公开(公告)号：US20080139625A1

公开(公告)日：2008-06-12

申请号：US11632675

申请日：2005-04-29

申请人： Libuse Jaroskova ,  Joannes Theodorus Maria Linders ,  Christophe Francis Robert Nestor Buyck ,  Louis Jozef Elizabeth Van Der Veken ,  Vladimir Dimichev Dimitrov ,  Theo Teofanov Nikiforov

发明人： Libuse Jaroskova ,  Joannes Theodorus Maria Linders ,  Christophe Francis Robert Nestor Buyck ,  Louis Jozef Elizabeth Van Der Veken ,  Vladimir Dimichev Dimitrov ,  Theo Teofanov Nikiforov

IPC分类号： A61K31/4015 ,  C07D207/12 ,  C07D405/10 ,  A61P3/00 ,  A61K31/4412 ,  C07D211/40

CPC分类号： C07D211/76 ,  C07D207/26 ,  C07D207/267 ,  C07D405/06

摘要： Formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl, hydroxy, C1-3alkyloxy- or phenyl-C1-4alkyl; M represents a direct bond or a C1-3alkyl linker optionally substituted with one or two substituents selected from hydroxy, C1-4alkyl or C1-4alkyloxy; R1 and R2 each independently represent hydrogen, halo, cyano, hydroxy, C1-4alkyl optionally substituted with halo, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar1 and halo; or R1 and R2 taken together with the phenyl ring to which they are attached form naphtyl or 1,3-benzodioxolyl, wherein said naphtyl or 1,3-benzodioxolyl are optionally substituted with halo; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R5 represents hydrogen, C1-4alkyl or Ar2-C1-4alky-; R6 represents hydrogen, halo, C1-4alkyl Or C1-4alkyoxy-; Ar1 and Ar2 each independently represent phenyl or naphtyl wherein said phenyl and naphtyl are optionally substituted with C1-4alkyl, C1-4alkyloxy-, or phenyl-C1-4alkyl; for use as a medicine.

公开(公告)号：US09012494B2

公开(公告)日：2015-04-21

申请号：US11632675

申请日：2005-04-29

申请人： Libuse Jaroskova ,  Joannes Theodorus Maria Linders ,  Christophe Francis Robert Nestor Buyck ,  Louis Jozef Elisabeth Van Der Veken ,  Vladimir Dimtchev Dimitrov ,  Theo Teofanov Nikiforov

发明人： Libuse Jaroskova ,  Joannes Theodorus Maria Linders ,  Christophe Francis Robert Nestor Buyck ,  Louis Jozef Elisabeth Van Der Veken ,  Vladimir Dimtchev Dimitrov ,  Theo Teofanov Nikiforov

IPC分类号： A61K31/4015 ,  C07D207/12 ,  C07D207/267 ,  C07D207/26 ,  C07D211/76 ,  C07D405/06

CPC分类号： C07D211/76 ,  C07D207/26 ,  C07D207/267 ,  C07D405/06

摘要： The N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 1 or 2; L represents a C1-3alkyl linker optionally substituted with one or two substituents selected from C1-4alkyl, C1-3alkyloxy-C1-4alkyl-, hydroxy-C1-4alkyl, hydroxy, C1-3alkyloxy- or phenyl-C1-4alkyl; M represents a direct bond or a C1-3alkyl linker optionally substituted with one or two substituents selected from hydroxy, C1-4alkyl or C1-4alkyloxy; R1 and R2 each independently represent hydrogen, halo, cyano, hydroxy, C1-4alkyl optionally substituted with halo, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy, Ar1 and halo; or R1 and R2 taken together with the phenyl ring to which they are attached form naphtyl or 1,3-benzodioxolyl, wherein said naphtyl or 1,3-benzodioxolyl are optionally substituted with halo; R3 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R4 represents hydrogen, halo, C1-4alkyl, C1-4alkyloxy-, cyano or hydroxy; R5 represents hydrogen, C1-4alkyl or Ar2-C1-4alky-; R6 represents hydrogen, halo, C1-4alkyl or C1-4alkyoxy-; Ar1 and Ar2 each independently represent phenyl or naphtyl wherein said phenyl and naphtyl are optionally substituted with C1-4alkyl, C1-4alkyloxy-, or phenyl-C1-4alkyl; for use as a medicine.

摘要翻译： N-氧化物形式，其药学上可接受的加成盐及其立体化学异构形式，其中n为1或2; L表示任选被一个或两个选自C 1-4烷基，C 1-3烷氧基-C 1-4烷基 - ，羟基-C 1-4烷基，羟基，C 1-3烷氧基或苯基-C 1-4烷基的取代基取代的C 1-3烷基接头。 M表示直接键或任选被一个或两个选自羟基，C 1-4烷基或C 1-4烷氧基的取代基取代的C 1-3烷基接头; R 1和R 2各自独立地表示氢，卤素，氰基，羟基，任选被卤素取代的C 1-4烷基，C 1-4烷氧基 - 任选被一个或可能的两个或三个选自羟基，Ar 1和卤素的取代基取代; 或者R 1和R 2与它们所连接的苯环一起形成萘基或1,3-苯并二恶唑基，其中所述萘基或1,3-苯并二恶唑基任选被卤素取代; R 3表示氢，卤素，C 1-4烷基，C 1-4烷氧基 - ，氰基或羟基; R4代表氢，卤素，C1-4烷基，C1-4烷氧基，氰基或羟基; R5表示氢，C1-4烷基或Ar2-C1-4烷基; R 6表示氢，卤素，C 1-4烷基或C 1-4烷氧基 - ; Ar1和Ar2各自独立地表示苯基或萘基，其中所述苯基和萘基任选被C 1-4烷基，C 1-4烷氧基 - 或苯基-C 1-4烷基取代; 用作药物。

公开(公告)号：US07332524B2

公开(公告)日：2008-02-19

申请号：US10540616

申请日：2003-12-16

申请人： Joannes Theodorus Maria Linders ,  Gustaaf Henri Maria Willemsens ,  Ronaldus Arnodus Hendrika Joseph Gilissen ,  Christophe Francis Robert Nestor Buyck ,  Greta Constantia Peter Vanhoof ,  Louis Jozef Elisabeth Van Der Veken ,  Libuse Jaroskova

发明人： Joannes Theodorus Maria Linders ,  Gustaaf Henri Maria Willemsens ,  Ronaldus Arnodus Hendrika Joseph Gilissen ,  Christophe Francis Robert Nestor Buyck ,  Greta Constantia Peter Vanhoof ,  Louis Jozef Elisabeth Van Der Veken ,  Libuse Jaroskova

IPC分类号： A61K31/165 ,  C07C233/57

CPC分类号： C07D207/27 ,  C07C233/11 ,  C07C233/14 ,  C07C233/22 ,  C07C233/23 ,  C07C233/32 ,  C07C233/41 ,  C07C233/58 ,  C07C235/36 ,  C07C235/40 ,  C07C237/20 ,  C07C237/22 ,  C07C255/41 ,  C07C255/57 ,  C07C271/22 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2601/20 ,  C07C2602/06 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2602/12 ,  C07C2602/18 ,  C07C2602/42 ,  C07C2602/46 ,  C07C2603/62 ,  C07C2603/66 ,  C07C2603/70 ,  C07C2603/74 ,  C07D209/08 ,  C07D209/18 ,  C07D213/56 ,  C07D215/08 ,  C07D215/48 ,  C07D217/06 ,  C07D217/26 ,  C07D243/08 ,  C07D257/04 ,  C07D277/40 ,  C07D277/48 ,  C07D295/088 ,  C07D295/155 ,  C07D295/185 ,  C07D309/12 ,  C07D311/58 ,  C07D311/64 ,  C07D317/60 ,  C07D317/72 ,  C07D333/24 ,  C07D333/68 ,  C07D335/06

摘要： the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n represents an integer being 1 or 2; R1 and R2 each independently represents hydrogen C1-4alkyl, NR9R10, C1-4alkyloxy; or R1 and R2 taken together with the carbon atom with which they are attached form a C3-6cycloalkyl; and where n is 2, either R1 or R2 may be absent to form an unsaturated bond; R3 represents a C6-12cycloalkyl, preferably selected from cylo-octanyl and cyclohexyl or R3 represents a monovalent radical having one of the following formulae wherein said C6-12cycloalkyl or monovalent radical may optionally be substituted with one, or where possible two, three or more substituents selected from the group consisting of C1-4alkyl, C1-4alkyloxy, halo or hydroxy; Q represents Het1 or Ar2 wherein said C3-8cycloalkyl, Het1 or Ar2 are optionally substituted with one or where possible two or more substituents selected from halo, C1-4alkyl, C1-4alkyloxy, hydroxy, nitro, NR5R6, C1-4alkyloxy substituted with one or where possible two, three or more substituents each independently selected from hydroxycarbonyl, Het2 and NR7R8, and C1-4alkyl substituted with one or where possible two or three halo substituents, preferably trifluoromethyl; R5 and R6 each independently represent hydrogen, C1-4alkyl, or C1-4alkyl substituted with phenyl; R7 and R8 each independently represent hydrogen or C1-4alkyl; R9 and R10 each independently represent hydrogen, C1-4alkyl or C1-4alkyloxycarbonyl; L represents C1-4alkyl; Het1 represents a heterocycle selected from pyridinyl, thiophenyl, or 1,3-benzodioxolyl; Het2 represents piperidinyl, pyrrolidinyl or morpholinyl; Ar2 represents phenyl, naphtyl or indenyl.

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：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：US08835437B2

公开(公告)日：2014-09-16

申请号：US12663009

申请日：2008-06-05

申请人： Jean-Pierre André Marc Bongartz ,  Lieven Meerpoel ,  Gustaaf Maria Boeckx ,  Guy Rosalia Eugeen Van Lommen ,  Christophe Francis Robert Nestor Buyck ,  Daniel Obrecht ,  Philipp Ermert ,  Anatol Luther

发明人： Jean-Pierre André Marc Bongartz ,  Lieven Meerpoel ,  Gustaaf Maria Boeckx ,  Guy Rosalia Eugeen Van Lommen ,  Christophe Francis Robert Nestor Buyck ,  Daniel Obrecht ,  Philipp Ermert ,  Anatol Luther

IPC分类号： A61K31/496 ,  C07D487/04 ,  C07D513/04 ,  C07D239/42 ,  C07D239/26 ,  A61K31/506 ,  A61K31/454 ,  C07D231/12 ,  C07D249/08 ,  C07D249/12 ,  C07D271/06 ,  C07D401/10

CPC分类号： C07D513/04 ,  C07D231/12 ,  C07D239/26 ,  C07D239/42 ,  C07D249/08 ,  C07D249/12 ,  C07D271/06 ,  C07D271/10 ,  C07D271/107 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D487/04

摘要： The invention further 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 —NRx—C(═O)—; —Z—C(═O)—; —Z—NRx—C(═O)—; —S(═O)p—; C(═S)—; —NRx—C(═S)—; —Z—C(═S)—; —Z—NRx—C(═S)—; —O—C(═O)—; —C(═O)—C(═O)—; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5-or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxlyl, 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-benzo-dioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or 6-membered aromatic heterocycle may optionally be substituted; 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.

摘要翻译： 本发明还涉及式（I）的DGAT抑制剂，其包括其任何立体化学异构形式，其中A表示CH或N; 在A代表碳原子的情况下，虚线代表任意键; X表示-NR x -C（= O） - ; -Z-C（= O） - ; -Z-NRx-C（= O） - ; -S（= O）p-; C（═S） - ; -NR x -C（= S） - ; -Z-C（= S） - ; -Z-NRx-C（= S） - ; -O-C（= O） - ; -C（= O）-C（= O） - ; R1表示含有至少2个杂原子的5元单环杂环; 6元芳族单环杂环; 或含有至少2个与苯基，环己基或5或6元杂环稠合的杂原子的5元杂环; 其中每个所述杂环可任选被取代; R2表示R3; R 3表示C 3-6环烷基，苯基，萘基，2,3-二氢-1,4-苯并二氧杂环己烯基，1,3-苯并二恶唑基，2,3-二氢苯并呋喃基或含1或2个N原子的6元芳族杂环，其中所述C3 6-环烷基，苯基，萘基，2,3-二氢-1,4-苯并二恶基，1,3-苯并二恶唑基，2,3-二氢苯并呋喃基或6-元芳香杂环可以任选被取代; 其N-氧化物，其药学上可接受的盐或其溶剂合物。 本发明还涉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：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：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.