The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Jul. 04, 2017

Filed:

Aug. 05, 2009
Applicants:

Daniel Obrecht, Bättwil, CH;

Philipp Ermert, Allschwil, CH;

Said Oumouch, Mulhouse, FR;

Franck Lach, Les Grandes Loges, FR;

Anatol Luther, Binzen, DE;

Karsten Marx, Basel, CH;

Kerstin Möhle, Wettswil, CH;

Inventors:

Daniel Obrecht, Bättwil, CH;

Philipp Ermert, Allschwil, CH;

Said Oumouch, Mulhouse, FR;

Franck Lach, Les Grandes Loges, FR;

Anatol Luther, Binzen, DE;

Karsten Marx, Basel, CH;

Kerstin Möhle, Wettswil, CH;

Assignee:

POLYPHOR AG, Allschwil, CH;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D 273/02 (2006.01); A61K 31/407 (2006.01); C07D 273/00 (2006.01); A61K 31/4985 (2006.01); A61K 31/437 (2006.01); C07D 498/04 (2006.01); C07D 497/18 (2006.01); C07D 498/18 (2006.01);
U.S. Cl.
CPC ...
C07D 498/04 (2013.01); A61K 31/407 (2013.01); A61K 31/437 (2013.01); A61K 31/4985 (2013.01); C07D 497/18 (2013.01); C07D 498/18 (2013.01);
Abstract

Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of type (I) are constituted by three distinct building blocks: an aromatic template a, a conformation modulator b and a spacer moiety c as detailed in the description and the claims. Macrocycles of type (I) are readily manufactured by parallel synthesis or combinatorial chemistry. They are designed to interact with specific biological targets. In particular, they show agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT(5-HTreceptor), and on the prostaglandin F2•receptor (FP receptor). They are thus potentially useful for the treatment of hypomotility disorders of the gastrointestinal tract such as diabetic gastroparesis and constipation type irritable bowl syndrome; of CNS related diseases like migraine, schizophrenia, psychosis or depression; of ocular hypertension such as associated with glaucoma and preterm labour.


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