AR036832A1 - Compuestos derivados de himbacina, agonistas receptores de trombina, composiciones farmaceuticas y el uso de dichos compuestos para la preparacion de medicamentos - Google Patents

Compuestos derivados de himbacina, agonistas receptores de trombina, composiciones farmaceuticas y el uso de dichos compuestos para la preparacion de medicamentos

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Publication number
AR036832A1
AR036832A1 ARP020103876A ARP020103876A AR036832A1 AR 036832 A1 AR036832 A1 AR 036832A1 AR P020103876 A ARP020103876 A AR P020103876A AR P020103876 A ARP020103876 A AR P020103876A AR 036832 A1 AR036832 A1 AR 036832A1
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Argentina
Prior art keywords
alkyl
group
aryl
independently selected
cycloalkyl
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ARP020103876A
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English (en)
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Schering Corp
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/06—Antiarrhythmics
    • 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
    • A61P9/10—Drugs 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
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Un compuesto derivado de himbacina representado por la fórmula estructural (1) o una sal farmacéuticamente aceptable de los mismos, en la cual R representa 1 a 3 sustituyentes independientemente seleccionados del grupo que consiste en H, alquilo C1-6, halógeno, hidroxi, amino, alquilo C1-6-amino, dialquilamino C1-6, alcoxi C1-6, -COR16, -COOR17, -SOR16, -SO2R16, -SO2NR17R18, -NR17SO2R18, -NR16COR16a, -NR16COOR16a, -NR16CONR4R5, flúor-alquilo C1-6, diflúor-alquilo C1-6, triflúor-alquilo C1-6, cicloalquilo C3-6, arilo-alquilo C1-6, hidroxi-alquilo C1-6, amino-alquilo C1-6, arilo y tio-alquilo C1-6; R1 y R2 están independientemente seleccionados del grupo que consiste en H, alquilo C1-6, flúor-alquilo C1-6, diflúor -alquilo C1-6, triflúor-alquilo C1-6, cicloalquilo C3-6, alquenilo C2-6, aril-alquilo C1-6, hidroxi-alquilo C1-6, amino-alquilo C1-6, arilo y tio-alquilo C1-6; ó R1 y R2 conjuntamente forman un grupo =O; R3 es H, hidroxi, alcoxi C1-6, ariloxi, aril-alquiloxi C1-6, heteroariloxi, heteroaril-alquiloxi C1-6, cicloalquiloxi C3-6, -SOR16, -SO2R17, -SO2NR18R19, -SR18, -SO3H, -C(O)OR17, -C(O)NR18R19, -OC(O)R32, -OC(O)NR33R34, -(CR33R34)nOR32, -NR4R5, -NR33COOR32, -NR33COR32, -NR33S(O)2R32, -NR33CONR33R34, -NR33S(O)2NR33R34, -(CR33R34)Nnr4r5, -(cr33r34)nNR33COOR32, -(CR33R34)nNR33COR32, -(CR33R34)nNR33S(O)R32, -(CR33R34)nNR33CONR33R34,-(CR33R34)nNR33S(O)2NR33R34, alquilo C1-6, halógeno, cicloalquilo C3-6, alquenilo C2-6, -CN, arilo, heteroarilo, heterocicloalquilo, -P(O)(OR7)2 ó alquilo C1-6 sustituido con 1 a 3 sustituyentes independientemente seleccionados del grupo que consiste en halógeno, -OH, -NH2, arilo, -COOH, -SO3H, tio y alquiltio C1-6; n es 1, 2, 3, ó 4; n1 y n2 son independientemente 0-3, con la condición de que ambos no sean 0; Het es un grupo heteroaromático mono-, bi- ó tricíclico C5-14 que comprende C1-13 y 1 a 4 heteroátomos independientemente seleccionados del grupo que consiste en N, O y S, donde un nitrógeno del anillo puede formar un N-óxido o un grupo cuaternario con un grupo alquilo C1-4, donde Het está adherido a B mediante un miembro de anillo de átomo de carbono y donde el grupo Het está sustituido con 1 a 4 sustituyentes, W, está independientemente seleccionado del grupo que consiste en alquilo C1-6; -NR4R5, -NHCOR26, -NHSO2R16, R21-arilo, arilo donde los átomos de carbono adyacentes forman un anillo con un grupo metilendioxi; y R21-heteroarilo; R4 y R5 están independientemente seleccionados del grupo que consiste en H, alquilo C1-6, fenilo, bencilo, y cicloalquilo C3-6, ó R4 y R5 conjuntamente son -(CH2)3-,-(CH2)4-,-(CH2)5- ó (CH2)2NR7-(CH2)2- y forman un anillo con el nitrógeno al cual están adheridos; R7 es H ó alquilo C1-6; R8, R10 y R11 están independientemente seleccionados del grupo que consiste en R1 y -OR1; R9 es H, OH, -NR4R5, alcoxi C1-6, halógeno o halo-alquilo C1-6; B es -(CH2)n3- ó cis ó trans -(CH2)n4CR12 =CR12a(CH2)n5, donde n3 es 0-5, n4 y n5 son independientemente 0-2, y R12 y R12a están independientemente seleccionados del grupo que consiste en H, alquilo C1-6 y halógeno; R16 y R16a están independientemente seleccionados del grupo que consiste en alquilo C1-6, fenilo y bencilo; R17, R18 y R19 están independientemente seleccionados del grupo que consiste en H, alquilo C1-6, fenilo y bencilo; R21 representa de 1 a 3 sustituyentes independientemente seleccionados del grupo que consiste en H, -CF3, -OCF3, halógeno, -NO2, alquilo C1-6, alcoxi C1-6, -NH2, alquiloC1-6-amino, di-(alquilo C1-6)amino, amino-alquilo C1-6, alquilamino C1-6 alquilo C1-6, di-(alquilo C1-6)-amino-alquilo C1-6, hidroxi-alquilo C1-6, -COOR17, -COR17, -CONR24R25, -NHCOR16, -NHSO2R16, NHSO2CH2CF3, -SO2NR24R25, -NR29C(O)NR24R25, -SO2R30, -P(O)(OR29)2, arilo, arilo-alquilo C1-6, heteroarilo, heterocicloalquilo, y -CR29(=NOR28); R22 es -COR23, -S(O)R31, -S(O)2R31, -SO2NR24R25 ó -COOR27; R23 es halo-alquilo C1-6, alquenilo C2-6, halo-alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquilo C3-7-alquilo C1-6, cicloalquilo C3-7 sustituido con 1 a 3 sustituyentes seleccionados del grupo que consiste en halo, alcoxi C1-3-alquilo C1-3, hidroxi y alcoxi C1-6, arilo, aril-alquilo C2-6, heteroarilo, heterocicloalquilo, alquilo C1-6 sustituido con 1-3 sustituyentes independientemente seleccionados de -COOH y SO3H; ó fórmula (2) donde R35 y R36 están independientemente seleccionados del grupo que consiste en H, alquilo, o alquilo C1-6 sustituido con R37, donde R37 está seleccionado del grupo que consiste en HO-, HS-, -CH2S-, -NH2, fenilo, p-hidroxifenilo e indolilo; R24 y R25 están independientemente seleccionados del grupo que consiste en H, alquilo C1-6, halo-alquilo C1-6, alquenilo C2-6, haloa-alquilo C2-6, alquinilo C2-6, arilo, aril-alquilo C1-6, cicloalquilo C3-7, halo-cicloalquilo C3-7, alcoxi C1-3-alquilo C1-3, hidroxi y alcoxi C1-6; R26 es cicloalquilo C3-7, arilo, aril-alquilo C1-6, heteroarilo, heteroaril-alquilo C1-6 ó alquilamino C1-6; R27 es alquilo C1-6, fenilo, bencilo, alcoxi C1-3-alquilo C1-3, cicloalquilo C3-7, carboxi-alquilo C1-6, sulfo-alquilo C1-6 ó alquilo C1-6 sustituido con NR18R19 y carboxi; R28 es H, alquilo C1-6, fenilo, bencilo ó alcoxi C1-3-alquilo C1-3; R29 y R30 están independientemente seleccionados del grupo que consiste en H, alquilo C1-6; R31 es alquilo C1-6, halo-alquilo C1-6, alquenilo C2-6, halo-alquilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquilo C3-7 sustituido con 1 a 3 sustituyentes seleccionados del grupo que consiste en halo, alcoxi C1-3-alquilo C1-3, hidroxi y alcoxi C1-6; arilo, aril-alquilo C1-6, heteroarilo, heterocicloalquilo, alquilo C1-6 sustituido con 1 a 3 sustituyentes independientemente seleccionados de -COOH y SO3H; ó alcoxi C1-6; R32 es R35-alquilo C1-6, R35-cicloalquilo C3-7, R35-alquenilo C2-6, R35-alquinilo C2-6 ó R35-arilo, donde R35 representa uno o dos sustituyentes independientemente seleccionados del grupo que consiste en H, -COOH, -NH2, -SO3H, =O y =NOR28; y R33 y R34 están independientemente seleccionados del grupo que consiste en H, alquilo C1-6 y cicloalquilo C3-7, así como también composiciones farmacéuticas que los contienen y un método para tratar enfermedades asociadas con trombosis, arteriosclerosis, restenosis, hipertensión, angina pectoris, arritmia, insuficiencia cardíaca y cáncer mediante la administración de dichos compuestos.
ARP020103876A 2001-10-18 2002-10-16 Compuestos derivados de himbacina, agonistas receptores de trombina, composiciones farmaceuticas y el uso de dichos compuestos para la preparacion de medicamentos AR036832A1 (es)

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US (2) US7037920B2 (es)
EP (1) EP1436298B1 (es)
JP (2) JP4307260B2 (es)
KR (1) KR100960170B1 (es)
CN (1) CN100369917C (es)
AR (1) AR036832A1 (es)
AT (1) ATE525378T1 (es)
AU (1) AU2002335031C1 (es)
BR (1) BR0213967A (es)
CA (1) CA2463628A1 (es)
CO (1) CO5570668A2 (es)
EC (1) ECSP045064A (es)
HU (1) HUP0500443A3 (es)
IL (1) IL160918A0 (es)
MX (1) MXPA04003610A (es)
MY (1) MY139335A (es)
NO (1) NO329349B1 (es)
NZ (1) NZ531869A (es)
PE (1) PE20030808A1 (es)
PL (1) PL371948A1 (es)
RU (1) RU2319704C9 (es)
WO (1) WO2003033501A1 (es)
ZA (1) ZA200402849B (es)

Families Citing this family (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6346510B1 (en) 1995-10-23 2002-02-12 The Children's Medical Center Corporation Therapeutic antiangiogenic endostatin compositions
US7488742B2 (en) * 2000-06-15 2009-02-10 Schering Corporation Thrombin receptor antagonists
US7235567B2 (en) * 2000-06-15 2007-06-26 Schering Corporation Crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist
SI2065384T1 (sl) 2002-04-16 2011-05-31 Schering Corp Tricikliäśni trombin receptor antagonist
US7790362B2 (en) * 2003-07-08 2010-09-07 Accumetrics, Inc. Controlled platelet activation to monitor therapy of ADP antagonists
US20070243632A1 (en) * 2003-07-08 2007-10-18 Coller Barry S Methods for measuring platelet reactivity of patients that have received drug eluting stents
JP4558788B2 (ja) * 2004-05-28 2010-10-06 シェーリング コーポレイション トロンビンレセプターアンタゴニストとしての条件付きヒンバシンアナログ
WO2006023844A2 (en) * 2004-08-20 2006-03-02 Entremed, Inc. Compositions and methods comprising proteinase activated receptor antagonists
AU2005294265A1 (en) * 2004-10-06 2006-04-20 University Of Rochester Treatment of pulmonary hypertension using an agent that inhibits a tissue factor pathway
MX2007004197A (es) * 2004-10-08 2007-06-15 Schering Corp Antagonistas del receptor de trombina.
EP1853592B1 (en) * 2005-01-14 2011-03-02 Schering Corporation Synthesis of himbacine analogs
ES2374379T3 (es) * 2005-01-14 2012-02-16 Schering Corporation Síntesis exo y diastereoselectiva de análogos de himbacina.
MX2007008622A (es) * 2005-01-14 2007-09-11 Schering Corp Una sintesis exo-selectiva de analogos de himbacina.
AU2006230292A1 (en) * 2005-03-31 2006-10-05 Schering Corporation Spirocyclic thrombin receptor antagonists
US7595169B2 (en) * 2005-04-27 2009-09-29 Accumetrics, Inc. Method for determining percent platelet aggregation
US20070219154A1 (en) * 2005-12-20 2007-09-20 Suxing Liu Methods for preventing and/or treating a cell proliferative disorder
EP1971336A2 (en) * 2005-12-22 2008-09-24 Shering Corporation Thrombin receptor antagonists as phophylaxis to complications from cardiopulmonary surgery
AU2006331703A1 (en) * 2005-12-22 2007-07-05 Schering Corporation Oxazoloisoquinoline derivatives as thrombin receptor antagonists
WO2007126771A2 (en) * 2006-03-29 2007-11-08 Schering Corporation Monocyclic and bicyclic himbacine derivatives useful as thrombin receptor antagonists
AU2007238756A1 (en) * 2006-04-13 2007-10-25 Schering Corporation Fused ring thrombin receptor antagonists
US8022088B2 (en) * 2006-06-29 2011-09-20 Schering Corporation Substituted bicyclic and tricyclic thrombin receptor antagonists
AR061727A1 (es) * 2006-06-30 2008-09-17 Schering Corp Sintesis de dietil [[ 5- ( 3-fluorofenil) -piridin -2il] metil] fosfonato
TWI367112B (en) 2006-06-30 2012-07-01 Schering Corp Immediate-release tablet formulations of a thrombin receptor antagonist
TWI343262B (en) * 2006-09-26 2011-06-11 Schering Corp Rapidly disintegrating lyophilized oral formulations of a thrombin receptor antagonist
AR063095A1 (es) * 2006-10-04 2008-12-30 Schering Corp Antagonistas del receptor de trombina basados en la unidad triciclica modificada de himbacina
AU2007305269A1 (en) * 2006-10-04 2008-04-10 Schering Corporation Bicyclic and tricyclic derivatives as thrombin receptor antagonists
CA2673228A1 (en) * 2006-12-22 2008-07-03 Schering Corporation Disintegration promoters in solid dose wet granulation formulations
BRPI0809095A2 (pt) * 2007-03-23 2014-09-09 Schering Corp Redução de eventos adversos após intervenção percutânea através de uso de um antagonista de receptor de trombina
WO2008137673A1 (en) * 2007-05-03 2008-11-13 Accumetrics, Inc. Methods of measuring inhibition of platelet aggregation by thrombin receptor antagonists
CN101981034B (zh) 2008-02-05 2013-08-14 赛诺菲-安万特 作为par1抑制剂的三唑并哒嗪、其制备及其制备药物的用途
WO2009143039A2 (en) 2008-05-19 2009-11-26 Schering Corporation Heterocyclic compounds as factor ixa inhibitors
US8575351B2 (en) 2009-06-04 2013-11-05 Merck Sharp & Dohme Corp. Active metabolite of a thrombin receptor antagonist
JP2012529431A (ja) 2009-06-08 2012-11-22 メルク・シャープ・アンド・ドーム・コーポレーション トロンビン受容体アンタゴニストおよびクロピドグレルの固定用量錠剤
TWI393716B (zh) 2009-08-04 2013-04-21 Merck Sharp & Dohme 作為ｉｘａ因子抑制劑之雜環化合物
EP2822557B1 (en) 2012-03-06 2017-08-23 Merck Sharp & Dohme Corp. Preparation and use of bicyclic himbacine derivatives as par-receptor antagonists
US9808473B2 (en) 2013-08-22 2017-11-07 Merck Sharp & Dohme Corp. Preparation and use of 3-pyridyl substituted-6,6-difluoro bicyclic himbacine derivatives as par-1 receptor antagonists
EP3035929B1 (en) 2013-08-22 2024-07-03 Merck Sharp & Dohme LLC 7a-amide substituted-6,6-difluoro bicyclic himbacine derivatives
WO2015026685A1 (en) 2013-08-22 2015-02-26 Merck Sharp & Dohme Corp. 7a-heterocycle substituted- 6, 6-difluoro bicyclic himbacine derivatives
US9969724B2 (en) 2014-04-16 2018-05-15 Merck Sharp & Dohme Corp. Factor IXa inhibitors
CN104610330A (zh) * 2015-02-25 2015-05-13 成都安斯利生物医药有限公司 一种制备(e)-3-丙烯酸乙酯频呐硼酸酯的方法
WO2022018156A1 (en) 2020-07-22 2022-01-27 Janssen Pharmaceutica Nv Compounds useful as factor xia inhibitors
US11845748B2 (en) 2021-03-18 2023-12-19 Janssen Pharmaceutica Nv Bicyclic pyridine N-oxide derivatives useful as a factor XIa inhibitors
US11919881B2 (en) 2021-03-18 2024-03-05 Janssen Pharmaceutica Nv Substituted pyridine N-oxide derivatives useful as a factor XIa inhibitors
US11814364B2 (en) 2021-03-18 2023-11-14 Janssen Pharmaceutica Nv Pyridine N-oxide derivatives useful as factor XIa inhibitors
US11897880B2 (en) 2021-04-30 2024-02-13 Janssen Pharmaceutica Nv 7,8-dihydrobenzo[e]pyrido[3,4-c]azocine-2,5(3H,6H)-dione derivatives useful as a factor XIa inhibitors
US11958856B2 (en) 2021-07-22 2024-04-16 Janssen Pharmaceutica Nv Substituted 1,2,3,8,9,9a-hexahydro-5H-pyrrolo[1,2-a]azepin-5-ones as factor XIa inhibitors

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5716952A (en) * 1992-03-18 1998-02-10 Allergan Method for reducing intraocular pressure in the mammalian eye by administration of muscarinic antagonists
IL106197A (en) 1992-07-30 1999-11-30 Cor Therapeutics Inc Agagonists for the rhombin receptors and pharmaceutical preparations containing them
JP2000229961A (ja) * 1998-12-11 2000-08-22 Sagami Chem Res Center ヒドロナフト［２，３−ｃ］フラン誘導体およびその製造方法
US6063847A (en) * 1997-11-25 2000-05-16 Schering Corporation Thrombin receptor antagonists
DE19801636A1 (de) * 1998-01-17 1999-07-22 Bayer Ag Substituierte bicyclische Lactone
PE20020235A1 (es) 2000-06-15 2002-04-02 Schering Corp Derivados de nor-seco himbacina como antagonistas de los receptores de trombina

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