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1. 发明授权

US07956063B2 Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile 有权
标题翻译： 4 - [[4 - [[4-（2-氰基乙烯基）-2,6-二甲基苯基]氨基] -2-嘧啶基]氨基]苄腈
公开(公告)号：US07956063B2
公开(公告)日：2011-06-07
申请号：US12168540
申请日：2008-07-07
申请人： Jérôme Emile Georges Guillemont , Paul Theodoor Agnes Stevens , Alex Herman Copmans , Jozef Peeters , Alfred Elisabeth Stappers , Roger Petrus Gerebern Vandecruys , Paul Stoffels
发明人： Jérôme Emile Georges Guillemont , Paul Theodoor Agnes Stevens , Alex Herman Copmans , Jozef Peeters , Alfred Elisabeth Stappers , Roger Petrus Gerebern Vandecruys , Paul Stoffels
IPC分类号： A61K31/505 , A61P31/18 , C07D239/48
CPC分类号： A61K31/505 , C07D239/48
摘要： The present invention relates to a pharmaceutical composition comprising as active ingredient the hydrochloric acid salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethyl-phenyl]amino]-2-pyrimidinyl]amino]benzonitrile and to processes for their preparation.
摘要翻译：本发明涉及药物组合物，其包含4 - [[4 - [[4-（2-氰基乙烯基）-2,6-二甲基 - 苯基]氨基] -2-嘧啶基]氨基] 苄腈和其制备方法。

2. 发明授权

US07638522B2 Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino] benzonitrile 有权
标题翻译： 4 - [[4 - [[4-（2-氰基乙烯基）-2,6-二甲基苯基]氨基] -2-嘧啶基]氨基]苄腈
公开(公告)号：US07638522B2
公开(公告)日：2009-12-29
申请号：US11219163
申请日：2005-09-02
申请人： Jérôme Emile Georges Guillemont , Paul Theodoor Agnes Stevens , Alex Herman Copmans , Jozef Peeters , Alfred Elisabeth Stappers , Roger Petrus Gerebern Vandecruys , Paul Stoffels
发明人： Jérôme Emile Georges Guillemont , Paul Theodoor Agnes Stevens , Alex Herman Copmans , Jozef Peeters , Alfred Elisabeth Stappers , Roger Petrus Gerebern Vandecruys , Paul Stoffels
IPC分类号： A61K31/505 , C07D239/48 , A61P31/18
CPC分类号： A61K31/505 , C07D239/48
摘要： The present invention relates to a pharmaceutical composition comprising as active ingredient the hydrochloric acid salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethyl-phenyl]amino]-2-pyrimidinyl]amino]benzonitrile and to processes for their preparation.
摘要翻译：本发明涉及药物组合物，其包含4 - [[4 - [[4-（2-氰基乙烯基）-2,6-二甲基 - 苯基]氨基] -2-嘧啶基]氨基] 苄腈和其制备方法。

3. 发明授权

US08101629B2 Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile 有权
标题翻译： 4 - [[4 - [[4-（2-氰基乙烯基）-2,6-二甲基苯基]氨基] -2-嘧啶基]氨基]苄腈
公开(公告)号：US08101629B2
公开(公告)日：2012-01-24
申请号：US12845463
申请日：2010-07-28
申请人： Jérôme Emile Georges Guillemont , Paul Theodoor Agnes Stevens , Alex Herman Copmans , Jozef Peeters , Alfred Elisabeth Stappers , Roger Petrus Gerebern Vandecruys , Paul Stoffels
发明人： Jérôme Emile Georges Guillemont , Paul Theodoor Agnes Stevens , Alex Herman Copmans , Jozef Peeters , Alfred Elisabeth Stappers , Roger Petrus Gerebern Vandecruys , Paul Stoffels
IPC分类号： A61K31/505 , C07D239/48 , A61P31/18
CPC分类号： A61K31/505 , A61K9/2018 , A61K9/2866 , C07D239/48
摘要： The present invention relates to a pharmaceutical composition comprising as active ingredient the hydrochloric acid salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethyl-phenyl]amino]-2-pyrimidinyl]amino]benzonitrile and to processes for their preparation.
摘要翻译：本发明涉及药物组合物，其包含4 - [[4 - [[4-（2-氰基乙烯基）-2,6-二甲基 - 苯基]氨基] -2-嘧啶基]氨基] 苄腈和其制备方法。

4. 发明授权

US07879857B2 6-substituted 2-quinolinones and 2-quinoxalinones as poly (adp-ribose) polymerase inhibitors 有权
标题翻译： 6-取代的2-喹啉酮和2-喹喔啉酮作为聚（adp-核糖）聚合酶抑制剂
公开(公告)号：US07879857B2
公开(公告)日：2011-02-01
申请号：US10596086
申请日：2004-11-18
申请人： Dominique Jean-Pierre Mabire , Jérôme Emile Georges Guillemont , Jacobus Alphonsus Josephus Van Dun , Maria Victorina Francisca Somers , Walter Boudewijn Leopold Wouters
发明人： Dominique Jean-Pierre Mabire , Jérôme Emile Georges Guillemont , Jacobus Alphonsus Josephus Van Dun , Maria Victorina Francisca Somers , Walter Boudewijn Leopold Wouters
IPC分类号： C07D241/44 , C07D215/227 , A61K31/498 , A61K31/4704 , A61P25/28
CPC分类号： C04B35/632 , C07D241/44 , C07D401/12 , C07D407/06 , C07D409/14
摘要： The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, R1, R2, R3, R4 and X have defined meanings.
摘要翻译：本发明提供式（I）化合物，它们作为PARP抑制剂的用途以及包含所述式（I）化合物的药物组合物，其中n，R1，R2，R3，R4和X具有定义的含义。

5. 发明申请

US20100204270A1 Quinoline Derivatives as Antibacterial Agents 审中-公开
标题翻译：喹啉衍生物作为抗菌剂
公开(公告)号：US20100204270A1
公开(公告)日：2010-08-12
申请号：US11917923
申请日：2006-06-26
申请人： Koenraad Jozef Lodewijk Marcel Andries , Anil Koul , Jérôme Emile Georges Guillemont , Magali Madeleine Simone Motte
发明人： Koenraad Jozef Lodewijk Marcel Andries , Anil Koul , Jérôme Emile Georges Guillemont , Magali Madeleine Simone Motte
IPC分类号： A61K31/47 , C07D215/16 , A61P31/04
CPC分类号： C07D215/227 , A61K31/4353 , A61K45/06 , C07D215/36 , A61K2300/00
摘要： Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of formula (Ia) or (Ib) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, a tautomeric form thereof or a N-oxide form thereof. Several of these compounds are also claimed as such. Further the combination of the above compounds with other antibacterial agents is described
摘要翻译：使用化合物制造用于治疗细菌感染的药物，只要细菌感染不是分枝杆菌感染，所述化合物是式（Ia）或（Ib）的化合物，其药学上可接受的酸或碱加成其盐，其立体化学异构形式，其互变异构形式或其N-氧化物形式。这些化合物中的几种也是这样声称的。此外，还描述了上述化合物与其它抗菌剂的组合

6. 发明授权

US07709498B2 Quinoline derivatives as antibacterial agents 有权
标题翻译：喹啉衍生物作为抗菌剂
公开(公告)号：US07709498B2
公开(公告)日：2010-05-04
申请号：US11296918
申请日：2005-12-08
申请人： Koenraad Jozef Lodewijk Marcel Andries , Anil Koul , Jérôme Emile Georges Guillemont , Elisabeth Therese Jeanne Pasquier
发明人： Koenraad Jozef Lodewijk Marcel Andries , Anil Koul , Jérôme Emile Georges Guillemont , Elisabeth Therese Jeanne Pasquier
IPC分类号： C07D215/38
CPC分类号： C07D215/227 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/541 , C07D215/36 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/06 , C07D409/06 , Y02A50/473
摘要： The present invention relates to a method for the treatment of a bacterial infection comprising administering a therapeutically effective amount of a compound of formula or a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof or a N-oxide form thereof, wherein R1 is hydrogen, halo, polyhaloC1-6alkyl, C1-6alkyl, Ar or Het; p is an integer equal to 1 or 2; R2 is C1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy or C1-6alkylthio; R3 is Ar, Het or Het1; R4 and R5 each independently are hydrogen, C1-6alkyl or benzyl; or R4 and R5 together and including the N to which they are attached may form a radical selected from the group of pyrrolidinyl, 2-pyrrolinyl, 3-pyrrolinyl, pyrrolyl, imidazolidinyl, pyrazolidinyl, 2-imidazolinyl, 2-pyrazolinyl, imidazolyl, pyrazolyl, triazolyl, piperidinyl, pyridinyl, piperazinyl, pyridazinyl, pyrimidinyl, pyrazinyl, triazinyl, morpholinyl and thiomorpholinyl, each of said rings may optionally be substituted with C1-6alkyl, halo, polyhaloC1-6alkyl, hydroxy, hydroxyC1-6alkyl, C1-6alkyloxy, amino, mono- or di(C1-6alkyl)amino, C1-6alkylthio, C1-6alkyloxyC1-6alkyl, C1-6alkylthioC1-6alkyl or pyrimidinyl; R6 is hydrogen, halo, polyhaloC1-6alkyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio; or two vicinal R6 radicals may be taken together to form a bivalent radical of formula —CH═CH—CH═CH—; r is an integer equal to 1 or 2; R7 is hydrogen, C1-6alkyl, Ar, Het or Het1; provided that to bacterial infection is other than a Mycobacterial infection.
摘要翻译：本发明涉及一种治疗细菌感染的方法，包括给予治疗有效量的式的化合物或其药学上可接受的酸或碱加成盐，其立体化学异构形式或其N-氧化物形式，其中 R 1是氢，卤素，多卤代C 1-6烷基，C 1-6烷基，Ar或Het; p是等于1或2的整数; R2是C1-6烷氧基，C1-6烷氧基C1-6烷氧基或C1-6烷硫基; R3是Ar，Het或Het1; R 4和R 5各自独立地为氢，C 1-6烷基或苄基; 或R4和R5一起并且包括它们所连接的N可以形成选自吡咯烷基，2-吡咯啉基，3-吡咯啉基，吡咯基，咪唑烷基，吡唑烷基，2-咪唑啉基，2-吡唑啉基，咪唑基，吡唑基三唑基，哌啶基，吡啶基，哌嗪基，哒嗪基，嘧啶基，吡嗪基，三嗪基，吗啉基和硫代吗啉基，每个所述环可任选被C 1-6烷基，卤素，多卤代C 1-6烷基，羟基，羟基C 1-6烷基，C 1-6烷氧基，氨基，单或二（C 1-6烷基）氨基，C 1-6烷硫基，C 1-6烷氧基C 1-6烷基，C 1-6烷硫基C 1-6烷基或嘧啶基; R 6是氢，卤素，多卤代C 1-6烷基，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基; 或两个连位的R6基团可以一起形成式-CH = CH-CH = CH-的二价基团; r是等于1或2的整数; R7是氢，C1-6烷基，Ar，Het或Het1; 只要细菌感染不是分枝杆菌感染。

7. 发明授权

US07071192B1 Respiratory syncytial virus replication inhibitors 失效
公开(公告)号：US07071192B1
公开(公告)日：2006-07-04
申请号：US10019376
申请日：2000-06-20
申请人： Frans Eduard Janssens , Jean Fernand Armand Lacrampe , Jérôme Emile Georges Guillemont , Marc Gaston Venet , Koenraad Jozef Lodewijk Marcel Andries
发明人： Frans Eduard Janssens , Jean Fernand Armand Lacrampe , Jérôme Emile Georges Guillemont , Marc Gaston Venet , Koenraad Jozef Lodewijk Marcel Andries
IPC分类号： A61P31/00 , A61K31/495 , A61K31/445 , C07D239/00 , C07D215/00
CPC分类号： C07D401/14 , C07D409/14 , C07D471/04 , Y02P20/55
摘要： The present invention concerns compounds of formula (I), prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof wherein -a1=a2-a3=a4-represents a radical of formula —CH═CH—CH═CH—; —N—CH—CH═CH—; —CH═N—CH═CH—; —CH═CH—N═CH—; —CH═CH—CH═N—; wherein each hydrogen atom may optionally be substituted; Q is a radical of formulae (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), wherein Alk is C1-6alkanediyl; Y1 is a bivalent radical of formula —NR2— or —CH(NR2R4)—; X1 is NR4, S, S(═O), S(═O)2, O, CH2, C(═O), CH(═CH2), CH(OH), CH(CH3), CH(OCH3), CH(SCH3), CH(NR5aR5b), CH2—NR4 or NR4—CH2; X2 is a direct bond, CH2, C(═O), NR4, C1-4alkyl-NR4, NR4—C1-4alkyl, t is 2 to 5; u is 1 to 5; v is 2 or 3; and whereby each hydrogen in Alk and in (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), may optionally be replaced by R3: provided that when R3 is hydroxy or C1-6alkyloxy, then R3 cannot replace a hydrogen atom in the a position relative to a nitrogen atom; G is a direct bond or optionally substituted C1-10alkanediyl; R1 is an optionally substituted bicyclic heterocycle; R2 is hydrogen, formyl, C1-6alkylcarbonyl, Hetcarbonyl, pyrrolidinyl, piperidinyl, homopiperidinyl, C3-7cycloalkyl or C1-10alkyl substituted with N(R6)2 and optionally with another substituent; R3 is hydrogen, hydroxy, C1-6alkyl, C1-6alkyloxy, aryl C1-6alkyl or aryl C1-6alkyloxy, R4 is hydrogen, C1-6alkyl or aryl C1-6alkyl; R5a, R5b, R5c and R5d are hydrogen or C1-6alkyl; or R5a and R5b, or R5c and R5d taken together from a bivalent radical of formula —(CH2)5- wherein S is 4 or 5; R6 is hydrogen, C1-4alkyl, formyl, hydroxy C1-6alkyl, C1-6alkylcarbonyl or C1-6alkyloxycarbonyl; aryl is optionally substituted phenyl; Het is pyridyl, pyrimidinyl, pyridazinyl, pyridazinyl; as respiratory syncytial virus replication inhibitors; their preparation, compositions containing them and their use as a medicine.

8. 发明申请

US20130030017A1 QUINOLINE DERIVATIVES AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译：喹诺酮衍生物作为抗菌剂
公开(公告)号：US20130030017A1
公开(公告)日：2013-01-31
申请号：US13568597
申请日：2012-08-07
申请人： Koenraad Jozef Lodewijk Marcel ANDRIES , Anil Koul , Jérôme Emile Georges Guillemont , Magali Madeleine Simone Motte
发明人： Koenraad Jozef Lodewijk Marcel ANDRIES , Anil Koul , Jérôme Emile Georges Guillemont , Magali Madeleine Simone Motte
IPC分类号： A61K31/47 , A61P31/04
CPC分类号： C07D215/227 , A61K31/4353 , A61K45/06 , C07D215/36 , A61K2300/00
摘要： Method of treating a bacterial infection other than a Mycobacterial infection, using a compound of formula (Ia) or (Ib) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, a tautomeric form thereof or a N-oxide form thereof, wherein the substituents R1, R2, R3, R4, R5, R6, R7, R8, and R9 are as defined.
摘要翻译：使用式（Ia）或（Ib）化合物或其药学上可接受的酸或碱加成盐，其立体化学异构形式，其互变异构形式或N-氧化物形式治疗除分枝杆菌感染之外的细菌感染的方法其中取代基R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8和R 9如上所定义。

9. 发明授权

US08080551B2 HIV inhibiting pyrimidines derivatives 有权
标题翻译： HIV抑制嘧啶衍生物
公开(公告)号：US08080551B2
公开(公告)日：2011-12-20
申请号：US11474855
申请日：2006-06-26
申请人： Jérôme Emile Georges Guillemont , Patrice Palandijian , Marc René De Jonge , Lucien Maria Henricus Koymans , Hendrik Maarten Vinkers , Frederik Frans Desiré Daeyaert , Jan Heeres , Koen Jeanne Alfons Van Aken , Paulus Joannes Lewi , Paul Adriaan Jan Janssen , Frank Xavier Jozef Herwig Arts, legal representative
发明人： Jérôme Emile Georges Guillemont , Patrice Palandijian , Marc René De Jonge , Lucien Maria Henricus Koymans , Hendrik Maarten Vinkers , Frederik Frans Desiré Daeyaert , Jan Heeres , Koen Jeanne Alfons Van Aken , Paulus Joannes Lewi , Paul Adriaan Jan Janssen
IPC分类号： A61K31/501 , A61K31/497 , C07D417/12 , C07D417/14 , C07D417/06 , C07D401/12 , C07D401/14 , C07D401/06 , C07D403/12 , C07D403/14 , C07D403/06 , C07D405/12 , C07D405/14 , C07D405/06 , C07D409/14 , C07D409/12 , C07D409/06 , C07D237/20 , C07F9/02 , C07D413/06 , C07D413/12 , C07D413/14 , C07C257/06 , C07C211/40 , C07C233/03 , C07C235/06 , C07C237/20 , C07C239/08 , C07C229/34 , C07C255/49 , C07C207/02
CPC分类号： C07D239/48 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K45/06 , C07C255/42 , C07C257/12 , C07D239/47 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： HIV replication inhibitors having formula (I) defined herein are disclosed. Pharmaceutical compositions containing the HIV replication inhibitors; the use of the HIV replication inhibitors in the treatment of HIV; and processes for preparing the HIV replication inhibitors are also disclosed.
摘要翻译：公开了具有本文定义的式（I）的HIV复制抑制剂。含有HIV复制抑制剂的药物组合物; 使用HIV复制抑制剂治疗艾滋病毒; 还公开了制备HIV复制抑制剂的方法。

10. 发明授权

US08071612B2 6-alkenyl and 6-phenylalkyl substituted 2-quinolinones and 2-quinoxalinones as poly(ADP-ribose) polymerase inhibitors 有权
标题翻译： 6-烯基和6-苯基烷基取代的2-喹啉酮和2-喹喔啉酮作为聚（ADP-核糖）聚合酶抑制剂
公开(公告)号：US08071612B2
公开(公告)日：2011-12-06
申请号：US12950345
申请日：2010-11-19
申请人： Dominique Jean-Pierre Mabire , Jérôme Emile Georges Guillemont , Jacobus Alphonsus Josephus Van Dun , Maria Victorina Francisca Somers , Walter Boudewijn Leopold Wouters
发明人： Dominique Jean-Pierre Mabire , Jérôme Emile Georges Guillemont , Jacobus Alphonsus Josephus Van Dun , Maria Victorina Francisca Somers , Walter Boudewijn Leopold Wouters
IPC分类号： C07D221/12
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。

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