82353-76-2Relevant academic research and scientific papers
5-MEMBERED HETEROARYLAMINOSULFONAMIDES FOR TREATING CONDITIONS MEDIATED BY DEFICIENT CFTR ACTIVITY
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, (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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, (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 46-48, (2017/03/14)
This invention relates to inhibitors of NTRK that are active against wild-type NTRK and its resistant mutants.
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.
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.
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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, (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.
Epoxide rearrangements using dilithiated aminoalcohols as chiral bases
Brookes, Paul C,Milne, David J,Murphy, Patrick J,Spolaore, Barbara
, p. 4675 - 4680 (2007/10/03)
Dilithiated norephedrine and ephedrine have been utilised in the enantioselective rearrangement of cyclic epoxides to allylic alcohols, with dilithiated norephedrine generally giving the best enantioselectivity. Dilithiated ephedrine offered better levels
Asymmetric microbial hydrolysis of epoxides
Mischitz,Kroutil,Wandel,Faber
, p. 1261 - 1272 (2007/10/03)
Kinetic resolution of 2-mono- and 2,2-disubstituted epoxides was accomplished using epoxide hydrolases from bacterial and fungal origin by employing lyophilized whole microbial cells. In all cases investigated, the biocatalytic hydrolysis was shown to proceed with retention of configuration at the stereogenic center leading to 1,2-diols and remaining epoxides. The selectivity of the reaction was dependent on the substrate structure and the strain used with E-values ranging from low or moderate (with 2-monosubstituted epoxides) to excellent (E >100, with 2,2-disubstituted oxiranes).
Dilithiated Aminoalcohols as Homochiral Bases
Milne, David,Murphy, Patrick J.
, p. 884 - 886 (2007/10/02)
The dilithium salts of (+)- or (-)-norephedrine effect the enantioselective and enantiodivergent deprotonation of meso-epoxide 17 in higher enantiomeric excess than previously reported.
