СПОСОБ ПОЛУЧЕНИЯ АЦЕТИЛАМИДИНИОФЕНИЛАЛАНИЛЦИКЛОГЕКСИЛГЛИЦИЛПИРИДИНИОАЛАНИНАМИДОВ

Изобретение относится к способу получения ацетиламидиниофенилаланилциклогексилглицилпиридинио-аланинамидов формулы (I), в которой анионы Х являются физиологически приемлемыми анионами, и их аналогов, которые являются эффективными ингибиторами фактора Ха свертывания крови и которые могут быть использованы, например, для предотвращения тромбозов. Способ согласно изобретению включает сочетание 2-[2-ацетиламино-3-(4-амидинофенил)-пропиониламино]-2-циклогексилуксусной кислоты, которую получают из 2-[2-ацетил-амино-3-(4-цианофенил)акрилоиламино]-2- циклогексилуксусной кислоты путем асимметрического гидрирования и превращения цианогруппы в амидин, или ее соли, с 3-(2-амино-2-карбамоилэтил)-1-метилпиридиниевой солью, или ее солью. Кроме того, изобретение относится к исходным материалам и промежуточным продуктам для этого способа, способам их получения и ацетил-(S)-4-амидиниофенилаланил-(S)-циклогексилглицил-(S)-(1-метил-3-пиридинио)аланинамид в виде дитозилата. Технический результат: упрощение ...

Ингибиторы фактора VIIa

Изобретение относится к группе новых соединений общей формулы I R1-A-B-D-En-R2 (I), в которой R1 представляет собой R12C(O), причем R12 выбран из группы, включающей алкенил, алкенилокси или алкениламино; А представляет собой группу А1-А2-А3, в которой A1 представляет собой NH, А2 представляет собой CHR93, в которой R93 представляет 4-амидинофенилметил; A3 представляет собой C(O); В представляет собой группу В1-В2-В3, в которой B1 представляет собой NH; B2 представляет собой CHR97, где R97 представляет этил, который замещен в положении 2 гидроксикарбонилом или алкилоксикарбонилом; В3 представляет собой C(O); D представляет группу D1-D2-D3, в которой D1 представляет собой NH, D2 представляет собой CR81R82, в которой R81 и R82 независимо выбраны из группы, состоящей из водорода и незамещенных или замещенных остатков алкила, арила, арилалкила, гетероарилалкила; D3 представляет собой С(О); Enпредставляет собой (E1-Е2-Е3)n, в которой n равно 0 или 1; E1 представляет NR70, где R70 представляет ...

ПРОИЗВОДНЫЕ ГЛИЦИНА ИЛИ ИХ ФИЗИОЛОГИЧЕСКИ ПРИЕМЛЕМЫЕ СОЛИ, ОБЛАДАЮЩИЕ СПОСОБНОСТЬЮ ТОРМОЗИТЬ СВЯЗЫВАНИЕ ФИБРИНОГЕНА У ФИБРИНОГЕННОГО РЕЦЕПТОРА ТРОМБОЦИТОВ

Назначение: в биохимии и медицинской химии благодаря способности тормозить связывание фибриногенного рецептора. Сущность изобретения: производные глицина общей формулы 1: R-CONH-CH2CONHCH(R′)CH2COOH , где R-группа формулы -CH(NHRa)-(CH2)1-6NH-Rb (R - 1) (T)m-C6H4·CH2NH2 (R - 2) (T)m-C6H4(NH)nC(NH)-L (R - 3) или n = 0 или , Ra -водород, -COOC1-C4 -алкил, Z, -COC5H4N3 , -SO2 -нафтил или -COCH2H(Y)CH2CH2NH-Y y-водород, Вос или Z, Rb -группа формулы -C(NH)(CH2)0-3CH3 или или же, если Ra -группа формулы -COC6H4N3, -SO2 -нафтил или -COCH2N(Y)CH2CH2NHY , то Rb -аминогруппа, где n - число 1 или 0, L-аминогруппа или же, если n - 1, то L - также -(CH2)0-3-CH3 Т - группа формулы -CH2-(O)n, n = 1 или, -CH(Rd)-CH2 или -CH2CO- , причем одна из содержащихся в Т-группе карбонильных групп может существовать в виде кеталя Rd -водород или NHRa или R′=H или COR0, R0- -NH0C1-4 алкил -NH(CH2)1-4-C0 H4Hal, -NHC0H4COOH или радикал, связанный через аминогруппу α -аминокарбоновой кислоты или их физиологически приемлемые ...

ПСЕВДОПЕПТИДЫ ИЛИ ИХ СОЛИ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ

Использование: в медицине для профилактики и лечения тромбоза. Сущность изобретения: псевдопептиды или их соли формулы I: A - NH - (CH2)m - x - y - CH (CH2 - R1) NHB, где R1 : COON, COOL1 , X = CH2- или R1 и X вместе - >CH - O - CO; y = -/CH2/m-, m = 1 или 2, A = -CO-/CH2/p - C6H4 - C 1 = NH1 NH2, где p = 0 или 1; B = -CO - /CH2/q - R3, где q = 1 или 2; R3 = /C1 - C4/ алкил, 1-адамантил, /C1 - C4/ алкоксифенил или B = -SO2 - (CH2)r - R4, где r = 0,1 или 2, R4 = n - /C1 - C4/ алкоксифенил; 2 способа получения соединений I; фармацевтическая композиция, содержащая в качестве активного ингредиента псевдопептид формулы I или его соль в эффективном количестве. 4 н.пункта, 4 з, пункта формулы. 2 с. и 6 з.п. ф-лы, 2 табл.

СРЕДСТВО ДЛЯ КОРРЕКЦИИ МЕТАБОЛИЧЕСКОГО СИНДРОМА

Изобретение относится к медицине, а именно к пептидам, которые могут найти применение для коррекции метаболического синдрома. Предложено средство для коррекции метаболического синдрома, представляющее собой трипептид L-лизил-L-глутамил-L-триптофан. 3 ил., 3 табл., 4 пр.

КОМПОЗИЦИЯ ИЗ ПЕПТИДОВ, ОБЛАДАЮЩАЯ ИММУНОРЕГУЛЯТОРНЫМ СВОЙСТВОМ

... 1. Композиция, обладающая иммунорегуляторным свойством, включающая по крайней мере два пептида формулы Arg-Gly-Asp и Н-Tyr-X-Y-Glu-OH, где Х-Gln и/или Glu, Y-Cys(acm) и/или Cys. 2. Композиция по п.1, отличающаяся тем, что пептиды взяты в долях, соотношение которых составляет 1:4 соответственно. 3. Композиция по п.1, отличающаяся тем, что пептиды взяты в равных долях.

RGD-содержащие пептиды

... 1. Пептиды общей формулы R3-Arg-Gly-Asp(OR1)-OR2, где R1 есть бензил или трет-бутил; R2 не равен R1 и выбирается из группы: трет-бутил; бензил; 4-метоксибензил; 4-нитробензил; дифенилметил; 2,2,2-трихлорэтил; 2,2,2-трихлор-1,1-диметилэтил; аллил; 9-флуоренилметил; карбоксамидометил; замещенный 2-сульфонилэтил вида A-SO2 -CH2-CH2-, где А представляет собой замещенный либо незамещенный фенил или бензил; R3 представляет собой атом водорода, либо уретановую защитную группу вида В1O-СО-, где В1 не равен R1 и может принимать значения: трет-бутил, бензил, 4-метоксибензил, 9-флуоренилметил, 2-(4-нитрофенил-сульфонил)этил; либо представляет собой пептидил, содержащий от одного до трех аминокислотных остатков. 2. Пептиды по п.1, где R3 представляет собой пептидил структуры E-Z-Y-X-, в котором Е есть атом водорода либо уретановая защитная группа вида В2O-СО-, где В2 не равен R1 и может принимать значения: трет-бутил; бензил; 4-метоксибензил; 9-флуоренилметил; 2-(4-нитрофенилсульфонил)этил; Х отсутствует ...

ПЕПТИД И СПОСОБ ЕГО ПОЛУЧЕНИЯ

Изобретение относится к медицине, а именно - к способам получения биологически активных веществ, обладающих иммуннорегулирующими свойствами, и может найти применение в медицине, ветеринарии, а также в экспериментальной биохимии. В основу изобретения положена задача создания нового синтетического биологически активного пептида, обладающего иммуннорегулирующими свойствами. Синтез пептида производится в растворе путем последовательного наращивания цепи с С-конца молекул, используя стратегию максимального блокирования функциональных групп, исходя из алкилового эфира аминокислоты с помощью метода активированных эфиров и метода смешанных ангидридов, используя третбутилоксикарбониламинокислоты.

ТРИПЕПТИДЫ

МЕДИАТОРЫ ОБРАТНОГО ТРАНСОРТА ХОЛЕСТЕРИНА ДЛЯ ЛЕЧЕНИЯ ГИПЕРХОЛЕСТЕРИНЕМИИ

... 1. Медиатор обратного транспорта холестерина, включающий молекулу, содержащую кислотный участок, липофильный или ароматический участок и основной участок, указанная молекула имеет структуру, способную образовывать комплексы с липопротеинами высокой плотности (ЛВП) и/или липопротеинами низкой плотности (ЛНП) и таким образом улучшает обратный транспорт холестерина. 2. Медиатор обратного транспорта холестерина по Пункту 1, где указанная молекула содержит от 3 до 10 аминокислотных остатков или их аналогов и содержит последовательность: Х1-Х2-Х3, где: X1 представляет собой аминокислоту с кислотной группой; Х2 представляет собой ароматическую или липофильную аминокислоту; ХЗ представляет аминокислоту с основной группой; и где X1, Х2, Х3 могут быть размещены в любом последовательном порядке; где амино терминальная группа включает первую защитную группу, выбранную из группы, состоящей из ацетила, фенилацетила, пиволила, 9-флуоренилметилоксикарбонила, 2-нафталиновой кислоты, никотиновой кислоты, ...

HIV-1- UND HIV-2-PEPTIDE ZUR INHIBITION VON MIT MEMBRANFUSIONEN IN ZUSAMMENHANG STEHENDEN PHÄNOMENEN, EINSCHLIESSLICH DER ÜBERTRAGUNG VON HIV

HEMMSTOFFE FÜR KATHEPSIN-G UND ELASTASE ZUR VERHÜTUNG VON BINDEGEWEBSABBAU

GLU-TRP ENTHALTENDE TRIPEPTIDE

Zyklische Peptide mit aggregationshemmenden Eigenschaften

POSSIBLY PROTECTED PEPTIDES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL AGENTS CONTAINING THEM

N-isobornyloxycarbonyl amino acids

N-Isobornyloxycarbonyl aminoacids and their derivs., are prepd. by reacting the aminoacid with isobornylcarbonyl chloride or an activated ester. The protecting isobornylcarbonyl chloride or an activated ester. The protecting gp. with attached to one or more of the NH2 or NH gps. is a molecule and to 2 of the 3 nitrogens in a guanidine residue. The cpds. are easily prepd., stable towards hydrogenation, and easily removed with HCl or CF3CO2H. They are useful intermediates in peptide and antibiotic synthesis.

PEPTIDES

N3-D-trans-2,3-Epoxysuccinamoyl-L-2,3-diaminopropanoic acid compositions

Chemical Compounds

A compound of formula (I) or a pharmaceutically acceptable salt, ester or pro-drug thereof: wherein R1 is a substituent; R2 and R5 are hydrogen or alkyl; R3 and R4 are hydrogen or a substituent, or, taken together with the atoms to which they are attached, R1 and R2 or R1 and R3 form a heterocyclyl ring; R6 and R7 are hydrogen or a substituent, or, taken together with the carbon atom to which they are attached, R6 and R7 form a cycloalkyl or heterocyclyl ring; W represents (Aaa)n, wherein each Aaa is an independently selected amino acid; n is an integer of from 1 to 20. These compounds are inhibitors of rhomboid intramembrane proteases based on peptidyl ketoamides. The compounds, and pharmaceutical compositions containing them, can be used for the use in the treatment of e.g. malaria, Parkinsons disease, cancer, diabetes and bacterial infections.

Inhibitors of Rhomboid Intramembrane Proteases

The invention comprises compounds of the general formula H2N-R-CO-Y1 where R is an aminomethyl - methylene, aminoethyl-methylene, aminopropyl - methylene, aminobutyl - methylene or (3 - guanidino propyl)-methylene group and Y1 is a hydroxy or alkoxy group; one of the amino groups or the guanidino group being substituted by a saturated or unsaturated aliphatic long-chain acyl group containing at least ten carbon atoms and the other amino or guanidino group being protected with a removable protecting group. The compounds are prepared by acylating the corresponding N-protected amino acid or ester with an agent which introduces a saturated or unsaturated aliphatic long chain acyl group on to the unprotected amino group and, if desired esterifying any free acid or de-esterifying any ester obtained. Ne -Phthaloyl-L-lysine ethyl ester hydrochloride is prepared from the free acid by reaction with ethanol and hydrochloric acid.

Process for the preparation of resin-bound cyclic peptides

Process for the preparation of resin-bound cyclic peptides.

This invention is directed to a process for the solid phase, fragment-based sythesis of resin bound cyclic peptide analogs of parathyroid hormones and analogs of parathyroid hormone-related proteins, which analogs contain at least one bridge between the side chains of two non-adjacent amino acid residues, and to peptide fragments useful therefor.

Process for the preparation of resin-bound cyclic peptides

Cocoa Flavour Precursor Peptides

The present invention pertains to peptides derived from fermented cocoa beans and representing cocoa and/or chocolate flavour precursor peptides from fermented cocoa beans and to the preparation of cocoa/chocolate flavour on a synthesic basis, and to the use threof in the preparation of chocolate.

Thioacylating reagents and intermediates thiopeptides and methods for preparing and using same

New peptide derivatives with nitrogenized polyclic structure, their method of preparation and the compositions pharmaceutical which contain them.

New tripeptides with nitrogenized polycyclic structure, their method of preparation and the compositions pharmaceutical which contain them.

New polypeptide and its preparation.

Process for the preparation of resin-bound cyclic peptides.

Cocoa flavour precursor peptides.

Process for the preparation of resin-bound cyclic peptides

Cocoa flavour precursor peptides.

COMPLEMENTARY, SYNTHETIC PEPTIDE AND YOUR USE IN THE OPHTHALMOLOGIE

ENTZÜNDUNGSCHEMMENDE CONNECTIONS

PROCEDURE FOR THE PRODUCTION OF NEW PEPTIDEN

BIOLOGICALLY ACTIVE PEPTIDE AND THEIR USE FOR THE REPAIR OF INJURED NERVES

TAR RNA BINDING PEPTIDE

TRANSFEKTIONSKOMPLEXE

TRANSFEKTIONS COMPLEXES

ANTI-TUMOR AMINO ACIDS AND PEPTID DERIVATIVES OF 1,4-BIS ((AMINOALKYL AND HYDROXYAMINOALKYL) AMINO>5,8 DIHYDROXYANTHRAQUINONEN.

HIGHLY PURE CRYSTALLINE ONES FORMS OF THE PEPTIDE BAD LYS ASP AND BAD LYS ASP VAL, PROCEDURE FOR YOUR PRODUCTION AND IT ABSTENTION PHARMACEUTICAL COMPOSITIONS

VERFAHREN ZUR HERSTELLUNG EINES NEUEN TRIPEPTIDS MIT IMMUNMODULIERENDER WIRKUNG

2,3-DISUBSTITUIERTE ISOXAZOLIDINE, PROCEDURES FOR YOUR PRODUCTION, THESE CONTAINING MEANS AND YOUR USE.

15-DEOXYSPERGUALINANALOGE CONNECTIONS, PROCEDURES FOR YOUR PRODUCTION AND YOUR USE IN the THERAPY

CARRIER TRIPEPTID WITH ANTIFUNGI EFFECTIVENESS.

THIOACYLIERUNGSMITTEL AND INTERMEDIATE PRODUCTS, THIOPEPTIDE, AND PROCEDURES FOR THEIR PRODUCTION AND APPLICATION

SULFONE AMIDE INHIBITORS OF THE INTERLEUKIN-1-BETA OF CONVERTING ENZYME

WITH ALZHEIMER'S PROCEDURES FOR THE DIAGNOSIS, FOR THE PRODUCTION OF MEDICINES AND FOR THE SCREENEN OF SUBSTANCES AS WELL AS FROM BETA AMYLOID DERIVED PEPTIDEN LINKED ILLNESS

PEPTIDDERIVATE OF THE BLOOD PANEL AGGREGATION INHIBITOR.

METALLCHELATE SCREEN END OF PEPTIDE AND YOUR USE

FACTOR XA INHIBITORS

SYNTHETIC PEPTIDINHIBITOREN OF THE HIV TRANSMISSION

PEPTIDKONJUGATE, THEIR USE AS CURES AND COMPOSITIONS, THIS CONTAINING

TECHNETIUM-99M MARKED PEPTIDE FOR THE IMAGING OF THROMBUS

COMPLEMENTARY, SYNTHETIC PEPTIDE AND YOUR USE IN THE OPHTHALMOLOGIE

COMPLEMENTARY, SYNTHETIC PEPTIDE AND YOUR USE IN THE OPHTHALMOLOGIE

COMPLEMENTARY, SYNTHETIC PEPTIDE AND YOUR USE IN THE OPHTHALMOLOGIE

COMPLEMENTARY, SYNTHETIC PEPTIDE AND YOUR USE IN THE OPHTHALMOLOGIE

COMPLEMENTARY, SYNTHETIC PEPTIDE AND YOUR USE IN THE OPHTHALMOLOGIE

COMPLEMENTARY, SYNTHETIC PEPTIDE AND YOUR USE IN THE OPHTHALMOLOGIE

COMPLEMENTARY, SYNTHETIC PEPTIDE AND YOUR USE IN THE OPHTHALMOLOGIE

C-terminal KPV dimers and methods of use

Collections of traceable compounds and uses thereof

PEPTIDES

NOVEL PEPTIDE DERIVATIVES

Polypeptides derived from amyloid precursor peptide (app) and their uses

TF BINDING COMPOUND

A tissue factor binding immunoconjugate comprising factor viia

Compounds useful in the treatment and/or care of the skin and their cosmetic or pharmaceutical compositions

Compounds of general formula (I): their stereoisomers, mixtures thereof and/or their cosmetically or pharmaceutically acceptable salts, cosmetic and/or pharmaceutical compositions which contain them and their use in medicine, and in the treatment and/or care of the skin, particularly in the aging and photoaging of the skin, and more particularly for the treatment and/or prevention of wrinkles and/or stretch marks.

New peptide derivatives with delta opioid receptor antagonist or mixed mu agonist/delta antagonist effects

Treatment for atherosclerosis and other cardiovascular and inflammatory diseases

ORGANOSULPHUR COMPOUNDS USEFUL FOR THE TREATMENT OF GLAUCOMA

NEW PEPTIDE DERIVATIVES HAVING A POLYCYCLIC NITROGENOUS STRUCTURE, PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

Cs-1 peptidomimetics, compositions and methods of using the same

Liquid phase peptide syntheses of kl-4 pulmonary surfactant

OLIGOPEPTIDES CONTAINING M-%D1-%2-CHLORETHYL<AMINOL-L- PHENYLALANINE

Antimicrobial amino acid sequences derived from alpha-melanocyte-stimulating hormone

Peptide analogues containing a 7-membered lactam ring

New pseudopeptides having an antiviral action

TRIPEPTIDES AND METHOD

SYNTHETIC PEPTIDE ANALOGS OF ARG-PRO-PRO-GLY-PHE AS SELECTIVE INHIBITORS OF THROMBIN AND THROMBIN ACTIVATION OF PROTEASE ACTIVATED RECEPTORS 1 AND 4

The invention relates to compounds and methods for inhibiting human platelet aggregation, thrombosis and cell activation mediated by PAR1 and PAR4 using peptide analogs of Arg-Pro-Pro-Gly-Phe that contain one or more amino acid substitutions. The invention also includes screening methods for identifying compounds that inhibit thrombin mediated activities.

HEPATITIS C INHIBITING COMPOUNDS

Compounds of formula (I) wherein B, X, R3, R21,R22, R1 and Rcare defined herein. The compounds are useful as inhibitors of HCV NS3 protease.

ANTIMICROBIAL COMPOUNDS AND FORMULATIONS

... ²²²The invention relates to the use of a molecule comprising a backbone of 2 to ²35 non-hydrogen atoms in length, having covalently attached thereto at least ²two bulky and lipophilic groups and having at least one more cationic than ²anionic moiety, in the manufacture of a medicament for destabilising microbial ²cell membranes and the use as a membrane acting antimicrobial agent of a ²molecule comprising a backbone of 2 to 35 non-hydrogen atoms in length, having ²covalently attached thereto a super bulky and lipophilic group comprising at ²least 9 non-hydrogen atoms and having at least two more cationic than anionic ²moieties and to methods of treatment involving such molecules, in particular ²peptides including peptide derivatives, and peptidomimetics.² ...

TREATMENT OF BIOFILMS

The present invention relates to a peptide or peptidomimetic for use in the treatment of a biofilm-associated infection in a subject, wherein said peptide or peptidomimetic a) carries a net positive charge,- b) is 1 to 6 amino acids in length or is an equivalently sized peptidomimetic; and c) is amphipathic in nature, having one or more lipophilic groups, one of said lipophilic groups comprising at least 7 non-hydrogen atoms.

PEPTIDE DERIVATIVES AND PROCESSES FOR THEIR PREPARATION

Peptide ester and amide derivatives of the general formula I: (I) in which X is H or an acyl, A and B are structurally defined amino acid residues, n is an integer of from 1 to 3, Rl is H or a lower alkyl and either R2 or C is a defined optionally modified amino acid residue and the other is a lower alkoxyl, an amino group or a direct chemical bond, are converted under physiologic conditions, by enzymic hydrolysis in pathologically altered tissues and subsequent spontaneous cyclization, into pharmacodynamically active spirocyclic peptide derivatives of the general formula III, (III) in which R3 and R4 are H atoms, optionally substituted alkyl groups or jointly an aliphatic chain forming preferably a 2,5-piperazinedione ring, and hence can act as pro-farmaca (drug precursors) of prolonged biological effect. A process for the production of these derivatives is also disclosed.

TRIPEPTIDES AND METHOD

ORTH 326 NEW TRIPEPTIDES AND METHODS There are disclosed new biological active polypeptides: A-X-B wherein A is deamino-LYS or LYS; X is a suitable neutral aliphatic amino acid residue; e.g., one selected from the group consisting of SER, ALA, 2-Me-ALA, GLY, LEU, THR, D-SER, D-ALA, D-THR, allo-THR, D-LEU, and SAR; B is GLN-R', decarboxy-GLN, or ; and R' is a substituent which does not substantially affect the biological activity of the tripeptide. These polypeptides have the capability of inducing the differentiation of T-lymphocytes as measured by the acquisition of the thymic differentiation antigen Th-l, as well as B-lymphocytes as measured by the acquisition of the differentiation antigen Bu-l. The polypeptides are thus useful in thymic function and immunity areas such as in treatment for congenital absence of thymus. Also provided are therapeutic compositions and methods for use of the polypeptides.

PEPTIDES RENFERMENT UN GROUPE ACIDE (ALPHA)-AMINOBORIQUE

AMINO THIOL PEPTIDES

NOVEL PEPTIDES FOR TREATING AND PREVENTING IMMUNE-RELATED DISORDERS, INCLUDING TREATING AND PREVENTING INFECTION BY MODULATING INNATE IMMUNITY

In one aspect, the present invention provides isolated novel peptides tha t can be used to modulate innate immunity in a subject and/or for the treatm ent of an immune- related disorder, including treating and preventing infect ion by modulating innate immunity. Also provided are an agent reactive with the peptide, a pharmaceutical composition that includes the peptide, an isol ated nucleic acid molecule encoding the peptide, a recombinant nucleic acid construct that includes the nucleic acid molecule, at least one host cell co mprising the recombinant nucleic acid construct, and a method of producing t he peptide using the host cell. The present invention further provides a met hod for treating and/or preventing infection in a subject by administering t he peptide of the invention to the subject, thereby modulating innate immuni ty in the subject. Additionally, the present invention provides a method for predicting whether a subject would be responsive to treatment with a peptid e of the ...

STABILITY-MODULATING LINKERS FOR USE WITH ANTIBODY DRUG CONJUGATES

The present invention provides stability-modulated antibody-drug conjugates, stability-modulating linker components used to make these stability-modulated antibody-drug conjugates, and methods of making stability modulating linkers and stability-modulated antibody-drug conjugates.

NANOTUBES AND COMPOSITIONS THEREOF

The present invention is directed to implants and the modification of the surface of implants using amino acid or polypeptide functionalized rosette nanotubes.

PEPTIDES INHIBITING THE MATURATION OF T-LYMPHOCYTES AND THE ACTIVITY OF MACROPHAGES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARING SAME

NOVEL PEPTIDES INHIBITING THE MATURATION OF T-LYMPHOCYTES AND THE ACTIVITY OF MACROPHAGES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARING SAME A b s t r a c t The invention relates to novel peptides and their acid addition salts inhibiting the maturation of T-lymphocytes and the activity of macrophages, pharmaceutical compositions containing these peptides as well as to a process for preparing these peptides and compositions. The novel peptides are represented by formulae (1) to (20): Arg-Lys(Chc)-Asp-Val (1) Arg-Lys(Chc)-Asp (2) Arg-Sar-Asp-Val (3) Arg-Sar-Asp (4) Orn-Lys-Asp-Val (5) Orn-Lys-Asp (6) Arg-Lys-Aad-Val (7) Arg-lys-Aad (8) ¢Arg-Lys-Asp-NH-CH2-!2 (9) (10) ¢Arg-Lys-Asp-Val-NH-CH2-!2 (11) ¢Arg-lys-Asp-?ys-NH2!2 (12) Iys-Ser-lys-leu (13) Ser-lys-leu (14) Ser-Ser-Ser-Thr (15) Iys-Glu-Thr (16) Iys-Thr-Glu-Thr (17) Pro-lys-leu-Thr (18) Iys-lys-Thr-Glu (19) Iys-His-leu-NH2 (20). The novel peptides are useful for the therapy of diseases, where a general suppressing ...

15-DEOXYSPERGUALIN ANALOGS, THEIR METHOD OF PREPARATION AND THEIR USE IN THERAPEUTICS

The present invention relates to a novel compound selected from the group consisting of: (i) the compounds of the formula in which: A is a group -CO-NH- or a group -NH-CO-, R is a hydrogen atom or a methyl group, and *C, if R is not the hydrogen atom, is an asymmetric carbon of (R,S) or (R) configuration; and (ii) their addition salts. It further relates to the method of preparing this compound and to its use in therapeutics.

NOVEL TRIPEPTIDES USEFUL IN IMMUNE AND CNS THERAPY

Tripeptides capable of regulating the function of cells of the mammalian immune and/or central nervous system, pharmaceutical compositions containing the peptides and methods of use thereof are provided.

SYNTHETIC PEPTIDE INHIBITORS OF HIV TRANSMISSION

The present invention relates to peptides which exhibit potent anti-retroviral activity. The peptides of the invention comprise DP-178 (SEQ ID:1) peptide corresponding to amino acids 638 to 673 of the HIV-1LaI gp41 protein, and fragments analogs and hamologs of DP-178. The invention further relates to the uses of such peptides as inhibitory of human and non-human retroviral, especially HIV, transmission to uninfected cells.

USE OF A LEAST ONE PEPTIDE IN A COSMETIC COMPOSITION OR FOR THE PREPARATION OF A DRUG

L'invention concerne l'utilisation à titre de principe actif, dans un milieu physiologiquement acceptable, dans une composition cosmétique ou pour la préparation d'un médicament, d'une quantité efficace d'au moins un peptide contenant le tripeptide Lysine-Proline-Valine, ou de tout équivalent biologique fonctionnel, dans lequel le résidu Proline est sous la forme de son isomère optique dextrogyre, destinée à traiter l'inflammation. L'invention concerne également un procédé de traitement cosmétique.

PEPTIDE AND A METHOD OF OBTAINING IT

The invention relates to medicine, specifically, to methods of obtaining biologically active substances with immuno-regulating properties, and can be used in medicine and veterinary science and in experimental biochemistry. The fundamental problem addressed by the invention is that of producing a novel synthetic biologically active peptide with immuno-regulating properties and of the formula: X-Glu-Trp-Y, in which X is H or Gly, Ala, Leu, Ile, Val, NVal, Pro, Tyr, Phe, Trp, D-Ala, D-Leu, D-Ile, D-Val, D-NVal, D-Pro, D-Tyr, D-Phe, DTrp, .gamma.-aminobutyric acid, -aminocaproic acid; Y is Gly, Ala, Leu, Ile, Val, NVal, Pro, Tyr, Phe, Trp, D-Ala, D-Leu, D-Ile, D-Val, D-NVal, D-Pro, DTyr, D-Phe, D-Trp, .gamma.-aminobutyric acid, - aminocaproic acid, -OH, monoor di-substituted amide (C1-C3). Peptide synthesis takes place in a solution by successive growth of a chain from the C termination of the molecules, using a strategy of maximum blocking of functional groups, starting from amino acid alkyl ...

3-AMINO-2-OXO-1-PIPERIDINEACETIC DERIVATIVES AS ENZYME INHIBITORS

The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.