- SUBSTITUTED, SATURATED AND UNSATURATED N-HETEROCYCLIC CARBOXAMIDES AND RELATED COMPOUNDS FOR THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS
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The invention provides substituted, saturated and unsaturated N-heterocyclic carboxamides and related compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., cancer, lysosomal storage disorder, neurodegenerative disorder, inflammatory disorder, in a patient.
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Paragraph 00448
(2021/04/01)
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- meta-Selective C?H Borylation of Benzylamine-, Phenethylamine-, and Phenylpropylamine-Derived Amides Enabled by a Single Anionic Ligand
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Selective functionalization at the meta position of arenes remains a significant challenge. In this work, we demonstrate that a single anionic bipyridine ligand bearing a remote sulfonate group enables selective iridium-catalyzed borylation of a range of common amine-containing aromatic molecules at the arene meta position. We propose that this selectivity is the result of a key hydrogen bonding interaction between the substrate and catalyst. The scope of this meta-selective borylation is demonstrated on amides derived from benzylamines, phenethylamines and phenylpropylamines; amine-containing building blocks of great utility in many applications.
- Davis, Holly J.,Genov, Georgi R.,Phipps, Robert J.
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supporting information
p. 13351 - 13355
(2017/10/07)
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- Heterocyclic compound with Wnt signal path inhibitory activity and application thereof
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The invention provides a heterocyclic compound with Wnt signal path inhibitory activity. The heterocyclic compound and chemically acceptable salt, isotope, isomer and a crystal structure thereof are provided with a structure shown as the general formula I (see the formula in the description). The invention further provides application of the heterocyclic compound with the Wnt signal path inhibitory activity. The heterocyclic compound with the Wnt signal path inhibitory activity serves as effective antagonist of a Wnt signal path, and can be used for treating or preventing diseases caused by abnormity of the Wnt signal path.
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Paragraph 0191; 0192; 0193
(2016/10/08)
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- ARYL LINKED IMIDAZOLE AND TRIAZOLE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG
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The present invention relates to aryl linked imidazole and triazole derivatives, compositions comprising said compounds, alone or in combination with other drugs, and methods of using the compounds for improving the pharmacokinetics of a drug. The compounds of the invention are useful in human and veterinary medicine for inhbiting CYP3A4 and for improving the pharmacokinetics of a therapeutic compound that is metabolized by CYP3A4.
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Page/Page column 83
(2015/06/03)
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- ARYL LINKED IMIDAZOLE AND TRIAZOLE DERIVATIVES AND METHODS OF USE THEREOF FOR IMPROVING THE PHARMACOKINETICS OF A DRUG
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The present invention relates to aryl linked imidazole and triazole derivatives, compositions comprising said compounds, alone or in combination with other drugs, and methods of using the compounds for improving the pharmacokinetics of a drug. The compounds of the invention are useful in human and veterinary medicine for inhbiting CYP3A4 and for improving the pharmacokinetics of a therapeutic compound that is metabolized by CYP3A4.
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Page/Page column 82
(2015/06/03)
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- Radical cyclization of ynamides into six- or eight-membered rings. Application to the synthesis of a protoberberine analog
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A straightforward formation of six- and eight-membered rings via the radical cyclization of specifically designed ynamides is reported. This strategy provides a protoberberine analog in only three steps by a radical cyclization cascade.
- Balieu, Sébastien,Toutah, Krimo,Carro, Laura,Chamoreau, Lise-Marie,Rousselière, Hélène,Courillon, Christine
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supporting information; experimental part
p. 2876 - 2880
(2011/06/21)
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- Iridium-catalyzed asymmetric intramolecular allylic amidation: Enantioselective synthesis of chiral tetrahydroisoquinolines and saturated nitrogen heterocycles
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For the first time iridium catalysis has been used for the synthesis of chiral tetrahydroisoquinolines with excellent yields and high enantioselectivities (see scheme; cod=1,5-cyclooctadiene, DBU=1,8- diazabicyclo[5.4.0]undec-7-ene). These products are important chiral building blocks for the synthesis of biologically active compounds, in particular alkaloids. Copyright
- Teichert, Johannes F.,Fananas-Mastral, Martin,Feringa, Ben L.
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supporting information; experimental part
p. 688 - 691
(2011/04/18)
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- 1,2,3,4-Tetrahydropyrazin-2-yl acetamides and methods of use
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Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and
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Page/Page column 42
(2010/02/15)
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