DK2935244T3 - Hidtil ukendte benzimidazol-derivater som kinase-inhibitorer - Google Patents
Hidtil ukendte benzimidazol-derivater som kinase-inhibitorer Download PDFInfo
- Publication number
- DK2935244T3 DK2935244T3 DK13811246.1T DK13811246T DK2935244T3 DK 2935244 T3 DK2935244 T3 DK 2935244T3 DK 13811246 T DK13811246 T DK 13811246T DK 2935244 T3 DK2935244 T3 DK 2935244T3
- Authority
- DK
- Denmark
- Prior art keywords
- heterocycle
- independently selected
- optionally substituted
- substituents independently
- group
- Prior art date
Links
Classifications
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
- C07D235/14—Radicals substituted by nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
- C07D235/30—Nitrogen atoms not forming part of a nitro radical
-
- 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
- C07D401/04—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
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- 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
- C07D405/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Rheumatology (AREA)
- Transplantation (AREA)
- Hospice & Palliative Care (AREA)
- Oncology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Hematology (AREA)
- Dermatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Epidemiology (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Claims (11)
1. Forbindelse af formel (I):
(i) hvor X1 er valgt fra gruppen bestående af nitro, cyano, trifluormethyl og -C(=O)OT4; Z og X2 er hver uafhængigt valgt fra gruppen bestående af F, Cl, Br og I; X3 er isopropyl eller ethyl; X4 enten mangler eller er valgt fra -NR4- og -N(R4)(CH2)-; R4 er valgt fra H og -Ci-6alkyl; Y1 er valgt fra gruppen bestående af H, -Ci-6alkyl og en 4- til 7-leddet mættet eller umættet aromatisk carbocykel eller heterocykel, med betingelsen at fastgørelsespunktet på nævnte heterocykel er carbon hvis X4 er -NR4- eller -N(R4)(CH2)-, hvor nævnte -Ci-6alkyl er eventuelt substitueret med en eller flere substituenter uafhængigt valgt fra F, -OT1, -N(T2)(T3), -C( = O)N(T2)(T3), -0( = 0)0^, -ST1, -5(=0)2^, -S( = O)2N(T2)(T3) og en 5- til 6-leddet mættet heterocykel, og hvor nævnte 4- til 7-leddede carbocykel eller heterocykel er eventuelt substitueret med en eller flere substituenter uafhængigt valgt fra F, -OT1, -N(T2)(T3), -C(=O)N(T2)(T3), -0(=0)0^, -ST1, -S(=O)2T1, -S(=O)2N(T2)(T3), oxo og -Ci-salkyl, hvor nævnte -Ci-3alkyl er eventuelt substitueret med en eller flere substituenter uafhængigt valgt fra -OT7, -N(T2)(T3) og en 6-leddet mættet heterocykel; T1, T2 og T3 er hver uafhængigt valgt fra H og -Ci-6alkyl eventuelt substitueret med en eller flere substituenter uafhængigt valgt fra F, -
N(T5)(T6), -OT7, -ST7, cyano, -C( = O)OT7, -C(=O)N(T5)(T6), -OC( = O)N(T5)(T6), -S( = O)2T7, -S( = O)2OT8 og -S( = O)2N(T5)(T6); T4 er -Ci-6alkyl eventuelt substitueret med en eller flere substituenter uafhængigt valgt fra F, -N(T5)(T6), -OT7, -ST7, cyano, -C(=O)OT7, -C( = O)N(T5)(T6), -OC(=O)N(T5)(T6), -S( = O)2T8, -S( = O)2OT7 og -S( = O)2N(T5)(T6); T5, T6 og T7 er hver uafhængigt valgt fra H og -Ci-6alkyl eventuelt substitueret med en eller flere substituenter uafhængigt valgt fra F, amino, hydroxyl, thiol og cyano; og T8 er valgt fra -Ci-6alkyl eventuelt substitueret med en eller flere substituenter uafhængigt valgt fra F, amino, hydroxyl, thiol og cyano; eller et farmaceutisk acceptabelt salt deraf.
2. Forbindelse ifølge krav 1, hvor X1 er valgt fra gruppen bestående af nitro, cyano og trifluormethyl.
3. Forbindelse ifølge krav 1 eller 2, hvor Y1 er en 4- til 7-leddet mættet eller umættet aromatisk carbocykel eller heterocykel, med betingelsen at fastgørelsespunktet på nævnte heterocykel er carbon hvis X4 er -NR4- eller -N(R4)(CH2)-, hvor nævnte 4- til 7-leddede carbocykel eller heterocykel er eventuelt substitueret med en eller flere substituenter uafhængigt valgt fra F, -OT1, -N(T2)(T3), -C( = O)N(T2)(T3), -0( = 0)0^, -ST1, -S^O^T1, -S( = O)2N(T2)(T3), oxo og -Ci-3alkyl, hvor nævnte -Ci-3alkyl er eventuelt substitueret med en eller flere substituenter uafhængigt valgt fra -OT7, -N(T2)(T3) og en 6-leddet mættet heterocykel.
4. Forbindelse ifølge krav 3, hvor Y1 er en 4- til 7-leddet mættet carbocykel eller heterocykel, med betingelsen at fastgørelsespunktet på nævnte heterocykel er carbon hvis X4 er -NR4- eller -N(R4)(CH2)-, hvor nævnte 4- til 7-leddede carbocykel eller heterocykel er eventuelt substitueret med en eller flere substituenter uafhængigt valgt fra F, -OT1, -N(T2)(T3), -C(=O)N(T2)(T3), -C(=O)OT1, -ST1, -S^O^T1, -S(=O)2N(T2)(T3), oxo og -Ci-3alkyl, hvor nævnte -Ci- 3alkyl er eventuelt substitueret med en eller flere substituenter uafhængigt valgt fra -OT7, -N(T2)(T3) og en 6-leddet mættet heterocykel.
5. Forbindelse ifølge krav 3 eller 4, hvor X4 mangler.
6. Forbindelse ifølge krav 1 eller 2, hvor X4 mangler og Y1 er en 6-leddet mættet heterocykel hvor nævnte 6-leddede heterocykel er eventuelt substitueret med en eller flere substituenter uafhængigt valgt fra F, -OT1, -N(T2)(T3), -C(=O)N(T2)(T3), -0(=0)0^, -ST1, -5(=0)2^, -S(=O)2N(T2)(T3), oxo og -Ci-salkyl.
7. Forbindelse ifølge krav 1, hvor nævnte forbindelse er valgt fra gruppen bestående af: 5.6- dibrom-l-ethyl-4-nitro-2-(piperazin-l-yl)-lH-l,3-benzodiazol; 5.6- dibrom-4-nitro-2-(piperazin-l-yl)-l-(propan-2-yl)-lH-l,3-benzodiazol; (3S)-l-(5,6-dibrom-l-ethyl-4-nitro-lH-l,3-benzodiazol-2-yl)piperidin-3-amine; 5,6-dibrom-2-[(2S)-2-methylpiperazin-l-yl]-4-nitro-l-(propan-2-yl)-lH-l,3-benzodiazol; og 5.6- dibrom-4-nitro-2-(piperidin-4-yl)-l-(propan-2-yl)-lH-l,3-benzodiazol.
8. Forbindelse ifølge et hvilket som helst af de foregående krav, hvor det farmaceutisk acceptable salt er valgt fra gruppen bestående af hydrochlorid, hydrobromid, hydroiodid, nitrat, sulfat, bisulfat, phosphat, syrephosphat, isonicotinat, acetat, lactat, salicylat, citrat, tartrat, pantothenat, bitartrat, ascorbat, succinat, maleat, gentisinat, fumarat, gluconat, glucaronat, saccharat, format, benzoat, glutamat, methansulfonat, ethansulfonat, benzensulfonat, p-toluensulfonat og pamoat.
9. Farmaceutisk sammensætning til anvendelse i en fremgangsmåde til behandling med terapi, hvor sammensætningen omfatter en forbindelse af formel (I): 0) hvor X1 er valgt fra gruppen bestående af nitro, cyano, trifluormethyl og -C(=O)OT4; Z og X2 er hver uafhængigt valgt fra gruppen bestående af F, Cl, Br og I; X3 er valgt fra gruppen bestående af -Ci-6alkyl, -C2-6alkenyl, -C2-6alkynyl og en 3- til 6-leddet mættet carbocykel eller heterocykel, med betingelsen at fastgørelsespunktet på nævnte heterocykel er carbon, hvor nævnte 3- til 6-leddede carbocykel eller heterocykel er eventuelt substitueret med en eller flere substituenter uafhængigt valgt fra F, -N(T2)(T3), -C(=O)N(T2)(T3), -0(=0)0^, -ST1, -3(=0)271 og -S(=O)2N(T2)(T3), og hvor nævnte -Ci-6alkyl, -C2-6alkenyl og -C2-6alkynyl er eventuelt substitueret med en eller flere substituenter uafhængigt valgt fra F, -OT1, -N(T2)(T3), - C(=O)N(T2)(T3), -0(=0)0^, -ST1, -S^O^T1, -S(=O)2N(T2)(T3) og en 3- til 6-leddet mættet carbocykel eller heterocykel, hvor nævnte 3- til 6-leddede carbocykel eller heterocykel er eventuelt substitueret med en eller flere substituenter uafhængigt valgt fra F, -OT1, -N(T2)(T3), -C(=O)N(T2)(T3), -0(=0)0^, -ST1, -3( = 0)271 og -S( = O)2N(T2)(T3); X4 enten mangler eller valgt fra -NR4- og -N(R4)(CH2)-; R4 er valgt fra H og -Ci-6alkyl; Y1 er valgt fra gruppen bestående af H, -Ci-6alkyl og en 4- til 7-leddet mættet eller umættet aromatisk carbocykel eller heterocykel, med betingelsen at fastgørelsespunktet på nævnte heterocykel er carbon hvis X4 er -NR4- eller -N(R4)(CH2)-, hvor nævnte -Ci-6alkyl er eventuelt substitueret med en eller flere substituenter uafhængigt valgt fra F, -OT1, -N(T2)(T3), -C( = O)N(T2)(T3), -0(=0)0^, -ST1, -S^O^T1, -S( = O)2N(T2)(T3) og en 5- til 6-leddet mættet heterocykel, og hvor nævnte 4- til 7-leddede
carbocykel eller heterocykel er eventuelt substitueret med en eller flere substituenter uafhængigt valgt fra F, -OT1, -N(T2)(T3), -C(=O)N(T2)(T3), -0(=0)0^, -ST1, -5(=0)2^, -S(=O)2N(T2)(T3), oxo og -Ci-salkyl, hvor nævnte -Ci-3alkyl er eventuelt substitueret med en eller flere substituenter uafhængigt valgt fra -OT7, -N(T2)(T3) og en 6-leddet mættet heterocykel; T1, T2 og T3 er hver uafhængigt valgt fra H og -Ci-6alkyl eventuelt substitueret med en eller flere substituenter uafhængigt valgt fra F, -N(T5)(T6), -OT7, -ST7, cyano, -C( = O)OT7, -C( = O)N(T5)(T6), -OC( = O)N(T5)(T6), -S( = O)2T7, -S( = O)2OT8 og -S( = O)2N(T5)(T6); T4 er -Ci-6alkyl eventuelt substitueret med en eller flere substituenter uafhængigt valgt fra F, -N(T5)(T6), -OT7, -ST7, cyano, -C(=O)OT7, -C( = O)N(T5)(T6), -OC(=O)N(T5)(T6), -S( = O)2T8, -S( = O)2OT7 og -S( = O)2N(T5)(T6); T5, T6 og T7 er hver uafhængigt valgt fra H og -Ci-6alkyl eventuelt substitueret med en eller flere substituenter uafhængigt valgt fra F, amino, hydroxyl, thiol og cyano; og T8 er valgt fra -Ci-6alkyl eventuelt substitueret med en eller flere substituenter uafhængigt valgt fra F, amino, hydroxyl, thiol og cyano; eller et farmaceutisk acceptabelt salt deraf.
10. Farmaceutisk sammensætning til anvendelse ifølge krav 9, hvor sammensætningen er til anvendelse i behandlingen af en sygdom valgt fra gruppen bestående af cancer, en autoimmun sygdom og en inflammatorisk sygdom.
11. Farmaceutisk sammensætning til anvendelse ifølge krav 9 eller 10, hvor sammensætningen er til anvendelse i behandlingen af en sygdom valgt fra gruppen bestående af leukæmier, inkluderende akut lymfoblastisk leukæmi, akut myeloid leukæmi og kronisk lymfatisk leukæmi, lymfom inkluderende diffust storcellet B-celle lymfom, myelom inkluderende multipel myelom, myeloproliferativ lidelse, allograft afstødning, inflammatorisk tarmsygdom, multipel sklerose, psoriasis, rheumatoid arthritis, systemisk lupus erythematosus, Alzheimers sygdom og Downs syndrom.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB1223265.8A GB201223265D0 (en) | 2012-12-21 | 2012-12-21 | Novel benzimidazole derivatives as kinase inhibitors |
PCT/EP2013/077754 WO2014096388A2 (en) | 2012-12-21 | 2013-12-20 | Novel benzimidazole derivatives as kinase inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
DK2935244T3 true DK2935244T3 (da) | 2018-09-10 |
Family
ID=47682482
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DK13811246.1T DK2935244T3 (da) | 2012-12-21 | 2013-12-20 | Hidtil ukendte benzimidazol-derivater som kinase-inhibitorer |
Country Status (22)
Country | Link |
---|---|
US (2) | US9388192B2 (da) |
EP (1) | EP2935244B1 (da) |
JP (1) | JP6169185B2 (da) |
KR (1) | KR101779272B1 (da) |
CN (1) | CN104936951B (da) |
AU (1) | AU2013366513B2 (da) |
BR (1) | BR112015014701B8 (da) |
CA (1) | CA2896156C (da) |
CY (1) | CY1120692T1 (da) |
DK (1) | DK2935244T3 (da) |
ES (1) | ES2688395T3 (da) |
GB (1) | GB201223265D0 (da) |
HR (1) | HRP20181429T8 (da) |
HU (1) | HUE039376T2 (da) |
IL (1) | IL239193A0 (da) |
LT (1) | LT2935244T (da) |
MX (1) | MX369589B (da) |
PL (1) | PL2935244T3 (da) |
PT (1) | PT2935244T (da) |
RS (1) | RS57658B1 (da) |
SI (1) | SI2935244T1 (da) |
WO (1) | WO2014096388A2 (da) |
Families Citing this family (23)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB201223265D0 (en) | 2012-12-21 | 2013-02-06 | Selvita Sa | Novel benzimidazole derivatives as kinase inhibitors |
BR112016016289B1 (pt) | 2014-01-14 | 2023-02-07 | Takeda Pharmaceutical Company Limited | Heteroaris e usos dos mesmos |
WO2015108881A1 (en) | 2014-01-14 | 2015-07-23 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
TW202140422A (zh) | 2014-10-06 | 2021-11-01 | 美商維泰克斯製藥公司 | 囊腫纖維化症跨膜傳導調節蛋白之調節劑 |
AU2016315881B2 (en) * | 2015-09-03 | 2019-09-19 | The Arizona Board Of Regents On Behalf Of The University Of Arizona | Small molecule inhibitors of DYRK1A and uses thereof |
CA3019380A1 (en) | 2016-03-31 | 2017-10-05 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
CN109803962B (zh) | 2016-09-30 | 2022-04-29 | 弗特克斯药品有限公司 | 囊性纤维化跨膜传导调控蛋白的调节剂、以及药物组合物 |
HUE052205T2 (hu) | 2016-12-09 | 2021-04-28 | Vertex Pharma | Cisztás fibrózis transzmembrán vezetõképesség szabályzó modulátora, gyógyszerészeti készítmények, kezelési eljárások és eljárás a modulátor elõállítására |
US9855255B1 (en) | 2017-05-26 | 2018-01-02 | King Saud University | Substituted naphthyridinyl hydrazines as anti-liver cancer agents |
US11253509B2 (en) | 2017-06-08 | 2022-02-22 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
BR112020000941A2 (pt) | 2017-07-17 | 2020-07-21 | Vertex Pharmaceuticals Incorporated | métodos de tratamento para fibrose cística |
US11434201B2 (en) | 2017-08-02 | 2022-09-06 | Vertex Pharmaceuticals Incorporated | Processes for preparing pyrrolidine compounds |
KR20200074965A (ko) | 2017-10-19 | 2020-06-25 | 암젠 인크 | 벤즈이미다졸 유도체 및 이의 용도 |
WO2019079760A1 (en) | 2017-10-19 | 2019-04-25 | Vertex Pharmaceuticals Incorporated | CRYSTALLINE FORMS AND COMPOSITIONS OF CFTR MODULATORS |
WO2019113476A2 (en) | 2017-12-08 | 2019-06-13 | Vertex Pharmaceuticals Incorporated | Processes for making modulators of cystic fibrosis transmembrane conductance regulator |
TWI810243B (zh) | 2018-02-05 | 2023-08-01 | 美商維泰克斯製藥公司 | 用於治療囊腫纖化症之醫藥組合物 |
US11414439B2 (en) | 2018-04-13 | 2022-08-16 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator |
KR20210059663A (ko) * | 2019-11-15 | 2021-05-25 | 가천대학교 산학협력단 | 신규한 벤즈이미다졸 유도체 및 이의 용도 |
CN113491691B (zh) * | 2020-04-02 | 2023-04-14 | 深圳贝瑞生物医药科技有限公司 | 一种用于制备抗肿瘤药物或14-3-3η蛋白抑制剂的化合物 |
KR20210131855A (ko) * | 2020-04-23 | 2021-11-03 | 런엑스 주식회사 | R-point 조절 단백질 복합체를 유효성분으로 포함하는 폐암 치료용 약학적 조성물, 상기 복합체의 형성 여부를 이용한 폐암 치료제 스크리닝 방법 및 폐암 진단 방법 |
WO2023241627A1 (en) * | 2022-06-15 | 2023-12-21 | Insilico Medicine Ip Limited | Cdk8/19 dual inhibitors and methods of use thereof |
WO2024023279A1 (en) | 2022-07-29 | 2024-02-01 | Ryvu Therapeutics S.A. | Cancer combination therapy including a bcl-2 inhibitor |
WO2024023278A1 (en) | 2022-07-29 | 2024-02-01 | Ryvu Therapeutics S.A. | Cancer combination therapy including a flt3-inhibitor |
Family Cites Families (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR1469504A (fr) * | 1964-10-22 | 1967-02-17 | Fisons Pest Control Ltd | Composés insecticides |
GB1122988A (en) | 1964-10-22 | 1968-08-07 | Fisons Pest Control Ltd | Benzimidazole derivatives |
DE3227893A1 (de) * | 1982-07-26 | 1984-01-26 | Macherey-Nagel & Co Chemikalienhandel, 5160 Düren | Verwendung von benzimidazolderivaten zum nachweis von blut und anderen peroxidatisch wirksamen substanzen in koerperfluessigkeiten und ausscheidungsprodukten, insbesondere als diagnostikum in form eines testpapiers |
GB9600142D0 (en) | 1996-01-05 | 1996-03-06 | Wellcome Found | Chemical compounds |
AU744939B2 (en) * | 1997-09-26 | 2002-03-07 | Merck & Co., Inc. | Novel angiogenesis inhibitors |
CZ300148B6 (cs) * | 1998-11-27 | 2009-02-25 | Abbott Gmbh & Co. Kg | Derivát substituovaného benzimidazolu, zpusob jeho prípravy a jeho použití |
WO2003020698A2 (en) * | 2001-09-06 | 2003-03-13 | Prochon Biotech Ltd. | Protein tyrosine kinase inhibitors |
US20090131470A1 (en) * | 2005-06-11 | 2009-05-21 | Vernalis R & D Limited | Pyrazole-substituted benzimidazole derivatives for use in the treatment of cancer and autoimmune disorders |
CN102448458B (zh) * | 2009-03-18 | 2015-07-22 | 小利兰·斯坦福大学理事会 | 治疗黄病毒科病毒感染的方法和组合物 |
BR112012011109A2 (pt) * | 2009-11-12 | 2019-09-24 | Selvita S A | um composto um processo para sua preparação uma composição farmaceutica uso de um composto um metodo modular ou regular serina treonina quinases |
EA201590482A1 (ru) | 2012-09-05 | 2015-07-30 | Байер Кропсайенс Аг | Применение замещенных 2-амидобензимидазолов, 2-амидобензоксазолов и 2-амидобензотиазолов или их солей в качестве биологически активных веществ против абиотического стресса растений |
GB201223265D0 (en) | 2012-12-21 | 2013-02-06 | Selvita Sa | Novel benzimidazole derivatives as kinase inhibitors |
-
2012
- 2012-12-21 GB GBGB1223265.8A patent/GB201223265D0/en not_active Ceased
-
2013
- 2013-12-20 BR BR112015014701A patent/BR112015014701B8/pt active IP Right Grant
- 2013-12-20 RS RS20181052A patent/RS57658B1/sr unknown
- 2013-12-20 US US14/654,779 patent/US9388192B2/en active Active
- 2013-12-20 CN CN201380067040.1A patent/CN104936951B/zh active Active
- 2013-12-20 SI SI201331149T patent/SI2935244T1/sl unknown
- 2013-12-20 LT LTEP13811246.1T patent/LT2935244T/lt unknown
- 2013-12-20 JP JP2015548646A patent/JP6169185B2/ja active Active
- 2013-12-20 WO PCT/EP2013/077754 patent/WO2014096388A2/en active Application Filing
- 2013-12-20 CA CA2896156A patent/CA2896156C/en active Active
- 2013-12-20 DK DK13811246.1T patent/DK2935244T3/da active
- 2013-12-20 ES ES13811246.1T patent/ES2688395T3/es active Active
- 2013-12-20 HU HUE13811246A patent/HUE039376T2/hu unknown
- 2013-12-20 PT PT13811246T patent/PT2935244T/pt unknown
- 2013-12-20 EP EP13811246.1A patent/EP2935244B1/en active Active
- 2013-12-20 MX MX2015007057A patent/MX369589B/es active IP Right Grant
- 2013-12-20 PL PL13811246T patent/PL2935244T3/pl unknown
- 2013-12-20 AU AU2013366513A patent/AU2013366513B2/en active Active
- 2013-12-20 KR KR1020157019215A patent/KR101779272B1/ko active IP Right Grant
-
2015
- 2015-06-03 IL IL239193A patent/IL239193A0/en active IP Right Grant
-
2016
- 2016-06-10 US US15/179,601 patent/US10174013B2/en active Active
-
2018
- 2018-09-06 HR HRP20181429TT patent/HRP20181429T8/hr unknown
- 2018-09-20 CY CY181100977T patent/CY1120692T1/el unknown
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
DK2935244T3 (da) | Hidtil ukendte benzimidazol-derivater som kinase-inhibitorer | |
ES2855135T3 (es) | Amidas heterocíclicas como inhibidores de quinasa | |
EP2499117B1 (en) | A compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine kinases and a serine/threonine kinases modulating agent | |
WO2018023029A1 (en) | Small molecule activators of parkin enzyme function | |
TW200829583A (en) | Anilinopiperazine derivatives and methods of use thereof | |
EP2167489A2 (en) | Pyrimidine derivatives useful as raf kinase inhibitors | |
BRPI0618520A2 (pt) | imidazopirazinas como inibidores de proteìna cinase | |
BRPI0614472A2 (pt) | compostos e composições como inibidores de proteìna quinase | |
EP3596084A1 (en) | 9,10,11,12-tetrahydro-8h-[1,4]diazepino[5',6':4,5]thieno[3,2-f]quinolin-8-one compounds and uses thereof | |
ES2930106T3 (es) | Compuesto derivado de pirrol-piridina, procedimiento para preparar el mismo y composición farmacéutica que contiene el mismo como ingrediente activo para la prevención o el tratamiento de enfermedades relacionadas con la proteína quinasa | |
DK2817301T3 (da) | Anvendelse af 1H-indazol-3-carboxamidforbindelser som glykogen-syntase-kinase 3-beta hæmmere | |
US10351578B2 (en) | Heterocyclic-substituted pyridinopyrimidinone derivative as CDK inhibitor and use thereof | |
AU2015274285C1 (en) | Pyrimidine compounds and methods using the same | |
PT1781639E (pt) | Derivados de indolil alquil amina substituídos como novos inibidores de histona-desacetilase | |
Patel | Design synthesis and biological evaluation of bioisosteric analogues of dasatinib as Src, Abl and Abl T3151 protein tyrosine kinase inhibitors |