公开(公告)号：US20100210618A1

公开(公告)日：2010-08-19

申请号：US12663011

申请日：2008-06-06

申请人： Jean-Pierre Andre Marc Bongartz ,  Joannes Theodorus Maria Linders ,  Lieven Mieerpoel ,  Guy Rosalia Eugeen Van Lommen ,  Erwin Coesemans ,  Mirielle Braeken ,  Christophe Francis Robert Nestor Buyck ,  Monique Jenny Marie Berwaer ,  Katharina Antonia Germania J.M. De Waepenaret ,  Peter Walter Maria Roevens ,  Petr Vladimirivich Davidenko

发明人： Jean-Pierre Andre Marc Bongartz ,  Joannes Theodorus Maria Linders ,  Lieven Mieerpoel ,  Guy Rosalia Eugeen Van Lommen ,  Erwin Coesemans ,  Mirielle Braeken ,  Christophe Francis Robert Nestor Buyck ,  Monique Jenny Marie Berwaer ,  Katharina Antonia Germania J.M. De Waepenaret ,  Peter Walter Maria Roevens ,  Petr Vladimirivich Davidenko

IPC分类号： A61K31/397 ,  C07D401/12 ,  C07D417/12 ,  A61K31/497 ,  A61K31/454 ,  C07D405/12 ,  C07D241/04 ,  A61K31/4965 ,  C07D211/78 ,  A61K31/451 ,  C07D403/12 ,  C07D413/12 ,  A61K31/5377 ,  C07D279/02 ,  A61K31/541 ,  C07D279/12 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P1/16

CPC分类号： A61K31/4523 ,  A61K31/451 ,  A61K31/454 ,  A61K31/495 ,  A61K31/496 ,  C07D207/277 ,  C07D207/323 ,  C07D211/26 ,  C07D211/60 ,  C07D231/12 ,  C07D233/54 ,  C07D233/64 ,  C07D235/18 ,  C07D249/08 ,  C07D257/04 ,  C07D263/34 ,  C07D277/56 ,  C07D279/02 ,  C07D279/12 ,  C07D295/20 ,  C07D295/205 ,  C07D295/21 ,  C07D295/215 ,  C07D307/54 ,  C07D319/18 ,  C07D401/12 ,  C07D417/12 ,  C07D417/14

摘要： The invention relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —O—C(═O)—; —C(═O)—C(═O)—; —NRX—C(═O)—; —Z—C(═O)—; —Z—NRX—C(═O)—; —C(═O)—Z—; —NRX—C(═O)—Z—; —C(═S)—; —NRX—C(═S)—; —Z—C(═S)—; —Z—NRX—C(═S)—; —C(═S)—Z—; —NRX—C(═S)—Z—; Z represents a bivalent radical selected from C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl; wherein each of said C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in C1-6alkanediyl may optionally be replaced by C1-6alkanediyl; Y represents —C(═O)—NRX— or —NRX—C(═O)—; R1 represents adamantanyl, C3-6cycloalkyl; aryl1 or Het1; R2 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6Cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl or heterocycle may optionally be substituted; R7 represents hydrogen, halo, C1-4alkyl, C1-4alkyl substituted with hydroxyl; provided that the following compounds (II), (III) are excluded; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine, as a DGAT inhibitor, of said compounds.

公开(公告)号：US08981094B2

公开(公告)日：2015-03-17

申请号：US12663013

申请日：2008-06-06

申请人： Jean-Pierre André Marc Bongartz ,  Joannes Theodorus Maria Linders ,  Lieven Meerpoel ,  Guy Rosalia Eugeen Van Lommen ,  Erwin Coesemans ,  Mirielle Braeken ,  Christophe Francis Robert Nestor Buyck ,  Monique Jenny Marie Berwaer ,  Katharina Antonia Germania J. M. De Waepenaert ,  Peter Walter Maria Roevens ,  Gustaaf Maria Boeckx ,  Petr Vladimirivich Davidenko

发明人： Jean-Pierre André Marc Bongartz ,  Joannes Theodorus Maria Linders ,  Lieven Meerpoel ,  Guy Rosalia Eugeen Van Lommen ,  Erwin Coesemans ,  Mirielle Braeken ,  Christophe Francis Robert Nestor Buyck ,  Monique Jenny Marie Berwaer ,  Katharina Antonia Germania J. M. De Waepenaert ,  Peter Walter Maria Roevens ,  Gustaaf Maria Boeckx ,  Petr Vladimirivich Davidenko

IPC分类号： C07D211/00 ,  C07D241/04 ,  C07D295/00 ,  C07D401/00 ,  C07D403/00 ,  C07D295/205 ,  C07D207/09 ,  C07D211/26 ,  C07D211/38 ,  C07D213/40 ,  C07D213/56 ,  C07D213/61 ,  C07D213/75 ,  C07D233/18 ,  C07D295/192 ,  C07D295/21 ,  C07D295/215 ,  C07D295/24 ,  C07D295/26 ,  C07D307/52 ,  C07D307/79 ,  C07D309/04 ,  C07D317/58 ,  C07D333/24

CPC分类号： C07D295/205 ,  C07D207/09 ,  C07D211/26 ,  C07D211/38 ,  C07D213/40 ,  C07D213/56 ,  C07D213/61 ,  C07D213/75 ,  C07D233/18 ,  C07D295/192 ,  C07D295/21 ,  C07D295/215 ,  C07D295/24 ,  C07D295/26 ,  C07D307/52 ,  C07D307/79 ,  C07D309/04 ,  C07D317/58 ,  C07D333/24

摘要： The invention relates to a DGAT inhibitor of formula (I): including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —C(═O)—; —O—C(═O)—; C(═O)—C(═O)—; —NRx—C(═O)—; —Z1—C(O)—; —Z1—NRx—C(═O)—; —C(═O)—Z1—; —NRx—C(═O)—Z1—; —S(═O)p-; —C(═S)—; —NRx—C(═S)—; —Z1—C(═S)—; —Z1—NRx—C(═S)—; —C(═S)—Z1-; —NRx—C(═S)—Z—; Y represents NRx—C(=0)-Z2—; —NRx—C(=0)-Z2—NRy—; —NRx—C(=0)-Z2—NRy—C(=0)-; —NRx—C(=0)-Z2—NRy—C(=0)-O—; —NRx—C(=0)-Z2-0-; —NRx—C(=0)-Z2-0-C(=0)-; —NRx—C(=0)-Z2—C(=0)-; —NRx—C(=0)-Z2—C(=0)-; —NRx—C(=0)-0-Z2—C(=0)-; —NRx—C(=0)-0-Z2—C(=0)-0-; —NRx—C(═O)—O—Z2—O—C(═O)—; —NRx—C(═O)—Z2—C(═O)—NRy—; —NRx—C(═O)—Z2—NRy—C(=0)-NRy—; —C(═O)—Z2—; —C(═O)—Z2—O—; —C(=0)-NRx—Z2—; —C(=0)-NRx—Z2-0-; —C(=0)-NRx—Z2—C(=0)-0-; —C(=0)-NRx—Z2-0-C(=0)-; —C(=0)-NRx—Z2—NRy—; —C(=0)-NRx—Z2—NRy—C(=0)-; —C(=0)-NRx—Z2—NRy—C(=0)-0-; R1 represents C1-12alkyl optionally substituted with cyano, C1-4alkyloxy, C1-4alkyl-oxyC1-4alkyloxy, C3-6Cycloalkyl or aryl; C2-6alkenyl; C2-6alkynyl; C3-6cycloalkyl; adamantanyl; aryl1; aryl1C1-6alkyl; Het1; or Het1C1-6alkyl; provided that when Y represents —NRX—C(═O)—Z2—; —NRx—C(=0)-Z2—NRy; —NRX—C(═O)—Z2—C(═O)—NRy—; —C(═O)—Z2—; —NRx—C(=0)-Z2—NRy—C(=0)-NRy—; —C(═O)—NRX—Z2—; —C(═O)—NRX—O—Z2—; or —C(=0)-NRx—Z2—NRy—; then R1 may also represent hydrogen; R2 represents hydrogen, C1-12alkyl, C2-6alkenyl or R3; provided that if X represents —O—C(═O)—; the R2 represents R3; and provided that (A) is excluded; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.

公开(公告)号：US20100190789A1

公开(公告)日：2010-07-29

申请号：US12663013

申请日：2008-06-06

申请人： Jean-Pierre Andre Marc Bongartz ,  Joannes Theodorus Maria Linders ,  Lieven Meerpoel ,  Guy Rosalia Eugeen Van Lommen ,  Erwin Coesemans ,  Mirielle Braeken ,  Christophe Francis Robert Nestor Buyck ,  Monique Jenny Marie Berwaer ,  Katharina Antonia Germania J.M De Waepenaert ,  Peter Walter Maria Roevens ,  Gustaaf Maria Boeckx ,  Peter Vladimirivich Davidenko

发明人： Jean-Pierre Andre Marc Bongartz ,  Joannes Theodorus Maria Linders ,  Lieven Meerpoel ,  Guy Rosalia Eugeen Van Lommen ,  Erwin Coesemans ,  Mirielle Braeken ,  Christophe Francis Robert Nestor Buyck ,  Monique Jenny Marie Berwaer ,  Katharina Antonia Germania J.M De Waepenaert ,  Peter Walter Maria Roevens ,  Gustaaf Maria Boeckx ,  Peter Vladimirivich Davidenko

IPC分类号： A61K31/5377 ,  C07D241/04 ,  A61K31/495 ,  C07D401/12 ,  A61K31/496 ,  C07D403/10 ,  C07D405/12 ,  C07D403/12 ,  C07D413/12 ,  C07D211/34 ,  A61K31/451 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P1/16

CPC分类号： C07D295/205 ,  C07D207/09 ,  C07D211/26 ,  C07D211/38 ,  C07D213/40 ,  C07D213/56 ,  C07D213/61 ,  C07D213/75 ,  C07D233/18 ,  C07D295/192 ,  C07D295/21 ,  C07D295/215 ,  C07D295/24 ,  C07D295/26 ,  C07D307/52 ,  C07D307/79 ,  C07D309/04 ,  C07D317/58 ,  C07D333/24

摘要： The invention relates to a DGAT inhibitor of formula (I): including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —C(═O)—; —O—C(═O)—; C(═O)—C(═O)—; —NRx—C(═O)—; —Z1—C(O)—; —Z1—NRx—C(═O)—; —C(═O)—Z1—; —NRx—C(═O)—Z1—; —S(═O)p-; —C(═S)—; —NRx—C(═S)—; —Z1—C(═S)—; —Z1—NRx—C(═S)—; —C(═S)—Z1-; NRx—C(═S)—Z—; Y represents NRx—C(=0)-Z2—; —NRx—C(=0)-Z2—NRy—; —NRx—C(=0)-Z 2—NRy—C(=0)—; —NRx—C(=0)-Z2—NRy—C(=0)-; O—; —NRx—C(=0)-Z2-0-; —NRx—C(=0)-Z2-0-C(=0)-; —NRx—C(=0)-Z2—C(=0)-; —NRx—C(=0)-Z2—C(=0)-; —NRx—C(=0)-0-Z2—C(=0)-; —NRx—C(=0)-0-Z2—C(=0)-0-; —NRx—C(═O)—O—Z2—O—C(═O)—; —NRx—C(═O)—Z2—C(═O)—NRy—; —NRx—C(═O)—Z2—NRy—C(=0)-NRy—; —C(═O)—Z2—; —C(═O)—Z2—O—; —C(=0)-NRx—Z2—; —C(=0)-NRx—Z2-0-; —C(=0)-NRx—Z2—C(=0)-0-; —C(=0)-NRx—Z2-0-C(=0)-; —C(=0)-NRx—Z2—NRy—; —C(=0)—NRx—Z2—NRy—C(=0)-; —C(=0)-NRx—Z2—NRy—C(=0)-0-; R1 represents C1-12alkyl optionally substituted with cyano, C1-4alkyloxy, C1-4alkyl-oxyC1-4alkyloxy, C3-6Cycloalkyl or aryl; C2-6alkenyl; C2-6alkynyl; C3-6cycloalkyl; adamantanyl; aryl1; aryl1C1-6alkyl; Het1; or Het1C1-6alkyl; provided that when Y represents —NRx—C(═O)—Z2—; —NRx—C(=0)-Z2—NRy; —NRx—C(═O)—Z2—C(═O)—NRy—; —C(═O)—Z2—; —NRx—C(=0)-Z2—NRy—C(=0)—NRy—; —C(═O)—NR—Z2—; —C(═O)—NR—O—Z2—; or —C(=0)-NRx—Z2—NRy—; then R1 may also represent hydrogen; R2 represents hydrogen, C1-12alkyl, C2-6alkenyl or R3; provided that if X represents —O—C(═O)—; the R2 O represents R3; and provided that (A) is excluded; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.

公开(公告)号：US08946228B2

公开(公告)日：2015-02-03

申请号：US12663011

申请日：2008-06-06

申请人： Jean-Pierre André Marc Bongartz ,  Joannes Theodorus Maria Linders ,  Lieven Meerpoel ,  Guy Rosalia Eugeen Van Lommen ,  Erwin Coesemans ,  Mirielle Braeken ,  Christophe Francis Robert Nestor Buyck ,  Monique Jenny Marie Berwaer ,  Katharina Antonia Germania J. M. De Waepenaert ,  Peter Walter Maria Roevens ,  Petr Vladimirivich Davidenko

发明人： Jean-Pierre André Marc Bongartz ,  Joannes Theodorus Maria Linders ,  Lieven Meerpoel ,  Guy Rosalia Eugeen Van Lommen ,  Erwin Coesemans ,  Mirielle Braeken ,  Christophe Francis Robert Nestor Buyck ,  Monique Jenny Marie Berwaer ,  Katharina Antonia Germania J. M. De Waepenaert ,  Peter Walter Maria Roevens ,  Petr Vladimirivich Davidenko

IPC分类号： A61K31/4965 ,  C07D241/04 ,  C07D295/00 ,  A61K31/451 ,  A61K31/495 ,  C07D207/323 ,  C07D211/26 ,  C07D231/12 ,  C07D233/54 ,  C07D233/64 ,  C07D235/18 ,  C07D249/08 ,  C07D257/04 ,  C07D263/34 ,  C07D277/56 ,  C07D279/02 ,  C07D279/12 ,  C07D295/20 ,  C07D307/54 ,  C07D319/18 ,  C07D401/12 ,  C07D417/12 ,  C07D417/14

CPC分类号： A61K31/4523 ,  A61K31/451 ,  A61K31/454 ,  A61K31/495 ,  A61K31/496 ,  C07D207/277 ,  C07D207/323 ,  C07D211/26 ,  C07D211/60 ,  C07D231/12 ,  C07D233/54 ,  C07D233/64 ,  C07D235/18 ,  C07D249/08 ,  C07D257/04 ,  C07D263/34 ,  C07D277/56 ,  C07D279/02 ,  C07D279/12 ,  C07D295/20 ,  C07D295/205 ,  C07D295/21 ,  C07D295/215 ,  C07D307/54 ,  C07D319/18 ,  C07D401/12 ,  C07D417/12 ,  C07D417/14

摘要： The invention relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof, and methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine, as a DGAT inhibitor, of said compounds.

摘要翻译： 本发明涉及式（I）的DGAT抑制剂，包括其任何立体化学异构形式，其N-氧化物，其药学上可接受的盐或其溶剂合物，以及制备这些化合物的方法，包含所述化合物的药物组合物 作为所述化合物作为DGAT抑制剂的药物使用。

公开(公告)号：US20100184776A1

公开(公告)日：2010-07-22

申请号：US12663007

申请日：2008-06-05

申请人： Jean-Pierre Andre Marc Bongartz ,  Guy Rosalia Eugeen Van Lommen ,  Erwin Coesemans ,  Christophe Francis Robert Nestor Buyck

发明人： Jean-Pierre Andre Marc Bongartz ,  Guy Rosalia Eugeen Van Lommen ,  Erwin Coesemans ,  Christophe Francis Robert Nestor Buyck

IPC分类号： A61K31/496 ,  C07D241/04 ,  A61K31/495 ,  C07D403/12 ,  A61P3/04 ,  A61P3/06 ,  A61P1/16

CPC分类号： C07D295/215 ,  C07D231/12

摘要： The invention relates to a DGAT inhibitor of formula (I) including any stereochemically isomeric form thereof, wherein A represents CH or N; X represents O or NRx; the dotted line represents an optional bond in case A represents a carbon atom; Y represents a direct bond; —NRx—C(═O)—; —C(═O)—NRx—; —NRx—C(═O)—Z—; —NRx—C(═O)—Z—NRy—; —NRx—C(═O)—Z—NRy—C(═O)—; —NRx—C(═O)—Z—NRy—C(═O)—O—; —NRx—C(═O)—Z—O—; —NRx—C(═O)—Z—O—C(═O)—; —NRx—C(═O)—Z—C(═O)—; —NRx—C(═O)—Z—C(═O)—O—; —NRx—C(═O)—O—Z—C(═O)—; —NRx—C(═O)—O—Z—C(═O)—O—; —NRx—C(═O)—O—Z—O—C(═O)—; —NRx—C(═O)—Z—C(═O)—NRy—; —NRx—C(═O)—Z—NRy—C(═O)—NRy—; —C(═O)—Z—; —C(═O)—Z—O—; —C(═O)—NRx—Z—; —C(═O)—NRx—Z—O—; —C(═O)—NRx—Z—C(═O)—O—; —C(═O)—NRx—Z—O—C(═O)—; —C(═O)—NRx—O—Z—; —C(═O)—NRx—Z—NRy—; —C(═O)—NRx—Z—NRy—C(═O)—; —C(═O)—NRx—Z—NRy—C(═O)—O—; R1 represents optionally substituted C1-12alkyl; C2-6alkenyl; C2-6alkynyl; C3-6cycloalkyl; aryl1; aryl1C1-6alkyl; Het1; or Het1C1-6alkyl; provided that when Y represents —NRx—C(═O)—Z—; —NRx—C(═O)—Z—NRy; —NRx—C(═O)—Z—C(═O)—NRy—; —C(═O)—Z—; —NRx—C(═O)—Z—NRy—C(═O)—NRy—; —C(═O)—NRx—Z—; —C(═O)—NRx—O—Z—; or —C(═O)—NRx—Z—NRy—; then R1 may also represent hydrogen; R2 and R3 each independently represent hydrogen; hydroxyl; carboxyl; halo; C1-6alkyl; polyhaloC1-6alkyl; C1-6alkyloxyoptionally substituted with C1-4alkyloxy; C1-6alkylthio; polyhaloC1-6alkyloxy; C1-6alkyloxycarbonyl; cyano; aminocarbonyl; mono- or di(C1-4alkyl)aminocarbonyl; C1-6alkylcarbonyl; nitro; amino; mono- or di(C1-4alkyl)amino; —S(═O)p-C1-4alkyl; R4 represents hydrogen; hydroxyl; carboxyl; halo; C1-6alkyl; polyhaloC1-6alkyl; optionally substituted C1-6alkyloxy; C1-6alkylthio; polyhalo-C1-6alkyloxy; C1-6alkyloxycarbonyl wherein C1-6alkyl may optionally be substituted; cyano; C1-6alkylcarbonyl; nitro; amino; mono- or di(C1-4alkyl)amino; C1-4alkylcarbonylamino; —S(═O)p-C1-4alkyl; R6R5N—C(═O)—; R6R5N—C1-6alkyl; C3-6cycloalkyl aryl; aryloxy; arylC1-4alkyl; aryl-C(═O)—C1-4alkyl; aryl-C(═O)—; Het; HetC1-4alkyl; Het-C(═O)—C1-4alkyl; Het-C(═O)—; Het-O—; R9 represents hydrogen, halo, C1-4alkyl, C1-4alkyl substituted with hydroxyl; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.

公开(公告)号：US08633197B2

公开(公告)日：2014-01-21

申请号：US12663007

申请日：2008-06-05

申请人： Jean-Pierre André Marc Bongartz ,  Guy Rosalia Eugeen Van Lommen ,  Erwin Coesemans ,  Christophe Francis Robert Nestor Buyck

发明人： Jean-Pierre André Marc Bongartz ,  Guy Rosalia Eugeen Van Lommen ,  Erwin Coesemans ,  Christophe Francis Robert Nestor Buyck

IPC分类号： A61K31/4965 ,  C07D241/04 ,  C07D295/00

CPC分类号： C07D295/215 ,  C07D231/12

摘要： The invention relates to a DGAT inhibitor of formula including any stereochemically isomeric form thereof, a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof, and methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.

摘要翻译： 本发明涉及一种DGAT抑制剂，其包括其任何立体化学异构形式，其N-氧化物，其药学上可接受的盐或其溶剂合物，以及制备这些化合物的方法，包含所述化合物的药物组合物以及用作 所述化合物的药物。

公开(公告)号：US07803823B2

公开(公告)日：2010-09-28

申请号：US11742741

申请日：2007-05-01

申请人： Christopher John Love ,  Guy Rosalia Eugeen Van Lommen ,  Julien Georges Pierre-Olivier Doyon ,  Jean-Pierre André Marc Bongartz ,  Marcel Jozef Maria Van der Aa ,  Robert Jozef Maria Hendrickx ,  Peter Jacobus Johannes Antonius Buijnsters ,  Ludwig Paul Cooymans ,  Nele Vandermaesen ,  Erwin Coesemans ,  Gustaaf Maria Boeckx

发明人： Christopher John Love ,  Guy Rosalia Eugeen Van Lommen ,  Julien Georges Pierre-Olivier Doyon ,  Jean-Pierre André Marc Bongartz ,  Marcel Jozef Maria Van der Aa ,  Robert Jozef Maria Hendrickx ,  Peter Jacobus Johannes Antonius Buijnsters ,  Ludwig Paul Cooymans ,  Nele Vandermaesen ,  Erwin Coesemans ,  Gustaaf Maria Boeckx

IPC分类号： A61K31/425 ,  C07D277/20

CPC分类号： C07D417/04 ,  C07D277/42 ,  C07D471/04

摘要： This invention concerns the use of a compound of formula (I′) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is halo; C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; aminocarbonyl; C1-6alkyl substituted with hydroxy, carboxyl, cyano, amino, amino substituted with piperidinyl, amino substituted with C1-4alkyl substituted piperidinyl, mono- or di(C1-6alkyl)amino, aminocarbonyl, mono- or di(C1-6alkyl)aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkyloxy, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl; polyhaloC1-4alkyl; cyano; amino; mono- or di(C1-6alkyl)aminocarbonyl; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; aminoS(═O)2—; mono- or di(C1-6alkyl)aminoS(═O)2; —C(═N—Rx)NRyRz; Q is optionally substituted C3-6cycloalkyl, phenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzthiazolyl, benzoxazolyl, benzimidazolyl, indazolyl, or imidazopyridyl, or Q is a radical of formula L is optionally substituted phenyl or an optionally substituted monocyclic 5 or 6-membered partially saturated or aromatic heterocycle or a bicyclic partially saturated or aromatic heterocycle; aryl is optionally substituted phenyl; for the manufacture of a medicament for the prevention or the treatment of inflammatory and/or auto-immune diseases mediated through TNF-α and/or IL-12.

摘要翻译： 本发明涉及式（I'）化合物的N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构体形式的用途，其中Z为卤素; C 1-6烷基; C 1-6烷基羰基; C 1-6烷氧基羰基; 氨基羰基; 被羟基，羧基，氰基，氨基，被哌啶取代的氨基，被C 1-4烷基取代的哌啶基取代的氨基，单或二（C 1-6烷基）氨基，氨基羰基，一或二（C 1-6烷基）氨基羰基 C 1-6烷氧基羰基，C 1-6烷氧基，哌啶基，哌嗪基，吗啉基，硫代吗啉基; 多卤代C 1-4烷基; 氰基; 氨基; 单或二（C 1-6烷基）氨基羰基; C 1-6烷氧基羰基; C 1-6烷基羰基氧基; 氨基S（= O）2-; 单或二（C 1-6烷基）氨基S（= O）2; -C（= N-Rx）NR y R z; Q是任选取代的C 3-6环烷基，苯基，吡啶基，嘧啶基，吡嗪基，哒嗪基，苯并噻唑基，苯并恶唑基，苯并咪唑基，吲唑基或咪唑并吡啶基，或Q是式L的基团是任选取代的苯基或任选取代的单环5或6- 元部分饱和或芳族杂环或双环部分饱和或芳族杂环; 芳基是任选取代的苯基; 用于制备用于预防或治疗通过TNF-α和/或IL-12介导的炎症和/或自身免疫疾病的药物。

公开(公告)号：US20070249691A1

公开(公告)日：2007-10-25

申请号：US11569268

申请日：2005-05-24

申请人： Gustaaf Boeckx ,  Guy Rosalia Eugeen Van Lommen ,  Julien Georges Pierre-Olivier Doyon ,  Erwin Coesemans

发明人： Gustaaf Boeckx ,  Guy Rosalia Eugeen Van Lommen ,  Julien Georges Pierre-Olivier Doyon ,  Erwin Coesemans

IPC分类号： A61K31/4164 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/426 ,  A61P29/00 ,  C07D233/84 ,  C07D261/06 ,  C07D271/10 ,  C07D277/18

CPC分类号： C07C211/29 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/501 ,  A61K31/502 ,  C07D233/84 ,  C07D233/88 ,  C07D401/04 ,  C07D401/06 ,  C07D403/06 ,  C07D409/04 ,  C07D409/06 ,  C07D413/04 ,  C07D413/06 ,  C07D417/06

摘要： The present invention relates to a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine, a polymorphic form or a stereochemically isomeric form thereof, wherein R1 represents hydrogen, C1-6alkyl, C3-7cycloalkyl, C1-6alkyloxyC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, aryl or heteroaryl; each R2 independently represents halo, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, polyhaloC1-6alkyl, polyhaloC1-6alkyloxy, cyano, aminocarbonyl, amino, mono- or di(C1-4alkyl)amino, nitro, aryl or aryloxy; R3 represents hydrogen, cyano, optionally substituted C1-6alkyl, C(═O)—O—R5, C(═O)—NR6aR6b, C(═S)—NR6aR6b, S(═O)2—NR6aR6b or C(═O)—R7; R4 represents hydrogen or C1-6alkyl; n is 1, 2, 3, 4 or 5; Z represents a cyclic ring system. The invention also relates to processes for preparing the compounds of formula (I), their use as CCR2 antagonists and pharmaceutical compositions comprising them.

摘要翻译： 本发明涉及式（I）化合物的N-氧化物，药学上可接受的加成盐，季胺，多晶型或其立体化学异构形式，其中R 1表示氢， C 1-6烷基，C 3-7环烷基，C 1-6烷氧基C 1-6烷基， 二（C 1-6烷基）氨基C 1-6烷基，芳基或杂芳基; 每个R 2独立地代表卤素，C 1-6烷基，C 1-6烷氧基，C 1-6 烷硫基，多卤C 1-6烷基，多卤C 1-6烷氧基，氰基，氨基羰基，氨基，单或二（C 1-4） 烷基）氨基，硝基，芳基或芳氧基; R 3表示氢，氰基，任选取代的C 1-6烷基，C（-O）-OR 5，C（O） -NR 6 C 6b，C（-S）-NR 6a R 6b，S（-O） C 1 -C 6烷基或C（-O）-R 7; R 4表示氢或C 1-6烷基; n为1,2,3,4或5; Z表示环状体系。 本发明还涉及制备式（I）化合物的方法，它们作为CCR2拮抗剂的用途和包含它们的药物组合物。

公开(公告)号：US07511068B2

公开(公告)日：2009-03-31

申请号：US10544569

申请日：2004-01-30

申请人： Guy Rosalia Eugeen Van Lommen ,  Julien Georges Pierre-Olivier Doyon ,  Jean Pierre Frans Van Wauwe ,  Marina Lucie Louise Cools ,  Erwin Coesemans

发明人： Guy Rosalia Eugeen Van Lommen ,  Julien Georges Pierre-Olivier Doyon ,  Jean Pierre Frans Van Wauwe ,  Marina Lucie Louise Cools ,  Erwin Coesemans

IPC分类号： A61K31/4164 ,  C07D233/04

CPC分类号： A61K31/4174 ,  A61K31/4178 ,  A61K31/5025 ,  C07D233/84 ,  C07D233/90 ,  C07D263/44 ,  C07D409/06 ,  C07D487/04

摘要： The present invention relates to a compound of formula (I) having CCR2 receptor antagonistic properties, particularly anti-inflammatory properties.

摘要翻译： 本发明涉及具有CCR2受体拮抗性质，特别是抗炎性质的式（I）化合物。

公开(公告)号：US07232838B2

公开(公告)日：2007-06-19

申请号：US10486819

申请日：2002-08-09

申请人： Christopher John Love ,  Guy Rosalia Eugeen Van Lommen ,  Julien Georges Pierre-Olivier Doyon ,  Jean-Pierre André Marc Bongartz ,  Marcel Jozef Maria Van der AA ,  Robert Jozef Maria Hendrickx ,  Peter Jacobus Johannes Antonius Buijnsters ,  Ludwig Paul Cooymans ,  Nele Vandermaesen ,  Erwin Coesemans ,  Gustaaf Maria Boeckx

发明人： Christopher John Love ,  Guy Rosalia Eugeen Van Lommen ,  Julien Georges Pierre-Olivier Doyon ,  Jean-Pierre André Marc Bongartz ,  Marcel Jozef Maria Van der AA ,  Robert Jozef Maria Hendrickx ,  Peter Jacobus Johannes Antonius Buijnsters ,  Ludwig Paul Cooymans ,  Nele Vandermaesen ,  Erwin Coesemans ,  Gustaaf Maria Boeckx

IPC分类号： A61K31/425 ,  C07D277/00 ,  C07D277/20

CPC分类号： C07D417/04 ,  C07D277/42 ,  C07D471/04

摘要： This invention concerns the use of a compound of formula (I′), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is halo; C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxy -carbonyl; aminocarbonyl; C1-6alkyl substituted with hydroxy, carboxyl, cyano, amino, amino substituted with piperidinyl, amino substituted with C1-4alkyl substituted piperidinyl, mono- or di(C1-6alkyl)amino, aminocarbonyl, mono- or di(C1-6alkyl)aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkyloxy, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl; polyhaloC1-4alkyl; cyano; amino; mono- or di(C1-6alkyl)aminocarbonyl; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; aminoS(═O)2—; mono- or di(C1-6alkyl)aminoS(═O)2; —C(═N—Rx)NRyRz; Q is optionally substituted C3-6cycloalkyl, phenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzthiazolyl, benzoxazolyl, benzimidazolyl, indazolyl, or imidazopyridyl, or Q is a radical of formula (b-1), (b-2), or (b-3), L is optionally substituted phenyl or an optionally substituted monocyclic 5 or 6-membered partially saturated or aromatic heterocycle or a bicyclic partially saturated or aromatic heterocycle; aryl is optionally substituted phenyl; for the manufacture of a medicament for the prevention or the treatment of inflammatory and/or auto-immune diseases mediated through TNF-α and/or IL-12

摘要翻译： 本发明涉及式（I'）化合物，N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构体形式的用途，其中Z是卤素; C 1-6烷基; C 1-6烷基羰基; C 1-6烷氧基羰基; 氨基羰基; 用羟基，羧基，氰基，氨基，被哌啶取代的氨基，被C 1-4烷基取代的哌啶基取代的氨基，单或二（ C 1-6烷基）氨基，氨基羰基，一或二（C 1-6烷基）氨基羰基，C 1-6烷氧基羰基， C 1-6烷基氧基，哌啶基，哌嗪基，吗啉基，硫代吗啉基; 多卤代1-4烷基; 氰基; 氨基; 单或二（C 1-6烷基）氨基羰基; C 1-6烷氧基羰基; C 1-6烷基羰基氧基; 氨基-S（-O）2 - ; 单或二（C 1-6烷基）氨基S（-O）2; -C（-N-R x X）NR z R z Z; Q为任选取代的C 3-6环烷基，苯基，吡啶基，嘧啶基，吡嗪基，哒嗪基，苯并噻唑基，苯并恶唑基，苯并咪唑基，吲唑基或咪唑并吡啶基，或Q为式（b-1） ，（b-2）或（b-3）中，L是任选取代的苯基或任选取代的单环5或6元部分饱和或芳族杂环或双环部分饱和或芳族杂环; 芳基是任选取代的苯基; 用于制备用于预防或治疗通过TNF-α和/或IL-12介导的炎症和/或自身免疫疾病的药物