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

PIRROLIDINAMIDAS SUSTITUIDAS COMO INHIBIDORES DEL FACTOR Xa Y SU PREPARACION

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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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WO2009063028A2 (en) 2007-11-15 2009-05-22 Boehringer Ingelheim International Gmbh Substituted amides, manufacturing and use thereof as medicaments
CN102066321A (zh) 2008-06-16 2011-05-18 弗·哈夫曼-拉罗切有限公司 作为nk2受体拮抗剂的吡咯烷衍生物
EP2475662A2 (en) * 2009-09-11 2012-07-18 Sunovion Pharmaceuticals Inc. Histamine h3 inverse agonists and antagonists and methods of use thereof
MA37756B1 (fr) 2012-06-13 2018-09-28 Hoffmann La Roche Nouveaux composés diazaspirocycloalcane et azaspirocycloalcane
EP3590940B1 (en) 2012-09-25 2021-06-09 F. Hoffmann-La Roche AG Hexahydropyrrolo[3,4-c]pyrrole derivatives and related compounds as autotaxin (atx) inhibitors and as inhibitors of the lysophosphatidic acid (lpa) production for treating e.g. renal diseases
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
MA38982A1 (fr) 2013-11-26 2017-09-29 Hoffmann La Roche Nouvel octahydro-cyclobuta [1,2-c; 3,4-c'] dipyrrol-2-yl
MX2016010675A (es) 2014-03-26 2016-11-10 Hoffmann La Roche Compuestos condensados de [1,4]diazepina como inhibidores de produccion de la autotaxina (atx) y acido lisofosfatidico (lpa).
CN106103446B (zh) 2014-03-26 2019-07-30 豪夫迈·罗氏有限公司 作为自分泌运动因子(atx)和溶血磷脂酸(lpa)生产抑制剂的二环化合物
EP3193609A4 (en) * 2014-09-10 2018-02-28 Epizyme, Inc. Substituted pyrrolidine carboxamide compounds
EP3078378B1 (en) 2015-04-08 2020-06-24 Vaiomer Use of factor xa inhibitors for regulating glycemia
CN108026077B (zh) 2015-09-04 2021-11-05 豪夫迈·罗氏有限公司 苯氧基甲基衍生物
MA42923A (fr) 2015-09-24 2021-04-28 Hoffmann La Roche Composés bicycliques comme inhibiteurs mixtes de atx/ca
WO2017050792A1 (en) 2015-09-24 2017-03-30 F. Hoffmann-La Roche Ag Bicyclic compounds as atx inhibitors
JP6845230B2 (ja) 2015-09-24 2021-03-17 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ デュアルａｔｘ／ｃａ阻害剤としての新規な二環式化合物
MA42918A (fr) 2015-09-24 2018-08-01 Hoffmann La Roche Composés bicycliques utilisés en tant qu'inhibiteurs d'atx
EP3559005A1 (en) 2016-12-21 2019-10-30 Biotheryx Inc. Thienopyrrole derivatives for use in targeting proteins, compositions, methods, and uses thereof
MA49879A (fr) 2017-03-16 2020-06-24 Hoffmann La Roche Composés hétérocycliques utiles en tant qu'inhibiteurs doubles d'atx/ca
CN110382484B (zh) 2017-03-16 2022-12-06 豪夫迈·罗氏有限公司 新的作为atx抑制剂的二环化合物
US20220133740A1 (en) 2019-02-08 2022-05-05 Frequency Therapeutics, Inc. Valproic acid compounds and wnt agonists for treating ear disorders
KR102333564B1 (ko) * 2019-11-28 2021-12-01 동방에프티엘(주) 광학 활성 다이아민 유도체 및 티아졸 유도체의 생산을 위한 새로운 합성경로

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1311501B1 (en) * 2000-08-17 2005-11-02 Eli Lilly And Company Antithrombotic agents
AU2003273179A1 (en) * 2002-05-10 2003-12-12 Bristol-Myers Squibb Company 1,1-disubstituted cycloalkyl derivatives as factor xa inhibitors
EP1572113B1 (en) * 2002-08-26 2017-05-17 Takeda Pharmaceutical Company Limited Calcium receptor modulating compound and use thereof
US7205318B2 (en) * 2003-03-18 2007-04-17 Bristol-Myers Squibb Company Lactam-containing cyclic diamines and derivatives as a factor Xa inhibitors
US20050119266A1 (en) * 2003-10-01 2005-06-02 Yan Shi Pyrrolidine and piperidine derivatives as factor Xa inhibitors
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PE20070171A1 (es) 2005-06-30 2007-03-08 Boehringer Ingelheim Int GLICINAMIDAS SUSTITUIDAS CON EFECTO ANTITROMBOTICO E INHIBIDOR DEL FACTOR Xa
US20070032473A1 (en) 2005-07-19 2007-02-08 Kai Gerlach Substituted amides and their use as medicaments
EP1818330A1 (de) 2006-02-14 2007-08-15 Boehringer Ingelheim Pharma GmbH & Co.KG Substituierte Prolinamide, deren Herstellung und deren Verwendung als Arzneimittel
MY146623A (en) 2006-05-16 2012-09-14 Boehringer Ingelheim Int Substituted prolinamides, manufacturing, and the use thereof as medicaments

Also Published As

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

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