公开(公告)号：US07153873B2

公开(公告)日：2006-12-26

申请号：US11447141

申请日：2006-06-06

申请人： Matthias Gerlach ,  Corinna Sundermann

发明人： Matthias Gerlach ,  Corinna Sundermann

IPC分类号： C07D487/04 ,  C07D417/04 ,  A61K31/4188 ,  C07D513/04

CPC分类号： C07D471/04 ,  C07D487/04 ,  C07D513/04

摘要： Salts of a bicyclic, N-acylated imidazo-3-amine or an imidazo-5-amine of the formula: addition products thereof with acids, and methods for preparing the salts and addition products. Also disclosed are pharmaceutical compositions comprising the same and methods using the pharmaceutical compositions for the treatment or prophylaxis of pain, drug or alcohol abuse, diarrhoea, gastritis, ulcers, urinary incontinence, depression, narcolepsy, overweight, asthma, glaucoma, tinnitus, itching, hyperkinetic syndrome, epilepsy, or schizophrenia, for inducing anesthesia, and for anxiolysis.

公开(公告)号：US07087607B2

公开(公告)日：2006-08-08

申请号：US10273344

申请日：2002-10-18

申请人： Matthias Gerlach ,  Corinna Sundermann

发明人： Matthias Gerlach ,  Corinna Sundermann

IPC分类号： C07D487/04 ,  C07D235/00 ,  A61K31/4188

CPC分类号： C07D471/04 ,  C07D487/04 ,  C07D513/04

摘要： Salts of a bicyclic, N-acylated imidazo-3-amine or an imidazo-5-amine of the formula: addition products thereof with acids, and methods for preparing the salts and addition products. Also disclosed are pharmaceutical compositions comprising the same and methods using the pharmaceutical compositions for the treatment or prophylaxis of pain, drug or alcohol abuse, diarrhoea, gastritis, ulcers, urinary incontinence, depression, narcolepsy, overweight, asthma, glaucoma, tinnitus, itching, hyperkinetic syndrome, epilepsy, or schizophrenia, for inducing anesthesia, and for anxiolysis.

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。

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）。

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.

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）。

公开(公告)号：US20100266538A1

公开(公告)日：2010-10-21

申请号：US12731243

申请日：2010-03-25

申请人： Matthias Gerlach ,  Irene Seipelt ,  Eckhard Guenther ,  Tilmann Schuster ,  Emmanuel Polymeropoulos ,  Michael Czech ,  Eckhard Claus

发明人： Matthias Gerlach ,  Irene Seipelt ,  Eckhard Guenther ,  Tilmann Schuster ,  Emmanuel Polymeropoulos ,  Michael Czech ,  Eckhard Claus

IPC分类号： A61K38/21 ,  C07D241/44 ,  A61K31/498 ,  A61K38/46 ,  A61K38/14 ,  A61K33/24 ,  A61K31/573 ,  A61P35/00 ,  A61P35/04

CPC分类号： C07D241/44 ,  C07D401/12 ,  C07D403/04 ,  C07D409/12 ,  C07D413/12

摘要： The invention provides quinoxalines of the general formula I which are used as medicaments preferably for treating tumour disorders, in particular in cases of drug resistance to other active compounds and in cases of metastasic carcinoma. The possible applications are not limited to tumour disorders.

摘要翻译： 本发明提供了通式I的喹喔啉，其用作优选用于治疗肿瘤病症的药物，特别是在对其它活性化合物的耐药性和转移性癌症的情况下。 可能的应用不限于肿瘤病症。

公开(公告)号：US07671074B2

公开(公告)日：2010-03-02

申请号：US11742946

申请日：2007-05-01

申请人： Matthias Gerlach ,  Heinz Uragg ,  Michael Haurand ,  Claudia Katharina Puetz ,  Corinna Sundermann ,  Boris Chizh

发明人： Matthias Gerlach ,  Heinz Uragg ,  Michael Haurand ,  Claudia Katharina Puetz ,  Corinna Sundermann ,  Boris Chizh

IPC分类号： A61K31/44

CPC分类号： C07D213/40 ,  C07C311/49 ,  C07C311/64 ,  C07C2601/14 ,  C07D213/75 ,  C07D213/77 ,  C07D231/40 ,  C07D239/26 ,  C07D295/215 ,  C07D295/32 ,  C07D307/52 ,  C07D333/20 ,  C07D401/12 ,  C07D409/12 ,  C07D521/00

摘要： Sulfonylguanidine compounds corresponding to the tautomeric formulas I and Ia, a method for producing them, pharmaceutical compositions containing them, and methods of using them to prepare medicaments and for treating various medical conditions. The sulfonylguanidine compounds have an affinity for the gabapentin binding site and can be used to treat conditions such as pain, epilepsy, migraine and others.

摘要翻译： 对应于互变异构体式I和Ia的磺酰胍化合物，其制备方法，含有它们的药物组合物及其用于制备药物和用于治疗各种医疗条件的方法。 磺酰胍类化合物对加巴喷丁结合位点具有亲和力，可用于治疗疼痛，癫痫，偏头痛等疾病。

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

IPC分类号： A61K31/403 ,  A61P35/00 ,  A61P31/12 ,  A61P25/28 ,  A61P29/00 ,  A61P19/02

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。

公开(公告)号：US20080051463A1

公开(公告)日：2008-02-28

申请号：US11833254

申请日：2007-08-03

申请人： Matthias Gerlach ,  Eckhard Gunther ,  Peter Schmidt ,  Helge Prinz ,  Konrad Bohm ,  Eberhard Unger

发明人： Matthias Gerlach ,  Eckhard Gunther ,  Peter Schmidt ,  Helge Prinz ,  Konrad Bohm ,  Eberhard Unger

IPC分类号： A61K31/12 ,  A61P35/00 ,  C07C49/14

CPC分类号： C07C49/683 ,  C07C49/697 ,  C07C49/747 ,  C07C49/755 ,  C07C2603/24

摘要： The present invention provides novel anthracene compounds according to the formulae (I) and (II) and also selected anthracene compound compounds. The present invention furthermore provides a process for preparing such anthracene compounds. Also provided are pharmaceutical formulations comprising these anthracene compounds. The anthracene compounds provided are particularly suitable for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions which can be treated by inhibiting tubulin polymerization and/or by inhibiting microtubuli-based motor proteins, in particular various tumor disorders.

摘要翻译： 本发明提供了式（I）和（II）的新型蒽化合物，还提供了选择的蒽化合物。 本发明还提供了制备这种蒽化合物的方法。 还提供了包含这些蒽化合物的药物制剂。 所提供的蒽化合物特别适用于治疗和/或预防可通过抑制微管蛋白聚合和/或抑制基于微管的运动蛋白，特别是各种肿瘤疾病来治疗的生理和/或病理生理学病症。