IP Library › Granted Patent US 10,196,423
Granted Patent B2
US 10,196,423 · App. 15/975,172 · Granted Feb 5, 2019

NPR-B agonists

Inventors: Frank Osterkamp (Berlin, DE); Heiko Hawlisch (Berlin, DE); Gerd Hummel (Berlin, DE); Tobias Knaute (Berlin, DE); Ulf Reimer (Berlin, DE); Ulrich Reineke (Berlin, DE); Bernadett Simon (Bonn, DE); Uwe Richter (Berlin, DE); Edgar Specker (Berlin, DE); Markus Woischnik (Berlin, DE); Mark R. Helberg (Arlington, TX)
Assignee: Shire Orphan Therapies GmbH
C07K7/06C07K7/02C07K7/08
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Quick Facts
Patent No.
US 10,196,423
App. No.
15/975,172
Granted
Feb 5, 2019
Kind
B2
Abstract

Disclosed are novel compounds having NPR-B agonistic activity. Preferred compounds are linear peptides containing 8-13 conventional or non-conventional L- or D-amino acid residues connected to one another via peptide bonds.

Claims (35)

1. A compound selected from:

Occ-ala-Nmf-Gly-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:111);

Occ-ala-Phe-Aib-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:119);

Occ-ala-Phe-ala-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:120);

Occ-ala-Phe-Ebc-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:121);

Occ-ala-Mcf-Gly-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:122);

Occ-Sar-Phe-Gly-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:123);

Occ-Gly-Phe-Gly-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:124);

Occ-pro-Nmf-Gly-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:134);

Occ-Az3-Phe-Gly-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:141);

Occ-ala-Thi-Gly-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:148);

Occ-ala-Pcf-Gly-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:149);

Occ-ala-Thk-Gly-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:150);

Occ-ala-Mtf-Gly-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:151);

Occ-ala-Mmf-Gly-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:152);

Occ-ala-Phe-val-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:155); and

Occ-pip-Phe-Gly-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:177).

2. The compound of claim 1 , wherein the compound is selected from:

Occ-ala-Nmf-Gly-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:111);

Occ-ala-Mcf-Gly-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:122);

Occ-Sar-Phe-Gly-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:123);

Occ-Gly-Phe-Gly-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:124);

Occ-pro-Nmf-Gly-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:134);

Occ-Az3-Phe-Gly-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:141);

Occ-ala-Thi-Gly-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:148);

Occ-ala-Pcf-Gly-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:149);

Occ-ala-Thk-Gly-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:150);

Occ-ala-Mtf-Gly-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:151);

Occ-ala-Mmf-Gly-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:152); and

Occ-pip-Phe-Gly-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:177).

3. The compound of claim 1 , wherein the compound is selected from:

Occ-ala-Phe-Aib-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:119);

Occ-ala-Phe-ala-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:120);

Occ-ala-Phe-Ebc-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:121); and

Occ-ala-Phe-val-Leu-Pro-Leu-Asp-Arg-Ile-NH 2 (SEQ ID NO:155).

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 1, 2021
From: SHIRE ORPHAN THERAPIES GMBH
To: TAKEDA PHARMACEUTICAL COMPANY LIMITED
Reel/Frame 055105/0363 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 2, 2018
From: ALCON RESEARCH, LTD.
To: SHIRE ORPHAN THERAPIES GMBH
Reel/Frame 047397/0031 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 2, 2018
From: OSTERKAMP, FRANK; KNAUTE, TOBIAS; RICHTER, UWE; HAWLISCH, HEIKO; REIMER, ULF; SIMON, BERNADETT; HELLBERG, MARK R.; HUMMEL, GERD; REINEKE, ULRICH; SPECKER, EDGAR; WOISCHNIK, MARKUS
To: ALCON RESEARCH, LTD.
Reel/Frame 047397/0075 →
Continuity (6)
Division 15645680 · Jul 10, 2017
Division 14824353 · Aug 12, 2015
Division 14011855 · Aug 28, 2013
Division 12888556 · Sep 23, 2010
Provisional Application 61245960 · Sep 25, 2009
Related Publication 20180334477A1 · Nov 22, 2018