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1. 发明申请

WO2018154088A1 1, 4, 6-TRISUBSTITUTED-2-ALKYL-1H-BENZO[D]IMIDAZOLE DERIVATIVES AS DIHYDROOROTATE OXYGENASE INHIBITORS 审中-公开
公开(公告)号：WO2018154088A1
公开(公告)日：2018-08-30
申请号：PCT/EP2018/054602
申请日：2018-02-23
申请人： MERCK PATENT GMBH
发明人： THUNUGUNTLA, Siva Sanjeeva Rao , HOSAHALLI, Subramanya , PANIGRAHI, Sunil Kumar , SCHWARZ, Matthias , ARLT, Michael
IPC分类号： C07D235/08 , C07D401/10 , C07D403/10 , C07D413/10 , C07D417/10 , A61K31/4184
摘要： The present invention provides 1, 4, 6-trisubstituted-2-alkyl-1H-benzo[d]imidazole derivatives as dihydroorotate oxygenase inhibitor compounds of formula (I), which may be therapeutically useful as DHODH inhibitors, in which R 1 to R 3 and 'm' have the meanings given in the specification, and pharmaceutically acceptable salts or stereoisomer thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting DHODH. The present invention also provides methods for synthesizing 1, 4, 6-trisubstituted-2-alkyl-1H-benzo[d]imidazole derivatives of formula (I). The present invention also provides pharmaceutical formulations comprising at least one of the DHODH inhibitor compound of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient.

2. 发明申请

WO2004089932A1 SUBSTITUIERTE PYRAZOLVERBINDUNGEN 审中-公开
标题翻译：取代的吡唑
公开(公告)号：WO2004089932A1
公开(公告)日：2004-10-21
申请号：PCT/EP2004/002453
申请日：2004-03-10
申请人： MERCK PATENT GMBH , SCHADT, Oliver , ARLT, Michael , FINSINGER, Dirk , SCHIEMANN, Kai , VAN AMSTERDAM, Christoph , BARTOSZYK, Gerd , SEYFRIED, Christoph
发明人： SCHADT, Oliver , ARLT, Michael , FINSINGER, Dirk , SCHIEMANN, Kai , VAN AMSTERDAM, Christoph , BARTOSZYK, Gerd , SEYFRIED, Christoph
IPC分类号： C07D401/04
CPC分类号： C07D231/12 , C07D231/40 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/10 , C07D405/14 , C07D409/10 , C07D409/14 , C07D413/04 , C07D413/14
摘要： Verbindungen der Formel (I) sowie deren Salze und Solvate, worin X, R 1 , R 2 , R 3 , und R 5 die in Anspruch (1) angegebenen Bedeutungen aufweisen, eignen sich als Liganden von 5 HT-Rezeptoren.
摘要翻译：式（I）和它们的盐和溶剂化物的化合物，其中X，R <1>，R <2>，R <3>，和R <5>具有在指定的权利要求（1），其是有用的作为配位体的含义 5个HT受体。

3. 发明申请

WO2004089931A1 SUBSTITUIERTE PYRAZOLE 审中-公开
标题翻译：取代的吡唑
公开(公告)号：WO2004089931A1
公开(公告)日：2004-10-21
申请号：PCT/EP2004/002353
申请日：2004-03-08
申请人： MERCK PATENT GMBH , SCHIEMANN, Kai , ACKERMANN, Karl-August , ARLT, Michael , FINSINGER, Dirk , SCHADT, Oliver , VAN AMSTERDAM, Christoph , BARTOSZYK, Gerd , SEYFRIED, Christoph
发明人： SCHIEMANN, Kai , ACKERMANN, Karl-August , ARLT, Michael , FINSINGER, Dirk , SCHADT, Oliver , VAN AMSTERDAM, Christoph , BARTOSZYK, Gerd , SEYFRIED, Christoph
IPC分类号： C07D401/04
CPC分类号： C07D231/12 , A61K31/415 , C07D231/14 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D409/06 , C07D409/10 , C07D413/12 , C07D451/06 , C07D453/06 , C07D471/04 , C07D471/10 , C07D487/08 , C07D491/08
摘要： Die Verbindungen der Formel (I) sowie deren Salze und Solvate, worin X, R 1 , R 2 , R 3 , R 4 und R 5 die in Anspruch (1) angegebenen Bedeutungen aufweisen, eignen sich als Liganden von 5 HT-Rezeptoren.
摘要翻译：式（I）和它们的盐和溶剂化物的化合物，其中X，R <1>，R <2>，R <3>，R <4>和R <5>有指定（1）含义要求，可用作5个HT受体的配体。

4. 发明申请

WO2003031435A1 PYRAZOLE DERIVATIVES 审中-公开
标题翻译：吡咯衍生物作为甘氨酸运输商抑制剂
公开(公告)号：WO2003031435A1
公开(公告)日：2003-04-17
申请号：PCT/EP2002/010172
申请日：2002-09-11
申请人： MERCK PATENT GMBH , YAMANOUCHI PHARMACEUTICAL CO. LTD. , SCHIEMANN, Kai , ARLT, Michael , FINSINGER, Dirk , ACKERMANN, Karl-August , RAUTENBERG, Wilfried , LEIBROCK, Joachim , GREINER, Hartmut , TOBE, Takahiko
发明人： SCHIEMANN, Kai , ARLT, Michael , FINSINGER, Dirk , ACKERMANN, Karl-August , RAUTENBERG, Wilfried , LEIBROCK, Joachim , GREINER, Hartmut , TOBE, Takahiko
IPC分类号： C07D401/06
CPC分类号： C07D231/12 , C07D231/14 , C07D401/04 , C07D401/06 , C07D403/06 , C07D409/10 , C07D417/06 , C07D471/04 , C07D491/10
摘要： Compounds of the formula (I) and salts and solvates thereof, in which X, R 1 , R 2 , R 3 , R 4 and R 5 are as defined in Claim 1, are suitable as glycine transporter inhibitors and can be used in human and veterinary medicine for the prophylaxis and treatment of schizophrenia, depression, dementia, Parkinson's disease, Alzheimer's disease, Lewy bodies dementia, Huntington's disease, Tourette's syndrome, anxiety, learning and memory restrictions, neurodegenerative disorders and other cognitive impairments, as well as nicotine dependence and pain.
摘要翻译：其中X，R 1，R 2，R 3，R 4和R 5如权利要求1中所定义的式（I）化合物及其盐和溶剂合物是合适的作为甘氨酸转运蛋白抑制剂，可用于人和兽医学用于预防和治疗精神分裂症，抑郁症，痴呆，帕金森病，阿尔茨海默氏病，路易体痴呆，亨廷顿舞蹈病，图雷特氏综合征，焦虑症，学习记忆障碍，神经变性疾病和其他认知障碍，以及尼古丁依赖和疼痛。

5. 发明公开

EP1293503A1 TRIAZOLE DERIVATIVES 审中-公开
标题翻译：三唑衍生物
公开(公告)号：EP1293503A1
公开(公告)日：2003-03-19
申请号：EP01930192.8
申请日：2001-05-17
申请人： YAMANOUCHI PHARMACEUTICAL CO. LTD. , Merck Patent GmbH
发明人： TOBE, Takahiko , SUGANE, Takashi , HAMAGUCHI, Wataru , SHIMADA, Itsuro , MAENO, Kyoichi , MIYATA, Junji , KIMIZUKA, Tetsuya , SUZUKI, Takeshi , KOHARA, Atsuyuki , MORITA, Takuma , ARLT, Michael , GREINER, Hartmut
IPC分类号： C07D249/08 , C07D249/12 , C07D401/04 , C07D413/14 , C07D405/14 , C07D405/12 , C07D405/04 , A61K31/41
CPC分类号： C07D249/08 , A61K31/41 , A61K31/4155 , A61K31/416 , A61K31/427 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61K31/517 , A61K31/5377 , C07D249/10 , C07D249/12 , C07D249/14 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/06 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/10 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/10 , C07D495/04
摘要： The invention relates to a triazole derivative with an activity inhibiting glycine transporter and for use as a pharmaceutical drug, and a novel triazole derivative. The inventive triazole derivative has an excellent activity inhibiting glycine transporter and is useful as a therapeutic agent of dementia, schizophrenia, cognitive disorders, or cognitive disorders involved in various diseases such as Alzheimer disease, Parkinson's disease, or Huntington disease or the like, or spasm involved in diseases such as nerve degenerative diseases and cerebrovascular disorders, or the like. Particularly, the pharmaceutical drug is useful for the amelioration of learning disability of dementia and the like.
摘要翻译：本发明涉及具有活性抑制甘氨酸转运体并用作药物的三唑衍生物和新的三唑衍生物。本发明的三唑衍生物具有优异的抑制甘氨酸转运蛋白的活性，可用作痴呆，精神分裂症，认知障碍或涉及各种疾病如阿尔茨海默病，帕金森病或亨廷顿病等的认知障碍或痉挛的治疗剂涉及诸如神经变性疾病和脑血管障碍等疾病。特别地，药物对于改善痴呆等的学习障碍是有用的。

6. 发明公开

EP1292592A1 HETEROCYCLISCHE AMINOALKYLPYRIDINDERIVATE ALS PSYCHOPHARMAKA 有权
标题翻译：杂环烯丙基氨基甲酰基吡啶二胺
公开(公告)号：EP1292592A1
公开(公告)日：2003-03-19
申请号：EP01956484.8
申请日：2001-06-19
申请人： MERCK PATENT GmbH
发明人： DORSCH, Dieter , BÖTTCHER, Henning , ARLT, Michael , GOTTSCHLICH, Rudolf , SEYFRIED, Christoph , BARTOSZYK, Gerd , HARTING, Jürgen
IPC分类号： C07D401/12 , C07D417/12 , A61K31/4427 , C07D405/12 , C07D213/64
CPC分类号： C07D213/64 , C07D213/38 , C07D401/12 , C07D405/12 , C07D417/12
摘要： The invention relates to formula (1) heterocyclic aminoalkyl pyridine derivatives, whereby R1 represents the radical of a heterocycle comprising 1 to 3 ring structures which are saturated, unsaturated or aromatic and optionally annellated with other ring structures to form a condensed ring system, and which comprise a total of 1 to 4 N-, O- and/or S-atoms, said heterocycle being optionally substituted once, twice or three times by at least one of the following groups: -A, -OR?4, -N(R4)¿2, -NO2, -CN, Hal, -COOR4, -CON(R4)2, -COR4, = O; R2 represents a phenyl group which is optionally substituted once, twice, three, four or five times by at least one of the following groups: Hal, A, -O-A, -NO¿2? or CN, or a thienyl group which is optionally substituted once or twice by at least one of the following groups: Hal, A, -O-A, -NO2, -CN or thienyl; -X- represents -O-, -S-, sulfinyl, sulfonyl, or -C(R?4)¿2-; -Y- represents -[C(R4)2]n-; -Z- represents -C(R4)2-; and n represents 1, 2, 3 or 4. The invention also relates to the compatible salts and solvates of the heterocyclic aminoalkyl pyridine derivatives and the use thereof as pharmaceuticals.
摘要翻译：本发明涉及式（1）杂环氨基烷基吡啶衍生物，其中R 1代表包含1至3个饱和，不饱和或芳族环结构的杂环基团，并且任选与其它环结构稠合形成稠合环体系，并且其包含总共1至4个N-，O-和/或S-原子，所述杂环任选被至少一个以下基团取代一次，两次或三次：-A，-OR 4，-N（ R4）2，-NO2，-CN，Hal，-COOR4，-CON（R4）2，-COR4，= O; R2表示任选被至少一个下列基团取代一次，两次，三次，四次或五次的苯基：Hal，A，-O-A，-NO 2，或CN，或任选被至少一个下列基团取代一次或两次的噻吩基：Hal，A，-O-A，-NO 2，-CN或噻吩基; -X-表示-O - ， - S-，亚磺酰基，磺酰基或-C（R 4）2 - -Y-代表 - [C（R4）2] n-; -Z-代表-C（R4）2-; 并且n代表1,2,3或4.本发明还涉及杂环氨基烷基吡啶衍生物的相容性盐和溶剂化物及其作为药物的用途。

7. 发明授权

EP1611122B1 SUBSTITUIERTE PYRAZOLVERBINDUNGEN 有权
标题翻译：取代的吡唑
公开(公告)号：EP1611122B1
公开(公告)日：2007-06-13
申请号：EP04718926.1
申请日：2004-03-10
申请人： Merck Patent GmbH
发明人： SCHADT, Oliver , ARLT, Michael , FINSINGER, Dirk , SCHIEMANN, Kai , VAN AMSTERDAM, Christoph , BARTOSZYK, Gerd , SEYFRIED, Christoph
IPC分类号： C07D401/04 , C07D231/10 , A61K31/435
CPC分类号： C07D231/12 , C07D231/40 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/10 , C07D405/14 , C07D409/10 , C07D409/14 , C07D413/04 , C07D413/14
摘要： The invention relates to compounds of formula (I), in addition to their salts and solvates. In said formula, X, R1, R2, R3, R4 and R5 are defined as cited in claim (1). Said compounds are suitable for use as ligands of 5 HT receptors.

8. 发明公开

EP1626967A1 SUBSTITUIERTE PYRAZOLE 审中-公开
标题翻译： SUBSTITUIERTE PRARAZOLE
公开(公告)号：EP1626967A1
公开(公告)日：2006-02-22
申请号：EP04718277.9
申请日：2004-03-08
申请人： Merck Patent GmbH
发明人： SCHIEMANN, Kai , ACKERMANN, Karl-August , ARLT, Michael , FINSINGER, Dirk , SCHADT, Oliver , VAN AMSTERDAM, Christoph , BARTOSZYK, Gerd , SEYFRIED, Christoph
IPC分类号： C07D401/04 , A61K31/415 , A61P25/28
CPC分类号： C07D231/12 , A61K31/415 , C07D231/14 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D409/06 , C07D409/10 , C07D413/12 , C07D451/06 , C07D453/06 , C07D471/04 , C07D471/10 , C07D487/08 , C07D491/08
摘要： The invention relates to the compounds of formula (I) and the salts and solvates thereof, wherein X, R1, R2, R3, R4 and R5 are defined as in claim 1. The inventive compounds are suitable as ligands of 5 HT receptors.
摘要翻译：本发明涉及式（I）化合物及其盐和溶剂化物，其中X，R 1，R 2，R 3，R 4和R 5如权利要求1中所定义。本发明化合物适合作为5HT受体的配体。

9. 发明公开

EP1185259A1 GLYCINE CLEAVAGE SYSTEM INHIBITORS AS POTENTIAL ANTIPSYCHOTICS 审中-公开
标题翻译：甘氨酸分体式系统有效的抗精神病药物抑制剂
公开(公告)号：EP1185259A1
公开(公告)日：2002-03-13
申请号：EP00929364.8
申请日：2000-04-17
申请人： MERCK PATENT GmbH
发明人： ARLT, Michael , BARTOSZYK, Gerd
IPC分类号： A61K31/19 , A61K31/13 , A61P25/18 , A61P25/24 , A61P25/28
CPC分类号： A61K31/19 , A61K31/00 , A61K31/145
摘要： The invention relates to inhibitors of the glycine cleavage system and their use as potential antipsychotic agents. The invention relates furthermore to a process for treating humans having psychosis, psychosis associated with an illness, schizophrenia, Alzheimer's disease or other related psychotic disorders.

10. 发明公开

EP0931067A1 PIPERAZIN-DERIVATE MIT EINER SELEKTIVITÄT FÜR DEN D-4 REZEPTOR 失效
标题翻译：哌嗪衍生物的选择性为对D-4受体
公开(公告)号：EP0931067A1
公开(公告)日：1999-07-28
申请号：EP97944823.0
申请日：1997-09-03
申请人： MERCK PATENT GmbH
发明人： ARLT, Michael , BÖTTCHER, Henning , BARTOSZYK, Gerd , SEYFRIED, Christoph
IPC分类号： C07D295 , A61K31 , A61P25 , A61P43 , C07D213 , C07D239 , C07D241 , C07D307 , C07D401 , C07D405 , C07D409
CPC分类号： C07D213/74 , C07D213/38 , C07D239/42 , C07D295/073 , C07D295/096 , C07D295/155 , C07D401/12 , C07D405/12 , C07D409/12
摘要： Piperazine derivatives having formula (I), wherein R?1 and R2¿ have the meanings given in claim 1, are dopamine ligands with D4 receptor selectivity and are suited for treatment and prophylaxis of anxiety states, depression, schizophrenia, obsessive ideas, Parkinson's disease, tardive diskinesia, nausea and gastro-intestinal tract disorders.

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