Three Or More Oxygens Bonded Directly To The Cyclopentanohydrophenanthrene Ring System Patents (Class 552/559)
  • Publication number: 20150105547
    Abstract: The invention relates to nitrooxyderivative of corticosteroids of general formula (I) and pharmaceutically acceptable salts or stereoisomers thereof R—(Z)a—Rx??(I) wherein R is the corticosteroid residue of formula (II): wherein: R1 is OH, R2 —CH3, or R1 and R2 are taken together to form a group of formula (III) R3 is Cl or F; R4 is H or F; wherein R1, R2, R3 and R4 can be linked to the correspondent carbon atoms of the steroidal structure in position ? or ?; with the proviso that: when R1 and R2 are the group of formula (III) then R3 is F and R4 is H or F; The compounds are useful in the treatment of respiratory diseases, inflammatory diseases, dermatological diseases and ocular diseases.
    Type: Application
    Filed: November 26, 2014
    Publication date: April 16, 2015
    Inventors: Francesca BENEDINI, Stefano BIONDI, Ennio ONGINI
  • Patent number: 8993633
    Abstract: It is reported herein that certain muscle diseases and conditions, including forms of muscular dystrophy, are characterized by impaired insulin-dependent signaling in the muscle tissue, in essence, a form of insulin resistance. The present disclosure relates to therapeutic agents, compositions and methods for treating a muscle disease or condition characterized by impaired insulin-dependent signaling by targeting components of the defective insulin signaling pathway. The disease or condition may be treated by administering a therapeutic agent that activates the insulin signaling pathway, in particular, therapeutic agents that act post-insulin receptor to modulate intracellular effector molecules. An exemplary modulator is metformin. Metformin may be administered alone or may be coadministered with another therapeutic agent for treating the muscle disease or condition, such as a corticosteroid.
    Type: Grant
    Filed: May 18, 2010
    Date of Patent: March 31, 2015
    Assignees: Fate Therapeutics, (Canada) Inc., Ottaw Hospital Research Institute
    Inventors: Lynn Megeney, Carol Evans
  • Patent number: 8685381
    Abstract: The invention provides skin protecting and penetrating, easy-to-administer base and active agent-containing compositions, such as those including hydrocortisone, for treating the skin of mammals for different dermatologic disorders. This is effected by topically administering effective amounts of the compositions thereto in forms that address the skin and mucosa of the mouth and lips, and the rest of the body. Additionally, an optional flavoring addition to these products affords significantly better tasting, and less bitter, compositions, allowing a more pleasant experience and better compliance by patients. The compositions include a unique formulation of FANCOL VB, Natunola Castor 1023, Finsolv TN, bees wax and, optionally, one or a plurality of plant or plant seed oils, fatty alcohols, fats and flavorings, in desirable weight percents thereof, in various forms, and preferably in a form of a solid roll-on stick in a variety of sizes and of a jar or pot.
    Type: Grant
    Filed: September 14, 2011
    Date of Patent: April 1, 2014
    Inventors: Joel Schlessinger, Daniel Isaac Schlessinger
  • Patent number: 8586770
    Abstract: The invention relates to methods to manipulate stem cells in vivo and in vitro to treat, e.g., a condition where cell or tissue repair is needed.
    Type: Grant
    Filed: February 18, 2011
    Date of Patent: November 19, 2013
    Assignee: Harbor Therapeutics, Inc.
    Inventor: James M. Frincke
  • Publication number: 20090137542
    Abstract: Sixteen new and one known metabolites were obtained by incubation of tibolone and hydroxytibolones with various fungi. Their structures were elucidated by means of a homo and heteronuclear 2D NMR and by HREI-MS techniques. The relative stereochemistry was deduced by 2D NOESY experiment. These metabolites have shown promising inhibitory activities against ?-glucosidase enzyme. Seven metabolites exhibited potent inhibitory activity against the ?-glucosidase enzyme and were thus found useful in the treatment of diabetes mellitus and other diseases related to the activity of ?-glucosidase enzyme.
    Type: Application
    Filed: November 23, 2007
    Publication date: May 28, 2009
    Applicant: International Center for Chemical Sciences
    Inventors: Attaur Rahman, Muhammed Iqbal Choudhary, Syed Adnan Ali Shah, Shamsun Nahar Khan
  • Patent number: 7214807
    Abstract: This invention discloses a novel method for the conversion of carboxylic acids to carbothioic acids and application of the method to the preparation of androstane carbothiolates, such as fluticasone propionate, which avoids column chromatography.
    Type: Grant
    Filed: May 18, 2004
    Date of Patent: May 8, 2007
    Assignee: Abbott Laboratories
    Inventors: Jufang Barkalow, Steven A. Chamberlin, Arthur J. Cooper, Azad Hossain, John J. Hufnagel, Denton Langridge
  • Patent number: 6992076
    Abstract: This invention is directed to methods for providing sustained systemic concentrations of therapeutic or prophylactic agents such as GABA analogs following oral administration to animals. This invention is also directed to compounds and pharmaceutical compositions that are used in such methods.
    Type: Grant
    Filed: October 5, 2001
    Date of Patent: January 31, 2006
    Assignee: XenoPort, Inc.
    Inventors: Kenneth C. Cundy, Mark A. Gallop, Cindy X. Zhou
  • Publication number: 20020091278
    Abstract: A series of novel steroid derivatives are described. The steroid derivatives are antibacterial agents. The steroid derivatives also act to sensitize bacteria to other antibiotics including erythromycin and novobiocin.
    Type: Application
    Filed: August 15, 2001
    Publication date: July 11, 2002
    Inventors: Paul B. Savage, Chunhong Li
  • Patent number: 6388108
    Abstract: Newly isolated aminosterol compounds and pharmaceutical compositions based on the aminosterol compounds are described. Methods for the treatment of various disorders, for example, a microbial infection, are also described.
    Type: Grant
    Filed: May 29, 2001
    Date of Patent: May 14, 2002
    Assignee: Genaera Corporation
    Inventors: Meena Rao, Binyamin Feibush, William Kinney, Michael Zasloff, Lincoln Noecker
  • Patent number: 5723455
    Abstract: Novel antiandrogenic agents are provided. An exemplary group of compounds has the structural formula (I) ##STR1## wherein R.sup.1 through R.sup.10, a and b are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat androgen-related clinical conditions are provided, as are methods and compositions for using the compounds as contraceptive agents.
    Type: Grant
    Filed: March 11, 1997
    Date of Patent: March 3, 1998
    Assignee: SRI International
    Inventors: Masato Tanabe, Wan-Ru Chao, Wesley K. M. Chong, David F. Crowe
  • Patent number: 5710293
    Abstract: The present invention relates to a method of using a perchloric acid catalyzed reaction to make acyl derivatives of norprogesterone compounds and, in particular, 16-methylene-17.alpha.-hydroxy-19-norpregn-4-ene-3,20-dione.
    Type: Grant
    Filed: October 13, 1995
    Date of Patent: January 20, 1998
    Assignee: The Population Council, Center for Biomedical Research
    Inventor: Fang Li
  • Patent number: 5637691
    Abstract: Compounds having a broad range of antimicrobial activity generally have a structure including asteroid nucleus with a cationic, preferably polyamine, side chain (X) and an anionic side chain (Y). The invention is also directed to compounds of the Formula III: ##STR1## preferably where the steroid ring nucleus is saturated; the steroid ring substituent Z.sub.5 is .alpha.-H; one Z.sub.7 is .beta.-H and the other is .alpha.-H or .alpha.-OH; both substituents Z.sub.12 are hydrogen; X' is a polyamine side chain of the formula --NH--(CH.sub.2).sub.p --NH--(CH.sub.2).sub.q --N(R.sup.II)(R.sup.III) where p and q are each independently 3 or 4, and R.sup.II and R.sup.III are each independently hydrogen or methyl; R' is methyl; and Y' is (C.sub.1 -C.sub.10)-alkyl substituted with a group such as --CO.sub.2 H or --SO.sub.3 H.
    Type: Grant
    Filed: August 18, 1994
    Date of Patent: June 10, 1997
    Assignee: Magainin Pharmaceuticals, Inc.
    Inventors: Leah L. Frye, Michael A. Zasloff, William A. Kinney, Robert Moriarty
  • 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: 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: 5352808
    Abstract: A process for the preparation of a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms optionally substituted by halogen or a nitrogen or oxygen function and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.2 is alkyl of 1 to 4 carbon atoms and the A, B, C and D rings are optionally substituted by at least one member of the group consisting of optionally protected --OH or .dbd.0, halogen, alkyl and alkoxy of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms comprising reacting a compound of the formula ##STR2## wherein R.sub.1 and R.sub.2 and the A, B, C and D rings are defined as above with an oxidizing agent in the presence of water and an at least partially water-miscible solvent to obtain a compound of the formula ##STR3## wherein R.sub.1 and R.sub.
    Type: Grant
    Filed: November 5, 1992
    Date of Patent: October 4, 1994
    Assignee: Roussel Uclaf
    Inventors: Jean Buendia, Michel Vivat
  • Patent number: 5182381
    Abstract: Novel 3-keto-19-nor-.DELTA..sup.4,9 -steroids of the formula ##STR1## and their non-toxic, pharmaceutically acceptable acid addition salts possessing a remarkable antiglucocorticoidal activity.
    Type: Grant
    Filed: September 10, 1991
    Date of Patent: January 26, 1993
    Assignee: Roussel Ulcaf
    Inventors: Daniel Philibert, Jean G. Teutsch, Germain Costerousse, Roger Deraedt
  • Patent number: 5112998
    Abstract: There are provided pregnane derivatives represented by formula ##STR1## wherein A.sup.1 represents a hydrogen atom or a hydroxyl group, A.sup.2 represents a substituent such as a hydroxyl group when A.sup.1 represents a hydrogen atom, or A.sup.2 represents a hydrogen atom when A.sup.1 represents a hydroxyl group, or A.sup.1 and A.sup.2 are combined together to form an oxo group; D.sup.1 represents a substitutent such as a hydroxyl group, and D.sup.2 represents a hydrogen atom, or D.sup.1 and D.sup.2 are combined together to form an epoxy group or a single bond; D.sup.3, D.sup.5 and D.sup.7 each represents a hydrogen atom, D.sup.4 represents a hydroxyl group, and D.sup.6 represents a substitutent such as a hydroxyl group, or D.sup.3 and D.sup.4 may be combined together to form an epoxy group or a single bond, or D.sup.4 and D.sup.5 may be combined together to form a single bond, or D.sup.5 and D.sup.6 may be combined together to form an epoxy group or a single bond, or D.sup.6 and D.sup.
    Type: Grant
    Filed: June 15, 1990
    Date of Patent: May 12, 1992
    Assignee: Kuraray Co., Ltd.
    Inventors: Jiro Tsuji, Takashi Takahashi, Masao Tsuji, Naoshi Nakagawa, Tetsuo Takigawa
  • Patent number: 5015746
    Abstract: 11.beta.,17.alpha.,21-Trihydroxy-1,4-pregnadiene-3,20-dione 21-[(E,E)-3,7,11-trimethyl-2,6,10-dodecatrienoate] of the formula ##STR1## an antiinflammatory composition thereof and a method for the production thereof.11.beta.,17.alpha.,21-Trihydroxy-1,4-pregnadiene-3,20-dione 21-[(E,E)-3,7,11-trimethyl-2,6,10-dodecatrienoate] of the present invention exhibits remarkably excellent antiinflammatory action and besides, displays reduced side effects and can be produced in high selectivity and good yield and conveniently.
    Type: Grant
    Filed: January 23, 1989
    Date of Patent: May 14, 1991
    Assignee: Kuraray Co., Ltd.
    Inventors: Yutaka Mizushima, Keiko Hoshi, Rie Igarashi, Hirofusa Ajioka, Noriyuki Yamamoto, Masahito Komuro, Koichi Kanehira, Masayuki Inoue, Takashi Nishida, Manzo Shiono, Michio Terasawa, Kenzo Arizono