JP4745446B2 - Ｇｌｙｔ−１阻害剤の合成 - Google Patents

Ｇｌｙｔ−１阻害剤の合成 Download PDF

Info

Publication number
JP4745446B2
JP4745446B2 JP2009552166A JP2009552166A JP4745446B2 JP 4745446 B2 JP4745446 B2 JP 4745446B2 JP 2009552166 A JP2009552166 A JP 2009552166A JP 2009552166 A JP2009552166 A JP 2009552166A JP 4745446 B2 JP4745446 B2 JP 4745446B2
Authority
JP
Japan
Prior art keywords
formula
hours
compound
suspension
reaction
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.)
Active
Application number
JP2009552166A
Other languages
English (en)
Japanese (ja)
Other versions
JP2010520251A5 (show.php
JP2010520251A (ja
Inventor
フレガー，クリストフ
ヴァルトマイヤー，ピウス
ワン，シャオニン
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
F Hoffmann La Roche AG
Original Assignee
F Hoffmann La Roche AG
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Publication of JP2010520251A publication Critical patent/JP2010520251A/ja
Publication of JP2010520251A5 publication Critical patent/JP2010520251A5/ja
Application granted granted Critical
Publication of JP4745446B2 publication Critical patent/JP4745446B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
JP2009552166A 2007-03-05 2008-02-25 Ｇｌｙｔ−１阻害剤の合成 Active JP4745446B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP07103485 2007-03-05
EP07103485.4 2007-03-05
PCT/EP2008/052244 WO2008107334A2 (en) 2007-03-05 2008-02-25 Process for the synthesis of glyt-1 inhibitors

Publications (3)

Publication Number Publication Date
JP2010520251A JP2010520251A (ja) 2010-06-10
JP2010520251A5 JP2010520251A5 (show.php) 2010-12-09
JP4745446B2 true JP4745446B2 (ja) 2011-08-10

Family

ID=39469606

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2009552166A Active JP4745446B2 (ja) 2007-03-05 2008-02-25 Ｇｌｙｔ−１阻害剤の合成

Country Status (13)

Country Link
US (1) US7812161B2 (show.php)
EP (1) EP2131843B1 (show.php)
JP (1) JP4745446B2 (show.php)
KR (1) KR101143073B1 (show.php)
CN (1) CN101622000B (show.php)
AT (1) ATE532516T1 (show.php)
AU (1) AU2008223915B2 (show.php)
BR (1) BRPI0808570B8 (show.php)
CA (1) CA2678630C (show.php)
ES (1) ES2375585T3 (show.php)
IL (1) IL200323A (show.php)
MX (1) MX2009009065A (show.php)
WO (1) WO2008107334A2 (show.php)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5656474B2 (ja) 2010-06-28 2015-01-21 関東化学株式会社 脂肪族光学活性フルオロアルコールの製造方法
CN104628679B (zh) * 2013-11-08 2018-02-09 江苏恩华药业股份有限公司 Bitopertin的合成方法及其中间体
CN106397312B (zh) * 2015-07-31 2020-03-24 广东东阳光药业有限公司 一种制备glyt-1抑制剂的方法
EP4087570A4 (en) 2020-01-09 2024-04-03 Disc Medicine, Inc. METHODS OF TREATING ERYTHROPOIETIC PROTOPORPHYRIA, X-LINKED PROTOPORPHYRIA OR CONGENITAL ERYTHROPOIETIC PORPHYRIA WITH GLYCINE TRANSPORT INHIBITORS
EP4229051A1 (en) 2020-10-13 2023-08-23 Boehringer Ingelheim International GmbH Process of reworking
CN119768399A (zh) 2022-08-24 2025-04-04 勃林格殷格翰国际有限公司 GlyT-1抑制剂的可规模化制备方法

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3992441A (en) * 1972-12-26 1976-11-16 Pfizer Inc. Sulfamylbenzoic acids
US4480102A (en) * 1982-07-23 1984-10-30 The Dow Chemical Company 2,3-Difluoro-5-(trifluoromethyl)pyridine and methods of making and using the same
IE62792B1 (en) * 1988-11-24 1995-03-08 Akzo Nv Pharmaceutical composition containing 1-(mono- or bis (Trifluoromethyl)-2-pyridinyl) piperazines
DE4235155A1 (de) * 1992-10-19 1994-04-21 Basf Ag Verfahren zur Herstellung von Methylsulfonylbenzoesäuren
KR20010042851A (ko) * 1998-04-20 2001-05-25 후지야마 아키라 ｃＧＭＰ 포스포디에스터라제 억제자로서의 안트라닐산유도체
DE10112040A1 (de) * 2001-03-14 2002-10-02 Aventis Pharma Gmbh Verbessertes Verfahren zur Herstellung von Sulfonylcarboxamidderivaten
GB0227240D0 (en) * 2002-11-21 2002-12-31 Glaxo Group Ltd Compounds
CN1867554B (zh) * 2003-08-11 2011-07-06 弗·哈夫曼-拉罗切有限公司 具有邻-取代的苯基的哌嗪及其作为glyt1抑制剂的用途
AU2005313581B2 (en) * 2004-12-09 2011-06-09 F. Hoffmann-La Roche Ag Phenyl-piperazin methanone derivatives
CA2593453A1 (en) * 2005-01-06 2006-07-13 F. Hoffmann-La Roche Ag Sulfanyl substituted phenyl methanones as glycine transporter 1 (glyt-1) inhibitors for the treatment of neurological and neuropsychiatric disorders
ATE472327T1 (de) * 2005-01-07 2010-07-15 Hoffmann La Roche Ä4-(heteroaryl)piperazin-1-ylü-(2,5-substituier e phenyl)methanon-derivate als glycin-transporter 1 (glyt-1) hemmer zur behandlung von neurologischen und neuropsychiatrischen erkrankungen
MX2008000260A (es) * 2005-07-08 2008-03-24 Hoffmann La Roche Reduccion asimetrica de 1,1,1-trifluoroacetona.

Also Published As

Publication number Publication date
CA2678630C (en) 2015-04-14
US20080221327A1 (en) 2008-09-11
KR101143073B1 (ko) 2012-05-08
BRPI0808570B1 (pt) 2020-09-15
EP2131843B1 (en) 2011-11-09
BRPI0808570B8 (pt) 2021-05-25
CN101622000A (zh) 2010-01-06
IL200323A0 (en) 2010-04-29
WO2008107334A2 (en) 2008-09-12
US7812161B2 (en) 2010-10-12
BRPI0808570A2 (pt) 2014-09-02
JP2010520251A (ja) 2010-06-10
AU2008223915A1 (en) 2008-09-12
EP2131843A2 (en) 2009-12-16
ATE532516T1 (de) 2011-11-15
KR20090110368A (ko) 2009-10-21
IL200323A (en) 2013-11-28
CA2678630A1 (en) 2008-09-12
CN101622000B (zh) 2012-07-04
MX2009009065A (es) 2009-08-31
AU2008223915B2 (en) 2013-05-02
WO2008107334A3 (en) 2008-10-23
ES2375585T3 (es) 2012-03-02

Similar Documents

Publication Publication Date Title
JP4745446B2 (ja) Ｇｌｙｔ−１阻害剤の合成
KR102230628B1 (ko) 보르티옥세틴 제조 방법
JP2021536471A (ja) メチル６−（２，４−ジクロロフェニル）−５−［４−［（３ｓ）−１−（３−フルオロプロピル）ピロリジン−３−イル］オキシフェニル］−８，９−ジヒドロ−７ｈ−ベンゾ［７］アンヌレン−２−カルボキシレートの塩およびその製造方法
JP5805880B2 (ja) １−（４−（４−（３，４−ジクロロ−２−フルオロフェニルアミノ）−７−メトキシキナゾリン−６−イルオキシ）ピペリジン−１−イル）−プロパ−２−エン−１−オン塩酸塩の製造方法および該方法で用いられる中間体
EP3848361B1 (en) Method of producing tetracyclic compound
JP5899204B2 (ja) キラルなβ−アミノカルボキサミド誘導体の製造方法
JP4688292B2 (ja) 純粋な鏡像体であるｎ−メチル−ｎ−［（１ｓ）−１−フェニル−２−（（３ｓ）−３−ヒドロキシピロリジン−１−イル）エチル］−２，２−ジフェニルアセトアミドの製造方法
JP4240146B2 (ja) ４（３ｈ）−キナゾリノン誘導体の製造方法
JP4157766B2 (ja) 置換イミダゾピリジン化合物の製造方法
JP2020070296A (ja) リナグリプチンの製造法
JP5065020B2 (ja) レボフロキサシンまたはその水和物の製造方法
JP2008115179A (ja) 光学活性２−［（ｎ−ベンジルプロリル）アミノ］ベンゾフェノン化合物の製造方法
CN102712600A (zh) 制备吲唑-3-甲酸和n-(s)-1-氮杂双环[2.2.2]辛-3-基-1h-吲唑-3-甲酰胺盐酸盐的方法
JP2003342259A (ja) 光学活性シスピペリジン誘導体の製造法
JP2003342259A5 (show.php)
US20240228437A1 (en) Method for producing pyrrolidine compound
CN117510398A (zh) 一种高光学纯度(3r,4r)/(3s,4s)-n-boc-4-氨基-3-羟基哌啶的制备方法
CN119306646A (zh) 制备吡咯酰胺化合物的方法及其中间体
CN118994148A (zh) 非奈利酮的制备方法及中间体
WO2020129877A1 (ja) イソキノリンスルホニルクロリド酸付加塩及びその製造方法
KR20220131963A (ko) Cdk 저해 활성을 나타내는 퓨린 유도체의 제조 방법
JPH11152267A (ja) ピロリジノン誘導体の製造方法
JP2008127308A (ja) 光学活性５−オキソピロリジン−３−カルボン酸誘導体の製造法
JP2014227362A (ja) 抗菌活性化合物の製造方法

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20101019

A871 Explanation of circumstances concerning accelerated examination

Free format text: JAPANESE INTERMEDIATE CODE: A871

Effective date: 20101019

A975 Report on accelerated examination

Free format text: JAPANESE INTERMEDIATE CODE: A971005

Effective date: 20101111

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20101116

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20110216

RD03 Notification of appointment of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7423

Effective date: 20110304

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20110322

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20110331

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20110510

A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20110511

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20140520

Year of fee payment: 3

R150 Certificate of patent or registration of utility model

Ref document number: 4745446

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250