The Ring Nitrogen Of The Six-membered Hetero Ring Is Pentavalent (e.g., Quaternary Pyridinium Salt, Etc.) Patents (Class 514/358)
  • Patent number: 5476864
    Abstract: A glycerin derivative having the following formula (I) or (I') and a pharmacologically acceptable salt thereof are useful to treat diseases caused by the platelet activating factor.
    Type: Grant
    Filed: November 10, 1993
    Date of Patent: December 19, 1995
    Assignee: Eisai Co., Ltd.
    Inventors: Kazuo Okano, Osamu Asano, Naoyuki Shimomura, Tetsuya Kawahara, Shinya Abe, Shuhei Miyazawa, Mitsuaki Miyamoto, Hiroyuki Yoshimura, Koukichi Harada, Junsaku Nagaoka, Tsutomu Kawata, Tsutomu Yoshimura, Hiromasa Suzuki, Shigeru Souda, Yoshimasa Machida, Kouichi Katayama, Isao Yamatsu
  • Patent number: 5476863
    Abstract: A glycerin derivative having the following formula (I) or (I') and a pharmacologically acceptable salt thereof are useful to treat diseases caused by the platelet activating factor.
    Type: Grant
    Filed: September 30, 1993
    Date of Patent: December 19, 1995
    Assignee: Eisai Co., Ltd.
    Inventors: Kazuo Okano, Osamu Asano, Naoyuki Shimomura, Tetsuya Kawahara, Shinya Abe, Shuhei Miyazawa, Mitsuaki Miyamoto, Hiroyuki Yoshimura, Koukichi Harada, Junsaku Nagaoka, Tsutomu Kawata, Tsutomu Yoshimura, Hiromasa Suzuki, Shigeru Souda, Yoshimasa Machida, Kouichi Katayama, Isao Yamatsu
  • Patent number: 5472687
    Abstract: Topical pyridine N-oxides, including 3-carboxypyridine N-oxide, niacinamide N-oxide, and .alpha.-(4-pyridyl-1-oxide)-N-t-butylnitrone, are disclosed. The topical compositions have utility in a topical pharmaceutical formulation for the cosmetic treatment of hair loss and the cosmetic stimulation of hair growth.
    Type: Grant
    Filed: February 7, 1994
    Date of Patent: December 5, 1995
    Inventor: Peter H. Proctor
  • Patent number: 5464840
    Abstract: Disclosed are compounds of Formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, methods for inhibiting tumor necrosis factor-.alpha. and methods for treating septic shock, inflammation, or allergic disease.
    Type: Grant
    Filed: December 6, 1993
    Date of Patent: November 7, 1995
    Assignee: Schering Corporation
    Inventors: Pauline C. Ting, Daniel M. Solomon, Wing C. Tom
  • Patent number: 5424323
    Abstract: A biocidal, aqueous composition for killing bacteria, spores, fungi, and viruses on nonabsorbent surfaces comprises at least one quaternary ammonium compound, at least one aliphatic dialdehyde having from two to six carbon atoms, and at least one aliphatic hydroxyl compound having form one to eight carbon atoms.This sterilant is stable for weeks, is especially useful between pH 4 to 9, and may additionally comprise a chelating agent.
    Type: Grant
    Filed: March 23, 1994
    Date of Patent: June 13, 1995
    Assignee: Cetylite Industries, Inc.
    Inventors: Stanley L. Wachman, Sidney Karlan
  • Patent number: 5422353
    Abstract: The invention relates to new tetrahydropyridine derivatives, processes for preparing them and their use as pharmaceutical compositions with cholinomimetic properties.
    Type: Grant
    Filed: October 29, 1993
    Date of Patent: June 6, 1995
    Assignee: Boehringer Ingelheim KG
    Inventors: Gerhard Walther, Karl-Heinz Weber, Werner Stransky, Franz J. Kuhn, Erich Lehr, Enzio Muller, Gunter Schingnitz, Helmut Ensinger
  • Patent number: 5407949
    Abstract: A biocidal, aqueous composition for killing bacteria, spores, fungi, and viruses on nonabsorbent surfaces comprises at least one quaternary ammonium compound, at least one aliphatic dialdehyde having from two to six carbon atoms, and at least one aliphatic hydroxyl compound having form one to eight carbon atoms.This sterilant is stable for weeks, is especially useful between pH 4 to 9, and may additionally comprise a chelating agent.
    Type: Grant
    Filed: March 23, 1994
    Date of Patent: April 18, 1995
    Assignee: Cetylite Industries, Inc.
    Inventors: Stanley L. Wachman, Sidney Karlan
  • Patent number: 5399589
    Abstract: Oxalyl hydrazide-hydroxamic acid derivatives of the formula I ##STR1## where the substituents have the following meanings: R, R.sup.1, R.sup.2 and R.sup.3 independently of one another arehydrogen, substituted or unsubstituted alkyl, alkenyl or alkynyl orsubstituted or unsubstituted cycloalkyl or cycloalkylmethyl,substituted or unsubstituted cycloalkenyl or cycloalkenylmethyl,substituted or unsubstituted phenyl, phenylalkyl, phenylalkenyl, hetaryl- or hetarylalkyl radicals, where R.sup.2 and R.sup.3 may also. together with the nitrogen atom whose substituents they are, form a 5- or 6-membered ring, orR.sup.2 together with R.sup.3 is the group ##STR2## where R.sup.4 and R.sup.5 are one of the radicals R, R.sup.1, R.sup.2 or R.sup.3, or R.sup.4 together with R.sup.5 and the carbon atom whose substituents they are, are monocyclic or polycyclic cycloalkyl, orR.sup.4 together with R.sup.5 and the carbon atom whose substituents they are, form a 5- or 6-membered, saturated heterocycle containing O, S or --N(R.sup.
    Type: Grant
    Filed: November 29, 1993
    Date of Patent: March 21, 1995
    Assignee: BASF Aktiengesellschaft
    Inventors: Costin Rentzea, Albrecht Harreus, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 5395842
    Abstract: Inhibitors of sex steroid activity, for example those having the general structure ##STR1## may be used as part of a pharmaceutical composition to provide antiestrogenic effects and/or to suppress estrogen synthesis. Such pharmaceutical compositions are useful for the treatment of breast cancer or other diseases whose progress is aided by activation of sex steroid receptors.
    Type: Grant
    Filed: December 2, 1991
    Date of Patent: March 7, 1995
    Assignee: Endorecherche Inc.
    Inventors: Fernand Labrie, Yves Merand
  • Patent number: 5366983
    Abstract: A composition and method for removing and preventing Salmonella contamination of meat products, in particular poultry. The composition comprises an effective amount of a quaternary ammonium compound in an aqueous solution. The quaternary ammonium compound are selected from the group consisting of alkylpyridinium, tetra-alkylammonium, and alkylalicyclic ammonium salts. Preferably, the quaternary ammonium compounds are cetylpyridinium chloride (CPC) and cetylpyridinium bromide (CPB). The method comprises treating meat and poultry products with an effective amount of the quaternary ammonium compound in an aqueous solution. Mutagenicity studies are also disclosed.
    Type: Grant
    Filed: April 3, 1992
    Date of Patent: November 22, 1994
    Assignee: The Board of Trustees of The University of Arkansas
    Inventors: Danny L. Lattin, Philip J. Breen, Cesar M. Compadre, E. Kim Fifer, Michael F. Slavik, Hamid Salari, Phillip V. Engler
  • Patent number: 5344838
    Abstract: A biocidal, aqueous composition for killing bacteria, spores, fungi, and viruses on nonabsorbent surfaces comprises at least one quaternary ammonium compound, at least one aliphatic dialdehyde having from two to six carbon atoms, and at least one aliphatic hydroxyl compound having form one to eight carbon atoms.This sterilant is stable for weeks, is especially useful between pH 4 to 9, and may additionally comprise a chelating agent.
    Type: Grant
    Filed: December 8, 1993
    Date of Patent: September 6, 1994
    Assignee: Cetylite Industries, Inc.
    Inventors: Stanley L. Wachman, Sidney Karlan
  • Patent number: 5338748
    Abstract: A biocidal, aqueous composition for killing bacteria, spores, fungi, and viruses on nonabsorbent surfaces comprises at least one quaternary ammonium compound, at least one aliphatic dialdehyde having from two to six carbon atoms, and at least one aliphatic hydroxyl compound having form one to eight carbon atoms.This sterilant is stable for weeks, is especially useful between pH 4 to 9, and may additionally comprise a chelating agent.
    Type: Grant
    Filed: December 9, 1993
    Date of Patent: August 16, 1994
    Assignee: Cetylite Industries, Inc.
    Inventors: Stanley L. Wachman, Sidney Karlan
  • Patent number: 5328921
    Abstract: The invention is aryl, amide, imide and carbamate pyridine antagonists of platelet activating factor.
    Type: Grant
    Filed: October 30, 1992
    Date of Patent: July 12, 1994
    Assignee: American Cyanamid Company
    Inventors: Michael P. Trova, Allan Wissner
  • Patent number: 5244913
    Abstract: Compositions and methods for dissolving calculi deposits in humans are disclosed. The compositions include solutions of quaternary ammonium salts and are particularly effective for the contact dissolution of pigment portions of biliary tract calculi such as gallstones. The solutions preferably further include mineral chelating agent and disulfide bond cleaving agent to aid in deaggregating mineral components and glycoprotein components of calculi.
    Type: Grant
    Filed: November 19, 1991
    Date of Patent: September 14, 1993
    Assignee: Baxter International Inc.
    Inventors: Stephen L. Coulter, Kenneth G. Mayhan, Christy L. H. Oviatt, Steven R. Morehead
  • Patent number: 5208247
    Abstract: The invention is aryl, amide, imide and carbamate pyridine antagonists of platelet activating factor.
    Type: Grant
    Filed: August 1, 1991
    Date of Patent: May 4, 1993
    Assignee: American Cyanamid Company
    Inventors: Michael P. Trova, Allan Wissner
  • Patent number: 5183823
    Abstract: There is disclosed a novel thiazolidinedione derivative of the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are a hydrogen atom or a lower alkyl group, or a salt thereof. The thiazolidinedione derivative has hypoglycemic activity and hypolipidemic activity.
    Type: Grant
    Filed: March 31, 1992
    Date of Patent: February 2, 1993
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takashi Sohda, Hitoshi Ikeda
  • Patent number: 5175167
    Abstract: Hetarylalkenes of the general formula I ##STR1## where Ar is hetaryl,A is C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.3 -C.sub.8 -cycloalkyl-C.sub.1 -C.sub.3 -alkyl or unsubstituted or monosubstituted, disubstituted or trisubstituted aryl or aralkyl, ##STR2## Z is whereR is hydrogen, C.sub.2 -C.sub.4 -acyl, unsubstituted or substituted benzoyl, C.sub.1 -C.sub.4 -alkylsulfonyl, unsubstituted or C.sub.1 -C.sub.4 -alkyl-substituted phenylsulfonyl or a radical R.sup.1,R.sup.1 is C.sub.1 -C.sub.4 -alkyl or unsubstituted or substituted phenyl or benzyland Hal is fluorine, chlorine, bromine or iodine,and B is unsubstituted or substituted mononuclear or dinuclear aryl, aralkyl or hetaryl,and their N-oxides and addition salts, the preparation of these substances, intermediates for this purpose and the preparation thereof, fungicides containing hetarylalkenes and a corresponding method for controlling harmful fungi.
    Type: Grant
    Filed: February 8, 1991
    Date of Patent: December 29, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernhard Zipperer, Manfred Lauer, Norbert Goetz, Thomas Zierke, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 5137923
    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: June 21, 1990
    Date of Patent: August 11, 1992
    Assignee: L'Oreal
    Inventors: Michel Philippe, Henri Sebag, Michel Hocquaux, Bernard Jacquet, Jean P. Laugier
  • Patent number: 5116861
    Abstract: Novel nitrosothiol derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.3 is a hydrogen atom, an acyl group or a hydrocarbon residue which may be substituted; X.sup.1 is a hydrogen atom, an acyl group, a lower alkoxy group or a hydrocarbon residue which may be substituted; X.sup.2 is an acyl group or a carboxyl group which may be esterified or which may form an amide; with proviso that when X.sup.2 is a carboxyl group X.sup.1 is not a hydrogen atom or acetyl group and that when both R.sup.1 and R.sup.2 are hydrogen atoms X.sup.1 is not acetyl group or .gamma.-glutamyl group, and salts thereof, show excellent hypotensive action, antiarrhythmic action, anti-anginal action, cardiotonic action or coronary vasodilation, thus being useful as therapeutic or prophylactic agents for the cardiovascular diseases such as hypertension and angina pectoris.
    Type: Grant
    Filed: August 3, 1990
    Date of Patent: May 26, 1992
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Giichi Goto, Shigenori Ohkawa, Shoji Fukumoto
  • Patent number: 5082853
    Abstract: The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are compounds of the formula ##STR1## and the non-toxic pharmaceutically acceptable salts thereof, wherein D is the residue of a centrally acting primary, secondary or tertiary amine and ##STR2## is an unsubstituted or substituted dihydropyridyl, dihydroquinolyl or dihydroisoquinolyl radical. The corresponding ionic pyridinium, quinolinium and isoquinolinium salts ##STR3## wherein X.sup.- is the anion of a non-toxic pharmaceutically acceptable acid, are also disclosed.
    Type: Grant
    Filed: April 4, 1990
    Date of Patent: January 21, 1992
    Inventor: Nicholas S. Bodor
  • Patent number: 5064813
    Abstract: A combination therapy for treatment of selected sex steroid dependent cancers in susceptible warm-blooded animals comprising administering to such animals whose hormone output of their testes or ovaries, respectively, is blocked a therapeutically effective amount of an antiandrogen and/or an antiestrogen and/or at least one inhibitor of sex steroid biosynthesis or pharmaceutical compositions thereof wherein the selected sex steroid dependent cancer are, for example, testicular cancer, ovarian cancer, renal cancer or uterine cancer is disclosed.
    Type: Grant
    Filed: November 9, 1989
    Date of Patent: November 12, 1991
    Inventor: Fernand Labrie
  • Patent number: 5039688
    Abstract: Quaternary ammonium salts such as the benzalkonium chlorides and cetylpyridinium chloride can prevent the transmission of AIDS-causing virus through blood transfusions and through the use of blood products prepared using the blood of an AIDS infected individual.
    Type: Grant
    Filed: April 14, 1989
    Date of Patent: August 13, 1991
    Assignee: Merrell Dow Pharmaceuticals, Inc.
    Inventor: Peter J. Lewis
  • Patent number: 5017617
    Abstract: A disinfectant composition for medical use is provided that has satisfactory bactericidal effects, and that rarely causes skin damage even when used frequently. The composition comprises ethanol used for disinfection, a bactericidal agent, and an emollient, wherein said bactericidal agent is at least one selected from the group consisting of chlorhexidine digluconate, alkylpyridinium salts, and quaternary ammonium salts, and said emollient is at least one selected from the group consisting of diesters of dibasic acid, triesters of citric acid, triesters of phosphoric acid, polyoxyethylene glyceride of higher fatty acid, and polyglycerol.
    Type: Grant
    Filed: March 13, 1989
    Date of Patent: May 21, 1991
    Assignee: Saraya Kabushiki Kaisha
    Inventors: Koji Kihara, Taro Furuta
  • 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: 4970220
    Abstract: An on-occlusive base composition for personal care compositions providing enhanced conditioning and protection against dryness includes a panthenyl moisturizer and an emollient which includes a polyhydric alcoholic humectant and a polyether derivative.
    Type: Grant
    Filed: November 14, 1988
    Date of Patent: November 13, 1990
    Assignee: S. C. Johnson & Son, Inc.
    Inventor: James G. Chaussee
  • 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: 4945098
    Abstract: A derivative of 2-methylenepropane-1,3-diol of the general formula I ##STR1## where O--A.sup.1 and O--A.sup.2, which can be the same or different, each represents O, O--C(O), O--C(O)NH, O--C(S)NH or O--C(O)O, R.sup.1 represents an alkyl or alkenyl group of 10-22 carbon atoms, n is an integer from 1 to 11, B.sup.+ represents a quaternary ammonium group, either N.sup.+ R.sup.4 R.sup.5 R.sup.6, or N.sup.+ (Het), where R.sup.4, R.sup.5 and R.sup.6 are similar or different alkyl groups of 1-4 carbon atoms, or two or all of R.sup.4, R.sup.5 and R.sup.6 may be incorporated into a cyclic or bicyclic structure, which may contain additional hetero atoms; X.sup.- means the anion of a pharmceutically acceptable inorganic or organic acid; and R.sup.2 and R.sup.3 are the same or different, and represent hydrogen or alkl groups of 1-4 carbon atoms.
    Type: Grant
    Filed: July 10, 1987
    Date of Patent: July 31, 1990
    Assignee: Leo Pharmaceutical Products Ltd. A/S (Lovens Kemiske Fabrik Produktionsaktieselskab)
    Inventors: Gunnar Grue-Sorensen, Christian K. Nielsen
  • Patent number: 4939142
    Abstract: The new compounds of the general Formula I ##STR1## (wherein A stands for a C.sub.2-4 straight or branched chain alkylene group;R.sup.1 and R.sup.2 may be same or different and each stands for hydrogen, halogen, lower alkyl or lower alkoxy; orR.sup.1 and R.sup.2 together form a methylenedioxy group;R.sup.3 and R.sup.4 may be the same or different and each stands for C.sub.1.ident. alkyl or C.sub.3.notident. cycloalkyl orR.sup.3 and R.sup.4 together with the nitrogen atom, they are attached to, form a 4-7 membered ring which may contain as additional ring member an oxygen or sulfur atom or a further nitrogen atom and the latter nitrogen atom may optionally bear a C.sub.
    Type: Grant
    Filed: January 26, 1989
    Date of Patent: July 3, 1990
    Assignee: EGIS Gyogyszergyar
    Inventors: Zoltan Budai, Lujza Petocz, Tibor Mezei, Eniko Szirt nee Kiszelly, Maria Szecsey nee Hegedus, Gabor Gigler, Klara Reiter nee Esses, Aranka Lay nee Konya, Eva Furdyga, Istvan Gertyan, Istvan Gacsalyi
  • Patent number: 4925860
    Abstract: Described is a stable pharmaceutical composition of 3-(hydroxymethyl-5,5-diphenylhydantoin disodium phosphate ester, the prodrug of 5,5-diphenylhydantoin (phenytoin) a commonly used drug for the treatment and management of epilepsy and other types of convulsive states. It has been found that degradation of the prodrug to phenytoin can be controlled by controlling the pH of the composition. Controlling the pH to between 8.3 to 9.4 results in the production of diphenylglycinamide as the primary degradant and minimization of degradation to phenytoin. If the pH is maintained at a lower or higher value, then the degradation pattern changes, with earlier than expected product failure.
    Type: Grant
    Filed: May 25, 1989
    Date of Patent: May 15, 1990
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Dale E. Herbranson, Earl R. Speicher, Leonard S. Rosenberg
  • Patent number: 4874775
    Abstract: A series of novel N-pyrinidyl- and pyrimidinyl sulfonamides are useful as fungicides and herbicides particularly for the protection of plants from phytopathogens.
    Type: Grant
    Filed: June 11, 1985
    Date of Patent: October 17, 1989
    Assignee: Eli Lilly and Company
    Inventors: Eriks V. Krumkalns, David L. Smiley
  • Patent number: 4859689
    Abstract: There is disclosed a fungicidal composition comprising (A) a fungicidal compound selected from the group consisting of (i) benzimidazole compounds of the formula ##STR1## wherein W is H, or alkyl carbamoyl; Y is thiazolyl, dihydrothiazolyl, tetrahydrothiazolyl or furyl; Z is H, halogen or alkyl and (ii) benzimidazole related compounds of the formula ##STR2## wherein R.sub.3 is C.sub.1-2 alkyl, and Z is as defined above, and (B) a synergist alkyl pyridinium salt of the formula ##STR3## wherein R is an alkyl containing 8 to 20 carbon atoms; and X is a monovalent anion.
    Type: Grant
    Filed: October 31, 1986
    Date of Patent: August 22, 1989
    Assignee: Safer, Inc.
    Inventors: George S. Puritch, Edward S. Kondo
  • Patent number: 4774329
    Abstract: A complex of cyclodextrin and cetylpyridinium chloride is disclosed as a controlled release agent of cetylpyridinium chloride. The cyclodextrin can be either cyclodextrin molecule, a polymer of cyclodextrin or modified cyclodextrin. The method of forming the complex is also disclosed.
    Type: Grant
    Filed: August 4, 1987
    Date of Patent: September 27, 1988
    Assignee: American Maize-Products Company
    Inventor: Robert B. Friedman
  • Patent number: 4771059
    Abstract: The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are compounds of the formula ##STR1## and the non-toxic pharmaceutically acceptable salts thereof, wherein D is the residue of a centrally acting primary, secondary or tertiary amine and ##STR2## is an unsubstituted or substituted dihydropyridyl, dihydroquinolyl or dihydroisoquinolyl radical. The corresponding ionic pyridinium, quinolinium and isoquinolinium salts ##STR3## X.sup.-, wherein X.sup.- is the anion of a non-toxic pharmaceutically acceptable acid, are also disclosed.
    Type: Grant
    Filed: August 29, 1985
    Date of Patent: September 13, 1988
    Assignee: University of Florida
    Inventor: Nicholas S. Bodor
  • Patent number: 4764527
    Abstract: 1-Hydroxypyrazoles of the formula ##STR1## where R.sup.1, R.sup.2 and R.sup.3 independently of one another are each hydrogen or halogen, and microbicides containing these compounds.
    Type: Grant
    Filed: May 29, 1987
    Date of Patent: August 16, 1988
    Assignee: BASF Aktiengesellschaft
    Inventors: Klaus Wagner, Norbert Rieber, Ernst-Heinrich Pommer
  • Patent number: 4760053
    Abstract: A combination therapy for treatment of selected sex steroid dependent cancers in susceptible warm-blooded animals comprising administering to such animals whose hormone output of their testes or ovaries, respectively, is blocked a therapeutically effective amount of an antiandrogen and/or an antiestrogen and/or at least one inhibitor of sex steroid biosynthesis or pharmaceutical compositions thereof wherein the selected sex steroid dependent cancer are, for example, testicular cancer, ovarian cancer, renal cancer or uterine cancer is disclosed.
    Type: Grant
    Filed: July 31, 1986
    Date of Patent: July 26, 1988
    Inventor: Fernand Labrie
  • Patent number: 4749522
    Abstract: Supercritical fluids (SCF) are found to be useful in extracting desired materials from animal tissues, cells, and organs. By varying the choice of SCF, experimental conditions, and animal source material, one may obtain lipids, proteins, nucleotides, saccharids, and other desirable components or remove undesirable components.
    Type: Grant
    Filed: October 31, 1985
    Date of Patent: June 7, 1988
    Assignee: Angio-Medical Corporation
    Inventor: Ahmad R. Kamarei
  • Patent number: 4737307
    Abstract: A cleansing composition capable of removing smegma comprises in an aqueous solution a cleansing agent comprising a mixture of surface active agents in the indicated amounts as follows:(i) from a trace to 0.2% by weight, based on the total weight of said composition, as an active material of cetylpyridinium chloride,(ii) from a trace to not more than 20 ppm chlorine dioxide, plus 20 ppm sodium hypochlorite,(iii) from a trace to 1% by weight, based on the total weight of said composition as an active material, of polyoxyethylene (20) sorbitan monostearate, and(iv) sodium benzoate from a trace to 2%.
    Type: Grant
    Filed: July 23, 1987
    Date of Patent: April 12, 1988
    Inventors: Robert L. Brown, Elizabeth C. Stewart
  • Patent number: 4731373
    Abstract: Glycerine derivatives of the formula ##STR1## wherein the residues R.sup.1, R.sup.2 and R.sup.3 have the significance given in the description,and their hydrates, which inhibit blood platelet activating factor (PAF), are descried.
    Type: Grant
    Filed: December 10, 1984
    Date of Patent: March 15, 1988
    Assignee: Hoffman-La Roche Inc.
    Inventors: Richard Barner, Kasper Burri, Jean-Marie Cassal, Paul Hadvary, Georges Hirth, Klaus Muller
  • Patent number: 4725432
    Abstract: Solid stick compositions comprising a long-chain fatty alcohol having from about 8 to about 18 carbon atoms in the chain, volatile silicone and C.sub.20 or longer chain alcohols at levels of from about 1% to about 3% of the total long-chain fatty alcohol present in the compositions. These solid sticks have improved strength and hardness without undue brittleness.
    Type: Grant
    Filed: April 23, 1984
    Date of Patent: February 16, 1988
    Assignee: The Procter & Gamble Company
    Inventor: William G. May
  • Patent number: 4692450
    Abstract: Polycyclic salts of the formulaA.sup.- XN.sup.+ CH.sub.2 --(Y).sub.n --(CH.sub.2).sub.p --(Z).sub.q --L--(T).sub.r --M IwhereinA.sup.- is the anion of a strong organic or inorganic acid;XN.sup.+ is pyridinium, pyrimidinium, thiazolium or imidazolium substituted by R.sup.1, R.sup.2 and R.sup.3 ;n, q and r individually are the integer 1 or 0 and p is an integer from 1 to 15;Y is CH.sub.2, C(H,OH) or C(O);Z is O, S, CH.sub.2, C(O), NQ.sup.1, SO.sub.2, C(O)O, OC(O), C(O)N(Q.sup.1) or N(Q.sup.1)C(O);L is p-phenylene substituted by R.sup.4 ; andM is phenyl substituted by R.sup.5 and R.sup.6,T has one of the meanings given above, for Z or is C(CH.sub.3).sub.2, C.sub.2 H.sub.4, C(Q.sup.2).dbd.C(Q.sup.3), C.tbd.C, CH.sub.2 C(O), C(O)CH.sub.2, CH.sub.2 O or OCH.sub.2,R.sup.1 is a group Ar, Ar--C.sub.1-4 -alkyl, ArO or Arc(O),Ar is phenyl substituted by R.sup.7, R.sup.8 and R.sup.9 ;R.sup.2 and R.sup.3 individually are H, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy or C.sub.6 H.sub.
    Type: Grant
    Filed: January 10, 1986
    Date of Patent: September 8, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean-Marie Cassal, Albrecht Edenhofer, Henri Ramuz
  • Patent number: 4692262
    Abstract: A cleansing composition capable of removing smegma comprises in an aqueous solution a cleansing agent comprising a mixture of surface active agents in the indicated amounts as follows:(i) from a trace to 0.2% by weight, based on the total weight of said composition, as an active material of cetylpyridinium chloride,(ii) from a trace to not more than 20 ppm chlorine dioxide,(iii) from a trace to 1% by weight, based on the total weight of said composition as an active material, of polyoxyethylene (20) sorbitan monosterate, and(iv) sodium lauryl sulfate from a trace to 2%.
    Type: Grant
    Filed: September 18, 1986
    Date of Patent: September 8, 1987
    Inventors: Robert L. Brown, Elizabeth C. Stewart
  • Patent number: 4576950
    Abstract: There is disclosed a fungicidal composition comprising (A) a fungicidal benzimidazole compound of the formula ##STR1## wherein W is H, or alkyl carbamoyl; Y is H, halogen, alkyl, alkoxy, alkyl thio, thiol, carbamic acid ester or hydroxy; Z is H, halogen or alkyl; and (B) a synergist alkyl pyridinium salt of the formula ##STR2## wherein R is an alkyl containing 8 to 20 carbon atoms; and X is a monovalent anion.
    Type: Grant
    Filed: December 14, 1983
    Date of Patent: March 18, 1986
    Assignee: Safer Agro-Chem Ltd.
    Inventors: George S. Puritch, Edward S. Kondo
  • Patent number: 4568683
    Abstract: A lipid metabolism improving drug or pharmaceutical composition contains pantetheine-S-sulfonic acid as an active ingredient. When an effective dose of pantetheine-S-sulfonic acid or a pharmaceutically active, non-toxic salt thereof is administered to an animal, such as a human, in pure form or composition form, the lipid concentration in the plasma is lowered, lipid peroxide concentration in the serum and liver is lowered, B-lipo protein-cholesterol concentration in serum is decreased and HDL-cholesterol concentration is increased.
    Type: Grant
    Filed: April 9, 1984
    Date of Patent: February 4, 1986
    Assignee: Sogo Pharmaceutical Company Limited
    Inventors: Tetsuya Suga, Omanabu Katsumata, Tomoyasu Tashiro
  • Patent number: 4563446
    Abstract: Novel compounds of the formula: ##STR1## wherein R.sup.2 is an aromatic or heterocyclic group, which may optionally be substituted, R.sup.2 is a methyl group, a hydroxymethyl group, a nitroxymethyl group, a formyl group, a nitrogen-containing five-membered ring-methyl group, an acetal-methyl group, a trialkylsilyloxymethyl group, an alkyl- or aryl-sulfonyloxymethyl group, an alkyl- or aryl-sulfonylaminocarbonyloxymethyl group, an acyloxymethyl group, an alkoxycarbonyloxymethyl group, a halogenomethyl group, an alkoxymethyl group, an aryloxymethyl group, a cyano group, a carbamoyl group which may optionally be substituted, a carbamoyloxymethyl group which may optionally be substituted, a thiocarbamoyloxymethyl group which may optionally be substituted, and an alkoxycarbonyl group, n is an integer of 1 to 20, and ##STR2## provided that n is an integer of 9 to 20 when ##STR3## and, at the same time, R.sup.
    Type: Grant
    Filed: July 19, 1984
    Date of Patent: January 7, 1986
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shinji Terao, Kohei Nishikawa
  • Patent number: 4562193
    Abstract: Compounds of formula (I): ##STR1## (in which R.sup.1, R.sup.2 and R.sup.6 represent hydrogen or methyl, R.sup.3 represents methyl or ethyl, R.sup.4 represents an alkyl group or allyl and R.sup.5 represents hydrogen, methyl or chlorine) and acid addition salts thereof have acaricidal and insecticidal activity and may be formulated with suitable carriers or diluents for agricultural, horticultural or domestic use. Processes for the preparation of these compounds are also disclosed.
    Type: Grant
    Filed: July 8, 1983
    Date of Patent: December 31, 1985
    Assignees: Sankyo Company Limited, UBE Industries Ltd.
    Inventors: Shinjiro Yamamoto, Shinji Yokoi, Keigo Matsumoto, Takeo Honda, Takashi Kobayashi
  • Patent number: 4532248
    Abstract: 1,4-Dihydropyridines of the formula ##STR1## in which n is 0,1 or 2, andR.sup.1 to R.sup.7 can have a wide variety of meanings, which possess inotropic action, and many of which are new, are useful in increasing the influx of Ca.sup.++ into cells, particularly in combatting coronary and vascular diseases, hypertension swelling in the mucous membranes and diseases involving increased blood sugar or an incorrect salt and fluid balance.
    Type: Grant
    Filed: July 14, 1982
    Date of Patent: July 30, 1985
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gerhard Franckowiak, Horst Boshagen, Friedrich Bossert, Siegfried Goldmann, Horst Meyer, Egbert Wehinger, Jurgen Stoltefuss, Matthias Schramm, Gunter Thomas, Robertson Towart