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1.发明授权Conjugates of disorazoles and their derivatives with cell-binding molecules, novel disorazole derivatives, processes of manufacturing and uses thereof 有权异恶唑及其衍生物与细胞结合分子的结合物，新型二唑衍生物，制造方法及其用途公开(公告)号：US08470776B2
公开(公告)日：2013-06-25
申请号：US12728050
申请日：2010-03-19
申请人： Eckhard Guenther , Olaf Schaefer , Michael Teifel , Klaus Paulini
发明人： Eckhard Guenther , Olaf Schaefer , Michael Teifel , Klaus Paulini
CPC分类号： C12P17/188 , C07D498/18 , C07D498/22 , C07K7/23 , C07K14/6555
摘要： The present invention provides conjugates of disorazoles and their derivatives with cell-binding molecules, such as peptides, proteins, hormones, blood proteins and antibodies. The present invention further provides novel disorazole derivatives and processes of manufacturing such conjugates and disorazole derivatives. These compounds can be used as medicaments for the treatment of physiological and/or pathophysiological conditions in mammals, in particular for the treatment of various tumors.
摘要翻译： 本发明提供了disorazole及其衍生物与细胞结合分子如肽，蛋白质，激素，血液蛋白和抗体的缀合物。 本发明还提供了新的二唑衍生物和制备这种缀合物和二唑衍生物的方法。 这些化合物可以用作治疗哺乳动物的生理和/或病理生理状况的药物，特别是用于治疗各种肿瘤。
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2.发明申请CONJUGATES OF DISORAZOLES AND THEIR DERIVATIVES WITH CELL-BINDING MOLECULES, NOVEL DISORAZOLE DERIVATIVES, PROCESSES OF MANUFACTURING AND USES THEREOF 审中-公开异恶唑及其衍生物与细胞结合分子的结合，新型异唑衍生物，制造方法及其用途公开(公告)号：US20100323963A1
公开(公告)日：2010-12-23
申请号：US12728075
申请日：2010-03-19
申请人： Eckhard GUENTHER , Olaf Schaefer , Michael Teifel , Klaus Paulini
发明人： Eckhard GUENTHER , Olaf Schaefer , Michael Teifel , Klaus Paulini
IPC分类号： A61K38/09 , C07D498/22 , C07D498/16 , C07K7/23 , C07K14/655 , A61K31/424 , A61K38/31 , A61P35/00 , A61P35/02
CPC分类号： C12P17/188 , C07D498/18 , C07D498/22 , C07K7/23 , C07K14/6555
摘要： The present invention provides conjugates of disorazoles and their derivatives with cell-binding molecules, such as peptides, proteins, hormones, blood proteins and antibodies. The present invention further provides novel disorazole derivatives and processes of manufacturing such conjugates and disorazole derivatives. These compounds can be used as medicaments for the treatment of physiological and/or pathophysiological conditions in mammals, in particular for the treatment of various tumors.
摘要翻译： 本发明提供了disorazole及其衍生物与细胞结合分子如肽，蛋白质，激素，血液蛋白和抗体的缀合物。 本发明还提供了新的二唑衍生物和制备这种缀合物和二唑衍生物的方法。 这些化合物可以用作治疗哺乳动物的生理和/或病理生理状况的药物，特别是用于治疗各种肿瘤。
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3.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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4.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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公开(公告)号：US07122570B2
公开(公告)日：2006-10-17
申请号：US10319833
申请日：2002-12-16
IPC分类号： A61K31/403 , C07D209/88
CPC分类号： C07D401/12 , A61K38/00 , C07D209/86 , C07D209/88 , C07K5/0202
摘要： This invention provides new tetrahydrocarbazole derivatives that act as ligands for G-protein-coupled receptors (GPCR), especially as antagonists of the gonadotropin-releasing hormone (GnRH). A pharmaceutical composition that contains these new tetrahydrocarbazole derivatives as well as a process for the production of the new tetrahydrocarbazole derivatives are also provided. Moreover, this invention relates to the administration of tetrahydrocarbazole derivatives for treating pathologic conditions that are mediated by GPCR, especially for inhibiting GnRH, in mammals, especially humans, who require such an administration, as well as the use of tetrahydrocarbazole derivatives for the production of a pharmaceutical agent for treating GPCR-mediated pathologic conditions, especially for inhibiting GnRH.
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公开(公告)号：US20050009809A1
公开(公告)日：2005-01-13
申请号：US10879280
申请日：2004-06-29
申请人： Matthias Gerlach , Peter Emig , Klaus Paulini , Michael Czech , Tilman Schuster , Eckhard Gunther
发明人： Matthias Gerlach , Peter Emig , Klaus Paulini , Michael Czech , Tilman Schuster , Eckhard Gunther
IPC分类号： A61K31/496 , A61K31/551 , C07D219/04 , C07D219/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D493/04 , C07
CPC分类号： C07D219/04 , C07D219/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D493/04
摘要： The invention relates to novel acridine derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for the treatment of tumors.
摘要翻译： 本发明涉及式1的新型吖啶衍生物，其制备及其用作药物，特别是用于治疗肿瘤。
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7.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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8.发明授权Triazole derivatives with improved receptor activity and bioavailability properties as ghrelin antagonists of growth hormone secretagogue receptors 有权具有改善的受体活性和生物利用度性质的三唑衍生物作为生长激素促分泌素受体的生长素释放肽拮抗剂公开(公告)号：US08546435B2
公开(公告)日：2013-10-01
申请号：US13235116
申请日：2011-09-16
申请人： Babette Aicher , Gilbert Mueller , Klaus Paulini , Lars Blumenstein , Peter Schmidt , Matthias Gerlach , Michael Teifel , Jean Martinez , Jean-Alain Fehrentz , Anne-Laure Blayo
发明人： Babette Aicher , Gilbert Mueller , Klaus Paulini , Lars Blumenstein , Peter Schmidt , Matthias Gerlach , Michael Teifel , Jean Martinez , Jean-Alain Fehrentz , Anne-Laure Blayo
IPC分类号： A61K31/41 , C07D249/08
CPC分类号： A61K31/4196 , C07D401/14 , C07D403/06 , C07D403/14 , C07D413/14
摘要： The present invention provides novel triazole derivatives with improved receptor activity and bioavailability properties as ghrelin analogue ligands of growth hormone secretagogue receptors according to formula (I) that are useful in the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, preferably humans, that are mediated by GHS receptors. The present invention further provides GHS receptor antagonists and agonists that can be used for modulation of these receptors and are useful for treating above conditions, in particular alcohol disorder, drug abuse, growth retardation, cachexia, short-, medium-, and/or long term regulation of energy balance, short-, medium-, and/or long term regulation (stimulation and/or inhibition) of food intake, intake of rewarding food, adipogenesis, adiposity and/or obesity, body weight gain and/or reduction, diabetes, diabetes type I, diabetes type II, tumor cell proliferation, inflammation, inflammatory effects, gastric postoperative ileus, postoperative ileus and/or gastrectomy (ghrelin replacement therapy).
摘要翻译： 本发明提供具有改善的受体活性和生物利用度性质的新型三唑衍生物，其作为根据式（I）的生长激素促分泌素受体的生长激素释放肽类似物配体可用于治疗或预防哺乳动物（优选人）中的生理和/或病理生理状况， 这是由GHS受体介导的。 本发明还提供了可用于调节这些受体的GHS受体拮抗剂和激动剂，并且可用于治疗上述病症，特别是酒精障碍，药物滥用，生长迟缓，恶病质，短期，中期和/或长期 能量平衡，短期，中期和/或长期调节（刺激和/或抑制）食物摄取，有益食物摄取，肥胖和/或肥胖，体重增加和/或减少的长期调节， 糖尿病，I型糖尿病，II型糖尿病，肿瘤细胞增殖，炎症，炎症反应，胃后肠梗阻，术后肠梗阻和/或胃切除术（Ghrelin替代疗法）。
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9.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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10.发明申请NOVEL TRIAZOLE DERIVATIVES WITH IMPROVED RECEPTOR ACTIVITY AND BIOAVAILABILITY PROPERTIES AS GHRELIN ANTAGONISTS OF GROWTH HORMONE SECRETAGOGUE RECEPTORS 有权具有改善的受体活性和生物利用性质的新型三唑衍生物作为生长激素分泌受体的GHRELIN拮抗剂公开(公告)号：US20120083494A1
公开(公告)日：2012-04-05
申请号：US13235116
申请日：2011-09-16
申请人： Babette Aicher , Gilbert Mueller , Klaus Paulini , Lars Blumenstein , Peter Schmidt , Matthias Gerlach , Michael Teifel , Jean Martinez , Jean-Alain Fehrentz , Anne-Laure Blayo
发明人： Babette Aicher , Gilbert Mueller , Klaus Paulini , Lars Blumenstein , Peter Schmidt , Matthias Gerlach , Michael Teifel , Jean Martinez , Jean-Alain Fehrentz , Anne-Laure Blayo
IPC分类号： A61K31/5377 , A61K31/4196 , A61K31/454 , C07D401/14 , C07D403/06 , C07D413/14 , C07D403/14 , A61P43/00 , A61P21/00 , A61P25/28 , A61P3/04 , A61P25/22 , A61P9/12 , A61P3/00 , A61P19/08 , A61P9/00 , A61P19/04 , A61P11/00 , A61P25/00 , A61P13/12 , A61P9/04 , A61P1/00 , A61P25/24 , A61P25/30 , A61P3/08 , A61P5/06 , A61P17/00 , A61P37/00 , A61P37/04 , A61P37/06 , A61P29/00 , A61P3/10 , A61P19/10 , A61P25/18 , A61P1/02 , A61P35/00 , A61P1/16 , A61P17/02 , A61K31/4439
CPC分类号： A61K31/4196 , C07D401/14 , C07D403/06 , C07D403/14 , C07D413/14
摘要： The present invention provides novel triazole derivatives with improved receptor activity and bioavailability properties as ghrelin analogue ligands of growth hormone secretagogue receptors according to formula (I) that are useful in the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, preferably humans, that are mediated by GHS receptors. The present invention further provides GHS receptor antagonists and agonists that can be used for modulation of these receptors and are useful for treating above conditions, in particular alcohol disorder, drug abuse, growth retardation, cachexia, short-, medium-, and/or long term regulation of energy balance, short-, medium-, and/or long term regulation (stimulation and/or inhibition) of food intake, intake of rewarding food, adipogenesis, adiposity and/or obesity, body weight gain and/or reduction, diabetes, diabetes type I, diabetes type II, tumor cell proliferation, inflammation, inflammatory effects, gastric postoperative ileus, postoperative ileus and/or gastrectomy (ghrelin replacement therapy).
摘要翻译： 本发明提供具有改善的受体活性和生物利用度性质的新型三唑衍生物，其作为根据式（I）的生长激素促分泌素受体的生长激素释放肽类似物配体可用于治疗或预防哺乳动物（优选人）中的生理和/或病理生理状况， 这是由GHS受体介导的。 本发明还提供了可用于调节这些受体的GHS受体拮抗剂和激动剂，并且可用于治疗上述病症，特别是酒精障碍，药物滥用，生长迟缓，恶病质，短期，中期和/或长期 能量平衡，短期，中期和/或长期调节（刺激和/或抑制）食物摄取，有益食物摄取，肥胖和/或肥胖，体重增加和/或减少的长期调节， 糖尿病，I型糖尿病，II型糖尿病，肿瘤细胞增殖，炎症，炎症反应，胃后肠梗阻，术后肠梗阻和/或胃切除术（Ghrelin替代疗法）。
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