329923-15-1Relevant articles and documents
ACID ADDITION SALTS OF BOSENTAN
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Paragraph 0075, (2014/09/30)
The present invention relates to the stable acid addition salts of Bosentan that are useful for the purification of Bosentan base. In particular, the Bosentan acid addition salt is selected from Bosentan citrate and Bosentan tartrate.
ACID ADDITION SALTS OF BOSENTAN
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Paragraph 14, (2013/05/09)
The present invention relates to the stable acid addition salts of Bosentan that are useful for the purification of Bosentan base. In particular, the Bosentan acid addition salt is selected from Bosentan citrate and Bosentan tartrate.
PROCESSES FOR THE PREPARATION OF BOSENTAN AND ITS INTERMEDIATES THEREOF
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Page/Page column 11, (2010/10/19)
The present invention relates to processes for the preparation of bosentan and compounds that can be used as structurally novel intermediates for the synthesis thereof, and a pharmaceutical composition of the same.
PROCESS FOR PREPARATION OF BOSENTAN
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Page/Page column 6; 12-13; 24, (2010/04/25)
The present invention provides improved processes for preparing Bosentan. The present invention provides novel intermediates like 4,6-dihydroxy-5-(2-methoxy phenoxy)[2,2'] bipyrimidine of formula (II) and N-(6-Chloro-5-(2- ethoxyphenoxy)[2,2'-bipyrimidinyl]-4-t-butyl benzenesulfonamide cesium salt and process for preparation thereof. The invention also disclosed novel polymorphic form of the intermediates.
IMPROVED AND NOVEL PROCESS FOR THE PREPARATION OF BOSENTAN
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Page/Page column 18; 21, (2009/09/05)
The present invention relates to an improved and novel process for the preparation of bosentan compound of formula (1). The present invention also relates to a crystalline form of bosentan and its intermediates.
Butyne diol derivatives
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, (2008/06/13)
The present invention relates to novel butyne diol derivatives of the general formula I and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more compounds of the general formula I and especially their use as endothelin receptor antagonists.
6 alkoxy-4-pyrimidinyl bis-sulfonamides
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, (2008/06/13)
The present invention relates to novel bis-sulfonamides represented, for example, by formula I below and a pure diastereomer, a mixture of diastereomers, a diastereomeric racemate, a mixture of diastereomeric racemates and meso-forms and a pharmaceutically acceptable salt thereof, wherein R1represents aryl; aryl-lower alkyl; aryl-lower alkenyl; heteroaryl; or heteroaryl-lower alkyl; and R2represents lower alkyl; trifluoromethyl; lower alkoxy-lower alkyl; lower alkenyl; lower alkynyl; aryl; aryl-lower alkyl; aryl-lower alkenyl; heterocyclyl; heterocyclyl-lower alkyl; heteroaryl; heteroaryl-lower alkyl; cycloalkyl; or cycloalkyl-lower alkyl. The present invention also relates to a process for manufacturing those compounds, pharmaceutical compositions containing one or more of those compounds as endothelin antagonists, and a method of treating a subject having a disorder involving endothelin with the compounds of the invention.
The use of sulfonylamido pyrimidines incorporating an unsaturated side chain as endothelin receptor antagonists
Bolli, Martin H.,Boss, Christoph,Clozel, Martine,Fischli, Walter,Hess, Patrick,Weller, Thomas
, p. 955 - 959 (2007/10/03)
A series of compounds structurally related to bosentan 1 featuring an unsaturated side chain at position 6 of the core pyrimidine have been studied for their potential to block the ETA and ETB receptor. Incorporation of a 2-butyne-1,4-diol linker bearing a pyridyl carbamoyl moiety led to in vitro highly potent endothelin receptor antagonists (e.g., 70 and 75). The propargyl derivative 26 significantly reduced blood pressure in in vivo model studies with hypertensive salt-sensitive Dahl rats.
Ethenesulfonamide and ethanesulfonamide derivatives, a novel class of orally active endothelin-A receptor antagonists
Harada, Hironori,Kazami, Jun-ichi,Watanuki, Susumu,Tsuzuki, Ryuji,Sudoh, Katsumi,Fujimori, Akira,Sanagi, Masanao,Orita, Masaya,Nakahara, Hideaki,Shimaya, Jun,Tsukamoto, Shin-ichi,Tanaka, Akihiro,Yanagisawa, Isao
, p. 2955 - 2968 (2007/10/03)
In the previous paper, we described a series of 2-phenylethenesulfonamide derivatives, a novel class of ETA -selective endothelin (ET) receptor antagonists, including the 2-methoxyethoxy derivative 2a and the 2-fluoroethoxy derivative (2b). In this paper, we wish to report further details of structure activity relationships (SARs) of the two regions of the molecule in compound 2b, which were the alkoxy region at the 6-position of the core pyrimidine ring and the 2-phenylethenesulfonamide region. In these modifications, replacement of the 2-fluoroethoxy group with a methoxy group (6e) and replacement of the 2-phenylethenesulfonamide group with a 2-(pyridin-3-yl)ethenesulfonamide group (6l) or 2-phenylethanesulfonamide group (6q) were well tolerated both in the ETA binding affinity and ETA selectivity. Among them, compound 6e showed further improvement in oral activity compared to 2b. After oral administration, compound 6e inhibited the big ET-1 induced pressor response in conscious rats at 0.3 mg /kg with a duration of > 6.5 h. Compound 6e also exhibited a potent antagonisti activity in the pithed rats. Copyright