- Povarov reaction, scope and limitations: Preparation of diversely heterocyclic tetrahydro-1H-cyclopenta[c]quinolines
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Parallel synthesis of diverse heterocyclic-tetrahydro-1H-cyclopenta[c]quinolines in excellent yields and high endo diastereoselectivity has been described hereia These compounds are highly functionalized natural product-like tricyclic systems, which may be useful as biologically relevant targets. Fine tuning of the reaction conditions need to be performed depending on the nature and molecular structure of the heterocyclic aromatic carbaldehyde, as well as the choice of the Lewis acid catalyst. Synthesis of the heterocyclic aromatic aldehyde precursors of the Povarov Reaction is also described.
- Ni?o, Patricia,Caba, Marta,Aguilar, Nuria,Terricabras, Emma,Albericio, Fernando,Fernàndez, Joan-Carles
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p. 1117 - 1130
(2017/04/28)
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- 7A-AMIDE SUBSTITUTED-6,6-DIFLUORO BICYCLIC HIMBACINE DERIVATIVES
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The present invention relates to bicyclic himbacine derivatives of the formula (structurally represented) or a pharmaceutically acceptable salt thereof wherein: R1 is -[C(Ra)(Rb)]x-[C(Rb)(Rb)]y-C(0)NH2, or -N(H)-[(CH2)]zC(0)-NH2; W is any of the recited c
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Page/Page column 34
(2015/03/13)
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- PHARMACEUTICAL FORMULATIONS, PROCESSES, SOLID FORMS AND METHODS OF USE RELATING TO 1-ETHYL-7-(2-METHYL-6-(1H-1,2,4-TRIAZOL-3-YL)PYRIDIN-3-YL)-3,4-DIHYDROPYRAZINO[2,3-b]PYRAZIN-2(1H)-ONE
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Provided herein are formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one.
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Paragraph 0302-0304
(2014/10/29)
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- SUBSTITUTED TRICYCLIC COMPOUNDS WITH ACTIVITY TOWARDS EP1 RECEPTORS
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The present invention belongs to the field of EPl receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EPl receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EPl receptor as well as to pharmaceutical compositions comprising them.
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Page/Page column 68
(2013/10/22)
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- SUBSTITUTED TRICYCLIC COMPOUNDS WITH ACTIVITY TOWARDS EP1 RECEPTORS
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The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP1 receptor as well as to pharmaceutical compositions comprising them.
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Page/Page column 55
(2013/10/22)
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- NOVEL COMPOUNDS AS ANTAGONISTS OR INVERSE AGONISTS FOR OPIOID RECEPTORS
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This invention relates to novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy.
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Page/Page column 95
(2010/09/07)
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