HUP0004353A2 - Benzamidin-származékok, eljárás előállításukra és az ezeket tartalmazó gyógyszerkészítmények - Google Patents

Benzamidin-származékok, eljárás előállításukra és az ezeket tartalmazó gyógyszerkészítmények

Info

Publication number
HUP0004353A2
HUP0004353A2 HU0004353A HUP0004353A HUP0004353A2 HU P0004353 A2 HUP0004353 A2 HU P0004353A2 HU 0004353 A HU0004353 A HU 0004353A HU P0004353 A HUP0004353 A HU P0004353A HU P0004353 A2 HUP0004353 A2 HU P0004353A2
Authority
HU
Hungary
Prior art keywords
group
coor5
con
formula
cor5
Prior art date
Application number
HU0004353A
Other languages
English (en)
Inventor
Soheila Anzali
Sabine Bernotat-Danielowski
Hans-Peter Buchstaller
Dieter Dorsch
Joachim Gante
Horst Juraszyk
Werner Mederski
Guido Melzer
Hanns Wurziger
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 HUP0004353A2 publication Critical patent/HUP0004353A2/hu
Publication of HUP0004353A3 publication Critical patent/HUP0004353A3/hu

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D263/18—Oxygen atoms
    • C07D263/20—Oxygen atoms attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • C07C257/00—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
    • C07C257/10—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
    • C07C257/18—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to carbon atoms of six-membered aromatic rings
    • 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
    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/03—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C311/05—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms to acyclic carbon atoms of hydrocarbon radicals substituted by nitrogen atoms, not being part of nitro or nitroso groups
    • 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
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C07C311/18—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms, not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/22—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with hetero atoms directly attached to ring nitrogen atoms
    • C07D295/26—Sulfur atoms
    • 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
    • C07D413/10—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 carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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 three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

A találmány szerinti antitrombotikus és antikoaguláris hatásúvegyületek (I) általános képletében R1 jelentése -C(=NH)-NH2, amelyadott esetben egy -COA, -CO-[C(R5)2]m-Ar, -COOA, -OH képletűcsoporttal vagy szokásos amino védőcsoporttal szubsztituálva lehet,valamint (a) vagy (b) képletű csoport, R2 jelentése H, A, OR5, N(R5)2,NO2, CN, Hal, NR5COA, NHCOAr, NHSO2A, NHSO2Ar, COOR5, CON(R5)2,CONHAr, COR5, COAr, S(O)nA vagy S(O)nAr, R3 jelentése R5 vagy -[C(R5)2]m-COOR5, vagy R3 és X jelentése együtt -CO-N-, amely öttagúgyűrűt képez, ahol R3 jelentése -C=O, és X jelentése N, R4 jelentéseA, cikloalkilcsoport, -[C(R5)2]mAr, -[C(R5)2]mHet vagy -CR5=CR5-Ar, R5jelentése H, A vagy benzilcsoport, X jelentése O, NR5 vagy CH2, Yjelentése O, NR5, N[C(R5)2]m-Ar, N[C(R5)2]m-Het, N[C(R5)2]m-COOR5,(c), (d) vagy (e) képletű csoport, N[C(R5)2]m-CON(R5)2, N[C(R5)2]m-CONR5Ar vagy N[C(R5)2]m-CONAr2, W jelentése közvetlen kötés, -SO2-, -CO-, -COO- vagy -CONR5-, A jelentése 1-20 szénatomos alkilcsoport,ahol egy vagy kettő CH2 csoport helyett oxigénatom vagy kénatom vagy -CR5=CR5- csoport állhat és/vagy 1-7 hidrogénatom helyett fluoratomállhat, Ar jelentése adott esetben szubsztituált fenilcsoport vagynaftilcsoport, Ar' jelentése szubsztituálatlan vagy egy, kettő vagyhárom R1, A,OR5, N(R5)2, NO2, CN, Hal, NHCOA, COOR5, CON(R5)2, COR5vagy S(O)nA csoporttal szubsztituált fenilcsoport vagy naftilcsoport,Het jelentése egy- vagy kétmagvú, adott esetben szubsztituált telítettvagy telítetlen heterociklusos gyűrűrendszer, amely egy, kettő, háromvagy négy azonos, vagy különböző heteroatomként nitrogénatomot,oxigénatomot vagy kénatomot tartalmaz, m értéke 0, 1, 2, 3 vagy 4, nértéke 0, 1 vagy 2. A találmány kiterjed a fenti vegyületekelőállítására, ezeket tartalmazó gyógyszerkészítményekre és avegyületek alkalmazására. Ó
HU0004353A 1997-12-12 1998-11-27 Benzamine derivatives, process for producing them and ph HUP0004353A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19755268A DE19755268A1 (de) 1997-12-12 1997-12-12 Benzamidinderivate
PCT/EP1998/007673 WO1999031092A1 (de) 1997-12-12 1998-11-27 Benzamidinderivate als koagulationsfaktor-xa-hemmer

Publications (2)

Publication Number Publication Date
HUP0004353A2 true HUP0004353A2 (hu) 2002-03-28
HUP0004353A3 HUP0004353A3 (en) 2002-04-29

Family

ID=7851688

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0004353A HUP0004353A3 (en) 1997-12-12 1998-11-27 Benzamine derivatives, process for producing them and ph

Country Status (16)

Country Link
EP (1) EP1056743A1 (hu)
JP (1) JP2002508370A (hu)
KR (1) KR20010032963A (hu)
CN (1) CN1281451A (hu)
AR (1) AR017844A1 (hu)
AU (1) AU744002B2 (hu)
BR (1) BR9813477A (hu)
CA (1) CA2313651A1 (hu)
DE (1) DE19755268A1 (hu)
HU (1) HUP0004353A3 (hu)
NO (1) NO20002958L (hu)
PL (1) PL341008A1 (hu)
RU (1) RU2203897C2 (hu)
SK (1) SK8572000A3 (hu)
WO (1) WO1999031092A1 (hu)
ZA (1) ZA9811339B (hu)

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DE10027024A1 (de) * 2000-05-31 2001-12-06 Merck Patent Gmbh Carbaminsäureester
AR028948A1 (es) 2000-06-20 2003-05-28 Astrazeneca Ab Compuestos novedosos
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DE10105989A1 (de) * 2001-02-09 2002-08-14 Bayer Ag Substituierte Oxazolidinone und ihre Verwendung
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GB0107228D0 (en) 2001-03-22 2001-05-16 Astrazeneca Ab Chemical compounds
SE0101038D0 (sv) 2001-03-23 2001-03-23 Astrazeneca Ab Novel compounds
DE10129725A1 (de) 2001-06-20 2003-01-02 Bayer Ag Kombinationstherapie substituierter Oxazolidinone
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KR101009594B1 (ko) 2007-05-09 2011-01-20 주식회사 레고켐 바이오사이언스 Ｐ4 위치에 사이클릭 아미딘을 가지는 ＦＸａ 저해제, 이의유도체, 제조방법 및 이를 함유하는 의약 조성물
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Also Published As

Publication number Publication date
SK8572000A3 (en) 2001-07-10
EP1056743A1 (de) 2000-12-06
AU744002B2 (en) 2002-02-14
AR017844A1 (es) 2001-10-24
CN1281451A (zh) 2001-01-24
ZA9811339B (en) 1999-07-08
NO20002958D0 (no) 2000-06-09
BR9813477A (pt) 2000-10-24
WO1999031092A1 (de) 1999-06-24
PL341008A1 (en) 2001-03-12
AU1964799A (en) 1999-07-05
RU2203897C2 (ru) 2003-05-10
HUP0004353A3 (en) 2002-04-29
NO20002958L (no) 2000-08-11
KR20010032963A (ko) 2001-04-25
JP2002508370A (ja) 2002-03-19
CA2313651A1 (en) 1999-06-24
DE19755268A1 (de) 1999-06-17

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