US20050080018A1 - Use of alkanoyl l-carnitine for the treatment of erectile dysfunction - Google Patents

Use of alkanoyl l-carnitine for the treatment of erectile dysfunction Download PDF

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Publication number
US20050080018A1
US20050080018A1 US10/497,498 US49749804A US2005080018A1 US 20050080018 A1 US20050080018 A1 US 20050080018A1 US 49749804 A US49749804 A US 49749804A US 2005080018 A1 US2005080018 A1 US 2005080018A1
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US
United States
Prior art keywords
treatment
erectile dysfunction
acid
carnitine
alkanoyl
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.)
Abandoned
Application number
US10/497,498
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English (en)
Inventor
Aleardo Koverech
Andrea Lenzi
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.)
Sigma Tau Industrie Farmaceutiche Riunite SpA
Original Assignee
Individual
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 Individual filed Critical Individual
Assigned to SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A. reassignment SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A. ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: KOVERECH, ALEARDO, LENZI, ANDREA
Publication of US20050080018A1 publication Critical patent/US20050080018A1/en
Priority to US11/649,796 priority Critical patent/US20070117762A1/en
Priority to US13/280,749 priority patent/US8343979B2/en
Abandoned legal-status Critical Current

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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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/205—Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/557—Eicosanoids, e.g. leukotrienes or prostaglandins
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Definitions

  • the present invention relates to the use of an alkanoyl L-carnitine for the treatment of the erectile dysfunction.
  • the erectile dysfunction is a syndrome characterised by a persistent inability to obtain or maintain a penis erection, for a time sufficient for a sexual intercourse.
  • the current knowledge indicates that the relaxation of the smooth musculature of the corpus cavernosum which is necessary for the erection is due to a non adrenergic, non cholinergic mechanism, mediated by nitric oxide (ON), in which prostaglandin (PG) is involved (Medicina Pratica, 2000; 12-16).
  • ON nitric oxide
  • PG prostaglandin
  • the maximum relaxation level may not be sufficient to permit an haematic flux sufficient for a normal erection.
  • VIP Vasoactive Intestinal Peptides
  • cGMP guanosin mono phosphate cyclic
  • alkanoyl L-carnitines wherein the alkanoyl group, linear or branched, has 2-6 carbon atoms, or a pharmaceutically acceptable salt thereof are useful agents for treating the erectile dysfunction.
  • pharmacologically acceptable salt of an alkanoyl L-carnitine is any salt of the latter with an acid that does not give rise to unwanted toxic or side effects.
  • Non-limiting examples of pharmacologically acceptable salts of alkanoyl L-carnitines are chloride, bromide, orotate, acid aspartate, acid citrate, magnesium citrate, acid phosphate, fumarate and acid fumarate, magnesium fumarate, lactate, maleate, acid maleate, mucate, acid oxalate, pamoate, acid pamoate, acid sulphate, glucose phosphate, tartrate, acid tartrate, magnesium tartrate, 2-amino ethansulphonate, magnesium 2-amino etansulphonate, Choline tartrate and trichloroacetate.
  • alkanoyl L-carnitines are acetyl, propionyl, butyryl, isobutyryl, valeryl and isovalery L-carnitine.
  • a further object of the present invention is the use of an alkanoyl L-carnitine for preparing a medicine for the treatment of erectile dysfunction in patients suffering from diabetes mellitus.
  • propionyl L-carnitine is preferred.
  • “useful drugs” it is intended any drug useful for treating E.D.
  • a further object of the present invention are pharmaceutical compositions comprising as active ingredient an alkanoyl L-carnitine in combination with one or more of said useful drugs, and at least an excipient and/or diluent pharmaceutically acceptable.
  • Non-limiting examples of said useful drugs are sildenafil, apomorphine, prostaglandin E1, pentolamine or papaverine.
  • a further object of the present invention is the use of an alkanoyl L-carnitine, or a pharmaceutical acceptable salt thereof, in combination with one or more of said useful drugs, for preparing a medicine for the treatment of erectile dysfunction.
  • a further object of the present invention is the use of an alkanoyl L-carnitine in combination with one or more of said useful drugs, for preparing a medicine for the treatment of erectile dysfunction in patients affected by diabetes mellitus.
  • a further object of the present invention is the use of an alkanoyl L-carnitine in combination with one or more of said useful drugs, for preparing a medicine for the treatment of erectile dysfunction, wherein said patients do not respond to the treatment with said useful drugs.
  • a further object of the present invention is the use of an alkanoyl L-carnitine in combination with one or more of said useful drugs, for preparing a medicine for the treatment of erectile dysfunction in patients suffering from diabetes mellitus, wherein said patients do not respond to the treatment with said useful drugs.
  • propionyl L-carnitine is preferred.
  • alkanoyl L-carnitines and the useful drugs above mentioned can be prepared for a simultaneous, sequential or separated administration.
  • the daily dose will depend, according to the judgement of the primary care physician, on the patient's weight, age and general condition, it is generally advisable to administer 0.5 to 4 g/die of alkanoyl L-carnitine or a stoichiometrically equivalent amount of one of its pharmacologically acceptable salts. 1-2 g/die are preferred.
  • the of administration regimen of the two active ingredients will depend on the primary care physician's judgement, the patient's weight, age and general conditions, it is generally advisable to administer the alkanoyl L-carnitine daily and said combined useful drug twice weekly.

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  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Emergency Medicine (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
US10/497,498 2001-12-04 2002-12-04 Use of alkanoyl l-carnitine for the treatment of erectile dysfunction Abandoned US20050080018A1 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
US11/649,796 US20070117762A1 (en) 2001-12-04 2007-01-05 Use of an alkanoyl L-carnitine for the treatment of the erectile dysfunction
US13/280,749 US8343979B2 (en) 2001-12-04 2011-10-25 Use of alkanoyl L-carnitine for the treatment of erectile dysfunction

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IT2001RM000708A ITRM20010708A1 (it) 2001-12-04 2001-12-04 Uso di una alcanoil l-carnitina per il trattamento della disfunzione erettile.
ITRM2001A000708 2001-12-04
PCT/IT2002/000758 WO2003047563A1 (en) 2001-12-04 2002-12-04 Use of alkanoyl l-carnitine for the treatment of erectile dysfunction

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
PCT/IT2002/000758 A-371-Of-International WO2003047563A1 (en) 2001-12-04 2002-12-04 Use of alkanoyl l-carnitine for the treatment of erectile dysfunction

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US11/649,796 Division US20070117762A1 (en) 2001-12-04 2007-01-05 Use of an alkanoyl L-carnitine for the treatment of the erectile dysfunction

Publications (1)

Publication Number Publication Date
US20050080018A1 true US20050080018A1 (en) 2005-04-14

Family

ID=11455907

Family Applications (3)

Application Number Title Priority Date Filing Date
US10/497,498 Abandoned US20050080018A1 (en) 2001-12-04 2002-12-04 Use of alkanoyl l-carnitine for the treatment of erectile dysfunction
US11/649,796 Abandoned US20070117762A1 (en) 2001-12-04 2007-01-05 Use of an alkanoyl L-carnitine for the treatment of the erectile dysfunction
US13/280,749 Expired - Fee Related US8343979B2 (en) 2001-12-04 2011-10-25 Use of alkanoyl L-carnitine for the treatment of erectile dysfunction

Family Applications After (2)

Application Number Title Priority Date Filing Date
US11/649,796 Abandoned US20070117762A1 (en) 2001-12-04 2007-01-05 Use of an alkanoyl L-carnitine for the treatment of the erectile dysfunction
US13/280,749 Expired - Fee Related US8343979B2 (en) 2001-12-04 2011-10-25 Use of alkanoyl L-carnitine for the treatment of erectile dysfunction

Country Status (16)

Country Link
US (3) US20050080018A1 (https=)
EP (1) EP1450782B9 (https=)
JP (1) JP4370169B2 (https=)
KR (1) KR100907938B1 (https=)
AT (1) ATE309800T1 (https=)
AU (1) AU2002365847A1 (https=)
CA (1) CA2465471C (https=)
DE (1) DE60207442T2 (https=)
DK (1) DK1450782T3 (https=)
ES (1) ES2250749T3 (https=)
HU (1) HU229214B1 (https=)
IT (1) ITRM20010708A1 (https=)
MX (1) MXPA04005269A (https=)
PL (1) PL211211B1 (https=)
SI (1) SI1450782T1 (https=)
WO (1) WO2003047563A1 (https=)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ITRM20040561A1 (it) * 2004-11-11 2005-02-11 Sigma Tau Ind Farmaceuti Uso della acetil l-carnitina in combinazione con propionil l-carnitina e sildenafil per il trattamento della disfunzione erettile.
AP2011005795A0 (en) 2009-02-13 2011-08-31 Boehringer Ingelheim Int SGLT-2 inhibitor for treating type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance or hyperglycemia.
IT1397867B1 (it) * 2010-02-03 2013-02-04 Brotzu Liposomi contenenti prostaglandina e1 (pge1), formulazioni che li contengono e loro uso
HRP20190101T1 (hr) 2013-04-05 2019-03-08 Boehringer Ingelheim International Gmbh Terapeutske uporabe empagliflozina
US20140303097A1 (en) 2013-04-05 2014-10-09 Boehringer Ingelheim International Gmbh Pharmaceutical composition, methods for treating and uses thereof
CA2812519A1 (en) 2013-04-05 2014-10-05 Boehringer Ingelheim International Gmbh Pharmaceutical composition, methods for treating and uses thereof
US11813275B2 (en) 2013-04-05 2023-11-14 Boehringer Ingelheim International Gmbh Pharmaceutical composition, methods for treating and uses thereof
FI4000608T3 (fi) 2013-04-18 2026-01-21 Boehringer Ingelheim Int Farmaseuttinen koostumus, menetelmä hoitamiseksi ja sen käyttöjä
JP6561136B2 (ja) * 2015-04-30 2019-08-14 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 勃起機能不全を治療又は改善するための方法及びｓｇｌｔ２阻害薬を含む医薬組成物
KR20250097990A (ko) 2016-11-10 2025-06-30 베링거 인겔하임 인터내셔날 게엠베하 약제학적 조성물, 치료 방법 및 이의 용도

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040087515A1 (en) * 1999-04-12 2004-05-06 Butler Terri L. Compositions methods for improving cardio vascular function

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2903579A1 (de) * 1978-02-03 1979-08-09 Sigma Tau Ind Farmaceuti Verwendung von acetylcarnitin und anderen acylderivaten des carnitins zur behandlung der hyperlipoproteinaemie und hyperlimpidaemie sowie arzneimittel
DK0793962T3 (da) * 1996-03-04 2000-05-22 Sigma Tau Ind Farmaceuti Lægemiddel indeholdende et carnitinderivat til behandling af arteriosclerosis obliterans
IT1290801B1 (it) * 1996-07-05 1998-12-11 Mendes Srl Uso della acetil l-carnitina, della isovaleril l-carnitina, della propionil l-carnitina o dei loro sali farmacologicamente accettabili
US6133281A (en) * 1996-10-24 2000-10-17 Harbor-Ucla Research And Education Institute NMDA receptor blockers in the therapy of urogenital disease
IT1293539B1 (it) * 1997-07-16 1999-03-01 Sigma Tau Ind Farmaceuti Composizione nutritiva per soggetti in stato di debilitazione causato da stress
US6241471B1 (en) * 1999-08-26 2001-06-05 General Electric Co. Turbine bucket tip shroud reinforcement
IT1306722B1 (it) * 1999-10-08 2001-10-02 Sigma Tau Healthscience Spa Composizione per la prevenzione e/o il trattamento di disfunzionicircolatorie, comprendente derivati della l-carnitina ed estratti di

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040087515A1 (en) * 1999-04-12 2004-05-06 Butler Terri L. Compositions methods for improving cardio vascular function

Also Published As

Publication number Publication date
EP1450782A1 (en) 2004-09-01
DK1450782T3 (da) 2006-02-20
ITRM20010708A0 (it) 2001-12-04
CA2465471A1 (en) 2003-06-12
HU229214B1 (hu) 2013-09-30
CA2465471C (en) 2010-10-19
HUP0402062A3 (en) 2012-09-28
ES2250749T3 (es) 2006-04-16
EP1450782B9 (en) 2006-05-17
AU2002365847A1 (en) 2003-06-17
KR20050044594A (ko) 2005-05-12
MXPA04005269A (es) 2004-10-11
PL371131A1 (en) 2005-06-13
US20070117762A1 (en) 2007-05-24
SI1450782T1 (sl) 2006-02-28
JP2005511655A (ja) 2005-04-28
JP4370169B2 (ja) 2009-11-25
ATE309800T1 (de) 2005-12-15
PL211211B1 (pl) 2012-04-30
EP1450782B1 (en) 2005-11-16
WO2003047563A1 (en) 2003-06-12
DE60207442T2 (de) 2006-07-27
ITRM20010708A1 (it) 2003-06-04
DE60207442D1 (de) 2005-12-22
US8343979B2 (en) 2013-01-01
HUP0402062A2 (hu) 2005-02-28
KR100907938B1 (ko) 2009-07-16
US20120041005A1 (en) 2012-02-16

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Legal Events

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AS Assignment

Owner name: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A.,

Free format text: ASSIGNMENT OF ASSIGNORS INTEREST;ASSIGNORS:KOVERECH, ALEARDO;LENZI, ANDREA;REEL/FRAME:015951/0724

Effective date: 20040430

STCB Information on status: application discontinuation

Free format text: ABANDONED -- FAILURE TO RESPOND TO AN OFFICE ACTION