Patents Examined by Elbert L. Roberts
  • Patent number: 4588530
    Abstract: Derivatives of prednisolone of the formula ##STR1## wherein CR.sub.1 is C.dbd.O, .alpha.-HCOH, .beta.-HCOH, or a mixture of .alpha.-HCOH and .beta.-HCOH CR.sub.2 is HC(OH) OR.sub.6 or HCO when CR.sub.1 is C.dbd.O;CR.sub.2 is COOR.sub.3 or CONHR.sub.4 when CR.sub.1 is .alpha.-HCOH, .beta.-HCOH, or a mixture of .alpha.-HCOH and .beta.-HCOH:R.sub.3 is alkyl of 1-5 carbon atoms;R.sub.4 is alkyl of 1-5 carbon atoms, benzyl, or phenethyl;R.sub.5 is hydrogen, acetyl, or benzoyl;R.sub.6 is alkyl of 1-5 carbon atoms;R.sub.7 is .alpha.- or .beta.-position of hydrogen, hydroxyl, methyl, acetate esters of 1-5 carbon atoms, or alkoxy of 1-5 carbon atoms; andX and Y are hydrogen, halogen or methyl;and process for preparing these compounds. The compounds are useful as anti-inflammatory agents which have reduced side effects.
    Type: Grant
    Filed: June 9, 1983
    Date of Patent: May 13, 1986
    Assignee: Florida Agricultural and Mechanical University
    Inventor: Henry J. Lee
  • Patent number: 4587235
    Abstract: Androstane derivatives of Formula I ##STR1## wherein is a single bond or a double bond,R.sub.1 is methyl or ethyl,R.sub.2 is hydrogen or alkyl of 1-8 carbon atoms,--X-- is --(CH.sub.2).sub.n --, --CH.dbd.CH(CH.sub.2).sub.m --, or --C.tbd.C--(CH.sub.2).sub.m -- wherein n is 2 to 6 and m is 1 to 4,--A--B-- is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --CCl.dbd.CH--, ##STR2## --U--V< is --CH.sub.2 --CH<, --CH.dbd.C<, --C(OH).dbd.C<, or --CCl.dbd.C<, and--W--Y-- is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --C(CH.sub.3).sub.2 --, or ##STR3## with the proviso that the compound is not 17.alpha.-(3-acetoxypropyl)-17.beta.-hydroxy-4,6-androstadien-3-one, are pharmacologically efficacious compounds, e.g., are sebum suppressive.
    Type: Grant
    Filed: June 27, 1984
    Date of Patent: May 6, 1986
    Assignee: Schering Aktiengesellschaft
    Inventors: Dieter Bittler, Henry Laurent, Klaus Nickisch, Rudolf Wiechert
  • Patent number: 4587236
    Abstract: 6.alpha.-Methylprednisolone derivatives of Formula I ##STR1## wherein R.sub.1 is 1-oxoalkyl of 2-6 carbon atoms or benzoyl andR.sub.2 is 1-oxoalkyl of 2-6 carbon atoms, are pharmacologically efficacious compounds, e.g., as antiinflammatories.
    Type: Grant
    Filed: October 27, 1983
    Date of Patent: May 6, 1986
    Assignee: Schering Aktiengesellschaft
    Inventors: Klaus Annen, Karl Petzoldt, Henry Laurent, Rudolf Wiechert, Helmut Hofmeister
  • Patent number: 4585591
    Abstract: This is disclosed novel intermediates, i.e. 17.beta.-ethynylsteroids, which are useful for the preparation of corticoids such as hydrocortisone and prednisolone, and a process for preparing the same.
    Type: Grant
    Filed: November 25, 1981
    Date of Patent: April 29, 1986
    Assignee: Mitsubishi Chemical Industries, Ltd.
    Inventors: Issei Nitta, Shinichiro Fujimori, Toshio Haruyama, Shinya Inoue
  • Patent number: 4585590
    Abstract: Using cyanohydrin intermediates, 17-keto steroids are transformed to corticoids and 17.alpha.-acyl progesterones.
    Type: Grant
    Filed: January 30, 1985
    Date of Patent: April 29, 1986
    Assignee: The Upjohn Company
    Inventor: Verlan H. VanRheenen
  • Patent number: 4585766
    Abstract: Novel 6-oxygenated corticoid 17.alpha.-carbonates are disclosed. These compounds have strong topical anti-inflammatory activity which are accompanied by extremely weak systemic adverse reaction. The present compounds are useful for the treatment of acute and chronic eczema, eczema seborrhoicorum, contact dermatitis, atopic dermatitis, asthma, etc.
    Type: Grant
    Filed: August 28, 1984
    Date of Patent: April 29, 1986
    Assignee: Mitsubishi Chemical Industries Ltd.
    Inventors: Issei Nitta, Kenichiro Nakao, Motoyoshi Miyake, Akira Maruyama, Junko Takashima
  • Patent number: 4585765
    Abstract: 17.beta.-Hydroxy-17.alpha.-methyl-5.alpha.-androstano[3,2-c]pyrazole 17-methyl ether is a very potent reversible male contraceptive which has a very low degree of androgenic side effects. Upon cessation of administration fertility promptly returns.
    Type: Grant
    Filed: April 16, 1980
    Date of Patent: April 29, 1986
    Assignee: The Upjohn Company
    Inventors: Donald J. Tindall, Anthony R. Means
  • Patent number: 4584136
    Abstract: An Estracyt compound having a carcinostatic bound thereto is obtained by reacting an Estracyt compound with a carcinostatic having one or more radicals selected from among COOH, Cl, NH.sub.2 and OH, either directly or after reaction with an amine to replace one or both Cl groups in the nitrogen mustard portion in the Estracyt compound with a NH.sub.2 group, in the presence or absence of a catalyst. The resulting compound is more effective in cancer control than the Estracyt compound associated substance.
    Type: Grant
    Filed: March 1, 1985
    Date of Patent: April 22, 1986
    Assignee: Japan Atomic Energy Research Institute
    Inventors: Masaru Yoshida, Masaharu Asano, Isao Kaetsu, Hidetoshi Yamanaka, Katsuyuki Nakai, Hisako Yuasa, Keizo Shida
  • Patent number: 4584137
    Abstract: Estrogens characterized by an aromatic ring of the formula ##STR1## are halogenated by electrophilic substitution of a halo atom at the 1-position of the aromatic ring after protection of the sensitive 3-hydroxyl substituent and amination at the 4-position. Preferred starting materials include estrones or derivatives thereof. The estrones are preferably reduced after masking and amination to form the corresponding estradiols, which are then halogenated, deaminated and deprotected to provide the novel 1-haloestradiols.
    Type: Grant
    Filed: April 9, 1984
    Date of Patent: April 22, 1986
    Assignee: University of New Mexico
    Inventors: Mark D. Hylarides, Fred A. Mettler, Jr.
  • Patent number: 4584288
    Abstract: 6,6-ethylene-15,16-methylene-3-oxo-17.alpha.-pregn-4-ene-21,17.alpha.-carbo lactones of general Formula I ##STR1## wherein ##STR2## is a CC-single of CC-double bond, R.sub.1 is a hydrogen atom or a methyl group,R.sub.2 is a methyl or ethyl group, and ##STR3## exhibit strong gestagen potency and an aldosterone-antagonistic activity.
    Type: Grant
    Filed: January 18, 1985
    Date of Patent: April 22, 1986
    Assignee: Schering Aktiengesellschaft
    Inventors: Klaus Nickish, Dieter Bittler, Henry Laurent, Rudolf Wiechert, Sybille Beier, Walter Elger
  • Patent number: 4584289
    Abstract: The present invention relates to new 14-aminosteroids and their application in therapy and also to a process for their preparation.
    Type: Grant
    Filed: August 12, 1983
    Date of Patent: April 22, 1986
    Assignee: Etablissements Nativelle S.A.
    Inventors: Francois-Xavier Jarreau, Jean-Jacques Koenig
  • Patent number: 4582644
    Abstract: Ethynylation of 17-keto steroids (I) by standard means in the presence of a polar amine solvent produces the epi (17.beta.-ethynyl-17.alpha.-hydroxy) configuration at C.sub.17. The epi-ethisterone compounds are useful intermediates in the production of 17.alpha.-hydroxyprogesterones.
    Type: Grant
    Filed: November 21, 1984
    Date of Patent: April 15, 1986
    Assignee: The Upjohn Company
    Inventor: Jean R. Runge
  • Patent number: 4582826
    Abstract: A method of treating thrombosis, which comprises administering to a living body a thrombosis preventive and curative preparation containing as an active ingredient a pharmaceutically effective amount of a plant sterol selected from the group consisting of sitosterol and fucosterol, or an ester thereof.
    Type: Grant
    Filed: July 26, 1984
    Date of Patent: April 15, 1986
    Assignee: Bellex Corporation
    Inventor: Yuji Inada
  • Patent number: 4578221
    Abstract: Androstane carbothioic acids of the formula: ##STR1## wherein R.sup.1 represents a hydrogen atom, a hydroxy group in the .alpha.-configuration, a methyl group which may be in either the .alpha.- or .beta.-configuration, or a methylene group;R.sup.2 represents a hydroxy or protected hydroxy group in either the .alpha.- or .beta.-configuration or an oxo group;R.sup.3 represents a hydrogen, bromine, chlorine or fluorine atom; or R.sup.2 and R.sup.3 together represent a carbon-carbon bond or an epoxy group in the .beta.-configuration;R.sup.4 represents a hydrogen or fluorine atom; and the symbol represents a single or double bond and the salts thereof are useful as intermediates in the preparation of anti-inflammatory androstane 17.beta.-carbothioate esters.The compounds of formula I are prepared by reaction of a reactive derivative of a 17.beta.-carboxylic acid corresponding to the compound of formula I with hydrogen sulphide or a sulphide or hydrosulphide salt.
    Type: Grant
    Filed: July 14, 1983
    Date of Patent: March 25, 1986
    Assignee: Glaxo Group Limited
    Inventors: Gordon H. Phillipps, Brian M. Bain, Stuart B. Laing
  • Patent number: 4576936
    Abstract: Novel 6.alpha.-fluoro-9.alpha.-chloro-16.beta.-methyl-prednisolone 17, 21-diesters, and a method for their preparation, are described. The novel products are particularly valuable as anti-inflammatory agents.
    Type: Grant
    Filed: March 23, 1982
    Date of Patent: March 18, 1986
    Assignee: Sterosynt Ltd.
    Inventor: Peter MacDonald
  • Patent number: 4571334
    Abstract: A composition for curing respiratory diseases which contains a medicine such as antibiotic, chemotherapeutic and anticancer drug for respiratory disease and lung surfactant.
    Type: Grant
    Filed: December 4, 1981
    Date of Patent: February 18, 1986
    Assignee: Teijin Limited
    Inventors: Tsunemasa Yoshida, Toshio Wakabayashi, Keizo Matsumoto
  • Patent number: 4569931
    Abstract: Sebum secretion accelerator composition comprising a cholesteryl ester of a branched fatty acid represented by the formula (I): ##STR1## in which R represents a saturated aliphatic hydrocarbon group having from 11 to 23 carbon atoms and at least one alkyl substituent at a position between the carboxyl bond and the center of the main chain. The cholesteryl ester should be contained not smaller than 25 wt % of the total composition.The composition according to the invention promotes sebum secretion, and is effective in keeping healthy and beautiful skin.The composition is further advantageous in that it can be readily formed into various types of cosmetics such as lotions, creams and ointments.
    Type: Grant
    Filed: July 3, 1984
    Date of Patent: February 11, 1986
    Assignee: Kao Corporation
    Inventors: Naonobu Yoshizuka, Eijiro Takeuchi, Genji Imokawa
  • Patent number: 4568491
    Abstract: The invention is concerned with a process for the preparation of 1 hydrogen or hydroxy cholesterol derivatives and intermediates therefor. The compounds of the present invention are useful as intermediates in the preparation of 24,25-dihydroxy and 1.alpha., 24,25-trihydroxycholecalciferol.
    Type: Grant
    Filed: February 27, 1984
    Date of Patent: February 4, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andor Furst, Ludwig Labler, Werner Meier
  • Patent number: 4568673
    Abstract: A compound of the formula ##STR1## wherein Z is alkoxy of 1-4 carbon atoms or hydroxyalkoxy of 2-4 carbon atoms and Y is nitro, inhibiting the growth of murine ductal carcinoma (MXT mammary tumors).
    Type: Grant
    Filed: March 20, 1984
    Date of Patent: February 4, 1986
    Assignee: Wayne State University
    Inventors: Samuel C. Brooks, Jerome P. Horwitz
  • Patent number: RE32112
    Abstract: A composition containing spironolactone in an amount effective to suppress excess androgenic activity. The spironolactone-containing composition is applied directly to the skin site afflicted with excess androgens.
    Type: Grant
    Filed: April 3, 1984
    Date of Patent: April 15, 1986
    Inventor: German Shapiro