- PRODRUGS OF ABIRATERONE
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The present invention relates to compounds of formula (I), or their isotopic forms, stereoisomers, tautomers, or pharmaceutically acceptable salt(s) thereof as prodrugs of abiraterone. The present invention also describes method of making such compounds, pharmaceutical compositions comprising such compounds and the use of the compounds of formula (I).
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Page/Page column 30-31
(2021/05/29)
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- DRUGS TO TREAT OCULAR DISORDERS
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The present invention provides new prodrugs of therapeutically active loop diuretics, including oligomeric prodrugs, and compositions to treat medical disorders, for example, ocular disorders such as glaucoma, a disorder or abnormality related to an increase in intraocular pressure (IOP), a disorder requiring neuroprotection, age-related macular degeneration, or diabetic retinopathy.
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Page/Page column 200-201
(2019/11/12)
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- One-pot synthesis of phenylseleno N-acetyl α-amino acids: Supra-molecular self-assembling in organoselenium compounds
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A convenient one-pot synthesis of phenylseleno N-acetyl α-amino acids, PhSeCH2C(O)NHC(R)COOH (R = H (1), Me (2), PhCH2 (3), 4-HOC6H4CH2 (4) and CH2OH (5)) is reported. These compounds have been characterized by microanalyses, UV-Vis, IR and NMR (1H, 13C, 77Se) spectroscopy. The molecular structures of [PhSeCH2CONHCH2COOH] (1), [PhSeCH2CONHCH(CH2C6H4OH-4)COOH] (4) and [PhSeCH2CONHCH(CH2OH)COOH] (5) have been established by X-ray diffraction analyses. These compounds are associated in the solid state through hydrogen bonding to give supra-molecular self-assembled structures. Free radical scavenging activity of these compounds has also been evaluated by DPPH assay.
- Parashiva Prabhu,Phadnis, Prasad P.,Wadawale, Amey,Priyadarsini, K. Indira,Jain, Vimal K.
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p. 140 - 147
(2013/10/01)
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- Reactions of N-(2-chloroacetyl)-α-amino acids with 3-cyanopyridine-2(1H)-thiones. New promising route to 3,4- dihydropyrido[3′,2′:4,5]thieno[3,2-e][1,4]diazepine-2(1H),5-diones
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The reactions of N-(2-chloroacetyl)-α-amino acids with 3-cyanopyridine-2(1H)-thiones afforded N-(3-ammothieno[2,3-b]pyridin-2- ylcarbonyl)-α-amino acids. Heating of the latter smoothly produced 3,4-dihydropyrido[3′,2′:4,5]thieno[3,2-e][1,4]diazepine-2(1H), 5-diones in high yields.
- Fedorov,Shestopalov,Belyakov
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p. 2197 - 2202
(2007/10/03)
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- 7-Oxabicycloheptyl Carboxylic Acids as Thromboxane A2 Antagonists: Aza ω-Chain Analogues
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A novel bicyclic prostaglandin analogue, >-7-acetyl>amino>methyl>-7-oxabicyclohept-2-yl>-5-heptenoic acid ((-)-7) was found to be a potent and selective thromboxane A2 (TxA2) receptor antagonist.Unlike the related series of ω-chain allylic alcohols, amide 7 and its congeners were uniformly free of direct contractile activity in vitro (bovine coronary) and in vivo (anesthetized guinea pig).Amide 7 was effective in the inhibition of (a) arachidonic acid induced platelet aggregation of human platelet-richplasma (I50 = 0.18 +/- 0.006 μM), (b) 11,9-epoxymethano-PGH2 induced platelet aggregation of human platelet-rich plasma (I50 = 0.24 μM), (c) 11,9-epoxymethano-PGH2 induced contraction of guinea pig trachea (Kb = 3.0 +/- 0.3 nM) or rat aorta (Kb = 8.8 +/- 1.1 nM), and (d) arachidonic acid induced bronchoconstriction in the anesthetized guinea pig (0.1-1.0 mg/kg iv).Amide 7 inhibited the binding of ->-7-hydrazino>methyl>-7-oxabicyclohept-2-yl>-5-heptenoic acid to human platelet membranes in a specific and saturable manner with a Kd = 49.6 +/- 1.4 nM.
- Nakane, Masami,Reid, Joyce A.,Han, Wen-Ching,Das, Jagabandhu,Truc, Vu Chi,et al.
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p. 2465 - 2476
(2007/10/02)
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- Bicycloheptane substituted diamide and its congener prostaglandin analogs
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Bicycloheptane substituted amide prostaglandin analogs are provided having the structural formula STR1 wherein m is 0 to 4; A is --CH=CH-- or --CH2 --CH2 --; n is 1 to 5; Q is --CH=CH--, --CH2 --, STR2 or a single bond; R is CO2 H, CO2 alkyl, CO2 alkali metal, CO2 polyhydroxyamine salt, --CH2 OH, STR3 wherein R4 and R5 are the same or different and are H, lower alkyl, hydroxy, lower alkoxy or aryl, at least one of R4 and R5 being other than hydroxy and lower alkoxy; p is 1 to 4; R1 is H or lower alkyl; q is 1 to 12; R2 is H or lower alkyl; and R3 is H, lower alkyl, lower alkenyl, lower alkynyl, aryl, arylalkyl, lower alkoxy, aryloxy, arylalkyloxy, amino, alkylamino arylamino, arylalkylamino, lower alkyl-S-, aryl-S-, arylalkyl-S-, STR4 (wherein n' is 0, 1 or 2), alkylaminoalkyl, arylaminoalkyl, arylalkylaminoalkyl, alkoxyalkyl, aryloxyalkyl or arylalkoxyalkyl. The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
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- 7-oxabicycloheptane substituted hydroxamic acid prostaglandin analogs
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7-Oxabicycloheptane substituted hydroxamic acid prostaglandin analogs are provided having the structural formula STR1 wherein A is --CH=CH-- or --CH2 -CH2 --; n is 1 to 5; R is CO2 H, CO2 alkyl, CO2 a
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- 5,6-epoxy-7-oxabicycloheptane substituted diamide prostaglandin analogs
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5,6-Epoxy-7-oxabicycloheptane substituted diamide prostaglandin analogs are provided having the structural formula STR1 wherein A is --CH=CH-- or --CH2 --CH2 --; n is 1 to 5; R is CO2 H, CO2 alkyl, CO2 alkali metal, CO2 polyhydroxyamine salt or STR2 q is 1 to 12; and R1 is H, lower alkyl, lower alkenyl, lower alkynyl, aryl, arylalkyl, lower alkoxy, aryloxy, arylalkyloxy, amino, alkylamino arylamino, arylalkylamino, STR3 (wherein n' is 0, 1 or 2), alkylaminoalkyl, arylaminoalkyl, arylalkylaminoalkyl, alkoxyalkyl, aryloxyalkyl or arylalkoxyalkyl. The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
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- 7-thiabicycloheptane substituted diamide and its congener prostaglandin analogs
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7-Thiabicycloheptane substituted diamide and congener prostaglandin analogs are provided having the structural formula STR1 wherein m is 1 to 4; A is --CH=CH-- or --CH2 --CH2 --; n is 1 to 5; R is CO2 H, CO2 alkyl, CO2 alkali metal, CO2 polyhydroxyamine salt, --CH2 OH, STR2 wherein R3 and R4 are the same or different and are H, lower alkyl, hydroxy, lower alkoxy or aryl, at least one of R3 and R4 being other than hydroxy and lower alkoxy; p is 1 to 4; Z is STR3 q is 1 to 12; R1 is H or lower alkyl; and R3 is H, lower alkyl, lower alkenyl, lower alkynyl, aryl, arylalkyl, lower alkoxy, aryloxy, arylalkyloxy, amino, alkylamino arylamino, arylalkylamino, STR4 (wherein n' is 0, 1 or 2), alkylaminoalkyl, arylaminoalkyl, arylalkylaminoalkyl, alkoxyalkyl, aryloxyalkyl or arylalkoxyalkyl. The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
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- 7-OXABICYCLOHEPTANE SUBSTITUTED DIAMIDE AND ITS CONGENER PROSTAGLANDIN ANALOGS USEFUL IN THE TREATMENT OF THROMBOTIC DISEASE
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7-Oxabicycloheptane substituted amide prostaglandin analogs are provided having the structural formula STR1 wherein m is 0 to 4; A is--CH=CH--or--CH 2--CH 2--; n is 1 to 5; Q is--CH=CH--,--CH 2--, STR2 or a single bond; R is CO 2 H, CO 2 alkyl, CO 2 alkali metal, CO 2 polyhydroxyamine salt,--CH 2 OH, STR3 wherein R. sup.4 and R 5 are the same or different and are H, lower alkyl, hydroxy, lower alkoxy or aryl, at least one of R 4 and R 5 being other than hydroxy and lower alkoxy; p is 1 to 4; R. sup.1 is H or lower alkyl; q is 1 to 12; R 2 is H or lower alkyl; and R 3 is H, lower alkyl, lower alkenyl, lower alkynyl, aryl, arylalkyl, lower alkoxy, aryloxy, arylalkyloxy, amino, alkylamino arylamino, arylalkylamino, STR4 (wherein n' is 0, 1 or 2), alkylaminoalkyl, arylaminoalkyl, arylalkylaminoalkyl, alkoxyalkyl, aryloxyalkyl or arylalkoxyalkyl.The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
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