JP2011157377A - ベンゾイソオキサゾール - Google Patents
ベンゾイソオキサゾール Download PDFInfo
- Publication number
- JP2011157377A JP2011157377A JP2011081947A JP2011081947A JP2011157377A JP 2011157377 A JP2011157377 A JP 2011157377A JP 2011081947 A JP2011081947 A JP 2011081947A JP 2011081947 A JP2011081947 A JP 2011081947A JP 2011157377 A JP2011157377 A JP 2011157377A
- Authority
- JP
- Japan
- Prior art keywords
- compound
- acid addition
- free base
- formula
- addition salt
- 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
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- 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
Abstract
Description
[式中、Rは上記に定義したものであり、Xはハロゲンである]
そうして得られた式Iの化合物を遊離塩基または酸付加塩の形で回収するステップとを含む、式Iの化合物およびその塩を生成するための方法を提供する。
式IIの化合物(R)−1−(4−{3−[4−(6−フルオロ−ベンゾ[d]イソオキサゾール−3−イル)−ピペリジン−1−イル]プロポキシ}−3−メトキシ−フェニル)−エタノールは、式Vbの試薬(S)−2−メチル−CBS−オキサザボロリジン−ボラン錯体を用いることにより得られる。
y E.らのAngew. Chem., Int. Ed. Engl. 1998, 37, 1986を参照されたい)。
(S)−(−)−デカン酸1−(4−{3−[4−(6−フルオロ−ベンゾ[d]イソオキサゾール−3−イル)−ピペリジン−1−イル]−プロポキシ}−3−メトキシ−フェニル)−エチルエステル
融点:138.2〜138.8℃
Claims (8)
- 薬剤として使用するための、遊離塩基の形または薬剤として許容される酸付加塩の形をとる、請求項1または2記載の化合物。
- 精神病性障害の治療に使用するための、遊離塩基の形または薬剤として許容される酸付加塩の形をとる、請求項1または2記載の化合物。
- 遊離塩基の形または薬剤として許容される酸付加塩の形をとる請求項1または2記載の化合物を、薬剤用の担体または希釈剤と組み合わせて含む薬剤組成物。
- 遊離塩基の形または薬剤として許容される酸付加塩の形をとる請求項1または2記載の化合物の、精神病性障害の治療用薬剤としての使用。
- 遊離塩基の形または薬剤として許容される酸付加塩の形をとる請求項1または2記載の化合物の、精神病性障害の治療用薬物を製造するための使用。
- 治療に有効な量の請求項1または2記載の化合物を遊離塩基の形または薬剤として許容される酸付加塩の形で患者に投与するステップを含む、精神病性障害の治療を必要とする患者の精神病性障害を治療するための方法。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB0322994.5 | 2003-10-01 | ||
GBGB0322994.5A GB0322994D0 (en) | 2003-10-01 | 2003-10-01 | Organic compounds |
Related Parent Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2006530057A Division JP2007507455A (ja) | 2003-10-01 | 2004-09-30 | ベンゾイソオキサゾール |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2011157377A true JP2011157377A (ja) | 2011-08-18 |
JP5794667B2 JP5794667B2 (ja) | 2015-10-14 |
Family
ID=29415309
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2006530057A Pending JP2007507455A (ja) | 2003-10-01 | 2004-09-30 | ベンゾイソオキサゾール |
JP2011081947A Active JP5794667B2 (ja) | 2003-10-01 | 2011-04-01 | ベンゾイソオキサゾール |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2006530057A Pending JP2007507455A (ja) | 2003-10-01 | 2004-09-30 | ベンゾイソオキサゾール |
Country Status (13)
Country | Link |
---|---|
US (7) | US20070197595A1 (ja) |
EP (1) | EP1668003B1 (ja) |
JP (2) | JP2007507455A (ja) |
AT (1) | ATE378331T1 (ja) |
CY (1) | CY1107277T1 (ja) |
DE (1) | DE602004010161T2 (ja) |
DK (1) | DK1668003T3 (ja) |
ES (1) | ES2297493T3 (ja) |
GB (1) | GB0322994D0 (ja) |
PL (1) | PL1668003T3 (ja) |
PT (1) | PT1668003E (ja) |
SI (1) | SI1668003T1 (ja) |
WO (1) | WO2005030763A1 (ja) |
Families Citing this family (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB0322994D0 (en) * | 2003-10-01 | 2003-11-05 | Novartis Ag | Organic compounds |
WO2012032532A1 (en) * | 2010-09-07 | 2012-03-15 | Symed Labs Limited | "processes for the preparation of 4'-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidino]propoxy]-3'-methoxyacetophenone and intermediates thereof" |
BR112014022687A8 (pt) * | 2012-03-14 | 2021-07-06 | Vanda Pharmaceuticals Inc | uso de uma quantidade eficaz de r-p88 ou um sal farmaceuticamente aceitável do mesmo, ou um éster do mesmo ou um sal farmaceuticamente aceitável de um éster do mesmo, composição farmacêutica, r-p88 ou um sal farmaceuticamente aceitável do mesmo, ou um éster do mesmo ou um sal farmaceuticamente aceitável de um éster do mesmo |
Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH0363263A (ja) * | 1989-05-19 | 1991-03-19 | Hoechst Roussel Pharmaceut Inc | N―(アリールオキシアルキル)ヘテロアリールピペリジンおよびn―(アリールオキシアルキル)ヘテロアリールピペラジン |
JPH07501055A (ja) * | 1991-11-05 | 1995-02-02 | ヘキスト マリオン ラッセル,インコーポレイティド | ヘテロアリールピペリジン、ピロリジン及びピペラジン、及び抗精神病薬及び鎮痛薬としてのそれらの使用 |
JPH09511215A (ja) * | 1993-10-28 | 1997-11-11 | ヘキスト・マリオン・ルセル・インコーポレイテツド | ヘテロアリールピペリジン、ピロリジンおよびピペラジンならびに抗精神病剤および鎮痛剤としてのその使用 |
Family Cites Families (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4804663A (en) * | 1985-03-27 | 1989-02-14 | Janssen Pharmaceutica N.V. | 3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles |
US5994392A (en) * | 1988-02-26 | 1999-11-30 | Neuromedica, Inc. | Antipsychotic prodrugs comprising an antipsychotic agent coupled to an unsaturated fatty acid |
US5158952A (en) * | 1988-11-07 | 1992-10-27 | Janssen Pharmaceutica N.V. | 3-[2-[4-(6-fluoro-1,2-benzisoxozol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9 tetrahydro-9-hydroxy-2-methyl-4H-pyrido [1,2-a]pyrimidin-4-one, compositions and method of use |
TW487572B (en) * | 1996-05-20 | 2002-05-21 | Janssen Pharmaceutica Nv | Aqueous suspensions of 9-hydroxyrisperidone fatty acid esters |
US5795909A (en) * | 1996-05-22 | 1998-08-18 | Neuromedica, Inc. | DHA-pharmaceutical agent conjugates of taxanes |
IL119095A (en) * | 1996-08-19 | 2000-06-01 | Mul T Lock Technologies Ltd | Lock housing |
US6225321B1 (en) * | 1997-06-05 | 2001-05-01 | Oliver Yoa-Pu Hu | Long analgesic acting nalbuphine polyester derivative and method of use |
UA72189C2 (uk) * | 1997-11-17 | 2005-02-15 | Янссен Фармацевтика Н.В. | Фармацевтична композиція, що містить водну суспензію субмікронних ефірів 9-гідроксирисперидон жирних кислот |
US5955459A (en) * | 1997-11-26 | 1999-09-21 | Neuromedica, Inc. | Fatty acid-antipsychotic compositions and uses thereof |
JP4634694B2 (ja) * | 2001-03-23 | 2011-02-16 | ルイトポルド・ファーマシューティカルズ・インコーポレーテッド | 脂肪アルコール薬物複合体 |
JP2005504783A (ja) * | 2001-08-31 | 2005-02-17 | ノバルティス アクチエンゲゼルシャフト | イロペリドン代謝産物の光学異性体 |
WO2004010932A2 (en) * | 2002-07-30 | 2004-02-05 | Peter Migaly | Combination therapy for depression, prevention of suicide, and varous medical and psychiatric conditions |
GB0322994D0 (en) * | 2003-10-01 | 2003-11-05 | Novartis Ag | Organic compounds |
-
2003
- 2003-10-01 GB GBGB0322994.5A patent/GB0322994D0/en not_active Ceased
-
2004
- 2004-09-30 AT AT04787069T patent/ATE378331T1/de active
- 2004-09-30 ES ES04787069T patent/ES2297493T3/es active Active
- 2004-09-30 EP EP04787069A patent/EP1668003B1/en active Active
- 2004-09-30 PL PL04787069T patent/PL1668003T3/pl unknown
- 2004-09-30 PT PT04787069T patent/PT1668003E/pt unknown
- 2004-09-30 DE DE602004010161T patent/DE602004010161T2/de active Active
- 2004-09-30 JP JP2006530057A patent/JP2007507455A/ja active Pending
- 2004-09-30 US US10/575,040 patent/US20070197595A1/en not_active Abandoned
- 2004-09-30 SI SI200430526T patent/SI1668003T1/sl unknown
- 2004-09-30 DK DK04787069T patent/DK1668003T3/da active
- 2004-09-30 WO PCT/EP2004/010938 patent/WO2005030763A1/en active IP Right Grant
-
2008
- 2008-02-01 CY CY20081100126T patent/CY1107277T1/el unknown
-
2011
- 2011-03-14 US US13/047,045 patent/US20110172272A1/en not_active Abandoned
- 2011-04-01 JP JP2011081947A patent/JP5794667B2/ja active Active
-
2017
- 2017-01-20 US US15/411,510 patent/US20170129878A1/en not_active Abandoned
- 2017-11-24 US US15/822,062 patent/US20180118729A1/en not_active Abandoned
-
2018
- 2018-08-21 US US16/107,073 patent/US20190055228A1/en not_active Abandoned
-
2019
- 2019-05-28 US US16/423,252 patent/US20190276444A1/en not_active Abandoned
- 2019-12-26 US US16/727,101 patent/US20200131166A1/en not_active Abandoned
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH0363263A (ja) * | 1989-05-19 | 1991-03-19 | Hoechst Roussel Pharmaceut Inc | N―(アリールオキシアルキル)ヘテロアリールピペリジンおよびn―(アリールオキシアルキル)ヘテロアリールピペラジン |
JPH07501055A (ja) * | 1991-11-05 | 1995-02-02 | ヘキスト マリオン ラッセル,インコーポレイティド | ヘテロアリールピペリジン、ピロリジン及びピペラジン、及び抗精神病薬及び鎮痛薬としてのそれらの使用 |
JPH09511215A (ja) * | 1993-10-28 | 1997-11-11 | ヘキスト・マリオン・ルセル・インコーポレイテツド | ヘテロアリールピペリジン、ピロリジンおよびピペラジンならびに抗精神病剤および鎮痛剤としてのその使用 |
Non-Patent Citations (1)
Title |
---|
JPN6010060513; 第4版 実験化学講座22 -酸・アミノ酸・ペプチド- 第2刷, 1994, 第43-54頁, 丸善株式会社 * |
Also Published As
Publication number | Publication date |
---|---|
ATE378331T1 (de) | 2007-11-15 |
DE602004010161D1 (de) | 2007-12-27 |
US20200131166A1 (en) | 2020-04-30 |
SI1668003T1 (sl) | 2008-04-30 |
WO2005030763A1 (en) | 2005-04-07 |
DK1668003T3 (da) | 2008-03-03 |
PT1668003E (pt) | 2007-12-31 |
PL1668003T3 (pl) | 2008-05-30 |
US20070197595A1 (en) | 2007-08-23 |
JP5794667B2 (ja) | 2015-10-14 |
US20170129878A1 (en) | 2017-05-11 |
JP2007507455A (ja) | 2007-03-29 |
GB0322994D0 (en) | 2003-11-05 |
US20190055228A1 (en) | 2019-02-21 |
ES2297493T3 (es) | 2008-05-01 |
CY1107277T1 (el) | 2012-11-21 |
DE602004010161T2 (de) | 2008-10-30 |
US20110172272A1 (en) | 2011-07-14 |
US20180118729A1 (en) | 2018-05-03 |
EP1668003A1 (en) | 2006-06-14 |
EP1668003B1 (en) | 2007-11-14 |
US20190276444A1 (en) | 2019-09-12 |
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