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1. 发明申请

WO2011154327A1 NITROGEN CONTAINING HETEROARYL COMPOUNDS 审中-公开
标题翻译：含氮异氰酸酯化合物
公开(公告)号：WO2011154327A1
公开(公告)日：2011-12-15
申请号：PCT/EP2011/059234
申请日：2011-06-06
申请人： F. HOFFMANN-LA ROCHE AG , BLEICHER, Konrad , FLOHR, Alexander , GROEBKE ZBINDEN, Katrin , GRUBER, Felix , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RODRIGUEZ SARMIENTO, Rosa Maria
发明人： BLEICHER, Konrad , FLOHR, Alexander , GROEBKE ZBINDEN, Katrin , GRUBER, Felix , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RODRIGUEZ SARMIENTO, Rosa Maria
IPC分类号： C07D401/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14 , A61K31/506 , A61P25/00 , A61P35/00
CPC分类号： C07D401/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The invention is concerned with novel nitrogen-containing heteroaryl compounds of formula (I) wherein A 1 , A 2 , (a), R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新型含氮杂芳基化合物，其中A1，A2，（a），R1，R2，R3，R4，R5和R6如说明书和权利要求书中所定义，以及其生理上可接受的盐和酯。这些化合物抑制PDE10A，可用作药物。

2. 发明申请

WO2011089132A1 NITROGEN-CONTAINING HETEROARYL DERIVATIVES 审中-公开
标题翻译：含氮含量衍生物
公开(公告)号：WO2011089132A1
公开(公告)日：2011-07-28
申请号：PCT/EP2011/050640
申请日：2011-01-19
申请人： F. HOFFMANN-LA ROCHE AG , BLEICHER, Konrad , FLOHR, Alexander , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RODRIGUEZ SARMIENTO, Rosa Maria , VIEIRA, Eric
发明人： BLEICHER, Konrad , FLOHR, Alexander , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RODRIGUEZ SARMIENTO, Rosa Maria , VIEIRA, Eric
IPC分类号： C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14 , A61K31/506 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/28
CPC分类号： C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The invention is concerned with novel nitrogen-containing heteroaryl derivatives of formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , A 1 , A 2 , and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新型含氮杂芳基衍生物，其中R1，R2，R3，R4，R5，A1，A2和Y如说明书和权利要求书中所定义，以及生理上可接受的盐及其酯。这些化合物抑制PDE10A，可用作药物。

3. 发明申请

WO2011036127A1 IMIDAZOPYRIDINE OR IMIDAZOPYRIMIDINE DERIVATIVES AS PHOSPHODIESTERASE 10A INHIBITORS 审中-公开
标题翻译：作为磷酸二酯酶10A抑制剂的咪唑并吡啶或咪唑并嘧啶衍生物
公开(公告)号：WO2011036127A1
公开(公告)日：2011-03-31
申请号：PCT/EP2010/063830
申请日：2010-09-21
申请人： F. HOFFMANN-LA ROCHE AG , ALBERATI, Daniela , ALVAREZ SÁNCHEZ, Rubén , BLEICHER, Konrad , FLOHR, Alexander , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RUDOLPH, Markus
发明人： ALBERATI, Daniela , ALVAREZ SÁNCHEZ, Rubén , BLEICHER, Konrad , FLOHR, Alexander , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RUDOLPH, Markus
IPC分类号： C07D471/04 , C07D487/04 , A61K31/437
CPC分类号： C07D471/04 , A61K31/437 , A61K31/496 , A61K31/5025 , A61K31/5377 , A61K31/553 , C07D487/04
摘要： The invention is concerned with novel imidazopyridine derivatives of formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 and A are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新咪唑并吡啶衍生物，其中R 1，R 2，R 3，R 4，R 5和A如说明书和权利要求书中所定义，以及其生理上可接受的盐和酯。这些化合物抑制PDE10A，可用作药物。

4. 发明申请

WO2011117264A1 N-(IMIDAZOPYRIMIDIN-7-YL)-HETEROARYLAMIDE DERIVATIVES AND THEIR USE AS PDE10A INHIBITORS 审中-公开
标题翻译： N-（咪唑并吡啶-7-YL）-HETEROARYLAMIDE衍生物及其作为PDE10A抑制剂的用途
公开(公告)号：WO2011117264A1
公开(公告)日：2011-09-29
申请号：PCT/EP2011/054385
申请日：2011-03-23
申请人： F. HOFFMANN-LA ROCHE AG , ALVAREZ SÁNCHEZ, Rubén , BLEICHER, Konrad , FLOHR, Alexander , GOBBI, Luca , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RUDOLPH, Markus
发明人： ALVAREZ SÁNCHEZ, Rubén , BLEICHER, Konrad , FLOHR, Alexander , GOBBI, Luca , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RUDOLPH, Markus
IPC分类号： C07D487/04 , C07D519/00 , A61K31/519 , A61P25/00 , A61P25/18
CPC分类号： C07D487/04 , C07D519/00
摘要： The invention is concerned with novel imidazopyrimidine derivatives of formula (I) wherein R 1 , R 2 and R 8 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDEIOA and used as medicaments.
摘要翻译：本发明涉及式（I）的新型咪唑并嘧啶衍生物，其中R 1，R 2和R 8如说明书和权利要求书中所定义，以及其生理上可接受的盐和酯。这些化合物抑制PDEIOA并用作药物。

5. 发明申请

WO2013034506A1 PDE10 MODULATORS 审中-公开
标题翻译： PDE10调制器
公开(公告)号：WO2013034506A1
公开(公告)日：2013-03-14
申请号：PCT/EP2012/067047
申请日：2012-09-03
申请人： F. HOFFMANN-LA ROCHE AG , BACHMANN, Stephan , FLOHR, Alexander , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RUDOLPH, Markus
发明人： BACHMANN, Stephan , FLOHR, Alexander , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias , KUHN, Bernd , PETERS, Jens-Uwe , RUDOLPH, Markus
IPC分类号： C07D231/14 , C07D233/90 , C07D401/14 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , A61P25/00 , A61K31/4155 , A61K31/4178 , A61K31/4192 , A61K31/4196 , A61K31/422
CPC分类号： C07D471/04 , C07D231/14 , C07D233/90 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention relates to compounds of formula (I) wherein R 1 , R 2 , R 3 , R 5 , W, X, X 1 , Y, Y 1 , Z and Z 1 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.
摘要翻译：本发明涉及式（I）化合物，其中R 1，R 2，R 3，R 5，W，X，X 1，Y，Y 1，Z和Z 1如说明书和权利要求书中所定义，以及生理上可接受的盐它们。这些化合物抑制PDE10A，可用作药物。

6. 发明申请

WO2012076430A1 TRIAZOLOPYRIDINE COMPOUNDS 审中-公开
标题翻译：三唑啉化合物
公开(公告)号：WO2012076430A1
公开(公告)日：2012-06-14
申请号：PCT/EP2011/071685
申请日：2011-12-05
申请人： F. HOFFMANN-LA ROCHE AG , FLOHR, Alexander , GOBBI, Luca , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias , PETERS, Jens-Uwe
发明人： FLOHR, Alexander , GOBBI, Luca , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias , PETERS, Jens-Uwe
IPC分类号： C07D471/04 , C07D519/00 , A61K31/437 , A61P25/00 , A61P35/00 , A61P3/10
CPC分类号： C07D471/04 , C07D519/00
摘要： The invention is concerned with triazolopyridine compounds of formula (I), wherein R 1 , R 2 , R 3 and R 4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDEIOA and can be used as medicaments.
摘要翻译：本发明涉及式（I）的三唑并吡啶化合物，其中R 1，R 2，R 3和R 4如说明书和权利要求书中所定义，以及其生理上可接受的盐。这些化合物抑制PDEIOA并可用作药物。

7. 发明申请

WO2013041472A1 TRIAZOLOPYRIDINE COMPOUNDS AS PDE10A INHIBITORS 审中-公开
标题翻译：三唑并吡啶化合物作为PDE10A抑制剂
公开(公告)号：WO2013041472A1
公开(公告)日：2013-03-28
申请号：PCT/EP2012/068203
申请日：2012-09-17
申请人： F. HOFFMANN-LA ROCHE AG , FLOHR, Alexander , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias
发明人： FLOHR, Alexander , GROEBKE ZBINDEN, Katrin , KOERNER, Matthias
IPC分类号： C07D471/04 , A61K31/437 , A61P25/00
CPC分类号： C07D471/04
摘要： The invention is concerned with triazolopyridine compounds of formula (I) wherein R 1 , R 2 and R 3 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.
摘要翻译：本发明涉及式（I）的三唑并吡啶化合物，其中R 1，R 2和R 3如说明书和权利要求书中所定义，以及其生理上可接受的盐。这些化合物抑制PDE10A，可用作药物。

8. 发明申请

WO2007057317A1 NOVEL PYRROLIDINE DERIVATIVES AS INHIBITORS OF COAGULATION FACTOR XA 审中-公开
标题翻译：作为凝血因子XA的抑制剂的新型吡咯烷衍生物
公开(公告)号：WO2007057317A1
公开(公告)日：2007-05-24
申请号：PCT/EP2006/068138
申请日：2006-11-06
申请人： F. HOFFMANN-LA ROCHE AG , ANSELM, Lilli , GROEBKE ZBINDEN, Katrin , HAAP, Wolfgang , HILPERT, Hans , HIMBER, Jacques , KUHN, Bernd , PANDAY, Narendra , RICKLIN, Fabienne , THOMI, Stefan
发明人： ANSELM, Lilli , GROEBKE ZBINDEN, Katrin , HAAP, Wolfgang , HILPERT, Hans , HIMBER, Jacques , KUHN, Bernd , PANDAY, Narendra , RICKLIN, Fabienne , THOMI, Stefan
IPC分类号： C07D409/14 , A61K31/4439 , A61P7/00
CPC分类号： C07D409/14 , C07D413/14
摘要： The invention is concerned with novel pyrrolidine derivatives of formula (I) wherein X, Y, R 1 , R 2 and R 3 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新型吡咯烷衍生物，其中X，Y，R 1，R 2和R 3定义如上在说明书和权利要求书中，以及其生理上可接受的盐。这些化合物抑制凝血因子Xa并可用作药物。

9. 发明申请

WO2008049747A1 NOVEL HETEROARYL CARBOXAMIDES 审中-公开
标题翻译：新型异氰脲酸酯
公开(公告)号：WO2008049747A1
公开(公告)日：2008-05-02
申请号：PCT/EP2007/060928
申请日：2007-10-15
申请人： F. HOFFMANN-LA ROCHE AG , GROEBKE ZBINDEN, Katrin , HAAP, Wolfgang , HILPERT, Hans , KUHN, Bernd , PANDAY, Narendra , RICKLIN, Fabienne
发明人： GROEBKE ZBINDEN, Katrin , HAAP, Wolfgang , HILPERT, Hans , KUHN, Bernd , PANDAY, Narendra , RICKLIN, Fabienne
IPC分类号： C07D413/14 , A61K31/497 , A61P7/02
CPC分类号： C07D413/14
摘要： The invention is concerned with novel heteroaryl carboxamides of formula (I), wherein A, R 1 , R 2 , X, Y, Z and m are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新型杂芳基羧酰胺，其中A，R 1，R 2，X，Y，Z和m如说明书中所定义和权利要求书以及其生理上可接受的盐。这些化合物抑制凝血因子Xa，并且可以用作药物。

10. 发明申请

WO2009016048A1 2-AZETIDINEMETHANEAMINES AND 2-PYRROLIDINEMETHANEAMINES AS TAAR-LIGANDS 审中-公开
标题翻译： 2-氨基乙酰胺和2-吡咯烷基磺酰胺作为TAAR-LIGANDS
公开(公告)号：WO2009016048A1
公开(公告)日：2009-02-05
申请号：PCT/EP2008/059429
申请日：2008-07-18
申请人： F. HOFFMANN-LA ROCHE AG , GALLEY, Guido , GOERGLER, Annick , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
发明人： GALLEY, Guido , GOERGLER, Annick , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
IPC分类号： C07D205/04 , C07D207/09 , A61K31/397 , A61K31/40 , A61P25/00
CPC分类号： C07D205/04 , C07D207/09
摘要： The present invention relates to compounds of formula (I) wherein R 1 is hydrogen, lower alkyl or benzyl which may be optionally substituted by halogen or lower alkoxy; R 2 is hydrogen, halogen or OR, wherein R is lower alkyl, aryl or lower alkyl substituted by halogen; R 3 is hydrogen or fluorine; Ar is phenyl; n is 0 or 1; o is 0, 1 or 2; and to their pharmaceutically active salts. It has been found that the compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
摘要翻译：本发明涉及式（I）化合物，其中R 1是氢，可以被卤素或低级烷氧基任意取代的低级烷基或苄基; R2是氢，卤素或OR，其中R是被卤素取代的低级烷基，芳基或低级烷基; R3是氢或氟; Ar是苯基; n为0或1; o为0,1或2; 和其药物活性盐。已经发现，式I化合物对微量胺相关受体（TAAR）具有良好的亲和力，特别是对于TAAR1。这些化合物可用于治疗抑郁症，焦虑障碍，双相情感障碍，注意力缺陷多动障碍（ADHD），应激相关疾病，精神病性精神障碍如精神分裂症，神经系统疾病如帕金森病，神经变性疾病如阿尔茨海默病，癫痫，偏头痛，高血压，药物滥用和代谢障碍如进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量消耗和同化障碍，体温平衡紊乱和失调，睡眠和昼夜节律紊乱以及心血管疾病。

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