US 7,605,272 B2Granted

IGF-1R inhibitor

AssigneeKyowa Hakko Kirin Co., Ltd.

InventorsYutaka Kanda, Hiromi Ando, Keiko Kawashima, Takamasa Sugita, Masayo Suzuki, Hisashi Tagaya, Tomoyuki Nakazato, Yoshinori Yamashita, Takeshi Takahashi, Shinji Nara, Hiroaki Nakamura

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Abstract

The present invention provides a type I insulin-like growth factor receptor (IGF-1R) inhibitor comprising, as an active ingredient, an indazole derivative represented by Formula (I): {wherein R1 represents —NR4R5 [wherein R4 represents a hydrogen atom or the like, R5 represents substituted or unsubstituted lower alkyl, —C(═O)R6 (wherein R6 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl or the like), or the like], or the like, and R2 and R3 may be the same or different and each represents a hydrogen atom, hydroxy, substituted or unsubstituted lower alkoxy, or the like} or a pharmaceutically acceptable salt thereof, and the like.

Claims16

Dependent claims

An indazole derivative represented by Formula (IIIb):

{wherein R4 represents a hydrogen atom or substituted or unsubstituted lower alkyl,
R5 represents a hydrogen atom, substituted or unsubstituted lower alkyl, a substituted or unsubstituted heterocyclic group, —C(═S)NH2, —C(═O)R6 [wherein R6 represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, substituted or unsubstituted aryl, a substituted or unsubstituted heterocyclic group, or —NR7aR7b (wherein R7a and R7b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, substituted or unsubstituted aryl, or a substituted or unsubstituted heterocyclic group, or R7a and R7b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group)] or —S(O)2R8 (wherein R8 represents substituted or unsubstituted lower alkyl or substituted or unsubstituted aryl), or R4 and R5 are combined together with the adjacent nitrogen atom thereto to form nitro, a substituted or unsubstituted heterocyclic group, —N═CH—R18 (wherein R18 represents substituted or unsubstituted aryl, or a substituted or unsubstituted heterocyclic group), or —N═CH—NR9aR9b (wherein R9a and R9b may be the same or different and each represents a hydrogen atom or lower alkyl), and
R11a and R11b have the same meanings as R7a and R7b defined above, respectively},
or a pharmaceutically acceptable salt thereof.

1 more element

An indazole derivative selected from the group consisting of:

(E)-N-{2-[2-(1H-indazol-3-yl)vinyl]-5-(4-methylpiperazin-1-ylmethyl)phenyl}-3-methylthiophene-2-carboxamide,
(E)-N-{5-[4-(2-hydroxyethyl)piperazin-1-ylmethyl]-2-[2-(1H-indazol-3-yl)vinyl]phenyl}-3-methylthiophene-2-carboxamide,
(E)-N-{2-[2-(1H-indazol-3-yl)vinyl]-5-piperazin-1-ylmethyl}phenyl}-3-methylthiophene-2-carboxamide,
(E)-N-{2-[2-(1H-indazol-3-yl)vinyl]-5-[4-(2-methoxyacetyl)piperazin-1-ylmethyl]phenyl}-3-methylthiophene-2-carboxamide,
(E)-N-{2-[2-(1H-indazol-3-yl)vinyl]-5-[4-(2-hydroxyacetyl)piperazin-1-ylmethyl]phenyl}-3-methylthiophene-2-carboxamide,
(E)-N-{5-(4-acetylpiperazin-1-ylmethyl)-2-[2-(1H-indazol-3-yl)vinyl]phenyl}-3-methylthiophene-2-carboxamide,
(E)-N-{2-[2-(1H-indazol-3-yl)vinyl]-5-[4-(2-methoxyethyl)piperazin-1-ylmethyl]phenyl}-3-methylthiophene-2-carboxamide,
(E)-N-{5-[4-(3-hydroxypropyl)piperazin-1-ylmethyl]-2-[2-(1H-indazol-3-yl)vinyl]phenyl}-3-methylthiophene-2-carboxamide,
(E)-N-{5-[4-(2-hydroxy-2-methylpropyl)piperazin-1-ylmethyl]-2-[2-(1H-indazol-3-yl)vinyl]phenyl}-3-methylthiophene-2-carboxamide,
(E)-{2-[2-(1H-indazol-3-yl)vinyl]-5-[4-(3-oxobutyl)piperazin-1-ylmethyl]phenyl}-3-methylthiophene-2-carboxamide, and
(E)-N-{5-[4-(3-hydroxy-3-methylbutyl)piperidin-1-ylmethyl]-2-[2-(1H-indazol-3-yl)vinyl]phenyl}-3-methylthiophene-2-carboxamide,
or a pharmaceutically acceptable salt thereof.

9 more elements

Dependencies are inferred from the claim text.

Facts

Application: 11/814,753Filed 27 Jan 2006
Priority: JP 2005-02015827 Jan 2005
Published: US 2009/0054508 A126 Feb 2009
Granted: 20 Oct 2009
Term ends: Not estimatedThe source records don’t support an estimate.

Classification16 codes

C07D 231/56
Condensed with carbocyclic rings or ring systems: benzopyrazoles; Hydrogenated benzopyrazoles
A61P 3/10
For glucose homeostasis: for hyperglycaemia, e.g. antidiabetics
A61P 13/08
Drugs for disorders of the urinary system: of the prostate
A61P 13/10
Drugs for disorders of the urinary system: of the bladder