公开(公告)号：HU227612B1

公开(公告)日：2011-09-28

申请号：HU0202967

申请日：2002-09-09

Applicant: SOLVAY PHARM GMBH

Inventor： JASSERAND DANIEL ,  PREUSCHOFF ULF ,  ANTEL JOCHEN ,  DAVID SAMUEL ,  SANN HOLGER ,  BRUECKNER REINHARD ,  REICHE DANIA ,  EECKOUT CHRISTIAN

IPC: C07D295/00 ,  C07D295/12 ,  A61K31/341 ,  A61K31/381 ,  A61K31/495 ,  A61K31/496 ,  A61P1/00 ,  A61P1/04 ,  A61P1/06 ,  A61P29/00 ,  A61P43/00 ,  C07D209/08 ,  C07D295/08 ,  C07D295/084 ,  C07D295/092 ,  C07D307/52 ,  C07D333/20 ,  C07D407/04 ,  C07D407/06 ,  C07D409/06

Abstract: 1-(1-(Hetero)aryl)-1-(polyhydroxyalkyl)-methyl)-4-(4-(N-methylbenzamid o)-3-phenylbutyl)-piperazine derivatives (I) are new. Also new are 1-unsubstituted analog intermediates (II). 1-(1-(Hetero)aryl)-1-(polyhydroxyalkyl)-methyl)-4-(4-(N-methylbenzamid o)-3-phenylbutyl)-piperazine derivatives of formula (I) and their acid addition salts are new. A = naphthyl, phenyl (optionally substituted by OH), mono- or bi-cyclic heteroaryl or 3-6C alkenyl (optionally substituted by phenyl); Q = (CHOR1)k-(CHOR2)l-(CHOR3)m-(CHOR4)n-CH2OR5 ; R1-R5 = H or lower alkanoyl, or two of R1-R5 = CO, CS or CH2 (optionally substituted by lower alkyl or 4-5C alkylene), completing a 5- or 6-membered ring; k, l, m, n = 0 or 1, and R6, R7 = H or halo. Independent claims are also included for: (1) the preparation of (I), and (2) new piperazine derivative intermediates of formula (II).

公开(公告)号：AU2002301141B2

公开(公告)日：2008-11-06

申请号：AU2002301141

申请日：2002-09-12

Applicant: SOLVAY PHARM GMBH

Inventor： EECKHOUT CHRISTIAN ,  ANTEL JOCHEN ,  JASSERAND DANIEL ,  REICHE DANIA ,  PREUSCHOFF ULF ,  DAVID SAMUEL ,  BRUCKNER REINHARD ,  SANN HOLGER

IPC: C07D295/12 ,  C07D405/06 ,  A61K31/341 ,  A61K31/381 ,  A61K31/495 ,  A61K31/496 ,  A61P1/00 ,  A61P29/00 ,  A61P43/00 ,  C07D209/08 ,  C07D295/08 ,  C07D295/084 ,  C07D295/092 ,  C07D295/13 ,  C07D307/52 ,  C07D333/20 ,  C07D403/06 ,  C07D407/04 ,  C07D407/06 ,  C07D409/06

Abstract: 1-(1-(Hetero)aryl)-1-(polyhydroxyalkyl)-methyl)-4-(4-(N-methylbenzamid o)-3-phenylbutyl)-piperazine derivatives (I) are new. Also new are 1-unsubstituted analog intermediates (II). 1-(1-(Hetero)aryl)-1-(polyhydroxyalkyl)-methyl)-4-(4-(N-methylbenzamid o)-3-phenylbutyl)-piperazine derivatives of formula (I) and their acid addition salts are new. A = naphthyl, phenyl (optionally substituted by OH), mono- or bi-cyclic heteroaryl or 3-6C alkenyl (optionally substituted by phenyl); Q = (CHOR1)k-(CHOR2)l-(CHOR3)m-(CHOR4)n-CH2OR5 ; R1-R5 = H or lower alkanoyl, or two of R1-R5 = CO, CS or CH2 (optionally substituted by lower alkyl or 4-5C alkylene), completing a 5- or 6-membered ring; k, l, m, n = 0 or 1, and R6, R7 = H or halo. Independent claims are also included for: (1) the preparation of (I), and (2) new piperazine derivative intermediates of formula (II).

公开(公告)号：CA2245484C

公开(公告)日：2008-04-29

申请号：CA2245484

申请日：1998-08-25

Applicant: SOLVAY PHARM GMBH

Inventor： ANTEL JOCHEN ,  JASSERAND DANIEL ,  DAVID SAMUEL ,  BRUECKNER REINHARD ,  EECKHOUT CHRISTIAN ,  BIELENBERG GERHARD-WILHELM

IPC: C07D403/06 ,  A61K31/495 ,  A61K31/496 ,  A61P1/00 ,  A61P29/00 ,  A61P43/00 ,  C07D209/00 ,  C07D209/14 ,  C07D241/00

Abstract: Compounds of Formula I (see formula I) wherein R1 is hydrogen or lower alkyl, R2 is hydrogen or halogen and R3 is hydrogen or lower alkoxy, and their pharmacologically acceptable acid addition salts and pharmaceutical compositions containing these compounds and also processes for the preparation of these compounds.

公开(公告)号：CA2245926C

公开(公告)日：2006-12-12

申请号：CA2245926

申请日：1998-08-26

Applicant: SOLVAY PHARM GMBH

Inventor： ANTEL JOCHEN ,  BRUECKNER REINHARD ,  ZIEGLER DIETER ,  BIELENBERG GERHARD-WILHELM ,  EECKHOUT CHRISTIAN ,  DAVID SAMUEL ,  PECK MICHAEL

IPC: C07D243/08 ,  A61K31/55 ,  A61P1/00 ,  A61P43/00 ,  C07D405/00

Abstract: Neurokinin-antagonistic compounds corresponding to formula I: See formula I in which R1 is hydrogen or lower alkyl, R2 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, and R3 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, or R2 and R3 together are alkylenedioxy with 1 to 2 carbon atoms, bonded to adjacent carbon atoms of the phenyl ring, R4 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, and R5 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, or R4 and R5 together are alkylenedioxy with 1 to 2 carbon atoms, bonded to adjacent carbon atoms of the phenyl ring, R6 is lower alkyl, halogen or trifluoromethyl, R7 is lower alkyl, halogen or trifluoromethyl, A is a -(CH2)n- group in which n represents an integer from 1 to 3, or an -NH-(CH2)m- group in which m represents an integer from 2 to 3, and B is an alkylene chain with 1 to 3 carbon atoms optionally substituted by lower alkyl, and physiologically acceptable salts thereof and processes for the preparation of these compounds.

公开(公告)号：ES2250561T3

公开(公告)日：2006-04-16

申请号：ES02020115

申请日：2002-09-07

Applicant: SOLVAY PHARM GMBH

Inventor： JASSERAND DANIEL ,  PREUSCHOFF ULF ,  ANTEL JOCHEN ,  DAVID SAMUEL ,  SANN HOLGER ,  BRUCKNER REINHARD

IPC: C07D295/12 ,  A61K31/341 ,  A61K31/381 ,  A61K31/496 ,  A61P1/00 ,  A61P29/00 ,  A61P43/00 ,  C07D209/08 ,  C07D295/08 ,  C07D295/084 ,  C07D295/092 ,  C07D307/52 ,  C07D333/20 ,  C07D407/04 ,  C07D407/06 ,  C07D409/06

Abstract: Compuestos de fórmula general I en la cual A significa naftilo, fenilo eventualmente sustituido con hidroxi, heteroarilo mono- o bicíclico, o alquenilo C3- 6 eventualmente sustituido con fenilo, Z significa un subgrupo de fórmula general en la cual R1 significa hidrógeno o alcanoílo C2-4, o bien puede formar, conjuntamente con otro sustituyente seleccionado del grupo compuesto por R2, R3, R4 y R5, un anillo de 5 ó 6 miembros, puenteado a través de carbonilo, tiocarbonilo, o a través de metileno eventualmente sustituido con alquilo C1- 4 o con alquileno C4-5, R2 significa hidrógeno o alcanoílo C2-4, o bien puede formar, conjuntamente con otro sustituyente seleccionado del grupo compuesto por R1, R3, R4 y R5, un anillo de 5 ó 6 miembros, puenteado a través de carbonilo, tiocarbonilo, o a través de metileno eventualmente sustituido con alquilo C1- 4 o con alquileno C4-5, R3 significa hidrógeno o alcanoílo C2-4, o bien puede formar, conjuntamente con otro sustituyente seleccionado del grupo compuesto por R1, R2, R4 y R5, un anillo de 5 ó 6 miembros, puenteado a través de carbonilo, tiocarbonilo, o a través de metileno eventualmente sustituido con alquilo C1- 4 o con alquileno C4-5, R4 significa hidrógeno o alcanoílo C2-4, o bien puede formar, conjuntamente con otro sustituyente seleccionado del grupo compuesto por R1, R2, R3 y R5, un anillo de 5 ó 6 miembros, puenteado a través de carbonilo, tiocarbonilo, o a través de metileno eventualmente sustituido con alquilo C1- 4 o con alquileno C4-5, R5 significa hidrógeno o alcanoílo C2-4, o bien puede formar, conjuntamente con otro sustituyente seleccionado del grupo compuesto por R1, R2, R3 y R4, un anillo de 5 ó 6 miembros, puenteado a través de carbonilo, tiocarbonilo, o a través de metileno eventualmente sustituido con alquilo C1- 4 o con alquileno C4-5, k significa 0 ó 1, l significa 0 ó 1, m significa 0 ó 1, n significa 0 ó 1, R6 significa halógeno o hidrógeno, y R7 significa halógeno o hidrógeno, así como sales por adición de ácidos fisiológicamente tolerables de compuestos de fórmula I.

公开(公告)号：DE10145044A1

公开(公告)日：2003-04-03

申请号：DE10145044

申请日：2001-09-13

Applicant: SOLVAY PHARM GMBH

Inventor： JASSERAND DANIEL ,  PREUSCHOFF ULF ,  ANTEL JOCHEN ,  DAVID SAMUEL ,  SANN HOLGER ,  BRUECKNER REINHARD ,  REICHE DANIA ,  EECKOUT CHRISTIAN

IPC: C07D295/12 ,  A61K31/341 ,  A61K31/381 ,  A61K31/496 ,  A61P1/00 ,  A61P29/00 ,  A61P43/00 ,  C07D209/08 ,  C07D295/08 ,  C07D295/084 ,  C07D295/092 ,  C07D307/52 ,  C07D333/20 ,  C07D407/04 ,  C07D407/06 ,  C07D409/06 ,  C07D241/04 ,  A61K31/495

Abstract: 1-(1-(Hetero)aryl)-1-(polyhydroxyalkyl)-methyl)-4-(4-(N-methylbenzamid o)-3-phenylbutyl)-piperazine derivatives (I) are new. Also new are 1-unsubstituted analog intermediates (II). 1-(1-(Hetero)aryl)-1-(polyhydroxyalkyl)-methyl)-4-(4-(N-methylbenzamid o)-3-phenylbutyl)-piperazine derivatives of formula (I) and their acid addition salts are new. A = naphthyl, phenyl (optionally substituted by OH), mono- or bi-cyclic heteroaryl or 3-6C alkenyl (optionally substituted by phenyl); Q = (CHOR1)k-(CHOR2)l-(CHOR3)m-(CHOR4)n-CH2OR5 ; R1-R5 = H or lower alkanoyl, or two of R1-R5 = CO, CS or CH2 (optionally substituted by lower alkyl or 4-5C alkylene), completing a 5- or 6-membered ring; k, l, m, n = 0 or 1, and R6, R7 = H or halo. Independent claims are also included for: (1) the preparation of (I), and (2) new piperazine derivative intermediates of formula (II).

公开(公告)号：DZ2597A1

公开(公告)日：2003-03-01

申请号：DZ980207

申请日：1998-08-26

Applicant: SOLVAY PHARM GMBH

Inventor： JASSERAND DANIEL ,  DAVID SAMUEL ,  ANTEL JOCHEN ,  BRUCKNER REINHARD ,  EECKHOUT CHRISTIAN ,  GERHARD-WILHELM BIELENBERG

IPC: C07D403/06 ,  A61K31/495 ,  A61K31/496 ,  A61P1/00 ,  A61P29/00 ,  A61P43/00 ,  C07D209/00 ,  C07D209/14 ,  C07D241/00 ,  C07D ,  A61K

Abstract: Compounds of Formula I wherein R1 is hydrogen or lower alkyl, R2 is hydrogen or halogen and R3 is hydrogen or lower alkoxy, and their pharmacologically acceptable acid addition salts and pharmaceutical compositions containing these compounds and also processes for the preparation of these compounds. Pharmaceutical composition containing these compounds are suitable, for example, for treating functional and inflammatory disorders of the gastrointestinal tract.

公开(公告)号：NO20024351D0

公开(公告)日：2002-09-12

申请号：NO20024351

申请日：2002-09-12

Applicant: SOLVAY PHARM GMBH

Inventor： JASSERAND DANIEL ,  ANTEL JOCHEN ,  SANN HOLGER ,  REICHE DANIA ,  PREUSCHOFF ULF ,  DAVID SAMUEL ,  BRUECKNER REINHARD ,  EECKHOUT CHRISTIAN

IPC: C07D295/12 ,  A61K31/341 ,  A61K31/381 ,  A61K31/496 ,  A61P1/00 ,  A61P29/00 ,  A61P43/00 ,  C07D209/08 ,  C07D295/08 ,  C07D295/084 ,  C07D295/092 ,  C07D307/52 ,  C07D333/20 ,  C07D407/04 ,  C07D407/06 ,  C07D409/06 ,  C07D

Abstract: 1-(1-(Hetero)aryl)-1-(polyhydroxyalkyl)-methyl)-4-(4-(N-methylbenzamid o)-3-phenylbutyl)-piperazine derivatives (I) are new. Also new are 1-unsubstituted analog intermediates (II). 1-(1-(Hetero)aryl)-1-(polyhydroxyalkyl)-methyl)-4-(4-(N-methylbenzamid o)-3-phenylbutyl)-piperazine derivatives of formula (I) and their acid addition salts are new. A = naphthyl, phenyl (optionally substituted by OH), mono- or bi-cyclic heteroaryl or 3-6C alkenyl (optionally substituted by phenyl); Q = (CHOR1)k-(CHOR2)l-(CHOR3)m-(CHOR4)n-CH2OR5 ; R1-R5 = H or lower alkanoyl, or two of R1-R5 = CO, CS or CH2 (optionally substituted by lower alkyl or 4-5C alkylene), completing a 5- or 6-membered ring; k, l, m, n = 0 or 1, and R6, R7 = H or halo. Independent claims are also included for: (1) the preparation of (I), and (2) new piperazine derivative intermediates of formula (II).

公开(公告)号：BR9803237A

公开(公告)日：2000-02-08

申请号：BR9803237

申请日：1998-08-26

Applicant: SOLVAY PHARM GMBH

Inventor： JASSERAND DANIEL ,  DAVID SAMUEL ,  ANTEL JOCHEN ,  BRUECKNER REINHARD ,  EECKHOUT CHRISTIAN ,  BIELENBERG GERHARD-WILHELM

IPC: C07D403/06 ,  A61K31/495 ,  A61K31/496 ,  A61P1/00 ,  A61P29/00 ,  A61P43/00 ,  C07D209/00 ,  C07D209/14 ,  C07D241/00

Abstract: Compounds of Formula I wherein R1 is hydrogen or lower alkyl, R2 is hydrogen or halogen and R3 is hydrogen or lower alkoxy, and their pharmacologically acceptable acid addition salts and pharmaceutical compositions containing these compounds and also processes for the preparation of these compounds. Pharmaceutical composition containing these compounds are suitable, for example, for treating functional and inflammatory disorders of the gastrointestinal tract.

公开(公告)号：TR199801681A2

公开(公告)日：1999-03-22

申请号：TR9801681

申请日：1998-08-27

Applicant: SOLVAY PHARM GMBH

Inventor： DAVID SAMUEL ,  ANTEL JOCHEN ,  BRUECKNER REINHARD ,  ZIEGLER DIETER ,  EECKHOUT CHIRISTIAN ,  BIELENBERG GERHARD-WILHELM ,  PECK MICHAEL

IPC: A61K31/55 ,  A61P1/00 ,  A61P43/00 ,  C07D243/08 ,  C07D ,  A61K

Abstract: 1-Benzoyl-4-aminoacyl-7-phenyl-1,4-diazepine derivatives (I) are new. Also new are four classes of intermediates. 1,4-Diazepine derivatives of formula (I) and their acid addition salts are new. Ph1 = phenyl substituted by R2 and R3; Ph2 = phenyl substituted by R4 and R5; Ph3 = 3-(R6)-5-(R7)-phenyl; R1 = H or alkyl; R2-R5 = H, alkyl, alkoxy, halo or CF3; or R2+R3 or R4+R5 on adjacent C = 1-2C alkylenedioxy; R6,R7 = alkyl, halo or CF3; A = (CH2)n or NH(CH2)m; n = 1-3; m = 2 or 3; and B = 1-3C alkylene chain (optionally substituted by alkyl).