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Title: US5710275: 7β-substituted-4-aza-5α-androstan-3-ones as 5α-reductase inhibitors
[ Derwent Title ]


Country: US United States of America

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95 pages

 
Inventor: Bakshi, Raman K.; Edison, NJ
Rasmusson, Gary H.; Watchung, NJ
Tolman, Richard L.; Warren, NJ
Patel, Gool F.; Califon, NJ
Harris, Georgianna S.; Tinton Falls, NJ
Graham, Donald W.; Mountainside, NJ
Witzel, Bruce E.; Westfield, NJ

Assignee: Merck & Co., Inc., Rahway, NJ
other patents from MERCK + CO., INC. (367520) (approx. 5,201)
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Published / Filed: 1998-01-20 / 1995-04-03

Application Number: US1995000341602

IPC Code: Advanced: A61K 31/565; A61P 13/02; A61P 15/00; A61P 17/00; A61P 43/00; C07C 59/82; C07C 59/90; C07J 51/00; C07J 73/00;
IPC-7: A61K 31/47;

ECLA Code: C07C59/82; C07C59/90; C07J51/00; C07J73/00B2;

U.S. Class: Current: 546/078; 546/077;
Original: 546/078; 546/077; 514/284;

Field of Search: 546/077,78 514/284

Priority Number:
1995-04-03  US1995000341602
1992-05-20  US1992000886572
1993-05-14  WO1993US0004643

Abstract:     PCT No. PCT/US93/04643 Sec. 371 Date Apr. 3, 1995 Sec. 102(e) Date Apr. 3, 1995 PCT Filed May 14, 1993 PCT Pub. No. WO93/23420 PCT Pub. Date Nov. 25, 1993Described are new 7 beta -substituted 4-aza-5 alpha -androstan-3-ones and related compounds as 5 alpha -reductase inhibitors.

Attorney, Agent or Firm: Fitch, Catherine D. ; Nicholson, William H. ; Winokur, Melvin ;

Primary / Asst. Examiners: Daus, Donald G.;

Maintenance Status: E2 Expired  Check current status

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Related Applications:
Application Number Filed Patent Pub. Date  Title
US1992000886572 1992-05-20       


       
Parent Case:

CROSS REFERENCE TO RELATED APPLICATIONS
    This application is a national phase application under 35 U.S.C. §371 of PCT application Ser. No. PCT/US93/04643, filed May 14, 1993, which, in turn is a continuation in part of application Ser. No. 07/886,572 filed May 20, 1992, now abandoned.

Designated Country: BB BG BR CZ FI HU KR KZ LK MG MN MW NO NZ OA PL RO RU  BE CH FR GB IE IT LI LU NL PT 

Family: Show 26 known family members

First Claim:
Show all 2 claims
What is claimed is:     1. A compound of structural formula [Figure] selected from the group consisting of those in the following table:
______________________________________
R A
______________________________________
[Figure]
CH3
[Figure]
CH3
[Figure]
CH3
[Figure]
CH3
[Figure]
CH3
[Figure]
CH3
[Figure]
______________________________________


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Description: Show description

PCT Number: PCT/US93/04643    WO9323420

PCT Pub./Filed Dates: 1993-11-25 / 1993-05-14

§ 371 / 102(e) Dates: 1995-04-03 / 1995-04-03

Forward References: Show 6 U.S. patent(s) that reference this one

       
U.S. References: Go to Result Set: All U.S. references   |  Forward references (6)   |   Backward references (17)   |   Citation Link

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Patent  Pub.Date  Inventor Assignee   Title
Get PDF - 16pp US4220775  1980-09 Rasmusson et al.  Merck & Co., Inc. Preparation of 4-aza-17-substituted-5α-androstan-3-ones useful as 5α-reductase inhibitors
Get PDF - 16pp US4377584  1983-03 Johnston et al.  Merck & Co., Inc. 4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors
Get PDF - 8pp US4760071  1988-07 Rasmusson et al.  Merck & Co., Inc. 17β-N-monosubstituted carbamoyl-4-aza-5α-androst-1-en-3-ones which are active as testosterone 5α-reductase inhibitors
Get PDF - 7pp US4859681  1989-08 Rasmusson et al.  Merck & Co., Inc. 17 α-Acyl-4-aza-5a-androst-1-en-3-ones as 5 alpha-reductase inhibitors
Get PDF - 7pp US5049562  1991-09 Rasmusson et al.  Merck & Co., Inc. 17β-acyl-4-aza-5α-androst-1-ene-3-ones as 5α-reductase inhibitors
Get PDF - 8pp US5138063  1992-08 Rasmusson et al.  Merck & Co., Inc. 17β-methoxycarbonyl-4-aza-androsten-1-en-3-ones
Get PDF - 7pp US5215894  1993-06 Arison et al.  Merck & Co., Inc. Biological process for producing 17β-N-monosubstituted carbamoyl-11-oxo-4-aza-5-α-androst-3-one testosterone-5-α reductase inhibitors
Get PDF - 13pp US5237064  1993-08 Bakshi et al.  Merck & Co., Inc. Process for producing 7β-substituted-aza-5αandrostan-3-ones
Get PDF - 15pp US5278159  1994-01 Bakshi et al.  Merck & Co., Inc. Aryl ester derivatives of 3-oxo-4-aza-androstane 17-β-carboxylates as 5-α-reductase inhibitors
Get PDF - 5pp US5300294  1994-04 Johnson  SmithKline Beecham Corporation Method of treating prostatic adenocarcinoma
Get PDF - 51pp US5302621  1994-04 Kojima et al.  Sankyo Company, Limited Azasteroid compounds for the treatment of prostatic hypertrophy, their preparation and use
Get PDF - 24pp US5494914  1996-02 Labrie  Endorecherche Inhibitors for testosterone 5α-reductase activity
Get PDF - 25pp US5510351  1996-04 Graham et al.  Merck & Co., Inc. Delta-17 and delta-20 olefinic and saturated 17 beta-substituted 4-aza-5 alpha-androstan-ones as 5 alpha reductase inhibitors useful in the prevention and treatment of hyperandrogenic disorders
Get PDF - 22pp US5510485  1996-04 Graham et al.  Merck & Co., Inc. 17-ester, amide, and ketone derivatives of 3-oxo-4-azasteroids as 5A-reductase inhibitors
Get PDF - 22pp US5527807  1996-06 Bakshi et al.  Merck & Co., Inc. 7β-substituted-4-aza-5α-cholestan-3-ones as 5α reductase inhibitors useful in the prevention and treatment of hyperandrogenetic disorders
Get PDF - 23pp US5536727  1996-07 Witzel et al.  Merck & Co., Inc. 17-Ethers and thioethers of 4-aza-steroids
Get PDF - 56pp US5543417  1996-08 Waldstreicher  Merck & Co., Inc. Combination method of treating acne using 4-AZA-5α-cholestan-ones and 4-AZA-5α-androstan-ones as selective 5α-reductase inhibitors with anti-bacterial, keratolytic, or anti-inflammatory agents
       
Foreign References:
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Publication Date IPC Code Assignee   Title
Get PDF - 44pp EP0004949 1979-10  C07J 3/00 Merck & Co., Inc. 4-Aza-17-substituted-5-alpha-androstan-3-one, their A and D homo analogs, process for their preparation and pharmaceutical compositions containing them 
Get PDF - 22pp EP0155096 1985-09  C07D 213/00 MERCK & CO INC 17 Beta-Substituted-4-aza-5-alpha-androstenones and their use as 5-alpha-reductase inhibitors 
Get PDF - 32pp EP0277002 1988-08  A61K 31/58 SMITHKLINE BECKMAN CORP Steroid-5-alpha-reductase inhibitors 
Get PDF - 11pp EP0314199 1989-05  C07J 73/00 MERCK & CO. INC. 17 Beta-substituted-4-aza-5 alpha-androstenones and their use as 5 alpha-reductase inhibitors 
Get PDF - 49pp EP0375349 1990-06  A61K 31/56 SMITHKLINE BEECHAM CORP Phosphinic acid substituted steroids as inhibitors of steroid 5alpha-reductase 
Get PDF - 21pp EP0414529 1991-02  C07J 3/00 SMITHKLINE BEECHAM CORPORATION Substituted steroid derivatives 
Get PDF - 14pp EP0547691 1993-06  A61K 31/58 MERCK & CO INC The use of 17B-N-mono-substituted-carbamoyl-4-aza-5alpha-androst-1-en-3-ones for the preparation of a medicament for the prevention of prostatic carcinoma 
Get PDF - 93pp WO9313124 1993-07  A61K 8/63 ANDREWS, Robert, Carl INHIBITORS OF 5-ALPHA-TESTOSTERONE REDUCTASE 
Get PDF - 359pp WO9323420 1993-11  A61K 31/565 BAKSHI RAMAN K NEW 7 beta -SUBSTITUTED-4-AZA-5 alpha -ANDROSTAN-3-ONES AS 5 alpha -REDUCTASE INHIBITORS 


Other Abstract Info: CHEMABS 121(23)280955G CAN128(12)140893E CHEMABS 128(12)140893E DERABS C93-386471

Other References:
  • The Daily (Tuesday, May 7, 1996), "New Data on Proscar, Abbott's Hytrin Show Conflicting Results".
  • Winslow Wall Street Journal (Tuesday, May 7, 1996), "Study Finds Abbott's Prostate Drug is Much More Effective than Merck's", p. B4.
  • US NEWS & WORLD REPORT, May 20, 1996, "Zapping a problem prostate".
  • Rasmusson et al., J. Med Chem., vol. 29, No. 11, pp. 2298-2315(1986), "Azasteroids: Structure-activity relationships for inhibition of 5alpha-reductase and of androgen receptor binding". (18 pages) Cited by 79 patents
  • Mellin et al., J. Steroid Biochem. Mol. Biol., vol. 44, No. 2, pp.121-131(1993), "Azasteroids as inhibitors of testosterone 5alpha-reductase in mammalian skin". (11 pages) Cited by 15 patents [ISI abstract]
  • Geldof et. al., "Enzyme Inhibitors in Hormone Dependent Prostate Cancer Treatment"Abstract 90-28432, Abstracted from Eur. J. Cancer 26(2): 188 (1990). (1 pages) Cited by 9 patents
  • Geldof, "Consideration of the Use of 17 beta-N, N-diethylcarbamoyl-4-methyl-4-aza-5-alpha-androstan-3-one(HMA), a 5 alpha-reductase inhibitor, in prostate cancer therapy"J. Cancer Res. Oncol. 118: 50-55 (1992). (6 pages) Cited by 15 patents [ISI abstract]
  • Diani, et al. "Hair Growth Effects of Oral Administration of Finasteride, A steroid 5 alpha-reductase inhibitor, alone and in combination with Topical Minoxidil in the Balding Stumptail Macaque", J. Clin. Endo. & Metab. 74(2):345-350 (1992). (6 pages) Cited by 29 patents [ISI abstract]
  • Rasmusson et al., "Azasteroids" Structure Activity Relationships for Inhibition of 5 alpha-reductase and of androgen receptor binding, J. Med. Chem. 29(11): 2298-2315 (1986). (18 pages) Cited by 79 patents
  • Brooks, et al., "5 Alpha-reductase Inhibitory and Anti-Androgenic Activities of Some 4-Aza-steroids in the rat" Steroids: Structure Function and Regulation vol. 47(1). . . 1-19(1986). (19 pages) Cited by 51 patents
  • Burger, Medicinal Chemistry, 2nd Ed. New York, Interscience p. 42 (1960).
  • Helliker, "Alopecia Sufferers Seek to Suffer Less, and Not In Silence" Wall Street Jour. pp. A1 and A7, Jun. 7, 1991.
  • Back "Oxidation of Azasteroid Lactams and Alcohols with Benzeneseleninic Anhydride". J. Org. Chem. 46(7); 1442-1446 (1981).
  • Back et al., "N-Chloroazasteroids: A Novel Class of Reactive Steroid Analogues Preparation, Reaction with Thiols and Photochemical Conversion to Electrophilic N-acylamines", J. Org. Chem. 54(8):1904-1910 (1989). (7 pages) Cited by 13 patents
  • Stinson, "Prostate Drug Proscar cleared for Marketing", Chem. Eng. News pp. 7-8, 29 Jun. 1992. (2 pages) Cited by 36 patents [ISI abstract]
  • Gormley, "Preparation of 17-Beta carbamoyl-4-aza-5 alpha-androstan-1-en-3-ones as testosterone 5 alpha reductase inhibitors for the prevention of prostatic carcinoma", Chem. Abstrs. vol. 119, Entry 160644S, Abstracting EP 547691 (1993).
  • Li et al., J. Med. Chem. 1995, 38, pp.1158-1173, "Synthesis and in Vitro Activity 0f 17Beta-(N-alkyl/arylform amido)-and 17Beta-[N-alkyl/aryl)alky/arylamido]-4-methyl-4-aza-3-oxo-5alpha-androstan-3-ones as Inhibitors of Human 5alpha-Reductases and Antagonists of the Androgen Receptor". (16 pages) Cited by 3 patents [ISI abstract]


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