WO2006125285B1 - Insulin sensitization to slow down pubertal tempo and to augment pubertal growth - Google Patents

Insulin sensitization to slow down pubertal tempo and to augment pubertal growth

Info

Publication number
WO2006125285B1
WO2006125285B1 PCT/BE2006/000060 BE2006000060W WO2006125285B1 WO 2006125285 B1 WO2006125285 B1 WO 2006125285B1 BE 2006000060 W BE2006000060 W BE 2006000060W WO 2006125285 B1 WO2006125285 B1 WO 2006125285B1
Authority
WO
WIPO (PCT)
Prior art keywords
pharmaceutically acceptable
pubertal
polymorphs
solvates
insulin
Prior art date
Application number
PCT/BE2006/000060
Other languages
French (fr)
Other versions
WO2006125285A1 (en
Inventor
Zegher Francis De
David Dunger
Lourdes Ibanez
Original Assignee
Leuven K U Res & Dev
Addenbrooke S Hospital
Zegher Francis De
David Dunger
Lourdes Ibanez
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 Leuven K U Res & Dev, Addenbrooke S Hospital, Zegher Francis De, David Dunger, Lourdes Ibanez filed Critical Leuven K U Res & Dev
Publication of WO2006125285A1 publication Critical patent/WO2006125285A1/en
Publication of WO2006125285B1 publication Critical patent/WO2006125285B1/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/13Amines
    • A61K31/155Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin

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  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (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)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

In accordance with the purpose of the invention, as embodied and broadly described herein, the invention is broadly drawn to a new method of treatment, the use of agents to manufacture a composition of treatment or the composition of treatment for the prevention of rapidly progressive puberty, the prevention of early menarche or the modulation, more particularly the delay, of the tempo of puberty in a female mammal, preferably a human girl, and the disorders related thereto. In a particular embodiment the present invention involves the use of at least one insulin-sensitizing agent such as metformin, any of the polymorphs of metformin or a pharmaceutically acceptable salt thereof for the preparation of a composition of treatment to modulate the tempo of pubertal progression in a girl.

Claims

AMENDED CLAIMS received by the International Bureau on 03 November 2006 (03.11.2006)
1) The use of af least one biguanide or glitazone (thiazolidinedione) insulin-sensitizing agent or aminoguanidine or a pharmaceutically acceptable sail, solvate or polymorph (hereof for the preparation of a composition of treatment to slow down the tempo of pubertal progression in a warm-blooded animal.
2) The use of claim 1, for the preparation of a composition of a treatment to slow down the- tempo of pubertal progression to prolong the pubertal growth in a warm-blooded animal.
3} The use of claim 1, to increase pubertal height gain or adult stature.
4) The use of claim 1 or 2, wherein the warm-blooded animal is a mammal.
5) The use of any of claim 1 to 3,. wherein the mammal is a human.
6) The use of any of claim 1 to 4, wherein the human is a boy. . 7} The use of any of claim 1 to 4, wherein the human is a girl.
8) The use of any of the claims 1 to 7, wherein the msulm-sensitizin g. compound is selected of the group consisting of metformin, rosiglitazone, pioglitazone, troglitazone, englitazone, (argretin, phenformin and bufomin , or pharmaceutically acceptable salts, solvates or polymorphs thereof.
9) The use of any of the claims 1 to 7, wherein the insulϊn-sensitizing compound is selected of the group consisting of metformin, rosiglitazone, pioglitazone, troglitazone, englitazone targretin , phenformin, CLX-0921, BLX-1002, tesaglitazar, oxegtitazar and buformm or pharmaceuticady accepiable salts, solvates or polymorphs.
10) The use of any of the claims 1 to 6 wherein the insulin-sensitizing compound is selected of the group consisting of 5-[[4-]2-{3-methyl-2-pyridinyl)ethoxy]phen.yl]methyI]- 2,4- Thiazolidinedione , 5-[4-[2-(5-ethyl-2-pyridinyl}-2-hydroxyethoxy]phenyl]methy]]-2,4- Thiazolidinedione, 5-[[4-[2-I5-(l-hydroxyethyl )-2-pyridmyl]ethoxy]phenyl ]methyl]]-2,4- Thiazolidinedione, 5-[[4-[2-(5-acetyl-2-pyriumyl)ethoxy]phenyl]methyl]]-2,4- li inedione 5-[[4-[2(methy]-2-pyridinylamino) ethoxy]phenyl]- methy]]-2,4- thiazolidine. dione maleate, 5-[4-(l-memy]cyclohexylmethoxy)benzyl ]-thiazolidine-2,4-dione and ([ or ~D)-5-[4-(6-methoxy-1-H-benzimidazol-2-ylmethoxy) benzyl [thiazoline-2,4-dione hydrochloride (CI-1037/CS-011) or pharmaceutically acceptable salts, solvates or polymorphs- thereof.
11) The use of any of the claims 1 to 7, wherein the insulin sensitizing compound has the general structure formula:
Figure imgf000003_0001
12) The use of any of the claims 1 to 1, wherein the insulin-sensitizing compound has the general structure formula :
Figure imgf000003_0002
13) The use of any of the claims 1 to 7, -wherein the insulin-sensitizing compound has the general structure formula
Figure imgf000003_0003
its tautomeric forms, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts, its pharmaceutically acceptable solvates, -wherein represents an optional double bond; Y represents oxygen, sulfur or NR, wherein R represents hydrogen or alkyl,; Z represents oxygen or surfer, R1, R2, R3 and R4 may be same or different and independently represent hydrogen, halogen, hydroxy, nitio, cyano, formyl, amino, alkyl, or alkoxy, A represents a bond or substituted or unsubstituted aryl, heterocyclyl or heteroaryl ring X represents an alpha amino carboxylo acid or aplha amino cariboxylic acid derivative bonded to A or Y through its aptha side chain.
14) The use of any of the claims 1 to 7, wherein the sensitizing agent is metformin or a pharmaceutically acceptable salts, solvates or polymorphs thereof.
15) The use- of any of the claims 1 to 7 wherein the sensitizing agent is rosiglitazone or a pharmaceutically acceptable salts, solvates or polymorphs thereof.
16) The use of any of ibe claims I to- 7, wherein the- sensitizing agent is pioglitazone or a pharmaceutically acceptable salts, solvates 07 polymorphs thereof
17) The- use of any of ihe claims 1 to7 wherein the senzitizing agent is C1-1037/CS-011 or a pharmaceutically acceptable salts, solvates or polymorphs thereof
18) The use of any of the claims 1 to 1, wherein the sensitizing agent is ammoguanidine or a pharmaceutically acceptable sails, solvates or polymorphs thereof
19) The use of any of the claims 1 to 7, wherein the sensitizing agent is conjugated linoliec acid or a pharmaceutically acceptable derivative thereof
20} The use of the claim 1 to 19, for the preparation of a composition further comprising a suitable pharmaceutical earner and/or excipient
21) The use of the claims I to 20, wherein the warm-blooded animal is not obese.
22) The use of the claims I to 21, wherein the warm-blooded animal is ohcse.
23) The use of insulin sensitizer which is a KPARy agonist selected from the group consisting of BRL 49653, troglitazone, pioglitazone, ciglitazone, WAY- 120,744, englitazone, AD 5075, darglitazone , G1-26257B, SB 217092, SB 236636, SB 217092, SB 219994, tesaglitazar, CLX- 0921, BLX- 1002, Metaglidasen ((-) (3-trihalomethylphenoxy) (4-halophenyl) acetic) and SB 219993 or a pharmaceutically acceptable salt, solvate or polymorph, thereof for the preparation of a composition of a treatment to slow down the tempo of pubertal progression or to prolong the pubertal growth in a warm-blooded animal.
PCT/BE2006/000060 2005-05-23 2006-05-23 Insulin sensitization to slow down pubertal tempo and to augment pubertal growth WO2006125285A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0510469.0 2005-05-23
GBGB0510469.0A GB0510469D0 (en) 2005-05-23 2005-05-23 Insulin sensitization to slow down pubertal tempo and to augment pubertal growth

Publications (2)

Publication Number Publication Date
WO2006125285A1 WO2006125285A1 (en) 2006-11-30
WO2006125285B1 true WO2006125285B1 (en) 2007-01-11

Family

ID=34834482

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/BE2006/000060 WO2006125285A1 (en) 2005-05-23 2006-05-23 Insulin sensitization to slow down pubertal tempo and to augment pubertal growth

Country Status (2)

Country Link
GB (1) GB0510469D0 (en)
WO (1) WO2006125285A1 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7040798B2 (en) 2016-12-01 2022-03-23 ミノリックス セラピューティクス エセ.エレ. 5-[[4- [2- [5- (1-hydroxyethyl) pyridin-2-yl] ethoxy] phenyl] methyl] -1,3-thiazolidine-2 for treating non-alcoholic fatty liver disease , 4-Zeon

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2462720C1 (en) * 2011-10-10 2012-09-27 Нина Викторовна Болотова Method for describing nature of arrested sexual development in boys in puberty with growth retardation
WO2019234690A1 (en) * 2018-06-06 2019-12-12 Minoryx Therapeutics S.L. Use of 5-[[4-[2-[5-acetylpyridin-2-yl]ethoxy]benzyl]-1,3-thiazolidine-2,4-dione and its salts

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7040798B2 (en) 2016-12-01 2022-03-23 ミノリックス セラピューティクス エセ.エレ. 5-[[4- [2- [5- (1-hydroxyethyl) pyridin-2-yl] ethoxy] phenyl] methyl] -1,3-thiazolidine-2 for treating non-alcoholic fatty liver disease , 4-Zeon

Also Published As

Publication number Publication date
GB0510469D0 (en) 2005-06-29
WO2006125285A1 (en) 2006-11-30

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