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US5099019A Expired / Lapsed US ⏱️ 0.0 years remaining

Amines useful in producing pharmaceutically active CNS compounds

Assignee: Pharmacia and Upjohn Co
•
Filing: 1988-08-08
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Granted: 1992-03-24
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Expires: 2008-08-08
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Abstract

Abstract Disclosed are Δ 9 (11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C 17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), Δ 16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), Δ 17 (20) -steroids (Va and Vb) and Δ 9 (11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.

Inventors

  • 👤 John M. McCall
  • 👤 Donald E. Ayer
  • 👤 E. Jonathan Jacobsen
  • 👤 Frederick J. VanDoornik
  • 👤 John R. Palmer
  • 👤 Harold A. Karnes

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-04 04:12
CPC Classifications
C; C07; C07D; C07D213/00; C07D213/02; C07D213/04; C07D213/60; C07D213/72; C07D213/74; C07D213/62; C07D213/63; C07D213/65; C07D239/00; C07D239/02; C07D239/24; C07D239/28; C07D239/46; C07D239/50; C07D249/00; C07D249/02; C07D249/08; C07D249/10; C07D249/14; C07D251/00; C07D251/02; C07D251/12; C07D251/26; C07D251/40; C07D251/54; C07D251/70; C07D295/00; C07D295/04; C07D295/12; C07D295/135; C07D307/00; C07D307/02; C07D307/34; C07D307/56; C07D307/68; C07D333/00; C07D333/50; C07D333/52; C07D333/62; C07D333/66; C07D401/00; C07D401/14; C07J; C07J21/00; C07J21/005; C07J21/006; C07J3/00; C07J3/005; C07J31/00; C07J31/006; C07J41/00; C07J41/0033; C07J41/005; C07J43/00; C07J43/003; C07J5/00; C07J5/0046; C07J5/0061; C07J5/0069; C07J5/0076; C07J7/00; C07J7/008; C07J7/0085

Claims Analysis

Total Claims: 4
Claim 1
Independent Claim 25 words
An amine selected from the group consisting of 4-[2,6-bis(diethylamino)-4-pyrimidinyl]piperazine, 4-[6-amino-4-(diethylamino)-2-pyrimidinyl]piperazine, 4-[2,6-bis(dimethylamino)-4-pyrimidinyl]piperazine, 4-[2-(diethylamino)-6-(1-pyrrolidinyl)-4-pyrimidinyl]piperazine, 4-[2,6-bis(4-methyl-1-piperazinyl)-4-pyrimidinyl]piperazine, 4-[2-(diethylamino)-6-(4-methyl-1-piperazinyl)-4-pyrimidinyl]-piperazine, 4-[2-(diethylamino)-6-(1-piperidinyl)-4-pyrimidinyl]piperazine, 4-[2,6-bis(1-pyrrolidinyl)-4-pyrimidinyl]piperazine, 4-[2,6-bis(4-morpholino)-4-pyrimidinyl]piperazine, 4-[2,6-bis(allylamino)-4-pyrimidinyl]piperazine, 4-[4,6-bis(diethylamino)-2-pyrimidinyl]piperazine, 4-[2-[4-[2,6-bis(1-pyrrolidinyl)-4-pyrimidinyl]-1-piperazinyl]-ethyl]piperazine and salts and hydrates thereof.
Claim 2
Dependent Claim 25 words
An amine selected from the group consisting of 4-[2,6-bis(diethylamino)-4-pyrimidinyl]piperazine, 4-[6-amino-4-(diethylamino)-2-pyrimidinyl]piperazine, 4-[2,6-bis(dimethylamino)-4-pyrimidinyl]piperazine, 4-[2-(diethylamino)-6-(1-pyrrolidinyl)-4-pyrimidinyl]piperazine, 4-[2,6-bis(4-methyl-1-piperazinyl)-4-pyrimidinyl]piperazine, 4-[2-(diethylamino)-6-(4-methyl-1-piperazinyl)-4-pyrimidinyl]-piperazine, 4-[2-(diethylamino)-6-(1-piperidinyl)-4-pyrimidinyl]piperazine, 4-[2,6-bis(1-pyrrolidinyl)-4-pyrimidinyl]piperazine, 4-[2,6-bis(4-morpholino)-4-pyrimidinyl]piperazine, 4-[2,6-bis(allylamino)-4-pyrimidinyl]piperazine, 4-[4,6-bis(diethylamino)-2-pyrimidinyl]piperazine, 4-[2-[4-[2,6-bis(1-pyrrolidinyl)-4-pyrimidinyl]-1-piperazinyl]-ethyl]piperazine and salts and hydrates thereof.
Claim 3
Dependent Claim 17 words
An amine according to claim 1 which is selected from the group consisting of 4-[2,6-bis(1-pyrrolidinyl)-4-pyrimidinyl]piperazine, 4-[2,6-bis(4-morpholino)-4-pyrimidinyl]piperazine, 4-[4,6-bis(diethylamino)-2-pyrimidinyl]piperazine.
Claim 4
Dependent Claim 9 words
An amine according to claim 2 which is 4-[2,6-bis(1-pyrrolidinyl)-4-pyrimidinyl]piperazine.

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1995-03-24 1995-09-23 1996-03-24 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1999-03-24 1999-09-23 2000-03-24 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2003-03-24 2003-09-23 2004-03-24 $7700.00 Window Closed / Lapsed

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