HUP0202464A2 - Imidazolyl aminoalkyl fluorene derivatives, process for their preparation, pharmaceutical compositions containing them and their use - Google Patents

Imidazolyl aminoalkyl fluorene derivatives, process for their preparation, pharmaceutical compositions containing them and their use

Info

Publication number
HUP0202464A2
HUP0202464A2 HU0202464A HUP0202464A HUP0202464A2 HU P0202464 A2 HUP0202464 A2 HU P0202464A2 HU 0202464 A HU0202464 A HU 0202464A HU P0202464 A HUP0202464 A HU P0202464A HU P0202464 A2 HUP0202464 A2 HU P0202464A2
Authority
HU
Hungary
Prior art keywords
group
unsubstituted
so2r7
nhr7
cooa
Prior art date
Application number
HU0202464A
Other languages
Hungarian (hu)
Inventor
Simon Goodman
Wolfgang Stähle
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 HUP0202464A2 publication Critical patent/HUP0202464A2/en
Publication of HUP0202464A3 publication Critical patent/HUP0202464A3/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole 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
    • C07D233/44Nitrogen atoms not forming part of a nitro radical
    • C07D233/48Nitrogen atoms not forming part of a nitro radical with acyclic hydrocarbon or substituted acyclic hydrocarbon radicals, attached to said nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C279/00Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/04Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton
    • C07C279/12Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to acyclic carbon atoms of a carbon skeleton being further substituted by nitrogen atoms not being part of nitro or nitroso groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00Systems containing at least three condensed rings
    • C07C2603/02Ortho- or ortho- and peri-condensed systems
    • C07C2603/04Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (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)
  • Public Health (AREA)
  • Cardiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

A találmány tárgya (I) általános képletű vegyületek - ahol R1jelentése OR7, NHR7 vagy NA<2; R2 jelentése hidrogénatom, CO-R7, CO-OR7, CONHR7, CONA<2 vagy SO2R7; R4 és R5 jelentése egymástólfüggetlenül hidrogénatom, Hal, NO2, NHR7, NA<2, OR7, -CO-R7, SO3R7,SO2R7 vagy SR7; R3 jelentése NH2, -C(=NH)-NH2, -NH-C(=NH)-NH2 vagy -C(=O)N=C(NH2)2, vagy amely lehet szubsztituálatlan vagy egyszerszubsztituált -COA, -COOA, -OH csoporttal vagy szokásosaminovédőcsoporttal vagy R6-NH- csoporttal; R6 jelentése 1-4nitrogén-, oxigén- és/vagy kénatomot tartalmazó mono- vagy biciklusosheterociklusos csoport, amely lehet szubsztituálatlan vagy egyszer,kétszer vagy háromszor lehet szubsztituálva a következő csoportokkal:Hal, A<, -CO-A', OA', CN, COOA', CONH2, NO2, -NH vagy =O; R7 jelentésehidrogénatom, A, aril- vagy aralkil-csoport A jelentése 1-15szénatomos alkil- vagy 3-15 szénatomos cikloalkilcsoport, amelyszubsztituálatlan vagy R8-cal egyszer, kétszer vagy háromszorszubsztituált, és ahol egy, kettő vagy három metiléncsoportotnitrogén-, oxigénés/vagy kénatom helyettesíthet; m és n minden esetbenegymástól függetlenül 0, 1, 2, 3 vagy 4 - és fiziológiailagelfogadható sóik és szolvátjaik, amelyek integrin inhibitorként,különösen vérkeringési betegségek, trombózis, miokardiális infarktus,koszorúér betegségek, arterioszklerózis, csontritkulás, és azangiogenézis során fenntartott vagy szaporodó patológiai folyamatokkezelésére használhatók, valamint a tumorterápiában alkalmazhatók. Atalálmány továbbá kiterjed az (I) általános képletű vegyületekelőállítására és az ezeket tartalmazó gyógyszerkészítményekre is. ÓThe subject of the invention is compounds of general formula (I) - where R1 means OR7, NHR7 or NA<2; R2 is hydrogen, CO-R7, CO-OR7, CONHR7, CONA<2 or SO2R7; R4 and R5 are independently hydrogen, Hal, NO2, NHR7, NA<2, OR7, -CO-R7, SO3R7, SO2R7 or SR7; R3 is NH2, -C(=NH)-NH2, -NH-C(=NH)-NH2 or -C(=O)N=C(NH2)2, or which can be unsubstituted or monosubstituted -COA, -COOA, with an -OH group or a conventional amino protecting group or an R6-NH- group; R6 is a mono- or bicyclic heterocyclic group containing 1-4 nitrogen, oxygen and/or sulfur atoms, which can be unsubstituted or substituted once, twice or three times with the following groups: Hal, A<, -CO-A', OA', CN , COOA', CONH 2 , NO 2 , -NH or =O; R7 is a hydrogen atom, A, an aryl or aralkyl group A is a C1-15 alkyl or C3-15 cycloalkyl group, which is unsubstituted or mono-, di- or tri-substituted by R8 and where one, two or three methylene groups are nitrogen, oxygen and/or sulfur atoms can replace; m and n are in each case independently 0, 1, 2, 3 or 4 - and their physiologically acceptable salts and solvates, which are used as integrin inhibitors, especially for the treatment of blood circulation diseases, thrombosis, myocardial infarction, coronary artery diseases, arteriosclerosis, osteoporosis, and pathological processes maintained or propagated during angiogenesis can be used as well as in tumor therapy. The invention also covers the production of compounds of general formula (I) and pharmaceutical preparations containing them. HE

HU0202464A 1999-08-07 2000-07-26 Imidazolyl aminoalkyl fluorene derivatives, process for their preparation, pharmaceutical compositions containing them and their use HUP0202464A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19937394A DE19937394A1 (en) 1999-08-07 1999-08-07 Fluorene derivatives
PCT/EP2000/007153 WO2001010841A2 (en) 1999-08-07 2000-07-26 Fluorene derivatives as integrin inhibitors

Publications (2)

Publication Number Publication Date
HUP0202464A2 true HUP0202464A2 (en) 2002-12-28
HUP0202464A3 HUP0202464A3 (en) 2003-02-28

Family

ID=7917613

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0202464A HUP0202464A3 (en) 1999-08-07 2000-07-26 Imidazolyl aminoalkyl fluorene derivatives, process for their preparation, pharmaceutical compositions containing them and their use

Country Status (18)

Country Link
EP (1) EP1208088A2 (en)
JP (1) JP2003506439A (en)
KR (1) KR20020012631A (en)
CN (1) CN1368962A (en)
AR (1) AR025042A1 (en)
AU (1) AU6828600A (en)
BR (1) BR0013083A (en)
CA (1) CA2380981A1 (en)
CZ (1) CZ2002298A3 (en)
DE (1) DE19937394A1 (en)
HK (1) HK1049006A1 (en)
HU (1) HUP0202464A3 (en)
MX (1) MXPA02001297A (en)
NO (1) NO20020592L (en)
PL (1) PL353054A1 (en)
SK (1) SK1402002A3 (en)
WO (1) WO2001010841A2 (en)
ZA (1) ZA200201873B (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101102808B1 (en) * 2010-04-13 2012-01-05 윤태삼 Riser tensioner
US8574899B2 (en) 2010-12-22 2013-11-05 Vladimir B Serikov Methods for augmentation collection of placental hematopoietic stem cells and uses thereof

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH04506350A (en) * 1989-06-22 1992-11-05 ノバ ファーマスーティカル コーポレイション Pharmaceutical compositions for treating inflammation and methods for treating inflammation
RU95104898A (en) * 1994-03-31 1996-12-27 Бристоль-Мейерз Сквибб Компани (US) Imedazole containing inhibitors of ferneside proteintansferase, and method of treatment diseases related therewith
JP2000506538A (en) * 1996-03-29 2000-05-30 ジー.ディー.サール アンド カンパニー Meta-substituted phenylene derivatives
DE19654483A1 (en) * 1996-06-28 1998-01-02 Merck Patent Gmbh Phenylalanine derivatives
CA2214931A1 (en) * 1996-09-26 1998-03-26 Henry Uhlman Bryant Tetrahydrobenzo-a-fluorene compounds and method of use

Also Published As

Publication number Publication date
SK1402002A3 (en) 2002-06-04
NO20020592L (en) 2002-04-04
CN1368962A (en) 2002-09-11
AU6828600A (en) 2001-03-05
PL353054A1 (en) 2003-10-06
HUP0202464A3 (en) 2003-02-28
DE19937394A1 (en) 2001-02-08
MXPA02001297A (en) 2004-07-16
CZ2002298A3 (en) 2002-04-17
JP2003506439A (en) 2003-02-18
CA2380981A1 (en) 2001-02-15
WO2001010841A3 (en) 2001-09-07
KR20020012631A (en) 2002-02-16
HK1049006A1 (en) 2003-04-25
AR025042A1 (en) 2002-11-06
ZA200201873B (en) 2003-08-27
NO20020592D0 (en) 2002-02-06
EP1208088A2 (en) 2002-05-29
BR0013083A (en) 2002-04-23
WO2001010841A2 (en) 2001-02-15

Similar Documents

Publication Publication Date Title
CY1105250T1 (en) METHOD OF THERAPEUTIC INDUCTION OF P38 KINASE-RELATED CONDITIONS AND PYRROLOTRIAZINE COMPOUNDS USABLE AS KINASE INHIBITORS
HUP0001446A2 (en) 4,4-disubstituted-3,4-dihydro-2(1h)-quinazolinone derivatives as hiv reverse transcriptase inhibitors, their use and pharmaceutical compositions containing them
NO913750D0 (en) PROCEDURE FOR THE PREPARATION OF THERAPEUTIC ACTIVE HETEROCYCLIC DERIVATIVES.
HUP0301195A2 (en) Aza-bridged-bicyclic amino acid derivatives as alpha4 integrin antagonists and pharmaceutical compositions containing the compounds
PA8510101A1 (en) ANTIBACTERIAL AGENTS OF 3-AMINOQUINAZOLIN-2,4 DIONAS.
HUP0201646A2 (en) Novel alpha-amino acid derivatives, process for producing them and pharmaceutical compositions containing them
HUP9903716A2 (en) Tyrosin-derivate as alpha-v-integrin inhibitors
EA200000842A1 (en) BICYCLO [2.2.1] HEPTANS AND RELATED CONNECTIONS
NO174549C (en) Analogous Process for Preparing Therapeutically Active, Asymmetrically Substituted Heterocyclic Compounds
TR200201505T2 (en) Pirazolopyrimidines as therapeutic agents
NO920035L (en) TRIFLUORMETHYLKETON DERIVATIVES AND THEIR PREPARATION AND USE
CA2280727A1 (en) Bicyclic amino acids
HUP0100488A2 (en) Thienopyrimidines, process for their preparation and pharmaceutical compositions containing them
DZ1694A1 (en) &#34;N- (2-Aminoethyl) -benzothialozones&#34;.
HUP0104164A2 (en) Imidazo[4,5-c]-pyridine-4-one derivatives with factor xa inhibiting effect, pharmaceutical compositions containing the same and process for their preparation
WO2003082861A3 (en) Morpholinyl-urea derivatives for use of the treatment of inflammatory diseases
HUP0301551A2 (en) New use of 5ht3 and neuronal nicotinicreceptor antagonist 1-amino-alkycyclohexanes
HUP0203275A2 (en) 1-cyclic amino-alkylcyclohexane compounds, pharmaceutical compositions thereof, and their use as anticonvulsants
HUP0202464A2 (en) Imidazolyl aminoalkyl fluorene derivatives, process for their preparation, pharmaceutical compositions containing them and their use
HUP0301784A2 (en) Biphenyl derivatives, of imidazole and benzimidazole the use thereof, process for the preparation of compounds and pharmaceutical compositions containing them
HUP0302753A2 (en) Urea and urethane derivatives as integrin inhibitors, process for their preparation, their use and pharmaceutical compositions containing them
ES2066755T3 (en) DERIVATIVES OF RENINE INHIBITING AMINO ACIDS.
HUP0203212A2 (en) Integrin inhibitors, process for preparation thereof, their use preparation of pharmaceutical compositions and the compositions
BR0012391A (en) Diacylhydrazine derivatives
AR004680A1 (en) DERIVATIVES OF THE ALQUENIL-BENZOILGUANIDINA, PROCEDURE TO PREPARE THEM AND PHARMACEUTICAL PREPARATIONS THAT CONTAIN THEM.