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61. 发明专利

AT256125T 未知
公开(公告)号：AT256125T
公开(公告)日：2003-12-15
申请号：AT00940267
申请日：2000-05-23
申请人： JANSSEN PHARMACEUTICA NV
发明人： VAN EMELEN KRISTOF , DE BRUYN MARCEL FRANS
IPC分类号： A61K31/4164 , A61K31/4178 , A61K31/513 , A61P1/14 , A61P9/00 , A61P9/08 , C07D405/12 , C07D417/12
摘要： The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z 1 -Z 2 - is a bivalent radical; R 1 , R 2 and R 3 are each independently selected from hydrogen, C 1-6 alkyl, hydroxy, halo and the like; or when R 1 and R 2 are on adjacent carbon atoms, R 1 and R 2 taken together may form a bivalent radical of formula; Alk 1 and Alk 2 are optionally substituted C 1-6 alkanediyl; R 6 is hydrogen or phenylmethyl; R 5 is a radical of formula wherein n is 1 or 2; p 1 is 0, and p 2 is 1 or 2; or p 1 is 1 or 2, and p 2 is 0; X is oxygen, sulfur or -NR 9 ; Y is oxygen or sulfur; R 7 is hydrogen, C 1-6 alkyl, C 3-6 cycloalkyl, phenyl or phenylmethyl; R 8 is C 1-6 alkyl, C 3-6 cycloalkyl phenyl or phenylmethyl; R 9 is cyano, C 1-6 alkyl, C 3-6 cyclo-alkyl, C 1-6 alkyloxycarbonyl or aminocarbonyl; R 10 is hydrogen or C 1-6 alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impaired fundic relaxation.

64. 发明专利

PL352063A1 DERIVATIVES (OF BENZODIOXANE, BENZOPHURANE OR BENZOPYRANE) SUBSTITUTED BY PYROLYDINYLENE, PIPERYDINYLENE OR HOMOPIPERYDINYLENE 未知
公开(公告)号：PL352063A1
公开(公告)日：2003-07-28
申请号：PL35206300
申请日：2000-05-23
申请人： JANSSEN PHARMACEUTICA NV
发明人： DE BRUYN MARCEL FRANS LEOPOLD , VAN EMELEN KRISTOF , WIGERINCK PIET TOM BERT PAUL , VERSCHUEREN WIM GASTON
IPC分类号： A61K31/505 , A61K31/513 , A61P1/06 , A61P1/14 , A61P9/00 , C07D405/12 , C07D405/14
摘要： The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z 1 -Z 2 - is a bivalent radical; R 1 , R 2 and R 3 are each independently selected from hydrogen, C 1-6 alkyl, hydroxy, halo and the like; or when R 1 and R 2 are on adjacent carbon atoms, R 1 and R 2 taken together may form a bivalent radical of formula; Alk is optionally substituted C 1-6 alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R 5 is a radical of formula wherein n is 1 or 2; p 1 is 0, and p 2 is 1 or 2; or p 1 is 1 or 2, and p 2 is 0; X is oxygen, sulfur or -NR 9 ; Y is oxygen or sulfur; R 7 is hydrogen, C 1-6 alkyl, C 3-6 cycloalkyl, phenyl or phenylmethyl; R 8 is C 1-6 alkyl, C 3-6 cycloalkyl phenyl or phenylmethyl; R 9 is cyano, C 1-6 alkyl, C 3-6 cyclo-alkyl, C 1-6 alkyloxycarbonyl or aminocarbonyl; R 10 is hydrogen or C 1-6 alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impaired fundic relaxation.

65. 发明专利

SK492003A3 Compounds for treating impaired fundic relaxation 未知
公开(公告)号：SK492003A3
公开(公告)日：2003-07-01
申请号：SK492003
申请日：2001-06-13
申请人： JANSSEN PHARMACEUTICA NV
发明人： VAN EMELEN KRISTOF , DE BRUYN MARCEL FRANS LEOPOLD , ALCAZAR-VACA MANUEL JESUS , ANDRES-GIL JOSE IGNACIO , FERNANDEZ-GADEA FRANCISCO JAVI , MATESANZ-BALLESTEROS MARIA ENC , BARTOLOME-NEBREDA JOSE MANUEL
IPC分类号： C07D491/056 , A61K31/435 , A61K31/436 , A61K31/4545 , A61K31/513 , A61K31/5383 , A61P1/00 , A61P1/14 , C07D411/04 , C07D491/04 , C07D491/052 , C07D491/06 , C07D497/04 , C07D498/04
摘要： The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -a 1 -a 2 -a 3 -a 4 - is a bivalent radical wherein one or two of a 1 to a 4 are nitrogen and the remaining a 1 to a 4 are -CH-; -Z 1 -Z 2 - is a bivalent radical; -A- is a bivalent radical of formula -N(R 6 )-Alk 2 - or a 5, 6 or 7-membered saturated heterocycle containing one or two nitrogen atoms; R 1 , R 2 and R 3 are each independently selected from hydrogen, C 1-6 alkyl, hydroxy, halo and the like; Alk 1 and Alk 2 are optionally substituted C 1-6 alkanediyl; R 5 is a radical of formula wherein n is 1 or 2; p 1 is 0, and p 2 is 1 or 2; or p 1 is 1 or 2, and p 2 is 0; X is oxygen, sulfur or -NR 9 ; Y 2 is oxygen or sulfur; R 7 is hydrogen, C 1-6 alkyl, C 3-6 cycloalkyl, phenyl or phenylmethyl; R 8 is C 1-6 alkyl, C 3-6 cycloalkyl phenyl or phenylmethyl; R 9 is cyano, C 1-6 alkyl, C 3-6 cycloalkyl, C 1-6 alkyloxycarbonyl or aminocarbonyl; R 10 is hydrogen or C 1-6 alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to disturbed fundic accomodation.

66. 发明专利

CZ2003115A3 Compounds for treating disorder of eyeground detachment 未知
公开(公告)号：CZ2003115A3
公开(公告)日：2003-06-18
申请号：CZ2003115
申请日：2001-06-13
申请人： JANSSEN PHARMACEUTICA NV
发明人： VAN EMELEN KRISTOF , DE BRUYN MARCEL FRANS LEOPOLD , ALCAZAR-VACA MANUEL JESUS , ANDRES-GIL JOSE IGNACIO , FERNANDEZ-GADEA FRANCISCO JAVI , MATESANZ-BALLESTEROS MARIA ENC , BARTOLOME-NEBREDA JOSE MANUEL
IPC分类号： C07D491/056 , A61K31/435 , A61K31/436 , A61K31/4545 , A61K31/513 , A61K31/5383 , A61P1/00 , A61P1/14 , C07D411/04 , C07D491/04 , C07D491/052 , C07D491/06 , C07D497/04 , C07D498/04
摘要： The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -a 1 -a 2 -a 3 -a 4 - is a bivalent radical wherein one or two of a 1 to a 4 are nitrogen and the remaining a 1 to a 4 are -CH-; -Z 1 -Z 2 - is a bivalent radical; -A- is a bivalent radical of formula -N(R 6 )-Alk 2 - or a 5, 6 or 7-membered saturated heterocycle containing one or two nitrogen atoms; R 1 , R 2 and R 3 are each independently selected from hydrogen, C 1-6 alkyl, hydroxy, halo and the like; Alk 1 and Alk 2 are optionally substituted C 1-6 alkanediyl; R 5 is a radical of formula wherein n is 1 or 2; p 1 is 0, and p 2 is 1 or 2; or p 1 is 1 or 2, and p 2 is 0; X is oxygen, sulfur or -NR 9 ; Y 2 is oxygen or sulfur; R 7 is hydrogen, C 1-6 alkyl, C 3-6 cycloalkyl, phenyl or phenylmethyl; R 8 is C 1-6 alkyl, C 3-6 cycloalkyl phenyl or phenylmethyl; R 9 is cyano, C 1-6 alkyl, C 3-6 cycloalkyl, C 1-6 alkyloxycarbonyl or aminocarbonyl; R 10 is hydrogen or C 1-6 alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to disturbed fundic accomodation.

68. 发明专利

HU0201404A2 AMINOALKYL SUBSTITUTED BENZODIOXAN, BENZOFURAN OR BENZOPYRAN DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USE AND PROCESS FOR THEIR PREPARATIONS 未知
公开(公告)号：HU0201404A2
公开(公告)日：2002-08-28
申请号：HU0201404
申请日：2000-05-23
申请人： JANSSEN PHARMACEUTICA NV
发明人： DE BRUYN MARCEL FRANS LEOPOLD , VAN EMELEN KRISTOF
IPC分类号： A61K31/4164 , A61K31/4178 , A61K31/513 , A61P1/14 , A61P9/00 , A61P9/08 , C07D405/12 , C07D417/12
摘要： The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z 1 -Z 2 - is a bivalent radical; R 1 , R 2 and R 3 are each independently selected from hydrogen, C 1-6 alkyl, hydroxy, halo and the like; or when R 1 and R 2 are on adjacent carbon atoms, R 1 and R 2 taken together may form a bivalent radical of formula; Alk 1 and Alk 2 are optionally substituted C 1-6 alkanediyl; R 6 is hydrogen or phenylmethyl; R 5 is a radical of formula wherein n is 1 or 2; p 1 is 0, and p 2 is 1 or 2; or p 1 is 1 or 2, and p 2 is 0; X is oxygen, sulfur or -NR 9 ; Y is oxygen or sulfur; R 7 is hydrogen, C 1-6 alkyl, C 3-6 cycloalkyl, phenyl or phenylmethyl; R 8 is C 1-6 alkyl, C 3-6 cycloalkyl phenyl or phenylmethyl; R 9 is cyano, C 1-6 alkyl, C 3-6 cyclo-alkyl, C 1-6 alkyloxycarbonyl or aminocarbonyl; R 10 is hydrogen or C 1-6 alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impaired fundic relaxation.

69. 发明专利

CA2374905A1 PYRROLIDINYL, PIPERIDINYL OR HOMOPIPERIDINYL SUBSTITUTED (BENZODIOXAN, BENZOFURAN OR BENZOPYRAN) DERIVATIVES 未知
公开(公告)号：CA2374905A1
公开(公告)日：2000-12-14
申请号：CA2374905
申请日：2000-05-23
申请人： JANSSEN PHARMACEUTICA NV
发明人： VAN EMELEN KRISTOF , DE BRUYN MARCEL FRANS LEOPOLD , WIGERINCK PIET TOM BERT PAUL , VERSCHUEREN WIM GASTON
IPC分类号： A61K31/505 , A61K31/513 , A61P1/06 , A61P1/14 , A61P9/00 , C07D405/12 , C07D405/14
摘要： The present invention concerns compounds of formula (I), a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical ; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical (a) is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula (c-1), (c - 2), (c-3), (c-4), (c-5) wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p 1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or =NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1- 6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3- 6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1- 6alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impair ed fundic relaxation.

70. 发明专利

CA2549869C PYRIDO- AND PYRIMIDOPYRIMIDINE DERIVATIVES AS ANTI- PROLIFERATIVE AGENTS 未知
公开(公告)号：CA2549869C
公开(公告)日：2015-05-05
申请号：CA2549869
申请日：2004-12-15
申请人： JANSSEN PHARMACEUTICA NV
发明人： FREYNE EDDY JEAN EDGARD , WILLEMS MARC , STORCK PIERRE HENRI , PONCELET VIRGINIE SOPHIE , VAN EMELEN KRISTOF , BUIJNSTERS PETER JACOBUS JOHANNES ANTONIUS , EMBRECHTS WERNER CONSTANT JOHAN , PERERA TIMOTHY PIETRO SUREN
IPC分类号： C07D498/18 , A61K31/519 , A61P35/00 , C07D471/04 , C07D471/18 , C07D487/04
摘要： The present invention concerns the compounds of formula (I) the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein a1-a2=a3-a4 represents a divalent radical selected from N-CH=CH-CH, N-CH N-CH or CH-CH=N-CH; Z represents NH; Y represents -C3-9alkyl-, -Cl-5alkyl-NR13-Cl-5alkyl-,-C1-6alkyl-NH-CO- or -CO-NH -C1-6alkyl- ; X1 represents -O- or -NR11-; X2 represents -C1-2alkyl-, -O-C1-2alkyl, -O- or -O-CH2-;R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-Cl-4 alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen; R4 represents hydroxy, C1-4alkyloxy-, Ar4-C1-4alkyloxy or R4 represents Cl-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R11 represents hydrogen; R12 represents hydrogen, Cl-4alkyl- or Cl-4alkyl-oxy-carbonyl-; R13represents Het14-Cl-4alkyl, in particular morpholinyl-Cl-4alkyl; Het2 represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferably methyl; Het14 represents morpholinyl; Het16 represents a heterocycle selected from morpholinyl or pyrrolidinyl; Ar4 represents phenyl; Ar5 represents phenyl optionally substituted with cyano.

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