766558-31-0Relevant academic research and scientific papers
ACID ADDITION SALTS OF THE 2-[2-[[(4-METHOXY-2,6-DIMETHYLPHENYL)SULFONYL]-(METHYL)AMINO]ETHOXY]-N-METHYL-N-[3-(4-METHYLPIPERAZIN-1-YL)CYCLOHEXYL] ACETAMIDE AND THE USE THEREOF AS BRADYKININ B1 RECEPTORANTAGONISTS
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, (2013/11/06)
The present invention relates to the new acid addition salts AB of the following free base of formula A or the enantiomer thereof with a physiologically acceptable acid B which is selected from among hydrochloric acid, fumaric acid and tartaric acid, as well as the polymorphs, hydrates and solvates thereof.
From bradykinin B2 receptor antagonists to orally active and selective bradykinin B1 receptor antagonists
Barth, Martine,Bondoux, Michel,Luccarini, Jean-Michel,Peyrou, Vincent,Dodey, Pierre,Pruneau, Didier,Massardier, Christine,Paquet, Jean-Luc
experimental part, p. 2574 - 2584 (2012/05/20)
The bradykinin (BK) B1 receptor is an attractive target for the treatment of chronic pain and inflammation. Starting from a dual B1 and B2 antagonist, novel antagonists were designed that display low-nanomolar affinity for human B1 receptor and selectivity over B2. Initially, potent imidazoline derivatives were studied, but these compounds suffered from low bioavailability. This issue could be overcome by the use of less basic amino derivatives leading to orally active compounds.
NEW COMPOUNDS
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, (2011/05/05)
Novel compounds of which the following is exemplary:
NOVEL COMPOUNDS
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Page/Page column 191, (2011/12/13)
Novel compounds which are useful for treating acute pain, visceral pain, neuropathic pain, inflammatory/pain receptor-mediated pain, tumour pain and headache diseases. The following is exemplary:
Substituted Pyrimidine and Triazine Compounds
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Page/Page column 34, (2010/07/10)
Substituted pyrimidine and triazine compounds corresponding to formula I wherein R1, R2, R3, R4a, R4b, R5a, R5b, R7, R8, R9a, R9b, R10, R11, A, a, b, s, t, V, W1, W2 and W3 have defined meanings, pharmaceutical compositions comprising such compounds, a process for preparing such compounds, and the use of such compounds and compositions to treat or inhibit pain and/or other disorders or disease states.
PROCESS FOR PREPARING
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Page/Page column 4, (2010/08/22)
The present invention relates to a method of preparing compounds of general formula I wherein m, n, R1 and R2 are defined as mentioned hereinafter, the enantiomers, the diastereomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases.
NOVEL B1-ANTAGONISTS
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Page/Page column 28, (2010/08/08)
Disclosed are compounds of the formula I wherein A, Y, R1, R2, R3, R4 and R5 are defined, suitable for treating diseases and symptoms of diseases caused at least to some extent by stimulation of bradykinin-B1 receptors, the preparation thereof and the use thereof.
SUBSTITUTED SULFONAMIDE DERIVATIVES
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, (2009/10/22)
The invention relates to substituted sulfonamide derivatives, processes for the preparation thereof, medicaments containing these compounds and the use of substituted sulfonamide derivatives for the preparation of medicaments.
SUBSTITUTED SULFONAMIDE DERIVATIVES
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, (2009/11/29)
The invention relates to substituted sulfonamide derivatives, processes for the preparation thereof, medicaments containing these compounds and the use of substituted sulfonamide derivatives for the preparation of medicaments.
