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

Links

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)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Immunology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Transplantation (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (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
US6110903A (en) * 1997-03-07 2000-08-29 Sankyo Company Ltd. Benzimidazole inhibitors of fructose 1,6-bisphosphatase
EP1402895A1 (en) * 1997-03-07 2004-03-31 Metabasis Therapeutics, Inc. Benzimidazole inhibitors of fructose 1,6-biphosphatase
US6284748B1 (en) * 1997-03-07 2001-09-04 Metabasis Therapeutics, Inc. Purine inhibitors of fructose 1,6-bisphosphatase
IL136495A0 (en) * 1997-12-17 2001-06-14 Merck & Co Inc Integrin receptor antagonists
US6919366B2 (en) * 1998-05-22 2005-07-19 Avanir Pharmaceuticals Benzimidazole derivatives as modulators of IgE
US6911462B2 (en) * 1998-05-22 2005-06-28 Avanir Pharmaceuticals Benzimidazole compounds for regulating IgE
US20050267148A1 (en) * 1998-07-15 2005-12-01 Teijin Limited Benzimidazole derivative
TR200100047T2 (tr) * 1998-07-15 2001-10-22 Teijin Limited Tiyobenzimidazol türevleri
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
US6780880B1 (en) 1999-08-26 2004-08-24 Robert R. Whittle FT-Raman spectroscopic measurement
US6326384B1 (en) 1999-08-26 2001-12-04 Robert R. Whittle Dry blend pharmaceutical unit dosage form
US6312712B1 (en) 1999-08-26 2001-11-06 Robert R. Whittle Method of improving bioavailability
US6262086B1 (en) 1999-08-26 2001-07-17 Robert R. Whittle Pharmaceutical unit dosage form
US6316020B1 (en) 1999-08-26 2001-11-13 Robert R. Whittle Pharmaceutical formulations
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
US6312723B1 (en) 1999-08-26 2001-11-06 Robert R. Whittle Pharmaceutical unit dosage form
EP1167360A1 (en) * 2000-01-17 2002-01-02 Teijin Limited Human chymase inhibitors
WO2001089519A1 (en) * 2000-05-22 2001-11-29 Nitromed, Inc. Thromboxane inhibitors, compositions and methods of use related applications
HUP0303460A3 (en) * 2001-03-12 2004-07-28 Avanir Pharmaceuticals San Die Benzimidazole compounds for modulating ige and inhibiting cellular proliferation and pharmaceutical compositions containing them
JP4173098B2 (ja) * 2001-08-24 2008-10-29 帝人株式会社 キマーゼ阻害剤及びａｃｅ阻害剤を有効成分として含有する薬剤
TW200304820A (en) * 2002-03-25 2003-10-16 Avanir Pharmaceuticals Use of benzimidazole analogs in the treatment of cell proliferation
AU2002368133A1 (en) * 2002-07-29 2004-02-16 Shizuoka Coffein Co., Ltd. 1,3-azole derivative and medicinal composition containing the derivative for treatment for thombosis
TWI276631B (en) * 2002-09-12 2007-03-21 Avanir Pharmaceuticals Phenyl-aza-benzimidazole compounds for modulating IgE and inhibiting cellular proliferation
AU2003270426A1 (en) 2002-09-12 2004-04-30 Avanir Pharmaceuticals PHENYL-INDOLE 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
CA2533990A1 (en) * 2003-08-08 2005-02-17 Avanir Pharmaceuticals Selective pharmacologic inhibition of protein trafficking and related methods of treating human diseases
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
US20130197044A1 (en) * 2010-07-14 2013-08-01 Leo Pavliv Methods of treating hepatorenal syndrome and hepatic encephalopathy with thromboxane-a2 receptor antagonists
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US9695149B2 (en) 2013-03-15 2017-07-04 Janssen Pharmaceutica Nv 1,2,6-substituted benzimidazoles as flap modulators
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US4880804A (en) * 1988-01-07 1989-11-14 E. I. Du Pont De Nemours And Company Angiotensin II receptor blocking benzimidazoles

Also Published As

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

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