Ring Is Alcohol Moiety Patents (Class 514/548)
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Patent number: 4939173Abstract: Aryloxyalkanol derivatives having the formulaAr--O(CH.sub.2).sub.n OHwherein n is an integer from 3 to 8 and Ar is (1) 1- or 2-naphthylenyl, (2) phenyl optionally substituted by from 1 to 3 C.sub.1-4 lower alkyl groups, or (3) a diphenyl moiety of structure ##STR1## wherein Y is a bond, CH.sub.2 or CH.sub.2 O, and esters thereof have antiretrovirus activity and are effective in a method for treating a retrovirus infection.Type: GrantFiled: December 14, 1988Date of Patent: July 3, 1990Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Roger A. Parker, Sai P. Sunkara
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Patent number: 4938960Abstract: The present invention relates to a method for the treatment and protection of human and animal skin which contains vitamin E in a high dose and, in addition, may optionally further contain vitamin C, vitamin A, vitamins of the B series, blood circulation-promoting agents and/or vasodilators, phospholipids, unsaturated fatty acids and/or emulsifiers.Type: GrantFiled: June 21, 1988Date of Patent: July 3, 1990Inventor: Roshdy Ismail
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Patent number: 4939169Abstract: Novel 1,4-naphthalenediol and 1,4-hydroquinone derivatives of formula I, II, III and IV and their therapeutic uses as 5-lipoxygenase inhibitors, leukotriene inhibitors, antiinflammatory and/or inhibitors of mucus secretion agents are described. Also provided are novel intermediates useful for the preparation of said derivatives.Type: GrantFiled: March 13, 1989Date of Patent: July 3, 1990Assignee: The Upjohn CompanyInventors: Gordon L. Bundy, Chiu-Hong Lin
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Patent number: 4937388Abstract: The invention provides insecticidally active compounds of formula I: ##STR1## wherein A is selected from oxygen and a group of formula S(O).sub.n, where n represents 0, 1 or 2; W represents one or two substituents selected from halo, alkyl, alkoxy, alkoxyalkyl, haloalkyl and haloalkoxy, or W represents a bidentate group linking adjacent carbon atoms, selected from alkylene and alkylenedioxy; Y represents a substituted aryl group where each substituent is selected from halo, alkyl, aryl, aralkyl, aryloxy and arylamino; Z represents a fluoroalkyl group of up to two carbon atoms; and either X' represents hydrogen and X is selected from hydrogen, halo, hydroxy, alkoxy and acyloxy, or X and X' together represent a second bond between the adjacent carbon atoms.The invention also provides processes and intermediates useful for the preparation of the compounds of formula I, insecticidal compositions comprising the compounds of formula I, and methods of combating and controlling pests therewith.Type: GrantFiled: October 29, 1987Date of Patent: June 26, 1990Assignee: Imperial Chemical Industries PLCInventors: Michael J. Bushell, Robin A. E. Carr
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Patent number: 4937243Abstract: Novel compounds of the formula (I), processes for their preparation and their use as collagenase inhibitors are described: ##STR1## in which R.sub.1 is hydroxy; alkoxy; aryloxy; aralkyloxy; --NR.sub.6 R.sub.7 where R.sub.6 and R.sub.7 are hydrogen or alkyl, or R.sub.6 and R.sub.7 together with the N-atom to which they are bonded form a 5- to 7-membered ring with an optional heteroatom; --NHCH(R.sub.8)COR.sub.9 where R.sub.8 is hydrogen; alkyl optionally substituted by hydroxy, alkoxy, --NR.sub.6 R.sub.7, quanidine, CO.sub.2 H, CONH.sub.2, SH, or S-alkyl; or CH.sub.2 -AR where Ar is optionally substituted aryl; and R.sub.9 is hydroxy, alkoxy or --NR.sub.6 R.sub.7.R.sub.2 is hydrogen or acyl.R.sub.3 is C.sub.3-6 alkyl.R.sub.4 is hydrogen; alkyl; --CH.sub.2 R.sub.10 where R.sub.10 is optionally substituted phenyl or heteroaryl; or --CH(R.sub.12)O--R.sub.11 where R.sub.11 is hydrogen; alkyl; or --CH.sub.2 Ph where Ph is optionally substituted phenyl; and R.sub.12 is hydrogen or alkyl.R.sub.Type: GrantFiled: December 22, 1987Date of Patent: June 26, 1990Assignee: Beecham Group p.l.c.Inventors: Roger E. Markwell, Stephen A. Smith, Ian Hughes
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Patent number: 4921873Abstract: This invention relates to antiviral and antitumor compositions, a process for producing the compositions and a method for inhibiting viruses and tumors utilizing the compositions. More particularly, the compositions are cyclohexadienone derivatives which are derived from red alga Desmia hornemanni.Type: GrantFiled: June 14, 1985Date of Patent: May 1, 1990Assignee: Harbor Branch Oceanographic Institution, Inc.Inventors: Tatsuo Higa, Kenneth M. Snader
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Patent number: 4918095Abstract: The compound N-[(1S,2R)-fluoromethyl-2-hydroxy-2-(4-methylsulphonyl-phenyl)-ethyl]-2-pr openamide and the derivatives thereof in which the hydroxy in 2 position is esterified by a mono or dicarboxylic acid or by an aminoacid are described.Such compounds have antibiotic activity and are useful in human and veterinary therapy.Type: GrantFiled: December 18, 1987Date of Patent: April 17, 1990Assignee: Zambon S.p.A.Inventors: Davide Della Bella, Giancarlo Jommi, Mario Fantucci, Dario Chiarino
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Patent number: 4918103Abstract: A pharmaceutically elegant, one phase, liquid composition for oral administration comprises a NSAID such as ibuprofen plus a di- or triglyceride of a medium chain fatty acid edible oil which has the characteristics of a pharmaceutical solvent carrier as known to those skilled in the art. Other pharmaceutical additives may be optionally added. An additional stipulation is that ethanol or other monohydric alcohol solvents should not be present.Type: GrantFiled: July 25, 1988Date of Patent: April 17, 1990Assignee: Formulations Development LabsInventors: Moo K. Park, Henry C. Caldwell
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Patent number: 4902714Abstract: Compounds of the formula (II) ##STR1## wherein R.sub.1 and R.sub.2 are each separately selected from hydrogen, alkyl, alkenyl and alkynyl groups having up to a maximum of four carbon atoms and being unsubstituted, and alkyl, alkenyl and alkynyl groups having up to a maximum of three carbon atoms and being substituted by one, or in the case of fluoro by one or more, substitutents but with the proviso that when R.sub.1 is hydrogen then R.sub.2 is hydrogen or methyl, or R.sub.1 and R.sub.2 together constitute an ethylene bridging group, and R.sub.3 is a group which under physiological conditions undergoes elimination with the formation of a 3,5-dioxopiperazinyl ring, with the further proviso that the compound is in the meso or erythro configuration when each of R.sub.1 and R.sub.Type: GrantFiled: April 19, 1988Date of Patent: February 20, 1990Assignee: National Research Development CorporationInventors: Andrew M. Creighton, William A. Jeffery
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Patent number: 4886835Abstract: Substituted alkadienes of the formula: ##STR1## in which R.sub.1 is hydroxy or acetoxy, R.sub.2 is hydrogen, carboxy, alkoxycarbonyl, phenyl or benzoyl, andR.sub.3 is alkylthio or alkoxy and R.sub.4 is naphthoyl or optionally substituted benzoyl,or R.sub.3 is alkoxycarbonyl, cycloalkyloxycarbonyl or cyano and R.sub.4 is alkyl, naphthyl, optionally substituted phenyl, alkylthio, naphthylmethanethio, optionally substituted benzylthio, optionally substituted phenylthio, naphthylthio, phenethylthio or allylthio,or R.sub.3 and R.sub.4 form, with the carbon atom to which they are attached, a ring-system of formula: ##STR2## in which R.sub.5 is hydrogen or alkoxy and X is methylene or S inhibit 5-lipoxygenase and are useful, for example, as anti-inflammatories.Type: GrantFiled: September 26, 1988Date of Patent: December 12, 1989Assignee: Rhone-Poulenc SanteInventors: Jean-Luc Malleron, Gerard Ponsinet, Gerard Roussel
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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
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Patent number: 4840970Abstract: Disclosed herein is an aqueous solution containing a lipid-soluble active vitamin substance and/or ubiquinone. The solution has a pH of 5.5-8 and additionally contains a hydrogenated lecithin and neutral amino acid. It is stable and free from side effects, and is rather easy to prepare.Type: GrantFiled: June 1, 1987Date of Patent: June 20, 1989Assignee: Eisai Co., Ltd.Inventors: Hiroyuki Ohasi, Toru Takami, Noritoshi Koyama, Yoshio Kogure, Katsumi Ida, Kazumi Iijima, Tomohiro Kobori
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Patent number: 4826873Abstract: Compounds of the general formula ##STR1## wherein R.sub.1 represents hydrogen, an acyl group having 1 to 18 carbon atoms or both R.sub.1 together the group ##STR2## R.sub.2 represents hydrogen or a methyl group, have been isolated in small amounts from the leaves of Clausena lansium. The new compounds are to be used for the production of compositions for the use of the treatment of acute and chronical viral hepatitis, liver intoxication, hypoxia or amnesia.Type: GrantFiled: January 15, 1987Date of Patent: May 2, 1989Assignees: Chinese Academy of Medical Sciences, Bayer AktiengesellschaftInventors: Ming-he Yang, Yan-rong Chen, Geng-tao Liu, Liang Huang
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Patent number: 4824867Abstract: Quaternary ammonium compounds have the formula R.sup.1 R.sup.2 R.sup.3 N.sup.+ (CH.sub.2).sub.m Y X.sup.- wherein R.sup.1 is an alkyl containing 8-20 carbon atoms, R.sup.2 is an alkyl containing 8-20 carbon atoms or methyl or ethyl, R.sup.3 is methyl or ethyl, m is an integer from 1-6, X is an anion and Y is a group having the structure --Z, --OH, --OR.sup.4, --OC(O)R.sup.5, --CN, --O--S(O) (O)--OQ, --C(O)OR.sup.6, --C.dbd.CH, --SR.sup.7, --S(O)(O)R.sup.8, --S(O)R.sup.9, --NR.sup.10 R.sup.11 and --CH.dbd.CH.sub.2 wherein R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11 are alkyls containing 1-12 carbon atoms or are phenyl and Z is halogen and Q is hydrogen or a cation having been found to be very effective bactericides.Type: GrantFiled: September 22, 1986Date of Patent: April 25, 1989Inventors: Kim R. Smith, James E. Borland, Joe D. Sauer
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Patent number: 4810697Abstract: The present invention concerns a pharmacological vehicle or carrier system, which makes possible administration of the active ingredient with a high absorption thereof in the blood circulation of the patient treated therewith, in particular also in the case of oral administration. The pharmacological vehicle system according to the invention comprises ultrafine particles of a reaction product of a reactive derivative of an at least dibasic inorganic acid or an alkane-carboxylic acid having 2 or 3 carboxyl groups and optionally one or two hydroxy groups, wherein one bond of the dibasic inorganic acid or one carboxy group of the alkane-carboxylic acid is bonded to a pharmacological active ingredient containing a hydroxy group, SH group and/or a primary or secondary amino group having a ractive hydrogen atom on this group, and the other bond is bonded to the free hydroxy group of a glycerolipid having at least one free hydroxy group on the glycerol.Type: GrantFiled: October 15, 1982Date of Patent: March 7, 1989Inventors: Peter Speiser, M. Orhan Vaizoglu
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Patent number: 4804535Abstract: Disclosed are aqueous multivitamin/trace elements formulations stabilized by a water soluble, organic acid that contains carbon-to-carbon unsaturation and water soluble salts thereof selected from the group consisting of maleic acid, fumaric acid, maleamic acid and acrylic acid.Type: GrantFiled: February 8, 1988Date of Patent: February 14, 1989Assignee: Rorer Pharmaceutical CorporationInventors: Morris Kesselman, Abdur R. Purkaystha, James Cahill
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Patent number: 4801610Abstract: Phenolic esters of the general formula I ##STR1## are useful for the prevention, management or alleviation of elastase mediated diseases or conditions.Type: GrantFiled: June 5, 1987Date of Patent: January 31, 1989Assignee: G. D. Searle & Co.Inventors: Masateru Miyano, James R. Deason
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Patent number: 4785004Abstract: Novel asymmetric thioethers of the formula ##STR1## in which the general symbols have the following meanings: R.sup.0 represents hydrogen or C.sub.1-7 -alkanoyl,R.sup.1 represents C.sub.1-3 -alkyl which may be substituted by one or more halogen atoms having an atomic number of at most 17,R.sup.2 represents an aliphatic radical having from 5 to 15 carbon atoms,A represents ethylene, a single bond or vinylene,B.sup.1 represents C.sub.1-7 -alkylene or phenylene,B.sup.2 represents a single bond, ethylene or phenylene, andM represents an aromatic radical of the partial formula ##STR2## in which the symbols have the following meanings: R.sup.3 represents hydrogen or C.sub.1-4 -alkyl,X represents NH, O, S or if R.sup.4 represents hydrogen, a single bond,one of the symbols R.sup.4 and R.sup.5 represents hydrogen and the other represents the group --CO--R.sup.6, orR.sup.4 and R.sup.5 together represent the radical --CO--C(R.sup.6).dbd.C(R.sup.7)--or--CO--C(R.sup.7).dbd.C(R.sup.6)--orR.sup.4 R.sup.Type: GrantFiled: December 15, 1986Date of Patent: November 15, 1988Assignee: Ciba-Geigy CorporationInventors: Andreas Von Sprecher, Werner Breitenstein, Andreas Beck, Robert W. Lang, Konrad Oertle
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Patent number: 4764530Abstract: Pharmaceutical compositions and their use in ophthalmology. Said compositions comprise ibopamine (epinine 3, 4-0-diisobutyrate and are used mainly as mydriatics.Type: GrantFiled: August 26, 1986Date of Patent: August 16, 1988Inventors: Angelo Carenzi, Oreste Cerri, Franco Pozzi, Cesare Casagrande, Giovanna Miragoli, Michele Virno
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Patent number: 4760061Abstract: Mono- or bis-complex esters or ethers of a phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined mono- or bis-phenolic nucleus including a hydroxyphenyl-hydroxynaphthyl; hydroxyphenyl-hydroxyindanyl, hydroxyphenyl-hydroxybenzothienyl or di-hydroxyphenyl-ethylene or vinylene nucleus; whereinA is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages, whereinR.sup.1 is hydrogen, or alkyl, alkenyl, cycloalkyl, halogenoalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 -- or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --S--, --SO-- or --SO.sub.2 --, whereinR.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene; whereinR.sup.12 is hydrogen or alkyl, and whereinR.sup.22 is hydrogen, cyano or nitro; or a salt thereof when appropriate.Type: GrantFiled: April 24, 1985Date of Patent: July 26, 1988Assignee: Imperial Chemical Industries PLCInventors: Philip N. Edwards, Brian S. Tait
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Patent number: 4760087Abstract: Phenol derivatives of the formula ##STR1## wherein A and B have the same or different meanings and each represent one of the groups --C.tbd.C--, cis--CH.dbd.CH-- or trans--CH.dbd.CH--, R.sub.1 is hydrogen, an optionally substituted alkyl or phenyl group or a cycloalkyl group, R.sub.2 is hydrogen, methyl or ethyl, R.sub.3 represents hydrogen, acetyl or propionyl, R.sub.4 has the same meaning as R.sub.3 or represents an alkyl group, R.sub.5 is a carboxylic or a hydroxy group or a functional derivative of such groups or R.sub.5 is a nitrile group and R.sub.6 is hydrogen, an alkyl group or the group OR.sub.4 which specifically inhibit 5-lipoxygenase and are useful in pharmaceutical compositions for prophylaxis and treatment of diseases due to the action of leukotrienes. The compounds are prepared by reacting suitable acetylene compounds or metal derivatives thereof with alkyl or aryl halides or by means of Wittig reactions optionally followed by transforming the member R.sub.Type: GrantFiled: May 13, 1986Date of Patent: July 26, 1988Assignee: Gruenenthal GmbHInventors: Oswald K. Zimmer, Werner P. Vollenberg, Gerriet K. H. Loschen, Werner Winter, Erwin Kiesewetter, Ulrich G. P. Seipp
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Patent number: 4758591Abstract: Disclosed herein are dialkanoyloxybenzylidene dialkanoate represented by the formula, ##STR1## wherein X.sup.1 and X.sup.2 represent respectively alkanoyloxy group and a pharmaceutical composition in dosage unit form which comprises a dosage effective for the treatment of inflammatory disease of the dialkanoyloxybenzylidene dialkanoate as an active ingredient thereof.Type: GrantFiled: December 13, 1984Date of Patent: July 19, 1988Assignee: Kureha Kagaku Kogyo Kabushiki KaishaInventors: Hitoshi Takita, Fumihiko Kimura, Sakuo Noda, Yutaka Mukaida, Toyohiko Nitta
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Patent number: 4755524Abstract: The compounds of the present invention comprise substituted phenolic thioethers represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different and independently represent tert-alkyl or phenyl; A represents methylene or methylene substituted by alkyl, dialkyl or hydroxy, provided that when A includes hydroxymethylene, the hydroxymethylene group is not adjacent to a heteroatom; B represents sulfur, sulfoxide, sulfone, oxygen, --NH-- or nitrogen substituted by alkyl, phenyl, benzyl, substituted phenyl or substituted benzyl; C represents methylene or methylene substituted by alkyl; R.sub.3 represents CO.sub.2 H, CO.sub.2 -alkyl or a tetrazole group; m is 0 or 1, n is 2, 3 or 4 and p is 1, 2 or 3; and the pharmaceutically acceptable salts thereof.Type: GrantFiled: January 15, 1987Date of Patent: July 5, 1988Assignee: G. D. Searle & Co.Inventors: Richard A. Mueller, Richard A. Partis, James R. Deason
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Patent number: 4751240Abstract: A phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined phenolic nucleus including a phenyl-hydroxynaphthyl; hydroxyphenyl-naphthyl; phenyl-hydroxyindanyl, phenyl-hydroxybenzothienyl or mono-hydroxyphenyl-ethylene or vinylene nucleus; wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages, wherein R.sup.1 is hydrogen, or alkyl, alkenyl, alkynyl, cycloalkyl, halogenoalkyl, alkoxyalkyl, halogenoalkoxyalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 --or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --(PO)R.sup.2 13 , --S--, --SO--or --SO.sub.2 --, wherein R.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene; wherein R.sup.12 is hydrogen or alkyl, and wherein R.sup.22 is hydrogen, cyano or nitro; or a salt thereof when appropriate.Type: GrantFiled: April 24, 1985Date of Patent: June 14, 1988Assignee: Imperial Chemical Industries PLCInventors: Jean Bowler, Graham C. Crawley, Philip N. Edwards, Alasdair T. Glen, Michael S. Large, Brian S. Tait
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Patent number: 4745233Abstract: Antitumor compounds corresponding to the following formula: ##STR1## in which the substituents R.sub.1 and R.sub.2 may be the same or different and represent hydrogen, an aminocarbonyl group, a C.sub.1 -C.sub.6 alkylaminocarbonyl group, a di-C.sub.1 -C.sub.6 -alkylaminocarbonyl group, the group PO(OH).sub.2, a C.sub.2 -C.sub.8 alkanoyl group, a C.sub.2 -C.sub.8 halogen alkanoyl group or a C.sub.3 -C.sub.8 alkenoyl group, a process for their preparation, and their use in treating oestrogen-receptor-positive-tumors as well as the prostate carcinoma.Type: GrantFiled: June 9, 1986Date of Patent: May 17, 1988Assignee: Asta-Werke AktiengesellschaftInventors: Helmut Schonenberger, Rolf W. Hartmann, Martin Schneider, Walter Schwarz, Jurgen Engel
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Patent number: 4740373Abstract: Disclosed are aqueous multivitamin/trace elements formulations stabilized by a water soluble, organic acid that contains carbon-to-carbon unsaturation and water soluble salts thereof selected from the group consisting of maleic acid, fumaric acid, maleamic acid and acrylic acid.Type: GrantFiled: May 27, 1986Date of Patent: April 26, 1988Assignee: USV Pharmaceutical CorporationInventors: Morris Kesselman, Abdur R. Purkaystha, James Cahill
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Patent number: 4711903Abstract: The compounds of the present invention comprise substituted phenolic thioethers represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different and independently represent tert-alkyl or phenyl; A represents methylene or methylene substituted by alkyl, dialkyl or hydroxy, provided that when A includes hydroxymethylene, the hydroxymethylene group is not adjacent to a heteroatom; B represents sulfur, sulfoxide, sulfone, oxygen, --NH-- or nitrogen substituted by alkyl, phenyl, benzyl, substituted phenyl or substituted benzyl; C represents methylene or methylene substituted by alkyl; R.sub.3 represents CO.sub.2 H, CO.sub.2 -alkyl or a tetrazole group; m is 0 or 1, n is 2, 3 or 4 and p is 1, 2 or 3; amd the pharmaceutically acceptable salts thereof.Type: GrantFiled: January 31, 1986Date of Patent: December 8, 1987Assignee: G. D. Searle & Co.Inventors: Richard A. Mueller, Richard A. Partis, James R. Deason
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Patent number: 4705805Abstract: Certain 2,2'-dithiobis-N-substituted or unsubstituted benzamides or derivatives thereof are useful as antithrombotic agents because of their ability to suppress aggregation of blood platelets.Type: GrantFiled: February 17, 1987Date of Patent: November 10, 1987Inventors: Koji Yamada, Tamotsu Hashimoto, Masao Naruse, Yo Murayama, Hideki Ninno
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Patent number: 4683241Abstract: Phenolic esters of the general formula I ##STR1## are useful for the prevention, management or alleviation of elastase mediated diseases or conditions.Type: GrantFiled: May 21, 1984Date of Patent: July 28, 1987Assignee: G. D. Searle & Co.Inventors: Masateru Miyano, James R. Deason
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Patent number: 4675341Abstract: The invention relates to novel [(5,6-dichloro-3-oxo-9a-propyl-2,3,9,9a-tetrahydrofluoren-7-yl)oxy]ethanol , its derivatives, and their salts. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections including that due to AIDS virus, various brain concussions and elevated intracranial pressure.Type: GrantFiled: August 13, 1986Date of Patent: June 23, 1987Assignee: Merck & Co., Inc.Inventor: Edward J. Cragoe, Jr.
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Patent number: 4670247Abstract: A process is described for the preparation of fat-soluble vitamin active beadlet compositions which exhibit superior stability when exposed to the feed pelleting process. The process includes forming an aqueous emulsion of a fat-soluble vitamin-active material, gelatin, and a sugar converting the emulsion to dry particulate form containing the non-aqueous constituents of the emulsion and heat treating the resulting product to form water insoluble beadlets.Type: GrantFiled: March 24, 1986Date of Patent: June 2, 1987Assignee: Hoffman-LaRoche Inc.Inventor: Leonard J. Scialpi
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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: 4663351Abstract: A novel, orally administrable pro-drug form of dobutamine of the formula ##STR1## or a pharmaceutically acceptable acid addition salt thereof.Type: GrantFiled: August 23, 1985Date of Patent: May 5, 1987Assignee: Berlex Laboratories, Inc.Inventor: Julius Diamond
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Patent number: 4618624Abstract: A method for increasing the growth rate and/or improving the lean meat to fat ratio in farm and domestic animals. An effective amount of a 3-amino-4-hydroxy(or alkoxy)phenethanolamine derivative, pharmacologically-acceptable acid addition or metal salt thereof is administered either orally or parenterally to animals. Novel 3-amino-4-hydroxy(or alkoxy)phenethanolamine derivatives are also described.Type: GrantFiled: July 5, 1984Date of Patent: October 21, 1986Assignee: American Cyanamid CompanyInventor: Goro Asato
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Patent number: 4612192Abstract: New oil components for cosmetic and pharmaceutical applications consist of reaction products of epoxidized triglyceride oils with monohydric alcohols containing from 1 to 4 carbon atoms. The oil components are produced by reacting an epoxidized triglyceride oil containing from about 4 to about 8% by weight of epoxide oxygen, preferably an epoxidized soya bean oil containing from about 6 to about 7% by weight of epoxide oxygen, in the presence of an acidic catalyst with a monohydric C.sub.1 -C.sub.4 -alcohol, preferably methanol, in excess at the boiling temperature of the alcohol until the oxirane rings have been completely opened, followed by neutralizing the catalyst and distilling off the excess alcohol. The new oil components are eminently suitable, inter alia, for the production of cosmetic stick preparations.Type: GrantFiled: July 12, 1984Date of Patent: September 16, 1986Assignee: Henkel Kommanditgesellschaft auf AktienInventors: Ingeborg Scheuffgen, Alfred Meffert
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Patent number: 4596828Abstract: [(2-Hydroxy-5-alkoxyphenyl)methylthio]phenylmethanol and derivatives thereof were prepared from an appropriate 2-hydroxy-5-alkoxybenzaldehyde with a hydroxymethylthiophenol. These compounds were found to be potent anti-inflammatory agents.Type: GrantFiled: March 28, 1985Date of Patent: June 24, 1986Assignee: Merck & Co., Inc.Inventors: Milton L. Hammond, Robert A. Zambias
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Patent number: 4594356Abstract: A method of inducing short-term pupil diameter enlargement and reducing intraocular pressure in animals without significant systemic effects is disclosed. There is provided a site-specific chemical delivery method for topically applying to the eye of an animal, an effective ophthalmologically acceptable amount of an adrenalone diester of the general formula: ##STR1## wherein R prepresents a member selected from the group consisting of hydrogen or a C.sub.1 -C.sub.3 straight alkyl group; and wherein R.sub.1 and R.sub.2 independently represent an acyl group or derivative thereof; or an opthalmologically acceptable acid addition salt thereof. The method allows the pupil diameter to be enlarged for a short period after which the pupil returns to normal and thus restores normal eye sight.Type: GrantFiled: January 8, 1985Date of Patent: June 10, 1986Assignee: Key Pharmaceuticals, Inc.Inventor: Nicholas Bodor
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Patent number: 4590210Abstract: Compositions for treating ocular hypertension by topical administration containing .alpha.-methyl epinephrine, .alpha.-methyl norepinephrine, their C.sub.1 -C.sub.8 alkanoyl diesters and the pharmacologically acceptable acid addition salts thereof are disclosed.Type: GrantFiled: April 1, 1981Date of Patent: May 20, 1986Inventor: Maurice E. Langham
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Patent number: 4587262Abstract: The invention concerns novel glyceride esters of anti-bacterial halogenated phenols having the formula I in which Ra and Rb are independently (3-20C)alkyl or (3-20C)alkenyl; Rc and Rd are independently chloro or bromo; Re is hydrogen, chloro or bromo; and A is (1-6C)alkylene optionally bearing one or two (1-4C)alkyl substituents.The esters are of use in the prophylaxis and/or therapy of acne vulgaris. Pharmaceutical compositions for topical administration and processes for the manufacture of the esters are also provided.Type: GrantFiled: June 6, 1983Date of Patent: May 6, 1986Assignee: Imperial Chemical Industries PLCInventors: Jean C. Arnould, John R. Evans, Geraint Jones, David S. Thomson
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Patent number: 4576964Abstract: Tricyclic benzo fused compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, wherein n is zero, 1 or 2, and t is 1 or 2; M is CH or N, R.sub.1 is H or certain acyl groups; Q is CO.sub.2 R.sub.4, COR.sub.5, C(OR.sub.7)R.sub.5 R.sub.6, CN, CONR.sub.9 R.sub.10, CH.sub.2 NR.sub.9 R.sub.10, CH.sub.2 NHCOR.sub.11, CH.sub.2 NHSO.sub.2 R.sub.12, 5-tetrazolyl or when n is 1, Q and OR.sub.1 together form a lactone or certain reduced derivatives thereof; and Z is certain alkyl, alkoxy, alkoxyalkyl, aralkyl, aralkoxy, aryloxyalkyl or aralkoxyalkyl groups, are valuable central nervous system active agents, methods for their use, pharmaceutical compositions containing them and certain intermediates therefor.Type: GrantFiled: June 7, 1984Date of Patent: March 18, 1986Assignee: Pfizer Inc.Inventors: James F. Eggler, Michael R. Johnson, Lawrence S. Melvin, Jr.
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Patent number: 4562206Abstract: A method for increasing cardiac contractility in a warm-blooded animal suffering from acutely depressed cardiac contractility which comprises administering to said animal an effective amount of a compound of the formula ##STR1## wherein R is hydrogen or isobutyrate, or a pharmaceutically acceptable acid addition salt thereof.Type: GrantFiled: March 8, 1984Date of Patent: December 31, 1985Assignee: Key Pharmaceuticals, Inc.Inventor: Ronald R. Tuttle
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Patent number: 4559360Abstract: New cysteine derivatives of mucolytic, antipyretic, analgesic and anti-inflammatory action are described, which are obtained by condensing S-(carboxymethyl)-L-cysteine with acetylsalicylic acid. The present invention also relates to salts of the new compounds formed with alkaline and/or alkaline-earth metals, ammonium salts, salts formed with compatible amines, with amino acids or with physiologically acceptable acids. A process is also described for their preparation.Type: GrantFiled: November 21, 1984Date of Patent: December 17, 1985Assignee: Magis Farmaceutici S.R.L.Inventor: Laura Puricelli
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Patent number: 4540695Abstract: Aminonaphthacene derivatives of the formula: ##STR1## wherein A is either one of the following groups: ##STR2## wherein R.sup.1 is a hydrogen atom or a group of the formula: --COR.sup.7, R.sup.2 and R.sup.3 are each a lower alkoxy group or, when taken together, represent an ethylenedioxy group or an oxo group, R.sup.4 and R.sup.5 are both hydrogen atoms or either one of them is a hydrogen atom and the other is a group of the formula: --COR.sup.7, R.sup.6 is a hydrogen atom, a hydroxyl group or a group of the formula: --OCOR.sup.7 and R.sup.7 is a lower alkyl group, a halo(lower)alkyl group, a phenyl group or a halophenyl group, which are useful as anti-microbial and/or anti-tumor agents, or as intermediates in their production.Type: GrantFiled: August 11, 1982Date of Patent: September 10, 1985Assignee: Sumitomo Chemical Co., Ltd.Inventors: Kikuo Ishizumi, Naohito Ohashi, Michihisa Muramatsu
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Patent number: 4540567Abstract: A cosmetically acceptable composition contains a C.sub.1 -C.sub.4 alkyl lactate dissolved in a mixture of water and a water-miscible C.sub.2 -C.sub.4 alkylene glycol of a polymer thereof. The composition should have stabilized pH of less than 7.Type: GrantFiled: September 17, 1979Date of Patent: September 10, 1985Assignee: Lever Brothers CompanyInventors: Francis E. J. Oneto, Marc Vermersch
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Patent number: 4530845Abstract: 1,4-naphthoquinone derivatives represented by the following general formula: ##STR1## (wherein R.sup.1 represents a hydrogen atom, a hydroxy group, a lower alkoxy group or an arylthio group, R.sup.2 represents a carboxy group, an esterified carboxy group or an amidated carboxy group or, when taken together, R.sup.1 and R.sup.2 form a group of ##STR2## R.sup.3 represents a hydrogen atom or a lower alkyl group, R.sup.4 represents a lower alkyl group, R.sup.5 represents a hydrogen atom or a halogen atom, and R.sup.6 represents a hydrogen atom, a lower alkyl group or a lower alkanoyl group), and the salts of the carboxy group thereof, which are novel compounds having an anticoccidium activity, and which can be obtained by synthesis or, partly, by cultivation of Streptomyces auranticolor.Type: GrantFiled: July 6, 1983Date of Patent: July 23, 1985Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Koichi Ikushima, Hirokazu Tanaka, Ohe Osamu, Eiko Kino, Masanobu Kohsaka, Hatsuo Aoki, Akira Arakawa, Hiroshi Imanaka
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Patent number: 4530934Abstract: There are described a new pharmaceutically active derivative of ursolic acid, 3.beta.-(3-carboxypropionyloxy)ursa-9(11),12-dien-28-oic acid, which possesses activity as an anti-ulcer and anti-viral agent, pharmaceutically acceptable, non-toxic salts thereof, a method of preparing the same and compositions containing the same.Type: GrantFiled: July 25, 1983Date of Patent: July 23, 1985Assignee: I.S.F. SpaInventors: Gaetano Clavenna, Carlo Farina, Mario Pinza, Giorgio Pifferi
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Patent number: 4526779Abstract: A stable topical skin depigmenting composition having no irritant action to the skin which comprises an active ingredient a fatty acid ester of hydroquinone of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different, each being hydrogen or a straight or branched, saturated or unsaturated aliphatic hydrocarbon radical having 1 to 20 carbon atoms, provided that at least one of R.sub.1 and R.sub.2 is the hydrocarbon radical and one or more conventional ingredients suitable for a topical preparation. A method of depigmentation of the skin using the ester of the formula [I] is also disclosed.Type: GrantFiled: February 26, 1982Date of Patent: July 2, 1985Assignee: Sunstar Kabushi KaishaInventor: Akira Hashimoto