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1. 发明申请

WO2005023772A1 MALONAMIDE DERIVATIVES BLOCKING THE ACTIVITY OF GAMA-SECRETASE 审中-公开
标题翻译：马洛酮衍生物阻断游离氨基酸酶的活性
公开(公告)号：WO2005023772A1
公开(公告)日：2005-03-17
申请号：PCT/EP2004/009700
申请日：2004-08-31
申请人： F. HOFFMANN-LA ROCHE AG , FLOHR, Alexander , GALLEY, Guido , JAKOB-ROETNE, Roland , KITAS, Eric, Argirios , PETERS, Jens-Uwe , WOSTL, Wolfgang
发明人： FLOHR, Alexander , GALLEY, Guido , JAKOB-ROETNE, Roland , KITAS, Eric, Argirios , PETERS, Jens-Uwe , WOSTL, Wolfgang
IPC分类号： C07D223/18
CPC分类号： C07D223/16 , A61K31/335 , A61K31/55 , A61K31/5513 , C07D223/20 , C07D243/24 , C07D273/00 , C07D313/14
摘要： The invention relates to malonamide derivatives of formula (I), wherein: R 1 is one of the following groups (Formulae a), b), c), d)); R 2 is lower alkyl, lower alkinyl, -(CH 2 ) n -O-lower alkyl, -(CH 2 ) n -S-lower alkyl, -(CH 2 ) n -CN, -(CR'R") n -CF 3 , -(CR'R") n -CHF 2 , -(CR'R") n -CH 2 F, -(CH 2 ) n -C(O)O-lower alkyl, -(CH 2 ) n -halogen, or is -(CH 2 ) n -cycloalkyl, optionally substituted by one or more substituents, selected from the group consisting of phenyl, halogen or CF 3 ; R',R" are independently from n and from each other hydrogen, lower alkyl, lower alkoxy, halogen or hydroxy; R 3 , R 4 are independently from each other hydrogen, lower alkyl, lower alkoxy, phenyl or halogen; R 5 is hydrogen, lower alkyl, -(CH 2 ) n -CF 3 or -(CH 2 ) n -cycloalkyl; R 6 is hydrogen or halogen; R 7 is hydrogen or lower alkyl; R 8 is hydrogen, lower alkyl, lower alkinyl, -(CH 2 ) n -CF 3 ,-(CH 2 ) n -cycloalkyl or -(CH 2 ) n -phenyl, optionally substituted by halogen; R 9 is hydrogen, lower alkyl, -C(O)H, -C(O)-lower alkyl, -C(O)-CF 3 ,-C(O)-CH 2 F,-C(O)-CHF 2 ,-C(O)-cycloalkyl,-C(O)-(CH 2 ) n -O-lower alkyl,-C(O)O-(CH 2 ) n -cycloalkyl, -C(O)-phenyl, optionally substituted by one or more substituents selected from the group consisting of halogen or -C(O)O-lower alkyl, or is -S(O) 2 -lower alkyl, -S(O) 2 -CF 3 ,-(CH 2 ) n -cycloalkyl or is -(CH 2 ) n -phenyl, optionally substituted by halogen; n is 0, 1, 2, 3 or 4; and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixture thereof. These compounds may be used for the treatment of Alzheimer’s disease.
摘要翻译：本发明涉及式（I）的丙二酰胺衍生物，其中：R 1是以下基团之一（式a），b），c），d））; R 2是低级烷基，低级炔基， - （CH 2）n O-低级烷基， - （CH 2）n S-低级烷基， - （CH 2）n -CN， - （CR'R“ CR'R“）n-CHF 2， - （CR'R”）n -CH 2 F， - （CH 2）n C（O）O-低级烷基， - （CH 2）n-卤素，或是 - （CH 2）任选被一个或多个选自苯基，卤素或CF 3的取代基取代; R'，R“独立地为n和彼此独立地为氢，低级烷基，低级烷氧基，卤素或羟基; R 3，R 4彼此独立地为氢，低级烷基，低级烷氧基，苯基或卤素; R 5是氢，低级烷基， - （CH 2）n -CF 3或 - （CH 2）n - 环烷基; R 6是氢或卤素; R 7是氢或低级烷基; R 8是任选被卤素取代的氢，低级烷基，低级炔基， - （CH 2）n -CF 3， - （CH 2）n - 环烷基或 - （CH 2） R 9是氢，低级烷基，-C（O）H，-C（O） - 低级烷基，-C（O）-CF 3，-C（O）-CH 2 F，-C（O） -C（O） - 环烷基，-C（O） - （CH 2）n O-低级烷基，-C（O）O-（CH 2）n - 环烷基，-C（O） - 苯基，任选被一个或多个或选自卤素或-C（O）O-低级烷基，或者是-S（O）2 - 低级烷基，-S（O）2-CF 3， - （CH 2）n - （CH 2）n - 苯基，任选被卤素取代; n为0,1,2,3或4; 和药学上合适的酸加成盐，旋光纯对映异构体，外消旋体或非对映体混合物。这些化合物可用于治疗阿尔茨海默病。

2. 发明申请

WO2007020190A1 FLUORO SUBSTITUTED 2-OXO AZEPAN DERIVATIVES 审中-公开
标题翻译：氟替代2-OXO AZEPAN衍生物
公开(公告)号：WO2007020190A1
公开(公告)日：2007-02-22
申请号：PCT/EP2006/064935
申请日：2006-08-02
申请人： F. HOFFMANN-LA ROCHE AG , FLOHR, Alexander , GALLEY, Guido , JAKOB-ROETNE, Roland , KITAS, Eric Argirios , WOSTL, Wolfgang
发明人： FLOHR, Alexander , GALLEY, Guido , JAKOB-ROETNE, Roland , KITAS, Eric Argirios , WOSTL, Wolfgang
IPC分类号： C07D223/12 , C07D413/12 , C07D401/12 , C07D403/12 , C07D409/14 , A61K31/55 , A61P25/28 , A61P35/00
CPC分类号： C07D409/14 , C07D223/12 , C07D401/12 , C07D403/12 , C07D413/12
摘要： The invention relates to compounds of general formula (I), wherein R 1 is lower alkyl substituted by halogen, or is aryl or heteroaryl, unsubstituted or substituted by halogen; R 2 is heterocycloalkyl, aryl or heteroaryl, which are unsubstituted or substituted by one or more substituents, selected from the group consisting of halogen, lower alkyloxy, lower alkyl substituted by halogen, O-lower alkyl substituted by halogen or are substituted by C(O)-NR" 2 , (CR 2 )m-C(O)-R’ heteroaryl or S(O) 2 -lower alkyl; R 3 /R 3’ , R 4 /R 4’ and R 5 /R5’ are independently from each other hydrogen or fluoro, wherein at least one of R4/R4’ or R 5 /R 5’ is always fluoro; R' is aryl or hydroxy; R" is hydrogen, cycloalkyl or is heterocycloalkyl; R is hydrogen or lower alkyl; m is 0, 1, 2 or 3; and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. It has been found that the compounds of general formula (I) are γ-secretase inhibitors and the related compounds may be useful in the treatment of Alzheimer's disease or common cancers including but not limited to cervical carcinomas and breast carcinomas and malignancies of the hematopoietic system.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1为被卤素取代的低级烷基，或未取代或被卤素取代的芳基或杂芳基; R 2是未取代的或被一个或多个选自以下的取代基取代的杂环烷基，芳基或杂芳基：卤素，低级烷氧基，被卤素取代的低级烷基，被卤素或被C（O）-NR“2取代，（CR 2）m C（O）-R'杂芳基或S（O） /低级烷基; R 3，R 3，R 3，R 4，R 4，R 4， R 5 / R 5'或R 5'或R 5'中的至少一个独立地为氢或氟，其中R 4 / R 4'或R 5' 总是氟; R'是芳基或羟基; R“是氢，环烷基或杂环烷基; R是氢或低级烷基; m为0,1,2或3; 以及药学上合适的酸加成盐，旋光纯对映异构体，外消旋体或非对映体混合物。已经发现通式（I）的化合物是γ-分泌酶抑制剂，相关化合物可用于治疗阿尔茨海默病或常见癌症，包括但不限于宫颈癌和乳腺癌以及造血系统的恶性肿瘤。

3. 发明申请

WO2005040126A1 SUBSTITUTED DIBENZO-AZEPINE AND BENZO-DIAZEPINE DERIVATIVES USEFUL AS GAMMA-SECRETASE INHIBITORS 审中-公开
标题翻译：用作GAMMA-分泌酶抑制剂的替代二苯并嗪和苯并二氮吡啶衍生物
公开(公告)号：WO2005040126A1
公开(公告)日：2005-05-06
申请号：PCT/EP2004/010821
申请日：2004-09-27
申请人： F. HOFFMAN-LA ROCHE AG , FLOHR, Alexander , GALLEY, Guido , JAKOB-ROETNE, Roland , KITAS, Eric, Argirios , PETERS, Jens-Uwe , WOSTL, Wolfgang
发明人： FLOHR, Alexander , GALLEY, Guido , JAKOB-ROETNE, Roland , KITAS, Eric, Argirios , PETERS, Jens-Uwe , WOSTL, Wolfgang
IPC分类号： C07D223/18
CPC分类号： C07D409/12 , C07D223/16 , C07D223/18 , C07D243/12 , C07D243/24
摘要： The present invention relates to compounds of the general formula (I) Wherein R 1 is -(CHR’) q -aryl or -(CHR') q -heteroaryl, which are unsubstituted or mono, di- or tri-substituted by lower alkyl, lower alkoxy, CF 3 or halogen, or is lower alkyl, lower alkenyl, -(CH 2 ) n -Si(CH 3 ) 3 , -(CH 2 ) n -O-lower alkyl, -(CH 2 )n-S-lower alkyl, -(CH 2 ) q -cycloalkyl, -(CH 2 ) n -[CH(OH)] m -(CF 2 )p-CH q F( 3-q) , or is -(CH 2 )n-CR 2 -CF 3 , wherein the two R radicals form together with the carbon atom a cycloalkyl ring; R' is hydrogen or lower alkyl; n is 1, 2 or 3; in is 0 or 1; p is 0, 1, 2, 3, 4, 5 or 6; q is 0, 1, 2 or 3; R 2 is hydrogen or lower alkyl; R 3 is hydrogen, lower alkyl, -CH 2 CF 2 CF 3 , CH 2 CF 3 , (CH 2 ) 2 CF 3 , CF 3 , CHF 2 , CF 3 , CHF 2 , CH 2 F, or is aryl, optionally mono, di or tri-substituted by halogen, or is (CH 2 ) n NR 5 R 6 , wherein R 5 and R 6 are independently from each other hydrogen or lower alkyl; R 4 is one of the following groups wherein R 7 is hydrogen, lower akl, -(CH 2 ) n -CF 3 or -(CH 2 ) n -cycloalkyl; R 8 is hydrogen, lower alkyl, -C(O)-phenyl, -C(O)-lower alkyl, -C(O)O-(CH 2 ) n - cycloalkyl, -C(O)O-(CH 2 ) n -lower alkyl, -C(O)NH-(CH 2 ) n -lower alkyl or -C(O)NH(CH 2 ).-CyClOalkYl; R 9 is hydrogen, lower alkyl, -(CH 2 ) n -cycloalkyl or -(CH 2 ) n -CF 3 ; and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racernates or diastereomeric mixtures thereof for the treatment of Alzheimer's disease..
摘要翻译：本发明涉及通式（I）的化合物，其中R 1是 - （CHR'）q-芳基或 - （CHR'）q-杂芳基，它们是未被取代的或被一个或二个或三个被低级烷基，低级烷氧基，CF 3或卤素，或低级烷基，低级烯基， - （CH 2）n -Si（CH 3）3 - ，（CH 2）n O-低级烷基， - （CH 2） CH 2）q - 环烷基， - （CH 2）n - [CH（OH）] m - （CF 2）p-CHFF（3-q）或 - 是（CH 2）n CR 2 CF 3，与碳原子一起为环烷基环; R'是氢或低级烷基; n为1,2或3; in是0或1; p是0，1，2，3，4，5或6; q为0,1,2或3; R 2是氢或低级烷基; R 3是氢，低级烷基，-CH 2 CF 2 CF 3，CH 2 CF 3，（CH 2）2 CF 3，CF 3，CHF 2，CF 3，CHF 2，CH 2 F，或者是芳基，任选地单，二或被卤素三取代，或是（CH 2）n NR 5 R 6，其中R 5和R 6彼此独立地是氢或低级烷基; R 4是下列基团之一，其中R 7是氢，低级ak， - （CH 2）n -CF 3或 - （CH 2）n - 环烷基; R8是氢，低级烷基，-C（O） - 苯基，-C（O） - 低级烷基，-C（O）O-（CH2）n-环烷基，-C（O）O-（CH2）低级烷基，-C（O）NH-（CH 2）n - 低级烷基或-C（O）NH（CH 2） R 9是氢，低级烷基， - （CH 2）n - 环烷基或 - （CH 2）n -CF 3; 以及用于治疗阿尔茨海默氏病的药学上合适的酸加成盐，光学纯对映异构体，ernernate或非对映体混合物。

4. 发明申请

WO2006005486A1 SULFONAMIDE DERIVATIVES 审中-公开
标题翻译：磺酰胺衍生物
公开(公告)号：WO2006005486A1
公开(公告)日：2006-01-19
申请号：PCT/EP2005/007268
申请日：2005-07-06
申请人： F. HOFFMANN-LA ROCHE AG , GALLEY, Guido , KITAS, Eric, Argirios , JAKOB-ROETNE, Roland
发明人： GALLEY, Guido , KITAS, Eric, Argirios , JAKOB-ROETNE, Roland
IPC分类号： C07D223/08
CPC分类号： C07D223/12 , C07D403/12
摘要： The invention relates to compounds of the general formula (I), wherein R 1 -R 5 and R 2’ -R 4’ are as described in the claims and to pharmaceutically suitable acid additon salts, optical pure enantiomers, racemates or diastereomeric mixtures thereof for the treatment of Alzheimer’s disease or common cancers.
摘要翻译：本发明涉及通式（I）的化合物，其中R

5. 发明申请

WO2004100958A1 2, 3, 4, 5-TETRAHYDROBENZO[F][1, 4]OXAZEPINE-5-CARBOXYLIC ACID AMIDE DERIVATIVES AS GAMMA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER’S DISEASE 审中-公开
标题翻译： 2，3，4，5-TETRAHYDROBENZO [F] [1,4]氧氮杂-5-羧酸酰胺衍生物作为治疗阿尔茨海默病的GAMMA-分泌酶抑制剂
公开(公告)号：WO2004100958A1
公开(公告)日：2004-11-25
申请号：PCT/EP2004/005177
申请日：2004-05-14
申请人： F. HOFFMANN-LA ROCHE AG , GALLEY, Guido , GOODNOW, Robert, Alan, Jr. , PETERS, Jens, Uwe
发明人： GALLEY, Guido , GOODNOW, Robert, Alan, Jr. , PETERS, Jens, Uwe
IPC分类号： A61K31/553
CPC分类号： C07D413/04 , C07D267/14
摘要： The invention relates to benzoxazepinone derivatives of formula (I) wherein R 1 is hydrogen, lower alkoxy, halogen or -NR'R"; n is 1 or 2; R',R" are independently from each other hydrogen or lower alkyl; R 2 is hydrogen, lower alkyl, -(CH 2 ) m -cycloalkyl, -(CH 2 ) m -phenyl or -(CH 2 ) m -O-lower alkyl; m is 0,1or 2; R 3 is lower alkyl, -(CH 2 ) m -C(O)O-lower alkyl, cycloalkyl or -(CH 2 ) m -phenyl, which is unsusbtituted or substituted by one or two substituents, selected from the group consisting of halogen or lower alkyl; R 4 is -(CH 2 ) ο -phenyl, which is unsusbtituted or substituted by one or two substituents, selected from the group consisting of halogen, trifluoromethyl, -NR'R", nitro or _ SO 2 NH 2 , or is - cycloalkyl, unsubstituted or substituted by phenyl, or is - (CR'R") ο -heterocyclyl, selected from the group defined in claim 1 and o is 1 or 2; and to pharmaceutically suitable acid addition salts thereof. These compounds are good γ-secretase inhibitors for the treatment of Alzheimer's disease.
摘要翻译：本发明涉及式（I）的苯并氧杂吖庚因酮衍生物，其中R 1是氢，低级烷氧基，卤素或-NR'R“; n是1或2; R'，R”彼此独立地是氢或低级烷基 ; R 2是氢，低级烷基， - （CH 2）m - 环烷基， - （CH 2）m - 苯基或 - （CH 2）m -O-低级烷基; m为0,1或2; R 3是低级烷基， - （CH 2）m C（O）O-低级烷基，环烷基或 - （CH 2）m - 苯基，其未取代或被一个或两个取代基取代，所述取代基选自卤素或低级烷基 R 4是 - （CH 2） - 亚 - 苯基，其是未取代的或被一个或两个选自卤素，三氟甲基，-NR'R“，硝基或SO 2 NH 2的取代基取代，或者是 - 或未被取代或被苯基取代的环烷基，或为选自权利要求1所定义的基团的 - （CR'R“） - 微 - 杂环基，且o为1或2; 和其药学上合适的酸加成盐。这些化合物是用于治疗阿尔茨海默病的良好γ-分泌酶抑制剂。

6. 发明申请

WO2013104591A1 HETEROCYCLIC DERIVATIVES AS TRACE AMINE ASSOCIATED RECEPTORS (TAARS) 审中-公开
标题翻译：作为胺类相关受体（TAARS）的杂环衍生物
公开(公告)号：WO2013104591A1
公开(公告)日：2013-07-18
申请号：PCT/EP2013/050170
申请日：2013-01-08
申请人： F. HOFFMANN-LA ROCHE AG , GALLEY, Guido , GOERGLER, Annick , NORCROSS, Roger , PFLIEGER, Philippe
发明人： GALLEY, Guido , GOERGLER, Annick , NORCROSS, Roger , PFLIEGER, Philippe
IPC分类号： C07D413/10 , C07D413/14 , C07D471/04 , A61K31/5377 , A61P25/00
CPC分类号： C07D413/10 , C07D413/14 , C07D471/04 , C07D487/04
摘要： The present invention relates to compounds of formula (I) wherein R 1 is a one or two membered heteroaryl group, selected from the group consisting of formula (a), (b), (c), (d), (e), (f), (g), (h), (i), (j); R 2 is hydrogen or halogen; or R 1 and R 2 may form together with the carbon atoms to with they are attached the following rings formula (k), (l), (m), (n), (o). R 3 is hydrogen, halogen or lower alkyl; n is 1 or 2; R 4 is phenyl, optionally substituted by one or two substituents, selected from halogen or cyano, or is pyridinyl, optionally substituted by halogen, or is tetrahydropyran, or is -NH-C(O)-phenyl, optionally substituted by halogen; R 5 is hydrogen or halogen; R 6 – R 13 are phenyl, optionally substituted by halogen: R 14 is –NH-C(O)-phenyl, substituted by halogen; R 15 is hydrogen, lower alkyl substituted by halogen or is halogen; R 16 is hydrogen or lower alkoxy; R 17 is pyridinyl, optionally substituted by lower alkoxy or lower alkyl substituted by halogen; or to a pharmaceutically suitable acid addition salt thereof, to all racemic mixtures, to all their corresponding enantiomers and/or optical isomers and to all tautomeric forms of compounds of formula I. 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是选自式（a），（b），（c），（d），（e），（d） f），（g），（h），（i），（j）; R2是氢或卤素; 或者R 1和R 2可以与碳原子一起形成，它们连接下列环（k），（l），（m），（n），（o）。 R3是氢，卤素或低级烷基; n为1或2; R4是任选被一个或两个选自卤素或氰基的取代基取代的苯基，或是任选被卤素取代的吡啶基，或是四氢吡喃，或者是任选被卤素取代的-NH-C（O） - 苯基; R5是氢或卤素; R6-R13是任选被卤素取代的苯基; R 14是被卤素取代的-NH-C（O） - 苯基; R 15是氢，被卤素取代的低级烷基或是卤素; R 16是氢或低级烷氧基; R 17为吡啶基，任选被低级烷氧基或被卤素取代的低级烷基取代; 或其药学上合适的酸加成盐，与所有相应的对映异构体和/或光学异构体以及式I化合物的所有互变异构体形式。式I化合物与微量胺相关联具有良好的亲和力受体（TAAR），特别是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。

7. 发明申请

WO2012168260A1 PYRAZOLE DERIVATIVES 审中-公开
标题翻译：吡唑衍生物
公开(公告)号：WO2012168260A1
公开(公告)日：2012-12-13
申请号：PCT/EP2012/060627
申请日：2012-06-06
申请人： F. HOFFMANN-LA ROCHE AG , GALLEY, Guido , GHELLAMALLAH, Cédric , NORCROSS, Roger , PFLIEGER, Philippe
发明人： GALLEY, Guido , GHELLAMALLAH, Cédric , NORCROSS, Roger , PFLIEGER, Philippe
IPC分类号： A61K31/4245 , C07D413/12 , C07D413/14 , A61P25/00
CPC分类号： C07D413/14 , C07D413/12
摘要： The invention relates to compounds of formula wherein R 1 is hydrogen or phenyl, optionally substitutes by halogen, CN or lower alkoxy or lower alkoxy substituted by halogen; R 2 is hydrogen or lower alkyl; R 3 is hydrogen or lower alkyl or is phenyl optionally substituted by one or more substituents, selected from halogen, cyano or lower alkoxy substituted by halogen, or is pyridinyl, optionally substituted by halogen or lower alkyl substituted by halogen, or is pyrimidinyl, optionally substituted by lower alkyl substituted by halogen, or is pyrazinyl, optionally substituted by halogen, cyano or lower alkyl substituted by halogen; R 4 is hydrogen, lower alkyl or phenyl; Z is a bond, -CH 2 - or -O-; or to a pharmaceutically suitable acid addition salt thereof. It has now been found that the compounds of formulas IA and IB 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：本发明涉及下式的化合物，其中R 1是氢或苯基，任选地被卤素，CN或被卤素取代的低级烷氧基或低级烷氧基取代; R2是氢或低级烷基; R 3是氢或低级烷基或被任选被一个或多个选自卤素，氰基或被卤素取代的低级烷氧基的取代基取代的苯基，或是任选被卤素取代的吡啶基或被卤素取代的低级烷基，或者是嘧啶基，被卤素取代的低级烷基，或任选被卤素，氰基或被卤素取代的低级烷基取代的吡嗪基; R4是氢，低级烷基或苯基; Z是键，-CH 2 - 或-O-; 或其药学上合适的酸加成盐。现已发现式IA和IB的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。

8. 发明申请

WO2011057973A1 OXAZOLINE DERIVATIVES FOR TREATMENT OF CNS DISORDERS 审中-公开
标题翻译：用于治疗CNS病症的OXAZOLINE衍生物
公开(公告)号：WO2011057973A1
公开(公告)日：2011-05-19
申请号：PCT/EP2010/066960
申请日：2010-11-08
申请人： F. HOFFMANN-LA ROCHE AG , GALLEY, Guido , NORCROSS, Roger , POLARA, Alessandra
发明人： GALLEY, Guido , NORCROSS, Roger , POLARA, Alessandra
IPC分类号： C07D263/28 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , A61K31/421 , A61K31/4439 , A61K31/506 , A61K31/422 , A61P25/00
CPC分类号： C07D263/28 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04
摘要： The invention relates to compounds of formula (I) wherein the definitions of X, R and R 1 are provided in claim 1. It has now been found that the compounds of formula (I) have a good affinity to the trace amine associated receptors (TAARs), especially for TAARl. 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X，R和R 1的定义在权利要求1中提供。现已发现式（I）化合物与微量胺相关受体（TAARs）具有良好的亲和力），特别是TAARl。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。

9. 发明申请

WO2008058867A2 SUBSTITUTED 4-IMIDAZOLES 审中-公开
标题翻译：取代的4-咪唑
公开(公告)号：WO2008058867A2
公开(公告)日：2008-05-22
申请号：PCT/EP2007/061921
申请日：2007-11-06
申请人： F. HOFFMANN-LA ROCHE AG , GALLEY, Guido , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
发明人： GALLEY, Guido , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger , STALDER, Henri
IPC分类号： C07D403/06 , C07D401/06 , C07D413/06 , A61K31/4178
CPC分类号： C07D401/06 , C07D403/06 , C07D413/06
摘要： The present invention relates to compounds of formula (I) wherein R 1 is hydrogen or lower alkyl; R 2 is hydrogen or lower alkyl; R 3 is hydrogen, lower alkyl, lower alkoxy, phenyloxy, benzyloxy, halogen or lower alkyl substituted by halogen; R 4 is hydrogen or lower alkyl; X is -CH 2 -, -CH- or -O-; Y is -CH 2 -, -CH 2 CH 2 -, -CH- or a bond; when X is -O-, then Y is -CH 2 -; Z is -CH 2 - or -CH-; m is 1 or 2; when m is 2, R 2 may be the same or not; n is 1 or 2; when n is 2, R 3 may be the same or not; and to pharmaceutically acceptable acid addition 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）的化合物，其中R 1为氢或低级烷基; R 2是氢或低级烷基; R 3是氢，低级烷基，低级烷氧基，苯氧基，苄氧基，卤素或被卤素取代的低级烷基; R 4是氢或低级烷基; X是-CH 2 - ， - CH-或-O-; Y是-CH 2 - ， - CH 2 CH 2 - ， - CH-或键; 当X是-O-时，则Y是-CH 2 - ; - Z为-CH 2 - 或-CH-; m是1或2; 当m是2时，R 2可以相同或不相同; n是1或2; 当n是2时，R 3可以相同或不同; 并涉及药学上可接受的酸加成盐。已经发现式I化合物对痕量胺相关受体（TAAR）具有良好的亲和力，特别是对于TAAR1。该化合物可用于治疗抑郁症，焦虑症，双相性精神障碍，注意力缺陷多动障碍（ADHD），压力相关障碍，精神障碍如精神分裂症，神经疾病如帕金森病，神经变性障碍如阿尔茨海默病，癫痫症，偏头痛，高血压，药物滥用和代谢障碍例如进食障碍，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，体温平衡紊乱和障碍，睡眠和昼夜节律紊乱以及心血管疾病

10. 发明申请

WO2010010014A1 4,5-DIHYDRO-OXAZOL-2-YL DERIVATIVES 审中-公开
标题翻译： 4,5-DIHYDRO-OXAZOL-2-YL衍生物
公开(公告)号：WO2010010014A1
公开(公告)日：2010-01-28
申请号：PCT/EP2009/059026
申请日：2009-07-15
申请人： F. HOFFMANN-LA ROCHE AG , GALLEY, Guido , GOERGLER, Annick , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger
发明人： GALLEY, Guido , GOERGLER, Annick , GROEBKE ZBINDEN, Katrin , NORCROSS, Roger
IPC分类号： C07D263/28 , C07D413/12 , A61K31/421 , A61K31/422 , A61P25/00 , A61P3/04 , A61P3/06 , A61P3/10
CPC分类号： C07D263/28 , C07D413/12
摘要： The invention relates to compounds of formula (I) wherein R 1 is hydrogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, halogen, cyano, nitro, hydroxy, C(O)O-lower alkyl, S(O) 2 -lower alkyl, C(O)OCH 2 -phenyl, OCH 2 -phenyl, tetrazol-1-yl, phenyl optionally substituted by halogen, or is phenyloxy optionally substituted by halogen, or is benzyl optionally substituted by halogen or is benzyloxy optionally substituted by halogen, wherein the substituents for n> 1 may be the same or different; X is -O-(CH 2 ) 2 -, -O-CHR"-CH 2 -, -O-CH 2 -CHR', -O-CR'' 2 -CH 2 -, -(CH 2 ) 2 -CHR', -CHR'-(CH 2 ) 2 -, -CR" 2 -(CH 2 ) 2 -, -CH 2 -CHR'-CH 2 -, -CH 2 -CR'' 2 -CH 2 -, -CHR"-O-CH 2 -, -CH 2 -O-CH 2 -, -CR'' 2 -O-CH 2 -, -CF 2 (CH 2 ) 2 -, -CR" 2 -CH 2 -, -SiR" 2 -(CH 2 ) 2 -, -S-(CH 2 ) 2 -, -S(O) 2 -(CH 2 ) 2 -, -(CH 2 ) 4 -, -CH 2 -O-(CH 2 ) 2 -, for m being 0, 1, 2 or 3; R' is lower alkyl, lower alkoxy or lower alkyl substituted by halogen; R'' is lower alkyl or lower alkyl substituted by halogen; R 2 is hydrogen or lower alkyl; Y is aryl, cycloalkyl or heteroaryl; n is 1, 2 or 3; or to a pharmaceutically suitable acid addition salt. The compounds disclosed in the present formula (I) may be used for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress- related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, 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，低级烷基，低级烷氧基，被卤素取代的低级烷基，被卤素，卤素，氰基，硝基，羟基，C（O）O-低级烷基取代的低级烷氧基， S（O）2 - 低级烷基，C（O）OCH 2 - 苯基，OCH 2 - 苯基，四唑-1-基，任选被卤素取代的苯基，或任选被卤素取代的苯氧基，或是任选被卤素取代的苄基，任选被卤素取代的苄氧基，其中n> 1的取代基可以相同或不同; X是-O-（CH 2）2 - ， - O-CHR“-CH 2 - ，-O-CH 2 -CHR'，-O-CR''2-CH 2 - ， - （CH 2）2 -CHR' ' - （CH 2）2 - ， - CR“2-（CH 2）2 - ， - CH 2 -CHR'-CH 2 - ， - CH 2 -CR''2-CH 2 - ， - CHR”-O-CH 2 - ， - CH 2 （CH 2）2 - ， - CR“2 -CH 2 - ，-SiR”2-（CH 2）2 - ， - S-（CH 2）2 - 2，-S（O）2 - （CH 2）2 - ， - （CH 2）4 - ， - CH 2 -O-（CH 2）2 - ，其中m为0,1,2或3; R' 低级烷氧基或被卤素取代的低级烷基; R“为被卤素取代的低级烷基或低级烷基; R 2为氢或低级烷基; Y为芳基，环烷基或杂芳基; n为1,2或3; 本发明式（I）中公开的化合物可用于治疗与微量胺相关受体的生物学功能有关的疾病，所述疾病是抑郁症，焦虑障碍，双相情感障碍，注意缺陷多动障碍，压力相关疾病，精神病，精神分裂症，神经系统疾病，帕金森病，神经变性疾病，阿尔茨海默病，癫痫，偏头痛，药物滥用和代谢紊乱，饮食失调，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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