- GPR35 MODULATORS
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Described herein are GPR35 modulators and methods of using these compounds in the treatment of diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.
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Paragraph 00337
(2020/08/13)
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- Catalytic asymmetric synthesis of (-)-E-δ-viniferin via an intramolecular C-H insertion of diaryldiazomethane using Rh2(S-TFPTTL)4
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An asymmetric synthesis of (-)-E-δ-viniferin, a trans-resveratrol dimer natural product containing a dihydrobenzofuran ring, has been achieved by exploiting a Rh(II)-catalyzed intramolecular C-H insertion reaction of a diaryldiazomethane derivative as a k
- Natori, Yoshihiro,Ito, Motoki,Anada, Masahiro,Nambu, Hisanori,Hashimoto, Shunichi
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supporting information
p. 4324 - 4327
(2015/06/22)
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- CCR5 receptor antagonists: Discovery and SAR study of guanylhydrazone derivatives
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High throughput screening (HTS) led to the identification of the guanylhydrazone of 2-(4-chlorobenzyloxy)-5-bromobenzaldehyde as a CCR5 receptor antagonist. Initial modifications of the guanylhydrazone series indicated that substitution of the benzyl group at the para-position was well tolerated. Substitution at the 5-position of the central phenyl ring was critical for potency. Replacement of the guanylhydrazone group led to the discovery of a novel series of CCR5 antagonists.
- Wei, Robert G.,Arnaiz, Damian O.,Chou, Yuo-Ling,Davey, Dave,Dunning, Laura,Lee, Wheeseong,Lu, Shou-Fu,Onuffer, James,Ye, Bin,Phillips, Gary
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p. 231 - 234
(2007/10/03)
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- Structure-activity relationships of 1,5-biaryl pyrroles as EP1 receptor antagonists
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The preliminary SAR of a series of novel 1,5-biaryl pyrrole EP1 receptor antagonists derived from compound 1 is described. Replacement of the benzyl group of 1 with isosteric groups was investigated. The most effective replacement was found to be the isobutyl group. The cyclopentylmethyl and cyclohexylmethyl groups were also effective benzyl replacements. The cyclohexylmethyl derivative 19 demonstrated the lowest metabolic clearance within this series. In addition, several high affinity substituted benzyl analogues were also identified. Compound 39 was found to have good bioavailability in rats and demonstrated efficacy in the established FCA preclinical model of inflammatory pain with a calculated ED50 of 9.2 mg/kg.
- Hall, Adrian,Atkinson, Stephen,Brown, Susan H.,Chessell, Iain P.,Chowdhury, Anita,Clayton, Nicholas M.,Coleman, Tanya,Giblin, Gerard M.P.,Gleave, Robert J.,Hammond, Beverley,Healy, Mark P.,Johnson, Matthew R.,Michel, Anton D.,Naylor, Alan,Novelli, Riccardo,Spalding, David J.,Tang, Sac P.
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p. 3657 - 3662
(2007/10/03)
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- PYRROLE COMPOUNDS FOR THE TREATMENT OF PROSTAGLANDIN MEDIATED DISEASES
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Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein A, R1, R2a, R2b, Rx, R8, and R9 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine, in particular their use in the treatment of prostaglandin mediated diseases such as pain, inflammatory, immunological, bone, neurodegenerative or renal disorder.
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- Benzenamine derivatives as anti-coagulants
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This invention is directed to benzenamine derivatives of formula (I): wherein A, W, m, n, R1, R2, R3, R4, R5and R6are defined herein. These compounds are useful as anti-coagulants.
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Page column 21-22
(2010/02/05)
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