- INHIBITORS OF ENL/AF9 YEATS
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Methods and compositions for treating leukemia are disclosed. Acylated 6-aminoindoles, acylated 6-aminopyrrolopyridines and acylated 3-aminopyrrolo[3,2-c]pyridazines of the following formula inhibit ENL/AF9 YEATS and are therefore useful for treating leukemia.
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- HEPATITIS B CORE PROTEIN MODULATORS
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The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound of formula:
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- Design and Synthesis of 2,2′-Diindolylmethanes to Selectively Target Certain G-Quadruplex DNA Structures
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G-quadruplex (G4) structures carry vital biological functions, and compounds that selectively target certain G4 structures have both therapeutic potential and value as research tools. Along this line, 2,2′-diindolylmethanes have been designed and synthesi
- Livendahl, Madeleine,Jamroskovic, Jan,Ivanova, Svetlana,Demirel, Peter,Sabouri, Nasim,Chorell, Erik
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supporting information
p. 13004 - 13009
(2016/09/09)
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- Synthesis of diverse indole libraries on polystyrene resin - Scope and limitations of an organometallic reaction on solid supports
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The synthesis of diverse substituted indole structures on solid supports is described. The immobilization of nitrobenzoic acid onto Merrifield resin and the subsequent treatment with alkenyl Grignard reagents delivered indole carboxylates bound to solid s
- Knepper, Kerstin,Vanderheiden, Sylvia,Braese, Stefan
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experimental part
p. 1191 - 1199
(2012/09/07)
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- 3, 4-SUBSTITUTED PYRROLIDINE DERIVATIVES FOR THE TREATMENT OF HYPERTENSION
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The invention relates to the use of (3,4-di-, 3,3,4-tri, 3,4,4-tri- or 3,3,4,4-tetra-)substituted pyrrolidine compounds for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; compounds that are part of a subclass of these substituted pyrrolidine compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (= disorder) that depends on activity of renin; new compounds that are part of a subclass of these substituted pyrrolidine compounds; pharmaceutical formulations comprising said substituted pyrrolidine compounds, and/or a method of treatment comprising administering said substituted pyrrolidine compounds, a method for the manufacture especially of said new substituted pyrrolidine compounds, as well as novel intermediates, starting materials and/or partial steps for their synthesis. The substituted pyrrolidine compounds are of the formula (I), wherein R1, R2, R3, R4, R5 and T are defined as in the specification.
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Page/Page column 159-160
(2010/11/24)
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- Method of inhibiting neoplastic cells with indole derivatives
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A method for inhibiting neoplasia, particularly cancerous and precancerous lesions, by exposing the affected cells to indole derivatives.
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- Method for inhibiting neoplastic cells with indole derivatives
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A method for inhibiting neoplastic cells and related conditions by exposing them to substituted indole derivatives.
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- Substituted azabicyclic compounds
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This invention is directed to certain physiologically active compounds of formula (I) wherein represents a bicyclic ring system, of about 10 to about 13 ring members, in which the ring is an azaheterocycle, and the ring represents an azaheteroaryl ring, or an optionally halo substituted benzene ring; and N-oxides thereof, and their prodrugs, and pharmaceutically acceptable salts and solvates of the compounds of formula (I) and N-oxides thereof, and their prodrugs. Such compounds inhibit the production or physiological effects of TNF and inhibit cyclic AMP phosphodiesterase. The invention is also directed to pharmaceutical compositions comprising compounds of formula (I), their pharmaceutical use and methods for their preparation.
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- Indole derivatives as cGMP-PDE inhibitors
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Compounds of the formula (I): STR1 and their pharmaceutically acceptable compositions are useful in inhibiting the activity of cyclic guanosine 3',5'-monophosphate phosphodiesterase.
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- The synthesis and biological evaluation of a novel series of indole PDE4 inhibitors I
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This communication describes the synthesis and in vitro evaluation of a novel potent series of phosphodiesterase type (IV) (PDE4) inhibitors. The compounds described contain an indole moiety which replaces the 'rolipram- like' 3-methoxy-4-cyclopentoxy motif. Several of the compounds presented possess low nanomolar IC50's for PDEIV inhibition. In vivo activities determined from measurement of serum TNF-α levels in LPS challenged mice (mouse endotoxemia model) are also reported.
- Hulme, Christopher,Moriarty, Kevin,Miller, Bruce,Mathew, Rose,Ramanjulu, Mercy,Cox, Paul,Souness, John,Page, Ken M.,Uhl, Joanne,Travis, Jeffrey,Huang, Fu-Chih,Labaudiniere, Richard,Djuric, Stevan W.
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p. 1867 - 1872
(2007/10/03)
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- Orally active indole N-oxide PDE4 inhibitors
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This communication describes the synthesis and in vitro and in vivo evaluation of a novel potent series of phosphodiesterase type (IV) (PDE4) inhibitors. Several of the compounds presented possess low nanomolar IC50's for PDE4 inhibition and excellent in vivo activity for inhibition of TNF-α levels in LPS challenged mice (mouse endotoxemia model). Emesis studies (dog) and efficacy in a SCW arthritis model for the most potent PDE4 inhibitors are presented.
- Hulme, Christopher,Mathew, Rose,Moriarty, Kevin,Miller, Bruce,Ramanjulu, Mercy,Cox, Paul,Souness, John,Page, Ken M.,Uhl, Joanne,Travis, Jeffrey,Labaudiniere, Richard,Huang, Fu-Chih,Djuric, Stevan W.
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p. 3053 - 3058
(2007/10/03)
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