Patents Examined by Joseph A. Lipovsky
  • Patent number: 4892730
    Abstract: Solid dihydropyridines, e.g. nifedipine and nimodipine preparations having a maximum standard deviation of the active compound content of 3% contain 1 part by weight of nifedipine, 2 to 6 parts by weight of PVP with a mean molecular weight of 15,000 to 50,000, 3.5 to 15 parts by weight of cellulose, 0.25 to 4 parts by weight of starch and 0.5 to 4 parts by weight of cross-linked insoluble PVPP, and, if appropriate, one or more further pharmaceutical auxiliaries and excipients. These preparations show a good release of dihydropyridine with good content uniformity.
    Type: Grant
    Filed: September 20, 1988
    Date of Patent: January 9, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventor: Ahmed Hegasy
  • Patent number: 4892867
    Abstract: 17.alpha.-Alkyl steroids of the formula ##STR1## wherein R.sub.1 is hydrogen, acyl, alkyl, alkenyl, alkyl or alkenyl interrupted by an oxygen atom, cyclopentyl, or tetrahydropyranyl,R.sub.2 is alkyl or alkenyl of 2-6 carbon atoms,X is oxygen or the grouping H(OR.sub.3) wherein R.sub.3 is hydrogen, acyl, alkyl, alkenyl, alkyl or alkenyl interrupted by an oxygen atom, cyclopentyl, or tetrahydropyranyl, upon topical application, display antiandrogenic properties and can be utilized for the treatment of acne, seborrhea, alopecia and hirsutism.
    Type: Grant
    Filed: October 14, 1986
    Date of Patent: January 9, 1990
    Assignee: Schering Aktiengesellschaft
    Inventors: Rudolf Wiechert, Dieter Bittler, Annerose Schleusener, Manfred Albring
  • Patent number: 4891365
    Abstract: 17-Substituted estradienes and estratrienes of Formula I ##STR1## wherein ##STR2## R is alkyl, alkenyl or cycloalkyl of up to 5 carbon atoms if ##STR3## R is hydrogen, alkyl, alkenyl or cycloalkyl of up to 5 carbon atoms if ##STR4## is a CC-single or CC-double bond, exhibit, an aldosterone-antagonistic activity and a strong gestagen potency.
    Type: Grant
    Filed: July 2, 1987
    Date of Patent: January 2, 1990
    Assignee: Schering Aktiengesellschaft
    Inventors: Rudolf Wiechert, Sybille Beier, Walter Elger, Klaus Annen, Klaus Nickisch, Henry Laurent
  • Patent number: 4891366
    Abstract: 2.beta.,16.beta.-diamino-3.alpha.,17.alpha.-oxygenated androstanes having one quaternized group, process for the preparation of these compounds and pharmaceutical compositions comprising such compounds as the active ingredient. The aforementioned compounds are favourable neuro-muscular blocking agents.
    Type: Grant
    Filed: April 20, 1988
    Date of Patent: January 2, 1990
    Assignee: Akzo N.V.
    Inventors: Thomas Sleigh, David S. Savage, Robert Taylor
  • Patent number: 4891368
    Abstract: Antigestagens are useful for softening the nonpregnant cervix.
    Type: Grant
    Filed: December 21, 1988
    Date of Patent: January 2, 1990
    Assignee: Schering Aktiengesellschaft
    Inventors: Krzysztof Chwalisz, Sybille Beier, Angelika Esch, Walter Elger
  • Patent number: 4891364
    Abstract: Vitamin D derivatives of the formula ##STR1## where R.sub.1, R.sub.2 and R.sub.3 which may be the same or different each represents a hydrogen atom or a hydroxyl group; X is an oxygen atom, the group of the formula OR.sub.4 (where R.sub.4 is either a hydrogen atom or a lower alkyl having 4 to 6 carbon atoms that may or may not be substituted by a hydroxyl group), or the group of the formula=N-OR.sub.5 (where R.sub.5 is either a hydrogen atom or a lower alkyl group having 1 to 5 carbon atoms that may or may not be substituted by a hydroxyl group, an amino group or a lower alkylamino group having 1 to 3 carbon atoms), provided that the carbon atom at 20-position is linked to X by a single bond when X is the group of the formula OR.sub.4, and by a double bond in other cases, and a process for preparing the derivatives are disclosed.
    Type: Grant
    Filed: June 13, 1988
    Date of Patent: January 2, 1990
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Noboru Kubodera, Katsuhito Miyamoto, Kiyoshige Ochi, Isao Matsunaga, Eigoro Murayama
  • Patent number: 4888331
    Abstract: An agent containing at least one compound having antiprogestational activity and at least one compound having anti-estrogenic activity is disclosed. The agent is suitable for the induction of labor, termination of preganancy, as well as for the treatment of gynecological disorders.
    Type: Grant
    Filed: October 3, 1988
    Date of Patent: December 19, 1989
    Assignee: Schering Aktiengesellschaft
    Inventors: Walter Elger, Sybille Beier, Marianne Fahnrich, Beate Kosub, Krzysztof Chwalisz, Syed H. Hasan
  • Patent number: 4886909
    Abstract: A novel aromatic amine terminated trifunctional polyoxyalkylene urea which is useful as an epoxy curing agent is disclosed and is prepared in a two step process comprising reacting a triamine or a triol with a diisocyanate to form an intermediate product and subsequently reacting the intermediate with a diprimary amine in the presence of an alcohol solvent.
    Type: Grant
    Filed: July 22, 1988
    Date of Patent: December 12, 1989
    Assignee: Texaco Chemical Company
    Inventors: Jiang-Jen Lin, George P. Speranza
  • Patent number: 4885289
    Abstract: The rate and character of androgen-stimulated beard hair growth in intact, sexually mature males is altered by the topical application out of a dermatologically acceptable carrier of an antiandrogen material. In a preferred practice of the invention, compositions containing both a steroid 5-alpha-reductase inhibitor and a cytoplasmic androgen receptor binding agent are employed.
    Type: Grant
    Filed: December 11, 1985
    Date of Patent: December 5, 1989
    Inventors: Miklos M. Breuer, Edwin G. Kaszynski, Douglas Shander, Vera R. Usdin, Hermes van der Lee
  • Patent number: 4885280
    Abstract: The invention relates to androstane-17-carboxylic acid esters, represented by general formula (I): ##STR1## wherein R.sub.1 represents a lower alkyl group containing 1 to 4 carbon atoms, a lower alkyl group containing 2 to 4 carbon atoms substituted by an amino group, or an aralkyl group from 6 to 12 carbon atoms, R.sub.2 and R.sub.3, which may be the same or different, represent a hydrogen atom or a lower alkyl group containing 1 to 4 carbon atoms, R.sub.4 represents a hydrogen atom, a hydroxy group or an acetoxy group, R.sub.5 represents a hydroxy or acetoxy group, or R.sub.4 and R.sub.5 represent together a divalent alkylenedioxy group, R.sub.6 represents a hydroxy group, a methoxy group, or an acetoxy group, R.sub.7 represents a methyl group or a hydroxymethyl group, R.sub.8 represents an hydrogen atom or a hydroxy group and ##STR2## represents either a ##STR3## group or a ##STR4## carbon atom having the double linkage in the 4- or 5-position of the steroid nucleus.
    Type: Grant
    Filed: September 30, 1988
    Date of Patent: December 5, 1989
    Assignee: Norwich Eaton Pharmaceuticals, Inc.
    Inventors: Francois-Xavier Jarreau, Jean-Jacques Koenig
  • Patent number: 4883658
    Abstract: A synergistic combination of an aqueous solution of a partially hydrolyzed poly(vinyl acetate) and a fully hydrolyzed poly(vinyl acetate), i.e. poly(vinyl alcohol), exhibiting a low surface tension at the water-air interface, while forming a completely wettable absorbed layer over hydrophobic solids. The combination is used as part of an ophthalmic solution including a hydrophilic low viscosity polymer, poly(N-glucose) or poly(N-vinyl pyrrolidone) with higher than normal oncotic pressure in a physiologically compatible electrolytic solution base. The formulation is effective in treating the two major underlying causes of the dry eye syndrome; ocular surface disorder and tear film abnormalities resulting in tear film instability. It can also be effective as an aqueous vehicle for topically used ophthalmic drugs or nutrients.
    Type: Grant
    Filed: May 16, 1988
    Date of Patent: November 28, 1989
    Inventor: Frank J. Holly
  • Patent number: 4882144
    Abstract: Solid dihydropyridines, e.g. nifedipine and nimodipine preparations having a maximum standard deviation of the active compound content of 3% contain 1 part by weight of nifedipine, 2 to 6 parts by weight of PVP with a mean molecular weight of 15,000 to 50,000, 3.5 to 15 parts by weight of cellulose, 0.25 to 4 parts by weight of starch and 0.5 to 4 parts by weight of cross-linked insoluble PVPP, and, if appropriate, one or more further pharmaceutical auxiliaries and excipients. These preparations show a good release of dihydropyridine with good content uniformity.
    Type: Grant
    Filed: May 19, 1986
    Date of Patent: November 21, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventor: Ahmed Hegasy
  • Patent number: 4882319
    Abstract: Invented are phosphonic acid substituted analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase, including using these compounds to reduce or maintain prostate size. Also invented are intermediates used in preparing these compounds.
    Type: Grant
    Filed: December 23, 1988
    Date of Patent: November 21, 1989
    Assignee: SmithKline Beckman Corporation
    Inventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
  • Patent number: 4882322
    Abstract: The present invention is directed to a group of compounds which are 3.beta.,17.beta.-hydroxy steriods, and related steroidal structures. These compounds are armatase inhibitors, and thus, regulate or inhibit the conversion of androgens to estrogens. These compounds may be utilized to treat conditions potentiated by the presence of estrogens. These compounds exhibit a slower onset of action and a longer half life relative to the 10-(2-alkynyl) steroidal aromatase inhibitors disclosed in U.S. Pat. No. 4,322,416.
    Type: Grant
    Filed: October 27, 1988
    Date of Patent: November 21, 1989
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: J. O'Neal Johnston, Gene W. Holbert
  • Patent number: 4880740
    Abstract: A process is provided for reducing iron ore by treatment with microorganisms which comprises forming an aqueous mixture of iron ore, microorganisms operable for reducing the ferric iron of the iron ore to ferrous iron, and a substrate operable as an energy source for the microbial reduction; and maintaining the aqueous mixture for a period of time and under conditions operable to effect the reduction of the ore. Preferably the microorganism is Pseudomonas sp. 200 and the reduction conducted anaerobically with a domestic wastewater as the substrate. An aqueous solution containing soluble ferrous iron can be separated from the reacted mixture, treated with a base to precipitate ferrous hydroxide which can then be recovered as a concentrated slurry.
    Type: Grant
    Filed: October 17, 1984
    Date of Patent: November 14, 1989
    Assignee: California Institute of Technology
    Inventors: Michael R. Hoffmann, Robert G. Arnold, Gregory Stephanopoulos
  • Patent number: 4880921
    Abstract: The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are:(a) compounds of the formula[D--DHC] (I)wherein [D] is a centrally acting drug species, and [DHC] is the reduced, biooxidizable, blood-brain barrier penetrating lipoidal form of a dihydropyridine .revreaction. pyridinium salt redox carrier, with the proviso that when [DHC] is ##STR1## wherein R is lower alkyl or benzyl and [D] is a drug species containing a single NH.sub.2 or OH functional group, the single OH group when present being a primary or secondary OH group, said drug species being linked directly through said NH.sub.
    Type: Grant
    Filed: July 20, 1987
    Date of Patent: November 14, 1989
    Assignee: University of Florida
    Inventor: Nicholas S. Bodor
  • Patent number: 4879106
    Abstract: A composition for preparing a medicament for topical treatment of paradentium diseases, said composition comprising the ammonium salt of sulfoichthyolic acid, zinc oxide, titanium dioxide and fluid extract of Hamamelis in a pharmaceutically acceptable carrier. Said composition is useful especially for treatment of gingivitis and alveolar pyorrhea.
    Type: Grant
    Filed: January 27, 1987
    Date of Patent: November 7, 1989
    Inventor: Giorgio Voli
  • Patent number: 4876250
    Abstract: Angiostatic steroids for use in controlling ocular hypertension are disclosed. Pharmaceutical composition of the angiostatic steroids and methods for their use in treating ocular hypertension, including controlling the ocular hypertension associated with primary open angle glaucoma, are disclosed.
    Type: Grant
    Filed: October 31, 1988
    Date of Patent: October 24, 1989
    Assignee: Alcon Laboratories, Inc.
    Inventor: Abbot F. Clark
  • Patent number: 4876045
    Abstract: The invention relates to a new process for the preparation of known aromatase inhibitors of the following formula ##STR1## wherein each of R.sub.1 and R.sub.3, independently, is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.2 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl andR.sub.4 is hydrogen or fluorine; the process comprising subjecting to Mannich reaction a compound of formula ##STR2## wherein R.sub.1,R.sub.2,R.sub.3 and R.sub.4 are as defined above, and then oxidizing the respective 6-methylene derivative thus obtained by methods known per se.
    Type: Grant
    Filed: September 12, 1988
    Date of Patent: October 24, 1989
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Antonio Longo, Paolo Lombardi
  • Patent number: 4874855
    Abstract: Disclosed are steroid compounds represented by general formula (I) ##STR1## wherein X and W together as >W-X represent a carbonyl group (>C.dbd.O) or a hydroxymethylene group (>CH(OH)), the hydroxy moiety of the hydroxymethylene group being of .beta.-arrangement, and OR.sup.1 and OR.sup.2 independently represent an ester residue, and Y and Z together as --Y--Z-- represent a --(PpSe)CH--CH.sub.2 -- group where Pp represent a phenyl group or a 2-pyridyl group, or Y and Z each represent an ethenylene group or a 1-bromoethylene group.Also disclosed is a process of preparing the compound (I) includes reacting 6.beta., 9.alpha.-difluoro-5.alpha.,17.alpha.,21-trihydroxypregna-3,11,20-trione-17 ,21-diesters or 6.beta.,9.alpha.-difluoro-5.alpha.,11.beta.,17.alpha.
    Type: Grant
    Filed: May 3, 1988
    Date of Patent: October 17, 1989
    Assignee: Dainippon Ink and Chemicals, Inc.
    Inventors: Hidetsugu Takagaki, Masayoshi Abe, Michihiro Watanabe, Kazuyuki Takeuchi, Shigenori Nakanishi, Yuuko Nakata, Keiji Yamazaki