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PE20081775A1 - Compuestos macrociclicos como inhibidores del factor viia - Google Patents

Compuestos macrociclicos como inhibidores del factor viia

Info

Publication number
PE20081775A1
PE20081775A1 PE2007001814A PE2007001814A PE20081775A1 PE 20081775 A1 PE20081775 A1 PE 20081775A1 PE 2007001814 A PE2007001814 A PE 2007001814A PE 2007001814 A PE2007001814 A PE 2007001814A PE 20081775 A1 PE20081775 A1 PE 20081775A1
Authority
PE
Peru
Prior art keywords
alkyl
phenyl
ring
compounds
factor viia
Prior art date
Application number
PE2007001814A
Other languages
English (en)
Inventor
Nicholas Ronald Wurtz
Eldon Scott Priestley
Daniel L Cheney
Peter W Glunz
Xiaojun Zhang
Vladimir Ladziata
Brandon Parkhurst
Original Assignee
Bristol Myers Squibb Co
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 Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of PE20081775A1 publication Critical patent/PE20081775A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D271/00Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/12Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D255/00Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00
    • C07D255/04Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00 condensed with carbocyclic rings or ring systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

SE REFIERE A COMPUESTOS MACROCICLICOS DE FORMULA (I) DONDE EL ANILLO A ES FENILO O PIRIDILO; EL ANILLO B ES FENILO O PIRIDILO; Z1 Y Z2 SON CADA UNO C O N; Z3 ES -C(=O)-, -C(=NH)-, -SO2-, ENTRE OTROS; Z4 ES C(O), CR20R20 O SO2, DONDE R20 ES H, CF3, HALOALQUILO(C1-C4), ENTRE OTROS; EL ANILLO D ES FENILO O UN HETEROARILO DE 5 A 6 MIEMBROS; M ES -CONH-, -SO2NH-, -NHCO- O -NHSO2-; L ES -XC(R12R13)-, C(R12R13)Y-, -XC(R12R13)Y-, ENTRE OTROS, DONDE X ES O, S(O)p O NR16; Y ES O U NR16a, EN DONDE R16 Y R16a SON CADA UNO H, ALQUILO(C1-C6), CICLOALQUILO(C3-C6), FENILO, ENTRE OTROS; p ES DE 0 A 2; R12 Y R13 SON CADA UNO H, F, CF3, CN, NO2, ENTRE OTROS; R1 ES H, F, Br, ALQUENILO(C2-C4), ENTRE OTROS; R2 ES H, F, I, FLUOROALQUILO(C1-C4), ENTRE OTROS; R3 ES H, F, ALQUILO(C1-C6), ALQUINILO(C2-C4), ENTRE OTROS; R4 ES H, F, Cl, Br, I O ALQUILO(C1-C4); R5 ES H, ALQUILO(C1-C6), ALQUENILO(C2-C4), ENTRE OTROS; R6 ES H, ALQUILO(C1-C6), ALQUINILO(C2-C4), ENTRE OTROS; R7 ES H O ALQUILO(C1-C6); R8 ES H, F, CN, CH2F, ENTRE OTROS; R9, R10 Y R11 SON CADA UNO H, F, Cl, Br, I, ALQUILO(C1-C4) O ALCOXI(C1-C4); W ES O, S O NRh, DONDE Rh ES H O ALQUILO(C1-C3). SON COMPUESTOS PREFERIDOS: SAL DEL ACIDO (R)-4-METIL-2-(3-OXO-2,3-DIHIDRO-1H-ISOINDOL-5-ILAMINO)-7-(PROPANO-2-SULFONIL)-4,11-DIAZA-TRICICLO[14.2.2.16,10]HENICOSA-1(19),6,8,10(21),16(20),17-HEXAENO-3,12-DIONA TRIFLUOROACETICO, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES SELECTIVOS DEL FACTOR VIIa
PE2007001814A 2006-12-20 2007-12-14 Compuestos macrociclicos como inhibidores del factor viia PE20081775A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US87086406P 2006-12-20 2006-12-20
US98446007P 2007-11-01 2007-11-01

Publications (1)

Publication Number Publication Date
PE20081775A1 true PE20081775A1 (es) 2008-12-18

Family

ID=39430763

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2007001814A PE20081775A1 (es) 2006-12-20 2007-12-14 Compuestos macrociclicos como inhibidores del factor viia

Country Status (12)

Country Link
US (1) US8420830B2 (es)
EP (1) EP2102176A2 (es)
JP (1) JP2010514681A (es)
AR (1) AR064471A1 (es)
AU (1) AU2007337025A1 (es)
CA (1) CA2673598A1 (es)
CL (1) CL2007003718A1 (es)
MX (1) MX2009006689A (es)
NO (1) NO20092279L (es)
PE (1) PE20081775A1 (es)
TW (1) TW200836735A (es)
WO (1) WO2008079836A2 (es)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101631784A (zh) 2006-12-20 2010-01-20 百时美施贵宝公司 用作抗凝血药的二环内酰胺凝血因子viia抑制剂
US20110137042A1 (en) * 2009-12-08 2011-06-09 Boehringer Ingelheim International Gmbh Process for Synthesis of Intermediates Useful for Making Substituted Indazole and Azaindazole Compounds
WO2011100401A1 (en) 2010-02-11 2011-08-18 Bristol-Myers Squibb Company Macrocycles as factor xia inhibitors
CN102993065B (zh) * 2011-09-13 2015-07-29 中国科学院上海药物研究所 含手性叔丁基亚磺酰基的α-芳基氨基酸酯类化合物、其制备方法及用途
EP2766346B1 (en) 2011-10-14 2017-03-29 Bristol-Myers Squibb Company Substituted tetrahydroisoquinoline compounds as factor xia inhibitors
EP2797879B1 (en) * 2011-12-27 2018-12-26 Bio-Pharm Solutions Co., Ltd. Phenyl carbamate compounds for use in alleviating or treating pain and neuropathic pain
EP2858977A1 (en) 2012-06-08 2015-04-15 Bristol-Myers Squibb Company Macrocyclic factor viia inhibitors
BR112015002081A2 (pt) * 2012-08-03 2017-07-04 Bristol Myers Squibb Co di-hidropiridona p1 como inibidores de fator xia
SMT201700003T1 (it) * 2012-08-03 2017-03-08 Bristol Myers Squibb Co DlIDROPIRIDONI COME INIBITORI DEL FATTORE XIA
EP2906552B1 (en) 2012-10-12 2017-11-22 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
US9920034B2 (en) 2012-10-12 2018-03-20 Bristol-Myers Squibb Company Crystalline forms of a factor XIa inhibitor
US9403774B2 (en) 2012-10-12 2016-08-02 Bristol-Myers Squibb Company Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
ES2712699T3 (es) 2013-03-25 2019-05-14 Bristol Myers Squibb Co Tetrahidroisoquinolinas que contienen azoles sustituidos como inhibidores del factor XIa
US9657006B2 (en) 2013-06-13 2017-05-23 Bristol-Myers Squibb Company Macrocyclic factor VIIa inhibitors
WO2015116885A1 (en) 2014-01-31 2015-08-06 Bristol-Myers Squibb Company Macrocycles with aromatic p2' groups as factor xia inhibitors
NO2760821T3 (es) 2014-01-31 2018-03-10
ES2714283T3 (es) 2014-09-04 2019-05-28 Bristol Myers Squibb Co Macrociclos de diamida que son inhibidores de FXIa
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
EP3072943B1 (en) 2015-03-26 2018-05-02 Idemitsu Kosan Co., Ltd. Dibenzofuran/carbazole-substituted benzonitriles
JP6816103B2 (ja) * 2015-07-29 2021-01-20 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company 非芳香族性P2’基を担持する新規大員環の第XIa因子阻害剤

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0028489B1 (en) 1979-11-05 1983-10-05 Beecham Group Plc Enzyme derivatives, and their preparation
US5023236A (en) 1988-04-07 1991-06-11 Corvas, Inc. Factor VII/VIIA active site inhibitors
US5843442A (en) 1990-10-22 1998-12-01 Corvas International, Inc. Blood coagulation protein antagonists and uses therefor
US5866542A (en) 1994-10-18 1999-02-02 Corvas International, Inc. Nematode-extracted anticoagulant protein
PE121699A1 (es) 1997-02-18 1999-12-08 Boehringer Ingelheim Pharma Heterociclos biciclicos disustituidos como inhibidores de la trombina
ZA985247B (en) 1997-06-19 1999-12-17 Du Pont Merck Pharma Guanidine mimics as factor Xa inhibitors.
CA2383008A1 (en) 1999-06-14 2000-12-21 Amanda Jane Lyons Compounds
DE19962924A1 (de) 1999-12-24 2001-07-05 Bayer Ag Substituierte Oxazolidinone und ihre Verwendung
HUP0400651A2 (hu) * 2000-11-07 2004-06-28 Bristol-Myers Squibb Company Szerin proteáz inhibitorokként alkalmazható savszármazékok és ezeket tartalmazó gyógyszerkészítmények
AR035216A1 (es) 2000-12-01 2004-05-05 Astrazeneca Ab Derivados de acido mandelico ,derivados farmaceuticamente aceptables, uso de estos derivados para la fabricacion de medicamentos, metodos de tratamiento ,procesos para la preparacion de estos derivados, y compuestos intermediarios
AU2002322802A1 (en) * 2001-07-27 2003-02-17 Merck And Co., Inc. Thrombin inhibitors
EP1427415B1 (en) 2001-09-21 2009-08-12 Brystol-Myers Squibb Company Lactam-containing compounds and derivatives thereof as factor xa inhibitors
WO2004072101A2 (en) * 2003-02-11 2004-08-26 Bristol-Myers Squibb Company Phenylglycine derivatives useful as serine protease inhibitors
JP2006517589A (ja) * 2003-02-11 2006-07-27 ブリストル−マイヤーズ スクイブ カンパニー セリンプロテアーゼ・インヒビターとして有用なベンゼンアセトアミド化合物
EP1856096B1 (en) * 2005-01-10 2010-09-01 Bristol-Myers Squibb Company Phenylglycinamide derivatives useful as anticoagulants
EP1866822A4 (en) * 2005-03-03 2010-09-01 Burnham Inst Medical Research SCREENING PROCEDURE FOR PROTEIN KINASE B INHIBITORS USING VIRTUAL DOCKING APPARATUS AND COMPOSITIONS AND COMPOSITIONS DISCOVERED THEREFOR
US7456195B2 (en) * 2005-06-24 2008-11-25 Bristol-Myers Squibb Company Phenylglycinamide and pyridylglycinamide derivatives useful as anticoagulants
AR058380A1 (es) * 2005-12-23 2008-01-30 Bristol Myers Squibb Co Inhibidores del factor viia macrociclicos utiles como anticoagulantes
US8044242B2 (en) 2006-03-09 2011-10-25 Bristol-Myers Squibb Company 2-(aryloxy) acetamide factor VIIa inhibitors useful as anticoagulants
CN101631784A (zh) 2006-12-20 2010-01-20 百时美施贵宝公司 用作抗凝血药的二环内酰胺凝血因子viia抑制剂

Also Published As

Publication number Publication date
AR064471A1 (es) 2009-04-01
WO2008079836A4 (en) 2009-03-12
US8420830B2 (en) 2013-04-16
US20100113488A1 (en) 2010-05-06
EP2102176A2 (en) 2009-09-23
NO20092279L (no) 2009-08-31
WO2008079836A2 (en) 2008-07-03
JP2010514681A (ja) 2010-05-06
MX2009006689A (es) 2009-06-30
AU2007337025A1 (en) 2008-07-03
CA2673598A1 (en) 2008-07-03
CL2007003718A1 (es) 2008-07-11
TW200836735A (en) 2008-09-16
WO2008079836A3 (en) 2009-01-15

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