CO5261504A1 - NEW DERIVATIVES OF CARBOXILIC ACIDS, WHICH CARRY SIDE CHAINS, THEIR PREPARATION AND USE AS ANTAGONISTS OF ENDOTHELINE RECEPTORS - Google Patents

NEW DERIVATIVES OF CARBOXILIC ACIDS, WHICH CARRY SIDE CHAINS, THEIR PREPARATION AND USE AS ANTAGONISTS OF ENDOTHELINE RECEPTORS

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Publication number
CO5261504A1
CO5261504A1 CO99050715A CO99050715A CO5261504A1 CO 5261504 A1 CO5261504 A1 CO 5261504A1 CO 99050715 A CO99050715 A CO 99050715A CO 99050715 A CO99050715 A CO 99050715A CO 5261504 A1 CO5261504 A1 CO 5261504A1
Authority
CO
Colombia
Prior art keywords
alkyl
phenyl
optionally substituted
alkynyl
alkenyl
Prior art date
Application number
CO99050715A
Other languages
Spanish (es)
Inventor
Wilhelm Amberg
Rolf Jansen
Georg Kettschau
Stefan Herms
Raschack Manfred
Unger Unger
Original Assignee
Basf Ag
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 Basf Ag filed Critical Basf Ag
Publication of CO5261504A1 publication Critical patent/CO5261504A1/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/34One oxygen atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52Two oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)

Abstract

Derivados de ácidos carboxílicos de la fórmula (I):<EMI FILE="99050715_1" ID="1" IMF=JPEG >en donde los sustituyentes tienen el siguiente significado:R1 significa un grupo: <EMI FILE="99050715_2" ID="2" IMF=JPEG >Ra) un resto OR9, en donde R9 significa:- hidrógeno, el catión de un metal alcalino, el catión de un metal alcalinotérreo o un ion amonio orgánico fisiológicamente tolerable;- cicloalquilo- C3-C8, alquilo C1-C8, alquenilo-C3-C6, alquinilo-C3-C6, CH2-fenilo o fenilo eventualmente sustituidos.b) un compuesto heteroaromático de 5 miembros, ligado a través de un átomo de nitrógeno, c) un grupo: <EMI FILE="99050715_3" ID="3" IMF=JPEG >En el cual k puede tomar los valores 0, 1 y 2, p los valores 1, 2, 3 y 4 y R10 representa:- alquilo C1-C4, cicloalquilo C3-C8, alquenilo C3-C6, alquinilo C3-C6 o fenilo eventualmente sustituido - 2 -d) un resto: <EMI FILE="99050715_4" ID="4" IMF=JPEG >En donde R11 significa:- alquilo-C1-C4, alquenilo-C3-C6, alquinilo-C3-C6, cicloalquilo-C3-C8, pudiendo estos restos llevar un resto alcoxi C1-C4, alquiltio C1-C4 y/o fenilo, fenilo eventualmente sustituido.R2 significa hidrógeno, hidroxi, NH2, NH(alquilo-C1-C4), N(alquilo-C1-C4)2, halógeno, alquilo-C1-C4, alquenilo-C2,C4, alquinilo-C2-C4, halógeno-alquilo-C1-C4, alcoxi-C1-C4, halógenoalcoxi-C1-C4 o alquiltio-C1-C4, o CR2 está unido con CR12 como se indica más abajo como un anillo de 5 o 6 miembros, X significa nitrógeno o metino;Y significa nitrógeno o metino;Z significa nitrógeno o CR12, en donde R12 significa hidrógeno o alquilo-C1-C4, o CR12 junto con CR2 o CR3 forma un anillo alquileno o alquenileno de 5 o 6 miembros, el cual puede estar eventualmente sustituido y en donde en cada caso uno o más grupos metileno pueden estar reemplazados por oxígeno, azufre, NH o -N(alquilo-C1-C4), R3 significa hidrógeno, hidroxi, NH2, NH(alquilo-C1-C4), N(alquilo-C1-C4)2, halógeno, alquilo-C1-C4, alquenilo-C2-C4, alquinilo-C2-C4, halógenoalquilo-C1-C4, alcoxi-C1-C4, halógenoalcoxi-C1-C4, alquiltio-C1-C4, o CR3 está unido con CR12 como se indica más arriba como un anillo de 5 o 6 miembros; R4 y R5 (que pueden ser iguales o diferentes) significan:- fenilo o naftilo, eventualmente sustituídos;- fenilo o naftilo, que pueden estar unidos entre sí en posición orto a través de una ligadura directa, un grupo metileno, etileno o etinileno, un átomo de oxígeno o azufre o un grupo SO2, o N-alquilo; - cicloalquilo C3-C8 eventualmente sustituído,R6 significa cicloalquilo C3-C8 eventualmente sustituído;- fenilo o naftilo, eventualmente sustituídosun compuesto heteroaromático de cinco o seis miembros que contiene uno a tres átomos de nitrógeno y/o un átomo de azufre u oxígeno, el cual puede estar eventualmente sustituido;R7 y R8 (que pueden ser iguales o diferentes): - significan hidrógeno o alquilo-C1-C4,W significa azufre u oxígeno.Carboxylic acid derivatives of the formula (I): <EMI FILE = "99050715_1" ID = "1" MFI = JPEG> where the substituents have the following meaning: R1 means a group: <EMI FILE = "99050715_2" ID = "2" IMF = JPEG> Ra) an OR9 moiety, wherein R9 means: - hydrogen, the cation of an alkali metal, the cation of an alkaline earth metal or a physiologically tolerable organic ammonium ion; - cycloalkyl- C3-C8, alkyl C1-C8, C3-C6 alkenyl, C3-C6 alkynyl, CH2-phenyl or optionally substituted phenyl. B) a 5-membered heteroaromatic compound, bound through a nitrogen atom, c) a group: <EMI FILE = "99050715_3" ID = "3" MFI = JPEG> In which k can take values 0, 1 and 2, p values 1, 2, 3 and 4 and R10 represents: - C1-C4 alkyl, C3 cycloalkyl- C8, C3-C6 alkenyl, C3-C6 alkynyl or optionally substituted phenyl - 2 -d) a moiety: <EMI FILE = "99050715_4" ID = "4" MFI = JPEG> Where R11 means: - C1-C4 alkyl , C3-C6 alkenyl, C3-C6 alkynyl, cycloalkyl -C3-C8, these moieties being able to carry a C1-C4 alkoxy, C1-C4 alkylthio and / or phenyl moiety, optionally substituted phenyl.R2 means hydrogen, hydroxy, NH2, NH (C1-C4 alkyl), N (alkyl- C1-C4) 2, halogen, C1-C4 alkyl, alkenyl-C2, C4, alkynyl-C2-C4, halogen-C1-C4 alkyl, alkoxy-C1-C4, halogenoalkoxy-C1-C4 or alkylthio-C1- C4, or CR2 is linked to CR12 as indicated below as a 5 or 6 membered ring, X means nitrogen or methine; Y means nitrogen or methine; Z means nitrogen or CR12, where R12 means hydrogen or C1-alkyl C4, or CR12 together with CR2 or CR3 forms a 5 or 6 membered alkylene or alkenylene ring, which may eventually be substituted and where in each case one or more methylene groups may be replaced by oxygen, sulfur, NH or -N (C1-C4 alkyl), R3 means hydrogen, hydroxy, NH2, NH (C1-C4 alkyl), N (C1-C4 alkyl) 2, halogen, C1-C4 alkyl, C2-C4 alkenyl, alkynyl -C2-C4, halogen-C1-C4 alkyl, C1-C4 alkoxy, h halogenoalkoxy-C1-C4, alkylthio-C1-C4, or CR3 is linked to CR12 as indicated above as a 5 or 6 membered ring; R4 and R5 (which may be the same or different) mean: - phenyl or naphthyl, optionally substituted; - phenyl or naphthyl, which may be linked to each other in an ortho position through a direct ligation, a methylene, ethylene or ethynylene group, an oxygen or sulfur atom or an SO2 group, or N-alkyl; - C3-C8 cycloalkyl optionally substituted, R6 means C3-C8 cycloalkyl optionally substituted; - phenyl or naphthyl, optionally substituted a five or six membered heteroaromatic compound containing one to three nitrogen atoms and / or one sulfur or oxygen atom, which may eventually be substituted; R7 and R8 (which may be the same or different): - mean hydrogen or C1-C4 alkyl, W means sulfur or oxygen.

CO99050715A 1998-08-10 1999-08-10 NEW DERIVATIVES OF CARBOXILIC ACIDS, WHICH CARRY SIDE CHAINS, THEIR PREPARATION AND USE AS ANTAGONISTS OF ENDOTHELINE RECEPTORS CO5261504A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE19836044A DE19836044A1 (en) 1998-08-10 1998-08-10 New 2-(hetero)aryl-alkanoic acid derivatives, useful as mixed endothelin receptor antagonists, e.g. for treating cardiac insufficiency, restenosis, hypertension or prostate cancer

Publications (1)

Publication Number Publication Date
CO5261504A1 true CO5261504A1 (en) 2003-03-31

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ID=7876981

Family Applications (1)

Application Number Title Priority Date Filing Date
CO99050715A CO5261504A1 (en) 1998-08-10 1999-08-10 NEW DERIVATIVES OF CARBOXILIC ACIDS, WHICH CARRY SIDE CHAINS, THEIR PREPARATION AND USE AS ANTAGONISTS OF ENDOTHELINE RECEPTORS

Country Status (22)

Country Link
EP (1) EP1104410A1 (en)
JP (1) JP2002522531A (en)
KR (1) KR20010072378A (en)
CN (1) CN1323298A (en)
AR (1) AR020147A1 (en)
AU (1) AU5374199A (en)
BG (1) BG105236A (en)
BR (1) BR9912889A (en)
CA (1) CA2340167A1 (en)
CO (1) CO5261504A1 (en)
DE (1) DE19836044A1 (en)
HK (1) HK1042086A1 (en)
HR (1) HRP20010164A2 (en)
HU (1) HUP0104007A3 (en)
ID (1) ID27965A (en)
IL (1) IL140915A0 (en)
NO (1) NO20010622D0 (en)
PL (1) PL345998A1 (en)
SK (1) SK832001A3 (en)
TR (1) TR200100427T2 (en)
WO (1) WO2000009489A1 (en)
ZA (1) ZA200101975B (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19924892A1 (en) * 1999-06-01 2000-12-07 Basf Ag New carboxylic acid derivatives with aryl-substituted nitrogen heterocycles, their production and use as endothelin receptor antagonists

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19636046A1 (en) * 1996-09-05 1998-03-12 Basf Ag New carboxylic acid derivatives, their production and use as mixed ET¶A¶ / ET¶B¶ receptor antagonists

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Publication number Publication date
DE19836044A1 (en) 2000-02-17
PL345998A1 (en) 2002-01-14
NO20010622L (en) 2001-02-06
WO2000009489A1 (en) 2000-02-24
HUP0104007A3 (en) 2002-12-28
NO20010622D0 (en) 2001-02-06
IL140915A0 (en) 2002-02-10
TR200100427T2 (en) 2001-07-23
EP1104410A1 (en) 2001-06-06
AU5374199A (en) 2000-03-06
CA2340167A1 (en) 2000-02-24
SK832001A3 (en) 2001-11-06
HUP0104007A2 (en) 2002-05-29
AR020147A1 (en) 2002-04-10
CN1323298A (en) 2001-11-21
BG105236A (en) 2001-12-29
KR20010072378A (en) 2001-07-31
JP2002522531A (en) 2002-07-23
HRP20010164A2 (en) 2002-04-30
ID27965A (en) 2001-05-03
ZA200101975B (en) 2002-03-11
HK1042086A1 (en) 2002-08-02
BR9912889A (en) 2001-05-08

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