical containing one to six carbon atoms and R.sub.2 is an alkyl radical containing one to six carbon atoms possess markedly increased activity against malaria-causing parasites. Pharmaceutical compositions and method of treatment of subjects with malaria are also disclosed.
    Type: Grant
    Filed: November 2, 1983
    Date of Patent: April 4, 1989
    Assignee: SmithKline Beckman Corporation
    Inventor: Jean F. Rossignol
  • Patent number: 4797423
    Abstract: It is hereby described and claimed the new lysine salt of 4-diphenylacetic acid, having an antiinflammatory and analgesic activity, its preparation method and the pharmaceutical compositions containing it which are therapeutically useful both systemically and topically.
    Type: Grant
    Filed: September 22, 1987
    Date of Patent: January 10, 1989
    Assignee: S.I.F.I. Societa Industria Farmaceutica Italiana S.p.A.
    Inventor: Giuseppe Benanti
  • Patent number: 4792551
    Abstract: Compounds useful for treating inflammation, pain and swelling, represented by the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein: Y and Z are each independently halo, alkyl or alkoxy;l and m are each independently integers of 0-4;b is an integer of 2-12; andX is selected from the group consisting of:--NR.sup.1 R.sup.2, --NR.sup.1 (CH.sub.2 CH.sub.2 OH), ##STR2## in which R.sup.1 and R.sup.2 are independently H, alkyl or cycloalkyl;R.sup.3 is H, alkyl or CH.sub.2 CH.sub.2 OH; andn is an integer of 3-7.
    Type: Grant
    Filed: July 15, 1983
    Date of Patent: December 20, 1988
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Peter H. Nelson, Stefan H. Unger, Thomas R. Thieme
  • Patent number: 4767784
    Abstract: The invention relates to novel crystalline salts of aryloxypropanolamines with diphenylacetic acid, a process for their preparation and the use of these salts for the preparation of chemically pure aryloxy-propanolamines or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: November 28, 1986
    Date of Patent: August 30, 1988
    Inventors: Gerhard Zolss, Gerhard Pfarrhofer
  • Patent number: 4764534
    Abstract: 4-Substituted-N-[2,4-dinitro-6-(trifluoromethyl)phenyl]-1-naphthalenamine derivatives, useful as anticoccidial agents both alone and in combination with polyether antibiotics.
    Type: Grant
    Filed: July 17, 1984
    Date of Patent: August 16, 1988
    Assignee: Eli Lilly and Company
    Inventors: Albert J. Clinton, deceased, George O. P. O'Doherty
  • Patent number: 4751242
    Abstract: Oral or parenteral administration of 1,000-2,000 mg/day of acetyl L-carnitine or an equivalent amount of a pharmacologically acceptable salt thereof to patients affected by acute or chronic peripheral neuropathy dramatically improves their symptomatological pattern.
    Type: Grant
    Filed: July 27, 1987
    Date of Patent: June 14, 1988
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Menotti Calvani, Luigi Mosconi
  • Patent number: 4748174
    Abstract: The water soluble acid addition salts of an NSAID, such as acetylsalicylic acid, fenbufen, diflunisal, piroxicam, naproxen, or the like, with either glucamine or meglumine (N-methylglucamine) are useful anti-inflammatory and analgesic drugs, well adopted for parenteral, oral, rectal or topical administration.
    Type: Grant
    Filed: January 5, 1987
    Date of Patent: May 31, 1988
    Assignee: Therapicon s.r.l.
    Inventor: Paolo A. Veronesi
  • Patent number: 4717736
    Abstract: Compounds having the formula: ##STR1##are antagonists of leukotrienes of C.sub.4, D.sub.4 and E.sub.4, the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory agents and cytoprotective agents.
    Type: Grant
    Filed: November 21, 1984
    Date of Patent: January 5, 1988
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Joshua Rokach, Robert N. Young
  • Patent number: 4704403
    Abstract: Novel compounds, viz. 3-(2,2,2-trisubstituted hydrazinium) propionates have the following general formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are an alkyl, a substituted alkyl, a substituted or unsubstituted aryl, an aralkyl or an unsaturated alkyl;R.sup.4, R.sup.5 are hydrogen or a lower alkyl; n is 0 to 2, except for the case where R.sup.1, R.sup.2 and R.sup.3 are methyl, R.sup.4 and R.sup.5 are not hydrogen.The compounds of the present invention possess both hypotensive and antiarrhythmic activity and are useful in medicine.
    Type: Grant
    Filed: December 27, 1985
    Date of Patent: November 3, 1987
    Inventors: Gunar A. Bremanis, Ivars Y. Kalvinsh, Irene B. Antsena, Edmund Y. Lukevits, Maris M. Veveris, Marina L. Erenshtein, Valdis D. Mikazhan, Valeryans Y. Kauss, Edvard E. Liepinsh, Petr T. Trapentsier
  • Patent number: 4689346
    Abstract: Compounds for effecting hemostatic and antifibrinolytic action, namely a 1-acylamino naphthalene-4 sulphonic acid derivative of the formula ##STR1## and compositions and method of achieving such action.
    Type: Grant
    Filed: October 28, 1985
    Date of Patent: August 25, 1987
    Assignee: Laboratorio Fides, S.A.
    Inventors: Pere P. Llobet, Elisa G. Baylina
  • Patent number: 4672077
    Abstract: The D-6-methoxy-alpha-methyl-2-naphthalenacetate of 1-carboxy-N-N',N"-trimethylmethanamine sodium salt, which is prepared by reacting 1-carboxy-N,N',N"-trimethylmethanamine sodium salt and D-6 methoxy-methyl-2-naphtalenacetic acid, at a temperature of between 10.degree. and 30.degree. C., shows a better and more ready absorption and higher tolerability at the level of the gastric mucosa.
    Type: Grant
    Filed: June 3, 1986
    Date of Patent: June 9, 1987
    Assignee: Istituto Biochimico Pavese SpA
    Inventor: Nelly Colombi
  • Patent number: 4665094
    Abstract: Hydroxyalkyl-phenoxy-propan-2-olamines and novel esters thereof are oculoselective .beta.-blockers useful in the treatment of elevated intraocular pressure with little or no effect on the pulmonary or cardiovascular system.
    Type: Grant
    Filed: August 29, 1985
    Date of Patent: May 12, 1987
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello
  • Patent number: 4659739
    Abstract: An agricultural and horticultural fungicide of low phytotoxicity comprising as an active ingredient an addition salt between a fungicidal guanidine compound and an acid having an oleophilic group with at least 9 carbon atoms in total. The acid addition salt is produced by reacting a fungicidal guanidine compound or its acid addition salt with an acid having an oleophilic group with at least 9 carbon atoms in total or its salt.
    Type: Grant
    Filed: February 25, 1985
    Date of Patent: April 21, 1987
    Assignee: Dainippon Ink and Chemicals, Inc.
    Inventors: Nobuyuki Yoshioka, Yasuji Okunishi, Yasuhisa Miura, Yoshikazu Mori, Yasuki Kataoka, Eiichi Adachi
  • Patent number: 4654371
    Abstract: The compounds of the formula (II): ##STR1## and their pharmaceutically acceptable salts wherein R.sub.1 is a hydrogen, fluorine or chlorine atom or a hydroxyl, hydroxymethyl, methyl, methoxyl, amino, formamido, acetamido, methylsulphonylamido, nitro, benzyloxy, methylsulphonylmethyl, ureido, trifluoromethyl or p-methoxybenzylamino group; R.sub.2 is a hydrogen, fluorine or chlorine atom or a hydroxyl group; R.sub.3 is a hydrogen or chlorine atom or a hydroxyl group; R.sub.4 is a carboxylic acid group or a salt, ester or amide thereof; R.sub.5 is a hydrogen, chlorine or fluorine atom or a methyl, methoxyl or hydroxyl group or a carboxylic acid group or a salt, ester or amide thereof; R.sub.6 is a hydrogen atom or a methyl, or propyl group; X is an oxygen atom or a bond; and Y is an alkylene group of up to 6 carbon atoms or a bond have been found to possess anti-obesity and/or anti-hyperglycaemic activity.
    Type: Grant
    Filed: October 8, 1985
    Date of Patent: March 31, 1987
    Assignee: Beecham Group p.l.c.
    Inventors: Anthony T. Ainsworth, David G. Smith
  • Patent number: 4623661
    Abstract: Compounds of the formula ##STR1## where R.sub.1 is a trinuclear aromatic or biaryl group; R.sub.2 is hydrogen or C.sub.1 to C.sub.6 alkyl or cycloalkyl; n is 0 or 1; and M is a pharmaceutically acceptable cation, are potent inhibitors of the enzymes 5-, 12-, and 15-lipoxygenase.
    Type: Grant
    Filed: April 26, 1985
    Date of Patent: November 18, 1986
    Assignee: Abbott Laboratories
    Inventor: James B. Summers, Jr.
  • Patent number: 4609673
    Abstract: The present invention provides carboxylic acid derivatives of the general formula: ##STR1## wherein R is a hydrogen atom, alkyl, a metal cation or an ammonium or alkylammonium ion, R.sub.1 is a hydrogen atom, a hydroxyl group or an alkyl, O-alkyl,O-benzyl or O-acyl radical, R.sub.2 is a hydrogen atom or an alkyl, aryl or aralkyl radical, n is 0, 1 or 2 and R.sub.
    Type: Grant
    Filed: December 18, 1984
    Date of Patent: September 2, 1986
    Assignee: Boehringer Mannheim GmbH
    Inventors: Hermann Eggerer, Bernd Hagenbruch, Tran G. Nguyen, Karlheinz Stegmeier, Johannes Pill
  • Patent number: 4608390
    Abstract: Compounds of the formula ##STR1## where X is selected from hydrogen, C.sub.1 to C.sub.22 alkyl or alkenyl, or an electron withdrawing group;n=0 or 1 and m=0, 1, 2 or 3; but n and m are not O simultaneously;R.sub.1 and R.sub.2 independently are hydrogen, C.sub.1 to C.sub.6 alkyl, an electron withdrawing group, or R.sub.4 ;R.sub.3 is H, C.sub.1 to C.sub.6 alkyl or cycloalkyl, or R.sub.4 ; andR.sub.4 independently at each occurrence, has the formula ##STR2## where Y is hydrogen or an electron withdrawing group; and wherein M is a pharmaceutically acceptable cation, are potent inhibitors of lipoxygenase enzymes.
    Type: Grant
    Filed: April 26, 1985
    Date of Patent: August 26, 1986
    Assignee: Abbott Laboratories
    Inventor: James B. Summers, Jr.
  • Patent number: 4607053
    Abstract: Arylhydroxamates are provided having the structure ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, aryl, lower alkenyl, cycloalkenyl, aralkyl, or ##STR2## wherein n is 1 to 4 and X is hydroxy, alkoxy, amino, C.sub.1 -C.sub.4 -alkylamino or C.sub.1 -C.sub.4 -dialkylamino.R.sup.2 is hydrogen or lower alkyl; andR.sup.3 is C.sub.1 -C.sub.20 alkyl or C.sub.3 -C.sub.20 alkenyl, aryl, aryl-alkyl, cycloalkyl, aryl-alkenyl, lower alkoxy, lower alkenyloxy, aryl-alkoxy or cycloalkyloxy.These compound are useful as inhibitors of .DELTA..sup.5 -lipoxygenase and as such are useful as antiallergy agents.
    Type: Grant
    Filed: April 4, 1985
    Date of Patent: August 19, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Donald S. Karanewsky, Martin F. Haslanger
  • Patent number: 4605669
    Abstract: Compounds of the formula ##STR1## where R.sub.1 is H, or C.sub.1 to C.sub.6 alkyl; R.sub.2 is selected from C.sub.1 to C.sub.22 alkyl, cycloalkyl, aralky or alkenyl; and M is a pharmaceutically acceptable cation, are potent inhibitors of the enzymes 5-, 12- and 15-lipoxygenase.
    Type: Grant
    Filed: April 26, 1985
    Date of Patent: August 12, 1986
    Assignee: Abbott Laboratories
    Inventor: James B. Summers, Jr.
  • Patent number: 4604407
    Abstract: Hydroxamates are provided having the structure ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, aryl, lower alkenyl, cycloalkenyl, aralkyl, or ##STR2## wherein n is 1 to 4 and X is hydroxy, alkoxy, amino, C.sub.1 -C.sub.4 -alkylamino or C.sub.1 -C.sub.4 -dialkylamino.R.sup.2 is hydrogen or lower alkyl; andR.sup.3 is C.sub.1 -C.sub.20 alkyl or C.sub.3 -C.sub.20 alkenyl, aryl, aryl-alkyl, cycloalkyl, aryl-alkenyl, lower alkoxy, lower alkenyloxy, aryl-alkoxy or cycloalkyloxy, and m is 0 to 5. These compounds are useful as inhibitors of .DELTA..sup.5 -lipoxygenase and as such are useful as antiallergy agents.
    Type: Grant
    Filed: April 4, 1985
    Date of Patent: August 5, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Martin F. Haslanger, Donald S. Karanewsky
  • Patent number: 4602023
    Abstract: The present invention provides various novel diphenic acid monoamide compounds, novel pharmaceutical compositions and methods of use thereof, as well as novel methods of synthesis therefor. The novel diphenic acid monoamides of the present invention are leukotriene antagonists, 5-lipoxygenase inhibitors, and mediator release inhibitors providing activity useful for treating asthma, allergies, cardiovascular diseases, migraines, and immunoinflammatory conditions.
    Type: Grant
    Filed: June 3, 1985
    Date of Patent: July 22, 1986
    Assignee: Warner-Lambert Company
    Inventors: John S. Kiely, Suchin Huang
  • Patent number: 4587356
    Abstract: The present invention provides an improved method for producing a nuclear substituted cinnamoylanthranilic acid compound.Illustrative of the process is the reaction of 3-hydroxy-4-methoxybenzaldehyde with 2-carboxymalonanilic acid in an inert solvent medium in the presence of a molar excess of piperidine to provide a high purity intermediate salt precipitate, and the salt is treated with an acidic reagent to yeild N-(3-hydroxy-4-methoxycinnamoyl)anthranilic acid product.
    Type: Grant
    Filed: September 25, 1984
    Date of Patent: May 6, 1986
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Kinji Iizuka, Tetsuhide Kamijo, Ryoji Yamamoto, Hiromu Harada
  • Patent number: 4568693
    Abstract: Herein disclosed are N-naphthoylglycine derivatives having aldose reductase inhibiting activity. The derivatives are useful for treating diabetic complications.
    Type: Grant
    Filed: September 9, 1983
    Date of Patent: February 4, 1986
    Assignee: Ayerst, McKenna & Harrison, Inc.
    Inventors: Kazimir Sestanj, Nedumparambil A. Abraham, Francesco Bellini, Adi Treasurywala
  • Patent number: 4562211
    Abstract: 2-Substituted-1-(omega-aminoalkoxy)benzenes are prepared and found useful as pharmaceutical agents, particularly as antidepressants.
    Type: Grant
    Filed: November 16, 1979
    Date of Patent: December 31, 1985
    Assignee: Mitsubishi Chemical Industries, Ltd.
    Inventors: Ryoji Kikumoto, Akihiro Tobe, Shinji Tonomura, Hidenobu Ikoma
  • Patent number: 4560553
    Abstract: Eucalyptol is used to enhance skin permeation of bio-affecting agents.
    Type: Grant
    Filed: November 21, 1983
    Date of Patent: December 24, 1985
    Assignee: Merck & Co., Inc.
    Inventor: Jacob A. Zupan