Hoechst Aktiengesellschaft

Other

Aventis Pharma Deutschland, Gmbh

Genentech, Inc.

Sanofi-A Ventis Deutschland Gmbh

Hoescht Aktiengesellschaft

Aventis Pharma S.a. Deutschland Gmbh Genentech, Inc.

Anuschirwan Peyman

Thomas Gadek

Eugen Uhlmann

Jochen Knolle

Robert S McDowell

Denis Carniato

Jean-Marie Ruxer

Volkmar Wehner

David William Will

Jean-Francois Gourvest

Hans Ulrich Stilz

Jean-Michel Lefrancois

Irvin Winkler

Matthias Helsberg

Karl-Heinz Budt

Karlheinz Scheunemann

Gerhard Breipohl

Sarah Catherine Bodary

Gerhard Zoller

Hans Matter

Uwe Gerlach

Karl-Heinz Scheunemann

Robert Andrew Cuthbertson

Bernd Stowasser

Gerard J O'Malley

Adolf Heinz Linkies

Gerhard Kretzschmar

Dieter Bernd Reuschling

Matthias Mag

Holger Wallmeier

Marc Nazaré

Carolin Carolus

Jian-Qi Li

Marc Nazare

Esther H Chang

Gerrit Schubert

Wilhelm Stahl

Fahad A Al-Obeidi

Kathleen F Pirollo

Dieter Ruppert

Hans G Berscheid

Christoph Meichsner

Hans-Peter Nestler

Theodor Andreas Wollmann

Antonina Rait

Konrad Wagner

Henning Schussler

J Org Spanig

Jorg Spanig

Karlheinz Budt

Jean Francois Gourvest

Caroline Weiser

Gerhard Brejpohl

Napoleane Ferrara

Robert Mcdowell

Jean-François Gourvest

The present invention relates to compounds of the formula I, in which R; Q; X; Q', D, Rand V have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

Guanidine and amidine derivatives as factor Xa inhibitors

The present invention relates to acylguanidino derivatives of formula (I), in which R, R, R, A, B, X, Y and n have the meanings indicated in claim, their physiologically tolerable salts and their prodrugs. The compounds of the formula (I) are valuable pharmaceutically active compounds. They are vitronectin receptor antagonists and inhibitors of cell adhesion and bone resorption by osteoclasts. This renders them suitable, for example, for the therapy and prophylaxis of illness which are based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-matrix interaction processes or which can be prevented, alleviated or cured by influencing such interactions. For example, they can be applied for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or proliferation of cells of the vascular smooth muscles. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as pharmaceutical active ingredients, and pharmaceutical compositions comprising them 

Guanidino derivatives as inhibitors of cell adhesion

Oligonucleotides of the formula5'-(CAP)-(Oligo)-(CAP)-3&#x2032;are disclosed where (oligo) is a nucleotide sequence of from 10 to 40 nucleotides in length, and CAP is G, where m is an integer of from zero to ten, the two CAP's which are present in the molecule can be defined independently of each other and must be different in the case where m is zero at the 5&#x2032; or 3&#x2032; end and the end of the Oligo sequence is other than guanine. The oligonucleotides can be synthesized chemically. The oligonucleotides are used to diagnose or treat cancer, restenosis, a disease caused by a virus, a disease affected by integrins or cell-cell adhesion receptor or a disease triggered by diffusible factors.

G cap-stabilized oligonucleotides

The present invention relates to compounds comprising the following formula:R-Q-X-Q'-W-U-V-G-M&#x2003;&#x2003;(I)These compounds are useful as pharmacologically active compounds. They exhibit an antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders such as thromboembolic diseases or restenoses. These compounds are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can generally be used to treat, prevent, or cure conditions in which an undesired activity of factor Xa and/or factor VIIa is present, or where inhibition of factor Xa and/or factor VIIa is intended. The invention further relates to processes for the preparation of these compounds, methods of their use (e.g., as active ingredients in pharmaceuticals), and pharmaceutical preparations comprising them.

Oxybenzamide derivatives useful for inhibiting factor Xa or Vlla

A process for the preparation of a compound of the formulawherein the substituents are defined as in the specification.

Process for the preparation of birthonectin receptor antagonists

The present invention relates to compounds comprising the following formula:R&#x2014;Q&#x2014;X&#x2014;Q'&#x2014;W&#x2014;U&#x2014;V&#x2014;G&#x2014;M&#x2003;&#x2003;(I)These compounds are useful as pharmacologically active compounds. They exhibit an antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders such as thromboembolic diseases or restenoses. These compounds are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can generally be used to treat, prevent, or cure conditions in which an undesired activity of factor Xa and/or factor VIIa is present, or where inhibition of factor Xa and/or factor VIIa is intended. The invention further relates to processes for the preparation of these compounds, methods of their use (e.g., as active ingredients in pharmaceuticals), and pharmaceutical preparations comprising them.

Oxybenzamide derivatives useful for inhibiting factor Xa or viia

The invention relates to specific, optionally modified oligonucleotides with a length of up to 17 nucleotides. Said oligonucleotides correspond to segments of tenascin-coding sequences or can bind to these sequences. The invention also relates to the production and use of the oligonucleotides, for example for the specific inhibition of the expression of tenascin and for producing medicaments used to treat vitiligo.

Antisense oligonucleotides against tenascin for treating vitiligo

(2S)-2-(Adamantan-1-ylmethoxycarbonylamino)-3-(4-(2-(1,4,5,6-tetrahydropyrimidin-2-ylcarbamoyl)ethyl)benzoylamino)propionic acid isopropyl ester, its preparation and its use The present invention relates to (2S)-2-(adamantan-1-ylmethoxycarbonylamino)-3-(4-(2-(1,4,5,6-tetrahydropyrimidin-2-ylcarbamoyl)ethyl)benzoylamino)propionic acid isopropyl ester of the formula Iand its physiologically tolerable salts, their preparation, their use as pharmaceuticals and to pharmaceutical compositions comprising them. The compound of the formula I and its physiologically tolerable salts are valuable pharmacologically active compounds which can be used, for example, in the treatment or prophylaxis of diseases which can be influenced by inhibiting the vitronectin receptor, for example of bone diseases such as osteoporosis.

(2S)-2-(adamantan-1-ylmethoxycarbonylamino)-3-(4-(2-(1,4,5,6-tetrhydropyrimidin-2-ylcarbamoyl)ethyl)benzoylamino)propionic acid isopropyl ester, its preparation and its use

The present invention relates to compounds of the formula IA&#x2014;B&#x2014;D&#x2014;E&#x2014;F&#x2014;G&#x2003;&#x2003;(I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.

Vitronectin receptor antagonists, their preparation and their use

The present invention relates to compounds of formula (I), in which A, B, X, Y, R , R , R and n have the meanings indicated in the claims. The compounds of formula (I) are valuable pharmacologically active compounds. They are vitronectin receptor antagonists and inhibitors of cell adhesion and are suitable for the therapy and prophylaxis of illnesses which are based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-matrix interaction processes or which can be prevented, alleviated or cured by influencing such interactions. For example, they can be applied for inhibiting bone resorption by osteoclasts and thus for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or proliferation of cells of the vascular smooth musculature. The invention furthermore relates to processes for the preparation of compounds of formula (I), their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.

Thienylalanine derivatives as inhibitors of cell adhesion

The present invention relates to compounds of formula (I), in which B, D, E, G, X, Y, Z, R , R and s have the meanings indicated in the claims, their physiologically tolerable salts and their prodrugs. The compounds of formula (I) are valuable pharmacologically active compounds. They are vitronectin receptor antagonist and inhibitors of cell adhesion and are suitable for the therapy and prophylaxis of illnesses which are based on the interaction between vitronectin receptors and their ligands in cell-cell or cell-matrix interaction processes or which can be prevented, alleviated or cured by influencing such interactions. For example, they can be applied for inhibiting bone resorption by osteoclasts and thus for treating and preventing osteoporosis, or for inhibiting undesired angiogenesis or prolifertion of cells of the vascular smooth musculature. The invention furthermore relates to processes for the preparation of compounds of formula (I), their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.

Substituted purine derivatives as inhibitors of cell adhesion

Sulfonamide derivatives, their physiologically tolerable salts and their prodrugs according to the present invention are vitronectin receptor antagonists and inhibitors of cell adhesion, as well as inhibit bone resorption by osteoclasts. These derivatives, salts and prodrugs are pharmaceutically active compounds useful in the therapy and prophylaxis of diseases which are caused at least partially by an undesired extent of bone resorption, for example of osteoporosis. Processes for the preparation of the sulfonamide derivatives according to the present invention, the use of these derivatives as pharmaceutically active ingredients, and pharmaceutical preparations comprising these derivatives also are disclosed.

Sulfonamide derivatives as inhibitors of bone resorption and as inhibitors of cell adhesion

The invention relates to a specific modified oligonucleotide complementary to a section of the human Ha-ras gene and mRNA, and its use to specifically regulate, modulate or inhibit expression of the HA-ras gene, and its use as a pharmaceutical for the treatment of conditions arising from the abnormal expression of the Ha-Ras gene, in particular in combination with chemotherapy and radiotherapy. The modified oligodeoxynucleotide according to the invention has the sequence 5&prime;-TxAxTxTxCxCxGxTxCxAxT-3&prime;-O&mdash;PO &mdash;O&mdash;R (SEQ ID NO:1), wherein X is an internucleotide linkage of type o or s, with the proviso that x is an s linkage at least 4 times and at most 9 times, and o means a phosphodiester internucleoside linkage, s means a phosphorothioate internucleoside linkage, R means a C -C alkyl group, &mdash;(CH &mdash;CH O)n-(CH ) &mdash;CH , or &mdash;CH &mdash;CH(OH)CH O&mdash;(CH ) &mdash;CH wherein n is an integer from 1 to 6, m is an integer from 0 to 20 and q is an integer from 7 to 20 and A is 2&prime;-deoxyadenosine, G is 2&prime;-deoxyguanosine, C is 2&prime;-deoxycytidine and T is thymidine.

Modified antisense nucleotides complementary to a section of the human Ha-ras gene

Substituted purine derivatives, processes for their preparation, their use, and compositions comprising them

The present invention relates to acylguanidine derivatives of formula (I) in which R , R , R , R , R , A, m and n have the meanings indicated in the patent claims, their physiologically tolerable salts and their prodrugs. The compounds of formula (I) are valuable pharmaceutical active ingredients. They are vitronectin receptor antagonists and inhibitors of bone resorption by osteoclasts and are suitable, for example, for the therapy or prophylaxis of diseases which are caused at least partially by an undesired extend of bone resorption, for example of osteoporosis. The invention furthermore relates to processes for the preparation of compounds of formula (I), their use, in particular as pharmaceutical active ingredients, and pharmaceutical preparations comprising them.

Acylguanidine derivatives as inhibitors of bone resorption and as vitronectin receptor antagonists

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Kelkheim, Germany

Anuschirwan Peyman