- METHODS AND COMPOSITIONS FOR TARGETED PROTEIN DEGRADATION
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Provided herein are methods and compositions for targeted protein degradation. In one aspect, a protein degradation chimera is provided, comprising: a first moiety that is capable of binding to a chaperone complex component; a second moiety that is capabl
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Page/Page column 21
(2020/10/21)
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- COMPOUNDS AND METHODS USEFUL FOR TREATMENT OF DISEASES MEDIATED BY HIF-1
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Provided herein are compounds that are useful in treatment of diseases mediated by HIF-1.
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Page/Page column 76
(2012/05/19)
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- Synthesis and activity of N-oxalylglycine and its derivatives as Jumonji C-domain-containing histone lysine demethylase inhibitors
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N-Oxalylglycine (NOG) derivatives were synthesized, and their inhibitory effect on histone lysine demethylase activity was evaluated. NOG and compound 1 inhibited histone lysine demethylases JMJD2A, 2C and 2D in enzyme assays, and their dimethyl ester prodrugs DMOG and 21 exerted histone lysine methylating activity in cellular assays.
- Hamada, Shohei,Kim, Tae-Dong,Suzuki, Takayoshi,Itoh, Yukihiro,Tsumoto, Hiroki,Nakagawa, Hidehiko,Janknecht, Ralf,Miyata, Naoki
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scheme or table
p. 2852 - 2855
(2010/07/03)
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- FLUORESCENT SUBSTRATES FOR MONOAMINE TRANSPORTERS AS OPTICAL FALSE NEUROTRANSMITTERS
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The present invention relates to compounds of the general structure: wherein Y is O, X is O, bond α is absent and bond β is present, or Y is H, X is CH, bond α is present, and bond β is absent; atom Z is a carbon and bonds χ, δ and γ are present, or is a nitrogen and bonds χ, δ and γ are absent; R1 is -H, -OH, -O-R7, -N(H) -R8, -N (H) - (CH2) n-NH2, -N(R9) (R10), or a piperazine cation; R2 is either covalently bound to R9, or is -H, or is covalently bound to R3 so as to form a substituted or unsubstituted pyrrole or R2 is covalently bound to R9 or R8 or R7; or R1 and R2 are covalently joined to form an aromatic ring; R3 is either covalently bound to R2 so as to form a pyrrole, or is, inter alia, -H, -OH, alkyl, or when Z is nitrogen R3 is =O; R4 is, inter alia, -H, -OH, or -R11NH2; R5 is, inter alia, -H, -OH, or -R12NH2, and R6 is either is covalently bound to R10 or is -H, or R6 is covalently bound to R10 or R8 or R7. This invention also provides processes for making the compounds as well as methods for monitoring activity of monoamine transporters or treating monoamine transporter-associated diseases by employing the compounds.
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- AMINOETHYLAROMATIC COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR
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The present invention relates to aromatic compounds of the formula (I) wherein Ar is phenyl or an aromatic 5-or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical Ra and wherein Ar may also carry 1 or 2 radicals Rb; X is N or CH; E is CR6R7 or NR3;R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated Cl-C4--alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C 4-cycloalkylmethyl, fluorinated C3-C4--alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H, C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1--C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C 3-C4-cycloalkylmethyl, fluorinated C3--C 4-alkenyl, or R1a and R2 together are (CH 2)n with n being 2, 3 or 4, or R1a and R 2a together are (CH2)n with n being 2, 3 or 4; R2 and R2a are independently of each other H, C1-C4-alkyl or fluorinated C1-C 4-alkyl or R2a and R2 together are (CH 2)m with m being 1, 2, 3, 4 or 5; R3 is H or C1-C4-alkyl; R6, R7 independently of each other are selected from H, fluorine, C1-C4-alkyl and fluorinated C1-C4-alkyl or together form a moiety (CH2)p with p being 2, 3, 4 or 5; and the physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula (I) or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.
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Page/Page column 98-99
(2010/11/08)
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- Phenethylamino sulfamic acids
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Compounds of formula (I): are effective in the treatment of protein tyrosine phosphatase (PTPase) mediated disorders such as diabetes.
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- Substituted alkylamine derivatives and methods of use
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Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
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- Substituted alkylamine derivatives and methods of use
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Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
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Page 49; 112
(2010/02/05)
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- Efficient synthesis of protected β-phenylethylamines, enantiomerically pure protected β-phenyl-α-benzylethylamines and β-phenyl-α-isopropylethylamines using organozinc chemistry
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The β-aminoalkylzinc reagents 9a, 10 and 11 have been efficiently prepared using DMF as a solvent. Palladium-catalysed coupling of these reagents with substituted aryl iodides, under mild and convenient conditions, gives protected β-phenylethylamines 6 in
- Hunter, Christopher,Jackson, Richard F. W.,Rami, Harshad K.
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p. 219 - 223
(2007/10/03)
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- Synthesis and Evaluation of Novel Spermidine Derivatives as Targeted Cancer Chemotherapeutic Agents
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The utility of the spermidine moiety as the homing device for the selective delivery of chemotherapeutic and diagnostic agents into cancer cells was explored.Two spermidine analogs containing a cytotoxic agent were synthesized, N-3,4-bis(benzyloxy)phenet
- Stark, Peter A.,Thrall, Brian D.,Meadows, Gary G.,Abdel-Monem, Mahmoud M.
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p. 4264 - 4269
(2007/10/02)
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