Overcoming hERG issues for brain-penetrating cathepsin S inhibitors: 2-Cyanopyrimidines. Part 2

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 19, 2008, Pages 5280-5284

  Irie, Osamu ^a   Kosaka, Takatoshi ^a   Kishida, Masashi ^a   Sakaki, Junichi ^a   Masuya, Keiichi ^a   Konishi, Kazuhide ^a   Yokokawa, Fumiaki ^a   Ehara, Takeru ^a   Iwasaki, Atsuko ^a   Iwaki, Yuki ^a   Hitomi, Yuko ^a   Toyao, Atsushi ^a   Gunji, Hiroki ^a   Teno, Naoki ^a   Iwasaki, Genji ^a   Hirao, Hajime ^a   Kanazawa, Takanori ^a   Tanabe, Keiko ^a   Hiestand, Peter C ^b   Malcangio, Marzia ^c   Fox, Alyson J ^c   Bevan, Stuart J ^c   Yaqoob, Mohammed ^c   Culshaw, Andrew J ^c   Hart, Terance W ^c   Hallett, Allan ^c   more..

^a Novartis Institutes for BioMedical Research   (Japan)

^b NOVARTIS PHARMA AG   (Switzerland)

^c NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH   (United States)

Author keywords

Brain penetrating; Cathepsin S inhibitor; hERG; Multiple sclerosis; Neuropathic pain

Indexed keywords

2 CYANOPYRIMIDINE DERIVATIVE; CATHEPSIN L; CATHEPSIN S; CATHEPSIN S INHIBITOR; POTASSIUM CHANNEL HERG; SPIRO[3.5]NON 6 YL METHYLAMINE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DISTRIBUTION VOLUME; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG CLEARANCE; DRUG EFFICACY; DRUG HALF LIFE; DRUG POTENCY; DRUG SELECTIVITY; HYDROPHOBICITY; MALE; MULTIPLE SCLEROSIS; NEUROPATHIC PAIN; NONHUMAN; RAT; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; BRAIN; CATHEPSINS; COMBINATORIAL CHEMISTRY TECHNIQUES; CYSTEINE ENDOPEPTIDASES; ETHER-A-GO-GO POTASSIUM CHANNELS; HUMANS; MALE; MOLECULAR STRUCTURE; MULTIPLE SCLEROSIS; PAIN; PYRIMIDINES; RATS; RATS, SPRAGUE-DAWLEY; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 52049104957     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.08.067     Document Type: Article

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