# US 11,298,363 B2 · Triazolobenzazepines as vasopressin V1a receptor antagonists

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- Number: US 11,298,363 B2
- Document ID: US11298363B2
- Status: Granted
- Kind: B2
- Application number: 16/954,085
- Filed: 2018-12-14
- Published: 2021-08-26
- Granted: 2022-04-12
- Earliest claimed: 2017-12-15
- Assignees: Richter Gedeon Nyrt.
- Applicants: Richter Gedeon Nyrt.
- Inventors: Ferenc Baska; Éva Bozó; Imre Bata; Krisztina Szondiné Kordás; Krisztina Vukics
- Web page: https://patentgrep.com/patent/US11298363B2

## CPC

- A61K 31/55: having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/24: Antidepressants
- C07D 223/06: with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms (halogen atoms C07D223/04)
- C07D 223/10: attached in position 2
- C07D 487/04: Ortho-condensed systems
- C07D 487/14: Ortho-condensed systems
- C07D 491/20: Spiro-condensed systems
- C07D 519/00: Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
- 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
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

The present invention relates to 5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine derivatives of general formula (I) and/or salts thereof and/or geometric isomers thereof and/or stereoisomers thereof and/or enantiomers thereof and/or racemates thereof and/or diastereomers thereof and/or biologically active metabolites thereof and/or prodrugs thereof and/or solvates thereof and/or hydrates thereof and/or polymorphs thereof which are centrally and/or peripherally acting V1a receptor modulators, particularly V1a receptor antagonists. Additional subject of the present invention is the process for the preparation of the compounds and the intermediates of the preparation process as well. The invention also relates to the pharmaceutical compositions containing the compounds or together with one or more other active substances, as well as to the use in the treatment and/or prophylaxis of a disease or condition associated with V1a receptor function.

## Claims

### Claim 1

A compound of general formula (I)
wherein
ring A is a cycloalkyl or heterocyclyl group;
Y is —O—, —C(O)—, —CH2—, —NH—, —C1-4alkyl-N(R18)— or bond if ring B is present; or —N(C1-4alkyl)2, C(O)OC1-4alkyl, C1-4alkyl optionally substituted with halogen, C1-4alkoxy group or halogen if ring B is absent;
ring B is absent or is an optionally substituted heteroaryl, aryl or heterocyclyl group;
or B—Y-A- jointly represents a 3H-spiro[2-benzofuran-1,4′-piperidin-1′-yl]; or
R1 is a hydrogen, halogen, C1-4alky, C1-4alkoxy, CF3 or CN;
R2 is a hydrogen or C1-4alkyl group;
R3 is a NR4R5, OR6 group or halogen;
or R2 and R3 jointly represent —O—(CH2)m—O—, oxo or ═N—OH group;
R4 and R5 is independently a hydrogen; C1-4alkyl optionally substituted with OH, halogen, cycloalkyl, optionally substituted aryl or NR8R9 group; Cy1; C(O)R7; —S(O2)R10 or C2-4alkynyl group;
or R4 and R5 taken together with the N to which they are attached form a heterocycle;
R6 is a hydrogen; C1-4alkyl optionally substituted with OH, halogen, Cy2, C1-4alkoxy, —S(O)2-C1-4alkyl or NR11R12 group; C(O)R13; Si(CH3)2-t-butyl or C2-4alkynyl group;
R7 is a C1-4alkyl optionally substituted with OH, CN, halogen, Cy3 or NR11R12 group; C1-4alkoxy, C2-4alkenyl, Cy3 or N(C1-4alkyl)2 group;
R8 and R9 is independently a hydrogen, C1-4alkyl or C(O)OR21 group;
R10 is a C1-4alkyl, OH or NR14R15 group;
R11 and R12 is independently a hydrogen or C1-4alkyl group;
or R11 and R12 taken together with the N to which they are attached form an optionally substituted heterocycle;
R13 is a C1-4alkyl optionally substituted with CN or NR19R20 group; Cy3 or NR16R17 group;
R14 and R15 is independently a hydrogen or C1-4alkyl group;
R16 and R17 is independently a hydrogen, C1-4alkyl, or optionally substituted aryl group;
or R16 and R17 taken together with the N to which they are attached form a heterocycle;
R18 and R21 is a hydrogen or C1-4alkyl group;
R19 and R20 is independently a hydrogen or C1-4alkyl group;
Cy1 is an optionally substituted cycloalkyl, heterocyclyl or heteroaryl group;
Cy2 is an optionally substituted aryl or cycloalkyl group;
Cy3 is an optionally substituted aryl, cycloalkyl, heterocyclyl or heteroaryl group;
X is a C1-4alkyl, aryl or heteroaryl group;
Z is a C1-4alkyl group;
m is 2, 3, 4 or 5
and/or salts thereof and/or geometric isomers thereof and/or stereoisomers thereof and/or enantiomers thereof and/or racemates thereof and/or diastereomers thereof and/or biologically active metabolites thereof and/or prodrugs thereof and/or solvates thereof and/or hydrates thereof and/or polymorphs thereof.

### Claim 2 (depends on 1)

The compound according to claim 1, wherein R1 is a hydrogen, fluorine, chlorine, bromine, methyl, methoxy, CF3 or CN.

### Claim 3 (depends on 1)

The compound according to claim 1, wherein
ring A is a 3- to 6-membered saturated carbocyclic group or a 4- to 7-membered saturated heterocycle containing 1 or 2 N;
ring B is absent or is an optionally substituted 6- or 5-membered mono-heteroaryl group, 6- to 10-membered aromatic carbocycle, or 4- to 7-membered saturated, monocyclic, bicyclic, fused and/or bridged heterocycle containing 1, 2 or 3 heteroatoms selected from O, S or N; or B—Y-A- jointly represents a 3H-spiro[2-benzofuran-1,4′-piperidin-1′-yl]; or
X is an isopropyl group
Z is a methyl group.

### Claim 4 (depends on 1)

The compound according to claim 1, wherein ring A is a 4- to 6-membered saturated carbocyclic group or a 4- to 7-membered saturated heterocycle containing 1 or 2 N attached via a ring nitrogen to Y or to the triazole ring of the 5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine core.

### Claim 5 (depends on 1)

The compound according to claim 1, wherein ring A is cyclohexyl, Y is —O—, ring B is pyridin-2-yl and R1 is chlorine.

### Claim 6 (depends on 1)

The compound according to claim 1, wherein
R2 is a hydrogen or C1-4alkyl group;
R3 is a NR4R5 group;
R4 and R5 is independently a hydrogen; C1-4alkyl optionally substituted with OH, halogen, cycloalkyl, optionally substituted aryl or NR8R9 group; Cy1; C(O)R7; —S(O2)R10 or C2-4alkynyl group,
or R4 and R5 taken together with the N to which they are attached form a heterocycle;
R7 is a C1-4alkyl optionally substituted with OH, CN, halogen, Cy3 or NR11R12 group; C1-4alkoxy, C2-4alkenyl, Cy3 or N(C1-4alkyl)2 group;
R8 and R9 is independently hydrogen, C1-4alkyl or C(O)OR21 group;
R10 is a C1-4alkyl, OH or NR14R15 group;
R11 and R12 is independently a hydrogen or C1-4alkyl group;
or R11 and R12 taken together with the N to which they are attached form an optionally substituted heterocycle:
R14 and R15 is independently a hydrogen or C1-4alkyl group;
R21 is a hydrogen or C1-4alkyl group;
Cy1 is an optionally substituted cycloalkyl, heterocyclyl or heteroaryl group;
Cy3 is an optionally substituted aryl, cycloalkyl, heterocyclyl or heteroaryl group.

### Claim 7 (depends on 6)

The compound according to claim 6, wherein R2 is a hydrogen and R4 and R5 are independently a hydrogen, or a C1-4alkyl group.

### Claim 8 (depends on 1)

The compound according to claim 1, wherein
R2 is a hydrogen or C1-4alkyl group;
R3 is an OR6 group;
R6 is a hydrogen; C1-4alkyl group optionally substituted with OH, halogen, Cy2, C1-4alkoxy, —S(O)2—C1-4alkyl or NR11R12 group; C(O)R13, Si(CH3)2-t-butyl or C2-4alkynyl group;
R11 and R12 is independently a hydrogen or C1-4alkyl group;
or R11 and R12 taken together with the N to which they are attached form an optionally substituted heterocycle;
R13 is a C1-4alkyl group optionally substituted with CN or NR19R20 group; Cy3 or NR16R17 group;
R16 and R17 is independently a hydrogen, C1-4alkyl or optionally substituted aryl group;
or R16 and R17 taken together with the N to which they are attached form a heterocycle;
R19 and R20 is independently a hydrogen or C1-4alkyl group;
Cy2 is an optionally substituted aryl or cycloalkyl group.

### Claim 9 (depends on 8)

The compound according to claim 8, wherein R2 is a hydrogen and R6 is a hydrogen, or a C1-4alkyl group.

### Claim 10 (depends on 6)

The compound according to claim 6, wherein the absolute configuration of the carbon at position 5 in the 5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine core is (S) or (R).

### Claim 11 (depends on 1)

The compound according to claim 1, wherein R2 and R3 jointly represent —O—(CH2)m—O—, oxo or ═N—OH group, m is 2, 3, 4 or 5.

### Claim 12 (depends on 11)

The compound according to claim 11, wherein R2 and R3 jointly represent —O—(CH2)m—O— and m is 2.

### Claim 13

A compound selected from the group consisting of:
tert-butyl [8-chloro-1-[1-(pyridin-2-yl)piperidin-4-yl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl] carbamate,
8-chloro-1-[1-(pyridin-2-yl)piperidin-4-yl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
N-[8-chloro-[1-(pyridin-2-yl)piperidin-4-yl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl]acetamide,
N-(8-chloro-[1-(pyridin-2-yl)piperidin-4-yl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl)-2-methylpropanamide,
tert-butyl {8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a]benzazepine-5-yl}carbamate,
8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
(5S)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
(5R)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
N-{8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}acetamide,
N-{8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}glycinamide,
N-{(5S)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}glycinamide,
N-{(5R)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}glycinamide,
(2S)-2-amino-N-{(5R)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-2-phenylacetamide,
(2R)-2-amino-N-{(5R)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-2-phenylacetamide,
N-{8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-2-hydroxyacetamide,
3-{8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-1,1-dimethylurea,
N-{8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-N2,N2-dimethylglycinamide,
N-{8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}methanesulfonamide,
N-{8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-N-methylmethanensulfonamide,
N-{8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-N,N-dimethylsulfamide,
8-chloro-N-methyl-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
8-chloro-N,N-dimethyl-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
8-chloro-N-ethyl-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
8-chloro-N-(propan-2-yl)-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
(5S)-8-chloro-N-(propan-2-yl)-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
(5R)-8-chloro-N-(propan-2-yl)-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
8-chloro-N-cyclobutyl-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
8-chloro-N-(oxetan-3-yl)-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-N-(tetrahydro-2H-pyran-4-yl)-5,6-dihydro 4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
8-chloro-N-(4,4-difluorocyclohexyl)-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
8-methoxy-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine hydrochloride,
8-methoxy-N-(propan-2-yl)-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
tert-butyl {1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-8-(trifluoromethyl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}carbamate,
1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-8-(trifluoromethyl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine hydrochloride,
N,N-dimethyl-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-8-(trifluoromethyl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
N-(propan-2-yl)-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-8-(trifluoromethyl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
8-methyl-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
8-methyl-N-(propan-2-yl)-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
8-bromo-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
8-bromo-N-(propan-2-yl)-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
8-chloro-1-(3,3-difluorocyclobutyl)-N-(propan-2-yl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
8-chloro-1-(4,4-difluorocyclohexyl)-N-(propan-2-yl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
8-chloro-1-[trans-4-(trifluoromethyl)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
8-chloro-N-(propan-2-yl)-1-[trans-4-(trifluoromethyl)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
8-bromo-1-[trans-4-(trifluoromethyl)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
8-bromo-N-(propan-2-yl)-1-[trans-4-(trifluoromethyl)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
1′-[trans-4-(pyridin-2-yloxy)cyclohexyl]-8′-(trifluoromethyl)-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-8-(trifluoromethyl)-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5(6H)-one,
1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-8-(trifluoromethyl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-ol,
5-methoxy-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-8-(trifluoromethyl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
5-(cyclopropylmethoxy)-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-8-(trifluoromethyl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
5-{[tert-butyl(dimethyl)silyl]oxy}-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
8′-chloro-1′-[trans-4-(pyridin-2-yloxy)cyclohexyl]-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5(6H)-one,
8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-ol,
(5S)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-ol,
(5R)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-ol,
8-chloro-5-methoxy-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
5-(cyclopropylmethoxy)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
2-({8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}oxy)-N,N-dimethylethanamine,
8′-chloro-1′-[trans-4-(trifluoromethyl)cyclohexyl]-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
8′-bromo-1′-[trans-4-(pyridin-2-yloxy)cyclohexyl]-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
1′-[trans-4-(pyridin-2-yloxy)cyclohexyl]-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
8-bromo-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5(6H)-one,
8-bromo-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-ol,
1′-[trans-4-(pyridin-2-yloxy)cyclohexyl]-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepin]-8′-carbonitrile,
(5S)-8-chloro-N,N-dimethyl-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
(5S)—N-{8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}acetamide,
8′-chloro-1′-[trans-4-(pyridin-2-ylmethyl)cyclohexyl]-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
[trans-4-(8′-chloro-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine]-1′-yl)cyclohexyl](pyrrolidin-1-yl)methanone,
8-chloro-1-[trans-4-(trifluoromethyl)cyclohexyl]-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5(6H)-one,
8-chloro-1-[trans-4-(trifluoromethyl)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-ol,
(cis)-8-(8′-chloro-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepin]-1′-yl)-3-methyl-1-oxa-3-azaspiro[4.5]decan-2-one,
8-chloro-5-methoxy-1-[trans-4-(trifluoromethyl)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
(trans)-8-(8′-chloro-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepin]-1′-yl)-3-methyl-1-oxa-3-azaspiro[4.5]decan-2-one,
N-{(5S)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-N-methylmethanesulfonamide,
(5S)-8-chloro-N-ethyl-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
(5S)-8-chloro-N-methyl-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
8′-chloro-1′-[1-(pyrimidin-2-yl)azetidin-3-yl]-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
N-{(5S)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-4-fluorobenzamide,
8′-bromo-1′-[trans-4-(trifluoromethyl)cyclohexyl]-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
5-(propan-2-ylamino)-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-8-carbonitrile trifluoroacetate,
(5S)-8-chloro-N-(4-fluorobenzyl)-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine-5-amine,
1′-[trans-4-(trifluoromethyl)cyclohexyl]-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine]-8′-carbonitrile,
[trans-4-(8′-bromo-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepin]-1′-yl)cyclohexyl](piperidin-1-yl)methanone,
methyl trans-4-(8-bromo-5-oxo-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-1-yl)cyclohexane carboxilate,
8-bromo-1-[trans-4-(piperidin-1-ylcarbonyl)cyclohexyl]-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5(6H)-one,
8′-chloro-1′-[trans-4-(trifluoromethyl)cyclohexyl]-4′H,6′H-spiro[1,3-dioxane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
1′-[trans-4-(piperidin-1-ylcarbonyl)cyclohexyl]-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepin]-8′-carbonitrile,
8′-chloro-1′-[trans-4-(pyridin-2-yloxy)cyclohexyl]-4′H,6′H-spiro[1,3-dioxane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
8-bromo-1-[trans-4-(trifluoromethyl)cyclohexyl]-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5(6H)-one,
[trans-4-(8-bromo-5-hydroxy-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-1-yl)cyclohexyl](piperidin-1-yl)methanone,
8-bromo-1-[trans-4-(trifluoromethyl)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-ol,
1′-(1,4′-bipiperidin-1′-yl)-8′-chloro-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
tert-butyl [1-(1,4′-bipiperidin-1′-yl)-8-chloro-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl]carbamate,
8′-fluoro-1′-[trans-4-(pyridin-2-yloxy)cyclohexyl]-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
(5S)-8-chloro-N-(4-fluorobenzyl)-N-methyl-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
N-{(5S)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}prop-2-enamide,
(5R)-8-chloro-N-ethyl-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
(5R)-8-chloro-N-methyl-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
(5R)-8-chloro-N,N-dimethyl-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5(6H)-one,
(5S)-8-chloro-5-methoxy-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
(5R)-8-chloro-5-methoxy-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
8-chloro-5-(propan-2-yloxy)-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
8′-chloro-1′-[trans-4-(pyridin-2-yloxy)cyclohexyl]-4′H,6′H-spiro[1,3-dioxepane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-ol,
[trans-4-(8′-chloro-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepin]-1′-yl)cyclohexyl](morpholin-4-yl)methanone
5-methoxy-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
8-fluoro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5(6H)-one,
8-fluoro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-ol,
tert-butyl {8-chloro-1-[trans-4-(morpholin-4-yl)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}carbamate,
8-chloro-1-[trans-4-(morpholin-4-yl)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
8-chloro-1-[trans-4-(morpholin-4-yl)cyclohexyl]-N-(propan-2-yl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
(5r,8r)-8-(8′-chloro-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepin]-1′-yl)-2-(propan-2-yl)-2-azaspiro[4.5]decan-1-one,
(5r,8r)-8-(8-chloro-5-hydroxy-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-1-yl)-2-(propan-2-yl)-2-azaspiro[4.5]decan-1-one,
(5S)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5-(pyrrolidin-1-yl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
N-{(5S)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-2,2-dimethylpropanamide,
N-{(5S)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}cyclopropanecarboxamide,
N-{(5S)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-2-methylpropanamide,
N-{(5S)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}cyclobutanecarboxamide,
(5S)-8-chloro-5-(morpholin-4-yl)-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
N-{(5R)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-2,2-dimethylpropanamide,
N-{(5R)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-2-methylpropanamide,
N-{(5R)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}cyclobutanecarboxamide,
N-{(5R)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}cyclopropanecarboxamide,
(5S)-8-chloro-5-(piperidin-1-yl)-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
(5S)—N-(butan-2-yl)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
(5s,8s)-8-(8′-chloro-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepin]-1′-yl)-2-(propan-2-yl)-2-azaspiro[4.5]decan-1-one,
8-chloro-5-methoxy-1-[trans-4-(morpholin-4-yl)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
8-chloro-5-ethoxy-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
(5R)-8-chloro-5-methoxy-1-[trans-4-(trifluoromethyl)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
(5S)-8-chloro-5-methoxy-1-[trans-4-(trifluoromethyl)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
8-fluoro-5-methoxy-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
8-chloro-N-(propan-2-yl)-1-[1-(pyridin-2-yl)piperidin-4-yl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
2-({8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}oxy)ethanol,
(5S)-8-chloro-N,N-diethyl-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
8-chloro-N-methyl-N-(propan-2-yl)-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
tert-butyl {8-chloro-1-[4-(3-chloropyridin-2-yl)piperazin-1-yl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}carbamate,
tert-butyl 4-(8-chloro-5-methoxy-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-1-yl)piperidine-1-carboxylate,
N-{(5R)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-D-valinamide,
tert-butyl {1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}carbamate,
tert-butyl {8-fluoro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}carbamate,
1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
8-fluoro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
8-fluoro-N-(propan-2-yl)-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
8-fluoro-N,N-dimethyl-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
N,N-dimethyl-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
8′-fluoro-1′-[trans-4-(trifluoromethyl)cyclohexyl]-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
N-(propan-2-yl)-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
N-{(5S)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}tetrahydro-2H-pyran-4-carboxamide,
N-{(5S)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-2-methylbutanamide,
N-{(5S)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-N3,N3-dimethyl-β-alaninamide,
(5S)-8-chloro-N-cyclopentyl-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
8′-chloro-1′-(1′H,3H-spiro[2-benzofuran-1,4′-piperidin]-1′-yl)-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
8-chloro-1-(1′H,3H-spiro[2-benzofuran-1,4′-piperidin]-1′-yl)-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5(6H)-one,
8′-chloro-1′-[4-(pyridin-2-yloxy)piperidin-1-yl]-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
N-{(5S)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-2,2-dimethylbutanamide,
N-{(5S)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-2-hydroxy-2-methylpropanamide,
(5S)-8-chloro-N-ethyl-N-methyl-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
(5S)-8-chloro-N-(2-methylpropyl)-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
8′-chloro-1′-[trans-4-(morpholin-4-yl)cyclohexyl]-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine] hydrochloride,
8-chloro-N,N-dimethyl-1-(1′H,3H-spiro[2-benzofuran-1,4′-piperidin]-1′-yl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
8′-chloro-1′-[4-(3-chloropyridin-2-yl)piperazin-1-yl]-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
(5S)-8-chloro-N-(2,2-dimethylpropyl)-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
[trans-4-(8-chloro-5-methoxy-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-1-yl)cyclohexyl](4-methylpiperazin-1-yl)methanone,
(5R)-8-chloro-5-(morpholin-4-yl)-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
N-{(5R)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}acetamide,
N-{(5R)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-2-hydroxy-2-methylpropanamide,
8-chloro-5-methoxy-1-[1-(tetrahydro-2H-pyran-4-yl)piperidin-4-yl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
8′-chloro-1-[4-(pyridin-2-yl)piperazin-1-yl]-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
8-chloro-1-(1′H,3H-spiro[2-benzofuran-1,4′-piperidin]-1′-yl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-ol,
8-chloro-1-[4-(3-chloropyridin-2-yl)piperidin-1-yl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-ol,
(5R)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5-(pyrrolidin-1-yl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
8-chloro-5-methoxy-1-{1-[(3S)-tetrahydrofuran-3-yl]piperidin-4-yl}-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
(5R)-8-fluoro-5-methoxy-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
(5S)-8-fluoro-5-methoxy-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
8-chloro-5-methoxy-1-{1-[(3R)-tetrahydrofuran-3-yl]piperidin-4-yl}-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
N-{(5R)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-N3,N3-dimethyl-β-alaninamide,
N-{(5R)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}tetrahydro-2H-pyran-4-carboxamide,
8-chloro-1-[4-(pyridin-2-yloxy)piperidin-1-yl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-ol,
8-chloro-5-methoxy-1-[trans-4-(4-methylpiperazin-1-yl)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
8-chloro-5-methoxy-1-[cis-4-(4-methylpiperazin-1-yl)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
8-chloro-5-methoxy-1-[1-(pyridin-3-ylmethyl)pyrrolidin-3-yl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
8-chloro-5-methoxy-1-[1-(pyridin-2-ylmethyl)pyrrolidin-3-yl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
N-{(5R)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-2-cyanoacetamide,
[3-(8-chloro-5-methoxy-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-1-yl)pyrrolidin-1-yl](pyridin-3-yl)methanone,
8′-chloro-1′-{1-[(3R)-tetrahydrofuran-3-yl]piperidin-4-yl}-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
[3-(8-chloro-5-methoxy-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-1-yl)pyrrolidin-1-yl](pyridin-2-yl)methanone,
trans-4-(8′-chloro-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepin]-1′-yl)-N,N-dimethylcyclohexanamine,
8-chloro-5-methoxy-1-(1′H,3H-spiro[2-benzofuran-1,4′-piperidin]-1′-yl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
8-chloro-1-[4-(3-chloropyridin-2-yl)piperazin-1-yl]-5-methoxy-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
N-[trans-4-(8′-chloro-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepin]-1′-yl)cyclohexyl]pyridin-2-amine,
N-{(5R)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-N,N-dimethylethane-1,2-diamine,
8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl acetate,
2-({(5R)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}amino)ethanol,
8-chloro-5-methoxy-1-[4-(pyridin-2-yloxy)piperidin-1-yl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
8′-chloro-1′-(trans-4-methoxy-4-methylcyclohexyl)-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1] benzazepine],
(5S)-8-chloro-N-(cyclopropylmethyl)-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
N-{(5S)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-1-methylpiperidine-4-carboxamide,
N-{(5S)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-2,2,2-trifluoroacetamide,
8-chloro-5-(2-methoxyethoxy)-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
8-chloro-1-(4-methoxy-4-methylcyclohexyl)-N-(propan-2-yl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
8′-chloro-1′-(trans-4-methoxy-4-methylcyclohexyl)-4′H,6′H-spiro[1,3-dioxane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
8′-chloro-1′-(cis-4-methoxy-4-methylcyclohexyl)-4′H,6′H-spiro[1,3-dioxane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
8-chloro-5-fluoro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
8-chloro-5-[2-(methylsulfonyl)ethoxy]-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
8-chloro-N-hydroxy-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5(6H)-imine,
(5S)-8-chloro-N-methyl-N-(prop-2-yn-1-yl)-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
N-{(5S)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-3,3-difluorocyclobutanecarboxamide,
8-chloro-5-(prop-2-yn-1-yloxy)-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl 4,4-difluorocyclohexanecarboxylate,
8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl 3,3-difluorocyclobutanecarboxylate,
N-{(5S)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-4,4-difluorocyclohexanecarboxamide,
8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl cyanoacetate,
8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl N,N-dimethylglycinate,
N-{(5R)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-2,2,2-trifluoroacetamide,
1-[cis-4-(8-chloro-5-methoxy-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-1-yl)cyclohexyl]pyrrolidin-2-one,
1-[trans-4-(8-chloro-5-methoxy-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-1-yl)cyclohexyl]pyrrolidin-2-one,
N-{(5R)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-3,3-difluorocyclobutanecarboxamide,
N-{(5R)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-4,4-difluorocyclohexanecarboxamide,
8-chloro-5-methoxy-1-[cis-4-methoxy-4-(trifluoromethyl)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
8-chloro-5-methoxy-1-[trans-4-methoxy-4-(trifluoromethyl)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
(5S)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-N-(2,2,2-trifluoroethyl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
N-{(5S)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-3-methyloxetane-3-carboxamide,
N-{(5R)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}-3-methyloxetane-3-carboxamide,
trans-4-(8′-chloro-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepin]-1′-yl)-N-(4-methoxybenzyl)cyclohexanamine,
tert-butyl [2-({(5R)-8-chloro-1-[trans-4-(pyridin-2-yloxy)cyclohexyl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-yl}amino)ethyl]carbamate,
8′-chloro-1′-(trans-4-ethoxy-4-ethylcyclohexyl)-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
trans-4-(8′-chloro-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepin]-1′-yl)-N-(4-methoxybenzyl)-N-methylcyclohexanamine,
8′-chloro-1′-[1-(pyridin-3-ylmethyl)pyrrolidin-3-yl]-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
8-chloro-5-methoxy-1-[4-(pyridin-2-yl)piperazin-1-yl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
8-chloro-1-(trans-4-ethyl-4-methoxycyclohexyl)-N,N-dimethyl-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
8-chloro-1-(trans-4-ethoxy-4-methylcyclohexyl)-N,N-dimethyl-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
8′-chloro-1′-[trans-4-methoxy-4-(trifluoromethyl)cyclohexyl]-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
8′-chloro-1′-[cis-4-methoxy-4-(trifluoromethyl)cyclohexyl]-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
8′-chloro-1′-(trans-4-ethoxy-4-methylcyclohexyl)-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
8′-chloro-1′-(trans-4-ethoxy-4-propylcyclohexyl)-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
8′-chloro-1′-[1-(pyridin-2-ylmethyl)pyrrolidin-3-yl]-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
8′-chloro-1′-(cis-4-ethyl-4-methoxycyclohexyl)-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
8′-chloro-1′-(trans-4-ethyl-4-methoxycyclohexyl)-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
8′-chloro-1′-(trans-4-methoxy-4-propylcyclohexyl)-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
8′-chloro-1′-(cis-4-methoxy-4-propylcyclohexyl)-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
8-chloro-1-(trans-4-ethoxy-4-ethylcyclohexyl)-N-(propan-2-yl)-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
8-chloro-1-(trans-4-ethoxy-4-ethylcyclohexyl)-N,N-dimethyl-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-5-amine,
8′-chloro-1′-[(3R)-1-(pyridin-2-ylmethyl)pyrrolidin-3-yl]-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
8-chloro-5-methoxy-1-[(3R)-1-(pyridin-3-ylmethyl)pyrrolidin-3-yl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
8-chloro-5-methoxy-1-[(3R)-1-(pyridin-2-ylmethyl)pyrrolidin-3-yl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
8′-chloro-1′-[(3S)-1-(pyridin-3-ylmethyl)pyrrolidin-3-yl]-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
8′-chloro-1′-[(3R)-1-(pyridin-3-ylmethyl)pyrrolidin-3-yl]-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine],
8-chloro-5-methoxy-1-[(3S)-1-(pyridin-3-ylmethyl)pyrrolidin-3-yl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine,
8′-chloro-1′-[(3S)-1-(pyridin-2-ylmethyl)pyrrolidin-3-yl]-4′H,6′H-spiro[1,3-dioxolane-2,5′-[1,2,4]triazolo[4,3-a][1]benzazepine] and
8-chloro-5-methoxy-1-[(3S)-1-(pyridin-2-ylmethyl)pyrrolidin-3-yl]-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepine.

### Claim 14 (depends on 1)

A pharmaceutical composition comprising therapeutically effective amount of a compound of general formula (I) and/or salt thereof and/or geometric isomer thereof and/or stereoisomer thereof and/or enantiomer thereof and/or racemate thereof and/or diastereomer thereof and/or biologically active metabolite thereof and/or prodrug thereof and/or solvate thereof and/or hydrate thereof and/or polymorph thereof according to claim 1 as active substance and a pharmaceutically acceptable excipient.

### Claim 15 (depends on 1)

A combinational composition comprising therapeutically effective amount of a compound of general formula (I) and/or salt thereof and/or geometric isomer thereof and/or stereoisomer thereof and/or enantiomer thereof and/or racemate thereof and/or diastereomer thereof and/or biologically active metabolite thereof and/or prodrug thereof and/or solvate thereof and/or hydrate thereof and/or polymorph thereof according to claim 1 and one or more other active substances.

### Claim 16 (depends on 14)

A method for treating and/or preventing a disease or condition associated with V1a receptor function comprising administering to a mammal in need of said treating and/or prophylaxis, the pharmaceutical composition of claim 14.

### Claim 17 (depends on 1)

A process for the preparation of a pharmaceutical composition having V1a receptor antagonist activity comprising combining a therapeutically effective amount of a compound of general formula (I) and/or salt thereof and/or geometric isomer thereof and/or stereoisomer thereof and/or enantiomer thereof and/or racemate thereof and/or diastereomer thereof and/or biologically active metabolite thereof and/or prodrug thereof and/or solvate thereof and/or hydrate thereof and/or polymorph thereof according to claim 1 as active substance with pharmaceutically acceptable excipients.

### Claim 18 (depends on 1)

A method for treating and/or preventing a disease or condition associated with V1a receptor function comprising administering to a mammal in need of said treating and/or prophylaxis, a therapeutically effective amount of a compound of general formula (I) and/or salt thereof and/or geometric isomer thereof and/or stereoisomer thereof and/or enantiomer thereof and/or racemate thereof and/or diastereomer thereof and/or biologically active metabolite thereof and/or prodrug thereof and/or solvate thereof and/or hydrate thereof and/or polymorph thereof according to claim 1 alone or with pharmaceutically acceptable excipients.

### Claim 19 (depends on 18)

The method according to claim 18, wherein the disease or condition associated with V1a receptor function is selected from the group consisting of various pathological conditions of the female sex organs, long-standing conditions in blood pressure control, conditions resulting from inappropriate secretion of vasopressin, anxiety, depression, aggression, disorders of the central nervous system where one of the symptoms and/or syndromes of the disease may be related to anxiety, depression, aggression or show comorbidity with them, aggressive behavioural disorders and/or irritability, behavioural hyperactivity disorders, cognitive disorders or other neuropsychiatric disorders.

### Claim 20

A compound selected from the group consisting of:
1 tert-butyl (7-chloro-2-oxo-2,3,4,5-tetrahydro-1H-1-benzazepin-4-yl)carbamate,
tert-butyl-(7-bromo-2-oxo-2,3,4,5-tetrahydro-1H-1-benzazepin-4-yl)carbamate,
tert-butyl-(7-chloro-2-thioxo-2,3,4,5-tetrahydro-11H-1-benzazepin-4-yl)carbamate,
tert-butyl-(7-bromo-2-thioxo-2,3,4,5-tetrahydro-1H-1-benzazepin-4-yl)carbamate,
tert-butyl-(7-chloro-2-(methylsulfanyl)-4,5-dihydro-3H-1-benzazepin-4-yl)carbamate,
7-chloro-1,5-dihydrospiro[1-benzazepine-4,2′-[1,3]dioxolane]-2(3H)-one,
7-bromo-1,5-dihydrospiro[1-benzazepine-4,2′-[1,3]dioxolane]-2(3H)-one,
4-{[tert-butyl(dimethyl)silyl]oxy}-7-chloro-1,3,4,5-tetrahydro-2H-1-benzazepin-2-one,
4-{[tert-butyl(dimethyl)silyl]oxy}-7-chloro-1,3,4,5-tetrahydro-2H-1-benzazepin-2-thione,
7-chloro-4-methoxy-1,3,4,5-tetrahydro-2H-1-benzazepin-2-one, and
7-chloro-4-methoxy-1,3,4,5-tetrahydro-2H-1-benzazepine-2-thione.

### Claim 21 (depends on 18)

The method according to claim 18, further comprising administering one or more additional active substances.