Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-06-09
1999-09-14
Raymond, Richard L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514432, 514456, 546169, 546170, 546171, 546173, 549 49, 549 51, 549 57, 549 58, 549404, 549405, 549406, C07D21516, C07D31158, C07D33506, A61K 3135
Patent
active
059523450
ABSTRACT:
Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity. These assays are based on the ability of negative hormones to down-regulate the activity of chimeric retinoid receptors engineered to possess a constitutive transcription activator domain.
REFERENCES:
patent: 4096341 (1978-06-01), Frazer
patent: 4326055 (1982-04-01), Loeliger
patent: 4391731 (1983-07-01), Boller et al.
patent: 4485252 (1984-11-01), Fuchs et al.
patent: 4539154 (1985-09-01), Krebs
patent: 4695649 (1987-09-01), Magami et al.
patent: 4723028 (1988-02-01), Shudo
patent: 4739098 (1988-04-01), Chandraratna
patent: 4740519 (1988-04-01), Shroot et al.
patent: 4810804 (1989-03-01), Chandraratna
patent: 4826969 (1989-05-01), Maignan et al.
patent: 4826984 (1989-05-01), Berlin et al.
patent: 4833240 (1989-05-01), Maignan et al.
patent: 4855320 (1989-08-01), Chatterjee et al.
patent: 4895868 (1990-01-01), Chandraratna
patent: 4923884 (1990-05-01), Chandraratna
patent: 4927947 (1990-05-01), Chandraratna
patent: 4980369 (1990-12-01), Chandraratna
patent: 4992468 (1991-02-01), Chandraratna
patent: 5006550 (1991-04-01), Chandraratna
patent: 5013744 (1991-05-01), Chandraratna
patent: 5015658 (1991-05-01), Chandraratna
patent: 5023341 (1991-06-01), Chandraratna
patent: 5037825 (1991-08-01), Klaus et al.
patent: 5045551 (1991-09-01), Chandraratna
patent: 5053523 (1991-10-01), Chandraratna
patent: 5068252 (1991-11-01), Chandraratna
patent: 5089509 (1992-02-01), Chandraratna
patent: 5130335 (1992-07-01), Chandraratna
patent: 5134159 (1992-07-01), Chandraratna
patent: 5162546 (1992-11-01), Chandraratna
patent: 5175185 (1992-12-01), Chandraratna
patent: 5183827 (1993-02-01), Chandraratna
patent: 5202471 (1993-04-01), Chandraratna
patent: 5231113 (1993-07-01), Chandraratna
patent: 5234926 (1993-08-01), Chandraratna
patent: 5248777 (1993-09-01), Chandraratna
patent: 5264456 (1993-11-01), Chandraratna
patent: 5264578 (1993-11-01), Chandraratna
patent: 5272156 (1993-12-01), Chandraratna
patent: 5278318 (1994-01-01), Chandraratna
patent: 5310662 (1994-05-01), Evans et al.
patent: 5324744 (1994-06-01), Chandraratna
patent: 5324840 (1994-06-01), Chandraratna
patent: 5326898 (1994-07-01), Chandraratna
patent: 5344959 (1994-09-01), Chandraratna
patent: 5346895 (1994-09-01), Chandraratna
patent: 5346915 (1994-09-01), Chandraratna
patent: 5348972 (1994-09-01), Chandraratna
patent: 5348975 (1994-09-01), Chandraratna
patent: 5349105 (1994-09-01), Chandraratna
patent: 5354752 (1994-10-01), Chandraratna
patent: 5354776 (1994-10-01), Chandratatna
patent: 5380877 (1995-01-01), Chandraratna
patent: 5391753 (1995-02-01), Chandraratna
patent: 5399561 (1995-03-01), Chandraratna
patent: 5399586 (1995-03-01), Davies et al.
patent: 5407937 (1995-04-01), Chandraratna
patent: 5414007 (1995-05-01), Chandraratna
patent: 5420145 (1995-05-01), Shudo
patent: 5426118 (1995-06-01), Chandraratna
patent: 5434173 (1995-07-01), Chandraratna
patent: 5451605 (1995-09-01), Chandraratna et al.
patent: 5455265 (1995-10-01), Chandraratna
patent: 5466861 (1995-11-01), Dawson et al.
patent: 5468879 (1995-11-01), Chandraratna
patent: 5470999 (1995-11-01), Chandraratna
patent: 5475022 (1995-12-01), Chandraratna
patent: 5475113 (1995-12-01), Chandraratna
patent: 5489584 (1996-02-01), Vuligonda et al.
patent: 5498755 (1996-03-01), Chandraratna et al.
patent: 5498795 (1996-03-01), Song et al.
patent: 5514825 (1996-05-01), Vuligonda et al.
patent: 5516904 (1996-05-01), Chandraratna
patent: 5523457 (1996-06-01), Starrett, Jr. et al.
patent: 5534516 (1996-07-01), Chandraratna
patent: 5534641 (1996-07-01), Song et al.
patent: 5543534 (1996-08-01), Vuligonda et al.
patent: 5556996 (1996-09-01), Beard et al.
patent: 5559248 (1996-09-01), Starrett, Jr. et al.
patent: 5563292 (1996-10-01), Sheh et al.
patent: 5571696 (1996-11-01), Evans et al.
patent: 5578483 (1996-11-01), Evans et al.
patent: 5591858 (1997-01-01), Vuligonda et al.
patent: 5599819 (1997-02-01), Chandraratna
patent: 5599967 (1997-02-01), Vuligonda et al.
patent: 5602130 (1997-02-01), Chandraratna
patent: 5602135 (1997-02-01), Chandraratna
patent: 5605915 (1997-02-01), Vuligond et al.
patent: 5616597 (1997-04-01), Chandraratna
patent: 5616712 (1997-04-01), Teng et al.
patent: 5618836 (1997-04-01), Chandraratna et al.
patent: 5618839 (1997-04-01), Starrett, Jr. et al.
patent: 5618931 (1997-04-01), Beard et al.
patent: 5618943 (1997-04-01), Vuligonda et al.
patent: 5648385 (1997-07-01), Starrett, Jr. et al.
patent: 5648503 (1997-07-01), Vuligonda et al.
patent: 5648514 (1997-07-01), Johnson et al.
patent: 5654469 (1997-08-01), Vuligonda et al.
patent: 5663347 (1997-09-01), Chandraratna
patent: 5663357 (1997-09-01), Teng et al.
patent: 5663367 (1997-09-01), Vuligonda et al.
patent: 5672710 (1997-09-01), Beard et al.
patent: 5675024 (1997-10-01), Teng et al.
patent: 5675033 (1997-10-01), Vuligonda et al.
patent: 5677320 (1997-10-01), Chandraratna
patent: 5677323 (1997-10-01), Chandraratna
patent: 5677451 (1997-10-01), Chandraratna
patent: 5688957 (1997-11-01), Teng et al.
patent: 5696162 (1997-12-01), Chandraratna
patent: 5698700 (1997-12-01), Song et al.
patent: 5717094 (1998-02-01), Chandraratna
patent: 5723666 (1998-03-01), Vuligonda et al.
patent: 5728846 (1998-03-01), Vuligonda et al.
patent: 5741896 (1998-04-01), Vuligonda et al.
patent: 5747542 (1998-05-01), Vuligonda et al.
patent: 5763635 (1998-06-01), Vuligonda et al.
patent: 5773594 (1998-06-01), Johnson et al.
Agarwal, et al., Cancer Research, 54,pp.2108-2112.
Hembree, et al., Cancer Research, 54, pp. 3160-3166.
A General Synthesis of Terminal and Internal Arylalkynes by the Palladium-Catalyzed Reaction of Alkynylzinc Reagents with Aryl Halides by Anthony O. King and Ei-itchi, J. Org. Chem., (1978) 43/2: p. 358.
Conversion of Methyl Ketones into Terminal Acetylenes and (E)-Tri-substituted Olefins of Terpenoid Origin by Ei-ichi, et al., J. Org. Chem., (1980) 45/12: p.2526.
Sporn et al. in J. Amer. Acad. Derm.., (1986) 15:756-764.
"A Convenient Synthesis of Ethynylarenes and Diethynylarenes" by S. Takahashi et al. Synthesis (1980) pp.627-630.
Shudo et al. in Chem. Phar. Bull., (1985) 33:404-407.
Kagechika et al. in J. Med. Chem., (1988) 31:2182-2192.
Chemistry and Biology of Synthetic Retinoids by Marcia I. Dawson and William H. Okamura, published by CRC Press Inc., 1990, pp. 334-335, 354.
Synthesis of 2,2'-Diacyl-1,1'-Biaryls. Regiocontrolled Protection of . . . by Mervic, et al, J. Org. Chem.,(1980) No. 45, pp.4720-4725.
A Dopsmine Receptor Model and Its Application in the Design of a New Class American Chemical Societe, (1981) 24/9:1026-1031.
6.2.3 Conformational Restriction, Williams, et al., Drug Discovery and Development, The Humana Press, (1987) pp. 54-55.
V. Retinoid Structure-Biological Activity Relationships, Chemistry and Biology of Synthetic Retinoids, (1990) pp. 324-356.
Davis et al. J. Organomettalic Chem (1990) 387:381-390.
"Effects of 13-Cis-Retinoic Acid, All Trans-Retinoic Acid, and Acitretin on the Proliferation, Lipid Synthesis and Keratin Expression of Cultured Human Sebocytes in Vitro" C.C. Zouboulis, The Journal of Investigative Dermatology, (1991) 96/5:792-797.
"Organ Maintenance of Human Sebaceous Glands: in Vit
Beard Richard L.
Chandraratna Roshantha A.
Duong Tien T.
Gillett Samuel J.
Johnson Alan T.
Allergan Sales Inc.
Baran Robert J.
Rao Deepak R.
Raymond Richard L.
Szekeres Gabor L.
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