ZA200508889B - Pyrrolidino-1,2-dicarboxy-1-(phenylamide)-2-(4-(3-oxomorpholino-4-yl)-phenylamide) derivatives and related compounds for use as inhibitors of coagulation factor Xa in the treatment of thrombo-embolic diseases - Google Patents

Pyrrolidino-1,2-dicarboxy-1-(phenylamide)-2-(4-(3-oxomorpholino-4-yl)-phenylamide) derivatives and related compounds for use as inhibitors of coagulation factor Xa in the treatment of thrombo-embolic diseases

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Publication number
ZA200508889B
ZA200508889B ZA200508889A ZA200508889A ZA200508889B ZA 200508889 B ZA200508889 B ZA 200508889B ZA 200508889 A ZA200508889 A ZA 200508889A ZA 200508889 A ZA200508889 A ZA 200508889A ZA 200508889 B ZA200508889 B ZA 200508889B
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South Africa
Prior art keywords
phenylamide
oxomorpholino
thrombo
dicarboxy
pyrrolidino
Prior art date
Application number
ZA200508889A
Inventor
Tsaklakidis Christos
Mederski Werner
Gleitz Johannes
Dorsch Dieter
Cezanne Bertram
Original Assignee
Merck Patent Gmbh
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Filing date
Publication date
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of ZA200508889B publication Critical patent/ZA200508889B/en

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    • 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
    • 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
    • A61P9/10Drugs 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
    • 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
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/301,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • C07D265/321,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms
    • 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • 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
    • C07D405/12Heterocyclic 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 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
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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

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  • 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)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
ZA200508889A 2003-04-03 2005-11-02 Pyrrolidino-1,2-dicarboxy-1-(phenylamide)-2-(4-(3-oxomorpholino-4-yl)-phenylamide) derivatives and related compounds for use as inhibitors of coagulation factor Xa in the treatment of thrombo-embolic diseases ZA200508889B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10315377A DE10315377A1 (en) 2003-04-03 2003-04-03 New carbonyl-substituted carbocyclic or heterocyclic compounds, are factor Xa and factor VIIa inhibitors useful e.g. for treating thrombosis, myocardial infarction, arteriosclerosis, inflammation or tumors

Publications (1)

Publication Number Publication Date
ZA200508889B true ZA200508889B (en) 2007-02-28

Family

ID=32981039

Family Applications (3)

Application Number Title Priority Date Filing Date
ZA200508891A ZA200508891B (en) 2003-04-03 2005-11-02 Pyrazolidine-1,2-dicarboxyldiphenylamide derivatives as coagulation factor Xa inhibitors for the treatment of thromboses
ZA200508889A ZA200508889B (en) 2003-04-03 2005-11-02 Pyrrolidino-1,2-dicarboxy-1-(phenylamide)-2-(4-(3-oxomorpholino-4-yl)-phenylamide) derivatives and related compounds for use as inhibitors of coagulation factor Xa in the treatment of thrombo-embolic diseases
ZA200508888A ZA200508888B (en) 2003-04-03 2005-11-02 Methods for the production of pyrrolidine-1,2-dicarboxylic acid-1-(phenyl(-amide))-2-(phenyl(-amide)) derivatives and 1-(phenylcarbamoyl)-pyrrolidine-2-carboxylic acid derivatives as intermediate products

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ZA200508891A ZA200508891B (en) 2003-04-03 2005-11-02 Pyrazolidine-1,2-dicarboxyldiphenylamide derivatives as coagulation factor Xa inhibitors for the treatment of thromboses

Family Applications After (1)

Application Number Title Priority Date Filing Date
ZA200508888A ZA200508888B (en) 2003-04-03 2005-11-02 Methods for the production of pyrrolidine-1,2-dicarboxylic acid-1-(phenyl(-amide))-2-(phenyl(-amide)) derivatives and 1-(phenylcarbamoyl)-pyrrolidine-2-carboxylic acid derivatives as intermediate products

Country Status (4)

Country Link
CN (3) CN1771237A (en)
DE (1) DE10315377A1 (en)
UA (1) UA85676C2 (en)
ZA (3) ZA200508891B (en)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102004045796A1 (en) * 2004-09-22 2006-03-23 Merck Patent Gmbh Medicaments containing carbonyl compounds and their use
US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
US8987242B2 (en) 2008-12-05 2015-03-24 Merck Sharp & Dohme Corp. Morpholinone compounds as factor IXA inhibitors
TW201033184A (en) 2008-12-05 2010-09-16 Mochida Pharm Co Ltd Morpholinone compounds as factor IXa inhibitors
JP2013503163A (en) * 2009-08-31 2013-01-31 持田製薬株式会社 Morpholinone compounds as factor IXa inhibitors
US8802868B2 (en) 2010-03-25 2014-08-12 Vertex Pharmaceuticals Incorporated Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide
MX342288B (en) 2010-04-22 2016-09-23 Vertex Pharma Process of producing cycloalkylcarboxamido-indole compounds.
CA2881566A1 (en) * 2012-07-19 2014-01-23 Yohei Ikuma 1-(cycloalkyl-carbonyl)proline derivative
AU2014378428A1 (en) * 2014-01-14 2016-09-01 Sumitomo Dainippon Pharma Co., Ltd. Condensed 5-oxazolidinone derivative
CN104974148B (en) * 2014-04-14 2017-11-24 北大方正集团有限公司 The method of one kind synthesis ketone of 4 { 4 [base of 1,3 oxazolidine of (5S) 5 (amino methyl) 2 oxo 3] phenyl } morpholine 3
ES2957761T3 (en) 2014-04-15 2024-01-25 Vertex Pharma Pharmaceutical compositions for the treatment of diseases mediated by the cystic fibrosis transmembrane conductance regulator
CN104098497B (en) * 2014-06-17 2016-04-13 王庚禹 A kind of new amides
TWI734702B (en) * 2015-10-01 2021-08-01 美商百歐克斯製藥公司 Human plasma kallikrein inhibitors
CN110240591A (en) * 2018-03-08 2019-09-17 天津药物研究院有限公司 Proline derivative and its preparation method and application
CN115974856B (en) * 2022-12-28 2023-08-11 北京康立生医药技术开发有限公司 Preparation method of drug valmotustat for treating adult T-cell leukemia lymphoma

Also Published As

Publication number Publication date
ZA200508891B (en) 2007-03-28
CN1771237A (en) 2006-05-10
CN1771249A (en) 2006-05-10
ZA200508888B (en) 2007-02-28
UA85676C2 (en) 2009-02-25
CN1771248A (en) 2006-05-10
DE10315377A1 (en) 2004-10-14

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