Title:
ISOTHIOUREA DERIVATIVE OR ISOUREA DERIVATIVE HAVING BACE1 INHIBITORY ACTIVITY
Document Type and Number:
WIPO Patent Application WO/2010/113848
Kind Code:
A1
Abstract:
Disclosed is a compound represented by formula (I) or the like, which serves as an agent for treatment of diseases that are induced by production, secretion and/or deposition of amyloid β protein.
Specifically disclosed is a compound represented by formula (I), a pharmaceutically acceptable salt thereof or a solvate thereof.
(In the formula, R1 represents a substituted amino group or the like; R2 represents a halogen atom or the like; R3 represents a substituted or unsubstituted lower alkyl group or the like; RA and RB each independently represents a hydrogen atom, a substituted or unsubstituted lower alkyl group or the like; RC and RD each independently represents a hydrogen atom, a substituted or unsubstituted lower alkyl group or the like, or alternatively, RC and RD combine together and form a substituted or unsubstituted carbocyclic ring together with an adjacent carbon atom; and ring A represents a heterocyclic ring or a carbocyclic ring.)
Inventors:
TAMURA YUUSUKE (JP)
SUZUKI SHINJI (JP)
MATSUMOTO SAE (JP)
HORI AKIHIRO (JP)
KOORIYAMA YUUJI (JP)
SUZUKI SHINJI (JP)
MATSUMOTO SAE (JP)
HORI AKIHIRO (JP)
KOORIYAMA YUUJI (JP)
Application Number:
PCT/JP2010/055528
Publication Date:
October 07, 2010
Filing Date:
March 29, 2010
Export Citation:
Assignee:
SHIONOGI & CO (JP)
TAMURA YUUSUKE (JP)
SUZUKI SHINJI (JP)
MATSUMOTO SAE (JP)
HORI AKIHIRO (JP)
KOORIYAMA YUUJI (JP)
TAMURA YUUSUKE (JP)
SUZUKI SHINJI (JP)
MATSUMOTO SAE (JP)
HORI AKIHIRO (JP)
KOORIYAMA YUUJI (JP)
International Classes:
C07C275/28; A61K31/44; A61K31/4965; A61K31/505; A61P25/28; A61P43/00; C07C335/12; C07C335/16; C07C335/18; C07D213/81; C07D213/85; C07D239/42; C07D241/24; C07D401/12; C07D405/12
Domestic Patent References:
| WO2007049532A1 | 2007-05-03 | |||
| WO2008133274A1 | 2008-11-06 | |||
| WO2008133273A1 | 2008-11-06 | |||
| WO2009151098A1 | 2009-12-17 | |||
| WO2002096897A1 | 2002-12-05 | |||
| WO2004043916A1 | 2004-05-27 | |||
| WO2005058311A1 | 2005-06-30 | |||
| WO2005097767A1 | 2005-10-20 | |||
| WO2006041404A1 | 2006-04-20 | |||
| WO2006041405A1 | 2006-04-20 | |||
| WO1995009619A2 | 1995-04-13 | |||
| WO1994012165A2 | 1994-06-09 | |||
| WO1996018608A1 | 1996-06-20 |
Foreign References:
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| JP2006519758A | 2006-08-31 | |||
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Other References:
SIDDIQUI, SALIMUZZAMAN ET AL.: "Some extensions of von Braun (cyanogen bromide) reaction on organic bases", PROCEEDINGS OF THE PAKISTAN ACADEMY OF SCIENCES, vol. 25, no. 3, 1988, pages 231 - 240, XP008167061
HIKARU OZAWA ET AL.: "Pharmacological Actions of 2-Aminoethylisothiuronium (AET) Derivatives. I", JOURNAL OF THE PHARMACEUTICAL SOCIETY OF JAPAN, vol. 88, no. 2, 1968, pages 156 - 162, XP008167083
CURTIS, R. F. ET AL.: "The biosynthesis of phenols. VIII. The synthesis of (2-carboxy-3,5- dihydroxyphenyl)propan-2-one(C-acetyl-o- orsellinic acid)", JOURNAL OF THE CHEMICAL SOCIETY, 1964, pages 5382 - 5385, XP008167059
BURTON, H. ET AL.: "Addition reactions of quinones. I. The reaction of cysteine and thiourea and its derivatives with some quinones", JOURNAL OF THE CHEMICAL SOCIETY, 1952, pages 2193 - 2196, XP008167062
KOJI MATSUI: "Yomo Bochuzai no Kenkyu (the 6th report) Kagaku Kozo to Yomo Shokugai Boshi Koka tono Kankei (III)", JOURNAL OF SYNTHETIC ORGANIC CHEMISTRY, vol. 8, no. 10, 1950, JAPAN, pages HO61 - HO65, XP008167060
DESAI, RANCHHODJI DAJIBHAI ET AL.: "The condensation of thiocarbamides with chloroacetic acid and the conversion of arylformamidinethiolacetic acids into pseudothiohydantoin derivatives", RECUEIL DES TRAVAUX CHIMIQUES DES PAYS-BAS ET DE LA BELGIQUE, vol. 54, 1935, pages 118 - 121, XP055099183
See also references of EP 2415756A4
FILER: "Isotopes in the Physical and Biomedical Sciences, Vol. 1, Labeled Compounds (Part A", 1987, article "The Preparation and Characterization of Tritiated Neurochemicals", pages: 155 - 192
THEODORA W GREEN: "Protective Groups in Organic Synthesis", JOHN WILEY & SONS
ORG. LETT., vol. 7, 2005, pages 355
HIKARU OZAWA ET AL.: "Pharmacological Actions of 2-Aminoethylisothiuronium (AET) Derivatives. I", JOURNAL OF THE PHARMACEUTICAL SOCIETY OF JAPAN, vol. 88, no. 2, 1968, pages 156 - 162, XP008167083
CURTIS, R. F. ET AL.: "The biosynthesis of phenols. VIII. The synthesis of (2-carboxy-3,5- dihydroxyphenyl)propan-2-one(C-acetyl-o- orsellinic acid)", JOURNAL OF THE CHEMICAL SOCIETY, 1964, pages 5382 - 5385, XP008167059
BURTON, H. ET AL.: "Addition reactions of quinones. I. The reaction of cysteine and thiourea and its derivatives with some quinones", JOURNAL OF THE CHEMICAL SOCIETY, 1952, pages 2193 - 2196, XP008167062
KOJI MATSUI: "Yomo Bochuzai no Kenkyu (the 6th report) Kagaku Kozo to Yomo Shokugai Boshi Koka tono Kankei (III)", JOURNAL OF SYNTHETIC ORGANIC CHEMISTRY, vol. 8, no. 10, 1950, JAPAN, pages HO61 - HO65, XP008167060
DESAI, RANCHHODJI DAJIBHAI ET AL.: "The condensation of thiocarbamides with chloroacetic acid and the conversion of arylformamidinethiolacetic acids into pseudothiohydantoin derivatives", RECUEIL DES TRAVAUX CHIMIQUES DES PAYS-BAS ET DE LA BELGIQUE, vol. 54, 1935, pages 118 - 121, XP055099183
See also references of EP 2415756A4
FILER: "Isotopes in the Physical and Biomedical Sciences, Vol. 1, Labeled Compounds (Part A", 1987, article "The Preparation and Characterization of Tritiated Neurochemicals", pages: 155 - 192
THEODORA W GREEN: "Protective Groups in Organic Synthesis", JOHN WILEY & SONS
ORG. LETT., vol. 7, 2005, pages 355
Attorney, Agent or Firm:
TAKAYAMA, Hirotsugu et al. (JP)
Hiromitsu Takayama (JP)
Hiromitsu Takayama (JP)
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