DK2675793T3 - Fak-inhibitorer - Google Patents

Fak-inhibitorer Download PDF

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Publication number
DK2675793T3
DK2675793T3 DK12705383.3T DK12705383T DK2675793T3 DK 2675793 T3 DK2675793 T3 DK 2675793T3 DK 12705383 T DK12705383 T DK 12705383T DK 2675793 T3 DK2675793 T3 DK 2675793T3
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Denmark
Prior art keywords
mmol
phenyl
trifluoromethyl
pyrimidin
amino
Prior art date
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DK12705383.3T
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English (en)
Inventor
Ian Peter Holmes
Ylva Bergman
Gillian Elizabeth Lunniss
Marica Nikac
Neil Choi
Catherine Fae Hemley
Scott Raymond Walker
Richard Charles Foitzik
Danny Ganame
Romina Lessene
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Cancer Therapeutics Crc Pty Ltd
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Publication of DK2675793T3 publication Critical patent/DK2675793T3/da

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    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D403/06—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 only aliphatic carbon atoms
    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • C07D413/12—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 chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Mycology (AREA)
  • Immunology (AREA)
  • Microbiology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Claims (15)

1. Forbindelse med formlen (I):
(O eller en ion-, salt- eller solvatform deraf, hvor: R1 er udvalgt blandt: H, og
hvor: RN1 er udvalgt blandt H, C1-3 alkyl og C(=O)Me; RN2 er udvalgt blandt H, C1-3 alkyl og C(=O)Me; RN3 er udvalgt blandt H, C1-3 alkyl og C(=O)Me; RN4 er udvalgt blandt H og CH3; RN7 og RN8 er uafhængigt udvalgt blandt H og CH3; RN9 er udvalgt blandt H, C1-3 alkyl og C(=O)Me; RN1° er udvalgt blandt H, C1-3 alkyl og C(=O)Me; RN11 er udvalgt blandt H, C1-3 alkyl og C(=O)Me; R2 er udvalgt blandt H og
hvor: RN5 er udvalgt blandt H, C1-3 alkyl og C(=O)Me; RN6 er udvalgt blandt H, C1-3 alkyl og C(=O)Me; og hvor kun ét af R1 og R2 er H; eller R1 og R2 sammen danner gruppen -CH2-N(RN12)-C2H4-, hvor RN12 er udvalgt blandt H, C1-3 alkyl og C(=O)Me; R4 er udvalgt blandt CF3, halogen, CF2H og CN; og
R5 er udvalgt blandt grupper med de følgende formler:
hvor: R6 er udvalgt blandt H, (CHRc1)niC(O)N(RN13)Z1 og (CH2)n2C(O)OZ2; hvor: n1 er 1; RC1 er H eller Me; RN13 er H eller CHs; Z1 er H, CHs eller OCHs; n2 er 1;og Z2 er CHs; og hvor kun ét af RN13 og Z1 kan være CH3, R7, hvis til stede, er udvalgt blandt H og (CH2)miC(0)N(RM1)Y1, hvor: m1 er 0 eller 1; RM1 er H; og Y1 erH, Me eller OCHs; og ét af R6 og R7 ikke er H; og R8, hvis til stede, er H, eller, når R7 er C(=O)NH2, R8 er udvalgt blandt H og C1-2 al kyl.
2. Forbindelse ifølge krav 1, hvor R2 er H, og R1 er:
hvor RN1 er C(=O)Me; eller
hvor RN1 er H, methyl eller ethyl; eller
hvor RN2 er udvalgt blandt H, methyl og ethyl; eller
hvor RN3 er udvalgt blandt H og methyl; eller
hvor RN4 er udvalgt blandt H og methyl; eller
hvor RN7 og RN8 begge er H eller begge methyl; eller
hvor RN9 er H; eller
hvor RN1° er udvalgt blandt H og methyl; eller
hvor RN11 er H.
3. Forbindelse ifølge krav 1, hvor R1 er H, og R2 er:
hvor RN5 er udvalgt blandt H og methyl; eller
hvor RN6 er udvalgt blandt H og methyl.
4. Forbindelse ifølge et af kravene 1 til 3, hvor R4 er udvalgt blandt CF3, Cl og CF2H, fortrinsvis CF3.
5. Forbindelse ifølge et af kravene 1 til 4, hvor R5 er en gruppe med den føl-aende formel:
(R5a)
6. Forbindelse ifølge et af kravene 1 til 4, hvor R5 er en gruppe udvalgt blandt:
(R50) (R5d) (R5j
7. Forbindelse ifølge krav 5 eller krav 6, hvor R7 er H, og R6 er udvalgt blandt CH2C(O)NH2, CH2C(O)NHCH3, CHCH3C(O)NH2 og CHCH3C(O)NHCH3.
8. Forbindelse ifølge krav 7, hvor R7 er H, og R6 er udvalgt blandt CH2C(O)NH2, CHCH3C(O)NH2 og CH2C(O)NHCH3.
9. Forbindelse ifølge krav 5 eller krav 6, hvor R6 er H, og R7 er udvalgt blandt C(O)NH2, C(O)NHCH3j CH2C(O)NH2 og CH2C(O)NHCH3.
10. Forbindelse ifølge krav 9, hvor R6 er H, og R7 er C(O)NH2.
11. Forbindelse ifølge krav 10, hvor R8 er methyl.
12. Forbindelse ifølge et af kravene 1 til 4, hvor R5 er en gruppe med den følgende formel:
(R5b)
13. Sammensætning omfattende en forbindelse ifølge et af kravene 1 til 12 og et farmaceutisk acceptabelt bærestof eller fortyndingsmiddel.
14. Forbindelse ifølge et af kravene 1 til 12 til anvendelse i en fremgangsmåde til terapi.
15. Forbindelse ifølge et af kravene 1 til 12 til anvendelse i fremgangsmåden til behandling af kræft.
DK12705383.3T 2011-02-17 2012-02-17 Fak-inhibitorer DK2675793T3 (da)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201161443773P 2011-02-17 2011-02-17
US201161523503P 2011-08-15 2011-08-15
US201161579719P 2011-12-23 2011-12-23
PCT/GB2012/000175 WO2012110773A1 (en) 2011-02-17 2012-02-17 Fak inhibitors

Publications (1)

Publication Number Publication Date
DK2675793T3 true DK2675793T3 (da) 2018-11-12

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ID=45755399

Family Applications (1)

Application Number Title Priority Date Filing Date
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Country Status (9)

Country Link
US (3) US20130324532A1 (da)
EP (1) EP2675793B1 (da)
JP (1) JP5937111B2 (da)
CN (1) CN103534241B (da)
AU (1) AU2012216893B2 (da)
CA (1) CA2827171C (da)
DK (1) DK2675793T3 (da)
ES (1) ES2691673T3 (da)
WO (1) WO2012110773A1 (da)

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CA2827171A1 (en) 2012-08-23
CN103534241B (zh) 2015-11-25
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EP2675793A1 (en) 2013-12-25
CA2827171C (en) 2019-04-09
ES2691673T3 (es) 2018-11-28
JP5937111B2 (ja) 2016-06-22
US20130324532A1 (en) 2013-12-05
EP2675793B1 (en) 2018-08-08
AU2012216893A1 (en) 2013-09-05
JP2014505718A (ja) 2014-03-06
AU2012216893B2 (en) 2016-08-11
US20150231135A1 (en) 2015-08-20
US9012461B2 (en) 2015-04-21
US20130017194A1 (en) 2013-01-17
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