- Amines useful in producing pharmaceutically active CNS compounds
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Disclosed are Δ9(11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), Δ16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), Δ17(20) -steroids (Va and Vb) and Δ9(11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.
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- Amines useful in producing pharmaceutically active CNS compounds
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Disclosed are Δ9(11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), Δ16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), Δ17(20) -steroids (Va and Vb) and Δ9(11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.
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- Steriod 5-alpha-reductase inhibitors
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Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-α-reductase. Also invented are intermediates used in preparing these compounds.
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- Steroid 5-alpha-reductase inhibitors
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[From equivalent EP0289327A3] Compounds of formula (I) : ψψ in which, inter alia, R± is H or C±±±alkyl and M is O or S, processes for their preparation, pharmaceutical compositions containing then and their use as inhibitors of 5-à-reductase in the treatment in the reduction of prostate size.ψ
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- PHOSPHINIC ACID SUBSTITUTED STEROIDS AS INHIBITORS OF STEROID 5 ALPHA-REDUCTASE
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The invention relates to 3-phosphinic acid steroidal compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5alpha-reductase.
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- PHOSPHONIC ACID SUBSTITUTED STEROIDS AS STEROID 5 ALPHA-REDUCTASE INHIBITORS
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Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5 alpha-reductase. Also invented are intermediates used in preparing these compounds
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- STEROID 5-ALPHA-REDUCTASE INHIBITORS
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Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-alpha-reductase. Also invented are intermediates used in preparing these compounds
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- C20 Through C26 amino steroids
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Disclosed are Δ9 (11)-steroids (VI) and amino substituted steroids of formula (XI) which contain an amino group attached to the terminal carbon atom of the C17-side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), Δ16 (11)-steroids (IIIa and IIIb), reduced A-ring steroids (IV), Δ17 (20)-steroids (Va and Vb) and Δ9 (11)-steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.
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- STUDIES ON THE CHEMO- AND STEREOSELECTIVITY OF SODIUM BOROHYDRIDE-POLYETHYLENE GLYCOL 400-MEDIATED REDUCTIONS
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Chemo- and stereoselectivity of reductions by the NaBH4/polyethylene glycol (PEG) 400 system have been studied and compared to the traditional NaBH4 reductions in methanol.When the stereoselectivity was tested on 3- and 7-keto steroids 1a and 1b, respectively, interesting improvements were observed.Aldehydes were reduced faster than ketones and in the case of 3-oxo-pregn-4-en-20β-carboxaldehyde, 2a, the aldehyde was reduced completely leaving the unsatured ketone moiety unchanged.Absorption on inorganic support or addition of a few cationic species led to inactive or much less active reducing species.
- Santaniello, Enzo,Ferraboschi, Patrizia,Fiecchi, Alberto,Grisenti, Paride,Manzocchi, Ada
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p. 701 - 704
(2007/10/02)
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- Process for the preparation of 21-hydroxy-20-methylpregnane derivatives
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In a process for preparing 21-hydroxy-20-methylpregnane derivatives by fermenting a zoosterol or a phytosterol with a culture of Mycobacterium spec. NRRL B-3683 or NRRL B-3805 or a variant or mutant thereof, an improvement comprises conducting the fermentation at a pH value of 6.0-8.0 in the presence of an amount of borate ions or an organic boron compound effective to increase the yield of the 21-hydroxy-20-methylpregnane derivatives produced.
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- Testosterone 5α-reductase inhibitors
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Compounds of the following general formula are testosterone 5α-reductase inhibitors rendering said compounds useful in the treatment of acne and oily skin: STR1 wherein n is an integer of from 0 to 4; R1 is --COOR2, --CONR3 R4, --CHO or --CH2 OR5 ; R2 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, or benzyl; each of R3 and R4 is hydrogen or a straight or branched lower alkyl group of from 1 to 4 carbon atoms; and R5 is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 20 carbon atoms and is straight or branched, benzoyl, phenylalkylcarbonyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched, or cycloalkylcarbonyl wherein the cycloalkyl moiety has from 5 to 10 carbon atoms.
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