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11. 发明申请

US20070043022A1 Morpholinyl containing benzimidazoles as inhibitors of respiratory syncytial virus replication 有权
公开(公告)号：US20070043022A1
公开(公告)日：2007-02-22
申请号：US10563691
申请日：2004-12-20
申请人： Jean-Francois Bonfanti , Koenraad Andries , Jerome Fortin , Phillippe Muller , Frederic Doublet , Christophe Meyer , Rudy Willebrords , Tom Gevers , Philip Maria Timmerman
发明人： Jean-Francois Bonfanti , Koenraad Andries , Jerome Fortin , Phillippe Muller , Frederic Doublet , Christophe Meyer , Rudy Willebrords , Tom Gevers , Philip Maria Timmerman
IPC分类号： A61K31/554 , A61K31/553 , A61K31/541 , A61K31/5377 , A61K31/4745 , A61K31/4743 , A61K31/4741 , A61K31/506 , A61K31/501 , A61K31/498 , A61K31/497 , A61K31/4184
CPC分类号： C07D413/12 , C07D401/06 , C07D401/14 , C07D413/14
摘要： The present invention concerns morpholinyl containing benzimidazoles having inhibitory activity on the replication of the respiratory syncytial virus and having the formula a prodrug, N-oxide, addition salt, quaternary amine, metal complex or stereochemically isomeric form thereof wherein G is a direct bond or optionally substituted C1-10alkanediyl; R1 is Ar1 or a monocyclic or bicyclic heterocycle Q is R7, pyrrolidinyl substituted with R7, piperidinyl substituted with R7 or homopiperidinyl substituted with R7; one of R2a and R3a is selected from halo, optionally mono- or polysubstituted C1-6alkyl, optionally mono- or polysubstituted C2-6alkenyl, nitro, hydroxy, Ar2, N(R4aR4b) N(R4aR4b)sulfonyl, N(R4aR4b)carbonyl, C1-6alkyloxy, Ar2oxy, Ar2C1-6alkyloxy, carboxyl, C1-6alkyloxycarbonyl, or —C(=Z)Ar2; and the other one of R2a and R3a is hydrogen; in case R2a is different from hydrogen then R2b is hydrogen, C1-6alkyl or halogen and R3b is hydrogen; in case R3a is different from hydrogen then R3b is hydrogen, C1-6alkyl or halogen and R2b is hydrogen. It further concerns the preparation thereof and compositions comprising these compounds, as well as the use thereof as a medicine.

12. 发明授权

US08716293B2 Macrocyclic integrase inhibitors 有权
标题翻译：大环整合酶抑制剂
公开(公告)号：US08716293B2
公开(公告)日：2014-05-06
申请号：US13637557
申请日：2011-04-01
申请人： Johannes Wilhelmus J. Thuring , Jean-Francois Bonfanti
发明人： Johannes Wilhelmus J. Thuring , Jean-Francois Bonfanti
IPC分类号： C07D487/18 , C07D498/18 , C07D515/18 , A61K31/529 , A61P31/18
CPC分类号： C07D515/18 , C07D487/18 , C07D498/18
摘要： Compound having formula I and pharmaceutically acceptable salts or solvates thereof, their pharmaceutical formulations and use as HIV inhibitors.
摘要翻译：具有式I的化合物及其药学上可接受的盐或溶剂合物，其药物制剂和用作HIV抑制剂。

13. 发明申请

US20130035341A1 MACROCYCLIC INTEGRASE INHIBITORS 有权
标题翻译：大环集成抑制剂
公开(公告)号：US20130035341A1
公开(公告)日：2013-02-07
申请号：US13637557
申请日：2011-04-01
申请人： Johannes Wilhelmus J. Thuring , Jean-Francois Bonfanti
发明人： Johannes Wilhelmus J. Thuring , Jean-Francois Bonfanti
IPC分类号： A61K31/5025 , C07D498/22 , A61P31/18 , C07D515/22
CPC分类号： C07D515/18 , C07D487/18 , C07D498/18
摘要： Compound having formula I and pharmaceutically acceptable salts or solvates thereof, their pharmaceutical formulations and use as HIV inhibitors.
摘要翻译：具有式I的化合物及其药学上可接受的盐或溶剂合物，其药物制剂和用作HIV抑制剂。

14. 发明授权

US07994173B2 2-piperazin-1-yl-3H-imidazo[4,5-b]pyridine derivatives 有权
标题翻译： 2-哌嗪-1-基-3H-咪唑并[4,5-b]吡啶衍生物
公开(公告)号：US07994173B2
公开(公告)日：2011-08-09
申请号：US12523936
申请日：2008-01-24
申请人： Frans Eduard Janssens , Jerome Emile Georges Guillemont , Francois Maria Sommen , Jean-Francois Bonfanti
发明人： Frans Eduard Janssens , Jerome Emile Georges Guillemont , Francois Maria Sommen , Jean-Francois Bonfanti
IPC分类号： A61K31/496 , A61P1/14 , C07D471/04
CPC分类号： C07D471/04
摘要： The present invention is concerned with novel compounds of formula (I) having fundic relaxating activity. 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：本发明涉及具有基础松弛活性的式（I）化合物。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。

15. 发明申请

US20090036466A1 AMINO-BENZIMIDAZOLES DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION 审中-公开
标题翻译：氨基苯并咪唑衍生物作为呼吸道同发病毒复制的抑制剂
公开(公告)号：US20090036466A1
公开(公告)日：2009-02-05
申请号：US10596500
申请日：2004-12-20
申请人： Jean-Francois Bonfanti , Koenraad Jozef Lodewijk Andries , Frans Eduard Janssens , Francois Maria Sommen , Jerome Emile Georges Guillemont , Jean Fernand Armand Lacrampe
发明人： Jean-Francois Bonfanti , Koenraad Jozef Lodewijk Andries , Frans Eduard Janssens , Francois Maria Sommen , Jerome Emile Georges Guillemont , Jean Fernand Armand Lacrampe
IPC分类号： A61K31/496 , C07D401/02 , A61K31/4439 , C07D401/14 , A61P31/12 , A61K31/4545 , C07D403/14
CPC分类号： C07D405/14 , C07D401/06 , C07D401/14
摘要： The present invention concerns 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 Ar1 or C1-6alkyl substituted with one or more substituents selected from trifluoromethyl, C3-7cycloalkyl, Ar2, hydroxy, C1-4alkoxy, C1-4alkylthio, Ar2-oxy-, Ar2-thio-, Ar2(CH2)noxy, Ar2(CH2)nthio, hydroxycarbonyl, aminocarbonyl, C1-4alkylcarbonyl, Ar2-carbonyl, C1-4alkoxycarbonyl, Ar2(CH2)ncarbonyl, aminocarbonyloxy, C1-4alkylcarbonyloxy, Ar2-carbonyloxy, Ar2(CH2)ncarbonyloxy, hydroxy-C2-4-alkyloxy, C1-4alkoxycarbonyl(CH2)noxy, mono- or di(C1-4alkyl)-aminocarbonyl, mono- or di(C1-4alkyl)aminocarbonyloxy, aminosulfonyl, mono- or di(C1-4alkyl)aminosulfonyl, dioxolanyl optionally substituted with one or two C1-6alkyl radicals, and a heterocycle selected from pyrrolidinyl, pyrrolyl, dihydropyrrolyl, thiazolidinyl, imidazolyl, triazolyl, piperidinyl, homopiperidinyl, piperazinyl, pyridyl and tetrahydropyridyl, which each 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; 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.
摘要翻译：本发明涉及对呼吸道合胞病毒复制具有抑制活性的氨基苯并咪唑，其具有其前药，N-氧化物，加成盐，季胺，金属络合物和立体化学异构体形式，其中Q为Ar 1或C 1-6烷基取代具有一个或多个选自三氟甲基，C 3-7环烷基，Ar 2，羟基，C 1-4烷氧基，C 1-4烷硫基，Ar 2 - 氧基 - ，Ar 2 - 硫基 - ，Ar 2（CH 2）n羟基，Ar 2（CH 2）n硫基，羟基羰基，氨基羰基，C 1-4烷基羰基，Ar 2 - 羰基，C 1-4烷氧基羰基，Ar 2（CH 2）n羰基，氨基羰基氧基，C 1-4烷基羰基氧基，Ar 2 - 羰基氧基，Ar 2（CH 2）n - 羰基氧基，羟基-C 2-4 4-烷氧基，C 1-4烷氧基羰基（CH 2）一或二（C 1-4烷基） - 氨基羰基，一或二（C 1-4烷基）氨基羰基氧基，氨基磺酰基，一或二（C 1-4烷基）氨基磺酰基，任选被一个或两个C 1-6烷基取代的二氧戊环基，选自吡咯烷基，吡咯基，二氢吡咯基，噻唑烷基的杂环，咪唑基，三唑基，哌啶基，高哌啶基，哌嗪基，吡啶基和四氢吡啶基，其各自可以任选被氧代或C 1-6烷基取代; G是直接键或任选取代的C 1-10烷二基R 1是Ar 1或单环或双环杂环; R2a和R3a之一是C1-6烷基，R2a和R3a中的另一个是氢; 在R2a不同于氢的情况下，则R2b为氢或C1-6烷基，R3b为氢; 在R3a不同于氢的情况下，R 3b是氢或C 1-6烷基，R 2b是氢; Ar 1是苯基或取代的苯基，Ar 2是苯基或取代的苯基。它还涉及它们的制备方法和包含它们的组合物，以及它们作为药物的用途。

16. 发明授权

US08497270B2 Macrocyclic integrase inhibitors 有权
标题翻译：大环整合酶抑制剂
公开(公告)号：US08497270B2
公开(公告)日：2013-07-30
申请号：US13395891
申请日：2010-10-13
申请人： Johannes Wilhelmus J Thuring , Jean-Francois Bonfanti , Jerome Michel Claude Fortin
发明人： Johannes Wilhelmus J Thuring , Jean-Francois Bonfanti , Jerome Michel Claude Fortin
IPC分类号： C07D471/18 , C07D498/18 , C07D513/18 , C07D515/18 , C07D498/22 , A61K31/547 , A61P31/18
CPC分类号： C07D513/18 , C07D471/18 , C07D498/18 , C07D498/22 , C07D515/18
摘要： Compound having formula (I), wherein —W is NH—, —N(CH3)— or piperazine, —X is a bond, —C(═O)— or S(═O)2—, —Y is C3-7alkylene, and —Z is NH—C(═O)— or —O—, and pharmaceutically acceptable salts thereof, their pharmaceutical formulations and use as HIV inhibitors.
摘要翻译：具有式（I）的化合物，其中-W是NH-，-N（CH 3） - 或哌嗪，-X是键，-C（= O） - 或S（= O）2 - ， - 7亚烷基和-Z是NH-C（= O） - 或-O-，及其药学上可接受的盐，它们的药物制剂和用作HIV抑制剂。

17. 发明申请

US20080146564A1 1,3-Dihydro-Benzimidazol-2-Ylidene Amines as Inhibitors of Respiratory Syncytial Virus Replication 有权
公开(公告)号：US20080146564A1
公开(公告)日：2008-06-19
申请号：US11908538
申请日：2006-03-17
申请人： Jean-Francois Bonfanti , Jerome Michel Claude Portin , Ismet Dorange
发明人： Jean-Francois Bonfanti , Jerome Michel Claude Portin , Ismet Dorange
IPC分类号： A61K31/5377 , C07D215/00 , A61K31/47 , C07D221/00 , A61K31/4523 , A61P31/12 , C07D213/02 , A61K31/4427 , C07D295/00
CPC分类号： C07D401/06 , C07D235/30 , C07D401/14
摘要： Novel 1,3-dihydro-benzimidazol-2-ylidene amine derivatives of formula the addition salts and stereochemically isomeric forms wherein each Alk is C1-6alkanediyl; Q is hydrogen; C1-6alkyl substituted with one or two Ar2 radicals; CI1-6alkyl substituted with quinolinyl, oxazolidinyl, thiazolidinyl, morpholinyl, thiomorpholinyl, or with pyrrolidinonyl; —CO—Ar2; or Q is a radical of formula wherein t is 1, 2 or 3; R4 is amino, mono- or di(C1-6alkyl)amino; R1 is Ar2, —CO—Ar2 or a monocyclic or bicyclic heterocycle which may optionally be substituted; R2 is as R1 and additionally can be hydrogen; where Q is other than hydrogen, R3 is hydrogen; and where Q is other than hydrogen, R3 is a radical: wherein R6 is hydrogen, C1-6alkyl, substituted C1-6alkyl; R7, R8, R9 are halo, cyano, C1-6alkyl, substituted C1-6alkyl, C2-6alkenyl, cyanoC2-6alkenyl, C2-6alkynyl, cyanoC2 6alkynyl, Ar1, R10a—0—, R10a —S—, —N(R5aR5b), R10a—O—C(═O)—, N(R5aR5b)—C(═O)—, R10a—C(═O)—NR5b1', R10b—C(═O)—O—; and R8 and/or R9 may also be hydrogen; which are RSV inhibitors. Compositions containing these compounds and processes for preparing these compounds and compositions.

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