Hoechst Aktiengesellschaft

Jurgen K Sandow

Wolfgang Konig

Rolf Geiger

Hans-Jochen Lang

Cenek Kolar

Christoph Naumann

Anne-Marie Moura

Klaus Wirth

Volker Teetz

Walter Durckheimer

Ulrich Stache

Heinrich Pajunk

Horst Pajunk

Hans G Alpermann

Werner Fritsch

Gunter Ditzinger

Wilfried De Felice

Wolfrad Von Rechenberg

Hans-Peter Merkle

Marianne Von Der Ohe

Axel Friedrich

Rainer Schmiedel

Hans P Merkle

Suzanne Raehs

Compounds of the tautomeric formula Ia, Ib or Ic, ##STR1## where R is a radical of the formula ##STR2## are effective compounds for the treatment and prophylaxis of degenerative bone disorders. They are used as pharmaceuticals.

Guanidinealkyl-1,1-bisphosphonic acid derivatives, process for their

Cyclopeptides and their use as absorption promoters when applied to the mucosa The invention relates to a compound of the formula I ##STR1## or a physiologically tolerated salt thereof, in which X is a basic L- or D-amino acid,

Cyclopeptides and their use as absorption promoters when applied to the

Guanidinealkyl-1,1-bisphosphonic acid derivatives, process for their preparation and their use Compounds of the tautomeric formula Ia, Ib or Ic, ##STR1## where R is a radical of the formula ##STR2## are effective compounds for the treatment and prophylaxis of degenerative bone disorders. They are used as pharmaceuticals.

Guanidinealkyl-1,1-bisphosphonic acid derivatives process for their

Peptides of the formula ##STR1## in which X is alkanoyl, A is optionally substituted D-Nal(2), D-Phe or D-Trp, B is optionally substituted D-Phe, C is D-Pal(3) or optionally substituted D-Phe or D-Trp, and D is Tyr or His, E is D-Ser (R.sup.1), F is Leu, Trp or Phe, G is L-Ser(R.sup.1), H is Gly-NH.sub.2, D-Ala-NH.sub.2 or Azagly-NH.sub.2 and R.sup.1 is a glycosyl radical. These peptides have an inhibitory effect on the formation of the gonadotropins lutropin and follitropin and thus also on the synthesis of testo-sterone and estrogen. A process for the preparation of these peptides is described.

Gonadoliberin antagonists

The invention relates to peptides of the formula ##STR1## in which X is absent or is hydrogen or acyl; A is Pgl, de-hydro-Pro, Pro, D-Thi or D-Pgl or represents optionally substituted D-Nal(2), D-Phe or D-Trp; B is His or optionally substituted D-Phe; C is Trp, D-Thi, D-Pal(3) or optionally substituted D-Trp; D is Tyr, Arg of His; E is D-Ser(R.sup.1), .beta.-Asn, .beta.-Asp-OMe, D-Thi or --NH--CH(CH.sub.2 R.sup.2)--CO--; F is Ser(R.sup.1), Leu, Trp or Phe; G is Gly-NH.sub.2, Aza-Gly-NH.sub.2, D-Ala-NH.sub.2 or NH-alkyl; R.sup.1 is glycosyl and R.sup.2 is hydrogen, acyl, aryl or heteroaryl. The invention also relates to methods for the preparation of these peptides, agents containing them and their use.

Analogs of gonadoliberin with improved solubility, methods for their

The invention relates to the use of aids of the general formula ##STR1## in which B denotes a basic amino acid, A/B denotes an acidic or basic amino acid, X denotes a neutral and hydrophilic amino acid, L denotes a lipophilic neutral amino acid, and R denotes hydrogen or an acyl radical, or the physiologically tolerated salts thereof, for promoting the absorption of peptides and proteins on administration onto the mocosa, as well as to pharmaceutical compositions which contain a pharmacologically effective amount of one or more peptides or proteins as well as an aid of the abovementioned formula.

Cyclic peptides as promoters of absorption on administration onto the

Competitive gonadoliberin antagonists

The invention relates to a device for the injection of implants, preferably implants 'in the form of small rods' (called rods), which are used for the long-term treatment of diseases, whose essential features are the completely transparent construction, especially of the injector body (3), as well as a protecting device which prevents the plunger rod from falling out, and a protective cap (6) for the plunger rod.

Device for the administration of implants

The invention relates to cyclic hexapeptides of the general formula III ##STR1## in which X represents the radical of an L-aminoacid of the general formula IIIa ##STR2## in which A and B are identical or different and denote alkyl having 1 to 3 carbon atoms, or A and B together represent a saturated, unsaturated or aromatic monocyclic or bicyclic structure having 3 to 6 carbon atoms, n denotes 0 or 1, and Y represents an aliphatic or aromatic L-aminoacid the side chain of which can be hydroxylated, and their salts with physiologically tolerated acids, and to a process for their preparation and their use and their intermediates.

Cyclic peptides having somatostatin activity

What are disclosed are a nonapeptide of the formula ##STR1## wherein D-Aad (OBu.sup.t) represents D-.alpha.-aminoadipic acid .delta.-tert. butyl ester, methods for making this peptide, pharmaceutical preparations containing this peptide, and methods for its use in increasing fertility or for contraception.

Nonapeptide, a process for its preparation, an agent containing it and

What is disclosed are steroid-21-halogeno-17-(alkyl carbonates), useful as medicaments for the treatment of inflammatory dermatoses, and a method for making them.

Corticoid-17-(alkyl carbonates) and process for their manufacture

What is disclosed in a method of inducing a contraceptive effect in a mammal by administering a contraceptively effective amount of a peptide of the formula ##STR1## in which X stands for D-serine-tert.butyl ether or D-glutamic acid .gamma.-cyclohexylamide.

LH-RH-Peptides as contraceptives

A peptide with LH-RH-activity which is a LH-RH-peptide wherein Gly in 6-position is replaced by D-glutaminic-acid which may be N-substituted at the CO-NH.sub.2 moiety, wherein in 10-position Gly-NH.sub.2 may be replaced by a NH-alkyl or NH-cycloalkyl group and/or wherein the amino acids in 4-, 5-, 7- and/or 8-position may be replaced by other amino acids and a process for its manufacture.

Peptides having gonadoliberin activity and process for their manufacture

The present invention relates to peptides having strong LH-RH/FSH-RH activity, wherein Gly in the 6-position is replaced by different substituted amino acids and in the 10-position there is glycinamide or glycine in the 10-position is replaced by a NH-alkyl group with 1-3 carbon atoms or a NH-cyclopropyl group. The invention relates as well to a process for manufacturing said peptides, and to pharmaceutical preparations containing said peptides.

Growing community of inventors

Konigstein/Taunus, Germany

Jurgen K Sandow