CA2241725A1 - Growth-hormone secretagogues - Google Patents

Growth-hormone secretagogues

Info

Publication number
CA2241725A1
CA2241725A1 CA002241725A CA2241725A CA2241725A1 CA 2241725 A1 CA2241725 A1 CA 2241725A1 CA 002241725 A CA002241725 A CA 002241725A CA 2241725 A CA2241725 A CA 2241725A CA 2241725 A1 CA2241725 A1 CA 2241725A1
Authority
CA
Canada
Prior art keywords
growth hormone
compounds
useful
directed
accelerating
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.)
Granted
Application number
CA002241725A
Other languages
French (fr)
Other versions
CA2241725C (en
Inventor
Philip A. Carpino
Paul A. Dasilva Jardine
Bruce A. Lefker
John A. Ragan
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.)
Raqualia Pharma Inc
Original Assignee
Pfizer Inc.
Philip A. Carpino
Paul A. Dasilva Jardine
Bruce A. Lefker
John A. Ragan
Raqualia Pharma Inc.
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=21737850&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CA2241725(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pfizer Inc., Philip A. Carpino, Paul A. Dasilva Jardine, Bruce A. Lefker, John A. Ragan, Raqualia Pharma Inc. filed Critical Pfizer Inc.
Publication of CA2241725A1 publication Critical patent/CA2241725A1/en
Application granted granted Critical
Publication of CA2241725C publication Critical patent/CA2241725C/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Abstract

This invention is directed to compounds of formula (I) and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretagogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis. The compounds of the present invention are also useful in treating osteoporosis when used in combination with: a bisphosphonate compound such as alendronate;
estrogen, premarin, and optionally progesterone; an estrogen agonist or antagonist; or calcitonin, and pharmaceutical compositions useful therefor.
Further, the present invention is directed to pharmaceutical compositions useful for increasing the endogenous production or release of growth hormone in a human or other animal which comprises an effective amount of a compound of the present invention and a growth hormone secretagogue selected from GHRP-6, Hexarelin, GHRP-1, growth hormone releasing factor (GRF), IGF-1, IGF-2 or B-HT920. The invention is also directed to intermediates useful in the preparation of compounds of formula (I).
CA002241725A 1995-12-28 1996-12-04 Growth-hormone secretagogues Expired - Lifetime CA2241725C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US946995P 1995-12-28 1995-12-28
US60/009,469 1995-12-28
PCT/IB1996/001353 WO1997024369A1 (en) 1995-12-28 1996-12-04 Growth-hormone secretagogues

Publications (2)

Publication Number Publication Date
CA2241725A1 true CA2241725A1 (en) 1997-07-10
CA2241725C CA2241725C (en) 2002-06-18

Family

ID=21737850

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002241725A Expired - Lifetime CA2241725C (en) 1995-12-28 1996-12-04 Growth-hormone secretagogues

Country Status (43)

Country Link
US (7) US6124264A (en)
EP (1) EP0869968B1 (en)
JP (2) JP3511382B2 (en)
KR (1) KR100320167B1 (en)
CN (1) CN1113895C (en)
AP (2) AP756A (en)
AR (2) AR004367A1 (en)
AT (1) ATE361314T1 (en)
AU (1) AU716934B2 (en)
BG (1) BG64055B1 (en)
BR (1) BR9612465B1 (en)
CA (1) CA2241725C (en)
CO (1) CO4480108A1 (en)
CZ (1) CZ293423B6 (en)
DE (1) DE69637063T2 (en)
DK (1) DK0869968T3 (en)
EG (1) EG24195A (en)
ES (1) ES2285715T3 (en)
GT (1) GT199600100A (en)
HN (1) HN1996000085A (en)
HR (1) HRP960618B1 (en)
HU (1) HUP9901246A3 (en)
IL (4) IL138909A0 (en)
IS (1) IS4758A (en)
MA (1) MA26415A1 (en)
MX (1) MX9805157A (en)
MY (1) MY135727A (en)
NO (1) NO325135B1 (en)
NZ (1) NZ322172A (en)
OA (1) OA10702A (en)
PE (1) PE30398A1 (en)
PL (1) PL186916B1 (en)
PT (1) PT869968E (en)
RS (1) RS49926B (en)
SA (1) SA97170581B1 (en)
SI (1) SI0869968T1 (en)
SK (1) SK285678B6 (en)
TN (1) TNSN96172A1 (en)
TR (1) TR199801233T2 (en)
TW (1) TW432073B (en)
UA (1) UA66754C2 (en)
WO (1) WO1997024369A1 (en)
ZA (1) ZA9610858B (en)

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