AR048326A1 - Derivados de prolinilo - Google Patents

Derivados de prolinilo

Info

Publication number
AR048326A1
AR048326A1 ARP050101135A ARP050101135A AR048326A1 AR 048326 A1 AR048326 A1 AR 048326A1 AR P050101135 A ARP050101135 A AR P050101135A AR P050101135 A ARP050101135 A AR P050101135A AR 048326 A1 AR048326 A1 AR 048326A1
Authority
AR
Argentina
Prior art keywords
hal
coo
derivatives
nr5r5
cona
Prior art date
Application number
ARP050101135A
Other languages
English (en)
Inventor
Werner Mederski
Christos Tsaklakidis
Dieter Dorsch
Bertram Cezanne
Johannes Gleitz
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
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR048326A1 publication Critical patent/AR048326A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D207/12Oxygen or sulfur atoms
    • 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • 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
    • 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
    • A61P9/08Vasodilators 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
    • 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

Landscapes

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

Abstract

Compuestos de la formula (1) en donde R es Hal, -C:::C-H, -C:::C-A u OA, R1 es 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, CONH2, CONHA, CON(A)2, O-alilo, O- propargilo, O-bencilo, =N-OH, =N-OA o =CF2; R2 es H o A; Ph es fenilo insustituido o mono, di o trisustituido con A, OA, OH o Hal, R3 es H, Hal o A, R4 es -C6H4-(CH2)n-NR5R5', -C(=NR5)NR5R5', o como se muestra en los restos de formulas (2); R5, R5' son en cada caso, de modo independiente entre sí, H o A, A es alquilo no ramificado, ramificado o cíclico con C1-12, en 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 o 3, así como sus derivados, solvatos, sales y estereoisomeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones, son inhibidores del factor de coagulacion Xa y se pueden emplear para la prevencion y/o la terapia de enfermedades tromboembolicas y para el tratamiento de tumores.
ARP050101135A 2004-03-26 2005-03-23 Derivados de prolinilo AR048326A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102004014945A DE102004014945A1 (de) 2004-03-26 2004-03-26 Prolinylderivate

Publications (1)

Publication Number Publication Date
AR048326A1 true AR048326A1 (es) 2006-04-19

Family

ID=34961159

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050101135A AR048326A1 (es) 2004-03-26 2005-03-23 Derivados de prolinilo

Country Status (14)

Country Link
US (1) US7683093B2 (es)
EP (1) EP1735279A1 (es)
JP (1) JP2007530469A (es)
KR (1) KR20070010131A (es)
CN (1) CN1938269A (es)
AR (1) AR048326A1 (es)
AU (1) AU2005225489B2 (es)
BR (1) BRPI0509174A (es)
CA (1) CA2561057A1 (es)
DE (1) DE102004014945A1 (es)
MX (1) MXPA06010771A (es)
RU (1) RU2006137656A (es)
WO (1) WO2005092849A1 (es)
ZA (1) ZA200608875B (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2004246766B2 (en) * 2003-06-18 2009-09-17 Merck Patent Gmbh Pyrrolidin-1, 2- dicarboxylic acid- 1- [(4- ethinyl- phenyl) - amid]- 2- [(phenyl)- amid] derivative as inhibitors of coagulation factor Xa and VIIa for the treatment of thrombosis
DE10358814A1 (de) * 2003-12-16 2005-07-21 Merck Patent Gmbh Prolinylarylacetamide
EP1818330A1 (de) * 2006-02-14 2007-08-15 Boehringer Ingelheim Pharma GmbH & Co.KG Substituierte Prolinamide, deren Herstellung und deren Verwendung als Arzneimittel
BRPI0711648A2 (pt) 2006-05-16 2011-11-29 Boehringer Ingelheim Int prolinamidas substituìdas, fabricação e uso das mesmas como medicamentos
AR067336A1 (es) * 2007-06-28 2009-10-07 Novartis Ag Moduladores de calicreina 7
AR106241A1 (es) * 2015-10-01 2017-12-27 Biocryst Pharm Inc Inhibidores de calicreína plasmática humana
CN110240591A (zh) * 2018-03-08 2019-09-17 天津药物研究院有限公司 脯氨酸衍生物及其制备方法和用途

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TR199800157T1 (xx) * 1995-07-31 1998-06-22 Shionogi & Co.,Ltd. Fosfolipaz A2 inhibit�r� aktivitesi olan pirolidin t�revleri.
US6673817B1 (en) 1999-05-24 2004-01-06 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
JP2003500390A (ja) * 1999-05-24 2003-01-07 シーオーアール セラピューティクス インコーポレイテッド Xa因子阻害剤
US7312235B2 (en) * 2001-03-30 2007-12-25 Millennium Pharmaceuticals, Inc. Benzamide inhibitors of factor Xa
US7030141B2 (en) 2001-11-29 2006-04-18 Christopher Franklin Bigge Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade

Also Published As

Publication number Publication date
WO2005092849A1 (de) 2005-10-06
JP2007530469A (ja) 2007-11-01
EP1735279A1 (de) 2006-12-27
AU2005225489A1 (en) 2005-10-06
CA2561057A1 (en) 2005-10-06
BRPI0509174A (pt) 2007-09-18
AU2005225489B2 (en) 2011-02-10
RU2006137656A (ru) 2008-05-10
MXPA06010771A (es) 2006-12-15
DE102004014945A1 (de) 2005-10-13
US20070135507A1 (en) 2007-06-14
CN1938269A (zh) 2007-03-28
ZA200608875B (en) 2008-06-25
KR20070010131A (ko) 2007-01-22
US7683093B2 (en) 2010-03-23

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