WO2001010841A3 - Fluorene derivatives as integrin inhibitors - Google Patents

Fluorene derivatives as integrin inhibitors Download PDF

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Publication number
WO2001010841A3
WO2001010841A3 PCT/EP2000/007153 EP0007153W WO0110841A3 WO 2001010841 A3 WO2001010841 A3 WO 2001010841A3 EP 0007153 W EP0007153 W EP 0007153W WO 0110841 A3 WO0110841 A3 WO 0110841A3
Authority
WO
WIPO (PCT)
Prior art keywords
integrin inhibitors
fluorene derivatives
disorders
arteriosclerosis
thrombosis
Prior art date
Application number
PCT/EP2000/007153
Other languages
German (de)
French (fr)
Other versions
WO2001010841A2 (en
Inventor
Wolfgang Staehle
Simon Goodman
Original Assignee
Merck Patent Gmbh
Wolfgang Staehle
Simon Goodman
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 BR0013083-4A priority Critical patent/BR0013083A/en
Priority to PL00353054A priority patent/PL353054A1/en
Priority to JP2001515308A priority patent/JP2003506439A/en
Priority to SK140-2002A priority patent/SK1402002A3/en
Priority to MXPA02001297A priority patent/MXPA02001297A/en
Priority to CA002380981A priority patent/CA2380981A1/en
Priority to HU0202464A priority patent/HUP0202464A3/en
Priority to AU68286/00A priority patent/AU6828600A/en
Application filed by Merck Patent Gmbh, Wolfgang Staehle, Simon Goodman filed Critical Merck Patent Gmbh
Priority to EP00956284A priority patent/EP1208088A2/en
Priority to KR1020027000660A priority patent/KR20020012631A/en
Publication of WO2001010841A2 publication Critical patent/WO2001010841A2/en
Publication of WO2001010841A3 publication Critical patent/WO2001010841A3/en
Priority to NO20020592A priority patent/NO20020592L/en
Priority to HK03101305.5A priority patent/HK1049006A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic 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
    • C07D233/28—Heterocyclic 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
    • C07D233/44—Nitrogen atoms not forming part of a nitro radical
    • C07D233/48—Nitrogen atoms not forming part of a nitro radical with acyclic hydrocarbon or substituted acyclic hydrocarbon radicals, attached to said nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/04—Derivatives 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
    • C07C279/12—Derivatives 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10—Ortho- 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)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Immunology (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (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

The invention relates to compounds of formula (I) wherein R?1, R2, R3, R4, R5¿, m and n have the meaning given in Claim 1, and to their physiologically acceptable salts and solvates, which can be used as integrin inhibitors, especially for the prophylaxis and treatment of blood circulation disorders, thrombosis, myocardial infarction, coronary disorders, arteriosclerosis, osteoporosis, pathological processes which are maintained or propagated through angiogenesis, as well as in tumour therapy.
PCT/EP2000/007153 1999-08-07 2000-07-26 Fluorene derivatives as integrin inhibitors WO2001010841A2 (en)

Priority Applications (12)

Application Number Priority Date Filing Date Title
HU0202464A HUP0202464A3 (en) 1999-08-07 2000-07-26 Imidazolyl aminoalkyl fluorene derivatives, process for their preparation, pharmaceutical compositions containing them and their use
JP2001515308A JP2003506439A (en) 1999-08-07 2000-07-26 Fluorene derivative
SK140-2002A SK1402002A3 (en) 1999-08-07 2000-07-26 Fluorene derivative, process for the preparation thereof and pharmaceutical composition comprising same
MXPA02001297A MXPA02001297A (en) 1999-08-07 2000-07-26 Fluorene derivatives.
CA002380981A CA2380981A1 (en) 1999-08-07 2000-07-26 Fluorene derivatives
BR0013083-4A BR0013083A (en) 1999-08-07 2000-07-26 Fluorane Derivatives
AU68286/00A AU6828600A (en) 1999-08-07 2000-07-26 Fluorene derivatives
PL00353054A PL353054A1 (en) 1999-08-07 2000-07-26 Fluorene derivatives as integrin inhibitors
EP00956284A EP1208088A2 (en) 1999-08-07 2000-07-26 Fluorene derivatives as integrin inhibitors
KR1020027000660A KR20020012631A (en) 1999-08-07 2000-07-26 Fluorene derivatives
NO20020592A NO20020592L (en) 1999-08-07 2002-02-06 Fluorine derivatives as integrin inhibitors
HK03101305.5A HK1049006A1 (en) 1999-08-07 2003-02-20 Fluorene derivatives

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19937394A DE19937394A1 (en) 1999-08-07 1999-08-07 Fluorene derivatives
DE19937394.9 1999-08-07

Publications (2)

Publication Number Publication Date
WO2001010841A2 WO2001010841A2 (en) 2001-02-15
WO2001010841A3 true WO2001010841A3 (en) 2001-09-07

Family

ID=7917613

Family Applications (1)

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

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

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1990015602A1 (en) * 1989-06-22 1990-12-27 Nova Pharmaceutical Corporation Pharmaceutical compositions and methods for treating inflammation
EP0675112A1 (en) * 1994-03-31 1995-10-04 Bristol-Myers Squibb Company Imidazole-containing inhibitors of farnesyl protein transferase
WO1997036862A1 (en) * 1996-03-29 1997-10-09 G.D. Searle & Co. META-SUBSTITUTED PHENYLENE DERIVATIVES AND THEIR USE AS ALPHAvBETA3 INTEGRIN ANTAGONISTS OR INHIBITORS
DE19654483A1 (en) * 1996-06-28 1998-01-02 Merck Patent Gmbh Phenylalanine derivatives
EP0832883A1 (en) * 1996-09-26 1998-04-01 Eli Lilly And Company Tetrahydrobenzo(a)fluorene compounds and methods of use

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1990015602A1 (en) * 1989-06-22 1990-12-27 Nova Pharmaceutical Corporation Pharmaceutical compositions and methods for treating inflammation
EP0675112A1 (en) * 1994-03-31 1995-10-04 Bristol-Myers Squibb Company Imidazole-containing inhibitors of farnesyl protein transferase
WO1997036862A1 (en) * 1996-03-29 1997-10-09 G.D. Searle & Co. META-SUBSTITUTED PHENYLENE DERIVATIVES AND THEIR USE AS ALPHAvBETA3 INTEGRIN ANTAGONISTS OR INHIBITORS
DE19654483A1 (en) * 1996-06-28 1998-01-02 Merck Patent Gmbh Phenylalanine derivatives
EP0832883A1 (en) * 1996-09-26 1998-04-01 Eli Lilly And Company Tetrahydrobenzo(a)fluorene compounds and methods of use

Also Published As

Publication number Publication date
ZA200201873B (en) 2003-08-27
KR20020012631A (en) 2002-02-16
BR0013083A (en) 2002-04-23
AU6828600A (en) 2001-03-05
WO2001010841A2 (en) 2001-02-15
EP1208088A2 (en) 2002-05-29
HUP0202464A3 (en) 2003-02-28
JP2003506439A (en) 2003-02-18
NO20020592D0 (en) 2002-02-06
CA2380981A1 (en) 2001-02-15
SK1402002A3 (en) 2002-06-04
AR025042A1 (en) 2002-11-06
DE19937394A1 (en) 2001-02-08
MXPA02001297A (en) 2004-07-16
HUP0202464A2 (en) 2002-12-28
PL353054A1 (en) 2003-10-06
NO20020592L (en) 2002-04-04
CZ2002298A3 (en) 2002-04-17
CN1368962A (en) 2002-09-11
HK1049006A1 (en) 2003-04-25

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