WO2001022919A3 - Spiro[bicyclic -azacycloalkyl and -cycloalkyl] derivatives and uses thereof - Google Patents

Spiro[bicyclic -azacycloalkyl and -cycloalkyl] derivatives and uses thereof Download PDF

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Publication number
WO2001022919A3
WO2001022919A3 PCT/US2000/026387 US0026387W WO0122919A3 WO 2001022919 A3 WO2001022919 A3 WO 2001022919A3 US 0026387 W US0026387 W US 0026387W WO 0122919 A3 WO0122919 A3 WO 0122919A3
Authority
WO
WIPO (PCT)
Prior art keywords
compounds
benign prostatic
prostatic hyperplasia
alpha
azacycloalkyl
Prior art date
Application number
PCT/US2000/026387
Other languages
French (fr)
Other versions
WO2001022919A2 (en
Inventor
Jacob M Hoffman
Original Assignee
Merck & Co Inc
Jacob M Hoffman
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 Merck & Co Inc, Jacob M Hoffman filed Critical Merck & Co Inc
Priority to AU77166/00A priority Critical patent/AU7716600A/en
Publication of WO2001022919A2 publication Critical patent/WO2001022919A2/en
Publication of WO2001022919A3 publication Critical patent/WO2001022919A3/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D419/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms
    • C07D419/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D419/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Urology & Nephrology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Spiro[bicyclic -azacycloalkyl and -cycloalkyl] derivatives and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are typically selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
PCT/US2000/026387 1999-09-30 2000-09-26 Spiro[bicyclic -azacycloalkyl and -cycloalkyl] derivatives and uses thereof WO2001022919A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU77166/00A AU7716600A (en) 1999-09-30 2000-09-26 Spiro[bicyclic -azacycloalkyl and -cycloalkyl] derivatives and uses thereof

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US15720799P 1999-09-30 1999-09-30
US60/157,207 1999-09-30

Publications (2)

Publication Number Publication Date
WO2001022919A2 WO2001022919A2 (en) 2001-04-05
WO2001022919A3 true WO2001022919A3 (en) 2002-07-11

Family

ID=22562765

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2000/026387 WO2001022919A2 (en) 1999-09-30 2000-09-26 Spiro[bicyclic -azacycloalkyl and -cycloalkyl] derivatives and uses thereof

Country Status (2)

Country Link
AU (1) AU7716600A (en)
WO (1) WO2001022919A2 (en)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002085354A1 (en) 2001-04-18 2002-10-31 Euro-Celtique S.A. Spiroindene and spiroindane compounds
AU2004222336B2 (en) * 2003-03-18 2010-06-03 Merck Sharp & Dohme Corp. Amino cyclobutylamide modulators of chemokine receptor activity
US7166603B2 (en) 2003-07-23 2007-01-23 Bristol-Myers Squibb Co. Dihydropyrimidone inhibitors of calcium channel function
MX2007002033A (en) 2004-08-19 2007-04-26 Vertex Pharma Modulators of muscarinic receptors.
US7786141B2 (en) 2004-08-19 2010-08-31 Vertex Pharmaceuticals Incorporated Dihydrospiroindene modulators of muscarinic receptors
RU2007124373A (en) 2004-11-29 2009-01-10 Вертекс Фармасьютикалз Инкорпорейтед (Us) MUSCARINE RECEPTION MODULATORS
JP2009521483A (en) 2005-12-22 2009-06-04 バーテックス ファーマシューティカルズ インコーポレイテッド Muscarinic receptor modulators
US7351706B2 (en) 2006-01-05 2008-04-01 Hoffmann-La Roche Inc. Indol-3-yl-carbonyl-spiro-piperidine derivatives
RU2008137593A (en) 2006-02-22 2010-03-27 Вертекс Фармасьютикалз Инкорпорейтед (Us) MUSCARINE RECEPTOR MODULATORS
AU2007221220A1 (en) 2006-02-22 2007-09-07 Vertex Pharmaceuticals Incorporated Spiro condensed piperidnes as modulators of muscarinic receptors
EP2040706A2 (en) 2006-06-29 2009-04-01 Vertex Pharmceuticals Incorporated Modulators of muscarinic receptors
EP2051712A2 (en) 2006-08-15 2009-04-29 Vertex Pharmceuticals Incorporated Modulators of muscarinic receptors
JP2010501561A (en) 2006-08-18 2010-01-21 バーテックス ファーマシューティカルズ インコーポレイテッド Modulator of muscarinic receptor
EP2207549A1 (en) 2007-10-03 2010-07-21 Vertex Pharmceuticals Incorporated Modulators of muscarinic receptors

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995028397A1 (en) * 1994-04-14 1995-10-26 Merck & Co., Inc. Alpha1c adrenergic receptor antagonists

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995028397A1 (en) * 1994-04-14 1995-10-26 Merck & Co., Inc. Alpha1c adrenergic receptor antagonists

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
DHAR T.G. ET AL.: "Design and synthesis of novel alpha 1a andrenoceptor-selective antagonists. 2. Approaches to eliminate opiod agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety", J. MED. CHEM., vol. 42, no. 23, October 1999 (1999-10-01), pages 4778 - 4793, XP002949069 *

Also Published As

Publication number Publication date
WO2001022919A2 (en) 2001-04-05
AU7716600A (en) 2001-04-30

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