Anti-inflammatory androstane derivatives

Details Anti-inflammatory androstane derivatives Anti-inflammatory androstane derivatives

2005-04-12

2005-04-12

Badio, Barbara P. (Department: 1616)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Cyclopentanohydrophenanthrene ring system doai

C540S108000, C540S114000

Reexamination Certificate

active

06878698

ABSTRACT:
According to one aspect of the invention, there is provided a pharmaceutical formulation for administration by inhalation comprising a compound of formula (I),whereinR1represents C1-6alkyl or C1-6haloalkyl;R2represents —C(═O)-aryl or —C(═O)-heteroaryl;R3represents hydrogen, methyl (which may be in either the α or β configuration) or methylene;R4and R5are the same or different and each represents hydrogen or halogen; andimg id="CUSTOM-CHARACTER-00001" he="3.13mm" wi="6.01mm" file="US06878698-20050412-P00900.TIF" alt="custom character" img-content="character" img-format="tif" ?represents a single or a double bond;and salts and solvates thereof together with a long-acting β2-adrenoreceptor agonist which formulation has a therapeutically useful effect in the treatment of COPD over a period of 24 hours or more.

REFERENCES:
patent: 3067197 (1962-12-01), Agnello et al.
patent: 3639434 (1972-02-01), Oxley et al.
patent: 3828080 (1974-08-01), May et al.
patent: 3856828 (1974-12-01), Phillips et al.
patent: 3981894 (1976-09-01), Phillips et al.
patent: 3989686 (1976-11-01), Phillips et al.
patent: 4093721 (1978-06-01), Phillips et al.
patent: 4187301 (1980-02-01), Edwards
patent: 4188385 (1980-02-01), Edwards
patent: 4198403 (1980-04-01), Alvarez
patent: 4261984 (1981-04-01), Alvarez
patent: 4263289 (1981-04-01), Edwards
patent: 4267173 (1981-05-01), Draper
patent: 4285937 (1981-08-01), Kalvoda
patent: 4310466 (1982-01-01), Edwards
patent: 4335121 (1982-06-01), Phillipps et al.
patent: 4377575 (1983-03-01), Phillips et al.
patent: 4472393 (1984-09-01), Shapiro
patent: 4607028 (1986-08-01), Schmidlin
patent: 4710495 (1987-12-01), Bodor
patent: 4861765 (1989-08-01), Mitsukuchi et al.
patent: 4992474 (1991-02-01), Skidmore et al.
patent: 4994439 (1991-02-01), Longenecker et al.
patent: 4996335 (1991-02-01), Bodor
patent: 5250293 (1993-10-01), Gleich
patent: 5420120 (1995-05-01), Boltralik
patent: 5658549 (1997-08-01), Akehurst et al.
patent: 5707984 (1998-01-01), Tjoeng et al.
patent: 5837699 (1998-11-01), Sequeira et al.
patent: 5849265 (1998-12-01), Li-Bovet et al.
patent: 5889015 (1999-03-01), Sequeira et al.
patent: 5919776 (1999-07-01), Hagmann et al.
patent: 5972920 (1999-10-01), Seidel
patent: 5981517 (1999-11-01), Bodor
patent: 6057307 (2000-05-01), Sequeira et al.
patent: 6127353 (2000-10-01), Yuen et al.
patent: 6136294 (2000-10-01), Adjei et al.
patent: 6197761 (2001-03-01), Biggadike et al.
patent: 6261539 (2001-07-01), Adjei et al.
patent: 6395300 (2002-05-01), Straub et al.
patent: 20020081266 (2002-06-01), Woolfe et al.
patent: 20020103392 (2002-08-01), Stache et al.
patent: 20020165211 (2002-11-01), Biggadike et al.
patent: 20020173496 (2002-11-01), Biggadike
patent: 20020177581 (2002-11-01), Biggadike
patent: 20030073676 (2003-04-01), Biggadike et al.
patent: 20030109511 (2003-06-01), Biggadike et al.
patent: 20030144257 (2003-07-01), Biggadike et al.
patent: 20030158163 (2003-08-01), Cuenoud et al.
patent: 2336693 (1975-02-01), None
patent: 2538569 (1977-03-01), None
patent: 0004773 (1979-10-01), None
patent: 0057401 (1982-08-01), None
patent: 0057401 (1982-08-01), None
patent: 0135476 (1985-03-01), None
patent: 0179583 (1986-04-01), None
patent: 0416951 (1991-03-01), None
patent: 0418716 (1991-03-01), None
patent: 0521455 (1993-01-01), None
patent: 0640616 (1995-03-01), None
patent: 0646593 (1995-04-01), None
patent: 580494 (1986-10-01), None
patent: 1384372 (1975-02-01), None
patent: 1438940 (1976-06-01), None
patent: 1517278 (1978-07-01), None
patent: 2079755 (1982-01-01), None
patent: 2140800 (1984-12-01), None
patent: 109656 (1998-02-01), None
patent: 04208267 (1992-07-01), None
patent: 9214472 (1992-09-01), None
patent: 9421229 (1994-09-01), None
patent: 9531964 (1995-11-01), None
patent: 9619199 (1996-06-01), None
patent: 9705136 (1997-02-01), None
patent: 9715298 (1997-05-01), None
patent: 9724365 (1997-07-01), None
patent: 9746243 (1997-12-01), None
patent: 9817676 (1998-04-01), None
patent: 9834596 (1998-08-01), None
patent: 9843630 (1998-10-01), None
patent: 9901467 (1999-01-01), None
patent: 9925359 (1999-05-01), None
patent: 9932089 (1999-07-01), None
patent: 0016814 (2000-03-01), None
patent: 0033892 (2000-06-01), None
patent: 0038811 (2000-07-01), None
patent: 0104118 (2001-01-01), None
patent: 0115744 (2001-03-01), None
patent: 0120331 (2001-03-01), None
patent: 0154664 (2001-08-01), None
patent: 0162722 (2001-08-01), None
patent: 0178736 (2001-10-01), None
patent: 0178739 (2001-10-01), None
patent: 0178741 (2001-10-01), None
patent: 0178745 (2001-10-01), None
patent: 0200199 (2002-01-01), None
patent: 0200679 (2002-01-01), None
patent: 02007767 (2002-01-01), None
patent: 02008243 (2002-01-01), None
patent: 0212265 (2002-02-01), None
patent: 0212266 (2002-02-01), None
patent: 02013868 (2002-02-01), None
patent: 0226723 (2002-04-01), None
patent: 02053186 (2002-07-01), None
patent: 02066422 (2002-08-01), None
patent: 02070490 (2002-09-01), None
patent: 02076933 (2002-10-01), None
patent: 02085296 (2002-10-01), None
patent: 02088167 (2002-11-01), None
patent: 02100879 (2002-12-01), None
patent: 03013427 (2003-02-01), None
patent: 03033000 (2003-04-01), None
patent: 03035668 (2003-05-01), None
patent: 03040691 (2003-05-01), None
patent: 03042229 (2003-05-01), None
patent: 03042230 (2003-05-01), None
patent: 872389 (1987-04-01), None
Janette M. Mahoney et al., “Drug effects on the neovascularization to silver nitrate cauterization of the rat cornea” Current Eye Research, vol. 4, No. 5, 1985, pp. 531-535.
Richard A. Kenley et al., “An Automated, Column-Switching HPLC Method for Analyzing Active and Excipient Materials in Both Cream and Ointment Formulations,” Drug Development and Industrial Pharmacy, vol. 11 (9&10), 1985, pp. 1781-1796.
R. Woodford et al., “Activity and bioavailability of a new steroid (Timobesone acetate) in cream and ointment compared with Lidex and Dermovate creams and ointments and Betnovate cream” Int'l Journal of Pharmaceutics, vol. 26 (1985) pp. 145-155.
Denis J. Kertesz et al., “Thiol Esters from Steroid 17β-Carboxylic Acids: Carboxylate Activation and Internal Participation by a 17 α-Acylates” J. Org. Chem., vol. 51, 1986, pp. 2315-2328.
John T. H. Ong et al., “Micellar Solubilization of Timobesone Acetate in Aqueous and Aqueous Propylene Glycol Solutions of Ninionic Surfactants”, Pharmaceutical Research, vol. 5, No. 11, 1988, pp. 704-708.
John T. H. Ong et al., Intrinsic Potencies of Novel Thiol Ester Corticosteroids RS-85095 and RS-21314 as Compared With Clobetasol 17-Propionate and Fluocinonide Arch Dermatol, vol. 125, Dec. 1989, pp. 1662-1665.
S.J. Lane et al., “Evaluation of a New Capillary Electrochromatography/Mass Spectrometry Interface Using Short Columns and High Field Strengths for Rapid and Efficient Analyses,” Rapid Communications in Mass Spectrometry, vol. 10, 1996, pp. 733-736.
Franklin I. Aigbirthio et al., “Automated Radiosynthesis of No-carrier-added [S-fluoromethyl-18F]Fluticasone Propionate as a Radiotracer for Lung Deposition Studies with PET” Journal of Labelled Compounds and Radiopharmaceuticals, vol. 39, No. 7, 1997, pp. 569-584.
Nisha Mistry et al., “Characterisation of impurities in bulk drug batches of fluticasone propionate using directly coupled HPLC-NMR spectroscopy and HPLC-MS,” Journal of Pharmaceutical and Biomedical Analysis vol. 16, 1997, pp. 697-705.
Knobil, K., et al., “Adding Salmeterol Is More Effective Than Increasing The Dose Of Fluticasone For Patients With Asthma Who Are Symptomatic On Low Dose Fluticasone,” European Respiratory review, Copenhagen, DK, vol. 12, No. SUPPL 29 Dec. 1998, pp. 19S-20S, XP000992769.
Nisha Mistry et al., Impurity profiling in bulk pharmaceutical batches uing 19F NMR spectroscopy and distinction between monomeric and dimeric impurities by NMR-based diffusion measurements, Journal of Pharmaceutical and Biomedical Analysis, vol. 19, 1999, pp. 511-517.
N. Smith et al., “Compari

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