- Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists II: Tuning of receptor selectivity and in vivo efficacy
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In the previous article we demonstrated how certain CCK2R-selective anthranilic amides could be structurally modified to afford high-affinity, selective CCK1R activity. We now describe our efforts at modulating and optimizing the CCK1R and CCK2R affinitie
- Pippel, Marna,Boyce, Kristen,Venkatesan, Hariharan,Phuong, Victor K.,Yan, Wen,Barrett, Terrance D.,Lagaud, Guy,Li, Lina,Morton, Magda F.,Prendergast, Clodagh,Wu, Xiaodong,Shankley, Nigel P.,Rabinowitz, Michael H.
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- COMPOUNDS
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This disclosure relates to compounds of formula (I), which are modulators of STING. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and methods of using compounds of formula (I) in the treatment or prevention of diseases
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Page/Page column 96
(2021/06/26)
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- N-SUBSTITUTED-5-SUBSTITUTED PHTHALAMIC ACIDS AS SORTILIN INHIBITORS
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The present invention is directed to N-substituted-5-substituted phthalamic acids which of formula (A). The compounds are considered useful for the treatment of diseases treatment of a neurodegenerative disease, psychiatric disease, motorneuron disease, peripheral neuropathies, pain, neuroinflammation or atherosclerosis such as Alzheimer's disease and Parkinson's disease.
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Page/Page column 51
(2015/02/06)
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- Protecting-group-free synthesis of a dual CCK1/CCK2 receptor antagonist
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In our pursuit of an efficient, protecting-group-free synthesis of the dual CCK1/CCK2 receptor antagonist 1, we have developed chemoselective conditions for sulfonamide formation reaction in pure water and a PhNMe2 mediated carboxamide formatio
- Liu, Jing,Deng, Xiaohu,Fitzgerald, Anne E.,Sales, Zachary S.,Venkatesan, Hariharan,Mani, Neelakandha S.
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scheme or table
p. 2654 - 2660
(2011/05/08)
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- MODULATORS OF 5-HT RECEPTORS AND METHODS OF USE THEREOF
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The present application relates to aryl- and heteroaryl-fused decahydropyrroloazepine, octahydrooxepinopyrrole, octahydropyrrolothiazepine dioxide, decahydrocyclohepta[c]pyrrole, and octahydrocyclohepta[c]pyrrole derivatives of formula (I), wherein R1,R2, R3, R4, R5, A, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, processes for making such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.
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Page/Page column 138
(2010/12/18)
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- SULFONAMIDE COMPOUNDS
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Certain sulfonamide compounds are dual CCK1/CCK2 inhibitors useful in the treatment of CCK1/CCK2 mediated diseases.
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Page/Page column 19
(2010/10/20)
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- Quinoxaline compounds
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Certain amidophenyl-sulfonylamino-quinoxaline compounds are CCK2 modulators useful in the treatment of CCK2 mediated diseases.
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Page/Page column 15
(2008/06/13)
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- COMPOUNDS HAVING ACTIVITY AT 5HT2C RECEPTOR AND USES THEREOF
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Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein R1 is halogen, cyano, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, C1-6alkoxy, C1 6alkylthio, hydroxy, amino, mono or di C1 6alkylamino, an N-linked 4 to 7 memb
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- Condensed pyridazinyl guanidines, their production and use
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Pyridazinyl guanidines of the formula: wherein ring A is a benzene ring or a nitrogen-containing 6-membered aromatic ring, each of which may be substituted; and R1is an aromatic ring group which may be substituted, or a salt thereof, which have activity for inhibiting Na-H exchange and are useful as a prophylactic/therapeutic agent for ischemic cardiovascular diseases such as myocardial infarction and arrythmia.
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- ANGIOTENSIN II ANTAGONISTS INCORPORATING A SUBSTITUTED INDOLE OR DIHYDROINDOLE
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Substituted heterocycles attached through a methylene bridge to novel substituted indole or dihydroindole derivative of the Formula I are useful as angiotensin II antagonists. STR1
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- ANGIOTENSIN II ANTAGONISTS INCORPORATING AN INDOLE OR DIHYDROINDOLE
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There are disclosed substituted indoles and dihydroindoles of Formula I which are useful as angiotensin II antagonists. STR1
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