187541-61-3Relevant academic research and scientific papers
COMPOUNDS AND METHODS FOR INHIBITING NHE-MEDIATED ANTIPORT IN THE TREATMENT OF DISORDERS ASSOCIATED WITH FLUID RETENTION OR SALT OVERLOAD AND GASTROINTESTINAL TRACT DISORDERS
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Page/Page column 205, (2010/08/04)
The present disclosure is directed to corn- pounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders. The methods generally comprise administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that is designed to be substantially active in the gastrointestinal (GI) tract to inhibit NHE-mediated antiport of sodium ions and hydrogen ions therein. More particularly, the method comprises administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that inhibits NHE-3, -2 and/ or -8 mediated antiport of sodium and/or hydrogen ions in the GI tract and is designed to be substantially impermeable to the layer of epithelial cells, or more specifically the epithelium of the GI tract. As a result of the compound being substantially impermeable, it is not absorbed and is thus essentially systemically non-bioavailable, so as to limit the exposure of other internal organs (e.g., liver, heart, brain, etc.) thereto. The present disclosure is still further directed to a method wherein a mammal is administered such a compound with a fluid-absorbing polymer, such that the combination acts as described above and further provides the ability to sequester fluid and/or salt present in the GI tract
Substituted acylguanidines, process for their preparation, their use as medicaments or diagnostics, and medicaments comprising them
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, (2008/06/13)
Substituted acylguanidines and their pharmaceutically tolerable salts and physiologically functional derivatives. Compounds of the formula I in which the radicals have the meanings indicated, and their physiologically tolerable salts, physiologically func
SUBSTITUTED CINNAMIC, ACID GUANIDIDES, PROCESS FOR THEIR PREPARATION, THEIR USE AS A MEDICAMENT, AND MEDICAMENT COMPRISING THEM
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, (2008/06/13)
Substituted cinnamic acid guanidides, process for their preparation, their use as a medicament or diagnostic, and medicament comprising them. Compounds of the 1, which may be obtained by reaction of a compound II 2with guanidine.
Substituted phenylalkenoylguanidines, process for their preparation, and their use in medicaments and in diagnostics
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, (2008/06/13)
Substituted phenylalkenoylguanidines, processes for their preparation, uses as medicaments or diagnostics, and medicaments containing them are described. The invention relates to substituted phenylalkenoylguanidines and their pharmaceutically tolerable sa
Substituted cinnamic acid guanidides, a process for their preparation, their use as medicaments or diagnostic agents and medicaments comprising them
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, (2008/06/13)
Compounds of the formula I STR1 are described in which at least one of the substituents R(1), R(2), R(3), R(4) and R(5) is a nitrogen-containing heterocyclic radical. They are outstanding cardiovascular therapeutic agents. They are obtained by reaction of
