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1.发明授权Tetrahydrocarbazole derivatives having improved biological action and improved solubility as ligands of G-protein coupled receptors (GPCRs) 有权具有改善的生物学作用和改善作为G蛋白偶联受体（GPCR）配体的溶解度的四氢咔唑衍生物公开(公告)号：US07375127B2
公开(公告)日：2008-05-20
申请号：US11172142
申请日：2005-06-30
申请人： Klaus Paulini , Matthias Gerlach , Eckhard Günther , Emmanuel Polymeropoulos , Silke Baasner , Peter Schmidt , Ronald Kühne , Arvid Söderhäll
发明人： Klaus Paulini , Matthias Gerlach , Eckhard Günther , Emmanuel Polymeropoulos , Silke Baasner , Peter Schmidt , Ronald Kühne , Arvid Söderhäll
IPC分类号： A61K31/403 , C07D209/82
CPC分类号： C07D209/88 , C07D209/82
摘要： The present invention provides novel tetrahydrocarbazole derivatives which have improved properties and which can be employed as inhibitors of GPCRs. This results in the possibility of using the novel compounds to treat pathological conditions whose severity depends on the pathobiochemical effect of GPCRs. The compounds of the invention act in particular via an antagonistic inhibition of the LHRH receptor. The invention further provides medicaments which comprise one or more of the novel compounds as active ingredient. The medicaments are suitable in particular to be employed in an oral dosage form for a mammal, in particular a human.
摘要翻译： 本发明提供具有改进性质的新型四氢咔唑衍生物，其可用作GPCR的抑制剂。 这导致使用新化合物治疗其严重程度取决于GPCR的病理生化作用的病理状况的可能性。 本发明的化合物特别是通过拮抗LHRH受体的抑制作用。 本发明进一步提供了包含一种或多种新化合物作为活性成分的药物。 药物特别适用于哺乳动物，特别是人的口服剂型。
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2.发明授权Tetrahydrocarbazole derivatives having improved biological action and improved solubility as ligands of G-protein coupled receptors (GPCPs) 有权具有改善的生物学作用和改善作为G蛋白偶联受体（GPCR）配体的溶解度的四氢咔唑衍生物公开(公告)号：US08067456B2
公开(公告)日：2011-11-29
申请号：US12070214
申请日：2008-02-14
申请人： Klaus Paulini , Matthias Gerlach , Eckhard Gunther , Emmanuel Polymeropoulos , Silke Baasner , Peter Schmidt , Ronald Kühne , Arvid Söderhäll
发明人： Klaus Paulini , Matthias Gerlach , Eckhard Gunther , Emmanuel Polymeropoulos , Silke Baasner , Peter Schmidt , Ronald Kühne , Arvid Söderhäll
IPC分类号： A61K31/403 , C07D209/82
CPC分类号： C07D209/88 , C07D209/82
摘要： The present invention provides novel tetrahydrocarbazole derivatives which have improved properties and which can be employed as inhibitors of GPCRs. This results in the possibility of using the novel compounds to treat pathological conditions whose severity depends on the pathobiochemical effect of GPCRs. The compounds of the invention act in particular via an antagonistic inhibition of the LHRH receptor. The invention further provides medicaments which comprise one or more of the novel compounds as active ingredient. The medicaments are suitable in particular to be employed in an oral dosage form for a mammal, in particular a human.
摘要翻译： 本发明提供具有改进性质的新型四氢咔唑衍生物，其可用作GPCR的抑制剂。 这导致使用新化合物治疗其严重程度取决于GPCR的病理生化作用的病理状况的可能性。 本发明的化合物特别是通过拮抗LHRH受体的抑制作用。 本发明进一步提供了包含一种或多种新化合物作为活性成分的药物。 药物特别适用于哺乳动物，特别是人的口服剂型。
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3.发明申请Novel tetrahydrocarbazole derivatives having improved biological action and improved solubility as ligands of G-protein coupled receptors (GPCRs) 有权新型四氢咔唑衍生物具有改善的生物学作用和改善的溶解度，作为G蛋白偶联受体（GPCR）的配体公开(公告)号：US20060014818A1
公开(公告)日：2006-01-19
申请号：US11172142
申请日：2005-06-30
申请人： Klaus Paulini , Matthias Gerlach , Eckhard Günther , Emmanuel Polymeropoulos , Silke Baasner , Peter Schmidt , Ronald Kühne , Arvid Soderhall
发明人： Klaus Paulini , Matthias Gerlach , Eckhard Günther , Emmanuel Polymeropoulos , Silke Baasner , Peter Schmidt , Ronald Kühne , Arvid Soderhall
IPC分类号： A61K31/403 , C07D209/82
CPC分类号： C07D209/88 , C07D209/82
摘要： The present invention provides novel tetrahydrocarbazole derivatives which have improved properties and which can be employed as inhibitors of GPCRs. This results in the possibility of using the novel compounds to treat pathological conditions whose severity depends on the pathobiochemical effect of GPCRs. The compounds of the invention act in particular via an antagonistic inhibition of the LHRH receptor. The invention further provides medicaments which comprise one or more of the novel compounds as active ingredient. The medicaments are suitable in particular to be employed in an oral dosage form for a mammal, in particular a human.
摘要翻译： 本发明提供具有改进性质的新型四氢咔唑衍生物，其可用作GPCR的抑制剂。 这导致使用新化合物治疗其严重程度取决于GPCR的病理生化作用的病理状况的可能性。 本发明的化合物特别是通过拮抗LHRH受体的抑制作用。 本发明进一步提供了包含一种或多种新化合物作为活性成分的药物。 药物特别适用于哺乳动物，特别是人的口服剂型。
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4.发明申请Novel tetrahydrocarbazole derivatives having improved biological action and improved solubility as ligands of G-protein coupled receptors (GPCPs) 有权新型四氢咔唑衍生物具有改善的生物学作用和改善的溶解度，作为G蛋白偶联受体（GPCR）的配体公开(公告)号：US20080280965A1
公开(公告)日：2008-11-13
申请号：US12070214
申请日：2008-02-14
申请人： Klaus Paulini , Matthias Gerlach , Eckhard Gunther , Emmanuel Polymeropoulos , Silke Baasner , Peter Schmidt , Ronald Kuhne , Arvid Soderhall
发明人： Klaus Paulini , Matthias Gerlach , Eckhard Gunther , Emmanuel Polymeropoulos , Silke Baasner , Peter Schmidt , Ronald Kuhne , Arvid Soderhall
CPC分类号： C07D209/88 , C07D209/82
摘要： The present invention provides novel tetrahydrocarbazole derivatives which have improved properties and which can be employed as inhibitors of GPCRs. This results in the possibility of using the novel compounds to treat pathological conditions whose severity depends on the pathobiochemical effect of GPCRs. The compounds of the invention act in particular via an antagonistic inhibition of the LHRH receptor. The invention further provides medicaments which comprise one or more of the novel compounds as active ingredient. The medicaments are suitable in particular to be employed in an oral dosage form for a mammal, in particular a human.
摘要翻译： 本发明提供具有改进性质的新型四氢咔唑衍生物，其可用作GPCR的抑制剂。 这导致使用新化合物治疗其严重程度取决于GPCR的病理生化作用的病理状况的可能性。 本发明的化合物特别是通过拮抗LHRH受体的抑制作用。 本发明进一步提供了包含一种或多种新化合物作为活性成分的药物。 药物特别适用于哺乳动物，特别是人的口服剂型。
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5.发明授权公开(公告)号：US08148546B2
公开(公告)日：2012-04-03
申请号：US12109479
申请日：2008-04-25
申请人： Tilmann Schuster , Klaus Paulini , Peter Schmidt , Silke Baasner , Emmanuel Polymeropoulos , Eckhard Guenther , Michael Teifel
发明人： Tilmann Schuster , Klaus Paulini , Peter Schmidt , Silke Baasner , Emmanuel Polymeropoulos , Eckhard Guenther , Michael Teifel
IPC分类号： C07D209/82 , A61K31/403
CPC分类号： C07K5/06191 , A61K38/00 , C07K5/0827
摘要： The present invention provides novel tetrahydrocarbazole compounds according to formula (I) as ligands of G-protein coupled receptors (GPCR) which are useful in the treatment and/or prophylaxis of physiological and/or pathological conditions in mammals mediated by GPCR or of physiological and/or pathological conditions which can be treated by modulation of these receptors.
摘要翻译： 本发明提供了根据式（I）的新型四氢咔唑化合物作为G蛋白偶联受体（GPCR）的配体，其可用于治疗和/或预防由GPCR介导的哺乳动物的生理和/或病理状况或生理和/ /或可以通过调节这些受体来治疗的病理状况。
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6.发明申请NOVEL TETRAHYDROCARBAZOLE DERIVATIVES AS LIGANDS OF G-PROTEIN COUPLED RECEPTORS 有权新型四氮唑衍生物作为G蛋白偶联受体的配体公开(公告)号：US20090170783A1
公开(公告)日：2009-07-02
申请号：US12109479
申请日：2008-04-25
申请人： Tilmann Schuster , Klaus Paulini , Peter Schmidt , Silke Baasner , Emmanuel Polymeropoulos , Eckhard Guenther , Michael Teifel
发明人： Tilmann Schuster , Klaus Paulini , Peter Schmidt , Silke Baasner , Emmanuel Polymeropoulos , Eckhard Guenther , Michael Teifel
CPC分类号： C07K5/06191 , A61K38/00 , C07K5/0827
摘要： The present invention provides novel tetrahydrocarbazole compounds according to formula (I) as ligands of G-protein coupled receptors (GPCR) which are useful in the treatment and/or prophylaxis of physiological and/or pathological conditions in mammals mediated by GPCR or of physiological and/or pathological conditions which can be treated by modulation of these receptors.
摘要翻译： 本发明提供了根据式（I）的新型四氢咔唑化合物作为G蛋白偶联受体（GPCR）的配体，其可用于治疗和/或预防由GPCR介导的哺乳动物的生理和/或病理状况或生理和/ /或可以通过调节这些受体来治疗的病理状况。
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7.发明授权公开(公告)号：US08541462B2
公开(公告)日：2013-09-24
申请号：US13358055
申请日：2012-01-25
申请人： Tilmann Schuster , Klaus Paulini , Peter Schmidt , Silke Baasner , Emmanuel Polymeropoulos , Eckhard Guenther , Michael Teifel
发明人： Tilmann Schuster , Klaus Paulini , Peter Schmidt , Silke Baasner , Emmanuel Polymeropoulos , Eckhard Guenther , Michael Teifel
IPC分类号： A61K31/403 , C07D209/82
CPC分类号： C07K5/06191 , A61K38/00 , C07K5/0827
摘要： The present invention provides novel tetrahydrocarbazole compounds according to formula (I) as ligands of G-protein coupled receptors (GPCR) which are useful in the treatment and/or prophylaxis of physiological and/or pathological conditions in mammals mediated by GPCR or of physiological and/or pathological conditions which can be treated by modulation of these receptors.
摘要翻译： 本发明提供了根据式（I）的新型四氢咔唑化合物作为G蛋白偶联受体（GPCR）的配体，其可用于治疗和/或预防由GPCR介导的哺乳动物的生理和/或病理状况或生理和/ /或可以通过调节这些受体来治疗的病理状况。
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8.发明申请NOVEL TETRAHYDROCARBAZOLE DERIVATIVES AS LIGANDS OF G-PROTEIN COUPLED RECEPTORS 失效新型四氮唑衍生物作为G蛋白偶联受体的配体公开(公告)号：US20120122763A1
公开(公告)日：2012-05-17
申请号：US13358055
申请日：2012-01-25
申请人： Tilmann SCHUSTER , Klaus Paulini , Peter Schmidt , Silke Baasner , Emmanuel Polymeropoulos , Eckhard Guenther , Michael Teifel
发明人： Tilmann SCHUSTER , Klaus Paulini , Peter Schmidt , Silke Baasner , Emmanuel Polymeropoulos , Eckhard Guenther , Michael Teifel
IPC分类号： A61K38/05 , A61P35/00 , A61P5/00 , A61P17/00 , A61P25/00 , A61P25/28 , A61P1/08 , A61P29/00 , A61P25/06 , A61P25/22 , A61P11/14 , A61P11/06 , A61P9/12 , A61P1/00 , A61P25/24 , A61P19/02 , A61K38/06
CPC分类号： C07K5/06191 , A61K38/00 , C07K5/0827
摘要： The present invention provides novel tetrahydrocarbazole compounds according to formula (I) as ligands of G-protein coupled receptors (GPCR) which are useful in the treatment and/or prophylaxis of physiological and/or pathological conditions in mammals mediated by GPCR or of physiological and/or pathological conditions which can be treated by modulation of these receptors.
摘要翻译： 本发明提供了根据式（I）的新型四氢咔唑化合物作为G蛋白偶联受体（GPCR）的配体，其可用于治疗和/或预防由GPCR介导的哺乳动物的生理和/或病理状况或生理和/ /或可以通过调节这些受体来治疗的病理状况。
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![Substituted pyrido[2,3-b]pyrazine compounds as modulators of tyrosine kinases](/abs-image/US/2012/06/19/US08202883B2/abs.jpg.150x150.jpg)
9.发明授权Substituted pyrido[2,3-b]pyrazine compounds as modulators of tyrosine kinases 失效取代的吡啶并[2,3-b]吡嗪化合物作为酪氨酸激酶的调节剂公开(公告)号：US08202883B2
公开(公告)日：2012-06-19
申请号：US12117942
申请日：2008-05-09
申请人： Matthias Gerlach , Irene Seipelt , Eckhard Guenther , Emmanuel Polymeropoulos , Tilmann Schuster , Eckhard Claus
发明人： Matthias Gerlach , Irene Seipelt , Eckhard Guenther , Emmanuel Polymeropoulos , Tilmann Schuster , Eckhard Claus
IPC分类号： A61K31/44
CPC分类号： C07D471/04
摘要： The invention relates to pyrido[2,3-b]pyrazine compounds of formulae (Ia) and (Ib) which have activity to the modulation of misdirected cellular signal transduction processes such as tyrosine kinases, serine/threonine kinases and/or lipid kinases, their preparation and use as medicaments, especially for the treatment of malignant disorders and other disorders based on pathological cell proliferations:
摘要翻译： 本发明涉及式（Ia）和（Ib）的吡啶并[2,3-b]吡嗪化合物，其具有调节错误定向的细胞信号转导过程如酪氨酸激酶，丝氨酸/苏氨酸激酶和/或脂质激酶的活性， 它们作为药物的制备和用途，特别是用于治疗基于病理性细胞增殖的恶性疾病和其它病症：
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公开(公告)号：US20120214768A1
公开(公告)日：2012-08-23
申请号：US13455435
申请日：2012-04-25
申请人： Matthias Gerlach , Irene Seipelt , Eckhard Guenther , Emmanuel Polymeropoulos , Tilmann Schuster , Eckhard Claus
发明人： Matthias Gerlach , Irene Seipelt , Eckhard Guenther , Emmanuel Polymeropoulos , Tilmann Schuster , Eckhard Claus
IPC分类号： A61K31/4985 , C07F9/6561 , A61K31/675 , A61K31/538 , A61P1/16 , A61K31/551 , A61P35/00 , A61P17/06 , A61P9/10 , C07D471/04 , A61K31/541
CPC分类号： C07D471/04
摘要： The invention relates to pyrido[2,3-b]pyrazine compounds of general formulae (Ia) and (Ib), to their preparation and use, for example, for the treatment of malignant disorders and other disorders based on pathological cell proliferations.
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