- 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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- 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 00581
(2021/04/01)
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- TRICYCLIC LACTAMS FOR USE IN THE PROTECTION OF NORMAL CELLS DURING CHEMOTHERAPY
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This invention is in the area of tricyclic lactam compounds, compositions and methods of protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC) as well as renal cells, from damage associated with DNA damaging chemotherapeutic agents. In one aspect, protection of healthy cells is disclosed using compounds that act as cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects undergoing DNA damaging chemotherapeutic regimens for the treatment of proliferative disorders.
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Page/Page column 119-120
(2015/11/09)
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- NITRATED HYDROCARBONS, DERIVATIVES, AND PROCESSES FOR THEIR MANUFACTURE
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Provided is a process for the formation of nitrated compounds by the nitration of hydrocarbon compounds with dilute nitric acid. Also provided are processes for preparing industrially useful downstream derivatives of the nitrated compounds, as well as novel nitrated compounds and derivatives, and methods of using the derivatives in various applications.
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Page/Page column 37-38
(2009/12/02)
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- AMINOALCOHOL AND BIOCIDE COMPOSITIONS FOR AQUEOUS BASED SYSTEMS
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Biocidal compositions and their use in aqueous media, such as metalworking fluids, the compositions comprising a biocidal agent; and a non-biocidal primary amino alcohol compound of the formula (I): wherein R1, R2, R3, R4, and R5 are as defined herein.
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Page/Page column 14
(2009/12/23)
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- Sterically demanding, bioxazoline-derived N-heterocyclic carbene ligands with restricted flexibility for catalysis
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A unique family of N-heterocyclic carbenes derived from bioxazolines (IBiox) suitable for application in transition-metal catalysis is described. The ligands are electron rich, sterically demanding, and have restricted flexibility. Their usefulness has been demonstrated in the Suzuki-Miyaura cross-coupling of sterically hindered aryl chlorides and boronic acids. For the first time, tetraortho-substituted biaryls with methyl and larger ortho-substituents have been synthesized from aryl chlorides using the Suzuki-Miyaura method.
- Altenhoff, Gereon,Goddard, Richard,Lehmann, Christian W.,Glorius, Frank
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p. 15195 - 15201
(2007/10/03)
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- Substituted 2-arylimino heterocycles and compositions containing them, for use as progesterone receptor binding agents
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This invention relates to 2-arylimino heterocycles, including 2-arylimino-1,3-thiazolidines, 2-arylimino-2,3,4,5-tetrahydro-1,3-thiazines, 2-arylimino-1,3-thiazolidin-4-ones, 2-arylimino-1,3-thiazolidin-5-ones, and 2-arylimino-1,3-oxazolidines, and their use in modulating progesterone receptor mediated processes, and pharmaceutical compositions for use in such therapies.
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Page column 30-31
(2010/02/05)
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- Enantioselective route to key intermediates in the synthesis of carbocyclic phosphoribosyltransferase transition state analogues
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The enantioselective preparation of key intermediates in the synthesis of transition state analogues of hypoxanthine-guanine phosphoribosyltransferase, (1S,2S,3R,4R)-4-acetoxymethyl-1-bromomethyl-2,3-isopropylidenedioxy-1- toluenesulfonamidocyclopentane (3a) and the 4-nitrobenzenesulfonamido analogue (3b), are described.
- Ahmadian, Mohammad,Khare, Naveen K.,Riordan, James M.,Klon, Anthony E.,Borhani, David W.
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p. 9899 - 9909
(2007/10/03)
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- Cyclit-Reaktionen, II. Darstellung von Bausteinen zur Synthese carbocyclischer Furanose-Analoga
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The four isomeric hydroxycyclopentenmethanols 6a to 9a can easily be made by allylhydroxylation of the epoxides 2 and 4 with phenyl selenide.In a second way the pair 8a and 9a has been synthesized from 11 via 15.As the preparation of 20 demonstrates, the functionalisation of 6a to 9a to carbocyclic furanoses is possible.The dicarboxylic diethyl esters 23 and 33 can be converted into models for carbocyclic ketofuranoses.
- Paulsen, Hans,Maass, Uwe
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p. 346 - 358
(2007/10/02)
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