- 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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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.
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Paragraph 0155-0157
(2013/11/06)
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- From bradykinin B2 receptor antagonists to orally active and selective bradykinin B1 receptor antagonists
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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.
- Barth, Martine,Bondoux, Michel,Luccarini, Jean-Michel,Peyrou, Vincent,Dodey, Pierre,Pruneau, Didier,Massardier, Christine,Paquet, Jean-Luc
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p. 2574 - 2584
(2012/05/20)
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- COMPOUNDS
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Novel compounds, with the following being exemplary:
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- NEW COMPOUNDS
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Novel compounds of which the following is exemplary:
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- NOVEL COMPOUNDS
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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:
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- NOVEL B1-ANTAGONISTS
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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.
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Page/Page column 29
(2010/08/08)
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- SUBSTITUTED SULFONAMIDE DERIVATIVES
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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.
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- SUBSTITUTED SULFONAMIDE DERIVATIVES
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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.
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- Substituted Sulfonamide Compounds
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Substituted sulfonamide compounds corresponding to the formula I wherein m, n, p, Q, R1, R2, R3, R4, X, Y and Z have the respective meanings defined herein, pharmaceutical compositions containing such compounds, a process for their preparation, and the use of such compounds for the treatment and/or inhibition of pain and other conditions mediated by bradykinin receptor 1 (B1R) and/or bradykinin receptor 2 (B2R).
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Page/Page column 23-24
(2009/07/25)
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- SUBSTITUTED SULFONAMIDE COMPOUNDS
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Substituted sulfonamide compounds corresponding to formula I processes for the preparation thereof, pharmaceutical compositions containing these compounds, and the use of such substituted sulfonamide compounds in pharmaceutical compositions for the treatment and/or inhibition of pain and other conditions at least partly mediated by the bradykinin 1 receptor
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Page/Page column 34
(2009/10/30)
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- Substituted Sulfonamide Compounds
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Substituted sulfonamide compounds corresponding to formula I: a process for their preparation, pharmaceutical compositions comprising such compounds, and the use of such substituted sulfonamide compounds in pharmaceutical compositions for the treatment of pain or other disorders or diseases that are mediated at least in part by B1R receptors.
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Page/Page column 29-30
(2009/10/30)
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- N-OXIDE ARYL SULFONES AND SULFOXIDES
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N-oxide aryl sulfones and sulfoxides of Formula (I) are provided: in which the variables are as described herein. Such compounds may be used to modulate bradykinin receptor activity in vivoor in vitro, and are particularly useful in the treatment of condi
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Page/Page column 39
(2010/11/30)
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- SPIROCYCLIC SULFONAMIDES AND RELATED COMPOUNDS
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Spirocyclic sulfonamides and related compounds of Formula 1 are provided : (Formula (I)): in which the variables are as described herein. Such compounds may be used to modulate bradykinin receptor activity in vivo or in vitro, and are particularly useful
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- Benzenesulphonamide derivatives, method for production and use thereof for treatment of pain
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The present invention concerns novel benzenesulphonamide compounds, defined by formula I and the description, their method of preparation and their use in therapy.
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Page/Page column 6
(2008/06/13)
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