Thio-oxindole derivatives

Details Thio-oxindole derivatives Thio-oxindole derivatives

2005-09-20

2005-09-20

Hui, San-Ming (Department: 1617)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Cyclopentanohydrophenanthrene ring system doai

C514S336000, C514S414000, C514S418000

Reexamination Certificate

active

06946454

ABSTRACT:
This invention relates to methods of co-administering compounds of formula 1 which are agonists of the progesterone receptor which have the general structure:wherein:R1, R2, R3, R4, R5and Q1are as defined herein, or a pharmaceutically acceptable salt thereof, with estrogen, an estrogen, or an estrogen receptor agonist for contraception, hormone replacement therapy, or treating progesterone-related carcinomas and adenocarcinomas.

REFERENCES:
patent: 3635964 (1972-01-01), Skorcz
patent: 3917592 (1975-11-01), Kobzina
patent: 4093730 (1978-06-01), Butti
patent: 4440785 (1984-04-01), Walsh
patent: 4617302 (1986-10-01), Robertson
patent: 4666913 (1987-05-01), Kuhla
patent: 4670566 (1987-06-01), Walsh
patent: 4721721 (1988-01-01), Kuhla
patent: 4822794 (1989-04-01), Spada
patent: 4831027 (1989-05-01), Narr
patent: 4853473 (1989-08-01), Fischer
patent: 4933336 (1990-06-01), Martin
patent: 5007952 (1991-04-01), Kume
patent: 5171851 (1992-12-01), Kim
patent: 5414088 (1995-05-01), von der Saal
patent: 5453516 (1995-09-01), Fischer
patent: 5475020 (1995-12-01), Johnson
patent: 5521166 (1996-05-01), Grubb
patent: 5681817 (1997-10-01), Hodgen
patent: 5688808 (1997-11-01), Jones
patent: 5688810 (1997-11-01), Jones
patent: 5693646 (1997-12-01), Jones
patent: 5693647 (1997-12-01), Jones
patent: 5696127 (1997-12-01), Jones
patent: 5696130 (1997-12-01), Jones
patent: 5696133 (1997-12-01), Jones
patent: 5719136 (1998-02-01), Chwalisz
patent: 5733902 (1998-03-01), Schneider
patent: 5808139 (1998-09-01), Pathirana
patent: 5874430 (1999-02-01), Christ
patent: 6077840 (2000-06-01), Kurihara
patent: 6306851 (2001-10-01), Santilli
patent: 6319912 (2001-11-01), Grubb
patent: 6329416 (2001-12-01), Grubb
patent: 6339098 (2002-01-01), Collins
patent: 6355648 (2002-03-01), Fensome
patent: 6358947 (2002-03-01), Zhi
patent: 6358948 (2002-03-01), Zhang
patent: 6369056 (2002-04-01), Zhang
patent: 6380178 (2002-04-01), Grubb
patent: 6380235 (2002-04-01), Zhang
patent: 6391907 (2002-05-01), Fensome
patent: 6399593 (2002-06-01), Grubb
patent: 3633861 (1988-04-01), None
patent: 4330234 (1995-03-01), None
patent: 4344463 (1995-06-01), None
patent: 022317 (1981-01-01), None
patent: 208510 (1987-01-01), None
patent: 311135 (1989-04-01), None
patent: 385850 (1990-09-01), None
patent: 483077 (1991-09-01), None
patent: 454330 (1991-10-01), None
patent: 535529 (1992-09-01), None
patent: 510235 (1992-10-01), None
patent: 947507 (1999-10-01), None
patent: 978279 (2000-02-01), None
patent: 63112584 (1988-05-01), None
patent: WO86/03749 (1986-07-01), None
patent: WO91/04974 (1991-04-01), None
patent: WO91/06545 (1991-05-01), None
patent: WO93/12085 (1993-06-01), None
patent: WO94/14434 (1994-07-01), None
patent: WO94/29272 (1994-12-01), None
patent: WO95/11013 (1995-04-01), None
patent: WO95/20389 (1995-08-01), None
patent: WO95/20972 (1995-08-01), None
patent: WO95/33746 (1995-12-01), None
patent: WO96/15794 (1996-05-01), None
patent: WO96/19458 (1996-06-01), None
patent: WO96/19997 (1996-07-01), None
patent: WO97/13767 (1997-04-01), None
patent: WO97/49407 (1997-12-01), None
patent: WO98/14436 (1998-04-01), None
patent: WO98/27059 (1998-06-01), None
patent: WO98/55116 (1998-12-01), None
patent: WO99/10325 (1999-03-01), None
patent: WO99/11264 (1999-03-01), None
patent: WO99/15500 (1999-04-01), None
patent: WO99/44608 (1999-09-01), None
Katzung, Basic & Clinical Pharmacology, 6thed., p. 620, Table 39-3.
R. Evans, “The Steroid and Thyroid Hormone Receptor Superfamily”, Science, 240:889 (May 13, 1988).
A. Ulmann et al, “Clinical Uses of Mifepristone (MFP)”, Ann. N.Y. Acad. Sci., 261:248 (Jun. 12, 1995).
R. Kekkonen et al, “Sequential Regiment of the Antiprogesterone RU486 and Synthetic Progestin for Contraception”, Fertility and Sterility, 60(4):610 (Oct., 1993).
K. Horwitz et al, “Progestin, Progesterone Receptors, and Breast Cancer”, Horm. Cancer, publisher: Birkhaeuser, Boston, Mass., ed. Vedeckis, pp. 283-306 (1996) (abstrct only).
A. Murphy et al, “Regression of Uterine Leiomyomata in Response to the Antiprogesterone RU486”, J. Clin. Endo. Metab., 76(2):513 (Feb., 1993).
L. Kettel et al, “Endocrine Responses to Long-Term Administration of the Antiprogesterone RU486 in Patients with Pelvic Endometriosis”, Fertility and Sterility, 56(3):402 (Sep., 1991).
H. Michna et al, “Differentiation Therapy with Progesterone Antagonists”, Ann. N.Y. Acad. Sci., 761:224 (Jun., 1995).
L. Zhi et al, “5-Aryl-1,2-Dihydrochromeno[3,4-f]quinolines: A Novel Class of Nonsteroidal Human Progesterone Receptor Agonists”, J. Med. Chem., 41(3):291 (Oct. 22, 1998).
D. Combs et al, “Nonsteroidal Progesterone Receptor Ligands. 2. High-Affinity Ligands with Selectivity for Bone Cell Progesterone Receptors”, J. Med. Chem., 38:4880 (Dec. 8, 1995).
K. Perlman et al, “20-Oxopregnacalciferols: Vitamin D Compounds that Bind the Progesterone Receptor”, Tet. Letters, 35(15)2295 (1994).
L. Hamann et al, “Synthesis and Biological Activity of Novel Nonsteroidal Progesterone Receptor Antagonists”, Ann. N.Y. Acad. Sci., 761:383 (Jun. 12, 1995).
R. Chen et al, “Synthesis and SAR of a Novel Series of Spirobenzothlzaepine Derivatives with Antiprogestin Activity”, POI-37, 16thInt. Cong. Het. Chem., Montana (1997).
B. Narr et al, “Preparation, Testing, and Formulation of Imidazobenzoxazinones as Cardiotonics”, Chemical Abstracts, 109:22973 (1988).
R. Hartmann et al, “Effects of Brofoxine, A New Anxiolytic on Experimentally Induced Conflict in Rats”, Proc. West. Pharmacol. Soc., 21:51-55 (1978).
B. Singh et al, “Novel cAMP PDE III Inhibitor” Imidazo[4,5-b]pyridin-2(3H)-ones and Thiazolo[4,5-b]pyridin-2(3H)-ones and their Analogs, J. Med. Chem., 37:248 (Jan. 21, 1994).
A. Andreani et al, “Potential Antitumor Agents XVII (I). Cytotoxic Agents from Indole Derivatives and their Intermediates”, Acta. Pharm. Nord., 2(6):407 (1990).
Sakata et al, “Silver Halide Photographic Materials Useful for Platemaking”, Chemical Abstracts, 123:301431 (1993).
P. Pflegel et al, “Polarografie con 7-Chlor-5-phenyl-2-thioxo-1H-2,3-dihydro-1,3,4-benzotriazepinen”, Pharmazie, 37(10):714-717 (1982).
E. Barengolts et al, “Progesterone Antagonist RU486 has Bone-Sparing Effects in Ovariectomized Rats”, Bone, 17(1):21 (Jul., 1995).
E. Gromachevskaya et al, “Studies of 4H-3, 1-Benzoxazines”, Chem. Heterocycl. Cmpds., 33(10):1209-1214 (1997).
D. Chiarino et al, “2,1-Benzisothiazoline 2,2-Dioxide and Derivatives”, J. Heterocycl. Chem., 23(6):1645-1649 (Nov.-Dec., 1986).
A. Turck et al, “On the Metabolism of 3-Substituted and 3,6-Disubstituted Pyridazines”, Tetrahedron, 49(3):599-606 (1993).
V. Kumar et al, “Synthesis of 7-Azaindole and 7-Azaoxindole Derivatives through a Palladium-Catalyzed Cross-Coupling Reaction”, J. Org. Chem., 57(25):6995-6998 (1992).
P. Canonne et al, “Spirocyclization of 1-(o-Aminophenyl)cycloalkanols and 1-(2′-Amino-3′-pyridinyl)cycloalkanols”, J Heterocyclic Chem., 26:113 (Jan.-Feb., 1989).
M-C. Forest et al, “A Novel Class of Cardiotonic Agents: Synthesis and Biological Evaluation of 5-Substituted 3,6-Dihydrothiadiazin-2-ones with Cyclic AMP Phosphodiesterase Inhibiting and Myofibrillar Calcium Sensitizing Properties”, J. Med. Chem., 35:163-172 (Jan., 1992).
D. Combs et al, “Heteroatom Analogues of Bemoradan: Chemistry and Cardiotonic Activity of 1,4-Benzothiazinylpyridazinones”, J. Med. Chem., 35:172-176 (Jan., 1992).
Kurihari et al., “Synthesis of (±)-PF1092A, B, and C; New Nonsteroidal Progesterone Receptor Ligands”, J. Antibiotics, 50(4):360 (Apr., 1997).
A. Kende et al., “Regioselective C-3 Alkylation of Oxindole Dianion”, Synth. Commun. 12(1):1 (1982).
T. Tucker et al., “Synthesis of a Series of 4-(Arylethylnyl)-6-Chloro-4-Cyclopropyl-3,4-dihydroquinazolin-2(

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