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)
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Patent number: 8445471Abstract: 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: GrantFiled: May 16, 2008Date of Patent: May 21, 2013Assignee: Hovione Inter LimitedInventors: Luis Sobral, Filipe Gaspar, William Heggie, Emilia Leitao, Jose Rafael Antunes
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Patent number: 6388108Abstract: 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: GrantFiled: May 29, 2001Date of Patent: May 14, 2002Assignee: Genaera CorporationInventors: Meena Rao, Binyamin Feibush, William Kinney, Michael Zasloff, Lincoln Noecker
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Patent number: 6028066Abstract: 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: GrantFiled: July 2, 1997Date of Patent: February 22, 2000Assignee: Imarx Pharmaceutical Corp.Inventor: Evan C. Unger
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Patent number: 5972922Abstract: 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: GrantFiled: December 21, 1995Date of Patent: October 26, 1999Assignee: Alcon Laboratories, Inc.Inventors: John W. Wilks, Thomas F. DeKoning, Paul A. Aristoff
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Patent number: 5637691Abstract: 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: GrantFiled: August 18, 1994Date of Patent: June 10, 1997Assignee: Magainin Pharmaceuticals, Inc.Inventors: Leah L. Frye, Michael A. Zasloff, William A. Kinney, Robert Moriarty
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Patent number: 5428181Abstract: 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: GrantFiled: December 24, 1992Date of Patent: June 27, 1995Assignee: Hoechst Japan LimitedInventors: Tatsuo Sugioka, Mizuho Inazu
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Patent number: 5391776Abstract: 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: GrantFiled: February 10, 1993Date of Patent: February 21, 1995Assignee: Mitsubishi Kasei CorporationInventors: Hiroaki Ueno, Syuichiro Kadowaki, Akihito Kamizono, Masahiko Morioka, Akihisa Mori
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Patent number: 5183815Abstract: 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: GrantFiled: February 19, 1992Date of Patent: February 2, 1993Assignee: Merck & Co., Inc.Inventors: Walfred S. Saari, Gideon A. Rodan, Thorsten E. Fisher, Paul S. Anderson
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Patent number: 5026882Abstract: 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: GrantFiled: December 23, 1988Date of Patent: June 25, 1991Assignee: SmithKline Beecham CorporationInventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf