Sulfur Or Nitrogen Attached Directly Or Indirectly To The Cyclopentanohydrophenanthrene Ring System By Acyclic Nonionic Bonding Patents (Class 540/67)
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Publication number: 20150105547Abstract: 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: ApplicationFiled: November 26, 2014Publication date: April 16, 2015Inventors: Francesca BENEDINI, Stefano BIONDI, Ennio ONGINI
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Patent number: 8933062Abstract: 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: GrantFiled: January 28, 2008Date of Patent: January 13, 2015Assignee: Nicox S.A.Inventors: Francesca Benedini, Stefano Biondi, Ennio Ongini
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Publication number: 20110294766Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: February 27, 2009Publication date: December 1, 2011Applicant: AstraZeneca ABInventors: Frank Burkamp, Tesfaledet Mussie, Paul Andersson, Inga-Britt Andersson, Sumita Bhatacharyya, Håkan Bladh, Svetlana Ivanova, Matti Lepistö
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Publication number: 20110263526Abstract: The present invention relates to nitric oxide releasing prodrugs of known drugs or therapeutic agents which are represented herein as compounds of formula (I) wherein the drugs or therapeutic agents contain one or more functional groups independently selected from a carboxylic acid, an amino, a hydroxyl and a sulfhydryl group. The invention also relates to processes for the preparation of the nitric oxide releasing prodrugs (the compounds of formula (I)), to pharmaceutical compositions containing them and to methods of using the prodrugs.Type: ApplicationFiled: April 22, 2011Publication date: October 27, 2011Applicant: PIRAMAL LIFE SCIENCES LIMITEDInventor: Apparao SATYAM
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Publication number: 20110144073Abstract: The invention relates to nitrooxy derivatives of fluocinolone acetonide, triamcinolone acetonide, betamethasone and beclomethasone, methods for their preparation, pharmaceutical compositions containing these compounds, and methods of using these compounds and compositions for treating diabetic macular edema, diabetic retinopathy, macular degeneration, age-related macular degeneration and other diseases of retina and macula lutea.Type: ApplicationFiled: July 7, 2009Publication date: June 16, 2011Inventors: Francesca Benedini, Annalisa Bonfanti, Valerio Chiroli, Rebecca Steele, Ennio Ongini, Stefano Biondi
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Publication number: 20100093685Abstract: 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: ApplicationFiled: January 28, 2008Publication date: April 15, 2010Inventors: Francesca Benedini, Stefano Biondi, Ennio Ongini
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Publication number: 20090318396Abstract: New chemical entities which comprise corticosteroids and phosphorylated ?-agonists for use in therapy and compositions comprising and processes for preparing the same.Type: ApplicationFiled: June 9, 2009Publication date: December 24, 2009Applicant: Gilead Sciences, Inc.Inventors: William R. Baker, Musong Kim, Alexander Rudolph, Marcin Stasiak, Josh Van Veldhuizen
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Patent number: 6197761Abstract: Compounds of the androstane series are described having general formula and solvates thereof, in which R1 represents O, S or NH; R2 individually represents OC(═O)C1-6 alkyl; R3 individually represents hydrogen, methyl (which may be in either the &agr; or &bgr; configuration) or methylene; or R2 and R3 together represent where R6 and R7 are the same or different and each represents hydrogen or C1-6 alkyl; R4 and R5 are the same or different and each represents hydrogen or halogen and represents a single or a double bond. These compounds and their solvates have use in medicine as anti-inflammatory or anti-allergic agents.Type: GrantFiled: June 24, 1998Date of Patent: March 6, 2001Assignee: Glaxo Wellcome Inc.Inventors: Keith Biggadike, Panayiotis Alexandrou Procopiou
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Patent number: 6114318Abstract: Compounds of the androstane series are described having the formula (I) and solvates thereof in which R.sub.1 and R.sub.2 are the same or different and each represents hydrogen or C.sub.1-6 alkyl; R.sub.3 and R.sub.4 are the same or different and each represents hydrogen or halogen; and ##STR1## represents a single or a double bond. Compounds of formula (I) and their solvates are useful as anti-inflammatory or anti-allergic agents.Type: GrantFiled: June 24, 1998Date of Patent: September 5, 2000Assignee: Glaxo Group LimitedInventors: Keith Biggadike, Panayiotis Alexandrou Procopiou
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Patent number: 5837698Abstract: The present invention relates to a pharmaceutical composition or preparation which comprises hydroxyl containing steroidal hormones and organic nitrite/nitrate or other nitric oxide donating agents.Type: GrantFiled: May 2, 1996Date of Patent: November 17, 1998Assignee: G. D. Searle & Co.Inventors: Foe S. Tjoeng, Mark G. Currie, Mark E. Zupec
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Patent number: 5801165Abstract: Compounds of formula I ##STR1## where R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, n, and are as defined herein, their use as antiinflammatory, immunosuppressive, and antiallergic agents, pharmaceutical compositions comprising them, and methods for their preparation comprising irradiating compounds of formula II ##STR2## under an inert atmosphere, in the presence or absence of a compound of formula R.sub.3 --S--S(O).sub.m --R.sub.8, where R.sub.7, R.sub.8, and m are as defined herein, and methods for their preparation comprising oxidizing, reducing, halogenating, or alkylating compounds of formula I are disclosed.Type: GrantFiled: June 2, 1995Date of Patent: September 1, 1998Assignee: Rhone-Poulenc Rorer LimitedInventors: Michael John Ashton, Sven Jan-Anders Karlsson, Bernard Yvon Jack Vacher, Michael Thomas Withnall
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Patent number: 5420120Abstract: Topically administrable C-21 thioether glucocorticoid steroid derivatives are disclosed as effective anti-inflammatory agents for the treatment of ophthalmic inflammatory disorders. These C-21 thioether derivatives do not cause a significant increase in intraocular pressure as a side effect.Type: GrantFiled: December 17, 1993Date of Patent: May 30, 1995Assignee: Alcon Laboratories, Inc.Inventor: John J. Boltralik
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Patent number: 5200518Abstract: Compounds of the formula: ##STR1## wherein X is H, F, Cl, or CH.sub.3and Y is ##STR2## wherein R.sub.1 is H, alkyl of 1-5 carbon atoms, phenyl, or benzyl;R.sub.2 is COOR.sub.6, R.sub.5 COOR.sub.6, or R.sub.5 CONHR.sub.6 ;R.sub.3 is H, F, OH, or CH.sub.3 ;R.sub.4 is CH.sub.2 OH, CH.sub.2 OCOR.sub.6, COOR.sub.6, or CONHR.sub.6 ;R.sub.5 is alkyl of 1-3 carbon atoms;R.sub.6 is alkyl of 1-5 carbon atoms, or benzyl;represents a single or double bond;.about. represents .alpha.-position, .beta.-position, or a mixture of both .alpha.- and .beta.-positions; and-- represents .alpha.-position;and methods for preparing the same.Type: GrantFiled: February 21, 1991Date of Patent: April 6, 1993Assignee: Kangweon National UniversityInventors: Hyun P. Kim, Kwan S. Sin, Chang M. Kim, Moon Y. Heo, Henry J. Lee
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Patent number: 5116829Abstract: A 21-substituted steroid compound is disclosed. The compound has a structure of formula (I), ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl, lower alkenyl, lower alkoxy, or phenyl group, R.sup.2 is a hydroxyl group or an acyloxy group having 1-6 carbon atoms, R.sup.3 is a hydrogen atom or a lower alkyl group, or R.sup.2 and R.sup.3 may together form a lower alkylidenedioxy group, X.sup.1 and X.sup.2 may be the same or different and individually represents a hydrogen atom or a halogen atom, Y.sup.1 and Y.sup.2 may be the same or different and individually represents a methylene group or a sulfur atom, Z is a sulfur atom or an imino group, the wave line means that the configuration of R.sup.3 may be of either .alpha. or .beta., and dotted line between the 1 and 2 position means that the bond may be the double bond.Type: GrantFiled: April 10, 1991Date of Patent: May 26, 1992Assignee: Kao CorporationInventors: Kimihiko Hori, Yasuto Suzuki, Tomoki Morioka, Shigeru Moriwaki, Osamu Hirota, Shuichi Tsuchiya
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Patent number: 4913852Abstract: Compounds obtained from the associative synthesis of sulfur-containing or sulfur-free amino acids with derivatives of .DELTA.-4-pregnene-3,20-dione or with derivatives of .DELTA.-1,4-pregnadiene-3,20-dione of the general formulas (I), (II) and (III), having glucocorticoidal and anti-inflammatory properties have been prepared and tested. Pharmaceutical compositions, medicaments containing them as well as their applications are claimed, particularly in the cutaneous and ophthalmic fields.Type: GrantFiled: February 24, 1988Date of Patent: April 3, 1990Inventors: Catherine Milioni, Constantin Efthyimiopoulos, Bernard Koch, Louis Jung, Jean Jung