1185019-97-9Relevant academic research and scientific papers
Discovery, Structure-Activity Relationships, and in Vivo Evaluation of Novel Aryl Amides as Brain Penetrant Adaptor Protein 2-Associated Kinase 1 (AAK1) Inhibitors for the Treatment of Neuropathic Pain
Hartz, Richard A,Ahuja, Vijay T.,Nara, Susheel J.,Kumar, C.M. Vijaya,Brown, Jeffrey M.,Bristow, Linda J.,Rajamani, Ramkumar,Muckelbauer, Jodi K.,Camac, Daniel,Kiefer, Susan E.,Hunihan, Lisa,Gulianello, Michael,Lewis, Martin,Easton, Amy,Lippy, Jonathan S.,Surti, Neha,Pattipati, Sreenivasulu N.,Dokania, Manoj,Elavazhagan, Saravanan,Dandapani, Kumaran,Hamman, Brian D.,Allen, Jason,Kostich, Walter,Bronson, Joanne J.,Macor, John E.,Dzierba, Carolyn D.
, p. 11090 - 11128 (2021/08/03)
Effective treatment of chronic pain, in particular neuropathic pain, without the side effects that often accompany currently available treatment options is an area of significant unmet medical need. A phenotypic screen of mouse gene knockouts led to the d
Vinyl-Fluorene Molecular Wires for Voltage Imaging with Enhanced Sensitivity and Reduced Phototoxicity
Boggess, Steven C.,Gandhi, Shivaani S.,Benlian, Brittany R.,Miller, Evan W.
supporting information, p. 11903 - 11907 (2021/08/20)
Fluorescent voltage indicators are an attractive alternative for studying the electrical activity of excitable cells; however, the development of indicators that are both highly sensitive and low in toxicity over long-term experiments remains a challenge.
AMINO-ACID ANILIDES AS SMALL MOLECULE MODULATORS OF IL-17
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Page/Page column 139; 143, (2020/07/14)
The present invention relates to a compound according to formula I (I) and pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments.
ARYL AMIDE KINASE INHIBITORS
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, (2015/02/02)
The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
GAMMA SECRETASE MODULATORS
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Page/Page column 60, (2011/08/08)
The invention relates to compounds of formula wherein R1, R1′, R2, R3, n, A, and hetaryl are defined herein or to pharmaceutically active acid addition salts thereof. The present compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.
GAMMA SECRETASE MODULATERS
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Page/Page column 126, (2011/08/21)
The invention relates to compounds of formula ( I ) wherein R1/R1' are independently from each other hydrogen, halogen, lower alkoxy or cyano; R2 is lower alkyl, halogen, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, lower alkyl substituted by OR, =0, -C(O)O-lower alkyl, -C(O)NH-lower alkyl, cyano, CH2-O-lower alkyl, cycloalkyl, NRR'or is -O-(CH2)o-phenyl optionally substituted by halogen, or is -(CH2)o-phenyl optionally substituted by one, two or three substituents, selected from halogen, -(CH2)o-cyano, lower alkyl, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, C(O)H, -CH2-NH2-, -CH2-NH-C(O)O-lower alkyl, -CH2-NH-C(O)-lower alkyl, -CH2-NH-lower alkyl, -CH2-NH-S(O)2-lower alkyl, lower alkoxy or by lower alkoxy substituted by halogen, or is -(CH2)o-cycloalkyl, or is -(CH2)o-heterocycloalkyl which is optionally substituted by halogen, CF3, lower alkyl, -CH2CN, -C(O)-lower alkyl, -C(O)O-lower alkyl or S(O)2-lower alkyl, or is heteroaryl selected from the group consisting of furanyl, pyrazinyl, pyridinyl, benzooxazolyl or benzoimidazolyl which are optionally substituted by lower alkyl, or is 4-methyl-3,4-dihydro-2H-benzo[l,4]oxazine R and R' are independently from each other hydrogen or lower alkyl, and o is 0 or 1; R3 may occur once or twice and is lower alkyl; A is Formula a), b), c), d), e), f), h), i), j) and Formula k); R2' is hydrogen, lower alkyl, lower alkyl substituted by halogen, C(O)-lower alkyl, S(O)2-lower alkyl or phenyl optionally substituted by halogen; hetaryl is a 5 or 6 membered N, S or O-containing heteroaryl group; n is O, 1, 2 or 3; if n is 2 or 3, R2 may be the same or not; or to pharmaceutically active acid addition salts thereof. The present compounds of formula ( I ) are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of β-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi- infarct dementia, dementia pugilistica and Down syndrome.
BICYCLIC COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION
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Page/Page column 48-49, (2010/08/08)
The present disclosure provides a series of compounds of the formula (I) which reduce β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production, wherein
MODULATORS FOR AMYLOID BETA
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Page/Page column 79, (2009/09/07)
The invention relates to compounds of formula wherein the substituents are as described in claim 1. Compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposi
