Category: 53838-27-0

On March 2, 2006, Andrzej, Roman Batt; Baxter, Andrew John; Heeney, Celine; Stockley, Martin Lee; Bryan Roe, Michael; Hudson, Peter; Handy, Rachel published a patent.Electric Literature of 53838-27-0 The title of the patent was Preparation of tetraaza-benzo[f]azulenes as vasopressin V1a antagonists. And the patent contained the following:

The title compounds I [G = NR5R6, II-V; A1 = CH2, CH(OH), NH, N(alkyl), O and S; A2 = CH2, CH(OH), C(O), NH; A3, A12 = S, NH, N(alkyl), etc.; A4, A13 = CR9, N; A5, A14 = CR10, N; A6 = CH2, NH, N(alkyl), O; A7, A11 = C, N; A8, A9 = CH, N, NH, S, etc.; A10 = CH:CH, CH, N, NH, etc.; the ring constituted by A7-A11 is aromatic; R1-R3 = H, alkyl, O(alkyl), NO2, F, Cl, Br; R4 = H, alkyl, aryl, heteroaryl, etc.; R5, R6 = alkyl, aryl, (CH2)f-aryl, (CH2)f-heteroaryl; R9, R10 = H, alkyl, alkoxy, etc.; W = O, NH; X = (CH2)m, C(O), SOj; Y = O, S, NH, N(alkyl); a, f, j = 1-2; m = 0-2; with provisos] which are vasopressin V1a receptor antagonists, were prepared and formulated. E.g., a multi-step synthesis of 4-(3,3-dimethylbutyl)piperazine-1-carboxylic acid 4-(3,6-dimethyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-2-fluorobenzylamide, starting from 4-(tert-butoxycarbonylamino-methyl)-3-fluorobenzoic acid and 3,6-dimethyl-3,4,9,10-tetrahydro-2,3,4,9-tetraazabenzo[f]azulene (preparations of the reactants was provided), was given. Compounds I were assayed to determine their ability to inhibit the cellular consequences of AVP stimulation on intact cells. In the assay, compounds I cause significant inhibition of cellular activation at concentrations of 30 μM or less. Preferred compounds I cause significant inhibition at concentrations of 300 nM. Pharmaceutical compositions of the compounds I are useful as treatment of dysmenorrhea. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).Electric Literature of 53838-27-0

The Article related to benzoazulene tetraaza triaza preparation vasopressin v1a antagonist dysmenorrhea treatment, Heterocyclic Compounds (More Than One Hetero Atom): Diazepines and other aspects.Electric Literature of 53838-27-0

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On January 29, 2004, Bergnes, Gustave; Smith, Whitney W.; Yao, Bing; Morgans, David J., Jr.; MacDonald, Andrew published a patent.COA of Formula: C10H19NO4 The title of the patent was Preparation of of quinazolinone-like derivatives to treat cellular proliferative diseases. And the patent contained the following:

The invention relates to quinazolinone-like derivatives that are inhibitors of the mitotic kinesin KSP and are useful in the treatment of cellular proliferative diseases, for example cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders and inflammation. Preparation of 3-Benzyl-7-chloro-2-(3-benzyl-2-oxohexahydropyrimidin-4-yl)-3H-quinazolin-4-one is included. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).COA of Formula: C10H19NO4

The Article related to quinazolinone derivative preparation proliferative disease kinesin, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.COA of Formula: C10H19NO4

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Rosowsky, Andre; Forsch, Ronald; Uren, Jack; Wick, Michael published an article in 1981, the title of the article was Methotrexate analogs. 14. Synthesis of new γ-substituted derivatives as dihydrofolate reductase inhibitors and potential anticancer agents.Recommanded Product: (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate And the article contains the following content:

The γ-tert-butyll ester (I) [79640-76-9], γ-hydrazide (II) [79640-75-8], γ-butylamide (III) [79640-74-7], and γ-benzylamide (IV) [71074-45-8] derivatives of methotrexate (MTX) were synthesized from 4-amino-4-deoxy-N10-methylpteroic acid  [19741-14-1] and the appropriate blocked L-glutamic acid precursors with the aid of the peptide bond forming reagent di-Et phosphorocyanidate. The affinity of these side chain modified products for dihydrofolate reductase  [9002-03-3] from Lactobacillus casei and L1210 mouse leukemic cells was determined spectrophotometrically or by competitive radioligand binding assay, and their cytotoxicity was evaluated against L1210 leukemic cells in culture. The results provide continuing support for the view that the γ-terminal region of the MTX side chain is an attractive site for mol. modification of this anticancer agent. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).Recommanded Product: (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate

The Article related to methotrexate analog preparation anticancer, dihydrofolate reductase inhibitor methotrexate analog, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Recommanded Product: (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On March 7, 1989, Kuefner, Ulrike; Lohrmann, Ute; Montejano, Yolanda D.; Vitols, Karin S.; Huennekens, F. M. published an article.Related Products of 53838-27-0 The title of the article was Carboxypeptidase-mediated release of methotrexate from methotrexate α-peptides. And the article contained the following:

Methotrexate (MTX) α-peptides containing representative neutral (alanine), acidic (aspartic acid), and basic (arginine) amino acids were synthesized by a regiospecific route. These peptides were hydrolyzed by carboxypeptidases to yield MTX and the amino acids. Pancreatic carboxypeptidase A (CP-A) hydrolyzed MTX-Ala and, at a much slower rate, MTX-Asp and MTX-Arg. MTX-Ala was also a substrate for pancreatic carboxypeptidase B (CP-B); marginal activity was observed with this enzyme and MTX-Arg. Human serum hydrolyzed only MTX-Arg; biphasic inhibition of this activity by 2-(mercaptomethyl)-3-(guanidinoethyl)thiopropionate was consistent with the known presence of 2 types of endogenous carboxypeptidase (CP-N). Cytotoxicity of the MTX peptides toward L1210 cells in culture was enhanced considerably in the presence of the appropriate carboxypeptidases. MTX-Ala was much less toxic than MTX (ID50 values of 2.0 × 10-6M and 2.4 × 10-8M, resp.), but in the presence of CP-A the ID50 of the peptide improved to 8.5 × 10-8M. Similar results were obtained with MTX-Asp/CP-A and MTX-Ala/CP-B combinations. MTX-Arg showed good cytotoxicity (ID50 of 5.0 × 10-8M), due to CP-N activity in the fetal bovine serum of the culture medium; inclusion of CP-B lowered the ID50 to that of MTX. Possible clin. uses of MTX peptides are discussed. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).Related Products of 53838-27-0

The Article related to methotrexate peptide preparation cytotoxicity carboxypeptidase, antitumor methotrexate peptide prodrug preparation, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Related Products of 53838-27-0

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On December 14, 2006, Degrado, William F.; Bennett, Joel S.; Snyder, Seth Elliot; Choi, Sungwook published a patent.Application In Synthesis of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate The title of the patent was Preparation of prolyl dipeptides as inhibitors of the α2β1/gpIa-IIa integrin. And the patent contained the following:

The invention discloses novel compounds I [X is alkylidene; R1 is aralkylamino, aryl- or alkylsulfonylamino, carbalkoxymethyl, aralkoxycarbonylamino, NHSO2R2, where R2 is aryl, alkyl, aralkyl, aralkoxy, aralkylamino, arylamino, or alkylamino; R3 is halo, nitro, aryl, amino, alkyl, alkoxy, alkylsulfonyl, etc.; R4 is amino, hydroxy, aralkoxy, arylamino, aroylamino; R5 is H or alkyl; R6 is H or :O; A is SO2, PO2, CO2, CO; D is optional and may be one or more CH2 groups; E is aryl or heteroaryl; n, q are 0-2; m is 0 or 1; one of the three dashed-line portions may represent a double bond] or a stereoisomer, prodrug, pharmaceutically-acceptable salt, or N-oxide, which inhibit the integrin α2β1/GPIa-IIa receptor and are useful for the treatment of α2β1-affected disease states. Thus, prolyl peptide II was prepared and showed IC50 = 15 nM for inhibition of platelet adhesion to type I collagen. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).Application In Synthesis of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate

The Article related to prolyl peptide preparation inhibitor integrin, Amino Acids, Peptides, and Proteins: Poly(Amino Acids) and Peptides and other aspects.Application In Synthesis of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On November 30, 1983, Naithani, Vinod K.; Schwertner, Eberhard published an article.Related Products of 53838-27-0 The title of the article was Human proinsulin VI. Synthesis of protected segment 46-70 of prohormone. And the article contained the following:

Title protected peptide Ph3C-Gly-Gly-Pro-Gly-Ala-Gly-Ser(CMe3)-Leu-Gln-Pro-Leu-Ala-Leu-Glu(OCMe3)-Gly-Ser(CMe3)-Leu-Gln-Lys(CO2CMe3)-Arg-Gly-Ile-Val-Glu(OCMe3)-Gln-OH was prepared by a series of fragment condensations in solution The final step involved 2 possible mixed anhydride condensations: the coupling of protected fragment 46-64 with protected fragment 65-70 or the coupling of protected fragment 46-59 with protected fragment 60-70. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).Related Products of 53838-27-0

The Article related to proinsulin pentacosapeptide, Amino Acids, Peptides, and Proteins: Poly(Amino Acids) and Peptides and other aspects.Related Products of 53838-27-0

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On August 26, 2016, Malolanarasimham, Krishnan; Murugan, Ravichandran Narayanasamy; Kedari, Chaitanya Kumar; Tulam, Vijaya Kumar published a patent.Safety of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate The title of the patent was Acylation process for the preparation of liraglutide. And the patent contained the following:

The invention is related to a process for the preparation of an N-substituted peptide or protein comprising: (a) reacting a peptide or protein with a copper agent to form a copper complex of peptide or protein; (b) converting the copper complex of the peptide or protein obtained in step (a) to the desired N-substituted peptide or protein in an organic solvent or in water or mixtures thereof; and (c) optionally, hydrolyzing the N-substituted peptide or protein obtained in step (b) to obtain the desired N-substituted peptide or protein, wherein the N-substituted peptide or protein is the GLP agonist H-His-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-N6 -[N-(1-oxohexadecyl)-γ-Glu]-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Arg-Gly-Arg-Gly-OH (liraglutide). The invention provides an alternate acylation process for preparation of liraglutide high yielding, scalable, cost effective, environment friendly and com. viable by avoiding repeated cumbersome and lengthy purification steps. Specifically, the invention is related to process for the preparation of liraglutide comprising: (i) reacting a liraglutide precursor with a copper agent, e.g., CuSO4•5H2O to form a copper complex of liraglutide precursor, (ii) converting the copper complex of liraglutide precursor obtained in step (i) to N-substituted liraglutide precursor by reacting with an N-acylating agent such as 1-Me palmityl glutamic acid or its reactive derivatives (preparation given); and (iii) hydrolyzing the N-substituted liraglutide precursor obtained in step (ii) to obtain liraglutide. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).Safety of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate

The Article related to acylation liraglutide preparation, Amino Acids, Peptides, and Proteins: Poly(Amino Acids) and Peptides and other aspects.Safety of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On August 31, 1985, Felix, Arthur M.; Heimer, Edgar P.; Wang, Ching Tso; Lambros, Theodore J.; Swistok, Joseph; Roszkowski, Martin; Ahmad, Mustaq; Confalone, Dianne; Scott, John W. published an article.Product Details of 53838-27-0 The title of the article was Synthesis of thymosin α1 by fragment condensation using tert-butyl side chain protection. And the article contained the following:

Thymosin α1 (I) was prepared by classical methods using 7 tert-Bu side chain protected fragments. Optimum conditions were found for the final DCC/HOBt coupling of the two key intermediates; decapeptide and octadecapeptide. I was purified by two stages of preparative HPLC (partial purification with C8 and final purification with C18 reverse phase silica gel) to give a 30% overall yield for the final four stages of synthesis (including catalytic hydrogenation of octadecapeptide, coupling, deprotection and purification). The product was homogeneous according to thin-layer and paper high voltage electrophoresis, isoelec. focusing anal., thin-layer chromatog. and high-performance liquid chromatog. Amino acid anal., optical rotation, 1H NMR spectroscopy, FAB mass spectroscopy and peptide mapping after tryptic digestion confirmed the structure of thymosin α1. Three minor stereoisomer contaminants were isolated by HPLC and characterized as [D-Lys14]-thymosin α1, [D-Lys17]-thymosin α1 and [D-Ala3]-thymosin α1 resulting from racemization at Lys14, Lys17 and Ala3 during the coupling of the fragments. A final contaminant, isolated by HPLC, was characterized as Nα-isobutyloxycarbonyl-thymosin α1 (15-28), which results from “wrong way opening” of an activated mixed anhydride. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).Product Details of 53838-27-0

The Article related to thymosin synthesis fragment condensation, Amino Acids, Peptides, and Proteins: Poly(Amino Acids) and Peptides and other aspects.Product Details of 53838-27-0

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On January 17, 1984, Meienhofer, Johannes A. published a patent.Application of 53838-27-0 The title of the patent was Immunopotentiating peptides. And the patent contained the following:

Peptides H-X-Glu-Asn-OH [X = null, Ala (I), Glu-Glu-Ala (II), Val-Glu-Glu-Ala, Val-Val-Glu-Glu-Ala] and their salts were prepared by known procedures. These di- to heptapeptides represent fragments of thymosin α1. Thus, I and II were prepared from their benzyl-protected derivatives by hydrogenolysis. I and II showed activity comparable to that of thymosin α1 in converting precursor T cells into steroid sensitive T1 cells or steroid resistant T2 cells. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).Application of 53838-27-0

The Article related to immunopotentiation thymosin peptide fragment, Amino Acids, Peptides, and Proteins: Poly(Amino Acids) and Peptides and other aspects.Application of 53838-27-0

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

On September 4, 2012, Degrado, William F.; Bennett, Joel S.; Snyder, Seth Elliott; Choi, Sungwook published a patent.Recommanded Product: (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate The title of the patent was Inhibitors of the α2β1/gpia-iia integrin. And the patent contained the following:

Novel compounds inhibiting the integrin α2β1/GPIa-IIa receptor are disclosed. Also disclosed are pharmaceutical compositions containing the compounds, as well as methods of their therapeutic use. The compounds disclosed are useful, inter alia, as inhibitors of integrin α2β1/GPIa-IIa-mediated activity. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).Recommanded Product: (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate

The Article related to prolyl peptide preparation inhibitor integrin, Amino Acids, Peptides, and Proteins: Poly(Amino Acids) and Peptides and other aspects.Recommanded Product: (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics