- NOVEL SMALL MOLECULE DRUG CONJUGATES OF GEMCITABINE DERIVATIVES
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Disclosed are compounds having formula (I) or a pharmaceutically acceptable salt, ester, amide, solvate, or stereoisomer thereof, wherein L, Y1, Y2, Y3, Y4, Y5, Z1, Z2, Z3, Z4, Z5, Z6, and Effector are each as defined in the specification; compositions thereof; uses thereof; and methods of use thereof.
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Page/Page column 52
(2019/08/26)
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- SMALL MOLECULE DRUG CONJUGATES OF GEMCITABINE MONOPHOSPHATE
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Disclosed are compounds having formula (I): or a pharmaceutically acceptable salt, ester, amide, solvate, or stereoisomer thereof, wherein L, Y1, Y2, Y3, Y4, Y5, Z1, Z2, Z3, Z4, Z5, Z6 are each as defined in the specification; compositions thereof; uses thereof; and methods of use thereof.
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Page/Page column 48
(2019/08/26)
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- LABELLED COUMARIN DERIVATIVES
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The present invention relates to compounds having selective binding for MAO-B as compared with MAO-A. The invention also provides radioactive versions of these compounds, and precursor compounds for the synthesis of these radioactive compounds. The radioactive compounds of the invention can find use for in vivo imaging applications.
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Page/Page column 13-14
(2016/07/05)
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- Synthesis and Evaluation of Novel 7- and 8-Aminophenoxazinones for the Detection of β-Alanine Aminopeptidase Activity and the Reliable Identification of Pseudomonas aeruginosa in Clinical Samples
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A series of novel 8-aminophenoxazin-3-one and 7-aminophenoxazin-3-one chromogens and their corresponding β-alanine derivatives were synthesized and evaluated for their ability to detect β-alanyl aminopeptidase activity in bacteria known to hydrolyze β-ala
- Bedernjak, Alexandre F.,Zaytsev, Andrey V.,Babolat, Michèle,Cellier, Marie,James, Arthur L.,Orenga, Sylvain,Perry, John D.,Groundwater, Paul W.,Anderson, Rosaleen J.
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supporting information
p. 4476 - 4487
(2016/06/13)
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- A Novel Covalent mTOR Inhibitor, DHM25, Shows in Vivo Antitumor Activity against Triple-Negative Breast Cancer Cells
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Constitutive activation of the PI3K/mTOR signaling pathway contributes to carcinogenesis and metastasis in most, if not all, breast cancers. From a chromene backbone reported to inhibit class I PI3K catalytic subunits, several rounds of chemical syntheses led to the generation of a new collection of chromologues that showed enhanced ability to kill PI3K-addicted cancer cells and to inhibit Akt phosphorylation at serine 473, a hallmark of PI3K/mTOR activation. This initial screen uncovered a chromene designated DHM25 that exerted potent antitumor activity against breast tumor cell lines. Strikingly, DHM25 was shown to be a selective and covalent inhibitor of mTOR using biochemical and cellular analyses, modeling, and a large panel of kinase activity assays spanning the human kinome (243 kinases). Finally, in vivo, this novel drug was an efficient inhibitor of growth and metastasis of triple-negative breast cancer cells, paving the way for its clinical application in oncology. (Figure Presented).
- Fouqué, Amélie,Delalande, Olivier,Jean, Mickael,Castellano, Rémy,Josselin, Emmanuelle,Malleter, Marine,Shoji, Kenji F.,Hung, Mac Dinh,Rampanarivo, Hariniaina,Collette, Yves,Van De Weghe, Pierre,Legembre, Patrick
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supporting information
p. 6559 - 6573
(2015/09/07)
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- 2-CARBOXAMIDE-7-PIPERAZINYL-BENZOFURAN DERIVATIVES 774
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The present invention relates to compounds of formula (I), wherein R1 is heteroaryl or heterocyclyl, optionally substituted;R2 is C1-4alkyl, heterocyclyl, C1-4alkylaryl, C1-4alkylheteroaryl, carbocycl
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Page/Page column 34
(2011/01/05)
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- PHARMACEUTICAL COMPOSITIONS AND METHODS OF PREVENTING, TREATING, OR INHIBITING INFLAMMATORY DISEASES, DISORDERS, OR CONDITIONS OF THE SKIN, AND DISEASES, DISORDERS, OR CONDITIONS ASSOCIATED WITH COLLAGEN DEPLETION
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The present invention provides compositions and methods for preventing, treating, or inhibiting inflammatory diseases, disorders, or conditions of the skin, and diseases, disorders, or conditions associated with collagen depletion using one or more estrogenic agents.
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- Tetracyclic compounds as estrogen ligands
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This invention provides estrogen receptor modulators having the structure: wherein R1, R2, R3, R4, Q, n, R8, R9, R10, and R11 have been defined in the specification; o
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Page/Page column 15; 21
(2010/02/15)
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- A Convergent Synthesis of the Macrocyclic Core of Cytotrienins: Application of RCM for Macrocyclization
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(Equation presented) The asymmetric synthesis of the fully elaborated macrocyclic core of cytotrienins A-D, potent apoptosis-inducing agents, is described. Synthetic highlights include the construction of the aniline bond using a copper-mediated amidation and the use of a ring-closing metathesis (RCM) reaction to efficiently install the (E,E,E)-triene and simultaneously construct the macrocyclic lactam.
- Evano, Gwilherm,Schaus, Jennifer V.,Panek, James S.
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p. 525 - 528
(2007/10/03)
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- Ligand tuning in the chromium-salen-mediated asymmetric epoxidation of alkenes
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A series of Cr(salen) complexes have been synthesised from 5-substituted-3-bromosalicylaldehydes and trans-1,2-cyclohexanediamine. These have been used to probe the Cr(salen)-mediated asymmetric epoxidation of alkenes. No simple correlation was found between the electronic character of the salen-substituents and the enantioselectivity - multiple oxidation pathways are proposed as a possible explanation. Enantioselectivities of up to 90% have been achieved using a novel, synthetically accessible Cr(salen) complex.
- McGarrigle,Murphy,Gilheany
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p. 1343 - 1354
(2007/10/03)
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- Substituted 2-phenyl benzofurans as estrogenic agents
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This invention provides estrogen receptor modulators of formula I, having the structure wherein R, R′, A, A′, X, Y, and Y are as defined in the specification, or a pharmaceutically acceptable salt thereof.
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- 1,2,3,4-Tetrahydroisoquinoline analogs of phenylalkylamine stimulants and hallucinogens
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Conformationally constrained, 1,2,3,4-tetrahydroisoquinoline (TIQ) analogs of central stimulant (e.g. amphetamine) and hallucinogenic (e.g. DOM) phenylalkylamines were prepared and evaluated to determine the contribution to activity of this conformational
- Malmusi, Luca,Dukat, Malgorzata,Young, Richard,Teitler, Milt,Darmani, Nissar A.,Ahmad, Bashir,Smith, Carol,Glennon, Richard A.
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p. 400 - 411
(2007/10/03)
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- SYNTHESIS OF 2,3-DIHYDRO-1H-PHENALENE DERIVATIVE BY THE INTRAMOLECULAR DIELS-ALDER REACTION OF BENZYNE WITH FURAN
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2,3-Dihydro-1H-phenalene derivative 1 was synthesized by the intramolecular Diels-Alder reaction (21->22). 2,5-Dimethylpyrrole was used as a protecting group for the primary amine.
- Darlington, W. H.,Szmuszkovicz, J.
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p. 1883 - 1886
(2007/10/02)
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