AR010909A1 - SUBSTITUTED DERIVATIVES OF 8- (AZA OR OXA OR TIA) -3-AZA-CICLOPENTA [A] INDEN AS ANTAGONISTS OF THE ENDOTHELIAL RECEPTOR, PROCEDURE TO PREPARE THEM, PROCEDURE FOR OBTAINING PHARMACEUTICAL COMPOSITIONS, AND COMPOSITIONS FROM THE DERIVATIVES, MEDICINES . - Google Patents

SUBSTITUTED DERIVATIVES OF 8- (AZA OR OXA OR TIA) -3-AZA-CICLOPENTA [A] INDEN AS ANTAGONISTS OF THE ENDOTHELIAL RECEPTOR, PROCEDURE TO PREPARE THEM, PROCEDURE FOR OBTAINING PHARMACEUTICAL COMPOSITIONS, AND COMPOSITIONS FROM THE DERIVATIVES, MEDICINES .

Info

Publication number
AR010909A1
AR010909A1 ARP980101274A ARP980101274A AR010909A1 AR 010909 A1 AR010909 A1 AR 010909A1 AR P980101274 A ARP980101274 A AR P980101274A AR P980101274 A ARP980101274 A AR P980101274A AR 010909 A1 AR010909 A1 AR 010909A1
Authority
AR
Argentina
Prior art keywords
aza
phenyl
procedure
derivatives
alkylene
Prior art date
Application number
ARP980101274A
Other languages
Spanish (es)
Original Assignee
Merck Patent Gmbh
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 Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR010909A1 publication Critical patent/AR010909A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Derivados sustituidos de 8-(aza u oxa o tia)-3-aza-ciclopenta[a]inden como antagonistas del receptor endotelial de la formula I, en donde X representaN-R3, O o S,R representa 2,1,3-benzotiadiazol-4- o 5-ilo o 2,1-benzo-isotia-zol-5- o -6-ilo no sustituido o mono o disustituido con R2 y/o R2, o fenilo nosustituido o mono, di o trisustituido con R2 y/o R2,R1 representa H o A,R2,R2 representan independientemente H,A,OH,OA,Hal,OCF3,OCHF2,-O-CO-A,-O-alquilen-COOR1, -O-alquilen-CH2-OR1, o OCH2-feniloo -O-CO-fenilo no sustituido o mono o disustituido en el fenilo con R4 y/o R4,R2 y R2, juntos, también reprsentan-OCH2O-,-OCH2CH2O- o -OCH2CH2-, R3 representa H,A,alquilen-O-A, -CO-OA o alquilen-fenilo no sustituido o mono o disustituido en elfenilo con R4 y/oR4,R4,R4 representan independientemente H,A,OH,OA,Hal,COOR1 o CH2OR1, A representa alquilo de 1 a 6 átomos de C, Hal representa fluor, cloro, bromo oyodo, y sus sales. Estos compuestos poseen propiedades antagonistas del receptor endotelial y son utiles para combatir la hipertonía, la insuficiencia cardiaca,la insuficiencia renal, el infarto cerebral, la enfermedad coronaria, la isquemia renal, cerebral y de miocardio, la hemorragia subaracnoidal, lasinflamaciones,el asma y el shock endotoxico. Un procedimiento para preparar dichos compuestos, un procedimiento para obtener composiciones farmaceuticas abase de los derivados, medicamentos y composiciones farmaceuticas que los contienen.Substituted derivatives of 8- (aza or oxa or thia) -3-aza-cyclopenta [a] inden as endothelial receptor antagonists of formula I, where X represents N-R3, O or S, R represents 2,1,3 -benzothiadiazol-4- or 5-yl or 2,1-benzo-isothia-zol-5- or -6-yl unsubstituted or mono or disubstituted with R2 and / or R2, or unsubstituted or mono, di or trisubstituted phenyl with R2 and / or R2, R1 represents H or A, R2, R2 independently represent H, A, OH, OA, Hal, OCF3, OCHF2, -O-CO-A, -O-alkylene-COOR1, -O-alkylene- CH2-OR1, or OCH2-phenyl or -O-CO-phenyl unsubstituted or mono or disubstituted in phenyl with R4 and / or R4, R2 and R2, together, also represent-OCH2O -, - OCH2CH2O- or -OCH2CH2-, R3 represents H, A, alkylene-OA, -CO-OA or alkylene-phenyl unsubstituted or mono or disubstituted in phenyl with R4 and / or R4, R4, R4 independently represent H, A, OH, OA, Hal, COOR1 or CH2OR1 , A represents alkyl of 1 to 6 C atoms, Hal represents fluorine, chlorine, bromine, and its salts. These compounds possess endothelial receptor antagonistic properties and are useful in combating hypertonia, heart failure, kidney failure, stroke, coronary heart disease, renal, cerebral and myocardial ischemia, subarachnoid hemorrhage, inflammation, asthma, and endotoxic shock. A method for preparing said compounds, a method for obtaining pharmaceutical compositions based on derivatives, medications and pharmaceutical compositions containing them.

ARP980101274A 1997-03-21 1998-03-20 SUBSTITUTED DERIVATIVES OF 8- (AZA OR OXA OR TIA) -3-AZA-CICLOPENTA [A] INDEN AS ANTAGONISTS OF THE ENDOTHELIAL RECEPTOR, PROCEDURE TO PREPARE THEM, PROCEDURE FOR OBTAINING PHARMACEUTICAL COMPOSITIONS, AND COMPOSITIONS FROM THE DERIVATIVES, MEDICINES . AR010909A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE19711785A DE19711785A1 (en) 1997-03-21 1997-03-21 Endothelin receptor antagonists

Publications (1)

Publication Number Publication Date
AR010909A1 true AR010909A1 (en) 2000-07-12

Family

ID=7824108

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP980101274A AR010909A1 (en) 1997-03-21 1998-03-20 SUBSTITUTED DERIVATIVES OF 8- (AZA OR OXA OR TIA) -3-AZA-CICLOPENTA [A] INDEN AS ANTAGONISTS OF THE ENDOTHELIAL RECEPTOR, PROCEDURE TO PREPARE THEM, PROCEDURE FOR OBTAINING PHARMACEUTICAL COMPOSITIONS, AND COMPOSITIONS FROM THE DERIVATIVES, MEDICINES .

Country Status (5)

Country Link
AR (1) AR010909A1 (en)
AU (1) AU6826598A (en)
DE (1) DE19711785A1 (en)
WO (1) WO1998042709A1 (en)
ZA (1) ZA982359B (en)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10155076A1 (en) * 2001-11-09 2003-05-22 Merck Patent Gmbh Use of endothelin receptor antagonists for the treatment of tumor diseases
ES2566479T3 (en) 2006-01-06 2016-04-13 Sunovion Pharmaceuticals Inc. Monoamine reabsorption inhibitors based on tetralone
US20070203111A1 (en) 2006-01-06 2007-08-30 Sepracor Inc. Cycloalkylamines as monoamine reuptake inhibitors
EP2816024B8 (en) 2006-03-31 2018-04-04 Sunovion Pharmaceuticals Inc. Chiral amines
US7884124B2 (en) 2006-06-30 2011-02-08 Sepracor Inc. Fluoro-substituted inhibitors of D-amino acid oxidase
US7902252B2 (en) 2007-01-18 2011-03-08 Sepracor, Inc. Inhibitors of D-amino acid oxidase
JP5420534B2 (en) 2007-05-31 2014-02-19 サノビオン ファーマシューティカルズ インク Phenyl-substituted cycloalkylamines as monoamine reuptake inhibitors

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH10510510A (en) * 1994-06-09 1998-10-13 スミスクライン・ビーチャム・コーポレイション Endothelin receptor antagonist

Also Published As

Publication number Publication date
WO1998042709A1 (en) 1998-10-01
DE19711785A1 (en) 1998-09-24
ZA982359B (en) 1998-09-22
AU6826598A (en) 1998-10-20

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