Benzene Ring In Acid Moiety Patents (Class 514/555)
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Patent number: 5681838Abstract: 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: GrantFiled: July 18, 1995Date of Patent: October 28, 1997Assignee: Hoechst AktiengesellschaftInventors: Gerhard Zoller, Bernd Jablonka, Melitta Just, Otmar Klingler, Gerhard Breipohl, Jochen Knolle, Wolfgang Konig
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Patent number: 5658954Abstract: 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: GrantFiled: January 29, 1996Date of Patent: August 19, 1997Inventor: Eugene F. Targosz
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Patent number: 5637616Abstract: 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: GrantFiled: October 5, 1993Date of Patent: June 10, 1997Assignee: Arcturus Pharmaceutical CorporationInventors: Richard J. Sharpe, Maureen H. McAloon, Stephen J. Galli, Kenneth A. Arndt
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Patent number: 5626838Abstract: 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: GrantFiled: March 13, 1995Date of Patent: May 6, 1997Assignee: The Procter & Gamble CompanyInventor: Paul F. Cavanaugh, Jr.
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Patent number: 5614510Abstract: 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: GrantFiled: August 22, 1994Date of Patent: March 25, 1997Assignee: Perstorp ABInventor: Lars Persson
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Patent number: 5614554Abstract: 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: GrantFiled: June 6, 1995Date of Patent: March 25, 1997Assignee: Nippon Flour Mills Co., Ltd.Inventors: Keijiro Uchino, Takashi Mizuno, Sachie Murakami, Hideki Nakashima, Naoki Yamamoto, Hiroshi Ogawara
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Patent number: 5567686Abstract: 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: GrantFiled: September 13, 1993Date of Patent: October 22, 1996Assignee: Arch Development CorporationInventor: David J. Grdina
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Patent number: 5510385Abstract: 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: GrantFiled: June 7, 1994Date of Patent: April 23, 1996Assignee: Zambon Group S.p.A.Inventors: Federico Stroppolo, Daniele Bonadeo, Gian F. Fornasini, Annibale Gazzaniga
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Patent number: 5496857Abstract: 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: GrantFiled: March 17, 1994Date of Patent: March 5, 1996Inventor: Eugene F. Targosz
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Patent number: 5449668Abstract: 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: GrantFiled: June 4, 1993Date of Patent: September 12, 1995Assignee: 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
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Patent number: 5385931Abstract: 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: GrantFiled: December 28, 1990Date of Patent: January 31, 1995Assignee: Pierre Fabre MedicamentInventors: Dennis Bigg, Alain Duflos, Jean-Pierre Rieu
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Patent number: 5331011Abstract: 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: GrantFiled: April 7, 1993Date of Patent: July 19, 1994Assignee: Mitsubishi Gas Chemical Co., Inc.Inventors: Mitsunori Oda, Kazutoshi Kikkawa, Akinori Tanaka, Satoko Imaruoka, Shigeo Yoshinaka
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Patent number: 5132118Abstract: 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: GrantFiled: November 29, 1990Date of Patent: July 21, 1992Inventor: John A. Mills
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Patent number: 5114716Abstract: 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: GrantFiled: July 28, 1989Date of Patent: May 19, 1992Assignee: Societe Anonyme Dite: L'OrealInventors: Quang L. N'Guyen, Jacqueline Griat, Francois Millecamps, Gerard Lang, Serge Forestier
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Patent number: 5011854Abstract: 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: GrantFiled: December 7, 1989Date of Patent: April 30, 1991Assignee: 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
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Patent number: 5001156Abstract: 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: GrantFiled: December 1, 1987Date of Patent: March 19, 1991Assignee: L'OrealInventors: Michel Philippe, Henri Sebag, Michel Hocquaux, Bernard Jacquet, Jean P. Laugier
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Patent number: 4960772Abstract: 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: GrantFiled: February 23, 1989Date of Patent: October 2, 1990Assignee: L'OrealInventors: Henri Sebag, Irina Beck
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Patent number: 4959394Abstract: 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: GrantFiled: November 17, 1989Date of Patent: September 25, 1990Assignee: Ciba-Geigy CorporationInventors: Gerhard Baschang, Alfred Sallman
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Patent number: 4945112Abstract: 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: GrantFiled: March 16, 1989Date of Patent: July 31, 1990Assignee: BASF AktiengesellschaftInventors: Matthias Zipplies, Hubert Sauter, Eberhard Ammermann, Gisela Lorenz
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Patent number: 4897422Abstract: 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: GrantFiled: February 10, 1987Date of Patent: January 30, 1990Assignee: Abbott LaboratoriesInventor: James B. Summers, Jr.
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Patent number: 4895842Abstract: 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: GrantFiled: September 29, 1986Date of Patent: January 23, 1990Assignees: Shosuke Okamoto, Showa Denko Kabushiki KaishaInventors: Shosuke Okamoto, Yoshio Okada, Akiko Okunomiya, Taketoshi Naito, Yoshio Kimura, Morihiko Yamada, Norio Ohno, Yasuhiro Katsuura, Yumi Seki
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Patent number: 4891386Abstract: A new compound, namely lidocaine salicylate monohydrate of formula: ##STR1## has been proposed, which has shown strong local anesthetic and cardiac antiarrhythmic activity.Type: GrantFiled: September 17, 1984Date of Patent: January 2, 1990Assignee: Molteni & C. Dei F.lli Alitti S.p.A.Inventor: Franca A. Gasparotti
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Patent number: 4883786Abstract: 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: GrantFiled: December 8, 1988Date of Patent: November 28, 1989Assignee: Magis Farmaceutici SrlInventor: Laura Puricelli
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Patent number: 4880840Type: GrantFiled: June 30, 1987Date of Patent: November 14, 1989Assignee: Bayer AktiengesellschaftInventors: Hans Lindel, Axel Ingendoh, Friedrich Berschauer, Anno de Jong, Martin Scheer
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Patent number: 4876282Abstract: The present invention provides 1-phenyl-(naphthalenyl)alkylamines which are selective inhibitors of serotonin uptake.Type: GrantFiled: November 25, 1987Date of Patent: October 24, 1989Assignee: Eli Lilly and CompanyInventors: David W. Robertson, David T. Wong
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Patent number: 4818767Abstract: 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: GrantFiled: November 2, 1983Date of Patent: April 4, 1989Assignee: SmithKline Beckman CorporationInventor: Jean F. Rossignol
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Patent number: 4797423Abstract: 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: GrantFiled: September 22, 1987Date of Patent: January 10, 1989Assignee: S.I.F.I. Societa Industria Farmaceutica Italiana S.p.A.Inventor: Giuseppe Benanti
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Patent number: 4792551Abstract: 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: GrantFiled: July 15, 1983Date of Patent: December 20, 1988Assignee: Syntex (U.S.A.) Inc.Inventors: Peter H. Nelson, Stefan H. Unger, Thomas R. Thieme
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Patent number: 4767784Abstract: 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: GrantFiled: November 28, 1986Date of Patent: August 30, 1988Inventors: Gerhard Zolss, Gerhard Pfarrhofer
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Patent number: 4764534Abstract: 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: GrantFiled: July 17, 1984Date of Patent: August 16, 1988Assignee: Eli Lilly and CompanyInventors: Albert J. Clinton, deceased, George O. P. O'Doherty
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Patent number: 4751242Abstract: 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: GrantFiled: July 27, 1987Date of Patent: June 14, 1988Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Menotti Calvani, Luigi Mosconi
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Patent number: 4748174Abstract: 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: GrantFiled: January 5, 1987Date of Patent: May 31, 1988Assignee: Therapicon s.r.l.Inventor: Paolo A. Veronesi
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Patent number: 4717736Abstract: 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: GrantFiled: November 21, 1984Date of Patent: January 5, 1988Assignee: Merck Frosst Canada, Inc.Inventors: Joshua Rokach, Robert N. Young
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Patent number: 4704403Abstract: 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: GrantFiled: December 27, 1985Date of Patent: November 3, 1987Inventors: 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
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Patent number: 4689346Abstract: 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: GrantFiled: October 28, 1985Date of Patent: August 25, 1987Assignee: Laboratorio Fides, S.A.Inventors: Pere P. Llobet, Elisa G. Baylina
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Patent number: 4672077Abstract: 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: GrantFiled: June 3, 1986Date of Patent: June 9, 1987Assignee: Istituto Biochimico Pavese SpAInventor: Nelly Colombi
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Patent number: 4665094Abstract: 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: GrantFiled: August 29, 1985Date of Patent: May 12, 1987Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Gerald S. Ponticello
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Patent number: 4659739Abstract: 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: GrantFiled: February 25, 1985Date of Patent: April 21, 1987Assignee: Dainippon Ink and Chemicals, Inc.Inventors: Nobuyuki Yoshioka, Yasuji Okunishi, Yasuhisa Miura, Yoshikazu Mori, Yasuki Kataoka, Eiichi Adachi
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Patent number: 4654371Abstract: 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: GrantFiled: October 8, 1985Date of Patent: March 31, 1987Assignee: Beecham Group p.l.c.Inventors: Anthony T. Ainsworth, David G. Smith
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Patent number: 4623661Abstract: 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: GrantFiled: April 26, 1985Date of Patent: November 18, 1986Assignee: Abbott LaboratoriesInventor: James B. Summers, Jr.
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Patent number: 4609673Abstract: 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: GrantFiled: December 18, 1984Date of Patent: September 2, 1986Assignee: Boehringer Mannheim GmbHInventors: Hermann Eggerer, Bernd Hagenbruch, Tran G. Nguyen, Karlheinz Stegmeier, Johannes Pill
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Patent number: 4608390Abstract: 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: GrantFiled: April 26, 1985Date of Patent: August 26, 1986Assignee: Abbott LaboratoriesInventor: James B. Summers, Jr.
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Patent number: 4607053Abstract: 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: GrantFiled: April 4, 1985Date of Patent: August 19, 1986Assignee: E. R. Squibb & Sons, Inc.Inventors: Donald S. Karanewsky, Martin F. Haslanger
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Patent number: 4605669Abstract: 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: GrantFiled: April 26, 1985Date of Patent: August 12, 1986Assignee: Abbott LaboratoriesInventor: James B. Summers, Jr.
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Patent number: 4604407Abstract: 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: GrantFiled: April 4, 1985Date of Patent: August 5, 1986Assignee: E. R. Squibb & Sons, Inc.Inventors: Martin F. Haslanger, Donald S. Karanewsky
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Patent number: 4602023Abstract: 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: GrantFiled: June 3, 1985Date of Patent: July 22, 1986Assignee: Warner-Lambert CompanyInventors: John S. Kiely, Suchin Huang
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Patent number: 4587356Abstract: 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: GrantFiled: September 25, 1984Date of Patent: May 6, 1986Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Kinji Iizuka, Tetsuhide Kamijo, Ryoji Yamamoto, Hiromu Harada
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Patent number: 4568693Abstract: Herein disclosed are N-naphthoylglycine derivatives having aldose reductase inhibiting activity. The derivatives are useful for treating diabetic complications.Type: GrantFiled: September 9, 1983Date of Patent: February 4, 1986Assignee: Ayerst, McKenna & Harrison, Inc.Inventors: Kazimir Sestanj, Nedumparambil A. Abraham, Francesco Bellini, Adi Treasurywala
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Patent number: 4562211Abstract: 2-Substituted-1-(omega-aminoalkoxy)benzenes are prepared and found useful as pharmaceutical agents, particularly as antidepressants.Type: GrantFiled: November 16, 1979Date of Patent: December 31, 1985Assignee: Mitsubishi Chemical Industries, Ltd.Inventors: Ryoji Kikumoto, Akihiro Tobe, Shinji Tonomura, Hidenobu Ikoma
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Patent number: 4560553Abstract: Eucalyptol is used to enhance skin permeation of bio-affecting agents.Type: GrantFiled: November 21, 1983Date of Patent: December 24, 1985Assignee: Merck & Co., Inc.Inventor: Jacob A. Zupan