Hoechst Aktiengesellschaft

Aventis Pharma Deutschland, Gmbh

Sanofi-a Ventis Deutschland Gmbh

Sanofi-aventis

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

Aventis Pharmaceuticals Inc.

Sanofi

Hoechst Japan Limited

Hoeschst Aktiengesellschaft

Hoechst Aktiengellschaft

Hoechst Aketiengesellschaft

Hans-Jochen Lang

Wolfgang Scholz

Udo Albus

Andreas Gerhard Weichert

Heinz-Werner Kleemann

Jan-Robert Schwark

Uwe Heinelt

Klaus Wirth

Armin Hofmeister

Heinrich Christian Englert

Martin Bickel

Karl Geisen

Roman Muschaweck

Markus Bleich

Max Hropot

Gerhard J&auml;hne

Michael Gekle

Ernold Granzer

Hans-Willi Jansen

Dieter Mania

Andreas W Herling

Wolfgang Linz

Klaus Weidmann

Christoph Naumann

Anne-Marie Moura

Robert Rippel

Hildegard Nimmesgern

Gerhard Jaehne

Joachim Brendel

Bernward Scholkens

Jurgen K Sandow

Peter Crause

Bela Kerekjarto

Bernhard Seuring

Rainer Greger

Thomas Licher

Denis Carniato

Matthias Gossel

Michael R Angelastro

John Weston

Roland Utz

Haifeng Eishingdrelo

Theresa Kuntzweiler

Bernd Knabe

Masakazu Katoh

Ryoichi Satoh

Florian Lang

Heiner Glombik

Hiroshi Kitagawa

Wendelin Frick

Tsutomu Inoue

Bansi Lal

Stefan Petry

Uwe Gerlach

Hans Ulrich Stilz

Milos Babej

Manfred Rosner

Mizuho Inazu

Wulf Merkel

Josef Musil

Anne Minnich

Sabine Faber

Karl-Heinz Scheunemann

Heinz-Werner Kleeman

Hartmut R&uuml;tten

Bela Kelety

Ramanujam Rajagopalan

Ramesh Gidwani

Radha Panicker

Chinnakulandai Sankar

Eike Druckrey

Weidmann, Klaus

Martin Hug

Peter Schmid

Friedrich E Beyhl

Ann Minnich

John C Ellory

Andreas G Weichert Dr

The invention provides the process illustrated in scheme 1 for synthesizing heterocyclic compounds of formula I. In the process, an isothiocyanate of formula II is initially reacted with a primary amine or formula III to give a thiourea of formula IV. Subsequently, the thiourea of formula IV is converted to the corresponding heterocycle of formula I using a base and a sulfonyl chloride.

Process for synthesizing heterocyclic compounds

The present invention relates to substituted 4-phenyltetrahydroisoquinoline compounds and pharmaceutical compositions comprising them which are excellent inhibitors of the sodium-hydrogen exchanger (NHE), in particular of the sodium-hydrogen exchanger of subtype 3 (NHE-3). As such these compounds are useful in the treatment of various disorders of the renal and respiratory systems such as acute or chronic renal failure, pulmonary complications, biliary function disorders, respiratory disorders such as snoring or sleep apneas and cardiovascular/central nervous system disorders such as stroke. More specifically, the present invention relates to substituted 4-phenyl-tetrahydroisoquinolines defined by the formula I in which R1-R8 are defined herein.

Substituted 4-phenyltetrahydroisoquinolines, process for their preparation, pharmaceutical compositions and therapeutic use

The present invention relates to compounds useful in the prevention or treatment of various disorders such as acute or chronic renal failure, for impairments of biliary function, for respiratory impairments such as snoring or sleep apneas or for stroke, and pharmaceutical compositions comprising them. More specifically, the compounds of the present invention comprises substituted 1-amino-4-phenyl-dihydroisoquinolines and their derivatives of formula I:  Wherein the substituents R1-R11 are more specifically defined hereinbelow. The claimed compounds of the present invention also include their pharmaceutically acceptable salts and trifluoroacetates thereof as well as methods for their preparation and pharmaceutical delivery systems thereof.

Substituted 1-amino-4-phenyl-dihydroisoquinolines, methods for the production thereof, use thereof as a medicament, and medicaments containing them

The invention relates to NHE-3 inhibitor compounds of formula I: In which R1-R11 are more specifically defined herein. These substituted 2-amino-4-phenyl-dihydroquinolines are useful the treatment of various renal and respiratory disorders such as acute or chronic renal failure, for impairments of biliary function and respiratory impairments such as snoring, sleep apneas or stroke. Formulations comprising them and methods for their use are also described herein.

Substituted 2-amino-4-phenyldihydroquinolines, processes for their preparation, pharmaceutical compositions and methods for their use

This invention is directed to the compound of formula (I), compositions containing said compounds to inhibit the sodium-proton exchanger of subtype 3 (NHE3) which are useful in the prevention or treatment of various disorders in a patient suffering from a disease state, such as, renal disorders including acute or chronic renal failure, disorders of biliary function and for respiratory disorders such as snoring or sleep apnea or for stroke.

N-substituted (benzoimidazol-2-yl)phenylamines, processes for their preparation, their use as a medicament or diagnostic aid, and a medicament comprising them

The invention relates to substituted 4-phenyltetrahydroisoquinolines of formula I wherein R1-R8, N, W, X and Z are defined herein. These compounds and pharmaceutical compositions comprising them are useful in the treatment of respiratory disorders, sleep apnea, kidney disorders, high blood pressure, hypertension, disorders of the central nervous system and the like.

Substituted 4-phenyltetrahydroisoquinolines, pharmaceutical compositions comprising them and therapeutic methods for their use

The present invention relates to substituted 4-phenyltetrahydroisoquinoline compounds of the structure of formula I and pharmaceutical compositions comprising them wherein the R groups are herein defined. These are excellent inhibitors of the sodium-hydrogen exchanger (NHE), in particular of the sodium-hydrogen exchanger of subtype 3 (NHE3). As such these compounds are useful in the treatment of various disorders of the renal and respiratory systems such as acute or chronic renal failure, pulmonary complications, biliary function disorders, respiratory disorders such as snoring or sleep apneas and cardiovascular/central nervous system disorders such as stroke. More specifically, the present invention relates to substituted 4-phenyl-tetrahydroisoquinolines, derivatives thereof and compositions containing them formulated in combination with other compounds which also regulate the intracellular pH environment such as inhibitors of carbonic anhydrase and inhibitors of the transport systems that carry bicarbonate ions, such as of the sodium-bicarbonate co-transporter (NBC) or the sodium-dependent chloride-bicarbonate exchanger.

Substituted 4-phenyltetrahydroisoquinolines, pharmaceutical compositions thereof, methods for their preparation and therapeutic use

The present invention comprises compounds and compositions comprising substituted thiophene derivatives with the following backbone structure:  The compounds of this type are of useful in the treatment of various disorders, such as, respiratory disorders and snoring, acute and chronic disorders, disorders induced by ischemic and/or reperfusion events and by proliferative or fibrotic events, disorders of the central nervous system and lipid metabolism, diabetes, blood coagulation and infection by parasites.

Substituted thiophenes: compositions, processes of making, and uses in disease treatment and diagnosis

Host cells expressing HM74 were used to obtain furosemide-like molecules with agonist activity having the following structure formula: 

Furosemide modulators of HM74

Substituted thiophenes, processes for their preparation, their use as medicament or diagnostic agent. The substituted thiophene derivatives have the following backbone structure: Medicaments comprising compounds of this type are of use for preventing or treating various disorders, such as, respiratory disorders and snoring, acute and chronic disorders, disorders induced by ischemic and/or reperfusion events and by proliferative or fibrotic events, disorders of the central nervous system and lipid metabolism, diabetes, blood coagulation and infection by parasites.

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 

Substituted 2-aminoimidazoles, process for their preparation, their use as medicament or diagnostic aid

Substituted 4-phenyltetrahydroisoquinolines of formula I, process for their preparation, their use as a medicament and medicaments containing them.  The compounds of formula I can be used, among other uses, in the event of renal disorders such as acute or chronic renal failure, in the event of disorders of biliary function, in the event of respiratory disorders such as snoring or sleep apneas or in the event of stroke.

Composition, process of making, and medical use of substituted 4-phenyltetrahydroisoquinolines

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.

Substituted imidazolidines, process for their preparation, and their use as a medicament or diagnostic, and medicament comprising them

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Hofheim, Germany

Hans-Jochen Lang