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WO1998016224A1 - Pyrazolinones pour traiter des troubles de l'erection - Google Patents

Pyrazolinones pour traiter des troubles de l'erection Download PDF

Info

Publication number
WO1998016224A1
WO1998016224A1 PCT/EP1997/005532 EP9705532W WO9816224A1 WO 1998016224 A1 WO1998016224 A1 WO 1998016224A1 EP 9705532 W EP9705532 W EP 9705532W WO 9816224 A1 WO9816224 A1 WO 9816224A1
Authority
WO
WIPO (PCT)
Prior art keywords
dihydro
methylene
pyrazol
oxo
ethylanilino
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/EP1997/005532
Other languages
German (de)
English (en)
Inventor
Michael Arlt
Rochus Jonas
Pierre Schelling
Maria Christadler
Franz-Werner Kluxen
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.)
Merck Patent GmbH
Original Assignee
Merck Patent GmbH
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 Patent GmbH filed Critical Merck Patent GmbH
Priority to CA002268823A priority Critical patent/CA2268823A1/fr
Priority to JP10517987A priority patent/JP2001501958A/ja
Priority to HU0000233A priority patent/HUP0000233A3/hu
Priority to PL97332821A priority patent/PL332821A1/xx
Priority to BR9712307-2A priority patent/BR9712307A/pt
Priority to AU49452/97A priority patent/AU4945297A/en
Priority to EP97912141A priority patent/EP0930881A1/fr
Publication of WO1998016224A1 publication Critical patent/WO1998016224A1/fr
Priority to NO991734A priority patent/NO991734D0/no
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4152—1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence

Definitions

  • R 4 and R 5 together also represent a saturated, wholly or partly unsaturated, Q-saturated 4- to 5-membered alkylene chain in which 1 to 3 C-
  • R 2 A alkoxy-CO-alkylene or HO-alkylene
  • the invention furthermore relates to the use of the compounds of the formula I and / or their physiologically acceptable salts for the production of pharmaceutical preparations, in particular by a non-chemical route. They can be brought into a suitable dosage form together with at least one solid, liquid and / or semi-liquid carrier or auxiliary and, if appropriate, in combination with one or more further active ingredients.
  • the invention further relates to the use of the compounds of the formula I and / or their physiologically acceptable salts for the production of a medicament for the treatment and / or therapy of potent disorders.
  • Tablets, pills, dragees, capsules, powders, granules, syrups, juices or drops are used for oral use, suppositories for rectal application, solutions, preferably oily or aqueous solutions, and also suspensions, emulsions or implants for parenteral use topical application ointments, creams or powder.
  • the new compounds can also be lyophilized and the lyophilizates obtained used, for example, for the production of injectables.
  • Example A Injection glasses
  • Example D ointment
  • 500 mg of an active ingredient of the formula I are mixed with 99.5 g of petroleum jelly under aseptic conditions.
  • each capsule contains 20 mg of the active ingredient.

Landscapes

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

Abstract

L'invention concerne l'utilisation des composés de la formule (I) dans laquelle R<1>, R<2> et R<3> ont la signification mentionnée dans la revendication 1, pour traiter et/ou soigner des troubles de l'érection.
PCT/EP1997/005532 1996-10-14 1997-10-08 Pyrazolinones pour traiter des troubles de l'erection Ceased WO1998016224A1 (fr)

Priority Applications (8)

Application Number Priority Date Filing Date Title
CA002268823A CA2268823A1 (fr) 1996-10-14 1997-10-08 Pyrazolinones pour traiter des troubles de l'erection
JP10517987A JP2001501958A (ja) 1996-10-14 1997-10-08 性的能力障害治療用ピラゾリノン化合物
HU0000233A HUP0000233A3 (en) 1996-10-14 1997-10-08 Use of pyrazolinone derivatives for producing pharmaceutical compositions useful for treating disturbances of potency
PL97332821A PL332821A1 (en) 1996-10-14 1997-10-08 Pyrazolydinones for treating potency disorders
BR9712307-2A BR9712307A (pt) 1996-10-14 1997-10-08 Pirazolinonas para o tratamento de potência enfraquecida
AU49452/97A AU4945297A (en) 1996-10-14 1997-10-08 Pyrazolinones to treat disturbances of potency
EP97912141A EP0930881A1 (fr) 1996-10-14 1997-10-08 Pyrazolinones pour traiter des troubles de l'erection
NO991734A NO991734D0 (no) 1996-10-14 1999-04-13 Pyrazolinoner for behandling av potensforstyrrelser

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19642284A DE19642284A1 (de) 1996-10-14 1996-10-14 Pyrazolinone zur Behandlung von Potenzstörungen
DE19642284.1 1996-10-14

Publications (1)

Publication Number Publication Date
WO1998016224A1 true WO1998016224A1 (fr) 1998-04-23

Family

ID=7808669

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1997/005532 Ceased WO1998016224A1 (fr) 1996-10-14 1997-10-08 Pyrazolinones pour traiter des troubles de l'erection

Country Status (14)

Country Link
EP (1) EP0930881A1 (fr)
JP (1) JP2001501958A (fr)
KR (1) KR20000049086A (fr)
CN (1) CN1233178A (fr)
AR (1) AR008494A1 (fr)
AU (1) AU4945297A (fr)
BR (1) BR9712307A (fr)
CA (1) CA2268823A1 (fr)
DE (1) DE19642284A1 (fr)
HU (1) HUP0000233A3 (fr)
NO (1) NO991734D0 (fr)
PL (1) PL332821A1 (fr)
WO (1) WO1998016224A1 (fr)
ZA (1) ZA979151B (fr)

Cited By (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6020379A (en) * 1999-02-19 2000-02-01 Cell Pathways, Inc. Position 7 substituted indenyl-3-acetic acid derivatives and amides thereof for the treatment of neoplasia
US6034099A (en) * 1998-11-24 2000-03-07 Cell Pathways, Inc. Method for inhibiting neoplastic lesions by administering 4-(arylmethylene)- 2, 3- dihydro-pyrazol-3-ones
US6077842A (en) * 1998-11-24 2000-06-20 Cell Pathways, Inc. Method of inhibiting neoplastic cells with pyrazolopyridylpyridazinone derivatives
US6133271A (en) * 1998-11-19 2000-10-17 Cell Pathways, Inc. Method for inhibiting neoplastic cells and related conditions by exposure thienopyrimidine derivatives
US6187779B1 (en) 1998-11-20 2001-02-13 Cell Pathways, Inc. Method for inhibiting neoplastic cells and related conditions by exposure to 2,8-disubstituted quinazoline derivatives
US6200771B1 (en) 1998-10-15 2001-03-13 Cell Pathways, Inc. Method of using a novel phosphodiesterase in pharmaceutical screeing to identify compounds for treatment of neoplasia
US6369092B1 (en) 1998-11-23 2002-04-09 Cell Pathways, Inc. Method for treating neoplasia by exposure to substituted benzimidazole derivatives
US6486155B1 (en) 1998-11-24 2002-11-26 Cell Pathways Inc Method of inhibiting neoplastic cells with isoquinoline derivatives
US6875575B1 (en) 1998-11-25 2005-04-05 Osi Pharmaceuticals, Inc. Diagnostic methods for neoplasia
US7115647B2 (en) 1998-01-14 2006-10-03 Osi Pharmaceuticals, Inc. Method of inhibiting neoplastic cells with indole derivatives
US7622486B2 (en) 2004-09-23 2009-11-24 Reddy Us Therapeutics, Inc. Pyridine compounds, process for their preparation and compositions containing them

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1994028902A1 (fr) * 1993-06-09 1994-12-22 Pfizer Limited Pyrazolopyrimidinones utilisees pour traiter l'impuissance
EP0743304A1 (fr) * 1995-05-17 1996-11-20 MERCK PATENT GmbH 4-(Arylaminométhylène)-2,4-dihydro-pyrazole-3-ones

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1994028902A1 (fr) * 1993-06-09 1994-12-22 Pfizer Limited Pyrazolopyrimidinones utilisees pour traiter l'impuissance
EP0743304A1 (fr) * 1995-05-17 1996-11-20 MERCK PATENT GmbH 4-(Arylaminométhylène)-2,4-dihydro-pyrazole-3-ones

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
N.K. TERRETT ET AL.: "Sildefanil, a potent and selective inhibitor of type 5 cGMP phosphodiesterase with utility for the treatment of male erectile dysfunction.", BIOORG. & MED. CHEM. LETT., vol. 6, no. 15, 1996, pages 1819 - 1824, XP002057392 *

Cited By (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7115647B2 (en) 1998-01-14 2006-10-03 Osi Pharmaceuticals, Inc. Method of inhibiting neoplastic cells with indole derivatives
US6200771B1 (en) 1998-10-15 2001-03-13 Cell Pathways, Inc. Method of using a novel phosphodiesterase in pharmaceutical screeing to identify compounds for treatment of neoplasia
US6133271A (en) * 1998-11-19 2000-10-17 Cell Pathways, Inc. Method for inhibiting neoplastic cells and related conditions by exposure thienopyrimidine derivatives
US6187779B1 (en) 1998-11-20 2001-02-13 Cell Pathways, Inc. Method for inhibiting neoplastic cells and related conditions by exposure to 2,8-disubstituted quinazoline derivatives
US6369092B1 (en) 1998-11-23 2002-04-09 Cell Pathways, Inc. Method for treating neoplasia by exposure to substituted benzimidazole derivatives
US6034099A (en) * 1998-11-24 2000-03-07 Cell Pathways, Inc. Method for inhibiting neoplastic lesions by administering 4-(arylmethylene)- 2, 3- dihydro-pyrazol-3-ones
US6077842A (en) * 1998-11-24 2000-06-20 Cell Pathways, Inc. Method of inhibiting neoplastic cells with pyrazolopyridylpyridazinone derivatives
US6486155B1 (en) 1998-11-24 2002-11-26 Cell Pathways Inc Method of inhibiting neoplastic cells with isoquinoline derivatives
US6875575B1 (en) 1998-11-25 2005-04-05 Osi Pharmaceuticals, Inc. Diagnostic methods for neoplasia
US6020379A (en) * 1999-02-19 2000-02-01 Cell Pathways, Inc. Position 7 substituted indenyl-3-acetic acid derivatives and amides thereof for the treatment of neoplasia
US7622486B2 (en) 2004-09-23 2009-11-24 Reddy Us Therapeutics, Inc. Pyridine compounds, process for their preparation and compositions containing them

Also Published As

Publication number Publication date
AU4945297A (en) 1998-05-11
BR9712307A (pt) 1999-08-31
NO991734L (no) 1999-04-13
AR008494A1 (es) 2000-01-19
CN1233178A (zh) 1999-10-27
CA2268823A1 (fr) 1998-04-23
PL332821A1 (en) 1999-10-11
NO991734D0 (no) 1999-04-13
EP0930881A1 (fr) 1999-07-28
HUP0000233A2 (hu) 2001-04-28
HUP0000233A3 (en) 2001-06-28
JP2001501958A (ja) 2001-02-13
DE19642284A1 (de) 1998-04-16
KR20000049086A (ko) 2000-07-25
ZA979151B (en) 1998-05-11

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