[go: up one dir, main page]

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)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (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)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (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
JP2010513562A (ja) 2006-12-20 2010-04-30 ブリストル−マイヤーズ スクイブ カンパニー 抗凝血剤として有用な二環状ラクタム第viia因子阻害剤
AU2010328480A1 (en) * 2009-12-08 2012-05-17 Boehringer Ingelheim International Gmbh Process for synthesis of intermediates useful for making substituted indazole and azaindazole compounds
TWI520965B (zh) 2010-02-11 2016-02-11 必治妥美雅史谷比公司 作為因子xia抑制劑之巨環類
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
AR088456A1 (es) 2011-10-14 2014-06-11 Bristol Myers Squibb Co Compuestos de tetrahidroisoquinolina sustituidos como inhibidores del factor xia
WO2013100566A1 (en) * 2011-12-27 2013-07-04 Bio-Pharm Solutions Co., Ltd. Phenyl alkyl carbamate derivative compound and pharmaceutical composition containing the same
WO2013184734A1 (en) 2012-06-08 2013-12-12 Bristol-Myers Squibb Company Macrocyclic factor viia inhibitors
SI2880026T1 (sl) 2012-08-03 2017-04-26 Bristol-Myers Squibb Company Dihidropiridon p1 kot faktor xia inhibitorjev
MX361370B (es) * 2012-08-03 2018-12-05 Bristol Myers Squibb Co Dihidropiridona p1 como inhibidores del factor xia.
WO2014059214A1 (en) 2012-10-12 2014-04-17 Bristol-Myers Squibb Company Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
US9315519B2 (en) 2012-10-12 2016-04-19 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor XIa inhibitors
SI2906551T1 (en) 2012-10-12 2018-05-31 Bristol-Myers Squibb Company Crystalline forms of a factor xia inhibitor
JP6479763B2 (ja) 2013-03-25 2019-03-06 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company 第xia因子阻害剤としての置換アゾール含有のテトラヒドロイソキノリン
EP3008052A1 (en) 2013-06-13 2016-04-20 Bristol-Myers Squibb Company Macrocyclic factor viia inhibitors
NO2760821T3 (es) 2014-01-31 2018-03-10
WO2015116885A1 (en) 2014-01-31 2015-08-06 Bristol-Myers Squibb Company Macrocycles with aromatic p2' groups as factor xia inhibitors
WO2016036893A1 (en) 2014-09-04 2016-03-10 Bristol-Myers Squibb Company Diamide macrocycles that are fxia inhibitors
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
US10676477B2 (en) * 2015-07-29 2020-06-09 Bristol-Myers Squibb Company Factor XIa macrocycle inhibitors bearing a non-aromatic P2' group

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3065190D1 (en) 1979-11-05 1983-11-10 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.
WO2000077027A2 (en) 1999-06-14 2000-12-21 Tularik Limited Serine protease inhibitors
DE19962924A1 (de) 1999-12-24 2001-07-05 Bayer Ag Substituierte Oxazolidinone und ihre Verwendung
US6642252B2 (en) 2000-11-07 2003-11-04 Bristol-Myers Squibb Company Acid derivatives useful as serine protease inhibitors
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
WO2003011222A2 (en) * 2001-07-27 2003-02-13 Merck & 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
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
US7122559B2 (en) 2003-02-11 2006-10-17 Bristol-Myers Squibb Company Phenylglycine derivatives useful as serine protease inhibitors
DE602006016566D1 (de) 2005-01-10 2010-10-14 Bristol Myers Squibb Co Als antikoagulanzien verwendbare phenylglycinamid-derivate
US20090131474A1 (en) * 2005-03-03 2009-05-21 Martino Forino Screening methods for protein kinase b inhibitors employing virtual docking approaches and compounds and compositions discovered thereby
US7456195B2 (en) 2005-06-24 2008-11-25 Bristol-Myers Squibb Company Phenylglycinamide and pyridylglycinamide derivatives useful as anticoagulants
PE20071132A1 (es) 2005-12-23 2007-12-14 Bristol Myers Squibb Co Compuestos macrociclicos como inhibidores del factor viia
US8044242B2 (en) 2006-03-09 2011-10-25 Bristol-Myers Squibb Company 2-(aryloxy) acetamide factor VIIa inhibitors useful as anticoagulants
JP2010513562A (ja) 2006-12-20 2010-04-30 ブリストル−マイヤーズ スクイブ カンパニー 抗凝血剤として有用な二環状ラクタム第viia因子阻害剤

Also Published As

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

Similar Documents

Publication Publication Date Title
PE20081775A1 (es) Compuestos macrociclicos como inhibidores del factor viia
CO5611147A2 (es) Derivados de nicotinamida utiles como inhibidores p38
HRP20090151T3 (en) Indozolone derivatives as 11b-hsd1 inhibitors
PE20070189A1 (es) COMPUESTO DE AMINO-5-HETEROARILO (5 MIEMBROS) IMIDAZOLONA Y SU USO PARA MODULACION DE LA ß-SECRETASA
AR056536A1 (es) Compuestos de 2-amino-5- [4-(difluormetoxi)fenil]-5-fenilimidazolona como inhibidores de la beta secretasa (bace)
AR041250A1 (es) Derivados de sulfonamida como inhibidores de enzimas convertidoras de tnf-alfa
RS53682B1 (en) PIRAZINONE DERIVATIVES AND THEIR USE IN THE TREATMENT OF LUNG DISEASE
AR038703A1 (es) Derivados de 5-feniltiazol y uso como inhibidor de quinasa p i 3
RS52545B (en) INHIBITORI PROTEIN APOPTOZE (IAP)
AR066107A1 (es) Derivados de triazolopiridin - carboxamidas y triazolopirimidin-carboxamidas, su preparacion y su aplicacion en terapeutica como inhibidores de la enzimamonoacil glicerol lipasa y composiciones qu los contienen.
RS53588B1 (en) COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS
PE20080318A1 (es) Derivados de diceto-piperazina y piperidina como agentes antivirales
ES2572155T3 (es) Compuestos insecticidas
PE20091974A1 (es) Derivados de indazoles sustituidos con fenil o piridinilo
PE20110835A1 (es) Piridiloxi-indoles inhibidores del vegf-r2 y uso de los mismos para el tratamiento de enfermedades
ES2530943T3 (es) Derivados de la cromenona con actividad antitumoral
PE20080906A1 (es) Derivados heteroarilo como inhibidores de citocina
RS51556B (en) 5,7-DIAMINOPYRAZOLO (4,3-D) PYRIMIDINE WITH PDE-5 INHIBITOR
AR062074A1 (es) Derivados de alcoholes 1-fenil-2-piridinil alquilenicos como inhibidores de fosfodiesterasa
NO20064326L (no) Aryl- og heteroarylpiperidinkarboksylatderivater, deres fremstilling og anvendelse derav i form av FAAH enzyminhibitorer
PE20080277A1 (es) Derivados de azaindol espirociclicos y sustituidos
PE20100737A1 (es) Nuevos compuestos
PE20080608A1 (es) Compuestos quimicos
SE0201937D0 (sv) Therapeutic agents
RS50968B (sr) Derivati 4-fenil-5-okso-1,4,5,6,7,8-heksahidrohinolina kao medikamenti u lečenju neplodnosti

Legal Events

Date Code Title Description
FC Refusal