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21. 发明授权

US07355051B2 Piperdine-amino-benzimidazole derivatives as inhibitors of respiratory syncytial virus replication 有权
公开(公告)号：US07355051B2
公开(公告)日：2008-04-08
申请号：US10596519
申请日：2004-12-20
申请人： Jean-François Bonfanti , Koenraad Jozef Lodewijk Andries , Frans Eduard Janssens , François Maria Sommen , Jerôme Emile Georges Guillemont , Jean Fernand Armand Lacrampe
发明人： Jean-François Bonfanti , Koenraad Jozef Lodewijk Andries , Frans Eduard Janssens , François Maria Sommen , Jerôme Emile Georges Guillemont , Jean Fernand Armand Lacrampe
IPC分类号： C07D401/106
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, C1−4alkyl-carbonyl, 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.

22. 发明授权

US08604200B2 Diaza-spiro-{4,4}-nonane derivatives as neurokinin (NK1) antagonists 失效
标题翻译： Diaza-spiro- {4,4} - 壬烷衍生物作为神经激肽（NK1）拮抗剂
公开(公告)号：US08604200B2
公开(公告)日：2013-12-10
申请号：US11886175
申请日：2006-03-03
申请人： Frans Eduard Janssens , Sophie Coupa , Alain Philippe Poncelet , Yvan Rene Ferdinand Simonnet , Bruno Schoentjes
发明人： Frans Eduard Janssens , Sophie Coupa , Alain Philippe Poncelet , Yvan Rene Ferdinand Simonnet , Bruno Schoentjes
IPC分类号： C07D215/00 , C07D217/00 , C07D219/00 , C07D221/00 , A01N43/42 , A61K31/44
CPC分类号： C07D487/08
摘要： This invention concerns substituted diaza-spiro-[4.4]-nonane derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nociception, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, chronic obstructive pulmonary disease (COPD) and micturition disorders such as urinary incontinence. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1.
摘要翻译：本发明涉及具有神经激肽拮抗活性的具有神经激肽拮抗活性的取代的二氮杂螺 - [4.4] - 壬烷衍生物，特别是NK1拮抗活性，其制备方法，包含它们的组合物及其作为药物的用途，特别是用于治疗和/或预防精神分裂症，呕吐，焦虑和抑郁，肠易激综合征（IBS），昼夜节律紊乱，先兆子痫，伤害感受，疼痛，特别是内脏和神经性疼痛，胰腺炎，神经源性炎症，哮喘，慢性阻塞性肺病（COPD）和排尿障碍作为尿失禁。根据本发明的化合物可以由通式（I）表示，并且还包括其药学上可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式及其前药，其中所有取代基定义为在权利要求1中。

23. 发明授权

US07612056B2 Substituted diaza-spiro-[4.5]-decane derivatives and their use as neurokinin antagonists 失效
标题翻译：取代的二氮 - 螺 - [4.5] - 癸烷衍生物及其作为神经激肽拮抗剂的用途
公开(公告)号：US07612056B2
公开(公告)日：2009-11-03
申请号：US11547705
申请日：2005-04-04
申请人： Frans Eduard Janssens , Bruno Schoentjes , Sophie Coupa , Alain Philippe Poncelet , Yvan René Ferdinand Simonnet
发明人： Frans Eduard Janssens , Bruno Schoentjes , Sophie Coupa , Alain Philippe Poncelet , Yvan René Ferdinand Simonnet
IPC分类号： A61K31/44
CPC分类号： C07D471/10
摘要： This invention concerns substituted diaza-spiro-[4.5]-decane derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK2 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nociception, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, chronic obstructive pulmonary disease (COPD) and micturition disorders such as urinary incontinence.The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
摘要翻译：本发明涉及具有神经激肽拮抗活性，特别是NK1拮抗活性，组合NK1 / NK2拮抗活性，组合NK1 / NK3拮抗活性和组合NK1 / NK2 / NK3拮抗活性的取代的二氮 - 螺 - [4.5] - 癸烷衍生物，它们的制剂，包含它们的组合物及其作为药物的用途，特别是用于治疗和/或预防精神分裂症，呕吐，焦虑和抑郁，肠易激综合征（IBS），昼夜节律紊乱，先兆子痫，伤害感受，疼痛，特别是内脏和神经性疼痛，胰腺炎，神经源性炎症，哮喘，慢性阻塞性肺病（COPD）和排尿障碍如尿失禁。根据本发明的化合物可以由通式（I）表示，并且还包括其药学上可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式及其前药，其中所有取代基定义为在权利要求1中。

24. 发明授权

US07407969B2 Respiratory syncytial virus replication inhibitors 失效
公开(公告)号：US07407969B2
公开(公告)日：2008-08-05
申请号：US11247392
申请日：2005-10-11
申请人： Frans Eduard Janssens , Jean Fernand Armand Lacrampe , Jerome Emile Geroges Guilemont , Marc G Venet , Koenraad Jozef Lodewijk Marcel Andries
发明人： Frans Eduard Janssens , Jean Fernand Armand Lacrampe , Jerome Emile Geroges Guilemont , Marc G Venet , Koenraad Jozef Lodewijk Marcel Andries
IPC分类号： A61P11/00 , A61P31/12 , A61K31/4709 , A61K31/4375 , A61K31/437 , A61K31/498 , A61K31/4409 , A61K31/436 , C07D471/04 , C07D417/14 , C07D413/14 , C07D409/14 , C07D401/06 , C07D491/056
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 α 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, arylC1-6alkyl or arylC1-6alkyloxy, R4 is hydrogen, C1-6alkyl or arylC1-6alkyl; 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)S— wherein S is 4 or 5; R6 is hydrogen, C1-4alkyl, formyl, hydroxyC1-6alkyl, C1-6alkylcarbonyl or C1-6alkyloxycarbonyl; aryl is optionally substituted phenyl; Het is pyridyl, pyrimidinyl, pyryzinyl, pyridazinyl; as respiratory syncytial virus replication inhibitors; their preparation, compositions containing them and their use as a medicine.

25. 发明授权

US07173034B2 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：US07173034B2
公开(公告)日：2007-02-06
申请号：US11144126
申请日：2005-06-03
申请人： Frans Eduard Janssens , Kathleen Petrus Marie-José Meersman , François Maria Sommen , Jérôme Emile Georges Guillemont , Jean Fernand Armand Lacrampe , Koenraad Jozef Lodewijk Marcel Andries
发明人： Frans Eduard Janssens , Kathleen Petrus Marie-José Meersman , François Maria Sommen , Jérôme Emile Georges Guillemont , Jean Fernand Armand Lacrampe , Koenraad Jozef Lodewijk Marcel Andries
IPC分类号： C07D401/12 , C07D401/06 , C07D401/14 , A61K31/4184
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 for 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-N-，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为直链或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。

26. 发明申请

US20100004260A1 2-PIPERAZIN-1-YL-3H-IMIDAZO[4,5-B]PYRIDINE DERIVATIVES 有权
标题翻译： 2-PIPERAZIN-1-YL-3H-咪唑并[4,5-B]吡啶衍生物
公开(公告)号：US20100004260A1
公开(公告)日：2010-01-07
申请号：US12523936
申请日：2008-01-24
申请人： Frans Eduard Janssens
发明人： Frans Eduard Janssens
IPC分类号： A61K31/497 , 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。

27. 发明授权

US07390811B2 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：US07390811B2
公开(公告)日：2008-06-24
申请号：US11519719
申请日：2006-09-11
申请人： Frans Eduard Janssens , Kathleen Petrus Marie-José Meersman , François Maria Sommen , Jérôme Emile Georges Guillemont , Jean Fernand Armand Lacrampe , Koenraad Jozef Lodewijk Marcel Andries
发明人： Frans Eduard Janssens , Kathleen Petrus Marie-José Meersman , François Maria Sommen , Jérôme Emile Georges Guillemont , Jean Fernand Armand Lacrampe , Koenraad Jozef Lodewijk Marcel Andries
IPC分类号： C07D401/12 , C07D401/14 , A61K31/4184
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-N-，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。

28. 发明申请

US20080146613A1 PIPERIDINE-AMINO-BENZIMIDAZOLE DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS REPLICATION 审中-公开
公开(公告)号：US20080146613A1
公开(公告)日：2008-06-19
申请号：US12030483
申请日：2008-02-13
申请人： Jean-Francois BONFANTI , Koenraad Jozef Lodewikjk Andries , Frans Eduard Janssens , Francois Maria Sommen , Jerome Emile Georges Guillemont , Jean Fernand Armand Lacrampe
发明人： Jean-Francois BONFANTI , Koenraad Jozef Lodewikjk Andries , Frans Eduard Janssens , Francois Maria Sommen , Jerome Emile Georges Guillemont , Jean Fernand Armand Lacrampe
IPC分类号： A61K31/4545 , A61P31/12
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, C1-4alkyl-carbonyl, Ar2-carbonyl, C1-4alkoxycarbonyl, Ar2(CH2)ncarbonyl, aminocarbonyloxy, C1-4alkylcarbonyloxy, Ar2-carbonyloxy, 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.

29. 发明授权

US07361657B2 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：US07361657B2
公开(公告)日：2008-04-22
申请号：US11332557
申请日：2006-01-12
申请人： Frans Eduard Janssens , Kathleen Petrus Marie-José Meersman , François Maria Sommen , Jérôme Emile Georges Guillemont , Jean Fernand Armand Lacrampe , Koenraad Jozef Lodewijk Marcel Andries
发明人： Frans Eduard Janssens , Kathleen Petrus Marie-José Meersman , François Maria Sommen , Jérôme Emile Georges Guillemont , Jean Fernand Armand Lacrampe , Koenraad Jozef Lodewijk Marcel Andries
IPC分类号： C07D401/12 , C07D401/14 , A61K31/4184
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- 该化合物是式-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为直链或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

30. 发明授权

US07528149B2 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：US07528149B2
公开(公告)日：2009-05-05
申请号：US11625648
申请日：2007-01-22
申请人： Frans Eduard Janssens , Kathleen Petrus Marie-José Meersman , François Maria Sommen , Koenraads Jozef Lodewijk Marcell Andries
发明人： Frans Eduard Janssens , Kathleen Petrus Marie-José Meersman , François Maria Sommen , Koenraads Jozef Lodewijk Marcell Andries
IPC分类号： C07D471/04 , A61K31/437
CPC分类号： C07D401/12 , C07D401/14 , C07D471/04 , Y02P20/55
摘要： This invention concerns compounds of formula (I) prodrugs, addition salts, or stereochemically isomeric forms thereof for use as, inter alia, respiratory syncytial virus replication inhibitors; their preparation, compositions containing them and methods of their use in treating respiratory syncytial viral infections.
摘要翻译：本发明涉及用作呼吸道合胞病毒复制抑制剂等的式（I）化合物前药，加成盐或立体化学异构体形式; 它们的制备方法，含有它们的组合物和它们用于治疗呼吸道合胞病毒感染的方法。

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