Creighton University

Innofinance Altalanos Innovacios Penzintezet

Richter Gedeon Vegyeszeti Gyar Rt

Reanal Finomvegyszergyar

Kozponti Valto- Es Hitelbank Rt. Innovacios Alap

Solvo Biotechnology

Mta Kutatas-Es Szervezetelemzo Intezete

Biosignal Kutato-Fejlesztokft

Innovacios Alap Kozponti Valto Es Hitelbank Rt.

Richter Gedeon Veyteszeti Gyar R.t.

Innofinance Altalanos Innovacios Pengintezet

Istvan Teplan

Janos Seprodi

Aniko Horvath

Imre Mezo

Zsolt Vadasz

Tamas Gulyas

Balazs Szoke

Karoly Nikolics

Borbala Vincze

Istvan Palyi

Judit Erchegyi

Sandor Lovas

Geza Toth

Sandor Vigh

Magdolna Kovacs

Judit Horvath

Orsolya Csuka

Adrienn Kalnay

Istvan Schon

Tamas Szirtes

Gyorgi Keri

Gabor Makara

Ferenc Antoni

J Michael Conlon

Bela Kanyicska

Imre Mezom

Peter Peczely

Tibor Muray

Istvan Gyorvari

Eszter Kovats

Csaba Banhazi

Zoltan Graf

Bokonyi Istvane

Judit Rchegyi

Andras Szell

Richard F Murphy

Dezso Gaal

Gyongyi Bokonyi

Miklos Idei

Balas Szoke

Agnes Balogh

Gizella Turi

Melinda Mora

Gyorgy Rappay

Edit Hegedus

Maria Magocsi

Andras Selmezci

Olga N Nee Kuprina

The present invention provides peptides and pharmacologically active compounds including gonadotropin-releasing hormone (GnRH) analogues according to formulas of the invention, wherein the compounds show an antitumor effect. The invention additionally provides compositions including these peptides and compounds.

GnRH analogues with antitumour effects and pharmaceutical compositions thereof

The invention features novel peptide derivatives called Reversins, and provides for their use in a method of reducing the activity of the multi-drug transporter protein MDR1 in order to overcome multidrug resistance in a mammal. The peptide derivatives are of the formula (I) X,-X,-X,(X,),-X,, wherein n is 0 or 1, and each n is the same or different; X,is BOC, BOC-Asu, Z-Asu, benzyloxycarbonyl, Glu(OBzl)-OBzl, Trp-OMe, Trp-Phe-OMe, Phe-Trp-OMe, Phe-Phe-OtBu, Trp-Trp-OtBu, indoloacetyl, benzoyl, an alkylanine of 1-4 carbons, dibenzylamide, tryptamide, 1-amino-adamantine, aminomethylcyclohexane, indoline, phenylethylamide or dicyclohexylamide; X,is Glu(OBzl), Asp(OBzl), succinyl, O,O-dibenzoyltartaroyl, diphenoyl, muconyl, Thx, Cpa, Asu, Nal, Pen, Phg, Dbt, Lys(BOC), Lys(Z), Cys(Bzl), Thr(Bzl), Glu(OtBu), tert.-Leu, Leu, Nle, Pro, Phe, Tyr(Bzl), or Ser(Bal); X,is Asp, Asu, Lys, Glu, Trp, Thx, Cpa, Nal, Pen, Phg, Dbt, Glu(OtBu), tert.-Leu, Leu, Nle, Pro, Tyr, Phe, or Tyr(Bzl); X,is BOC-Glu(OBzl), Glu(OBzl), Asu, OBzl, Bzl, BOC, BOC-Lys(BOC), Z-Glu(OtBu), Asp(OBzl), Asp(OBz)-OBzl, benzyloxycarbonyl, O-(cyclo-hexyl), fluorenylmethyl ester, Glu(OtBu), Glu(OtBu)-OBzl, 1-amino-adamantine, aminomethylcyclohexane, indoline, phenylethylarnide, or dicyclohexylamide; and X,is OMe, OBzl, OtBu, Phe-OMe, -O-(cyclohexyl), Trp-OMe, (chlorophenyl)-isobutylamide, fluorenylmethyl ester, ONp, 1-aminoadamantane, aminomethylcyclohexane, indoline, phenylethylamide, or dicyclohexylamide.

Compounds for reversing drug resistance

The present invention provides a novel pharmaceutical composition for the treatment of breast cancer. Also provided are various methods of treating breast cancer.

Anti-tumor effects of GnRH-III

The invention relates to tumor-inhibiting heptapeptide and octapeptide amide derivatives and to a method of treating mammals, including men, suffering from tumors or from the excessive secretion of insulin, glucagon or growth hormone using these compounds.

Tumor growth-inhibiting somatostatin analogues, pharmaceutical

The invention relates to new peptides of the formula ##STR1## wherein R.sup.2 represents Ala or D-Ala,

Analogs of growth hormone releasing factor (GRF) and a method for the

The present invention relates to novel gonadoliberine analogues of formula I

Gonadoliberine analogues of high activity

The invention relates to novel gonadoliberin nonapeptide ethylamide or decapeptide amide derivatives of the general formula (I),

Gonadoliberin derivatives containing an aromatic aminocarboxylic acid in

The invention relates to a process for producing sexual products suitable for natural or artificial fertilization from mammalia through controlling the activity of their sexual organs in their pre- and post-natal lives, during their infancy, puberty and mature state and, in a given case, to produce offsprings from them as well as to increase several times the production of sexual products to a level far above that typical of the life's performance of the species. According to the invention the mammalia are treated at least once and at most 60 times with a compound of general formula (I),

Process for obtaining sexual products from mammals suitable for natural

The invention relates to a process for increasing the sexual activity of birds and useful domestic mammals and for preparing spermatozoa suitable to their propagation. The process of the invention comprises treating sexually mature male birds or useful domestic mammals at least twice and at most four times with 0.1 to 5 .mu.g/kg of body weight of a compound of the general formula (I),

Process for increasing the sexual activity of birds and useful domestic

The invention relates to gonadoliberin derivatives of the general formula (I)

Gonadoliberin derivatives and process for the preparation thereof

The invention relates to a process for obtaining ready-for-fertilization sexual products from sexually mature fish in a period independent of their natural spawning season, in which actual stage of ripening is determined by probing of sexual products [sperm or eggs], fish not yet ripe for ovulation are separated from ripe fish, compounds of hormonal effect are administered to fish, and after the ovulation sexual products are obtained from the fish or from their environment. In the process according to the invention a nonapeptide-C.sub.1-4 -alkyl-amide or a decapeptide amide of the general formula (I),

Process for obtaining ready for fertilization sexual products from

The invention relates to novel gonadoliberine derivatives of the general formula (I) ##STR1## wherein X represents an --O--R group wherein R is a benzyl group or a C.sub.1-4 alkyl group, an ##STR2## group wherein R1 and R2 independently stand for hydrogen, a C.sub.1-5 alkyl, aryl, aryl-C.sub.1-2 -alkyl, morpholino, 1-indolinyl or 1-pyrrolidinyl group,

Gonadoliberin derivatives containing a .beta.-aspartyl group, a process

Gonadoliberin derivatives process for the preparation and pharmaceutical

Growing community of inventors

Budapest, Hungary

Istvan Teplan