Patents Examined by E. C. Ward
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Patent number: 5232915Abstract: 9.alpha.-Hydroxy-19,11.beta.-bridged steroids of general formula I ##STR1## are described. The more detailed meaning of A, B, R.sup.1, R.sup.2, G, Z, R.sup.4 --Y and R.sup.4' --Y' follows from the description. The steroids of general formula I have antigestagen and/or antiglucocorticoidal action and can be used for the production of pharmaceutical agents.Type: GrantFiled: January 14, 1992Date of Patent: August 3, 1993Assignee: Schering AktiengesellschaftInventors: Eckhard Ottow, Gunter Neef, Rudolf Wiechert, Walter Elger, Sybille Beier, Karl-Heinrich Fritzemeier
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Patent number: 5232916Abstract: Compounds having the formula: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.Type: GrantFiled: October 28, 1991Date of Patent: August 3, 1993Assignee: Merck Frosst Canada, Inc.Inventors: Robert Zamboni, Petpiboon Prasit, Robert N. Young
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Patent number: 5229508Abstract: A process for the preparation of a copper phthalocyanine pigment, which comprises dry grinding crude copper phthalocyanine, treating the dry ground crude copper phthalocyanine with an aqueous solution of a mineral acid under such conditions of acid concentration and temperature as not to transform the .beta. form contained in the ground crude copper phthalocyanine into the .alpha. one to thereby carry out the pigmentation and removing the mineral acid from the resulting mixture.Type: GrantFiled: December 13, 1991Date of Patent: July 20, 1993Assignee: Toyo Ink Manufacturing Co., Inc.Inventors: Toshimitsu Ikegaya, Yusaku Ide, Tsuneo Kawamura, Michichika Hikosaka
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Patent number: 5227474Abstract: The present invention provides bifunctional chelating agents comprising a unique substrate reactive moiety incorporated into a carboxymethyl arm of a polyaminopolycarboxylate chelating framework capable of forming stable complexes with metal ions.Type: GrantFiled: May 28, 1991Date of Patent: July 13, 1993Assignee: Abbott LaboratoriesInventors: David K. Johnson, Steven J. Kline
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Patent number: 5227375Abstract: Novel aromatase inhibitors are disclosed for use in therapeutic preparations for treatment of estrogen-dependent diseases. The compounds are specified 7.alpha.-substituted androstanedione and androstenedione derivatives which show a strong inhibitory activity towards aromatase. The invention includes synthesis and pharmaceutical compositions of said compounds.Type: GrantFiled: February 8, 1990Date of Patent: July 13, 1993Assignee: Endorecherche, Inc.Inventors: Fernand Labrie, Yves Merand
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Patent number: 5225551Abstract: An imaging member comprised of a supporting substrate, a photogenerating layer comprised of a titanyl phthalocyanine of the type selected from the group consisting of Type IV, Type X, Type Z-1, and Type Z-2, prepared by the process which comprises dissolving a titanyl phthalocyanine in a solution of trifluoroacetic acid and methylene chloride; adding the resultant solution to a solvent or solvent mixture that will enable precipitation; and separating the product titanyl phthalocyanine from the solution followed by an optional washing, and a charge transport layer.Type: GrantFiled: October 5, 1992Date of Patent: July 6, 1993Assignee: Xerox CorporationInventors: James M. Duff, James D. Mayo, Cheng-Kuo Hsiao, Ah-Mee Hor, Terry L. Bluhm, Gordon K. Hamer, Peter M. Kazmaier
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Patent number: 5225402Abstract: Novel carbostyril derivatives of the formula: ##STR1## wherein R.sup.1 is H, NO.sub.2, alkoxy, alkoxycarbonyl, alkyl, halogen, optionally substituted amino, OH, CN, COOH, alkanoyloxy, hydrazinocarbonyl; q is 1 to 3, and R is a group of the formula ##STR2## [wherein R.sup.2 is H, alkoxycarbonyl, optionally substituted phenoxycarbonyl, phenylalkenyl-CO-, optionally substituted phenylalkanoyl, alkanoyl, alkenyl-CO-, optionally substituted phenyl--SO.sub.2 --, --CONR.sup.8 R.sup.9, optionally substituted heterocyclic group--CO--, naphthyl--CO--, thienylalkanoyl, tricyclo[3.3.1.1]alkanoyl, ##STR3## (R.sup.13 is OH, optionally substituted alkoxy, --NR.sup.32 R.sup.33, --O--A--(E).sub.l --NR.sup.4 R.sup.5, --(B).sub.l 'NR.sup.6 R.sup.7, etc.), n is 1 or 2, m is 0 or 1 to 3, R.sup.3 is alkyl, R.sup.10 is --(CO).sub.l --NR.sup.11 R.sup.Type: GrantFiled: September 18, 1991Date of Patent: July 6, 1993Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hidenori Ogawa, Hisashi Miyamoto, Kazumi Kondo, Hiroshi Yamashita, Kenji Nakaya, Michiaki Tominaga, Yoichi Yabuuchi
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Patent number: 5223494Abstract: Disclosed is a pharmaceutical composition for oral administration to control heme oxygenase comprising mettaloprotoporhyrins and mettalomesoporphyrins.Type: GrantFiled: September 21, 1990Date of Patent: June 29, 1993Assignee: The Rockefeller UniversityInventors: Attallah Kappas, Daniel W. Rosenberg, George S. Drummond
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Patent number: 5223492Abstract: This invention relates to the field of chemistry and more precisely to the field of medicinal Chemistry.It has specifically as subject matter the compounds of general formula I ##STR1## wherein R is a hydrogen, a lower alkyl radical a methoxymethyl, a tetrahydropyranyl or the acyl residue of an organic carboxylic.Type: GrantFiled: August 26, 1991Date of Patent: June 29, 1993Inventors: Nejib M. Nasraoui, Alain Piasco
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Patent number: 5219862Abstract: Compounds of formula I ##STR1## in which R.sup.2 means optionally substituted C.sub.1-7 alkyl, C.sub.2-7 alkenyl, CH.sub.2 --O--C.sub.1-4 alkyl or CH.sub.2 --S--C.sub.1-4 alkylR.sup.6 means C.sub.2-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-5 -cycloalkyl-C.sub.1-2 alkyl andR.sup.8 means CH.sub.2 --X, ##STR2## in which X stands for CN, OCH.sub.3, SCH.sub.3 or CONH.sub.2 and R.sup.1 stands for hydrogen, halogen, methyl or methoxy, and R.sup.3 and R.sup.4 each mean C.sub.1-4 alkyl or (CH.sub.2).sub.n --N(CH.sub.3).sub.2, in which n=1-4, and their acid addition salts, the process for their production, their use as pharmaceutical agents as well as intermediate compounds are described.Type: GrantFiled: December 21, 1990Date of Patent: June 15, 1993Assignee: Schering AktiengesellschaftInventors: Gerhard Sauer, Thomas Brumby, Helmut Wachtel, Jonathan Turner, Peter A. Loschmann
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Patent number: 5218109Abstract: Steroid compounds of the following general formulas (I), (II) and (III) are provided: ##STR1## In the above formulas, R.sup.1 and R.sup.2 each is a hydrogen atom or a hydroxyl-protecting group, R is a group of the formula --CH.sub.2 --X (in which X is a substituent such as a hydroxyl group), a carboxyl group or a protected carboxyl group, A.sup.1 is an aryl group, a lower alkyl group or an aralkyl group, and Z.sup.1, Z.sup.2, Z.sup.3 and Z.sup.4 each is a hydrogen atom, a hydroxyl group or a protected hydroxyl group.The above steroid compounds are useful as intermediates for the synthesis of vitamin D.sub.3 derivatives having a hydroxyl group at the 1.alpha.-position.Type: GrantFiled: March 5, 1990Date of Patent: June 8, 1993Assignee: Kuraray Co., Ltd.Inventors: Jiro Tsuji, Takashi Takahashi, Masao Tsuji, Naoshi Nakagawa, Tetsuo Takigawa
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Patent number: 5217977Abstract: The invention concerns a heterocyclic cycloalkane of the formula I ##STR1## wherein Q is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen atoms;A is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene;X is oxy, thio, sulphinyl, sulphonyl or imino;Ar is phenylene which may optionally bear one or two substituents or Ar is an optionally substituted 6-membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 is hydrogen, (1-6C)alkyl, (3-6C)alkenyl, (3-6C)alkynyl, cyano-(1-4C)alkyl or (2-4C)alkanoyl, or optionally substituted benzoyl; and R.sup.2 and R.sup.3 together form a (3-6C)alkylene group which, together with the carbon atom to which R.sup.2 and R.sup.3 are attached, defines a ring having 4 to 7 ring atoms, and which ring may bear one or two substituents;or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.Type: GrantFiled: November 15, 1991Date of Patent: June 8, 1993Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Graham C. Crawley, Jean-Marc M. M. Girodeau
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Patent number: 5214036Abstract: Green porphyrins (Gp), compounds important in photodynamic therapy, have been associated with lipocomplexes to reduce the required amount of photosensitizer through higher effective absorption and increased specificity. BPDs, especially in conjunction with the HDL fraction of plasma lipoproteins, has been shown to be particularly effective in this context. Pharmaceutical compositions in which these combinations are the active ingredients for use in diagnosis and treatment of tumors are also disclosed.Type: GrantFiled: March 8, 1990Date of Patent: May 25, 1993Assignee: University of British ColumbiaInventors: Beth A. Allison, Anna M. Richter, P. Haydn Pritchard, Julia G. Levy
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Patent number: 5214171Abstract: Process for fractionating phosphatide mixtures into two or more fractions which are enriched in one or more of phosphatidyl choline (PC), phosphatidyl ethanolamine (PE), phosphatidyl inositol (PI) and phosphatidic acid (PA) by carrying out extraction steps using alcoholic solvent in which the solubilities of PC, PE and PA are controlled by suitably adjusting the acidity of the solvent, the pH being adjusted to above 8 for solubilizing PC and PE and to below 5 for solubilizing PA. PI is substantially insoluble in the solvent used in the process and thus is mainly recovered in the extraction residue. Further parameters influencing the solubility of the components of the phosphatide mixtures to be fractionated are water content of the alcoholic solvent, temperature and choice of bases and acids for adjusting the pH. For further separating fractions rich in PC and PE di- or trivalent metal salt solutions are used.Type: GrantFiled: November 19, 1991Date of Patent: May 25, 1993Assignee: N.V. Vandemoortele InternationalInventors: Albert J. Dijkstra, Jan De Kock
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Patent number: 5212158Abstract: The L-proline derivatives of the invention correspond to the Formula I: ##STR1## in which R.sub.1 corresponds to the Formula II: ##STR2## in which R is a carbonyl group, an acyl group --Y--CO-- or an oxy-acyl group --O--Y--CO--, Y being an alkyl or an alkenyl chain, Z being one or more hydrogen atoms, or one or more substituents chosen from among halogen atoms, CF.sub.3, alkyl or alkoxy groups and an alkylenedioxy group in the case of two neighbouring substituents,R.sub.2 is --NH.sub.2, --OH, or a derivative of these groups,A.sub.1 and A.sub.2 are amino acid residues andB.sub.1 and B.sub.2 represents a hydrogen atom or a methyl group, and the pharmacologically acceptable salts of these derivatives.These derivatives are useful particularly as the active principles of medicines possessing, in particular, a nootropic action.Type: GrantFiled: November 3, 1988Date of Patent: May 18, 1993Assignee: Inorgan SA Recherche & Developpement Pharmaceutiques, CASInventor: Pierre-Yves Fiez Vandai
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Patent number: 5212179Abstract: The invention concerns the preparation of compounds of formula ##STR1## and acid addition and quaternary ammonium salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula ##STR2## in which Q is O, S, --CR.sup.7 .dbd.CR.sup.8 --, --N.dbd.CR.sup.8 -- and --N.dbd.N--; R.sup.4, R.sup.5 and R.sup.6 ; and R.sup.7 and R.sup.8 when present, each represent hydrogen or a substituent selected from lower alkyl, lower alkenyl, lower alkoxy, NO.sub.2, NH.sub.2, haloloweralkyl, hydroxyloweralkyl, aminoloweralkyl, substituted amino, halogen, loweralkoxycarbonyl, cyano, CONH.sub.2 and hydroxy; and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.Type: GrantFiled: October 25, 1990Date of Patent: May 18, 1993Assignee: John Wyeth and Brother LimitedInventors: John L. Archibald, Terence J. Ward
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Patent number: 5210301Abstract: Novel squarium compounds which have a flat photosensitivity in the wide range from visible ray region to the near infrared ray region as a charge generator and which can be prepared by reacting squaric acid and an aniline derivative, and electrophotographic photoreceptors containing the squarium compounds are disclosed.Type: GrantFiled: August 17, 1988Date of Patent: May 11, 1993Assignee: Fuji Xerox Co., Ltd.Inventors: Satoshi Saeki, Seki Kin, Kaoru Torikoshi, Hiroyuki Tanaka, Lyong S. Pu
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Patent number: 5206231Abstract: Novel 2,5-benzodiazocines of formulas II and IV, pharmaceutical compositions containing them, processes for preparing them and methods of treating cardiac arrhythmias in mammals utilizing them.Type: GrantFiled: September 10, 1991Date of Patent: April 27, 1993Assignee: Sterling Drug Inc.Inventor: Robert E. Johnson
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Patent number: 5206233Abstract: Substituted thiazepines are described as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as antipsychotic and antidepressant agents as well as for treating cerebral ischemia or cerebral infarction.Type: GrantFiled: August 27, 1991Date of Patent: April 27, 1993Assignee: Warner-Lambert CompanyInventors: William J. Smith, III, Lawrence D. Wise, David J. Wustrow
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Patent number: 5202319Abstract: There are disclosed various compounds of the formula below, ##STR1## where n is 1 or 2;m is 1 or 2;each X is independently hydrogen or loweralkoxy;Y is hydrogen, halogen or trifluoromethyl;R.sub.1 is hydrogen, loweralkyl, arylloweralkyl, heteroarylloweralkyl, pyridinyl, loweralkylcarbonyl, arylloweralkylcarbonyl, heteroarylloweralkylcarbonyl, trifluoromethylcarbonyl or arylcarbonyl; andR.sub.2 is hydrogen, loweralkyl, loweralkoxycarbonyl, aminoloweralkylcarbonyl, loweralkylaminoloweralkylcarbonyl or diloweralkylaminoloweralkylcarbonyl;which are useful as modulators of neurotransmitter function such as serotonergic and adrenergic, and as such are useful as antidepressants and for the treatment of personality disorders such as obsessive compulsive disorders.Type: GrantFiled: September 23, 1991Date of Patent: April 13, 1993Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Joseph T. Klein