319451-51-9Relevant academic research and scientific papers
SUBSTITUTED AZETIDINE DERIVATIVES AS TAAR LIGANDS
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Page/Page column 46; 47, (2016/03/22)
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.
NAMPT INHIBITORS
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Paragraph 1779, (2014/11/27)
Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.
NAMPT INHIBITORS
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Page/Page column 167, (2013/12/03)
Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.
5- [4- (AZETIDIN-3-YL0XY) -PHENYL] -2-PHENYL-5H-THIAZ0L0 [5,4-C] PYRIDIN-4-0NE DERIVATIVES AND THEIR USE AS MCH RECEPTOR ANTAGONISTS
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Page/Page column 26, (2008/12/06)
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.
Indoline derivatives I: Synthesis and Factor Xa (FXa) inhibitory activities
Noguchi, Tetsuji,Tanaka, Naoki,Nishimata, Toyoki,Goto, Riki,Hayakawa, Miho,Sugidachi, Atsuhiro,Ogawa, Taketoshi,Asai, Fumitoshi,Matsui, Yumi,Fujimoto, Koichi
, p. 163 - 174 (2007/10/03)
A series of bisamidine derivatives each having a ring structure in the center of the molecule was synthesized and their Factor Xa (FXa) inhibitory activities were evaluated. Among them, some indoline derivatives showed potent inhibitory activities in vitr
DIAMINOTHIAZOLES
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Page/Page column 28, (2010/02/05)
The present invention is directed to novel diaminothiazoles of formula These compounds inhibit cyclin-dependent kinase 4 (Cdk4) and are selective against Cdk2 and Cdk1. These compounds and their pharmaceutically acceptable salts and esters have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors. This invention is also directed to pharmaceutical compositions containing such compounds and to methods of treating or controlling cancer, most particularly the treatment 6r control of breast, lung and colon and prostate tumors.
