- A practical method for stabilizing lithiated halogenated aromatic compounds
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An exothermic decomposition was observed during a metalation/acylation of 3,4-difluoroanisole (5), resulting in a significant thermal hazard. The lithiated anion 6 was found to decompose exothermically at temperatures above -47°C showing an adiabatic temp
- Rawalpally, Thimma,Ji, Yaohui,Shankar, Ashish,Edwards, William,Allen, Joshua,Jiang, Yong,Cleary, Thomas P.,Pierce, Michael E.
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- TRIAZOLOPYRIDINE COMPOUNDS AND USES THEREOF
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A compound of Formula (IA), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a PRC2-mediated disease or disorder: wherein A, R6, R7 and R8 are as defined herein.
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Paragraph 00142
(2018/04/11)
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- 2,3-difluoro-6-methoxybenzene process for the preparation of formaldehyde (by machine translation)
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The invention discloses a 2,3-difluoro-6-methoxybenzene process for the preparation of formaldehyde, the compound 3,4-difluoroanisole steams newly methyl tetrahydrofuran is added in, weighing anhydrous magnesium chloride, stirring the mixture at room temp
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Paragraph 0011; 0012; 0013; 0014
(2016/12/16)
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- SULTAM DERIVATIVES
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The present invention relates to compounds according to formula 1, which exhibit cytotoxic activity. The compounds may be used in the treatment of cancer.
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Page/Page column 45
(2011/06/19)
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- METHODS FOR STABILIZING LITHIATED HALOGEN-SUBSTITUTED AROMATIC COMPOUNDS
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The present invention provides novel methods for stabilizing lithiated halogen-substituted aromatic compounds. In particular, the method is useful for the preparation of 2-methoxy-5, 6-difluorobenzaldehyde, an important intermediate for the preparation of
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Page/Page column 5-6
(2009/05/28)
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- INDAZOLES USED TO TREAT ESTROGEN RECEPTOR BETA MEDIATED DISORDERS
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The present invention relates to novel indazole derivatives (I) having pharmacological activity, processes for their preparation, compositions containing them and uses of these compounds in the treatment of estrogen receptor beta mediated diseases.
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Page/Page column 27-28
(2008/12/07)
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- 3-ARYLOXY/ THIO-2, 3-SUBSTITUTED PROPANAMINES AND THEIR USE IN INHIBITING SEROTONIN AND NOREPINEPHRINE REUPTAKE
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There is provided a compound of formula (I) wherein A is selected from -O- and -S-; X is selected from phenyl optionally substituted with up to 5 substituents each independently selected from halo, C1-C4 alkyl and C1-C4 alkoxy, thienyl optionally substituted with up to 3 substituents each independently selected from halo and C1-C4 alkyl, and C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n- where n is 0, 1 or 2, -CF3, -CN and -CONH2; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl, 1,3-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to 4 or, where possible, up to 5 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n- where n is 0, 1 or 2, nitro, acetyl, -CF3, -SCF3 and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C1-C4 alkyl; Z is selected from OR3 or F, wherein R3 is selected from H, C1-C6 alkyl and phenyl C1-C6 alkyl; R1 and R2 are each independently H or C1-C4 alkyl; and pharmaceutically acceptable salts thereofwith the proviso that when Y is optionally substituted phenyl or optionally substituted 1,3-benzodioxolyl and Z is OR3 and X is optionally substituted phenyl then A is -S-.
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Page 40 - 41
(2010/02/07)
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- Benzothienyloxy phenylpropanamines, novel dual inhibitors of serotonin and norepinephrine reuptake
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A series of benzothienyloxy phenylpropylamines have been prepared and are demonstrated to be inhibitors of both serotonin and norepinephrine reuptake. A series of benzothienyloxy propylamines have been prepared and are demonstrated to be inhibitors of both serotonin and norepinephrine reuptake.
- Boot,Brace,Delatour,Dezutter,Fairhurst,Findlay,Gallagher,Hoes,Mahadevan,Mitchell,Rathmell,Richards,Simmonds,Wallace,Whatton
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p. 5395 - 5399
(2007/10/03)
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- Heterocyclcarboxamide derivatives and their use as therapeutic agents
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Compounds of formula I STR1 and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R1 is an optional substituent; U is an alkylene chain optionally substituted by one or more alkyl; Q
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- Phenethylthiazolylthiourea (PETT) compounds as a new class of HIV-1 reverse transcriptase inhibitors. 2. Synthesis and further structure-activity relationship studies of PETT analogs
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Phenylethylthiazolylthiourea (PETT) derivatives have been identified as a new series of nonnucleoside inhibitors of HIV-1 RT. Structure-activity relationship studies of this class of compounds resulted in the identification of N-[2-(2-pyridyl)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea hydrochloride (trovirdine; LY300046.HCl) as a highly potent anti-HIV-1 agent. Trovirdine is currently in phase one clinical trials for potential use in the treatment of AIDS. Extension of these structure-activity relationship studies to identify additional compounds in this series with improved properties is ongoing. A part of this work is described here. Replacement of the two aromatic moleties of the PETT compounds by various substituted or unsubstituted heteroaromatic rings was investigated. In addition, the effects of multiple substitution in the phenyl ring were also studied. The antiviral activities were determined on wild-type and constructed mutants of HIV-1 RT and on wild-type HIV-1 and mutant viruses derived thereof, Ile100 and Cys181, in cell culture assays. Some selected compounds were determined on double- mutant viruses, HIV-1 (Ile100/Asn103) and HIV-1 (Ile100/Cys181). A number of highly potent analogs were synthesized. These compounds displayed IC50's against wild-type RT between 0.6 and 5 nM. In cell culture, these agents inhibited wild-type HIV-1 with ED50's between I and 5 nM in MT-4 cells. In addition, these derivatives inhibited mutant HIV-1 RT (Ile 100) with IC50's between 20 and 50 nM and mutant HIV-1 RT (Cys 181) with IC50's between 4 and 10 nM, and in cell culture they inhibited mutant HIV-1 (Ile100) with ED50's between 9 and 100 nM and mutant HIV-1 (Cys181) with ED50's between 3 and 20 nM.
- Cantrell, Amanda S.,Engelhardt, Per,H?gberg, Marita,Jaskunas, S. Richard,Johansson, Nils Gunnar,Jordan, Christopher L.,Kangasmets?, Jussi,Kinnick, Michael D.,Lind, Peter,Morin Jr., John M.,Muesing,Noreén, Rolf,?berg, Bo,Pranc, Paul,Sahlberg, Christer,Ternansky, Robert J.,Vasileff, Robert T.,Vrang, Lotta,West, Sarah J.,Zhang, Hong
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p. 4261 - 4274
(2007/10/03)
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