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 useInfo
- 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
Links
- -1 Imidazolyl aminoalkyl fluorene derivatives Chemical class 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 101100516568 Caenorhabditis elegans nhr-7 gene Proteins 0.000 abstract 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 239000001301 oxygen Substances 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 125000004434 sulfur atom Chemical group 0.000 abstract 2
- 125000006647 (C3-C15) cycloalkyl group Chemical group 0.000 abstract 1
- 206010003210 Arteriosclerosis Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000001132 Osteoporosis Diseases 0.000 abstract 1
- 208000037273 Pathologic Processes Diseases 0.000 abstract 1
- 208000007536 Thrombosis Diseases 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 230000033115 angiogenesis Effects 0.000 abstract 1
- 208000011775 arteriosclerosis disease Diseases 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 abstract 1
- 230000017531 blood circulation Effects 0.000 abstract 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 abstract 1
- 208000029078 coronary artery disease Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 102000006495 integrins Human genes 0.000 abstract 1
- 108010044426 integrins Proteins 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 abstract 1
- 125000002911 monocyclic heterocycle group Chemical group 0.000 abstract 1
- 208000010125 myocardial infarction Diseases 0.000 abstract 1
- 230000009054 pathological process Effects 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 230000000644 propagated effect Effects 0.000 abstract 1
- 125000006239 protecting group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
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)
- 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
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)
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)
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 |
-
1999
- 1999-08-07 DE DE19937394A patent/DE19937394A1/en not_active Withdrawn
-
2000
- 2000-07-26 CA CA002380981A patent/CA2380981A1/en not_active Abandoned
- 2000-07-26 WO PCT/EP2000/007153 patent/WO2001010841A2/en not_active Application Discontinuation
- 2000-07-26 SK SK140-2002A patent/SK1402002A3/en unknown
- 2000-07-26 AU AU68286/00A patent/AU6828600A/en not_active Abandoned
- 2000-07-26 HU HU0202464A patent/HUP0202464A3/en unknown
- 2000-07-26 JP JP2001515308A patent/JP2003506439A/en active Pending
- 2000-07-26 EP EP00956284A patent/EP1208088A2/en not_active Withdrawn
- 2000-07-26 BR BR0013083-4A patent/BR0013083A/en not_active Application Discontinuation
- 2000-07-26 CZ CZ2002298A patent/CZ2002298A3/en unknown
- 2000-07-26 CN CN00811476A patent/CN1368962A/en active Pending
- 2000-07-26 KR KR1020027000660A patent/KR20020012631A/en not_active Application Discontinuation
- 2000-07-26 PL PL00353054A patent/PL353054A1/en unknown
- 2000-07-26 MX MXPA02001297A patent/MXPA02001297A/en not_active Application Discontinuation
- 2000-08-04 AR ARP000104035A patent/AR025042A1/en unknown
-
2002
- 2002-02-06 NO NO20020592A patent/NO20020592L/en not_active Application Discontinuation
- 2002-03-06 ZA ZA200201873A patent/ZA200201873B/en unknown
-
2003
- 2003-02-20 HK HK03101305.5A patent/HK1049006A1/en unknown
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 |
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