KR100739901B1 - (s,s)-시스-2-벤즈하이드릴-3-벤질아미노퀴누클리딘의제조 방법 - Google Patents

(s,s)-시스-2-벤즈하이드릴-3-벤질아미노퀴누클리딘의제조 방법 Download PDF

Info

Publication number
KR100739901B1
KR100739901B1 KR1020057006471A KR20057006471A KR100739901B1 KR 100739901 B1 KR100739901 B1 KR 100739901B1 KR 1020057006471 A KR1020057006471 A KR 1020057006471A KR 20057006471 A KR20057006471 A KR 20057006471A KR 100739901 B1 KR100739901 B1 KR 100739901B1
Authority
KR
South Korea
Prior art keywords
acid
benzhydryl
delete
imine
isomer
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.)
Expired - Fee Related
Application number
KR1020057006471A
Other languages
English (en)
Korean (ko)
Other versions
KR20050083764A (ko
Inventor
토마스 씨. 너겐트
로버트 시마이어
Original Assignee
화이자 프로덕츠 인코포레이티드
디에스엠 파마슈티칼스 인코포레이티드
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 화이자 프로덕츠 인코포레이티드, 디에스엠 파마슈티칼스 인코포레이티드 filed Critical 화이자 프로덕츠 인코포레이티드
Publication of KR20050083764A publication Critical patent/KR20050083764A/ko
Application granted granted Critical
Publication of KR100739901B1 publication Critical patent/KR100739901B1/ko
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D453/00Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyrrole Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
KR1020057006471A 2002-10-16 2003-10-10 (s,s)-시스-2-벤즈하이드릴-3-벤질아미노퀴누클리딘의제조 방법 Expired - Fee Related KR100739901B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US41905102P 2002-10-16 2002-10-16
US60/419,051 2002-10-16
PCT/US2003/032275 WO2004035575A1 (en) 2002-10-16 2003-10-10 Process for the preparation of (s,s)-cis-2-benzhydryl-3-benzylaminoquinuclidine

Publications (2)

Publication Number Publication Date
KR20050083764A KR20050083764A (ko) 2005-08-26
KR100739901B1 true KR100739901B1 (ko) 2007-07-13

Family

ID=32108014

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020057006471A Expired - Fee Related KR100739901B1 (ko) 2002-10-16 2003-10-10 (s,s)-시스-2-벤즈하이드릴-3-벤질아미노퀴누클리딘의제조 방법

Country Status (21)

Country Link
US (2) US6861526B2 (enExample)
EP (1) EP1551833A4 (enExample)
JP (1) JP2006506368A (enExample)
KR (1) KR100739901B1 (enExample)
CN (1) CN100418964C (enExample)
AP (1) AP2005003288A0 (enExample)
AR (1) AR041587A1 (enExample)
AU (1) AU2003277353B2 (enExample)
BR (1) BR0315335A (enExample)
CA (1) CA2500635A1 (enExample)
EA (1) EA008192B1 (enExample)
HR (1) HRP20050328A2 (enExample)
IS (1) IS7755A (enExample)
MX (1) MXPA05004058A (enExample)
PA (1) PA8586601A1 (enExample)
PE (1) PE20040777A1 (enExample)
PL (1) PL376218A1 (enExample)
TN (1) TNSN05111A1 (enExample)
UY (1) UY28024A1 (enExample)
WO (1) WO2004035575A1 (enExample)
ZA (1) ZA200502411B (enExample)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7407955B2 (en) 2002-08-21 2008-08-05 Boehringer Ingelheim Pharma Gmbh & Co., Kg 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
EP1713504B1 (en) * 2004-01-30 2017-06-07 Zoetis Services LLC Antimicrobial preservatives to achieve multi-dose formulation using beta-cyclodextrins for liquid dosage forms
ES2296131T3 (es) * 2004-02-02 2008-04-16 Pfizer Products Incorporated Procedimiento para la preparacion de 1-(2s,3s)-2-bencidril-n-(5-terc-butil-2-metoxibencil)quinuclidin-3-amina.
DE102004054054A1 (de) 2004-11-05 2006-05-11 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine
PE20110235A1 (es) 2006-05-04 2011-04-14 Boehringer Ingelheim Int Combinaciones farmaceuticas que comprenden linagliptina y metmorfina
EA030606B1 (ru) 2006-05-04 2018-08-31 Бёрингер Ингельхайм Интернациональ Гмбх Способы приготовления лекарственного средства, содержащего полиморфы
EP1852108A1 (en) 2006-05-04 2007-11-07 Boehringer Ingelheim Pharma GmbH & Co.KG DPP IV inhibitor formulations
PE20140960A1 (es) 2008-04-03 2014-08-15 Boehringer Ingelheim Int Formulaciones que comprenden un inhibidor de dpp4
UY32030A (es) 2008-08-06 2010-03-26 Boehringer Ingelheim Int "tratamiento para diabetes en pacientes inapropiados para terapia con metformina"
KR20200118243A (ko) 2008-08-06 2020-10-14 베링거 인겔하임 인터내셔날 게엠베하 메트포르민 요법이 부적합한 환자에서의 당뇨병 치료
US20200155558A1 (en) 2018-11-20 2020-05-21 Boehringer Ingelheim International Gmbh Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug
CN102256976A (zh) 2008-12-23 2011-11-23 贝林格尔.英格海姆国际有限公司 有机化合物的盐形式
TW201036975A (en) 2009-01-07 2010-10-16 Boehringer Ingelheim Int Treatment for diabetes in patients with inadequate glycemic control despite metformin therapy
EA034869B1 (ru) 2009-11-27 2020-03-31 Бёрингер Ингельхайм Интернациональ Гмбх Лечение генотипированных пациентов с диабетом ингибиторами дпп-4, такими как линаглиптин
KR101819609B1 (ko) 2010-05-05 2018-01-17 베링거 인겔하임 인터내셔날 게엠베하 체중 감소 치료에 후속하는 dpp-4 억제제에 의한 순차적 병용 요법
KR20230051307A (ko) 2010-06-24 2023-04-17 베링거 인겔하임 인터내셔날 게엠베하 당뇨병 요법
AR083878A1 (es) 2010-11-15 2013-03-27 Boehringer Ingelheim Int Terapia antidiabetica vasoprotectora y cardioprotectora, linagliptina, metodo de tratamiento
MX366629B (es) 2011-07-15 2019-07-17 Boehringer Ingelheim Int Quinazolinas sustituidas, su preparación y su uso en composiciones farmacéuticas.
US9555001B2 (en) 2012-03-07 2017-01-31 Boehringer Ingelheim International Gmbh Pharmaceutical composition and uses thereof
EP2849755A1 (en) 2012-05-14 2015-03-25 Boehringer Ingelheim International GmbH A xanthine derivative as dpp -4 inhibitor for use in the treatment of podocytes related disorders and/or nephrotic syndrome
JP6218811B2 (ja) 2012-05-14 2017-10-25 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Sirs及び/又は敗血症の治療に用いるdpp−4阻害薬としてのキサンチン誘導体
WO2013174767A1 (en) 2012-05-24 2013-11-28 Boehringer Ingelheim International Gmbh A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference
WO2015128453A1 (en) 2014-02-28 2015-09-03 Boehringer Ingelheim International Gmbh Medical use of a dpp-4 inhibitor
US10155000B2 (en) 2016-06-10 2018-12-18 Boehringer Ingelheim International Gmbh Medical use of pharmaceutical combination or composition
CN108341812A (zh) * 2017-01-23 2018-07-31 科贝源(北京)生物医药科技有限公司 一种含奎宁环化合物的制备方法
CN108341811A (zh) * 2017-01-23 2018-07-31 科贝源(北京)生物医药科技有限公司 马罗皮坦杂质的制备方法
CN106977512B (zh) * 2017-05-04 2019-01-01 海门慧聚药业有限公司 制备马罗匹坦游离碱的方法

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5162339A (en) * 1988-11-23 1992-11-10 Pfizer Inc. Quinuclidine therapeutic agents

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3560510A (en) * 1969-03-05 1971-02-02 Aldrich Chem Co Inc 2-benzhydrylquinuclidines
US4680283A (en) 1984-09-26 1987-07-14 Merck & Co., Inc. Analogs of substance P and eledoisin
US5138060A (en) 1991-01-03 1992-08-11 Pfizer Inc. Process and intermediates for preparing azabicyclo(2.2.2)octan-3-imines
PL170513B1 (en) 1991-05-22 1996-12-31 Pfizer Method of obtaining novel derivatives of 3-amino quinuclidine
WO1992021677A1 (en) * 1991-05-31 1992-12-10 Pfizer Inc. bibNUCLIDINE DERIVATIVES
EP1114823A3 (en) 1992-08-19 2001-07-18 Pfizer Inc. Substituted benzylamino nitrogen containing non-aromatic heterocycles
US5604241A (en) * 1992-10-21 1997-02-18 Pfizer Inc. Substituted benzylaminoquinuclidines as substance P antagonists
JP2656699B2 (ja) 1992-10-21 1997-09-24 ファイザー製薬株式会社 置換ベンジルアミノキヌクリジン
JP2656700B2 (ja) 1992-10-28 1997-09-24 ファイザー製薬株式会社 置換キヌクリジン誘導体
KR950704311A (ko) * 1992-11-12 1995-11-17 알렌 제이. 스피겔 물질 p 길항체로서의 퀴누클리딘 유도체(quinuclidine derivative as substance p antagonist)
IL109646A0 (en) 1993-05-19 1994-08-26 Pfizer Heteroatom substituted alkyl benzylamino-quinuclidines
PE8798A1 (es) * 1995-07-17 1998-03-02 Pfizer Procedimiento de separacion de los enantiomeros del 1-azabiciclo[2.2.2] octan-3-amina, 2-(difenilmetil) -n- [[2-metoxi-5-(1-metiletil) fenil] metil]
MX9706944A (es) 1996-09-12 1998-08-30 Pfizer Quinuclidinas sustituidas con tetrazolilo como antagonistas de la sustancia p.

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5162339A (en) * 1988-11-23 1992-11-10 Pfizer Inc. Quinuclidine therapeutic agents

Also Published As

Publication number Publication date
CA2500635A1 (en) 2004-04-29
PE20040777A1 (es) 2004-11-20
AR041587A1 (es) 2005-05-26
US20050085641A1 (en) 2005-04-21
US20040116704A1 (en) 2004-06-17
IS7755A (is) 2005-03-17
CN1705664A (zh) 2005-12-07
PA8586601A1 (es) 2005-02-04
UY28024A1 (es) 2004-05-31
HRP20050328A2 (en) 2005-06-30
MXPA05004058A (es) 2005-06-08
AU2003277353B2 (en) 2007-08-09
BR0315335A (pt) 2005-08-16
KR20050083764A (ko) 2005-08-26
WO2004035575A1 (en) 2004-04-29
TNSN05111A1 (en) 2007-05-14
HK1078087A1 (en) 2006-03-03
EA008192B1 (ru) 2007-04-27
AP2005003288A0 (en) 2005-06-30
US6861526B2 (en) 2005-03-01
JP2006506368A (ja) 2006-02-23
EP1551833A1 (en) 2005-07-13
EP1551833A4 (en) 2010-06-02
PL376218A1 (en) 2005-12-27
EA200500650A1 (ru) 2005-10-27
CN100418964C (zh) 2008-09-17
ZA200502411B (en) 2006-05-31
WO2004035575A8 (en) 2005-05-12
AU2003277353A1 (en) 2004-05-04

Similar Documents

Publication Publication Date Title
KR100739901B1 (ko) (s,s)-시스-2-벤즈하이드릴-3-벤질아미노퀴누클리딘의제조 방법
EP3956292B1 (en) A process for the preparation of enantiomerically pure norepinephrine
WO2009084024A2 (en) A process for the preparation of r-sit agliptin and its pharmaceutically acceptable salts thereof
US5504253A (en) Amine preparation
US5936091A (en) Processes and intermediates for resolving piperidyl acetamide stereoisomers
JP2007519710A (ja) 1−(2S,3S)−2−ベンズヒドリル−N−(5−tert−ブチル−2−メトキシベンジル)キヌクリジン−3−アミンの製造方法
US6359139B1 (en) Methods for production of piperidyl acetamide stereoisomers
EP1082307B1 (en) Processes and intermediates for preparing 2-substituted piperidine stereoisomers
US6962997B1 (en) Process and intermediates for resolving piperidyl acetamide steroisomers
KR100220766B1 (ko) 피소스티그민의 제조시 중간체로서 사용되는 알킬화 옥스인돌의 거울상 이성체 선택적 합성방법
US6703508B2 (en) Methods for the stereoselective synthesis of substituted piperidines
HK1078087B (en) Process for the preparation of (s,s)-cis-2-benzhydryl-3-benzylaminoquinuclidine
CN1989097A (zh) 用于制备非对映异构体富集的化合物的方法
CN101460446A (zh) 用于生产光学活性1-(氟-、三氟甲基-或三氟甲氧基-取代苯基)烷基胺n-单烷基衍生物的方法
JP2005075754A (ja) トランス−1,2−ビス(3,5−ジメチルフェニル)−1,2−エタンジアミンの光学分割方法
SK287537B6 (sk) Spôsob výroby N,N-diizopropyl-3-(2-hydroxy-5-metylfenyl)-3- fenylpropylamínu v jeho racemickej alebo opticky aktívnej forme
JP2002308836A (ja) 光学活性1−(フルオロフェニル)エチルアミンの精製方法
JP2002128745A (ja) 光学活性1,2−ビス(2,4,6−トリメチルフェニル)−1,2−エタンジアミンの製造方法

Legal Events

Date Code Title Description
A201 Request for examination
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

AMND Amendment
E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

E601 Decision to refuse application
PE0601 Decision on rejection of patent

St.27 status event code: N-2-6-B10-B15-exm-PE0601

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

J201 Request for trial against refusal decision
PJ0201 Trial against decision of rejection

St.27 status event code: A-3-3-V10-V11-apl-PJ0201

AMND Amendment
P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PB0901 Examination by re-examination before a trial

St.27 status event code: A-6-3-E10-E12-rex-PB0901

B701 Decision to grant
PB0701 Decision of registration after re-examination before a trial

St.27 status event code: A-3-4-F10-F13-rex-PB0701

GRNT Written decision to grant
PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

LAPS Lapse due to unpaid annual fee
PC1903 Unpaid annual fee

St.27 status event code: A-4-4-U10-U13-oth-PC1903

Not in force date: 20100710

Payment event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

PC1903 Unpaid annual fee

St.27 status event code: N-4-6-H10-H13-oth-PC1903

Ip right cessation event data comment text: Termination Category : DEFAULT_OF_REGISTRATION_FEE

Not in force date: 20100710