- MALT1 MODULATORS AND USES THEREOF
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Provided herein are compounds, compositions, and methods useful for modulating MALT1 and for treating related diseases, disorders, and conditions.
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Paragraph 00120; 00157
(2021/07/10)
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- Nickel-catalyzed methylation of aryl halides/tosylates with methyl tosylate
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This work describes the cross-electrophile methylation of aryl bromides and aryl tosylates with methyl tosylate. The mild reaction conditions allow effective methylation of a wide set of heteroaryl electrophiles and dimethylation of dibromoarenes.
- Wang, Jiawang,Zhao, Jianhong,Gong, Hegui
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supporting information
p. 10180 - 10183
(2017/09/23)
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- 7-(MORPHOLINYL)-2-(N-PIPERAZINYL) METHYL THIENO [2, 3-C] PYRIDINE DERIVATIVES AS ANTICANCER DRUGS
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The present invention relates to novel series of substituted 7-(morpholinyl)-2-(N-piperazinyl)-methyl thieno [2, 3-c] pyridines of the following structure of formula I. Where in R1, R2, R3 and R4 are defined.
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Page/Page column 36; 37
(2016/06/28)
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- INHIBITORS OF BRUTON'S TYROSINE KINASE
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This application discloses compounds according to generic Formula I: wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with exc
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Page/Page column 114; 115
(2014/05/24)
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- INHIBITORS OF BRUTON'S TYROSINE KINASE
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This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
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Page/Page column 79-80
(2014/06/11)
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- PYRIDAZINONES, METHOD OF MAKING, AND METHOD OF USE THEREOF
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Pyridazinone compounds of Formula (I) including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula (I) for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
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Page/Page column 52
(2012/03/26)
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- PYRIDINONES/PYRAZINONES, METHOD OF MAKING, AND METHOD OF USE THEREOF
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Pyridone and pyrazinone compounds of Formula (I) including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
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Page/Page column 61
(2012/03/26)
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- OXAZOLE AND ISOXAZOLE CRAC MODULATORS
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The present invention relates to compounds of Formula (I) along with processes for their preparation that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of CRAC. The invention further relates to methods of treating, preventing managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of CRAC of Formula (I).
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Page/Page column 75-76
(2012/05/19)
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- Synthesis of N-(Methoxycarbonylthienylmethyl)thioureas and evaluation of their interaction with inducible and neuronal nitric oxide synthase
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Two isomeric N-(memoxycarbonylmienylmemyl)mioureas were synthesised by a sequence of radical bromination of methylthiophenecarboxylic esters, substitution with trifluoroacetamide anion, deprotection, formation of the corresponding isothiocyanates and addition of ammonia. The interaction of these new thiophene-based thioureas with inducible and neuronal nitric oxide synthase was evaluauted. These novel thienylmethyl- thioureas stimulated the activity of inducible Nitric Oxide Synthase (iNOS).
- Suaifan, Ghadeer A.R.Y.,Goodyer, Claire L.M.,Threadgill, Michael D.
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experimental part
p. 3121 - 3134
(2010/09/04)
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- Gold-catalyzed oxidative cleavage of aryl-substituted alkynyl ethers using molecular oxygen. Simultaneous degradation of C-H and single and triple carbon-carbon bonds under ambient conditions
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We report the gold-catalyzed oxidative cleavage of aryl-substituted alkynyl ethers using molecular oxygen under ambient conditions; the transformation involves a remarkable cleavage of C-H, C-C and CC bonds simultaneously.
- Das, Arindam,Chaudhuri, Rupsha,Liu, Rai-Shung
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scheme or table
p. 4046 - 4048
(2009/12/08)
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- Iron-catalyzed one-pot oxidative esterification of aldehydes
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A highly efficient, mild, and simple protocol for Fe(ClO4) 3·xH2O-catalyzed oxidative esterification of aldehydes was developed. Several aromatic and aliphatic aldehydes reacted with simple primary and secondary alcohols, used as the solvent, smoothly in the presence of an iron salt catalyst (10 mol-%) and hydroperoxide (4 equiv.) as an oxidant to generate the corresponding esters in good to excellent yields. Wiley-VCH Verlag GmbH & Co. KGaA, 2009.
- Wu, Xiao-Feng,Darcel, Christophe
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supporting information; experimental part
p. 1144 - 1147
(2009/07/11)
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- Synthesis of 2-thiophenecarboxylic and 2,5-thiophenedicarboxylic acid esters via the reaction of thiophenes with the CCl4-ROH reagent in the presence of vanadium, iron, and molybdenum catalysts
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2-Thiophenecarboxylic and 2,5-thiohenedicarboxylic acid esters were synthesized via the reaction of thiophene with the CCl4-ROH-catalyst system, with a total yield of 44-85%. A possible reaction scheme includes the successive steps of alkylation of thiophene with carbon tetrachloride, leading to 2-trichloromethylthiophene, and alcoholysis of the product giving the corresponding 2-thiophenecarboxylate. The best catalysts for this reaction are VO(acac)2, Fe(acac)3, and Mo(CO)6.
- Khusnutdinov,Shchadneva,Baiguzina,Mukminov,Mayakova,Smirnov,Dzhemilev
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experimental part
p. 471 - 478
(2010/03/31)
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- INTEGRASE INHIBITORS 3
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The present invention provides a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. Compounds of formula (I) are also provided.
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Page/Page column 58
(2008/06/13)
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- Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: Role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonis
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Some N3-substituted analogues of willardiine such as 11 and 13 are selective kainate receptor antagonists. In an attempt to improve the potency and selectivity for kainate receptors, a range of analogues of 11 and 13 were synthesized with 5-sub
- Dolman, Nigel P.,More, Julia C. A.,Alt, Andrew,Knauss, Jody L.,Pentik?inen, Olli T.,Glasser, Carla R.,Bleakman, David,Mayer, Mark L.,Collingridge, Graham L.,Jane, David E.
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p. 1558 - 1570
(2007/10/03)
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- Novel thienopyridine compounds, and methods of use thereof
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The present invention relates to novel compounds capable of modulating the stability and/or activity of hypoxia inducible factor (HIF).
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Page/Page column 35
(2008/06/13)
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- TRICYCLIC DERIVATIVES OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, THEIR PREPARATIONS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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The present invention relates to tricyclic derivatives or pharmaceutically acceptable salts thereof, their preparations and pharmaceutical compositions containing them. More precisely, the present invention relates to tricyclic derivatives as colchicine derivatives, pharmaceutically acceptable salts thereof, their preparations and pharmaceutical compositions containing them. Tricyclic derivatives of the present invention show very powerful cytotoxicity to cancer cell lines but were much less toxic than colchicine or taxol, confirmed through animal toxicity test. Tricyclic derivatives of the invention also decrease the volume and weight of a tumor and have a strong angiogenesis inhibiting activity in HUVEC cells. Thus, tricyclic derivatives of the present invention can effectively be used as an anticancer agent, anti-proliferation agent and an angiogenesis inhibitor.
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- 3-(substituted phenyl)-5-thienyl-1,2,4-triazole compounds with activity against whitefly
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3-(Substituted phenyl)-5-(thienyl)-1,2,4-triazole compounds are useful as insecticides and acaricides.
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- Synthesis and antitumour activity of new derivatives of flavone-8- acetic acid (FAA). Part 31): 2-Heteroaryl derivatives
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A range of 14 derivatives of flavone-8-acetic acid (FAA) with a heterocyclic substituent in place of the 2-phenyl group have been prepared and their anti-tumour activity evaluated in vitro against a panel of human and murine tumour cell lines and in vivo against MAC 15A. Some of the compounds, notably 2c,d and s, showed significant in vivo activity and these require further studies in order to evaluate their potential for development.
- Aitken, R. Alan,Bibby, Michael C.,Bielefeldt, Florian,Double, John A.,Laws, Andrea L.,Mathieu, Anne-Laure,Ritchie, Robert B.,Wilson, David W. J.
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p. 405 - 411
(2007/10/03)
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- Reaction of thioglycolate with α-fluoro-β-(phenylthio)enones (or -enals): Synthesis of substituted α-carboxy-γ-fluorothiophenes
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A new synthetic method to substituted α-carboxy-γ-fluorothiophenes 2F is reported. They were prepared by the reaction between two equivalents of methyl thioglycolate anion and α-fluoro-β-(phenylthio)enones (or -enals) 1F, in DMSO (70°C) in yields ranging from 41% to 85%. We show from the reaction of (Z)-α-fluoro-β-(phenylthio)but-enone 1aF, that cyclisation to fluorothiophene 2aF occurs via the formation of stable enolates of α-fluoro-β-(dithianyl)butanone.
- Andres, Didier F.,Laurent, Eliane G.,Marquet, Bernard S.
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p. 1049 - 1052
(2007/10/03)
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- Aminomethylthiophene-2-carboxylic acids as dipeptide mimetic in new growth hormone secretagogues
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3-Aminomethylbenzoic acid is a well established dipeptide mimetic. Herein, aminomethylthiophene-2-carboxylic acids have been synthesized as analogues of 3-aminomethylbenzoic acid. Their use as a dipeptide-mimetic at the N-terminal of novel growth hormone secretagogues is described.
- Peschke, Bernd,Madsen, Kjeld,Hansen, Birgit Sehested,Johansen, Nils Langeland
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p. 1969 - 1972
(2007/10/03)
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- N-3-Substituted Pyrimidones as Potent, Orally Active, AT1 Selective Angiotensin II Receptor Antagonists
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A novel series of nonpeptide angiotensin II (A II) antagonists containing a pyrimidinone ring which carries a C-linked biphenyltetrazole moiety and a carboxyheteroaryl group on the 3-position have been prepared.Their affinity for the AT1 receptor was determined in a binding assay on rat adrenal cortical membranes.The in vivo antihypertensive properties were tested by evaluating the inhibition of the pressor response to A II followed by iv and id administration.Extensive molecular modeling studies, including comparison of molecular electrostatic potential distributions, conformational analysis, and overlays on a computational pharmacophore model of A II, were used to evaluate structural parameters of the new compounds, in comparison to other known A II antagonists (e.g., DUP-753 and SKandF 108566).According to the modeling studies, the introduction of a (carboxyheteroaryl)methyl moiety at the 3-position of the pyrimidinone ring led to derivatives with increased potency.Methyl 2-methyl>-1-(6H)-pyrimidinyl>methyl>-3-thiophenecarboxylate (3k, LR-B/081), one of the most potent compounds in the series (Ki = 1.4 nM), exhibited a marked antihypertensive activity on oral administration to conscious renal hypertensive rats, with long duration of action.It was selected for clinical evaluation in the treatment of hypertension in man.
- Salimbeni, Aldo,Canevotti, Renato,Paleari, Fabio,Poma, Davide,Caliari, Saturnino,et al.
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p. 4806 - 4820
(2007/10/03)
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- A CONVENIENT SYNTHESIS OF SUBSTITUTED HETEROAROMATIC COMPOUNDS VIA THE PALLADIUM-CATALYZED CROSS-COUPLING REACTION OF ORGANOSILICON COMPOUNDS
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The silicon-based cross-coupling reaction promoted by fluoride ion and a Pd catalyst provides us with a new entry to substituted heteroaromatic compounds.
- Hatanaka, Yasuo,Fukushima, Satoshi,Hiyama, Tamejiro
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p. 303 - 306
(2007/10/02)
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- A New Synthesis of Benzothiophenes and Benzothiophenes by Annulation of Disubstituted Thiophenes
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Nine newly prepared ortho-disubtituted thiophenes (1-5) react with Michael acceptors to form benzo- and benzothiophenes.This novel annulation process is specifically suited to form benzothiophenes with substituents in the benzene moiety.Substitution
- Terpstra, Jan W.,Leusen, Albert M. van
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p. 230 - 238
(2007/10/02)
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- SYNTHESIS OF QUINOLINE AND BENZOTHIOPHENE DERIVATIVES BY RING ANNELATION OF PYRIDINES AND THIOPHENES
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Selected ortho-disubstituted pyridines and thiophenes react with Michael acceptors to give functionalized quinolines or benzothiophenes, respectively.
- Leusen, Albert M. van,Terpstra, Jan Willem
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p. 5097 - 5100
(2007/10/02)
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