DK2513088T3 - Hidtil ukendte derivater af (heterocyklus-tetrahydro-pyridin)-(piperazinyl)-1-alkanon og (heterocyklus-dihydro-pyrrolidin)-(piperazinyl)-1-alkanon og deres anvendelse som inhibitorer af p75 - Google Patents

Hidtil ukendte derivater af (heterocyklus-tetrahydro-pyridin)-(piperazinyl)-1-alkanon og (heterocyklus-dihydro-pyrrolidin)-(piperazinyl)-1-alkanon og deres anvendelse som inhibitorer af p75 Download PDF

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DK2513088T3
DK2513088T3 DK10801663.5T DK10801663T DK2513088T3 DK 2513088 T3 DK2513088 T3 DK 2513088T3 DK 10801663 T DK10801663 T DK 10801663T DK 2513088 T3 DK2513088 T3 DK 2513088T3
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pyridin
compound
dihydro
ethanone
piperazin
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Marco Baroni
Sandrine Delbary-Gossart
Valentina Vercesi
Françoise Bono
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Sanofi Sa
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Claims (13)

1. Forbindelse med formlen (I):
O) hvor: - n betegner 1 eller 2; - n betegner 0 eller 1; - A betegner en kondenseret heterocyklisk gruppe med formlen (Y)
(Y) og B betegner et hydrogenatom; eller A betegner et hydrogenatom; og B betegner en kondenseret heterocyklisk gruppe med formlen (Y)
(Y) hvor den kondenserede heterocykliske gruppe med formlen Y kan være bundet til resten af molekylet via et hvilket som helst af de tilgængelige carbonatomer, og hvor: - U supplerer: - enten en aromatisk eller mættet ring med 6 atomer, der indeholder 1 eller 2 nitrogenatomer, hvor ringen kan være substitueret med et eller to halogenatomer, en eller to (Cl-C4)alkyl- eller (C1-C4)alkoxygrupper, en eller to perfluoralkylgrupper; eller en aromatisk eller mættet ring med 5 atomer, der indeholder et nitrogen-, oxygen- eller svovlatom, hvor ringen kan være substitueret med en eller to (C1-C4)alkylgrupper; - X og XI betegner CH eller N; - R og Ri, der sidder i en hvilken som helst af de tilgængelige stillinger, uafhængigt betegner et hydrogenatom, et halogenatom, en (C1-C4)alkyl- eller (C1-C4)alkoxygruppe, en perfluoralkyl- eller trifluormethoxygruppe, en cyanogruppe, en COOH-, COOalkyl-, CONR3R4- eller NHC0R3-gruppe; - -W- er en nitrogenholdig heterocyklus valgt blandt:
- 1-2 betegner 1 eller 2; - 1-3 betegner 1, 2 eller 3; - R2 betegner en gruppe med formlen:
- hvor R5 og R6, der sidder i en hvilken som helst af de tilgængelige stillinger, uafhængigt betegner et hydrogenatom, et halogenatom, en (C1-C4)alkyl- eller (C1-C4)alkoxygruppe, en trifluormethyl- eller trifluormethoxygruppe, en cyanogruppe, en COOH-, COOalkyl-, COOcycloalkyl-, SOalkyl-, S02alkyl-, CONR3R4-, NR3R4- eller NHC0R3-gruppe; eller en af R5 og R6 kan også betegne en heterocyklus valgt blandt:
- Z betegner et oxygen- eller svovlatom; R3 og R4 betegner et hydrogenatom eller en (Cl — C6)alkylgruppe; i form af en base eller et additionssalt med en syre.
2. Forbindelse ifølge krav 1, hvor - A betegner en kondenseret heterocyklisk gruppe med formlen (Y)
(Y) og B betegner et hydrogenatom; eller A betegner et hydrogenatom; og B betegner en kondenseret heterocyklisk gruppe med formlen (Y)
(Y) hvor den kondenserede heterocyklus med formlen Y kan være bundet til resten af molekylet via et hvilket som helst af de tilgængelige carbonatomer på benzenringen; i form af en base eller et additionssalt med en syre.
3. Forbindelse ifølge et af kravene 1 til 2, hvor R og RI, der sidder i en hvilken som helst af de tilgængelige stillinger, uafhængigt betegner et hydrogenatom, en (C1-C4) alkyl- eller COOalkylgruppe; i form af en base eller et additionssalt med en syre.
4. Forbindelse ifølge et af kravene 1 til 3, hvor: - -W- er en nitrogenholdig heterocyklus valgt blandt:
- R3 og R4 betegner et hydrogenatom eller en methylgruppe; i form af en base eller et additionssalt med en syre.
5. Forbindelse ifølge et af kravene 1 til 4, hvor: - R2 betegner en gruppe med formlen:
R5 og R6, der sidder i en hvilken som helst af de tilgængelige stillinger, uafhængigt betegner et hydrogenatom, en trifluormethylgruppe, en COOH-, COOalkyl- eller COOcycloalkylgruppe; eller en af R5 og R6 kan også betegne en heterocyklus valgt blandt:
- Z betegner et oxygen- eller svovlatom; - R3 og R4 betegner et hydrogenatom eller en methylgruppe; i form af en base eller et additionssalt med en syre.
6. Forbindelse ifølge et hvilket som helst af kravene 1 til 5 valgt blandt: - Forbindelse nr. 1: 1-(4-Benzo[b]thiophen-7-yl-3,6-dihydro- 2H-pyridin-l-yl)-2-(3,5-dimethyl-2,3,5,6-tetrahydro- [1,2']bipyrazinyl-4-yl)-ethanon; - Forbindelse nr. 2: 1-(4-Benzo[b]thiophen-7-yl-3,6-dihydro- 2H-pyridin-l-yl)-2-(8-pyrimidin-2-yl-3,8-diaza- bicyclo[3.2.1]oct-3-yl)-ethanon; - Forbindelse nr. 3: 1-(4-Benzo[b]thiophen-5-yl-3,6-dihydro- 2H-pyridin-l-yl)-2-(8-pyrimidin -2-yl-3,8-diaza- bicyclo[3.2.1]oct-3-yl)-ethanon; - Forbindelse nr. 4: 1-(4-Benzo[b]thiophen-7-yl-3,6-dihydro- 2H-pyridin-l-yl)-2-[(2 S,6R)-2,6-dimethyl-4-(5-trifluormethyl-pyridin-2-yl)-piperazin-l-yl]-ethanon; - Forbindelse nr. 5: 1-(4-Benzo[b]thiophen-5-yl-3,6-dihydro- 2H-pyridin-l-yl)-2-((2 S,5R)-2,5-dimethyl-2,3,5,6-tetrahydro-[1,2']bipyrazinyl-4-yl)-ethanon; - Forbindelse nr. 6: 1-(4-Benzo[b]thiophen-7-yl-3,6-dihydro- 2H-pyridin-l-yl)-2-((2 S,5R)-2,5-dimethyl-2,3,5,6-tetrahydro- [1,2']bipyrazinyl-4-yl)-ethanon; - Forbindelse nr. 7: 1-(4-Benzo[b]thiophen-5-yl-3,6-dihydro- 2H-pyridin-l-yl)-2-[(2S,6R)-2,6-dimethyl-4-(5-trifluormethyl-pyridin-2-yl)-piperazin-l-yl]-ethanon; - Forbindelse nr. 8: 1-(4-Benzo[b]thiophen-7-yl-3,6-dihydro- 2H-pyridin-l-yl)-2-[8-(5-trifluormethyl-pyridin-2-yl)-3,8-diaza-bicyclo[3.2.1]oct-3-yl]-ethanon; - Forbindelse nr. 9: 1-(4-Benzo[b]thiophen-7-yl-3,6-dihydro- 2H-pyridin-l-yl)-2-[(2R,5S)-2,5-dimethyl-4-(5-trifluormethyl-pyridin-2-yl)-piperazin-l-yl]-ethanon; Forbindelse_nr ._1_0: 2-[ (2S, 6R)-2, 6-Dimethyl-4-(5- trifluormethyl-pyridin-2-yl)-piperazin -1-yl]-1-[4-(2-methyl- benzo[b]thiophen-7-yl)-3,6-dihydro-2H-pyridin-l-yl]-ethanon; Forbindelse_nr ._1_1: 2-[ (2S, 6R)-2, 6-Dimethyl-4-(5- trifluormethyl-pyridin-2-yl)-piperazin -1-yl]-1-[4-(2-propyl- benzo[b]thiophen-7-yl)-3,6-dihydro-2H-pyridin-l-yl]-ethanon; - Forbindelse nr. 12: 1-(4-Benzo[b]thiophen-7-yl-3,6-dihydro- 2H-pyridin-l-yl)-2-[5-(5-trifluormethyl-pyridin-2-yl)-2,5-diaza-bicyclo[2.2.1]hept-2-yl]-ethanon; - Forbindelse nr. 13: 1-(4-Benzo[b]thiophen-6-yl-3,6-dihydro- 2H-pyridin-l-yl)-2-[(2R,5S)-2,5-dimethyl-4-(5-trifluormethyl-pyridin-2-yl)-piperazin-l-yl]-ethanon; Forbindelse nr. 14: 1-(4-Benzofuran-7-yl-3,6-dihydro-2H- pyridin-l-yl)-2-[(2R,5S)-2,5-dimethyl-4-(5-trifluormethyl-pyridin-2-yl)-piperazin-l-yl]-ethanon; - Forbindelse nr. 15: 1-[4-(2-Methyl-benzo[b]thiophen-5-yl)- 3.6- dihydro-2H-pyridin-l-yl]-2-(8-pyrimidin-2-yl-3,8-diaza-bicyclo[3.2.1]oct-3-yl)-ethanon; - Forbindelse nr. 16: 1-[4-(2-Methyl-benzo[b]thiophen-5-yl)- 3.6- dihydro-2H-pyridin-l-yl]-2-[4-(5-trifluormethyl-pyridin-2-yl)-piperazin-l-yl]-ethanon; - Forbindelse nr. 17: 4-{2-[4-(2-Methyl-benzo[b]thiophen-5- yl)-3,6-dihydro-2H-pyridin-l-yl]-2-oxo-ethyl}-1-(5- trifluormethyl-pyridin-2-yl)-piperazin-2-on; Forbindelse nr. 18: 2-[(2 S,6R)-2,6-Dimethyl-4-(5- trifluormethyl-pyridin-2-yl)-piperazin -1-yl]-1-[4-(2-methyl-benzo[b]thiophen-5-yl)-3,6-dihydro-2H-pyridin-l-yl]-ethanon; - Forbindelse nr. 19: 1-(4-Benzo[b]thiophen-7-yl-3, 6-dihydro- 2H-pyridin-l-yl)-2-((2S,6R)-2,6-dimethyl-4-quinolein-2-yl-piperazin-l-yl)-ethanon; Forbindelse nr. 20: 1-(4-Quinolin-8-yl-3,6-dihydro-2H- pyridin-l-yl)-2-[4-(5-trifluormethyl-pyridin-2-yl)-piperazin-1-yl]-ethanon; - Forbindelse nr. 21: 1-[4-(2,3-Dihydro-benzo[1,4]dioxin-6-yl)-3, 6-dihydro-2H-pyridin-l-yl]-2-[4-(5-trifluormethyl-pyridin-2-yl)-piperazin-l-yl]-ethanon; - Forbindelse nr. 22; 2-[8-(5-Fluor-pyrimidin-2-yl)-3,8-diaza-bicyclo[3.2.1]oct-3-yl]-1-[4-(2-methyl-benzo[b]thiophen-5-yl)- 3,6-dihydro-2H-pyridin-l-yl]-ethanon; Forbindelse nr. 23: 1-(4-Benzofuran-7-yl-3,6-dihydro-2H-pyridin-l-yl)-2-[8-(5-fluor-pyrimidin-2-yl)-3,8-diaza-bicyclo[3.2.1]oct-3-yl]-ethanon; - Forbindelse nr. 24: 1-[4-(2,3-Dihydro-benzo[1,4]dioxin-6-yl)-3, 6-dihydro-2H-pyridin-l-yl]-2-[8-(5 — fluor-pyrimidin-2- yl)-3, 8-diaza-bicyclo[3.2.1]oct-3-yl]-ethanon; - Forbindelse nr. 25: 2-[8-(5-Fluor-pyrimidin-2-yl)-3,8-diaza-bicyclo [3.2.1]oct-3-yl]-1-(4-thieno[3,2-c]pyridin-4-yl-3,6-dihydro-2H-pyridin-l-yl)-ethanon; Forbindelse nr. 26: 1-(4-Benzofuran-3-yl-3,6-dihydro-2H-pyridin-l-yl)-2-[8-(5-fluor-pyrimidin-2-yl)-3,8-diaza-bicyclo [3.2.1]oct-3-yl]-ethanon; - Forbindelse nr. 27: 2-[8-(5-Fluor-pyrimidin-2-yl)-3,8-diaza-bicyclo [3.2.1]oct-3-yl]-1-[4-(lH-indol-3-yl)-3,6-dihydro-2H-pyridin-l-yl]-ethanon; Forbindelse nr. 28: 1-[4-(6-Fluor-lH-indol-3-yl)-3,6- dihydro-2H-pyridin-l-yl]-2-[8-(5 — fluor-pyrimidin-2-yl)-3,8-diaza-bicyclo[3.2.1]oct-3-yl]-ethanon; - Forbindelse nr. 29: 1-(4-Benzo[b]thiophen-3-yl-3,6-dihydro- 2H-pyridin-l-yl)-2-[8-(5-fluor-pyrimidin-2-yl)-3,8-diaza-bicyclo[3.2.1]oct-3-yl]-ethanon; - Forbindelse nr. 30: 4-{2-[4-(lH-Indol-3-yl)-3,6-dihydro-2H- pyridin-l-yl]-2-oxo-ethyl}-1-(5-trifluormethyl-pyridin-2-yl)-piperazin-2-on; Forbindelse nr. 31: 4-[2-(4-Benzo[b]thiophen-7-yl-3,6- dihydro-2H-pyridin-l-yl)-2-oxo-ethyl]-1-(5-trifluormethyl-pyridin-2-yl)-piperazin-2-on; - Forbindelse nr. 32: 4-[2-(4-Benzofuran-7-yl-3,6-dihydro-2H- pyridin-l-yl)-2-oxo-ethyl]-1-(5-trifluormethyl-pyridin-2-yl)-piperazin-2-on; Forbindelse nr. 33: 1-(4-Benzofuran-7-yl-3,6-dihydro-2H- pyridin-l-yl)-2-[4-(5-trifluormethyl-pyridin-2-yl)-piperazin-1-yl]-ethanon; Forbindelse nr. 34: 1-(4-Benzofuran-7-yl-3,6-dihydro-2H- pyridin-l-yl)-2-[(2S,6R)-2,6-dimethyl-4-(5-trifluormethyl-pyridin-2-yl)-piperazin-l-yl]-ethanon; Forbindelse nr. 35: 1-(4-Benzofuran-7-yl-3,6-dihydro-2H- pyridin-l-yl)-2-((2 S,6R)-2,6-dimethyl-4-pyrimidin-5-yl-piperazin-l-yl)-ethanon; Forbindelse nr. 36: 1-(4-Benzofuran-7-yl-3,6-dihydro-2H- pyridin-l-yl)-2-[(2S,6R)-4-(5-fluor-pyrimidin-2-yl)-2,6-dimethyl-piperazin-l-yl]-ethanon; Forbindelse nr. 37: 1-(4-Benzofuran-7-yl-3,6-dihydro-2H- pyridin-l-yl)-2-[(2 S,6R)-2,6-dimethyl-4-(6-trifluormethyl-pyridin-3-yl)-piperazin-l-yl]-ethanon; - Forbindelse nr. 38: 2-[(2 S,6R)-4-(5-Fluor-pyrimidin-2-yl)- 2,6-dimethyl-piperazin-l-yl]-1-[4-(2-methyl-benzo[b]thiophen- 5-yl)-3,6-dihydro-2H-pyridin-l-yl]-ethanon; Forbindelse_nr ._3_9: 2-[(2S,6R)-2,6-Dimethyl-4-(6- trifluormethyl-pyridin-3-yl)-piperazin -1-yl]-1-[4-(2-methyl- benzo [b]thiophen-5-yl)-3,6-dihydro-2H-pyridin-l-yl]-ethanon; - Forbindelse nr. 40: 2-((2S,6R)-2,6-Dimethyl-4-pyrimidin-5-yl-piperazin-l-yl)-1-[4-(2-methyl-benzo[b]thiophen-5-yl)-3,6-dihydro-2H-pyridin-l-yl]-ethanon; - Forbindelse nr. 41: 1-(4-Benzo[b]thiophen-5-yl-3,6-dihydro- 2H-pyridin-l-yl)-2-((2 S,6R)-2,6-dimethyl-4-pyrimidin-5-yl-piperazin-l-yl)-ethanon; - Forbindelse nr. 42: 1-(4-Benzo[b]thiophen-5-yl-3,6-dihydro- 2H-pyridin-l-yl)-2-[(2 S,6R)-4-(5-fluor-pyrimidin-2-yl)-2,6-dimethyl-piperazin-1-yl]-ethanon; Forbindelse nr. 43: 4-[2-(4-Benzo[b]thiophen-5-yl-3,6- dihydro-2H-pyridin-l-yl)-2-oxo-ethyl]-1-(5-trifluormethyl-pyridin-2-yl)-piperazin-2-on; Forbindelse nr. 44: 1-[4-(2,3-Dihydro-benzo[1,4]dioxin-6- yl)-3,6-dihydro-2H-pyridin-l-yl]-2-[(2S,6R)-4-(5-fluor- pyrimidin-2-yl)-2,β-dimethyl-piperazin-l-yl]-ethanon; - Forbindelse nr. 45: 1-[4-(2,3-Dihydro-benzo[1,4]dioxin-6- yl)-3,6-dihydro-2H-pyridin-l-yl]-2-[(2 S,6R)-2,6-dimethyl-4-(6-trifluormethyl-pyridin-3-yl)-piperazin-l-yl]-ethanon; - Forbindelse nr. 46: 1-(4-Benzo[b]thiophen-5-yl-3,6-dihydro- 2H-pyridin-l-yl)-2-[4-(5-trifluormethyl-pyridin-2-yl)-piperazin-l-yl]-ethanon; - Forbindelse nr. 47: 1-(4-Benzo[b]thiophen-5-yl-3,6-dihydro- 2H-pyridin-l-yl)-2-[(2S,6R)-2,6-dimethyl-4-(6-trifluormethyl-pyridin-3-yl)-piperazin-l-yl]-ethanon; - Forbindelse nr. 48: 5-{ (3 S,5R)-4-[2-(4-Benzo[b]thiophen-4- yl-3, 6-dihydro-2H-pyridin-l-yl)-2-oxo-ethyl]-3,5-dimethyl-piperazin-l-yl}-pyridin-2-carboxylsyre; - Forbindelse nr. 49: 4-{2-[4-(2,3-Dihydro-benzo[1,4]dioxin-6-yl)-3,6-dihydro-2H-pyridin-l-yl]-2-oxo-ethyl}-1-(6- trifluormethyl-pyridin-3-yl)-piperazin-2-on; - Forbindelse nr. 50: 1-(4-Benzo[b]thiophen-7-yl-3,6-dihydro- 2H-pyridin-l-yl)-2-[4-(6-trifluormethyl-pyridin-3-yl)-piperazin-l-yl]-ethanon; - Forbindelse nr. 51; 5-{(3S,5R)-4-[2-(4-Benzofuran-7-yl-3,6- dihydro-2H-pyridin-l-yl)-2-oxo-ethyl]-3,5-dimethyl-piperazin-1-yl}-pyridin-2-carboxylsyremethylester; - Forbindelse nr. 52: 6-{(3S,5R)-4-[2-(4-Benzo[b]thiophen-5- yl-3, 6-dihydro-2H-pyridin-l-yl)-2-oxo-ethyl]-3,5-dimethyl-piperazin-l-yl}-nicotinsyremethylester; Forbindelse nr. 53: 1-(4-Benzo[b]thiophen-7-yl-3,6-dihydro-2H- pyridin-l-yl)-2-[(2S,6R)-4-(5-fluor-pyrimidin-2-yl)-2,6-dimethyl-piperazin-l-yl]-ethanon; - Forbindelse nr. 54: 1-(4-Benzo[b]thiophen-7-yl-3,6-dihydro- 2H-pyridin-l-yl)-2-[(2 S,6R)-2,6-dimethyl-4-(6-trifluormethyl-pyridin-3-yl)-piperazin-l-yl]-ethanon; - Forbindelse nr. 55: 1-(4-Benzo[b]thiophen-7-yl-3,6-dihydro- 2H-pyridin-l-yl)-2-((2 S,6R)-2,6-dimethyl-4-pyrimidin-5-yl-piperazin-l-yl)-ethanon; - Forbindelse nr. 56: 6-{(3S,5R)-4-[2-(4-Benzo[b]thiophen-5- yl-3,6-dihydro-2H-pyridin-l-yl)-2-oxo-ethyl]-3,5-dimethyl-piperazin-l-yl}-nicotinsyre; - Forbindelse nr. 57: 6-{ (3 S,5R)-4-[2-(4-Benzofuran-7-yl-3,6- dihydro-2H-pyridin-l-yl)-2-oxo-ethyl]-3,5-dimethyl-piperazin-1-yl}-nicotinsyre; - Forbindelse nr. 58: 6-{ (3 S,5R)-4-[2-(4-Benzo[b]thiophen-7- yl-3,6-dihydro-2H-pyridin-l-yl)-2-oxo-ethyl]-3,5-dimethyl-piperazin-l-yl}-nicotinsyremethylester; - Forbindelse nr. 59: 6-{(3 S,5R)-4-[2-(4-Benzo[b]thiophen-7- yl-3,6-dihydro-2H-pyridin-l-yl)-2-oxo-ethyl]-3,5-dimethyl-piperazin-l-yl}-nicotinsyre; - Forbindelse nr. 60: 4-[2-(4-Benzofuran-5-yl-3,6-dihydro-2H- pyridin-l-yl)-2-oxo-ethyl]-1-(5-trifluormethyl-pyridin-2-yl)-piperazin-2-on; Forbindelse nr. 61: 6-((3S,5R)-3,5-Dimethyl-4-{2-[4-(2- methyl-benzo[b]thiophen-5-yl)-3,6-dihydro-2H-pyridin-l-yl]-2-oxo-ethyl}-piperazin-l-yl)-nicotinsyremethylester; Forbindelse nr. 62: 6-((3S,5R)-3,5-Dimethyl-4-{2-[4-(2- methyl-benzo[b]thiophen-5-yl)-3,6-dihydro-2H-pyridin-l-yl]-2-oxo-ethyl}-piperazin-l-yl)-nicotinsyre; Forbindelse nr. 63: 1-(5-Benzofuran-7-yl-3,6-dihydro-2H- pyridin-l-yl)-2-[ (2 S,6R)-2,6-dimethyl-4-(5-trifluormethyl-pyridin-2-yl)-piperazin-l-yl]-ethanon; - Forbindelse nr. 64: 6-{ (3S,5R)-4-[2-(4-Benzofuran-7-yl-3, 6- dihydro-2H-pyridin-l-yl)-2-oxo-ethyl]-3,5-dimethyl-piperazin-l-yl } -nicotinsyreethylester; - Forbindelse nr. 65: 6-{3-[2-(4-Benzofuran-7-yl-3, 6-dihydro- 2H-pyridin-1-yl)-2-oxo-ethyl]-3,8-diaza-bicyclo[3.2.1]oct-8- yl}-nicotinsyremethylester; Forbindelse nr. 66: 7-(1-{2-[(2S,6R)-2,6-Dimethyl-4-(5- trifluormethyl-pyridin-2-yl)-piperazin-l-yl]-acetyl}—1,2,3,6-tetrahydro-pyridin-4-yl)-benzo[b]thiophene-2-carboxylsyremethylester; Forbindelse nr, 67: 5-(l-{2-[(2S,6R)-2,6-Dimethyl-4-(5- trifluormethyl-pyridin-2-yl)-piperazin-l-yl]-acetyl}-1,2,3,6-tetrahydro-pyridin-4-yl)-benzo[b]thiophene-2-carboxylsyremethylester; Forbindelse_nr ._6_8: 2-[ (2S, 6R) -2, 6-Dimethyl-4-(5- trifluormethyl-pyridin-2-yl)-piperazin -1-yl]-1-[4-(2-propyl- benzo[b]thiophen-5-yl)-3,6-dihydro-2H-pyridin-l-yl]-ethanon; - Forbindelse nr. 69: 6-{3-[2-(4-Benzo[b]thiophen-7-yl-3,6- dihydro-2H-pyridin-1-yl)_2 oxo ethyl] 3,8 diaza bicyclo[3.2.1]oct-8-yl}-nicotinsyremethylester; - Forbindelse nr. 70: 6-{3-[2-(4-Benzo[b]thiophen-5-yl-3,6-dihydro-2H-pyridin-l-yl)-2-oxo-ethyl]-3,8-diaza- bicyclo[3.2.1]oct-8-yl}-nicotinsyremethylester; - Forbindelse nr. 71: 6-{3-[2-(4-Benzo[b]thiophen-7-yl-3,6-dihydro-2H-pyridin-l-yl)-2-oxo-ethyl]-3,8-diaza-bicyclo[3.2.1]oct-8-yl}-nicotinsyre; - Forbindelse_nr.__72 : 2- [ (2S, 6R) -2, 6-Dimethyl-4- (5 — trifluormethyl-pyridin-2-yl)-piperazin -1-yl]-1-[4-(7-fluor- benzofuran-5-yl)-3,6-dihydro-2H-pyridin-l-yl]-ethanon; - Forbindelse nr. 73: 1-[4-(2,3-Dimethyl-benzofuran-6-yl)-3,6-dihydro-2H-pyridin-1-yl]-2-[(2S,6R)-2,6-dimethyl-4-(5- trifluormethyl-pyridin-2-yl)-piperazin-l-yl]-ethanon; Forbindelse nr. 74: 2-[(2 S,6R)-2,6-Dimethyl-4-(5- trifluormethyl-pyridin-2-yl)-piperazin -1-yl]-1-(4-quinolein- 2-yl-3,6-dihydro-2H-pyridin-l-yl)-ethanon; Forbindelse nr. 75: 1-(4-Benzofuran-5-yl-3,6-dihydro-2H- pyridin-l-yl)-2-(2,3,5,6-tetrahydro-[1,2']bipyrazinyl-4-yl)-ethanon; - Forbindelse nr. 76: 6-{3-[2-Oxo-2-(4-thiéno[3,2-c]pyridin-4- yl-3,6-dihydro-2H-pyridin-l-yl)-ethyl]-3,8-diaza- bicyclo[3.2.1]oct-8-yl}-nicotinsyremethylester; - Forbindelse nr. 77: 6-(3-{2-[4-(2-Methyl-benzo[b]thiophen-5- yl)-3,6-dihydro-2H-pyridin-l-yl]-2-oxo-ethyl}-3,8-diaza-bicyclo[3.2.1]oct-8-yl)-nicotinsyremethylester; Forbindelse nr. 78: 1-(4-Benzofuran-7-yl-3,6-dihydro-2H- pyridin-l-yl)-2-(4-pyridin-3-yl-[1,4]diazepan-l-yl)-ethanon; - Forbindelse nr. 79: 6-{3-[2-Oxo-2-(4-thiéno[3,2-c]pyridin-4- yl-3,6-dihydro-2H-pyridin-l-yl)-ethyl]-3,8-diaza- bicyclo[3.2.1]oct-8-yl]-nicotinsyre; - Forbindelse nr. 80: 6-(3-{2-[4-(2-Methyl-benzo[b]thiophen-5- yl)-3, 6-dihydro-2H-pyridin-l-yl]-2-oxo-ethyl}-3,8-diaza-bicyclo[3.2.1]oct-8-yl)-nicotinsyre; - Forbindelse nr. 81: 6-{3-[2-(3-Benzofuran-7-yl-2,5-dihydro- pyrrol-l-yl)-2-oxo-ethyl]-3,8-diaza-bicyclo[3.2.1]oct-8-yl}-nicotinsyremethylester; - Forbindelse nr. 82: 6-{3-[2-(3-Benzo[b]thiophen-7-yl-2,5- dihydro-pyrrol-1-yl)-2-oxo-ethyl]-3,8-diaza-bicyclo[3.2.1]oct-8-yl}-nicotinsyremethylester; Forbindelse nr. 83: 4-[2-(3-Benzofuran-7-yl-2,5-dihydro- pyrrol-l-yl)-2-oxo-ethyl]-1-(5-trifluormethyl-pyridin-2-yl)-piperazin-2-on; - Forbindelse nr. 84: 6-{3-[2-(4-Benzofuran-7-yl-2,3-dihydro- pyrrol- 1-yl)-2-oxo-ethyl]-3,8-diaza-bicyclo[3.2.1]oct-8-yl]-nicotinsyre; Forbindelse nr. 85: 6-{3-[2-(5-Benzo[b]thiophen-7-yl-3,4- dihydro-2H-pyridin-l-yl)-2-oxo-ethyl]-3,8-diaza-bicyclo[3.2.1]oct-8-yl}-nicotinsyre; Forbindelse nr. 86: 6-{3-[2-(4-Benzo[b]thiophen-7-yl-2,3- dihydro-pyrrol-l-yl)-2-oxo-ethyl]-3,8-diaza-bicyclo[3.2.1]oct-8-yl}-nicotinsyre; Forbindelse_nr._87 : 6-(3-{2-[4-(2,3-Dihydro- benzo[1,4]dioxin-6-yl)-3,6-dihydro-2H-pyridin-l-yl]-2-oxo-ethyl }-3,8-diaza-bicyclo[3.2.1]oct-8-yl)-nicotinsyremethylester; - Forbindelse nr. 88: 2-{(3S,5R)-4-[2-(4-Benzo[b]thiophen-7- yl-3,6-dihydro-2H-pyridin-l-yl)-2-oxo-ethyl]-3,5-dimethyl-piperazin-l-yl}-pyrimidin-5-carboxylsyre; Forbindelse nr. 89: 3-(6-{3-[2-(4-Benzofuran-7-yl-3,6- dihydro-2H-pyridin-l-yl)-2-oxo-ethyl]-3,8-diaza-bicyclo[3.2.1]oct-8-yl}-pyridin-3-yl)-4H-[l,2,4]oxadiazol-5-on; - Forbindelse nr. 90: 3-(6-{3-[2-(4-Benzo[b]thiophen-7-yl-3,6-dihydro-2H-pyridin-l-yl)-2-oxo-ethyl]-3,8-diaza- bicyclo [3.2.1]oct-8-yl]-pyridin-3-yl)-4H-[1,2,4]oxadiazol-5-on; - Forbindelse nr. 91: 6-(3-{2-[4-(2-Methyl-benzo[b]thiophen-5-yl) -3, 6-dihydro-2H-pyridin-l-yl]-2-oxo-ethyl}-3,8-diaza-bicyclo[3.2.1]oct-8-yl)-nicotinonitril; Forbindelse nr. 92; 1-(4-Benzofuran-7-yl-3,6-dihydro-2H- pyridin-l-yl)-2-[(2S,6R)-4-(3-chlor-5-trifluormethyl-pyridin-2-yl)-2,6-dimethyl-piperazin-l-yl]-ethanon; Forbindelse nr. 93: 1-(4-Benzofuran-7-yl-3,6-dihydro-2H- pyridin-l-yl)-2-(8-pyridin-3-yl-3,8-diaza-bicyclo[3.2.1]oct-3-yl)-ethanon; - Forbindelse nr. 94: 6-{3-[2-(4-Benzofuran-7-yl-3,6-dihydro- 2H-pyridin-l-yl)-2-oxo-ethyl]-3,8-diaza-bicyclo[3.2.1]oct-8-yl}-nicotinonitril; Forbindelse nr. 95: 1-(4-Benzofuran-7-yl-3,6-dihydro-2H- pyridin-l-yl)-2-[5-(5-trifluormethyl-pyridin-2-yl)-2,5-diaza-bicyclo[2.2.1]hept-2-yl]-ethanon; - Forbindelse nr. 96: 6-(3-{2-[4-(2-Methyl-benzo[b]thiophen-5 -yl)-3, 6-dihydro-2H-pyridin-l-yl]-2-oxo-ethyl}-3,8-diaza-bicyclo [3.2.1]oct-8-yl)-nicotinsyrecyclobutylester; Forbindelse_nr._97_: 2-[ (2S, 6R) -2, 6-Dimethyl-4-(5- trifluormethyl-pyridin-2-yl)-piperazin -1-yl]-1-[4-(lH-indol- 3-yl)-3,6-dihydro-2H-pyridin-l-yl]-ethanon; Forbindelse nr. 98: 1-[4-(lH-Indol-3-yl)-3,6-dihydro-2H- pyridin-l-yl]-2-(4-quinolin-2-yl-piperazin-l-yl)-ethanon; Forbindelse nr. 99: 1-(4-Benzofuran-7-yl-3,6-dihydro-2H- pyridin-l-yl)-2-[4-(7-chlor-quinolin-4-yl)-piperazin-l-yl]-ethanon; - Forbindelse nr. 100: 2-[(2S,6R)-4-(5-Fluor-pyrimidin-2-yl)- 2,6-dimethyl-piperazin-l-yl]-1-[4-(lH-indol-3-yl)-3,6-dihydro-2H-pyridin-l-yl]-ethanon; - Forbindelse nr. 101: 1-(4-Benzo[b]thiophen-7-yl-3,6-dihydro-2H-pyridin-l-yl)-2-[(2S,6R)-4-(5-chlor-pyridin-2-yl)-2, 6-dimethyl-piperazin-1-yl]-ethanon; - Forbindelse nr. 102: 1-(4-Benzo[b]thiophen-7-yl-3,6-dihydro-2H-pyridin-l-yl)-2-((2R,5S)-2,5-dimethyl-2,3,5,6-tetrahydro-[1,2']bipyrazinyl-4-yl)-ethanon; - Forbindelse nr. 103: 1-(4-Benzo[b]thiophen-7-yl-3,6-dihydro-2H-pyridin-l-yl)-2-[8-(5 — fluor-pyrimidin-2-yl)-3,8-diaza-bicyclo [3.2.1]oct-3-yl]-ethanon; - Forbindelse nr. 104: 1-(4-Benzo[b]thiophen-7-yl-3,6-dihydro-2H-pyridin-l-yl)-2-[8-(6-trifluormethyl-pyridin-2-yl)-3,8-diaza-bicyclo[3.2.1]oct-3-yl]-ethanon; - Forbindelse nr. 105: 1-(4-Benzo[b]thiophen-7-yl-3,6-dihydro- 2H-pyridin-l-yl)-2-(4-quinolin-2-yl-piperazin-l-yl)-ethanon; - Forbindelse nr. 106: 1-(4-Benzo[b]thiophen-7-yl-3,6-dihydro- 2H-pyridin-l-yl)-2-[4-(7-chlor-quinolin-4-yl)-piperazin-l-yl]-ethanon; - Forbindelse nr. 107: 1-(4-Benzo[b]thiophen-7-yl-3,6-dihydro- 2H-pyridin-l-yl)-2-[4-(5-chlor-pyridin-2-yl)-piperazin-l-yl]-ethanon; - Forbindelse nr. 108: 2-[4-(6-Chlor-pyridin-2-yl)-piperazin- l-yl] -1-[4-(lH-indol-3-yl)-3,6-dihydro-2H-pyridin-l-yl]-ethanon; Forbindelse nr. 109: 1-[4-(lH-Indol-3-yl)-3,6-dihydro-2H- pyridin-l-yl]-2-[4-(5-trifluormethyl-pyridin-2-yl)-piperazin-l-yl ]-ethanon; - Forbindelse nr. 110; 2-((2 S,6R)-2,6-Dimethyl-4-quinolin-2- yl-piperazin-l-yl)-1-[4-(lH-indol-3-yl)-3, 6-dihydro-2H-pyridin-l-yl]-ethanon; - Forbindelse nr. Ill: 1-(4-Benzo[b]thiophen-7-yl-3,6-dihydro- 2H-pyridin-l-yl)-2-(4-pyridin-3-yl-[1,4]diazepan-l-yl)-ethanon; - Forbindelse nr. 112: 1-(4-Benzo[b]thiophen-7-yl-3,6-dihydro- 2H-pyridin-l-yl)-2-[4-(5,6-dichlor-pyridin-2-yl)-piperazin-l-yl ]-ethanon; - Forbindelse nr. 113: 1-(4-Benzo[b]thiophen-7-yl-3, 6-dihydro-2H-pyridin-l-yl)-2-[4-(6-bromo-pyridin-2-yl)-piperazin-l-yl]-ethanon; - Forbindelse nr. 114: 1-[4-(2-Methyl-benzo[b]thiophen-5-yl)- 3.6- dihydro-2H-pyridin-l-yl]-2-(4-quinolin-2-yl-piperazin-l-yl)-ethanon; - Forbindelse nr. 115: 1-(4-Benzo[b]thiophen-7-yl-3,6-dihydro-2H-pyridin-l-yl)-2-[5-(6-trifluormethyl-pyridazin-3-yl)-2,5-diaza-bicyclo[2.2.1]hept-2-yl]-ethanon; - Forbindelse nr. 116: 1-[4-(2-Methyl-benzo[b]thiophen-5-yl)- 3.6- dihydro-2H-pyridin-l-yl]-2-[4-(6-trifluormethyl-pyridin-2-yl)-piperazin-l-yl]-ethanon; - Forbindelse nr. 117: 2-[4-(7-Chlor-quinolin-4-yl)-piperazin-l-yl] -1-[4-(2-methyl-benzo[b]thiophen-5-yl)-3,6-dihydro-2H-pyridin-l-yl]-ethanon; - Forbindelse nr. 118: 4-[2-Oxo-2-(4-thieno[3,2-c]pyridin-4- yl-3,6-dihydro-2H-pyridin-l-yl)-ethyl]-1-(5-trifluormethyl-pyridin-2-yl)-piperazin-2-on; - Forbindelse nr. 119: 1-(4-Benzofuran-7-yl-3,6-dihydro-2H- pyridin-l-yl)-2-((2S,6R)-2,6-dimethyl-4-(5-thiazol-2-yl-pyridin-2-yl)-piperazin-l-yl]-ethanon; - Forbindelse nr. 120: 1-(4-Benzofuran-7-yl-3,6-dihydro-2H- pyridin-l-yl)-2-{ (2S, 6R)-2,6-dimethyl-4-[5-(2-methyl-2H-tetrazol-5-yl)-pyridin-2-yl]-piperazin-l-yl}-ethanon; Forbindelse_nr._121: 2-[ (2S, 6R) -2, 6-Dimethyl-4-(5- trifluormethyl-pyridin-2-yl)-piperazin-l-yl]-1-(4-quinolin-2-yl-3,6-dihydro-2H-pyridin-l-yl)-ethanon; Forbindelse nr. 122: 4-[2-Oxo-2-(4-quinolin-2-yl-3,6- dihydro-2H-pyridin-l-yl)-ethyl]-1-(5-trifluormethyl-pyridin-2-yl)-piperazin-2-on; Forbindelse nr. 123: 1-(4-Quinolin-2-yl-3,6-dihydro-2H- pyridin-l-yl)-2-[8-(5-trifluormethyl-pyridin-2-yl)-3,8-diaza-bicyclo[3.2.1]oct-3-yl]-ethanon; Forbindelse nr. 124: 1-(4-Benzofuran-7-yl-3,6-dihydro-2H-pyridin-l-yl)—2 —{8 —[5-(l-methyl-lH-tetrazol-5-yl)-pyridin-2-yl]-3,8-diaza-bicyclo[3.2.1]oct-3-yl]-ethanon; Forbindelse nr. 125: 1-(4-Benzofuran-7-yl-3,6-dihydro-2H-pyridin-l-yl)-2-[(2 S,6R)-4-(5-methansulfonyl-pyridin-2-yl)- 2,6-dimethyl-piperazin-l-yl]-ethanon; i form af en base eller et additionssalt med en syre.
7. Fremgangsmåde til fremstilling af en forbindelse med formlen (I) ifølge et hvilket som helst af kravene 1 til 6, kendetegnet ved, at en forbindelse med formlen (II):
(II) hvor A, B, m og n er defineret ifølge et hvilket som helst af kravene 1 til 6, og Hal betegner et halogenatom, omsættes med en forbindelse med den almene formel (III): H-W-R2 (III) hvor W og R2 er defineret ifølge et hvilket som helst af kravene 1 til 6.
8. Lægemiddel, kendetegnet ved, at det omfatter en forbindelse med formlen (I) ifølge et hvilket som helst af kravene 1 til 6 eller et additionssalt af denne forbindelse med en farmaceutisk acceptabel syre.
9. Farmaceutisk præparat, kendetegnet ved, at det omfatter en forbindelse med formlen (I) ifølge et hvilket som helst af kravene 1 til 6 eller et farmaceutisk acceptabelt salt samt mindst en farmaceutisk acceptabel excipiens.
10. Forbindelse ifølge et hvilket som helst af kravene 1 til 6 i dens egenskab af lægemiddel.
11. Forbindelse ifølge et hvilket som helst af kravene 1 til 6 til fremstilling af et lægemiddel, der er beregnet til forebyggelse eller behandling af centrale og perifere neurodegenerative sygdomme, senildemens, epilepsi, Alzheimers sygdom, Parkinsons sygdom, Huntingtons chorea, Downs syndrom, prionsygdomme, amnesi, skizofreni, depression, bipolar sygdom, amyotrofisk lateral sklerose, dissemineret sklerose, hjertekarsygdomme, post-iskæmiske hjerteskader, kardiomyopati, myokardieinfarkt, hjerteinsufficiens, hjerteiskæmi, hjerneinfarkt; perifere neuropatier, skader på synsnerven og nethinden, degeneration af nethindens pigment, glaukom, nethindeiskæmi, maculadegeneration, rygmarvstraumer, kranietraumer, atherosklerose, stenoser, forstyrrelser af ardannelsen, alopeci, pankreatitis, leverfibrose, cancer, tumorer, metastaser, leukæmi, åndedrætsforstyrrelser, lungeinflammation, allergi, astma, kronisk obstruktiv bronkopneumopati, kutane, somatiske, viscerale og neurologiske smerter, kroniske neuropatiske og inflammatoriske smerter, autoimmune sygdomme, reumatoid artritis, ankyloserende spondylitis, psoriasisgigt, almindelig psoriasis, knoglebrud, knoglesygdomme, osteoporose.
12. Forbindelse ifølge et af kravene 1 til 6 i dens egenskab af inhibitor af dimeriseringen af receptoren p75NTR.
13. Anvendelse af en forbindelse ifølge et af kravene 1 til 6 til fremstilling af lægemidler, der er nyttige i behandlingen og forebyggelsen af centrale og perifere neurodegenerative sygdomme, senildemens, epilepsi, Alzheimers sygdom, Parkinsons sygdom, Huntingtons chorea, Downs syndrom, prionsygdomme, amnesi, skizofreni, depression, bipolar sygdom, amyotrofisk lateral sklerose, dissemineret sklerose, hjertekarsygdomme, post-iskæmiske hjerteskader, kardiomyopati, myokardieinfarkt, hjerteinsufficiens, hjerteiskæmi, hjerneinfarkt; perifere neuropatier, skader på synsnerven og nethinden, degeneration af nethindens pigment, glaukom, nethindeiskæmi, maculadegeneration, rygmarvstraumer, kranietraumer, atherosklerose, stenoser, forstyrrelser af ardannelsen, alopeci, pankreatitis, leverfibrose, cancer, tumorer, metastaser, leukæmi, åndedrætsforstyrrelser, lungeinflammation, allergi, astma, kronisk obstruktiv bronkopneumopati, kutane, somatiske, viscerale og neurologiske smerter, kroniske neuropatiske og inflammatoriske smerter, autoimmune sygdomme, reumatoid artritis, ankyloserende spondylitis, psoriasisgigt, almindelig psoriasis, knoglebrud, knoglesygdomme, osteoporose.
DK10801663.5T 2009-12-14 2010-12-13 Hidtil ukendte derivater af (heterocyklus-tetrahydro-pyridin)-(piperazinyl)-1-alkanon og (heterocyklus-dihydro-pyrrolidin)-(piperazinyl)-1-alkanon og deres anvendelse som inhibitorer af p75 DK2513088T3 (da)

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FR0906025A FR2953836B1 (fr) 2009-12-14 2009-12-14 Nouveaux derives (heterocycle-tetrahydro-pyridine)-(piperazinyl)-1-alcanone et (heterocycle-dihydro-pyrrolidine)-(piperazinyl)-1-alcanone et leur utilisation comme inhibiteurs de p75
PCT/FR2010/052686 WO2011080445A1 (fr) 2009-12-14 2010-12-13 NOUVEAUX DERIVES (HETEROCYCLE-TETRAHYDRO-PYRIDINE)-(PIPERAZINYL)-1-ALCANONE ET (HETEROCYCLE-DIHYDRO-PYRROLIDINE)-(PIPERAZINYL)-1-ALCANONE ET LEUR UTILISATION COMME INHIBITEURS DE p75

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JP2003514508A (ja) 1997-07-01 2003-04-15 ノボ ノルディスク アクティーゼルスカブ グルカゴン拮抗剤／逆作用剤
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DK2513088T3 (da) Hidtil ukendte derivater af (heterocyklus-tetrahydro-pyridin)-(piperazinyl)-1-alkanon og (heterocyklus-dihydro-pyrrolidin)-(piperazinyl)-1-alkanon og deres anvendelse som inhibitorer af p75