Title:
AMINODIHYDROTHIAZINE DERIVATIVE
Document Type and Number:
WIPO Patent Application WO/2007/049532
Kind Code:
A1
Abstract:
A BACE 1 inhibitor containing, as an active ingredient, any one of a compound represented by the formula (I): (wherein ring A is an optionally substituted carbocyclic group or optionally substituted heterocyclic group; E is lower alkylene, etc.; X is S, O, or NR1 (R1 is hydrogen or lower alkyl); R2a, R2b, R3a, R3b, R4a, and R4b each independently is hydrogen, halogeno, hydroxy, etc.; n and m each independently is an integer of 0-3, provided that n+m is 1-3; and R5 is hydrogen, optionally substituted lower alkyl, etc.), a pharmaceutically acceptable salt thereof, and a solvate of either.
Inventors:
KOBAYASHI NAOTAKE (JP)
UEDA KAZUO (JP)
ITOH NAOHIRO (JP)
SUZUKI SHINJI (JP)
SAKAGUCHI GAKU (JP)
KATO AKIRA (JP)
YUKIMASA AKIRA (JP)
HORI AKIHIRO (JP)
KORIYAMA YUJI (JP)
HARAGUCHI HIDEKAZU (JP)
YASUI KEN (JP)
KANDA YASUHIKO (JP)
UEDA KAZUO (JP)
ITOH NAOHIRO (JP)
SUZUKI SHINJI (JP)
SAKAGUCHI GAKU (JP)
KATO AKIRA (JP)
YUKIMASA AKIRA (JP)
HORI AKIHIRO (JP)
KORIYAMA YUJI (JP)
HARAGUCHI HIDEKAZU (JP)
YASUI KEN (JP)
KANDA YASUHIKO (JP)
Application Number:
PCT/JP2006/321015
Publication Date:
May 03, 2007
Filing Date:
October 23, 2006
Export Citation:
Assignee:
SHIONOGI & CO (JP)
KOBAYASHI NAOTAKE (JP)
UEDA KAZUO (JP)
ITOH NAOHIRO (JP)
SUZUKI SHINJI (JP)
SAKAGUCHI GAKU (JP)
KATO AKIRA (JP)
YUKIMASA AKIRA (JP)
HORI AKIHIRO (JP)
KORIYAMA YUJI (JP)
HARAGUCHI HIDEKAZU (JP)
YASUI KEN (JP)
KANDA YASUHIKO (JP)
KOBAYASHI NAOTAKE (JP)
UEDA KAZUO (JP)
ITOH NAOHIRO (JP)
SUZUKI SHINJI (JP)
SAKAGUCHI GAKU (JP)
KATO AKIRA (JP)
YUKIMASA AKIRA (JP)
HORI AKIHIRO (JP)
KORIYAMA YUJI (JP)
HARAGUCHI HIDEKAZU (JP)
YASUI KEN (JP)
KANDA YASUHIKO (JP)
International Classes:
C07D239/14; A61K31/426; A61K31/505; A61K31/506; A61K31/535; A61K31/54; A61K31/541; A61K31/5415; A61K31/55; A61K31/551; A61K31/554; A61P25/28; A61P43/00; C07D239/24; C07D265/08; C07D277/18; C07D279/06; C07D279/08; C07D281/02; C07D405/04; C07D417/04; C07D417/10; C07D417/12; C07D417/14; C07D471/04
Domestic Patent References:
| WO2004014843A1 | 2004-02-19 | |||
| WO2004043916A1 | 2004-05-27 | |||
| WO2002096897A1 | 2002-12-05 | |||
| WO1996014842A1 | 1996-05-23 | |||
| WO2001087293A1 | 2001-11-22 | |||
| WO2004014843A1 | 2004-02-19 | |||
| WO2002096897A1 | 2002-12-05 | |||
| WO2004043916A1 | 2004-05-27 | |||
| WO2005058311A1 | 2005-06-30 | |||
| WO2005097767A1 | 2005-10-20 | |||
| WO2006041404A1 | 2006-04-20 | |||
| WO2006041405A1 | 2006-04-20 |
Foreign References:
| JPH08231521A | 1996-09-10 | |||
| JP2005509651A | 2005-04-14 | |||
| JP2005526005A | 2005-09-02 | |||
| JP2005517634A | 2005-06-16 | |||
| US20050165080A1 | 2005-07-28 | |||
| JP2005531520A | 2005-10-20 | |||
| JP2004149429A | 2004-05-27 | |||
| US3235551A | 1966-02-15 | |||
| US3227713A | 1966-01-04 | |||
| JPH0967355A | 1997-03-11 | |||
| JP2004149429A | 2004-05-27 |
Other References:
LIEBSCHER J. ET AL.: "2-ARYLIMINO-3-THIAZOLINES - FORMATION OF UNUSUAL TAUTOMERS OF 2-ARYLAMINO-THIAZOLINES - A REVISION", TETRAHEDRON LETTERS, vol. 26, no. 35, 1985, pages 4179 - 4180, XP003011652
GARCIA FERNANDEZ J.M. ET AL.: "Syntheses and Spectral Properties of beta-Idoureas and 2-Amino-4,4-diphenyl-2-oxazolines", JOURNAL OF HETEROCYCLIC CHEMISTRY, vol. 28, no. 3, 1991, pages 777 - 780, XP003011653
SCHAUMANN. ET AL.: "Stickstoffhaltige Funfring-Heterocyclen aus Carbodiimiden oder Ketenimine mit 3-Dimethylamino-2H-azirinen", LIEBIGS ANNALEN DER CHEMIE, no. 2, 1981, pages 290 - 305, XP003011654
GARCIA FERNANDEZ J.M. ET AL.: "Syntheses of beta-iodourea derivatives of carbohydrates and glycosylamino-oxazolines", CARBOHYDRATE RESEARCH, vol. 216, 1991, pages 21 - 32, XP003011655
COHEN N. ET AL.: "Synthesis of 2-Amino-5-, 6-dihydro-4H-1,3-thiazines and Related Compounds by Acid Catalyzed Cyclization of Allylic Isothiuronium Salts", JOURNAL OF HETEROCYCLIC CHEMISTRY, vol. 14, no. 5, 1977, pages 717 - 723, XP003011656
CAMBIE R.C. ET AL.: "vic-Iodothiocyanates and Iodoisothiocyanates. Part 2. New Syntheses of Thiazolidin-2-ones and 2-Amino-2-thiazolines", JOURNAL OF THE CHEMICAL SOCIETY, PERKIN TRANSACTIONS I, no. 3, 1979, pages 765 - 770, XP003011657
KONDRAT'EVA G.Y. ET AL.: "Noncyclic dimer of 4-methyl-2-(dimethylamino)oxazole", IZVESTIYA AKADEMII NAUK SSSR, SERIYA KHIMICHESKAYA, no. 7, 1977, pages 1680 - 1682, XP003011658
DATABASE CAPLUS [online] HUENIG S. ET AL.: "Azo dyes by oxidative coupling. XVIII. Synthesis of 3-substituted 2-thiazolone hydrazones and 2-thiazolone benzenesulfonylhydrazones", XP003011659, accession no. STN Database accession no. (1962:46595)
See also references of EP 1942105A4
JOURNAL OF HETEROCYCLIC CHEMISTRY, vol. 14, 1977, pages 717 - 723
JOURNAL OF ORGANIC CHEMISTRY, vol. 33, no. 8, 1968, pages 3126 - 3132
THEODORA W GREEN: "Protective Groups in Organic Synthesis", JOHN WILEY & SONS
GARCIA FERNANDEZ J.M. ET AL.: "Syntheses and Spectral Properties of beta-Idoureas and 2-Amino-4,4-diphenyl-2-oxazolines", JOURNAL OF HETEROCYCLIC CHEMISTRY, vol. 28, no. 3, 1991, pages 777 - 780, XP003011653
SCHAUMANN. ET AL.: "Stickstoffhaltige Funfring-Heterocyclen aus Carbodiimiden oder Ketenimine mit 3-Dimethylamino-2H-azirinen", LIEBIGS ANNALEN DER CHEMIE, no. 2, 1981, pages 290 - 305, XP003011654
GARCIA FERNANDEZ J.M. ET AL.: "Syntheses of beta-iodourea derivatives of carbohydrates and glycosylamino-oxazolines", CARBOHYDRATE RESEARCH, vol. 216, 1991, pages 21 - 32, XP003011655
COHEN N. ET AL.: "Synthesis of 2-Amino-5-, 6-dihydro-4H-1,3-thiazines and Related Compounds by Acid Catalyzed Cyclization of Allylic Isothiuronium Salts", JOURNAL OF HETEROCYCLIC CHEMISTRY, vol. 14, no. 5, 1977, pages 717 - 723, XP003011656
CAMBIE R.C. ET AL.: "vic-Iodothiocyanates and Iodoisothiocyanates. Part 2. New Syntheses of Thiazolidin-2-ones and 2-Amino-2-thiazolines", JOURNAL OF THE CHEMICAL SOCIETY, PERKIN TRANSACTIONS I, no. 3, 1979, pages 765 - 770, XP003011657
KONDRAT'EVA G.Y. ET AL.: "Noncyclic dimer of 4-methyl-2-(dimethylamino)oxazole", IZVESTIYA AKADEMII NAUK SSSR, SERIYA KHIMICHESKAYA, no. 7, 1977, pages 1680 - 1682, XP003011658
DATABASE CAPLUS [online] HUENIG S. ET AL.: "Azo dyes by oxidative coupling. XVIII. Synthesis of 3-substituted 2-thiazolone hydrazones and 2-thiazolone benzenesulfonylhydrazones", XP003011659, accession no. STN Database accession no. (1962:46595)
See also references of EP 1942105A4
JOURNAL OF HETEROCYCLIC CHEMISTRY, vol. 14, 1977, pages 717 - 723
JOURNAL OF ORGANIC CHEMISTRY, vol. 33, no. 8, 1968, pages 3126 - 3132
THEODORA W GREEN: "Protective Groups in Organic Synthesis", JOHN WILEY & SONS
Attorney, Agent or Firm:
TAKAYAMA, Hirotsugu et al. (Ltd. Intellectual Property Department 12-4 Sagisu 5-chome,, Fukushima-k, Osaka-shi Osaka02, JP)
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