WO2003057161A3 - BENZOTHIENO [3,2-c]PYRAZOLYL AND BENZOFURANO [3,2-c] PYRAZOLYL COMPOUNDS, THEIR USE IN DISEASES ASSOCIATED WITH THE 5-HT2C RECEPTOR AND INTERMEDIATE COMPOUNDS THEREOF - Google Patents

BENZOTHIENO [3,2-c]PYRAZOLYL AND BENZOFURANO [3,2-c] PYRAZOLYL COMPOUNDS, THEIR USE IN DISEASES ASSOCIATED WITH THE 5-HT2C RECEPTOR AND INTERMEDIATE COMPOUNDS THEREOF Download PDF

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Publication number
WO2003057161A3
WO2003057161A3 PCT/US2002/041859 US0241859W WO03057161A3 WO 2003057161 A3 WO2003057161 A3 WO 2003057161A3 US 0241859 W US0241859 W US 0241859W WO 03057161 A3 WO03057161 A3 WO 03057161A3
Authority
WO
WIPO (PCT)
Prior art keywords
pyrazolyl
compounds
benzofurano
benzothieno
diseases associated
Prior art date
Application number
PCT/US2002/041859
Other languages
French (fr)
Other versions
WO2003057161A2 (en
Inventor
Gaetan H. Ladouceur
Soongyou Choi
Yamin Wang
Original Assignee
Bayer Pharmaceuticals Corporation
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Bayer Pharmaceuticals Corporation filed Critical Bayer Pharmaceuticals Corporation
Priority to AU2002367323A priority Critical patent/AU2002367323A1/en
Publication of WO2003057161A2 publication Critical patent/WO2003057161A2/en
Publication of WO2003057161A3 publication Critical patent/WO2003057161A3/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

Abstract

Disclosed are benzothieno[3,2-c]pyrazolyl and benzofurano[3,2-c]pyrazolyl compounds of the formula (I) and (II), and intermediates of the formula (Ia) and (IIa) which are tautomers, wherein the variables A, X, y, R1, R2, R3 and R4 are as defined in the specification. The compounds are useful for the treatment or prevention of diseases and/or behaviors involving the 5-HT2C receptor site.
PCT/US2002/041859 2001-12-28 2002-12-28 BENZOTHIENO [3,2-c]PYRAZOLYL AND BENZOFURANO [3,2-c] PYRAZOLYL COMPOUNDS, THEIR USE IN DISEASES ASSOCIATED WITH THE 5-HT2C RECEPTOR AND INTERMEDIATE COMPOUNDS THEREOF WO2003057161A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2002367323A AU2002367323A1 (en) 2001-12-28 2002-12-28 Benzothieno (3,2-

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US34415101P 2001-12-28 2001-12-28
US60/344,151 2001-12-28

Publications (2)

Publication Number Publication Date
WO2003057161A2 WO2003057161A2 (en) 2003-07-17
WO2003057161A3 true WO2003057161A3 (en) 2011-08-04

Family

ID=23349272

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2002/041859 WO2003057161A2 (en) 2001-12-28 2002-12-28 BENZOTHIENO [3,2-c]PYRAZOLYL AND BENZOFURANO [3,2-c] PYRAZOLYL COMPOUNDS, THEIR USE IN DISEASES ASSOCIATED WITH THE 5-HT2C RECEPTOR AND INTERMEDIATE COMPOUNDS THEREOF

Country Status (2)

Country Link
AU (1) AU2002367323A1 (en)
WO (1) WO2003057161A2 (en)

Families Citing this family (19)

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CL2004000826A1 (en) 2003-04-25 2005-03-04 Pfizer USE OF AN AGONIST FOR THE 5-HT2C RECEPTOR TO PREPARE A USEFUL MEDICINAL PRODUCT IN THE TREATMENT OF URINARY INCONTINENCE CAUSED BY STRESS, WITH THE CONDITION THAT THE AGONIST IS NOT 1- [6-CHLORINE-5- (TRIFLUOROMETIL) -2- PIRIDINIL] PIPERAZINA (ORG-129
EP2305352A1 (en) 2004-04-02 2011-04-06 Merck Sharp & Dohme Corp. 5-alpha-reductase inhibitors for use in the treatment of men with metabolic and anthropometric disorders
EP2400300A1 (en) 2004-08-25 2011-12-28 Takeda Pharmaceutical Company Limited Method of screening preventives/remedies for stress urinary incontinence
CN102631349A (en) 2004-12-23 2012-08-15 艾尼纳制药公司 5ht2c receptor modulator compositions and methods of use
AU2012201515B2 (en) * 2004-12-23 2015-01-29 Arena Pharmaceuticals, Inc. 5HT2C receptor modulator compositions and methods of use
WO2007132841A1 (en) 2006-05-16 2007-11-22 Takeda Pharmaceutical Company Limited Fused heterocyclic compound and use thereof
ES2745411T3 (en) * 2006-07-27 2020-03-02 Wang Nai Fang Arylsulfanil compounds and compositions for administration of active agents
EP2216023A4 (en) 2007-11-15 2013-03-13 Takeda Pharmaceutical Condensed pyridine derivative and use thereof
JP5491421B2 (en) 2008-03-04 2014-05-14 アリーナ ファーマシューティカルズ， インコーポレイテッド Process for the preparation of intermediates related to the 5-HT2C agonist (R) -8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine
WO2010148207A2 (en) 2009-06-18 2010-12-23 Arena Pharmaceuticals, Inc. Processes for the preparation of 5-ht2c receptor agonists
US20120253036A1 (en) 2009-12-11 2012-10-04 Yukinori Nagakura Agent for treating fibromyalgia
WO2011153206A1 (en) 2010-06-02 2011-12-08 Arena Pharmaceuticals, Inc. Processes for the preparation of 5-ht2c receptor agonists
SG10201506870PA (en) 2010-09-01 2015-10-29 Arena Pharm Inc Salts of lorcaserin with optically active acids
SG188362A1 (en) 2010-09-01 2013-04-30 Arena Pharm Inc Modified-release dosage forms of 5-ht2c agonists useful for weight management
US8999970B2 (en) 2010-09-01 2015-04-07 Arena Pharmaceuticals, Inc. Administration of an anti-obesity compound to individuals with renal impairment
EP2611433A2 (en) 2010-09-01 2013-07-10 Arena Pharmaceuticals, Inc. Non-hygroscopic salts of 5-ht2c agonists
KR20150070249A (en) 2012-10-09 2015-06-24 아레나 파마슈티칼스, 인크. Method of weight management
GB201304811D0 (en) * 2013-03-15 2013-05-01 Proximagen Ltd Novel treatment for hypertension
EP3733204A4 (en) 2017-12-27 2021-09-15 Takeda Pharmaceutical Company Limited Therapeutic agent for stress urinary incontinence and fecal incontinence

Citations (1)

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Publication number Priority date Publication date Assignee Title
EP0700905A1 (en) * 1994-08-12 1996-03-13 F. Hoffmann-La Roche Ag Tricyclic pyrazole derivatives

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0700905A1 (en) * 1994-08-12 1996-03-13 F. Hoffmann-La Roche Ag Tricyclic pyrazole derivatives

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
BERTACCINI G ET AL: "THE RELATIVE POTENCY OF 5-HYDROXYTRYPTAMINE LIKE SUBSTANCES", ARCHIVES INTERNATIONALES DE PHARMACODYNAMIE ET DE THERAPIE, HEYMANS INSTITUTE OF PHARMACOLOGY, GHENT, BE, vol. 133, no. 1/02, 24 January 1961 (1961-01-24), pages 138 - 156, XP000881463, ISSN: 0003-9780 *
CHIPPENDALE, K. E. ET AL: "Condensed thiophene ring systems. XI. Synthesis of 2-aryl[1]benzothieno[3,2-c]pyrazoles and 2-aryl[1]benzothieno[2,3-c]pyrazoles", JOURNAL OF THE CHEMICAL SOCIETY, PERKIN TRANSACTIONS 1: ORGANIC AND BIO-ORGANIC CHEMISTRY (1972-1999) , (2), 129-33 CODEN: JCPRB4; ISSN: 0300-922X, 1973, XP002639047 *

Also Published As

Publication number Publication date
AU2002367323A1 (en) 2003-07-24
AU2002367323A8 (en) 2011-08-25
WO2003057161A2 (en) 2003-07-17

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