Patents Examined by Elbert L. Roberts
  • Patent number: 4543351
    Abstract: A spironolactone containing composition for topical use in the form of a cream active in combatting acne and causing only skin absorption and therefore devoid of any undesired systemic effect.
    Type: Grant
    Filed: March 27, 1984
    Date of Patent: September 24, 1985
    Assignee: Schiapparelli Farmaceutici S.p.A.
    Inventor: Michele Messina
  • Patent number: 4542128
    Abstract: 17.alpha.-Pregn-4-ene-3-oxo-21-carboxylic acid esters of Formula I ##STR1## wherein C.sub.1 C.sub.2 is a CC single or C.dbd.C double bond,--A--B--is ##STR2## --C--D--is ##STR3## and R is an alkyl or alkenyl residue of up to 6 carbon atoms,in addition to antialdosterone activity, exhibit greatly reduced antiandrogenic and progestational side effects.
    Type: Grant
    Filed: July 22, 1983
    Date of Patent: September 17, 1985
    Assignee: Schering Aktiengesellschaft
    Inventors: Dieter Bittler, Henry Laurent, Klaus Nickisch, Rudolf Weichert, Jorge Casals-Stenzel
  • Patent number: 4541956
    Abstract: A method and composition for the preparation of steroid compounds by the reaction of various organotin compounds with steroids. Said compounds retard the growth of malignant tumors and, in some cases, completely destroy the tumor.
    Type: Grant
    Filed: July 28, 1983
    Date of Patent: September 17, 1985
    Assignee: Unique Technologies, Inc.
    Inventors: Nathan F. Cardarelli, Sebastian V. Kanakkanatt
  • Patent number: 4542024
    Abstract: New 15,16-methylene-17.alpha.-pregna-4,6-diene-21-carboxylic acid salts of formula I ##STR1## wherein R.sup.1 and R.sup.2 each alone is hydrogen or together they form an additional CC bond or a methylene group,M is an alkali metal,and the methylene group in the 15,16 position is in the .alpha. or .beta. position, in addition to having a strong antialdosterone effect, have reduced antiandrogenic and progestogenic side effects.
    Type: Grant
    Filed: July 13, 1984
    Date of Patent: September 17, 1985
    Assignee: Schering Aktiengesellschaft
    Inventors: Klaus Nickisch, Dieter Bittler, Henry Laurent, Rudolf Wiechert, Wolfgang Losert
  • Patent number: 4542025
    Abstract: An anti-inflammatory agent containing microparticle composition prepared by a process, comprising (a) dissolving or dispersing an anti-inflammatory agent in a solvent and dissolving a biocompatible and biodegradable wall forming material in said solvent; (b) dispersing said solvent containing said anti-inflammatory agent and wall forming material in a continuous phase processing medium; (c) evaporating a portion of said solvent from said dispersion of step (b), thereby forming microparticles containing said anti-inflammatory agent in the suspension; and (d) extracting the remainder of the solvent from said microcapsules.
    Type: Grant
    Filed: April 30, 1984
    Date of Patent: September 17, 1985
    Assignees: The Stolle Research and Development Corporation, Southern Research Institute
    Inventors: Thomas R. Tice, Danny H. Lewis, Donald R. Cowsar, Lee R. Beck
  • Patent number: 4542129
    Abstract: Topical formulations for treating dry skin with dehydroepiandrosterone (DHEA) may contain a keratolytic agent to counteract the formation of acne-like skin lesions without diminishing the effectiveness of DHEA in increasing sebum production. The keratolytic agent may be a hydroxybenzoic acid, alpha-hydroxycarboxylic acid or urea, with salicylic acid being preferred. The DHEA and keratolytic agent may be formulated in a non-toxic, dermatologically acceptable vehicle including tinctures, creams, ointments, gels and lotions.
    Type: Grant
    Filed: January 24, 1985
    Date of Patent: September 17, 1985
    Inventor: Norman Orentreich
  • Patent number: 4540686
    Abstract: Novel 3-keto-19-nor-.DELTA..sup.4,9 -steroids of the formula ##STR1## possessing a remarkable antiglucocorticoidal activity.
    Type: Grant
    Filed: June 8, 1984
    Date of Patent: September 10, 1985
    Assignee: Roussel Uclaf
    Inventors: Daniel Philibert, Jean G. Teutsch, Germain Costerousse, Roger Deraedt
  • Patent number: 4539153
    Abstract: The invention relates to a method of preparing 1 .alpha.-hydroxyvitamin D or 1 .alpha.-hydroxy-previtamin D compounds by hydroxylating the 1 .alpha.-position of an adduct of a previtamin D compound with a suitable dienophile, in which adduct optionally present hydroxy group or hydroxy groups is or are protected, if desired, and after removal of the protecting group or groups, isolating the 1 .alpha.-hydroxyvitamin D or 1 .alpha.-hydroxy-previtamin D compound.The invention also relates to 1 .alpha.-hydroxy-previtamin D compounds.The invention further relates to an adduct of a previtamin D or tachysterol compound with a dienophile of the general formula ##STR1## in which A' and B' are equal and represent methoxy groups or ethoxy groups, or in which A' and B' together constitute a phenylimino or o-phenylene group.
    Type: Grant
    Filed: July 31, 1984
    Date of Patent: September 3, 1985
    Assignee: Duphar International Research B.V.
    Inventors: Maurits Vandewalle, Luc J. Vanmaele, Pierre J. De Clercq, Sebastianus J. Halkes, Wilhelmus R. M. Overbeek
  • Patent number: 4539200
    Abstract: Method and composition for cleansing wounds and skin burns or lesions by application of particles of cross-linked polymers of acrylamide, methacrylamide, ethacrylamide, and N-hydrocarbon substituted derivatives thereof.
    Type: Grant
    Filed: November 4, 1983
    Date of Patent: September 3, 1985
    Assignee: The Kendall Company
    Inventor: Alan Quarfoot
  • Patent number: 4537722
    Abstract: This invention relates to an improved steroid ester synthesis in which carbodiimides and catalytic amounts of 4-(tertiary amino)-pyridines, in combination with acid catalysts, are used as condensing agents, resulting in pure, non discolored compounds in high yields.
    Type: Grant
    Filed: May 29, 1984
    Date of Patent: August 27, 1985
    Assignee: Ab Leo
    Inventors: Anders R. Stamvik, Sten K. Kristensson, Karl-Erik Lundvall
  • Patent number: 4537776
    Abstract: Topical pharmaceutical compositions comprising a pharmaceutically-active agent and a novel, penetration-enhancing vehicle or carrier are disclosed. The vehicle or carrier comprises a binary combination of N-(2-Hydroxyethyl) pyrrolidone and a "cell-envelope disordering compound". The compositions provide marked transepidermal and percutaneous delivery of the active selected. A method of treating certain pathologies and conditions responsive to the selected active, systemically or locally, is also disclosed.
    Type: Grant
    Filed: June 21, 1983
    Date of Patent: August 27, 1985
    Assignee: The Procter & Gamble Company
    Inventor: Eugene R. Cooper
  • Patent number: 4537898
    Abstract: A rapidly absorbable liquid formulation of a dihydropyridine comprising, by weight, about 0.5 to 10 parts of a dihydropyridine of the formula ##STR1## in which R.sub.1 is C.sub.1 -C.sub.4 -alkyl, optionally substituted by C.sub.2 -C.sub.3 -alkoxy,R.sub.2 is C.sub.1 -C.sub.10 -alkyl, optionally substituted by C.sub.1 -C.sub.3 -alkoxy, trifluoromethyl or N-methyl-N-benzylamino,R.sub.3 is C.sub.1 -C.sub.4 -alkyl, cyano or hydroxymethyl, andX is 2- or 3-nitro, 2,3-dichloro or 2,3.dbd.N--O--N.dbd.,20 to 60 parts of a solubilizing agent and 80 to 40 parts of a diluent.
    Type: Grant
    Filed: February 13, 1984
    Date of Patent: August 27, 1985
    Assignee: Bayer Aktiengesellschaft
    Inventors: Dieter Hoff, Klaus-Dieter Ramsch
  • Patent number: 4536401
    Abstract: Compounds of the formula I ##STR1## wherein R.sub.1 is ##STR2## wherein R.sup.I and R.sup.II each independently is alkyl of 1-4 carbon atoms, or R.sup.I and R.sup.II together with the connecting N-atom form a 5- or 6-membered heterocyclic ring whose remaining atoms are all C-atoms, or which also includes and additional N-atom, an additional O or S atom or a combination thereof; ##STR3## wherein R.sup.I and R.sup.II are as defined above; --SR.sup.III, wherein R.sup.III is methyl, ethyl or phenyl; or--OR.sup.IV, wherein R.sup.IV is methyl, ethyl, propyl, methoxymethyl, allyl, or .beta.-dimethylaminoethyl;R.sub.2 is hydrogen, methyl, or ethyl; ##STR4## wherein the wavy lines mean that the substituent is in the .alpha.- or .beta.-position, and ##STR5## M is Na, K or Li; and R.sup.V, R.sup.VI, R.sup.VII and R.sup.VIII each independently is alkyl of 1-4 carbon atoms, have valuable pharmacological properties, e.g., a combination of antiprogestational and antimineralocorticordal effects.
    Type: Grant
    Filed: February 21, 1984
    Date of Patent: August 20, 1985
    Assignee: Schering Aktiengesellschaft
    Inventors: Guenter Neef, Gerhard Sauer, Rudolf Wiechert, Helmut Hofmeister, Ralph Rohde, Klaus Annen, Henry Laurent, Sybille Beier, Wolfgang Losert, Walter Elger, David Henderson
  • Patent number: 4536519
    Abstract: Disclosed herein is an emulsifying agent comprising (a) a partially or completely neutralized product, with a basic substance, of a phosphoric acid ester which contains a phosphoric acid monoester represented by the general formula (I) and a phosphoric acid diester represented by the general formula (II) from 100:0 to 70:30 molar ratio: ##STR1## wherein R.sub.1 and R.sub.4 represent individually a linear alkyl group or a linear alkenyl group of 10-22 carbon atoms or a branched alkyl group of 12-24 carbon atoms, R.sub.2 and R.sub.3 represent individually an ethylene group or a propylene group, and m and n represent individually a number of 0-30, and (b) a nonionic surfactant with HLB of 6 or less. Emulsified cosmetics comprising (a) the neutralized product of the phosphoric acid ester, (b) a nonionic surfactant with HLB of 6 or less, (c) an oily substrate, and (d) water is also disclosed.
    Type: Grant
    Filed: June 9, 1982
    Date of Patent: August 20, 1985
    Assignee: Kao Soap Co., Ltd.
    Inventors: Toshiyuki Suzuki, Tohru Nakamura, Hisao Tsutsumi
  • Patent number: 4534976
    Abstract: Described for use as a key ingredient in an animal control composition and more particularly in an animal repellent composition, is the genus of steroids defined according to the structure: ##STR1## wherein X completes a substituted cyclopentyl moiety and is one of the moieties: ##STR2## wherein Y represents methylene, carbinol or keto; and wherein Z completes a substituted cyclohexyl moiety and is one of the moieties:hydroxycyclohexyl;ketocyclohexyl;ketocyclohexenyl;hydroxyphenyl;cyclohexenyl; orbicyclohexyland wherein the dashed line represents a carbon-carbon single bond or a carbon-carbon double bond.Also described are animal control articles consisting of one or more members of the above mentioned steroid genus and imbedded in a compatible polymer.
    Type: Grant
    Filed: August 1, 1983
    Date of Patent: August 13, 1985
    Assignee: International Flavors & Fragrances Inc.
    Inventors: Helge Hansen, Borje Nystrom, Eyvin Torneng
  • Patent number: 4530795
    Abstract: This invention discloses a general process for the production of corticoids from respective steroid-type compounds having a double bond from C-16 to C-17. The invention provides a viable alternative synthesis of 17.alpha.-hydroxy-progesterones and like corticoids.
    Type: Grant
    Filed: February 27, 1984
    Date of Patent: July 23, 1985
    Assignee: The Upjohn Company
    Inventor: Joel E. Huber
  • Patent number: 4530839
    Abstract: A method of contraception in which an estrogen and a progestogen are administered daily for 21 days, the first seven days at a low contraceptively effective daily dose, the next 7 days at a daily progestogen dose about 1.5-2 times that of the first 7 days, and the next 7 days at a daily progestogen dose of 2-2.5 times that of the first 7 days, provided that the dosage of the estrogen is maintained at a constant level for the entire 21 days.
    Type: Grant
    Filed: September 26, 1983
    Date of Patent: July 23, 1985
    Assignee: Ortho Pharmaceutical Corporation
    Inventor: Samuel A. Pasquale
  • Patent number: 4530840
    Abstract: An anti-inflammatory agent containing microparticle composition prepared by a process, comprising (a) dissolving or dispersing an anti-inflammatory agent in a solvent and dissolving a biocompatible and biodegradable wall forming material in said solvent; (b) dispersing said solvent containing said anti-inflammatory agent and wall forming material in a continuous phase processing medium; (c) evaporating a portion of said solvent from said dispersion of step (b), thereby forming microparticles containing said anti-inflammatory agent in the suspension; and (d) extracting the remainder of the solvent from said microcapsules.
    Type: Grant
    Filed: July 29, 1982
    Date of Patent: July 23, 1985
    Assignees: The Stolle Research and Development Corporation, Southern Research Institute
    Inventors: Thomas R. Tice, Danny H. Lewis, Donald R. Cowsar, Lee R. Beck
  • Patent number: 4529548
    Abstract: Antiinflammatory activity is exhibited by steroids having the formula ##STR1## or the 1,2-dehydro derivative thereof, wherein R.sub.1 is alkyl, alkanoyloxyalkyl, arylcarbonyloxyalkyl, alkenyl, alkynyl, cycloalkyl, aryl or arylalkyl;R.sub.2 is hydrogen, hydroxy, alkoxy, aryloxy, methylene, alkylthio, arylthio, alkanoyl, alkanoyloxy, or halogen;R.sub.3 is hydrogen, methyl, hydroxy or halogen; andn is 0, 1 or 2.
    Type: Grant
    Filed: May 7, 1984
    Date of Patent: July 16, 1985
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Ravi K. Varma, Rudiger D. Haugwitz
  • Patent number: 4529547
    Abstract: Topical antiinflammatory activity is by steroids having the formula ##STR1## and the 1,2-dehydro derivatives thereof wherein R.sub.1 and R.sub.2 are the same or different and each is alkyl, aryl, arylalkyl or cycloalkyl;R.sub.3 is carbonyl or .beta.-hydroxymethylene;R.sub.4 is hydrogen or halogen; andR.sub.5 is hydrogen, methyl or fluorine.
    Type: Grant
    Filed: June 20, 1984
    Date of Patent: July 16, 1985
    Assignee: E.R. Squibb & Sons, Inc.
    Inventor: Ravi K. Varma