UY25941A1 - PROCEDURE FOR PREPARING DERIVATIVES OF 7H-PIRROLO (2,3-D) PIRIMIDINA. - Google Patents

PROCEDURE FOR PREPARING DERIVATIVES OF 7H-PIRROLO (2,3-D) PIRIMIDINA.

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Publication number
UY25941A1
UY25941A1 UY25941A UY25941A UY25941A1 UY 25941 A1 UY25941 A1 UY 25941A1 UY 25941 A UY25941 A UY 25941A UY 25941 A UY25941 A UY 25941A UY 25941 A1 UY25941 A1 UY 25941A1
Authority
UY
Uruguay
Prior art keywords
carbamoyl
lower alkyl
substituted
derivatives
dialkyl
Prior art date
Application number
UY25941A
Other languages
Spanish (es)
Inventor
Peter Traxler
Guido Bold
Wolfgang Karl-Diether Brill
Joerg Frei
Original Assignee
Novartis 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 Novartis Ag filed Critical Novartis Ag
Publication of UY25941A1 publication Critical patent/UY25941A1/en

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  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Derivados de 7H-[2,3-d]pirimidina de fórmula (I), en donde: q es 0 o 1; n es de 1 a 3 cuando q es 0, ó n es de 0 a 3 cuando q es 1; R es halógeno, alquilo inferior, hidroxi, alcanoiloxi inferior, alcoxi inferior, carboxi, alcoxi inferior-carbonilo, carbamoílo, N-alquilo inferior-carbamoílo, N,N-dialquilo inferior-carbamoílo, ciano, amino, alcanoílo inferior-amino, alquilo inferior-amino, N,N-dialquilo inferior-amino o trifluorometilo, siendo posible que cuando varios radicales R están presentes en la molécula, dichos radicales sean idénticos o diferentes; (a) R1 y R2 son ambos independientes uno del otro pudiendo ser fenilo sustituido, hidrógeno, piridilo sustituido o no; N-bencil-piridinio-2-ilo, naftilo, ciano, carboxi, alcoxi inferior-carbonilo, carbamoílo, N-alquilo inferior-carbamoílo, N,N-dialquilo inferior-carbamoílo, N-bencil-carbamoílo, formilo, alcanoílo inferior, alquenilo inferior, alqueniloxi inferior, o alquilo inferior sustituido; (b) cuando q es 0, uno de los radicales R1 y R2 es alquilo inferior no sustituido o fenilo no sustituido y el otro de los radicales R1 y R2 tiene uno de los significados que se dan anteriormente en el párrafo (a) con la excepción de hidrógeno; (c) R1 y R2 juntos son C4-C10-1,4-alcadienileno sustituido, ó (d) cuando q es 1, R1 y R2 son independientemente del otro alquilo inferior no sustituido o fenilo no sustituido o tienen uno de los significados que se dan anteriormente en el párrafo (a); y R6 es hidrógeno, alquilo inferior, alcoxi inferior-carbonilo, carbamoílo, N-alquilo inferior-carbamoílo ó N,N-dialquilo inferior-carbamoílo o una sal de los mismos, con la excepción del compuesto de fórmula (I) en el que n es 0, q es 1, R1 y R6 son los dos hidrógeno y R2 es metilo. Por ejemplo: 4-(3-cloro-anilino)-6-(pirid-2-il)-7H-pirrolo(2,3-d)pirimidina. La invención se refiere a procedimientos para preparar dichos derivados y a los procedimientos y compuestos intermedios nuevos para la preparación de las mismas, formulaciones farmacéuticas que comprenden tales derivados y al uso de tales derivados para quimioterapia de tumores.Derivatives of 7H- [2,3-d] pyrimidine of formula (I), wherein: q is 0 or 1; n is from 1 to 3 when q is 0, or n is from 0 to 3 when q is 1; R is halogen, lower alkyl, hydroxy, lower alkanoyloxy, lower alkoxy, carboxy, lower alkoxy-carbonyl, carbamoyl, N-lower alkyl-carbamoyl, N, N-dialkyl-lower carbamoyl, cyano, amino, lower alkanoyl-amino, alkyl lower-amino, N, N-lower dialkyl-amino or trifluoromethyl, it being possible that when several R radicals are present in the molecule, said radicals are identical or different; (a) R1 and R2 are both independent of each other and may be substituted phenyl, hydrogen, substituted or not substituted pyridyl; N-benzyl-pyridinium-2-yl, naphthyl, cyano, carboxy, lower alkoxy-carbonyl, carbamoyl, N-lower alkyl-carbamoyl, N, N-dialkyl-carbamoyl, N-benzyl-carbamoyl, formyl, lower alkanoyl, lower alkenyl, lower alkenyloxy, or substituted lower alkyl; (b) when q is 0, one of the radicals R1 and R2 is unsubstituted lower alkyl or unsubstituted phenyl and the other of the radicals R1 and R2 has one of the meanings given in paragraph (a) above with the hydrogen exception; (c) R1 and R2 together are C4-C10-1,4-substituted alkadienylene, or (d) when q is 1, R1 and R2 are independently of the other unsubstituted lower alkyl or unsubstituted phenyl or have one of the meanings that given above in paragraph (a); and R6 is hydrogen, lower alkyl, lower alkoxy-carbonyl, carbamoyl, N-lower alkyl-carbamoyl or N, N-dialkyl lower-carbamoyl or a salt thereof, with the exception of the compound of formula (I) in which n is 0, q is 1, R1 and R6 are both hydrogen and R2 is methyl. For example: 4- (3-chloro-anilino) -6- (pyrid-2-yl) -7H-pyrrolo (2,3-d) pyrimidine. The invention relates to procedures for preparing such derivatives and to novel methods and intermediates for the preparation thereof, pharmaceutical formulations comprising such derivatives and to the use of such derivatives for tumor chemotherapy.

UY25941A 1995-07-06 2000-01-17 PROCEDURE FOR PREPARING DERIVATIVES OF 7H-PIRROLO (2,3-D) PIRIMIDINA. UY25941A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CH197695 1995-07-06

Publications (1)

Publication Number Publication Date
UY25941A1 true UY25941A1 (en) 2000-09-29

Family

ID=4223021

Family Applications (1)

Application Number Title Priority Date Filing Date
UY25941A UY25941A1 (en) 1995-07-06 2000-01-17 PROCEDURE FOR PREPARING DERIVATIVES OF 7H-PIRROLO (2,3-D) PIRIMIDINA.

Country Status (3)

Country Link
TW (1) TW472057B (en)
UY (1) UY25941A1 (en)
ZA (1) ZA965723B (en)

Also Published As

Publication number Publication date
TW472057B (en) 2002-01-11
ZA965723B (en) 1997-01-06

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Effective date: 20200117