JP2004189733A5 - - Google Patents

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JP2004189733A5
JP2004189733A5 JP2003393809A JP2003393809A JP2004189733A5 JP 2004189733 A5 JP2004189733 A5 JP 2004189733A5 JP 2003393809 A JP2003393809 A JP 2003393809A JP 2003393809 A JP2003393809 A JP 2003393809A JP 2004189733 A5 JP2004189733 A5 JP 2004189733A5
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compound
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Claims (15)

式(I)
Figure 2004189733
[式中、Rは2個の、同一であっても異なっていても良い炭素数1〜3のアルキル基、またはRが隣接する2個の基である場合、共に結合して硫黄、窒素および酸素原子からなる群から選択される1または2のヘテロ原子を含んでいてもよい飽和の5員または6員の環状基を形成してもよい:
Xは酸素原子または硫黄原子:
は置換基を有していてもよいフェニル、ベンジル、ピリジル、ピリジルメチル、ピリミジニル、シクロヘキシル、メチルピペラジニル、インダニル、1,3−ベンゾジオキソリルおよびナフチルから成る群から選択される、但し、Rがフェニル基の場合、フェニル基の3位および4位が同時にアルコキシで置換されることはない:
Figure 2004189733
は単結合または二重結合:および、
Lは
−(CH−H
(式中、nは1〜8の数);
Figure 2004189733
(式中、Rは水素、炭素数1〜8の直鎖または分岐鎖状アルキル、炭素数1〜3の1以上のフッ素で置換されているアルキル、シクロペンチル、シクロヘキシル、シクロヘプチル、シクロヘキシルメチル、ベンジル、2−ピリジルおよび2−ピリミジニルからなる群から選択される、n'は1〜3の数);
Figure 2004189733
(式中、Wは酸素または硫黄原子、Aは炭素数1〜5の直鎖または分岐鎖状アルキル、2−ジメチルアミノエチルアミノ、2−チアゾリルアミノ、4−メチルホモピペラジニル、4−ピペリジノピペリジノ、ジメチルアミノアニリノ、ピリジルアミノ、ピペリジノ、4−エトキシカルボニルピペリジノ、4−カルボキシピペリジノ、および式(J)
Figure 2004189733
で表される基(式中、Rは上記と同意)からなる群から選択される、n”は0〜3の数);
Figure 2004189733
(式中、Eは水素、炭素数1〜6の直鎖または分岐鎖状アルキルまたはアルケニル、炭素数1〜3の1以上のフッ素で置換されているアルキル、2−メトキシエチル、2−メチルチオエチル、2−ジメチルアミノエチル、フェニル、ピリジル、ベンジル、ピリジルメチル、シクロペンチル、シクロヘキシル、テトラヒドロ−2−ピラニル、シクロヘキシルメチル、1−メチル−4−ピペリジル、インダニル、1,3−ベンゾジオキソリルおよび1−インドリルからなる群から選択される、ここでフェニルおよびピリジルはハロゲン、メチル、メトキシ、イソプロピルおよびアリルからなる群から選択される基で置換されていてもよいn”は0〜3の数);
−(CH)n’−T−G
(式中、Tは酸素、硫黄またはNH、Gは水素、炭素数1〜5の直鎖または分岐鎖状アルキル、炭素数1〜3の1以上のフッ素で置換されているアルキル、2−メトキシエチル、およびアルキルカルボニルからなる群から選択される、n’は1〜3の数);
Figure 2004189733
(式中、Rは前記と同意義);
Figure 2004189733
(式中、Eは前記と同意義);
Figure 2004189733
(式中、Rは前記と同意義):または、
Figure 2004189733
(式中、Eは前記と同意義)]
で表される化合物、またはその塩。
Formula (I)
Figure 2004189733
[Wherein, R 1 is two alkyl groups having 1 to 3 carbon atoms which may be the same or different, or, when R 1 is two adjacent groups, they are bonded together to form sulfur, A saturated 5- or 6-membered cyclic group that may contain 1 or 2 heteroatoms selected from the group consisting of nitrogen and oxygen atoms may be formed:
X is an oxygen atom or a sulfur atom:
R 2 is selected from the group consisting of optionally substituted phenyl, benzyl, pyridyl, pyridylmethyl, pyrimidinyl, cyclohexyl, methylpiperazinyl, indanyl, 1,3-benzodioxolyl and naphthyl; However, when R 2 is a phenyl group, the 3-position and 4-position of the phenyl group are not simultaneously substituted with alkoxy:
Figure 2004189733
Is a single bond or a double bond: and
L is - (CH 2) n -H
(Where n is a number from 1 to 8);
Figure 2004189733
(Wherein R 3 is hydrogen, linear or branched alkyl having 1 to 8 carbon atoms, alkyl substituted with one or more fluorines having 1 to 3 carbon atoms, cyclopentyl, cyclohexyl, cycloheptyl, cyclohexylmethyl, Selected from the group consisting of benzyl, 2-pyridyl and 2-pyrimidinyl, n ′ is a number from 1 to 3);
Figure 2004189733
Wherein W is an oxygen or sulfur atom, A is a linear or branched alkyl having 1 to 5 carbon atoms, 2-dimethylaminoethylamino, 2-thiazolylamino, 4-methylhomopiperazinyl, 4-piperidin Nopiperidino, dimethylaminoanilino, pyridylamino, piperidino, 4-ethoxycarbonylpiperidino, 4-carboxypiperidino, and formula (J)
Figure 2004189733
(Wherein R 3 is the same as above), n ″ is a number from 0 to 3);
Figure 2004189733
(In the formula, E is hydrogen, linear or branched alkyl or alkenyl having 1 to 6 carbon atoms, alkyl substituted with one or more fluorines having 1 to 3 carbon atoms, 2-methoxyethyl, 2-methylthioethyl) , 2-dimethylaminoethyl, phenyl, pyridyl, benzyl, pyridylmethyl, cyclopentyl, cyclohexyl, tetrahydro -2 H - pyranyl, cyclohexylmethyl, 1-methyl-4-piperidyl, indanyl, 1,3-benzodioxolyl and 1 Selected from the group consisting of H -indolyl, wherein phenyl and pyridyl may be substituted with a group selected from the group consisting of halogen, methyl, methoxy, isopropyl and allyl, n ″ is a number from 0 to 3) ;
- (CH 2) n '-T -G
(Wherein T is oxygen, sulfur or NH, G is hydrogen, linear or branched alkyl having 1 to 5 carbon atoms, alkyl substituted with one or more fluorines having 1 to 3 carbon atoms, 2-methoxy Selected from the group consisting of ethyl and alkylcarbonyl, n ′ is a number from 1 to 3);
Figure 2004189733
(Wherein R 3 is as defined above);
Figure 2004189733
(Wherein E is as defined above);
Figure 2004189733
(Wherein R 3 is as defined above): or
Figure 2004189733
(Wherein E is as defined above)]
Or a salt thereof.
がメチルおよびエチルからなる群から選択される2個の基である、請求項1記載の化合物。 The compound according to claim 1, wherein R 1 is two groups selected from the group consisting of methyl and ethyl. が5,6−ジメチルである、請求項2記載の化合物。 The compound according to claim 2, wherein R 1 is 5,6-dimethyl. 式(I−1):
Figure 2004189733
[式中、Mはイソインドリン環と共に、硫黄、窒素および酸素原子からなる群から選択される1または2のヘテロ原子を含んでいてもよい飽和の5員または6員の環状基を形成する基、
X、RおよびLは請求項1と同意義]
で表される、請求項1記載の化合物またはその塩。
Formula (I-1):
Figure 2004189733
[Wherein, M is a group which forms a saturated 5-membered or 6-membered cyclic group which may contain 1 or 2 heteroatoms selected from the group consisting of sulfur, nitrogen and oxygen atoms together with an isoindoline ring. ,
X, R 2 and L are as defined in claim 1]
The compound or its salt of Claim 1 represented by these.
Mが
−CHCHCH
−CHOCH−および
−OCHO−
からなる群から選択される、請求項4記載の化合物
M is —CH 2 CH 2 CH 2 —.
—CH 2 OCH 2 — and —OCH 2 O—
5. A compound according to claim 4 selected from the group consisting of
が置換されていてもよいフェニルまたはピリジルである、請求項1〜5いずれかに記載の化合物。 And R 2 is is an optionally substituted phenyl or pyridyl, A compound according to any claims 1-5. Lが
Figure 2004189733
[式中、Wは酸素、Aは炭素数1〜5の直鎖、分岐鎖状アルキルおよび式(J)
Figure 2004189733
(式(J)中、Rはメチルまたはイソプロピル)からなる群から選択される]
である、請求項1〜6いずれかに記載の化合物。
L is
Figure 2004189733
[Wherein W is oxygen, A is a linear or branched alkyl having 1 to 5 carbon atoms, and formula (J)
Figure 2004189733
(In the formula (J), R 3 is selected from the group consisting of methyl or isopropyl)]
The compound according to any one of claims 1 to 6, wherein
Lが
Figure 2004189733
[式中、Eはプロピル、イソブチルおよび1以上のメチルおよび/またはメトキシで置換されているフェニル基からなる群から選択される]
である、請求項1〜6いずれかに記載の化合物。
L is
Figure 2004189733
Wherein E is selected from the group consisting of propyl, isobutyl and a phenyl group substituted with one or more methyl and / or methoxy.
The compound according to any one of claims 1 to 6, wherein
Lが
―(CH―T―G
[式中、Tは酸素若しくは硫黄であり、Gはエチルまたはプロピル基である]
である、請求項1〜6いずれかに記載の化合物。
L is — (CH 2 ) 2 —TG
[Wherein T is oxygen or sulfur, and G is an ethyl or propyl group]
The compound according to any one of claims 1 to 6, wherein
下式:
Figure 2004189733
式中、RおよびLは以下の組合せから選択される
Figure 2004189733
Figure 2004189733
で表される化合物またはその医薬上許容される塩である、請求項1記載の化合物。
The following formula:
Figure 2004189733
Wherein R 2 and L are selected from the following combinations
Figure 2004189733
Figure 2004189733
The compound of Claim 1 which is a compound represented by these, or its pharmaceutically acceptable salt.
下式:
Figure 2004189733
式中、RおよびLは以下の組合せから選択される
Figure 2004189733
Figure 2004189733
で表される化合物またはその医薬上許容される塩である、請求項1記載の化合物。
The following formula:
Figure 2004189733
Wherein R 2 and L are selected from the following combinations
Figure 2004189733
Figure 2004189733
The compound of Claim 1 which is a compound represented by these, or its pharmaceutically acceptable salt.
下式
Figure 2004189733
または
Figure 2004189733

[式中、R
Figure 2004189733
(Rは炭素数1〜5のアルキル基、置換されていてもよいフェニルおよびベンジルからなる群から選択される)、Lは
Figure 2004189733
である]
で表される、請求項1記載の化合物。
The following formula
Figure 2004189733
Or
Figure 2004189733

[Wherein R 2 is
Figure 2004189733
(R 4 is selected from the group consisting of an alkyl group having 1 to 5 carbon atoms, optionally substituted phenyl and benzyl), L is
Figure 2004189733
Is]
The compound of Claim 1 represented by these.
麻酔有効量の請求項1〜12いずれかに記載の化合物および医薬上許容されるキャリアを含有してなる、哺乳動物のための麻酔・鎮静薬組成物。   An anesthetic / sedative composition for mammals comprising an anesthetic effective amount of the compound according to any one of claims 1 to 12 and a pharmaceutically acceptable carrier. 静脈投与のためのものである、請求項13記載の組成物。   14. A composition according to claim 13, which is for intravenous administration. 請求項1〜12いずれかに記載の化合物の、哺乳動物用麻酔・鎮静薬組成物を製造するための使用。   Use of the compound according to any one of claims 1 to 12 for producing an anesthetic / sedative composition for mammals.
JP2003393809A 2002-11-26 2003-11-25 Isoindoline derivatives Expired - Fee Related JP4205559B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2003393809A JP4205559B2 (en) 2002-11-26 2003-11-25 Isoindoline derivatives

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Application Number Priority Date Filing Date Title
JP2002342399 2002-11-26
JP2003393809A JP4205559B2 (en) 2002-11-26 2003-11-25 Isoindoline derivatives

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JP2004189733A JP2004189733A (en) 2004-07-08
JP2004189733A5 true JP2004189733A5 (en) 2007-01-18
JP4205559B2 JP4205559B2 (en) 2009-01-07

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Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009513704A (en) * 2005-11-01 2009-04-02 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Substituted dihydroisoindolones as allosteric modulators of glucokinase
CA2627910A1 (en) * 2005-11-01 2007-05-10 Janssen Pharmaceutica N.V. Substituted cycloalkylpyrrolones as allosteric modulators of glucokinase
US7531671B2 (en) * 2005-11-01 2009-05-12 Janssen Pharmaceutica N.V. Dihydroisoindolones as allosteric modulators of glucokinase
CN101316837A (en) * 2005-11-01 2008-12-03 詹森药业有限公司 Substituted pyrrolones as allosteric modulators of glucokinase
EP2948147B1 (en) 2013-01-28 2019-03-13 H. Lundbeck A/S N-substituted-5-substituted phthalamic acids as sortilin inhibitors

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