PE20090226A1 - PIRROLIDINAMIDAS SUSTITUIDAS COMO INHIBIDORES DEL FACTOR Xa Y SU PREPARACION - Google Patents

PIRROLIDINAMIDAS SUSTITUIDAS COMO INHIBIDORES DEL FACTOR Xa Y SU PREPARACION

Info

Publication number
PE20090226A1
PE20090226A1 PE2008000536A PE2008000536A PE20090226A1 PE 20090226 A1 PE20090226 A1 PE 20090226A1 PE 2008000536 A PE2008000536 A PE 2008000536A PE 2008000536 A PE2008000536 A PE 2008000536A PE 20090226 A1 PE20090226 A1 PE 20090226A1
Authority
PE
Peru
Prior art keywords
alkyl
chloro
thiofen
pyrrolidin
tetrahydro
Prior art date
Application number
PE2008000536A
Other languages
English (en)
Inventor
Kai Gerlach
Henning Priepke
Wolfgang Wienen
Annette Schuler-Metz
Georg Dahmann
Herbert Nar
Original Assignee
Boehringer Ingelheim Int
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 Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of PE20090226A1 publication Critical patent/PE20090226A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D419/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms
    • C07D419/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

Abstract

REFERIDA A UN COMPUESTO DE PIRROLIDINAMIDA DE FORMULA (I), DONDE D SE SELECCIONA DE (IIa), (IIb) Y (IIc); K1 Y K4 SON CH2, C(O), UN ENLACE, ENTRE OTROS; K2 Y K3 SON CH2, C(O), CHR8a, ENTRE OTROS; R8a ES ALQUILO C1-C5, HIDROXIALQUILO C1-C5, AMINOALQUILO C1-C5, ENTRE OTROS; X ES O, S, CF2, SULFONA, ENTRE OTROS; A1 ES N O CR10; A2 ES N O CR11; A3 ES N O CR12; A5 ES NH, S U O; R10, R11 Y R12 SON H, F, Cl, CF3, ALQUILO C1-C5, ENTRE OTROS; -L-E-G-J- ES -C-C-C-C OPCIONALMENTE SUSTITUIDO CON R4 Y R5; L1 ES C(O); R4 ES ALQUILO C1-C6, ALQUENILO C2-C6, ALQUINILO C2-C6, ENTRE OTROS; R5 ES H, ALQUILO C1-C5, ALQUENILO C2-C5, ALQUINILO C2-C5, ENTRE OTROS; L2 ES C(O); M ES FENILO, PIRIDILO, TIENILO, FURILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: [1-(3-METIL-2,3,4,5-TETRAHIDRO-1H-BENZO[d]AZEPIN-7-CARBONIL)-PIRROLIDIN-3-IL]-AMIDA DE ACIDO 5-CLORO-TIOFEN-2-CLORO-TIOFEN-2-CARBOXILICO, [1-(2-METIL-1,2,3,4-TETRAHIDRO-ISOQUINOLIN-6-CARBONIL)-PIRROLIDIN-3-IL]-AMIDA DEL ACIDO 5-CLORO-TIOFEN-2-CARBOXILICO, [4-HIDROXI-1-(2-METIL-1,2,3,4-TETRAHIDRO-ISOQUINOLIN-6-CARBONIL)-PIRROLIDIN-3-IL]-AMIDA DEL ACIDO (3SR,4SR)-5-CLORO-TIOFEN-2-CARBOXILICO, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DEL FACTOR Xa Y SON UTILES EN EL TRATAMIENTO DE ENFERMEDADES TROMBOTICAS VENOSAS Y ARTERIALES
PE2008000536A 2007-03-27 2008-03-25 PIRROLIDINAMIDAS SUSTITUIDAS COMO INHIBIDORES DEL FACTOR Xa Y SU PREPARACION PE20090226A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP07105053A EP1975165A1 (de) 2007-03-27 2007-03-27 Substituierte Pyrrolidinamide, deren Herstellung und deren Verwendung als Arzneimittel

Publications (1)

Publication Number Publication Date
PE20090226A1 true PE20090226A1 (es) 2009-04-02

Family

ID=38599360

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2008000536A PE20090226A1 (es) 2007-03-27 2008-03-25 PIRROLIDINAMIDAS SUSTITUIDAS COMO INHIBIDORES DEL FACTOR Xa Y SU PREPARACION

Country Status (10)

Country Link
US (1) US8309542B2 (es)
EP (2) EP1975165A1 (es)
JP (1) JP5397959B2 (es)
AR (1) AR065852A1 (es)
CA (1) CA2682012A1 (es)
CL (1) CL2008000873A1 (es)
PE (1) PE20090226A1 (es)
TW (1) TW200902022A (es)
UY (1) UY30979A1 (es)
WO (1) WO2008116881A1 (es)

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US8741890B2 (en) * 2007-11-15 2014-06-03 Boehringer Ingelheim International Gmbh Substituted amides, manufacturing and use thereof as medicaments
WO2009153179A1 (en) * 2008-06-16 2009-12-23 F. Hoffmann-La Roche Ag Pyrrolidine derivatives as nk2 receptor antagonists
CA2772525A1 (en) * 2009-09-11 2011-03-17 Sunovion Pharmaceuticals Inc. Histamine h3 inverse agonists and antagonists and methods of use thereof
EA201492223A1 (ru) 2012-06-13 2015-03-31 Ф. Хоффманн-Ля Рош Аг Новые диазаспироциклоалканы и азаспироциклоалканы
CN104684915B (zh) 2012-09-25 2017-10-31 霍夫曼-拉罗奇有限公司 新型双环衍生物
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
PE20160845A1 (es) 2013-11-26 2016-09-10 Hoffmann La Roche Nuevo octahidro-ciclobuta[1,2-c;3,4-c']dipirrol-2-ilo
DK3122750T3 (da) 2014-03-26 2019-11-04 Hoffmann La Roche Bicykliske forbindelser som autotaxin (ATX)- og lysofosfatidsyre (LPA)-produktionshæmmere
JP6554481B2 (ja) 2014-03-26 2019-07-31 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ オートタキシン（ａｔｘ）及びリゾホスファチジン酸（ｌｐａ）産生の阻害剤としての縮合［１，４］ジアゼピン化合物
AU2015315177A1 (en) * 2014-09-10 2017-03-16 Epizyme, Inc. Substituted pyrrolidine carboxamide compounds
EP3078378B1 (en) 2015-04-08 2020-06-24 Vaiomer Use of factor xa inhibitors for regulating glycemia
KR20180043837A (ko) 2015-09-04 2018-04-30 에프. 호프만-라 로슈 아게 페녹시메틸 유도체
RU2018114289A (ru) 2015-09-24 2019-10-24 Ф. Хоффманн-Ля Рош Аг Бициклические соединения в качестве ингибиторов аутотаксина (atx)
CR20180057A (es) 2015-09-24 2018-04-02 Hoffmann La Roche Nuevos compuestos biciclicos como inhibidores duales de atx/ca.
KR20180053408A (ko) 2015-09-24 2018-05-21 에프. 호프만-라 로슈 아게 이중 오토탁신(atx)/탄산 무수화효소(ca) 억제제로서의 신규한 이환형 화합물
CN107922412B (zh) 2015-09-24 2021-02-23 豪夫迈·罗氏有限公司 作为atx抑制剂的二环化合物
CN110099907A (zh) 2016-12-21 2019-08-06 拜欧赛里克斯公司 靶向蛋白质的噻吩并吡咯衍生物、组合物、方法及其用途
WO2018167001A1 (en) 2017-03-16 2018-09-20 F. Hoffmann-La Roche Ag Heterocyclic compounds useful as dual atx/ca inhibitors
WO2018167113A1 (en) 2017-03-16 2018-09-20 F. Hoffmann-La Roche Ag New bicyclic compounds as atx inhibitors
JP2022520671A (ja) 2019-02-08 2022-03-31 フリークエンシー・セラピューティクス・インコーポレイテッド 耳障害を治療するためのバルプロ酸化合物及びｗｎｔ作動薬
KR102333564B1 (ko) * 2019-11-28 2021-12-01 동방에프티엘(주) 광학 활성 다이아민 유도체 및 티아졸 유도체의 생산을 위한 새로운 합성경로

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Also Published As

Publication number Publication date
US20100099664A1 (en) 2010-04-22
UY30979A1 (es) 2008-10-31
TW200902022A (en) 2009-01-16
US8309542B2 (en) 2012-11-13
CL2008000873A1 (es) 2009-03-27
JP2010522713A (ja) 2010-07-08
EP2132193A1 (de) 2009-12-16
JP5397959B2 (ja) 2014-01-22
CA2682012A1 (en) 2008-10-02
EP1975165A1 (de) 2008-10-01
WO2008116881A1 (de) 2008-10-02
AR065852A1 (es) 2009-07-08
EP2132193B1 (de) 2012-10-24

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