CA2350609A1 - N-substituted 2-cyanopyrrolidines - Google Patents

N-substituted 2-cyanopyrrolidines Download PDF

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Publication number
CA2350609A1
CA2350609A1 CA002350609A CA2350609A CA2350609A1 CA 2350609 A1 CA2350609 A1 CA 2350609A1 CA 002350609 A CA002350609 A CA 002350609A CA 2350609 A CA2350609 A CA 2350609A CA 2350609 A1 CA2350609 A1 CA 2350609A1
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CA
Canada
Prior art keywords
dpp
formula
substituted
cyanopyrrolidines
dipeptidyl
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Granted
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CA002350609A
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French (fr)
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CA2350609C (en
Inventor
Edwin Bernard Villhauer
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Novartis AG
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Application filed by Individual filed Critical Individual
Publication of CA2350609A1 publication Critical patent/CA2350609A1/en
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Publication of CA2350609C publication Critical patent/CA2350609C/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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

Abstract

The present invention relates to a compound of formula (I), wherein R is substituted adamantyl; and n is 0 to 3; in free form or in acid addition salt form. Compounds of formula (I) inhibit DPP-IV (dipeptidyl-peptidase-IV) activity. They are therefore indicated for use as pharmaceuticals in inhibiting DPP-IV and in the treatment of conditions mediated by DPP-IV, such as non-insulin-dependent diabetes mellitus, arthritis, obesity, osteoporosis and further conditions of impaired glucose tolerance.
CA002350609A 1998-12-10 1999-12-09 N-substituted 2-cyanopyrrolidines Expired - Lifetime CA2350609C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US20906898A 1998-12-10 1998-12-10
US09/209,068 1998-12-10
PCT/EP1999/009708 WO2000034241A1 (en) 1998-12-10 1999-12-09 N-substituted 2-cyanopyrrolidines

Publications (2)

Publication Number Publication Date
CA2350609A1 true CA2350609A1 (en) 2000-06-15
CA2350609C CA2350609C (en) 2008-09-02

Family

ID=22777194

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002350609A Expired - Lifetime CA2350609C (en) 1998-12-10 1999-12-09 N-substituted 2-cyanopyrrolidines

Country Status (34)

Country Link
US (1) US6166063A (en)
EP (1) EP1137635B1 (en)
JP (2) JP3681110B2 (en)
KR (2) KR100509311B1 (en)
CN (1) CN1160330C (en)
AR (1) AR023719A1 (en)
AT (1) ATE307112T1 (en)
BR (1) BRPI9915985B8 (en)
CA (1) CA2350609C (en)
CO (1) CO5150173A1 (en)
CY (3) CY1105355T1 (en)
CZ (1) CZ299151B6 (en)
DE (3) DE122008000007I1 (en)
DK (1) DK1137635T3 (en)
ES (1) ES2251847T3 (en)
FR (1) FR08C0005I2 (en)
HK (1) HK1040394B (en)
HU (1) HU226769B1 (en)
ID (1) ID28796A (en)
IL (2) IL143091A0 (en)
LU (2) LU91409I2 (en)
MY (1) MY123244A (en)
NL (2) NL300333I2 (en)
NO (3) NO318741B1 (en)
NZ (1) NZ511935A (en)
PE (1) PE20001317A1 (en)
PL (1) PL199443B1 (en)
RU (1) RU2251544C2 (en)
SK (1) SK286635B6 (en)
TR (1) TR200101478T2 (en)
TW (1) TW509674B (en)
UY (1) UY25843A1 (en)
WO (1) WO2000034241A1 (en)
ZA (1) ZA200104581B (en)

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