- 2,3-DIHYDRO-1H-PYRROLIZINE-7-FORMAMIDE DERIVATIVE AND APPLICATION THEREOF
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The present application relates to a 2,3-dihydro-1H-pyrrolizine-7-formamide derivative as a nucleoprotein inhibitor and a use in preparation of a drug for treating HBV related diseases. The present application specifically relates to a compound represented by formula (II), and isomers or pharmaceutically acceptable salts thereof.
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Paragraph 0257; 0258; 0259; 0260
(2021/04/16)
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- Preparation method of heterocyclic compound and salt thereof
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The invention belongs to the field of organic chemistry and specifically relates to a preparation method of a heterocyclic compound as shown in the formula I and salt thereof. In comparison with the prior art, the invention has the following beneficial effects: the use of the extremely toxic substance cyanide is avoided; there is no cyanide ion residue in the reaction product and the reaction waste such that environmental burden is greatly reduced. In addition, the price of the reaction materials is low; the preparation method is simple; the yield is high; and the preparation method is suitable for large-scale industrial production. It is found unexpectedly that by the adoption of the method of the scheme 4, such as use of a reducing agent and under the acidic condition, the compound VIIIcan be obtained by one-step reaction and the off-protecting group, alkylation and cyano group reduction are realized to obtain the target product. The defect that polystep reactions are required in the prior art is greatly improved.
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Paragraph 0148-0150
(2019/07/01)
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- Primary α-tertiary amine synthesis via α-C-H functionalization
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A quinone-mediated general synthetic platform for the construction of primary α-tertiary amines from abundant primary α-branched amine starting materials is described. This procedure pivots on the efficient in situ generation of reactive ketimine intermediates and subsequent reaction with carbon-centered nucleophiles such as organomagnesium and organolithium reagents, and TMSCN, creating quaternary centers. Furthermore, extension to reverse polarity photoredox catalysis enables reactivity with electrophiles, via a nucleophilic α-amino radical intermediate. This efficient, broadly applicable and scalable amine-to-amine synthetic platform was successfully applied to library and API synthesis and in the functionalization of drug molecules.
- Vasu, Dhananjayan,Fuentes de Arriba, Angel L.,Leitch, Jamie A.,De Gombert, Antoine,Dixon, Darren J.
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p. 3401 - 3407
(2019/03/21)
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- PYRIMIDINE-BASED ANTIPROLIFERATIVE AGENTS
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This invention is in the area of pyrimidine-based compounds for the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers.
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Page/Page column 172; 197
(2018/02/28)
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- PYRIMIDINE-BASED COMPOUNDS FOR THE TREATMENT OF CANCER
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This invention is in the area of pyrimidine-based compounds for the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers.
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Page/Page column 126-127
(2018/02/28)
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- Design and Synthesis of Fsp3-Rich, Bis-Spirocyclic-Based Compound Libraries for Biological Screening
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The exploration of innovative chemical space is a critical step in the early phases of drug discovery. Bis-spirocyclic frameworks occur in natural products and other biologically relevant metabolites and show attractive features, such as molecular compactness, structural complexity, and three-dimensional character. A concise approach to the synthesis of bis-spirocyclic-based compound libraries starting from readily available commercial reagents and robust chemical transformations has been developed. A number of novel bis-spirocyclic scaffold examples, as implemented in the European Lead Factory project, is presented.
- Stotani, Silvia,Lorenz, Christoph,Winkler, Matthias,Medda, Federico,Picazo, Edwige,Ortega Martinez, Raquel,Karawajczyk, Anna,Sanchez-Quesada, Jorge,Giordanetto, Fabrizio
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supporting information
p. 330 - 336
(2016/07/06)
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- 3-PYRIDYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS
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The invention provides certain 3-pyridyl carboxamide-containing compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
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Paragraph 00178
(2013/04/24)
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- 2-PYRIDYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (SYK) INHIBITORS
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The invention provides certain 2-pyridyl carboxamide-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
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Paragraph 00262
(2013/04/24)
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- HALOALKYL CONTAINING COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
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The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
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Page/Page column 80
(2008/06/13)
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- Compounds useful as reversible inhibitors of cysteine proteases
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Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds.
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- METHOD OF INDUCING ANTIANDROGENIC ACTIVITY USING IMIDAZOLIDINES SUBSTITUTED WITH A HETEROCYCLE
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Novel imidazoles of the formula STR1 wherein the substituents are as defined in the disclosure and their non-toxic, pharmaceutically acceptable addition salts with acids and bases having antiandrogenic activity.
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