AR043833A1 - Derivados de 1,2 diazol. metodo de preparacion y composiciones farmaceuticas - Google Patents

Derivados de 1,2 diazol. metodo de preparacion y composiciones farmaceuticas

Info

Publication number
AR043833A1
AR043833A1 ARP040101115A ARP040101115A AR043833A1 AR 043833 A1 AR043833 A1 AR 043833A1 AR P040101115 A ARP040101115 A AR P040101115A AR P040101115 A ARP040101115 A AR P040101115A AR 043833 A1 AR043833 A1 AR 043833A1
Authority
AR
Argentina
Prior art keywords
hal
atoms
coo
derivatives
cona
Prior art date
Application number
ARP040101115A
Other languages
English (en)
Inventor
Mederski Werner Dr
Gleitz Johannes Dr
Tsaklakidis Christos Dr
Cezanne Bertram Dr
Dipl Chem Dorsch Dieter Dr
Original Assignee
Merck Patent Gmbh
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
Priority claimed from DE10315377A external-priority patent/DE10315377A1/de
Priority claimed from DE2003129295 external-priority patent/DE10329295A1/de
Priority claimed from DE10336570A external-priority patent/DE10336570A1/de
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR043833A1 publication Critical patent/AR043833A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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 chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P35/04Antineoplastic agents specific for metastasis
    • 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
    • A61P9/02Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/04Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D453/00Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/06Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing isoquinuclidine ring systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Los compuestos de la fórmula (1) en donde R es H, A, A-CO-, Hal, -C:::C-H, -C:::C-A o -C:::C-C(=O)-A; R1es H, =O, Hal, A, OH, OA, A-COO-, Ph-(CH2)n-COO-, cicloalquil-(CH2)n-COO-, A-CONH-, A-CONA-, Ph-CONA-, N3, NH2, NO2, CN, COOH, COOA, CO-NH2, CONHA, CON(A)2, O-alilo, O-propargilo, O-bencilo, =N-OH, =N-OA o =CF2; Ph es fenilo insustituido o mono, di o trisustituido con A, OA o Hal; R2 es H, Hal o A; R3n es un heterociclo monocíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que puede estar insustituido o mono, di o trisustituido con Hal, A, OA, CN, (CH2)nOH, (CH2)nHal, NR4R5, =NH, =N-OH, =N-OA y/o el O del carbonilo (=O), o CONR4R5; R4, R5 son, de modo independiente entre sí, H o A, R4 y R5 también son juntos una cadena de alquileno con 3, 4 o 5 átomos de C que también puede estar sustituida con A, Hal, OA y/o el O del carbonilo (=CO); A es alquilo no ramificado, ramificado o cíclico con 1-10 átomos de C, donde también 1-7 átomos de H pueden estar reemplazados por F y/o Cl; Hal es F, Cl, Br o I; n es 0, 1, 2, 3, o 4; así como sus derivados, sales, solvatos y estereoisómeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones. Son inhibidores del factor de coagulación Xa y pueden emplearse para la profilaxis y/o la terapia de enfermedades tromboembólicas y para el tratamiento de tumores.
ARP040101115A 2003-04-03 2004-04-02 Derivados de 1,2 diazol. metodo de preparacion y composiciones farmaceuticas AR043833A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE10315377A DE10315377A1 (de) 2003-04-03 2003-04-03 Carbonylverbindungen
DE2003129295 DE10329295A1 (de) 2003-06-30 2003-06-30 Carbonylverbindungen
DE10336570A DE10336570A1 (de) 2003-08-08 2003-08-08 Azaprolinderivate

Publications (1)

Publication Number Publication Date
AR043833A1 true AR043833A1 (es) 2005-08-17

Family

ID=33135448

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP040101115A AR043833A1 (es) 2003-04-03 2004-04-02 Derivados de 1,2 diazol. metodo de preparacion y composiciones farmaceuticas

Country Status (14)

Country Link
US (1) US7557102B2 (es)
EP (1) EP1608645B1 (es)
JP (1) JP4624982B2 (es)
KR (1) KR20050109617A (es)
AR (1) AR043833A1 (es)
AT (1) ATE361296T1 (es)
AU (1) AU2004226281B2 (es)
BR (1) BRPI0408444A (es)
CA (1) CA2520894C (es)
DE (1) DE502004003688D1 (es)
ES (1) ES2285444T3 (es)
MX (1) MXPA05010445A (es)
PL (1) PL377864A1 (es)
WO (1) WO2004087696A1 (es)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10358814A1 (de) * 2003-12-16 2005-07-21 Merck Patent Gmbh Prolinylarylacetamide
DE102004016605A1 (de) * 2004-04-03 2005-10-20 Merck Patent Gmbh Thiocarbamoylproline
CA2627426A1 (en) * 2005-11-11 2007-05-18 Markus Boehringer Carbocyclic fused cyclic amines as inhibitors of the coagulation factor xa
US7601752B2 (en) 2005-11-16 2009-10-13 Hoffmann-La Roche Inc. Pyrrolidine derivatives
US8673920B2 (en) * 2009-05-06 2014-03-18 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2632465B1 (en) 2010-10-27 2015-12-30 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2632464B1 (en) 2010-10-29 2015-04-29 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
AR085698A1 (es) 2011-03-09 2013-10-23 Glaxosmithkline Llc Inhibidores de la peptido desformilasa
WO2013028474A1 (en) 2011-08-19 2013-02-28 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2013039802A1 (en) 2011-09-16 2013-03-21 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2013062892A1 (en) 2011-10-25 2013-05-02 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2013062900A1 (en) 2011-10-25 2013-05-02 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2013066717A1 (en) 2011-10-31 2013-05-10 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2773199B1 (en) 2011-10-31 2019-04-10 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2773351B1 (en) 2011-10-31 2017-08-23 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2013088456A1 (en) 2011-12-15 2013-06-20 Council Of Scientific & Industrial Research A new organocatalytic synthesis of chiral pyrazolidines and their analogues
US9206199B2 (en) 2011-12-16 2015-12-08 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
AR092031A1 (es) 2012-07-26 2015-03-18 Merck Sharp & Dohme Inhibidores del canal de potasio medular externo renal
EP2925322B1 (en) 2012-11-29 2018-10-24 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2934533B1 (en) 2012-12-19 2017-11-15 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
EP2956142B1 (en) 2013-02-18 2017-09-20 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2014150132A1 (en) 2013-03-15 2014-09-25 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel
WO2015017305A1 (en) 2013-07-31 2015-02-05 Merck Sharp & Dohme Corp Inhibitors of the renal outer medullary potassium channel
WO2015065866A1 (en) 2013-10-31 2015-05-07 Merck Sharp & Dohme Corp. Inhibitors of the renal outer medullary potassium channel

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1259485T3 (da) * 2000-02-29 2006-04-10 Millennium Pharm Inc Benzamider og beslægtede inhibitorer for faktor Xa
DE10113402A1 (de) * 2001-03-20 2002-09-26 Merck Patent Gmbh Biurethanderivate
US6821971B2 (en) * 2001-09-20 2004-11-23 The Procter & Gamble Company Fused pyrazolone compounds which inhibit the release of inflammatory cytokines

Also Published As

Publication number Publication date
AU2004226281A1 (en) 2004-10-14
JP2006522038A (ja) 2006-09-28
CA2520894C (en) 2013-02-05
WO2004087696A1 (de) 2004-10-14
EP1608645A1 (de) 2005-12-28
ES2285444T3 (es) 2007-11-16
KR20050109617A (ko) 2005-11-21
PL377864A1 (pl) 2006-02-20
US7557102B2 (en) 2009-07-07
ATE361296T1 (de) 2007-05-15
BRPI0408444A (pt) 2006-04-04
US20060183742A1 (en) 2006-08-17
CA2520894A1 (en) 2004-10-14
MXPA05010445A (es) 2005-11-04
JP4624982B2 (ja) 2011-02-02
EP1608645B1 (de) 2007-05-02
DE502004003688D1 (de) 2007-06-14
AU2004226281B2 (en) 2010-06-10

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