37005-79-1Relevant academic research and scientific papers
5-MEMBERED HETEROARYLAMINOSULFONAMIDES FOR TREATING CONDITIONS MEDIATED BY DEFICIENT CFTR ACTIVITY
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Page/Page column 431, (2021/05/21)
The invention relates to heteroaryl compounds, pharmaceutically acceptable salts thereof, and pharmaceutical preparations thereof. Also described herein are compositions and the use of such compounds in methods of treating diseases and conditions mediated by deficient CFTR activity, in particular cystic fibrosis.
6,7-DIHYDRO-4H-PYRAZOLO[1,5-A]PYRAZINE COMPOUNDS FOR THE TREATMENT OF INFECTIOUS DISEASES
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Page/Page column 72, (2018/03/26)
The present invention relates to compounds of the formula (I) or pharmaceutically acceptable salts, enantiomer or diastereomer thereof, wherein R1 to R4 are as described above. The compounds may be useful for the treatment or prophylaxis of hepatitis B virus infection.
COMPOUNDS AND COMPOSITIONS USEFUL FOR TREATING DISORDERS RELATED TO NTRK
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Page/Page column 46; 47, (2017/03/14)
This invention relates to inhibitors of NTRK that are active against wild-type NTRK and its resistant mutants.
IN-SITU GENERATION OF RUTHENIUM CATALYSTS FOR OLEFIN METATHESIS
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Paragraph 0141; 0142; 0143, (2016/02/22)
The present invention relates to a process for preparing olefins by means of metathesis, which comprises the following steps a. provision of an olefin reaction mixture containing at least one olefin, b. addition of a ruthenium compound of the general formula [RuX2L1xL2y]z (I), where X=anionic ligand; L1=uncharged π-bonding ligand; L2=uncharged electron donor ligand; x=0, 1; y=1, 2, 3; z=1, 2, c. addition of a Lewis acid and/or an anionic, noncoordinating salt, d. reaction at temperatures in the range from 30° C. to 140° C., where no addition of an alkyne or alkynol is carried out. The invention further relates to the use of this process in metathesis reactions.
4-Aminocyclopentane-1,3-diols as platforms for diversity: Synthesis of a screening library
Zohrabi-Kalantari,Wilde,Grünert,Bednarski,Link
, p. 203 - 213 (2014/03/21)
Trisubstituted cyclopentanes have a discrete shapely curvature. While the central ring of these compounds is devoid of rotatable bonds, the pseudo rotation of the cyclopentane ring leads to a desirable disruption of planarity. This is favorable for aqueous solubility and enables addressing of wide-ranging conformational space. The sp3-rich framework of 4-aminocyclopentane- 1,3-diols offers stereochemically defined attachment points for substituents and renders these fragment-like molecules good platforms for molecular diversity. By using an established N-selective polymer-assisted acylation protocol, these scaffolds with natural product-like properties were transformed into a screening library by attachment of substituents at defined positions. Here we describe the synthesis and characterization of these molecular platforms and their use as starting points for the construction of an 80-member library of 4-amidocyclopentane-1,3-diol monoethers. Five of the compounds displayed cytotoxicity in a tumor cell line assay with IC50 values in the low micromolar range.
Lewis acid assisted ruthenium-catalyzed metathesis reactions
Luebbe, Christa,Dumrath, Andreas,Neumann, Helfried,Beller, Matthias,Kadyrov, Renat
, p. 105 - 108 (2014/01/23)
The combination of a ruthenium-arene complex, a noncoordinating salt, and a Lewis acid facilitates access to a highly active and selective in situ metathesis catalyst. The catalyst is formed from an inexpensive ruthenium precursor and olefins are used as the substrates. RCM=Ring-closing metathesis, acac=acetylacetonate. Copyright
4-aminocyclopentane-1,3-diols as platforms for diversity: Synthesis of anandamide analogs
Zohrabi-Kalantari, Vida,Jarrahian, Abbas,Bissantz, Caterina,Bergstrom, Donald E.,Barker, Eric L.,Link, Andreas
, p. 881 - 888 (2013/09/23)
Starting from cyclopentadiene, two racemic mixtures of 4-aminocyclopentane- 1,3-diols were prepared in 8 steps and characterized. Structure determination proved the anticipated trans-orientation of the two oxygen atoms with respect to the plane of the ring. The fragment-like new compounds are small and hydrophilic, devoid of rotatable bonds, and offer stereochemically defined attachment points for substituents. Thus, these platforms for diversity are suitable starting points for the construction of combinatorial libraries of lead-like 4-amidocyclopentane-1,3-diols or natural product analogs. As a proof of concept, cyclopentanoid anandamide analogs were prepared using these molecular platforms and evaluated as tools for the investigation of unresolved issues in the molecular biology of anandamide.
Low catalyst loading in ring-closing metathesis reactions
Kadyrov, Renat
supporting information, p. 1002 - 1012 (2013/02/23)
An efficient procedure is described for ring-closing metathesis reactions. A conversion of 95 % for diethyl diallylmalonate in dilute solution could be achieved within a few minutes, reaching TOF=4173min-1, with very low loading of commercially available Ru catalysts that contained unsaturated NHC ligands. In general, only 50 to 250ppm of the catalyst is required to achieve near-quantitative conversion into a broad variety of 5-16-membered heterocyclic compounds. The practicality of this procedure was illustrated in the synthesis of 5-8-membered N-tert-butoxycarbonyl (N-Boc)- and N-para-toluenesulfonyl (N-Ts)-protected cyclic amines and 9-16-membered lactones. The synthesis of macrocyclic proline-based lactams required slightly higher catalyst loadings. Along with monocyclic products, oligomeric byproducts, mostly cyclodimers, were isolated and characterized. Getting some closure: An efficient procedure is described for ring-closing metathesis reactions in which only 50 to 250ppm of catalyst is required to effect almost-quantitative conversion into a broad range of 5-16-membered heterocyclic compounds. The practicality of this procedure was illustrated in the synthesis of 5-8-membered N-protected cyclic amines, 9-16-membered lactones, and 11-16-membered proline-based lactams. Copyright
FUSED HETEROAROMATIC PYRROLIDINONES
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, (2011/07/06)
Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, L1, L2, R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, pharmaceutical compositions containing them, and their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other disorders, diseases, and conditions for which inhibition of SYK is indicated.
PTERIDINONES AS INHIBITORS OF POLO - LIKE KINASE
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Page/Page column 86-88, (2011/07/09)
The present invention provides compounds having a structure according to Formula (I) or a salt or solvate thereof, wherein ring A, X, R1, R2, R3, R4, R5 and R6, are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.
