# US 2014/0194440 A1 · 5,6-disubstituted oxindole-derivatives and use thereof for treating vasopressin-dependent diseases

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- Number: US 2014/0194440 A1
- Document ID: US20140194440A1
- Status: Published application
- Kind: A1
- Application number: 14/040,412
- Filed: 2013-09-27
- Published: 2014-07-10
- Earliest claimed: 2007-12-07
- Assignees: AbbVie Deutschland GmbH & Co. KG
- Applicants: Abbvie Deutschland GmbH & Co KG
- Inventors: Wilfried Braje; Thorsten Oost; Astrid Netz; Wolfgang Wernet; Liliane Unger; Wilfried Hornberger; Wilfried Lubisch
- Web page: https://patentgrep.com/patent/US20140194440A1

## CPC

- C07D 401/14: containing three or more hetero rings
- 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 1/08: for nausea, cinetosis or vertigo; Antiemetics
- A61P 1/12: Antidiarrhoeals
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 7/00: Drugs for disorders of the blood or the extracellular fluid
- A61P 7/02: Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
- A61P 7/10: Antioedematous agents; Diuretics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 9/12: Antihypertensives
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 13/00: Drugs for disorders of the urinary system
- A61P 13/12: of the kidneys
- A61P 25/00: Drugs for disorders of the nervous system
- 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 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention relates to novel 5,6-disubstituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the manufacture of a medicament.

## Claims

### Claim 1

A compound of the formula I
in which
R1 and R2 are independently of one another hydrogen, C1-C3-alkyl, C1-C3-fluoroalkyl, C1-C3-alkoxy, C1-C3-fluoroalkoxy, halogen or CN;
R3 is hydrogen or C1-C4-alkyl;
R4 is ethoxy, fluorinated ethoxy or isopropoxy;
R5 is hydrogen or methyl;
R6 is Br, Cl, F or CN;
R7 is Cl, F or CN;
R8 and R9 are independently of one another C1-C3-alkyl or C1-C3-fluoroalkyl;
X1 is O, NH or CH2;
X2 and X3 are N or CH, with the proviso that X2 and X3 are not simultaneously N;
X4 is N or CH;
a and b are independently of one another 0, 1 or 2; and
m, n, o and p are independently of one another 1, 2 or 3;
and their pharmaceutically acceptable salts and prodrugs thereof.

### Claim at position 2

-47. (canceled)

### Claim 48 (depends on 1)

A method for the treatment of vasopressin-dependent diseases, the method comprising administering a compound of claim 1 or a pharmaceutically acceptable salt thereof to a subject in need thereof.

### Claim 49 (depends on 1)

A method for the treatment of diseases selected from hypertension, pulmonary hypertension, heart failure, myocardial infarction, coronary spasm, unstable angina, PTCA (percutaneous transluminal coronary angioplasty), ischemias of the heart, impairments of the renal system, edemas, renal vasospasm, necrosis of the renal cortex, hyponatremia, hypokalemia, Schwartz-Bartter syndrome, impairments of the gastrointestinal tract, gastritic vasospasm, hepatocirrhosis, gastric and intestinal ulcers, emesis, emesis occurring during chemotherapy, travel sickness, diabetes, insulin resistance, nocturnal enuresis, incontinence, and diseases in which impairments of blood clotting occur, and/or for delaying micturition, the method comprising administering a compound of claim 1 or a pharmaceutically acceptable salt thereof to a subject in need thereof.

### Claim 50 (depends on 1)

A method for the treatment of behavioral diseases selected from affective disorders, depressive disorders, psychoses, psychotic disorders, anxiety disorders, stress-dependent anxiety disorders, sleep disorders, childhood onset mood disorders, Cushing's syndrome, memory impairment, Alzheimer's disease, vasomotor symptoms, thermoregulatory dysfunctions, schizophrenia, and stress-related diseases or disorders, the method comprising administering a compound of claim 1 or a pharmaceutically acceptable salt thereof to a subject in need thereof.

### Claim 51 (depends on 1)

A method for treatment of drug or pharmaceutical dependencies and/or mediated by other actors of stress caused by withdrawal of one or more factors mediating the dependence; and/or of stress-induced relapses into drug or pharmaceutical dependencies and/or dependencies mediated by other factors, the method comprising administering a compound of claim 1 or a pharmaceutically acceptable salt thereof to a subject in need thereof.