- Synthesis of the Tripeptides Tyr-Thr-Lys Phosphorylated with Isopropyl Methyl- and (Deuteromethyl)phosphonochloridates as Reference Standards for the Analysis of Biomedical Samples
-
A procedure for the phosphorylation of the tripeptide Tyr-Thr-Lys with isopropyl methyl- or (deuteromethyl)phosphonochloridate is developed. The phosphorylated tripeptides are intended for use as reference standards in the analysis of blood samples of people suspected to have been exposed to acetylcholinesterase inhibitors. Conditions of hromatographic separation and purification of the synthesized compounds are determined and optimized, which ensures the preparation of high-purity phosphorylated tripeptides.
- Rodin,Baygildiev,Krylov,Osipov,Krylov,Yashkir,Rybalchenko
-
p. 2103 - 2107
(2019/11/29)
-
- SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF
-
Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
- -
-
Page/Page column 63
(2018/03/09)
-
- OXABOROLE ESTERS AND USES THEREOF
-
The present invention provides oxaborole ester compounds and compositions thereof which are useful to treat diseases associated with parasites, such as Chagas Disease and African Animal Trypanosomosis.
- -
-
Page/Page column 66
(2017/12/05)
-
- SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF
-
Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed. Formula (I).
- -
-
Page/Page column 26; 32; 33
(2017/12/16)
-
- SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF
-
Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
- -
-
Paragraph 0101
(2014/08/19)
-
- SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF
-
Disclosed are compounds having enhanced potency in the modulation of NMD A receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
- -
-
Paragraph 0093
(2014/08/19)
-
- Fatty acid analogs and prodrugs
-
Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitrites thereof. These compounds are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, and as anti-viral and anti-fungal agents or pro-drugs of such agents. Illustrative of the disclosed compounds are fatty acid amino acid analogs of the structure STR1 in which x is the ethyl or t-butyl ester of an amino acid such as Gly, L-Ala, L-Ile, L-Phe, L-Trp, L-Thr or an amide such as NHCH2 C6 H5 or NH(CH2)2 C6 H5.
- -
-
-
- Selective detachment of Boc-protected amino acids and peptides from Merrifield, PAM and Wang resins by trimethyltin hydroxide
-
We describe the development of a new non-acidolytic and non- nucleophilic method for the selective cleavage by trimethyltin hydroxide of amino acids and dipeptides at benzyl ester links attached to resins commonly used in peptide synthesis.
- Furlan, Ricardo L. E.,Mata, Ernesto G.,Mascaretti, Oreste A.,Pena, Clara,Coba, Marcelo P.
-
p. 13023 - 13034
(2007/10/03)
-
- Fatty acid analogs and prodrugs
-
Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitriles thereof. These compounds are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, and as anti-viral and anti-fungal agents or pro-drugs of such agents. Illustrative of the disclosed compounds are fatty acid amino acid analogs of the structure STR1 in which X is the ethyl or t-butyl ester of an amino acid such as Gly, L--Ala, L--Ile, L--Phe, L--Trp, L--Thr or an amide such as NHCH2 C6 H5 or NH(CH2)2 C6 H5,
- -
-
-
- Stable polypeptides having c-AMP production enhancing activity and the use thereof
-
Disclosed are (1) a polypeptide represented by formula (I), or a pharmaceutically acceptable amide, ester or salt thereof: wherein X is hydrogen atom; or a lower alkyl group which may be substituted with a member selected from the group consisting of hydroxy group, substituted or unsubstituted amino group, carboxyl group, carbamoyl group, and substituted or unsubstituted aromatic group; and Y is one of amino acids or peptides consisting of 1 to 16 amino acid residues counted from the N-terminal side of Leu-Ala-Ala-Val-Leu-Gly-Lys-Arg-Tyr-Lys-Gln-Arg-Val-Lys-Asn-Lys SEQ ID NO: 20, and (2) a pharmaceutical composition comprising a polypeptide represented by formula (I), or a pharmaceutically acceptable amide, ester or salt thereof, which has remarkable c-AMP activity and is useful as a nerve activating agent.
- -
-
-
- Mild, selective cleavage of amino acid and peptide β-(trimethylsilyl)ethoxymethyl (SEM) esters by magnesium bromide
-
Magnesium bromide etherate has been previously shown to cleave β-(trimethylsilyl)ethoxymethyl (SEM) esters of aliphatic acids. This methodology has now been extended to amino acid and peptide derivatives in the presence of protecting groups typically encountered in peptide chemistry, including the Boc, Cbz, Fmoc and Troc carbamates as well as benzyl-, tert-butyl- and tert-butyldimethylsilyl ethers. The stability of fluoride sensitive protecting groups to magnesium bromide allows for added selectivity in the removal of SEM esters in organic synthesis.
- Chen, Wei-Chuan,Vera, Matthew D.,Joullie, Madeleine M.
-
p. 4025 - 4028
(2007/10/03)
-
- Dehydrooligopeptides. XVII. Practical syntheses of all of the diastereomers of N,N-protected 2,3-diaminobutanoic acids from L- and D-threonine derivatives
-
Syntheses of all of the dioctereomers of 2,3-diaminobutanoic acids, found in some pedtide antibiotics and toxins, were accomplished. The four isomers were derived mainly through two pathways including S(N)2 inversions of the β-substituent of L- or D-threonine derivatives. The various protecting groups and effective nucleophiles for the S(N)2 inversion were examined.
- Nakamura,Hirai,Tamotsu,Yonezawa,Shin
-
p. 1369 - 1377
(2007/10/02)
-
- HIV related peptides
-
Fragments of HIV p17 protein ranging in length from about 12 to abut 40 amino acids are used to form diagnostics and vaccines for detection or treatment of AIDS. Specific peptide fragments extend from the N-terminal to the C-terminal. Peptides having the amino acid sequences shown by the following formula (I), (II), (III), (IV) and (V):, Tyr-Ser-Val-His-Gln-Arg-Ile-Asp-Val-Lys--Asp-Thr-Lys-Glu-Ala-Leu-Gly-Lys-Ile-Glu--Glu-Glu-Gln-Asn-Lys-Ser-Lys-Lys-Lys-Ala (I), Gly-Ala-Arg-Ala-Ser-Val-Leu-Ser-Gly-Gly--Glu-Leu-Asp-Arg-Trp-Glu-Lys-Ile-Arg-Leu--Arg-Pro-Gly-Gly-Lys-Lys-Lys-Tyr-Lys-Leu--Lys-His (II), Ile-Val-Trp-Ala-Ser-Arg-Glu-Leu-Glu-Arg--Phe-Ala-Val-Asn-Pro-Gly-Leu-Leu (III), Glu-Thr-Ser-Glu-Gly-Cys-Arg-Gln-Ile-Leu--Gly-Gln-Leu-Gln-Pro-Ser-Leu-Gln-Thr-Gly--Ser-Glu-Glu-Leu-Arg-Ser-Leu-Tyr-Asn-Thr--Val-Ala-Thr-Leu (IV), Ala-Gln-Gln-Ala-Ala-Ala-Asp-Thr-Gly-His--Ser-Ser-Gln-Val-Ser-Gln-Asn-Tyr (V), are immunoreactive to antibodies in sera of patients testing seropositive for p17 of HIV-1.
- -
-
-
- 3,5-substituted 4,5-dihydroisoxazoles as transglutaminase inhibitors
-
The present invention is directed to certain 3,5 substituted, 4,5-dihydroisoxazoles, and methods for their use. These compounds are transgulatminase inhibitors, and are particularly effective in the inhibition of epidermal transglutaminase and the treatment of acne.
- -
-
-
- Antigen determinant peptides and a process for the preparation thereof
-
Antigen determinant peptides of the general formula I, H - Val - X - Y (I), in which X represents an octapeptidic to undecapeptidic sequence of a defined structure, Tyr-Tyr-Arg-Asp-Ser-Arg-Asn-Pro-Leu,Phe-Ile-His-Asn-Phe-Lys-Arg-Lys-Gly,Val-Pro-Arg-Arg-Lys-Ala-Lys-Ile,Leu-His-Thr-Gly-Glu-Arg-Asp-Trp-His-Leu-Gly,Ser-Gly-Lys-Ala-Arg-Gly-Trp-Phe, or Ser-Ile-Glu-Trp-Arg-Lys-Lys-Arg-Tyr-Ser, and Y stands for a hydroxyl or an amino group,available by fragment synthesis or successive condensation of the respective amino acid residues (stepwise build-up) in solution or on a solid carrier, are expected to be of use as diagnostic agents for the so-called acquired immunodeficiency syndrome (AIDS), and also to have a potential as monodeterminant antibodies and safe synthetic vaccine agents combating the human T-cell lymphotropic type III virus (HTLV-III, HIV).
- -
-
-
- Alkyl 1-Chloroalkyl Carbonates: Reagents for the Synthesis of Carbamates and Protection of Amino Groups
-
The synthesis of 1-chloroalkyl carbonates and their reaction with various type of amines are described.This reaction is useful for the synthesis of carbamate pesticides and for the protection of various amino groups, including amino acids.
- Barcelo, Gerard,Senet, Jean-Pierre,Sennyey, Gerard,Bensoam, Jean,Loffet, Albert
-
p. 627 - 632
(2007/10/02)
-
- Peptides related to somatostatin
-
Peptides of the formula: STR1 wherein: X is H, --NH2, --NH--Gly--Ala, --NH--D--Ala--Ala, --NH--Gly--Gly--Gly, --NH--acetyl, or --NH--benzoyl; X1 is His or Arg; X2 is His, Glu, Tyr, Trp, or Phe; X3 is Trp, D-Trp, or 6-F-D-Trp; and X4 is a D-α-amino acid; or the reduced, linear form thereof, or a non-toxic, pharmaceutically acceptable acid addition salt thereof; inhibit the release of growth hormone, insulin, and glucagon; and show prolonged inhibition activity. Said peptides are prepared by solid-state methodology.
- -
-
-
- Polypeptides related to somatostatin
-
Compounds of the formula: STR1 wherein: X is H, Ala-Gly, Gly-Gly-Gly, Ala-D-Ala, acetyl, or benzoyl; X1 is Arg or His; X2 is Glu or Asp; X3 is Trp or D-Trp; or 6-F-D-Trp; and X4 is Cys- or D-Cys; or a non-toxic pharmaceutically acceptable acid addition salt thereof; inhibit the secretion of growth hormone and glucagon without materially affecting the secretion of insulin.
- -
-
-
- Peptides related to somatostatin
-
The tetradecapaptides of the formula STR1 wherein X is H-Ala-D-Ala, H-D-Ala-Gly, or H-D-Val-Gly, or the non-toxic, pharmaceutically acceptable acid addition salts thereof; inhibit the secretion of growth hormone, while not materially inhibiting the secretion of insulin or glucagon. Intermediates used in the synthesis of the tetradecapeptides are also described.
- -
-
-
- Peptides related to somatostatin
-
Tetradecapeptides of the formula STR1 wherein X is H-Ala-D-Ala, H-D-Ala-Gly, or H-D-Val-Gly, and X1 is Phe or Cha, or a non-toxic pharmaceutically acceptable acid addition salt thereof, inhibit the secretion of growth hormone without materially inhibiting the secretion of glucagon or insulin. Intermediates and processes for making the tetradecapeptides are also described.
- -
-
-
- Peptides related to somatostatin
-
The tetradecapeptides of the formula STR1 wherein X is H--Ala--D--Ala, H--D--Ala--Gly, or H--D--Val--Gly; and X is Ala--Leu, Ala--Phe, Ala--D--Phe, D--Ala--Phe, or D--Ala--Cha; or the non-toxic, pharmaceutically acceptable acid addition salts thereof; inhibit secretion of growth hormone, while not materially inhibiting the secretion of insulin or glucagon. Intermediates used in the synthesis of the tetradecapeptides are also described.
- -
-
-