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11. 发明专利

CA2879176C TRIAZOLE CARBOXAMIDE DERIVATIVES 未知
公开(公告)号：CA2879176C
公开(公告)日：2020-10-27
申请号：CA2879176
申请日：2013-09-13
申请人： HOFFMANN LA ROCHE
发明人： GALLEY GUIDO , GHELLAMALLAH CEDRIC , NORCROSS ROGER , PFLIEGER PHILIPPE
IPC分类号： C07D403/12 , A61K31/4192 , A61K31/4196 , A61P25/00 , C07D413/12
摘要： The invention relates to compounds of formula (I), wherein R1 is phenyl or pyridinyl, optionally substituted by halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen and lower alkoxy substituted by halogen; X1 is -N= or CH; X2 is CR2 or =N-; X3 is -N= or CH; with the proviso that only two of X1, X2 or X3 are nitrogen; wherein is a triazole group, selected from R2 is hydrogen or lower alkyl; Z is a bond, -O- or -CH2-; or to pharmaceutically suitable acid addition salts thereof. It has now been found that the compounds of formulas I have a good affinity to the trace amine associated receptors (TAARs), especially for TAARI. 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.

12. 发明专利

CA2834675C SUBSTITUTED BENZAMIDE DERIVATIVES 未知
公开(公告)号：CA2834675C
公开(公告)日：2019-09-03
申请号：CA2834675
申请日：2012-06-06
申请人： HOFFMANN LA ROCHE
发明人： GALLEY GUIDO , NORCROSS ROGER , PFLIEGER PHILIPPE , TRUSSARDI RENE
IPC分类号： C07D265/30 , A61K31/4245 , A61P25/00 , C07D401/12 , C07D413/12 , C07D413/14
摘要： The present invention relates to compounds of formula (I) wherein R1 is hydrogen, halogen, cyano, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen or C(O)NH2, or is phenyl optionally substituted by halogen, cyano or lower alkoxy substituted by halogen, or is 2,2-difluorobenzo[d][1,3]dioxol-5-yl, or is 6-(trifluoromethyl)pyrazin-2-yl or 5-(trifluoromethyl)pyrazin-2-yl or is 6-(trifluoromethyl)pyrimidin-4-yl, or is 6- (trifluoromethyl)pyridin-3-yl, or is 5-cyanopyrazin-2-yl or is 2- (trifluoromethyl)pyrimidin-4-yl; n is 1 or 2 R2 is halogen, lower alkyl or cyano and R3 is hydrogen, or R2 is hydrogen and R3 is halogen, lower alkyl or cyano; X is a bond, -NR'-, -CH2NH- or -CHR'-; R' is hydrogen or lower alkyl; Z is a bond, -CH2- or -O-; Ar is phenyl or is heteroaryl, selected from the group consisting of 1H-indazole-3yl, pyridine-2-yl, pyridine-3-yl, pyridine-4-yl, pyrimidine-5-yl, lH-pyrazole-3-yl, 1H- pyrazole-4-yl or lH-pyrazole-5-yl; or to a pharmaceutically suitable acid addition salt thereof, which may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse, 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.

13. 发明专利

CR20180443A DERIVADO DE MORFOLINA 未知
公开(公告)号：CR20180443A
公开(公告)日：2018-11-21
申请号：CR20180443
申请日：2017-03-14
申请人： HOFFMANN LA ROCHE
发明人： HOENER MARIUS; , NORCROSS ROGER , GALLEY GUIDO; , PFLIEGER PHILIPPE;
IPC分类号： C07D413/12 , A61K31/4245 , A61P25/00
摘要： La presente invención se refiere a un compuesto de fórmula I, y a una sal de adición de ácido farmacéuticamente aceptable del mismo con una buena afinidad por los receptores asociados a aminas traza (TAAR), específicamente por TAAR1, para el tratamiento de determinadas enfermedades del SNC.

14. 发明专利

PL3149002T3 Pochodne 5-oksa-2-azabicyklo[2.2.2]oktan-4-ylu i 5-oksa-2-azabicyklo [2.2.1]heptan-4-ylu jako modulatory TAAR1 未知
公开(公告)号：PL3149002T3
公开(公告)日：2018-08-31
申请号：PL15724624
申请日：2015-05-22
申请人： HOFFMANN LA ROCHE
发明人： CECERE GIUSEPPE , GALLEY GUIDO , HU YIMIN , NORCROSS ROGER , PFLIEGER PHILIPPE , SHEN HONG
IPC分类号： C07D491/08 , A61K31/5386 , A61P25/00

15. 发明专利

CO2018007515A2 Derivado de 5-etil-4-metil-pirazol-3-carboxamida que tiene actividad como agonista de taar 未知
公开(公告)号：CO2018007515A2
公开(公告)日：2018-07-31
申请号：CO2018007515
申请日：2018-07-17
申请人： HOFFMANN LA ROCHE
发明人： GALLEY GUIDO , HOENER MARIUS , NORCROSS ROGER , PFLIEGER PHILIPPE
IPC分类号： C07D413/12 , A61K31/4245 , A61P25/00
摘要： La presente invención se refiere a un compuesto de fórmula I, y a una sal de adición de ácido farmacéuticamente aceptable del mismo con una buena afinidad por los receptores asociados a aminas traza (TAAR), específicamente por TAAR1, para el tratamiento de determinadas enfermedades del SNC.

16. 发明专利

ES2654653T3 Derivados de pirazol-carboxamida como moduladores de TAAR para su uso en el tratamiento de varios trastornos, tales como depresión, diabetes y enfermedad de Parkinson 未知
公开(公告)号：ES2654653T3
公开(公告)日：2018-02-14
申请号：ES13759754
申请日：2013-09-11
申请人： HOFFMANN LA ROCHE
发明人： GALLEY GUIDO , NORCROSS ROGER , PFLIEGER PHILIPPE
IPC分类号： C07D403/12 , A61K31/4155 , A61K31/454 , A61K31/5377 , A61P25/00 , C07D401/12 , C07D413/12 , C07D413/14 , C07D417/14
摘要： Un compuesto de fórmula **Fórmula** en la que R1 es fenilo, opcionalmente sustituido con halógeno, alquilo C1-7, cicloalquilo C3-6, alcoxi C1-7, ciano, alquilo C1-7 sustituido con halógeno, alquilo C1-7 sustituido con hidroxi, alcoxi C1-7 sustituido con halógeno o alcoxi C1-7 sustituido con hidroxi; o es piridin-2, 3 o 4-ilo, opcionalmente sustituido con halógeno, alquilo C1-7, cicloalquilo C3-6, ciano, alquilo C1-7 sustituido con halógeno, alquilo C1-7 sustituido con hidroxilo, alcoxi C1-7, alcoxi C1-7 sustituido con halógeno, o alcoxi C1-7 sustituido con hidroxilo; o es pirimidin-2, 4 o 5-ilo, opcionalmente sustituido con halógeno, alquilo C1-7, cicloalquilo-C3-6, alquilo C1-7 sustituido con hidroxi o alquilo C1-7 sustituido con halógeno, o es pirazin-2- ilo, opcionalmente sustituido con halógeno, alquilo C1-7, cicloalquilo C3-6, alquilo C1-7 sustituido con halógeno, alquilo C1-7 sustituido con hidroxi o ciano, o es 2,2-difluorobenzo[d][1,3]dioxol-5-ilo o es tiazolilo, opcionalmente sustituido con alquilo C1-7 sustituido con halógeno; R2 es hidrógeno o alquilo C1-7; R3 es hidrógeno, amino o alquilo C1-7; Z es un enlace, -CH2- u -O-; o una sal de adición de ácido farmacéuticamente adecuada del mismo.

18. 发明专利

CA2780161C SUBSTITUTED BENZAMIDE DERIVATIVES 未知
公开(公告)号：CA2780161C
公开(公告)日：2017-09-26
申请号：CA2780161
申请日：2010-12-17
申请人： HOFFMANN LA ROCHE
发明人： GROEBKE ZBINDEN KATRIN , NORCROSS ROGER , PFLIEGER PHILIPPE
IPC分类号： C07D207/09 , A61K31/4025 , A61K31/4523 , A61K31/5355 , C07D207/10 , C07D207/12 , C07D211/26 , C07D241/04 , C07D265/30 , C07D401/04 , C07D401/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The invention relates to compounds of formula I wherein R is hydrogen or lower alkyl; R1 is -(CH2)n-(O)o-heterocycloalkyl or -C(O)-heterocycloalkyl, wherein the heterocycloalkyl group is optionally substituted by lower alkyl, hydroxy, halogen or by -(CH2)p-aryl; n is 0, 1 or 2; o is 0 or 1; p is 0, 1 or 2; R2 is CF3, cycloalkyl, optionally substituted by lower alkoxy or halogen, or is indan-2-yl, or is heterocycloalkyl, optionally substituted by heteroaryl, or is aryl or heteroaryl, wherein the aromatic rings are optionally substituted by one or two substituents, selected from lower alkyl, halogen, heteroaryl, hydroxy, CF3, OCF3, OCH2CF3, OCH2-cycloalkyl, OCH2C(CH2OH)(CH2C1)(CH3), S-lower alkyl, lower alkoxy, CH2-lower alkoxy, lower alkinyl or cyano, or by-C(O)-phenyl, -O-phenyl, -O- CH2-phenyl, phenyl or -CH2-phenyl, and wherein the phenyl rings may optionally be substituted by halogen, -C(O)-lower alkyl, -C(O)OH or -C(O)O-lower alkyl, or the aromatic rings are optionally substituted by heterocycloalkyl, OCH2-oxetan-3-yl or O-tetrahydropyran-4-yl, optionally substituted by lower alkyl; X is a bond, -NR'-, -CH2NH-, -CHR''-, -(CHR'')q-O-, -O-(CHR'')q- or -(CH2)2-; Y is a bond or -CH2- R' is hydrogen or lower alkyl, R'' is hydrogen, lower alkyl, CF3, lower alkoxy, q is 0, 1, 2 or 3; or to a pharmaceutically suitable acid addition salt thereof. It has now 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 Parkinsons disease, neurodegenerative disorders such as Alzheimers 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.

19. 发明专利

MY162461A SUBSTITUTED BENZAMIDE DERIVATIVES 未知
公开(公告)号：MY162461A
公开(公告)日：2017-06-15
申请号：MYPI2013003963
申请日：2012-06-06
申请人： HOFFMANN LA ROCHE
发明人： GALLEY GUIDO , NORCROSS ROGER , PFLIEGER PHILIPPE , RENÉ TRUSSARDI
IPC分类号： C07D265/30 , A61K31/4245 , A61P25/00 , C07D401/12 , C07D413/12 , C07D413/14
摘要： THE PRESENT INVENTION RELATES TO COMPOUNDS OF FORMULA WHEREIN R1 IS HYDROGEN, HALOGEN, CYANO, LOWER ALKYL, LOWER ALKYL SUBSTITUTED BY HALOGEN, LOWER ALKOXY, LOWER ALKOXY SUBSTITUTED BY HALOGEN OR C(O)NH2, OR IS PHENYL OPTIONALLY SUBSTITUTED BY HALOGEN, CYANO OR LOWER ALKOXY SUBSTITUTED BY HALOGEN, OR IS 2,2-DIFLUOROBENZO[D][1,3)DIOXOL-5-YL, OR IS 6-(TRIFLUOROMETHYL)PYRAZIN-2-YL OR 5-(TRIFLUOROMETHYL)PYRAZIN-2-YL OR IS 6-(TRIFLUOROMETHYL)PYRIMIDIN-4-YL, OR IS 6-(TRIFLUOROMETHYL)PYRIDIN-3-YL, OR IS 5-CYANOPYRAZIN-2-YL OR IS 2-(TRIFLUOROMETHYL)PYRIMIDIN-4-YL; N IS 1 OR 2 R2 IS HALOGEN, LOWER ALKYL OR CYANO AND R3 IS HYDROGEN, OR R2 IS HYDROGEN AND R3 IS HALOGEN, LOWER ALKYL OR CYANO; X IS A BOND, -NR’-, -CH2NH- OR -CHR’-; R’ IS HYDROGEN OR LOWER ALKYL; Z IS A BOND, -CH2- OR -O-; AR IS PHENYL OR IS HETEROARYL, SELECTED FROM THE GROUP CONSISTING OF 1H-INDAZOLE-3YL, PYRIDINE-2-YL, PYRIDINE-3-YL, PYRIDINE-4-YL, PYRIMIDINE-5-YL, 1H-PYRAZOLE-3-YL, 1H-PYRAZOLE-4-YL OR 1H-PYRAZOLE-5-YL; OR TO A PHARMACEUTICALLY SUITABLE ACID ADDITION SALT THEREOF, WHICH MAY BE USED FOR THE TREATMENT OF DEPRESSION, ANXIETY DISORDERS, BIPOLAR DISORDER, ATTENTION DEFICIT HYPERACTIVITY DISORDER (ADHD), STRESS-RELATED DISORDERS, PSYCHOTIC DISORDERS, SCHIZOPHRENIA, NEUROLOGICAL DISEASES, PARKINSON’S DISEASE, NEURODEGENERATIVE DISORDERS, ALZHEIMER’S DISEASE, EPILEPSY, MIGRAINE, HYPERTENSION, SUBSTANCE ABUSE, 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. (NO SUITABLE

20. 发明专利

BR112013031324A2 derivados de pirazol 未知
公开(公告)号：BR112013031324A2
公开(公告)日：2016-11-29
申请号：BR112013031324
申请日：2012-06-06
申请人： HOFFMANN LA ROCHE
发明人： GHELLAMALLAH CÉDRIC , GALLEY GUIDO , PFLIEGER PHILIPPE , NORCROSS ROGER
IPC分类号： C07D413/14 , A61K31/4245 , A61P25/00 , C07D413/12
摘要： resumo patente de invenção: "derivados de pirazol". a presente invenção refere-se a composto de fórmula ia ou ib em que r1 é hidrogênio ou fenila, opcionalmente substituído com halogênio, cn ou alcóxi inferior ou alcóxi inferior substituído com halogênio; r2 é hidrogênio ou alquila inferior; r3 é hidrogênio ou alquila inferior ou é fenila opcionalmente substituído com um ou mais substituintes, selecionados dentre halogênio, ciano ou alcóxi inferior substituído com halogênio, ou é piridinila, opcionalmente substituído com halogênio ou alquila inferior substituído com halogênio, ou é pirimidinila, opcionalmente substituído com alquila inferior substituído com halogênio, ou é pirazinila, opcionalmente substituído com halogênio, ciano ou alquila inferior substituído com halogênio; r4 é hidrogênio, alquila inferior ou fenila; z é uma ligação, -ch2- ou -o-; ou a um sal de adição de ácido farmaceuticamente adequado do mesmo. foi agora descoberto que os compostos de fórmulas ia e ib têm boa afinidade para receptores associados a aminas traço (taars), especialmente para a taar1. os compostos podem ser usados para o tratamento de depressão, transtornos de ansiedade, transtorno bipolar, transtorno de deficiência de atenção com hiperatividade (adhd), transtornos relacionados com estresse, transtornos psicóticos tais como esquizofrenia, doenças neurológicas tais como mal de parkinson, distúrbios neurodegenerativos tais como mal de alzheimer, epilepsia, enxaqueca, hipertensão, dependência química e distúrbios metabólicos tais como distúrbios alimentares, diabetes, complicações do diabetes, obesidade, dislipidemia, distúrbios de consumo e assimilação de energia, distúrbios e malfuncionamento da homeostasia da temperatura do corpo, distúrbios do sono e do ritmo circadiano, e distúrbios cardiovasculares.

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