RS51831B - 1-phenil-2-heteroaryl substitated benzimidazol derivatives, the use thereof for producing drugs used in the treatment of immunological diseases. - Google Patents

1-phenil-2-heteroaryl substitated benzimidazol derivatives, the use thereof for producing drugs used in the treatment of immunological diseases.

Info

Publication number
RS51831B
RS51831B YU71404A YUP71404A RS51831B RS 51831 B RS51831 B RS 51831B YU 71404 A YU71404 A YU 71404A YU P71404 A YUP71404 A YU P71404A RS 51831 B RS51831 B RS 51831B
Authority
RS
Serbia
Prior art keywords
alkyl
group
ring
substituted
heteroaryl
Prior art date
Application number
YU71404A
Other languages
Serbian (sr)
Inventor
Thorsten Blume
Wolfgang Halfbrodt
Joachim Kuhnke
Ursula MÖNNING
Bernd Elger
Herbert Schneider
Original Assignee
Bayer Schering Pharma Aktiengesellschaft
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.)
Filing date
Publication date
Application filed by Bayer Schering Pharma Aktiengesellschaft filed Critical Bayer Schering Pharma Aktiengesellschaft
Publication of RS71404A publication Critical patent/RS71404A/en
Publication of RS51831B publication Critical patent/RS51831B/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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 three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Transplantation (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

1-FENIL-2-HETEROARIL SUPSTITUISANI DERIVATI BENZIMIDAZOLA, NJIHOVA PRIMENA ZA DOBIJANJE LEKOVA ZA LEČENJE IMUNOLOŠKIH OBOLJENJA. Derivati benzimidazola opšte formule Iu njoj su: R1 fenil grupa, koja je u datom slučaju medjusobno nezavisnosupstituisana sa do tri sledeća supstituenta:F, Cl, Br, JOH, OR4, OCOR4SR4, SOR4, SO2R4,R4NH2, NHR4, NR4R4ili dva susedna supstituenta na R1 čine zajedno jednu -O-CH2-O-, -O-CH2-CH2-O- ili -CH2-CH2-CH2- grupu,R2 monociklična ili biciklična 5 - 10-člana heteroarilgrupa sa 1-2heteroatoma izabranih od N, S i O, koja je u datom slučajusupstituisana medjusobno nezavisno sa do dva od sledećihsupstituenata:F, Cl, Br, JOH, OR4, OCOR4COR4SR4, SOR4, SO2R4, R4,ili dva susedna supstituenta na R2 čine zajedno jednu -O-CH2-O-, -O-CH2-CH2-O- ili -CH2-CH2-CH2- grupu,R3 H, OH ili O-C1-6-alkil,R4 i R4' medjusobno nezavisno C1-4-perfluoralkil ili C1-6-alkilA ravnolančasta alkilengrupa izabrana između etilena, propilena ibutilena, koja je u datom slučaju supstituisana sa =O, OH, O-C1-3-alkilom, NH2, NH-C1-3-alkilom, NH-C1-3-al-kanoilom, N(C1-3-alkilom)2 i N(C1-3-alkil)(C1-3-alkanoilom),B COOH, CONH2, CONHNH2, CONHR5, CONR5R5',svaka vezana na ugljenikov atom grupe A,R5 i R5' medjusobno nezavisno ostatak, izabran iz grupe koja obuhvata C1-6-alkil, C2-6-alkenil, C2-6-alkinil, pri čemu jedan ugljenikov atom može da bude zamenjen sa O, S, SO, SO2, NH, N-C1-3-alkilom ili N-C-1-3-alkanoilom, dalje (C0-3-alkandiil-C3-7-cikloalkil), pri čemu u petočlanom cikloalkil-prstenu jedan član prstena može da bude prsten-N ili prsten-O, a u šestočlanom ili sedmočlanom cikloalkil-prstenu jedan ili dva člana prstena mogu da budu svaki N-atom prstena i/ili O-atom prstena, pri čemu N-atomi prstena mogu biti supstituisani u datom slučaju sa C1-3-alkilom ili C1-3-alkanoilom, kao i dalje (C0-3-alkandiil-fenil) i (C0-3-alkandiil-heteroaril), pri čemu je heteroaril grupa peto- ili šestočlana i sadrži jedan ili dva heteroatoma, izabranih iz grupe koja obuhvata N, S i O,pri čemu svi prethodno navedeni alkil- i cikloalkil ostaci u datom slučaju mogu biti supstituisani sa do dva ostatka izabrana iz grupe koja obuhvata CF3, C2F2, OH, O-C1-3-alkil, NH2, NH-C1-3-alkil, NH-C1-3-alkanoil, N(C1-3-alkil)2, N(C1-3-alkil)(C1-3-alkanoil), COOH, CONH2 i COO- C1-3-alkil, i sve prethodno navedene fenil- i heteroaril grupe mogu biti supstituisane sa do dva ostatka izabrana iz grupe koja obuhvata F, Cl, Br, CH3, C2H5, OH, OCH3, OC2H5, NO2, N(CH3)2, CF3, C2F5, i SO2NH2ili R5 i R5´ čine zajedno sa N-atomom peto- do sedmočlani heterociklični prsten koji može da sadrži dalji N- ili O- ili S-atom koji može biti supstituisan sa C1-4-alkilom, (C0-2-alkandiil-C1-4-alkoksi), C1-4-alkoksikarbonilom, amin1-PHENYL-2-HETEROARYL SUBSTITUTED BENZIMIDAZOLE DERIVATIVES, THEIR APPLICATION FOR OBTAINING DRUGS FOR THE TREATMENT OF IMMUNOLOGICAL DISEASES. Derivatives of benzimidazole of the general formula I in it are: R1 phenyl group, which in a given case is mutually independently substituted with up to three of the following substituents: F, Cl, Br, JOH, OR4, OCOR4SR4, SOR4, SO2R4, R4NH2, NHR4, NR4R4 or two adjacent substituents on R1 together form one -O-CH2-O-, -O-CH2-CH2-O- or -CH2-CH2-CH2- group, R2 monocyclic or bicyclic 5-10-membered heteroaryl group with 1-2 heteroatoms selected from N, S and O, which in a given case is substituted independently of each other with up to two of the following substituents: F, Cl, Br, JOH, OR4, OCOR4COR4SR4, SOR4, SO2R4, R4, or two adjacent substituents on R2 together form one -O-CH2-O- , -O-CH2-CH2-O- or -CH2-CH2-CH2- group, R3 H, OH or O-C1-6-alkyl, R4 and R4' mutually independent C1-4-perfluoroalkyl or C1-6-alkylA a straight-chain alkylene group selected from ethylene, propylene, and butylene, which in a given case is substituted with =O, OH, O-C1-3-alkyl, NH2, NH-C1-3-alkyl, NH-C1-3-al-kanoyl, N (C1-3-alkyl)2 and N(C1-3-alkyl)(C1-3-alkanoyl),B COOH, CONH2, CONHNH2, CONHR5, CONR5R5', each attached to a carbon atom of group A, R5 and R5' to each other independently a residue selected from the group consisting of C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, wherein one carbon atom may be replaced by O, S, SO, SO2, NH, N-C1- 3-alkyl or N-C-1-3-alkanoyl, further (C0-3-alkanediyl-C3-7-cycloalkyl), whereby in a five-membered cycloalkyl-ring one member of the ring can be ring-N or ring-O, and in a six-membered or a seven-membered cycloalkyl ring, one or two members of the ring may each be an N-atom of the ring and/or an O-atom of the ring, wherein the N-atoms of the ring may be substituted in a given case with C1-3-alkyl or C1-3-alkanoyl , as well as (C0-3-alkanediyl-phenyl) and (C0-3-alkanediyl-heteroaryl), wherein the heteroaryl group is five- or six-membered and contains one or two heteroatoms, selected from the group consisting of N, S and O , whereby all the aforementioned alkyl- and cycloalkyl residues in a given case can be substituted with up to two residues selected from the group consisting of CF3, C2F2, OH, O-C1-3-alkyl, NH2, NH-C1-3-alkyl, NH-C1-3-alkanoyl, N(C1-3-alkyl)2, N(C1-3-alkyl)(C1-3-alkanoyl), COOH, CONH2 and COO-C1-3-alkyl, and all of the above phenyl- and heteroaryl groups may be substituted with up to two residues selected from the group consisting of F, Cl, Br, CH3, C2H5, OH, OCH3, OC2H5, NO2, N(CH3)2, CF3, C2F5, and SO2NH2 or R5 and R5 ´ form together with the N-atom a five- to seven-membered heterocyclic ring which may contain a further N- or O- or S-atom which may be substituted with C1-4-alkyl, (C0-2-alkanediyl-C1-4-alkoxy ), C1-4-Alkoxycarbonyl, amine

YU71404A 2002-02-15 2003-01-17 1-phenil-2-heteroaryl substitated benzimidazol derivatives, the use thereof for producing drugs used in the treatment of immunological diseases. RS51831B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10207844A DE10207844A1 (en) 2002-02-15 2002-02-15 1-phenyl-2-heteroaryl-substituted benzimidazole derivatives, their use for the preparation of medicaments and pharmaceutical preparations containing these derivatives
PCT/EP2003/000462 WO2003068766A1 (en) 2002-02-15 2003-01-17 1-phenyl-2-heteroaryl-substituted benzimidazole derivatives, the use thereof for producing drugs used in the treatment of immunological diseases

Publications (2)

Publication Number Publication Date
RS71404A RS71404A (en) 2006-10-27
RS51831B true RS51831B (en) 2012-02-29

Family

ID=27674913

Family Applications (1)

Application Number Title Priority Date Filing Date
YU71404A RS51831B (en) 2002-02-15 2003-01-17 1-phenil-2-heteroaryl substitated benzimidazol derivatives, the use thereof for producing drugs used in the treatment of immunological diseases.

Country Status (30)

Country Link
EP (1) EP1474415B1 (en)
JP (1) JP4739675B2 (en)
KR (1) KR101027556B1 (en)
CN (1) CN1317274C (en)
AR (1) AR038492A1 (en)
AT (1) ATE517881T1 (en)
AU (1) AU2003205624B2 (en)
BR (1) BR0307723A (en)
CA (1) CA2475780C (en)
CR (1) CR7442A (en)
CY (1) CY1113230T1 (en)
DE (1) DE10207844A1 (en)
DK (1) DK1474415T3 (en)
EC (1) ECSP045296A (en)
ES (1) ES2369662T3 (en)
IL (1) IL163431A (en)
MX (1) MXPA04007949A (en)
NO (1) NO329667B1 (en)
NZ (1) NZ534660A (en)
PE (1) PE20030941A1 (en)
PL (1) PL216233B1 (en)
PT (1) PT1474415E (en)
RS (1) RS51831B (en)
RU (1) RU2325384C2 (en)
SI (1) SI1474415T1 (en)
TW (1) TWI328583B (en)
UA (1) UA81243C2 (en)
UY (1) UY27661A1 (en)
WO (1) WO2003068766A1 (en)
ZA (1) ZA200407381B (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1497266T3 (en) 2002-03-27 2008-10-06 Glaxo Group Ltd Quinoline derivatives and their use as 5HT6 ligands
WO2004103309A2 (en) * 2003-05-19 2004-12-02 Irm Llc Immunosuppressant compounds and compositions
WO2014044611A1 (en) 2012-09-20 2014-03-27 Bayer Pharma Aktiengesellschaft 1-aryl-2-heteroaryl benzimidazoles for the induction of neuronal regeneration

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4330959A1 (en) * 1993-09-09 1995-03-16 Schering Ag New benzimidazole derivatives, processes for their preparation and their pharmaceutical use
HU228366B1 (en) * 2000-01-14 2013-03-28 Schering Ag 1,2-diaryl benzimidazoles, pharmaceutical compositions containing them and their use for producing pharmaceutical compositions for treating illnesses associated with a microglia activation
US7115645B2 (en) * 2000-01-14 2006-10-03 Schering Aktiengesellschaft 1,2 diarylbenzimidazoles and their pharmaceutical use
DE10207843A1 (en) * 2002-02-15 2003-09-04 Schering Ag Microlia inhibitors for interruption of interleukin 12 and IFN-gamma mediated immune responses

Also Published As

Publication number Publication date
CA2475780A1 (en) 2003-08-21
CR7442A (en) 2006-02-06
KR101027556B1 (en) 2011-04-06
WO2003068766A1 (en) 2003-08-21
EP1474415A1 (en) 2004-11-10
NO329667B1 (en) 2010-11-29
UA81243C2 (en) 2007-12-25
CN1317274C (en) 2007-05-23
ES2369662T3 (en) 2011-12-02
JP4739675B2 (en) 2011-08-03
RU2325384C2 (en) 2008-05-27
TW200303307A (en) 2003-09-01
IL163431A (en) 2010-11-30
ATE517881T1 (en) 2011-08-15
TWI328583B (en) 2010-08-11
RS71404A (en) 2006-10-27
JP2005521686A (en) 2005-07-21
DK1474415T3 (en) 2011-11-21
EP1474415B1 (en) 2011-07-27
ZA200407381B (en) 2005-11-30
PL216233B1 (en) 2014-03-31
AU2003205624A1 (en) 2003-09-04
CY1113230T1 (en) 2016-04-13
AR038492A1 (en) 2005-01-19
KR20040081795A (en) 2004-09-22
PT1474415E (en) 2011-10-13
NZ534660A (en) 2006-02-24
MXPA04007949A (en) 2004-11-26
RU2004127678A (en) 2005-07-10
DE10207844A1 (en) 2003-09-04
CN1633429A (en) 2005-06-29
NO20043841L (en) 2004-11-12
AU2003205624B2 (en) 2009-08-27
BR0307723A (en) 2005-01-25
PE20030941A1 (en) 2004-01-17
CA2475780C (en) 2011-08-02
ECSP045296A (en) 2004-10-26
UY27661A1 (en) 2003-09-30
PL371269A1 (en) 2005-06-13
SI1474415T1 (en) 2011-12-30

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