# US 10,370,380 B2 · Octahydropyrrolo[3,4-c]pyrrole derivatives and uses thereof

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- Number: US 10,370,380 B2
- Document ID: US10370380B2
- Status: Granted
- Kind: B2
- Application number: 15/777,219
- Filed: 2016-11-23
- Published: 2018-11-22
- Granted: 2019-08-06
- Earliest claimed: 2015-11-23
- Assignees: Sunshine Lake Pharma Co., Ltd.
- Applicants: Sunshine Lake Pharma Co., Ltd.
- Inventors: Yingjun Zhang; Chuanfei Jin; Ji Zhang
- Web page: https://patentgrep.com/patent/US10370380B2

## CPC

- C07D 487/04: Ortho-condensed systems
- A61K 31/423: condensed with carbocyclic rings
- A61K 31/428: condensed with carbocyclic rings
- A61K 31/4709: Non-condensed quinolines and containing further heterocyclic rings
- A61K 31/517: ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/02: Nutrients, e.g. vitamins, minerals
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 5/00: Drugs for disorders of the endocrine system
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/12: Antihypertensives
- A61P 15/10: for impotence
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/02: for peripheral neuropathies
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 25/06: Antimigraine agents
- A61P 25/08: Antiepileptics; Anticonvulsants
- A61P 25/14: for treating abnormal movements, e.g. chorea, dyskinesia
- A61P 25/16: Anti-Parkinson drugs
- A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- A61P 25/20: Hypnotics; Sedatives
- A61P 25/22: Anxiolytics
- A61P 25/24: Antidepressants
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61P 25/30: for treating abuse or dependence
- A61P 25/36: Opioid-abuse
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 37/02: Immunomodulators
- A61P 39/02: Antidotes
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The invention relates to octahydropyrrolo [3, 4-c] pyrrole derivatives and uses thereof. Compounds and pharmaceutical compositions comprising the compounds provided herein are used for antagonizing orexin receptors. The invention also relates to processes for preparing the compounds and pharmaceutical compositions, and uses thereof in treating or preventing a disease related to orexin receptors.

## Claims

### Claim 1

The compound having Formula (III), or a stereoisomer, a tautomer, an N-oxide, a solvate, a pharmaceutically acceptable salt or a prodrug thereof,
wherein X is —O—, —S—, —NH—, or *—CR9═CR9a—, wherein * refers to an end attached to the benzene ring; and
each R1, R2, R3, R4, R9 and R9a is independently H, D, —CD3, —CN, —NH2, —OH, —NO2, —COOH, —C(═O)NH2, halogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkoxy, C1-6 alkylamino, C1-6 hydroxy-substituted alkyl, (C1-6 alkyl)—C(═O)—, (C1-6 alkoxy)—C(═O)—, (C1-6 alkylamino)—C(═O)—, cycloalkyl, heterocyclyl, aryl or heteroaryl.

### Claim 2 (depends on 1)

The compound of claim 1, wherein each R1, R2, R3, R4, R9 and R9a is independently H, D, —CD3, —CN, —NH2, —OH, —NO2, —COOH, —C(═O)NH2, halogen, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, C1-4 haloalkyl, C1-4 alkoxy, C1-4 haloalkoxy, C1-4 alkylamino, C1-4 hydroxy-substituted alkyl, (C1-4 alkyl)—C(═O)—, (C1-4 alkoxy)—C(═O)— or (C1-4 alkylamino)—C(═O)—.

### Claim 3 (depends on 1)

The compound of claim 1, wherein each R1, R2, R3, R4, R9 and R9a is independently H, D, —CD3, —CN, —NH2, —OH, —NO2, —COOH, —C(═O)NH2, F, Cl, Br, I, methyl, ethyl, n-propyl, isopropyl, —CF3, —CH2CF3, —CF2CF3, methoxy, ethoxy, n-propyloxy, isopropyloxy, —NHCH3, —N(CH3)2 or —CH2OH.

### Claim 4

A compound having one of the following structures or a stereoisomer, a tautomer, an N-oxide, a solvate, a pharmaceutically acceptable salt or a prodrug thereof,

### Claim 5 (depends on 1)

A pharmaceutical composition comprising the compound of claim 1 and optionally, wherein the pharmaceutical composition further comprising a pharmaceutically acceptable carrier, excipient, adjuvant or a combination thereof.

### Claim 6 (depends on 1)

A pharmaceutical combination for use in treating or lessening a disease related to one or more orexin receptors, wherein the pharmaceutical combination comprising the compound of claim 1 as a first active agent; and a medicament different from the compound of claim 1 as the second active agent, wherein the medicament different from the compound of claim 1 is for use in preventing, treating or lessening a disease related to one or more orexin receptors.

### Claim 7 (depends on 1)

A kit for use in treating or lessening a disease related to one or more orexin receptors, wherein the kit comprises:
a first container, wherein the first container is provided with the compound of claim 1 and
optionally, a second container, wherein the second container is provided with a medicament different from the compound of claim 1, wherein the medicament different from the compound of claim 1 is for use in preventing, treating or lessening a disease related to one or more orexin receptors.