PE20091429A1 - 4-(4-ciano-2-tioaril)dihidropirimidinonas como inhibidores de la elastasa neutrofila humana (hne) - Google Patents

4-(4-ciano-2-tioaril)dihidropirimidinonas como inhibidores de la elastasa neutrofila humana (hne)

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Publication number
PE20091429A1
PE20091429A1 PE2008002054A PE2008002054A PE20091429A1 PE 20091429 A1 PE20091429 A1 PE 20091429A1 PE 2008002054 A PE2008002054 A PE 2008002054A PE 2008002054 A PE2008002054 A PE 2008002054A PE 20091429 A1 PE20091429 A1 PE 20091429A1
Authority
PE
Peru
Prior art keywords
cyane
alkyl
phenyl
hne
inhibitors
Prior art date
Application number
PE2008002054A
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English (en)
Inventor
Franz Nussbaum
Dagmar Karthaus
Sonja Anlauf
Martina Klein
Volkhart Min-Jian Li
Daniel Meibom
Klemens Lustig
Jens Schamberger
Original Assignee
Bayer Schering Pharma Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40394273&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20091429(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from DE102007061766A external-priority patent/DE102007061766A1/de
Priority claimed from DE102008022521A external-priority patent/DE102008022521A1/de
Priority claimed from DE102008052013A external-priority patent/DE102008052013A1/de
Application filed by Bayer Schering Pharma Ag filed Critical Bayer Schering Pharma Ag
Publication of PE20091429A1 publication Critical patent/PE20091429A1/es

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    • C07D239/08—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms directly attached in position 2
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
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    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
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    • C07D239/20—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D239/22—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring carbon atoms
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    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

SE REFIERE A DERIVADOS DE HIDROPIRIMIDINAS DE FORMULA (I), DONDE A Y E REPRESENTAN LOS DOS C-R7 O UNO DE LOS DOS MIEMBROS DEL ANILLO A Y E ES N Y EL OTRO ES C-R7; R7 ES H, F O CL; Z ES O o S; n ES 0, 1 O 2; R1 ES ALQUILO (C1-C6) OPCIONALMENTE SUSTITUIDO CON HIDROXILO, ALCOXI (C1-C4), AMINO, ENTRE OTROS; R2 ES H, F O CL; R3 ES CIANO O UN GRUPO DE -C(=O)-R8, -C(=O)-O-R8, -C(=O)-NH2 O -C-(=O)-NH-R8; R8 ES ALQUILO (C1-C6), ALQUENILO (C3-C6) O CICLOALQUILO (C3-C6); R4 ES METILO O ETILO, O R3 Y R4 ESTAN UNIDOS ENTRE SI Y FORMAN UN GRUPO CONDENSADO DE FORMULA (a), DONDE * Y ** SON CADA UNO UNION EN LAS POSICIONES 5 Y 6 RESPECTIVAMENTE EN EL ANILLO DE DIHIDROPIRIMIDINA, R9 ES H, ALQUILO (C1-C6) O CICLOALQUILO (C3-C6); R5 ES H O ALQUILO (C1-C6), SUSTITUIDO OPCIONALMENTE CON CIANO, HIDROXILO, ALCOXI (C1-C4), ENTRE OTROS; R6 ES H, F O CL. SON COMPUESTOS PREFERIDOS: (4S)-4-[2-(CICLOBUTILSULFONIL)-4-CIANOFENIL]-3,6-DIMETIL-2-OXO-1[3-(TRIFLUOROMETIL)FENIL]-1,2,3,4-TETRAHIDROPIRIMIDINA-5-CARBONILO, (4S)-3-(CIANOMETIL)-4-[4-CIANO-2-(METILSULFONIL)FENIL]-6-METIL-2.OXO-1-[3-(TRIFLUOROMETIL)-FENIL]-1,2,3,4-TETRAHIDROPIRIMIDINA-5-CARBONITRILO, ENTRE OTROS. TAMBIEN SE REFIERE A UN METODO DE PREPARACION PARA UNA COMPOSICION FARMACEUTICA QUE LOS CONTIENE. DICHOS COMPUESTOS SON INHIBIDORES DE ELASTASA NEUTROFILA HUMANA (HNE), SIENDO DE UTILIDAD EN EL TRATAMIENTO DE TRASTORNOS PULMONARES Y DEL SISTEMA CARDIOVASCULAR TAL COMO HIPERTENSION ARTERIAL PULMONAR, ENTRE OTROS
PE2008002054A 2007-12-20 2008-12-11 4-(4-ciano-2-tioaril)dihidropirimidinonas como inhibidores de la elastasa neutrofila humana (hne) PE20091429A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE102007061766A DE102007061766A1 (de) 2007-12-20 2007-12-20 4-(4-Cyano-2-thioaryl)-dihydropyrimidinone und ihre Verwendung
DE102008022521A DE102008022521A1 (de) 2008-05-07 2008-05-07 1,4-Diaryl-pyrimidopyridazin-2,5-dione und ihre Verwendung
DE102008052013A DE102008052013A1 (de) 2008-10-17 2008-10-17 4-(4-Cyano-2-thioaryl)-dihydropyrimidinone und ihre Verwendung

Publications (1)

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PE20091429A1 true PE20091429A1 (es) 2009-09-26

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PE2008002054A PE20091429A1 (es) 2007-12-20 2008-12-11 4-(4-ciano-2-tioaril)dihidropirimidinonas como inhibidores de la elastasa neutrofila humana (hne)

Country Status (39)

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US (3) US8288402B2 (es)
EP (1) EP2234985B1 (es)
JP (1) JP5519526B2 (es)
KR (2) KR101712786B1 (es)
CN (2) CN103204815B (es)
AR (1) AR069765A1 (es)
AT (1) ATE548355T1 (es)
AU (1) AU2008340733B9 (es)
BR (1) BRPI0821027B8 (es)
CA (1) CA2709786C (es)
CL (1) CL2008003691A1 (es)
CO (1) CO6280490A2 (es)
CR (1) CR11472A (es)
CY (1) CY1112813T1 (es)
DK (1) DK2234985T3 (es)
DO (1) DOP2010000165A (es)
EC (1) ECSP10010216A (es)
ES (1) ES2382143T3 (es)
HK (2) HK1146485A1 (es)
HR (1) HRP20120457T1 (es)
IL (2) IL205742A (es)
JO (1) JO2756B1 (es)
MA (1) MA31920B1 (es)
MX (1) MX2010006033A (es)
MY (1) MY150285A (es)
NZ (1) NZ586263A (es)
PE (1) PE20091429A1 (es)
PL (1) PL2234985T3 (es)
PT (1) PT2234985E (es)
RS (1) RS52270B (es)
RU (1) RU2497813C2 (es)
SG (2) SG186679A1 (es)
SI (1) SI2234985T1 (es)
SV (1) SV2010003581A (es)
TN (1) TN2010000288A1 (es)
TW (1) TWI455715B (es)
UY (1) UY31526A1 (es)
WO (1) WO2009080199A1 (es)
ZA (1) ZA201004239B (es)

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