Abstract: The present invention relates to an improved process for the preparation of substituted Fluticasone derivatives. The invention also reveals the processes for the purification of Fluticasones and related intermediates to provide the highly pure product.
Type:
Grant
Filed:
September 2, 2011
Date of Patent:
September 23, 2014
Assignee:
Cadila Healthcare Limited
Inventors:
Kirtipalsinh Solanki, Ruchir Z Bavadia, Dhaval P Patel, Dhaval J Patel, Tejash C Shah, Manoj Kumar Singh
Abstract: The present invention refers to a pharmaceutical formulation characterized in that it includes mainly clobetasolpropionate, minoxidil and 11 alpha hydroxyprogesterone as main active principles, besides other excipients, vitamins and/or minerals, and to its use in the treatment of skin diseases, mainly in the symptomatic treatment of psoriasis.
Abstract: 6-hydroxy and 6-oxo-androstane derivatives of formula (I), active on the cardiovascular system. ##STR1## wherein: the symbol A represents CH--OR, C.dbd.N--OR, CH--CH.dbd.N--OR and C.dbd.CH--N--OR; and R.sup.1, R.sup.2 and R.sup.3 are as defined herein.
Abstract: The unsaturated 17.alpha.-cyanomethyl-17.beta.-hydroxy steroids of the formula I, ##STR1## in which R.sub.1 =Me, Eth; R.sub.2 =H, Me; R.sub.3 =H, OH, an acetoxy or alkoxy group; R.sub.4 =H, R.sub.5 =OH, an acetoxy, alkoxy group of R.sub.4 and R.sub.5 together represent a keto- or ketal group and double bonds are contained in the basic structure of the steroid, particularly between the 15 and 16 position in the steroid ring, from unsaturated 17-ketosteroids of the general formula II as described herein with the aforementioned meanings of R.sub.1 to R.sub.5 by reacting the unsaturated 17-ketosteroids with LiCH.sub.2 CN and subsequently hydrolyzing.The compounds of formula I are pharmacologically interesting steroid compounds or also intermediate products for the synthesis of highly-effective steroid products which can be used in human and veterinary medicine for the treatment of endocrine disorders and for reproductive control based on their specific hormonal/anti-hormonal actions.
Abstract: The present invention involves improved processes for the dehalogenation of 9.alpha.-halosteroids (I) ##STR1## to produce the corresponding 11.beta.-hydroxy steroids (II) ##STR2## which are known to be useful as pharmaceutical, where the improvements comprise (1) adding the 9.alpha.-halo steroid (I) to the chromium and (2) using catalytic amounts of chromium in the presence of a means of converting chromium (II) to chromium (III).
Abstract: A method for controlling weight gain or promoting weight loss which includes the step of treating a subject with an effective weight gain controlling or weight loss promoting amount of a substituted .DELTA.5-Androstene which is biologically effective for controlling weight gain or promoting weight loss and biologically ineffective for promoting the synthesis of sex hormones. Steroids believed to provide the desired weight control/weight loss characteristics include:.DELTA.5-Androstene-3.beta.,7.alpha.-diol-17-one.DELTA.5-Androstene-3.beta.-ol-7,17-dione.DELTA.5-Androstene-3.beta.,7.alpha.,17-triol.DELTA.5-Androstene-3.beta.,17.beta.-diol-7-oneand various derivatives thereof.
Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.6 is selected from the group consisting of halogen, --CH.sub.3, fluorine and chlorine, R.sub.9 and R.sub.11 together form a second bond at 9(11) or R.sub.9 is hydrogen or fluorine and R.sub.11 is selected from the group consisnting of hydrogen, --OH and .dbd.O, the dotted lines in rings A and B indicate a possible additonal bond at 1(2) and 6(7), R.sub.17 is hydrogen or acyl or an organic carboxylic acid of 1 to 18 carbon atoms, R'.sub.17 is ##STR2## Z is selected from the group consisting of a single bond, alkylene of 1 to 5 carbon atoms and alkenylene and alkynylene of 2 to 5 carbon atoms, P is pyrimidinyl or pyridyl optionally substituted with one or two individual members of the group consisting of --NH.sub.
Type:
Grant
Filed:
March 21, 1990
Date of Patent:
January 14, 1992
Assignee:
Roussel Uclaf
Inventors:
Andre Claussner, Jacques Leclaire, Lucien Nedelec, Daniel Philibert
Abstract: Novel esters of 9.alpha.-fluoro- and chloro-corticosteroids of the formula ##STR1## wherein Y is chlorine or OR.sub.1, R.sub.1 and R.sub.2 represent an acyl group of 2-6 carbon atoms or a benzoyl group and where R.sub.1 and R.sub.2 can be the same or different in the same molecule, R.sub.3 is methyl or fluorine in either the .alpha.- or .beta.- orientation, X is chlorine or fluorine, and the C.sub.1 C.sub.2 bond can be saturated or not, especially those compounds of the formula ##STR2## wherein Y and R.sub.2 have the significance given above, are prepared by reacting the respective 9.beta.,11.beta.-epoxy compounds with hydrogen fluoride or chloride.
Type:
Grant
Filed:
May 21, 1990
Date of Patent:
June 25, 1991
Assignee:
Hovione Inter Ltd.
Inventors:
Ivan Villax, William Heggie, Philip R. Page