IP Library › Granted Patent US 7,452,862
Granted Patent B2
US 7,452,862 · App. 10/911,221 · Granted Nov 18, 2008

Conformationally-controlled biologically active macrocyclic small molecules as motilin antagonists or ghrelin agonists

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Quick Facts
Patent No.
US 7,452,862
App. No.
10/911,221
Granted
Nov 18, 2008
Kind
B2
Abstract

Novel spatially-defined macrocyclic compounds containing specific conformational control elements are disclosed. Libraries of these macrocycles are then used to select one or more macrocycle species that exhibit a specific interaction with a particular biological target. In particular, compounds according to the invention are disclosed as agonists or antagonists of a mammalian motilin receptor and a mammalian ghrelin receptor.

Claims (161)

1. A compound having the structure of formula II:

wherein W, A 1 , A 2 , A 3 and T are defined as below with the NH of A 1 bonded to T, the C═O of A 1 bonded to the NH of A2, the C═O of A2 bonded to the NH of A 3, the C═O of A 3 bonded to W, and (W) and (A 1 ) indicate the site of bonding of T to W and A 1 , respectively:

W

A 1

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

W

A 2

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

W

A 3

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

NH

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W

T

NH

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NH

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NH

NH

NH

2. An antagonist of a mammalian motilin receptor having the following structure:

3. An agonist of a mammalian ghrelin receptor having the following structure:

4. A compound having a structure selected from the following:

Assignments (2)
RELEASE OF PATENT SECURITY INTERESTS RECORDED AT REEL 044949, FRAME 0634 Recorded Nov 16, 2023
From: DEUTSCHE BANK AG NEW YORK BRANCH, AS COLLATERAL AGENT
To: MALLINCKRODT INTERNATIONAL FINANCE S.A.; MALLINCKRODT CB LLC; MALLINCKRODT FINANCE GMBH; MALLINCKRODT US HOLDINGS LLC (F/K/A MALLINCKRODT US HOLDINGS INC.); MALLINCKRODT CARRIBEAN, INC.; MALLINCKRODT US POOL LLC; MNK 2011 LLC (F/K/A MALLINCKRODT INC.); LUDLOW LLC (F/K/A LUDLOW CORPORATION); CNS THERAPEUTICS, INC.; MALLINCKRODT ENTERPRISES HOLDINGS LLC (F/K/A MALLINCKRODT ENTERPRISES HOLDINGS, INC.); MALLINCKRODT ENTERPRISES LLC; MALLINCKRODT LLC; LAFAYETTE PHARMACEUTICALS LLC; LIEBEL-FLARSHEIM COMPANY LLC; MALLINCKRODT BRAND PHARMACEUTICALS LLC (F/K/A MALLINCKRODT BRAND PHARMACEUTICALS, INC.); MALLINCKRODT VETERINARY, INC.; MALLINCKRODT US HOLDINGS LLC; IMC EXPLORATION COMPANY; MEH, INC.; MALLINCKRODT HOSPITAL PRODUCTS IP UNLIMITED COMPANY (F/K/A MALLINCKRODT HOSPITAL PRODUCTS IP LIMITED); MALLINCKRODT ARD IP UNLIMITED COMPANY (F/K/A MALLINCKRODT ARD IP LIMITED); OCERA THERAPEUTICS LLC (F/K/A OCERA THERAPEUTICS, INC.); SPECGX LLC; STRATATECH CORPORATION; SUCAMPO PHARMA AMERICAS LLC; VTESSE LLC (F/K/A VTESSE INC.); MALLINCKRODT PHARMACEUTICALS IRELAND LIMITED; MALLINCKRODT PHARMA IP TRADING UNLIMITED COMPANY (F/K/A MALLINCKRODT PHARMA IP TRADING D.A.C.); INFACARE PHARMACEUTICAL CORPORATION; ST SHARED SERVICES LLC; THERAKOS, INC.; IKARIA THERAPEUTICS LLC; INO THERAPEUTICS LLC
Reel/Frame 065610/0460 →
NOTICE OF GRANT OF SECURITY INTEREST IN INTELLECTUAL PROPERTY Recorded Dec 22, 2017
From: OCERA THERAPEUTICS, INC.
To: DEUTSCHE BANK AG NEW YORK BRANCH, AS COLLATERAL AGENT
Reel/Frame 044949/0634 →