JP2002502844A - 5員複素環縮合ベンゾ誘導体、その調製及び医薬品としてのそれらの使用 - Google Patents

5員複素環縮合ベンゾ誘導体、その調製及び医薬品としてのそれらの使用

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Publication number
JP2002502844A
JP2002502844A JP2000530502A JP2000530502A JP2002502844A JP 2002502844 A JP2002502844 A JP 2002502844A JP 2000530502 A JP2000530502 A JP 2000530502A JP 2000530502 A JP2000530502 A JP 2000530502A JP 2002502844 A JP2002502844 A JP 2002502844A
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Japan
Prior art keywords
group
methyl
alkyl
substituted
carboxy
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
JP2000530502A
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English (en)
Japanese (ja)
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JP2002502844A5 (enExample
Inventor
ウーヴェ リース
ノルベルト ハウエル
ゲルハルト ミーム
ヘンニング プリープケ
クラウス ビンデル
ジャン マリー シュターセン
ヴォルフガング ヴィーネン
ライネル ツィンマーマン
Original Assignee
ベーリンガー インゲルハイム ファルマ コマンディトゲゼルシャフト
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Priority claimed from DE1998104085 external-priority patent/DE19804085A1/de
Priority claimed from DE1998134325 external-priority patent/DE19834325A1/de
Application filed by ベーリンガー インゲルハイム ファルマ コマンディトゲゼルシャフト filed Critical ベーリンガー インゲルハイム ファルマ コマンディトゲゼルシャフト
Publication of JP2002502844A publication Critical patent/JP2002502844A/ja
Publication of JP2002502844A5 publication Critical patent/JP2002502844A5/ja
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/56Benzoxazoles; Hydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/24Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with an alkyl or cycloalkyl radical attached to the ring nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/16Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62Benzothiazoles
    • C07D277/64Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
    • 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
    • C07D401/06Heterocyclic 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
    • 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
    • C07D401/08Heterocyclic 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
    • 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/08Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6503Five-membered rings
    • C07F9/6506Five-membered rings having the nitrogen atoms in positions 1 and 3
    • C07F9/65068Five-membered rings having the nitrogen atoms in positions 1 and 3 condensed with carbocyclic rings or carbocyclic ring systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Furan Compounds (AREA)
JP2000530502A 1998-02-03 1999-01-28 5員複素環縮合ベンゾ誘導体、その調製及び医薬品としてのそれらの使用 Pending JP2002502844A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
DE1998104085 DE19804085A1 (de) 1998-02-03 1998-02-03 5-Gliedrige heterocyclische kondensierte Benzoderivate, deren Herstellung und deren Verwendung als Arzneimittel
DE1998134325 DE19834325A1 (de) 1998-07-30 1998-07-30 5-Gliedrige heterocyclische kondensierte Derivate, deren Herstellung und deren Verwendung als Arzneimittel
DE19834325.6 1998-07-30
DE19804085.7 1998-07-30
PCT/EP1999/000537 WO1999040072A1 (de) 1998-02-03 1999-01-28 5-gliedrige benzokondensierte heterocyclen als antithrombotika

Publications (2)

Publication Number Publication Date
JP2002502844A true JP2002502844A (ja) 2002-01-29
JP2002502844A5 JP2002502844A5 (enExample) 2006-03-23

Family

ID=26043548

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2000530502A Pending JP2002502844A (ja) 1998-02-03 1999-01-28 5員複素環縮合ベンゾ誘導体、その調製及び医薬品としてのそれらの使用

Country Status (5)

Country Link
EP (1) EP1060166A1 (enExample)
JP (1) JP2002502844A (enExample)
AU (1) AU2720199A (enExample)
CA (1) CA2319494A1 (enExample)
WO (1) WO1999040072A1 (enExample)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010511635A (ja) * 2006-12-04 2010-04-15 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 Hiv複製の阻害剤
JP2011507929A (ja) * 2007-12-28 2011-03-10 アジェンデ・キミケ・リウニテ・アンジェリニ・フランチェスコ・ア・チ・エレ・ア・エフェ・ソシエタ・ペル・アチオニ 5位置換アザインドール誘導体,それを含む医薬組成物,中間化合物及びその製造方法
JP2013538800A (ja) * 2010-08-10 2013-10-17 アッヴィ・インコーポレイテッド 新規trpv3モジュレーター
JP2015532916A (ja) * 2012-09-21 2015-11-16 サノフイ Apj受容体モジュレーターとしてのベンゾイミダゾールカルボン酸アミド誘導体

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AR023510A1 (es) 1999-04-21 2002-09-04 Astrazeneca Ab Un equipo de partes, formulacion farmaceutica y uso de un inhibidor de trombina.
EP1214330A1 (en) * 1999-09-21 2002-06-19 LION Bioscience AG Benzimidazole derivatives and combinatorial libraries thereof
DK1220844T3 (da) * 1999-09-24 2003-07-28 Boehringer Ingelheim Pharma Arylsulfonamid-substituerede benzimidazolderivater og deres anvendelse som tryptase-inhibitorer
US6407130B1 (en) 1999-11-10 2002-06-18 Boehringer Ingelheim Pharma Kg Carboxamide-substituted benzimidazoles having tryptase-inhibiting activity
DE19953899A1 (de) * 1999-11-10 2001-05-17 Boehringer Ingelheim Pharma Carboxamid-substituierte Benzimidazolderivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
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
US6448281B1 (en) * 2000-07-06 2002-09-10 Boehringer Ingelheim (Canada) Ltd. Viral polymerase inhibitors
US6670364B2 (en) 2001-01-31 2003-12-30 Telik, Inc. Antagonists of MCP-1 function and methods of use thereof
US6962926B2 (en) 2001-01-31 2005-11-08 Telik, Inc. Antagonist of MCP-1 function, and compositions and methods of use thereof
US6656956B2 (en) 2001-02-08 2003-12-02 Boehringer Ingelheim Pharma Kg Benzimidazole derivatives, processes for preparing them and their use as pharmaceutical compositions
DE10105628A1 (de) * 2001-02-08 2002-08-22 Boehringer Ingelheim Pharma Benzimidazolderivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
TWI245761B (en) 2001-03-01 2005-12-21 Telik Inc Antagonists of MCP-1 function and methods of use thereof
TWI236474B (en) 2001-04-03 2005-07-21 Telik Inc Antagonists of MCP-1 function and methods of use thereof
HUP0400467A3 (en) * 2001-04-19 2012-08-28 Eisai R & D Man Co 2-iminopyrrolidine derivatives, pharmaceutical compositions containing them and their use
DE10125478A1 (de) * 2001-05-25 2002-11-28 Boehringer Ingelheim Pharma Verwendung bicyclischer Heterocyclen zur Behandlung und Vorbeugung arterieller thrombotischer Erkrankungen
US7232924B2 (en) 2001-06-11 2007-06-19 Xenoport, Inc. Methods for synthesis of acyloxyalkyl derivatives of GABA analogs
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
US7186855B2 (en) 2001-06-11 2007-03-06 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
EP1569912B1 (en) 2002-12-03 2015-04-29 Pharmacyclics, Inc. 2-(2-hydroxybiphenyl-3-yl)-1h-benzoimidazole-5-carboxamidine derivatives as factor viia inhibitors
AU2003215664A1 (en) * 2002-03-21 2003-10-08 Basf Aktiengesellschaft Fungicidal triazolopyrimidines, methods for producing the same, use thereof for combating harmful fungi and agents containing said substances
JP4628678B2 (ja) * 2002-03-29 2011-02-09 ノバルティス バクシンズ アンド ダイアグノスティックス,インコーポレーテッド 置換ベンズアゾールおよびRafキナーゼ阻害剤としてのそれらの使用
JP4334476B2 (ja) * 2002-07-29 2009-09-30 株式会社静岡カフェイン工業所 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
PE20040804A1 (es) * 2002-12-19 2004-12-31 Boehringer Ingelheim Pharma DERIVADOS DE CARBOXAMIDAS COMO INHIBIDORES DEL FACTOR Xa
AU2004218187C1 (en) 2003-02-19 2011-04-07 Eisai R&D Management Co., Ltd. Methods for producing cyclic benzamidine derivatives
BRPI0515522A (pt) * 2004-09-21 2008-07-29 Athersys Inc composto, composição farmacêutica. métodos de inibir a ligação de ligandos endógenos ao receptor crth-2 em uma célula, de tratar, melhorar ou prevenir um distúrbio responsivo à inibição da ligação de ligandos endógenos ao receptor crth-2 em um animal e de preparar um composto, e, kit
ES2318556T3 (es) * 2004-11-02 2009-05-01 Pfizer, Inc. Derivados de sulfonil bencimidazol.
US7514460B2 (en) 2004-12-22 2009-04-07 4Sc Ag Benzazole analogues and uses thereof
WO2012129491A1 (en) 2011-03-24 2012-09-27 Abbott Laboratories Trpv3 modulators
CA2853097A1 (en) 2011-10-24 2013-05-02 Abbvie Inc. Novel trpv3 modulators
US9056874B2 (en) 2012-05-04 2015-06-16 Novartis Ag Complement pathway modulators and uses thereof
JP6488239B2 (ja) 2013-01-18 2019-03-20 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Rock阻害剤としてのフタラジノンおよびイソキノリノン
JP6387391B2 (ja) 2013-03-14 2018-09-05 ノバルティス アーゲー 眼科疾患の処置に有用な補体因子B阻害剤としての2−(1H−インドール−4−イルメチル)−3H−イミダゾ[4,5−b]ピリジン−6−カルボニトリル誘導体
EP3089963A1 (en) 2013-10-30 2016-11-09 Novartis AG 2-benzyl-benzimidazole complement factor b inhibitors and uses thereof
US9902702B2 (en) 2014-07-15 2018-02-27 Bristol-Myers Squibb Company Spirocycloheptanes as inhibitors of rock
WO2016187620A2 (en) * 2015-05-21 2016-11-24 The Regents Of The University Of California Anti-cancer compounds
KR102494294B1 (ko) 2016-06-24 2023-01-31 더 리전트 오브 더 유니버시티 오브 캘리포니아 Parp1, pap2 및/또는 튜블린의 저해제로서 암 치료에 유용한 프탈라진 유도체
WO2024243692A1 (en) * 2023-05-30 2024-12-05 Queen's University At Kingston Cyp26b1 inhibitor compounds and methods of use thereof

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Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010511635A (ja) * 2006-12-04 2010-04-15 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 Hiv複製の阻害剤
JP2011507929A (ja) * 2007-12-28 2011-03-10 アジェンデ・キミケ・リウニテ・アンジェリニ・フランチェスコ・ア・チ・エレ・ア・エフェ・ソシエタ・ペル・アチオニ 5位置換アザインドール誘導体,それを含む医薬組成物,中間化合物及びその製造方法
JP2013538800A (ja) * 2010-08-10 2013-10-17 アッヴィ・インコーポレイテッド 新規trpv3モジュレーター
JP2015532916A (ja) * 2012-09-21 2015-11-16 サノフイ Apj受容体モジュレーターとしてのベンゾイミダゾールカルボン酸アミド誘導体

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CA2319494A1 (en) 1999-08-12
AU2720199A (en) 1999-08-23
WO1999040072A1 (de) 1999-08-12
EP1060166A1 (de) 2000-12-20

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