Asta Medica, Aktiengesellschaft

Asta Pharma Aktiengesellschaft

Degussa Aktiengesellschaft

Aeterna Zentaris Gmbh

Asta-werke Aktiengesellschaft, Chemische Fabrik

Zentaris Gmbh

Asta-werke Aktiengesellschaft

Max-planck-gesellschaft Zur Forderung Der Wissenschaften E.v.

Boehringer Mannheim Gmbh

Degussa Gmbh

Asta Medica Aktiengellschaft

Zentaris Ivf Gmbh

Zentaris Ivp Gmbh

Aasta Pharma Ag

Asta Pharma Akteingesellschaft

Jurgen Engel

Bernhard Kutscher

Peter Hilgard

Bernd Nickel

Dieter Sauerbier

Wolfgang Schumacher

Helmut Hettche

Axel Kleemann

Istvan Szelenyi

Peter Emig

Gerhard Scheffler

Thomas Reissmann

Stefan Szelenyi

Klaus Thiemer

Helmut Schonenberger

Gerhard Nossner

Hilde Riethmuller-Winzen

Wolfgang Deger

Ulf Niemeyer

Jurij Stekar

Erwin Von Angerer

Elisabeth Wolf-Heuss

Eckhard Milsmann

Klaus Diedrich

Rainer Voegeli

Heinz Ulrich

Ilona Fleischhauer

Alfred Olbrich

Henri Brunner

Vladimir Jakovlev

Michael Lobisch

Jurgen Rawert

Giancarlo Camuglia

Hansjorg Eibl

Ulrich Werner

Joachim Goede

Otto Isaac

Fritz Stroman

Michael Bernd

Carl-Heinrich Weischer

Herbert Sindermann

Hans-Reinhold Dieter

Gabriela Pergande

Clemens Unger

Norbert Knebel

Ralph Venhaus

Peter Hankofer

Rene Frydman

Gunter Losse

Friedrich Maiterth

Peter Metzenauer

Sandra Murgas

Ricardo Felberbaum

Bernd Kutscher

Paul Devroey

Margaretha Jennerwein

Gerhard Oepen

Wolfgang Naumann

Philippe Bouchard

Georg Niebch

Gisbert Sponer

Winfried Orth

Kurt Thiele

Manfred Schmidt

Thomas Klenner

Klaus Posselt

Roland Moller

Burkhard Wichert

Reinhard Muckenschnabel

Jorg Pohl

Reinhold Carle

Horst Bauer

Hans Pohle

Gerfried Unger

Karl-Heinz Mangartz

Ute Achterrath-Tuckermann

Jurgen Schmidt

Karl-Heinz Klingler

Klaus Molge

Gerhard N&ouml;ssner

Michael Molliere

Claus Gehringer

Jurgen Beyer

Helmut Orth

Ute Achterath-Tuckermann

Emanuel Polymeropoulos

Karin Klokkers-Bethke

Thomas Reissman

Heinz Grossmann

Maria Kick

Jurgen Arp

Wolfgang Küpker

Manfred Lieflander

Jens-Peter Wulf

Michael Schwarz

Jurij Stekar, Deceased

Gerhard Nssner

Margrit Stekar

Ute Achterrath-Tuckerman

Rudolf Aurich

A method for obtaining the production of a fertilizable oocyte within a program of assisted reproduction techniques comprising normal follicular growth and development to proceed in the absence of stimulation by an exogenous gonadotropin, followed by administering an amount of an LHRH antagonist in a dosage regimen that prevents a premature LH surge while maintaining FSH secretion at a natural level and individual estrogen development is not affected.

LHRH&#x2014;antagonists in the treatment of fertility disorders

The invention relates to the use of alkylphosphocholines in combination with antimetabolite antitumor substances for the treatment of benign and malignant oncoses in humans and animals. It is possible in this connection for the alkylphosphocholines to be employed in a combination according to the invention with one or more antimetabolite antitumor substances. Preferred alkylphosphocholines are described by the Formula II.  One such preferred alkylphosphocholine is perifosine.

Use of perifosine in combination with antimetabolites for the treatment of benign and malignant oncoses in humans and mammals

The invention relates to pharmaceutical compositions comprising alkylphosphocholines and antimetabolite antitumor substances. The pharmaceutical compositions of the invention are useful for the treatment of benign and malignant oncoses in humans and animals. Preferred alkylphosphocholines are described by the Formula II.  One such preferred alkylphosphocholine is perifosine.

A method of therapeutic management of infertility by programming of controlled ovarian stimulation and assisted reproductive procedures is disclosed containing the steps of a) suppression of premature ovulation with an LHRH-antagonist in controlled ovarian stimulation and assisted reproductive techniques with multiple follicle and oocyte development; b) programming the start of controlled ovarian stimulation by the administration to a patient of progestogen only-preparations or, alternatively, combined oral contraceptive preparations; c) exogenous stimulation of the ovarian follicle growth; d) ovulation induction with HCG, native LHRH, LHRH-agonists or recombinant LH; and e) application of assisted reproduction techniques, especially of IVF, ICSI, GIFT, ZIFT or by intrauterine insemination by sperm injection, wherein onset of the patient's menstrual cycle and of controlled ovarian stimulation are programmed in order to perform oocyte pickup and fertilization procedures during Mondays to Fridays.

Method for a programmed controlled ovarian stimulation protocol

A method of treating infertility disorders by 1) administering an LH-RH antagonist, preferably Cetrorelix, in amounts to selectively suppress endogenous LH but not FSH secretion and 2) inducing follicle growth by administration of exogenous gonadotropin. The selective suppression OF LH allows FSH secretion to be at natural levelS thereby not affecting individual estrogen development. The LH-RH antagonist can be given as a single or dual subcutaneous dose in the range of 1 mg to 10 mg, preferably 2 mg-6 mg. In multiple dosing-posology, LH-RH antagonist can be administered subcutaneously in an amount in the range of 0.1 to 0.5 mg of LH-RH antagonist/day. LH-RH antagonist is applied starting cycle day 1 to 10, preferably on day 4 to 8, and ovulation can be induced between day 9 and 20 of the menstruation cycle by administering rec. LH, native LH-RH, LH-RH agonist or by HCG. In addition rec. LH, native LH-RH or LH-RH agonist can be given to avoid hyperstimulation syndrome and native LH-RH or a LH-RH agonist can be administered to avoid luteal phase stimulation by neutralizing the negative effects of HCG.

LHRH-antagonists in the treatment of fertility disorders

The present inventions provides a method for therapeutic management of extrauterine proliferation of endometrial tissue, chronic pelvic pain and fallopian tube obstruction by short term induction treatment with an LH-RH antagonist for 4 to 12 weeks. According to another aspect of the present invention, the short term LH-RH treatment is followed by the combined or separate administration of one or more active agents selected from the group consisting of a contraceptive, preferably an oral contraceptive, a non-steroidal anti-rheumatic agent, an analgetic, an androgen other than a 17-alpha-alkyl substituted testosterone or any combinations thereof. According to a further aspect of the present invention a pharmaceutical composition comprising an LHRH antagonist and one ore more active agents selected from the group consisting of a contraceptive, preferably an oral contraceptive, a non-steroidal anti-rheumatic agent, an analgetic, an androgen other than a 17-alpha-alkyl substituted testosterone or any combinations thereof are provided.

Method for the therapeutic management of extrauterine proliferation of endometrial tissue, chronic pelvic pain and fallopian tube obstruction

A method of treating protozoal and fungal diseases is described, in which an effective amount of a compound of formula I is administered to a host having a protozoal or fungal disease. Also described are methods of treating bone marrow damage composed of administering, to a host having bone marrow damage due to treatment with cytostatic agents or other myelotoxic active ingredients, an effective amount of a compound of formula I

Disease treatment with novel phospholipid derivatives

Phospholipid derivatives

The invention relates to a diagnostic composition for improving the effectiveness of hysteroscopy, characterized in that it contains an LH-RH antagonist, in particular cetrorelix. The composition is envisaged for use prior to hysteroscopy and/or for preparation for surgery, specifically in a single dose of between 0.1 and 2 mg/kg. However, the composition can also be administered, for use prior to hysteroscopy and/or for preparation for surgery, in a multiple dose of between 0.01 and 0.5 mg/kg, preferably spread over 1-14 days. The composition is furthermore suitable for use in hysteroscopy in combination with the subsequent treatment of pathological conditions of the uterus such as myoma and endometrial hyperplasia.

Diagnostic composition containing an LH-RH antagonist for hysteroscopy

The side effect of decrease in body weight caused by the alkylphosphocholines such as miltefosine can be antagonized by certain acetylcholine receptor antagonists such as domperidone and pimozide. The combination of alkylphosphocholine plus the antagonist does not have any effect on the anti-tumor action of the alkylphosphocholine. The combination also caused no new side effects in the animals.

Use of dopamine receptor antagonists in palliative tumor therapy

A regime for therapeutic management of a benign prostatic hyperplasia and prostatic cancer employs Cetrorelix alone or in combination with .alpha.-reductase inhibitors or .alpha.-receptor blocking agents. The regimen reduces the volume of the prostate and avoids the side effects associated with testosterone levels being in a castration range. Cetrorelix is administered at dosages between 0.5 mg/day and 20 mg/week or about 0.014 mg/kg body weight per day to 0.30 mg/kg body weight per week or at levels of about 25 to 120 mg of Cetrorelix per month or 0.376 mg/kg to 1.71 mg/kg per month. Cetrorelix can be administered with .alpha.-reductase inhibitors or .alpha.-receptor blocking agents.

Means for treating prostate hypertrophy and prostate cancer

A regime for therapeutic management of a benign prostatic hyperplasia and prostatic cancer employs Cetrorelix alone or in combination with .alpha.-reductase inhibitors or .alpha.-receptor blocking agents. The regimen reduces the volume of the prostate and avoids the side effects associated with testosterone levels being in a castration range Cetrorelix is administered at dosages between 0,5 mg/day and 20 mg/week or about 0.014 mg/kg body weight per day to 0,30 mg/kg body weight per week or at levels of about 25 to 120 mg of Cetrorelix per month or 0.376 mg kg to 1.71 mg/kg per month Cetrorelix can be administered with .alpha.-reductase inhibitors or .alpha.-receptor blocking agents.

In this invention, a release-delaying system is to be developed for LHRH antagonists, in particular for cetrorelix, which allows the active compound to be released in a controlled manner over several weeks by complexation with suitable biophilic carriers. The acidic polyamino acids polyglutamic acid and polyaspartic acid were selected for complexation with cetrorelix. The cetrorelix polyamino acid complexes are prepared from aqueous solutions by combination of the solutions and precipitation of the complexes, which are subsequently centrifuged off and dried over P.sub.2 O.sub.5 in vacuo. If complexes having a defined composition are to be obtained, lyophilization proves to be a suitable method. The cetrorelix-carboxylic acid complexes were also prepared from the aqueous solutions. In the random liberation system, the acidic polyamino acids poly-Glu and poly-Asp showed good release-delaying properties as a function of the hydrophobicity and the molecular mass of the polyamino acid. In animal experiments, it was possible to confirm the activity of the cetrorelix-polyamino acid complexes as a depot system in principle. It is thus possible by complexation of cetrorelix with polyamino acids to achieve testosterone suppression in male rats over 600 hours. The release of active compound here can be controlled by the nature and the molecular mass of the polymers.

Process for the preparation of immobilized and activity-stabilized

A process for the preparation of C.sub.14 -C.sub.18 -alkylphosphocholines by reacting an n-alkanol with a chain length of C.sub.14 -C.sub.18 with phosphorus oxychloride in an inert solvent or also without solvent in the presence or absence of a basic substance in a single vessel process and subsequent reaction of the reaction product in an inert solvent with a choline salt in the presence of a basic substance to form phosphoric acid diester chloride, subsequent hydrolysis and isolation of alkylphosphocholine as well as optionally purification using a mixed-bed ion exchanger or in successive steps with an acid ion exchanger and a basic ion exchanger.

Process for the preparation of alkylphosphocholines and the production

Immobilized and activity-stabilized complexes of LHRH antagonists and

Growing community of inventors

Alzenau, Germany

Jurgen Engel