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PE20010290A1 - Pirazinonas sustituidas de arilos y heteroarilos policiclicos utiles para la inhibicion selectiva de la cascada de coagulacion - Google Patents

Pirazinonas sustituidas de arilos y heteroarilos policiclicos utiles para la inhibicion selectiva de la cascada de coagulacion

Info

Publication number
PE20010290A1
PE20010290A1 PE2000000593A PE0005932000A PE20010290A1 PE 20010290 A1 PE20010290 A1 PE 20010290A1 PE 2000000593 A PE2000000593 A PE 2000000593A PE 0005932000 A PE0005932000 A PE 0005932000A PE 20010290 A1 PE20010290 A1 PE 20010290A1
Authority
PE
Peru
Prior art keywords
link
useful
alkyl
pirazinones
coagulation cascade
Prior art date
Application number
PE2000000593A
Other languages
English (en)
Inventor
Wei Huang
Michael S South
Melvin L Rueppel
Darin E Jones
William Neumann
John J Parlow
Brenda Case
Tom Dice
Richard Lindmark
Michael J Hayes
Rick Fenton
Gary W Franklin
Horng-Chih Huang
Carrie Kusturin
Scott A Long
Matthew Mahoney
David Reitz
John Trujillo
Ching-Cheng Wang
Rhonda Wood
Qingping Zeng
Original Assignee
Monsanto 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 Monsanto Co filed Critical Monsanto Co
Publication of PE20010290A1 publication Critical patent/PE20010290A1/es

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    • 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
    • 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/20Nitrogen atoms
    • 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
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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
    • 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
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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 two hetero rings
    • C07D417/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06191Dipeptides containing heteroatoms different from O, S, or N

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

SE REFIERE A PIRAZINONAS SUSTITUIDAS DE ARILOS Y HETEROARILOS POLICICLICOS DE FORMULA I, DONDE: B ES UN GRUPO V; D1, D2, J1, J2 Y K1 SON C, N, O, S Y UN ENLACE CON LA CONDIDICON QUE NO MAS DE UNO ES UN ENLACE, O, S, ENTRE OTRAS CONDICIONES; R9-R13 Y R32-R36 SON ACETAMIDO, HALOACETAMIDO, ENTRE OTROS; R16, R19, R32-R36 SON Qb, NO MAS DE UNO DE R16 Y R19 ES Qb; Qb ES Qbe; B ES TRIALQUILSILILO, ALQUILO C2-C8, ENTRE OTROS; A ES UN ENLACE, (W7)rr-(CH(R15))pa, rr ES 0-1, pa ES 0-6; W7 ES O, S, CO (R7)NC(O), ENTRE OTROS; R7 ES OH, ALQUILO; R15 ES OH, HALO, ALQUILO; ES NH, NOH; R1 ES ALQUILO, ALQUENILO, ENTRE OTROS; R2 ES Z°-Q; Z° ES UN ENLACE, (CR41R42)q; q ES 1-3, ENTRE OTROS; R41 Y R42 SON AMIDINO, HIDROXIAMINO, ENTRE OTROS; Q ES HIDRURO CON LA CONDICION QUE Z° NO ES UN ENLACE, GRUPO II; K ES (CR4aR4b)n, n ES 1-2; R4a Y R4b SON HALO, ENTRE OTROS; E° ES E1, CUANDO K ES (CR4aR4b)n; E1 ES CO, CS, CON(R7), ENTRE OTROS; Y° ES UN GRUPO IV; Qb ES NR20R21, AMINOALQUILENILO, Qbe; Qbe ES NR26CNR25NR23R24, CNR25NR23R24; R20-R26 SON ALQUILO, OH, ENTRE OTROS. UN COMPUESTO PREFERIDO ES 6-[3-AMINOFENIL]-5-CLORO-N-[[4-IMINOMETILFENIL]METIL]-3-[N,N-DIMETILHIDRAZINA-2-OXO-1(2H)-PIRAZINAACETAMIDA, ENTRE OTROS. LOS COMPUESTOS I SON INHIBIDORES DE LAS PROTEASAS DE SERINA Y PUEDEN SER UTILES COMO ANTICOAGULANTE, INHIBIR LA FORMACION DE PLAQUETAS
PE2000000593A 1999-05-19 2000-06-15 Pirazinonas sustituidas de arilos y heteroarilos policiclicos utiles para la inhibicion selectiva de la cascada de coagulacion PE20010290A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US13495899P 1999-05-19 1999-05-19

Publications (1)

Publication Number Publication Date
PE20010290A1 true PE20010290A1 (es) 2001-03-07

Family

ID=22465803

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2000000593A PE20010290A1 (es) 1999-05-19 2000-06-15 Pirazinonas sustituidas de arilos y heteroarilos policiclicos utiles para la inhibicion selectiva de la cascada de coagulacion

Country Status (24)

Country Link
EP (1) EP1202975B1 (es)
JP (1) JP2002544264A (es)
KR (1) KR20010113971A (es)
CN (1) CN1351595A (es)
AR (1) AR029752A1 (es)
AT (1) ATE292629T1 (es)
AU (1) AU775229B2 (es)
BR (1) BR0011295A (es)
CA (1) CA2372617A1 (es)
CZ (1) CZ20014115A3 (es)
DE (1) DE60019296T2 (es)
EA (1) EA005031B1 (es)
ES (1) ES2240100T3 (es)
HU (1) HUP0202191A3 (es)
IL (1) IL146245A0 (es)
MX (1) MXPA01011807A (es)
NO (1) NO20015605L (es)
NZ (1) NZ514876A (es)
PE (1) PE20010290A1 (es)
PL (1) PL352368A1 (es)
SK (1) SK15872001A3 (es)
UY (1) UY26155A1 (es)
WO (1) WO2000069834A1 (es)
ZA (2) ZA200109341B (es)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA58636C2 (uk) 1999-06-04 2003-08-15 Мерк Енд Ко., Інк. Піразинонові інгібітори тромбіну, фармацевтична композиція, спосіб інгібування утворення тромбів у крові, спосіб лікування станів, пов'язаних із тромбоутворенням
AU2044401A (en) 1999-11-23 2001-06-04 Merck & Co., Inc. Pyrazinone thrombin inhibitors
AU2001255399A1 (en) * 2000-04-14 2001-10-30 Corvas International, Inc. Pyridine and pyrazine derivatives as thrombin inhibitors
US6506754B1 (en) * 2000-04-14 2003-01-14 Corvas International, Inc. Non-covalent thrombin inhibitors
US6710058B2 (en) 2000-11-06 2004-03-23 Bristol-Myers Squibb Pharma Company Monocyclic or bicyclic carbocycles and heterocycles as factor Xa inhibitors
US7243153B2 (en) 2001-06-26 2007-07-10 Eastman Kodak Company System and method for managing images over a communication network
CA2462601A1 (en) * 2001-10-03 2003-04-10 Pharmacia Corporation Prodrugs of substituted polycyclic compounds useful for selective inhibition of the coagulation cascade
AU2002367752A1 (en) * 2001-10-03 2003-11-17 Pharmacia Corporation Substituted 5-membered polycyclic compounds useful for selective inhibition of the coagulation cascade
WO2003029224A1 (en) * 2001-10-03 2003-04-10 Pharmacia Corporation 6-membered unsaturated heterocyclic compounds useful for selective inhibition of the coagulation cascade
TW200307667A (en) 2002-05-06 2003-12-16 Bristol Myers Squibb Co Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors
EP1526131A1 (en) * 2003-10-22 2005-04-27 Graffinity Pharmaceuticals Aktiengesellschaft Aminoalkyl-pyrazinones and -pyridones as thrombin inhibitors
US7905872B2 (en) * 2004-06-04 2011-03-15 The Procter & Gamble Company Absorbent articles comprising a slow recovery stretch laminate
US9017305B2 (en) 2010-11-12 2015-04-28 The Procter Gamble Company Elastomeric compositions that resist force loss and disintegration
US11584714B2 (en) 2018-05-29 2023-02-21 Omeros Corporation MASP-2 inhibitors and methods of use
SG11202010925UA (en) 2018-05-29 2020-12-30 Omeros Corp Masp-2 inhibitors and methods of use
KR20220050942A (ko) 2019-08-21 2022-04-25 칼비스타 파마슈티컬즈 리미티드 효소 저해제
AU2020396565C1 (en) * 2019-12-04 2025-05-15 Omeros Corporation MASP-2 inhibitors and methods of use
KR20220110529A (ko) 2019-12-04 2022-08-08 오메로스 코포레이션 Masp-2 억제자 및 사용 방법
WO2021113698A1 (en) 2019-12-04 2021-06-10 Omeros Corporation Masp-2 inhibitors and methods of use
KR20220110530A (ko) 2019-12-04 2022-08-08 오메로스 코포레이션 Masp-2 억제자 및 사용 방법

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EP0835109A4 (en) * 1995-06-27 1999-02-03 Merck & Co Inc PYRIDINONE AS A THROMBINE INHIBITOR
WO1999011267A1 (en) * 1997-09-05 1999-03-11 Merck & Co., Inc. Pyrazinone thrombin inhibitors
AU714985B2 (en) * 1996-04-23 2000-01-13 Merck & Co., Inc. Pyrazinone thrombin inhibitors
CA2283704A1 (en) * 1997-03-24 1998-10-01 Merck & Co., Inc. Thrombin inhibitors
CA2329914A1 (en) * 1998-05-19 1999-11-25 Merck & Co., Inc. Pyrazinone thrombin inhibitors
CA2333040A1 (en) * 1998-05-26 1999-12-02 Merck & Co., Inc. Imidazopyridine thrombin inhibitors
ATE461210T1 (de) * 1998-06-11 2010-04-15 Ortho Mcneil Pharm Inc Pyrazine protease inhibitore

Also Published As

Publication number Publication date
KR20010113971A (ko) 2001-12-28
CN1351595A (zh) 2002-05-29
DE60019296T2 (de) 2006-03-09
EP1202975B1 (en) 2005-04-06
PL352368A1 (en) 2003-08-25
ZA200109341B (en) 2004-05-26
SK15872001A3 (sk) 2002-10-08
HUP0202191A3 (en) 2003-02-28
JP2002544264A (ja) 2002-12-24
EA200101212A1 (ru) 2002-06-27
BR0011295A (pt) 2002-05-28
CA2372617A1 (en) 2000-11-23
ES2240100T3 (es) 2005-10-16
AU4972300A (en) 2000-12-05
ATE292629T1 (de) 2005-04-15
NO20015605L (no) 2002-01-18
NO20015605D0 (no) 2001-11-16
AU775229B2 (en) 2004-07-22
DE60019296D1 (de) 2005-05-12
HUP0202191A2 (hu) 2002-12-28
CZ20014115A3 (cs) 2002-05-15
EA005031B1 (ru) 2004-10-28
NZ514876A (en) 2005-03-24
EP1202975A1 (en) 2002-05-08
WO2000069834A1 (en) 2000-11-23
IL146245A0 (en) 2002-07-25
UY26155A1 (es) 2000-12-29
ZA200400455B (en) 2004-09-29
AR029752A1 (es) 2003-07-16
MXPA01011807A (es) 2003-09-04

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