- BCL-2 INHIBITOR
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Disclosed herein is a compound of Formula (I) for inhibiting both Bcl-2 wild type and mutated Bcl-2, in particular, Bcl-2 G101V and D103Y, and a method of using the compound disclosed herein for treating dysregulated apoptotic diseases.
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Paragraph 0506-0508
(2021/10/22)
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- N-substituted acrylamide derivatives as DHODH inhibitors and preparation and use of N-substituted acrylamide derivatives
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The invention relates to N-substituted acrylamide derivatives as DHODH inhibitors and preparation and use of the N-substituted acrylamide derivatives. In particular, the invention discloses a compoundshown in a general formula I and the preparation and use of the compound. The compound has excellent DHODH inhibitory activation, so the compound can be used for treating or preventing various diseases caused by DHODH, the various diseases include but not limited to cancer, rheumatoid arthritis, lupus erythematosus, organ transplant rejection and other autoimmune diseases, and colitis, rhinitis and other inflammatory diseases.
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Paragraph 0233-0234; 0236
(2019/11/04)
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- BI-CYCLO ALDEHYDE AS PERFUMING INGREDIENT
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The present invention relates to the field of perfumery and concerns some bi-cyclo derivative of formula (I), wherein R1 represents a hydrogen atom or a C1-2 alkyl group; R2 represents a hydrogen atom or a methyl group; and A represents a group of formula C3-5 alkanediyl group; at least one of said R1 or R2 represents a group containing at least one carbon atom; and said compound being in the form of a E or Z isomer or of a mixture thereof. Said compounds are valuable perfuming ingredients capable of imparting lily of the valley and citrus notes.
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Page/Page column 11-12
(2015/01/16)
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- Exploring naphthyl-carbohydrazides as inhibitors of influenza A viruses
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A library of hydrazide derivatives was synthesized to target non-structural protein 1 of influenza A virus (NS1) as a means to develop anti-influenza drug leads. The lead compound 3-hydroxy-N-[(Z)-1-(5,6,7,8-tetrahydronaphthalen-2-yl) ethylideneamino]naphthalene-2-carboxamide, which we denoted as "HENC", was identified by its ability to increase the melting temperature of the effector domain (ED) of the NS1 protein, as assayed using differential scanning fluorimetry. A library of HENC analogs was tested for inhibitory effect against influenza A virus replication in MDCK cells. A systematic diversification of HENC revealed the identity of the R group attached to the imine carbon atom significantly influenced the antiviral activity. A phenyl or cyclohexyl at this position yielded the most potent antiviral activity. The phenyl containing compound had antiviral activity similar to that of the active form of oseltamivir (Tamiflu), and had no detectable effect on cell viability.
- Barman, Sanmitra,You, Lei,Chen, Ran,Codrea, Vlad,Kago, Grace,Edupuganti, Ramakrishna,Robertus, Jon,Krug, Robert M.,Anslyn, Eric V.
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- Synthesis of aromatic aldehydes by organocatalytic [4+2] and [3+3] cycloaddition of α,β-unsaturated aldehydes
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Organocatalytic inter- and intramolecular [4+2] and [3+3] cycloadditions of α,β-unsaturated aldehydes to give polysubstituted aromatic aldehydes are described. High periselectivity for the cycloadditions, with catalyst effects exerted by l-proline and pyrrolidine-HOAc, as well as cocatalyst, additive effects, has been observed.
- Hong, Bor-Cherng,Tseng, Hsing-Chang,Chen, Shang-Hung
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p. 2840 - 2850
(2007/10/03)
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- AMIDES AND METHOD FOR PLANT DISEASE CONTROL WITH THE SAME
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N-(α-cyanobenzyl)amide compounds represented by the formula (1): wherein R1 represents a hydrogen atom; a halogen atom; a C1-C6 alkyl group optionally substituted with a halogen atom or the like; or the like, R2 represents a hydrogen atom, a halogen atom, a C1-C6 alkyl group or the like, R3 represents a hydrogen atom or the like, R4 represents a C1-C4 alkyl group, a C3-C4 alkenyl group or the like, R5 represents a C1-C4 alkyl group, a C3-C4 alkenyl group, or the like, R6 represents a hydrogen atom or the like, R7 represents a hydrogen atom or the like, R8 represents a hydrogen atom or the like, R9 represents a hydrogen atom or the like, R10 represents a hydrogen atom or the like, R11 represents a hydrogen atom or the like, and R12 represents a hydrogen atom or the like, have excellent control activities against plant diseases.
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Page/Page column 79
(2010/11/08)
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- AMIDE COMPOUND AND USE OF THE SAME
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PROBLEM TO BE SOLVED: To provide a compound having an excellent controlling effect against plant pests. SOLUTION: This amide compound expressed by formula (1) [wherein, R1 is H, a halogen atom, a 1-4C alkyl or the like; R2 is a 1-4C alkyl, a 1-4C haloalkyl or the like; R3 is H or a 1-3C alkyl; R4 is a halogen, a 1-4C alkylthio, a 2-5C alkylcarbonyloxy or the like; R5 is a 3-4C alkynyl; and X is O or S] has the excellent controlling effect against the plant pests. COPYRIGHT: (C)2006,JPOandNCIPI
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Page/Page column 55
(2010/02/14)
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- Fungicidal Composition
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A fungicidal composition comprising: an amide compound represented by formula (1) and dimethomorph as active ingredients, and a method for controlling plant diseases applying effective amount of an amide compound represented by formula (1) and dimethomorph to plant(s) or soil where plant(s) are growing.
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Page/Page column 18
(2010/02/15)
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- AMIDE COMPOUND AND METHOD OF CONTROLLING PLANT DISEASE WITH THE SAME
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A amid compound of the formula (1): wherein, in the formula, R51 represents a halogen atom, a C1-C6 alkyl group and the like; R52 represents a hydrogen atom, a halogen atom, a C1-C6 alkyl group and the like; R53 represents a halogen atom and the like; R56 represents a halogen atom and the like; R57 represents a hydrogen atom and the like; R58 and R59 independently represent a hydrogen atom, a C1-C3 alkyl group and the like; R60 represents a C1-C4 alkyl group, a C1-C4 haloalkyl group, a C3-C4 alkenyl group, or a C3-C6 alkynyl group; R61 represents a C1-C4 alkyl group, a C1-C4 haloalkyl group, a C3-C4 alkenyl group or a C3-C6 alkynyl group or a C2-C4 cyanoalkyl group; R62, R63 and R64 represent a hydrogen atom, a halogen atom and the like; X represents a oxygen atom or a sulfur atom; has an excellent activity against plant diseases.
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Page/Page column 103
(2010/02/14)
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- Synthesis and Pharmacological Examination of Benzofuran, Indan, and Tetralin Analogues of 3,4-(Methylenedioxy)amphetamine
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Benzofuran, indan and tetrahydronaphthalene analogs of 3,4-(methylenedioxy)amphetamine (MDA) were prepared in order to examine the role of the dioxole ring oxygen atoms of MDA in interacting with the serotonin and catecholamine uptake carriers.The series of compounds was evaluated for discriminative stimulus effects in rats trained to discriminate saline from the training drugs (S)-(+)-MBDB (1c), MMAI (3), and (S)-(+)-amphetamine and for the ability to inhibit the uptake of 3H>serotonin, 3H>dopamine, and 3H>norepinephrine into crude synaptosome preparations.Behaviorally, the benzofuran and indan analogs 4-6 produced similar discriminative cues, whereas the tetralin derivative 7 did not fully substitute for the training drugs.The results in the in vitro pharmacology studies indicate that selectivity for 5-HT versus catecholamine uptake carriers may be modulated by the position and orientation of ring oxygen atoms.However, the nonoxygenated isostere 6 possessed high potency at all uptake sites examined.Enlargement of the saturated ring by one methylene unit to give the tetralin derivative resulted in a large (3-4-fold) reduction in activity at catecholamine sites.
- Monte, Aaron P.,Marona-Lewicka, Danuta,Cozzi, Nicholas V.,Nichols, David E.
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p. 3700 - 3706
(2007/10/02)
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- Formylation of Aromatic Compounds with CO in HSO3F-SbF5 under Atmospheric Pressure
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The formylation of aromatic compounds such as benzene, toluene, xylenes, mesitylene, indan, tetralin, fluorobenzene, chlorobenzene, and bromobenzene was carried out in HSO3F-SbF5 under atmospheric CO pressure at 0 deg C.In HSO3F-SbF5, both formylation and sulfonation took place to give formyl and sulfonyl compounds.In the case of alkylbenzenes, including toluene, xylenes, mesitylene, and tetralin, formylalkylbenzenesulfonyl fluorides, new compounds, were obtained by a one-pot reaction as well as alkylbenzaldehydes, alkylbenzenesulfonyl fluorides, and bis(alkylphenyl) sulfones.The direct introduction of a formyl and sulfonyl group was achieved in alkylbenzenes.The reaction path of the new compounds is a two-step reaction comprised of formylation as the first step and sulfonation as the second step.The product composition was strongly dependent on the acid strength of the HSO3F-SbF5 systems.The formyl compounds became predominant with increasing acidity of the HSO3F-SbF5 system.On the other hand, only sulfonyl compounds were produced when the acidity of the HSO3F-SbF5 system was low.
- Tanaka, Mutsuo,Iyoda, Jun,Souma, Yoshie
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p. 2677 - 2680
(2007/10/02)
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- Highly Selective Adenosine A2 Receptor Agonists in a Series of N-Alkylated 2-Aminoadenosines
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A wide variety of 2-substituted aminoadenosines were prepared for comparison with the moderately A2 receptor selective adenosine agonist 2-anilinoadenosine (CV-1808).High selectivity combined with significant affinity at the A2 receptor in rat membranes was observed for those amines bearing a two-carbon chain to which was attached an aryl, heteroaryl, or alicyclic moiety. 2-(2-Phenethylamino)adenosine (3d), a 14-fold A2 selective compound, was modified by introduction of a variety of substituents in the benzene ring and the side chain.Some of these changes led to improved A2 affinity and increased selectivity.Replacement of the phenyl moiety by cyclohexenyl produced a 210-fold selective agonist 3ag (CGS 22989) whereas the cyclohexanyl analogue 3af (CGS 22492) was 530-fold selective at the A2 site.These compounds showed hypotensive activity in rat models over a range of doses without the bradycardia observed with less selective agonists.
- Francis, John E.,Webb, Randy L.,Ghai, Geetha R.,Hutchison, Alan J.,Moskal, Michael A.,et al.
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p. 2570 - 2579
(2007/10/02)
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- Aromatic Spiranes, XVI: Syntheses of Mono- and Dianellated 2,2'-Spirobiindane-1,1'diones
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The spiroketones 19, 21, 24, 27, and 31 were prepared by cyclisation of the dicarboxylic acids and their acid chlorides, resp., (18, 20, 22, 23, 25, 26, 28, and 30) with polyphosphoric acid (PPA) or SnCl4.The latter compounds were synthesized by alkylation of the appropriate β-keto esters 10, 11, 12, and 13 with the "benzyl chlorides" 14, 15, 16, and subsequent retro-Claisen reaction.The spiro compounds 21a and 39 were obtained by PPA-cyclisation of the keto acids 35 and 38, which in turn were prepared by aldol-reaction of the ketones s-hydrindacen-1-on and 9a with phthalaldehydic acid to the olefinic keto acids 33 and 36 followed by catalytic hydrogenation. - Keywords: Indane-1-one; s-Hydrindacene-1-one; Tetrahydrobenzoindane-1-one; β-Keto esters; Phthalaldehydic acid; Spiro cyclisation; 2,2'-Spirobiindane-1,1'-diones; 1H-nmr spectra; Mass spectra
- Neudeck, Horst K.
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p. 597 - 622
(2007/10/02)
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- Benzannulation of Cyclopentanone, Cyclohexanone and Cycloheptanone: A Short Synthesis of Indane-5-carboxaldehyde, a Monoterpenoid Constituent of Ammomum medium
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The Vilsmeier reaction on the homoallyl alcohols (1a-c), derived from cyclopentanone, cyclohexanone and cycloheptanone respectively, leads to a mixture of monocarboxaldehydes (2a-c) and dicarboxaldehydes (3a-c) which have been readily separated and characterized.The Vilsmeier route incidentally provides a short synthesis of indane-5-carboxaldehyde (2a), a terpenoid constituent of a medicinal plant.
- Rao, M. Suresh Chander,Rao, G. S. Krishna
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p. 660 - 661
(2007/10/02)
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