250371-89-2

Upstream product

• 369-34-6 3,4-difluoronitrobenzene 
• 141699-55-0 tert-butyl 3-hydroxyazetidine-1-carboxylate 

Downstream Products

• 250372-01-1 tert-butyl 3-(4-amino-2-fluorophenoxy)azetidine-1-carboxylate 

Relevant academic research and scientific papers

SUBSTITUTED AZETIDINE DERIVATIVES AS TAAR LIGANDS

The present invention relates to a compound of formula I wherein R1 is hydrogen, methoxy or fluoro; R2/R2' are independently from each other hydrogen, methoxy or fluoro; R3/R4 are independently from each other hydrogen or halogen; R is hydrogen or fluoro; L1 is -CH2-, -NR'-, -0-, -S-, CF2- or CH=; R' is hydrogen or lower alkyl; L2 is a bond, -C(0)NH-, -NH-, -CH2NHC(O)-, -NHC(O)- or -NHC(0)NH-; R is hydrogen, halogen, lower alkoxy, cyano or is phenyl optionally substituted by one or more substituents, selected from halogen, lower alkyl substituted by halogen or lower alkoxy, or is a five or six membered heteroaryl, selected from pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl or pyrazolyl, which heteroaryls are optionally substituted by one or more substituents, selected from halogen, lower alkyl, lower alkoxy, cyano, cycloalkyl, lower alkyl substituted by halogen, lower alkoxy substituted by halogen or by phenyl substituted by halogen; N is a ring nitrogen atom in position 1 or 2; or to a pharmaceutically suitable acid addition salt thereof. The compounds of formulas I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and 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.

5- [4- (AZETIDIN-3-YL0XY) -PHENYL] -2-PHENYL-5H-THIAZ0L0 [5,4-C] PYRIDIN-4-0NE DERIVATIVES AND THEIR USE AS MCH RECEPTOR ANTAGONISTS

The present invention relates to a melanin concentrating hormone antagonist compound of formula I: wherein "-----" is absent or is optionally a bond; q is 1 or 2; R1 is independently selected from hydrogen, -C1-C2 alkyl, halo, hydroxy, -C1-C2 haloalkyl, -C1-C3 alkoxy, cyano, -O-C3-C4 cycloalkyl, and -OC1-C2 haloalkyl; R2 is selected from the group consisting of hydrogen, -C1-C3 alkyl, hydroxy, -C1-C3 alkoxy, cyano, -C1-C2 haloalkyl, -OC1-C2 haloalkyl, and halo; R3 is selected from the group consisting of hydrogen, -C1-C4 alkyl, -C2-C4 haloalkyl, -C2-C4 alkylOH, -C3-C6 cycloalkyl, -CH2C3-C6 cyxloalkyl, -C2-C4 alkyl-O-C1-C4 alkyl, -C(O)C1-C4 alkyl, -C(O)C1-C4 haloalkyl, -CH2-thiazole, phenyl, benzyl, tetrahydrothiopyranyl, and tetrahydropyranyl, wherein the cycloalkyl, tetrahydrothiopyranyl, tetrahydropyranyl and thiazolyl group is optionally substituted with one or two groups independently selected from the group consisting of halo, hydroxy, C1-C2 alkyl, and -C1-C2 haloalkyl; or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture thereof,, useful in the treating, preventing or ameliorating of symptoms associated with obesity and related diseases.

NOVEL MCH RECEPTOR ANTAGONISTS

The present invention relates to a melanin concentrating hormone antagonist compound of formula (I): wherein R1, Ra, Rb, R2, L1, R3, R4 and R5 are as defined, or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture of diasteromers thereof useful in the treatment, obesity and related diseases.