Invention Grant
US09408840B2 Compounds and methods for inhibiting NHE-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorder
有权
用于抑制NHE介导的止痒剂用于治疗与流体滞留或盐过载和胃肠道疾病相关的疾病的化合物和方法
- Patent Title: Compounds and methods for inhibiting NHE-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorder
- Patent Title (中): 用于抑制NHE介导的止痒剂用于治疗与流体滞留或盐过载和胃肠道疾病相关的疾病的化合物和方法
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Application No.: US14592200Application Date: 2015-01-08
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Publication No.: US09408840B2Publication Date: 2016-08-09
- Inventor: Noah Bell , Christopher Carreras , Dominique Charmot , Jeffrey W. Jacobs , Michael Robert Leadbetter , Marc Navre
- Applicant: Ardelyx, Inc.
- Applicant Address: US CA Fremont
- Assignee: Ardelyx, Inc.
- Current Assignee: Ardelyx, Inc.
- Current Assignee Address: US CA Fremont
- Agency: Cooley LLP
- Agent J. Dean Farmer; Serge R. Banini
- Main IPC: A61K31/18
- IPC: A61K31/18 ; A61K31/4725 ; A61K31/472 ; A61K31/517 ; A61K31/662 ; A61K31/675 ; A61K45/06 ; C07C311/29 ; C07D217/04 ; C07D217/14 ; C07D401/12 ; C07F9/38 ; C07F9/576 ; C07F9/6558 ; C07D217/16 ; C07D215/14 ; C07F9/60

Abstract:
The present disclosure is directed to compounds of the structure (X): CoreL-NHE)n (X) wherein: n is 2 or 3; NHE has the structure wherein: R1 is H or —SO2—NR7R8—; R2 is selected from H, —NR7(CO)R8, —SO2—NR7R8— and —NR7R8; R3 is hydrogen; R7 is hydrogen; R8 is a bond linking to L; L is a polyalkylene glycol linker; and Core has the following structure: wherein: X is selected from the group consisting of a bond, —O—, —NH—, NHC(═O)—, —NHC(═O)NH— and —NHSO2—; and Y is selected from the group consisting of a bond, optionally substituted C1-6 alkylene, optionally substituted benzene, pyridinyl, a polyethylene glycol linker and —(CH2)1-6O(CH2)1-6—, and methods of using such compounds for the treatment of irritable bowel syndrome, chronic kidney disease and end-stage renal disease.
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