Title:
新規化合物
Document Type and Number:
Japanese Patent JP5291623
Kind Code:
B2
Abstract:
Pyridine-piperazine-phenyl derivatives (I) or their enantiomers, diastereomers or salts, preferably salts with organic or inorganic acid or base, are new. Pyridin-piperazin-phenyl derivative (I) of formula (R 5>-A-R 4>-B 1>-R 3>-A-D-Y 1>-N(R 2>)-SO 2-R 1>) or their enantiomers, diastereomers or salts, preferably salts with organic or inorganic acid or base, are new. A : a bond or 1-4C alkylene; B 1> : a bond, 1-3C alkylene, -O- or -C(O)-; D : amine group of formula (-N(R 2>)-C(O)-) or (-C(O)-N(R 2>)-); Y 1> : 1-4C-alkylene optionally substituted by R 2>, where a methylene group can be replaced in addition by Y 2>; Y 2> : -O-, -S-, -S(O)-, -N(R 2>)-, -N(R 2>)-C(O)-, -C(O)-N(R 2>)-, -C(O)-, -CH(aryl)- or -S(O) 2-; R 1> : 3-7C-cycloalkyl- or aryl-, heteroaryl- or aryl-1-3C-alkyl- (all substituted with 1-4 R1a); R 2> : H or 1-3C-alkyl, where each methylene group is substituted with up to two F and each methyl group is replaced with up to 3 F; R 3> : arylene, heteroarylene, saturated 4-7-membered heterocyclic ring, unsaturated 5-7 membered heterocyclic ring (all substituted with 1 or 2 R3a) or 1-6C-alkylene; R 4> : arylene, heteroarylene, saturated 4-7-membered heterocyclic ring, unsaturated 5-7 membered heterocyclic ring (all substituted with 1 or 2 R4a), -O-, -C(O)O-, -C(O)NR 2>-, -NR 2>-, -NR 2>-NR 2>-, -3-7C-cycloalkylene- or -1-6C-alkylene-; R 5> : heteroaryl, 4-7 membered saturated heterocyclic ring (both substituted with 1 or 2 R5a), H, 1-8C alkyl, 3-7C-cycloalkyl (optionally substituted with 1-3C alkyl), H 2N-, 1-4C-alkyl-NH-, (1-4C-alkyl) 2N- or H 2N-C(O)-; and R1a, R3a, R4a, R5a : H, F, Cl, Br, I, 1-3C-alkyl-, HO-, 1-3C-alkyl-O- or 1-3C-alkyl-O-2-4C-alkylene-O-. An independent claim is included for pyridin-piperazin-phenyl salts with inorganic or organic acids or bases. ACTIVITY : Analgesic; Antimigraine; Neuroprotective; Dermatological; Cerebroprotective; Vasotropic; Antiallergic; Immunosuppressive; Gastrointestinal-Gen; Respiratory-Gen; Antiasthmatic; Antiinflammatory; Antiarthritic; Osteopathic. MECHANISM OF ACTION : None given.
Inventors:
Kaufmann Hefner Iris
Howell norbert
Walter liner
Abel Heiner
Dorts Henry
Cecí Angelo
Schuler Mets Anette
Connectsky ingo
Howell norbert
Walter liner
Abel Heiner
Dorts Henry
Cecí Angelo
Schuler Mets Anette
Connectsky ingo
Application Number:
JP2009525021A
Publication Date:
September 18, 2013
Filing Date:
August 14, 2007
Export Citation:
Assignee:
Boehringer Ingelheim International GmbH
International Classes:
C07D209/44; A61K31/18; A61K31/341; A61K31/40; A61K31/4035; A61K31/404; A61K31/4164; A61K31/4168; A61K31/417; A61K31/4184; A61K31/4196; A61K31/422; A61K31/426; A61K31/427; A61K31/437; A61K31/438; A61K31/44; A61K31/4418; A61K31/4427; A61K31/4439; A61K31/445; A61K31/451; A61K31/454; A61K31/4545; A61K31/47; A61K31/472; A61K31/4725; A61K31/495; A61K31/496; A61K31/501; A61K31/502; A61K31/505; A61K31/5375; A61K31/5377; A61K31/55; A61K31/551; A61P25/04; A61P25/06; A61P29/00; C07D211/26; C07D211/56; C07D211/58; C07D213/40; C07D215/38; C07D223/12; C07D223/16; C07D235/04; C07D235/18; C07D241/04; C07D295/10; C07D295/12; C07D295/18; C07D401/04; C07D401/06; C07D471/04; C07D471/10
Domestic Patent References:
JP2004534729A | ||||
JP2005535613A | ||||
JP10506122A | ||||
JP2006516132A |
Foreign References:
WO2006048209A1 | ||||
WO2006071775A2 | ||||
WO2006036664A1 | ||||
WO2006035967A1 | ||||
WO2001037826A1 | ||||
US20060178360 |
Other References:
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MORISSETTE,G. et al.,Dual antagonists of the bradykinin B1 and B2 receptors based on a postulated common pharmacophore from existing non-peptide antagonists,Biological Chemistry ,2006年,387(2),p.189-194
EL-NAGGAR,A.M. et al.,Synthesis and biological activity of some new 4-(aminoacyl)aminopyridines and 2-(aminoacyl)aminopyrimidine derivatives,Polish Journal of Chemistry ,1982年,56(10-12),p.1279-1285
BRAICHENKO,V.T. et al.,N-aryl-β-amino acids. III. N-aryl-sulfonyl-β-alanine hydrazides,Khimiko-Farmatsevticheskii Zhurnal,1972年,6(8),p.6-8
MUKHERJEE,G.N. and CHAKRABORTY,P.K.,Metal complexes of some peptide derivatives. Part-XIV. Complex formation of copper(II) with N-benzenesulfonamides of some dipeptides,Journal of the Indian Chemical Society ,2002年,79(2),p.137-141
SELVAMURUGAN,V. and AIDHEN,I.S.,Simple synthetic equivalents for the β-(N,N-disubstituted)ethylamino acyl cation synthon and their applications,Synthesis,2001年,(15),p.2239-2246
PAUL,H. et al.,Synthesis of β-(β-alanylamino)propionamidine and cis- and trans-(+-)-amidinomycin,Archiv der Pharmazie und Berichte der Deutschen Pharmazeutischen Gesellschaft,1968年,301(7),p.512-519
EI-SHARIEF,A.M. et al.,Amino acids in the synthesis of heterocyclic systems: The synthesis of triazinoquinazolinones, triazepinoquinazolinones and triazocinoquinazolinones of potential biological interest,Molecules [online computer file] ,2001年,6(3),p.267-278
SHOEB,A. et al.,Oral hypoglycemic agents. IV. Synthesis of 1-arylsulfonyl-3-substituted-2-imidazolidinones and 1,2,3-trisubstituted ureas,Indian Journal of Chemistry,1965年,3(11),p.507-509
SEN,A.B. and YAJNIK,M.S.,Synthesis of peptides of β-amino acids,Journal of the Indian Chemical Society,1965年,42(3),p.145-148
MOLANDER,G.A. and STENGEL,P.J.,Reduction of 2-acylaziridines by samarium(II) iodide. An efficient and regioselective route to β-amino carbonyl compounds,TETRAHEDRON,NL,ELSEVIER SCIENCE PUBLISHERS,1997年 6月30日,53(26),p.8887-8912
SARTORI,E. et al.,Synthesis and activities of new arylsulfonamide thromboxane A2 receptor antagonists,EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,フランス,EDITIONS SCIENTIFIQUE ELSEVIER,1993年,28(7-8),p.625-632
MORISSETTE,G. et al.,Dual antagonists of the bradykinin B1 and B2 receptors based on a postulated common pharmacophore from existing non-peptide antagonists,Biological Chemistry ,2006年,387(2),p.189-194
EL-NAGGAR,A.M. et al.,Synthesis and biological activity of some new 4-(aminoacyl)aminopyridines and 2-(aminoacyl)aminopyrimidine derivatives,Polish Journal of Chemistry ,1982年,56(10-12),p.1279-1285
BRAICHENKO,V.T. et al.,N-aryl-β-amino acids. III. N-aryl-sulfonyl-β-alanine hydrazides,Khimiko-Farmatsevticheskii Zhurnal,1972年,6(8),p.6-8
MUKHERJEE,G.N. and CHAKRABORTY,P.K.,Metal complexes of some peptide derivatives. Part-XIV. Complex formation of copper(II) with N-benzenesulfonamides of some dipeptides,Journal of the Indian Chemical Society ,2002年,79(2),p.137-141
SELVAMURUGAN,V. and AIDHEN,I.S.,Simple synthetic equivalents for the β-(N,N-disubstituted)ethylamino acyl cation synthon and their applications,Synthesis,2001年,(15),p.2239-2246
PAUL,H. et al.,Synthesis of β-(β-alanylamino)propionamidine and cis- and trans-(+-)-amidinomycin,Archiv der Pharmazie und Berichte der Deutschen Pharmazeutischen Gesellschaft,1968年,301(7),p.512-519
EI-SHARIEF,A.M. et al.,Amino acids in the synthesis of heterocyclic systems: The synthesis of triazinoquinazolinones, triazepinoquinazolinones and triazocinoquinazolinones of potential biological interest,Molecules [online computer file] ,2001年,6(3),p.267-278
SHOEB,A. et al.,Oral hypoglycemic agents. IV. Synthesis of 1-arylsulfonyl-3-substituted-2-imidazolidinones and 1,2,3-trisubstituted ureas,Indian Journal of Chemistry,1965年,3(11),p.507-509
SEN,A.B. and YAJNIK,M.S.,Synthesis of peptides of β-amino acids,Journal of the Indian Chemical Society,1965年,42(3),p.145-148
MOLANDER,G.A. and STENGEL,P.J.,Reduction of 2-acylaziridines by samarium(II) iodide. An efficient and regioselective route to β-amino carbonyl compounds,TETRAHEDRON,NL,ELSEVIER SCIENCE PUBLISHERS,1997年 6月30日,53(26),p.8887-8912
SARTORI,E. et al.,Synthesis and activities of new arylsulfonamide thromboxane A2 receptor antagonists,EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,フランス,EDITIONS SCIENTIFIQUE ELSEVIER,1993年,28(7-8),p.625-632
Attorney, Agent or Firm:
Koichi Tsujii
Sadao Kumakura
Atsushi Hakoda
Kenji Asai
Kazuo Yamazaki
Satsuki Ichikawa
Yasushi Sasaki
Sadao Kumakura
Atsushi Hakoda
Kenji Asai
Kazuo Yamazaki
Satsuki Ichikawa
Yasushi Sasaki