Patents Examined by Kimberly J. Kestler
  • Patent number: 5886175
    Abstract: The invention provides compounds of the formulas ##STR1## which are useful as intermediates for the preparation of 6-demethyl-6-deotetracycline antibiotic agents.
    Type: Grant
    Filed: December 8, 1994
    Date of Patent: March 23, 1999
    Assignee: American Cyanamid Company
    Inventors: Phaik-Eng Sum, Ving J. Lee, Joseph J. Hlavka, Raymond T. Testa
  • Patent number: 5583127
    Abstract: Disclosed are 17-iminomethylalkenyl and 17-iminoalkyl-14.beta.-hydroxy-5.beta.-androstane derivatives of the formula (I): ##STR1## wherein the symbol means .alpha. or .beta. configuration or a Z or E configuration; A represents (CH.sub.2).sub.m or --(CH.dbd.CH).sub.n --; m represents an integer number from 1 to 6; n represents an integer number from 1 to 3; R.sup.2 represents hydrogen or hydroxy; R.sup.1 represents hydrogen, C.sub.2 -C.sub.4 alkyl unsubstituted or substituted by NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5, which may be the same or different, represent hydrogen, C.sub.1 -C.sub.4 alkyl or R.sup.4 and R.sup.5 may form, when taken together with the nitrogen atom, a five- or six- membered heterocyclic ring optionally containing one or more heteroatoms selected from oxygen and nitrogen; R.sup.3 represents NHC(.dbd.X)NR.sup.6 R.sup.7 or OR.sup.8 wherein R.sup.6 and R.sup.7, which may be the same or different, represent hydrogen, methyl, or C.sub.2 -C.sub.4 alkyl unsubstituted or substituted by NR.
    Type: Grant
    Filed: December 23, 1994
    Date of Patent: December 10, 1996
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Alberto Cerri, Giuseppe Bianchi, Patrizia Ferrari, Elena Folpini, Piero Melloni
  • Patent number: 5554603
    Abstract: The invention presents 17.beta.-nitro and 11.beta., 17.beta.-dinitro esters of estradiol which are made from 3-acyloxy-17-keto- or 3,17-dihydroxy-1,3,5-estratrienes by processes known in the art. The compounds exhibit estrogenic activity.
    Type: Grant
    Filed: September 17, 1993
    Date of Patent: September 10, 1996
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Hyun K. Kim, Richard P. Blye, Gabriel Bialy
  • Patent number: 5508453
    Abstract: The present invention relates to intermediates for use in the preparation of taurocholanic acids. The intermediates have the following formula (IV): ##STR1## in which A completes the 5.beta.-cyclopentaneperhydrophenanthrene structure of a cholanic acid; E is hydrogen or a methyl; and R is a hydrocarbon residue bonded to the carbonyl group by a tertiary carbon.
    Type: Grant
    Filed: May 19, 1994
    Date of Patent: April 16, 1996
    Assignee: Sanofi
    Inventors: Roberto Arosio, Vittorio Rossetti
  • Patent number: 5506221
    Abstract: The invention presents compounds useful for the prevention of inflammatory or allergic reaction or the treatment of cardiovascular or haemodynamic disorders having the formula: ##STR1## where R= ##STR2## where R= ##STR3## or pharmaceutically acceptable acids or salts thereof.
    Type: Grant
    Filed: April 12, 1994
    Date of Patent: April 9, 1996
    Assignees: University of British Columbia, University of Alberta
    Inventors: Raymond J. Andersen, Theresa M. Allen, David L. Burgoyne
  • Patent number: 5502222
    Abstract: Described is a process for the regioselective dehydration of 11-hydroxy steroids using PCl.sub.5, PCl.sub.3, POCl.sub.3 or either SO.sub. Cl.sub.2 and imidazole, or PPh.sub.3 and CCl.sub.4. The disclosed process selectively forms .increment..sup.9,11 steroids from either 11-.alpha.- or 11-.beta.-hydroxy steroids, and can also be used for the one-step conversion of 11,21-dihydroxy steroids to 21-chloro-.increment..sup.9,11 steroids.
    Type: Grant
    Filed: June 1, 1994
    Date of Patent: March 26, 1996
    Assignee: Schering Corporation
    Inventors: Xiaoyong Fu, Tiruvettipuram K. Thiruvengadam, Chou-Hong Tann, Junning Lee, Cesar Colon
  • Patent number: 5502183
    Abstract: Novel steroids having a 9.alpha.-hydroxy or a 9.alpha.-carbonate substituent can be prepared from 9.alpha.-hydroxyandrostenedione and can be utilized in the synthesis of commercially valuable corticosteroids such as betamethasone. The 9.alpha.-carbonates are prepared by reaction of the corresponding 9.alpha.-hydroxy steroid with a sequence of excess base, trialkylsilyl chloride, alkyl haloformate and alkanol or by using excess base, alkyl haloformate and alkoxide. 9.alpha.-Carbonate-17-keto compounds can be treated with lithium acetylide and a lithium salt to afford the corresponding 17.alpha.-ethynyl-17.beta.-hydroxy-9.alpha.-carbonate. This compound is then esterified with a novel series of reagents to give the 17-ester which can be reduced the corresponding 17-allene. Oxidation of this allene to the bis-epoxide compound, followed by treatment with an alkali metal salt of a carboxylic acid under phase transfer conditions gives the 17.alpha.-hydroxy 21-ester 9.alpha.-carbonate. Elimination of the 9.alpha.
    Type: Grant
    Filed: July 25, 1994
    Date of Patent: March 26, 1996
    Assignee: Schering Corporation
    Inventors: David R. Andrews, Anantha R. Sudhakar
  • Patent number: 5502046
    Abstract: The invention relates to 11 .beta.-substituted 14,17-ethanoestratrienes of the general formula 1 ##STR1## where R.sup.1, R.sup.2 and R.sup.3 are defined in the specification. The compound have antiestrogenic activity and are, therefore, useful for the treatment of estrogen dependent disorders.
    Type: Grant
    Filed: June 24, 1994
    Date of Patent: March 26, 1996
    Assignee: Schering Aktiengesellschaft
    Inventors: Rolf Bohlmann, Hermann Kunzer, Hans-Peter Muhn-Seipoldy, Yukishige Nishino, Martin Schneider
  • Patent number: 5500421
    Abstract: The invention discloses N-alkyl-tauroursodeoxycholic acids and their pharmaceutically acceptable salts of the formula ##STR1## wherein R is a C.sub.2 -C.sub.4 alkyl group and R.sub.1 is hydrogen, an alkali metal, an alkaline earth metal or a radical of a basic amino acid.The compounds are prepared by reacting a mixed anhydride of ursodeoxycholic acid and alkyltaurine followed by percolation through two columns respectively containing a strong cationic resin in H.sup.+ form and a weakly anionic resin OH.sup.- form. The compounds are useful for the treatment of hepatic diseases.
    Type: Grant
    Filed: February 15, 1994
    Date of Patent: March 19, 1996
    Assignee: Prodotti Chimici Alimentari SPA
    Inventor: Massimo Parenti
  • Patent number: 5498740
    Abstract: Compositions which, in the form of aqueous dispersions or of solutions in organic solvents, are suitable for the treatment of fiber materials can be obtained by reaction of organic phosphites and quinones and subsequent reaction with mono-, di- or polyisocyanates. Flame-retardant properties having a good permanence are imparted, above all, to fabrics comprising polyester fibers by this procedure.
    Type: Grant
    Filed: March 5, 1993
    Date of Patent: March 12, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Salman Dermeik, Martina Wanner, Karl-Heinz Lemmer, Reinhold Braun
  • Patent number: 5496814
    Abstract: This invention relates to 8.alpha.-3-hydroxyestra-1,3,5(10),9(11)tetraen-17-one (.DELTA.9(11)-dehydro-8-isoestrone) (VI), ##STR1## to the process for its preparation, to pharmaceutical compositions containing said 8.alpha.-3-hydroxyestra-1,3,5(10),9(11)tetraen-17-one (.DELTA.9(11)-dehydro-8-isoestrone) (VI) and to the use of said 8.alpha.-3-hydroxyestra-1,3,5(10),9(11)tetraen-17-one (.DELTA.9(11)-dehydro-8-isoestrone) (VI) for modifying the balance between bone production and bone resorption, and as an antioxidant in a host animal, including man.
    Type: Grant
    Filed: December 1, 1994
    Date of Patent: March 5, 1996
    Assignee: American Home Products Corporation
    Inventors: Frederick O. Gemmill, Jr., Chester E. Orzech, Steven J. Adelman
  • Patent number: 5496813
    Abstract: There are described spontaneously dispersible agents containing sterolester and/or sterolphosphor compounds having a pronounced antitumour activity. Novel sterolesters and sterolphosphor compounds, their use for treating tumors, and processes for their preparation are disclosed.
    Type: Grant
    Filed: August 13, 1992
    Date of Patent: March 5, 1996
    Assignee: Marigen S.A.
    Inventors: Carl Eugster, Conrad H. Eugster, Walter Haldemann, Giorgio Rivara
  • Patent number: 5495031
    Abstract: The invention provides a process for the production of compounds of the formula: ##STR1## wherein R, R.sup.3, R.sup.4 and W are defined in the specification in which a compound of the following formula: ##STR2## is reacted with a nucleophile of the formula WH in an inert atmosphere in the presence of a polar aprotic solvent. The resulting compounds are useful as antibiotics.
    Type: Grant
    Filed: September 13, 1994
    Date of Patent: February 27, 1996
    Assignee: American Cyanamid Company
    Inventors: Phaik-Eng Sum, Ving J. Lee, Raymond T. Testa
  • Patent number: 5495032
    Abstract: The invention provides a process for the production of compounds of the formula: ##STR1## wherein, R, R.sup.3, R.sup.4, X and W are defined in the specification in which a compound of the following formula: ##STR2## is reacted with a nucleophile of the formula WH in an inert atmosphere in the presence of a polar-protic or a polar-aprotic solvent. The resulting compounds are useful as antibiotics.
    Type: Grant
    Filed: September 27, 1994
    Date of Patent: February 27, 1996
    Assignee: American Cyanamid Company
    Inventors: Phaik-Eng Sum, Ving J. Lee, Joseph J. Hlavka, Raymond T. Testa
  • Patent number: 5494903
    Abstract: The invention is drawn to 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds of the formula ##STR1## wherein R, X, R.sup.5 and R.sup.6 are defined in the specification. The compounds of the invention are useful as broad spectrum antibiotics.
    Type: Grant
    Filed: August 4, 1994
    Date of Patent: February 27, 1996
    Assignee: American Cyanamid Company
    Inventors: Joseph J. Hlavka, Phaik-Eng Sum, Yakov Gluzman, Ving J. Lee, Adma A. Ross
  • Patent number: 5495018
    Abstract: The invention provides compounds of the formulas ##STR1## which are useful as intermediates for the preparation of 6-demethyl-6-deotetracycline antibiotic agents.
    Type: Grant
    Filed: December 8, 1994
    Date of Patent: February 27, 1996
    Assignee: American Cyanamid Company
    Inventors: Phaik-Eng Sum, Ving J. Lee, Joseph J. Hlavka, Raymond T. Testa
  • Patent number: 5495030
    Abstract: The invention provides compounds of the formula: ##STR1## wherein R, R.sup.1 and Y are defined in the specification. The compounds are useful for the production of 6-demethyl-6-deoxytracycline derivatives.
    Type: Grant
    Filed: September 1, 1994
    Date of Patent: February 27, 1996
    Assignee: American Cyanamid Company
    Inventors: Phaik-Eng Sum, Ving J. Lee, Raymond T. Testa
  • Patent number: 5494906
    Abstract: Vitamin D.sub.2 analogs in which a cyclopentane ring is introduced onto the 25-carbon of the side chain of 1.alpha.,25-dihydroxyvitamin D.sub.2 and its 24-epimer. The compounds are characterized by a marked intestinal calcium transport activity while exhibiting much lower activity than 1.alpha.,25-dihydroxyvitamin D.sub.3 in their ability to mobilize calcium from bone. Because of their preferential calcemic activity, these compounds would be useful for the treatment of diseases where bone formation is desired, such as osteoporosis.
    Type: Grant
    Filed: May 5, 1995
    Date of Patent: February 27, 1996
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Naoshi Nakagawa
  • Patent number: 5491138
    Abstract: Disclosed is a method of inhibiting the growth of tumors by administering an estradiol derivative-alkylating agent conjugate of the formula (I'): ##STR1## wherein R.sup.1 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy; R.sup.2 is acyl or benzyl; m is an integer of 1 to 3; and n is an integer of 0 to 3. Also disclosed is a method of inhibiting the growth of tumors by administering a compound of the formula (II); ##STR2## wherein R.sup.1 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy; R.sup.2 is acyl or benzyl; m is an integer of 1 to 3; n is an integer of 0 to 3; and X is hydroxy or halogen.
    Type: Grant
    Filed: March 22, 1995
    Date of Patent: February 13, 1996
    Assignee: Kureha Kagaku Kogyo Kabushiki Kaisha
    Inventors: Koichi Niimura, Takako Kawabe, Tsutomu Wada, Tsuyoshi Saitoh, Kenji Bannai
  • Patent number: 5488044
    Abstract: Vitamin D.sub.3 analogs in which a double bond has been introduced into the side chain between carbons 20 and 22. The compounds are characterized by a marked intestinal calcium transport activity while exhibiting much lower activity than 1.alpha.,25-dihyroxyvitamin D.sub.3 their ability to mobilize calcium from bone. Because of their preferential calcemic activity, these compounds would be useful for the treatment of diseases where bone formation is desired, such as osteoporosis. The compounds also have relatively high HL-60 cell differentiation activity making them useful for the treatment of diseases characterized by abnormal cell differentiation or cell proliferation, such as psoriasis.
    Type: Grant
    Filed: May 16, 1995
    Date of Patent: January 30, 1996
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Rafal R. Sicinski