JP2019073507A5 - - Google Patents

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JP2019073507A5
JP2019073507A5 JP2018195550A JP2018195550A JP2019073507A5 JP 2019073507 A5 JP2019073507 A5 JP 2019073507A5 JP 2018195550 A JP2018195550 A JP 2018195550A JP 2018195550 A JP2018195550 A JP 2018195550A JP 2019073507 A5 JP2019073507 A5 JP 2019073507A5
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carbonyl
pharmaceutically acceptable
oral
active ingredient
acceptable salt
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JP7314494B2 (en
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Claims (5)

式（Ｉ）
Figure 2019073507
 ［式（Ｉ）中、
Ｒ1は、エチル基、４−フルオロフェニル基、又は３，４−ジフルオロフェニル基を示し、
Ｒ2は、下記式群（ＩＩＩｂ）のいずれかの構造を示し、
Figure 2019073507
 Ｒ3は、メチル基を示す。］
で表される化合物、又はその医薬上許容される塩を有効成分として含有し、１種又は２種以上の医薬的に許容される担体、賦形剤及び希釈剤とを含む、気分障害（うつ病、双極性障害を含む）、不安障害、認知障害、発達障害、アルツハイマー病、パーキンソン病、睡眠障害、ハンチントン舞踏病、摂食障害、薬物依存症、てんかん、脳梗塞、脳虚血、脳浮腫、頭部外傷、炎症、免疫関連疾患からなる群から選択される疾患の予防又は治療に用いる経口又は非経口用医薬製剤。 Equation (I)
Figure 2019073507
 [In formula (I),
R 1 represents an ethyl group, a 4-fluorophenyl group, or a 3,4-difluorophenyl group.
R 2 shows the structure of any of the following formula group (IIIb).
Figure 2019073507
 R 3 represents a methyl group. ]
A mood disorder (depression) containing a compound represented by the above, or a pharmaceutically acceptable salt thereof as an active ingredient, and containing one or more pharmaceutically acceptable carriers, excipients and diluents. Diseases, including bipolar disorders), anxiety disorders, cognitive disorders, developmental disorders, Alzheimer's disease, Parkinson's disease, sleep disorders, Huntington's chorea, feeding disorders, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema An oral or parenteral pharmaceutical preparation used for the prevention or treatment of a disease selected from the group consisting of head trauma, inflammation, and immune-related diseases. 有効成分として含有する請求項１に記載の化合物、又はその医薬上許容される塩の投与量が１日当たり０．０１〜５００ｍｇである請求項１に記載の経口又は非経口用医薬製剤。 The oral or parenteral pharmaceutical preparation according to claim 1, wherein the dose of the compound according to claim 1 or a pharmaceutically acceptable salt thereof contained as an active ingredient is 0.01 to 500 mg per day. 有効成分が（１Ｒ，２Ｒ，３Ｒ，５Ｒ，６Ｒ）−２−アミノ−６−フルオロ−３−［（４−フルオロフェニル）メトキシ］−２−（｛（１Ｓ）−１−［（トリシクロ［３．３．１．１3,7］デカン−１−カルボニル）オキシ］エトキシ｝カルボニル）ビシクロ［３．１．０］ヘキサン−６−カルボン酸、又はその医薬上許容される塩である請求項１又は２に記載の経口又は非経口用医薬製剤。
Figure 2019073507
 The active ingredient is (1R, 2R, 3R, 5R, 6R) -2-amino-6-fluoro-3-[(4-fluorophenyl) methoxy] -2-({(1S) -1-[(tricyclo [3]). 3..1.1 3,7 ] Decane-1-carbonyl) Oxy] ethoxy} carbonyl) Bicyclo [3.1.0] Hexane-6-carboxylic acid, or a pharmaceutically acceptable salt thereof. Or the pharmaceutical preparation for oral or parenteral use according to 2.
Figure 2019073507
 有効成分が（１Ｒ，２Ｒ，３Ｒ，５Ｒ，６Ｒ）−２−アミノ−３−［（３，４−ジフルオロフェニル）メトキシ］−６−フルオロ−２−（｛（１Ｓ）−１−［（トリシクロ［３．３．１．１3,7］デカン−１−カルボニル）オキシ］エトキシ｝カルボニル）ビシクロ［３．１．０］ヘキサン−６−カルボン酸、又はその医薬上許容される塩である請求項１又は２に記載の経口又は非経口用医薬製剤。
Figure 2019073507
 The active ingredient is (1R, 2R, 3R, 5R, 6R) -2-amino-3-[(3,4-difluorophenyl) methoxy] -6-fluoro-2-({(1S) -1-[(tricyclo). [3.3.1.1 3,7 ] Decane-1-carbonyl) Oxy] ethoxy} carbonyl) Bicyclo [3.1.0] Hexa-6-carboxylic acid, or a pharmaceutically acceptable salt thereof. Item 3. The oral or parenteral pharmaceutical preparation according to Item 1 or 2.
Figure 2019073507
 有効成分が（１Ｒ，２Ｒ，３Ｒ，５Ｒ，６Ｒ）−２−アミノ−６−フルオロ−２−（｛（１Ｒ）−１−［（｛［（１Ｒ，２Ｓ，５Ｒ）−５−メチル−２−（プロパン−２−イル）シクロヘキシル］オキシ｝カルボニル）オキシ］エトキシ｝カルボニル）−３−プロポキシビシクロ［３．１．０］ヘキサン−６−カルボン酸、又はその医薬上許容される塩である請求項１又は２に記載の経口又は非経口用医薬製剤。
Figure 2019073507
 The active ingredient is (1R, 2R, 3R, 5R, 6R) -2-amino-6-fluoro-2-({(1R) -1-[({[(1R, 2S, 5R) -5-methyl-2). -(Propane-2-yl) cyclohexyl] oxy} carbonyl) oxy] ethoxy} carbonyl) -3-propoxybicyclo [3.1.0] hexane-6-carboxylic acid, or a pharmaceutically acceptable salt thereof. Item 3. The oral or parenteral pharmaceutical preparation according to Item 1 or 2.
Figure 2019073507
JP2018195550A 2017-10-17 2018-10-17 Pharmaceuticals containing prodrugs of amino acid derivatives Active JP7314494B2 (en)

Applications Claiming Priority (2)

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JP2017200722 2017-10-17
JP2017200722 2017-10-17

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JP2019073507A JP2019073507A (en) 2019-05-16
JP2019073507A5 true JP2019073507A5 (en) 2021-11-25
JP7314494B2 JP7314494B2 (en) 2023-07-26

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* Cited by examiner, † Cited by third party
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JP2024004505A (en) * 2020-11-26 2024-01-17 大正製薬株式会社 Method for producing amino acid derivative

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA04006322A (en) 2001-12-27 2004-10-04 Taisho Pharmaceutical Co Ltd 6-fluorobicyclo[3.1.0]hexane derivatives.
JP4461865B2 (en) 2003-04-23 2010-05-12 大正製薬株式会社 Group II metabotropic glutamate receptor antagonist
RS56328B1 (en) 2012-06-01 2017-12-29 Taisho Pharmaceutical Co Ltd Prodrug of fluorine-containing amino acid
JP5983713B2 (en) 2013-11-29 2016-09-06 大正製薬株式会社 Pharmaceuticals containing prodrugs of fluorine-containing amino acids
MX2018012442A (en) 2016-04-18 2019-02-21 Taisho Pharmaceutical Co Ltd Prodrug of amino acid derivative.

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