41639-23-0Relevant articles and documents
Diastereoselective reduction of the enone intermediate of Travoprost
Aswathanarayanappa, C.,Bodke, Yadav D.,Bheemappa, E.
experimental part, p. 1085 - 1087 (2011/12/21)
A scalable process for the diastereoselective reduction of the prochiral enone intermediate 1 has been developed with DEANB/(R)-methyl CBS as reducing agent, to obtain the key intermediate alcohol 15R-isomer 2, used in a process for the manufacture of Travoprost (3). Various advantages of this process against the DMSB reduction assisted by (R)-methyl CBS have been studied. Specific comparison has been made to highlight the salient features of the chosen process on yield and optical purity with those of the DMSB reduction.
Bimatoprost crystalline form I
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Page/Page column 13, (2009/07/10)
The invention provides a novel polymorphic form I of crystalline bimatoprost, method for preparation thereof and new crystalline intermediates in the preparation. This form I of crystalline bimatoprost is used in purification of crude bimatoprost and in storage of bimatoprost as active pharmaceutical intermediate. Use of the physical form of bimatoprost in the manufacture of a medicament is also disclosed.
Composition and method for the treatment of psoriasis
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Page/Page column 4, (2008/06/13)
The use of a prostaglandin A2 derivative, and prodrugs of the compound, for the manufacture of a medicament for the treatment and/or alleviation of psoriasis is presented, as well as a method of treatment, involving the topical application of such prostaglandins. Compositions containing a therapeutically active, and physiologically acceptable amount of the above compound or derivatives thereof, as such or in the form of a prodrug, in a suitable vehicle are also described. Importantly, the derivatives can be applied in therapeutically active amounts without or with only minimal side effects, such as hyperemia, irritation or pain.
Phenyl-Substituted Prostaglandins: Potent and Selective Antiglaucoma Agents
Resul, Bahram,Stjernschantz, Johan,No, Kiyo,Liljebris, Charlotta,Selen, Goeran,et al.
, p. 243 - 248 (2007/10/02)
A series of phenyl-substituted analoques of prostaglandin F2α (PGF2α) were prepared and evaluated for ocular hypotensive effect and side effects in different animal models.In addition, the activity of the analogues on FP receptors was studied in vitro.The results were compared with those of PGF2α and its isopropyl ester.The phenyl-substituted PGF2α analogues exhibited good intraocular pressure reducing effect, were more selective, and exhibited a much higher therapeutic index in the eye than PGF2α or its isopropyl ester.The analogues exhibited high activity on FP receptors in a stereoselective manner for the 15a-hydroxyl group.
N-(Methanesulfonyl)-16-phenoxyprostaglandincarboxamides: Tissue-Selective, Uterine Stimulants
Schaaf, Thomas K.,Bindra, Jasjit S.,Eggler, James F.,Plattner, Jacob J.,Nelson, A. James,et al.
, p. 1353 - 1359 (2007/10/02)
In an effort to develop tissue-selective prostaglandin analogues resistant to the metabolic inactivating pathways of the natural materials, hybrid compounds modified both at C-1 with a sulfonimide moiety and in the n-amylcarbinol side chain with substituted phenoxy groups were synthesized and evaluated in a variety of in vitro and in vivo models.Several of these analogues exhibited potent, tissue-selective, uterine stimulant activity, a finding subsequently confirmed in clinical studies with one member of this series, N-(methanesulfonyl)-16-phenoxy-ω-tetranor-PGE2-carboxamide (CP-34089/ZK-57671, sulprostone).
