公开(公告)号：CZ37396A3

公开(公告)日：1996-05-15

申请号：CZ37396

申请日：1994-08-12

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： VAN LOMMEN GUY ROSALIA EUGENE ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  ANDRES-GIL JOSE IGNACIO ,  MATESANZ-BALLESTEROS MARIA E E

IPC: A61K31/35 ,  A61K31/436 ,  A61K31/44 ,  A61K31/453 ,  A61K31/505 ,  A61P9/02 ,  A61P9/08 ,  A61P25/04 ,  A61P25/06 ,  C07D405/12 ,  C07D491/04 ,  C07D491/052

Abstract: PCT No. PCT/EP94/02700 Sec. 371 Date Jan. 24, 1996 Sec. 102(e) Date Jan. 24, 1996 PCT Filed Aug. 12, 1994 PCT Pub. No. WO95/05381 PCT Pub. Date Feb. 23, 1995The present invention is concerned with compounds of formula (I) the pharmaceutically acceptable acid addition salts thereof, the +E,uns N+EE -oxides thereof and the stereochemically isomeric forms thereof, wherein =a1-a2=a3-a4= is a bivalent radical of formula:=N-CH=CH-CH=(a),=CH-N=CH-CH=(b),=CH-CH=N-CH=(c),=CH-CH=CH-N=(d),wherein in said bivalent radicals one or two hydrogen atoms can be substituted by halo, hydroxy, C1-6alkyl or C1-6alkyloxy; R1 is hydrogen or C1-6alkyl; R2 is hydrogen or C1-6alkyl; R3 is hydrogen or C1-6alkyl; Alk1 is C1-5alkanediyl; Alk2 is C2-15alkanediyl; Q is a five- or six-membered heterocyclic ring containing at least one nitrogen atom or a radical of formula (aa) wherein R4 is hydrogen, cyano, aminocarbonyl or C1-6alkyl; R5 is hydrogen, C1-6alkyl, C3-6alkenyl or C3-6alkynyl; R6 is hydrogen or C1-6alkyl; or R5 and R6 taken together may form a bivalent radical of formula -(CH2)4- or -(CH2)5-. Pharmaceutical compositions, preparations and use as a medicine are described.

公开(公告)号：CZ9600373A3

公开(公告)日：1996-05-15

申请号：CZ37396

申请日：1994-08-12

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： VAN LOMMEN GUY ROSALIA EUGENE ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  ANDRES-GIL JOSE IGNACIO ,  MATESANZ-BALLESTEROS MARIA E E

IPC: A61K31/35 ,  A61K31/436 ,  A61K31/44 ,  A61K31/453 ,  A61K31/505 ,  A61P9/02 ,  A61P9/08 ,  A61P25/04 ,  A61P25/06 ,  C07D405/12 ,  C07D491/04 ,  C07D491/052

CPC classification number: C07D491/04

公开(公告)号：CZ286645B6

公开(公告)日：2000-05-17

申请号：CZ37396

申请日：1994-08-12

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： VAN LOMMEN GUY ROSALIA EUGENE ,  FERNANDEZ-GADEA FRANCISCO JAVI ,  ANDR S-GIL JOS IGNACIO ,  MATESANZ-BALLESTEROS MARIA E E

IPC: A61K31/35 ,  A61K31/436 ,  A61K31/44 ,  A61K31/453 ,  A61K31/505 ,  A61P9/02 ,  A61P9/08 ,  A61P25/04 ,  A61P25/06 ,  C07D405/12 ,  C07D491/04 ,  C07D491/052

Abstract: In the present invention there are disclosed substituted dihydropyranopyridines of the general formula I, in which =ai1-ai2=ai3-ai4= represents a bivalent radical =N-CH=CH-CH=, =CH-N=CH-CH=, =CH-CH=N-CH= or =CH-CH=CH-N=, whereby in those bivalent radicals can be optionally one or two hydrogen atoms substituted with a halogen, hydroxy, alkyl containing 1 to 6 carbon atoms or alkoxyl containing 1 to 6 carbon atoms Re1, Re2 and Re3 represent each independently on each other hydrogen or alkyl containing 1 to 6 carbon atoms, Alke1 represents alkanediyl containing 1 to 5 carbon atoms, Alke2 represents alkanediyl containing 2 to 15 carbon atoms, Q represents a five- or six-membered heterocyclic radical containing at least one nitrogen atom or the radical aa, wherein Re4 represents hydrogen, cyano, aminocarbonyl or alkyl containing 1 to 6 carbon atoms, Re5 represents hydrogen, alkyl containing 1 to 6 carbon atoms alkenyl containing 3 to 6 carbon atoms or alkynyl containing 3 to 6 carbon atoms, Re6 represents hydrogen or alkyl containing 1 to 6 carbon atoms or Re5 and Re6 together form a bivalent radical of the general formula -(CHi2)i4- or -(CHi2)i5-, and their pharmaceutically acceptable acid addition salts, N-oxides and stereochemically isomeric forms per se and for use in medicine. In the present invention there are also claimed a process for preparing those compounds and pharmaceutical preparations based thereon. The above indicated derivatives are suitable for prevention and/or therapy of disorders characterized by excessive vasodilatation, particularly migraine.

公开(公告)号：SK19496A3

公开(公告)日：1997-02-05

申请号：SK19496

申请日：1994-08-12

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： VAN LOMMEN GUY R E ,  FERNANDEZ-GADEA F J ,  ANDRES-GIL JOSE I ,  MATESANZ-BALLESTEROS MARIA E E

IPC: A61K31/35 ,  A61K31/436 ,  A61K31/44 ,  A61K31/453 ,  A61K31/505 ,  A61P9/02 ,  A61P9/08 ,  A61P25/04 ,  A61P25/06 ,  C07D405/12 ,  C07D491/04 ,  C07D491/052

Abstract: Substituted dihydropyranopyridines of general formula (I), wherein =a1-a2=a3-a4= is a bivalent radical of formula: =N-CH=CH-CH=; =CH-N=CH-CH=; =CH-CH=N-CH=; or =CH-CH=CH-N=, wherein in said bivalent radicals one or two hydrogen atoms can be substituted by halogen, hydroxy, C1-6 alkyl or C1-6 alkyloxy; Alk1 is C1-5 alkanediyl; Alk2 is C2-15 alkanediyl; Q is a five- or six-membered heterocyclic ring containing at least one nitrogen atom or a radical of formula (aa), wherein R4 is hydrogen, cyano, aminocarbonyl or C1-6 alkyl; R5 is hydrogen, C1-6 alkyl, C3-6 alkenyl or C3-6 alkynyl; R6 is hydrogen or C1-6 alkyl; R5 and R6 taken together may form a bivalent radical of formula -(CH2)4- or -(CH2)5- and their pharmaceutically suitable additive salts with acids, N-oxides and stereochemically isomeric forms thereof for their use in medicine. Disclosed is also method and intermediates for their preparation and pharmaceutical preparation based on them. Derivatives are suitable for prevention and/or treatment of defects characterised by excessive vasodilatation, particularly migraine.