- Convenient one-pot preparation of dimethyl bicyclo[2.2.2]octane-1,4- dicarbolylate, a key intermediate for a novel adenosine A1 receptor antagonist
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Dimethyl bicyclo[2.2.2]octane-1,4-dicarboxylate (4), a key starting material for a novel adenosine A1 receptor antagonist, was prepared in a one-pot reaction with convenient workup and improved yield. Copyright Taylor & Francis Group, LLC.
- Chang, HeXi,Kiesman, William F.,Petter, Russell C.
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- BRIDGED BICYCLIC COMPOUNDS FOR THE TREATMENT OF BACTERIAL INFECTIONS
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Novel bridged bicyclic compounds are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antibacterial agents. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating bacterial infections and associated diseases and conditions.
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Page/Page column 63-64
(2013/03/26)
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- SUBSTITUTED DIAMINOCARBOXAMIDE AND DIAMINOCARBONITRILE PYRIMIDINES, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
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Provided herein are Diaminopyrimidine Compounds having the following structures: wherein R1, R2, R3, and R4 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidine Compound, and methods for treating or preventing liver fibrotic disorders or a condition treatable or preventable by inhibition of a JNK pathway.
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Page/Page column 134; 135
(2012/11/07)
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- NOVEL AMIDE AND AMIDINE DERIVATIVES AND USES THEREOF
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The present invention relates to inhibitors of 11-β-hydroxysteroid dehydrogenase type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.
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Page/Page column 31
(2010/11/03)
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- HETEROBICYCLIC METALLOPROTEASE INHIBITORS
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The present invention relates generally to heterobicyclic containing pharmaceutical agents, and in particular, to heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic metalloprotease inhibiting compounds that exhibit an increased potency in relation to currently known metalloprotease inhibitors.
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Page/Page column 176-177
(2008/12/05)
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- PEPTIDASE INHIBITORS
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The present invention relates to a series of novel compounds having the formula: [INSERT FORMULA I] wherein A is a bicyclic carbocycle and R?1? and R?2? are independently [INSERT MOLECULE FROM CLAIM 1] The compounds are useful as DPP-IV inhibitors and for treating diabetes.
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Page/Page column 32-33
(2010/10/19)
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- HETEROBICYCLIC METALLOPROTEASE INHIBITORS
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The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic MMP- 13 inhibiting compounds, that exhibit an increased potency in relation to currently known MMP- 13 inhibitors.
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Page/Page column 164
(2008/06/13)
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- Adenosine receptor antagonists and methods of making and using the same
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The invention is based on the discovery that compounds of Formula I are unexpectedly highly potent and selective inhibitors of the adenosine A1receptor. Adenosine A1antagonists can be usefull in the prevention and/or treatment of numerous diseases, including cardiac and circulatory disorders, degenerative disorders of the central nervous system, respiratory disorders, and many diseases for which diuretic treatment is suitable. In one embodiment, the invention features a compound of formula I: wherein: R3is an optionally substituted bicyclic, tricylic, or pentacyclic group selected from: ?and wherein R1, R2, R6, X1, X2, and Z are as described in the specification.
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Page/Page column 51
(2008/06/13)
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- Synthesis of Bridgehead-Bridgehead Substituted Bicycloalkanes
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A convenient synthetic route to several bicycloalkanes bearing substitution at both bridgehead positions is described.The two-step procedure, which involves alkylation of the monoenolates of readily available cyclohexane diesters with 1,2-dihaloethane followed by a base-inducted cyclization of the derived haloethylated product, was successfully applied to the synthesis of dimethyl bicyclooctane-1,4-dicarboxylate, dimethyl bicycloheptane-1,4-dicarboxylate and dimethyl bicyclooctane-1,5-dicarboxylate.Additionally, it was found that the two latter diesters could be obtained in quite acceptable yields in a one-pot procedure through their corresponding cyclohexyl bisenolate precursors.
- Della, Ernest W.,Tsanaktsidis, John
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p. 1705 - 1718
(2007/10/02)
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