429669-07-8Relevant articles and documents
Generation and electrophile trapping of N -Boc-2-lithio-2-azetine: Synthesis of 2-substituted 2-azetines
Hodgson, David M.,Pearson, Christopher I.,Kazmi, Madiha
, p. 856 - 859 (2014)
s-BuLi-induced α-lithiation-elimination of LiOMe from N-Boc-3-methoxyazetidine and further in situ α-lithiation generates N-Boc-2-lithio-2-azetine which can be trapped with electrophiles, either directly (carbonyl or heteroatom electrophiles) or after transmetalation to copper (allowing allylations and propargylations), providing a concise access to 2-substituted 2-azetines.
Chemodivergent and Stereoselective Access to Fused Isoxazoline Azetidines and Thietanes through [3 + 2]-Cycloadditions
Baumann, Andreas N.,Reiners, Felix,Juli, Thomas,Didier, Dorian
supporting information, p. 6736 - 6740 (2018/11/02)
By combining efficient methodologies for the preparation of substituted azetines and thietes with a highly regio- and diastereoselective [3 + 2]-cycloaddition, a straightforward pathway for the synthesis of fused isoxazoline azetidines and thietanes has been designed. With minimal steps and starting from commercial sources, a new library of elaborated architectures was synthesized opening up a new class of molecules with large potential in pharmacology. Finally, a retro [2 + 2]-cycloaddition leading to substituted isoxazoles is described.
PDE9I WITH IMIDAZO PYRAZINONE BACKBONE
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Page/Page column 37; 38, (2013/04/25)
This invention is directed to compounds, which are PDE9 enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The pres
HEPATITIS C INHIBITOR COMPOUNDS
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Page/Page column 50, (2011/06/23)
Compounds of Formula (I) wherein R1, R2, R3, R4 and R5 are defined herein, maintain good activity against NS3 proteases containing clinically relevant genotype 1a R155K and genotype 1b D168V resistance mutations. The compounds are useful as inhibitors of HCV NS3 protease for the treatment of hepatitis C viral infection.
NEW BRADYKININ B1 ANTAGONISTS
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Page/Page column 202, (2010/04/03)
The invention relates to compounds of formula (I) where in R1, R1a, R1b, R2, R3 and X, X1, X2, X3 have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
Process for preparing phenoxypyridine derivatives
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Page/Page column 16, (2008/12/08)
A process for preparing a compound represented by the formula (I): comprising reacting a compound represented by the formula (II) or salt thereof: with a compound represented by the formula (III): in the presence of a condensation reagent, wherein R1 represents 1) optionally substituted azetidin-1-yl, 2) optionally substituted pyrrolidin-1-yl, 3) optionally substituted piperidin-1-yl, etc.; R2, R3, R4 and R5 may be the same or different and each represents hydrogen or fluorine; and R6 represents hydrogen or fluorine.
NOVEL PYRIDINE DERIVATIVE AND PYRIMIDINE DERIVATIVE (3)
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Page/Page column 81, (2008/06/13)
A compound represented by the following formula, a salt thereof or a hydrate of the foregoing has an excellent hepatocyte growth factor receptor (HGFR) inhibitory activity, and exhibits anti-tumor activity, angiogenesis inhibitory activity and cancer metastasis inhibitory activity. [R1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents -CH=, nitrogen or the like.]
HETROARYL BENZAMIDE DERIVATIVES FOR USE AS GLK ACTIVATORS IN THE TREATMENT OF DIABETES
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Page/Page column 155, (2008/06/13)
Compounds of Formula (I) wherein: R1 is hydroxymethyl; R2 is selected from -C(O)NR4R5, SO2NR4R5, S(O)pR4 and HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; R3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R4 is selected from for example hydrogen, optionally substituted (1-4C)alkyl and HET-2; R5 is hydrogen or (1-4C)alkyl; or R4 and R5 together with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; HET-3 is for example an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; p is (independently at each occurrence) 0, 1 or 2; m is 0 or 1; n is 0, 1 or 2; provided that when m is 0, then n is 1 or 2; or a salt, pro drug or solvate thereof, are described. Their use as GLK activators, pharmaceutical compositions containing them, and processes for their preparation are also described.
1-Methylcarbapenem derivatives
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Page/Page column 135, (2010/02/05)
1-Methylcarbapenem compounds having antibacterial activity, pharmacologically acceptable esters or salts thereof and pharmaceutical compositions (particularly antibacterial agents) containing them as an active ingredient are described. In addition, the invention includes the use of these compounds, ester derivatives or salts for the manufacture of pharmaceutical compositions, or a method for the prevention or treatment of diseases (particularly bacterial infections) by administering a pharmacologically effective amount of the compounds, ester derivatives or salts to warm-blooded animals (particularly human beings).
1-METHYLCARBAPENEM DERIVATIVES
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, (2016/01/26)
The present invention relates to 1-methylcarbapenem compounds having excellent antibacterial activity, pharmacologically acceptable ester derivatives thereof, pharmacologically acceptable salts thereof, pharmaceutical compositions (particularly antibacterial agents) containing them as active ingredient, use of the compounds, ester derivatives or salts thereof for preparing such pharmaceutical compositions and a method of preventing or treating diseases (particularly bacterial infections) in which a pharmacologically effective amount of the compound, ester derivative or salt is administered to a warm-blooded animal (particularly a human being). The 1-methylcarbapenem compounds of the present invention are represented by the general formula (I): wherein:R1 is a group represented by the formula COOR3 (wherein R3 represents a hydrogen atom, a C1-C6 alkyl group or the like), a group represented by the formula CONR4R5 (wherein R4 and R5 each independently represent a hydrogen atom, a C1-C6 alkyl group which may be substituted or the like), a cyano group, a group represented by the formula CH2OR6 (wherein R6 represents a hydrogen atom, a C1-C6 alkyl group or the like) or a group represented by the formula CH2NR7R8 (wherein R7 represents a hydrogen atom, a C1-C6 alkyl group or the like, and R8 represents a hydrogen atom, a C1-C6 alkyl group, a C1-C6 alkanoyl group, a C1- C6 alkoxycarbonyl group or the like);R2 represents a hydrogen atom or a C1-C6 alkyl group;n represents 1, 2 or 3; andX represents a sulfur atom or an oxygen atom.