WO2002008177A3 - N-substituierte-1-amino-1,1-dialkylcarbonsäurederivate - Google Patents

N-substituierte-1-amino-1,1-dialkylcarbonsäurederivate Download PDF

Info

Publication number
WO2002008177A3
WO2002008177A3 PCT/EP2001/007596 EP0107596W WO0208177A3 WO 2002008177 A3 WO2002008177 A3 WO 2002008177A3 EP 0107596 W EP0107596 W EP 0107596W WO 0208177 A3 WO0208177 A3 WO 0208177A3
Authority
WO
WIPO (PCT)
Prior art keywords
amino
substituted
acid derivatives
dialkylcarboxylic acid
tumour
Prior art date
Application number
PCT/EP2001/007596
Other languages
English (en)
French (fr)
Other versions
WO2002008177A2 (de
WO2002008177A8 (de
Inventor
Horst Juraszyk
Dieter Dorsch
Werner Mederski
Christos Tsaklakidis
Christopher Barnes
Johannes Gleitz
Original Assignee
Merck Patent Gmbh
Horst Juraszyk
Dieter Dorsch
Werner Mederski
Christos Tsaklakidis
Christopher Barnes
Johannes Gleitz
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 to BR0112771-3A priority Critical patent/BR0112771A/pt
Application filed by Merck Patent Gmbh, Horst Juraszyk, Dieter Dorsch, Werner Mederski, Christos Tsaklakidis, Christopher Barnes, Johannes Gleitz filed Critical Merck Patent Gmbh
Priority to CA002418173A priority patent/CA2418173A1/en
Priority to SK151-2003A priority patent/SK1512003A3/sk
Priority to MXPA03000664A priority patent/MXPA03000664A/es
Priority to JP2002514086A priority patent/JP2004504375A/ja
Priority to AU2001293697A priority patent/AU2001293697A1/en
Priority to PL01358585A priority patent/PL358585A1/xx
Priority to HU0302948A priority patent/HUP0302948A2/hu
Priority to EP01974078A priority patent/EP1303482A2/de
Publication of WO2002008177A2 publication Critical patent/WO2002008177A2/de
Publication of WO2002008177A8 publication Critical patent/WO2002008177A8/de
Publication of WO2002008177A3 publication Critical patent/WO2002008177A3/de
Priority to NO20030375A priority patent/NO20030375L/no

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40—Acylated substituent nitrogen atom
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • A61P9/10—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
    • C07C311/46—Y being a hydrogen or a carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • C07D211/66—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4 having a hetero atom as the second substituent in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings 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
    • C07D309/14—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D335/00—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom
    • C07D335/02—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Neue Verbindungen der Formel (I) worin R?1, R2, R2', R2', R3, R4, R5, R5', R5', R5''', R''''¿, X, Y, U, V und W die in Patentanspruch 1 angegebene Bedeutung haben, sind Inhibitoren des Koagulationsfaktors Xa und VIIa und können zur Behandlung von Thrombosen, myocardialem Infarkt, Arteriosklerose, Entzündungen, Apoplexie, Angina pectoris, Restenose nach Angioplastie, Claudicatio intermittens, Tumoren, Tumorerkrankungen und/oder Tumor-metastasen eingesetzt werden.
PCT/EP2001/007596 2000-07-25 2001-07-03 N-substituierte-1-amino-1,1-dialkylcarbonsäurederivate WO2002008177A2 (de)

Priority Applications (10)

Application Number Priority Date Filing Date Title
AU2001293697A AU2001293697A1 (en) 2000-07-25 2001-07-03 N-substituted-1-amino-1,1-dialkylcarboxylic acid derivatives
CA002418173A CA2418173A1 (en) 2000-07-25 2001-07-03 N-substituted-1-amino-1,1-dialkylcarboxylic acid derivatives
SK151-2003A SK1512003A3 (en) 2000-07-25 2001-07-03 N-substituted-1-amino-1,1-dialkylcarboxylic acid derivatives
MXPA03000664A MXPA03000664A (es) 2000-07-25 2001-07-03 Derivados n-sustituidos del acido 1-amino-1, 1-dialquilcarboxilico.
JP2002514086A JP2004504375A (ja) 2000-07-25 2001-07-03 Ｎ置換１−アミノ−１，１−ジアルキルカルボン酸誘導体
BR0112771-3A BR0112771A (pt) 2000-07-25 2001-07-03 Derivados de ácido 1-amino-1,1-dialquil-carboxilico n-substituìdo
PL01358585A PL358585A1 (en) 2000-07-25 2001-07-03 N-substituted-1-amino-1,1-dialkylcarboxylic acid derivatives
HU0302948A HUP0302948A2 (hu) 2000-07-25 2001-07-03 N-szubsztituált 1-amino-1,1-dialkil-karbonsav-származékok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények
EP01974078A EP1303482A2 (de) 2000-07-25 2001-07-03 N-substituierte-1-amino-1,1-dialkylcarbonsäurederivate
NO20030375A NO20030375L (no) 2000-07-25 2003-01-24 N-substituerte 1-amino-1,1-dialkylkarboksylsyrederivater

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10036121A DE10036121A1 (de) 2000-07-25 2000-07-25 N-Substituierte-1-amino-1,1-dialkyl-carbonsäurederivate
DE10036121.8 2000-07-25

Publications (3)

Publication Number Publication Date
WO2002008177A2 WO2002008177A2 (de) 2002-01-31
WO2002008177A8 WO2002008177A8 (de) 2002-04-18
WO2002008177A3 true WO2002008177A3 (de) 2002-07-25

Family

ID=7650099

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2001/007596 WO2002008177A2 (de) 2000-07-25 2001-07-03 N-substituierte-1-amino-1,1-dialkylcarbonsäurederivate

Country Status (18)

Country Link
US (1) US20030162814A1 (de)
EP (1) EP1303482A2 (de)
JP (1) JP2004504375A (de)
KR (1) KR20030022163A (de)
CN (1) CN1443160A (de)
AR (1) AR029980A1 (de)
AU (1) AU2001293697A1 (de)
BR (1) BR0112771A (de)
CA (1) CA2418173A1 (de)
CZ (1) CZ2003338A3 (de)
DE (1) DE10036121A1 (de)
HU (1) HUP0302948A2 (de)
MX (1) MXPA03000664A (de)
NO (1) NO20030375L (de)
PL (1) PL358585A1 (de)
SK (1) SK1512003A3 (de)
WO (1) WO2002008177A2 (de)
ZA (1) ZA200301471B (de)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10110325A1 (de) * 2001-03-03 2002-09-05 Merck Patent Gmbh Phenylderivate 2
US7030141B2 (en) 2001-11-29 2006-04-18 Christopher Franklin Bigge Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
AR038377A1 (es) 2002-02-08 2005-01-12 Merck & Co Inc Derivados de n-bifenil-aminocicloalcancarboxamida (con sustitucion con metilo)
ATE316954T1 (de) * 2002-02-08 2006-02-15 Merck & Co Inc N-biphenylmethylaminocycloalkancarboxamid- derivative
BR0314219A (pt) * 2002-09-11 2005-07-19 Warner Lambert Co Inibidores do fator xa e outras serina proteases envolvidas na cascata da coagulação
WO2009007015A1 (en) * 2007-07-10 2009-01-15 Sanofi-Aventis Malonamide derivatives with antithrombotic activity

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1020434A1 (de) * 1997-08-27 2000-07-19 Kissei Pharmaceutical Co., Ltd. 3-amidinoanilin-derivate, inhibitoren des aktivierten blutgerinnungsfaktors x und zwischenpodukte zur herstellung beider

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU180240B (en) * 1978-04-21 1983-02-28 Gyogyszerkutato Intezet Process for producing new,substituted 1,3-diaryl-2-iminoimidasolidines and 2-imino-hexahydro-pyrimidines
US4310429A (en) * 1978-06-19 1982-01-12 The B. F. Goodrich Company Stabilized polymers, novel stabilizers, and synthesis thereof

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1020434A1 (de) * 1997-08-27 2000-07-19 Kissei Pharmaceutical Co., Ltd. 3-amidinoanilin-derivate, inhibitoren des aktivierten blutgerinnungsfaktors x und zwischenpodukte zur herstellung beider

Non-Patent Citations (10)

* Cited by examiner, † Cited by third party
Title
A. KJŸR: "Cyclodehydration of aclyated alpha-amino acid amides. I. Saturated amides", ACTA CHEMICA SCANDINAVICA, vol. 7, no. 6, 1953, Munksgaard, Copenhagen, DK, pages 889 - 899, XP002193955, ISSN: 0904-213X *
A.M. KNOWLES, ET AL.: "The formation of 4-imidazolidinones from 2-phenyloxazolonium perchlorate and Schiff bases", TETRAHEDRON LETTERS, no. 6, February 1971 (1971-02-01), Elsevier Science Publishers, Amsterdam, NL, pages 485 - 488, XP002193951, ISSN: 0040-4039 *
B. BUCHHOLZ, ET AL.: "Aziridnes, 61. Ring opening of 2,2-dimethyl-1-sulphonylaziridines by anilines: regioselectivity and revised structure of main products", ZEITSCHRIFT FUR NATURFORSCHUNG, TEIL B: ANORGANISCHE CHEMIE, ORGANISCHE CHEMIE, vol. 48, no. 4, April 1993 (1993-04-01), Verlag der Zeitschrift Für Naturforschung, Tubingen, DE, pages 483 - 487, XP002193952, ISSN: 0932-0776 *
D.P. DEL'TSOVA, ET AL.: "Fluorine-containing imines. Communication 4. Synthesis and properties of hexafluoroacetone N-perfluoropivaloylimine", BULLETIN OF THE ACADEMY OF SCIENCES OF THE USSR, DIVISION OF CHEMICAL SCIENCE, vol. 33, no. 12, Teil 1, December 1984 (1984-12-01), Consultants Bureau, New York, US, pages 2504 - 2508, XP002193954, ISSN: 0568-5230 *
D.ST.C. BLACK, ET AL.: "Double ring-opening of bicyclic oxaziridines to N-(3-oxopropyl)amides by iron(II) sulphate", ANGEWANDTE CHEMIE, INTERNATIONAL EDITION IN ENGLISH, vol. 20, no. 8, 1981, Verlag Chemie, Weinheim, DE, pages 669 - 670, XP002193957, ISSN: 0570-0833 *
E. STRACK, ET AL.: "Zur Darstellung der Diamino-butane, I. Meteil.: d,l-1.2-Diamino-butan; 1.2-Diamino-2-methyl-propan (d,l-1.2-Diamino-propan)", BERICHTE DER DEUTSCHEN CHEMISCHEN GESELLSCHAFT, vol. 66, 1933, Verlag Chemie, Weinheim, DE, pages 1330 - 1333, XP002193956 *
J. BARLUENGA, ET AL.: "Regiospecific one-pot synthesis of substituted 1,2-alkanediamines, 2-aminoalkyl thioethers, and 2-aminoalkanethiols via aminomercuration-demercuration of allylamines and allyl sulphides", SYNTHESIS, no. 3, March 1981 (1981-03-01), Georg Thieme Verlag, Stuttgart, DE, pages 201 - 204, XP002193949, ISSN: 0039-7881 *
J.T. LAI: "Hindered amines. Synthesis of hindered acyclic alpha-aminoacetamides", JOURNAL OF ORGANIC CHEMISTRY, vol. 45, no. 18, 29 August 1980 (1980-08-29), American Chemical Society, Washington, DC, US, pages 3671 - 3673, XP002193948, ISSN: 0022-3263 *
L.B. CLAPP: "Reactions of ethylenimines: with ammonia and amines", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, vol. 48, no. 1, January 1948 (1948-01-01), American Chemical Society, Washington, DC, US, pages 184 - 186, XP002193950, ISSN: 0002-7863 *
M. PROST, ET AL.: "Amino-3 hydroxy-4' butyrophénones", CHIMICA THERAPEUTICA, vol. 5, no. 5, September 1970 (1970-09-01), Société d'Etudes de Chimie Thérapeutique, FR, pages 303 - 311, XP002193953, ISSN: 0223-5234 *

Also Published As

Publication number Publication date
MXPA03000664A (es) 2003-06-06
JP2004504375A (ja) 2004-02-12
WO2002008177A2 (de) 2002-01-31
NO20030375D0 (no) 2003-01-24
AR029980A1 (es) 2003-07-23
US20030162814A1 (en) 2003-08-28
CA2418173A1 (en) 2003-01-23
NO20030375L (no) 2003-01-24
HUP0302948A2 (hu) 2003-12-29
BR0112771A (pt) 2003-06-24
ZA200301471B (en) 2004-06-29
CZ2003338A3 (cs) 2003-05-14
WO2002008177A8 (de) 2002-04-18
DE10036121A1 (de) 2002-02-07
KR20030022163A (ko) 2003-03-15
CN1443160A (zh) 2003-09-17
EP1303482A2 (de) 2003-04-23
PL358585A1 (en) 2004-08-09
SK1512003A3 (en) 2003-07-01
AU2001293697A1 (en) 2002-02-05

Similar Documents

Publication Publication Date Title
TR200402535T4 (tr) Serin proteaz inhibitörleri.
CY1107149T1 (el) Νεα παραγωγα αμιδινοβενζυλαμινης και χρηση τους ως αναστολεων θρομβινης
CY1113487T1 (el) Νεα παραγωγα μανδελικου οξεος και η χρηση τους ως αναστολεις θροβινης
AU2001274220A1 (en) Serine protease inhibitors
MXPA05013536A (es) Derivados de etinilprolina.
CA2294059A1 (en) New amidino derivatives and their use as thrombin inhibitors
TR200201168T2 (tr) CGRP-Antagonistleri-yeni siklopropanlar içeren ilaçlar ve üretim yöntemleri.
WO2000071516A3 (en) INHIBITORS OF FACTOR Xa
TR199802536T2 (xx) Yeni amino asit t�revleri,trombin inhibit�rleri olarak kullan�lmalar�.
CA2312431A1 (en) New compounds
WO2002037937A3 (en) Acid derivatives useful as serine protease inhibitors
WO2002008177A3 (de) N-substituierte-1-amino-1,1-dialkylcarbonsäurederivate
TR200201128T2 (tr) PDE4 inhibitörleri olarak tetrahidrotiyopiranfitalazinon türevleri.
IS5966A (is) Nýjar amídínóafleiður og notkun þeirra sem þrombínhemlar
MXPA03010205A (es) Derivados de acido oxalico.
SI1377574T1 (de)
MXPA04004307A (es) Derivados de fenoxi-n-`4-(1,1-dioxoisotiazolidin-2-il)fenil-valeramida y otros compuestos como inhibidores del factor de coagulacion xa para el tratamiento de enfermedades tromboembolicas y tumores.
WO2002006280A3 (en) INHIBITORS OF FACTOR Xa
MXPA04001121A (es) Derivados de fenilo.
DE60224805D1 (de) 1-glycinyl-4-(1-methylpiperidin-4-yl)piperazine un
NO20030431L (no) Acetamidderivater og anvendelse derav som inhibitorer for koagulasjonsfaktorene Xa og VIIa
BR0112777A (pt) Derivados de uretano
TR200001365T2 (tr) Yeni heterosiklik ikame edilmiş a-hidroksikarbonik asit türevleri
ES2184633A1 (es) Procedimiento para la preparacion de derivados de 4-(imidazol-1-il) bencenosulfonamida.
BR9913140A (pt) Derivados 2-oxo-2h-quinolina

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ PL PT RO RU SD SE SG SI SK SL TJ TM TR TT TZ UA UG US UZ VN YU ZA ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE TR BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
121 Ep: the epo has been informed by wipo that ep was designated in this application
AK Designated states

Kind code of ref document: C1

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ PL PT RO RU SD SE SG SI SK SL TJ TM TR TT TZ UA UG US UZ VN YU ZA ZW

AL Designated countries for regional patents

Kind code of ref document: C1

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE TR BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

CFP Corrected version of a pamphlet front page
CR1 Correction of entry in section i
WWE Wipo information: entry into national phase

Ref document number: 2001974078

Country of ref document: EP

WWE Wipo information: entry into national phase

Ref document number: 1020027017764

Country of ref document: KR

WWE Wipo information: entry into national phase

Ref document number: 018131816

Country of ref document: CN

WWE Wipo information: entry into national phase

Ref document number: PA/a/2003/000664

Country of ref document: MX

WWE Wipo information: entry into national phase

Ref document number: 2001293697

Country of ref document: AU

Ref document number: 10333633

Country of ref document: US

Ref document number: 2418173

Country of ref document: CA

WWE Wipo information: entry into national phase

Ref document number: PV2003-338

Country of ref document: CZ

WWE Wipo information: entry into national phase

Ref document number: 1512003

Country of ref document: SK

WWE Wipo information: entry into national phase

Ref document number: 1200300148

Country of ref document: VN

WWE Wipo information: entry into national phase

Ref document number: 215/KOLNP/2003

Country of ref document: IN

WWE Wipo information: entry into national phase

Ref document number: 2003/01471

Country of ref document: ZA

Ref document number: 200301471

Country of ref document: ZA

ENP Entry into the national phase

Ref document number: 2003104790

Country of ref document: RU

Kind code of ref document: A

Ref country code: RU

Ref document number: RU A

WWP Wipo information: published in national office

Ref document number: 1020027017764

Country of ref document: KR

WWP Wipo information: published in national office

Ref document number: 2001974078

Country of ref document: EP

REG Reference to national code

Ref country code: DE

Ref legal event code: 8642

WWP Wipo information: published in national office

Ref document number: PV2003-338

Country of ref document: CZ

WWW Wipo information: withdrawn in national office

Ref document number: 2001974078

Country of ref document: EP

WWR Wipo information: refused in national office

Ref document number: PV2003-338

Country of ref document: CZ