Acyclic amide and sulfonamide ligands for the estrogen receptor

Organic compounds -- part of the class 532-570 series – Organic compounds – Chalcogen in the nitrogen containing substituent

Reexamination Certificate

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

C544S059000, C544S149000, C544S159000, C546S153000, C546S232000, C548S565000, C514S422000, C514S428000

Reexamination Certificate

active

07053212

ABSTRACT:
The present invention provides estrogen receptor (ER) ligands of structural formula (I)the pharmaceutically acceptable salts, stereoisomers, and prodrugs thereof, and the pharmaceutically acceptable salts of the prodrugs, wherein R1, R2, R3, R4, R5, X, and Q are as defined herein. The invention further provides pharmaceutical compositions comprising the compounds of formula (I), and methods for treating or preventing diseases, disorders, conditions, or symptoms mediated by an ER which comprise administering to a mammalian subject in need of treatment therewith, an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt, stereoisomer, or prodrug thereof, or a pharmaceutically acceptable salt of the prodrug, or a pharmaceutical composition comprising a compound of formula (I), or a pharmaceutically acceptable salt, stereoisomer, or prodrug thereof, or a pharmaceutically acceptable salt of the prodrug. The invention further provides pharmaceutical compositions comprising combinations of the compounds of formula (I) and one or more of sodium fluoride, estrogen, a bone anabolic agent, a growth hormone or growth hormone secretagogue, a prostaglandin agonist/antagonist, and a parathyroid hormone, and methods of treating or preventing diseases, disorders, conditions, or symptoms mediated by an ER comprising the administration of an effective amount of such combination to a mammalian subject in need of treatment therewith.

REFERENCES:
patent: 4243804 (1981-01-01), Krapcho
patent: 4271188 (1981-06-01), Hindley
patent: 5296454 (1994-03-01), Goto et al.
patent: 5892114 (1999-04-01), Goldmann et al.
patent: 5958934 (1999-09-01), Berger et al.
patent: 6225316 (2001-05-01), Bos et al.
patent: 6511980 (2003-01-01), Johnson et al.
patent: 2002/0156281 (2002-10-01), Booth et al.
patent: 1122076 (1962-01-01), None
patent: 0585500 (1994-03-01), None
patent: 0873992 (1998-10-01), None
patent: 0947500 (1999-10-01), None
patent: 811130 (1959-04-01), None
patent: 2124615 (1984-02-01), None
patent: 2347422 (2000-09-01), None
patent: 04145067 (1992-05-01), None
patent: WO 9420467 (1994-09-01), None
patent: WO 9420467 (1994-09-01), None
patent: WO 0050398 (2000-08-01), None
patent: WO 0051983 (2000-08-01), None
Cummings, Jeffrey, “Drug Therapy: Alzheimer's Disease,” N. Engl. J. Med., vol. 351, pp. 56-67 (2004), especially at p. 61, 1st col., lines 31-47.
Bowman, W. Russell, et al., “Synthesis of Oxindoles by Radical Cyclisation,” Tetrahedron Letters, vol. 29(50), pp. 6657-6660 (1988) at p. 6659, lines 1-3.
Linfield, Warner, et al., “Antibacterially Active Substituted Anilides of Carboxylic and Sulfonic Acids,” J. Med. Chem., vol. 26(12), pp. 1741-1746 (Dec. 1983) at p. 1743, Table IV, compound 105.
Munusamy, R., et al., “Cathodic reduction of N-(2-iodophenyl)-N-alkylcinnamides,” J. Chem. Soc. (Perkin Trans. 2), vol. 7, pp. 1154-1166 (Jun. 11, 2001) at p. 1154, compounds 1b, 1f, 1h, 1i, 1k.
Petigara, R.B., et al., “Synthesis and Central Nervous System Depressant Activity of New Piperazine and Related Derivatives,” J. Med. Chem., vol. 12, pp. 865-870, at p. 868, Table II.
Patent Abstract of Japan Publication No. 2000072734 of Jul. 3, 2000.
Labrie, et al., “EM-652 (SCH 57068), a third generation SERM acting as pure antiestrogen in the mammary gland and endometrium”,Journal of Steroid Biochemistry and Molecular Biology69, pp. 51-84 (1999), XP-000852985.
Database Crossfire Beilstein Registry No. 2824215, abstract & J.Gen.Chem. 32, p. 712 (1962), XP-002260924.
Database Crossfire Beilstein Registry No. 405454, abstract & Yakugaku Sasshi, 86, pp. 107-109 (1966), XP002260925.

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

Acyclic amide and sulfonamide ligands for the estrogen receptor does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Acyclic amide and sulfonamide ligands for the estrogen receptor, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Acyclic amide and sulfonamide ligands for the estrogen receptor will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-3648821

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.