BG105111A - Бензимидазоли, тяхното получаване и употребата имкато лекарствени средства - Google Patents

Бензимидазоли, тяхното получаване и употребата имкато лекарствени средства

Info

Publication number
BG105111A
BG105111A BG105111A BG10511101A BG105111A BG 105111 A BG105111 A BG 105111A BG 105111 A BG105111 A BG 105111A BG 10511101 A BG10511101 A BG 10511101A BG 105111 A BG105111 A BG 105111A
Authority
BG
Bulgaria
Prior art keywords
compounds
useful
production
formula
group
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
BG105111A
Other languages
English (en)
Inventor
Uwe Ries
Iris Kauffmann
Norbert Hauel
Henning Priepke
Herbert Nar
Jean Marie Stassen
Wolfgang Wienen
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Boehringer Ingelheim Pharma GmbH Co KG
Original Assignee
Boehringer Ingelheim Pharma GmbH Co KG
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
Priority claimed from DE1998129964 external-priority patent/DE19829964A1/de
Priority claimed from DE1998157202 external-priority patent/DE19857202A1/de
Priority claimed from DE1999112690 external-priority patent/DE19912690A1/de
Application filed by Boehringer Ingelheim Pharma GmbH Co KG filed Critical Boehringer Ingelheim Pharma GmbH Co KG
Publication of BG105111A publication Critical patent/BG105111A/bg
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/12—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/14—Radicals substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/16—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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
    • C07D401/08—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 alicyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/08—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing alicyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Abstract

Съединенията имат формула, в която значенията на Ra до Rc, A, Ar и В са посочени в описанието. Изобретението се отнася и до техни тавтомери, стереоизомери, смеси, пролекарства и производни, които на мястото на карбоксилна група съдържат група, коятопри физиологичните условия е отрицателно заредена, и до техни соли, по-специално до техни физиологично приемливи соли с неорганични или органични киселини или основи. Съединенията с посочената формула, в която Rc e цианогрупа, са междинни продукти за получаване на останалите съединения със същата формула, а тези, в чиято формула Rc е една от посочените в описанието амидиногрупи, имат ценни фармакологични свойства, по-специално антитромбозна активност.
BG105111A 1998-07-04 2001-01-03 Бензимидазоли, тяхното получаване и употребата имкато лекарствени средства Pending BG105111A (bg)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
DE1998129964 DE19829964A1 (de) 1998-07-04 1998-07-04 Benzimidazole, deren Herstellung und deren Verwendung als Arzneimittel
DE1998157202 DE19857202A1 (de) 1998-12-11 1998-12-11 Benzimidazole, deren Herstellung und deren Verwendung als Arzneimittel
DE1999112690 DE19912690A1 (de) 1999-03-20 1999-03-20 Benzimidazole, deren Herstellung und deren Verwendung als Arzneimittel
PCT/EP1999/004531 WO2000001704A2 (de) 1998-07-04 1999-07-01 Benzimidazole, deren herstellung und deren verwendung als arzneimittel

Publications (1)

Publication Number Publication Date
BG105111A true BG105111A (bg) 2001-12-29

Family

ID=27218486

Family Applications (1)

Application Number Title Priority Date Filing Date
BG105111A Pending BG105111A (bg) 1998-07-04 2001-01-03 Бензимидазоли, тяхното получаване и употребата имкато лекарствени средства

Country Status (34)

Country Link
EP (1) EP1095025B1 (bg)
JP (1) JP4224215B2 (bg)
KR (1) KR20010083087A (bg)
CN (1) CN1152866C (bg)
AR (1) AR019222A1 (bg)
AT (1) ATE229511T1 (bg)
AU (1) AU763094C (bg)
BG (1) BG105111A (bg)
BR (1) BR9911826A (bg)
CA (1) CA2337804C (bg)
CO (1) CO5080729A1 (bg)
DE (1) DE59903765D1 (bg)
DK (1) DK1095025T3 (bg)
EA (1) EA003947B1 (bg)
EE (1) EE04236B1 (bg)
ES (1) ES2188192T3 (bg)
HK (1) HK1036976A1 (bg)
HR (1) HRPK20010007B1 (bg)
HU (1) HUP0200710A3 (bg)
ID (1) ID26774A (bg)
IL (1) IL140060A0 (bg)
MX (1) MXPA00012819A (bg)
MY (1) MY123310A (bg)
NO (1) NO20010028D0 (bg)
NZ (1) NZ509625A (bg)
PE (1) PE20000754A1 (bg)
PL (1) PL345852A1 (bg)
PT (1) PT1095025E (bg)
SK (1) SK283744B6 (bg)
TR (1) TR200100148T2 (bg)
TW (1) TWI248435B (bg)
UA (1) UA70951C2 (bg)
WO (1) WO2000001704A2 (bg)
YU (1) YU84700A (bg)

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DE19907813A1 (de) * 1999-02-24 2000-08-31 Boehringer Ingelheim Pharma Substituierte bicyclische Heterocyclen, deren Herstellung und deren Verwendung als Arzneimittel
AR023510A1 (es) 1999-04-21 2002-09-04 Astrazeneca Ab Un equipo de partes, formulacion farmaceutica y uso de un inhibidor de trombina.
US6451832B2 (en) 1999-12-23 2002-09-17 Boehringer Ingelheim Pharma Kg Benzimidazoles with antithrombotic activity
DE19962329A1 (de) * 1999-12-23 2001-06-28 Boehringer Ingelheim Pharma Benzimidazole, deren Herstellung und deren Verwendung als Arzneimittel
EP1193248A1 (en) 2000-09-30 2002-04-03 Aventis Pharma Deutschland GmbH Malonamid and malonamic ester derivatives with antithrombotic activity, their preparation and their use
US6818787B2 (en) 2001-06-11 2004-11-16 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
US8048917B2 (en) 2005-04-06 2011-11-01 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
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DE10227668A1 (de) * 2002-06-20 2004-01-08 Boehringer Ingelheim Pharma Gmbh & Co. Kg Arzneimittel zur Behandlung des systemic inflammatory response syndrome
WO2004010996A1 (ja) * 2002-07-29 2004-02-05 Shizuoka Coffein Co., Ltd. 1,3アゾール誘導体及び同誘導体を含む血栓症治療のための医薬組成物
AU2003302238A1 (en) 2002-12-03 2004-06-23 Axys Pharmaceuticals, Inc. 2-(2-hydroxybiphenyl-3-yl)-1h-benzoimidazole-5-carboxamidine derivatives as factor viia inhibitors
PE20040804A1 (es) 2002-12-19 2004-12-31 Boehringer Ingelheim Pharma DERIVADOS DE CARBOXAMIDAS COMO INHIBIDORES DEL FACTOR Xa
DE10359797A1 (de) 2003-12-19 2005-07-21 Bayer Chemicals Ag Verfahren zur Herstellung von N,N'-Carbonyldiazolen
US7371743B2 (en) 2004-02-28 2008-05-13 Boehringer Ingelheim International Gmbh Carboxylic acid amides, the preparation thereof and their use as medicaments
TWI350168B (en) * 2004-05-07 2011-10-11 Incyte Corp Amido compounds and their use as pharmaceuticals
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EP1609784A1 (de) 2004-06-25 2005-12-28 Boehringer Ingelheim Pharma GmbH & Co.KG Verfahren zur Herstellung von 4-(Benzimidazolylmethylamino)-Benzamidinen
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
DE102005061623A1 (de) * 2005-12-21 2007-06-28 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verbessertes Verfahren zur Herstellung von 4-(Benzimidazolylmethylamino)-Benzamidinen und deren Salzen
DE102005061624A1 (de) * 2005-12-21 2007-06-28 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verbessertes Verfahren zur Herstellung von Salzen von 4-(Benzimidazolylmethylamino)-Benzamidinen
JP5662319B2 (ja) * 2008-09-09 2015-01-28 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング アザ−ベンゾイミダゾロンキマーゼ阻害剤
US20110301192A1 (en) * 2008-10-01 2011-12-08 The Regents Of The University Of California Inhibitors of Cyclin Kinase Inhibitor p21
JP5535931B2 (ja) 2008-10-27 2014-07-02 武田薬品工業株式会社 二環性化合物
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PE121699A1 (es) * 1997-02-18 1999-12-08 Boehringer Ingelheim Pharma Heterociclos biciclicos disustituidos como inhibidores de la trombina

Also Published As

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MY123310A (en) 2006-05-31
CA2337804A1 (en) 2000-01-13
AU763094C (en) 2004-01-08
UA70951C2 (uk) 2004-11-15
DE59903765D1 (de) 2003-01-23
EP1095025B1 (de) 2002-12-11
NZ509625A (en) 2003-08-29
HRPK20010007B1 (en) 2003-04-30
ID26774A (id) 2001-02-08
JP2002519429A (ja) 2002-07-02
SK82001A3 (en) 2001-08-06
EP1095025A2 (de) 2001-05-02
WO2000001704A2 (de) 2000-01-13
CN1308614A (zh) 2001-08-15
JP4224215B2 (ja) 2009-02-12
AR019222A1 (es) 2001-12-26
DK1095025T3 (da) 2003-04-07
PL345852A1 (en) 2002-01-14
IL140060A0 (en) 2002-02-10
KR20010083087A (ko) 2001-08-31
CA2337804C (en) 2008-12-09
CN1152866C (zh) 2004-06-09
EE200100009A (et) 2002-06-17
ATE229511T1 (de) 2002-12-15
PE20000754A1 (es) 2000-08-25
HK1036976A1 (en) 2002-01-25
TR200100148T2 (tr) 2001-09-21
MXPA00012819A (es) 2004-06-03
EE04236B1 (et) 2004-02-16
AU4903399A (en) 2000-01-24
HUP0200710A3 (en) 2003-05-28
HRP20010007A2 (en) 2001-12-31
ES2188192T3 (es) 2003-06-16
YU84700A (sh) 2003-02-28
PT1095025E (pt) 2003-04-30
NO20010028L (no) 2001-01-03
SK283744B6 (sk) 2003-12-02
CO5080729A1 (es) 2001-09-25
EA003947B1 (ru) 2003-10-30
AU763094B2 (en) 2003-07-10
EA200100042A1 (ru) 2001-06-25
WO2000001704A3 (de) 2000-04-06
HUP0200710A2 (en) 2002-06-29
TWI248435B (en) 2006-02-01
BR9911826A (pt) 2001-03-27
NO20010028D0 (no) 2001-01-03

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