- Arab league swiss tanzania and luck sha pitan chain fragment preparation method (by machine translation)
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The invention relates to a process for preparing arab league swiss tanzania and luck sha pitan chain fragment of the new method, in particular to the preparation of 5 - chloromethyl - 2, 4 - dihydro [1, 2, 4] triazole - 3 - ones. This method uses the 2 - benzyloxy bromide and animal pen amidogen chloride as the starting material, first of all the one-pot synthesis to achieve 5 - hydroxymethyl - 2, 4 - dihydro [1, 2, 4] triazole - 3 - ketone preparation, then 5 - hydroxymethyl - 2, 4 - dihydro [1, 2, 4] triazole - 3 - ketone SOCl2 Under the effect of the 5 - chloromethyl - 2, 4 - dihydro [1, 2, 4] triazole - 3 - one of the preparation. (by machine translation)
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Paragraph 0022
(2019/04/06)
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- Synthetic method of 3-chloromethyl-1,2,4-triazolin-5-one
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The invention relates to a synthetic method of 3-chloromethyl-1,2,4-triazolin-5-one. The 3-chloromethyl-1,2,4-triazolin-5-one is prepared by mixing chloroacetonitrile, an alcohol and a solvent A. Compared with a conventional process, the synthesis method has the advantages that the raw materials with low price are selected, and production cost is remarkably reduced. For the whole technological process, the synthetic route is shortened, and production efficiency is improved. Production operation and quality control are more convenient while the production process is simplified.
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Paragraph 0019; 0020
(2019/04/26)
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- NOVEL COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE INHIBITORS
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Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme:(I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
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Page/Page column 65
(2017/07/14)
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- PYRROLO[2,3-B]PYRIDINE CDK9 KINASE INHIBITORS
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Disclosed are compounds of Formula (IIa), wherein R1, R2, R3A, R3B, R3C, R3D, R3E, and R4 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds may be used as agents in the treatment of diseases, including cancer. Also provided are pharmaceutical compositions comprising one or more compounds of Formula (IIa)
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Page/Page column 614
(2014/09/29)
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- SUBSTITUTED NAPHTHYRIDINES AND THEIR USE AS MEDICAMENTS
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The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein R1 is selected from among —O—R3 or —NR3R4,R3 is C1-6-alkyl which is substituted by R5 and R6,R5 is selected from hydrogen, branched or linear C1-6-alkyl, C2-6-alkenyl, —C1-6-alkylen-O—C1-3-alkyl, C1-3-haloalkyl,R6 is ring X wherein n is either 0 or 1, and is a either a single or a double bond andwherein A, B, D and E are each independently from one another selected from CH2, CH, C, N, NH, O or S and wherein ring X is attached to the molecule either via position A, B, D or E, wherein said ring X may optionally be further substituted by one, two or three residues each selected individually from the group consisting of -oxo, hydroxy, —C1-3-alkyl, —C1-3-haloalkyl, —O—C1-3-alkyl, —C1-3-alkanol and halogen,and wherein R4, R2, R7, R8, R9, R10, R11 and Q may have the meanings as given in claim 1, as well as pharmaceutical compositions containing these compounds.
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Page/Page column 27
(2012/02/06)
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- SUBSTITUTED NAPHTHYRIDINES AND THEIR USE AS SYK KINASE INHIBITORS
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The invention relates to new substituted naphthyridines of formula (1), as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein R1 is selected from among -O-R3 or -NR3R4, R3 is C1-6-alkyl which is substituted by R5 and R6 R5 is selected from hydrogen, branched or linear C1-6-alkyl, C2-6-alkenyl, -C1-6-alkylen-O-C1-3-alkyl, C1-3-haloalkyl, R6 is ring X wherein n is either 0 or 1, and Formula (I) is a either a single or a double bond and wherein A, B, D and E are each independently from one another selected from CH2, CH, C, N, NH, O or S and wherein ring X is attached to the molecule either via position A, B, D or E, wherein said ring X may optionally be further substituted by one, two or three residues each selected individually from the group consisting of -oxo, hydroxy, -C1-3-alkyl, -C1-3-haloalkyl, -O-C1-3-alkyl, -C1-3-alkanol and halogen, and wherein R4, R2, R7, R8, R9, R10, R11 and Q may have the meanings as given in claim 1, as well as pharmaceutical compositions containing these compounds.
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Page/Page column 51-52
(2011/08/21)
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- BETA CARBOLINES AND USES THEREOF
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This invention provides beta-carboline compounds of formula I: wherein R1, R2, R3, R4, R5, G, and x are as described in the specification. The compounds are useful for treating cancer and inflammatory disorders.
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Page/Page column 69
(2009/06/27)
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- COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY
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The invention encompasses compounds having formula (I-V) and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.
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Page/Page column 276
(2008/06/13)
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- Process for the preparation of 1,2,4- triazolin-5-one derivatives
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The present invention relates to a process for the preparation of a compound of formula (I) wherein R represents hydrogen, C1-10alkyl, haloC1-10alkyl or aryl; which are useful intermediates in the preparation of morpholine derivatives of formula (A). Compounds of formula (A) are useful as therapeutic agents.
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- Chemical synthesis of morpholine derivatives
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The present invention relates to a process for the preparation of mopholine derivatives of formula (I) which are useful as a therapeutic agents.
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- A new synthesis of 1,2,4-triazolin-5-ones: Application to the convergent synthesis of an NK1 antagonist
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Chlorotriazolinone 4 has been synthesised in a single step via the novel condensation of semicarbazide hydrochloride with orthoester 8. Alkylation of secondary amine 3 with compound 4 proceeds in 99% yield to afford the target NK1 antagonist 1. (C) 2000 Published by Elsevier Science Ltd.
- Cowden,Wilson,Bishop,Cottrell,Davies,Dolling
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p. 8661 - 8664
(2007/10/03)
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- PHARMACOLOGICALLY ACTIVE THIOUREA AND UREA COMPOUNDS
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The compounds are substituted thioalkyl-, aminoalkyl-and oxyalkyl-thioureas and ureas which are inhibitors of histamine activity.
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