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21. 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.

22. 发明授权

US06177432B1 Farnesyltransferase inhibiting quinazolinones 有权
标题翻译：法呢基转移酶抑制喹唑啉酮
公开(公告)号：US06177432B1
公开(公告)日：2001-01-23
申请号：US09403705
申请日：1999-10-22
申请人： Patrick Ren{acute over (e)} Angibaud , Marc Gaston Venet , Eddy Jean Edgard Freyne
发明人： Patrick Ren{acute over (e)} Angibaud , Marc Gaston Venet , Eddy Jean Edgard Freyne
IPC分类号： A61K31505
CPC分类号： C07D231/12 , C07D233/56 , C07D239/82 , C07D249/08 , C07D403/06 , C07D405/04
摘要： This invention concerns compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; R1 and R2 each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy, C1-6alkyloxycarbonyl, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, Ar1, Ar1C1-6alkyl, Ar1oxy, Ar1C1-6alkyloxy; or when on adjacent positions R1 and R2 taken together may form a bivalent radical; R3 and R4 each independently are hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxy, Ar1oxy, C1-6alkylthio, di(C1-6alkyl)amino, trihalomethyl, trihalomethoxy; R5 is hydrogen, halo, cyano, optionally substituted C1-6alkyl, C1-6alkyloxycarbonyl or Ar1; or a radical of formula —OR10, —SR10, —NR11R12; R6 is an optionally substituted imidazolyl moiety; R7 is hydrogen or C1-6alkyl provided that the dotted line does not represent a bond; R8 is hydrogen, C1-6alkyl or Ar2CH2 or Het1CH2; R9 is hydrogen, C1-6alkyl, C1-6alkyloxy or halo, or R8 and R9 taken together may form a bivalent radical; Ar1 and Ar2 are optionally substituted phenyl and Het1 is optionally substituted pyridinyl; having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明涉及配制药学上可接受的酸加成盐和其立体化学异构形式的化合物，其中虚线表示任选的键; X是氧或硫; R 1和R 2各自独立地为氢，羟基，卤素，氰基，C 1-6烷基，三卤代甲基，三卤甲氧基，C 2-6烯基，C 1-6烷氧基，羟基C 1-6烷氧基，C 1-6烷氧基C 1-6烷氧基，C 1-6烷氧基羰基，氨基C 1-6烷氧基，或二（C 1-6烷基）氨基C 1-6烷氧基，Ar 1，Ar 1 C 1-6烷基，Ar 1氧基，Ar 1 C 1-6烷氧基; 或者当在相邻位置R1和R2一起可以形成二价基团时; R 3和R 4各自独立地为氢，卤素，氰基，C 1-6烷基，C 1-6烷氧基，Ar 1氧基，C 1-6烷硫基，二（C 1-6烷基）氨基，三卤甲基，三卤甲氧基; R5是氢，卤素，氰基，任意取代的C 1-6烷基，C 1-6烷氧基羰基或Ar 1; 或式-OR 10，-SR 10，-NR 11 R 12的基团; R6是任选取代的咪唑基部分; R 7是氢或C 1-6烷基，条件是虚线不代表键; R8是氢，C1-6烷基或Ar2CH2或Het1CH2; R9是氢，C1-6烷基，C1-6烷氧基或卤素，或R8和R9一起可以形成二价基; Ar1和Ar2是任选取代的苯基，Het1是任选取代的吡啶基; 具有法呢基转移酶抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

23. 发明授权

US6124330A N-[4-(Heteroarylmethyl)phenyl]-heteroarylamines 有权
标题翻译： N- [4-（杂芳基甲基）苯基] - 杂芳基胺
公开(公告)号：US6124330A
公开(公告)日：2000-09-26
申请号：US214080
申请日：1999-04-29
申请人： Marc Gaston Venet , Dominique Jean-Pierre Mabire , Jean Fernand Armand Lacrampe , Gerard Charles Sanz
发明人： Marc Gaston Venet , Dominique Jean-Pierre Mabire , Jean Fernand Armand Lacrampe , Gerard Charles Sanz
IPC分类号： C07D473/34 , A61K31/00 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/4184 , A61K31/42 , A61K31/423 , A61K31/425 , A61K31/427 , A61K31/435 , A61K31/4353 , A61K31/437 , A61K31/44 , A61K31/4427 , A61K31/4439 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/454 , A61K31/47 , A61K31/472 , A61K31/4725 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/498 , A61K31/50 , A61K31/501 , A61K31/502 , A61K31/505 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/52 , A61K31/529 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61P17/00 , A61P17/06 , A61P35/00 , A61P43/00 , C07D277/22 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D513/04 , C07D521/00 , A61K31/426 , C07D277/60 , C07D417/10
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D487/04 , C07D513/04
摘要： The present invention is concerned with compounds of formula ##STR1## the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 is hydrogen, hydroxy, C.sub.1-6 alkyl or aryl; R.sup.2 is hydrogen; optionally substituted C.sub.1-12 alkyl; C.sub.3-7 cycloalkyl; C.sub.2-8 alkenyl, optionally substituted pyrrolidinyl or aryl; R.sup.3 is hydrogen, optionally substituted C.sub.1-6 alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; ##STR2## is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.
摘要翻译： PCT No.PCT / EP97 / 03248 Sec。 371日期1999年4月29日第 102（e）1999年4月29日PCT 1997年6月19日PCT公布。公开号WO97 / 49704 PCT 日期1997年12月31日本发明涉及式I化合物的N-氧化物，其药学上可接受的加成盐及其立体化学异构形式，其中R 1是氢，羟基，C 1-6烷基或芳基; R2是氢; 任选取代的C 1-12烷基; C 3-7环烷基; C 2-8烯基，任选取代的吡咯烷基或芳基; R3是氢，任选取代的C 1-6烷基或芳基; Het是选自咪唑基，三唑基，四唑基和吡啶基的任选取代的不饱和杂环; 是任选取代的不饱和单环或双环杂环; 并且芳基是任选取代的苯基。本发明还涉及其制备方法和包含所述新化合物的组合物，以及它们作为药物的用途。

24. 发明授权

US07205312B2 N-[4-(heteroarylmethyl)phenyl]-heteroarylamines 有权
标题翻译： N- [4-（杂芳基甲基）苯基] - 杂芳基胺
公开(公告)号：US07205312B2
公开(公告)日：2007-04-17
申请号：US10979362
申请日：2004-11-02
申请人： Marc Gaston Venet , Dominique Jean-Pierre Mabire , Jean Fernand Armand Lacrampe , Gerard Charles Sanz
发明人： Marc Gaston Venet , Dominique Jean-Pierre Mabire , Jean Fernand Armand Lacrampe , Gerard Charles Sanz
IPC分类号： A61K31/44 , C07D415/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D487/04 , C07D513/04
摘要： The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.
摘要翻译：本发明涉及式的化合物

25. 发明授权

US06867207B2 IL-5 inhibiting 6-azauracil derivatives 失效
标题翻译： IL-5抑制6-氮尿嘧啶衍生物
公开(公告)号：US06867207B2
公开(公告)日：2005-03-15
申请号：US09891888
申请日：2001-06-26
申请人： Jean Fernand Armand Lacrampe , Eddy Jean Edgard Freyne , Marc Gaston Venet , Gustaaf Maria Boeckx
发明人： Jean Fernand Armand Lacrampe , Eddy Jean Edgard Freyne , Marc Gaston Venet , Gustaaf Maria Boeckx
IPC分类号： A61P37/08 , C07D401/10 , C07D403/10 , C07D403/12 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D253/065 , A61K31/53 , A61K17/00
CPC分类号： C07D401/10 , C07D403/10 , C07D403/12 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14
摘要： The present invention is concerned with the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, p and q are 0, 1, 2, 3 or 4 and q is also 5; X is O, S, NR3 or a direct bond; R1 is hydrogen, hydroxy, halo, optionally substituted amino, optionally substituted C1-6alkyl, C1-6alkyloxy, C3-7cycloalkyl or aryl; R2 is aryl, Het1, C3-7cycloalkyl, optionally substituted C1-6alkyl; and if X is O, S or NR3, then R2 may also be a carbonyl or thiocarbonyl linked substituent; R3 is hydrogen or C1-4alkyl; R4 and R5 independently are optionally substituted C1-6alkyl, halo, hydroxy, mercapto, C1-6alkyloxy, C1-6akylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het3, R6 or NR7R8; R6 is substituted sulfonyl or sulfinyl; R7 and R8 are hydrogen, optionally substituted C1-4alkyl, aryl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl, Het3 and R6; R9 and R10 are each independently selected from hydrogen, optionally substituted C1-4alkyl, phenyl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl, Het3 and R6; R11 is hydroxy, mercapto, cyano, nitro, halo, trihalomethyl, C1-4alkyloxy, carboxyl, C1-4alkyloxycarbonyl, trihaloC1-4alkylsulfonyloxy, R6, NR7R8, C(═O)NR7R8, aryl, aryloxy, arylcarbonyl, C3-7cycloalkyl, C3-7cycloalkyloxy, phthalimide-2-yl, Het3 and C(═O)Het3; R12 and R13 are each independently selected from hydrogen, optionally substituted C1-4alkyl, phenyl, a carbonyl or thiocarbonyl linked substituent, C3-7cycloalkyl and R6; aryl is optionally substituted phenyl; Het1, Het2 and Het3 are optionally substituted heterocycles; to processes for their preparation and compositions comprising them. It further relates to their use as a medicine.
摘要翻译：本发明涉及配制N-氧化物的化合物，其药学上可接受的加成盐及其立体化学异构形式，p和q分别为0,1,2,3或4，q也为5; X是O，S，NR 3或直接键; R 1是氢，羟基，卤素，任选取代的氨基，任选取代的C 1-6烷基，C 1-6烷氧基，C 3-7环烷基或芳基; R 2是芳基，Het 1，C 3-7环烷基，任选取代的C 1-6烷基; 并且如果X是O，S或NR 3，则R 2也可以是羰基或硫代羰基连接的取代基; R 3是氢或C 1-4烷基; R 4和R 5独立地是任选取代的C 1-6烷基，卤素，羟基，巯基，C 1-6烷氧基，C 1-6烷硫基，C 1-6烷基羰基氧基，芳基，氰基，硝基，Het 3，或NR 7 R 8; R 6是取代的磺酰基或亚磺酰基; R 7和R 8是氢，任选取代的C 1-4烷基，芳基，羰基或硫代羰基连接的取代基，C 3-7环烷基，Het 3和R 6; R 9和R 10各自独立地选自氢，任选取代的C 1-4烷基，苯基，羰基或硫代羰基连接的取代基，C 3-7环烷基，Het 3和R 6; R 11是羟基，巯基，氰基，硝基，卤素，三卤代甲基，C 1-4烷氧基，羧基，C 1-4烷氧基羰基，三卤代C 1-4烷基磺酰氧基，R 6，NR 7 R 8，C（= O） NR 7 R 8，芳基，芳氧基，芳基羰基，C 3-7环烷基，C 3-7环烷氧基，邻苯二甲酰亚胺-2-基，Het 3和C（= O）Het 3; R 12和R 13各自独立地选自氢，任选取代的C 1-4烷基，苯基，羰基或硫代羰基连接的取代基，C 3-7环烷基和R 6; 芳基是任选取代的苯基; Het <1>，Het <

26. 发明授权

US5922734A 6-�triazolyl�3-(trifluoromethyl)phenyl!methyl!-2-quinolines and -quinolinethiones 失效
标题翻译： 6- [三唑基[3-（三氟甲基）苯基]甲基] -2-喹啉和喹啉硫酮
公开(公告)号：US5922734A
公开(公告)日：1999-07-13
申请号：US860239
申请日：1997-06-16
申请人： Marc Gaston Venet , Dominique Jean-Pierre Mabire , Gerard Charles Sanz
发明人： Marc Gaston Venet , Dominique Jean-Pierre Mabire , Gerard Charles Sanz
IPC分类号： C07D401/06 , A61K8/14 , A61K8/49 , A61K31/47 , A61P17/00 , A61P43/00 , C07D521/00
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56
摘要： This invention is concerned with the compounds of formula ##STR1## the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof,wherein: R.sup.1 is hydrogen, amino or C.sub.1-4 alkyl; R.sup.2 is hydrogen, halo or C.sub.1-4 alkyl; R.sup.3 is hydrogen, halo or C.sub.1-4 alkyl; Y is 0 or S, and --X.sup.1 .dbd.X.sup.2 --is a bivalent radical having the formula --N.dbd.CH--(a-1) or --CH.dbd.N--(a-2);compositions containing the same, and processes of preparing these compounds. It further relates to their use as a medicine, in particular their use as a medicine to treat keratinization disorders.
摘要翻译： PCT No.PCT / EP95 / 05173 Sec。 371日期：1997年6月16日 102（e）日期1996年6月16日PCT 1995年12月21日PCT PCT。 WO96 / 20200 PCT出版物日期：1996年7月4日本发明涉及药学上可接受的酸加成盐及其立体化学异构形式的化合物，其中：R1是氢，氨基或C1-4烷基; R2是氢，卤素或C1-4烷基; R3是氢，卤素或C1-4烷基; Y为0或S，-X1 = X2-为具有式-N = CH-（a-1）或-CH = N-（a-2）的二价基团。含有它们的组合物，以及制备这些化合物的方法。它还涉及它们作为药物的用途，特别是它们作为治疗角质化障碍的药物的用途。

27. 发明授权

US5663354A Process for preparing enantiomerically pure 6-[(4-chlorophenyl) (1H-1,2,4-triazol-1-yl) methyl]-1-methyl-1H-benzotrizole 失效
标题翻译：制备对映体纯的6 - [（4-氯苯基）（1H-1,2,4-三唑-1-基）甲基] -1-甲基-1H-苯并三唑的方法
公开(公告)号：US5663354A
公开(公告)日：1997-09-02
申请号：US424295
申请日：1995-04-18
申请人： Albert Louis Anna Willemsens , Walter Louis Antoine Verstappen , Alex Herman Copmans , Anna Maria Jozefa Vandendriessche , Alfons Gaston Maria De Knaep , Marc Gaston Venet
发明人： Albert Louis Anna Willemsens , Walter Louis Antoine Verstappen , Alex Herman Copmans , Anna Maria Jozefa Vandendriessche , Alfons Gaston Maria De Knaep , Marc Gaston Venet
IPC分类号： C07B57/00 , C07D249/18 , C07D403/06 , C07D521/00
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D249/18
摘要： A process for preparing (+)-6-[(4-chlorophenyl)(1H-1,2,4-triazol-1-yl)methyl]-1-methyl-1H-benzotriazole comprising the resolution of (.+-.)-6-[(4-chlorophenyl)-hydrazinomethyl)-1-methyl-1H-benzotriazole and converting the appropriate enantiomerically pure hydrazine intermediate into (+)-6-[(4-chlorophenyl)(1 H-1,2,4-triazol-1-yl)methyl]-1-methyl-1H-benzotriazole.
摘要翻译： PCT No.PCT / EP93 / 03066 Sec。 371日期1995年04月18日 102（e）日期1995年4月18日PCT 1993年11月2日PCT公布。公开号WO94 / 11364 日期1994年5月26日制备（+） - 6 - [（4-氯苯基）（1H-1,2,4-三唑-1-基）甲基] -1-甲基-1H-苯并三唑的制备方法，包括（ +/-） - 6 - [（4-氯苯基） - 肼基甲基）-1-甲基-1H-苯并三唑，并将合适的对映体纯的肼中间体转化为（+） - 6 - [（4-氯苯基）（1H-1 ，2,4-三唑-1-基）甲基] -1-甲基-1H-苯并三唑。

28. 发明授权

US07498343B2 Mycobacterial inhibitors 有权
标题翻译：分枝杆菌抑制剂
公开(公告)号：US07498343B2
公开(公告)日：2009-03-03
申请号：US11007026
申请日：2004-12-08
申请人： Jozef Frans Elisabetha Van Gestel , Jérôme Emile Georges Guillemont , Marc Gaston Venet , Hervé Jean Joseph Poignet , Laurence Françoise Bernadette Decrane , Daniel F. J. Vernier , Frank Christopher Odds
发明人： Jozef Frans Elisabetha Van Gestel , Jérôme Emile Georges Guillemont , Marc Gaston Venet , Hervé Jean Joseph Poignet , Laurence Françoise Bernadette Decrane , Daniel F. J. Vernier , Frank Christopher Odds
IPC分类号： A61K31/44 , C07D215/38
CPC分类号： C07D215/227 , C07D215/36 , C07D215/48 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/06 , C07D409/04 , C07D409/06 , C07D471/04
摘要： The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or the general Formula (Ib) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof and the N-oxide forms thereof. The claimed compounds are useful for the treatment of mycobacterial diseases, particularly those diseases caused by pathogenic mycobacteria such as Mycobacterium tuberculosis, M. bovis, M. avium and M. marinum. In particular, compounds are claimed in which, independently from each other, R1 is bromo, p=1, R2 is alkyloxy, R3 is optionally substituted naphthyl or phenyl, q=1, R4 and R5 each independently are hydrogen, methyl or ethyl, R6 is hydrogen, r is equal to 0 or 1 and R7 is hydrogen. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of 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.
摘要翻译：本发明涉及根据通式（Ia）或通式（Ib）的药学上可接受的酸或碱加成盐，其立体化学异构形式，其互变异构形式和N-氧化物形式的新的取代喹啉衍生物其中。所要求保护的化合物可用于治疗分枝杆菌疾病，特别是由致病性分枝杆菌引起的疾病如结核分枝杆菌，牛分枝杆菌，鸟分枝杆菌和马氏海马。特别是要求保护的化合物，其中R 1为溴，p = 1，R 2为烷氧基，R 3为任选取代的萘基或苯基，q为1，R 4和R 5各自独立地为氢，甲基或乙基， R6是氢，r等于0或1，而R7是氢。还要求保护的是包含药学上可接受的载体和作为活性成分的治疗有效量的要求保护的化合物的组合物，所要求保护的化合物或组合物在制备用于治疗分枝杆菌疾病的药物中的用途以及制备方法要求保护的化合物。

29. 发明申请

US20080255191A1 BENZYLIMIDAZOLYL SUBSTITUTED 2-QUINOLINE AND QUINAZOLINE DERIVATIVES FOR USE AS FARNESYL TRANSFERASE INHIBITORS 有权
标题翻译：苄基咪唑取代的2-喹啉和喹唑啉衍生物，用作呋喃葡萄糖转移酶抑制剂
公开(公告)号：US20080255191A1
公开(公告)日：2008-10-16
申请号：US11758346
申请日：2007-06-05
申请人： Patrick Rene Angibaud , Marc Gaston Venet , Christophe Meyer , Henry Joseph Breslin
发明人： Patrick Rene Angibaud , Marc Gaston Venet , Christophe Meyer , Henry Joseph Breslin
IPC分类号： A61K31/4709 , C07D403/08 , A61K31/4155 , C07D401/08
CPC分类号： C07D401/06 , C07D401/14 , C07D471/04
摘要： This invention comprises the novel compounds of formula (I) wherein r, t, Y1, Y2, R1, R2, R3, R5, R6 and R7 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括式（I）的新化合物，其中r，t，Y 1，Y 2，R 1，R 2， 2，R 3，R 5，R 6和R 7具有定义的含义，具有法呢基转移酶抑制活性; 其制剂，含有它们的组合物及其作为药物的用途。

30. 发明授权

US07115630B2 Metabotropic glutamate receptor antagonists 有权
公开(公告)号：US07115630B2
公开(公告)日：2006-10-03
申请号：US10381987
申请日：2001-09-25
申请人： Dominique Jean-Pierre Mabire , Marc Gaston Venet , Sophie Coupa , Alain Philippe Poncelet , Anne Simone Josephine Lesage
发明人： Dominique Jean-Pierre Mabire , Marc Gaston Venet , Sophie Coupa , Alain Philippe Poncelet , Anne Simone Josephine Lesage
IPC分类号： C07D215/17 , C07D215/20 , A61K31/47
CPC分类号： C07D215/04 , C07D215/12 , C07D215/14 , C07D215/18 , C07D215/227 , C07D215/36 , C07D215/38 , C07D215/48 , C07D215/50 , C07D215/54 , C07D221/10 , C07D221/12 , C07D221/16 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D417/04 , C07D453/06 , C07D471/04 , C07D491/04 , C07D495/04 , C07F7/0812
摘要： The present invention concerns compounds of formula. In a preferable embodiment, X represents O; R1 represents C1-6alkyl; cycloC3-12alkyl or (cycloC3-12alkyl)C1-6alkyl, wherein one or more hydrogen atoms in a C1-6alkyl-moiety or in a cycloC3-12alkyl-moiety optionally may be replaced by C1-6alkyloxy, aryl, halo or thienyl; R2 represents hydrogen; halo; C1-6alkyl or amino; R3 and R4 each independently represent hydrogen or C1-6alkyl; or R2 and R3 may be taken together to form —R2—R3—, which represents a bivalent radical of formula —Z4—CH2—CH2—CH2— or —Z4—CH2—CH2— with Z4 being O or NR11 wherein R11 is C1-6alkyl; and wherein each bivalent radical is optionally substituted with C1-6alkyl; or R3 and R4 may be taken together to form a bivalent radical of formula —CH2—CH2—CH2—CH2—; R5 represents hydrogen; Y represents O; and aryl represents phenyl optionally substituted with halo. The invention also relates to the use of a compound according to the invention as a medicament and in the manufacture of a medicament for treating or preventing glutamate-induced diseases of the central nervous system, as well as formulations comprising such a compound and processes for preparing such a compound.

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