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1. 发明申请

US20100092426A1 2-SUBSTITUTED BENZIMIDAZOLES 有权
公开(公告)号：US20100092426A1
公开(公告)日：2010-04-15
申请号：US11993136
申请日：2006-06-20
申请人： Jean-Francois Bonfanti , Philippe Muller , Jérôme Michel Claude Fortin , Frédéric Marc Maurice Doublet
发明人： Jean-Francois Bonfanti , Philippe Muller , Jérôme Michel Claude Fortin , Frédéric Marc Maurice Doublet
IPC分类号： C07D401/06 , C07D413/14 , A61K31/5377 , A61K31/4439 , A61P31/12 , A61K38/21 , A61K38/19
CPC分类号： C07D401/06 , C07D235/30
摘要： Inhibitors of RSV replication of formula (I) the addition salts and stereochemically isomeric forms thereof, wherein Q is hydrogen, C1-6alkyl optionally substituted with a heterocycle or Q is C1-6alkyl substituted with both —OR4 and a heterocycle; wherein said heterocycle is oxazolidine, thiazolidine, 1-oxo-thiazolidine, 1,1-dioxothiazolidine, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxothiomorpholinyl, hexahydrooxazepine, hexahydro-thiazepine, 1-oxo-hexahydrothiazepine, 1,1-dioxo-hexahydrothiazepine, pyrrolidine, piperidine, homopiperidine, piperazine; which heterocyle may be substituted with 1-2 substituents; each Alk is C1-6alkanediyl; R1 is Ar2 or optionally substituted piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, pyridyl, pyrazinyl, pyridazinyl, pyrimidinyl, furanyl, tetrahydro-furanyl, thienyl, pyrrolyl, thiazolyl, oxazolyl, imidazolyl, isothiazolyl, pyrazolyl, isoxazolyl, oxadiazolyl, quinolinyl, quinoxalinyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzthiazolyl, pyridopyridyl, naphthiridinyl, 1H-imidazo[4,5-b]pyridinyl, 3H-imidazo[4,5-b]pyridinyl, imidazo[1,2-a]pyridinyl or 2,3-dihydro-1,4-dioxino[2,3-b]pyridyl; R3 is hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, cyanoC1-6alkyl, aminocarbonyl-C1-6-alkyl, mono- or di(C1-6alkyl)aminocarbonyl-C1-6-alkyl, carboxyl-C1-6-alkyl, C1-6alkoxycarbonyl-C1-6alkyl; R2 is hydrogen or C1-6alkyl; R3 and R4 are hydrogen, C1-6alkyl, Ar2, Ar2C1-6alkyl, C1-6alkylcarbonyl, Ar2carbonyl, Ar2C1-6alkylcarbonyl, C1-6alkylsulfonyl, aminosulfonyl, Ar1sulfonyl, Ar1C1-6alkylsulfonyl, C1-6alkyloxyC1-6alkyl, aminoC1-6alkyl, mono- or di(C1-6alkyl)-aminoC1-6alkyl, hydroxyC1-6alkyl, aminocarbonylC1-6alkyl, C1-4alkyloxycarbonyl-C1-6alkyl, hydroxycarbonylC1-6alkyl, aminosulfonylC1-6alkyl, Het, Het-C1-6alkyl, Het-carbonyl, Het-sulfonyl, HetC1-6alkylsulfonyl, Het-C1-6alkylcarbonyl; Het is an optionally substituted heterocycle; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I).

2. 发明授权

US08883837B2 Morpholinyl containing benzimidazoles as inhibitors of respiratory syncytial virus replication 有权
标题翻译：含有吗啉基的苯并咪唑作为呼吸道合胞病毒复制的抑制剂
公开(公告)号：US08883837B2
公开(公告)日：2014-11-11
申请号：US12140686
申请日：2008-06-17
申请人： Jean-Francois Bonfanti , Koenraad Jozef Lodewijk Andries , Jérôme Michel Claude Fortin , Philippe Muller , Frédéric Marc Maurice Doublet , Christophe Meyer , Rudy Edmond Willebrords , Tom Valerius Josepha Gevers , Philip Maria Martha Bern Timmerman
发明人： Jean-Francois Bonfanti , Koenraad Jozef Lodewijk Andries , Jérôme Michel Claude Fortin , Philippe Muller , Frédéric Marc Maurice Doublet , Christophe Meyer , Rudy Edmond Willebrords , Tom Valerius Josepha Gevers , Philip Maria Martha Bern Timmerman
IPC分类号： A01N43/52 , A61K31/415 , C07D233/00 , C07D235/02 , C07D487/04 , C07D487/06 , C07D413/12
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. It further concerns the preparation thereof and compositions comprising these compounds, as well as the use thereof as a medicine.
摘要翻译：本发明涉及对具有对呼吸道合胞病毒复制具有抑制活性的含有吗啉基的苯并咪唑，其具有前药，N-氧化物，加成盐，季胺，金属络合物或其立体化学异构形式。还涉及其制备方法和包含这些化合物的组合物，以及作为药物的用途。

3. 发明申请

US20100183552A1 1-[2-AMINO-3-(SUBSTITUTED ALKYL)-3H-BENZIMIDAZOLYLMETHYL]-3-SUBSTITUTED-1,3-DIHYDRO-BENZOIMIDAZOL-2-ONES AND STRUCTURAL ANALOGS 有权
标题翻译： 1- [2-氨基-3-（取代的烷基）-3H-苯并咪唑基]乙基] -3-取代的1,3-二氢苯并咪唑-2-酮和结构模拟物
公开(公告)号：US20100183552A1
公开(公告)日：2010-07-22
申请号：US11993109
申请日：2006-06-20
申请人： Jean-François Bonfanti , Philippe Muller , Jérôme Michel Claude Fortin , Frédéric Marc Maurice Doublet
发明人： Jean-François Bonfanti , Philippe Muller , Jérôme Michel Claude Fortin , Frédéric Marc Maurice Doublet
IPC分类号： A61K38/21 , A61K38/19 , A61P31/12 , C07D471/04 , A61K31/437 , C07D413/14 , A61K31/5377
CPC分类号： C07D471/04 , C07D401/14
摘要： Inhibitors of RSV replication of formula (I) which can be represented by formula (I) the salts and stereochemically isomeric forms thereof, wherein R is a radical of formula Q is hydrogen or C1-6alkyl optionally substituted with a heterocycle or Q is C1-6alkyl substituted with both a radical —OR4 and a heterocycle; Alk is C1-6alkanediyl; X is O or S; -a1=a2-a3=a4- is —N═CH—CH═CH—, —CH═N—CH═CH—, —CH═CH—N═CH— or —CH═CH—CH═N—; R1 is Ar or a heterocycle; R2 is hydrogen, C1-6alkyl, substituted C1-6alkyl, C3-7cycloalkyl; R3 is hydrogen, C1-6alkyl, cyano, aminocarbonyl, polyhaloC1-6alkyl, C2-6alkenyl or C2-6alkynyl; R4 is hydrogen or C1-6alkyl; Ar is phenyl or substituted phenyl; Het is a heterocycle; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I).
摘要翻译：式（I）的RSV复制抑制剂，其可以由式（I）表示其盐和立体化学异构形式，其中R是式Q的基团是氢或任选被杂环取代的C 1-6烷基或Q是C1- 被烷基和-OR4基团取代的6个烷基; Alk是C1-6烷二基; X是O或S; -a1 = a2-a3 = a4-是-N = CH-CH = CH-，-CH = N-CH = CH-，-CH = CH-N = CH-或-CH = CH-CH = N- R1是Ar或杂环; R 2是氢，C 1-6烷基，取代的C 1-6烷基，C 3-7环烷基; R3是氢，C1-6烷基，氰基，氨基羰基，多卤代C 1-6烷基，C 2-6烯基或C 2-6炔基; R4是氢或C1-6烷基; Ar是苯基或取代的苯基; Het是杂环; 含有化合物（I）的药物组合物和制备化合物（I）的方法。

4. 发明授权

US08278455B2 5- or 6-substituted benzimidazole derivatives as inhibitors of respiratory syncytial virus replication 有权
标题翻译： 5-或6-取代的苯并咪唑衍生物作为呼吸道合胞病毒复制的抑制剂
公开(公告)号：US08278455B2
公开(公告)日：2012-10-02
申请号：US12253450
申请日：2008-10-17
申请人： Jean-François Bonfanti , Koenraad Jozef Lodewijk Andries , Jérôme Michel Claude Fortin , Philippe Muller , Frédéric Marc Maurice Doublet , Christophe Meyer , Rudy Edmond Willebrords , Tom Valerius Josepha Gevers , Philip Maria Martha Bern Timmerman
发明人： Jean-François Bonfanti , Koenraad Jozef Lodewijk Andries , Jérôme Michel Claude Fortin , Philippe Muller , Frédéric Marc Maurice Doublet , Christophe Meyer , Rudy Edmond Willebrords , Tom Valerius Josepha Gevers , Philip Maria Martha Bern Timmerman
IPC分类号： A61K31/4439 , C07D401/06
CPC分类号： C07D401/06 , C07D401/14 , C07D405/14
摘要： The present invention concerns 5- or 6-substituted-benzimidazole derivatives 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 Q is Ar2, R6, pyrrolidinyl substituted with R6, piperidinyl substituted with R6 or homopiperidinyl substituted with R6, G is a direct bond or optionally substituted C1-10alkanediyl; R1 is Ar1 or a monocyclic or bicyclic heterocycle; one of R2a and R2b is cyanoC1-6alkyl, cyanoC2-6alkenyl, Ar3C1-6alkyl, Het1C1-6alkyl, N(R8aR8b)C1-6alkyl, Ar3C2-6alkenyl, Het1C2-6alkenyl, Ar3aminoC1-6alkyl, Het1aminoC1-6alkyl, Ar3thioC1-6alkyl, Het1thioC1-6alkyl, Ar3sulfonylC1-6alkyl, Het1sulfonylC1-6alkyl, Ar3aminocarbonyl, Het1aminocarbonyl, Ar3(CH2)namino-carbonyl, Het1(CH2)naminocarbonyl, Ar3carbonylamino, Het1carbonylamino, Ar3(CH2)ncarbonylamino, Het1(CH2)ncarbonylamino, and the other one of R2a and R2b is hydrogen; in case R2a is hydrogen, then R3 is hydrogen; in case R2b is hydrogen, the R3 is hydrogen or C1-6alkyl. 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5-或6-取代苯并咪唑衍生物，其具有前药，N-氧化物，加成盐，季胺，金属络合物或其立体化学异构形式，其中Q 是Ar 2，R 6，被R 6取代的吡咯烷基，被R 6取代的哌啶基或被R 6取代的高哌啶基，G是直接键或任意取代的C 1-10烷二基; R1是Ar1或单环或双环杂环; R2a和R2b之一是氰基C 1-6烷基，氰基C 2-6烯基，Ar 3 C 1-6烷基，Het 1 C 1-6烷基，N（R 8 a R 8 b）C 1-6烷基，Ar 3 C 2-6烯基，Het 1 C 2-6烯基，Ar 3氨基C 1-6烷基，Het 1氨基C 1-6烷基，Ar 3硫代C 1-6烷基，（CH 2）n氨基 - 羰基，Het 1（CH 2）n氨基羰基，Ar 3羰基氨基，Het 1羰基氨基，Ar 3（CH 2）n - 羰基氨基，Het 1（CH 2）n - 羰基氨基，和另一个（CH 2）n C 1 -C 6烷基， R2a和R2b是氢; 在R2a为氢的情况下，R3为氢; 在R2b为氢的情况下，R3为氢或C1-6烷基。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。

5. 发明授权

US07884215B2 2-substituted benzimidazoles 有权
公开(公告)号：US07884215B2
公开(公告)日：2011-02-08
申请号：US11993136
申请日：2006-06-20
申请人： Jean-François Bonfanti , Philippe Muller , Jérôme Michel Claude Fortin , Frédéric Marc Maurice Doublet
发明人： Jean-François Bonfanti , Philippe Muller , Jérôme Michel Claude Fortin , Frédéric Marc Maurice Doublet
IPC分类号： C07D295/00
CPC分类号： C07D401/06 , C07D235/30
摘要： Inhibitors of RSV replication of formula (I) the addition salts and stereochemically isomeric forms thereof, wherein Q is hydrogen, C1-6alkyl optionally substituted with a heterocycle or Q is C1-6alkyl substituted with both —OR4 and a heterocycle; wherein said heterocycle is oxazolidine, thiazolidine, 1-oxo-thiazolidine, 1,1-dioxothiazolidine, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxothiomorpholinyl, hexahydrooxazepine, hexahydro-thiazepine, 1-oxo-hexahydrothiazepine, 1,1-dioxo-hexahydrothiazepine, pyrrolidine, piperidine, homopiperidine, piperazine; which heterocyle may be substituted with 1-2 substituents; each Alk is C1-6alkanediyl; R1 is Ar2 or optionally substituted piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, pyridyl, pyrazinyl, pyridazinyl, pyrimidinyl, furanyl, tetrahydro-furanyl, thienyl, pyrrolyl, thiazolyl, oxazolyl, imidazolyl, isothiazolyl, pyrazolyl, isoxazolyl, oxadiazolyl, quinolinyl, quinoxalinyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzthiazolyl, pyridopyridyl, naphthiridinyl, 1H-imidazo[4,5-b]pyridinyl, 3H-imidazo[4,5-b]pyridinyl, imidazo[1,2-a]pyridinyl or 2,3-dihydro-1,4-dioxino[2,3-b]pyridyl; R3 is hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, cyanoC1-6alkyl, aminocarbonyl-C1-6-alkyl, mono- or di(C1-6alkyl)aminocarbonyl-C1-6-alkyl, carboxyl-C1-6-alkyl, C1-6alkoxycarbonyl-C1-6alkyl; R2 is hydrogen or C1-6alkyl; R3 and R4 are hydrogen, C1-6alkyl, Ar2, Ar2C1-6alkyl, C1-6alkylcarbonyl, Ar2carbonyl, Ar2C1-6alkylcarbonyl, C1-6alkylsulfonyl, aminosulfonyl, Ar1sulfonyl, Ar1C1-6alkylsulfonyl, C1-6alkyloxyC1-6alkyl, aminoC1-6alkyl, mono- or di(C1-6alkyl)-aminoC1-6alkyl, hydroxyC1-6alkyl, aminocarbonylC1-6alkyl, C1-4alkyloxycarbonyl-C1-6alkyl, hydroxycarbonylC1-6alkyl, aminosulfonylC1-6alkyl, Het, Het-C1-6alkyl, Het-carbonyl, Het-sulfonyl, HetC1-6alkylsulfonyl, Het-C1-6alkylcarbonyl; Het is an optionally substituted heterocycle; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I).

6. 发明授权

US08178694B2 Heterocyclylaminoalkyl substituted benzimidazoles 有权
公开(公告)号：US08178694B2
公开(公告)日：2012-05-15
申请号：US11993126
申请日：2006-06-20
申请人： Jean-François Bonfanti , Philippe Muller , Jérôme Michel Claude Fortin , Frédéric Marc Maurice Doublet
发明人： Jean-François Bonfanti , Philippe Muller , Jérôme Michel Claude Fortin , Frédéric Marc Maurice Doublet
IPC分类号： A61K31/5377 , C07D413/14
CPC分类号： C07D401/06 , C07D401/14
摘要： Heterocyclylaminoalkyl Substituted Benzimidazoles Inhibitors of RSV replication of formula (I): The salts and stereochemically isomeric forms thereof, wherein Q is hydrogen, C1-6alkyl optionally substituted with a heterocycle or Q is C1-6alkyl substituted with both —OR4 and a heterocycle; wherein said heterocycle is oxazolidine, thiazolidine, 1-oxo-thiazolidine, 1,1-dioxothiazolidine, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxothiomorpholinyl, hexahydrooxazepine, hexahydrothiazepine, 1-oxo-hexahydrothiazepine, 1,1-dioxo-hexahydrothiazepine, pyrrolidine, piperidine, homopiperidine, piperazine; which heterocyle may be substituted with 1-2 substituents; each Alk is C1-6alkanediyl; R1 is Ar or optionally substituted piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, pyridyl, pyrazinyl, pyridazinyl, pyrimidinyl, furanyl, tetrahydrofuranyl, thienyl, pyrrolyl, thiazolyl, oxazolyl, imidazolyl, isothiazolyl, pyrazolyl, isoxazo lyl, oxadiazolyl, quinolinyl, quinoxalinyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzthiazolyl, pyridopyridyl, naphthiridinyl, 1H-imidazo[4,5-b]pyridinyl, 3H-imidazo[4,5-b]pyridinyl, imidazo[1,2-a]pyridinyl or 2,3-dihydro-1,4-dioxino[2,3-b]pyridyl; R3 is hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, cyanoC1-6alkyl, aminocarbonyl-C1-6-alkyl, mono- or di(C1-6alkyl)aminocarbonyl-C1-6-alkyl, carboxyl-C1-6-alkyl, C1-6alkoxycarbonyl-C1-6 alkyl; R2, R4 and R5 are hydrogen or C1-6alkyl; Het is pyridyl, pyrazinyl, pyridazinyl, pyrimidinyl, furanyl, tetrahydrofuranyl, thienyl, pyrrolyl, thiazolyl, oxazolyl, imidazolyl, isothiazolyl, pyrazolyl, isoxazolyl, oxadiazolyl, quinolinyl, quinoxalinyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazo lyl, benzthiazolyl, pyridopyridyl, naphthiridinyl, 1H-imidazo[4,5-b]-pyridinyl, 3H-imidazo[4,5-b]pyridinyl, imidazo[1,2-a]pyridinyl and 2,3-dihydro-1,4-dioxino[2,3-b]pyridyl; Ar is optionally substituted phenyl; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I).

7. 发明授权

US08034835B2 1-[[2-amino-3-(substituted alkyl)-3H-benzimidazolyl[methyl]-3-substituted-1,3-dihydro-benzoimidazol-2-ones and structural analogs 有权
标题翻译： 1 - [[2-氨基-3-（取代的烷基）-3H-苯并咪唑基[甲基] -3-取代-1,3-二氢 - 苯并咪唑-2-酮和结构类似物
公开(公告)号：US08034835B2
公开(公告)日：2011-10-11
申请号：US11993109
申请日：2006-06-20
申请人： Jean-François Bonfanti , Philippe Muller , Jérôme Michel Claude Fortin , Frédéric Marc Maurice Doublet
发明人： Jean-François Bonfanti , Philippe Muller , Jérôme Michel Claude Fortin , Frédéric Marc Maurice Doublet
IPC分类号： C07D235/04 , C07D403/02 , A01N43/52 , A61K31/415
CPC分类号： C07D471/04 , C07D401/14
摘要： Inhibitors of RSV replication of formula (I) which can be represented by formula (I) the salts and stereochemically isomeric forms thereof, wherein R is a radical of formula Q is hydrogen or C1-6alkyl optionally substituted with a heterocycle or Q is C1-6alkyl substituted with both a radical —OR4 and a heterocycle; Alk is C1-6alkanediyl; X is O or S; -a1=a2-a3=a4- is —N═CH—CH═CH—, —CH═N—CH═CH—, —CH═CH—N═CH— or —CH═CH—CH═N—; R1 is Ar or a heterocycle; R2 is hydrogen, C1-6alkyl, substituted C1-6alkyl, C3-7cycloalkyl; R3 is hydrogen, C1-6alkyl, cyano, aminocarbonyl, polyhaloC1-6alkyl, C2-6alkenyl or C2-6alkynyl; R4 is hydrogen or C1-6alkyl; Ar is phenyl or substituted phenyl; Het is a heterocycle; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I).
摘要翻译：式（I）的RSV复制抑制剂，其可以由式（I）表示其盐和立体化学异构形式，其中R是式Q的基团是氢或任选被杂环取代的C 1-6烷基或Q是C1- 被烷基和-OR4基团取代的6个烷基; Alk是C1-6烷二基; X是O或S; -a1 = a2-a3 = a4-是-N = CH-CH = CH-，-CH = N-CH = CH-，-CH = CH-N = CH-或-CH = CH-CH = N- R1是Ar或杂环; R 2是氢，C 1-6烷基，取代的C 1-6烷基，C 3-7环烷基; R3是氢，C1-6烷基，氰基，氨基羰基，多卤代C 1-6烷基，C 2-6烯基或C 2-6炔基; R4是氢或C1-6烷基; Ar是苯基或取代的苯基; Het是杂环; 含有化合物（I）的药物组合物和制备化合物（I）的方法。

8. 发明授权

US07449463B2 Morpholinyl containing benzimidazoles as inhibitors of respiratory syncytial virus replication 有权
公开(公告)号：US07449463B2
公开(公告)日：2008-11-11
申请号：US10563691
申请日：2004-12-20
申请人： Jean-François Bonfanti , Koenraad Jozef Lodewijk Andries , Jérôme Michel Claude Fortin , Philippe Muller , Frédéric Marc Maurice Doublet , Christophe Meyer , Rudy Edmond Willebrords , Tom Valerius Josepha Gevers , Philip Maria Martha Bern Timmerman
发明人： Jean-François Bonfanti , Koenraad Jozef Lodewijk Andries , Jérôme Michel Claude Fortin , Philippe Muller , Frédéric Marc Maurice Doublet , Christophe Meyer , Rudy Edmond Willebrords , Tom Valerius Josepha Gevers , Philip Maria Martha Bern Timmerman
IPC分类号： A61K31/535 , C07D413/00
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.

9. 发明授权

US07956196B2 1,3-dihydro-benzimidazol-2-ylidene amines as inhibitors of respiratory syncytial virus replication 有权
标题翻译： 1,3-二氢 - 苯并咪唑-2-亚基胺作为呼吸道合胞病毒复制的抑制剂
公开(公告)号：US07956196B2
公开(公告)日：2011-06-07
申请号：US11908538
申请日：2006-03-17
申请人： Jean-François Bonfanti , Jérôme Michel Claude Fortin , Ismet Dorange
发明人： Jean-François Bonfanti , Jérôme Michel Claude Fortin , Ismet Dorange
IPC分类号： A61K31/4184 , A61K31/5377 , C07D235/30 , C07D401/12 , C07D401/14 , C07D413/14
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; C1-6alkyl 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)—NR5b—, 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.
摘要翻译：新的1,3-二氢 - 苯并咪唑-2-亚基胺衍生物，其加成盐和立体化学异构形式，其中每个Alk是C 1-6烷二基; Q是氢; 被一个或两个Ar 2基团取代的C 1-6烷基; 用喹啉基，恶唑烷基，噻唑烷基，吗啉基，硫代吗啉基或吡咯烷基取代的C 1-6烷基; -CO-Ar2; 或Q是式的基团，其中t是1,2或3; R4是氨基，单或二（C1-6烷基）氨基; R 1是Ar 2，-CO-Ar 2或可任选被取代的单环或双环杂环; R2是R1，另外可以是氢; 其中Q不是氢，R3是氢; 并且其中Q不是氢，R 3是基团：其中R 6是氢，C 1-6烷基，取代的C 1-6烷基; R 7，R 8，R 9为卤素，氰基，C 1-6烷基，取代的C 1-6烷基，C 2-6烯基，氰基C 2-6烯基，C 2-6炔基，氰基C 2-6炔基，Ar 1，R 10a-O-，R 10a-S，），R 10a-O-C（= O） - ，N（R 5a，R b）-C（= O） - ，R 10 a -C（= O）-NR 5 b - ，R 10 b -C（= O）并且R 8和/或R 9也可以是氢; 其为RSV抑制剂。含有这些化合物的组合物和制备这些化合物和组合物的方法。

10. 发明授权

US06911444B2 Non-steroidal IL-5 inhibitors, processes and intermediates for their preparation and pharmaceutical compositions comprising said inhibitors 失效
标题翻译：非甾体IL-5抑制剂，其制备方法和中间体以及包含所述抑制剂的药物组合物
公开(公告)号：US06911444B2
公开(公告)日：2005-06-28
申请号：US10075876
申请日：2002-02-14
申请人： Jean Fernand Armand Lacrampe , Eddy Jean Edgard Freyne , Frederik Dirk Deroose , Jérôme Michel Claude Fortin , Erwin Coesemans
发明人： Jean Fernand Armand Lacrampe , Eddy Jean Edgard Freyne , Frederik Dirk Deroose , Jérôme Michel Claude Fortin , Erwin Coesemans
IPC分类号： C07D413/10 , A61K31/53 , A61K31/5377 , A61K51/04 , A61P1/02 , A61P1/04 , A61P11/06 , A61P11/08 , A61P15/02 , A61P17/06 , A61P27/02 , A61P27/16 , A61P37/08 , A61P43/00 , C07D417/10 , C07D417/14 , C07D253/075
CPC分类号： A61K51/0491 , A61K51/0461 , A61K51/0463 , A61K51/0468 , C07D417/10 , C07D417/14
摘要： The present invention relates to IL-5 inhibiting 6-azauracil derivatives useful for treating eosinophil-dependent inflammatory diseases, to processes and intermediates for their preparation as well as to pharmaceutical compositions comprising the said derivatives. It further relates to the use of such derivatives as a medicine, and to processes for marking a receptor or imaging an organ using the said derivatives.
摘要翻译：本发明涉及用于治疗嗜酸性粒细胞依赖性炎性疾病的IL-5抑制性6-氮尿嘧啶衍生物，其制备方法和中间体以及包含所述衍生物的药物组合物。它还涉及这样的衍生物作为药物的使用，以及使用所述衍生物标记受体或成像器官的方法。

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