- AROMATIC RING DERIVATIVE AS IMMUNOREGULATION AND PREPARATION METHOD AND APPLICATION OF AROMATIC RING DERIVATIVE
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Relating to a compound represented by formula (I) and a pharmaceutically acceptable salt of the compound, and an application of the compound as an S1P1 agonist.
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Paragraph 0335-0336
(2021/10/15)
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- Intermediate of siponimod and synthesis method thereof
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The invention relates to a novel intermediate compound (a compound as shown in a formula 2A) of siponimod, a synthesis method of the novel intermediate compound, and a method for synthesizing siponimod by adopting the compound as shown in the formula 2A. Specifically, 3-trifluoromethyl-4-halogenated benzoic acid or 3-trifluoromethyl-4-halogenated toluene is taken as an initial raw material and is subjected to reduction, bromination, coupling, substitution and reduction to obtain a compound as shown in a formula 2A, and R is Boc or Ac.
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Paragraph 0071-0075
(2021/05/05)
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- SELECTIVE FLUORESCENT PROBE FOR ALDEHYDE DEHYDROGENASE
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High aldehyde dehydrogenase 1A1 (ALDH1A1) activity has emerged as a reliable marker for the identification of both normal and cancer stem cells. Herein, is presented AlDeSense, a turn-on green fluorescent probe for aldehyde dehydrogenase 1A1 (ALDH1A1) and Ctrl-AlDeSense, a matching non-responsive reagent. AlDeSense exhibits a 20-fold fluorescent enhancement when treated with ALDH1A1. Through the application of surface marker antibody staining, tumorsphere assays, and assessment of tumorigenicity, the disclosed results show that cells exhibiting high AlDeSense signal intensity have properties of cancer stem cells. Herein, is also reported the development of a red congener, red-AlDeSense. Importantly, red-AlDeSense represents one of only a few examples of a turn-on sensor in the red region using the d-PeT quenching mechanism.
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Paragraph 0260
(2020/07/14)
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- COMPOUNDS USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS
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The present invention relates to certain compounds of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor: Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, a disease or disorder mediated by lymphocytes, an autoimmune disease or disorder, an inflammatory disease or disorder, an inflammatory skin disease or disorder, cancer, psoriasis, atopic dermatitis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, and acne, microbial infections or diseases and viral infections or diseases.
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Page/Page column 46; 52; 53
(2020/03/29)
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- Molecules having pesticidal utility, and intermediates, compositions, and processes, related thereto
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This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Arthropoda, Mollusca, and Nematoda, processes to produce such molecules, intermediates used in such processes, pesticidal compositions containing such molecules, and processes of using such pesticidal compositions against such pests. These pesticidal compositions may be used, for example, as acaricides, insecticides, miticides, molluscicides, and nematicides. This document discloses molecules having the following formula (“Formula One”).
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Paragraph 0386-0387
(2018/10/21)
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- Identification and development of biphenyl substituted iminosugars as improved dual glucosylceramide synthase/neutral glucosylceramidase inhibitors
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This work details the evaluation of a number of N-alkylated deoxynojirimycin derivatives on their merits as dual glucosylceramide synthase/neutral glucosylceramidase inhibitors. Building on our previous work, we synthesized a series of d-gluco and l-ido-configured iminosugars N-modified with a variety of hydrophobic functional groups. We found that iminosugars featuring N-pentyloxymethylaryl substituents are considerably more potent inhibitors of glucosylceramide synthase than their aliphatic counterparts. In a next optimization round, we explored a series of biphenyl-substituted iminosugars of both configurations (d-gluco and l-ido) with the aim to introduce structural features known to confer metabolic stability to drug-like molecules. From these series, two sets of molecules emerge as lead series for further profiling. Biphenyl-substituted l-ido-configured deoxynojirimycin derivatives are selective for glucosylceramidase and the nonlysosomal glucosylceramidase, and we consider these as leads for the treatment of neuropathological lysosomal storage disorders. Their d-gluco-counterparts are also potent inhibitors of intestinal glycosidases, and because of this characteristic, we regard these as the prime candidates for type 2 diabetes therapeutics.
- Ghisaidoobe, Amar T.,Van Den Berg, Richard J. B. H. N.,Butt, Saleem S.,Strijland, Anneke,Donker-Koopman, Wilma E.,Scheij, Saskia,Van Den Nieuwendijk, Adrianus M. C. H.,Koomen, Gerrit-Jan,Van Loevezijn, Arnold,Leemhuis, Mark,Wennekes, Tom,Van Der Stelt, Mario,Van Der Marel, Gijsbert A.,Van Boeckel, Constant A. A.,Aerts, Johannes M. F. G.,Overkleeft, Herman S.
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p. 9096 - 9104
(2015/03/14)
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- N- (HETERO)ARYL, 2- (HETERO)ARYL-SUBSTITUTED ACETAMIDES FOR USE AS WNT SIGNALING MODULATORS
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The present invention relates to compounds of formulae 1 and 2 and methods for modulating the Wnt signaling pathway using these compounds, wherein A1, A2, B, Y and Z all represent rings.
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Page/Page column 47-48
(2010/09/18)
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- SUBSTITUTED IMIDAZOLONE DERIVATIVES, PREPARATIONS AND USES
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The present invention relates to polysubstituted imidazolone derivatives, to the pharmaceutical compositions comprising them and to the therapeutic uses thereof in the human and animal health fields. The present invention also relates to a process for preparing these derivatives.
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Page/Page column 64-65
(2010/02/16)
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- HETEROARYLAMIDE LOWER CARBOXYLIC ACID DERIVATIVE
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To provide a novel compound which has S1P receptor agonistic activity, exhibits excellent immunosuppressing effect, gives less adverse side effects, and can be orally administered. The invention provides a compound represented by general formula (I) (wherein A is a single bond, -O-, or - CH2-; R1 represents a hydrogen atom or a C1-C6 alkyl group, and V represents any one group selected from among the following groups (1) to (3) : (1) -G1-, (2) -G2-N(R2) -G3-, and (3) a group represented by formula 2, wherein each of Z1 and Z2 represents a hydrogen atom or a C1-C6 alkyl group, Z3 represents a hydrogen or the like, Q represents -CH2-O- or the like, and Y represents a group represented by foumula 3, a salt thereof, or a solvate thereof.
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Page/Page column 249-250
(2009/02/10)
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