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| 20080287404 | High Purity 17Alpha-Cyanomethyl-17Beta-Hydroxy-Estra-4,9-Diene-3- One and Process For the Syntheses Thereof - The invention relates to a new process for the synthesis of high purity 17α-cyanomethyl-17β-hydroxy-estra-4,9-diene-3-one (further on dienogest) of formula (I) from 3-methoxy-17-hydroxy-estra-2,5(10)-diene of formula (V). The invention relates also to the high purity 17α-cyanomethyl-17β-hydroxy-estra-4,9-diene-3-one and pharmaceutical compositions containing that as active ingredient. The pharmaceutical compositions according to this invention contain high purity dienogest of formula (I) in which the total amount of impurities is less than 0.1%, while the amount of 4-bromo-dienogest is under the detection limit (0.02%) as active ingredient or at least one of the active ingredients and auxiliary materials, which are commonly used in practice, such as carriers, excipients or diluents. According to our invention the dienogest of formula (I) is synthesized the following way: i) 3-methoxy-17-hydroxy-estra-2,5(10)-diene of formula (V) is reacted with aluminum isopropylate in the presence of cyclohexanone in an inert organic solvent under heating; ii) the so obtained 3-methoxy-estra-2,5(10)-diene-17-one of formula (IV) is reacted with cyanomethyl lithium at a temperature between 0 and −30° C.; iii) the obtained 3-methoxy-17α-cyanomethyl-17β-hydroxy-estra-2,5(10)-diene of formula (III) is reacted with a strong organic acid in tetrahydrofuran solution; iv) the obtained 17α-cyanomethyl-17β-hydroxy-estr-5(10)-ene-3-one of formula (II) is reacted with 1-1.5 equivalent of pyridinium tribromide in pyridine solution at a temperature between 0 and 60° C., then the obtained crude dienogest of formula (I) is purified by recrystallization and preparative HPLC. | 11-20-2008 |
| 20100137622 | INDUSTRIAL METHOD FOR THE SYNTHESIS OF 17-ACETOXY-11beta-[4-(DIMETHYLAMINO)-PHENYL]-21-METHOXY-19-NORPREGNA-4,9-- DIEN-3,20-DIONE AND THE KEY INTERMEDIATES OF THE PROCESS - The present invention relates to a process for the synthesis of the known 17-acetoxy-11-β-[4-(dimethyl amino)-phenyl]-21-methoxy-19-norpregna-4,9-dien-3,20-dione (further on CDB-4124) of formula (I) from 3,3-[1,2-ethandiyl-bis(oxy)]-oestr-5(10),9(11)-dien-17-one of formula (II). Compound CDB-4124 belongs to the group of anti-hormones. The process has the following steps: i) formation of an epoxide; ii) addition of hydrogen cyanide; iii) silylation of a hydroxyl group; iv) reaction with 4-(dimethylamino)-phenyl magnesium bromide Grignard reagent in the presence of CuCl (Teutsch reaction); v) silylation of a hydroxyl group with trimethyl chlorosilane; vi) reaction with diisobutyl aluminum hydride and after addition of acid to the reaction mixture; vii) methoxy-methylation with methoxy-methyl Grignard reagent formed in situ, while hydrolyzing the trimethylsilyl protective groups; viii) oxidation of a hydroxyl group with dicyclohexyl carbodiimide in the presence of dimethyl sulfoxide and a strong organic acid (Swern oxidation), and in given case after purification by chromatography; ix) acetylation of a hydroxyl group with acetic anhydride in the presence of perchloric acid, and in given case, purification by chromatography. The invention also relates to new intermediates of the process. | 06-03-2010 |
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| 20080214967 | ULTRASONIC SURGICAL INSTRUMENT - An ultrasonic surgical instrument is provided which includes a handle assembly, a body extending distally from the handle assembly and an end effector configured to effect cutting, dissection, coagulation and/or ligation of tissue. The end effector includes an ultrasonic member. A transducer is supported adjacent, on or within the ultrasonic member and is connected to a power source. Upon actuation of the power source, the transducer effects vibration of the ultrasonic member. In one preferred embodiment, the end effector is mounted for articulation about the distal end of the instrument. | 09-04-2008 |
| 20080281353 | Powered tacker instrument - There is provided a powered tacker device for use in installing multiple surgical fasteners through a prosthetic mesh in into tissue. The powered tacker device generally includes a handle assembly and a tacker assembly extending distally from handle assembly. The handle assembly includes a motor and self-contained power assembly to rotate the surgical fasteners into tissue. The handle assembly is provided with a drive assembly which allows for rotation, as well as distal longitudinal movement, of a surgical fastener relative to the powered tacker device. The tacker assembly includes an inner tube for containing the plurality of surgical fasteners and a driver which is movable out of alignment with the inner tube so as to install a single fastener at a time into tissue. | 11-13-2008 |
| 20090008425 | Angled surgical fastener apparatus - A surgical fastening apparatus includes a handle, an elongated member extending distally from the handle and a fastener applier and anvil head disposed at the distal end of the elongated member. The elongated member defines a distal offset end portion upon which the fastener applier and the anvil head are mounted. The offset end portion is angularly oriented with respect to the axis of the instrument at a predetermined fixed angle (e.g., either 45°, 60° and 75° relative to the axis of the instrument) thereby positioning the fastener applier and the anvil head at the fixed angle This feature facilitates positioning of the tissue with respect to the instrument and enhances visual access to the tissue when appropriately disposed within the fastener applier and the anvil head. Various mechanisms for effectuating the clamping of the tissue between the fastener holder and anvil, and the firing of the instrument are disclosed. | 01-08-2009 |
| 20090259186 | ACCESS ASSEMBLY WITH MULTI-FLAPPER DESIGN - An apparatus for the reception of an instrument inserted through a surgical portal apparatus includes a valve mount, a major opening through the valve mount, a primary valve for selectively sealing the major opening, a minor opening through the primary valve, and a secondary valve for selectively sealing the minor opening. Components of both the major valve and the minor valve may be displaced to permit passage of a broad instrument, while components of only the secondary valve may be displaced to permit passage of a narrow instrument. | 10-15-2009 |
| 20110172681 | POWERED TACKER INSTRUMENT - There is provided a powered tacker device for use in installing multiple surgical fasteners through a prosthetic mesh into tissue. The powered tacker device generally includes a handle assembly and a tacker assembly extending distally from handle assembly. The handle assembly includes a motor and self-contained power assembly to rotate the surgical fasteners into tissue. The handle assembly is provided with a drive assembly which allows for rotation, as well as distal longitudinal movement, of a surgical fastener relative to the powered tacker device. The tacker assembly includes an inner tube for containing the plurality of surgical fasteners and a driver which is movable out of alignment with the inner tube so as to install a single fastener at a time into tissue. | 07-14-2011 |
