Title:
pillage non as tissue-transglutaminase inhibitor -- a derivative
Document Type and Number:
Japanese Patent JP6236445
Kind Code:
B2
Abstract:
Pyridinone derivatives (I) and stereoisomeric forms, E/Z isomers, enantiomers, mixtures of enantiomers, diastereomers, mixtures of diastereomers, racemates, tautomers, anomers, keto-enol forms, betaine form, prodrugs, solvates, hydrates and salts, in new. Pyridinone derivatives of formula (I) and stereoisomeric forms, E/Z isomers, enantiomers, mixtures of enantiomers, diastereomers, mixtures of diastereomers, racemates, tautomers, anomers, keto-enol forms, betaine form, prodrugs, solvates, hydrates and salts, in new. E1, E2 : -CO- or -SO 2; Rc : -NYY1a, -NH-CH 2-COOH, -NH-CH(CH 3)-COOH, -NH-CH (CH 2CH 2SCH 3)-COOH, -NH-CH(CH 2OH)-COOH, -NH-CH(CH 2SH)-COOH, -NH-CH(CH 2CONH 2)-COOH,-NH-CH(CH 2CH 2CONH 2)-COOH, [(1-carboxy-2-methyl-propyl)amino], [(1-carboxy-2-methyl-butyl)amino], [(1-carboxy-3-methyl-butyl)amino], [(1-carboxy-2-hydroxy-propyl)amino], [(1-benzyl-2-hydroxy-2-oxo-ethyl)amino], [[2-hydroxy-2-oxo-1-(p-tolylmethyl)ethyl]amino], [(1-carboxy-3-hydroxy-3-oxo-propyl)amino], [(1-carboxy-4-hydroxy-4-oxo-butyl)amino], piperazin-1-yl, morpholino, 1-piperidyl, (4-phenylpiperazin-1-yl), (4-benzylpiperazin-1-yl), (4-phenylpiperazin-1-yl), (4-methylpiperazin-1-yl), (2-oxo-1-piperidyl), (2,6-dioxo-1-piperidyl), isoindolin-2-yl, azepan-1-yl, azetidin-1-yl, aziridin-1-yl, 4,5-dihydrotriazol-1-yl, (3-methylimidazolidin-1-yl), pyrrolidin-1-yl, (2-oxopyrrolidin-1-yl), or (2,5-dioxopyrrolidin-1-yl); and Z : -CH 3, -C 2H 5, -C 3H 7, -CH(CH 3) 2,-C 4H 9, -C 6H 5, -CH 2-C 6H 5, -OCH 3, -OC 2H 5, -OC 3H 7, -OCH(CH 3) 2, -OC 4H 9, -OC 6H 5, -OCH 2C 6H 5, -OCH=CH 2 or -OCH 2-CH=CH 2. N.B. Rd is not defined. Full Definitions are given in the DEFINITIONS (Full Definitions) Field. Independent claims are included for: (1) a pharmaceutical composition comprising (I) and carrier, excipient or solvent; and (2) preparation of (I). [Image] ACTIVITY : Antiinflammatory; Neuroprotective; Anticonvulsant; Nootropic; Antiparkinsonian; Ophthalmological; Antiseborrheic; Dermatological; Antipsoriatic; Thrombolytic. MECHANISM OF ACTION : Transglutaminase 2 inhibitor.
Inventors:
Viewhold christian
Gerlach Ube
Hills martin
Pastel Nac Ralph
Weber Johannes
Gerlach Ube
Hills martin
Pastel Nac Ralph
Weber Johannes
Application Number:
JP2015522048A
Publication Date:
November 22, 2017
Filing Date:
July 12, 2013
Export Citation:
Assignee:
Zedira Game Behr
International Classes:
C07D213/75; A61K31/44; A61K31/443; A61K31/4436; A61K31/4439; A61K31/4545; A61K31/455; A61K31/496; A61K31/538; A61P7/02; A61P11/00; A61P17/00; A61P17/06; A61P17/10; A61P25/14; A61P25/16; A61P25/28; A61P27/12; A61P31/10; A61P41/00; A61P43/00; C07D213/82; C07D401/12; C07D405/12; C07D409/12; C07D413/12; C07D417/12; C07D493/10
Domestic Patent References:
| JP2010509195A | ||||
| JP2003530435A | ||||
| JP2007511607A | ||||
| JP3128360A | ||||
| JP2013180955A |
Other References:
BANNWARTH,L. et al,JOURNAL OF MEDICINAL CHEMISTRY,2006年,49(15),4657-4664
WILLOUGHBY,C.A. et al.,BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2002年,12(16),2197-2200
GOLEC,J.M.C. et al,BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,1997年,7(17),2181-2186
WILLOUGHBY,C.A. et al.,BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2002年,12(16),2197-2200
GOLEC,J.M.C. et al,BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,1997年,7(17),2181-2186
Attorney, Agent or Firm:
Nagoya International Patent Service Corporation