公开(公告)号：US11697636B2

公开(公告)日：2023-07-11

申请号：US17096438

申请日：2020-11-12

Applicant: Hoffmann-La Roche Inc.

Inventor： Katrin Groebke Zbinden ,  Roger Norcross ,  Phillippe Pfileger

IPC: C07D207/09 ,  C07D207/10 ,  C07D207/12 ,  C07D211/26 ,  C07D241/04 ,  C07D263/32 ,  C07D265/30 ,  C07D267/08 ,  C07D267/10 ,  C07D295/135 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  A61K9/20 ,  C07D495/04

CPC classification number: C07D207/09 ,  A61K9/2018 ,  C07D207/10 ,  C07D207/12 ,  C07D211/26 ,  C07D241/04 ,  C07D263/32 ,  C07D265/30 ,  C07D267/08 ,  C07D267/10 ,  C07D295/135 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D495/04

Abstract: The invention relates to compounds of formula




wherein R, R1, R2, X, and Y are as defined herein and to a pharmaceutically suitable acid addition salt thereof.

Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can 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.

公开(公告)号：US20210061760A1

公开(公告)日：2021-03-04

申请号：US17096438

申请日：2020-11-12

Applicant: Hoffmann-La Roche Inc.

Inventor： Katrin Groebke Zbinden ,  Roger Norcross ,  Phillippe Pfileger

IPC: C07D207/09 ,  C07D207/10 ,  C07D207/12 ,  C07D211/26 ,  C07D241/04 ,  C07D265/30 ,  C07D267/08 ,  C07D295/135 ,  C07D401/04 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  A61K9/20 ,  C07D263/32 ,  C07D267/10 ,  C07D401/14 ,  C07D403/12 ,  C07D495/04

Abstract: The invention relates to compounds of formula wherein R, R1, R2, X, and Y are as defined herein and to a pharmaceutically suitable acid addition salt thereof.
Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can 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.

公开(公告)号：US20200048194A1

公开(公告)日：2020-02-13

申请号：US16653210

申请日：2019-10-15

Applicant: Hoffmann-La Roche Inc.

Inventor： Katrin Groebke Zbinden ,  Roger Norcross ,  Phillippe Pfileger

IPC: C07D207/09 ,  C07D207/10 ,  C07D207/12 ,  C07D211/26 ,  C07D241/04 ,  C07D265/30 ,  C07D267/08 ,  C07D295/135 ,  C07D401/04 ,  C07D401/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  A61K9/20 ,  C07D263/32 ,  C07D267/10 ,  C07D401/14 ,  C07D403/12 ,  C07D495/04

Abstract: The invention relates to compounds of formula wherein R, R1, R2, X, and Y are as defined herein and to a pharmaceutically suitable acid addition salt thereof.Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can 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.