- HETEROARYLDIHYDROPYRIMIDINE DERIVATIVES AND METHODS OF TREATING HEPATITIS B INFECTIONS
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Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
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Page/Page column 146
(2020/07/14)
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- PYRIDOPYRIMIDINE COMPOUNDS ACTING AS MTORC 1/2 DOUBLE-KINASE INHIBITORS
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Disclosed are a series of pyridopyrimidine compounds and a use of same in the preparation of drugs associated with mTORC 1/2 dual complex inhibitors, and specifically disclosed is a use of the compounds as shown in formula (IV), tautomers thereof or pharmaceutically acceptable salts thereof in the preparation of drugs associated with mTORC 1/2 dual complex inhibitors.
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Paragraph 0366-0368
(2020/11/30)
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- Synthesis of the First Representatives of Spiro-1λ6-isothiazolidine-1,1,4-triones
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A strategy for the construction of spiro[cycloalkane-1,3′-1′λ6-isothiazolidine]-1′,1′,4′-triones through the sulfonylation of 1-aminocyclopropane- and 1-aminocyclobutanecarboxylates with methanesulfonyl chloride followed by alkylation with methyl iodide and subsequent cyclization in the presence of potassium tert-butoxide in N,N-dimethylformamide is reported. An efficient synthesis of starting 1-aminocyclopropane- and 1-aminocyclobutanecarboxylic acids was developed. The reaction of spiro[cycloalkane-1,3′-1′λ6-isothiazolidine]-1′,1′,4′-triones with N,N-dimethylformamide dimethyl acetal (DMF-DMA) gives 5′-[(Z)-(dimethylamino)methylene]spiro[cycloalkane-1,3′-1′λ6-isothiazolidine]-1′,1′,4′-triones, the structure of which was confirmed by X-ray diffraction study.
- Dobrydnev, Alexey V.,Popova, Maria V.,Saffon-Merceron, Nathalie,Listunov, Dymytrii,Volovenko, Yulian M.
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p. 2523 - 2528
(2015/09/01)
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- POLO-LIKE KINASE INHIBITORS
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Compounds of the following formula are provided for use with kinases, wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful
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Page/Page column 281-282
(2009/06/27)
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- Synthesis of 3-aminomethyl-3-fluoropiperidines
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A synthetic route toward new 1-alkyl-3-aminomethyl-3-fluoropiperidines, which are of high interest as building blocks in medicinal chemistry, is described. The successful approach consists of the fluorination of ethyl 3-chloropropyl-2-cyanoacetate with Nf
- Van Hende, Eva,Verniest, Guido,Thuring, Jan-Willem,Macdonald, Gregor,Deroose, Frederik,De Kimpe, Norbert
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scheme or table
p. 1765 - 1768
(2009/12/05)
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- AMIDE SUBSTITUTED IMIDAZOPYRIDINES, IMIDAZOQUINOLINES, AND IMIDAZONAPHTHYRIDINES
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Imidazopyridine, imidazoquinoline, and imidazonaphthyridine compounds having an amide substituent at the 1-position, pharmaceutical compositions containing the compounds, intermediates, and methods of making and methods of use of these compounds as immunomodulators, for modulating cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
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Page/Page column 75
(2010/11/28)
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- 1-BENZYLINDOLE-2-CARBOXAMIDE DERIVATIVES
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The present invention relates to i-benzylindole-2-carboxamide derivatives of formula I, or a pharmaceutically acceptable salt or solvate thereof. The invention also relates to pharmaceutical compositions comprising said 1-benzylindole-2-carboxamide deriva
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Page/Page column 50
(2010/11/24)
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- Anionic ring-opening polymerization of alkyl 1- cyanocyclopropanecarboxylates
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Poly(alkyl 1-cyanotrimethylene-1-carboxylate)s (CH2CH 2C(CN)(COOR))n are the next higher chain homologues of poly(α-cyanoacrylate)s. They were synthesized via the anionic ring-opening polymerization of the corresponding alkyl 1-cyanocyclopropanecarboxylate monomers initiated with thiophenolate salts (PhSM, with M = Li, Na, K, and NBu4) and at temperatures above 50°C. Precipitation of the growing polymer chains at an early stage during the polymerization did not prevent further propagation, probably via polymerization in the solid or at the solid surface. The propagating cyanoacetate carbanion is very stable in a normal air atmosphere, surviving for long periods of time in the absence of strong acids. Although monodisperse polymers were obtained in most experiments (M w/Mn + and NBu 4+ counterions were used. Nonquantitative initiations characterized polymerizations initiated by PhSLi and PhSNa. Attempted polymerizations of ethyl 1-cyanocyclobutanecarboxylate failed under similar or slightly more energetic experimental conditions, with the thiophenolate initiator attacking the pendant ester rather than the cyclic methylene group.
- Kagumba, Lawino C.,Penelle, Jacques
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p. 4588 - 4594
(2007/10/03)
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- CATHODIC SYNTHESIS OF CYCLOBUTANES
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Cathodic electrolysis of compounds with an activated methylene group in the presence of 1,3-dibromopropane affords 1,1-disubstituted cyclobutanes.
- Vasil'ev, A. A.,Tatarinova, V. I.,Petrosyan, V. A.
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p. 1221 - 1224
(2007/10/02)
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- A FACILE PROCEDURE FOR THE PREPARATION OF ALICYCLIC α-AMINO ACIDS
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A convenient method for the preparation of alicyclic α-amino acids is described which utilizes ethyl isocyanoacetate and the appropriate dibromo-substituted aliphatic alkylating agent.
- Kalvin, Douglas,Ramalingam, Kondareddiar,Woodward, Ronald
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p. 267 - 272
(2007/10/02)
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- CYCLOALKYLATION BY THE α,ω-DIBROMIDES OF COMPOUNDS CONTAINING AN ACTIVATED METHYLENE GROUP AS A METHOD FOR THE SYNTHESIS OF 1,1-DISUBSTITUTED CYCLOALKENES
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A convenient preparative method was developed for the cycloalkylation of active methylene compounds, including β-diketones, by the dibromides BrCH2(CH2)nCH2Br (n = 0,1,2) in the presence of an excess of potassium carbonate in DMSO.The reaction gives high yields for the dibromides with n = 0 and 2, whereas the formation of cyclobutanes (n=1) is complicated by O,C-alkylation.The 1-substituted 1-acylcyclopropanes undergo thermal isomerization to the corresponding dihydrofuranes.
- Zefirov, N. S.,Kuznetsova, T. S.,Kozhushkov, S. I.,Surmina, L. S.,Rashchupkina, Z. A.
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p. 474 - 480
(2007/10/02)
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- 6-(Substituted-cycloalkylcarboxamide) penicillanic acids
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Penicillins of the formula SPC1 Or a pharmaceutically-acceptable, nontoxic salt thereof, Wherein R1 and R2 are the same or different and each is hydrogen, fluorine, chlorine or bromine; or when R2 is hydrogen, R1 can also be cyano, hydroxyl, azido, amino or nitro; or R1 and R2 are bonded to a ring carbon atom and constitute a single oxygen atom; R3 is hydrogen, methyl, chlorine, bromine, cyano, methoxy or carboxyl; and n is 2 to 7; Are useful for their antibacterial activity.
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