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11. 发明授权

US5266708A New intermediates, process for their preparation, and their use for the synthesis of vitamins A and E 失效
标题翻译：新中间体，其制备方法及其用于合成维生素A和E的用途
公开(公告)号：US5266708A
公开(公告)日：1993-11-30
申请号：US858621
申请日：1992-03-27
申请人： Pierre F. Charbardes , Lucette Duhamel , Pierre Duhamel , Jerome Guillemont , Jean-Marie Poirier
发明人： Pierre F. Charbardes , Lucette Duhamel , Pierre Duhamel , Jerome Guillemont , Jean-Marie Poirier
IPC分类号： C07C45/59 , C07C47/24 , C07D317/20 , C07D319/06 , C07F9/655 , C07D317/18
CPC分类号： C07C403/14 , C07C45/59 , C07C47/24 , C07D317/20 , C07D319/06 , C07F9/65515
摘要： New intermediates and processes for the preparation of vitamins A and E, which are the acetals of 5,6-dihalo-3-methyl-3-hydroxyhexanal or of 6-halo-3-hydroxy-3-methyl-5-hexenal or 3-methyl-3-hydroxy-5-hexenal, as well as processes for making the intermediates. After dehydrohalogenation and dehydration these intermediates are condensed directly with .beta.-ionone or with 2-methyl-2-heptene-6-one to synthesize vitamins A and E respectively.
摘要翻译：用于制备维生素A和E的新中间体和方法，其为5,6-二卤代-3-甲基-3-羟基己醛或6-卤代-3-羟基-3-甲基-5-己烯醛或3 3-甲基-3-羟基-5-己烯醛，以及制备中间体的方法。在脱卤化氢和脱水后，这些中间体直接与β-戊酮或2-甲基-2-庚烯-6-酮缩合以分别合成维生素A和E。

12. 发明授权

US5250710A Dihydropyran derivatives, processes for preparation and use 失效
标题翻译：二氢吡喃衍生物，制备和使用方法
公开(公告)号：US5250710A
公开(公告)日：1993-10-05
申请号：US879335
申请日：1992-05-07
申请人： Pierre F. Chabardes , Lucette Duhamel , Pierre Duhamel , Jerome Guillemont , Jean-Marie Poirier
发明人： Pierre F. Chabardes , Lucette Duhamel , Pierre Duhamel , Jerome Guillemont , Jean-Marie Poirier
IPC分类号： C07C45/60 , C07D309/30 , C07D315/00
CPC分类号： C07C403/14 , C07C45/60 , C07D309/30
摘要： The present invention relates to dihydropyran derivatives, processes for preparing, and processes of using the derivatives. The derivatives are prepared by condensation of lithium dienolate of prenal with an aldehyde or a ketone.The pyran derivative prepared from .beta.-ionylideneacetaldehyde when treated in the presence of a catalyst directly forms retinal.
摘要翻译：本发明涉及二氢吡喃衍生物，制备方法和使用衍生物的方法。衍生物通过将prenal的二烯酸锂与醛或酮的缩合来制备。由β-亚酰基乙醛制备的吡喃衍生物在催化剂存在下处理直接形成视网膜。

13. 发明申请

US20070191407A1 PROCESSES FOR THE PREPARATION OF 4-[[4-[[4-(2-CYANOETHENYL)-2,6-DIMETHYLPHENYL]-2-PYRIMIDINYL]AMINO]BENZONITRILE 有权
标题翻译：制备4 - [[4 - [[4-（2-氰基乙基）-2,6-二甲基苯基] -2-吡啶基]氨基]苯并噻唑的方法
公开(公告)号：US20070191407A1
公开(公告)日：2007-08-16
申请号：US11738688
申请日：2007-04-23
申请人： Didier Schils , Joannes Willems , Bart Petrus Anna Medaer , Elisabeth Therese Pasquier , Paul Janssen , Jan Heeres , Ruben Gerardus Leenders , Jerome Guillemont
发明人： Didier Schils , Joannes Willems , Bart Petrus Anna Medaer , Elisabeth Therese Pasquier , Paul Janssen , Jan Heeres , Ruben Gerardus Leenders , Jerome Guillemont
IPC分类号： A61K31/505 , C07D239/48
CPC分类号： C07D239/48 , C07C253/20 , C07C253/30 , C07C255/42
摘要： Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]amino]benzonitrile of formula (I), a N-oxide, a pharmaceutically acceptable acid addition salt, a quaternary amine or a stereochemically isomeric form thereof are provided, said processes comprise: a) reacting 4-(2-cyanoethenyl)-2,6-dimethylbenzenamine with an intermediate of formula (III) in the presence of a suitable solvent; b) reacting an intermediate of formula (IV) with acrylonitrile in the presence of a suitable palladium catalyst, a suitable base and a suitable solvent; c) dehydrating the corresponding amide of the compound of formula (I).
摘要翻译：用于制备式（I）的4 - [[4 - [[4-（2-氰基乙烯基）-2,6-二甲基苯基] - 氨基] -2-嘧啶基]氨基]苄腈的方法，N-氧化物，提供药学上可接受的酸加成盐，季胺或其立体化学异构形式，所述方法包括：a）使4-（2-氰基乙烯基）-2,6-二甲基苯胺与式（III）的中间体在合适的溶剂; b）在合适的钯催化剂，合适的碱和合适的溶剂的存在下使式（Ⅳ）的中间体与丙烯腈反应; c）使相应的式（I）化合物的酰胺脱水。

14. 发明申请

US20070093659A1 Piperdine-amino-benzimidazole derivatives as inhibitors of respiratory syncytial virus replication 有权
公开(公告)号：US20070093659A1
公开(公告)日：2007-04-26
申请号：US10596519
申请日：2004-12-20
申请人： Jean-Francois Bonfanti , Koenraad Andries , Frans Janssens , Francois Sommen , Jerome Guillemont , Jean Lacrampe
发明人： Jean-Francois Bonfanti , Koenraad Andries , Frans Janssens , Francois Sommen , Jerome Guillemont , Jean Lacrampe
IPC分类号： C07D473/00
CPC分类号： C07D401/14 , C07D417/14
摘要： The present invention concerns piperidine-amino-benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula their prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms wherein Q is C1-6alkyl optionally substituted with trifluoromethyl, C3-7cycloalkyl, Ar2, hydroxy, C1-4alkoxy, C1-4alkylthio, Ar2-oxy-, Ar2-thio-, Ar2(CH2)noxy, Ar2(CH2)nthio, hydroxycarbonyl, aminocarbonyl, C1-4alkylcarbonyl, Ar2carbonyl, C1-4alkoxycarbonyl, Ar2(CH2)ncarbonyl, aminocarbonyloxy, C1-4alkylcarbonyloxy, Ar2carbonyloxy, Ar2(CH2)ncarbonyloxy, C1-4alkoxy-carbonyl(CH2)noxy, mono- or di(C1-4alkyl)aminocarbonyl, mono- or di(C1-4alkyl)-aminocarbonyloxy, aminosulfonyl, mono- or di(C1-4alkyl)aminosulfonyl or a heterocycles selected from the group consisting of pyrrolidinyl, pyrrolyl, dihydropyrrolyl, imidazolyl, triazolyl, piperidinyl, homopiperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxothiomorpholinyl, pyridyl and tetrahydropyridyl, wherein each of said heterocycle may optionally be substituted with oxo or C1-6alkyl; G is a direct bond or optionally substituted C1-10alkanediyl; R1 is Ar1 or a monocyclic or bicyclic heterocycle; one of R2a and R3a is C1-6alkyl and the other one of R2a and R3a is hydrogen; in case R2a is different from hydrogen then R2b is hydrogen or C1-6alkyl, and R3b is hydrogen; in case R3a is different from hydrogen then R3b is hydrogen or C1-6alkyl, and R2b is hydrogen; t is 1, 2 or 3; Ar1 is phenyl or substituted phenyl; and Ar2 is phenyl or substituted phenyl. It further concerns their preparation and compositions comprising them, as well as their use as a medicine.

15. 发明申请

US20060167253A1 Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-2pyrimidinyl]amino]benzonitrile 有权
标题翻译：制备4 - [[4 - [[4-（2-氰基乙烯基）-2,6-二甲基苯基]氨基] -2-2嘧啶基]氨基]苄腈的方法
公开(公告)号：US20060167253A1
公开(公告)日：2006-07-27
申请号：US10523753
申请日：2003-08-07
申请人： Didier Philippe Schils , Joannes Josephus Willems , Bart Petrus Anna Medaer , Elisabeth Pasquier , Paul Janssen , Jan Heeres , Ruben Gerardus Leenders , Jerome Guillemont
发明人： Didier Philippe Schils , Joannes Josephus Willems , Bart Petrus Anna Medaer , Elisabeth Pasquier , Paul Janssen , Jan Heeres , Ruben Gerardus Leenders , Jerome Guillemont
IPC分类号： C07D239/48
CPC分类号： C07D239/48 , C07C253/20 , C07C253/30 , C07C255/42
摘要： Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]amino]benzonitrile of formula (I), a N-oxide, a pharmaceutically acceptable acid addition salt, a quaternary amine or a stereochemically isomeric form thereof are provided, said processes comprise: a) reacting 4-(2-cyanoethenyl)-2,6-dimethylbenzenamine with an intermediate of formula (III) in the presence of a suitable solvent; b) reacting an intermediate of formula (IV) with acrylonitrile in the presence of a suitable palladium catalyst, a suitable base and a suitable solvent; c) dehydrating the corresponding amide of the compound of formula (I).
摘要翻译：用于制备式（I）的4 - [[4 - [[4-（2-氰基乙烯基）-2,6-二甲基苯基] - 氨基] -2-嘧啶基]氨基]苄腈的方法，N-氧化物，提供药学上可接受的酸加成盐，季胺或其立体化学异构形式，所述方法包括：a）使4-（2-氰基乙烯基）-2,6-二甲基苯胺与式（III）的中间体在合适的溶剂; b）在合适的钯催化剂，合适的碱和合适的溶剂的存在下使式（Ⅳ）的中间体与丙烯腈反应; c）使相应的式（I）化合物的酰胺脱水。

16. 发明申请

US20060154913A1 Respiratory syncytial virus replication inhibitors 失效
标题翻译：呼吸道合胞病毒复制抑制剂
公开(公告)号：US20060154913A1
公开(公告)日：2006-07-13
申请号：US11332557
申请日：2006-01-12
申请人： Frans Janssens , Kathleen Meersman , Francois Sommen , Jerome Guillemont , Jean Lacrampe , Koenraad Jozef Andries
发明人： Frans Janssens , Kathleen Meersman , Francois Sommen , Jerome Guillemont , Jean Lacrampe , Koenraad Jozef Andries
IPC分类号： A61K31/551 , A61K31/496 , A61K31/4745 , C07D471/02
CPC分类号： A61K31/4184 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4745 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/551 , C07D235/24 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： This invention concerns the use of compounds of formula (I) wherein -a1=a2-a3=a4- is 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 formulas (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7), (b-8). G is a direct bond or C1-10alkanediyl; R1 is an optionally substituted monocyclic heterocycle; for the manufacture of a medicament for the treatment of viral infections, in particular RSV infections. Certain compounds of formula (I) are new.
摘要翻译：本发明涉及式（I）化合物的用途，其中-a-1-a- 是式-CH-CH-CH-CH-，-N-CH-CH-CH-，-CH-N-CH-CH-，-CH-CH-N-CH-， - CH-CH-CH-，其中每个氢原子可以任选被取代; Q是式（b-1），（b-2），（b-3），（b-4），（b-5），（b-6），（b-7） -8）。 G是直链或C 1-10烷二基; R 1是任选取代的单环杂环; 用于制备用于治疗病毒感染，特别是RSV感染的药物。某些式（I）化合物是新的。

17. 发明授权

US5120864A Intermediates, process for their preparation, and their use for the synthesis of vitamins A and E 失效
标题翻译：中间体，其制备方法及其合成维生素A和E的用途
公开(公告)号：US5120864A
公开(公告)日：1992-06-09
申请号：US620854
申请日：1990-12-03
申请人： Pierre F. Charbardes , Lucette Duhamel , Pierre Duhamel , Jerome Guillemont , Jean-Marie Poirier
发明人： Pierre F. Charbardes , Lucette Duhamel , Pierre Duhamel , Jerome Guillemont , Jean-Marie Poirier
IPC分类号： C07D317/12 , B01J27/08 , B01J31/02 , C07B61/00 , C07C45/59 , C07C47/24 , C07C403/14 , C07C403/22 , C07D317/16 , C07D317/20 , C07D319/06 , C07D325/00 , C07F9/655
CPC分类号： C07C403/14 , C07C45/59 , C07C47/24 , C07D317/20 , C07D319/06 , C07F9/65515 , C07C2101/16
摘要： New intermediates and processes for the preparation of vitamins A and E, which are the acetals of 5,6-dihalo-3-methyl-3-hydroxyhexanal or of 6-halo-3-hydroxy-3-methyl-5-hexenal or 3-methyl-3-hydroxy-5-hexenal, as well as processes for making the intermediates. After dehydrohalogenation and dehydration these intermediates are condensed directly with .beta.-ionone or with 2-methyl-2-heptene-6-one to synthesize vitamins A and E respectively.
摘要翻译：用于制备维生素A和E的新中间体和方法，其为5,6-二卤代-3-甲基-3-羟基己醛或6-卤代-3-羟基-3-甲基-5-己烯醛或3 3-甲基-3-羟基-5-己烯醛，以及制备中间体的方法。在脱卤化氢和脱水后，这些中间体直接与β-戊酮或2-甲基-2-庚烯-6-酮缩合以分别合成维生素A和E。

18. 发明申请

US20080085907A1 Hiv Inhibiting Bicyclic Pyrimdine Derivatives 有权
公开(公告)号：US20080085907A1
公开(公告)日：2008-04-10
申请号：US11718181
申请日：2005-10-27
申请人： Jerome Guillemont , Mikael Paugam , Bruno Delest , Jan Heeres , Paulus Lewi , Paul Adriaan Janssen , Frank Javier Arts
发明人： Jerome Guillemont , Mikael Paugam , Bruno Delest , Jan Heeres , Paulus Lewi , Paul Adriaan Janssen , Frank Javier Arts
IPC分类号： C07D473/36 , A61K31/519 , A61K31/52 , A61P31/18 , C07D487/04 , C07D239/70 , C07D473/32
CPC分类号： C07D487/04 , C07D473/00 , C07D473/16 , C07D473/24 , C07D473/34
摘要： HIV replication inhibitors of formula (1) N-oxides, pharmaceutically acceptable addition salts, quaternary amines or stereoisomeric forms thereof, 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, 1, 2, 3 and in certain cases also 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl: optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalomethylthio; —S(═O)pR6; C(═NH)R6; R2a is CN; amino; substituted amino; optionally substituted C1-6alkyl; halo; optionally substituted C1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R16; optionally substituted C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4 alkyl; R7 or —X—R4; R3 is CN; amino; C1-6alkyl; halo; optionally substituted C1-6alkyloxy; substituted carbonyl; —CH═N—NH—C(═O)—R16: substituted C1-6alkyl; optionally substituted C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(═N—O—R8)—C1-4 alkyl; R7; —X—R7; R4 is halo; OH; optionally substituted 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—; pharmaceutical compositions comprising these; methods for the preparation of these compounds and compositions; the use of these compounds for the prevention or the treatment of HIV infection.

19. 发明申请

US20070299106A1 NOVEL MYCOBACTERIAL INHIBITORS 有权
公开(公告)号：US20070299106A1
公开(公告)日：2007-12-27
申请号：US11422152
申请日：2006-06-05
申请人： Jerome Guillemont , Elisabeth Therese Pasquier , David Francis Lancois
发明人： Jerome Guillemont , Elisabeth Therese Pasquier , David Francis Lancois
IPC分类号： A61K31/47 , A61K31/4706 , A61P31/06 , C07D215/12
CPC分类号： C07D215/18
摘要： The present invention relates to novel substituted quinoline derivatives according to the general Formula (I) pharmaceutically acceptable addition salts, quaternary amines, stereochemically isomeric forms, tautomeric forms and N-oxide forms thereof, wherein R1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1, 2 or 3; s is 0, 1, 2, 3 or 4; R2 is hydrogen; halo; alkyl; hydroxy; mercapto; optionally substituted alkyloxy; alkyloxyalkyloxy; alkylthio; mono or di(alkyl)amino wherein alkyl may optionally be substituted; Ar; Het, a radical of formula R3 is alkyl, Ar, Ar-alkyl, Het, Het-alkyl; q is 0, 1, 2, 3 or 4; R4 and R5 are hydrogen, alkyl, benzyl; or R4 and R5 may be taken together including the N to which they are attached; R6 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; or two vicinal R6 radicals may be taken together to form together with the phenyl ring to which they are attached a naphthyl; r is 1, 2, 3, 4 or 5; R7 is hydrogen, alkyl, Ar or Het; R8 is hydrogen-, alkyl, hydroxyl, aminocarbonyl, mono-or di(alkyl)aminocarbonyl, Ar, Het, substituted alkyl, Het-C(═O)— or Ar—C(═O)—; provided that when the quinoline substituent carrying the R3 to R6 substituents is placed in position 3 of the quinoline moiety; R7 is placed in position 4 and R2 is placed in position 2 and represents hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula then s is 1, 2, 3 or 4; also claimed is a composition comprising the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of mycobacterial diseases and a process for preparing the claimed compounds.

20. 发明申请

US20060194804A1 Hiv replication inhibiting pyrimidines and triazines 有权
标题翻译： Hiv复制抑制嘧啶和三嗪
公开(公告)号：US20060194804A1
公开(公告)日：2006-08-31
申请号：US10545358
申请日：2004-02-20
申请人： Jerome Guillemont , Elisabeth Pasquier , Jan Heeres , Kurt Hertogs , Eva Bettens , Paulus Lewi , Marc De Jonge , Lucien Maria Koymans , Frederik Daeyaert , Hendrik Vinkers , Adriaan Janssen , Frank Zavier Jozef Arts
发明人： Jerome Guillemont , Elisabeth Pasquier , Jan Heeres , Kurt Hertogs , Eva Bettens , Paulus Lewi , Marc De Jonge , Lucien Maria Koymans , Frederik Daeyaert , Hendrik Vinkers , Adriaan Janssen , Frank Zavier Jozef Arts
IPC分类号： A61K31/53 , A61K31/506 , C07D405/14
CPC分类号： C07D239/47 , C07D239/48 , C07D413/12
摘要： This invention concerns HIV replication inhibitors of formula (I), The N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式（I）的N-复制抑制剂，N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构形式，它们作为药物的用途，其制备方法和包含它们的药物组合物。

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