Nitrogen In R Patents (Class 514/626)
-
Patent number: 5411990Abstract: An industrial microbicide which comprises at least one haloglyoxime derivative of the formula (I): ##STR1## wherein X is a halogen atom; Y is a hydrogen atom, a halogen atom or a lower alkyl group having 1 to 4 carbon atoms; and Z is a hydrogen atom or an optionally halogenated lower alkanoyl group having 1 to 5 carbon atoms; and a known industrial microbicidal ingredient selected from the group consisting of an organonitrogen-sulfur compound, an organohalogen compound, an organonitrogen compound and an organosulfur compound; and optionally a carrier or diluent.Type: GrantFiled: May 17, 1993Date of Patent: May 2, 1995Assignees: Yoshitomi Pharmaceutical Industries Ltd., Katayama Chemical Inc.Inventors: Katsuji Tsuji, Hidenori Hirashima
-
Patent number: 5399590Abstract: The invention relates to the field of organic chemistry and more particularly to that of therapeutic chemistry.More particularly it relates to new quaternary ammonium salts of general formula (I): ##STR1## in which Hal is a halogen atom other than fluorine R and R.sub.1, identical or different, are lower alkyl radicals, n is an integer varying from 2 to 16, Z is an alkenyl radical having up to 3 carbon atoms, a carboxyl, or the OR.sub.2 group in which R.sub.2 is a hydrogen, a lower alkyl radical, an acyl remainder, a tocol radical, a sterol radical or a carboxamide chain and A is a hydroxyl or an anion of a mineral or organic acid.The compounds according to the invention are the active ingredients of pharmaceutical compositions with an anti-tumorous and/or immuno-suppressive action.Type: GrantFiled: January 14, 1993Date of Patent: March 21, 1995Inventor: Jean M. Gastaud
-
Patent number: 5368866Abstract: A deer repellent composition for the protection of vegetation includes an active ingredient comprising egg and a red hot sauce, composed of pepper, vinegar, garlic, salt and water; a carrier; and a diluent. The vegetation is protected by applying an effective amount of the composition thereto, preferably by spraying. The composition may include the aforementioned ingredients in the following percentages: about 3-7 percent eggs; about 6-19 percent red hot sauce; about 3-7 percent carrier; and about 68-91 percent diluent, the total composition equaling 100 percent by weight. A process for preparing the mixture is also enclosed.Type: GrantFiled: October 25, 1993Date of Patent: November 29, 1994Inventor: Athena P. Loucas
-
Patent number: 5334377Abstract: Alkylamino-mercaptoalkylamides have the formula ##STR1## where in A represents the divalent radical --(CH.sub.2).sub.n --, wherein n is a whole number ranging from 2 to 5, or the divalent radical --(CH.sub.2).sub.2 --O--(CH.sub.2).sub.2 --,m is 0, 1 or 2,R.sub.1 represents hydrogen or linear or branched lower alkyl having 1-5 carbon atoms,R.sub.2 and R.sub.3, each independently, represent hydrogen or a linear or branched lower alkyl having 1-4 carbon atoms with the proviso that R.sub.2 and R.sub.3 are not hydrogen simultaneously and the salts of the compound of formula I as well as the corresponding disulfides with the exclusion of the disulfide in which A.dbd.--(CH.sub.2).sub.2 --, m.dbd.0, R.sub.1 and R.sub.2 .dbd.H and R.sub.3 .dbd.--C.sub.2 H.sub.5. The compound of formula I is used as a reducing agent in a cosmetic composition for the permanent deformation of hair.Type: GrantFiled: May 15, 1992Date of Patent: August 2, 1994Assignee: L'OrealInventors: Alex Junino, Gerard Malle, Bernadette Luppi
-
Patent number: 5334607Abstract: Antimycotics containing a compound of the formula ##STR1## where .dbd.Y is .dbd.CH--OCH.sub.3, .dbd.CH--CH.sub.3, .dbd.CH--CH.sub.2 --CH.sub.3, .dbd.CH--SCH.sub.3 or .dbd.N--OCH.sub.3, and X is oxygen, or X may also be NH if Y is .dbd.N--OCH.sub.3,Z is halogen, nitro, cyano, unsubstituted or substituted organic radicals, OR.sup.12, SR.sup.13, SOR.sup.14, SO.sub.2 R.sup.15, --COOR.sup.16, --CONR.sup.17 R.sup.18, --COR.sup.19, --CR.sup.20 .dbd.NR.sup.21, --N.dbd.CR.sup.22 R.sup.23, --CR.sup.24 .dbd.N--OR.sup.25, --CR.sup.25 R.sup.26 --O--N.dbd.CR.sup.27 R.sup.28 andU, V, W can be hydrogen or one of the meanings given for Z, or where two of Z, U, V and W in adjacent positions on the phenyl ring can form an unsubstituted or substituted five- or six-membered, aromatic or aliphatic ring which may contain one to three hetero atoms (N, S, O), and R.sup.12 to R.sup.26 are identical or different and are hydrogen, unsubstituted or substituted organic radicals,are used for controlling mycoses.Type: GrantFiled: May 28, 1992Date of Patent: August 2, 1994Assignee: BASF AktiengesellschaftInventors: Hubert Sauter, Gisela Lorenz, Gerd Steiner, Bernd Janssen, Timm Anke, Wolfgang Steglich
-
Patent number: 5331007Abstract: There is provided a method of treatment of neurological disorders, such as epilepsy, stroke and cerebral ischaemia, which comprises the administration of a compound of Formula I: ##STR1## wherein, Ar.sub.1 and Ar.sub.2, which may be the same or different, independently represent phenyl or phenyl substituted by one or more of amino, nitro, halogen, hydroxy, C1 to 6 alkoxy, C1 to 6 alkyl or cyano;R.sub.1 represents hydrogen, C1 to 6 alkyl, C1 to 6 alkoxycarbonyl;R.sub.2 represents hydrogen or COCH.sub.2 NH.sub.2 ;R.sub.3 represents hydrogen or C1 to 6 alkyl;in addition, when R.sub.2 represents hydrogen either one or both of Ar.sub.1 and Ar.sub.2 may also represent 2-, 3- or 4-pyridinyl and R.sub.1 may also represent trihalomethyl;or a pharmaceutically acceptable salt thereof.Some of the compounds of formula I are novel, and these are also provided, together with pharmaceutical compositions containing the novel compounds.Type: GrantFiled: July 20, 1992Date of Patent: July 19, 1994Assignee: Fisons CorporationInventors: Ronald C. Griffith, James J. Napier
-
Patent number: 5331012Abstract: The present invention relates to a method and pharmaceutical composition for treating fever blisters or cold sores in mammals, and particularly in humans, by topically administering a pharmaceutical composition comprising ethyl alcohol in a concentration of at least 85% W/V and lidocaine in a concentration of 0.5-10% W/V at a periodicity of at least 10 to 12 times daily.Type: GrantFiled: March 5, 1992Date of Patent: July 19, 1994Inventors: Kenneth B. Riddick, Joe G. Matheson, Jr., Louis E. Mizelle, Jr.
-
Patent number: 5331013Abstract: A method for treatment of ulcerative colitis (and sequelae to surgically treated colitis, for instance ileal pouchiris) and ulcerative proctitis comprising administration to a patient suffering therefrom of a therapeutically effective amount of a local anaesthetic or a pharmaceutically acceptable salt thereof, preferably lidocaine hydrochloride in the form of a pharmaceutically acceptable preparation.Type: GrantFiled: April 1, 1992Date of Patent: July 19, 1994Assignee: Aktiebolaget AstraInventors: B. Hakan J. Ahlman, Stellan Bjorck, Annica B. Dahlstrom
-
Patent number: 5328909Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.Type: GrantFiled: June 25, 1992Date of Patent: July 12, 1994Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
-
Patent number: 5298528Abstract: An insect repellent composition for against mosquitoes or other insects that attack man and or warm-blooded animals contains up to 5% by weight of a local anaesthetic selected from the group comprising alkyl p-aminobenzoate (I), arylamide of 2-aminoacetic acid (II), 2-aminoalkyl aryl ether (III), 2-aminoalkyl p-aminobensoate (IV) and mixtures thereof. Particularly preferred is lidocaine and a mixture of lidocaine and prilocaine.Type: GrantFiled: October 6, 1992Date of Patent: March 29, 1994Assignee: Baker Cummins Dermatologicals, Inc.Inventor: Hans Evers
-
Patent number: 5290775Abstract: An euthanasia solution based upon gamma-hydroxybutramide, a cardiotoxic amount of a compound selected from a chloroquine and quinacrine compound and lidocaine as a base or as a water soluble salt is described. The composition provides effective euthanasia without unwanted side effects, particularly in dogs, cats and horses. In addition, it does not contain substances controlled by the Federal Drug Control Administration.Type: GrantFiled: June 3, 1991Date of Patent: March 1, 1994Assignee: Board of Trustees operating Michigan State UniversityInventors: Donald C. Sawyer, Marlee A. Langham, Theodore M. Brody
-
Patent number: 5278148Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or methyl, R.sup.2 is ethyl, propyl, isopropyl, imidazol-2-yl, imidazol-4-yl, pyrazol-3-yl, thiazol-4-yl, thien-2-yl, ethoxycarbonyl, t-butylcarbonylmethyl, benzyloxycarbonylmethyl or t-butoxy, R.sup.3 is isobutyl, cyclohexylmethyl or benzyl, R.sup.4 is nitro, amino or a group of the formula --N(R.sup.5)(R.sup.6) and A is one of the groups ##STR2## wherein R.sup.5 and R.sup.6 is alkyl or alkoxyalkyl; or optionally substituted phenyl, phenylalkyl or phenylsulfonylalkyl among others with the proviso that A is not group (b) when R.sup.6 is alkanoyl, alkoxycarbonyl or arylalkoxycarbonyl, the dotted line can be an additional bond, R.sup.7 is phenyl or substituted phenyl and R.sup.8 is hydrogen or organocarbonylalkyl, with the proviso that R.sup.8 is not alkoxycarbonylamino or arylalkoxycarbonylamino when R.sup.7 is phenyl, benzyl or .alpha.Type: GrantFiled: March 27, 1990Date of Patent: January 11, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Quirico Branca, Hans P. Marki, Werner Neidhart, Henri Ramuz, Wolfgang Wostl
-
Patent number: 5276032Abstract: A new visualizing and anesthetic composition and the process for the preparation thereof. The composition, generally as a gel, contains an effective amount of a topical anesthetic, an effective amount of a visualizing agent and a pharmaceutically acceptable gelling reservoir as a heat exchanger and/or a light transmitter. The composition is useful for topical application to a region of mammalian skin to supply visualization to a lesion therein and to anesthetize the region for a subsequent destructive therapy.Type: GrantFiled: November 7, 1991Date of Patent: January 4, 1994Inventors: O. Newton King, Henry W. Buck
-
Patent number: 5262436Abstract: Mercapto-acylamino acids useful in the treatment of hypertension and combinations of mercapto-acylamino acids and atrial natriuretic factors or angiotensin converting enzyme inhibitors useful for treating hypertension are disclosed.Type: GrantFiled: August 6, 1991Date of Patent: November 16, 1993Assignee: Schering CorporationInventors: Martin F. Haslanger, Bernard R. Neustadt, Elizabeth M. Smith
-
Patent number: 5254591Abstract: A pharmaceutical composition useful for treating gastroesophageal reflux comprising oxethazaine and a carrier selected from alginic acid and alginates.Type: GrantFiled: April 10, 1992Date of Patent: October 19, 1993Assignee: The University of MelbourneInventor: Christopher J. Martin
-
Patent number: 5208034Abstract: Disclosed are novel tetraamide compounds and intermediates therefor which are useful in methods for improving feed conversion and/or weight gain in animals such as chickens.Type: GrantFiled: August 25, 1992Date of Patent: May 4, 1993Assignee: Eastman Kodak CompanyInventors: David C. Herting, Alan W. White
-
Patent number: 5190974Abstract: Novel .alpha.-mercapto-alkylamines in all possible racemic, enantiomeric and diastereoisomeric forms of the formula ##STR1## wherein n, R.sub.1, R.sub.2, X, A, R.sub.3A and R.sub.4A are set forth in the claims and their non-toxic, pharmaceutically acceptable acid addition salts having excellent analgesic, psychotropic and enkephalinase inhibiting properties.Type: GrantFiled: July 5, 1991Date of Patent: March 2, 1993Assignee: Roussel UclafInventors: Francoise Clemence, Odile Le Martret, Francis Petit
-
Patent number: 5175192Abstract: The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylatin. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.Type: GrantFiled: April 3, 1990Date of Patent: December 29, 1992Assignee: The Rockefeller UniversityInventors: Peter C. Ulrich, Anthony Cerami
-
Patent number: 5171678Abstract: New lipopolyamines of general formula (I), their salts, their preparation and their use. ##STR1## n=1 to 5 and m=2 to 6; R represents a radical ##STR2## (R.sub.1 and R.sub.2 : aliphatic radical containing 12 to 22 carbon atoms; R: hydrogen atom or alkyl radical optionally substituted with phenyl), or a radical ##STR3## (X=CH.sub.2, CO; R.sub.3 and R.sub.4 aliphatic radical containing 11 to 21 carbon atoms), their preparation and their use.The lipopolyamines of general formula (I) are especially useful as vectors for the transfection of eukaryotic cells.Type: GrantFiled: April 17, 1990Date of Patent: December 15, 1992Assignee: Centre National de la Recherche ScientifiqueInventors: Jean-Paul Behr, Jean-Philippe Loeffler
-
Patent number: 5153226Abstract: The present invention are novel amino acid amide compounds of the following general formula which inhibit the enzyme acylcoenzyme A:cholesterol acyltransferase: ##STR1## wherein R is phenyl or 1- or 2-naphthyl which are unsubstituted or may be substituted; R.sub.1 is hydrogen or a straight or branched alkyl group having from 1 to 6 carbon atoms; R.sub.2 is hydrogen, an aliphatic group, an aromatic group, an aralkyl or diarylalkyl group or R.sub.1 and R.sub.2 form a carbocyclic group; R.sub.3 is hydrogen, an aliphatic group, an aralkyl group wherein the alkyl moiety may contain a carbocyclic entity; R.sub.4 is hydrogen, an aliphatic group, SO.sub.2 R.sub.14, --C(.dbd.S)NHR.sub.15, --CO.sub.2 R.sub.15, --COR.sub.18, or --C(.dbd.O)NHR.sub.15 wherein R.sub.14 is morpholino, phenyl or substituted phenyl; R.sub.15 is an alkyl group, phenyl or phenylalkyl wherein the phenyl group may be substituted; and R.sub.18 is the same is R.sub.15 or is halo-substituted alkyl, 9-fluoroenylmethylene or pyrrolidino.Type: GrantFiled: July 30, 1990Date of Patent: October 6, 1992Assignee: Warner-Lambert CompanyInventors: Alexander W. Chucholowski, Mark W. Creswell, William H. Roark, Ila Sircar
-
Patent number: 5112620Abstract: A therapeutic ointment having wet adherent properties and particularly well suited for delivery of medicaments to mucosal surfaces includes a base material comprising from about 3 to 15% by weight of a water soluble salt of a copolymer of methyl vinyl ether and maleic acid or anhydride in a polyethylene glycol ointment. Formulations of the base material with triamcinolone acetonide and lidocaine are particularly efficacious in the treatment of recurrent aphthous ulcers.Type: GrantFiled: September 20, 1990Date of Patent: May 12, 1992Assignee: Mikkur, Inc.Inventors: Michael A. Repka, Thomas G. Gerding
-
Patent number: 5110797Abstract: Peptide compounds of formula (I): ##STR1## wherein A is hydrogen or an amino-protecting group; X is a member selected from the group consisting of Gly, Glu, Tyr, Asp, Phe, Ile, Ala, Pro, Leu, Hyp, Val, His, Arg, Ser, Thr, Pyr, Trp, 5-HTP, Cys, Met, .tau.-Glu, .beta.-Asp; Y is a (CH.sub.2).sub.3-6 or (CH.sub.2).sub.3-6 having an hydroxy group; R is an hydroxy group or an oxygen atom with a carboxy-protecting group; are useful as neurotropic agents.Type: GrantFiled: April 29, 1988Date of Patent: May 5, 1992Assignee: Nippon Zoki Pharmaceutical Co., Ltd.Inventors: Kazuharu Ienaga, Kunihiko Higashiura
-
Patent number: 5084452Abstract: Use of 2-azabicyclo[2.2.2]octane-3-carboxylic acid derivatives and their salts for the production of medicinal products intended for the treatment of arteritis and more especially arteritis of the lower limbs, disorders of the cerebral circulation and more especially disorders of cerebral senescence and migraine, and disorders of vision such as retinal disorders of vascular origin, diabetic retinopathy, chorioretinal atrophy and chorioretinal degeneration.Type: GrantFiled: April 24, 1990Date of Patent: January 28, 1992Assignee: Adir et CompagnieInventor: Bernard Teisseire
-
Patent number: 5075337Abstract: Deuterated 2-alkylaminoacetamide compounds are described having the alpha carbon of the alkyl side chain of the compounds substituted by one or two deuterium atoms. These compounds have pharmacokinetic properties which enable treatment of CNS diseases with lower toxic effects. These compounds are also useful in evaluating the metabolic fate of non-deuterated counterpart compounds. Of particular interest are compounds of Formula I: ##STR1## wherein X is deutero or hydrido; wherein R.sup.1 is selected from alkyl and aralkenyl; wherein each of R.sup.2 and R.sup.3 is independently selected from hydrido and alkyl; wherein each of R.sup.1, R.sup.2 and R.sup.3 having a substitutable position may be substituted with one or more halo radicals; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: July 26, 1989Date of Patent: December 24, 1991Assignee: G. D. Searle & Co.Inventors: Alex A. Cordi, Philippe Janssens de Varebeke, Hugo Gorissen
-
Patent number: 5070105Abstract: Stabilized antimicrobial compositions containing an antimicrobial amount of 2,2-dibromo-3-nitrilopropionamide in water miscible organic solvents. The stabilizer used is selected from chain-breaking antioxidants of the phenolic or amine type in an amount in the range of 0.001% to 0.5% by weight of the composition. Typical examples of stabilizers are: 2,6-di-tert-butyl-p-cresol; 4,4'-bis-(2,6-di-tert-butylphenol); 2,6-di-tert-butyl-.alpha.-methoxy-p-cresol and N-phenyl-.beta.-naphthylamine. The antimicrobial compositions also contain one or more water miscible organic solvents selected from those known in the art, in which the 2,2-dibromo-3-nitrilopropionamide is at least partially soluble. The compositions according to the present invention are characterized by their outstanding stability, compared with formulations which do not contain these stabilizers.Type: GrantFiled: May 3, 1989Date of Patent: December 3, 1991Inventors: Jeanne Segall, Leonard M. Shorr
-
Patent number: 5059589Abstract: A method and a composition for treating or reducing and/or controlling intraocular pressure comprising administering an effective amount of a renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; W is CO or CHOH and U is CH.sub.2 or NR.sub.2 wherein R.sub.2 is hydrogen or loweralkyl; with the proviso that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloalkylmethyl, benzyl, (alpha, alpha)-dimethylbenzyl, 4-hydroxybenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, 1-bezyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R.sub.3 is loweralkyl, loweralkenyl, ((alkoxy)alkoxy)loweralkyl, (thioalkoxy)alkyl, benzyl or heterocyclic ring substituted methyl; and R.sub.4 is substituted hydroxyalkylamino.Type: GrantFiled: March 2, 1990Date of Patent: October 22, 1991Assignee: Abbott LaboratoriesInventors: Herman H. Stein, Jacob J. Plattner, Steven R. Crowley
-
Patent number: 5045306Abstract: N-alkylamide of DL and L(-)-carnitine having general formula (I) ##STR1## wherein: x.sup.- is OH.sup.- or the anion of a pharmacologically acceptable acid (preferably Cl.sup.-`), andR is a straight C.sub.10 -C.sub.16 alkyl radicalare prepared via transamination by reacting DL or L(-)-carnitinamide halogenide with an amine of formula NH.sub.2 R wherein R has the above-identified meaning in an acid environment (e.g. H.sub.3 PO.sub.4) in the presence of a high-boiling solvent (e.g. ethylene glycol).N-alkylamides (I) are endowed with potent antibacterial activity and are suitable for preparing pharmaceutical and cosmetic compositions.Type: GrantFiled: November 4, 1988Date of Patent: September 3, 1991Assignee: Avantgarde S.p.A.Inventors: Paolo Cavazza, Giulio Fiorentini
-
Patent number: 5036057Abstract: A pharmaceutical composition comprising a local anaesthetic adapted to inhibit relaxation of the lower oesophageal sphincter and a carrier therefor comprising a material adapted to float on gastrointestinal fluids contained in the stomach whereby to be more proximate to the gastric mucosa below said sphincter, than said fluids.Type: GrantFiled: June 21, 1989Date of Patent: July 30, 1991Assignee: The University of MelbourneInventor: Christopher J. Martin
-
Patent number: 5008289Abstract: Compositions and methods for treating the symptoms of certain allergy-related conditions using capsaicin in solution or suspension combined with a selected local anesthetic, topical steroid or antihistamine. The same methods and compositions may be used to treat headaches.Type: GrantFiled: December 2, 1988Date of Patent: April 16, 1991Assignee: GalenPharma, Inc.Inventor: Joel E. Bernstein
-
Patent number: 4997853Abstract: A method and composition for treating superficial pain syndromes incorporates capsaicin in a therapeutically effective amount into a pharmaceutically acceptable carrier and adding to this composition a local anesthetic such as lidocaine or benzocaine. The composition containing the anesthetic is then applied to the site of the pain. A variation on the treatment includes initial treatment with the composition containing the local anesthetic until the patient has become desenstitized to the presence of capsaicin and subsequent treatment with a composition ommitting the local anesthetic.Type: GrantFiled: March 28, 1990Date of Patent: March 5, 1991Assignee: Galenpharma, Inc.Inventor: Joel E. Bernstein
-
Patent number: 4990536Abstract: The present invention provides a use for the preparation of an immunopotentiator of a spergualin-related compound represented by the following general formula [I] or a pharmacologically acceptable salt thereof: ##STR1## wherein X represents ##STR2## or --(CH.sub.2).sub.n --, Y represents a hydrogen atom or a hydroxyl or hydroxymethyl group,n is an integer of 3 or 5, andR represents --(CH.sub.2).sub.4 --R.sub.1 (wherein R.sub.1 is --NH.sub.2 or --OH), --(CH.sub.2).sub.3 --R.sub.2 (wherein R.sub.2 is --COOH or --CHO), --(CH.sub.2).sub.4 --NH--(CH.sub.2).sub.3 --OH or --(CH.sub.2).sub.4 --NH--(CH.sub.2).sub.2 --R.sub.2 (wherein R.sub.2 is as defined above).Type: GrantFiled: March 16, 1990Date of Patent: February 5, 1991Assignees: Nippon Kayaku Kabushiki Kaisha, Takara Shuzo Co., Ltd.Inventors: Takeji Sakasai, Tsugio Tomiyoshi, Keiko Watanabe, Kyuichi Nemoto, Tetushi Saino, Yoshihisa Umeda
-
Patent number: 4980366Abstract: Novel 4'-hydroxybenzylamine derivatives of the formula ##STR1## pharmaceutical compositions and methods of use thereof are the present invention. Utility is for the treatment of arthritis, asthma, Raynaud's disease, inflammatory bowel disorders, trigeminal or herpetic neuralgia, inflammatory eye disorders, psoriasis, dental pain, and headaches, particularly vascular headache, succh as migraine, cluster, mixed vascular syndromes, as well as nonvascular, tension headaches.Type: GrantFiled: March 16, 1989Date of Patent: December 25, 1990Assignee: Warner-Lambert Co.Inventors: Graham Johnson, Michael F. Rafferty
-
Patent number: 4943307Abstract: The invention relates to a plant-protective solution containing 2.5 to 40 % by weight of one or more water-insoluble plant-protective ingredient(s) 20 to 71.5 % by weight of dimethylformamide and/or dimethylsulfoxide and/or acetone as water-miscible solvent, 10 to 71.5 % by weight of furfurol and/or furfuryl alcohol as partially water-miscible solvent, 1 to 15 % by weight of commonly used additives such as anionic and/or nonionic surface active agents and macromolecules.The invention also relates to the ready-for-use plant-protective suspension containing 0.2 to 10 % by weight of one or more water-insoluble plant-protective ingredient(s) with a particle size of 0.1 to 50 .mu.m, 0 to 60 % by weight of a fertilizer, 0.2 to 10 % by weight of dimethylformamide and/or dimethylsulfoxide and/or acetone as water-miscible solvent, 0.2 to 10 % by weight of furfurol and/or furfuryl alcohol as partially water-miscible solvent, 0.05 to 2.Type: GrantFiled: July 15, 1988Date of Patent: July 24, 1990Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.Inventors: Tamas Detre, Sandor ngyan, Laszlo Pap, Andras Szego, Zoltan Karadi, Klara Bertus nee Bende, Katalin Marmarosi nee Kellner
-
Patent number: 4914131Abstract: The present invention relates to a method and pharmaceutical composition for treating herpes group virus infections in mammals, and in particular, in humans, by administering an effective antiviral amount of lidocaine or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 14, 1989Date of Patent: April 3, 1990Assignee: Dana P. BrighamInventors: Harold G. Haines, Caroline B. Dickens
-
Patent number: 4906659Abstract: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.4 are independently amino or an organic residue bonded through nitrogen, R.sup.2 is hydrogen or alkyl which may be substituted, R.sup.3 is hydrogen or a protecting group and R5 is hydroxyl which may be substituted or amino which may be substituted or salts thereof; with the proviso that when R.sup.1 is amino, leucylamino, acetylamino or benzyloxycarbonylamino, R.sup.3 is hydrogen, methyl or 2-tettrahydropyranyl, R.sup.4 is amino, acetylamino or benzyloxycarbonylamino and R.sup.5 is hydroxyl which may be substituted or amino which may be substituted, R.sup.2 is alkyl which may be substituted, has antibacterial activities against drug-resistant bacteria and therefore can be useful as a chemotherapeutic drug for bacterial infections in mammals.Type: GrantFiled: December 7, 1987Date of Patent: March 6, 1990Assignee: Takeda Chemical Industries, Ltd.Inventors: Setsuo Harada, Hideo Ono, Hirotomo Masuya, Hideaki Natsugari
-
Patent number: 4897382Abstract: Organic amide compounds of the formula ##STR1## wherein R.sub.1 --CO is a residue of a carboxylic acid with the proviso that the carboxylic acid is not a natural fatty acid normally bound to nitrogen of nitrogenous lipids, R.sub.2 is a hydrogen atom, a C.sub.1-7 alkyl group, or a C.sub.4-7 cycloalkyl group, and R.sub.3-N is a residue of a nitrogenous lipid. The compounds are useful in increasing or stimulating the in vivo biological activity of in vitro biologically active carboxylic acids.Type: GrantFiled: June 21, 1988Date of Patent: January 30, 1990Assignee: Fidia S.p.A.Inventors: Francesco della Valle, Aurelio Romeo
-
Patent number: 4879274Abstract: Novel external medications comprise, as essential components, the following three components (A) to (C):(A) an .alpha.-monoglyceryl ether represented by the following formula (I): ##STR1## wherein R means an alkyl or alkenyl group having 10 - 24 carbon atoms; (B) a physiologically active material; and(C) an oily material.The external medications have extremely high skin occlusive properties and significantly-improved absorptivity of phosiologically active materials. Therefore, a smaller amount of the medications compared with the conventional ones can give sufficient pharmacological effects and thus side effects can be reduced. The external medications may contain physiologically active materials such as drugs, growth hormones and the like, which are expected to show pharmacological effects upon their percutaneous absorption.Type: GrantFiled: September 12, 1986Date of Patent: November 7, 1989Assignee: Kao CorporationInventors: Tetsuro Kamiya, Shuichi Tsuchiya, Kenji Hara
-
Patent number: 4873241Abstract: 2-Amino-N-(2-phenylindan-2-yl)acetamides of the following formula are provided ##STR1## wherein, a=0 to 3,R.sub.1, R.sub.2 and R.sub.3 are independently selected from hydrogen and methyl,R.sub.4 is hydrogen or C.sub.1 -C.sub.4 alkyl,R.sub.5 is selected from hydrogen, C.sub.1 -C.sub.4 alkyl, cyclopropyl and (aminomethyl)carbonyl, orR.sub.4 and R.sub.5 taken together with the nitrogen atom to which they are attached from a heterocyclic ring selected from pyrrolidinyl, piperidinyl and morpholinyl, orR.sub.3 and R.sub.4 taken together with the carbon atom and nitrogen atom to which they are respectively attached form a heterocyclic ring selected from pyrrolidinyl and piperidinyl, andR.sub.6 is selected from hydrogen, halogen, C.sub.1 -C.sub.4 alkoxy, trifluoromethyl, C.sub.1 -C.sub.4 alkyl and combinations thereof.The compounds have antiepileptic or antihypoxia activity.Type: GrantFiled: October 31, 1988Date of Patent: October 10, 1989Assignee: Fisons CorporationInventors: James J. Napier, Ronald C. Griffith
-
Patent number: 4871773Abstract: N-alkylamide of D(+)-carnitine having general formula (I) ##STR1## wherein: X.sup.- is OH.sup.- or the anion of a pharmacologically acceptable acid (preferably Cl.sup.-), andR is a straight C.sub.10 -C.sub.16 alkyl radicalare prepared via transamination by reacting D(+)-carnitinamide halogenide with an amine of formula NH.sub.2 R wherein R has the above-identified meaning in an acid environment (e.g. H.sub.3 PO.sub.4) in the presence of a high-boiling solvent (e.g. ethylene glycol).N-alkylamides (I) are endowed with potent antibacterial activity and are suitable for preparing pharmaceutical and cosmetic compositions.Type: GrantFiled: January 11, 1989Date of Patent: October 3, 1989Assignee: Avantgarde S.p.A.Inventors: Paolo Cavazza, Giulio Fiorentini
-
Patent number: 4863926Abstract: New nitro aliphatic compounds useful as antithrombotic and antihypertensing agents are disclosed.Type: GrantFiled: November 10, 1987Date of Patent: September 5, 1989Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masanori Okamoto, Morita Iwami, Shigehiro Takase, Itsuo Uchida, Kazuyoshi Umehara, Masanobu Konsaka, Hiroshi Imanaka
-
Patent number: 4851446Abstract: The present invention relates to an immunosuppressing method which comprises administering a spergualin-related compound represented by the following formula ##STR1## (wherein R.sub.1 is --(CH.sub.2).sub.4 --, --(CH.sub.2).sub.6 --, ##STR2## R.sub.2 is --(CH.sub.2).sub.2 -- or --CH.dbd.CH--; and R.sub.3 is ##STR3## or pharmacologically acceptable salts thereof in an effective amount to a warm-blood animal.Type: GrantFiled: March 6, 1987Date of Patent: July 25, 1989Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Hamao Umezawa, deceased, Tomio Takeuchi, Masaaki Ishizuka, Fuminori Abe, Akio Fujii, Teruya Nakamura
-
Patent number: 4826841Abstract: The present invention is in alkanoyl anilides exhibiting insecticidal and arachnicidal activity, wherein the alkanoyl is both branched and substantially or totally fluorinated.Type: GrantFiled: March 5, 1986Date of Patent: May 2, 1989Assignee: Eli Lilly and CompanyInventor: Robert P. Gajewski
-
Patent number: 4808572Abstract: Novel asymmetric thioethers of the formula ##STR1## in which the general symbols have the following meanings: a is an integer of from 1 to 7,R.sup.o represents hydrogen or C.sub.1-7 -alkanoyl,R.sup.1 represents C.sub.1-3 -alkyl which may be substituted at the terminal carbon atom by a free or acylated hydroxy group, by a halogen atom having an atomic number of at most 17, or by methoxy, or represents C.sub.1-3 -perfluoroalkyl,R.sup.2 represents an optionally unsaturated aliphatic radical having from 5 to 15 carbon atoms,A represents ethylene or alternatively, if R.sup.1 represents a halogenated radical and/or B represents phenylene or ethylene, a single bond or vinylene,B represents a single bond, ethynylene or phenylene,R.sup.3 represents hydroxy, C.sub.Type: GrantFiled: December 1, 1986Date of Patent: February 28, 1989Assignee: Ciba-Geigy CorporationInventors: Andreas Beck, Werner Breitenstein, Andreas von Sprecher, Robert W. Lang, Konrad Oertle
-
Patent number: 4778804Abstract: New nitro aliphatic compounds and their pharmaceutically acceptable salts are disclosed.Type: GrantFiled: October 11, 1985Date of Patent: October 18, 1988Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masanori Okamoto, Morita Iwami, Shigehiro Takase, Itsuo Uchida, Kazuyoshi Umehara, Masanobu Kohsaka, Hiroshi Imanaka
-
Patent number: 4778824Abstract: This invention relates to method for suppressing a transplantation immunity and treating an allergic disease and an autoimmune disease in a mammal which comprises administering spergualin or a pharmaceutically acceptable salt thereof in effective amount to the said mammal.Type: GrantFiled: June 30, 1987Date of Patent: October 18, 1988Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Hamao Umezawa, Tomio Takeuchi, Masaaki Ishizuka, Fuminori Abe, Akio Fujii, Teruya Nakamura
-
Patent number: 4767768Abstract: New Nitro aliphatic compounds and their pharmaceutically acceptable salts are disclosed.Type: GrantFiled: December 8, 1983Date of Patent: August 30, 1988Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masanori Okamoto, Morita Iwami, Shigehiro Takase, Itsuo Uchida, Kazuyoshi Umehara, Masanobu Kohsaka, Hiroshi Imanaka
-
Patent number: 4757088Abstract: The present invention relates to a method and pharmaceutical composition for treating herpes group virus infections in mammals, and in particular, in humans, by administering an effective antiviral amount of lidocaine or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 22, 1986Date of Patent: July 12, 1988Assignee: Dana P. BrighamInventors: Harold G. Haines, Caroline B. Dickens
-
Patent number: 4725440Abstract: An antifungal pastille formulation, preferably containing nystatin as the antifungal agent, is provided which is soft and smooth in texture and when dissolved slowly in the mouth does not cause irritation of and will not adhere to oral mucosa and yet distributes nystatin in sufficiently high saliva concentrations, throughout the oral cavity, for long enough periods of time so as to be particularly effective in the treatment of candidiasis in the oral cavity and esophagus. A method for treating candidiasis in the oral cavity and esophagus employing the antifungal pastille and a method for preparing a nystatin pastille formulation are also provided.Type: GrantFiled: May 24, 1984Date of Patent: February 16, 1988Assignee: E. R. Squibb & Sons, Inc.Inventors: Frank Ridgway, Michael D. Ward
-
Patent number: 4690950Abstract: The present invention relates to new derivatives selected from the group consisting of:(i) 1-[N-(.alpha.-alkylamino-.alpha.-methylacetyl)aminophenyl]-2-alkylaminopro panones of the general formula: ##STR1## in which R represents a C.sub.1 -C.sub.4 alkyl group and R' represents H or a C.sub.1 -C.sub.4 alkyl group; and(ii) addition salts thereof.These new derivatives are useful as CNS-active substances, in particular as stimulants and antidepressants.The invention also relates to the method for their preparation.Type: GrantFiled: August 16, 1985Date of Patent: September 1, 1987Assignee: Laboratoire L. LafonInventor: Louis Lafon
-
Patent number: 4689344Abstract: A novel class of compounds has been found to be effective in blocking cholesterol and neutral lipid synthesis in-vivo without adversely affecting energy metabolism, useful for the treatment of obesity, hyperlipidemia and maturity-onset diabetes. The active compounds have the general formula ##STR1## or in-vivo hydrolyzable functional derivatives of the carboxylic groups thereof,whereinR.sub.1 and R.sub.2 each independently represents an unsubstituted or substituted hydrocarbyl or hetercyclyl radical;X and Y each independently represents hydrogen, optionally substituted lower alkyl, halogen, cyano, carboxy, lower alkoxycarbonyl or carbamoyl; andQ represents a diradical consisting of a linear chain of 8 to 14 carbon atoms, one or more of which may be replaced by heteroatoms, said chain being optionally substituted by inert substituents and one or more of said carbon or heteratom chain members optionally forming part of a ring structure.Type: GrantFiled: June 22, 1984Date of Patent: August 25, 1987Assignee: Epis S.A.Inventor: Jacob Bar-Tana