公开(公告)号：US08575342B2

公开(公告)日：2013-11-05

申请号：US11575818

申请日：2005-09-29

申请人： Jerôme Emile Georges Guillemont ,  Jan Heeres ,  Paulus Joannes Lewi

发明人： Jerôme Emile Georges Guillemont ,  Jan Heeres ,  Paulus Joannes Lewi

IPC分类号： C07D239/02 ,  A61K31/505

CPC分类号： C07D405/04 ,  C07D401/04 ,  C07D403/04 ,  C07D409/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

摘要： Compounds of formula (I), N-oxides, pharmaceutical acceptable salts, quaternary amines or stereoisomeric forms thereof, and their use as HIV replication inhibitors, In the formula, -a1=a2-a3=a4- and -b1=b2-b3=b4- may be —C═C—C═C—; X1 may be O, NR1, etc.; R1, R2, R2a, R3, R4 and R5 are assorted substituents as defined in the specification.

摘要翻译： 式（I）的化合物，N-氧化物，药学上可接受的盐，季胺或其立体异构形式及其作为HIV复制抑制剂的用途在式中，-a1 = a2-a3 = a4-和-b1 = b2-b3 = b4-可以是-C = CC = C-; X1可以是O，NR1等; R1，R2，R2a，R3，R4和R5是说明书中定义的各种取代基。

公开(公告)号：US08318736B2

公开(公告)日：2012-11-27

申请号：US12521379

申请日：2007-12-28

申请人： Jerôme Emile Georges Guillemont ,  Céline Isabelle Mordant ,  Benoit Antoine Schmitt

发明人： Jerôme Emile Georges Guillemont ,  Céline Isabelle Mordant ,  Benoit Antoine Schmitt

IPC分类号： A61K31/535 ,  A61K31/497 ,  A61K31/505 ,  C07D239/02 ,  C07D401/08 ,  C07D413/08

CPC分类号： C07D239/48 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D417/06

摘要： HIV replication inhibitors of formula wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and X have specific definitions, and pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds and compositions.

摘要翻译： 具有下式的HIV复制抑制剂其中R1，R2，R3，R4，R5，R6，R7，R8，R9和X具有特定定义，以及含有这些化合物作为活性成分的药物组合物和制备所述化合物和组合物的方法。

公开(公告)号：US20110124673A1

公开(公告)日：2011-05-26

申请号：US12950345

申请日：2010-11-19

申请人： Dominique Jean-Pierre Mabire ,  Jerôme Emile Georges Guillemont ,  Jacobus Alphonsus Josephus Van Dun ,  Maria Victorina Francisca Somers ,  Walter Boudewijn Leopold Wouters

发明人： Dominique Jean-Pierre Mabire ,  Jerôme Emile Georges Guillemont ,  Jacobus Alphonsus Josephus Van Dun ,  Maria Victorina Francisca Somers ,  Walter Boudewijn Leopold Wouters

IPC分类号： A61K31/473 ,  C07D405/14 ,  C07D401/12 ,  C07D221/12 ,  A61P35/00 ,  A61P25/00 ,  A61P25/28 ,  A61P25/02 ,  A61P29/00 ,  A61P19/02 ,  A61P3/10 ,  A61P9/10

CPC分类号： C07D215/227 ,  C07D241/44 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/06 ,  C07D405/06 ,  C07D405/10 ,  C07D405/14 ,  C07D407/06 ,  C07D409/12

摘要： The present invention provides compounds of formula (I) and compounds of formula (VII-a) as well as pharmaceutical compositions comprising said compounds and their use as PARP inhibitors wherein n, R1, R2, R3, R4, R5, R6, R7, Re, Rd and X have defined meanings.

摘要翻译： 本发明提供式（I）化合物和式（VII-a）化合物以及包含所述化合物及其用作PARP抑制剂的药物组合物，其中n，R1，R2，R3，R4，R5，R6，R7， Re，Rd和X定义含义。

公开(公告)号：US20100016317A1

公开(公告)日：2010-01-21

申请号：US12521189

申请日：2007-12-28

申请人： Jerôme Emile Georges Guillemont ,  Celine Isabelle Mordant

发明人： Jerôme Emile Georges Guillemont ,  Celine Isabelle Mordant

IPC分类号： A61K31/5377 ,  C07D239/02 ,  A61K31/505 ,  C07D413/00

CPC分类号： C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D403/06 ,  C07D405/12 ,  C07D409/12 ,  C07D417/06

摘要： HIV replication inhibitors of formula R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2, R3, R6 and R7 are hydrogen; hydroxy; halo; C3-7cycloalkyl; C1-6alkyloxy; carboxyl; C1-6alkyloxycarbonyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; —C(═O)R9; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R4 and R5 are hydroxy; halo; C3-7cycloalkyl; C1-6alkyloxy; carboxyl; C1-6alkyloxycarbonyl; formyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; —C(═O)R9; cyano; —S(═O)rR9; —NH—S(═O)2R9; —NHC(═O)H; —C(═O)NHNH2; —NHC(═O)R9; Het; —Y-Het; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R5 is pyridyl, —C(═O)NR5aR5b; —CH(OR5c)R5d; —CH2—NR5eR5f; —CH═NOR5a; —CH2—O—C2-6alkenyl; —CH2—O—P(═O)(OR5g)2; —CH2—O—C(═O)—NH2; —C(═O)—R5d; X is —NR1—, —O—, —CH2—, —S—; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds and compositions.

摘要翻译： 式R1的HIV复制抑制剂是氢; 芳基; 甲酰基 C 1-6烷基羰基; C 1-6烷基; C 1-6烷氧基羰基; R2，R3，R6和R7是氢; 羟基; 光环; C 3-7环烷基; C 1-6烷氧基; 羧基; C 1-6烷氧基羰基; 氰基; 硝基 氨基; 单或二（C 1-6烷基）氨基; 多卤代C 1-6烷基; 多卤代C 1-6烷氧基; -C（-O）R 9; 任选取代的C 1-6烷基，C 2-6烯基或C 2-6炔基; R4和R5是羟基; 光环; C 3-7环烷基; C 1-6烷氧基; 羧基; C 1-6烷氧基羰基; 甲酰基 氰基; 硝基 氨基; 单或二（C 1-6烷基）氨基; 多卤代C 1-6烷基; 多卤代C 1-6烷氧基; -C（-O）R 9; 氰基; -S（-O）r R 9; -NH-S（-O）2 R 9; -NHC（-O）H; -C（-O）NHNH 2; -NHC（-O）R 9; Het; -Y-Het; 任选取代的C 1-6烷基，C 2-6烯基或C 2-6炔基; R5是吡啶基，-C（-O）NR5aR5b; -CH（OR 5 c）R 5d; -CH2-NR5eR5f; -CH-NOR5a; -CH 2 -O-C 2-6烯基; -CH 2 -O-P（-O）（OR 5 g）2; -CH 2 -O-C（-O）-NH 2; -C（-O）-R5d; X是-NR 1 - ， - O - ， - CH 2 - ， - S- 含有这些化合物作为活性成分的药物组合物和制备所述化合物和组合物的方法。

公开(公告)号：US09487518B2

公开(公告)日：2016-11-08

申请号：US13410779

申请日：2012-03-02

申请人： Jerôme Emile Georges Guillemont ,  Mikaël Paugam ,  Bruno Francois Marie Delest ,  Jan Heeres ,  Paulus Joannes Lewi ,  Paul Adriaan Jan Janssen ,  Frank Xavier Jozef Herwig Arts

发明人： Jerôme Emile Georges Guillemont ,  Mikaël Paugam ,  Bruno Francois Marie Delest ,  Jan Heeres ,  Paulus Joannes Lewi ,  Paul Adriaan Jan Janssen

IPC分类号： C07D487/04 ,  A61K31/519 ,  C07D473/00 ,  C07D473/34 ,  A61P31/18 ,  A61K31/52

CPC分类号： C07D487/04 ,  C07D473/00 ,  C07D473/16 ,  C07D473/24 ,  C07D473/34

摘要： HIV replication inhibitors of formula wherein -a1=a2-a3=a4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; -b1=b2-b3=b4- is —CH═CH—CH═CH—, —N═CH—CH═CH—, —N═CH—N═CH—, —N═CH—CH═N—, —N═N—CH═CH—; n and m is 0-4, R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; polyhalomethyl; polyhalomethylthio; —S(═O)pR6; C(═NH)R6; R2a is CN; amino; substituted amino; C1-6alkyl; halo; C1-6alkyloxy; carbonyl; —CH═N—NH—C(═O)—R16; C1-6alkyloxyC1-6alkyl; C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7 or —X—R7; R3 is CN; amino; C1-6alkyl; halo; C1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R16; substituted C1-6alkyl; C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4alkyl; R7; —X—R7; R4 is halo; OH; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; CN; nitro; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; substituted carbonyl; formyl; amino; mono- or di(C1-4alkyl)amino or R7; -A-B— is —CR5═N—, —N═N—, —CH2—CH2—, —CS—NH—, —CO—NH—, —CH═CH—; and the use of these compounds for the prevention or the treatment of HIV infection.

公开(公告)号：US09394295B2

公开(公告)日：2016-07-19

申请号：US14237841

申请日：2012-08-10

申请人： Jerôme Emile Georges Guillemont ,  David Francis Alain Lançois ,  Magali Madeleine Simone Motte ,  Anil Koul ,  Wendy Mia Albert Balemans

发明人： Jerôme Emile Georges Guillemont ,  David Francis Alain Lançois ,  Magali Madeleine Simone Motte ,  Anil Koul ,  Wendy Mia Albert Balemans

IPC分类号： A61K31/55 ,  A61K31/551 ,  C07D471/04

CPC分类号： C07D471/04

摘要： The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.

摘要翻译： 本发明涉及抑制因此可用于治疗细菌感染的FabI酶的活性的式（I）化合物。 它还涉及包含这些化合物的药物组合物和用于制备这些化合物的化学方法。

公开(公告)号：US09012634B2

公开(公告)日：2015-04-21

申请号：US14237851

申请日：2012-08-10

申请人： Jerôme Emile Georges Guillemont ,  David Francis Alain Lançois ,  Magali Madeleine Simone Motte ,  Anil Koul ,  Wendy Mia Albert Balemans

发明人： Jerôme Emile Georges Guillemont ,  David Francis Alain Lançois ,  Magali Madeleine Simone Motte ,  Anil Koul ,  Wendy Mia Albert Balemans

IPC分类号： A61K31/4375 ,  C07D515/04 ,  C07D471/04

CPC分类号： C07D471/04

摘要： The present invention is related to novel compounds of formula (I) that inhibit the activity of the Fab1 enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.

摘要翻译： 本发明涉及抑制Fab1酶活性的新型式（I）化合物，因此可用于治疗细菌感染。 它还涉及包含这些化合物的药物组合物和用于制备这些化合物的化学方法。

公开(公告)号：US09006243B2

公开(公告)日：2015-04-14

申请号：US12521189

申请日：2007-12-28

申请人： Jerôme Emile Georges Guillemont ,  Céline Isabelle Mordant

发明人： Jerôme Emile Georges Guillemont ,  Céline Isabelle Mordant

IPC分类号： C07D239/48 ,  A61K31/506 ,  C07D401/04 ,  C07D401/12 ,  C07D403/06 ,  C07D405/12 ,  C07D409/12 ,  C07D417/06

CPC分类号： C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D403/06 ,  C07D405/12 ,  C07D409/12 ,  C07D417/06

摘要： HIV replication inhibitors of formula R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2, R3, R6 and R7 are hydrogen; hydroxy; halo; C3-7cycloalkyl; C1-6alkyloxy; carboxyl; C1-6alkyloxycarbonyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; —C(═O)R9; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R4 and R5 are hydroxy; halo; C3-7cycloalkyl; C1-6alkyloxy; carboxyl; C1-6alkyloxycarbonyl; formyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; —C(═O)R9; cyano; —S(═O)rR9; —NH—S(═O)2R9; —NHC(═O)H; —C(═O)NHNH2; —NHC(═O)R9; Het; —Y-Het; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R5 is pyridyl, —C(═O)NR5aR5b; —CH(OR5c)R5d; —CH2—NR5eR5f; —CH═NOR5a; —CH2—O—C2-6alkenyl; —CH2—O—P(═O)(OR5g)2; —CH2—O—C(═O)—NH2; —C(═O)—R5d; X is —NR1—, —O—, —CH2—, —S—; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds and compositions.

摘要翻译： 式R1的HIV复制抑制剂是氢; 芳基; 甲酰基 C 1-6烷基羰基; C 1-6烷基; C 1-6烷氧基羰基; R2，R3，R6和R7是氢; 羟基; 光环; C 3-7环烷基; C 1-6烷氧基; 羧基; C 1-6烷氧基羰基; 氰基; 硝基 氨基; 单或二（C 1-6烷基）氨基; 多卤代C 1-6烷基; 多卤代C 1-6烷氧基; -C（= O）R 9; 任选取代的C 1-6烷基，C 2-6烯基或C 2-6炔基; R4和R5是羟基; 光环; C 3-7环烷基; C 1-6烷氧基; 羧基; C 1-6烷氧基羰基; 甲酰基 氰基; 硝基 氨基; 单或二（C 1-6烷基）氨基; 多卤代C 1-6烷基; 多卤代C 1-6烷氧基; -C（= O）R 9; 氰基; -S（= O）r R 9; -NH-S（= O）2 R 9; -NHC（= O）H; -C（= O）NHNH 2; -NHC（= O）R 9; Het; -Y-Het; 任选取代的C 1-6烷基，C 2-6烯基或C 2-6炔基; R5是吡啶基，-C（= O）NR5aR5b; -CH（OR 5 c）R 5d; -CH2-NR5eR5f; -CH=NOR5a; -CH 2 -O-C 2-6烯基; -CH 2 -O-P（= O）（OR 5 g）2; -CH 2 -O-C（= O）-NH 2; -C（= O）-R5d; X是-NR 1 - ， - O - ， - CH 2 - ， - S- 含有这些化合物作为活性成分的药物组合物和制备所述化合物和组合物的方法。

公开(公告)号：US08946248B2

公开(公告)日：2015-02-03

申请号：US11576315

申请日：2005-09-29

申请人： Jerôme Emile Georges Guillemont ,  Jan Heeres ,  Paulus Joannes Lewi

发明人： Jerôme Emile Georges Guillemont ,  Jan Heeres ,  Paulus Joannes Lewi

IPC分类号： C07D239/48 ,  A61K31/505 ,  C07D239/50

CPC分类号： C07D239/48 ,  C07D239/50

摘要： HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein A is —CH2—CH2—, —CH═CH—, —C≡C—; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, R2 hydroxy, halo, C1-6alkyl, carboxyl, cyano, —C(═O)R6, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl; X1 is —NR1—, —O—, —S—, —S(═O)p—; R3 is H, C1-6alkyl, halo; R4 is H, C1-6alkyl, halo; R5 is nitro, amino, mono- and diC1-4alkylamino, aryl, halo, —CHO, —CO—R6, —COOR7, —NH—C(═O)H, —NH—C(═O)R6, —CH═N—O—R8; R6 is C1-4alkyl, amino, mono- or di(C1-4alkyl)amino or polyhaloC1-4alkyl; R7 is hydrogen, C1-6alkyl, arylC1-6alkyl; R8 is hydrogen, C1-6alkyl, aryl; p is 1 or 2; aryl is optionally substituted phenyl; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds and compositions.

摘要翻译： 其中A是-CH 2 -CH 2 - ， - CH = CH - ， - C≡C-;其中A是-CH 2 -CH 2 - ， - CH = CH - ， - C≡C-; R1是氢，芳基，甲酰基，C1-6烷基羰基，C1-6烷基，C1-6烷氧基羰基，R2羟基，卤素，C1-6烷基，羧基，氰基，-C（= O）R6，硝基，氨基，单或二 C 1-6烷基）氨基，多卤甲基; X 1是-NR 1 - ， - O - ， - S - ， - S（= O）p - ; R 3是H，C 1-6烷基，卤素; R4是H，C1-6烷基，卤素; R 5是硝基，氨基，单和二C 1-4烷基氨基，芳基，卤素，-CHO，-CO-R 6，-COOR 7，-NH-C（= O）H，-NH-C（= = N-O-R8; R 6是C 1-4烷基，氨基，单或二（C 1-4烷基）氨基或多卤代C 1-4烷基; R 7是氢，C 1-6烷基，芳基C 1-6烷基; R8是氢，C1-6烷基，芳基; p为1或2; 芳基是任选取代的苯基; 含有这些化合物作为活性成分的药物组合物及其制备方法。

公开(公告)号：US08933089B2

公开(公告)日：2015-01-13

申请号：US12294692

申请日：2007-03-30

申请人： Jerôme Emile Georges Guillemont ,  Mikaël Paugam ,  Bruno François Marie Delest

发明人： Jerôme Emile Georges Guillemont ,  Mikaël Paugam ,  Bruno François Marie Delest

IPC分类号： A61K31/515 ,  C07D239/02 ,  C07D239/48 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

CPC分类号： C07D417/12 ,  C07D239/48 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12

摘要： This invention concerns pyrimidine derivatives of formula having HIV (Human Immunodeficiency Virus) replication inhibiting properties, the preparation thereof and pharmaceutical compositions comprising these compounds.

摘要翻译： 本发明涉及具有HIV（人类免疫缺陷病毒）复制抑制性质的式的嘧啶衍生物，其制备方法和包含这些化合物的药物组合物。