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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
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/US2002/041859
Other languages
French (fr)
Other versions
WO2003057161A2 (en
Inventor
Gaetan H. Ladouceur
Soongyou Choi
Yamin Wang
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bayer Pharmaceuticals Corp
Original Assignee
Bayer Pharmaceuticals Corp
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 Corp filed Critical Bayer Pharmaceuticals Corp
Priority to AU2002367323A priority Critical patent/AU2002367323A1/en
Publication of WO2003057161A2 publication Critical patent/WO2003057161A2/en
Anticipated expiration legal-status Critical
Publication of WO2003057161A3 publication Critical patent/WO2003057161A3/en
Ceased legal-status Critical Current

Links

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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

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 Ceased 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 Ceased 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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
EP1734963A4 (en) 2004-04-02 2008-06-18 Merck & Co Inc METHOD FOR TREATING MEN WITH METABOLIC AND ANTHROPOMETRIC DISORDERS
US8685924B2 (en) 2004-08-25 2014-04-01 Takeda Pharmaceutical Company Limited Preventives/remedies for stress urinary incontinence and method of screening the same
AU2012201515B2 (en) * 2004-12-23 2015-01-29 Arena Pharmaceuticals, Inc. 5HT2C receptor modulator compositions and methods of use
AU2005322183B2 (en) * 2004-12-23 2012-03-29 Arena Pharmaceuticals, Inc. 5HT2C receptor modulator compositions and methods of use
EP2018863B9 (en) 2006-05-16 2015-02-18 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
JP5520051B2 (en) 2007-11-15 2014-06-11 武田薬品工業株式会社 Condensed pyridine derivatives and uses thereof
EP2288585A1 (en) 2008-03-04 2011-03-02 Arena Pharmaceuticals, Inc. Processes for the preparation of intermediates related to the 5-ht2c agonist (r)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1h-3-benzazepine
CN102648170A (en) 2009-06-18 2012-08-22 艾尼纳制药公司 Processes for the preparation of 5-HT2C receptor agonists
WO2011071136A1 (en) 2009-12-11 2011-06-16 アステラス製薬株式会社 Therapeutic agent for fibromyalgia
US9045431B2 (en) 2010-06-02 2015-06-02 Arena Pharmaceuticals, Inc. Processes for the preparation of 5-HT2C receptor agonists
EP2611782A1 (en) 2010-09-01 2013-07-10 Arena Pharmaceuticals, Inc. Salts of lorcaserin with optically active acids
CN103347523A (en) 2010-09-01 2013-10-09 艾尼纳制药公司 Administration of lorcaserin to individual with renal impairment
KR20130101524A (en) 2010-09-01 2013-09-13 아레나 파마슈티칼스, 인크. Non-hygroscopic Salts of 5-HT2C Agonists
CN103189053A (en) 2010-09-01 2013-07-03 艾尼纳制药公司 Modified release dosage form of a 5-HT2C agonist for weight management
CA2886875A1 (en) 2012-10-09 2014-04-17 Arena Pharmaceuticals, Inc. Method of weight management
GB201304811D0 (en) * 2013-03-15 2013-05-01 Proximagen Ltd Novel treatment for hypertension
WO2019131902A1 (en) 2017-12-27 2019-07-04 武田薬品工業株式会社 Therapeutic agent for stress urinary incontinence and fecal incontinence

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

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

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