ES2080919T3 - Nuevos derivados de bencimidazol y de azabencimidazol, antagonistas de los receptores al tromboxano, sus procedimientos de preparacion, intermediarios de sintesis, composiciones que los contienen. - Google Patents

Nuevos derivados de bencimidazol y de azabencimidazol, antagonistas de los receptores al tromboxano, sus procedimientos de preparacion, intermediarios de sintesis, composiciones que los contienen.

Info

Publication number
ES2080919T3
ES2080919T3 ES91400393T ES91400393T ES2080919T3 ES 2080919 T3 ES2080919 T3 ES 2080919T3 ES 91400393 T ES91400393 T ES 91400393T ES 91400393 T ES91400393 T ES 91400393T ES 2080919 T3 ES2080919 T3 ES 2080919T3
Authority
ES
Spain
Prior art keywords
radical
lower alkyl
group
hydrogen atom
cycloalkyl
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.)
Expired - Lifetime
Application number
ES91400393T
Other languages
English (en)
Inventor
Nicole Bru-Magniez
Eric Nicolai
Jean-Marie Teulon
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.)
UNION PHARMA SCIENT APPL
UPSA SAS
Original Assignee
UNION PHARMA SCIENT APPL
UPSA SAS
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 UNION PHARMA SCIENT APPL, UPSA SAS filed Critical UNION PHARMA SCIENT APPL
Application granted granted Critical
Publication of ES2080919T3 publication Critical patent/ES2080919T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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Classifications

    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • 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
    • 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
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D235/28—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6503—Five-membered rings
    • C07F9/6506—Five-membered rings having the nitrogen atoms in positions 1 and 3
    • C07F9/65068—Five-membered rings having the nitrogen atoms in positions 1 and 3 condensed with carbocyclic rings or carbocyclic ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)

Abstract

LA PRESENTE INVENCION SE REFIERE A LOS DERIVADOS DE FORMULA: EN LA QUE A ES UN NUCLEO AROMATICO O UN HETEROCICLO QUE CONTIENE NITROGENO. X SUB 1, X SUB 2, X SUB 3 Y X SUB 4 REPRESENTAN INDEPENDIENTEMENTE UN ATOMO DE HIDROGENO, UN ATOMO DE HALOGENO, UN RADICAL ALQUILO INFERIOR, UN RADICAL CICLOALQUILO DE C SUB 3 -C SUB 7, UN RADICAL ALCOXI, UN RADICAL TIOALQUILO, UN GRUPO SULFONA, SO SUB 2 ALQUILO INFERIOR, UN GRUPO SULFOXIDO, SO ALQUILO INFERIOR, UN GRUPO TRIFLUORMETILO, UN GRUPO NITRO, UN GRUPO HIDROXILO, UN RADICAL METILENO ALCOHOL O UNA FUNCION COOR'' DONDE R'' ES UN HIDROGENO O UN ALQUILO INFERIOR. X SUB 3 Y X SUB 4 PUEDEN TAMBIEN FORMAR CON EL FENILO UN NAFTALENO. B REPRESENTA CR SUB 5 R SUB 6, SIENDO R SUB 5 Y R SUB 6 UN ATOMO DE HIDROGENO O UN RADICAL ALQUILO INFERIOR, O UN RADICAL CICLOALQUILO DE C SUB 3 -C SUB 7 O UN ATOMO DE AZUFRE. R SUB 1, R SUB 2, R SUB 3 Y R SUB 4 REPRESENTAN INDEPENDIENTEMENTE UN ATOMO DE HIDROGENO O UN RADICAL ALQUILO INFERIOR O UN RADICAL CICLOALQUILO DE C SUB 3 -C SUB 7. CR SUB 1 R SUB 2 O CR SUB 3 R SUB 4 PUEDEN FORMAR CON B, CUANDO ESTE ULTIMO REPRESENTA CR SUB 5 R SUB 6, UN CICLOALQUILO O UN CICLOALQUENO DE 3 A 7 ATOMOS DE CARBONO. R SUB 1 R SUB 2 , R SUB 3 R SUB 4 PUEDEN TAMBIEN FORMAR UN CICLO DE 3 A 7 ATOMOS DE CARBONO. N ES UN NUMERO ENTERO DE 1 A 4 Y PUEDE SER 0 SI R SUB 1 Y R SUB 2 NO SON HIDROGENO. D REPRESENTA UNA FUNCION QUIMICA QUE PUEDE SER COOR SUB 7, SIENDO R SUB 7 UN ATOMO DE HIDROGENO O UN RADICAL ALQUILO INFERIOR O UN RADICAL CICLOALQUILO DE C SUB 3 -C SUB 7 CONH-R SUB 8, SIENDO R SUB 8 UN ATOMO DE HIDROGENO O UN RADICAL INFERIOR O UN RADICAL CICLOALQUILO DE C SUB 3 -C SUB 7 CN ASI COMO SUS SALES DE ADICION.
ES91400393T 1990-02-16 1991-02-15 Nuevos derivados de bencimidazol y de azabencimidazol, antagonistas de los receptores al tromboxano, sus procedimientos de preparacion, intermediarios de sintesis, composiciones que los contienen. Expired - Lifetime ES2080919T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
FR9001925A FR2658511B1 (fr) 1990-02-16 1990-02-16 Nouveaux derives de benzimidazole et d'azabenzimidazole, antagonistes des recepteurs au thromboxane; leurs procedes de preparation, compositions pharmaceutiques les contenant.

Publications (1)

Publication Number Publication Date
ES2080919T3 true ES2080919T3 (es) 1996-02-16

Family

ID=9393829

Family Applications (1)

Application Number Title Priority Date Filing Date
ES91400393T Expired - Lifetime ES2080919T3 (es) 1990-02-16 1991-02-15 Nuevos derivados de bencimidazol y de azabencimidazol, antagonistas de los receptores al tromboxano, sus procedimientos de preparacion, intermediarios de sintesis, composiciones que los contienen.

Country Status (18)

Country Link
US (2) US5021443A (es)
EP (1) EP0442820B1 (es)
JP (1) JPH05155858A (es)
KR (1) KR910021382A (es)
AT (1) ATE127794T1 (es)
AU (1) AU638096B2 (es)
CA (1) CA2035710A1 (es)
DE (1) DE69112863T2 (es)
DK (1) DK0442820T3 (es)
ES (1) ES2080919T3 (es)
FR (1) FR2658511B1 (es)
GR (1) GR3018000T3 (es)
IE (1) IE910339A1 (es)
IL (2) IL97191A0 (es)
LV (1) LV11028B (es)
NZ (1) NZ237121A (es)
PT (1) PT96792A (es)
ZA (1) ZA911061B (es)

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US5128359A (en) * 1990-02-16 1992-07-07 Laboratoires Upsa Benzimidazole and azabenzimidazole derivatives which are thromboxane receptor antagonists, their methods of preparation
DE4200954A1 (de) * 1991-04-26 1992-10-29 Bayer Ag Heterocyclisch substituierte phenylessigsaeurederivate
TW300219B (es) * 1991-09-14 1997-03-11 Hoechst Ag
US5187159A (en) * 1991-10-07 1993-02-16 Merck & Co., Inc. Angiotensin II antagonists incorporating a substituted 1,3-benzodioxole or 1,3-benzodithiole
US5468757A (en) * 1994-01-31 1995-11-21 Eli Lilly And Company 6-azaindole thromboxane synthase inhibitors
EP1402895A1 (en) * 1997-03-07 2004-03-31 Metabasis Therapeutics, Inc. Benzimidazole inhibitors of fructose 1,6-biphosphatase
WO1998039343A1 (en) * 1997-03-07 1998-09-11 Metabasis Therapeutics, Inc. Novel benzimidazole inhibitors of fructose-1,6-bisphosphatase
AU6452098A (en) * 1997-03-07 1998-09-22 Metabasis Therapeutics, Inc. Novel purine inhibitors of fructose-1,6-bisphosphatase
JP3585839B2 (ja) * 1997-12-17 2004-11-04 メルク エンド カムパニー インコーポレーテッド インテグリン受容体拮抗薬
US6911462B2 (en) * 1998-05-22 2005-06-28 Avanir Pharmaceuticals Benzimidazole compounds for regulating IgE
US6919366B2 (en) * 1998-05-22 2005-07-19 Avanir Pharmaceuticals Benzimidazole derivatives as modulators of IgE
US20050267148A1 (en) * 1998-07-15 2005-12-01 Teijin Limited Benzimidazole derivative
WO2000003997A1 (fr) * 1998-07-15 2000-01-27 Teijin Limited Derives de thiobenzimidazole
US6312723B1 (en) 1999-08-26 2001-11-06 Robert R. Whittle Pharmaceutical unit dosage form
US6262086B1 (en) 1999-08-26 2001-07-17 Robert R. Whittle Pharmaceutical unit dosage form
US6268385B1 (en) 1999-08-26 2001-07-31 Robert R. Whittle Dry blend pharmaceutical formulations
US6262085B1 (en) 1999-08-26 2001-07-17 Robert R. Whittle Alkoxy substituted Benzimidazole compounds, pharmaceutical preparations containing the same, and methods of using the same
US6312712B1 (en) 1999-08-26 2001-11-06 Robert R. Whittle Method of improving bioavailability
US6326384B1 (en) 1999-08-26 2001-12-04 Robert R. Whittle Dry blend pharmaceutical unit dosage form
US6316020B1 (en) 1999-08-26 2001-11-13 Robert R. Whittle Pharmaceutical formulations
US6780880B1 (en) 1999-08-26 2004-08-24 Robert R. Whittle FT-Raman spectroscopic measurement
US6369087B1 (en) 1999-08-26 2002-04-09 Robert R. Whittle Alkoxy substituted benzimidazole compounds, pharmaceutical preparations containing the same, and methods of using the same
CA2365118A1 (en) * 2000-01-17 2001-07-26 Teijin Limited Inhibitor against human chymase activity
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JP2004528304A (ja) * 2001-03-12 2004-09-16 アバニール・ファーマシューティカルズ ＩｇＥを調節し、細胞増殖を阻害するためのベンゾイミダゾール化合物
KR100902799B1 (ko) * 2001-08-24 2009-06-12 데이진 가부시키가이샤 키마제 저해제 및 ａｃｅ 저해제를 유효성분으로 함유하는약제
TW200304820A (en) * 2002-03-25 2003-10-16 Avanir Pharmaceuticals Use of benzimidazole analogs in the treatment of cell proliferation
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
AU2003270426A1 (en) 2002-09-12 2004-04-30 Avanir Pharmaceuticals PHENYL-INDOLE COMPOUNDS FOR MODULATING IgE AND INHIBITING CELLULAR PROLIFERATION
TWI276631B (en) * 2002-09-12 2007-03-21 Avanir Pharmaceuticals Phenyl-aza-benzimidazole compounds for modulating IgE and inhibiting cellular proliferation
AU2003282510A1 (en) * 2002-10-11 2004-05-04 Bristol-Myers Squibb Company Hexahydro-benzimidazolone compounds useful as anti-inflammatory agents
JP2007501618A (ja) * 2003-08-08 2007-02-01 アバニール・ファーマシューティカルズ タンパク質輸送の選択的薬理学的阻害、および関連した、ヒト疾患を治療する方法
DE102004027821A1 (de) * 2004-06-08 2006-01-05 Boehringer Ingelheim Pharma Gmbh & Co. Kg Benzimidazole, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel
JP4953455B2 (ja) * 2004-09-30 2012-06-13 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 選択的アンドロゲン受容体モジュレーター（ｓａｒｍ）として有用な新規なベンゾイミダゾール誘導体
WO2008153129A1 (ja) * 2007-06-14 2008-12-18 Teijin Pharma Limited 尿酸値低下剤
KR20130026504A (ko) * 2010-07-14 2013-03-13 큠버랜드 에멀징 테크놀로지스 아이앤씨 트롬복산-a2 수용체 길항제를 이용한 간신증후군 및 간성뇌증의 치료방법
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US8952177B2 (en) 2013-03-15 2015-02-10 Janssen Pharmaceutica Nv 1,2,6-substituted benzimidazoles as FLAP modulators
US9682971B2 (en) 2013-03-15 2017-06-20 Janssen Pharmaceutica Nv 1,2,5-Substituted benzimidazoles as flap modulators
CN113329996B (zh) * 2018-06-25 2023-03-10 博远医药(苏州)有限公司 用于治疗刺猬途径相关病症的化合物和方法

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Also Published As

Publication number Publication date
ATE127794T1 (de) 1995-09-15
FR2658511A1 (fr) 1991-08-23
EP0442820A1 (fr) 1991-08-21
EP0442820B1 (fr) 1995-09-13
FR2658511B1 (fr) 1992-06-19
DE69112863T2 (de) 1996-03-28
CA2035710A1 (en) 1991-08-17
JPH05155858A (ja) 1993-06-22
PT96792A (pt) 1991-10-31
DE69112863D1 (de) 1995-10-19
IL97191A (en) 1995-03-15
KR910021382A (ko) 1991-12-20
AU7087491A (en) 1991-08-22
IE910339A1 (en) 1991-08-28
LV11028B (en) 1996-06-20
LV11028A (lv) 1996-02-20
GR3018000T3 (en) 1996-02-29
IL97191A0 (en) 1992-05-25
AU638096B2 (en) 1993-06-17
US5021443A (en) 1991-06-04
DK0442820T3 (da) 1996-02-05
NZ237121A (en) 1993-12-23
ZA911061B (en) 1991-11-27
US5124336A (en) 1992-06-23

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