CO5080792A1 - Heterociclos biciclicos disustituidos, su preparacion y su empleo como medicamentos - Google Patents

Heterociclos biciclicos disustituidos, su preparacion y su empleo como medicamentos

Info

Publication number
CO5080792A1
CO5080792A1 CO99048371A CO99048371A CO5080792A1 CO 5080792 A1 CO5080792 A1 CO 5080792A1 CO 99048371 A CO99048371 A CO 99048371A CO 99048371 A CO99048371 A CO 99048371A CO 5080792 A1 CO5080792 A1 CO 5080792A1
Authority
CO
Colombia
Prior art keywords
group
alkyl
substituted
carboxy
phenyl
Prior art date
Application number
CO99048371A
Other languages
English (en)
Inventor
Norbert Hauel
Ries Uwe
Priepke Henning
Gerhard Mihm
Wolfgang Wienen
Jean Marie Stassen
Binder Klaus
Rainer Zimmermann
Original Assignee
Boehringer Ingelheim Pharma
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 Boehringer Ingelheim Pharma filed Critical Boehringer Ingelheim Pharma
Publication of CO5080792A1 publication Critical patent/CO5080792A1/es

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Classifications

    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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 to ring carbon atoms
    • C07D215/38—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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 to ring carbon atoms
    • C07D215/38—Nitrogen atoms
    • C07D215/40—Nitrogen atoms attached in position 8
    • 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
    • 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
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/79—Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D307/81—Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Heterociclos bicíclicos disustituidos de la fórmula general (I):Ra - Het - B - Ar - EEn la que B significa un grupo etileno, eventualmente sustituido con uno o dos grupos alquilo C1-3, pudiendo estar reemplazado un grupo metileno del grupo etileno, que está enlazado con el radical Het o Ar, por un átomo de oxígeno o azufre, por un grupo sulfinilo, sulfonilo, carbonilo o -NR1,representando R1 un átomo de hidrógeno o un grupo alquilo C1-6 , o B significa también un grupo alquileno C3-5 de cadena lineal, en el que un grupo metileno, que no está enlazado con el radical Het ni con el radical Ar, está reemplazado por un grupo -NR1, en el que R1, está definido como se ha mencionado precedentemente, E significa un grupo ciano o RbNH-C(=NH), en el queRb representa un átomo de hidrógeno, un grupo hidroxi, un grupo alquilo C1-3 o un radical separable in vivo,Ar significa un grupo fenileno o naftileno, eventualmente sustituido con un átomo de flúor, cloro bromo, con un grupo trifluorometilo, alquilo C1-3, o alcoxi C1-3, significa un grupo tienilo, tiazolileno, pirimidinileno, pirazinileno o piridazinileno eventualmente sustituido en el esqueleto de carbonos con un grupo alquilo C1-3, Het significa un heterociclo bicíclico de la fórmula<EMI FILE="99048371_1" ID="1" IMF=JPEG >X representa un átomo de nitrógeno o un grupo metino, eventualmente sustituido con un grupo alquilo C1-3, eY representa un grupo imino eventualmente sustituido con un grupo alquilo C1-5 o cicloalquilo C3-7 , o X representa un átomo de nitrógeno eY representa un grupo imino sustituido con un grupo alquilo C1-5 o cicloalquilo C3-7, estando sustituido el sustituyentes alquilo y cicloalquilo en cada caso con un grupo carboxi o con un grupo transformable in vivo en un grupo carboxi,Y Ra significa un grupo fenil-alcoxi C1-3,un grupo amino,un grupo alquil C1-3 -amino que está sustituido en el - 2 -átomo de nitrógeno adicionalmente con un grupo fenil-alquilo C1-3, un grupo R3 -CO-R4N O R3 -SO2 -R4N, en los que R3 representa un grupo alquilo C1-5, fenil-alquilo C1-3, cicloalquilo C3-7, fenilo, naftilo, piridilo, quinolilo, isoquinolilo, tetrahidroquinolilo o tetrahidroisoquinolilo yR4 representa un átomo de hidrógeno, un grupo alquilo C1-5 o fenil-alquilo C1-3, que en cada caso está sustituido en la parte de alquilo con un grupo transformable in vivo en un grupo carboxi, con un grupo carboxi o tetrazolilo, con un grupo aminocarbonilo o alquil C1-3 -amino carbonilo, que en cada caso están sustituidos en el átomo de nitrógeno adicionalmente con un grupo carboxi-alquilo C1-3, o con un grupo carboxi, representa un grupo alquilo C2-5 sustituido en posición terminal con un grupo di-(alquil C1-3 )-amino, o un grupo cicloalquilo C3-7, sus tautómeros, sus estereoisómeros y sus sales.
CO99048371A 1998-08-01 1999-07-30 Heterociclos biciclicos disustituidos, su preparacion y su empleo como medicamentos CO5080792A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE19834751A DE19834751A1 (de) 1998-08-01 1998-08-01 Disubstituierte bicyclische Heterocyclen, ihre Herstellung und ihre Verwendung als Arzneimittel

Publications (1)

Publication Number Publication Date
CO5080792A1 true CO5080792A1 (es) 2001-09-25

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ID=7876118

Family Applications (1)

Application Number Title Priority Date Filing Date
CO99048371A CO5080792A1 (es) 1998-08-01 1999-07-30 Heterociclos biciclicos disustituidos, su preparacion y su empleo como medicamentos

Country Status (13)

Country Link
US (1) US6121308A (es)
EP (1) EP1100795B1 (es)
JP (1) JP2002522432A (es)
AR (1) AR019976A1 (es)
AT (1) ATE268763T1 (es)
AU (1) AU5288599A (es)
CA (1) CA2337825C (es)
CO (1) CO5080792A1 (es)
DE (2) DE19834751A1 (es)
DK (1) DK1100795T3 (es)
ES (1) ES2223177T3 (es)
PT (1) PT1100795E (es)
WO (1) WO2000008014A1 (es)

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* Cited by examiner, † Cited by third party
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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.
DE19945810A1 (de) * 1999-09-24 2001-03-29 Boehringer Ingelheim Pharma Substituierte Benzimidazolderivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
US6413990B1 (en) 1999-09-24 2002-07-02 Boehringer Ingelheim Pharma Kg Arylsulphonamide-substituted benzimidazoles having tryptase-inhibiting activity
DE19945787A1 (de) 1999-09-24 2001-03-29 Boehringer Ingelheim Pharma Arylsulfonamid-substituierte Benzimidazolderivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
AU7288900A (en) * 1999-09-24 2001-04-30 Boehringer Ingelheim Pharma Kg Aryl sulfonamide-substituted benzimidazol derivatives thereof as tryptase inhibitors
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
EP1681287A1 (en) 2000-07-04 2006-07-19 Ube Industries, Ltd. Benzoxazole compounds, process for producing the same, and herbicides
DE10125478A1 (de) * 2001-05-25 2002-11-28 Boehringer Ingelheim Pharma Verwendung bicyclischer Heterocyclen zur Behandlung und Vorbeugung arterieller thrombotischer Erkrankungen
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GB0907551D0 (en) * 2009-05-01 2009-06-10 Univ Dundee Treatment or prophylaxis of proliferative conditions
CN111108105B (zh) 2017-09-22 2023-03-31 朱比兰特埃皮帕德有限公司 作为pad抑制剂的杂环化合物
BR112020007607A2 (pt) 2017-10-18 2020-09-29 Jubilant Epipad LLC compostos das fórmulas (i), (ii) e (iii); processos de preparação de compostos das fórmulas (i), (ii) e (iii); composição farmacêutica; compostos; método para a inibição de uma ou mais famílias de pad em uma célula; método de tratamento de uma afecção mediada por uma ou mais pad; composto da fórmula (i), fórmula (ii) e fórmula (iii); uso do composto; método para o tratamento e/ou prevenção de uma afecção; método para o tratamento de artrite reumatoide; e método de tratamento de câncer
JP7279057B6 (ja) 2017-11-06 2024-02-15 ジュビラント プローデル エルエルシー Ｐｄ１／ｐｄ－ｌ１活性化の阻害剤としてのピリミジン誘導体
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Also Published As

Publication number Publication date
AU5288599A (en) 2000-02-28
EP1100795B1 (de) 2004-06-09
DE19834751A1 (de) 2000-02-03
DE59909697D1 (de) 2004-07-15
JP2002522432A (ja) 2002-07-23
ES2223177T3 (es) 2005-02-16
WO2000008014A8 (de) 2000-03-16
PT1100795E (pt) 2004-10-29
ATE268763T1 (de) 2004-06-15
CA2337825C (en) 2008-09-23
WO2000008014A1 (de) 2000-02-17
US6121308A (en) 2000-09-19
EP1100795A1 (de) 2001-05-23
AR019976A1 (es) 2002-03-27
DK1100795T3 (da) 2004-10-18
CA2337825A1 (en) 2000-02-17

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