- ALKYLBORONIC ACIDS AS ARGINASE INHIBITORS
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Provided are alkylboronic acids as arginase inhibitors represented by formula (I), or a pharmaceutically acceptable salt, stereoisomer, tautomer, or prodrug thereof and a pharmaceutical composition comprising said compounds.
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Page/Page column 103
(2020/08/22)
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- DIPEPTIDE ANALOGS AS TGF-BETA INHIBITORS
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The present disclosure is concerned with dipeptide analogs that are capable of inhibiting TGF-β and methods of treating cancers such as, for example, multiple myeloma and a hematologic malignancy, methods for immunotherapy, and methods of treating fibroti
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Paragraph 0457-0460
(2019/05/15)
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- HETEROCYCLIC COMPOUNDS AS ARGINASE INHIBITORS
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The present invention relates to heterocyclic compounds as arginase inhibitors, in particular to a compound represented by Formula (I), or a pharmaceutically acceptable salt, stereoisomer or tautomer, or prodrug thereof and a pharmaceutical composition comprising said compound.
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Page/Page column 68
(2019/07/13)
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- NOVEL PYRIDINE DERIVATIVES
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The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
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Page/Page column 33-34
(2013/02/27)
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- PYRIDIN- 2 -AMIDES USEFUL AS CB2 AGONISTS
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The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
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Page/Page column 80
(2013/02/27)
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- Isoselenocyanates derived from Boc/Z-amino acids: Synthesis, isolation, characterization, and application to the efficient synthesis of unsymmetrical selenoureas and selenoureidopeptidomimetics
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Isoselenocyanates derived from Boc/Z-amino acids are prepared by the reaction of the corresponding isonitriles with selenium powder in presence of triethylamine at reflux. The utility of these new classes of isoselenocyanates in the preparation of selenoureidodipeptidomimetics possessing both amino as well as carboxy termini has been accomplished. The 1H NMR analysis confirmed that the protocol involving the conversion of isonitriles to isoselenocyanates and their use as coupling agents in assembling selenoureido derivatives is free from racemization.
- Chennakrishnareddy, Gundala,Nagendra, Govindappa,Hemantha, Hosahalli P.,Das, Ushati,Guru Row, Tayur N.,Sureshbabu, Vommina V.
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supporting information; experimental part
p. 6718 - 6724
(2010/09/30)
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- Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C
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A series of dipeptide nitriles with a thienyl alanine in P2 were identified as potent and selective cathepsin C inhibitors. Incorporation of a substituted cyclopropyl moiety in P1 effectively protects these derivatives against hydrolase activity in whole blood.
- Guay, Daniel,Beaulieu, Christian,Jagadeeswar Reddy,Zamboni, Robert,Methot, Nathalie,Rubin, Joel,Ethier, Diane,David Percival
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scheme or table
p. 5392 - 5396
(2010/05/02)
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- DERIVATIVES OF 6,7-DIHYDRO-5H-IMIDAZO[1,2-α]IMIDAZOLE-3- CARBOXYLIC ACID AMIDES
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Derivatives of 6,7-dihydro-5H-imidazo[1,2-α]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
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Page/Page column 102
(2009/07/03)
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- PYRIDINE DERIVATIVES AS SODIUM CHANNEL BLOCKERS
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Compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein; each of R1 to R4 is independently selected from hydrogen and C1-4 alkyl, and each of rings A and B independently is optionally further substi
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Page/Page column 24
(2010/11/30)
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- QUINAZOLINE DERIVATIVES
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A quinazoline derivative of the formula (I) wherein: R1, R2, R3, R3a, R4, R5, R5a R6, R7, a, m and p are as defined in the description. Also claimed are pharmaceutical compositions containing the quinazoline derivative, the use of the quinazoline derivatives as medicaments and processes for the preparation of the quinazoline derivative. The quinazoline derivatives of formula (I), are useful in the treatment of hyperproliferative disorders such as a cancer.
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Page/Page column 199
(2008/06/13)
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- Synthesis and conformational investigation of tetrapeptide analogues of the fragment B23-B26 of insulin
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Tetrapeptides containing one of a set of four different α,α-dialkyl glycines at the C-terminus were synthesized by conventional methods in solution and their conformational behavior investigated by 1H NMR spectroscopy in connection with molecular mechanics calculations. The results were consistent with conformations stabilized by a γ-turn in the case of compounds with alkyl groups larger than methyl, while the corresponding Aib derivative did not exhibit intramolecular hydrogen bonding. Graphical Abstract
- Rodrigues, Lígia M.,Fonseca, José I.,Maia, Hernani L.S.
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p. 8929 - 8936
(2007/10/03)
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- Ammonium salts from polymer-bound N-hydroxysuccinimide as solid-supported reagents for EDC-mediated amidations
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New ammonium and alkylammonium salts derived from a polymeric N-hydroxysuccinimide (P-HOSu) have been prepared and used for the amidation of carboxylic acids and amino acids mediated by 1-ethyl-3-(3′-dimethylamino-propyl)carbodiimide hydrochloride (EDC). These polymer-supported ammonium salts afforded the corresponding amides in good yield, without detectable α-racemization and with easy recovery of the P-HOSu after the amidation reaction, being especially suitable for the amidation of Fmoc-protected amino acids.
- Chinchilla, Rafael,Dodsworth, David J.,Nájera, Carmen,Soriano, José M.
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p. 463 - 466
(2007/10/03)
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- Dipeptide nitriles
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N-terminal substituted dipeptide nitriles as defined are useful as inhibitors of cysteine cathepsins, e.g. cathepsins B, K, L and S, and can be used for the treatment of cysteine cathepsin dependent diseases and conditions, including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis, tumors (especially tumor invasion and tumor metastasis), coronary disease, atherosclerosis (including atherosclerotic plaque rupture and destabilization). Particular dipeptide nitriles are compounds of formula I, or physiologically-acceptable and -cleavable esters or a salts thereof wherein: the symbols are as defined. In particular it has been found that by appropriate choice of groups R, R2, R3, R4, R5, X1, Y and L, the relative selectivity of the compounds as inhibitors of the various cysteine cathepsin types, e.g. cathepsins B, K, L and S may be altered, e.g. to obtain inhibitors which selectively inhibit a particular cathepsin type or combination of cathepsin types.
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Page column 26-27
(2010/02/05)
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- Design and synthesis of dipeptide nitriles as reversible and potent cathepsin S inhibitors
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The specificity of the immune response relies on processing of foreign proteins and presentation of antigenic peptides at the cell surface. Inhibition of antigen presentation, and the subsequent activation of T-cells, should, in theory, modulate the immune response. The cysteine protease Cathepsin S performs a fundamental step in antigen presentation and therefore represents an attractive target for inhibition. Herein, we report a series of potent and reversible Cathepsin S inhibitors based on dipeptide nitriles. These inhibitors show nanomolar inhibition of the target enzyme as well as cellular potency in a human B cell line. The first X-ray crystal structure of a reversible inhibitor cocrystallized with Cathepsin S is also reported.
- Ward, Yancey D.,Thomson, David S.,Frye, Leah L.,Cywin, Charles L.,Morwick, Tina,Emmanuel, Michel J.,Zindell, Renée,McNeil, Daniel,Bekkali, Younes,Giradot, Marc,Hrapchak, Matt,DeTuri, Molly,Crane, Kathy,White, Della,Pav, Susan,Wang, Yong,Hao, Ming-Hong,Grygon, Christine A.,Labadia, Mark E.,Freeman, Dorothy M.,Davidson, Walter,Hopkins, Jerry L.,Brown, Maryanne L.,Spero, Denice M.
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p. 5471 - 5482
(2007/10/03)
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- Efficient synthesis of primary amides using 2-mercaptopyridone-1-oxide-based uronium salts
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S-(1-Oxido-2-pyridinyl)-1,1,3,3-tetramethylthiouronium tetrafluoroborate (TOTT) and hexafluorophosphate (HOTT) are cheap and convenient reagents for the rapid and high-yielding preparation of primary amides when reacted with carboxylic acids and ammonium chloride in the presence of diisopropylethylamine. The reaction is chemoselective and undesired ammonolysis of other sensitive functional groups is not observed. (C) 2000 Elsevier Science Ltd.
- Bailen,Chinchilla,Dodsworth,Najera
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p. 9809 - 9813
(2007/10/03)
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