The Phosphorus Is Bonded Directly At The 21-position Or Is Bonded Directly To A Chalcogen Which Is Bonded Directly At The 21-positon Patents (Class 552/507)
  • Patent number: 8445471
    Abstract: A process for obtaining 21-disodium phosphate pregnane derivative compounds of formula (I), wherein X?R?H or X?F and R=?-CH3 or X?F and R=?-CH3: comprises spray drying a solution comprising compound of formula (I).
    Type: Grant
    Filed: May 16, 2008
    Date of Patent: May 21, 2013
    Assignee: Hovione Inter Limited
    Inventors: Luis Sobral, Filipe Gaspar, William Heggie, Emilia Leitao, Jose Rafael Antunes
  • 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: 6028066
    Abstract: The present invention describes, inter alia, novel prodrugs comprising fluorinated amphiphiles, compositions comprising the novel prodrugs, and methods of use of the prodrugs and compositions.
    Type: Grant
    Filed: July 2, 1997
    Date of Patent: February 22, 2000
    Assignee: Imarx Pharmaceutical Corp.
    Inventor: Evan C. Unger
  • Patent number: 5972922
    Abstract: Novel angiostatic .DELTA..sup.4,9(11) -steroids (I), ##STR1## C.sub.21 -oxygenated steroids (II) and other known steroidal compounds have been found to be useful in treating angiogenesis in mammals who have a need for the same. These steroids are useful in treating diseases of neovascularization such as cancer, diabetes and arthritis.
    Type: Grant
    Filed: December 21, 1995
    Date of Patent: October 26, 1999
    Assignee: Alcon Laboratories, Inc.
    Inventors: John W. Wilks, Thomas F. DeKoning, Paul A. Aristoff
  • 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: 5428181
    Abstract: A compound represented by the general formula: ##STR1## wherein A-O-denotes a residue of a compound having an estrogenic activity; R.sub.1 denotes H or a C.sub.1 -C.sub.6 alkyl group; X denotes a single bond, a C.sub.1 -C.sub.10 alkylene group or a group of the formula ##STR2## wherein R.sub.2 denotes H or a C.sub.1 -C.sub.5 alkyl group; Z denotes a nitro group or a halogen; n is an integer of 3 to 12; k is an integer of 1 to 5; L is an integer of 0 to 5; and q is an integer of 1 to 3,and physiologically acceptable salts thereof are disclosed.The compounds have a high affinity to bone tissues, and the compounds per se and metabolites thereof show significant therapeutic effect on bone diseases such as osteoporosis, rheumatoid arthritis and osteoarthritis.
    Type: Grant
    Filed: December 24, 1992
    Date of Patent: June 27, 1995
    Assignee: Hoechst Japan Limited
    Inventors: Tatsuo Sugioka, Mizuho Inazu
  • Patent number: 5391776
    Abstract: Asteroid derivative of the general formula: ##STR1## wherein X--O-- represents a residue of steroid compound and --A-- represents --CO[NH(CHR.sup.1).sub.y --(Y).sub.p --CO].sub.m NH--, --CO--(R.sup.2).sub.x --(Z).sub.q --CO--NH--, or --CO--(CH.sub.2).sub.n --. A therapeutic agent to osteopathy comprising the above steroid derivative is also provided.
    Type: Grant
    Filed: February 10, 1993
    Date of Patent: February 21, 1995
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Hiroaki Ueno, Syuichiro Kadowaki, Akihito Kamizono, Masahiko Morioka, Akihisa Mori
  • Patent number: 5183815
    Abstract: Described are new agents for treating bone disorders associated with a reduction in bone mass and abnormalities in bone resportion or bone formation including osteoporosis. Paget's disease, bone metastases and malignant hypercalcemia. The agents are hydroxyl containing steroidal hormones, having bone resportion antagonist or bone formation stimulatory activity, covalently linked through the hydroxyl group via a bond hydrolyzable in the human body, e.g. carbamate or carbonate, which is further covalently linked to an amino, or hydroxy substituted alkylidene-1,1-bisphosphonate, through the respective amino or hydroxy group. The alkyl bisphosphonate moiety confers bone affinity. The agent acts by delivering the steroidal hormone directly to the bone target site where it is released for bone resorption antagonist or bone formation stimulatory action by hydrolysis of the hydrolyzable covalent bond.
    Type: Grant
    Filed: February 19, 1992
    Date of Patent: February 2, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Walfred S. Saari, Gideon A. Rodan, Thorsten E. Fisher, Paul S. Anderson
  • Patent number: 5026882
    Abstract: The invention relates to 3-phosphinic acid steroidal compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5.alpha.-reductase.
    Type: Grant
    Filed: December 23, 1988
    Date of Patent: June 25, 1991
    Assignee: SmithKline Beecham Corporation
    Inventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf