cas 62965-10-0, Cbz-L-tert-Leucine | Articles data

Articles about 62965-10-0Total 21 be found

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Optimization of peptide-based inhibitors targeting the HtrA serine protease in Chlamydia: Design, synthesis and biological evaluation of pyridone-based and N-Capping group-modified analogues
The obligate intracellular bacterium Chlamydia trachomatis (C. trachomatis) is responsible for the most common bacterial sexually transmitted infection and is the leading cause of preventable blindness, representing a major global health burden. While C.
Hwang, Jimin,Strange, Natalie,Phillips, Matthew J.A.,Krause, Alexandra L.,Heywood, Astra,Gamble, Allan B.,Huston, Wilhelmina M.,Tyndall, Joel D.A.
supporting information

(2021/07/16)

Amino acid chiral ligand containing bidentate coordination group, chiral catalyst, and corresponding preparation methods and applications thereof
The present invention relates to an amino acid chiral ligand containing a bidentate coordination group, a chiral catalyst, and corresponding preparation methods and applications thereof. The chiral ligand is prepared from a cheap and easily available amino acid, and the development of the chiral ligand can improve the diversity of the chiral ligand. The chiral Ir (III) catalyst is simply and efficiently prepared from the chiral ligand only through a one-step reaction. The chiral Ir (III) catalyst is characterized in that a bidentate guiding group is introduced to an amino acid framework to change the original coordination mode of the amino acid and Ir in order to enhance the chiral control ability of the amino acid to the Ir(III) catalyst. The chiral Ir(III) catalyst is designed and synthesized for the first time, and the selectivity reaches up to 99% ee when the catalyst is successfully applied to the high-efficiency asymmetric synthesis of chiral gamma-cyclolactam, so the catalyst has superior stereo control ability.
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Paragraph 0073

(2019/10/02)

Bifunctional Br?nsted Base Catalyzes Direct Asymmetric Aldol Reaction of α-Keto Amides
The first enantioselective direct cross-aldol reaction of α-keto amides with aldehydes, mediated by a bifunctional ureidopeptide-based Br?nsted base catalyst, is described. The appropriate combination of a tertiary amine base and an aminal, and urea hydro
Echave, Haizea,López, Rosa,Palomo, Claudio
supporting information
p. 3364 - 3368
(2016/03/22)

Prodrug of an ice inhibitor
This invention describes an ICE inhibitor prodrug (I) having good bioavailability. Compound I is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, inflammatory periton
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Page/Page column 14-15

(2016/11/24)

PEPTIDOMIMETIC COMPOUNDS AND ANTIBODY-DRUG CONJUGATES THEREOF
This invention relates to peptidomimetic linkers and anti-body drug conjugates thereof, to pharmaceutical compositions containing them, and to their use in therapy for the prevention or treatment of cancer.
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Page/Page column 177; 178

(2015/07/07)

Ureidopeptide-based Bronsted bases: Design, synthesis and application to the catalytic enantioselective synthesis of β-amino nitriles from (arylsulfonyl)acetonitriles
The addition of cyanoalkyl moieties to imines is a very attractive method for the preparation of β-amino nitriles. We present a highly efficient organocatalytic methodology for the stereoselective synthesis of β-amino nitriles, in which the key to success is the use of ureidopeptide-based Bronsted base catalysts in combination with (arylsulfonyl)acetonitriles as synthetic equivalents of the acetonitrile anion. The method gives access to a variety of β-amino nitriles with good yields and excellent enantioselectivities, and broadens the stereoselective Mannich-type methodologies available for their synthesis. Learning from peptides: A concise route for the catalytic enantioselective synthesis of β-amino nitriles has been achieved by using ureidopeptide-based Bronsted bases as catalysts in the Mannich reaction of N-Boc imines and (arylsulfonyl)acetonitriles (see scheme; Boc=tert-butoxycarbonyl, napht=naphthyl, TMS=trimethylsilyl).
Diosdado, Saioa,Lopez, Rosa,Palomo, Claudio
p. 6526 - 6531
(2014/06/09)

IAP ANTAGONISTS
There are disclosed compounds that modulate the activity of inhibitors of apoptosis (IAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
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Paragraph 00232

(2014/01/09)

PROCESS FOR THE PREPARATION OF PROTEASE INHIBITORS
A process for preparing enantioselectively a compound of formula (la) or (Ib) over a compound of formulas I-2—1h.
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Page/Page column 36

(2012/12/13)

PROCESSES AND INTERMEDIATES
A process for preparing enantioselectively a compound of formula la or lb: over a compound of formulas 1-2 - Ih:
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Page/Page column 37

(2012/12/13)

PROCESS FOR PRODUCTION OF N-ALKOXYCARBONYL-tert-LEUCINES
A high quality N-alcoxycarbonyl-tert leucine can be efficiently and stably produced with an easy procedure by reacting tert-leucine with an N-alcoxycarbonylating agent in the presence of water, wherein the use amount of the N-alcoxycarbonylating agent is not less than 0.90 times by mole and not more than 1.00 times by mole relative to the tert-leucine, with maintaining the pH of the reaction mixture in the range of not less than 9 and not more than 13 using a basic agent. In addition, an N-alcoxycarbonyl-tert-leucine can be efficiently extracted from the basic aqueous solution thereof under a mild condition using a water-immiscible solvent by mixing a hydroxide. Furthermore, the two crystal forms of N-butoxycarbonyl-tert-leucine can be controlled by adjusting the water amount in crystallization step, and the compound can be stably produced in an industrial production.
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Page/Page column 12-13

(2012/03/26)

PROCESSES AND INTERMEDIATES
A process for preparing enantioselectively a compound of formula I-la or I-lb: over a compound of formulas 1-2 - 1-7
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Page/Page column 35-36

(2011/12/14)

Hybrid NH2-benzimidazole ligands for efficient Ru-catalyzed asymmetric hydrogenation of aryl ketones
Readily available hybrid NH2/benzimidazole ligands (R-bimaH, 1) dramatically influence the outcome of established Ru-based catalysts during asymmetric hydrogenation of aryl ketones. The benzimidazole functionality results in reversal of the typically observed chiral induction and allows for hydrogenation to be uncharacteristically conducted in nonprotic solvents. The developed systems efficiently catalyzed the AH of a number of ketones in up to 99% ee.
Li, Yuehui,Ding, Kuiling,Sandoval, Christian A.
supporting information; experimental part
p. 907 - 910
(2009/07/25)

Processes and intermediates
The invention relates to compounds and processes useful for the preparation of protease inhibitors, particularly serine protease inhibitors. The protease inhibitors are useful for treatment of HCV infections.
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Page/Page column 44

(2010/11/26)

PROCESSES AND INTERMEDIATES
The invention relates to processes and compounds useful for producing modified aspartic acid derivatives, such as aspartic acid aldehyde moieties. Aspartic acid derivatives are useful for preparing caspase inhibitors and/or prodrugs thereof.
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Page/Page column 70

(2008/06/13)

ANTIBACTERIAL AGENTS
Selected compounds of formula (I) are antibacterial agents: formula (I) wherein R2 represents a substituted or unsubstituted C1-C6 alkyl, cycloalkyl (C1-C6 alkyl)- or aryl (C1-C6 /SUB
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Page/Page column 9-10

(2010/02/11)

Antipicornaviral compounds compositions containing them and methods for their use
Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treatin
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(2008/06/13)

Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 3. Structure-activity studies of ketomethylene-containing peptidomimetics
The structure-based design, chemical synthesis, and biological evaluation of various ketomethylene-containing human rhinovirus (HRV) 3C protease (3CP) inhibitors are described. These compounds are comprised of a peptidomimetic binding determinant and an e
Dragovich, Peter S.,Prins, Thomas J.,Zhou, Ru,Fuhrman, Shella A.,Patick, Amy K.,Matthews, David A.,Ford, Clifford E.,Meador III, James W.,Ferre, Rose Ann,Worland, Stephen T.
p. 1203 - 1212
(2007/10/03)

CYTOKINE INHIBITING IMIDAZOLE SUBSTITUTED HYDROXAMIC ACID DERIVATIVES
The present invention relates to a series of novel imidazole substituted hydroxamic acid derivatives, and compositions useful thereof as inhibitors of matrix degrading metalloproteinases, in particular collagenase.
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(2008/06/13)

Inhibitors of farnesyl protein transferase
Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formula their enantiomers, diastereomers, and pharmaceutically acceptable salts, prodrugs, and solvates, wherein:, ???G is ???when G is it is optionally substituted, at any available position or positions, with halo, alkyl or substituted alkyl having 1 to 20 carbon atoms, alkoxy, or a combination of these groups;, ???G1is optionally substituted, at any of the available position or positions on the ring, with halo, alkyl or substituted alkyl having 1 to 20 carbon atoms, alkoxy, aryl, aralkyl, hydroxy, alkanoyl, alkanoyloxy, amino, alkylamino, dialkylamino, alkanoylamino, thiol, alkylthio, alkylthiono, alkylsulfonyl, sulfonamido, nitro, cyano, carboxy, carbamyl, N-hydroxycarbamyl, N-alkylcarbamyl, N-dialkylcarbamyl, alkoxycarbonyl, phenyl, substituted phenyl, or a combination of these groups;, ???G2is or -NR6-CH(Q1)-;, ???J, K and L are each, independently, N, NR7, O, S or CR6with the provisos that only one of the groups J, K and L can be O or S, and at least one of the groups J or L must be N, NR7, O or S to form a fused five-membered heteroring; the bond between J and K or K and L may also form one side of a phenyl ring fused to the fused five-membered heteroring;, ???Q is is alkyl, cycloalkyl, substituted alkyl, aryl, pyrrolyl, furyl, thiophenyl, imidazolyl, oxazolyl, thiazolyl, pyrazolyl, pyrrolidyl or pyridyl;, ???Q1, A1and A2are each, independently, H, alkyl, substituted alkyl, phenyl or substituted phenyl;, ???G3is R8, -C(O)OR8, -C(O)NR8R9, -C(O)N(R10)OR8, -C(O)NHSO2R11or -CH2OR8;, ???X is -SH, -OH or -NHR12;, ???X1is -NR13-, -CH2- or -CH(NHR14)-;, ???Y and Z are each, independently, -CH2- or -C(O)-;, ???R1- R14are each, independently, H or alkyl having 1 to 20 carbon atoms;, ???R3may also be substituted alkyl or cycloalkyl; R4, R5and R11may also be aryl or aralkyl; R7, R8, R9and R10may also be aralkyl; and R12, R13and R14may also be substituted alkyl or aralkyl;, ???m is 0 or an integer from 1 to 2;, ???q is 0 or an integer from 1 to 3;, ???t is an integer from 1 to 2; and, ???the dotted line represents an optional double bond.
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(2008/06/13)

Imidazole-containing inhibitors of farnesyl protein transferase
Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formula their enantiomers, diastereomers, and pharmaceutically acceptable salts, prodrugs, and solvates, wherein:, G is G1 is G2 is or -NR10-CH(Q1)-;, J, K and L are each, independently, N, NR9, O, S or CR10 with the provisos that only one of the groups J, K and L can be O or S, and at least one of the groups J or L must be N, NR9, O or S to form a fused five-membered heteroring; the bond between J and K or K and L may also form one side of a phenyl ring fused to the fused five-membered heteroring;, Q is aryl;, Q1, A1 and A2 are each, independently, H, alkyl, substituted alkyl, phenyl or substituted phenyl;, G3 is R11, -C(O)OR11, -C(O)NR11R12, 5-tetrazolyl, -C(O)N(R13)OR11, -C(O)NHSO2R14 or -CH2OR11;, G4 is attached at the 1, 2, 4 or 5 position and optionally substituted, at any of the available position or positions on the ring, with halo, alkyl or substituted alkyl having 1 to 20 carbon atoms, alkoxy, aryl, aralkyl, hydroxy, alkanoyl, alkanoyloxy, amino, alkylamino, dialkylamino, alkanoylamino, thiol, alkylthio, alkylthiono, alkylsulfonyl, sulfonamido, nitro, cyano, carboxy, carbamyl, N-hydroxycarbamyl, N-alkylcarbamyl, N-dialkylcarbamyl, alkoxycarbonyl, phenyl, substituted phenyl, or a combinaton of these groups;, Y and Z are each, independently, -CH2- or -C(O)-;, R1 - R14 are each, independently, H or alkyl having 1 to 20 carbon atoms;, R7, R8 and R14 may also be aryl or aralkyl, and R3, R9, R11, R12 and R13 may also be aralkyl;, m, n and p are each, independently, 0 or an integer from 1 to 2;, q is 0 or an integer from 1 to 4; and, the dotted line represents an optional double bond.
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(2008/06/13)

Heterocyclic inhibitors of farnesyl protein transferase
Inhibition of farnesyl protein transferase is effected by compounds of the formula its enantiomers, diastereomers, pharmaceutically acceptable salts, prodrugs or solvates thereof, wherein:, A1 and A2 are each independently H, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, phenyl or substituted phenyl;, G1 is S or O;, G2 is H, -C(O)OH, -C(O)NH2, 5-tetrazolyl, -C(O)N(R7)OH or -CH2OH;, X is O or R8N;, Y and Z are each independently -CH2- or -C(O)-;, R1, R2, R3, R4, R5, R6 and R7 are each independently H or alkyl;, R1 may also be alkanoyl, R1 and A1 taken together may be -(CH2)m;, R8 is H, alkyl, phenyl, phenylalkyl, substituted phenyl, (substituted phenyl)alkyl or -C(O)R9;, R9 is H, alkyl, phenyl, phenylalkyl, substituted phenyl or (substituted phenyl)alkyl;, m is 3 or 4;, n is 0, 1 or 2;, p is 0, 1 or 2; and, q is 0 or 1, with the proviso that when p is 0, then q is also 0.
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(2008/06/13)