HUP0402003A2 - Szubsztituált 1,4-benzodiazepinek, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk - Google Patents

Szubsztituált 1,4-benzodiazepinek, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk

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Publication number
HUP0402003A2
HUP0402003A2 HU0402003A HUP0402003A HUP0402003A2 HU P0402003 A2 HUP0402003 A2 HU P0402003A2 HU 0402003 A HU0402003 A HU 0402003A HU P0402003 A HUP0402003 A HU P0402003A HU P0402003 A2 HUP0402003 A2 HU P0402003A2
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HU
Hungary
Prior art keywords
optionally substituted
alkyl
cycloalkyl
aralkyl
heteroaryl
Prior art date
Application number
HU0402003A
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English (en)
Inventor
Tianbao Lu
Louis V. Lafrance Iii
Daniel J. Parks
Karen L. Milkiewicz
Raul R. Calvo
Maxwell David Cummings
Alexander J. Kim
Bruce L. Grasberger
Theodore E. Carver
Original Assignee
3-Dimensional Pharmaceuticals, Inc.
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Publication date
Application filed by 3-Dimensional Pharmaceuticals, Inc. filed Critical 3-Dimensional Pharmaceuticals, Inc.
Publication of HUP0402003A2 publication Critical patent/HUP0402003A2/hu
Publication of HUP0402003A3 publication Critical patent/HUP0402003A3/hu

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    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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    • 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
    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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
    • C07D409/04—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 directly linked by a ring-member-to-ring-member bond

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Immunology (AREA)
  • Diabetes (AREA)
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  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
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  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

A találmány tárgya új 1,4-benzodiazepinek, gyógyászatilag elfogadhatókészítményei, és alkalmazásuk rák kezelésére alkalmasgyógyszerkészítmények előállítására. A találmány szerinti vegyületek,szolvátjai, hidrátjai vagy gyógyászatilag elfogadható sói az (I)általános képlettel jellemezhetők, ahol X és Y egymástól függetlenül -C(O)-, CH2- vagy -C(S)-; R1, R2, R3 és R4 jelentése egymástólfüggetlenül hidrogén- vagy halogénatom, alkil-, alkenil-, alkinil-,cikloalkil-, adott esetben szubsztituált aril-, adott esetbenszubsztituált aralkil-, adott esetben szubsztituált heteroaril-, adottesetben szubsztituált heteroaralkil-, alkoxi-, adott esetbenszubsztituált aril-oxi-, adott esetben szubsztituált heteroaril-oxi-,ciano-, amino-, alkanoil-amino-, nitro-, hidroxil-, karboxil-, vagyalkoxi-karbonil-csoport; vagy R1 és R2, vagy R2 és R3, vagy R3 és R4együtt -(CH2)n- csoportot képez, ahol u értéke 3-6, vagy -CH=CH-CH=CH-vagy -CH2CH=CHCH2-; R5 jelentése hidrogénatom, alkil-, cikloalkil-,adott esetben szubsztituált aril-, adott esetben szubsztituáltheteroaril-, adott esetben szubsztituált aralkil-, adott esetbenszubsztituált heteroaralkil-, karboxi-alkil-, alkoxi-karbonil-,alkoxi-karbonil-alkil-, amino-karbonil-, amino-karbonil-alkil-, alkil-amino-karbonil- vagy alkil-amino-karbonil-alkil-csoport; R6 jelentésecikloalkil-, aril-, heteroaril-, cikloalkil-alkil-, aralkil-,heteroaril-alkil vagy telített vagy részben telítetlen heterociklusoscsoport, melyek mindegyike adott esetben szubsztituált; R7 és R8jelentése egymástól függetlenül hidrogénatom vagy alkilcsoport; R9jelentése cikloalkil-, aril-, heteroaril-, telített vagy részbentelítetlen heterociklusos csoport, cikloalkil(alkil)-, aralkil- vagyheteroaril-alkil-csoport, melyek mindegyike adott esetbenszubsztituált; és R10 jelentése -(CH2)n-CO2Rb, -(CH2)m,-CO2M vagy -(CH2)i-OH, ahol Rb jelentése hidrogénatom, alkil-, adott esetbenszubsztituált cikloalkil vagy adott esetben szubsztituált, telítettvagy részben telítetlen heterociklusos csoport; M jelentése kation; ésn értéke 0-8, m értéke 0-8 és i értéke 1-8 közötti egész szám. Ó
HU0402003A 2001-11-13 2002-11-13 Substituted 1,4-benzodiazepines, pharmaceutical compositions containing them and uses thereof HUP0402003A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US33123501P 2001-11-13 2001-11-13
PCT/US2002/036208 WO2003041715A1 (en) 2001-11-13 2002-11-13 Substituted 1,4-benzodiazepines and uses thereof for the treatment of cancer

Publications (2)

Publication Number Publication Date
HUP0402003A2 true HUP0402003A2 (hu) 2005-02-28
HUP0402003A3 HUP0402003A3 (en) 2005-06-28

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ID=23293137

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0402003A HUP0402003A3 (en) 2001-11-13 2002-11-13 Substituted 1,4-benzodiazepines, pharmaceutical compositions containing them and uses thereof

Country Status (26)

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US (2) US7067512B2 (hu)
EP (1) EP1443937B1 (hu)
JP (1) JP4497921B2 (hu)
KR (1) KR20050044413A (hu)
CN (1) CN1596114A (hu)
AT (1) ATE398453T1 (hu)
AU (1) AU2002340464B2 (hu)
BR (1) BR0214048A (hu)
CA (1) CA2466055A1 (hu)
CY (1) CY1108352T1 (hu)
DE (1) DE60227185D1 (hu)
DK (1) DK1443937T3 (hu)
ES (1) ES2309209T3 (hu)
HR (1) HRP20040415A2 (hu)
HU (1) HUP0402003A3 (hu)
IL (1) IL161692A0 (hu)
MX (1) MXPA04004500A (hu)
NO (1) NO20042146L (hu)
NZ (1) NZ532463A (hu)
PL (1) PL370176A1 (hu)
PT (1) PT1443937E (hu)
RU (1) RU2004118243A (hu)
SI (1) SI1443937T1 (hu)
UA (1) UA76798C2 (hu)
WO (1) WO2003041715A1 (hu)
ZA (1) ZA200403082B (hu)

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