- DIPHENYL DERIVATIVES AND USES THEREOF
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The present disclosure provides a compound of formula (I): or a pharmaceutically acceptable salt thereof, and its therapeutic uses for activating a growth factor pathway, promoting wound healing, promoting tissue repair, and treating hearing loss, skeletal muscle loss, organ degeneration, tissue damage, neurodegeneration, and muscular atrophy. The disclosure further provides pharmaceutical compositions and combinations. The present disclosure also relates to the use of such compounds for research or other non-therapeutic purposes.
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Paragraph 1142
(2019/03/30)
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- Coumarin-surfactant modified polyoxometalate catalyzed cross dehydrogenative coupling of benzyl alcohol with the: Para -C-H of unprotected aniline
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This paper presents a novel method for synthesizing para-aminobenzophenone and its derivatives (p-ABPs) using a coumarin-surfactant modified polyoxometalate as the catalyst. Preliminary mechanistic studies indicate that the reaction has undergone an oxidative cross dehydrogenative coupling process. This method has the advantages of an easy process, a convenient raw material source, safe and green oxidants, and tolerances of several functional groups.
- Xu, Qian,Yu, Gang,Liu, Min,Peng, Chang,Banks, M. Katherine,Xu, Weijian,Wu, Ruoxi,Lu, Yanbing
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p. 5133 - 5136
(2018/10/24)
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- METHYLENE LINKED QUINOLINYL MODULATORS OF ROR-GAMMA-T
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The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
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Page/Page column 81; 82; 83
(2015/05/05)
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- Palladacycle-Catalyzed Carbonylative Suzuki-Miyaura Coupling with High Turnover Number and Turnover Frequency
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This work reports the carbonylative Suzuki-Miyaura coupling of aryl iodides catalyzed by palladacycles. More importantly, the palladacycles have been used to generate high turnover numbers (TON's) and turnover frequencies (TOF's). A range of aryl iodides can be coupled with arylboronic acids, generating TON's in the range of 106 to 107 and TOF's in the range of 105 to 106 h-1. Comparison of the palladacycles with a conventional palladium source shows their superiority in generating high TON's and TOF's.
- Gautam, Prashant,Bhanage, Bhalchandra M.
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p. 7810 - 7815
(2015/08/18)
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- QUINOLINE DERIVATIVES USEFUL AS CB-1 INVERSE AGONISTS
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The present invention is directed to quinoline derivatives, pharmaceutical compositions containing said derivatives and their use in the treatment of disorders and conditions mediated by the CB-1 receptor; more particularly, in the treatment of disorders
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- QUINOLINE DERIVATIVES USEFUL AS CB-1 INVERSE AGONISTS
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The present invention is directed to quinoline derivatives, pharmaceutical compositions containing said derivatives and their use in the treatment of disorders and conditions mediated by the CB-1 receptor; more particularly, in the treatment of disorders
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- METHYLENE LINKED QUINOLINYL MODULATORS OF RORyt
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The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
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Paragraph 0465; 0466; 0471; 0472
(2014/05/07)
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- ARYL-AND HETEROARYL-SUBSTITUTED BENZENE DERIVATIVES AS MODULATORS OF PI3-KINASE SIGNALLING PATHWAYS
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The present disclosure relates to certain aryl- or heteroaryl-substituted benzene derivatives, pharmaceutical compositions containing them, and methods of using them, including methods for modulating autophagy or preventing, reversing, slowing or inhibiting the PI3K-AKT-MTOR pathway, and methods of treating diseases that are associated with autophagy or the PI3K-AKT-MTOR pathway.
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- Synthesis, molecular modelling and biological evaluation of 4-amino-2(1H)-quinazolinone and 2,4(1H,3H)-quinazolidone derivatives as antitumor agents
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A series of 6-benzoyl-, 6-arylthio- and 6-arylsulfonyl-4-amino-2(1H)- quinazolinones and -2,4(1H,3H)-quinazolinediones were prepared. They were evaluated in vitro for their cytotoxicity against the NCI-60 cancer cell lines. A series of 6-benzoyl-, 6-arylthio- and 6-arylsulfonyl-4-amino-2(1H)- quinazolinones and -2,4(1H,3H)-quinazolinediones were prepared. They were evaluated in vitro for their cytotoxicity against the NCI-60 cancer cell lines. Copyright
- Richter, Stephanie,Gioffreda, Barbara
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p. 810 - 820
(2012/03/08)
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- The first heterogeneous carbonylative Stille coupling of organostannanes with aryl iodides catalyzed by MCM-41-supported bidentate phosphine palladium(0) complex
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The first heterogeneous carbonylative Stille coupling reaction of organostannanes with aryl iodides under an atmospheric pressure of carbon monoxide has been achieved in DMF at 80 °C in the presence of a catalytic amount of an MCM-41-supported bidentate phosphine palladium(0) complex [MCM-41-2P-Pd(0)], yielding a variety of unsymmetrical ketones in good to high yields. This polymeric palladium catalyst exhibited higher activity and selectivity than PdCl2(PPh3)2 and can be recovered and recycled by a simple filtration of the reaction solution and used for at least 10 consecutive trials without any decrease in activity. Our system not only avoids the use of carbon monoxide under pressure, but also solves the basic problem of palladium catalyst recovery and reuse. The Royal Society of Chemistry 2009.
- Cai, Mingzhong,Zheng, Guomin,Ding, Guodong
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experimental part
p. 1687 - 1693
(2010/06/11)
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- Studies on the Insecticidal Activities of Some New N-Benzoyl-N'-Arylureas
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This paper reports the synthesis and the insecticidal activities of some N-benzoyl-N'-arylureas 4-arylsubstituted with alkylated or halogenated aroyl moieties. The compounds, tested against some representative insect species, displayed very high activity against Aedes aegypti, especially the halosubstituted derivatives. None of the newly synthesized compounds showed genotoxic activity in the Bacillus subtilis rec-assay and in the Salmonella-microsome test.
- Carmellino, Maria L.,Pagani, Giuseppe,Pregnolato, Massimo,Terreni, Marco,Caprioli, Vincenzo,Zani, Franca
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p. 227 - 236
(2007/10/03)
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- N-phenyl-2-cyano-3-hydroxy-propenamides
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A compound selected from the group consisting of a compound of the formula STR1 wherein R1 is selected from the group consisting of alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms and alkenyl and alkynyl of 2 to 6 carbon atoms, R2 is hydrogen or alkyl of 1 to 3 carbon atoms, Y is selected from the group consisting of STR2 Z1 and Z2 are individually selected from the group consisting of hydrogen, halogen, --NO2, --CN and alkyl of 1 to 3 carbon atoms, R3 is hydrogen or alkyl of 1 to 3 carbon atoms, m is an integer from 0 to 6, R4, R5, R6, R7 and R8 are individually selected from the group consisting of hydrogen, halogen, --CN, --NO2, alkyl, alkylthio and alkoxy of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, --COR10, --(CH2)n --CX3, --O--(CH2)n CX3 and --S--(CH2)n --CX3, R10 is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and cycloalkyl of 3 to 6 carbon atoms, n is an integer from 0 to 3, X is halogen or R6 and R7 together form --O--CH2 --O-- and their non-toxic, pharmaceutically acceptable salts with a base having anti-inflammatory and immunomodulatory activity.
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- Aromatic ether-ketone polyamines, intermediates and products, and methods for preparing same
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Novel aromatic ether ketone diamine compounds and methods for their preparation are disclosed which comprise from about 3 to 8 aromatic rings interspersed with ether and ketone linkages. The novel ether ketone diamine compounds are useful as monomeric starting materials for the preparation of useful intermediates and useful thermoplastic and high temperature resistant polymers. In preferred embodiments, the novel ether ketone diamines are useful as curing agents for epoxy resin compositions and composite materials.
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- Acrylic acid heterocyclic amides, fungicidal compositions and use
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Compounds of the formula STR1 wherein A, B, R1, X and Q are substituents of various types, and acid addition salts thereof. The compounds are useful as fungicides.
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- Benzophenone ureas and method for utilizing the same
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This invention provides for novel benzophenone ureas, a method for preparing the same, and a method for controlling undesirable broadleaf weeds and grasses therewith, wherein said benzophenone is represented by the generic formula: SPC1 Where A and B each represent hydrogen, methyl, halogen, trifluoromethyl, or methoxy; R1 and R2 are taken singly or in combination and represent hydrogen, lower alkyl, alkoxy, alkoxyalkyl, cycloalkyl, cyclohetero, loweralkylamino, lower alkenyl or lower alkynyl, with the proviso that A is either meta or para to the --HN--CO--NR1 R2 substituent.
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