Novartis Ag

The Scripps Research Institute

Other

Sandoz Ag

Erwin Paul Schreiner

Kyriacos Costa Nicolaou

Wilhelm Stahl

Peter Emmanuel Maligres

Chan-Kou Hwang

Adrian Leonard Smith

Philipp Krastel

Esther Schmitt

Wei-Min Dai

Josef Gottfried Meingassner

Andreas Billich

Peter Nussbaumer

Marijan Stefinovic

Brigitta-Maria Liechty

Toshio Suzuki

Sebastian V Wendeborn

Philipp Lehr

Nolwenn Martin

Barbara Wolff-Winiski

Ingeborg Schuster

Sebastian V Wenderborn

Robert D Groneberg

Amarylla Horvath

Herbert Silberberger

The present application relates to cyclic depsipeptides, or derivatives thereof, having the structure of formula (I), and uses thereof, e.g. as inhibitors of kallikrein 7 and human neutrophil elastase.

Cyclic depsipeptides

The present application relates to cyclic depsipeptides of Formula I: or derivatives thereof, wherein X, A, A, A, A, A, Aand Aare defined herein. The cyclic depsipeptides of Formula I are inhibitors of kallikrein 7 and thus can be employed for the treatment of kallikrein-7 dependent diseases.

Use of cyclic depsipeptides to inhibit kallikrein 7

A compound of formula wherein Ris haloalkyl, alkenyl, phenyl, thienyl, pyridine, benzthiazolyl, chromanyl (1,2-dihydrobenzopyranyl) or (C)aryl, and Ror Rindependently of each other are substituted (C)cycloalkyl, a substituted bridged cycloalkyl system, substituted piperidine, substituted tetrahydropyridine, or a substituted bridged heterocyclic system, useful as a pharmaceutical.

Acylsulfonamides as inhibitors of steroid sulfatase

N-(4,5,6,7-tetrahydro-thiazolo-[5,4-c]pyridin-2-yl)-(C)arylsulfonamides, wherein the nitrogen atom of the pyridine is substituted, and wherein the pyridine ring is optionally bridged, useful as a pharmaceutical related to steroid sulfatase 

N-sulfonylaminothiazole

Benzoxa- and benzthiazoles substituted at the 2 position and carrying a sulfamic acid ester group bound via oxygen to the phenyl part of the ring structure, such as the compounds of formula (I) wherein the symbols have various significances, possess interesting pharmacological activity. They can be prepared by sulfamoylation of a corresponding compound carrying a hydroxy group on the phenyl part of the ring structure, or by N-substitution. They are indicated for use as steroid sulfatase inhibitors in the prevention and treatment of illnesses responsive to steroid sulfatase inhibition, such as acne.

Benzoxa- and benzthiazoles

Chromanone and thiochromanone compounds

A fused ring system compound is disclosed that contains an epoxide group on one side of the fused rings and an enediyne macrocyclic ring on the other side of the fused rings. The compounds have DNA-cleaving, antimicrobial and tumor growth-inhibiting properties. Chimeric compounds having the fused ring system compound as an aglycone bonded to (i) a sugar moiety as the oligosaccharide portion or (ii) a monoclonal antibody or antibody combining site portion thereof that immunoreacts with target tumor cells are also disclosed. Compositions containing a compound or a chimer are disclosed, as are methods of preparing a compound.

Dynemicin analogs: syntheses, methods of preparation and use

Intermediates useful in preparing the calicheamicin and esperamicin oligosaccharides, and particularly the sulfur- and O-substituted hydroxylamine-containing B ring of both oligosaccharides, are disclosed as are methods of making and using the same, including the preparation of chimeric antibiotics using the same.

Saccharide intermediates in the formation of the calicheamicin and

Dynemicin analogs: synthesis, methods of preparation and use

Growing community of inventors

Vienna, Austria

Erwin Paul Schreiner