BENZENE DERIVATIVES, PROCESS FOR PREPARING THE SAME AND USE THEREOF

Title:

BENZENE DERIVATIVES, PROCESS FOR PREPARING THE SAME AND USE THEREOF

Document Type and Number:

WIPO Patent Application WO/2003/029199

Kind Code:

A1

Abstract:

Novel benzene derivatives represented by the general formula (&Verbar ), which exhibit vanilloid receptor agonism and are useful as preventive and therapeutic drugs for pollakisuria and urinary incontinence, analgesic, or the like: (&Verbar ) wherein R¹, R⁴ and R⁶ are each independently hydrogen, halogeno, or hydrocarbyl&semi R² is hydrocarbyl or a heterocyclic group&semi R³ is hydrocarbyl, NR^7’R⁷, or OR⁸ (wherein R^7’ is hydrogen or hydrocarbyl and R⁷ is a non−aromatic group, or alternatively R^7’and R⁷ together with the nitrogen atom adjacent thereto may form a ring&semi and R⁸ is hydrocarbyl or a heterocyclic group)&semi R⁵ is hydrocarbyl or a heterocyclic group (except quinolyl) and R^5’ is hydrogen or hydrocarbyl, or R⁵ and R^5’ together with the nitrogen atom adjacent thereto may form a ring&semi and R^5’’ is hydrogen or hydrocarbyl.

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Inventors:

MATSUMOTO TAKAHIRO (JP)
YAMAMOTO MASATAKA (JP)
NAGABUKURO HIROSHI (JP)
MOCHIZUKI MANABU (JP)

Application Number:

PCT/JP2002/009995

Publication Date:

April 10, 2003

Filing Date:

September 27, 2002

Export Citation:

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Assignee:

TAKEDA CHEMICAL INDUSTRIES LTD (JP)
MATSUMOTO TAKAHIRO (JP)
YAMAMOTO MASATAKA (JP)
NAGABUKURO HIROSHI (JP)
MOCHIZUKI MANABU (JP)

International Classes:

A61K31/17; A61K31/216; A61K31/357; A61K31/36; A61K31/4045; A61K31/4184; A61K31/42; A61K31/44; A61K31/4409; A61K31/445; A61K31/4453; A61K31/4468; A61K31/495; A61K31/55; A61K31/551; A61P1/06; A61P1/08; A61P1/14; A61P3/04; A61P3/06; A61P3/08; A61P9/00; A61P9/02; A61P9/10; A61P11/02; A61P13/02; A61P15/12; A61P17/00; A61P17/04; A61P17/06; A61P19/02; A61P25/00; A61P25/02; C07C275/38; C07C275/42; C07C309/66; C07C311/08; C07C311/21; C07C311/47; C07C317/42; C07C323/42; C07C323/44; C07C323/62; C07D207/14; C07D207/27; C07D209/08; C07D209/16; C07D211/46; C07D211/52; C07D211/58; C07D211/62; C07D213/30; C07D213/40; C07D213/56; C07D213/65; C07D213/74; C07D213/75; C07D215/08; C07D215/38; C07D217/02; C07D223/12; C07D233/54; C07D235/30; C07D261/14; C07D277/82; C07D295/13; C07D295/192; C07D295/215; C07D307/14; C07D307/52; C07D317/66; C07D321/10; C07D333/16; C07D207/26; (IPC1-7): C07C275/38; C07C275/42; C07D213/30; C07D213/40; C07D213/65; C07D213/75; C07D261/14; C07D295/20; C07D317/58; C07D317/66; C07D319/18; C07D321/10; A61K31/17; A61K31/216; A61K31/357; A61K31/36; A61K31/4045; A61K31/4184; A61K31/42; A61K31/44; A61K31/4409; A61K31/445; A61K31/4453; A61K31/4468; A61K31/495; A61K31/55; A61K31/551; A61P1/06; A61P1/08; A61P1/14; A61P3/04; A61P3/06; A61P3/08; A61P9/00; A61P9/02; A61P9/10; A61P11/02; A61P13/02; A61P15/12; A61P17/00; A61P17/04; A61P17/06; A61P19/02; A61P25/00; A61P25/02

Domestic Patent References:

WO2000047577A1

2000-08-17

Foreign References:

EP0135162A2	1985-03-27
JPH0680911A	1994-03-22
DE2458624A1	1975-07-03

Other References:

LINDNER W., LEITNER CH., URAY G.: "Liquid chromatographic separation of enantiomeric alkanolamines via diastereomeric tartaric acid monoesters", JOURNAL OF CHROMATOGRAPHY, vol. 316, 1984, pages 605 - 616, XP009007117
VON ZOELSS G.: "Zur synthese des kardioselektiven beta-Rezeptoren-Blockers Celiprolol", ARZNEIMITTEL-FORSCHUNG, vol. 33, no. 1A, 1983, pages 2 - 4, XP002963467
NOBUYOSHI SUMI ET AL.: "Celiprolol no taisha sanbutsu, bunkaibutsu, kyozatsubutsu, kogaku iseitai no mouth ni okeru kyusei dokusei shiken", PHARMACOMETRICS, vol. 38, no. 4, 1989, pages 295 - 303, XP002963468
VON HOFER O., SCHLOEGL K.: "Absolute Konfiguration und Enantiomere reinheit von Celiprolol", ARZNEIMITTEL-FORSCHUNG, vol. 36, no. 8, 1986, pages 1157 - 1161, XP002963469
ALMOTREFI ABDULRAHMAN A. ET AL.: "Synthesis and pharmacological evaluation of the antifibrillatory effect of fluorinated derivatives of carazolol and ceriprolol: comparison with propranolol", GENERAL PHARMACOLOGY, vol. 24, no. 3, 1993, pages 721 - 725, XP002963470
DIFEO THOMAS J., SHUSTER JUDITH E.: "Determination of a process intermediate of celiprolol and its potential impurities by gradient high-performance liquid chromatography-application of high-low chromatography", JOURNAL OF PHARMACEUTICAL & BIOMEDICAL ANALYSIS, vol. 9, no. 10-12, 1991, pages 823 - 828, XP002963471
SMITH, L.H.: "BETA-ADRENERGIC BLOCKING AGENTS. 15. 1-SUBSTITUTED UREIDOPHENOXY-3-AMINO-2-PROPANOLS", JOURNAL OF MEDICINAL CHEMISTRY, vol. 20, no. 5, 1977, pages 705 - 708, XP002963472
MAIER, NORBERT M., URAY, GEORG: "Efficient high-performance liquid chromatographic enantioseparation of five-memberd aryl-substituted lactones and cyclic carbamates on a (R, R)-diaminodihydroethanoanthracene-derived chiral stationary phase", JOURNAL OF CHROMATOGRAPHY A, vol. 740, no. 1, 1996, pages 11 - 19, XP004020151
See also references of EP 1437344A4

Attorney, Agent or Firm:

Aoyama, Tamotsu (IMP Building 3-7, Shiromi 1-chome, Chuo-ku, Osaka-shi Osaka, JP)

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