Abstract: The invention relates to novel compounds of the type of the imidazolidines of the formula I in which R1 to R7 are as defined in the claims. They are used for preparing a medicament for the treatment or prophylaxis of the central nervous system, of lipid metabolism, of infection by ectoparasites, of disorders of gall function and for improving the respiratory drive and are therefore used for treating respiratory distress. Additionally, the compounds increase the muscle tone of the upper respiratory tract, thus suppressing snoring.
Type:
Application
Filed:
July 16, 2004
Publication date:
January 6, 2005
Applicant:
AVENTIS PHARMA DEUTSCHLAND GMBH
Inventors:
Uwe Heinelt, Hans-Jochen Lang, Armin Hofmeister, Klaus Wirth
Abstract: Substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives, processes for their preparation and their use as medicaments The invention relates to substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives and to the physiologically tolerated salts and physiologically functional derivatives thereof. Compounds of the formula I in which the radicals have the stated meanings, and the physiologically tolerated salts thereof and processes for preparing them are described. The compounds are suitable for example as anorectic agents.
Type:
Application
Filed:
February 13, 2004
Publication date:
January 6, 2005
Applicant:
Aventis Pharma Deutschland GmbH
Inventors:
Stefanie Flohr, Siegfried Stengelin, Matthias Gossel, Thomas Klabunde
Abstract: The present invention relates to compounds of the formula I which are inhibitors of the adhesion and migration of leucocytes and/or antagonists of the adhesion receptor VLA-4 which belongs to the group of integrins. The invention also relates to processes for the preparation of formula I, pharmaceutical compositions containing compounds of formula I, and the treatment or prophylaxis of various diseases caused by or are associated with excess leucocyte adhesion and/or leucocyte migration, as well as diseases associated with cell-cell or cell-matrix interactions, which on interactions of VLA-4 receptors with their ligands play a part of, for example, inflammatory processes, rheumatoid arthritis or allergic disorders.
Type:
Grant
Filed:
November 29, 2001
Date of Patent:
January 4, 2005
Assignee:
Aventis Pharma Deutschland GmbH
Inventors:
Hans Ulrich Stilz, Volkmar Wehner, Christoph Huls, Dirk Seiffge
Abstract: The present invention relates to PNA derivatives which carry, at the N terminus of the PNA backbone, a phosphoryl radical. The phosphoryl radical can be, for example, a phosphate radical, or a substituted phosphoryl radical, with substituted phosphoryl derivatives carrying, where appropriate, one or more labeling groups, groups for crosslinking, groups which promote intracellular uptake, or groups which increase the binding affinity of the PNA derivative for nucleic acids. The invention furthermore relates to a process for preparing the abovementioned PNA derivatives and to their use as pharmaceuticals and diagnostic agents.
Type:
Application
Filed:
June 9, 2004
Publication date:
December 30, 2004
Applicant:
Aventis Pharma Deutschland GmbH
Inventors:
Eugen Uhlmann, Gerhard Breipohl, David William Will
Abstract: Corticoid 17,21-dicarboxylic esters and corticosteroid 17-carboxylic ester 21-carbonic esters, processes for their preparation and pharmaceuticals containing these compounds
Corticoid 17,21-dicarboxylic esters and corticoid 17-carboxylic ester 21-carbonic esters of the formula I:
are described, in which A is CHOH and CHCl, CH2, C═O or 9(11) double bond; Y is H, F or Cl; Z is H, F or methyl; R(1) is aryl or hetaryl; R(2) is alkyl and R(3) is H or methyl. They are obtained, inter alia, by reacting a compound of the formula II:
in which R(5) is OH, with an activated carboxylic acid of the formula III:
R(6)-CO—(O)n[(C1-C4)-alkyl]m-R(1) III.
They have a very strong local and topical antiinflammatory action and exhibit a very good ratio of local to systemic antiinflammatory effects. They are used, inter alia, as agents for treating inflammatory dermatoses.
Type:
Grant
Filed:
July 22, 1997
Date of Patent:
December 28, 2004
Assignee:
Aventis Pharma Deutschland GmbH
Inventors:
Ulrich Stache, Hans-Georg Alpermann, Walter Dürckheimer, Manfred Bohn
Abstract: The invention relates to the identification and use of the DAF-2/IR responsive sod-3 promoter. Transgenic C. elegans containing sod-3 reporter gene constructs are described which are useful for, among other things, the identification of genes or compounds capable of modulating the DAF-2/IR-akt pathway. Conditions are disclosed that increase or decrease the reporter activity, demonstrating the presence of either activators or inhibitors of the DAF-2/IR pathway.
Type:
Application
Filed:
January 28, 2004
Publication date:
December 23, 2004
Applicant:
Aventis Pharma Deutschland GmbH
Inventors:
Edmund Hoppe, Ulrike Siebers, Heike Schauerte, Jonathan Rothblatt
Abstract: Novel substituted 2-aminoimidazoles of formula I, process for their preparation, their use as medicament or diagnostic aid, and medicament containing them. The compounds of this type are useful in the prevention or treatment of various disorders and can be employed inter alia for renal disorders such as acute or chronic renal failure, for disorders of biliary function, for respiratory disorders such as snoring or sleep apneas or for stroke.
Abstract: Peptides having bradykinin-antagonistic action are suitable for the production of pharmaceuticals for the prophylaxis and therapy of diseases in whose course an increased activity of matrix metalloproteinases is involved. These include diseases such as degenerative joint diseases, for example osteoarthrosis, spondylosis and chondroporosis after joint trauma or relatively long immobilization of a joint after meniscus or patella injuries or torn ligaments.
Abstract: The invention relates to pyrimido[5,4-e][1,2,4]triazine-5,7-diones, pharmaceutically acceptable salts thereof and physiologically functional derivatives.
Type:
Application
Filed:
January 20, 2004
Publication date:
December 2, 2004
Applicant:
Aventis Pharma Deutschland GmbH
Inventors:
Stefan Petry, Karl-Heinz Barimghaus, Norbert Tennagels, Guenter Mueller
Abstract: The application discloses substituted norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics and a medicament comprising them
Substituted norbornylamino derivatives having exo-configured nitrogen and an endo-fused five-membered ring of the formula I, or having exo-configured nitrogen and an exo-fused five-membered ring of the formula I a
in which R1, R2, R3, R4, R5, A, B, S1, and S2 are as defined in the claims, are highly suitable for use as antihypertensive agents, for reducing or preventing ischemically induced damage, for use as medicaments for surgical interventions for the treatment of ischemias of the nervous system, of stroke and cerebral edema, of shock, of impaired respiratory drive, for the treatment of snoring, as laxatives, as agents against ectoparasites, for the prevention of the formation of biliary calculus, as antiatherosclerotics, as agents against late diabetic complications, carcinomatous disorders, fibrotic disorders, endot
Abstract: An ethanol solvate form of (−)-cis-2-(2-chlorophenyl)-5,7-dihydroxy-8[4R-(3S-hydroxy-1-methyl)piperidinyl]-4H-1-benzopyran-4-one hydrochloride (Form II), a method of making Form II and a composition comprising Form II.
Abstract: The present invention relates to a process for the storage of proteins in an aqueous solution. The addition of cysteine delays the temporal decrease in the effective concentration of the protein. The process is suitable for use in the production of heterologous proteins in microorganisms.
Abstract: The present invention relates to novel compounds of the formula I
in which R(1), R(2), R(3) and R(4) are, independently of each other, hydrogen or an alkyl radical. The compounds of the formula I are inhibitors of KDR kinase and, due to their antiangiogenic effect, are suitable for preventing and/or treating malignant diseases. The compounds of the formula I can be obtained by fermenting the microorganism Eurotium echinulatum Delacroix (DSM 13872) or by chemically derivatizing the compounds which are obtained after fermenting said microorganism. The invention consequently also relates to a process for preparing the compounds of the formula I, to the use of the compounds of the formula I for preparing a pharmaceutical for treating malignant diseases and diseases which can be treated by inhibiting KDR kinase, and also to pharmaceutical preparations which have a content of at least one compound of the formula I.
Type:
Grant
Filed:
June 26, 2002
Date of Patent:
November 16, 2004
Assignee:
Aventis Pharma Deutschland GmbH
Inventors:
Claudia Eder, Herbert Kogler, Luigi Toti