Patent application number | Description | Published |
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 |
20120142655 | NOVEL CRYSTAL FORM OF AN ORGANIC COMPOUND AND PROCESS FOR THE PREPARATION THEREOF - The present invention relates to novel crystalline Form II of 17α-acetoxy-21-methoxy-11β-[4-N,N-dimethylaminophenyl]-19-norpregna-4,9-diene-3,20-dione, (also known as CDB-4124), processes for the preparation thereof and pharmaceutical compositions comprising it. Form II can be crystallized from different medium such as esters of C1-C4 alcohols and carboxylic acids, ketones, cyclohexane, acetonitrile, dimethylformamide, dimethyl sulfoxide, water and any mixture thereof. | 06-07-2012 |
Patent application number | Description | Published |
20090187032 | INDUSTRIAL PROCESS FOR THE SYNTHESIS OF 17alpha-ACETOXY-11beta-[4-(N,N-DIMETHYL-AMINO)-PHENYL]-19-NORPREGNA-4,9-D- IENE-3,20-DIONE AND NEW INTERMEDIATES OF THE PROCESS - The present invention relates to a new industrial process for the synthesis of solvate-free 17α-acetoxy-11β-[4-(N,N-dimethyl-amino)-phenyl]-19-norpregna-4,9-diene-3,20-dione [CDB-2914] of formula (I) which is a strong antiprogestogene and antiglucocorticoid agent. The invention also relates to compounds of formula (VII) and (VIII) used as intermediates in the process. | 07-23-2009 |
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 |
Patent application number | Description | Published |
20100061231 | MULTI-DOMAIN NETWORK AND METHOD FOR MULTI-DOMAIN NETWORK - Each domain of a multi-domain network collects intra-domain routing information relating to that domain and makes a reduced view of that information available to other domains of the network, and in which each domain of the network uses its own intra-domain routing information together with the reduced-view routing information from the other domains to form a logical view of the network so as to enable that domain to make an end-to-end route selection decision. | 03-11-2010 |
20100110918 | Method and apparatus for performance monitoring in a communications network - A method and device for determining a packet drop indicator, for use in a communication system is described. The method comprises the following steps: A. determining the number of packets sent at a sending side within a first time period; B. determining the number of packets received at a receiving side within a second time period; and C. calculating a packet drop indicator on the basis of said number of sent packets and said number of received packets. | 05-06-2010 |
20100195492 | Controlling Traffic in a Packet Switched Communications Network - The present invention relates to a packet switched communications network especially to an Ethernet network in which User Network Interfaces (UNI) are standardized between client network ( | 08-05-2010 |
20100208614 | METHOD AND ARRANGEMENT FOR SCHEDULING DATA PACKETS IN A COMMUNICATION NETWORK SYSTEM - The present invention relates to a method and an arrangement for scheduling data packets each belonging to a particular traffic class associated with a certain quality of service (QoS) level and transmitted between a first communication network node and a second communication network node. Initially a token rate for assigning tokens to each traffic class is set and an incoming traffic rate of each traffic class is measured by counting a number of incoming data packets during a pre-determined period of time. Then, based on said measured incoming traffic rate said token rate is adjusted in order to obtain a fair scheduling of data packets belonging to different traffic classes. | 08-19-2010 |
20100309894 | Method and Apparatuses for Allowing a Nomadic Terminal to Access a Home Network on Layer 2 Level - A method of allowing a nomadic terminal to access a home network on the Layer 2 level. The method comprises connecting said terminal to a remote access network via an access point, the remote access network being connected to an operator's backbone network via a remote access router. Signalling is exchanged between the access point and an authentication server within the backbone network in order to authenticate the terminal to the authentication server and, following successful authentication, a Layer 2 tunnel extending across the backbone network is established for the purpose of connecting said nomadic terminal to the home network. | 12-09-2010 |
20110019654 | Method and Apparatus for Use in a Communications Network - A method is provided of enabling access for a terminal ( | 01-27-2011 |
20110026502 | Method and System for Simultaneous Local and EPC Connectivity - A system for providing simultaneous local and global connectivity for a 3 | 02-03-2011 |
20130142093 | Mobile Layer 2 Virtual Private Network Over Internet Protocol Networks - The present disclosure relates to a technique for maintaining communication established between a mobile node ( | 06-06-2013 |
20130301416 | MULTI-LEVEL BEARER PROFILING IN TRANSPORT NETWORKS - A method is provided for transporting data packets over a telecommunications transport network. The data packets are carried by a plurality of bearers, the bearers each carrying data packets that relate to different ones of a plurality of services. In the method a multi-level bandwidth profiling scheme is applied to the data packets of each bearer. A series of information rates are assigned to a bearer, the profiling scheme identifying and marking each data packet of the bearer based on a desired resource sharing according to the minimum information rate with which the packet is conformant. The marked data packets are forwarded for transport through the transport network. If there is insufficient bandwidth available in the transport network to transport all data packets, data packets identified by the profiling and marked as only being conformant with a higher information rate are discarded before any data packets marked as being conformant with a lower information rate. | 11-14-2013 |
20140293793 | Service-Aware Profiling for Transport Networks - A method is provided of transporting data packets over a telecommunications transport network. The data packets are carried by a plurality of bearers, each carrying data packets that relate to different ones of a plurality of services. In the method bandwidth profiling is applied to the data packets of each bearer, independently of the other bearers, to identify and mark the data packets of each of the bearers that are conformant with a predetermined maximum information rate for the bearer. The data packets are forwarded for transport through the transport network, wherein, if there is insufficient bandwidth available in the transport network to transport all data packets, data packets not identified by the profiling as being conformant are discarded, so as not to be transported through the transport network. | 10-02-2014 |
20140321284 | Optimised Packet Delivery Across a Transport Network - A method of prioritising packets for delivery over a transport network interconnecting nodes of a mobile network, where a guaranteed minimum information rate over the transport network is specified for the mobile network. The method comprises, for each bearer to be injected into the transport network from the mobile network, specifying a bearer information rate and marking packets up to that rate as conformant with the bearer information rate and marking packets exceeding that rate as non-conformant with the bearer information rate. A plurality of traffic type streams from the mobile network are converged, each traffic type stream comprising a plurality of bearers. Packets of the converged traffic type streams are inspected to identify packets marked as conformant and non-conformant, and re-marking non-conformant packets, or at least a fraction of non-conformant packets, as conformant if the converged rate of conformant packets is less than said minimum information rate. The transport network prioritises the delivery of packets marked as conformant over those packets marked as non-conformant. | 10-30-2014 |
20140328170 | Enhanced Performance Service-Based Profiling for Transport Networks - A method is presented of transporting data packets over a telecommunications transport network. The data packets are carried by a plurality of bearers. For each of the bearers, independently of the other bearers, bandwidth profiling is applied to the data packets of the bearer to designate as ‘green’ data packets that are conformant with a predetermined maximum Information Rate for the bearer. One or more data packets is buffered for up to a predetermined maximum ‘green’ buffer time, during which if transporting the data packet would not cause the maximum information rate of the bearer to be exceeded, the data packet is designated as a ‘green’ data packet. The data packets are forwarded for transporting over the transport network. If there is insufficient bandwidth available in the transport network to transport all data packets, data packets that are not designated as ‘green’ data packets are discarded, so as not to be transported through the transport network. | 11-06-2014 |
20140341042 | Conditional Routing Technique - A technique for controlling network routing in a network ( | 11-20-2014 |
20150063121 | Load Balancing Among Alternative Paths - A method and a transmitting node for redirecting of a flow of data packets to a path of alternative paths, and a method and a receiving node for enabling redirection of a flow of data packets to a path of alternative paths, where data packets are marked with a value indicating the importance of the data packets. The method for directing directs one or more flows of data packets for the alternative paths, wherein data packets marked with a higher value are prioritized over data packets marked with a lower value. Based on feedback information, the transmitting node redirects a flow of data packets to a second path of the alternative paths, if the metric of congestion indicates a higher congestion on the first path than on the second path. | 03-05-2015 |
Patent application number | Description | Published |
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 |
20090312299 | Isolated Isomers of Norelgestromin and Methods of Making and Using the Same - The invention is directed to a process of preparing substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene-20-yn-3-one-3E- and -3Z-oxime isomers, as well as a process for the synthesis of the mixture of isomers and the pure isomers. The invention also relates to substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene20-yn-3-one-3E-oxime and substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene-20-yn-3-one-3Z-oxime isomer. Further aspects of the invention include a composition comprising substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene20-yn-3-one-3E-oxime or substantially pure d-(17α)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene-20-yn-3-one-3Z-oxime isomer, and methods of treatment using said compositions. | 12-17-2009 |
Patent application number | Description | Published |
20090018149 | 4,5,6,7-tetrahydrobenzo[b]thiophene derivatives and methods for medical intervention against mycobacterial infections - Described are 4,5,6,7-tetrahydrobenzo[b]thiophene derivatives and pharmaceutically acceptable salts thereof, the use of these derivatives for the prophylaxis and/or treatment of mycobacteria-induced infections and opportunistic infections, as well as compositions containing at least one 4,5,6,7-tetrahydrobenzo[b]thiophene derivative and/or pharmaceutically acceptable salts thereof. Furthermore, the present application refers to the use of mycobacterial protein serine/threonine kinases for developing methods for detection and determination of these kinases for recognising and monitoring diseases and for controlling therapy of diseases. | 01-15-2009 |
20090298842 | Novel therapeutic targets for the treatment of mycobacterial infections and compounds useful therefor - Described herein is the discovery that certain mycobacterial serine/threonine protein kinases, particularly protein kinase G (PknG), are effective therapeutic targets for the treatment of mycobacterial infections. Furthermore, the present application refers to the use of mycobacterial serine/threonine protein kinases for developing methods for detection and determination of these kinases for recognizing and monitoring diseases and for controlling therapy of diseases. Additionally disclosed are novel 4,5,6,7-tetrahydrobenzo[b]thiophene compounds, benzo(g)quinoxaline compounds, and pharmaceutically acceptable salts thereof, and methods of using such compounds and salts thereof for the prophylaxis and/or treatment of virally and/or bacterially induced infections, particularly mycobacteria-induced infections, including opportunistic infections, as well as pharmaceutical compositions containing at least one 4,5,6,7-tetrahydrobenzo[b]thiophene compound and/or benzo(g)quinoxaline compound and/or pharmaceutically acceptable salts thereof in a pharmaceutically acceptable carrier. | 12-03-2009 |