BR0315335A - Processo para a preparação de (s,s)-cis-2-benzidril-3-benzilaminoquinuclina - Google Patents
Processo para a preparação de (s,s)-cis-2-benzidril-3-benzilaminoquinuclinaInfo
- Publication number
- BR0315335A BR0315335A BR0315335-5A BR0315335A BR0315335A BR 0315335 A BR0315335 A BR 0315335A BR 0315335 A BR0315335 A BR 0315335A BR 0315335 A BR0315335 A BR 0315335A
- Authority
- BR
- Brazil
- Prior art keywords
- acid
- organic
- cis
- chiral
- isomer
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs 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)
Abstract
"PROCESSO PARA A PREPARAçãO DE (S,S)-CIS-2-BENZIDRIL-3-BENZILAMINOQUINUCLIDINA". A presente invenção refere-se a um processo para preparação de (S,S)-cis-2-benzidril-3-benzilaminoquinuclidina. O processo inclui as etapas de um composto contendo uma mistura de isómeros R e S e tendo a Fórmula (I) em contato com uma quantidade eficaz de um ácido orgânico quiral na presença de um solvente orgânico e de uma quantidade eficaz de um ácido carboxílico orgânico para converter o isómero R em um sal ácido do isómero S, no qual o solvente orgânico e capaz de solubilizar o composto contendo a mistura de isómeros R e S, enquanto precipita o sal ácido e o ácido carboxílico orgânico, é diferente do ácido orgânico quiral; neutralizar o sal ácido com uma base para fornecer um isómero S de uma cetona quiral de Fórmula (II) e reagir a cetona quiral com uma amina orgânica na presença de um ácido de Lewis para fornecer a imina correspondente e reduzir a imina.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US41905102P | 2002-10-16 | 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 (1)
Publication Number | Publication Date |
---|---|
BR0315335A true BR0315335A (pt) | 2005-08-16 |
Family
ID=32108014
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR0315335-5A BR0315335A (pt) | 2002-10-16 | 2003-10-10 | Processo para a preparação de (s,s)-cis-2-benzidril-3-benzilaminoquinuclina |
Country Status (22)
Country | Link |
---|---|
US (2) | US6861526B2 (pt) |
EP (1) | EP1551833A4 (pt) |
JP (1) | JP2006506368A (pt) |
KR (1) | KR100739901B1 (pt) |
CN (1) | CN100418964C (pt) |
AP (1) | AP2005003288A0 (pt) |
AR (1) | AR041587A1 (pt) |
AU (1) | AU2003277353B2 (pt) |
BR (1) | BR0315335A (pt) |
CA (1) | CA2500635A1 (pt) |
EA (1) | EA008192B1 (pt) |
HK (1) | HK1078087A1 (pt) |
HR (1) | HRP20050328A2 (pt) |
IS (1) | IS7755A (pt) |
MX (1) | MXPA05004058A (pt) |
PA (1) | PA8586601A1 (pt) |
PE (1) | PE20040777A1 (pt) |
PL (1) | PL376218A1 (pt) |
TN (1) | TNSN05111A1 (pt) |
UY (1) | UY28024A1 (pt) |
WO (1) | WO2004035575A1 (pt) |
ZA (1) | ZA200502411B (pt) |
Families Citing this family (26)
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 |
LT1713504T (lt) * | 2004-01-30 | 2017-09-11 | Zoetis Services Llc | Antimikrobinis konservantas, skirtas multi-dozinėms kompozicijoms, panaudojant beta-ciklodekstrinus, skirtas skystoms vaisto formoms |
DK1713801T3 (da) * | 2004-02-02 | 2008-03-17 | Pfizer Prod Inc | Fremgangsmåde til fremstilling af 1-(2S,3S)-2-benzhydryl-N-(5-tert-butyl-2-methoxybenzyl)quinuclidin-3-amin |
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 |
NZ619413A (en) | 2006-05-04 | 2015-08-28 | Boehringer Ingelheim Int | Polymorphs of a dpp-iv enzyme inhibitor |
PE20110235A1 (es) | 2006-05-04 | 2011-04-14 | Boehringer Ingelheim Int | Combinaciones farmaceuticas que comprenden linagliptina y metmorfina |
EP1852108A1 (en) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
AR071175A1 (es) | 2008-04-03 | 2010-06-02 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende un inhibidor de la dipeptidil-peptidasa-4 (dpp4) y un farmaco acompanante |
KR20190016601A (ko) | 2008-08-06 | 2019-02-18 | 베링거 인겔하임 인터내셔날 게엠베하 | 메트포르민 요법이 부적합한 환자에서의 당뇨병 치료 |
UY32030A (es) | 2008-08-06 | 2010-03-26 | Boehringer Ingelheim Int | "tratamiento para diabetes en pacientes inapropiados para terapia con metformina" |
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 |
JP2012512848A (ja) | 2008-12-23 | 2012-06-07 | 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 | 有機化合物の塩の形態 |
AR074990A1 (es) | 2009-01-07 | 2011-03-02 | Boehringer Ingelheim Int | Tratamiento de diabetes en pacientes con un control glucemico inadecuado a pesar de la terapia con metformina |
JP2013512229A (ja) | 2009-11-27 | 2013-04-11 | 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 | 遺伝子型が同定された糖尿病患者のリナグリプチン等のddp−iv阻害薬による治療 |
BR112012028136A2 (pt) | 2010-05-05 | 2016-08-09 | Boehringer Ingelheim Int | terapia de combinaçao |
EP3725325B1 (en) | 2010-06-24 | 2023-05-31 | Boehringer Ingelheim International GmbH | Diabetes therapy |
US9034883B2 (en) | 2010-11-15 | 2015-05-19 | Boehringer Ingelheim International Gmbh | Vasoprotective and cardioprotective antidiabetic therapy |
CN103781788B (zh) | 2011-07-15 | 2016-08-17 | 勃林格殷格翰国际有限公司 | 经取代的喹唑啉、其制备及其在药物组合物中的用途 |
US9555001B2 (en) | 2012-03-07 | 2017-01-31 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
EP3685839A1 (en) | 2012-05-14 | 2020-07-29 | Boehringer Ingelheim International GmbH | Linagliptin for use in the treatment of albuminuria and kidney related diseases |
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 |
EP3110449B1 (en) | 2014-02-28 | 2023-06-28 | Boehringer Ingelheim International GmbH | Medical use of a dpp-4 inhibitor |
MX2018015089A (es) | 2016-06-10 | 2019-05-13 | Boehringer Ingelheim Int | Combinacion de linagliptina y metformina. |
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 |
Family Cites Families (14)
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 |
MX18467A (es) | 1988-11-23 | 1993-07-01 | Pfizer | Agentes terapeuticos de quinuclidinas |
US5138060A (en) | 1991-01-03 | 1992-08-11 | Pfizer Inc. | Process and intermediates for preparing azabicyclo(2.2.2)octan-3-imines |
AU658898B2 (en) | 1991-05-22 | 1995-05-04 | Pfizer Inc. | Substituted 3-aminoquinuclidines |
DE122006000066I2 (de) | 1991-05-31 | 2007-12-06 | Pfizer | Chinuclidinderivate |
EP0655996B1 (en) | 1992-08-19 | 2001-11-07 | Pfizer Inc. | Substituted benzylamino nitrogen containing non-aromatic heterocycles |
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 |
US5604241A (en) * | 1992-10-21 | 1997-02-18 | Pfizer Inc. | Substituted benzylaminoquinuclidines as substance P antagonists |
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 |
AU676489B2 (en) * | 1992-11-12 | 1997-03-13 | Pfizer Inc. | 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. |
-
2003
- 2003-10-06 US US10/679,961 patent/US6861526B2/en not_active Expired - Fee Related
- 2003-10-10 AU AU2003277353A patent/AU2003277353B2/en not_active Ceased
- 2003-10-10 EA EA200500650A patent/EA008192B1/ru not_active IP Right Cessation
- 2003-10-10 BR BR0315335-5A patent/BR0315335A/pt not_active IP Right Cessation
- 2003-10-10 JP JP2004544849A patent/JP2006506368A/ja active Pending
- 2003-10-10 MX MXPA05004058A patent/MXPA05004058A/es active IP Right Grant
- 2003-10-10 CN CNB200380101563XA patent/CN100418964C/zh not_active Expired - Fee Related
- 2003-10-10 PL PL03376218A patent/PL376218A1/xx not_active Application Discontinuation
- 2003-10-10 CA CA002500635A patent/CA2500635A1/en not_active Abandoned
- 2003-10-10 AR ARP030103709A patent/AR041587A1/es unknown
- 2003-10-10 AP AP2005003288A patent/AP2005003288A0/xx unknown
- 2003-10-10 KR KR1020057006471A patent/KR100739901B1/ko not_active IP Right Cessation
- 2003-10-10 WO PCT/US2003/032275 patent/WO2004035575A1/en active IP Right Grant
- 2003-10-10 EP EP03808986A patent/EP1551833A4/en not_active Withdrawn
- 2003-10-14 PE PE2003001050A patent/PE20040777A1/es not_active Application Discontinuation
- 2003-10-15 UY UY28024A patent/UY28024A1/es not_active Application Discontinuation
- 2003-10-16 PA PA20038586601A patent/PA8586601A1/es unknown
-
2004
- 2004-10-27 US US10/974,447 patent/US20050085641A1/en not_active Abandoned
-
2005
- 2005-03-17 IS IS7755A patent/IS7755A/is unknown
- 2005-03-23 ZA ZA200502411A patent/ZA200502411B/en unknown
- 2005-04-13 HR HR20050328A patent/HRP20050328A2/xx not_active Application Discontinuation
- 2005-04-15 TN TNP2005000111A patent/TNSN05111A1/en unknown
-
2006
- 2006-01-16 HK HK06100706.9A patent/HK1078087A1/xx not_active IP Right Cessation
Also Published As
Publication number | Publication date |
---|---|
TNSN05111A1 (en) | 2007-05-14 |
KR100739901B1 (ko) | 2007-07-13 |
EA008192B1 (ru) | 2007-04-27 |
IS7755A (is) | 2005-03-17 |
HRP20050328A2 (en) | 2005-06-30 |
EP1551833A1 (en) | 2005-07-13 |
AU2003277353B2 (en) | 2007-08-09 |
EP1551833A4 (en) | 2010-06-02 |
JP2006506368A (ja) | 2006-02-23 |
PA8586601A1 (es) | 2005-02-04 |
WO2004035575A1 (en) | 2004-04-29 |
CA2500635A1 (en) | 2004-04-29 |
AP2005003288A0 (en) | 2005-06-30 |
PE20040777A1 (es) | 2004-11-20 |
ZA200502411B (en) | 2006-05-31 |
UY28024A1 (es) | 2004-05-31 |
CN100418964C (zh) | 2008-09-17 |
KR20050083764A (ko) | 2005-08-26 |
PL376218A1 (en) | 2005-12-27 |
AU2003277353A1 (en) | 2004-05-04 |
US20050085641A1 (en) | 2005-04-21 |
US6861526B2 (en) | 2005-03-01 |
AR041587A1 (es) | 2005-05-26 |
WO2004035575A8 (en) | 2005-05-12 |
EA200500650A1 (ru) | 2005-10-27 |
CN1705664A (zh) | 2005-12-07 |
US20040116704A1 (en) | 2004-06-17 |
MXPA05004058A (es) | 2005-06-08 |
HK1078087A1 (en) | 2006-03-03 |
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Legal Events
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B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE A 7A, 8A ANUIDADE(S). |
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B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: NAO APRESENTADA A GUIA DE CUMPRIMENTO DE EXIGENCIA. REFERENTE AS 7A E 8A ANUIDADES. |