- Columnar Propeller-Like 1,3,5-Triphenylbenzenes: Probing the Effect of Chlorine on the Suzuki Cross-Coupling and Liquid Crystalline Properties
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Suzuki cross-couplings either between chlorinated N-methyliminodiacetic acid (MIDA)-protected aryl boronates and 1,3,5-tribromobenzene or between chlorinated aryl bromides and phenyltrisboronic species to star-shaped 1,3,5-triphenylbenzenes with different substitution patterns and chloro substituents at the outer phenyl rings were studied. The chlorinated precursors required for the respective reaction were synthesized and characterized. Depending on the used coupling reaction target triphenylbenzenes were isolated in yields between 42 % and 88 %. Their mesomorphic properties were influenced by the substitution pattern and number of peripheral chlorine atoms. Triphenylbenzene with 3,5-alkoxy substitution and H in para-position self-assembled into either columnar hexagonal (Colh) mesophases or a soft crystal. While threefold chloro substitution in meta-position of the outer phenyl rings led to stable room temperature Colho phases, triphenylbenzenes with threefold para-chloro or 3,5-dichloro substitution were non-mesomorphic. Based on X-ray diffraction data a helical packing model for the observed phases similar to that of related alkoxy-substituted triphenylbenzenes was proposed.
- Grunwald, Marco André,W?hrle, Tobias,Forschner, Robert,Baro, Angelika,Laschat, Sabine
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supporting information
p. 2190 - 2198
(2020/03/03)
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- CYCLOPROPYLDERIVATIVES AND THEIR USE AS KINASE INHIBITORS
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The invention generally relates to cyclic compounds and, more particularly, to a compound represented by Structural Formula I: or a pharmaceutically acceptable salt thereof and pharmaceutical comopositions comprising the multicyclic compounds. The invention also relates to a method for treating a disease or disorder selected from cancer (e.g., lymphoma, such as mantle cell lymphoma), a neurodegenerative disease, an inflammatory diseases or an immune system disease (e.g., a T-Cell mediated autoimmune disesase) in a subject in need thereof. The method comprises administering to a subject in need thereof a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof, or a composition comprising a compound of the invention, or a pharmaceutically acceptable salt thereof.
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Paragraph 00446; 00447
(2017/03/21)
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- SUBSTITUTED BENZOFURANYL AND BENZOXAZOLYL COMPOUNDS AND USES THEREOF
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The invention generally relates to substituted benzofuranyl and substituted benzoxazolyl compounds, and more particularly to a compound represented by Structural Formula (A) : or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of Structural Formula (A), or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders.
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Paragraph 00360
(2015/01/16)
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- 3,6-DICHLOROSALICYLIC ACID COMPOUNDS AND RELATED SYNTHETIC PROCESSES
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The present disclosure relates, in general, to 5-halo-3,6-dichlorosalicylic acid compounds, 5-halo-3,6-dichlorosalicyaldehyde compounds, processes for preparing 5-halo-3,6-dichlorosalicylic acid compounds, processes for preparing 5-halo-3,6- dichlorosalicyaldehyde compounds, processes for preparing 3,6-dichlorosalicylic acid compounds, and processes that employ such compounds as intermediates in the preparation of the herbicide dicamba.
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Paragraph 0180
(2016/01/26)
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- KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF
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Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and
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Paragraph 00206
(2015/04/15)
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- A Selective Prostaglandin E2 Receptor Subtype 2 (EP2) Antagonist Increases the Macrophage-Mediated Clearance of Amyloid-Beta Plaques
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A high-throughput screen resulted in the discovery of benzoxazepine 1, an EP2 antagonist possessing low microsomal stability and potent CYP3A4 inhibition. Modular optimization of lead compound 1 resulted in the discovery of benzoxazepine 52, a molecule with single-digit nM binding affinity for the EP2 receptor and significantly improved microsomal stability. It was devoid of CYP inhibition and was 4000-fold selective against the other EP receptors. Compound 52 was shown to have good PK properties in CD-1 mice and high CNS permeability in C57Bl/6s mice and Sprague-Dawley rats. In an ex vivo assay, it demonstrated the ability to increase the macrophage-mediated clearance of amyloid-beta plaques from brain slices in a dose-dependent manner.
- Fox, Brian M.,Beck, Hilary P.,Roveto, Philip M.,Kayser, Frank,Cheng, Qingwen,Dou, Hannah,Williamson, Toni,Treanor, James,Liu, Hantao,Jin, Lixia,Xu, Guifen,Ma, Ji,Wang, Songli,Olson, Steven H.
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supporting information
p. 5256 - 5273
(2015/08/03)
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- TRICYCLIC SULFONAMIDE DERIVATIVES
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The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of pain.
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Page/Page column 1374-1376
(2015/07/15)
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- TRICYCLIC SULFONAMIDE DERIVATIVES
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The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of pain.
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Page/Page column 161
(2015/07/16)
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- CONDENSED TRICLYCLIC COMPOUNDS AS INHIBITORS OF HIV REPLICATION
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Compounds of formula (I) and pharmaceutical compositions thereof: wherein A1 A2 and A3 are each independently selected from the group consisting of N and CR3, wherein R1 is an optionally substituted heterocyclyl or an optionally substituted -(C1-6)alkyl-heterocyclyl, R2 is an optionally substituted aryl or an optionally subsisted heteroaryl, R4 is an optionally substituted aryl, an optionally substituted heterocyclyl or an optionally substituted heteroaryl, useful as an inbitor of HIV replication.
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- PAI-1 INHIBITOR
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The compound represented by the following formula (I) and the like have PAI-1 inhibition activity; wherein: R1 represents a C6-10 aryl group which may be substituted or the like; T represents a single bond or the like; m represents 0
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Page/Page column 273
(2011/02/17)
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- The first simple and efficient synthesis of the unusual dipeptide part of Phomopsin A
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A practical high yielding synthesis of the key halogenated dipeptide part of Phomopsin A 2 is reported. The key steps are a selective Heck coupling, a Sharpless asymmetric dihydroxylation in PEG and a benzoyl isocyanate mediated synthesis of dehydrovaline
- Chandrasekhar, Srivari,Chandrashekar, Gudise
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p. 2209 - 2214
(2007/10/03)
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- Design, synthesis, anti-HIV activities, and metabolic stabilities of alkenyldiarylmethane (ADAM) non-nucleoside reverse transcriptase inhibitors
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The alkenyldiarylmethane (ADAM) HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) are effective anti-HIV agents in cell culture. However, the potential clinical utility of the ADAMs is expected to be limited by the presence of methyl ester mo
- Silvestri, Maximilian A.,Nagarajan, Muthukaman,De Clercq, Erik,Pannecouque, Christophe,Cushman, Mark
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p. 3149 - 3162
(2007/10/03)
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- ανβ3 integrin antagonists in combination with chemotherapeutic agents
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The present invention is directed to compounds of the formula and pharmaceutically acceptable salts and isomers thereof administered in combination with chemotherapeutic agents.
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- Chiral-β-amino acid compounds and derivatives thereof
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The present invention is directed to a method for the preparation of a chiral β-amino ester of the formula wherein R is lower alkyl; and X and Y are the same or different Cl, Br or I.
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- Meta-azacyclic amino benzoic acid compounds and derivatives thereof
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The present invention is directed to compounds of the formula and pharmaceutically acceptable salts and isomers thereof.
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- Amino benzenepropanoic acid compounds and derivatives thereof
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The present invention is directed to compounds of the formula STR1 where R1 is BOC or H, R is H or lower alkyl; X and Y are the same or different halo atoms selected from the group consisting of Cl, Br or I and pharmaceutically acceptable salts and isomers thereof.
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